Ligand source activities (1 row/activity)



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Ligands (move mouse cursor over ligand name to see structure) Receptor Activity Chemical information
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 Activity
Type		 Activity
Relation		 Activity
Value		 p-value
(-log)		 Fold
selectivity		 Tested
GPCRs		 Assay
Description		 Source

 Mol
weight		 Rot
Bonds		 H don

 H acc

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 DOI
168278159 190360 None 0 Human Functional pEC50 = 9.5 9.5 23 4
Agonist activity at A2BR in human NHVCF cells assessed as cAMP accumulation incubated for 30 mins by LANCE cAMP assayAgonist activity at A2BR in human NHVCF cells assessed as cAMP accumulation incubated for 30 mins by LANCE cAMP assay
ChEMBL 839 15 5 15 6.6 Nc1sc(-c2ccc(-c3cn(CCCCCCNc4ncnc5c4ncn5[C@@H]4O[C@H](CO)[C@@H](O)[C@H]4O)nn3)cc2)c(-c2cccc(C(F)(F)F)c2)c1C(=O)c1ccccc1 10.1021/acs.jmedchem.2c00320
CHEMBL5177040 190360 None 0 Human Functional pEC50 = 9.5 9.5 23 4
Agonist activity at A2BR in human NHVCF cells assessed as cAMP accumulation incubated for 30 mins by LANCE cAMP assayAgonist activity at A2BR in human NHVCF cells assessed as cAMP accumulation incubated for 30 mins by LANCE cAMP assay
ChEMBL 839 15 5 15 6.6 Nc1sc(-c2ccc(-c3cn(CCCCCCNc4ncnc5c4ncn5[C@@H]4O[C@H](CO)[C@@H](O)[C@H]4O)nn3)cc2)c(-c2cccc(C(F)(F)F)c2)c1C(=O)c1ccccc1 10.1021/acs.jmedchem.2c00320
168278159 190360 None 0 Human Functional pEC50 = 9.4 9.4 23 4
Agonist activity at human A2B receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 10 mins in presence of forskolin by LANCE cAMP assayAgonist activity at human A2B receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 10 mins in presence of forskolin by LANCE cAMP assay
ChEMBL 839 15 5 15 6.6 Nc1sc(-c2ccc(-c3cn(CCCCCCNc4ncnc5c4ncn5[C@@H]4O[C@H](CO)[C@@H](O)[C@H]4O)nn3)cc2)c(-c2cccc(C(F)(F)F)c2)c1C(=O)c1ccccc1 10.1021/acs.jmedchem.2c00320
CHEMBL5177040 190360 None 0 Human Functional pEC50 = 9.4 9.4 23 4
Agonist activity at human A2B receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 10 mins in presence of forskolin by LANCE cAMP assayAgonist activity at human A2B receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 10 mins in presence of forskolin by LANCE cAMP assay
ChEMBL 839 15 5 15 6.6 Nc1sc(-c2ccc(-c3cn(CCCCCCNc4ncnc5c4ncn5[C@@H]4O[C@H](CO)[C@@H](O)[C@H]4O)nn3)cc2)c(-c2cccc(C(F)(F)F)c2)c1C(=O)c1ccccc1 10.1021/acs.jmedchem.2c00320
9975036 16328 None 0 Human Functional pEC50 = 8 8.0 - 1
Agonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as increase in cAMP productionAgonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as increase in cAMP production
ChEMBL 348 4 3 7 2.8 N#Cc1c(N)nc(SCc2ncc[nH]2)c(C#N)c1-c1cccc(O)c1 10.1021/acs.jmedchem.6b00552
CHEMBL122806 16328 None 0 Human Functional pEC50 = 8 8.0 - 1
Agonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as increase in cAMP productionAgonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as increase in cAMP production
ChEMBL 348 4 3 7 2.8 N#Cc1c(N)nc(SCc2ncc[nH]2)c(C#N)c1-c1cccc(O)c1 10.1021/acs.jmedchem.6b00552
9975036 16328 None 0 Human Functional pEC50 = 8 8.0 - 1
Agonistic activity against human adenosine A2B receptor expressed in CHO cellsAgonistic activity against human adenosine A2B receptor expressed in CHO cells
ChEMBL 348 4 3 7 2.8 N#Cc1c(N)nc(SCc2ncc[nH]2)c(C#N)c1-c1cccc(O)c1 10.1021/jm049947s
CHEMBL122806 16328 None 0 Human Functional pEC50 = 8 8.0 - 1
Agonistic activity against human adenosine A2B receptor expressed in CHO cellsAgonistic activity against human adenosine A2B receptor expressed in CHO cells
ChEMBL 348 4 3 7 2.8 N#Cc1c(N)nc(SCc2ncc[nH]2)c(C#N)c1-c1cccc(O)c1 10.1021/jm049947s
71657835 159737 None 3 Human Functional pEC50 = 8.0 8.0 -1 4
Agonist activity at A2BR in human NHVCF cells assessed as cAMP accumulation incubated for 30 mins by LANCE cAMP assayAgonist activity at A2BR in human NHVCF cells assessed as cAMP accumulation incubated for 30 mins by LANCE cAMP assay
ChEMBL 815 15 6 13 6.1 Nc1sc(-c2ccc(C(=O)NCCCCCCNc3ncnc4c3ncn4[C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)cc2)c(-c2cccc(C(F)(F)F)c2)c1C(=O)c1ccccc1 10.1021/acs.jmedchem.2c00320
CHEMBL4104819 159737 None 3 Human Functional pEC50 = 8.0 8.0 -1 4
Agonist activity at A2BR in human NHVCF cells assessed as cAMP accumulation incubated for 30 mins by LANCE cAMP assayAgonist activity at A2BR in human NHVCF cells assessed as cAMP accumulation incubated for 30 mins by LANCE cAMP assay
ChEMBL 815 15 6 13 6.1 Nc1sc(-c2ccc(C(=O)NCCCCCCNc3ncnc4c3ncn4[C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)cc2)c(-c2cccc(C(F)(F)F)c2)c1C(=O)c1ccccc1 10.1021/acs.jmedchem.2c00320
44423814 142098 None 0 Human Functional pEC50 = 8.0 8.0 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 611 9 5 11 2.1 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(Nc4ccc(OCC(=O)Nc5ccc(Br)cc5)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1016/j.bmc.2007.01.055
CHEMBL388193 142098 None 0 Human Functional pEC50 = 8.0 8.0 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 611 9 5 11 2.1 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(Nc4ccc(OCC(=O)Nc5ccc(Br)cc5)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1016/j.bmc.2007.01.055
9869857 66830 None 11 Human Functional pEC50 = 6 6.0 -213 5
Potency against cAMP formation in CHO cells expressing recombinant human A2B receptorPotency against cAMP formation in CHO cells expressing recombinant human A2B receptor
ChEMBL 482 8 5 14 -0.6 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(N[C@H](CO)Cc5ccccc5)nc43)[C@H](O)[C@@H]2O)n1 10.1021/jm031143+
CHEMBL186113 66830 None 11 Human Functional pEC50 = 6 6.0 -213 5
Potency against cAMP formation in CHO cells expressing recombinant human A2B receptorPotency against cAMP formation in CHO cells expressing recombinant human A2B receptor
ChEMBL 482 8 5 14 -0.6 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(N[C@H](CO)Cc5ccccc5)nc43)[C@H](O)[C@@H]2O)n1 10.1021/jm031143+
49870952 58820 None 0 Human Functional pEC50 = 5 5.0 -831 2
Agonist activity at human adenosine A2B receptor expressed in CHO cells by cyclic AMP functional assayAgonist activity at human adenosine A2B receptor expressed in CHO cells by cyclic AMP functional assay
ChEMBL 333 3 3 8 0.9 CCCCC#Cc1nc(N)c2ncn([C@@H]3SC[C@@H](O)[C@H]3O)c2n1 10.1021/ml1001823
CHEMBL1688378 58820 None 0 Human Functional pEC50 = 5 5.0 -831 2
Agonist activity at human adenosine A2B receptor expressed in CHO cells by cyclic AMP functional assayAgonist activity at human adenosine A2B receptor expressed in CHO cells by cyclic AMP functional assay
ChEMBL 333 3 3 8 0.9 CCCCC#Cc1nc(N)c2ncn([C@@H]3SC[C@@H](O)[C@H]3O)c2n1 10.1021/ml1001823
219024 3300 None 65 Human Functional pEC50 = 5 5.0 -51 5
Agonist activity at human recombinant adenosine receptor A2b by cAMP assayAgonist activity at human recombinant adenosine receptor A2b by cAMP assay
ChEMBL 390 4 5 12 -2.4 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(nc2N)n1ncc(c1)C(=O)NC 10.1021/jm4011669
219024.0 3300 None 65 Human Functional pEC50 = 5 5.0 -51 5
Agonist activity at human recombinant adenosine receptor A2b by cAMP assayAgonist activity at human recombinant adenosine receptor A2b by cAMP assay
ChEMBL 390 4 5 12 -2.4 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(nc2N)n1ncc(c1)C(=O)NC 10.1021/jm4011669
2362 3300 None 65 Human Functional pEC50 = 5 5.0 -51 5
Agonist activity at human recombinant adenosine receptor A2b by cAMP assayAgonist activity at human recombinant adenosine receptor A2b by cAMP assay
ChEMBL 390 4 5 12 -2.4 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(nc2N)n1ncc(c1)C(=O)NC 10.1021/jm4011669
5596 3300 None 65 Human Functional pEC50 = 5 5.0 -51 5
Agonist activity at human recombinant adenosine receptor A2b by cAMP assayAgonist activity at human recombinant adenosine receptor A2b by cAMP assay
ChEMBL 390 4 5 12 -2.4 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(nc2N)n1ncc(c1)C(=O)NC 10.1021/jm4011669
CHEMBL317052 3300 None 65 Human Functional pEC50 = 5 5.0 -51 5
Agonist activity at human recombinant adenosine receptor A2b by cAMP assayAgonist activity at human recombinant adenosine receptor A2b by cAMP assay
ChEMBL 390 4 5 12 -2.4 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(nc2N)n1ncc(c1)C(=O)NC 10.1021/jm4011669
DB06213 3300 None 65 Human Functional pEC50 = 5 5.0 -51 5
Agonist activity at human recombinant adenosine receptor A2b by cAMP assayAgonist activity at human recombinant adenosine receptor A2b by cAMP assay
ChEMBL 390 4 5 12 -2.4 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(nc2N)n1ncc(c1)C(=O)NC 10.1021/jm4011669
9910098 70683 None 31 Human Functional pEC50 = 5 5.0 - 1
Agonist activity at human recombinant adenosine receptor A2b by cAMP assayAgonist activity at human recombinant adenosine receptor A2b by cAMP assay
ChEMBL 421 6 4 10 0.3 Nc1nc(OCCc2ccc(Cl)cc2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm4011669
CHEMBL1950553 70683 None 31 Human Functional pEC50 = 5 5.0 - 1
Agonist activity at human recombinant adenosine receptor A2b by cAMP assayAgonist activity at human recombinant adenosine receptor A2b by cAMP assay
ChEMBL 421 6 4 10 0.3 Nc1nc(OCCc2ccc(Cl)cc2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm4011669
118732976 118517 None 0 Human Functional pEC50 = 6 6.0 -213 4
Agonist activity at human recombinant adenosine A2B receptor transfected in CHO cells assessed as induction of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2B receptor transfected in CHO cells assessed as induction of adenylyl cyclase activity
ChEMBL 427 5 3 12 0.4 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N[C@H]5C[C@@H]6CC[C@@H]5C6)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.5b00074
CHEMBL3414942 118517 None 0 Human Functional pEC50 = 6 6.0 -213 4
Agonist activity at human recombinant adenosine A2B receptor transfected in CHO cells assessed as induction of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2B receptor transfected in CHO cells assessed as induction of adenylyl cyclase activity
ChEMBL 427 5 3 12 0.4 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N[C@H]5C[C@@H]6CC[C@@H]5C6)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.5b00074
377 2758 None 53 Human Functional pEC50 = 7.0 7.0 -48 10
Agonistic activity against human adenosine A2B receptor expressed in CHO cellsAgonistic activity against human adenosine A2B receptor expressed in CHO cells
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm049947s
425 2758 None 53 Human Functional pEC50 = 7.0 7.0 -48 10
Agonistic activity against human adenosine A2B receptor expressed in CHO cellsAgonistic activity against human adenosine A2B receptor expressed in CHO cells
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm049947s
448222 2758 None 53 Human Functional pEC50 = 7.0 7.0 -48 10
Agonistic activity against human adenosine A2B receptor expressed in CHO cellsAgonistic activity against human adenosine A2B receptor expressed in CHO cells
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm049947s
CHEMBL464859 2758 None 53 Human Functional pEC50 = 7.0 7.0 -48 10
Agonistic activity against human adenosine A2B receptor expressed in CHO cellsAgonistic activity against human adenosine A2B receptor expressed in CHO cells
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm049947s
44423816 85218 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 601 9 5 11 2.4 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(Nc4ccc(OCC(=O)Nc5ccccc5C(F)(F)F)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1016/j.bmc.2007.01.055
CHEMBL225579 85218 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 601 9 5 11 2.4 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(Nc4ccc(OCC(=O)Nc5ccccc5C(F)(F)F)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1016/j.bmc.2007.01.055
16203542 85198 None 0 Human Functional pEC50 = 7.0 7.0 -3 2
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 504 6 5 10 0.9 Nc1nc(OCCc2c[nH]c3cc(Br)ccc23)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm061278q
CHEMBL225459 85198 None 0 Human Functional pEC50 = 7.0 7.0 -3 2
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 504 6 5 10 0.9 Nc1nc(OCCc2c[nH]c3cc(Br)ccc23)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm061278q
145965471 164176 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assayAgonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assay
ChEMBL 376 6 2 7 3.5 CCOc1ccc(-c2c(C#N)c(N)nc(SCc3ncc[nH]3)c2C#N)cc1 10.1016/j.ejmech.2018.02.081
CHEMBL4210592 164176 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assayAgonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assay
ChEMBL 376 6 2 7 3.5 CCOc1ccc(-c2c(C#N)c(N)nc(SCc3ncc[nH]3)c2C#N)cc1 10.1016/j.ejmech.2018.02.081
377 2758 None 53 Human Functional pEC50 = 7.0 7.0 -48 10
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm061278q
425 2758 None 53 Human Functional pEC50 = 7.0 7.0 -48 10
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm061278q
448222 2758 None 53 Human Functional pEC50 = 7.0 7.0 -48 10
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm061278q
CHEMBL464859 2758 None 53 Human Functional pEC50 = 7.0 7.0 -48 10
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm061278q
137659441 159099 None 0 Human Functional pEC50 = 6.0 6.0 -87 4
Agonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assayAgonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assay
ChEMBL 441 6 3 12 0.6 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5cccc(F)c5)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
CHEMBL4097468 159099 None 0 Human Functional pEC50 = 6.0 6.0 -87 4
Agonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assayAgonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assay
ChEMBL 441 6 3 12 0.6 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5cccc(F)c5)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
123683 3121 None 63 Human Functional pEC50 = 5.0 5.0 -1258 5
Effective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNAEffective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNA
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1021/jm9804984
422 3121 None 63 Human Functional pEC50 = 5.0 5.0 -1258 5
Effective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNAEffective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNA
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1021/jm9804984
CHEMBL119709 3121 None 63 Human Functional pEC50 = 5.0 5.0 -1258 5
Effective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNAEffective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNA
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1021/jm9804984
DB05511 3121 None 63 Human Functional pEC50 = 5.0 5.0 -1258 5
Effective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNAEffective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNA
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1021/jm9804984
118732981 118522 None 0 Human Functional pEC50 = 6.0 6.0 -38 4
Agonist activity at human recombinant adenosine A2B receptor transfected in CHO cells assessed as induction of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2B receptor transfected in CHO cells assessed as induction of adenylyl cyclase activity
ChEMBL 495 5 3 12 2.0 CCn1nnc([C@H]2O[C@@H](n3cnc4c(Nc5ccc(Cl)cc5F)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.5b00074
CHEMBL3414947 118522 None 0 Human Functional pEC50 = 6.0 6.0 -38 4
Agonist activity at human recombinant adenosine A2B receptor transfected in CHO cells assessed as induction of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2B receptor transfected in CHO cells assessed as induction of adenylyl cyclase activity
ChEMBL 495 5 3 12 2.0 CCn1nnc([C@H]2O[C@@H](n3cnc4c(Nc5ccc(Cl)cc5F)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.5b00074
11352497 122967 None 0 Human Functional pEC50 = 5.9 5.9 -416 3
Relative efficacy against phenylephrine precontracted tissue relaxation in Guinea pig aortaRelative efficacy against phenylephrine precontracted tissue relaxation in Guinea pig aorta
ChEMBL 498 8 6 15 -0.9 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(N[C@H](CO)Cc5ccc(O)cc5)nc43)[C@H](O)[C@@H]2O)n1 10.1021/jm031143+
CHEMBL360837 122967 None 0 Human Functional pEC50 = 5.9 5.9 -416 3
Relative efficacy against phenylephrine precontracted tissue relaxation in Guinea pig aortaRelative efficacy against phenylephrine precontracted tissue relaxation in Guinea pig aorta
ChEMBL 498 8 6 15 -0.9 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(N[C@H](CO)Cc5ccc(O)cc5)nc43)[C@H](O)[C@@H]2O)n1 10.1021/jm031143+
118732975 118516 None 0 Human Functional pEC50 = 5.9 5.9 -173 4
Agonist activity at human recombinant adenosine A2B receptor transfected in CHO cells assessed as induction of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2B receptor transfected in CHO cells assessed as induction of adenylyl cyclase activity
ChEMBL 407 5 3 12 0.1 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NC5CC5)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.5b00074
CHEMBL3414941 118516 None 0 Human Functional pEC50 = 5.9 5.9 -173 4
Agonist activity at human recombinant adenosine A2B receptor transfected in CHO cells assessed as induction of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2B receptor transfected in CHO cells assessed as induction of adenylyl cyclase activity
ChEMBL 407 5 3 12 0.1 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NC5CC5)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.5b00074
132991435 180798 None 0 Human Functional pEC50 = 6.9 6.9 -123 4
Irreversible agonist activity at human adenosine A2B receptor expressed in Flp-In-CHO cells assessed as effect on forskolin-induced cAMP accumulation incubated for 30 mins by LANCE cAMP detection assayIrreversible agonist activity at human adenosine A2B receptor expressed in Flp-In-CHO cells assessed as effect on forskolin-induced cAMP accumulation incubated for 30 mins by LANCE cAMP detection assay
ChEMBL 558 8 5 12 0.8 O=C(NCc1ccc(Nc2ncnc3c2ncn3[C@@H]2O[C@H](CO)[C@@H](O)[C@H]2O)cc1)c1ccc(S(=O)(=O)F)cc1 10.1021/acs.jmedchem.6b01561
CHEMBL4756472 180798 None 0 Human Functional pEC50 = 6.9 6.9 -123 4
Irreversible agonist activity at human adenosine A2B receptor expressed in Flp-In-CHO cells assessed as effect on forskolin-induced cAMP accumulation incubated for 30 mins by LANCE cAMP detection assayIrreversible agonist activity at human adenosine A2B receptor expressed in Flp-In-CHO cells assessed as effect on forskolin-induced cAMP accumulation incubated for 30 mins by LANCE cAMP detection assay
ChEMBL 558 8 5 12 0.8 O=C(NCc1ccc(Nc2ncnc3c2ncn3[C@@H]2O[C@H](CO)[C@@H](O)[C@H]2O)cc1)c1ccc(S(=O)(=O)F)cc1 10.1021/acs.jmedchem.6b01561
57388054 75483 None 0 Human Functional pEC50 = 5.9 5.9 -17 4
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 607 12 5 10 3.5 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(NCCc4ccccc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm300206u
CHEMBL2042305 75483 None 0 Human Functional pEC50 = 5.9 5.9 -17 4
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 607 12 5 10 3.5 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(NCCc4ccccc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm300206u
135543624 16309 None 28 Human Functional pEC50 = 7.9 7.9 - 1
Agonistic activity against human adenosine A2B receptor expressed in CHO cellsAgonistic activity against human adenosine A2B receptor expressed in CHO cells
ChEMBL 348 4 3 7 2.8 N#Cc1c(N)nc(SCc2ncc[nH]2)c(C#N)c1-c1ccc(O)cc1 10.1021/jm049947s
CHEMBL122622 16309 None 28 Human Functional pEC50 = 7.9 7.9 - 1
Agonistic activity against human adenosine A2B receptor expressed in CHO cellsAgonistic activity against human adenosine A2B receptor expressed in CHO cells
ChEMBL 348 4 3 7 2.8 N#Cc1c(N)nc(SCc2ncc[nH]2)c(C#N)c1-c1ccc(O)cc1 10.1021/jm049947s
377 2758 None 53 Human Functional pEC50 = 7.9 7.9 -48 10
Agonist activity at A2BR in human NHVCF cells assessed as cAMP accumulation incubated for 30 mins by LANCE cAMP assayAgonist activity at A2BR in human NHVCF cells assessed as cAMP accumulation incubated for 30 mins by LANCE cAMP assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.2c00320
425 2758 None 53 Human Functional pEC50 = 7.9 7.9 -48 10
Agonist activity at A2BR in human NHVCF cells assessed as cAMP accumulation incubated for 30 mins by LANCE cAMP assayAgonist activity at A2BR in human NHVCF cells assessed as cAMP accumulation incubated for 30 mins by LANCE cAMP assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.2c00320
448222 2758 None 53 Human Functional pEC50 = 7.9 7.9 -48 10
Agonist activity at A2BR in human NHVCF cells assessed as cAMP accumulation incubated for 30 mins by LANCE cAMP assayAgonist activity at A2BR in human NHVCF cells assessed as cAMP accumulation incubated for 30 mins by LANCE cAMP assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.2c00320
CHEMBL464859 2758 None 53 Human Functional pEC50 = 7.9 7.9 -48 10
Agonist activity at A2BR in human NHVCF cells assessed as cAMP accumulation incubated for 30 mins by LANCE cAMP assayAgonist activity at A2BR in human NHVCF cells assessed as cAMP accumulation incubated for 30 mins by LANCE cAMP assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.2c00320
44423813 168749 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 567 9 5 11 2.0 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(Nc4ccc(OCC(=O)Nc5ccc(Cl)cc5)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1016/j.bmc.2007.01.055
CHEMBL437168 168749 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 567 9 5 11 2.0 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(Nc4ccc(OCC(=O)Nc5ccc(Cl)cc5)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1016/j.bmc.2007.01.055
145974358 164489 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assayAgonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assay
ChEMBL 455 8 2 7 4.3 N#Cc1c(N)nc(SCc2cccc(C(N)=O)c2)c(C#N)c1-c1ccc(OCC2CC2)cc1 10.1016/j.ejmech.2018.02.081
CHEMBL4214347 164489 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assayAgonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assay
ChEMBL 455 8 2 7 4.3 N#Cc1c(N)nc(SCc2cccc(C(N)=O)c2)c(C#N)c1-c1ccc(OCC2CC2)cc1 10.1016/j.ejmech.2018.02.081
57387596 75489 None 0 Human Functional pEC50 = 6.9 6.9 -60 4
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 492 7 4 9 1.6 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(F)nc32)[C@H](O)[C@@H]1O 10.1021/jm300206u
CHEMBL2042311 75489 None 0 Human Functional pEC50 = 6.9 6.9 -60 4
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 492 7 4 9 1.6 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(F)nc32)[C@H](O)[C@@H]1O 10.1021/jm300206u
11386951 66885 None 0 Human Functional pEC50 = 5.9 5.9 -389 2
Potency against cAMP formation in CHO cells expressing recombinant human A2B receptorPotency against cAMP formation in CHO cells expressing recombinant human A2B receptor
ChEMBL 527 9 5 16 -0.7 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(N[C@H](CO)Cc5ccc([N+](=O)[O-])cc5)nc43)[C@H](O)[C@@H]2O)n1 10.1021/jm031143+
CHEMBL186403 66885 None 0 Human Functional pEC50 = 5.9 5.9 -389 2
Potency against cAMP formation in CHO cells expressing recombinant human A2B receptorPotency against cAMP formation in CHO cells expressing recombinant human A2B receptor
ChEMBL 527 9 5 16 -0.7 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(N[C@H](CO)Cc5ccc([N+](=O)[O-])cc5)nc43)[C@H](O)[C@@H]2O)n1 10.1021/jm031143+
57385043 75488 None 0 Human Functional pEC50 = 4.9 4.9 -134 4
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 810 18 6 13 6.1 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(NCCc4ccc(NC(=O)CCCC[C@H]5CCSS5)cc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm300206u
CHEMBL2042310 75488 None 0 Human Functional pEC50 = 4.9 4.9 -134 4
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 810 18 6 13 6.1 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(NCCc4ccc(NC(=O)CCCC[C@H]5CCSS5)cc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm300206u
76329266 106062 None 0 Human Functional pEC50 = 6.9 6.9 -3 4
Agonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 399 5 5 10 -0.6 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NCc4ccccc4)nc(N)nc32)[C@H](O)[C@@H]1O 10.1039/C3MD00364G
CHEMBL3133160 106062 None 0 Human Functional pEC50 = 6.9 6.9 -3 4
Agonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 399 5 5 10 -0.6 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NCc4ccccc4)nc(N)nc32)[C@H](O)[C@@H]1O 10.1039/C3MD00364G
16203665 136678 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 456 7 5 11 0.1 COc1ccc2[nH]cc(CCOc3nc(N)c4ncn([C@@H]5O[C@H](CO)[C@@H](O)[C@H]5O)c4n3)c2c1 10.1021/jm061278q
CHEMBL374028 136678 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 456 7 5 11 0.1 COc1ccc2[nH]cc(CCOc3nc(N)c4ncn([C@@H]5O[C@H](CO)[C@@H](O)[C@H]5O)c4n3)c2c1 10.1021/jm061278q
76311197 106058 None 0 Human Functional pEC50 = 5.9 5.9 -31 3
Agonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 365 6 5 10 -1.0 CCCCNc1nc(N)nc2c1ncn2[C@@H]1O[C@H](C(=O)NC)[C@@H](O)[C@H]1O 10.1039/C3MD00364G
CHEMBL3133156 106058 None 0 Human Functional pEC50 = 5.9 5.9 -31 3
Agonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 365 6 5 10 -1.0 CCCCNc1nc(N)nc2c1ncn2[C@@H]1O[C@H](C(=O)NC)[C@@H](O)[C@H]1O 10.1039/C3MD00364G
168282699 191018 None 0 Human Functional pEC50 = 4.9 4.9 -12022 3
Agonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 427 6 4 10 0.9 OC[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4Oc4ccccc4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
CHEMBL5186757 191018 None 0 Human Functional pEC50 = 4.9 4.9 -12022 3
Agonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 427 6 4 10 0.9 OC[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4Oc4ccccc4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
57387824 75477 None 0 Human Functional pEC50 = 6.9 6.9 -8 4
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 442 7 6 11 -0.6 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(NCCc4ccc(N)cc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm300206u
CHEMBL2042299 75477 None 0 Human Functional pEC50 = 6.9 6.9 -8 4
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 442 7 6 11 -0.6 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(NCCc4ccc(N)cc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm300206u
16203542 85198 None 0 Human Functional pEC50 = 6.9 6.9 -3 2
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 504 6 5 10 0.9 Nc1nc(OCCc2c[nH]c3cc(Br)ccc23)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm061278q
CHEMBL225459 85198 None 0 Human Functional pEC50 = 6.9 6.9 -3 2
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 504 6 5 10 0.9 Nc1nc(OCCc2c[nH]c3cc(Br)ccc23)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm061278q
137651756 157486 None 0 Human Functional pEC50 = 4.9 4.9 -91 2
Agonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity in presence of [alpha-31P]ATPAgonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity in presence of [alpha-31P]ATP
ChEMBL 355 4 3 9 -0.1 O[C@@H]1[C@@H](CCl)O[C@@H](n2cnc3c(N[C@@H]4CCOC4)ncnc32)[C@@H]1O 10.1021/acs.jmedchem.7b01399
CHEMBL4079464 157486 None 0 Human Functional pEC50 = 4.9 4.9 -91 2
Agonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity in presence of [alpha-31P]ATPAgonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity in presence of [alpha-31P]ATP
ChEMBL 355 4 3 9 -0.1 O[C@@H]1[C@@H](CCl)O[C@@H](n2cnc3c(N[C@@H]4CCOC4)ncnc32)[C@@H]1O 10.1021/acs.jmedchem.7b01399
137657841 159570 None 0 Human Functional pEC50 = 5.9 5.9 -50 4
Agonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assayAgonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assay
ChEMBL 475 6 3 12 1.2 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5ccc(Cl)cc5F)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
CHEMBL4102750 159570 None 0 Human Functional pEC50 = 5.9 5.9 -50 4
Agonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assayAgonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assay
ChEMBL 475 6 3 12 1.2 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5ccc(Cl)cc5F)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
9869857 66830 None 11 Human Functional pEC50 = 5.9 5.9 -213 5
Agonist activity at human recombinant adenosine receptor A2b by cAMP assayAgonist activity at human recombinant adenosine receptor A2b by cAMP assay
ChEMBL 482 8 5 14 -0.6 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(N[C@H](CO)Cc5ccccc5)nc43)[C@H](O)[C@@H]2O)n1 10.1021/jm4011669
CHEMBL186113 66830 None 11 Human Functional pEC50 = 5.9 5.9 -213 5
Agonist activity at human recombinant adenosine receptor A2b by cAMP assayAgonist activity at human recombinant adenosine receptor A2b by cAMP assay
ChEMBL 482 8 5 14 -0.6 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(N[C@H](CO)Cc5ccccc5)nc43)[C@H](O)[C@@H]2O)n1 10.1021/jm4011669
11352497 122967 None 0 Human Functional pEC50 = 5.9 5.9 -416 3
Potency against cAMP formation in CHO cells expressing recombinant human A2B receptorPotency against cAMP formation in CHO cells expressing recombinant human A2B receptor
ChEMBL 498 8 6 15 -0.9 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(N[C@H](CO)Cc5ccc(O)cc5)nc43)[C@H](O)[C@@H]2O)n1 10.1021/jm031143+
CHEMBL360837 122967 None 0 Human Functional pEC50 = 5.9 5.9 -416 3
Potency against cAMP formation in CHO cells expressing recombinant human A2B receptorPotency against cAMP formation in CHO cells expressing recombinant human A2B receptor
ChEMBL 498 8 6 15 -0.9 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(N[C@H](CO)Cc5ccc(O)cc5)nc43)[C@H](O)[C@@H]2O)n1 10.1021/jm031143+
11157262 123640 None 0 Human Functional pEC50 = 5.9 5.9 -537 3
Relative efficacy against phenylephrine precontracted tissue relaxation in Guinea pig aortaRelative efficacy against phenylephrine precontracted tissue relaxation in Guinea pig aorta
ChEMBL 560 8 5 14 0.2 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(N[C@H](CO)Cc5ccc(Br)cc5)nc43)[C@H](O)[C@@H]2O)n1 10.1021/jm031143+
CHEMBL361925 123640 None 0 Human Functional pEC50 = 5.9 5.9 -537 3
Relative efficacy against phenylephrine precontracted tissue relaxation in Guinea pig aortaRelative efficacy against phenylephrine precontracted tissue relaxation in Guinea pig aorta
ChEMBL 560 8 5 14 0.2 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(N[C@H](CO)Cc5ccc(Br)cc5)nc43)[C@H](O)[C@@H]2O)n1 10.1021/jm031143+
71459958 79219 None 0 Human Functional pEC50 = 4.9 4.9 - 1
Effective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNAEffective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNA
ChEMBL 336 3 4 9 -0.9 Nc1ncnc2c1ncn2[C@@H]1O[C@H](C(=S)NC2CC2)[C@@H](O)[C@H]1O 10.1021/jm9804984
CHEMBL2113421 79219 None 0 Human Functional pEC50 = 4.9 4.9 - 1
Effective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNAEffective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNA
ChEMBL 336 3 4 9 -0.9 Nc1ncnc2c1ncn2[C@@H]1O[C@H](C(=S)NC2CC2)[C@@H](O)[C@H]1O 10.1021/jm9804984
118732978 118519 None 0 Human Functional pEC50 = 5.9 5.9 -154 4
Agonist activity at human recombinant adenosine A2B receptor transfected in CHO cells assessed as induction of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2B receptor transfected in CHO cells assessed as induction of adenylyl cyclase activity
ChEMBL 403 5 3 13 -0.6 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NC5CCCO5)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.5b00074
CHEMBL3414944 118519 None 0 Human Functional pEC50 = 5.9 5.9 -154 4
Agonist activity at human recombinant adenosine A2B receptor transfected in CHO cells assessed as induction of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2B receptor transfected in CHO cells assessed as induction of adenylyl cyclase activity
ChEMBL 403 5 3 13 -0.6 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NC5CCCO5)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.5b00074
145977469 163992 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assayAgonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assay
ChEMBL 402 7 2 7 3.9 N#Cc1c(N)nc(SCc2cnc[nH]2)c(C#N)c1-c1ccc(OCC2CC2)cc1 10.1016/j.ejmech.2018.02.081
CHEMBL4208189 163992 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assayAgonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assay
ChEMBL 402 7 2 7 3.9 N#Cc1c(N)nc(SCc2cnc[nH]2)c(C#N)c1-c1ccc(OCC2CC2)cc1 10.1016/j.ejmech.2018.02.081
57387594 75482 None 0 Human Functional pEC50 = 7.9 7.9 -16 4
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 506 8 4 9 2.0 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(F)nc32)[C@H](O)[C@@H]1O 10.1021/jm300206u
CHEMBL2042304 75482 None 0 Human Functional pEC50 = 7.9 7.9 -16 4
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 506 8 4 9 2.0 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(F)nc32)[C@H](O)[C@@H]1O 10.1021/jm300206u
377 2758 None 53 Human Functional pEC50 = 6.9 6.9 -48 10
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm061278q
425 2758 None 53 Human Functional pEC50 = 6.9 6.9 -48 10
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm061278q
448222 2758 None 53 Human Functional pEC50 = 6.9 6.9 -48 10
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm061278q
CHEMBL464859 2758 None 53 Human Functional pEC50 = 6.9 6.9 -48 10
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm061278q
24827417 96347 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of adenylate cyclaseAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of adenylate cyclase
ChEMBL 729 12 6 12 4.1 O=C(COc1ccc(Nc2nc(OCCc3c[nH]c4cc(Br)ccc34)nc3c2ncn3[C@@H]2O[C@H](CO)[C@@H](O)[C@H]2O)cc1)Nc1ccccc1 10.1021/jm701442d
CHEMBL261546 96347 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of adenylate cyclaseAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of adenylate cyclase
ChEMBL 729 12 6 12 4.1 O=C(COc1ccc(Nc2nc(OCCc3c[nH]c4cc(Br)ccc34)nc3c2ncn3[C@@H]2O[C@H](CO)[C@@H](O)[C@H]2O)cc1)Nc1ccccc1 10.1021/jm701442d
9954747 137111 None 15 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 437 6 4 10 0.8 Nc1nc(OCCc2ccc3ccccc3c2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm061278q
CHEMBL374760 137111 None 15 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 437 6 4 10 0.8 Nc1nc(OCCc2ccc3ccccc3c2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm061278q
149362 75476 None 6 Human Functional pEC50 = 6.8 6.8 -12 4
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 427 7 5 10 -0.2 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(NCCc4ccccc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm300206u
CHEMBL2042298 75476 None 6 Human Functional pEC50 = 6.8 6.8 -12 4
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 427 7 5 10 -0.2 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(NCCc4ccccc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm300206u
168290627 192003 None 0 Human Functional pEC50 = 6.8 6.8 3 4
Agonist activity at human A2B receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 10 mins in presence of forskolin by LANCE cAMP assayAgonist activity at human A2B receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 10 mins in presence of forskolin by LANCE cAMP assay
ChEMBL 859 11 6 13 6.6 Nc1sc(-c2ccc(C(=O)NCCC#Cc3ccc(Nc4ncnc5c4ncn5[C@@H]4O[C@H](CO)[C@@H](O)[C@H]4O)cc3)cc2)c(-c2cccc(C(F)(F)F)c2)c1C(=O)c1ccccc1 10.1021/acs.jmedchem.2c00320
CHEMBL5201533 192003 None 0 Human Functional pEC50 = 6.8 6.8 3 4
Agonist activity at human A2B receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 10 mins in presence of forskolin by LANCE cAMP assayAgonist activity at human A2B receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 10 mins in presence of forskolin by LANCE cAMP assay
ChEMBL 859 11 6 13 6.6 Nc1sc(-c2ccc(C(=O)NCCC#Cc3ccc(Nc4ncnc5c4ncn5[C@@H]4O[C@H](CO)[C@@H](O)[C@H]4O)cc3)cc2)c(-c2cccc(C(F)(F)F)c2)c1C(=O)c1ccccc1 10.1021/acs.jmedchem.2c00320
137656845 159796 None 0 Human Functional pEC50 = 6.8 6.8 1 3
Agonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 800 15 5 12 6.5 O=C(NCCCCCCNc1ncnc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O)c1ccc(-c2scc(C(=O)c3ccccc3)c2-c2cccc(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.8b00047
CHEMBL4105473 159796 None 0 Human Functional pEC50 = 6.8 6.8 1 3
Agonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 800 15 5 12 6.5 O=C(NCCCCCCNc1ncnc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O)c1ccc(-c2scc(C(=O)c3ccccc3)c2-c2cccc(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.8b00047
118732972 118513 None 0 Human Functional pEC50 = 5.8 5.8 -234 4
Agonist activity at human recombinant adenosine A2B receptor transfected in CHO cells assessed as induction of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2B receptor transfected in CHO cells assessed as induction of adenylyl cyclase activity
ChEMBL 347 4 3 12 -1.1 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NC)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.5b00074
CHEMBL3414938 118513 None 0 Human Functional pEC50 = 5.8 5.8 -234 4
Agonist activity at human recombinant adenosine A2B receptor transfected in CHO cells assessed as induction of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2B receptor transfected in CHO cells assessed as induction of adenylyl cyclase activity
ChEMBL 347 4 3 12 -1.1 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NC)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.5b00074
57384287 75479 None 0 Human Functional pEC50 = 5.8 5.8 -33 4
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 658 9 6 11 3.7 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(NCCc4ccc(NC(=O)c5cc(C(C)(C)C)cc(C(C)(C)C)c5)cc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm300206u
CHEMBL2042301 75479 None 0 Human Functional pEC50 = 5.8 5.8 -33 4
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 658 9 6 11 3.7 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(NCCc4ccc(NC(=O)c5cc(C(C)(C)C)cc(C(C)(C)C)c5)cc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm300206u
11776764 7899 None 15 Human Functional pEC50 = 4.8 4.8 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 248 2 1 8 1.1 CSc1nc(N)n2nc(-c3ccco3)nc2n1 10.1016/j.bmc.2010.02.039
CHEMBL1090123 7899 None 15 Human Functional pEC50 = 4.8 4.8 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 248 2 1 8 1.1 CSc1nc(N)n2nc(-c3ccco3)nc2n1 10.1016/j.bmc.2010.02.039
44423812 85372 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 551 9 5 11 1.5 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(Nc4ccc(OCC(=O)Nc5ccc(F)cc5)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1016/j.bmc.2007.01.055
CHEMBL226194 85372 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 551 9 5 11 1.5 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(Nc4ccc(OCC(=O)Nc5ccc(F)cc5)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1016/j.bmc.2007.01.055
377 2758 None 53 Human Functional pEC50 = 7.8 7.8 -48 10
Agonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.8b00047
425 2758 None 53 Human Functional pEC50 = 7.8 7.8 -48 10
Agonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.8b00047
448222 2758 None 53 Human Functional pEC50 = 7.8 7.8 -48 10
Agonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.8b00047
CHEMBL464859 2758 None 53 Human Functional pEC50 = 7.8 7.8 -48 10
Agonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.8b00047
44423824 137585 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 547 10 5 11 1.0 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(Nc4ccc(OCC(=O)NCc5ccccc5)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1016/j.bmc.2007.01.055
CHEMBL375501 137585 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 547 10 5 11 1.0 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(Nc4ccc(OCC(=O)NCc5ccccc5)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1016/j.bmc.2007.01.055
377 2758 None 53 Human Functional pEC50 = 5.8 5.8 -48 10
Agonist activity at human adenosine receptor A2B expressed in CHO cell membranes assessed as forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by forskolin addition measured after 10 mins by liquid scintillation counter methodAgonist activity at human adenosine receptor A2B expressed in CHO cell membranes assessed as forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by forskolin addition measured after 10 mins by liquid scintillation counter method
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.7b00457
425 2758 None 53 Human Functional pEC50 = 5.8 5.8 -48 10
Agonist activity at human adenosine receptor A2B expressed in CHO cell membranes assessed as forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by forskolin addition measured after 10 mins by liquid scintillation counter methodAgonist activity at human adenosine receptor A2B expressed in CHO cell membranes assessed as forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by forskolin addition measured after 10 mins by liquid scintillation counter method
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.7b00457
448222 2758 None 53 Human Functional pEC50 = 5.8 5.8 -48 10
Agonist activity at human adenosine receptor A2B expressed in CHO cell membranes assessed as forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by forskolin addition measured after 10 mins by liquid scintillation counter methodAgonist activity at human adenosine receptor A2B expressed in CHO cell membranes assessed as forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by forskolin addition measured after 10 mins by liquid scintillation counter method
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.7b00457
CHEMBL464859 2758 None 53 Human Functional pEC50 = 5.8 5.8 -48 10
Agonist activity at human adenosine receptor A2B expressed in CHO cell membranes assessed as forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by forskolin addition measured after 10 mins by liquid scintillation counter methodAgonist activity at human adenosine receptor A2B expressed in CHO cell membranes assessed as forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by forskolin addition measured after 10 mins by liquid scintillation counter method
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.7b00457
377 2758 None 53 Human Functional pEC50 = 6.8 6.8 -48 10
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1016/j.bmc.2007.01.055
425 2758 None 53 Human Functional pEC50 = 6.8 6.8 -48 10
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1016/j.bmc.2007.01.055
448222 2758 None 53 Human Functional pEC50 = 6.8 6.8 -48 10
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1016/j.bmc.2007.01.055
CHEMBL464859 2758 None 53 Human Functional pEC50 = 6.8 6.8 -48 10
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1016/j.bmc.2007.01.055
137649841 157430 None 0 Human Functional pEC50 = 6.8 6.8 -1 4
Agonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 656 14 5 12 3.8 O=C(NCCCCCCNc1ncnc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O)c1cccc(-c2cc(C(=O)c3ccccc3)cs2)c1 10.1021/acs.jmedchem.8b00047
CHEMBL4078771 157430 None 0 Human Functional pEC50 = 6.8 6.8 -1 4
Agonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 656 14 5 12 3.8 O=C(NCCCCCCNc1ncnc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O)c1cccc(-c2cc(C(=O)c3ccccc3)cs2)c1 10.1021/acs.jmedchem.8b00047
76311194 106046 None 0 Human Functional pEC50 = 6.8 6.8 -100 4
Agonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 525 5 5 10 -0.0 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NCc4cccc(I)c4)nc(N)nc32)[C@H](O)[C@@H]1O 10.1039/C3MD00364G
CHEMBL3133078 106046 None 0 Human Functional pEC50 = 6.8 6.8 -100 4
Agonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 525 5 5 10 -0.0 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NCc4cccc(I)c4)nc(N)nc32)[C@H](O)[C@@H]1O 10.1039/C3MD00364G
76329263 106047 None 0 Human Functional pEC50 = 6.8 6.8 -39 4
Agonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 413 6 5 10 -0.6 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NCCc4ccccc4)nc(N)nc32)[C@H](O)[C@@H]1O 10.1039/C3MD00364G
CHEMBL3133079 106047 None 0 Human Functional pEC50 = 6.8 6.8 -39 4
Agonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 413 6 5 10 -0.6 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NCCc4ccccc4)nc(N)nc32)[C@H](O)[C@@H]1O 10.1039/C3MD00364G
76332919 106055 None 0 Human Functional pEC50 = 5.8 5.8 -316 3
Agonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 323 3 5 10 -2.2 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NC)nc(N)nc32)[C@H](O)[C@@H]1O 10.1039/C3MD00364G
CHEMBL3133153 106055 None 0 Human Functional pEC50 = 5.8 5.8 -316 3
Agonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 323 3 5 10 -2.2 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NC)nc(N)nc32)[C@H](O)[C@@H]1O 10.1039/C3MD00364G
76336525 106056 None 0 Human Functional pEC50 = 5.8 5.8 -158 3
Agonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 337 4 5 10 -1.8 CCNc1nc(N)nc2c1ncn2[C@@H]1O[C@H](C(=O)NC)[C@@H](O)[C@H]1O 10.1039/C3MD00364G
CHEMBL3133154 106056 None 0 Human Functional pEC50 = 5.8 5.8 -158 3
Agonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 337 4 5 10 -1.8 CCNc1nc(N)nc2c1ncn2[C@@H]1O[C@H](C(=O)NC)[C@@H](O)[C@H]1O 10.1039/C3MD00364G
44423821 142193 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 589 9 5 11 2.6 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(Nc4ccc(OCC(=O)Nc5ccc(C(C)(C)C)cc5)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1016/j.bmc.2007.01.055
CHEMBL388405 142193 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 589 9 5 11 2.6 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(Nc4ccc(OCC(=O)Nc5ccc(C(C)(C)C)cc5)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1016/j.bmc.2007.01.055
72141742 162576 None 1 Human Functional pEC50 = 7.8 7.8 - 1
Antagonist activity at Adenosine receptor subtype 2B in human RBC assessed as change in erythrocyte morphology incubated for 3 hrs with occasional gentle stirring for every 30 min measured for every 12 hrs by microscopic analysisAntagonist activity at Adenosine receptor subtype 2B in human RBC assessed as change in erythrocyte morphology incubated for 3 hrs with occasional gentle stirring for every 30 min measured for every 12 hrs by microscopic analysis
ChEMBL 302 5 1 7 0.0 O=C(CN1CCOC(Cn2cncn2)C1)Nc1cccnc1 10.1016/j.ejmech.2017.05.035
CHEMBL4168653 162576 None 1 Human Functional pEC50 = 7.8 7.8 - 1
Antagonist activity at Adenosine receptor subtype 2B in human RBC assessed as change in erythrocyte morphology incubated for 3 hrs with occasional gentle stirring for every 30 min measured for every 12 hrs by microscopic analysisAntagonist activity at Adenosine receptor subtype 2B in human RBC assessed as change in erythrocyte morphology incubated for 3 hrs with occasional gentle stirring for every 30 min measured for every 12 hrs by microscopic analysis
ChEMBL 302 5 1 7 0.0 O=C(CN1CCOC(Cn2cncn2)C1)Nc1cccnc1 10.1016/j.ejmech.2017.05.035
377 2758 None 53 Human Functional pEC50 = 6.8 6.8 -48 10
Activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP levelsActivity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP levels
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm061170a
425 2758 None 53 Human Functional pEC50 = 6.8 6.8 -48 10
Activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP levelsActivity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP levels
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm061170a
448222 2758 None 53 Human Functional pEC50 = 6.8 6.8 -48 10
Activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP levelsActivity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP levels
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm061170a
CHEMBL464859 2758 None 53 Human Functional pEC50 = 6.8 6.8 -48 10
Activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP levelsActivity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP levels
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm061170a
14157150 79229 None 0 Human Functional pEC50 = 4.8 4.8 - 1
Effective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNAEffective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNA
ChEMBL 324 3 4 9 -1.0 CCNC(=S)[C@H]1O[C@@H](n2cnc3c(N)ncnc32)[C@H](O)[C@@H]1O 10.1021/jm9804984
CHEMBL2113431 79229 None 0 Human Functional pEC50 = 4.8 4.8 - 1
Effective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNAEffective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNA
ChEMBL 324 3 4 9 -1.0 CCNC(=S)[C@H]1O[C@@H](n2cnc3c(N)ncnc32)[C@H](O)[C@@H]1O 10.1021/jm9804984
21893339 163912 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assayAgonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assay
ChEMBL 366 5 3 7 1.6 CC(=O)Nc1ccc(-c2c(C#N)c(N)nc(SCC(N)=O)c2C#N)cc1 10.1016/j.ejmech.2018.02.081
CHEMBL4207286 163912 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assayAgonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assay
ChEMBL 366 5 3 7 1.6 CC(=O)Nc1ccc(-c2c(C#N)c(N)nc(SCC(N)=O)c2C#N)cc1 10.1016/j.ejmech.2018.02.081
137636099 155825 None 0 Human Functional pEC50 = 5.8 5.8 -173 4
Agonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assayAgonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assay
ChEMBL 535 6 3 12 1.9 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5cccc(Br)c5)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
CHEMBL4059961 155825 None 0 Human Functional pEC50 = 5.8 5.8 -173 4
Agonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assayAgonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assay
ChEMBL 535 6 3 12 1.9 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5cccc(Br)c5)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
414 3382 None 33 Human Functional pEC50 = 5.8 5.8 -213 5
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 385 6 4 9 0.5 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N[C@@H](Cc1ccccc1)C 10.1021/jm061278q
93205 3382 None 33 Human Functional pEC50 = 5.8 5.8 -213 5
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 385 6 4 9 0.5 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N[C@@H](Cc1ccccc1)C 10.1021/jm061278q
CHEMBL139000 3382 None 33 Human Functional pEC50 = 5.8 5.8 -213 5
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 385 6 4 9 0.5 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N[C@@H](Cc1ccccc1)C 10.1021/jm061278q
46885472 8333 None 0 Human Functional pEC50 = 4.8 4.8 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 381 4 2 8 3.5 CSc1nc(NC(=O)Nc2ccc(C)cc2)n2nc(-c3ccco3)nc2n1 10.1016/j.bmc.2010.02.039
CHEMBL1092869 8333 None 0 Human Functional pEC50 = 4.8 4.8 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 381 4 2 8 3.5 CSc1nc(NC(=O)Nc2ccc(C)cc2)n2nc(-c3ccco3)nc2n1 10.1016/j.bmc.2010.02.039
11395785 186514 None 0 Human Functional pEC50 = 4.8 4.8 - 1
Agonist activity at human adenosine receptor A2B expressed in CHO cell membranes assessed as forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by forskolin addition measured after 10 mins by liquid scintillation counter methodAgonist activity at human adenosine receptor A2B expressed in CHO cell membranes assessed as forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by forskolin addition measured after 10 mins by liquid scintillation counter method
ChEMBL 410 5 4 9 0.6 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NC4CCCC4)nc(Cl)nc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.7b00457
CHEMBL487754 186514 None 0 Human Functional pEC50 = 4.8 4.8 - 1
Agonist activity at human adenosine receptor A2B expressed in CHO cell membranes assessed as forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by forskolin addition measured after 10 mins by liquid scintillation counter methodAgonist activity at human adenosine receptor A2B expressed in CHO cell membranes assessed as forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by forskolin addition measured after 10 mins by liquid scintillation counter method
ChEMBL 410 5 4 9 0.6 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NC4CCCC4)nc(Cl)nc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.7b00457
168280775 191157 None 0 Human Functional pEC50 = 4.8 4.8 -1096 4
Agonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 524 7 4 10 2.3 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4Oc4ccc(C(C)(C)C)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
CHEMBL5188601 191157 None 0 Human Functional pEC50 = 4.8 4.8 -1096 4
Agonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 524 7 4 10 2.3 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4Oc4ccc(C(C)(C)C)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
137643164 158101 None 0 Human Functional pEC50 = 7.8 7.8 5 4
Agonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 552 12 5 11 2.6 O=C(NCCCCCCNc1ncnc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O)c1cccc(-c2cccs2)c1 10.1021/acs.jmedchem.8b00047
CHEMBL4086624 158101 None 0 Human Functional pEC50 = 7.8 7.8 5 4
Agonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 552 12 5 11 2.6 O=C(NCCCCCCNc1ncnc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O)c1cccc(-c2cccs2)c1 10.1021/acs.jmedchem.8b00047
46885471 8332 None 0 Human Functional pEC50 = 4.8 4.8 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 367 4 2 8 3.1 CSc1nc(NC(=O)Nc2ccccc2)n2nc(-c3ccco3)nc2n1 10.1016/j.bmc.2010.02.039
CHEMBL1092868 8332 None 0 Human Functional pEC50 = 4.8 4.8 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 367 4 2 8 3.1 CSc1nc(NC(=O)Nc2ccccc2)n2nc(-c3ccco3)nc2n1 10.1016/j.bmc.2010.02.039
24827415 159426 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of adenylate cyclaseAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of adenylate cyclase
ChEMBL 519 7 6 11 0.6 NNc1nc(OCCc2c[nH]c3cc(Br)ccc23)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm701442d
CHEMBL410104 159426 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of adenylate cyclaseAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of adenylate cyclase
ChEMBL 519 7 6 11 0.6 NNc1nc(OCCc2c[nH]c3cc(Br)ccc23)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm701442d
16103168 83218 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP levelsActivity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP levels
ChEMBL 481 6 5 11 0.4 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NNC(=O)c4ccc(C)s4)nc(Cl)nc32)[C@H](O)[C@@H]1O 10.1021/jm061170a
CHEMBL218585 83218 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP levelsActivity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP levels
ChEMBL 481 6 5 11 0.4 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NNC(=O)c4ccc(C)s4)nc(Cl)nc32)[C@H](O)[C@@H]1O 10.1021/jm061170a
44423837 85249 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 581 10 5 11 1.7 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(Nc4ccc(OCC(=O)NCc5ccccc5)cc4)nc(Cl)nc32)[C@H](O)[C@@H]1O 10.1016/j.bmc.2007.01.055
CHEMBL225944 85249 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 581 10 5 11 1.7 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(Nc4ccc(OCC(=O)NCc5ccccc5)cc4)nc(Cl)nc32)[C@H](O)[C@@H]1O 10.1016/j.bmc.2007.01.055
44420921 85162 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 393 6 4 11 -0.3 Nc1nc(OCCc2cccs2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm061278q
CHEMBL225233 85162 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 393 6 4 11 -0.3 Nc1nc(OCCc2cccs2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm061278q
137649083 157307 None 0 Human Functional pEC50 = 7.7 7.7 7 3
Agonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 849 15 6 13 6.7 Nc1sc(-c2ccc(C(=O)NCCCCCCNc3nc(Cl)nc4c3ncn4[C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)cc2)c(-c2cccc(C(F)(F)F)c2)c1C(=O)c1ccccc1 10.1021/acs.jmedchem.8b00047
CHEMBL4077152 157307 None 0 Human Functional pEC50 = 7.7 7.7 7 3
Agonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 849 15 6 13 6.7 Nc1sc(-c2ccc(C(=O)NCCCCCCNc3nc(Cl)nc4c3ncn4[C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)cc2)c(-c2cccc(C(F)(F)F)c2)c1C(=O)c1ccccc1 10.1021/acs.jmedchem.8b00047
145968949 164817 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assayAgonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assay
ChEMBL 409 8 3 8 2.0 N#Cc1c(N)nc(SCC(=O)NCO)c(C#N)c1-c1ccc(OCC2CC2)cc1 10.1016/j.ejmech.2018.02.081
CHEMBL4218613 164817 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assayAgonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assay
ChEMBL 409 8 3 8 2.0 N#Cc1c(N)nc(SCC(=O)NCO)c(C#N)c1-c1ccc(OCC2CC2)cc1 10.1016/j.ejmech.2018.02.081
16202726 84712 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 552 6 5 10 0.7 Nc1nc(OCCc2c[nH]c3ccc(I)cc23)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm061278q
CHEMBL222748 84712 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 552 6 5 10 0.7 Nc1nc(OCCc2c[nH]c3ccc(I)cc23)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm061278q
11174953 16762 None 1 Human Functional pEC50 = 7.7 7.7 -1 2
Agonistic activity against human adenosine A2B receptor expressed in CHO cellsAgonistic activity against human adenosine A2B receptor expressed in CHO cells
ChEMBL 332 4 2 6 3.1 N#Cc1c(N)nc(SCc2ncc[nH]2)c(C#N)c1-c1ccccc1 10.1021/jm049947s
CHEMBL124345 16762 None 1 Human Functional pEC50 = 7.7 7.7 -1 2
Agonistic activity against human adenosine A2B receptor expressed in CHO cellsAgonistic activity against human adenosine A2B receptor expressed in CHO cells
ChEMBL 332 4 2 6 3.1 N#Cc1c(N)nc(SCc2ncc[nH]2)c(C#N)c1-c1ccccc1 10.1021/jm049947s
168283013 190875 None 0 Human Functional pEC50 = 4.7 4.7 -3715 4
Agonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 516 8 4 10 1.8 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4OCc4cccc(Cl)c4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
CHEMBL5184828 190875 None 0 Human Functional pEC50 = 4.7 4.7 -3715 4
Agonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 516 8 4 10 1.8 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4OCc4cccc(Cl)c4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
137650899 157203 None 0 Human Functional pEC50 = 5.7 5.7 -35 4
Agonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assayAgonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assay
ChEMBL 413 6 3 13 0.0 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5ccco5)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
CHEMBL4076003 157203 None 0 Human Functional pEC50 = 5.7 5.7 -35 4
Agonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assayAgonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assay
ChEMBL 413 6 3 13 0.0 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5ccco5)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
137657926 159768 None 0 Human Functional pEC50 = 5.7 5.7 -269 4
Agonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assayAgonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assay
ChEMBL 421 6 3 12 0.3 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCC5CC5)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
CHEMBL4105164 159768 None 0 Human Functional pEC50 = 5.7 5.7 -269 4
Agonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assayAgonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assay
ChEMBL 421 6 3 12 0.3 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCC5CC5)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
76322076 106048 None 0 Human Functional pEC50 = 6.7 6.7 -39 4
Agonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 489 7 5 10 1.0 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(N)nc32)[C@H](O)[C@@H]1O 10.1039/C3MD00364G
CHEMBL3133080 106048 None 0 Human Functional pEC50 = 6.7 6.7 -39 4
Agonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 489 7 5 10 1.0 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(N)nc32)[C@H](O)[C@@H]1O 10.1039/C3MD00364G
76318403 106059 None 0 Human Functional pEC50 = 6.7 6.7 -39 4
Agonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 363 4 5 10 -1.3 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NC4CCC4)nc(N)nc32)[C@H](O)[C@@H]1O 10.1039/C3MD00364G
CHEMBL3133157 106059 None 0 Human Functional pEC50 = 6.7 6.7 -39 4
Agonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 363 4 5 10 -1.3 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NC4CCC4)nc(N)nc32)[C@H](O)[C@@H]1O 10.1039/C3MD00364G
57387337 75475 None 0 Human Functional pEC50 = 8.6 8.6 -6 4
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 326 3 4 9 -1.7 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(F)nc32)[C@H](O)[C@@H]1O 10.1021/jm300206u
CHEMBL2042297 75475 None 0 Human Functional pEC50 = 8.6 8.6 -6 4
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 326 3 4 9 -1.7 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(F)nc32)[C@H](O)[C@@H]1O 10.1021/jm300206u
16103185 166043 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP levelsActivity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP levels
ChEMBL 467 6 5 11 0.1 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NNC(=O)c4cccs4)nc(Cl)nc32)[C@H](O)[C@@H]1O 10.1021/jm061170a
CHEMBL425643 166043 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP levelsActivity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP levels
ChEMBL 467 6 5 11 0.1 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NNC(=O)c4cccs4)nc(Cl)nc32)[C@H](O)[C@@H]1O 10.1021/jm061170a
70689262 77977 None 0 Human Functional pEC50 = 5.7 5.7 -954 3
Potency against cAMP formation in CHO cells expressing recombinant human A2B receptorPotency against cAMP formation in CHO cells expressing recombinant human A2B receptor
ChEMBL 496 8 4 14 0.5 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(N[C@H](C)Cc5ccc(OC)cc5)nc43)[C@H](O)[C@@H]2O)n1 10.1021/jm031143+
CHEMBL2096798 77977 None 0 Human Functional pEC50 = 5.7 5.7 -954 3
Potency against cAMP formation in CHO cells expressing recombinant human A2B receptorPotency against cAMP formation in CHO cells expressing recombinant human A2B receptor
ChEMBL 496 8 4 14 0.5 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(N[C@H](C)Cc5ccc(OC)cc5)nc43)[C@H](O)[C@@H]2O)n1 10.1021/jm031143+
137656913 159653 None 0 Human Functional pEC50 = 4.7 4.7 -371 2
Agonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity in presence of [alpha-31P]ATPAgonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity in presence of [alpha-31P]ATP
ChEMBL 389 4 3 9 0.5 O[C@@H]1[C@@H](CCl)O[C@@H](n2cnc3c(N[C@@H]4CCOC4)nc(Cl)nc32)[C@@H]1O 10.1021/acs.jmedchem.7b01399
CHEMBL4103712 159653 None 0 Human Functional pEC50 = 4.7 4.7 -371 2
Agonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity in presence of [alpha-31P]ATPAgonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity in presence of [alpha-31P]ATP
ChEMBL 389 4 3 9 0.5 O[C@@H]1[C@@H](CCl)O[C@@H](n2cnc3c(N[C@@H]4CCOC4)nc(Cl)nc32)[C@@H]1O 10.1021/acs.jmedchem.7b01399
46885518 7798 None 0 Human Functional pEC50 = 4.7 4.7 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 427 5 2 8 4.5 Cc1ccc(NC(=O)Nc2nc(Oc3ccccc3)nc3nc(-c4ccco4)nn23)cc1 10.1016/j.bmc.2010.02.039
CHEMBL1089441 7798 None 0 Human Functional pEC50 = 4.7 4.7 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 427 5 2 8 4.5 Cc1ccc(NC(=O)Nc2nc(Oc3ccccc3)nc3nc(-c4ccco4)nn23)cc1 10.1016/j.bmc.2010.02.039
16109359 161778 None 0 Human Functional pEC50 = 5.7 5.7 -758 4
Activity at human adenosine A2B receptor assessed as stimulation of [3H]cAMP accumulation in CHO cellsActivity at human adenosine A2B receptor assessed as stimulation of [3H]cAMP accumulation in CHO cells
ChEMBL 924 21 6 14 4.5 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCCCCNC(=O)CCCCCNC(=O)COc4ccc(/C=C/C5=[N+]6C(=Cc7ccc(-c8cccs8)n7[B-]6(F)F)C=C5)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1021/jm061279i
CHEMBL414055 161778 None 0 Human Functional pEC50 = 5.7 5.7 -758 4
Activity at human adenosine A2B receptor assessed as stimulation of [3H]cAMP accumulation in CHO cellsActivity at human adenosine A2B receptor assessed as stimulation of [3H]cAMP accumulation in CHO cells
ChEMBL 924 21 6 14 4.5 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCCCCNC(=O)CCCCCNC(=O)COc4ccc(/C=C/C5=[N+]6C(=Cc7ccc(-c8cccs8)n7[B-]6(F)F)C=C5)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1021/jm061279i
16103167 83383 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP levelsActivity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP levels
ChEMBL 451 6 5 11 -0.4 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NNC(=O)c4ccco4)nc(Cl)nc32)[C@H](O)[C@@H]1O 10.1021/jm061170a
CHEMBL219413 83383 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP levelsActivity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP levels
ChEMBL 451 6 5 11 -0.4 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NNC(=O)c4ccco4)nc(Cl)nc32)[C@H](O)[C@@H]1O 10.1021/jm061170a
145977114 163771 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assayAgonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assay
ChEMBL 367 6 2 7 2.3 CCOc1ccc(-c2c(C#N)c(N)nc(SCC(=O)NC)c2C#N)cc1 10.1016/j.ejmech.2018.02.081
CHEMBL4205729 163771 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assayAgonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assay
ChEMBL 367 6 2 7 2.3 CCOc1ccc(-c2c(C#N)c(N)nc(SCC(=O)NC)c2C#N)cc1 10.1016/j.ejmech.2018.02.081
137650221 157255 None 0 Human Functional pEC50 = 5.7 5.7 -56 4
Agonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assayAgonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assay
ChEMBL 463 6 3 13 1.2 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5cccs5)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
CHEMBL4076561 157255 None 0 Human Functional pEC50 = 5.7 5.7 -56 4
Agonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assayAgonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assay
ChEMBL 463 6 3 13 1.2 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5cccs5)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
16202727 84739 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 460 6 5 10 0.8 Nc1nc(OCCc2c[nH]c3cc(Cl)ccc23)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm061278q
CHEMBL222907 84739 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 460 6 5 10 0.8 Nc1nc(OCCc2c[nH]c3cc(Cl)ccc23)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm061278q
16202725 84661 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 460 6 5 10 0.8 Nc1nc(OCCc2c[nH]c3ccc(Cl)cc23)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm061278q
CHEMBL222442 84661 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 460 6 5 10 0.8 Nc1nc(OCCc2c[nH]c3ccc(Cl)cc23)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm061278q
23757284 85129 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 438 4 5 10 -0.8 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(C#C[C@@H](O)c4ccccc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm061278q
CHEMBL224874 85129 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 438 4 5 10 -0.8 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(C#C[C@@H](O)c4ccccc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm061278q
118732974 118515 None 0 Human Functional pEC50 = 6.7 6.7 -47 4
Agonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assayAgonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assay
ChEMBL 373 5 3 12 -0.6 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NC5CC5)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
CHEMBL3414940 118515 None 0 Human Functional pEC50 = 6.7 6.7 -47 4
Agonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assayAgonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assay
ChEMBL 373 5 3 12 -0.6 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NC5CC5)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
137650918 157245 None 0 Human Functional pEC50 = 6.7 6.7 -6 4
Agonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 671 14 6 13 3.4 Nc1sc(-c2ccc(C(=O)NCCCCCCNc3ncnc4c3ncn4[C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)cc2)cc1C(=O)c1ccccc1 10.1021/acs.jmedchem.8b00047
CHEMBL4076495 157245 None 0 Human Functional pEC50 = 6.7 6.7 -6 4
Agonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 671 14 6 13 3.4 Nc1sc(-c2ccc(C(=O)NCCCCCCNc3ncnc4c3ncn4[C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)cc2)cc1C(=O)c1ccccc1 10.1021/acs.jmedchem.8b00047
132991434 179958 None 0 Human Functional pEC50 = 6.7 6.7 -23 4
Irreversible agonist activity at human adenosine A2B receptor expressed in Flp-In-CHO cells assessed as effect on forskolin-induced cAMP accumulation incubated for 30 mins by LANCE cAMP detection assayIrreversible agonist activity at human adenosine A2B receptor expressed in Flp-In-CHO cells assessed as effect on forskolin-induced cAMP accumulation incubated for 30 mins by LANCE cAMP detection assay
ChEMBL 564 8 6 12 2.4 OC[C@H]1O[C@@H](n2cnc3c(Nc4ccc(CNC(=S)Nc5ccc(N=C=S)cc5)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.6b01561
CHEMBL4746617 179958 None 0 Human Functional pEC50 = 6.7 6.7 -23 4
Irreversible agonist activity at human adenosine A2B receptor expressed in Flp-In-CHO cells assessed as effect on forskolin-induced cAMP accumulation incubated for 30 mins by LANCE cAMP detection assayIrreversible agonist activity at human adenosine A2B receptor expressed in Flp-In-CHO cells assessed as effect on forskolin-induced cAMP accumulation incubated for 30 mins by LANCE cAMP detection assay
ChEMBL 564 8 6 12 2.4 OC[C@H]1O[C@@H](n2cnc3c(Nc4ccc(CNC(=S)Nc5ccc(N=C=S)cc5)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.6b01561
137651747 157481 None 0 Human Functional pEC50 = 5.7 5.7 -70 4
Agonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assayAgonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assay
ChEMBL 475 6 3 12 1.2 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5cccc(F)c5)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
CHEMBL4079433 157481 None 0 Human Functional pEC50 = 5.7 5.7 -70 4
Agonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assayAgonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assay
ChEMBL 475 6 3 12 1.2 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5cccc(F)c5)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
16103178 160658 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP levelsActivity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP levels
ChEMBL 431 6 5 11 -0.8 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NNC(=O)c4ccc(C)o4)ncnc32)[C@H](O)[C@@H]1O 10.1021/jm061170a
CHEMBL411332 160658 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP levelsActivity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP levels
ChEMBL 431 6 5 11 -0.8 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NNC(=O)c4ccc(C)o4)ncnc32)[C@H](O)[C@@H]1O 10.1021/jm061170a
57384543 75486 None 0 Human Functional pEC50 = 5.6 5.6 -6 4
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 838 14 6 11 7.3 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(NCCc4ccc(NC(=O)c5cc(C(C)(C)C)cc(C(C)(C)C)c5)cc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm300206u
CHEMBL2042308 75486 None 0 Human Functional pEC50 = 5.6 5.6 -6 4
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 838 14 6 11 7.3 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(NCCc4ccc(NC(=O)c5cc(C(C)(C)C)cc(C(C)(C)C)c5)cc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm300206u
449 2643 None 52 Human Functional pEC50 = 7.6 7.6 1 4
Antagonist activity at Adenosine receptor subtype 2B in human RBC assessed as change in erythrocyte morphology incubated for 3 hrs with occasional gentle stirring for every 30 min measured for every 12 hrs by microscopic analysisAntagonist activity at Adenosine receptor subtype 2B in human RBC assessed as change in erythrocyte morphology incubated for 3 hrs with occasional gentle stirring for every 30 min measured for every 12 hrs by microscopic analysis
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10.1016/j.ejmech.2017.05.035
453 2643 None 52 Human Functional pEC50 = 7.6 7.6 1 4
Antagonist activity at Adenosine receptor subtype 2B in human RBC assessed as change in erythrocyte morphology incubated for 3 hrs with occasional gentle stirring for every 30 min measured for every 12 hrs by microscopic analysisAntagonist activity at Adenosine receptor subtype 2B in human RBC assessed as change in erythrocyte morphology incubated for 3 hrs with occasional gentle stirring for every 30 min measured for every 12 hrs by microscopic analysis
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10.1016/j.ejmech.2017.05.035
6603931 2643 None 52 Human Functional pEC50 = 7.6 7.6 1 4
Antagonist activity at Adenosine receptor subtype 2B in human RBC assessed as change in erythrocyte morphology incubated for 3 hrs with occasional gentle stirring for every 30 min measured for every 12 hrs by microscopic analysisAntagonist activity at Adenosine receptor subtype 2B in human RBC assessed as change in erythrocyte morphology incubated for 3 hrs with occasional gentle stirring for every 30 min measured for every 12 hrs by microscopic analysis
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10.1016/j.ejmech.2017.05.035
CHEMBL273807 2643 None 52 Human Functional pEC50 = 7.6 7.6 1 4
Antagonist activity at Adenosine receptor subtype 2B in human RBC assessed as change in erythrocyte morphology incubated for 3 hrs with occasional gentle stirring for every 30 min measured for every 12 hrs by microscopic analysisAntagonist activity at Adenosine receptor subtype 2B in human RBC assessed as change in erythrocyte morphology incubated for 3 hrs with occasional gentle stirring for every 30 min measured for every 12 hrs by microscopic analysis
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10.1016/j.ejmech.2017.05.035
136015813 162364 None 4 Human Functional pEC50 = 7.6 7.6 - 1
Antagonist activity at Adenosine receptor subtype 2B in human RBC assessed as change in erythrocyte morphology incubated for 3 hrs with occasional gentle stirring for every 30 min measured for every 12 hrs by microscopic analysisAntagonist activity at Adenosine receptor subtype 2B in human RBC assessed as change in erythrocyte morphology incubated for 3 hrs with occasional gentle stirring for every 30 min measured for every 12 hrs by microscopic analysis
ChEMBL 322 6 2 7 2.6 CCCc1cc(O)nc(SC(C)C(=O)Nc2cc(C)no2)n1 10.1016/j.ejmech.2017.05.035
CHEMBL4165135 162364 None 4 Human Functional pEC50 = 7.6 7.6 - 1
Antagonist activity at Adenosine receptor subtype 2B in human RBC assessed as change in erythrocyte morphology incubated for 3 hrs with occasional gentle stirring for every 30 min measured for every 12 hrs by microscopic analysisAntagonist activity at Adenosine receptor subtype 2B in human RBC assessed as change in erythrocyte morphology incubated for 3 hrs with occasional gentle stirring for every 30 min measured for every 12 hrs by microscopic analysis
ChEMBL 322 6 2 7 2.6 CCCc1cc(O)nc(SC(C)C(=O)Nc2cc(C)no2)n1 10.1016/j.ejmech.2017.05.035
168273986 190176 None 0 Human Functional pEC50 = 4.6 4.6 -234422 2
Agonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 505 6 4 10 1.6 OC[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4Oc4cccc(Br)c4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
CHEMBL5174052 190176 None 0 Human Functional pEC50 = 4.6 4.6 -234422 2
Agonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 505 6 4 10 1.6 OC[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4Oc4cccc(Br)c4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
137648928 157405 None 0 Human Functional pEC50 = 6.6 6.6 -97 4
Agonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assayAgonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assay
ChEMBL 549 6 3 12 1.0 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5cccc(I)c5)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
CHEMBL4078479 157405 None 0 Human Functional pEC50 = 6.6 6.6 -97 4
Agonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assayAgonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assay
ChEMBL 549 6 3 12 1.0 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5cccc(I)c5)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
2844 283 None 107 Human Functional pEC50 = 4.6 4.6 -16 5
Agonist activity at human adenosine A2B receptor transfected in CHO cells assessed as changes in cAMP formation in the presence of nitrobenzylthioinosineAgonist activity at human adenosine A2B receptor transfected in CHO cells assessed as changes in cAMP formation in the presence of nitrobenzylthioinosine
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.5b00828
60961 283 None 107 Human Functional pEC50 = 4.6 4.6 -16 5
Agonist activity at human adenosine A2B receptor transfected in CHO cells assessed as changes in cAMP formation in the presence of nitrobenzylthioinosineAgonist activity at human adenosine A2B receptor transfected in CHO cells assessed as changes in cAMP formation in the presence of nitrobenzylthioinosine
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.5b00828
60961.0 283 None 107 Human Functional pEC50 = 4.6 4.6 -16 5
Agonist activity at human adenosine A2B receptor transfected in CHO cells assessed as changes in cAMP formation in the presence of nitrobenzylthioinosineAgonist activity at human adenosine A2B receptor transfected in CHO cells assessed as changes in cAMP formation in the presence of nitrobenzylthioinosine
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.5b00828
90 283 None 107 Human Functional pEC50 = 4.6 4.6 -16 5
Agonist activity at human adenosine A2B receptor transfected in CHO cells assessed as changes in cAMP formation in the presence of nitrobenzylthioinosineAgonist activity at human adenosine A2B receptor transfected in CHO cells assessed as changes in cAMP formation in the presence of nitrobenzylthioinosine
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.5b00828
CHEMBL477 283 None 107 Human Functional pEC50 = 4.6 4.6 -16 5
Agonist activity at human adenosine A2B receptor transfected in CHO cells assessed as changes in cAMP formation in the presence of nitrobenzylthioinosineAgonist activity at human adenosine A2B receptor transfected in CHO cells assessed as changes in cAMP formation in the presence of nitrobenzylthioinosine
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.5b00828
DB00640 283 None 107 Human Functional pEC50 = 4.6 4.6 -16 5
Agonist activity at human adenosine A2B receptor transfected in CHO cells assessed as changes in cAMP formation in the presence of nitrobenzylthioinosineAgonist activity at human adenosine A2B receptor transfected in CHO cells assessed as changes in cAMP formation in the presence of nitrobenzylthioinosine
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.5b00828
137661132 159175 None 0 Human Functional pEC50 = 5.6 5.6 -316 4
Agonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assayAgonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assay
ChEMBL 491 6 3 12 1.7 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5cccc(Cl)c5)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
CHEMBL4098377 159175 None 0 Human Functional pEC50 = 5.6 5.6 -316 4
Agonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assayAgonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assay
ChEMBL 491 6 3 12 1.7 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5cccc(Cl)c5)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
44423825 85400 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 577 11 5 12 1.0 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(Nc4ccc(OCC(=O)NCc5ccc(OC)cc5)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1016/j.bmc.2007.01.055
CHEMBL226304 85400 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 577 11 5 12 1.0 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(Nc4ccc(OCC(=O)NCc5ccc(OC)cc5)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1016/j.bmc.2007.01.055
377 2758 None 53 Human Functional pEC50 = 5.6 5.6 -48 10
Receptor stimulated adenylyl cyclase activity in CHO cells expressing human recombinant Adenosine A2B receptorReceptor stimulated adenylyl cyclase activity in CHO cells expressing human recombinant Adenosine A2B receptor
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1016/s0960-894x(01)00347-x
425 2758 None 53 Human Functional pEC50 = 5.6 5.6 -48 10
Receptor stimulated adenylyl cyclase activity in CHO cells expressing human recombinant Adenosine A2B receptorReceptor stimulated adenylyl cyclase activity in CHO cells expressing human recombinant Adenosine A2B receptor
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1016/s0960-894x(01)00347-x
448222 2758 None 53 Human Functional pEC50 = 5.6 5.6 -48 10
Receptor stimulated adenylyl cyclase activity in CHO cells expressing human recombinant Adenosine A2B receptorReceptor stimulated adenylyl cyclase activity in CHO cells expressing human recombinant Adenosine A2B receptor
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1016/s0960-894x(01)00347-x
CHEMBL464859 2758 None 53 Human Functional pEC50 = 5.6 5.6 -48 10
Receptor stimulated adenylyl cyclase activity in CHO cells expressing human recombinant Adenosine A2B receptorReceptor stimulated adenylyl cyclase activity in CHO cells expressing human recombinant Adenosine A2B receptor
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1016/s0960-894x(01)00347-x
2844 283 None 107 Human Functional pEC50 = 4.6 4.6 -16 5
Agonist activity at human adenosine A2B receptor expressed in CHO cellsAgonist activity at human adenosine A2B receptor expressed in CHO cells
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1016/j.bmcl.2011.02.053
60961 283 None 107 Human Functional pEC50 = 4.6 4.6 -16 5
Agonist activity at human adenosine A2B receptor expressed in CHO cellsAgonist activity at human adenosine A2B receptor expressed in CHO cells
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1016/j.bmcl.2011.02.053
60961.0 283 None 107 Human Functional pEC50 = 4.6 4.6 -16 5
Agonist activity at human adenosine A2B receptor expressed in CHO cellsAgonist activity at human adenosine A2B receptor expressed in CHO cells
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1016/j.bmcl.2011.02.053
90 283 None 107 Human Functional pEC50 = 4.6 4.6 -16 5
Agonist activity at human adenosine A2B receptor expressed in CHO cellsAgonist activity at human adenosine A2B receptor expressed in CHO cells
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1016/j.bmcl.2011.02.053
CHEMBL477 283 None 107 Human Functional pEC50 = 4.6 4.6 -16 5
Agonist activity at human adenosine A2B receptor expressed in CHO cellsAgonist activity at human adenosine A2B receptor expressed in CHO cells
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1016/j.bmcl.2011.02.053
DB00640 283 None 107 Human Functional pEC50 = 4.6 4.6 -16 5
Agonist activity at human adenosine A2B receptor expressed in CHO cellsAgonist activity at human adenosine A2B receptor expressed in CHO cells
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1016/j.bmcl.2011.02.053
2844 283 None 107 Human Functional pEC50 = 4.6 4.6 -16 5
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase of intracellular calcium levelAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase of intracellular calcium level
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1016/j.bmcl.2010.05.056
60961 283 None 107 Human Functional pEC50 = 4.6 4.6 -16 5
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase of intracellular calcium levelAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase of intracellular calcium level
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1016/j.bmcl.2010.05.056
60961.0 283 None 107 Human Functional pEC50 = 4.6 4.6 -16 5
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase of intracellular calcium levelAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase of intracellular calcium level
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1016/j.bmcl.2010.05.056
90 283 None 107 Human Functional pEC50 = 4.6 4.6 -16 5
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase of intracellular calcium levelAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase of intracellular calcium level
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1016/j.bmcl.2010.05.056
CHEMBL477 283 None 107 Human Functional pEC50 = 4.6 4.6 -16 5
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase of intracellular calcium levelAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase of intracellular calcium level
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1016/j.bmcl.2010.05.056
DB00640 283 None 107 Human Functional pEC50 = 4.6 4.6 -16 5
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase of intracellular calcium levelAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase of intracellular calcium level
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1016/j.bmcl.2010.05.056
2844 283 None 107 Human Functional pEC50 = 4.6 4.6 -16 5
Agonist activity at human recombinant adenosine receptor A2b by cAMP assayAgonist activity at human recombinant adenosine receptor A2b by cAMP assay
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm4011669
60961 283 None 107 Human Functional pEC50 = 4.6 4.6 -16 5
Agonist activity at human recombinant adenosine receptor A2b by cAMP assayAgonist activity at human recombinant adenosine receptor A2b by cAMP assay
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm4011669
60961.0 283 None 107 Human Functional pEC50 = 4.6 4.6 -16 5
Agonist activity at human recombinant adenosine receptor A2b by cAMP assayAgonist activity at human recombinant adenosine receptor A2b by cAMP assay
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm4011669
90 283 None 107 Human Functional pEC50 = 4.6 4.6 -16 5
Agonist activity at human recombinant adenosine receptor A2b by cAMP assayAgonist activity at human recombinant adenosine receptor A2b by cAMP assay
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm4011669
CHEMBL477 283 None 107 Human Functional pEC50 = 4.6 4.6 -16 5
Agonist activity at human recombinant adenosine receptor A2b by cAMP assayAgonist activity at human recombinant adenosine receptor A2b by cAMP assay
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm4011669
DB00640 283 None 107 Human Functional pEC50 = 4.6 4.6 -16 5
Agonist activity at human recombinant adenosine receptor A2b by cAMP assayAgonist activity at human recombinant adenosine receptor A2b by cAMP assay
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm4011669
168278159 190360 None 0 Human Functional pEC50 = 6.6 6.6 23 4
Agonist activity at A2BR in human NHVCF cells assessed as cAMP accumulation incubated for 30 mins in presence of PSB603 by LANCE cAMP assayAgonist activity at A2BR in human NHVCF cells assessed as cAMP accumulation incubated for 30 mins in presence of PSB603 by LANCE cAMP assay
ChEMBL 839 15 5 15 6.6 Nc1sc(-c2ccc(-c3cn(CCCCCCNc4ncnc5c4ncn5[C@@H]4O[C@H](CO)[C@@H](O)[C@H]4O)nn3)cc2)c(-c2cccc(C(F)(F)F)c2)c1C(=O)c1ccccc1 10.1021/acs.jmedchem.2c00320
CHEMBL5177040 190360 None 0 Human Functional pEC50 = 6.6 6.6 23 4
Agonist activity at A2BR in human NHVCF cells assessed as cAMP accumulation incubated for 30 mins in presence of PSB603 by LANCE cAMP assayAgonist activity at A2BR in human NHVCF cells assessed as cAMP accumulation incubated for 30 mins in presence of PSB603 by LANCE cAMP assay
ChEMBL 839 15 5 15 6.6 Nc1sc(-c2ccc(-c3cn(CCCCCCNc4ncnc5c4ncn5[C@@H]4O[C@H](CO)[C@@H](O)[C@H]4O)nn3)cc2)c(-c2cccc(C(F)(F)F)c2)c1C(=O)c1ccccc1 10.1021/acs.jmedchem.2c00320
377 2758 None 53 Human Functional pEC50 = 6.6 6.6 -48 10
Relative efficacy against phenylephrine precontracted tissue relaxation in Guinea pig aortaRelative efficacy against phenylephrine precontracted tissue relaxation in Guinea pig aorta
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm031143+
425 2758 None 53 Human Functional pEC50 = 6.6 6.6 -48 10
Relative efficacy against phenylephrine precontracted tissue relaxation in Guinea pig aortaRelative efficacy against phenylephrine precontracted tissue relaxation in Guinea pig aorta
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm031143+
448222 2758 None 53 Human Functional pEC50 = 6.6 6.6 -48 10
Relative efficacy against phenylephrine precontracted tissue relaxation in Guinea pig aortaRelative efficacy against phenylephrine precontracted tissue relaxation in Guinea pig aorta
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm031143+
CHEMBL464859 2758 None 53 Human Functional pEC50 = 6.6 6.6 -48 10
Relative efficacy against phenylephrine precontracted tissue relaxation in Guinea pig aortaRelative efficacy against phenylephrine precontracted tissue relaxation in Guinea pig aorta
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm031143+
76325694 106061 None 0 Human Functional pEC50 = 5.6 5.6 -39 4
Agonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 391 4 5 10 -0.5 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NC4CCCCC4)nc(N)nc32)[C@H](O)[C@@H]1O 10.1039/C3MD00364G
CHEMBL3133159 106061 None 0 Human Functional pEC50 = 5.6 5.6 -39 4
Agonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 391 4 5 10 -0.5 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NC4CCCCC4)nc(N)nc32)[C@H](O)[C@@H]1O 10.1039/C3MD00364G
57388055 75484 None 0 Human Functional pEC50 = 6.6 6.6 -40 4
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 622 12 6 11 3.1 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(NCCc4ccc(N)cc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm300206u
CHEMBL2042306 75484 None 0 Human Functional pEC50 = 6.6 6.6 -40 4
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 622 12 6 11 3.1 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(NCCc4ccc(N)cc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm300206u
137641990 158079 None 0 Human Functional pEC50 = 5.6 5.6 -48 4
Agonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assayAgonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assay
ChEMBL 447 6 3 13 0.7 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5ccco5)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
CHEMBL4086325 158079 None 0 Human Functional pEC50 = 5.6 5.6 -48 4
Agonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assayAgonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assay
ChEMBL 447 6 3 13 0.7 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5ccco5)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
16204411 84747 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 376 6 5 10 -1.0 Nc1nc(OCCc2cc[nH]c2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm061278q
CHEMBL222945 84747 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 376 6 5 10 -1.0 Nc1nc(OCCc2cc[nH]c2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm061278q
168290340 191893 None 0 Human Functional pEC50 = 4.6 4.6 -7943 3
Agonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 475 7 4 10 1.6 OC[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4OCc4ccccc4Cl)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
CHEMBL5199871 191893 None 0 Human Functional pEC50 = 4.6 4.6 -7943 3
Agonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 475 7 4 10 1.6 OC[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4OCc4ccccc4Cl)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
16103165 83382 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP levelsActivity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP levels
ChEMBL 447 6 5 11 -0.3 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NNC(=O)c4ccc(C)s4)ncnc32)[C@H](O)[C@@H]1O 10.1021/jm061170a
CHEMBL219411 83382 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP levelsActivity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP levels
ChEMBL 447 6 5 11 -0.3 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NNC(=O)c4ccc(C)s4)ncnc32)[C@H](O)[C@@H]1O 10.1021/jm061170a
137639588 156884 None 0 Human Functional pEC50 = 6.5 6.5 -1 3
Agonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 815 15 6 13 6.1 Nc1sc(-c2ccccc2C(=O)NCCCCCCNc2ncnc3c2ncn3[C@@H]2O[C@H](CO)[C@@H](O)[C@H]2O)c(-c2cccc(C(F)(F)F)c2)c1C(=O)c1ccccc1 10.1021/acs.jmedchem.8b00047
CHEMBL4072009 156884 None 0 Human Functional pEC50 = 6.5 6.5 -1 3
Agonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 815 15 6 13 6.1 Nc1sc(-c2ccccc2C(=O)NCCCCCCNc2ncnc3c2ncn3[C@@H]2O[C@H](CO)[C@@H](O)[C@H]2O)c(-c2cccc(C(F)(F)F)c2)c1C(=O)c1ccccc1 10.1021/acs.jmedchem.8b00047
24827289 167423 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of adenylate cyclaseAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of adenylate cyclase
ChEMBL 613 9 6 12 1.7 O=C(NNc1nc(OCCc2c[nH]c3cc(Br)ccc23)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O)c1ccco1 10.1021/jm701442d
CHEMBL429684 167423 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of adenylate cyclaseAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of adenylate cyclase
ChEMBL 613 9 6 12 1.7 O=C(NNc1nc(OCCc2c[nH]c3cc(Br)ccc23)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O)c1ccco1 10.1021/jm701442d
3044933 16483 None 6 Human Functional pEC50 = 4.5 4.5 - 1
Effective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNAEffective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNA
ChEMBL 322 4 4 9 -1.4 CCCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)ncnc32)[C@H](O)[C@@H]1O 10.1021/jm9804984
CHEMBL1235128 16483 None 6 Human Functional pEC50 = 4.5 4.5 - 1
Effective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNAEffective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNA
ChEMBL 322 4 4 9 -1.4 CCCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)ncnc32)[C@H](O)[C@@H]1O 10.1021/jm9804984
57388056 75485 None 0 Human Functional pEC50 = 6.5 6.5 -9 4
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 685 12 5 10 4.2 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(NCCc4ccc(Br)cc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm300206u
CHEMBL2042307 75485 None 0 Human Functional pEC50 = 6.5 6.5 -9 4
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 685 12 5 10 4.2 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(NCCc4ccc(Br)cc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm300206u
16203429 84807 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 426 6 5 10 0.1 Nc1nc(OCCc2c[nH]c3ccccc23)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm061278q
CHEMBL223366 84807 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 426 6 5 10 0.1 Nc1nc(OCCc2c[nH]c3ccccc23)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm061278q
377 2758 None 53 Human Functional pEC50 = 8.5 8.5 -48 10
Agonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1039/C3MD00364G
425 2758 None 53 Human Functional pEC50 = 8.5 8.5 -48 10
Agonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1039/C3MD00364G
448222 2758 None 53 Human Functional pEC50 = 8.5 8.5 -48 10
Agonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1039/C3MD00364G
CHEMBL464859 2758 None 53 Human Functional pEC50 = 8.5 8.5 -48 10
Agonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1039/C3MD00364G
44423815 85384 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 659 9 5 11 1.9 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(Nc4ccc(OCC(=O)Nc5ccc(I)cc5)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1016/j.bmc.2007.01.055
CHEMBL226242 85384 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 659 9 5 11 1.9 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(Nc4ccc(OCC(=O)Nc5ccc(I)cc5)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1016/j.bmc.2007.01.055
44423822 85399 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 618 10 5 13 1.2 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(Nc4ccc(OCC(=O)Nc5ccc(N6CCOCC6)cc5)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1016/j.bmc.2007.01.055
CHEMBL226303 85399 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 618 10 5 13 1.2 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(Nc4ccc(OCC(=O)Nc5ccc(N6CCOCC6)cc5)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1016/j.bmc.2007.01.055
70689262 77977 None 0 Human Functional pEC50 = 5.5 5.5 -954 3
Relative efficacy against phenylephrine precontracted tissue relaxation in Guinea pig aortaRelative efficacy against phenylephrine precontracted tissue relaxation in Guinea pig aorta
ChEMBL 496 8 4 14 0.5 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(N[C@H](C)Cc5ccc(OC)cc5)nc43)[C@H](O)[C@@H]2O)n1 10.1021/jm031143+
CHEMBL2096798 77977 None 0 Human Functional pEC50 = 5.5 5.5 -954 3
Relative efficacy against phenylephrine precontracted tissue relaxation in Guinea pig aortaRelative efficacy against phenylephrine precontracted tissue relaxation in Guinea pig aorta
ChEMBL 496 8 4 14 0.5 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(N[C@H](C)Cc5ccc(OC)cc5)nc43)[C@H](O)[C@@H]2O)n1 10.1021/jm031143+
71456259 79233 None 0 Human Functional pEC50 = 4.5 4.5 - 1
Effective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNAEffective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNA
ChEMBL 376 4 4 9 -0.9 Nc1ncnc2c1ncn2[C@@H]1O[C@H](C(=O)NCCC(F)(F)F)[C@@H](O)[C@H]1O 10.1021/jm9804984
CHEMBL2113435 79233 None 0 Human Functional pEC50 = 4.5 4.5 - 1
Effective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNAEffective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNA
ChEMBL 376 4 4 9 -0.9 Nc1ncnc2c1ncn2[C@@H]1O[C@H](C(=O)NCCC(F)(F)F)[C@@H](O)[C@H]1O 10.1021/jm9804984
44423838 142277 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 573 9 5 11 1.8 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(Nc4ccc(OCC(=O)NC5CCCCC5)cc4)nc(Cl)nc32)[C@H](O)[C@@H]1O 10.1016/j.bmc.2007.01.055
CHEMBL388505 142277 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 573 9 5 11 1.8 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(Nc4ccc(OCC(=O)NC5CCCCC5)cc4)nc(Cl)nc32)[C@H](O)[C@@H]1O 10.1016/j.bmc.2007.01.055
11717831 585 None 48 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assayAgonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assay
ChEMBL 379 7 2 7 2.4 N#Cc1c(N)nc(c(c1c1ccc(cc1)OCC1CC1)C#N)SCC(=O)N 10.1016/j.ejmech.2018.02.081
3289 585 None 48 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assayAgonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assay
ChEMBL 379 7 2 7 2.4 N#Cc1c(N)nc(c(c1c1ccc(cc1)OCC1CC1)C#N)SCC(=O)N 10.1016/j.ejmech.2018.02.081
CHEMBL4202825 585 None 48 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assayAgonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assay
ChEMBL 379 7 2 7 2.4 N#Cc1c(N)nc(c(c1c1ccc(cc1)OCC1CC1)C#N)SCC(=O)N 10.1016/j.ejmech.2018.02.081
123683 3121 None 63 Human Functional pEC50 = 7.5 7.5 -1258 5
Agonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1039/C3MD00364G
422 3121 None 63 Human Functional pEC50 = 7.5 7.5 -1258 5
Agonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1039/C3MD00364G
CHEMBL119709 3121 None 63 Human Functional pEC50 = 7.5 7.5 -1258 5
Agonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1039/C3MD00364G
DB05511 3121 None 63 Human Functional pEC50 = 7.5 7.5 -1258 5
Agonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1039/C3MD00364G
377 2758 None 53 Human Functional pEC50 = 5.5 5.5 -48 10
Effective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNAEffective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNA
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm9804984
425 2758 None 53 Human Functional pEC50 = 5.5 5.5 -48 10
Effective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNAEffective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNA
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm9804984
448222 2758 None 53 Human Functional pEC50 = 5.5 5.5 -48 10
Effective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNAEffective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNA
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm9804984
CHEMBL464859 2758 None 53 Human Functional pEC50 = 5.5 5.5 -48 10
Effective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNAEffective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNA
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm9804984
44423826 85402 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 539 9 5 11 1.2 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(Nc4ccc(OCC(=O)NC5CCCCC5)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1016/j.bmc.2007.01.055
CHEMBL226307 85402 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 539 9 5 11 1.2 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(Nc4ccc(OCC(=O)NC5CCCCC5)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1016/j.bmc.2007.01.055
118732979 118520 None 0 Human Functional pEC50 = 5.5 5.5 -426 4
Agonist activity at human recombinant adenosine A2B receptor transfected in CHO cells assessed as induction of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2B receptor transfected in CHO cells assessed as induction of adenylyl cyclase activity
ChEMBL 437 5 3 13 0.0 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NC5CCCO5)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.5b00074
CHEMBL3414945 118520 None 0 Human Functional pEC50 = 5.5 5.5 -426 4
Agonist activity at human recombinant adenosine A2B receptor transfected in CHO cells assessed as induction of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2B receptor transfected in CHO cells assessed as induction of adenylyl cyclase activity
ChEMBL 437 5 3 13 0.0 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NC5CCCO5)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.5b00074
44423823 142195 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 534 9 5 12 0.7 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(Nc4ccc(OCC(=O)Nc5ccncc5)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1016/j.bmc.2007.01.055
CHEMBL388406 142195 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 534 9 5 12 0.7 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(Nc4ccc(OCC(=O)Nc5ccncc5)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1016/j.bmc.2007.01.055
44423817 85385 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 563 10 5 12 1.4 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(Nc4ccc(OCC(=O)Nc5ccc(OC)cc5)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1016/j.bmc.2007.01.055
CHEMBL226243 85385 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 563 10 5 12 1.4 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(Nc4ccc(OCC(=O)Nc5ccc(OC)cc5)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1016/j.bmc.2007.01.055
10688700 76932 None 0 Human Functional pEC50 = 4.5 4.5 - 1
Effective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNAEffective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNA
ChEMBL 342 4 4 9 -1.6 Nc1ncnc2c1ncn2[C@@H]1O[C@H](C(=O)NCCCl)[C@@H](O)[C@H]1O 10.1021/jm9804984
CHEMBL2070399 76932 None 0 Human Functional pEC50 = 4.5 4.5 - 1
Effective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNAEffective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNA
ChEMBL 342 4 4 9 -1.6 Nc1ncnc2c1ncn2[C@@H]1O[C@H](C(=O)NCCCl)[C@@H](O)[C@H]1O 10.1021/jm9804984
16203668 96340 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 454 8 5 10 1.0 CCNc1nc(OCCc2c[nH]c3ccccc23)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm061278q
CHEMBL261515 96340 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 454 8 5 10 1.0 CCNc1nc(OCCc2c[nH]c3ccccc23)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm061278q
377 2758 None 53 Human Functional pEC50 = 6.5 6.5 -48 10
Agonist activity at human recombinant adenosine receptor A2b by cAMP assayAgonist activity at human recombinant adenosine receptor A2b by cAMP assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm4011669
425 2758 None 53 Human Functional pEC50 = 6.5 6.5 -48 10
Agonist activity at human recombinant adenosine receptor A2b by cAMP assayAgonist activity at human recombinant adenosine receptor A2b by cAMP assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm4011669
448222 2758 None 53 Human Functional pEC50 = 6.5 6.5 -48 10
Agonist activity at human recombinant adenosine receptor A2b by cAMP assayAgonist activity at human recombinant adenosine receptor A2b by cAMP assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm4011669
CHEMBL464859 2758 None 53 Human Functional pEC50 = 6.5 6.5 -48 10
Agonist activity at human recombinant adenosine receptor A2b by cAMP assayAgonist activity at human recombinant adenosine receptor A2b by cAMP assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm4011669
10449535 76934 None 0 Human Functional pEC50 = 4.5 4.5 -2187 3
Effective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNAEffective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNA
ChEMBL 334 3 4 9 -1.3 Nc1ncnc2c1ncn2[C@@H]1O[C@H](C(=O)NC2CCC2)[C@@H](O)[C@H]1O 10.1021/jm9804984
CHEMBL2070507 76934 None 0 Human Functional pEC50 = 4.5 4.5 -2187 3
Effective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNAEffective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNA
ChEMBL 334 3 4 9 -1.3 Nc1ncnc2c1ncn2[C@@H]1O[C@H](C(=O)NC2CCC2)[C@@H](O)[C@H]1O 10.1021/jm9804984
377 2758 None 53 Human Functional pEC50 = 6.5 6.5 -48 10
Agonist activity at A2BR in human NHVCF cells assessed as cAMP accumulation incubated for 30 mins in presence of PSB603 by LANCE cAMP assayAgonist activity at A2BR in human NHVCF cells assessed as cAMP accumulation incubated for 30 mins in presence of PSB603 by LANCE cAMP assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.2c00320
425 2758 None 53 Human Functional pEC50 = 6.5 6.5 -48 10
Agonist activity at A2BR in human NHVCF cells assessed as cAMP accumulation incubated for 30 mins in presence of PSB603 by LANCE cAMP assayAgonist activity at A2BR in human NHVCF cells assessed as cAMP accumulation incubated for 30 mins in presence of PSB603 by LANCE cAMP assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.2c00320
448222 2758 None 53 Human Functional pEC50 = 6.5 6.5 -48 10
Agonist activity at A2BR in human NHVCF cells assessed as cAMP accumulation incubated for 30 mins in presence of PSB603 by LANCE cAMP assayAgonist activity at A2BR in human NHVCF cells assessed as cAMP accumulation incubated for 30 mins in presence of PSB603 by LANCE cAMP assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.2c00320
CHEMBL464859 2758 None 53 Human Functional pEC50 = 6.5 6.5 -48 10
Agonist activity at A2BR in human NHVCF cells assessed as cAMP accumulation incubated for 30 mins in presence of PSB603 by LANCE cAMP assayAgonist activity at A2BR in human NHVCF cells assessed as cAMP accumulation incubated for 30 mins in presence of PSB603 by LANCE cAMP assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.2c00320
145967103 164137 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assayAgonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assay
ChEMBL 376 6 2 7 3.5 CCOc1ccc(-c2c(C#N)c(N)nc(SCc3ccn[nH]3)c2C#N)cc1 10.1016/j.ejmech.2018.02.081
CHEMBL4210096 164137 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assayAgonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assay
ChEMBL 376 6 2 7 3.5 CCOc1ccc(-c2c(C#N)c(N)nc(SCc3ccn[nH]3)c2C#N)cc1 10.1016/j.ejmech.2018.02.081
127043828 141125 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Antagonist activity at human adenosine receptor A2b expressed in CHO cell membranes assessed as inhibition of NECA-induced cAMP accumulation measured as NECA EC50 at 2 uM incubated for 15 mins in presence of [3H]cAMP by liquid scintillation counting (Rvb = 73 nM)Antagonist activity at human adenosine receptor A2b expressed in CHO cell membranes assessed as inhibition of NECA-induced cAMP accumulation measured as NECA EC50 at 2 uM incubated for 15 mins in presence of [3H]cAMP by liquid scintillation counting (Rvb = 73 nM)
ChEMBL 538 15 0 9 4.1 CCCCn1c(=O)c2c(nc3n2CCCN3CCc2ccc(OCCN(CC)CC)cc2)n(CCCC)c1=O 10.1016/j.bmc.2016.07.028
CHEMBL3827331 141125 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Antagonist activity at human adenosine receptor A2b expressed in CHO cell membranes assessed as inhibition of NECA-induced cAMP accumulation measured as NECA EC50 at 2 uM incubated for 15 mins in presence of [3H]cAMP by liquid scintillation counting (Rvb = 73 nM)Antagonist activity at human adenosine receptor A2b expressed in CHO cell membranes assessed as inhibition of NECA-induced cAMP accumulation measured as NECA EC50 at 2 uM incubated for 15 mins in presence of [3H]cAMP by liquid scintillation counting (Rvb = 73 nM)
ChEMBL 538 15 0 9 4.1 CCCCn1c(=O)c2c(nc3n2CCCN3CCc2ccc(OCCN(CC)CC)cc2)n(CCCC)c1=O 10.1016/j.bmc.2016.07.028
15729982 7900 None 0 Human Functional pEC50 = 4.5 4.5 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 245 2 1 8 0.4 CN(C)c1nc(N)n2nc(-c3ccco3)nc2n1 10.1016/j.bmc.2010.02.039
CHEMBL1090124 7900 None 0 Human Functional pEC50 = 4.5 4.5 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 245 2 1 8 0.4 CN(C)c1nc(N)n2nc(-c3ccco3)nc2n1 10.1016/j.bmc.2010.02.039
11256992 17944 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Agonistic activity against human adenosine A2B receptor expressed in CHO cellsAgonistic activity against human adenosine A2B receptor expressed in CHO cells
ChEMBL 362 5 2 7 3.1 COc1cccc(-c2c(C#N)c(N)nc(SCc3ncc[nH]3)c2C#N)c1 10.1021/jm049947s
CHEMBL125979 17944 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Agonistic activity against human adenosine A2B receptor expressed in CHO cellsAgonistic activity against human adenosine A2B receptor expressed in CHO cells
ChEMBL 362 5 2 7 3.1 COc1cccc(-c2c(C#N)c(N)nc(SCc3ncc[nH]3)c2C#N)c1 10.1021/jm049947s
51112335 162235 None 6 Human Functional pEC50 = 7.5 7.5 - 1
Antagonist activity at Adenosine receptor subtype 2B in human RBC assessed as change in erythrocyte morphology incubated for 3 hrs with occasional gentle stirring for every 30 min measured for every 12 hrs by microscopic analysisAntagonist activity at Adenosine receptor subtype 2B in human RBC assessed as change in erythrocyte morphology incubated for 3 hrs with occasional gentle stirring for every 30 min measured for every 12 hrs by microscopic analysis
ChEMBL 311 4 2 6 2.4 Cc1cc(NC(=O)CNc2ccc3c(c2)OC(F)(F)O3)on1 10.1016/j.ejmech.2017.05.035
CHEMBL4163380 162235 None 6 Human Functional pEC50 = 7.5 7.5 - 1
Antagonist activity at Adenosine receptor subtype 2B in human RBC assessed as change in erythrocyte morphology incubated for 3 hrs with occasional gentle stirring for every 30 min measured for every 12 hrs by microscopic analysisAntagonist activity at Adenosine receptor subtype 2B in human RBC assessed as change in erythrocyte morphology incubated for 3 hrs with occasional gentle stirring for every 30 min measured for every 12 hrs by microscopic analysis
ChEMBL 311 4 2 6 2.4 Cc1cc(NC(=O)CNc2ccc3c(c2)OC(F)(F)O3)on1 10.1016/j.ejmech.2017.05.035
56783276 162471 None 3 Human Functional pEC50 = 7.5 7.5 - 1
Antagonist activity at Adenosine receptor subtype 2B in human RBC assessed as change in erythrocyte morphology incubated for 3 hrs with occasional gentle stirring for every 30 min measured for every 12 hrs by microscopic analysisAntagonist activity at Adenosine receptor subtype 2B in human RBC assessed as change in erythrocyte morphology incubated for 3 hrs with occasional gentle stirring for every 30 min measured for every 12 hrs by microscopic analysis
ChEMBL 319 6 1 7 1.6 CC(C)c1noc(OCC(=O)NCc2ccc3c(c2)OCO3)n1 10.1016/j.ejmech.2017.05.035
CHEMBL4167064 162471 None 3 Human Functional pEC50 = 7.5 7.5 - 1
Antagonist activity at Adenosine receptor subtype 2B in human RBC assessed as change in erythrocyte morphology incubated for 3 hrs with occasional gentle stirring for every 30 min measured for every 12 hrs by microscopic analysisAntagonist activity at Adenosine receptor subtype 2B in human RBC assessed as change in erythrocyte morphology incubated for 3 hrs with occasional gentle stirring for every 30 min measured for every 12 hrs by microscopic analysis
ChEMBL 319 6 1 7 1.6 CC(C)c1noc(OCC(=O)NCc2ccc3c(c2)OCO3)n1 10.1016/j.ejmech.2017.05.035
16103186 158848 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP levelsActivity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP levels
ChEMBL 481 6 5 11 0.4 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NNC(=O)c4sccc4C)nc(Cl)nc32)[C@H](O)[C@@H]1O 10.1021/jm061170a
CHEMBL409483 158848 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP levelsActivity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP levels
ChEMBL 481 6 5 11 0.4 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NNC(=O)c4sccc4C)nc(Cl)nc32)[C@H](O)[C@@H]1O 10.1021/jm061170a
3071852 8397 None 7 Human Functional pEC50 = 5.5 5.5 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 294 3 1 8 2.2 Nc1nc(Oc2ccccc2)nc2nc(-c3ccco3)nn12 10.1016/j.bmc.2010.02.039
CHEMBL1093313 8397 None 7 Human Functional pEC50 = 5.5 5.5 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 294 3 1 8 2.2 Nc1nc(Oc2ccccc2)nc2nc(-c3ccco3)nn12 10.1016/j.bmc.2010.02.039
145965011 164200 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assayAgonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assay
ChEMBL 470 8 1 8 4.9 COC(=O)c1cccc(CSc2nc(N)c(C#N)c(-c3ccc(OCC4CC4)cc3)c2C#N)c1 10.1016/j.ejmech.2018.02.081
CHEMBL4210852 164200 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assayAgonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assay
ChEMBL 470 8 1 8 4.9 COC(=O)c1cccc(CSc2nc(N)c(C#N)c(-c3ccc(OCC4CC4)cc3)c2C#N)c1 10.1016/j.ejmech.2018.02.081
118732971 118511 None 0 Human Functional pEC50 = 6.5 6.5 -147 4
Agonist activity at human recombinant adenosine A2B receptor transfected in CHO cells assessed as induction of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2B receptor transfected in CHO cells assessed as induction of adenylyl cyclase activity
ChEMBL 333 3 3 12 -1.6 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.5b00074
CHEMBL3414936 118511 None 0 Human Functional pEC50 = 6.5 6.5 -147 4
Agonist activity at human recombinant adenosine A2B receptor transfected in CHO cells assessed as induction of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2B receptor transfected in CHO cells assessed as induction of adenylyl cyclase activity
ChEMBL 333 3 3 12 -1.6 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.5b00074
131432 137057 None 12 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 387 6 4 10 -0.4 Nc1nc(OCCc2ccccc2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm061278q
CHEMBL374685 137057 None 12 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 387 6 4 10 -0.4 Nc1nc(OCCc2ccccc2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm061278q
137661505 159496 None 0 Human Functional pEC50 = 7.5 7.5 2 4
Agonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 815 15 6 13 6.1 Nc1sc(-c2cccc(C(=O)NCCCCCCNc3ncnc4c3ncn4[C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)c2)c(-c2cccc(C(F)(F)F)c2)c1C(=O)c1ccccc1 10.1021/acs.jmedchem.8b00047
CHEMBL4101850 159496 None 0 Human Functional pEC50 = 7.5 7.5 2 4
Agonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 815 15 6 13 6.1 Nc1sc(-c2cccc(C(=O)NCCCCCCNc3ncnc4c3ncn4[C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)c2)c(-c2cccc(C(F)(F)F)c2)c1C(=O)c1ccccc1 10.1021/acs.jmedchem.8b00047
44423820 142099 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 577 9 5 13 1.1 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(Nc4ccc(OCC(=O)Nc5ccc6c(c5)OCO6)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1016/j.bmc.2007.01.055
CHEMBL388194 142099 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 577 9 5 13 1.1 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(Nc4ccc(OCC(=O)Nc5ccc6c(c5)OCO6)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1016/j.bmc.2007.01.055
118732973 118514 None 0 Human Functional pEC50 = 5.5 5.5 -446 4
Agonist activity at human recombinant adenosine A2B receptor transfected in CHO cells assessed as induction of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2B receptor transfected in CHO cells assessed as induction of adenylyl cyclase activity
ChEMBL 381 4 3 12 -0.5 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NC)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.5b00074
CHEMBL3414939 118514 None 0 Human Functional pEC50 = 5.5 5.5 -446 4
Agonist activity at human recombinant adenosine A2B receptor transfected in CHO cells assessed as induction of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2B receptor transfected in CHO cells assessed as induction of adenylyl cyclase activity
ChEMBL 381 4 3 12 -0.5 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NC)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.5b00074
57387825 75478 None 0 Human Functional pEC50 = 6.5 6.5 -8 4
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 505 7 5 10 0.6 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(NCCc4ccc(Br)cc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm300206u
CHEMBL2042300 75478 None 0 Human Functional pEC50 = 6.5 6.5 -8 4
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 505 7 5 10 0.6 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(NCCc4ccc(Br)cc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm300206u
16103187 83297 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP levelsActivity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP levels
ChEMBL 450 6 6 10 -0.7 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NNC(=O)c4ccc[nH]4)nc(Cl)nc32)[C@H](O)[C@@H]1O 10.1021/jm061170a
CHEMBL218989 83297 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP levelsActivity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP levels
ChEMBL 450 6 6 10 -0.7 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NNC(=O)c4ccc[nH]4)nc(Cl)nc32)[C@H](O)[C@@H]1O 10.1021/jm061170a
44423828 85401 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 597 10 5 12 2.0 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(Nc4ccc(OCC(=O)Nc5ccc(OC)cc5)cc4)nc(Cl)nc32)[C@H](O)[C@@H]1O 10.1016/j.bmc.2007.01.055
CHEMBL226305 85401 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 597 10 5 12 2.0 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(Nc4ccc(OCC(=O)Nc5ccc(OC)cc5)cc4)nc(Cl)nc32)[C@H](O)[C@@H]1O 10.1016/j.bmc.2007.01.055
377 2758 None 53 Human Functional pEC50 = 5.4 5.4 -48 10
Activity at human adenosine A2B receptor assessed as stimulation of [3H]cAMP accumulation in CHO cellsActivity at human adenosine A2B receptor assessed as stimulation of [3H]cAMP accumulation in CHO cells
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm061279i
425 2758 None 53 Human Functional pEC50 = 5.4 5.4 -48 10
Activity at human adenosine A2B receptor assessed as stimulation of [3H]cAMP accumulation in CHO cellsActivity at human adenosine A2B receptor assessed as stimulation of [3H]cAMP accumulation in CHO cells
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm061279i
448222 2758 None 53 Human Functional pEC50 = 5.4 5.4 -48 10
Activity at human adenosine A2B receptor assessed as stimulation of [3H]cAMP accumulation in CHO cellsActivity at human adenosine A2B receptor assessed as stimulation of [3H]cAMP accumulation in CHO cells
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm061279i
CHEMBL464859 2758 None 53 Human Functional pEC50 = 5.4 5.4 -48 10
Activity at human adenosine A2B receptor assessed as stimulation of [3H]cAMP accumulation in CHO cellsActivity at human adenosine A2B receptor assessed as stimulation of [3H]cAMP accumulation in CHO cells
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm061279i
16203540 84626 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 504 6 5 10 0.9 Nc1nc(OCCc2c[nH]c3ccc(Br)cc23)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm061278q
CHEMBL222194 84626 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 504 6 5 10 0.9 Nc1nc(OCCc2c[nH]c3ccc(Br)cc23)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm061278q
16103177 83369 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP levelsActivity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP levels
ChEMBL 495 6 5 11 -0.3 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NNC(=O)c4ccc(Br)o4)ncnc32)[C@H](O)[C@@H]1O 10.1021/jm061170a
CHEMBL219361 83369 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP levelsActivity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP levels
ChEMBL 495 6 5 11 -0.3 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NNC(=O)c4ccc(Br)o4)ncnc32)[C@H](O)[C@@H]1O 10.1021/jm061170a
21128750 201663 None 0 Human Functional pEC50 = 4.4 4.4 - 1
Effective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNAEffective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNA
ChEMBL 322 3 4 9 -1.4 CC(C)NC(=O)[C@H]1OC(n2cnc3c(N)ncnc32)[C@H](O)[C@@H]1O 10.1021/jm9804984
CHEMBL606095 201663 None 0 Human Functional pEC50 = 4.4 4.4 - 1
Effective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNAEffective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNA
ChEMBL 322 3 4 9 -1.4 CC(C)NC(=O)[C@H]1OC(n2cnc3c(N)ncnc32)[C@H](O)[C@@H]1O 10.1021/jm9804984
137658761 159182 None 0 Human Functional pEC50 = 5.4 5.4 -66 3
Agonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity in presence of [alpha-31P]ATPAgonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity in presence of [alpha-31P]ATP
ChEMBL 413 4 3 8 2.2 O[C@@H]1[C@@H](CCl)O[C@@H](n2cnc3c(Nc4ccc(Cl)cc4F)ncnc32)[C@@H]1O 10.1021/acs.jmedchem.7b01399
CHEMBL4098408 159182 None 0 Human Functional pEC50 = 5.4 5.4 -66 3
Agonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity in presence of [alpha-31P]ATPAgonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity in presence of [alpha-31P]ATP
ChEMBL 413 4 3 8 2.2 O[C@@H]1[C@@H](CCl)O[C@@H](n2cnc3c(Nc4ccc(Cl)cc4F)ncnc32)[C@@H]1O 10.1021/acs.jmedchem.7b01399
145975919 163865 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assayAgonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assay
ChEMBL 353 6 2 7 2.1 CCOc1ccc(-c2c(C#N)c(N)nc(SCC(N)=O)c2C#N)cc1 10.1016/j.ejmech.2018.02.081
CHEMBL4206762 163865 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assayAgonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assay
ChEMBL 353 6 2 7 2.1 CCOc1ccc(-c2c(C#N)c(N)nc(SCC(N)=O)c2C#N)cc1 10.1016/j.ejmech.2018.02.081
377 2758 None 53 Human Functional pEC50 = 7.4 7.4 -48 10
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as effect on cAMP production by luciferase reporter gene assayAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as effect on cAMP production by luciferase reporter gene assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1016/j.bmcl.2009.11.131
425 2758 None 53 Human Functional pEC50 = 7.4 7.4 -48 10
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as effect on cAMP production by luciferase reporter gene assayAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as effect on cAMP production by luciferase reporter gene assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1016/j.bmcl.2009.11.131
448222 2758 None 53 Human Functional pEC50 = 7.4 7.4 -48 10
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as effect on cAMP production by luciferase reporter gene assayAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as effect on cAMP production by luciferase reporter gene assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1016/j.bmcl.2009.11.131
CHEMBL464859 2758 None 53 Human Functional pEC50 = 7.4 7.4 -48 10
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as effect on cAMP production by luciferase reporter gene assayAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as effect on cAMP production by luciferase reporter gene assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1016/j.bmcl.2009.11.131
168269860 189976 None 0 Human Functional pEC50 = 4.4 4.4 -17782 3
Agonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 512 9 4 11 1.1 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4OCc4cccc(OC)c4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
CHEMBL5170857 189976 None 0 Human Functional pEC50 = 4.4 4.4 -17782 3
Agonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 512 9 4 11 1.1 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4OCc4cccc(OC)c4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
118734376 118638 None 0 Human Functional pEC50 = 6.4 6.4 -14 2
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting methodAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting method
ChEMBL 602 10 4 12 1.5 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(N4CCN(c5ccc(OCCCc6ccccc6)cc5)CC4)nc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.5b00215
CHEMBL3416810 118638 None 0 Human Functional pEC50 = 6.4 6.4 -14 2
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting methodAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting method
ChEMBL 602 10 4 12 1.5 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(N4CCN(c5ccc(OCCCc6ccccc6)cc5)CC4)nc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.5b00215
3086599 904 None 45 Human Functional pEC50 = 7.4 7.4 -1 6
Agonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 499 10 6 11 -0.2 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(NCCc1ccc(cc1)CCC(=O)O)nc2N 10.1039/C3MD00364G
375 904 None 45 Human Functional pEC50 = 7.4 7.4 -1 6
Agonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 499 10 6 11 -0.2 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(NCCc1ccc(cc1)CCC(=O)O)nc2N 10.1039/C3MD00364G
424 904 None 45 Human Functional pEC50 = 7.4 7.4 -1 6
Agonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 499 10 6 11 -0.2 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(NCCc1ccc(cc1)CCC(=O)O)nc2N 10.1039/C3MD00364G
CHEMBL331372 904 None 45 Human Functional pEC50 = 7.4 7.4 -1 6
Agonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 499 10 6 11 -0.2 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(NCCc1ccc(cc1)CCC(=O)O)nc2N 10.1039/C3MD00364G
76336527 106063 None 0 Human Functional pEC50 = 6.4 6.4 -630 4
Agonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 433 5 5 10 0.0 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NCc4cccc(Cl)c4)nc(N)nc32)[C@H](O)[C@@H]1O 10.1039/C3MD00364G
CHEMBL3133161 106063 None 0 Human Functional pEC50 = 6.4 6.4 -630 4
Agonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 433 5 5 10 0.0 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NCc4cccc(Cl)c4)nc(N)nc32)[C@H](O)[C@@H]1O 10.1039/C3MD00364G
71657835 159737 None 3 Human Functional pEC50 = 8.3 8.3 -1 4
Agonist activity at human A2B receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 10 mins in presence of forskolin by LANCE cAMP assayAgonist activity at human A2B receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 10 mins in presence of forskolin by LANCE cAMP assay
ChEMBL 815 15 6 13 6.1 Nc1sc(-c2ccc(C(=O)NCCCCCCNc3ncnc4c3ncn4[C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)cc2)c(-c2cccc(C(F)(F)F)c2)c1C(=O)c1ccccc1 10.1021/acs.jmedchem.2c00320
CHEMBL4104819 159737 None 3 Human Functional pEC50 = 8.3 8.3 -1 4
Agonist activity at human A2B receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 10 mins in presence of forskolin by LANCE cAMP assayAgonist activity at human A2B receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 10 mins in presence of forskolin by LANCE cAMP assay
ChEMBL 815 15 6 13 6.1 Nc1sc(-c2ccc(C(=O)NCCCCCCNc3ncnc4c3ncn4[C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)cc2)c(-c2cccc(C(F)(F)F)c2)c1C(=O)c1ccccc1 10.1021/acs.jmedchem.2c00320
377 2758 None 53 Human Functional pEC50 = 8.3 8.3 -48 10
Agonist activity at human A2B receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 10 mins in presence of forskolin by LANCE cAMP assayAgonist activity at human A2B receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 10 mins in presence of forskolin by LANCE cAMP assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.2c00320
425 2758 None 53 Human Functional pEC50 = 8.3 8.3 -48 10
Agonist activity at human A2B receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 10 mins in presence of forskolin by LANCE cAMP assayAgonist activity at human A2B receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 10 mins in presence of forskolin by LANCE cAMP assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.2c00320
448222 2758 None 53 Human Functional pEC50 = 8.3 8.3 -48 10
Agonist activity at human A2B receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 10 mins in presence of forskolin by LANCE cAMP assayAgonist activity at human A2B receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 10 mins in presence of forskolin by LANCE cAMP assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.2c00320
CHEMBL464859 2758 None 53 Human Functional pEC50 = 8.3 8.3 -48 10
Agonist activity at human A2B receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 10 mins in presence of forskolin by LANCE cAMP assayAgonist activity at human A2B receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 10 mins in presence of forskolin by LANCE cAMP assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.2c00320
57384544 75487 None 0 Human Functional pEC50 = 4.4 4.4 -57 4
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 854 14 7 12 7.0 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(NCCc4ccc(NC(=O)c5cc(C(C)(C)C)c(O)c(C(C)(C)C)c5)cc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm300206u
CHEMBL2042309 75487 None 0 Human Functional pEC50 = 4.4 4.4 -57 4
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 854 14 7 12 7.0 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(NCCc4ccc(NC(=O)c5cc(C(C)(C)C)c(O)c(C(C)(C)C)c5)cc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm300206u
137647420 157701 None 0 Human Functional pEC50 = 6.4 6.4 -194 4
Agonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assayAgonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assay
ChEMBL 501 6 3 12 1.2 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5cccc(Br)c5)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
CHEMBL4081876 157701 None 0 Human Functional pEC50 = 6.4 6.4 -194 4
Agonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assayAgonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assay
ChEMBL 501 6 3 12 1.2 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5cccc(Br)c5)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
44423827 85413 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 567 9 5 11 2.0 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(Nc4ccc(OCC(=O)Nc5ccccc5)cc4)nc(Cl)nc32)[C@H](O)[C@@H]1O 10.1016/j.bmc.2007.01.055
CHEMBL226356 85413 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 567 9 5 11 2.0 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(Nc4ccc(OCC(=O)Nc5ccccc5)cc4)nc(Cl)nc32)[C@H](O)[C@@H]1O 10.1016/j.bmc.2007.01.055
377 2758 None 53 Human Functional pEC50 = 7.4 7.4 -48 10
Irreversible agonist activity at human adenosine A2B receptor expressed in Flp-In-CHO cells assessed as effect on forskolin-induced cAMP accumulation incubated for 30 mins by LANCE cAMP detection assayIrreversible agonist activity at human adenosine A2B receptor expressed in Flp-In-CHO cells assessed as effect on forskolin-induced cAMP accumulation incubated for 30 mins by LANCE cAMP detection assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.6b01561
425 2758 None 53 Human Functional pEC50 = 7.4 7.4 -48 10
Irreversible agonist activity at human adenosine A2B receptor expressed in Flp-In-CHO cells assessed as effect on forskolin-induced cAMP accumulation incubated for 30 mins by LANCE cAMP detection assayIrreversible agonist activity at human adenosine A2B receptor expressed in Flp-In-CHO cells assessed as effect on forskolin-induced cAMP accumulation incubated for 30 mins by LANCE cAMP detection assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.6b01561
448222 2758 None 53 Human Functional pEC50 = 7.4 7.4 -48 10
Irreversible agonist activity at human adenosine A2B receptor expressed in Flp-In-CHO cells assessed as effect on forskolin-induced cAMP accumulation incubated for 30 mins by LANCE cAMP detection assayIrreversible agonist activity at human adenosine A2B receptor expressed in Flp-In-CHO cells assessed as effect on forskolin-induced cAMP accumulation incubated for 30 mins by LANCE cAMP detection assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.6b01561
CHEMBL464859 2758 None 53 Human Functional pEC50 = 7.4 7.4 -48 10
Irreversible agonist activity at human adenosine A2B receptor expressed in Flp-In-CHO cells assessed as effect on forskolin-induced cAMP accumulation incubated for 30 mins by LANCE cAMP detection assayIrreversible agonist activity at human adenosine A2B receptor expressed in Flp-In-CHO cells assessed as effect on forskolin-induced cAMP accumulation incubated for 30 mins by LANCE cAMP detection assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.6b01561
46885404 8023 None 0 Human Functional pEC50 = 4.4 4.4 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 396 6 1 9 2.7 COc1ccc(CC(=O)Nc2nc(SC)nc3nc(-c4ccco4)nn23)cc1 10.1016/j.bmc.2010.02.039
CHEMBL1090806 8023 None 0 Human Functional pEC50 = 4.4 4.4 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 396 6 1 9 2.7 COc1ccc(CC(=O)Nc2nc(SC)nc3nc(-c4ccco4)nn23)cc1 10.1016/j.bmc.2010.02.039
168293442 192135 None 0 Human Functional pEC50 = 5.4 5.4 -17782 4
Agonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 546 7 4 10 1.8 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4Oc4cccc(Br)c4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
CHEMBL5203632 192135 None 0 Human Functional pEC50 = 5.4 5.4 -17782 4
Agonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 546 7 4 10 1.8 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4Oc4cccc(Br)c4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
168297905 192431 None 0 Human Functional pEC50 = 5.4 5.4 -2041 4
Agonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 516 8 4 10 1.8 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4OCc4ccccc4Cl)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
CHEMBL5208245 192431 None 0 Human Functional pEC50 = 5.4 5.4 -2041 4
Agonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 516 8 4 10 1.8 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4OCc4ccccc4Cl)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
377 2758 None 53 Human Functional pEC50 = 6.4 6.4 -48 10
Potency against cAMP formation in CHO cells expressing recombinant human A2B receptorPotency against cAMP formation in CHO cells expressing recombinant human A2B receptor
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm031143+
425 2758 None 53 Human Functional pEC50 = 6.4 6.4 -48 10
Potency against cAMP formation in CHO cells expressing recombinant human A2B receptorPotency against cAMP formation in CHO cells expressing recombinant human A2B receptor
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm031143+
448222 2758 None 53 Human Functional pEC50 = 6.4 6.4 -48 10
Potency against cAMP formation in CHO cells expressing recombinant human A2B receptorPotency against cAMP formation in CHO cells expressing recombinant human A2B receptor
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm031143+
CHEMBL464859 2758 None 53 Human Functional pEC50 = 6.4 6.4 -48 10
Potency against cAMP formation in CHO cells expressing recombinant human A2B receptorPotency against cAMP formation in CHO cells expressing recombinant human A2B receptor
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm031143+
137646655 157626 None 0 Human Functional pEC50 = 6.4 6.4 -6 4
Agonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 711 13 6 12 4.8 Nc1cc(-c2cccc(C(F)(F)F)c2)c(-c2ccc(C(=O)NCCCCCCNc3ncnc4c3ncn4[C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)cc2)s1 10.1021/acs.jmedchem.8b00047
CHEMBL4081224 157626 None 0 Human Functional pEC50 = 6.4 6.4 -6 4
Agonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 711 13 6 12 4.8 Nc1cc(-c2cccc(C(F)(F)F)c2)c(-c2ccc(C(=O)NCCCCCCNc3ncnc4c3ncn4[C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)cc2)s1 10.1021/acs.jmedchem.8b00047
44423818 85386 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 593 11 5 13 1.4 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(Nc4ccc(OCC(=O)Nc5ccc(OC)c(OC)c5)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1016/j.bmc.2007.01.055
CHEMBL226244 85386 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 593 11 5 13 1.4 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(Nc4ccc(OCC(=O)Nc5ccc(OC)c(OC)c5)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1016/j.bmc.2007.01.055
16103184 83296 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP levelsActivity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP levels
ChEMBL 467 6 5 11 0.1 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NNC(=O)c4ccsc4)nc(Cl)nc32)[C@H](O)[C@@H]1O 10.1021/jm061170a
CHEMBL218988 83296 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP levelsActivity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP levels
ChEMBL 467 6 5 11 0.1 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NNC(=O)c4ccsc4)nc(Cl)nc32)[C@H](O)[C@@H]1O 10.1021/jm061170a
3042985 79232 None 2 Human Functional pEC50 = 4.4 4.4 - 1
Effective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNAEffective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNA
ChEMBL 310 3 4 10 -2.3 CONC(=O)[C@H]1O[C@@H](n2cnc3c(N)ncnc32)[C@H](O)[C@@H]1O 10.1021/jm9804984
CHEMBL2113434 79232 None 2 Human Functional pEC50 = 4.4 4.4 - 1
Effective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNAEffective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNA
ChEMBL 310 3 4 10 -2.3 CONC(=O)[C@H]1O[C@@H](n2cnc3c(N)ncnc32)[C@H](O)[C@@H]1O 10.1021/jm9804984
98567 191781 None 18 Human Functional pEC50 = 4.4 4.4 -1174 3
Effective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNAEffective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNA
ChEMBL 294 2 4 9 -2.2 CNC(=O)[C@H]1O[C@@H](n2cnc3c(N)ncnc32)[C@H](O)[C@@H]1O 10.1021/jm9804984
CHEMBL519809 191781 None 18 Human Functional pEC50 = 4.4 4.4 -1174 3
Effective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNAEffective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNA
ChEMBL 294 2 4 9 -2.2 CNC(=O)[C@H]1O[C@@H](n2cnc3c(N)ncnc32)[C@H](O)[C@@H]1O 10.1021/jm9804984
16365293 162898 None 3 Human Functional pEC50 = 7.3 7.3 - 1
Antagonist activity at Adenosine receptor subtype 2B in human RBC assessed as change in erythrocyte morphology incubated for 3 hrs with occasional gentle stirring for every 30 min measured for every 12 hrs by microscopic analysisAntagonist activity at Adenosine receptor subtype 2B in human RBC assessed as change in erythrocyte morphology incubated for 3 hrs with occasional gentle stirring for every 30 min measured for every 12 hrs by microscopic analysis
ChEMBL 344 5 2 8 0.6 CC(OC(=O)c1nccnc1N)C(=O)NCc1ccc2c(c1)OCO2 10.1016/j.ejmech.2017.05.035
CHEMBL4173768 162898 None 3 Human Functional pEC50 = 7.3 7.3 - 1
Antagonist activity at Adenosine receptor subtype 2B in human RBC assessed as change in erythrocyte morphology incubated for 3 hrs with occasional gentle stirring for every 30 min measured for every 12 hrs by microscopic analysisAntagonist activity at Adenosine receptor subtype 2B in human RBC assessed as change in erythrocyte morphology incubated for 3 hrs with occasional gentle stirring for every 30 min measured for every 12 hrs by microscopic analysis
ChEMBL 344 5 2 8 0.6 CC(OC(=O)c1nccnc1N)C(=O)NCc1ccc2c(c1)OCO2 10.1016/j.ejmech.2017.05.035
137652475 157145 None 0 Human Functional pEC50 = 6.3 6.3 -6 4
Agonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 829 16 6 13 6.5 Nc1sc(-c2ccc(C(=O)NCCCCCCCNc3ncnc4c3ncn4[C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)cc2)c(-c2cccc(C(F)(F)F)c2)c1C(=O)c1ccccc1 10.1021/acs.jmedchem.8b00047
CHEMBL4075186 157145 None 0 Human Functional pEC50 = 6.3 6.3 -6 4
Agonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 829 16 6 13 6.5 Nc1sc(-c2ccc(C(=O)NCCCCCCCNc3ncnc4c3ncn4[C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)cc2)c(-c2cccc(C(F)(F)F)c2)c1C(=O)c1ccccc1 10.1021/acs.jmedchem.8b00047
10256007 122929 None 0 Human Functional pEC50 = 5.3 5.3 -47 2
Potency against cAMP formation in CHO cells expressing recombinant human A2B receptorPotency against cAMP formation in CHO cells expressing recombinant human A2B receptor
ChEMBL 516 8 5 14 0.1 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(N[C@H](CO)Cc5ccc(Cl)cc5)nc43)[C@H](O)[C@@H]2O)n1 10.1021/jm031143+
CHEMBL360646 122929 None 0 Human Functional pEC50 = 5.3 5.3 -47 2
Potency against cAMP formation in CHO cells expressing recombinant human A2B receptorPotency against cAMP formation in CHO cells expressing recombinant human A2B receptor
ChEMBL 516 8 5 14 0.1 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(N[C@H](CO)Cc5ccc(Cl)cc5)nc43)[C@H](O)[C@@H]2O)n1 10.1021/jm031143+
10388920 69824 None 7 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity at recombinant human A2BAR expressed in CHO cells assessed as stimulation of cAMP formation preincubated for 30 mins in presence of rolipram and adenosine deaminase followed by compound addition and measured after 20 mins by alphascreen cAMP assayAgonist activity at recombinant human A2BAR expressed in CHO cells assessed as stimulation of cAMP formation preincubated for 30 mins in presence of rolipram and adenosine deaminase followed by compound addition and measured after 20 mins by alphascreen cAMP assay
ChEMBL 447 7 4 9 1.7 OC[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acsmedchemlett.0c00509
CHEMBL193692 69824 None 7 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity at recombinant human A2BAR expressed in CHO cells assessed as stimulation of cAMP formation preincubated for 30 mins in presence of rolipram and adenosine deaminase followed by compound addition and measured after 20 mins by alphascreen cAMP assayAgonist activity at recombinant human A2BAR expressed in CHO cells assessed as stimulation of cAMP formation preincubated for 30 mins in presence of rolipram and adenosine deaminase followed by compound addition and measured after 20 mins by alphascreen cAMP assay
ChEMBL 447 7 4 9 1.7 OC[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acsmedchemlett.0c00509
168285984 191742 None 0 Human Functional pEC50 = 5.3 5.3 -5248 4
Agonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 461 6 4 10 1.5 OC[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4Oc4ccccc4Cl)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
CHEMBL5197358 191742 None 0 Human Functional pEC50 = 5.3 5.3 -5248 4
Agonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 461 6 4 10 1.5 OC[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4Oc4ccccc4Cl)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
76336526 106057 None 0 Human Functional pEC50 = 5.3 5.3 -501 3
Agonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 351 5 5 10 -1.4 CCCNc1nc(N)nc2c1ncn2[C@@H]1O[C@H](C(=O)NC)[C@@H](O)[C@H]1O 10.1039/C3MD00364G
CHEMBL3133155 106057 None 0 Human Functional pEC50 = 5.3 5.3 -501 3
Agonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 351 5 5 10 -1.4 CCCNc1nc(N)nc2c1ncn2[C@@H]1O[C@H](C(=O)NC)[C@@H](O)[C@H]1O 10.1039/C3MD00364G
145972065 164542 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assayAgonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assay
ChEMBL 403 7 2 8 3.3 N#Cc1c(N)nc(SCc2ncn[nH]2)c(C#N)c1-c1ccc(OCC2CC2)cc1 10.1016/j.ejmech.2018.02.081
CHEMBL4215091 164542 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assayAgonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assay
ChEMBL 403 7 2 8 3.3 N#Cc1c(N)nc(SCc2ncn[nH]2)c(C#N)c1-c1ccc(OCC2CC2)cc1 10.1016/j.ejmech.2018.02.081
9869857 66830 None 11 Human Functional pEC50 = 7.3 7.3 -213 5
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as effect on cAMP production by luciferase reporter gene assayAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as effect on cAMP production by luciferase reporter gene assay
ChEMBL 482 8 5 14 -0.6 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(N[C@H](CO)Cc5ccccc5)nc43)[C@H](O)[C@@H]2O)n1 10.1016/j.bmcl.2009.11.131
CHEMBL186113 66830 None 11 Human Functional pEC50 = 7.3 7.3 -213 5
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as effect on cAMP production by luciferase reporter gene assayAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as effect on cAMP production by luciferase reporter gene assay
ChEMBL 482 8 5 14 -0.6 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(N[C@H](CO)Cc5ccccc5)nc43)[C@H](O)[C@@H]2O)n1 10.1016/j.bmcl.2009.11.131
168297825 192283 None 0 Human Functional pEC50 = 5.3 5.3 -8317 4
Agonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 461 6 4 10 1.5 OC[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4Oc4cccc(Cl)c4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
CHEMBL5205907 192283 None 0 Human Functional pEC50 = 5.3 5.3 -8317 4
Agonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 461 6 4 10 1.5 OC[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4Oc4cccc(Cl)c4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
168286257 191596 None 0 Human Functional pEC50 = 7.3 7.3 6 4
Agonist activity at human A2B receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 10 mins in presence of forskolin by LANCE cAMP assayAgonist activity at human A2B receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 10 mins in presence of forskolin by LANCE cAMP assay
ChEMBL 863 14 6 13 6.3 Nc1sc(-c2ccc(C(=O)NCCc3ccc(CCNc4ncnc5c4ncn5[C@@H]4O[C@H](CO)[C@@H](O)[C@H]4O)cc3)cc2)c(-c2cccc(C(F)(F)F)c2)c1C(=O)c1ccccc1 10.1021/acs.jmedchem.2c00320
CHEMBL5195260 191596 None 0 Human Functional pEC50 = 7.3 7.3 6 4
Agonist activity at human A2B receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 10 mins in presence of forskolin by LANCE cAMP assayAgonist activity at human A2B receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 10 mins in presence of forskolin by LANCE cAMP assay
ChEMBL 863 14 6 13 6.3 Nc1sc(-c2ccc(C(=O)NCCc3ccc(CCNc4ncnc5c4ncn5[C@@H]4O[C@H](CO)[C@@H](O)[C@H]4O)cc3)cc2)c(-c2cccc(C(F)(F)F)c2)c1C(=O)c1ccccc1 10.1021/acs.jmedchem.2c00320
2844 283 None 107 Human Functional pEC50 = 7.3 7.3 -16 5
Agonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.2c01414
60961 283 None 107 Human Functional pEC50 = 7.3 7.3 -16 5
Agonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.2c01414
60961.0 283 None 107 Human Functional pEC50 = 7.3 7.3 -16 5
Agonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.2c01414
90 283 None 107 Human Functional pEC50 = 7.3 7.3 -16 5
Agonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.2c01414
CHEMBL477 283 None 107 Human Functional pEC50 = 7.3 7.3 -16 5
Agonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.2c01414
DB00640 283 None 107 Human Functional pEC50 = 7.3 7.3 -16 5
Agonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.2c01414
168293183 192126 None 0 Human Functional pEC50 = 6.3 6.3 1 3
Agonist activity at human A2B receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 10 mins in presence of forskolin by LANCE cAMP assayAgonist activity at human A2B receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 10 mins in presence of forskolin by LANCE cAMP assay
ChEMBL 767 16 6 13 4.7 Nc1sc(CCC(=O)NCCCCCCNc2ncnc3c2ncn3[C@@H]2O[C@H](CO)[C@@H](O)[C@H]2O)c(-c2cccc(C(F)(F)F)c2)c1C(=O)c1ccccc1 10.1021/acs.jmedchem.2c00320
CHEMBL5203535 192126 None 0 Human Functional pEC50 = 6.3 6.3 1 3
Agonist activity at human A2B receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 10 mins in presence of forskolin by LANCE cAMP assayAgonist activity at human A2B receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 10 mins in presence of forskolin by LANCE cAMP assay
ChEMBL 767 16 6 13 4.7 Nc1sc(CCC(=O)NCCCCCCNc2ncnc3c2ncn3[C@@H]2O[C@H](CO)[C@@H](O)[C@H]2O)c(-c2cccc(C(F)(F)F)c2)c1C(=O)c1ccccc1 10.1021/acs.jmedchem.2c00320
137642153 158368 None 0 Human Functional pEC50 = 6.3 6.3 -35 4
Agonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assayAgonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assay
ChEMBL 429 6 3 13 0.5 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5cccs5)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
CHEMBL4089741 158368 None 0 Human Functional pEC50 = 6.3 6.3 -35 4
Agonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assayAgonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assay
ChEMBL 429 6 3 13 0.5 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5cccs5)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
44423819 85387 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 593 11 5 13 1.4 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(Nc4ccc(OCC(=O)Nc5cc(OC)cc(OC)c5)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1016/j.bmc.2007.01.055
CHEMBL226245 85387 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 593 11 5 13 1.4 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(Nc4ccc(OCC(=O)Nc5cc(OC)cc(OC)c5)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1016/j.bmc.2007.01.055
118732980 118521 None 0 Human Functional pEC50 = 6.3 6.3 -63 4
Agonist activity at human recombinant adenosine A2B receptor transfected in CHO cells assessed as induction of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2B receptor transfected in CHO cells assessed as induction of adenylyl cyclase activity
ChEMBL 461 5 3 12 1.4 CCn1nnc([C@H]2O[C@@H](n3cnc4c(Nc5ccc(Cl)cc5F)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.5b00074
CHEMBL3414946 118521 None 0 Human Functional pEC50 = 6.3 6.3 -63 4
Agonist activity at human recombinant adenosine A2B receptor transfected in CHO cells assessed as induction of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2B receptor transfected in CHO cells assessed as induction of adenylyl cyclase activity
ChEMBL 461 5 3 12 1.4 CCn1nnc([C@H]2O[C@@H](n3cnc4c(Nc5ccc(Cl)cc5F)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.5b00074
10403711 96333 None 33 Human Functional pEC50 = 5.3 5.3 -501 3
Effective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNAEffective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNA
ChEMBL 320 3 4 9 -1.7 Nc1ncnc2c1ncn2[C@@H]1O[C@H](C(=O)NC2CC2)[C@@H](O)[C@H]1O 10.1021/jm9804984
CHEMBL261482 96333 None 33 Human Functional pEC50 = 5.3 5.3 -501 3
Effective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNAEffective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNA
ChEMBL 320 3 4 9 -1.7 Nc1ncnc2c1ncn2[C@@H]1O[C@H](C(=O)NC2CC2)[C@@H](O)[C@H]1O 10.1021/jm9804984
44420926 138064 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 350 4 6 9 -2.1 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NC(=N)N)ncnc32)[C@H](O)[C@@H]1O 10.1021/jm061278q
CHEMBL376542 138064 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 350 4 6 9 -2.1 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NC(=N)N)ncnc32)[C@H](O)[C@@H]1O 10.1021/jm061278q
215610 76935 None 4 Human Functional pEC50 = 4.3 4.3 -239 2
Effective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNAEffective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNA
ChEMBL 348 3 4 9 -0.9 Nc1ncnc2c1ncn2[C@@H]1O[C@H](C(=O)NC2CCCC2)[C@@H](O)[C@H]1O 10.1021/jm9804984
CHEMBL2070508 76935 None 4 Human Functional pEC50 = 4.3 4.3 -239 2
Effective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNAEffective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNA
ChEMBL 348 3 4 9 -0.9 Nc1ncnc2c1ncn2[C@@H]1O[C@H](C(=O)NC2CCCC2)[C@@H](O)[C@H]1O 10.1021/jm9804984
56627882 118512 None 0 Human Functional pEC50 = 6.3 6.3 -141 4
Agonist activity at human recombinant adenosine A2B receptor transfected in CHO cells assessed as induction of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2B receptor transfected in CHO cells assessed as induction of adenylyl cyclase activity
ChEMBL 367 3 3 12 -0.9 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.5b00074
CHEMBL3414937 118512 None 0 Human Functional pEC50 = 6.3 6.3 -141 4
Agonist activity at human recombinant adenosine A2B receptor transfected in CHO cells assessed as induction of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2B receptor transfected in CHO cells assessed as induction of adenylyl cyclase activity
ChEMBL 367 3 3 12 -0.9 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.5b00074
11157262 123640 None 0 Human Functional pEC50 = 6.3 6.3 -537 3
Potency against cAMP formation in CHO cells expressing recombinant human A2B receptorPotency against cAMP formation in CHO cells expressing recombinant human A2B receptor
ChEMBL 560 8 5 14 0.2 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(N[C@H](CO)Cc5ccc(Br)cc5)nc43)[C@H](O)[C@@H]2O)n1 10.1021/jm031143+
CHEMBL361925 123640 None 0 Human Functional pEC50 = 6.3 6.3 -537 3
Potency against cAMP formation in CHO cells expressing recombinant human A2B receptorPotency against cAMP formation in CHO cells expressing recombinant human A2B receptor
ChEMBL 560 8 5 14 0.2 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(N[C@H](CO)Cc5ccc(Br)cc5)nc43)[C@H](O)[C@@H]2O)n1 10.1021/jm031143+
137638080 156835 None 0 Human Functional pEC50 = 6.2 6.2 -269 4
Agonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assayAgonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assay
ChEMBL 457 6 3 12 1.1 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5cccc(Cl)c5)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
CHEMBL4071338 156835 None 0 Human Functional pEC50 = 6.2 6.2 -269 4
Agonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assayAgonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assay
ChEMBL 457 6 3 12 1.1 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5cccc(Cl)c5)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
168293564 192157 None 0 Human Functional pEC50 = 8.2 8.2 45 4
Agonist activity at human A2B receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 10 mins in presence of forskolin by LANCE cAMP assayAgonist activity at human A2B receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 10 mins in presence of forskolin by LANCE cAMP assay
ChEMBL 849 13 6 13 6.8 Nc1sc(-c2ccc(C(=O)NCCCc3ccc(Nc4ncnc5c4ncn5[C@@H]4O[C@H](CO)[C@@H](O)[C@H]4O)cc3)cc2)c(-c2cccc(C(F)(F)F)c2)c1C(=O)c1ccccc1 10.1021/acs.jmedchem.2c00320
CHEMBL5203917 192157 None 0 Human Functional pEC50 = 8.2 8.2 45 4
Agonist activity at human A2B receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 10 mins in presence of forskolin by LANCE cAMP assayAgonist activity at human A2B receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 10 mins in presence of forskolin by LANCE cAMP assay
ChEMBL 849 13 6 13 6.8 Nc1sc(-c2ccc(C(=O)NCCCc3ccc(Nc4ncnc5c4ncn5[C@@H]4O[C@H](CO)[C@@H](O)[C@H]4O)cc3)cc2)c(-c2cccc(C(F)(F)F)c2)c1C(=O)c1ccccc1 10.1021/acs.jmedchem.2c00320
137653409 159037 None 0 Human Functional pEC50 = 7.2 7.2 -1 4
Agonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 567 12 6 12 2.2 Nc1ccc(-c2cccc(C(=O)NCCCCCCNc3ncnc4c3ncn4[C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)c2)s1 10.1021/acs.jmedchem.8b00047
CHEMBL4096796 159037 None 0 Human Functional pEC50 = 7.2 7.2 -1 4
Agonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 567 12 6 12 2.2 Nc1ccc(-c2cccc(C(=O)NCCCCCCNc3ncnc4c3ncn4[C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)c2)s1 10.1021/acs.jmedchem.8b00047
168288912 191628 None 0 Human Functional pEC50 = 6.2 6.2 -4897 4
Agonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 502 7 4 10 1.6 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4Oc4ccccc4Cl)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
CHEMBL5195714 191628 None 0 Human Functional pEC50 = 6.2 6.2 -4897 4
Agonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 502 7 4 10 1.6 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4Oc4ccccc4Cl)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
16103169 82670 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP levelsActivity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP levels
ChEMBL 481 7 5 11 -0.0 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NNC(=O)Cc4cccs4)nc(Cl)nc32)[C@H](O)[C@@H]1O 10.1021/jm061170a
CHEMBL217952 82670 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP levelsActivity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP levels
ChEMBL 481 7 5 11 -0.0 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NNC(=O)Cc4cccs4)nc(Cl)nc32)[C@H](O)[C@@H]1O 10.1021/jm061170a
57384288 75480 None 0 Human Functional pEC50 = 5.2 5.2 -426 4
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 674 9 7 12 3.4 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(NCCc4ccc(NC(=O)c5cc(C(C)(C)C)c(O)c(C(C)(C)C)c5)cc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm300206u
CHEMBL2042302 75480 None 0 Human Functional pEC50 = 5.2 5.2 -426 4
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 674 9 7 12 3.4 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(NCCc4ccc(NC(=O)c5cc(C(C)(C)C)c(O)c(C(C)(C)C)c5)cc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm300206u
118719026 115435 None 0 Human Functional pEC50 = 5.2 5.2 - 1
Agonist activity at human recombinant adenosine receptor A2b by cAMP assayAgonist activity at human recombinant adenosine receptor A2b by cAMP assay
ChEMBL 582 13 4 8 2.1 CC(C)(C)OC(=O)C1CCCN1C[C@@H](O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(N)=O)NC(=O)OCc1ccccc1 10.1021/jm4011669
CHEMBL3350613 115435 None 0 Human Functional pEC50 = 5.2 5.2 - 1
Agonist activity at human recombinant adenosine receptor A2b by cAMP assayAgonist activity at human recombinant adenosine receptor A2b by cAMP assay
ChEMBL 582 13 4 8 2.1 CC(C)(C)OC(=O)C1CCCN1C[C@@H](O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(N)=O)NC(=O)OCc1ccccc1 10.1021/jm4011669
137650461 157256 None 0 Human Functional pEC50 = 6.2 6.2 -1 4
Agonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 857 16 6 13 6.4 CC(=O)Nc1sc(-c2ccc(C(=O)NCCCCCCNc3ncnc4c3ncn4[C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)cc2)c(-c2cccc(C(F)(F)F)c2)c1C(=O)c1ccccc1 10.1021/acs.jmedchem.8b00047
CHEMBL4076565 157256 None 0 Human Functional pEC50 = 6.2 6.2 -1 4
Agonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 857 16 6 13 6.4 CC(=O)Nc1sc(-c2ccc(C(=O)NCCCCCCNc3ncnc4c3ncn4[C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)cc2)c(-c2cccc(C(F)(F)F)c2)c1C(=O)c1ccccc1 10.1021/acs.jmedchem.8b00047
137634444 156163 None 0 Human Functional pEC50 = 7.2 7.2 1 3
Agonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 801 14 6 13 5.7 Nc1sc(-c2ccc(C(=O)NCCCCCNc3ncnc4c3ncn4[C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)cc2)c(-c2cccc(C(F)(F)F)c2)c1C(=O)c1ccccc1 10.1021/acs.jmedchem.8b00047
CHEMBL4063841 156163 None 0 Human Functional pEC50 = 7.2 7.2 1 3
Agonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 801 14 6 13 5.7 Nc1sc(-c2ccc(C(=O)NCCCCCNc3ncnc4c3ncn4[C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)cc2)c(-c2cccc(C(F)(F)F)c2)c1C(=O)c1ccccc1 10.1021/acs.jmedchem.8b00047
377 2758 None 53 Human Functional pEC50 = 7.2 7.2 -48 10
Agonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.2c01414
425 2758 None 53 Human Functional pEC50 = 7.2 7.2 -48 10
Agonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.2c01414
448222 2758 None 53 Human Functional pEC50 = 7.2 7.2 -48 10
Agonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.2c01414
CHEMBL464859 2758 None 53 Human Functional pEC50 = 7.2 7.2 -48 10
Agonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.2c01414
137642036 158152 None 0 Human Functional pEC50 = 6.2 6.2 -177 4
Agonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assayAgonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assay
ChEMBL 387 6 3 12 -0.4 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCC5CC5)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
CHEMBL4087306 158152 None 0 Human Functional pEC50 = 6.2 6.2 -177 4
Agonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assayAgonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assay
ChEMBL 387 6 3 12 -0.4 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCC5CC5)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
57387822 75490 None 0 Human Functional pEC50 = 5.2 5.2 -3 3
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 840 13 7 12 6.6 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(NCCc4ccc(NC(=O)c5cc(C(C)(C)C)c(O)c(C(C)(C)C)c5)cc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm300206u
CHEMBL2042312 75490 None 0 Human Functional pEC50 = 5.2 5.2 -3 3
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 840 13 7 12 6.6 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC(c4ccccc4)c4ccccc4)nc(NCCc4ccc(NC(=O)c5cc(C(C)(C)C)c(O)c(C(C)(C)C)c5)cc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm300206u
118732974 118515 None 0 Human Functional pEC50 = 6.2 6.2 -47 4
Agonist activity at human recombinant adenosine A2B receptor transfected in CHO cells assessed as induction of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2B receptor transfected in CHO cells assessed as induction of adenylyl cyclase activity
ChEMBL 373 5 3 12 -0.6 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NC5CC5)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.5b00074
CHEMBL3414940 118515 None 0 Human Functional pEC50 = 6.2 6.2 -47 4
Agonist activity at human recombinant adenosine A2B receptor transfected in CHO cells assessed as induction of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2B receptor transfected in CHO cells assessed as induction of adenylyl cyclase activity
ChEMBL 373 5 3 12 -0.6 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NC5CC5)ncnc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.5b00074
118732975 118516 None 0 Human Functional pEC50 = 6.2 6.2 -173 4
Agonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assayAgonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assay
ChEMBL 407 5 3 12 0.1 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NC5CC5)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
CHEMBL3414941 118516 None 0 Human Functional pEC50 = 6.2 6.2 -173 4
Agonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assayAgonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assay
ChEMBL 407 5 3 12 0.1 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NC5CC5)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.7b00291
10436433 131373 None 0 Human Functional pEC50 = 6.2 6.2 -478 2
Potency against cAMP formation in CHO cells expressing recombinant human A2B receptorPotency against cAMP formation in CHO cells expressing recombinant human A2B receptor
ChEMBL 512 9 5 15 -0.6 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(N[C@H](CO)Cc5ccc(OC)cc5)nc43)[C@H](O)[C@@H]2O)n1 10.1021/jm031143+
CHEMBL368880 131373 None 0 Human Functional pEC50 = 6.2 6.2 -478 2
Potency against cAMP formation in CHO cells expressing recombinant human A2B receptorPotency against cAMP formation in CHO cells expressing recombinant human A2B receptor
ChEMBL 512 9 5 15 -0.6 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(N[C@H](CO)Cc5ccc(OC)cc5)nc43)[C@H](O)[C@@H]2O)n1 10.1021/jm031143+
44423811 85371 None 0 Human Functional pEC50 = 8.1 8.1 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 533 9 5 11 1.3 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(Nc4ccc(OCC(=O)Nc5ccccc5)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1016/j.bmc.2007.01.055
CHEMBL226193 85371 None 0 Human Functional pEC50 = 8.1 8.1 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 533 9 5 11 1.3 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(Nc4ccc(OCC(=O)Nc5ccccc5)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1016/j.bmc.2007.01.055
162645916 179496 None 0 Human Functional pEC50 = 6.2 6.2 -9 4
Irreversible agonist activity at human adenosine A2B receptor expressed in Flp-In-CHO cells assessed as effect on forskolin-induced cAMP accumulation incubated for 30 mins by LANCE cAMP detection assayIrreversible agonist activity at human adenosine A2B receptor expressed in Flp-In-CHO cells assessed as effect on forskolin-induced cAMP accumulation incubated for 30 mins by LANCE cAMP detection assay
ChEMBL 414 6 4 11 0.8 OC[C@H]1O[C@@H](n2cnc3c(Nc4ccc(CN=C=S)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.6b01561
CHEMBL4741079 179496 None 0 Human Functional pEC50 = 6.2 6.2 -9 4
Irreversible agonist activity at human adenosine A2B receptor expressed in Flp-In-CHO cells assessed as effect on forskolin-induced cAMP accumulation incubated for 30 mins by LANCE cAMP detection assayIrreversible agonist activity at human adenosine A2B receptor expressed in Flp-In-CHO cells assessed as effect on forskolin-induced cAMP accumulation incubated for 30 mins by LANCE cAMP detection assay
ChEMBL 414 6 4 11 0.8 OC[C@H]1O[C@@H](n2cnc3c(Nc4ccc(CN=C=S)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.6b01561
118734347 118611 None 0 Human Functional pEC50 = 5.2 5.2 -45 2
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting methodAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting method
ChEMBL 637 8 5 12 0.0 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(NCCN4CCN(c5ccc(I)cc5)CC4)nc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.5b00215
CHEMBL3416782 118611 None 0 Human Functional pEC50 = 5.2 5.2 -45 2
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting methodAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting method
ChEMBL 637 8 5 12 0.0 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(NCCN4CCN(c5ccc(I)cc5)CC4)nc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.5b00215
57384289 75481 None 0 Human Functional pEC50 = 6.1 6.1 -112 4
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 630 13 6 13 2.5 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(NCCc4ccc(NC(=O)CCCC[C@H]5CCSS5)cc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm300206u
CHEMBL2042303 75481 None 0 Human Functional pEC50 = 6.1 6.1 -112 4
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 minsAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins
ChEMBL 630 13 6 13 2.5 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(NCCc4ccc(NC(=O)CCCC[C@H]5CCSS5)cc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm300206u
137646828 158006 None 0 Human Functional pEC50 = 7.1 7.1 -1 4
Agonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 856 16 6 13 6.2 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCCCCCCNC(=O)c4ccc(-c5sc(N)c(C(=O)c6ccccc6)c5-c5cccc(C(F)(F)F)c5)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.8b00047
CHEMBL4085418 158006 None 0 Human Functional pEC50 = 7.1 7.1 -1 4
Agonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 856 16 6 13 6.2 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCCCCCCNC(=O)c4ccc(-c5sc(N)c(C(=O)c6ccccc6)c5-c5cccc(C(F)(F)F)c5)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.8b00047
16203539 136349 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 444 6 5 10 0.3 Nc1nc(OCCc2c[nH]c3ccc(F)cc23)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm061278q
CHEMBL373478 136349 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 444 6 5 10 0.3 Nc1nc(OCCc2c[nH]c3ccc(F)cc23)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm061278q
76329265 106060 None 0 Human Functional pEC50 = 6.1 6.1 -50 4
Agonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 377 4 5 10 -0.9 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NC4CCCC4)nc(N)nc32)[C@H](O)[C@@H]1O 10.1039/C3MD00364G
CHEMBL3133158 106060 None 0 Human Functional pEC50 = 6.1 6.1 -50 4
Agonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assayAgonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay
ChEMBL 377 4 5 10 -0.9 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NC4CCCC4)nc(N)nc32)[C@H](O)[C@@H]1O 10.1039/C3MD00364G
168283120 191061 None 0 Human Functional pEC50 = 5.1 5.1 -60255 4
Agonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 498 8 4 11 1.0 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4Oc4cccc(OC)c4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
CHEMBL5187330 191061 None 0 Human Functional pEC50 = 5.1 5.1 -60255 4
Agonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 498 8 4 11 1.0 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4Oc4cccc(OC)c4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
168287894 191351 None 0 Human Functional pEC50 = 5.1 5.1 -776 4
Agonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 502 7 4 10 1.6 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4Oc4ccc(Cl)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
CHEMBL5191989 191351 None 0 Human Functional pEC50 = 5.1 5.1 -776 4
Agonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 502 7 4 10 1.6 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4Oc4ccc(Cl)cc4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
71657835 159737 None 3 Human Functional pEC50 = 4.1 4.1 -1 4
Agonist activity at A2BR in human NHVCF cells assessed as cAMP accumulation incubated for 30 mins in presence of PSB603 by LANCE cAMP assayAgonist activity at A2BR in human NHVCF cells assessed as cAMP accumulation incubated for 30 mins in presence of PSB603 by LANCE cAMP assay
ChEMBL 815 15 6 13 6.1 Nc1sc(-c2ccc(C(=O)NCCCCCCNc3ncnc4c3ncn4[C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)cc2)c(-c2cccc(C(F)(F)F)c2)c1C(=O)c1ccccc1 10.1021/acs.jmedchem.2c00320
CHEMBL4104819 159737 None 3 Human Functional pEC50 = 4.1 4.1 -1 4
Agonist activity at A2BR in human NHVCF cells assessed as cAMP accumulation incubated for 30 mins in presence of PSB603 by LANCE cAMP assayAgonist activity at A2BR in human NHVCF cells assessed as cAMP accumulation incubated for 30 mins in presence of PSB603 by LANCE cAMP assay
ChEMBL 815 15 6 13 6.1 Nc1sc(-c2ccc(C(=O)NCCCCCCNc3ncnc4c3ncn4[C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)cc2)c(-c2cccc(C(F)(F)F)c2)c1C(=O)c1ccccc1 10.1021/acs.jmedchem.2c00320
16103176 83223 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP levelsActivity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP levels
ChEMBL 417 6 5 11 -1.1 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NNC(=O)c4ccco4)ncnc32)[C@H](O)[C@@H]1O 10.1021/jm061170a
CHEMBL218596 83223 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP levelsActivity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP levels
ChEMBL 417 6 5 11 -1.1 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NNC(=O)c4ccco4)ncnc32)[C@H](O)[C@@H]1O 10.1021/jm061170a
118732982 118523 None 0 Human Functional pEC50 = 6.1 6.1 -91 4
Agonist activity at human recombinant adenosine A2B receptor transfected in CHO cells assessed as induction of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2B receptor transfected in CHO cells assessed as induction of adenylyl cyclase activity
ChEMBL 583 6 3 12 1.7 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5ccccc5I)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.5b00074
CHEMBL3414948 118523 None 0 Human Functional pEC50 = 6.1 6.1 -91 4
Agonist activity at human recombinant adenosine A2B receptor transfected in CHO cells assessed as induction of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2B receptor transfected in CHO cells assessed as induction of adenylyl cyclase activity
ChEMBL 583 6 3 12 1.7 CCn1nnc([C@H]2O[C@@H](n3cnc4c(NCc5ccccc5I)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1021/acs.jmedchem.5b00074
145976032 163587 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assayAgonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assay
ChEMBL 402 7 2 7 3.9 N#Cc1c(N)nc(SCc2ccn[nH]2)c(C#N)c1-c1ccc(OCC2CC2)cc1 10.1016/j.ejmech.2018.02.081
CHEMBL4203420 163587 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assayAgonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assay
ChEMBL 402 7 2 7 3.9 N#Cc1c(N)nc(SCc2ccn[nH]2)c(C#N)c1-c1ccc(OCC2CC2)cc1 10.1016/j.ejmech.2018.02.081
155535452 172090 None 0 Human Functional pEC50 = 6.1 6.1 -14 2
Agonist activity at human A2B expressed in CHO cells assessed as stimulation of cAMP production by alphascreen assayAgonist activity at human A2B expressed in CHO cells assessed as stimulation of cAMP production by alphascreen assay
ChEMBL 286 4 2 7 1.8 N#Cc1c(N)nc(SCCO)c(C#N)c1-c1ccoc1 10.1021/acs.jmedchem.9b00106
CHEMBL4472401 172090 None 0 Human Functional pEC50 = 6.1 6.1 -14 2
Agonist activity at human A2B expressed in CHO cells assessed as stimulation of cAMP production by alphascreen assayAgonist activity at human A2B expressed in CHO cells assessed as stimulation of cAMP production by alphascreen assay
ChEMBL 286 4 2 7 1.8 N#Cc1c(N)nc(SCCO)c(C#N)c1-c1ccoc1 10.1021/acs.jmedchem.9b00106
118734374 118635 None 0 Human Functional pEC50 = 6.1 6.1 -22 2
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting methodAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting method
ChEMBL 642 8 4 12 2.1 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(N4CCN(c5ccc(OCc6ccc(C(F)(F)F)cc6)cc5)CC4)nc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.5b00215
CHEMBL3416808 118635 None 0 Human Functional pEC50 = 6.1 6.1 -22 2
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting methodAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting method
ChEMBL 642 8 4 12 2.1 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(N4CCN(c5ccc(OCc6ccc(C(F)(F)F)cc6)cc5)CC4)nc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.5b00215
69961639 175732 None 0 Human Functional pEC50 = 6.1 6.1 -8 2
Agonist activity at human A2B expressed in CHO cells assessed as stimulation of cAMP production by alphascreen assayAgonist activity at human A2B expressed in CHO cells assessed as stimulation of cAMP production by alphascreen assay
ChEMBL 302 4 2 7 2.2 N#Cc1c(N)nc(SCCO)c(C#N)c1-c1cccs1 10.1021/acs.jmedchem.9b00106
CHEMBL4582726 175732 None 0 Human Functional pEC50 = 6.1 6.1 -8 2
Agonist activity at human A2B expressed in CHO cells assessed as stimulation of cAMP production by alphascreen assayAgonist activity at human A2B expressed in CHO cells assessed as stimulation of cAMP production by alphascreen assay
ChEMBL 302 4 2 7 2.2 N#Cc1c(N)nc(SCCO)c(C#N)c1-c1cccs1 10.1021/acs.jmedchem.9b00106
46865897 7797 None 0 Human Functional pEC50 = 5.1 5.1 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 413 5 2 8 4.2 O=C(Nc1ccccc1)Nc1nc(Oc2ccccc2)nc2nc(-c3ccco3)nn12 10.1016/j.bmc.2010.02.039
CHEMBL1089440 7797 None 0 Human Functional pEC50 = 5.1 5.1 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 413 5 2 8 4.2 O=C(Nc1ccccc1)Nc1nc(Oc2ccccc2)nc2nc(-c3ccco3)nn12 10.1016/j.bmc.2010.02.039
16202841 84676 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 442 6 6 11 -0.2 Nc1nc(OCCc2c[nH]c3ccc(O)cc23)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm061278q
CHEMBL222500 84676 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 442 6 6 11 -0.2 Nc1nc(OCCc2c[nH]c3ccc(O)cc23)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm061278q
11164346 16136 None 0 Human Functional pEC50 = 8.1 8.1 - 1
Agonistic activity against human adenosine A2B receptor expressed in CHO cellsAgonistic activity against human adenosine A2B receptor expressed in CHO cells
ChEMBL 362 5 2 7 3.1 COc1ccc(-c2c(C#N)c(N)nc(SCc3ncc[nH]3)c2C#N)cc1 10.1021/jm049947s
CHEMBL122396 16136 None 0 Human Functional pEC50 = 8.1 8.1 - 1
Agonistic activity against human adenosine A2B receptor expressed in CHO cellsAgonistic activity against human adenosine A2B receptor expressed in CHO cells
ChEMBL 362 5 2 7 3.1 COc1ccc(-c2c(C#N)c(N)nc(SCc3ncc[nH]3)c2C#N)cc1 10.1021/jm049947s
145973077 164677 None 0 Human Functional pEC50 = 8.0 8.0 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assayAgonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assay
ChEMBL 402 7 2 7 3.9 N#Cc1c(N)nc(SCc2ncc[nH]2)c(C#N)c1-c1ccc(OCC2CC2)cc1 10.1016/j.ejmech.2018.02.081
CHEMBL4216880 164677 None 0 Human Functional pEC50 = 8.0 8.0 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assayAgonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assay
ChEMBL 402 7 2 7 3.9 N#Cc1c(N)nc(SCc2ncc[nH]2)c(C#N)c1-c1ccc(OCC2CC2)cc1 10.1016/j.ejmech.2018.02.081
137641858 158307 None 0 Human Functional pEC50 = 7.0 7.0 1 4
Agonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 696 13 5 11 5.3 O=C(NCCCCCCNc1ncnc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O)c1ccc(-c2sccc2-c2cccc(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.8b00047
CHEMBL4089092 158307 None 0 Human Functional pEC50 = 7.0 7.0 1 4
Agonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 696 13 5 11 5.3 O=C(NCCCCCCNc1ncnc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O)c1ccc(-c2sccc2-c2cccc(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.8b00047
168269866 189988 None 0 Human Functional pEC50 = 6.0 6.0 -3090 4
Agonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 468 7 4 10 1.0 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4Oc4ccccc4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
CHEMBL5171042 189988 None 0 Human Functional pEC50 = 6.0 6.0 -3090 4
Agonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 468 7 4 10 1.0 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4Oc4ccccc4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
118734372 118633 None 0 Human Functional pEC50 = 6.0 6.0 -17 2
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting methodAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting method
ChEMBL 608 8 4 12 1.7 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(N4CCN(c5ccc(OCc6ccc(Cl)cc6)cc5)CC4)nc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.5b00215
CHEMBL3416806 118633 None 0 Human Functional pEC50 = 6.0 6.0 -17 2
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting methodAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting method
ChEMBL 608 8 4 12 1.7 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(N4CCN(c5ccc(OCc6ccc(Cl)cc6)cc5)CC4)nc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.5b00215
118734345 118609 None 0 Human Functional pEC50 = 5.0 5.0 -301 2
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting methodAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting method
ChEMBL 545 8 5 12 0.1 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(NCCN4CCN(c5ccc(Cl)cc5)CC4)nc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.5b00215
CHEMBL3416780 118609 None 0 Human Functional pEC50 = 5.0 5.0 -301 2
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting methodAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting method
ChEMBL 545 8 5 12 0.1 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(NCCN4CCN(c5ccc(Cl)cc5)CC4)nc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.5b00215
118734346 118610 None 0 Human Functional pEC50 = 5.0 5.0 -218 2
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting methodAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting method
ChEMBL 589 8 5 12 0.2 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(NCCN4CCN(c5ccc(Br)cc5)CC4)nc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.5b00215
CHEMBL3416781 118610 None 0 Human Functional pEC50 = 5.0 5.0 -218 2
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting methodAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting method
ChEMBL 589 8 5 12 0.2 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(NCCN4CCN(c5ccc(Br)cc5)CC4)nc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.5b00215
89534951 164431 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assayAgonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assay
ChEMBL 393 7 2 7 2.7 CNC(=O)CSc1nc(N)c(C#N)c(-c2ccc(OCC3CC3)cc2)c1C#N 10.1016/j.ejmech.2018.02.081
CHEMBL4213681 164431 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assayAgonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as induction of cAMP accumulation by AlphaScreen assay
ChEMBL 393 7 2 7 2.7 CNC(=O)CSc1nc(N)c(C#N)c(-c2ccc(OCC3CC3)cc2)c1C#N 10.1016/j.ejmech.2018.02.081
377 2758 None 53 Human Functional pEC50 = 7.0 7.0 -48 10
Agonist activity at recombinant human A2BAR expressed in CHO cells assessed as stimulation of cAMP formation preincubated for 30 mins in presence of rolipram and adenosine deaminase followed by compound addition and measured after 20 mins by alphascreen cAMP assayAgonist activity at recombinant human A2BAR expressed in CHO cells assessed as stimulation of cAMP formation preincubated for 30 mins in presence of rolipram and adenosine deaminase followed by compound addition and measured after 20 mins by alphascreen cAMP assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acsmedchemlett.0c00509
425 2758 None 53 Human Functional pEC50 = 7.0 7.0 -48 10
Agonist activity at recombinant human A2BAR expressed in CHO cells assessed as stimulation of cAMP formation preincubated for 30 mins in presence of rolipram and adenosine deaminase followed by compound addition and measured after 20 mins by alphascreen cAMP assayAgonist activity at recombinant human A2BAR expressed in CHO cells assessed as stimulation of cAMP formation preincubated for 30 mins in presence of rolipram and adenosine deaminase followed by compound addition and measured after 20 mins by alphascreen cAMP assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acsmedchemlett.0c00509
448222 2758 None 53 Human Functional pEC50 = 7.0 7.0 -48 10
Agonist activity at recombinant human A2BAR expressed in CHO cells assessed as stimulation of cAMP formation preincubated for 30 mins in presence of rolipram and adenosine deaminase followed by compound addition and measured after 20 mins by alphascreen cAMP assayAgonist activity at recombinant human A2BAR expressed in CHO cells assessed as stimulation of cAMP formation preincubated for 30 mins in presence of rolipram and adenosine deaminase followed by compound addition and measured after 20 mins by alphascreen cAMP assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acsmedchemlett.0c00509
CHEMBL464859 2758 None 53 Human Functional pEC50 = 7.0 7.0 -48 10
Agonist activity at recombinant human A2BAR expressed in CHO cells assessed as stimulation of cAMP formation preincubated for 30 mins in presence of rolipram and adenosine deaminase followed by compound addition and measured after 20 mins by alphascreen cAMP assayAgonist activity at recombinant human A2BAR expressed in CHO cells assessed as stimulation of cAMP formation preincubated for 30 mins in presence of rolipram and adenosine deaminase followed by compound addition and measured after 20 mins by alphascreen cAMP assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acsmedchemlett.0c00509
168272212 190431 None 0 Human Functional pEC50 = 7.0 7.0 -2 4
Agonist activity at human A2B receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 10 mins in presence of forskolin by LANCE cAMP assayAgonist activity at human A2B receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 10 mins in presence of forskolin by LANCE cAMP assay
ChEMBL 518 10 5 10 1.9 O=C(NCCCCc1ccc(Nc2ncnc3c2ncn3[C@@H]2O[C@H](CO)[C@@H](O)[C@H]2O)cc1)c1ccccc1 10.1021/acs.jmedchem.2c00320
CHEMBL5178142 190431 None 0 Human Functional pEC50 = 7.0 7.0 -2 4
Agonist activity at human A2B receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 10 mins in presence of forskolin by LANCE cAMP assayAgonist activity at human A2B receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 10 mins in presence of forskolin by LANCE cAMP assay
ChEMBL 518 10 5 10 1.9 O=C(NCCCCc1ccc(Nc2ncnc3c2ncn3[C@@H]2O[C@H](CO)[C@@H](O)[C@H]2O)cc1)c1ccccc1 10.1021/acs.jmedchem.2c00320
71657835 159737 None 3 Human Functional pEC50 = 7.0 7.0 -1 4
Agonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 815 15 6 13 6.1 Nc1sc(-c2ccc(C(=O)NCCCCCCNc3ncnc4c3ncn4[C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)cc2)c(-c2cccc(C(F)(F)F)c2)c1C(=O)c1ccccc1 10.1021/acs.jmedchem.8b00047
CHEMBL4104819 159737 None 3 Human Functional pEC50 = 7.0 7.0 -1 4
Agonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 815 15 6 13 6.1 Nc1sc(-c2ccc(C(=O)NCCCCCCNc3ncnc4c3ncn4[C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)cc2)c(-c2cccc(C(F)(F)F)c2)c1C(=O)c1ccccc1 10.1021/acs.jmedchem.8b00047
9869857 66830 None 11 Human Functional pEC50 = 6.0 6.0 -213 5
Relative efficacy against phenylephrine precontracted tissue relaxation in Guinea pig aortaRelative efficacy against phenylephrine precontracted tissue relaxation in Guinea pig aorta
ChEMBL 482 8 5 14 -0.6 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(N[C@H](CO)Cc5ccccc5)nc43)[C@H](O)[C@@H]2O)n1 10.1021/jm031143+
CHEMBL186113 66830 None 11 Human Functional pEC50 = 6.0 6.0 -213 5
Relative efficacy against phenylephrine precontracted tissue relaxation in Guinea pig aortaRelative efficacy against phenylephrine precontracted tissue relaxation in Guinea pig aorta
ChEMBL 482 8 5 14 -0.6 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(N[C@H](CO)Cc5ccccc5)nc43)[C@H](O)[C@@H]2O)n1 10.1021/jm031143+
24827290 156355 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of adenylate cyclaseAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of adenylate cyclase
ChEMBL 707 11 5 12 3.0 O=C(COc1ccc(Nc2nc(OCCc3c[nH]c4cc(Br)ccc34)nc3c2ncn3[C@@H]2O[C@H](CO)[C@@H](O)[C@H]2O)cc1)N1CCCC1 10.1021/jm701442d
CHEMBL406594 156355 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of adenylate cyclaseAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of adenylate cyclase
ChEMBL 707 11 5 12 3.0 O=C(COc1ccc(Nc2nc(OCCc3c[nH]c4cc(Br)ccc34)nc3c2ncn3[C@@H]2O[C@H](CO)[C@@H](O)[C@H]2O)cc1)N1CCCC1 10.1021/jm701442d
137634052 156645 None 0 Human Functional pEC50 = 7.0 7.0 6 3
Agonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 830 15 7 14 5.7 Nc1nc(NCCCCCCNC(=O)c2ccc(-c3sc(N)c(C(=O)c4ccccc4)c3-c3cccc(C(F)(F)F)c3)cc2)c2ncn([C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)c2n1 10.1021/acs.jmedchem.8b00047
CHEMBL4069296 156645 None 0 Human Functional pEC50 = 7.0 7.0 6 3
Agonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assayAgonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assay
ChEMBL 830 15 7 14 5.7 Nc1nc(NCCCCCCNC(=O)c2ccc(-c3sc(N)c(C(=O)c4ccccc4)c3-c3cccc(C(F)(F)F)c3)cc2)c2ncn([C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)c2n1 10.1021/acs.jmedchem.8b00047
168276883 190200 None 0 Human Functional pEC50 = 6.0 6.0 -1862 4
Agonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 502 7 4 10 1.6 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4Oc4cccc(Cl)c4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
CHEMBL5174429 190200 None 0 Human Functional pEC50 = 6.0 6.0 -1862 4
Agonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assayAgonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay
ChEMBL 502 7 4 10 1.6 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCC[C@H]4Oc4cccc(Cl)c4)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.2c01414
155541051 172966 None 0 Human Functional pEC50 = 6.0 6.0 -251 2
Agonist activity at human A2B expressed in CHO cells assessed as stimulation of cAMP production by alphascreen assayAgonist activity at human A2B expressed in CHO cells assessed as stimulation of cAMP production by alphascreen assay
ChEMBL 406 5 1 8 4.2 COC(=O)c1cccc(CSc2nc(N)c(C#N)c(-c3cccs3)c2C#N)c1 10.1021/acs.jmedchem.9b00106
CHEMBL4517597 172966 None 0 Human Functional pEC50 = 6.0 6.0 -251 2
Agonist activity at human A2B expressed in CHO cells assessed as stimulation of cAMP production by alphascreen assayAgonist activity at human A2B expressed in CHO cells assessed as stimulation of cAMP production by alphascreen assay
ChEMBL 406 5 1 8 4.2 COC(=O)c1cccc(CSc2nc(N)c(C#N)c(-c3cccs3)c2C#N)c1 10.1021/acs.jmedchem.9b00106
16203669 85005 None 0 Human Functional pEC50 = 6 6.0 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 467 7 5 10 0.3 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(OCCc4c[nH]c5ccccc45)nc32)[C@H](O)[C@@H]1O 10.1021/jm061278q
CHEMBL223845 85005 None 0 Human Functional pEC50 = 6 6.0 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP productionAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production
ChEMBL 467 7 5 10 0.3 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(OCCc4c[nH]c5ccccc45)nc32)[C@H](O)[C@@H]1O 10.1021/jm061278q
156018418 177793 None 0 Human Functional pIC50 = 9.5 9.5 - 1
Inverse agonist activity at human A2B receptor expressed in CHO cells assessed as reduction in cAMP levelInverse agonist activity at human A2B receptor expressed in CHO cells assessed as reduction in cAMP level
ChEMBL 500 7 3 11 1.8 Nc1nc(NCCN2CCN(c3ccc(S(N)(=O)=O)cc3)CC2)nc2sc(-c3ccco3)nc12 10.1016/j.bmcl.2020.127067
CHEMBL4643397 177793 None 0 Human Functional pIC50 = 9.5 9.5 - 1
Inverse agonist activity at human A2B receptor expressed in CHO cells assessed as reduction in cAMP levelInverse agonist activity at human A2B receptor expressed in CHO cells assessed as reduction in cAMP level
ChEMBL 500 7 3 11 1.8 Nc1nc(NCCN2CCN(c3ccc(S(N)(=O)=O)cc3)CC2)nc2sc(-c3ccco3)nc12 10.1016/j.bmcl.2020.127067
3284 3216 None 35 Human Functional pIC50 = 9.0 9.0 - 1
Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2
ChEMBL 528 6 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)c1ccc(cc1)Cl 10.1021/jm900413e
44185871 3216 None 35 Human Functional pIC50 = 9.0 9.0 - 1
Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2
ChEMBL 528 6 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)c1ccc(cc1)Cl 10.1021/jm900413e
5728 3216 None 35 Human Functional pIC50 = 9.0 9.0 - 1
Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2
ChEMBL 528 6 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)c1ccc(cc1)Cl 10.1021/jm900413e
CHEMBL483688 3216 None 35 Human Functional pIC50 = 9.0 9.0 - 1
Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2
ChEMBL 528 6 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)c1ccc(cc1)Cl 10.1021/jm900413e
12066874 204253 None 0 Human Functional pIC50 = 8.9 8.9 - 1
Antagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulationAntagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulation
ChEMBL 262 1 1 5 2.7 Oc1c(-c2ccccc2)nnc2nc3ccccc3n12 10.1021/jm201177b
CHEMBL7113 204253 None 0 Human Functional pIC50 = 8.9 8.9 - 1
Antagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulationAntagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulation
ChEMBL 262 1 1 5 2.7 Oc1c(-c2ccccc2)nnc2nc3ccccc3n12 10.1021/jm201177b
25207803 5685 None 0 Human Functional pIC50 = 8.9 8.9 10 4
Fluorometric Imaging Plate Reader (FLIPR) Asssay: The use of a Fluorometric Imaging Plate Reader (FLIPR) to measure calcium flux in Adenosine-receptor expressing cells is a well-established technique. In this assay calcium flux is triggered by receptor activation and measured through the fluorescence of an incorporated calcium-sensitive dye. The potencies shown were determined using expressed human adenosine A2B receptors in mammalian cell lines. Selectivity values were obtained by using mammalian cell lines expressing the human adenosine A1, A2A and A3 receptors.Fluorometric Imaging Plate Reader (FLIPR) Asssay: The use of a Fluorometric Imaging Plate Reader (FLIPR) to measure calcium flux in Adenosine-receptor expressing cells is a well-established technique. In this assay calcium flux is triggered by receptor activation and measured through the fluorescence of an incorporated calcium-sensitive dye. The potencies shown were determined using expressed human adenosine A2B receptors in mammalian cell lines. Selectivity values were obtained by using mammalian cell lines expressing the human adenosine A1, A2A and A3 receptors.
ChEMBL 381 6 2 8 4.0 CNc1cc2nc(NCc3cccnc3)nc(C(=O)c3cccs3)c2s1 nan
CHEMBL1077943 5685 None 0 Human Functional pIC50 = 8.9 8.9 10 4
Fluorometric Imaging Plate Reader (FLIPR) Asssay: The use of a Fluorometric Imaging Plate Reader (FLIPR) to measure calcium flux in Adenosine-receptor expressing cells is a well-established technique. In this assay calcium flux is triggered by receptor activation and measured through the fluorescence of an incorporated calcium-sensitive dye. The potencies shown were determined using expressed human adenosine A2B receptors in mammalian cell lines. Selectivity values were obtained by using mammalian cell lines expressing the human adenosine A1, A2A and A3 receptors.Fluorometric Imaging Plate Reader (FLIPR) Asssay: The use of a Fluorometric Imaging Plate Reader (FLIPR) to measure calcium flux in Adenosine-receptor expressing cells is a well-established technique. In this assay calcium flux is triggered by receptor activation and measured through the fluorescence of an incorporated calcium-sensitive dye. The potencies shown were determined using expressed human adenosine A2B receptors in mammalian cell lines. Selectivity values were obtained by using mammalian cell lines expressing the human adenosine A1, A2A and A3 receptors.
ChEMBL 381 6 2 8 4.0 CNc1cc2nc(NCc3cccnc3)nc(C(=O)c3cccs3)c2s1 nan
156821415 185473 None 0 Human Functional pIC50 = 8.8 8.8 5 2
Antagonist activity at human A2bR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assayAntagonist activity at human A2bR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assay
ChEMBL 398 4 1 8 3.0 Nc1nc(-c2ccccc2)c(-c2ccnnc2)c2nc(Cc3ncccc3F)nn12 10.1021/acsmedchemlett.1c00620
CHEMBL4862010 185473 None 0 Human Functional pIC50 = 8.8 8.8 5 2
Antagonist activity at human A2bR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assayAntagonist activity at human A2bR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assay
ChEMBL 398 4 1 8 3.0 Nc1nc(-c2ccccc2)c(-c2ccnnc2)c2nc(Cc3ncccc3F)nn12 10.1021/acsmedchemlett.1c00620
44186667 185659 None 0 Human Functional pIC50 = 8.8 8.8 - 1
Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2
ChEMBL 576 7 2 7 3.0 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc(C(F)(F)F)cc5)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
CHEMBL486479 185659 None 0 Human Functional pIC50 = 8.8 8.8 - 1
Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2
ChEMBL 576 7 2 7 3.0 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc(C(F)(F)F)cc5)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
44186622 184229 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2
ChEMBL 542 7 2 7 2.7 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5cccc(Cl)c5)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
CHEMBL483469 184229 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2
ChEMBL 542 7 2 7 2.7 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5cccc(Cl)c5)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
10641040 9765 None 0 Human Functional pIC50 = 8 8.0 - 1
Antagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulationAntagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulation
ChEMBL 342 3 0 6 3.4 O=c1c(-c2ccco2)nnc2n(Cc3ccccc3)c3ccccc3n12 10.1021/jm201177b
CHEMBL113518 9765 None 0 Human Functional pIC50 = 8 8.0 - 1
Antagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulationAntagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulation
ChEMBL 342 3 0 6 3.4 O=c1c(-c2ccco2)nnc2n(Cc3ccccc3)c3ccccc3n12 10.1021/jm201177b
11605883 79952 None 6 Human Functional pIC50 = 8 8.0 - 1
Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2
ChEMBL 508 7 2 7 2.0 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccccc5)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
CHEMBL212625 79952 None 6 Human Functional pIC50 = 8 8.0 - 1
Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2
ChEMBL 508 7 2 7 2.0 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccccc5)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
44185933 186709 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2
ChEMBL 522 8 2 7 2.0 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(CCc5ccccc5)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
CHEMBL488541 186709 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2
ChEMBL 522 8 2 7 2.0 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(CCc5ccccc5)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
135493268 110486 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptorInhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor
ChEMBL 449 8 2 8 2.3 CCCn1c(=O)c2nc(-c3cc(NC(=O)Cc4ccccc4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
CHEMBL32481 110486 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptorInhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor
ChEMBL 449 8 2 8 2.3 CCCn1c(=O)c2nc(-c3cc(NC(=O)Cc4ccccc4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
134142435 145338 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 341 4 2 7 3.7 Nc1nc(NCc2cccc(F)c2)nc2sc(-c3ccco3)nc12 10.1021/acs.jmedchem.6b01068
CHEMBL3913413 145338 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 341 4 2 7 3.7 Nc1nc(NCc2cccc(F)c2)nc2sc(-c3ccco3)nc12 10.1021/acs.jmedchem.6b01068
45481749 198534 None 0 Human Functional pIC50 = 5.0 5.0 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity
ChEMBL 437 5 1 8 4.1 CCn1cc2c(nc(NC(=O)Cc3ccc4ccccc4c3)n3nc(-c4ccco4)nc23)n1 10.1016/j.bmc.2009.05.038
CHEMBL578008 198534 None 0 Human Functional pIC50 = 5.0 5.0 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity
ChEMBL 437 5 1 8 4.1 CCn1cc2c(nc(NC(=O)Cc3ccc4ccccc4c3)n3nc(-c4ccco4)nc23)n1 10.1016/j.bmc.2009.05.038
60156108 76986 None 0 Human Functional pIC50 = 6.0 6.0 -69 2
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production
ChEMBL 532 5 3 9 2.9 Cn1cc2c(nc(NC(=O)NC3CCN(C(=O)NCc4ccc(F)cc4)CC3)n3nc(-c4ccco4)nc23)n1 10.1021/jm300323t
CHEMBL2071046 76986 None 0 Human Functional pIC50 = 6.0 6.0 -69 2
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production
ChEMBL 532 5 3 9 2.9 Cn1cc2c(nc(NC(=O)NC3CCN(C(=O)NCc4ccc(F)cc4)CC3)n3nc(-c4ccco4)nc23)n1 10.1021/jm300323t
135874429 95755 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP levelsAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP levels
ChEMBL 483 8 2 8 3.2 CCCn1c(=O)c2[nH]c(-c3cc(C)n(CC(=O)Nc4cccc(Cl)c4)n3)nc2n(CCC)c1=O 10.1016/j.bmc.2007.11.058
CHEMBL258473 95755 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP levelsAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP levels
ChEMBL 483 8 2 8 3.2 CCCn1c(=O)c2[nH]c(-c3cc(C)n(CC(=O)Nc4cccc(Cl)c4)n3)nc2n(CCC)c1=O 10.1016/j.bmc.2007.11.058
57429602 157239 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human adenosine A2B receptor expressed in mouse NIH/3T3 cells assessed as inhibition of NECA-induced IL-6 releaseAntagonist activity at human adenosine A2B receptor expressed in mouse NIH/3T3 cells assessed as inhibition of NECA-induced IL-6 release
ChEMBL 500 7 1 8 3.5 CCCn1c(=O)c2[nH]c(-c3cnn(CC#Cc4cccc(OC(F)(F)F)c4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2021.113907
CHEMBL4076435 157239 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human adenosine A2B receptor expressed in mouse NIH/3T3 cells assessed as inhibition of NECA-induced IL-6 releaseAntagonist activity at human adenosine A2B receptor expressed in mouse NIH/3T3 cells assessed as inhibition of NECA-induced IL-6 release
ChEMBL 500 7 1 8 3.5 CCCn1c(=O)c2[nH]c(-c3cnn(CC#Cc4cccc(OC(F)(F)F)c4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2021.113907
51039214 71523 None 0 Human Functional pIC50 = 5.0 5.0 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 342 5 3 9 1.5 NCC1CCC(CNc2nc(N)n3nc(-c4ccco4)nc3n2)CC1 10.1021/jm101349u
CHEMBL1927444 71523 None 0 Human Functional pIC50 = 5.0 5.0 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 342 5 3 9 1.5 NCC1CCC(CNc2nc(N)n3nc(-c4ccco4)nc3n2)CC1 10.1021/jm101349u
CHEMBL1962813 71523 None 0 Human Functional pIC50 = 5.0 5.0 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 342 5 3 9 1.5 NCC1CCC(CNc2nc(N)n3nc(-c4ccco4)nc3n2)CC1 10.1021/jm101349u
135522388 100112 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptorInhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor
ChEMBL 543 9 2 9 2.9 CCCn1c(=O)c2nc(-c3cc(OCC(=O)Nc4ccc(Br)cc4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
CHEMBL287529 100112 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptorInhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor
ChEMBL 543 9 2 9 2.9 CCCn1c(=O)c2nc(-c3cc(OCC(=O)Nc4ccc(Br)cc4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
46883206 6317 None 0 Human Functional pIC50 = 7.0 7.0 10 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 347 5 1 7 3.3 O=C(c1cccnc1)c1nc(NCc2cccnc2)nc2ccsc12 10.1016/j.bmcl.2009.08.040
CHEMBL1081873 6317 None 0 Human Functional pIC50 = 7.0 7.0 10 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 347 5 1 7 3.3 O=C(c1cccnc1)c1nc(NCc2cccnc2)nc2ccsc12 10.1016/j.bmcl.2009.08.040
145436767 162478 None 0 Human Functional pIC50 = 7.0 7.0 -4365 2
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 324 4 2 8 2.9 Nc1nc(NCc2cccnc2)nc2sc(-c3ccco3)nc12 10.1016/j.ejmech.2018.06.020
CHEMBL4167125 162478 None 0 Human Functional pIC50 = 7.0 7.0 -4365 2
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 324 4 2 8 2.9 Nc1nc(NCc2cccnc2)nc2sc(-c3ccco3)nc12 10.1016/j.ejmech.2018.06.020
136042340 71166 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 527 8 2 9 3.6 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5cc(Br)ccc5[nH]4)no3)nc2n(CCC)c1=O 10.1021/jm201292w
CHEMBL1955916 71166 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 527 8 2 9 3.6 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5cc(Br)ccc5[nH]4)no3)nc2n(CCC)c1=O 10.1021/jm201292w
10007115 116344 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Inhibitory activity against NECA stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptorInhibitory activity against NECA stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptor
ChEMBL 527 8 1 8 5.7 O=C(Cc1cccc2ccccc12)Nc1nc2nn(CCCc3ccccc3)cc2c2nc(-c3ccco3)nn12 10.1021/jm030852k
CHEMBL335950 116344 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Inhibitory activity against NECA stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptorInhibitory activity against NECA stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptor
ChEMBL 527 8 1 8 5.7 O=C(Cc1cccc2ccccc12)Nc1nc2nn(CCCc3ccccc3)cc2c2nc(-c3ccco3)nn12 10.1021/jm030852k
52947525 17659 None 0 Human Functional pIC50 = 6.0 6.0 -389 3
Antagonist activity at adenosine A2B receptor by cAMP assayAntagonist activity at adenosine A2B receptor by cAMP assay
ChEMBL 451 6 2 7 5.2 COc1ccc(Nc2c(-c3ccc4nccnc4c3)c(C)nn2-c2ccccc2)c(C(=O)O)c1 10.1016/j.bmcl.2010.07.095
CHEMBL1258397 17659 None 0 Human Functional pIC50 = 6.0 6.0 -389 3
Antagonist activity at adenosine A2B receptor by cAMP assayAntagonist activity at adenosine A2B receptor by cAMP assay
ChEMBL 451 6 2 7 5.2 COc1ccc(Nc2c(-c3ccc4nccnc4c3)c(C)nn2-c2ccccc2)c(C(=O)O)c1 10.1016/j.bmcl.2010.07.095
1922 202818 None 44 Rat Functional pIC50 = 6.0 6.0 -363 9
Inhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytesInhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytes
ChEMBL 256 1 1 5 0.6 Cn1c(=O)c2nc(-c3ccccc3)[nH]c2n(C)c1=O 10.1021/jm990499b
CHEMBL62350 202818 None 44 Rat Functional pIC50 = 6.0 6.0 -363 9
Inhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytesInhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytes
ChEMBL 256 1 1 5 0.6 Cn1c(=O)c2nc(-c3ccccc3)[nH]c2n(C)c1=O 10.1021/jm990499b
145960667 161482 None 0 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assayAntagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assay
ChEMBL 285 4 2 6 2.6 Cc1nc2c(N)nc(NCCc3ccccc3)nc2s1 10.1016/j.bmc.2018.05.048
CHEMBL4127811 161482 None 0 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assayAntagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assay
ChEMBL 285 4 2 6 2.6 Cc1nc2c(N)nc(NCCc3ccccc3)nc2s1 10.1016/j.bmc.2018.05.048
60156105 76984 None 0 Human Functional pIC50 = 6.0 6.0 -38 2
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production
ChEMBL 514 5 3 9 2.8 Cn1cc2c(nc(NC(=O)NC3CCN(C(=O)NCc4ccccc4)CC3)n3nc(-c4ccco4)nc23)n1 10.1021/jm300323t
CHEMBL2071044 76984 None 0 Human Functional pIC50 = 6.0 6.0 -38 2
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production
ChEMBL 514 5 3 9 2.8 Cn1cc2c(nc(NC(=O)NC3CCN(C(=O)NCc4ccccc4)CC3)n3nc(-c4ccco4)nc23)n1 10.1021/jm300323t
45481761 198005 None 0 Human Functional pIC50 = 5.0 5.0 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity
ChEMBL 539 8 1 8 5.8 O=C(Cc1ccc(-c2ccccc2)cc1)Nc1nc2nn(CCc3ccccc3)cc2c2nc(-c3ccco3)nn12 10.1016/j.bmc.2009.05.038
CHEMBL573771 198005 None 0 Human Functional pIC50 = 5.0 5.0 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity
ChEMBL 539 8 1 8 5.8 O=C(Cc1ccc(-c2ccccc2)cc1)Nc1nc2nn(CCc3ccccc3)cc2c2nc(-c3ccco3)nn12 10.1016/j.bmc.2009.05.038
51051249 69287 None 1 Human Functional pIC50 = 5.0 5.0 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 217 1 2 8 -0.1 Nc1nc(N)n2nc(-c3ccco3)nc2n1 10.1021/jm101349u
CHEMBL1927632 69287 None 1 Human Functional pIC50 = 5.0 5.0 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 217 1 2 8 -0.1 Nc1nc(N)n2nc(-c3ccco3)nc2n1 10.1021/jm101349u
127046494 139745 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated cAMP level preincubated for 10 mins followed by NECA stimulation by scintillation counting method in presence of [3H]-cyclic AMPAntagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated cAMP level preincubated for 10 mins followed by NECA stimulation by scintillation counting method in presence of [3H]-cyclic AMP
ChEMBL 307 3 2 7 2.4 Nc1nc(-c2ccco2)nc2cn(Cc3ccccc3O)nc12 10.1016/j.bmc.2016.04.048
CHEMBL3798383 139745 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated cAMP level preincubated for 10 mins followed by NECA stimulation by scintillation counting method in presence of [3H]-cyclic AMPAntagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated cAMP level preincubated for 10 mins followed by NECA stimulation by scintillation counting method in presence of [3H]-cyclic AMP
ChEMBL 307 3 2 7 2.4 Nc1nc(-c2ccco2)nc2cn(Cc3ccccc3O)nc12 10.1016/j.bmc.2016.04.048
145436765 162795 None 0 Human Functional pIC50 = 7.0 7.0 -2511 2
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 343 5 2 8 3.6 Nc1nc(NCCc2cccs2)nc2sc(-c3ccco3)nc12 10.1016/j.ejmech.2018.06.020
CHEMBL4172264 162795 None 0 Human Functional pIC50 = 7.0 7.0 -2511 2
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 343 5 2 8 3.6 Nc1nc(NCCc2cccs2)nc2sc(-c3ccco3)nc12 10.1016/j.ejmech.2018.06.020
136042342 71168 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 479 9 2 10 2.8 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5cc(OC)ccc5[nH]4)no3)nc2n(CCC)c1=O 10.1021/jm201292w
CHEMBL1955918 71168 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 479 9 2 10 2.8 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5cc(OC)ccc5[nH]4)no3)nc2n(CCC)c1=O 10.1021/jm201292w
135874414 96255 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP levelsAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP levels
ChEMBL 575 8 2 8 3.1 CCCn1c(=O)c2[nH]c(-c3cc(C)n(CC(=O)Nc4ccc(I)cc4)n3)nc2n(CCC)c1=O 10.1016/j.bmc.2007.11.058
CHEMBL261027 96255 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP levelsAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP levels
ChEMBL 575 8 2 8 3.1 CCCn1c(=O)c2[nH]c(-c3cc(C)n(CC(=O)Nc4ccc(I)cc4)n3)nc2n(CCC)c1=O 10.1016/j.bmc.2007.11.058
135443359 490 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptorInhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor
ChEMBL 509 9 3 11 -0.1 CCCn1c2=N/C(=c\3/cc([nH]n3C)OCC(=O)Nc3ccc(cc3)C(=O)O)/N=c2c(=O)n(c1=O)CCC 10.1021/jm0309654
441 490 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptorInhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor
ChEMBL 509 9 3 11 -0.1 CCCn1c2=N/C(=c\3/cc([nH]n3C)OCC(=O)Nc3ccc(cc3)C(=O)O)/N=c2c(=O)n(c1=O)CCC 10.1021/jm0309654
CHEMBL431703 490 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptorInhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor
ChEMBL 509 9 3 11 -0.1 CCCn1c2=N/C(=c\3/cc([nH]n3C)OCC(=O)Nc3ccc(cc3)C(=O)O)/N=c2c(=O)n(c1=O)CCC 10.1021/jm0309654
127036844 137558 None 0 Human Functional pIC50 = 4.9 4.9 - 1
Antagonist activity at human A2B adenosine receptor expressed in CHO cell membranes assessed as inhibition of NECA stimulated adenylyl cyclase activityAntagonist activity at human A2B adenosine receptor expressed in CHO cell membranes assessed as inhibition of NECA stimulated adenylyl cyclase activity
ChEMBL 397 7 2 8 4.0 c1ccc(CNc2nc(NCc3ccccc3)n3nc(-c4ccco4)nc3n2)cc1 10.1016/j.ejmech.2015.12.019
CHEMBL3754573 137558 None 0 Human Functional pIC50 = 4.9 4.9 - 1
Antagonist activity at human A2B adenosine receptor expressed in CHO cell membranes assessed as inhibition of NECA stimulated adenylyl cyclase activityAntagonist activity at human A2B adenosine receptor expressed in CHO cell membranes assessed as inhibition of NECA stimulated adenylyl cyclase activity
ChEMBL 397 7 2 8 4.0 c1ccc(CNc2nc(NCc3ccccc3)n3nc(-c4ccco4)nc3n2)cc1 10.1016/j.ejmech.2015.12.019
49797906 10744 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 467 7 1 7 4.3 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3cnn(Cc4cccc(F)c4)c3)sc12 10.1016/j.bmcl.2010.05.056
CHEMBL1171165 10744 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 467 7 1 7 4.3 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3cnn(Cc4cccc(F)c4)c3)sc12 10.1016/j.bmcl.2010.05.056
9930130 10801 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 387 5 1 5 4.1 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(F)cc3)sc12 10.1016/j.bmcl.2010.05.056
CHEMBL1171897 10801 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 387 5 1 5 4.1 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(F)cc3)sc12 10.1016/j.bmcl.2010.05.056
25231167 6217 None 0 Human Functional pIC50 = 6.9 6.9 20 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 313 5 2 6 2.4 CCNC(=O)c1nc(NCc2cccnc2)nc2ccsc12 10.1016/j.bmcl.2009.08.040
CHEMBL1081335 6217 None 0 Human Functional pIC50 = 6.9 6.9 20 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 313 5 2 6 2.4 CCNC(=O)c1nc(NCc2cccnc2)nc2ccsc12 10.1016/j.bmcl.2009.08.040
16071896 58025 None 44 Human Functional pIC50 = 6.9 6.9 4 2
Antagonist activity at human adenosine A2B receptor expressed in HEK293 cells assessed as inhibition of NECA-induced increase of intracellular cAMP level after 30 mins by ELISAAntagonist activity at human adenosine A2B receptor expressed in HEK293 cells assessed as inhibition of NECA-induced increase of intracellular cAMP level after 30 mins by ELISA
ChEMBL 335 4 1 5 3.1 O=C(Nc1cnc(-c2ccncc2F)c(-c2cccnc2)n1)C1CC1 10.1021/ml100249e
CHEMBL1672627 58025 None 44 Human Functional pIC50 = 6.9 6.9 4 2
Antagonist activity at human adenosine A2B receptor expressed in HEK293 cells assessed as inhibition of NECA-induced increase of intracellular cAMP level after 30 mins by ELISAAntagonist activity at human adenosine A2B receptor expressed in HEK293 cells assessed as inhibition of NECA-induced increase of intracellular cAMP level after 30 mins by ELISA
ChEMBL 335 4 1 5 3.1 O=C(Nc1cnc(-c2ccncc2F)c(-c2cccnc2)n1)C1CC1 10.1021/ml100249e
71508481 86276 None 6 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human adenosine A2b receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation by scintillation countingAntagonist activity at human adenosine A2b receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation by scintillation counting
ChEMBL 250 1 1 5 2.7 Nc1nc2ccccc2c2cc(-c3ccco3)nn12 10.1016/j.bmc.2012.10.031
CHEMBL2312725 86276 None 6 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human adenosine A2b receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation by scintillation countingAntagonist activity at human adenosine A2b receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation by scintillation counting
ChEMBL 250 1 1 5 2.7 Nc1nc2ccccc2c2cc(-c3ccco3)nn12 10.1016/j.bmc.2012.10.031
135529386 489 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptorInhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor
ChEMBL 537 10 2 12 0.4 CCOC(=O)c1ccc(cc1)NC(=O)COc1c/c(=C\2/N=c3c(=N2)c(=O)n(c(=O)n3CCC)CCC)/n([nH]1)C 10.1021/jm0309654
440 489 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptorInhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor
ChEMBL 537 10 2 12 0.4 CCOC(=O)c1ccc(cc1)NC(=O)COc1c/c(=C\2/N=c3c(=N2)c(=O)n(c(=O)n3CCC)CCC)/n([nH]1)C 10.1021/jm0309654
CHEMBL284615 489 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptorInhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor
ChEMBL 537 10 2 12 0.4 CCOC(=O)c1ccc(cc1)NC(=O)COc1c/c(=C\2/N=c3c(=N2)c(=O)n(c(=O)n3CCC)CCC)/n([nH]1)C 10.1021/jm0309654
135546657 157698 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptorInhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor
ChEMBL 509 10 2 10 2.3 CCCn1c(=O)c2[nH]c(-c3cc(NC(=O)Cc4ccc(OC)c(OC)c4)nn3C)nc2n(CCC)c1=O 10.1021/jm0309654
CHEMBL408186 157698 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptorInhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor
ChEMBL 509 10 2 10 2.3 CCCn1c(=O)c2[nH]c(-c3cc(NC(=O)Cc4ccc(OC)c(OC)c4)nn3C)nc2n(CCC)c1=O 10.1021/jm0309654
145954471 162382 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 367 5 2 8 3.9 COc1cccc(CNc2nc(N)c3nc(-c4ccc(C)o4)sc3n2)c1 10.1016/j.ejmech.2018.06.020
CHEMBL4165484 162382 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 367 5 2 8 3.9 COc1cccc(CNc2nc(N)c3nc(-c4ccc(C)o4)sc3n2)c1 10.1016/j.ejmech.2018.06.020
11793210 185872 None 0 Rat Functional pIC50 = 5.9 5.9 -7 2
Inhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytesInhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytes
ChEMBL 365 1 2 6 2.8 Cn1c(-c2ccc(F)cc2)nc2c(N)nc(C#CC3(O)CCCCC3)nc21 10.1021/jm990499b
CHEMBL48681 185872 None 0 Rat Functional pIC50 = 5.9 5.9 -7 2
Inhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytesInhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytes
ChEMBL 365 1 2 6 2.8 Cn1c(-c2ccc(F)cc2)nc2c(N)nc(C#CC3(O)CCCCC3)nc21 10.1021/jm990499b
57395163 69789 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assayAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assay
ChEMBL 404 4 2 9 2.9 COc1ccc(NC(=O)Nc2nc3cnn(C)c3c3nc(-c4ccco4)nn23)cc1 10.1016/j.bmc.2011.11.037
CHEMBL1935756 69789 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assayAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assay
ChEMBL 404 4 2 9 2.9 COc1ccc(NC(=O)Nc2nc3cnn(C)c3c3nc(-c4ccco4)nn23)cc1 10.1016/j.bmc.2011.11.037
45482090 197956 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity
ChEMBL 463 7 1 8 4.6 CC(C)CCn1cc2c(nc(NC(=O)Cc3ccc(Cl)cc3)n3nc(-c4ccco4)nc23)n1 10.1016/j.bmc.2009.05.038
CHEMBL573327 197956 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity
ChEMBL 463 7 1 8 4.6 CC(C)CCn1cc2c(nc(NC(=O)Cc3ccc(Cl)cc3)n3nc(-c4ccco4)nc23)n1 10.1016/j.bmc.2009.05.038
118708225 113358 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP level by scintillation counting analysisAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP level by scintillation counting analysis
ChEMBL 319 3 1 5 3.1 Nc1nc(Cc2ccccc2F)nc2cn(-c3ccccc3)nc12 10.1016/j.ejmech.2014.07.060
CHEMBL3317565 113358 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP level by scintillation counting analysisAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP level by scintillation counting analysis
ChEMBL 319 3 1 5 3.1 Nc1nc(Cc2ccccc2F)nc2cn(-c3ccccc3)nc12 10.1016/j.ejmech.2014.07.060
45482075 198303 None 0 Human Functional pIC50 = 4.9 4.9 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity
ChEMBL 451 6 1 8 4.5 CCCn1cc2c(nc(NC(=O)Cc3cccc4ccccc34)n3nc(-c4ccco4)nc23)n1 10.1016/j.bmc.2009.05.038
CHEMBL576018 198303 None 0 Human Functional pIC50 = 4.9 4.9 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity
ChEMBL 451 6 1 8 4.5 CCCn1cc2c(nc(NC(=O)Cc3cccc4ccccc34)n3nc(-c4ccco4)nc23)n1 10.1016/j.bmc.2009.05.038
46882998 5641 None 0 Human Functional pIC50 = 5.9 5.9 -10 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 303 4 1 6 3.7 CCNc1nc(C(=O)c2ccc(C)s2)c2sccc2n1 10.1016/j.bmcl.2009.08.040
CHEMBL1077752 5641 None 0 Human Functional pIC50 = 5.9 5.9 -10 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 303 4 1 6 3.7 CCNc1nc(C(=O)c2ccc(C)s2)c2sccc2n1 10.1016/j.bmcl.2009.08.040
164627235 186413 None 0 Human Functional pIC50 = 6.9 6.9 -22 2
Antagonist activity at human A2bR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assayAntagonist activity at human A2bR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assay
ChEMBL 433 4 2 7 3.2 Cc1cc(-c2c(-c3ccc(F)cc3)nc(N)n3nc(CN4CCCCC4)nc23)c[nH]c1=O 10.1021/acsmedchemlett.1c00620
CHEMBL4876056 186413 None 0 Human Functional pIC50 = 6.9 6.9 -22 2
Antagonist activity at human A2bR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assayAntagonist activity at human A2bR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assay
ChEMBL 433 4 2 7 3.2 Cc1cc(-c2c(-c3ccc(F)cc3)nc(N)n3nc(CN4CCCCC4)nc23)c[nH]c1=O 10.1021/acsmedchemlett.1c00620
135493281 109626 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptorInhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor
ChEMBL 483 8 2 8 2.9 CCCn1c(=O)c2nc(-c3cc(NC(=O)Cc4ccc(Cl)cc4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
CHEMBL32225 109626 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptorInhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor
ChEMBL 483 8 2 8 2.9 CCCn1c(=O)c2nc(-c3cc(NC(=O)Cc4ccc(Cl)cc4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
46883205 5850 None 0 Human Functional pIC50 = 5.9 5.9 -2 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 376 6 1 7 3.9 COc1ccc(C(=O)c2nc(NCc3cccnc3)nc3ccsc23)cc1 10.1016/j.bmcl.2009.08.040
CHEMBL1079232 5850 None 0 Human Functional pIC50 = 5.9 5.9 -2 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 376 6 1 7 3.9 COc1ccc(C(=O)c2nc(NCc3cccnc3)nc3ccsc23)cc1 10.1016/j.bmcl.2009.08.040
155554091 175691 None 0 Human Functional pIC50 = 7.9 7.9 -4 3
Antagonist activity at human A2BR expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP production by alphascreen assayAntagonist activity at human A2BR expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP production by alphascreen assay
ChEMBL 375 5 2 7 3.1 N#Cc1c(N)nc(SCc2cccc(C(N)=O)c2)c(C#N)c1-c1ccco1 10.1021/acs.jmedchem.9b00106
CHEMBL4581984 175691 None 0 Human Functional pIC50 = 7.9 7.9 -4 3
Antagonist activity at human A2BR expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP production by alphascreen assayAntagonist activity at human A2BR expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP production by alphascreen assay
ChEMBL 375 5 2 7 3.1 N#Cc1c(N)nc(SCc2cccc(C(N)=O)c2)c(C#N)c1-c1ccco1 10.1021/acs.jmedchem.9b00106
49798140 10870 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 484 9 1 7 3.6 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(C(=O)N(C)CCOC)cc3)sc12 10.1016/j.bmcl.2010.05.056
CHEMBL1172442 10870 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 484 9 1 7 3.6 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(C(=O)N(C)CCOC)cc3)sc12 10.1016/j.bmcl.2010.05.056
25231166 6353 None 0 Human Functional pIC50 = 7.9 7.9 181 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 353 4 1 6 3.5 CC(Nc1nc(C(=O)N2CCCC2)c2sccc2n1)c1cccnc1 10.1016/j.bmcl.2009.08.040
CHEMBL1082064 6353 None 0 Human Functional pIC50 = 7.9 7.9 181 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 353 4 1 6 3.5 CC(Nc1nc(C(=O)N2CCCC2)c2sccc2n1)c1cccnc1 10.1016/j.bmcl.2009.08.040
54581142 60732 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Inhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 minsInhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 mins
ChEMBL 598 8 2 7 5.2 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)[C@H]3CC[C@H](NS(=O)(=O)c4cccc(C(F)(F)F)c4)CC3)sc12 10.1016/j.bmcl.2011.02.053
CHEMBL1760896 60732 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Inhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 minsInhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 mins
ChEMBL 598 8 2 7 5.2 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)[C@H]3CC[C@H](NS(=O)(=O)c4cccc(C(F)(F)F)c4)CC3)sc12 10.1016/j.bmcl.2011.02.053
145436761 162837 None 0 Human Functional pIC50 = 7.9 7.9 -1 2
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 325 4 2 9 2.3 Nc1nc(NCc2cnccn2)nc2sc(-c3ccco3)nc12 10.1016/j.ejmech.2018.06.020
CHEMBL4172818 162837 None 0 Human Functional pIC50 = 7.9 7.9 -1 2
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 325 4 2 9 2.3 Nc1nc(NCc2cnccn2)nc2sc(-c3ccco3)nc12 10.1016/j.ejmech.2018.06.020
11826924 118745 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Inhibitory activity against NECA stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptorInhibitory activity against NECA stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptor
ChEMBL 479 8 1 9 4.0 O=C(COc1ccccc1)Nc1nc2nn(CCc3ccccc3)cc2c2nc(-c3ccco3)nn12 10.1021/jm030852k
CHEMBL341777 118745 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Inhibitory activity against NECA stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptorInhibitory activity against NECA stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptor
ChEMBL 479 8 1 9 4.0 O=C(COc1ccccc1)Nc1nc2nn(CCc3ccccc3)cc2c2nc(-c3ccco3)nn12 10.1021/jm030852k
10665407 190748 None 0 Rat Functional pIC50 = 5.9 5.9 - 1
Inhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytesInhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytes
ChEMBL 348 1 2 7 2.1 Cn1c(-c2ccccn2)nc2c(N)nc(C#CC3(O)CCCCC3)nc21 10.1021/jm990499b
CHEMBL51829 190748 None 0 Rat Functional pIC50 = 5.9 5.9 - 1
Inhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytesInhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytes
ChEMBL 348 1 2 7 2.1 Cn1c(-c2ccccn2)nc2c(N)nc(C#CC3(O)CCCCC3)nc21 10.1021/jm990499b
45482076 198102 None 0 Human Functional pIC50 = 4.9 4.9 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity
ChEMBL 391 4 1 8 2.6 Cn1cc2c(nc(NC(=O)Cc3ccc(F)cc3)n3nc(-c4ccco4)nc23)n1 10.1016/j.bmc.2009.05.038
CHEMBL574483 198102 None 0 Human Functional pIC50 = 4.9 4.9 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity
ChEMBL 391 4 1 8 2.6 Cn1cc2c(nc(NC(=O)Cc3ccc(F)cc3)n3nc(-c4ccco4)nc23)n1 10.1016/j.bmc.2009.05.038
46238067 8506 None 0 Human Functional pIC50 = 5.9 5.9 -229 2
Antagonist activity human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated [3H]cAMP accumulation treated 15 mins before NECA challenge measured after 30 mins by liquid scintillation spectrometryAntagonist activity human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated [3H]cAMP accumulation treated 15 mins before NECA challenge measured after 30 mins by liquid scintillation spectrometry
ChEMBL 420 5 2 5 5.2 O=C(Nc1ccccc1)Nc1nc(-c2ccccc2)nc2nn(Cc3ccccc3)cc12 10.1021/jm901785w
CHEMBL1094132 8506 None 0 Human Functional pIC50 = 5.9 5.9 -229 2
Antagonist activity human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated [3H]cAMP accumulation treated 15 mins before NECA challenge measured after 30 mins by liquid scintillation spectrometryAntagonist activity human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated [3H]cAMP accumulation treated 15 mins before NECA challenge measured after 30 mins by liquid scintillation spectrometry
ChEMBL 420 5 2 5 5.2 O=C(Nc1ccccc1)Nc1nc(-c2ccccc2)nc2nn(Cc3ccccc3)cc12 10.1021/jm901785w
46238066 8505 None 0 Human Functional pIC50 = 5.9 5.9 -173 2
Antagonist activity human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated [3H]cAMP accumulation treated 15 mins before NECA challenge measured after 30 mins by liquid scintillation spectrometryAntagonist activity human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated [3H]cAMP accumulation treated 15 mins before NECA challenge measured after 30 mins by liquid scintillation spectrometry
ChEMBL 439 5 1 5 5.4 O=C(Nc1nc(-c2ccccc2)nc2nn(Cc3ccccc3)cc12)c1cccc(Cl)c1 10.1021/jm901785w
CHEMBL1094131 8505 None 0 Human Functional pIC50 = 5.9 5.9 -173 2
Antagonist activity human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated [3H]cAMP accumulation treated 15 mins before NECA challenge measured after 30 mins by liquid scintillation spectrometryAntagonist activity human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated [3H]cAMP accumulation treated 15 mins before NECA challenge measured after 30 mins by liquid scintillation spectrometry
ChEMBL 439 5 1 5 5.4 O=C(Nc1nc(-c2ccccc2)nc2nn(Cc3ccccc3)cc12)c1cccc(Cl)c1 10.1021/jm901785w
145962529 161391 None 0 Human Functional pIC50 = 6.9 6.9 -1 3
Antagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assayAntagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assay
ChEMBL 291 4 2 7 2.7 Cc1nc2c(N)nc(NCCc3cccs3)nc2s1 10.1016/j.bmc.2018.05.048
CHEMBL4126427 161391 None 0 Human Functional pIC50 = 6.9 6.9 -1 3
Antagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assayAntagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assay
ChEMBL 291 4 2 7 2.7 Cc1nc2c(N)nc(NCCc3cccs3)nc2s1 10.1016/j.bmc.2018.05.048
15729970 137298 None 0 Human Functional pIC50 = 4.9 4.9 - 1
Antagonist activity at human A2B adenosine receptor expressed in CHO cell membranes assessed as inhibition of NECA stimulated adenylyl cyclase activityAntagonist activity at human A2B adenosine receptor expressed in CHO cell membranes assessed as inhibition of NECA stimulated adenylyl cyclase activity
ChEMBL 299 3 2 8 2.1 Nc1nc(NC2CCCCC2)nc2nc(-c3ccco3)nn12 10.1016/j.ejmech.2015.12.019
CHEMBL3752431 137298 None 0 Human Functional pIC50 = 4.9 4.9 - 1
Antagonist activity at human A2B adenosine receptor expressed in CHO cell membranes assessed as inhibition of NECA stimulated adenylyl cyclase activityAntagonist activity at human A2B adenosine receptor expressed in CHO cell membranes assessed as inhibition of NECA stimulated adenylyl cyclase activity
ChEMBL 299 3 2 8 2.1 Nc1nc(NC2CCCCC2)nc2nc(-c3ccco3)nn12 10.1016/j.ejmech.2015.12.019
145964662 164438 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-induced cAMP accumulation preincubated for 1 hr followed by NECA induction measured after 5 mins in presence of [3H]cAMP and bovine cAMP-binding protein by liquid scintillation counting methodAntagonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-induced cAMP accumulation preincubated for 1 hr followed by NECA induction measured after 5 mins in presence of [3H]cAMP and bovine cAMP-binding protein by liquid scintillation counting method
ChEMBL 433 8 3 6 2.2 CCCn1c(=O)[nH]c2nc(-c3ccc(OCC(=O)NCc4ccccc4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.7b01627
CHEMBL4213768 164438 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-induced cAMP accumulation preincubated for 1 hr followed by NECA induction measured after 5 mins in presence of [3H]cAMP and bovine cAMP-binding protein by liquid scintillation counting methodAntagonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-induced cAMP accumulation preincubated for 1 hr followed by NECA induction measured after 5 mins in presence of [3H]cAMP and bovine cAMP-binding protein by liquid scintillation counting method
ChEMBL 433 8 3 6 2.2 CCCn1c(=O)[nH]c2nc(-c3ccc(OCC(=O)NCc4ccccc4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.7b01627
45481758 198346 None 0 Human Functional pIC50 = 4.9 4.9 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity
ChEMBL 379 4 1 9 2.5 Cn1cc2c(nc(NC(=O)Cc3ccsc3)n3nc(-c4ccco4)nc23)n1 10.1016/j.bmc.2009.05.038
CHEMBL576369 198346 None 0 Human Functional pIC50 = 4.9 4.9 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity
ChEMBL 379 4 1 9 2.5 Cn1cc2c(nc(NC(=O)Cc3ccsc3)n3nc(-c4ccco4)nc23)n1 10.1016/j.bmc.2009.05.038
45481619 198327 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity
ChEMBL 463 7 1 8 4.6 CC(C)CCn1cc2c(nc(NC(=O)Cc3cccc(Cl)c3)n3nc(-c4ccco4)nc23)n1 10.1016/j.bmc.2009.05.038
CHEMBL576185 198327 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity
ChEMBL 463 7 1 8 4.6 CC(C)CCn1cc2c(nc(NC(=O)Cc3cccc(Cl)c3)n3nc(-c4ccco4)nc23)n1 10.1016/j.bmc.2009.05.038
53248698 60723 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Inhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 minsInhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 mins
ChEMBL 534 6 1 6 4.8 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)[C@@H]3CCN(C(=O)c4cccc(C(F)(F)F)c4)C3)sc12 10.1016/j.bmcl.2011.02.053
CHEMBL1760886 60723 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Inhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 minsInhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 mins
ChEMBL 534 6 1 6 4.8 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)[C@@H]3CCN(C(=O)c4cccc(C(F)(F)F)c4)C3)sc12 10.1016/j.bmcl.2011.02.053
10544916 188309 None 0 Human Functional pIC50 = 7.9 7.9 15 2
Inhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptorInhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptor
ChEMBL 337 1 2 7 2.3 Cn1c(-c2ccco2)nc2c(N)nc(C#CC3(O)CCCCC3)nc21 10.1021/jm990499b
CHEMBL50051 188309 None 0 Human Functional pIC50 = 7.9 7.9 15 2
Inhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptorInhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptor
ChEMBL 337 1 2 7 2.3 Cn1c(-c2ccco2)nc2c(N)nc(C#CC3(O)CCCCC3)nc21 10.1021/jm990499b
145436762 162510 None 0 Human Functional pIC50 = 7.9 7.9 -3 2
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 327 5 2 8 3.2 Nc1nc(NCCc2ccco2)nc2sc(-c3ccco3)nc12 10.1016/j.ejmech.2018.06.020
CHEMBL4167557 162510 None 0 Human Functional pIC50 = 7.9 7.9 -3 2
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 327 5 2 8 3.2 Nc1nc(NCCc2ccco2)nc2sc(-c3ccco3)nc12 10.1016/j.ejmech.2018.06.020
11027412 29629 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Inhibitory activity against NECA stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptorInhibitory activity against NECA stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptor
ChEMBL 493 9 1 9 4.4 O=C(COc1ccccc1)Nc1nc2nn(CCCc3ccccc3)cc2c2nc(-c3ccco3)nn12 10.1021/jm030852k
CHEMBL138593 29629 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Inhibitory activity against NECA stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptorInhibitory activity against NECA stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptor
ChEMBL 493 9 1 9 4.4 O=C(COc1ccccc1)Nc1nc2nn(CCCc3ccccc3)cc2c2nc(-c3ccco3)nn12 10.1021/jm030852k
135465785 488 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptorInhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor
ChEMBL 496 8 2 12 0.0 CCCn1c2=N/C(=c/3\o[nH]c(c3)OCC(=O)Nc3ccc4c(c3)OCO4)/N=c2c(=O)n(c1=O)CCC 10.1021/jm0309654
439 488 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptorInhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor
ChEMBL 496 8 2 12 0.0 CCCn1c2=N/C(=c/3\o[nH]c(c3)OCC(=O)Nc3ccc4c(c3)OCO4)/N=c2c(=O)n(c1=O)CCC 10.1021/jm0309654
CHEMBL32582 488 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptorInhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor
ChEMBL 496 8 2 12 0.0 CCCn1c2=N/C(=c/3\o[nH]c(c3)OCC(=O)Nc3ccc4c(c3)OCO4)/N=c2c(=O)n(c1=O)CCC 10.1021/jm0309654
10665761 189276 None 0 Human Functional pIC50 = 6.9 6.9 3 2
Inhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptorInhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptor
ChEMBL 353 3 2 6 2.7 CCC(O)(C#Cc1nc(N)c2nc(-c3cccc(F)c3)n(C)c2n1)CC 10.1021/jm990499b
CHEMBL51192 189276 None 0 Human Functional pIC50 = 6.9 6.9 3 2
Inhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptorInhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptor
ChEMBL 353 3 2 6 2.7 CCC(O)(C#Cc1nc(N)c2nc(-c3cccc(F)c3)n(C)c2n1)CC 10.1021/jm990499b
145976828 163678 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-induced cAMP accumulation preincubated for 1 hr followed by NECA induction measured after 5 mins in presence of [3H]cAMP and bovine cAMP-binding protein by liquid scintillation counting methodAntagonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-induced cAMP accumulation preincubated for 1 hr followed by NECA induction measured after 5 mins in presence of [3H]cAMP and bovine cAMP-binding protein by liquid scintillation counting method
ChEMBL 447 9 3 6 2.2 CCCn1c(=O)[nH]c2nc(-c3ccc(OCC(=O)NCCc4ccccc4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.7b01627
CHEMBL4204683 163678 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-induced cAMP accumulation preincubated for 1 hr followed by NECA induction measured after 5 mins in presence of [3H]cAMP and bovine cAMP-binding protein by liquid scintillation counting methodAntagonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-induced cAMP accumulation preincubated for 1 hr followed by NECA induction measured after 5 mins in presence of [3H]cAMP and bovine cAMP-binding protein by liquid scintillation counting method
ChEMBL 447 9 3 6 2.2 CCCn1c(=O)[nH]c2nc(-c3ccc(OCC(=O)NCCc4ccccc4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.7b01627
45482081 197929 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity
ChEMBL 497 7 1 8 5.3 CC(C)CCn1cc2c(nc(NC(=O)Cc3c(Cl)cccc3Cl)n3nc(-c4ccco4)nc23)n1 10.1016/j.bmc.2009.05.038
CHEMBL573089 197929 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity
ChEMBL 497 7 1 8 5.3 CC(C)CCn1cc2c(nc(NC(=O)Cc3c(Cl)cccc3Cl)n3nc(-c4ccco4)nc23)n1 10.1016/j.bmc.2009.05.038
156010667 177117 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Inhibition of human A2B receptor expressed in CHO cells assessed as reduction in cAMP productionInhibition of human A2B receptor expressed in CHO cells assessed as reduction in cAMP production
ChEMBL 556 9 4 11 2.0 Nc1nc(NCC2CCN(CC(=O)NCc3ccc(S(N)(=O)=O)cc3)CC2)nc2sc(-c3ccco3)nc12 10.1016/j.bmcl.2020.127067
CHEMBL4633630 177117 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Inhibition of human A2B receptor expressed in CHO cells assessed as reduction in cAMP productionInhibition of human A2B receptor expressed in CHO cells assessed as reduction in cAMP production
ChEMBL 556 9 4 11 2.0 Nc1nc(NCC2CCN(CC(=O)NCc3ccc(S(N)(=O)=O)cc3)CC2)nc2sc(-c3ccco3)nc12 10.1016/j.bmcl.2020.127067
46238068 8735 None 0 Human Functional pIC50 = 5.8 5.8 -181 2
Antagonist activity human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated [3H]cAMP accumulation treated 15 mins before NECA challenge measured after 30 mins by liquid scintillation spectrometryAntagonist activity human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated [3H]cAMP accumulation treated 15 mins before NECA challenge measured after 30 mins by liquid scintillation spectrometry
ChEMBL 450 6 2 6 5.2 COc1ccc(NC(=O)Nc2nc(-c3ccccc3)nc3nn(Cc4ccccc4)cc23)cc1 10.1021/jm901785w
CHEMBL1096078 8735 None 0 Human Functional pIC50 = 5.8 5.8 -181 2
Antagonist activity human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated [3H]cAMP accumulation treated 15 mins before NECA challenge measured after 30 mins by liquid scintillation spectrometryAntagonist activity human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated [3H]cAMP accumulation treated 15 mins before NECA challenge measured after 30 mins by liquid scintillation spectrometry
ChEMBL 450 6 2 6 5.2 COc1ccc(NC(=O)Nc2nc(-c3ccccc3)nc3nn(Cc4ccccc4)cc23)cc1 10.1021/jm901785w
46883157 5822 None 0 Human Functional pIC50 = 6.8 6.8 11 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 353 5 1 8 3.4 O=C(c1cncs1)c1nc(NCc2cccnc2)nc2ccsc12 10.1016/j.bmcl.2009.08.040
CHEMBL1079044 5822 None 0 Human Functional pIC50 = 6.8 6.8 11 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 353 5 1 8 3.4 O=C(c1cncs1)c1nc(NCc2cccnc2)nc2ccsc12 10.1016/j.bmcl.2009.08.040
46883155 5837 None 0 Human Functional pIC50 = 6.8 6.8 2 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 352 5 1 7 4.0 O=C(c1ccsc1)c1nc(NCc2cccnc2)nc2ccsc12 10.1016/j.bmcl.2009.08.040
CHEMBL1079132 5837 None 0 Human Functional pIC50 = 6.8 6.8 2 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 352 5 1 7 4.0 O=C(c1ccsc1)c1nc(NCc2cccnc2)nc2ccsc12 10.1016/j.bmcl.2009.08.040
10449783 9646 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulationAntagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulation
ChEMBL 338 2 0 5 3.7 O=c1c(-c2ccccc2)nnc2n(-c3ccccc3)c3ccccc3n12 10.1021/jm201177b
CHEMBL112756 9646 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulationAntagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulation
ChEMBL 338 2 0 5 3.7 O=c1c(-c2ccccc2)nnc2n(-c3ccccc3)c3ccccc3n12 10.1021/jm201177b
10237267 10802 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 373 4 1 5 3.7 COc1ccc(N(C)C(C)=O)c2sc(NC(=O)c3ccc(F)cc3)nc12 10.1016/j.bmcl.2010.05.056
CHEMBL1171898 10802 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 373 4 1 5 3.7 COc1ccc(N(C)C(C)=O)c2sc(NC(=O)c3ccc(F)cc3)nc12 10.1016/j.bmcl.2010.05.056
136042350 71150 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 496 8 2 9 3.2 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5cc(Cl)ccc5[nH]4)nn3C)nc2n(CCC)c1=O 10.1021/jm201292w
CHEMBL1955899 71150 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 496 8 2 9 3.2 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5cc(Cl)ccc5[nH]4)nn3C)nc2n(CCC)c1=O 10.1021/jm201292w
10824674 204908 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulationAntagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulation
ChEMBL 252 1 1 6 2.2 Oc1c(-c2ccco2)nnc2nc3ccccc3n12 10.1021/jm201177b
CHEMBL7608 204908 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulationAntagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulation
ChEMBL 252 1 1 6 2.2 Oc1c(-c2ccco2)nnc2nc3ccccc3n12 10.1021/jm201177b
10895565 168452 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Inhibitory activity against NECA stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptorInhibitory activity against NECA stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptor
ChEMBL 445 8 1 9 3.8 CC(C)CCn1cc2c(nc(NC(=O)COc3ccccc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm030852k
CHEMBL435022 168452 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Inhibitory activity against NECA stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptorInhibitory activity against NECA stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptor
ChEMBL 445 8 1 9 3.8 CC(C)CCn1cc2c(nc(NC(=O)COc3ccccc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm030852k
10616023 101862 None 0 Human Functional pIC50 = 6.8 6.8 3 2
Inhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptorInhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptor
ChEMBL 325 1 2 6 1.9 Cn1c(-c2cccc(F)c2)nc2c(N)nc(C#CC(C)(C)O)nc21 10.1021/jm990499b
CHEMBL300624 101862 None 0 Human Functional pIC50 = 6.8 6.8 3 2
Inhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptorInhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptor
ChEMBL 325 1 2 6 1.9 Cn1c(-c2cccc(F)c2)nc2c(N)nc(C#CC(C)(C)O)nc21 10.1021/jm990499b
6448585 98339 None 6 Human Functional pIC50 = 5.8 5.8 -1513 3
Inhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptorInhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptor
ChEMBL 412 8 0 8 2.9 CCCn1c(=O)c2c(nc(/C=C/c3ccc(OC)c(OC)c3)n2C)n(CCC)c1=O 10.1021/jm990499b
CHEMBL2311150 98339 None 6 Human Functional pIC50 = 5.8 5.8 -1513 3
Inhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptorInhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptor
ChEMBL 412 8 0 8 2.9 CCCn1c(=O)c2c(nc(/C=C/c3ccc(OC)c(OC)c3)n2C)n(CCC)c1=O 10.1021/jm990499b
CHEMBL27508 98339 None 6 Human Functional pIC50 = 5.8 5.8 -1513 3
Inhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptorInhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptor
ChEMBL 412 8 0 8 2.9 CCCn1c(=O)c2c(nc(/C=C/c3ccc(OC)c(OC)c3)n2C)n(CCC)c1=O 10.1021/jm990499b
45481757 198007 None 0 Human Functional pIC50 = 4.8 4.8 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity
ChEMBL 393 5 1 9 3.0 CCn1cc2c(nc(NC(=O)Cc3cccs3)n3nc(-c4ccco4)nc23)n1 10.1016/j.bmc.2009.05.038
CHEMBL573779 198007 None 0 Human Functional pIC50 = 4.8 4.8 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity
ChEMBL 393 5 1 9 3.0 CCn1cc2c(nc(NC(=O)Cc3cccs3)n3nc(-c4ccco4)nc23)n1 10.1016/j.bmc.2009.05.038
155554464 174602 None 0 Human Functional pIC50 = 6.8 6.8 -30 3
Antagonist activity at human A2BR expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP production by alphascreen assayAntagonist activity at human A2BR expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP production by alphascreen assay
ChEMBL 362 5 2 7 3.5 N#Cc1c(N)nc(SCc2cccc(CO)c2)c(C#N)c1-c1ccco1 10.1021/acs.jmedchem.9b00106
CHEMBL4557250 174602 None 0 Human Functional pIC50 = 6.8 6.8 -30 3
Antagonist activity at human A2BR expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP production by alphascreen assayAntagonist activity at human A2BR expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP production by alphascreen assay
ChEMBL 362 5 2 7 3.5 N#Cc1c(N)nc(SCc2cccc(CO)c2)c(C#N)c1-c1ccco1 10.1021/acs.jmedchem.9b00106
127045701 139970 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated cAMP level preincubated for 10 mins followed by NECA stimulation by scintillation counting method in presence of [3H]-cyclic AMPAntagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated cAMP level preincubated for 10 mins followed by NECA stimulation by scintillation counting method in presence of [3H]-cyclic AMP
ChEMBL 339 3 1 6 3.7 Cc1ccc(-c2nc(N)c3nn(Cc4ccccc4Cl)cc3n2)o1 10.1016/j.bmc.2016.04.048
CHEMBL3799848 139970 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated cAMP level preincubated for 10 mins followed by NECA stimulation by scintillation counting method in presence of [3H]-cyclic AMPAntagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated cAMP level preincubated for 10 mins followed by NECA stimulation by scintillation counting method in presence of [3H]-cyclic AMP
ChEMBL 339 3 1 6 3.7 Cc1ccc(-c2nc(N)c3nn(Cc4ccccc4Cl)cc3n2)o1 10.1016/j.bmc.2016.04.048
136002186 109701 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptorInhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor
ChEMBL 449 8 2 8 2.3 CCCn1c(=O)c2nc(-c3cc(NC(=O)Cc4ccccc4)n(C)n3)[nH]c2n(CCC)c1=O 10.1021/jm0309654
CHEMBL32281 109701 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptorInhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor
ChEMBL 449 8 2 8 2.3 CCCn1c(=O)c2nc(-c3cc(NC(=O)Cc4ccccc4)n(C)n3)[nH]c2n(CCC)c1=O 10.1021/jm0309654
23656936 154896 None 0 Human Functional pIC50 = 5.8 5.8 -2630 2
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP accumulationAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP accumulation
ChEMBL 425 4 1 7 3.6 COc1ccc(C(=O)Nc2nc3ccccc3n3c(=O)c(-c4ccc(C)cc4)nn23)cc1 10.1021/jm0708376
CHEMBL400812 154896 None 0 Human Functional pIC50 = 5.8 5.8 -2630 2
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP accumulationAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP accumulation
ChEMBL 425 4 1 7 3.6 COc1ccc(C(=O)Nc2nc3ccccc3n3c(=O)c(-c4ccc(C)cc4)nn23)cc1 10.1021/jm0708376
60156107 76985 None 0 Human Functional pIC50 = 5.8 5.8 -33 2
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production
ChEMBL 542 7 3 9 3.2 Cn1cc2c(nc(NC(=O)NC3CCN(C(=O)NCCCc4ccccc4)CC3)n3nc(-c4ccco4)nc23)n1 10.1021/jm300323t
CHEMBL2071045 76985 None 0 Human Functional pIC50 = 5.8 5.8 -33 2
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production
ChEMBL 542 7 3 9 3.2 Cn1cc2c(nc(NC(=O)NC3CCN(C(=O)NCCCc4ccccc4)CC3)n3nc(-c4ccco4)nc23)n1 10.1021/jm300323t
135874415 95894 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP levelsAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP levels
ChEMBL 527 8 2 8 3.3 CCCn1c(=O)c2[nH]c(-c3cc(C)n(CC(=O)Nc4ccc(Br)cc4)n3)nc2n(CCC)c1=O 10.1016/j.bmc.2007.11.058
CHEMBL259177 95894 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP levelsAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP levels
ChEMBL 527 8 2 8 3.3 CCCn1c(=O)c2[nH]c(-c3cc(C)n(CC(=O)Nc4ccc(Br)cc4)n3)nc2n(CCC)c1=O 10.1016/j.bmc.2007.11.058
156018055 177920 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Inhibition of human A2B receptor expressed in CHO cells assessed as reduction in cAMP productionInhibition of human A2B receptor expressed in CHO cells assessed as reduction in cAMP production
ChEMBL 570 10 4 11 2.1 Nc1nc(NCC2CCN(CC(=O)NCCc3ccc(S(N)(=O)=O)cc3)CC2)nc2sc(-c3ccco3)nc12 10.1016/j.bmcl.2020.127067
CHEMBL4645283 177920 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Inhibition of human A2B receptor expressed in CHO cells assessed as reduction in cAMP productionInhibition of human A2B receptor expressed in CHO cells assessed as reduction in cAMP production
ChEMBL 570 10 4 11 2.1 Nc1nc(NCC2CCN(CC(=O)NCCc3ccc(S(N)(=O)=O)cc3)CC2)nc2sc(-c3ccco3)nc12 10.1016/j.bmcl.2020.127067
49797748 10620 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 480 6 1 6 4.6 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(C(=O)N4CCCCC4)cc3)sc12 10.1016/j.bmcl.2010.05.056
CHEMBL1170135 10620 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 480 6 1 6 4.6 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(C(=O)N4CCCCC4)cc3)sc12 10.1016/j.bmcl.2010.05.056
49798137 10745 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 466 6 1 6 4.2 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(C(=O)N4CCCC4)cc3)sc12 10.1016/j.bmcl.2010.05.056
CHEMBL1171200 10745 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 466 6 1 6 4.2 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(C(=O)N4CCCC4)cc3)sc12 10.1016/j.bmcl.2010.05.056
46883208 5980 None 0 Human Functional pIC50 = 7.8 7.8 3 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 386 5 1 7 4.6 O=C(c1cccs1)c1nc(NCc2cccnc2)nc2cc(Cl)sc12 10.1016/j.bmcl.2009.08.040
CHEMBL1080068 5980 None 0 Human Functional pIC50 = 7.8 7.8 3 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 386 5 1 7 4.6 O=C(c1cccs1)c1nc(NCc2cccnc2)nc2cc(Cl)sc12 10.1016/j.bmcl.2009.08.040
54581142 60721 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Inhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 minsInhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 mins
ChEMBL 598 8 2 7 5.2 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)[C@H]3CC[C@@H](NS(=O)(=O)c4cccc(C(F)(F)F)c4)CC3)sc12 10.1016/j.bmcl.2011.02.053
CHEMBL1760884 60721 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Inhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 minsInhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 mins
ChEMBL 598 8 2 7 5.2 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)[C@H]3CC[C@@H](NS(=O)(=O)c4cccc(C(F)(F)F)c4)CC3)sc12 10.1016/j.bmcl.2011.02.053
44186717 184145 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2
ChEMBL 538 8 2 8 2.0 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc(OC)cc5)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
CHEMBL482855 184145 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2
ChEMBL 538 8 2 8 2.0 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc(OC)cc5)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
135465774 111479 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptorInhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor
ChEMBL 467 8 2 8 2.4 CCCn1c(=O)c2nc(-c3cc(NC(=O)Cc4cccc(F)c4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
CHEMBL32770 111479 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptorInhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor
ChEMBL 467 8 2 8 2.4 CCCn1c(=O)c2nc(-c3cc(NC(=O)Cc4cccc(F)c4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
11793210 185872 None 0 Human Functional pIC50 = 6.8 6.8 7 2
Inhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptorInhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptor
ChEMBL 365 1 2 6 2.8 Cn1c(-c2ccc(F)cc2)nc2c(N)nc(C#CC3(O)CCCCC3)nc21 10.1021/jm990499b
CHEMBL48681 185872 None 0 Human Functional pIC50 = 6.8 6.8 7 2
Inhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptorInhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptor
ChEMBL 365 1 2 6 2.8 Cn1c(-c2ccc(F)cc2)nc2c(N)nc(C#CC3(O)CCCCC3)nc21 10.1021/jm990499b
10667322 101501 None 0 Rat Functional pIC50 = 5.8 5.8 - 1
Inhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytesInhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytes
ChEMBL 377 2 2 7 2.7 COc1cccc(-c2nc3c(N)nc(C#CC4(O)CCCCC4)nc3n2C)c1 10.1021/jm990499b
CHEMBL297949 101501 None 0 Rat Functional pIC50 = 5.8 5.8 - 1
Inhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytesInhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytes
ChEMBL 377 2 2 7 2.7 COc1cccc(-c2nc3c(N)nc(C#CC4(O)CCCCC4)nc3n2C)c1 10.1021/jm990499b
46883107 5832 None 0 Human Functional pIC50 = 7.8 7.8 5 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 380 5 1 7 4.9 Cc1ccc(C(=O)c2nc(NC(C)c3cccnc3)nc3ccsc23)s1 10.1016/j.bmcl.2009.08.040
CHEMBL1079115 5832 None 0 Human Functional pIC50 = 7.8 7.8 5 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 380 5 1 7 4.9 Cc1ccc(C(=O)c2nc(NC(C)c3cccnc3)nc3ccsc23)s1 10.1016/j.bmcl.2009.08.040
54584124 60728 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Inhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 minsInhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 mins
ChEMBL 548 6 1 6 5.2 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)C3CCN(C(=O)c4cccc(C(F)(F)F)c4)CC3)sc12 10.1016/j.bmcl.2011.02.053
CHEMBL1760892 60728 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Inhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 minsInhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 mins
ChEMBL 548 6 1 6 5.2 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)C3CCN(C(=O)c4cccc(C(F)(F)F)c4)CC3)sc12 10.1016/j.bmcl.2011.02.053
10906943 116530 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Inhibitory activity against NECA stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptorInhibitory activity against NECA stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptor
ChEMBL 479 7 1 8 5.1 CC(C)CCn1cc2c(nc(NC(=O)Cc3cccc4ccccc34)n3nc(-c4ccco4)nc23)n1 10.1021/jm030852k
CHEMBL336217 116530 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Inhibitory activity against NECA stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptorInhibitory activity against NECA stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptor
ChEMBL 479 7 1 8 5.1 CC(C)CCn1cc2c(nc(NC(=O)Cc3cccc4ccccc34)n3nc(-c4ccco4)nc23)n1 10.1021/jm030852k
155520955 170570 None 0 Human Functional pIC50 = 4.8 4.8 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity by Glo-sensor cAMP assayAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity by Glo-sensor cAMP assay
ChEMBL 351 2 4 9 1.2 Nc1nc(-c2cc(O)c(O)c(O)c2)cn2c(=O)n(-c3ccccc3)nc12 10.1021/acs.jmedchem.9b00778
CHEMBL4450312 170570 None 0 Human Functional pIC50 = 4.8 4.8 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity by Glo-sensor cAMP assayAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity by Glo-sensor cAMP assay
ChEMBL 351 2 4 9 1.2 Nc1nc(-c2cc(O)c(O)c(O)c2)cn2c(=O)n(-c3ccccc3)nc12 10.1021/acs.jmedchem.9b00778
145964230 164011 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-induced cAMP accumulation preincubated for 1 hr followed by NECA induction measured after 5 mins in presence of [3H]cAMP and bovine cAMP-binding protein by liquid scintillation counting methodAntagonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-induced cAMP accumulation preincubated for 1 hr followed by NECA induction measured after 5 mins in presence of [3H]cAMP and bovine cAMP-binding protein by liquid scintillation counting method
ChEMBL 461 10 3 6 2.6 CCCn1c(=O)[nH]c2nc(-c3ccc(OCC(=O)NCCCc4ccccc4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.7b01627
CHEMBL4208432 164011 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-induced cAMP accumulation preincubated for 1 hr followed by NECA induction measured after 5 mins in presence of [3H]cAMP and bovine cAMP-binding protein by liquid scintillation counting methodAntagonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-induced cAMP accumulation preincubated for 1 hr followed by NECA induction measured after 5 mins in presence of [3H]cAMP and bovine cAMP-binding protein by liquid scintillation counting method
ChEMBL 461 10 3 6 2.6 CCCn1c(=O)[nH]c2nc(-c3ccc(OCC(=O)NCCCc4ccccc4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.7b01627
60156106 76803 None 0 Human Functional pIC50 = 5.8 5.8 -75 2
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production
ChEMBL 528 6 3 9 2.8 Cn1cc2c(nc(NC(=O)NC3CCN(C(=O)NCCc4ccccc4)CC3)n3nc(-c4ccco4)nc23)n1 10.1021/jm300323t
CHEMBL2069325 76803 None 0 Human Functional pIC50 = 5.8 5.8 -75 2
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production
ChEMBL 528 6 3 9 2.8 Cn1cc2c(nc(NC(=O)NC3CCN(C(=O)NCCc4ccccc4)CC3)n3nc(-c4ccco4)nc23)n1 10.1021/jm300323t
46883156 5821 None 0 Human Functional pIC50 = 6.8 6.8 4 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 353 5 1 8 3.4 O=C(c1nccs1)c1nc(NCc2cccnc2)nc2ccsc12 10.1016/j.bmcl.2009.08.040
CHEMBL1079043 5821 None 0 Human Functional pIC50 = 6.8 6.8 4 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 353 5 1 8 3.4 O=C(c1nccs1)c1nc(NCc2cccnc2)nc2ccsc12 10.1016/j.bmcl.2009.08.040
134147994 150110 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 351 6 2 7 4.0 Nc1nc(NCCCc2ccccc2)nc2sc(-c3ccco3)nc12 10.1021/acs.jmedchem.6b01068
CHEMBL3951103 150110 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 351 6 2 7 4.0 Nc1nc(NCCCc2ccccc2)nc2sc(-c3ccco3)nc12 10.1021/acs.jmedchem.6b01068
46883110 5835 None 0 Human Functional pIC50 = 7.8 7.8 2 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 352 5 1 7 4.0 O=C(c1cccs1)c1nc(NCc2cccnc2)nc2ccsc12 10.1016/j.bmcl.2009.08.040
CHEMBL1079118 5835 None 0 Human Functional pIC50 = 7.8 7.8 2 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 352 5 1 7 4.0 O=C(c1cccs1)c1nc(NCc2cccnc2)nc2ccsc12 10.1016/j.bmcl.2009.08.040
25230181 5959 None 0 Human Functional pIC50 = 7.8 7.8 26 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 353 4 1 6 3.5 C[C@H](Nc1nc(C(=O)N2CCCC2)c2sccc2n1)c1cccnc1 10.1016/j.bmcl.2009.08.040
CHEMBL1079894 5959 None 0 Human Functional pIC50 = 7.8 7.8 26 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 353 4 1 6 3.5 C[C@H](Nc1nc(C(=O)N2CCCC2)c2sccc2n1)c1cccnc1 10.1016/j.bmcl.2009.08.040
54585058 60735 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Inhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 minsInhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 mins
ChEMBL 520 5 1 5 6.1 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)N3CCC(c4cccc(C(F)(F)F)c4)CC3)sc12 10.1016/j.bmcl.2011.02.053
CHEMBL1760900 60735 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Inhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 minsInhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 mins
ChEMBL 520 5 1 5 6.1 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)N3CCC(c4cccc(C(F)(F)F)c4)CC3)sc12 10.1016/j.bmcl.2011.02.053
134152846 153542 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 369 5 4 9 3.0 Nc1nc(NCCc2ccc(O)c(O)c2)nc2sc(-c3ccco3)nc12 10.1021/acs.jmedchem.6b01068
CHEMBL3980049 153542 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 369 5 4 9 3.0 Nc1nc(NCCc2ccc(O)c(O)c2)nc2sc(-c3ccco3)nc12 10.1021/acs.jmedchem.6b01068
3284 3216 None 35 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-induced cAMP accumulation preincubated for 1 hr followed by NECA induction measured after 5 mins in presence of [3H]cAMP and bovine cAMP-binding protein by liquid scintillation counting methodAntagonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-induced cAMP accumulation preincubated for 1 hr followed by NECA induction measured after 5 mins in presence of [3H]cAMP and bovine cAMP-binding protein by liquid scintillation counting method
ChEMBL 528 6 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)c1ccc(cc1)Cl 10.1021/acs.jmedchem.7b01627
44185871 3216 None 35 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-induced cAMP accumulation preincubated for 1 hr followed by NECA induction measured after 5 mins in presence of [3H]cAMP and bovine cAMP-binding protein by liquid scintillation counting methodAntagonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-induced cAMP accumulation preincubated for 1 hr followed by NECA induction measured after 5 mins in presence of [3H]cAMP and bovine cAMP-binding protein by liquid scintillation counting method
ChEMBL 528 6 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)c1ccc(cc1)Cl 10.1021/acs.jmedchem.7b01627
5728 3216 None 35 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-induced cAMP accumulation preincubated for 1 hr followed by NECA induction measured after 5 mins in presence of [3H]cAMP and bovine cAMP-binding protein by liquid scintillation counting methodAntagonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-induced cAMP accumulation preincubated for 1 hr followed by NECA induction measured after 5 mins in presence of [3H]cAMP and bovine cAMP-binding protein by liquid scintillation counting method
ChEMBL 528 6 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)c1ccc(cc1)Cl 10.1021/acs.jmedchem.7b01627
CHEMBL483688 3216 None 35 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-induced cAMP accumulation preincubated for 1 hr followed by NECA induction measured after 5 mins in presence of [3H]cAMP and bovine cAMP-binding protein by liquid scintillation counting methodAntagonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-induced cAMP accumulation preincubated for 1 hr followed by NECA induction measured after 5 mins in presence of [3H]cAMP and bovine cAMP-binding protein by liquid scintillation counting method
ChEMBL 528 6 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)c1ccc(cc1)Cl 10.1021/acs.jmedchem.7b01627
136042335 71162 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 490 8 2 10 1.9 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc(=O)c5ccccc5[nH]4)nn3C)nc2n(CCC)c1=O 10.1021/jm201292w
CHEMBL1955911 71162 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 490 8 2 10 1.9 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc(=O)c5ccccc5[nH]4)nn3C)nc2n(CCC)c1=O 10.1021/jm201292w
11762982 26205 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Inhibitory activity against NECA stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptorInhibitory activity against NECA stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptor
ChEMBL 513 7 1 8 5.3 O=C(Cc1cccc2ccccc12)Nc1nc2nn(CCc3ccccc3)cc2c2nc(-c3ccco3)nn12 10.1021/jm030852k
CHEMBL135719 26205 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Inhibitory activity against NECA stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptorInhibitory activity against NECA stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptor
ChEMBL 513 7 1 8 5.3 O=C(Cc1cccc2ccccc12)Nc1nc2nn(CCc3ccccc3)cc2c2nc(-c3ccco3)nn12 10.1021/jm030852k
145960536 161628 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assayAntagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assay
ChEMBL 271 3 2 6 2.6 Cc1nc2c(N)nc(NCc3ccccc3)nc2s1 10.1016/j.bmc.2018.05.048
CHEMBL4130003 161628 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assayAntagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assay
ChEMBL 271 3 2 6 2.6 Cc1nc2c(N)nc(NCc3ccccc3)nc2s1 10.1016/j.bmc.2018.05.048
45482085 198105 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity
ChEMBL 421 7 1 9 3.8 CCCCn1cc2c(nc(NC(=O)Cc3cccs3)n3nc(-c4ccco4)nc23)n1 10.1016/j.bmc.2009.05.038
CHEMBL574489 198105 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity
ChEMBL 421 7 1 9 3.8 CCCCn1cc2c(nc(NC(=O)Cc3cccs3)n3nc(-c4ccco4)nc23)n1 10.1016/j.bmc.2009.05.038
135529391 481 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptorInhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor
ChEMBL 555 10 2 10 1.5 CCCn1c2=N/C(=c\3/cc([nH]n3C)NC(=O)Cc3ccc(cc3)OCc3ccccc3)/N=c2c(=O)n(c1=O)CCC 10.1021/jm0309654
438 481 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptorInhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor
ChEMBL 555 10 2 10 1.5 CCCn1c2=N/C(=c\3/cc([nH]n3C)NC(=O)Cc3ccc(cc3)OCc3ccccc3)/N=c2c(=O)n(c1=O)CCC 10.1021/jm0309654
CHEMBL285900 481 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptorInhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor
ChEMBL 555 10 2 10 1.5 CCCn1c2=N/C(=c\3/cc([nH]n3C)NC(=O)Cc3ccc(cc3)OCc3ccccc3)/N=c2c(=O)n(c1=O)CCC 10.1021/jm0309654
134157761 154029 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 289 5 2 7 3.1 CCCCNc1nc(N)c2nc(-c3ccco3)sc2n1 10.1021/acs.jmedchem.6b01068
CHEMBL3984266 154029 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 289 5 2 7 3.1 CCCCNc1nc(N)c2nc(-c3ccco3)sc2n1 10.1021/acs.jmedchem.6b01068
135874430 160130 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP levelsAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP levels
ChEMBL 517 8 2 8 3.8 CCCn1c(=O)c2[nH]c(-c3cc(C)n(CC(=O)Nc4ccc(Cl)c(Cl)c4)n3)nc2n(CCC)c1=O 10.1016/j.bmc.2007.11.058
CHEMBL410895 160130 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP levelsAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP levels
ChEMBL 517 8 2 8 3.8 CCCn1c(=O)c2[nH]c(-c3cc(C)n(CC(=O)Nc4ccc(Cl)c(Cl)c4)n3)nc2n(CCC)c1=O 10.1016/j.bmc.2007.11.058
25231168 5698 None 0 Human Functional pIC50 = 6.7 6.7 32 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 339 4 1 6 2.9 O=C(c1nc(NCc2cccnc2)nc2ccsc12)N1CCCC1 10.1016/j.bmcl.2009.08.040
CHEMBL1078030 5698 None 0 Human Functional pIC50 = 6.7 6.7 32 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 339 4 1 6 2.9 O=C(c1nc(NCc2cccnc2)nc2ccsc12)N1CCCC1 10.1016/j.bmcl.2009.08.040
49797856 10851 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 401 5 1 5 4.5 COc1ccc(N(C(C)=O)C(C)C)c2sc(NC(=O)c3ccc(F)cc3)nc12 10.1016/j.bmcl.2010.05.056
CHEMBL1172270 10851 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 401 5 1 5 4.5 COc1ccc(N(C(C)=O)C(C)C)c2sc(NC(=O)c3ccc(F)cc3)nc12 10.1016/j.bmcl.2010.05.056
49797771 10855 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 435 6 1 7 4.1 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(-n4ccnc4)cc3)sc12 10.1016/j.bmcl.2010.05.056
CHEMBL1172275 10855 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 435 6 1 7 4.1 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(-n4ccnc4)cc3)sc12 10.1016/j.bmcl.2010.05.056
49797773 10857 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 490 8 1 7 3.3 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(CN(C)S(C)(=O)=O)cc3)sc12 10.1016/j.bmcl.2010.05.056
CHEMBL1172277 10857 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 490 8 1 7 3.3 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(CN(C)S(C)(=O)=O)cc3)sc12 10.1016/j.bmcl.2010.05.056
46883106 5683 None 0 Human Functional pIC50 = 7.7 7.7 6 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 380 5 1 7 4.9 Cc1ccc(C(=O)c2nc(NC(C)c3ccccn3)nc3ccsc23)s1 10.1016/j.bmcl.2009.08.040
CHEMBL1077915 5683 None 0 Human Functional pIC50 = 7.7 7.7 6 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 380 5 1 7 4.9 Cc1ccc(C(=O)c2nc(NC(C)c3ccccn3)nc3ccsc23)s1 10.1016/j.bmcl.2009.08.040
25230948 6035 None 0 Human Functional pIC50 = 7.7 7.7 3 4
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 395 7 2 8 4.4 CCNc1cc2nc(NCc3cccnc3)nc(C(=O)c3cccs3)c2s1 10.1016/j.bmcl.2009.08.040
CHEMBL1080421 6035 None 0 Human Functional pIC50 = 7.7 7.7 3 4
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 395 7 2 8 4.4 CCNc1cc2nc(NCc3cccnc3)nc(C(=O)c3cccs3)c2s1 10.1016/j.bmcl.2009.08.040
54583134 63109 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Inhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 minsInhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 mins
ChEMBL 534 8 2 6 5.6 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)[C@@H]3CC[C@H](NCc4cccc(C(F)(F)F)c4)C3)sc12 10.1016/j.bmcl.2011.02.053
CHEMBL1760891 63109 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Inhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 minsInhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 mins
ChEMBL 534 8 2 6 5.6 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)[C@@H]3CC[C@H](NCc4cccc(C(F)(F)F)c4)C3)sc12 10.1016/j.bmcl.2011.02.053
CHEMBL1789250 63109 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Inhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 minsInhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 mins
ChEMBL 534 8 2 6 5.6 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)[C@@H]3CC[C@H](NCc4cccc(C(F)(F)F)c4)C3)sc12 10.1016/j.bmcl.2011.02.053
11080491 22796 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Inhibitory activity against NECA stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptorInhibitory activity against NECA stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptor
ChEMBL 429 7 1 8 4.0 CC(C)CCn1cc2c(nc(NC(=O)Cc3ccccc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm030852k
CHEMBL132806 22796 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Inhibitory activity against NECA stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptorInhibitory activity against NECA stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptor
ChEMBL 429 7 1 8 4.0 CC(C)CCn1cc2c(nc(NC(=O)Cc3ccccc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm030852k
10597086 208083 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Inhibition of 50 uM 5`-(N-ethylcarboxamido)adenosine induced cAMP production in CHO cell line expressing human Adenosine A2B receptor at 50 uMInhibition of 50 uM 5`-(N-ethylcarboxamido)adenosine induced cAMP production in CHO cell line expressing human Adenosine A2B receptor at 50 uM
ChEMBL 399 6 2 7 3.4 O=C(O)CCCC(=O)Nc1nc2ccc(Cl)cc2c2nc(-c3ccco3)nn12 10.1021/jm980094b
CHEMBL97753 208083 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Inhibition of 50 uM 5`-(N-ethylcarboxamido)adenosine induced cAMP production in CHO cell line expressing human Adenosine A2B receptor at 50 uMInhibition of 50 uM 5`-(N-ethylcarboxamido)adenosine induced cAMP production in CHO cell line expressing human Adenosine A2B receptor at 50 uM
ChEMBL 399 6 2 7 3.4 O=C(O)CCCC(=O)Nc1nc2ccc(Cl)cc2c2nc(-c3ccco3)nn12 10.1021/jm980094b
52948788 17730 None 0 Human Functional pIC50 = 4.7 4.7 -2137 2
Antagonist activity at adenosine A2B receptor by cAMP assayAntagonist activity at adenosine A2B receptor by cAMP assay
ChEMBL 489 5 2 6 6.3 Cc1ccccc1-n1nc(C(F)(F)F)c(-c2ccc3nccnc3c2)c1Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.07.095
CHEMBL1258622 17730 None 0 Human Functional pIC50 = 4.7 4.7 -2137 2
Antagonist activity at adenosine A2B receptor by cAMP assayAntagonist activity at adenosine A2B receptor by cAMP assay
ChEMBL 489 5 2 6 6.3 Cc1ccccc1-n1nc(C(F)(F)F)c(-c2ccc3nccnc3c2)c1Nc1ccccc1C(=O)O 10.1016/j.bmcl.2010.07.095
136042345 71171 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 585 8 2 9 4.9 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5c(C(F)(F)F)cc(C(F)(F)F)cc5[nH]4)no3)nc2n(CCC)c1=O 10.1021/jm201292w
CHEMBL1955921 71171 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 585 8 2 9 4.9 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5c(C(F)(F)F)cc(C(F)(F)F)cc5[nH]4)no3)nc2n(CCC)c1=O 10.1021/jm201292w
56964460 74723 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulationAntagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulation
ChEMBL 362 2 0 6 3.9 O=c1c(-c2ccco2)nnc2n(-c3ccc(Cl)cc3)c3ccccc3n12 10.1021/jm201177b
CHEMBL2030704 74723 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulationAntagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulation
ChEMBL 362 2 0 6 3.9 O=c1c(-c2ccco2)nnc2n(-c3ccc(Cl)cc3)c3ccccc3n12 10.1021/jm201177b
44186668 191510 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2
ChEMBL 562 6 2 7 2.6 CCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5cccc(C(F)(F)F)c5)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
CHEMBL519390 191510 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2
ChEMBL 562 6 2 7 2.6 CCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5cccc(C(F)(F)F)c5)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
56964459 74722 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulationAntagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulation
ChEMBL 372 2 0 5 4.4 O=c1c(-c2ccccc2)nnc2n(-c3ccc(Cl)cc3)c3ccccc3n12 10.1021/jm201177b
CHEMBL2030703 74722 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulationAntagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulation
ChEMBL 372 2 0 5 4.4 O=c1c(-c2ccccc2)nnc2n(-c3ccc(Cl)cc3)c3ccccc3n12 10.1021/jm201177b
56964461 74724 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulationAntagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulation
ChEMBL 366 4 0 5 4.0 O=c1c(-c2ccccc2)nnc2n(CCc3ccccc3)c3ccccc3n12 10.1021/jm201177b
CHEMBL2030705 74724 None 0 Human Functional pIC50 = 8.6 8.6 - 1
Antagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulationAntagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulation
ChEMBL 366 4 0 5 4.0 O=c1c(-c2ccccc2)nnc2n(CCc3ccccc3)c3ccccc3n12 10.1021/jm201177b
56924646 71172 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 332 5 2 7 0.4 CCCn1c(=O)c2[nH]c(-c3cc(=O)[nH]n3C)nc2n(CCC)c1=O 10.1021/jm201292w
CHEMBL1955922 71172 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 332 5 2 7 0.4 CCCn1c(=O)c2[nH]c(-c3cc(=O)[nH]n3C)nc2n(CCC)c1=O 10.1021/jm201292w
53242165 60736 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Inhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 minsInhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 mins
ChEMBL 584 6 1 7 5.2 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)N3CCC(S(=O)(=O)c4cccc(C(F)(F)F)c4)CC3)sc12 10.1016/j.bmcl.2011.02.053
CHEMBL1760901 60736 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Inhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 minsInhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 mins
ChEMBL 584 6 1 7 5.2 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)N3CCC(S(=O)(=O)c4cccc(C(F)(F)F)c4)CC3)sc12 10.1016/j.bmcl.2011.02.053
10539663 204232 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulationAntagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulation
ChEMBL 266 1 0 6 1.8 Cn1c2ccccc2n2c(=O)c(-c3ccco3)nnc12 10.1021/jm201177b
CHEMBL7098 204232 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulationAntagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulation
ChEMBL 266 1 0 6 1.8 Cn1c2ccccc2n2c(=O)c(-c3ccco3)nnc12 10.1021/jm201177b
135874421 168958 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP levelsAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP levels
ChEMBL 477 8 2 8 3.1 CCCn1c(=O)c2[nH]c(-c3cc(C)n(CC(=O)Nc4ccc(C)c(C)c4)n3)nc2n(CCC)c1=O 10.1016/j.bmc.2007.11.058
CHEMBL438938 168958 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP levelsAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP levels
ChEMBL 477 8 2 8 3.1 CCCn1c(=O)c2[nH]c(-c3cc(C)n(CC(=O)Nc4ccc(C)c(C)c4)n3)nc2n(CCC)c1=O 10.1016/j.bmc.2007.11.058
51050845 69263 None 0 Human Functional pIC50 = 4.7 4.7 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 374 6 3 10 1.7 CC(C)(C)OC(=O)NCCCNc1nc(N)n2nc(-c3ccco3)nc2n1 10.1021/jm101349u
CHEMBL1927428 69263 None 0 Human Functional pIC50 = 4.7 4.7 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 374 6 3 10 1.7 CC(C)(C)OC(=O)NCCCNc1nc(N)n2nc(-c3ccco3)nc2n1 10.1021/jm101349u
60155796 76966 None 0 Human Functional pIC50 = 5.7 5.7 -16 2
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production
ChEMBL 471 5 2 9 3.1 Cn1cc2c(nc(NC(=O)NC3CCN(Cc4ccccc4)CC3)n3nc(-c4ccco4)nc23)n1 10.1021/jm300323t
CHEMBL2070886 76966 None 0 Human Functional pIC50 = 5.7 5.7 -16 2
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production
ChEMBL 471 5 2 9 3.1 Cn1cc2c(nc(NC(=O)NC3CCN(Cc4ccccc4)CC3)n3nc(-c4ccco4)nc23)n1 10.1021/jm300323t
145962364 161448 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assayAntagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assay
ChEMBL 277 3 2 7 2.7 Cc1nc2c(N)nc(NCc3cccs3)nc2s1 10.1016/j.bmc.2018.05.048
CHEMBL4127395 161448 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assayAntagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assay
ChEMBL 277 3 2 7 2.7 Cc1nc2c(N)nc(NCc3cccs3)nc2s1 10.1016/j.bmc.2018.05.048
49797747 10619 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 482 6 1 7 3.4 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(C(=O)N4CCOCC4)cc3)sc12 10.1016/j.bmcl.2010.05.056
CHEMBL1170134 10619 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 482 6 1 7 3.4 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(C(=O)N4CCOCC4)cc3)sc12 10.1016/j.bmcl.2010.05.056
49797749 10621 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 435 6 1 7 4.1 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(-n4cccn4)cc3)sc12 10.1016/j.bmcl.2010.05.056
CHEMBL1170136 10621 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 435 6 1 7 4.1 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(-n4cccn4)cc3)sc12 10.1016/j.bmcl.2010.05.056
46911060 10648 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 373 5 1 7 2.7 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccnn3C)sc12 10.1016/j.bmcl.2010.05.056
CHEMBL1170367 10648 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 373 5 1 7 2.7 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccnn3C)sc12 10.1016/j.bmcl.2010.05.056
49798138 10671 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 426 6 2 6 3.3 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(C(=O)NC)cc3)sc12 10.1016/j.bmcl.2010.05.056
CHEMBL1170582 10671 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 426 6 2 6 3.3 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(C(=O)NC)cc3)sc12 10.1016/j.bmcl.2010.05.056
49797903 10741 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 359 5 2 6 2.7 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3cn[nH]c3)sc12 10.1016/j.bmcl.2010.05.056
CHEMBL1171162 10741 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 359 5 2 6 2.7 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3cn[nH]c3)sc12 10.1016/j.bmcl.2010.05.056
46911060 10648 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Inhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 minsInhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 mins
ChEMBL 373 5 1 7 2.7 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccnn3C)sc12 10.1016/j.bmcl.2011.02.053
CHEMBL1170367 10648 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Inhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 minsInhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 mins
ChEMBL 373 5 1 7 2.7 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccnn3C)sc12 10.1016/j.bmcl.2011.02.053
10994216 194919 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Inhibitory activity against NECA stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptorInhibitory activity against NECA stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptor
ChEMBL 463 7 1 8 4.2 O=C(Cc1ccccc1)Nc1nc2nn(CCc3ccccc3)cc2c2nc(-c3ccco3)nn12 10.1021/jm030852k
CHEMBL541455 194919 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Inhibitory activity against NECA stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptorInhibitory activity against NECA stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptor
ChEMBL 463 7 1 8 4.2 O=C(Cc1ccccc1)Nc1nc2nn(CCc3ccccc3)cc2c2nc(-c3ccco3)nn12 10.1021/jm030852k
1922 202818 None 44 Human Functional pIC50 = 6.7 6.7 -97 9
Inhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptorInhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptor
ChEMBL 256 1 1 5 0.6 Cn1c(=O)c2nc(-c3ccccc3)[nH]c2n(C)c1=O 10.1021/jm990499b
CHEMBL62350 202818 None 44 Human Functional pIC50 = 6.7 6.7 -97 9
Inhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptorInhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptor
ChEMBL 256 1 1 5 0.6 Cn1c(=O)c2nc(-c3ccccc3)[nH]c2n(C)c1=O 10.1021/jm990499b
135874431 96256 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP levelsAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP levels
ChEMBL 463 8 2 8 2.8 CCCn1c(=O)c2[nH]c(-c3cc(C)n(CC(=O)Nc4ccc(C)cc4)n3)nc2n(CCC)c1=O 10.1016/j.bmc.2007.11.058
CHEMBL261028 96256 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP levelsAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP levels
ChEMBL 463 8 2 8 2.8 CCCn1c(=O)c2[nH]c(-c3cc(C)n(CC(=O)Nc4ccc(C)cc4)n3)nc2n(CCC)c1=O 10.1016/j.bmc.2007.11.058
60154739 76988 None 0 Human Functional pIC50 = 5.7 5.7 -177 2
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production
ChEMBL 528 5 3 9 3.1 Cc1ccc(CNC(=O)N2CCC(NC(=O)Nc3nc4nn(C)cc4c4nc(-c5ccco5)nn34)CC2)cc1 10.1021/jm300323t
CHEMBL2071048 76988 None 0 Human Functional pIC50 = 5.7 5.7 -177 2
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production
ChEMBL 528 5 3 9 3.1 Cc1ccc(CNC(=O)N2CCC(NC(=O)Nc3nc4nn(C)cc4c4nc(-c5ccco5)nn34)CC2)cc1 10.1021/jm300323t
60154835 77199 None 0 Human Functional pIC50 = 5.7 5.7 -17 2
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production
ChEMBL 507 3 2 10 1.2 CN1CCN(C(=O)N2CCC(NC(=O)Nc3nc4nn(C)cc4c4nc(-c5ccco5)nn34)CC2)CC1 10.1021/jm300323t
CHEMBL2071051 77199 None 0 Human Functional pIC50 = 5.7 5.7 -17 2
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production
ChEMBL 507 3 2 10 1.2 CN1CCN(C(=O)N2CCC(NC(=O)Nc3nc4nn(C)cc4c4nc(-c5ccco5)nn34)CC2)CC1 10.1021/jm300323t
CHEMBL2079181 77199 None 0 Human Functional pIC50 = 5.7 5.7 -17 2
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production
ChEMBL 507 3 2 10 1.2 CN1CCN(C(=O)N2CCC(NC(=O)Nc3nc4nn(C)cc4c4nc(-c5ccco5)nn34)CC2)CC1 10.1021/jm300323t
46883159 5839 None 0 Human Functional pIC50 = 6.7 6.7 2 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 360 5 1 6 4.2 Cc1ccc(C(=O)c2nc(NCc3cccnc3)nc3ccsc23)cc1 10.1016/j.bmcl.2009.08.040
CHEMBL1079142 5839 None 0 Human Functional pIC50 = 6.7 6.7 2 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 360 5 1 6 4.2 Cc1ccc(C(=O)c2nc(NCc3cccnc3)nc3ccsc23)cc1 10.1016/j.bmcl.2009.08.040
136042337 71163 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 520 10 1 12 2.7 CCCn1c(=O)c2[nH]c(-c3cc(OCc4noc(-c5cccc(OC)c5)n4)nn3C)nc2n(CCC)c1=O 10.1021/jm201292w
CHEMBL1955913 71163 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 520 10 1 12 2.7 CCCn1c(=O)c2[nH]c(-c3cc(OCc4noc(-c5cccc(OC)c5)n4)nn3C)nc2n(CCC)c1=O 10.1021/jm201292w
136042330 71156 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 506 9 3 10 2.3 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5cc(C(=O)O)ccc5[nH]4)nn3C)nc2n(CCC)c1=O 10.1021/jm201292w
CHEMBL1955905 71156 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 506 9 3 10 2.3 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5cc(C(=O)O)ccc5[nH]4)nn3C)nc2n(CCC)c1=O 10.1021/jm201292w
10544916 188309 None 0 Rat Functional pIC50 = 6.7 6.7 -15 2
Inhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytesInhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytes
ChEMBL 337 1 2 7 2.3 Cn1c(-c2ccco2)nc2c(N)nc(C#CC3(O)CCCCC3)nc21 10.1021/jm990499b
CHEMBL50051 188309 None 0 Rat Functional pIC50 = 6.7 6.7 -15 2
Inhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytesInhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytes
ChEMBL 337 1 2 7 2.3 Cn1c(-c2ccco2)nc2c(N)nc(C#CC3(O)CCCCC3)nc21 10.1021/jm990499b
9839545 137312 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human A2B adenosine receptor expressed in CHO cell membranes assessed as inhibition of NECA stimulated adenylyl cyclase activityAntagonist activity at human A2B adenosine receptor expressed in CHO cell membranes assessed as inhibition of NECA stimulated adenylyl cyclase activity
ChEMBL 307 4 2 8 2.0 Nc1nc(NCc2ccccc2)nc2nc(-c3ccco3)nn12 10.1016/j.ejmech.2015.12.019
CHEMBL3752514 137312 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human A2B adenosine receptor expressed in CHO cell membranes assessed as inhibition of NECA stimulated adenylyl cyclase activityAntagonist activity at human A2B adenosine receptor expressed in CHO cell membranes assessed as inhibition of NECA stimulated adenylyl cyclase activity
ChEMBL 307 4 2 8 2.0 Nc1nc(NCc2ccccc2)nc2nc(-c3ccco3)nn12 10.1016/j.ejmech.2015.12.019
135874422 159085 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP levelsAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP levels
ChEMBL 509 10 2 10 2.5 CCCn1c(=O)c2[nH]c(-c3cc(C)n(CC(=O)Nc4ccc(OC)c(OC)c4)n3)nc2n(CCC)c1=O 10.1016/j.bmc.2007.11.058
CHEMBL409736 159085 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP levelsAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP levels
ChEMBL 509 10 2 10 2.5 CCCn1c(=O)c2[nH]c(-c3cc(C)n(CC(=O)Nc4ccc(OC)c(OC)c4)n3)nc2n(CCC)c1=O 10.1016/j.bmc.2007.11.058
49797796 10617 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 391 4 1 4 4.7 CCN(C(C)=O)c1ccc(Cl)c2nc(NC(=O)c3ccc(F)cc3)sc12 10.1016/j.bmcl.2010.05.056
CHEMBL1170130 10617 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 391 4 1 4 4.7 CCN(C(C)=O)c1ccc(Cl)c2nc(NC(=O)c3ccc(F)cc3)sc12 10.1016/j.bmcl.2010.05.056
49797878 10782 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 415 6 1 5 4.7 COc1ccc(N(CC(C)C)C(C)=O)c2sc(NC(=O)c3ccc(F)cc3)nc12 10.1016/j.bmcl.2010.05.056
CHEMBL1171718 10782 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 415 6 1 5 4.7 COc1ccc(N(CC(C)C)C(C)=O)c2sc(NC(=O)c3ccc(F)cc3)nc12 10.1016/j.bmcl.2010.05.056
9842054 183940 None 0 Human Functional pIC50 = 7.6 7.6 10 2
Inhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptorInhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptor
ChEMBL 365 1 2 6 2.8 Cn1c(-c2cccc(F)c2)nc2c(N)nc(C#CC3(O)CCCCC3)nc21 10.1021/jm990499b
CHEMBL48153 183940 None 0 Human Functional pIC50 = 7.6 7.6 10 2
Inhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptorInhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptor
ChEMBL 365 1 2 6 2.8 Cn1c(-c2cccc(F)c2)nc2c(N)nc(C#CC3(O)CCCCC3)nc21 10.1021/jm990499b
44186719 185916 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2
ChEMBL 552 7 2 9 1.7 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc6c(c5)OCO6)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
CHEMBL486893 185916 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2
ChEMBL 552 7 2 9 1.7 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc6c(c5)OCO6)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
49797854 10849 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 409 5 1 5 4.3 COc1ccc(N(C(C)=O)C(F)F)c2sc(NC(=O)c3ccc(F)cc3)nc12 10.1016/j.bmcl.2010.05.056
CHEMBL1172268 10849 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 409 5 1 5 4.3 COc1ccc(N(C(C)=O)C(F)F)c2sc(NC(=O)c3ccc(F)cc3)nc12 10.1016/j.bmcl.2010.05.056
136042348 71176 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 508 9 2 10 2.5 CCCn1c(=O)c2[nH]c(-c3cc(OCC(=O)Nc4ccc5c(c4)OCO5)nn3C)cc2n(CCC)c1=O 10.1021/jm201292w
CHEMBL1955926 71176 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 508 9 2 10 2.5 CCCn1c(=O)c2[nH]c(-c3cc(OCC(=O)Nc4ccc5c(c4)OCO5)nn3C)cc2n(CCC)c1=O 10.1021/jm201292w
145962202 161538 None 0 Human Functional pIC50 = 5.6 5.6 -64 3
Antagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assayAntagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assay
ChEMBL 363 5 2 7 4.0 COc1cccc(CNc2nc(N)c3nc(-c4ccccc4)sc3n2)c1 10.1016/j.bmc.2018.05.048
CHEMBL4128596 161538 None 0 Human Functional pIC50 = 5.6 5.6 -64 3
Antagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assayAntagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assay
ChEMBL 363 5 2 7 4.0 COc1cccc(CNc2nc(N)c3nc(-c4ccccc4)sc3n2)c1 10.1016/j.bmc.2018.05.048
156821341 186416 None 0 Human Functional pIC50 = 7.6 7.6 -2 2
Antagonist activity at human A2bR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assayAntagonist activity at human A2bR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assay
ChEMBL 461 4 2 9 2.5 Cn1cc(-c2c(-c3ccc(F)cc3)nc(N)n3nc([C@H](O)c4ncccc4F)nc23)ccc1=O 10.1021/acsmedchemlett.1c00620
CHEMBL4876080 186416 None 0 Human Functional pIC50 = 7.6 7.6 -2 2
Antagonist activity at human A2bR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assayAntagonist activity at human A2bR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assay
ChEMBL 461 4 2 9 2.5 Cn1cc(-c2c(-c3ccc(F)cc3)nc(N)n3nc([C@H](O)c4ncccc4F)nc23)ccc1=O 10.1021/acsmedchemlett.1c00620
134138275 147753 None 0 Human Functional pIC50 = 7.6 7.6 -1 2
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 339 4 3 8 3.2 Nc1nc(NCc2cccc(O)c2)nc2sc(-c3ccco3)nc12 10.1021/acs.jmedchem.6b01068
CHEMBL3932413 147753 None 0 Human Functional pIC50 = 7.6 7.6 -1 2
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 339 4 3 8 3.2 Nc1nc(NCc2cccc(O)c2)nc2sc(-c3ccco3)nc12 10.1021/acs.jmedchem.6b01068
60155712 76961 None 0 Human Functional pIC50 = 5.6 5.6 -9 2
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production
ChEMBL 381 3 3 9 1.1 Cn1cc2c(nc(NC(=O)NC3CCNCC3)n3nc(-c4ccco4)nc23)n1 10.1021/jm300323t
CHEMBL2070880 76961 None 0 Human Functional pIC50 = 5.6 5.6 -9 2
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production
ChEMBL 381 3 3 9 1.1 Cn1cc2c(nc(NC(=O)NC3CCNCC3)n3nc(-c4ccco4)nc23)n1 10.1021/jm300323t
11497239 11812 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Inhibition of NECA-stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptorInhibition of NECA-stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptor
ChEMBL 390 3 2 8 1.7 Cn1cc2c(nc(NC(=O)Nc3ccc[n+](C)c3)n3nc(-c4ccco4)nc23)n1 10.1021/jm051147+
CHEMBL1181982 11812 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Inhibition of NECA-stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptorInhibition of NECA-stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptor
ChEMBL 390 3 2 8 1.7 Cn1cc2c(nc(NC(=O)Nc3ccc[n+](C)c3)n3nc(-c4ccco4)nc23)n1 10.1021/jm051147+
CHEMBL203660 11812 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Inhibition of NECA-stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptorInhibition of NECA-stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptor
ChEMBL 390 3 2 8 1.7 Cn1cc2c(nc(NC(=O)Nc3ccc[n+](C)c3)n3nc(-c4ccco4)nc23)n1 10.1021/jm051147+
118708238 113368 None 0 Human Functional pIC50 = 6.6 6.6 -57 2
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP level by scintillation counting analysisAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP level by scintillation counting analysis
ChEMBL 345 5 2 6 3.3 Nc1nc(CCCc2ccccc2O)nc2cn(-c3ccccc3)nc12 10.1016/j.ejmech.2014.07.060
CHEMBL3317578 113368 None 0 Human Functional pIC50 = 6.6 6.6 -57 2
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP level by scintillation counting analysisAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP level by scintillation counting analysis
ChEMBL 345 5 2 6 3.3 Nc1nc(CCCc2ccccc2O)nc2cn(-c3ccccc3)nc12 10.1016/j.ejmech.2014.07.060
134142611 145885 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 353 5 3 8 3.3 Nc1nc(NCCc2cccc(O)c2)nc2sc(-c3ccco3)nc12 10.1021/acs.jmedchem.6b01068
CHEMBL3917647 145885 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 353 5 3 8 3.3 Nc1nc(NCCc2cccc(O)c2)nc2sc(-c3ccco3)nc12 10.1021/acs.jmedchem.6b01068
11625796 74701 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Inhibition of NECA-stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptorInhibition of NECA-stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptor
ChEMBL 414 3 2 9 3.7 Cn1cc2c(nc(NC(=O)Nc3cc4ccccc4o3)n3nc(-c4ccco4)nc23)n1 10.1021/jm051147+
CHEMBL203054 74701 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Inhibition of NECA-stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptorInhibition of NECA-stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptor
ChEMBL 414 3 2 9 3.7 Cn1cc2c(nc(NC(=O)Nc3cc4ccccc4o3)n3nc(-c4ccco4)nc23)n1 10.1021/jm051147+
11733496 24905 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Inhibitory activity against NECA stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptorInhibitory activity against NECA stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptor
ChEMBL 477 8 1 8 4.5 O=C(Cc1ccccc1)Nc1nc2nn(CCCc3ccccc3)cc2c2nc(-c3ccco3)nn12 10.1021/jm030852k
CHEMBL134566 24905 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Inhibitory activity against NECA stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptorInhibitory activity against NECA stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptor
ChEMBL 477 8 1 8 4.5 O=C(Cc1ccccc1)Nc1nc2nn(CCCc3ccccc3)cc2c2nc(-c3ccco3)nn12 10.1021/jm030852k
9842054 183940 None 0 Rat Functional pIC50 = 6.6 6.6 -10 2
Inhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytesInhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytes
ChEMBL 365 1 2 6 2.8 Cn1c(-c2cccc(F)c2)nc2c(N)nc(C#CC3(O)CCCCC3)nc21 10.1021/jm990499b
CHEMBL48153 183940 None 0 Rat Functional pIC50 = 6.6 6.6 -10 2
Inhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytesInhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytes
ChEMBL 365 1 2 6 2.8 Cn1c(-c2cccc(F)c2)nc2c(N)nc(C#CC3(O)CCCCC3)nc21 10.1021/jm990499b
57391653 69778 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assayAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assay
ChEMBL 358 5 1 7 3.6 Nc1nc2cn(CCCc3ccccc3)cc2c2nc(-c3ccco3)nn12 10.1016/j.bmc.2011.11.037
CHEMBL1935746 69778 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assayAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assay
ChEMBL 358 5 1 7 3.6 Nc1nc2cn(CCCc3ccccc3)cc2c2nc(-c3ccco3)nn12 10.1016/j.bmc.2011.11.037
25231169 5514 None 0 Human Functional pIC50 = 6.6 6.6 2 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 325 5 2 6 2.6 O=C(NC1CC1)c1nc(NCc2cccnc2)nc2ccsc12 10.1016/j.bmcl.2009.08.040
CHEMBL1076503 5514 None 0 Human Functional pIC50 = 6.6 6.6 2 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 325 5 2 6 2.6 O=C(NC1CC1)c1nc(NCc2cccnc2)nc2ccsc12 10.1016/j.bmcl.2009.08.040
136002248 71158 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 564 8 2 9 4.2 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5c(Cl)cc(C(F)(F)F)cc5[nH]4)nn3C)nc2n(CCC)c1=O 10.1021/jm201292w
CHEMBL1955907 71158 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 564 8 2 9 4.2 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5c(Cl)cc(C(F)(F)F)cc5[nH]4)nn3C)nc2n(CCC)c1=O 10.1021/jm201292w
54585057 60733 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Inhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 minsInhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 mins
ChEMBL 562 7 2 6 5.6 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)[C@H]3CC[C@@H](NC(=O)c4cccc(C(F)(F)F)c4)CC3)sc12 10.1016/j.bmcl.2011.02.053
CHEMBL1760898 60733 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Inhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 minsInhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 mins
ChEMBL 562 7 2 6 5.6 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)[C@H]3CC[C@@H](NC(=O)c4cccc(C(F)(F)F)c4)CC3)sc12 10.1016/j.bmcl.2011.02.053
11560202 74702 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Inhibition of NECA-stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptorInhibition of NECA-stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptor
ChEMBL 391 3 2 9 1.5 Cn1cc2c(nc(NC(=O)Nc3ccc[n+]([O-])c3)n3nc(-c4ccco4)nc23)n1 10.1021/jm051147+
CHEMBL203060 74702 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Inhibition of NECA-stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptorInhibition of NECA-stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptor
ChEMBL 391 3 2 9 1.5 Cn1cc2c(nc(NC(=O)Nc3ccc[n+]([O-])c3)n3nc(-c4ccco4)nc23)n1 10.1021/jm051147+
145977111 163765 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-induced cAMP accumulation preincubated for 1 hr followed by NECA induction measured after 5 mins in presence of [3H]cAMP and bovine cAMP-binding protein by liquid scintillation counting methodAntagonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-induced cAMP accumulation preincubated for 1 hr followed by NECA induction measured after 5 mins in presence of [3H]cAMP and bovine cAMP-binding protein by liquid scintillation counting method
ChEMBL 617 9 3 7 3.9 CCCn1c(=O)[nH]c2nc(-c3ccc(OCC(=O)NCCC4=C5C(C)=CC(C)=[N+]5[B-](F)(F)n5c(C)cc(C)c54)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.7b01627
CHEMBL4205635 163765 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-induced cAMP accumulation preincubated for 1 hr followed by NECA induction measured after 5 mins in presence of [3H]cAMP and bovine cAMP-binding protein by liquid scintillation counting methodAntagonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-induced cAMP accumulation preincubated for 1 hr followed by NECA induction measured after 5 mins in presence of [3H]cAMP and bovine cAMP-binding protein by liquid scintillation counting method
ChEMBL 617 9 3 7 3.9 CCCn1c(=O)[nH]c2nc(-c3ccc(OCC(=O)NCCC4=C5C(C)=CC(C)=[N+]5[B-](F)(F)n5c(C)cc(C)c54)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.7b01627
145962355 161436 None 0 Human Functional pIC50 = 5.6 5.6 -416 3
Antagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assayAntagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assay
ChEMBL 363 5 2 7 4.0 COc1ccccc1CNc1nc(N)c2nc(-c3ccccc3)sc2n1 10.1016/j.bmc.2018.05.048
CHEMBL4127213 161436 None 0 Human Functional pIC50 = 5.6 5.6 -416 3
Antagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assayAntagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assay
ChEMBL 363 5 2 7 4.0 COc1ccccc1CNc1nc(N)c2nc(-c3ccccc3)sc2n1 10.1016/j.bmc.2018.05.048
135874428 167562 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP levelsAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP levels
ChEMBL 479 9 2 9 2.5 CCCn1c(=O)c2[nH]c(-c3cc(C)n(CC(=O)Nc4cccc(OC)c4)n3)nc2n(CCC)c1=O 10.1016/j.bmc.2007.11.058
CHEMBL430044 167562 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP levelsAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP levels
ChEMBL 479 9 2 9 2.5 CCCn1c(=O)c2[nH]c(-c3cc(C)n(CC(=O)Nc4cccc(OC)c4)n3)nc2n(CCC)c1=O 10.1016/j.bmc.2007.11.058
57403905 69795 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assayAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assay
ChEMBL 345 4 1 8 2.6 Nc1nc2cn(CCc3ccccc3)nc2c2nc(-c3ccco3)nn12 10.1016/j.bmc.2011.11.037
CHEMBL1935762 69795 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assayAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assay
ChEMBL 345 4 1 8 2.6 Nc1nc2cn(CCc3ccccc3)nc2c2nc(-c3ccco3)nn12 10.1016/j.bmc.2011.11.037
136042346 71174 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 461 8 2 8 3.2 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5ccccc5[nH]4)nn3C)cc2n(CCC)c1=O 10.1021/jm201292w
CHEMBL1955924 71174 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 461 8 2 8 3.2 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5ccccc5[nH]4)nn3C)cc2n(CCC)c1=O 10.1021/jm201292w
46238064 8510 None 0 Human Functional pIC50 = 6.6 6.6 -5 2
Antagonist activity human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated [3H]cAMP accumulation treated 15 mins before NECA challenge measured after 30 mins by liquid scintillation spectrometryAntagonist activity human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated [3H]cAMP accumulation treated 15 mins before NECA challenge measured after 30 mins by liquid scintillation spectrometry
ChEMBL 405 5 1 5 4.8 O=C(Nc1nc(-c2ccccc2)nc2nn(Cc3ccccc3)cc12)c1ccccc1 10.1021/jm901785w
CHEMBL1094143 8510 None 0 Human Functional pIC50 = 6.6 6.6 -5 2
Antagonist activity human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated [3H]cAMP accumulation treated 15 mins before NECA challenge measured after 30 mins by liquid scintillation spectrometryAntagonist activity human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated [3H]cAMP accumulation treated 15 mins before NECA challenge measured after 30 mins by liquid scintillation spectrometry
ChEMBL 405 5 1 5 4.8 O=C(Nc1nc(-c2ccccc2)nc2nn(Cc3ccccc3)cc12)c1ccccc1 10.1021/jm901785w
145972655 163030 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 369 5 2 8 4.0 COc1cccc(CNc2nc(N)c3nc(-c4cccs4)sc3n2)c1 10.1016/j.ejmech.2018.06.020
CHEMBL4175878 163030 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 369 5 2 8 4.0 COc1cccc(CNc2nc(N)c3nc(-c4cccs4)sc3n2)c1 10.1016/j.ejmech.2018.06.020
49797794 10588 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 394 5 1 6 3.8 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(C#N)cc3)sc12 10.1016/j.bmcl.2010.05.056
CHEMBL1169934 10588 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 394 5 1 6 3.8 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(C#N)cc3)sc12 10.1016/j.bmcl.2010.05.056
49797750 10753 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 437 6 1 9 2.9 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(-n4cnnn4)cc3)sc12 10.1016/j.bmcl.2010.05.056
CHEMBL1171349 10753 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 437 6 1 9 2.9 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(-n4cnnn4)cc3)sc12 10.1016/j.bmcl.2010.05.056
49797772 10856 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 466 7 1 6 4.1 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(CN4CCCC4=O)cc3)sc12 10.1016/j.bmcl.2010.05.056
CHEMBL1172276 10856 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 466 7 1 6 4.1 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(CN4CCCC4=O)cc3)sc12 10.1016/j.bmcl.2010.05.056
156017813 177827 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Inhibition of human A2B receptor expressed in CHO cells assessed as reduction in cAMP productionInhibition of human A2B receptor expressed in CHO cells assessed as reduction in cAMP production
ChEMBL 402 5 3 9 2.2 Nc1nc(NCc2ccc(S(N)(=O)=O)cc2)nc2sc(-c3ccco3)nc12 10.1016/j.bmcl.2020.127067
CHEMBL4643898 177827 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Inhibition of human A2B receptor expressed in CHO cells assessed as reduction in cAMP productionInhibition of human A2B receptor expressed in CHO cells assessed as reduction in cAMP production
ChEMBL 402 5 3 9 2.2 Nc1nc(NCc2ccc(S(N)(=O)=O)cc2)nc2sc(-c3ccco3)nc12 10.1016/j.bmcl.2020.127067
54585057 60731 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Inhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 minsInhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 mins
ChEMBL 562 7 2 6 5.6 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)[C@H]3CC[C@H](NC(=O)c4cccc(C(F)(F)F)c4)CC3)sc12 10.1016/j.bmcl.2011.02.053
CHEMBL1760895 60731 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Inhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 minsInhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 mins
ChEMBL 562 7 2 6 5.6 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)[C@H]3CC[C@H](NC(=O)c4cccc(C(F)(F)F)c4)CC3)sc12 10.1016/j.bmcl.2011.02.053
11684980 12313 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Inhibition of NECA-stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptorInhibition of NECA-stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptor
ChEMBL 390 3 2 8 1.7 Cn1cc2c(nc(NC(=O)Nc3cccc[n+]3C)n3nc(-c4ccco4)nc23)n1 10.1021/jm051147+
CHEMBL1185010 12313 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Inhibition of NECA-stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptorInhibition of NECA-stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptor
ChEMBL 390 3 2 8 1.7 Cn1cc2c(nc(NC(=O)Nc3cccc[n+]3C)n3nc(-c4ccco4)nc23)n1 10.1021/jm051147+
CHEMBL383689 12313 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Inhibition of NECA-stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptorInhibition of NECA-stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptor
ChEMBL 390 3 2 8 1.7 Cn1cc2c(nc(NC(=O)Nc3cccc[n+]3C)n3nc(-c4ccco4)nc23)n1 10.1021/jm051147+
164611330 185084 None 0 Human Functional pIC50 = 6.6 6.6 -380 2
Antagonist activity at human A2bR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assayAntagonist activity at human A2bR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assay
ChEMBL 418 4 2 6 3.4 Nc1nc(-c2ccc(F)cc2)c(-c2ccc(=O)[nH]c2)c2nc(CCC(F)(F)F)nn12 10.1021/acsmedchemlett.1c00620
CHEMBL4855908 185084 None 0 Human Functional pIC50 = 6.6 6.6 -380 2
Antagonist activity at human A2bR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assayAntagonist activity at human A2bR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assay
ChEMBL 418 4 2 6 3.4 Nc1nc(-c2ccc(F)cc2)c(-c2ccc(=O)[nH]c2)c2nc(CCC(F)(F)F)nn12 10.1021/acsmedchemlett.1c00620
134138961 147624 None 0 Human Functional pIC50 = 6.6 6.6 -1 2
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 353 5 2 8 3.5 COc1ccc(CNc2nc(N)c3nc(-c4ccco4)sc3n2)cc1 10.1021/acs.jmedchem.6b01068
CHEMBL3931329 147624 None 0 Human Functional pIC50 = 6.6 6.6 -1 2
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 353 5 2 8 3.5 COc1ccc(CNc2nc(N)c3nc(-c4ccco4)sc3n2)cc1 10.1021/acs.jmedchem.6b01068
46883071 5693 None 0 Human Functional pIC50 = 6.5 6.5 -1 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 380 4 1 7 3.9 Cc1ccc(C(=O)c2nc(NC(=O)c3cccnc3)nc3ccsc23)s1 10.1016/j.bmcl.2009.08.040
CHEMBL1078001 5693 None 0 Human Functional pIC50 = 6.5 6.5 -1 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 380 4 1 7 3.9 Cc1ccc(C(=O)c2nc(NC(=O)c3cccnc3)nc3ccsc23)s1 10.1016/j.bmcl.2009.08.040
49797904 10742 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 373 5 1 7 2.7 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3cnn(C)c3)sc12 10.1016/j.bmcl.2010.05.056
CHEMBL1171163 10742 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 373 5 1 7 2.7 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3cnn(C)c3)sc12 10.1016/j.bmcl.2010.05.056
127046050 140091 None 0 Human Functional pIC50 = 6.5 6.5 -45 3
Antagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated cAMP level preincubated for 10 mins followed by NECA stimulation by scintillation counting method in presence of [3H]-cyclic AMPAntagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated cAMP level preincubated for 10 mins followed by NECA stimulation by scintillation counting method in presence of [3H]-cyclic AMP
ChEMBL 335 4 1 7 3.0 COc1cccc(Cn2cc3nc(-c4ccc(C)o4)nc(N)c3n2)c1 10.1016/j.bmc.2016.04.048
CHEMBL3800587 140091 None 0 Human Functional pIC50 = 6.5 6.5 -45 3
Antagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated cAMP level preincubated for 10 mins followed by NECA stimulation by scintillation counting method in presence of [3H]-cyclic AMPAntagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated cAMP level preincubated for 10 mins followed by NECA stimulation by scintillation counting method in presence of [3H]-cyclic AMP
ChEMBL 335 4 1 7 3.0 COc1cccc(Cn2cc3nc(-c4ccc(C)o4)nc(N)c3n2)c1 10.1016/j.bmc.2016.04.048
56964576 74726 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulationAntagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulation
ChEMBL 372 2 0 5 4.4 O=c1c(-c2ccccc2)nnc2n(-c3ccccc3)c3ccc(Cl)cc3n12 10.1021/jm201177b
CHEMBL2030707 74726 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulationAntagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulation
ChEMBL 372 2 0 5 4.4 O=c1c(-c2ccccc2)nnc2n(-c3ccccc3)c3ccc(Cl)cc3n12 10.1021/jm201177b
44186626 184609 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2
ChEMBL 526 7 2 7 2.1 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5cccc(F)c5)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
CHEMBL484900 184609 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2
ChEMBL 526 7 2 7 2.1 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5cccc(F)c5)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
25207803 5685 None 0 Human Functional pIC50 = 8.5 8.5 10 4
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 381 6 2 8 4.0 CNc1cc2nc(NCc3cccnc3)nc(C(=O)c3cccs3)c2s1 10.1016/j.bmcl.2009.08.040
CHEMBL1077943 5685 None 0 Human Functional pIC50 = 8.5 8.5 10 4
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 381 6 2 8 4.0 CNc1cc2nc(NCc3cccnc3)nc(C(=O)c3cccs3)c2s1 10.1016/j.bmcl.2009.08.040
44186669 185797 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2
ChEMBL 576 7 2 7 3.0 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5cccc(C(F)(F)F)c5)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
CHEMBL486688 185797 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2
ChEMBL 576 7 2 7 3.0 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5cccc(C(F)(F)F)c5)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
44186581 3205 None 27 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2
ChEMBL 542 7 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)Cc1ccc(cc1)Cl 10.1021/jm900413e
6561 3205 None 27 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2
ChEMBL 542 7 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)Cc1ccc(cc1)Cl 10.1021/jm900413e
CHEMBL482436 3205 None 27 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2
ChEMBL 542 7 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)Cc1ccc(cc1)Cl 10.1021/jm900413e
53248699 63103 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Inhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 minsInhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 mins
ChEMBL 548 8 2 6 6.0 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)[C@H]3CC[C@H](NCc4cccc(C(F)(F)F)c4)CC3)sc12 10.1016/j.bmcl.2011.02.053
CHEMBL1760897 63103 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Inhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 minsInhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 mins
ChEMBL 548 8 2 6 6.0 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)[C@H]3CC[C@H](NCc4cccc(C(F)(F)F)c4)CC3)sc12 10.1016/j.bmcl.2011.02.053
CHEMBL1789197 63103 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Inhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 minsInhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 mins
ChEMBL 548 8 2 6 6.0 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)[C@H]3CC[C@H](NCc4cccc(C(F)(F)F)c4)CC3)sc12 10.1016/j.bmcl.2011.02.053
4355631 193770 None 2 Human Functional pIC50 = 5.5 5.5 1 3
Inhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptorInhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptor
ChEMBL 320 2 0 6 2.2 COC(=O)C1=C2C=CN(C)C=C2c2nc(-c3ccccc3)nn2C1 10.1021/jm990499b
CHEMBL52735 193770 None 2 Human Functional pIC50 = 5.5 5.5 1 3
Inhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptorInhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptor
ChEMBL 320 2 0 6 2.2 COC(=O)C1=C2C=CN(C)C=C2c2nc(-c3ccccc3)nn2C1 10.1021/jm990499b
25230180 5958 None 0 Human Functional pIC50 = 5.5 5.5 2 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 353 4 1 6 3.5 C[C@@H](Nc1nc(C(=O)N2CCCC2)c2sccc2n1)c1cccnc1 10.1016/j.bmcl.2009.08.040
CHEMBL1079893 5958 None 0 Human Functional pIC50 = 5.5 5.5 2 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 353 4 1 6 3.5 C[C@@H](Nc1nc(C(=O)N2CCCC2)c2sccc2n1)c1cccnc1 10.1016/j.bmcl.2009.08.040
25231170 5515 None 0 Human Functional pIC50 = 6.5 6.5 8 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 327 5 2 6 2.8 CC(C)NC(=O)c1nc(NCc2cccnc2)nc2ccsc12 10.1016/j.bmcl.2009.08.040
CHEMBL1076504 5515 None 0 Human Functional pIC50 = 6.5 6.5 8 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 327 5 2 6 2.8 CC(C)NC(=O)c1nc(NCc2cccnc2)nc2ccsc12 10.1016/j.bmcl.2009.08.040
57396935 69785 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assayAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assay
ChEMBL 255 1 1 8 0.9 Cn1ncc2nc(N)n3nc(-c4ccco4)nc3c21 10.1016/j.bmc.2011.11.037
CHEMBL1935752 69785 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assayAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assay
ChEMBL 255 1 1 8 0.9 Cn1ncc2nc(N)n3nc(-c4ccco4)nc3c21 10.1016/j.bmc.2011.11.037
132991405 151063 None 3 Human Functional pIC50 = 6.5 6.5 -6165 2
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 353 5 2 8 3.5 COc1ccccc1CNc1nc(N)c2nc(-c3ccco3)sc2n1 10.1021/acs.jmedchem.6b01068
CHEMBL3958838 151063 None 3 Human Functional pIC50 = 6.5 6.5 -6165 2
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 353 5 2 8 3.5 COc1ccccc1CNc1nc(N)c2nc(-c3ccco3)sc2n1 10.1021/acs.jmedchem.6b01068
118708239 113369 None 0 Human Functional pIC50 = 6.5 6.5 -109 2
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP level by scintillation counting analysisAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP level by scintillation counting analysis
ChEMBL 345 5 2 6 3.3 Nc1nc(CCCc2cccc(O)c2)nc2cn(-c3ccccc3)nc12 10.1016/j.ejmech.2014.07.060
CHEMBL3317579 113369 None 0 Human Functional pIC50 = 6.5 6.5 -109 2
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP level by scintillation counting analysisAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP level by scintillation counting analysis
ChEMBL 345 5 2 6 3.3 Nc1nc(CCCc2cccc(O)c2)nc2cn(-c3ccccc3)nc12 10.1016/j.ejmech.2014.07.060
57391694 69787 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assayAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assay
ChEMBL 345 4 1 8 2.6 Nc1nc2cnn(CCc3ccccc3)c2c2nc(-c3ccco3)nn12 10.1016/j.bmc.2011.11.037
CHEMBL1935754 69787 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assayAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assay
ChEMBL 345 4 1 8 2.6 Nc1nc2cnn(CCc3ccccc3)c2c2nc(-c3ccco3)nn12 10.1016/j.bmc.2011.11.037
57403904 69790 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assayAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assay
ChEMBL 432 6 2 9 3.8 CCCn1ncc2nc(NC(=O)Nc3ccc(OC)cc3)n3nc(-c4ccco4)nc3c21 10.1016/j.bmc.2011.11.037
CHEMBL1935757 69790 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assayAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assay
ChEMBL 432 6 2 9 3.8 CCCn1ncc2nc(NC(=O)Nc3ccc(OC)cc3)n3nc(-c4ccco4)nc3c21 10.1016/j.bmc.2011.11.037
57398676 69796 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assayAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assay
ChEMBL 359 5 1 8 2.9 Nc1nc2cn(CCCc3ccccc3)nc2c2nc(-c3ccco3)nn12 10.1016/j.bmc.2011.11.037
CHEMBL1935763 69796 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assayAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assay
ChEMBL 359 5 1 8 2.9 Nc1nc2cn(CCCc3ccccc3)nc2c2nc(-c3ccco3)nn12 10.1016/j.bmc.2011.11.037
25230949 6005 None 0 Human Functional pIC50 = 7.5 7.5 15 4
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 367 5 2 8 3.6 Nc1cc2nc(NCc3cccnc3)nc(C(=O)c3cccs3)c2s1 10.1016/j.bmcl.2009.08.040
CHEMBL1080241 6005 None 0 Human Functional pIC50 = 7.5 7.5 15 4
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 367 5 2 8 3.6 Nc1cc2nc(NCc3cccnc3)nc(C(=O)c3cccs3)c2s1 10.1016/j.bmcl.2009.08.040
136042333 71160 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 514 8 2 9 3.4 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5cc(Cl)c(F)cc5[nH]4)nn3C)nc2n(CCC)c1=O 10.1021/jm201292w
CHEMBL1955909 71160 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 514 8 2 9 3.4 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5cc(Cl)c(F)cc5[nH]4)nn3C)nc2n(CCC)c1=O 10.1021/jm201292w
134147788 149991 None 0 Human Functional pIC50 = 7.5 7.5 -1 2
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 323 4 2 7 3.5 Nc1nc(NCc2ccccc2)nc2sc(-c3ccco3)nc12 10.1021/acs.jmedchem.6b01068
CHEMBL3950142 149991 None 0 Human Functional pIC50 = 7.5 7.5 -1 2
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 323 4 2 7 3.5 Nc1nc(NCc2ccccc2)nc2sc(-c3ccco3)nc12 10.1021/acs.jmedchem.6b01068
71601630 86922 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP production by scintillation counting methodAntagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP production by scintillation counting method
ChEMBL 225 1 1 5 1.7 Cc1nc(N)c2nn(-c3ccccc3)cc2n1 10.1016/j.ejmech.2015.11.015
CHEMBL2322916 86922 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP production by scintillation counting methodAntagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP production by scintillation counting method
ChEMBL 225 1 1 5 1.7 Cc1nc(N)c2nn(-c3ccccc3)cc2n1 10.1016/j.ejmech.2015.11.015
71601630 86922 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated cAMP level preincubated for 10 mins followed by NECA stimulation by scintillation counting method in presence of [3H]-cyclic AMPAntagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated cAMP level preincubated for 10 mins followed by NECA stimulation by scintillation counting method in presence of [3H]-cyclic AMP
ChEMBL 225 1 1 5 1.7 Cc1nc(N)c2nn(-c3ccccc3)cc2n1 10.1016/j.bmc.2016.04.048
CHEMBL2322916 86922 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated cAMP level preincubated for 10 mins followed by NECA stimulation by scintillation counting method in presence of [3H]-cyclic AMPAntagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated cAMP level preincubated for 10 mins followed by NECA stimulation by scintillation counting method in presence of [3H]-cyclic AMP
ChEMBL 225 1 1 5 1.7 Cc1nc(N)c2nn(-c3ccccc3)cc2n1 10.1016/j.bmc.2016.04.048
71601630 86922 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP level by scintillation counting analysisAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP level by scintillation counting analysis
ChEMBL 225 1 1 5 1.7 Cc1nc(N)c2nn(-c3ccccc3)cc2n1 10.1016/j.ejmech.2014.07.060
CHEMBL2322916 86922 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP level by scintillation counting analysisAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP level by scintillation counting analysis
ChEMBL 225 1 1 5 1.7 Cc1nc(N)c2nn(-c3ccccc3)cc2n1 10.1016/j.ejmech.2014.07.060
44408316 75405 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Inhibition of NECA-stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptorInhibition of NECA-stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptor
ChEMBL 391 3 2 9 1.5 Cn1cc2c(nc(NC(=O)Nc3cccc[n+]3[O-])n3nc(-c4ccco4)nc23)n1 10.1021/jm051147+
CHEMBL203998 75405 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Inhibition of NECA-stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptorInhibition of NECA-stimulated cAMP accumulation in CHO cells expressing human adenosine A2B receptor
ChEMBL 391 3 2 9 1.5 Cn1cc2c(nc(NC(=O)Nc3cccc[n+]3[O-])n3nc(-c4ccco4)nc23)n1 10.1021/jm051147+
10687707 110357 None 0 Human Functional pIC50 = 5.5 5.5 - 1
Antagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulationAntagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulation
ChEMBL 328 2 0 6 3.3 O=c1c(-c2ccco2)nnc2n(-c3ccccc3)c3ccccc3n12 10.1021/jm201177b
CHEMBL324100 110357 None 0 Human Functional pIC50 = 5.5 5.5 - 1
Antagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulationAntagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulation
ChEMBL 328 2 0 6 3.3 O=c1c(-c2ccco2)nnc2n(-c3ccccc3)c3ccccc3n12 10.1021/jm201177b
11716665 2281 None 37 Human Functional pIC50 = 6.5 6.5 1 2
Activity at human A2B receptor expressed in HEK293 cells assessed as inhibition of NECA-induced intracellular cAMP levels by ELISAActivity at human A2B receptor expressed in HEK293 cells assessed as inhibition of NECA-induced intracellular cAMP levels by ELISA
ChEMBL 316 4 1 7 3.3 n1ccc(nc1)c1cnc(nc1c1ccco1)Nc1cccnc1 10.1021/jm061333v
5617 2281 None 37 Human Functional pIC50 = 6.5 6.5 1 2
Activity at human A2B receptor expressed in HEK293 cells assessed as inhibition of NECA-induced intracellular cAMP levels by ELISAActivity at human A2B receptor expressed in HEK293 cells assessed as inhibition of NECA-induced intracellular cAMP levels by ELISA
ChEMBL 316 4 1 7 3.3 n1ccc(nc1)c1cnc(nc1c1ccco1)Nc1cccnc1 10.1021/jm061333v
CHEMBL375293 2281 None 37 Human Functional pIC50 = 6.5 6.5 1 2
Activity at human A2B receptor expressed in HEK293 cells assessed as inhibition of NECA-induced intracellular cAMP levels by ELISAActivity at human A2B receptor expressed in HEK293 cells assessed as inhibition of NECA-induced intracellular cAMP levels by ELISA
ChEMBL 316 4 1 7 3.3 n1ccc(nc1)c1cnc(nc1c1ccco1)Nc1cccnc1 10.1021/jm061333v
135522362 100021 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptorInhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor
ChEMBL 472 8 1 10 0.3 CCCn1c(=O)c2nc(-c3cc(OCC(=O)N4CCN(C)CC4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
CHEMBL286838 100021 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptorInhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor
ChEMBL 472 8 1 10 0.3 CCCn1c(=O)c2nc(-c3cc(OCC(=O)N4CCN(C)CC4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
134151346 151571 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 275 4 2 7 2.8 CCCNc1nc(N)c2nc(-c3ccco3)sc2n1 10.1021/acs.jmedchem.6b01068
CHEMBL3963278 151571 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 275 4 2 7 2.8 CCCNc1nc(N)c2nc(-c3ccco3)sc2n1 10.1021/acs.jmedchem.6b01068
60154742 77171 None 0 Human Functional pIC50 = 5.5 5.5 -39 2
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production
ChEMBL 501 4 3 10 2.5 Cn1cc2c(nc(NC(=O)NC3CCN(C(=O)Nc4ccncc4)CC3)n3nc(-c4ccco4)nc23)n1 10.1021/jm300323t
CHEMBL2071050 77171 None 0 Human Functional pIC50 = 5.5 5.5 -39 2
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production
ChEMBL 501 4 3 10 2.5 Cn1cc2c(nc(NC(=O)NC3CCN(C(=O)Nc4ccncc4)CC3)n3nc(-c4ccco4)nc23)n1 10.1021/jm300323t
CHEMBL2078766 77171 None 0 Human Functional pIC50 = 5.5 5.5 -39 2
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production
ChEMBL 501 4 3 10 2.5 Cn1cc2c(nc(NC(=O)NC3CCN(C(=O)Nc4ccncc4)CC3)n3nc(-c4ccco4)nc23)n1 10.1021/jm300323t
60154740 76989 None 0 Human Functional pIC50 = 5.5 5.5 -95 2
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production
ChEMBL 544 6 3 10 2.8 COc1ccc(CNC(=O)N2CCC(NC(=O)Nc3nc4nn(C)cc4c4nc(-c5ccco5)nn34)CC2)cc1 10.1021/jm300323t
CHEMBL2071049 76989 None 0 Human Functional pIC50 = 5.5 5.5 -95 2
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production
ChEMBL 544 6 3 10 2.8 COc1ccc(CNC(=O)N2CCC(NC(=O)Nc3nc4nn(C)cc4c4nc(-c5ccco5)nn34)CC2)cc1 10.1021/jm300323t
57402161 69793 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assayAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assay
ChEMBL 255 1 1 8 0.9 Cn1cc2nc(N)n3nc(-c4ccco4)nc3c2n1 10.1016/j.bmc.2011.11.037
CHEMBL1935760 69793 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assayAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assay
ChEMBL 255 1 1 8 0.9 Cn1cc2nc(N)n3nc(-c4ccco4)nc3c2n1 10.1016/j.bmc.2011.11.037
10126989 10766 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 417 7 1 6 3.7 COCCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(F)cc3)sc12 10.1016/j.bmcl.2010.05.056
CHEMBL1171526 10766 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 417 7 1 6 3.7 COCCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(F)cc3)sc12 10.1016/j.bmcl.2010.05.056
145971923 163018 None 0 Human Functional pIC50 = 7.5 7.5 -1 2
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 324 4 2 8 2.9 Nc1nc(NCc2ccncc2)nc2sc(-c3ccco3)nc12 10.1016/j.ejmech.2018.06.020
CHEMBL4175676 163018 None 0 Human Functional pIC50 = 7.5 7.5 -1 2
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 324 4 2 8 2.9 Nc1nc(NCc2ccncc2)nc2sc(-c3ccco3)nc12 10.1016/j.ejmech.2018.06.020
118708236 113366 None 0 Human Functional pIC50 = 6.5 6.5 -138 2
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP level by scintillation counting analysisAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP level by scintillation counting analysis
ChEMBL 359 6 1 6 3.6 COc1cccc(CCCc2nc(N)c3nn(-c4ccccc4)cc3n2)c1 10.1016/j.ejmech.2014.07.060
CHEMBL3317576 113366 None 0 Human Functional pIC50 = 6.5 6.5 -138 2
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP level by scintillation counting analysisAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP level by scintillation counting analysis
ChEMBL 359 6 1 6 3.6 COc1cccc(CCCc2nc(N)c3nn(-c4ccccc4)cc3n2)c1 10.1016/j.ejmech.2014.07.060
156017042 177758 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Inverse agonist activity at human A2B receptor expressed in CHO cells assessed as reduction in cAMP levelInverse agonist activity at human A2B receptor expressed in CHO cells assessed as reduction in cAMP level
ChEMBL 450 5 1 10 3.4 CCOC(=O)c1ccc(N2CCN(c3nc(N)c4nc(-c5ccco5)sc4n3)CC2)cc1 10.1016/j.bmcl.2020.127067
CHEMBL4642713 177758 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Inverse agonist activity at human A2B receptor expressed in CHO cells assessed as reduction in cAMP levelInverse agonist activity at human A2B receptor expressed in CHO cells assessed as reduction in cAMP level
ChEMBL 450 5 1 10 3.4 CCOC(=O)c1ccc(N2CCN(c3nc(N)c4nc(-c5ccco5)sc4n3)CC2)cc1 10.1016/j.bmcl.2020.127067
156010442 177043 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Inhibition of human A2B receptor expressed in CHO cells assessed as reduction in cAMP productionInhibition of human A2B receptor expressed in CHO cells assessed as reduction in cAMP production
ChEMBL 416 6 3 9 2.2 Nc1nc(NCCc2ccc(S(N)(=O)=O)cc2)nc2sc(-c3ccco3)nc12 10.1016/j.bmcl.2020.127067
CHEMBL4632532 177043 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Inhibition of human A2B receptor expressed in CHO cells assessed as reduction in cAMP productionInhibition of human A2B receptor expressed in CHO cells assessed as reduction in cAMP production
ChEMBL 416 6 3 9 2.2 Nc1nc(NCCc2ccc(S(N)(=O)=O)cc2)nc2sc(-c3ccco3)nc12 10.1016/j.bmcl.2020.127067
11716665 2281 None 37 Mouse Functional pIC50 = 6.5 6.5 -1 2
Activity at mouse A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced intracellular cAMP levels by ELISAActivity at mouse A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced intracellular cAMP levels by ELISA
ChEMBL 316 4 1 7 3.3 n1ccc(nc1)c1cnc(nc1c1ccco1)Nc1cccnc1 10.1021/jm061333v
5617 2281 None 37 Mouse Functional pIC50 = 6.5 6.5 -1 2
Activity at mouse A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced intracellular cAMP levels by ELISAActivity at mouse A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced intracellular cAMP levels by ELISA
ChEMBL 316 4 1 7 3.3 n1ccc(nc1)c1cnc(nc1c1ccco1)Nc1cccnc1 10.1021/jm061333v
CHEMBL375293 2281 None 37 Mouse Functional pIC50 = 6.5 6.5 -1 2
Activity at mouse A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced intracellular cAMP levels by ELISAActivity at mouse A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced intracellular cAMP levels by ELISA
ChEMBL 316 4 1 7 3.3 n1ccc(nc1)c1cnc(nc1c1ccco1)Nc1cccnc1 10.1021/jm061333v
49797793 10854 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 427 6 1 7 3.7 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(C(=O)OC)cc3)sc12 10.1016/j.bmcl.2010.05.056
CHEMBL1172274 10854 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 427 6 1 7 3.7 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(C(=O)OC)cc3)sc12 10.1016/j.bmcl.2010.05.056
136042329 71155 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 534 10 2 11 2.7 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5cc(C(=O)OCC)ccc5[nH]4)nn3C)nc2n(CCC)c1=O 10.1021/jm201292w
CHEMBL1955904 71155 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 534 10 2 11 2.7 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5cc(C(=O)OCC)ccc5[nH]4)nn3C)nc2n(CCC)c1=O 10.1021/jm201292w
22283414 10663 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 359 4 2 5 3.7 COc1ccc(NC(C)=O)c2sc(NC(=O)c3ccc(F)cc3)nc12 10.1016/j.bmcl.2010.05.056
CHEMBL1170518 10663 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 359 4 2 5 3.7 COc1ccc(NC(C)=O)c2sc(NC(=O)c3ccc(F)cc3)nc12 10.1016/j.bmcl.2010.05.056
49797825 10666 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 430 6 2 6 2.8 CNC(=O)CN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(F)cc3)sc12 10.1016/j.bmcl.2010.05.056
CHEMBL1170525 10666 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 430 6 2 6 2.8 CNC(=O)CN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(F)cc3)sc12 10.1016/j.bmcl.2010.05.056
22283414 10663 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Inhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 minsInhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 mins
ChEMBL 359 4 2 5 3.7 COc1ccc(NC(C)=O)c2sc(NC(=O)c3ccc(F)cc3)nc12 10.1016/j.bmcl.2011.02.053
CHEMBL1170518 10663 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Inhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 minsInhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 mins
ChEMBL 359 4 2 5 3.7 COc1ccc(NC(C)=O)c2sc(NC(=O)c3ccc(F)cc3)nc12 10.1016/j.bmcl.2011.02.053
145961997 161555 None 0 Human Functional pIC50 = 5.5 5.5 - 1
Antagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assayAntagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assay
ChEMBL 301 4 2 7 2.6 COc1cccc(CNc2nc(N)c3nc(C)sc3n2)c1 10.1016/j.bmc.2018.05.048
CHEMBL4128787 161555 None 0 Human Functional pIC50 = 5.5 5.5 - 1
Antagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assayAntagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assay
ChEMBL 301 4 2 7 2.6 COc1cccc(CNc2nc(N)c3nc(C)sc3n2)c1 10.1016/j.bmc.2018.05.048
127045699 139635 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated cAMP level preincubated for 10 mins followed by NECA stimulation by scintillation counting method in presence of [3H]-cyclic AMPAntagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated cAMP level preincubated for 10 mins followed by NECA stimulation by scintillation counting method in presence of [3H]-cyclic AMP
ChEMBL 323 3 1 6 3.2 Cc1ccc(-c2nc(N)c3nn(Cc4ccccc4F)cc3n2)o1 10.1016/j.bmc.2016.04.048
CHEMBL3797666 139635 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated cAMP level preincubated for 10 mins followed by NECA stimulation by scintillation counting method in presence of [3H]-cyclic AMPAntagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated cAMP level preincubated for 10 mins followed by NECA stimulation by scintillation counting method in presence of [3H]-cyclic AMP
ChEMBL 323 3 1 6 3.2 Cc1ccc(-c2nc(N)c3nn(Cc4ccccc4F)cc3n2)o1 10.1016/j.bmc.2016.04.048
145963230 161507 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assayAntagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assay
ChEMBL 333 4 2 6 3.9 Nc1nc(NCc2ccccc2)nc2sc(-c3ccccc3)nc12 10.1016/j.bmc.2018.05.048
CHEMBL4128138 161507 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assayAntagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assay
ChEMBL 333 4 2 6 3.9 Nc1nc(NCc2ccccc2)nc2sc(-c3ccccc3)nc12 10.1016/j.bmc.2018.05.048
49797795 10616 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 447 6 1 7 3.3 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(S(C)(=O)=O)cc3)sc12 10.1016/j.bmcl.2010.05.056
CHEMBL1170129 10616 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 447 6 1 7 3.3 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(S(C)(=O)=O)cc3)sc12 10.1016/j.bmcl.2010.05.056
25230951 150299 None 0 Human Functional pIC50 = 7.4 7.4 5 4
Fluorometric Imaging Plate Reader (FLIPR) Asssay: The use of a Fluorometric Imaging Plate Reader (FLIPR) to measure calcium flux in Adenosine-receptor expressing cells is a well-established technique. In this assay calcium flux is triggered by receptor activation and measured through the fluorescence of an incorporated calcium-sensitive dye. The potencies shown were determined using expressed human adenosine A2B receptors in mammalian cell lines. Selectivity values were obtained by using mammalian cell lines expressing the human adenosine A1, A2A and A3 receptors.Fluorometric Imaging Plate Reader (FLIPR) Asssay: The use of a Fluorometric Imaging Plate Reader (FLIPR) to measure calcium flux in Adenosine-receptor expressing cells is a well-established technique. In this assay calcium flux is triggered by receptor activation and measured through the fluorescence of an incorporated calcium-sensitive dye. The potencies shown were determined using expressed human adenosine A2B receptors in mammalian cell lines. Selectivity values were obtained by using mammalian cell lines expressing the human adenosine A1, A2A and A3 receptors.
ChEMBL 380 6 1 7 4.6 CCc1cc2nc(NCc3cccnc3)nc(C(=O)c3cccs3)c2s1 nan
CHEMBL3952824 150299 None 0 Human Functional pIC50 = 7.4 7.4 5 4
Fluorometric Imaging Plate Reader (FLIPR) Asssay: The use of a Fluorometric Imaging Plate Reader (FLIPR) to measure calcium flux in Adenosine-receptor expressing cells is a well-established technique. In this assay calcium flux is triggered by receptor activation and measured through the fluorescence of an incorporated calcium-sensitive dye. The potencies shown were determined using expressed human adenosine A2B receptors in mammalian cell lines. Selectivity values were obtained by using mammalian cell lines expressing the human adenosine A1, A2A and A3 receptors.Fluorometric Imaging Plate Reader (FLIPR) Asssay: The use of a Fluorometric Imaging Plate Reader (FLIPR) to measure calcium flux in Adenosine-receptor expressing cells is a well-established technique. In this assay calcium flux is triggered by receptor activation and measured through the fluorescence of an incorporated calcium-sensitive dye. The potencies shown were determined using expressed human adenosine A2B receptors in mammalian cell lines. Selectivity values were obtained by using mammalian cell lines expressing the human adenosine A1, A2A and A3 receptors.
ChEMBL 380 6 1 7 4.6 CCc1cc2nc(NCc3cccnc3)nc(C(=O)c3cccs3)c2s1 nan
45481750 198564 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity
ChEMBL 449 5 1 8 4.0 Cn1cc2c(nc(NC(=O)C(c3ccccc3)c3ccccc3)n3nc(-c4ccco4)nc23)n1 10.1016/j.bmc.2009.05.038
CHEMBL578224 198564 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity
ChEMBL 449 5 1 8 4.0 Cn1cc2c(nc(NC(=O)C(c3ccccc3)c3ccccc3)n3nc(-c4ccco4)nc23)n1 10.1016/j.bmc.2009.05.038
46882996 5639 None 0 Human Functional pIC50 = 5.4 5.4 1 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 288 3 0 5 3.9 CCc1nc(C(=O)c2ccc(C)s2)c2sccc2n1 10.1016/j.bmcl.2009.08.040
CHEMBL1077750 5639 None 0 Human Functional pIC50 = 5.4 5.4 1 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 288 3 0 5 3.9 CCc1nc(C(=O)c2ccc(C)s2)c2sccc2n1 10.1016/j.bmcl.2009.08.040
49797774 10622 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 462 7 2 7 3.3 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(NS(C)(=O)=O)cc3)sc12 10.1016/j.bmcl.2010.05.056
CHEMBL1170137 10622 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 462 7 2 7 3.3 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(NS(C)(=O)=O)cc3)sc12 10.1016/j.bmcl.2010.05.056
145961339 161565 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assayAntagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assay
ChEMBL 257 2 2 6 2.7 Cc1nc2c(N)nc(Nc3ccccc3)nc2s1 10.1016/j.bmc.2018.05.048
CHEMBL4128862 161565 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assayAntagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assay
ChEMBL 257 2 2 6 2.7 Cc1nc2c(N)nc(Nc3ccccc3)nc2s1 10.1016/j.bmc.2018.05.048
49798139 10672 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 495 6 1 7 3.3 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(C(=O)N4CCN(C)CC4)cc3)sc12 10.1016/j.bmcl.2010.05.056
CHEMBL1170583 10672 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 495 6 1 7 3.3 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(C(=O)N4CCN(C)CC4)cc3)sc12 10.1016/j.bmcl.2010.05.056
135484064 2616 None 4 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 509 9 2 11 1.9 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)Nc1ccc2c(c1)OCO2 10.1021/jm201292w
390 2616 None 4 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 509 9 2 11 1.9 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)Nc1ccc2c(c1)OCO2 10.1021/jm201292w
CHEMBL260331 2616 None 4 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 509 9 2 11 1.9 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)Nc1ccc2c(c1)OCO2 10.1021/jm201292w
136042353 71153 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 530 8 2 9 3.6 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5cc(C(F)(F)F)ccc5[nH]4)nn3C)nc2n(CCC)c1=O 10.1021/jm201292w
CHEMBL1955902 71153 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 530 8 2 9 3.6 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5cc(C(F)(F)F)ccc5[nH]4)nn3C)nc2n(CCC)c1=O 10.1021/jm201292w
135484064 2616 None 4 Human Functional pIC50 = 7.4 7.4 - 1
Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptorInhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor
ChEMBL 509 9 2 11 1.9 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)Nc1ccc2c(c1)OCO2 10.1021/jm0309654
390 2616 None 4 Human Functional pIC50 = 7.4 7.4 - 1
Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptorInhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor
ChEMBL 509 9 2 11 1.9 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)Nc1ccc2c(c1)OCO2 10.1021/jm0309654
CHEMBL260331 2616 None 4 Human Functional pIC50 = 7.4 7.4 - 1
Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptorInhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor
ChEMBL 509 9 2 11 1.9 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)Nc1ccc2c(c1)OCO2 10.1021/jm0309654
118708235 113365 None 0 Human Functional pIC50 = 6.4 6.4 -32 2
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP level by scintillation counting analysisAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP level by scintillation counting analysis
ChEMBL 359 6 1 6 3.6 COc1ccccc1CCCc1nc(N)c2nn(-c3ccccc3)cc2n1 10.1016/j.ejmech.2014.07.060
CHEMBL3317575 113365 None 0 Human Functional pIC50 = 6.4 6.4 -32 2
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP level by scintillation counting analysisAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP level by scintillation counting analysis
ChEMBL 359 6 1 6 3.6 COc1ccccc1CCCc1nc(N)c2nn(-c3ccccc3)cc2n1 10.1016/j.ejmech.2014.07.060
134149255 148164 None 0 Human Functional pIC50 = 6.4 6.4 -16 2
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 337 5 2 7 3.6 Nc1nc(NCCc2ccccc2)nc2sc(-c3ccco3)nc12 10.1021/acs.jmedchem.6b01068
CHEMBL3935610 148164 None 0 Human Functional pIC50 = 6.4 6.4 -16 2
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 337 5 2 7 3.6 Nc1nc(NCCc2ccccc2)nc2sc(-c3ccco3)nc12 10.1021/acs.jmedchem.6b01068
145954398 162595 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 367 5 2 8 3.9 COc1ccccc1CNc1nc(N)c2nc(-c3ccc(C)o3)sc2n1 10.1016/j.ejmech.2018.06.020
CHEMBL4168980 162595 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 367 5 2 8 3.9 COc1ccccc1CNc1nc(N)c2nc(-c3ccc(C)o3)sc2n1 10.1016/j.ejmech.2018.06.020
25230881 6177 None 0 Human Functional pIC50 = 7.4 7.4 1 4
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 395 6 1 8 4.1 CN(C)c1cc2nc(NCc3cccnc3)nc(C(=O)c3cccs3)c2s1 10.1016/j.bmcl.2009.08.040
CHEMBL1081160 6177 None 0 Human Functional pIC50 = 7.4 7.4 1 4
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 395 6 1 8 4.1 CN(C)c1cc2nc(NCc3cccnc3)nc(C(=O)c3cccs3)c2s1 10.1016/j.bmcl.2009.08.040
127045909 139988 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated cAMP level preincubated for 10 mins followed by NECA stimulation by scintillation counting method in presence of [3H]-cyclic AMPAntagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated cAMP level preincubated for 10 mins followed by NECA stimulation by scintillation counting method in presence of [3H]-cyclic AMP
ChEMBL 321 3 2 7 2.7 Cc1ccc(-c2nc(N)c3nn(Cc4ccccc4O)cc3n2)o1 10.1016/j.bmc.2016.04.048
CHEMBL3799921 139988 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated cAMP level preincubated for 10 mins followed by NECA stimulation by scintillation counting method in presence of [3H]-cyclic AMPAntagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated cAMP level preincubated for 10 mins followed by NECA stimulation by scintillation counting method in presence of [3H]-cyclic AMP
ChEMBL 321 3 2 7 2.7 Cc1ccc(-c2nc(N)c3nn(Cc4ccccc4O)cc3n2)o1 10.1016/j.bmc.2016.04.048
156821369 185623 None 2 Human Functional pIC50 = 8.4 8.4 -14 2
Antagonist activity at human A2bR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assayAntagonist activity at human A2bR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assay
ChEMBL 447 4 2 7 3.5 Nc1nc(-c2ccccc2)c(-c2ccc(=O)[nH]c2)c2nc(Cc3ncc(F)cc3Cl)nn12 10.1021/acsmedchemlett.1c00620
CHEMBL4864129 185623 None 2 Human Functional pIC50 = 8.4 8.4 -14 2
Antagonist activity at human A2bR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assayAntagonist activity at human A2bR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assay
ChEMBL 447 4 2 7 3.5 Nc1nc(-c2ccccc2)c(-c2ccc(=O)[nH]c2)c2nc(Cc3ncc(F)cc3Cl)nn12 10.1021/acsmedchemlett.1c00620
145436763 162197 None 0 Human Functional pIC50 = 8.4 8.4 -13 2
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 338 5 2 8 3.0 Nc1nc(NCCc2cccnc2)nc2sc(-c3ccco3)nc12 10.1016/j.ejmech.2018.06.020
CHEMBL4162638 162197 None 0 Human Functional pIC50 = 8.4 8.4 -13 2
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 338 5 2 8 3.0 Nc1nc(NCCc2cccnc2)nc2sc(-c3ccco3)nc12 10.1016/j.ejmech.2018.06.020
44186579 191784 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2
ChEMBL 494 6 2 7 1.6 CCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccccc5)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
CHEMBL519813 191784 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2
ChEMBL 494 6 2 7 1.6 CCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccccc5)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
57400352 69786 None 0 Human Functional pIC50 = 7.4 7.4 12 2
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assayAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assay
ChEMBL 283 3 1 8 1.7 CCCn1ncc2nc(N)n3nc(-c4ccco4)nc3c21 10.1016/j.bmc.2011.11.037
CHEMBL1935753 69786 None 0 Human Functional pIC50 = 7.4 7.4 12 2
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assayAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assay
ChEMBL 283 3 1 8 1.7 CCCn1ncc2nc(N)n3nc(-c4ccco4)nc3c21 10.1016/j.bmc.2011.11.037
49797855 10850 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 441 5 1 5 4.6 COc1ccc(N(CC(F)(F)F)C(C)=O)c2sc(NC(=O)c3ccc(F)cc3)nc12 10.1016/j.bmcl.2010.05.056
CHEMBL1172269 10850 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 441 5 1 5 4.6 COc1ccc(N(CC(F)(F)F)C(C)=O)c2sc(NC(=O)c3ccc(F)cc3)nc12 10.1016/j.bmcl.2010.05.056
135522368 492 None 1 Human Functional pIC50 = 7.4 7.4 - 1
Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptorInhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor
ChEMBL 493 9 2 9 2.7 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)Nc1ccc(c(c1)C)C 10.1021/jm0309654
383 492 None 1 Human Functional pIC50 = 7.4 7.4 - 1
Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptorInhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor
ChEMBL 493 9 2 9 2.7 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)Nc1ccc(c(c1)C)C 10.1021/jm0309654
CHEMBL33491 492 None 1 Human Functional pIC50 = 7.4 7.4 - 1
Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptorInhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor
ChEMBL 493 9 2 9 2.7 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)Nc1ccc(c(c1)C)C 10.1021/jm0309654
11371101 67567 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human cloned adenosine A2B cells expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP productionAntagonist activity at human cloned adenosine A2B cells expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP production
ChEMBL 336 4 0 6 2.2 CCCn1c(=O)c2c(nc3n2CC(C)=C3)n(Cc2ccccc2)c1=O 10.1016/j.bmc.2008.10.049
CHEMBL189904 67567 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human cloned adenosine A2B cells expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP productionAntagonist activity at human cloned adenosine A2B cells expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP production
ChEMBL 336 4 0 6 2.2 CCCn1c(=O)c2c(nc3n2CC(C)=C3)n(Cc2ccccc2)c1=O 10.1016/j.bmc.2008.10.049
11371101 67567 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Inhibition of 100 nM NECA-stimulated cAMP production in CHO cells expressing human adenosine A2B receptorInhibition of 100 nM NECA-stimulated cAMP production in CHO cells expressing human adenosine A2B receptor
ChEMBL 336 4 0 6 2.2 CCCn1c(=O)c2c(nc3n2CC(C)=C3)n(Cc2ccccc2)c1=O 10.1021/jm058008c
CHEMBL189904 67567 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Inhibition of 100 nM NECA-stimulated cAMP production in CHO cells expressing human adenosine A2B receptorInhibition of 100 nM NECA-stimulated cAMP production in CHO cells expressing human adenosine A2B receptor
ChEMBL 336 4 0 6 2.2 CCCn1c(=O)c2c(nc3n2CC(C)=C3)n(Cc2ccccc2)c1=O 10.1021/jm058008c
145961748 161511 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assayAntagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assay
ChEMBL 365 5 2 9 2.7 COc1ccccc1CNc1nc(N)c2nc(-c3cnccn3)sc2n1 10.1016/j.bmc.2018.05.048
CHEMBL4128190 161511 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assayAntagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assay
ChEMBL 365 5 2 9 2.7 COc1ccccc1CNc1nc(N)c2nc(-c3cnccn3)sc2n1 10.1016/j.bmc.2018.05.048
54586036 60724 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Inhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 minsInhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 mins
ChEMBL 534 6 1 6 4.8 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)[C@H]3CCN(C(=O)c4cccc(C(F)(F)F)c4)C3)sc12 10.1016/j.bmcl.2011.02.053
CHEMBL1760887 60724 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Inhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 minsInhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 mins
ChEMBL 534 6 1 6 4.8 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)[C@H]3CCN(C(=O)c4cccc(C(F)(F)F)c4)C3)sc12 10.1016/j.bmcl.2011.02.053
10761800 188219 None 0 Rat Functional pIC50 = 6.4 6.4 -5 2
Inhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytesInhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytes
ChEMBL 372 1 2 7 2.5 Cn1c(-c2cccc(C#N)c2)nc2c(N)nc(C#CC3(O)CCCCC3)nc21 10.1021/jm990499b
CHEMBL49925 188219 None 0 Rat Functional pIC50 = 6.4 6.4 -5 2
Inhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytesInhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytes
ChEMBL 372 1 2 7 2.5 Cn1c(-c2cccc(C#N)c2)nc2c(N)nc(C#CC3(O)CCCCC3)nc21 10.1021/jm990499b
46883041 5733 None 0 Human Functional pIC50 = 6.4 6.4 2 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 379 5 1 6 5.5 Cc1ccc(C(=O)c2nc(NC(C)c3ccccc3)nc3ccsc23)s1 10.1016/j.bmcl.2009.08.040
CHEMBL1078347 5733 None 0 Human Functional pIC50 = 6.4 6.4 2 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 379 5 1 6 5.5 Cc1ccc(C(=O)c2nc(NC(C)c3ccccc3)nc3ccsc23)s1 10.1016/j.bmcl.2009.08.040
46883074 5705 None 0 Human Functional pIC50 = 5.4 5.4 -1 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 380 5 0 7 4.3 Cc1ccc(C(=O)c2nc(N(C)Cc3cccnc3)nc3ccsc23)s1 10.1016/j.bmcl.2009.08.040
CHEMBL1078087 5705 None 0 Human Functional pIC50 = 5.4 5.4 -1 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 380 5 0 7 4.3 Cc1ccc(C(=O)c2nc(N(C)Cc3cccnc3)nc3ccsc23)s1 10.1016/j.bmcl.2009.08.040
57402117 69775 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assayAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assay
ChEMBL 254 1 1 7 1.5 Cn1cc2nc(N)n3nc(-c4ccco4)nc3c2c1 10.1016/j.bmc.2011.11.037
CHEMBL1935743 69775 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assayAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assay
ChEMBL 254 1 1 7 1.5 Cn1cc2nc(N)n3nc(-c4ccco4)nc3c2c1 10.1016/j.bmc.2011.11.037
49797852 10764 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 417 7 2 6 3.4 COc1ccc(N(CCCO)C(C)=O)c2sc(NC(=O)c3ccc(F)cc3)nc12 10.1016/j.bmcl.2010.05.056
CHEMBL1171524 10764 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 417 7 2 6 3.4 COc1ccc(N(CCCO)C(C)=O)c2sc(NC(=O)c3ccc(F)cc3)nc12 10.1016/j.bmcl.2010.05.056
54587015 60722 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Inhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 minsInhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 mins
ChEMBL 570 7 1 7 4.3 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)[C@@H]3CCN(S(=O)(=O)c4cccc(C(F)(F)F)c4)C3)sc12 10.1016/j.bmcl.2011.02.053
CHEMBL1760885 60722 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Inhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 minsInhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 mins
ChEMBL 570 7 1 7 4.3 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)[C@@H]3CCN(S(=O)(=O)c4cccc(C(F)(F)F)c4)C3)sc12 10.1016/j.bmcl.2011.02.053
71601632 86924 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP production by scintillation counting methodAntagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP production by scintillation counting method
ChEMBL 301 3 1 5 3.0 Nc1nc(Cc2ccccc2)nc2cn(-c3ccccc3)nc12 10.1016/j.ejmech.2015.11.015
CHEMBL2322918 86924 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP production by scintillation counting methodAntagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP production by scintillation counting method
ChEMBL 301 3 1 5 3.0 Nc1nc(Cc2ccccc2)nc2cn(-c3ccccc3)nc12 10.1016/j.ejmech.2015.11.015
71601632 86924 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated cAMP level preincubated for 10 mins followed by NECA stimulation by scintillation counting method in presence of [3H]-cyclic AMPAntagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated cAMP level preincubated for 10 mins followed by NECA stimulation by scintillation counting method in presence of [3H]-cyclic AMP
ChEMBL 301 3 1 5 3.0 Nc1nc(Cc2ccccc2)nc2cn(-c3ccccc3)nc12 10.1016/j.bmc.2016.04.048
CHEMBL2322918 86924 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated cAMP level preincubated for 10 mins followed by NECA stimulation by scintillation counting method in presence of [3H]-cyclic AMPAntagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated cAMP level preincubated for 10 mins followed by NECA stimulation by scintillation counting method in presence of [3H]-cyclic AMP
ChEMBL 301 3 1 5 3.0 Nc1nc(Cc2ccccc2)nc2cn(-c3ccccc3)nc12 10.1016/j.bmc.2016.04.048
71601632 86924 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP level by scintillation counting analysisAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP level by scintillation counting analysis
ChEMBL 301 3 1 5 3.0 Nc1nc(Cc2ccccc2)nc2cn(-c3ccccc3)nc12 10.1016/j.ejmech.2014.07.060
CHEMBL2322918 86924 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP level by scintillation counting analysisAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP level by scintillation counting analysis
ChEMBL 301 3 1 5 3.0 Nc1nc(Cc2ccccc2)nc2cn(-c3ccccc3)nc12 10.1016/j.ejmech.2014.07.060
9841364 101457 None 1 Rat Functional pIC50 = 6.4 6.4 -6 2
Inhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytesInhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytes
ChEMBL 351 1 2 6 2.4 Cn1c(-c2cccc(F)c2)nc2c(N)nc(C#CC3(O)CCCC3)nc21 10.1021/jm990499b
CHEMBL297685 101457 None 1 Rat Functional pIC50 = 6.4 6.4 -6 2
Inhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytesInhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytes
ChEMBL 351 1 2 6 2.4 Cn1c(-c2cccc(F)c2)nc2c(N)nc(C#CC3(O)CCCC3)nc21 10.1021/jm990499b
127045700 139722 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated cAMP level preincubated for 10 mins followed by NECA stimulation by scintillation counting method in presence of [3H]-cyclic AMPAntagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated cAMP level preincubated for 10 mins followed by NECA stimulation by scintillation counting method in presence of [3H]-cyclic AMP
ChEMBL 323 3 1 6 3.2 Cc1ccc(-c2nc(N)c3nn(Cc4cccc(F)c4)cc3n2)o1 10.1016/j.bmc.2016.04.048
CHEMBL3798214 139722 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated cAMP level preincubated for 10 mins followed by NECA stimulation by scintillation counting method in presence of [3H]-cyclic AMPAntagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated cAMP level preincubated for 10 mins followed by NECA stimulation by scintillation counting method in presence of [3H]-cyclic AMP
ChEMBL 323 3 1 6 3.2 Cc1ccc(-c2nc(N)c3nn(Cc4cccc(F)c4)cc3n2)o1 10.1016/j.bmc.2016.04.048
1329 1472 None 86 Human Functional pIC50 = 7.4 7.4 -9 8
Antagonist activity at human A2BR expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP production by alphascreen assayAntagonist activity at human A2BR expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP production by alphascreen assay
ChEMBL 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 10.1021/acs.jmedchem.9b00106
386 1472 None 86 Human Functional pIC50 = 7.4 7.4 -9 8
Antagonist activity at human A2BR expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP production by alphascreen assayAntagonist activity at human A2BR expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP production by alphascreen assay
ChEMBL 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 10.1021/acs.jmedchem.9b00106
CHEMBL183 1472 None 86 Human Functional pIC50 = 7.4 7.4 -9 8
Antagonist activity at human A2BR expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP production by alphascreen assayAntagonist activity at human A2BR expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP production by alphascreen assay
ChEMBL 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 10.1021/acs.jmedchem.9b00106
DB12946 1472 None 86 Human Functional pIC50 = 7.4 7.4 -9 8
Antagonist activity at human A2BR expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP production by alphascreen assayAntagonist activity at human A2BR expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP production by alphascreen assay
ChEMBL 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 10.1021/acs.jmedchem.9b00106
135678052 95777 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP levelsAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP levels
ChEMBL 483 8 2 8 3.2 CCCn1c(=O)c2[nH]c(-c3cc(C)n(CC(=O)Nc4ccc(Cl)cc4)n3)nc2n(CCC)c1=O 10.1016/j.bmc.2007.11.058
CHEMBL258571 95777 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP levelsAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP levels
ChEMBL 483 8 2 8 3.2 CCCn1c(=O)c2[nH]c(-c3cc(C)n(CC(=O)Nc4ccc(Cl)cc4)n3)nc2n(CCC)c1=O 10.1016/j.bmc.2007.11.058
46883042 5734 None 0 Human Functional pIC50 = 7.4 7.4 4 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 366 5 1 7 4.3 Cc1ccc(C(=O)c2nc(NCc3ccccn3)nc3ccsc23)s1 10.1016/j.bmcl.2009.08.040
CHEMBL1078348 5734 None 0 Human Functional pIC50 = 7.4 7.4 4 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 366 5 1 7 4.3 Cc1ccc(C(=O)c2nc(NCc3ccccn3)nc3ccsc23)s1 10.1016/j.bmcl.2009.08.040
136042347 71175 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 482 9 2 8 2.9 CCCn1c(=O)c2[nH]c(-c3cc(OCC(=O)Nc4ccc(F)cc4)nn3C)cc2n(CCC)c1=O 10.1021/jm201292w
CHEMBL1955925 71175 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 482 9 2 8 2.9 CCCn1c(=O)c2[nH]c(-c3cc(OCC(=O)Nc4ccc(F)cc4)nn3C)cc2n(CCC)c1=O 10.1021/jm201292w
118708234 113364 None 0 Human Functional pIC50 = 6.4 6.4 -10 3
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP level by scintillation counting analysisAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP level by scintillation counting analysis
ChEMBL 329 5 1 5 3.6 Nc1nc(CCCc2ccccc2)nc2cn(-c3ccccc3)nc12 10.1016/j.ejmech.2014.07.060
CHEMBL3317574 113364 None 0 Human Functional pIC50 = 6.4 6.4 -10 3
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP level by scintillation counting analysisAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP level by scintillation counting analysis
ChEMBL 329 5 1 5 3.6 Nc1nc(CCCc2ccccc2)nc2cn(-c3ccccc3)nc12 10.1016/j.ejmech.2014.07.060
127035626 137318 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity at human A2B adenosine receptor expressed in CHO cell membranes assessed as inhibition of NECA stimulated adenylyl cyclase activityAntagonist activity at human A2B adenosine receptor expressed in CHO cell membranes assessed as inhibition of NECA stimulated adenylyl cyclase activity
ChEMBL 426 6 3 8 4.0 O=C(Nc1ccccc1)Nc1nc(NCc2ccccc2)nc2nc(-c3ccco3)nn12 10.1016/j.ejmech.2015.12.019
CHEMBL3752621 137318 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity at human A2B adenosine receptor expressed in CHO cell membranes assessed as inhibition of NECA stimulated adenylyl cyclase activityAntagonist activity at human A2B adenosine receptor expressed in CHO cell membranes assessed as inhibition of NECA stimulated adenylyl cyclase activity
ChEMBL 426 6 3 8 4.0 O=C(Nc1ccccc1)Nc1nc(NCc2ccccc2)nc2nc(-c3ccco3)nn12 10.1016/j.ejmech.2015.12.019
145960873 161444 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assayAntagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assay
ChEMBL 347 5 2 6 4.0 Nc1nc(NCCc2ccccc2)nc2sc(-c3ccccc3)nc12 10.1016/j.bmc.2018.05.048
CHEMBL4127351 161444 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assayAntagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assay
ChEMBL 347 5 2 6 4.0 Nc1nc(NCCc2ccccc2)nc2sc(-c3ccccc3)nc12 10.1016/j.bmc.2018.05.048
54580150 60730 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Inhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 minsInhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 mins
ChEMBL 534 7 1 6 5.5 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)C3CCN(Cc4cccc(C(F)(F)F)c4)CC3)sc12 10.1016/j.bmcl.2011.02.053
CHEMBL1760894 60730 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Inhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 minsInhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 mins
ChEMBL 534 7 1 6 5.5 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)C3CCN(Cc4cccc(C(F)(F)F)c4)CC3)sc12 10.1016/j.bmcl.2011.02.053
71601631 86923 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP production by scintillation counting methodAntagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP production by scintillation counting method
ChEMBL 287 2 1 5 3.1 Nc1nc(-c2ccccc2)nc2cn(-c3ccccc3)nc12 10.1016/j.ejmech.2015.11.015
CHEMBL2322917 86923 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP production by scintillation counting methodAntagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP production by scintillation counting method
ChEMBL 287 2 1 5 3.1 Nc1nc(-c2ccccc2)nc2cn(-c3ccccc3)nc12 10.1016/j.ejmech.2015.11.015
71601631 86923 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated cAMP level preincubated for 10 mins followed by NECA stimulation by scintillation counting method in presence of [3H]-cyclic AMPAntagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated cAMP level preincubated for 10 mins followed by NECA stimulation by scintillation counting method in presence of [3H]-cyclic AMP
ChEMBL 287 2 1 5 3.1 Nc1nc(-c2ccccc2)nc2cn(-c3ccccc3)nc12 10.1016/j.bmc.2016.04.048
CHEMBL2322917 86923 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated cAMP level preincubated for 10 mins followed by NECA stimulation by scintillation counting method in presence of [3H]-cyclic AMPAntagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated cAMP level preincubated for 10 mins followed by NECA stimulation by scintillation counting method in presence of [3H]-cyclic AMP
ChEMBL 287 2 1 5 3.1 Nc1nc(-c2ccccc2)nc2cn(-c3ccccc3)nc12 10.1016/j.bmc.2016.04.048
71601631 86923 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP level by scintillation counting analysisAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP level by scintillation counting analysis
ChEMBL 287 2 1 5 3.1 Nc1nc(-c2ccccc2)nc2cn(-c3ccccc3)nc12 10.1016/j.ejmech.2014.07.060
CHEMBL2322917 86923 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP level by scintillation counting analysisAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP level by scintillation counting analysis
ChEMBL 287 2 1 5 3.1 Nc1nc(-c2ccccc2)nc2cn(-c3ccccc3)nc12 10.1016/j.ejmech.2014.07.060
10691124 101281 None 0 Rat Functional pIC50 = 6.4 6.4 -8 2
Inhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytesInhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytes
ChEMBL 379 1 2 6 3.2 Cn1c(-c2cccc(F)c2)nc2c(N)nc(C#CC3(O)CCCCCC3)nc21 10.1021/jm990499b
CHEMBL296389 101281 None 0 Rat Functional pIC50 = 6.4 6.4 -8 2
Inhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytesInhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytes
ChEMBL 379 1 2 6 3.2 Cn1c(-c2cccc(F)c2)nc2c(N)nc(C#CC3(O)CCCCCC3)nc21 10.1021/jm990499b
10618828 101988 None 0 Rat Functional pIC50 = 6.4 6.4 -5 2
Inhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytesInhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytes
ChEMBL 365 1 2 6 2.8 Cn1c(-c2ccccc2F)nc2c(N)nc(C#CC3(O)CCCCC3)nc21 10.1021/jm990499b
CHEMBL301512 101988 None 0 Rat Functional pIC50 = 6.4 6.4 -5 2
Inhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytesInhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytes
ChEMBL 365 1 2 6 2.8 Cn1c(-c2ccccc2F)nc2c(N)nc(C#CC3(O)CCCCC3)nc21 10.1021/jm990499b
10754589 193320 None 0 Rat Functional pIC50 = 5.4 5.4 - 1
Inhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytesInhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytes
ChEMBL 271 0 2 6 1.0 Cn1cnc2c(N)nc(C#CC3(O)CCCCC3)nc21 10.1021/jm990499b
CHEMBL52432 193320 None 0 Rat Functional pIC50 = 5.4 5.4 - 1
Inhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytesInhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytes
ChEMBL 271 0 2 6 1.0 Cn1cnc2c(N)nc(C#CC3(O)CCCCC3)nc21 10.1021/jm990499b
57396936 69794 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assayAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assay
ChEMBL 283 3 1 8 1.7 CCCn1cc2nc(N)n3nc(-c4ccco4)nc3c2n1 10.1016/j.bmc.2011.11.037
CHEMBL1935761 69794 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assayAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assay
ChEMBL 283 3 1 8 1.7 CCCn1cc2nc(N)n3nc(-c4ccco4)nc3c2n1 10.1016/j.bmc.2011.11.037
136042354 71154 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 476 8 2 9 2.9 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5cc(C)ccc5[nH]4)nn3C)nc2n(CCC)c1=O 10.1021/jm201292w
CHEMBL1955903 71154 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 476 8 2 9 2.9 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5cc(C)ccc5[nH]4)nn3C)nc2n(CCC)c1=O 10.1021/jm201292w
46883073 5704 None 0 Human Functional pIC50 = 6.4 6.4 -2 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 380 6 1 7 4.3 Cc1ccc(C(=O)c2nc(NCCc3cccnc3)nc3ccsc23)s1 10.1016/j.bmcl.2009.08.040
CHEMBL1078086 5704 None 0 Human Functional pIC50 = 6.4 6.4 -2 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 380 6 1 7 4.3 Cc1ccc(C(=O)c2nc(NCCc3cccnc3)nc3ccsc23)s1 10.1016/j.bmcl.2009.08.040
132991406 144213 None 0 Human Functional pIC50 = 6.3 6.3 -4786 2
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 353 5 2 8 3.5 COc1cccc(CNc2nc(N)c3nc(-c4ccco4)sc3n2)c1 10.1021/acs.jmedchem.6b01068
CHEMBL3904408 144213 None 0 Human Functional pIC50 = 6.3 6.3 -4786 2
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 353 5 2 8 3.5 COc1cccc(CNc2nc(N)c3nc(-c4ccco4)sc3n2)c1 10.1021/acs.jmedchem.6b01068
145958464 162159 None 0 Human Functional pIC50 = 5.3 5.3 -1174 2
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 369 5 2 8 4.0 COc1ccccc1CNc1nc(N)c2nc(-c3cccs3)sc2n1 10.1016/j.ejmech.2018.06.020
CHEMBL4162037 162159 None 0 Human Functional pIC50 = 5.3 5.3 -1174 2
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 369 5 2 8 4.0 COc1ccccc1CNc1nc(N)c2nc(-c3cccs3)sc2n1 10.1016/j.ejmech.2018.06.020
57396888 69777 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assayAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assay
ChEMBL 344 4 1 7 3.2 Nc1nc2cn(CCc3ccccc3)cc2c2nc(-c3ccco3)nn12 10.1016/j.bmc.2011.11.037
CHEMBL1935745 69777 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assayAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assay
ChEMBL 344 4 1 7 3.2 Nc1nc2cn(CCc3ccccc3)cc2c2nc(-c3ccco3)nn12 10.1016/j.bmc.2011.11.037
135522375 114257 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptorInhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor
ChEMBL 525 11 2 11 2.1 CCCn1c(=O)c2nc(-c3cc(OCC(=O)Nc4ccc(OC)c(OC)c4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
CHEMBL33305 114257 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptorInhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor
ChEMBL 525 11 2 11 2.1 CCCn1c(=O)c2nc(-c3cc(OCC(=O)Nc4ccc(OC)c(OC)c4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
46883109 5834 None 0 Human Functional pIC50 = 6.3 6.3 2 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 350 5 1 7 3.8 Cc1ccc(C(=O)c2nc(NCc3cccnc3)nc3ccsc23)o1 10.1016/j.bmcl.2009.08.040
CHEMBL1079117 5834 None 0 Human Functional pIC50 = 6.3 6.3 2 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 350 5 1 7 3.8 Cc1ccc(C(=O)c2nc(NCc3cccnc3)nc3ccsc23)o1 10.1016/j.bmcl.2009.08.040
134132667 144583 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 367 6 2 8 3.6 COc1cccc(CCNc2nc(N)c3nc(-c4ccco4)sc3n2)c1 10.1021/acs.jmedchem.6b01068
CHEMBL3907658 144583 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 367 6 2 8 3.6 COc1cccc(CCNc2nc(N)c3nc(-c4ccco4)sc3n2)c1 10.1021/acs.jmedchem.6b01068
10175278 170384 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptorInhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor
ChEMBL 588 9 2 8 3.4 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccc(I)cc4)nc3)[nH]c2n(CCC)c1=O 10.1021/jm0309654
CHEMBL444787 170384 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptorInhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor
ChEMBL 588 9 2 8 3.4 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccc(I)cc4)nc3)[nH]c2n(CCC)c1=O 10.1021/jm0309654
CHEMBL5075422 214372 None 3 Human Functional pIC50 = 6.3 6.3 -83 4
Antagonist activity at human recombinant adenosine A2B receptor transfected in HEK293 cells co-transfected with Galpha15/16 assessed as intracellular calcium change incubated for 10 mins by microplate reader methodAntagonist activity at human recombinant adenosine A2B receptor transfected in HEK293 cells co-transfected with Galpha15/16 assessed as intracellular calcium change incubated for 10 mins by microplate reader method
ChEMBL None None None Cn1cc(-c2cnc(N)n3nc(-c4ccco4)nc23)ccc1=O 10.1021/acsmedchemlett.1c00599
176407 4148 None 84 Human Functional pIC50 = 7.3 7.3 -13 2
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1021/acs.jmedchem.6b01068
405 4148 None 84 Human Functional pIC50 = 7.3 7.3 -13 2
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1021/acs.jmedchem.6b01068
CHEMBL113142 4148 None 84 Human Functional pIC50 = 7.3 7.3 -13 2
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1021/acs.jmedchem.6b01068
DB08770 4148 None 84 Human Functional pIC50 = 7.3 7.3 -13 2
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1021/acs.jmedchem.6b01068
134132684 144720 None 0 Human Functional pIC50 = 6.3 6.3 -20 2
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 353 5 3 8 3.3 Nc1nc(NCCc2ccc(O)cc2)nc2sc(-c3ccco3)nc12 10.1021/acs.jmedchem.6b01068
CHEMBL3908770 144720 None 0 Human Functional pIC50 = 6.3 6.3 -20 2
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 353 5 3 8 3.3 Nc1nc(NCCc2ccc(O)cc2)nc2sc(-c3ccco3)nc12 10.1021/acs.jmedchem.6b01068
46883108 5833 None 0 Human Functional pIC50 = 6.3 6.3 3 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 386 5 1 7 4.6 O=C(c1ccc(Cl)s1)c1nc(NCc2cccnc2)nc2ccsc12 10.1016/j.bmcl.2009.08.040
CHEMBL1079116 5833 None 0 Human Functional pIC50 = 6.3 6.3 3 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 386 5 1 7 4.6 O=C(c1ccc(Cl)s1)c1nc(NCc2cccnc2)nc2ccsc12 10.1016/j.bmcl.2009.08.040
54584125 60729 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Inhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 minsInhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 mins
ChEMBL 584 7 1 7 4.7 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)C3CCN(S(=O)(=O)c4cccc(C(F)(F)F)c4)CC3)sc12 10.1016/j.bmcl.2011.02.053
CHEMBL1760893 60729 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Inhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 minsInhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 mins
ChEMBL 584 7 1 7 4.7 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)C3CCN(S(=O)(=O)c4cccc(C(F)(F)F)c4)CC3)sc12 10.1016/j.bmcl.2011.02.053
10691124 101281 None 0 Human Functional pIC50 = 7.3 7.3 8 2
Inhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptorInhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptor
ChEMBL 379 1 2 6 3.2 Cn1c(-c2cccc(F)c2)nc2c(N)nc(C#CC3(O)CCCCCC3)nc21 10.1021/jm990499b
CHEMBL296389 101281 None 0 Human Functional pIC50 = 7.3 7.3 8 2
Inhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptorInhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptor
ChEMBL 379 1 2 6 3.2 Cn1c(-c2cccc(F)c2)nc2c(N)nc(C#CC3(O)CCCCCC3)nc21 10.1021/jm990499b
46237928 8809 None 0 Human Functional pIC50 = 7.3 7.3 -42 2
Antagonist activity human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated [3H]cAMP accumulation treated 15 mins before NECA challenge measured after 30 mins by liquid scintillation spectrometryAntagonist activity human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated [3H]cAMP accumulation treated 15 mins before NECA challenge measured after 30 mins by liquid scintillation spectrometry
ChEMBL 329 3 1 5 3.3 Cn1cc2c(NC(=O)c3ccccc3)nc(-c3ccccc3)nc2n1 10.1021/jm901785w
CHEMBL1096754 8809 None 0 Human Functional pIC50 = 7.3 7.3 -42 2
Antagonist activity human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated [3H]cAMP accumulation treated 15 mins before NECA challenge measured after 30 mins by liquid scintillation spectrometryAntagonist activity human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated [3H]cAMP accumulation treated 15 mins before NECA challenge measured after 30 mins by liquid scintillation spectrometry
ChEMBL 329 3 1 5 3.3 Cn1cc2c(NC(=O)c3ccccc3)nc(-c3ccccc3)nc2n1 10.1021/jm901785w
10762430 189160 None 0 Rat Functional pIC50 = 6.3 6.3 - 1
Inhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytesInhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytes
ChEMBL 381 1 2 6 3.3 Cn1c(-c2cccc(Cl)c2)nc2c(N)nc(C#CC3(O)CCCCC3)nc21 10.1021/jm990499b
CHEMBL51107 189160 None 0 Rat Functional pIC50 = 6.3 6.3 - 1
Inhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytesInhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytes
ChEMBL 381 1 2 6 3.3 Cn1c(-c2cccc(Cl)c2)nc2c(N)nc(C#CC3(O)CCCCC3)nc21 10.1021/jm990499b
45481754 198151 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity
ChEMBL 477 7 1 8 4.9 CCCn1cc2c(nc(NC(=O)C(c3ccccc3)c3ccccc3)n3nc(-c4ccco4)nc23)n1 10.1016/j.bmc.2009.05.038
CHEMBL574775 198151 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity
ChEMBL 477 7 1 8 4.9 CCCn1cc2c(nc(NC(=O)C(c3ccccc3)c3ccccc3)n3nc(-c4ccco4)nc23)n1 10.1016/j.bmc.2009.05.038
25230098 6216 None 0 Human Functional pIC50 = 6.3 6.3 14 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 299 4 2 6 2.1 CNC(=O)c1nc(NCc2cccnc2)nc2ccsc12 10.1016/j.bmcl.2009.08.040
CHEMBL1081334 6216 None 0 Human Functional pIC50 = 6.3 6.3 14 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 299 4 2 6 2.1 CNC(=O)c1nc(NCc2cccnc2)nc2ccsc12 10.1016/j.bmcl.2009.08.040
156010442 177043 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Inverse agonist activity at human A2B receptor expressed in CHO cells assessed as reduction in cAMP levelInverse agonist activity at human A2B receptor expressed in CHO cells assessed as reduction in cAMP level
ChEMBL 416 6 3 9 2.2 Nc1nc(NCCc2ccc(S(N)(=O)=O)cc2)nc2sc(-c3ccco3)nc12 10.1016/j.bmcl.2020.127067
CHEMBL4632532 177043 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Inverse agonist activity at human A2B receptor expressed in CHO cells assessed as reduction in cAMP levelInverse agonist activity at human A2B receptor expressed in CHO cells assessed as reduction in cAMP level
ChEMBL 416 6 3 9 2.2 Nc1nc(NCCc2ccc(S(N)(=O)=O)cc2)nc2sc(-c3ccco3)nc12 10.1016/j.bmcl.2020.127067
44186716 184114 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2
ChEMBL 524 7 2 8 1.6 CCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc(OC)cc5)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
CHEMBL482648 184114 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2
ChEMBL 524 7 2 8 1.6 CCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc(OC)cc5)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
44186718 184173 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2
ChEMBL 538 6 2 9 1.3 CCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc6c(c5)OCO6)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
CHEMBL483065 184173 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2
ChEMBL 538 6 2 9 1.3 CCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc6c(c5)OCO6)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
57325914 74725 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulationAntagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulation
ChEMBL 356 4 0 6 3.5 O=c1c(-c2ccco2)nnc2n(CCc3ccccc3)c3ccccc3n12 10.1021/jm201177b
CHEMBL2030706 74725 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulationAntagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulation
ChEMBL 356 4 0 6 3.5 O=c1c(-c2ccco2)nnc2n(CCc3ccccc3)c3ccccc3n12 10.1021/jm201177b
10714900 189450 None 0 Human Functional pIC50 = 6.3 6.3 12 2
Inhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptorInhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptor
ChEMBL 381 1 2 6 3.3 Cn1c(-c2ccc(Cl)cc2)nc2c(N)nc(C#CC3(O)CCCCC3)nc21 10.1021/jm990499b
CHEMBL51353 189450 None 0 Human Functional pIC50 = 6.3 6.3 12 2
Inhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptorInhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptor
ChEMBL 381 1 2 6 3.3 Cn1c(-c2ccc(Cl)cc2)nc2c(N)nc(C#CC3(O)CCCCC3)nc21 10.1021/jm990499b
45482074 198302 None 0 Human Functional pIC50 = 4.3 4.3 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity
ChEMBL 511 8 1 8 5.2 O=C(Cc1cccc(Cl)c1)Nc1nc2nn(CCCc3ccccc3)cc2c2nc(-c3ccco3)nn12 10.1016/j.bmc.2009.05.038
CHEMBL576017 198302 None 0 Human Functional pIC50 = 4.3 4.3 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity
ChEMBL 511 8 1 8 5.2 O=C(Cc1cccc(Cl)c1)Nc1nc2nn(CCCc3ccccc3)cc2c2nc(-c3ccco3)nn12 10.1016/j.bmc.2009.05.038
145960746 161604 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assayAntagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assay
ChEMBL 365 5 2 9 2.7 COc1cccc(CNc2nc(N)c3nc(-c4cnccn4)sc3n2)c1 10.1016/j.bmc.2018.05.048
CHEMBL4129565 161604 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assayAntagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assay
ChEMBL 365 5 2 9 2.7 COc1cccc(CNc2nc(N)c3nc(-c4cnccn4)sc3n2)c1 10.1016/j.bmc.2018.05.048
60154738 76987 None 0 Human Functional pIC50 = 6.3 6.3 -5 2
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production
ChEMBL 548 5 3 9 3.4 Cn1cc2c(nc(NC(=O)NC3CCN(C(=O)NCc4ccc(Cl)cc4)CC3)n3nc(-c4ccco4)nc23)n1 10.1021/jm300323t
CHEMBL2071047 76987 None 0 Human Functional pIC50 = 6.3 6.3 -5 2
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production
ChEMBL 548 5 3 9 3.4 Cn1cc2c(nc(NC(=O)NC3CCN(C(=O)NCc4ccc(Cl)cc4)CC3)n3nc(-c4ccco4)nc23)n1 10.1021/jm300323t
45482464 198532 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity
ChEMBL 447 7 1 8 4.1 CC(C)CCn1cc2c(nc(NC(=O)Cc3ccc(F)cc3)n3nc(-c4ccco4)nc23)n1 10.1016/j.bmc.2009.05.038
CHEMBL578005 198532 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity
ChEMBL 447 7 1 8 4.1 CC(C)CCn1cc2c(nc(NC(=O)Cc3ccc(F)cc3)n3nc(-c4ccco4)nc23)n1 10.1016/j.bmc.2009.05.038
136042341 71167 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 517 8 2 9 3.8 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5cc(C(F)(F)F)ccc5[nH]4)no3)nc2n(CCC)c1=O 10.1021/jm201292w
CHEMBL1955917 71167 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 517 8 2 9 3.8 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5cc(C(F)(F)F)ccc5[nH]4)no3)nc2n(CCC)c1=O 10.1021/jm201292w
176407 4148 None 84 Human Functional pIC50 = 7.3 7.3 -13 2
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1016/j.ejmech.2018.06.020
405 4148 None 84 Human Functional pIC50 = 7.3 7.3 -13 2
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1016/j.ejmech.2018.06.020
CHEMBL113142 4148 None 84 Human Functional pIC50 = 7.3 7.3 -13 2
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1016/j.ejmech.2018.06.020
DB08770 4148 None 84 Human Functional pIC50 = 7.3 7.3 -13 2
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1016/j.ejmech.2018.06.020
10616023 101862 None 0 Rat Functional pIC50 = 6.3 6.3 -3 2
Inhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytesInhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytes
ChEMBL 325 1 2 6 1.9 Cn1c(-c2cccc(F)c2)nc2c(N)nc(C#CC(C)(C)O)nc21 10.1021/jm990499b
CHEMBL300624 101862 None 0 Rat Functional pIC50 = 6.3 6.3 -3 2
Inhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytesInhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytes
ChEMBL 325 1 2 6 1.9 Cn1c(-c2cccc(F)c2)nc2c(N)nc(C#CC(C)(C)O)nc21 10.1021/jm990499b
46883158 5838 None 0 Human Functional pIC50 = 6.3 6.3 3 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 346 5 1 6 3.9 O=C(c1ccccc1)c1nc(NCc2cccnc2)nc2ccsc12 10.1016/j.bmcl.2009.08.040
CHEMBL1079141 5838 None 0 Human Functional pIC50 = 6.3 6.3 3 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 346 5 1 6 3.9 O=C(c1ccccc1)c1nc(NCc2cccnc2)nc2ccsc12 10.1016/j.bmcl.2009.08.040
127046493 139797 None 0 Human Functional pIC50 = 6.3 6.3 -83 3
Antagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated cAMP level preincubated for 10 mins followed by NECA stimulation by scintillation counting method in presence of [3H]-cyclic AMPAntagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated cAMP level preincubated for 10 mins followed by NECA stimulation by scintillation counting method in presence of [3H]-cyclic AMP
ChEMBL 321 4 1 7 2.7 COc1ccccc1Cn1cc2nc(-c3ccco3)nc(N)c2n1 10.1016/j.bmc.2016.04.048
CHEMBL3798766 139797 None 0 Human Functional pIC50 = 6.3 6.3 -83 3
Antagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated cAMP level preincubated for 10 mins followed by NECA stimulation by scintillation counting method in presence of [3H]-cyclic AMPAntagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated cAMP level preincubated for 10 mins followed by NECA stimulation by scintillation counting method in presence of [3H]-cyclic AMP
ChEMBL 321 4 1 7 2.7 COc1ccccc1Cn1cc2nc(-c3ccco3)nc(N)c2n1 10.1016/j.bmc.2016.04.048
16071896 58025 None 44 Mouse Functional pIC50 = 6.3 6.3 -4 2
Antagonist activity at mouse adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced increase of intracellular cAMP level after 30 mins by ELISAAntagonist activity at mouse adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced increase of intracellular cAMP level after 30 mins by ELISA
ChEMBL 335 4 1 5 3.1 O=C(Nc1cnc(-c2ccncc2F)c(-c2cccnc2)n1)C1CC1 10.1021/ml100249e
CHEMBL1672627 58025 None 44 Mouse Functional pIC50 = 6.3 6.3 -4 2
Antagonist activity at mouse adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced increase of intracellular cAMP level after 30 mins by ELISAAntagonist activity at mouse adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced increase of intracellular cAMP level after 30 mins by ELISA
ChEMBL 335 4 1 5 3.1 O=C(Nc1cnc(-c2ccncc2F)c(-c2cccnc2)n1)C1CC1 10.1021/ml100249e
25230950 152745 None 0 Human Functional pIC50 = 7.3 7.3 3 4
Fluorometric Imaging Plate Reader (FLIPR) Asssay: The use of a Fluorometric Imaging Plate Reader (FLIPR) to measure calcium flux in Adenosine-receptor expressing cells is a well-established technique. In this assay calcium flux is triggered by receptor activation and measured through the fluorescence of an incorporated calcium-sensitive dye. The potencies shown were determined using expressed human adenosine A2B receptors in mammalian cell lines. Selectivity values were obtained by using mammalian cell lines expressing the human adenosine A1, A2A and A3 receptors.Fluorometric Imaging Plate Reader (FLIPR) Asssay: The use of a Fluorometric Imaging Plate Reader (FLIPR) to measure calcium flux in Adenosine-receptor expressing cells is a well-established technique. In this assay calcium flux is triggered by receptor activation and measured through the fluorescence of an incorporated calcium-sensitive dye. The potencies shown were determined using expressed human adenosine A2B receptors in mammalian cell lines. Selectivity values were obtained by using mammalian cell lines expressing the human adenosine A1, A2A and A3 receptors.
ChEMBL 378 6 1 7 4.6 C=Cc1cc2nc(NCc3cccnc3)nc(C(=O)c3cccs3)c2s1 nan
CHEMBL3973260 152745 None 0 Human Functional pIC50 = 7.3 7.3 3 4
Fluorometric Imaging Plate Reader (FLIPR) Asssay: The use of a Fluorometric Imaging Plate Reader (FLIPR) to measure calcium flux in Adenosine-receptor expressing cells is a well-established technique. In this assay calcium flux is triggered by receptor activation and measured through the fluorescence of an incorporated calcium-sensitive dye. The potencies shown were determined using expressed human adenosine A2B receptors in mammalian cell lines. Selectivity values were obtained by using mammalian cell lines expressing the human adenosine A1, A2A and A3 receptors.Fluorometric Imaging Plate Reader (FLIPR) Asssay: The use of a Fluorometric Imaging Plate Reader (FLIPR) to measure calcium flux in Adenosine-receptor expressing cells is a well-established technique. In this assay calcium flux is triggered by receptor activation and measured through the fluorescence of an incorporated calcium-sensitive dye. The potencies shown were determined using expressed human adenosine A2B receptors in mammalian cell lines. Selectivity values were obtained by using mammalian cell lines expressing the human adenosine A1, A2A and A3 receptors.
ChEMBL 378 6 1 7 4.6 C=Cc1cc2nc(NCc3cccnc3)nc(C(=O)c3cccs3)c2s1 nan
136042334 71161 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 490 8 2 9 3.2 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5cc(C)c(C)cc5[nH]4)nn3C)nc2n(CCC)c1=O 10.1021/jm201292w
CHEMBL1955910 71161 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 490 8 2 9 3.2 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5cc(C)c(C)cc5[nH]4)nn3C)nc2n(CCC)c1=O 10.1021/jm201292w
46237929 8956 None 0 Human Functional pIC50 = 7.3 7.3 -138 2
Antagonist activity human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated [3H]cAMP accumulation treated 15 mins before NECA challenge measured after 30 mins by liquid scintillation spectrometryAntagonist activity human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated [3H]cAMP accumulation treated 15 mins before NECA challenge measured after 30 mins by liquid scintillation spectrometry
ChEMBL 359 4 1 6 3.3 COc1ccc(C(=O)Nc2nc(-c3ccccc3)nc3nn(C)cc23)cc1 10.1021/jm901785w
CHEMBL1098108 8956 None 0 Human Functional pIC50 = 7.3 7.3 -138 2
Antagonist activity human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated [3H]cAMP accumulation treated 15 mins before NECA challenge measured after 30 mins by liquid scintillation spectrometryAntagonist activity human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated [3H]cAMP accumulation treated 15 mins before NECA challenge measured after 30 mins by liquid scintillation spectrometry
ChEMBL 359 4 1 6 3.3 COc1ccc(C(=O)Nc2nc(-c3ccccc3)nc3nn(C)cc23)cc1 10.1021/jm901785w
10633978 185877 None 0 Rat Functional pIC50 = 5.3 5.3 - 1
Inhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytesInhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytes
ChEMBL 243 1 1 5 1.8 Cn1c(-c2cccc(F)c2)nc2c(N)ncnc21 10.1021/jm990499b
CHEMBL48682 185877 None 0 Rat Functional pIC50 = 5.3 5.3 - 1
Inhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytesInhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytes
ChEMBL 243 1 1 5 1.8 Cn1c(-c2cccc(F)c2)nc2c(N)ncnc21 10.1021/jm990499b
45482080 198425 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity
ChEMBL 451 6 1 8 4.5 CCCn1cc2c(nc(NC(=O)Cc3ccc4ccccc4c3)n3nc(-c4ccco4)nc23)n1 10.1016/j.bmc.2009.05.038
CHEMBL577135 198425 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity
ChEMBL 451 6 1 8 4.5 CCCn1cc2c(nc(NC(=O)Cc3ccc4ccccc4c3)n3nc(-c4ccco4)nc23)n1 10.1016/j.bmc.2009.05.038
46882994 5825 None 0 Human Functional pIC50 = 5.3 5.3 1 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 260 2 0 5 3.3 Cc1ccc(C(=O)c2ncnc3ccsc23)s1 10.1016/j.bmcl.2009.08.040
CHEMBL1079059 5825 None 0 Human Functional pIC50 = 5.3 5.3 1 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 260 2 0 5 3.3 Cc1ccc(C(=O)c2ncnc3ccsc23)s1 10.1016/j.bmcl.2009.08.040
136042351 71151 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 492 9 2 10 2.6 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5cc(OC)ccc5[nH]4)nn3C)nc2n(CCC)c1=O 10.1021/jm201292w
CHEMBL1955900 71151 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 492 9 2 10 2.6 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5cc(OC)ccc5[nH]4)nn3C)nc2n(CCC)c1=O 10.1021/jm201292w
386674 111321 None 2 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulationAntagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulation
ChEMBL 352 3 0 5 3.8 O=c1c(-c2ccccc2)nnc2n(Cc3ccccc3)c3ccccc3n12 10.1021/jm201177b
CHEMBL326752 111321 None 2 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulationAntagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulation
ChEMBL 352 3 0 5 3.8 O=c1c(-c2ccccc2)nnc2n(Cc3ccccc3)c3ccccc3n12 10.1021/jm201177b
10665761 189276 None 0 Rat Functional pIC50 = 6.3 6.3 -3 2
Inhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytesInhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytes
ChEMBL 353 3 2 6 2.7 CCC(O)(C#Cc1nc(N)c2nc(-c3cccc(F)c3)n(C)c2n1)CC 10.1021/jm990499b
CHEMBL51192 189276 None 0 Rat Functional pIC50 = 6.3 6.3 -3 2
Inhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytesInhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytes
ChEMBL 353 3 2 6 2.7 CCC(O)(C#Cc1nc(N)c2nc(-c3cccc(F)c3)n(C)c2n1)CC 10.1021/jm990499b
145954098 162539 None 0 Human Functional pIC50 = 6.3 6.3 -35 2
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 345 4 2 8 4.1 Nc1nc(NCc2cccs2)nc2sc(-c3cccs3)nc12 10.1016/j.ejmech.2018.06.020
CHEMBL4168016 162539 None 0 Human Functional pIC50 = 6.3 6.3 -35 2
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 345 4 2 8 4.1 Nc1nc(NCc2cccs2)nc2sc(-c3cccs3)nc12 10.1016/j.ejmech.2018.06.020
57402162 69799 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assayAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assay
ChEMBL 494 7 2 9 4.6 COc1ccc(NC(=O)Nc2nc3cn(CCc4ccccc4)nc3c3nc(-c4ccco4)nn23)cc1 10.1016/j.bmc.2011.11.037
CHEMBL1935766 69799 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assayAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assay
ChEMBL 494 7 2 9 4.6 COc1ccc(NC(=O)Nc2nc3cn(CCc4ccccc4)nc3c3nc(-c4ccco4)nn23)cc1 10.1016/j.bmc.2011.11.037
44537897 198076 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity
ChEMBL 497 7 1 8 5.0 CC(C)CCn1cc2c(nc(NC(=O)Cc3ccc(C(F)(F)F)cc3)n3nc(-c4ccco4)nc23)n1 10.1016/j.bmc.2009.05.038
CHEMBL574263 198076 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity
ChEMBL 497 7 1 8 5.0 CC(C)CCn1cc2c(nc(NC(=O)Cc3ccc(C(F)(F)F)cc3)n3nc(-c4ccco4)nc23)n1 10.1016/j.bmc.2009.05.038
46883043 5735 None 0 Human Functional pIC50 = 7.3 7.3 18 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 366 5 1 7 4.3 Cc1ccc(C(=O)c2nc(NCc3cccnc3)nc3ccsc23)s1 10.1016/j.bmcl.2009.08.040
CHEMBL1078349 5735 None 0 Human Functional pIC50 = 7.3 7.3 18 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 366 5 1 7 4.3 Cc1ccc(C(=O)c2nc(NCc3cccnc3)nc3ccsc23)s1 10.1016/j.bmcl.2009.08.040
134138322 148039 None 0 Human Functional pIC50 = 6.3 6.3 -15 2
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 367 6 2 8 3.6 COc1ccc(CCNc2nc(N)c3nc(-c4ccco4)sc3n2)cc1 10.1021/acs.jmedchem.6b01068
CHEMBL3934626 148039 None 0 Human Functional pIC50 = 6.3 6.3 -15 2
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 367 6 2 8 3.6 COc1ccc(CCNc2nc(N)c3nc(-c4ccco4)sc3n2)cc1 10.1021/acs.jmedchem.6b01068
145963661 161542 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assayAntagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assay
ChEMBL 301 4 2 7 2.6 COc1ccccc1CNc1nc(N)c2nc(C)sc2n1 10.1016/j.bmc.2018.05.048
CHEMBL4128638 161542 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assayAntagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assay
ChEMBL 301 4 2 7 2.6 COc1ccccc1CNc1nc(N)c2nc(C)sc2n1 10.1016/j.bmc.2018.05.048
46883040 5687 None 0 Human Functional pIC50 = 5.3 5.3 1 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 365 5 1 6 4.9 Cc1ccc(C(=O)c2nc(NCc3ccccc3)nc3ccsc23)s1 10.1016/j.bmcl.2009.08.040
CHEMBL1077985 5687 None 0 Human Functional pIC50 = 5.3 5.3 1 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 365 5 1 6 4.9 Cc1ccc(C(=O)c2nc(NCc3ccccc3)nc3ccsc23)s1 10.1016/j.bmcl.2009.08.040
10621771 193119 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Inhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptorInhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptor
ChEMBL 415 1 2 6 3.7 Cn1c(-c2cccc(C(F)(F)F)c2)nc2c(N)nc(C#CC3(O)CCCCC3)nc21 10.1021/jm990499b
CHEMBL52276 193119 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Inhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptorInhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptor
ChEMBL 415 1 2 6 3.7 Cn1c(-c2cccc(C(F)(F)F)c2)nc2c(N)nc(C#CC3(O)CCCCC3)nc21 10.1021/jm990499b
25230100 6352 None 0 Human Functional pIC50 = 6.2 6.2 5 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 367 5 2 6 3.8 O=C(NC1CCCCC1)c1nc(NCc2cccnc2)nc2ccsc12 10.1016/j.bmcl.2009.08.040
CHEMBL1082063 6352 None 0 Human Functional pIC50 = 6.2 6.2 5 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 367 5 2 6 3.8 O=C(NC1CCCCC1)c1nc(NCc2cccnc2)nc2ccsc12 10.1016/j.bmcl.2009.08.040
9970667 205281 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulationAntagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulation
ChEMBL 276 1 0 5 2.2 Cn1c2ccccc2n2c(=O)c(-c3ccccc3)nnc12 10.1021/jm201177b
CHEMBL7909 205281 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulationAntagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulation
ChEMBL 276 1 0 5 2.2 Cn1c2ccccc2n2c(=O)c(-c3ccccc3)nnc12 10.1021/jm201177b
135874413 96390 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP levelsAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP levels
ChEMBL 449 8 2 8 2.5 CCCn1c(=O)c2[nH]c(-c3cc(C)n(CC(=O)Nc4ccccc4)n3)nc2n(CCC)c1=O 10.1016/j.bmc.2007.11.058
CHEMBL261810 96390 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP levelsAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP levels
ChEMBL 449 8 2 8 2.5 CCCn1c(=O)c2[nH]c(-c3cc(C)n(CC(=O)Nc4ccccc4)n3)nc2n(CCC)c1=O 10.1016/j.bmc.2007.11.058
156018440 177852 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Inverse agonist activity at human A2B receptor expressed in CHO cells assessed as reduction in cAMP levelInverse agonist activity at human A2B receptor expressed in CHO cells assessed as reduction in cAMP level
ChEMBL 457 4 2 10 1.9 Nc1nc(N2CCN(c3ccc(S(N)(=O)=O)cc3)CC2)nc2sc(-c3ccco3)nc12 10.1016/j.bmcl.2020.127067
CHEMBL4644153 177852 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Inverse agonist activity at human A2B receptor expressed in CHO cells assessed as reduction in cAMP levelInverse agonist activity at human A2B receptor expressed in CHO cells assessed as reduction in cAMP level
ChEMBL 457 4 2 10 1.9 Nc1nc(N2CCN(c3ccc(S(N)(=O)=O)cc3)CC2)nc2sc(-c3ccco3)nc12 10.1016/j.bmcl.2020.127067
57395164 69797 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assayAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assay
ChEMBL 404 4 2 9 2.9 COc1ccc(NC(=O)Nc2nc3cn(C)nc3c3nc(-c4ccco4)nn23)cc1 10.1016/j.bmc.2011.11.037
CHEMBL1935764 69797 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assayAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assay
ChEMBL 404 4 2 9 2.9 COc1ccc(NC(=O)Nc2nc3cn(C)nc3c3nc(-c4ccco4)nn23)cc1 10.1016/j.bmc.2011.11.037
45481760 198008 None 0 Human Functional pIC50 = 5.2 5.2 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity
ChEMBL 539 8 1 8 5.7 O=C(Nc1nc2nn(CCc3ccccc3)cc2c2nc(-c3ccco3)nn12)C(c1ccccc1)c1ccccc1 10.1016/j.bmc.2009.05.038
CHEMBL573780 198008 None 0 Human Functional pIC50 = 5.2 5.2 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity
ChEMBL 539 8 1 8 5.7 O=C(Nc1nc2nn(CCc3ccccc3)cc2c2nc(-c3ccco3)nn12)C(c1ccccc1)c1ccccc1 10.1016/j.bmc.2009.05.038
57395162 69788 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assayAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assay
ChEMBL 359 5 1 8 2.9 Nc1nc2cnn(CCCc3ccccc3)c2c2nc(-c3ccco3)nn12 10.1016/j.bmc.2011.11.037
CHEMBL1935755 69788 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assayAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assay
ChEMBL 359 5 1 8 2.9 Nc1nc2cnn(CCCc3ccccc3)c2c2nc(-c3ccco3)nn12 10.1016/j.bmc.2011.11.037
49797905 10743 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 517 7 1 7 5.2 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3cnn(Cc4cccc(C(F)(F)F)c4)c3)sc12 10.1016/j.bmcl.2010.05.056
CHEMBL1171164 10743 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 517 7 1 7 5.2 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3cnn(Cc4cccc(C(F)(F)F)c4)c3)sc12 10.1016/j.bmcl.2010.05.056
49797905 10743 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Inhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 minsInhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 mins
ChEMBL 517 7 1 7 5.2 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3cnn(Cc4cccc(C(F)(F)F)c4)c3)sc12 10.1016/j.bmcl.2011.02.053
CHEMBL1171164 10743 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Inhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 minsInhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 mins
ChEMBL 517 7 1 7 5.2 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3cnn(Cc4cccc(C(F)(F)F)c4)c3)sc12 10.1016/j.bmcl.2011.02.053
136042339 71165 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 483 8 2 9 3.5 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5cc(Cl)ccc5[nH]4)no3)nc2n(CCC)c1=O 10.1021/jm201292w
CHEMBL1955915 71165 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 483 8 2 9 3.5 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5cc(Cl)ccc5[nH]4)no3)nc2n(CCC)c1=O 10.1021/jm201292w
25230881 6177 None 0 Human Functional pIC50 = 8.2 8.2 1 4
Fluorometric Imaging Plate Reader (FLIPR) Asssay: The use of a Fluorometric Imaging Plate Reader (FLIPR) to measure calcium flux in Adenosine-receptor expressing cells is a well-established technique. In this assay calcium flux is triggered by receptor activation and measured through the fluorescence of an incorporated calcium-sensitive dye. The potencies shown were determined using expressed human adenosine A2B receptors in mammalian cell lines. Selectivity values were obtained by using mammalian cell lines expressing the human adenosine A1, A2A and A3 receptors.Fluorometric Imaging Plate Reader (FLIPR) Asssay: The use of a Fluorometric Imaging Plate Reader (FLIPR) to measure calcium flux in Adenosine-receptor expressing cells is a well-established technique. In this assay calcium flux is triggered by receptor activation and measured through the fluorescence of an incorporated calcium-sensitive dye. The potencies shown were determined using expressed human adenosine A2B receptors in mammalian cell lines. Selectivity values were obtained by using mammalian cell lines expressing the human adenosine A1, A2A and A3 receptors.
ChEMBL 395 6 1 8 4.1 CN(C)c1cc2nc(NCc3cccnc3)nc(C(=O)c3cccs3)c2s1 nan
CHEMBL1081160 6177 None 0 Human Functional pIC50 = 8.2 8.2 1 4
Fluorometric Imaging Plate Reader (FLIPR) Asssay: The use of a Fluorometric Imaging Plate Reader (FLIPR) to measure calcium flux in Adenosine-receptor expressing cells is a well-established technique. In this assay calcium flux is triggered by receptor activation and measured through the fluorescence of an incorporated calcium-sensitive dye. The potencies shown were determined using expressed human adenosine A2B receptors in mammalian cell lines. Selectivity values were obtained by using mammalian cell lines expressing the human adenosine A1, A2A and A3 receptors.Fluorometric Imaging Plate Reader (FLIPR) Asssay: The use of a Fluorometric Imaging Plate Reader (FLIPR) to measure calcium flux in Adenosine-receptor expressing cells is a well-established technique. In this assay calcium flux is triggered by receptor activation and measured through the fluorescence of an incorporated calcium-sensitive dye. The potencies shown were determined using expressed human adenosine A2B receptors in mammalian cell lines. Selectivity values were obtained by using mammalian cell lines expressing the human adenosine A1, A2A and A3 receptors.
ChEMBL 395 6 1 8 4.1 CN(C)c1cc2nc(NCc3cccnc3)nc(C(=O)c3cccs3)c2s1 nan
25230948 6035 None 0 Human Functional pIC50 = 8.2 8.2 3 4
Fluorometric Imaging Plate Reader (FLIPR) Asssay: The use of a Fluorometric Imaging Plate Reader (FLIPR) to measure calcium flux in Adenosine-receptor expressing cells is a well-established technique. In this assay calcium flux is triggered by receptor activation and measured through the fluorescence of an incorporated calcium-sensitive dye. The potencies shown were determined using expressed human adenosine A2B receptors in mammalian cell lines. Selectivity values were obtained by using mammalian cell lines expressing the human adenosine A1, A2A and A3 receptors.Fluorometric Imaging Plate Reader (FLIPR) Asssay: The use of a Fluorometric Imaging Plate Reader (FLIPR) to measure calcium flux in Adenosine-receptor expressing cells is a well-established technique. In this assay calcium flux is triggered by receptor activation and measured through the fluorescence of an incorporated calcium-sensitive dye. The potencies shown were determined using expressed human adenosine A2B receptors in mammalian cell lines. Selectivity values were obtained by using mammalian cell lines expressing the human adenosine A1, A2A and A3 receptors.
ChEMBL 395 7 2 8 4.4 CCNc1cc2nc(NCc3cccnc3)nc(C(=O)c3cccs3)c2s1 nan
CHEMBL1080421 6035 None 0 Human Functional pIC50 = 8.2 8.2 3 4
Fluorometric Imaging Plate Reader (FLIPR) Asssay: The use of a Fluorometric Imaging Plate Reader (FLIPR) to measure calcium flux in Adenosine-receptor expressing cells is a well-established technique. In this assay calcium flux is triggered by receptor activation and measured through the fluorescence of an incorporated calcium-sensitive dye. The potencies shown were determined using expressed human adenosine A2B receptors in mammalian cell lines. Selectivity values were obtained by using mammalian cell lines expressing the human adenosine A1, A2A and A3 receptors.Fluorometric Imaging Plate Reader (FLIPR) Asssay: The use of a Fluorometric Imaging Plate Reader (FLIPR) to measure calcium flux in Adenosine-receptor expressing cells is a well-established technique. In this assay calcium flux is triggered by receptor activation and measured through the fluorescence of an incorporated calcium-sensitive dye. The potencies shown were determined using expressed human adenosine A2B receptors in mammalian cell lines. Selectivity values were obtained by using mammalian cell lines expressing the human adenosine A1, A2A and A3 receptors.
ChEMBL 395 7 2 8 4.4 CCNc1cc2nc(NCc3cccnc3)nc(C(=O)c3cccs3)c2s1 nan
156821433 185994 None 0 Human Functional pIC50 = 8.2 8.2 -12 2
Antagonist activity at human A2bR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assayAntagonist activity at human A2bR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assay
ChEMBL 427 4 1 8 2.9 Cn1cc(-c2c(-c3ccccc3)nc(N)n3nc(Cc4ncccc4F)nc23)ccc1=O 10.1021/acsmedchemlett.1c00620
CHEMBL4870159 185994 None 0 Human Functional pIC50 = 8.2 8.2 -12 2
Antagonist activity at human A2bR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assayAntagonist activity at human A2bR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assay
ChEMBL 427 4 1 8 2.9 Cn1cc(-c2c(-c3ccccc3)nc(N)n3nc(Cc4ncccc4F)nc23)ccc1=O 10.1021/acsmedchemlett.1c00620
49797826 10667 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 416 6 2 6 2.5 COc1ccc(N(CC(N)=O)C(C)=O)c2sc(NC(=O)c3ccc(F)cc3)nc12 10.1016/j.bmcl.2010.05.056
CHEMBL1170526 10667 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 416 6 2 6 2.5 COc1ccc(N(CC(N)=O)C(C)=O)c2sc(NC(=O)c3ccc(F)cc3)nc12 10.1016/j.bmcl.2010.05.056
136042331 71157 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 476 8 2 9 2.9 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5c(C)cccc5[nH]4)nn3C)nc2n(CCC)c1=O 10.1021/jm201292w
CHEMBL1955906 71157 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 476 8 2 9 2.9 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5c(C)cccc5[nH]4)nn3C)nc2n(CCC)c1=O 10.1021/jm201292w
135489238 477 None 1 Human Functional pIC50 = 7.2 7.2 - 1
Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptorInhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor
ChEMBL 533 9 2 9 3.4 CCCn1c2[nH]c(nc2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)Nc1ccc(c(c1)Cl)Cl 10.1021/jm0309654
381 477 None 1 Human Functional pIC50 = 7.2 7.2 - 1
Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptorInhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor
ChEMBL 533 9 2 9 3.4 CCCn1c2[nH]c(nc2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)Nc1ccc(c(c1)Cl)Cl 10.1021/jm0309654
CHEMBL32802 477 None 1 Human Functional pIC50 = 7.2 7.2 - 1
Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptorInhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor
ChEMBL 533 9 2 9 3.4 CCCn1c2[nH]c(nc2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)Nc1ccc(c(c1)Cl)Cl 10.1021/jm0309654
49797797 10618 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 444 6 1 6 3.1 COc1ccc(N(CC(=O)N(C)C)C(C)=O)c2sc(NC(=O)c3ccc(F)cc3)nc12 10.1016/j.bmcl.2010.05.056
CHEMBL1170131 10618 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 444 6 1 6 3.1 COc1ccc(N(CC(=O)N(C)C)C(C)=O)c2sc(NC(=O)c3ccc(F)cc3)nc12 10.1016/j.bmcl.2010.05.056
49797827 10642 None 0 Human Functional pIC50 = 5.2 5.2 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 417 6 2 6 3.1 COc1ccc(N(CC(=O)O)C(C)=O)c2sc(NC(=O)c3ccc(F)cc3)nc12 10.1016/j.bmcl.2010.05.056
CHEMBL1170295 10642 None 0 Human Functional pIC50 = 5.2 5.2 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 417 6 2 6 3.1 COc1ccc(N(CC(=O)O)C(C)=O)c2sc(NC(=O)c3ccc(F)cc3)nc12 10.1016/j.bmcl.2010.05.056
135874420 161302 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP levelsAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP levels
ChEMBL 479 9 2 9 2.5 CCCn1c(=O)c2[nH]c(-c3cc(C)n(CC(=O)Nc4ccc(OC)cc4)n3)nc2n(CCC)c1=O 10.1016/j.bmc.2007.11.058
CHEMBL412284 161302 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP levelsAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP levels
ChEMBL 479 9 2 9 2.5 CCCn1c(=O)c2[nH]c(-c3cc(C)n(CC(=O)Nc4ccc(OC)cc4)n3)nc2n(CCC)c1=O 10.1016/j.bmc.2007.11.058
136042328 71147 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 507 9 2 11 2.5 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5cc([N+](=O)[O-])ccc5[nH]4)nn3C)nc2n(CCC)c1=O 10.1021/jm201292w
CHEMBL1955894 71147 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 507 9 2 11 2.5 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5cc([N+](=O)[O-])ccc5[nH]4)nn3C)nc2n(CCC)c1=O 10.1021/jm201292w
136042352 71152 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 540 8 2 9 3.3 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5cc(Br)ccc5[nH]4)nn3C)nc2n(CCC)c1=O 10.1021/jm201292w
CHEMBL1955901 71152 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 540 8 2 9 3.3 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5cc(Br)ccc5[nH]4)nn3C)nc2n(CCC)c1=O 10.1021/jm201292w
156821338 185819 None 0 Human Functional pIC50 = 7.2 7.2 -8 2
Antagonist activity at human A2bR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assayAntagonist activity at human A2bR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assay
ChEMBL 439 5 1 9 2.7 COc1ccc(Cc2nc3c(-c4ccc(=O)n(C)c4)c(-c4ccccc4)nc(N)n3n2)nc1 10.1021/acsmedchemlett.1c00620
CHEMBL4867286 185819 None 0 Human Functional pIC50 = 7.2 7.2 -8 2
Antagonist activity at human A2bR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assayAntagonist activity at human A2bR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assay
ChEMBL 439 5 1 9 2.7 COc1ccc(Cc2nc3c(-c4ccc(=O)n(C)c4)c(-c4ccccc4)nc(N)n3n2)nc1 10.1021/acsmedchemlett.1c00620
9841364 101457 None 1 Human Functional pIC50 = 7.2 7.2 6 2
Inhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptorInhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptor
ChEMBL 351 1 2 6 2.4 Cn1c(-c2cccc(F)c2)nc2c(N)nc(C#CC3(O)CCCC3)nc21 10.1021/jm990499b
CHEMBL297685 101457 None 1 Human Functional pIC50 = 7.2 7.2 6 2
Inhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptorInhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptor
ChEMBL 351 1 2 6 2.4 Cn1c(-c2cccc(F)c2)nc2c(N)nc(C#CC3(O)CCCC3)nc21 10.1021/jm990499b
118708214 113353 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP level by scintillation counting analysisAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP level by scintillation counting analysis
ChEMBL 211 1 1 5 1.4 Nc1ncnc2cn(-c3ccccc3)nc12 10.1016/j.ejmech.2014.07.060
CHEMBL3317555 113353 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP level by scintillation counting analysisAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP level by scintillation counting analysis
ChEMBL 211 1 1 5 1.4 Nc1ncnc2cn(-c3ccccc3)nc12 10.1016/j.ejmech.2014.07.060
10714900 189450 None 0 Rat Functional pIC50 = 5.2 5.2 -12 2
Inhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytesInhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytes
ChEMBL 381 1 2 6 3.3 Cn1c(-c2ccc(Cl)cc2)nc2c(N)nc(C#CC3(O)CCCCC3)nc21 10.1021/jm990499b
CHEMBL51353 189450 None 0 Rat Functional pIC50 = 5.2 5.2 -12 2
Inhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytesInhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytes
ChEMBL 381 1 2 6 3.3 Cn1c(-c2ccc(Cl)cc2)nc2c(N)nc(C#CC3(O)CCCCC3)nc21 10.1021/jm990499b
134139825 146497 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 309 3 2 7 3.7 Nc1nc(Nc2ccccc2)nc2sc(-c3ccco3)nc12 10.1021/acs.jmedchem.6b01068
CHEMBL3922410 146497 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 309 3 2 7 3.7 Nc1nc(Nc2ccccc2)nc2sc(-c3ccco3)nc12 10.1021/acs.jmedchem.6b01068
127045910 140039 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated cAMP level preincubated for 10 mins followed by NECA stimulation by scintillation counting method in presence of [3H]-cyclic AMPAntagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated cAMP level preincubated for 10 mins followed by NECA stimulation by scintillation counting method in presence of [3H]-cyclic AMP
ChEMBL 321 3 2 7 2.7 Cc1ccc(-c2nc(N)c3nn(Cc4cccc(O)c4)cc3n2)o1 10.1016/j.bmc.2016.04.048
CHEMBL3800254 140039 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated cAMP level preincubated for 10 mins followed by NECA stimulation by scintillation counting method in presence of [3H]-cyclic AMPAntagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated cAMP level preincubated for 10 mins followed by NECA stimulation by scintillation counting method in presence of [3H]-cyclic AMP
ChEMBL 321 3 2 7 2.7 Cc1ccc(-c2nc(N)c3nn(Cc4cccc(O)c4)cc3n2)o1 10.1016/j.bmc.2016.04.048
136042344 71170 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 551 8 2 9 4.5 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5c(Cl)cc(C(F)(F)F)cc5[nH]4)no3)nc2n(CCC)c1=O 10.1021/jm201292w
CHEMBL1955920 71170 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 551 8 2 9 4.5 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5c(Cl)cc(C(F)(F)F)cc5[nH]4)no3)nc2n(CCC)c1=O 10.1021/jm201292w
11716665 2281 None 37 Mouse Functional pIC50 = 6.2 6.2 -1 2
Inhibition of NECA-induced IL6 production in Swiss mouse fibroblasts after 24 hrs by ELISAInhibition of NECA-induced IL6 production in Swiss mouse fibroblasts after 24 hrs by ELISA
ChEMBL 316 4 1 7 3.3 n1ccc(nc1)c1cnc(nc1c1ccco1)Nc1cccnc1 10.1021/jm061333v
5617 2281 None 37 Mouse Functional pIC50 = 6.2 6.2 -1 2
Inhibition of NECA-induced IL6 production in Swiss mouse fibroblasts after 24 hrs by ELISAInhibition of NECA-induced IL6 production in Swiss mouse fibroblasts after 24 hrs by ELISA
ChEMBL 316 4 1 7 3.3 n1ccc(nc1)c1cnc(nc1c1ccco1)Nc1cccnc1 10.1021/jm061333v
CHEMBL375293 2281 None 37 Mouse Functional pIC50 = 6.2 6.2 -1 2
Inhibition of NECA-induced IL6 production in Swiss mouse fibroblasts after 24 hrs by ELISAInhibition of NECA-induced IL6 production in Swiss mouse fibroblasts after 24 hrs by ELISA
ChEMBL 316 4 1 7 3.3 n1ccc(nc1)c1cnc(nc1c1ccco1)Nc1cccnc1 10.1021/jm061333v
45482087 198106 None 0 Human Functional pIC50 = 5.2 5.2 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity
ChEMBL 441 4 1 8 3.8 Cn1cc2c(nc(NC(=O)Cc3c(Cl)cccc3Cl)n3nc(-c4ccco4)nc23)n1 10.1016/j.bmc.2009.05.038
CHEMBL574490 198106 None 0 Human Functional pIC50 = 5.2 5.2 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity
ChEMBL 441 4 1 8 3.8 Cn1cc2c(nc(NC(=O)Cc3c(Cl)cccc3Cl)n3nc(-c4ccco4)nc23)n1 10.1016/j.bmc.2009.05.038
136042355 71148 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 462 8 2 9 2.6 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5ccccc5[nH]4)nn3C)nc2n(CCC)c1=O 10.1021/jm201292w
CHEMBL1955897 71148 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 462 8 2 9 2.6 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5ccccc5[nH]4)nn3C)nc2n(CCC)c1=O 10.1021/jm201292w
135443367 487 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptorInhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor
ChEMBL 534 9 1 10 1.8 CCCn1c2[nH]c(nc2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)N1CCN(CC1)c1ccccc1 10.1021/jm0309654
382 487 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptorInhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor
ChEMBL 534 9 1 10 1.8 CCCn1c2[nH]c(nc2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)N1CCN(CC1)c1ccccc1 10.1021/jm0309654
CHEMBL33455 487 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptorInhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor
ChEMBL 534 9 1 10 1.8 CCCn1c2[nH]c(nc2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)N1CCN(CC1)c1ccccc1 10.1021/jm0309654
135874416 96388 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP levelsAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP levels
ChEMBL 467 8 2 8 2.7 CCCn1c(=O)c2[nH]c(-c3cc(C)n(CC(=O)Nc4ccc(F)cc4)n3)nc2n(CCC)c1=O 10.1016/j.bmc.2007.11.058
CHEMBL261809 96388 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP levelsAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP levels
ChEMBL 467 8 2 8 2.7 CCCn1c(=O)c2[nH]c(-c3cc(C)n(CC(=O)Nc4ccc(F)cc4)n3)nc2n(CCC)c1=O 10.1016/j.bmc.2007.11.058
25230952 146552 None 0 Human Functional pIC50 = 7.2 7.2 3 4
Fluorometric Imaging Plate Reader (FLIPR) Asssay: The use of a Fluorometric Imaging Plate Reader (FLIPR) to measure calcium flux in Adenosine-receptor expressing cells is a well-established technique. In this assay calcium flux is triggered by receptor activation and measured through the fluorescence of an incorporated calcium-sensitive dye. The potencies shown were determined using expressed human adenosine A2B receptors in mammalian cell lines. Selectivity values were obtained by using mammalian cell lines expressing the human adenosine A1, A2A and A3 receptors.Fluorometric Imaging Plate Reader (FLIPR) Asssay: The use of a Fluorometric Imaging Plate Reader (FLIPR) to measure calcium flux in Adenosine-receptor expressing cells is a well-established technique. In this assay calcium flux is triggered by receptor activation and measured through the fluorescence of an incorporated calcium-sensitive dye. The potencies shown were determined using expressed human adenosine A2B receptors in mammalian cell lines. Selectivity values were obtained by using mammalian cell lines expressing the human adenosine A1, A2A and A3 receptors.
ChEMBL 458 8 2 9 5.0 O=C(c1cccs1)c1nc(NCc2cccnc2)nc2cc(NCc3cccnc3)sc12 nan
CHEMBL3922797 146552 None 0 Human Functional pIC50 = 7.2 7.2 3 4
Fluorometric Imaging Plate Reader (FLIPR) Asssay: The use of a Fluorometric Imaging Plate Reader (FLIPR) to measure calcium flux in Adenosine-receptor expressing cells is a well-established technique. In this assay calcium flux is triggered by receptor activation and measured through the fluorescence of an incorporated calcium-sensitive dye. The potencies shown were determined using expressed human adenosine A2B receptors in mammalian cell lines. Selectivity values were obtained by using mammalian cell lines expressing the human adenosine A1, A2A and A3 receptors.Fluorometric Imaging Plate Reader (FLIPR) Asssay: The use of a Fluorometric Imaging Plate Reader (FLIPR) to measure calcium flux in Adenosine-receptor expressing cells is a well-established technique. In this assay calcium flux is triggered by receptor activation and measured through the fluorescence of an incorporated calcium-sensitive dye. The potencies shown were determined using expressed human adenosine A2B receptors in mammalian cell lines. Selectivity values were obtained by using mammalian cell lines expressing the human adenosine A1, A2A and A3 receptors.
ChEMBL 458 8 2 9 5.0 O=C(c1cccs1)c1nc(NCc2cccnc2)nc2cc(NCc3cccnc3)sc12 nan
49797879 10664 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 358 5 2 5 3.3 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3cc[nH]c3)sc12 10.1016/j.bmcl.2010.05.056
CHEMBL1170519 10664 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 358 5 2 5 3.3 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3cc[nH]c3)sc12 10.1016/j.bmcl.2010.05.056
25230949 6005 None 0 Human Functional pIC50 = 8.2 8.2 15 4
Fluorometric Imaging Plate Reader (FLIPR) Asssay: The use of a Fluorometric Imaging Plate Reader (FLIPR) to measure calcium flux in Adenosine-receptor expressing cells is a well-established technique. In this assay calcium flux is triggered by receptor activation and measured through the fluorescence of an incorporated calcium-sensitive dye. The potencies shown were determined using expressed human adenosine A2B receptors in mammalian cell lines. Selectivity values were obtained by using mammalian cell lines expressing the human adenosine A1, A2A and A3 receptors.Fluorometric Imaging Plate Reader (FLIPR) Asssay: The use of a Fluorometric Imaging Plate Reader (FLIPR) to measure calcium flux in Adenosine-receptor expressing cells is a well-established technique. In this assay calcium flux is triggered by receptor activation and measured through the fluorescence of an incorporated calcium-sensitive dye. The potencies shown were determined using expressed human adenosine A2B receptors in mammalian cell lines. Selectivity values were obtained by using mammalian cell lines expressing the human adenosine A1, A2A and A3 receptors.
ChEMBL 367 5 2 8 3.6 Nc1cc2nc(NCc3cccnc3)nc(C(=O)c3cccs3)c2s1 nan
CHEMBL1080241 6005 None 0 Human Functional pIC50 = 8.2 8.2 15 4
Fluorometric Imaging Plate Reader (FLIPR) Asssay: The use of a Fluorometric Imaging Plate Reader (FLIPR) to measure calcium flux in Adenosine-receptor expressing cells is a well-established technique. In this assay calcium flux is triggered by receptor activation and measured through the fluorescence of an incorporated calcium-sensitive dye. The potencies shown were determined using expressed human adenosine A2B receptors in mammalian cell lines. Selectivity values were obtained by using mammalian cell lines expressing the human adenosine A1, A2A and A3 receptors.Fluorometric Imaging Plate Reader (FLIPR) Asssay: The use of a Fluorometric Imaging Plate Reader (FLIPR) to measure calcium flux in Adenosine-receptor expressing cells is a well-established technique. In this assay calcium flux is triggered by receptor activation and measured through the fluorescence of an incorporated calcium-sensitive dye. The potencies shown were determined using expressed human adenosine A2B receptors in mammalian cell lines. Selectivity values were obtained by using mammalian cell lines expressing the human adenosine A1, A2A and A3 receptors.
ChEMBL 367 5 2 8 3.6 Nc1cc2nc(NCc3cccnc3)nc(C(=O)c3cccs3)c2s1 nan
136042332 71159 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 598 8 2 9 4.6 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5c(C(F)(F)F)cc(C(F)(F)F)cc5[nH]4)nn3C)nc2n(CCC)c1=O 10.1021/jm201292w
CHEMBL1955908 71159 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 598 8 2 9 4.6 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5c(C(F)(F)F)cc(C(F)(F)F)cc5[nH]4)nn3C)nc2n(CCC)c1=O 10.1021/jm201292w
135443367 487 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptorInhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor
ChEMBL 534 9 1 10 1.8 CCCn1c2[nH]c(nc2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)N1CCN(CC1)c1ccccc1 10.1021/jm0309654
382 487 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptorInhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor
ChEMBL 534 9 1 10 1.8 CCCn1c2[nH]c(nc2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)N1CCN(CC1)c1ccccc1 10.1021/jm0309654
CHEMBL33455 487 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptorInhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor
ChEMBL 534 9 1 10 1.8 CCCn1c2[nH]c(nc2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)N1CCN(CC1)c1ccccc1 10.1021/jm0309654
51051251 69289 None 0 Human Functional pIC50 = 5.2 5.2 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 321 3 2 8 1.6 Nc1nc(NC(=O)c2ccccc2)n2nc(-c3ccco3)nc2n1 10.1021/jm101349u
CHEMBL1927634 69289 None 0 Human Functional pIC50 = 5.2 5.2 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 321 3 2 8 1.6 Nc1nc(NC(=O)c2ccccc2)n2nc(-c3ccco3)nc2n1 10.1021/jm101349u
51050844 69262 None 0 Human Functional pIC50 = 5.2 5.2 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 442 6 3 10 3.1 CC(C)(C)OC(=O)NCC1CCC(CNc2nc(N)n3nc(-c4ccco4)nc3n2)CC1 10.1021/jm101349u
CHEMBL1927427 69262 None 0 Human Functional pIC50 = 5.2 5.2 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 442 6 3 10 3.1 CC(C)(C)OC(=O)NCC1CCC(CNc2nc(N)n3nc(-c4ccco4)nc3n2)CC1 10.1021/jm101349u
145960813 161350 None 0 Human Functional pIC50 = 7.1 7.1 -1 3
Antagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assayAntagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assay
ChEMBL 339 4 2 7 4.0 Nc1nc(NCc2cccs2)nc2sc(-c3ccccc3)nc12 10.1016/j.bmc.2018.05.048
CHEMBL4125975 161350 None 0 Human Functional pIC50 = 7.1 7.1 -1 3
Antagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assayAntagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assay
ChEMBL 339 4 2 7 4.0 Nc1nc(NCc2cccs2)nc2sc(-c3ccccc3)nc12 10.1016/j.bmc.2018.05.048
54587016 60727 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Inhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 minsInhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 mins
ChEMBL 520 7 1 6 5.2 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)[C@@H]3CCN(Cc4cccc(C(F)(F)F)c4)C3)sc12 10.1016/j.bmcl.2011.02.053
CHEMBL1760890 60727 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Inhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 minsInhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 mins
ChEMBL 520 7 1 6 5.2 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)[C@@H]3CCN(Cc4cccc(C(F)(F)F)c4)C3)sc12 10.1016/j.bmcl.2011.02.053
10761800 188219 None 0 Human Functional pIC50 = 7.1 7.1 5 2
Inhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptorInhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptor
ChEMBL 372 1 2 7 2.5 Cn1c(-c2cccc(C#N)c2)nc2c(N)nc(C#CC3(O)CCCCC3)nc21 10.1021/jm990499b
CHEMBL49925 188219 None 0 Human Functional pIC50 = 7.1 7.1 5 2
Inhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptorInhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptor
ChEMBL 372 1 2 7 2.5 Cn1c(-c2cccc(C#N)c2)nc2c(N)nc(C#CC3(O)CCCCC3)nc21 10.1021/jm990499b
10688203 101725 None 0 Rat Functional pIC50 = 6.1 6.1 - 1
Inhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytesInhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytes
ChEMBL 335 1 1 5 3.3 Cn1c(-c2cccc(F)c2)nc2c(N)nc(C#CC3CCCC3)nc21 10.1021/jm990499b
CHEMBL299548 101725 None 0 Rat Functional pIC50 = 6.1 6.1 - 1
Inhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytesInhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytes
ChEMBL 335 1 1 5 3.3 Cn1c(-c2cccc(F)c2)nc2c(N)nc(C#CC3CCCC3)nc21 10.1021/jm990499b
45482082 198223 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity
ChEMBL 465 7 1 8 4.9 CCCCn1cc2c(nc(NC(=O)Cc3cccc4ccccc34)n3nc(-c4ccco4)nc23)n1 10.1016/j.bmc.2009.05.038
CHEMBL575386 198223 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity
ChEMBL 465 7 1 8 4.9 CCCCn1cc2c(nc(NC(=O)Cc3cccc4ccccc34)n3nc(-c4ccco4)nc23)n1 10.1016/j.bmc.2009.05.038
136042338 71164 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 449 8 2 9 2.8 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5ccccc5[nH]4)no3)nc2n(CCC)c1=O 10.1021/jm201292w
CHEMBL1955914 71164 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 449 8 2 9 2.8 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5ccccc5[nH]4)no3)nc2n(CCC)c1=O 10.1021/jm201292w
57402118 69781 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assayAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assay
ChEMBL 493 7 2 8 5.2 COc1ccc(NC(=O)Nc2nc3cn(CCc4ccccc4)cc3c3nc(-c4ccco4)nn23)cc1 10.1016/j.bmc.2011.11.037
CHEMBL1935749 69781 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assayAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assay
ChEMBL 493 7 2 8 5.2 COc1ccc(NC(=O)Nc2nc3cn(CCc4ccccc4)cc3c3nc(-c4ccco4)nn23)cc1 10.1016/j.bmc.2011.11.037
135546649 116636 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptorInhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor
ChEMBL 479 9 2 9 2.4 CCCn1c(=O)c2nc(-c3cc(OCC(=O)Nc4ccc(C)cc4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
CHEMBL33695 116636 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptorInhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor
ChEMBL 479 9 2 9 2.4 CCCn1c(=O)c2nc(-c3cc(OCC(=O)Nc4ccc(C)cc4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
145436760 162142 None 0 Human Functional pIC50 = 7.1 7.1 -2089 2
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 329 4 2 8 3.6 Nc1nc(NCc2cccs2)nc2sc(-c3ccco3)nc12 10.1016/j.ejmech.2018.06.020
CHEMBL4161758 162142 None 0 Human Functional pIC50 = 7.1 7.1 -2089 2
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 329 4 2 8 3.6 Nc1nc(NCc2cccs2)nc2sc(-c3ccco3)nc12 10.1016/j.ejmech.2018.06.020
10570068 185884 None 0 Rat Functional pIC50 = 6.1 6.1 - 1
Inhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytesInhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytes
ChEMBL 353 1 2 7 2.7 Cn1c(-c2cccs2)nc2c(N)nc(C#CC3(O)CCCCC3)nc21 10.1021/jm990499b
CHEMBL48683 185884 None 0 Rat Functional pIC50 = 6.1 6.1 - 1
Inhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytesInhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytes
ChEMBL 353 1 2 7 2.7 Cn1c(-c2cccs2)nc2c(N)nc(C#CC3(O)CCCCC3)nc21 10.1021/jm990499b
145962310 161368 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Antagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assayAntagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assay
ChEMBL 363 5 3 7 3.7 Nc1nc(NCCc2ccc(O)cc2)nc2sc(-c3ccccc3)nc12 10.1016/j.bmc.2018.05.048
CHEMBL4126116 161368 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Antagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assayAntagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assay
ChEMBL 363 5 3 7 3.7 Nc1nc(NCCc2ccc(O)cc2)nc2sc(-c3ccccc3)nc12 10.1016/j.bmc.2018.05.048
46882997 5640 None 0 Human Functional pIC50 = 6.1 6.1 -3 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 275 2 1 6 2.9 Cc1ccc(C(=O)c2nc(N)nc3ccsc23)s1 10.1016/j.bmcl.2009.08.040
CHEMBL1077751 5640 None 0 Human Functional pIC50 = 6.1 6.1 -3 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 275 2 1 6 2.9 Cc1ccc(C(=O)c2nc(N)nc3ccsc23)s1 10.1016/j.bmcl.2009.08.040
10807613 189496 None 0 Rat Functional pIC50 = 6.1 6.1 - 1
Inhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytesInhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytes
ChEMBL 347 1 2 6 2.7 Cn1c(-c2ccccc2)nc2c(N)nc(C#CC3(O)CCCCC3)nc21 10.1021/jm990499b
CHEMBL51394 189496 None 0 Rat Functional pIC50 = 6.1 6.1 - 1
Inhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytesInhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytes
ChEMBL 347 1 2 6 2.7 Cn1c(-c2ccccc2)nc2c(N)nc(C#CC3(O)CCCCC3)nc21 10.1021/jm990499b
127035806 137374 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Antagonist activity at human A2B adenosine receptor expressed in CHO cell membranes assessed as inhibition of NECA stimulated adenylyl cyclase activityAntagonist activity at human A2B adenosine receptor expressed in CHO cell membranes assessed as inhibition of NECA stimulated adenylyl cyclase activity
ChEMBL 425 7 2 8 3.6 O=C(Cc1ccccc1)Nc1nc(NCc2ccccc2)nc2nc(-c3ccco3)nn12 10.1016/j.ejmech.2015.12.019
CHEMBL3753079 137374 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Antagonist activity at human A2B adenosine receptor expressed in CHO cell membranes assessed as inhibition of NECA stimulated adenylyl cyclase activityAntagonist activity at human A2B adenosine receptor expressed in CHO cell membranes assessed as inhibition of NECA stimulated adenylyl cyclase activity
ChEMBL 425 7 2 8 3.6 O=C(Cc1ccccc1)Nc1nc(NCc2ccccc2)nc2nc(-c3ccco3)nn12 10.1016/j.ejmech.2015.12.019
49797853 10848 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 403 6 2 6 3.0 COc1ccc(N(CCO)C(C)=O)c2sc(NC(=O)c3ccc(F)cc3)nc12 10.1016/j.bmcl.2010.05.056
CHEMBL1172267 10848 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 403 6 2 6 3.0 COc1ccc(N(CCO)C(C)=O)c2sc(NC(=O)c3ccc(F)cc3)nc12 10.1016/j.bmcl.2010.05.056
10618828 101988 None 0 Human Functional pIC50 = 7.1 7.1 5 2
Inhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptorInhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptor
ChEMBL 365 1 2 6 2.8 Cn1c(-c2ccccc2F)nc2c(N)nc(C#CC3(O)CCCCC3)nc21 10.1021/jm990499b
CHEMBL301512 101988 None 0 Human Functional pIC50 = 7.1 7.1 5 2
Inhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptorInhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptor
ChEMBL 365 1 2 6 2.8 Cn1c(-c2ccccc2F)nc2c(N)nc(C#CC3(O)CCCCC3)nc21 10.1021/jm990499b
57393433 69791 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assayAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assay
ChEMBL 494 7 2 9 4.6 COc1ccc(NC(=O)Nc2nc3cnn(CCc4ccccc4)c3c3nc(-c4ccco4)nn23)cc1 10.1016/j.bmc.2011.11.037
CHEMBL1935758 69791 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assayAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assay
ChEMBL 494 7 2 9 4.6 COc1ccc(NC(=O)Nc2nc3cnn(CCc4ccccc4)c3c3nc(-c4ccco4)nn23)cc1 10.1016/j.bmc.2011.11.037
45481621 197909 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity
ChEMBL 491 8 1 8 5.3 CCCCn1cc2c(nc(NC(=O)C(c3ccccc3)c3ccccc3)n3nc(-c4ccco4)nc23)n1 10.1016/j.bmc.2009.05.038
CHEMBL572906 197909 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity
ChEMBL 491 8 1 8 5.3 CCCCn1cc2c(nc(NC(=O)C(c3ccccc3)c3ccccc3)n3nc(-c4ccco4)nc23)n1 10.1016/j.bmc.2009.05.038
145961937 161456 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assayAntagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assay
ChEMBL 341 4 2 9 2.8 Nc1nc(NCc2cccs2)nc2sc(-c3cnccn3)nc12 10.1016/j.bmc.2018.05.048
CHEMBL4127472 161456 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assayAntagonist activity at human A2B adenosine receptor assessed as inhibition of NECA-stimulated cAMP level after 30 mins by Alphascreen assay
ChEMBL 341 4 2 9 2.8 Nc1nc(NCc2cccs2)nc2sc(-c3cnccn3)nc12 10.1016/j.bmc.2018.05.048
57325915 74727 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Antagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulationAntagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulation
ChEMBL 362 2 0 6 3.9 O=c1c(-c2ccco2)nnc2n(-c3ccccc3)c3ccc(Cl)cc3n12 10.1021/jm201177b
CHEMBL2030708 74727 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Antagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulationAntagonist activity at human A2B receptor expressed in CHO cells assessed as inhibition of NECA-mediated cAMP accumulation
ChEMBL 362 2 0 6 3.9 O=c1c(-c2ccco2)nnc2n(-c3ccccc3)c3ccc(Cl)cc3n12 10.1021/jm201177b
49797828 10765 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 431 6 1 7 3.2 COC(=O)CN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(F)cc3)sc12 10.1016/j.bmcl.2010.05.056
CHEMBL1171525 10765 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of adenosine-induced cAMP production
ChEMBL 431 6 1 7 3.2 COC(=O)CN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(F)cc3)sc12 10.1016/j.bmcl.2010.05.056
136042343 71169 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 501 8 2 9 3.6 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5cc(Cl)c(F)cc5[nH]4)no3)nc2n(CCC)c1=O 10.1021/jm201292w
CHEMBL1955919 71169 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 501 8 2 9 3.6 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5cc(Cl)c(F)cc5[nH]4)no3)nc2n(CCC)c1=O 10.1021/jm201292w
54582166 60725 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Inhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 minsInhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 mins
ChEMBL 548 7 2 6 5.2 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)[C@@H]3CC[C@H](NC(=O)c4cccc(C(F)(F)F)c4)C3)sc12 10.1016/j.bmcl.2011.02.053
CHEMBL1760888 60725 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Inhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 minsInhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 mins
ChEMBL 548 7 2 6 5.2 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)[C@@H]3CC[C@H](NC(=O)c4cccc(C(F)(F)F)c4)C3)sc12 10.1016/j.bmcl.2011.02.053
54581143 60726 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Inhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 minsInhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 mins
ChEMBL 548 7 2 6 5.2 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)[C@@H]3CC[C@@H](NC(=O)c4cccc(C(F)(F)F)c4)C3)sc12 10.1016/j.bmcl.2011.02.053
CHEMBL1760889 60726 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Inhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 minsInhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 mins
ChEMBL 548 7 2 6 5.2 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)[C@@H]3CC[C@@H](NC(=O)c4cccc(C(F)(F)F)c4)C3)sc12 10.1016/j.bmcl.2011.02.053
53248700 60734 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Inhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 minsInhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 mins
ChEMBL 536 5 2 6 5.2 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)N3CCC(O)(c4cccc(C(F)(F)F)c4)CC3)sc12 10.1016/j.bmcl.2011.02.053
CHEMBL1760899 60734 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Inhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 minsInhibition of human adenosine A2B receptor expressed in CHO cells assessed as decrease in cellular cAMP level after 20 to 25 mins
ChEMBL 536 5 2 6 5.2 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)N3CCC(O)(c4cccc(C(F)(F)F)c4)CC3)sc12 10.1016/j.bmcl.2011.02.053
156821421 186219 None 0 Human Functional pIC50 = 8.1 8.1 -16 2
Antagonist activity at human A2bR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assayAntagonist activity at human A2bR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assay
ChEMBL 443 4 2 9 2.4 Cn1cc(-c2c(-c3ccccc3)nc(N)n3nc([C@H](O)c4ncccc4F)nc23)ccc1=O 10.1021/acsmedchemlett.1c00620
CHEMBL4873266 186219 None 0 Human Functional pIC50 = 8.1 8.1 -16 2
Antagonist activity at human A2bR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assayAntagonist activity at human A2bR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assay
ChEMBL 443 4 2 9 2.4 Cn1cc(-c2c(-c3ccccc3)nc(N)n3nc([C@H](O)c4ncccc4F)nc23)ccc1=O 10.1021/acsmedchemlett.1c00620
145436764 161987 None 0 Human Functional pIC50 = 8.1 8.1 -22 2
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 329 4 2 8 3.6 Nc1nc(NCc2ccsc2)nc2sc(-c3ccco3)nc12 10.1016/j.ejmech.2018.06.020
CHEMBL4159215 161987 None 0 Human Functional pIC50 = 8.1 8.1 -22 2
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 329 4 2 8 3.6 Nc1nc(NCc2ccsc2)nc2sc(-c3ccco3)nc12 10.1016/j.ejmech.2018.06.020
135874424 95848 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP levelsAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP levels
ChEMBL 469 8 2 8 2.9 CCCn1c(=O)c2[nH]c(-c3ccn(CC(=O)Nc4ccc(Cl)cc4)n3)nc2n(CCC)c1=O 10.1016/j.bmc.2007.11.058
CHEMBL258987 95848 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP levelsAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP levels
ChEMBL 469 8 2 8 2.9 CCCn1c(=O)c2[nH]c(-c3ccn(CC(=O)Nc4ccc(Cl)cc4)n3)nc2n(CCC)c1=O 10.1016/j.bmc.2007.11.058
136042327 71146 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 512 8 2 9 3.7 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5cc6ccccc6cc5[nH]4)nn3C)nc2n(CCC)c1=O 10.1021/jm201292w
CHEMBL1955893 71146 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 512 8 2 9 3.7 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5cc6ccccc6cc5[nH]4)nn3C)nc2n(CCC)c1=O 10.1021/jm201292w
135416058 491 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptorInhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor
ChEMBL 530 8 1 11 -0.5 C=CCn1c2=N/C(=c\3/cc([nH]n3C)OCC(=O)N3CCN(CC3)c3ccccc3)/N=c2c(=O)n(c1=O)CC=C 10.1021/jm0309654
442 491 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptorInhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor
ChEMBL 530 8 1 11 -0.5 C=CCn1c2=N/C(=c\3/cc([nH]n3C)OCC(=O)N3CCN(CC3)c3ccccc3)/N=c2c(=O)n(c1=O)CC=C 10.1021/jm0309654
CHEMBL2113342 491 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptorInhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor
ChEMBL 530 8 1 11 -0.5 C=CCn1c2=N/C(=c\3/cc([nH]n3C)OCC(=O)N3CCN(CC3)c3ccccc3)/N=c2c(=O)n(c1=O)CC=C 10.1021/jm0309654
5606 1644 None 17 Rat Functional pIC50 = 5.1 5.1 -316 7
Inhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytesInhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytes
ChEMBL 375 5 1 4 3.8 OCC[C@H]1CCCCN1C(=O)/C=C/c1c(nn2c1cccc2)c1ccccc1 10.1021/jm990499b
6439091 1644 None 17 Rat Functional pIC50 = 5.1 5.1 -316 7
Inhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytesInhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytes
ChEMBL 375 5 1 4 3.8 OCC[C@H]1CCCCN1C(=O)/C=C/c1c(nn2c1cccc2)c1ccccc1 10.1021/jm990499b
CHEMBL440115 1644 None 17 Rat Functional pIC50 = 5.1 5.1 -316 7
Inhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytesInhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytes
ChEMBL 375 5 1 4 3.8 OCC[C@H]1CCCCN1C(=O)/C=C/c1c(nn2c1cccc2)c1ccccc1 10.1021/jm990499b
145436769 162804 None 0 Human Functional pIC50 = 7.1 7.1 -2041 2
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 313 4 2 8 3.1 Nc1nc(NCc2ccco2)nc2sc(-c3ccco3)nc12 10.1016/j.ejmech.2018.06.020
CHEMBL4172399 162804 None 0 Human Functional pIC50 = 7.1 7.1 -2041 2
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 313 4 2 8 3.1 Nc1nc(NCc2ccco2)nc2sc(-c3ccco3)nc12 10.1016/j.ejmech.2018.06.020
56950235 69779 None 0 Human Functional pIC50 = 6.1 6.1 -10 2
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assayAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assay
ChEMBL 403 4 2 8 3.5 COc1ccc(NC(=O)Nc2nc3cn(C)cc3c3nc(-c4ccco4)nn23)cc1 10.1016/j.bmc.2011.11.037
CHEMBL1935747 69779 None 0 Human Functional pIC50 = 6.1 6.1 -10 2
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assayAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assay
ChEMBL 403 4 2 8 3.5 COc1ccc(NC(=O)Nc2nc3cn(C)cc3c3nc(-c4ccco4)nn23)cc1 10.1016/j.bmc.2011.11.037
57400353 69798 None 0 Human Functional pIC50 = 6.1 6.1 -3 2
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assayAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assay
ChEMBL 432 6 2 9 3.8 CCCn1cc2nc(NC(=O)Nc3ccc(OC)cc3)n3nc(-c4ccco4)nc3c2n1 10.1016/j.bmc.2011.11.037
CHEMBL1935765 69798 None 0 Human Functional pIC50 = 6.1 6.1 -3 2
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assayAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assay
ChEMBL 432 6 2 9 3.8 CCCn1cc2nc(NC(=O)Nc3ccc(OC)cc3)n3nc(-c4ccco4)nc3c2n1 10.1016/j.bmc.2011.11.037
45481771 197961 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity
ChEMBL 491 8 1 8 5.4 CCCCn1cc2c(nc(NC(=O)Cc3ccc(-c4ccccc4)cc3)n3nc(-c4ccco4)nc23)n1 10.1016/j.bmc.2009.05.038
CHEMBL573360 197961 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity
ChEMBL 491 8 1 8 5.4 CCCCn1cc2c(nc(NC(=O)Cc3ccc(-c4ccccc4)cc3)n3nc(-c4ccco4)nc23)n1 10.1016/j.bmc.2009.05.038
46883207 5979 None 0 Human Functional pIC50 = 6.1 6.1 2 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 347 5 1 7 3.3 O=C(c1ccncc1)c1nc(NCc2cccnc2)nc2ccsc12 10.1016/j.bmcl.2009.08.040
CHEMBL1080067 5979 None 0 Human Functional pIC50 = 6.1 6.1 2 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 347 5 1 7 3.3 O=C(c1ccncc1)c1nc(NCc2cccnc2)nc2ccsc12 10.1016/j.bmcl.2009.08.040
135493279 100382 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 483 9 2 9 2.3 CCCn1c(=O)c2nc(-c3cc(OCC(=O)Nc4ccc(F)cc4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm201292w
CHEMBL289903 100382 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 483 9 2 9 2.3 CCCn1c(=O)c2nc(-c3cc(OCC(=O)Nc4ccc(F)cc4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm201292w
135493279 100382 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptorInhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor
ChEMBL 483 9 2 9 2.3 CCCn1c(=O)c2nc(-c3cc(OCC(=O)Nc4ccc(F)cc4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
CHEMBL289903 100382 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptorInhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor
ChEMBL 483 9 2 9 2.3 CCCn1c(=O)c2nc(-c3cc(OCC(=O)Nc4ccc(F)cc4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
45481759 198343 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity
ChEMBL 505 8 1 8 5.6 CC(C)CCn1cc2c(nc(NC(=O)Cc3ccc(-c4ccccc4)cc3)n3nc(-c4ccco4)nc23)n1 10.1016/j.bmc.2009.05.038
CHEMBL576351 198343 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity
ChEMBL 505 8 1 8 5.6 CC(C)CCn1cc2c(nc(NC(=O)Cc3ccc(-c4ccccc4)cc3)n3nc(-c4ccco4)nc23)n1 10.1016/j.bmc.2009.05.038
45481753 198863 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity
ChEMBL 407 4 1 8 3.1 Cn1cc2c(nc(NC(=O)Cc3cccc(Cl)c3)n3nc(-c4ccco4)nc23)n1 10.1016/j.bmc.2009.05.038
CHEMBL583960 198863 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity
ChEMBL 407 4 1 8 3.1 Cn1cc2c(nc(NC(=O)Cc3cccc(Cl)c3)n3nc(-c4ccco4)nc23)n1 10.1016/j.bmc.2009.05.038
56951623 71173 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 331 5 2 6 1.0 CCCn1c(=O)c2[nH]c(-c3cc(=O)[nH]n3C)cc2n(CCC)c1=O 10.1021/jm201292w
CHEMBL1955923 71173 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 331 5 2 6 1.0 CCCn1c(=O)c2[nH]c(-c3cc(=O)[nH]n3C)cc2n(CCC)c1=O 10.1021/jm201292w
156821390 185236 None 0 Human Functional pIC50 = 8.0 8.0 -30 2
Antagonist activity at human A2bR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assayAntagonist activity at human A2bR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assay
ChEMBL 431 4 2 7 3.0 Nc1nc(-c2ccc(F)cc2)c(-c2ccc(=O)[nH]c2)c2nc(Cc3ccc(F)cn3)nn12 10.1021/acsmedchemlett.1c00620
CHEMBL4858144 185236 None 0 Human Functional pIC50 = 8.0 8.0 -30 2
Antagonist activity at human A2bR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assayAntagonist activity at human A2bR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assay
ChEMBL 431 4 2 7 3.0 Nc1nc(-c2ccc(F)cc2)c(-c2ccc(=O)[nH]c2)c2nc(Cc3ccc(F)cn3)nn12 10.1021/acsmedchemlett.1c00620
57398641 69776 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assayAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assay
ChEMBL 282 3 1 7 2.3 CCCn1cc2nc(N)n3nc(-c4ccco4)nc3c2c1 10.1016/j.bmc.2011.11.037
CHEMBL1935744 69776 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assayAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assay
ChEMBL 282 3 1 7 2.3 CCCn1cc2nc(N)n3nc(-c4ccco4)nc3c2c1 10.1016/j.bmc.2011.11.037
156821411 185699 None 0 Human Functional pIC50 = 7.0 7.0 -1 2
Antagonist activity at human A2bR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assayAntagonist activity at human A2bR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assay
ChEMBL 373 4 1 8 2.6 Nc1nc(-c2ccccc2)c(-c2ccnnc2)c2nc(CC3CCCO3)nn12 10.1021/acsmedchemlett.1c00620
CHEMBL4865474 185699 None 0 Human Functional pIC50 = 7.0 7.0 -1 2
Antagonist activity at human A2bR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assayAntagonist activity at human A2bR expressed in CHO-K1 cells assessed as inhibition of cAMP accumulation preincubated for 30 mins followed by adenosine addition and measured for 30 mins by HTRF assay
ChEMBL 373 4 1 8 2.6 Nc1nc(-c2ccccc2)c(-c2ccnnc2)c2nc(CC3CCCO3)nn12 10.1021/acsmedchemlett.1c00620
45482086 197866 None 0 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity
ChEMBL 421 7 1 9 3.8 CCCCn1cc2c(nc(NC(=O)Cc3ccsc3)n3nc(-c4ccco4)nc23)n1 10.1016/j.bmc.2009.05.038
CHEMBL572601 197866 None 0 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity
ChEMBL 421 7 1 9 3.8 CCCCn1cc2c(nc(NC(=O)Cc3ccsc3)n3nc(-c4ccco4)nc23)n1 10.1016/j.bmc.2009.05.038
57395120 69780 None 0 Human Functional pIC50 = 6.0 6.0 -18 2
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assayAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assay
ChEMBL 431 6 2 8 4.4 CCCn1cc2nc(NC(=O)Nc3ccc(OC)cc3)n3nc(-c4ccco4)nc3c2c1 10.1016/j.bmc.2011.11.037
CHEMBL1935748 69780 None 0 Human Functional pIC50 = 6.0 6.0 -18 2
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assayAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assay
ChEMBL 431 6 2 8 4.4 CCCn1cc2nc(NC(=O)Nc3ccc(OC)cc3)n3nc(-c4ccco4)nc3c2c1 10.1016/j.bmc.2011.11.037
145949481 162830 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 343 4 2 8 3.9 Cc1ccc(-c2nc3c(N)nc(NCc4cccs4)nc3s2)o1 10.1016/j.ejmech.2018.06.020
CHEMBL4172715 162830 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 343 4 2 8 3.9 Cc1ccc(-c2nc3c(N)nc(NCc4cccs4)nc3s2)o1 10.1016/j.ejmech.2018.06.020
45482094 197839 None 0 Human Functional pIC50 = 5.0 5.0 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity
ChEMBL 497 7 1 8 4.8 O=C(Cc1cccc(Cl)c1)Nc1nc2nn(CCc3ccccc3)cc2c2nc(-c3ccco3)nn12 10.1016/j.bmc.2009.05.038
CHEMBL572386 197839 None 0 Human Functional pIC50 = 5.0 5.0 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity
ChEMBL 497 7 1 8 4.8 O=C(Cc1cccc(Cl)c1)Nc1nc2nn(CCc3ccccc3)cc2c2nc(-c3ccco3)nn12 10.1016/j.bmc.2009.05.038
57391695 69801 None 0 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assayAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assay
ChEMBL 337 3 1 8 3.0 Cn1ncc2nc(NC3CCCCC3)n3nc(-c4ccco4)nc3c21 10.1016/j.bmc.2011.11.037
CHEMBL1935768 69801 None 0 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assayAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production by competition protein binding assay
ChEMBL 337 3 1 8 3.0 Cn1ncc2nc(NC3CCCCC3)n3nc(-c4ccco4)nc3c21 10.1016/j.bmc.2011.11.037
46883070 5680 None 0 Human Functional pIC50 = 7.0 7.0 1 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 367 5 1 8 3.7 Cc1ccc(C(=O)c2nc(NCc3ccncn3)nc3ccsc23)s1 10.1016/j.bmcl.2009.08.040
CHEMBL1077902 5680 None 0 Human Functional pIC50 = 7.0 7.0 1 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 367 5 1 8 3.7 Cc1ccc(C(=O)c2nc(NCc3ccncn3)nc3ccsc23)s1 10.1016/j.bmcl.2009.08.040
135443378 109637 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptorInhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor
ChEMBL 623 11 2 9 4.9 CCCn1c(=O)c2nc(-c3cc(NC(=O)Cc4ccc(OCc5ccccc5C(F)(F)F)cc4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
CHEMBL32229 109637 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptorInhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor
ChEMBL 623 11 2 9 4.9 CCCn1c(=O)c2nc(-c3cc(NC(=O)Cc4ccc(OCc5ccccc5C(F)(F)F)cc4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
45481756 198208 None 0 Human Functional pIC50 = 5.0 5.0 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity
ChEMBL 393 5 1 9 3.0 CCn1cc2c(nc(NC(=O)Cc3ccsc3)n3nc(-c4ccco4)nc23)n1 10.1016/j.bmc.2009.05.038
CHEMBL575198 198208 None 0 Human Functional pIC50 = 5.0 5.0 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity
ChEMBL 393 5 1 9 3.0 CCn1cc2c(nc(NC(=O)Cc3ccsc3)n3nc(-c4ccco4)nc23)n1 10.1016/j.bmc.2009.05.038
46883072 5703 None 0 Human Functional pIC50 = 6.0 6.0 -2 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 380 6 1 7 4.3 Cc1ccc(C(=O)c2nc(NCCc3ccccn3)nc3ccsc23)s1 10.1016/j.bmcl.2009.08.040
CHEMBL1078085 5703 None 0 Human Functional pIC50 = 6.0 6.0 -2 2
Antagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHOK1 cells assessed as inhibition of calcium mobilization by FLIPR assay
ChEMBL 380 6 1 7 4.3 Cc1ccc(C(=O)c2nc(NCCc3ccccn3)nc3ccsc23)s1 10.1016/j.bmcl.2009.08.040
136042349 71149 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 480 8 2 9 2.7 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5cc(F)ccc5[nH]4)nn3C)nc2n(CCC)c1=O 10.1021/jm201292w
CHEMBL1955898 71149 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation countingAntagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting
ChEMBL 480 8 2 9 2.7 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5cc(F)ccc5[nH]4)nn3C)nc2n(CCC)c1=O 10.1021/jm201292w
135522367 110663 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptorInhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor
ChEMBL 493 8 2 10 2.0 CCCn1c(=O)c2nc(-c3cc(NC(=O)Cc4ccc5c(c4)OCO5)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
CHEMBL32591 110663 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptorInhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor
ChEMBL 493 8 2 10 2.0 CCCn1c(=O)c2nc(-c3cc(NC(=O)Cc4ccc5c(c4)OCO5)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
134133787 143488 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 397 7 2 9 3.6 COc1ccc(CCNc2nc(N)c3nc(-c4ccco4)sc3n2)cc1OC 10.1021/acs.jmedchem.6b01068
CHEMBL3898647 143488 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 397 7 2 9 3.6 COc1ccc(CCNc2nc(N)c3nc(-c4ccco4)sc3n2)cc1OC 10.1021/acs.jmedchem.6b01068
145436766 162527 None 0 Human Functional pIC50 = 7.0 7.0 -102 2
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 324 4 2 8 2.9 Nc1nc(NCc2ccccn2)nc2sc(-c3ccco3)nc12 10.1016/j.ejmech.2018.06.020
CHEMBL4167813 162527 None 0 Human Functional pIC50 = 7.0 7.0 -102 2
Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting methodInverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
ChEMBL 324 4 2 8 2.9 Nc1nc(NCc2ccccn2)nc2sc(-c3ccco3)nc12 10.1016/j.ejmech.2018.06.020
155516071 170049 None 0 Human Functional pIC50 = 5.0 5.0 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity by Glo-sensor cAMP assayAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity by Glo-sensor cAMP assay
ChEMBL 389 5 3 8 1.4 NCCC(=O)Nc1ccc(-c2cn3c(=O)n(-c4ccccc4)nc3c(N)n2)cc1 10.1021/acs.jmedchem.9b00778
CHEMBL4442908 170049 None 0 Human Functional pIC50 = 5.0 5.0 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity by Glo-sensor cAMP assayAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity by Glo-sensor cAMP assay
ChEMBL 389 5 3 8 1.4 NCCC(=O)Nc1ccc(-c2cn3c(=O)n(-c4ccccc4)nc3c(N)n2)cc1 10.1021/acs.jmedchem.9b00778
10570586 189053 None 0 Rat Functional pIC50 = 6.0 6.0 - 1
Inhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytesInhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytes
ChEMBL 361 1 2 6 3.0 Cc1cccc(-c2nc3c(N)nc(C#CC4(O)CCCCC4)nc3n2C)c1 10.1021/jm990499b
CHEMBL50950 189053 None 0 Rat Functional pIC50 = 6.0 6.0 - 1
Inhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytesInhibitory activity on N-ethylcarboxamidoadenosine (NECA)-induced glucose production in primary cultured rat hepatocytes
ChEMBL 361 1 2 6 3.0 Cc1cccc(-c2nc3c(N)nc(C#CC4(O)CCCCC4)nc3n2C)c1 10.1021/jm990499b
5606 1644 None 17 Human Functional pIC50 = 6.0 6.0 -38 7
Inhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptorInhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptor
ChEMBL 375 5 1 4 3.8 OCC[C@H]1CCCCN1C(=O)/C=C/c1c(nn2c1cccc2)c1ccccc1 10.1021/jm990499b
6439091 1644 None 17 Human Functional pIC50 = 6.0 6.0 -38 7
Inhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptorInhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptor
ChEMBL 375 5 1 4 3.8 OCC[C@H]1CCCCN1C(=O)/C=C/c1c(nn2c1cccc2)c1ccccc1 10.1021/jm990499b
CHEMBL440115 1644 None 17 Human Functional pIC50 = 6.0 6.0 -38 7
Inhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptorInhibitory activity on NECA-induced cyclic-AMP accumulation in CHO-K1 cells expressing human Adenosine A2B receptor
ChEMBL 375 5 1 4 3.8 OCC[C@H]1CCCCN1C(=O)/C=C/c1c(nn2c1cccc2)c1ccccc1 10.1021/jm990499b
44587956 174772 None 0 Rat Functional pKd = 9.3 9.3 - 0
Antagonist activity at adenosine A2B receptor in Wistar-Kyoto rat distal colon assessed as inhibition of bethanecol-induced contractionAntagonist activity at adenosine A2B receptor in Wistar-Kyoto rat distal colon assessed as inhibition of bethanecol-induced contraction
ChEMBL 554 9 3 7 4.5 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(Br)cc4)cc3)c(O)c2n(CCC)c1=O 10.1016/j.bmc.2008.09.067
CHEMBL456125 174772 None 0 Rat Functional pKd = 9.3 9.3 - 0
Antagonist activity at adenosine A2B receptor in Wistar-Kyoto rat distal colon assessed as inhibition of bethanecol-induced contractionAntagonist activity at adenosine A2B receptor in Wistar-Kyoto rat distal colon assessed as inhibition of bethanecol-induced contraction
ChEMBL 554 9 3 7 4.5 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(Br)cc4)cc3)c(O)c2n(CCC)c1=O 10.1016/j.bmc.2008.09.067
11632785 73536 None 0 Human Functional pKd = 8 8.0 - 0
Antagonist potency at cloned recombinant human adenosine A2B receptor transfected in CHO cells by cAMP assayAntagonist potency at cloned recombinant human adenosine A2B receptor transfected in CHO cells by cAMP assay
ChEMBL 404 5 2 6 2.3 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccccc4)cc3)cc2n(C)c1=O 10.1021/jm0506221
CHEMBL201721 73536 None 0 Human Functional pKd = 8 8.0 - 0
Antagonist potency at cloned recombinant human adenosine A2B receptor transfected in CHO cells by cAMP assayAntagonist potency at cloned recombinant human adenosine A2B receptor transfected in CHO cells by cAMP assay
ChEMBL 404 5 2 6 2.3 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccccc4)cc3)cc2n(C)c1=O 10.1021/jm0506221
136 3292 None 32 Rat Functional pKd = 7.9 7.9 - 1
In vitro presynaptic agonist potency at alpha-2 adrenergic receptor in rat or mouse vas deferens relative to clonidineIn vitro presynaptic agonist potency at alpha-2 adrenergic receptor in rat or mouse vas deferens relative to clonidine
ChEMBL 354 1 2 4 2.6 COC(=O)[C@@H]1[C@@H](O)CC[C@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1021/jm00360a008
223 3292 None 32 Rat Functional pKd = 7.9 7.9 - 1
In vitro presynaptic agonist potency at alpha-2 adrenergic receptor in rat or mouse vas deferens relative to clonidineIn vitro presynaptic agonist potency at alpha-2 adrenergic receptor in rat or mouse vas deferens relative to clonidine
ChEMBL 354 1 2 4 2.6 COC(=O)[C@@H]1[C@@H](O)CC[C@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1021/jm00360a008
643606 3292 None 32 Rat Functional pKd = 7.9 7.9 - 1
In vitro presynaptic agonist potency at alpha-2 adrenergic receptor in rat or mouse vas deferens relative to clonidineIn vitro presynaptic agonist potency at alpha-2 adrenergic receptor in rat or mouse vas deferens relative to clonidine
ChEMBL 354 1 2 4 2.6 COC(=O)[C@@H]1[C@@H](O)CC[C@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1021/jm00360a008
CHEMBL10347 3292 None 32 Rat Functional pKd = 7.9 7.9 - 1
In vitro presynaptic agonist potency at alpha-2 adrenergic receptor in rat or mouse vas deferens relative to clonidineIn vitro presynaptic agonist potency at alpha-2 adrenergic receptor in rat or mouse vas deferens relative to clonidine
ChEMBL 354 1 2 4 2.6 COC(=O)[C@@H]1[C@@H](O)CC[C@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1021/jm00360a008
44574165 189467 None 0 Rat Functional pKd = 8.7 8.7 - 0
Antagonist activity at adenosine A2B receptor in Wistar-Kyoto rat colon assessed as inhibition of bethanecol-induced contraction after 30 minsAntagonist activity at adenosine A2B receptor in Wistar-Kyoto rat colon assessed as inhibition of bethanecol-induced contraction after 30 mins
ChEMBL 410 4 2 7 3.0 Cn1c(=O)c2[nH]c(-c3ccc(COC(=O)Nc4ccsc4)cc3)cc2n(C)c1=O 10.1016/j.bmc.2009.03.062
CHEMBL513681 189467 None 0 Rat Functional pKd = 8.7 8.7 - 0
Antagonist activity at adenosine A2B receptor in Wistar-Kyoto rat colon assessed as inhibition of bethanecol-induced contraction after 30 minsAntagonist activity at adenosine A2B receptor in Wistar-Kyoto rat colon assessed as inhibition of bethanecol-induced contraction after 30 mins
ChEMBL 410 4 2 7 3.0 Cn1c(=O)c2[nH]c(-c3ccc(COC(=O)Nc4ccsc4)cc3)cc2n(C)c1=O 10.1016/j.bmc.2009.03.062
11684443 133159 None 0 Human Functional pKd = 8.5 8.5 - 0
Antagonist potency against adenosine A2B receptor of guinea pig thoracic aortic smooth muscleAntagonist potency against adenosine A2B receptor of guinea pig thoracic aortic smooth muscle
ChEMBL 482 5 2 6 3.0 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(Br)cc4)cc3)cc2n(C)c1=O 10.1021/jm0506221
CHEMBL370378 133159 None 0 Human Functional pKd = 8.5 8.5 - 0
Antagonist potency against adenosine A2B receptor of guinea pig thoracic aortic smooth muscleAntagonist potency against adenosine A2B receptor of guinea pig thoracic aortic smooth muscle
ChEMBL 482 5 2 6 3.0 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(Br)cc4)cc3)cc2n(C)c1=O 10.1021/jm0506221
11568001 72630 None 0 Human Functional pKd = 8.4 8.4 - 0
Antagonist potency at cloned recombinant human adenosine A2B receptor transfected in CHO cells by cAMP assayAntagonist potency at cloned recombinant human adenosine A2B receptor transfected in CHO cells by cAMP assay
ChEMBL 422 5 2 6 2.4 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(F)cc4)cc3)cc2n(C)c1=O 10.1021/jm0506221
CHEMBL199446 72630 None 0 Human Functional pKd = 8.4 8.4 - 0
Antagonist potency at cloned recombinant human adenosine A2B receptor transfected in CHO cells by cAMP assayAntagonist potency at cloned recombinant human adenosine A2B receptor transfected in CHO cells by cAMP assay
ChEMBL 422 5 2 6 2.4 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(F)cc4)cc3)cc2n(C)c1=O 10.1021/jm0506221
21874557 3996 None 51 Human Functional pKd = 7.5 7.5 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO-K1 cells by calcium mobilization-based FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHO-K1 cells by calcium mobilization-based FLIPR assay
ChEMBL 321 3 2 8 2.0 Nc1nc(c2ccco2)c2c(n1)n(nn2)Cc1ccc(c(c1)C)N 10.1021/jm800961g
5612 3996 None 51 Human Functional pKd = 7.5 7.5 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO-K1 cells by calcium mobilization-based FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHO-K1 cells by calcium mobilization-based FLIPR assay
ChEMBL 321 3 2 8 2.0 Nc1nc(c2ccco2)c2c(n1)n(nn2)Cc1ccc(c(c1)C)N 10.1021/jm800961g
CHEMBL447664 3996 None 51 Human Functional pKd = 7.5 7.5 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO-K1 cells by calcium mobilization-based FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHO-K1 cells by calcium mobilization-based FLIPR assay
ChEMBL 321 3 2 8 2.0 Nc1nc(c2ccco2)c2c(n1)n(nn2)Cc1ccc(c(c1)C)N 10.1021/jm800961g
DB06625 3996 None 51 Human Functional pKd = 7.5 7.5 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO-K1 cells by calcium mobilization-based FLIPR assayAntagonist activity at human adenosine A2B receptor expressed in CHO-K1 cells by calcium mobilization-based FLIPR assay
ChEMBL 321 3 2 8 2.0 Nc1nc(c2ccco2)c2c(n1)n(nn2)Cc1ccc(c(c1)C)N 10.1021/jm800961g
11642035 73544 None 0 Human Functional pKd = 8.3 8.3 - 0
Antagonist potency at cloned recombinant human adenosine A2B receptor transfected in CHO cells by cAMP assayAntagonist potency at cloned recombinant human adenosine A2B receptor transfected in CHO cells by cAMP assay
ChEMBL 512 6 2 7 3.0 COc1cc(OCC(=O)Nc2ccc(Br)cc2)ccc1-c1cc2c([nH]1)c(=O)n(C)c(=O)n2C 10.1021/jm0506221
CHEMBL201750 73544 None 0 Human Functional pKd = 8.3 8.3 - 0
Antagonist potency at cloned recombinant human adenosine A2B receptor transfected in CHO cells by cAMP assayAntagonist potency at cloned recombinant human adenosine A2B receptor transfected in CHO cells by cAMP assay
ChEMBL 512 6 2 7 3.0 COc1cc(OCC(=O)Nc2ccc(Br)cc2)ccc1-c1cc2c([nH]1)c(=O)n(C)c(=O)n2C 10.1021/jm0506221
11642035 73544 None 0 Human Functional pKd = 8.3 8.3 - 0
Antagonist potency against adenosine A2B receptor of guinea pig thoracic aortic smooth muscleAntagonist potency against adenosine A2B receptor of guinea pig thoracic aortic smooth muscle
ChEMBL 512 6 2 7 3.0 COc1cc(OCC(=O)Nc2ccc(Br)cc2)ccc1-c1cc2c([nH]1)c(=O)n(C)c(=O)n2C 10.1021/jm0506221
CHEMBL201750 73544 None 0 Human Functional pKd = 8.3 8.3 - 0
Antagonist potency against adenosine A2B receptor of guinea pig thoracic aortic smooth muscleAntagonist potency against adenosine A2B receptor of guinea pig thoracic aortic smooth muscle
ChEMBL 512 6 2 7 3.0 COc1cc(OCC(=O)Nc2ccc(Br)cc2)ccc1-c1cc2c([nH]1)c(=O)n(C)c(=O)n2C 10.1021/jm0506221
11568001 72630 None 0 Human Functional pKd = 8.3 8.3 - 0
Antagonist potency against adenosine A2B receptor of guinea pig thoracic aortic smooth muscleAntagonist potency against adenosine A2B receptor of guinea pig thoracic aortic smooth muscle
ChEMBL 422 5 2 6 2.4 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(F)cc4)cc3)cc2n(C)c1=O 10.1021/jm0506221
CHEMBL199446 72630 None 0 Human Functional pKd = 8.3 8.3 - 0
Antagonist potency against adenosine A2B receptor of guinea pig thoracic aortic smooth muscleAntagonist potency against adenosine A2B receptor of guinea pig thoracic aortic smooth muscle
ChEMBL 422 5 2 6 2.4 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(F)cc4)cc3)cc2n(C)c1=O 10.1021/jm0506221
11632785 73536 None 0 Human Functional pKd = 7.3 7.3 - 0
Antagonist potency against adenosine A2B receptor of guinea pig thoracic aortic smooth muscleAntagonist potency against adenosine A2B receptor of guinea pig thoracic aortic smooth muscle
ChEMBL 404 5 2 6 2.3 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccccc4)cc3)cc2n(C)c1=O 10.1021/jm0506221
CHEMBL201721 73536 None 0 Human Functional pKd = 7.3 7.3 - 0
Antagonist potency against adenosine A2B receptor of guinea pig thoracic aortic smooth muscleAntagonist potency against adenosine A2B receptor of guinea pig thoracic aortic smooth muscle
ChEMBL 404 5 2 6 2.3 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccccc4)cc3)cc2n(C)c1=O 10.1021/jm0506221
11649145 135204 None 0 Human Functional pKd = 8.2 8.2 - 0
Antagonist potency at cloned recombinant human adenosine A2B receptor transfected in CHO cells by cAMP assayAntagonist potency at cloned recombinant human adenosine A2B receptor transfected in CHO cells by cAMP assay
ChEMBL 508 8 2 6 4.8 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(-c5ccccc5)cc4)cc3)cc2n(C)c1=O 10.1021/jm0506221
CHEMBL372148 135204 None 0 Human Functional pKd = 8.2 8.2 - 0
Antagonist potency at cloned recombinant human adenosine A2B receptor transfected in CHO cells by cAMP assayAntagonist potency at cloned recombinant human adenosine A2B receptor transfected in CHO cells by cAMP assay
ChEMBL 508 8 2 6 4.8 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(-c5ccccc5)cc4)cc3)cc2n(C)c1=O 10.1021/jm0506221
11640539 140899 None 0 Human Functional pKd = 8.2 8.2 - 0
Antagonist potency at cloned recombinant human adenosine A2B receptor transfected in CHO cells by cAMP assayAntagonist potency at cloned recombinant human adenosine A2B receptor transfected in CHO cells by cAMP assay
ChEMBL 429 5 2 7 2.1 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(C#N)cc4)cc3)cc2n(C)c1=O 10.1021/jm0506221
CHEMBL382135 140899 None 0 Human Functional pKd = 8.2 8.2 - 0
Antagonist potency at cloned recombinant human adenosine A2B receptor transfected in CHO cells by cAMP assayAntagonist potency at cloned recombinant human adenosine A2B receptor transfected in CHO cells by cAMP assay
ChEMBL 429 5 2 7 2.1 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(C#N)cc4)cc3)cc2n(C)c1=O 10.1021/jm0506221
11640539 140899 None 0 Human Functional pKd = 8.1 8.1 - 0
Antagonist potency against adenosine A2B receptor of guinea pig thoracic aortic smooth muscleAntagonist potency against adenosine A2B receptor of guinea pig thoracic aortic smooth muscle
ChEMBL 429 5 2 7 2.1 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(C#N)cc4)cc3)cc2n(C)c1=O 10.1021/jm0506221
CHEMBL382135 140899 None 0 Human Functional pKd = 8.1 8.1 - 0
Antagonist potency against adenosine A2B receptor of guinea pig thoracic aortic smooth muscleAntagonist potency against adenosine A2B receptor of guinea pig thoracic aortic smooth muscle
ChEMBL 429 5 2 7 2.1 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(C#N)cc4)cc3)cc2n(C)c1=O 10.1021/jm0506221
11649145 135204 None 0 Human Functional pKd = 8.1 8.1 - 0
Antagonist potency against adenosine A2B receptor of guinea pig thoracic aortic smooth muscleAntagonist potency against adenosine A2B receptor of guinea pig thoracic aortic smooth muscle
ChEMBL 508 8 2 6 4.8 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(-c5ccccc5)cc4)cc3)cc2n(C)c1=O 10.1021/jm0506221
CHEMBL372148 135204 None 0 Human Functional pKd = 8.1 8.1 - 0
Antagonist potency against adenosine A2B receptor of guinea pig thoracic aortic smooth muscleAntagonist potency against adenosine A2B receptor of guinea pig thoracic aortic smooth muscle
ChEMBL 508 8 2 6 4.8 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(-c5ccccc5)cc4)cc3)cc2n(C)c1=O 10.1021/jm0506221
11684443 133159 None 0 Human Functional pKd = 8.1 8.1 - 0
Antagonist potency at cloned recombinant human adenosine A2B receptor transfected in CHO cells by cAMP assayAntagonist potency at cloned recombinant human adenosine A2B receptor transfected in CHO cells by cAMP assay
ChEMBL 482 5 2 6 3.0 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(Br)cc4)cc3)cc2n(C)c1=O 10.1021/jm0506221
CHEMBL370378 133159 None 0 Human Functional pKd = 8.1 8.1 - 0
Antagonist potency at cloned recombinant human adenosine A2B receptor transfected in CHO cells by cAMP assayAntagonist potency at cloned recombinant human adenosine A2B receptor transfected in CHO cells by cAMP assay
ChEMBL 482 5 2 6 3.0 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(Br)cc4)cc3)cc2n(C)c1=O 10.1021/jm0506221
52950040 19160 None 0 Human Functional pKi = 9.4 9.4 - 0
Antagonist activity at adenosien A2B receptor in human HMC-1 cells assessed as inhibition of NECA-induced IL-8 release after 6 hr by ELISAAntagonist activity at adenosien A2B receptor in human HMC-1 cells assessed as inhibition of NECA-induced IL-8 release after 6 hr by ELISA
ChEMBL 523 10 2 5 6.1 CC[C@H](NC(=O)COc1ccc2[nH]c(=O)c(-c3nccs3)c(CCc3ccccc3)c2c1)c1ccccc1 10.1016/j.bmcl.2010.10.030
CHEMBL1289569 19160 None 0 Human Functional pKi = 9.4 9.4 - 0
Antagonist activity at adenosien A2B receptor in human HMC-1 cells assessed as inhibition of NECA-induced IL-8 release after 6 hr by ELISAAntagonist activity at adenosien A2B receptor in human HMC-1 cells assessed as inhibition of NECA-induced IL-8 release after 6 hr by ELISA
ChEMBL 523 10 2 5 6.1 CC[C@H](NC(=O)COc1ccc2[nH]c(=O)c(-c3nccs3)c(CCc3ccccc3)c2c1)c1ccccc1 10.1016/j.bmcl.2010.10.030
52945195 19179 None 0 Human Functional pKi = 9.4 9.4 - 0
Antagonist activity at adenosien A2B receptor in human HMC-1 cells assessed as inhibition of NECA-induced IL-8 release after 6 hr by ELISAAntagonist activity at adenosien A2B receptor in human HMC-1 cells assessed as inhibition of NECA-induced IL-8 release after 6 hr by ELISA
ChEMBL 525 10 3 6 4.7 O=C(COc1ccc2[nH]c(=O)c(-c3nccs3)c(CCc3ccccc3)c2c1)N[C@@H](CO)c1ccccc1 10.1016/j.bmcl.2010.10.030
CHEMBL1289676 19179 None 0 Human Functional pKi = 9.4 9.4 - 0
Antagonist activity at adenosien A2B receptor in human HMC-1 cells assessed as inhibition of NECA-induced IL-8 release after 6 hr by ELISAAntagonist activity at adenosien A2B receptor in human HMC-1 cells assessed as inhibition of NECA-induced IL-8 release after 6 hr by ELISA
ChEMBL 525 10 3 6 4.7 O=C(COc1ccc2[nH]c(=O)c(-c3nccs3)c(CCc3ccccc3)c2c1)N[C@@H](CO)c1ccccc1 10.1016/j.bmcl.2010.10.030
450 2970 None 9 Human Functional pKi = 9.3 9.3 - 0
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 525 10 3 6 3.6 CC(=O)NCCNc1nc(nc2c1cc([nH]2)C(=O)N1CCN(CC1)CCCc1ccccc1)c1ccccc1 10.1016/j.ejmech.2010.04.039
454 2970 None 9 Human Functional pKi = 9.3 9.3 - 0
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 525 10 3 6 3.6 CC(=O)NCCNc1nc(nc2c1cc([nH]2)C(=O)N1CCN(CC1)CCCc1ccccc1)c1ccccc1 10.1016/j.ejmech.2010.04.039
5311041 2970 None 9 Human Functional pKi = 9.3 9.3 - 0
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 525 10 3 6 3.6 CC(=O)NCCNc1nc(nc2c1cc([nH]2)C(=O)N1CCN(CC1)CCCc1ccccc1)c1ccccc1 10.1016/j.ejmech.2010.04.039
CHEMBL485862 2970 None 9 Human Functional pKi = 9.3 9.3 - 0
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 525 10 3 6 3.6 CC(=O)NCCNc1nc(nc2c1cc([nH]2)C(=O)N1CCN(CC1)CCCc1ccccc1)c1ccccc1 10.1016/j.ejmech.2010.04.039
44574165 189467 None 0 Human Functional pKi = 9.1 9.1 - 0
Antagonist activity at Adenosine receptor subtype 2B in human RBC assessed as change in erythrocyte morphology incubated for 3 hrs with occasional gentle stirring for every 30 min measured for every 12 hrs by microscopic analysisAntagonist activity at Adenosine receptor subtype 2B in human RBC assessed as change in erythrocyte morphology incubated for 3 hrs with occasional gentle stirring for every 30 min measured for every 12 hrs by microscopic analysis
ChEMBL 410 4 2 7 3.0 Cn1c(=O)c2[nH]c(-c3ccc(COC(=O)Nc4ccsc4)cc3)cc2n(C)c1=O 10.1016/j.ejmech.2017.05.035
CHEMBL513681 189467 None 0 Human Functional pKi = 9.1 9.1 - 0
Antagonist activity at Adenosine receptor subtype 2B in human RBC assessed as change in erythrocyte morphology incubated for 3 hrs with occasional gentle stirring for every 30 min measured for every 12 hrs by microscopic analysisAntagonist activity at Adenosine receptor subtype 2B in human RBC assessed as change in erythrocyte morphology incubated for 3 hrs with occasional gentle stirring for every 30 min measured for every 12 hrs by microscopic analysis
ChEMBL 410 4 2 7 3.0 Cn1c(=O)c2[nH]c(-c3ccc(COC(=O)Nc4ccsc4)cc3)cc2n(C)c1=O 10.1016/j.ejmech.2017.05.035
66894241 157813 None 0 Human Functional pKi = 9.1 9.1 - 0
Antagonist activity at human adenosine A2B receptor expressed in HEK293 cells assessed as inhibition of cAMP productionAntagonist activity at human adenosine A2B receptor expressed in HEK293 cells assessed as inhibition of cAMP production
ChEMBL 543 8 1 8 3.6 CCCn1c(=O)c2[nH]c(-c3cnn(CC4CC(=O)N(c5ccc(C(F)(F)F)cc5)C4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2021.113907
CHEMBL4083317 157813 None 0 Human Functional pKi = 9.1 9.1 - 0
Antagonist activity at human adenosine A2B receptor expressed in HEK293 cells assessed as inhibition of cAMP productionAntagonist activity at human adenosine A2B receptor expressed in HEK293 cells assessed as inhibition of cAMP production
ChEMBL 543 8 1 8 3.6 CCCn1c(=O)c2[nH]c(-c3cnn(CC4CC(=O)N(c5ccc(C(F)(F)F)cc5)C4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2021.113907
66894241 157813 None 0 Human Functional pKi = 9.1 9.1 - 0
Antagonist activity at human adenosine receptor A2b expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP level preincubated for 15 mins followed by NECA stimulation for 15 mins by HTRF assayAntagonist activity at human adenosine receptor A2b expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP level preincubated for 15 mins followed by NECA stimulation for 15 mins by HTRF assay
ChEMBL 543 8 1 8 3.6 CCCn1c(=O)c2[nH]c(-c3cnn(CC4CC(=O)N(c5ccc(C(F)(F)F)cc5)C4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2016.11.007
CHEMBL4083317 157813 None 0 Human Functional pKi = 9.1 9.1 - 0
Antagonist activity at human adenosine receptor A2b expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP level preincubated for 15 mins followed by NECA stimulation for 15 mins by HTRF assayAntagonist activity at human adenosine receptor A2b expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP level preincubated for 15 mins followed by NECA stimulation for 15 mins by HTRF assay
ChEMBL 543 8 1 8 3.6 CCCn1c(=O)c2[nH]c(-c3cnn(CC4CC(=O)N(c5ccc(C(F)(F)F)cc5)C4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2016.11.007
52946453 19223 None 0 Human Functional pKi = 9 9.0 - 0
Antagonist activity at adenosien A2B receptor in human HMC-1 cells assessed as inhibition of NECA-induced IL-8 release after 6 hr by ELISAAntagonist activity at adenosien A2B receptor in human HMC-1 cells assessed as inhibition of NECA-induced IL-8 release after 6 hr by ELISA
ChEMBL 521 9 2 5 5.6 O=C(COc1ccc2[nH]c(=O)c(-c3nccs3)c(CCc3ccccc3)c2c1)NC1(c2ccccc2)CC1 10.1016/j.bmcl.2010.10.030
CHEMBL1290001 19223 None 0 Human Functional pKi = 9 9.0 - 0
Antagonist activity at adenosien A2B receptor in human HMC-1 cells assessed as inhibition of NECA-induced IL-8 release after 6 hr by ELISAAntagonist activity at adenosien A2B receptor in human HMC-1 cells assessed as inhibition of NECA-induced IL-8 release after 6 hr by ELISA
ChEMBL 521 9 2 5 5.6 O=C(COc1ccc2[nH]c(=O)c(-c3nccs3)c(CCc3ccccc3)c2c1)NC1(c2ccccc2)CC1 10.1016/j.bmcl.2010.10.030
145958145 162077 None 0 Human Functional pKi = 9.0 9.0 - 0
Antagonist activity at Adenosine receptor subtype 2B in human RBC assessed as change in erythrocyte morphology incubated for 3 hrs with occasional gentle stirring for every 30 min measured for every 12 hrs by microscopic analysisAntagonist activity at Adenosine receptor subtype 2B in human RBC assessed as change in erythrocyte morphology incubated for 3 hrs with occasional gentle stirring for every 30 min measured for every 12 hrs by microscopic analysis
ChEMBL 606 7 1 9 4.5 CCCn1c(=O)n(C)c(=O)c2[nH]c(-c3ccc(O[C@@H](C)C(=O)N4CCN(c5nc6ccc(Cl)cc6s5)CC4)cc3)cc21 10.1016/j.ejmech.2017.05.035
CHEMBL4160732 162077 None 0 Human Functional pKi = 9.0 9.0 - 0
Antagonist activity at Adenosine receptor subtype 2B in human RBC assessed as change in erythrocyte morphology incubated for 3 hrs with occasional gentle stirring for every 30 min measured for every 12 hrs by microscopic analysisAntagonist activity at Adenosine receptor subtype 2B in human RBC assessed as change in erythrocyte morphology incubated for 3 hrs with occasional gentle stirring for every 30 min measured for every 12 hrs by microscopic analysis
ChEMBL 606 7 1 9 4.5 CCCn1c(=O)n(C)c(=O)c2[nH]c(-c3ccc(O[C@@H](C)C(=O)N4CCN(c5nc6ccc(Cl)cc6s5)CC4)cc3)cc21 10.1016/j.ejmech.2017.05.035
50925499 19236 None 0 Human Functional pKi = 8.9 8.9 - 0
Antagonist activity at adenosien A2B receptor in human HMC-1 cells assessed as inhibition of NECA-induced IL-8 release after 6 hr by ELISAAntagonist activity at adenosien A2B receptor in human HMC-1 cells assessed as inhibition of NECA-induced IL-8 release after 6 hr by ELISA
ChEMBL 523 9 2 5 5.9 CC(C)(NC(=O)COc1ccc2[nH]c(=O)c(-c3nccs3)c(CCc3ccccc3)c2c1)c1ccccc1 10.1016/j.bmcl.2010.10.030
CHEMBL1290101 19236 None 0 Human Functional pKi = 8.9 8.9 - 0
Antagonist activity at adenosien A2B receptor in human HMC-1 cells assessed as inhibition of NECA-induced IL-8 release after 6 hr by ELISAAntagonist activity at adenosien A2B receptor in human HMC-1 cells assessed as inhibition of NECA-induced IL-8 release after 6 hr by ELISA
ChEMBL 523 9 2 5 5.9 CC(C)(NC(=O)COc1ccc2[nH]c(=O)c(-c3nccs3)c(CCc3ccccc3)c2c1)c1ccccc1 10.1016/j.bmcl.2010.10.030
3284 3216 None 35 Human Functional pKi = 8.9 8.9 - 1
Antagonist activity at human adenosine A2B receptor expressed in Flp-In-CHO cell membrane assessed as inhibition of NECA-induced cAMP accumulation in presence of forskolin measured after 40 mins by alpha screen LANCE assayAntagonist activity at human adenosine A2B receptor expressed in Flp-In-CHO cell membrane assessed as inhibition of NECA-induced cAMP accumulation in presence of forskolin measured after 40 mins by alpha screen LANCE assay
ChEMBL 528 6 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)c1ccc(cc1)Cl 10.1021/acs.jmedchem.0c02169
44185871 3216 None 35 Human Functional pKi = 8.9 8.9 - 1
Antagonist activity at human adenosine A2B receptor expressed in Flp-In-CHO cell membrane assessed as inhibition of NECA-induced cAMP accumulation in presence of forskolin measured after 40 mins by alpha screen LANCE assayAntagonist activity at human adenosine A2B receptor expressed in Flp-In-CHO cell membrane assessed as inhibition of NECA-induced cAMP accumulation in presence of forskolin measured after 40 mins by alpha screen LANCE assay
ChEMBL 528 6 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)c1ccc(cc1)Cl 10.1021/acs.jmedchem.0c02169
5728 3216 None 35 Human Functional pKi = 8.9 8.9 - 1
Antagonist activity at human adenosine A2B receptor expressed in Flp-In-CHO cell membrane assessed as inhibition of NECA-induced cAMP accumulation in presence of forskolin measured after 40 mins by alpha screen LANCE assayAntagonist activity at human adenosine A2B receptor expressed in Flp-In-CHO cell membrane assessed as inhibition of NECA-induced cAMP accumulation in presence of forskolin measured after 40 mins by alpha screen LANCE assay
ChEMBL 528 6 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)c1ccc(cc1)Cl 10.1021/acs.jmedchem.0c02169
CHEMBL483688 3216 None 35 Human Functional pKi = 8.9 8.9 - 1
Antagonist activity at human adenosine A2B receptor expressed in Flp-In-CHO cell membrane assessed as inhibition of NECA-induced cAMP accumulation in presence of forskolin measured after 40 mins by alpha screen LANCE assayAntagonist activity at human adenosine A2B receptor expressed in Flp-In-CHO cell membrane assessed as inhibition of NECA-induced cAMP accumulation in presence of forskolin measured after 40 mins by alpha screen LANCE assay
ChEMBL 528 6 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)c1ccc(cc1)Cl 10.1021/acs.jmedchem.0c02169
145971695 163028 None 0 Human Functional pKi = 8.9 8.9 - 0
Antagonist activity at Adenosine receptor subtype 2B in human RBC assessed as change in erythrocyte morphology incubated for 3 hrs with occasional gentle stirring for every 30 min measured for every 12 hrs by microscopic analysisAntagonist activity at Adenosine receptor subtype 2B in human RBC assessed as change in erythrocyte morphology incubated for 3 hrs with occasional gentle stirring for every 30 min measured for every 12 hrs by microscopic analysis
ChEMBL 496 5 2 6 3.4 C[C@H](Oc1ccc(-c2cc3c([nH]2)c(=O)n(C)c(=O)n3C)cc1)C(=O)Nc1ccc(Br)cc1 10.1016/j.ejmech.2017.05.035
CHEMBL4175851 163028 None 0 Human Functional pKi = 8.9 8.9 - 0
Antagonist activity at Adenosine receptor subtype 2B in human RBC assessed as change in erythrocyte morphology incubated for 3 hrs with occasional gentle stirring for every 30 min measured for every 12 hrs by microscopic analysisAntagonist activity at Adenosine receptor subtype 2B in human RBC assessed as change in erythrocyte morphology incubated for 3 hrs with occasional gentle stirring for every 30 min measured for every 12 hrs by microscopic analysis
ChEMBL 496 5 2 6 3.4 C[C@H](Oc1ccc(-c2cc3c([nH]2)c(=O)n(C)c(=O)n3C)cc1)C(=O)Nc1ccc(Br)cc1 10.1016/j.ejmech.2017.05.035
3287 2642 None 43 Human Functional pKi = 8.9 8.9 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 503 10 2 8 3.6 CCCn1c2[nH]c(nc2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C(=O)C 10.1021/jm990421v
5139184 2642 None 43 Human Functional pKi = 8.9 8.9 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 503 10 2 8 3.6 CCCn1c2[nH]c(nc2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C(=O)C 10.1021/jm990421v
CHEMBL17002 2642 None 43 Human Functional pKi = 8.9 8.9 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 503 10 2 8 3.6 CCCn1c2[nH]c(nc2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C(=O)C 10.1021/jm990421v
3287 2642 None 43 Human Functional pKi = 8.9 8.9 - 0
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 503 10 2 8 3.6 CCCn1c2[nH]c(nc2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C(=O)C 10.1016/j.ejmech.2010.04.039
5139184 2642 None 43 Human Functional pKi = 8.9 8.9 - 0
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 503 10 2 8 3.6 CCCn1c2[nH]c(nc2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C(=O)C 10.1016/j.ejmech.2010.04.039
CHEMBL17002 2642 None 43 Human Functional pKi = 8.9 8.9 - 0
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 503 10 2 8 3.6 CCCn1c2[nH]c(nc2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C(=O)C 10.1016/j.ejmech.2010.04.039
9825550 57592 None 0 Human Functional pKi = 8.8 8.8 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 461 9 2 7 3.4 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccccc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
CHEMBL16677 57592 None 0 Human Functional pKi = 8.8 8.8 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 461 9 2 7 3.4 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccccc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
10839296 58143 None 1 Human Functional pKi = 8.8 8.8 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 506 10 2 9 3.3 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccc([N+](=O)[O-])cc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
CHEMBL16787 58143 None 1 Human Functional pKi = 8.8 8.8 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 506 10 2 9 3.3 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccc([N+](=O)[O-])cc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
52943652 19252 None 0 Human Functional pKi = 8.8 8.8 - 0
Antagonist activity at adenosien A2B receptor in human HMC-1 cells assessed as inhibition of NECA-induced IL-8 release after 6 hr by ELISAAntagonist activity at adenosien A2B receptor in human HMC-1 cells assessed as inhibition of NECA-induced IL-8 release after 6 hr by ELISA
ChEMBL 509 9 2 5 5.7 C[C@H](NC(=O)COc1ccc2[nH]c(=O)c(-c3nccs3)c(CCc3ccccc3)c2c1)c1ccccc1 10.1016/j.bmcl.2010.10.030
CHEMBL1290210 19252 None 0 Human Functional pKi = 8.8 8.8 - 0
Antagonist activity at adenosien A2B receptor in human HMC-1 cells assessed as inhibition of NECA-induced IL-8 release after 6 hr by ELISAAntagonist activity at adenosien A2B receptor in human HMC-1 cells assessed as inhibition of NECA-induced IL-8 release after 6 hr by ELISA
ChEMBL 509 9 2 5 5.7 C[C@H](NC(=O)COc1ccc2[nH]c(=O)c(-c3nccs3)c(CCc3ccccc3)c2c1)c1ccccc1 10.1016/j.bmcl.2010.10.030
9846447 58761 None 0 Human Functional pKi = 8.8 8.8 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 447 7 2 7 2.9 CCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccc(C)cc4)cc3)[nH]c2n(CC)c1=O 10.1021/jm990421v
CHEMBL16866 58761 None 0 Human Functional pKi = 8.8 8.8 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 447 7 2 7 2.9 CCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccc(C)cc4)cc3)[nH]c2n(CC)c1=O 10.1021/jm990421v
44236539 156792 None 0 Human Functional pKi = 8.7 8.7 - 1
Antagonist activity at human adenosine A2B receptor expressed in HEK293 cells assessed as inhibition of NECA-induced increase in cAMP accumulation incubated for 15 mins followed by agonist treatment for 15 mins by HTRF assayAntagonist activity at human adenosine A2B receptor expressed in HEK293 cells assessed as inhibition of NECA-induced increase in cAMP accumulation incubated for 15 mins followed by agonist treatment for 15 mins by HTRF assay
ChEMBL 460 7 2 8 2.3 CCCn1c(=O)c2[nH]c(-c3cnn(CC#Cc4cccc(C(=O)O)c4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2017.04.014
CHEMBL4070936 156792 None 0 Human Functional pKi = 8.7 8.7 - 1
Antagonist activity at human adenosine A2B receptor expressed in HEK293 cells assessed as inhibition of NECA-induced increase in cAMP accumulation incubated for 15 mins followed by agonist treatment for 15 mins by HTRF assayAntagonist activity at human adenosine A2B receptor expressed in HEK293 cells assessed as inhibition of NECA-induced increase in cAMP accumulation incubated for 15 mins followed by agonist treatment for 15 mins by HTRF assay
ChEMBL 460 7 2 8 2.3 CCCn1c(=O)c2[nH]c(-c3cnn(CC#Cc4cccc(C(=O)O)c4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2017.04.014
145952391 162999 None 0 Human Functional pKi = 8.7 8.7 - 0
Antagonist activity at Adenosine receptor subtype 2B in human RBC assessed as change in erythrocyte morphology incubated for 3 hrs with occasional gentle stirring for every 30 min measured for every 12 hrs by microscopic analysisAntagonist activity at Adenosine receptor subtype 2B in human RBC assessed as change in erythrocyte morphology incubated for 3 hrs with occasional gentle stirring for every 30 min measured for every 12 hrs by microscopic analysis
ChEMBL 501 5 1 7 2.7 Cc1ccc(N2CCN(C(=O)[C@H](C)Oc3ccc(-c4cc5c([nH]4)c(=O)n(C)c(=O)n5C)cc3)CC2)cc1 10.1016/j.ejmech.2017.05.035
CHEMBL4175454 162999 None 0 Human Functional pKi = 8.7 8.7 - 0
Antagonist activity at Adenosine receptor subtype 2B in human RBC assessed as change in erythrocyte morphology incubated for 3 hrs with occasional gentle stirring for every 30 min measured for every 12 hrs by microscopic analysisAntagonist activity at Adenosine receptor subtype 2B in human RBC assessed as change in erythrocyte morphology incubated for 3 hrs with occasional gentle stirring for every 30 min measured for every 12 hrs by microscopic analysis
ChEMBL 501 5 1 7 2.7 Cc1ccc(N2CCN(C(=O)[C@H](C)Oc3ccc(-c4cc5c([nH]4)c(=O)n(C)c(=O)n5C)cc3)CC2)cc1 10.1016/j.ejmech.2017.05.035
44276476 168094 None 0 Human Functional pKi = 8.7 8.7 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 475 9 2 7 3.7 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccc(C)cc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
CHEMBL432664 168094 None 0 Human Functional pKi = 8.7 8.7 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 475 9 2 7 3.7 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccc(C)cc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
449 2643 None 52 Human Functional pKi = 8.7 8.7 1 4
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10.1021/jm990421v
453 2643 None 52 Human Functional pKi = 8.7 8.7 1 4
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10.1021/jm990421v
6603931 2643 None 52 Human Functional pKi = 8.7 8.7 1 4
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10.1021/jm990421v
CHEMBL273807 2643 None 52 Human Functional pKi = 8.7 8.7 1 4
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10.1021/jm990421v
449 2643 None 52 Human Functional pKi = 8.7 8.7 1 4
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10.1016/j.ejmech.2010.04.039
453 2643 None 52 Human Functional pKi = 8.7 8.7 1 4
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10.1016/j.ejmech.2010.04.039
6603931 2643 None 52 Human Functional pKi = 8.7 8.7 1 4
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10.1016/j.ejmech.2010.04.039
CHEMBL273807 2643 None 52 Human Functional pKi = 8.7 8.7 1 4
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10.1016/j.ejmech.2010.04.039
52948915 19295 None 0 Human Functional pKi = 8 8.0 - 0
Antagonist activity at adenosien A2B receptor in human HMC-1 cells assessed as inhibition of NECA-induced IL-8 release after 6 hr by ELISAAntagonist activity at adenosien A2B receptor in human HMC-1 cells assessed as inhibition of NECA-induced IL-8 release after 6 hr by ELISA
ChEMBL 541 9 2 5 6.0 CC(C)(NC(=O)COc1ccc2[nH]c(=O)c(-c3nccs3)c(CCc3ccc(F)cc3)c2c1)c1ccccc1 10.1016/j.bmcl.2010.10.030
CHEMBL1290437 19295 None 0 Human Functional pKi = 8 8.0 - 0
Antagonist activity at adenosien A2B receptor in human HMC-1 cells assessed as inhibition of NECA-induced IL-8 release after 6 hr by ELISAAntagonist activity at adenosien A2B receptor in human HMC-1 cells assessed as inhibition of NECA-induced IL-8 release after 6 hr by ELISA
ChEMBL 541 9 2 5 6.0 CC(C)(NC(=O)COc1ccc2[nH]c(=O)c(-c3nccs3)c(CCc3ccc(F)cc3)c2c1)c1ccccc1 10.1016/j.bmcl.2010.10.030
145982075 166483 None 0 Human Functional pKi = 6 6.0 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated adenylyl cyclase activity by [alpha-32P]ATP based assayAntagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated adenylyl cyclase activity by [alpha-32P]ATP based assay
ChEMBL 379 6 1 9 2.8 CNc1ncc(C(=O)OCc2cccc(OC)c2)c2nc(-c3ccco3)nn12 10.1016/j.ejmech.2018.08.042
CHEMBL4278340 166483 None 0 Human Functional pKi = 6 6.0 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated adenylyl cyclase activity by [alpha-32P]ATP based assayAntagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated adenylyl cyclase activity by [alpha-32P]ATP based assay
ChEMBL 379 6 1 9 2.8 CNc1ncc(C(=O)OCc2cccc(OC)c2)c2nc(-c3ccco3)nn12 10.1016/j.ejmech.2018.08.042
1329 1472 None 86 Human Functional pKi = 6 6.0 -9 8
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 10.1016/j.bmc.2009.02.030
386 1472 None 86 Human Functional pKi = 6 6.0 -9 8
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 10.1016/j.bmc.2009.02.030
CHEMBL183 1472 None 86 Human Functional pKi = 6 6.0 -9 8
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 10.1016/j.bmc.2009.02.030
DB12946 1472 None 86 Human Functional pKi = 6 6.0 -9 8
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 10.1016/j.bmc.2009.02.030
137661874 159302 None 0 Human Functional pKi = 6 6.0 - 0
Antagonist activity at human adenosine A2B receptor expressed in HEK293 cell membranes assessed as decrease in NECA/forskolin-induced cAMP level pretreated for 15 mins followed by agonist addition for 15 mins and subsequent forskolin stimulation measured after 30 minsAntagonist activity at human adenosine A2B receptor expressed in HEK293 cell membranes assessed as decrease in NECA/forskolin-induced cAMP level pretreated for 15 mins followed by agonist addition for 15 mins and subsequent forskolin stimulation measured after 30 mins
ChEMBL 405 4 2 7 3.0 COc1ccc(N2CCOCC2)c2sc(NC(=O)C3(C)CCC(O)CC3)nc12 10.1021/acs.jmedchem.6b01584
CHEMBL4099688 159302 None 0 Human Functional pKi = 6 6.0 - 0
Antagonist activity at human adenosine A2B receptor expressed in HEK293 cell membranes assessed as decrease in NECA/forskolin-induced cAMP level pretreated for 15 mins followed by agonist addition for 15 mins and subsequent forskolin stimulation measured after 30 minsAntagonist activity at human adenosine A2B receptor expressed in HEK293 cell membranes assessed as decrease in NECA/forskolin-induced cAMP level pretreated for 15 mins followed by agonist addition for 15 mins and subsequent forskolin stimulation measured after 30 mins
ChEMBL 405 4 2 7 3.0 COc1ccc(N2CCOCC2)c2sc(NC(=O)C3(C)CCC(O)CC3)nc12 10.1021/acs.jmedchem.6b01584
145980971 166535 None 0 Human Functional pKi = 5 5.0 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated adenylyl cyclase activity by [alpha-32P]ATP based assayAntagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated adenylyl cyclase activity by [alpha-32P]ATP based assay
ChEMBL 383 5 1 8 3.4 CNc1ncc(C(=O)OCc2cccc(Cl)c2)c2nc(-c3ccco3)nn12 10.1016/j.ejmech.2018.08.042
CHEMBL4279340 166535 None 0 Human Functional pKi = 5 5.0 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated adenylyl cyclase activity by [alpha-32P]ATP based assayAntagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated adenylyl cyclase activity by [alpha-32P]ATP based assay
ChEMBL 383 5 1 8 3.4 CNc1ncc(C(=O)OCc2cccc(Cl)c2)c2nc(-c3ccco3)nn12 10.1016/j.ejmech.2018.08.042
145994259 167327 None 0 Human Functional pKi = 5 5.0 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated adenylyl cyclase activity by [alpha-32P]ATP based assayAntagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated adenylyl cyclase activity by [alpha-32P]ATP based assay
ChEMBL 424 6 2 7 3.9 CNc1ncc(C(=O)NC(c2ccccc2)c2ccccc2)c2nc(-c3ccco3)nn12 10.1016/j.ejmech.2018.08.042
CHEMBL4294246 167327 None 0 Human Functional pKi = 5 5.0 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated adenylyl cyclase activity by [alpha-32P]ATP based assayAntagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated adenylyl cyclase activity by [alpha-32P]ATP based assay
ChEMBL 424 6 2 7 3.9 CNc1ncc(C(=O)NC(c2ccccc2)c2ccccc2)c2nc(-c3ccco3)nn12 10.1016/j.ejmech.2018.08.042
118707857 113235 None 0 Human Functional pKi = 5 5.0 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 315 5 1 8 2.4 CCOC(=O)c1cnc(NC(C)C)n2nc(-c3ccco3)nc12 10.1021/jm500752h
CHEMBL3314890 113235 None 0 Human Functional pKi = 5 5.0 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 315 5 1 8 2.4 CCOC(=O)c1cnc(NC(C)C)n2nc(-c3ccco3)nc12 10.1021/jm500752h
118707863 113241 None 0 Human Functional pKi = 5 5.0 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 377 6 1 8 3.5 CCOC(=O)c1cnc(NCc2ccc(C)cc2)n2nc(-c3ccco3)nc12 10.1021/jm500752h
CHEMBL3314896 113241 None 0 Human Functional pKi = 5 5.0 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 377 6 1 8 3.5 CCOC(=O)c1cnc(NCc2ccc(C)cc2)n2nc(-c3ccco3)nc12 10.1021/jm500752h
155532918 171802 None 0 Human Functional pKi = 5 5.0 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase by [alpha-32P]ATP based methodAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase by [alpha-32P]ATP based method
ChEMBL 480 6 2 10 4.0 Cn1cc2c(nc(NCC3CCC(CNC(=O)OC(C)(C)C)CC3)n3nc(-c4ccco4)nc23)n1 10.1039/C9MD00014C
CHEMBL4468152 171802 None 0 Human Functional pKi = 5 5.0 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase by [alpha-32P]ATP based methodAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase by [alpha-32P]ATP based method
ChEMBL 480 6 2 10 4.0 Cn1cc2c(nc(NCC3CCC(CNC(=O)OC(C)(C)C)CC3)n3nc(-c4ccco4)nc23)n1 10.1039/C9MD00014C
52949999 19125 None 0 Human Functional pKi = 6.0 6.0 - 0
Antagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hrAntagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hr
ChEMBL 572 9 1 5 5.1 CN(Cc1ccc(Cl)c(Cl)c1)C(=O)COc1ccc2[nH]c(=O)c(S(C)(=O)=O)c(CCc3ccccc3)c2c1 10.1016/j.bmcl.2010.10.030
CHEMBL1289343 19125 None 0 Human Functional pKi = 6.0 6.0 - 0
Antagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hrAntagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hr
ChEMBL 572 9 1 5 5.1 CN(Cc1ccc(Cl)c(Cl)c1)C(=O)COc1ccc2[nH]c(=O)c(S(C)(=O)=O)c(CCc3ccccc3)c2c1 10.1016/j.bmcl.2010.10.030
11687483 163015 None 0 Human Functional pKi = 6.0 6.0 - 0
Antagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assay
ChEMBL 253 3 1 5 2.5 CCCn1c(-c2ccccc2)nc2c(N)ncnc21 10.1016/j.ejmech.2018.03.067
CHEMBL4175631 163015 None 0 Human Functional pKi = 6.0 6.0 - 0
Antagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assay
ChEMBL 253 3 1 5 2.5 CCCn1c(-c2ccccc2)nc2c(N)ncnc21 10.1016/j.ejmech.2018.03.067
2519 779 None 86 Human Functional pKi = 5.0 5.0 -17378 8
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1016/j.ejmech.2010.04.039
2519.0 779 None 86 Human Functional pKi = 5.0 5.0 -17378 8
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1016/j.ejmech.2010.04.039
407 779 None 86 Human Functional pKi = 5.0 5.0 -17378 8
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1016/j.ejmech.2010.04.039
463 779 None 86 Human Functional pKi = 5.0 5.0 -17378 8
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1016/j.ejmech.2010.04.039
CHEMBL113 779 None 86 Human Functional pKi = 5.0 5.0 -17378 8
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1016/j.ejmech.2010.04.039
DB00201 779 None 86 Human Functional pKi = 5.0 5.0 -17378 8
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1016/j.ejmech.2010.04.039
44572292 171412 None 1 Human Functional pKi = 6.0 6.0 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 255 1 1 5 1.8 CC(C)n1c(Br)nc2c(N)ncnc21 10.1016/j.bmc.2009.02.030
CHEMBL446264 171412 None 1 Human Functional pKi = 6.0 6.0 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 255 1 1 5 1.8 CC(C)n1c(Br)nc2c(N)ncnc21 10.1016/j.bmc.2009.02.030
123683 3121 None 63 Human Functional pKi = 5.0 5.0 -1258 5
Antagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated adenylyl cyclase activity by [alpha-32P]ATP based assayAntagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated adenylyl cyclase activity by [alpha-32P]ATP based assay
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1016/j.ejmech.2018.08.042
422 3121 None 63 Human Functional pKi = 5.0 5.0 -1258 5
Antagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated adenylyl cyclase activity by [alpha-32P]ATP based assayAntagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated adenylyl cyclase activity by [alpha-32P]ATP based assay
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1016/j.ejmech.2018.08.042
CHEMBL119709 3121 None 63 Human Functional pKi = 5.0 5.0 -1258 5
Antagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated adenylyl cyclase activity by [alpha-32P]ATP based assayAntagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated adenylyl cyclase activity by [alpha-32P]ATP based assay
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1016/j.ejmech.2018.08.042
DB05511 3121 None 63 Human Functional pKi = 5.0 5.0 -1258 5
Antagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated adenylyl cyclase activity by [alpha-32P]ATP based assayAntagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated adenylyl cyclase activity by [alpha-32P]ATP based assay
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1016/j.ejmech.2018.08.042
71455624 82953 None 0 Human Functional pKi = 6.0 6.0 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 309 3 1 8 2.2 Cn1cc2c(nc(NC3CCC3)n3nc(-c4ccco4)nc23)n1 10.1021/jm300899q
CHEMBL2181159 82953 None 0 Human Functional pKi = 6.0 6.0 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 309 3 1 8 2.2 Cn1cc2c(nc(NC3CCC3)n3nc(-c4ccco4)nc23)n1 10.1021/jm300899q
22002449 113221 None 0 Human Functional pKi = 6.0 6.0 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 273 3 1 8 1.1 CCOC(=O)c1cnc(N)n2nc(-c3ccco3)nc12 10.1021/jm500752h
CHEMBL3314876 113221 None 0 Human Functional pKi = 6.0 6.0 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 273 3 1 8 1.1 CCOC(=O)c1cnc(N)n2nc(-c3ccco3)nc12 10.1021/jm500752h
823558 15244 None 9 Human Functional pKi = 7.0 7.0 - 0
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 271 2 2 6 0.8 COc1ccc2c(C)nc(NC3=NCC(=O)N3)nc2c1 10.1016/j.ejmech.2010.04.039
CHEMBL1210817 15244 None 9 Human Functional pKi = 7.0 7.0 - 0
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 271 2 2 6 0.8 COc1ccc2c(C)nc(NC3=NCC(=O)N3)nc2c1 10.1016/j.ejmech.2010.04.039
10475082 74 None 23 Human Functional pKi = 5.9 5.9 - 0
Agonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activity
ChEMBL 383 4 4 9 0.8 OC[C@H]1O[C@H]([C@]([C@@H]1O)(C)O)n1cnc2c1nc(Cl)nc2NC1CCCC1 10.1016/j.bmc.2007.09.035
5591 74 None 23 Human Functional pKi = 5.9 5.9 - 0
Agonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activity
ChEMBL 383 4 4 9 0.8 OC[C@H]1O[C@H]([C@]([C@@H]1O)(C)O)n1cnc2c1nc(Cl)nc2NC1CCCC1 10.1016/j.bmc.2007.09.035
CHEMBL251997 74 None 23 Human Functional pKi = 5.9 5.9 - 0
Agonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activity
ChEMBL 383 4 4 9 0.8 OC[C@H]1O[C@H]([C@]([C@@H]1O)(C)O)n1cnc2c1nc(Cl)nc2NC1CCCC1 10.1016/j.bmc.2007.09.035
155562044 175770 None 0 Human Functional pKi = 4.9 4.9 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase by [alpha-32P]ATP based methodAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase by [alpha-32P]ATP based method
ChEMBL 426 7 2 10 3.0 Cn1cc2c(nc(NCCCCNC(=O)OC(C)(C)C)n3nc(-c4ccco4)nc23)n1 10.1039/C9MD00014C
CHEMBL4583657 175770 None 0 Human Functional pKi = 4.9 4.9 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase by [alpha-32P]ATP based methodAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase by [alpha-32P]ATP based method
ChEMBL 426 7 2 10 3.0 Cn1cc2c(nc(NCCCCNC(=O)OC(C)(C)C)n3nc(-c4ccco4)nc23)n1 10.1039/C9MD00014C
11681113 162258 None 0 Human Functional pKi = 4.9 4.9 - 0
Antagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assay
ChEMBL 309 4 1 6 2.7 CCn1c(-c2ccccc2)nc2c(NC3CCOC3)ncnc21 10.1016/j.ejmech.2018.03.067
CHEMBL4163630 162258 None 0 Human Functional pKi = 4.9 4.9 - 0
Antagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assay
ChEMBL 309 4 1 6 2.7 CCn1c(-c2ccccc2)nc2c(NC3CCOC3)ncnc21 10.1016/j.ejmech.2018.03.067
118707845 113222 None 0 Human Functional pKi = 5.9 5.9 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 377 4 3 7 2.4 CNC(=O)c1cnc(NC(=O)Nc2ccccc2)n2nc(-c3ccco3)nc12 10.1021/jm500752h
CHEMBL3314877 113222 None 0 Human Functional pKi = 5.9 5.9 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 377 4 3 7 2.4 CNC(=O)c1cnc(NC(=O)Nc2ccccc2)n2nc(-c3ccco3)nc12 10.1021/jm500752h
44572295 189042 None 0 Human Functional pKi = 5.9 5.9 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 269 2 1 5 2.1 CCC(C)n1c(Br)nc2c(N)ncnc21 10.1016/j.bmc.2009.02.030
CHEMBL509367 189042 None 0 Human Functional pKi = 5.9 5.9 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 269 2 1 5 2.1 CCC(C)n1c(Br)nc2c(N)ncnc21 10.1016/j.bmc.2009.02.030
44447535 95006 None 0 Human Functional pKi = 4.9 4.9 - 0
Agonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activity
ChEMBL 458 5 4 11 0.2 CNC(=S)OC[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCOC4)nc(Cl)nc32)[C@](C)(O)[C@@H]1O 10.1016/j.bmc.2007.09.035
CHEMBL254896 95006 None 0 Human Functional pKi = 4.9 4.9 - 0
Agonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activity
ChEMBL 458 5 4 11 0.2 CNC(=S)OC[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCOC4)nc(Cl)nc32)[C@](C)(O)[C@@H]1O 10.1016/j.bmc.2007.09.035
71457390 82923 None 0 Human Functional pKi = 4.9 4.9 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 359 4 1 8 3.4 C[C@@H](Nc1nc2nn(C)cc2c2nc(-c3ccco3)nn12)c1ccccc1 10.1021/jm300899q
CHEMBL2180932 82923 None 0 Human Functional pKi = 4.9 4.9 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 359 4 1 8 3.4 C[C@@H](Nc1nc2nn(C)cc2c2nc(-c3ccco3)nn12)c1ccccc1 10.1021/jm300899q
49863226 15218 None 0 Human Functional pKi = 5.9 5.9 - 0
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 311 3 1 9 0.6 Nc1nc(-n2cncn2)c2nnn(Cc3ccccc3F)c2n1 10.1016/j.ejmech.2010.04.039
CHEMBL1210734 15218 None 0 Human Functional pKi = 5.9 5.9 - 0
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 311 3 1 9 0.6 Nc1nc(-n2cncn2)c2nnn(Cc3ccccc3F)c2n1 10.1016/j.ejmech.2010.04.039
22002364 113216 None 0 Human Functional pKi = 4.9 4.9 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 423 8 1 10 3.2 CCOC(=O)c1cnc(NCc2ccc(OC)c(OC)c2)n2nc(-c3ccco3)nc12 10.1021/jm500752h
CHEMBL3314871 113216 None 0 Human Functional pKi = 4.9 4.9 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 423 8 1 10 3.2 CCOC(=O)c1cnc(NCc2ccc(OC)c(OC)c2)n2nc(-c3ccco3)nc12 10.1021/jm500752h
11659363 162718 None 0 Human Functional pKi = 4.9 4.9 - 0
Antagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assay
ChEMBL 295 3 1 6 2.2 Cn1c(-c2ccccc2)nc2c(NC3CCOC3)ncnc21 10.1016/j.ejmech.2018.03.067
CHEMBL4170873 162718 None 0 Human Functional pKi = 4.9 4.9 - 0
Antagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assay
ChEMBL 295 3 1 6 2.2 Cn1c(-c2ccccc2)nc2c(NC3CCOC3)ncnc21 10.1016/j.ejmech.2018.03.067
11568203 96244 None 0 Human Functional pKi = 7.9 7.9 - 0
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 432 5 1 7 2.8 CCCn1c(=O)c2[nH]c(-c3cnn(Cc4cccc(C(F)(F)F)c4)c3)nc2n(C)c1=O 10.1016/j.ejmech.2010.04.039
CHEMBL260975 96244 None 0 Human Functional pKi = 7.9 7.9 - 0
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 432 5 1 7 2.8 CCCn1c(=O)c2[nH]c(-c3cnn(Cc4cccc(C(F)(F)F)c4)c3)nc2n(C)c1=O 10.1016/j.ejmech.2010.04.039
66892244 158932 None 0 Human Functional pKi = 7.9 7.9 - 0
Antagonist activity at human adenosine receptor A2b expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP level preincubated for 15 mins followed by NECA stimulation for 15 mins by HTRF assayAntagonist activity at human adenosine receptor A2b expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP level preincubated for 15 mins followed by NECA stimulation for 15 mins by HTRF assay
ChEMBL 491 8 1 9 2.2 CCCn1c(=O)c2[nH]c(-c3cnn(CC4CC(=O)N(c5ccc(OC)cc5)C4)c3)nc2n(CC)c1=O 10.1016/j.ejmech.2016.11.007
CHEMBL4095686 158932 None 0 Human Functional pKi = 7.9 7.9 - 0
Antagonist activity at human adenosine receptor A2b expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP level preincubated for 15 mins followed by NECA stimulation for 15 mins by HTRF assayAntagonist activity at human adenosine receptor A2b expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP level preincubated for 15 mins followed by NECA stimulation for 15 mins by HTRF assay
ChEMBL 491 8 1 9 2.2 CCCn1c(=O)c2[nH]c(-c3cnn(CC4CC(=O)N(c5ccc(OC)cc5)C4)c3)nc2n(CC)c1=O 10.1016/j.ejmech.2016.11.007
71412032 138272 None 4 Human Functional pKi = 6.9 6.9 - 0
Agonist activity at recombinant human adenosine A2B receptor assessed as cAMP accumulation preincubated for 45 mins followed by forskolin addition measured after 15 mins by protein kinase A-based assay in presence of [3H]cyclic AMP, rolipram, adenosine deaminaseAgonist activity at recombinant human adenosine A2B receptor assessed as cAMP accumulation preincubated for 45 mins followed by forskolin addition measured after 15 mins by protein kinase A-based assay in presence of [3H]cyclic AMP, rolipram, adenosine deaminase
ChEMBL 294 4 4 9 -1.4 CCNC[C@H]1O[C@@H](n2cnc3c(N)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.5b00828
CHEMBL3770601 138272 None 4 Human Functional pKi = 6.9 6.9 - 0
Agonist activity at recombinant human adenosine A2B receptor assessed as cAMP accumulation preincubated for 45 mins followed by forskolin addition measured after 15 mins by protein kinase A-based assay in presence of [3H]cyclic AMP, rolipram, adenosine deaminaseAgonist activity at recombinant human adenosine A2B receptor assessed as cAMP accumulation preincubated for 45 mins followed by forskolin addition measured after 15 mins by protein kinase A-based assay in presence of [3H]cyclic AMP, rolipram, adenosine deaminase
ChEMBL 294 4 4 9 -1.4 CCNC[C@H]1O[C@@H](n2cnc3c(N)ncnc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.5b00828
541903 57947 None 1 Human Functional pKi = 6.9 6.9 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 382 8 2 7 1.4 C=CCn1c(=O)c2nc(-c3ccc(OCC(=O)O)cc3)[nH]c2n(CC=C)c1=O 10.1021/jm990421v
CHEMBL16724 57947 None 1 Human Functional pKi = 6.9 6.9 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 382 8 2 7 1.4 C=CCn1c(=O)c2nc(-c3ccc(OCC(=O)O)cc3)[nH]c2n(CC=C)c1=O 10.1021/jm990421v
11529450 162777 None 0 Human Functional pKi = 5.8 5.8 - 0
Antagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assay
ChEMBL 293 4 1 5 3.5 CCn1c(-c2ccccc2)nc2c(NC3CCC3)ncnc21 10.1016/j.ejmech.2018.03.067
CHEMBL4171919 162777 None 0 Human Functional pKi = 5.8 5.8 - 0
Antagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assay
ChEMBL 293 4 1 5 3.5 CCn1c(-c2ccccc2)nc2c(NC3CCC3)ncnc21 10.1016/j.ejmech.2018.03.067
18440405 136619 None 0 Human Functional pKi = 5.8 5.8 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 374 6 2 6 3.2 CCCn1c(Br)nc2c(N)nc(NCCc3ccccc3)nc21 10.1039/C5MD00034C
CHEMBL3739795 136619 None 0 Human Functional pKi = 5.8 5.8 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 374 6 2 6 3.2 CCCn1c(Br)nc2c(N)nc(NCCc3ccccc3)nc21 10.1039/C5MD00034C
52943652 19252 None 0 Human Functional pKi = 7.8 7.8 - 0
Antagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hrAntagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hr
ChEMBL 509 9 2 5 5.7 C[C@H](NC(=O)COc1ccc2[nH]c(=O)c(-c3nccs3)c(CCc3ccccc3)c2c1)c1ccccc1 10.1016/j.bmcl.2010.10.030
CHEMBL1290210 19252 None 0 Human Functional pKi = 7.8 7.8 - 0
Antagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hrAntagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hr
ChEMBL 509 9 2 5 5.7 C[C@H](NC(=O)COc1ccc2[nH]c(=O)c(-c3nccs3)c(CCc3ccccc3)c2c1)c1ccccc1 10.1016/j.bmcl.2010.10.030
9871761 59483 None 0 Human Functional pKi = 7.8 7.8 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 533 11 4 9 1.2 CCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccc(CC(=O)NCCN)cc4)cc3)[nH]c2n(CC)c1=O 10.1021/jm990421v
CHEMBL17141 59483 None 0 Human Functional pKi = 7.8 7.8 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 533 11 4 9 1.2 CCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccc(CC(=O)NCCN)cc4)cc3)[nH]c2n(CC)c1=O 10.1021/jm990421v
11610869 80256 None 0 Human Functional pKi = 6.8 6.8 - 0
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 393 5 3 8 -1.0 Cn1c(=O)c2nc(-c3ccc(S(=O)(=O)NCC(=O)O)cc3)[nH]c2n(C)c1=O 10.1016/j.ejmech.2010.04.039
CHEMBL213878 80256 None 0 Human Functional pKi = 6.8 6.8 - 0
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 393 5 3 8 -1.0 Cn1c(=O)c2nc(-c3ccc(S(=O)(=O)NCC(=O)O)cc3)[nH]c2n(C)c1=O 10.1016/j.ejmech.2010.04.039
9935943 59025 None 0 Human Functional pKi = 7.8 7.8 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 505 10 3 8 3.1 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccc(C(=O)O)cc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
CHEMBL16931 59025 None 0 Human Functional pKi = 7.8 7.8 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 505 10 3 8 3.1 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccc(C(=O)O)cc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
541615 97525 None 1 Human Functional pKi = 7.8 7.8 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 385 8 2 7 1.2 CCCn1c(=O)c2nc(-c3ccc(OCC(N)=O)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
CHEMBL27043 97525 None 1 Human Functional pKi = 7.8 7.8 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 385 8 2 7 1.2 CCCn1c(=O)c2nc(-c3ccc(OCC(N)=O)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
10839228 59865 None 0 Human Functional pKi = 7.8 7.8 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 504 8 2 8 2.1 CCCn1c(=O)c2nc(-c3ccc(/C=C/C(=O)NN4C(=O)C(C)=C(C)C4=O)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
CHEMBL17294 59865 None 0 Human Functional pKi = 7.8 7.8 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 504 8 2 8 2.1 CCCn1c(=O)c2nc(-c3ccc(/C=C/C(=O)NN4C(=O)C(C)=C(C)C4=O)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
414707 203640 None 13 Human Functional pKi = 4.8 4.8 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 177 1 1 5 1.0 CC(C)n1cnc2c(N)ncnc21 10.1016/j.bmc.2009.02.030
CHEMBL67199 203640 None 13 Human Functional pKi = 4.8 4.8 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 177 1 1 5 1.0 CC(C)n1cnc2c(N)ncnc21 10.1016/j.bmc.2009.02.030
118707866 113244 None 0 Human Functional pKi = 5.8 5.8 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 397 6 1 8 3.8 CCOC(=O)c1cnc(NCc2ccc(Cl)cc2)n2nc(-c3ccco3)nc12 10.1021/jm500752h
CHEMBL3314899 113244 None 0 Human Functional pKi = 5.8 5.8 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 397 6 1 8 3.8 CCOC(=O)c1cnc(NCc2ccc(Cl)cc2)n2nc(-c3ccco3)nc12 10.1021/jm500752h
317946 15217 None 4 Human Functional pKi = 5.8 5.8 - 0
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 272 1 1 7 0.3 Cn1c(=O)c2c(nc(-c3ccccc3)n2O)n(C)c1=O 10.1016/j.ejmech.2010.04.039
CHEMBL1210733 15217 None 4 Human Functional pKi = 5.8 5.8 - 0
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 272 1 1 7 0.3 Cn1c(=O)c2c(nc(-c3ccccc3)n2O)n(C)c1=O 10.1016/j.ejmech.2010.04.039
52950206 19111 None 0 Human Functional pKi = 5.8 5.8 - 0
Antagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hrAntagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hr
ChEMBL 476 8 2 5 3.7 CS(=O)(=O)c1c(CCc2ccccc2)c2cc(OCC(=O)Nc3ccccc3)ccc2[nH]c1=O 10.1016/j.bmcl.2010.10.030
CHEMBL1289228 19111 None 0 Human Functional pKi = 5.8 5.8 - 0
Antagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hrAntagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hr
ChEMBL 476 8 2 5 3.7 CS(=O)(=O)c1c(CCc2ccccc2)c2cc(OCC(=O)Nc3ccccc3)ccc2[nH]c1=O 10.1016/j.bmcl.2010.10.030
52946113 19271 None 0 Human Functional pKi = 7.8 7.8 - 0
Antagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hrAntagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hr
ChEMBL 522 8 3 4 6.2 CC(C)(NC(=O)NCc1ccc2[nH]c(=O)c(-c3nccs3)c(CCc3ccccc3)c2c1)c1ccccc1 10.1016/j.bmcl.2010.10.030
CHEMBL1290323 19271 None 0 Human Functional pKi = 7.8 7.8 - 0
Antagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hrAntagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hr
ChEMBL 522 8 3 4 6.2 CC(C)(NC(=O)NCc1ccc2[nH]c(=O)c(-c3nccs3)c(CCc3ccccc3)c2c1)c1ccccc1 10.1016/j.bmcl.2010.10.030
CHEMBL5080823 214707 None 0 Human Functional pKi = 7.8 7.8 - 0
Antagonist activity at human adenosine A2B receptor expressed in Flp-In-CHO cell membrane assessed as inhibition of NECA-induced cAMP accumulation in presence of forskolin measured after 40 mins by alpha screen LANCE assayAntagonist activity at human adenosine A2B receptor expressed in Flp-In-CHO cell membrane assessed as inhibition of NECA-induced cAMP accumulation in presence of forskolin measured after 40 mins by alpha screen LANCE assay
ChEMBL None None None CCCn1c(=O)c2nc(C34CCC(C(=O)NCCCN=[N+]=[N-])(CC3)CC4)[nH]c2n(CCCNC(=O)c2ccc(S(=O)(=O)F)cc2)c1=O 10.1021/acs.jmedchem.0c02169
247436 180247 None 30 Human Functional pKi = 5.8 5.8 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 177 2 1 5 0.8 CCCn1cnc2c(N)ncnc21 10.1016/j.bmc.2009.02.030
247436 180247 None 30 Human Functional pKi = 5.8 5.8 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 177 2 1 5 0.8 CCCn1cnc2c(N)ncnc21 10.1039/C5MD00034C
CHEMBL475023 180247 None 30 Human Functional pKi = 5.8 5.8 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 177 2 1 5 0.8 CCCn1cnc2c(N)ncnc21 10.1016/j.bmc.2009.02.030
CHEMBL475023 180247 None 30 Human Functional pKi = 5.8 5.8 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 177 2 1 5 0.8 CCCn1cnc2c(N)ncnc21 10.1039/C5MD00034C
452612 174503 None 16 Human Functional pKi = 4.8 4.8 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 189 1 1 5 1.1 Nc1ncnc2c1ncn2C1CCC1 10.1016/j.bmc.2009.02.030
CHEMBL455493 174503 None 16 Human Functional pKi = 4.8 4.8 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 189 1 1 5 1.1 Nc1ncnc2c1ncn2C1CCC1 10.1016/j.bmc.2009.02.030
52947452 19312 None 0 Human Functional pKi = 6.8 6.8 - 0
Antagonist activity at adenosien A2B receptor in human HMC-1 cells assessed as inhibition of NECA-induced IL-8 release after 6 hr by ELISAAntagonist activity at adenosien A2B receptor in human HMC-1 cells assessed as inhibition of NECA-induced IL-8 release after 6 hr by ELISA
ChEMBL 558 9 2 5 4.7 CS(=O)(=O)c1c(CCc2ccccc2)c2cc(OCC(=O)NCc3ccc(Cl)c(Cl)c3)ccc2[nH]c1=O 10.1016/j.bmcl.2010.10.030
CHEMBL1290543 19312 None 0 Human Functional pKi = 6.8 6.8 - 0
Antagonist activity at adenosien A2B receptor in human HMC-1 cells assessed as inhibition of NECA-induced IL-8 release after 6 hr by ELISAAntagonist activity at adenosien A2B receptor in human HMC-1 cells assessed as inhibition of NECA-induced IL-8 release after 6 hr by ELISA
ChEMBL 558 9 2 5 4.7 CS(=O)(=O)c1c(CCc2ccccc2)c2cc(OCC(=O)NCc3ccc(Cl)c(Cl)c3)ccc2[nH]c1=O 10.1016/j.bmcl.2010.10.030
1892 204045 None 78 Human Functional pKi = 4.8 4.8 - 0
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 224 2 1 7 -1.6 Cn1c(=O)c2c(ncn2CCO)n(C)c1=O 10.1016/j.ejmech.2010.04.039
CHEMBL699 204045 None 78 Human Functional pKi = 4.8 4.8 - 0
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 224 2 1 7 -1.6 Cn1c(=O)c2c(ncn2CCO)n(C)c1=O 10.1016/j.ejmech.2010.04.039
127038356 136710 None 0 Human Functional pKi = 5.8 5.8 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 360 5 2 6 3.2 CCCn1c(Br)nc2c(N)nc(NCc3ccccc3)nc21 10.1039/C5MD00034C
CHEMBL3740631 136710 None 0 Human Functional pKi = 5.8 5.8 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 360 5 2 6 3.2 CCCn1c(Br)nc2c(N)nc(NCc3ccccc3)nc21 10.1039/C5MD00034C
71462774 82952 None 0 Human Functional pKi = 5.8 5.8 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 295 3 1 8 1.8 Cn1cc2c(nc(NC3CC3)n3nc(-c4ccco4)nc23)n1 10.1021/jm300899q
CHEMBL2181158 82952 None 0 Human Functional pKi = 5.8 5.8 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 295 3 1 8 1.8 Cn1cc2c(nc(NC3CC3)n3nc(-c4ccco4)nc23)n1 10.1021/jm300899q
10624626 163137 None 0 Human Functional pKi = 5.8 5.8 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 482 8 2 7 3.1 O=C(O)COc1ccc(-c2nc3c(=O)n(Cc4ccccc4)c(=O)n(Cc4ccccc4)c3[nH]2)cc1 10.1021/jm990421v
CHEMBL417812 163137 None 0 Human Functional pKi = 5.8 5.8 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 482 8 2 7 3.1 O=C(O)COc1ccc(-c2nc3c(=O)n(Cc4ccccc4)c(=O)n(Cc4ccccc4)c3[nH]2)cc1 10.1021/jm990421v
127042993 136631 None 0 Human Functional pKi = 5.8 5.8 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 333 6 1 6 4.1 CCCn1c(-c2ccco2)nc2c(NCc3ccccc3)ncnc21 10.1039/C5MD00034C
CHEMBL3739903 136631 None 0 Human Functional pKi = 5.8 5.8 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 333 6 1 6 4.1 CCCn1c(-c2ccco2)nc2c(NCc3ccccc3)ncnc21 10.1039/C5MD00034C
127042996 136754 None 0 Human Functional pKi = 5.8 5.8 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 373 7 1 5 4.0 CCCn1c(Br)nc2c(NCCCc3ccccc3)ncnc21 10.1039/C5MD00034C
CHEMBL3741012 136754 None 0 Human Functional pKi = 5.8 5.8 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 373 7 1 5 4.0 CCCn1c(Br)nc2c(NCCCc3ccccc3)ncnc21 10.1039/C5MD00034C
2840092 201049 None 43 Human Functional pKi = 5.8 5.8 - 0
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 245 3 3 4 1.6 CCOc1cccc2c(C)nc(NC(=N)N)nc12 10.1016/j.ejmech.2010.04.039
CHEMBL602578 201049 None 43 Human Functional pKi = 5.8 5.8 - 0
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 245 3 3 4 1.6 CCOc1cccc2c(C)nc(NC(=N)N)nc12 10.1016/j.ejmech.2010.04.039
135438480 162918 None 0 Human Functional pKi = 4.8 4.8 - 1
Antagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assay
ChEMBL 309 3 2 6 3.1 Cn1c(-c2ccc(O)cc2)nc2c(NC3CCCC3)ncnc21 10.1016/j.ejmech.2018.03.067
CHEMBL4174108 162918 None 0 Human Functional pKi = 4.8 4.8 - 1
Antagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assay
ChEMBL 309 3 2 6 3.1 Cn1c(-c2ccc(O)cc2)nc2c(NC3CCCC3)ncnc21 10.1016/j.ejmech.2018.03.067
135610070 72301 None 0 Human Functional pKi = 7.8 7.8 - 0
Antagonist activity against human Adenosine A2b receptorAntagonist activity against human Adenosine A2b receptor
ChEMBL 377 8 2 9 0.8 CCCn1c(=O)c2nc(-c3cc(OCC(=O)O)no3)[nH]c2n(CCC)c1=O 10.1021/jm049418o
CHEMBL198326 72301 None 0 Human Functional pKi = 7.8 7.8 - 0
Antagonist activity against human Adenosine A2b receptorAntagonist activity against human Adenosine A2b receptor
ChEMBL 377 8 2 9 0.8 CCCn1c(=O)c2nc(-c3cc(OCC(=O)O)no3)[nH]c2n(CCC)c1=O 10.1021/jm049418o
52947301 18979 None 0 Human Functional pKi = 6.7 6.7 - 0
Antagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hrAntagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hr
ChEMBL 517 9 2 4 5.8 CC(C)(NC(=O)COc1ccc2[nH]c(=O)c(-c3cccnc3)c(CCc3ccccc3)c2c1)c1ccccc1 10.1016/j.bmcl.2010.10.030
CHEMBL1287832 18979 None 0 Human Functional pKi = 6.7 6.7 - 0
Antagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hrAntagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hr
ChEMBL 517 9 2 4 5.8 CC(C)(NC(=O)COc1ccc2[nH]c(=O)c(-c3cccnc3)c(CCc3ccccc3)c2c1)c1ccccc1 10.1016/j.bmcl.2010.10.030
127042997 136881 None 0 Human Functional pKi = 5.7 5.7 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 361 8 1 6 4.5 CCCn1c(-c2ccco2)nc2c(NCCCc3ccccc3)ncnc21 10.1039/C5MD00034C
CHEMBL3742158 136881 None 0 Human Functional pKi = 5.7 5.7 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 361 8 1 6 4.5 CCCn1c(-c2ccco2)nc2c(NCCCc3ccccc3)ncnc21 10.1039/C5MD00034C
118707851 113228 None 0 Human Functional pKi = 5.7 5.7 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 392 5 2 8 3.2 CCOC(=O)c1cnc(NC(=O)Nc2ccccc2)n2nc(-c3ccco3)nc12 10.1021/jm500752h
CHEMBL3314883 113228 None 0 Human Functional pKi = 5.7 5.7 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 392 5 2 8 3.2 CCOC(=O)c1cnc(NC(=O)Nc2ccccc2)n2nc(-c3ccco3)nc12 10.1021/jm500752h
44572293 178430 None 1 Human Functional pKi = 4.7 4.7 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 191 2 1 5 1.4 CCC(C)n1cnc2c(N)ncnc21 10.1016/j.bmc.2009.02.030
CHEMBL466044 178430 None 1 Human Functional pKi = 4.7 4.7 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 191 2 1 5 1.4 CCC(C)n1cnc2c(N)ncnc21 10.1016/j.bmc.2009.02.030
66892382 159152 None 0 Human Functional pKi = 6.7 6.7 - 0
Antagonist activity at human adenosine receptor A2b expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP level preincubated for 15 mins followed by NECA stimulation for 15 mins by HTRF assayAntagonist activity at human adenosine receptor A2b expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP level preincubated for 15 mins followed by NECA stimulation for 15 mins by HTRF assay
ChEMBL 559 9 1 9 3.5 CCCn1c(=O)c2[nH]c(-c3cnn(CC4CCN(c5ccc(OC(F)(F)F)cc5)C4=O)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2016.11.007
CHEMBL4098127 159152 None 0 Human Functional pKi = 6.7 6.7 - 0
Antagonist activity at human adenosine receptor A2b expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP level preincubated for 15 mins followed by NECA stimulation for 15 mins by HTRF assayAntagonist activity at human adenosine receptor A2b expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP level preincubated for 15 mins followed by NECA stimulation for 15 mins by HTRF assay
ChEMBL 559 9 1 9 3.5 CCCn1c(=O)c2[nH]c(-c3cnn(CC4CCN(c5ccc(OC(F)(F)F)cc5)C4=O)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2016.11.007
52946159 19293 None 0 Human Functional pKi = 5.7 5.7 - 0
Antagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hrAntagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hr
ChEMBL 493 9 2 4 5.7 O=C(CCc1ccccc1)NCc1ccc2[nH]c(=O)c(-c3nccs3)c(CCc3ccccc3)c2c1 10.1016/j.bmcl.2010.10.030
CHEMBL1290435 19293 None 0 Human Functional pKi = 5.7 5.7 - 0
Antagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hrAntagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hr
ChEMBL 493 9 2 4 5.7 O=C(CCc1ccccc1)NCc1ccc2[nH]c(=O)c(-c3nccs3)c(CCc3ccccc3)c2c1 10.1016/j.bmcl.2010.10.030
52949755 19238 None 0 Human Functional pKi = 5.7 5.7 - 0
Antagonist activity at adenosien A2B receptor in human HMC-1 cells assessed as inhibition of NECA-induced IL-8 release after 6 hr by ELISAAntagonist activity at adenosien A2B receptor in human HMC-1 cells assessed as inhibition of NECA-induced IL-8 release after 6 hr by ELISA
ChEMBL 468 6 2 5 3.2 Cc1c(S(C)(=O)=O)c(=O)[nH]c2ccc(OCC(=O)NCc3ccc(Cl)c(Cl)c3)cc12 10.1016/j.bmcl.2010.10.030
CHEMBL1290103 19238 None 0 Human Functional pKi = 5.7 5.7 - 0
Antagonist activity at adenosien A2B receptor in human HMC-1 cells assessed as inhibition of NECA-induced IL-8 release after 6 hr by ELISAAntagonist activity at adenosien A2B receptor in human HMC-1 cells assessed as inhibition of NECA-induced IL-8 release after 6 hr by ELISA
ChEMBL 468 6 2 5 3.2 Cc1c(S(C)(=O)=O)c(=O)[nH]c2ccc(OCC(=O)NCc3ccc(Cl)c(Cl)c3)cc12 10.1016/j.bmcl.2010.10.030
118707865 113243 None 0 Human Functional pKi = 5.7 5.7 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 381 6 1 8 3.3 CCOC(=O)c1cnc(NCc2ccc(F)cc2)n2nc(-c3ccco3)nc12 10.1021/jm500752h
CHEMBL3314898 113243 None 0 Human Functional pKi = 5.7 5.7 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 381 6 1 8 3.3 CCOC(=O)c1cnc(NCc2ccc(F)cc2)n2nc(-c3ccco3)nc12 10.1021/jm500752h
9957239 59416 None 0 Human Functional pKi = 6.7 6.7 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 490 7 2 6 4.8 O=C(O)/C=C/c1ccc(-c2nc3c(=O)n(CC4CCCCC4)c(=O)n(CC4CCCCC4)c3[nH]2)cc1 10.1021/jm990421v
CHEMBL17103 59416 None 0 Human Functional pKi = 6.7 6.7 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 490 7 2 6 4.8 O=C(O)/C=C/c1ccc(-c2nc3c(=O)n(CC4CCCCC4)c(=O)n(CC4CCCCC4)c3[nH]2)cc1 10.1021/jm990421v
136086750 8721 None 0 Human Functional pKi = 5.7 5.7 - 0
Antagonist activity at human adenosine A2B receptor expressed in HEK293 cells assessed as inhibition of NSCA-induced cAMP accumulation pre-incubated for 15 mins by enzyme immunoassayAntagonist activity at human adenosine A2B receptor expressed in HEK293 cells assessed as inhibition of NSCA-induced cAMP accumulation pre-incubated for 15 mins by enzyme immunoassay
ChEMBL 349 3 4 6 1.9 N=C1c2c(C(N)=O)nc(-c3ccccc3O)n2CN1c1ccc(O)cc1 10.1016/j.bmc.2010.03.048
CHEMBL1095872 8721 None 0 Human Functional pKi = 5.7 5.7 - 0
Antagonist activity at human adenosine A2B receptor expressed in HEK293 cells assessed as inhibition of NSCA-induced cAMP accumulation pre-incubated for 15 mins by enzyme immunoassayAntagonist activity at human adenosine A2B receptor expressed in HEK293 cells assessed as inhibition of NSCA-induced cAMP accumulation pre-incubated for 15 mins by enzyme immunoassay
ChEMBL 349 3 4 6 1.9 N=C1c2c(C(N)=O)nc(-c3ccccc3O)n2CN1c1ccc(O)cc1 10.1016/j.bmc.2010.03.048
9912816 98434 None 0 Human Functional pKi = 8.7 8.7 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 475 10 2 7 3.1 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)NCc4ccccc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
CHEMBL275605 98434 None 0 Human Functional pKi = 8.7 8.7 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 475 10 2 7 3.1 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)NCc4ccccc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
11801496 98746 None 0 Human Functional pKi = 8.7 8.7 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 587 9 2 7 4.0 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccc(I)cc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
CHEMBL278039 98746 None 0 Human Functional pKi = 8.7 8.7 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 587 9 2 7 4.0 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccc(I)cc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
11801496 98746 None 0 Human Functional pKi = 8.7 8.7 - 0
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 587 9 2 7 4.0 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccc(I)cc4)cc3)[nH]c2n(CCC)c1=O 10.1016/j.ejmech.2010.04.039
CHEMBL278039 98746 None 0 Human Functional pKi = 8.7 8.7 - 0
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 587 9 2 7 4.0 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccc(I)cc4)cc3)[nH]c2n(CCC)c1=O 10.1016/j.ejmech.2010.04.039
10792296 98666 None 0 Human Functional pKi = 8.7 8.7 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 529 9 2 7 4.4 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccc(C(F)(F)F)cc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
CHEMBL277386 98666 None 0 Human Functional pKi = 8.7 8.7 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 529 9 2 7 4.4 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccc(C(F)(F)F)cc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
10767043 59023 None 0 Human Functional pKi = 8.7 8.7 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 479 9 2 7 3.5 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccc(F)cc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
CHEMBL16929 59023 None 0 Human Functional pKi = 8.7 8.7 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 479 9 2 7 3.5 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccc(F)cc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
10840167 59178 None 0 Human Functional pKi = 8.6 8.6 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 539 9 2 7 4.2 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccc(Br)cc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
CHEMBL17003 59178 None 0 Human Functional pKi = 8.6 8.6 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 539 9 2 7 4.2 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccc(Br)cc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
10720065 98397 None 0 Human Functional pKi = 8.6 8.6 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 495 9 2 7 4.0 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccc(Cl)cc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
CHEMBL275427 98397 None 0 Human Functional pKi = 8.6 8.6 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 495 9 2 7 4.0 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccc(Cl)cc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
9870718 59986 None 0 Human Functional pKi = 8.6 8.6 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 503 10 2 8 3.6 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccccc4C(C)=O)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
CHEMBL17341 59986 None 0 Human Functional pKi = 8.6 8.6 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 503 10 2 8 3.6 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccccc4C(C)=O)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
72197880 90798 None 0 Human Functional pKi = 8.6 8.6 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 347 4 1 5 4.7 O=C(Nc1nc(-c2ccccc2)c(-c2ccncc2)s1)c1ccco1 10.1016/j.ejmech.2013.03.020
CHEMBL2391834 90798 None 0 Human Functional pKi = 8.6 8.6 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 347 4 1 5 4.7 O=C(Nc1nc(-c2ccccc2)c(-c2ccncc2)s1)c1ccco1 10.1016/j.ejmech.2013.03.020
52945195 19179 None 0 Human Functional pKi = 8.6 8.6 - 0
Antagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hrAntagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hr
ChEMBL 525 10 3 6 4.7 O=C(COc1ccc2[nH]c(=O)c(-c3nccs3)c(CCc3ccccc3)c2c1)N[C@@H](CO)c1ccccc1 10.1016/j.bmcl.2010.10.030
CHEMBL1289676 19179 None 0 Human Functional pKi = 8.6 8.6 - 0
Antagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hrAntagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hr
ChEMBL 525 10 3 6 4.7 O=C(COc1ccc2[nH]c(=O)c(-c3nccs3)c(CCc3ccccc3)c2c1)N[C@@H](CO)c1ccccc1 10.1016/j.bmcl.2010.10.030
11849871 188829 None 2 Human Functional pKi = 6.7 6.7 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 255 2 1 5 1.6 CCCn1c(Br)nc2c(N)ncnc21 10.1016/j.bmc.2009.02.030
11849871 188829 None 2 Human Functional pKi = 6.7 6.7 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 255 2 1 5 1.6 CCCn1c(Br)nc2c(N)ncnc21 10.1016/j.ejmech.2013.10.006
11849871 188829 None 2 Human Functional pKi = 6.7 6.7 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 255 2 1 5 1.6 CCCn1c(Br)nc2c(N)ncnc21 10.1039/C5MD00034C
CHEMBL506450 188829 None 2 Human Functional pKi = 6.7 6.7 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 255 2 1 5 1.6 CCCn1c(Br)nc2c(N)ncnc21 10.1016/j.bmc.2009.02.030
CHEMBL506450 188829 None 2 Human Functional pKi = 6.7 6.7 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 255 2 1 5 1.6 CCCn1c(Br)nc2c(N)ncnc21 10.1016/j.ejmech.2013.10.006
CHEMBL506450 188829 None 2 Human Functional pKi = 6.7 6.7 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 255 2 1 5 1.6 CCCn1c(Br)nc2c(N)ncnc21 10.1039/C5MD00034C
137636304 156201 None 0 Human Functional pKi = 5.7 5.7 - 0
Antagonist activity at human adenosine A2B receptor expressed in HEK293 cell membranes assessed as decrease in NECA/forskolin-induced cAMP level pretreated for 15 mins followed by agonist addition for 15 mins and subsequent forskolin stimulation measured after 30 minsAntagonist activity at human adenosine A2B receptor expressed in HEK293 cell membranes assessed as decrease in NECA/forskolin-induced cAMP level pretreated for 15 mins followed by agonist addition for 15 mins and subsequent forskolin stimulation measured after 30 mins
ChEMBL 419 4 2 7 3.4 COc1ccc(N2CCOCC2)c2sc(NC(=O)C3(C)CCC(C)(O)CC3)nc12 10.1021/acs.jmedchem.6b01584
CHEMBL4064207 156201 None 0 Human Functional pKi = 5.7 5.7 - 0
Antagonist activity at human adenosine A2B receptor expressed in HEK293 cell membranes assessed as decrease in NECA/forskolin-induced cAMP level pretreated for 15 mins followed by agonist addition for 15 mins and subsequent forskolin stimulation measured after 30 minsAntagonist activity at human adenosine A2B receptor expressed in HEK293 cell membranes assessed as decrease in NECA/forskolin-induced cAMP level pretreated for 15 mins followed by agonist addition for 15 mins and subsequent forskolin stimulation measured after 30 mins
ChEMBL 419 4 2 7 3.4 COc1ccc(N2CCOCC2)c2sc(NC(=O)C3(C)CCC(C)(O)CC3)nc12 10.1021/acs.jmedchem.6b01584
137645935 157576 None 0 Human Functional pKi = 5.7 5.7 - 0
Antagonist activity at human adenosine A2B receptor expressed in HEK293 cell membranes assessed as decrease in NECA/forskolin-induced cAMP level pretreated for 15 mins followed by agonist addition for 15 mins and subsequent forskolin stimulation measured after 30 minsAntagonist activity at human adenosine A2B receptor expressed in HEK293 cell membranes assessed as decrease in NECA/forskolin-induced cAMP level pretreated for 15 mins followed by agonist addition for 15 mins and subsequent forskolin stimulation measured after 30 mins
ChEMBL 446 6 1 8 3.5 COc1cnc(N2CCOCC2)c2sc(NC(=O)C(C)(C)Oc3ccc(F)cc3)nc12 10.1021/acs.jmedchem.6b01584
CHEMBL4080594 157576 None 0 Human Functional pKi = 5.7 5.7 - 0
Antagonist activity at human adenosine A2B receptor expressed in HEK293 cell membranes assessed as decrease in NECA/forskolin-induced cAMP level pretreated for 15 mins followed by agonist addition for 15 mins and subsequent forskolin stimulation measured after 30 minsAntagonist activity at human adenosine A2B receptor expressed in HEK293 cell membranes assessed as decrease in NECA/forskolin-induced cAMP level pretreated for 15 mins followed by agonist addition for 15 mins and subsequent forskolin stimulation measured after 30 mins
ChEMBL 446 6 1 8 3.5 COc1cnc(N2CCOCC2)c2sc(NC(=O)C(C)(C)Oc3ccc(F)cc3)nc12 10.1021/acs.jmedchem.6b01584
22002375 113220 None 0 Human Functional pKi = 5.7 5.7 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 258 2 2 7 0.3 CNC(=O)c1cnc(N)n2nc(-c3ccco3)nc12 10.1021/jm500752h
CHEMBL3314875 113220 None 0 Human Functional pKi = 5.7 5.7 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 258 2 2 7 0.3 CNC(=O)c1cnc(N)n2nc(-c3ccco3)nc12 10.1021/jm500752h
18440417 136661 None 0 Human Functional pKi = 5.7 5.7 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 362 7 2 7 3.7 CCCn1c(-c2ccco2)nc2c(N)nc(NCCc3ccccc3)nc21 10.1039/C5MD00034C
CHEMBL3740141 136661 None 0 Human Functional pKi = 5.7 5.7 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 362 7 2 7 3.7 CCCn1c(-c2ccco2)nc2c(N)nc(NCCc3ccccc3)nc21 10.1039/C5MD00034C
118707867 113245 None 0 Human Functional pKi = 5.7 5.7 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 431 6 1 8 4.2 CCOC(=O)c1cnc(NCc2ccc(C(F)(F)F)cc2)n2nc(-c3ccco3)nc12 10.1021/jm500752h
CHEMBL3314900 113245 None 0 Human Functional pKi = 5.7 5.7 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 431 6 1 8 4.2 CCOC(=O)c1cnc(NCc2ccc(C(F)(F)F)cc2)n2nc(-c3ccco3)nc12 10.1021/jm500752h
52944930 19294 None 0 Human Functional pKi = 7.7 7.7 - 0
Antagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hrAntagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hr
ChEMBL 495 9 2 5 5.1 O=C(COc1ccc2[nH]c(=O)c(-c3nccs3)c(CCc3ccccc3)c2c1)NCc1ccccc1 10.1016/j.bmcl.2010.10.030
CHEMBL1290436 19294 None 0 Human Functional pKi = 7.7 7.7 - 0
Antagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hrAntagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hr
ChEMBL 495 9 2 5 5.1 O=C(COc1ccc2[nH]c(=O)c(-c3nccs3)c(CCc3ccccc3)c2c1)NCc1ccccc1 10.1016/j.bmcl.2010.10.030
459 2618 None 34 Human Functional pKi = 5.7 5.7 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production
ChEMBL 432 6 2 9 3.8 CCCn1cc2c(n1)nc(n1c2nc(n1)c1ccco1)NC(=O)Nc1ccc(cc1)OC 10.1021/jm300323t
477 2618 None 34 Human Functional pKi = 5.7 5.7 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production
ChEMBL 432 6 2 9 3.8 CCCn1cc2c(n1)nc(n1c2nc(n1)c1ccco1)NC(=O)Nc1ccc(cc1)OC 10.1021/jm300323t
5310960 2618 None 34 Human Functional pKi = 5.7 5.7 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production
ChEMBL 432 6 2 9 3.8 CCCn1cc2c(n1)nc(n1c2nc(n1)c1ccco1)NC(=O)Nc1ccc(cc1)OC 10.1021/jm300323t
CHEMBL302765 2618 None 34 Human Functional pKi = 5.7 5.7 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production
ChEMBL 432 6 2 9 3.8 CCCn1cc2c(n1)nc(n1c2nc(n1)c1ccco1)NC(=O)Nc1ccc(cc1)OC 10.1021/jm300323t
20592013 94605 None 0 Human Functional pKi = 6.7 6.7 - 0
Agonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activity
ChEMBL 371 4 4 10 -0.7 OC[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCOC4)nc(Cl)nc32)[C@H](O)[C@@H]1O 10.1016/j.bmc.2007.09.035
CHEMBL252198 94605 None 0 Human Functional pKi = 6.7 6.7 - 0
Agonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activity
ChEMBL 371 4 4 10 -0.7 OC[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCOC4)nc(Cl)nc32)[C@H](O)[C@@H]1O 10.1016/j.bmc.2007.09.035
21874755 176892 None 1 Human Functional pKi = 5.7 5.7 - 0
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 336 4 2 8 1.8 Nc1nc(-c2ccco2)c2nnn(Cc3cccc(C(=O)O)c3)c2n1 10.1016/j.ejmech.2010.04.039
CHEMBL461656 176892 None 1 Human Functional pKi = 5.7 5.7 - 0
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 336 4 2 8 1.8 Nc1nc(-c2ccco2)c2nnn(Cc3cccc(C(=O)O)c3)c2n1 10.1016/j.ejmech.2010.04.039
71450241 82940 None 0 Human Functional pKi = 5.7 5.7 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 269 2 1 8 1.3 CNc1nc2nn(C)cc2c2nc(-c3ccco3)nn12 10.1021/jm300899q
CHEMBL2181147 82940 None 0 Human Functional pKi = 5.7 5.7 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 269 2 1 8 1.3 CNc1nc2nn(C)cc2c2nc(-c3ccco3)nn12 10.1021/jm300899q
71453892 82941 None 0 Human Functional pKi = 5.7 5.7 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 283 3 1 8 1.7 CCNc1nc2nn(C)cc2c2nc(-c3ccco3)nn12 10.1021/jm300899q
CHEMBL2181148 82941 None 0 Human Functional pKi = 5.7 5.7 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 283 3 1 8 1.7 CCNc1nc2nn(C)cc2c2nc(-c3ccco3)nn12 10.1021/jm300899q
24827444 96344 None 0 Human Functional pKi = 7.7 7.7 - 0
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 365 5 1 8 1.6 CCCn1c(=O)c2[nH]c(-c3cnn(-c4cccnc4)c3)nc2n(CC)c1=O 10.1016/j.ejmech.2010.04.039
CHEMBL261526 96344 None 0 Human Functional pKi = 7.7 7.7 - 0
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 365 5 1 8 1.6 CCCn1c(=O)c2[nH]c(-c3cnn(-c4cccnc4)c3)nc2n(CC)c1=O 10.1016/j.ejmech.2010.04.039
9870396 139037 None 0 Human Functional pKi = 7.7 7.7 - 0
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 494 7 1 7 4.3 CCCn1c(=O)c2nc(-c3cnn(Cc4cc(C(F)(F)F)ccc4Cl)c3)[nH]c2n(CCC)c1=O 10.1016/j.ejmech.2010.04.039
CHEMBL378598 139037 None 0 Human Functional pKi = 7.7 7.7 - 0
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 494 7 1 7 4.3 CCCn1c(=O)c2nc(-c3cnn(Cc4cc(C(F)(F)F)ccc4Cl)c3)[nH]c2n(CCC)c1=O 10.1016/j.ejmech.2010.04.039
21916394 160813 None 0 Human Functional pKi = 7.7 7.7 - 0
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 458 6 1 7 3.2 CCn1c(=O)n(CC2CC2)c(=O)c2[nH]c(-c3cnn(Cc4cccc(C(F)(F)F)c4)c3)nc21 10.1016/j.ejmech.2010.04.039
CHEMBL411452 160813 None 0 Human Functional pKi = 7.7 7.7 - 0
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 458 6 1 7 3.2 CCn1c(=O)n(CC2CC2)c(=O)c2[nH]c(-c3cnn(Cc4cccc(C(F)(F)F)c4)c3)nc21 10.1016/j.ejmech.2010.04.039
CHEMBL5074992 214350 None 0 Human Functional pKi = 7.6 7.6 - 0
Antagonist activity at human adenosine A2B receptor expressed in Flp-In-CHO cell membrane assessed as inhibition of NECA-induced cAMP accumulation in presence of forskolin measured after 40 mins by alpha screen LANCE assayAntagonist activity at human adenosine A2B receptor expressed in Flp-In-CHO cell membrane assessed as inhibition of NECA-induced cAMP accumulation in presence of forskolin measured after 40 mins by alpha screen LANCE assay
ChEMBL None None None CCCCn1c(=O)c2nc(C34CCC(C(=O)NCCOCCOCCN=[N+]=[N-])(CC3)CC4)[nH]c2n(CCCNC(=O)c2ccc(S(=O)(=O)F)cc2)c1=O 10.1021/acs.jmedchem.0c02169
9929470 110473 None 0 Human Functional pKi = 6.7 6.7 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 374 3 2 8 2.9 Cn1cc2c(nc(NC(=O)Nc3ccccc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm500752h
CHEMBL324735 110473 None 0 Human Functional pKi = 6.7 6.7 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 374 3 2 8 2.9 Cn1cc2c(nc(NC(=O)Nc3ccccc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm500752h
118707859 113237 None 0 Human Functional pKi = 5.7 5.7 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 313 5 1 8 2.1 CCOC(=O)c1cnc(NC2CC2)n2nc(-c3ccco3)nc12 10.1021/jm500752h
CHEMBL3314892 113237 None 0 Human Functional pKi = 5.7 5.7 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 313 5 1 8 2.1 CCOC(=O)c1cnc(NC2CC2)n2nc(-c3ccco3)nc12 10.1021/jm500752h
158795 3770 None 33 Human Functional pKi = 6.6 6.6 - 2
Agonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activity
ChEMBL 337 4 4 10 -1.4 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N[C@H]1COCC1 10.1016/j.bmc.2007.09.035
5592 3770 None 33 Human Functional pKi = 6.6 6.6 - 2
Agonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activity
ChEMBL 337 4 4 10 -1.4 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N[C@H]1COCC1 10.1016/j.bmc.2007.09.035
CHEMBL392149 3770 None 33 Human Functional pKi = 6.6 6.6 - 2
Agonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activity
ChEMBL 337 4 4 10 -1.4 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N[C@H]1COCC1 10.1016/j.bmc.2007.09.035
DB04954 3770 None 33 Human Functional pKi = 6.6 6.6 - 2
Agonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activity
ChEMBL 337 4 4 10 -1.4 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N[C@H]1COCC1 10.1016/j.bmc.2007.09.035
99619 203471 None 23 Human Functional pKi = 4.6 4.6 - 0
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 223 2 1 7 -1.6 Cn1c(=O)c2c(ncn2CCN)n(C)c1=O 10.1016/j.ejmech.2010.04.039
CHEMBL66011 203471 None 23 Human Functional pKi = 4.6 4.6 - 0
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 223 2 1 7 -1.6 Cn1c(=O)c2c(ncn2CCN)n(C)c1=O 10.1016/j.ejmech.2010.04.039
101874280 113232 None 0 Human Functional pKi = 5.6 5.6 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 287 4 1 8 1.6 CCOC(=O)c1cnc(NC)n2nc(-c3ccco3)nc12 10.1021/jm500752h
CHEMBL3314887 113232 None 0 Human Functional pKi = 5.6 5.6 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 287 4 1 8 1.6 CCOC(=O)c1cnc(NC)n2nc(-c3ccco3)nc12 10.1021/jm500752h
22002319 113218 None 0 Human Functional pKi = 5.6 5.6 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 408 7 2 9 2.4 CNC(=O)c1cnc(NCc2ccc(OC)c(OC)c2)n2nc(-c3ccco3)nc12 10.1021/jm500752h
CHEMBL3314873 113218 None 0 Human Functional pKi = 5.6 5.6 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 408 7 2 9 2.4 CNC(=O)c1cnc(NCc2ccc(OC)c(OC)c2)n2nc(-c3ccco3)nc12 10.1021/jm500752h
1330 163218 None 45 Human Functional pKi = 6.6 6.6 - 3
Antagonist activity against human Adenosine A2b receptorAntagonist activity against human Adenosine A2b receptor
ChEMBL 392 6 2 7 1.6 CCCn1c(=O)c2nc(-c3ccc(S(=O)(=O)O)cc3)[nH]c2n(CCC)c1=O 10.1021/jm049418o
CHEMBL418333 163218 None 45 Human Functional pKi = 6.6 6.6 - 3
Antagonist activity against human Adenosine A2b receptorAntagonist activity against human Adenosine A2b receptor
ChEMBL 392 6 2 7 1.6 CCCn1c(=O)c2nc(-c3ccc(S(=O)(=O)O)cc3)[nH]c2n(CCC)c1=O 10.1021/jm049418o
CHEMBL435575 163218 None 45 Human Functional pKi = 6.6 6.6 - 3
Antagonist activity against human Adenosine A2b receptorAntagonist activity against human Adenosine A2b receptor
ChEMBL 392 6 2 7 1.6 CCCn1c(=O)c2nc(-c3ccc(S(=O)(=O)O)cc3)[nH]c2n(CCC)c1=O 10.1021/jm049418o
9887859 113512 None 0 Human Functional pKi = 6.6 6.6 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production
ChEMBL 375 3 2 9 2.3 Cn1cc2c(nc(NC(=O)Nc3ccncc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm300323t
CHEMBL118923 113512 None 0 Human Functional pKi = 6.6 6.6 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production
ChEMBL 375 3 2 9 2.3 Cn1cc2c(nc(NC(=O)Nc3ccncc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm300323t
CHEMBL332091 113512 None 0 Human Functional pKi = 6.6 6.6 - 1
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP productionAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production
ChEMBL 375 3 2 9 2.3 Cn1cc2c(nc(NC(=O)Nc3ccncc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm300323t
76331702 103698 None 0 Human Functional pKi = 6.6 6.6 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 243 3 1 6 2.1 CCCn1c(-c2ccco2)nc2c(N)ncnc21 10.1016/j.ejmech.2013.10.006
CHEMBL3087706 103698 None 0 Human Functional pKi = 6.6 6.6 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 243 3 1 6 2.1 CCCn1c(-c2ccco2)nc2c(N)ncnc21 10.1016/j.ejmech.2013.10.006
76335304 103700 None 0 Human Functional pKi = 5.6 5.6 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 333 4 1 6 2.8 Cn1c(-c2ccco2)nc2c(NC(=O)Cc3ccccc3)ncnc21 10.1016/j.ejmech.2013.10.006
CHEMBL3087708 103700 None 0 Human Functional pKi = 5.6 5.6 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 333 4 1 6 2.8 Cn1c(-c2ccco2)nc2c(NC(=O)Cc3ccccc3)ncnc21 10.1016/j.ejmech.2013.10.006
118707862 113240 None 0 Human Functional pKi = 5.6 5.6 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 363 6 1 8 3.2 CCOC(=O)c1cnc(NCc2ccccc2)n2nc(-c3ccco3)nc12 10.1021/jm500752h
CHEMBL3314895 113240 None 0 Human Functional pKi = 5.6 5.6 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 363 6 1 8 3.2 CCOC(=O)c1cnc(NCc2ccccc2)n2nc(-c3ccco3)nc12 10.1021/jm500752h
76331702 103698 None 0 Human Functional pKi = 6.6 6.6 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 243 3 1 6 2.1 CCCn1c(-c2ccco2)nc2c(N)ncnc21 10.1039/C5MD00034C
CHEMBL3087706 103698 None 0 Human Functional pKi = 6.6 6.6 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 243 3 1 6 2.1 CCCn1c(-c2ccco2)nc2c(N)ncnc21 10.1039/C5MD00034C
11587927 162673 None 0 Human Functional pKi = 5.6 5.6 - 0
Antagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assay
ChEMBL 327 3 1 5 4.0 Cn1c(-c2cccc(Cl)c2)nc2c(NC3CCCC3)ncnc21 10.1016/j.ejmech.2018.03.067
CHEMBL4170180 162673 None 0 Human Functional pKi = 5.6 5.6 - 0
Antagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assay
ChEMBL 327 3 1 5 4.0 Cn1c(-c2cccc(Cl)c2)nc2c(NC3CCCC3)ncnc21 10.1016/j.ejmech.2018.03.067
CHEMBL5089483 215209 None 0 Human Functional pKi = 7.6 7.6 - 0
Antagonist activity at human adenosine A2B receptor expressed in Flp-In-CHO cell membrane assessed as inhibition of NECA-induced cAMP accumulation in presence of forskolin measured after 40 mins by alpha screen LANCE assayAntagonist activity at human adenosine A2B receptor expressed in Flp-In-CHO cell membrane assessed as inhibition of NECA-induced cAMP accumulation in presence of forskolin measured after 40 mins by alpha screen LANCE assay
ChEMBL None None None CCCCn1c(=O)c2nc(C34CCC(C(=O)NCCCCN=[N+]=[N-])(CC3)CC4)[nH]c2n(CCCNC(=O)c2ccc(S(=O)(=O)F)cc2)c1=O 10.1021/acs.jmedchem.0c02169
9936058 59558 None 2 Human Functional pKi = 7.6 7.6 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 508 9 2 9 1.5 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)NN4C(=O)C(C)=C(C)C4=O)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
CHEMBL17173 59558 None 2 Human Functional pKi = 7.6 7.6 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 508 9 2 9 1.5 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)NN4C(=O)C(C)=C(C)C4=O)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
377 2758 None 53 Rat Functional pKi = 5.6 5.6 - 10
Activity against Adenosine A2B receptor as cAMP production in VA-13 cellsActivity against Adenosine A2B receptor as cAMP production in VA-13 cells
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm9802822
425 2758 None 53 Rat Functional pKi = 5.6 5.6 - 10
Activity against Adenosine A2B receptor as cAMP production in VA-13 cellsActivity against Adenosine A2B receptor as cAMP production in VA-13 cells
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm9802822
448222 2758 None 53 Rat Functional pKi = 5.6 5.6 - 10
Activity against Adenosine A2B receptor as cAMP production in VA-13 cellsActivity against Adenosine A2B receptor as cAMP production in VA-13 cells
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm9802822
CHEMBL464859 2758 None 53 Rat Functional pKi = 5.6 5.6 - 10
Activity against Adenosine A2B receptor as cAMP production in VA-13 cellsActivity against Adenosine A2B receptor as cAMP production in VA-13 cells
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm9802822
71462773 82945 None 0 Human Functional pKi = 5.6 5.6 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 311 4 1 8 2.5 CC[C@H](C)Nc1nc2nn(C)cc2c2nc(-c3ccco3)nn12 10.1021/jm300899q
CHEMBL2181151 82945 None 0 Human Functional pKi = 5.6 5.6 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 311 4 1 8 2.5 CC[C@H](C)Nc1nc2nn(C)cc2c2nc(-c3ccco3)nn12 10.1021/jm300899q
71457391 82926 None 0 Human Functional pKi = 5.6 5.6 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 379 4 1 8 3.5 Cn1cc2c(nc(NCc3ccc(Cl)cc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm300899q
CHEMBL2180935 82926 None 0 Human Functional pKi = 5.6 5.6 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 379 4 1 8 3.5 Cn1cc2c(nc(NCc3ccc(Cl)cc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm300899q
71457407 82954 None 0 Human Functional pKi = 5.6 5.6 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 323 3 1 8 2.6 Cn1cc2c(nc(NC3CCCC3)n3nc(-c4ccco4)nc23)n1 10.1021/jm300899q
CHEMBL2181160 82954 None 0 Human Functional pKi = 5.6 5.6 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 323 3 1 8 2.6 Cn1cc2c(nc(NC3CCCC3)n3nc(-c4ccco4)nc23)n1 10.1021/jm300899q
52942475 19254 None 0 Human Functional pKi = 5.6 5.6 - 0
Antagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hrAntagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hr
ChEMBL 489 9 2 5 5.7 CC(C)CCc1c(-c2nccs2)c(=O)[nH]c2ccc(OCC(=O)NC(C)(C)c3ccccc3)cc12 10.1016/j.bmcl.2010.10.030
CHEMBL1290212 19254 None 0 Human Functional pKi = 5.6 5.6 - 0
Antagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hrAntagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hr
ChEMBL 489 9 2 5 5.7 CC(C)CCc1c(-c2nccs2)c(=O)[nH]c2ccc(OCC(=O)NC(C)(C)c3ccccc3)cc12 10.1016/j.bmcl.2010.10.030
42636897 172640 None 25 Human Functional pKi = 5.6 5.6 - 0
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 379 4 3 8 1.3 O[C@@H]1[C@@H](CCl)O[C@@H](n2cnc3c(NC4CC5CCC4C5)ncnc32)[C@@H]1O 10.1021/jm801456g
CHEMBL449575 172640 None 25 Human Functional pKi = 5.6 5.6 - 0
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 379 4 3 8 1.3 O[C@@H]1[C@@H](CCl)O[C@@H](n2cnc3c(NC4CC5CCC4C5)ncnc32)[C@@H]1O 10.1021/jm801456g
76331703 103704 None 0 Human Functional pKi = 5.6 5.6 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 453 7 1 7 4.7 Cc1ccc(COc2ccc(CC(=O)Nc3ncnc4c3nc(-c3ccco3)n4C)cc2)cc1 10.1016/j.ejmech.2013.10.006
CHEMBL3087712 103704 None 0 Human Functional pKi = 5.6 5.6 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 453 7 1 7 4.7 Cc1ccc(COc2ccc(CC(=O)Nc3ncnc4c3nc(-c3ccco3)n4C)cc2)cc1 10.1016/j.ejmech.2013.10.006
71462755 82931 None 0 Human Functional pKi = 5.6 5.6 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 359 5 1 8 2.9 Cn1cc2c(nc(NCCc3ccccc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm300899q
CHEMBL2180940 82931 None 0 Human Functional pKi = 5.6 5.6 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 359 5 1 8 2.9 Cn1cc2c(nc(NCCc3ccccc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm300899q
44572469 179451 None 11 Human Functional pKi = 5.6 5.6 - 0
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 257 2 2 6 0.2 Nc1ncnc2c1nc(Br)n2CCO 10.1016/j.ejmech.2010.04.039
CHEMBL474058 179451 None 11 Human Functional pKi = 5.6 5.6 - 0
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 257 2 2 6 0.2 Nc1ncnc2c1nc(Br)n2CCO 10.1016/j.ejmech.2010.04.039
44572469 179451 None 11 Human Functional pKi = 5.6 5.6 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 257 2 2 6 0.2 Nc1ncnc2c1nc(Br)n2CCO 10.1016/j.bmc.2009.02.030
44572469 179451 None 11 Human Functional pKi = 5.6 5.6 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 257 2 2 6 0.2 Nc1ncnc2c1nc(Br)n2CCO 10.1016/j.ejmech.2013.10.006
CHEMBL474058 179451 None 11 Human Functional pKi = 5.6 5.6 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 257 2 2 6 0.2 Nc1ncnc2c1nc(Br)n2CCO 10.1016/j.bmc.2009.02.030
CHEMBL474058 179451 None 11 Human Functional pKi = 5.6 5.6 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 257 2 2 6 0.2 Nc1ncnc2c1nc(Br)n2CCO 10.1016/j.ejmech.2013.10.006
24882472 154654 None 0 Human Functional pKi = 5.6 5.6 - 0
Agonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activity
ChEMBL 456 5 4 10 1.4 CNC(=S)OC[C@H]1O[C@@H](n2cnc3c(NC4CCCC4)nc(Cl)nc32)[C@](C)(O)[C@@H]1O 10.1016/j.bmc.2007.09.035
CHEMBL399514 154654 None 0 Human Functional pKi = 5.6 5.6 - 0
Agonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activity
ChEMBL 456 5 4 10 1.4 CNC(=S)OC[C@H]1O[C@@H](n2cnc3c(NC4CCCC4)nc(Cl)nc32)[C@](C)(O)[C@@H]1O 10.1016/j.bmc.2007.09.035
71459268 82934 None 0 Human Functional pKi = 5.5 5.5 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 398 5 2 8 3.4 Cn1cc2c(nc(NCCc3c[nH]c4ccccc34)n3nc(-c4ccco4)nc23)n1 10.1021/jm300899q
CHEMBL2181141 82934 None 0 Human Functional pKi = 5.5 5.5 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 398 5 2 8 3.4 Cn1cc2c(nc(NCCc3c[nH]c4ccccc34)n3nc(-c4ccco4)nc23)n1 10.1021/jm300899q
9806649 59543 None 0 Human Functional pKi = 8.5 8.5 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 518 10 3 8 2.8 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccc(C(=O)NC)cc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
CHEMBL17167 59543 None 0 Human Functional pKi = 8.5 8.5 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 518 10 3 8 2.8 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccc(C(=O)NC)cc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
11605883 79952 None 6 Human Functional pKi = 8.4 8.4 - 1
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 508 7 2 7 2.0 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccccc5)CC4)cc3)[nH]c2c1=O 10.1016/j.ejmech.2010.04.039
CHEMBL212625 79952 None 6 Human Functional pKi = 8.4 8.4 - 1
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 508 7 2 7 2.0 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccccc5)CC4)cc3)[nH]c2c1=O 10.1016/j.ejmech.2010.04.039
9892149 59625 None 0 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 499 9 2 7 4.2 CCCn1c(=O)c2nc(-c3ccc(/C=C/C(=O)Nc4ccccc4C(C)=O)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
CHEMBL17202 59625 None 0 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 499 9 2 7 4.2 CCCn1c(=O)c2nc(-c3ccc(/C=C/C(=O)Nc4ccccc4C(C)=O)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
541759 170035 None 1 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 477 9 3 8 3.1 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccc(O)cc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
CHEMBL444281 170035 None 1 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 477 9 3 8 3.1 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccc(O)cc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
9936467 58092 None 1 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 519 10 2 9 3.2 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccc(C(=O)OC)cc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
CHEMBL16741 58092 None 1 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 519 10 2 9 3.2 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccc(C(=O)OC)cc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
155544096 173306 None 0 Human Functional pKi = 5.5 5.5 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase by [alpha-32P]ATP based methodAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase by [alpha-32P]ATP based method
ChEMBL 440 8 2 10 3.4 Cn1cc2c(nc(NCCCCCNC(=O)OC(C)(C)C)n3nc(-c4ccco4)nc23)n1 10.1039/C9MD00014C
CHEMBL4526138 173306 None 0 Human Functional pKi = 5.5 5.5 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase by [alpha-32P]ATP based methodAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase by [alpha-32P]ATP based method
ChEMBL 440 8 2 10 3.4 Cn1cc2c(nc(NCCCCCNC(=O)OC(C)(C)C)n3nc(-c4ccco4)nc23)n1 10.1039/C9MD00014C
11053743 162878 None 0 Human Functional pKi = 5.5 5.5 - 0
Antagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assay
ChEMBL 239 2 1 5 2.1 CCn1c(-c2ccccc2)nc2c(N)ncnc21 10.1016/j.ejmech.2018.03.067
CHEMBL4173347 162878 None 0 Human Functional pKi = 5.5 5.5 - 0
Antagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assay
ChEMBL 239 2 1 5 2.1 CCn1c(-c2ccccc2)nc2c(N)ncnc21 10.1016/j.ejmech.2018.03.067
118707855 113233 None 0 Human Functional pKi = 5.5 5.5 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 301 5 1 8 2.0 CCNc1ncc(C(=O)OCC)c2nc(-c3ccco3)nn12 10.1021/jm500752h
CHEMBL3314888 113233 None 0 Human Functional pKi = 5.5 5.5 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 301 5 1 8 2.0 CCNc1ncc(C(=O)OCC)c2nc(-c3ccco3)nn12 10.1021/jm500752h
44447534 94981 None 0 Human Functional pKi = 4.5 4.5 - 0
Agonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activity
ChEMBL 442 5 4 11 0.0 CNC(=O)OC[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCOC4)nc(Cl)nc32)[C@](C)(O)[C@@H]1O 10.1016/j.bmc.2007.09.035
CHEMBL254693 94981 None 0 Human Functional pKi = 4.5 4.5 - 0
Agonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activity
ChEMBL 442 5 4 11 0.0 CNC(=O)OC[C@H]1O[C@@H](n2cnc3c(N[C@@H]4CCOC4)nc(Cl)nc32)[C@](C)(O)[C@@H]1O 10.1016/j.bmc.2007.09.035
136199393 19237 None 0 Human Functional pKi = 7.5 7.5 - 0
Antagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hrAntagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hr
ChEMBL 521 9 2 5 5.7 Cc1cc(-c2c(CCc3ccccc3)c3cc(OCC(=O)NC(C)(C)c4ccccc4)ccc3[nH]c2=O)on1 10.1016/j.bmcl.2010.10.030
CHEMBL1290102 19237 None 0 Human Functional pKi = 7.5 7.5 - 0
Antagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hrAntagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hr
ChEMBL 521 9 2 5 5.7 Cc1cc(-c2c(CCc3ccccc3)c3cc(OCC(=O)NC(C)(C)c4ccccc4)ccc3[nH]c2=O)on1 10.1016/j.bmcl.2010.10.030
52947452 19312 None 0 Human Functional pKi = 6.5 6.5 - 0
Antagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hrAntagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hr
ChEMBL 558 9 2 5 4.7 CS(=O)(=O)c1c(CCc2ccccc2)c2cc(OCC(=O)NCc3ccc(Cl)c(Cl)c3)ccc2[nH]c1=O 10.1016/j.bmcl.2010.10.030
CHEMBL1290543 19312 None 0 Human Functional pKi = 6.5 6.5 - 0
Antagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hrAntagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hr
ChEMBL 558 9 2 5 4.7 CS(=O)(=O)c1c(CCc2ccccc2)c2cc(OCC(=O)NCc3ccc(Cl)c(Cl)c3)ccc2[nH]c1=O 10.1016/j.bmcl.2010.10.030
71461028 82927 None 0 Human Functional pKi = 5.5 5.5 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 363 4 1 8 3.0 Cn1cc2c(nc(NCc3ccc(F)cc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm300899q
CHEMBL2180936 82927 None 0 Human Functional pKi = 5.5 5.5 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 363 4 1 8 3.0 Cn1cc2c(nc(NCc3ccc(F)cc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm300899q
127038355 136708 None 0 Human Functional pKi = 5.5 5.5 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 359 6 1 5 3.7 CCCn1c(Br)nc2c(NCCc3ccccc3)ncnc21 10.1039/C5MD00034C
CHEMBL3740619 136708 None 0 Human Functional pKi = 5.5 5.5 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 359 6 1 5 3.7 CCCn1c(Br)nc2c(NCCc3ccccc3)ncnc21 10.1039/C5MD00034C
52941244 19251 None 0 Human Functional pKi = 6.5 6.5 - 0
Antagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hrAntagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hr
ChEMBL 509 9 2 5 5.7 C[C@@H](NC(=O)COc1ccc2[nH]c(=O)c(-c3nccs3)c(CCc3ccccc3)c2c1)c1ccccc1 10.1016/j.bmcl.2010.10.030
CHEMBL1290209 19251 None 0 Human Functional pKi = 6.5 6.5 - 0
Antagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hrAntagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hr
ChEMBL 509 9 2 5 5.7 C[C@@H](NC(=O)COc1ccc2[nH]c(=O)c(-c3nccs3)c(CCc3ccccc3)c2c1)c1ccccc1 10.1016/j.bmcl.2010.10.030
14426726 181637 None 0 Human Functional pKi = 5.5 5.5 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 353 4 3 8 1.0 O[C@@H]1[C@@H](CCl)O[C@@H](n2cnc3c(NC4CCCC4)ncnc32)[C@@H]1O 10.1021/jm801456g
CHEMBL477444 181637 None 0 Human Functional pKi = 5.5 5.5 - 1
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 353 4 3 8 1.0 O[C@@H]1[C@@H](CCl)O[C@@H](n2cnc3c(NC4CCCC4)ncnc32)[C@@H]1O 10.1021/jm801456g
9807634 59884 None 0 Human Functional pKi = 7.5 7.5 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 551 11 2 7 4.7 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)NC(c4ccccc4)c4ccccc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
CHEMBL17299 59884 None 0 Human Functional pKi = 7.5 7.5 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 551 11 2 7 4.7 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)NC(c4ccccc4)c4ccccc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
52950027 19143 None 0 Human Functional pKi = 6.5 6.5 - 0
Antagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hrAntagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hr
ChEMBL 478 9 2 4 5.3 O=C(COc1ccc2[nH]c(=O)c(-c3ccco3)c(CCc3ccccc3)c2c1)NCc1ccccc1 10.1016/j.bmcl.2010.10.030
CHEMBL1289461 19143 None 0 Human Functional pKi = 6.5 6.5 - 0
Antagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hrAntagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hr
ChEMBL 478 9 2 4 5.3 O=C(COc1ccc2[nH]c(=O)c(-c3ccco3)c(CCc3ccccc3)c2c1)NCc1ccccc1 10.1016/j.bmcl.2010.10.030
71453874 82921 None 0 Human Functional pKi = 5.5 5.5 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 345 4 1 8 2.9 Cn1cc2c(nc(NCc3ccccc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm300899q
CHEMBL2180930 82921 None 0 Human Functional pKi = 5.5 5.5 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 345 4 1 8 2.9 Cn1cc2c(nc(NCc3ccccc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm300899q
2519 779 None 86 Human Functional pKi = 4.5 4.5 -17378 8
Antagonist activity at adenosine A2B receptor (unknown origin)Antagonist activity at adenosine A2B receptor (unknown origin)
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1016/j.ejmech.2021.113907
2519.0 779 None 86 Human Functional pKi = 4.5 4.5 -17378 8
Antagonist activity at adenosine A2B receptor (unknown origin)Antagonist activity at adenosine A2B receptor (unknown origin)
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1016/j.ejmech.2021.113907
407 779 None 86 Human Functional pKi = 4.5 4.5 -17378 8
Antagonist activity at adenosine A2B receptor (unknown origin)Antagonist activity at adenosine A2B receptor (unknown origin)
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1016/j.ejmech.2021.113907
463 779 None 86 Human Functional pKi = 4.5 4.5 -17378 8
Antagonist activity at adenosine A2B receptor (unknown origin)Antagonist activity at adenosine A2B receptor (unknown origin)
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1016/j.ejmech.2021.113907
CHEMBL113 779 None 86 Human Functional pKi = 4.5 4.5 -17378 8
Antagonist activity at adenosine A2B receptor (unknown origin)Antagonist activity at adenosine A2B receptor (unknown origin)
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1016/j.ejmech.2021.113907
DB00201 779 None 86 Human Functional pKi = 4.5 4.5 -17378 8
Antagonist activity at adenosine A2B receptor (unknown origin)Antagonist activity at adenosine A2B receptor (unknown origin)
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1016/j.ejmech.2021.113907
52950028 19144 None 0 Human Functional pKi = 5.5 5.5 - 0
Antagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hrAntagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hr
ChEMBL 461 7 2 5 4.7 CC(C)(C)NC(=O)COc1ccc2[nH]c(=O)c(-c3nccs3)c(CCc3ccccc3)c2c1 10.1016/j.bmcl.2010.10.030
CHEMBL1289462 19144 None 0 Human Functional pKi = 5.5 5.5 - 0
Antagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hrAntagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hr
ChEMBL 461 7 2 5 4.7 CC(C)(C)NC(=O)COc1ccc2[nH]c(=O)c(-c3nccs3)c(CCc3ccccc3)c2c1 10.1016/j.bmcl.2010.10.030
11623934 162050 None 0 Human Functional pKi = 5.5 5.5 - 0
Antagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assay
ChEMBL 321 5 1 5 4.3 CCCn1c(-c2ccccc2)nc2c(NC3CCCC3)ncnc21 10.1016/j.ejmech.2018.03.067
CHEMBL4160264 162050 None 0 Human Functional pKi = 5.5 5.5 - 0
Antagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assay
ChEMBL 321 5 1 5 4.3 CCCn1c(-c2ccccc2)nc2c(NC3CCCC3)ncnc21 10.1016/j.ejmech.2018.03.067
52941597 19092 None 0 Human Functional pKi = 5.5 5.5 - 0
Antagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hrAntagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hr
ChEMBL 357 5 1 4 2.7 COc1ccc2[nH]c(=O)c(S(C)(=O)=O)c(CCc3ccccc3)c2c1 10.1016/j.bmcl.2010.10.030
CHEMBL1289109 19092 None 0 Human Functional pKi = 5.5 5.5 - 0
Antagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hrAntagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hr
ChEMBL 357 5 1 4 2.7 COc1ccc2[nH]c(=O)c(S(C)(=O)=O)c(CCc3ccccc3)c2c1 10.1016/j.bmcl.2010.10.030
CHEMBL5092788 215389 None 0 Human Functional pKi = 7.5 7.5 - 0
Antagonist activity at human adenosine A2B receptor expressed in Flp-In-CHO cell membrane assessed as inhibition of NECA-induced cAMP accumulation in presence of forskolin measured after 40 mins by alpha screen LANCE assayAntagonist activity at human adenosine A2B receptor expressed in Flp-In-CHO cell membrane assessed as inhibition of NECA-induced cAMP accumulation in presence of forskolin measured after 40 mins by alpha screen LANCE assay
ChEMBL None None None C#CCCCCNC(=O)C12CCC(c3nc4c(=O)n(CCCC)c(=O)n(CCCNC(=O)c5ccc(S(=O)(=O)F)cc5)c4[nH]3)(CC1)CC2 10.1021/acs.jmedchem.0c02169
76335303 103699 None 0 Human Functional pKi = 6.5 6.5 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 259 4 2 7 1.1 Nc1ncnc2c1nc(-c1ccco1)n2CCCO 10.1016/j.ejmech.2013.10.006
CHEMBL3087707 103699 None 0 Human Functional pKi = 6.5 6.5 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 259 4 2 7 1.1 Nc1ncnc2c1nc(-c1ccco1)n2CCCO 10.1016/j.ejmech.2013.10.006
52945098 19353 None 0 Human Functional pKi = 6.5 6.5 - 0
Antagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hrAntagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hr
ChEMBL 504 9 1 6 3.4 Cn1c(=O)c(S(C)(=O)=O)c(CCc2ccccc2)c2cc(OCC(=O)NCc3ccccc3)ccc21 10.1016/j.bmcl.2010.10.030
CHEMBL1290782 19353 None 0 Human Functional pKi = 6.5 6.5 - 0
Antagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hrAntagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hr
ChEMBL 504 9 1 6 3.4 Cn1c(=O)c(S(C)(=O)=O)c(CCc2ccccc2)c2cc(OCC(=O)NCc3ccccc3)ccc21 10.1016/j.bmcl.2010.10.030
145987819 167154 None 0 Human Functional pKi = 5.4 5.4 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated adenylyl cyclase activity by [alpha-32P]ATP based assayAntagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated adenylyl cyclase activity by [alpha-32P]ATP based assay
ChEMBL 363 5 1 8 3.3 CNc1ncc(C(=O)OC(C)c2ccccc2)c2nc(-c3ccco3)nn12 10.1016/j.ejmech.2018.08.042
CHEMBL4290842 167154 None 0 Human Functional pKi = 5.4 5.4 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated adenylyl cyclase activity by [alpha-32P]ATP based assayAntagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated adenylyl cyclase activity by [alpha-32P]ATP based assay
ChEMBL 363 5 1 8 3.3 CNc1ncc(C(=O)OC(C)c2ccccc2)c2nc(-c3ccco3)nn12 10.1016/j.ejmech.2018.08.042
11492857 162351 None 0 Human Functional pKi = 5.4 5.4 - 0
Antagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assay
ChEMBL 279 3 1 5 3.0 Cn1c(-c2ccccc2)nc2c(NC3CCC3)ncnc21 10.1016/j.ejmech.2018.03.067
CHEMBL4165013 162351 None 0 Human Functional pKi = 5.4 5.4 - 0
Antagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assay
ChEMBL 279 3 1 5 3.0 Cn1c(-c2ccccc2)nc2c(NC3CCC3)ncnc21 10.1016/j.ejmech.2018.03.067
11229946 103707 None 1 Human Functional pKi = 6.4 6.4 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 229 2 1 6 1.7 CCn1c(-c2ccco2)nc2c(N)ncnc21 10.1016/j.ejmech.2013.10.006
CHEMBL3087715 103707 None 1 Human Functional pKi = 6.4 6.4 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 229 2 1 6 1.7 CCn1c(-c2ccco2)nc2c(N)ncnc21 10.1016/j.ejmech.2013.10.006
71457405 82944 None 0 Human Functional pKi = 5.4 5.4 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 311 4 1 8 2.5 CCC(C)Nc1nc2nn(C)cc2c2nc(-c3ccco3)nn12 10.1021/jm300899q
CHEMBL2181150 82944 None 0 Human Functional pKi = 5.4 5.4 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 311 4 1 8 2.5 CCC(C)Nc1nc2nn(C)cc2c2nc(-c3ccco3)nn12 10.1021/jm300899q
71455619 82932 None 0 Human Functional pKi = 5.4 5.4 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 419 7 1 10 2.9 COc1ccc(CCNc2nc3nn(C)cc3c3nc(-c4ccco4)nn23)cc1OC 10.1021/jm300899q
CHEMBL2181139 82932 None 0 Human Functional pKi = 5.4 5.4 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 419 7 1 10 2.9 COc1ccc(CCNc2nc3nn(C)cc3c3nc(-c4ccco4)nn23)cc1OC 10.1021/jm300899q
10085373 10428 None 6 Human Functional pKi = 6.4 6.4 - 1
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 286 2 1 6 0.6 COc1ccc(-c2nc3c(=O)n(C)c(=O)n(C)c3[nH]2)cc1 10.1016/j.ejmech.2010.04.039
CHEMBL11635 10428 None 6 Human Functional pKi = 6.4 6.4 - 1
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 286 2 1 6 0.6 COc1ccc(-c2nc3c(=O)n(C)c(=O)n(C)c3[nH]2)cc1 10.1016/j.ejmech.2010.04.039
71455603 82924 None 0 Human Functional pKi = 5.4 5.4 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 359 4 1 8 3.2 Cc1ccc(CNc2nc3nn(C)cc3c3nc(-c4ccco4)nn23)cc1 10.1021/jm300899q
CHEMBL2180933 82924 None 0 Human Functional pKi = 5.4 5.4 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 359 4 1 8 3.2 Cc1ccc(CNc2nc3nn(C)cc3c3nc(-c4ccco4)nn23)cc1 10.1021/jm300899q
71455622 82947 None 0 Human Functional pKi = 5.4 5.4 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 325 6 1 8 2.9 CCCCCNc1nc2nn(C)cc2c2nc(-c3ccco3)nn12 10.1021/jm300899q
CHEMBL2181153 82947 None 0 Human Functional pKi = 5.4 5.4 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 325 6 1 8 2.9 CCCCCNc1nc2nn(C)cc2c2nc(-c3ccco3)nn12 10.1021/jm300899q
57429649 158942 None 0 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity at human adenosine A2B receptor expressed in HEK293 cells assessed as inhibition of cAMP productionAntagonist activity at human adenosine A2B receptor expressed in HEK293 cells assessed as inhibition of cAMP production
ChEMBL 572 8 1 9 2.9 CCCn1c(=O)c2[nH]c(-c3cnn(CC(=O)N4CCN(c5cccc(C(F)(F)F)c5)CC4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2021.113907
CHEMBL4095843 158942 None 0 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity at human adenosine A2B receptor expressed in HEK293 cells assessed as inhibition of cAMP productionAntagonist activity at human adenosine A2B receptor expressed in HEK293 cells assessed as inhibition of cAMP production
ChEMBL 572 8 1 9 2.9 CCCn1c(=O)c2[nH]c(-c3cnn(CC(=O)N4CCN(c5cccc(C(F)(F)F)c5)CC4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2021.113907
66892867 156319 None 0 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity at human adenosine receptor A2b expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP level preincubated for 15 mins followed by NECA stimulation for 15 mins by HTRF assayAntagonist activity at human adenosine receptor A2b expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP level preincubated for 15 mins followed by NECA stimulation for 15 mins by HTRF assay
ChEMBL 479 7 1 8 2.4 CCCn1c(=O)c2[nH]c(-c3cnn(CC4CC(=O)N(c5ccc(F)cc5)C4)c3)nc2n(CC)c1=O 10.1016/j.ejmech.2016.11.007
CHEMBL4065629 156319 None 0 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity at human adenosine receptor A2b expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP level preincubated for 15 mins followed by NECA stimulation for 15 mins by HTRF assayAntagonist activity at human adenosine receptor A2b expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP level preincubated for 15 mins followed by NECA stimulation for 15 mins by HTRF assay
ChEMBL 479 7 1 8 2.4 CCCn1c(=O)c2[nH]c(-c3cnn(CC4CC(=O)N(c5ccc(F)cc5)C4)c3)nc2n(CC)c1=O 10.1016/j.ejmech.2016.11.007
57429649 158942 None 0 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity at human adenosine receptor A2b expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP level preincubated for 15 mins followed by NECA stimulation for 15 mins by HTRF assayAntagonist activity at human adenosine receptor A2b expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP level preincubated for 15 mins followed by NECA stimulation for 15 mins by HTRF assay
ChEMBL 572 8 1 9 2.9 CCCn1c(=O)c2[nH]c(-c3cnn(CC(=O)N4CCN(c5cccc(C(F)(F)F)c5)CC4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2016.11.007
CHEMBL4095843 158942 None 0 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity at human adenosine receptor A2b expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP level preincubated for 15 mins followed by NECA stimulation for 15 mins by HTRF assayAntagonist activity at human adenosine receptor A2b expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP level preincubated for 15 mins followed by NECA stimulation for 15 mins by HTRF assay
ChEMBL 572 8 1 9 2.9 CCCn1c(=O)c2[nH]c(-c3cnn(CC(=O)N4CCN(c5cccc(C(F)(F)F)c5)CC4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2016.11.007
11690712 77792 None 0 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 439 7 3 6 2.0 CCCn1c(=O)[nH]c2[nH]c(-c3ccc(S(=O)(=O)NCc4ccccc4)cc3)nc2c1=O 10.1016/j.ejmech.2010.04.039
CHEMBL209230 77792 None 0 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 439 7 3 6 2.0 CCCn1c(=O)[nH]c2[nH]c(-c3ccc(S(=O)(=O)NCc4ccccc4)cc3)nc2c1=O 10.1016/j.ejmech.2010.04.039
52946453 19223 None 0 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hrAntagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hr
ChEMBL 521 9 2 5 5.6 O=C(COc1ccc2[nH]c(=O)c(-c3nccs3)c(CCc3ccccc3)c2c1)NC1(c2ccccc2)CC1 10.1016/j.bmcl.2010.10.030
CHEMBL1290001 19223 None 0 Human Functional pKi = 8.4 8.4 - 0
Antagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hrAntagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hr
ChEMBL 521 9 2 5 5.6 O=C(COc1ccc2[nH]c(=O)c(-c3nccs3)c(CCc3ccccc3)c2c1)NC1(c2ccccc2)CC1 10.1016/j.bmcl.2010.10.030
44404010 72577 None 0 Human Functional pKi = 8.3 8.3 - 0
Antagonist activity against human Adenosine A2b receptorAntagonist activity against human Adenosine A2b receptor
ChEMBL 480 9 2 8 2.9 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccc(F)cc4)nc3)[nH]c2n(CCC)c1=O 10.1021/jm049418o
CHEMBL199249 72577 None 0 Human Functional pKi = 8.3 8.3 - 0
Antagonist activity against human Adenosine A2b receptorAntagonist activity against human Adenosine A2b receptor
ChEMBL 480 9 2 8 2.9 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccc(F)cc4)nc3)[nH]c2n(CCC)c1=O 10.1021/jm049418o
135528632 72563 None 0 Human Functional pKi = 8.3 8.3 - 0
Antagonist activity against human Adenosine A2b receptorAntagonist activity against human Adenosine A2b receptor
ChEMBL 329 5 2 7 1.5 CCCn1c(=O)c2nc(-c3ccc(O)nc3)[nH]c2n(CCC)c1=O 10.1021/jm049418o
CHEMBL199196 72563 None 0 Human Functional pKi = 8.3 8.3 - 0
Antagonist activity against human Adenosine A2b receptorAntagonist activity against human Adenosine A2b receptor
ChEMBL 329 5 2 7 1.5 CCCn1c(=O)c2nc(-c3ccc(O)nc3)[nH]c2n(CCC)c1=O 10.1021/jm049418o
9870719 57417 None 0 Human Functional pKi = 8.3 8.3 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 503 10 2 8 3.6 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4cccc(C(C)=O)c4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
CHEMBL16534 57417 None 0 Human Functional pKi = 8.3 8.3 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 503 10 2 8 3.6 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4cccc(C(C)=O)c4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
126079 4100 None 31 Human Functional pKi = 7.4 7.4 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 386 8 2 7 1.8 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)O 10.1021/jm990421v
451 4100 None 31 Human Functional pKi = 7.4 7.4 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 386 8 2 7 1.8 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)O 10.1021/jm990421v
CHEMBL27041 4100 None 31 Human Functional pKi = 7.4 7.4 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 386 8 2 7 1.8 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)O 10.1021/jm990421v
52950027 19143 None 0 Human Functional pKi = 6.4 6.4 - 0
Antagonist activity at adenosien A2B receptor in human HMC-1 cells assessed as inhibition of NECA-induced IL-8 release after 6 hr by ELISAAntagonist activity at adenosien A2B receptor in human HMC-1 cells assessed as inhibition of NECA-induced IL-8 release after 6 hr by ELISA
ChEMBL 478 9 2 4 5.3 O=C(COc1ccc2[nH]c(=O)c(-c3ccco3)c(CCc3ccccc3)c2c1)NCc1ccccc1 10.1016/j.bmcl.2010.10.030
CHEMBL1289461 19143 None 0 Human Functional pKi = 6.4 6.4 - 0
Antagonist activity at adenosien A2B receptor in human HMC-1 cells assessed as inhibition of NECA-induced IL-8 release after 6 hr by ELISAAntagonist activity at adenosien A2B receptor in human HMC-1 cells assessed as inhibition of NECA-induced IL-8 release after 6 hr by ELISA
ChEMBL 478 9 2 4 5.3 O=C(COc1ccc2[nH]c(=O)c(-c3ccco3)c(CCc3ccccc3)c2c1)NCc1ccccc1 10.1016/j.bmcl.2010.10.030
52950000 19126 None 0 Human Functional pKi = 6.4 6.4 - 0
Antagonist activity at adenosien A2B receptor in human HMC-1 cells assessed as inhibition of NECA-induced IL-8 release after 6 hr by ELISAAntagonist activity at adenosien A2B receptor in human HMC-1 cells assessed as inhibition of NECA-induced IL-8 release after 6 hr by ELISA
ChEMBL 505 8 2 4 5.2 N#Cc1c(CCc2ccccc2)c2cc(OCC(=O)NCc3ccc(Cl)c(Cl)c3)ccc2[nH]c1=O 10.1016/j.bmcl.2010.10.030
CHEMBL1289344 19126 None 0 Human Functional pKi = 6.4 6.4 - 0
Antagonist activity at adenosien A2B receptor in human HMC-1 cells assessed as inhibition of NECA-induced IL-8 release after 6 hr by ELISAAntagonist activity at adenosien A2B receptor in human HMC-1 cells assessed as inhibition of NECA-induced IL-8 release after 6 hr by ELISA
ChEMBL 505 8 2 4 5.2 N#Cc1c(CCc2ccccc2)c2cc(OCC(=O)NCc3ccc(Cl)c(Cl)c3)ccc2[nH]c1=O 10.1016/j.bmcl.2010.10.030
52948915 19295 None 0 Human Functional pKi = 7.4 7.4 - 0
Antagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hrAntagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hr
ChEMBL 541 9 2 5 6.0 CC(C)(NC(=O)COc1ccc2[nH]c(=O)c(-c3nccs3)c(CCc3ccc(F)cc3)c2c1)c1ccccc1 10.1016/j.bmcl.2010.10.030
CHEMBL1290437 19295 None 0 Human Functional pKi = 7.4 7.4 - 0
Antagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hrAntagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hr
ChEMBL 541 9 2 5 6.0 CC(C)(NC(=O)COc1ccc2[nH]c(=O)c(-c3nccs3)c(CCc3ccc(F)cc3)c2c1)c1ccccc1 10.1016/j.bmcl.2010.10.030
44572409 189691 None 0 Human Functional pKi = 5.4 5.4 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 267 1 1 5 1.9 Nc1ncnc2c1nc(Br)n2C1CCC1 10.1016/j.bmc.2009.02.030
CHEMBL515419 189691 None 0 Human Functional pKi = 5.4 5.4 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 267 1 1 5 1.9 Nc1ncnc2c1nc(Br)n2C1CCC1 10.1016/j.bmc.2009.02.030
123807 871 None 54 Human Functional pKi = 7.4 7.4 -12022 7
Agonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activity
ChEMBL 369 4 4 9 0.4 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NC1CCCC1 10.1016/j.bmc.2007.09.035
374 871 None 54 Human Functional pKi = 7.4 7.4 -12022 7
Agonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activity
ChEMBL 369 4 4 9 0.4 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NC1CCCC1 10.1016/j.bmc.2007.09.035
379 871 None 54 Human Functional pKi = 7.4 7.4 -12022 7
Agonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activity
ChEMBL 369 4 4 9 0.4 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NC1CCCC1 10.1016/j.bmc.2007.09.035
CHEMBL284969 871 None 54 Human Functional pKi = 7.4 7.4 -12022 7
Agonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activity
ChEMBL 369 4 4 9 0.4 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NC1CCCC1 10.1016/j.bmc.2007.09.035
176407 4148 None 84 Human Functional pKi = 7.4 7.4 -13 2
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated [3H]cAMP production by scintillation countingAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated [3H]cAMP production by scintillation counting
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1021/jm900718w
405 4148 None 84 Human Functional pKi = 7.4 7.4 -13 2
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated [3H]cAMP production by scintillation countingAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated [3H]cAMP production by scintillation counting
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1021/jm900718w
CHEMBL113142 4148 None 84 Human Functional pKi = 7.4 7.4 -13 2
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated [3H]cAMP production by scintillation countingAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated [3H]cAMP production by scintillation counting
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1021/jm900718w
DB08770 4148 None 84 Human Functional pKi = 7.4 7.4 -13 2
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated [3H]cAMP production by scintillation countingAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated [3H]cAMP production by scintillation counting
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1021/jm900718w
44572355 179584 None 0 Human Functional pKi = 5.4 5.4 - 0
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 269 2 1 5 1.8 CC(C)Cn1c(Br)nc2c(N)ncnc21 10.1016/j.ejmech.2010.04.039
CHEMBL474207 179584 None 0 Human Functional pKi = 5.4 5.4 - 0
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 269 2 1 5 1.8 CC(C)Cn1c(Br)nc2c(N)ncnc21 10.1016/j.ejmech.2010.04.039
44572355 179584 None 0 Human Functional pKi = 5.4 5.4 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 269 2 1 5 1.8 CC(C)Cn1c(Br)nc2c(N)ncnc21 10.1016/j.bmc.2009.02.030
CHEMBL474207 179584 None 0 Human Functional pKi = 5.4 5.4 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 269 2 1 5 1.8 CC(C)Cn1c(Br)nc2c(N)ncnc21 10.1016/j.bmc.2009.02.030
380 1287 None 54 Human Functional pKi = 7.4 7.4 - 5
Agonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activity
ChEMBL 335 4 4 9 -0.2 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NC1CCCC1 10.1016/j.bmc.2007.09.035
657378 1287 None 54 Human Functional pKi = 7.4 7.4 - 5
Agonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activity
ChEMBL 335 4 4 9 -0.2 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NC1CCCC1 10.1016/j.bmc.2007.09.035
CHEMBL68738 1287 None 54 Human Functional pKi = 7.4 7.4 - 5
Agonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activity
ChEMBL 335 4 4 9 -0.2 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NC1CCCC1 10.1016/j.bmc.2007.09.035
9915751 59129 None 0 Human Functional pKi = 7.4 7.4 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 557 14 1 11 1.7 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)N(CC(=O)OCC)CC(=O)OCC)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
CHEMBL16984 59129 None 0 Human Functional pKi = 7.4 7.4 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 557 14 1 11 1.7 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)N(CC(=O)OCC)CC(=O)OCC)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
44447542 154790 None 0 Human Functional pKi = 5.4 5.4 - 0
Agonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activity
ChEMBL 351 4 4 10 -1.0 C[C@@]1(O)[C@H](O)[C@@H](CO)O[C@H]1n1cnc2c(N[C@@H]3CCOC3)ncnc21 10.1016/j.bmc.2007.09.035
CHEMBL400190 154790 None 0 Human Functional pKi = 5.4 5.4 - 0
Agonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activity
ChEMBL 351 4 4 10 -1.0 C[C@@]1(O)[C@H](O)[C@@H](CO)O[C@H]1n1cnc2c(N[C@@H]3CCOC3)ncnc21 10.1016/j.bmc.2007.09.035
44447548 154886 None 0 Human Functional pKi = 5.4 5.4 - 0
Agonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activity
ChEMBL 385 4 4 10 -0.3 C[C@@]1(O)[C@H](O)[C@@H](CO)O[C@H]1n1cnc2c(N[C@@H]3CCOC3)nc(Cl)nc21 10.1016/j.bmc.2007.09.035
CHEMBL400782 154886 None 0 Human Functional pKi = 5.4 5.4 - 0
Agonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activity
ChEMBL 385 4 4 10 -0.3 C[C@@]1(O)[C@H](O)[C@@H](CO)O[C@H]1n1cnc2c(N[C@@H]3CCOC3)nc(Cl)nc21 10.1016/j.bmc.2007.09.035
44572408 188860 None 0 Human Functional pKi = 5.3 5.3 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 253 2 1 5 1.4 C=CCn1c(Br)nc2c(N)ncnc21 10.1016/j.bmc.2009.02.030
CHEMBL506888 188860 None 0 Human Functional pKi = 5.3 5.3 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 253 2 1 5 1.4 C=CCn1c(Br)nc2c(N)ncnc21 10.1016/j.bmc.2009.02.030
127042409 136774 None 0 Human Functional pKi = 5.3 5.3 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 348 6 2 7 3.7 CCCn1c(-c2ccco2)nc2c(N)nc(NCc3ccccc3)nc21 10.1039/C5MD00034C
CHEMBL3741217 136774 None 0 Human Functional pKi = 5.3 5.3 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 348 6 2 7 3.7 CCCn1c(-c2ccco2)nc2c(N)nc(NCc3ccccc3)nc21 10.1039/C5MD00034C
118707860 113238 None 0 Human Functional pKi = 5.3 5.3 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 341 5 1 8 2.9 CCOC(=O)c1cnc(NC2CCCC2)n2nc(-c3ccco3)nc12 10.1021/jm500752h
CHEMBL3314893 113238 None 0 Human Functional pKi = 5.3 5.3 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 341 5 1 8 2.9 CCOC(=O)c1cnc(NC2CCCC2)n2nc(-c3ccco3)nc12 10.1021/jm500752h
9912946 59002 None 0 Human Functional pKi = 6.3 6.3 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 478 7 2 6 3.7 O=C(O)/C=C/c1ccc(-c2nc3c(=O)n(Cc4ccccc4)c(=O)n(Cc4ccccc4)c3[nH]2)cc1 10.1021/jm990421v
CHEMBL16908 59002 None 0 Human Functional pKi = 6.3 6.3 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 478 7 2 6 3.7 O=C(O)/C=C/c1ccc(-c2nc3c(=O)n(Cc4ccccc4)c(=O)n(Cc4ccccc4)c3[nH]2)cc1 10.1021/jm990421v
76335305 103709 None 0 Human Functional pKi = 6.3 6.3 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 245 3 2 7 0.7 Nc1ncnc2c1nc(-c1ccco1)n2CCO 10.1016/j.ejmech.2013.10.006
CHEMBL3087717 103709 None 0 Human Functional pKi = 6.3 6.3 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 245 3 2 7 0.7 Nc1ncnc2c1nc(-c1ccco1)n2CCO 10.1016/j.ejmech.2013.10.006
10387088 59456 None 0 Human Functional pKi = 7.3 7.3 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 414 10 2 7 2.6 CCCCn1c(=O)c2nc(-c3ccc(OCC(=O)O)cc3)[nH]c2n(CCCC)c1=O 10.1021/jm990421v
CHEMBL17123 59456 None 0 Human Functional pKi = 7.3 7.3 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 414 10 2 7 2.6 CCCCn1c(=O)c2nc(-c3ccc(OCC(=O)O)cc3)[nH]c2n(CCCC)c1=O 10.1021/jm990421v
71455621 82946 None 0 Human Functional pKi = 5.3 5.3 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 311 4 1 8 2.5 CC[C@@H](C)Nc1nc2nn(C)cc2c2nc(-c3ccco3)nn12 10.1021/jm300899q
CHEMBL2181152 82946 None 0 Human Functional pKi = 5.3 5.3 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 311 4 1 8 2.5 CC[C@@H](C)Nc1nc2nn(C)cc2c2nc(-c3ccco3)nn12 10.1021/jm300899q
118707864 113242 None 0 Human Functional pKi = 5.3 5.3 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 393 7 1 9 3.2 CCOC(=O)c1cnc(NCc2ccc(OC)cc2)n2nc(-c3ccco3)nc12 10.1021/jm500752h
CHEMBL3314897 113242 None 0 Human Functional pKi = 5.3 5.3 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 393 7 1 9 3.2 CCOC(=O)c1cnc(NCc2ccc(OC)cc2)n2nc(-c3ccco3)nc12 10.1021/jm500752h
44582613 181638 None 0 Human Functional pKi = 5.3 5.3 - 0
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 387 4 3 8 1.7 O[C@@H]1[C@@H](CCl)O[C@@H](n2cnc3c(NC4CCCC4)nc(Cl)nc32)[C@@H]1O 10.1021/jm801456g
CHEMBL477445 181638 None 0 Human Functional pKi = 5.3 5.3 - 0
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 387 4 3 8 1.7 O[C@@H]1[C@@H](CCl)O[C@@H](n2cnc3c(NC4CCCC4)nc(Cl)nc32)[C@@H]1O 10.1021/jm801456g
118707847 113224 None 0 Human Functional pKi = 5.3 5.3 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 376 5 2 7 1.9 CNC(=O)c1cnc(NC(=O)Cc2ccccc2)n2nc(-c3ccco3)nc12 10.1021/jm500752h
CHEMBL3314879 113224 None 0 Human Functional pKi = 5.3 5.3 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 376 5 2 7 1.9 CNC(=O)c1cnc(NC(=O)Cc2ccccc2)n2nc(-c3ccco3)nc12 10.1021/jm500752h
21958762 155780 None 0 Human Functional pKi = 7.3 7.3 - 0
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 288 4 2 6 0.7 CCCn1c(=O)c2[nH]c(-c3cn[nH]c3)nc2n(CC)c1=O 10.1016/j.ejmech.2010.04.039
CHEMBL405901 155780 None 0 Human Functional pKi = 7.3 7.3 - 0
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 288 4 2 6 0.7 CCCn1c(=O)c2[nH]c(-c3cn[nH]c3)nc2n(CC)c1=O 10.1016/j.ejmech.2010.04.039
10021483 186883 None 0 Human Functional pKi = 5.3 5.3 - 0
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 361 4 4 9 0.0 OC[C@H]1O[C@@H](n2cnc3c(NC4CC5CCC4C5)ncnc32)[C@H](O)[C@@H]1O 10.1021/jm801456g
CHEMBL489640 186883 None 0 Human Functional pKi = 5.3 5.3 - 0
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAgonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 361 4 4 9 0.0 OC[C@H]1O[C@@H](n2cnc3c(NC4CC5CCC4C5)ncnc32)[C@H](O)[C@@H]1O 10.1021/jm801456g
50925499 19236 None 0 Human Functional pKi = 8.3 8.3 - 0
Antagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hrAntagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hr
ChEMBL 523 9 2 5 5.9 CC(C)(NC(=O)COc1ccc2[nH]c(=O)c(-c3nccs3)c(CCc3ccccc3)c2c1)c1ccccc1 10.1016/j.bmcl.2010.10.030
CHEMBL1290101 19236 None 0 Human Functional pKi = 8.3 8.3 - 0
Antagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hrAntagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hr
ChEMBL 523 9 2 5 5.9 CC(C)(NC(=O)COc1ccc2[nH]c(=O)c(-c3nccs3)c(CCc3ccccc3)c2c1)c1ccccc1 10.1016/j.bmcl.2010.10.030
10648228 98435 None 0 Human Functional pKi = 8.3 8.3 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 475 9 1 7 3.4 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)N(C)c4ccccc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
CHEMBL275606 98435 None 0 Human Functional pKi = 8.3 8.3 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 475 9 1 7 3.4 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)N(C)c4ccccc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
135484064 2616 None 4 Human Functional pKi = 8.3 8.3 - 1
Antagonist activity against human Adenosine A2b receptorAntagonist activity against human Adenosine A2b receptor
ChEMBL 509 9 2 11 1.9 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)Nc1ccc2c(c1)OCO2 10.1021/jm049418o
390 2616 None 4 Human Functional pKi = 8.3 8.3 - 1
Antagonist activity against human Adenosine A2b receptorAntagonist activity against human Adenosine A2b receptor
ChEMBL 509 9 2 11 1.9 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)Nc1ccc2c(c1)OCO2 10.1021/jm049418o
CHEMBL260331 2616 None 4 Human Functional pKi = 8.3 8.3 - 1
Antagonist activity against human Adenosine A2b receptorAntagonist activity against human Adenosine A2b receptor
ChEMBL 509 9 2 11 1.9 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)Nc1ccc2c(c1)OCO2 10.1021/jm049418o
135484064 2616 None 4 Human Functional pKi = 8.3 8.3 - 1
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 509 9 2 11 1.9 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)Nc1ccc2c(c1)OCO2 10.1016/j.ejmech.2010.04.039
390 2616 None 4 Human Functional pKi = 8.3 8.3 - 1
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 509 9 2 11 1.9 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)Nc1ccc2c(c1)OCO2 10.1016/j.ejmech.2010.04.039
CHEMBL260331 2616 None 4 Human Functional pKi = 8.3 8.3 - 1
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 509 9 2 11 1.9 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)Nc1ccc2c(c1)OCO2 10.1016/j.ejmech.2010.04.039
52942359 19194 None 0 Human Functional pKi = 6.3 6.3 - 0
Antagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hrAntagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hr
ChEMBL 517 9 2 4 5.8 CC(C)(NC(=O)COc1ccc2[nH]c(=O)c(-c3ccccn3)c(CCc3ccccc3)c2c1)c1ccccc1 10.1016/j.bmcl.2010.10.030
CHEMBL1289778 19194 None 0 Human Functional pKi = 6.3 6.3 - 0
Antagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hrAntagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hr
ChEMBL 517 9 2 4 5.8 CC(C)(NC(=O)COc1ccc2[nH]c(=O)c(-c3ccccn3)c(CCc3ccccc3)c2c1)c1ccccc1 10.1016/j.bmcl.2010.10.030
76313600 103703 None 0 Human Functional pKi = 5.3 5.3 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 439 7 1 7 4.4 Cn1c(-c2ccco2)nc2c(NC(=O)Cc3ccc(OCc4ccccc4)cc3)ncnc21 10.1016/j.ejmech.2013.10.006
CHEMBL3087711 103703 None 0 Human Functional pKi = 5.3 5.3 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 439 7 1 7 4.4 Cn1c(-c2ccco2)nc2c(NC(=O)Cc3ccc(OCc4ccccc4)cc3)ncnc21 10.1016/j.ejmech.2013.10.006
44572471 180607 None 2 Human Functional pKi = 5.3 5.3 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 271 3 2 6 0.6 Nc1ncnc2c1nc(Br)n2CCCO 10.1016/j.bmc.2009.02.030
44572471 180607 None 2 Human Functional pKi = 5.3 5.3 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 271 3 2 6 0.6 Nc1ncnc2c1nc(Br)n2CCCO 10.1016/j.ejmech.2013.10.006
CHEMBL475455 180607 None 2 Human Functional pKi = 5.3 5.3 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 271 3 2 6 0.6 Nc1ncnc2c1nc(Br)n2CCCO 10.1016/j.bmc.2009.02.030
CHEMBL475455 180607 None 2 Human Functional pKi = 5.3 5.3 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 271 3 2 6 0.6 Nc1ncnc2c1nc(Br)n2CCCO 10.1016/j.ejmech.2013.10.006
52942501 19272 None 0 Human Functional pKi = 5.3 5.3 - 0
Antagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hrAntagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hr
ChEMBL 515 8 2 5 5.6 CC(C)(NC(=O)COc1ccc2[nH]c(=O)c(-c3nccs3)c(CCC(F)(F)F)c2c1)c1ccccc1 10.1016/j.bmcl.2010.10.030
CHEMBL1290324 19272 None 0 Human Functional pKi = 5.3 5.3 - 0
Antagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hrAntagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hr
ChEMBL 515 8 2 5 5.6 CC(C)(NC(=O)COc1ccc2[nH]c(=O)c(-c3nccs3)c(CCC(F)(F)F)c2c1)c1ccccc1 10.1016/j.bmcl.2010.10.030
71455620 82933 None 0 Human Functional pKi = 5.3 5.3 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 387 6 1 8 3.7 CC(CCc1ccccc1)Nc1nc2nn(C)cc2c2nc(-c3ccco3)nn12 10.1021/jm300899q
CHEMBL2181140 82933 None 0 Human Functional pKi = 5.3 5.3 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 387 6 1 8 3.7 CC(CCc1ccccc1)Nc1nc2nn(C)cc2c2nc(-c3ccco3)nn12 10.1021/jm300899q
71452056 82922 None 0 Human Functional pKi = 5.3 5.3 - 0
Antagonist activity at human A2B receptor expressed in CHO cell membrane assessed as reduction in NECA-stimulated adenylyl cyclase activity in presence of [alpha32P]ATPAntagonist activity at human A2B receptor expressed in CHO cell membrane assessed as reduction in NECA-stimulated adenylyl cyclase activity in presence of [alpha32P]ATP
ChEMBL 359 4 1 8 3.4 C[C@H](Nc1nc2nn(C)cc2c2nc(-c3ccco3)nn12)c1ccccc1 10.1039/d0md00380h
CHEMBL2180931 82922 None 0 Human Functional pKi = 5.3 5.3 - 0
Antagonist activity at human A2B receptor expressed in CHO cell membrane assessed as reduction in NECA-stimulated adenylyl cyclase activity in presence of [alpha32P]ATPAntagonist activity at human A2B receptor expressed in CHO cell membrane assessed as reduction in NECA-stimulated adenylyl cyclase activity in presence of [alpha32P]ATP
ChEMBL 359 4 1 8 3.4 C[C@H](Nc1nc2nn(C)cc2c2nc(-c3ccco3)nn12)c1ccccc1 10.1039/d0md00380h
71452056 82922 None 0 Human Functional pKi = 5.3 5.3 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 359 4 1 8 3.4 C[C@H](Nc1nc2nn(C)cc2c2nc(-c3ccco3)nn12)c1ccccc1 10.1021/jm300899q
CHEMBL2180931 82922 None 0 Human Functional pKi = 5.3 5.3 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 359 4 1 8 3.4 C[C@H](Nc1nc2nn(C)cc2c2nc(-c3ccco3)nn12)c1ccccc1 10.1021/jm300899q
11602451 162253 None 0 Human Functional pKi = 5.3 5.3 - 0
Antagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assay
ChEMBL 335 5 1 5 4.6 CCCn1c(-c2ccccc2)nc2c(NC3CCCCC3)ncnc21 10.1016/j.ejmech.2018.03.067
CHEMBL4163601 162253 None 0 Human Functional pKi = 5.3 5.3 - 0
Antagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assay
ChEMBL 335 5 1 5 4.6 CCCn1c(-c2ccccc2)nc2c(NC3CCCCC3)ncnc21 10.1016/j.ejmech.2018.03.067
118707844 113103 None 0 Human Functional pKi = 5.3 5.3 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 348 5 2 7 1.9 Nc1ncc(C(=O)NCCc2ccccc2)c2nc(-c3ccco3)nn12 10.1021/jm500752h
CHEMBL3313941 113103 None 0 Human Functional pKi = 5.3 5.3 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 348 5 2 7 1.9 Nc1ncc(C(=O)NCCc2ccccc2)c2nc(-c3ccco3)nn12 10.1021/jm500752h
136414902 159714 None 0 Human Functional pKi = 6.3 6.3 - 0
Antagonist activity at human adenosine receptor A2b expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP level preincubated for 15 mins followed by NECA stimulation for 15 mins by HTRF assayAntagonist activity at human adenosine receptor A2b expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP level preincubated for 15 mins followed by NECA stimulation for 15 mins by HTRF assay
ChEMBL 560 9 1 9 3.8 CCCn1c(=O)c2[nH]c(-c3cc(OCC4CC(=O)N(c5ccc(C(F)(F)F)cc5)C4)no3)nc2n(CCC)c1=O 10.1016/j.ejmech.2016.11.007
CHEMBL4104450 159714 None 0 Human Functional pKi = 6.3 6.3 - 0
Antagonist activity at human adenosine receptor A2b expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP level preincubated for 15 mins followed by NECA stimulation for 15 mins by HTRF assayAntagonist activity at human adenosine receptor A2b expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP level preincubated for 15 mins followed by NECA stimulation for 15 mins by HTRF assay
ChEMBL 560 9 1 9 3.8 CCCn1c(=O)c2[nH]c(-c3cc(OCC4CC(=O)N(c5ccc(C(F)(F)F)cc5)C4)no3)nc2n(CCC)c1=O 10.1016/j.ejmech.2016.11.007
1329 1472 None 86 Human Functional pKi = 7.3 7.3 -9 8
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 10.1016/j.ejmech.2010.04.039
386 1472 None 86 Human Functional pKi = 7.3 7.3 -9 8
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 10.1016/j.ejmech.2010.04.039
CHEMBL183 1472 None 86 Human Functional pKi = 7.3 7.3 -9 8
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 10.1016/j.ejmech.2010.04.039
DB12946 1472 None 86 Human Functional pKi = 7.3 7.3 -9 8
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 10.1016/j.ejmech.2010.04.039
52933926 156182 None 0 Human Functional pKi = 6.3 6.3 - 0
Antagonist activity at human adenosine A2B receptor expressed in HEK293 cells assessed as reduction in NECA-induced increase in cAMP level preincubated for 15 mins followed by NECA addition measured after 15 mins by HTRF assayAntagonist activity at human adenosine A2B receptor expressed in HEK293 cells assessed as reduction in NECA-induced increase in cAMP level preincubated for 15 mins followed by NECA addition measured after 15 mins by HTRF assay
ChEMBL 353 5 1 6 3.7 CCCn1c(Oc2cccnc2C)nc2nc(C3CCCC3)[nH]c2c1=O 10.1016/j.bmc.2017.02.029
CHEMBL4063997 156182 None 0 Human Functional pKi = 6.3 6.3 - 0
Antagonist activity at human adenosine A2B receptor expressed in HEK293 cells assessed as reduction in NECA-induced increase in cAMP level preincubated for 15 mins followed by NECA addition measured after 15 mins by HTRF assayAntagonist activity at human adenosine A2B receptor expressed in HEK293 cells assessed as reduction in NECA-induced increase in cAMP level preincubated for 15 mins followed by NECA addition measured after 15 mins by HTRF assay
ChEMBL 353 5 1 6 3.7 CCCn1c(Oc2cccnc2C)nc2nc(C3CCCC3)[nH]c2c1=O 10.1016/j.bmc.2017.02.029
11608719 188742 None 24 Human Functional pKi = 5.3 5.3 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 269 3 1 5 2.0 CCCCn1c(Br)nc2c(N)ncnc21 10.1016/j.bmc.2009.02.030
CHEMBL505089 188742 None 24 Human Functional pKi = 5.3 5.3 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 269 3 1 5 2.0 CCCCn1c(Br)nc2c(N)ncnc21 10.1016/j.bmc.2009.02.030
11623708 162503 None 0 Human Functional pKi = 5.2 5.2 - 0
Antagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assay
ChEMBL 307 4 1 5 3.9 CCn1c(-c2ccccc2)nc2c(NC3CCCC3)ncnc21 10.1016/j.ejmech.2018.03.067
CHEMBL4167491 162503 None 0 Human Functional pKi = 5.2 5.2 - 0
Antagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assay
ChEMBL 307 4 1 5 3.9 CCn1c(-c2ccccc2)nc2c(NC3CCCC3)ncnc21 10.1016/j.ejmech.2018.03.067
11774068 94564 None 0 Human Functional pKi = 8.2 8.2 - 0
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 404 4 2 6 2.4 CCn1c(=O)[nH]c2nc(-c3cnn(Cc4cccc(C(F)(F)F)c4)c3)[nH]c2c1=O 10.1016/j.ejmech.2010.04.039
CHEMBL251876 94564 None 0 Human Functional pKi = 8.2 8.2 - 0
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 404 4 2 6 2.4 CCn1c(=O)[nH]c2nc(-c3cnn(Cc4cccc(C(F)(F)F)c4)c3)[nH]c2c1=O 10.1016/j.ejmech.2010.04.039
10158974 155506 None 0 Human Functional pKi = 8.2 8.2 - 0
Antagonist activity at Adenosine receptor subtype 2B in human RBC assessed as change in erythrocyte morphology incubated for 3 hrs with occasional gentle stirring for every 30 min measured for every 12 hrs by microscopic analysisAntagonist activity at Adenosine receptor subtype 2B in human RBC assessed as change in erythrocyte morphology incubated for 3 hrs with occasional gentle stirring for every 30 min measured for every 12 hrs by microscopic analysis
ChEMBL 418 5 2 6 2.8 CCCn1c(=O)[nH]c2nc(-c3cnn(Cc4cccc(C(F)(F)F)c4)c3)[nH]c2c1=O 10.1016/j.ejmech.2017.05.035
CHEMBL404168 155506 None 0 Human Functional pKi = 8.2 8.2 - 0
Antagonist activity at Adenosine receptor subtype 2B in human RBC assessed as change in erythrocyte morphology incubated for 3 hrs with occasional gentle stirring for every 30 min measured for every 12 hrs by microscopic analysisAntagonist activity at Adenosine receptor subtype 2B in human RBC assessed as change in erythrocyte morphology incubated for 3 hrs with occasional gentle stirring for every 30 min measured for every 12 hrs by microscopic analysis
ChEMBL 418 5 2 6 2.8 CCCn1c(=O)[nH]c2nc(-c3cnn(Cc4cccc(C(F)(F)F)c4)c3)[nH]c2c1=O 10.1016/j.ejmech.2017.05.035
CHEMBL5076192 214419 None 0 Human Functional pKi = 8.2 8.2 - 0
Antagonist activity at human adenosine A2B receptor expressed in Flp-In-CHO cell membrane assessed as inhibition of NECA-induced cAMP accumulation in presence of forskolin measured after 40 mins by alpha screen LANCE assayAntagonist activity at human adenosine A2B receptor expressed in Flp-In-CHO cell membrane assessed as inhibition of NECA-induced cAMP accumulation in presence of forskolin measured after 40 mins by alpha screen LANCE assay
ChEMBL None None None CCCCn1c(=O)c2nc(C34CCC(C(=O)NCCCCCCCCN=[N+]=[N-])(CC3)CC4)[nH]c2n(CCCNC(=O)c2ccc(S(=O)(=O)F)cc2)c1=O 10.1021/acs.jmedchem.0c02169
443 755 None 10 Human Functional pKi = 7.2 7.2 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 382 7 2 6 2.5 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)/C=C/C(=O)O 10.1021/jm990421v
6439089 755 None 10 Human Functional pKi = 7.2 7.2 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 382 7 2 6 2.5 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)/C=C/C(=O)O 10.1021/jm990421v
CHEMBL16997 755 None 10 Human Functional pKi = 7.2 7.2 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 382 7 2 6 2.5 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)/C=C/C(=O)O 10.1021/jm990421v
52941244 19251 None 0 Human Functional pKi = 7.2 7.2 - 0
Antagonist activity at adenosien A2B receptor in human HMC-1 cells assessed as inhibition of NECA-induced IL-8 release after 6 hr by ELISAAntagonist activity at adenosien A2B receptor in human HMC-1 cells assessed as inhibition of NECA-induced IL-8 release after 6 hr by ELISA
ChEMBL 509 9 2 5 5.7 C[C@@H](NC(=O)COc1ccc2[nH]c(=O)c(-c3nccs3)c(CCc3ccccc3)c2c1)c1ccccc1 10.1016/j.bmcl.2010.10.030
CHEMBL1290209 19251 None 0 Human Functional pKi = 7.2 7.2 - 0
Antagonist activity at adenosien A2B receptor in human HMC-1 cells assessed as inhibition of NECA-induced IL-8 release after 6 hr by ELISAAntagonist activity at adenosien A2B receptor in human HMC-1 cells assessed as inhibition of NECA-induced IL-8 release after 6 hr by ELISA
ChEMBL 509 9 2 5 5.7 C[C@@H](NC(=O)COc1ccc2[nH]c(=O)c(-c3nccs3)c(CCc3ccccc3)c2c1)c1ccccc1 10.1016/j.bmcl.2010.10.030
118732285 118365 None 0 Human Functional pKi = 4.2 4.2 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity
ChEMBL 311 5 1 7 1.8 CCOC(=O)c1nc(N)nc2nn(CCc3ccccc3)cc12 10.1016/j.ejmech.2015.01.046
CHEMBL3410301 118365 None 0 Human Functional pKi = 4.2 4.2 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity
ChEMBL 311 5 1 7 1.8 CCOC(=O)c1nc(N)nc2nn(CCc3ccccc3)cc12 10.1016/j.ejmech.2015.01.046
11681092 162711 None 0 Human Functional pKi = 5.2 5.2 - 1
Antagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assay
ChEMBL 307 3 1 5 3.7 Cc1cccc(-c2nc3c(NC4CCCC4)ncnc3n2C)c1 10.1016/j.ejmech.2018.03.067
CHEMBL4170850 162711 None 0 Human Functional pKi = 5.2 5.2 - 1
Antagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assay
ChEMBL 307 3 1 5 3.7 Cc1cccc(-c2nc3c(NC4CCCC4)ncnc3n2C)c1 10.1016/j.ejmech.2018.03.067
145991283 166846 None 0 Human Functional pKi = 5.2 5.2 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated adenylyl cyclase activity by [alpha-32P]ATP based assayAntagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated adenylyl cyclase activity by [alpha-32P]ATP based assay
ChEMBL 364 6 2 9 3.0 CCOC(=O)c1cnc(NNc2ccccc2)n2nc(-c3ccco3)nc12 10.1016/j.ejmech.2018.08.042
CHEMBL4285374 166846 None 0 Human Functional pKi = 5.2 5.2 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated adenylyl cyclase activity by [alpha-32P]ATP based assayAntagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated adenylyl cyclase activity by [alpha-32P]ATP based assay
ChEMBL 364 6 2 9 3.0 CCOC(=O)c1cnc(NNc2ccccc2)n2nc(-c3ccco3)nc12 10.1016/j.ejmech.2018.08.042
52944930 19294 None 0 Human Functional pKi = 7.2 7.2 - 0
Antagonist activity at adenosien A2B receptor in human HMC-1 cells assessed as inhibition of NECA-induced IL-8 release after 6 hr by ELISAAntagonist activity at adenosien A2B receptor in human HMC-1 cells assessed as inhibition of NECA-induced IL-8 release after 6 hr by ELISA
ChEMBL 495 9 2 5 5.1 O=C(COc1ccc2[nH]c(=O)c(-c3nccs3)c(CCc3ccccc3)c2c1)NCc1ccccc1 10.1016/j.bmcl.2010.10.030
CHEMBL1290436 19294 None 0 Human Functional pKi = 7.2 7.2 - 0
Antagonist activity at adenosien A2B receptor in human HMC-1 cells assessed as inhibition of NECA-induced IL-8 release after 6 hr by ELISAAntagonist activity at adenosien A2B receptor in human HMC-1 cells assessed as inhibition of NECA-induced IL-8 release after 6 hr by ELISA
ChEMBL 495 9 2 5 5.1 O=C(COc1ccc2[nH]c(=O)c(-c3nccs3)c(CCc3ccccc3)c2c1)NCc1ccccc1 10.1016/j.bmcl.2010.10.030
76324475 103705 None 0 Human Functional pKi = 5.2 5.2 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 334 3 2 6 3.3 Cn1c(-c2ccco2)nc2c(NC(=O)Nc3ccccc3)ncnc21 10.1016/j.ejmech.2013.10.006
CHEMBL3087713 103705 None 0 Human Functional pKi = 5.2 5.2 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 334 3 2 6 3.3 Cn1c(-c2ccco2)nc2c(NC(=O)Nc3ccccc3)ncnc21 10.1016/j.ejmech.2013.10.006
18440528 136632 None 0 Human Functional pKi = 5.2 5.2 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 388 7 2 6 3.6 CCCn1c(Br)nc2c(N)nc(NCCCc3ccccc3)nc21 10.1039/C5MD00034C
CHEMBL3739922 136632 None 0 Human Functional pKi = 5.2 5.2 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 388 7 2 6 3.6 CCCn1c(Br)nc2c(N)nc(NCCCc3ccccc3)nc21 10.1039/C5MD00034C
71453894 82955 None 0 Human Functional pKi = 5.2 5.2 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 337 3 1 8 3.0 Cn1cc2c(nc(NC3CCCCC3)n3nc(-c4ccco4)nc23)n1 10.1021/jm300899q
CHEMBL2181161 82955 None 0 Human Functional pKi = 5.2 5.2 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 337 3 1 8 3.0 Cn1cc2c(nc(NC3CCCCC3)n3nc(-c4ccco4)nc23)n1 10.1021/jm300899q
52948671 19313 None 0 Human Functional pKi = 6.2 6.2 - 0
Antagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hrAntagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hr
ChEMBL 520 11 1 5 4.8 COCCCNC(=O)COc1ccc2c(c1)c(CCc1ccccc1)c(-c1ccc(F)cc1F)c(=O)n2C 10.1016/j.bmcl.2010.10.030
CHEMBL1290544 19313 None 0 Human Functional pKi = 6.2 6.2 - 0
Antagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hrAntagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hr
ChEMBL 520 11 1 5 4.8 COCCCNC(=O)COc1ccc2c(c1)c(CCc1ccccc1)c(-c1ccc(F)cc1F)c(=O)n2C 10.1016/j.bmcl.2010.10.030
44572473 180763 None 2 Human Functional pKi = 6.2 6.2 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 271 2 2 6 0.6 CC(O)Cn1c(Br)nc2c(N)ncnc21 10.1016/j.bmc.2009.02.030
CHEMBL475617 180763 None 2 Human Functional pKi = 6.2 6.2 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 271 2 2 6 0.6 CC(O)Cn1c(Br)nc2c(N)ncnc21 10.1016/j.bmc.2009.02.030
132941757 158899 None 0 Human Functional pKi = 6.2 6.2 - 0
Antagonist activity at human adenosine A2B receptor expressed in HEK293 cell membranes assessed as decrease in NECA/forskolin-induced cAMP level pretreated for 15 mins followed by agonist addition for 15 mins and subsequent forskolin stimulation measured after 30 minsAntagonist activity at human adenosine A2B receptor expressed in HEK293 cell membranes assessed as decrease in NECA/forskolin-induced cAMP level pretreated for 15 mins followed by agonist addition for 15 mins and subsequent forskolin stimulation measured after 30 mins
ChEMBL 460 7 1 7 4.4 CCN(CC)C1CCC(C)(C(=O)Nc2nc3c(OC)ccc(N4CCOCC4)c3s2)CC1 10.1021/acs.jmedchem.6b01584
CHEMBL4095355 158899 None 0 Human Functional pKi = 6.2 6.2 - 0
Antagonist activity at human adenosine A2B receptor expressed in HEK293 cell membranes assessed as decrease in NECA/forskolin-induced cAMP level pretreated for 15 mins followed by agonist addition for 15 mins and subsequent forskolin stimulation measured after 30 minsAntagonist activity at human adenosine A2B receptor expressed in HEK293 cell membranes assessed as decrease in NECA/forskolin-induced cAMP level pretreated for 15 mins followed by agonist addition for 15 mins and subsequent forskolin stimulation measured after 30 mins
ChEMBL 460 7 1 7 4.4 CCN(CC)C1CCC(C)(C(=O)Nc2nc3c(OC)ccc(N4CCOCC4)c3s2)CC1 10.1021/acs.jmedchem.6b01584
137631671 156333 None 0 Human Functional pKi = 6.2 6.2 - 0
Antagonist activity at human adenosine A2B receptor expressed in HEK293 cells assessed as reduction in NECA-induced increase in cAMP level preincubated for 15 mins followed by NECA addition measured after 15 mins by HTRF assayAntagonist activity at human adenosine A2B receptor expressed in HEK293 cells assessed as reduction in NECA-induced increase in cAMP level preincubated for 15 mins followed by NECA addition measured after 15 mins by HTRF assay
ChEMBL 352 5 1 5 3.9 CCCn1c(-c2cccc(OC)c2)nc2nc(C3CCCC3)[nH]c2c1=O 10.1016/j.bmc.2017.02.029
CHEMBL4065762 156333 None 0 Human Functional pKi = 6.2 6.2 - 0
Antagonist activity at human adenosine A2B receptor expressed in HEK293 cells assessed as reduction in NECA-induced increase in cAMP level preincubated for 15 mins followed by NECA addition measured after 15 mins by HTRF assayAntagonist activity at human adenosine A2B receptor expressed in HEK293 cells assessed as reduction in NECA-induced increase in cAMP level preincubated for 15 mins followed by NECA addition measured after 15 mins by HTRF assay
ChEMBL 352 5 1 5 3.9 CCCn1c(-c2cccc(OC)c2)nc2nc(C3CCCC3)[nH]c2c1=O 10.1016/j.bmc.2017.02.029
71450242 82956 None 0 Human Functional pKi = 5.2 5.2 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 351 3 1 8 3.4 Cn1cc2c(nc(NC3CCCCCC3)n3nc(-c4ccco4)nc23)n1 10.1021/jm300899q
CHEMBL2181162 82956 None 0 Human Functional pKi = 5.2 5.2 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 351 3 1 8 3.4 Cn1cc2c(nc(NC3CCCCCC3)n3nc(-c4ccco4)nc23)n1 10.1021/jm300899q
52950000 19126 None 0 Human Functional pKi = 6.2 6.2 - 0
Antagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hrAntagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hr
ChEMBL 505 8 2 4 5.2 N#Cc1c(CCc2ccccc2)c2cc(OCC(=O)NCc3ccc(Cl)c(Cl)c3)ccc2[nH]c1=O 10.1016/j.bmcl.2010.10.030
CHEMBL1289344 19126 None 0 Human Functional pKi = 6.2 6.2 - 0
Antagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hrAntagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hr
ChEMBL 505 8 2 4 5.2 N#Cc1c(CCc2ccccc2)c2cc(OCC(=O)NCc3ccc(Cl)c(Cl)c3)ccc2[nH]c1=O 10.1016/j.bmcl.2010.10.030
52949755 19238 None 0 Human Functional pKi = 5.2 5.2 - 0
Antagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hrAntagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hr
ChEMBL 468 6 2 5 3.2 Cc1c(S(C)(=O)=O)c(=O)[nH]c2ccc(OCC(=O)NCc3ccc(Cl)c(Cl)c3)cc12 10.1016/j.bmcl.2010.10.030
CHEMBL1290103 19238 None 0 Human Functional pKi = 5.2 5.2 - 0
Antagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hrAntagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hr
ChEMBL 468 6 2 5 3.2 Cc1c(S(C)(=O)=O)c(=O)[nH]c2ccc(OCC(=O)NCc3ccc(Cl)c(Cl)c3)cc12 10.1016/j.bmcl.2010.10.030
52948949 19270 None 0 Human Functional pKi = 7.2 7.2 - 0
Antagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hrAntagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hr
ChEMBL 494 8 3 4 5.4 O=C(NCc1ccccc1)NCc1ccc2[nH]c(=O)c(-c3nccs3)c(CCc3ccccc3)c2c1 10.1016/j.bmcl.2010.10.030
CHEMBL1290322 19270 None 0 Human Functional pKi = 7.2 7.2 - 0
Antagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hrAntagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hr
ChEMBL 494 8 3 4 5.4 O=C(NCc1ccccc1)NCc1ccc2[nH]c(=O)c(-c3nccs3)c(CCc3ccccc3)c2c1 10.1016/j.bmcl.2010.10.030
10226014 94591 None 0 Human Functional pKi = 8.2 8.2 - 0
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 452 6 2 9 2.4 CCCn1c(=O)[nH]c2nc(-c3cnn(Cc4noc(-c5ccc(Cl)cc5)n4)c3)[nH]c2c1=O 10.1016/j.ejmech.2010.04.039
CHEMBL252048 94591 None 0 Human Functional pKi = 8.2 8.2 - 0
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 452 6 2 9 2.4 CCCn1c(=O)[nH]c2nc(-c3cnn(Cc4noc(-c5ccc(Cl)cc5)n4)c3)[nH]c2c1=O 10.1016/j.ejmech.2010.04.039
52950040 19160 None 0 Human Functional pKi = 8.1 8.1 - 0
Antagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hrAntagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hr
ChEMBL 523 10 2 5 6.1 CC[C@H](NC(=O)COc1ccc2[nH]c(=O)c(-c3nccs3)c(CCc3ccccc3)c2c1)c1ccccc1 10.1016/j.bmcl.2010.10.030
CHEMBL1289569 19160 None 0 Human Functional pKi = 8.1 8.1 - 0
Antagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hrAntagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hr
ChEMBL 523 10 2 5 6.1 CC[C@H](NC(=O)COc1ccc2[nH]c(=O)c(-c3nccs3)c(CCc3ccccc3)c2c1)c1ccccc1 10.1016/j.bmcl.2010.10.030
404 4098 None 33 Human Functional pKi = 8.1 8.1 1318 2
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 428 10 3 8 0.8 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)NCCN 10.1021/jm990421v
432 4098 None 33 Human Functional pKi = 8.1 8.1 1318 2
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 428 10 3 8 0.8 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)NCCN 10.1021/jm990421v
5697 4098 None 33 Human Functional pKi = 8.1 8.1 1318 2
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 428 10 3 8 0.8 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)NCCN 10.1021/jm990421v
CHEMBL273094 4098 None 33 Human Functional pKi = 8.1 8.1 1318 2
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 428 10 3 8 0.8 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)NCCN 10.1021/jm990421v
9827467 98387 None 0 Human Functional pKi = 8.1 8.1 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 504 10 3 8 2.5 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccc(C(N)=O)cc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
CHEMBL275360 98387 None 0 Human Functional pKi = 8.1 8.1 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 504 10 3 8 2.5 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccc(C(N)=O)cc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
135921140 11343 None 0 Mouse Functional pKi = 5.2 5.2 - 0
Inhibition against A2B-Adenosine Receptor in mouse NIH 3T3 fibroblast cell membranes (functional antagonist activity)Inhibition against A2B-Adenosine Receptor in mouse NIH 3T3 fibroblast cell membranes (functional antagonist activity)
ChEMBL 267 1 1 4 1.7 Cn1c(-c2ccccc2)nc2c1C1=NCCN1C(=O)N2 10.1021/jm011093d
CHEMBL117962 11343 None 0 Mouse Functional pKi = 5.2 5.2 - 0
Inhibition against A2B-Adenosine Receptor in mouse NIH 3T3 fibroblast cell membranes (functional antagonist activity)Inhibition against A2B-Adenosine Receptor in mouse NIH 3T3 fibroblast cell membranes (functional antagonist activity)
ChEMBL 267 1 1 4 1.7 Cn1c(-c2ccccc2)nc2c1C1=NCCN1C(=O)N2 10.1021/jm011093d
52946114 19273 None 0 Human Functional pKi = 7.2 7.2 - 0
Antagonist activity at adenosien A2B receptor in human HMC-1 cells assessed as inhibition of NECA-induced IL-8 release after 6 hr by ELISAAntagonist activity at adenosien A2B receptor in human HMC-1 cells assessed as inhibition of NECA-induced IL-8 release after 6 hr by ELISA
ChEMBL 525 9 2 6 5.7 CC(C)(NC(=O)COc1ccc2[nH]c(=O)c(-c3nccs3)c(COc3ccccc3)c2c1)c1ccccc1 10.1016/j.bmcl.2010.10.030
CHEMBL1290325 19273 None 0 Human Functional pKi = 7.2 7.2 - 0
Antagonist activity at adenosien A2B receptor in human HMC-1 cells assessed as inhibition of NECA-induced IL-8 release after 6 hr by ELISAAntagonist activity at adenosien A2B receptor in human HMC-1 cells assessed as inhibition of NECA-induced IL-8 release after 6 hr by ELISA
ChEMBL 525 9 2 6 5.7 CC(C)(NC(=O)COc1ccc2[nH]c(=O)c(-c3nccs3)c(COc3ccccc3)c2c1)c1ccccc1 10.1016/j.bmcl.2010.10.030
69029783 156327 None 0 Human Functional pKi = 7.2 7.2 - 0
Antagonist activity at human adenosine receptor A2b expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP level preincubated for 15 mins followed by NECA stimulation for 15 mins by HTRF assayAntagonist activity at human adenosine receptor A2b expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP level preincubated for 15 mins followed by NECA stimulation for 15 mins by HTRF assay
ChEMBL 570 9 1 8 4.2 CCCn1c(=O)c2[nH]c(-c3ccc(OCC4CC(=O)N(c5ccc(C(F)(F)F)cc5)C4)nc3)nc2n(CCC)c1=O 10.1016/j.ejmech.2016.11.007
CHEMBL4065717 156327 None 0 Human Functional pKi = 7.2 7.2 - 0
Antagonist activity at human adenosine receptor A2b expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP level preincubated for 15 mins followed by NECA stimulation for 15 mins by HTRF assayAntagonist activity at human adenosine receptor A2b expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP level preincubated for 15 mins followed by NECA stimulation for 15 mins by HTRF assay
ChEMBL 570 9 1 8 4.2 CCCn1c(=O)c2[nH]c(-c3ccc(OCC4CC(=O)N(c5ccc(C(F)(F)F)cc5)C4)nc3)nc2n(CCC)c1=O 10.1016/j.ejmech.2016.11.007
2773172 188777 None 12 Human Functional pKi = 5.2 5.2 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 287 3 3 7 -0.5 Nc1ncnc2c1nc(Br)n2CC(O)CO 10.1016/j.bmc.2009.02.030
CHEMBL505633 188777 None 12 Human Functional pKi = 5.2 5.2 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 287 3 3 7 -0.5 Nc1ncnc2c1nc(Br)n2CC(O)CO 10.1016/j.bmc.2009.02.030
118707879 113257 None 0 Human Functional pKi = 5.2 5.2 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 329 6 1 8 2.6 CCOC(=O)c1cnc(NCC(C)C)n2nc(-c3ccco3)nc12 10.1021/jm500752h
CHEMBL3314913 113257 None 0 Human Functional pKi = 5.2 5.2 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 329 6 1 8 2.6 CCOC(=O)c1cnc(NCC(C)C)n2nc(-c3ccco3)nc12 10.1021/jm500752h
822296 189113 None 18 Human Functional pKi = 6.1 6.1 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 227 0 1 5 0.7 Cn1c(Br)nc2c(N)ncnc21 10.1016/j.bmc.2009.02.030
822296 189113 None 18 Human Functional pKi = 6.1 6.1 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 227 0 1 5 0.7 Cn1c(Br)nc2c(N)ncnc21 10.1016/j.ejmech.2013.10.006
CHEMBL510288 189113 None 18 Human Functional pKi = 6.1 6.1 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 227 0 1 5 0.7 Cn1c(Br)nc2c(N)ncnc21 10.1016/j.bmc.2009.02.030
CHEMBL510288 189113 None 18 Human Functional pKi = 6.1 6.1 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 227 0 1 5 0.7 Cn1c(Br)nc2c(N)ncnc21 10.1016/j.ejmech.2013.10.006
71457403 82935 None 0 Human Functional pKi = 5.1 5.1 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 299 4 2 9 0.7 Cn1cc2c(nc(NCCO)n3nc(-c4ccco4)nc23)n1 10.1021/jm300899q
CHEMBL2181142 82935 None 0 Human Functional pKi = 5.1 5.1 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 299 4 2 9 0.7 Cn1cc2c(nc(NCCO)n3nc(-c4ccco4)nc23)n1 10.1021/jm300899q
127040410 136770 None 0 Human Functional pKi = 5.1 5.1 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 345 5 1 5 3.6 CCCn1c(Br)nc2c(NCc3ccccc3)ncnc21 10.1039/C5MD00034C
CHEMBL3741167 136770 None 0 Human Functional pKi = 5.1 5.1 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 345 5 1 5 3.6 CCCn1c(Br)nc2c(NCc3ccccc3)ncnc21 10.1039/C5MD00034C
71455601 82909 None 0 Human Functional pKi = 5.1 5.1 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 375 6 1 9 2.8 Cn1cc2c(nc(NCCOc3ccccc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm300899q
CHEMBL2180918 82909 None 0 Human Functional pKi = 5.1 5.1 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 375 6 1 9 2.8 Cn1cc2c(nc(NCCOc3ccccc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm300899q
71452072 82948 None 0 Human Functional pKi = 5.1 5.1 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 353 7 1 8 3.7 CCCCCC(C)Nc1nc2nn(C)cc2c2nc(-c3ccco3)nn12 10.1021/jm300899q
CHEMBL2181154 82948 None 0 Human Functional pKi = 5.1 5.1 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 353 7 1 8 3.7 CCCCCC(C)Nc1nc2nn(C)cc2c2nc(-c3ccco3)nn12 10.1021/jm300899q
11565780 162280 None 0 Human Functional pKi = 6.1 6.1 - 0
Antagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assay
ChEMBL 307 5 1 5 3.9 CCCn1c(-c2ccccc2)nc2c(NC3CCC3)ncnc21 10.1016/j.ejmech.2018.03.067
CHEMBL4164048 162280 None 0 Human Functional pKi = 6.1 6.1 - 0
Antagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assay
ChEMBL 307 5 1 5 3.9 CCCn1c(-c2ccccc2)nc2c(NC3CCC3)ncnc21 10.1016/j.ejmech.2018.03.067
308531 165721 None 10 Human Functional pKi = 5.1 5.1 - 0
Antagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assay
ChEMBL 225 1 1 5 1.6 Cn1c(-c2ccccc2)nc2c(N)ncnc21 10.1016/j.ejmech.2018.03.067
CHEMBL424597 165721 None 10 Human Functional pKi = 5.1 5.1 - 0
Antagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assay
ChEMBL 225 1 1 5 1.6 Cn1c(-c2ccccc2)nc2c(N)ncnc21 10.1016/j.ejmech.2018.03.067
76324476 103708 None 0 Human Functional pKi = 6.1 6.1 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 215 1 1 6 1.2 Cn1c(-c2ccco2)nc2c(N)ncnc21 10.1016/j.ejmech.2013.10.006
CHEMBL3087716 103708 None 0 Human Functional pKi = 6.1 6.1 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 215 1 1 6 1.2 Cn1c(-c2ccco2)nc2c(N)ncnc21 10.1016/j.ejmech.2013.10.006
CHEMBL5073669 214301 None 0 Human Functional pKi = 7.1 7.1 - 0
Antagonist activity at human adenosine A2B receptor expressed in Flp-In-CHO cell membrane assessed as inhibition of NECA-induced cAMP accumulation in presence of forskolin measured after 40 mins by alpha screen LANCE assayAntagonist activity at human adenosine A2B receptor expressed in Flp-In-CHO cell membrane assessed as inhibition of NECA-induced cAMP accumulation in presence of forskolin measured after 40 mins by alpha screen LANCE assay
ChEMBL None None None CCCCn1c(=O)c2nc(C34CCC(C(=O)NCCCN=[N+]=[N-])(CC3)CC4)[nH]c2n(CCCNC(=O)c2ccc(S(=O)(=O)F)cc2)c1=O 10.1021/acs.jmedchem.0c02169
76309882 103702 None 0 Human Functional pKi = 6.1 6.1 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 409 5 1 6 4.4 Cn1c(-c2ccco2)nc2c(NC(=O)C(c3ccccc3)c3ccccc3)ncnc21 10.1016/j.ejmech.2013.10.006
CHEMBL3087710 103702 None 0 Human Functional pKi = 6.1 6.1 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 409 5 1 6 4.4 Cn1c(-c2ccco2)nc2c(NC(=O)C(c3ccccc3)c3ccccc3)ncnc21 10.1016/j.ejmech.2013.10.006
44236568 156470 None 0 Human Functional pKi = 8.1 8.1 - 1
Antagonist activity at human adenosine A2B receptor expressed in HEK293 cells assessed as inhibition of NECA-induced increase in cAMP accumulation incubated for 15 mins followed by agonist treatment for 15 mins by HTRF assayAntagonist activity at human adenosine A2B receptor expressed in HEK293 cells assessed as inhibition of NECA-induced increase in cAMP accumulation incubated for 15 mins followed by agonist treatment for 15 mins by HTRF assay
ChEMBL 486 6 1 8 3.1 CCCn1c(=O)c2[nH]c(-c3cnn(CC#Cc4cccc(OC(F)(F)F)c4)c3)nc2n(CC)c1=O 10.1016/j.ejmech.2017.04.014
CHEMBL4067401 156470 None 0 Human Functional pKi = 8.1 8.1 - 1
Antagonist activity at human adenosine A2B receptor expressed in HEK293 cells assessed as inhibition of NECA-induced increase in cAMP accumulation incubated for 15 mins followed by agonist treatment for 15 mins by HTRF assayAntagonist activity at human adenosine A2B receptor expressed in HEK293 cells assessed as inhibition of NECA-induced increase in cAMP accumulation incubated for 15 mins followed by agonist treatment for 15 mins by HTRF assay
ChEMBL 486 6 1 8 3.1 CCCn1c(=O)c2[nH]c(-c3cnn(CC#Cc4cccc(OC(F)(F)F)c4)c3)nc2n(CC)c1=O 10.1016/j.ejmech.2017.04.014
69031481 157077 None 0 Human Functional pKi = 8.1 8.1 - 0
Antagonist activity at human adenosine A2B receptor expressed in HEK293 cells assessed as inhibition of cAMP productionAntagonist activity at human adenosine A2B receptor expressed in HEK293 cells assessed as inhibition of cAMP production
ChEMBL 529 7 1 8 3.3 CCCn1c(=O)c2[nH]c(-c3cnn(CC4CC(=O)N(c5ccc(C(F)(F)F)cc5)C4)c3)nc2n(CC)c1=O 10.1016/j.ejmech.2021.113907
CHEMBL4074253 157077 None 0 Human Functional pKi = 8.1 8.1 - 0
Antagonist activity at human adenosine A2B receptor expressed in HEK293 cells assessed as inhibition of cAMP productionAntagonist activity at human adenosine A2B receptor expressed in HEK293 cells assessed as inhibition of cAMP production
ChEMBL 529 7 1 8 3.3 CCCn1c(=O)c2[nH]c(-c3cnn(CC4CC(=O)N(c5ccc(C(F)(F)F)cc5)C4)c3)nc2n(CC)c1=O 10.1016/j.ejmech.2021.113907
57429602 157239 None 0 Human Functional pKi = 8.1 8.1 - 1
Antagonist activity at human adenosine A2B receptor expressed in HEK293 cells assessed as inhibition of cAMP productionAntagonist activity at human adenosine A2B receptor expressed in HEK293 cells assessed as inhibition of cAMP production
ChEMBL 500 7 1 8 3.5 CCCn1c(=O)c2[nH]c(-c3cnn(CC#Cc4cccc(OC(F)(F)F)c4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2021.113907
CHEMBL4076435 157239 None 0 Human Functional pKi = 8.1 8.1 - 1
Antagonist activity at human adenosine A2B receptor expressed in HEK293 cells assessed as inhibition of cAMP productionAntagonist activity at human adenosine A2B receptor expressed in HEK293 cells assessed as inhibition of cAMP production
ChEMBL 500 7 1 8 3.5 CCCn1c(=O)c2[nH]c(-c3cnn(CC#Cc4cccc(OC(F)(F)F)c4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2021.113907
69031481 157077 None 0 Human Functional pKi = 8.1 8.1 - 0
Antagonist activity at human adenosine receptor A2b expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP level preincubated for 15 mins followed by NECA stimulation for 15 mins by HTRF assayAntagonist activity at human adenosine receptor A2b expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP level preincubated for 15 mins followed by NECA stimulation for 15 mins by HTRF assay
ChEMBL 529 7 1 8 3.3 CCCn1c(=O)c2[nH]c(-c3cnn(CC4CC(=O)N(c5ccc(C(F)(F)F)cc5)C4)c3)nc2n(CC)c1=O 10.1016/j.ejmech.2016.11.007
CHEMBL4074253 157077 None 0 Human Functional pKi = 8.1 8.1 - 0
Antagonist activity at human adenosine receptor A2b expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP level preincubated for 15 mins followed by NECA stimulation for 15 mins by HTRF assayAntagonist activity at human adenosine receptor A2b expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP level preincubated for 15 mins followed by NECA stimulation for 15 mins by HTRF assay
ChEMBL 529 7 1 8 3.3 CCCn1c(=O)c2[nH]c(-c3cnn(CC4CC(=O)N(c5ccc(C(F)(F)F)cc5)C4)c3)nc2n(CC)c1=O 10.1016/j.ejmech.2016.11.007
57429602 157239 None 0 Human Functional pKi = 8.1 8.1 - 1
Antagonist activity at human adenosine A2B receptor expressed in HEK293 cells assessed as inhibition of NECA-induced increase in cAMP accumulation incubated for 15 mins followed by agonist treatment for 15 mins by HTRF assayAntagonist activity at human adenosine A2B receptor expressed in HEK293 cells assessed as inhibition of NECA-induced increase in cAMP accumulation incubated for 15 mins followed by agonist treatment for 15 mins by HTRF assay
ChEMBL 500 7 1 8 3.5 CCCn1c(=O)c2[nH]c(-c3cnn(CC#Cc4cccc(OC(F)(F)F)c4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2017.04.014
CHEMBL4076435 157239 None 0 Human Functional pKi = 8.1 8.1 - 1
Antagonist activity at human adenosine A2B receptor expressed in HEK293 cells assessed as inhibition of NECA-induced increase in cAMP accumulation incubated for 15 mins followed by agonist treatment for 15 mins by HTRF assayAntagonist activity at human adenosine A2B receptor expressed in HEK293 cells assessed as inhibition of NECA-induced increase in cAMP accumulation incubated for 15 mins followed by agonist treatment for 15 mins by HTRF assay
ChEMBL 500 7 1 8 3.5 CCCn1c(=O)c2[nH]c(-c3cnn(CC#Cc4cccc(OC(F)(F)F)c4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2017.04.014
72197883 90801 None 0 Human Functional pKi = 5.1 5.1 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 407 5 2 9 3.2 CN(C)c1nc(N)nc(-c2sc(NC(=O)c3ccco3)nc2-c2ccccc2)n1 10.1016/j.ejmech.2013.03.020
CHEMBL2391837 90801 None 0 Human Functional pKi = 5.1 5.1 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 407 5 2 9 3.2 CN(C)c1nc(N)nc(-c2sc(NC(=O)c3ccco3)nc2-c2ccccc2)n1 10.1016/j.ejmech.2013.03.020
52946114 19273 None 0 Human Functional pKi = 7.1 7.1 - 0
Antagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hrAntagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hr
ChEMBL 525 9 2 6 5.7 CC(C)(NC(=O)COc1ccc2[nH]c(=O)c(-c3nccs3)c(COc3ccccc3)c2c1)c1ccccc1 10.1016/j.bmcl.2010.10.030
CHEMBL1290325 19273 None 0 Human Functional pKi = 7.1 7.1 - 0
Antagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hrAntagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hr
ChEMBL 525 9 2 6 5.7 CC(C)(NC(=O)COc1ccc2[nH]c(=O)c(-c3nccs3)c(COc3ccccc3)c2c1)c1ccccc1 10.1016/j.bmcl.2010.10.030
439176 98621 None 71 Human Functional pKi = 5.1 5.1 - 2
Binding affinity towards human adenosine A2B receptor in VA13 fibroblasts as inhibition of adenylate cyclase at 10 uM; Less than 10% inhibitionBinding affinity towards human adenosine A2B receptor in VA13 fibroblasts as inhibition of adenylate cyclase at 10 uM; Less than 10% inhibition
ChEMBL 297 3 3 9 -0.6 CSC[C@H]1O[C@@H](n2cnc3c(N)ncnc32)[C@H](O)[C@@H]1O 10.1021/jm031092g
CHEMBL277041 98621 None 71 Human Functional pKi = 5.1 5.1 - 2
Binding affinity towards human adenosine A2B receptor in VA13 fibroblasts as inhibition of adenylate cyclase at 10 uM; Less than 10% inhibitionBinding affinity towards human adenosine A2B receptor in VA13 fibroblasts as inhibition of adenylate cyclase at 10 uM; Less than 10% inhibition
ChEMBL 297 3 3 9 -0.6 CSC[C@H]1O[C@@H](n2cnc3c(N)ncnc32)[C@H](O)[C@@H]1O 10.1021/jm031092g
127040064 136751 None 0 Human Functional pKi = 5.1 5.1 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 376 8 2 7 4.1 CCCn1c(-c2ccco2)nc2c(N)nc(NCCCc3ccccc3)nc21 10.1039/C5MD00034C
CHEMBL3740992 136751 None 0 Human Functional pKi = 5.1 5.1 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 376 8 2 7 4.1 CCCn1c(-c2ccco2)nc2c(N)nc(NCCCc3ccccc3)nc21 10.1039/C5MD00034C
44447519 94886 None 0 Human Functional pKi = 5.1 5.1 - 0
Agonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activity
ChEMBL 440 5 4 10 1.2 CNC(=O)OC[C@H]1O[C@@H](n2cnc3c(NC4CCCC4)nc(Cl)nc32)[C@](C)(O)[C@@H]1O 10.1016/j.bmc.2007.09.035
CHEMBL254064 94886 None 0 Human Functional pKi = 5.1 5.1 - 0
Agonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activity
ChEMBL 440 5 4 10 1.2 CNC(=O)OC[C@H]1O[C@@H](n2cnc3c(NC4CCCC4)nc(Cl)nc32)[C@](C)(O)[C@@H]1O 10.1016/j.bmc.2007.09.035
25188209 178759 None 0 Human Functional pKi = 6.1 6.1 - 0
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 311 3 1 8 1.6 Nc1nc(-c2ncco2)c2nnn(Cc3ccccc3F)c2n1 10.1016/j.ejmech.2010.04.039
CHEMBL468701 178759 None 0 Human Functional pKi = 6.1 6.1 - 0
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 311 3 1 8 1.6 Nc1nc(-c2ncco2)c2nnn(Cc3ccccc3F)c2n1 10.1016/j.ejmech.2010.04.039
5248753 178753 None 6 Human Functional pKi = 6.1 6.1 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 241 1 1 5 1.2 CCn1c(Br)nc2c(N)ncnc21 10.1016/j.bmc.2009.02.030
5248753 178753 None 6 Human Functional pKi = 6.1 6.1 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 241 1 1 5 1.2 CCn1c(Br)nc2c(N)ncnc21 10.1016/j.ejmech.2013.10.006
CHEMBL468633 178753 None 6 Human Functional pKi = 6.1 6.1 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 241 1 1 5 1.2 CCn1c(Br)nc2c(N)ncnc21 10.1016/j.bmc.2009.02.030
CHEMBL468633 178753 None 6 Human Functional pKi = 6.1 6.1 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 241 1 1 5 1.2 CCn1c(Br)nc2c(N)ncnc21 10.1016/j.ejmech.2013.10.006
72197703 90797 None 0 Human Functional pKi = 6.1 6.1 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 347 4 1 5 4.7 O=C(Nc1nc(-c2ccccc2)c(-c2ccccn2)s1)c1ccco1 10.1016/j.ejmech.2013.03.020
CHEMBL2391833 90797 None 0 Human Functional pKi = 6.1 6.1 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 347 4 1 5 4.7 O=C(Nc1nc(-c2ccccc2)c(-c2ccccn2)s1)c1ccco1 10.1016/j.ejmech.2013.03.020
71457389 82907 None 0 Human Functional pKi = 5.1 5.1 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 285 3 1 9 1.2 CONc1nc2nn(C)cc2c2nc(-c3ccco3)nn12 10.1021/jm300899q
CHEMBL2180916 82907 None 0 Human Functional pKi = 5.1 5.1 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 285 3 1 9 1.2 CONc1nc2nn(C)cc2c2nc(-c3ccco3)nn12 10.1021/jm300899q
11587409 162996 None 0 Human Functional pKi = 5.1 5.1 - 1
Antagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assay
ChEMBL 293 3 1 5 3.4 Cn1c(-c2ccccc2)nc2c(NC3CCCC3)ncnc21 10.1016/j.ejmech.2018.03.067
CHEMBL4175366 162996 None 0 Human Functional pKi = 5.1 5.1 - 1
Antagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assay
ChEMBL 293 3 1 5 3.4 Cn1c(-c2ccccc2)nc2c(NC3CCCC3)ncnc21 10.1016/j.ejmech.2018.03.067
12016633 172670 None 1 Human Functional pKi = 6.1 6.1 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 281 1 1 5 2.3 Nc1ncnc2c1nc(Br)n2C1CCCC1 10.1016/j.bmc.2009.02.030
CHEMBL449924 172670 None 1 Human Functional pKi = 6.1 6.1 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 281 1 1 5 2.3 Nc1ncnc2c1nc(Br)n2C1CCCC1 10.1016/j.bmc.2009.02.030
9946338 154789 None 43 Human Functional pKi = 6.1 6.1 - 0
Agonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activity
ChEMBL 349 4 4 9 0.2 C[C@@]1(O)[C@H](O)[C@@H](CO)O[C@H]1n1cnc2c(NC3CCCC3)ncnc21 10.1016/j.bmc.2007.09.035
CHEMBL400189 154789 None 43 Human Functional pKi = 6.1 6.1 - 0
Agonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activityAgonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activity
ChEMBL 349 4 4 9 0.2 C[C@@]1(O)[C@H](O)[C@@H](CO)O[C@H]1n1cnc2c(NC3CCCC3)ncnc21 10.1016/j.bmc.2007.09.035
52941201 19224 None 0 Human Functional pKi = 6.1 6.1 - 0
Antagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hrAntagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hr
ChEMBL 517 9 2 4 5.8 CC(C)(NC(=O)COc1ccc2[nH]c(=O)c(-c3ccncc3)c(CCc3ccccc3)c2c1)c1ccccc1 10.1016/j.bmcl.2010.10.030
CHEMBL1290002 19224 None 0 Human Functional pKi = 6.1 6.1 - 0
Antagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hrAntagonist activity at human adenosine A2B receptor transfected in CHO cells assessed as inhibition of NECA-induced cAMP accumulation treated 15 mins before NECA challenge measured after 1 hr
ChEMBL 517 9 2 4 5.8 CC(C)(NC(=O)COc1ccc2[nH]c(=O)c(-c3ccncc3)c(CCc3ccccc3)c2c1)c1ccccc1 10.1016/j.bmcl.2010.10.030
10267860 176823 None 0 Human Functional pKi = 6.1 6.1 - 0
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 317 3 1 8 2.0 N#Cc1ccc(Cn2nnc3c(-c4ccco4)nc(N)nc32)cc1 10.1016/j.ejmech.2010.04.039
CHEMBL461007 176823 None 0 Human Functional pKi = 6.1 6.1 - 0
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 317 3 1 8 2.0 N#Cc1ccc(Cn2nnc3c(-c4ccco4)nc(N)nc32)cc1 10.1016/j.ejmech.2010.04.039
11198201 110677 None 7 Human Functional pKi = 8.1 8.1 - 0
Antagonist activity against human Adenosine A2b receptorAntagonist activity against human Adenosine A2b receptor
ChEMBL 327 5 2 6 2.0 CCCn1c(=O)c2nc(-c3ccc(N)cc3)[nH]c2n(CCC)c1=O 10.1021/jm049418o
CHEMBL32598 110677 None 7 Human Functional pKi = 8.1 8.1 - 0
Antagonist activity against human Adenosine A2b receptorAntagonist activity against human Adenosine A2b receptor
ChEMBL 327 5 2 6 2.0 CCCn1c(=O)c2nc(-c3ccc(N)cc3)[nH]c2n(CCC)c1=O 10.1021/jm049418o
14484978 97592 None 0 Human Functional pKi = 8.0 8.0 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 483 9 1 10 1.4 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)ON4C(=O)CCC4=O)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
CHEMBL27081 97592 None 0 Human Functional pKi = 8.0 8.0 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 483 9 1 10 1.4 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)ON4C(=O)CCC4=O)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
9850900 98351 None 0 Human Functional pKi = 8.0 8.0 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 565 12 1 7 5.0 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)N(Cc4ccccc4)Cc4ccccc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
CHEMBL275149 98351 None 0 Human Functional pKi = 8.0 8.0 - 0
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPXAntagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
ChEMBL 565 12 1 7 5.0 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)N(Cc4ccccc4)Cc4ccccc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm990421v
9850900 98351 None 0 Human Functional pKi = 8.0 8.0 - 0
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 565 12 1 7 5.0 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)N(Cc4ccccc4)Cc4ccccc4)cc3)[nH]c2n(CCC)c1=O 10.1016/j.ejmech.2010.04.039
CHEMBL275149 98351 None 0 Human Functional pKi = 8.0 8.0 - 0
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 565 12 1 7 5.0 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)N(Cc4ccccc4)Cc4ccccc4)cc3)[nH]c2n(CCC)c1=O 10.1016/j.ejmech.2010.04.039
11508049 161982 None 0 Human Functional pKi = 5.0 5.0 - 0
Antagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assay
ChEMBL 321 4 1 5 4.3 CCn1c(-c2ccccc2)nc2c(NC3CCCCC3)ncnc21 10.1016/j.ejmech.2018.03.067
CHEMBL4159165 161982 None 0 Human Functional pKi = 5.0 5.0 - 0
Antagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assay
ChEMBL 321 4 1 5 4.3 CCn1c(-c2ccccc2)nc2c(NC3CCCCC3)ncnc21 10.1016/j.ejmech.2018.03.067
2153 3800 None 115 Human Functional pKi = 5.0 5.0 - 5
Antagonist activity against human Adenosine A2b receptorAntagonist activity against human Adenosine A2b receptor
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1021/jm049418o
2153.0 3800 None 115 Human Functional pKi = 5.0 5.0 - 5
Antagonist activity against human Adenosine A2b receptorAntagonist activity against human Adenosine A2b receptor
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1021/jm049418o
2620 3800 None 115 Human Functional pKi = 5.0 5.0 - 5
Antagonist activity against human Adenosine A2b receptorAntagonist activity against human Adenosine A2b receptor
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1021/jm049418o
413 3800 None 115 Human Functional pKi = 5.0 5.0 - 5
Antagonist activity against human Adenosine A2b receptorAntagonist activity against human Adenosine A2b receptor
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1021/jm049418o
CHEMBL190 3800 None 115 Human Functional pKi = 5.0 5.0 - 5
Antagonist activity against human Adenosine A2b receptorAntagonist activity against human Adenosine A2b receptor
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1021/jm049418o
DB00277 3800 None 115 Human Functional pKi = 5.0 5.0 - 5
Antagonist activity against human Adenosine A2b receptorAntagonist activity against human Adenosine A2b receptor
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1021/jm049418o
2153 3800 None 115 Human Functional pKi = 5.0 5.0 - 5
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1016/j.ejmech.2010.04.039
2153.0 3800 None 115 Human Functional pKi = 5.0 5.0 - 5
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1016/j.ejmech.2010.04.039
2620 3800 None 115 Human Functional pKi = 5.0 5.0 - 5
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1016/j.ejmech.2010.04.039
413 3800 None 115 Human Functional pKi = 5.0 5.0 - 5
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1016/j.ejmech.2010.04.039
CHEMBL190 3800 None 115 Human Functional pKi = 5.0 5.0 - 5
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1016/j.ejmech.2010.04.039
DB00277 3800 None 115 Human Functional pKi = 5.0 5.0 - 5
Antagonist activity against human adenosine A2B receptorAntagonist activity against human adenosine A2B receptor
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1016/j.ejmech.2010.04.039
2153 3800 None 115 Human Functional pKi = 5.0 5.0 - 5
Antagonist activity at adenosine A2B receptor (unknown origin)Antagonist activity at adenosine A2B receptor (unknown origin)
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1016/j.ejmech.2021.113907
2153.0 3800 None 115 Human Functional pKi = 5.0 5.0 - 5
Antagonist activity at adenosine A2B receptor (unknown origin)Antagonist activity at adenosine A2B receptor (unknown origin)
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1016/j.ejmech.2021.113907
2620 3800 None 115 Human Functional pKi = 5.0 5.0 - 5
Antagonist activity at adenosine A2B receptor (unknown origin)Antagonist activity at adenosine A2B receptor (unknown origin)
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1016/j.ejmech.2021.113907
413 3800 None 115 Human Functional pKi = 5.0 5.0 - 5
Antagonist activity at adenosine A2B receptor (unknown origin)Antagonist activity at adenosine A2B receptor (unknown origin)
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1016/j.ejmech.2021.113907
CHEMBL190 3800 None 115 Human Functional pKi = 5.0 5.0 - 5
Antagonist activity at adenosine A2B receptor (unknown origin)Antagonist activity at adenosine A2B receptor (unknown origin)
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1016/j.ejmech.2021.113907
DB00277 3800 None 115 Human Functional pKi = 5.0 5.0 - 5
Antagonist activity at adenosine A2B receptor (unknown origin)Antagonist activity at adenosine A2B receptor (unknown origin)
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1016/j.ejmech.2021.113907
11681354 162936 None 0 Human Functional pKi = 5.0 5.0 - 0
Antagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assay
ChEMBL 323 5 1 6 3.1 CCCn1c(-c2ccccc2)nc2c(NC3CCOC3)ncnc21 10.1016/j.ejmech.2018.03.067
CHEMBL4174308 162936 None 0 Human Functional pKi = 5.0 5.0 - 0
Antagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assayAntagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assay
ChEMBL 323 5 1 6 3.1 CCCn1c(-c2ccccc2)nc2c(NC3CCOC3)ncnc21 10.1016/j.ejmech.2018.03.067
72197701 90795 None 0 Human Functional pKi = 5.0 5.0 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 375 5 1 6 4.3 O=C(Nc1nc(-c2ccccc2)c(C(=O)c2ccccn2)s1)c1ccco1 10.1016/j.ejmech.2013.03.020
CHEMBL2391831 90795 None 0 Human Functional pKi = 5.0 5.0 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 375 5 1 6 4.3 O=C(Nc1nc(-c2ccccc2)c(C(=O)c2ccccn2)s1)c1ccco1 10.1016/j.ejmech.2013.03.020
18440431 136644 None 0 Human Functional pKi = 5.0 5.0 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 296 6 2 6 2.5 CCCn1cnc2c(N)nc(NCCc3ccccc3)nc21 10.1039/C5MD00034C
CHEMBL3739985 136644 None 0 Human Functional pKi = 5.0 5.0 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 296 6 2 6 2.5 CCCn1cnc2c(N)nc(NCCc3ccccc3)nc21 10.1039/C5MD00034C
127042994 136788 None 0 Human Functional pKi = 5.0 5.0 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 347 7 1 6 4.2 CCCn1c(-c2ccco2)nc2c(NCCc3ccccc3)ncnc21 10.1039/C5MD00034C
CHEMBL3741337 136788 None 0 Human Functional pKi = 5.0 5.0 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
ChEMBL 347 7 1 6 4.2 CCCn1c(-c2ccco2)nc2c(NCCc3ccccc3)ncnc21 10.1039/C5MD00034C
71453891 82936 None 0 Human Functional pKi = 5.0 5.0 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 313 5 2 9 1.1 Cn1cc2c(nc(NCCCO)n3nc(-c4ccco4)nc23)n1 10.1021/jm300899q
CHEMBL2181143 82936 None 0 Human Functional pKi = 5.0 5.0 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 313 5 2 9 1.1 Cn1cc2c(nc(NCCCO)n3nc(-c4ccco4)nc23)n1 10.1021/jm300899q
CHEMBL5088372 215155 None 0 Human Functional pKi = 7.0 7.0 - 0
Antagonist activity at human adenosine A2B receptor expressed in Flp-In-CHO cell membrane assessed as inhibition of NECA-induced cAMP accumulation in presence of forskolin measured after 40 mins by alpha screen LANCE assayAntagonist activity at human adenosine A2B receptor expressed in Flp-In-CHO cell membrane assessed as inhibition of NECA-induced cAMP accumulation in presence of forskolin measured after 40 mins by alpha screen LANCE assay
ChEMBL None None None CCCCn1c(=O)c2nc(C34CCC(C(=O)NCCOCCOCCOCCN=[N+]=[N-])(CC3)CC4)[nH]c2n(CCCNC(=O)c2ccc(S(=O)(=O)F)cc2)c1=O 10.1021/acs.jmedchem.0c02169
71462775 82958 None 0 Human Functional pKi = 5.0 5.0 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 351 4 1 8 3.3 Cn1cc2c(nc(NCC3CCCCC3)n3nc(-c4ccco4)nc23)n1 10.1021/jm300899q
CHEMBL2181164 82958 None 0 Human Functional pKi = 5.0 5.0 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 351 4 1 8 3.3 Cn1cc2c(nc(NCC3CCCCC3)n3nc(-c4ccco4)nc23)n1 10.1021/jm300899q
71457404 82942 None 0 Human Functional pKi = 5.0 5.0 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 297 3 1 8 2.1 CC(C)Nc1nc2nn(C)cc2c2nc(-c3ccco3)nn12 10.1021/jm300899q
CHEMBL2181149 82942 None 0 Human Functional pKi = 5.0 5.0 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 297 3 1 8 2.1 CC(C)Nc1nc2nn(C)cc2c2nc(-c3ccco3)nn12 10.1021/jm300899q
71455604 82925 None 0 Human Functional pKi = 5.0 5.0 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 375 5 1 9 2.9 COc1ccc(CNc2nc3nn(C)cc3c3nc(-c4ccco4)nn23)cc1 10.1021/jm300899q
CHEMBL2180934 82925 None 0 Human Functional pKi = 5.0 5.0 - 0
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activityAntagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
ChEMBL 375 5 1 9 2.9 COc1ccc(CNc2nc3nn(C)cc3c3nc(-c4ccco4)nn23)cc1 10.1021/jm300899q
162657141 180923 None 0 Human Functional pKi = 5.0 5.0 - 0
Antagonist activity at human A2B receptor expressed in CHO cell membrane assessed as reduction in NECA-stimulated adenylyl cyclase activity in presence of [alpha32P]ATPAntagonist activity at human A2B receptor expressed in CHO cell membrane assessed as reduction in NECA-stimulated adenylyl cyclase activity in presence of [alpha32P]ATP
ChEMBL 371 6 2 11 0.6 CCOC(=O)C(CO)Nc1nc2nn(C)cc2c2nc(-c3ccco3)nn12 10.1039/d0md00380h
CHEMBL4757966 180923 None 0 Human Functional pKi = 5.0 5.0 - 0
Antagonist activity at human A2B receptor expressed in CHO cell membrane assessed as reduction in NECA-stimulated adenylyl cyclase activity in presence of [alpha32P]ATPAntagonist activity at human A2B receptor expressed in CHO cell membrane assessed as reduction in NECA-stimulated adenylyl cyclase activity in presence of [alpha32P]ATP
ChEMBL 371 6 2 11 0.6 CCOC(=O)C(CO)Nc1nc2nn(C)cc2c2nc(-c3ccco3)nn12 10.1039/d0md00380h
2690 903 None 66 Human Functional pA2 = 7.8 7.8 -31 5
UnclassifiedUnclassified
Guide to Pharmacology 285 1 1 6 2.8 Clc1ccc2c(c1)c1nc(nn1c(n2)N)c1ccco1 8937736
384 903 None 66 Human Functional pA2 = 7.8 7.8 -31 5
UnclassifiedUnclassified
Guide to Pharmacology 285 1 1 6 2.8 Clc1ccc2c(c1)c1nc(nn1c(n2)N)c1ccco1 8937736
CHEMBL16687 903 None 66 Human Functional pA2 = 7.8 7.8 -31 5
UnclassifiedUnclassified
Guide to Pharmacology 285 1 1 6 2.8 Clc1ccc2c(c1)c1nc(nn1c(n2)N)c1ccco1 8937736
404 4098 None 33 Human Functional pA2 = 7.9 7.9 1318 2
UnclassifiedUnclassified
Guide to Pharmacology 428 10 3 8 0.8 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)NCCN 8937736
432 4098 None 33 Human Functional pA2 = 7.9 7.9 1318 2
UnclassifiedUnclassified
Guide to Pharmacology 428 10 3 8 0.8 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)NCCN 8937736
5697 4098 None 33 Human Functional pA2 = 7.9 7.9 1318 2
UnclassifiedUnclassified
Guide to Pharmacology 428 10 3 8 0.8 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)NCCN 8937736
CHEMBL273094 4098 None 33 Human Functional pA2 = 7.9 7.9 1318 2
UnclassifiedUnclassified
Guide to Pharmacology 428 10 3 8 0.8 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)NCCN 8937736
2844 283 None 107 Human Functional pEC50 = 8.3 8.3 -16 5
NoneNone
Drug Central 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N None
60961 283 None 107 Human Functional pEC50 = 8.3 8.3 -16 5
NoneNone
Drug Central 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N None
60961.0 283 None 107 Human Functional pEC50 = 8.3 8.3 -16 5
NoneNone
Drug Central 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N None
90 283 None 107 Human Functional pEC50 = 8.3 8.3 -16 5
NoneNone
Drug Central 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N None
CHEMBL477 283 None 107 Human Functional pEC50 = 8.3 8.3 -16 5
NoneNone
Drug Central 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N None
DB00640 283 None 107 Human Functional pEC50 = 8.3 8.3 -16 5
NoneNone
Drug Central 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N None
219024 3300 None 65 Human Functional pEC50 = 8.3 8.3 -51 5
Agonist activity at human recombinant adenosine receptor A2b by cAMP assayAgonist activity at human recombinant adenosine receptor A2b by cAMP assay
Drug Central 390 4 5 12 -2.4 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(nc2N)n1ncc(c1)C(=O)NC None
219024.0 3300 None 65 Human Functional pEC50 = 8.3 8.3 -51 5
Agonist activity at human recombinant adenosine receptor A2b by cAMP assayAgonist activity at human recombinant adenosine receptor A2b by cAMP assay
Drug Central 390 4 5 12 -2.4 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(nc2N)n1ncc(c1)C(=O)NC None
2362 3300 None 65 Human Functional pEC50 = 8.3 8.3 -51 5
Agonist activity at human recombinant adenosine receptor A2b by cAMP assayAgonist activity at human recombinant adenosine receptor A2b by cAMP assay
Drug Central 390 4 5 12 -2.4 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(nc2N)n1ncc(c1)C(=O)NC None
5596 3300 None 65 Human Functional pEC50 = 8.3 8.3 -51 5
Agonist activity at human recombinant adenosine receptor A2b by cAMP assayAgonist activity at human recombinant adenosine receptor A2b by cAMP assay
Drug Central 390 4 5 12 -2.4 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(nc2N)n1ncc(c1)C(=O)NC None
CHEMBL317052 3300 None 65 Human Functional pEC50 = 8.3 8.3 -51 5
Agonist activity at human recombinant adenosine receptor A2b by cAMP assayAgonist activity at human recombinant adenosine receptor A2b by cAMP assay
Drug Central 390 4 5 12 -2.4 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(nc2N)n1ncc(c1)C(=O)NC None
DB06213 3300 None 65 Human Functional pEC50 = 8.3 8.3 -51 5
Agonist activity at human recombinant adenosine receptor A2b by cAMP assayAgonist activity at human recombinant adenosine receptor A2b by cAMP assay
Drug Central 390 4 5 12 -2.4 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(nc2N)n1ncc(c1)C(=O)NC None
11224 582 None 35 Mouse Functional pIC50 = 6.4 6.4 -6 7
UnclassifiedUnclassified
Guide to Pharmacology 433 4 1 7 2.1 CCn1c(=O)c2c(C)c(sc2n(c1=O)CCC(F)(F)F)C(=O)N1CCC(CC1)O 30576906
118016229 582 None 35 Mouse Functional pIC50 = 6.4 6.4 -6 7
UnclassifiedUnclassified
Guide to Pharmacology 433 4 1 7 2.1 CCn1c(=O)c2c(C)c(sc2n(c1=O)CCC(F)(F)F)C(=O)N1CCC(CC1)O 30576906
CHEMBL4522981 582 None 35 Mouse Functional pIC50 = 6.4 6.4 -6 7
UnclassifiedUnclassified
Guide to Pharmacology 433 4 1 7 2.1 CCn1c(=O)c2c(C)c(sc2n(c1=O)CCC(F)(F)F)C(=O)N1CCC(CC1)O 30576906
11224 582 None 35 Rat Functional pIC50 = 6.6 6.6 -4 7
UnclassifiedUnclassified
Guide to Pharmacology 433 4 1 7 2.1 CCn1c(=O)c2c(C)c(sc2n(c1=O)CCC(F)(F)F)C(=O)N1CCC(CC1)O 30576906
118016229 582 None 35 Rat Functional pIC50 = 6.6 6.6 -4 7
UnclassifiedUnclassified
Guide to Pharmacology 433 4 1 7 2.1 CCn1c(=O)c2c(C)c(sc2n(c1=O)CCC(F)(F)F)C(=O)N1CCC(CC1)O 30576906
CHEMBL4522981 582 None 35 Rat Functional pIC50 = 6.6 6.6 -4 7
UnclassifiedUnclassified
Guide to Pharmacology 433 4 1 7 2.1 CCn1c(=O)c2c(C)c(sc2n(c1=O)CCC(F)(F)F)C(=O)N1CCC(CC1)O 30576906


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Ligands (move mouse cursor over ligand name to see structure) Receptor Activity Chemical information
Sel. page Common
name		 GPCRdb
ID		 Reference
ligand		 Vendors

 Species

 Assay
Type		 Activity
Type		 Activity
Relation		 Activity
Value		 p-value
(-log)		 Fold
selectivity		 Tested
GPCRs		 Assay
Description		 Source

 Mol
weight		 Rot
Bonds		 H don

 H acc

 LogP

 Smiles

 DOI
10981286 1919 None 30 Human Binding pEC50 = 4 4.0 -28183 4
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 361 5 4 9 0.0 CCCCC#Cc1nc(NC)c2c(n1)n(cn2)[C@@H]1O[C@@H]([C@H]([C@H]1O)O)CO 10.1021/jm0109762
5599 1919 None 30 Human Binding pEC50 = 4 4.0 -28183 4
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 361 5 4 9 0.0 CCCCC#Cc1nc(NC)c2c(n1)n(cn2)[C@@H]1O[C@@H]([C@H]([C@H]1O)O)CO 10.1021/jm0109762
5736 1919 None 30 Human Binding pEC50 = 4 4.0 -28183 4
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 361 5 4 9 0.0 CCCCC#Cc1nc(NC)c2c(n1)n(cn2)[C@@H]1O[C@@H]([C@H]([C@H]1O)O)CO 10.1021/jm0109762
CHEMBL260563 1919 None 30 Human Binding pEC50 = 4 4.0 -28183 4
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 361 5 4 9 0.0 CCCCC#Cc1nc(NC)c2c(n1)n(cn2)[C@@H]1O[C@@H]([C@H]([C@H]1O)O)CO 10.1021/jm0109762
11014608 96359 None 0 Human Binding pEC50 = 4 4.0 - 3
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 389 6 4 9 0.8 CCCCC#Cc1nc(NC(C)C)c2ncn([C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)c2n1 10.1021/jm0109762
CHEMBL261623 96359 None 0 Human Binding pEC50 = 4 4.0 - 3
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 389 6 4 9 0.8 CCCCC#Cc1nc(NC(C)C)c2ncn([C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)c2n1 10.1021/jm0109762
10020580 107973 None 5 Human Binding pEC50 = 4 4.0 - 5
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 347 4 4 9 -0.4 CCCCC#Cc1nc(N)c2ncn([C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)c2n1 10.1021/jm0109762
CHEMBL319387 107973 None 5 Human Binding pEC50 = 4 4.0 - 5
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 347 4 4 9 -0.4 CCCCC#Cc1nc(N)c2ncn([C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)c2n1 10.1021/jm0109762
11112381 159441 None 0 Human Binding pEC50 = 4 4.0 - 3
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 411 4 5 10 -0.4 CNc1nc(C#C[C@H](O)c2ccccc2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm0109762
CHEMBL410115 159441 None 0 Human Binding pEC50 = 4 4.0 - 3
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 411 4 5 10 -0.4 CNc1nc(C#C[C@H](O)c2ccccc2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm0109762
10970819 168836 None 0 Human Binding pEC50 = 4 4.0 - 3
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 375 6 4 9 0.4 CCCCC#Cc1nc(NCC)c2ncn([C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)c2n1 10.1021/jm0109762
CHEMBL437842 168836 None 0 Human Binding pEC50 = 4 4.0 - 3
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 375 6 4 9 0.4 CCCCC#Cc1nc(NCC)c2ncn([C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)c2n1 10.1021/jm0109762
11068963 198121 None 1 Human Binding pEC50 = 4 4.0 - 3
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 381 3 4 9 -0.1 CNc1nc(C#Cc2ccccc2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm0109762
CHEMBL574597 198121 None 1 Human Binding pEC50 = 4 4.0 - 3
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 381 3 4 9 -0.1 CNc1nc(C#Cc2ccccc2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm0109762
9932840 77898 None 1 Human Binding pEC50 = 6.0 6.0 - 4
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 438 4 5 10 -0.8 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(C#CC(O)c4ccccc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm0109762
CHEMBL2094083 77898 None 1 Human Binding pEC50 = 6.0 6.0 - 4
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 438 4 5 10 -0.8 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(C#CC(O)c4ccccc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm0109762
377 2758 None 53 Human Binding pEC50 = 6.9 6.9 -1479 15
Agonist activity at human A2B adenosine receptor by cell based assayAgonist activity at human A2B adenosine receptor by cell based assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.8b01662
425 2758 None 53 Human Binding pEC50 = 6.9 6.9 -1479 15
Agonist activity at human A2B adenosine receptor by cell based assayAgonist activity at human A2B adenosine receptor by cell based assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.8b01662
448222 2758 None 53 Human Binding pEC50 = 6.9 6.9 -1479 15
Agonist activity at human A2B adenosine receptor by cell based assayAgonist activity at human A2B adenosine receptor by cell based assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.8b01662
CHEMBL464859 2758 None 53 Human Binding pEC50 = 6.9 6.9 -1479 15
Agonist activity at human A2B adenosine receptor by cell based assayAgonist activity at human A2B adenosine receptor by cell based assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.8b01662
377 2758 None 53 Human Binding pEC50 = 4.8 4.8 -1479 15
Agonist activity at human Adenosine A2B receptor expressed in yeast cells coexpressed with chimeric GPA1/Galphas after 16 hrs by beta-galactosidase reporter gene assayAgonist activity at human Adenosine A2B receptor expressed in yeast cells coexpressed with chimeric GPA1/Galphas after 16 hrs by beta-galactosidase reporter gene assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.5b01402
425 2758 None 53 Human Binding pEC50 = 4.8 4.8 -1479 15
Agonist activity at human Adenosine A2B receptor expressed in yeast cells coexpressed with chimeric GPA1/Galphas after 16 hrs by beta-galactosidase reporter gene assayAgonist activity at human Adenosine A2B receptor expressed in yeast cells coexpressed with chimeric GPA1/Galphas after 16 hrs by beta-galactosidase reporter gene assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.5b01402
448222 2758 None 53 Human Binding pEC50 = 4.8 4.8 -1479 15
Agonist activity at human Adenosine A2B receptor expressed in yeast cells coexpressed with chimeric GPA1/Galphas after 16 hrs by beta-galactosidase reporter gene assayAgonist activity at human Adenosine A2B receptor expressed in yeast cells coexpressed with chimeric GPA1/Galphas after 16 hrs by beta-galactosidase reporter gene assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.5b01402
CHEMBL464859 2758 None 53 Human Binding pEC50 = 4.8 4.8 -1479 15
Agonist activity at human Adenosine A2B receptor expressed in yeast cells coexpressed with chimeric GPA1/Galphas after 16 hrs by beta-galactosidase reporter gene assayAgonist activity at human Adenosine A2B receptor expressed in yeast cells coexpressed with chimeric GPA1/Galphas after 16 hrs by beta-galactosidase reporter gene assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.5b01402
70682890 77814 None 5 Human Binding pEC50 = 5.8 5.8 - 3
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 425 5 5 10 -0.0 CCNc1nc(C#CC(O)c2ccccc2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm0109762
CHEMBL2092788 77814 None 5 Human Binding pEC50 = 5.8 5.8 - 3
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 425 5 5 10 -0.0 CCNc1nc(C#CC(O)c2ccccc2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm0109762
23757284 85129 None 0 Human Binding pEC50 = 6.7 6.7 - 3
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 438 4 5 10 -0.8 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(C#C[C@@H](O)c4ccccc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm0109762
CHEMBL224874 85129 None 0 Human Binding pEC50 = 6.7 6.7 - 3
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 438 4 5 10 -0.8 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(C#C[C@@H](O)c4ccccc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm0109762
25268841 8661 None 12 Human Binding pEC50 = 6.6 6.6 - 3
Binding affinity to human recombinant adenosine A2B receptor expressed in CHO cells using [3H]PSB-603 by functional activity assayBinding affinity to human recombinant adenosine A2B receptor expressed in CHO cells using [3H]PSB-603 by functional activity assay
ChEMBL 402 5 1 7 2.6 Nc1nc(-c2ccccc2)c2c(n1)-c1cc(OCCN3CCOCC3)ccc1C2=O 10.1021/acs.jmedchem.0c00914
CHEMBL1095488 8661 None 12 Human Binding pEC50 = 6.6 6.6 - 3
Binding affinity to human recombinant adenosine A2B receptor expressed in CHO cells using [3H]PSB-603 by functional activity assayBinding affinity to human recombinant adenosine A2B receptor expressed in CHO cells using [3H]PSB-603 by functional activity assay
ChEMBL 402 5 1 7 2.6 Nc1nc(-c2ccccc2)c2c(n1)-c1cc(OCCN3CCOCC3)ccc1C2=O 10.1021/acs.jmedchem.0c00914
13830108 77835 None 1 Human Binding pEC50 = 5.6 5.6 - 4
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 397 3 5 10 -0.9 Nc1nc(C#CC(O)c2ccccc2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm0109762
CHEMBL2092941 77835 None 1 Human Binding pEC50 = 5.6 5.6 - 4
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 397 3 5 10 -0.9 Nc1nc(C#CC(O)c2ccccc2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm0109762
23900137 95765 None 0 Human Binding pEC50 = 5.6 5.6 - 3
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 438 4 5 10 -0.8 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(C#C[C@H](O)c4ccccc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm0109762
CHEMBL258534 95765 None 0 Human Binding pEC50 = 5.6 5.6 - 3
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 438 4 5 10 -0.8 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(N)nc(C#C[C@H](O)c4ccccc4)nc32)[C@H](O)[C@@H]1O 10.1021/jm0109762
2844 283 None 107 Human Binding pEC50 = 4.6 4.6 -467 8
Agonist activity at A2B receptor (unknown origin)Agonist activity at A2B receptor (unknown origin)
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.0c01431
60961 283 None 107 Human Binding pEC50 = 4.6 4.6 -467 8
Agonist activity at A2B receptor (unknown origin)Agonist activity at A2B receptor (unknown origin)
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.0c01431
60961.0 283 None 107 Human Binding pEC50 = 4.6 4.6 -467 8
Agonist activity at A2B receptor (unknown origin)Agonist activity at A2B receptor (unknown origin)
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.0c01431
90 283 None 107 Human Binding pEC50 = 4.6 4.6 -467 8
Agonist activity at A2B receptor (unknown origin)Agonist activity at A2B receptor (unknown origin)
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.0c01431
CHEMBL477 283 None 107 Human Binding pEC50 = 4.6 4.6 -467 8
Agonist activity at A2B receptor (unknown origin)Agonist activity at A2B receptor (unknown origin)
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.0c01431
DB00640 283 None 107 Human Binding pEC50 = 4.6 4.6 -467 8
Agonist activity at A2B receptor (unknown origin)Agonist activity at A2B receptor (unknown origin)
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.0c01431
11026001 96327 None 0 Human Binding pEC50 = 5.6 5.6 - 3
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 411 4 5 10 -0.4 CNc1nc(C#C[C@@H](O)c2ccccc2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm0109762
CHEMBL261453 96327 None 0 Human Binding pEC50 = 5.6 5.6 - 3
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 411 4 5 10 -0.4 CNc1nc(C#C[C@@H](O)c2ccccc2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm0109762
69427076 77812 None 0 Human Binding pEC50 = 5.6 5.6 - 3
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 411 4 5 10 -0.4 CNc1nc(C#CC(O)c2ccccc2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm0109762
CHEMBL2092786 77812 None 0 Human Binding pEC50 = 5.6 5.6 - 3
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 411 4 5 10 -0.4 CNc1nc(C#CC(O)c2ccccc2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm0109762
377 2758 None 53 Human Binding pEC50 = 6.5 6.5 -1479 15
Agonist activity at Homo sapiens (human) adenosine A2b receptor expressed in CHO cellsAgonist activity at Homo sapiens (human) adenosine A2b receptor expressed in CHO cells
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1007/s00044-004-0013-y
425 2758 None 53 Human Binding pEC50 = 6.5 6.5 -1479 15
Agonist activity at Homo sapiens (human) adenosine A2b receptor expressed in CHO cellsAgonist activity at Homo sapiens (human) adenosine A2b receptor expressed in CHO cells
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1007/s00044-004-0013-y
448222 2758 None 53 Human Binding pEC50 = 6.5 6.5 -1479 15
Agonist activity at Homo sapiens (human) adenosine A2b receptor expressed in CHO cellsAgonist activity at Homo sapiens (human) adenosine A2b receptor expressed in CHO cells
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1007/s00044-004-0013-y
CHEMBL464859 2758 None 53 Human Binding pEC50 = 6.5 6.5 -1479 15
Agonist activity at Homo sapiens (human) adenosine A2b receptor expressed in CHO cellsAgonist activity at Homo sapiens (human) adenosine A2b receptor expressed in CHO cells
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1007/s00044-004-0013-y
2844 283 None 107 Human Binding pEC50 = 4.3 4.3 -467 8
Agonist activity at human Adenosine A2B receptor expressed in yeast cells coexpressed with chimeric GPA1/Galphas after 16 hrs by beta-galactosidase reporter gene assayAgonist activity at human Adenosine A2B receptor expressed in yeast cells coexpressed with chimeric GPA1/Galphas after 16 hrs by beta-galactosidase reporter gene assay
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.5b01402
60961 283 None 107 Human Binding pEC50 = 4.3 4.3 -467 8
Agonist activity at human Adenosine A2B receptor expressed in yeast cells coexpressed with chimeric GPA1/Galphas after 16 hrs by beta-galactosidase reporter gene assayAgonist activity at human Adenosine A2B receptor expressed in yeast cells coexpressed with chimeric GPA1/Galphas after 16 hrs by beta-galactosidase reporter gene assay
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.5b01402
60961.0 283 None 107 Human Binding pEC50 = 4.3 4.3 -467 8
Agonist activity at human Adenosine A2B receptor expressed in yeast cells coexpressed with chimeric GPA1/Galphas after 16 hrs by beta-galactosidase reporter gene assayAgonist activity at human Adenosine A2B receptor expressed in yeast cells coexpressed with chimeric GPA1/Galphas after 16 hrs by beta-galactosidase reporter gene assay
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.5b01402
90 283 None 107 Human Binding pEC50 = 4.3 4.3 -467 8
Agonist activity at human Adenosine A2B receptor expressed in yeast cells coexpressed with chimeric GPA1/Galphas after 16 hrs by beta-galactosidase reporter gene assayAgonist activity at human Adenosine A2B receptor expressed in yeast cells coexpressed with chimeric GPA1/Galphas after 16 hrs by beta-galactosidase reporter gene assay
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.5b01402
CHEMBL477 283 None 107 Human Binding pEC50 = 4.3 4.3 -467 8
Agonist activity at human Adenosine A2B receptor expressed in yeast cells coexpressed with chimeric GPA1/Galphas after 16 hrs by beta-galactosidase reporter gene assayAgonist activity at human Adenosine A2B receptor expressed in yeast cells coexpressed with chimeric GPA1/Galphas after 16 hrs by beta-galactosidase reporter gene assay
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.5b01402
DB00640 283 None 107 Human Binding pEC50 = 4.3 4.3 -467 8
Agonist activity at human Adenosine A2B receptor expressed in yeast cells coexpressed with chimeric GPA1/Galphas after 16 hrs by beta-galactosidase reporter gene assayAgonist activity at human Adenosine A2B receptor expressed in yeast cells coexpressed with chimeric GPA1/Galphas after 16 hrs by beta-galactosidase reporter gene assay
ChEMBL 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.5b01402
70697521 77813 None 0 Human Binding pEC50 = 5.2 5.2 - 3
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 439 5 5 10 0.3 CC(C)Nc1nc(C#CC(O)c2ccccc2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm0109762
CHEMBL2092787 77813 None 0 Human Binding pEC50 = 5.2 5.2 - 3
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 439 5 5 10 0.3 CC(C)Nc1nc(C#CC(O)c2ccccc2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm0109762
118719026 115435 None 0 Human Binding pEC50 = 5.2 5.2 - 5
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 582 13 4 8 2.1 CC(C)(C)OC(=O)C1CCCN1C[C@@H](O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(N)=O)NC(=O)OCc1ccccc1 10.1021/jm0109762
CHEMBL3350613 115435 None 0 Human Binding pEC50 = 5.2 5.2 - 5
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 582 13 4 8 2.1 CC(C)(C)OC(=O)C1CCCN1C[C@@H](O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(N)=O)NC(=O)OCc1ccccc1 10.1021/jm0109762
9978117 158320 None 0 Human Binding pEC50 = 5.2 5.2 - 3
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 397 3 5 10 -0.9 Nc1nc(C#C[C@H](O)c2ccccc2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm0109762
CHEMBL408918 158320 None 0 Human Binding pEC50 = 5.2 5.2 - 3
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 397 3 5 10 -0.9 Nc1nc(C#C[C@H](O)c2ccccc2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm0109762
123807 871 None 54 Human Binding pEC50 = 4.1 4.1 -13803 13
Agonist activity at human Adenosine A2B receptor expressed in yeast cells coexpressed with chimeric GPA1/Galphas after 16 hrs by beta-galactosidase reporter gene assayAgonist activity at human Adenosine A2B receptor expressed in yeast cells coexpressed with chimeric GPA1/Galphas after 16 hrs by beta-galactosidase reporter gene assay
ChEMBL 369 4 4 9 0.4 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NC1CCCC1 10.1021/acs.jmedchem.5b01402
374 871 None 54 Human Binding pEC50 = 4.1 4.1 -13803 13
Agonist activity at human Adenosine A2B receptor expressed in yeast cells coexpressed with chimeric GPA1/Galphas after 16 hrs by beta-galactosidase reporter gene assayAgonist activity at human Adenosine A2B receptor expressed in yeast cells coexpressed with chimeric GPA1/Galphas after 16 hrs by beta-galactosidase reporter gene assay
ChEMBL 369 4 4 9 0.4 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NC1CCCC1 10.1021/acs.jmedchem.5b01402
379 871 None 54 Human Binding pEC50 = 4.1 4.1 -13803 13
Agonist activity at human Adenosine A2B receptor expressed in yeast cells coexpressed with chimeric GPA1/Galphas after 16 hrs by beta-galactosidase reporter gene assayAgonist activity at human Adenosine A2B receptor expressed in yeast cells coexpressed with chimeric GPA1/Galphas after 16 hrs by beta-galactosidase reporter gene assay
ChEMBL 369 4 4 9 0.4 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NC1CCCC1 10.1021/acs.jmedchem.5b01402
CHEMBL284969 871 None 54 Human Binding pEC50 = 4.1 4.1 -13803 13
Agonist activity at human Adenosine A2B receptor expressed in yeast cells coexpressed with chimeric GPA1/Galphas after 16 hrs by beta-galactosidase reporter gene assayAgonist activity at human Adenosine A2B receptor expressed in yeast cells coexpressed with chimeric GPA1/Galphas after 16 hrs by beta-galactosidase reporter gene assay
ChEMBL 369 4 4 9 0.4 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NC1CCCC1 10.1021/acs.jmedchem.5b01402
10455080 95766 None 0 Human Binding pEC50 = 6.1 6.1 - 3
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 425 5 5 10 -0.0 CCNc1nc(C#C[C@@H](O)c2ccccc2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm0109762
CHEMBL258535 95766 None 0 Human Binding pEC50 = 6.1 6.1 - 3
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 425 5 5 10 -0.0 CCNc1nc(C#C[C@@H](O)c2ccccc2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm0109762
11048438 168898 None 0 Human Binding pEC50 = 5.1 5.1 - 3
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 439 5 5 10 0.3 CC(C)Nc1nc(C#C[C@H](O)c2ccccc2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm0109762
CHEMBL438418 168898 None 0 Human Binding pEC50 = 5.1 5.1 - 3
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 439 5 5 10 0.3 CC(C)Nc1nc(C#C[C@H](O)c2ccccc2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm0109762
11112711 159421 None 0 Human Binding pEC50 = 5.0 5.0 - 3
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 425 5 5 10 -0.0 CCNc1nc(C#C[C@H](O)c2ccccc2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm0109762
CHEMBL410095 159421 None 0 Human Binding pEC50 = 5.0 5.0 - 3
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 425 5 5 10 -0.0 CCNc1nc(C#C[C@H](O)c2ccccc2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm0109762
44450290 96475 None 0 Human Binding pEC50 = 6.0 6.0 - 3
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 397 3 5 10 -0.9 Nc1nc(C#C[C@@H](O)c2ccccc2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm0109762
CHEMBL262363 96475 None 0 Human Binding pEC50 = 6.0 6.0 - 3
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 397 3 5 10 -0.9 Nc1nc(C#C[C@@H](O)c2ccccc2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm0109762
215492 16471 None 3 Human Binding pEC50 = 6.0 6.0 - 3
Agonist activity at human A2B adenosine receptor by cell based assayAgonist activity at human A2B adenosine receptor by cell based assay
ChEMBL 324 4 5 10 -2.9 Nc1ncnc2c1ncn2[C@@H]1O[C@H](C(=O)NCCO)[C@@H](O)[C@H]1O 10.1021/acs.jmedchem.8b01662
CHEMBL1234591 16471 None 3 Human Binding pEC50 = 6.0 6.0 - 3
Agonist activity at human A2B adenosine receptor by cell based assayAgonist activity at human A2B adenosine receptor by cell based assay
ChEMBL 324 4 5 10 -2.9 Nc1ncnc2c1ncn2[C@@H]1O[C@H](C(=O)NCCO)[C@@H](O)[C@H]1O 10.1021/acs.jmedchem.8b01662
10455852 96053 None 0 Human Binding pEC50 = 6.0 6.0 - 3
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 439 5 5 10 0.3 CC(C)Nc1nc(C#C[C@@H](O)c2ccccc2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm0109762
CHEMBL259938 96053 None 0 Human Binding pEC50 = 6.0 6.0 - 3
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligandReceptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand
ChEMBL 439 5 5 10 0.3 CC(C)Nc1nc(C#C[C@@H](O)c2ccccc2)nc2c1ncn2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm0109762
3284 3216 None 35 Human Binding pIC50 = 9.3 9.3 -1 7
Displacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes after 60 mins by flow cytometric methodDisplacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes after 60 mins by flow cytometric method
ChEMBL 528 6 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)c1ccc(cc1)Cl 10.1021/acs.jmedchem.7b01627
44185871 3216 None 35 Human Binding pIC50 = 9.3 9.3 -1 7
Displacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes after 60 mins by flow cytometric methodDisplacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes after 60 mins by flow cytometric method
ChEMBL 528 6 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)c1ccc(cc1)Cl 10.1021/acs.jmedchem.7b01627
5728 3216 None 35 Human Binding pIC50 = 9.3 9.3 -1 7
Displacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes after 60 mins by flow cytometric methodDisplacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes after 60 mins by flow cytometric method
ChEMBL 528 6 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)c1ccc(cc1)Cl 10.1021/acs.jmedchem.7b01627
CHEMBL483688 3216 None 35 Human Binding pIC50 = 9.3 9.3 -1 7
Displacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes after 60 mins by flow cytometric methodDisplacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes after 60 mins by flow cytometric method
ChEMBL 528 6 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)c1ccc(cc1)Cl 10.1021/acs.jmedchem.7b01627
3284 3216 None 35 Human Binding pIC50 = 9.1 9.1 -1 7
Displacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes preincubated for 30 mins followed by PSB-12105 addition measured after 20 mins by flow cytometric methodDisplacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes preincubated for 30 mins followed by PSB-12105 addition measured after 20 mins by flow cytometric method
ChEMBL 528 6 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)c1ccc(cc1)Cl 10.1021/acs.jmedchem.7b01627
44185871 3216 None 35 Human Binding pIC50 = 9.1 9.1 -1 7
Displacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes preincubated for 30 mins followed by PSB-12105 addition measured after 20 mins by flow cytometric methodDisplacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes preincubated for 30 mins followed by PSB-12105 addition measured after 20 mins by flow cytometric method
ChEMBL 528 6 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)c1ccc(cc1)Cl 10.1021/acs.jmedchem.7b01627
5728 3216 None 35 Human Binding pIC50 = 9.1 9.1 -1 7
Displacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes preincubated for 30 mins followed by PSB-12105 addition measured after 20 mins by flow cytometric methodDisplacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes preincubated for 30 mins followed by PSB-12105 addition measured after 20 mins by flow cytometric method
ChEMBL 528 6 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)c1ccc(cc1)Cl 10.1021/acs.jmedchem.7b01627
CHEMBL483688 3216 None 35 Human Binding pIC50 = 9.1 9.1 -1 7
Displacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes preincubated for 30 mins followed by PSB-12105 addition measured after 20 mins by flow cytometric methodDisplacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes preincubated for 30 mins followed by PSB-12105 addition measured after 20 mins by flow cytometric method
ChEMBL 528 6 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)c1ccc(cc1)Cl 10.1021/acs.jmedchem.7b01627
16037920 168762 None 0 Human Binding pIC50 = 9 9.0 - 0
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 571 5 1 7 2.5 Cn1c(=O)c2[nH]c(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc(Br)cc5)CC4)cc3)cc2n(C)c1=O 10.1016/j.bmcl.2006.04.074
CHEMBL437309 168762 None 0 Human Binding pIC50 = 9 9.0 - 0
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 571 5 1 7 2.5 Cn1c(=O)c2[nH]c(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc(Br)cc5)CC4)cc3)cc2n(C)c1=O 10.1016/j.bmcl.2006.04.074
74944536 164589 None 3 Human Binding pIC50 = 9.0 9.0 - 0
Displacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes preincubated for 30 mins followed by PSB-12105 addition measured after 20 mins by flow cytometric methodDisplacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes preincubated for 30 mins followed by PSB-12105 addition measured after 20 mins by flow cytometric method
ChEMBL 540 7 0 7 2.8 CCCN1C(=O)N=C2N=C(c3ccc(S(=O)(=O)N4CCN(Cc5ccc(Cl)cc5)CC4)cc3)N=C2C1=O 10.1021/acs.jmedchem.7b01627
CHEMBL4215606 164589 None 3 Human Binding pIC50 = 9.0 9.0 - 0
Displacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes preincubated for 30 mins followed by PSB-12105 addition measured after 20 mins by flow cytometric methodDisplacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes preincubated for 30 mins followed by PSB-12105 addition measured after 20 mins by flow cytometric method
ChEMBL 540 7 0 7 2.8 CCCN1C(=O)N=C2N=C(c3ccc(S(=O)(=O)N4CCN(Cc5ccc(Cl)cc5)CC4)cc3)N=C2C1=O 10.1021/acs.jmedchem.7b01627
44413112 139305 None 0 Human Binding pIC50 = 8 8.0 - 0
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 511 5 1 7 1.9 Cn1c(=O)c2[nH]c(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc(F)cc5)CC4)cc3)cc2n(C)c1=O 10.1016/j.bmcl.2006.04.074
CHEMBL379217 139305 None 0 Human Binding pIC50 = 8 8.0 - 0
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 511 5 1 7 1.9 Cn1c(=O)c2[nH]c(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc(F)cc5)CC4)cc3)cc2n(C)c1=O 10.1016/j.bmcl.2006.04.074
134148336 148327 None 0 Human Binding pIC50 = 6 6.0 - 2
Displacement of [3H]PSB603 from recombinant human adenosine A2B receptor expressed in HEK293 cell membranes after 1 hr by beta scintillation counting methodDisplacement of [3H]PSB603 from recombinant human adenosine A2B receptor expressed in HEK293 cell membranes after 1 hr by beta scintillation counting method
ChEMBL 395 4 2 4 5.7 O[C@H]1CC[C@H](Nc2ncc(-c3ccc4ccccc4c3)c(-c3ccccc3)n2)CC1 10.1016/j.ejmech.2016.09.081
CHEMBL3937015 148327 None 0 Human Binding pIC50 = 6 6.0 - 2
Displacement of [3H]PSB603 from recombinant human adenosine A2B receptor expressed in HEK293 cell membranes after 1 hr by beta scintillation counting methodDisplacement of [3H]PSB603 from recombinant human adenosine A2B receptor expressed in HEK293 cell membranes after 1 hr by beta scintillation counting method
ChEMBL 395 4 2 4 5.7 O[C@H]1CC[C@H](Nc2ncc(-c3ccc4ccccc4c3)c(-c3ccccc3)n2)CC1 10.1016/j.ejmech.2016.09.081
2519 779 None 86 Human Binding pIC50 = 5.0 5.0 -11 12
Inhibition of human A2b adenosine receptorInhibition of human A2b adenosine receptor
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1021/acs.jmedchem.1c00261
2519.0 779 None 86 Human Binding pIC50 = 5.0 5.0 -11 12
Inhibition of human A2b adenosine receptorInhibition of human A2b adenosine receptor
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1021/acs.jmedchem.1c00261
407 779 None 86 Human Binding pIC50 = 5.0 5.0 -11 12
Inhibition of human A2b adenosine receptorInhibition of human A2b adenosine receptor
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1021/acs.jmedchem.1c00261
463 779 None 86 Human Binding pIC50 = 5.0 5.0 -11 12
Inhibition of human A2b adenosine receptorInhibition of human A2b adenosine receptor
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1021/acs.jmedchem.1c00261
CHEMBL113 779 None 86 Human Binding pIC50 = 5.0 5.0 -11 12
Inhibition of human A2b adenosine receptorInhibition of human A2b adenosine receptor
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1021/acs.jmedchem.1c00261
DB00201 779 None 86 Human Binding pIC50 = 5.0 5.0 -11 12
Inhibition of human A2b adenosine receptorInhibition of human A2b adenosine receptor
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1021/acs.jmedchem.1c00261
44236568 156470 None 0 Human Binding pIC50 = 7.0 7.0 - 1
Antagonist activity at human adenosine A2B receptor expressed in mouse NIH/3T3 cells assessed as inhibition of NECA-induced IL-6 release incubated for 15 mins followed by agonist treatment for 15 mins by HTRF assayAntagonist activity at human adenosine A2B receptor expressed in mouse NIH/3T3 cells assessed as inhibition of NECA-induced IL-6 release incubated for 15 mins followed by agonist treatment for 15 mins by HTRF assay
ChEMBL 486 6 1 8 3.1 CCCn1c(=O)c2[nH]c(-c3cnn(CC#Cc4cccc(OC(F)(F)F)c4)c3)nc2n(CC)c1=O 10.1016/j.ejmech.2017.04.014
CHEMBL4067401 156470 None 0 Human Binding pIC50 = 7.0 7.0 - 1
Antagonist activity at human adenosine A2B receptor expressed in mouse NIH/3T3 cells assessed as inhibition of NECA-induced IL-6 release incubated for 15 mins followed by agonist treatment for 15 mins by HTRF assayAntagonist activity at human adenosine A2B receptor expressed in mouse NIH/3T3 cells assessed as inhibition of NECA-induced IL-6 release incubated for 15 mins followed by agonist treatment for 15 mins by HTRF assay
ChEMBL 486 6 1 8 3.1 CCCn1c(=O)c2[nH]c(-c3cnn(CC#Cc4cccc(OC(F)(F)F)c4)c3)nc2n(CC)c1=O 10.1016/j.ejmech.2017.04.014
155552077 175428 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 496 6 1 9 2.6 Cc1csc2c1c(=O)n(CCc1ccccc1)c(=O)n2Cc1nc2cc(S(N)(=O)=O)ccc2o1 10.1016/j.ejmech.2018.11.045
CHEMBL4576194 175428 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 496 6 1 9 2.6 Cc1csc2c1c(=O)n(CCc1ccccc1)c(=O)n2Cc1nc2cc(S(N)(=O)=O)ccc2o1 10.1016/j.ejmech.2018.11.045
155542641 173154 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 424 8 0 8 2.7 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(Cn3ccnc3)sc21 10.1016/j.ejmech.2018.11.045
CHEMBL4521489 173154 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 424 8 0 8 2.7 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(Cn3ccnc3)sc21 10.1016/j.ejmech.2018.11.045
10237847 77459 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 411 4 2 7 1.4 Cn1c(=O)c2[nH]c(-c3ccc(S(=O)(=O)Nc4ccccn4)cc3)cc2n(C)c1=O 10.1016/j.bmcl.2006.04.074
CHEMBL208705 77459 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 411 4 2 7 1.4 Cn1c(=O)c2[nH]c(-c3ccc(S(=O)(=O)Nc4ccccn4)cc3)cc2n(C)c1=O 10.1016/j.bmcl.2006.04.074
10196517 78323 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 553 8 2 7 3.3 CCn1c(=O)c2[nH]c(-c3ccc(S(=O)(=O)NC4CCN(Cc5ccc(F)cc5)CC4)cc3)cc2n(CC)c1=O 10.1016/j.bmcl.2006.04.074
CHEMBL210969 78323 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 553 8 2 7 3.3 CCn1c(=O)c2[nH]c(-c3ccc(S(=O)(=O)NC4CCN(Cc5ccc(F)cc5)CC4)cc3)cc2n(CC)c1=O 10.1016/j.bmcl.2006.04.074
155568402 176011 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 468 8 1 9 2.4 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(C(C)(O)c3cncn3C)sc21 10.1016/j.ejmech.2018.11.045
CHEMBL4589654 176011 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 468 8 1 9 2.4 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(C(C)(O)c3cncn3C)sc21 10.1016/j.ejmech.2018.11.045
2690 903 None 66 Human Binding pIC50 = 5.9 5.9 -30 9
Inhibition of 50 uM 5`-(N-ethylcarboxamido)adenosine induced cAMP production in CHO cell line expressing human Adenosine A2B receptorInhibition of 50 uM 5`-(N-ethylcarboxamido)adenosine induced cAMP production in CHO cell line expressing human Adenosine A2B receptor
ChEMBL 285 1 1 6 2.8 Clc1ccc2c(c1)c1nc(nn1c(n2)N)c1ccco1 10.1021/jm980094b
384 903 None 66 Human Binding pIC50 = 5.9 5.9 -30 9
Inhibition of 50 uM 5`-(N-ethylcarboxamido)adenosine induced cAMP production in CHO cell line expressing human Adenosine A2B receptorInhibition of 50 uM 5`-(N-ethylcarboxamido)adenosine induced cAMP production in CHO cell line expressing human Adenosine A2B receptor
ChEMBL 285 1 1 6 2.8 Clc1ccc2c(c1)c1nc(nn1c(n2)N)c1ccco1 10.1021/jm980094b
CHEMBL16687 903 None 66 Human Binding pIC50 = 5.9 5.9 -30 9
Inhibition of 50 uM 5`-(N-ethylcarboxamido)adenosine induced cAMP production in CHO cell line expressing human Adenosine A2B receptorInhibition of 50 uM 5`-(N-ethylcarboxamido)adenosine induced cAMP production in CHO cell line expressing human Adenosine A2B receptor
ChEMBL 285 1 1 6 2.8 Clc1ccc2c(c1)c1nc(nn1c(n2)N)c1ccco1 10.1021/jm980094b
10812045 15521 None 0 Human Binding pIC50 = 6.9 6.9 - 1
Antagonist activity at adenosine A2B receptor (unknown origin)Antagonist activity at adenosine A2B receptor (unknown origin)
ChEMBL 419 7 1 7 2.9 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(c2ccccc2OC)CC1 10.1039/C1MD00213A
CHEMBL121766 15521 None 0 Human Binding pIC50 = 6.9 6.9 - 1
Antagonist activity at adenosine A2B receptor (unknown origin)Antagonist activity at adenosine A2B receptor (unknown origin)
ChEMBL 419 7 1 7 2.9 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(c2ccccc2OC)CC1 10.1039/C1MD00213A
44413202 78393 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 565 7 1 9 2.3 CCCn1c(=O)n(C)c(=O)c2[nH]c(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc6c(c5)OCO6)CC4)cc3)cc21 10.1016/j.bmcl.2006.04.074
CHEMBL211071 78393 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 565 7 1 9 2.3 CCCn1c(=O)n(C)c(=O)c2[nH]c(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc6c(c5)OCO6)CC4)cc3)cc21 10.1016/j.bmcl.2006.04.074
155527056 171141 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 366 5 1 6 2.5 Cc1csc2c1c(=O)n(CCc1ccccc1)c(=O)n2Cc1ncc[nH]1 10.1016/j.ejmech.2018.11.045
CHEMBL4458469 171141 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 366 5 1 6 2.5 Cc1csc2c1c(=O)n(CCc1ccccc1)c(=O)n2Cc1ncc[nH]1 10.1016/j.ejmech.2018.11.045
155550407 173931 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 325 4 0 6 2.3 Cc1csc2c1c(=O)n(CCc1ccccc1)c(=O)n2CC#N 10.1016/j.ejmech.2018.11.045
CHEMBL4540909 173931 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 325 4 0 6 2.3 Cc1csc2c1c(=O)n(CCc1ccccc1)c(=O)n2CC#N 10.1016/j.ejmech.2018.11.045
155525648 171093 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 366 5 1 6 2.5 Cc1csc2c1c(=O)n(CCc1ccccc1)c(=O)n2Cc1cnc[nH]1 10.1016/j.ejmech.2018.11.045
CHEMBL4457584 171093 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 366 5 1 6 2.5 Cc1csc2c1c(=O)n(CCc1ccccc1)c(=O)n2Cc1cnc[nH]1 10.1016/j.ejmech.2018.11.045
10766773 208119 None 0 Human Binding pIC50 = 4.9 4.9 - 3
Inhibition of 50 uM 5`-(N-ethylcarboxamido)adenosine induced cAMP production in CHO cell line expressing human Adenosine A2B receptorInhibition of 50 uM 5`-(N-ethylcarboxamido)adenosine induced cAMP production in CHO cell line expressing human Adenosine A2B receptor
ChEMBL 356 4 2 7 2.5 NCCC(=O)Nc1nc2ccc(Cl)cc2c2nc(-c3ccco3)nn12 10.1021/jm980094b
CHEMBL97961 208119 None 0 Human Binding pIC50 = 4.9 4.9 - 3
Inhibition of 50 uM 5`-(N-ethylcarboxamido)adenosine induced cAMP production in CHO cell line expressing human Adenosine A2B receptorInhibition of 50 uM 5`-(N-ethylcarboxamido)adenosine induced cAMP production in CHO cell line expressing human Adenosine A2B receptor
ChEMBL 356 4 2 7 2.5 NCCC(=O)Nc1nc2ccc(Cl)cc2c2nc(-c3ccco3)nn12 10.1021/jm980094b
155515805 170007 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 332 5 0 5 2.7 Cc1csc2c1c(=O)n(CCc1ccccc1)c(=O)n2CCF 10.1016/j.ejmech.2018.11.045
CHEMBL4442438 170007 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 332 5 0 5 2.7 Cc1csc2c1c(=O)n(CCc1ccccc1)c(=O)n2CCF 10.1016/j.ejmech.2018.11.045
155526484 171126 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 414 8 1 7 2.9 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(C(O)C3CC3)sc21 10.1016/j.ejmech.2018.11.045
CHEMBL4458223 171126 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 414 8 1 7 2.9 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(C(O)C3CC3)sc21 10.1016/j.ejmech.2018.11.045
10288169 79759 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 439 6 2 7 1.1 Cn1c(=O)c2[nH]c(-c3ccc(S(=O)(=O)NCCc4ccccn4)cc3)cc2n(C)c1=O 10.1016/j.bmcl.2006.04.074
CHEMBL211762 79759 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 439 6 2 7 1.1 Cn1c(=O)c2[nH]c(-c3ccc(S(=O)(=O)NCCc4ccccn4)cc3)cc2n(C)c1=O 10.1016/j.bmcl.2006.04.074
155515166 169931 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 380 5 0 7 2.6 Cc1csc2c1c(=O)n(CCc1ccccc1)c(=O)n2Cc1nccn1C 10.1016/j.ejmech.2018.11.045
CHEMBL4441343 169931 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 380 5 0 7 2.6 Cc1csc2c1c(=O)n(CCc1ccccc1)c(=O)n2Cc1nccn1C 10.1016/j.ejmech.2018.11.045
44413113 78318 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 539 7 1 7 2.8 CCn1c(=O)c2[nH]c(-c3ccc(S(=O)(=O)N4CCN(Cc5cccc(F)c5)CC4)cc3)cc2n(CC)c1=O 10.1016/j.bmcl.2006.04.074
CHEMBL210931 78318 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 539 7 1 7 2.8 CCn1c(=O)c2[nH]c(-c3ccc(S(=O)(=O)N4CCN(Cc5cccc(F)c5)CC4)cc3)cc2n(CC)c1=O 10.1016/j.bmcl.2006.04.074
44413192 79933 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 483 8 2 8 2.0 CCCn1c(=O)c2[nH]c(-c3ccc(S(=O)(=O)NCc4ccc(OC)cn4)cc3)cc2n(C)c1=O 10.1016/j.bmcl.2006.04.074
CHEMBL212528 79933 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 483 8 2 8 2.0 CCCn1c(=O)c2[nH]c(-c3ccc(S(=O)(=O)NCc4ccc(OC)cn4)cc3)cc2n(C)c1=O 10.1016/j.bmcl.2006.04.074
122574772 171087 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 374 7 1 7 1.9 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(CO)sc21 10.1016/j.ejmech.2018.11.045
CHEMBL4457476 171087 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 374 7 1 7 1.9 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(CO)sc21 10.1016/j.ejmech.2018.11.045
155548802 173808 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 428 8 1 7 3.0 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(C(C)(O)C3CC3)sc21 10.1016/j.ejmech.2018.11.045
CHEMBL4538262 173808 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 428 8 1 7 3.0 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(C(C)(O)C3CC3)sc21 10.1016/j.ejmech.2018.11.045
155562247 175723 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 370 6 0 6 2.9 COCCn1c(=O)n(CC2(c3ccccc3)CC2)c(=O)c2c(C)csc21 10.1016/j.ejmech.2018.11.045
CHEMBL4582620 175723 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 370 6 0 6 2.9 COCCn1c(=O)n(CC2(c3ccccc3)CC2)c(=O)c2c(C)csc21 10.1016/j.ejmech.2018.11.045
10311222 77743 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 493 5 1 7 1.7 Cn1c(=O)c2[nH]c(-c3ccc(S(=O)(=O)N4CCN(Cc5ccccc5)CC4)cc3)cc2n(C)c1=O 10.1016/j.bmcl.2006.04.074
CHEMBL209019 77743 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 493 5 1 7 1.7 Cn1c(=O)c2[nH]c(-c3ccc(S(=O)(=O)N4CCN(Cc5ccccc5)CC4)cc3)cc2n(C)c1=O 10.1016/j.bmcl.2006.04.074
155521875 170608 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 310 4 0 6 2.2 COCCn1c(=O)n(CC(C)(C)C)c(=O)c2c(C)csc21 10.1016/j.ejmech.2018.11.045
CHEMBL4450782 170608 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 310 4 0 6 2.2 COCCn1c(=O)n(CC(C)(C)C)c(=O)c2c(C)csc21 10.1016/j.ejmech.2018.11.045
10310578 77789 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 455 7 2 8 1.0 Cn1c(=O)c2[nH]c(-c3ccc(S(=O)(=O)NCCOc4ccccn4)cc3)cc2n(C)c1=O 10.1016/j.bmcl.2006.04.074
CHEMBL209208 77789 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 455 7 2 8 1.0 Cn1c(=O)c2[nH]c(-c3ccc(S(=O)(=O)NCCOc4ccccn4)cc3)cc2n(C)c1=O 10.1016/j.bmcl.2006.04.074
10238677 79915 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 467 8 2 7 2.0 CCCn1c(=O)c2[nH]c(-c3ccc(S(=O)(=O)NCCc4ccccn4)cc3)cc2n(C)c1=O 10.1016/j.bmcl.2006.04.074
CHEMBL212464 79915 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 467 8 2 7 2.0 CCCn1c(=O)c2[nH]c(-c3ccc(S(=O)(=O)NCCc4ccccn4)cc3)cc2n(C)c1=O 10.1016/j.bmcl.2006.04.074
44413193 140132 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 539 7 1 7 2.8 CCCn1c(=O)n(C)c(=O)c2[nH]c(-c3ccc(S(=O)(=O)N4CCN(Cc5cccc(F)c5)CC4)cc3)cc21 10.1016/j.bmcl.2006.04.074
CHEMBL380177 140132 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 539 7 1 7 2.8 CCCn1c(=O)n(C)c(=O)c2[nH]c(-c3ccc(S(=O)(=O)N4CCN(Cc5cccc(F)c5)CC4)cc3)cc21 10.1016/j.bmcl.2006.04.074
155523243 170834 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 469 7 1 7 2.7 Cc1csc2c1c(=O)n(CCc1ccccc1)c(=O)n2CCc1ccc(S(N)(=O)=O)cc1 10.1016/j.ejmech.2018.11.045
CHEMBL4453664 170834 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 469 7 1 7 2.7 Cc1csc2c1c(=O)n(CCc1ccccc1)c(=O)n2CCc1ccc(S(N)(=O)=O)cc1 10.1016/j.ejmech.2018.11.045
155533818 171896 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 416 8 0 8 2.6 CCOC(=O)c1sc2c(c1C)c(=O)n(CCc1ccccc1)c(=O)n2CCOC 10.1016/j.ejmech.2018.11.045
CHEMBL4469697 171896 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 416 8 0 8 2.6 CCOC(=O)c1sc2c(c1C)c(=O)n(CCc1ccccc1)c(=O)n2CCOC 10.1016/j.ejmech.2018.11.045
10577289 208073 None 0 Human Binding pIC50 = 5.8 5.8 - 3
Inhibition of 50 uM 5`-(N-ethylcarboxamido)adenosine induced cAMP production in CHO cell line expressing human Adenosine A2B receptorInhibition of 50 uM 5`-(N-ethylcarboxamido)adenosine induced cAMP production in CHO cell line expressing human Adenosine A2B receptor
ChEMBL 384 6 2 7 3.3 NCCCCC(=O)Nc1nc2ccc(Cl)cc2c2nc(-c3ccco3)nn12 10.1021/jm980094b
CHEMBL97700 208073 None 0 Human Binding pIC50 = 5.8 5.8 - 3
Inhibition of 50 uM 5`-(N-ethylcarboxamido)adenosine induced cAMP production in CHO cell line expressing human Adenosine A2B receptorInhibition of 50 uM 5`-(N-ethylcarboxamido)adenosine induced cAMP production in CHO cell line expressing human Adenosine A2B receptor
ChEMBL 384 6 2 7 3.3 NCCCCC(=O)Nc1nc2ccc(Cl)cc2c2nc(-c3ccco3)nn12 10.1021/jm980094b
10153029 78048 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 563 10 2 7 3.9 CCCn1c(=O)c2[nH]c(-c3ccc(S(=O)(=O)NC4CCN(Cc5ccccc5)CC4)cc3)cc2n(CCC)c1=O 10.1016/j.bmcl.2006.04.074
CHEMBL209944 78048 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 563 10 2 7 3.9 CCCn1c(=O)c2[nH]c(-c3ccc(S(=O)(=O)NC4CCN(Cc5ccccc5)CC4)cc3)cc2n(CCC)c1=O 10.1016/j.bmcl.2006.04.074
10288197 78174 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 441 5 2 8 1.4 COc1ccc(NS(=O)(=O)c2ccc(-c3cc4c([nH]3)c(=O)n(C)c(=O)n4C)cc2)cn1 10.1016/j.bmcl.2006.04.074
CHEMBL210456 78174 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 441 5 2 8 1.4 COc1ccc(NS(=O)(=O)c2ccc(-c3cc4c([nH]3)c(=O)n(C)c(=O)n4C)cc2)cn1 10.1016/j.bmcl.2006.04.074
155521508 170704 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 370 5 0 6 3.0 Cc1csc2c1c(=O)n(CCc1ccccc1)c(=O)n2CC1CCCO1 10.1016/j.ejmech.2018.11.045
CHEMBL4451942 170704 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 370 5 0 6 3.0 Cc1csc2c1c(=O)n(CCc1ccccc1)c(=O)n2CC1CCCO1 10.1016/j.ejmech.2018.11.045
155555355 174442 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 452 8 0 9 2.4 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(C(=O)c3cn(C)cn3)sc21 10.1016/j.ejmech.2018.11.045
CHEMBL4553423 174442 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 452 8 0 9 2.4 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(C(=O)c3cn(C)cn3)sc21 10.1016/j.ejmech.2018.11.045
155551709 175143 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 438 8 1 7 3.0 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(Cc3nc[nH]c3C)sc21 10.1016/j.ejmech.2018.11.045
CHEMBL4569909 175143 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 438 8 1 7 3.0 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(Cc3nc[nH]c3C)sc21 10.1016/j.ejmech.2018.11.045
44413182 78175 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 455 6 2 8 1.1 COc1ccc(CNS(=O)(=O)c2ccc(-c3cc4c([nH]3)c(=O)n(C)c(=O)n4C)cc2)nc1 10.1016/j.bmcl.2006.04.074
CHEMBL210457 78175 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 455 6 2 8 1.1 COc1ccc(CNS(=O)(=O)c2ccc(-c3cc4c([nH]3)c(=O)n(C)c(=O)n4C)cc2)nc1 10.1016/j.bmcl.2006.04.074
155521394 170590 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 443 7 1 8 1.2 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(C(=O)N3CC(O)C3)sc21 10.1016/j.ejmech.2018.11.045
CHEMBL4450633 170590 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 443 7 1 8 1.2 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(C(=O)N3CC(O)C3)sc21 10.1016/j.ejmech.2018.11.045
155523200 170755 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 427 8 0 7 3.0 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(CN3CCCC3)sc21 10.1016/j.ejmech.2018.11.045
CHEMBL4452532 170755 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 427 8 0 7 3.0 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(CN3CCCC3)sc21 10.1016/j.ejmech.2018.11.045
155526352 171213 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 358 6 0 6 2.7 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(C)sc21 10.1016/j.ejmech.2018.11.045
CHEMBL4459477 171213 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 358 6 0 6 2.7 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(C)sc21 10.1016/j.ejmech.2018.11.045
155543633 173202 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 405 4 1 7 1.3 CCn1c(=O)c2c(C)c(C(=O)N3CC(O)C3)sc2n(CCC(F)(F)F)c1=O 10.1016/j.ejmech.2018.11.045
CHEMBL4522738 173202 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 405 4 1 7 1.3 CCn1c(=O)c2c(C)c(C(=O)N3CC(O)C3)sc2n(CCC(F)(F)F)c1=O 10.1016/j.ejmech.2018.11.045
44236539 156792 None 0 Human Binding pIC50 = 5.7 5.7 - 1
Antagonist activity at human adenosine A2B receptor expressed in mouse NIH/3T3 cells assessed as inhibition of NECA-induced IL-6 release incubated for 15 mins followed by agonist treatment for 15 mins by HTRF assayAntagonist activity at human adenosine A2B receptor expressed in mouse NIH/3T3 cells assessed as inhibition of NECA-induced IL-6 release incubated for 15 mins followed by agonist treatment for 15 mins by HTRF assay
ChEMBL 460 7 2 8 2.3 CCCn1c(=O)c2[nH]c(-c3cnn(CC#Cc4cccc(C(=O)O)c4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2017.04.014
CHEMBL4070936 156792 None 0 Human Binding pIC50 = 5.7 5.7 - 1
Antagonist activity at human adenosine A2B receptor expressed in mouse NIH/3T3 cells assessed as inhibition of NECA-induced IL-6 release incubated for 15 mins followed by agonist treatment for 15 mins by HTRF assayAntagonist activity at human adenosine A2B receptor expressed in mouse NIH/3T3 cells assessed as inhibition of NECA-induced IL-6 release incubated for 15 mins followed by agonist treatment for 15 mins by HTRF assay
ChEMBL 460 7 2 8 2.3 CCCn1c(=O)c2[nH]c(-c3cnn(CC#Cc4cccc(C(=O)O)c4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2017.04.014
10645984 18817 None 0 Human Binding pIC50 = 5.7 5.7 - 1
Antagonist activity at adenosine A2B receptor (unknown origin)Antagonist activity at adenosine A2B receptor (unknown origin)
ChEMBL 423 6 1 6 3.6 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(c2cccc(Cl)c2)CC1 10.1039/C1MD00213A
CHEMBL127876 18817 None 0 Human Binding pIC50 = 5.7 5.7 - 1
Antagonist activity at adenosine A2B receptor (unknown origin)Antagonist activity at adenosine A2B receptor (unknown origin)
ChEMBL 423 6 1 6 3.6 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(c2cccc(Cl)c2)CC1 10.1039/C1MD00213A
155549589 173917 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 362 6 0 6 2.6 COCCn1c(=O)n(CCc2ccccc2F)c(=O)c2c(C)csc21 10.1016/j.ejmech.2018.11.045
CHEMBL4540558 173917 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 362 6 0 6 2.6 COCCn1c(=O)n(CCc2ccccc2F)c(=O)c2c(C)csc21 10.1016/j.ejmech.2018.11.045
118016325 170073 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 388 7 1 7 2.1 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(C(=O)O)sc21 10.1016/j.ejmech.2018.11.045
CHEMBL4443243 170073 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 388 7 1 7 2.1 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(C(=O)O)sc21 10.1016/j.ejmech.2018.11.045
155514761 169891 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 294 4 0 6 1.4 CCn1c(=O)c2c3c(sc2n(CCOC)c1=O)CCC3 10.1016/j.ejmech.2018.11.045
CHEMBL4440686 169891 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 294 4 0 6 1.4 CCn1c(=O)c2c3c(sc2n(CCOC)c1=O)CCC3 10.1016/j.ejmech.2018.11.045
45073485 163617 None 7 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes preincubated for 30 mins followed by PSB-12105 addition measured after 20 mins by flow cytometric methodDisplacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes preincubated for 30 mins followed by PSB-12105 addition measured after 20 mins by flow cytometric method
ChEMBL 506 7 0 7 2.2 CCCN1C(=O)N=C2N=C(c3ccc(S(=O)(=O)N4CCN(Cc5ccccc5)CC4)cc3)N=C2C1=O 10.1021/acs.jmedchem.7b01627
CHEMBL4203745 163617 None 7 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes preincubated for 30 mins followed by PSB-12105 addition measured after 20 mins by flow cytometric methodDisplacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes preincubated for 30 mins followed by PSB-12105 addition measured after 20 mins by flow cytometric method
ChEMBL 506 7 0 7 2.2 CCCN1C(=O)N=C2N=C(c3ccc(S(=O)(=O)N4CCN(Cc5ccccc5)CC4)cc3)N=C2C1=O 10.1021/acs.jmedchem.7b01627
155562338 175847 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 448 8 0 7 3.7 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(C(=O)c3ccccc3)sc21 10.1016/j.ejmech.2018.11.045
CHEMBL4585480 175847 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 448 8 0 7 3.7 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(C(=O)c3ccccc3)sc21 10.1016/j.ejmech.2018.11.045
10474279 107310 None 0 Human Binding pIC50 = 5.6 5.6 - 3
Inhibition of 50 uM 5`-(N-ethylcarboxamido)adenosine induced cAMP production in CHO cell line expressing human Adenosine A2B receptorInhibition of 50 uM 5`-(N-ethylcarboxamido)adenosine induced cAMP production in CHO cell line expressing human Adenosine A2B receptor
ChEMBL 369 2 1 6 4.2 CC(C)(C)C(=O)Nc1nc2ccc(Cl)cc2c2nc(-c3ccco3)nn12 10.1021/jm980094b
CHEMBL317310 107310 None 0 Human Binding pIC50 = 5.6 5.6 - 3
Inhibition of 50 uM 5`-(N-ethylcarboxamido)adenosine induced cAMP production in CHO cell line expressing human Adenosine A2B receptorInhibition of 50 uM 5`-(N-ethylcarboxamido)adenosine induced cAMP production in CHO cell line expressing human Adenosine A2B receptor
ChEMBL 369 2 1 6 4.2 CC(C)(C)C(=O)Nc1nc2ccc(Cl)cc2c2nc(-c3ccco3)nn12 10.1021/jm980094b
10691504 207781 None 0 Human Binding pIC50 = 5.6 5.6 - 3
Inhibition of 50 uM 5`-(N-ethylcarboxamido)adenosine induced cAMP production in CHO cell line expressing human Adenosine A2B receptorInhibition of 50 uM 5`-(N-ethylcarboxamido)adenosine induced cAMP production in CHO cell line expressing human Adenosine A2B receptor
ChEMBL 385 2 1 7 4.5 CC(C)(C)OC(=O)Nc1nc2ccc(Cl)cc2c2nc(-c3ccco3)nn12 10.1021/jm980094b
CHEMBL96041 207781 None 0 Human Binding pIC50 = 5.6 5.6 - 3
Inhibition of 50 uM 5`-(N-ethylcarboxamido)adenosine induced cAMP production in CHO cell line expressing human Adenosine A2B receptorInhibition of 50 uM 5`-(N-ethylcarboxamido)adenosine induced cAMP production in CHO cell line expressing human Adenosine A2B receptor
ChEMBL 385 2 1 7 4.5 CC(C)(C)OC(=O)Nc1nc2ccc(Cl)cc2c2nc(-c3ccco3)nn12 10.1021/jm980094b
10669778 117475 None 0 Human Binding pIC50 = 6.6 6.6 - 1
Antagonist activity at adenosine A2B receptor (unknown origin)Antagonist activity at adenosine A2B receptor (unknown origin)
ChEMBL 419 7 1 7 2.9 COc1ccc(N2CCN(CCOC(=O)c3cc(Cl)c(N)cc3OC)CC2)cc1 10.1039/C1MD00213A
CHEMBL339936 117475 None 0 Human Binding pIC50 = 6.6 6.6 - 1
Antagonist activity at adenosine A2B receptor (unknown origin)Antagonist activity at adenosine A2B receptor (unknown origin)
ChEMBL 419 7 1 7 2.9 COc1ccc(N2CCN(CCOC(=O)c3cc(Cl)c(N)cc3OC)CC2)cc1 10.1039/C1MD00213A
155522968 170769 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 442 9 0 7 3.9 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(COC3CCCC3)sc21 10.1016/j.ejmech.2018.11.045
CHEMBL4452799 170769 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 442 9 0 7 3.9 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(COC3CCCC3)sc21 10.1016/j.ejmech.2018.11.045
155558166 174754 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 441 7 0 7 2.7 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(C(=O)N3CCCC3)sc21 10.1016/j.ejmech.2018.11.045
CHEMBL4560841 174754 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 441 7 0 7 2.7 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(C(=O)N3CCCC3)sc21 10.1016/j.ejmech.2018.11.045
71600087 154357 None 54 Human Binding pIC50 = 5.6 5.6 - 0
Antagonist activity at adenosine A2B receptor (unknown origin)Antagonist activity at adenosine A2B receptor (unknown origin)
ChEMBL 459 6 2 5 4.4 CCS(=O)(=O)Nc1ccc(Oc2ccc(F)cc2F)c(-c2cn(C)c(=O)c3[nH]ccc23)c1 10.1021/acs.jmedchem.7b00746
CHEMBL3987016 154357 None 54 Human Binding pIC50 = 5.6 5.6 - 0
Antagonist activity at adenosine A2B receptor (unknown origin)Antagonist activity at adenosine A2B receptor (unknown origin)
ChEMBL 459 6 2 5 4.4 CCS(=O)(=O)Nc1ccc(Oc2ccc(F)cc2F)c(-c2cn(C)c(=O)c3[nH]ccc23)c1 10.1021/acs.jmedchem.7b00746
10616222 107446 None 0 Human Binding pIC50 = 5.6 5.6 - 3
Inhibition of 50 uM 5`-(N-ethylcarboxamido)adenosine induced cAMP production in CHO cell line expressing human Adenosine A2B receptorInhibition of 50 uM 5`-(N-ethylcarboxamido)adenosine induced cAMP production in CHO cell line expressing human Adenosine A2B receptor
ChEMBL 327 2 1 6 3.1 CC(=O)Nc1nc2ccc(Cl)cc2c2nc(-c3ccco3)nn12 10.1021/jm980094b
CHEMBL318251 107446 None 0 Human Binding pIC50 = 5.6 5.6 - 3
Inhibition of 50 uM 5`-(N-ethylcarboxamido)adenosine induced cAMP production in CHO cell line expressing human Adenosine A2B receptorInhibition of 50 uM 5`-(N-ethylcarboxamido)adenosine induced cAMP production in CHO cell line expressing human Adenosine A2B receptor
ChEMBL 327 2 1 6 3.1 CC(=O)Nc1nc2ccc(Cl)cc2c2nc(-c3ccco3)nn12 10.1021/jm980094b
44413130 79958 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 494 5 1 8 1.1 Cn1c(=O)c2[nH]c(-c3ccc(S(=O)(=O)N4CCN(Cc5ccncc5)CC4)cc3)cc2n(C)c1=O 10.1016/j.bmcl.2006.04.074
CHEMBL212642 79958 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 494 5 1 8 1.1 Cn1c(=O)c2[nH]c(-c3ccc(S(=O)(=O)N4CCN(Cc5ccncc5)CC4)cc3)cc2n(C)c1=O 10.1016/j.bmcl.2006.04.074
10339165 207744 None 0 Human Binding pIC50 = 6.6 6.6 -2 4
Inhibition of 50 uM 5`-(N-ethylcarboxamido)adenosine induced cAMP production in CHO cell line expressing human Adenosine A2B receptorInhibition of 50 uM 5`-(N-ethylcarboxamido)adenosine induced cAMP production in CHO cell line expressing human Adenosine A2B receptor
ChEMBL 370 5 2 7 2.9 NCCCC(=O)Nc1nc2ccc(Cl)cc2c2nc(-c3ccco3)nn12 10.1021/jm980094b
CHEMBL95811 207744 None 0 Human Binding pIC50 = 6.6 6.6 -2 4
Inhibition of 50 uM 5`-(N-ethylcarboxamido)adenosine induced cAMP production in CHO cell line expressing human Adenosine A2B receptorInhibition of 50 uM 5`-(N-ethylcarboxamido)adenosine induced cAMP production in CHO cell line expressing human Adenosine A2B receptor
ChEMBL 370 5 2 7 2.9 NCCCC(=O)Nc1nc2ccc(Cl)cc2c2nc(-c3ccco3)nn12 10.1021/jm980094b
135418256 15569 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Displacement of specific [3H]DPCPX binding at human adenosine A2B receptor expressed in HEK293 cells.Displacement of specific [3H]DPCPX binding at human adenosine A2B receptor expressed in HEK293 cells.
ChEMBL 326 4 1 5 3.7 CCCCc1nc2[nH]ncc2c2nc(-c3ccc(Cl)cc3)nn12 10.1016/j.bmcl.2004.04.099
CHEMBL122037 15569 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Displacement of specific [3H]DPCPX binding at human adenosine A2B receptor expressed in HEK293 cells.Displacement of specific [3H]DPCPX binding at human adenosine A2B receptor expressed in HEK293 cells.
ChEMBL 326 4 1 5 3.7 CCCCc1nc2[nH]ncc2c2nc(-c3ccc(Cl)cc3)nn12 10.1016/j.bmcl.2004.04.099
11224 582 None 35 Rat Binding pIC50 = 6.6 6.6 - 1
Antagonist activity at recombinant rat A2B adenosine receptor expressed in CHO cells after 3 to 4 hrs by luciferase reporter gene assayAntagonist activity at recombinant rat A2B adenosine receptor expressed in CHO cells after 3 to 4 hrs by luciferase reporter gene assay
ChEMBL 433 4 1 7 2.1 CCn1c(=O)c2c(C)c(sc2n(c1=O)CCC(F)(F)F)C(=O)N1CCC(CC1)O 10.1016/j.ejmech.2018.11.045
118016229 582 None 35 Rat Binding pIC50 = 6.6 6.6 - 1
Antagonist activity at recombinant rat A2B adenosine receptor expressed in CHO cells after 3 to 4 hrs by luciferase reporter gene assayAntagonist activity at recombinant rat A2B adenosine receptor expressed in CHO cells after 3 to 4 hrs by luciferase reporter gene assay
ChEMBL 433 4 1 7 2.1 CCn1c(=O)c2c(C)c(sc2n(c1=O)CCC(F)(F)F)C(=O)N1CCC(CC1)O 10.1016/j.ejmech.2018.11.045
CHEMBL4522981 582 None 35 Rat Binding pIC50 = 6.6 6.6 - 1
Antagonist activity at recombinant rat A2B adenosine receptor expressed in CHO cells after 3 to 4 hrs by luciferase reporter gene assayAntagonist activity at recombinant rat A2B adenosine receptor expressed in CHO cells after 3 to 4 hrs by luciferase reporter gene assay
ChEMBL 433 4 1 7 2.1 CCn1c(=O)c2c(C)c(sc2n(c1=O)CCC(F)(F)F)C(=O)N1CCC(CC1)O 10.1016/j.ejmech.2018.11.045
155548182 173788 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 345 6 0 7 1.8 COCCn1c(=O)n(CCc2cccnc2)c(=O)c2c(C)csc21 10.1016/j.ejmech.2018.11.045
CHEMBL4537687 173788 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 345 6 0 7 1.8 COCCn1c(=O)n(CCc2cccnc2)c(=O)c2c(C)csc21 10.1016/j.ejmech.2018.11.045
155536243 172180 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 470 8 0 6 4.6 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(C(F)(F)c3ccccc3)sc21 10.1016/j.ejmech.2018.11.045
CHEMBL4473551 172180 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 470 8 0 6 4.6 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(C(F)(F)c3ccccc3)sc21 10.1016/j.ejmech.2018.11.045
1329 1472 None 86 Human Binding pIC50 = 8.4 8.4 -1288 14
Displacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes preincubated for 30 mins followed by PSB-12105 addition measured after 20 mins by flow cytometric methodDisplacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes preincubated for 30 mins followed by PSB-12105 addition measured after 20 mins by flow cytometric method
ChEMBL 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 10.1021/acs.jmedchem.7b01627
386 1472 None 86 Human Binding pIC50 = 8.4 8.4 -1288 14
Displacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes preincubated for 30 mins followed by PSB-12105 addition measured after 20 mins by flow cytometric methodDisplacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes preincubated for 30 mins followed by PSB-12105 addition measured after 20 mins by flow cytometric method
ChEMBL 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 10.1021/acs.jmedchem.7b01627
CHEMBL183 1472 None 86 Human Binding pIC50 = 8.4 8.4 -1288 14
Displacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes preincubated for 30 mins followed by PSB-12105 addition measured after 20 mins by flow cytometric methodDisplacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes preincubated for 30 mins followed by PSB-12105 addition measured after 20 mins by flow cytometric method
ChEMBL 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 10.1021/acs.jmedchem.7b01627
DB12946 1472 None 86 Human Binding pIC50 = 8.4 8.4 -1288 14
Displacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes preincubated for 30 mins followed by PSB-12105 addition measured after 20 mins by flow cytometric methodDisplacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes preincubated for 30 mins followed by PSB-12105 addition measured after 20 mins by flow cytometric method
ChEMBL 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 10.1021/acs.jmedchem.7b01627
155519860 170415 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 450 8 1 7 3.5 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(C(O)c3ccccc3)sc21 10.1016/j.ejmech.2018.11.045
CHEMBL4448231 170415 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 450 8 1 7 3.5 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(C(O)c3ccccc3)sc21 10.1016/j.ejmech.2018.11.045
155544551 173394 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 344 6 0 6 2.4 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)csc21 10.1016/j.ejmech.2018.11.045
CHEMBL4528081 173394 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 344 6 0 6 2.4 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)csc21 10.1016/j.ejmech.2018.11.045
449 2643 None 52 Human Binding pIC50 = 7.5 7.5 -1 9
Inhibition of A2bR (unknown origin) expressed in HEK293 cells incubated overnight by dual luciferase reporter assayInhibition of A2bR (unknown origin) expressed in HEK293 cells incubated overnight by dual luciferase reporter assay
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N nan
453 2643 None 52 Human Binding pIC50 = 7.5 7.5 -1 9
Inhibition of A2bR (unknown origin) expressed in HEK293 cells incubated overnight by dual luciferase reporter assayInhibition of A2bR (unknown origin) expressed in HEK293 cells incubated overnight by dual luciferase reporter assay
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N nan
6603931 2643 None 52 Human Binding pIC50 = 7.5 7.5 -1 9
Inhibition of A2bR (unknown origin) expressed in HEK293 cells incubated overnight by dual luciferase reporter assayInhibition of A2bR (unknown origin) expressed in HEK293 cells incubated overnight by dual luciferase reporter assay
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N nan
CHEMBL273807 2643 None 52 Human Binding pIC50 = 7.5 7.5 -1 9
Inhibition of A2bR (unknown origin) expressed in HEK293 cells incubated overnight by dual luciferase reporter assayInhibition of A2bR (unknown origin) expressed in HEK293 cells incubated overnight by dual luciferase reporter assay
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N nan
71601630 86922 None 0 Human Binding pIC50 = 6.5 6.5 - 2
Inhibition of human A2B adenosine receptor transfected in CHO cells assessed as inhibition of NECA-induced cyclic AMP production after 10 mins by competitive protein binding assayInhibition of human A2B adenosine receptor transfected in CHO cells assessed as inhibition of NECA-induced cyclic AMP production after 10 mins by competitive protein binding assay
ChEMBL 225 1 1 5 1.7 Cc1nc(N)c2nn(-c3ccccc3)cc2n1 10.1021/jm400068e
CHEMBL2322916 86922 None 0 Human Binding pIC50 = 6.5 6.5 - 2
Inhibition of human A2B adenosine receptor transfected in CHO cells assessed as inhibition of NECA-induced cyclic AMP production after 10 mins by competitive protein binding assayInhibition of human A2B adenosine receptor transfected in CHO cells assessed as inhibition of NECA-induced cyclic AMP production after 10 mins by competitive protein binding assay
ChEMBL 225 1 1 5 1.7 Cc1nc(N)c2nn(-c3ccccc3)cc2n1 10.1021/jm400068e
155517038 170159 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 378 6 0 6 3.1 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(Cl)sc21 10.1016/j.ejmech.2018.11.045
CHEMBL4444370 170159 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 378 6 0 6 3.1 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(Cl)sc21 10.1016/j.ejmech.2018.11.045
155541364 172990 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 380 5 1 6 2.9 Cc1[nH]cnc1Cn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)csc21 10.1016/j.ejmech.2018.11.045
CHEMBL4517977 172990 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 380 5 1 6 2.9 Cc1[nH]cnc1Cn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)csc21 10.1016/j.ejmech.2018.11.045
10717193 16782 None 0 Human Binding pIC50 = 5.4 5.4 - 1
Antagonist activity at adenosine A2B receptor (unknown origin)Antagonist activity at adenosine A2B receptor (unknown origin)
ChEMBL 423 6 1 6 3.6 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(c2ccc(Cl)cc2)CC1 10.1039/C1MD00213A
CHEMBL124485 16782 None 0 Human Binding pIC50 = 5.4 5.4 - 1
Antagonist activity at adenosine A2B receptor (unknown origin)Antagonist activity at adenosine A2B receptor (unknown origin)
ChEMBL 423 6 1 6 3.6 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(c2ccc(Cl)cc2)CC1 10.1039/C1MD00213A
155526277 171118 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 449 7 1 7 2.7 CCN(CC(C)(C)O)C(=O)c1sc2c(c1C)c(=O)n(CC)c(=O)n2CCC(F)(F)F 10.1016/j.ejmech.2018.11.045
CHEMBL4458042 171118 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 449 7 1 7 2.7 CCN(CC(C)(C)O)C(=O)c1sc2c(c1C)c(=O)n(CC)c(=O)n2CCC(F)(F)F 10.1016/j.ejmech.2018.11.045
155522797 170801 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 308 4 0 6 1.8 CCn1c(=O)c2c3c(sc2n(CCOC)c1=O)CCCC3 10.1016/j.ejmech.2018.11.045
CHEMBL4453228 170801 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 308 4 0 6 1.8 CCn1c(=O)c2c3c(sc2n(CCOC)c1=O)CCCC3 10.1016/j.ejmech.2018.11.045
155548102 173718 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 431 8 0 8 2.1 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(C(=O)N(C)OC)sc21 10.1016/j.ejmech.2018.11.045
CHEMBL4536104 173718 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 431 8 0 8 2.1 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(C(=O)N(C)OC)sc21 10.1016/j.ejmech.2018.11.045
10218183 79766 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 533 5 1 8 2.5 Cn1c(=O)c2[nH]c(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc(Cl)s5)CC4)cc3)cc2n(C)c1=O 10.1016/j.bmcl.2006.04.074
CHEMBL211813 79766 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 533 5 1 8 2.5 Cn1c(=O)c2[nH]c(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc(Cl)s5)CC4)cc3)cc2n(C)c1=O 10.1016/j.bmcl.2006.04.074
11224 582 None 35 Mouse Binding pIC50 = 6.4 6.4 - 1
Antagonist activity at recombinant mouse A2B adenosine receptor expressed in CHO cells after 3 to 4 hrs by luciferase reporter gene assayAntagonist activity at recombinant mouse A2B adenosine receptor expressed in CHO cells after 3 to 4 hrs by luciferase reporter gene assay
ChEMBL 433 4 1 7 2.1 CCn1c(=O)c2c(C)c(sc2n(c1=O)CCC(F)(F)F)C(=O)N1CCC(CC1)O 10.1016/j.ejmech.2018.11.045
118016229 582 None 35 Mouse Binding pIC50 = 6.4 6.4 - 1
Antagonist activity at recombinant mouse A2B adenosine receptor expressed in CHO cells after 3 to 4 hrs by luciferase reporter gene assayAntagonist activity at recombinant mouse A2B adenosine receptor expressed in CHO cells after 3 to 4 hrs by luciferase reporter gene assay
ChEMBL 433 4 1 7 2.1 CCn1c(=O)c2c(C)c(sc2n(c1=O)CCC(F)(F)F)C(=O)N1CCC(CC1)O 10.1016/j.ejmech.2018.11.045
CHEMBL4522981 582 None 35 Mouse Binding pIC50 = 6.4 6.4 - 1
Antagonist activity at recombinant mouse A2B adenosine receptor expressed in CHO cells after 3 to 4 hrs by luciferase reporter gene assayAntagonist activity at recombinant mouse A2B adenosine receptor expressed in CHO cells after 3 to 4 hrs by luciferase reporter gene assay
ChEMBL 433 4 1 7 2.1 CCn1c(=O)c2c(C)c(sc2n(c1=O)CCC(F)(F)F)C(=O)N1CCC(CC1)O 10.1016/j.ejmech.2018.11.045
1922 202818 None 44 Human Binding pIC50 = 6.4 6.4 -26 6
Inhibitory activity against cyclic AMP production in human Adenosine A2B receptor assayInhibitory activity against cyclic AMP production in human Adenosine A2B receptor assay
ChEMBL 256 1 1 5 0.6 Cn1c(=O)c2nc(-c3ccccc3)[nH]c2n(C)c1=O 10.1021/jm990499b
CHEMBL62350 202818 None 44 Human Binding pIC50 = 6.4 6.4 -26 6
Inhibitory activity against cyclic AMP production in human Adenosine A2B receptor assayInhibitory activity against cyclic AMP production in human Adenosine A2B receptor assay
ChEMBL 256 1 1 5 0.6 Cn1c(=O)c2nc(-c3ccccc3)[nH]c2n(C)c1=O 10.1021/jm990499b
155520492 170482 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 443 9 0 7 2.9 CCN(CC)C(=O)c1sc2c(c1C)c(=O)n(CCc1ccccc1)c(=O)n2CCOC 10.1016/j.ejmech.2018.11.045
CHEMBL4449139 170482 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 443 9 0 7 2.9 CCN(CC)C(=O)c1sc2c(c1C)c(=O)n(CCc1ccccc1)c(=O)n2CCOC 10.1016/j.ejmech.2018.11.045
71601632 86924 None 0 Human Binding pIC50 = 6.4 6.4 - 2
Inhibition of human A2B adenosine receptor transfected in CHO cells assessed as inhibition of NECA-induced cyclic AMP production after 10 mins by competitive protein binding assayInhibition of human A2B adenosine receptor transfected in CHO cells assessed as inhibition of NECA-induced cyclic AMP production after 10 mins by competitive protein binding assay
ChEMBL 301 3 1 5 3.0 Nc1nc(Cc2ccccc2)nc2cn(-c3ccccc3)nc12 10.1021/jm400068e
CHEMBL2322918 86924 None 0 Human Binding pIC50 = 6.4 6.4 - 2
Inhibition of human A2B adenosine receptor transfected in CHO cells assessed as inhibition of NECA-induced cyclic AMP production after 10 mins by competitive protein binding assayInhibition of human A2B adenosine receptor transfected in CHO cells assessed as inhibition of NECA-induced cyclic AMP production after 10 mins by competitive protein binding assay
ChEMBL 301 3 1 5 3.0 Nc1nc(Cc2ccccc2)nc2cn(-c3ccccc3)nc12 10.1021/jm400068e
44413136 79267 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 507 6 2 7 2.2 Cn1c(=O)c2[nH]c(-c3ccc(S(=O)(=O)NC4CCN(Cc5ccccc5)CC4)cc3)cc2n(C)c1=O 10.1016/j.bmcl.2006.04.074
CHEMBL211347 79267 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 507 6 2 7 2.2 Cn1c(=O)c2[nH]c(-c3ccc(S(=O)(=O)NC4CCN(Cc5ccccc5)CC4)cc3)cc2n(C)c1=O 10.1016/j.bmcl.2006.04.074
155518555 170294 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 387 7 1 7 1.5 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(C(N)=O)sc21 10.1016/j.ejmech.2018.11.045
CHEMBL4446433 170294 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 387 7 1 7 1.5 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(C(N)=O)sc21 10.1016/j.ejmech.2018.11.045
155537687 172331 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 380 6 0 6 3.0 COCCn1c(=O)n(CC(F)(F)c2ccccc2)c(=O)c2c(C)csc21 10.1016/j.ejmech.2018.11.045
CHEMBL4475483 172331 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 380 6 0 6 3.0 COCCn1c(=O)n(CC(F)(F)c2ccccc2)c(=O)c2c(C)csc21 10.1016/j.ejmech.2018.11.045
155560676 175115 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 282 4 0 6 1.5 CCn1c(=O)c2c(C)c(C)sc2n(CCOC)c1=O 10.1016/j.ejmech.2018.11.045
CHEMBL4569387 175115 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 282 4 0 6 1.5 CCn1c(=O)c2c(C)c(C)sc2n(CCOC)c1=O 10.1016/j.ejmech.2018.11.045
71601631 86923 None 0 Human Binding pIC50 = 6.4 6.4 - 2
Inhibition of human A2B adenosine receptor transfected in CHO cells assessed as inhibition of NECA-induced cyclic AMP production after 10 mins by competitive protein binding assayInhibition of human A2B adenosine receptor transfected in CHO cells assessed as inhibition of NECA-induced cyclic AMP production after 10 mins by competitive protein binding assay
ChEMBL 287 2 1 5 3.1 Nc1nc(-c2ccccc2)nc2cn(-c3ccccc3)nc12 10.1021/jm400068e
CHEMBL2322917 86923 None 0 Human Binding pIC50 = 6.4 6.4 - 2
Inhibition of human A2B adenosine receptor transfected in CHO cells assessed as inhibition of NECA-induced cyclic AMP production after 10 mins by competitive protein binding assayInhibition of human A2B adenosine receptor transfected in CHO cells assessed as inhibition of NECA-induced cyclic AMP production after 10 mins by competitive protein binding assay
ChEMBL 287 2 1 5 3.1 Nc1nc(-c2ccccc2)nc2cn(-c3ccccc3)nc12 10.1021/jm400068e
155512463 169635 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 330 6 0 6 2.1 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2ccsc21 10.1016/j.ejmech.2018.11.045
CHEMBL4437132 169635 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 330 6 0 6 2.1 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2ccsc21 10.1016/j.ejmech.2018.11.045
59351824 174026 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 286 3 1 4 2.3 Cc1csc2[nH]c(=O)n(CCc3ccccc3)c(=O)c12 10.1016/j.ejmech.2018.11.045
CHEMBL4543255 174026 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 286 3 1 4 2.3 Cc1csc2[nH]c(=O)n(CCc3ccccc3)c(=O)c12 10.1016/j.ejmech.2018.11.045
155537810 172328 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 384 6 0 6 3.0 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c3c(sc21)CCCC3 10.1016/j.ejmech.2018.11.045
CHEMBL4475461 172328 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 384 6 0 6 3.0 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c3c(sc21)CCCC3 10.1016/j.ejmech.2018.11.045
155520204 170467 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 420 7 0 6 4.1 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(-c3ccccc3)sc21 10.1016/j.ejmech.2018.11.045
CHEMBL4448896 170467 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 420 7 0 6 4.1 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(-c3ccccc3)sc21 10.1016/j.ejmech.2018.11.045
155559377 174848 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 316 5 0 6 2.0 COCCn1c(=O)n(CC=C(F)F)c(=O)c2c(C)csc21 10.1016/j.ejmech.2018.11.045
CHEMBL4562969 174848 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 316 5 0 6 2.0 COCCn1c(=O)n(CC=C(F)F)c(=O)c2c(C)csc21 10.1016/j.ejmech.2018.11.045
11796362 115101 None 0 Human Binding pIC50 = 7.3 7.3 - 1
Antagonist activity at adenosine A2B receptor (unknown origin)Antagonist activity at adenosine A2B receptor (unknown origin)
ChEMBL 419 7 1 7 2.9 COc1cccc(N2CCN(CCOC(=O)c3cc(Cl)c(N)cc3OC)CC2)c1 10.1039/C1MD00213A
CHEMBL334325 115101 None 0 Human Binding pIC50 = 7.3 7.3 - 1
Antagonist activity at adenosine A2B receptor (unknown origin)Antagonist activity at adenosine A2B receptor (unknown origin)
ChEMBL 419 7 1 7 2.9 COc1cccc(N2CCN(CCOC(=O)c3cc(Cl)c(N)cc3OC)CC2)c1 10.1039/C1MD00213A
155529645 171428 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 421 7 1 7 2.0 CCN(CCO)C(=O)c1sc2c(c1C)c(=O)n(CC)c(=O)n2CCC(F)(F)F 10.1016/j.ejmech.2018.11.045
CHEMBL4462879 171428 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 421 7 1 7 2.0 CCN(CCO)C(=O)c1sc2c(c1C)c(=O)n(CC)c(=O)n2CCC(F)(F)F 10.1016/j.ejmech.2018.11.045
155521508 170704 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 370 5 0 6 3.0 Cc1csc2c1c(=O)n(CCc1ccccc1)c(=O)n2CC1CCCO1 10.1016/j.ejmech.2018.11.045
CHEMBL4451942 170704 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 370 5 0 6 3.0 Cc1csc2c1c(=O)n(CCc1ccccc1)c(=O)n2CC1CCCO1 10.1016/j.ejmech.2018.11.045
155551418 173963 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 434 8 0 6 4.0 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(Cc3ccccc3)sc21 10.1016/j.ejmech.2018.11.045
CHEMBL4541543 173963 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 434 8 0 6 4.0 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(Cc3ccccc3)sc21 10.1016/j.ejmech.2018.11.045
155569093 176003 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 383 5 0 6 3.1 Cc1csc2c1c(=O)n(CCc1cccnc1)c(=O)n2CCC(F)(F)F 10.1016/j.ejmech.2018.11.045
CHEMBL4589448 176003 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 383 5 0 6 3.1 Cc1csc2c1c(=O)n(CCc1cccnc1)c(=O)n2CCC(F)(F)F 10.1016/j.ejmech.2018.11.045
155537122 172265 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 382 5 0 5 3.7 Cc1csc2c1c(=O)n(CCc1ccccc1)c(=O)n2CCC(F)(F)F 10.1016/j.ejmech.2018.11.045
CHEMBL4474572 172265 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 382 5 0 5 3.7 Cc1csc2c1c(=O)n(CCc1ccccc1)c(=O)n2CCC(F)(F)F 10.1016/j.ejmech.2018.11.045
10550242 17257 None 0 Human Binding pIC50 = 5.2 5.2 - 1
Antagonist activity at adenosine A2B receptor (unknown origin)Antagonist activity at adenosine A2B receptor (unknown origin)
ChEMBL 423 6 1 6 3.6 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(c2ccccc2Cl)CC1 10.1039/C1MD00213A
CHEMBL125670 17257 None 0 Human Binding pIC50 = 5.2 5.2 - 1
Antagonist activity at adenosine A2B receptor (unknown origin)Antagonist activity at adenosine A2B receptor (unknown origin)
ChEMBL 423 6 1 6 3.6 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(c2ccccc2Cl)CC1 10.1039/C1MD00213A
11224 582 None 35 Human Binding pIC50 = 7.2 7.2 - 1
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 433 4 1 7 2.1 CCn1c(=O)c2c(C)c(sc2n(c1=O)CCC(F)(F)F)C(=O)N1CCC(CC1)O 10.1016/j.ejmech.2018.11.045
118016229 582 None 35 Human Binding pIC50 = 7.2 7.2 - 1
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 433 4 1 7 2.1 CCn1c(=O)c2c(C)c(sc2n(c1=O)CCC(F)(F)F)C(=O)N1CCC(CC1)O 10.1016/j.ejmech.2018.11.045
CHEMBL4522981 582 None 35 Human Binding pIC50 = 7.2 7.2 - 1
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 433 4 1 7 2.1 CCn1c(=O)c2c(C)c(sc2n(c1=O)CCC(F)(F)F)C(=O)N1CCC(CC1)O 10.1016/j.ejmech.2018.11.045
44413154 78005 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 479 4 1 7 1.7 Cn1c(=O)c2[nH]c(-c3ccc(S(=O)(=O)N4CCN(c5ccccc5)CC4)cc3)cc2n(C)c1=O 10.1016/j.bmcl.2006.04.074
CHEMBL209742 78005 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 479 4 1 7 1.7 Cn1c(=O)c2[nH]c(-c3ccc(S(=O)(=O)N4CCN(c5ccccc5)CC4)cc3)cc2n(C)c1=O 10.1016/j.bmcl.2006.04.074
44413106 79902 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 546 7 1 8 2.5 CCCn1c(=O)c2[nH]c(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc(C#N)cc5)CC4)cc3)cc2n(C)c1=O 10.1016/j.bmcl.2006.04.074
CHEMBL212416 79902 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 546 7 1 8 2.5 CCCn1c(=O)c2[nH]c(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc(C#N)cc5)CC4)cc3)cc2n(C)c1=O 10.1016/j.bmcl.2006.04.074
2690 903 None 66 Human Binding pIC50 = 7.2 7.2 -30 9
Displacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes preincubated for 30 mins followed by PSB-12105 addition measured after 20 mins by flow cytometric methodDisplacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes preincubated for 30 mins followed by PSB-12105 addition measured after 20 mins by flow cytometric method
ChEMBL 285 1 1 6 2.8 Clc1ccc2c(c1)c1nc(nn1c(n2)N)c1ccco1 10.1021/acs.jmedchem.7b01627
384 903 None 66 Human Binding pIC50 = 7.2 7.2 -30 9
Displacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes preincubated for 30 mins followed by PSB-12105 addition measured after 20 mins by flow cytometric methodDisplacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes preincubated for 30 mins followed by PSB-12105 addition measured after 20 mins by flow cytometric method
ChEMBL 285 1 1 6 2.8 Clc1ccc2c(c1)c1nc(nn1c(n2)N)c1ccco1 10.1021/acs.jmedchem.7b01627
CHEMBL16687 903 None 66 Human Binding pIC50 = 7.2 7.2 -30 9
Displacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes preincubated for 30 mins followed by PSB-12105 addition measured after 20 mins by flow cytometric methodDisplacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes preincubated for 30 mins followed by PSB-12105 addition measured after 20 mins by flow cytometric method
ChEMBL 285 1 1 6 2.8 Clc1ccc2c(c1)c1nc(nn1c(n2)N)c1ccco1 10.1021/acs.jmedchem.7b01627
122574669 175832 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 268 4 0 6 1.2 CCn1c(=O)c2c(C)csc2n(CCOC)c1=O 10.1016/j.ejmech.2018.11.045
CHEMBL4585015 175832 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 268 4 0 6 1.2 CCn1c(=O)c2c(C)csc2n(CCOC)c1=O 10.1016/j.ejmech.2018.11.045
10645103 164341 None 0 Human Binding pIC50 = 6.2 6.2 - 1
Antagonist activity at adenosine A2B receptor (unknown origin)Antagonist activity at adenosine A2B receptor (unknown origin)
ChEMBL 407 6 1 6 3.0 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(c2ccccc2F)CC1 10.1039/C1MD00213A
CHEMBL421256 164341 None 0 Human Binding pIC50 = 6.2 6.2 - 1
Antagonist activity at adenosine A2B receptor (unknown origin)Antagonist activity at adenosine A2B receptor (unknown origin)
ChEMBL 407 6 1 6 3.0 COc1cc(N)c(Cl)cc1C(=O)OCCN1CCN(c2ccccc2F)CC1 10.1039/C1MD00213A
11224 582 None 35 Human Binding pIC50 = 7.2 7.2 - 1
Antagonist activity at recombinant human A2B adenosine receptor expressed in CHO cells after 3 to 4 hrs by luciferase reporter gene assayAntagonist activity at recombinant human A2B adenosine receptor expressed in CHO cells after 3 to 4 hrs by luciferase reporter gene assay
ChEMBL 433 4 1 7 2.1 CCn1c(=O)c2c(C)c(sc2n(c1=O)CCC(F)(F)F)C(=O)N1CCC(CC1)O 10.1016/j.ejmech.2018.11.045
118016229 582 None 35 Human Binding pIC50 = 7.2 7.2 - 1
Antagonist activity at recombinant human A2B adenosine receptor expressed in CHO cells after 3 to 4 hrs by luciferase reporter gene assayAntagonist activity at recombinant human A2B adenosine receptor expressed in CHO cells after 3 to 4 hrs by luciferase reporter gene assay
ChEMBL 433 4 1 7 2.1 CCn1c(=O)c2c(C)c(sc2n(c1=O)CCC(F)(F)F)C(=O)N1CCC(CC1)O 10.1016/j.ejmech.2018.11.045
CHEMBL4522981 582 None 35 Human Binding pIC50 = 7.2 7.2 - 1
Antagonist activity at recombinant human A2B adenosine receptor expressed in CHO cells after 3 to 4 hrs by luciferase reporter gene assayAntagonist activity at recombinant human A2B adenosine receptor expressed in CHO cells after 3 to 4 hrs by luciferase reporter gene assay
ChEMBL 433 4 1 7 2.1 CCn1c(=O)c2c(C)c(sc2n(c1=O)CCC(F)(F)F)C(=O)N1CCC(CC1)O 10.1016/j.ejmech.2018.11.045
10193 3010 None 40 Human Binding pIC50 = 6.2 6.2 -46 4
Inhibition of A2bR (unknown origin) expressed in HEK293 cells incubated overnight by dual luciferase reporter assayInhibition of A2bR (unknown origin) expressed in HEK293 cells incubated overnight by dual luciferase reporter assay
ChEMBL 305 2 1 7 1.2 Nc1nc(nc(c1Br)n1cccn1)n1cccn1 nan
53466958 3010 None 40 Human Binding pIC50 = 6.2 6.2 -46 4
Inhibition of A2bR (unknown origin) expressed in HEK293 cells incubated overnight by dual luciferase reporter assayInhibition of A2bR (unknown origin) expressed in HEK293 cells incubated overnight by dual luciferase reporter assay
ChEMBL 305 2 1 7 1.2 Nc1nc(nc(c1Br)n1cccn1)n1cccn1 nan
53466958.0 3010 None 40 Human Binding pIC50 = 6.2 6.2 -46 4
Inhibition of A2bR (unknown origin) expressed in HEK293 cells incubated overnight by dual luciferase reporter assayInhibition of A2bR (unknown origin) expressed in HEK293 cells incubated overnight by dual luciferase reporter assay
ChEMBL 305 2 1 7 1.2 Nc1nc(nc(c1Br)n1cccn1)n1cccn1 nan
CHEMBL3638684 3010 None 40 Human Binding pIC50 = 6.2 6.2 -46 4
Inhibition of A2bR (unknown origin) expressed in HEK293 cells incubated overnight by dual luciferase reporter assayInhibition of A2bR (unknown origin) expressed in HEK293 cells incubated overnight by dual luciferase reporter assay
ChEMBL 305 2 1 7 1.2 Nc1nc(nc(c1Br)n1cccn1)n1cccn1 nan
CHEMBL3694769 3010 None 40 Human Binding pIC50 = 6.2 6.2 -46 4
Inhibition of A2bR (unknown origin) expressed in HEK293 cells incubated overnight by dual luciferase reporter assayInhibition of A2bR (unknown origin) expressed in HEK293 cells incubated overnight by dual luciferase reporter assay
ChEMBL 305 2 1 7 1.2 Nc1nc(nc(c1Br)n1cccn1)n1cccn1 nan
44413125 78077 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 529 5 1 7 2.0 Cn1c(=O)c2[nH]c(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc(F)cc5F)CC4)cc3)cc2n(C)c1=O 10.1016/j.bmcl.2006.04.074
CHEMBL210088 78077 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 529 5 1 7 2.0 Cn1c(=O)c2[nH]c(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc(F)cc5F)CC4)cc3)cc2n(C)c1=O 10.1016/j.bmcl.2006.04.074
10196060 78149 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 511 5 1 7 1.9 Cn1c(=O)c2[nH]c(-c3ccc(S(=O)(=O)N4CCN(Cc5cccc(F)c5)CC4)cc3)cc2n(C)c1=O 10.1016/j.bmcl.2006.04.074
CHEMBL210383 78149 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 511 5 1 7 1.9 Cn1c(=O)c2[nH]c(-c3ccc(S(=O)(=O)N4CCN(Cc5cccc(F)c5)CC4)cc3)cc2n(C)c1=O 10.1016/j.bmcl.2006.04.074
155259564 185219 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Inhibition of A2bR (unknown origin) expressed in HEK293 cells incubated overnight by dual luciferase reporter assayInhibition of A2bR (unknown origin) expressed in HEK293 cells incubated overnight by dual luciferase reporter assay
ChEMBL 339 5 3 9 1.2 Nc1nc(NCCc2ccc(O)cc2)nc2nc(C3=CCCO3)nn12 nan
CHEMBL4857871 185219 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Inhibition of A2bR (unknown origin) expressed in HEK293 cells incubated overnight by dual luciferase reporter assayInhibition of A2bR (unknown origin) expressed in HEK293 cells incubated overnight by dual luciferase reporter assay
ChEMBL 339 5 3 9 1.2 Nc1nc(NCCc2ccc(O)cc2)nc2nc(C3=CCCO3)nn12 nan
155559834 174920 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 400 5 0 5 3.9 Cc1csc2c1c(=O)n(CCc1ccccc1F)c(=O)n2CCC(F)(F)F 10.1016/j.ejmech.2018.11.045
CHEMBL4564912 174920 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 400 5 0 5 3.9 Cc1csc2c1c(=O)n(CCc1ccccc1F)c(=O)n2CCC(F)(F)F 10.1016/j.ejmech.2018.11.045
10621961 208080 None 0 Human Binding pIC50 = 5.1 5.1 - 3
Inhibition of 50 uM 5`-(N-ethylcarboxamido)adenosine induced cAMP production in CHO cell line expressing human Adenosine A2B receptorInhibition of 50 uM 5`-(N-ethylcarboxamido)adenosine induced cAMP production in CHO cell line expressing human Adenosine A2B receptor
ChEMBL 418 4 2 7 4.0 Nc1ccc(CC(=O)Nc2nc3ccc(Cl)cc3c3nc(-c4ccco4)nn23)cc1 10.1021/jm980094b
CHEMBL97748 208080 None 0 Human Binding pIC50 = 5.1 5.1 - 3
Inhibition of 50 uM 5`-(N-ethylcarboxamido)adenosine induced cAMP production in CHO cell line expressing human Adenosine A2B receptorInhibition of 50 uM 5`-(N-ethylcarboxamido)adenosine induced cAMP production in CHO cell line expressing human Adenosine A2B receptor
ChEMBL 418 4 2 7 4.0 Nc1ccc(CC(=O)Nc2nc3ccc(Cl)cc3c3nc(-c4ccco4)nn23)cc1 10.1021/jm980094b
44413096 138970 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 467 8 2 7 2.1 CCn1c(=O)c2[nH]c(-c3ccc(S(=O)(=O)NCCc4ccccn4)cc3)cc2n(CC)c1=O 10.1016/j.bmcl.2006.04.074
CHEMBL378527 138970 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 467 8 2 7 2.1 CCn1c(=O)c2[nH]c(-c3ccc(S(=O)(=O)NCCc4ccccn4)cc3)cc2n(CC)c1=O 10.1016/j.bmcl.2006.04.074
155552481 174057 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 443 8 0 8 2.3 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(CN3CCOCC3)sc21 10.1016/j.ejmech.2018.11.045
CHEMBL4544040 174057 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 443 8 0 8 2.3 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(CN3CCOCC3)sc21 10.1016/j.ejmech.2018.11.045
155541183 173012 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 412 8 0 7 3.0 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(C(=O)C3CC3)sc21 10.1016/j.ejmech.2018.11.045
CHEMBL4518356 173012 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 412 8 0 7 3.0 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(C(=O)C3CC3)sc21 10.1016/j.ejmech.2018.11.045
155553932 175450 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 438 8 1 7 3.0 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(Cc3c[nH]c(C)n3)sc21 10.1016/j.ejmech.2018.11.045
CHEMBL4576817 175450 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 438 8 1 7 3.0 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c(C)c(Cc3c[nH]c(C)n3)sc21 10.1016/j.ejmech.2018.11.045
57429602 157239 None 0 Human Binding pIC50 = 7.1 7.1 - 1
Antagonist activity at human adenosine A2B receptor expressed in mouse NIH/3T3 cells assessed as inhibition of NECA-induced IL-6 release incubated for 15 mins followed by agonist treatment for 15 mins by HTRF assayAntagonist activity at human adenosine A2B receptor expressed in mouse NIH/3T3 cells assessed as inhibition of NECA-induced IL-6 release incubated for 15 mins followed by agonist treatment for 15 mins by HTRF assay
ChEMBL 500 7 1 8 3.5 CCCn1c(=O)c2[nH]c(-c3cnn(CC#Cc4cccc(OC(F)(F)F)c4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2017.04.014
CHEMBL4076435 157239 None 0 Human Binding pIC50 = 7.1 7.1 - 1
Antagonist activity at human adenosine A2B receptor expressed in mouse NIH/3T3 cells assessed as inhibition of NECA-induced IL-6 release incubated for 15 mins followed by agonist treatment for 15 mins by HTRF assayAntagonist activity at human adenosine A2B receptor expressed in mouse NIH/3T3 cells assessed as inhibition of NECA-induced IL-6 release incubated for 15 mins followed by agonist treatment for 15 mins by HTRF assay
ChEMBL 500 7 1 8 3.5 CCCn1c(=O)c2[nH]c(-c3cnn(CC#Cc4cccc(OC(F)(F)F)c4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2017.04.014
44413142 78211 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 521 6 1 7 2.5 CN(C1CCN(Cc2ccccc2)CC1)S(=O)(=O)c1ccc(-c2cc3c([nH]2)c(=O)n(C)c(=O)n3C)cc1 10.1016/j.bmcl.2006.04.074
CHEMBL210560 78211 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 521 6 1 7 2.5 CN(C1CCN(Cc2ccccc2)CC1)S(=O)(=O)c1ccc(-c2cc3c([nH]2)c(=O)n(C)c(=O)n3C)cc1 10.1016/j.bmcl.2006.04.074
176407 4148 None 84 Human Binding pIC50 = 7.0 7.0 -34 6
Displacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes preincubated for 30 mins followed by PSB-12105 addition measured after 20 mins by flow cytometric methodDisplacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes preincubated for 30 mins followed by PSB-12105 addition measured after 20 mins by flow cytometric method
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1021/acs.jmedchem.7b01627
405 4148 None 84 Human Binding pIC50 = 7.0 7.0 -34 6
Displacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes preincubated for 30 mins followed by PSB-12105 addition measured after 20 mins by flow cytometric methodDisplacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes preincubated for 30 mins followed by PSB-12105 addition measured after 20 mins by flow cytometric method
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1021/acs.jmedchem.7b01627
CHEMBL113142 4148 None 84 Human Binding pIC50 = 7.0 7.0 -34 6
Displacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes preincubated for 30 mins followed by PSB-12105 addition measured after 20 mins by flow cytometric methodDisplacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes preincubated for 30 mins followed by PSB-12105 addition measured after 20 mins by flow cytometric method
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1021/acs.jmedchem.7b01627
DB08770 4148 None 84 Human Binding pIC50 = 7.0 7.0 -34 6
Displacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes preincubated for 30 mins followed by PSB-12105 addition measured after 20 mins by flow cytometric methodDisplacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes preincubated for 30 mins followed by PSB-12105 addition measured after 20 mins by flow cytometric method
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1021/acs.jmedchem.7b01627
135515408 117074 None 0 Human Binding pIC50 = 5.0 5.0 - 0
Displacement of specific [3H]DPCPX binding at human adenosine A2B receptor expressed in HEK293 cells.Displacement of specific [3H]DPCPX binding at human adenosine A2B receptor expressed in HEK293 cells.
ChEMBL 310 4 1 5 3.1 CCCCc1nc2[nH]ncc2c2nc(-c3ccc(F)cc3)nn12 10.1016/j.bmcl.2004.04.099
CHEMBL339218 117074 None 0 Human Binding pIC50 = 5.0 5.0 - 0
Displacement of specific [3H]DPCPX binding at human adenosine A2B receptor expressed in HEK293 cells.Displacement of specific [3H]DPCPX binding at human adenosine A2B receptor expressed in HEK293 cells.
ChEMBL 310 4 1 5 3.1 CCCCc1nc2[nH]ncc2c2nc(-c3ccc(F)cc3)nn12 10.1016/j.bmcl.2004.04.099
155540197 172902 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 370 6 0 6 2.6 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c3c(sc21)CCC3 10.1016/j.ejmech.2018.11.045
CHEMBL4516075 172902 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 370 6 0 6 2.6 COCCn1c(=O)n(CCc2ccccc2)c(=O)c2c3c(sc21)CCC3 10.1016/j.ejmech.2018.11.045
155549654 173906 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 435 8 0 7 2.6 CCN(CC)C(=O)c1sc2c(c1C)c(=O)n(CCOC)c(=O)n2CCC(F)(F)F 10.1016/j.ejmech.2018.11.045
CHEMBL4540250 173906 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Displacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assayDisplacement of [3H]DPCPX from human A2B adenosine receptor expressed in HEK293 cell membranes after 60 mins by radioligand displacement assay
ChEMBL 435 8 0 7 2.6 CCN(CC)C(=O)c1sc2c(c1C)c(=O)n(CCOC)c(=O)n2CCC(F)(F)F 10.1016/j.ejmech.2018.11.045
450 2970 None 9 Human Binding pKd = 9.8 9.8 257 4
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 525 10 3 6 3.6 CC(=O)NCCNc1nc(nc2c1cc([nH]2)C(=O)N1CCN(CC1)CCCc1ccccc1)c1ccccc1 10.1021/jm900413e
454 2970 None 9 Human Binding pKd = 9.8 9.8 257 4
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 525 10 3 6 3.6 CC(=O)NCCNc1nc(nc2c1cc([nH]2)C(=O)N1CCN(CC1)CCCc1ccccc1)c1ccccc1 10.1021/jm900413e
5311041 2970 None 9 Human Binding pKd = 9.8 9.8 257 4
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 525 10 3 6 3.6 CC(=O)NCCNc1nc(nc2c1cc([nH]2)C(=O)N1CCN(CC1)CCCc1ccccc1)c1ccccc1 10.1021/jm900413e
CHEMBL485862 2970 None 9 Human Binding pKd = 9.8 9.8 257 4
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 525 10 3 6 3.6 CC(=O)NCCNc1nc(nc2c1cc([nH]2)C(=O)N1CCN(CC1)CCCc1ccccc1)c1ccccc1 10.1021/jm900413e
3284 3216 None 35 Mouse Binding pKd = 9.5 9.5 1 7
Displacement of [3H]PSB-603 from mouse recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from mouse recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 528 6 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)c1ccc(cc1)Cl 10.1021/jm900413e
44185871 3216 None 35 Mouse Binding pKd = 9.5 9.5 1 7
Displacement of [3H]PSB-603 from mouse recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from mouse recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 528 6 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)c1ccc(cc1)Cl 10.1021/jm900413e
5728 3216 None 35 Mouse Binding pKd = 9.5 9.5 1 7
Displacement of [3H]PSB-603 from mouse recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from mouse recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 528 6 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)c1ccc(cc1)Cl 10.1021/jm900413e
CHEMBL483688 3216 None 35 Mouse Binding pKd = 9.5 9.5 1 7
Displacement of [3H]PSB-603 from mouse recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from mouse recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 528 6 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)c1ccc(cc1)Cl 10.1021/jm900413e
3284 3216 None 35 Human Binding pKd = 9.4 9.4 -1 7
Binding affinity to human recombinant adenosine A2B receptor expressed in CHO cells by saturation experimentBinding affinity to human recombinant adenosine A2B receptor expressed in CHO cells by saturation experiment
ChEMBL 528 6 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)c1ccc(cc1)Cl 10.1021/jm900413e
44185871 3216 None 35 Human Binding pKd = 9.4 9.4 -1 7
Binding affinity to human recombinant adenosine A2B receptor expressed in CHO cells by saturation experimentBinding affinity to human recombinant adenosine A2B receptor expressed in CHO cells by saturation experiment
ChEMBL 528 6 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)c1ccc(cc1)Cl 10.1021/jm900413e
5728 3216 None 35 Human Binding pKd = 9.4 9.4 -1 7
Binding affinity to human recombinant adenosine A2B receptor expressed in CHO cells by saturation experimentBinding affinity to human recombinant adenosine A2B receptor expressed in CHO cells by saturation experiment
ChEMBL 528 6 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)c1ccc(cc1)Cl 10.1021/jm900413e
CHEMBL483688 3216 None 35 Human Binding pKd = 9.4 9.4 -1 7
Binding affinity to human recombinant adenosine A2B receptor expressed in CHO cells by saturation experimentBinding affinity to human recombinant adenosine A2B receptor expressed in CHO cells by saturation experiment
ChEMBL 528 6 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)c1ccc(cc1)Cl 10.1021/jm900413e
3284 3216 None 35 Human Binding pKd = 9.2 9.2 -1 7
Binding affinity to human recombinant adenosine A2B receptor expressed in CHO cells by kinetic experimentBinding affinity to human recombinant adenosine A2B receptor expressed in CHO cells by kinetic experiment
ChEMBL 528 6 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)c1ccc(cc1)Cl 10.1021/jm900413e
44185871 3216 None 35 Human Binding pKd = 9.2 9.2 -1 7
Binding affinity to human recombinant adenosine A2B receptor expressed in CHO cells by kinetic experimentBinding affinity to human recombinant adenosine A2B receptor expressed in CHO cells by kinetic experiment
ChEMBL 528 6 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)c1ccc(cc1)Cl 10.1021/jm900413e
5728 3216 None 35 Human Binding pKd = 9.2 9.2 -1 7
Binding affinity to human recombinant adenosine A2B receptor expressed in CHO cells by kinetic experimentBinding affinity to human recombinant adenosine A2B receptor expressed in CHO cells by kinetic experiment
ChEMBL 528 6 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)c1ccc(cc1)Cl 10.1021/jm900413e
CHEMBL483688 3216 None 35 Human Binding pKd = 9.2 9.2 -1 7
Binding affinity to human recombinant adenosine A2B receptor expressed in CHO cells by kinetic experimentBinding affinity to human recombinant adenosine A2B receptor expressed in CHO cells by kinetic experiment
ChEMBL 528 6 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)c1ccc(cc1)Cl 10.1021/jm900413e
449 2643 None 52 Human Binding pKd = 9.0 9.0 -1 9
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10.1021/jm900413e
453 2643 None 52 Human Binding pKd = 9.0 9.0 -1 9
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10.1021/jm900413e
6603931 2643 None 52 Human Binding pKd = 9.0 9.0 -1 9
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10.1021/jm900413e
CHEMBL273807 2643 None 52 Human Binding pKd = 9.0 9.0 -1 9
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10.1021/jm900413e
135484064 2616 None 4 Human Binding pKd = 8.8 8.8 21 4
Binding affinity of [3H]-MRE 2029-F20 towards human adenosine A2b receptor expressed in CHO cellsBinding affinity of [3H]-MRE 2029-F20 towards human adenosine A2b receptor expressed in CHO cells
ChEMBL 509 9 2 11 1.9 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)Nc1ccc2c(c1)OCO2 10.1016/j.bmcl.2004.03.110
390 2616 None 4 Human Binding pKd = 8.8 8.8 21 4
Binding affinity of [3H]-MRE 2029-F20 towards human adenosine A2b receptor expressed in CHO cellsBinding affinity of [3H]-MRE 2029-F20 towards human adenosine A2b receptor expressed in CHO cells
ChEMBL 509 9 2 11 1.9 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)Nc1ccc2c(c1)OCO2 10.1016/j.bmcl.2004.03.110
CHEMBL260331 2616 None 4 Human Binding pKd = 8.8 8.8 21 4
Binding affinity of [3H]-MRE 2029-F20 towards human adenosine A2b receptor expressed in CHO cellsBinding affinity of [3H]-MRE 2029-F20 towards human adenosine A2b receptor expressed in CHO cells
ChEMBL 509 9 2 11 1.9 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)Nc1ccc2c(c1)OCO2 10.1016/j.bmcl.2004.03.110
135484064 2616 None 4 Human Binding pKd = 8.8 8.8 21 4
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 509 9 2 11 1.9 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)Nc1ccc2c(c1)OCO2 10.1021/jm900413e
390 2616 None 4 Human Binding pKd = 8.8 8.8 21 4
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 509 9 2 11 1.9 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)Nc1ccc2c(c1)OCO2 10.1021/jm900413e
CHEMBL260331 2616 None 4 Human Binding pKd = 8.8 8.8 21 4
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 509 9 2 11 1.9 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)Nc1ccc2c(c1)OCO2 10.1021/jm900413e
2690 903 None 66 Human Binding pKd = 8 8.0 -30 9
pA2 value at human Adenosine A2B receptor from Schild plots with slopes approaching unitypA2 value at human Adenosine A2B receptor from Schild plots with slopes approaching unity
ChEMBL 285 1 1 6 2.8 Clc1ccc2c(c1)c1nc(nn1c(n2)N)c1ccco1 10.1021/jm980094b
384 903 None 66 Human Binding pKd = 8 8.0 -30 9
pA2 value at human Adenosine A2B receptor from Schild plots with slopes approaching unitypA2 value at human Adenosine A2B receptor from Schild plots with slopes approaching unity
ChEMBL 285 1 1 6 2.8 Clc1ccc2c(c1)c1nc(nn1c(n2)N)c1ccco1 10.1021/jm980094b
CHEMBL16687 903 None 66 Human Binding pKd = 8 8.0 -30 9
pA2 value at human Adenosine A2B receptor from Schild plots with slopes approaching unitypA2 value at human Adenosine A2B receptor from Schild plots with slopes approaching unity
ChEMBL 285 1 1 6 2.8 Clc1ccc2c(c1)c1nc(nn1c(n2)N)c1ccco1 10.1021/jm980094b
10339165 207744 None 0 Human Binding pKd = 8 8.0 -2 4
pA2 value at human Adenosine A2B receptor from Schild plots with slopes approaching unitypA2 value at human Adenosine A2B receptor from Schild plots with slopes approaching unity
ChEMBL 370 5 2 7 2.9 NCCCC(=O)Nc1nc2ccc(Cl)cc2c2nc(-c3ccco3)nn12 10.1021/jm980094b
CHEMBL95811 207744 None 0 Human Binding pKd = 8 8.0 -2 4
pA2 value at human Adenosine A2B receptor from Schild plots with slopes approaching unitypA2 value at human Adenosine A2B receptor from Schild plots with slopes approaching unity
ChEMBL 370 5 2 7 2.9 NCCCC(=O)Nc1nc2ccc(Cl)cc2c2nc(-c3ccco3)nn12 10.1021/jm980094b
7064 116714 None 98 Human Binding pKd = 4.0 4.0 -70 4
Binding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assayBinding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assay
ChEMBL 187 1 2 5 0.7 Nc1nc(N)nc(-c2ccccc2)n1 10.1021/acsmedchemlett.2c00099
CHEMBL337319 116714 None 98 Human Binding pKd = 4.0 4.0 -70 4
Binding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assayBinding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assay
ChEMBL 187 1 2 5 0.7 Nc1nc(N)nc(-c2ccccc2)n1 10.1021/acsmedchemlett.2c00099
554203 191439 None 75 Human Binding pKd = 4.0 4.0 -1 4
Binding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assayBinding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assay
ChEMBL 177 1 1 4 1.8 Nc1nsc(-c2ccccc2)n1 10.1021/acsmedchemlett.2c00099
CHEMBL5193006 191439 None 75 Human Binding pKd = 4.0 4.0 -1 4
Binding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assayBinding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assay
ChEMBL 177 1 1 4 1.8 Nc1nsc(-c2ccccc2)n1 10.1021/acsmedchemlett.2c00099
2727447 150437 None 7 Human Binding pKd = 3.9 3.9 -109 4
Binding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assayBinding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assay
ChEMBL 211 1 1 5 1.4 Nc1ccc2nnc(-c3ccccc3)n2n1 10.1021/acsmedchemlett.2c00099
CHEMBL3954022 150437 None 7 Human Binding pKd = 3.9 3.9 -109 4
Binding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assayBinding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assay
ChEMBL 211 1 1 5 1.4 Nc1ccc2nnc(-c3ccccc3)n2n1 10.1021/acsmedchemlett.2c00099
CHEMBL4550896 214000 None 5 Human Binding pKd = 3.9 3.9 -3 4
Binding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assayBinding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assay
ChEMBL None None None O=C(Nc1ccc2ccccc2n1)c1ccco1 10.1021/acsmedchemlett.2c00099
2774349 33135 None 39 Human Binding pKd = 3.9 3.9 -1 4
Binding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assayBinding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assay
ChEMBL 202 2 1 4 0.7 Cc1nn(-c2ccccc2)nc1C(N)=O 10.1021/acsmedchemlett.2c00099
CHEMBL1417210 33135 None 39 Human Binding pKd = 3.9 3.9 -1 4
Binding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assayBinding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assay
ChEMBL 202 2 1 4 0.7 Cc1nn(-c2ccccc2)nc1C(N)=O 10.1021/acsmedchemlett.2c00099
344385 192209 None 49 Human Binding pKd = 3.8 3.8 -7 4
Binding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assayBinding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assay
ChEMBL 176 0 1 3 0.2 Cn1c(=O)[nH]c2ccccc2c1=O 10.1021/acsmedchemlett.2c00099
CHEMBL5204663 192209 None 49 Human Binding pKd = 3.8 3.8 -7 4
Binding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assayBinding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assay
ChEMBL 176 0 1 3 0.2 Cn1c(=O)[nH]c2ccccc2c1=O 10.1021/acsmedchemlett.2c00099
2747546 192414 None 12 Human Binding pKd = 4.7 4.7 -2 4
Binding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assayBinding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assay
ChEMBL 309 3 1 3 3.0 CS(=O)(=O)c1ccc(C(=O)Nc2cccc(Cl)c2)cc1 10.1021/acsmedchemlett.2c00099
CHEMBL5208068 192414 None 12 Human Binding pKd = 4.7 4.7 -2 4
Binding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assayBinding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assay
ChEMBL 309 3 1 3 3.0 CS(=O)(=O)c1ccc(C(=O)Nc2cccc(Cl)c2)cc1 10.1021/acsmedchemlett.2c00099
16362023 191444 None 4 Human Binding pKd = 3.7 3.7 -3 4
Binding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assayBinding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assay
ChEMBL 229 3 2 2 2.2 CC(C)NC(=O)c1cc(-c2ccccc2)[nH]n1 10.1021/acsmedchemlett.2c00099
CHEMBL5193059 191444 None 4 Human Binding pKd = 3.7 3.7 -3 4
Binding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assayBinding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assay
ChEMBL 229 3 2 2 2.2 CC(C)NC(=O)c1cc(-c2ccccc2)[nH]n1 10.1021/acsmedchemlett.2c00099
2314144 50483 None 4 Human Binding pKd = 3.7 3.7 -1 4
Binding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assayBinding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assay
ChEMBL 251 3 1 4 2.3 O=c1cc(NCc2ccccc2)nc2ccccn12 10.1021/acsmedchemlett.2c00099
CHEMBL1573515 50483 None 4 Human Binding pKd = 3.7 3.7 -1 4
Binding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assayBinding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assay
ChEMBL 251 3 1 4 2.3 O=c1cc(NCc2ccccc2)nc2ccccn12 10.1021/acsmedchemlett.2c00099
2823411 191580 None 5 Human Binding pKd = 4.7 4.7 4 4
Binding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assayBinding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assay
ChEMBL 253 3 1 4 2.2 O=C(NCc1ccccc1)c1ccc2nonc2c1 10.1021/acsmedchemlett.2c00099
CHEMBL5195119 191580 None 5 Human Binding pKd = 4.7 4.7 4 4
Binding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assayBinding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assay
ChEMBL 253 3 1 4 2.2 O=C(NCc1ccccc1)c1ccc2nonc2c1 10.1021/acsmedchemlett.2c00099
9857146 185188 None 1 Human Binding pKd = 6.6 6.6 2 4
Binding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assayBinding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assay
ChEMBL 289 2 0 3 4.2 Fc1ccc(-c2nn3ccccc3c2-c2ccncc2)cc1 10.1021/acsmedchemlett.2c00099
CHEMBL485745 185188 None 1 Human Binding pKd = 6.6 6.6 2 4
Binding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assayBinding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assay
ChEMBL 289 2 0 3 4.2 Fc1ccc(-c2nn3ccccc3c2-c2ccncc2)cc1 10.1021/acsmedchemlett.2c00099
135543624 16309 None 28 Human Binding pKd = 5.5 5.5 -16 4
Binding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assayBinding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assay
ChEMBL 348 4 3 7 2.8 N#Cc1c(N)nc(SCc2ncc[nH]2)c(C#N)c1-c1ccc(O)cc1 10.1021/acsmedchemlett.2c00099
CHEMBL122622 16309 None 28 Human Binding pKd = 5.5 5.5 -16 4
Binding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assayBinding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assay
ChEMBL 348 4 3 7 2.8 N#Cc1c(N)nc(SCc2ncc[nH]2)c(C#N)c1-c1ccc(O)cc1 10.1021/acsmedchemlett.2c00099
221427 35333 None 35 Human Binding pKd = 4.4 4.4 -1 4
Binding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assayBinding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assay
ChEMBL 213 2 2 2 2.7 O=C(Nc1ccccc1)Nc1ccccn1 10.1021/acsmedchemlett.2c00099
CHEMBL143703 35333 None 35 Human Binding pKd = 4.4 4.4 -1 4
Binding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assayBinding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assay
ChEMBL 213 2 2 2 2.7 O=C(Nc1ccccc1)Nc1ccccn1 10.1021/acsmedchemlett.2c00099
2794757 190888 None 46 Human Binding pKd = 4.4 4.4 -2 4
Binding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assayBinding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assay
ChEMBL 211 1 1 4 2.4 Nc1nsc(-c2ccc(Cl)cc2)n1 10.1021/acsmedchemlett.2c00099
CHEMBL5184937 190888 None 46 Human Binding pKd = 4.4 4.4 -2 4
Binding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assayBinding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assay
ChEMBL 211 1 1 4 2.4 Nc1nsc(-c2ccc(Cl)cc2)n1 10.1021/acsmedchemlett.2c00099
CHEMBL5080679 214701 None 0 Human Binding pKd = 7.3 7.3 -3 4
Binding affinity to NLuc human A2B adenosine receptor expressed in HEK293-A cells in presence of 1 uM PSB603 by NanoBRET binding assayBinding affinity to NLuc human A2B adenosine receptor expressed in HEK293-A cells in presence of 1 uM PSB603 by NanoBRET binding assay
ChEMBL None None None CCCn1c(=O)c2[nH]c(C34CC5CC(CC(C5)C3)C4)nc2n(CCCNC(=O)c2ccc(C(=O)NCCNC(=O)CCNC(=O)CCCCCNC(=O)COc3ccc(/C=C/C4=[N+]5C(=Cc6ccc(-c7cccs7)n6[B-]5(F)F)C=C4)cc3)cc2)c1=O 10.1021/acs.jmedchem.0c02067
44583036 186955 None 0 Human Binding pKd = 7.2 7.2 7 5
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 400 8 3 7 0.6 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)NCCO)cc3)cc2n(C)c1=O 10.1021/jm900413e
CHEMBL490262 186955 None 0 Human Binding pKd = 7.2 7.2 7 5
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 400 8 3 7 0.6 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)NCCO)cc3)cc2n(C)c1=O 10.1021/jm900413e
CHEMBL521280 186955 None 0 Human Binding pKd = 7.2 7.2 7 5
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 400 8 3 7 0.6 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)NCCO)cc3)cc2n(C)c1=O 10.1021/jm900413e
28561 181372 None 76 Human Binding pKd = 4.2 4.2 -1 4
Binding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assayBinding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assay
ChEMBL 177 1 1 4 1.8 Nc1nc(-c2ccccc2)ns1 10.1021/acsmedchemlett.2c00099
CHEMBL47633 181372 None 76 Human Binding pKd = 4.2 4.2 -1 4
Binding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assayBinding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assay
ChEMBL 177 1 1 4 1.8 Nc1nc(-c2ccccc2)ns1 10.1021/acsmedchemlett.2c00099
CHEMBL5075285 214366 None 0 Human Binding pKd = 8.1 8.1 -7 4
Binding affinity to NLuc human A2B adenosine receptor expressed in HEK293-A cells in presence of 1 uM PSB603 by NanoBRET binding assayBinding affinity to NLuc human A2B adenosine receptor expressed in HEK293-A cells in presence of 1 uM PSB603 by NanoBRET binding assay
ChEMBL None None None CCCn1c(=O)c2[nH]c(C34CCC(C(=O)NCCNC(=O)CCNC(=O)CCNC(=O)CCCCCNC(=O)COc5ccc(/C=C/C6=[N+]7C(=Cc8ccc(-c9cccs9)n8[B-]7(F)F)C=C6)cc5)(CC3)CC4)nc2n(CCC)c1=O 10.1021/acs.jmedchem.0c02067
17457984 191720 None 5 Human Binding pKd = 4.1 4.1 -2 4
Binding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assayBinding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assay
ChEMBL 284 4 1 5 2.5 CC(C)n1ncc2cc(C(=O)NCc3ccco3)cnc21 10.1021/acsmedchemlett.2c00099
CHEMBL5197070 191720 None 5 Human Binding pKd = 4.1 4.1 -2 4
Binding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assayBinding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as dissociation constant by surface plasmon resonance assay
ChEMBL 284 4 1 5 2.5 CC(C)n1ncc2cc(C(=O)NCc3ccco3)cnc21 10.1021/acsmedchemlett.2c00099
136 3292 None 32 Rat Binding pKd = 7.0 7.0 -57 15
Alpha-2 adrenergic receptor pA2 value against norepinephrine in vitro experiment in rat anococcygeus.Alpha-2 adrenergic receptor pA2 value against norepinephrine in vitro experiment in rat anococcygeus.
ChEMBL 354 1 2 4 2.6 COC(=O)[C@@H]1[C@@H](O)CC[C@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1021/jm00360a008
223 3292 None 32 Rat Binding pKd = 7.0 7.0 -57 15
Alpha-2 adrenergic receptor pA2 value against norepinephrine in vitro experiment in rat anococcygeus.Alpha-2 adrenergic receptor pA2 value against norepinephrine in vitro experiment in rat anococcygeus.
ChEMBL 354 1 2 4 2.6 COC(=O)[C@@H]1[C@@H](O)CC[C@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1021/jm00360a008
643606 3292 None 32 Rat Binding pKd = 7.0 7.0 -57 15
Alpha-2 adrenergic receptor pA2 value against norepinephrine in vitro experiment in rat anococcygeus.Alpha-2 adrenergic receptor pA2 value against norepinephrine in vitro experiment in rat anococcygeus.
ChEMBL 354 1 2 4 2.6 COC(=O)[C@@H]1[C@@H](O)CC[C@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1021/jm00360a008
CHEMBL10347 3292 None 32 Rat Binding pKd = 7.0 7.0 -57 15
Alpha-2 adrenergic receptor pA2 value against norepinephrine in vitro experiment in rat anococcygeus.Alpha-2 adrenergic receptor pA2 value against norepinephrine in vitro experiment in rat anococcygeus.
ChEMBL 354 1 2 4 2.6 COC(=O)[C@@H]1[C@@H](O)CC[C@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1021/jm00360a008
155555721 174393 None 7 Human Binding pKi = 10.1 10.1 1 2
Displacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 572 6 2 7 2.8 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(c5ccc(Br)cc5)CC4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
CHEMBL4552275 174393 None 7 Human Binding pKi = 10.1 10.1 1 2
Displacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 572 6 2 7 2.8 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(c5ccc(Br)cc5)CC4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
155555721 174393 None 7 Mouse Binding pKi = 9.9 9.9 -1 2
Displacement of [3H]PSB-603 from recombinant mouse A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant mouse A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 572 6 2 7 2.8 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(c5ccc(Br)cc5)CC4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
CHEMBL4552275 174393 None 7 Mouse Binding pKi = 9.9 9.9 -1 2
Displacement of [3H]PSB-603 from recombinant mouse A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant mouse A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 572 6 2 7 2.8 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(c5ccc(Br)cc5)CC4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
155521543 170610 None 0 Human Binding pKi = 9.9 9.9 645 2
Displacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 572 6 2 7 2.8 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(c5ccccc5Br)CC4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
CHEMBL4450864 170610 None 0 Human Binding pKi = 9.9 9.9 645 2
Displacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 572 6 2 7 2.8 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(c5ccccc5Br)CC4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
155530514 171548 None 0 Human Binding pKi = 9.8 9.8 6 5
Displacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 586 7 2 7 2.8 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5cccc(Br)c5)CC4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
CHEMBL4464522 171548 None 0 Human Binding pKi = 9.8 9.8 6 5
Displacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 586 7 2 7 2.8 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5cccc(Br)c5)CC4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
155550159 173903 None 0 Human Binding pKi = 9.8 9.8 501 2
Displacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 586 7 2 7 2.8 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc(Br)cc5)CC4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
CHEMBL4540206 173903 None 0 Human Binding pKi = 9.8 9.8 501 2
Displacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 586 7 2 7 2.8 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc(Br)cc5)CC4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
44186666 185658 None 0 Human Binding pKi = 9.8 9.8 144 5
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 562 6 2 7 2.6 CCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc(C(F)(F)F)cc5)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
CHEMBL486478 185658 None 0 Human Binding pKi = 9.8 9.8 144 5
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 562 6 2 7 2.6 CCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc(C(F)(F)F)cc5)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
155524032 170890 None 0 Human Binding pKi = 9.8 9.8 19054 2
Displacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 620 6 2 7 2.6 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(c5ccc(I)cc5)CC4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
CHEMBL4454481 170890 None 0 Human Binding pKi = 9.8 9.8 19054 2
Displacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 620 6 2 7 2.6 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(c5ccc(I)cc5)CC4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
76328910 105521 None 0 Human Binding pKi = 9.8 9.8 -1 4
Binding affinity to human recombinant adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated adenylyl cyclase activity after 20 minsBinding affinity to human recombinant adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated adenylyl cyclase activity after 20 mins
ChEMBL 522 8 1 8 2.9 Cn1c(=O)c2[nH]c(-c3ccc(OCCCN4CCN(Cc5ccccc5Cl)CC4)cc3)nc2n(C)c1=O 10.1016/j.ejmech.2014.01.045
CHEMBL3121728 105521 None 0 Human Binding pKi = 9.8 9.8 -1 4
Binding affinity to human recombinant adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated adenylyl cyclase activity after 20 minsBinding affinity to human recombinant adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated adenylyl cyclase activity after 20 mins
ChEMBL 522 8 1 8 2.9 Cn1c(=O)c2[nH]c(-c3ccc(OCCCN4CCN(Cc5ccccc5Cl)CC4)cc3)nc2n(C)c1=O 10.1016/j.ejmech.2014.01.045
145977111 163765 None 0 Rat Binding pKi = 9.7 9.7 7 4
Displacement of [3H]PSB-603 from recombinant rat adenosine A2B receptor expressed in CHO cell membranes after 75 mins by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant rat adenosine A2B receptor expressed in CHO cell membranes after 75 mins by liquid scintillation counting method
ChEMBL 617 9 3 7 3.9 CCCn1c(=O)[nH]c2nc(-c3ccc(OCC(=O)NCCC4=C5C(C)=CC(C)=[N+]5[B-](F)(F)n5c(C)cc(C)c54)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.7b01627
CHEMBL4205635 163765 None 0 Rat Binding pKi = 9.7 9.7 7 4
Displacement of [3H]PSB-603 from recombinant rat adenosine A2B receptor expressed in CHO cell membranes after 75 mins by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant rat adenosine A2B receptor expressed in CHO cell membranes after 75 mins by liquid scintillation counting method
ChEMBL 617 9 3 7 3.9 CCCn1c(=O)[nH]c2nc(-c3ccc(OCC(=O)NCCC4=C5C(C)=CC(C)=[N+]5[B-](F)(F)n5c(C)cc(C)c54)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.7b01627
44186580 184206 None 0 Human Binding pKi = 9.7 9.7 30 6
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 528 6 2 7 2.3 CCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc(Cl)cc5)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
CHEMBL483261 184206 None 0 Human Binding pKi = 9.7 9.7 30 6
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 528 6 2 7 2.3 CCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc(Cl)cc5)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
155529872 171506 None 0 Human Binding pKi = 9.7 9.7 165 3
Displacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 558 7 2 8 2.7 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(c5ccc(Cl)c(OC)c5)CC4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
CHEMBL4463929 171506 None 0 Human Binding pKi = 9.7 9.7 165 3
Displacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 558 7 2 8 2.7 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(c5ccc(Cl)c(OC)c5)CC4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
155532274 171697 None 0 Human Binding pKi = 9.6 9.6 - 1
Displacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 572 6 2 7 2.8 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(c5cccc(Br)c5)CC4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
CHEMBL4466625 171697 None 0 Human Binding pKi = 9.6 9.6 - 1
Displacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 572 6 2 7 2.8 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(c5cccc(Br)c5)CC4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
155560510 175048 None 0 Human Binding pKi = 9.6 9.6 851 3
Displacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 549 8 2 8 2.9 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc(N=[N+]=[N-])cc5)CC4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
CHEMBL4567785 175048 None 0 Human Binding pKi = 9.6 9.6 851 3
Displacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 549 8 2 8 2.9 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc(N=[N+]=[N-])cc5)CC4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
44186668 191510 None 0 Human Binding pKi = 9.6 9.6 245 6
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 562 6 2 7 2.6 CCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5cccc(C(F)(F)F)c5)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
CHEMBL519390 191510 None 0 Human Binding pKi = 9.6 9.6 245 6
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 562 6 2 7 2.6 CCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5cccc(C(F)(F)F)c5)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
44186667 185659 None 0 Human Binding pKi = 9.5 9.5 478 6
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 576 7 2 7 3.0 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc(C(F)(F)F)cc5)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
CHEMBL486479 185659 None 0 Human Binding pKi = 9.5 9.5 478 6
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 576 7 2 7 3.0 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc(C(F)(F)F)cc5)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
155528136 171257 None 0 Human Binding pKi = 9.5 9.5 158 3
Displacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 528 6 2 7 2.7 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(c5cccc(Cl)c5)CC4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
CHEMBL4460114 171257 None 0 Human Binding pKi = 9.5 9.5 158 3
Displacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 528 6 2 7 2.7 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(c5cccc(Cl)c5)CC4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
155545762 173479 None 0 Human Binding pKi = 9.5 9.5 - 1
Displacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 558 7 2 8 2.7 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(c5ccc(OC)c(Cl)c5)CC4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
CHEMBL4530074 173479 None 0 Human Binding pKi = 9.5 9.5 - 1
Displacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 558 7 2 8 2.7 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(c5ccc(OC)c(Cl)c5)CC4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
44186581 3205 None 27 Human Binding pKi = 9.4 9.4 851 6
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 542 7 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)Cc1ccc(cc1)Cl 10.1021/jm900413e
6561 3205 None 27 Human Binding pKi = 9.4 9.4 851 6
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 542 7 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)Cc1ccc(cc1)Cl 10.1021/jm900413e
CHEMBL482436 3205 None 27 Human Binding pKi = 9.4 9.4 851 6
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 542 7 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)Cc1ccc(cc1)Cl 10.1021/jm900413e
155514860 169881 None 0 Human Binding pKi = 9.4 9.4 478 3
Displacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 522 7 2 7 2.3 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5cccc(C)c5)CC4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
CHEMBL4440526 169881 None 0 Human Binding pKi = 9.4 9.4 478 3
Displacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 522 7 2 7 2.3 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5cccc(C)c5)CC4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
450 2970 None 9 Human Binding pKi = 9.4 9.4 257 4
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 525 10 3 6 3.6 CC(=O)NCCNc1nc(nc2c1cc([nH]2)C(=O)N1CCN(CC1)CCCc1ccccc1)c1ccccc1 10.1021/jm201292w
454 2970 None 9 Human Binding pKi = 9.4 9.4 257 4
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 525 10 3 6 3.6 CC(=O)NCCNc1nc(nc2c1cc([nH]2)C(=O)N1CCN(CC1)CCCc1ccccc1)c1ccccc1 10.1021/jm201292w
5311041 2970 None 9 Human Binding pKi = 9.4 9.4 257 4
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 525 10 3 6 3.6 CC(=O)NCCNc1nc(nc2c1cc([nH]2)C(=O)N1CCN(CC1)CCCc1ccccc1)c1ccccc1 10.1021/jm201292w
CHEMBL485862 2970 None 9 Human Binding pKi = 9.4 9.4 257 4
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 525 10 3 6 3.6 CC(=O)NCCNc1nc(nc2c1cc([nH]2)C(=O)N1CCN(CC1)CCCc1ccccc1)c1ccccc1 10.1021/jm201292w
155514957 169927 None 0 Human Binding pKi = 9.4 9.4 501 2
Displacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 528 6 2 7 2.7 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(c5ccccc5Cl)CC4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
CHEMBL4441276 169927 None 0 Human Binding pKi = 9.4 9.4 501 2
Displacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 528 6 2 7 2.7 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(c5ccccc5Cl)CC4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
44185870 184230 None 0 Human Binding pKi = 9.4 9.4 117 5
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 514 5 2 7 2.3 CCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(c5ccc(Cl)cc5)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
CHEMBL483487 184230 None 0 Human Binding pKi = 9.4 9.4 117 5
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 514 5 2 7 2.3 CCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(c5ccc(Cl)cc5)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
450 2970 None 9 Human Binding pKi = 9.4 9.4 257 4
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 525 10 3 6 3.6 CC(=O)NCCNc1nc(nc2c1cc([nH]2)C(=O)N1CCN(CC1)CCCc1ccccc1)c1ccccc1 10.1021/jm900413e
454 2970 None 9 Human Binding pKi = 9.4 9.4 257 4
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 525 10 3 6 3.6 CC(=O)NCCNc1nc(nc2c1cc([nH]2)C(=O)N1CCN(CC1)CCCc1ccccc1)c1ccccc1 10.1021/jm900413e
5311041 2970 None 9 Human Binding pKi = 9.4 9.4 257 4
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 525 10 3 6 3.6 CC(=O)NCCNc1nc(nc2c1cc([nH]2)C(=O)N1CCN(CC1)CCCc1ccccc1)c1ccccc1 10.1021/jm900413e
CHEMBL485862 2970 None 9 Human Binding pKi = 9.4 9.4 257 4
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 525 10 3 6 3.6 CC(=O)NCCNc1nc(nc2c1cc([nH]2)C(=O)N1CCN(CC1)CCCc1ccccc1)c1ccccc1 10.1021/jm900413e
155523968 170887 None 0 Human Binding pKi = 9.4 9.4 97 3
Displacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 544 6 3 8 2.4 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(c5ccc(Cl)c(O)c5)CC4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
CHEMBL4454417 170887 None 0 Human Binding pKi = 9.4 9.4 97 3
Displacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 544 6 3 8 2.4 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(c5ccc(Cl)c(O)c5)CC4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
155516277 170064 None 0 Human Binding pKi = 9.4 9.4 331 3
Displacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 508 6 2 7 2.3 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(c5ccccc5C)CC4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
CHEMBL4443090 170064 None 0 Human Binding pKi = 9.4 9.4 331 3
Displacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 508 6 2 7 2.3 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(c5ccccc5C)CC4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
44186626 184609 None 0 Human Binding pKi = 9.4 9.4 245 6
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 526 7 2 7 2.1 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5cccc(F)c5)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
CHEMBL484900 184609 None 0 Human Binding pKi = 9.4 9.4 245 6
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 526 7 2 7 2.1 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5cccc(F)c5)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
44185872 191398 None 0 Human Binding pKi = 9.3 9.3 416 4
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 524 5 2 7 1.9 C#CCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(c5ccc(Cl)cc5)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
CHEMBL519253 191398 None 0 Human Binding pKi = 9.3 9.3 416 4
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 524 5 2 7 1.9 C#CCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(c5ccc(Cl)cc5)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
155561141 174974 None 0 Human Binding pKi = 9.3 9.3 676 3
Displacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 604 7 2 7 2.9 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc(Br)c(F)c5)CC4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
CHEMBL4566170 174974 None 0 Human Binding pKi = 9.3 9.3 676 3
Displacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 604 7 2 7 2.9 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc(Br)c(F)c5)CC4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
450 2970 None 9 Human Binding pKi = 9.3 9.3 257 4
Antagonist activity at human A2B receptorAntagonist activity at human A2B receptor
ChEMBL 525 10 3 6 3.6 CC(=O)NCCNc1nc(nc2c1cc([nH]2)C(=O)N1CCN(CC1)CCCc1ccccc1)c1ccccc1 10.1021/acs.jmedchem.0c01431
454 2970 None 9 Human Binding pKi = 9.3 9.3 257 4
Antagonist activity at human A2B receptorAntagonist activity at human A2B receptor
ChEMBL 525 10 3 6 3.6 CC(=O)NCCNc1nc(nc2c1cc([nH]2)C(=O)N1CCN(CC1)CCCc1ccccc1)c1ccccc1 10.1021/acs.jmedchem.0c01431
5311041 2970 None 9 Human Binding pKi = 9.3 9.3 257 4
Antagonist activity at human A2B receptorAntagonist activity at human A2B receptor
ChEMBL 525 10 3 6 3.6 CC(=O)NCCNc1nc(nc2c1cc([nH]2)C(=O)N1CCN(CC1)CCCc1ccccc1)c1ccccc1 10.1021/acs.jmedchem.0c01431
CHEMBL485862 2970 None 9 Human Binding pKi = 9.3 9.3 257 4
Antagonist activity at human A2B receptorAntagonist activity at human A2B receptor
ChEMBL 525 10 3 6 3.6 CC(=O)NCCNc1nc(nc2c1cc([nH]2)C(=O)N1CCN(CC1)CCCc1ccccc1)c1ccccc1 10.1021/acs.jmedchem.0c01431
450 2970 None 9 Human Binding pKi = 9.3 9.3 257 4
Binding affinity to human recombinant A2B receptor expressed in HEK293 cell membranesBinding affinity to human recombinant A2B receptor expressed in HEK293 cell membranes
ChEMBL 525 10 3 6 3.6 CC(=O)NCCNc1nc(nc2c1cc([nH]2)C(=O)N1CCN(CC1)CCCc1ccccc1)c1ccccc1 10.1021/acs.jmedchem.9b01340
454 2970 None 9 Human Binding pKi = 9.3 9.3 257 4
Binding affinity to human recombinant A2B receptor expressed in HEK293 cell membranesBinding affinity to human recombinant A2B receptor expressed in HEK293 cell membranes
ChEMBL 525 10 3 6 3.6 CC(=O)NCCNc1nc(nc2c1cc([nH]2)C(=O)N1CCN(CC1)CCCc1ccccc1)c1ccccc1 10.1021/acs.jmedchem.9b01340
5311041 2970 None 9 Human Binding pKi = 9.3 9.3 257 4
Binding affinity to human recombinant A2B receptor expressed in HEK293 cell membranesBinding affinity to human recombinant A2B receptor expressed in HEK293 cell membranes
ChEMBL 525 10 3 6 3.6 CC(=O)NCCNc1nc(nc2c1cc([nH]2)C(=O)N1CCN(CC1)CCCc1ccccc1)c1ccccc1 10.1021/acs.jmedchem.9b01340
CHEMBL485862 2970 None 9 Human Binding pKi = 9.3 9.3 257 4
Binding affinity to human recombinant A2B receptor expressed in HEK293 cell membranesBinding affinity to human recombinant A2B receptor expressed in HEK293 cell membranes
ChEMBL 525 10 3 6 3.6 CC(=O)NCCNc1nc(nc2c1cc([nH]2)C(=O)N1CCN(CC1)CCCc1ccccc1)c1ccccc1 10.1021/acs.jmedchem.9b01340
127033645 139120 None 0 Human Binding pKi = 9.3 9.3 - 1
Displacement of [3H]OSIP339391 from human recombinant Adenosine A2B receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]OSIP339391 from human recombinant Adenosine A2B receptor expressed in HEK293 cells after 60 mins
ChEMBL 526 10 3 7 3.0 CC(=O)NCCNc1nc(-c2ccccc2)nc2nc(C(=O)N3CCN(CCCc4ccccc4)CC3)[nH]c12 10.1021/acs.jmedchem.5b01586
CHEMBL3786849 139120 None 0 Human Binding pKi = 9.3 9.3 - 1
Displacement of [3H]OSIP339391 from human recombinant Adenosine A2B receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]OSIP339391 from human recombinant Adenosine A2B receptor expressed in HEK293 cells after 60 mins
ChEMBL 526 10 3 7 3.0 CC(=O)NCCNc1nc(-c2ccccc2)nc2nc(C(=O)N3CCN(CCCc4ccccc4)CC3)[nH]c12 10.1021/acs.jmedchem.5b01586
127033645 139120 None 0 Human Binding pKi = 9.3 9.3 - 1
Displacement of [3H]OSIP339391 from human recombinant adenosine A2B receptor expressed in HEK293 cell membranes after 60 mins by liquid scintillation counting methodDisplacement of [3H]OSIP339391 from human recombinant adenosine A2B receptor expressed in HEK293 cell membranes after 60 mins by liquid scintillation counting method
ChEMBL 526 10 3 7 3.0 CC(=O)NCCNc1nc(-c2ccccc2)nc2nc(C(=O)N3CCN(CCCc4ccccc4)CC3)[nH]c12 10.1021/acs.jmedchem.7b00138
CHEMBL3786849 139120 None 0 Human Binding pKi = 9.3 9.3 - 1
Displacement of [3H]OSIP339391 from human recombinant adenosine A2B receptor expressed in HEK293 cell membranes after 60 mins by liquid scintillation counting methodDisplacement of [3H]OSIP339391 from human recombinant adenosine A2B receptor expressed in HEK293 cell membranes after 60 mins by liquid scintillation counting method
ChEMBL 526 10 3 7 3.0 CC(=O)NCCNc1nc(-c2ccccc2)nc2nc(C(=O)N3CCN(CCCc4ccccc4)CC3)[nH]c12 10.1021/acs.jmedchem.7b00138
3284 3216 None 35 Human Binding pKi = 9.3 9.3 -1 7
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 528 6 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)c1ccc(cc1)Cl 10.1021/jm900413e
44185871 3216 None 35 Human Binding pKi = 9.3 9.3 -1 7
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 528 6 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)c1ccc(cc1)Cl 10.1021/jm900413e
5728 3216 None 35 Human Binding pKi = 9.3 9.3 -1 7
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 528 6 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)c1ccc(cc1)Cl 10.1021/jm900413e
CHEMBL483688 3216 None 35 Human Binding pKi = 9.3 9.3 -1 7
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 528 6 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)c1ccc(cc1)Cl 10.1021/jm900413e
44186624 192436 None 0 Human Binding pKi = 9.2 9.2 57 4
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 526 7 2 7 2.1 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc(F)cc5)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
CHEMBL520830 192436 None 0 Human Binding pKi = 9.2 9.2 57 4
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 526 7 2 7 2.1 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc(F)cc5)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
53324032 58029 None 0 Human Binding pKi = 9.2 9.2 165 3
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 352 4 1 4 3.8 O=C(Nc1cnc(-c2ccncc2F)c(-c2ccccc2F)n1)C1CC1 10.1021/ml100249e
CHEMBL1672631 58029 None 0 Human Binding pKi = 9.2 9.2 165 3
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 352 4 1 4 3.8 O=C(Nc1cnc(-c2ccncc2F)c(-c2ccccc2F)n1)C1CC1 10.1021/ml100249e
44186582 184113 None 0 Human Binding pKi = 9.2 9.2 158 4
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 528 6 2 7 2.3 CCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5cccc(Cl)c5)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
CHEMBL482638 184113 None 0 Human Binding pKi = 9.2 9.2 158 4
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 528 6 2 7 2.3 CCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5cccc(Cl)c5)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
155525050 170979 None 0 Human Binding pKi = 9.2 9.2 316 2
Displacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 524 7 2 8 2.0 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(c5cccc(OC)c5)CC4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
CHEMBL4456096 170979 None 0 Human Binding pKi = 9.2 9.2 316 2
Displacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 524 7 2 8 2.0 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(c5cccc(OC)c5)CC4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
155530257 171522 None 0 Human Binding pKi = 9.2 9.2 213 2
Displacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 556 8 2 8 2.1 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc(F)c(OC)c5)CC4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
CHEMBL4464175 171522 None 0 Human Binding pKi = 9.2 9.2 213 2
Displacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 556 8 2 8 2.1 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc(F)c(OC)c5)CC4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
155531990 171708 None 0 Human Binding pKi = 9.2 9.2 1 2
Displacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 512 6 2 7 2.1 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(c5cccc(F)c5)CC4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
CHEMBL4466765 171708 None 0 Human Binding pKi = 9.2 9.2 1 2
Displacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 512 6 2 7 2.1 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(c5cccc(F)c5)CC4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
155564465 175257 None 0 Human Binding pKi = 9.2 9.2 190 3
Displacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 494 6 2 7 2.0 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(c5ccccc5)CC4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
CHEMBL4572369 175257 None 0 Human Binding pKi = 9.2 9.2 190 3
Displacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 494 6 2 7 2.0 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(c5ccccc5)CC4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
155534836 171997 None 0 Human Binding pKi = 9.2 9.2 165 2
Displacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 512 6 2 7 2.1 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(c5ccc(F)cc5)CC4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
CHEMBL4471205 171997 None 0 Human Binding pKi = 9.2 9.2 165 2
Displacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 512 6 2 7 2.1 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(c5ccc(F)cc5)CC4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
168297247 192377 None 0 Human Binding pKi = 9.2 9.2 - 1
Displacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cell membrane preincubated for 4 hrs followed by [3H]PSB-603 addition and measured after 0.5 hrs by radioligand displacement assayDisplacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cell membrane preincubated for 4 hrs followed by [3H]PSB-603 addition and measured after 0.5 hrs by radioligand displacement assay
ChEMBL 327 4 2 6 2.2 CCCn1c(=O)[nH]c2nc(-c3ccc(N=C=S)cc3)[nH]c2c1=O 10.1039/d2md00132b
CHEMBL5207498 192377 None 0 Human Binding pKi = 9.2 9.2 - 1
Displacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cell membrane preincubated for 4 hrs followed by [3H]PSB-603 addition and measured after 0.5 hrs by radioligand displacement assayDisplacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cell membrane preincubated for 4 hrs followed by [3H]PSB-603 addition and measured after 0.5 hrs by radioligand displacement assay
ChEMBL 327 4 2 6 2.2 CCCn1c(=O)[nH]c2nc(-c3ccc(N=C=S)cc3)[nH]c2c1=O 10.1039/d2md00132b
168296088 192366 None 1 Human Binding pKi = 9.2 9.2 - 1
Displacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cell membrane preincubated for 4 hrs followed by [3H]PSB-603 addition and measured after 0.5 hrs by radioligand displacement assayDisplacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cell membrane preincubated for 4 hrs followed by [3H]PSB-603 addition and measured after 0.5 hrs by radioligand displacement assay
ChEMBL 352 4 2 6 1.1 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)F)cc3)[nH]c2c1=O 10.1039/d2md00132b
CHEMBL5207290 192366 None 1 Human Binding pKi = 9.2 9.2 - 1
Displacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cell membrane preincubated for 4 hrs followed by [3H]PSB-603 addition and measured after 0.5 hrs by radioligand displacement assayDisplacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cell membrane preincubated for 4 hrs followed by [3H]PSB-603 addition and measured after 0.5 hrs by radioligand displacement assay
ChEMBL 352 4 2 6 1.1 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)F)cc3)[nH]c2c1=O 10.1039/d2md00132b
44186625 184608 None 0 Human Binding pKi = 9.2 9.2 208 6
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 512 6 2 7 1.7 CCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5cccc(F)c5)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
CHEMBL484899 184608 None 0 Human Binding pKi = 9.2 9.2 208 6
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 512 6 2 7 1.7 CCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5cccc(F)c5)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
155530381 171564 None 0 Human Binding pKi = 9.2 9.2 - 1
Displacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 508 6 2 7 2.3 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(c5ccc(C)cc5)CC4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
CHEMBL4464738 171564 None 0 Human Binding pKi = 9.2 9.2 - 1
Displacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 508 6 2 7 2.3 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(c5ccc(C)cc5)CC4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
44186669 185797 None 0 Human Binding pKi = 9.1 9.1 354 6
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 576 7 2 7 3.0 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5cccc(C(F)(F)F)c5)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
CHEMBL486688 185797 None 0 Human Binding pKi = 9.1 9.1 354 6
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 576 7 2 7 3.0 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5cccc(C(F)(F)F)c5)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
44186622 184229 None 0 Human Binding pKi = 9.1 9.1 208 6
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 542 7 2 7 2.7 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5cccc(Cl)c5)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
CHEMBL483469 184229 None 0 Human Binding pKi = 9.1 9.1 208 6
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 542 7 2 7 2.7 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5cccc(Cl)c5)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
44574165 189467 None 0 Human Binding pKi = 9.1 9.1 2 6
Displacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells by beta scintillation counterDisplacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells by beta scintillation counter
ChEMBL 410 4 2 7 3.0 Cn1c(=O)c2[nH]c(-c3ccc(COC(=O)Nc4ccsc4)cc3)cc2n(C)c1=O 10.1016/j.bmc.2009.03.062
CHEMBL513681 189467 None 0 Human Binding pKi = 9.1 9.1 2 6
Displacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells by beta scintillation counterDisplacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells by beta scintillation counter
ChEMBL 410 4 2 7 3.0 Cn1c(=O)c2[nH]c(-c3ccc(COC(=O)Nc4ccsc4)cc3)cc2n(C)c1=O 10.1016/j.bmc.2009.03.062
44186715 191219 None 0 Human Binding pKi = 9.1 9.1 54 4
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 522 7 2 7 2.3 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc(C)cc5)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
CHEMBL518972 191219 None 0 Human Binding pKi = 9.1 9.1 54 4
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 522 7 2 7 2.3 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc(C)cc5)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
44186718 184173 None 0 Human Binding pKi = 9.1 9.1 117 6
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 538 6 2 9 1.3 CCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc6c(c5)OCO6)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
CHEMBL483065 184173 None 0 Human Binding pKi = 9.1 9.1 117 6
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 538 6 2 9 1.3 CCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc6c(c5)OCO6)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
155522541 170811 None 0 Human Binding pKi = 9.1 9.1 275 2
Displacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 556 8 2 8 2.1 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc(OC)c(F)c5)CC4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
CHEMBL4453324 170811 None 0 Human Binding pKi = 9.1 9.1 275 2
Displacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 556 8 2 8 2.1 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc(OC)c(F)c5)CC4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
44236421 156571 None 0 Human Binding pKi = 9.1 9.1 - 1
Displacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting methodDisplacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting method
ChEMBL 572 8 1 9 2.9 CCCn1c(=O)c2[nH]c(-c3cnn(CC(=O)N4CCN(c5ccc(C(F)(F)F)cc5)CC4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2016.11.007
CHEMBL4068507 156571 None 0 Human Binding pKi = 9.1 9.1 - 1
Displacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting methodDisplacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting method
ChEMBL 572 8 1 9 2.9 CCCn1c(=O)c2[nH]c(-c3cnn(CC(=O)N4CCN(c5ccc(C(F)(F)F)cc5)CC4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2016.11.007
155530514 171548 None 0 Mouse Binding pKi = 9.0 9.0 -6 5
Displacement of [3H]PSB-603 from recombinant mouse A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant mouse A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 586 7 2 7 2.8 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5cccc(Br)c5)CC4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
CHEMBL4464522 171548 None 0 Mouse Binding pKi = 9.0 9.0 -6 5
Displacement of [3H]PSB-603 from recombinant mouse A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant mouse A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 586 7 2 7 2.8 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5cccc(Br)c5)CC4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
155531990 171708 None 0 Mouse Binding pKi = 9.0 9.0 -1 2
Displacement of [3H]PSB-603 from recombinant mouse A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant mouse A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 512 6 2 7 2.1 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(c5cccc(F)c5)CC4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
CHEMBL4466765 171708 None 0 Mouse Binding pKi = 9.0 9.0 -1 2
Displacement of [3H]PSB-603 from recombinant mouse A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant mouse A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 512 6 2 7 2.1 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(c5cccc(F)c5)CC4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
44186717 184145 None 0 Human Binding pKi = 9.0 9.0 89 6
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 538 8 2 8 2.0 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc(OC)cc5)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
CHEMBL482855 184145 None 0 Human Binding pKi = 9.0 9.0 89 6
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 538 8 2 8 2.0 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc(OC)cc5)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
76336198 105519 None 0 Human Binding pKi = 9 9.0 -13 2
Binding affinity to human recombinant adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated adenylyl cyclase activity after 20 minsBinding affinity to human recombinant adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated adenylyl cyclase activity after 20 mins
ChEMBL 340 3 1 6 1.9 Cn1c(=O)c2[nH]c(-c3ccc(OC4CCCC4)cc3)nc2n(C)c1=O 10.1016/j.ejmech.2014.01.045
CHEMBL3121726 105519 None 0 Human Binding pKi = 9 9.0 -13 2
Binding affinity to human recombinant adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated adenylyl cyclase activity after 20 minsBinding affinity to human recombinant adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated adenylyl cyclase activity after 20 mins
ChEMBL 340 3 1 6 1.9 Cn1c(=O)c2[nH]c(-c3ccc(OC4CCCC4)cc3)nc2n(C)c1=O 10.1016/j.ejmech.2014.01.045
135543624 16309 None 28 Human Binding pKi = 9 9.0 -16 4
Binding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as inhibition constant by surface plasmon resonance assayBinding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as inhibition constant by surface plasmon resonance assay
ChEMBL 348 4 3 7 2.8 N#Cc1c(N)nc(SCc2ncc[nH]2)c(C#N)c1-c1ccc(O)cc1 10.1021/acsmedchemlett.2c00099
CHEMBL122622 16309 None 28 Human Binding pKi = 9 9.0 -16 4
Binding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as inhibition constant by surface plasmon resonance assayBinding affinity to human wild type adenosine A2B receptor expressed in Expi293F cells assessed as inhibition constant by surface plasmon resonance assay
ChEMBL 348 4 3 7 2.8 N#Cc1c(N)nc(SCc2ncc[nH]2)c(C#N)c1-c1ccc(O)cc1 10.1021/acsmedchemlett.2c00099
66894241 157813 None 0 Human Binding pKi = 9 9.0 114 3
Displacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting methodDisplacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting method
ChEMBL 543 8 1 8 3.6 CCCn1c(=O)c2[nH]c(-c3cnn(CC4CC(=O)N(c5ccc(C(F)(F)F)cc5)C4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2016.11.007
CHEMBL4083317 157813 None 0 Human Binding pKi = 9 9.0 114 3
Displacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting methodDisplacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting method
ChEMBL 543 8 1 8 3.6 CCCn1c(=O)c2[nH]c(-c3cnn(CC4CC(=O)N(c5ccc(C(F)(F)F)cc5)C4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2016.11.007
66899873 158934 None 0 Human Binding pKi = 9 9.0 - 1
Displacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting methodDisplacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting method
ChEMBL 569 9 1 7 4.8 CCCn1c(=O)c2[nH]c(-c3ccc(OCC4CC(=O)N(c5ccc(C(F)(F)F)cc5)C4)cc3)nc2n(CCC)c1=O 10.1016/j.ejmech.2016.11.007
CHEMBL4095766 158934 None 0 Human Binding pKi = 9 9.0 - 1
Displacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting methodDisplacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting method
ChEMBL 569 9 1 7 4.8 CCCn1c(=O)c2[nH]c(-c3ccc(OCC4CC(=O)N(c5ccc(C(F)(F)F)cc5)C4)cc3)nc2n(CCC)c1=O 10.1016/j.ejmech.2016.11.007
44451166 95965 None 0 Human Binding pKi = 9 9.0 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 620 7 1 9 4.9 CCCn1c(=O)n(C)c(=O)c2[nH]c(-c3ccc(OC(C)(C)C(=O)N4CCN(c5nc6ccc(Cl)cc6s5)CC4)cc3)cc21 10.1016/j.bmc.2008.01.002
CHEMBL259479 95965 None 0 Human Binding pKi = 9 9.0 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 620 7 1 9 4.9 CCCn1c(=O)n(C)c(=O)c2[nH]c(-c3ccc(OC(C)(C)C(=O)N4CCN(c5nc6ccc(Cl)cc6s5)CC4)cc3)cc21 10.1016/j.bmc.2008.01.002
46866593 5940 None 0 Human Binding pKi = 9 9.0 151 3
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 323 4 1 4 3.9 O=C(Nc1ccc(-c2ccncc2F)c(-c2ccco2)n1)C1CC1 10.1016/j.bmcl.2010.01.045
CHEMBL1079804 5940 None 0 Human Binding pKi = 9 9.0 151 3
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 323 4 1 4 3.9 O=C(Nc1ccc(-c2ccncc2F)c(-c2ccco2)n1)C1CC1 10.1016/j.bmcl.2010.01.045
46880424 6051 None 0 Human Binding pKi = 9 9.0 181 4
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 307 2 2 6 1.3 O=c1[nH]c(=O)c2cc(-c3ccncn3)c(-c3ccco3)nc2[nH]1 10.1016/j.bmcl.2010.01.077
CHEMBL1080513 6051 None 0 Human Binding pKi = 9 9.0 181 4
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 307 2 2 6 1.3 O=c1[nH]c(=O)c2cc(-c3ccncn3)c(-c3ccco3)nc2[nH]1 10.1016/j.bmcl.2010.01.077
46866591 6306 None 0 Human Binding pKi = 9 9.0 30 4
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 305 4 1 4 3.8 O=C(Nc1ccc(-c2ccncc2)c(-c2ccco2)n1)C1CC1 10.1016/j.bmcl.2010.01.045
CHEMBL1081812 6306 None 0 Human Binding pKi = 9 9.0 30 4
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 305 4 1 4 3.8 O=C(Nc1ccc(-c2ccncc2)c(-c2ccco2)n1)C1CC1 10.1016/j.bmcl.2010.01.045
16071901 58021 None 0 Human Binding pKi = 9 9.0 25 4
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 334 4 1 4 3.7 O=C(Nc1cnc(-c2ccncc2)c(-c2ccccc2F)n1)C1CC1 10.1021/ml100249e
CHEMBL1672623 58021 None 0 Human Binding pKi = 9 9.0 25 4
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 334 4 1 4 3.7 O=C(Nc1cnc(-c2ccncc2)c(-c2ccccc2F)n1)C1CC1 10.1021/ml100249e
44587956 174772 None 0 Human Binding pKi = 9 9.0 -2 6
Displacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cells
ChEMBL 554 9 3 7 4.5 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(Br)cc4)cc3)c(O)c2n(CCC)c1=O 10.1016/j.bmc.2008.09.067
CHEMBL456125 174772 None 0 Human Binding pKi = 9 9.0 -2 6
Displacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cells
ChEMBL 554 9 3 7 4.5 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(Br)cc4)cc3)c(O)c2n(CCC)c1=O 10.1016/j.bmc.2008.09.067
11705261 72991 None 0 Human Binding pKi = 9 9.0 371 4
Displacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cellsDisplacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cells
ChEMBL 460 8 1 10 2.7 CCCn1c(=O)c2nc(-c3cnn(Cc4nc(-c5ccccc5)no4)c3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2005.10.002
CHEMBL200779 72991 None 0 Human Binding pKi = 9 9.0 371 4
Displacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cellsDisplacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cells
ChEMBL 460 8 1 10 2.7 CCCn1c(=O)c2nc(-c3cnn(Cc4nc(-c5ccccc5)no4)c3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2005.10.002
9822488 77625 None 0 Human Binding pKi = 9 9.0 691 4
Displacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 404 3 1 7 1.9 Cn1c(=O)c2nc(-c3cnn(Cc4cccc(C(F)(F)F)c4)c3)[nH]c2n(C)c1=O 10.1021/jm7014815
CHEMBL208824 77625 None 0 Human Binding pKi = 9 9.0 691 4
Displacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 404 3 1 7 1.9 Cn1c(=O)c2nc(-c3cnn(Cc4cccc(C(F)(F)F)c4)c3)[nH]c2n(C)c1=O 10.1021/jm7014815
9822488 77625 None 0 Human Binding pKi = 9 9.0 691 4
Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cellsDisplacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells
ChEMBL 404 3 1 7 1.9 Cn1c(=O)c2nc(-c3cnn(Cc4cccc(C(F)(F)F)c4)c3)[nH]c2n(C)c1=O 10.1021/jm051268+
CHEMBL208824 77625 None 0 Human Binding pKi = 9 9.0 691 4
Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cellsDisplacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells
ChEMBL 404 3 1 7 1.9 Cn1c(=O)c2nc(-c3cnn(Cc4cccc(C(F)(F)F)c4)c3)[nH]c2n(C)c1=O 10.1021/jm051268+
155532514 171767 None 0 Human Binding pKi = 9.0 9.0 154 2
Displacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 556 8 2 8 2.1 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5cc(F)cc(OC)c5)CC4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
CHEMBL4467573 171767 None 0 Human Binding pKi = 9.0 9.0 154 2
Displacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 556 8 2 8 2.1 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5cc(F)cc(OC)c5)CC4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
44451166 95965 None 0 Human Binding pKi = 9.0 9.0 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 620 7 1 9 4.9 CCCn1c(=O)n(C)c(=O)c2[nH]c(-c3ccc(OC(C)(C)C(=O)N4CCN(c5nc6ccc(Cl)cc6s5)CC4)cc3)cc21 10.1016/j.bmc.2008.01.002
CHEMBL259479 95965 None 0 Human Binding pKi = 9.0 9.0 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 620 7 1 9 4.9 CCCn1c(=O)n(C)c(=O)c2[nH]c(-c3ccc(OC(C)(C)C(=O)N4CCN(c5nc6ccc(Cl)cc6s5)CC4)cc3)cc21 10.1016/j.bmc.2008.01.002
76325371 105520 None 0 Human Binding pKi = 9.0 9.0 -25 4
Binding affinity to human recombinant adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated adenylyl cyclase activity after 20 minsBinding affinity to human recombinant adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated adenylyl cyclase activity after 20 mins
ChEMBL 380 6 1 8 1.3 Cn1c(=O)c2[nH]c(-c3ccc(OCCCn4ccnc4)cc3)nc2n(C)c1=O 10.1016/j.ejmech.2014.01.045
CHEMBL3121727 105520 None 0 Human Binding pKi = 9.0 9.0 -25 4
Binding affinity to human recombinant adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated adenylyl cyclase activity after 20 minsBinding affinity to human recombinant adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated adenylyl cyclase activity after 20 mins
ChEMBL 380 6 1 8 1.3 Cn1c(=O)c2[nH]c(-c3ccc(OCCCn4ccnc4)cc3)nc2n(C)c1=O 10.1016/j.ejmech.2014.01.045
44186719 185916 None 0 Human Binding pKi = 9.0 9.0 74 6
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 552 7 2 9 1.7 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc6c(c5)OCO6)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
CHEMBL486893 185916 None 0 Human Binding pKi = 9.0 9.0 74 6
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 552 7 2 9 1.7 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc6c(c5)OCO6)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
44186579 191784 None 0 Human Binding pKi = 8.9 8.9 131 6
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 494 6 2 7 1.6 CCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccccc5)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
CHEMBL519813 191784 None 0 Human Binding pKi = 8.9 8.9 131 6
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 494 6 2 7 1.6 CCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccccc5)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
44186716 184114 None 0 Human Binding pKi = 8.9 8.9 194 6
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 524 7 2 8 1.6 CCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc(OC)cc5)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
CHEMBL482648 184114 None 0 Human Binding pKi = 8.9 8.9 194 6
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 524 7 2 8 1.6 CCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc(OC)cc5)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
44583036 186955 None 0 Human Binding pKi = 8.9 8.9 7 5
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 400 8 3 7 0.6 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)NCCO)cc3)cc2n(C)c1=O 10.1021/jm900413e
CHEMBL490262 186955 None 0 Human Binding pKi = 8.9 8.9 7 5
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 400 8 3 7 0.6 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)NCCO)cc3)cc2n(C)c1=O 10.1021/jm900413e
CHEMBL521280 186955 None 0 Human Binding pKi = 8.9 8.9 7 5
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 400 8 3 7 0.6 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)NCCO)cc3)cc2n(C)c1=O 10.1021/jm900413e
57429647 158637 None 0 Human Binding pKi = 8.9 8.9 - 1
Displacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting methodDisplacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting method
ChEMBL 573 9 2 9 3.0 CCCn1c(=O)c2[nH]c(-c3cnn(CC(O)C4CC(=O)N(c5cccc(C(F)(F)F)c5)C4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2016.11.007
CHEMBL4092455 158637 None 0 Human Binding pKi = 8.9 8.9 - 1
Displacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting methodDisplacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting method
ChEMBL 573 9 2 9 3.0 CCCn1c(=O)c2[nH]c(-c3cnn(CC(O)C4CC(=O)N(c5cccc(C(F)(F)F)c5)C4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2016.11.007
10875138 138390 None 0 Human Binding pKi = 8.9 8.9 19 4
Inhibition of [3H]ZM-241385 binding to human adenosine A2B receptorInhibition of [3H]ZM-241385 binding to human adenosine A2B receptor
ChEMBL 532 9 2 8 2.6 CCCCn1c(=O)[nH]c2[nH]c(-c3ccc(OCC(=O)N4CCN(c5ccccc5OC)CC4)cc3)nc2c1=O 10.1021/jm011049y
CHEMBL37726 138390 None 0 Human Binding pKi = 8.9 8.9 19 4
Inhibition of [3H]ZM-241385 binding to human adenosine A2B receptorInhibition of [3H]ZM-241385 binding to human adenosine A2B receptor
ChEMBL 532 9 2 8 2.6 CCCCn1c(=O)[nH]c2[nH]c(-c3ccc(OCC(=O)N4CCN(c5ccccc5OC)CC4)cc3)nc2c1=O 10.1021/jm011049y
10452788 162291 None 0 Human Binding pKi = 8.9 8.9 28 5
Inhibition of [3H]ZM-241385 binding to human adenosine A2B receptorInhibition of [3H]ZM-241385 binding to human adenosine A2B receptor
ChEMBL 387 8 4 7 -0.0 CCCn1c(=O)[nH]c2[nH]c(-c3ccc(OCC(=O)NCCO)cc3)nc2c1=O 10.1021/jm011049y
CHEMBL416417 162291 None 0 Human Binding pKi = 8.9 8.9 28 5
Inhibition of [3H]ZM-241385 binding to human adenosine A2B receptorInhibition of [3H]ZM-241385 binding to human adenosine A2B receptor
ChEMBL 387 8 4 7 -0.0 CCCn1c(=O)[nH]c2[nH]c(-c3ccc(OCC(=O)NCCO)cc3)nc2c1=O 10.1021/jm011049y
155556884 174579 None 0 Human Binding pKi = 8.9 8.9 - 1
Displacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 542 7 2 8 2.1 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(c5ccc(OC)c(F)c5)CC4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
CHEMBL4556744 174579 None 0 Human Binding pKi = 8.9 8.9 - 1
Displacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 542 7 2 8 2.1 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(c5ccc(OC)c(F)c5)CC4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
44186623 192089 None 0 Human Binding pKi = 8.9 8.9 31 6
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 512 6 2 7 1.7 CCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc(F)cc5)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
CHEMBL520297 192089 None 0 Human Binding pKi = 8.9 8.9 31 6
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 512 6 2 7 1.7 CCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc(F)cc5)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
155512438 169645 None 0 Human Binding pKi = 8.9 8.9 102 3
Displacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 538 8 2 8 2.0 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5cccc(OC)c5)CC4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
CHEMBL4437222 169645 None 0 Human Binding pKi = 8.9 8.9 102 3
Displacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 538 8 2 8 2.0 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5cccc(OC)c5)CC4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
57429619 158136 None 0 Human Binding pKi = 8.9 8.9 - 1
Displacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 minsDisplacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 mins
ChEMBL 442 4 2 6 2.8 CCCn1c(=O)[nH]c2nc(-c3cnn(CC#Cc4ccc(C(F)(F)F)cc4)c3)[nH]c2c1=O 10.1016/j.ejmech.2017.04.014
CHEMBL4087158 158136 None 0 Human Binding pKi = 8.9 8.9 - 1
Displacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 minsDisplacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 mins
ChEMBL 442 4 2 6 2.8 CCCn1c(=O)[nH]c2nc(-c3cnn(CC#Cc4ccc(C(F)(F)F)cc4)c3)[nH]c2c1=O 10.1016/j.ejmech.2017.04.014
10075248 141246 None 0 Human Binding pKi = 8.9 8.9 28 5
Inhibition of [3H]ZM-241385 binding to human adenosine A2B receptorInhibition of [3H]ZM-241385 binding to human adenosine A2B receptor
ChEMBL 516 9 2 7 2.6 CCCCn1c(=O)[nH]c2[nH]c(-c3ccc(OCC(=O)N4CCN(Cc5ccccc5)CC4)cc3)nc2c1=O 10.1021/jm011049y
CHEMBL38304 141246 None 0 Human Binding pKi = 8.9 8.9 28 5
Inhibition of [3H]ZM-241385 binding to human adenosine A2B receptorInhibition of [3H]ZM-241385 binding to human adenosine A2B receptor
ChEMBL 516 9 2 7 2.6 CCCCn1c(=O)[nH]c2[nH]c(-c3ccc(OCC(=O)N4CCN(Cc5ccccc5)CC4)cc3)nc2c1=O 10.1021/jm011049y
145977111 163765 None 0 Mouse Binding pKi = 8.9 8.9 -7 4
Displacement of [3H]PSB-603 from recombinant mouse adenosine A2B receptor expressed in CHO cell membranes after 75 mins by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant mouse adenosine A2B receptor expressed in CHO cell membranes after 75 mins by liquid scintillation counting method
ChEMBL 617 9 3 7 3.9 CCCn1c(=O)[nH]c2nc(-c3ccc(OCC(=O)NCCC4=C5C(C)=CC(C)=[N+]5[B-](F)(F)n5c(C)cc(C)c54)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.7b01627
CHEMBL4205635 163765 None 0 Mouse Binding pKi = 8.9 8.9 -7 4
Displacement of [3H]PSB-603 from recombinant mouse adenosine A2B receptor expressed in CHO cell membranes after 75 mins by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant mouse adenosine A2B receptor expressed in CHO cell membranes after 75 mins by liquid scintillation counting method
ChEMBL 617 9 3 7 3.9 CCCn1c(=O)[nH]c2nc(-c3ccc(OCC(=O)NCCC4=C5C(C)=CC(C)=[N+]5[B-](F)(F)n5c(C)cc(C)c54)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.7b01627
11605883 79952 None 6 Human Binding pKi = 8.9 8.9 42 6
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 508 7 2 7 2.0 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccccc5)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
CHEMBL212625 79952 None 6 Human Binding pKi = 8.9 8.9 42 6
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 508 7 2 7 2.0 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccccc5)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
76325369 105516 None 0 Human Binding pKi = 8.9 8.9 -4 4
Binding affinity to human recombinant adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated adenylyl cyclase activity after 20 minsBinding affinity to human recombinant adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated adenylyl cyclase activity after 20 mins
ChEMBL 385 5 1 8 0.3 Cn1c(=O)c2[nH]c(-c3ccc(OCCN4CCOCC4)cc3)nc2n(C)c1=O 10.1016/j.ejmech.2014.01.045
CHEMBL3121723 105516 None 0 Human Binding pKi = 8.9 8.9 -4 4
Binding affinity to human recombinant adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated adenylyl cyclase activity after 20 minsBinding affinity to human recombinant adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated adenylyl cyclase activity after 20 mins
ChEMBL 385 5 1 8 0.3 Cn1c(=O)c2[nH]c(-c3ccc(OCCN4CCOCC4)cc3)nc2n(C)c1=O 10.1016/j.ejmech.2014.01.045
3287 2642 None 43 Human Binding pKi = 8.9 8.9 27 6
Displacement of [125I]IABOPX to human A2B receptor assessed as inhibition constant by fluorescence based assayDisplacement of [125I]IABOPX to human A2B receptor assessed as inhibition constant by fluorescence based assay
ChEMBL 503 10 2 8 3.6 CCCn1c2[nH]c(nc2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C(=O)C 10.1021/acs.jmedchem.1c00261
5139184 2642 None 43 Human Binding pKi = 8.9 8.9 27 6
Displacement of [125I]IABOPX to human A2B receptor assessed as inhibition constant by fluorescence based assayDisplacement of [125I]IABOPX to human A2B receptor assessed as inhibition constant by fluorescence based assay
ChEMBL 503 10 2 8 3.6 CCCn1c2[nH]c(nc2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C(=O)C 10.1021/acs.jmedchem.1c00261
CHEMBL17002 2642 None 43 Human Binding pKi = 8.9 8.9 27 6
Displacement of [125I]IABOPX to human A2B receptor assessed as inhibition constant by fluorescence based assayDisplacement of [125I]IABOPX to human A2B receptor assessed as inhibition constant by fluorescence based assay
ChEMBL 503 10 2 8 3.6 CCCn1c2[nH]c(nc2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C(=O)C 10.1021/acs.jmedchem.1c00261
46229140 199645 None 0 Human Binding pKi = 8.9 8.9 - 1
Inhibition of adenosine A2B receptorInhibition of adenosine A2B receptor
ChEMBL 517 10 1 9 3.6 CCCn1c(=O)c2c(nc(-c3ccc(OCC(=O)Nc4ccc(C(C)=O)cc4)cc3)n2C)n(CCC)c1=O 10.1016/j.bmc.2010.02.014
CHEMBL592891 199645 None 0 Human Binding pKi = 8.9 8.9 - 1
Inhibition of adenosine A2B receptorInhibition of adenosine A2B receptor
ChEMBL 517 10 1 9 3.6 CCCn1c(=O)c2c(nc(-c3ccc(OCC(=O)Nc4ccc(C(C)=O)cc4)cc3)n2C)n(CCC)c1=O 10.1016/j.bmc.2010.02.014
44236600 158247 None 0 Human Binding pKi = 8.8 8.8 - 1
Displacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 minsDisplacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 mins
ChEMBL 484 6 1 7 3.6 CCCn1c(=O)c2[nH]c(-c3cnn(CC#Cc4ccc(C(F)(F)F)cc4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2017.04.014
CHEMBL4088514 158247 None 0 Human Binding pKi = 8.8 8.8 - 1
Displacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 minsDisplacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 mins
ChEMBL 484 6 1 7 3.6 CCCn1c(=O)c2[nH]c(-c3cnn(CC#Cc4ccc(C(F)(F)F)cc4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2017.04.014
57429649 158942 None 0 Human Binding pKi = 8.8 8.8 23 3
Displacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting methodDisplacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting method
ChEMBL 572 8 1 9 2.9 CCCn1c(=O)c2[nH]c(-c3cnn(CC(=O)N4CCN(c5cccc(C(F)(F)F)c5)CC4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2016.11.007
CHEMBL4095843 158942 None 0 Human Binding pKi = 8.8 8.8 23 3
Displacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting methodDisplacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting method
ChEMBL 572 8 1 9 2.9 CCCn1c(=O)c2[nH]c(-c3cnn(CC(=O)N4CCN(c5cccc(C(F)(F)F)c5)CC4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2016.11.007
44451075 96076 None 0 Human Binding pKi = 8.8 8.8 75 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 563 9 1 7 4.4 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCN(c5cccc(Cl)c5)CC4)cc3)cc2n(CCC)c1=O 10.1016/j.bmc.2008.01.002
CHEMBL260051 96076 None 0 Human Binding pKi = 8.8 8.8 75 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 563 9 1 7 4.4 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCN(c5cccc(Cl)c5)CC4)cc3)cc2n(CCC)c1=O 10.1016/j.bmc.2008.01.002
9825550 57592 None 0 Human Binding pKi = 8.8 8.8 2 6
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 461 9 2 7 3.4 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccccc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm0506221
CHEMBL16677 57592 None 0 Human Binding pKi = 8.8 8.8 2 6
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 461 9 2 7 3.4 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccccc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm0506221
44451075 96076 None 0 Human Binding pKi = 8.8 8.8 75 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 563 9 1 7 4.4 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCN(c5cccc(Cl)c5)CC4)cc3)cc2n(CCC)c1=O 10.1016/j.bmc.2008.01.002
CHEMBL260051 96076 None 0 Human Binding pKi = 8.8 8.8 75 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 563 9 1 7 4.4 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCN(c5cccc(Cl)c5)CC4)cc3)cc2n(CCC)c1=O 10.1016/j.bmc.2008.01.002
11684701 133435 None 0 Human Binding pKi = 8.8 8.8 17 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 496 5 2 6 3.4 CC(Oc1ccc(-c2cc3c([nH]2)c(=O)n(C)c(=O)n3C)cc1)C(=O)Nc1ccc(Br)cc1 10.1021/jm0506221
CHEMBL370588 133435 None 0 Human Binding pKi = 8.8 8.8 17 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 496 5 2 6 3.4 CC(Oc1ccc(-c2cc3c([nH]2)c(=O)n(C)c(=O)n3C)cc1)C(=O)Nc1ccc(Br)cc1 10.1021/jm0506221
44186670 192302 None 0 Human Binding pKi = 8.8 8.8 24 4
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 508 6 2 7 1.9 CCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc(C)cc5)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
CHEMBL520617 192302 None 0 Human Binding pKi = 8.8 8.8 24 4
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 508 6 2 7 1.9 CCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc(C)cc5)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
57429620 155809 None 0 Human Binding pKi = 8.8 8.8 - 1
Displacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 minsDisplacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 mins
ChEMBL 458 5 2 7 2.6 CCCn1c(=O)[nH]c2nc(-c3cnn(CC#Cc4ccc(OC(F)(F)F)cc4)c3)[nH]c2c1=O 10.1016/j.ejmech.2017.04.014
CHEMBL4059779 155809 None 0 Human Binding pKi = 8.8 8.8 - 1
Displacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 minsDisplacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 mins
ChEMBL 458 5 2 7 2.6 CCCn1c(=O)[nH]c2nc(-c3cnn(CC#Cc4ccc(OC(F)(F)F)cc4)c3)[nH]c2c1=O 10.1016/j.ejmech.2017.04.014
57429617 157466 None 0 Human Binding pKi = 8.8 8.8 - 1
Displacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 minsDisplacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 mins
ChEMBL 392 4 2 6 1.9 CCCn1c(=O)[nH]c2nc(-c3cnn(CC#Cc4ccc(F)cc4)c3)[nH]c2c1=O 10.1016/j.ejmech.2017.04.014
CHEMBL4079273 157466 None 0 Human Binding pKi = 8.8 8.8 - 1
Displacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 minsDisplacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 mins
ChEMBL 392 4 2 6 1.9 CCCn1c(=O)[nH]c2nc(-c3cnn(CC#Cc4ccc(F)cc4)c3)[nH]c2c1=O 10.1016/j.ejmech.2017.04.014
155536745 172203 None 0 Human Binding pKi = 8.8 8.8 208 3
Displacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 467 8 2 6 2.4 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N(C)CCc4ccccc4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
CHEMBL4473749 172203 None 0 Human Binding pKi = 8.8 8.8 208 3
Displacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 467 8 2 6 2.4 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N(C)CCc4ccccc4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
44574251 178429 None 0 Human Binding pKi = 8.8 8.8 12 2
Displacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells by beta scintillation counterDisplacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells by beta scintillation counter
ChEMBL 451 8 2 8 3.7 CCCn1c(=O)c2[nH]c(-c3ccc(COC(=O)Nc4ccon4)cc3)cc2n(CCC)c1=O 10.1016/j.bmc.2009.03.062
CHEMBL466035 178429 None 0 Human Binding pKi = 8.8 8.8 12 2
Displacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells by beta scintillation counterDisplacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells by beta scintillation counter
ChEMBL 451 8 2 8 3.7 CCCn1c(=O)c2[nH]c(-c3ccc(COC(=O)Nc4ccon4)cc3)cc2n(CCC)c1=O 10.1016/j.bmc.2009.03.062
44236445 157540 None 0 Human Binding pKi = 8.7 8.7 - 1
Displacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting methodDisplacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting method
ChEMBL 556 8 1 9 2.7 CCCn1c(=O)c2[nH]c(-c3cnn(CC(=O)N4CCN(c5ccc(F)c(Cl)c5)CC4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2016.11.007
CHEMBL4080171 157540 None 0 Human Binding pKi = 8.7 8.7 - 1
Displacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting methodDisplacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting method
ChEMBL 556 8 1 9 2.7 CCCn1c(=O)c2[nH]c(-c3cnn(CC(=O)N4CCN(c5ccc(F)c(Cl)c5)CC4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2016.11.007
44451329 96183 None 0 Human Binding pKi = 8.7 8.7 204 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 501 5 1 7 2.7 Cc1ccc(N2CCN(C(=O)C(C)Oc3ccc(-c4cc5c([nH]4)c(=O)n(C)c(=O)n5C)cc3)CC2)cc1 10.1016/j.bmc.2008.01.002
CHEMBL260692 96183 None 0 Human Binding pKi = 8.7 8.7 204 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 501 5 1 7 2.7 Cc1ccc(N2CCN(C(=O)C(C)Oc3ccc(-c4cc5c([nH]4)c(=O)n(C)c(=O)n5C)cc3)CC2)cc1 10.1016/j.bmc.2008.01.002
145977111 163765 None 0 Human Binding pKi = 8.7 8.7 -10 4
Displacement of [3H]PSB-603 from recombinant human adenosine A2B receptor expressed in CHO cell membranes after 75 mins by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human adenosine A2B receptor expressed in CHO cell membranes after 75 mins by liquid scintillation counting method
ChEMBL 617 9 3 7 3.9 CCCn1c(=O)[nH]c2nc(-c3ccc(OCC(=O)NCCC4=C5C(C)=CC(C)=[N+]5[B-](F)(F)n5c(C)cc(C)c54)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.7b01627
CHEMBL4205635 163765 None 0 Human Binding pKi = 8.7 8.7 -10 4
Displacement of [3H]PSB-603 from recombinant human adenosine A2B receptor expressed in CHO cell membranes after 75 mins by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human adenosine A2B receptor expressed in CHO cell membranes after 75 mins by liquid scintillation counting method
ChEMBL 617 9 3 7 3.9 CCCn1c(=O)[nH]c2nc(-c3ccc(OCC(=O)NCCC4=C5C(C)=CC(C)=[N+]5[B-](F)(F)n5c(C)cc(C)c54)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.7b01627
449 2643 None 52 Human Binding pKi = 8.7 8.7 -1 9
Displacement of [3H]ZM241385/[125I]IABOPX from human recombinant adenosine A2B receptor expressed in HEK293 cells after 3 hrsDisplacement of [3H]ZM241385/[125I]IABOPX from human recombinant adenosine A2B receptor expressed in HEK293 cells after 3 hrs
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10.1021/acs.jmedchem.7b00138
453 2643 None 52 Human Binding pKi = 8.7 8.7 -1 9
Displacement of [3H]ZM241385/[125I]IABOPX from human recombinant adenosine A2B receptor expressed in HEK293 cells after 3 hrsDisplacement of [3H]ZM241385/[125I]IABOPX from human recombinant adenosine A2B receptor expressed in HEK293 cells after 3 hrs
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10.1021/acs.jmedchem.7b00138
6603931 2643 None 52 Human Binding pKi = 8.7 8.7 -1 9
Displacement of [3H]ZM241385/[125I]IABOPX from human recombinant adenosine A2B receptor expressed in HEK293 cells after 3 hrsDisplacement of [3H]ZM241385/[125I]IABOPX from human recombinant adenosine A2B receptor expressed in HEK293 cells after 3 hrs
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10.1021/acs.jmedchem.7b00138
CHEMBL273807 2643 None 52 Human Binding pKi = 8.7 8.7 -1 9
Displacement of [3H]ZM241385/[125I]IABOPX from human recombinant adenosine A2B receptor expressed in HEK293 cells after 3 hrsDisplacement of [3H]ZM241385/[125I]IABOPX from human recombinant adenosine A2B receptor expressed in HEK293 cells after 3 hrs
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10.1021/acs.jmedchem.7b00138
44276476 168094 None 0 Human Binding pKi = 8.7 8.7 13 3
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 475 9 2 7 3.7 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccc(C)cc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm0506221
CHEMBL432664 168094 None 0 Human Binding pKi = 8.7 8.7 13 3
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 475 9 2 7 3.7 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccc(C)cc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm0506221
155528717 171348 None 0 Human Binding pKi = 8.7 8.7 - 1
Displacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 546 6 2 7 2.8 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(c5ccc(Cl)cc5F)CC4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
CHEMBL4461478 171348 None 0 Human Binding pKi = 8.7 8.7 - 1
Displacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 546 6 2 7 2.8 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(c5ccc(Cl)cc5F)CC4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
155548264 173768 None 0 Human Binding pKi = 8.7 8.7 4 3
Displacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 542 6 1 8 2.7 CCCn1c(=O)c2[nH]c(-c3ccc(S(=O)(=O)N4CCN(c5ccc(Cl)cc5)CC4)cc3)nc2n(C)c1=O 10.1021/acs.jmedchem.9b00071
CHEMBL4537196 173768 None 0 Human Binding pKi = 8.7 8.7 4 3
Displacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 542 6 1 8 2.7 CCCn1c(=O)c2[nH]c(-c3ccc(S(=O)(=O)N4CCN(c5ccc(Cl)cc5)CC4)cc3)nc2n(C)c1=O 10.1021/acs.jmedchem.9b00071
449 2643 None 52 Human Binding pKi = 8.7 8.7 -1 9
Antagonist activity at human A2B receptorAntagonist activity at human A2B receptor
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10.1021/acs.jmedchem.0c01431
453 2643 None 52 Human Binding pKi = 8.7 8.7 -1 9
Antagonist activity at human A2B receptorAntagonist activity at human A2B receptor
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10.1021/acs.jmedchem.0c01431
6603931 2643 None 52 Human Binding pKi = 8.7 8.7 -1 9
Antagonist activity at human A2B receptorAntagonist activity at human A2B receptor
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10.1021/acs.jmedchem.0c01431
CHEMBL273807 2643 None 52 Human Binding pKi = 8.7 8.7 -1 9
Antagonist activity at human A2B receptorAntagonist activity at human A2B receptor
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10.1021/acs.jmedchem.0c01431
449 2643 None 52 Human Binding pKi = 8.7 8.7 -1 9
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10.1021/jm900413e
453 2643 None 52 Human Binding pKi = 8.7 8.7 -1 9
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10.1021/jm900413e
6603931 2643 None 52 Human Binding pKi = 8.7 8.7 -1 9
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10.1021/jm900413e
CHEMBL273807 2643 None 52 Human Binding pKi = 8.7 8.7 -1 9
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10.1021/jm900413e
76310832 105517 None 0 Human Binding pKi = 8.7 8.7 -9 4
Binding affinity to human recombinant adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated adenylyl cyclase activity after 20 minsBinding affinity to human recombinant adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated adenylyl cyclase activity after 20 mins
ChEMBL 369 5 1 7 1.1 Cn1c(=O)c2[nH]c(-c3ccc(OCCN4CCCC4)cc3)nc2n(C)c1=O 10.1016/j.ejmech.2014.01.045
CHEMBL3121724 105517 None 0 Human Binding pKi = 8.7 8.7 -9 4
Binding affinity to human recombinant adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated adenylyl cyclase activity after 20 minsBinding affinity to human recombinant adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated adenylyl cyclase activity after 20 mins
ChEMBL 369 5 1 7 1.1 Cn1c(=O)c2[nH]c(-c3ccc(OCCN4CCCC4)cc3)nc2n(C)c1=O 10.1016/j.ejmech.2014.01.045
449 2643 None 52 Human Binding pKi = 8.7 8.7 -1 9
Binding affinity towards human Adenosine A2B receptorBinding affinity towards human Adenosine A2B receptor
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10.1021/jm011049y
453 2643 None 52 Human Binding pKi = 8.7 8.7 -1 9
Binding affinity towards human Adenosine A2B receptorBinding affinity towards human Adenosine A2B receptor
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10.1021/jm011049y
6603931 2643 None 52 Human Binding pKi = 8.7 8.7 -1 9
Binding affinity towards human Adenosine A2B receptorBinding affinity towards human Adenosine A2B receptor
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10.1021/jm011049y
CHEMBL273807 2643 None 52 Human Binding pKi = 8.7 8.7 -1 9
Binding affinity towards human Adenosine A2B receptorBinding affinity towards human Adenosine A2B receptor
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10.1021/jm011049y
449 2643 None 52 Human Binding pKi = 8.7 8.7 -1 9
Displacement of [125I]IABOPX from human recombinant Adenosine A2B receptor expressed in HEK293 cells after 3 hrsDisplacement of [125I]IABOPX from human recombinant Adenosine A2B receptor expressed in HEK293 cells after 3 hrs
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10.1021/acs.jmedchem.5b01586
453 2643 None 52 Human Binding pKi = 8.7 8.7 -1 9
Displacement of [125I]IABOPX from human recombinant Adenosine A2B receptor expressed in HEK293 cells after 3 hrsDisplacement of [125I]IABOPX from human recombinant Adenosine A2B receptor expressed in HEK293 cells after 3 hrs
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10.1021/acs.jmedchem.5b01586
6603931 2643 None 52 Human Binding pKi = 8.7 8.7 -1 9
Displacement of [125I]IABOPX from human recombinant Adenosine A2B receptor expressed in HEK293 cells after 3 hrsDisplacement of [125I]IABOPX from human recombinant Adenosine A2B receptor expressed in HEK293 cells after 3 hrs
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10.1021/acs.jmedchem.5b01586
CHEMBL273807 2643 None 52 Human Binding pKi = 8.7 8.7 -1 9
Displacement of [125I]IABOPX from human recombinant Adenosine A2B receptor expressed in HEK293 cells after 3 hrsDisplacement of [125I]IABOPX from human recombinant Adenosine A2B receptor expressed in HEK293 cells after 3 hrs
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10.1021/acs.jmedchem.5b01586
449 2643 None 52 Human Binding pKi = 8.7 8.7 -1 9
Displacement of [125I]IABOPX to human A2B receptor assessed as inhibition constant by fluorescence based assayDisplacement of [125I]IABOPX to human A2B receptor assessed as inhibition constant by fluorescence based assay
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10.1021/acs.jmedchem.1c00261
453 2643 None 52 Human Binding pKi = 8.7 8.7 -1 9
Displacement of [125I]IABOPX to human A2B receptor assessed as inhibition constant by fluorescence based assayDisplacement of [125I]IABOPX to human A2B receptor assessed as inhibition constant by fluorescence based assay
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10.1021/acs.jmedchem.1c00261
6603931 2643 None 52 Human Binding pKi = 8.7 8.7 -1 9
Displacement of [125I]IABOPX to human A2B receptor assessed as inhibition constant by fluorescence based assayDisplacement of [125I]IABOPX to human A2B receptor assessed as inhibition constant by fluorescence based assay
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10.1021/acs.jmedchem.1c00261
CHEMBL273807 2643 None 52 Human Binding pKi = 8.7 8.7 -1 9
Displacement of [125I]IABOPX to human A2B receptor assessed as inhibition constant by fluorescence based assayDisplacement of [125I]IABOPX to human A2B receptor assessed as inhibition constant by fluorescence based assay
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10.1021/acs.jmedchem.1c00261
449 2643 None 52 Human Binding pKi = 8.7 8.7 -1 9
Displacement of [3H]ZM241385/[125I]IABOPX from recombinant human A2B adenosine receptor expressed in HEK293 cell membranes measured after 3 hrsDisplacement of [3H]ZM241385/[125I]IABOPX from recombinant human A2B adenosine receptor expressed in HEK293 cell membranes measured after 3 hrs
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10.1021/acs.jmedchem.9b00071
453 2643 None 52 Human Binding pKi = 8.7 8.7 -1 9
Displacement of [3H]ZM241385/[125I]IABOPX from recombinant human A2B adenosine receptor expressed in HEK293 cell membranes measured after 3 hrsDisplacement of [3H]ZM241385/[125I]IABOPX from recombinant human A2B adenosine receptor expressed in HEK293 cell membranes measured after 3 hrs
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10.1021/acs.jmedchem.9b00071
6603931 2643 None 52 Human Binding pKi = 8.7 8.7 -1 9
Displacement of [3H]ZM241385/[125I]IABOPX from recombinant human A2B adenosine receptor expressed in HEK293 cell membranes measured after 3 hrsDisplacement of [3H]ZM241385/[125I]IABOPX from recombinant human A2B adenosine receptor expressed in HEK293 cell membranes measured after 3 hrs
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10.1021/acs.jmedchem.9b00071
CHEMBL273807 2643 None 52 Human Binding pKi = 8.7 8.7 -1 9
Displacement of [3H]ZM241385/[125I]IABOPX from recombinant human A2B adenosine receptor expressed in HEK293 cell membranes measured after 3 hrsDisplacement of [3H]ZM241385/[125I]IABOPX from recombinant human A2B adenosine receptor expressed in HEK293 cell membranes measured after 3 hrs
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10.1021/acs.jmedchem.9b00071
44185874 185660 None 0 Human Binding pKi = 8.7 8.7 20 5
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 524 7 2 8 2.0 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(c5ccc(OC)cc5)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
CHEMBL486481 185660 None 0 Human Binding pKi = 8.7 8.7 20 5
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 524 7 2 8 2.0 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(c5ccc(OC)cc5)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
449 2643 None 52 Human Binding pKi = 8.7 8.7 -1 9
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10.1021/jm0506221
453 2643 None 52 Human Binding pKi = 8.7 8.7 -1 9
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10.1021/jm0506221
6603931 2643 None 52 Human Binding pKi = 8.7 8.7 -1 9
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10.1021/jm0506221
CHEMBL273807 2643 None 52 Human Binding pKi = 8.7 8.7 -1 9
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10.1021/jm0506221
135522368 492 None 1 Human Binding pKi = 8 8.0 117 2
Binding affinity of compound for displacement of [3H]DPCPX binding in HEK293 membranes expressing human A2B adenosine receptorsBinding affinity of compound for displacement of [3H]DPCPX binding in HEK293 membranes expressing human A2B adenosine receptors
ChEMBL 493 9 2 9 2.7 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)Nc1ccc(c(c1)C)C 10.1021/jm0309654
383 492 None 1 Human Binding pKi = 8 8.0 117 2
Binding affinity of compound for displacement of [3H]DPCPX binding in HEK293 membranes expressing human A2B adenosine receptorsBinding affinity of compound for displacement of [3H]DPCPX binding in HEK293 membranes expressing human A2B adenosine receptors
ChEMBL 493 9 2 9 2.7 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)Nc1ccc(c(c1)C)C 10.1021/jm0309654
CHEMBL33491 492 None 1 Human Binding pKi = 8 8.0 117 2
Binding affinity of compound for displacement of [3H]DPCPX binding in HEK293 membranes expressing human A2B adenosine receptorsBinding affinity of compound for displacement of [3H]DPCPX binding in HEK293 membranes expressing human A2B adenosine receptors
ChEMBL 493 9 2 9 2.7 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)Nc1ccc(c(c1)C)C 10.1021/jm0309654
135522368 492 None 1 Human Binding pKi = 8 8.0 117 2
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 493 9 2 9 2.7 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)Nc1ccc(c(c1)C)C 10.1021/jm0309654
383 492 None 1 Human Binding pKi = 8 8.0 117 2
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 493 9 2 9 2.7 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)Nc1ccc(c(c1)C)C 10.1021/jm0309654
CHEMBL33491 492 None 1 Human Binding pKi = 8 8.0 117 2
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 493 9 2 9 2.7 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)Nc1ccc(c(c1)C)C 10.1021/jm0309654
16072023 58012 None 0 Human Binding pKi = 8 8.0 1 4
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 308 4 1 5 3.4 CC(C)C(=O)Nc1cnc(-c2ccncc2)c(-c2ccco2)n1 10.1021/ml100249e
CHEMBL1672614 58012 None 0 Human Binding pKi = 8 8.0 1 4
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 308 4 1 5 3.4 CC(C)C(=O)Nc1cnc(-c2ccncc2)c(-c2ccco2)n1 10.1021/ml100249e
44574166 178705 None 0 Human Binding pKi = 8 8.0 1 2
Displacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells by beta scintillation counterDisplacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells by beta scintillation counter
ChEMBL 410 4 2 7 3.0 Cn1c(=O)c2[nH]c(-c3ccc(COC(=O)Nc4cccs4)cc3)cc2n(C)c1=O 10.1016/j.bmc.2009.03.062
CHEMBL468295 178705 None 0 Human Binding pKi = 8 8.0 1 2
Displacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells by beta scintillation counterDisplacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells by beta scintillation counter
ChEMBL 410 4 2 7 3.0 Cn1c(=O)c2[nH]c(-c3ccc(COC(=O)Nc4cccs4)cc3)cc2n(C)c1=O 10.1016/j.bmc.2009.03.062
136042341 71167 None 0 Human Binding pKi = 8 8.0 17 2
Displacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation countingDisplacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation counting
ChEMBL 517 8 2 9 3.8 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5cc(C(F)(F)F)ccc5[nH]4)no3)nc2n(CCC)c1=O 10.1021/jm201292w
CHEMBL1955917 71167 None 0 Human Binding pKi = 8 8.0 17 2
Displacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation countingDisplacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation counting
ChEMBL 517 8 2 9 3.8 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5cc(C(F)(F)F)ccc5[nH]4)no3)nc2n(CCC)c1=O 10.1021/jm201292w
49797794 10588 None 0 Human Binding pKi = 8 8.0 5 3
Displacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cells after 1 hr by scintillation countingDisplacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 394 5 1 6 3.8 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(C#N)cc3)sc12 10.1016/j.bmcl.2010.05.056
CHEMBL1169934 10588 None 0 Human Binding pKi = 8 8.0 5 3
Displacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cells after 1 hr by scintillation countingDisplacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 394 5 1 6 3.8 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(C#N)cc3)sc12 10.1016/j.bmcl.2010.05.056
9901196 188833 None 0 Human Binding pKi = 8 8.0 -2 4
Displacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation countingDisplacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation counting
ChEMBL 308 3 2 8 1.8 Nc1nc(-c2ccco2)c2nnn(Cc3cccc(O)c3)c2n1 10.1021/jm800961g
CHEMBL506511 188833 None 0 Human Binding pKi = 8 8.0 -2 4
Displacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation countingDisplacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation counting
ChEMBL 308 3 2 8 1.8 Nc1nc(-c2ccco2)c2nnn(Cc3cccc(O)c3)c2n1 10.1021/jm800961g
11760836 100219 None 0 Human Binding pKi = 8 8.0 2 3
Inhibition of [3H]ZM-241380 binding to adenosine A2b receptorInhibition of [3H]ZM-241380 binding to adenosine A2b receptor
ChEMBL 386 8 4 7 -0.1 CCCn1c(=O)[nH]c2[nH]c(-c3ccc(OCC(=O)NCCN)cc3)nc2c1=O 10.1021/jm049513x
CHEMBL288459 100219 None 0 Human Binding pKi = 8 8.0 2 3
Inhibition of [3H]ZM-241380 binding to adenosine A2b receptorInhibition of [3H]ZM-241380 binding to adenosine A2b receptor
ChEMBL 386 8 4 7 -0.1 CCCn1c(=O)[nH]c2[nH]c(-c3ccc(OCC(=O)NCCN)cc3)nc2c1=O 10.1021/jm049513x
11760836 100219 None 0 Human Binding pKi = 8 8.0 2 3
Inhibition of [3H]ZM-241385 binding to human adenosine A2B receptorInhibition of [3H]ZM-241385 binding to human adenosine A2B receptor
ChEMBL 386 8 4 7 -0.1 CCCn1c(=O)[nH]c2[nH]c(-c3ccc(OCC(=O)NCCN)cc3)nc2c1=O 10.1021/jm011049y
CHEMBL288459 100219 None 0 Human Binding pKi = 8 8.0 2 3
Inhibition of [3H]ZM-241385 binding to human adenosine A2B receptorInhibition of [3H]ZM-241385 binding to human adenosine A2B receptor
ChEMBL 386 8 4 7 -0.1 CCCn1c(=O)[nH]c2[nH]c(-c3ccc(OCC(=O)NCCN)cc3)nc2c1=O 10.1021/jm011049y
2748282 103854 None 7 Human Binding pKi = 8.0 8.0 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 280 3 2 4 2.0 CC1=C(C(=O)OC(C)C)C(c2ccco2)NC(=S)N1 10.1021/acs.jmedchem.0c01431
CHEMBL3091713 103854 None 7 Human Binding pKi = 8.0 8.0 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 280 3 2 4 2.0 CC1=C(C(=O)OC(C)C)C(c2ccco2)NC(=S)N1 10.1021/acs.jmedchem.0c01431
2748282 103854 None 7 Human Binding pKi = 8.0 8.0 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by Scatchard plot analysisDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by Scatchard plot analysis
ChEMBL 280 3 2 4 2.0 CC1=C(C(=O)OC(C)C)C(c2ccco2)NC(=S)N1 10.1021/ml400185v
CHEMBL3091713 103854 None 7 Human Binding pKi = 8.0 8.0 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by Scatchard plot analysisDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by Scatchard plot analysis
ChEMBL 280 3 2 4 2.0 CC1=C(C(=O)OC(C)C)C(c2ccco2)NC(=S)N1 10.1021/ml400185v
136042354 71154 None 0 Human Binding pKi = 8.0 8.0 72 2
Displacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation countingDisplacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation counting
ChEMBL 476 8 2 9 2.9 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5cc(C)ccc5[nH]4)nn3C)nc2n(CCC)c1=O 10.1021/jm201292w
CHEMBL1955903 71154 None 0 Human Binding pKi = 8.0 8.0 72 2
Displacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation countingDisplacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation counting
ChEMBL 476 8 2 9 2.9 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5cc(C)ccc5[nH]4)nn3C)nc2n(CCC)c1=O 10.1021/jm201292w
9904456 99148 None 0 Human Binding pKi = 8.0 8.0 -8 4
Displacement of [3H]- DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]- DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 301 2 1 9 1.6 CSc1c2c(nc(N)n3nc(-c4ccco4)nc23)nn1C 10.1021/jm021023m
CHEMBL281129 99148 None 0 Human Binding pKi = 8.0 8.0 -8 4
Displacement of [3H]- DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]- DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 301 2 1 9 1.6 CSc1c2c(nc(N)n3nc(-c4ccco4)nc23)nn1C 10.1021/jm021023m
449 2643 None 52 Human Binding pKi = 8.0 8.0 -1 9
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by liquid scintillation countingDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by liquid scintillation counting
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10.1016/j.ejmech.2012.05.033
453 2643 None 52 Human Binding pKi = 8.0 8.0 -1 9
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by liquid scintillation countingDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by liquid scintillation counting
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10.1016/j.ejmech.2012.05.033
6603931 2643 None 52 Human Binding pKi = 8.0 8.0 -1 9
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by liquid scintillation countingDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by liquid scintillation counting
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10.1016/j.ejmech.2012.05.033
CHEMBL273807 2643 None 52 Human Binding pKi = 8.0 8.0 -1 9
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by liquid scintillation countingDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by liquid scintillation counting
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10.1016/j.ejmech.2012.05.033
44451229 155197 None 0 Human Binding pKi = 8.0 8.0 77 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 620 9 1 9 5.0 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCN(c5nc6ccc(Cl)cc6s5)CC4)cc3)cc2n(CCC)c1=O 10.1016/j.bmc.2008.01.002
CHEMBL402474 155197 None 0 Human Binding pKi = 8.0 8.0 77 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 620 9 1 9 5.0 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCN(c5nc6ccc(Cl)cc6s5)CC4)cc3)cc2n(CCC)c1=O 10.1016/j.bmc.2008.01.002
69030712 157961 None 0 Human Binding pKi = 8.0 8.0 - 1
Displacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting methodDisplacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting method
ChEMBL 489 8 1 8 2.9 CCCn1c(=O)c2[nH]c(-c3cnn(CC4CC(=O)N(c5cccc(C)c5)C4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2016.11.007
CHEMBL4084760 157961 None 0 Human Binding pKi = 8.0 8.0 - 1
Displacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting methodDisplacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting method
ChEMBL 489 8 1 8 2.9 CCCn1c(=O)c2[nH]c(-c3cnn(CC4CC(=O)N(c5cccc(C)c5)C4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2016.11.007
44236419 159156 None 0 Human Binding pKi = 8.0 8.0 - 1
Displacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting methodDisplacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting method
ChEMBL 540 8 1 9 2.2 CCCn1c(=O)c2[nH]c(-c3cnn(CC(=O)N4CCN(c5ccc(F)cc5F)CC4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2016.11.007
CHEMBL4098199 159156 None 0 Human Binding pKi = 8.0 8.0 - 1
Displacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting methodDisplacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting method
ChEMBL 540 8 1 9 2.2 CCCn1c(=O)c2[nH]c(-c3cnn(CC(=O)N4CCN(c5ccc(F)cc5F)CC4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2016.11.007
11584027 139558 None 0 Human Binding pKi = 8.0 8.0 10 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 491 10 2 8 3.4 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(OC)nc4)cc3)cc2n(CCC)c1=O 10.1021/jm0506221
CHEMBL379688 139558 None 0 Human Binding pKi = 8.0 8.0 10 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 491 10 2 8 3.4 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(OC)nc4)cc3)cc2n(CCC)c1=O 10.1021/jm0506221
10981207 133525 None 0 Human Binding pKi = 8.0 8.0 7 4
Inhibition of [3H]ZM-241385 binding to human adenosine A2B receptorInhibition of [3H]ZM-241385 binding to human adenosine A2B receptor
ChEMBL 358 7 3 6 1.3 CCCCn1c(=O)[nH]c2[nH]c(-c3ccc(OCC(=O)O)cc3)nc2c1=O 10.1021/jm011049y
CHEMBL37082 133525 None 0 Human Binding pKi = 8.0 8.0 7 4
Inhibition of [3H]ZM-241385 binding to human adenosine A2B receptorInhibition of [3H]ZM-241385 binding to human adenosine A2B receptor
ChEMBL 358 7 3 6 1.3 CCCCn1c(=O)[nH]c2[nH]c(-c3ccc(OCC(=O)O)cc3)nc2c1=O 10.1021/jm011049y
11656570 73410 None 0 Human Binding pKi = 8.0 8.0 8 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 522 11 2 10 2.8 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4cc(OC)nc(OC)n4)cc3)cc2n(CCC)c1=O 10.1021/jm0506221
CHEMBL201594 73410 None 0 Human Binding pKi = 8.0 8.0 8 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 522 11 2 10 2.8 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4cc(OC)nc(OC)n4)cc3)cc2n(CCC)c1=O 10.1021/jm0506221
11632785 73536 None 0 Human Binding pKi = 8.0 8.0 13 4
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 404 5 2 6 2.3 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccccc4)cc3)cc2n(C)c1=O 10.1021/jm0506221
CHEMBL201721 73536 None 0 Human Binding pKi = 8.0 8.0 13 4
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 404 5 2 6 2.3 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccccc4)cc3)cc2n(C)c1=O 10.1021/jm0506221
44451254 156889 None 10 Human Binding pKi = 8.0 8.0 912 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 592 5 1 9 4.0 Cn1c(=O)c2[nH]c(-c3ccc(OC(C)(C)C(=O)N4CCN(c5nc6cc(Cl)ccc6s5)CC4)cc3)cc2n(C)c1=O 10.1016/j.bmc.2008.01.002
CHEMBL407204 156889 None 10 Human Binding pKi = 8.0 8.0 912 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 592 5 1 9 4.0 Cn1c(=O)c2[nH]c(-c3ccc(OC(C)(C)C(=O)N4CCN(c5nc6cc(Cl)ccc6s5)CC4)cc3)cc2n(C)c1=O 10.1016/j.bmc.2008.01.002
135529371 109185 None 0 Human Binding pKi = 7 7.0 8 2
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 479 9 2 9 2.3 CCCn1c(=O)c2nc(-c3cc(NC(=O)Cc4ccc(OC)cc4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
CHEMBL32150 109185 None 0 Human Binding pKi = 7 7.0 8 2
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 479 9 2 9 2.3 CCCn1c(=O)c2nc(-c3cc(NC(=O)Cc4ccc(OC)cc4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
11505071 72584 None 0 Human Binding pKi = 7 7.0 -1 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 566 10 3 11 1.7 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)c4c(NC(=O)O)n(C)c(=O)n(C)c4=O)cc3)cc2n(CCC)c1=O 10.1021/jm0506221
CHEMBL199280 72584 None 0 Human Binding pKi = 7 7.0 -1 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 566 10 3 11 1.7 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)c4c(NC(=O)O)n(C)c(=O)n(C)c4=O)cc3)cc2n(CCC)c1=O 10.1021/jm0506221
9844693 82207 None 0 Human Binding pKi = 7 7.0 -10 3
Displacement of [125I]3-(4-aminobenzyl)-8-phenyloxyacetate-1-propyl-xanthine from human adenosine A2B receptor expressed in HEK cellsDisplacement of [125I]3-(4-aminobenzyl)-8-phenyloxyacetate-1-propyl-xanthine from human adenosine A2B receptor expressed in HEK cells
ChEMBL 414 7 2 6 2.9 CCCn1c(=O)c2nc([C@]34CC[C@](/C=C/C(=O)O)(CC3)CC4)[nH]c2n(CCC)c1=O 10.1021/jm0605381
CHEMBL217076 82207 None 0 Human Binding pKi = 7 7.0 -10 3
Displacement of [125I]3-(4-aminobenzyl)-8-phenyloxyacetate-1-propyl-xanthine from human adenosine A2B receptor expressed in HEK cellsDisplacement of [125I]3-(4-aminobenzyl)-8-phenyloxyacetate-1-propyl-xanthine from human adenosine A2B receptor expressed in HEK cells
ChEMBL 414 7 2 6 2.9 CCCn1c(=O)c2nc([C@]34CC[C@](/C=C/C(=O)O)(CC3)CC4)[nH]c2n(CCC)c1=O 10.1021/jm0605381
137649458 157147 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 minsDisplacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 mins
ChEMBL 438 6 2 8 2.3 CCCn1c(=O)c2[nH]c(-c3cnn(CC#CC4(O)CCCCC4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2017.04.014
CHEMBL4075201 157147 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 minsDisplacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 mins
ChEMBL 438 6 2 8 2.3 CCCn1c(=O)c2[nH]c(-c3cnn(CC#CC4(O)CCCCC4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2017.04.014
44451165 158801 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 531 9 1 9 2.5 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCN(c5cnccn5)CC4)cc3)cc2n(CCC)c1=O 10.1016/j.bmc.2008.01.002
CHEMBL409440 158801 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 531 9 1 9 2.5 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCN(c5cnccn5)CC4)cc3)cc2n(CCC)c1=O 10.1016/j.bmc.2008.01.002
46837563 10590 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells after 30 minsDisplacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells after 30 mins
ChEMBL 436 7 3 5 3.3 CCCn1c(=O)[nH]c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(F)cc4)cc3)cc21 10.1016/j.ejmech.2010.03.011
CHEMBL1169969 10590 None 0 Human Binding pKi = 7 7.0 - 1
Displacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells after 30 minsDisplacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells after 30 mins
ChEMBL 436 7 3 5 3.3 CCCn1c(=O)[nH]c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(F)cc4)cc3)cc21 10.1016/j.ejmech.2010.03.011
44406567 72694 None 0 Human Binding pKi = 7 7.0 6 3
Displacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cellsDisplacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cells
ChEMBL 528 8 1 10 3.7 CCCn1c(=O)c2nc(-c3cnn(Cc4noc(-c5ccccc5C(F)(F)F)n4)c3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2005.10.002
CHEMBL199692 72694 None 0 Human Binding pKi = 7 7.0 6 3
Displacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cellsDisplacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cells
ChEMBL 528 8 1 10 3.7 CCCn1c(=O)c2nc(-c3cnn(Cc4noc(-c5ccccc5C(F)(F)F)n4)c3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2005.10.002
11618633 78124 None 0 Human Binding pKi = 7 7.0 -1 3
Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cellsDisplacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells
ChEMBL 420 9 1 7 3.2 CCCn1c(=O)c2nc(-c3cnn(CCCc4ccccc4)c3)[nH]c2n(CCC)c1=O 10.1021/jm051268+
CHEMBL210319 78124 None 0 Human Binding pKi = 7 7.0 -1 3
Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cellsDisplacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells
ChEMBL 420 9 1 7 3.2 CCCn1c(=O)c2nc(-c3cnn(CCCc4ccccc4)c3)[nH]c2n(CCC)c1=O 10.1021/jm051268+
10193 3010 None 40 Human Binding pKi = 6 6.0 -46 4
Antagonist activity at human adenosine A2b receptor expressed in HEK293 cells by radioligand competition binding assayAntagonist activity at human adenosine A2b receptor expressed in HEK293 cells by radioligand competition binding assay
ChEMBL 305 2 1 7 1.2 Nc1nc(nc(c1Br)n1cccn1)n1cccn1 10.1021/acs.jmedchem.0c00237
53466958 3010 None 40 Human Binding pKi = 6 6.0 -46 4
Antagonist activity at human adenosine A2b receptor expressed in HEK293 cells by radioligand competition binding assayAntagonist activity at human adenosine A2b receptor expressed in HEK293 cells by radioligand competition binding assay
ChEMBL 305 2 1 7 1.2 Nc1nc(nc(c1Br)n1cccn1)n1cccn1 10.1021/acs.jmedchem.0c00237
53466958.0 3010 None 40 Human Binding pKi = 6 6.0 -46 4
Antagonist activity at human adenosine A2b receptor expressed in HEK293 cells by radioligand competition binding assayAntagonist activity at human adenosine A2b receptor expressed in HEK293 cells by radioligand competition binding assay
ChEMBL 305 2 1 7 1.2 Nc1nc(nc(c1Br)n1cccn1)n1cccn1 10.1021/acs.jmedchem.0c00237
CHEMBL3638684 3010 None 40 Human Binding pKi = 6 6.0 -46 4
Antagonist activity at human adenosine A2b receptor expressed in HEK293 cells by radioligand competition binding assayAntagonist activity at human adenosine A2b receptor expressed in HEK293 cells by radioligand competition binding assay
ChEMBL 305 2 1 7 1.2 Nc1nc(nc(c1Br)n1cccn1)n1cccn1 10.1021/acs.jmedchem.0c00237
CHEMBL3694769 3010 None 40 Human Binding pKi = 6 6.0 -46 4
Antagonist activity at human adenosine A2b receptor expressed in HEK293 cells by radioligand competition binding assayAntagonist activity at human adenosine A2b receptor expressed in HEK293 cells by radioligand competition binding assay
ChEMBL 305 2 1 7 1.2 Nc1nc(nc(c1Br)n1cccn1)n1cccn1 10.1021/acs.jmedchem.0c00237
155521637 170667 None 0 Human Binding pKi = 6 6.0 -25 3
Displacement of [3H]DPCPX from human A2B receptor expressed in HEK-293-A2B cells incubated for 30 mins by scintillation counting method based radioligand competitive binding assayDisplacement of [3H]DPCPX from human A2B receptor expressed in HEK-293-A2B cells incubated for 30 mins by scintillation counting method based radioligand competitive binding assay
ChEMBL 313 2 1 4 3.7 Clc1cccc(-c2nc(N3CCCCC3)c3nc[nH]c3n2)c1 10.1016/j.bmc.2019.06.034
CHEMBL4451553 170667 None 0 Human Binding pKi = 6 6.0 -25 3
Displacement of [3H]DPCPX from human A2B receptor expressed in HEK-293-A2B cells incubated for 30 mins by scintillation counting method based radioligand competitive binding assayDisplacement of [3H]DPCPX from human A2B receptor expressed in HEK-293-A2B cells incubated for 30 mins by scintillation counting method based radioligand competitive binding assay
ChEMBL 313 2 1 4 3.7 Clc1cccc(-c2nc(N3CCCCC3)c3nc[nH]c3n2)c1 10.1016/j.bmc.2019.06.034
70686119 75447 None 0 Human Binding pKi = 6 6.0 -1 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by beta scintillation countingDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by beta scintillation counting
ChEMBL 338 5 3 5 2.4 COc1cccc2cc(C(=O)NCC(O)c3ccccc3)c(=N)oc12 10.1016/j.ejmech.2012.05.009
CHEMBL2042072 75447 None 0 Human Binding pKi = 6 6.0 -1 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by beta scintillation countingDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by beta scintillation counting
ChEMBL 338 5 3 5 2.4 COc1cccc2cc(C(=O)NCC(O)c3ccccc3)c(=N)oc12 10.1016/j.ejmech.2012.05.009
6032251 75455 None 3 Human Binding pKi = 6 6.0 -3 3
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by beta scintillation countingDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by beta scintillation counting
ChEMBL 233 3 1 5 1.5 COC(=O)/C(C#N)=C/c1cccc(OC)c1O 10.1016/j.ejmech.2012.05.009
CHEMBL2042091 75455 None 3 Human Binding pKi = 6 6.0 -3 3
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by beta scintillation countingDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by beta scintillation counting
ChEMBL 233 3 1 5 1.5 COC(=O)/C(C#N)=C/c1cccc(OC)c1O 10.1016/j.ejmech.2012.05.009
2989630 104034 None 13 Human Binding pKi = 5 5.0 -67 5
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 329 1 0 7 1.1 Cn1c(=O)c2c(nc3n2CCCN3c2ccc(F)cc2)n(C)c1=O 10.1016/j.bmc.2013.09.044
CHEMBL3093328 104034 None 13 Human Binding pKi = 5 5.0 -67 5
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 329 1 0 7 1.1 Cn1c(=O)c2c(nc3n2CCCN3c2ccc(F)cc2)n(C)c1=O 10.1016/j.bmc.2013.09.044
137632333 156531 None 0 Human Binding pKi = 5 5.0 -1348 4
Displacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes measured after 90 minsDisplacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes measured after 90 mins
ChEMBL 445 6 1 7 4.1 COc1ccc(N2CCOCC2)c2sc(NC(=O)C(C)(C)Oc3ccc(F)cc3)nc12 10.1021/acs.jmedchem.6b01584
CHEMBL4068032 156531 None 0 Human Binding pKi = 5 5.0 -1348 4
Displacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes measured after 90 minsDisplacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes measured after 90 mins
ChEMBL 445 6 1 7 4.1 COc1ccc(N2CCOCC2)c2sc(NC(=O)C(C)(C)Oc3ccc(F)cc3)nc12 10.1021/acs.jmedchem.6b01584
70688247 75443 None 0 Human Binding pKi = 5 5.0 -25 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by beta scintillation countingDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by beta scintillation counting
ChEMBL 476 8 4 8 2.7 COc1cccc2cc(C(=O)NCCCNC(=O)c3cc4cccc(OC)c4oc3=N)c(=N)oc12 10.1016/j.ejmech.2012.05.009
CHEMBL2042060 75443 None 0 Human Binding pKi = 5 5.0 -25 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by beta scintillation countingDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by beta scintillation counting
ChEMBL 476 8 4 8 2.7 COc1cccc2cc(C(=O)NCCCNC(=O)c3cc4cccc(OC)c4oc3=N)c(=N)oc12 10.1016/j.ejmech.2012.05.009
70683991 75444 None 0 Human Binding pKi = 5 5.0 -31 3
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by beta scintillation countingDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by beta scintillation counting
ChEMBL 602 12 4 10 2.7 COc1cccc2cc(C(=O)NCCCN3CCN(CCCNC(=O)c4cc5cccc(OC)c5oc4=N)CC3)c(=N)oc12 10.1016/j.ejmech.2012.05.009
CHEMBL2042061 75444 None 0 Human Binding pKi = 5 5.0 -31 3
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by beta scintillation countingDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by beta scintillation counting
ChEMBL 602 12 4 10 2.7 COc1cccc2cc(C(=O)NCCCN3CCN(CCCNC(=O)c4cc5cccc(OC)c5oc4=N)CC3)c(=N)oc12 10.1016/j.ejmech.2012.05.009
2989630 104034 None 13 Human Binding pKi = 5 5.0 -67 5
Displacement of [3H]PSB-603 from human adenosine A2B receptorDisplacement of [3H]PSB-603 from human adenosine A2B receptor
ChEMBL 329 1 0 7 1.1 Cn1c(=O)c2c(nc3n2CCCN3c2ccc(F)cc2)n(C)c1=O 10.1016/j.bmc.2013.09.044
CHEMBL3093328 104034 None 13 Human Binding pKi = 5 5.0 -67 5
Displacement of [3H]PSB-603 from human adenosine A2B receptorDisplacement of [3H]PSB-603 from human adenosine A2B receptor
ChEMBL 329 1 0 7 1.1 Cn1c(=O)c2c(nc3n2CCCN3c2ccc(F)cc2)n(C)c1=O 10.1016/j.bmc.2013.09.044
11081 3217 None 5 Human Binding pKi = 5 5.0 -30 6
Displacement of [3H]ZM-241385 from human adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]ZM-241385 from human adenosine A2B receptor expressed in CHO cells
ChEMBL 378 3 1 7 1.4 Cn1c(=O)n(C)c(=O)c2c1nc1n2CCCN1CCc1c[nH]c2c1cccc2 10.1016/j.bmc.2007.07.051
44437220 3217 None 5 Human Binding pKi = 5 5.0 -30 6
Displacement of [3H]ZM-241385 from human adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]ZM-241385 from human adenosine A2B receptor expressed in CHO cells
ChEMBL 378 3 1 7 1.4 Cn1c(=O)n(C)c(=O)c2c1nc1n2CCCN1CCc1c[nH]c2c1cccc2 10.1016/j.bmc.2007.07.051
CHEMBL239232 3217 None 5 Human Binding pKi = 5 5.0 -30 6
Displacement of [3H]ZM-241385 from human adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]ZM-241385 from human adenosine A2B receptor expressed in CHO cells
ChEMBL 378 3 1 7 1.4 Cn1c(=O)n(C)c(=O)c2c1nc1n2CCCN1CCc1c[nH]c2c1cccc2 10.1016/j.bmc.2007.07.051
3162488 91144 None 10 Human Binding pKi = 5 5.0 -31 5
Displacement of [3H]ZM-241385 from human adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]ZM-241385 from human adenosine A2B receptor expressed in CHO cells
ChEMBL 339 3 0 7 0.9 Cn1c(=O)c2c(nc3n2CCCN3CCc2ccccc2)n(C)c1=O 10.1016/j.bmc.2007.07.051
CHEMBL239864 91144 None 10 Human Binding pKi = 5 5.0 -31 5
Displacement of [3H]ZM-241385 from human adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]ZM-241385 from human adenosine A2B receptor expressed in CHO cells
ChEMBL 339 3 0 7 0.9 Cn1c(=O)c2c(nc3n2CCCN3CCc2ccccc2)n(C)c1=O 10.1016/j.bmc.2007.07.051
11003653 145838 None 0 Human Binding pKi = 5 5.0 -2 4
Displacement of [3H]ZM-241385 from human adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]ZM-241385 from human adenosine A2B receptor expressed in CHO cells
ChEMBL 389 4 0 8 1.4 Cn1c(=O)c2c(nc3n2CCCN3CCOc2ccc(Cl)cc2)n(C)c1=O 10.1016/j.bmc.2007.07.051
CHEMBL391718 145838 None 0 Human Binding pKi = 5 5.0 -2 4
Displacement of [3H]ZM-241385 from human adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]ZM-241385 from human adenosine A2B receptor expressed in CHO cells
ChEMBL 389 4 0 8 1.4 Cn1c(=O)c2c(nc3n2CCCN3CCOc2ccc(Cl)cc2)n(C)c1=O 10.1016/j.bmc.2007.07.051
2519 779 None 86 Human Binding pKi = 5 5.0 -11 12
Inhibition of human A2B adenosine receptorInhibition of human A2B adenosine receptor
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1016/j.ejmech.2018.11.045
2519.0 779 None 86 Human Binding pKi = 5 5.0 -11 12
Inhibition of human A2B adenosine receptorInhibition of human A2B adenosine receptor
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1016/j.ejmech.2018.11.045
407 779 None 86 Human Binding pKi = 5 5.0 -11 12
Inhibition of human A2B adenosine receptorInhibition of human A2B adenosine receptor
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1016/j.ejmech.2018.11.045
463 779 None 86 Human Binding pKi = 5 5.0 -11 12
Inhibition of human A2B adenosine receptorInhibition of human A2B adenosine receptor
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1016/j.ejmech.2018.11.045
CHEMBL113 779 None 86 Human Binding pKi = 5 5.0 -11 12
Inhibition of human A2B adenosine receptorInhibition of human A2B adenosine receptor
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1016/j.ejmech.2018.11.045
DB00201 779 None 86 Human Binding pKi = 5 5.0 -11 12
Inhibition of human A2B adenosine receptorInhibition of human A2B adenosine receptor
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1016/j.ejmech.2018.11.045
3280 4062 None 43 Human Binding pKi = 5 5.0 -245 4
Percent displacement of [3H]DPCPX binding in human adenosine A2B receptor expressed in COS-7 cellsPercent displacement of [3H]DPCPX binding in human adenosine A2B receptor expressed in COS-7 cells
ChEMBL 371 4 2 5 4.3 COc1ccccc1NC(=O)Nc1nc(nc2c1cccc2)c1cccnc1 10.1021/jm0003945
4046493 4062 None 43 Human Binding pKi = 5 5.0 -245 4
Percent displacement of [3H]DPCPX binding in human adenosine A2B receptor expressed in COS-7 cellsPercent displacement of [3H]DPCPX binding in human adenosine A2B receptor expressed in COS-7 cells
ChEMBL 371 4 2 5 4.3 COc1ccccc1NC(=O)Nc1nc(nc2c1cccc2)c1cccnc1 10.1021/jm0003945
CHEMBL70880 4062 None 43 Human Binding pKi = 5 5.0 -245 4
Percent displacement of [3H]DPCPX binding in human adenosine A2B receptor expressed in COS-7 cellsPercent displacement of [3H]DPCPX binding in human adenosine A2B receptor expressed in COS-7 cells
ChEMBL 371 4 2 5 4.3 COc1ccccc1NC(=O)Nc1nc(nc2c1cccc2)c1cccnc1 10.1021/jm0003945
162677251 183537 None 0 Human Binding pKi = 6 6.0 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 278 4 2 3 3.0 CC1=C(C(=O)CC(C)C)C(c2ccsc2)NC(=O)N1 10.1021/acs.jmedchem.0c01431
CHEMBL4800076 183537 None 0 Human Binding pKi = 6 6.0 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 278 4 2 3 3.0 CC1=C(C(=O)CC(C)C)C(c2ccsc2)NC(=O)N1 10.1021/acs.jmedchem.0c01431
162643106 181655 None 0 Human Binding pKi = 6 6.0 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 262 4 2 3 2.5 CC1=C(C(=O)CC(C)C)C(c2ccoc2)NC(=O)N1 10.1021/acs.jmedchem.0c01431
CHEMBL4776088 181655 None 0 Human Binding pKi = 6 6.0 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 262 4 2 3 2.5 CC1=C(C(=O)CC(C)C)C(c2ccoc2)NC(=O)N1 10.1021/acs.jmedchem.0c01431
162673336 183145 None 0 Human Binding pKi = 6 6.0 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 290 3 2 4 2.4 CC1=C(C(=O)OC2CCCC2)C(c2ccoc2)NC(=O)N1 10.1021/acs.jmedchem.0c01431
CHEMBL4795209 183145 None 0 Human Binding pKi = 6 6.0 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 290 3 2 4 2.4 CC1=C(C(=O)OC2CCCC2)C(c2ccoc2)NC(=O)N1 10.1021/acs.jmedchem.0c01431
11811761 56550 None 0 Human Binding pKi = 7 7.0 -8 4
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 89-116Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 89-116
ChEMBL 415 7 1 8 3.7 CCCCn1cc2c(nc(NC(=O)Cc3ccccc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm0109614
CHEMBL163968 56550 None 0 Human Binding pKi = 7 7.0 -8 4
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 89-116Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 89-116
ChEMBL 415 7 1 8 3.7 CCCCn1cc2c(nc(NC(=O)Cc3ccccc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm0109614
10927693 56751 None 0 Human Binding pKi = 7 7.0 -3 4
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 89-116Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 89-116
ChEMBL 408 3 2 8 3.6 Cn1cc2c(nc(NC(=O)Nc3ccccc3Cl)n3nc(-c4ccco4)nc23)n1 10.1021/jm0109614
CHEMBL164281 56751 None 0 Human Binding pKi = 7 7.0 -3 4
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 89-116Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 89-116
ChEMBL 408 3 2 8 3.6 Cn1cc2c(nc(NC(=O)Nc3ccccc3Cl)n3nc(-c4ccco4)nc23)n1 10.1021/jm0109614
11661440 79853 None 0 Human Binding pKi = 7 7.0 1 3
Displacement of [3H]PSB298 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB298 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 407 7 4 7 -0.1 CCCn1c(=O)[nH]c2[nH]c(-c3ccc(S(=O)(=O)NCC(=O)O)cc3)nc2c1=O 10.1021/jm060277v
CHEMBL212217 79853 None 0 Human Binding pKi = 7 7.0 1 3
Displacement of [3H]PSB298 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB298 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 407 7 4 7 -0.1 CCCn1c(=O)[nH]c2[nH]c(-c3ccc(S(=O)(=O)NCC(=O)O)cc3)nc2c1=O 10.1021/jm060277v
44390615 122629 None 0 Human Binding pKi = 6 6.0 - 1
Binding affinity for adenosine A2b receptor by using as [3H]ZM-241385 (14 nM) radioligand in membranes from HEK-A2B cellsBinding affinity for adenosine A2b receptor by using as [3H]ZM-241385 (14 nM) radioligand in membranes from HEK-A2B cells
ChEMBL 554 9 1 9 5.0 CCCn1c(=O)c2nc(-c3ccc(OCc4noc(-c5cccc(C(F)(F)F)c5)n4)cc3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2004.11.044
CHEMBL360366 122629 None 0 Human Binding pKi = 6 6.0 - 1
Binding affinity for adenosine A2b receptor by using as [3H]ZM-241385 (14 nM) radioligand in membranes from HEK-A2B cellsBinding affinity for adenosine A2b receptor by using as [3H]ZM-241385 (14 nM) radioligand in membranes from HEK-A2B cells
ChEMBL 554 9 1 9 5.0 CCCn1c(=O)c2nc(-c3ccc(OCc4noc(-c5cccc(C(F)(F)F)c5)n4)cc3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2004.11.044
136002185 168180 None 0 Human Binding pKi = 6 6.0 - 1
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 480 9 2 10 1.8 CCCn1c(=O)c2nc(-c3cc(OCC(=O)Nc4ccc(C)cn4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
CHEMBL433235 168180 None 0 Human Binding pKi = 6 6.0 - 1
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 480 9 2 10 1.8 CCCn1c(=O)c2nc(-c3cc(OCC(=O)Nc4ccc(C)cn4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
137640212 156966 None 0 Human Binding pKi = 7.0 7.0 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes after 30 minsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes after 30 mins
ChEMBL 274 3 2 5 1.2 CCOC(=O)C1=C(C)N/C(=N\C#N)NC1c1ccoc1 10.1021/acs.jmedchem.7b00138
CHEMBL4072891 156966 None 0 Human Binding pKi = 7.0 7.0 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes after 30 minsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes after 30 mins
ChEMBL 274 3 2 5 1.2 CCOC(=O)C1=C(C)N/C(=N\C#N)NC1c1ccoc1 10.1021/acs.jmedchem.7b00138
11567017 79953 None 0 Human Binding pKi = 7.0 7.0 -1 3
Displacement of [3H]PSB298 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB298 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 377 4 2 7 0.3 CC(C)NS(=O)(=O)c1ccc(-c2nc3c(=O)n(C)c(=O)n(C)c3[nH]2)cc1 10.1021/jm060277v
CHEMBL212626 79953 None 0 Human Binding pKi = 7.0 7.0 -1 3
Displacement of [3H]PSB298 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB298 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 377 4 2 7 0.3 CC(C)NS(=O)(=O)c1ccc(-c2nc3c(=O)n(C)c(=O)n(C)c3[nH]2)cc1 10.1021/jm060277v
11821203 203097 None 5 Human Binding pKi = 5.0 5.0 -6 5
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 256 2 1 5 0.5 Cn1c(=O)n(Cc2ccccc2)c(=O)c2[nH]cnc21 10.1021/jm0104318
CHEMBL63944 203097 None 5 Human Binding pKi = 5.0 5.0 -6 5
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 256 2 1 5 0.5 Cn1c(=O)n(Cc2ccccc2)c(=O)c2[nH]cnc21 10.1021/jm0104318
11821203 203097 None 5 Rat Binding pKi = 5.0 5.0 -6 5
Inhibition of [125I]-APOBX binding to rat Adenosine A2B receptor expressed in HEK cellsInhibition of [125I]-APOBX binding to rat Adenosine A2B receptor expressed in HEK cells
ChEMBL 256 2 1 5 0.5 Cn1c(=O)n(Cc2ccccc2)c(=O)c2[nH]cnc21 10.1021/jm0104318
CHEMBL63944 203097 None 5 Rat Binding pKi = 5.0 5.0 -6 5
Inhibition of [125I]-APOBX binding to rat Adenosine A2B receptor expressed in HEK cellsInhibition of [125I]-APOBX binding to rat Adenosine A2B receptor expressed in HEK cells
ChEMBL 256 2 1 5 0.5 Cn1c(=O)n(Cc2ccccc2)c(=O)c2[nH]cnc21 10.1021/jm0104318
9928335 120097 None 2 Rat Binding pKi = 6.0 6.0 -28 6
In vivo binding affinity was evaluated against Alpha-2 adrenergic receptorIn vivo binding affinity was evaluated against Alpha-2 adrenergic receptor
ChEMBL 349 4 1 3 3.3 Cc1ccc(N2CCN(CC[C@H]3NC(=O)c4ccccc43)CC2)cc1C 10.1016/s0960-894x(98)00252-2
CHEMBL35093 120097 None 2 Rat Binding pKi = 6.0 6.0 -28 6
In vivo binding affinity was evaluated against Alpha-2 adrenergic receptorIn vivo binding affinity was evaluated against Alpha-2 adrenergic receptor
ChEMBL 349 4 1 3 3.3 Cc1ccc(N2CCN(CC[C@H]3NC(=O)c4ccccc43)CC2)cc1C 10.1016/s0960-894x(98)00252-2
135493272 111457 None 0 Human Binding pKi = 7.0 7.0 - 1
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 465 8 3 9 2.0 CCCn1c(=O)c2nc(-c3cc(NC(=O)Cc4ccc(O)cc4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
CHEMBL32757 111457 None 0 Human Binding pKi = 7.0 7.0 - 1
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 465 8 3 9 2.0 CCCn1c(=O)c2nc(-c3cc(NC(=O)Cc4ccc(O)cc4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
135464144 112997 None 0 Human Binding pKi = 6.0 6.0 -5623 4
Inhibition of [3H]DPCPX binding to human Adenosine A2B receptor expressed in HEK cells; Range 772-1390Inhibition of [3H]DPCPX binding to human Adenosine A2B receptor expressed in HEK cells; Range 772-1390
ChEMBL 322 5 1 6 3.0 CCCCc1nc2[nH]cnc2c2nc(-c3ccc(OC)cc3)nn12 10.1021/jm010570p
CHEMBL331111 112997 None 0 Human Binding pKi = 6.0 6.0 -5623 4
Inhibition of [3H]DPCPX binding to human Adenosine A2B receptor expressed in HEK cells; Range 772-1390Inhibition of [3H]DPCPX binding to human Adenosine A2B receptor expressed in HEK cells; Range 772-1390
ChEMBL 322 5 1 6 3.0 CCCCc1nc2[nH]cnc2c2nc(-c3ccc(OC)cc3)nn12 10.1021/jm010570p
156017083 177679 None 0 Human Binding pKi = 6.0 6.0 - 1
Displacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting methodDisplacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting method
ChEMBL 338 3 1 7 3.3 CC1=C(C(=O)OC(C)C)C(c2ccno2)n2c(nc3ccccc32)N1 10.1021/acs.jmedchem.0c00564
CHEMBL4641788 177679 None 0 Human Binding pKi = 6.0 6.0 - 1
Displacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting methodDisplacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting method
ChEMBL 338 3 1 7 3.3 CC1=C(C(=O)OC(C)C)C(c2ccno2)n2c(nc3ccccc32)N1 10.1021/acs.jmedchem.0c00564
2519 779 None 86 Human Binding pKi = 5.0 5.0 -11 12
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1021/jm0104318
2519.0 779 None 86 Human Binding pKi = 5.0 5.0 -11 12
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1021/jm0104318
407 779 None 86 Human Binding pKi = 5.0 5.0 -11 12
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1021/jm0104318
463 779 None 86 Human Binding pKi = 5.0 5.0 -11 12
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1021/jm0104318
CHEMBL113 779 None 86 Human Binding pKi = 5.0 5.0 -11 12
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1021/jm0104318
DB00201 779 None 86 Human Binding pKi = 5.0 5.0 -11 12
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1021/jm0104318
2519 779 None 86 Human Binding pKi = 5.0 5.0 -11 12
Displacement of [125I]I-ABOPX from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [125I]I-ABOPX from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1021/jm900413e
2519.0 779 None 86 Human Binding pKi = 5.0 5.0 -11 12
Displacement of [125I]I-ABOPX from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [125I]I-ABOPX from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1021/jm900413e
407 779 None 86 Human Binding pKi = 5.0 5.0 -11 12
Displacement of [125I]I-ABOPX from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [125I]I-ABOPX from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1021/jm900413e
463 779 None 86 Human Binding pKi = 5.0 5.0 -11 12
Displacement of [125I]I-ABOPX from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [125I]I-ABOPX from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1021/jm900413e
CHEMBL113 779 None 86 Human Binding pKi = 5.0 5.0 -11 12
Displacement of [125I]I-ABOPX from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [125I]I-ABOPX from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1021/jm900413e
DB00201 779 None 86 Human Binding pKi = 5.0 5.0 -11 12
Displacement of [125I]I-ABOPX from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [125I]I-ABOPX from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1021/jm900413e
162668237 182505 None 0 Human Binding pKi = 6.0 6.0 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 306 4 2 4 2.7 CC1=C(C(=O)OCC2CCC2)C(c2ccsc2)NC(=O)N1 10.1021/acs.jmedchem.0c01431
CHEMBL4786993 182505 None 0 Human Binding pKi = 6.0 6.0 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 306 4 2 4 2.7 CC1=C(C(=O)OCC2CCC2)C(c2ccsc2)NC(=O)N1 10.1021/acs.jmedchem.0c01431
46837564 10591 None 1 Human Binding pKi = 6.0 6.0 - 1
Displacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells after 30 minsDisplacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells after 30 mins
ChEMBL 418 7 3 5 3.1 CCCn1c(=O)[nH]c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccccc4)cc3)cc21 10.1016/j.ejmech.2010.03.011
CHEMBL1169970 10591 None 1 Human Binding pKi = 6.0 6.0 - 1
Displacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells after 30 minsDisplacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells after 30 mins
ChEMBL 418 7 3 5 3.1 CCCn1c(=O)[nH]c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccccc4)cc3)cc21 10.1016/j.ejmech.2010.03.011
52948915 19295 None 0 Human Binding pKi = 7.0 7.0 33 2
Displacement of [3H]ZM241385 from human adenosine A2B receptor transfected in CHO cells after 60 mins by scintillation countingDisplacement of [3H]ZM241385 from human adenosine A2B receptor transfected in CHO cells after 60 mins by scintillation counting
ChEMBL 541 9 2 5 6.0 CC(C)(NC(=O)COc1ccc2[nH]c(=O)c(-c3nccs3)c(CCc3ccc(F)cc3)c2c1)c1ccccc1 10.1016/j.bmcl.2010.10.030
CHEMBL1290437 19295 None 0 Human Binding pKi = 7.0 7.0 33 2
Displacement of [3H]ZM241385 from human adenosine A2B receptor transfected in CHO cells after 60 mins by scintillation countingDisplacement of [3H]ZM241385 from human adenosine A2B receptor transfected in CHO cells after 60 mins by scintillation counting
ChEMBL 541 9 2 5 6.0 CC(C)(NC(=O)COc1ccc2[nH]c(=O)c(-c3nccs3)c(CCc3ccc(F)cc3)c2c1)c1ccccc1 10.1016/j.bmcl.2010.10.030
44406556 134361 None 0 Human Binding pKi = 7.0 7.0 14 3
Displacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cellsDisplacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cells
ChEMBL 490 9 1 11 2.7 CCCn1c(=O)c2nc(-c3cnn(Cc4nc(-c5ccc(OC)cc5)no4)c3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2005.10.002
CHEMBL371731 134361 None 0 Human Binding pKi = 7.0 7.0 14 3
Displacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cellsDisplacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cells
ChEMBL 490 9 1 11 2.7 CCCn1c(=O)c2nc(-c3cnn(Cc4nc(-c5ccc(OC)cc5)no4)c3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2005.10.002
162663910 182057 None 0 Human Binding pKi = 6.0 6.0 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 246 3 2 3 1.9 CC1=C(C(=O)C2CC2)C(c2ccco2)NC(=O)N1 10.1021/acs.jmedchem.0c01431
CHEMBL4781313 182057 None 0 Human Binding pKi = 6.0 6.0 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 246 3 2 3 1.9 CC1=C(C(=O)C2CC2)C(c2ccco2)NC(=O)N1 10.1021/acs.jmedchem.0c01431
CHEMBL5070276 214230 None 0 Human Binding pKi = 7.0 7.0 -16 3
Displacement of [3H]DPCPX from human A2BAR expressed in HEK293 cell membrane incubated for 30 mins by microbeta trilux scintillation counter analysisDisplacement of [3H]DPCPX from human A2BAR expressed in HEK293 cell membrane incubated for 30 mins by microbeta trilux scintillation counter analysis
ChEMBL None None None N#Cc1c(-c2ccccc2)nc(Nc2ccccc2)nc1-c1ccccc1F 10.1021/acs.jmedchem.1c01636
10175278 170384 None 0 Human Binding pKi = 7.0 7.0 - 1
Binding affinity of compound for displacement of [3H]DPCPX binding in HEK293 membranes expressing human A2B adenosine receptorsBinding affinity of compound for displacement of [3H]DPCPX binding in HEK293 membranes expressing human A2B adenosine receptors
ChEMBL 588 9 2 8 3.4 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccc(I)cc4)nc3)[nH]c2n(CCC)c1=O 10.1021/jm0309654
CHEMBL444787 170384 None 0 Human Binding pKi = 7.0 7.0 - 1
Binding affinity of compound for displacement of [3H]DPCPX binding in HEK293 membranes expressing human A2B adenosine receptorsBinding affinity of compound for displacement of [3H]DPCPX binding in HEK293 membranes expressing human A2B adenosine receptors
ChEMBL 588 9 2 8 3.4 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccc(I)cc4)nc3)[nH]c2n(CCC)c1=O 10.1021/jm0309654
10175278 170384 None 0 Human Binding pKi = 7.0 7.0 - 1
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 588 9 2 8 3.4 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccc(I)cc4)nc3)[nH]c2n(CCC)c1=O 10.1021/jm0309654
CHEMBL444787 170384 None 0 Human Binding pKi = 7.0 7.0 - 1
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 588 9 2 8 3.4 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccc(I)cc4)nc3)[nH]c2n(CCC)c1=O 10.1021/jm0309654
127034213 139127 None 0 Human Binding pKi = 7.0 7.0 - 1
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 minsDisplacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 mins
ChEMBL 273 3 1 6 2.3 CCOC(=O)C1=C(C)Nc2nccn2C1c1ccco1 10.1021/acs.jmedchem.5b01586
CHEMBL3786936 139127 None 0 Human Binding pKi = 7.0 7.0 - 1
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 minsDisplacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 mins
ChEMBL 273 3 1 6 2.3 CCOC(=O)C1=C(C)Nc2nccn2C1c1ccco1 10.1021/acs.jmedchem.5b01586
44520941 202030 None 0 Human Binding pKi = 6.0 6.0 -275 4
Displacement of radioligand from human adenosine A2B receptor expressed in cells by topcount microplate scintillation countingDisplacement of radioligand from human adenosine A2B receptor expressed in cells by topcount microplate scintillation counting
ChEMBL 309 4 2 6 2.0 Cc1ccc(-c2cc(C(=O)NCc3ccccn3)nc(N)n2)o1 10.1016/j.bmc.2009.07.078
CHEMBL608383 202030 None 0 Human Binding pKi = 6.0 6.0 -275 4
Displacement of radioligand from human adenosine A2B receptor expressed in cells by topcount microplate scintillation countingDisplacement of radioligand from human adenosine A2B receptor expressed in cells by topcount microplate scintillation counting
ChEMBL 309 4 2 6 2.0 Cc1ccc(-c2cc(C(=O)NCc3ccccn3)nc(N)n2)o1 10.1016/j.bmc.2009.07.078
127043828 141125 None 0 Human Binding pKi = 7.0 7.0 -1 7
Displacement of [3H]PSB-603 from recombinant human adenosine receptor A2b expressed in CHO cell membranesDisplacement of [3H]PSB-603 from recombinant human adenosine receptor A2b expressed in CHO cell membranes
ChEMBL 538 15 0 9 4.1 CCCCn1c(=O)c2c(nc3n2CCCN3CCc2ccc(OCCN(CC)CC)cc2)n(CCCC)c1=O 10.1016/j.bmc.2016.07.028
CHEMBL3827331 141125 None 0 Human Binding pKi = 7.0 7.0 -1 7
Displacement of [3H]PSB-603 from recombinant human adenosine receptor A2b expressed in CHO cell membranesDisplacement of [3H]PSB-603 from recombinant human adenosine receptor A2b expressed in CHO cell membranes
ChEMBL 538 15 0 9 4.1 CCCCn1c(=O)c2c(nc3n2CCCN3CCc2ccc(OCCN(CC)CC)cc2)n(CCCC)c1=O 10.1016/j.bmc.2016.07.028
9901260 190089 None 0 Human Binding pKi = 7.0 7.0 -40 4
Displacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation countingDisplacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation counting
ChEMBL 310 3 1 7 2.3 Nc1nc(-c2ccco2)c2nnn(Cc3ccccc3F)c2n1 10.1021/jm800961g
CHEMBL517278 190089 None 0 Human Binding pKi = 7.0 7.0 -40 4
Displacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation countingDisplacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation counting
ChEMBL 310 3 1 7 2.3 Nc1nc(-c2ccco2)c2nnn(Cc3ccccc3F)c2n1 10.1021/jm800961g
168297723 192452 None 0 Human Binding pKi = 7.0 7.0 - 1
Displacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cell membrane and measured after 0.5 hrs by radioligand displacement assayDisplacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cell membrane and measured after 0.5 hrs by radioligand displacement assay
ChEMBL 327 4 2 6 2.2 CCCn1c(=O)[nH]c2nc(-c3cccc(N=C=S)c3)[nH]c2c1=O 10.1039/d2md00132b
CHEMBL5208506 192452 None 0 Human Binding pKi = 7.0 7.0 - 1
Displacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cell membrane and measured after 0.5 hrs by radioligand displacement assayDisplacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cell membrane and measured after 0.5 hrs by radioligand displacement assay
ChEMBL 327 4 2 6 2.2 CCCn1c(=O)[nH]c2nc(-c3cccc(N=C=S)c3)[nH]c2c1=O 10.1039/d2md00132b
162664587 182061 None 0 Human Binding pKi = 6.0 6.0 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 292 3 2 4 2.5 CC1=C(C(=O)OC2CCC2)C(c2cccs2)NC(=O)N1 10.1021/acs.jmedchem.0c01431
CHEMBL4781342 182061 None 0 Human Binding pKi = 6.0 6.0 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 292 3 2 4 2.5 CC1=C(C(=O)OC2CCC2)C(c2cccs2)NC(=O)N1 10.1021/acs.jmedchem.0c01431
44583035 172741 None 0 Human Binding pKi = 8.0 8.0 7 4
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 593 5 1 10 3.4 Cn1c(=O)c2[nH]c(-c3ccc(OC(C)(C)C(=O)N4CCN(c5nc6cc(Cl)ccc6s5)CC4)cc3)nc2n(C)c1=O 10.1021/jm900413e
CHEMBL450826 172741 None 0 Human Binding pKi = 8.0 8.0 7 4
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 593 5 1 10 3.4 Cn1c(=O)c2[nH]c(-c3ccc(OC(C)(C)C(=O)N4CCN(c5nc6cc(Cl)ccc6s5)CC4)cc3)nc2n(C)c1=O 10.1021/jm900413e
9821879 94984 None 14 Human Binding pKi = 8.0 8.0 6 4
Displacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranesDisplacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranes
ChEMBL 392 7 1 7 2.6 CCCn1c(=O)c2[nH]c(-c3cnn(Cc4ccccc4)c3)nc2n(CCC)c1=O 10.1016/j.bmcl.2008.01.008
CHEMBL254725 94984 None 14 Human Binding pKi = 8.0 8.0 6 4
Displacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranesDisplacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranes
ChEMBL 392 7 1 7 2.6 CCCn1c(=O)c2[nH]c(-c3cnn(Cc4ccccc4)c3)nc2n(CCC)c1=O 10.1016/j.bmcl.2008.01.008
21958593 155501 None 0 Human Binding pKi = 8.0 8.0 14 4
Displacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranesDisplacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranes
ChEMBL 368 5 2 6 1.9 CCCn1c(=O)[nH]c2nc(-c3cnn(Cc4cccc(F)c4)c3)[nH]c2c1=O 10.1016/j.bmcl.2008.01.008
CHEMBL404131 155501 None 0 Human Binding pKi = 8.0 8.0 14 4
Displacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranesDisplacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranes
ChEMBL 368 5 2 6 1.9 CCCn1c(=O)[nH]c2nc(-c3cnn(Cc4cccc(F)c4)c3)[nH]c2c1=O 10.1016/j.bmcl.2008.01.008
44451254 156889 None 10 Human Binding pKi = 8.0 8.0 912 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 592 5 1 9 4.0 Cn1c(=O)c2[nH]c(-c3ccc(OC(C)(C)C(=O)N4CCN(c5nc6cc(Cl)ccc6s5)CC4)cc3)cc2n(C)c1=O 10.1016/j.bmc.2008.01.002
CHEMBL407204 156889 None 10 Human Binding pKi = 8.0 8.0 912 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 592 5 1 9 4.0 Cn1c(=O)c2[nH]c(-c3ccc(OC(C)(C)C(=O)N4CCN(c5nc6cc(Cl)ccc6s5)CC4)cc3)cc2n(C)c1=O 10.1016/j.bmc.2008.01.002
11952559 6309 None 0 Human Binding pKi = 8.0 8.0 194 3
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 293 2 1 6 2.0 Cn1c(=O)[nH]c2nc(-c3ccco3)c(-c3ccncn3)cc21 10.1016/j.bmcl.2010.01.077
CHEMBL1081841 6309 None 0 Human Binding pKi = 8.0 8.0 194 3
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 293 2 1 6 2.0 Cn1c(=O)[nH]c2nc(-c3ccco3)c(-c3ccncn3)cc21 10.1016/j.bmcl.2010.01.077
16070335 58018 None 0 Human Binding pKi = 8.0 8.0 28 3
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 317 4 1 5 2.9 O=C(Nc1cnc(-c2ccncc2)c(-c2ccccn2)n1)C1CC1 10.1021/ml100249e
CHEMBL1672620 58018 None 0 Human Binding pKi = 8.0 8.0 28 3
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 317 4 1 5 2.9 O=C(Nc1cnc(-c2ccncc2)c(-c2ccccn2)n1)C1CC1 10.1021/ml100249e
16071897 58028 None 1 Human Binding pKi = 8.0 8.0 120 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 335 4 1 5 3.1 O=C(Nc1cnc(-c2ccncc2F)c(-c2ccncc2)n1)C1CC1 10.1021/ml100249e
CHEMBL1672630 58028 None 1 Human Binding pKi = 8.0 8.0 120 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 335 4 1 5 3.1 O=C(Nc1cnc(-c2ccncc2F)c(-c2ccncc2)n1)C1CC1 10.1021/ml100249e
44588471 174716 None 0 Human Binding pKi = 8.0 8.0 10 2
Displacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cells
ChEMBL 343 5 3 6 2.4 CCCn1c(=O)c2[nH]c(-c3ccc(O)cc3)c(O)c2n(CCC)c1=O 10.1016/j.bmc.2008.09.067
CHEMBL455999 174716 None 0 Human Binding pKi = 8.0 8.0 10 2
Displacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cells
ChEMBL 343 5 3 6 2.4 CCCn1c(=O)c2[nH]c(-c3ccc(O)cc3)c(O)c2n(CCC)c1=O 10.1016/j.bmc.2008.09.067
24827442 95761 None 0 Human Binding pKi = 8.0 8.0 22 4
Displacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 460 6 1 7 3.5 CCn1c(=O)n(CC(C)C)c(=O)c2[nH]c(-c3cnn(Cc4cccc(C(F)(F)F)c4)c3)nc21 10.1021/jm7014815
CHEMBL258499 95761 None 0 Human Binding pKi = 8.0 8.0 22 4
Displacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 460 6 1 7 3.5 CCn1c(=O)n(CC(C)C)c(=O)c2[nH]c(-c3cnn(Cc4cccc(C(F)(F)F)c4)c3)nc21 10.1021/jm7014815
22266778 95762 None 0 Human Binding pKi = 8.0 8.0 38 4
Displacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 446 6 1 7 3.2 CCCCn1c(=O)c2[nH]c(-c3cnn(Cc4cccc(C(F)(F)F)c4)c3)nc2n(C)c1=O 10.1021/jm7014815
CHEMBL258507 95762 None 0 Human Binding pKi = 8.0 8.0 38 4
Displacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 446 6 1 7 3.2 CCCCn1c(=O)c2[nH]c(-c3cnn(Cc4cccc(C(F)(F)F)c4)c3)nc2n(C)c1=O 10.1021/jm7014815
21916419 95975 None 0 Human Binding pKi = 8.0 8.0 8 4
Displacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 376 5 1 7 1.7 Cn1c(=O)n(CC2CC2)c(=O)c2[nH]c(-c3cnn(Cc4ccccc4)c3)nc21 10.1021/jm7014815
CHEMBL259524 95975 None 0 Human Binding pKi = 8.0 8.0 8 4
Displacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 376 5 1 7 1.7 Cn1c(=O)n(CC2CC2)c(=O)c2[nH]c(-c3cnn(Cc4ccccc4)c3)nc21 10.1021/jm7014815
9821879 94984 None 14 Human Binding pKi = 8.0 8.0 6 4
Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cellsDisplacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells
ChEMBL 392 7 1 7 2.6 CCCn1c(=O)c2[nH]c(-c3cnn(Cc4ccccc4)c3)nc2n(CCC)c1=O 10.1021/jm051268+
CHEMBL254725 94984 None 14 Human Binding pKi = 8.0 8.0 6 4
Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cellsDisplacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells
ChEMBL 392 7 1 7 2.6 CCCn1c(=O)c2[nH]c(-c3cnn(Cc4ccccc4)c3)nc2n(CCC)c1=O 10.1021/jm051268+
876881 182406 None 2 Human Binding pKi = 8.0 8.0 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 266 3 2 4 1.9 CCOC(=O)C1=C(C)NC(=O)N[C@@H]1c1ccsc1 10.1021/acs.jmedchem.0c01431
CHEMBL4785606 182406 None 2 Human Binding pKi = 8.0 8.0 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 266 3 2 4 1.9 CCOC(=O)C1=C(C)NC(=O)N[C@@H]1c1ccsc1 10.1021/acs.jmedchem.0c01431
11677724 140690 None 0 Human Binding pKi = 8.0 8.0 3 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 499 10 2 7 4.1 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(CC#N)cc4)cc3)cc2n(CCC)c1=O 10.1021/jm0506221
CHEMBL381540 140690 None 0 Human Binding pKi = 8.0 8.0 3 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 499 10 2 7 4.1 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(CC#N)cc4)cc3)cc2n(CCC)c1=O 10.1021/jm0506221
44450930 95816 None 0 Human Binding pKi = 8.0 8.0 26 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 518 6 1 7 2.9 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCC(C(=O)c5ccc(F)cc5)CC4)cc3)cc2n(C)c1=O 10.1016/j.bmc.2008.01.002
CHEMBL258810 95816 None 0 Human Binding pKi = 8.0 8.0 26 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 518 6 1 7 2.9 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCC(C(=O)c5ccc(F)cc5)CC4)cc3)cc2n(C)c1=O 10.1016/j.bmc.2008.01.002
155527939 171261 None 0 Human Binding pKi = 8.0 8.0 - 1
Displacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assayDisplacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assay
ChEMBL 377 3 1 6 4.0 CC1=C(C(=O)OCC(F)(F)F)[C@@H](c2ccco2)n2c(nc3ccccc32)N1 10.1021/acs.jmedchem.9b01340
CHEMBL4460214 171261 None 0 Human Binding pKi = 8.0 8.0 - 1
Displacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assayDisplacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assay
ChEMBL 377 3 1 6 4.0 CC1=C(C(=O)OCC(F)(F)F)[C@@H](c2ccco2)n2c(nc3ccccc32)N1 10.1021/acs.jmedchem.9b01340
127031266 139065 None 0 Human Binding pKi = 7.9 7.9 - 1
Displacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting methodDisplacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting method
ChEMBL 337 3 1 6 3.9 CC1=C(C(=O)OC(C)C)C(c2ccoc2)n2c(nc3ccccc32)N1 10.1021/acs.jmedchem.0c00564
CHEMBL3786336 139065 None 0 Human Binding pKi = 7.9 7.9 - 1
Displacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting methodDisplacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting method
ChEMBL 337 3 1 6 3.9 CC1=C(C(=O)OC(C)C)C(c2ccoc2)n2c(nc3ccccc32)N1 10.1021/acs.jmedchem.0c00564
127031266 139065 None 0 Human Binding pKi = 7.9 7.9 - 1
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 minsDisplacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 mins
ChEMBL 337 3 1 6 3.9 CC1=C(C(=O)OC(C)C)C(c2ccoc2)n2c(nc3ccccc32)N1 10.1021/acs.jmedchem.5b01586
CHEMBL3786336 139065 None 0 Human Binding pKi = 7.9 7.9 - 1
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 minsDisplacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 mins
ChEMBL 337 3 1 6 3.9 CC1=C(C(=O)OC(C)C)C(c2ccoc2)n2c(nc3ccccc32)N1 10.1021/acs.jmedchem.5b01586
127031266 139065 None 0 Human Binding pKi = 7.9 7.9 - 1
Displacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assayDisplacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assay
ChEMBL 337 3 1 6 3.9 CC1=C(C(=O)OC(C)C)C(c2ccoc2)n2c(nc3ccccc32)N1 10.1021/acs.jmedchem.9b01340
CHEMBL3786336 139065 None 0 Human Binding pKi = 7.9 7.9 - 1
Displacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assayDisplacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assay
ChEMBL 337 3 1 6 3.9 CC1=C(C(=O)OC(C)C)C(c2ccoc2)n2c(nc3ccccc32)N1 10.1021/acs.jmedchem.9b01340
136042346 71174 None 0 Human Binding pKi = 7.9 7.9 2 2
Displacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation countingDisplacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation counting
ChEMBL 461 8 2 8 3.2 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5ccccc5[nH]4)nn3C)cc2n(CCC)c1=O 10.1021/jm201292w
CHEMBL1955924 71174 None 0 Human Binding pKi = 7.9 7.9 2 2
Displacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation countingDisplacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation counting
ChEMBL 461 8 2 8 3.2 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5ccccc5[nH]4)nn3C)cc2n(CCC)c1=O 10.1021/jm201292w
44574191 189410 None 0 Human Binding pKi = 7.9 7.9 11 2
Displacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells by beta scintillation counterDisplacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells by beta scintillation counter
ChEMBL 473 4 1 7 2.7 Cn1c(=O)c2[nH]c(-c3ccc(COC(=O)N4CCN(c5ccccc5)CC4)cc3)cc2n(C)c1=O 10.1016/j.bmc.2009.03.062
CHEMBL513135 189410 None 0 Human Binding pKi = 7.9 7.9 11 2
Displacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells by beta scintillation counterDisplacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells by beta scintillation counter
ChEMBL 473 4 1 7 2.7 Cn1c(=O)c2[nH]c(-c3ccc(COC(=O)N4CCN(c5ccccc5)CC4)cc3)cc2n(C)c1=O 10.1016/j.bmc.2009.03.062
145971798 164493 None 0 Human Binding pKi = 7.9 7.9 14 4
Displacement of [3H]PSB-603 from recombinant human adenosine A2B receptor expressed in CHO cell membranes after 75 mins by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human adenosine A2B receptor expressed in CHO cell membranes after 75 mins by liquid scintillation counting method
ChEMBL 631 10 3 7 4.3 CCCn1c(=O)[nH]c2nc(-c3ccc(OCC(=O)NCCCC4=C5C(C)=CC(C)=[N+]5[B-](F)(F)n5c(C)cc(C)c54)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.7b01627
CHEMBL4214450 164493 None 0 Human Binding pKi = 7.9 7.9 14 4
Displacement of [3H]PSB-603 from recombinant human adenosine A2B receptor expressed in CHO cell membranes after 75 mins by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human adenosine A2B receptor expressed in CHO cell membranes after 75 mins by liquid scintillation counting method
ChEMBL 631 10 3 7 4.3 CCCn1c(=O)[nH]c2nc(-c3ccc(OCC(=O)NCCCC4=C5C(C)=CC(C)=[N+]5[B-](F)(F)n5c(C)cc(C)c54)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.7b01627
44185873 192487 None 0 Human Binding pKi = 7.9 7.9 31 3
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 510 6 2 8 1.6 CCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(c5ccc(OC)cc5)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
CHEMBL520899 192487 None 0 Human Binding pKi = 7.9 7.9 31 3
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 510 6 2 8 1.6 CCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(c5ccc(OC)cc5)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
45268867 196182 None 0 Human Binding pKi = 7.9 7.9 12 3
Binding affinity to human adenosine A2b receptor expressed in HEK293 cellsBinding affinity to human adenosine A2b receptor expressed in HEK293 cells
ChEMBL 519 11 2 9 2.8 CCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(C(C)=O)cc4)cc3)nc2n(CCCOC)c1=O 10.1016/j.bmc.2009.03.029
CHEMBL561364 196182 None 0 Human Binding pKi = 7.9 7.9 12 3
Binding affinity to human adenosine A2b receptor expressed in HEK293 cellsBinding affinity to human adenosine A2b receptor expressed in HEK293 cells
ChEMBL 519 11 2 9 2.8 CCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(C(C)=O)cc4)cc3)nc2n(CCCOC)c1=O 10.1016/j.bmc.2009.03.029
11519021 141355 None 0 Human Binding pKi = 7.9 7.9 223 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 504 9 2 8 3.3 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(C(=O)OCC)cc4)cc3)cc2n(C)c1=O 10.1021/jm0506221
CHEMBL383638 141355 None 0 Human Binding pKi = 7.9 7.9 223 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 504 9 2 8 3.3 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(C(=O)OCC)cc4)cc3)cc2n(C)c1=O 10.1021/jm0506221
44451073 157570 None 0 Human Binding pKi = 7.9 7.9 4 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 553 9 1 7 3.7 O=C(COc1ccc(-c2cc3c([nH]2)c(=O)n(CC2CC2)c(=O)n3CC2CC2)cc1)N1CCN(c2ccccc2)CC1 10.1016/j.bmc.2008.01.002
CHEMBL408048 157570 None 0 Human Binding pKi = 7.9 7.9 4 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 553 9 1 7 3.7 O=C(COc1ccc(-c2cc3c([nH]2)c(=O)n(CC2CC2)c(=O)n3CC2CC2)cc1)N1CCN(c2ccccc2)CC1 10.1016/j.bmc.2008.01.002
168297138 192241 None 0 Human Binding pKi = 7.9 7.9 - 1
Displacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cell membrane and measured after 0.5 hrs by radioligand displacement assayDisplacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cell membrane and measured after 0.5 hrs by radioligand displacement assay
ChEMBL 368 5 2 7 1.1 CCCn1c(=O)[nH]c2nc(-c3ccc(OS(=O)(=O)F)cc3)[nH]c2c1=O 10.1039/d2md00132b
CHEMBL5205220 192241 None 0 Human Binding pKi = 7.9 7.9 - 1
Displacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cell membrane and measured after 0.5 hrs by radioligand displacement assayDisplacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cell membrane and measured after 0.5 hrs by radioligand displacement assay
ChEMBL 368 5 2 7 1.1 CCCn1c(=O)[nH]c2nc(-c3ccc(OS(=O)(=O)F)cc3)[nH]c2c1=O 10.1039/d2md00132b
11781054 206421 None 0 Human Binding pKi = 7.9 7.9 3 3
Binding affinity for human adenosine A2B receptor using [3H]ZM-241385 in CHO cell membranesBinding affinity for human adenosine A2B receptor using [3H]ZM-241385 in CHO cell membranes
ChEMBL 284 4 2 4 1.9 CCCCn1c(=O)[nH]c2[nH]c(-c3ccccc3)nc2c1=O 10.1021/jm0310030
CHEMBL8789 206421 None 0 Human Binding pKi = 7.9 7.9 3 3
Binding affinity for human adenosine A2B receptor using [3H]ZM-241385 in CHO cell membranesBinding affinity for human adenosine A2B receptor using [3H]ZM-241385 in CHO cell membranes
ChEMBL 284 4 2 4 1.9 CCCCn1c(=O)[nH]c2[nH]c(-c3ccccc3)nc2c1=O 10.1021/jm0310030
11781054 206421 None 0 Human Binding pKi = 7.9 7.9 3 3
Inhibition of [3H]ZM-241385 binding to human adenosine A2B receptorInhibition of [3H]ZM-241385 binding to human adenosine A2B receptor
ChEMBL 284 4 2 4 1.9 CCCCn1c(=O)[nH]c2[nH]c(-c3ccccc3)nc2c1=O 10.1021/jm011049y
CHEMBL8789 206421 None 0 Human Binding pKi = 7.9 7.9 3 3
Inhibition of [3H]ZM-241385 binding to human adenosine A2B receptorInhibition of [3H]ZM-241385 binding to human adenosine A2B receptor
ChEMBL 284 4 2 4 1.9 CCCCn1c(=O)[nH]c2[nH]c(-c3ccccc3)nc2c1=O 10.1021/jm011049y
44281700 111441 None 0 Human Binding pKi = 7.0 7.0 12 2
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 480 7 3 6 4.7 CCCn1c(=O)c2nc(-c3ccc(NC(=O)Nc4cccc(Cl)c4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm0309654
CHEMBL32751 111441 None 0 Human Binding pKi = 7.0 7.0 12 2
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 480 7 3 6 4.7 CCCn1c(=O)c2nc(-c3ccc(NC(=O)Nc4cccc(Cl)c4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm0309654
137631671 156333 None 0 Human Binding pKi = 6.0 6.0 -53 2
Displacement of [3H]MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 minsDisplacement of [3H]MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 mins
ChEMBL 352 5 1 5 3.9 CCCn1c(-c2cccc(OC)c2)nc2nc(C3CCCC3)[nH]c2c1=O 10.1016/j.bmc.2017.02.029
CHEMBL4065762 156333 None 0 Human Binding pKi = 6.0 6.0 -53 2
Displacement of [3H]MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 minsDisplacement of [3H]MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 mins
ChEMBL 352 5 1 5 3.9 CCCn1c(-c2cccc(OC)c2)nc2nc(C3CCCC3)[nH]c2c1=O 10.1016/j.bmc.2017.02.029
127043828 141125 None 0 Rat Binding pKi = 6.0 6.0 -13 7
Displacement of [3H]PSB-603 from recombinant rat adenosine receptor A2b expressed in CHO cell membranesDisplacement of [3H]PSB-603 from recombinant rat adenosine receptor A2b expressed in CHO cell membranes
ChEMBL 538 15 0 9 4.1 CCCCn1c(=O)c2c(nc3n2CCCN3CCc2ccc(OCCN(CC)CC)cc2)n(CCCC)c1=O 10.1016/j.bmc.2016.07.028
CHEMBL3827331 141125 None 0 Rat Binding pKi = 6.0 6.0 -13 7
Displacement of [3H]PSB-603 from recombinant rat adenosine receptor A2b expressed in CHO cell membranesDisplacement of [3H]PSB-603 from recombinant rat adenosine receptor A2b expressed in CHO cell membranes
ChEMBL 538 15 0 9 4.1 CCCCn1c(=O)c2c(nc3n2CCCN3CCc2ccc(OCCN(CC)CC)cc2)n(CCCC)c1=O 10.1016/j.bmc.2016.07.028
135424850 78282 None 0 Human Binding pKi = 6.0 6.0 - 1
Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cellsDisplacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells
ChEMBL 378 6 1 7 2.6 CCCn1c(=O)c2nc(-c3ccnn3-c3ccccc3)[nH]c2n(CCC)c1=O 10.1021/jm051268+
CHEMBL210738 78282 None 0 Human Binding pKi = 6.0 6.0 - 1
Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cellsDisplacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells
ChEMBL 378 6 1 7 2.6 CCCn1c(=O)c2nc(-c3ccnn3-c3ccccc3)[nH]c2n(CCC)c1=O 10.1021/jm051268+
2895908 44288 None 14 Human Binding pKi = 6.0 6.0 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 282 3 2 5 2.5 CCOC(=O)C1=C(C)N=C(S)NC1c1ccsc1 10.1021/acs.jmedchem.0c01431
CHEMBL1517366 44288 None 14 Human Binding pKi = 6.0 6.0 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 282 3 2 5 2.5 CCOC(=O)C1=C(C)N=C(S)NC1c1ccsc1 10.1021/acs.jmedchem.0c01431
2895908 44288 None 14 Human Binding pKi = 6.0 6.0 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by Scatchard plot analysisDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by Scatchard plot analysis
ChEMBL 282 3 2 5 2.5 CCOC(=O)C1=C(C)N=C(S)NC1c1ccsc1 10.1021/ml400185v
CHEMBL1517366 44288 None 14 Human Binding pKi = 6.0 6.0 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by Scatchard plot analysisDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by Scatchard plot analysis
ChEMBL 282 3 2 5 2.5 CCOC(=O)C1=C(C)N=C(S)NC1c1ccsc1 10.1021/ml400185v
156014646 177233 None 0 Human Binding pKi = 6.0 6.0 - 1
Displacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting methodDisplacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting method
ChEMBL 337 3 2 6 3.0 CC1=C(C(=O)OC(C)C)C(c2cc[nH]n2)n2c(nc3ccccc32)N1 10.1021/acs.jmedchem.0c00564
CHEMBL4635701 177233 None 0 Human Binding pKi = 6.0 6.0 - 1
Displacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting methodDisplacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting method
ChEMBL 337 3 2 6 3.0 CC1=C(C(=O)OC(C)C)C(c2cc[nH]n2)n2c(nc3ccccc32)N1 10.1021/acs.jmedchem.0c00564
135529398 118278 None 0 Human Binding pKi = 7.0 7.0 1 2
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 600 12 2 11 3.8 CCCn1c(=O)c2nc(-c3cc(NC(=O)Cc4ccc(OCc5ccc([N+](=O)[O-])cc5)cc4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
CHEMBL34097 118278 None 0 Human Binding pKi = 7.0 7.0 1 2
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 600 12 2 11 3.8 CCCn1c(=O)c2nc(-c3cc(NC(=O)Cc4ccc(OCc5ccc([N+](=O)[O-])cc5)cc4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
22266763 72823 None 0 Human Binding pKi = 7.0 7.0 20 3
Displacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cellsDisplacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cells
ChEMBL 493 8 1 9 3.9 CCCn1c(=O)c2nc(-c3cnn(Cc4cc(-c5ccccc5Cl)on4)c3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2005.10.002
CHEMBL200154 72823 None 0 Human Binding pKi = 7.0 7.0 20 3
Displacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cellsDisplacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cells
ChEMBL 493 8 1 9 3.9 CCCn1c(=O)c2nc(-c3cnn(Cc4cc(-c5ccccc5Cl)on4)c3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2005.10.002
169317 1201 None 38 Human Binding pKi = 6.0 6.0 -44 9
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 236 4 1 5 0.7 CCCn1c(=O)n(CCC)c2c(c1=O)[nH]cn2 10.1021/jm0104318
427 1201 None 38 Human Binding pKi = 6.0 6.0 -44 9
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 236 4 1 5 0.7 CCCn1c(=O)n(CCC)c2c(c1=O)[nH]cn2 10.1021/jm0104318
CHEMBL157655 1201 None 38 Human Binding pKi = 6.0 6.0 -44 9
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 236 4 1 5 0.7 CCCn1c(=O)n(CCC)c2c(c1=O)[nH]cn2 10.1021/jm0104318
176408 3557 None 84 Human Binding pKi = 6.0 6.0 -407 7
Inhibition of human adenosine 2B receptorInhibition of human adenosine 2B receptor
ChEMBL 345 4 1 8 2.6 Nc1nc2n(CCc3ccccc3)ncc2c2n1nc(n2)c1ccco1 10.1021/acs.jmedchem.0c00237
403 3557 None 84 Human Binding pKi = 6.0 6.0 -407 7
Inhibition of human adenosine 2B receptorInhibition of human adenosine 2B receptor
ChEMBL 345 4 1 8 2.6 Nc1nc2n(CCc3ccccc3)ncc2c2n1nc(n2)c1ccco1 10.1021/acs.jmedchem.0c00237
431 3557 None 84 Human Binding pKi = 6.0 6.0 -407 7
Inhibition of human adenosine 2B receptorInhibition of human adenosine 2B receptor
ChEMBL 345 4 1 8 2.6 Nc1nc2n(CCc3ccccc3)ncc2c2n1nc(n2)c1ccco1 10.1021/acs.jmedchem.0c00237
CHEMBL17127 3557 None 84 Human Binding pKi = 6.0 6.0 -407 7
Inhibition of human adenosine 2B receptorInhibition of human adenosine 2B receptor
ChEMBL 345 4 1 8 2.6 Nc1nc2n(CCc3ccccc3)ncc2c2n1nc(n2)c1ccco1 10.1021/acs.jmedchem.0c00237
176408 3557 None 84 Human Binding pKi = 6.0 6.0 -407 7
Inhibition of human recombinant adenosine receptor A2bInhibition of human recombinant adenosine receptor A2b
ChEMBL 345 4 1 8 2.6 Nc1nc2n(CCc3ccccc3)ncc2c2n1nc(n2)c1ccco1 10.1021/jm4011669
403 3557 None 84 Human Binding pKi = 6.0 6.0 -407 7
Inhibition of human recombinant adenosine receptor A2bInhibition of human recombinant adenosine receptor A2b
ChEMBL 345 4 1 8 2.6 Nc1nc2n(CCc3ccccc3)ncc2c2n1nc(n2)c1ccco1 10.1021/jm4011669
431 3557 None 84 Human Binding pKi = 6.0 6.0 -407 7
Inhibition of human recombinant adenosine receptor A2bInhibition of human recombinant adenosine receptor A2b
ChEMBL 345 4 1 8 2.6 Nc1nc2n(CCc3ccccc3)ncc2c2n1nc(n2)c1ccco1 10.1021/jm4011669
CHEMBL17127 3557 None 84 Human Binding pKi = 6.0 6.0 -407 7
Inhibition of human recombinant adenosine receptor A2bInhibition of human recombinant adenosine receptor A2b
ChEMBL 345 4 1 8 2.6 Nc1nc2n(CCc3ccccc3)ncc2c2n1nc(n2)c1ccco1 10.1021/jm4011669
13525063 9385 None 0 Human Binding pKi = 5.0 5.0 - 1
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 300 2 2 6 0.3 Cn1c(=O)c2nc(-c3ccccc3C(=O)O)[nH]c2n(C)c1=O 10.1021/jm0104318
CHEMBL11146 9385 None 0 Human Binding pKi = 5.0 5.0 - 1
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 300 2 2 6 0.3 Cn1c(=O)c2nc(-c3ccccc3C(=O)O)[nH]c2n(C)c1=O 10.1021/jm0104318
10769581 36760 None 1 Human Binding pKi = 6.0 6.0 -4 4
Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 934-1327Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 934-1327
ChEMBL 579 4 1 8 4.8 Nc1nc2nn(CCc3cc(Br)c(Br)cc3Br)cc2c2nc(-c3ccco3)nn12 10.1021/jm001047y
CHEMBL144972 36760 None 1 Human Binding pKi = 6.0 6.0 -4 4
Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 934-1327Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 934-1327
ChEMBL 579 4 1 8 4.8 Nc1nc2nn(CCc3cc(Br)c(Br)cc3Br)cc2c2nc(-c3ccco3)nn12 10.1021/jm001047y
9949541 96292 None 0 Human Binding pKi = 7.0 7.0 -107 4
Inhibition of human recombinant adenosine receptor A2bInhibition of human recombinant adenosine receptor A2b
ChEMBL 334 3 2 7 2.4 Nc1nc(-c2ccco2)c2ncn(C(=O)NCc3ccccc3)c2n1 10.1021/jm4011669
CHEMBL261203 96292 None 0 Human Binding pKi = 7.0 7.0 -107 4
Inhibition of human recombinant adenosine receptor A2bInhibition of human recombinant adenosine receptor A2b
ChEMBL 334 3 2 7 2.4 Nc1nc(-c2ccco2)c2ncn(C(=O)NCc3ccccc3)c2n1 10.1021/jm4011669
44390522 64477 None 0 Human Binding pKi = 6.0 6.0 - 1
Binding affinity for adenosine A2b receptor by using as [3H]ZM-241385 (14 nM) radioligand in membranes from HEK-A2B cellsBinding affinity for adenosine A2b receptor by using as [3H]ZM-241385 (14 nM) radioligand in membranes from HEK-A2B cells
ChEMBL 500 9 1 9 4.3 CCCn1c(=O)c2nc(-c3ccc(OCc4nc(-c5ccccc5C)no4)cc3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2004.11.044
CHEMBL181400 64477 None 0 Human Binding pKi = 6.0 6.0 - 1
Binding affinity for adenosine A2b receptor by using as [3H]ZM-241385 (14 nM) radioligand in membranes from HEK-A2B cellsBinding affinity for adenosine A2b receptor by using as [3H]ZM-241385 (14 nM) radioligand in membranes from HEK-A2B cells
ChEMBL 500 9 1 9 4.3 CCCn1c(=O)c2nc(-c3ccc(OCc4nc(-c5ccccc5C)no4)cc3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2004.11.044
52950027 19143 None 0 Human Binding pKi = 6.0 6.0 -1 2
Displacement of [3H]ZM241385 from human adenosine A2B receptor transfected in CHO cells after 60 mins by scintillation countingDisplacement of [3H]ZM241385 from human adenosine A2B receptor transfected in CHO cells after 60 mins by scintillation counting
ChEMBL 478 9 2 4 5.3 O=C(COc1ccc2[nH]c(=O)c(-c3ccco3)c(CCc3ccccc3)c2c1)NCc1ccccc1 10.1016/j.bmcl.2010.10.030
CHEMBL1289461 19143 None 0 Human Binding pKi = 6.0 6.0 -1 2
Displacement of [3H]ZM241385 from human adenosine A2B receptor transfected in CHO cells after 60 mins by scintillation countingDisplacement of [3H]ZM241385 from human adenosine A2B receptor transfected in CHO cells after 60 mins by scintillation counting
ChEMBL 478 9 2 4 5.3 O=C(COc1ccc2[nH]c(=O)c(-c3ccco3)c(CCc3ccccc3)c2c1)NCc1ccccc1 10.1016/j.bmcl.2010.10.030
162677300 183538 None 0 Human Binding pKi = 6.0 6.0 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 275 2 2 4 2.8 CC1=C(c2ncc(C)o2)C(c2ccsc2)NC(=O)N1 10.1021/acs.jmedchem.0c01431
CHEMBL4800081 183538 None 0 Human Binding pKi = 6.0 6.0 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 275 2 2 4 2.8 CC1=C(c2ncc(C)o2)C(c2ccsc2)NC(=O)N1 10.1021/acs.jmedchem.0c01431
145981370 166731 None 0 Human Binding pKi = 7.0 7.0 -2 4
Displacement of [3H]PSB-602 from human adenosine A2B receptor expressed in CHO cell membranesDisplacement of [3H]PSB-602 from human adenosine A2B receptor expressed in CHO cell membranes
ChEMBL 595 17 1 10 3.3 CCCCn1c(=O)c2c(nc3n2CCCN3CCc2ccc(OCC(=O)NCCN(CC)CC)cc2)n(CCCC)c1=O 10.1039/C8MD00070K
CHEMBL4283160 166731 None 0 Human Binding pKi = 7.0 7.0 -2 4
Displacement of [3H]PSB-602 from human adenosine A2B receptor expressed in CHO cell membranesDisplacement of [3H]PSB-602 from human adenosine A2B receptor expressed in CHO cell membranes
ChEMBL 595 17 1 10 3.3 CCCCn1c(=O)c2c(nc3n2CCCN3CCc2ccc(OCC(=O)NCCN(CC)CC)cc2)n(CCCC)c1=O 10.1039/C8MD00070K
52941597 19092 None 0 Human Binding pKi = 5.0 5.0 - 1
Displacement of [3H]ZM241385 from human adenosine A2B receptor transfected in CHO cells after 60 mins by scintillation countingDisplacement of [3H]ZM241385 from human adenosine A2B receptor transfected in CHO cells after 60 mins by scintillation counting
ChEMBL 357 5 1 4 2.7 COc1ccc2[nH]c(=O)c(S(C)(=O)=O)c(CCc3ccccc3)c2c1 10.1016/j.bmcl.2010.10.030
CHEMBL1289109 19092 None 0 Human Binding pKi = 5.0 5.0 - 1
Displacement of [3H]ZM241385 from human adenosine A2B receptor transfected in CHO cells after 60 mins by scintillation countingDisplacement of [3H]ZM241385 from human adenosine A2B receptor transfected in CHO cells after 60 mins by scintillation counting
ChEMBL 357 5 1 4 2.7 COc1ccc2[nH]c(=O)c(S(C)(=O)=O)c(CCc3ccccc3)c2c1 10.1016/j.bmcl.2010.10.030
21874634 190088 None 0 Human Binding pKi = 6.0 6.0 -9 4
Displacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation countingDisplacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation counting
ChEMBL 294 3 1 9 0.9 Nc1nc(-c2ccco2)c2nnn(Cc3cnccn3)c2n1 10.1021/jm800961g
CHEMBL517277 190088 None 0 Human Binding pKi = 6.0 6.0 -9 4
Displacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation countingDisplacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation counting
ChEMBL 294 3 1 9 0.9 Nc1nc(-c2ccco2)c2nnn(Cc3cnccn3)c2n1 10.1021/jm800961g
CHEMBL5087059 215068 None 0 Human Binding pKi = 6.9 6.9 -3 4
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells by liquid scintillation counting analysisDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells by liquid scintillation counting analysis
ChEMBL None None None Nc1nc(-c2ccccc2)c2c(n1)-c1ccc(OCCCN3CCCCC3)cc1C2=O 10.1021/acs.jmedchem.0c00914
46837702 10592 None 0 Human Binding pKi = 6.9 6.9 - 1
Displacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells after 30 minsDisplacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells after 30 mins
ChEMBL 487 7 2 6 2.8 CCCn1c(=O)[nH]c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCN(c5ccccc5)CC4)cc3)cc21 10.1016/j.ejmech.2010.03.011
CHEMBL1169971 10592 None 0 Human Binding pKi = 6.9 6.9 - 1
Displacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells after 30 minsDisplacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells after 30 mins
ChEMBL 487 7 2 6 2.8 CCCn1c(=O)[nH]c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCN(c5ccccc5)CC4)cc3)cc21 10.1016/j.ejmech.2010.03.011
5053422 203552 None 42 Human Binding pKi = 4.9 4.9 -1 3
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 296 3 0 6 1.3 C=CCn1c(=O)c2c(nc(-c3ccccc3)n2C)n(C)c1=O 10.1021/jm0104318
CHEMBL66610 203552 None 42 Human Binding pKi = 4.9 4.9 -1 3
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 296 3 0 6 1.3 C=CCn1c(=O)c2c(nc(-c3ccccc3)n2C)n(C)c1=O 10.1021/jm0104318
11638790 142481 None 0 Human Binding pKi = 6.9 6.9 - 1
Displacement of [3H]DPCPX from human A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human A2B receptor expressed in HEK293 cells
ChEMBL 346 5 1 8 3.3 COc1ccc(Nc2ncc(-c3ccncn3)c(-c3ccco3)n2)cn1 10.1021/jm061333v
CHEMBL389040 142481 None 0 Human Binding pKi = 6.9 6.9 - 1
Displacement of [3H]DPCPX from human A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human A2B receptor expressed in HEK293 cells
ChEMBL 346 5 1 8 3.3 COc1ccc(Nc2ncc(-c3ccncn3)c(-c3ccco3)n2)cn1 10.1021/jm061333v
44588470 174714 None 0 Human Binding pKi = 6.9 6.9 -1 2
Displacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cells
ChEMBL 343 5 2 7 2.4 CCCn1c(=O)c2c(cc(-c3ccc(O)cc3)n2O)n(CCC)c1=O 10.1016/j.bmc.2008.09.067
CHEMBL455998 174714 None 0 Human Binding pKi = 6.9 6.9 -1 2
Displacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cells
ChEMBL 343 5 2 7 2.4 CCCn1c(=O)c2c(cc(-c3ccc(O)cc3)n2O)n(CCC)c1=O 10.1016/j.bmc.2008.09.067
76309933 103856 None 0 Human Binding pKi = 5.9 5.9 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 278 3 1 4 2.2 CC1=C(C(=O)OC(C)C)C(c2ccco2)NC(=O)N1C 10.1021/acs.jmedchem.0c01431
CHEMBL3091715 103856 None 0 Human Binding pKi = 5.9 5.9 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 278 3 1 4 2.2 CC1=C(C(=O)OC(C)C)C(c2ccco2)NC(=O)N1C 10.1021/acs.jmedchem.0c01431
76309933 103856 None 0 Human Binding pKi = 5.9 5.9 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by Scatchard plot analysisDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by Scatchard plot analysis
ChEMBL 278 3 1 4 2.2 CC1=C(C(=O)OC(C)C)C(c2ccco2)NC(=O)N1C 10.1021/ml400185v
CHEMBL3091715 103856 None 0 Human Binding pKi = 5.9 5.9 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by Scatchard plot analysisDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by Scatchard plot analysis
ChEMBL 278 3 1 4 2.2 CC1=C(C(=O)OC(C)C)C(c2ccco2)NC(=O)N1C 10.1021/ml400185v
9955052 119883 None 0 Human Binding pKi = 6.9 6.9 -1 4
Displacement of [3H]-DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 91-148Displacement of [3H]-DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 91-148
ChEMBL 442 3 2 8 4.2 Cn1cc2c(nc(NC(=O)Nc3ccc(Cl)c(Cl)c3)n3nc(-c4ccco4)nc23)n1 10.1021/jm0109614
CHEMBL349019 119883 None 0 Human Binding pKi = 6.9 6.9 -1 4
Displacement of [3H]-DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 91-148Displacement of [3H]-DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 91-148
ChEMBL 442 3 2 8 4.2 Cn1cc2c(nc(NC(=O)Nc3ccc(Cl)c(Cl)c3)n3nc(-c4ccco4)nc23)n1 10.1021/jm0109614
11565927 85370 None 0 Human Binding pKi = 6.9 6.9 - 1
Displacement of [3H]DPCPX from human A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human A2B receptor expressed in HEK293 cells
ChEMBL 317 4 1 8 2.7 c1coc(-c2nc(Nc3cnccn3)ncc2-c2ccncn2)c1 10.1021/jm061333v
CHEMBL226188 85370 None 0 Human Binding pKi = 6.9 6.9 - 1
Displacement of [3H]DPCPX from human A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human A2B receptor expressed in HEK293 cells
ChEMBL 317 4 1 8 2.7 c1coc(-c2nc(Nc3cnccn3)ncc2-c2ccncn2)c1 10.1021/jm061333v
46228011 200177 None 0 Human Binding pKi = 6.9 6.9 2 3
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 364 6 1 6 2.5 CCCn1c(=O)c2[nH]c(Cc3ccccc3)nc2n(Cc2ccco2)c1=O 10.1016/j.bmc.2009.07.034
CHEMBL596558 200177 None 0 Human Binding pKi = 6.9 6.9 2 3
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 364 6 1 6 2.5 CCCn1c(=O)c2[nH]c(Cc3ccccc3)nc2n(Cc2ccco2)c1=O 10.1016/j.bmc.2009.07.034
155548797 173737 None 0 Human Binding pKi = 6.9 6.9 - 1
Displacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assayDisplacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assay
ChEMBL 393 3 1 6 4.5 CCOC(=O)C1=C(C(F)(F)F)Nc2nc3ccccc3n2C1c1ccsc1 10.1021/acs.jmedchem.9b01340
CHEMBL4536469 173737 None 0 Human Binding pKi = 6.9 6.9 - 1
Displacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assayDisplacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assay
ChEMBL 393 3 1 6 4.5 CCOC(=O)C1=C(C(F)(F)F)Nc2nc3ccccc3n2C1c1ccsc1 10.1021/acs.jmedchem.9b01340
21874756 190795 None 0 Human Binding pKi = 6.9 6.9 -117 4
Displacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation countingDisplacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation counting
ChEMBL 335 4 2 8 2.3 CCc1cc(Cn2nnc3c(-c4ccco4)nc(N)nc32)ccc1N 10.1021/jm800961g
CHEMBL518364 190795 None 0 Human Binding pKi = 6.9 6.9 -117 4
Displacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation countingDisplacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation counting
ChEMBL 335 4 2 8 2.3 CCc1cc(Cn2nnc3c(-c4ccco4)nc(N)nc32)ccc1N 10.1021/jm800961g
10436433 131373 None 0 Human Binding pKi = 5.9 5.9 -30 3
Inhibition of [3H]DPCPX binding to human adenosine A2B receptor expressed in HEK293 cellsInhibition of [3H]DPCPX binding to human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 512 9 5 15 -0.6 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(N[C@H](CO)Cc5ccc(OC)cc5)nc43)[C@H](O)[C@@H]2O)n1 10.1021/jm031143+
CHEMBL368880 131373 None 0 Human Binding pKi = 5.9 5.9 -30 3
Inhibition of [3H]DPCPX binding to human adenosine A2B receptor expressed in HEK293 cellsInhibition of [3H]DPCPX binding to human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 512 9 5 15 -0.6 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(N[C@H](CO)Cc5ccc(OC)cc5)nc43)[C@H](O)[C@@H]2O)n1 10.1021/jm031143+
44410554 140871 None 0 Human Binding pKi = 5.9 5.9 -346 4
Displacement of [125I]ABOPX from human adenosine A2B receptor in HEK cellsDisplacement of [125I]ABOPX from human adenosine A2B receptor in HEK cells
ChEMBL 511 7 5 12 0.0 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC)nc(C#CC(O)c4cccc([N+](=O)[O-])c4)nc32)[C@H](O)[C@@H]1O 10.1016/j.bmcl.2006.01.110
CHEMBL381972 140871 None 0 Human Binding pKi = 5.9 5.9 -346 4
Displacement of [125I]ABOPX from human adenosine A2B receptor in HEK cellsDisplacement of [125I]ABOPX from human adenosine A2B receptor in HEK cells
ChEMBL 511 7 5 12 0.0 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC)nc(C#CC(O)c4cccc([N+](=O)[O-])c4)nc32)[C@H](O)[C@@H]1O 10.1016/j.bmcl.2006.01.110
3481963 38087 None 7 Human Binding pKi = 5.9 5.9 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 294 4 2 4 2.6 CC1=C(C(=O)OCC(C)C)C(c2ccsc2)NC(=O)N1 10.1021/acs.jmedchem.0c01431
CHEMBL1460793 38087 None 7 Human Binding pKi = 5.9 5.9 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 294 4 2 4 2.6 CC1=C(C(=O)OCC(C)C)C(c2ccsc2)NC(=O)N1 10.1021/acs.jmedchem.0c01431
16720104 85262 None 0 Human Binding pKi = 6.9 6.9 - 1
Displacement of [3H]DPCPX from human A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human A2B receptor expressed in HEK293 cells
ChEMBL 386 6 1 8 3.5 O=c1ccc(Nc2ncc(-c3ccncn3)c(-c3ccco3)n2)cn1CC1CC1 10.1021/jm061333v
CHEMBL225982 85262 None 0 Human Binding pKi = 6.9 6.9 - 1
Displacement of [3H]DPCPX from human A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human A2B receptor expressed in HEK293 cells
ChEMBL 386 6 1 8 3.5 O=c1ccc(Nc2ncc(-c3ccncn3)c(-c3ccco3)n2)cn1CC1CC1 10.1021/jm061333v
71680890 90215 None 0 Human Binding pKi = 6.9 6.9 -2 6
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells after 75 mins by liquid scintillation counting analysisDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells after 75 mins by liquid scintillation counting analysis
ChEMBL 322 4 1 4 3.7 O=C(C/C=C/c1ccccc1)Nc1nc2ccccc2c(=O)s1 10.1021/jm400336x
CHEMBL2382438 90215 None 0 Human Binding pKi = 6.9 6.9 -2 6
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells after 75 mins by liquid scintillation counting analysisDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells after 75 mins by liquid scintillation counting analysis
ChEMBL 322 4 1 4 3.7 O=C(C/C=C/c1ccccc1)Nc1nc2ccccc2c(=O)s1 10.1021/jm400336x
162669248 182609 None 0 Human Binding pKi = 5.9 5.9 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 264 4 2 4 1.9 CCCOC(=O)C1=C(C)NC(=O)NC1c1ccoc1 10.1021/acs.jmedchem.0c01431
CHEMBL4788318 182609 None 0 Human Binding pKi = 5.9 5.9 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 264 4 2 4 1.9 CCCOC(=O)C1=C(C)NC(=O)NC1c1ccoc1 10.1021/acs.jmedchem.0c01431
135443367 487 None 0 Human Binding pKi = 7.9 7.9 22 2
Binding affinity of compound for displacement of [3H]DPCPX binding in HEK293 membranes expressing human A2B adenosine receptorsBinding affinity of compound for displacement of [3H]DPCPX binding in HEK293 membranes expressing human A2B adenosine receptors
ChEMBL 534 9 1 10 1.8 CCCn1c2[nH]c(nc2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)N1CCN(CC1)c1ccccc1 10.1021/jm0309654
382 487 None 0 Human Binding pKi = 7.9 7.9 22 2
Binding affinity of compound for displacement of [3H]DPCPX binding in HEK293 membranes expressing human A2B adenosine receptorsBinding affinity of compound for displacement of [3H]DPCPX binding in HEK293 membranes expressing human A2B adenosine receptors
ChEMBL 534 9 1 10 1.8 CCCn1c2[nH]c(nc2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)N1CCN(CC1)c1ccccc1 10.1021/jm0309654
CHEMBL33455 487 None 0 Human Binding pKi = 7.9 7.9 22 2
Binding affinity of compound for displacement of [3H]DPCPX binding in HEK293 membranes expressing human A2B adenosine receptorsBinding affinity of compound for displacement of [3H]DPCPX binding in HEK293 membranes expressing human A2B adenosine receptors
ChEMBL 534 9 1 10 1.8 CCCn1c2[nH]c(nc2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)N1CCN(CC1)c1ccccc1 10.1021/jm0309654
135493279 100382 None 0 Human Binding pKi = 7.9 7.9 5 2
Binding affinity of compound for displacement of [3H]DPCPX binding in HEK293 membranes expressing human A2B adenosine receptorsBinding affinity of compound for displacement of [3H]DPCPX binding in HEK293 membranes expressing human A2B adenosine receptors
ChEMBL 483 9 2 9 2.3 CCCn1c(=O)c2nc(-c3cc(OCC(=O)Nc4ccc(F)cc4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
CHEMBL289903 100382 None 0 Human Binding pKi = 7.9 7.9 5 2
Binding affinity of compound for displacement of [3H]DPCPX binding in HEK293 membranes expressing human A2B adenosine receptorsBinding affinity of compound for displacement of [3H]DPCPX binding in HEK293 membranes expressing human A2B adenosine receptors
ChEMBL 483 9 2 9 2.3 CCCn1c(=O)c2nc(-c3cc(OCC(=O)Nc4ccc(F)cc4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
135522375 114257 None 0 Human Binding pKi = 7.9 7.9 - 1
Binding affinity of compound for displacement of [3H]DPCPX binding in HEK293 membranes expressing human A2B adenosine receptorsBinding affinity of compound for displacement of [3H]DPCPX binding in HEK293 membranes expressing human A2B adenosine receptors
ChEMBL 525 11 2 11 2.1 CCCn1c(=O)c2nc(-c3cc(OCC(=O)Nc4ccc(OC)c(OC)c4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
CHEMBL33305 114257 None 0 Human Binding pKi = 7.9 7.9 - 1
Binding affinity of compound for displacement of [3H]DPCPX binding in HEK293 membranes expressing human A2B adenosine receptorsBinding affinity of compound for displacement of [3H]DPCPX binding in HEK293 membranes expressing human A2B adenosine receptors
ChEMBL 525 11 2 11 2.1 CCCn1c(=O)c2nc(-c3cc(OCC(=O)Nc4ccc(OC)c(OC)c4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
135443367 487 None 0 Human Binding pKi = 7.9 7.9 22 2
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 534 9 1 10 1.8 CCCn1c2[nH]c(nc2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)N1CCN(CC1)c1ccccc1 10.1021/jm0309654
382 487 None 0 Human Binding pKi = 7.9 7.9 22 2
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 534 9 1 10 1.8 CCCn1c2[nH]c(nc2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)N1CCN(CC1)c1ccccc1 10.1021/jm0309654
CHEMBL33455 487 None 0 Human Binding pKi = 7.9 7.9 22 2
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 534 9 1 10 1.8 CCCn1c2[nH]c(nc2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)N1CCN(CC1)c1ccccc1 10.1021/jm0309654
135493279 100382 None 0 Human Binding pKi = 7.9 7.9 5 2
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 483 9 2 9 2.3 CCCn1c(=O)c2nc(-c3cc(OCC(=O)Nc4ccc(F)cc4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
CHEMBL289903 100382 None 0 Human Binding pKi = 7.9 7.9 5 2
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 483 9 2 9 2.3 CCCn1c(=O)c2nc(-c3cc(OCC(=O)Nc4ccc(F)cc4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
135522375 114257 None 0 Human Binding pKi = 7.9 7.9 - 1
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 525 11 2 11 2.1 CCCn1c(=O)c2nc(-c3cc(OCC(=O)Nc4ccc(OC)c(OC)c4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
CHEMBL33305 114257 None 0 Human Binding pKi = 7.9 7.9 - 1
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 525 11 2 11 2.1 CCCn1c(=O)c2nc(-c3cc(OCC(=O)Nc4ccc(OC)c(OC)c4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
10926253 81058 None 0 Human Binding pKi = 7.9 7.9 1 3
Displacement of [3H]- DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]- DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 353 2 1 10 0.6 CN1CCN(c2c3c(nc(N)n4nc(-c5ccco5)nc34)nn2C)CC1 10.1021/jm021023m
CHEMBL21541 81058 None 0 Human Binding pKi = 7.9 7.9 1 3
Displacement of [3H]- DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]- DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 353 2 1 10 0.6 CN1CCN(c2c3c(nc(N)n4nc(-c5ccco5)nc34)nn2C)CC1 10.1021/jm021023m
CHEMBL553587 81058 None 0 Human Binding pKi = 7.9 7.9 1 3
Displacement of [3H]- DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]- DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 353 2 1 10 0.6 CN1CCN(c2c3c(nc(N)n4nc(-c5ccco5)nc34)nn2C)CC1 10.1021/jm021023m
10852375 37551 None 0 Human Binding pKi = 7.9 7.9 -15 4
Displacement of [3H]-DPCPX from Adenosine A2b receptor expressed in CHO cells; range 8-18Displacement of [3H]-DPCPX from Adenosine A2b receptor expressed in CHO cells; range 8-18
ChEMBL 309 3 1 8 2.3 CC(C)=CCn1cc2c(nc(N)n3nc(-c4ccco4)nc23)n1 10.1021/jm001047y
CHEMBL145623 37551 None 0 Human Binding pKi = 7.9 7.9 -15 4
Displacement of [3H]-DPCPX from Adenosine A2b receptor expressed in CHO cells; range 8-18Displacement of [3H]-DPCPX from Adenosine A2b receptor expressed in CHO cells; range 8-18
ChEMBL 309 3 1 8 2.3 CC(C)=CCn1cc2c(nc(N)n3nc(-c4ccco4)nc23)n1 10.1021/jm001047y
44236850 156154 None 0 Human Binding pKi = 7.9 7.9 - 1
Displacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 minsDisplacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 mins
ChEMBL 582 8 1 9 3.4 CCCn1c(=O)c2[nH]c(-c3cnn(CC#CCN4CCN(c5cccc(C(F)(F)F)c5)CC4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2017.04.014
CHEMBL4063759 156154 None 0 Human Binding pKi = 7.9 7.9 - 1
Displacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 minsDisplacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 mins
ChEMBL 582 8 1 9 3.4 CCCn1c(=O)c2[nH]c(-c3cnn(CC#CCN4CCN(c5cccc(C(F)(F)F)c5)CC4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2017.04.014
57429608 156665 None 0 Human Binding pKi = 7.9 7.9 - 1
Displacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 minsDisplacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 mins
ChEMBL 470 5 1 7 3.3 CCCn1c(=O)c2[nH]c(-c3cnn(CC#Cc4ccc(C(F)(F)F)cc4)c3)nc2n(CC)c1=O 10.1016/j.ejmech.2017.04.014
CHEMBL4069518 156665 None 0 Human Binding pKi = 7.9 7.9 - 1
Displacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 minsDisplacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 mins
ChEMBL 470 5 1 7 3.3 CCCn1c(=O)c2[nH]c(-c3cnn(CC#Cc4ccc(C(F)(F)F)cc4)c3)nc2n(CC)c1=O 10.1016/j.ejmech.2017.04.014
44236506 159440 None 0 Human Binding pKi = 7.9 7.9 - 1
Displacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 minsDisplacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 mins
ChEMBL 474 7 1 9 2.4 CCCn1c(=O)c2[nH]c(-c3cnn(CC#Cc4ccccc4C(=O)OC)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2017.04.014
CHEMBL4101147 159440 None 0 Human Binding pKi = 7.9 7.9 - 1
Displacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 minsDisplacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 mins
ChEMBL 474 7 1 9 2.4 CCCn1c(=O)c2[nH]c(-c3cnn(CC#Cc4ccccc4C(=O)OC)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2017.04.014
66892867 156319 None 0 Human Binding pKi = 7.9 7.9 27 3
Displacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting methodDisplacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting method
ChEMBL 479 7 1 8 2.4 CCCn1c(=O)c2[nH]c(-c3cnn(CC4CC(=O)N(c5ccc(F)cc5)C4)c3)nc2n(CC)c1=O 10.1016/j.ejmech.2016.11.007
CHEMBL4065629 156319 None 0 Human Binding pKi = 7.9 7.9 27 3
Displacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting methodDisplacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting method
ChEMBL 479 7 1 8 2.4 CCCn1c(=O)c2[nH]c(-c3cnn(CC4CC(=O)N(c5ccc(F)cc5)C4)c3)nc2n(CC)c1=O 10.1016/j.ejmech.2016.11.007
66892710 157536 None 0 Human Binding pKi = 7.9 7.9 - 1
Displacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting methodDisplacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting method
ChEMBL 475 8 1 8 3.4 CCCn1c(=O)c2[nH]c(-c3cnn(CC4CCN(c5ccc(C)cc5)C4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2016.11.007
CHEMBL4080098 157536 None 0 Human Binding pKi = 7.9 7.9 - 1
Displacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting methodDisplacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting method
ChEMBL 475 8 1 8 3.4 CCCn1c(=O)c2[nH]c(-c3cnn(CC4CCN(c5ccc(C)cc5)C4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2016.11.007
22266742 94567 None 0 Human Binding pKi = 7.9 7.9 - 1
Displacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranesDisplacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranes
ChEMBL 431 6 2 8 2.6 CC(C)Cn1c(=O)[nH]c2nc(-c3cnn(Cc4cc(-c5ccccc5)on4)c3)[nH]c2c1=O 10.1016/j.bmcl.2008.01.008
CHEMBL251880 94567 None 0 Human Binding pKi = 7.9 7.9 - 1
Displacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranesDisplacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranes
ChEMBL 431 6 2 8 2.6 CC(C)Cn1c(=O)[nH]c2nc(-c3cnn(Cc4cc(-c5ccccc5)on4)c3)[nH]c2c1=O 10.1016/j.bmcl.2008.01.008
16072024 58016 None 0 Human Binding pKi = 7.9 7.9 8 3
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 348 5 1 5 4.3 O=C(CC1CCCC1)Nc1cnc(-c2ccncc2)c(-c2ccco2)n1 10.1021/ml100249e
CHEMBL1672618 58016 None 0 Human Binding pKi = 7.9 7.9 8 3
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 348 5 1 5 4.3 O=C(CC1CCCC1)Nc1cnc(-c2ccncc2)c(-c2ccco2)n1 10.1021/ml100249e
50940964 57278 None 0 Human Binding pKi = 7.9 7.9 -3 4
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 269 3 1 5 3.0 CC(=O)Nc1cc(-c2ccco2)nc(-c2ccco2)n1 10.1021/jm100843z
CHEMBL1650384 57278 None 0 Human Binding pKi = 7.9 7.9 -3 4
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 269 3 1 5 3.0 CC(=O)Nc1cc(-c2ccco2)nc(-c2ccco2)n1 10.1021/jm100843z
136042329 71155 None 0 Human Binding pKi = 7.9 7.9 41 2
Displacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation countingDisplacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation counting
ChEMBL 534 10 2 11 2.7 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5cc(C(=O)OCC)ccc5[nH]4)nn3C)nc2n(CCC)c1=O 10.1021/jm201292w
CHEMBL1955904 71155 None 0 Human Binding pKi = 7.9 7.9 41 2
Displacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation countingDisplacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation counting
ChEMBL 534 10 2 11 2.7 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5cc(C(=O)OCC)ccc5[nH]4)nn3C)nc2n(CCC)c1=O 10.1021/jm201292w
135493279 100382 None 0 Human Binding pKi = 7.9 7.9 5 2
Displacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation countingDisplacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation counting
ChEMBL 483 9 2 9 2.3 CCCn1c(=O)c2nc(-c3cc(OCC(=O)Nc4ccc(F)cc4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm201292w
CHEMBL289903 100382 None 0 Human Binding pKi = 7.9 7.9 5 2
Displacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation countingDisplacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation counting
ChEMBL 483 9 2 9 2.3 CCCn1c(=O)c2nc(-c3cc(OCC(=O)Nc4ccc(F)cc4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm201292w
135874420 161302 None 0 Human Binding pKi = 7.9 7.9 - 1
Displacement of [3H]MRE2029F20 from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]MRE2029F20 from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 479 9 2 9 2.5 CCCn1c(=O)c2[nH]c(-c3cc(C)n(CC(=O)Nc4ccc(OC)cc4)n3)nc2n(CCC)c1=O 10.1016/j.bmc.2007.11.058
CHEMBL412284 161302 None 0 Human Binding pKi = 7.9 7.9 - 1
Displacement of [3H]MRE2029F20 from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]MRE2029F20 from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 479 9 2 9 2.5 CCCn1c(=O)c2[nH]c(-c3cc(C)n(CC(=O)Nc4ccc(OC)cc4)n3)nc2n(CCC)c1=O 10.1016/j.bmc.2007.11.058
52946453 19223 None 0 Human Binding pKi = 7.9 7.9 3 2
Displacement of [3H]ZM241385 from human adenosine A2B receptor transfected in CHO cells after 60 mins by scintillation countingDisplacement of [3H]ZM241385 from human adenosine A2B receptor transfected in CHO cells after 60 mins by scintillation counting
ChEMBL 521 9 2 5 5.6 O=C(COc1ccc2[nH]c(=O)c(-c3nccs3)c(CCc3ccccc3)c2c1)NC1(c2ccccc2)CC1 10.1016/j.bmcl.2010.10.030
CHEMBL1290001 19223 None 0 Human Binding pKi = 7.9 7.9 3 2
Displacement of [3H]ZM241385 from human adenosine A2B receptor transfected in CHO cells after 60 mins by scintillation countingDisplacement of [3H]ZM241385 from human adenosine A2B receptor transfected in CHO cells after 60 mins by scintillation counting
ChEMBL 521 9 2 5 5.6 O=C(COc1ccc2[nH]c(=O)c(-c3nccs3)c(CCc3ccccc3)c2c1)NC1(c2ccccc2)CC1 10.1016/j.bmcl.2010.10.030
11720113 74232 None 0 Human Binding pKi = 7.9 7.9 1 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 490 10 2 7 4.0 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(OC)cc4)cc3)cc2n(CCC)c1=O 10.1021/jm0506221
CHEMBL202358 74232 None 0 Human Binding pKi = 7.9 7.9 1 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 490 10 2 7 4.0 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(OC)cc4)cc3)cc2n(CCC)c1=O 10.1021/jm0506221
3909843 138972 None 14 Human Binding pKi = 7.9 7.9 - 1
Displacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting methodDisplacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting method
ChEMBL 323 3 1 6 3.5 CCOC(=O)C1=C(C)Nc2nc3ccccc3n2C1c1ccco1 10.1021/acs.jmedchem.0c00564
CHEMBL3785290 138972 None 14 Human Binding pKi = 7.9 7.9 - 1
Displacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting methodDisplacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting method
ChEMBL 323 3 1 6 3.5 CCOC(=O)C1=C(C)Nc2nc3ccccc3n2C1c1ccco1 10.1021/acs.jmedchem.0c00564
3909843 138972 None 14 Human Binding pKi = 7.9 7.9 - 1
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 minsDisplacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 mins
ChEMBL 323 3 1 6 3.5 CCOC(=O)C1=C(C)Nc2nc3ccccc3n2C1c1ccco1 10.1021/acs.jmedchem.5b01586
CHEMBL3785290 138972 None 14 Human Binding pKi = 7.9 7.9 - 1
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 minsDisplacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 mins
ChEMBL 323 3 1 6 3.5 CCOC(=O)C1=C(C)Nc2nc3ccccc3n2C1c1ccco1 10.1021/acs.jmedchem.5b01586
3909843 138972 None 14 Human Binding pKi = 7.9 7.9 - 1
Displacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assayDisplacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assay
ChEMBL 323 3 1 6 3.5 CCOC(=O)C1=C(C)Nc2nc3ccccc3n2C1c1ccco1 10.1021/acs.jmedchem.9b01340
CHEMBL3785290 138972 None 14 Human Binding pKi = 7.9 7.9 - 1
Displacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assayDisplacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assay
ChEMBL 323 3 1 6 3.5 CCOC(=O)C1=C(C)Nc2nc3ccccc3n2C1c1ccco1 10.1021/acs.jmedchem.9b01340
155545585 173456 None 0 Human Binding pKi = 7.9 7.9 19 3
Displacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 568 10 3 9 1.4 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc(OCCO)cc5)CC4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
CHEMBL4529435 173456 None 0 Human Binding pKi = 7.9 7.9 19 3
Displacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 568 10 3 9 1.4 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc(OCCO)cc5)CC4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
11561073 74756 None 0 Human Binding pKi = 7.9 7.9 13 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 432 7 2 6 3.1 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccccc4)cc3)cc2n(C)c1=O 10.1021/jm0506221
CHEMBL203088 74756 None 0 Human Binding pKi = 7.9 7.9 13 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 432 7 2 6 3.1 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccccc4)cc3)cc2n(C)c1=O 10.1021/jm0506221
11693081 138427 None 0 Human Binding pKi = 7.9 7.9 34 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 637 14 3 8 5.0 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(C(=O)NCCc5ccc(OC)cc5)cc4)cc3)cc2n(CCC)c1=O 10.1021/jm0506221
CHEMBL377434 138427 None 0 Human Binding pKi = 7.9 7.9 34 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 637 14 3 8 5.0 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(C(=O)NCCc5ccc(OC)cc5)cc4)cc3)cc2n(CCC)c1=O 10.1021/jm0506221
44450931 96037 None 0 Human Binding pKi = 7.9 7.9 64 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 472 5 1 6 3.0 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCC(c5ccccc5)CC4)cc3)cc2n(C)c1=O 10.1016/j.bmc.2008.01.002
CHEMBL259869 96037 None 0 Human Binding pKi = 7.9 7.9 64 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 472 5 1 6 3.0 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCC(c5ccccc5)CC4)cc3)cc2n(C)c1=O 10.1016/j.bmc.2008.01.002
11525776 73411 None 0 Human Binding pKi = 7.9 7.9 21 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 475 9 2 7 3.7 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(C)cn4)cc3)cc2n(CCC)c1=O 10.1021/jm0506221
CHEMBL201595 73411 None 0 Human Binding pKi = 7.9 7.9 21 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 475 9 2 7 3.7 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(C)cn4)cc3)cc2n(CCC)c1=O 10.1021/jm0506221
11548559 74237 None 0 Human Binding pKi = 7.9 7.9 1 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 556 9 2 6 4.9 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(F)cc4)cc3)c(Br)c2n(CCC)c1=O 10.1021/jm0506221
CHEMBL202359 74237 None 0 Human Binding pKi = 7.9 7.9 1 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 556 9 2 6 4.9 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(F)cc4)cc3)c(Br)c2n(CCC)c1=O 10.1021/jm0506221
449 2643 None 52 Rat Binding pKi = 7.9 7.9 -9 9
Binding affinity to rat A2B adenosine receptor by radio-ligand displacement assayBinding affinity to rat A2B adenosine receptor by radio-ligand displacement assay
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10.1021/acs.jmedchem.9b00071
453 2643 None 52 Rat Binding pKi = 7.9 7.9 -9 9
Binding affinity to rat A2B adenosine receptor by radio-ligand displacement assayBinding affinity to rat A2B adenosine receptor by radio-ligand displacement assay
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10.1021/acs.jmedchem.9b00071
6603931 2643 None 52 Rat Binding pKi = 7.9 7.9 -9 9
Binding affinity to rat A2B adenosine receptor by radio-ligand displacement assayBinding affinity to rat A2B adenosine receptor by radio-ligand displacement assay
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10.1021/acs.jmedchem.9b00071
CHEMBL273807 2643 None 52 Rat Binding pKi = 7.9 7.9 -9 9
Binding affinity to rat A2B adenosine receptor by radio-ligand displacement assayBinding affinity to rat A2B adenosine receptor by radio-ligand displacement assay
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10.1021/acs.jmedchem.9b00071
449 2643 None 52 Rat Binding pKi = 7.9 7.9 -9 9
Binding affinity to rat adenosine A2B receptorBinding affinity to rat adenosine A2B receptor
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10.1021/jm900413e
453 2643 None 52 Rat Binding pKi = 7.9 7.9 -9 9
Binding affinity to rat adenosine A2B receptorBinding affinity to rat adenosine A2B receptor
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10.1021/jm900413e
6603931 2643 None 52 Rat Binding pKi = 7.9 7.9 -9 9
Binding affinity to rat adenosine A2B receptorBinding affinity to rat adenosine A2B receptor
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10.1021/jm900413e
CHEMBL273807 2643 None 52 Rat Binding pKi = 7.9 7.9 -9 9
Binding affinity to rat adenosine A2B receptorBinding affinity to rat adenosine A2B receptor
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10.1021/jm900413e
136414902 159714 None 0 Human Binding pKi = 7.9 7.9 34 3
Displacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting methodDisplacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting method
ChEMBL 560 9 1 9 3.8 CCCn1c(=O)c2[nH]c(-c3cc(OCC4CC(=O)N(c5ccc(C(F)(F)F)cc5)C4)no3)nc2n(CCC)c1=O 10.1016/j.ejmech.2016.11.007
CHEMBL4104450 159714 None 0 Human Binding pKi = 7.9 7.9 34 3
Displacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting methodDisplacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting method
ChEMBL 560 9 1 9 3.8 CCCn1c(=O)c2[nH]c(-c3cc(OCC4CC(=O)N(c5ccc(C(F)(F)F)cc5)C4)no3)nc2n(CCC)c1=O 10.1016/j.ejmech.2016.11.007
449 2643 None 52 Rat Binding pKi = 7.9 7.9 -9 9
Inhibition of [125I]-APOBX binding to rat Adenosine A2B receptor expressed in HEK cellsInhibition of [125I]-APOBX binding to rat Adenosine A2B receptor expressed in HEK cells
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10.1021/jm0104318
453 2643 None 52 Rat Binding pKi = 7.9 7.9 -9 9
Inhibition of [125I]-APOBX binding to rat Adenosine A2B receptor expressed in HEK cellsInhibition of [125I]-APOBX binding to rat Adenosine A2B receptor expressed in HEK cells
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10.1021/jm0104318
6603931 2643 None 52 Rat Binding pKi = 7.9 7.9 -9 9
Inhibition of [125I]-APOBX binding to rat Adenosine A2B receptor expressed in HEK cellsInhibition of [125I]-APOBX binding to rat Adenosine A2B receptor expressed in HEK cells
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10.1021/jm0104318
CHEMBL273807 2643 None 52 Rat Binding pKi = 7.9 7.9 -9 9
Inhibition of [125I]-APOBX binding to rat Adenosine A2B receptor expressed in HEK cellsInhibition of [125I]-APOBX binding to rat Adenosine A2B receptor expressed in HEK cells
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10.1021/jm0104318
46228006 199698 None 0 Human Binding pKi = 7.9 7.9 2 3
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 364 5 0 7 2.1 CCn1c(=O)c2c(nc(Cc3ccccc3)n2C)n(Cc2ccco2)c1=O 10.1016/j.bmc.2009.07.034
CHEMBL593217 199698 None 0 Human Binding pKi = 7.9 7.9 2 3
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 364 5 0 7 2.1 CCn1c(=O)c2c(nc(Cc3ccccc3)n2C)n(Cc2ccco2)c1=O 10.1016/j.bmc.2009.07.034
137647216 157779 None 0 Human Binding pKi = 6.9 6.9 - 1
Displacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 minsDisplacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 mins
ChEMBL 423 7 1 8 1.7 CCCn1c(=O)c2[nH]c(-c3cnn(CC#CCN4CCCC4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2017.04.014
CHEMBL4082841 157779 None 0 Human Binding pKi = 6.9 6.9 - 1
Displacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 minsDisplacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 mins
ChEMBL 423 7 1 8 1.7 CCCn1c(=O)c2[nH]c(-c3cnn(CC#CCN4CCCC4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2017.04.014
22266753 96797 None 0 Human Binding pKi = 6.9 6.9 - 1
Displacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 260 2 2 6 -0.2 CCn1c(=O)c2[nH]c(-c3cn[nH]c3)nc2n(C)c1=O 10.1021/jm7014815
CHEMBL264952 96797 None 0 Human Binding pKi = 6.9 6.9 - 1
Displacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 260 2 2 6 -0.2 CCn1c(=O)c2[nH]c(-c3cn[nH]c3)nc2n(C)c1=O 10.1021/jm7014815
46228003 200018 None 0 Human Binding pKi = 6.9 6.9 3 3
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 356 5 1 7 2.2 CCn1c(=O)c2[nH]c(Cc3cccs3)nc2n(Cc2ccco2)c1=O 10.1016/j.bmc.2009.07.034
CHEMBL595431 200018 None 0 Human Binding pKi = 6.9 6.9 3 3
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 356 5 1 7 2.2 CCn1c(=O)c2[nH]c(Cc3cccs3)nc2n(Cc2ccco2)c1=O 10.1016/j.bmc.2009.07.034
11381738 195048 None 0 Human Binding pKi = 6.9 6.9 -19 4
Binding affinity to adenosine A2B receptorBinding affinity to adenosine A2B receptor
ChEMBL 324 5 2 6 2.3 COc1cccc(CNC(=O)c2cc(-c3ccco3)nc(N)n2)c1 10.1016/j.bmcl.2009.03.142
CHEMBL549477 195048 None 0 Human Binding pKi = 6.9 6.9 -19 4
Binding affinity to adenosine A2B receptorBinding affinity to adenosine A2B receptor
ChEMBL 324 5 2 6 2.3 COc1cccc(CNC(=O)c2cc(-c3ccco3)nc(N)n2)c1 10.1016/j.bmcl.2009.03.142
10918042 120084 None 0 Human Binding pKi = 6.9 6.9 -4 4
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 88-165Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 88-165
ChEMBL 494 6 2 8 4.9 CCCCn1cc2c(nc(NC(=O)Nc3ccc(Br)cc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm0109614
CHEMBL350830 120084 None 0 Human Binding pKi = 6.9 6.9 -4 4
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 88-165Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 88-165
ChEMBL 494 6 2 8 4.9 CCCCn1cc2c(nc(NC(=O)Nc3ccc(Br)cc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm0109614
44406398 72984 None 0 Human Binding pKi = 6.9 6.9 30 3
Displacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cellsDisplacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cells
ChEMBL 527 8 1 9 4.3 CCCn1c(=O)c2nc(-c3cnn(Cc4cc(-c5ccccc5C(F)(F)F)on4)c3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2005.10.002
CHEMBL200739 72984 None 0 Human Binding pKi = 6.9 6.9 30 3
Displacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cellsDisplacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cells
ChEMBL 527 8 1 9 4.3 CCCn1c(=O)c2nc(-c3cnn(Cc4cc(-c5ccccc5C(F)(F)F)on4)c3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2005.10.002
9805713 162846 None 0 Human Binding pKi = 4.9 4.9 -2238 6
Displacement of [3H]- ZM-241385 from human adenosine A2B receptor expressed in HEK cellsDisplacement of [3H]- ZM-241385 from human adenosine A2B receptor expressed in HEK cells
ChEMBL 493 5 4 8 1.3 OC[C@@]12C[C@@H]1[C@@H](n1cnc3c(NCc4cccc(I)c4)ncnc31)[C@H](O)[C@@H]2O 10.1021/jm9905965
CHEMBL417292 162846 None 0 Human Binding pKi = 4.9 4.9 -2238 6
Displacement of [3H]- ZM-241385 from human adenosine A2B receptor expressed in HEK cellsDisplacement of [3H]- ZM-241385 from human adenosine A2B receptor expressed in HEK cells
ChEMBL 493 5 4 8 1.3 OC[C@@]12C[C@@H]1[C@@H](n1cnc3c(NCc4cccc(I)c4)ncnc31)[C@H](O)[C@@H]2O 10.1021/jm9905965
135522362 100021 None 0 Human Binding pKi = 6.9 6.9 - 1
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 472 8 1 10 0.3 CCCn1c(=O)c2nc(-c3cc(OCC(=O)N4CCN(C)CC4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
CHEMBL286838 100021 None 0 Human Binding pKi = 6.9 6.9 - 1
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 472 8 1 10 0.3 CCCn1c(=O)c2nc(-c3cc(OCC(=O)N4CCN(C)CC4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
11531253 77365 None 0 Human Binding pKi = 6.9 6.9 -4 3
Displacement of [3H]PSB298 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB298 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 391 6 2 7 0.7 CCCCNS(=O)(=O)c1ccc(-c2nc3c(=O)n(C)c(=O)n(C)c3[nH]2)cc1 10.1021/jm060277v
CHEMBL208550 77365 None 0 Human Binding pKi = 6.9 6.9 -4 3
Displacement of [3H]PSB298 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB298 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 391 6 2 7 0.7 CCCCNS(=O)(=O)c1ccc(-c2nc3c(=O)n(C)c(=O)n(C)c3[nH]2)cc1 10.1021/jm060277v
21874685 188896 None 0 Human Binding pKi = 6.9 6.9 -64 4
Displacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation countingDisplacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation counting
ChEMBL 292 3 1 7 2.1 Nc1nc(-c2ccco2)c2nnn(Cc3ccccc3)c2n1 10.1021/jm800961g
CHEMBL507426 188896 None 0 Human Binding pKi = 6.9 6.9 -64 4
Displacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation countingDisplacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation counting
ChEMBL 292 3 1 7 2.1 Nc1nc(-c2ccco2)c2nnn(Cc3ccccc3)c2n1 10.1021/jm800961g
44406570 72848 None 0 Human Binding pKi = 6.9 6.9 18 3
Displacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cellsDisplacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cells
ChEMBL 490 9 1 11 2.7 CCCn1c(=O)c2nc(-c3cnn(Cc4noc(-c5ccc(OC)cc5)n4)c3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2005.10.002
CHEMBL200230 72848 None 0 Human Binding pKi = 6.9 6.9 18 3
Displacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cellsDisplacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cells
ChEMBL 490 9 1 11 2.7 CCCn1c(=O)c2nc(-c3cnn(Cc4noc(-c5ccc(OC)cc5)n4)c3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2005.10.002
9857735 189827 None 0 Human Binding pKi = 6.9 6.9 -61 4
Displacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation countingDisplacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation counting
ChEMBL 307 3 2 8 1.7 Nc1nc(-c2ccco2)c2nnn(Cc3ccccc3N)c2n1 10.1021/jm800961g
CHEMBL516483 189827 None 0 Human Binding pKi = 6.9 6.9 -61 4
Displacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation countingDisplacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation counting
ChEMBL 307 3 2 8 1.7 Nc1nc(-c2ccco2)c2nnn(Cc3ccccc3N)c2n1 10.1021/jm800961g
11503979 73406 None 0 Human Binding pKi = 6.9 6.9 1 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 482 7 2 7 2.6 COc1cc(OCC(=O)NCc2ccc(Cl)cc2)ccc1-c1cc2c([nH]1)c(=O)n(C)c(=O)n2C 10.1021/jm0506221
CHEMBL201580 73406 None 0 Human Binding pKi = 6.9 6.9 1 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 482 7 2 7 2.6 COc1cc(OCC(=O)NCc2ccc(Cl)cc2)ccc1-c1cc2c([nH]1)c(=O)n(C)c(=O)n2C 10.1021/jm0506221
11645609 141044 None 0 Human Binding pKi = 6.9 6.9 33 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 329 4 2 6 0.7 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)O)cc3)cc2n(C)c1=O 10.1021/jm0506221
CHEMBL382413 141044 None 0 Human Binding pKi = 6.9 6.9 33 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 329 4 2 6 0.7 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)O)cc3)cc2n(C)c1=O 10.1021/jm0506221
44452535 155772 None 0 Human Binding pKi = 6.9 6.9 -38 4
Displacement of [3]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 295 4 2 7 1.9 OCCNc1nc2ccccc2n2nc(-c3ccco3)nc12 10.1016/j.bmc.2007.10.103
CHEMBL405868 155772 None 0 Human Binding pKi = 6.9 6.9 -38 4
Displacement of [3]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 295 4 2 7 1.9 OCCNc1nc2ccccc2n2nc(-c3ccco3)nc12 10.1016/j.bmc.2007.10.103
45273122 195769 None 0 Human Binding pKi = 5.9 5.9 -128 4
Binding affinity to adenosine A2B receptorBinding affinity to adenosine A2B receptor
ChEMBL 308 4 2 5 2.6 Cc1ccc(CNC(=O)c2cc(-c3ccco3)nc(N)n2)cc1 10.1016/j.bmcl.2009.03.142
CHEMBL557696 195769 None 0 Human Binding pKi = 5.9 5.9 -128 4
Binding affinity to adenosine A2B receptorBinding affinity to adenosine A2B receptor
ChEMBL 308 4 2 5 2.6 Cc1ccc(CNC(=O)c2cc(-c3ccco3)nc(N)n2)cc1 10.1016/j.bmcl.2009.03.142
136044108 129692 None 0 Human Binding pKi = 6.9 6.9 -3 2
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 344 5 3 7 1.8 CCCn1c(=O)c2nc(-c3cccc(O)c3O)[nH]c2n(CCC)c1=O 10.1021/jm0104318
CHEMBL36740 129692 None 0 Human Binding pKi = 6.9 6.9 -3 2
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 344 5 3 7 1.8 CCCn1c(=O)c2nc(-c3cccc(O)c3O)[nH]c2n(CCC)c1=O 10.1021/jm0104318
11059351 119945 None 0 Human Binding pKi = 6.9 6.9 -6 4
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 116-134Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 116-134
ChEMBL 446 7 2 9 4.2 CCCCn1cc2c(nc(NC(=O)Nc3ccccc3OC)n3nc(-c4ccco4)nc23)n1 10.1021/jm0109614
CHEMBL349611 119945 None 0 Human Binding pKi = 6.9 6.9 -6 4
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 116-134Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 116-134
ChEMBL 446 7 2 9 4.2 CCCCn1cc2c(nc(NC(=O)Nc3ccccc3OC)n3nc(-c4ccco4)nc23)n1 10.1021/jm0109614
45268920 196686 None 0 Human Binding pKi = 6.9 6.9 1 2
Binding affinity to human adenosine A2b receptor expressed in HEK293 cellsBinding affinity to human adenosine A2b receptor expressed in HEK293 cells
ChEMBL 334 6 1 7 1.7 CCn1c(=O)c2[nH]c(-c3cccs3)nc2n(CCCOC)c1=O 10.1016/j.bmc.2009.03.029
CHEMBL564680 196686 None 0 Human Binding pKi = 6.9 6.9 1 2
Binding affinity to human adenosine A2b receptor expressed in HEK293 cellsBinding affinity to human adenosine A2b receptor expressed in HEK293 cells
ChEMBL 334 6 1 7 1.7 CCn1c(=O)c2[nH]c(-c3cccs3)nc2n(CCCOC)c1=O 10.1016/j.bmc.2009.03.029
46228002 201445 None 0 Human Binding pKi = 6.9 6.9 4 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 340 5 1 7 1.7 CCn1c(=O)c2[nH]c(Cc3ccco3)nc2n(Cc2ccco2)c1=O 10.1016/j.bmc.2009.07.034
CHEMBL604896 201445 None 0 Human Binding pKi = 6.9 6.9 4 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 340 5 1 7 1.7 CCn1c(=O)c2[nH]c(Cc3ccco3)nc2n(Cc2ccco2)c1=O 10.1016/j.bmc.2009.07.034
11582537 169301 None 0 Human Binding pKi = 5.9 5.9 -2 3
Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cellsDisplacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells
ChEMBL 420 7 1 7 3.1 CC(C)Cn1c(=O)c2nc(-c3cnn(Cc4ccccc4)c3)[nH]c2n(CC(C)C)c1=O 10.1021/jm051268+
CHEMBL441530 169301 None 0 Human Binding pKi = 5.9 5.9 -2 3
Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cellsDisplacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells
ChEMBL 420 7 1 7 3.1 CC(C)Cn1c(=O)c2nc(-c3cnn(Cc4ccccc4)c3)[nH]c2n(CC(C)C)c1=O 10.1021/jm051268+
54577823 80997 None 0 Human Binding pKi = 4.9 4.9 -30 5
Displacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cells
ChEMBL 289 2 0 7 0.1 Cn1c(=O)c2c(nc3n2CCCN3CC2CC2)n(C)c1=O 10.1016/j.ejmech.2011.05.023
CHEMBL2153627 80997 None 0 Human Binding pKi = 4.9 4.9 -30 5
Displacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cells
ChEMBL 289 2 0 7 0.1 Cn1c(=O)c2c(nc3n2CCCN3CC2CC2)n(C)c1=O 10.1016/j.ejmech.2011.05.023
70696537 75450 None 0 Human Binding pKi = 5.9 5.9 -1 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by beta scintillation countingDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by beta scintillation counting
ChEMBL 304 7 3 5 1.8 COc1cccc2cc(C(=O)NCCCCCO)c(=N)oc12 10.1016/j.ejmech.2012.05.009
CHEMBL2042075 75450 None 0 Human Binding pKi = 5.9 5.9 -1 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by beta scintillation countingDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by beta scintillation counting
ChEMBL 304 7 3 5 1.8 COc1cccc2cc(C(=O)NCCCCCO)c(=N)oc12 10.1016/j.ejmech.2012.05.009
145987354 167163 None 0 Human Binding pKi = 6.9 6.9 -5 4
Displacement of [3H]PSB-602 from human adenosine A2B receptor expressed in CHO cell membranesDisplacement of [3H]PSB-602 from human adenosine A2B receptor expressed in CHO cell membranes
ChEMBL 609 18 1 10 3.6 CCCCn1c(=O)c2c(nc3n2CCCN3CCc2ccc(OCC(=O)NCCCN(CC)CC)cc2)n(CCCC)c1=O 10.1039/C8MD00070K
CHEMBL4291015 167163 None 0 Human Binding pKi = 6.9 6.9 -5 4
Displacement of [3H]PSB-602 from human adenosine A2B receptor expressed in CHO cell membranesDisplacement of [3H]PSB-602 from human adenosine A2B receptor expressed in CHO cell membranes
ChEMBL 609 18 1 10 3.6 CCCCn1c(=O)c2c(nc3n2CCCN3CCc2ccc(OCC(=O)NCCCN(CC)CC)cc2)n(CCCC)c1=O 10.1039/C8MD00070K
44410566 141379 None 0 Human Binding pKi = 5.9 5.9 -1071 4
Displacement of [125I]ABOPX from human adenosine A2B receptor in HEK cellsDisplacement of [125I]ABOPX from human adenosine A2B receptor in HEK cells
ChEMBL 496 7 5 11 0.1 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC)nc(C#CC(O)c4cccc(OC)c4)nc32)[C@H](O)[C@@H]1O 10.1016/j.bmcl.2006.01.110
CHEMBL383836 141379 None 0 Human Binding pKi = 5.9 5.9 -1071 4
Displacement of [125I]ABOPX from human adenosine A2B receptor in HEK cellsDisplacement of [125I]ABOPX from human adenosine A2B receptor in HEK cells
ChEMBL 496 7 5 11 0.1 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC)nc(C#CC(O)c4cccc(OC)c4)nc32)[C@H](O)[C@@H]1O 10.1016/j.bmcl.2006.01.110
10311510 123572 None 0 Human Binding pKi = 6.9 6.9 -25 4
Binding affinity against Adenosine A2b receptor labeled by [3H]ZM-241385 in membranes prepared from HEK-A2B cellsBinding affinity against Adenosine A2b receptor labeled by [3H]ZM-241385 in membranes prepared from HEK-A2B cells
ChEMBL 516 10 1 10 4.0 CCCn1c(=O)c2nc(-c3ccc(OCc4noc(-c5ccccc5OC)n4)cc3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2004.11.044
CHEMBL361826 123572 None 0 Human Binding pKi = 6.9 6.9 -25 4
Binding affinity against Adenosine A2b receptor labeled by [3H]ZM-241385 in membranes prepared from HEK-A2B cellsBinding affinity against Adenosine A2b receptor labeled by [3H]ZM-241385 in membranes prepared from HEK-A2B cells
ChEMBL 516 10 1 10 4.0 CCCn1c(=O)c2nc(-c3ccc(OCc4noc(-c5ccccc5OC)n4)cc3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2004.11.044
10311510 123572 None 0 Human Binding pKi = 6.9 6.9 -25 4
Binding affinity for adenosine A2b receptor by using as [3H]ZM-241385 (14 nM) radioligand in membranes from HEK-A2B cellsBinding affinity for adenosine A2b receptor by using as [3H]ZM-241385 (14 nM) radioligand in membranes from HEK-A2B cells
ChEMBL 516 10 1 10 4.0 CCCn1c(=O)c2nc(-c3ccc(OCc4noc(-c5ccccc5OC)n4)cc3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2004.11.044
CHEMBL361826 123572 None 0 Human Binding pKi = 6.9 6.9 -25 4
Binding affinity for adenosine A2b receptor by using as [3H]ZM-241385 (14 nM) radioligand in membranes from HEK-A2B cellsBinding affinity for adenosine A2b receptor by using as [3H]ZM-241385 (14 nM) radioligand in membranes from HEK-A2B cells
ChEMBL 516 10 1 10 4.0 CCCn1c(=O)c2nc(-c3ccc(OCc4noc(-c5ccccc5OC)n4)cc3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2004.11.044
9954406 96700 None 0 Human Binding pKi = 6.9 6.9 -31 3
Displacement of [125I]3-(4-aminobenzyl)-8-phenyloxyacetate-1-propyl-xanthine from human adenosine A2B receptor expressed in HEK cellsDisplacement of [125I]3-(4-aminobenzyl)-8-phenyloxyacetate-1-propyl-xanthine from human adenosine A2B receptor expressed in HEK cells
ChEMBL 430 9 2 6 3.6 CCCn1c(=O)c2nc([C@]34CC[C@](CCCC(=O)O)(CC3)CC4)[nH]c2n(CCC)c1=O 10.1021/jm0605381
CHEMBL264070 96700 None 0 Human Binding pKi = 6.9 6.9 -31 3
Displacement of [125I]3-(4-aminobenzyl)-8-phenyloxyacetate-1-propyl-xanthine from human adenosine A2B receptor expressed in HEK cellsDisplacement of [125I]3-(4-aminobenzyl)-8-phenyloxyacetate-1-propyl-xanthine from human adenosine A2B receptor expressed in HEK cells
ChEMBL 430 9 2 6 3.6 CCCn1c(=O)c2nc([C@]34CC[C@](CCCC(=O)O)(CC3)CC4)[nH]c2n(CCC)c1=O 10.1021/jm0605381
377 2758 None 53 Human Binding pKi = 5.9 5.9 -1479 15
Displacement of [3H]MRS1754 from human adenosine A2B receptor expressed in CHO cell membraneDisplacement of [3H]MRS1754 from human adenosine A2B receptor expressed in CHO cell membrane
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm701594y
425 2758 None 53 Human Binding pKi = 5.9 5.9 -1479 15
Displacement of [3H]MRS1754 from human adenosine A2B receptor expressed in CHO cell membraneDisplacement of [3H]MRS1754 from human adenosine A2B receptor expressed in CHO cell membrane
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm701594y
448222 2758 None 53 Human Binding pKi = 5.9 5.9 -1479 15
Displacement of [3H]MRS1754 from human adenosine A2B receptor expressed in CHO cell membraneDisplacement of [3H]MRS1754 from human adenosine A2B receptor expressed in CHO cell membrane
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm701594y
CHEMBL464859 2758 None 53 Human Binding pKi = 5.9 5.9 -1479 15
Displacement of [3H]MRS1754 from human adenosine A2B receptor expressed in CHO cell membraneDisplacement of [3H]MRS1754 from human adenosine A2B receptor expressed in CHO cell membrane
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm701594y
10431614 58131 None 0 Human Binding pKi = 6.9 6.9 -14 4
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 115-143Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 115-143
ChEMBL 408 3 2 8 3.6 Cn1cc2c(nc(NC(=O)Nc3ccc(Cl)cc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm0109614
CHEMBL167753 58131 None 0 Human Binding pKi = 6.9 6.9 -14 4
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 115-143Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 115-143
ChEMBL 408 3 2 8 3.6 Cn1cc2c(nc(NC(=O)Nc3ccc(Cl)cc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm0109614
44406582 72885 None 0 Human Binding pKi = 6.9 6.9 7 3
Displacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cellsDisplacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cells
ChEMBL 474 8 1 10 3.0 CCCn1c(=O)c2nc(-c3cnn(Cc4nc(-c5cccc(C)c5)no4)c3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2005.10.002
CHEMBL200350 72885 None 0 Human Binding pKi = 6.9 6.9 7 3
Displacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cellsDisplacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cells
ChEMBL 474 8 1 10 3.0 CCCn1c(=O)c2nc(-c3cnn(Cc4nc(-c5cccc(C)c5)no4)c3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2005.10.002
21874721 178587 None 0 Human Binding pKi = 6.9 6.9 -58 4
Displacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation countingDisplacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation counting
ChEMBL 328 3 1 7 2.4 Nc1nc(-c2ccco2)c2nnn(Cc3cc(F)ccc3F)c2n1 10.1021/jm800961g
CHEMBL467245 178587 None 0 Human Binding pKi = 6.9 6.9 -58 4
Displacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation countingDisplacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation counting
ChEMBL 328 3 1 7 2.4 Nc1nc(-c2ccco2)c2nnn(Cc3cc(F)ccc3F)c2n1 10.1021/jm800961g
21874639 178653 None 0 Human Binding pKi = 5.9 5.9 -3 4
Displacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation countingDisplacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation counting
ChEMBL 311 3 2 8 0.8 Nc1nc(-c2cnn[nH]2)c2nnn(Cc3ccccc3F)c2n1 10.1021/jm800961g
CHEMBL467655 178653 None 0 Human Binding pKi = 5.9 5.9 -3 4
Displacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation countingDisplacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation counting
ChEMBL 311 3 2 8 0.8 Nc1nc(-c2cnn[nH]2)c2nnn(Cc3ccccc3F)c2n1 10.1021/jm800961g
11282829 206011 None 0 Human Binding pKi = 7.9 7.9 -1 3
Binding affinity for human adenosine A2B receptor using [3H]-PSB-298 in CHO cell membranesBinding affinity for human adenosine A2B receptor using [3H]-PSB-298 in CHO cell membranes
ChEMBL 471 7 2 9 2.2 CCCn1c(=O)[nH]c2[nH]c(-c3ccc(S(=O)(=O)Oc4cccc([N+](=O)[O-])c4)cc3)nc2c1=O 10.1021/jm0310030
CHEMBL8495 206011 None 0 Human Binding pKi = 7.9 7.9 -1 3
Binding affinity for human adenosine A2B receptor using [3H]-PSB-298 in CHO cell membranesBinding affinity for human adenosine A2B receptor using [3H]-PSB-298 in CHO cell membranes
ChEMBL 471 7 2 9 2.2 CCCn1c(=O)[nH]c2[nH]c(-c3ccc(S(=O)(=O)Oc4cccc([N+](=O)[O-])c4)cc3)nc2c1=O 10.1021/jm0310030
135443378 109637 None 0 Human Binding pKi = 7.9 7.9 4 2
Binding affinity of compound for displacement of [3H]DPCPX binding in HEK293 membranes expressing human A2B adenosine receptorsBinding affinity of compound for displacement of [3H]DPCPX binding in HEK293 membranes expressing human A2B adenosine receptors
ChEMBL 623 11 2 9 4.9 CCCn1c(=O)c2nc(-c3cc(NC(=O)Cc4ccc(OCc5ccccc5C(F)(F)F)cc4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
CHEMBL32229 109637 None 0 Human Binding pKi = 7.9 7.9 4 2
Binding affinity of compound for displacement of [3H]DPCPX binding in HEK293 membranes expressing human A2B adenosine receptorsBinding affinity of compound for displacement of [3H]DPCPX binding in HEK293 membranes expressing human A2B adenosine receptors
ChEMBL 623 11 2 9 4.9 CCCn1c(=O)c2nc(-c3cc(NC(=O)Cc4ccc(OCc5ccccc5C(F)(F)F)cc4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
135443378 109637 None 0 Human Binding pKi = 7.9 7.9 4 2
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 623 11 2 9 4.9 CCCn1c(=O)c2nc(-c3cc(NC(=O)Cc4ccc(OCc5ccccc5C(F)(F)F)cc4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
CHEMBL32229 109637 None 0 Human Binding pKi = 7.9 7.9 4 2
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 623 11 2 9 4.9 CCCn1c(=O)c2nc(-c3cc(NC(=O)Cc4ccc(OCc5ccccc5C(F)(F)F)cc4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
57429602 157239 None 0 Human Binding pKi = 7.9 7.9 - 1
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 500 7 1 8 3.5 CCCn1c(=O)c2[nH]c(-c3cnn(CC#Cc4cccc(OC(F)(F)F)c4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2021.113907
CHEMBL4076435 157239 None 0 Human Binding pKi = 7.9 7.9 - 1
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 500 7 1 8 3.5 CCCn1c(=O)c2[nH]c(-c3cnn(CC#Cc4cccc(OC(F)(F)F)c4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2021.113907
44236568 156470 None 0 Human Binding pKi = 7.9 7.9 - 1
Displacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 minsDisplacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 mins
ChEMBL 486 6 1 8 3.1 CCCn1c(=O)c2[nH]c(-c3cnn(CC#Cc4cccc(OC(F)(F)F)c4)c3)nc2n(CC)c1=O 10.1016/j.ejmech.2017.04.014
CHEMBL4067401 156470 None 0 Human Binding pKi = 7.9 7.9 - 1
Displacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 minsDisplacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 mins
ChEMBL 486 6 1 8 3.1 CCCn1c(=O)c2[nH]c(-c3cnn(CC#Cc4cccc(OC(F)(F)F)c4)c3)nc2n(CC)c1=O 10.1016/j.ejmech.2017.04.014
69028196 159563 None 0 Human Binding pKi = 7.9 7.9 - 1
Displacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting methodDisplacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting method
ChEMBL 491 9 1 9 3.1 CCCn1c(=O)c2[nH]c(-c3cnn(CC4CCN(c5ccc(OC)cc5)C4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2016.11.007
CHEMBL4102641 159563 None 0 Human Binding pKi = 7.9 7.9 - 1
Displacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting methodDisplacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting method
ChEMBL 491 9 1 9 3.1 CCCn1c(=O)c2[nH]c(-c3cnn(CC4CCN(c5ccc(OC)cc5)C4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2016.11.007
21958783 94593 None 0 Human Binding pKi = 7.9 7.9 85 2
Displacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranesDisplacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranes
ChEMBL 364 5 2 6 2.0 CC(C)Cn1c(=O)[nH]c2nc(-c3cnn(Cc4ccccc4)c3)[nH]c2c1=O 10.1016/j.bmcl.2008.01.008
CHEMBL252068 94593 None 0 Human Binding pKi = 7.9 7.9 85 2
Displacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranesDisplacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranes
ChEMBL 364 5 2 6 2.0 CC(C)Cn1c(=O)[nH]c2nc(-c3cnn(Cc4ccccc4)c3)[nH]c2c1=O 10.1016/j.bmcl.2008.01.008
22266766 155471 None 0 Human Binding pKi = 7.9 7.9 - 1
Displacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranesDisplacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranes
ChEMBL 498 6 2 9 2.8 O=c1[nH]c2nc(-c3cnn(Cc4noc(-c5ccc(C(F)(F)F)cc5)n4)c3)[nH]c2c(=O)n1CC1CC1 10.1016/j.bmcl.2008.01.008
CHEMBL403975 155471 None 0 Human Binding pKi = 7.9 7.9 - 1
Displacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranesDisplacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranes
ChEMBL 498 6 2 9 2.8 O=c1[nH]c2nc(-c3cnn(Cc4noc(-c5ccc(C(F)(F)F)cc5)n4)c3)[nH]c2c(=O)n1CC1CC1 10.1016/j.bmcl.2008.01.008
10308937 155500 None 0 Human Binding pKi = 7.9 7.9 9 3
Displacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranesDisplacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranes
ChEMBL 350 5 2 6 1.7 CCCn1c(=O)[nH]c2nc(-c3cnn(Cc4ccccc4)c3)[nH]c2c1=O 10.1016/j.bmcl.2008.01.008
CHEMBL404130 155500 None 0 Human Binding pKi = 7.9 7.9 9 3
Displacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranesDisplacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranes
ChEMBL 350 5 2 6 1.7 CCCn1c(=O)[nH]c2nc(-c3cnn(Cc4ccccc4)c3)[nH]c2c1=O 10.1016/j.bmcl.2008.01.008
11952665 6050 None 0 Human Binding pKi = 7.9 7.9 19 3
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 262 2 1 4 3.3 c1coc(-c2nc3[nH]ccc3cc2-c2ccncn2)c1 10.1016/j.bmcl.2010.01.077
CHEMBL1080512 6050 None 0 Human Binding pKi = 7.9 7.9 19 3
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 262 2 1 4 3.3 c1coc(-c2nc3[nH]ccc3cc2-c2ccncn2)c1 10.1016/j.bmcl.2010.01.077
53318744 58014 None 0 Human Binding pKi = 7.9 7.9 2 4
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 334 4 1 5 3.9 O=C(Nc1cnc(-c2ccncc2)c(-c2ccco2)n1)C1CCCC1 10.1021/ml100249e
CHEMBL1672616 58014 None 0 Human Binding pKi = 7.9 7.9 2 4
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 334 4 1 5 3.9 O=C(Nc1cnc(-c2ccncc2)c(-c2ccco2)n1)C1CCCC1 10.1021/ml100249e
11690561 78302 None 0 Human Binding pKi = 7.9 7.9 34 3
Displacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 432 5 1 7 2.9 CCn1c(=O)c2nc(-c3cnn(Cc4cccc(C(F)(F)F)c4)c3)[nH]c2n(CC)c1=O 10.1021/jm7014815
CHEMBL210808 78302 None 0 Human Binding pKi = 7.9 7.9 34 3
Displacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 432 5 1 7 2.9 CCn1c(=O)c2nc(-c3cnn(Cc4cccc(C(F)(F)F)c4)c3)[nH]c2n(CC)c1=O 10.1021/jm7014815
21958583 96245 None 0 Human Binding pKi = 7.9 7.9 7 4
Displacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 382 5 1 7 1.9 CCCn1c(=O)c2[nH]c(-c3cnn(Cc4cccc(F)c4)c3)nc2n(C)c1=O 10.1021/jm7014815
CHEMBL260976 96245 None 0 Human Binding pKi = 7.9 7.9 7 4
Displacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 382 5 1 7 1.9 CCCn1c(=O)c2[nH]c(-c3cnn(Cc4cccc(F)c4)c3)nc2n(C)c1=O 10.1021/jm7014815
9930130 10801 None 0 Human Binding pKi = 7.9 7.9 1 3
Displacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cells after 1 hr by scintillation countingDisplacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 387 5 1 5 4.1 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(F)cc3)sc12 10.1016/j.bmcl.2010.05.056
CHEMBL1171897 10801 None 0 Human Binding pKi = 7.9 7.9 1 3
Displacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cells after 1 hr by scintillation countingDisplacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 387 5 1 5 4.1 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(F)cc3)sc12 10.1016/j.bmcl.2010.05.056
49798140 10870 None 0 Human Binding pKi = 7.9 7.9 2 3
Displacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cells after 1 hr by scintillation countingDisplacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 484 9 1 7 3.6 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(C(=O)N(C)CCOC)cc3)sc12 10.1016/j.bmcl.2010.05.056
CHEMBL1172442 10870 None 0 Human Binding pKi = 7.9 7.9 2 3
Displacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cells after 1 hr by scintillation countingDisplacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 484 9 1 7 3.6 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(C(=O)N(C)CCOC)cc3)sc12 10.1016/j.bmcl.2010.05.056
11690561 78302 None 0 Human Binding pKi = 7.9 7.9 34 3
Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cellsDisplacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells
ChEMBL 432 5 1 7 2.9 CCn1c(=O)c2nc(-c3cnn(Cc4cccc(C(F)(F)F)c4)c3)[nH]c2n(CC)c1=O 10.1021/jm051268+
CHEMBL210808 78302 None 0 Human Binding pKi = 7.9 7.9 34 3
Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cellsDisplacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells
ChEMBL 432 5 1 7 2.9 CCn1c(=O)c2nc(-c3cnn(Cc4cccc(C(F)(F)F)c4)c3)[nH]c2n(CC)c1=O 10.1021/jm051268+
10970525 99947 None 0 Human Binding pKi = 7.9 7.9 8 3
Inhibition of [3H]ZM-241385 binding to human adenosine A2B receptorInhibition of [3H]ZM-241385 binding to human adenosine A2B receptor
ChEMBL 364 4 3 5 2.3 CCCn1c(=O)[nH]c2[nH]c(-c3ccc4cc(C(=O)O)ccc4c3)nc2c1=O 10.1021/jm011049y
CHEMBL286350 99947 None 0 Human Binding pKi = 7.9 7.9 8 3
Inhibition of [3H]ZM-241385 binding to human adenosine A2B receptorInhibition of [3H]ZM-241385 binding to human adenosine A2B receptor
ChEMBL 364 4 3 5 2.3 CCCn1c(=O)[nH]c2[nH]c(-c3ccc4cc(C(=O)O)ccc4c3)nc2c1=O 10.1021/jm011049y
44451252 95976 None 0 Human Binding pKi = 7.9 7.9 12 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 503 6 1 8 2.0 COc1ccc(N2CCN(C(=O)COc3ccc(-c4cc5c([nH]4)c(=O)n(C)c(=O)n5C)cc3)CC2)cc1 10.1016/j.bmc.2008.01.002
CHEMBL259529 95976 None 0 Human Binding pKi = 7.9 7.9 12 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 503 6 1 8 2.0 COc1ccc(N2CCN(C(=O)COc3ccc(-c4cc5c([nH]4)c(=O)n(C)c(=O)n5C)cc3)CC2)cc1 10.1016/j.bmc.2008.01.002
44451050 95987 None 0 Human Binding pKi = 7.9 7.9 23 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 501 7 1 7 2.8 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCN(c5ccccc5)CC4)cc3)cc2n(C)c1=O 10.1016/j.bmc.2008.01.002
CHEMBL259581 95987 None 0 Human Binding pKi = 7.9 7.9 23 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 501 7 1 7 2.8 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCN(c5ccccc5)CC4)cc3)cc2n(C)c1=O 10.1016/j.bmc.2008.01.002
168292492 191640 None 0 Human Binding pKi = 7.9 7.9 - 1
Displacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cell membrane preincubated for 4 hrs followed by [3H]PSB-603 addition and measured after 0.5 hrs by radioligand displacement assayDisplacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cell membrane preincubated for 4 hrs followed by [3H]PSB-603 addition and measured after 0.5 hrs by radioligand displacement assay
ChEMBL 352 4 2 6 1.1 CCCn1c(=O)[nH]c2nc(-c3cccc(S(=O)(=O)F)c3)[nH]c2c1=O 10.1039/d2md00132b
CHEMBL5195884 191640 None 0 Human Binding pKi = 7.9 7.9 - 1
Displacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cell membrane preincubated for 4 hrs followed by [3H]PSB-603 addition and measured after 0.5 hrs by radioligand displacement assayDisplacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cell membrane preincubated for 4 hrs followed by [3H]PSB-603 addition and measured after 0.5 hrs by radioligand displacement assay
ChEMBL 352 4 2 6 1.1 CCCn1c(=O)[nH]c2nc(-c3cccc(S(=O)(=O)F)c3)[nH]c2c1=O 10.1039/d2md00132b
10377463 96313 None 0 Human Binding pKi = 7.9 7.9 -2 4
Displacement of [3]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 251 1 1 6 2.1 Nc1nc2ccccc2n2nc(-c3ccco3)nc12 10.1016/j.bmc.2007.10.103
CHEMBL261345 96313 None 0 Human Binding pKi = 7.9 7.9 -2 4
Displacement of [3]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 251 1 1 6 2.1 Nc1nc2ccccc2n2nc(-c3ccco3)nc12 10.1016/j.bmc.2007.10.103
136042347 71175 None 0 Human Binding pKi = 7.9 7.9 3 2
Displacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation countingDisplacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation counting
ChEMBL 482 9 2 8 2.9 CCCn1c(=O)c2[nH]c(-c3cc(OCC(=O)Nc4ccc(F)cc4)nn3C)cc2n(CCC)c1=O 10.1021/jm201292w
CHEMBL1955925 71175 None 0 Human Binding pKi = 7.9 7.9 3 2
Displacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation countingDisplacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation counting
ChEMBL 482 9 2 8 2.9 CCCn1c(=O)c2[nH]c(-c3cc(OCC(=O)Nc4ccc(F)cc4)nn3C)cc2n(CCC)c1=O 10.1021/jm201292w
11525368 73388 None 0 Human Binding pKi = 7.9 7.9 8 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 457 7 2 7 3.1 CCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(C#N)cc4)cc3)cc2n(CC)c1=O 10.1021/jm0506221
CHEMBL201496 73388 None 0 Human Binding pKi = 7.9 7.9 8 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 457 7 2 7 3.1 CCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(C#N)cc4)cc3)cc2n(CC)c1=O 10.1021/jm0506221
44450929 95815 None 0 Human Binding pKi = 7.9 7.9 85 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 544 9 2 7 3.9 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCC(O)(c5ccccc5)CC4)cc3)cc2n(CCC)c1=O 10.1016/j.bmc.2008.01.002
CHEMBL258809 95815 None 0 Human Binding pKi = 7.9 7.9 85 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 544 9 2 7 3.9 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCC(O)(c5ccccc5)CC4)cc3)cc2n(CCC)c1=O 10.1016/j.bmc.2008.01.002
44451491 96676 None 0 Human Binding pKi = 7.9 7.9 30 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 475 5 1 9 0.8 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCN(c5ncccn5)CC4)cc3)cc2n(C)c1=O 10.1016/j.bmc.2008.01.002
CHEMBL263895 96676 None 0 Human Binding pKi = 7.9 7.9 30 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 475 5 1 9 0.8 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCN(c5ncccn5)CC4)cc3)cc2n(C)c1=O 10.1016/j.bmc.2008.01.002
69032552 157955 None 0 Human Binding pKi = 7.9 7.9 - 1
Displacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting methodDisplacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting method
ChEMBL 491 9 1 9 3.1 CCCn1c(=O)c2[nH]c(-c3cnn(CC4CCN(c5cccc(OC)c5)C4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2016.11.007
CHEMBL4084707 157955 None 0 Human Binding pKi = 7.9 7.9 - 1
Displacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting methodDisplacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting method
ChEMBL 491 9 1 9 3.1 CCCn1c(=O)c2[nH]c(-c3cnn(CC4CCN(c5cccc(OC)c5)C4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2016.11.007
155562321 175846 None 0 Human Binding pKi = 7.9 7.9 - 1
Displacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assayDisplacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assay
ChEMBL 377 3 1 6 4.0 CCOC(=O)C1=C(C(F)(F)F)Nc2nc3ccccc3n2[C@@H]1c1ccoc1 10.1021/acs.jmedchem.9b01340
CHEMBL4585472 175846 None 0 Human Binding pKi = 7.9 7.9 - 1
Displacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assayDisplacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assay
ChEMBL 377 3 1 6 4.0 CCOC(=O)C1=C(C(F)(F)F)Nc2nc3ccccc3n2[C@@H]1c1ccoc1 10.1021/acs.jmedchem.9b01340
11720513 73027 None 0 Human Binding pKi = 7.9 7.9 4 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 517 10 3 7 4.0 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(NC(C)=O)cc4)cc3)cc2n(CCC)c1=O 10.1021/jm0506221
CHEMBL200967 73027 None 0 Human Binding pKi = 7.9 7.9 4 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 517 10 3 7 4.0 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(NC(C)=O)cc4)cc3)cc2n(CCC)c1=O 10.1021/jm0506221
11561715 73401 None 0 Human Binding pKi = 7.9 7.9 8 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 462 9 2 7 2.7 COCCCn1c(=O)n(C)c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccccc4)cc3)cc21 10.1021/jm0506221
CHEMBL201554 73401 None 0 Human Binding pKi = 7.9 7.9 8 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 462 9 2 7 2.7 COCCCn1c(=O)n(C)c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccccc4)cc3)cc21 10.1021/jm0506221
46228018 199835 None 0 Human Binding pKi = 7.9 7.9 7 3
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 354 5 0 8 1.7 CCn1c(=O)c2c(nc(Cc3ccco3)n2C)n(Cc2ccco2)c1=O 10.1016/j.bmc.2009.07.034
CHEMBL594271 199835 None 0 Human Binding pKi = 7.9 7.9 7 3
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 354 5 0 8 1.7 CCn1c(=O)c2c(nc(Cc3ccco3)n2C)n(Cc2ccco2)c1=O 10.1016/j.bmc.2009.07.034
44574282 178782 None 0 Human Binding pKi = 7.9 7.9 - 1
Displacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells by beta scintillation counterDisplacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells by beta scintillation counter
ChEMBL 432 6 2 6 3.9 CCCn1c(=O)c2[nH]c(-c3ccc(COC(=O)Nc4ccccc4)cc3)cc2n(C)c1=O 10.1016/j.bmc.2009.03.062
CHEMBL468920 178782 None 0 Human Binding pKi = 7.9 7.9 - 1
Displacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells by beta scintillation counterDisplacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells by beta scintillation counter
ChEMBL 432 6 2 6 3.9 CCCn1c(=O)c2[nH]c(-c3ccc(COC(=O)Nc4ccccc4)cc3)cc2n(C)c1=O 10.1016/j.bmc.2009.03.062
CHEMBL5080757 214704 None 0 Human Binding pKi = 7.9 7.9 -2 3
Displacement of [3H]DPCPX from human A2BAR expressed in HEK293 cell membrane incubated for 30 mins by microbeta trilux scintillation counter analysisDisplacement of [3H]DPCPX from human A2BAR expressed in HEK293 cell membrane incubated for 30 mins by microbeta trilux scintillation counter analysis
ChEMBL None None None N#Cc1c(-c2ccc(F)cc2)nc(N)nc1-c1ccco1 10.1021/acs.jmedchem.1c01636
135416055 110482 None 0 Human Binding pKi = 6.9 6.9 5 2
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 517 8 2 8 3.3 CCCn1c(=O)c2nc(-c3cc(NC(=O)Cc4ccc(C(F)(F)F)cc4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
CHEMBL32478 110482 None 0 Human Binding pKi = 6.9 6.9 5 2
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 517 8 2 8 3.3 CCCn1c(=O)c2nc(-c3cc(NC(=O)Cc4ccc(C(F)(F)F)cc4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
57429611 159552 None 0 Human Binding pKi = 6.9 6.9 - 1
Displacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 minsDisplacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 mins
ChEMBL 446 6 2 8 1.9 CCCn1c(=O)c2[nH]c(-c3cnn(CC#Cc4ccc(C(=O)O)cc4)c3)nc2n(CC)c1=O 10.1016/j.ejmech.2017.04.014
CHEMBL4102581 159552 None 0 Human Binding pKi = 6.9 6.9 - 1
Displacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 minsDisplacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 mins
ChEMBL 446 6 2 8 1.9 CCCn1c(=O)c2[nH]c(-c3cnn(CC#Cc4ccc(C(=O)O)cc4)c3)nc2n(CC)c1=O 10.1016/j.ejmech.2017.04.014
11733601 119989 None 0 Human Binding pKi = 6.9 6.9 -5 4
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 105-170Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 105-170
ChEMBL 484 6 2 8 5.2 CCCCn1cc2c(nc(NC(=O)Nc3ccc(C(F)(F)F)cc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm0109614
CHEMBL349954 119989 None 0 Human Binding pKi = 6.9 6.9 -5 4
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 105-170Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 105-170
ChEMBL 484 6 2 8 5.2 CCCCn1cc2c(nc(NC(=O)Nc3ccc(C(F)(F)F)cc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm0109614
22283414 10663 None 0 Human Binding pKi = 6.9 6.9 1 3
Displacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cells after 1 hrDisplacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cells after 1 hr
ChEMBL 359 4 2 5 3.7 COc1ccc(NC(C)=O)c2sc(NC(=O)c3ccc(F)cc3)nc12 10.1016/j.bmcl.2011.02.053
CHEMBL1170518 10663 None 0 Human Binding pKi = 6.9 6.9 1 3
Displacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cells after 1 hrDisplacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cells after 1 hr
ChEMBL 359 4 2 5 3.7 COc1ccc(NC(C)=O)c2sc(NC(=O)c3ccc(F)cc3)nc12 10.1016/j.bmcl.2011.02.053
22283414 10663 None 0 Human Binding pKi = 6.9 6.9 1 3
Displacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cells after 1 hr by scintillation countingDisplacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 359 4 2 5 3.7 COc1ccc(NC(C)=O)c2sc(NC(=O)c3ccc(F)cc3)nc12 10.1016/j.bmcl.2010.05.056
CHEMBL1170518 10663 None 0 Human Binding pKi = 6.9 6.9 1 3
Displacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cells after 1 hr by scintillation countingDisplacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 359 4 2 5 3.7 COc1ccc(NC(C)=O)c2sc(NC(=O)c3ccc(F)cc3)nc12 10.1016/j.bmcl.2010.05.056
9869857 66830 None 11 Human Binding pKi = 5.9 5.9 -109 4
Inhibition of [3H]DPCPX binding to human adenosine A2B receptor expressed in HEK293 cellsInhibition of [3H]DPCPX binding to human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 482 8 5 14 -0.6 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(N[C@H](CO)Cc5ccccc5)nc43)[C@H](O)[C@@H]2O)n1 10.1021/jm031143+
CHEMBL186113 66830 None 11 Human Binding pKi = 5.9 5.9 -109 4
Inhibition of [3H]DPCPX binding to human adenosine A2B receptor expressed in HEK293 cellsInhibition of [3H]DPCPX binding to human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 482 8 5 14 -0.6 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(N[C@H](CO)Cc5ccccc5)nc43)[C@H](O)[C@@H]2O)n1 10.1021/jm031143+
71300326 118501 None 40 Human Binding pKi = 5.9 5.9 2 3
Selectivity interaction (Enzyme panel (ion channels, GPCRs, other targets)) EUB0000196bCl ADORA2BSelectivity interaction (Enzyme panel (ion channels, GPCRs, other targets)) EUB0000196bCl ADORA2B
ChEMBL 499 6 2 4 3.0 O=C([C@@H](Cc1cccc(C(F)(F)F)c1)NS(=O)(=O)c1cc(F)c2c(c1)CCNC2)N1CCCC1 10.6019/CHEMBL5212743
CHEMBL3414622 118501 None 40 Human Binding pKi = 5.9 5.9 2 3
Selectivity interaction (Enzyme panel (ion channels, GPCRs, other targets)) EUB0000196bCl ADORA2BSelectivity interaction (Enzyme panel (ion channels, GPCRs, other targets)) EUB0000196bCl ADORA2B
ChEMBL 499 6 2 4 3.0 O=C([C@@H](Cc1cccc(C(F)(F)F)c1)NS(=O)(=O)c1cc(F)c2c(c1)CCNC2)N1CCCC1 10.6019/CHEMBL5212743
CHEMBL4789678 118501 None 40 Human Binding pKi = 5.9 5.9 2 3
Selectivity interaction (Enzyme panel (ion channels, GPCRs, other targets)) EUB0000196bCl ADORA2BSelectivity interaction (Enzyme panel (ion channels, GPCRs, other targets)) EUB0000196bCl ADORA2B
ChEMBL 499 6 2 4 3.0 O=C([C@@H](Cc1cccc(C(F)(F)F)c1)NS(=O)(=O)c1cc(F)c2c(c1)CCNC2)N1CCCC1 10.6019/CHEMBL5212743
44520983 201238 None 0 Human Binding pKi = 5.9 5.9 -380 4
Displacement of radioligand from human adenosine A2B receptor expressed in cells by topcount microplate scintillation countingDisplacement of radioligand from human adenosine A2B receptor expressed in cells by topcount microplate scintillation counting
ChEMBL 326 5 2 7 1.8 CCn1ccnc1CNC(=O)c1cc(-c2ccc(C)o2)nc(N)n1 10.1016/j.bmc.2009.07.078
CHEMBL603748 201238 None 0 Human Binding pKi = 5.9 5.9 -380 4
Displacement of radioligand from human adenosine A2B receptor expressed in cells by topcount microplate scintillation countingDisplacement of radioligand from human adenosine A2B receptor expressed in cells by topcount microplate scintillation counting
ChEMBL 326 5 2 7 1.8 CCn1ccnc1CNC(=O)c1cc(-c2ccc(C)o2)nc(N)n1 10.1016/j.bmc.2009.07.078
127043669 141178 None 0 Human Binding pKi = 6.9 6.9 1 4
Displacement of [3H]PSB-603 from recombinant human adenosine receptor A2b expressed in CHO cell membranesDisplacement of [3H]PSB-603 from recombinant human adenosine receptor A2b expressed in CHO cell membranes
ChEMBL 439 9 1 8 3.1 CCCCn1c(=O)c2c(nc3n2CCCN3CCc2ccc(O)cc2)n(CCCC)c1=O 10.1016/j.bmc.2016.07.028
CHEMBL3828002 141178 None 0 Human Binding pKi = 6.9 6.9 1 4
Displacement of [3H]PSB-603 from recombinant human adenosine receptor A2b expressed in CHO cell membranesDisplacement of [3H]PSB-603 from recombinant human adenosine receptor A2b expressed in CHO cell membranes
ChEMBL 439 9 1 8 3.1 CCCCn1c(=O)c2c(nc3n2CCCN3CCc2ccc(O)cc2)n(CCCC)c1=O 10.1016/j.bmc.2016.07.028
44406403 72987 None 0 Human Binding pKi = 6.9 6.9 26 2
Displacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cellsDisplacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cells
ChEMBL 489 9 1 10 3.3 CCCn1c(=O)c2nc(-c3cnn(Cc4cc(-c5cccc(OC)c5)on4)c3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2005.10.002
CHEMBL200747 72987 None 0 Human Binding pKi = 6.9 6.9 26 2
Displacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cellsDisplacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cells
ChEMBL 489 9 1 10 3.3 CCCn1c(=O)c2nc(-c3cnn(Cc4cc(-c5cccc(OC)c5)on4)c3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2005.10.002
11577210 74594 None 0 Human Binding pKi = 6.9 6.9 - 1
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 518 10 2 8 3.2 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(CC(=O)OCC)cc4)cc3)cc2n(C)c1=O 10.1021/jm0506221
CHEMBL202980 74594 None 0 Human Binding pKi = 6.9 6.9 - 1
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 518 10 2 8 3.2 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(CC(=O)OCC)cc4)cc3)cc2n(C)c1=O 10.1021/jm0506221
168292492 191640 None 0 Human Binding pKi = 6.9 6.9 - 1
Displacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cell membrane and measured after 0.5 hrs by radioligand displacement assayDisplacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cell membrane and measured after 0.5 hrs by radioligand displacement assay
ChEMBL 352 4 2 6 1.1 CCCn1c(=O)[nH]c2nc(-c3cccc(S(=O)(=O)F)c3)[nH]c2c1=O 10.1039/d2md00132b
CHEMBL5195884 191640 None 0 Human Binding pKi = 6.9 6.9 - 1
Displacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cell membrane and measured after 0.5 hrs by radioligand displacement assayDisplacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cell membrane and measured after 0.5 hrs by radioligand displacement assay
ChEMBL 352 4 2 6 1.1 CCCn1c(=O)[nH]c2nc(-c3cccc(S(=O)(=O)F)c3)[nH]c2c1=O 10.1039/d2md00132b
135465796 110570 None 0 Human Binding pKi = 6.9 6.9 18 2
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 571 9 2 9 3.4 CC(C)Cn1c(=O)c2nc(-c3cc(OCC(=O)Nc4ccc(Br)cc4)nn3C)[nH]c2n(CC(C)C)c1=O 10.1021/jm0309654
CHEMBL32534 110570 None 0 Human Binding pKi = 6.9 6.9 18 2
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 571 9 2 9 3.4 CC(C)Cn1c(=O)c2nc(-c3cc(OCC(=O)Nc4ccc(Br)cc4)nn3C)[nH]c2n(CC(C)C)c1=O 10.1021/jm0309654
10938276 119877 None 0 Human Binding pKi = 6.9 6.9 -29 4
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 118-146Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 118-146
ChEMBL 402 4 2 8 3.7 CCn1cc2c(nc(NC(=O)Nc3ccc(C)cc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm0109614
CHEMBL348975 119877 None 0 Human Binding pKi = 6.9 6.9 -29 4
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 118-146Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 118-146
ChEMBL 402 4 2 8 3.7 CCn1cc2c(nc(NC(=O)Nc3ccc(C)cc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm0109614
21874626 190676 None 0 Human Binding pKi = 6.9 6.9 -12 4
Displacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation countingDisplacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation counting
ChEMBL 335 4 2 8 1.2 NC(=O)c1cccc(Cn2nnc3c(-c4ccco4)nc(N)nc32)c1 10.1021/jm800961g
CHEMBL518178 190676 None 0 Human Binding pKi = 6.9 6.9 -12 4
Displacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation countingDisplacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation counting
ChEMBL 335 4 2 8 1.2 NC(=O)c1cccc(Cn2nnc3c(-c4ccco4)nc(N)nc32)c1 10.1021/jm800961g
22995178 100010 None 4 Human Binding pKi = 5.9 5.9 3 3
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 232 4 1 5 0.3 C=CCn1c(=O)c2nc[nH]c2n(CC=C)c1=O 10.1021/jm0104318
CHEMBL286785 100010 None 4 Human Binding pKi = 5.9 5.9 3 3
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 232 4 1 5 0.3 C=CCn1c(=O)c2nc[nH]c2n(CC=C)c1=O 10.1021/jm0104318
1908 206001 None 33 Human Binding pKi = 5.9 5.9 1 6
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 336 2 2 7 -0.1 Cn1c(=O)c2nc(-c3ccc(S(=O)(=O)O)cc3)[nH]c2n(C)c1=O 10.1021/jm0104318
CHEMBL8488 206001 None 33 Human Binding pKi = 5.9 5.9 1 6
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 336 2 2 7 -0.1 Cn1c(=O)c2nc(-c3ccc(S(=O)(=O)O)cc3)[nH]c2n(C)c1=O 10.1021/jm0104318
1908 206001 None 33 Human Binding pKi = 5.9 5.9 1 6
Binding affinity for human HEK293 adenosine A2B receptor using [125I]ABOPX in CHO cell membranesBinding affinity for human HEK293 adenosine A2B receptor using [125I]ABOPX in CHO cell membranes
ChEMBL 336 2 2 7 -0.1 Cn1c(=O)c2nc(-c3ccc(S(=O)(=O)O)cc3)[nH]c2n(C)c1=O 10.1021/jm0310030
CHEMBL8488 206001 None 33 Human Binding pKi = 5.9 5.9 1 6
Binding affinity for human HEK293 adenosine A2B receptor using [125I]ABOPX in CHO cell membranesBinding affinity for human HEK293 adenosine A2B receptor using [125I]ABOPX in CHO cell membranes
ChEMBL 336 2 2 7 -0.1 Cn1c(=O)c2nc(-c3ccc(S(=O)(=O)O)cc3)[nH]c2n(C)c1=O 10.1021/jm0310030
1908 206001 None 33 Human Binding pKi = 5.9 5.9 1 6
Displacement of [125I]ABOPX from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [125I]ABOPX from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 336 2 2 7 -0.1 Cn1c(=O)c2nc(-c3ccc(S(=O)(=O)O)cc3)[nH]c2n(C)c1=O 10.1021/jm060277v
CHEMBL8488 206001 None 33 Human Binding pKi = 5.9 5.9 1 6
Displacement of [125I]ABOPX from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [125I]ABOPX from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 336 2 2 7 -0.1 Cn1c(=O)c2nc(-c3ccc(S(=O)(=O)O)cc3)[nH]c2n(C)c1=O 10.1021/jm060277v
46880471 6077 None 0 Human Binding pKi = 6.9 6.9 10 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 306 4 1 5 3.1 O=C(Nc1ccc(-c2ccncc2)c(-c2cocn2)n1)C1CC1 10.1016/j.bmcl.2010.01.045
CHEMBL1080677 6077 None 0 Human Binding pKi = 6.9 6.9 10 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 306 4 1 5 3.1 O=C(Nc1ccc(-c2ccncc2)c(-c2cocn2)n1)C1CC1 10.1016/j.bmcl.2010.01.045
44406625 72820 None 0 Human Binding pKi = 6.9 6.9 22 3
Displacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cellsDisplacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cells
ChEMBL 494 8 1 10 3.3 CCCn1c(=O)c2nc(-c3cnn(Cc4noc(-c5cccc(Cl)c5)n4)c3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2005.10.002
CHEMBL200146 72820 None 0 Human Binding pKi = 6.9 6.9 22 3
Displacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cellsDisplacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cells
ChEMBL 494 8 1 10 3.3 CCCn1c(=O)c2nc(-c3cnn(Cc4noc(-c5cccc(Cl)c5)n4)c3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2005.10.002
21874538 169442 None 0 Human Binding pKi = 6.9 6.9 -11 4
Displacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation countingDisplacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation counting
ChEMBL 333 3 2 9 1.4 Nc1nc(-c2ccco2)c2nnn(Cc3ccc4[nH]nnc4c3)c2n1 10.1021/jm800961g
CHEMBL442670 169442 None 0 Human Binding pKi = 6.9 6.9 -11 4
Displacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation countingDisplacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation counting
ChEMBL 333 3 2 9 1.4 Nc1nc(-c2ccco2)c2nnn(Cc3ccc4[nH]nnc4c3)c2n1 10.1021/jm800961g
46233379 200339 None 0 Human Binding pKi = 6.9 6.9 -1 3
Displacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells by microplate beta scintillation counterDisplacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells by microplate beta scintillation counter
ChEMBL 416 5 0 7 2.9 CCn1c(=O)c2c(nc(Cc3c(F)cccc3F)n2C)n(Cc2cccs2)c1=O 10.1016/j.bmc.2010.01.028
CHEMBL597560 200339 None 0 Human Binding pKi = 6.9 6.9 -1 3
Displacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells by microplate beta scintillation counterDisplacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells by microplate beta scintillation counter
ChEMBL 416 5 0 7 2.9 CCn1c(=O)c2c(nc(Cc3c(F)cccc3F)n2C)n(Cc2cccs2)c1=O 10.1016/j.bmc.2010.01.028
44437219 90651 None 0 Human Binding pKi = 4.9 4.9 -1 2
Displacement of [3H]ZM-241385 from human adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]ZM-241385 from human adenosine A2B receptor expressed in CHO cells
ChEMBL 340 3 0 8 0.3 Cn1c(=O)c2c(nc3n2CCCN3CCc2ccccn2)n(C)c1=O 10.1016/j.bmc.2007.07.051
CHEMBL239018 90651 None 0 Human Binding pKi = 4.9 4.9 -1 2
Displacement of [3H]ZM-241385 from human adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]ZM-241385 from human adenosine A2B receptor expressed in CHO cells
ChEMBL 340 3 0 8 0.3 Cn1c(=O)c2c(nc3n2CCCN3CCc2ccccn2)n(C)c1=O 10.1016/j.bmc.2007.07.051
24894016 64481 None 0 Human Binding pKi = 5.9 5.9 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by liquid scintillation countingDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by liquid scintillation counting
ChEMBL 297 2 3 5 2.5 O=C(Nc1ccc(O)c(O)c1)c1coc2ccccc2c1=O 10.1016/j.ejmech.2012.05.033
CHEMBL1814066 64481 None 0 Human Binding pKi = 5.9 5.9 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by liquid scintillation countingDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by liquid scintillation counting
ChEMBL 297 2 3 5 2.5 O=C(Nc1ccc(O)c(O)c1)c1coc2ccccc2c1=O 10.1016/j.ejmech.2012.05.033
11133843 57457 None 0 Human Binding pKi = 6.9 6.9 -5 4
Displacement of [3H]-DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 107-172Displacement of [3H]-DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 107-172
ChEMBL 434 6 2 8 4.3 CCCCn1cc2c(nc(NC(=O)Nc3ccc(F)cc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm0109614
CHEMBL165620 57457 None 0 Human Binding pKi = 6.9 6.9 -5 4
Displacement of [3H]-DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 107-172Displacement of [3H]-DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 107-172
ChEMBL 434 6 2 8 4.3 CCCCn1cc2c(nc(NC(=O)Nc3ccc(F)cc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm0109614
10994317 57094 None 0 Human Binding pKi = 6.9 6.9 -8 4
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 115-161Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 115-161
ChEMBL 470 5 2 8 4.8 CCCn1cc2c(nc(NC(=O)Nc3ccc(C(F)(F)F)cc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm0109614
CHEMBL164509 57094 None 0 Human Binding pKi = 6.9 6.9 -8 4
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 115-161Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 115-161
ChEMBL 470 5 2 8 4.8 CCCn1cc2c(nc(NC(=O)Nc3ccc(C(F)(F)F)cc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm0109614
44406588 133535 None 0 Human Binding pKi = 6.9 6.9 6 3
Displacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cellsDisplacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cells
ChEMBL 490 9 1 11 2.7 CCCn1c(=O)c2nc(-c3cnn(Cc4noc(-c5cccc(OC)c5)n4)c3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2005.10.002
CHEMBL370860 133535 None 0 Human Binding pKi = 6.9 6.9 6 3
Displacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cellsDisplacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cells
ChEMBL 490 9 1 11 2.7 CCCn1c(=O)c2nc(-c3cnn(Cc4noc(-c5cccc(OC)c5)n4)c3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2005.10.002
45267990 196104 None 0 Human Binding pKi = 6.9 6.9 -53 4
Binding affinity to adenosine A2B receptorBinding affinity to adenosine A2B receptor
ChEMBL 328 4 2 5 2.9 Nc1nc(C(=O)NCc2ccccc2Cl)cc(-c2ccco2)n1 10.1016/j.bmcl.2009.03.142
CHEMBL560904 196104 None 0 Human Binding pKi = 6.9 6.9 -53 4
Binding affinity to adenosine A2B receptorBinding affinity to adenosine A2B receptor
ChEMBL 328 4 2 5 2.9 Nc1nc(C(=O)NCc2ccccc2Cl)cc(-c2ccco2)n1 10.1016/j.bmcl.2009.03.142
136044107 131224 None 0 Human Binding pKi = 6.9 6.9 -2 3
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 344 5 3 7 1.8 CCCn1c(=O)c2nc(-c3cc(O)ccc3O)[nH]c2n(CCC)c1=O 10.1021/jm0104318
CHEMBL36867 131224 None 0 Human Binding pKi = 6.9 6.9 -2 3
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 344 5 3 7 1.8 CCCn1c(=O)c2nc(-c3cc(O)ccc3O)[nH]c2n(CCC)c1=O 10.1021/jm0104318
162666539 182290 None 0 Human Binding pKi = 6.9 6.9 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 276 4 2 4 1.9 CC1=C(C(=O)OCC2CC2)C(c2ccco2)NC(=O)N1 10.1021/acs.jmedchem.0c01431
CHEMBL4783992 182290 None 0 Human Binding pKi = 6.9 6.9 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 276 4 2 4 1.9 CC1=C(C(=O)OCC2CC2)C(c2ccco2)NC(=O)N1 10.1021/acs.jmedchem.0c01431
45272308 195347 None 0 Human Binding pKi = 6.9 6.9 3 2
Binding affinity to human adenosine A2b receptor expressed in HEK293 cellsBinding affinity to human adenosine A2b receptor expressed in HEK293 cells
ChEMBL 318 6 1 7 1.2 CCn1c(=O)c2[nH]c(-c3ccco3)nc2n(CCCOC)c1=O 10.1016/j.bmc.2009.03.029
CHEMBL551761 195347 None 0 Human Binding pKi = 6.9 6.9 3 2
Binding affinity to human adenosine A2b receptor expressed in HEK293 cellsBinding affinity to human adenosine A2b receptor expressed in HEK293 cells
ChEMBL 318 6 1 7 1.2 CCn1c(=O)c2[nH]c(-c3ccco3)nc2n(CCCOC)c1=O 10.1016/j.bmc.2009.03.029
46233315 200386 None 0 Human Binding pKi = 6.9 6.9 4 4
Displacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells by microplate beta scintillation counterDisplacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells by microplate beta scintillation counter
ChEMBL 372 5 1 7 2.7 CCn1c(=O)c2[nH]c(Cc3cccs3)nc2n(Cc2cccs2)c1=O 10.1016/j.bmc.2010.01.028
CHEMBL597955 200386 None 0 Human Binding pKi = 6.9 6.9 4 4
Displacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells by microplate beta scintillation counterDisplacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells by microplate beta scintillation counter
ChEMBL 372 5 1 7 2.7 CCn1c(=O)c2[nH]c(Cc3cccs3)nc2n(Cc2cccs2)c1=O 10.1016/j.bmc.2010.01.028
164622009 186089 None 0 Human Binding pKi = 5.9 5.9 -309 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK cell membrane incubated for 30 mins by microplate beta scintillation counting based radioligand inhibition assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK cell membrane incubated for 30 mins by microplate beta scintillation counting based radioligand inhibition assay
ChEMBL 426 8 4 9 0.6 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NCCCCc4ccccc4)ncnc32)[C@H](O)[C@@H]1O 10.1016/j.ejmech.2021.113607
CHEMBL4871554 186089 None 0 Human Binding pKi = 5.9 5.9 -309 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK cell membrane incubated for 30 mins by microplate beta scintillation counting based radioligand inhibition assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK cell membrane incubated for 30 mins by microplate beta scintillation counting based radioligand inhibition assay
ChEMBL 426 8 4 9 0.6 CNC(=O)[C@H]1O[C@@H](n2cnc3c(NCCCCc4ccccc4)ncnc32)[C@H](O)[C@@H]1O 10.1016/j.ejmech.2021.113607
1882 90652 None 66 Human Binding pKi = 5.9 5.9 3 5
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 242 2 0 6 -0.3 Cn1c(=O)c2c(ncn2CCCl)n(C)c1=O 10.1021/jm0104318
CHEMBL23903 90652 None 66 Human Binding pKi = 5.9 5.9 3 5
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 242 2 0 6 -0.3 Cn1c(=O)c2c(ncn2CCCl)n(C)c1=O 10.1021/jm0104318
439176 98621 None 71 Human Binding pKi = 4.9 4.9 -54 4
Displacement of [3H]PSB-298 from human adenosine A2B receptor expressed in HEK293 cells at 10 uM; Less than 10% inhibitionDisplacement of [3H]PSB-298 from human adenosine A2B receptor expressed in HEK293 cells at 10 uM; Less than 10% inhibition
ChEMBL 297 3 3 9 -0.6 CSC[C@H]1O[C@@H](n2cnc3c(N)ncnc32)[C@H](O)[C@@H]1O 10.1021/jm031092g
CHEMBL277041 98621 None 71 Human Binding pKi = 4.9 4.9 -54 4
Displacement of [3H]PSB-298 from human adenosine A2B receptor expressed in HEK293 cells at 10 uM; Less than 10% inhibitionDisplacement of [3H]PSB-298 from human adenosine A2B receptor expressed in HEK293 cells at 10 uM; Less than 10% inhibition
ChEMBL 297 3 3 9 -0.6 CSC[C@H]1O[C@@H](n2cnc3c(N)ncnc32)[C@H](O)[C@@H]1O 10.1021/jm031092g
44236632 158668 None 0 Human Binding pKi = 7.9 7.9 - 1
Displacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 minsDisplacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 mins
ChEMBL 441 6 1 8 2.5 CCCn1c(=O)c2[nH]c(-c3cnn(CC#Cc4ccc(C#N)cc4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2017.04.014
CHEMBL4092863 158668 None 0 Human Binding pKi = 7.9 7.9 - 1
Displacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 minsDisplacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 mins
ChEMBL 441 6 1 8 2.5 CCCn1c(=O)c2[nH]c(-c3cnn(CC#Cc4ccc(C#N)cc4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2017.04.014
69031810 158856 None 0 Human Binding pKi = 7.9 7.9 - 1
Displacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting methodDisplacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting method
ChEMBL 545 9 1 9 4.0 CCCn1c(=O)c2[nH]c(-c3cnn(CC4CCN(c5ccc(OC(F)(F)F)cc5)C4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2016.11.007
CHEMBL4094895 158856 None 0 Human Binding pKi = 7.9 7.9 - 1
Displacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting methodDisplacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting method
ChEMBL 545 9 1 9 4.0 CCCn1c(=O)c2[nH]c(-c3cnn(CC4CCN(c5ccc(OC(F)(F)F)cc5)C4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2016.11.007
11654460 94559 None 0 Human Binding pKi = 7.9 7.9 3 4
Displacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranesDisplacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranes
ChEMBL 410 7 1 7 2.8 CCCn1c(=O)c2[nH]c(-c3cnn(Cc4cccc(F)c4)c3)nc2n(CCC)c1=O 10.1016/j.bmcl.2008.01.008
CHEMBL251869 94559 None 0 Human Binding pKi = 7.9 7.9 3 4
Displacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranesDisplacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranes
ChEMBL 410 7 1 7 2.8 CCCn1c(=O)c2[nH]c(-c3cnn(Cc4cccc(F)c4)c3)nc2n(CCC)c1=O 10.1016/j.bmcl.2008.01.008
9890439 94560 None 0 Human Binding pKi = 7.9 7.9 10 4
Displacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranesDisplacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranes
ChEMBL 460 7 1 7 3.6 CCCn1c(=O)c2[nH]c(-c3cnn(Cc4cccc(C(F)(F)F)c4)c3)nc2n(CCC)c1=O 10.1016/j.bmcl.2008.01.008
CHEMBL251870 94560 None 0 Human Binding pKi = 7.9 7.9 10 4
Displacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranesDisplacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranes
ChEMBL 460 7 1 7 3.6 CCCn1c(=O)c2[nH]c(-c3cnn(Cc4cccc(C(F)(F)F)c4)c3)nc2n(CCC)c1=O 10.1016/j.bmcl.2008.01.008
22266775 94620 None 0 Human Binding pKi = 7.9 7.9 29 4
Displacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranesDisplacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranes
ChEMBL 459 8 1 9 3.3 CCCn1c(=O)c2[nH]c(-c3cnn(Cc4cc(-c5ccccc5)on4)c3)nc2n(CCC)c1=O 10.1016/j.bmcl.2008.01.008
CHEMBL252245 94620 None 0 Human Binding pKi = 7.9 7.9 29 4
Displacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranesDisplacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranes
ChEMBL 459 8 1 9 3.3 CCCn1c(=O)c2[nH]c(-c3cnn(Cc4cc(-c5ccccc5)on4)c3)nc2n(CCC)c1=O 10.1016/j.bmcl.2008.01.008
22266741 155080 None 0 Human Binding pKi = 7.9 7.9 - 1
Displacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranesDisplacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranes
ChEMBL 500 6 2 9 3.1 CC(C)Cn1c(=O)[nH]c2nc(-c3cnn(Cc4noc(-c5ccc(C(F)(F)F)cc5)n4)c3)[nH]c2c1=O 10.1016/j.bmcl.2008.01.008
CHEMBL401834 155080 None 0 Human Binding pKi = 7.9 7.9 - 1
Displacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranesDisplacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranes
ChEMBL 500 6 2 9 3.1 CC(C)Cn1c(=O)[nH]c2nc(-c3cnn(Cc4noc(-c5ccc(C(F)(F)F)cc5)n4)c3)[nH]c2c1=O 10.1016/j.bmcl.2008.01.008
46880510 6157 None 0 Human Binding pKi = 7.9 7.9 11 3
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 316 4 1 4 3.6 O=C(Nc1ccc(-c2ccncc2)c(-c2ccncc2)n1)C1CC1 10.1016/j.bmcl.2010.01.045
CHEMBL1081041 6157 None 0 Human Binding pKi = 7.9 7.9 11 3
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 316 4 1 4 3.6 O=C(Nc1ccc(-c2ccncc2)c(-c2ccncc2)n1)C1CC1 10.1016/j.bmcl.2010.01.045
135874416 96388 None 0 Human Binding pKi = 7.9 7.9 35 2
Displacement of [3H]MRE2029F20 from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]MRE2029F20 from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 467 8 2 8 2.7 CCCn1c(=O)c2[nH]c(-c3cc(C)n(CC(=O)Nc4ccc(F)cc4)n3)nc2n(CCC)c1=O 10.1016/j.bmc.2007.11.058
CHEMBL261809 96388 None 0 Human Binding pKi = 7.9 7.9 35 2
Displacement of [3H]MRE2029F20 from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]MRE2029F20 from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 467 8 2 8 2.7 CCCn1c(=O)c2[nH]c(-c3cc(C)n(CC(=O)Nc4ccc(F)cc4)n3)nc2n(CCC)c1=O 10.1016/j.bmc.2007.11.058
44406611 72753 None 0 Human Binding pKi = 7.9 7.9 40 3
Displacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cellsDisplacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cells
ChEMBL 485 8 1 11 2.5 CCCn1c(=O)c2nc(-c3cnn(Cc4noc(-c5ccc(C#N)cc5)n4)c3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2005.10.002
CHEMBL199895 72753 None 0 Human Binding pKi = 7.9 7.9 40 3
Displacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cellsDisplacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cells
ChEMBL 485 8 1 11 2.5 CCCn1c(=O)c2nc(-c3cnn(Cc4noc(-c5ccc(C#N)cc5)n4)c3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2005.10.002
22266775 94620 None 0 Human Binding pKi = 7.9 7.9 29 4
Displacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cellsDisplacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cells
ChEMBL 459 8 1 9 3.3 CCCn1c(=O)c2[nH]c(-c3cnn(Cc4cc(-c5ccccc5)on4)c3)nc2n(CCC)c1=O 10.1016/j.bmcl.2005.10.002
CHEMBL252245 94620 None 0 Human Binding pKi = 7.9 7.9 29 4
Displacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cellsDisplacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cells
ChEMBL 459 8 1 9 3.3 CCCn1c(=O)c2[nH]c(-c3cnn(Cc4cc(-c5ccccc5)on4)c3)nc2n(CCC)c1=O 10.1016/j.bmcl.2005.10.002
11654460 94559 None 0 Human Binding pKi = 7.9 7.9 3 4
Displacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 410 7 1 7 2.8 CCCn1c(=O)c2[nH]c(-c3cnn(Cc4cccc(F)c4)c3)nc2n(CCC)c1=O 10.1021/jm7014815
CHEMBL251869 94559 None 0 Human Binding pKi = 7.9 7.9 3 4
Displacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 410 7 1 7 2.8 CCCn1c(=O)c2[nH]c(-c3cnn(Cc4cccc(F)c4)c3)nc2n(CCC)c1=O 10.1021/jm7014815
9890439 94560 None 0 Human Binding pKi = 7.9 7.9 10 4
Displacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 460 7 1 7 3.6 CCCn1c(=O)c2[nH]c(-c3cnn(Cc4cccc(C(F)(F)F)c4)c3)nc2n(CCC)c1=O 10.1021/jm7014815
CHEMBL251870 94560 None 0 Human Binding pKi = 7.9 7.9 10 4
Displacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 460 7 1 7 3.6 CCCn1c(=O)c2[nH]c(-c3cnn(Cc4cccc(C(F)(F)F)c4)c3)nc2n(CCC)c1=O 10.1021/jm7014815
11568203 96244 None 0 Human Binding pKi = 7.9 7.9 28 4
Displacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 432 5 1 7 2.8 CCCn1c(=O)c2[nH]c(-c3cnn(Cc4cccc(C(F)(F)F)c4)c3)nc2n(C)c1=O 10.1021/jm7014815
CHEMBL260975 96244 None 0 Human Binding pKi = 7.9 7.9 28 4
Displacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 432 5 1 7 2.8 CCCn1c(=O)c2[nH]c(-c3cnn(Cc4cccc(C(F)(F)F)c4)c3)nc2n(C)c1=O 10.1021/jm7014815
49797772 10856 None 0 Human Binding pKi = 7.9 7.9 1 3
Displacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cells after 1 hr by scintillation countingDisplacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 466 7 1 6 4.1 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(CN4CCCC4=O)cc3)sc12 10.1016/j.bmcl.2010.05.056
CHEMBL1172276 10856 None 0 Human Binding pKi = 7.9 7.9 1 3
Displacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cells after 1 hr by scintillation countingDisplacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 466 7 1 6 4.1 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(CN4CCCC4=O)cc3)sc12 10.1016/j.bmcl.2010.05.056
11654460 94559 None 0 Human Binding pKi = 7.9 7.9 3 4
Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cellsDisplacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells
ChEMBL 410 7 1 7 2.8 CCCn1c(=O)c2[nH]c(-c3cnn(Cc4cccc(F)c4)c3)nc2n(CCC)c1=O 10.1021/jm051268+
CHEMBL251869 94559 None 0 Human Binding pKi = 7.9 7.9 3 4
Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cellsDisplacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells
ChEMBL 410 7 1 7 2.8 CCCn1c(=O)c2[nH]c(-c3cnn(Cc4cccc(F)c4)c3)nc2n(CCC)c1=O 10.1021/jm051268+
9890439 94560 None 0 Human Binding pKi = 7.9 7.9 10 4
Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cellsDisplacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells
ChEMBL 460 7 1 7 3.6 CCCn1c(=O)c2[nH]c(-c3cnn(Cc4cccc(C(F)(F)F)c4)c3)nc2n(CCC)c1=O 10.1021/jm051268+
CHEMBL251870 94560 None 0 Human Binding pKi = 7.9 7.9 10 4
Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cellsDisplacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells
ChEMBL 460 7 1 7 3.6 CCCn1c(=O)c2[nH]c(-c3cnn(Cc4cccc(C(F)(F)F)c4)c3)nc2n(CCC)c1=O 10.1021/jm051268+
136042331 71157 None 0 Human Binding pKi = 7.9 7.9 48 2
Displacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation countingDisplacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation counting
ChEMBL 476 8 2 9 2.9 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5c(C)cccc5[nH]4)nn3C)nc2n(CCC)c1=O 10.1021/jm201292w
CHEMBL1955906 71157 None 0 Human Binding pKi = 7.9 7.9 48 2
Displacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation countingDisplacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation counting
ChEMBL 476 8 2 9 2.9 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5c(C)cccc5[nH]4)nn3C)nc2n(CCC)c1=O 10.1021/jm201292w
11670078 72780 None 0 Human Binding pKi = 7.9 7.9 - 1
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 474 9 2 6 4.3 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(C)cc4)cc3)cc2n(CCC)c1=O 10.1021/jm0506221
CHEMBL199999 72780 None 0 Human Binding pKi = 7.9 7.9 - 1
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 474 9 2 6 4.3 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(C)cc4)cc3)cc2n(CCC)c1=O 10.1021/jm0506221
CHEMBL5086487 215034 None 0 Human Binding pKi = 7.9 7.9 -5 3
Displacement of [3H]DPCPX from human A2BAR expressed in HEK293 cell membrane incubated for 30 mins by microbeta trilux scintillation counter analysisDisplacement of [3H]DPCPX from human A2BAR expressed in HEK293 cell membrane incubated for 30 mins by microbeta trilux scintillation counter analysis
ChEMBL None None None CCNc1nc(-c2ccccc2)c(C#N)c(-c2cccc(C#N)c2)n1 10.1021/acs.jmedchem.1c01636
136042351 71151 None 0 Human Binding pKi = 7.9 7.9 53 2
Displacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation countingDisplacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation counting
ChEMBL 492 9 2 10 2.6 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5cc(OC)ccc5[nH]4)nn3C)nc2n(CCC)c1=O 10.1021/jm201292w
CHEMBL1955900 71151 None 0 Human Binding pKi = 7.9 7.9 53 2
Displacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation countingDisplacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation counting
ChEMBL 492 9 2 10 2.6 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5cc(OC)ccc5[nH]4)nn3C)nc2n(CCC)c1=O 10.1021/jm201292w
44450828 157695 None 0 Human Binding pKi = 7.8 7.8 44 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 472 6 1 6 3.1 CCCn1c(=O)n(C)c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCc5ccccc5C4)cc3)cc21 10.1016/j.bmc.2008.01.002
CHEMBL408185 157695 None 0 Human Binding pKi = 7.8 7.8 44 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 472 6 1 6 3.1 CCCn1c(=O)n(C)c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCc5ccccc5C4)cc3)cc21 10.1016/j.bmc.2008.01.002
11089092 139786 None 0 Human Binding pKi = 7.8 7.8 4 3
Inhibition of [3H]ZM-241385 binding to human adenosine A2B receptorInhibition of [3H]ZM-241385 binding to human adenosine A2B receptor
ChEMBL 340 5 3 5 1.6 CCCn1c(=O)[nH]c2[nH]c(-c3ccc(/C=C/C(=O)O)cc3)nc2c1=O 10.1021/jm011049y
CHEMBL37987 139786 None 0 Human Binding pKi = 7.8 7.8 4 3
Inhibition of [3H]ZM-241385 binding to human adenosine A2B receptorInhibition of [3H]ZM-241385 binding to human adenosine A2B receptor
ChEMBL 340 5 3 5 1.6 CCCn1c(=O)[nH]c2[nH]c(-c3ccc(/C=C/C(=O)O)cc3)nc2c1=O 10.1021/jm011049y
CHEMBL5071174 214252 None 0 Human Binding pKi = 7.8 7.8 -6 3
Displacement of [3H]DPCPX from human A2BAR expressed in HEK293 cell membrane incubated for 30 mins by microbeta trilux scintillation counter analysisDisplacement of [3H]DPCPX from human A2BAR expressed in HEK293 cell membrane incubated for 30 mins by microbeta trilux scintillation counter analysis
ChEMBL None None None N#Cc1c(-c2ccccc2)nc(Nc2ccccc2)nc1-c1ccco1 10.1021/acs.jmedchem.1c01636
11038429 119495 None 0 Human Binding pKi = 7.8 7.8 1 2
Inhibition of [3H]ZM-241385 binding to human adenosine A2B receptorInhibition of [3H]ZM-241385 binding to human adenosine A2B receptor
ChEMBL 502 8 2 7 2.6 CCCCn1c(=O)[nH]c2[nH]c(-c3ccc(OCC(=O)N4CCN(c5ccccc5)CC4)cc3)nc2c1=O 10.1021/jm011049y
CHEMBL34543 119495 None 0 Human Binding pKi = 7.8 7.8 1 2
Inhibition of [3H]ZM-241385 binding to human adenosine A2B receptorInhibition of [3H]ZM-241385 binding to human adenosine A2B receptor
ChEMBL 502 8 2 7 2.6 CCCCn1c(=O)[nH]c2[nH]c(-c3ccc(OCC(=O)N4CCN(c5ccccc5)CC4)cc3)nc2c1=O 10.1021/jm011049y
44451049 160182 None 0 Human Binding pKi = 7.8 7.8 74 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 535 7 1 7 3.5 CCCn1c(=O)n(C)c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCN(c5ccccc5Cl)CC4)cc3)cc21 10.1016/j.bmc.2008.01.002
CHEMBL410934 160182 None 0 Human Binding pKi = 7.8 7.8 74 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 535 7 1 7 3.5 CCCn1c(=O)n(C)c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCN(c5ccccc5Cl)CC4)cc3)cc21 10.1016/j.bmc.2008.01.002
46228058 200058 None 0 Human Binding pKi = 7.8 7.8 12 3
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 384 6 0 8 2.6 CCCn1c(=O)c2c(nc(Cc3cccs3)n2C)n(Cc2ccco2)c1=O 10.1016/j.bmc.2009.07.034
CHEMBL595658 200058 None 0 Human Binding pKi = 7.8 7.8 12 3
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 384 6 0 8 2.6 CCCn1c(=O)c2c(nc(Cc3cccs3)n2C)n(Cc2ccco2)c1=O 10.1016/j.bmc.2009.07.034
136042328 71147 None 0 Human Binding pKi = 7.8 7.8 10 2
Displacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation countingDisplacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation counting
ChEMBL 507 9 2 11 2.5 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5cc([N+](=O)[O-])ccc5[nH]4)nn3C)nc2n(CCC)c1=O 10.1021/jm201292w
CHEMBL1955894 71147 None 0 Human Binding pKi = 7.8 7.8 10 2
Displacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation countingDisplacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation counting
ChEMBL 507 9 2 11 2.5 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5cc([N+](=O)[O-])ccc5[nH]4)nn3C)nc2n(CCC)c1=O 10.1021/jm201292w
11586663 72069 None 0 Human Binding pKi = 6.9 6.9 -1 3
Binding affinity towards human Adenosine A2b receptor expressed in HEK293 cells using 5 nM [3H]DPCPXBinding affinity towards human Adenosine A2b receptor expressed in HEK293 cells using 5 nM [3H]DPCPX
ChEMBL 229 1 1 7 0.4 Cc1cc2c(nc(-n3nccn3)n2C)c(N)n1 10.1021/jm058018d
CHEMBL197682 72069 None 0 Human Binding pKi = 6.9 6.9 -1 3
Binding affinity towards human Adenosine A2b receptor expressed in HEK293 cells using 5 nM [3H]DPCPXBinding affinity towards human Adenosine A2b receptor expressed in HEK293 cells using 5 nM [3H]DPCPX
ChEMBL 229 1 1 7 0.4 Cc1cc2c(nc(-n3nccn3)n2C)c(N)n1 10.1021/jm058018d
137660519 159410 None 0 Human Binding pKi = 6.9 6.9 - 1
Displacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 minsDisplacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 mins
ChEMBL 437 7 1 8 2.1 CCCn1c(=O)c2[nH]c(-c3cnn(CC#CCN4CCCCC4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2017.04.014
CHEMBL4100823 159410 None 0 Human Binding pKi = 6.9 6.9 - 1
Displacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 minsDisplacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 mins
ChEMBL 437 7 1 8 2.1 CCCn1c(=O)c2[nH]c(-c3cnn(CC#CCN4CCCCC4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2017.04.014
137645935 157576 None 0 Human Binding pKi = 5.9 5.9 -354 4
Displacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes measured after 90 minsDisplacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes measured after 90 mins
ChEMBL 446 6 1 8 3.5 COc1cnc(N2CCOCC2)c2sc(NC(=O)C(C)(C)Oc3ccc(F)cc3)nc12 10.1021/acs.jmedchem.6b01584
CHEMBL4080594 157576 None 0 Human Binding pKi = 5.9 5.9 -354 4
Displacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes measured after 90 minsDisplacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes measured after 90 mins
ChEMBL 446 6 1 8 3.5 COc1cnc(N2CCOCC2)c2sc(NC(=O)C(C)(C)Oc3ccc(F)cc3)nc12 10.1021/acs.jmedchem.6b01584
44308394 102635 None 0 Human Binding pKi = 4.9 4.9 - 1
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 224 2 0 7 -1.0 COCn1c(=O)c2c(ncn2C)n(C)c1=O 10.1021/jm0104318
CHEMBL304319 102635 None 0 Human Binding pKi = 4.9 4.9 - 1
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 224 2 0 7 -1.0 COCn1c(=O)c2c(ncn2C)n(C)c1=O 10.1021/jm0104318
22266744 96392 None 0 Human Binding pKi = 6.9 6.9 2 3
Displacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 302 4 2 6 1.0 CCn1c(=O)n(CC(C)C)c(=O)c2[nH]c(-c3cn[nH]c3)nc21 10.1021/jm7014815
CHEMBL261817 96392 None 0 Human Binding pKi = 6.9 6.9 2 3
Displacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 302 4 2 6 1.0 CCn1c(=O)n(CC(C)C)c(=O)c2[nH]c(-c3cn[nH]c3)nc21 10.1021/jm7014815
9923269 96030 None 0 Human Binding pKi = 6.9 6.9 -75 4
Inhibition of human recombinant adenosine receptor A2bInhibition of human recombinant adenosine receptor A2b
ChEMBL 324 3 2 8 2.0 Nc1nc(-c2ccco2)c2ncn(C(=O)NCc3ccco3)c2n1 10.1021/jm4011669
CHEMBL259832 96030 None 0 Human Binding pKi = 6.9 6.9 -75 4
Inhibition of human recombinant adenosine receptor A2bInhibition of human recombinant adenosine receptor A2b
ChEMBL 324 3 2 8 2.0 Nc1nc(-c2ccco2)c2ncn(C(=O)NCc3ccco3)c2n1 10.1021/jm4011669
11720443 140651 None 0 Human Binding pKi = 6.9 6.9 5 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 512 9 2 6 4.8 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccccc4F)cc3)c(Cl)c2n(CCC)c1=O 10.1021/jm0506221
CHEMBL381473 140651 None 0 Human Binding pKi = 6.9 6.9 5 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 512 9 2 6 4.8 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccccc4F)cc3)c(Cl)c2n(CCC)c1=O 10.1021/jm0506221
168281755 190905 None 0 Human Binding pKi = 6.9 6.9 - 1
Displacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cell membrane and measured after 0.5 hrs by radioligand displacement assayDisplacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cell membrane and measured after 0.5 hrs by radioligand displacement assay
ChEMBL 368 5 2 7 1.1 CCCn1c(=O)[nH]c2nc(-c3cccc(OS(=O)(=O)F)c3)[nH]c2c1=O 10.1039/d2md00132b
CHEMBL5185103 190905 None 0 Human Binding pKi = 6.9 6.9 - 1
Displacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cell membrane and measured after 0.5 hrs by radioligand displacement assayDisplacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cell membrane and measured after 0.5 hrs by radioligand displacement assay
ChEMBL 368 5 2 7 1.1 CCCn1c(=O)[nH]c2nc(-c3cccc(OS(=O)(=O)F)c3)[nH]c2c1=O 10.1039/d2md00132b
10884265 57410 None 0 Human Binding pKi = 6.9 6.9 -588 4
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 128-156Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 128-156
ChEMBL 418 3 2 10 2.6 Cn1cc2c(nc(NC(=O)Nc3ccc4c(c3)OCO4)n3nc(-c4ccco4)nc23)n1 10.1021/jm0109614
CHEMBL165224 57410 None 0 Human Binding pKi = 6.9 6.9 -588 4
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 128-156Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 128-156
ChEMBL 418 3 2 10 2.6 Cn1cc2c(nc(NC(=O)Nc3ccc4c(c3)OCO4)n3nc(-c4ccco4)nc23)n1 10.1021/jm0109614
76011 203657 None 8 Rat Binding pKi = 4.9 4.9 -2 3
Inhibition of [125I]-APOBX binding to rat Adenosine A2B receptor expressed in HEK cellsInhibition of [125I]-APOBX binding to rat Adenosine A2B receptor expressed in HEK cells
ChEMBL 256 3 0 6 0.1 Cn1c(=O)c2c(ncn2CCCCl)n(C)c1=O 10.1021/jm0104318
CHEMBL67323 203657 None 8 Rat Binding pKi = 4.9 4.9 -2 3
Inhibition of [125I]-APOBX binding to rat Adenosine A2B receptor expressed in HEK cellsInhibition of [125I]-APOBX binding to rat Adenosine A2B receptor expressed in HEK cells
ChEMBL 256 3 0 6 0.1 Cn1c(=O)c2c(ncn2CCCCl)n(C)c1=O 10.1021/jm0104318
11784369 119925 None 0 Human Binding pKi = 6.8 6.8 -4 4
Displacement of [3H]-DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 118-173Displacement of [3H]-DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 118-173
ChEMBL 401 6 1 8 3.3 CCCn1cc2c(nc(NC(=O)Cc3ccccc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm0109614
CHEMBL349464 119925 None 0 Human Binding pKi = 6.8 6.8 -4 4
Displacement of [3H]-DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 118-173Displacement of [3H]-DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 118-173
ChEMBL 401 6 1 8 3.3 CCCn1cc2c(nc(NC(=O)Cc3ccccc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm0109614
11683855 72602 None 0 Human Binding pKi = 6.8 6.8 -3 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 452 6 2 7 2.4 COc1cc(-c2cc3c([nH]2)c(=O)n(C)c(=O)n3C)ccc1OCC(=O)Nc1ccc(F)cc1 10.1021/jm0506221
CHEMBL199353 72602 None 0 Human Binding pKi = 6.8 6.8 -3 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 452 6 2 7 2.4 COc1cc(-c2cc3c([nH]2)c(=O)n(C)c(=O)n3C)ccc1OCC(=O)Nc1ccc(F)cc1 10.1021/jm0506221
44452454 95954 None 0 Human Binding pKi = 6.8 6.8 3 4
Displacement of [3]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 332 4 0 7 3.7 c1coc(-c2nc3c(OCc4ccoc4)nc4ccccc4n3n2)c1 10.1016/j.bmc.2007.10.103
CHEMBL259430 95954 None 0 Human Binding pKi = 6.8 6.8 3 4
Displacement of [3]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 332 4 0 7 3.7 c1coc(-c2nc3c(OCc4ccoc4)nc4ccccc4n3n2)c1 10.1016/j.bmc.2007.10.103
44316331 205499 None 0 Rat Binding pKi = 5.8 5.8 -97 3
Compound was tested for its binding affinity against Alpha-2 adrenergic receptorCompound was tested for its binding affinity against Alpha-2 adrenergic receptor
ChEMBL 468 11 4 6 4.8 Oc1ccc(C[C@@H]2CCCN2CCCCCCN2CCC[C@H]2Cc2ccc(O)c(O)c2)cc1O 10.1016/0960-894X(95)00413-N
CHEMBL80686 205499 None 0 Rat Binding pKi = 5.8 5.8 -97 3
Compound was tested for its binding affinity against Alpha-2 adrenergic receptorCompound was tested for its binding affinity against Alpha-2 adrenergic receptor
ChEMBL 468 11 4 6 4.8 Oc1ccc(C[C@@H]2CCCN2CCCCCCN2CCC[C@H]2Cc2ccc(O)c(O)c2)cc1O 10.1016/0960-894X(95)00413-N
24812771 175707 None 4 Human Binding pKi = 6.8 6.8 -16 5
Inhibition of human adenosine A2B receptorInhibition of human adenosine A2B receptor
ChEMBL 344 5 1 7 1.9 COC[C@H]1CCCN1c1cc(NC(C)=O)nc(-n2nc(C)cc2C)n1 10.1021/jm800908d
CHEMBL458224 175707 None 4 Human Binding pKi = 6.8 6.8 -16 5
Inhibition of human adenosine A2B receptorInhibition of human adenosine A2B receptor
ChEMBL 344 5 1 7 1.9 COC[C@H]1CCCN1c1cc(NC(C)=O)nc(-n2nc(C)cc2C)n1 10.1021/jm800908d
44390527 64547 None 0 Human Binding pKi = 5.8 5.8 1 2
Binding affinity for adenosine A2b receptor by using as [3H]ZM-241385 (14 nM) radioligand in membranes from HEK-A2B cellsBinding affinity for adenosine A2b receptor by using as [3H]ZM-241385 (14 nM) radioligand in membranes from HEK-A2B cells
ChEMBL 504 9 1 9 4.1 CCCn1c(=O)c2nc(-c3ccc(OCc4nc(-c5cccc(F)c5)no4)cc3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2004.11.044
CHEMBL181468 64547 None 0 Human Binding pKi = 5.8 5.8 1 2
Binding affinity for adenosine A2b receptor by using as [3H]ZM-241385 (14 nM) radioligand in membranes from HEK-A2B cellsBinding affinity for adenosine A2b receptor by using as [3H]ZM-241385 (14 nM) radioligand in membranes from HEK-A2B cells
ChEMBL 504 9 1 9 4.1 CCCn1c(=O)c2nc(-c3ccc(OCc4nc(-c5cccc(F)c5)no4)cc3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2004.11.044
44442167 154884 None 0 Human Binding pKi = 5.8 5.8 -204 3
Binding affinity to adenosine A2B receptorBinding affinity to adenosine A2B receptor
ChEMBL 602 8 5 11 2.3 CC1(C)c2ccc(C(=O)NCCc3ccc(Nc4ncnc5c4ncn5[C@@H]4O[C@H](CO)[C@@H](O)[C@H]4O)cc3)cc2C(C)(C)N1[O] 10.1016/j.bmcl.2007.07.035
CHEMBL400746 154884 None 0 Human Binding pKi = 5.8 5.8 -204 3
Binding affinity to adenosine A2B receptorBinding affinity to adenosine A2B receptor
ChEMBL 602 8 5 11 2.3 CC1(C)c2ccc(C(=O)NCCc3ccc(Nc4ncnc5c4ncn5[C@@H]4O[C@H](CO)[C@@H](O)[C@H]4O)cc3)cc2C(C)(C)N1[O] 10.1016/j.bmcl.2007.07.035
217940 203479 None 28 Human Binding pKi = 4.8 4.8 - 1
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 219 1 0 7 -1.0 Cn1c(=O)c2c(ncn2CC#N)n(C)c1=O 10.1021/jm0104318
CHEMBL66058 203479 None 28 Human Binding pKi = 4.8 4.8 - 1
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 219 1 0 7 -1.0 Cn1c(=O)c2c(ncn2CC#N)n(C)c1=O 10.1021/jm0104318
45268928 196146 None 0 Human Binding pKi = 6.8 6.8 2 2
Binding affinity to human adenosine A2b receptor expressed in HEK293 cellsBinding affinity to human adenosine A2b receptor expressed in HEK293 cells
ChEMBL 331 7 2 6 1.3 CCCn1c(=O)c2[nH]c(-c3ccc[nH]3)nc2n(CCCOC)c1=O 10.1016/j.bmc.2009.03.029
CHEMBL561168 196146 None 0 Human Binding pKi = 6.8 6.8 2 2
Binding affinity to human adenosine A2b receptor expressed in HEK293 cellsBinding affinity to human adenosine A2b receptor expressed in HEK293 cells
ChEMBL 331 7 2 6 1.3 CCCn1c(=O)c2[nH]c(-c3ccc[nH]3)nc2n(CCCOC)c1=O 10.1016/j.bmc.2009.03.029
11711754 72603 None 0 Human Binding pKi = 6.8 6.8 2 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 434 6 2 7 2.3 COc1cc(-c2cc3c([nH]2)c(=O)n(C)c(=O)n3C)ccc1OCC(=O)Nc1ccccc1 10.1021/jm0506221
CHEMBL199354 72603 None 0 Human Binding pKi = 6.8 6.8 2 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 434 6 2 7 2.3 COc1cc(-c2cc3c([nH]2)c(=O)n(C)c(=O)n3C)ccc1OCC(=O)Nc1ccccc1 10.1021/jm0506221
127026188 138085 None 0 Human Binding pKi = 5.8 5.8 -1348 5
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 329 3 2 5 2.7 Nc1nc(C(=O)NCc2cccc3cccnc23)c2ccccc2n1 10.1016/j.bmcl.2015.11.048
CHEMBL3765818 138085 None 0 Human Binding pKi = 5.8 5.8 -1348 5
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 329 3 2 5 2.7 Nc1nc(C(=O)NCc2cccc3cccnc23)c2ccccc2n1 10.1016/j.bmcl.2015.11.048
76320870 103843 None 0 Human Binding pKi = 5.8 5.8 - 1
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 minsDisplacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 mins
ChEMBL 264 3 2 4 1.9 CC1=C(C(=O)OC(C)C)C(c2ccoc2)NC(=O)N1 10.1021/acs.jmedchem.5b01586
CHEMBL3091699 103843 None 0 Human Binding pKi = 5.8 5.8 - 1
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 minsDisplacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 mins
ChEMBL 264 3 2 4 1.9 CC1=C(C(=O)OC(C)C)C(c2ccoc2)NC(=O)N1 10.1021/acs.jmedchem.5b01586
76320870 103843 None 0 Human Binding pKi = 5.8 5.8 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes after 30 minsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes after 30 mins
ChEMBL 264 3 2 4 1.9 CC1=C(C(=O)OC(C)C)C(c2ccoc2)NC(=O)N1 10.1021/acs.jmedchem.7b00138
CHEMBL3091699 103843 None 0 Human Binding pKi = 5.8 5.8 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes after 30 minsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes after 30 mins
ChEMBL 264 3 2 4 1.9 CC1=C(C(=O)OC(C)C)C(c2ccoc2)NC(=O)N1 10.1021/acs.jmedchem.7b00138
76320870 103843 None 0 Human Binding pKi = 5.8 5.8 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 264 3 2 4 1.9 CC1=C(C(=O)OC(C)C)C(c2ccoc2)NC(=O)N1 10.1021/acs.jmedchem.0c01431
CHEMBL3091699 103843 None 0 Human Binding pKi = 5.8 5.8 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 264 3 2 4 1.9 CC1=C(C(=O)OC(C)C)C(c2ccoc2)NC(=O)N1 10.1021/acs.jmedchem.0c01431
76320870 103843 None 0 Human Binding pKi = 5.8 5.8 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by Scatchard plot analysisDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by Scatchard plot analysis
ChEMBL 264 3 2 4 1.9 CC1=C(C(=O)OC(C)C)C(c2ccoc2)NC(=O)N1 10.1021/ml400185v
CHEMBL3091699 103843 None 0 Human Binding pKi = 5.8 5.8 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by Scatchard plot analysisDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by Scatchard plot analysis
ChEMBL 264 3 2 4 1.9 CC1=C(C(=O)OC(C)C)C(c2ccoc2)NC(=O)N1 10.1021/ml400185v
76320870 103843 None 0 Human Binding pKi = 5.8 5.8 - 1
Displacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assayDisplacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assay
ChEMBL 264 3 2 4 1.9 CC1=C(C(=O)OC(C)C)C(c2ccoc2)NC(=O)N1 10.1021/acs.jmedchem.9b01340
CHEMBL3091699 103843 None 0 Human Binding pKi = 5.8 5.8 - 1
Displacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assayDisplacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assay
ChEMBL 264 3 2 4 1.9 CC1=C(C(=O)OC(C)C)C(c2ccoc2)NC(=O)N1 10.1021/acs.jmedchem.9b01340
135443367 487 None 0 Human Binding pKi = 7.8 7.8 22 2
Binding affinity of compound for displacement of [3H]DPCPX binding in HEK293 membranes expressing human A2B adenosine receptorsBinding affinity of compound for displacement of [3H]DPCPX binding in HEK293 membranes expressing human A2B adenosine receptors
ChEMBL 534 9 1 10 1.8 CCCn1c2[nH]c(nc2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)N1CCN(CC1)c1ccccc1 10.1021/jm0309654
382 487 None 0 Human Binding pKi = 7.8 7.8 22 2
Binding affinity of compound for displacement of [3H]DPCPX binding in HEK293 membranes expressing human A2B adenosine receptorsBinding affinity of compound for displacement of [3H]DPCPX binding in HEK293 membranes expressing human A2B adenosine receptors
ChEMBL 534 9 1 10 1.8 CCCn1c2[nH]c(nc2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)N1CCN(CC1)c1ccccc1 10.1021/jm0309654
CHEMBL33455 487 None 0 Human Binding pKi = 7.8 7.8 22 2
Binding affinity of compound for displacement of [3H]DPCPX binding in HEK293 membranes expressing human A2B adenosine receptorsBinding affinity of compound for displacement of [3H]DPCPX binding in HEK293 membranes expressing human A2B adenosine receptors
ChEMBL 534 9 1 10 1.8 CCCn1c2[nH]c(nc2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)N1CCN(CC1)c1ccccc1 10.1021/jm0309654
135443367 487 None 0 Human Binding pKi = 7.8 7.8 22 2
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 534 9 1 10 1.8 CCCn1c2[nH]c(nc2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)N1CCN(CC1)c1ccccc1 10.1021/jm0309654
382 487 None 0 Human Binding pKi = 7.8 7.8 22 2
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 534 9 1 10 1.8 CCCn1c2[nH]c(nc2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)N1CCN(CC1)c1ccccc1 10.1021/jm0309654
CHEMBL33455 487 None 0 Human Binding pKi = 7.8 7.8 22 2
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 534 9 1 10 1.8 CCCn1c2[nH]c(nc2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)N1CCN(CC1)c1ccccc1 10.1021/jm0309654
135915276 158621 None 0 Human Binding pKi = 7.8 7.8 - 1
Displacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 minsDisplacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 mins
ChEMBL 451 7 1 8 2.9 CCCn1c(=O)c2[nH]c(-c3cc(OCC#Cc4ccc(F)cc4)no3)nc2n(CCC)c1=O 10.1016/j.ejmech.2017.04.014
CHEMBL4092291 158621 None 0 Human Binding pKi = 7.8 7.8 - 1
Displacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 minsDisplacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 mins
ChEMBL 451 7 1 8 2.9 CCCn1c(=O)c2[nH]c(-c3cc(OCC#Cc4ccc(F)cc4)no3)nc2n(CCC)c1=O 10.1016/j.ejmech.2017.04.014
22266761 94555 None 0 Human Binding pKi = 7.8 7.8 229 2
Displacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranesDisplacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranes
ChEMBL 418 6 2 9 1.8 CCCn1c(=O)[nH]c2nc(-c3cnn(Cc4noc(-c5ccccc5)n4)c3)[nH]c2c1=O 10.1016/j.bmcl.2008.01.008
CHEMBL251854 94555 None 0 Human Binding pKi = 7.8 7.8 229 2
Displacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranesDisplacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranes
ChEMBL 418 6 2 9 1.8 CCCn1c(=O)[nH]c2nc(-c3cnn(Cc4noc(-c5ccccc5)n4)c3)[nH]c2c1=O 10.1016/j.bmcl.2008.01.008
22266751 94568 None 0 Human Binding pKi = 7.8 7.8 - 1
Displacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranesDisplacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranes
ChEMBL 497 6 2 8 3.4 O=c1[nH]c2nc(-c3cnn(Cc4cc(-c5ccc(C(F)(F)F)cc5)on4)c3)[nH]c2c(=O)n1CC1CC1 10.1016/j.bmcl.2008.01.008
CHEMBL251881 94568 None 0 Human Binding pKi = 7.8 7.8 - 1
Displacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranesDisplacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranes
ChEMBL 497 6 2 8 3.4 O=c1[nH]c2nc(-c3cnn(Cc4cc(-c5ccc(C(F)(F)F)cc5)on4)c3)[nH]c2c(=O)n1CC1CC1 10.1016/j.bmcl.2008.01.008
22266776 166515 None 0 Human Binding pKi = 7.8 7.8 93 2
Displacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranesDisplacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranes
ChEMBL 486 6 2 9 2.8 CCCn1c(=O)[nH]c2nc(-c3cnn(Cc4noc(-c5ccc(C(F)(F)F)cc5)n4)c3)[nH]c2c1=O 10.1016/j.bmcl.2008.01.008
CHEMBL427887 166515 None 0 Human Binding pKi = 7.8 7.8 93 2
Displacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranesDisplacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranes
ChEMBL 486 6 2 9 2.8 CCCn1c(=O)[nH]c2nc(-c3cnn(Cc4noc(-c5ccc(C(F)(F)F)cc5)n4)c3)[nH]c2c1=O 10.1016/j.bmcl.2008.01.008
135874413 96390 None 0 Human Binding pKi = 7.8 7.8 22 2
Displacement of [3H]MRE2029F20 from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]MRE2029F20 from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 449 8 2 8 2.5 CCCn1c(=O)c2[nH]c(-c3cc(C)n(CC(=O)Nc4ccccc4)n3)nc2n(CCC)c1=O 10.1016/j.bmc.2007.11.058
CHEMBL261810 96390 None 0 Human Binding pKi = 7.8 7.8 22 2
Displacement of [3H]MRE2029F20 from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]MRE2029F20 from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 449 8 2 8 2.5 CCCn1c(=O)c2[nH]c(-c3cc(C)n(CC(=O)Nc4ccccc4)n3)nc2n(CCC)c1=O 10.1016/j.bmc.2007.11.058
49797793 10854 None 0 Human Binding pKi = 7.8 7.8 11 3
Displacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cells after 1 hr by scintillation countingDisplacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 427 6 1 7 3.7 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(C(=O)OC)cc3)sc12 10.1016/j.bmcl.2010.05.056
CHEMBL1172274 10854 None 0 Human Binding pKi = 7.8 7.8 11 3
Displacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cells after 1 hr by scintillation countingDisplacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 427 6 1 7 3.7 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(C(=O)OC)cc3)sc12 10.1016/j.bmcl.2010.05.056
137638964 156862 None 0 Human Binding pKi = 7.8 7.8 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes after 30 minsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes after 30 mins
ChEMBL 288 3 2 5 1.6 CC1=C(C(=O)OC(C)C)[C@@H](c2ccco2)N/C(=N/C#N)N1 10.1021/acs.jmedchem.7b00138
CHEMBL4071734 156862 None 0 Human Binding pKi = 7.8 7.8 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes after 30 minsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes after 30 mins
ChEMBL 288 3 2 5 1.6 CC1=C(C(=O)OC(C)C)[C@@H](c2ccco2)N/C(=N/C#N)N1 10.1021/acs.jmedchem.7b00138
10882425 79169 None 0 Human Binding pKi = 7.8 7.8 13 4
Inhibition of [3H]ZM-241385 binding to human adenosine A2B receptorInhibition of [3H]ZM-241385 binding to human adenosine A2B receptor
ChEMBL 342 6 3 5 1.5 CCCCn1c(=O)[nH]c2nc(-c3ccc(CC(=O)O)cc3)[nH]c2c1=O 10.1021/jm011049y
CHEMBL2113345 79169 None 0 Human Binding pKi = 7.8 7.8 13 4
Inhibition of [3H]ZM-241385 binding to human adenosine A2B receptorInhibition of [3H]ZM-241385 binding to human adenosine A2B receptor
ChEMBL 342 6 3 5 1.5 CCCCn1c(=O)[nH]c2nc(-c3ccc(CC(=O)O)cc3)[nH]c2c1=O 10.1021/jm011049y
11611298 139223 None 0 Human Binding pKi = 7.8 7.8 1 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 412 5 2 9 1.1 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4nncs4)cc3)cc2n(C)c1=O 10.1021/jm0506221
CHEMBL378815 139223 None 0 Human Binding pKi = 7.8 7.8 1 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 412 5 2 9 1.1 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4nncs4)cc3)cc2n(C)c1=O 10.1021/jm0506221
44451048 95986 None 0 Human Binding pKi = 7.8 7.8 15 3
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 519 7 1 7 3.0 CCCn1c(=O)n(C)c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCN(c5ccc(F)cc5)CC4)cc3)cc21 10.1016/j.bmc.2008.01.002
CHEMBL259580 95986 None 0 Human Binding pKi = 7.8 7.8 15 3
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 519 7 1 7 3.0 CCCn1c(=O)n(C)c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCN(c5ccc(F)cc5)CC4)cc3)cc21 10.1016/j.bmc.2008.01.002
155511376 169555 None 0 Human Binding pKi = 7.8 7.8 - 1
Displacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assayDisplacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assay
ChEMBL 391 3 1 6 4.4 CC1=C(C(=O)O[C@@H](C)C(F)(F)F)C(c2ccco2)n2c(nc3ccccc32)N1 10.1021/acs.jmedchem.9b01340
CHEMBL4435630 169555 None 0 Human Binding pKi = 7.8 7.8 - 1
Displacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assayDisplacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assay
ChEMBL 391 3 1 6 4.4 CC1=C(C(=O)O[C@@H](C)C(F)(F)F)C(c2ccco2)n2c(nc3ccccc32)N1 10.1021/acs.jmedchem.9b01340
45272259 195643 None 0 Human Binding pKi = 7.8 7.8 10 2
Binding affinity to human adenosine A2b receptor expressed in HEK293 cellsBinding affinity to human adenosine A2b receptor expressed in HEK293 cells
ChEMBL 478 10 2 9 2.0 CCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccccn4)cc3)nc2n(CCCOC)c1=O 10.1016/j.bmc.2009.03.029
CHEMBL556389 195643 None 0 Human Binding pKi = 7.8 7.8 10 2
Binding affinity to human adenosine A2b receptor expressed in HEK293 cellsBinding affinity to human adenosine A2b receptor expressed in HEK293 cells
ChEMBL 478 10 2 9 2.0 CCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccccn4)cc3)nc2n(CCCOC)c1=O 10.1016/j.bmc.2009.03.029
45269711 196343 None 0 Human Binding pKi = 7.8 7.8 11 3
Binding affinity to human adenosine A2b receptor expressed in HEK293 cellsBinding affinity to human adenosine A2b receptor expressed in HEK293 cells
ChEMBL 493 10 3 9 2.3 CCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(O)cc4)cc3)nc2n(CCCOC)c1=O 10.1016/j.bmc.2009.03.029
CHEMBL562427 196343 None 0 Human Binding pKi = 7.8 7.8 11 3
Binding affinity to human adenosine A2b receptor expressed in HEK293 cellsBinding affinity to human adenosine A2b receptor expressed in HEK293 cells
ChEMBL 493 10 3 9 2.3 CCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(O)cc4)cc3)nc2n(CCCOC)c1=O 10.1016/j.bmc.2009.03.029
11660995 72812 None 0 Human Binding pKi = 7.8 7.8 7 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 385 8 2 6 2.4 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)O)cc3)cc2n(CCC)c1=O 10.1021/jm0506221
CHEMBL200112 72812 None 0 Human Binding pKi = 7.8 7.8 7 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 385 8 2 6 2.4 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)O)cc3)cc2n(CCC)c1=O 10.1021/jm0506221
136042352 71152 None 0 Human Binding pKi = 7.8 7.8 17 2
Displacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation countingDisplacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation counting
ChEMBL 540 8 2 9 3.3 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5cc(Br)ccc5[nH]4)nn3C)nc2n(CCC)c1=O 10.1021/jm201292w
CHEMBL1955901 71152 None 0 Human Binding pKi = 7.8 7.8 17 2
Displacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation countingDisplacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation counting
ChEMBL 540 8 2 9 3.3 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5cc(Br)ccc5[nH]4)nn3C)nc2n(CCC)c1=O 10.1021/jm201292w
9910158 32450 None 0 Human Binding pKi = 6.8 6.8 -10 6
Displacement of [3H]-DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 107-210Displacement of [3H]-DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 107-210
ChEMBL 422 4 2 8 4.1 CCn1cc2c(nc(NC(=O)Nc3cccc(Cl)c3)n3nc(-c4ccco4)nc23)n1 10.1021/jm0109614
CHEMBL141154 32450 None 0 Human Binding pKi = 6.8 6.8 -10 6
Displacement of [3H]-DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 107-210Displacement of [3H]-DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 107-210
ChEMBL 422 4 2 8 4.1 CCn1cc2c(nc(NC(=O)Nc3cccc(Cl)c3)n3nc(-c4ccco4)nc23)n1 10.1021/jm0109614
9910158 32450 None 0 Human Binding pKi = 6.8 6.8 -10 6
Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 107-210Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 107-210
ChEMBL 422 4 2 8 4.1 CCn1cc2c(nc(NC(=O)Nc3cccc(Cl)c3)n3nc(-c4ccco4)nc23)n1 10.1021/jm001047y
CHEMBL141154 32450 None 0 Human Binding pKi = 6.8 6.8 -10 6
Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 107-210Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 107-210
ChEMBL 422 4 2 8 4.1 CCn1cc2c(nc(NC(=O)Nc3cccc(Cl)c3)n3nc(-c4ccco4)nc23)n1 10.1021/jm001047y
11080788 56760 None 0 Human Binding pKi = 6.8 6.8 -7 4
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 124-180Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 124-180
ChEMBL 446 7 2 9 4.2 CCCCn1cc2c(nc(NC(=O)Nc3cccc(OC)c3)n3nc(-c4ccco4)nc23)n1 10.1021/jm0109614
CHEMBL164325 56760 None 0 Human Binding pKi = 6.8 6.8 -7 4
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 124-180Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 124-180
ChEMBL 446 7 2 9 4.2 CCCCn1cc2c(nc(NC(=O)Nc3cccc(OC)c3)n3nc(-c4ccco4)nc23)n1 10.1021/jm0109614
11733556 120017 None 0 Human Binding pKi = 6.8 6.8 -10 4
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 124-180Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 124-180
ChEMBL 480 5 2 8 4.6 CCCn1cc2c(nc(NC(=O)Nc3ccc(Br)cc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm0109614
CHEMBL350205 120017 None 0 Human Binding pKi = 6.8 6.8 -10 4
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 124-180Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 124-180
ChEMBL 480 5 2 8 4.6 CCCn1cc2c(nc(NC(=O)Nc3ccc(Br)cc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm0109614
11780616 203611 None 5 Human Binding pKi = 4.8 4.8 1 4
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 270 4 0 6 0.5 Cn1c(=O)c2c(ncn2CCCCCl)n(C)c1=O 10.1021/jm0104318
CHEMBL67060 203611 None 5 Human Binding pKi = 4.8 4.8 1 4
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 270 4 0 6 0.5 Cn1c(=O)c2c(ncn2CCCCCl)n(C)c1=O 10.1021/jm0104318
2153 3800 None 115 Rat Binding pKi = 4.8 4.8 -1 14
Binding affinity to rat adenosine A2B receptorBinding affinity to rat adenosine A2B receptor
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1016/j.bmc.2010.01.072
2153 3800 None 115 Rat Binding pKi = 4.8 4.8 -1 14
Binding affinity to rat adenosine A2B receptorBinding affinity to rat adenosine A2B receptor
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1021/jm900413e
2153.0 3800 None 115 Rat Binding pKi = 4.8 4.8 -1 14
Binding affinity to rat adenosine A2B receptorBinding affinity to rat adenosine A2B receptor
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1016/j.bmc.2010.01.072
2153.0 3800 None 115 Rat Binding pKi = 4.8 4.8 -1 14
Binding affinity to rat adenosine A2B receptorBinding affinity to rat adenosine A2B receptor
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1021/jm900413e
2620 3800 None 115 Rat Binding pKi = 4.8 4.8 -1 14
Binding affinity to rat adenosine A2B receptorBinding affinity to rat adenosine A2B receptor
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1016/j.bmc.2010.01.072
2620 3800 None 115 Rat Binding pKi = 4.8 4.8 -1 14
Binding affinity to rat adenosine A2B receptorBinding affinity to rat adenosine A2B receptor
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1021/jm900413e
413 3800 None 115 Rat Binding pKi = 4.8 4.8 -1 14
Binding affinity to rat adenosine A2B receptorBinding affinity to rat adenosine A2B receptor
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1016/j.bmc.2010.01.072
413 3800 None 115 Rat Binding pKi = 4.8 4.8 -1 14
Binding affinity to rat adenosine A2B receptorBinding affinity to rat adenosine A2B receptor
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1021/jm900413e
CHEMBL190 3800 None 115 Rat Binding pKi = 4.8 4.8 -1 14
Binding affinity to rat adenosine A2B receptorBinding affinity to rat adenosine A2B receptor
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1016/j.bmc.2010.01.072
CHEMBL190 3800 None 115 Rat Binding pKi = 4.8 4.8 -1 14
Binding affinity to rat adenosine A2B receptorBinding affinity to rat adenosine A2B receptor
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1021/jm900413e
DB00277 3800 None 115 Rat Binding pKi = 4.8 4.8 -1 14
Binding affinity to rat adenosine A2B receptorBinding affinity to rat adenosine A2B receptor
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1016/j.bmc.2010.01.072
DB00277 3800 None 115 Rat Binding pKi = 4.8 4.8 -1 14
Binding affinity to rat adenosine A2B receptorBinding affinity to rat adenosine A2B receptor
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1021/jm900413e
2153 3800 None 115 Rat Binding pKi = 4.8 4.8 -1 14
Inhibition of [125I]-APOBX binding to rat Adenosine A2B receptor expressed in HEK cellsInhibition of [125I]-APOBX binding to rat Adenosine A2B receptor expressed in HEK cells
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1021/jm0104318
2153.0 3800 None 115 Rat Binding pKi = 4.8 4.8 -1 14
Inhibition of [125I]-APOBX binding to rat Adenosine A2B receptor expressed in HEK cellsInhibition of [125I]-APOBX binding to rat Adenosine A2B receptor expressed in HEK cells
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1021/jm0104318
2620 3800 None 115 Rat Binding pKi = 4.8 4.8 -1 14
Inhibition of [125I]-APOBX binding to rat Adenosine A2B receptor expressed in HEK cellsInhibition of [125I]-APOBX binding to rat Adenosine A2B receptor expressed in HEK cells
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1021/jm0104318
413 3800 None 115 Rat Binding pKi = 4.8 4.8 -1 14
Inhibition of [125I]-APOBX binding to rat Adenosine A2B receptor expressed in HEK cellsInhibition of [125I]-APOBX binding to rat Adenosine A2B receptor expressed in HEK cells
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1021/jm0104318
CHEMBL190 3800 None 115 Rat Binding pKi = 4.8 4.8 -1 14
Inhibition of [125I]-APOBX binding to rat Adenosine A2B receptor expressed in HEK cellsInhibition of [125I]-APOBX binding to rat Adenosine A2B receptor expressed in HEK cells
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1021/jm0104318
DB00277 3800 None 115 Rat Binding pKi = 4.8 4.8 -1 14
Inhibition of [125I]-APOBX binding to rat Adenosine A2B receptor expressed in HEK cellsInhibition of [125I]-APOBX binding to rat Adenosine A2B receptor expressed in HEK cells
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1021/jm0104318
11509299 72782 None 0 Human Binding pKi = 5.8 5.8 2 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 387 6 1 8 1.2 CCOC(=O)COc1ccc(-c2cc3c([nH]2)c(=O)n(C)c(=O)n3C)cc1OC 10.1021/jm0506221
CHEMBL200012 72782 None 0 Human Binding pKi = 5.8 5.8 2 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 387 6 1 8 1.2 CCOC(=O)COc1ccc(-c2cc3c([nH]2)c(=O)n(C)c(=O)n3C)cc1OC 10.1021/jm0506221
2917279 181677 None 15 Human Binding pKi = 5.8 5.8 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 280 4 2 4 2.3 CCCOC(=O)C1=C(C)NC(=O)NC1c1cccs1 10.1021/acs.jmedchem.0c01431
CHEMBL4776470 181677 None 15 Human Binding pKi = 5.8 5.8 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 280 4 2 4 2.3 CCCOC(=O)C1=C(C)NC(=O)NC1c1cccs1 10.1021/acs.jmedchem.0c01431
9814428 71497 None 0 Human Binding pKi = 6.8 6.8 -45 4
Binding affinity towards human Adenosine A2b receptor expressed in HEK293 cells using 5 nM [3H]DPCPXBinding affinity towards human Adenosine A2b receptor expressed in HEK293 cells using 5 nM [3H]DPCPX
ChEMBL 286 5 1 8 1.3 CCCCCc1nc(N)c2nc(-n3nccn3)n(C)c2n1 10.1021/jm058018d
CHEMBL196258 71497 None 0 Human Binding pKi = 6.8 6.8 -45 4
Binding affinity towards human Adenosine A2b receptor expressed in HEK293 cells using 5 nM [3H]DPCPXBinding affinity towards human Adenosine A2b receptor expressed in HEK293 cells using 5 nM [3H]DPCPX
ChEMBL 286 5 1 8 1.3 CCCCCc1nc(N)c2nc(-n3nccn3)n(C)c2n1 10.1021/jm058018d
11822168 203656 None 0 Rat Binding pKi = 4.8 4.8 -6 4
Inhibition of [125I]-APOBX binding to rat Adenosine A2B receptor expressed in HEK cellsInhibition of [125I]-APOBX binding to rat Adenosine A2B receptor expressed in HEK cells
ChEMBL 284 4 1 5 1.1 Cn1c(=O)n(CCCc2ccccc2)c(=O)c2[nH]cnc21 10.1021/jm0104318
CHEMBL67313 203656 None 0 Rat Binding pKi = 4.8 4.8 -6 4
Inhibition of [125I]-APOBX binding to rat Adenosine A2B receptor expressed in HEK cellsInhibition of [125I]-APOBX binding to rat Adenosine A2B receptor expressed in HEK cells
ChEMBL 284 4 1 5 1.1 Cn1c(=O)n(CCCc2ccccc2)c(=O)c2[nH]cnc21 10.1021/jm0104318
11610869 80256 None 0 Human Binding pKi = 6.8 6.8 -2 3
Displacement of [3H]PSB298 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB298 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 393 5 3 8 -1.0 Cn1c(=O)c2nc(-c3ccc(S(=O)(=O)NCC(=O)O)cc3)[nH]c2n(C)c1=O 10.1021/jm060277v
CHEMBL213878 80256 None 0 Human Binding pKi = 6.8 6.8 -2 3
Displacement of [3H]PSB298 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB298 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 393 5 3 8 -1.0 Cn1c(=O)c2nc(-c3ccc(S(=O)(=O)NCC(=O)O)cc3)[nH]c2n(C)c1=O 10.1021/jm060277v
71451329 81019 None 0 Human Binding pKi = 5.8 5.8 -5128 3
Displacement of [3H]MRS-1754 from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]MRS-1754 from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 372 5 1 7 1.4 CCCn1c(=O)c2[nH]c(C3C4CC5OC(=O)C3C5C4)nc2n(CCC)c1=O 10.1016/j.ejmech.2011.05.023
CHEMBL2153721 81019 None 0 Human Binding pKi = 5.8 5.8 -5128 3
Displacement of [3H]MRS-1754 from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]MRS-1754 from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 372 5 1 7 1.4 CCCn1c(=O)c2[nH]c(C3C4CC5OC(=O)C3C5C4)nc2n(CCC)c1=O 10.1016/j.ejmech.2011.05.023
44308307 102642 None 0 Human Binding pKi = 4.8 4.8 - 1
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 346 3 1 9 0.4 Cn1c(=O)c2nc(-c3ccc([N+](=O)[O-])cc3[N+](=O)[O-])[nH]c2n(C)c1=O 10.1021/jm0104318
CHEMBL304356 102642 None 0 Human Binding pKi = 4.8 4.8 - 1
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 346 3 1 9 0.4 Cn1c(=O)c2nc(-c3ccc([N+](=O)[O-])cc3[N+](=O)[O-])[nH]c2n(C)c1=O 10.1021/jm0104318
11530568 73362 None 0 Human Binding pKi = 5.8 5.8 - 1
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 359 5 2 7 0.7 COc1cc(OCC(=O)O)ccc1-c1cc2c([nH]1)c(=O)n(C)c(=O)n2C 10.1021/jm0506221
CHEMBL201330 73362 None 0 Human Binding pKi = 5.8 5.8 - 1
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 359 5 2 7 0.7 COc1cc(OCC(=O)O)ccc1-c1cc2c([nH]1)c(=O)n(C)c(=O)n2C 10.1021/jm0506221
44588437 175554 None 0 Human Binding pKi = 6.8 6.8 1 2
Displacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cells
ChEMBL 342 5 2 7 2.3 CCCn1c(=O)c2c(cc(-c3ccc(N)cc3)n2O)n(CCC)c1=O 10.1016/j.bmc.2008.09.067
CHEMBL457880 175554 None 0 Human Binding pKi = 6.8 6.8 1 2
Displacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cells
ChEMBL 342 5 2 7 2.3 CCCn1c(=O)c2c(cc(-c3ccc(N)cc3)n2O)n(CCC)c1=O 10.1016/j.bmc.2008.09.067
11393155 195614 None 0 Human Binding pKi = 6.8 6.8 -44 4
Binding affinity to adenosine A2B receptorBinding affinity to adenosine A2B receptor
ChEMBL 324 5 2 6 2.3 COc1ccccc1CNC(=O)c1cc(-c2ccco2)nc(N)n1 10.1016/j.bmcl.2009.03.142
CHEMBL556083 195614 None 0 Human Binding pKi = 6.8 6.8 -44 4
Binding affinity to adenosine A2B receptorBinding affinity to adenosine A2B receptor
ChEMBL 324 5 2 6 2.3 COc1ccccc1CNC(=O)c1cc(-c2ccco2)nc(N)n1 10.1016/j.bmcl.2009.03.142
44449635 155193 None 0 Human Binding pKi = 5.8 5.8 -676 4
Binding affinity at human adenosine A2B receptorBinding affinity at human adenosine A2B receptor
ChEMBL 262 2 0 6 2.9 CN(C)c1nc(-c2nccs2)c2sccc2n1 10.1016/j.bmcl.2008.03.076
CHEMBL402464 155193 None 0 Human Binding pKi = 5.8 5.8 -676 4
Binding affinity at human adenosine A2B receptorBinding affinity at human adenosine A2B receptor
ChEMBL 262 2 0 6 2.9 CN(C)c1nc(-c2nccs2)c2sccc2n1 10.1016/j.bmcl.2008.03.076
155516146 170051 None 0 Human Binding pKi = 6.8 6.8 - 1
Displacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assayDisplacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assay
ChEMBL 304 3 2 4 2.0 CC1=C(C(=O)OCC(F)(F)F)C(c2ccco2)NC(=O)N1 10.1021/acs.jmedchem.9b01340
CHEMBL4442922 170051 None 0 Human Binding pKi = 6.8 6.8 - 1
Displacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assayDisplacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assay
ChEMBL 304 3 2 4 2.0 CC1=C(C(=O)OCC(F)(F)F)C(c2ccco2)NC(=O)N1 10.1021/acs.jmedchem.9b01340
5130381 49070 None 17 Human Binding pKi = 5.8 5.8 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 296 3 2 5 2.9 CC1=C(C(=O)OC(C)C)C(c2cccs2)NC(S)=N1 10.1021/acs.jmedchem.0c01431
CHEMBL1561375 49070 None 17 Human Binding pKi = 5.8 5.8 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 296 3 2 5 2.9 CC1=C(C(=O)OC(C)C)C(c2cccs2)NC(S)=N1 10.1021/acs.jmedchem.0c01431
162671451 182865 None 0 Human Binding pKi = 5.8 5.8 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 292 4 2 4 2.3 CC1=C(C(=O)OCC2CC2)C(c2cccs2)NC(=O)N1 10.1021/acs.jmedchem.0c01431
CHEMBL4791727 182865 None 0 Human Binding pKi = 5.8 5.8 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 292 4 2 4 2.3 CC1=C(C(=O)OCC2CC2)C(c2cccs2)NC(=O)N1 10.1021/acs.jmedchem.0c01431
5130381 49070 None 17 Human Binding pKi = 5.8 5.8 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by Scatchard plot analysisDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by Scatchard plot analysis
ChEMBL 296 3 2 5 2.9 CC1=C(C(=O)OC(C)C)C(c2cccs2)NC(S)=N1 10.1021/ml400185v
CHEMBL1561375 49070 None 17 Human Binding pKi = 5.8 5.8 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by Scatchard plot analysisDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by Scatchard plot analysis
ChEMBL 296 3 2 5 2.9 CC1=C(C(=O)OC(C)C)C(c2cccs2)NC(S)=N1 10.1021/ml400185v
11676113 73394 None 0 Human Binding pKi = 6.8 6.8 2 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 419 8 2 6 3.1 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)O)cc3)c(Cl)c2n(CCC)c1=O 10.1021/jm0506221
CHEMBL201523 73394 None 0 Human Binding pKi = 6.8 6.8 2 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 419 8 2 6 3.1 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)O)cc3)c(Cl)c2n(CCC)c1=O 10.1021/jm0506221
25070230 202439 None 0 Human Binding pKi = 6.8 6.8 -15 4
Displacement of [3H]DPCPX from human A2B receptor expressed in HEK-293-A2B cells incubated for 30 mins by scintillation counting method based radioligand competitive binding assayDisplacement of [3H]DPCPX from human A2B receptor expressed in HEK-293-A2B cells incubated for 30 mins by scintillation counting method based radioligand competitive binding assay
ChEMBL 295 2 2 5 2.7 Oc1cccc(-c2nc(N3CCCCC3)c3nc[nH]c3n2)c1 10.1016/j.bmc.2019.06.034
CHEMBL611021 202439 None 0 Human Binding pKi = 6.8 6.8 -15 4
Displacement of [3H]DPCPX from human A2B receptor expressed in HEK-293-A2B cells incubated for 30 mins by scintillation counting method based radioligand competitive binding assayDisplacement of [3H]DPCPX from human A2B receptor expressed in HEK-293-A2B cells incubated for 30 mins by scintillation counting method based radioligand competitive binding assay
ChEMBL 295 2 2 5 2.7 Oc1cccc(-c2nc(N3CCCCC3)c3nc[nH]c3n2)c1 10.1016/j.bmc.2019.06.034
168288152 191830 None 0 Human Binding pKi = 6.8 6.8 - 1
Displacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cell membrane preincubated for 4 hrs followed by [3H]PSB-603 addition and measured after 0.5 hrs by radioligand displacement assayDisplacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cell membrane preincubated for 4 hrs followed by [3H]PSB-603 addition and measured after 0.5 hrs by radioligand displacement assay
ChEMBL 394 6 1 7 2.0 CCCn1c(=O)c2[nH]c(-c3cccc(S(=O)(=O)F)c3)nc2n(CCC)c1=O 10.1039/d2md00132b
CHEMBL5198830 191830 None 0 Human Binding pKi = 6.8 6.8 - 1
Displacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cell membrane preincubated for 4 hrs followed by [3H]PSB-603 addition and measured after 0.5 hrs by radioligand displacement assayDisplacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cell membrane preincubated for 4 hrs followed by [3H]PSB-603 addition and measured after 0.5 hrs by radioligand displacement assay
ChEMBL 394 6 1 7 2.0 CCCn1c(=O)c2[nH]c(-c3cccc(S(=O)(=O)F)c3)nc2n(CCC)c1=O 10.1039/d2md00132b
67364057 74289 None 0 Human Binding pKi = 6.8 6.8 -15 3
Inhibition of adenosine A2B receptorInhibition of adenosine A2B receptor
ChEMBL 295 2 1 5 2.9 Cc1cc(-c2nnc(N)nc2-c2ccc(F)cc2)cc(C)n1 10.1021/jm201376w
CHEMBL2024116 74289 None 0 Human Binding pKi = 6.8 6.8 -15 3
Inhibition of adenosine A2B receptorInhibition of adenosine A2B receptor
ChEMBL 295 2 1 5 2.9 Cc1cc(-c2nnc(N)nc2-c2ccc(F)cc2)cc(C)n1 10.1021/jm201376w
136086750 8721 None 0 Human Binding pKi = 5.8 5.8 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by beta scintillation countingDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by beta scintillation counting
ChEMBL 349 3 4 6 1.9 N=C1c2c(C(N)=O)nc(-c3ccccc3O)n2CN1c1ccc(O)cc1 10.1016/j.bmc.2010.03.048
CHEMBL1095872 8721 None 0 Human Binding pKi = 5.8 5.8 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by beta scintillation countingDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by beta scintillation counting
ChEMBL 349 3 4 6 1.9 N=C1c2c(C(N)=O)nc(-c3ccccc3O)n2CN1c1ccc(O)cc1 10.1016/j.bmc.2010.03.048
CHEMBL5071873 214270 None 0 Human Binding pKi = 5.8 5.8 -20 3
Displacement of [3H] DPCPX from human recombinant A2B adenosine receptor expressed in HEK293 cells incubated for 30 mins by radioligand binding competition assayDisplacement of [3H] DPCPX from human recombinant A2B adenosine receptor expressed in HEK293 cells incubated for 30 mins by radioligand binding competition assay
ChEMBL None None None Cn1cc(-c2cnc(N)n3nc(-c4nccs4)nc23)ccc1=O 10.1021/acsmedchemlett.1c00599
135489238 477 None 1 Human Binding pKi = 7.8 7.8 30 2
Binding affinity of compound for displacement of [3H]DPCPX binding in HEK293 membranes expressing human A2B adenosine receptorsBinding affinity of compound for displacement of [3H]DPCPX binding in HEK293 membranes expressing human A2B adenosine receptors
ChEMBL 533 9 2 9 3.4 CCCn1c2[nH]c(nc2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)Nc1ccc(c(c1)Cl)Cl 10.1021/jm0309654
381 477 None 1 Human Binding pKi = 7.8 7.8 30 2
Binding affinity of compound for displacement of [3H]DPCPX binding in HEK293 membranes expressing human A2B adenosine receptorsBinding affinity of compound for displacement of [3H]DPCPX binding in HEK293 membranes expressing human A2B adenosine receptors
ChEMBL 533 9 2 9 3.4 CCCn1c2[nH]c(nc2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)Nc1ccc(c(c1)Cl)Cl 10.1021/jm0309654
CHEMBL32802 477 None 1 Human Binding pKi = 7.8 7.8 30 2
Binding affinity of compound for displacement of [3H]DPCPX binding in HEK293 membranes expressing human A2B adenosine receptorsBinding affinity of compound for displacement of [3H]DPCPX binding in HEK293 membranes expressing human A2B adenosine receptors
ChEMBL 533 9 2 9 3.4 CCCn1c2[nH]c(nc2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)Nc1ccc(c(c1)Cl)Cl 10.1021/jm0309654
135489238 477 None 1 Human Binding pKi = 7.8 7.8 30 2
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 533 9 2 9 3.4 CCCn1c2[nH]c(nc2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)Nc1ccc(c(c1)Cl)Cl 10.1021/jm0309654
381 477 None 1 Human Binding pKi = 7.8 7.8 30 2
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 533 9 2 9 3.4 CCCn1c2[nH]c(nc2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)Nc1ccc(c(c1)Cl)Cl 10.1021/jm0309654
CHEMBL32802 477 None 1 Human Binding pKi = 7.8 7.8 30 2
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 533 9 2 9 3.4 CCCn1c2[nH]c(nc2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)Nc1ccc(c(c1)Cl)Cl 10.1021/jm0309654
66892244 158932 None 0 Human Binding pKi = 7.8 7.8 32 3
Displacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting methodDisplacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting method
ChEMBL 491 8 1 9 2.2 CCCn1c(=O)c2[nH]c(-c3cnn(CC4CC(=O)N(c5ccc(OC)cc5)C4)c3)nc2n(CC)c1=O 10.1016/j.ejmech.2016.11.007
CHEMBL4095686 158932 None 0 Human Binding pKi = 7.8 7.8 32 3
Displacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting methodDisplacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting method
ChEMBL 491 8 1 9 2.2 CCCn1c(=O)c2[nH]c(-c3cnn(CC4CC(=O)N(c5ccc(OC)cc5)C4)c3)nc2n(CC)c1=O 10.1016/j.ejmech.2016.11.007
11544506 85383 None 0 Human Binding pKi = 7.8 7.8 - 1
Displacement of [3H]DPCPX from human A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human A2B receptor expressed in HEK293 cells
ChEMBL 332 4 2 7 2.6 O=c1ccc(Nc2ncc(-c3ccncn3)c(-c3ccco3)n2)c[nH]1 10.1021/jm061333v
CHEMBL226238 85383 None 0 Human Binding pKi = 7.8 7.8 - 1
Displacement of [3H]DPCPX from human A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human A2B receptor expressed in HEK293 cells
ChEMBL 332 4 2 7 2.6 O=c1ccc(Nc2ncc(-c3ccncn3)c(-c3ccco3)n2)c[nH]1 10.1021/jm061333v
24827555 166428 None 0 Human Binding pKi = 7.8 7.8 25 4
Displacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 445 5 1 8 2.6 CCn1c(=O)n(CC2CC2)c(=O)c2[nH]c(-c3cnn(-c4ccc(C(F)(F)F)nc4)c3)nc21 10.1021/jm7014815
CHEMBL427736 166428 None 0 Human Binding pKi = 7.8 7.8 25 4
Displacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 445 5 1 8 2.6 CCn1c(=O)n(CC2CC2)c(=O)c2[nH]c(-c3cnn(-c4ccc(C(F)(F)F)nc4)c3)nc21 10.1021/jm7014815
11306173 166625 None 0 Human Binding pKi = 7.8 7.8 26 4
Displacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 480 7 1 10 2.9 CCCn1c(=O)c2[nH]c(-c3cnn(Cc4nc(-c5ccc(Cl)cc5)no4)c3)nc2n(CC)c1=O 10.1021/jm7014815
CHEMBL428086 166625 None 0 Human Binding pKi = 7.8 7.8 26 4
Displacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 480 7 1 10 2.9 CCCn1c(=O)c2[nH]c(-c3cnn(Cc4nc(-c5ccc(Cl)cc5)no4)c3)nc2n(CC)c1=O 10.1021/jm7014815
44574193 189250 None 0 Human Binding pKi = 7.8 7.8 61 2
Displacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells by beta scintillation counterDisplacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells by beta scintillation counter
ChEMBL 418 5 2 6 2.7 Cn1c(=O)c2[nH]c(-c3ccc(COC(=O)NCc4ccccc4)cc3)cc2n(C)c1=O 10.1016/j.bmc.2009.03.062
CHEMBL511714 189250 None 0 Human Binding pKi = 7.8 7.8 61 2
Displacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells by beta scintillation counterDisplacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells by beta scintillation counter
ChEMBL 418 5 2 6 2.7 Cn1c(=O)c2[nH]c(-c3ccc(COC(=O)NCc4ccccc4)cc3)cc2n(C)c1=O 10.1016/j.bmc.2009.03.062
11713561 72669 None 0 Human Binding pKi = 7.8 7.8 4 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 536 10 2 6 5.7 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(-c5ccccc5)cc4)cc3)cc2n(CCC)c1=O 10.1021/jm0506221
CHEMBL199583 72669 None 0 Human Binding pKi = 7.8 7.8 4 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 536 10 2 6 5.7 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(-c5ccccc5)cc4)cc3)cc2n(CCC)c1=O 10.1021/jm0506221
2690 903 None 66 Human Binding pKi = 7.8 7.8 -30 9
Displacement of [125I]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [125I]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 285 1 1 6 2.8 Clc1ccc2c(c1)c1nc(nn1c(n2)N)c1ccco1 10.1021/jm900413e
384 903 None 66 Human Binding pKi = 7.8 7.8 -30 9
Displacement of [125I]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [125I]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 285 1 1 6 2.8 Clc1ccc2c(c1)c1nc(nn1c(n2)N)c1ccco1 10.1021/jm900413e
CHEMBL16687 903 None 66 Human Binding pKi = 7.8 7.8 -30 9
Displacement of [125I]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [125I]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 285 1 1 6 2.8 Clc1ccc2c(c1)c1nc(nn1c(n2)N)c1ccco1 10.1021/jm900413e
CHEMBL5084815 214936 None 0 Human Binding pKi = 7.8 7.8 1 2
Displacement of [3H]DPCPX from human A2BAR expressed in HEK293 cell membrane incubated for 30 mins by microbeta trilux scintillation counter analysisDisplacement of [3H]DPCPX from human A2BAR expressed in HEK293 cell membrane incubated for 30 mins by microbeta trilux scintillation counter analysis
ChEMBL None None None N#Cc1cccc(-c2nc(Nc3ccccc3)nc(-c3ccccc3)c2C#N)c1 10.1021/acs.jmedchem.1c01636
50941005 57280 None 0 Human Binding pKi = 7.8 7.8 -2 4
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 297 5 1 5 3.7 CCCC(=O)Nc1cc(-c2ccco2)nc(-c2ccco2)n1 10.1021/jm100843z
CHEMBL1650386 57280 None 0 Human Binding pKi = 7.8 7.8 -2 4
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 297 5 1 5 3.7 CCCC(=O)Nc1cc(-c2ccco2)nc(-c2ccco2)n1 10.1021/jm100843z
11524904 73352 None 0 Human Binding pKi = 7.8 7.8 2 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 436 6 2 6 2.1 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)NCc4ccc(F)cc4)cc3)cc2n(C)c1=O 10.1021/jm0506221
CHEMBL201323 73352 None 0 Human Binding pKi = 7.8 7.8 2 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 436 6 2 6 2.1 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)NCc4ccc(F)cc4)cc3)cc2n(C)c1=O 10.1021/jm0506221
11576014 133007 None 0 Human Binding pKi = 7.8 7.8 1 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 450 8 2 9 2.5 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)n4ccc(N)n4)cc3)cc2n(CCC)c1=O 10.1021/jm0506221
CHEMBL370205 133007 None 0 Human Binding pKi = 7.8 7.8 1 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 450 8 2 9 2.5 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)n4ccc(N)n4)cc3)cc2n(CCC)c1=O 10.1021/jm0506221
44451227 96385 None 0 Human Binding pKi = 7.8 7.8 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 532 10 1 8 2.4 COCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCc5ccccc5C4)cc3)cc2n(CCOC)c1=O 10.1016/j.bmc.2008.01.002
CHEMBL261790 96385 None 0 Human Binding pKi = 7.8 7.8 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 532 10 1 8 2.4 COCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCc5ccccc5C4)cc3)cc2n(CCOC)c1=O 10.1016/j.bmc.2008.01.002
135493280 110378 None 0 Human Binding pKi = 6.8 6.8 28 2
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 483 8 2 8 2.9 CCCn1c(=O)c2nc(-c3cc(NC(=O)Cc4cccc(Cl)c4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
CHEMBL32425 110378 None 0 Human Binding pKi = 6.8 6.8 28 2
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 483 8 2 8 2.9 CCCn1c(=O)c2nc(-c3cc(NC(=O)Cc4cccc(Cl)c4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
9945226 176979 None 0 Human Binding pKi = 6.8 6.8 -69 4
Displacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation countingDisplacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation counting
ChEMBL 326 3 1 7 2.8 Nc1nc(-c2ccco2)c2nnn(Cc3cccc(Cl)c3)c2n1 10.1021/jm800961g
CHEMBL462488 176979 None 0 Human Binding pKi = 6.8 6.8 -69 4
Displacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation countingDisplacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation counting
ChEMBL 326 3 1 7 2.8 Nc1nc(-c2ccco2)c2nnn(Cc3cccc(Cl)c3)c2n1 10.1021/jm800961g
10971099 57300 None 0 Human Binding pKi = 6.8 6.8 -5 4
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells (95% confidence limits)Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells (95% confidence limits)
ChEMBL 387 5 1 8 2.9 CCn1cc2c(nc(NC(=O)Cc3ccccc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm0109614
CHEMBL165073 57300 None 0 Human Binding pKi = 6.8 6.8 -5 4
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells (95% confidence limits)Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells (95% confidence limits)
ChEMBL 387 5 1 8 2.9 CCn1cc2c(nc(NC(=O)Cc3ccccc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm0109614
11732736 57579 None 0 Human Binding pKi = 6.8 6.8 -24 4
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 127-203Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 127-203
ChEMBL 430 6 2 8 4.5 CCCCn1cc2c(nc(NC(=O)Nc3ccc(C)cc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm0109614
CHEMBL166684 57579 None 0 Human Binding pKi = 6.8 6.8 -24 4
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 127-203Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 127-203
ChEMBL 430 6 2 8 4.5 CCCCn1cc2c(nc(NC(=O)Nc3ccc(C)cc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm0109614
10971841 57475 None 0 Human Binding pKi = 6.8 6.8 -17 4
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 140-186Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 140-186
ChEMBL 420 5 2 8 3.9 CCCn1cc2c(nc(NC(=O)Nc3ccc(F)cc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm0109614
CHEMBL165778 57475 None 0 Human Binding pKi = 6.8 6.8 -17 4
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 140-186Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 140-186
ChEMBL 420 5 2 8 3.9 CCCn1cc2c(nc(NC(=O)Nc3ccc(F)cc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm0109614
46227994 199833 None 0 Human Binding pKi = 6.8 6.8 6 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 350 5 1 6 2.1 CCn1c(=O)c2[nH]c(Cc3ccccc3)nc2n(Cc2ccco2)c1=O 10.1016/j.bmc.2009.07.034
CHEMBL594255 199833 None 0 Human Binding pKi = 6.8 6.8 6 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 350 5 1 6 2.1 CCn1c(=O)c2[nH]c(Cc3ccccc3)nc2n(Cc2ccco2)c1=O 10.1016/j.bmc.2009.07.034
12905388 91769 None 2 Human Binding pKi = 5.8 5.8 3 5
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 194 1 1 5 -0.6 CCn1c(=O)c2nc[nH]c2n(C)c1=O 10.1021/jm0104318
CHEMBL24107 91769 None 2 Human Binding pKi = 5.8 5.8 3 5
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 194 1 1 5 -0.6 CCn1c(=O)c2nc[nH]c2n(C)c1=O 10.1021/jm0104318
135493285 99772 None 0 Human Binding pKi = 5.8 5.8 - 1
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 492 9 2 9 2.4 CCCn1c(=O)c2nc(-c3cc(NC(=O)Cc4ccc(N(C)C)cc4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
CHEMBL285151 99772 None 0 Human Binding pKi = 5.8 5.8 - 1
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 492 9 2 9 2.4 CCCn1c(=O)c2nc(-c3cc(NC(=O)Cc4ccc(N(C)C)cc4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
22282339 83104 None 3 Rat Binding pKi = 6.8 6.8 -234 15
Displacement of [3H] DPCPX from rat adenosine A2B receptor expressed in HEK293 cells incubated for 60 mins by radioligand binding assayDisplacement of [3H] DPCPX from rat adenosine A2B receptor expressed in HEK293 cells incubated for 60 mins by radioligand binding assay
ChEMBL 386 4 1 5 5.1 Cc1cc(C)cc(-c2nc(NC(=O)c3cccnc3)sc2-c2ccncc2)c1 10.1021/acsmedchemlett.1c00685
CHEMBL2181976 83104 None 3 Rat Binding pKi = 6.8 6.8 -234 15
Displacement of [3H] DPCPX from rat adenosine A2B receptor expressed in HEK293 cells incubated for 60 mins by radioligand binding assayDisplacement of [3H] DPCPX from rat adenosine A2B receptor expressed in HEK293 cells incubated for 60 mins by radioligand binding assay
ChEMBL 386 4 1 5 5.1 Cc1cc(C)cc(-c2nc(NC(=O)c3cccnc3)sc2-c2ccncc2)c1 10.1021/acsmedchemlett.1c00685
CHEMBL5084951 83104 None 3 Rat Binding pKi = 6.8 6.8 -234 15
Displacement of [3H] DPCPX from rat adenosine A2B receptor expressed in HEK293 cells incubated for 60 mins by radioligand binding assayDisplacement of [3H] DPCPX from rat adenosine A2B receptor expressed in HEK293 cells incubated for 60 mins by radioligand binding assay
ChEMBL 386 4 1 5 5.1 Cc1cc(C)cc(-c2nc(NC(=O)c3cccnc3)sc2-c2ccncc2)c1 10.1021/acsmedchemlett.1c00685
44406397 72905 None 0 Human Binding pKi = 6.8 6.8 26 3
Displacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cellsDisplacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cells
ChEMBL 493 8 1 9 3.9 CCCn1c(=O)c2nc(-c3cnn(Cc4cc(-c5cccc(Cl)c5)on4)c3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2005.10.002
CHEMBL200417 72905 None 0 Human Binding pKi = 6.8 6.8 26 3
Displacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cellsDisplacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cells
ChEMBL 493 8 1 9 3.9 CCCn1c(=O)c2nc(-c3cnn(Cc4cc(-c5cccc(Cl)c5)on4)c3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2005.10.002
9857422 188811 None 0 Human Binding pKi = 6.8 6.8 -85 4
Displacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation countingDisplacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation counting
ChEMBL 298 3 1 8 2.2 Nc1nc(-c2ccco2)c2nnn(Cc3ccsc3)c2n1 10.1021/jm800961g
CHEMBL506101 188811 None 0 Human Binding pKi = 6.8 6.8 -85 4
Displacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation countingDisplacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation counting
ChEMBL 298 3 1 8 2.2 Nc1nc(-c2ccco2)c2nnn(Cc3ccsc3)c2n1 10.1021/jm800961g
50940981 57288 None 0 Human Binding pKi = 6.8 6.8 -4 4
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 315 4 1 5 4.3 CCC(=O)Nc1cc(-c2ccsc2)nc(-c2ccsc2)n1 10.1021/jm100843z
CHEMBL1650394 57288 None 0 Human Binding pKi = 6.8 6.8 -4 4
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 315 4 1 5 4.3 CCC(=O)Nc1cc(-c2ccsc2)nc(-c2ccsc2)n1 10.1021/jm100843z
10928182 57452 None 0 Human Binding pKi = 6.8 6.8 -15 4
Displacement of [3H]-DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 125-218Displacement of [3H]-DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 125-218
ChEMBL 432 6 2 9 3.8 CCCn1cc2c(nc(NC(=O)Nc3ccccc3OC)n3nc(-c4ccco4)nc23)n1 10.1021/jm0109614
CHEMBL165560 57452 None 0 Human Binding pKi = 6.8 6.8 -15 4
Displacement of [3H]-DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 125-218Displacement of [3H]-DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 125-218
ChEMBL 432 6 2 9 3.8 CCCn1cc2c(nc(NC(=O)Nc3ccccc3OC)n3nc(-c4ccco4)nc23)n1 10.1021/jm0109614
11014188 118483 None 0 Human Binding pKi = 6.8 6.8 -6 4
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells
ChEMBL 373 4 1 8 2.5 Cn1cc2c(nc(NC(=O)Cc3ccccc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm0109614
CHEMBL341376 118483 None 0 Human Binding pKi = 6.8 6.8 -6 4
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells
ChEMBL 373 4 1 8 2.5 Cn1cc2c(nc(NC(=O)Cc3ccccc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm0109614
11014188 118483 None 0 Human Binding pKi = 6.8 6.8 -6 4
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 373 4 1 8 2.5 Cn1cc2c(nc(NC(=O)Cc3ccccc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm030852k
CHEMBL341376 118483 None 0 Human Binding pKi = 6.8 6.8 -6 4
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 373 4 1 8 2.5 Cn1cc2c(nc(NC(=O)Cc3ccccc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm030852k
11524240 72598 None 0 Human Binding pKi = 6.8 6.8 1 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 404 5 2 6 2.3 Cn1c(=O)c2[nH]c(-c3cccc(OCC(=O)Nc4ccccc4)c3)cc2n(C)c1=O 10.1021/jm0506221
CHEMBL199330 72598 None 0 Human Binding pKi = 6.8 6.8 1 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 404 5 2 6 2.3 Cn1c(=O)c2[nH]c(-c3cccc(OCC(=O)Nc4ccccc4)c3)cc2n(C)c1=O 10.1021/jm0506221
15578102 173229 None 0 Human Binding pKi = 5.8 5.8 - 1
Displacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cells
ChEMBL 271 1 1 6 0.9 Cn1c(=O)c2c(cc(-c3ccccc3)n2O)n(C)c1=O 10.1016/j.bmc.2008.09.067
CHEMBL452359 173229 None 0 Human Binding pKi = 5.8 5.8 - 1
Displacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cells
ChEMBL 271 1 1 6 0.9 Cn1c(=O)c2c(cc(-c3ccccc3)n2O)n(C)c1=O 10.1016/j.bmc.2008.09.067
50940976 57274 None 0 Human Binding pKi = 5.8 5.8 -316 4
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 391 4 1 7 3.6 CCC(=O)Nc1cc(-c2ccc3c(c2)OCO3)nc(-c2ccc3c(c2)OCO3)n1 10.1021/jm100843z
CHEMBL1650380 57274 None 0 Human Binding pKi = 5.8 5.8 -316 4
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 391 4 1 7 3.6 CCC(=O)Nc1cc(-c2ccc3c(c2)OCO3)nc(-c2ccc3c(c2)OCO3)n1 10.1021/jm100843z
10052252 96631 None 0 Human Binding pKi = 5.8 5.8 - 1
Binding affinity for adenosine A2b receptor by using as [3H]ZM-241385 (14 nM) radioligand in membranes from HEK-A2B cellsBinding affinity for adenosine A2b receptor by using as [3H]ZM-241385 (14 nM) radioligand in membranes from HEK-A2B cells
ChEMBL 516 10 1 10 4.0 CCCn1c(=O)c2nc(-c3ccc(OCc4nc(-c5cccc(OC)c5)no4)cc3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2004.11.044
CHEMBL263494 96631 None 0 Human Binding pKi = 5.8 5.8 - 1
Binding affinity for adenosine A2b receptor by using as [3H]ZM-241385 (14 nM) radioligand in membranes from HEK-A2B cellsBinding affinity for adenosine A2b receptor by using as [3H]ZM-241385 (14 nM) radioligand in membranes from HEK-A2B cells
ChEMBL 516 10 1 10 4.0 CCCn1c(=O)c2nc(-c3ccc(OCc4nc(-c5cccc(OC)c5)no4)cc3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2004.11.044
44451197 95890 None 0 Human Binding pKi = 6.8 6.8 39 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 474 5 1 7 2.2 COc1cc(-c2cc3c([nH]2)c(=O)n(C)c(=O)n3C)ccc1OCC(=O)N1CCc2ccccc2C1 10.1016/j.bmc.2008.01.002
CHEMBL259155 95890 None 0 Human Binding pKi = 6.8 6.8 39 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 474 5 1 7 2.2 COc1cc(-c2cc3c([nH]2)c(=O)n(C)c(=O)n3C)ccc1OCC(=O)N1CCc2ccccc2C1 10.1016/j.bmc.2008.01.002
11716665 2281 None 37 Human Binding pKi = 7.8 7.8 58 4
Displacement of [3H]DPCPX from human A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human A2B receptor expressed in HEK293 cells
ChEMBL 316 4 1 7 3.3 n1ccc(nc1)c1cnc(nc1c1ccco1)Nc1cccnc1 10.1021/jm061333v
5617 2281 None 37 Human Binding pKi = 7.8 7.8 58 4
Displacement of [3H]DPCPX from human A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human A2B receptor expressed in HEK293 cells
ChEMBL 316 4 1 7 3.3 n1ccc(nc1)c1cnc(nc1c1ccco1)Nc1cccnc1 10.1021/jm061333v
CHEMBL375293 2281 None 37 Human Binding pKi = 7.8 7.8 58 4
Displacement of [3H]DPCPX from human A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human A2B receptor expressed in HEK293 cells
ChEMBL 316 4 1 7 3.3 n1ccc(nc1)c1cnc(nc1c1ccco1)Nc1cccnc1 10.1021/jm061333v
11716665 2281 None 37 Human Binding pKi = 7.8 7.8 58 4
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 316 4 1 7 3.3 n1ccc(nc1)c1cnc(nc1c1ccco1)Nc1cccnc1 10.1016/j.bmcl.2010.01.045
5617 2281 None 37 Human Binding pKi = 7.8 7.8 58 4
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 316 4 1 7 3.3 n1ccc(nc1)c1cnc(nc1c1ccco1)Nc1cccnc1 10.1016/j.bmcl.2010.01.045
CHEMBL375293 2281 None 37 Human Binding pKi = 7.8 7.8 58 4
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 316 4 1 7 3.3 n1ccc(nc1)c1cnc(nc1c1ccco1)Nc1cccnc1 10.1016/j.bmcl.2010.01.045
155533829 171882 None 0 Human Binding pKi = 7.8 7.8 - 1
Displacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assayDisplacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assay
ChEMBL 391 3 1 6 4.4 CC1=C(C(=O)O[C@H](C)C(F)(F)F)C(c2ccco2)n2c(nc3ccccc32)N1 10.1021/acs.jmedchem.9b01340
CHEMBL4469484 171882 None 0 Human Binding pKi = 7.8 7.8 - 1
Displacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assayDisplacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assay
ChEMBL 391 3 1 6 4.4 CC1=C(C(=O)O[C@H](C)C(F)(F)F)C(c2ccco2)n2c(nc3ccccc32)N1 10.1021/acs.jmedchem.9b01340
11678808 73038 None 0 Human Binding pKi = 7.8 7.8 16 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 600 11 2 8 4.8 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(S(=O)(=O)c5ccccc5)cc4)cc3)cc2n(CCC)c1=O 10.1021/jm0506221
CHEMBL201042 73038 None 0 Human Binding pKi = 7.8 7.8 16 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 600 11 2 8 4.8 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(S(=O)(=O)c5ccccc5)cc4)cc3)cc2n(CCC)c1=O 10.1021/jm0506221
66894039 156557 None 0 Human Binding pKi = 7.8 7.8 - 1
Displacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting methodDisplacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting method
ChEMBL 545 8 1 9 3.1 CCCn1c(=O)c2[nH]c(-c3cnn(CC4CC(=O)N(c5cccc(OC(F)(F)F)c5)C4)c3)nc2n(CC)c1=O 10.1016/j.ejmech.2016.11.007
CHEMBL4068331 156557 None 0 Human Binding pKi = 7.8 7.8 - 1
Displacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting methodDisplacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting method
ChEMBL 545 8 1 9 3.1 CCCn1c(=O)c2[nH]c(-c3cnn(CC4CC(=O)N(c5cccc(OC(F)(F)F)c5)C4)c3)nc2n(CC)c1=O 10.1016/j.ejmech.2016.11.007
44236657 156335 None 0 Human Binding pKi = 7.8 7.8 - 1
Displacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 minsDisplacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 mins
ChEMBL 460 7 2 8 2.3 CCCn1c(=O)c2[nH]c(-c3cnn(CC#Cc4ccc(C(=O)O)cc4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2017.04.014
CHEMBL4065780 156335 None 0 Human Binding pKi = 7.8 7.8 - 1
Displacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 minsDisplacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 mins
ChEMBL 460 7 2 8 2.3 CCCn1c(=O)c2[nH]c(-c3cnn(CC#Cc4ccc(C(=O)O)cc4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2017.04.014
22266759 94566 None 0 Human Binding pKi = 6.8 6.8 - 1
Displacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranesDisplacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranes
ChEMBL 451 6 2 8 3.0 CCCn1c(=O)[nH]c2nc(-c3cnn(Cc4cc(-c5ccc(Cl)cc5)on4)c3)[nH]c2c1=O 10.1016/j.bmcl.2008.01.008
CHEMBL251879 94566 None 0 Human Binding pKi = 6.8 6.8 - 1
Displacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranesDisplacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranes
ChEMBL 451 6 2 8 3.0 CCCn1c(=O)[nH]c2nc(-c3cnn(Cc4cc(-c5ccc(Cl)cc5)on4)c3)[nH]c2c1=O 10.1016/j.bmcl.2008.01.008
24950370 178718 None 0 Human Binding pKi = 6.8 6.8 -15 3
Displacement of [3H]MRS1754 from human adenosine A2B receptor expressed in CHO cell membraneDisplacement of [3H]MRS1754 from human adenosine A2B receptor expressed in CHO cell membrane
ChEMBL 261 2 1 4 3.5 N#Cc1c(-c2ccccc2)cc(-c2ccco2)nc1N 10.1021/jm701594y
CHEMBL468370 178718 None 0 Human Binding pKi = 6.8 6.8 -15 3
Displacement of [3H]MRS1754 from human adenosine A2B receptor expressed in CHO cell membraneDisplacement of [3H]MRS1754 from human adenosine A2B receptor expressed in CHO cell membrane
ChEMBL 261 2 1 4 3.5 N#Cc1c(-c2ccccc2)cc(-c2ccco2)nc1N 10.1021/jm701594y
11067937 203621 None 0 Rat Binding pKi = 5.8 5.8 -5 3
Inhibition of [125I]-APOBX binding to rat Adenosine A2B receptor expressed in HEK cellsInhibition of [125I]-APOBX binding to rat Adenosine A2B receptor expressed in HEK cells
ChEMBL 344 5 0 6 2.0 C=CCn1c(=O)c2c(nc(-c3ccccc3)n2CCCl)n(C)c1=O 10.1021/jm0104318
CHEMBL67110 203621 None 0 Rat Binding pKi = 5.8 5.8 -5 3
Inhibition of [125I]-APOBX binding to rat Adenosine A2B receptor expressed in HEK cellsInhibition of [125I]-APOBX binding to rat Adenosine A2B receptor expressed in HEK cells
ChEMBL 344 5 0 6 2.0 C=CCn1c(=O)c2c(nc(-c3ccccc3)n2CCCl)n(C)c1=O 10.1021/jm0104318
9798466 134278 None 1 Rat Binding pKi = 5.8 5.8 -218 6
In vivo binding affinity was evaluated against Alpha-2 adrenergic receptorIn vivo binding affinity was evaluated against Alpha-2 adrenergic receptor
ChEMBL 349 4 1 3 3.3 Cc1ccc(N2CCN(CC[C@@H]3NC(=O)c4ccccc43)CC2)cc1C 10.1016/s0960-894x(98)00252-2
CHEMBL37170 134278 None 1 Rat Binding pKi = 5.8 5.8 -218 6
In vivo binding affinity was evaluated against Alpha-2 adrenergic receptorIn vivo binding affinity was evaluated against Alpha-2 adrenergic receptor
ChEMBL 349 4 1 3 3.3 Cc1ccc(N2CCN(CC[C@@H]3NC(=O)c4ccccc43)CC2)cc1C 10.1016/s0960-894x(98)00252-2
72697932 104027 None 0 Human Binding pKi = 4.8 4.8 -54 5
Displacement of [3H]PSB-603 from human adenosine A2B receptorDisplacement of [3H]PSB-603 from human adenosine A2B receptor
ChEMBL 341 2 0 7 1.1 C#CCn1c(=O)c2c(nc3n2CCCN3C2CCCCC2)n(C)c1=O 10.1016/j.bmc.2013.09.044
CHEMBL3093321 104027 None 0 Human Binding pKi = 4.8 4.8 -54 5
Displacement of [3H]PSB-603 from human adenosine A2B receptorDisplacement of [3H]PSB-603 from human adenosine A2B receptor
ChEMBL 341 2 0 7 1.1 C#CCn1c(=O)c2c(nc3n2CCCN3C2CCCCC2)n(C)c1=O 10.1016/j.bmc.2013.09.044
9824812 121142 None 0 Human Binding pKi = 5.8 5.8 -67 4
Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 1531-1920Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 1531-1920
ChEMBL 446 4 2 9 4.1 COc1ccc(NC(=O)Nc2nc3nn(C(C)(C)C)cc3c3nc(-c4ccco4)nn23)cc1 10.1021/jm001047y
CHEMBL357663 121142 None 0 Human Binding pKi = 5.8 5.8 -67 4
Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 1531-1920Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 1531-1920
ChEMBL 446 4 2 9 4.1 COc1ccc(NC(=O)Nc2nc3nn(C(C)(C)C)cc3c3nc(-c4ccco4)nn23)cc1 10.1021/jm001047y
22446266 203589 None 2 Human Binding pKi = 5.8 5.8 1 2
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 236 4 1 5 0.7 CCCCn1c(=O)c2nc[nH]c2n(CC)c1=O 10.1021/jm0104318
CHEMBL66881 203589 None 2 Human Binding pKi = 5.8 5.8 1 2
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 236 4 1 5 0.7 CCCCn1c(=O)c2nc[nH]c2n(CC)c1=O 10.1021/jm0104318
45273118 196471 None 0 Human Binding pKi = 6.8 6.8 1 4
Binding affinity to human adenosine A2b receptor expressed in HEK293 cellsBinding affinity to human adenosine A2b receptor expressed in HEK293 cells
ChEMBL 520 11 2 9 2.7 CCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(N(C)C)cc4)cc3)nc2n(CCCOC)c1=O 10.1016/j.bmc.2009.03.029
CHEMBL563259 196471 None 0 Human Binding pKi = 6.8 6.8 1 4
Binding affinity to human adenosine A2b receptor expressed in HEK293 cellsBinding affinity to human adenosine A2b receptor expressed in HEK293 cells
ChEMBL 520 11 2 9 2.7 CCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(N(C)C)cc4)cc3)nc2n(CCCOC)c1=O 10.1016/j.bmc.2009.03.029
11685118 73028 None 0 Human Binding pKi = 6.8 6.8 -3 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 526 10 2 6 4.5 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)NCc4ccc(F)cc4)cc3)c(Cl)c2n(CCC)c1=O 10.1021/jm0506221
CHEMBL201006 73028 None 0 Human Binding pKi = 6.8 6.8 -3 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 526 10 2 6 4.5 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)NCc4ccc(F)cc4)cc3)c(Cl)c2n(CCC)c1=O 10.1021/jm0506221
44451106 166383 None 0 Human Binding pKi = 6.8 6.8 4 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 411 4 1 7 0.4 CN1CCN(C(=O)COc2ccc(-c3cc4c([nH]3)c(=O)n(C)c(=O)n4C)cc2)CC1 10.1016/j.bmc.2008.01.002
CHEMBL427602 166383 None 0 Human Binding pKi = 6.8 6.8 4 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 411 4 1 7 0.4 CN1CCN(C(=O)COc2ccc(-c3cc4c([nH]3)c(=O)n(C)c(=O)n4C)cc2)CC1 10.1016/j.bmc.2008.01.002
1892 204045 None 78 Human Binding pKi = 4.8 4.8 34 3
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 224 2 1 7 -1.6 Cn1c(=O)c2c(ncn2CCO)n(C)c1=O 10.1021/jm0104318
CHEMBL699 204045 None 78 Human Binding pKi = 4.8 4.8 34 3
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 224 2 1 7 -1.6 Cn1c(=O)c2c(ncn2CCO)n(C)c1=O 10.1021/jm0104318
44452695 159562 None 0 Human Binding pKi = 5.8 5.8 -52 3
Displacement of [3]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 331 4 1 7 3.7 c1coc(CNc2nc3ccccc3n3nc(-c4ccco4)nc23)c1 10.1016/j.bmc.2007.10.103
CHEMBL410264 159562 None 0 Human Binding pKi = 5.8 5.8 -52 3
Displacement of [3]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 331 4 1 7 3.7 c1coc(CNc2nc3ccccc3n3nc(-c4ccco4)nc23)c1 10.1016/j.bmc.2007.10.103
10379032 7521 None 0 Rat Binding pKi = 6.8 6.8 -4 4
Inhibition of [125I]-APOBX binding to rat Adenosine A2B receptor expressed in HEK cellsInhibition of [125I]-APOBX binding to rat Adenosine A2B receptor expressed in HEK cells
ChEMBL 282 3 1 5 1.3 C=CCn1c(=O)c2[nH]c(-c3ccccc3)nc2n(C)c1=O 10.1021/jm0104318
CHEMBL10873 7521 None 0 Rat Binding pKi = 6.8 6.8 -4 4
Inhibition of [125I]-APOBX binding to rat Adenosine A2B receptor expressed in HEK cellsInhibition of [125I]-APOBX binding to rat Adenosine A2B receptor expressed in HEK cells
ChEMBL 282 3 1 5 1.3 C=CCn1c(=O)c2[nH]c(-c3ccccc3)nc2n(C)c1=O 10.1021/jm0104318
72697789 104021 None 0 Human Binding pKi = 5.8 5.8 -15 5
Displacement of [3H]PSB-603 from human adenosine A2B receptorDisplacement of [3H]PSB-603 from human adenosine A2B receptor
ChEMBL 355 3 0 8 1.0 C#CCn1c(=O)c2c(nc3n2CCCN3Cc2cccs2)n(C)c1=O 10.1016/j.bmc.2013.09.044
CHEMBL3093315 104021 None 0 Human Binding pKi = 5.8 5.8 -15 5
Displacement of [3H]PSB-603 from human adenosine A2B receptorDisplacement of [3H]PSB-603 from human adenosine A2B receptor
ChEMBL 355 3 0 8 1.0 C#CCn1c(=O)c2c(nc3n2CCCN3Cc2cccs2)n(C)c1=O 10.1016/j.bmc.2013.09.044
136002187 108831 None 0 Human Binding pKi = 6.8 6.8 - 1
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 275 1 2 8 -1.1 Cn1nc(-c2nc3c(=O)n(C)c(=O)n(C)c3[nH]2)cc1N 10.1021/jm0309654
CHEMBL32098 108831 None 0 Human Binding pKi = 6.8 6.8 - 1
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 275 1 2 8 -1.1 Cn1nc(-c2nc3c(=O)n(C)c(=O)n(C)c3[nH]2)cc1N 10.1021/jm0309654
156014066 177255 None 0 Human Binding pKi = 6.8 6.8 - 1
Displacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting methodDisplacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting method
ChEMBL 354 3 1 7 3.7 CC1=C(C(=O)OC(C)C)C(c2ccns2)n2c(nc3ccccc32)N1 10.1021/acs.jmedchem.0c00564
CHEMBL4636018 177255 None 0 Human Binding pKi = 6.8 6.8 - 1
Displacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting methodDisplacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting method
ChEMBL 354 3 1 7 3.7 CC1=C(C(=O)OC(C)C)C(c2ccns2)n2c(nc3ccccc32)N1 10.1021/acs.jmedchem.0c00564
11133804 120025 None 0 Human Binding pKi = 6.8 6.8 -13 4
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 149-204Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 149-204
ChEMBL 432 6 2 9 3.8 CCCn1cc2c(nc(NC(=O)Nc3cccc(OC)c3)n3nc(-c4ccco4)nc23)n1 10.1021/jm0109614
CHEMBL350261 120025 None 0 Human Binding pKi = 6.8 6.8 -13 4
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 149-204Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 149-204
ChEMBL 432 6 2 9 3.8 CCCn1cc2c(nc(NC(=O)Nc3cccc(OC)c3)n3nc(-c4ccco4)nc23)n1 10.1021/jm0109614
3645619 3034 None 20 Rat Binding pKi = 6.8 6.8 -112 9
Binding affinity at Alpha-2 adrenergic receptorBinding affinity at Alpha-2 adrenergic receptor
ChEMBL 334 4 1 4 2.4 N#Cc1ccccc1N1CCN(CC1)CNC(=O)c1cccc(c1)C 10.1021/jm970021c
975 3034 None 20 Rat Binding pKi = 6.8 6.8 -112 9
Binding affinity at Alpha-2 adrenergic receptorBinding affinity at Alpha-2 adrenergic receptor
ChEMBL 334 4 1 4 2.4 N#Cc1ccccc1N1CCN(CC1)CNC(=O)c1cccc(c1)C 10.1021/jm970021c
CHEMBL45244 3034 None 20 Rat Binding pKi = 6.8 6.8 -112 9
Binding affinity at Alpha-2 adrenergic receptorBinding affinity at Alpha-2 adrenergic receptor
ChEMBL 334 4 1 4 2.4 N#Cc1ccccc1N1CCN(CC1)CNC(=O)c1cccc(c1)C 10.1021/jm970021c
CHEMBL5072422 214280 None 0 Human Binding pKi = 6.8 6.8 -41 3
Displacement of [3H]DPCPX from human A2BAR expressed in HEK293 cell membrane incubated for 30 mins by microbeta trilux scintillation counter analysisDisplacement of [3H]DPCPX from human A2BAR expressed in HEK293 cell membrane incubated for 30 mins by microbeta trilux scintillation counter analysis
ChEMBL None None None N#Cc1c(-c2ccccc2)nc(N)nc1-c1cccc(Cl)c1 10.1021/acs.jmedchem.1c01636
101420 162039 None 17 Human Binding pKi = 5.8 5.8 1 3
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 208 2 1 5 -0.1 CCn1c(=O)c2nc[nH]c2n(CC)c1=O 10.1021/jm0104318
CHEMBL416013 162039 None 17 Human Binding pKi = 5.8 5.8 1 3
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 208 2 1 5 -0.1 CCn1c(=O)c2nc[nH]c2n(CC)c1=O 10.1021/jm0104318
9836304 176915 None 0 Human Binding pKi = 5.8 5.8 -7 4
Displacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation countingDisplacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation counting
ChEMBL 310 3 2 7 1.4 Nc1nc(-c2cc[nH]n2)c2nnn(Cc3ccccc3F)c2n1 10.1021/jm800961g
CHEMBL461858 176915 None 0 Human Binding pKi = 5.8 5.8 -7 4
Displacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation countingDisplacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation counting
ChEMBL 310 3 2 7 1.4 Nc1nc(-c2cc[nH]n2)c2nnn(Cc3ccccc3F)c2n1 10.1021/jm800961g
145993861 167398 None 0 Human Binding pKi = 6.8 6.8 -1 4
Displacement of [3H]PSB-602 from human adenosine A2B receptor expressed in CHO cell membranesDisplacement of [3H]PSB-602 from human adenosine A2B receptor expressed in CHO cell membranes
ChEMBL 567 15 1 10 2.5 CCCn1c(=O)c2c(nc3n2CCCN3CCc2ccc(OCC(=O)NCCN(CC)CC)cc2)n(CCC)c1=O 10.1039/C8MD00070K
CHEMBL4295248 167398 None 0 Human Binding pKi = 6.8 6.8 -1 4
Displacement of [3H]PSB-602 from human adenosine A2B receptor expressed in CHO cell membranesDisplacement of [3H]PSB-602 from human adenosine A2B receptor expressed in CHO cell membranes
ChEMBL 567 15 1 10 2.5 CCCn1c(=O)c2c(nc3n2CCCN3CCc2ccc(OCC(=O)NCCN(CC)CC)cc2)n(CCC)c1=O 10.1039/C8MD00070K
135522367 110663 None 0 Human Binding pKi = 7.8 7.8 31 2
Binding affinity of compound for displacement of [3H]DPCPX binding in HEK293 membranes expressing human A2B adenosine receptorsBinding affinity of compound for displacement of [3H]DPCPX binding in HEK293 membranes expressing human A2B adenosine receptors
ChEMBL 493 8 2 10 2.0 CCCn1c(=O)c2nc(-c3cc(NC(=O)Cc4ccc5c(c4)OCO5)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
CHEMBL32591 110663 None 0 Human Binding pKi = 7.8 7.8 31 2
Binding affinity of compound for displacement of [3H]DPCPX binding in HEK293 membranes expressing human A2B adenosine receptorsBinding affinity of compound for displacement of [3H]DPCPX binding in HEK293 membranes expressing human A2B adenosine receptors
ChEMBL 493 8 2 10 2.0 CCCn1c(=O)c2nc(-c3cc(NC(=O)Cc4ccc5c(c4)OCO5)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
135522367 110663 None 0 Human Binding pKi = 7.8 7.8 31 2
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 493 8 2 10 2.0 CCCn1c(=O)c2nc(-c3cc(NC(=O)Cc4ccc5c(c4)OCO5)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
CHEMBL32591 110663 None 0 Human Binding pKi = 7.8 7.8 31 2
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 493 8 2 10 2.0 CCCn1c(=O)c2nc(-c3cc(NC(=O)Cc4ccc5c(c4)OCO5)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
11608581 72480 None 0 Human Binding pKi = 7.8 7.8 4 3
Binding affinity towards human Adenosine A2b receptor expressed in HEK293 cells using 5 nM [3H]DPCPXBinding affinity towards human Adenosine A2b receptor expressed in HEK293 cells using 5 nM [3H]DPCPX
ChEMBL 258 3 1 8 0.5 CCCc1nc(N)c2nc(-n3nccn3)n(C)c2n1 10.1021/jm058018d
CHEMBL198942 72480 None 0 Human Binding pKi = 7.8 7.8 4 3
Binding affinity towards human Adenosine A2b receptor expressed in HEK293 cells using 5 nM [3H]DPCPXBinding affinity towards human Adenosine A2b receptor expressed in HEK293 cells using 5 nM [3H]DPCPX
ChEMBL 258 3 1 8 0.5 CCCc1nc(N)c2nc(-n3nccn3)n(C)c2n1 10.1021/jm058018d
10150517 94730 None 0 Human Binding pKi = 7.8 7.8 15 3
Displacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranesDisplacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranes
ChEMBL 382 6 2 6 2.3 CCCCn1c(=O)[nH]c2nc(-c3cnn(Cc4cccc(F)c4)c3)[nH]c2c1=O 10.1016/j.bmcl.2008.01.008
CHEMBL253048 94730 None 0 Human Binding pKi = 7.8 7.8 15 3
Displacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranesDisplacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranes
ChEMBL 382 6 2 6 2.3 CCCCn1c(=O)[nH]c2nc(-c3cnn(Cc4cccc(F)c4)c3)[nH]c2c1=O 10.1016/j.bmcl.2008.01.008
136042355 71148 None 0 Human Binding pKi = 7.8 7.8 12 2
Displacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation countingDisplacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation counting
ChEMBL 462 8 2 9 2.6 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5ccccc5[nH]4)nn3C)nc2n(CCC)c1=O 10.1021/jm201292w
CHEMBL1955897 71148 None 0 Human Binding pKi = 7.8 7.8 12 2
Displacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation countingDisplacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation counting
ChEMBL 462 8 2 9 2.6 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5ccccc5[nH]4)nn3C)nc2n(CCC)c1=O 10.1021/jm201292w
44406642 72760 None 0 Human Binding pKi = 7.8 7.8 53 3
Displacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cellsDisplacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cells
ChEMBL 485 8 1 11 2.5 CCCn1c(=O)c2nc(-c3cnn(Cc4nc(-c5ccc(C#N)cc5)no4)c3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2005.10.002
CHEMBL199908 72760 None 0 Human Binding pKi = 7.8 7.8 53 3
Displacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cellsDisplacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cells
ChEMBL 485 8 1 11 2.5 CCCn1c(=O)c2nc(-c3cnn(Cc4nc(-c5ccc(C#N)cc5)no4)c3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2005.10.002
24827553 96026 None 0 Human Binding pKi = 7.8 7.8 24 4
Displacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 433 5 1 8 2.6 CCCn1c(=O)c2[nH]c(-c3cnn(-c4ccc(C(F)(F)F)nc4)c3)nc2n(CC)c1=O 10.1021/jm7014815
CHEMBL259772 96026 None 0 Human Binding pKi = 7.8 7.8 24 4
Displacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 433 5 1 8 2.6 CCCn1c(=O)c2[nH]c(-c3cnn(-c4ccc(C(F)(F)F)nc4)c3)nc2n(CC)c1=O 10.1021/jm7014815
53248698 60723 None 0 Human Binding pKi = 7.8 7.8 5 3
Displacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cells after 1 hrDisplacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cells after 1 hr
ChEMBL 534 6 1 6 4.8 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)[C@@H]3CCN(C(=O)c4cccc(C(F)(F)F)c4)C3)sc12 10.1016/j.bmcl.2011.02.053
CHEMBL1760886 60723 None 0 Human Binding pKi = 7.8 7.8 5 3
Displacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cells after 1 hrDisplacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cells after 1 hr
ChEMBL 534 6 1 6 4.8 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)[C@@H]3CCN(C(=O)c4cccc(C(F)(F)F)c4)C3)sc12 10.1016/j.bmcl.2011.02.053
53248699 63103 None 0 Human Binding pKi = 7.8 7.8 3 3
Displacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cells after 1 hrDisplacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cells after 1 hr
ChEMBL 548 8 2 6 6.0 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)[C@H]3CC[C@H](NCc4cccc(C(F)(F)F)c4)CC3)sc12 10.1016/j.bmcl.2011.02.053
CHEMBL1760897 63103 None 0 Human Binding pKi = 7.8 7.8 3 3
Displacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cells after 1 hrDisplacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cells after 1 hr
ChEMBL 548 8 2 6 6.0 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)[C@H]3CC[C@H](NCc4cccc(C(F)(F)F)c4)CC3)sc12 10.1016/j.bmcl.2011.02.053
CHEMBL1789197 63103 None 0 Human Binding pKi = 7.8 7.8 3 3
Displacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cells after 1 hrDisplacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cells after 1 hr
ChEMBL 548 8 2 6 6.0 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)[C@H]3CC[C@H](NCc4cccc(C(F)(F)F)c4)CC3)sc12 10.1016/j.bmcl.2011.02.053
49797749 10621 None 0 Human Binding pKi = 7.8 7.8 3 3
Displacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cells after 1 hr by scintillation countingDisplacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 435 6 1 7 4.1 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(-n4cccn4)cc3)sc12 10.1016/j.bmcl.2010.05.056
CHEMBL1170136 10621 None 0 Human Binding pKi = 7.8 7.8 3 3
Displacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cells after 1 hr by scintillation countingDisplacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 435 6 1 7 4.1 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(-n4cccn4)cc3)sc12 10.1016/j.bmcl.2010.05.056
49798139 10672 None 0 Human Binding pKi = 7.8 7.8 5 3
Displacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cells after 1 hr by scintillation countingDisplacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 495 6 1 7 3.3 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(C(=O)N4CCN(C)CC4)cc3)sc12 10.1016/j.bmcl.2010.05.056
CHEMBL1170583 10672 None 0 Human Binding pKi = 7.8 7.8 5 3
Displacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cells after 1 hr by scintillation countingDisplacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 495 6 1 7 3.3 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(C(=O)N4CCN(C)CC4)cc3)sc12 10.1016/j.bmcl.2010.05.056
11575498 78319 None 0 Human Binding pKi = 7.8 7.8 1 3
Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cellsDisplacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells
ChEMBL 426 7 1 7 3.3 CCCn1c(=O)c2nc(-c3cnn(Cc4cccc(Cl)c4)c3)[nH]c2n(CCC)c1=O 10.1021/jm051268+
CHEMBL210938 78319 None 0 Human Binding pKi = 7.8 7.8 1 3
Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cellsDisplacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells
ChEMBL 426 7 1 7 3.3 CCCn1c(=O)c2nc(-c3cnn(Cc4cccc(Cl)c4)c3)[nH]c2n(CCC)c1=O 10.1021/jm051268+
11582697 140158 None 0 Human Binding pKi = 7.8 7.8 -2 3
Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cellsDisplacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells
ChEMBL 426 7 1 7 3.3 CCCn1c(=O)c2nc(-c3cnn(Cc4ccc(Cl)cc4)c3)[nH]c2n(CCC)c1=O 10.1021/jm051268+
CHEMBL380284 140158 None 0 Human Binding pKi = 7.8 7.8 -2 3
Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cellsDisplacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells
ChEMBL 426 7 1 7 3.3 CCCn1c(=O)c2nc(-c3cnn(Cc4ccc(Cl)cc4)c3)[nH]c2n(CCC)c1=O 10.1021/jm051268+
136042355 71148 None 0 Human Binding pKi = 7.7 7.7 12 2
Displacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation countingDisplacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation counting
ChEMBL 462 8 2 9 2.6 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5ccccc5[nH]4)nn3C)nc2n(CCC)c1=O 10.1021/jm201292w
CHEMBL1955897 71148 None 0 Human Binding pKi = 7.7 7.7 12 2
Displacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation countingDisplacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation counting
ChEMBL 462 8 2 9 2.6 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5ccccc5[nH]4)nn3C)nc2n(CCC)c1=O 10.1021/jm201292w
155561189 175661 None 0 Human Binding pKi = 7.7 7.7 2 4
Displacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 377 5 2 6 0.7 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N(C)C)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
CHEMBL4581448 175661 None 0 Human Binding pKi = 7.7 7.7 2 4
Displacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 377 5 2 6 0.7 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N(C)C)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
11591558 73041 None 0 Human Binding pKi = 7.7 7.7 1 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 508 9 2 6 5.0 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(C)cc4)cc3)c(Cl)c2n(CCC)c1=O 10.1021/jm0506221
CHEMBL201054 73041 None 0 Human Binding pKi = 7.7 7.7 1 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 508 9 2 6 5.0 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(C)cc4)cc3)c(Cl)c2n(CCC)c1=O 10.1021/jm0506221
128784 51803 None 45 Human Binding pKi = 7.7 7.7 -2 5
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 312 5 1 5 2.4 CCCn1c(=O)c2nc(-c3ccccc3)[nH]c2n(CCC)c1=O 10.1021/jm0104318
CHEMBL158507 51803 None 45 Human Binding pKi = 7.7 7.7 -2 5
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 312 5 1 5 2.4 CCCn1c(=O)c2nc(-c3ccccc3)[nH]c2n(CCC)c1=O 10.1021/jm0104318
128784 51803 None 45 Human Binding pKi = 7.7 7.7 -2 5
Binding affinity for human HEK293 adenosine A2B receptor using [125I]ABOPX in CHO cell membranesBinding affinity for human HEK293 adenosine A2B receptor using [125I]ABOPX in CHO cell membranes
ChEMBL 312 5 1 5 2.4 CCCn1c(=O)c2nc(-c3ccccc3)[nH]c2n(CCC)c1=O 10.1021/jm0310030
CHEMBL158507 51803 None 45 Human Binding pKi = 7.7 7.7 -2 5
Binding affinity for human HEK293 adenosine A2B receptor using [125I]ABOPX in CHO cell membranesBinding affinity for human HEK293 adenosine A2B receptor using [125I]ABOPX in CHO cell membranes
ChEMBL 312 5 1 5 2.4 CCCn1c(=O)c2nc(-c3ccccc3)[nH]c2n(CCC)c1=O 10.1021/jm0310030
11102838 169034 None 0 Human Binding pKi = 6.8 6.8 -3 3
Displacement of [3H]- DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]- DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 475 7 1 9 4.4 CSc1c2c(nc(NC(=O)Cc3ccc(CC(C)C)cc3)n3nc(-c4ccco4)nc23)nn1C 10.1021/jm021023m
CHEMBL439447 169034 None 0 Human Binding pKi = 6.8 6.8 -3 3
Displacement of [3H]- DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]- DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 475 7 1 9 4.4 CSc1c2c(nc(NC(=O)Cc3ccc(CC(C)C)cc3)n3nc(-c4ccco4)nc23)nn1C 10.1021/jm021023m
11133545 120470 None 0 Human Binding pKi = 6.8 6.8 -13 4
Displacement of [3H]DPCPX binding at human Adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX binding at human Adenosine A2B receptor expressed in HEK293 cells
ChEMBL 419 4 2 10 2.8 Cn1cc2c(nc(NC(=O)Nc3ccc([N+](=O)[O-])cc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm0109614
CHEMBL354161 120470 None 0 Human Binding pKi = 6.8 6.8 -13 4
Displacement of [3H]DPCPX binding at human Adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX binding at human Adenosine A2B receptor expressed in HEK293 cells
ChEMBL 419 4 2 10 2.8 Cn1cc2c(nc(NC(=O)Nc3ccc([N+](=O)[O-])cc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm0109614
CHEMBL5081556 214753 None 0 Human Binding pKi = 6.8 6.8 -5 5
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells by liquid scintillation counting analysisDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells by liquid scintillation counting analysis
ChEMBL None None None Nc1nc(-c2ccccc2)c2c(n1)-c1ccc(OCCCN3CCCC3)cc1C2=O 10.1021/acs.jmedchem.0c00914
4882 2099 None 82 Human Binding pKi = 5.8 5.8 -104 6
Inhibition of human adenosine 2B receptorInhibition of human adenosine 2B receptor
ChEMBL 384 6 0 8 2.1 COc1cc(/C=C/c2nc3c(n2C)c(=O)n(c(=O)n3CC)CC)ccc1OC 10.1021/acs.jmedchem.0c00237
5311037 2099 None 82 Human Binding pKi = 5.8 5.8 -104 6
Inhibition of human adenosine 2B receptorInhibition of human adenosine 2B receptor
ChEMBL 384 6 0 8 2.1 COc1cc(/C=C/c2nc3c(n2C)c(=O)n(c(=O)n3CC)CC)ccc1OC 10.1021/acs.jmedchem.0c00237
5311037.0 2099 None 82 Human Binding pKi = 5.8 5.8 -104 6
Inhibition of human adenosine 2B receptorInhibition of human adenosine 2B receptor
ChEMBL 384 6 0 8 2.1 COc1cc(/C=C/c2nc3c(n2C)c(=O)n(c(=O)n3CC)CC)ccc1OC 10.1021/acs.jmedchem.0c00237
5608 2099 None 82 Human Binding pKi = 5.8 5.8 -104 6
Inhibition of human adenosine 2B receptorInhibition of human adenosine 2B receptor
ChEMBL 384 6 0 8 2.1 COc1cc(/C=C/c2nc3c(n2C)c(=O)n(c(=O)n3CC)CC)ccc1OC 10.1021/acs.jmedchem.0c00237
CHEMBL431770 2099 None 82 Human Binding pKi = 5.8 5.8 -104 6
Inhibition of human adenosine 2B receptorInhibition of human adenosine 2B receptor
ChEMBL 384 6 0 8 2.1 COc1cc(/C=C/c2nc3c(n2C)c(=O)n(c(=O)n3CC)CC)ccc1OC 10.1021/acs.jmedchem.0c00237
DB11757 2099 None 82 Human Binding pKi = 5.8 5.8 -104 6
Inhibition of human adenosine 2B receptorInhibition of human adenosine 2B receptor
ChEMBL 384 6 0 8 2.1 COc1cc(/C=C/c2nc3c(n2C)c(=O)n(c(=O)n3CC)CC)ccc1OC 10.1021/acs.jmedchem.0c00237
4882 2099 None 82 Human Binding pKi = 5.8 5.8 -104 6
Inhibition of human recombinant adenosine receptor A2bInhibition of human recombinant adenosine receptor A2b
ChEMBL 384 6 0 8 2.1 COc1cc(/C=C/c2nc3c(n2C)c(=O)n(c(=O)n3CC)CC)ccc1OC 10.1021/jm4011669
5311037 2099 None 82 Human Binding pKi = 5.8 5.8 -104 6
Inhibition of human recombinant adenosine receptor A2bInhibition of human recombinant adenosine receptor A2b
ChEMBL 384 6 0 8 2.1 COc1cc(/C=C/c2nc3c(n2C)c(=O)n(c(=O)n3CC)CC)ccc1OC 10.1021/jm4011669
5311037.0 2099 None 82 Human Binding pKi = 5.8 5.8 -104 6
Inhibition of human recombinant adenosine receptor A2bInhibition of human recombinant adenosine receptor A2b
ChEMBL 384 6 0 8 2.1 COc1cc(/C=C/c2nc3c(n2C)c(=O)n(c(=O)n3CC)CC)ccc1OC 10.1021/jm4011669
5608 2099 None 82 Human Binding pKi = 5.8 5.8 -104 6
Inhibition of human recombinant adenosine receptor A2bInhibition of human recombinant adenosine receptor A2b
ChEMBL 384 6 0 8 2.1 COc1cc(/C=C/c2nc3c(n2C)c(=O)n(c(=O)n3CC)CC)ccc1OC 10.1021/jm4011669
CHEMBL431770 2099 None 82 Human Binding pKi = 5.8 5.8 -104 6
Inhibition of human recombinant adenosine receptor A2bInhibition of human recombinant adenosine receptor A2b
ChEMBL 384 6 0 8 2.1 COc1cc(/C=C/c2nc3c(n2C)c(=O)n(c(=O)n3CC)CC)ccc1OC 10.1021/jm4011669
DB11757 2099 None 82 Human Binding pKi = 5.8 5.8 -104 6
Inhibition of human recombinant adenosine receptor A2bInhibition of human recombinant adenosine receptor A2b
ChEMBL 384 6 0 8 2.1 COc1cc(/C=C/c2nc3c(n2C)c(=O)n(c(=O)n3CC)CC)ccc1OC 10.1021/jm4011669
11144868 119872 None 0 Human Binding pKi = 6.7 6.7 -12 4
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 152-216Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 152-216
ChEMBL 452 3 2 8 3.7 Cn1cc2c(nc(NC(=O)Nc3ccc(Br)cc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm0109614
CHEMBL348925 119872 None 0 Human Binding pKi = 6.7 6.7 -12 4
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 152-216Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 152-216
ChEMBL 452 3 2 8 3.7 Cn1cc2c(nc(NC(=O)Nc3ccc(Br)cc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm0109614
21874681 189098 None 0 Human Binding pKi = 6.7 6.7 -114 4
Displacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation countingDisplacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation counting
ChEMBL 321 4 2 8 2.2 CNc1ccc(Cn2nnc3c(-c4ccco4)nc(N)nc32)cc1 10.1021/jm800961g
CHEMBL510134 189098 None 0 Human Binding pKi = 6.7 6.7 -114 4
Displacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation countingDisplacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation counting
ChEMBL 321 4 2 8 2.2 CNc1ccc(Cn2nnc3c(-c4ccco4)nc(N)nc32)cc1 10.1021/jm800961g
2882039 28238 None 11 Human Binding pKi = 5.7 5.7 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by Scatchard plot analysisDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by Scatchard plot analysis
ChEMBL 294 3 1 4 2.7 CC1=C(C(=O)OC(C)C)C(c2ccsc2)NC(=O)N1C 10.1021/ml400185v
CHEMBL1373953 28238 None 11 Human Binding pKi = 5.7 5.7 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by Scatchard plot analysisDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by Scatchard plot analysis
ChEMBL 294 3 1 4 2.7 CC1=C(C(=O)OC(C)C)C(c2ccsc2)NC(=O)N1C 10.1021/ml400185v
12267225 141629 None 0 Human Binding pKi = 6.7 6.7 -3 3
Displacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cells
ChEMBL 255 1 1 4 1.2 Cn1c(=O)c2[nH]c(-c3ccccc3)cc2n(C)c1=O 10.1016/j.bmc.2008.09.067
CHEMBL38528 141629 None 0 Human Binding pKi = 6.7 6.7 -3 3
Displacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cells
ChEMBL 255 1 1 4 1.2 Cn1c(=O)c2[nH]c(-c3ccccc3)cc2n(C)c1=O 10.1016/j.bmc.2008.09.067
44390549 63487 None 0 Human Binding pKi = 5.7 5.7 - 1
Binding affinity for adenosine A2b receptor by using as [3H]ZM-241385 (14 nM) radioligand in membranes from HEK-A2B cellsBinding affinity for adenosine A2b receptor by using as [3H]ZM-241385 (14 nM) radioligand in membranes from HEK-A2B cells
ChEMBL 520 9 1 9 4.7 CCCn1c(=O)c2nc(-c3ccc(OCc4nc(-c5ccccc5Cl)no4)cc3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2004.11.044
CHEMBL179932 63487 None 0 Human Binding pKi = 5.7 5.7 - 1
Binding affinity for adenosine A2b receptor by using as [3H]ZM-241385 (14 nM) radioligand in membranes from HEK-A2B cellsBinding affinity for adenosine A2b receptor by using as [3H]ZM-241385 (14 nM) radioligand in membranes from HEK-A2B cells
ChEMBL 520 9 1 9 4.7 CCCn1c(=O)c2nc(-c3ccc(OCc4nc(-c5ccccc5Cl)no4)cc3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2004.11.044
45268869 195551 None 0 Human Binding pKi = 6.7 6.7 -48 4
Binding affinity to adenosine A2B receptorBinding affinity to adenosine A2B receptor
ChEMBL 328 4 2 5 2.9 Nc1nc(C(=O)NCc2cccc(Cl)c2)cc(-c2ccco2)n1 10.1016/j.bmcl.2009.03.142
CHEMBL554623 195551 None 0 Human Binding pKi = 6.7 6.7 -48 4
Binding affinity to adenosine A2B receptorBinding affinity to adenosine A2B receptor
ChEMBL 328 4 2 5 2.9 Nc1nc(C(=O)NCc2cccc(Cl)c2)cc(-c2ccco2)n1 10.1016/j.bmcl.2009.03.142
44520985 199858 None 0 Human Binding pKi = 5.7 5.7 -338 4
Displacement of radioligand from human adenosine A2B receptor expressed in cells by topcount microplate scintillation countingDisplacement of radioligand from human adenosine A2B receptor expressed in cells by topcount microplate scintillation counting
ChEMBL 340 5 2 7 2.3 Cc1ccc(-c2cc(C(=O)NCc3nccn3C(C)C)nc(N)n2)o1 10.1016/j.bmc.2009.07.078
CHEMBL594455 199858 None 0 Human Binding pKi = 5.7 5.7 -338 4
Displacement of radioligand from human adenosine A2B receptor expressed in cells by topcount microplate scintillation countingDisplacement of radioligand from human adenosine A2B receptor expressed in cells by topcount microplate scintillation counting
ChEMBL 340 5 2 7 2.3 Cc1ccc(-c2cc(C(=O)NCc3nccn3C(C)C)nc(N)n2)o1 10.1016/j.bmc.2009.07.078
135440428 78540 None 0 Human Binding pKi = 6.7 6.7 -1 2
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 483 9 2 9 2.3 CCCn1c(=O)c2nc(-c3cc(OCC(=O)Nc4ccc(F)cc4)n(C)n3)[nH]c2n(CCC)c1=O 10.1021/jm0309654
CHEMBL2112066 78540 None 0 Human Binding pKi = 6.7 6.7 -1 2
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 483 9 2 9 2.3 CCCn1c(=O)c2nc(-c3cc(OCC(=O)Nc4ccc(F)cc4)n(C)n3)[nH]c2n(CCC)c1=O 10.1021/jm0309654
CHEMBL5081937 214778 None 0 Human Binding pKi = 6.7 6.7 -3 2
Displacement of [3H]DPCPX from human A2BAR expressed in HEK293 cell membrane incubated for 30 mins by microbeta trilux scintillation counter analysisDisplacement of [3H]DPCPX from human A2BAR expressed in HEK293 cell membrane incubated for 30 mins by microbeta trilux scintillation counter analysis
ChEMBL None None None COc1ccc(-c2nc(Nc3ccccc3)nc(-c3ccccc3)c2C#N)cc1 10.1021/acs.jmedchem.1c01636
CHEMBL5088089 215137 None 0 Human Binding pKi = 6.7 6.7 -13 3
Displacement of [3H]DPCPX from human A2BAR expressed in HEK293 cell membrane incubated for 30 mins by microbeta trilux scintillation counter analysisDisplacement of [3H]DPCPX from human A2BAR expressed in HEK293 cell membrane incubated for 30 mins by microbeta trilux scintillation counter analysis
ChEMBL None None None N#Cc1c(-c2ccccc2)nc(N)nc1-c1cccc(F)c1 10.1021/acs.jmedchem.1c01636
1329 1472 None 86 Rat Binding pKi = 6.7 6.7 -1905 14
Inhibition of [125I]-APOBX binding to rat Adenosine A2B receptor expressed in HEK cellsInhibition of [125I]-APOBX binding to rat Adenosine A2B receptor expressed in HEK cells
ChEMBL 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 10.1021/jm0104318
386 1472 None 86 Rat Binding pKi = 6.7 6.7 -1905 14
Inhibition of [125I]-APOBX binding to rat Adenosine A2B receptor expressed in HEK cellsInhibition of [125I]-APOBX binding to rat Adenosine A2B receptor expressed in HEK cells
ChEMBL 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 10.1021/jm0104318
CHEMBL183 1472 None 86 Rat Binding pKi = 6.7 6.7 -1905 14
Inhibition of [125I]-APOBX binding to rat Adenosine A2B receptor expressed in HEK cellsInhibition of [125I]-APOBX binding to rat Adenosine A2B receptor expressed in HEK cells
ChEMBL 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 10.1021/jm0104318
DB12946 1472 None 86 Rat Binding pKi = 6.7 6.7 -1905 14
Inhibition of [125I]-APOBX binding to rat Adenosine A2B receptor expressed in HEK cellsInhibition of [125I]-APOBX binding to rat Adenosine A2B receptor expressed in HEK cells
ChEMBL 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 10.1021/jm0104318
44406906 72810 None 0 Human Binding pKi = 6.7 6.7 -1 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 447 7 3 7 1.8 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(CCN)cc4)cc3)cc2n(C)c1=O 10.1021/jm0506221
CHEMBL200105 72810 None 0 Human Binding pKi = 6.7 6.7 -1 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 447 7 3 7 1.8 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(CCN)cc4)cc3)cc2n(C)c1=O 10.1021/jm0506221
11547533 140913 None 0 Human Binding pKi = 6.7 6.7 -1 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 482 7 2 7 2.6 COc1cc(-c2cc3c([nH]2)c(=O)n(C)c(=O)n3C)ccc1OCC(=O)NCc1ccc(Cl)cc1 10.1021/jm0506221
CHEMBL382234 140913 None 0 Human Binding pKi = 6.7 6.7 -1 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 482 7 2 7 2.6 COc1cc(-c2cc3c([nH]2)c(=O)n(C)c(=O)n3C)ccc1OCC(=O)NCc1ccc(Cl)cc1 10.1021/jm0506221
10605011 118760 None 0 Human Binding pKi = 5.7 5.7 -4 4
Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 1681-1961Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 1681-1961
ChEMBL 732 6 2 8 7.6 O=C(Nc1cccc(Cl)c1)Nc1nc2nn(CCc3cc(Br)c(Br)cc3Br)cc2c2nc(-c3ccco3)nn12 10.1021/jm001047y
CHEMBL341852 118760 None 0 Human Binding pKi = 5.7 5.7 -4 4
Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 1681-1961Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 1681-1961
ChEMBL 732 6 2 8 7.6 O=C(Nc1cccc(Cl)c1)Nc1nc2nn(CCc3cc(Br)c(Br)cc3Br)cc2c2nc(-c3ccco3)nn12 10.1021/jm001047y
76320909 104033 None 0 Human Binding pKi = 6.7 6.7 -1513 6
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 300 1 1 5 1.0 Cn1c(=O)c2[nH]c([C@]34C[C@@H]5C[C@H](C[C@H]3C5)C4)nc2n(C)c1=O 10.1016/j.bmc.2013.09.044
CHEMBL3093327 104033 None 0 Human Binding pKi = 6.7 6.7 -1513 6
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 300 1 1 5 1.0 Cn1c(=O)c2[nH]c([C@]34C[C@@H]5C[C@H](C[C@H]3C5)C4)nc2n(C)c1=O 10.1016/j.bmc.2013.09.044
15667105 108744 None 0 Human Binding pKi = 6.7 6.7 -263 5
Binding affinity to human adenosine A2B receptor by radioligand displacement assayBinding affinity to human adenosine A2B receptor by radioligand displacement assay
ChEMBL 384 7 1 5 3.6 CCCCn1c(=O)c2nc(C34CC5CC(CC3C5)C4)[nH]c2n(CCCC)c1=O 10.1039/C8MD00070K
CHEMBL320872 108744 None 0 Human Binding pKi = 6.7 6.7 -263 5
Binding affinity to human adenosine A2B receptor by radioligand displacement assayBinding affinity to human adenosine A2B receptor by radioligand displacement assay
ChEMBL 384 7 1 5 3.6 CCCCn1c(=O)c2nc(C34CC5CC(CC3C5)C4)[nH]c2n(CCCC)c1=O 10.1039/C8MD00070K
11689583 3214 None 29 Human Binding pKi = 6.7 6.7 -1513 7
Displacement of [3H]PSB-603 from human adenosine receptor A2B expressed in CHO cell membranes incubated for 75 mins by radioligand competition assayDisplacement of [3H]PSB-603 from human adenosine receptor A2B expressed in CHO cell membranes incubated for 75 mins by radioligand competition assay
ChEMBL 386 7 2 6 2.1 OCCCn1c2[nH]c(nc2c(=O)n(c1=O)CCCC)C12CC3CC2CC(C1)C3 10.1016/j.ejmech.2019.111879
3285 3214 None 29 Human Binding pKi = 6.7 6.7 -1513 7
Displacement of [3H]PSB-603 from human adenosine receptor A2B expressed in CHO cell membranes incubated for 75 mins by radioligand competition assayDisplacement of [3H]PSB-603 from human adenosine receptor A2B expressed in CHO cell membranes incubated for 75 mins by radioligand competition assay
ChEMBL 386 7 2 6 2.1 OCCCn1c2[nH]c(nc2c(=O)n(c1=O)CCCC)C12CC3CC2CC(C1)C3 10.1016/j.ejmech.2019.111879
CHEMBL1316674 3214 None 29 Human Binding pKi = 6.7 6.7 -1513 7
Displacement of [3H]PSB-603 from human adenosine receptor A2B expressed in CHO cell membranes incubated for 75 mins by radioligand competition assayDisplacement of [3H]PSB-603 from human adenosine receptor A2B expressed in CHO cell membranes incubated for 75 mins by radioligand competition assay
ChEMBL 386 7 2 6 2.1 OCCCn1c2[nH]c(nc2c(=O)n(c1=O)CCCC)C12CC3CC2CC(C1)C3 10.1016/j.ejmech.2019.111879
11780616 203611 None 5 Rat Binding pKi = 4.7 4.7 -1 4
Inhibition of [125I]-APOBX binding to rat Adenosine A2B receptor expressed in HEK cellsInhibition of [125I]-APOBX binding to rat Adenosine A2B receptor expressed in HEK cells
ChEMBL 270 4 0 6 0.5 Cn1c(=O)c2c(ncn2CCCCCl)n(C)c1=O 10.1021/jm0104318
CHEMBL67060 203611 None 5 Rat Binding pKi = 4.7 4.7 -1 4
Inhibition of [125I]-APOBX binding to rat Adenosine A2B receptor expressed in HEK cellsInhibition of [125I]-APOBX binding to rat Adenosine A2B receptor expressed in HEK cells
ChEMBL 270 4 0 6 0.5 Cn1c(=O)c2c(ncn2CCCCCl)n(C)c1=O 10.1021/jm0104318
136044130 49112 None 0 Human Binding pKi = 6.7 6.7 4 3
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 402 8 3 8 1.5 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)O)cc3O)[nH]c2n(CCC)c1=O 10.1021/jm0104318
CHEMBL156178 49112 None 0 Human Binding pKi = 6.7 6.7 4 3
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 402 8 3 8 1.5 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)O)cc3O)[nH]c2n(CCC)c1=O 10.1021/jm0104318
CHEMBL5090384 215259 None 0 Human Binding pKi = 6.7 6.7 -16 3
Displacement of [3H]DPCPX from human A2BAR expressed in HEK293 cell membrane incubated for 30 mins by microbeta trilux scintillation counter analysisDisplacement of [3H]DPCPX from human A2BAR expressed in HEK293 cell membrane incubated for 30 mins by microbeta trilux scintillation counter analysis
ChEMBL None None None N#Cc1c(-c2ccccc2)nc(Nc2ccccc2)nc1-c1ccc2c(c1)OCO2 10.1021/acs.jmedchem.1c01636
128525 154724 None 10 Rat Binding pKi = 5.7 5.7 -5 6
Inhibition of [125I]-APOBX binding to rat Adenosine A2B receptor expressed in HEK cellsInhibition of [125I]-APOBX binding to rat Adenosine A2B receptor expressed in HEK cells
ChEMBL 194 2 2 4 -0.2 CCCn1c(=O)[nH]c2[nH]cnc2c1=O 10.1021/jm0104318
CHEMBL39986 154724 None 10 Rat Binding pKi = 5.7 5.7 -5 6
Inhibition of [125I]-APOBX binding to rat Adenosine A2B receptor expressed in HEK cellsInhibition of [125I]-APOBX binding to rat Adenosine A2B receptor expressed in HEK cells
ChEMBL 194 2 2 4 -0.2 CCCn1c(=O)[nH]c2[nH]cnc2c1=O 10.1021/jm0104318
44401051 124371 None 0 Human Binding pKi = 4.7 4.7 -23442 4
Binding affinity for human adenosine A2b receptor subtype expressed in CHO cellsBinding affinity for human adenosine A2b receptor subtype expressed in CHO cells
ChEMBL 355 3 4 9 0.4 O[C@H]1O[C@@H](n2cnc3c(NC4CCCC4)nc(Cl)nc32)[C@H](O)[C@@H]1O 10.1021/jm049408n
CHEMBL363807 124371 None 0 Human Binding pKi = 4.7 4.7 -23442 4
Binding affinity for human adenosine A2b receptor subtype expressed in CHO cellsBinding affinity for human adenosine A2b receptor subtype expressed in CHO cells
ChEMBL 355 3 4 9 0.4 O[C@H]1O[C@@H](n2cnc3c(NC4CCCC4)nc(Cl)nc32)[C@H](O)[C@@H]1O 10.1021/jm049408n
11395785 186514 None 0 Human Binding pKi = 4.7 4.7 -15488 4
Displacement of [3H]PSB-603 from human adenosine receptor A2B in CHO cells after 75 mins by liquid scintillation methodDisplacement of [3H]PSB-603 from human adenosine receptor A2B in CHO cells after 75 mins by liquid scintillation method
ChEMBL 410 5 4 9 0.6 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NC4CCCC4)nc(Cl)nc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.7b00457
CHEMBL487754 186514 None 0 Human Binding pKi = 4.7 4.7 -15488 4
Displacement of [3H]PSB-603 from human adenosine receptor A2B in CHO cells after 75 mins by liquid scintillation methodDisplacement of [3H]PSB-603 from human adenosine receptor A2B in CHO cells after 75 mins by liquid scintillation method
ChEMBL 410 5 4 9 0.6 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NC4CCCC4)nc(Cl)nc32)[C@H](O)[C@@H]1O 10.1021/acs.jmedchem.7b00457
22282339 83104 None 3 Mouse Binding pKi = 6.7 6.7 -275 15
Displacement of [3H] DPCPX from mouse adenosine A2B receptor expressed in HEK293 cells incubated for 60 mins by radioligand binding assayDisplacement of [3H] DPCPX from mouse adenosine A2B receptor expressed in HEK293 cells incubated for 60 mins by radioligand binding assay
ChEMBL 386 4 1 5 5.1 Cc1cc(C)cc(-c2nc(NC(=O)c3cccnc3)sc2-c2ccncc2)c1 10.1021/acsmedchemlett.1c00685
CHEMBL2181976 83104 None 3 Mouse Binding pKi = 6.7 6.7 -275 15
Displacement of [3H] DPCPX from mouse adenosine A2B receptor expressed in HEK293 cells incubated for 60 mins by radioligand binding assayDisplacement of [3H] DPCPX from mouse adenosine A2B receptor expressed in HEK293 cells incubated for 60 mins by radioligand binding assay
ChEMBL 386 4 1 5 5.1 Cc1cc(C)cc(-c2nc(NC(=O)c3cccnc3)sc2-c2ccncc2)c1 10.1021/acsmedchemlett.1c00685
CHEMBL5084951 83104 None 3 Mouse Binding pKi = 6.7 6.7 -275 15
Displacement of [3H] DPCPX from mouse adenosine A2B receptor expressed in HEK293 cells incubated for 60 mins by radioligand binding assayDisplacement of [3H] DPCPX from mouse adenosine A2B receptor expressed in HEK293 cells incubated for 60 mins by radioligand binding assay
ChEMBL 386 4 1 5 5.1 Cc1cc(C)cc(-c2nc(NC(=O)c3cccnc3)sc2-c2ccncc2)c1 10.1021/acsmedchemlett.1c00685
377 2758 None 53 Human Binding pKi = 5.7 5.7 -1479 15
Displacement of [3H]PSB-603 from human adenosine receptor A2B in CHO cells after 75 mins by liquid scintillation methodDisplacement of [3H]PSB-603 from human adenosine receptor A2B in CHO cells after 75 mins by liquid scintillation method
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.7b00457
425 2758 None 53 Human Binding pKi = 5.7 5.7 -1479 15
Displacement of [3H]PSB-603 from human adenosine receptor A2B in CHO cells after 75 mins by liquid scintillation methodDisplacement of [3H]PSB-603 from human adenosine receptor A2B in CHO cells after 75 mins by liquid scintillation method
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.7b00457
448222 2758 None 53 Human Binding pKi = 5.7 5.7 -1479 15
Displacement of [3H]PSB-603 from human adenosine receptor A2B in CHO cells after 75 mins by liquid scintillation methodDisplacement of [3H]PSB-603 from human adenosine receptor A2B in CHO cells after 75 mins by liquid scintillation method
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.7b00457
CHEMBL464859 2758 None 53 Human Binding pKi = 5.7 5.7 -1479 15
Displacement of [3H]PSB-603 from human adenosine receptor A2B in CHO cells after 75 mins by liquid scintillation methodDisplacement of [3H]PSB-603 from human adenosine receptor A2B in CHO cells after 75 mins by liquid scintillation method
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.7b00457
377 2758 None 53 Human Binding pKi = 5.7 5.7 -1479 15
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm900413e
425 2758 None 53 Human Binding pKi = 5.7 5.7 -1479 15
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm900413e
448222 2758 None 53 Human Binding pKi = 5.7 5.7 -1479 15
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm900413e
CHEMBL464859 2758 None 53 Human Binding pKi = 5.7 5.7 -1479 15
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm900413e
377 2758 None 53 Human Binding pKi = 5.7 5.7 -1479 15
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells after 75 mins by liquid scintillation assayDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells after 75 mins by liquid scintillation assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/ml200189u
425 2758 None 53 Human Binding pKi = 5.7 5.7 -1479 15
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells after 75 mins by liquid scintillation assayDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells after 75 mins by liquid scintillation assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/ml200189u
448222 2758 None 53 Human Binding pKi = 5.7 5.7 -1479 15
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells after 75 mins by liquid scintillation assayDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells after 75 mins by liquid scintillation assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/ml200189u
CHEMBL464859 2758 None 53 Human Binding pKi = 5.7 5.7 -1479 15
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells after 75 mins by liquid scintillation assayDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells after 75 mins by liquid scintillation assay
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/ml200189u
162660983 181871 None 0 Human Binding pKi = 5.7 5.7 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 294 2 2 4 2.4 CC1=C(C(=O)OC(C)(C)C)C(c2ccoc2)NC(=S)N1 10.1021/acs.jmedchem.0c01431
CHEMBL4778860 181871 None 0 Human Binding pKi = 5.7 5.7 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 294 2 2 4 2.4 CC1=C(C(=O)OC(C)(C)C)C(c2ccoc2)NC(=S)N1 10.1021/acs.jmedchem.0c01431
135546649 116636 None 0 Human Binding pKi = 7.7 7.7 4 2
Binding affinity of compound for displacement of [3H]DPCPX binding in HEK293 membranes expressing human A2B adenosine receptorsBinding affinity of compound for displacement of [3H]DPCPX binding in HEK293 membranes expressing human A2B adenosine receptors
ChEMBL 479 9 2 9 2.4 CCCn1c(=O)c2nc(-c3cc(OCC(=O)Nc4ccc(C)cc4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
CHEMBL33695 116636 None 0 Human Binding pKi = 7.7 7.7 4 2
Binding affinity of compound for displacement of [3H]DPCPX binding in HEK293 membranes expressing human A2B adenosine receptorsBinding affinity of compound for displacement of [3H]DPCPX binding in HEK293 membranes expressing human A2B adenosine receptors
ChEMBL 479 9 2 9 2.4 CCCn1c(=O)c2nc(-c3cc(OCC(=O)Nc4ccc(C)cc4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
135546649 116636 None 0 Human Binding pKi = 7.7 7.7 4 2
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 479 9 2 9 2.4 CCCn1c(=O)c2nc(-c3cc(OCC(=O)Nc4ccc(C)cc4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
CHEMBL33695 116636 None 0 Human Binding pKi = 7.7 7.7 4 2
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 479 9 2 9 2.4 CCCn1c(=O)c2nc(-c3cc(OCC(=O)Nc4ccc(C)cc4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
66894703 157593 None 0 Human Binding pKi = 7.7 7.7 - 1
Displacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting methodDisplacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting method
ChEMBL 511 8 1 8 2.9 CCCn1c(=O)c2[nH]c(-c3cnn(CC4CC(=O)N(c5ccc(F)cc5F)C4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2016.11.007
CHEMBL4080807 157593 None 0 Human Binding pKi = 7.7 7.7 - 1
Displacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting methodDisplacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting method
ChEMBL 511 8 1 8 2.9 CCCn1c(=O)c2[nH]c(-c3cnn(CC4CC(=O)N(c5ccc(F)cc5F)C4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2016.11.007
44588438 189119 None 0 Human Binding pKi = 7.7 7.7 8 2
Displacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cells
ChEMBL 342 5 3 6 2.3 CCCn1c(=O)c2[nH]c(-c3ccc(N)cc3)c(O)c2n(CCC)c1=O 10.1016/j.bmc.2008.09.067
CHEMBL510409 189119 None 0 Human Binding pKi = 7.7 7.7 8 2
Displacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cells
ChEMBL 342 5 3 6 2.3 CCCn1c(=O)c2[nH]c(-c3ccc(N)cc3)c(O)c2n(CCC)c1=O 10.1016/j.bmc.2008.09.067
136042333 71160 None 0 Human Binding pKi = 7.7 7.7 10 2
Displacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation countingDisplacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation counting
ChEMBL 514 8 2 9 3.4 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5cc(Cl)c(F)cc5[nH]4)nn3C)nc2n(CCC)c1=O 10.1021/jm201292w
CHEMBL1955909 71160 None 0 Human Binding pKi = 7.7 7.7 10 2
Displacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation countingDisplacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation counting
ChEMBL 514 8 2 9 3.4 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5cc(Cl)c(F)cc5[nH]4)nn3C)nc2n(CCC)c1=O 10.1021/jm201292w
44406545 72891 None 0 Human Binding pKi = 7.7 7.7 25 4
Displacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cellsDisplacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cells
ChEMBL 494 8 1 10 3.3 CCCn1c(=O)c2nc(-c3cnn(Cc4nc(-c5ccccc5Cl)no4)c3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2005.10.002
CHEMBL200370 72891 None 0 Human Binding pKi = 7.7 7.7 25 4
Displacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cellsDisplacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cells
ChEMBL 494 8 1 10 3.3 CCCn1c(=O)c2nc(-c3cnn(Cc4nc(-c5ccccc5Cl)no4)c3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2005.10.002
21958557 95789 None 0 Human Binding pKi = 7.7 7.7 6 3
Displacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 364 5 1 7 1.7 CCCn1c(=O)c2[nH]c(-c3cnn(Cc4ccccc4)c3)nc2n(C)c1=O 10.1021/jm7014815
CHEMBL258686 95789 None 0 Human Binding pKi = 7.7 7.7 6 3
Displacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 364 5 1 7 1.7 CCCn1c(=O)c2[nH]c(-c3cnn(Cc4ccccc4)c3)nc2n(C)c1=O 10.1021/jm7014815
49797795 10616 None 0 Human Binding pKi = 7.7 7.7 4 3
Displacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cells after 1 hr by scintillation countingDisplacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 447 6 1 7 3.3 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(S(C)(=O)=O)cc3)sc12 10.1016/j.bmcl.2010.05.056
CHEMBL1170129 10616 None 0 Human Binding pKi = 7.7 7.7 4 3
Displacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cells after 1 hr by scintillation countingDisplacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 447 6 1 7 3.3 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(S(C)(=O)=O)cc3)sc12 10.1016/j.bmcl.2010.05.056
49797904 10742 None 0 Human Binding pKi = 7.7 7.7 2 2
Displacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cells after 1 hr by scintillation countingDisplacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 373 5 1 7 2.7 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3cnn(C)c3)sc12 10.1016/j.bmcl.2010.05.056
CHEMBL1171163 10742 None 0 Human Binding pKi = 7.7 7.7 2 2
Displacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cells after 1 hr by scintillation countingDisplacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 373 5 1 7 2.7 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3cnn(C)c3)sc12 10.1016/j.bmcl.2010.05.056
52948949 19270 None 0 Human Binding pKi = 7.7 7.7 1 2
Displacement of [3H]ZM241385 from human adenosine A2B receptor transfected in CHO cells after 60 mins by scintillation countingDisplacement of [3H]ZM241385 from human adenosine A2B receptor transfected in CHO cells after 60 mins by scintillation counting
ChEMBL 494 8 3 4 5.4 O=C(NCc1ccccc1)NCc1ccc2[nH]c(=O)c(-c3nccs3)c(CCc3ccccc3)c2c1 10.1016/j.bmcl.2010.10.030
CHEMBL1290322 19270 None 0 Human Binding pKi = 7.7 7.7 1 2
Displacement of [3H]ZM241385 from human adenosine A2B receptor transfected in CHO cells after 60 mins by scintillation countingDisplacement of [3H]ZM241385 from human adenosine A2B receptor transfected in CHO cells after 60 mins by scintillation counting
ChEMBL 494 8 3 4 5.4 O=C(NCc1ccccc1)NCc1ccc2[nH]c(=O)c(-c3nccs3)c(CCc3ccccc3)c2c1 10.1016/j.bmcl.2010.10.030
11588630 78107 None 0 Human Binding pKi = 7.7 7.7 6 3
Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cellsDisplacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells
ChEMBL 364 5 1 7 1.8 CCn1c(=O)c2nc(-c3cnn(Cc4ccccc4)c3)[nH]c2n(CC)c1=O 10.1021/jm051268+
CHEMBL210271 78107 None 0 Human Binding pKi = 7.7 7.7 6 3
Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cellsDisplacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells
ChEMBL 364 5 1 7 1.8 CCn1c(=O)c2nc(-c3cnn(Cc4ccccc4)c3)[nH]c2n(CC)c1=O 10.1021/jm051268+
640847 100059 None 1 Human Binding pKi = 7.7 7.7 7 4
Inhibition of [3H]ZM-241385 binding to human adenosine A2B receptorInhibition of [3H]ZM-241385 binding to human adenosine A2B receptor
ChEMBL 256 2 2 4 1.1 CCn1c(=O)[nH]c2[nH]c(-c3ccccc3)nc2c1=O 10.1021/jm011049y
CHEMBL287129 100059 None 1 Human Binding pKi = 7.7 7.7 7 4
Inhibition of [3H]ZM-241385 binding to human adenosine A2B receptorInhibition of [3H]ZM-241385 binding to human adenosine A2B receptor
ChEMBL 256 2 2 4 1.1 CCn1c(=O)[nH]c2[nH]c(-c3ccccc3)nc2c1=O 10.1021/jm011049y
11591029 141296 None 0 Human Binding pKi = 7.7 7.7 1 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 476 9 3 7 3.7 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccccc4O)cc3)cc2n(CCC)c1=O 10.1021/jm0506221
CHEMBL383321 141296 None 0 Human Binding pKi = 7.7 7.7 1 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 476 9 3 7 3.7 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccccc4O)cc3)cc2n(CCC)c1=O 10.1021/jm0506221
46228022 199909 None 0 Human Binding pKi = 7.7 7.7 6 3
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 368 6 0 8 2.1 CCCn1c(=O)c2c(nc(Cc3ccco3)n2C)n(Cc2ccco2)c1=O 10.1016/j.bmc.2009.07.034
CHEMBL594734 199909 None 0 Human Binding pKi = 7.7 7.7 6 3
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 368 6 0 8 2.1 CCCn1c(=O)c2c(nc(Cc3ccco3)n2C)n(Cc2ccco2)c1=O 10.1016/j.bmc.2009.07.034
176407 4148 None 84 Human Binding pKi = 7.7 7.7 -34 6
Displacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cell membraneDisplacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cell membrane
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1016/j.bmc.2010.02.014
405 4148 None 84 Human Binding pKi = 7.7 7.7 -34 6
Displacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cell membraneDisplacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cell membrane
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1016/j.bmc.2010.02.014
CHEMBL113142 4148 None 84 Human Binding pKi = 7.7 7.7 -34 6
Displacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cell membraneDisplacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cell membrane
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1016/j.bmc.2010.02.014
DB08770 4148 None 84 Human Binding pKi = 7.7 7.7 -34 6
Displacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cell membraneDisplacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cell membrane
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1016/j.bmc.2010.02.014
11570614 140685 None 0 Human Binding pKi = 7.7 7.7 8 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 586 9 2 6 4.6 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(I)cc4)cc3)cc2n(CCC)c1=O 10.1021/jm0506221
CHEMBL381522 140685 None 0 Human Binding pKi = 7.7 7.7 8 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 586 9 2 6 4.6 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(I)cc4)cc3)cc2n(CCC)c1=O 10.1021/jm0506221
44185935 185533 None 0 Human Binding pKi = 7.7 7.7 4 4
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 417 5 2 6 1.7 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCCCC4)cc3)[nH]c2c1=O 10.1021/jm900413e
CHEMBL486281 185533 None 0 Human Binding pKi = 7.7 7.7 4 4
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 417 5 2 6 1.7 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCCCC4)cc3)[nH]c2c1=O 10.1021/jm900413e
11627494 72321 None 0 Human Binding pKi = 7.7 7.7 - 1
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 502 10 2 7 4.2 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(C(C)=O)cc4)cc3)cc2n(CCC)c1=O 10.1021/jm0506221
CHEMBL198403 72321 None 0 Human Binding pKi = 7.7 7.7 - 1
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 502 10 2 7 4.2 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(C(C)=O)cc4)cc3)cc2n(CCC)c1=O 10.1021/jm0506221
11517907 74697 None 0 Human Binding pKi = 7.7 7.7 - 1
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 444 5 3 7 2.1 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4nc5ccccc5[nH]4)cc3)cc2n(C)c1=O 10.1021/jm0506221
CHEMBL203043 74697 None 0 Human Binding pKi = 7.7 7.7 - 1
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 444 5 3 7 2.1 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4nc5ccccc5[nH]4)cc3)cc2n(C)c1=O 10.1021/jm0506221
44236603 157389 None 0 Human Binding pKi = 6.7 6.7 - 1
Displacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 minsDisplacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 mins
ChEMBL 446 6 2 8 1.9 CCCn1c(=O)c2[nH]c(-c3cnn(CC#Cc4cccc(C(=O)O)c4)c3)nc2n(CC)c1=O 10.1016/j.ejmech.2017.04.014
CHEMBL4078316 157389 None 0 Human Binding pKi = 6.7 6.7 - 1
Displacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 minsDisplacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 mins
ChEMBL 446 6 2 8 1.9 CCCn1c(=O)c2[nH]c(-c3cnn(CC#Cc4cccc(C(=O)O)c4)c3)nc2n(CC)c1=O 10.1016/j.ejmech.2017.04.014
1509337 49130 None 13 Human Binding pKi = 6.7 6.7 -10 3
Displacement of [3H]DPCPX from human A2B receptor expressed in cell membranes after 30 mins by beta-scintillation counting methodDisplacement of [3H]DPCPX from human A2B receptor expressed in cell membranes after 30 mins by beta-scintillation counting method
ChEMBL 324 5 1 7 2.2 COc1cccc(COC(=O)c2nn(-c3ccccc3)nc2N)c1 10.1021/acs.jmedchem.8b00204
CHEMBL1561896 49130 None 13 Human Binding pKi = 6.7 6.7 -10 3
Displacement of [3H]DPCPX from human A2B receptor expressed in cell membranes after 30 mins by beta-scintillation counting methodDisplacement of [3H]DPCPX from human A2B receptor expressed in cell membranes after 30 mins by beta-scintillation counting method
ChEMBL 324 5 1 7 2.2 COc1cccc(COC(=O)c2nn(-c3ccccc3)nc2N)c1 10.1021/acs.jmedchem.8b00204
46233161 200523 None 0 Human Binding pKi = 6.7 6.7 -2 4
Displacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells by microplate beta scintillation counterDisplacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells by microplate beta scintillation counter
ChEMBL 358 7 1 6 2.7 CCCn1c(=O)c2[nH]c(-c3ccccc3)nc2n(CCSCC)c1=O 10.1016/j.bmc.2010.01.028
CHEMBL598819 200523 None 0 Human Binding pKi = 6.7 6.7 -2 4
Displacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells by microplate beta scintillation counterDisplacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells by microplate beta scintillation counter
ChEMBL 358 7 1 6 2.7 CCCn1c(=O)c2[nH]c(-c3ccccc3)nc2n(CCSCC)c1=O 10.1016/j.bmc.2010.01.028
3286 3209 None 31 Human Binding pKi = 6.7 6.7 4 9
Displacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cell membrane preincubated for 4 hrs followed by [3H]PSB-603 addition and measured after 0.5 hrs by radioligand displacement assayDisplacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cell membrane preincubated for 4 hrs followed by [3H]PSB-603 addition and measured after 0.5 hrs by radioligand displacement assay
ChEMBL 350 4 3 6 0.7 CCCn1c(=O)[nH]c2c(c1=O)nc([nH]2)c1ccc(cc1)S(=O)(=O)O 10.1039/d2md00132b
5311479 3209 None 31 Human Binding pKi = 6.7 6.7 4 9
Displacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cell membrane preincubated for 4 hrs followed by [3H]PSB-603 addition and measured after 0.5 hrs by radioligand displacement assayDisplacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cell membrane preincubated for 4 hrs followed by [3H]PSB-603 addition and measured after 0.5 hrs by radioligand displacement assay
ChEMBL 350 4 3 6 0.7 CCCn1c(=O)[nH]c2c(c1=O)nc([nH]2)c1ccc(cc1)S(=O)(=O)O 10.1039/d2md00132b
CHEMBL8565 3209 None 31 Human Binding pKi = 6.7 6.7 4 9
Displacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cell membrane preincubated for 4 hrs followed by [3H]PSB-603 addition and measured after 0.5 hrs by radioligand displacement assayDisplacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cell membrane preincubated for 4 hrs followed by [3H]PSB-603 addition and measured after 0.5 hrs by radioligand displacement assay
ChEMBL 350 4 3 6 0.7 CCCn1c(=O)[nH]c2c(c1=O)nc([nH]2)c1ccc(cc1)S(=O)(=O)O 10.1039/d2md00132b
135404340 82397 None 0 Human Binding pKi = 5.7 5.7 -229 3
Displacement of [125I]3-(4-aminobenzyl)-8-phenyloxyacetate-1-propyl-xanthine from human adenosine A2B receptorDisplacement of [125I]3-(4-aminobenzyl)-8-phenyloxyacetate-1-propyl-xanthine from human adenosine A2B receptor
ChEMBL 427 7 2 4 4.1 CCCN1C(=O)N2C[C@@H](CC)N=C2c2[nH]c(C34CCC(CCC(=O)O)(CC3)CC4)nc21 10.1021/jm060539t
CHEMBL217268 82397 None 0 Human Binding pKi = 5.7 5.7 -229 3
Displacement of [125I]3-(4-aminobenzyl)-8-phenyloxyacetate-1-propyl-xanthine from human adenosine A2B receptorDisplacement of [125I]3-(4-aminobenzyl)-8-phenyloxyacetate-1-propyl-xanthine from human adenosine A2B receptor
ChEMBL 427 7 2 4 4.1 CCCN1C(=O)N2C[C@@H](CC)N=C2c2[nH]c(C34CCC(CCC(=O)O)(CC3)CC4)nc21 10.1021/jm060539t
11408692 75560 None 0 Human Binding pKi = 5.7 5.7 -2511 4
Displacement of [125I]ABOPX from human adenosine A2B receptor in HEK cellsDisplacement of [125I]ABOPX from human adenosine A2B receptor in HEK cells
ChEMBL 466 6 5 10 0.1 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC)nc(C#CC(O)c4ccccc4)nc32)[C@H](O)[C@@H]1O 10.1016/j.bmcl.2006.01.110
CHEMBL204527 75560 None 0 Human Binding pKi = 5.7 5.7 -2511 4
Displacement of [125I]ABOPX from human adenosine A2B receptor in HEK cellsDisplacement of [125I]ABOPX from human adenosine A2B receptor in HEK cells
ChEMBL 466 6 5 10 0.1 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC)nc(C#CC(O)c4ccccc4)nc32)[C@H](O)[C@@H]1O 10.1016/j.bmcl.2006.01.110
3467695 90944 None 41 Human Binding pKi = 5.7 5.7 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 328 4 2 4 3.1 CC1=C(C(=O)OCc2ccccc2)C(c2cccs2)NC(=O)N1 10.1021/acs.jmedchem.0c01431
CHEMBL239336 90944 None 41 Human Binding pKi = 5.7 5.7 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 328 4 2 4 3.1 CC1=C(C(=O)OCc2ccccc2)C(c2cccs2)NC(=O)N1 10.1021/acs.jmedchem.0c01431
21874668 176890 None 0 Human Binding pKi = 6.7 6.7 -21 4
Displacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation countingDisplacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation counting
ChEMBL 282 3 1 8 1.7 Nc1nc(-c2ccco2)c2nnn(Cc3ccco3)c2n1 10.1021/jm800961g
CHEMBL461650 176890 None 0 Human Binding pKi = 6.7 6.7 -21 4
Displacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation countingDisplacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation counting
ChEMBL 282 3 1 8 1.7 Nc1nc(-c2ccco2)c2nnn(Cc3ccco3)c2n1 10.1021/jm800961g
145986422 167146 None 0 Human Binding pKi = 6.7 6.7 -1 4
Displacement of [3H]PSB-602 from human adenosine A2B receptor expressed in CHO cell membranesDisplacement of [3H]PSB-602 from human adenosine A2B receptor expressed in CHO cell membranes
ChEMBL 565 13 1 10 2.2 CCCn1c(=O)c2c(nc3n2CCCN3CCc2ccc(OCC(=O)NCCN3CCCC3)cc2)n(CCC)c1=O 10.1039/C8MD00070K
CHEMBL4290710 167146 None 0 Human Binding pKi = 6.7 6.7 -1 4
Displacement of [3H]PSB-602 from human adenosine A2B receptor expressed in CHO cell membranesDisplacement of [3H]PSB-602 from human adenosine A2B receptor expressed in CHO cell membranes
ChEMBL 565 13 1 10 2.2 CCCn1c(=O)c2c(nc3n2CCCN3CCc2ccc(OCC(=O)NCCN3CCCC3)cc2)n(CCC)c1=O 10.1039/C8MD00070K
76313652 103846 None 0 Human Binding pKi = 6.7 6.7 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 280 3 2 4 2.0 CC1=C(C(=O)OC(C)C)C(c2ccoc2)NC(=S)N1 10.1021/acs.jmedchem.0c01431
CHEMBL3091701 103846 None 0 Human Binding pKi = 6.7 6.7 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 280 3 2 4 2.0 CC1=C(C(=O)OC(C)C)C(c2ccoc2)NC(=S)N1 10.1021/acs.jmedchem.0c01431
76313652 103846 None 0 Human Binding pKi = 6.7 6.7 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by Scatchard plot analysisDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by Scatchard plot analysis
ChEMBL 280 3 2 4 2.0 CC1=C(C(=O)OC(C)C)C(c2ccoc2)NC(=S)N1 10.1021/ml400185v
CHEMBL3091701 103846 None 0 Human Binding pKi = 6.7 6.7 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by Scatchard plot analysisDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by Scatchard plot analysis
ChEMBL 280 3 2 4 2.0 CC1=C(C(=O)OC(C)C)C(c2ccoc2)NC(=S)N1 10.1021/ml400185v
3286 3209 None 31 Human Binding pKi = 6.7 6.7 4 9
Displacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cell membrane and measured after 0.5 hrs by radioligand displacement assayDisplacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cell membrane and measured after 0.5 hrs by radioligand displacement assay
ChEMBL 350 4 3 6 0.7 CCCn1c(=O)[nH]c2c(c1=O)nc([nH]2)c1ccc(cc1)S(=O)(=O)O 10.1039/d2md00132b
5311479 3209 None 31 Human Binding pKi = 6.7 6.7 4 9
Displacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cell membrane and measured after 0.5 hrs by radioligand displacement assayDisplacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cell membrane and measured after 0.5 hrs by radioligand displacement assay
ChEMBL 350 4 3 6 0.7 CCCn1c(=O)[nH]c2c(c1=O)nc([nH]2)c1ccc(cc1)S(=O)(=O)O 10.1039/d2md00132b
CHEMBL8565 3209 None 31 Human Binding pKi = 6.7 6.7 4 9
Displacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cell membrane and measured after 0.5 hrs by radioligand displacement assayDisplacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cell membrane and measured after 0.5 hrs by radioligand displacement assay
ChEMBL 350 4 3 6 0.7 CCCn1c(=O)[nH]c2c(c1=O)nc([nH]2)c1ccc(cc1)S(=O)(=O)O 10.1039/d2md00132b
3286 3209 None 31 Mouse Binding pKi = 5.7 5.7 -16 9
Displacement of [3H]PSB-603 from recombinant mouse A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant mouse A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins by liquid scintillation counting method
ChEMBL 350 4 3 6 0.7 CCCn1c(=O)[nH]c2c(c1=O)nc([nH]2)c1ccc(cc1)S(=O)(=O)O 10.1021/acs.jmedchem.9b00071
5311479 3209 None 31 Mouse Binding pKi = 5.7 5.7 -16 9
Displacement of [3H]PSB-603 from recombinant mouse A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant mouse A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins by liquid scintillation counting method
ChEMBL 350 4 3 6 0.7 CCCn1c(=O)[nH]c2c(c1=O)nc([nH]2)c1ccc(cc1)S(=O)(=O)O 10.1021/acs.jmedchem.9b00071
CHEMBL8565 3209 None 31 Mouse Binding pKi = 5.7 5.7 -16 9
Displacement of [3H]PSB-603 from recombinant mouse A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant mouse A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins by liquid scintillation counting method
ChEMBL 350 4 3 6 0.7 CCCn1c(=O)[nH]c2c(c1=O)nc([nH]2)c1ccc(cc1)S(=O)(=O)O 10.1021/acs.jmedchem.9b00071
95028 93808 None 31 Human Binding pKi = 4.7 4.7 -3 4
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 270 2 0 6 0.5 Cn1c(=O)c2c(ncn2Cc2ccccc2)n(C)c1=O 10.1021/jm0104318
CHEMBL24759 93808 None 31 Human Binding pKi = 4.7 4.7 -3 4
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 270 2 0 6 0.5 Cn1c(=O)c2c(ncn2Cc2ccccc2)n(C)c1=O 10.1021/jm0104318
44406334 72932 None 0 Human Binding pKi = 6.7 6.7 16 3
Displacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cellsDisplacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cells
ChEMBL 489 9 1 10 3.3 CCCn1c(=O)c2nc(-c3cnn(Cc4cc(-c5ccccc5OC)on4)c3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2005.10.002
CHEMBL200509 72932 None 0 Human Binding pKi = 6.7 6.7 16 3
Displacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cellsDisplacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cells
ChEMBL 489 9 1 10 3.3 CCCn1c(=O)c2nc(-c3cnn(Cc4cc(-c5ccccc5OC)on4)c3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2005.10.002
11112543 57153 None 0 Human Binding pKi = 6.7 6.7 -10 4
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 162-237Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 162-237
ChEMBL 418 5 2 9 3.4 CCn1cc2c(nc(NC(=O)Nc3ccccc3OC)n3nc(-c4ccco4)nc23)n1 10.1021/jm0109614
CHEMBL164647 57153 None 0 Human Binding pKi = 6.7 6.7 -10 4
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 162-237Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 162-237
ChEMBL 418 5 2 9 3.4 CCn1cc2c(nc(NC(=O)Nc3ccccc3OC)n3nc(-c4ccco4)nc23)n1 10.1021/jm0109614
2748296 182154 None 8 Human Binding pKi = 6.7 6.7 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 278 4 2 4 2.1 CC1=C(C(=O)OCC(C)C)C(c2ccco2)NC(=O)N1 10.1021/acs.jmedchem.0c01431
CHEMBL4782393 182154 None 8 Human Binding pKi = 6.7 6.7 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 278 4 2 4 2.1 CC1=C(C(=O)OCC(C)C)C(c2ccco2)NC(=O)N1 10.1021/acs.jmedchem.0c01431
11267343 175350 None 0 Human Binding pKi = 6.7 6.7 3 2
Displacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cells
ChEMBL 325 5 1 4 3.3 CCCn1c(=O)c2[nH]c(-c3ccc(C)cc3)cc2n(CCC)c1=O 10.1016/j.bmc.2008.09.067
CHEMBL457442 175350 None 0 Human Binding pKi = 6.7 6.7 3 2
Displacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cells
ChEMBL 325 5 1 4 3.3 CCCn1c(=O)c2[nH]c(-c3ccc(C)cc3)cc2n(CCC)c1=O 10.1016/j.bmc.2008.09.067
21916371 95883 None 0 Human Binding pKi = 6.7 6.7 3 3
Displacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 446 5 1 7 3.0 CC(C)Cn1c(=O)c2[nH]c(-c3cnn(Cc4cccc(C(F)(F)F)c4)c3)nc2n(C)c1=O 10.1021/jm7014815
CHEMBL259129 95883 None 0 Human Binding pKi = 6.7 6.7 3 3
Displacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 446 5 1 7 3.0 CC(C)Cn1c(=O)c2[nH]c(-c3cnn(Cc4cccc(C(F)(F)F)c4)c3)nc2n(C)c1=O 10.1021/jm7014815
9902562 172635 None 0 Human Binding pKi = 6.7 6.7 -23 4
Displacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation countingDisplacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation counting
ChEMBL 341 3 1 8 2.4 Cc1cnc(-c2nc(N)nc3c2nnn3Cc2ccccc2F)s1 10.1021/jm800961g
CHEMBL449469 172635 None 0 Human Binding pKi = 6.7 6.7 -23 4
Displacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation countingDisplacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation counting
ChEMBL 341 3 1 8 2.4 Cc1cnc(-c2nc(N)nc3c2nnn3Cc2ccccc2F)s1 10.1021/jm800961g
11649548 72781 None 0 Human Binding pKi = 6.7 6.7 - 1
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 539 10 3 8 2.6 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(S(N)(=O)=O)cc4)cc3)cc2n(CCC)c1=O 10.1021/jm0506221
CHEMBL200011 72781 None 0 Human Binding pKi = 6.7 6.7 - 1
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 539 10 3 8 2.6 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(S(N)(=O)=O)cc4)cc3)cc2n(CCC)c1=O 10.1021/jm0506221
46227958 200114 None 0 Human Binding pKi = 6.7 6.7 1 3
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 432 7 1 7 2.8 CSCCn1c(=O)c2[nH]c(Cc3c(F)cccc3F)nc2n(Cc2ccco2)c1=O 10.1016/j.bmc.2009.07.034
CHEMBL596125 200114 None 0 Human Binding pKi = 6.7 6.7 1 3
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 432 7 1 7 2.8 CSCCn1c(=O)c2[nH]c(Cc3c(F)cccc3F)nc2n(Cc2ccco2)c1=O 10.1016/j.bmc.2009.07.034
45268854 196067 None 0 Human Binding pKi = 5.7 5.7 - 1
Binding affinity to human adenosine A2b receptor expressed in HEK293 cellsBinding affinity to human adenosine A2b receptor expressed in HEK293 cells
ChEMBL 392 10 1 8 1.9 CCSCCn1c(=O)c2[nH]c(Cc3ccco3)nc2n(CCCOC)c1=O 10.1016/j.bmc.2009.03.029
CHEMBL560562 196067 None 0 Human Binding pKi = 5.7 5.7 - 1
Binding affinity to human adenosine A2b receptor expressed in HEK293 cellsBinding affinity to human adenosine A2b receptor expressed in HEK293 cells
ChEMBL 392 10 1 8 1.9 CCSCCn1c(=O)c2[nH]c(Cc3ccco3)nc2n(CCCOC)c1=O 10.1016/j.bmc.2009.03.029
19574107 75441 None 0 Human Binding pKi = 4.7 4.7 -50 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by beta scintillation countingDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by beta scintillation counting
ChEMBL 300 3 2 4 3.0 COc1cccc2cc(C(=O)NC3CCCCC3)c(=N)oc12 10.1016/j.ejmech.2012.05.009
CHEMBL2042059 75441 None 0 Human Binding pKi = 4.7 4.7 -50 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by beta scintillation countingDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by beta scintillation counting
ChEMBL 300 3 2 4 3.0 COc1cccc2cc(C(=O)NC3CCCCC3)c(=N)oc12 10.1016/j.ejmech.2012.05.009
449 2643 None 52 Human Binding pKi = 8.7 8.7 -1 9
Binding affinity against Adenosine A2b receptor labeled by [3H]ZM-241385 in membranes prepared from HEK-A2B cellsBinding affinity against Adenosine A2b receptor labeled by [3H]ZM-241385 in membranes prepared from HEK-A2B cells
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10.1016/j.bmcl.2004.11.044
453 2643 None 52 Human Binding pKi = 8.7 8.7 -1 9
Binding affinity against Adenosine A2b receptor labeled by [3H]ZM-241385 in membranes prepared from HEK-A2B cellsBinding affinity against Adenosine A2b receptor labeled by [3H]ZM-241385 in membranes prepared from HEK-A2B cells
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10.1016/j.bmcl.2004.11.044
6603931 2643 None 52 Human Binding pKi = 8.7 8.7 -1 9
Binding affinity against Adenosine A2b receptor labeled by [3H]ZM-241385 in membranes prepared from HEK-A2B cellsBinding affinity against Adenosine A2b receptor labeled by [3H]ZM-241385 in membranes prepared from HEK-A2B cells
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10.1016/j.bmcl.2004.11.044
CHEMBL273807 2643 None 52 Human Binding pKi = 8.7 8.7 -1 9
Binding affinity against Adenosine A2b receptor labeled by [3H]ZM-241385 in membranes prepared from HEK-A2B cellsBinding affinity against Adenosine A2b receptor labeled by [3H]ZM-241385 in membranes prepared from HEK-A2B cells
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10.1016/j.bmcl.2004.11.044
449 2643 None 52 Human Binding pKi = 8.7 8.7 -1 9
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10.1021/jm201292w
453 2643 None 52 Human Binding pKi = 8.7 8.7 -1 9
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10.1021/jm201292w
6603931 2643 None 52 Human Binding pKi = 8.7 8.7 -1 9
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10.1021/jm201292w
CHEMBL273807 2643 None 52 Human Binding pKi = 8.7 8.7 -1 9
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10.1021/jm201292w
449 2643 None 52 Human Binding pKi = 8.7 8.7 -1 9
Displacement of [125I]ABOPX from human adenosine receptor A2b expressed in HEK293 cell membranes after 3 hrs by fluorescence assayDisplacement of [125I]ABOPX from human adenosine receptor A2b expressed in HEK293 cell membranes after 3 hrs by fluorescence assay
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10.1016/j.ejmech.2016.11.007
453 2643 None 52 Human Binding pKi = 8.7 8.7 -1 9
Displacement of [125I]ABOPX from human adenosine receptor A2b expressed in HEK293 cell membranes after 3 hrs by fluorescence assayDisplacement of [125I]ABOPX from human adenosine receptor A2b expressed in HEK293 cell membranes after 3 hrs by fluorescence assay
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10.1016/j.ejmech.2016.11.007
6603931 2643 None 52 Human Binding pKi = 8.7 8.7 -1 9
Displacement of [125I]ABOPX from human adenosine receptor A2b expressed in HEK293 cell membranes after 3 hrs by fluorescence assayDisplacement of [125I]ABOPX from human adenosine receptor A2b expressed in HEK293 cell membranes after 3 hrs by fluorescence assay
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10.1016/j.ejmech.2016.11.007
CHEMBL273807 2643 None 52 Human Binding pKi = 8.7 8.7 -1 9
Displacement of [125I]ABOPX from human adenosine receptor A2b expressed in HEK293 cell membranes after 3 hrs by fluorescence assayDisplacement of [125I]ABOPX from human adenosine receptor A2b expressed in HEK293 cell membranes after 3 hrs by fluorescence assay
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10.1016/j.ejmech.2016.11.007
44451329 96183 None 0 Human Binding pKi = 8.7 8.7 204 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 501 5 1 7 2.7 Cc1ccc(N2CCN(C(=O)C(C)Oc3ccc(-c4cc5c([nH]4)c(=O)n(C)c(=O)n5C)cc3)CC2)cc1 10.1016/j.bmc.2008.01.002
CHEMBL260692 96183 None 0 Human Binding pKi = 8.7 8.7 204 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 501 5 1 7 2.7 Cc1ccc(N2CCN(C(=O)C(C)Oc3ccc(-c4cc5c([nH]4)c(=O)n(C)c(=O)n5C)cc3)CC2)cc1 10.1016/j.bmc.2008.01.002
44451127 161280 None 0 Human Binding pKi = 8.7 8.7 44 4
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 569 7 1 7 3.9 CCCn1c(=O)n(C)c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCN(c5ccc(C(F)(F)F)cc5)CC4)cc3)cc21 10.1016/j.bmc.2008.01.002
CHEMBL412112 161280 None 0 Human Binding pKi = 8.7 8.7 44 4
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 569 7 1 7 3.9 CCCn1c(=O)n(C)c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCN(c5ccc(C(F)(F)F)cc5)CC4)cc3)cc21 10.1016/j.bmc.2008.01.002
46880475 5535 None 0 Human Binding pKi = 8.7 8.7 7 4
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 333 4 1 3 4.3 O=C(Nc1ccc(-c2ccncc2)c(-c2cccc(F)c2)n1)C1CC1 10.1016/j.bmcl.2010.01.045
CHEMBL1076587 5535 None 0 Human Binding pKi = 8.7 8.7 7 4
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 333 4 1 3 4.3 O=C(Nc1ccc(-c2ccncc2)c(-c2cccc(F)c2)n1)C1CC1 10.1016/j.bmcl.2010.01.045
46880474 6347 None 0 Human Binding pKi = 8.7 8.7 30 4
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 333 4 1 3 4.3 O=C(Nc1ccc(-c2ccncc2)c(-c2ccccc2F)n1)C1CC1 10.1016/j.bmcl.2010.01.045
CHEMBL1082028 6347 None 0 Human Binding pKi = 8.7 8.7 30 4
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 333 4 1 3 4.3 O=C(Nc1ccc(-c2ccncc2)c(-c2ccccc2F)n1)C1CC1 10.1016/j.bmcl.2010.01.045
53318745 58031 None 0 Human Binding pKi = 8.7 8.7 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 325 4 1 6 2.7 O=C(Nc1cnc(-c2ccncc2F)c(-c2cnco2)n1)C1CC1 10.1021/ml100249e
CHEMBL1672633 58031 None 0 Human Binding pKi = 8.7 8.7 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 325 4 1 6 2.7 O=C(Nc1cnc(-c2ccncc2F)c(-c2cnco2)n1)C1CC1 10.1021/ml100249e
44574222 189308 None 0 Human Binding pKi = 8.7 8.7 -5 4
Displacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells by beta scintillation counterDisplacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells by beta scintillation counter
ChEMBL 478 8 2 6 4.9 CCCn1c(=O)c2[nH]c(-c3ccc(COC(=O)Nc4ccc(F)cc4)cc3)cc2n(CCC)c1=O 10.1016/j.bmc.2009.03.062
CHEMBL512276 189308 None 0 Human Binding pKi = 8.7 8.7 -5 4
Displacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells by beta scintillation counterDisplacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells by beta scintillation counter
ChEMBL 478 8 2 6 4.9 CCCn1c(=O)c2[nH]c(-c3ccc(COC(=O)Nc4ccc(F)cc4)cc3)cc2n(CCC)c1=O 10.1016/j.bmc.2009.03.062
22266746 157764 None 0 Human Binding pKi = 8.7 8.7 36 4
Displacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 350 4 1 7 1.4 CCn1c(=O)c2[nH]c(-c3cnn(Cc4ccccc4)c3)nc2n(C)c1=O 10.1021/jm7014815
CHEMBL408266 157764 None 0 Human Binding pKi = 8.7 8.7 36 4
Displacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 350 4 1 7 1.4 CCn1c(=O)c2[nH]c(-c3cnn(Cc4ccccc4)c3)nc2n(C)c1=O 10.1021/jm7014815
449 2643 None 52 Human Binding pKi = 8.7 8.7 -1 9
Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cellsDisplacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10.1021/jm051268+
453 2643 None 52 Human Binding pKi = 8.7 8.7 -1 9
Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cellsDisplacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10.1021/jm051268+
6603931 2643 None 52 Human Binding pKi = 8.7 8.7 -1 9
Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cellsDisplacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10.1021/jm051268+
CHEMBL273807 2643 None 52 Human Binding pKi = 8.7 8.7 -1 9
Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cellsDisplacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10.1021/jm051268+
449 2643 None 52 Human Binding pKi = 8.7 8.7 -1 9
Inhibition of human A2B adenosine receptorInhibition of human A2B adenosine receptor
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10.1016/j.ejmech.2018.11.045
453 2643 None 52 Human Binding pKi = 8.7 8.7 -1 9
Inhibition of human A2B adenosine receptorInhibition of human A2B adenosine receptor
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10.1016/j.ejmech.2018.11.045
6603931 2643 None 52 Human Binding pKi = 8.7 8.7 -1 9
Inhibition of human A2B adenosine receptorInhibition of human A2B adenosine receptor
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10.1016/j.ejmech.2018.11.045
CHEMBL273807 2643 None 52 Human Binding pKi = 8.7 8.7 -1 9
Inhibition of human A2B adenosine receptorInhibition of human A2B adenosine receptor
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10.1016/j.ejmech.2018.11.045
44451127 161280 None 0 Human Binding pKi = 8.7 8.7 44 4
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 569 7 1 7 3.9 CCCn1c(=O)n(C)c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCN(c5ccc(C(F)(F)F)cc5)CC4)cc3)cc21 10.1016/j.bmc.2008.01.002
CHEMBL412112 161280 None 0 Human Binding pKi = 8.7 8.7 44 4
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 569 7 1 7 3.9 CCCn1c(=O)n(C)c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCN(c5ccc(C(F)(F)F)cc5)CC4)cc3)cc21 10.1016/j.bmc.2008.01.002
44574192 178810 None 0 Human Binding pKi = 8.7 8.7 20 2
Displacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells by beta scintillation counterDisplacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells by beta scintillation counter
ChEMBL 444 3 1 6 2.9 Cn1c(=O)c2[nH]c(-c3ccc(COC(=O)N4CCc5ccccc5C4)cc3)cc2n(C)c1=O 10.1016/j.bmc.2009.03.062
CHEMBL469136 178810 None 0 Human Binding pKi = 8.7 8.7 20 2
Displacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells by beta scintillation counterDisplacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells by beta scintillation counter
ChEMBL 444 3 1 6 2.9 Cn1c(=O)c2[nH]c(-c3ccc(COC(=O)N4CCc5ccccc5C4)cc3)cc2n(C)c1=O 10.1016/j.bmc.2009.03.062
11801496 98746 None 0 Human Binding pKi = 8.7 8.7 7 6
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 587 9 2 7 4.0 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccc(I)cc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm0506221
CHEMBL278039 98746 None 0 Human Binding pKi = 8.7 8.7 7 6
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 587 9 2 7 4.0 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccc(I)cc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm0506221
168297247 192377 None 0 Human Binding pKi = 8.7 8.7 - 1
Displacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cell membrane and measured after 0.5 hrs by radioligand displacement assayDisplacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cell membrane and measured after 0.5 hrs by radioligand displacement assay
ChEMBL 327 4 2 6 2.2 CCCn1c(=O)[nH]c2nc(-c3ccc(N=C=S)cc3)[nH]c2c1=O 10.1039/d2md00132b
CHEMBL5207498 192377 None 0 Human Binding pKi = 8.7 8.7 - 1
Displacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cell membrane and measured after 0.5 hrs by radioligand displacement assayDisplacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cell membrane and measured after 0.5 hrs by radioligand displacement assay
ChEMBL 327 4 2 6 2.2 CCCn1c(=O)[nH]c2nc(-c3ccc(N=C=S)cc3)[nH]c2c1=O 10.1039/d2md00132b
11649544 73133 None 0 Human Binding pKi = 8.7 8.7 9 4
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 538 9 2 6 4.8 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(Br)cc4)cc3)cc2n(CCC)c1=O 10.1021/jm0506221
CHEMBL201145 73133 None 0 Human Binding pKi = 8.7 8.7 9 4
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 538 9 2 6 4.8 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(Br)cc4)cc3)cc2n(CCC)c1=O 10.1021/jm0506221
57429615 159752 None 0 Human Binding pKi = 8.7 8.7 - 1
Displacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 minsDisplacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 mins
ChEMBL 442 4 2 6 2.8 CCCn1c(=O)[nH]c2nc(-c3cnn(CC#Cc4cccc(C(F)(F)F)c4)c3)[nH]c2c1=O 10.1016/j.ejmech.2017.04.014
CHEMBL4105001 159752 None 0 Human Binding pKi = 8.7 8.7 - 1
Displacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 minsDisplacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 mins
ChEMBL 442 4 2 6 2.8 CCCn1c(=O)[nH]c2nc(-c3cnn(CC#Cc4cccc(C(F)(F)F)c4)c3)[nH]c2c1=O 10.1016/j.ejmech.2017.04.014
16072021 58009 None 0 Human Binding pKi = 8.7 8.7 19 4
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 306 4 1 5 3.1 O=C(Nc1cnc(-c2ccncc2)c(-c2ccco2)n1)C1CC1 10.1021/ml100249e
CHEMBL1672611 58009 None 0 Human Binding pKi = 8.7 8.7 19 4
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 306 4 1 5 3.1 O=C(Nc1cnc(-c2ccncc2)c(-c2ccco2)n1)C1CC1 10.1021/ml100249e
16071777 58017 None 0 Human Binding pKi = 8.7 8.7 -1 4
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 320 4 1 5 3.5 Cc1ccc(-c2nc(NC(=O)C3CC3)cnc2-c2ccncc2)o1 10.1021/ml100249e
CHEMBL1672619 58017 None 0 Human Binding pKi = 8.7 8.7 -1 4
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 320 4 1 5 3.5 Cc1ccc(-c2nc(NC(=O)C3CC3)cnc2-c2ccncc2)o1 10.1021/ml100249e
11649544 73133 None 0 Human Binding pKi = 8.7 8.7 9 4
Displacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cells
ChEMBL 538 9 2 6 4.8 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(Br)cc4)cc3)cc2n(CCC)c1=O 10.1016/j.bmc.2008.09.067
CHEMBL201145 73133 None 0 Human Binding pKi = 8.7 8.7 9 4
Displacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cells
ChEMBL 538 9 2 6 4.8 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(Br)cc4)cc3)cc2n(CCC)c1=O 10.1016/j.bmc.2008.09.067
10767043 59023 None 0 Human Binding pKi = 8.7 8.7 7 6
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 479 9 2 7 3.5 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccc(F)cc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm0506221
CHEMBL16929 59023 None 0 Human Binding pKi = 8.7 8.7 7 6
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 479 9 2 7 3.5 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccc(F)cc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm0506221
9827315 95846 None 0 Human Binding pKi = 8.6 8.6 40 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 500 8 1 6 3.9 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCc5ccccc5C4)cc3)cc2n(CCC)c1=O 10.1016/j.bmc.2008.01.002
CHEMBL258978 95846 None 0 Human Binding pKi = 8.6 8.6 40 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 500 8 1 6 3.9 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCc5ccccc5C4)cc3)cc2n(CCC)c1=O 10.1016/j.bmc.2008.01.002
46837704 10623 None 0 Human Binding pKi = 8.6 8.6 32 3
Displacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells after 30 minsDisplacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells after 30 mins
ChEMBL 436 7 3 5 3.3 CCCn1c(=O)[nH]c2cc(-c3ccc(OCC(=O)Nc4ccc(F)cc4)cc3)[nH]c2c1=O 10.1016/j.ejmech.2010.03.011
CHEMBL1170166 10623 None 0 Human Binding pKi = 8.6 8.6 32 3
Displacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells after 30 minsDisplacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells after 30 mins
ChEMBL 436 7 3 5 3.3 CCCn1c(=O)[nH]c2cc(-c3ccc(OCC(=O)Nc4ccc(F)cc4)cc3)[nH]c2c1=O 10.1016/j.ejmech.2010.03.011
10840167 59178 None 0 Human Binding pKi = 8.6 8.6 3 6
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 539 9 2 7 4.2 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccc(Br)cc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm0506221
CHEMBL17003 59178 None 0 Human Binding pKi = 8.6 8.6 3 6
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 539 9 2 7 4.2 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccc(Br)cc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm0506221
168271107 190069 None 0 Human Binding pKi = 8.6 8.6 - 1
Displacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cell membrane preincubated for 4 hrs followed by [3H]PSB-603 addition and measured after 0.5 hrs by radioligand displacement assayDisplacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cell membrane preincubated for 4 hrs followed by [3H]PSB-603 addition and measured after 0.5 hrs by radioligand displacement assay
ChEMBL 394 6 1 7 2.0 CCCn1c(=O)c2[nH]c(-c3ccc(S(=O)(=O)F)cc3)nc2n(CCC)c1=O 10.1039/d2md00132b
CHEMBL5172513 190069 None 0 Human Binding pKi = 8.6 8.6 - 1
Displacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cell membrane preincubated for 4 hrs followed by [3H]PSB-603 addition and measured after 0.5 hrs by radioligand displacement assayDisplacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cell membrane preincubated for 4 hrs followed by [3H]PSB-603 addition and measured after 0.5 hrs by radioligand displacement assay
ChEMBL 394 6 1 7 2.0 CCCn1c(=O)c2[nH]c(-c3ccc(S(=O)(=O)F)cc3)nc2n(CCC)c1=O 10.1039/d2md00132b
44450997 96035 None 0 Human Binding pKi = 8.6 8.6 398 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 500 7 1 6 3.9 CCCn1c(=O)n(C)c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCC(c5ccccc5)CC4)cc3)cc21 10.1016/j.bmc.2008.01.002
CHEMBL259857 96035 None 0 Human Binding pKi = 8.6 8.6 398 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 500 7 1 6 3.9 CCCn1c(=O)n(C)c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCC(c5ccccc5)CC4)cc3)cc21 10.1016/j.bmc.2008.01.002
11123022 132125 None 0 Human Binding pKi = 8.6 8.6 -1 3
Inhibition of [3H]ZM-241385 binding to human adenosine A2B receptorInhibition of [3H]ZM-241385 binding to human adenosine A2B receptor
ChEMBL 438 5 1 5 3.0 CCCn1c(=O)c2nc(-c3ccc(I)cc3)[nH]c2n(CCC)c1=O 10.1021/jm011049y
CHEMBL36963 132125 None 0 Human Binding pKi = 8.6 8.6 -1 3
Inhibition of [3H]ZM-241385 binding to human adenosine A2B receptorInhibition of [3H]ZM-241385 binding to human adenosine A2B receptor
ChEMBL 438 5 1 5 3.0 CCCn1c(=O)c2nc(-c3ccc(I)cc3)[nH]c2n(CCC)c1=O 10.1021/jm011049y
44450997 96035 None 0 Human Binding pKi = 8.6 8.6 398 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 500 7 1 6 3.9 CCCn1c(=O)n(C)c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCC(c5ccccc5)CC4)cc3)cc21 10.1016/j.bmc.2008.01.002
CHEMBL259857 96035 None 0 Human Binding pKi = 8.6 8.6 398 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 500 7 1 6 3.9 CCCn1c(=O)n(C)c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCC(c5ccccc5)CC4)cc3)cc21 10.1016/j.bmc.2008.01.002
76321753 105514 None 0 Human Binding pKi = 8.6 8.6 -10 4
Binding affinity to human recombinant adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated adenylyl cyclase activity after 20 minsBinding affinity to human recombinant adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated adenylyl cyclase activity after 20 mins
ChEMBL 371 7 1 7 1.3 CCN(CC)CCOc1ccc(-c2nc3c([nH]2)c(=O)n(C)c(=O)n3C)cc1 10.1016/j.ejmech.2014.01.045
CHEMBL3121721 105514 None 0 Human Binding pKi = 8.6 8.6 -10 4
Binding affinity to human recombinant adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated adenylyl cyclase activity after 20 minsBinding affinity to human recombinant adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated adenylyl cyclase activity after 20 mins
ChEMBL 371 7 1 7 1.3 CCN(CC)CCOc1ccc(-c2nc3c([nH]2)c(=O)n(C)c(=O)n3C)cc1 10.1016/j.ejmech.2014.01.045
57429644 159346 None 0 Human Binding pKi = 8.6 8.6 - 1
Displacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting methodDisplacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting method
ChEMBL 557 9 1 8 4.0 CCCn1c(=O)c2[nH]c(-c3cnn(CCC4CC(=O)N(c5cccc(C(F)(F)F)c5)C4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2016.11.007
CHEMBL4100199 159346 None 0 Human Binding pKi = 8.6 8.6 - 1
Displacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting methodDisplacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting method
ChEMBL 557 9 1 8 4.0 CCCn1c(=O)c2[nH]c(-c3cnn(CCC4CC(=O)N(c5cccc(C(F)(F)F)c5)C4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2016.11.007
44587957 188814 None 0 Human Binding pKi = 8.6 8.6 35 4
Displacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cells
ChEMBL 559 10 2 8 3.4 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCN(Cc5ccccc5)CC4)cc3)c(O)c2n(CCC)c1=O 10.1016/j.bmc.2008.09.067
CHEMBL506179 188814 None 0 Human Binding pKi = 8.6 8.6 35 4
Displacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cells
ChEMBL 559 10 2 8 3.4 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCN(Cc5ccccc5)CC4)cc3)c(O)c2n(CCC)c1=O 10.1016/j.bmc.2008.09.067
11684443 133159 None 0 Human Binding pKi = 8.6 8.6 4 4
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 482 5 2 6 3.0 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(Br)cc4)cc3)cc2n(C)c1=O 10.1021/jm0506221
CHEMBL370378 133159 None 0 Human Binding pKi = 8.6 8.6 4 4
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 482 5 2 6 3.0 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(Br)cc4)cc3)cc2n(C)c1=O 10.1021/jm0506221
11684443 133159 None 0 Human Binding pKi = 8.6 8.6 4 4
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 482 5 2 6 3.0 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(Br)cc4)cc3)cc2n(C)c1=O 10.1016/j.bmc.2008.01.002
CHEMBL370378 133159 None 0 Human Binding pKi = 8.6 8.6 4 4
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 482 5 2 6 3.0 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(Br)cc4)cc3)cc2n(C)c1=O 10.1016/j.bmc.2008.01.002
11111247 119731 None 0 Human Binding pKi = 8.6 8.6 4 3
Inhibition of [3H]ZM-241385 binding to human adenosine A2B receptorInhibition of [3H]ZM-241385 binding to human adenosine A2B receptor
ChEMBL 362 4 2 4 2.6 CCCCn1c(=O)[nH]c2[nH]c(-c3ccc(Br)cc3)nc2c1=O 10.1021/jm011049y
CHEMBL34762 119731 None 0 Human Binding pKi = 8.6 8.6 4 3
Inhibition of [3H]ZM-241385 binding to human adenosine A2B receptorInhibition of [3H]ZM-241385 binding to human adenosine A2B receptor
ChEMBL 362 4 2 4 2.6 CCCCn1c(=O)[nH]c2[nH]c(-c3ccc(Br)cc3)nc2c1=O 10.1021/jm011049y
72197880 90798 None 0 Human Binding pKi = 8.6 8.6 -4 4
Displacement of [3H]PSB-603 from human adenosine receptor A2B expressed in CHO cell membranes incubated for 75 mins by radioligand competition assayDisplacement of [3H]PSB-603 from human adenosine receptor A2B expressed in CHO cell membranes incubated for 75 mins by radioligand competition assay
ChEMBL 347 4 1 5 4.7 O=C(Nc1nc(-c2ccccc2)c(-c2ccncc2)s1)c1ccco1 10.1016/j.ejmech.2019.111879
CHEMBL2391834 90798 None 0 Human Binding pKi = 8.6 8.6 -4 4
Displacement of [3H]PSB-603 from human adenosine receptor A2B expressed in CHO cell membranes incubated for 75 mins by radioligand competition assayDisplacement of [3H]PSB-603 from human adenosine receptor A2B expressed in CHO cell membranes incubated for 75 mins by radioligand competition assay
ChEMBL 347 4 1 5 4.7 O=C(Nc1nc(-c2ccccc2)c(-c2ccncc2)s1)c1ccco1 10.1016/j.ejmech.2019.111879
57429616 157682 None 0 Human Binding pKi = 8.6 8.6 - 1
Displacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 minsDisplacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 mins
ChEMBL 458 5 2 7 2.6 CCCn1c(=O)[nH]c2nc(-c3cnn(CC#Cc4cccc(OC(F)(F)F)c4)c3)[nH]c2c1=O 10.1016/j.ejmech.2017.04.014
CHEMBL4081707 157682 None 0 Human Binding pKi = 8.6 8.6 - 1
Displacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 minsDisplacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 mins
ChEMBL 458 5 2 7 2.6 CCCn1c(=O)[nH]c2nc(-c3cnn(CC#Cc4cccc(OC(F)(F)F)c4)c3)[nH]c2c1=O 10.1016/j.ejmech.2017.04.014
44574117 189311 None 0 Human Binding pKi = 8.6 8.6 -1 4
Displacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells by beta scintillation counterDisplacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells by beta scintillation counter
ChEMBL 404 4 2 6 3.0 Cn1c(=O)c2[nH]c(-c3ccc(COC(=O)Nc4ccccc4)cc3)cc2n(C)c1=O 10.1016/j.bmc.2009.03.062
CHEMBL512290 189311 None 0 Human Binding pKi = 8.6 8.6 -1 4
Displacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells by beta scintillation counterDisplacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells by beta scintillation counter
ChEMBL 404 4 2 6 3.0 Cn1c(=O)c2[nH]c(-c3ccc(COC(=O)Nc4ccccc4)cc3)cc2n(C)c1=O 10.1016/j.bmc.2009.03.062
44451330 96184 None 0 Human Binding pKi = 8.6 8.6 53 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 507 5 1 7 2.6 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCN(c5cccc(Cl)c5)CC4)cc3)cc2n(C)c1=O 10.1016/j.bmc.2008.01.002
CHEMBL260693 96184 None 0 Human Binding pKi = 8.6 8.6 53 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 507 5 1 7 2.6 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCN(c5cccc(Cl)c5)CC4)cc3)cc2n(C)c1=O 10.1016/j.bmc.2008.01.002
168297723 192452 None 0 Human Binding pKi = 8.6 8.6 - 1
Displacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cell membrane preincubated for 4 hrs followed by [3H]PSB-603 addition and measured after 0.5 hrs by radioligand displacement assayDisplacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cell membrane preincubated for 4 hrs followed by [3H]PSB-603 addition and measured after 0.5 hrs by radioligand displacement assay
ChEMBL 327 4 2 6 2.2 CCCn1c(=O)[nH]c2nc(-c3cccc(N=C=S)c3)[nH]c2c1=O 10.1039/d2md00132b
CHEMBL5208506 192452 None 0 Human Binding pKi = 8.6 8.6 - 1
Displacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cell membrane preincubated for 4 hrs followed by [3H]PSB-603 addition and measured after 0.5 hrs by radioligand displacement assayDisplacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cell membrane preincubated for 4 hrs followed by [3H]PSB-603 addition and measured after 0.5 hrs by radioligand displacement assay
ChEMBL 327 4 2 6 2.2 CCCn1c(=O)[nH]c2nc(-c3cccc(N=C=S)c3)[nH]c2c1=O 10.1039/d2md00132b
44219683 196496 None 0 Human Binding pKi = 8.5 8.5 33 4
Binding affinity to human adenosine A2b receptor expressed in HEK293 cellsBinding affinity to human adenosine A2b receptor expressed in HEK293 cells
ChEMBL 555 10 2 8 3.4 CCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(Br)cc4)cc3)nc2n(CCCOC)c1=O 10.1016/j.bmc.2009.03.029
CHEMBL563425 196496 None 0 Human Binding pKi = 8.5 8.5 33 4
Binding affinity to human adenosine A2b receptor expressed in HEK293 cellsBinding affinity to human adenosine A2b receptor expressed in HEK293 cells
ChEMBL 555 10 2 8 3.4 CCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(Br)cc4)cc3)nc2n(CCCOC)c1=O 10.1016/j.bmc.2009.03.029
44450981 95939 None 0 Human Binding pKi = 8.5 8.5 112 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 522 5 2 7 2.8 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCC(O)(c5ccc(Cl)cc5)CC4)cc3)cc2n(C)c1=O 10.1016/j.bmc.2008.01.002
CHEMBL259360 95939 None 0 Human Binding pKi = 8.5 8.5 112 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 522 5 2 7 2.8 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCC(O)(c5ccc(Cl)cc5)CC4)cc3)cc2n(C)c1=O 10.1016/j.bmc.2008.01.002
76318040 105515 None 0 Human Binding pKi = 8.5 8.5 -10 4
Binding affinity to human recombinant adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated adenylyl cyclase activity after 20 minsBinding affinity to human recombinant adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated adenylyl cyclase activity after 20 mins
ChEMBL 383 5 2 7 1.4 Cn1c(=O)c2[nH]c(-c3ccc(OCCC4CCNCC4)cc3)nc2n(C)c1=O 10.1016/j.ejmech.2014.01.045
CHEMBL3121722 105515 None 0 Human Binding pKi = 8.5 8.5 -10 4
Binding affinity to human recombinant adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated adenylyl cyclase activity after 20 minsBinding affinity to human recombinant adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated adenylyl cyclase activity after 20 mins
ChEMBL 383 5 2 7 1.4 Cn1c(=O)c2[nH]c(-c3ccc(OCCC4CCNCC4)cc3)nc2n(C)c1=O 10.1016/j.ejmech.2014.01.045
10962751 162636 None 0 Human Binding pKi = 8.5 8.5 5 3
Inhibition of [3H]ZM-241385 binding to human adenosine A2B receptorInhibition of [3H]ZM-241385 binding to human adenosine A2B receptor
ChEMBL 560 9 2 8 2.7 CCCCn1c(=O)[nH]c2[nH]c(-c3ccc(OCC(=O)N4CCN(C(=O)OCc5ccccc5)CC4)cc3)nc2c1=O 10.1021/jm011049y
CHEMBL416963 162636 None 0 Human Binding pKi = 8.5 8.5 5 3
Inhibition of [3H]ZM-241385 binding to human adenosine A2B receptorInhibition of [3H]ZM-241385 binding to human adenosine A2B receptor
ChEMBL 560 9 2 8 2.7 CCCCn1c(=O)[nH]c2[nH]c(-c3ccc(OCC(=O)N4CCN(C(=O)OCc5ccccc5)CC4)cc3)nc2c1=O 10.1021/jm011049y
135522388 100112 None 0 Human Binding pKi = 7.7 7.7 7 2
Binding affinity of compound for displacement of [3H]DPCPX binding in HEK293 membranes expressing human A2B adenosine receptorsBinding affinity of compound for displacement of [3H]DPCPX binding in HEK293 membranes expressing human A2B adenosine receptors
ChEMBL 543 9 2 9 2.9 CCCn1c(=O)c2nc(-c3cc(OCC(=O)Nc4ccc(Br)cc4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
CHEMBL287529 100112 None 0 Human Binding pKi = 7.7 7.7 7 2
Binding affinity of compound for displacement of [3H]DPCPX binding in HEK293 membranes expressing human A2B adenosine receptorsBinding affinity of compound for displacement of [3H]DPCPX binding in HEK293 membranes expressing human A2B adenosine receptors
ChEMBL 543 9 2 9 2.9 CCCn1c(=O)c2nc(-c3cc(OCC(=O)Nc4ccc(Br)cc4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
135522388 100112 None 0 Human Binding pKi = 7.7 7.7 7 2
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 543 9 2 9 2.9 CCCn1c(=O)c2nc(-c3cc(OCC(=O)Nc4ccc(Br)cc4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
CHEMBL287529 100112 None 0 Human Binding pKi = 7.7 7.7 7 2
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 543 9 2 9 2.9 CCCn1c(=O)c2nc(-c3cc(OCC(=O)Nc4ccc(Br)cc4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
10007115 116344 None 0 Human Binding pKi = 7.7 7.7 15 5
Binding affinity to human adenosine A2b receptorBinding affinity to human adenosine A2b receptor
ChEMBL 527 8 1 8 5.7 O=C(Cc1cccc2ccccc12)Nc1nc2nn(CCCc3ccccc3)cc2c2nc(-c3ccco3)nn12 10.1016/j.bmc.2010.09.043
CHEMBL335950 116344 None 0 Human Binding pKi = 7.7 7.7 15 5
Binding affinity to human adenosine A2b receptorBinding affinity to human adenosine A2b receptor
ChEMBL 527 8 1 8 5.7 O=C(Cc1cccc2ccccc12)Nc1nc2nn(CCCc3ccccc3)cc2c2nc(-c3ccco3)nn12 10.1016/j.bmc.2010.09.043
10007115 116344 None 0 Human Binding pKi = 7.7 7.7 15 5
Displacement of [3H] DPCPX from human recombinant Adenosine A2B receptor expressed in HEK293 cells after 60 minsDisplacement of [3H] DPCPX from human recombinant Adenosine A2B receptor expressed in HEK293 cells after 60 mins
ChEMBL 527 8 1 8 5.7 O=C(Cc1cccc2ccccc12)Nc1nc2nn(CCCc3ccccc3)cc2c2nc(-c3ccco3)nn12 10.1021/acs.jmedchem.5b01586
CHEMBL335950 116344 None 0 Human Binding pKi = 7.7 7.7 15 5
Displacement of [3H] DPCPX from human recombinant Adenosine A2B receptor expressed in HEK293 cells after 60 minsDisplacement of [3H] DPCPX from human recombinant Adenosine A2B receptor expressed in HEK293 cells after 60 mins
ChEMBL 527 8 1 8 5.7 O=C(Cc1cccc2ccccc12)Nc1nc2nn(CCCc3ccccc3)cc2c2nc(-c3ccco3)nn12 10.1021/acs.jmedchem.5b01586
10007115 116344 None 0 Human Binding pKi = 7.7 7.7 15 5
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 527 8 1 8 5.7 O=C(Cc1cccc2ccccc12)Nc1nc2nn(CCCc3ccccc3)cc2c2nc(-c3ccco3)nn12 10.1021/jm030852k
CHEMBL335950 116344 None 0 Human Binding pKi = 7.7 7.7 15 5
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 527 8 1 8 5.7 O=C(Cc1cccc2ccccc12)Nc1nc2nn(CCCc3ccccc3)cc2c2nc(-c3ccco3)nn12 10.1021/jm030852k
155530961 171591 None 0 Human Binding pKi = 7.7 7.7 15 4
Displacement of [3H]DPCPX from recombinant human A2B adenosine receptor expressed in HEK293 cell membranes measured after 60 mins by topcount scintillation counting methodDisplacement of [3H]DPCPX from recombinant human A2B adenosine receptor expressed in HEK293 cell membranes measured after 60 mins by topcount scintillation counting method
ChEMBL 513 7 1 8 5.8 O=C(Nc1nc2nn(CCCc3ccccc3)cc2c2nc(-c3ccco3)nn12)c1cccc2ccccc12 10.1021/acs.jmedchem.9b00071
CHEMBL4465141 171591 None 0 Human Binding pKi = 7.7 7.7 15 4
Displacement of [3H]DPCPX from recombinant human A2B adenosine receptor expressed in HEK293 cell membranes measured after 60 mins by topcount scintillation counting methodDisplacement of [3H]DPCPX from recombinant human A2B adenosine receptor expressed in HEK293 cell membranes measured after 60 mins by topcount scintillation counting method
ChEMBL 513 7 1 8 5.8 O=C(Nc1nc2nn(CCCc3ccccc3)cc2c2nc(-c3ccco3)nn12)c1cccc2ccccc12 10.1021/acs.jmedchem.9b00071
136042327 71146 None 0 Human Binding pKi = 7.7 7.7 - 1
Displacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation countingDisplacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation counting
ChEMBL 512 8 2 9 3.7 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5cc6ccccc6cc5[nH]4)nn3C)nc2n(CCC)c1=O 10.1021/jm201292w
CHEMBL1955893 71146 None 0 Human Binding pKi = 7.7 7.7 - 1
Displacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation countingDisplacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation counting
ChEMBL 512 8 2 9 3.7 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5cc6ccccc6cc5[nH]4)nn3C)nc2n(CCC)c1=O 10.1021/jm201292w
135874424 95848 None 0 Human Binding pKi = 7.7 7.7 7 2
Displacement of [3H]MRE2029F20 from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]MRE2029F20 from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 469 8 2 8 2.9 CCCn1c(=O)c2[nH]c(-c3ccn(CC(=O)Nc4ccc(Cl)cc4)n3)nc2n(CCC)c1=O 10.1016/j.bmc.2007.11.058
CHEMBL258987 95848 None 0 Human Binding pKi = 7.7 7.7 7 2
Displacement of [3H]MRE2029F20 from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]MRE2029F20 from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 469 8 2 8 2.9 CCCn1c(=O)c2[nH]c(-c3ccn(CC(=O)Nc4ccc(Cl)cc4)n3)nc2n(CCC)c1=O 10.1016/j.bmc.2007.11.058
24827554 95984 None 0 Human Binding pKi = 7.7 7.7 17 4
Displacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 447 5 1 8 2.8 CCn1c(=O)n(CC(C)C)c(=O)c2[nH]c(-c3cnn(-c4ccc(C(F)(F)F)nc4)c3)nc21 10.1021/jm7014815
CHEMBL259565 95984 None 0 Human Binding pKi = 7.7 7.7 17 4
Displacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 447 5 1 8 2.8 CCn1c(=O)n(CC(C)C)c(=O)c2[nH]c(-c3cnn(-c4ccc(C(F)(F)F)nc4)c3)nc21 10.1021/jm7014815
52950040 19160 None 0 Human Binding pKi = 7.7 7.7 2 3
Displacement of [3H]ZM241385 from human adenosine A2B receptor transfected in CHO cells after 60 mins by scintillation countingDisplacement of [3H]ZM241385 from human adenosine A2B receptor transfected in CHO cells after 60 mins by scintillation counting
ChEMBL 523 10 2 5 6.1 CC[C@H](NC(=O)COc1ccc2[nH]c(=O)c(-c3nccs3)c(CCc3ccccc3)c2c1)c1ccccc1 10.1016/j.bmcl.2010.10.030
CHEMBL1289569 19160 None 0 Human Binding pKi = 7.7 7.7 2 3
Displacement of [3H]ZM241385 from human adenosine A2B receptor transfected in CHO cells after 60 mins by scintillation countingDisplacement of [3H]ZM241385 from human adenosine A2B receptor transfected in CHO cells after 60 mins by scintillation counting
ChEMBL 523 10 2 5 6.1 CC[C@H](NC(=O)COc1ccc2[nH]c(=O)c(-c3nccs3)c(CCc3ccccc3)c2c1)c1ccccc1 10.1016/j.bmcl.2010.10.030
11547107 77080 None 0 Human Binding pKi = 7.7 7.7 2 3
Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cellsDisplacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells
ChEMBL 460 7 1 7 3.6 CCCn1c(=O)c2nc(-c3cnn(Cc4ccc(C(F)(F)F)cc4)c3)[nH]c2n(CCC)c1=O 10.1021/jm051268+
CHEMBL207434 77080 None 0 Human Binding pKi = 7.7 7.7 2 3
Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cellsDisplacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells
ChEMBL 460 7 1 7 3.6 CCCn1c(=O)c2nc(-c3cnn(Cc4ccc(C(F)(F)F)cc4)c3)[nH]c2n(CCC)c1=O 10.1021/jm051268+
11495611 139084 None 0 Human Binding pKi = 7.7 7.7 2 3
Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cellsDisplacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells
ChEMBL 426 7 1 7 3.3 CCCn1c(=O)c2nc(-c3cnn(Cc4ccccc4Cl)c3)[nH]c2n(CCC)c1=O 10.1021/jm051268+
CHEMBL378652 139084 None 0 Human Binding pKi = 7.7 7.7 2 3
Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cellsDisplacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells
ChEMBL 426 7 1 7 3.3 CCCn1c(=O)c2nc(-c3cnn(Cc4ccccc4Cl)c3)[nH]c2n(CCC)c1=O 10.1021/jm051268+
11503942 73091 None 0 Human Binding pKi = 7.7 7.7 - 1
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 480 8 2 6 3.5 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)NCc4ccc(Cl)cc4)cc3)cc2n(C)c1=O 10.1021/jm0506221
CHEMBL201109 73091 None 0 Human Binding pKi = 7.7 7.7 - 1
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 480 8 2 6 3.5 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)NCc4ccc(Cl)cc4)cc3)cc2n(C)c1=O 10.1021/jm0506221
44451230 96386 None 0 Human Binding pKi = 7.7 7.7 7 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 573 9 1 8 3.7 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCN(C(=O)Oc5ccccc5)CC4)cc3)cc2n(CCC)c1=O 10.1016/j.bmc.2008.01.002
CHEMBL261792 96386 None 0 Human Binding pKi = 7.7 7.7 7 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 573 9 1 8 3.7 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCN(C(=O)Oc5ccccc5)CC4)cc3)cc2n(CCC)c1=O 10.1016/j.bmc.2008.01.002
44451492 159075 None 0 Human Binding pKi = 7.7 7.7 17 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 487 5 1 7 2.3 CC(Oc1ccc(-c2cc3c([nH]2)c(=O)n(C)c(=O)n3C)cc1)C(=O)N1CCN(c2ccccc2)CC1 10.1016/j.bmc.2008.01.002
CHEMBL409726 159075 None 0 Human Binding pKi = 7.7 7.7 17 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 487 5 1 7 2.3 CC(Oc1ccc(-c2cc3c([nH]2)c(=O)n(C)c(=O)n3C)cc1)C(=O)N1CCN(c2ccccc2)CC1 10.1016/j.bmc.2008.01.002
50940978 57279 None 0 Human Binding pKi = 7.7 7.7 -3 4
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 283 4 1 5 3.3 CCC(=O)Nc1cc(-c2ccco2)nc(-c2ccco2)n1 10.1021/jm100843z
CHEMBL1650385 57279 None 0 Human Binding pKi = 7.7 7.7 -3 4
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 283 4 1 5 3.3 CCC(=O)Nc1cc(-c2ccco2)nc(-c2ccco2)n1 10.1021/jm100843z
127033039 139001 None 0 Human Binding pKi = 7.7 7.7 - 1
Displacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting methodDisplacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting method
ChEMBL 323 3 1 6 3.5 CCOC(=O)C1=C(C)Nc2nc3ccccc3n2C1c1ccoc1 10.1021/acs.jmedchem.0c00564
CHEMBL3785582 139001 None 0 Human Binding pKi = 7.7 7.7 - 1
Displacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting methodDisplacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting method
ChEMBL 323 3 1 6 3.5 CCOC(=O)C1=C(C)Nc2nc3ccccc3n2C1c1ccoc1 10.1021/acs.jmedchem.0c00564
127033039 139001 None 0 Human Binding pKi = 7.7 7.7 - 1
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 minsDisplacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 mins
ChEMBL 323 3 1 6 3.5 CCOC(=O)C1=C(C)Nc2nc3ccccc3n2C1c1ccoc1 10.1021/acs.jmedchem.5b01586
CHEMBL3785582 139001 None 0 Human Binding pKi = 7.7 7.7 - 1
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 minsDisplacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 mins
ChEMBL 323 3 1 6 3.5 CCOC(=O)C1=C(C)Nc2nc3ccccc3n2C1c1ccoc1 10.1021/acs.jmedchem.5b01586
127033039 139001 None 0 Human Binding pKi = 7.7 7.7 - 1
Displacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assayDisplacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assay
ChEMBL 323 3 1 6 3.5 CCOC(=O)C1=C(C)Nc2nc3ccccc3n2C1c1ccoc1 10.1021/acs.jmedchem.9b01340
CHEMBL3785582 139001 None 0 Human Binding pKi = 7.7 7.7 - 1
Displacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assayDisplacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assay
ChEMBL 323 3 1 6 3.5 CCOC(=O)C1=C(C)Nc2nc3ccccc3n2C1c1ccoc1 10.1021/acs.jmedchem.9b01340
136044106 49949 None 0 Human Binding pKi = 7.7 7.7 2 3
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 344 5 3 7 1.8 CCCn1c(=O)c2nc(-c3ccc(O)cc3O)[nH]c2n(CCC)c1=O 10.1021/jm0104318
CHEMBL156863 49949 None 0 Human Binding pKi = 7.7 7.7 2 3
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 344 5 3 7 1.8 CCCn1c(=O)c2nc(-c3ccc(O)cc3O)[nH]c2n(CCC)c1=O 10.1021/jm0104318
45267991 196105 None 0 Human Binding pKi = 7.7 7.7 4 4
Binding affinity to human adenosine A2b receptor expressed in HEK293 cellsBinding affinity to human adenosine A2b receptor expressed in HEK293 cells
ChEMBL 468 10 2 10 1.6 CCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccon4)cc3)nc2n(CCCOC)c1=O 10.1016/j.bmc.2009.03.029
CHEMBL560905 196105 None 0 Human Binding pKi = 7.7 7.7 4 4
Binding affinity to human adenosine A2b receptor expressed in HEK293 cellsBinding affinity to human adenosine A2b receptor expressed in HEK293 cells
ChEMBL 468 10 2 10 1.6 CCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccon4)cc3)nc2n(CCCOC)c1=O 10.1016/j.bmc.2009.03.029
11525816 73360 None 0 Human Binding pKi = 7.7 7.7 15 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 477 9 3 8 3.1 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ncccc4O)cc3)cc2n(CCC)c1=O 10.1021/jm0506221
CHEMBL201329 73360 None 0 Human Binding pKi = 7.7 7.7 15 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 477 9 3 8 3.1 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ncccc4O)cc3)cc2n(CCC)c1=O 10.1021/jm0506221
44450904 96098 None 0 Human Binding pKi = 7.7 7.7 28 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 528 9 1 6 4.8 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCC(c5ccccc5)CC4)cc3)cc2n(CCC)c1=O 10.1016/j.bmc.2008.01.002
CHEMBL260180 96098 None 0 Human Binding pKi = 7.7 7.7 28 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 528 9 1 6 4.8 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCC(c5ccccc5)CC4)cc3)cc2n(CCC)c1=O 10.1016/j.bmc.2008.01.002
9887859 113512 None 0 Human Binding pKi = 6.7 6.7 -10000 6
Displacement of [3H]-DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins
ChEMBL 375 3 2 9 2.3 Cn1cc2c(nc(NC(=O)Nc3ccncc3)n3nc(-c4ccco4)nc23)n1 10.1016/j.bmc.2011.11.037
CHEMBL118923 113512 None 0 Human Binding pKi = 6.7 6.7 -10000 6
Displacement of [3H]-DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins
ChEMBL 375 3 2 9 2.3 Cn1cc2c(nc(NC(=O)Nc3ccncc3)n3nc(-c4ccco4)nc23)n1 10.1016/j.bmc.2011.11.037
CHEMBL332091 113512 None 0 Human Binding pKi = 6.7 6.7 -10000 6
Displacement of [3H]-DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins
ChEMBL 375 3 2 9 2.3 Cn1cc2c(nc(NC(=O)Nc3ccncc3)n3nc(-c4ccco4)nc23)n1 10.1016/j.bmc.2011.11.037
137636200 156066 None 0 Human Binding pKi = 6.7 6.7 - 1
Displacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 minsDisplacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 mins
ChEMBL 425 9 1 8 1.9 CCCn1c(=O)c2[nH]c(-c3cnn(CC#CCN(CC)CC)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2017.04.014
CHEMBL4062691 156066 None 0 Human Binding pKi = 6.7 6.7 - 1
Displacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 minsDisplacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 mins
ChEMBL 425 9 1 8 1.9 CCCn1c(=O)c2[nH]c(-c3cnn(CC#CCN(CC)CC)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2017.04.014
9887859 113512 None 0 Human Binding pKi = 6.7 6.7 -10000 6
Displacement of [3H]DPCPX from Human Adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from Human Adenosine A2B receptor expressed in HEK293 cells
ChEMBL 375 3 2 9 2.3 Cn1cc2c(nc(NC(=O)Nc3ccncc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm020974x
CHEMBL118923 113512 None 0 Human Binding pKi = 6.7 6.7 -10000 6
Displacement of [3H]DPCPX from Human Adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from Human Adenosine A2B receptor expressed in HEK293 cells
ChEMBL 375 3 2 9 2.3 Cn1cc2c(nc(NC(=O)Nc3ccncc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm020974x
CHEMBL332091 113512 None 0 Human Binding pKi = 6.7 6.7 -10000 6
Displacement of [3H]DPCPX from Human Adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from Human Adenosine A2B receptor expressed in HEK293 cells
ChEMBL 375 3 2 9 2.3 Cn1cc2c(nc(NC(=O)Nc3ccncc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm020974x
11569515 78215 None 0 Human Binding pKi = 6.7 6.7 - 1
Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cellsDisplacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells
ChEMBL 494 7 1 7 4.3 CCCn1c(=O)c2nc(-c3cnn(Cc4ccc(Cl)c(C(F)(F)F)c4)c3)[nH]c2n(CCC)c1=O 10.1021/jm051268+
CHEMBL210565 78215 None 0 Human Binding pKi = 6.7 6.7 - 1
Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cellsDisplacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells
ChEMBL 494 7 1 7 4.3 CCCn1c(=O)c2nc(-c3cnn(Cc4ccc(Cl)c(C(F)(F)F)c4)c3)[nH]c2n(CCC)c1=O 10.1021/jm051268+
135428630 81583 None 0 Human Binding pKi = 5.7 5.7 -2818 5
Displacement of [125I]3-(4-aminobenzyl)-8-phenyloxyacetate-1-propyl-xanthine from human adenosine A2B receptorDisplacement of [125I]3-(4-aminobenzyl)-8-phenyloxyacetate-1-propyl-xanthine from human adenosine A2B receptor
ChEMBL 385 4 2 4 3.2 CCCN1C(=O)N2C[C@@H](C(C)C)N=C2c2[nH]c(C34CCC(O)(CC3)CC4)nc21 10.1021/jm060539t
CHEMBL216269 81583 None 0 Human Binding pKi = 5.7 5.7 -2818 5
Displacement of [125I]3-(4-aminobenzyl)-8-phenyloxyacetate-1-propyl-xanthine from human adenosine A2B receptorDisplacement of [125I]3-(4-aminobenzyl)-8-phenyloxyacetate-1-propyl-xanthine from human adenosine A2B receptor
ChEMBL 385 4 2 4 3.2 CCCN1C(=O)N2C[C@@H](C(C)C)N=C2c2[nH]c(C34CCC(O)(CC3)CC4)nc21 10.1021/jm060539t
162663149 181949 None 0 Human Binding pKi = 6.7 6.7 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 278 4 2 4 2.2 CCC(C)OC(=O)C1=C(C)NC(=O)NC1c1ccoc1 10.1021/acs.jmedchem.0c01431
CHEMBL4779925 181949 None 0 Human Binding pKi = 6.7 6.7 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 278 4 2 4 2.2 CCC(C)OC(=O)C1=C(C)NC(=O)NC1c1ccoc1 10.1021/acs.jmedchem.0c01431
162667688 182479 None 0 Human Binding pKi = 6.7 6.7 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 280 4 2 4 2.3 CCCOC(=O)C1=C(C)NC(=O)NC1c1ccsc1 10.1021/acs.jmedchem.0c01431
CHEMBL4786646 182479 None 0 Human Binding pKi = 6.7 6.7 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 280 4 2 4 2.3 CCCOC(=O)C1=C(C)NC(=O)NC1c1ccsc1 10.1021/acs.jmedchem.0c01431
46880472 6078 None 0 Human Binding pKi = 6.7 6.7 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 305 4 2 4 2.9 O=C(Nc1ccc(-c2ccncc2)c(-c2cc[nH]n2)n1)C1CC1 10.1016/j.bmcl.2010.01.045
CHEMBL1080678 6078 None 0 Human Binding pKi = 6.7 6.7 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 305 4 2 4 2.9 O=C(Nc1ccc(-c2ccncc2)c(-c2cc[nH]n2)n1)C1CC1 10.1016/j.bmcl.2010.01.045
10765059 102695 None 0 Human Binding pKi = 5.7 5.7 -354 4
Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 1770-2327Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 1770-2327
ChEMBL 430 6 2 9 3.6 C=CCn1cc2c(nc(NC(=O)Nc3ccc(OC)cc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm001047y
CHEMBL304726 102695 None 0 Human Binding pKi = 5.7 5.7 -354 4
Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 1770-2327Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 1770-2327
ChEMBL 430 6 2 9 3.6 C=CCn1cc2c(nc(NC(=O)Nc3ccc(OC)cc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm001047y
123683 3121 None 63 Human Binding pKi = 5.7 5.7 -95499 13
Displacement of [125I]ABOPX from human adenosine A2B receptor in HEK cellsDisplacement of [125I]ABOPX from human adenosine A2B receptor in HEK cells
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1016/j.bmcl.2006.01.110
422 3121 None 63 Human Binding pKi = 5.7 5.7 -95499 13
Displacement of [125I]ABOPX from human adenosine A2B receptor in HEK cellsDisplacement of [125I]ABOPX from human adenosine A2B receptor in HEK cells
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1016/j.bmcl.2006.01.110
CHEMBL119709 3121 None 63 Human Binding pKi = 5.7 5.7 -95499 13
Displacement of [125I]ABOPX from human adenosine A2B receptor in HEK cellsDisplacement of [125I]ABOPX from human adenosine A2B receptor in HEK cells
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1016/j.bmcl.2006.01.110
DB05511 3121 None 63 Human Binding pKi = 5.7 5.7 -95499 13
Displacement of [125I]ABOPX from human adenosine A2B receptor in HEK cellsDisplacement of [125I]ABOPX from human adenosine A2B receptor in HEK cells
ChEMBL 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10.1016/j.bmcl.2006.01.110
123807 871 None 54 Human Binding pKi = 4.7 4.7 -13803 13
Displacement of [3H]- ZM-241385 from human adenosine A2B receptor expressed in HEK cellsDisplacement of [3H]- ZM-241385 from human adenosine A2B receptor expressed in HEK cells
ChEMBL 369 4 4 9 0.4 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NC1CCCC1 10.1021/jm9905965
374 871 None 54 Human Binding pKi = 4.7 4.7 -13803 13
Displacement of [3H]- ZM-241385 from human adenosine A2B receptor expressed in HEK cellsDisplacement of [3H]- ZM-241385 from human adenosine A2B receptor expressed in HEK cells
ChEMBL 369 4 4 9 0.4 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NC1CCCC1 10.1021/jm9905965
379 871 None 54 Human Binding pKi = 4.7 4.7 -13803 13
Displacement of [3H]- ZM-241385 from human adenosine A2B receptor expressed in HEK cellsDisplacement of [3H]- ZM-241385 from human adenosine A2B receptor expressed in HEK cells
ChEMBL 369 4 4 9 0.4 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NC1CCCC1 10.1021/jm9905965
CHEMBL284969 871 None 54 Human Binding pKi = 4.7 4.7 -13803 13
Displacement of [3H]- ZM-241385 from human adenosine A2B receptor expressed in HEK cellsDisplacement of [3H]- ZM-241385 from human adenosine A2B receptor expressed in HEK cells
ChEMBL 369 4 4 9 0.4 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NC1CCCC1 10.1021/jm9905965
9822747 119381 None 0 Human Binding pKi = 6.7 6.7 -16 4
Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 157-268Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 157-268
ChEMBL 408 3 2 8 3.6 Cn1cc2c(nc(NC(=O)Nc3cccc(Cl)c3)n3nc(-c4ccco4)nc23)n1 10.1021/jm001047y
CHEMBL344501 119381 None 0 Human Binding pKi = 6.7 6.7 -16 4
Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 157-268Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 157-268
ChEMBL 408 3 2 8 3.6 Cn1cc2c(nc(NC(=O)Nc3cccc(Cl)c3)n3nc(-c4ccco4)nc23)n1 10.1021/jm001047y
9822747 119381 None 0 Human Binding pKi = 6.7 6.7 -16 4
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 157-268Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 157-268
ChEMBL 408 3 2 8 3.6 Cn1cc2c(nc(NC(=O)Nc3cccc(Cl)c3)n3nc(-c4ccco4)nc23)n1 10.1021/jm0109614
CHEMBL344501 119381 None 0 Human Binding pKi = 6.7 6.7 -16 4
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 157-268Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 157-268
ChEMBL 408 3 2 8 3.6 Cn1cc2c(nc(NC(=O)Nc3cccc(Cl)c3)n3nc(-c4ccco4)nc23)n1 10.1021/jm0109614
2519 779 None 86 Human Binding pKi = 4.7 4.7 -11 12
Displacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cells
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1016/j.ejmech.2011.05.023
2519.0 779 None 86 Human Binding pKi = 4.7 4.7 -11 12
Displacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cells
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1016/j.ejmech.2011.05.023
407 779 None 86 Human Binding pKi = 4.7 4.7 -11 12
Displacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cells
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1016/j.ejmech.2011.05.023
463 779 None 86 Human Binding pKi = 4.7 4.7 -11 12
Displacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cells
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1016/j.ejmech.2011.05.023
CHEMBL113 779 None 86 Human Binding pKi = 4.7 4.7 -11 12
Displacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cells
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1016/j.ejmech.2011.05.023
DB00201 779 None 86 Human Binding pKi = 4.7 4.7 -11 12
Displacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cells
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1016/j.ejmech.2011.05.023
2519 779 None 86 Human Binding pKi = 4.7 4.7 -11 12
Inhibition of human adenosine 2B receptorInhibition of human adenosine 2B receptor
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1021/acs.jmedchem.0c00237
2519.0 779 None 86 Human Binding pKi = 4.7 4.7 -11 12
Inhibition of human adenosine 2B receptorInhibition of human adenosine 2B receptor
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1021/acs.jmedchem.0c00237
407 779 None 86 Human Binding pKi = 4.7 4.7 -11 12
Inhibition of human adenosine 2B receptorInhibition of human adenosine 2B receptor
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1021/acs.jmedchem.0c00237
463 779 None 86 Human Binding pKi = 4.7 4.7 -11 12
Inhibition of human adenosine 2B receptorInhibition of human adenosine 2B receptor
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1021/acs.jmedchem.0c00237
CHEMBL113 779 None 86 Human Binding pKi = 4.7 4.7 -11 12
Inhibition of human adenosine 2B receptorInhibition of human adenosine 2B receptor
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1021/acs.jmedchem.0c00237
DB00201 779 None 86 Human Binding pKi = 4.7 4.7 -11 12
Inhibition of human adenosine 2B receptorInhibition of human adenosine 2B receptor
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1021/acs.jmedchem.0c00237
2519 779 None 86 Human Binding pKi = 4.7 4.7 -11 12
Inhibition of human recombinant adenosine receptor A2bInhibition of human recombinant adenosine receptor A2b
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1021/jm4011669
2519.0 779 None 86 Human Binding pKi = 4.7 4.7 -11 12
Inhibition of human recombinant adenosine receptor A2bInhibition of human recombinant adenosine receptor A2b
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1021/jm4011669
407 779 None 86 Human Binding pKi = 4.7 4.7 -11 12
Inhibition of human recombinant adenosine receptor A2bInhibition of human recombinant adenosine receptor A2b
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1021/jm4011669
463 779 None 86 Human Binding pKi = 4.7 4.7 -11 12
Inhibition of human recombinant adenosine receptor A2bInhibition of human recombinant adenosine receptor A2b
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1021/jm4011669
CHEMBL113 779 None 86 Human Binding pKi = 4.7 4.7 -11 12
Inhibition of human recombinant adenosine receptor A2bInhibition of human recombinant adenosine receptor A2b
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1021/jm4011669
DB00201 779 None 86 Human Binding pKi = 4.7 4.7 -11 12
Inhibition of human recombinant adenosine receptor A2bInhibition of human recombinant adenosine receptor A2b
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1021/jm4011669
459 2618 None 34 Human Binding pKi = 5.7 5.7 -389 5
Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 1637-2582Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 1637-2582
ChEMBL 432 6 2 9 3.8 CCCn1cc2c(n1)nc(n1c2nc(n1)c1ccco1)NC(=O)Nc1ccc(cc1)OC 10.1021/jm001047y
477 2618 None 34 Human Binding pKi = 5.7 5.7 -389 5
Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 1637-2582Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 1637-2582
ChEMBL 432 6 2 9 3.8 CCCn1cc2c(n1)nc(n1c2nc(n1)c1ccco1)NC(=O)Nc1ccc(cc1)OC 10.1021/jm001047y
5310960 2618 None 34 Human Binding pKi = 5.7 5.7 -389 5
Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 1637-2582Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 1637-2582
ChEMBL 432 6 2 9 3.8 CCCn1cc2c(n1)nc(n1c2nc(n1)c1ccco1)NC(=O)Nc1ccc(cc1)OC 10.1021/jm001047y
CHEMBL302765 2618 None 34 Human Binding pKi = 5.7 5.7 -389 5
Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 1637-2582Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 1637-2582
ChEMBL 432 6 2 9 3.8 CCCn1cc2c(n1)nc(n1c2nc(n1)c1ccco1)NC(=O)Nc1ccc(cc1)OC 10.1021/jm001047y
459 2618 None 34 Human Binding pKi = 5.7 5.7 -389 5
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells
ChEMBL 432 6 2 9 3.8 CCCn1cc2c(n1)nc(n1c2nc(n1)c1ccco1)NC(=O)Nc1ccc(cc1)OC 10.1021/jm010818a
477 2618 None 34 Human Binding pKi = 5.7 5.7 -389 5
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells
ChEMBL 432 6 2 9 3.8 CCCn1cc2c(n1)nc(n1c2nc(n1)c1ccco1)NC(=O)Nc1ccc(cc1)OC 10.1021/jm010818a
5310960 2618 None 34 Human Binding pKi = 5.7 5.7 -389 5
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells
ChEMBL 432 6 2 9 3.8 CCCn1cc2c(n1)nc(n1c2nc(n1)c1ccco1)NC(=O)Nc1ccc(cc1)OC 10.1021/jm010818a
CHEMBL302765 2618 None 34 Human Binding pKi = 5.7 5.7 -389 5
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells
ChEMBL 432 6 2 9 3.8 CCCn1cc2c(n1)nc(n1c2nc(n1)c1ccco1)NC(=O)Nc1ccc(cc1)OC 10.1021/jm010818a
459 2618 None 34 Human Binding pKi = 5.7 5.7 -389 5
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 1637-2582Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 1637-2582
ChEMBL 432 6 2 9 3.8 CCCn1cc2c(n1)nc(n1c2nc(n1)c1ccco1)NC(=O)Nc1ccc(cc1)OC 10.1021/jm0109614
477 2618 None 34 Human Binding pKi = 5.7 5.7 -389 5
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 1637-2582Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 1637-2582
ChEMBL 432 6 2 9 3.8 CCCn1cc2c(n1)nc(n1c2nc(n1)c1ccco1)NC(=O)Nc1ccc(cc1)OC 10.1021/jm0109614
5310960 2618 None 34 Human Binding pKi = 5.7 5.7 -389 5
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 1637-2582Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 1637-2582
ChEMBL 432 6 2 9 3.8 CCCn1cc2c(n1)nc(n1c2nc(n1)c1ccco1)NC(=O)Nc1ccc(cc1)OC 10.1021/jm0109614
CHEMBL302765 2618 None 34 Human Binding pKi = 5.7 5.7 -389 5
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 1637-2582Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 1637-2582
ChEMBL 432 6 2 9 3.8 CCCn1cc2c(n1)nc(n1c2nc(n1)c1ccco1)NC(=O)Nc1ccc(cc1)OC 10.1021/jm0109614
459 2618 None 34 Human Binding pKi = 5.7 5.7 -389 5
Inhibition of [3H]DPCPX binding to human Adenosine A2B receptor expressed in HEK cells; Range 1640-2580Inhibition of [3H]DPCPX binding to human Adenosine A2B receptor expressed in HEK cells; Range 1640-2580
ChEMBL 432 6 2 9 3.8 CCCn1cc2c(n1)nc(n1c2nc(n1)c1ccco1)NC(=O)Nc1ccc(cc1)OC 10.1021/jm010570p
477 2618 None 34 Human Binding pKi = 5.7 5.7 -389 5
Inhibition of [3H]DPCPX binding to human Adenosine A2B receptor expressed in HEK cells; Range 1640-2580Inhibition of [3H]DPCPX binding to human Adenosine A2B receptor expressed in HEK cells; Range 1640-2580
ChEMBL 432 6 2 9 3.8 CCCn1cc2c(n1)nc(n1c2nc(n1)c1ccco1)NC(=O)Nc1ccc(cc1)OC 10.1021/jm010570p
5310960 2618 None 34 Human Binding pKi = 5.7 5.7 -389 5
Inhibition of [3H]DPCPX binding to human Adenosine A2B receptor expressed in HEK cells; Range 1640-2580Inhibition of [3H]DPCPX binding to human Adenosine A2B receptor expressed in HEK cells; Range 1640-2580
ChEMBL 432 6 2 9 3.8 CCCn1cc2c(n1)nc(n1c2nc(n1)c1ccco1)NC(=O)Nc1ccc(cc1)OC 10.1021/jm010570p
CHEMBL302765 2618 None 34 Human Binding pKi = 5.7 5.7 -389 5
Inhibition of [3H]DPCPX binding to human Adenosine A2B receptor expressed in HEK cells; Range 1640-2580Inhibition of [3H]DPCPX binding to human Adenosine A2B receptor expressed in HEK cells; Range 1640-2580
ChEMBL 432 6 2 9 3.8 CCCn1cc2c(n1)nc(n1c2nc(n1)c1ccco1)NC(=O)Nc1ccc(cc1)OC 10.1021/jm010570p
15524546 103851 None 0 Human Binding pKi = 6.7 6.7 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 264 4 2 4 1.9 CCCOC(=O)C1=C(C)NC(=O)NC1c1ccco1 10.1021/acs.jmedchem.0c01431
CHEMBL3091707 103851 None 0 Human Binding pKi = 6.7 6.7 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 264 4 2 4 1.9 CCCOC(=O)C1=C(C)NC(=O)NC1c1ccco1 10.1021/acs.jmedchem.0c01431
21874662 189369 None 0 Human Binding pKi = 6.7 6.7 -23 4
Displacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation countingDisplacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation counting
ChEMBL 332 3 2 8 2.0 Nc1nc(-c2ccco2)c2nnn(Cc3ccc4[nH]ncc4c3)c2n1 10.1021/jm800961g
CHEMBL512812 189369 None 0 Human Binding pKi = 6.7 6.7 -23 4
Displacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation countingDisplacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation counting
ChEMBL 332 3 2 8 2.0 Nc1nc(-c2ccco2)c2nnn(Cc3ccc4[nH]ncc4c3)c2n1 10.1021/jm800961g
15524546 103851 None 0 Human Binding pKi = 6.7 6.7 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by Scatchard plot analysisDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by Scatchard plot analysis
ChEMBL 264 4 2 4 1.9 CCCOC(=O)C1=C(C)NC(=O)NC1c1ccco1 10.1021/ml400185v
CHEMBL3091707 103851 None 0 Human Binding pKi = 6.7 6.7 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by Scatchard plot analysisDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by Scatchard plot analysis
ChEMBL 264 4 2 4 1.9 CCCOC(=O)C1=C(C)NC(=O)NC1c1ccco1 10.1021/ml400185v
135486084 13851 None 0 Human Binding pKi = 5.7 5.7 -3 2
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 416 9 3 9 0.8 CCCn1c(=O)c2nc(-c3cc(NC(=O)CCCN)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
CHEMBL1195913 13851 None 0 Human Binding pKi = 5.7 5.7 -3 2
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 416 9 3 9 0.8 CCCn1c(=O)c2nc(-c3cc(NC(=O)CCCN)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
CHEMBL555577 13851 None 0 Human Binding pKi = 5.7 5.7 -3 2
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 416 9 3 9 0.8 CCCn1c(=O)c2nc(-c3cc(NC(=O)CCCN)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
44390651 64770 None 0 Human Binding pKi = 6.7 6.7 1 2
Binding affinity for adenosine A2b receptor by using as [3H]ZM-241385 (14 nM) radioligand in membranes from HEK-A2B cellsBinding affinity for adenosine A2b receptor by using as [3H]ZM-241385 (14 nM) radioligand in membranes from HEK-A2B cells
ChEMBL 511 9 1 10 3.9 CCCn1c(=O)c2nc(-c3ccc(OCc4noc(-c5ccc(C#N)cc5)n4)cc3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2004.11.044
CHEMBL181925 64770 None 0 Human Binding pKi = 6.7 6.7 1 2
Binding affinity for adenosine A2b receptor by using as [3H]ZM-241385 (14 nM) radioligand in membranes from HEK-A2B cellsBinding affinity for adenosine A2b receptor by using as [3H]ZM-241385 (14 nM) radioligand in membranes from HEK-A2B cells
ChEMBL 511 9 1 10 3.9 CCCn1c(=O)c2nc(-c3ccc(OCc4noc(-c5ccc(C#N)cc5)n4)cc3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2004.11.044
135546658 116292 None 0 Human Binding pKi = 6.7 6.7 -2 2
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 511 9 2 9 2.8 CC(C)Cn1c(=O)c2nc(-c3cc(OCC(=O)Nc4ccc(F)cc4)n(C)n3)[nH]c2n(CC(C)C)c1=O 10.1021/jm0309654
CHEMBL33591 116292 None 0 Human Binding pKi = 6.7 6.7 -2 2
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 511 9 2 9 2.8 CC(C)Cn1c(=O)c2nc(-c3cc(OCC(=O)Nc4ccc(F)cc4)n(C)n3)[nH]c2n(CC(C)C)c1=O 10.1021/jm0309654
11995557 165859 None 0 Human Binding pKi = 6.7 6.7 -26 4
Displacement of [125I]3-(4-aminobenzyl)-8-phenyloxyacetate-1-propyl-xanthine from human adenosine A2B receptor expressed in HEK cellsDisplacement of [125I]3-(4-aminobenzyl)-8-phenyloxyacetate-1-propyl-xanthine from human adenosine A2B receptor expressed in HEK cells
ChEMBL 459 8 2 8 1.6 CCCn1c(=O)c2nc([C@]34CC[C@](C(=O)NCC(=O)OC)(CC3)CC4)[nH]c2n(CCC)c1=O 10.1021/jm0605381
CHEMBL424908 165859 None 0 Human Binding pKi = 6.7 6.7 -26 4
Displacement of [125I]3-(4-aminobenzyl)-8-phenyloxyacetate-1-propyl-xanthine from human adenosine A2B receptor expressed in HEK cellsDisplacement of [125I]3-(4-aminobenzyl)-8-phenyloxyacetate-1-propyl-xanthine from human adenosine A2B receptor expressed in HEK cells
ChEMBL 459 8 2 8 1.6 CCCn1c(=O)c2nc([C@]34CC[C@](C(=O)NCC(=O)OC)(CC3)CC4)[nH]c2n(CCC)c1=O 10.1021/jm0605381
46880511 6158 None 0 Human Binding pKi = 6.7 6.7 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 317 4 1 5 2.9 O=C(Nc1ccc(-c2ccncc2)c(-c2ccncn2)n1)C1CC1 10.1016/j.bmcl.2010.01.045
CHEMBL1081042 6158 None 0 Human Binding pKi = 6.7 6.7 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 317 4 1 5 2.9 O=C(Nc1ccc(-c2ccncc2)c(-c2ccncn2)n1)C1CC1 10.1016/j.bmcl.2010.01.045
44390587 63914 None 0 Human Binding pKi = 5.7 5.7 - 1
Binding affinity for adenosine A2b receptor by using as [3H]ZM-241385 (14 nM) radioligand in membranes from HEK-A2B cellsBinding affinity for adenosine A2b receptor by using as [3H]ZM-241385 (14 nM) radioligand in membranes from HEK-A2B cells
ChEMBL 520 9 1 9 4.7 CCCn1c(=O)c2nc(-c3ccc(OCc4noc(-c5cccc(Cl)c5)n4)cc3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2004.11.044
CHEMBL180588 63914 None 0 Human Binding pKi = 5.7 5.7 - 1
Binding affinity for adenosine A2b receptor by using as [3H]ZM-241385 (14 nM) radioligand in membranes from HEK-A2B cellsBinding affinity for adenosine A2b receptor by using as [3H]ZM-241385 (14 nM) radioligand in membranes from HEK-A2B cells
ChEMBL 520 9 1 9 4.7 CCCn1c(=O)c2nc(-c3ccc(OCc4noc(-c5cccc(Cl)c5)n4)cc3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2004.11.044
350741 163417 None 2 Human Binding pKi = 4.7 4.7 - 1
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 236 2 0 7 -1.0 CC(=O)Cn1c(=O)c2c(ncn2C)n(C)c1=O 10.1021/jm0104318
CHEMBL419617 163417 None 2 Human Binding pKi = 4.7 4.7 - 1
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 236 2 0 7 -1.0 CC(=O)Cn1c(=O)c2c(ncn2C)n(C)c1=O 10.1021/jm0104318
22266765 94590 None 0 Human Binding pKi = 7.7 7.7 30 4
Displacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranesDisplacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranes
ChEMBL 460 8 1 10 2.7 CCCn1c(=O)c2[nH]c(-c3cnn(Cc4noc(-c5ccccc5)n4)c3)nc2n(CCC)c1=O 10.1016/j.bmcl.2008.01.008
CHEMBL252045 94590 None 0 Human Binding pKi = 7.7 7.7 30 4
Displacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranesDisplacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranes
ChEMBL 460 8 1 10 2.7 CCCn1c(=O)c2[nH]c(-c3cnn(Cc4noc(-c5ccccc5)n4)c3)nc2n(CCC)c1=O 10.1016/j.bmcl.2008.01.008
11952504 6022 None 0 Human Binding pKi = 7.7 7.7 34 3
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 263 2 1 5 2.7 c1coc(-c2nc3[nH]cnc3cc2-c2ccncn2)c1 10.1016/j.bmcl.2010.01.077
CHEMBL1080327 6022 None 0 Human Binding pKi = 7.7 7.7 34 3
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 263 2 1 5 2.7 c1coc(-c2nc3[nH]cnc3cc2-c2ccncn2)c1 10.1016/j.bmcl.2010.01.077
22266765 94590 None 0 Human Binding pKi = 7.7 7.7 30 4
Displacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cellsDisplacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cells
ChEMBL 460 8 1 10 2.7 CCCn1c(=O)c2[nH]c(-c3cnn(Cc4noc(-c5ccccc5)n4)c3)nc2n(CCC)c1=O 10.1016/j.bmcl.2005.10.002
CHEMBL252045 94590 None 0 Human Binding pKi = 7.7 7.7 30 4
Displacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cellsDisplacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cells
ChEMBL 460 8 1 10 2.7 CCCn1c(=O)c2[nH]c(-c3cnn(Cc4noc(-c5ccccc5)n4)c3)nc2n(CCC)c1=O 10.1016/j.bmcl.2005.10.002
11260448 135194 None 0 Human Binding pKi = 7.7 7.7 19 4
Displacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cellsDisplacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cells
ChEMBL 494 8 1 10 3.3 CCCn1c(=O)c2nc(-c3cnn(Cc4nc(-c5ccc(Cl)cc5)no4)c3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2005.10.002
CHEMBL372084 135194 None 0 Human Binding pKi = 7.7 7.7 19 4
Displacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cellsDisplacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cells
ChEMBL 494 8 1 10 3.3 CCCn1c(=O)c2nc(-c3cnn(Cc4nc(-c5ccc(Cl)cc5)no4)c3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2005.10.002
10029879 135195 None 0 Human Binding pKi = 7.7 7.7 61 2
Displacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cellsDisplacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cells
ChEMBL 528 8 1 10 3.7 CCCn1c(=O)c2nc(-c3cnn(Cc4noc(-c5ccc(C(F)(F)F)cc5)n4)c3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2005.10.002
CHEMBL372086 135195 None 0 Human Binding pKi = 7.7 7.7 61 2
Displacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cellsDisplacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cells
ChEMBL 528 8 1 10 3.7 CCCn1c(=O)c2nc(-c3cnn(Cc4noc(-c5ccc(C(F)(F)F)cc5)n4)c3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2005.10.002
21916408 159192 None 0 Human Binding pKi = 7.7 7.7 9 4
Displacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 378 5 1 7 2.0 CC(C)Cn1c(=O)c2[nH]c(-c3cnn(Cc4ccccc4)c3)nc2n(C)c1=O 10.1021/jm7014815
CHEMBL409852 159192 None 0 Human Binding pKi = 7.7 7.7 9 4
Displacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 378 5 1 7 2.0 CC(C)Cn1c(=O)c2[nH]c(-c3cnn(Cc4ccccc4)c3)nc2n(C)c1=O 10.1021/jm7014815
21916406 161455 None 0 Human Binding pKi = 7.7 7.7 7 4
Displacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 444 5 1 7 2.8 Cn1c(=O)n(CC2CC2)c(=O)c2[nH]c(-c3cnn(Cc4cccc(C(F)(F)F)c4)c3)nc21 10.1021/jm7014815
CHEMBL412747 161455 None 0 Human Binding pKi = 7.7 7.7 7 4
Displacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 444 5 1 7 2.8 Cn1c(=O)n(CC2CC2)c(=O)c2[nH]c(-c3cnn(Cc4cccc(C(F)(F)F)c4)c3)nc21 10.1021/jm7014815
135444614 114737 None 0 Human Binding pKi = 7.7 7.7 -40 4
Inhibition of [3H]DPCPX binding to human Adenosine A2B receptor expressed in HEK cells at 10000 nMInhibition of [3H]DPCPX binding to human Adenosine A2B receptor expressed in HEK cells at 10000 nM
ChEMBL 350 7 1 6 3.8 CCCCc1nc2[nH]cnc2c2nc(-c3ccc(OCCC)cc3)nn12 10.1021/jm010570p
CHEMBL333860 114737 None 0 Human Binding pKi = 7.7 7.7 -40 4
Inhibition of [3H]DPCPX binding to human Adenosine A2B receptor expressed in HEK cells at 10000 nMInhibition of [3H]DPCPX binding to human Adenosine A2B receptor expressed in HEK cells at 10000 nM
ChEMBL 350 7 1 6 3.8 CCCCc1nc2[nH]cnc2c2nc(-c3ccc(OCCC)cc3)nn12 10.1021/jm010570p
11640595 140192 None 0 Human Binding pKi = 7.7 7.7 9 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 432 7 2 6 3.1 CCCn1c(=O)n(C)c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccccc4)cc3)cc21 10.1021/jm0506221
CHEMBL380481 140192 None 0 Human Binding pKi = 7.7 7.7 9 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 432 7 2 6 3.1 CCCn1c(=O)n(C)c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccccc4)cc3)cc21 10.1021/jm0506221
44450905 96020 None 0 Human Binding pKi = 7.7 7.7 48 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 604 10 1 6 6.0 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCC(c5ccccc5)(c5ccccc5)CC4)cc3)cc2n(CCC)c1=O 10.1016/j.bmc.2008.01.002
CHEMBL259760 96020 None 0 Human Binding pKi = 7.7 7.7 48 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 604 10 1 6 6.0 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCC(c5ccccc5)(c5ccccc5)CC4)cc3)cc2n(CCC)c1=O 10.1016/j.bmc.2008.01.002
46228023 199910 None 0 Human Binding pKi = 7.7 7.7 6 3
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 382 6 0 8 2.4 C=CCn1c(=O)c2c(nc(Cc3cccs3)n2C)n(Cc2ccco2)c1=O 10.1016/j.bmc.2009.07.034
CHEMBL594735 199910 None 0 Human Binding pKi = 7.7 7.7 6 3
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 382 6 0 8 2.4 C=CCn1c(=O)c2c(nc(Cc3cccs3)n2C)n(Cc2ccco2)c1=O 10.1016/j.bmc.2009.07.034
46227952 201145 None 0 Human Binding pKi = 7.7 7.7 6 3
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 412 6 0 7 2.6 C=CCn1c(=O)c2c(nc(Cc3c(F)cccc3F)n2C)n(Cc2ccco2)c1=O 10.1016/j.bmc.2009.07.034
CHEMBL603209 201145 None 0 Human Binding pKi = 7.7 7.7 6 3
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 412 6 0 7 2.6 C=CCn1c(=O)c2c(nc(Cc3c(F)cccc3F)n2C)n(Cc2ccco2)c1=O 10.1016/j.bmc.2009.07.034
66893508 157096 None 0 Human Binding pKi = 7.7 7.7 - 1
Displacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting methodDisplacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting method
ChEMBL 505 9 1 9 2.6 CCCn1c(=O)c2[nH]c(-c3cnn(CC4CC(=O)N(c5cccc(OC)c5)C4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2016.11.007
CHEMBL4074473 157096 None 0 Human Binding pKi = 7.7 7.7 - 1
Displacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting methodDisplacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting method
ChEMBL 505 9 1 9 2.6 CCCn1c(=O)c2[nH]c(-c3cnn(CC4CC(=O)N(c5cccc(OC)c5)C4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2016.11.007
CHEMBL5092037 215344 None 0 Human Binding pKi = 7.7 7.7 -2 3
Displacement of [3H]DPCPX from human A2BAR expressed in HEK293 cell membrane incubated for 30 mins by microbeta trilux scintillation counter analysisDisplacement of [3H]DPCPX from human A2BAR expressed in HEK293 cell membrane incubated for 30 mins by microbeta trilux scintillation counter analysis
ChEMBL None None None N#Cc1c(-c2ccccc2)nc(N)nc1-c1ccco1 10.1021/acs.jmedchem.1c01636
11584826 73034 None 0 Human Binding pKi = 7.7 7.7 -1 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 552 10 4 10 1.7 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)c4c(NC(=O)O)[nH]c(=O)n(C)c4=O)cc3)cc2n(CCC)c1=O 10.1021/jm0506221
CHEMBL201026 73034 None 0 Human Binding pKi = 7.7 7.7 -1 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 552 10 4 10 1.7 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)c4c(NC(=O)O)[nH]c(=O)n(C)c4=O)cc3)cc2n(CCC)c1=O 10.1021/jm0506221
46837562 10722 None 0 Human Binding pKi = 7.7 7.7 - 1
Displacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells after 30 minsDisplacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells after 30 mins
ChEMBL 496 7 3 5 3.9 CCCn1c(=O)[nH]c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(Br)cc4)cc3)cc21 10.1016/j.ejmech.2010.03.011
CHEMBL1170990 10722 None 0 Human Binding pKi = 7.7 7.7 - 1
Displacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells after 30 minsDisplacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells after 30 mins
ChEMBL 496 7 3 5 3.9 CCCn1c(=O)[nH]c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(Br)cc4)cc3)cc21 10.1016/j.ejmech.2010.03.011
136396061 159032 None 0 Human Binding pKi = 6.7 6.7 - 1
Displacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting methodDisplacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting method
ChEMBL 510 9 1 9 2.9 CCCn1c(=O)c2[nH]c(-c3cc(OCC4CC(=O)N(c5ccc(F)cc5)C4)no3)nc2n(CCC)c1=O 10.1016/j.ejmech.2016.11.007
CHEMBL4096730 159032 None 0 Human Binding pKi = 6.7 6.7 - 1
Displacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting methodDisplacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting method
ChEMBL 510 9 1 9 2.9 CCCn1c(=O)c2[nH]c(-c3cc(OCC4CC(=O)N(c5ccc(F)cc5)C4)no3)nc2n(CCC)c1=O 10.1016/j.ejmech.2016.11.007
459 2618 None 34 Human Binding pKi = 5.7 5.7 -389 5
Displacement of [3H]-DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins
ChEMBL 432 6 2 9 3.8 CCCn1cc2c(n1)nc(n1c2nc(n1)c1ccco1)NC(=O)Nc1ccc(cc1)OC 10.1016/j.bmc.2011.11.037
477 2618 None 34 Human Binding pKi = 5.7 5.7 -389 5
Displacement of [3H]-DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins
ChEMBL 432 6 2 9 3.8 CCCn1cc2c(n1)nc(n1c2nc(n1)c1ccco1)NC(=O)Nc1ccc(cc1)OC 10.1016/j.bmc.2011.11.037
5310960 2618 None 34 Human Binding pKi = 5.7 5.7 -389 5
Displacement of [3H]-DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins
ChEMBL 432 6 2 9 3.8 CCCn1cc2c(n1)nc(n1c2nc(n1)c1ccco1)NC(=O)Nc1ccc(cc1)OC 10.1016/j.bmc.2011.11.037
CHEMBL302765 2618 None 34 Human Binding pKi = 5.7 5.7 -389 5
Displacement of [3H]-DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins
ChEMBL 432 6 2 9 3.8 CCCn1cc2c(n1)nc(n1c2nc(n1)c1ccco1)NC(=O)Nc1ccc(cc1)OC 10.1016/j.bmc.2011.11.037
135489505 139744 None 0 Human Binding pKi = 5.7 5.7 - 1
Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cellsDisplacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells
ChEMBL 344 6 1 7 1.9 CCCn1c(=O)c2nc(-c3cc(C)nn3CC)[nH]c2n(CCC)c1=O 10.1021/jm051268+
CHEMBL379838 139744 None 0 Human Binding pKi = 5.7 5.7 - 1
Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cellsDisplacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells
ChEMBL 344 6 1 7 1.9 CCCn1c(=O)c2nc(-c3cc(C)nn3CC)[nH]c2n(CCC)c1=O 10.1021/jm051268+
52947452 19312 None 0 Human Binding pKi = 6.7 6.7 3 2
Displacement of [3H]ZM241385 from human adenosine A2B receptor transfected in CHO cells after 60 mins by scintillation countingDisplacement of [3H]ZM241385 from human adenosine A2B receptor transfected in CHO cells after 60 mins by scintillation counting
ChEMBL 558 9 2 5 4.7 CS(=O)(=O)c1c(CCc2ccccc2)c2cc(OCC(=O)NCc3ccc(Cl)c(Cl)c3)ccc2[nH]c1=O 10.1016/j.bmcl.2010.10.030
CHEMBL1290543 19312 None 0 Human Binding pKi = 6.7 6.7 3 2
Displacement of [3H]ZM241385 from human adenosine A2B receptor transfected in CHO cells after 60 mins by scintillation countingDisplacement of [3H]ZM241385 from human adenosine A2B receptor transfected in CHO cells after 60 mins by scintillation counting
ChEMBL 558 9 2 5 4.7 CS(=O)(=O)c1c(CCc2ccccc2)c2cc(OCC(=O)NCc3ccc(Cl)c(Cl)c3)ccc2[nH]c1=O 10.1016/j.bmcl.2010.10.030
21874755 176892 None 1 Human Binding pKi = 5.7 5.7 -2 4
Displacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation countingDisplacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation counting
ChEMBL 336 4 2 8 1.8 Nc1nc(-c2ccco2)c2nnn(Cc3cccc(C(=O)O)c3)c2n1 10.1021/jm800961g
CHEMBL461656 176892 None 1 Human Binding pKi = 5.7 5.7 -2 4
Displacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation countingDisplacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation counting
ChEMBL 336 4 2 8 1.8 Nc1nc(-c2ccco2)c2nnn(Cc3cccc(C(=O)O)c3)c2n1 10.1021/jm800961g
380 1287 None 54 Human Binding pKi = 4.7 4.7 -17782 13
Displacement of [3H]- ZM-241385 from human adenosine A2B receptor expressed in HEK cellsDisplacement of [3H]- ZM-241385 from human adenosine A2B receptor expressed in HEK cells
ChEMBL 335 4 4 9 -0.2 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NC1CCCC1 10.1021/jm9905965
657378 1287 None 54 Human Binding pKi = 4.7 4.7 -17782 13
Displacement of [3H]- ZM-241385 from human adenosine A2B receptor expressed in HEK cellsDisplacement of [3H]- ZM-241385 from human adenosine A2B receptor expressed in HEK cells
ChEMBL 335 4 4 9 -0.2 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NC1CCCC1 10.1021/jm9905965
CHEMBL68738 1287 None 54 Human Binding pKi = 4.7 4.7 -17782 13
Displacement of [3H]- ZM-241385 from human adenosine A2B receptor expressed in HEK cellsDisplacement of [3H]- ZM-241385 from human adenosine A2B receptor expressed in HEK cells
ChEMBL 335 4 4 9 -0.2 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NC1CCCC1 10.1021/jm9905965
11610747 73121 None 0 Human Binding pKi = 6.7 6.7 53 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 387 8 2 7 1.2 COCCCn1c(=O)n(C)c(=O)c2[nH]c(-c3ccc(OCC(=O)O)cc3)cc21 10.1021/jm0506221
CHEMBL201133 73121 None 0 Human Binding pKi = 6.7 6.7 53 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 387 8 2 7 1.2 COCCCn1c(=O)n(C)c(=O)c2[nH]c(-c3ccc(OCC(=O)O)cc3)cc21 10.1021/jm0506221
11510891 73409 None 0 Human Binding pKi = 6.7 6.7 2 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 459 6 2 8 2.1 COc1cc(-c2cc3c([nH]2)c(=O)n(C)c(=O)n3C)ccc1OCC(=O)Nc1ccc(C#N)cc1 10.1021/jm0506221
CHEMBL201585 73409 None 0 Human Binding pKi = 6.7 6.7 2 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 459 6 2 8 2.1 COc1cc(-c2cc3c([nH]2)c(=O)n(C)c(=O)n3C)ccc1OCC(=O)Nc1ccc(C#N)cc1 10.1021/jm0506221
162673131 182997 None 0 Human Binding pKi = 5.7 5.7 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 294 4 2 4 2.6 CC1=C(C(=O)OCC(C)C)C(c2cccs2)NC(=O)N1 10.1021/acs.jmedchem.0c01431
CHEMBL4793530 182997 None 0 Human Binding pKi = 5.7 5.7 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 294 4 2 4 2.6 CC1=C(C(=O)OCC(C)C)C(c2cccs2)NC(=O)N1 10.1021/acs.jmedchem.0c01431
372 58 None 103 Human Binding pKi = 4.7 4.7 -2630 9
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 301 2 4 9 -1.3 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2N 10.1021/jm900413e
8974 58 None 103 Human Binding pKi = 4.7 4.7 -2630 9
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 301 2 4 9 -1.3 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2N 10.1021/jm900413e
CHEMBL285819 58 None 103 Human Binding pKi = 4.7 4.7 -2630 9
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 301 2 4 9 -1.3 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2N 10.1021/jm900413e
44410555 169013 None 0 Human Binding pKi = 4.7 4.7 -15848 4
Displacement of [125I]ABOPX from human adenosine A2B receptor in HEK cellsDisplacement of [125I]ABOPX from human adenosine A2B receptor in HEK cells
ChEMBL 450 6 4 9 0.6 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC)nc(C#CCc4ccccc4)nc32)[C@H](O)[C@@H]1O 10.1016/j.bmcl.2006.01.110
CHEMBL439335 169013 None 0 Human Binding pKi = 4.7 4.7 -15848 4
Displacement of [125I]ABOPX from human adenosine A2B receptor in HEK cellsDisplacement of [125I]ABOPX from human adenosine A2B receptor in HEK cells
ChEMBL 450 6 4 9 0.6 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC)nc(C#CCc4ccccc4)nc32)[C@H](O)[C@@H]1O 10.1016/j.bmcl.2006.01.110
44390545 62509 None 0 Human Binding pKi = 6.7 6.7 -5 3
Binding affinity for adenosine A2b receptor by using as [3H]ZM-241385 (14 nM) radioligand in membranes from HEK-A2B cellsBinding affinity for adenosine A2b receptor by using as [3H]ZM-241385 (14 nM) radioligand in membranes from HEK-A2B cells
ChEMBL 504 9 1 9 4.1 CCCn1c(=O)c2nc(-c3ccc(OCc4nc(-c5ccc(F)cc5)no4)cc3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2004.11.044
CHEMBL178172 62509 None 0 Human Binding pKi = 6.7 6.7 -5 3
Binding affinity for adenosine A2b receptor by using as [3H]ZM-241385 (14 nM) radioligand in membranes from HEK-A2B cellsBinding affinity for adenosine A2b receptor by using as [3H]ZM-241385 (14 nM) radioligand in membranes from HEK-A2B cells
ChEMBL 504 9 1 9 4.1 CCCn1c(=O)c2nc(-c3ccc(OCc4nc(-c5ccc(F)cc5)no4)cc3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2004.11.044
44390545 62509 None 0 Human Binding pKi = 6.7 6.7 -5 3
Binding affinity for adenosine A2b receptor by using as [3H]ZM-241385 radioligand in membranes from HEK-A2B cellsBinding affinity for adenosine A2b receptor by using as [3H]ZM-241385 radioligand in membranes from HEK-A2B cells
ChEMBL 504 9 1 9 4.1 CCCn1c(=O)c2nc(-c3ccc(OCc4nc(-c5ccc(F)cc5)no4)cc3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2004.11.044
CHEMBL178172 62509 None 0 Human Binding pKi = 6.7 6.7 -5 3
Binding affinity for adenosine A2b receptor by using as [3H]ZM-241385 radioligand in membranes from HEK-A2B cellsBinding affinity for adenosine A2b receptor by using as [3H]ZM-241385 radioligand in membranes from HEK-A2B cells
ChEMBL 504 9 1 9 4.1 CCCn1c(=O)c2nc(-c3ccc(OCc4nc(-c5ccc(F)cc5)no4)cc3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2004.11.044
156011975 177313 None 0 Human Binding pKi = 6.7 6.7 - 1
Displacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting methodDisplacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting method
ChEMBL 340 3 1 7 3.3 CCOC(=O)C1=C(C)Nc2nc3ccccc3n2C1c1cncs1 10.1021/acs.jmedchem.0c00564
CHEMBL4636932 177313 None 0 Human Binding pKi = 6.7 6.7 - 1
Displacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting methodDisplacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting method
ChEMBL 340 3 1 7 3.3 CCOC(=O)C1=C(C)Nc2nc3ccccc3n2C1c1cncs1 10.1021/acs.jmedchem.0c00564
10971806 56844 None 0 Human Binding pKi = 6.7 6.7 -7 4
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 184-250Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 184-250
ChEMBL 418 5 2 9 3.4 CCn1cc2c(nc(NC(=O)Nc3cccc(OC)c3)n3nc(-c4ccco4)nc23)n1 10.1021/jm0109614
CHEMBL164381 56844 None 0 Human Binding pKi = 6.7 6.7 -7 4
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 184-250Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 184-250
ChEMBL 418 5 2 9 3.4 CCn1cc2c(nc(NC(=O)Nc3cccc(OC)c3)n3nc(-c4ccco4)nc23)n1 10.1021/jm0109614
145988962 167241 None 0 Human Binding pKi = 6.7 6.7 -1 4
Displacement of [3H]PSB-602 from human adenosine A2B receptor expressed in CHO cell membranesDisplacement of [3H]PSB-602 from human adenosine A2B receptor expressed in CHO cell membranes
ChEMBL 635 17 2 10 4.2 CCCCn1c(=O)c2c(nc3n2CCCN3CCc2ccc(OCC(=O)NCCCNC3CCCCC3)cc2)n(CCCC)c1=O 10.1039/C8MD00070K
CHEMBL4292514 167241 None 0 Human Binding pKi = 6.7 6.7 -1 4
Displacement of [3H]PSB-602 from human adenosine A2B receptor expressed in CHO cell membranesDisplacement of [3H]PSB-602 from human adenosine A2B receptor expressed in CHO cell membranes
ChEMBL 635 17 2 10 4.2 CCCCn1c(=O)c2c(nc3n2CCCN3CCc2ccc(OCC(=O)NCCCNC3CCCCC3)cc2)n(CCCC)c1=O 10.1039/C8MD00070K
14978313 102655 None 0 Rat Binding pKi = 5.7 5.7 -4 5
Inhibition of [125I]-APOBX binding to rat Adenosine A2B receptor expressed in HEK cellsInhibition of [125I]-APOBX binding to rat Adenosine A2B receptor expressed in HEK cells
ChEMBL 204 1 1 5 -0.9 C#CCn1c(=O)c2[nH]cnc2n(C)c1=O 10.1021/jm0104318
CHEMBL304455 102655 None 0 Rat Binding pKi = 5.7 5.7 -4 5
Inhibition of [125I]-APOBX binding to rat Adenosine A2B receptor expressed in HEK cellsInhibition of [125I]-APOBX binding to rat Adenosine A2B receptor expressed in HEK cells
ChEMBL 204 1 1 5 -0.9 C#CCn1c(=O)c2[nH]cnc2n(C)c1=O 10.1021/jm0104318
2867529 51890 None 8 Human Binding pKi = 5.7 5.7 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 236 2 2 4 1.1 COC(=O)C1=C(C)NC(=O)NC1c1ccco1 10.1021/acs.jmedchem.0c01431
CHEMBL1585743 51890 None 8 Human Binding pKi = 5.7 5.7 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 236 2 2 4 1.1 COC(=O)C1=C(C)NC(=O)NC1c1ccco1 10.1021/acs.jmedchem.0c01431
2867529 51890 None 8 Human Binding pKi = 5.7 5.7 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by Scatchard plot analysisDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by Scatchard plot analysis
ChEMBL 236 2 2 4 1.1 COC(=O)C1=C(C)NC(=O)NC1c1ccco1 10.1021/ml400185v
CHEMBL1585743 51890 None 8 Human Binding pKi = 5.7 5.7 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by Scatchard plot analysisDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by Scatchard plot analysis
ChEMBL 236 2 2 4 1.1 COC(=O)C1=C(C)NC(=O)NC1c1ccco1 10.1021/ml400185v
44307909 103064 None 1 Human Binding pKi = 4.7 4.7 - 1
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 219 1 0 7 -1.0 Cn1cnc2c1c(=O)n(CC#N)c(=O)n2C 10.1021/jm0104318
CHEMBL307326 103064 None 1 Human Binding pKi = 4.7 4.7 - 1
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 219 1 0 7 -1.0 Cn1cnc2c1c(=O)n(CC#N)c(=O)n2C 10.1021/jm0104318
CHEMBL5076095 214414 None 0 Human Binding pKi = 6.7 6.7 -32 3
Displacement of [3H]DPCPX from human A2BAR expressed in HEK293 cell membrane incubated for 30 mins by microbeta trilux scintillation counter analysisDisplacement of [3H]DPCPX from human A2BAR expressed in HEK293 cell membrane incubated for 30 mins by microbeta trilux scintillation counter analysis
ChEMBL None None None CCNc1nc(-c2ccccc2)c(C#N)c(-c2ccc3c(c2)OCO3)n1 10.1021/acs.jmedchem.1c01636
11560108 169067 None 0 Human Binding pKi = 5.7 5.7 - 1
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 387 6 1 8 1.2 CCOC(=O)COc1ccc(-c2cc3c([nH]2)c(=O)n(C)c(=O)n3C)c(OC)c1 10.1021/jm0506221
CHEMBL439684 169067 None 0 Human Binding pKi = 5.7 5.7 - 1
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 387 6 1 8 1.2 CCOC(=O)COc1ccc(-c2cc3c([nH]2)c(=O)n(C)c(=O)n3C)c(OC)c1 10.1021/jm0506221
127038753 136657 None 0 Human Binding pKi = 5.7 5.7 -165 3
Displacement of [3H]-DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by liquid scintillation counting analysis
ChEMBL 466 7 4 13 0.5 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(N[C@H](C)Cc5ccccc5)nc43)[C@H](O)[C@@H]2O)n1 10.1039/C5MD00086F
CHEMBL3740085 136657 None 0 Human Binding pKi = 5.7 5.7 -165 3
Displacement of [3H]-DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by liquid scintillation counting analysis
ChEMBL 466 7 4 13 0.5 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(N[C@H](C)Cc5ccccc5)nc43)[C@H](O)[C@@H]2O)n1 10.1039/C5MD00086F
11270783 1226 None 35 Human Binding pKi = 7.7 7.7 67 4
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 446 6 1 7 3.2 CCCn1c(=O)c2nc([nH]c2n(c1=O)CC)c1cnn(c1)Cc1cccc(c1)C(F)(F)F 10.1021/jm900413e
5615 1226 None 35 Human Binding pKi = 7.7 7.7 67 4
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 446 6 1 7 3.2 CCCn1c(=O)c2nc([nH]c2n(c1=O)CC)c1cnn(c1)Cc1cccc(c1)C(F)(F)F 10.1021/jm900413e
CHEMBL260933 1226 None 35 Human Binding pKi = 7.7 7.7 67 4
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 446 6 1 7 3.2 CCCn1c(=O)c2nc([nH]c2n(c1=O)CC)c1cnn(c1)Cc1cccc(c1)C(F)(F)F 10.1021/jm900413e
DB05936 1226 None 35 Human Binding pKi = 7.7 7.7 67 4
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 446 6 1 7 3.2 CCCn1c(=O)c2nc([nH]c2n(c1=O)CC)c1cnn(c1)Cc1cccc(c1)C(F)(F)F 10.1021/jm900413e
22266771 94624 None 0 Human Binding pKi = 7.7 7.7 - 1
Displacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranesDisplacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranes
ChEMBL 417 6 2 8 2.4 CCCn1c(=O)[nH]c2nc(-c3cnn(Cc4cc(-c5ccccc5)on4)c3)[nH]c2c1=O 10.1016/j.bmcl.2008.01.008
CHEMBL252272 94624 None 0 Human Binding pKi = 7.7 7.7 - 1
Displacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranesDisplacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranes
ChEMBL 417 6 2 8 2.4 CCCn1c(=O)[nH]c2nc(-c3cnn(Cc4cc(-c5ccccc5)on4)c3)[nH]c2c1=O 10.1016/j.bmcl.2008.01.008
10296638 36769 None 0 Human Binding pKi = 7.7 7.7 -4 4
Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 19-27Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 19-27
ChEMBL 434 4 2 7 4.8 COc1ccc(NC(=O)Nc2nc3ccc(Cl)cc3c3nc(-c4ccco4)nn23)cc1 10.1021/jm001047y
CHEMBL144979 36769 None 0 Human Binding pKi = 7.7 7.7 -4 4
Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 19-27Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 19-27
ChEMBL 434 4 2 7 4.8 COc1ccc(NC(=O)Nc2nc3ccc(Cl)cc3c3nc(-c4ccco4)nn23)cc1 10.1021/jm001047y
10296638 36769 None 0 Human Binding pKi = 7.7 7.7 -4 4
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 19-27Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 19-27
ChEMBL 434 4 2 7 4.8 COc1ccc(NC(=O)Nc2nc3ccc(Cl)cc3c3nc(-c4ccco4)nn23)cc1 10.1021/jm0109614
CHEMBL144979 36769 None 0 Human Binding pKi = 7.7 7.7 -4 4
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 19-27Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 19-27
ChEMBL 434 4 2 7 4.8 COc1ccc(NC(=O)Nc2nc3ccc(Cl)cc3c3nc(-c4ccco4)nn23)cc1 10.1021/jm0109614
11826924 118745 None 0 Human Binding pKi = 7.7 7.7 -1 4
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 479 8 1 9 4.0 O=C(COc1ccccc1)Nc1nc2nn(CCc3ccccc3)cc2c2nc(-c3ccco3)nn12 10.1021/jm030852k
CHEMBL341777 118745 None 0 Human Binding pKi = 7.7 7.7 -1 4
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 479 8 1 9 4.0 O=C(COc1ccccc1)Nc1nc2nn(CCc3ccccc3)cc2c2nc(-c3ccco3)nn12 10.1021/jm030852k
136042334 71161 None 0 Human Binding pKi = 7.7 7.7 33 2
Displacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation countingDisplacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation counting
ChEMBL 490 8 2 9 3.2 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5cc(C)c(C)cc5[nH]4)nn3C)nc2n(CCC)c1=O 10.1021/jm201292w
CHEMBL1955910 71161 None 0 Human Binding pKi = 7.7 7.7 33 2
Displacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation countingDisplacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation counting
ChEMBL 490 8 2 9 3.2 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5cc(C)c(C)cc5[nH]4)nn3C)nc2n(CCC)c1=O 10.1021/jm201292w
136042344 71170 None 0 Human Binding pKi = 7.7 7.7 - 1
Displacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation countingDisplacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation counting
ChEMBL 551 8 2 9 4.5 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5c(Cl)cc(C(F)(F)F)cc5[nH]4)no3)nc2n(CCC)c1=O 10.1021/jm201292w
CHEMBL1955920 71170 None 0 Human Binding pKi = 7.7 7.7 - 1
Displacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation countingDisplacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation counting
ChEMBL 551 8 2 9 4.5 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5c(Cl)cc(C(F)(F)F)cc5[nH]4)no3)nc2n(CCC)c1=O 10.1021/jm201292w
21958701 72992 None 0 Human Binding pKi = 7.7 7.7 4 4
Displacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cellsDisplacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cells
ChEMBL 469 8 2 8 2.9 CCCn1c(=O)c2nc(-c3cnn(CC(=O)Nc4ccccc4Cl)c3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2005.10.002
CHEMBL200780 72992 None 0 Human Binding pKi = 7.7 7.7 4 4
Displacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cellsDisplacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cells
ChEMBL 469 8 2 8 2.9 CCCn1c(=O)c2nc(-c3cnn(CC(=O)Nc4ccccc4Cl)c3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2005.10.002
11270783 1226 None 35 Human Binding pKi = 7.7 7.7 67 4
Displacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 446 6 1 7 3.2 CCCn1c(=O)c2nc([nH]c2n(c1=O)CC)c1cnn(c1)Cc1cccc(c1)C(F)(F)F 10.1021/jm7014815
5615 1226 None 35 Human Binding pKi = 7.7 7.7 67 4
Displacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 446 6 1 7 3.2 CCCn1c(=O)c2nc([nH]c2n(c1=O)CC)c1cnn(c1)Cc1cccc(c1)C(F)(F)F 10.1021/jm7014815
CHEMBL260933 1226 None 35 Human Binding pKi = 7.7 7.7 67 4
Displacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 446 6 1 7 3.2 CCCn1c(=O)c2nc([nH]c2n(c1=O)CC)c1cnn(c1)Cc1cccc(c1)C(F)(F)F 10.1021/jm7014815
DB05936 1226 None 35 Human Binding pKi = 7.7 7.7 67 4
Displacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 446 6 1 7 3.2 CCCn1c(=O)c2nc([nH]c2n(c1=O)CC)c1cnn(c1)Cc1cccc(c1)C(F)(F)F 10.1021/jm7014815
24827444 96344 None 0 Human Binding pKi = 7.7 7.7 14 3
Displacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 365 5 1 8 1.6 CCCn1c(=O)c2[nH]c(-c3cnn(-c4cccnc4)c3)nc2n(CC)c1=O 10.1021/jm7014815
CHEMBL261526 96344 None 0 Human Binding pKi = 7.7 7.7 14 3
Displacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 365 5 1 8 1.6 CCCn1c(=O)c2[nH]c(-c3cnn(-c4cccnc4)c3)nc2n(CC)c1=O 10.1021/jm7014815
21916394 160813 None 0 Human Binding pKi = 7.7 7.7 10 4
Displacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 458 6 1 7 3.2 CCn1c(=O)n(CC2CC2)c(=O)c2[nH]c(-c3cnn(Cc4cccc(C(F)(F)F)c4)c3)nc21 10.1021/jm7014815
CHEMBL411452 160813 None 0 Human Binding pKi = 7.7 7.7 10 4
Displacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 458 6 1 7 3.2 CCn1c(=O)n(CC2CC2)c(=O)c2[nH]c(-c3cnn(Cc4cccc(C(F)(F)F)c4)c3)nc21 10.1021/jm7014815
49797774 10622 None 0 Human Binding pKi = 7.7 7.7 2 3
Displacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cells after 1 hr by scintillation countingDisplacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 462 7 2 7 3.3 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(NS(C)(=O)=O)cc3)sc12 10.1016/j.bmcl.2010.05.056
CHEMBL1170137 10622 None 0 Human Binding pKi = 7.7 7.7 2 3
Displacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cells after 1 hr by scintillation countingDisplacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 462 7 2 7 3.3 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(NS(C)(=O)=O)cc3)sc12 10.1016/j.bmcl.2010.05.056
10237267 10802 None 0 Human Binding pKi = 7.7 7.7 1 3
Displacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cells after 1 hr by scintillation countingDisplacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 373 4 1 5 3.7 COc1ccc(N(C)C(C)=O)c2sc(NC(=O)c3ccc(F)cc3)nc12 10.1016/j.bmcl.2010.05.056
CHEMBL1171898 10802 None 0 Human Binding pKi = 7.7 7.7 1 3
Displacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cells after 1 hr by scintillation countingDisplacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 373 4 1 5 3.7 COc1ccc(N(C)C(C)=O)c2sc(NC(=O)c3ccc(F)cc3)nc12 10.1016/j.bmcl.2010.05.056
9870396 139037 None 0 Human Binding pKi = 7.7 7.7 17 4
Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cellsDisplacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells
ChEMBL 494 7 1 7 4.3 CCCn1c(=O)c2nc(-c3cnn(Cc4cc(C(F)(F)F)ccc4Cl)c3)[nH]c2n(CCC)c1=O 10.1021/jm051268+
CHEMBL378598 139037 None 0 Human Binding pKi = 7.7 7.7 17 4
Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cellsDisplacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells
ChEMBL 494 7 1 7 4.3 CCCn1c(=O)c2nc(-c3cnn(Cc4cc(C(F)(F)F)ccc4Cl)c3)[nH]c2n(CCC)c1=O 10.1021/jm051268+
11654461 139512 None 0 Human Binding pKi = 7.7 7.7 1 3
Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cellsDisplacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells
ChEMBL 410 7 1 7 2.8 CCCn1c(=O)c2nc(-c3cnn(Cc4ccc(F)cc4)c3)[nH]c2n(CCC)c1=O 10.1021/jm051268+
CHEMBL379474 139512 None 0 Human Binding pKi = 7.7 7.7 1 3
Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cellsDisplacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells
ChEMBL 410 7 1 7 2.8 CCCn1c(=O)c2nc(-c3cnn(Cc4ccc(F)cc4)c3)[nH]c2n(CCC)c1=O 10.1021/jm051268+
11495984 72749 None 0 Human Binding pKi = 7.7 7.7 9 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 444 5 2 6 2.4 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)NC4CCc5ccccc54)cc3)cc2n(C)c1=O 10.1021/jm0506221
CHEMBL199884 72749 None 0 Human Binding pKi = 7.7 7.7 9 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 444 5 2 6 2.4 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)NC4CCc5ccccc54)cc3)cc2n(C)c1=O 10.1021/jm0506221
11591823 74813 None 0 Human Binding pKi = 7.6 7.6 3 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 528 9 2 6 5.3 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(Cl)cc4)cc3)c(Cl)c2n(CCC)c1=O 10.1021/jm0506221
CHEMBL203148 74813 None 0 Human Binding pKi = 7.6 7.6 3 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 528 9 2 6 5.3 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(Cl)cc4)cc3)c(Cl)c2n(CCC)c1=O 10.1021/jm0506221
10164201 123781 None 0 Human Binding pKi = 6.7 6.7 - 1
Binding affinity for adenosine A2b receptor by using as [3H]ZM-241385 (14 nM) radioligand in membranes from HEK-A2B cellsBinding affinity for adenosine A2b receptor by using as [3H]ZM-241385 (14 nM) radioligand in membranes from HEK-A2B cells
ChEMBL 504 9 1 9 4.1 CCCn1c(=O)c2nc(-c3ccc(OCc4noc(-c5ccc(F)cc5)n4)cc3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2004.11.044
CHEMBL362268 123781 None 0 Human Binding pKi = 6.7 6.7 - 1
Binding affinity for adenosine A2b receptor by using as [3H]ZM-241385 (14 nM) radioligand in membranes from HEK-A2B cellsBinding affinity for adenosine A2b receptor by using as [3H]ZM-241385 (14 nM) radioligand in membranes from HEK-A2B cells
ChEMBL 504 9 1 9 4.1 CCCn1c(=O)c2nc(-c3ccc(OCc4noc(-c5ccc(F)cc5)n4)cc3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2004.11.044
743242 172054 None 12 Human Binding pKi = 6.7 6.7 -38 3
Displacement of [3H]MRS1754 from human adenosine A2B receptor expressed in CHO cell membraneDisplacement of [3H]MRS1754 from human adenosine A2B receptor expressed in CHO cell membrane
ChEMBL 261 2 1 4 3.5 N#Cc1c(-c2ccco2)cc(-c2ccccc2)nc1N 10.1021/jm701594y
CHEMBL447192 172054 None 12 Human Binding pKi = 6.7 6.7 -38 3
Displacement of [3H]MRS1754 from human adenosine A2B receptor expressed in CHO cell membraneDisplacement of [3H]MRS1754 from human adenosine A2B receptor expressed in CHO cell membrane
ChEMBL 261 2 1 4 3.5 N#Cc1c(-c2ccco2)cc(-c2ccccc2)nc1N 10.1021/jm701594y
853426 40979 None 11 Human Binding pKi = 6.7 6.7 -30 4
Displacement of [3H]PBS603 from human adenosine A2B receptor expressed in CHO cells after 2 hrs by scintillation countingDisplacement of [3H]PBS603 from human adenosine A2B receptor expressed in CHO cells after 2 hrs by scintillation counting
ChEMBL 264 2 2 5 2.5 Nc1nc(-c2ccccc2)nc(-c2ccccc2O)n1 10.1021/jm3003069
CHEMBL1487093 40979 None 11 Human Binding pKi = 6.7 6.7 -30 4
Displacement of [3H]PBS603 from human adenosine A2B receptor expressed in CHO cells after 2 hrs by scintillation countingDisplacement of [3H]PBS603 from human adenosine A2B receptor expressed in CHO cells after 2 hrs by scintillation counting
ChEMBL 264 2 2 5 2.5 Nc1nc(-c2ccccc2)nc(-c2ccccc2O)n1 10.1021/jm3003069
135428628 141463 None 0 Human Binding pKi = 5.7 5.7 -218 3
Displacement of [125I]3-(4-aminobenzyl)-8-phenyloxyacetate-1-propyl-xanthine from human adenosine A2B receptorDisplacement of [125I]3-(4-aminobenzyl)-8-phenyloxyacetate-1-propyl-xanthine from human adenosine A2B receptor
ChEMBL 357 3 2 4 2.5 CCCN1C(=O)N2C[C@@H](C)N=C2c2[nH]c(C34CCC(O)(CC3)CC4)nc21 10.1021/jm060539t
CHEMBL384279 141463 None 0 Human Binding pKi = 5.7 5.7 -218 3
Displacement of [125I]3-(4-aminobenzyl)-8-phenyloxyacetate-1-propyl-xanthine from human adenosine A2B receptorDisplacement of [125I]3-(4-aminobenzyl)-8-phenyloxyacetate-1-propyl-xanthine from human adenosine A2B receptor
ChEMBL 357 3 2 4 2.5 CCCN1C(=O)N2C[C@@H](C)N=C2c2[nH]c(C34CCC(O)(CC3)CC4)nc21 10.1021/jm060539t
9929470 110473 None 0 Human Binding pKi = 6.7 6.7 -44 4
Displacement of [3H]-DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells after 60 mins by scintillation counting analysisDisplacement of [3H]-DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells after 60 mins by scintillation counting analysis
ChEMBL 374 3 2 8 2.9 Cn1cc2c(nc(NC(=O)Nc3ccccc3)n3nc(-c4ccco4)nc23)n1 10.1021/acs.jmedchem.5b00551
CHEMBL324735 110473 None 0 Human Binding pKi = 6.7 6.7 -44 4
Displacement of [3H]-DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells after 60 mins by scintillation counting analysisDisplacement of [3H]-DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells after 60 mins by scintillation counting analysis
ChEMBL 374 3 2 8 2.9 Cn1cc2c(nc(NC(=O)Nc3ccccc3)n3nc(-c4ccco4)nc23)n1 10.1021/acs.jmedchem.5b00551
9929470 110473 None 0 Human Binding pKi = 6.7 6.7 -44 4
Displacement of [3H]DPCPX from Human Adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from Human Adenosine A2B receptor expressed in HEK293 cells
ChEMBL 374 3 2 8 2.9 Cn1cc2c(nc(NC(=O)Nc3ccccc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm020974x
CHEMBL324735 110473 None 0 Human Binding pKi = 6.7 6.7 -44 4
Displacement of [3H]DPCPX from Human Adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from Human Adenosine A2B receptor expressed in HEK293 cells
ChEMBL 374 3 2 8 2.9 Cn1cc2c(nc(NC(=O)Nc3ccccc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm020974x
9929470 110473 None 0 Human Binding pKi = 6.7 6.7 -44 4
Displacement of [3H]DPCPX from human A2B receptor expressed in HEK293 cells by scintillation counterDisplacement of [3H]DPCPX from human A2B receptor expressed in HEK293 cells by scintillation counter
ChEMBL 374 3 2 8 2.9 Cn1cc2c(nc(NC(=O)Nc3ccccc3)n3nc(-c4ccco4)nc23)n1 10.1016/j.ejmech.2015.12.019
CHEMBL324735 110473 None 0 Human Binding pKi = 6.7 6.7 -44 4
Displacement of [3H]DPCPX from human A2B receptor expressed in HEK293 cells by scintillation counterDisplacement of [3H]DPCPX from human A2B receptor expressed in HEK293 cells by scintillation counter
ChEMBL 374 3 2 8 2.9 Cn1cc2c(nc(NC(=O)Nc3ccccc3)n3nc(-c4ccco4)nc23)n1 10.1016/j.ejmech.2015.12.019
9929470 110473 None 0 Human Binding pKi = 6.7 6.7 -44 4
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 181-273Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 181-273
ChEMBL 374 3 2 8 2.9 Cn1cc2c(nc(NC(=O)Nc3ccccc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm0109614
CHEMBL324735 110473 None 0 Human Binding pKi = 6.7 6.7 -44 4
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 181-273Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 181-273
ChEMBL 374 3 2 8 2.9 Cn1cc2c(nc(NC(=O)Nc3ccccc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm0109614
9929470 110473 None 0 Human Binding pKi = 6.7 6.7 -44 4
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 374 3 2 8 2.9 Cn1cc2c(nc(NC(=O)Nc3ccccc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm030852k
CHEMBL324735 110473 None 0 Human Binding pKi = 6.7 6.7 -44 4
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 374 3 2 8 2.9 Cn1cc2c(nc(NC(=O)Nc3ccccc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm030852k
135874432 95798 None 0 Human Binding pKi = 6.7 6.7 - 1
Displacement of [3H]MRE2029F20 from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]MRE2029F20 from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 517 8 2 8 3.8 CCCn1c(=O)c2[nH]c(-c3nn(CC(=O)Nc4ccc(Cl)cc4)c(C)c3Cl)nc2n(CCC)c1=O 10.1016/j.bmc.2007.11.058
CHEMBL258755 95798 None 0 Human Binding pKi = 6.7 6.7 - 1
Displacement of [3H]MRE2029F20 from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]MRE2029F20 from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 517 8 2 8 3.8 CCCn1c(=O)c2[nH]c(-c3nn(CC(=O)Nc4ccc(Cl)cc4)c(C)c3Cl)nc2n(CCC)c1=O 10.1016/j.bmc.2007.11.058
11058550 120131 None 0 Human Binding pKi = 6.7 6.7 -10 4
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 187-265Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 187-265
ChEMBL 404 4 2 9 2.9 COc1ccccc1NC(=O)Nc1nc2nn(C)cc2c2nc(-c3ccco3)nn12 10.1021/jm0109614
CHEMBL351211 120131 None 0 Human Binding pKi = 6.7 6.7 -10 4
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 187-265Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 187-265
ChEMBL 404 4 2 9 2.9 COc1ccccc1NC(=O)Nc1nc2nn(C)cc2c2nc(-c3ccco3)nn12 10.1021/jm0109614
15578103 176786 None 0 Human Binding pKi = 5.7 5.7 - 1
Displacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cells
ChEMBL 285 1 1 6 1.3 Cc1ccc(-c2cc3c(c(=O)n(C)c(=O)n3C)n2O)cc1 10.1016/j.bmc.2008.09.067
CHEMBL460617 176786 None 0 Human Binding pKi = 5.7 5.7 - 1
Displacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cells
ChEMBL 285 1 1 6 1.3 Cc1ccc(-c2cc3c(c(=O)n(C)c(=O)n3C)n2O)cc1 10.1016/j.bmc.2008.09.067
71683092 89938 None 0 Human Binding pKi = 6.7 6.7 -3 6
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells after 75 mins by liquid scintillation counting analysisDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells after 75 mins by liquid scintillation counting analysis
ChEMBL 340 5 1 5 3.2 COc1cccc(CCC(=O)Nc2nc3ccccc3c(=O)s2)c1 10.1021/jm400336x
CHEMBL2380386 89938 None 0 Human Binding pKi = 6.7 6.7 -3 6
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells after 75 mins by liquid scintillation counting analysisDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells after 75 mins by liquid scintillation counting analysis
ChEMBL 340 5 1 5 3.2 COc1cccc(CCC(=O)Nc2nc3ccccc3c(=O)s2)c1 10.1021/jm400336x
21874687 172641 None 0 Human Binding pKi = 6.7 6.7 -15 4
Displacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation countingDisplacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation counting
ChEMBL 293 3 1 8 1.5 Nc1nc(-c2ccco2)c2nnn(Cc3cccnc3)c2n1 10.1021/jm800961g
CHEMBL449596 172641 None 0 Human Binding pKi = 6.7 6.7 -15 4
Displacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation countingDisplacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation counting
ChEMBL 293 3 1 8 1.5 Nc1nc(-c2ccco2)c2nnn(Cc3cccnc3)c2n1 10.1021/jm800961g
11026434 57492 None 0 Human Binding pKi = 6.7 6.7 -10 4
Displacement of [3H]DPCPX binding at human Adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX binding at human Adenosine A2B receptor expressed in HEK293 cells
ChEMBL 433 5 2 10 3.3 CCn1cc2c(nc(NC(=O)Nc3ccc([N+](=O)[O-])cc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm0109614
CHEMBL165910 57492 None 0 Human Binding pKi = 6.7 6.7 -10 4
Displacement of [3H]DPCPX binding at human Adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX binding at human Adenosine A2B receptor expressed in HEK293 cells
ChEMBL 433 5 2 10 3.3 CCn1cc2c(nc(NC(=O)Nc3ccc([N+](=O)[O-])cc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm0109614
10601859 119150 None 0 Human Binding pKi = 6.7 6.7 -1 5
Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 183-278Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 183-278
ChEMBL 512 7 2 8 5.7 O=C(Nc1cccc(Cl)c1)Nc1nc2nn(CCCc3ccccc3)cc2c2nc(-c3ccco3)nn12 10.1021/jm001047y
CHEMBL342906 119150 None 0 Human Binding pKi = 6.7 6.7 -1 5
Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 183-278Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 183-278
ChEMBL 512 7 2 8 5.7 O=C(Nc1cccc(Cl)c1)Nc1nc2nn(CCCc3ccccc3)cc2c2nc(-c3ccco3)nn12 10.1021/jm001047y
10453097 197893 None 0 Human Binding pKi = 6.7 6.7 -20 4
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 183-278Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 183-278
ChEMBL 392 3 2 8 3.1 Cn1cc2c(nc(NC(=O)Nc3ccc(F)cc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm0109614
CHEMBL572765 197893 None 0 Human Binding pKi = 6.7 6.7 -20 4
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 183-278Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 183-278
ChEMBL 392 3 2 8 3.1 Cn1cc2c(nc(NC(=O)Nc3ccc(F)cc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm0109614
21874676 189463 None 0 Human Binding pKi = 6.7 6.7 -112 4
Displacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation countingDisplacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation counting
ChEMBL 328 3 1 7 2.4 Nc1nc(-c2ccco2)c2nnn(Cc3ccc(F)cc3F)c2n1 10.1021/jm800961g
CHEMBL513661 189463 None 0 Human Binding pKi = 6.7 6.7 -112 4
Displacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation countingDisplacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation counting
ChEMBL 328 3 1 7 2.4 Nc1nc(-c2ccco2)c2nnn(Cc3ccc(F)cc3F)c2n1 10.1021/jm800961g
11157262 123640 None 0 Human Binding pKi = 5.7 5.7 -446 4
Inhibition of [3H]DPCPX binding to human adenosine A2B receptor expressed in HEK293 cellsInhibition of [3H]DPCPX binding to human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 560 8 5 14 0.2 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(N[C@H](CO)Cc5ccc(Br)cc5)nc43)[C@H](O)[C@@H]2O)n1 10.1021/jm031143+
CHEMBL361925 123640 None 0 Human Binding pKi = 5.7 5.7 -446 4
Inhibition of [3H]DPCPX binding to human adenosine A2B receptor expressed in HEK293 cellsInhibition of [3H]DPCPX binding to human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 560 8 5 14 0.2 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(N[C@H](CO)Cc5ccc(Br)cc5)nc43)[C@H](O)[C@@H]2O)n1 10.1021/jm031143+
9995603 100327 None 0 Human Binding pKi = 6.6 6.6 -17 5
Displacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cells
ChEMBL 311 5 1 4 3.0 CCCn1c(=O)c2[nH]c(-c3ccccc3)cc2n(CCC)c1=O 10.1016/j.bmc.2008.09.067
CHEMBL289413 100327 None 0 Human Binding pKi = 6.6 6.6 -17 5
Displacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cells
ChEMBL 311 5 1 4 3.0 CCCn1c(=O)c2[nH]c(-c3ccccc3)cc2n(CCC)c1=O 10.1016/j.bmc.2008.09.067
11213889 206457 None 0 Human Binding pKi = 7.6 7.6 -3 3
Binding affinity for human adenosine A2B receptor using [3H]-PSB-298 in CHO cell membranesBinding affinity for human adenosine A2B receptor using [3H]-PSB-298 in CHO cell membranes
ChEMBL 485 8 2 9 2.6 CCCCn1c(=O)[nH]c2[nH]c(-c3ccc(S(=O)(=O)Oc4cccc([N+](=O)[O-])c4)cc3)nc2c1=O 10.1021/jm0310030
CHEMBL8810 206457 None 0 Human Binding pKi = 7.6 7.6 -3 3
Binding affinity for human adenosine A2B receptor using [3H]-PSB-298 in CHO cell membranesBinding affinity for human adenosine A2B receptor using [3H]-PSB-298 in CHO cell membranes
ChEMBL 485 8 2 9 2.6 CCCCn1c(=O)[nH]c2[nH]c(-c3ccc(S(=O)(=O)Oc4cccc([N+](=O)[O-])c4)cc3)nc2c1=O 10.1021/jm0310030
10961304 76012 None 0 Human Binding pKi = 7.6 7.6 -2 4
Displacement of [3H]- DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]- DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 447 6 3 10 3.4 CCNc1c2c(nc(NC(=O)Nc3ccc(OC)cc3)n3nc(-c4ccco4)nc23)nn1C 10.1021/jm021023m
CHEMBL20555 76012 None 0 Human Binding pKi = 7.6 7.6 -2 4
Displacement of [3H]- DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]- DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 447 6 3 10 3.4 CCNc1c2c(nc(NC(=O)Nc3ccc(OC)cc3)n3nc(-c4ccco4)nc23)nn1C 10.1021/jm021023m
CHEMBL554955 76012 None 0 Human Binding pKi = 7.6 7.6 -2 4
Displacement of [3H]- DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]- DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 447 6 3 10 3.4 CCNc1c2c(nc(NC(=O)Nc3ccc(OC)cc3)n3nc(-c4ccco4)nc23)nn1C 10.1021/jm021023m
137642862 158459 None 0 Human Binding pKi = 7.6 7.6 - 1
Displacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 minsDisplacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 mins
ChEMBL 354 6 1 7 1.6 CC#CCn1cc(-c2nc3c([nH]2)c(=O)n(CCC)c(=O)n3CCC)cn1 10.1016/j.ejmech.2017.04.014
CHEMBL4090649 158459 None 0 Human Binding pKi = 7.6 7.6 - 1
Displacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 minsDisplacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 mins
ChEMBL 354 6 1 7 1.6 CC#CCn1cc(-c2nc3c([nH]2)c(=O)n(CCC)c(=O)n3CCC)cn1 10.1016/j.ejmech.2017.04.014
137661874 159302 None 0 Human Binding pKi = 7.6 7.6 -60 3
Displacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes measured after 90 minsDisplacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes measured after 90 mins
ChEMBL 405 4 2 7 3.0 COc1ccc(N2CCOCC2)c2sc(NC(=O)C3(C)CCC(O)CC3)nc12 10.1021/acs.jmedchem.6b01584
CHEMBL4099688 159302 None 0 Human Binding pKi = 7.6 7.6 -60 3
Displacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes measured after 90 minsDisplacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes measured after 90 mins
ChEMBL 405 4 2 7 3.0 COc1ccc(N2CCOCC2)c2sc(NC(=O)C3(C)CCC(O)CC3)nc12 10.1021/acs.jmedchem.6b01584
66892501 156710 None 0 Human Binding pKi = 7.6 7.6 - 1
Displacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting methodDisplacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting method
ChEMBL 500 8 1 9 2.5 CCCn1c(=O)c2[nH]c(-c3cnn(CC4CC(=O)N(c5ccc(C#N)cc5)C4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2016.11.007
CHEMBL4070150 156710 None 0 Human Binding pKi = 7.6 7.6 - 1
Displacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting methodDisplacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting method
ChEMBL 500 8 1 9 2.5 CCCn1c(=O)c2[nH]c(-c3cnn(CC4CC(=O)N(c5ccc(C#N)cc5)C4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2016.11.007
10310768 94565 None 0 Human Binding pKi = 7.6 7.6 - 1
Displacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranesDisplacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranes
ChEMBL 466 7 2 9 2.8 CCCCn1c(=O)[nH]c2nc(-c3cnn(Cc4noc(-c5ccc(Cl)cc5)n4)c3)[nH]c2c1=O 10.1016/j.bmcl.2008.01.008
CHEMBL251878 94565 None 0 Human Binding pKi = 7.6 7.6 - 1
Displacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranesDisplacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranes
ChEMBL 466 7 2 9 2.8 CCCCn1c(=O)[nH]c2nc(-c3cnn(Cc4noc(-c5ccc(Cl)cc5)n4)c3)[nH]c2c1=O 10.1016/j.bmcl.2008.01.008
2690 903 None 66 Human Binding pKi = 7.6 7.6 -30 9
Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 18-29Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 18-29
ChEMBL 285 1 1 6 2.8 Clc1ccc2c(c1)c1nc(nn1c(n2)N)c1ccco1 10.1021/jm001047y
384 903 None 66 Human Binding pKi = 7.6 7.6 -30 9
Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 18-29Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 18-29
ChEMBL 285 1 1 6 2.8 Clc1ccc2c(c1)c1nc(nn1c(n2)N)c1ccco1 10.1021/jm001047y
CHEMBL16687 903 None 66 Human Binding pKi = 7.6 7.6 -30 9
Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 18-29Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 18-29
ChEMBL 285 1 1 6 2.8 Clc1ccc2c(c1)c1nc(nn1c(n2)N)c1ccco1 10.1021/jm001047y
11952560 6337 None 1 Human Binding pKi = 7.6 7.6 20 3
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 263 2 1 5 2.7 c1coc(-c2nc3[nH]ncc3cc2-c2ccncn2)c1 10.1016/j.bmcl.2010.01.077
CHEMBL1082002 6337 None 1 Human Binding pKi = 7.6 7.6 20 3
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 263 2 1 5 2.7 c1coc(-c2nc3[nH]ncc3cc2-c2ccncn2)c1 10.1016/j.bmcl.2010.01.077
44588518 174167 None 0 Human Binding pKi = 7.6 7.6 4 2
Displacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cells
ChEMBL 317 5 2 6 2.3 CCCn1c(=O)c2[nH]c(-c3ccco3)c(O)c2n(CCC)c1=O 10.1016/j.bmc.2008.09.067
CHEMBL454700 174167 None 0 Human Binding pKi = 7.6 7.6 4 2
Displacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cells
ChEMBL 317 5 2 6 2.3 CCCn1c(=O)c2[nH]c(-c3ccco3)c(O)c2n(CCC)c1=O 10.1016/j.bmc.2008.09.067
136042338 71164 None 0 Human Binding pKi = 7.6 7.6 12 2
Displacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation countingDisplacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation counting
ChEMBL 449 8 2 9 2.8 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5ccccc5[nH]4)no3)nc2n(CCC)c1=O 10.1021/jm201292w
CHEMBL1955914 71164 None 0 Human Binding pKi = 7.6 7.6 12 2
Displacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation countingDisplacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation counting
ChEMBL 449 8 2 9 2.8 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5ccccc5[nH]4)no3)nc2n(CCC)c1=O 10.1021/jm201292w
49797750 10753 None 0 Human Binding pKi = 7.6 7.6 3 3
Displacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cells after 1 hr by scintillation countingDisplacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 437 6 1 9 2.9 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(-n4cnnn4)cc3)sc12 10.1016/j.bmcl.2010.05.056
CHEMBL1171349 10753 None 0 Human Binding pKi = 7.6 7.6 3 3
Displacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cells after 1 hr by scintillation countingDisplacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 437 6 1 9 2.9 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(-n4cnnn4)cc3)sc12 10.1016/j.bmcl.2010.05.056
21874571 189863 None 0 Human Binding pKi = 7.6 7.6 -6 4
Displacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation countingDisplacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation counting
ChEMBL 325 3 2 8 1.8 Nc1ccc(Cn2nnc3c(-c4ccco4)nc(N)nc32)c(F)c1 10.1021/jm800961g
CHEMBL516800 189863 None 0 Human Binding pKi = 7.6 7.6 -6 4
Displacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation countingDisplacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation counting
ChEMBL 325 3 2 8 1.8 Nc1ccc(Cn2nnc3c(-c4ccco4)nc(N)nc32)c(F)c1 10.1021/jm800961g
156011786 177329 None 0 Human Binding pKi = 7.6 7.6 - 1
Displacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting methodDisplacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting method
ChEMBL 324 3 1 7 2.9 CCOC(=O)C1=C(C)Nc2nc3ccccc3n2C1c1cnoc1 10.1021/acs.jmedchem.0c00564
CHEMBL4637204 177329 None 0 Human Binding pKi = 7.6 7.6 - 1
Displacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting methodDisplacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting method
ChEMBL 324 3 1 7 2.9 CCOC(=O)C1=C(C)Nc2nc3ccccc3n2C1c1cnoc1 10.1021/acs.jmedchem.0c00564
2874872 49674 None 14 Human Binding pKi = 7.6 7.6 - 1
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 minsDisplacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 mins
ChEMBL 266 3 2 4 1.9 CCOC(=O)C1=C(C)NC(=O)NC1c1ccsc1 10.1021/acs.jmedchem.5b01586
CHEMBL1566489 49674 None 14 Human Binding pKi = 7.6 7.6 - 1
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 minsDisplacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 mins
ChEMBL 266 3 2 4 1.9 CCOC(=O)C1=C(C)NC(=O)NC1c1ccsc1 10.1021/acs.jmedchem.5b01586
2874872 49674 None 14 Human Binding pKi = 7.6 7.6 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes after 30 minsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes after 30 mins
ChEMBL 266 3 2 4 1.9 CCOC(=O)C1=C(C)NC(=O)NC1c1ccsc1 10.1021/acs.jmedchem.7b00138
CHEMBL1566489 49674 None 14 Human Binding pKi = 7.6 7.6 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes after 30 minsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes after 30 mins
ChEMBL 266 3 2 4 1.9 CCOC(=O)C1=C(C)NC(=O)NC1c1ccsc1 10.1021/acs.jmedchem.7b00138
2874872 49674 None 14 Human Binding pKi = 7.6 7.6 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 266 3 2 4 1.9 CCOC(=O)C1=C(C)NC(=O)NC1c1ccsc1 10.1021/acs.jmedchem.0c01431
CHEMBL1566489 49674 None 14 Human Binding pKi = 7.6 7.6 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 266 3 2 4 1.9 CCOC(=O)C1=C(C)NC(=O)NC1c1ccsc1 10.1021/acs.jmedchem.0c01431
2874872 49674 None 14 Human Binding pKi = 7.6 7.6 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by Scatchard plot analysisDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by Scatchard plot analysis
ChEMBL 266 3 2 4 1.9 CCOC(=O)C1=C(C)NC(=O)NC1c1ccsc1 10.1021/ml400185v
CHEMBL1566489 49674 None 14 Human Binding pKi = 7.6 7.6 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by Scatchard plot analysisDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by Scatchard plot analysis
ChEMBL 266 3 2 4 1.9 CCOC(=O)C1=C(C)NC(=O)NC1c1ccsc1 10.1021/ml400185v
2874872 49674 None 14 Human Binding pKi = 7.6 7.6 - 1
Displacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assayDisplacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assay
ChEMBL 266 3 2 4 1.9 CCOC(=O)C1=C(C)NC(=O)NC1c1ccsc1 10.1021/acs.jmedchem.9b01340
CHEMBL1566489 49674 None 14 Human Binding pKi = 7.6 7.6 - 1
Displacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assayDisplacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assay
ChEMBL 266 3 2 4 1.9 CCOC(=O)C1=C(C)NC(=O)NC1c1ccsc1 10.1021/acs.jmedchem.9b01340
168287172 191650 None 0 Human Binding pKi = 7.6 7.6 - 1
Displacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cell membrane and measured after 0.5 hrs by radioligand displacement assayDisplacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cell membrane and measured after 0.5 hrs by radioligand displacement assay
ChEMBL 369 6 1 7 3.1 CCCn1c(=O)c2[nH]c(-c3ccc(N=C=S)cc3)nc2n(CCC)c1=O 10.1039/d2md00132b
CHEMBL5196082 191650 None 0 Human Binding pKi = 7.6 7.6 - 1
Displacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cell membrane and measured after 0.5 hrs by radioligand displacement assayDisplacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cell membrane and measured after 0.5 hrs by radioligand displacement assay
ChEMBL 369 6 1 7 3.1 CCCn1c(=O)c2[nH]c(-c3ccc(N=C=S)cc3)nc2n(CCC)c1=O 10.1039/d2md00132b
22282339 83104 None 3 Human Binding pKi = 6.6 6.6 -331 15
Displacement of [3H] DPCPX from human adenosine A2B receptor expressed in HEK293 cells incubated for 60 mins by radioligand binding assayDisplacement of [3H] DPCPX from human adenosine A2B receptor expressed in HEK293 cells incubated for 60 mins by radioligand binding assay
ChEMBL 386 4 1 5 5.1 Cc1cc(C)cc(-c2nc(NC(=O)c3cccnc3)sc2-c2ccncc2)c1 10.1021/acsmedchemlett.1c00685
CHEMBL2181976 83104 None 3 Human Binding pKi = 6.6 6.6 -331 15
Displacement of [3H] DPCPX from human adenosine A2B receptor expressed in HEK293 cells incubated for 60 mins by radioligand binding assayDisplacement of [3H] DPCPX from human adenosine A2B receptor expressed in HEK293 cells incubated for 60 mins by radioligand binding assay
ChEMBL 386 4 1 5 5.1 Cc1cc(C)cc(-c2nc(NC(=O)c3cccnc3)sc2-c2ccncc2)c1 10.1021/acsmedchemlett.1c00685
CHEMBL5084951 83104 None 3 Human Binding pKi = 6.6 6.6 -331 15
Displacement of [3H] DPCPX from human adenosine A2B receptor expressed in HEK293 cells incubated for 60 mins by radioligand binding assayDisplacement of [3H] DPCPX from human adenosine A2B receptor expressed in HEK293 cells incubated for 60 mins by radioligand binding assay
ChEMBL 386 4 1 5 5.1 Cc1cc(C)cc(-c2nc(NC(=O)c3cccnc3)sc2-c2ccncc2)c1 10.1021/acsmedchemlett.1c00685
145960933 161562 None 0 Human Binding pKi = 6.6 6.6 -2 3
Displacement of [3H]DPCPX from human A2B receptor expressed in cell membranes after 30 mins by beta-scintillation counting methodDisplacement of [3H]DPCPX from human A2B receptor expressed in cell membranes after 30 mins by beta-scintillation counting method
ChEMBL 271 2 2 2 3.5 O=C(Nc1nc2cccc(Cl)c2[nH]1)c1ccccc1 10.1021/acs.jmedchem.8b00204
CHEMBL4128848 161562 None 0 Human Binding pKi = 6.6 6.6 -2 3
Displacement of [3H]DPCPX from human A2B receptor expressed in cell membranes after 30 mins by beta-scintillation counting methodDisplacement of [3H]DPCPX from human A2B receptor expressed in cell membranes after 30 mins by beta-scintillation counting method
ChEMBL 271 2 2 2 3.5 O=C(Nc1nc2cccc(Cl)c2[nH]1)c1ccccc1 10.1021/acs.jmedchem.8b00204
11493754 168761 None 0 Human Binding pKi = 5.6 5.6 1 2
Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cellsDisplacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells
ChEMBL 336 3 1 7 0.9 Cn1c(=O)c2nc(-c3cnn(Cc4ccccc4)c3)[nH]c2n(C)c1=O 10.1021/jm051268+
CHEMBL437301 168761 None 0 Human Binding pKi = 5.6 5.6 1 2
Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cellsDisplacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells
ChEMBL 336 3 1 7 0.9 Cn1c(=O)c2nc(-c3cnn(Cc4ccccc4)c3)[nH]c2n(C)c1=O 10.1021/jm051268+
2519 779 None 86 Mouse Binding pKi = 4.6 4.6 -1 12
Displacement of [3H]PSB-603 from recombinant mouse adenosine A2B receptor expressed in CHO cell membranes after 75 mins by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant mouse adenosine A2B receptor expressed in CHO cell membranes after 75 mins by liquid scintillation counting method
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1021/acs.jmedchem.7b01627
2519.0 779 None 86 Mouse Binding pKi = 4.6 4.6 -1 12
Displacement of [3H]PSB-603 from recombinant mouse adenosine A2B receptor expressed in CHO cell membranes after 75 mins by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant mouse adenosine A2B receptor expressed in CHO cell membranes after 75 mins by liquid scintillation counting method
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1021/acs.jmedchem.7b01627
407 779 None 86 Mouse Binding pKi = 4.6 4.6 -1 12
Displacement of [3H]PSB-603 from recombinant mouse adenosine A2B receptor expressed in CHO cell membranes after 75 mins by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant mouse adenosine A2B receptor expressed in CHO cell membranes after 75 mins by liquid scintillation counting method
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1021/acs.jmedchem.7b01627
463 779 None 86 Mouse Binding pKi = 4.6 4.6 -1 12
Displacement of [3H]PSB-603 from recombinant mouse adenosine A2B receptor expressed in CHO cell membranes after 75 mins by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant mouse adenosine A2B receptor expressed in CHO cell membranes after 75 mins by liquid scintillation counting method
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1021/acs.jmedchem.7b01627
CHEMBL113 779 None 86 Mouse Binding pKi = 4.6 4.6 -1 12
Displacement of [3H]PSB-603 from recombinant mouse adenosine A2B receptor expressed in CHO cell membranes after 75 mins by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant mouse adenosine A2B receptor expressed in CHO cell membranes after 75 mins by liquid scintillation counting method
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1021/acs.jmedchem.7b01627
DB00201 779 None 86 Mouse Binding pKi = 4.6 4.6 -1 12
Displacement of [3H]PSB-603 from recombinant mouse adenosine A2B receptor expressed in CHO cell membranes after 75 mins by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant mouse adenosine A2B receptor expressed in CHO cell membranes after 75 mins by liquid scintillation counting method
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1021/acs.jmedchem.7b01627
44459944 94845 None 6 Human Binding pKi = 4.6 4.6 1 3
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 266 3 0 8 -1.0 CC(=O)OCCn1cnc2c1c(=O)n(C)c(=O)n2C 10.1021/jm0104318
CHEMBL25373 94845 None 6 Human Binding pKi = 4.6 4.6 1 3
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 266 3 0 8 -1.0 CC(=O)OCCn1cnc2c1c(=O)n(C)c(=O)n2C 10.1021/jm0104318
11822168 203656 None 0 Human Binding pKi = 5.6 5.6 3 4
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 284 4 1 5 1.1 Cn1c(=O)n(CCCc2ccccc2)c(=O)c2[nH]cnc21 10.1021/jm0104318
CHEMBL67313 203656 None 0 Human Binding pKi = 5.6 5.6 3 4
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 284 4 1 5 1.1 Cn1c(=O)n(CCCc2ccccc2)c(=O)c2[nH]cnc21 10.1021/jm0104318
11702501 71500 None 0 Human Binding pKi = 5.6 5.6 -501 3
Binding affinity towards human Adenosine A2b receptor expressed in HEK293 cells using 5 nM [3H]DPCPXBinding affinity towards human Adenosine A2b receptor expressed in HEK293 cells using 5 nM [3H]DPCPX
ChEMBL 320 4 1 8 1.3 Cn1c(-n2nccn2)nc2c(N)nc(CCc3ccccc3)nc21 10.1021/jm058018d
CHEMBL196259 71500 None 0 Human Binding pKi = 5.6 5.6 -501 3
Binding affinity towards human Adenosine A2b receptor expressed in HEK293 cells using 5 nM [3H]DPCPXBinding affinity towards human Adenosine A2b receptor expressed in HEK293 cells using 5 nM [3H]DPCPX
ChEMBL 320 4 1 8 1.3 Cn1c(-n2nccn2)nc2c(N)nc(CCc3ccccc3)nc21 10.1021/jm058018d
155556575 174500 None 0 Human Binding pKi = 6.6 6.6 - 1
Displacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assayDisplacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assay
ChEMBL 318 3 2 4 2.4 CC1=C(C(=O)OC(C)C(F)(F)F)C(c2ccoc2)NC(=O)N1 10.1021/acs.jmedchem.9b01340
CHEMBL4554893 174500 None 0 Human Binding pKi = 6.6 6.6 - 1
Displacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assayDisplacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assay
ChEMBL 318 3 2 4 2.4 CC1=C(C(=O)OC(C)C(F)(F)F)C(c2ccoc2)NC(=O)N1 10.1021/acs.jmedchem.9b01340
135443302 116409 None 0 Human Binding pKi = 6.6 6.6 -1 2
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 331 5 2 8 0.7 CCCn1c(=O)c2nc(-c3cc(N)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
CHEMBL33602 116409 None 0 Human Binding pKi = 6.6 6.6 -1 2
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 331 5 2 8 0.7 CCCn1c(=O)c2nc(-c3cc(N)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
11826577 57296 None 0 Human Binding pKi = 6.6 6.6 -7 4
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 178-310Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 178-310
ChEMBL 456 4 2 8 4.4 CCn1cc2c(nc(NC(=O)Nc3ccc(C(F)(F)F)cc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm0109614
CHEMBL165044 57296 None 0 Human Binding pKi = 6.6 6.6 -7 4
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 178-310Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 178-310
ChEMBL 456 4 2 8 4.4 CCn1cc2c(nc(NC(=O)Nc3ccc(C(F)(F)F)cc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm0109614
99619 203471 None 23 Human Binding pKi = 4.6 4.6 - 1
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 223 2 1 7 -1.6 Cn1c(=O)c2c(ncn2CCN)n(C)c1=O 10.1021/jm0104318
CHEMBL66011 203471 None 23 Human Binding pKi = 4.6 4.6 - 1
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 223 2 1 7 -1.6 Cn1c(=O)c2c(ncn2CCN)n(C)c1=O 10.1021/jm0104318
22375 203620 None 30 Human Binding pKi = 4.6 4.6 - 1
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 238 2 1 7 -1.5 Cn1cnc2c1c(=O)n(CC(=O)O)c(=O)n2C 10.1021/jm0104318
CHEMBL67109 203620 None 30 Human Binding pKi = 4.6 4.6 - 1
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 238 2 1 7 -1.5 Cn1cnc2c1c(=O)n(CC(=O)O)c(=O)n2C 10.1021/jm0104318
3286 3209 None 31 Human Binding pKi = 6.6 6.6 4 9
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 350 4 3 6 0.7 CCCn1c(=O)[nH]c2c(c1=O)nc([nH]2)c1ccc(cc1)S(=O)(=O)O 10.1021/jm900413e
5311479 3209 None 31 Human Binding pKi = 6.6 6.6 4 9
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 350 4 3 6 0.7 CCCn1c(=O)[nH]c2c(c1=O)nc([nH]2)c1ccc(cc1)S(=O)(=O)O 10.1021/jm900413e
CHEMBL8565 3209 None 31 Human Binding pKi = 6.6 6.6 4 9
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 350 4 3 6 0.7 CCCn1c(=O)[nH]c2c(c1=O)nc([nH]2)c1ccc(cc1)S(=O)(=O)O 10.1021/jm900413e
155550704 174306 None 0 Human Binding pKi = 6.6 6.6 - 1
Displacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assayDisplacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assay
ChEMBL 318 3 2 4 2.4 CC(C)OC(=O)C1=C(C(F)(F)F)NC(=O)NC1c1ccco1 10.1021/acs.jmedchem.9b01340
CHEMBL4550201 174306 None 0 Human Binding pKi = 6.6 6.6 - 1
Displacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assayDisplacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assay
ChEMBL 318 3 2 4 2.4 CC(C)OC(=O)C1=C(C(F)(F)F)NC(=O)NC1c1ccco1 10.1021/acs.jmedchem.9b01340
44410556 140549 None 0 Human Binding pKi = 4.6 4.6 -10715 4
Displacement of [125I]ABOPX from human adenosine A2B receptor in HEK cellsDisplacement of [125I]ABOPX from human adenosine A2B receptor in HEK cells
ChEMBL 404 5 5 10 -1.3 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC)nc(C#C[C@H](C)O)nc32)[C@H](O)[C@@H]1O 10.1016/j.bmcl.2006.01.110
CHEMBL381108 140549 None 0 Human Binding pKi = 4.6 4.6 -10715 4
Displacement of [125I]ABOPX from human adenosine A2B receptor in HEK cellsDisplacement of [125I]ABOPX from human adenosine A2B receptor in HEK cells
ChEMBL 404 5 5 10 -1.3 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC)nc(C#C[C@H](C)O)nc32)[C@H](O)[C@@H]1O 10.1016/j.bmcl.2006.01.110
44452493 96473 None 0 Human Binding pKi = 5.6 5.6 -17 3
Displacement of [3]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 307 4 0 6 3.4 CCN(CC)c1nc2ccccc2n2nc(-c3ccco3)nc12 10.1016/j.bmc.2007.10.103
CHEMBL262353 96473 None 0 Human Binding pKi = 5.6 5.6 -17 3
Displacement of [3]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 307 4 0 6 3.4 CCN(CC)c1nc2ccccc2n2nc(-c3ccco3)nc12 10.1016/j.bmc.2007.10.103
135416058 491 None 0 Human Binding pKi = 7.6 7.6 - 1
Binding affinity of compound for displacement of [3H]DPCPX binding in HEK293 membranes expressing human A2B adenosine receptorsBinding affinity of compound for displacement of [3H]DPCPX binding in HEK293 membranes expressing human A2B adenosine receptors
ChEMBL 530 8 1 11 -0.5 C=CCn1c2=N/C(=c\3/cc([nH]n3C)OCC(=O)N3CCN(CC3)c3ccccc3)/N=c2c(=O)n(c1=O)CC=C 10.1021/jm0309654
442 491 None 0 Human Binding pKi = 7.6 7.6 - 1
Binding affinity of compound for displacement of [3H]DPCPX binding in HEK293 membranes expressing human A2B adenosine receptorsBinding affinity of compound for displacement of [3H]DPCPX binding in HEK293 membranes expressing human A2B adenosine receptors
ChEMBL 530 8 1 11 -0.5 C=CCn1c2=N/C(=c\3/cc([nH]n3C)OCC(=O)N3CCN(CC3)c3ccccc3)/N=c2c(=O)n(c1=O)CC=C 10.1021/jm0309654
CHEMBL2113342 491 None 0 Human Binding pKi = 7.6 7.6 - 1
Binding affinity of compound for displacement of [3H]DPCPX binding in HEK293 membranes expressing human A2B adenosine receptorsBinding affinity of compound for displacement of [3H]DPCPX binding in HEK293 membranes expressing human A2B adenosine receptors
ChEMBL 530 8 1 11 -0.5 C=CCn1c2=N/C(=c\3/cc([nH]n3C)OCC(=O)N3CCN(CC3)c3ccccc3)/N=c2c(=O)n(c1=O)CC=C 10.1021/jm0309654
135416058 491 None 0 Human Binding pKi = 7.6 7.6 - 1
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 530 8 1 11 -0.5 C=CCn1c2=N/C(=c\3/cc([nH]n3C)OCC(=O)N3CCN(CC3)c3ccccc3)/N=c2c(=O)n(c1=O)CC=C 10.1021/jm0309654
442 491 None 0 Human Binding pKi = 7.6 7.6 - 1
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 530 8 1 11 -0.5 C=CCn1c2=N/C(=c\3/cc([nH]n3C)OCC(=O)N3CCN(CC3)c3ccccc3)/N=c2c(=O)n(c1=O)CC=C 10.1021/jm0309654
CHEMBL2113342 491 None 0 Human Binding pKi = 7.6 7.6 - 1
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 530 8 1 11 -0.5 C=CCn1c2=N/C(=c\3/cc([nH]n3C)OCC(=O)N3CCN(CC3)c3ccccc3)/N=c2c(=O)n(c1=O)CC=C 10.1021/jm0309654
16071896 58025 None 44 Human Binding pKi = 7.6 7.6 - 1
Binding affinity to human adenosine A2B receptor at 10 uMBinding affinity to human adenosine A2B receptor at 10 uM
ChEMBL 335 4 1 5 3.1 O=C(Nc1cnc(-c2ccncc2F)c(-c2cccnc2)n1)C1CC1 10.1021/jm201292w
CHEMBL1672627 58025 None 44 Human Binding pKi = 7.6 7.6 - 1
Binding affinity to human adenosine A2B receptor at 10 uMBinding affinity to human adenosine A2B receptor at 10 uM
ChEMBL 335 4 1 5 3.1 O=C(Nc1cnc(-c2ccncc2F)c(-c2cccnc2)n1)C1CC1 10.1021/jm201292w
10874051 84250 None 0 Human Binding pKi = 7.6 7.6 -7 4
Displacement of [3H]- DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]- DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 450 5 2 10 3.6 COc1ccc(NC(=O)Nc2nc3nn(C)c(SC)c3c3nc(-c4ccco4)nn23)cc1 10.1021/jm021023m
CHEMBL22113 84250 None 0 Human Binding pKi = 7.6 7.6 -7 4
Displacement of [3H]- DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]- DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 450 5 2 10 3.6 COc1ccc(NC(=O)Nc2nc3nn(C)c(SC)c3c3nc(-c4ccco4)nn23)cc1 10.1021/jm021023m
66894080 158130 None 0 Human Binding pKi = 7.6 7.6 - 1
Displacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting methodDisplacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting method
ChEMBL 479 7 1 8 2.4 CCCn1c(=O)c2[nH]c(-c3cnn(CC4CC(=O)N(c5cccc(F)c5)C4)c3)nc2n(CC)c1=O 10.1016/j.ejmech.2016.11.007
CHEMBL4087056 158130 None 0 Human Binding pKi = 7.6 7.6 - 1
Displacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting methodDisplacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting method
ChEMBL 479 7 1 8 2.4 CCCn1c(=O)c2[nH]c(-c3cnn(CC4CC(=O)N(c5cccc(F)c5)C4)c3)nc2n(CC)c1=O 10.1016/j.ejmech.2016.11.007
21958761 169419 None 0 Human Binding pKi = 7.6 7.6 66 2
Displacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranesDisplacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranes
ChEMBL 382 5 2 6 2.1 CC(C)Cn1c(=O)[nH]c2nc(-c3cnn(Cc4cccc(F)c4)c3)[nH]c2c1=O 10.1016/j.bmcl.2008.01.008
CHEMBL442434 169419 None 0 Human Binding pKi = 7.6 7.6 66 2
Displacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranesDisplacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranes
ChEMBL 382 5 2 6 2.1 CC(C)Cn1c(=O)[nH]c2nc(-c3cnn(Cc4cccc(F)c4)c3)[nH]c2c1=O 10.1016/j.bmcl.2008.01.008
11659696 85256 None 0 Human Binding pKi = 7.6 7.6 - 1
Displacement of [3H]DPCPX from human A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human A2B receptor expressed in HEK293 cells
ChEMBL 317 4 1 8 2.7 c1coc(-c2nc(Nc3cncnc3)ncc2-c2ccncn2)c1 10.1021/jm061333v
CHEMBL225972 85256 None 0 Human Binding pKi = 7.6 7.6 - 1
Displacement of [3H]DPCPX from human A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human A2B receptor expressed in HEK293 cells
ChEMBL 317 4 1 8 2.7 c1coc(-c2nc(Nc3cncnc3)ncc2-c2ccncn2)c1 10.1021/jm061333v
16071896 58025 None 44 Human Binding pKi = 7.6 7.6 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 335 4 1 5 3.1 O=C(Nc1cnc(-c2ccncc2F)c(-c2cccnc2)n1)C1CC1 10.1021/ml100249e
CHEMBL1672627 58025 None 44 Human Binding pKi = 7.6 7.6 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 335 4 1 5 3.1 O=C(Nc1cnc(-c2ccncc2F)c(-c2cccnc2)n1)C1CC1 10.1021/ml100249e
44588474 175341 None 0 Human Binding pKi = 7.6 7.6 6 2
Displacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cells
ChEMBL 357 6 2 6 2.7 CCCn1c(=O)c2[nH]c(-c3ccc(OC)cc3)c(O)c2n(CCC)c1=O 10.1016/j.bmc.2008.09.067
CHEMBL457418 175341 None 0 Human Binding pKi = 7.6 7.6 6 2
Displacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cells
ChEMBL 357 6 2 6 2.7 CCCn1c(=O)c2[nH]c(-c3ccc(OC)cc3)c(O)c2n(CCC)c1=O 10.1016/j.bmc.2008.09.067
44574254 173244 None 0 Human Binding pKi = 7.6 7.6 1 2
Displacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells by beta scintillation counterDisplacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells by beta scintillation counter
ChEMBL 563 8 1 7 5.1 CCCn1c(=O)c2[nH]c(-c3ccc(COC(=O)N4CCN(c5cccc(Cl)c5)CC4)cc3)cc2n(CCC)c1=O 10.1016/j.bmc.2009.03.062
CHEMBL452454 173244 None 0 Human Binding pKi = 7.6 7.6 1 2
Displacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells by beta scintillation counterDisplacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells by beta scintillation counter
ChEMBL 563 8 1 7 5.1 CCCn1c(=O)c2[nH]c(-c3ccc(COC(=O)N4CCN(c5cccc(Cl)c5)CC4)cc3)cc2n(CCC)c1=O 10.1016/j.bmc.2009.03.062
22266732 159348 None 0 Human Binding pKi = 7.6 7.6 - 1
Displacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 514 7 1 10 3.3 CCCn1c(=O)c2[nH]c(-c3cnn(Cc4noc(-c5ccc(C(F)(F)F)cc5)n4)c3)nc2n(CC)c1=O 10.1021/jm7014815
CHEMBL410021 159348 None 0 Human Binding pKi = 7.6 7.6 - 1
Displacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 514 7 1 10 3.3 CCCn1c(=O)c2[nH]c(-c3cnn(Cc4noc(-c5ccc(C(F)(F)F)cc5)n4)c3)nc2n(CC)c1=O 10.1021/jm7014815
21874697 178588 None 0 Human Binding pKi = 7.6 7.6 -12 4
Displacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation countingDisplacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation counting
ChEMBL 328 3 1 7 2.4 Nc1nc(-c2ccco2)c2nnn(Cc3c(F)cccc3F)c2n1 10.1021/jm800961g
CHEMBL467246 178588 None 0 Human Binding pKi = 7.6 7.6 -12 4
Displacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation countingDisplacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation counting
ChEMBL 328 3 1 7 2.4 Nc1nc(-c2ccco2)c2nnn(Cc3c(F)cccc3F)c2n1 10.1021/jm800961g
10404217 120099 None 0 Human Binding pKi = 7.6 7.6 19 5
Inhibition of [3H]ZM-241385 binding to human adenosine A2B receptorInhibition of [3H]ZM-241385 binding to human adenosine A2B receptor
ChEMBL 328 5 3 5 1.6 CCCCn1c(=O)[nH]c2[nH]c(-c3ccc(C(=O)O)cc3)nc2c1=O 10.1021/jm011049y
CHEMBL35094 120099 None 0 Human Binding pKi = 7.6 7.6 19 5
Inhibition of [3H]ZM-241385 binding to human adenosine A2B receptorInhibition of [3H]ZM-241385 binding to human adenosine A2B receptor
ChEMBL 328 5 3 5 1.6 CCCCn1c(=O)[nH]c2[nH]c(-c3ccc(C(=O)O)cc3)nc2c1=O 10.1021/jm011049y
16071896 58025 None 44 Human Binding pKi = 7.6 7.6 - 1
Inhibition of human A2B adenosine receptorInhibition of human A2B adenosine receptor
ChEMBL 335 4 1 5 3.1 O=C(Nc1cnc(-c2ccncc2F)c(-c2cccnc2)n1)C1CC1 10.1016/j.ejmech.2018.11.045
CHEMBL1672627 58025 None 44 Human Binding pKi = 7.6 7.6 - 1
Inhibition of human A2B adenosine receptorInhibition of human A2B adenosine receptor
ChEMBL 335 4 1 5 3.1 O=C(Nc1cnc(-c2ccncc2F)c(-c2cccnc2)n1)C1CC1 10.1016/j.ejmech.2018.11.045
137634776 155975 None 0 Human Binding pKi = 7.6 7.6 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes after 30 minsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes after 30 mins
ChEMBL 288 3 2 5 1.6 CC1=C(C(=O)OC(C)C)C(c2ccco2)N/C(=N/C#N)N1 10.1021/acs.jmedchem.7b00138
CHEMBL4061502 155975 None 0 Human Binding pKi = 7.6 7.6 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes after 30 minsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes after 30 mins
ChEMBL 288 3 2 5 1.6 CC1=C(C(=O)OC(C)C)C(c2ccco2)N/C(=N/C#N)N1 10.1021/acs.jmedchem.7b00138
145975418 163852 None 0 Human Binding pKi = 7.6 7.6 7 4
Displacement of [3H]PSB-603 from recombinant human adenosine A2B receptor expressed in CHO cell membranes after 75 mins by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human adenosine A2B receptor expressed in CHO cell membranes after 75 mins by liquid scintillation counting method
ChEMBL 645 11 3 7 4.7 CCCn1c(=O)[nH]c2nc(-c3ccc(OCC(=O)NCCCCC4=C5C(C)=CC(C)=[N+]5[B-](F)(F)n5c(C)cc(C)c54)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.7b01627
CHEMBL4206556 163852 None 0 Human Binding pKi = 7.6 7.6 7 4
Displacement of [3H]PSB-603 from recombinant human adenosine A2B receptor expressed in CHO cell membranes after 75 mins by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human adenosine A2B receptor expressed in CHO cell membranes after 75 mins by liquid scintillation counting method
ChEMBL 645 11 3 7 4.7 CCCn1c(=O)[nH]c2nc(-c3ccc(OCC(=O)NCCCCC4=C5C(C)=CC(C)=[N+]5[B-](F)(F)n5c(C)cc(C)c54)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.7b01627
11548714 73333 None 0 Human Binding pKi = 7.6 7.6 5 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 572 9 2 6 5.4 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(Br)cc4)cc3)c(Cl)c2n(CCC)c1=O 10.1021/jm0506221
CHEMBL201321 73333 None 0 Human Binding pKi = 7.6 7.6 5 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 572 9 2 6 5.4 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(Br)cc4)cc3)c(Cl)c2n(CCC)c1=O 10.1021/jm0506221
11628044 74695 None 0 Human Binding pKi = 7.6 7.6 1 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 538 9 2 6 4.8 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccccc4)cc3)c(Br)c2n(CCC)c1=O 10.1021/jm0506221
CHEMBL203030 74695 None 0 Human Binding pKi = 7.6 7.6 1 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 538 9 2 6 4.8 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccccc4)cc3)c(Br)c2n(CCC)c1=O 10.1021/jm0506221
44451199 156868 None 0 Human Binding pKi = 7.6 7.6 10 3
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 557 9 1 7 4.5 CCCn1c(=O)c2[nH]c(-c3ccc(OC(C)(C)C(=O)N4CCN(c5ccccc5)CC4)cc3)cc2n(CCC)c1=O 10.1016/j.bmc.2008.01.002
CHEMBL407179 156868 None 0 Human Binding pKi = 7.6 7.6 10 3
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 557 9 1 7 4.5 CCCn1c(=O)c2[nH]c(-c3ccc(OC(C)(C)C(=O)N4CCN(c5ccccc5)CC4)cc3)cc2n(CCC)c1=O 10.1016/j.bmc.2008.01.002
162668796 182725 None 0 Human Binding pKi = 6.6 6.6 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 262 4 2 3 2.5 CC1=C(C(=O)CC(C)C)C(c2ccco2)NC(=O)N1 10.1021/acs.jmedchem.0c01431
CHEMBL4789729 182725 None 0 Human Binding pKi = 6.6 6.6 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 262 4 2 3 2.5 CC1=C(C(=O)CC(C)C)C(c2ccco2)NC(=O)N1 10.1021/acs.jmedchem.0c01431
11597118 77092 None 0 Human Binding pKi = 6.6 6.6 - 1
Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cellsDisplacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells
ChEMBL 428 7 1 7 2.9 CCCn1c(=O)c2nc(-c3cnn(Cc4cccc(F)c4F)c3)[nH]c2n(CCC)c1=O 10.1021/jm051268+
CHEMBL207482 77092 None 0 Human Binding pKi = 6.6 6.6 - 1
Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cellsDisplacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells
ChEMBL 428 7 1 7 2.9 CCCn1c(=O)c2nc(-c3cnn(Cc4cccc(F)c4F)c3)[nH]c2n(CCC)c1=O 10.1021/jm051268+
44410585 77319 None 0 Human Binding pKi = 4.6 4.6 -9999 4
Displacement of [125I]ABOPX from human adenosine A2B receptor in HEK cellsDisplacement of [125I]ABOPX from human adenosine A2B receptor in HEK cells
ChEMBL 478 8 4 9 1.4 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC)nc(C#CCCCc4ccccc4)nc32)[C@H](O)[C@@H]1O 10.1016/j.bmcl.2006.01.110
CHEMBL208311 77319 None 0 Human Binding pKi = 4.6 4.6 -9999 4
Displacement of [125I]ABOPX from human adenosine A2B receptor in HEK cellsDisplacement of [125I]ABOPX from human adenosine A2B receptor in HEK cells
ChEMBL 478 8 4 9 1.4 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC)nc(C#CCCCc4ccccc4)nc32)[C@H](O)[C@@H]1O 10.1016/j.bmcl.2006.01.110
11761221 58157 None 0 Human Binding pKi = 6.6 6.6 -50 4
Displacement of [3H]-DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 206-282Displacement of [3H]-DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 206-282
ChEMBL 402 5 2 8 3.8 CCCn1cc2c(nc(NC(=O)Nc3ccccc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm0109614
CHEMBL168018 58157 None 0 Human Binding pKi = 6.6 6.6 -50 4
Displacement of [3H]-DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 206-282Displacement of [3H]-DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 206-282
ChEMBL 402 5 2 8 3.8 CCCn1cc2c(nc(NC(=O)Nc3ccccc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm0109614
18440425 198353 None 0 Human Binding pKi = 5.6 5.6 -15 3
Binding affinity to adenosine A2B receptor (unknown origin)Binding affinity to adenosine A2B receptor (unknown origin)
ChEMBL 282 5 2 6 2.1 CCn1cnc2c(N)nc(NCCc3ccccc3)nc21 10.1039/C5MD00034C
CHEMBL576447 198353 None 0 Human Binding pKi = 5.6 5.6 -15 3
Binding affinity to adenosine A2B receptor (unknown origin)Binding affinity to adenosine A2B receptor (unknown origin)
ChEMBL 282 5 2 6 2.1 CCn1cnc2c(N)nc(NCCc3ccccc3)nc21 10.1039/C5MD00034C
9953799 203374 None 2 Human Binding pKi = 6.6 6.6 -47 4
Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 188-320Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 188-320
ChEMBL 418 5 2 9 3.4 CCn1cc2c(nc(NC(=O)Nc3ccc(OC)cc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm001047y
CHEMBL65271 203374 None 2 Human Binding pKi = 6.6 6.6 -47 4
Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 188-320Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 188-320
ChEMBL 418 5 2 9 3.4 CCn1cc2c(nc(NC(=O)Nc3ccc(OC)cc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm001047y
9953799 203374 None 2 Human Binding pKi = 6.6 6.6 -47 4
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells
ChEMBL 418 5 2 9 3.4 CCn1cc2c(nc(NC(=O)Nc3ccc(OC)cc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm010818a
CHEMBL65271 203374 None 2 Human Binding pKi = 6.6 6.6 -47 4
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells
ChEMBL 418 5 2 9 3.4 CCn1cc2c(nc(NC(=O)Nc3ccc(OC)cc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm010818a
9953799 203374 None 2 Human Binding pKi = 6.6 6.6 -47 4
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 188-320Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 188-320
ChEMBL 418 5 2 9 3.4 CCn1cc2c(nc(NC(=O)Nc3ccc(OC)cc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm0109614
CHEMBL65271 203374 None 2 Human Binding pKi = 6.6 6.6 -47 4
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 188-320Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 188-320
ChEMBL 418 5 2 9 3.4 CCn1cc2c(nc(NC(=O)Nc3ccc(OC)cc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm0109614
11015003 57155 None 0 Human Binding pKi = 6.6 6.6 -9 4
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 211-287Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 211-287
ChEMBL 406 4 2 8 3.5 CCn1cc2c(nc(NC(=O)Nc3ccc(F)cc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm0109614
CHEMBL164685 57155 None 0 Human Binding pKi = 6.6 6.6 -9 4
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 211-287Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 211-287
ChEMBL 406 4 2 8 3.5 CCn1cc2c(nc(NC(=O)Nc3ccc(F)cc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm0109614
44520980 199813 None 0 Human Binding pKi = 5.6 5.6 -977 4
Displacement of radioligand from human adenosine A2B receptor expressed in cells by topcount microplate scintillation countingDisplacement of radioligand from human adenosine A2B receptor expressed in cells by topcount microplate scintillation counting
ChEMBL 311 4 2 6 1.9 Cc1ccc(-c2cc(C(=O)NCc3cccn3C)nc(N)n2)o1 10.1016/j.bmc.2009.07.078
CHEMBL594136 199813 None 0 Human Binding pKi = 5.6 5.6 -977 4
Displacement of radioligand from human adenosine A2B receptor expressed in cells by topcount microplate scintillation countingDisplacement of radioligand from human adenosine A2B receptor expressed in cells by topcount microplate scintillation counting
ChEMBL 311 4 2 6 1.9 Cc1ccc(-c2cc(C(=O)NCc3cccn3C)nc(N)n2)o1 10.1016/j.bmc.2009.07.078
44449532 96188 None 0 Human Binding pKi = 5.6 5.6 -870 4
Binding affinity at human adenosine A2B receptorBinding affinity at human adenosine A2B receptor
ChEMBL 318 3 1 7 2.8 OC[C@@H]1CCCN1c1nc(-c2nccs2)c2sccc2n1 10.1016/j.bmcl.2008.03.076
CHEMBL260718 96188 None 0 Human Binding pKi = 5.6 5.6 -870 4
Binding affinity at human adenosine A2B receptorBinding affinity at human adenosine A2B receptor
ChEMBL 318 3 1 7 2.8 OC[C@@H]1CCCN1c1nc(-c2nccs2)c2sccc2n1 10.1016/j.bmcl.2008.03.076
9880392 189209 None 0 Human Binding pKi = 6.6 6.6 -30 4
Displacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation countingDisplacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation counting
ChEMBL 326 3 1 7 2.7 Nc1nc(-c2cccs2)c2nnn(Cc3ccccc3F)c2n1 10.1021/jm800961g
CHEMBL511405 189209 None 0 Human Binding pKi = 6.6 6.6 -30 4
Displacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation countingDisplacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation counting
ChEMBL 326 3 1 7 2.7 Nc1nc(-c2cccs2)c2nnn(Cc3ccccc3F)c2n1 10.1021/jm800961g
44410597 139221 None 0 Human Binding pKi = 5.6 5.6 -3235 4
Displacement of [125I]ABOPX from human adenosine A2B receptor in HEK cellsDisplacement of [125I]ABOPX from human adenosine A2B receptor in HEK cells
ChEMBL 496 7 5 11 0.1 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC)nc(C#CC(O)c4ccc(OC)cc4)nc32)[C@H](O)[C@@H]1O 10.1016/j.bmcl.2006.01.110
CHEMBL378810 139221 None 0 Human Binding pKi = 5.6 5.6 -3235 4
Displacement of [125I]ABOPX from human adenosine A2B receptor in HEK cellsDisplacement of [125I]ABOPX from human adenosine A2B receptor in HEK cells
ChEMBL 496 7 5 11 0.1 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC)nc(C#CC(O)c4ccc(OC)cc4)nc32)[C@H](O)[C@@H]1O 10.1016/j.bmcl.2006.01.110
168278363 191165 None 0 Human Binding pKi = 5.6 5.6 -169 3
Displacement of [3H]DPCPX from human A2BAR incubated for 60 mins by scintillation counter analysisDisplacement of [3H]DPCPX from human A2BAR incubated for 60 mins by scintillation counter analysis
ChEMBL 451 11 3 10 2.9 Nc1nc(-c2ccco2)c2cnn(Cc3cccc(OCCCCCCC(=O)NO)n3)c2n1 10.1016/j.ejmech.2022.114326
CHEMBL5188801 191165 None 0 Human Binding pKi = 5.6 5.6 -169 3
Displacement of [3H]DPCPX from human A2BAR incubated for 60 mins by scintillation counter analysisDisplacement of [3H]DPCPX from human A2BAR incubated for 60 mins by scintillation counter analysis
ChEMBL 451 11 3 10 2.9 Nc1nc(-c2ccco2)c2cnn(Cc3cccc(OCCCCCCC(=O)NO)n3)c2n1 10.1016/j.ejmech.2022.114326
11027412 29629 None 0 Human Binding pKi = 7.6 7.6 1 4
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 493 9 1 9 4.4 O=C(COc1ccccc1)Nc1nc2nn(CCCc3ccccc3)cc2c2nc(-c3ccco3)nn12 10.1021/jm030852k
CHEMBL138593 29629 None 0 Human Binding pKi = 7.6 7.6 1 4
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 493 9 1 9 4.4 O=C(COc1ccccc1)Nc1nc2nn(CCCc3ccccc3)cc2c2nc(-c3ccco3)nn12 10.1021/jm030852k
10895565 168452 None 0 Human Binding pKi = 7.6 7.6 1 4
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 445 8 1 9 3.8 CC(C)CCn1cc2c(nc(NC(=O)COc3ccccc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm030852k
CHEMBL435022 168452 None 0 Human Binding pKi = 7.6 7.6 1 4
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 445 8 1 9 3.8 CC(C)CCn1cc2c(nc(NC(=O)COc3ccccc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm030852k
16070337 58019 None 0 Human Binding pKi = 7.6 7.6 12 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 317 4 1 5 2.9 O=C(Nc1cnc(-c2ccncc2)c(-c2cccnc2)n1)C1CC1 10.1021/ml100249e
CHEMBL1672621 58019 None 0 Human Binding pKi = 7.6 7.6 12 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 317 4 1 5 2.9 O=C(Nc1cnc(-c2ccncc2)c(-c2cccnc2)n1)C1CC1 10.1021/ml100249e
136042332 71159 None 0 Human Binding pKi = 7.6 7.6 177 2
Displacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation countingDisplacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation counting
ChEMBL 598 8 2 9 4.6 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5c(C(F)(F)F)cc(C(F)(F)F)cc5[nH]4)nn3C)nc2n(CCC)c1=O 10.1021/jm201292w
CHEMBL1955908 71159 None 0 Human Binding pKi = 7.6 7.6 177 2
Displacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation countingDisplacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation counting
ChEMBL 598 8 2 9 4.6 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5c(C(F)(F)F)cc(C(F)(F)F)cc5[nH]4)nn3C)nc2n(CCC)c1=O 10.1021/jm201292w
22266769 157504 None 0 Human Binding pKi = 7.6 7.6 87 4
Displacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 513 7 1 9 3.9 CCCn1c(=O)c2[nH]c(-c3cnn(Cc4cc(-c5ccc(C(F)(F)F)cc5)on4)c3)nc2n(CC)c1=O 10.1021/jm7014815
CHEMBL407969 157504 None 0 Human Binding pKi = 7.6 7.6 87 4
Displacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 513 7 1 9 3.9 CCCn1c(=O)c2[nH]c(-c3cnn(Cc4cc(-c5ccc(C(F)(F)F)cc5)on4)c3)nc2n(CC)c1=O 10.1021/jm7014815
11690983 72640 None 0 Human Binding pKi = 7.6 7.6 3 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 452 6 2 7 2.4 COc1cc(OCC(=O)Nc2ccc(F)cc2)ccc1-c1cc2c([nH]1)c(=O)n(C)c(=O)n2C 10.1021/jm0506221
CHEMBL199485 72640 None 0 Human Binding pKi = 7.6 7.6 3 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 452 6 2 7 2.4 COc1cc(OCC(=O)Nc2ccc(F)cc2)ccc1-c1cc2c([nH]1)c(=O)n(C)c(=O)n2C 10.1021/jm0506221
11699025 73654 None 0 Human Binding pKi = 7.6 7.6 -1 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 503 10 3 7 3.1 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(C(N)=O)cc4)cc3)cc2n(CCC)c1=O 10.1021/jm0506221
CHEMBL201791 73654 None 0 Human Binding pKi = 7.6 7.6 -1 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 503 10 3 7 3.1 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(C(N)=O)cc4)cc3)cc2n(CCC)c1=O 10.1021/jm0506221
44451019 95865 None 0 Human Binding pKi = 7.6 7.6 27 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 501 7 1 7 2.8 CCCn1c(=O)n(C)c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCN(c5ccccc5)CC4)cc3)cc21 10.1016/j.bmc.2008.01.002
CHEMBL259056 95865 None 0 Human Binding pKi = 7.6 7.6 27 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 501 7 1 7 2.8 CCCn1c(=O)n(C)c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCN(c5ccccc5)CC4)cc3)cc21 10.1016/j.bmc.2008.01.002
44451020 158845 None 0 Human Binding pKi = 7.6 7.6 26 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 501 7 1 7 2.9 CCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCN(c5ccccc5)CC4)cc3)cc2n(CC)c1=O 10.1016/j.bmc.2008.01.002
CHEMBL409481 158845 None 0 Human Binding pKi = 7.6 7.6 26 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 501 7 1 7 2.9 CCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCN(c5ccccc5)CC4)cc3)cc2n(CC)c1=O 10.1016/j.bmc.2008.01.002
11511897 66102 None 0 Human Binding pKi = 6.6 6.6 8 2
Binding affinity for adenosine A2b receptor by using as [3H]ZM-241385 (14 nM) radioligand in membranes from HEK-A2B cellsBinding affinity for adenosine A2b receptor by using as [3H]ZM-241385 (14 nM) radioligand in membranes from HEK-A2B cells
ChEMBL 516 10 1 10 4.0 CCCn1c(=O)c2nc(-c3ccc(OCc4noc(-c5ccc(OC)cc5)n4)cc3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2004.11.044
CHEMBL183915 66102 None 0 Human Binding pKi = 6.6 6.6 8 2
Binding affinity for adenosine A2b receptor by using as [3H]ZM-241385 (14 nM) radioligand in membranes from HEK-A2B cellsBinding affinity for adenosine A2b receptor by using as [3H]ZM-241385 (14 nM) radioligand in membranes from HEK-A2B cells
ChEMBL 516 10 1 10 4.0 CCCn1c(=O)c2nc(-c3ccc(OCc4noc(-c5ccc(OC)cc5)n4)cc3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2004.11.044
1330 163218 None 45 Human Binding pKi = 6.6 6.6 -1 6
Binding affinity for human adenosine A2B receptor using [3H]-PSB-298 in CHO cell membranesBinding affinity for human adenosine A2B receptor using [3H]-PSB-298 in CHO cell membranes
ChEMBL 392 6 2 7 1.6 CCCn1c(=O)c2nc(-c3ccc(S(=O)(=O)O)cc3)[nH]c2n(CCC)c1=O 10.1021/jm0310030
CHEMBL418333 163218 None 45 Human Binding pKi = 6.6 6.6 -1 6
Binding affinity for human adenosine A2B receptor using [3H]-PSB-298 in CHO cell membranesBinding affinity for human adenosine A2B receptor using [3H]-PSB-298 in CHO cell membranes
ChEMBL 392 6 2 7 1.6 CCCn1c(=O)c2nc(-c3ccc(S(=O)(=O)O)cc3)[nH]c2n(CCC)c1=O 10.1021/jm0310030
CHEMBL435575 163218 None 45 Human Binding pKi = 6.6 6.6 -1 6
Binding affinity for human adenosine A2B receptor using [3H]-PSB-298 in CHO cell membranesBinding affinity for human adenosine A2B receptor using [3H]-PSB-298 in CHO cell membranes
ChEMBL 392 6 2 7 1.6 CCCn1c(=O)c2nc(-c3ccc(S(=O)(=O)O)cc3)[nH]c2n(CCC)c1=O 10.1021/jm0310030
1330 163218 None 45 Human Binding pKi = 6.6 6.6 -1 6
Displacement of [125I]ABOPX from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [125I]ABOPX from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 392 6 2 7 1.6 CCCn1c(=O)c2nc(-c3ccc(S(=O)(=O)O)cc3)[nH]c2n(CCC)c1=O 10.1021/jm060277v
CHEMBL418333 163218 None 45 Human Binding pKi = 6.6 6.6 -1 6
Displacement of [125I]ABOPX from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [125I]ABOPX from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 392 6 2 7 1.6 CCCn1c(=O)c2nc(-c3ccc(S(=O)(=O)O)cc3)[nH]c2n(CCC)c1=O 10.1021/jm060277v
CHEMBL435575 163218 None 45 Human Binding pKi = 6.6 6.6 -1 6
Displacement of [125I]ABOPX from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [125I]ABOPX from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 392 6 2 7 1.6 CCCn1c(=O)c2nc(-c3ccc(S(=O)(=O)O)cc3)[nH]c2n(CCC)c1=O 10.1021/jm060277v
9887859 113512 None 0 Human Binding pKi = 6.6 6.6 -10000 6
Displacement of [3H]DPCPX from Human Adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from Human Adenosine A2B receptor expressed in HEK293 cells
ChEMBL 375 3 2 9 2.3 Cn1cc2c(nc(NC(=O)Nc3ccncc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm020974x
CHEMBL118923 113512 None 0 Human Binding pKi = 6.6 6.6 -10000 6
Displacement of [3H]DPCPX from Human Adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from Human Adenosine A2B receptor expressed in HEK293 cells
ChEMBL 375 3 2 9 2.3 Cn1cc2c(nc(NC(=O)Nc3ccncc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm020974x
CHEMBL332091 113512 None 0 Human Binding pKi = 6.6 6.6 -10000 6
Displacement of [3H]DPCPX from Human Adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from Human Adenosine A2B receptor expressed in HEK293 cells
ChEMBL 375 3 2 9 2.3 Cn1cc2c(nc(NC(=O)Nc3ccncc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm020974x
135874433 96091 None 0 Human Binding pKi = 6.6 6.6 - 1
Displacement of [3H]MRE2029F20 from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]MRE2029F20 from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 561 8 2 8 3.9 CCCn1c(=O)c2[nH]c(-c3nn(CC(=O)Nc4ccc(Cl)cc4)c(C)c3Br)nc2n(CCC)c1=O 10.1016/j.bmc.2007.11.058
CHEMBL260153 96091 None 0 Human Binding pKi = 6.6 6.6 - 1
Displacement of [3H]MRE2029F20 from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]MRE2029F20 from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 561 8 2 8 3.9 CCCn1c(=O)c2[nH]c(-c3nn(CC(=O)Nc4ccc(Cl)cc4)c(C)c3Br)nc2n(CCC)c1=O 10.1016/j.bmc.2007.11.058
11574428 138317 None 0 Human Binding pKi = 6.6 6.6 -2 3
Displacement of [3H]PSB298 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB298 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 379 5 3 8 -1.1 Cn1c(=O)c2nc(-c3ccc(S(=O)(=O)NCCO)cc3)[nH]c2n(C)c1=O 10.1021/jm060277v
CHEMBL377106 138317 None 0 Human Binding pKi = 6.6 6.6 -2 3
Displacement of [3H]PSB298 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB298 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 379 5 3 8 -1.1 Cn1c(=O)c2nc(-c3ccc(S(=O)(=O)NCCO)cc3)[nH]c2n(C)c1=O 10.1021/jm060277v
1330 163218 None 45 Human Binding pKi = 6.6 6.6 -1 6
Inhibition of [3H]ZM-241385 binding to human adenosine A2B receptorInhibition of [3H]ZM-241385 binding to human adenosine A2B receptor
ChEMBL 392 6 2 7 1.6 CCCn1c(=O)c2nc(-c3ccc(S(=O)(=O)O)cc3)[nH]c2n(CCC)c1=O 10.1021/jm011049y
CHEMBL418333 163218 None 45 Human Binding pKi = 6.6 6.6 -1 6
Inhibition of [3H]ZM-241385 binding to human adenosine A2B receptorInhibition of [3H]ZM-241385 binding to human adenosine A2B receptor
ChEMBL 392 6 2 7 1.6 CCCn1c(=O)c2nc(-c3ccc(S(=O)(=O)O)cc3)[nH]c2n(CCC)c1=O 10.1021/jm011049y
CHEMBL435575 163218 None 45 Human Binding pKi = 6.6 6.6 -1 6
Inhibition of [3H]ZM-241385 binding to human adenosine A2B receptorInhibition of [3H]ZM-241385 binding to human adenosine A2B receptor
ChEMBL 392 6 2 7 1.6 CCCn1c(=O)c2nc(-c3ccc(S(=O)(=O)O)cc3)[nH]c2n(CCC)c1=O 10.1021/jm011049y
11811544 57205 None 0 Human Binding pKi = 6.6 6.6 -10 4
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 213-296Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 213-296
ChEMBL 404 4 2 9 2.9 COc1cccc(NC(=O)Nc2nc3nn(C)cc3c3nc(-c4ccco4)nn23)c1 10.1021/jm0109614
CHEMBL164992 57205 None 0 Human Binding pKi = 6.6 6.6 -10 4
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 213-296Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 213-296
ChEMBL 404 4 2 9 2.9 COc1cccc(NC(=O)Nc2nc3nn(C)cc3c3nc(-c4ccco4)nn23)c1 10.1021/jm0109614
44452434 160639 None 0 Human Binding pKi = 6.6 6.6 -3 4
Displacement of [3]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 369 4 1 6 3.7 O=C(Cc1ccccc1)Nc1nc2ccccc2n2nc(-c3ccco3)nc12 10.1016/j.bmc.2007.10.103
CHEMBL411319 160639 None 0 Human Binding pKi = 6.6 6.6 -3 4
Displacement of [3]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 369 4 1 6 3.7 O=C(Cc1ccccc1)Nc1nc2ccccc2n2nc(-c3ccco3)nc12 10.1016/j.bmc.2007.10.103
44452455 160842 None 0 Human Binding pKi = 6.6 6.6 -2 4
Displacement of [3]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 293 2 1 6 2.5 CC(=O)Nc1nc2ccccc2n2nc(-c3ccco3)nc12 10.1016/j.bmc.2007.10.103
CHEMBL411482 160842 None 0 Human Binding pKi = 6.6 6.6 -2 4
Displacement of [3]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 293 2 1 6 2.5 CC(=O)Nc1nc2ccccc2n2nc(-c3ccco3)nc12 10.1016/j.bmc.2007.10.103
44452431 96611 None 0 Human Binding pKi = 5.6 5.6 -12 4
Displacement of [3]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 345 3 1 7 3.4 O=C(Nc1nc2ccccc2n2nc(-c3ccco3)nc12)c1ccco1 10.1016/j.bmc.2007.10.103
CHEMBL263370 96611 None 0 Human Binding pKi = 5.6 5.6 -12 4
Displacement of [3]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 345 3 1 7 3.4 O=C(Nc1nc2ccccc2n2nc(-c3ccco3)nc12)c1ccco1 10.1016/j.bmc.2007.10.103
24827998 138997 None 0 Human Binding pKi = 5.6 5.6 - 1
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 minsDisplacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 mins
ChEMBL 249 3 1 4 1.7 CCOC(=O)C1=C(C)NC(=O)CC1c1ccco1 10.1021/acs.jmedchem.5b01586
CHEMBL3785517 138997 None 0 Human Binding pKi = 5.6 5.6 - 1
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 minsDisplacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 mins
ChEMBL 249 3 1 4 1.7 CCOC(=O)C1=C(C)NC(=O)CC1c1ccco1 10.1021/acs.jmedchem.5b01586
9857698 176891 None 0 Human Binding pKi = 6.6 6.6 -85 4
Displacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation countingDisplacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation counting
ChEMBL 306 3 1 7 2.4 Cc1cccc(Cn2nnc3c(-c4ccco4)nc(N)nc32)c1 10.1021/jm800961g
CHEMBL461651 176891 None 0 Human Binding pKi = 6.6 6.6 -85 4
Displacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation countingDisplacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation counting
ChEMBL 306 3 1 7 2.4 Cc1cccc(Cn2nnc3c(-c4ccco4)nc(N)nc32)c1 10.1021/jm800961g
21958541 62996 None 0 Human Binding pKi = 6.6 6.6 19 3
Binding affinity for adenosine A2b receptor by using as [3H]ZM-241385 (14 nM) radioligand in membranes from HEK-A2B cellsBinding affinity for adenosine A2b receptor by using as [3H]ZM-241385 (14 nM) radioligand in membranes from HEK-A2B cells
ChEMBL 554 9 1 9 5.0 CCCn1c(=O)c2nc(-c3ccc(OCc4noc(-c5ccc(C(F)(F)F)cc5)n4)cc3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2004.11.044
CHEMBL178662 62996 None 0 Human Binding pKi = 6.6 6.6 19 3
Binding affinity for adenosine A2b receptor by using as [3H]ZM-241385 (14 nM) radioligand in membranes from HEK-A2B cellsBinding affinity for adenosine A2b receptor by using as [3H]ZM-241385 (14 nM) radioligand in membranes from HEK-A2B cells
ChEMBL 554 9 1 9 5.0 CCCn1c(=O)c2nc(-c3ccc(OCc4noc(-c5ccc(C(F)(F)F)cc5)n4)cc3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2004.11.044
176408 3557 None 84 Human Binding pKi = 6.6 6.6 -407 7
Displacement of [3H]DPCPX from human adenosine A2B receptor membrane (unknown origin) measured after 60 mins by scintillation counting analysisDisplacement of [3H]DPCPX from human adenosine A2B receptor membrane (unknown origin) measured after 60 mins by scintillation counting analysis
ChEMBL 345 4 1 8 2.6 Nc1nc2n(CCc3ccccc3)ncc2c2n1nc(n2)c1ccco1 10.1021/acs.jmedchem.1c01155
403 3557 None 84 Human Binding pKi = 6.6 6.6 -407 7
Displacement of [3H]DPCPX from human adenosine A2B receptor membrane (unknown origin) measured after 60 mins by scintillation counting analysisDisplacement of [3H]DPCPX from human adenosine A2B receptor membrane (unknown origin) measured after 60 mins by scintillation counting analysis
ChEMBL 345 4 1 8 2.6 Nc1nc2n(CCc3ccccc3)ncc2c2n1nc(n2)c1ccco1 10.1021/acs.jmedchem.1c01155
431 3557 None 84 Human Binding pKi = 6.6 6.6 -407 7
Displacement of [3H]DPCPX from human adenosine A2B receptor membrane (unknown origin) measured after 60 mins by scintillation counting analysisDisplacement of [3H]DPCPX from human adenosine A2B receptor membrane (unknown origin) measured after 60 mins by scintillation counting analysis
ChEMBL 345 4 1 8 2.6 Nc1nc2n(CCc3ccccc3)ncc2c2n1nc(n2)c1ccco1 10.1021/acs.jmedchem.1c01155
CHEMBL17127 3557 None 84 Human Binding pKi = 6.6 6.6 -407 7
Displacement of [3H]DPCPX from human adenosine A2B receptor membrane (unknown origin) measured after 60 mins by scintillation counting analysisDisplacement of [3H]DPCPX from human adenosine A2B receptor membrane (unknown origin) measured after 60 mins by scintillation counting analysis
ChEMBL 345 4 1 8 2.6 Nc1nc2n(CCc3ccccc3)ncc2c2n1nc(n2)c1ccco1 10.1021/acs.jmedchem.1c01155
372 58 None 103 Human Binding pKi = 4.6 4.6 -2630 9
Displacement of [125I]I-ABOPX from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [125I]I-ABOPX from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 301 2 4 9 -1.3 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2N 10.1021/jm900413e
8974 58 None 103 Human Binding pKi = 4.6 4.6 -2630 9
Displacement of [125I]I-ABOPX from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [125I]I-ABOPX from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 301 2 4 9 -1.3 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2N 10.1021/jm900413e
CHEMBL285819 58 None 103 Human Binding pKi = 4.6 4.6 -2630 9
Displacement of [125I]I-ABOPX from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [125I]I-ABOPX from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 301 2 4 9 -1.3 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2N 10.1021/jm900413e
72546539 103853 None 0 Human Binding pKi = 6.6 6.6 2 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by Scatchard plot analysisDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by Scatchard plot analysis
ChEMBL 278 5 2 4 2.3 CCCC1=C(C(=O)OCC)C(c2ccco2)NC(=O)N1 10.1021/ml400185v
CHEMBL3091711 103853 None 0 Human Binding pKi = 6.6 6.6 2 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by Scatchard plot analysisDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by Scatchard plot analysis
ChEMBL 278 5 2 4 2.3 CCCC1=C(C(=O)OCC)C(c2ccco2)NC(=O)N1 10.1021/ml400185v
9857266 176981 None 0 Human Binding pKi = 6.6 6.6 -21 4
Displacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation countingDisplacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation counting
ChEMBL 293 3 1 8 1.5 Nc1nc(-c2ccco2)c2nnn(Cc3ccccn3)c2n1 10.1021/jm800961g
CHEMBL462501 176981 None 0 Human Binding pKi = 6.6 6.6 -21 4
Displacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation countingDisplacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation counting
ChEMBL 293 3 1 8 1.5 Nc1nc(-c2ccco2)c2nnn(Cc3ccccn3)c2n1 10.1021/jm800961g
10155413 176889 None 0 Human Binding pKi = 6.6 6.6 -117 4
Displacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation countingDisplacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation counting
ChEMBL 360 3 1 7 3.1 Nc1nc(-c2ccco2)c2nnn(Cc3cccc(C(F)(F)F)c3)c2n1 10.1021/jm800961g
CHEMBL461649 176889 None 0 Human Binding pKi = 6.6 6.6 -117 4
Displacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation countingDisplacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation counting
ChEMBL 360 3 1 7 3.1 Nc1nc(-c2ccco2)c2nnn(Cc3cccc(C(F)(F)F)c3)c2n1 10.1021/jm800961g
10051061 161537 None 0 Human Binding pKi = 7.6 7.6 -10 3
Binding affinity for human adenosine A2B receptor using [3H]-PSB-298 in CHO cell membranesBinding affinity for human adenosine A2B receptor using [3H]-PSB-298 in CHO cell membranes
ChEMBL 485 8 2 9 2.6 CCCCn1c(=O)[nH]c2[nH]c(-c3ccc(S(=O)(=O)Oc4ccc([N+](=O)[O-])cc4)cc3)nc2c1=O 10.1021/jm0310030
CHEMBL412854 161537 None 0 Human Binding pKi = 7.6 7.6 -10 3
Binding affinity for human adenosine A2B receptor using [3H]-PSB-298 in CHO cell membranesBinding affinity for human adenosine A2B receptor using [3H]-PSB-298 in CHO cell membranes
ChEMBL 485 8 2 9 2.6 CCCCn1c(=O)[nH]c2[nH]c(-c3ccc(S(=O)(=O)Oc4ccc([N+](=O)[O-])cc4)cc3)nc2c1=O 10.1021/jm0310030
11071159 99509 None 0 Human Binding pKi = 7.6 7.6 12 2
Displacement of [3H]- DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]- DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 502 5 2 11 2.7 COc1ccc(NC(=O)Nc2nc3nn(C)c(N4CCN(C)CC4)c3c3nc(-c4ccco4)nn23)cc1 10.1021/jm021023m
CHEMBL283319 99509 None 0 Human Binding pKi = 7.6 7.6 12 2
Displacement of [3H]- DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]- DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 502 5 2 11 2.7 COc1ccc(NC(=O)Nc2nc3nn(C)c(N4CCN(C)CC4)c3c3nc(-c4ccco4)nn23)cc1 10.1021/jm021023m
53321372 58027 None 0 Human Binding pKi = 7.6 7.6 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 353 4 1 5 3.2 O=C(Nc1cnc(-c2c(F)cncc2F)c(-c2cccnc2)n1)C1CC1 10.1021/ml100249e
CHEMBL1672629 58027 None 0 Human Binding pKi = 7.6 7.6 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 353 4 1 5 3.2 O=C(Nc1cnc(-c2c(F)cncc2F)c(-c2cccnc2)n1)C1CC1 10.1021/ml100249e
21958512 166526 None 1 Human Binding pKi = 7.6 7.6 8 3
Displacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 396 6 1 7 2.3 CCCCn1c(=O)c2[nH]c(-c3cnn(Cc4cccc(F)c4)c3)nc2n(C)c1=O 10.1021/jm7014815
CHEMBL427911 166526 None 1 Human Binding pKi = 7.6 7.6 8 3
Displacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 396 6 1 7 2.3 CCCCn1c(=O)c2[nH]c(-c3cnn(Cc4cccc(F)c4)c3)nc2n(C)c1=O 10.1021/jm7014815
11121771 100343 None 0 Human Binding pKi = 7.6 7.6 3 3
Inhibition of [3H]ZM-241385 binding to human adenosine A2B receptorInhibition of [3H]ZM-241385 binding to human adenosine A2B receptor
ChEMBL 354 5 2 6 1.7 CCCn1c(=O)[nH]c2[nH]c(-c3ccc(/C=C/C(=O)OC)cc3)nc2c1=O 10.1021/jm011049y
CHEMBL289516 100343 None 0 Human Binding pKi = 7.6 7.6 3 3
Inhibition of [3H]ZM-241385 binding to human adenosine A2B receptorInhibition of [3H]ZM-241385 binding to human adenosine A2B receptor
ChEMBL 354 5 2 6 1.7 CCCn1c(=O)[nH]c2[nH]c(-c3ccc(/C=C/C(=O)OC)cc3)nc2c1=O 10.1021/jm011049y
11676986 165754 None 0 Human Binding pKi = 7.6 7.6 11 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 461 9 2 7 3.4 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccccn4)cc3)cc2n(CCC)c1=O 10.1021/jm0506221
CHEMBL424671 165754 None 0 Human Binding pKi = 7.6 7.6 11 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 461 9 2 7 3.4 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccccn4)cc3)cc2n(CCC)c1=O 10.1021/jm0506221
46233378 200338 None 0 Human Binding pKi = 7.6 7.6 3 3
Displacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells by microplate beta scintillation counterDisplacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells by microplate beta scintillation counter
ChEMBL 370 5 0 8 2.2 CCn1c(=O)c2c(nc(Cc3ccco3)n2C)n(Cc2cccs2)c1=O 10.1016/j.bmc.2010.01.028
CHEMBL597559 200338 None 0 Human Binding pKi = 7.6 7.6 3 3
Displacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells by microplate beta scintillation counterDisplacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells by microplate beta scintillation counter
ChEMBL 370 5 0 8 2.2 CCn1c(=O)c2c(nc(Cc3ccco3)n2C)n(Cc2cccs2)c1=O 10.1016/j.bmc.2010.01.028
16122818 57863 None 20 Human Binding pKi = 6.6 6.6 -44 3
Displacement of [3H]-MRS1754 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-MRS1754 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 60 mins
ChEMBL 353 4 2 4 4.0 CC(C)(C)CC(=O)Nc1c(F)cc(C(=O)Nc2nccs2)cc1F 10.1021/jm1008659
CHEMBL1671936 57863 None 20 Human Binding pKi = 6.6 6.6 -44 3
Displacement of [3H]-MRS1754 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-MRS1754 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 60 mins
ChEMBL 353 4 2 4 4.0 CC(C)(C)CC(=O)Nc1c(F)cc(C(=O)Nc2nccs2)cc1F 10.1021/jm1008659
9801343 112424 None 0 Human Binding pKi = 6.6 6.6 -41 4
Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 226-301Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 226-301
ChEMBL 404 4 2 9 2.9 COc1ccc(NC(=O)Nc2nc3nn(C)cc3c3nc(-c4ccco4)nn23)cc1 10.1021/jm001047y
CHEMBL329791 112424 None 0 Human Binding pKi = 6.6 6.6 -41 4
Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 226-301Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 226-301
ChEMBL 404 4 2 9 2.9 COc1ccc(NC(=O)Nc2nc3nn(C)cc3c3nc(-c4ccco4)nn23)cc1 10.1021/jm001047y
9801343 112424 None 0 Human Binding pKi = 6.6 6.6 -41 4
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells
ChEMBL 404 4 2 9 2.9 COc1ccc(NC(=O)Nc2nc3nn(C)cc3c3nc(-c4ccco4)nn23)cc1 10.1021/jm010818a
CHEMBL329791 112424 None 0 Human Binding pKi = 6.6 6.6 -41 4
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells
ChEMBL 404 4 2 9 2.9 COc1ccc(NC(=O)Nc2nc3nn(C)cc3c3nc(-c4ccco4)nn23)cc1 10.1021/jm010818a
9801343 112424 None 0 Human Binding pKi = 6.6 6.6 -41 4
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 226-301Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 226-301
ChEMBL 404 4 2 9 2.9 COc1ccc(NC(=O)Nc2nc3nn(C)cc3c3nc(-c4ccco4)nn23)cc1 10.1021/jm0109614
CHEMBL329791 112424 None 0 Human Binding pKi = 6.6 6.6 -41 4
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 226-301Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 226-301
ChEMBL 404 4 2 9 2.9 COc1ccc(NC(=O)Nc2nc3nn(C)cc3c3nc(-c4ccco4)nn23)cc1 10.1021/jm0109614
377 2758 None 53 Human Binding pKi = 6.6 6.6 -1479 15
Displacement of [3H]MRE-2029F20 from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]MRE-2029F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm900413e
425 2758 None 53 Human Binding pKi = 6.6 6.6 -1479 15
Displacement of [3H]MRE-2029F20 from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]MRE-2029F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm900413e
448222 2758 None 53 Human Binding pKi = 6.6 6.6 -1479 15
Displacement of [3H]MRE-2029F20 from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]MRE-2029F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm900413e
CHEMBL464859 2758 None 53 Human Binding pKi = 6.6 6.6 -1479 15
Displacement of [3H]MRE-2029F20 from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]MRE-2029F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm900413e
11641051 168852 None 0 Human Binding pKi = 6.6 6.6 1 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 454 9 2 7 2.2 COCCCn1c(=O)n(C)c(=O)c2[nH]c(-c3ccc(OCC(=O)NC4CCCC4)cc3)cc21 10.1021/jm0506221
CHEMBL438071 168852 None 0 Human Binding pKi = 6.6 6.6 1 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 454 9 2 7 2.2 COCCCn1c(=O)n(C)c(=O)c2[nH]c(-c3ccc(OCC(=O)NC4CCCC4)cc3)cc21 10.1021/jm0506221
44410402 76120 None 0 Human Binding pKi = 4.6 4.6 -12882 4
Displacement of [125I]ABOPX from human adenosine A2B receptor in HEK cellsDisplacement of [125I]ABOPX from human adenosine A2B receptor in HEK cells
ChEMBL 444 5 5 10 -0.3 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC)nc(C#CC4(O)CCCC4)nc32)[C@H](O)[C@@H]1O 10.1016/j.bmcl.2006.01.110
CHEMBL205768 76120 None 0 Human Binding pKi = 4.6 4.6 -12882 4
Displacement of [125I]ABOPX from human adenosine A2B receptor in HEK cellsDisplacement of [125I]ABOPX from human adenosine A2B receptor in HEK cells
ChEMBL 444 5 5 10 -0.3 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC)nc(C#CC4(O)CCCC4)nc32)[C@H](O)[C@@H]1O 10.1016/j.bmcl.2006.01.110
5604 3368 None 35 Human Binding pKi = 6.6 6.6 -1995 10
Binding affinity to human adenosine A2B receptor by radioligand displacement assayBinding affinity to human adenosine A2B receptor by radioligand displacement assay
ChEMBL 356 5 1 5 2.8 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C12CC3CC2CC(C1)C3 10.1039/C8MD00070K
64627 3368 None 35 Human Binding pKi = 6.6 6.6 -1995 10
Binding affinity to human adenosine A2B receptor by radioligand displacement assayBinding affinity to human adenosine A2B receptor by radioligand displacement assay
ChEMBL 356 5 1 5 2.8 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C12CC3CC2CC(C1)C3 10.1039/C8MD00070K
CHEMBL52333 3368 None 35 Human Binding pKi = 6.6 6.6 -1995 10
Binding affinity to human adenosine A2B receptor by radioligand displacement assayBinding affinity to human adenosine A2B receptor by radioligand displacement assay
ChEMBL 356 5 1 5 2.8 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C12CC3CC2CC(C1)C3 10.1039/C8MD00070K
DB05360 3368 None 35 Human Binding pKi = 6.6 6.6 -1995 10
Binding affinity to human adenosine A2B receptor by radioligand displacement assayBinding affinity to human adenosine A2B receptor by radioligand displacement assay
ChEMBL 356 5 1 5 2.8 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C12CC3CC2CC(C1)C3 10.1039/C8MD00070K
11674882 73397 None 0 Human Binding pKi = 6.6 6.6 - 1
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 359 5 2 7 0.7 COc1cc(-c2cc3c([nH]2)c(=O)n(C)c(=O)n3C)ccc1OCC(=O)O 10.1021/jm0506221
CHEMBL201547 73397 None 0 Human Binding pKi = 6.6 6.6 - 1
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 359 5 2 7 0.7 COc1cc(-c2cc3c([nH]2)c(=O)n(C)c(=O)n3C)ccc1OCC(=O)O 10.1021/jm0506221
46228057 201331 None 0 Human Binding pKi = 6.6 6.6 -1 3
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 366 5 1 7 1.8 C#CCn1c(=O)c2[nH]c(Cc3cccs3)nc2n(Cc2ccco2)c1=O 10.1016/j.bmc.2009.07.034
CHEMBL604283 201331 None 0 Human Binding pKi = 6.6 6.6 -1 3
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 366 5 1 7 1.8 C#CCn1c(=O)c2[nH]c(Cc3cccs3)nc2n(Cc2ccco2)c1=O 10.1016/j.bmc.2009.07.034
11544894 96376 None 0 Human Binding pKi = 7.6 7.6 7 3
Displacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 354 3 1 7 1.0 Cn1c(=O)c2[nH]c(-c3cnn(Cc4cccc(F)c4)c3)nc2n(C)c1=O 10.1021/jm7014815
CHEMBL261722 96376 None 0 Human Binding pKi = 7.6 7.6 7 3
Displacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 354 3 1 7 1.0 Cn1c(=O)c2[nH]c(-c3cnn(Cc4cccc(F)c4)c3)nc2n(C)c1=O 10.1021/jm7014815
44450517 158335 None 0 Human Binding pKi = 7.6 7.6 6 3
Displacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 390 6 1 7 2.2 CCn1c(=O)n(CC2CC2)c(=O)c2[nH]c(-c3cnn(Cc4ccccc4)c3)nc21 10.1021/jm7014815
CHEMBL408936 158335 None 0 Human Binding pKi = 7.6 7.6 6 3
Displacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 390 6 1 7 2.2 CCn1c(=O)n(CC2CC2)c(=O)c2[nH]c(-c3cnn(Cc4ccccc4)c3)nc21 10.1021/jm7014815
11544894 96376 None 0 Human Binding pKi = 7.6 7.6 7 3
Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cellsDisplacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells
ChEMBL 354 3 1 7 1.0 Cn1c(=O)c2[nH]c(-c3cnn(Cc4cccc(F)c4)c3)nc2n(C)c1=O 10.1021/jm051268+
CHEMBL261722 96376 None 0 Human Binding pKi = 7.6 7.6 7 3
Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cellsDisplacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells
ChEMBL 354 3 1 7 1.0 Cn1c(=O)c2[nH]c(-c3cnn(Cc4cccc(F)c4)c3)nc2n(C)c1=O 10.1021/jm051268+
155537221 172276 None 0 Human Binding pKi = 7.6 7.6 - 1
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 377 3 1 6 4.0 CC1=C(C(=O)OCC(F)(F)F)C(c2ccco2)n2c(nc3ccccc32)N1 10.1016/j.ejmech.2021.113907
CHEMBL4474714 172276 None 0 Human Binding pKi = 7.6 7.6 - 1
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 377 3 1 6 4.0 CC1=C(C(=O)OCC(F)(F)F)C(c2ccco2)n2c(nc3ccccc32)N1 10.1016/j.ejmech.2021.113907
155537221 172276 None 0 Human Binding pKi = 7.6 7.6 - 1
Displacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assayDisplacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assay
ChEMBL 377 3 1 6 4.0 CC1=C(C(=O)OCC(F)(F)F)C(c2ccco2)n2c(nc3ccccc32)N1 10.1021/acs.jmedchem.9b01340
CHEMBL4474714 172276 None 0 Human Binding pKi = 7.6 7.6 - 1
Displacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assayDisplacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assay
ChEMBL 377 3 1 6 4.0 CC1=C(C(=O)OCC(F)(F)F)C(c2ccco2)n2c(nc3ccccc32)N1 10.1021/acs.jmedchem.9b01340
11710918 138806 None 0 Human Binding pKi = 7.6 7.6 1 3
Displacement of [3H]PSB298 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB298 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 393 7 4 7 -0.2 CCCn1c(=O)[nH]c2[nH]c(-c3ccc(S(=O)(=O)NCCO)cc3)nc2c1=O 10.1021/jm060277v
CHEMBL378102 138806 None 0 Human Binding pKi = 7.6 7.6 1 3
Displacement of [3H]PSB298 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB298 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 393 7 4 7 -0.2 CCCn1c(=O)[nH]c2[nH]c(-c3ccc(S(=O)(=O)NCCO)cc3)nc2c1=O 10.1021/jm060277v
11713242 72595 None 0 Human Binding pKi = 7.6 7.6 1 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 512 9 2 6 4.8 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(F)cc4)cc3)c(Cl)c2n(CCC)c1=O 10.1021/jm0506221
CHEMBL199326 72595 None 0 Human Binding pKi = 7.6 7.6 1 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 512 9 2 6 4.8 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(F)cc4)cc3)c(Cl)c2n(CCC)c1=O 10.1021/jm0506221
11590097 74488 None 0 Human Binding pKi = 7.6 7.6 8 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 432 6 2 6 2.5 CC(NC(=O)COc1ccc(-c2cc3c([nH]2)c(=O)n(C)c(=O)n3C)cc1)c1ccccc1 10.1021/jm0506221
CHEMBL202828 74488 None 0 Human Binding pKi = 7.6 7.6 8 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 432 6 2 6 2.5 CC(NC(=O)COc1ccc(-c2cc3c([nH]2)c(=O)n(C)c(=O)n3C)cc1)c1ccccc1 10.1021/jm0506221
11548192 165998 None 0 Human Binding pKi = 7.6 7.6 1 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 524 10 2 7 4.7 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(OC)cc4)cc3)c(Cl)c2n(CCC)c1=O 10.1021/jm0506221
CHEMBL425395 165998 None 0 Human Binding pKi = 7.6 7.6 1 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 524 10 2 7 4.7 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(OC)cc4)cc3)c(Cl)c2n(CCC)c1=O 10.1021/jm0506221
44451489 159074 None 0 Human Binding pKi = 7.6 7.6 22 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 489 5 2 8 1.7 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCN(c5ccc(O)cc5)CC4)cc3)cc2n(C)c1=O 10.1016/j.bmc.2008.01.002
CHEMBL409725 159074 None 0 Human Binding pKi = 7.6 7.6 22 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 489 5 2 8 1.7 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCN(c5ccc(O)cc5)CC4)cc3)cc2n(C)c1=O 10.1016/j.bmc.2008.01.002
46227973 199743 None 0 Human Binding pKi = 7.6 7.6 14 3
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 400 7 0 9 1.8 COCCn1c(=O)c2c(nc(Cc3cccs3)n2C)n(Cc2ccco2)c1=O 10.1016/j.bmc.2009.07.034
CHEMBL593572 199743 None 0 Human Binding pKi = 7.6 7.6 14 3
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 400 7 0 9 1.8 COCCn1c(=O)c2c(nc(Cc3cccs3)n2C)n(Cc2ccco2)c1=O 10.1016/j.bmc.2009.07.034
145964230 164011 None 0 Human Binding pKi = 7.6 7.6 1 3
Displacement of [3H]PSB-603 from recombinant human adenosine A2B receptor expressed in CHO cell membranes after 75 mins by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human adenosine A2B receptor expressed in CHO cell membranes after 75 mins by liquid scintillation counting method
ChEMBL 461 10 3 6 2.6 CCCn1c(=O)[nH]c2nc(-c3ccc(OCC(=O)NCCCc4ccccc4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.7b01627
CHEMBL4208432 164011 None 0 Human Binding pKi = 7.6 7.6 1 3
Displacement of [3H]PSB-603 from recombinant human adenosine A2B receptor expressed in CHO cell membranes after 75 mins by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human adenosine A2B receptor expressed in CHO cell membranes after 75 mins by liquid scintillation counting method
ChEMBL 461 10 3 6 2.6 CCCn1c(=O)[nH]c2nc(-c3ccc(OCC(=O)NCCCc4ccccc4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.7b01627
9901171 176824 None 0 Human Binding pKi = 6.6 6.6 -107 4
Displacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation countingDisplacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation counting
ChEMBL 307 3 2 8 1.7 Nc1cccc(Cn2nnc3c(-c4ccco4)nc(N)nc32)c1 10.1021/jm800961g
CHEMBL461008 176824 None 0 Human Binding pKi = 6.6 6.6 -107 4
Displacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation countingDisplacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation counting
ChEMBL 307 3 2 8 1.7 Nc1cccc(Cn2nnc3c(-c4ccco4)nc(N)nc32)c1 10.1021/jm800961g
2153 3800 None 115 Human Binding pKi = 5.6 5.6 -21 14
Displacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cell membraneDisplacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cell membrane
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1016/j.bmc.2010.02.014
2153.0 3800 None 115 Human Binding pKi = 5.6 5.6 -21 14
Displacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cell membraneDisplacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cell membrane
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1016/j.bmc.2010.02.014
2620 3800 None 115 Human Binding pKi = 5.6 5.6 -21 14
Displacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cell membraneDisplacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cell membrane
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1016/j.bmc.2010.02.014
413 3800 None 115 Human Binding pKi = 5.6 5.6 -21 14
Displacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cell membraneDisplacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cell membrane
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1016/j.bmc.2010.02.014
CHEMBL190 3800 None 115 Human Binding pKi = 5.6 5.6 -21 14
Displacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cell membraneDisplacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cell membrane
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1016/j.bmc.2010.02.014
DB00277 3800 None 115 Human Binding pKi = 5.6 5.6 -21 14
Displacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cell membraneDisplacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cell membrane
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1016/j.bmc.2010.02.014
9858578 188986 None 0 Human Binding pKi = 6.6 6.6 -31 4
Displacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation countingDisplacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation counting
ChEMBL 327 3 1 8 2.1 Nc1nc(-c2nccs2)c2nnn(Cc3ccccc3F)c2n1 10.1021/jm800961g
CHEMBL508558 188986 None 0 Human Binding pKi = 6.6 6.6 -31 4
Displacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation countingDisplacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation counting
ChEMBL 327 3 1 8 2.1 Nc1nc(-c2nccs2)c2nnn(Cc3ccccc3F)c2n1 10.1021/jm800961g
10256007 122929 None 0 Human Binding pKi = 5.6 5.6 -10 4
Inhibition of [3H]DPCPX binding to human adenosine A2B receptor expressed in HEK293 cellsInhibition of [3H]DPCPX binding to human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 516 8 5 14 0.1 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(N[C@H](CO)Cc5ccc(Cl)cc5)nc43)[C@H](O)[C@@H]2O)n1 10.1021/jm031143+
CHEMBL360646 122929 None 0 Human Binding pKi = 5.6 5.6 -10 4
Inhibition of [3H]DPCPX binding to human adenosine A2B receptor expressed in HEK293 cellsInhibition of [3H]DPCPX binding to human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 516 8 5 14 0.1 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(N[C@H](CO)Cc5ccc(Cl)cc5)nc43)[C@H](O)[C@@H]2O)n1 10.1021/jm031143+
145979285 166680 None 0 Human Binding pKi = 6.6 6.6 -1 4
Displacement of [3H]PSB-602 from human adenosine A2B receptor expressed in CHO cell membranesDisplacement of [3H]PSB-602 from human adenosine A2B receptor expressed in CHO cell membranes
ChEMBL 604 16 1 11 3.2 CCCCn1c(=O)c2c(nc3n2CCCN3CCc2ccc(OCC(=O)NCCCn3ccnc3)cc2)n(CCCC)c1=O 10.1039/C8MD00070K
CHEMBL4282002 166680 None 0 Human Binding pKi = 6.6 6.6 -1 4
Displacement of [3H]PSB-602 from human adenosine A2B receptor expressed in CHO cell membranesDisplacement of [3H]PSB-602 from human adenosine A2B receptor expressed in CHO cell membranes
ChEMBL 604 16 1 11 3.2 CCCCn1c(=O)c2c(nc3n2CCCN3CCc2ccc(OCC(=O)NCCCn3ccnc3)cc2)n(CCCC)c1=O 10.1039/C8MD00070K
46228025 199947 None 0 Human Binding pKi = 6.6 6.6 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 416 8 1 8 2.9 CCSCCn1c(=O)c2[nH]c(Cc3cccs3)nc2n(Cc2ccco2)c1=O 10.1016/j.bmc.2009.07.034
CHEMBL594970 199947 None 0 Human Binding pKi = 6.6 6.6 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 416 8 1 8 2.9 CCSCCn1c(=O)c2[nH]c(Cc3cccs3)nc2n(Cc2ccco2)c1=O 10.1016/j.bmc.2009.07.034
127034216 138961 None 0 Human Binding pKi = 6.6 6.6 - 1
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 minsDisplacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 mins
ChEMBL 287 3 1 6 2.7 CC1=C(C(=O)OC(C)C)C(c2ccoc2)n2ccnc2N1 10.1021/acs.jmedchem.5b01586
CHEMBL3785215 138961 None 0 Human Binding pKi = 6.6 6.6 - 1
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 minsDisplacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 mins
ChEMBL 287 3 1 6 2.7 CC1=C(C(=O)OC(C)C)C(c2ccoc2)n2ccnc2N1 10.1021/acs.jmedchem.5b01586
69550 204102 None 86 Human Binding pKi = 4.6 4.6 - 1
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 238 2 1 7 -1.5 Cn1c(=O)c2c(ncn2CC(=O)O)n(C)c1=O 10.1021/jm0104318
CHEMBL70246 204102 None 86 Human Binding pKi = 4.6 4.6 - 1
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 238 2 1 7 -1.5 Cn1c(=O)c2c(ncn2CC(=O)O)n(C)c1=O 10.1021/jm0104318
156018530 177794 None 0 Human Binding pKi = 6.6 6.6 - 1
Displacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting methodDisplacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting method
ChEMBL 354 3 1 7 3.7 CC1=C(C(=O)OC(C)C)C(c2cnsc2)n2c(nc3ccccc32)N1 10.1021/acs.jmedchem.0c00564
CHEMBL4643403 177794 None 0 Human Binding pKi = 6.6 6.6 - 1
Displacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting methodDisplacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting method
ChEMBL 354 3 1 7 3.7 CC1=C(C(=O)OC(C)C)C(c2cnsc2)n2c(nc3ccccc32)N1 10.1021/acs.jmedchem.0c00564
44390444 64933 None 0 Human Binding pKi = 5.6 5.6 - 1
Binding affinity for adenosine A2b receptor by using as [3H]ZM-241385 (14 nM) radioligand in membranes from HEK-A2B cellsBinding affinity for adenosine A2b receptor by using as [3H]ZM-241385 (14 nM) radioligand in membranes from HEK-A2B cells
ChEMBL 516 10 1 10 4.0 CCCn1c(=O)c2nc(-c3ccc(OCc4nc(-c5ccc(OC)cc5)no4)cc3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2004.11.044
CHEMBL182259 64933 None 0 Human Binding pKi = 5.6 5.6 - 1
Binding affinity for adenosine A2b receptor by using as [3H]ZM-241385 (14 nM) radioligand in membranes from HEK-A2B cellsBinding affinity for adenosine A2b receptor by using as [3H]ZM-241385 (14 nM) radioligand in membranes from HEK-A2B cells
ChEMBL 516 10 1 10 4.0 CCCn1c(=O)c2nc(-c3ccc(OCc4nc(-c5ccc(OC)cc5)no4)cc3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2004.11.044
70689262 77977 None 0 Human Binding pKi = 5.6 5.6 -1202 4
Inhibition of [3H]DPCPX binding to human adenosine A2B receptor expressed in HEK293 cellsInhibition of [3H]DPCPX binding to human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 496 8 4 14 0.5 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(N[C@H](C)Cc5ccc(OC)cc5)nc43)[C@H](O)[C@@H]2O)n1 10.1021/jm031143+
CHEMBL2096798 77977 None 0 Human Binding pKi = 5.6 5.6 -1202 4
Inhibition of [3H]DPCPX binding to human adenosine A2B receptor expressed in HEK293 cellsInhibition of [3H]DPCPX binding to human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 496 8 4 14 0.5 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(N[C@H](C)Cc5ccc(OC)cc5)nc43)[C@H](O)[C@@H]2O)n1 10.1021/jm031143+
135493281 109626 None 0 Human Binding pKi = 7.6 7.6 18 2
Binding affinity of compound for displacement of [3H]DPCPX binding in HEK293 membranes expressing human A2B adenosine receptorsBinding affinity of compound for displacement of [3H]DPCPX binding in HEK293 membranes expressing human A2B adenosine receptors
ChEMBL 483 8 2 8 2.9 CCCn1c(=O)c2nc(-c3cc(NC(=O)Cc4ccc(Cl)cc4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
CHEMBL32225 109626 None 0 Human Binding pKi = 7.6 7.6 18 2
Binding affinity of compound for displacement of [3H]DPCPX binding in HEK293 membranes expressing human A2B adenosine receptorsBinding affinity of compound for displacement of [3H]DPCPX binding in HEK293 membranes expressing human A2B adenosine receptors
ChEMBL 483 8 2 8 2.9 CCCn1c(=O)c2nc(-c3cc(NC(=O)Cc4ccc(Cl)cc4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
135493281 109626 None 0 Human Binding pKi = 7.6 7.6 18 2
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 483 8 2 8 2.9 CCCn1c(=O)c2nc(-c3cc(NC(=O)Cc4ccc(Cl)cc4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
CHEMBL32225 109626 None 0 Human Binding pKi = 7.6 7.6 18 2
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 483 8 2 8 2.9 CCCn1c(=O)c2nc(-c3cc(NC(=O)Cc4ccc(Cl)cc4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
21958525 155558 None 0 Human Binding pKi = 7.6 7.6 - 1
Displacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranesDisplacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranes
ChEMBL 432 5 2 6 3.0 CC(C)Cn1c(=O)[nH]c2nc(-c3cnn(Cc4cccc(C(F)(F)F)c4)c3)[nH]c2c1=O 10.1016/j.bmcl.2008.01.008
CHEMBL404348 155558 None 0 Human Binding pKi = 7.6 7.6 - 1
Displacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranesDisplacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranes
ChEMBL 432 5 2 6 3.0 CC(C)Cn1c(=O)[nH]c2nc(-c3cnn(Cc4cccc(C(F)(F)F)c4)c3)[nH]c2c1=O 10.1016/j.bmcl.2008.01.008
16720106 168885 None 0 Human Binding pKi = 7.6 7.6 - 1
Displacement of [3H]DPCPX from human A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human A2B receptor expressed in HEK293 cells
ChEMBL 346 4 1 8 2.6 Cn1cc(Nc2ncc(-c3ccncn3)c(-c3ccco3)n2)ccc1=O 10.1021/jm061333v
CHEMBL438306 168885 None 0 Human Binding pKi = 7.6 7.6 - 1
Displacement of [3H]DPCPX from human A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human A2B receptor expressed in HEK293 cells
ChEMBL 346 4 1 8 2.6 Cn1cc(Nc2ncc(-c3ccncn3)c(-c3ccco3)n2)ccc1=O 10.1021/jm061333v
10906943 116530 None 0 Human Binding pKi = 7.6 7.6 1 4
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 479 7 1 8 5.1 CC(C)CCn1cc2c(nc(NC(=O)Cc3cccc4ccccc34)n3nc(-c4ccco4)nc23)n1 10.1021/jm030852k
CHEMBL336217 116530 None 0 Human Binding pKi = 7.6 7.6 1 4
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 479 7 1 8 5.1 CC(C)CCn1cc2c(nc(NC(=O)Cc3cccc4ccccc34)n3nc(-c4ccco4)nc23)n1 10.1021/jm030852k
46880372 5521 None 0 Human Binding pKi = 7.6 7.6 1 4
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 306 3 1 3 3.5 O=C(Nc1ccc(Br)c(-c2ccco2)n1)C1CC1 10.1016/j.bmcl.2010.01.045
CHEMBL1076562 5521 None 0 Human Binding pKi = 7.6 7.6 1 4
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 306 3 1 3 3.5 O=C(Nc1ccc(Br)c(-c2ccco2)n1)C1CC1 10.1016/j.bmcl.2010.01.045
135874429 95755 None 0 Human Binding pKi = 7.6 7.6 23 2
Displacement of [3H]MRE2029F20 from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]MRE2029F20 from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 483 8 2 8 3.2 CCCn1c(=O)c2[nH]c(-c3cc(C)n(CC(=O)Nc4cccc(Cl)c4)n3)nc2n(CCC)c1=O 10.1016/j.bmc.2007.11.058
CHEMBL258473 95755 None 0 Human Binding pKi = 7.6 7.6 23 2
Displacement of [3H]MRE2029F20 from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]MRE2029F20 from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 483 8 2 8 3.2 CCCn1c(=O)c2[nH]c(-c3cc(C)n(CC(=O)Nc4cccc(Cl)c4)n3)nc2n(CCC)c1=O 10.1016/j.bmc.2007.11.058
135874414 96255 None 0 Human Binding pKi = 7.6 7.6 - 1
Displacement of [3H]MRE2029F20 from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]MRE2029F20 from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 575 8 2 8 3.1 CCCn1c(=O)c2[nH]c(-c3cc(C)n(CC(=O)Nc4ccc(I)cc4)n3)nc2n(CCC)c1=O 10.1016/j.bmc.2007.11.058
CHEMBL261027 96255 None 0 Human Binding pKi = 7.6 7.6 - 1
Displacement of [3H]MRE2029F20 from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]MRE2029F20 from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 575 8 2 8 3.1 CCCn1c(=O)c2[nH]c(-c3cc(C)n(CC(=O)Nc4ccc(I)cc4)n3)nc2n(CCC)c1=O 10.1016/j.bmc.2007.11.058
176407 4148 None 84 Human Binding pKi = 7.6 7.6 -34 6
Displacement of [3H]ZM-241385 from human A2B receptor expressed in HEK-293 cell membranesDisplacement of [3H]ZM-241385 from human A2B receptor expressed in HEK-293 cell membranes
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1016/j.ejmech.2015.12.019
405 4148 None 84 Human Binding pKi = 7.6 7.6 -34 6
Displacement of [3H]ZM-241385 from human A2B receptor expressed in HEK-293 cell membranesDisplacement of [3H]ZM-241385 from human A2B receptor expressed in HEK-293 cell membranes
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1016/j.ejmech.2015.12.019
CHEMBL113142 4148 None 84 Human Binding pKi = 7.6 7.6 -34 6
Displacement of [3H]ZM-241385 from human A2B receptor expressed in HEK-293 cell membranesDisplacement of [3H]ZM-241385 from human A2B receptor expressed in HEK-293 cell membranes
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1016/j.ejmech.2015.12.019
DB08770 4148 None 84 Human Binding pKi = 7.6 7.6 -34 6
Displacement of [3H]ZM-241385 from human A2B receptor expressed in HEK-293 cell membranesDisplacement of [3H]ZM-241385 from human A2B receptor expressed in HEK-293 cell membranes
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1016/j.ejmech.2015.12.019
50925499 19236 None 0 Human Binding pKi = 7.6 7.6 3 2
Displacement of [3H]ZM241385 from human adenosine A2B receptor transfected in CHO cells after 60 mins by scintillation countingDisplacement of [3H]ZM241385 from human adenosine A2B receptor transfected in CHO cells after 60 mins by scintillation counting
ChEMBL 523 9 2 5 5.9 CC(C)(NC(=O)COc1ccc2[nH]c(=O)c(-c3nccs3)c(CCc3ccccc3)c2c1)c1ccccc1 10.1016/j.bmcl.2010.10.030
CHEMBL1290101 19236 None 0 Human Binding pKi = 7.6 7.6 3 2
Displacement of [3H]ZM241385 from human adenosine A2B receptor transfected in CHO cells after 60 mins by scintillation countingDisplacement of [3H]ZM241385 from human adenosine A2B receptor transfected in CHO cells after 60 mins by scintillation counting
ChEMBL 523 9 2 5 5.9 CC(C)(NC(=O)COc1ccc2[nH]c(=O)c(-c3nccs3)c(CCc3ccccc3)c2c1)c1ccccc1 10.1016/j.bmcl.2010.10.030
52943652 19252 None 0 Human Binding pKi = 7.6 7.6 1 3
Displacement of [3H]ZM241385 from human adenosine A2B receptor transfected in CHO cells after 60 mins by scintillation countingDisplacement of [3H]ZM241385 from human adenosine A2B receptor transfected in CHO cells after 60 mins by scintillation counting
ChEMBL 509 9 2 5 5.7 C[C@H](NC(=O)COc1ccc2[nH]c(=O)c(-c3nccs3)c(CCc3ccccc3)c2c1)c1ccccc1 10.1016/j.bmcl.2010.10.030
CHEMBL1290210 19252 None 0 Human Binding pKi = 7.6 7.6 1 3
Displacement of [3H]ZM241385 from human adenosine A2B receptor transfected in CHO cells after 60 mins by scintillation countingDisplacement of [3H]ZM241385 from human adenosine A2B receptor transfected in CHO cells after 60 mins by scintillation counting
ChEMBL 509 9 2 5 5.7 C[C@H](NC(=O)COc1ccc2[nH]c(=O)c(-c3nccs3)c(CCc3ccccc3)c2c1)c1ccccc1 10.1016/j.bmcl.2010.10.030
11589625 78247 None 0 Human Binding pKi = 7.6 7.6 -1 3
Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cellsDisplacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells
ChEMBL 410 7 1 7 2.8 CCCn1c(=O)c2nc(-c3cnn(Cc4ccccc4F)c3)[nH]c2n(CCC)c1=O 10.1021/jm051268+
CHEMBL210649 78247 None 0 Human Binding pKi = 7.6 7.6 -1 3
Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cellsDisplacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells
ChEMBL 410 7 1 7 2.8 CCCn1c(=O)c2nc(-c3cnn(Cc4ccccc4F)c3)[nH]c2n(CCC)c1=O 10.1021/jm051268+
11677252 73862 None 0 Human Binding pKi = 7.6 7.6 10 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 475 10 2 7 3.1 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)NCc4ccncc4)cc3)cc2n(CCC)c1=O 10.1021/jm0506221
CHEMBL201895 73862 None 0 Human Binding pKi = 7.6 7.6 10 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 475 10 2 7 3.1 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)NCc4ccncc4)cc3)cc2n(CCC)c1=O 10.1021/jm0506221
11386134 67469 None 0 Human Binding pKi = 4.6 4.6 -1995 5
Selectivity for recombinant human adenosine A2b receptorSelectivity for recombinant human adenosine A2b receptor
ChEMBL 482 4 1 11 2.1 Cn1nc(C(F)(F)F)c(CN2CCN(c3nc(N)n4nc(-c5ccco5)nc4n3)CC2)c1Cl 10.1021/jm0498405
CHEMBL189192 67469 None 0 Human Binding pKi = 4.6 4.6 -1995 5
Selectivity for recombinant human adenosine A2b receptorSelectivity for recombinant human adenosine A2b receptor
ChEMBL 482 4 1 11 2.1 Cn1nc(C(F)(F)F)c(CN2CCN(c3nc(N)n4nc(-c5ccco5)nc4n3)CC2)c1Cl 10.1021/jm0498405
46233348 200298 None 0 Human Binding pKi = 6.6 6.6 6 2
Displacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells by microplate beta scintillation counterDisplacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells by microplate beta scintillation counter
ChEMBL 364 5 0 7 2.1 CCn1c(=O)c2c(nc(Cc3ccco3)n2C)n(Cc2ccccc2)c1=O 10.1016/j.bmc.2010.01.028
CHEMBL597355 200298 None 0 Human Binding pKi = 6.6 6.6 6 2
Displacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells by microplate beta scintillation counterDisplacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells by microplate beta scintillation counter
ChEMBL 364 5 0 7 2.1 CCn1c(=O)c2c(nc(Cc3ccco3)n2C)n(Cc2ccccc2)c1=O 10.1016/j.bmc.2010.01.028
21874786 189839 None 0 Human Binding pKi = 6.6 6.6 -93 4
Displacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation countingDisplacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation counting
ChEMBL 306 3 1 7 2.4 Cc1ccccc1Cn1nnc2c(-c3ccco3)nc(N)nc21 10.1021/jm800961g
CHEMBL516611 189839 None 0 Human Binding pKi = 6.6 6.6 -93 4
Displacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation countingDisplacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation counting
ChEMBL 306 3 1 7 2.4 Cc1ccccc1Cn1nnc2c(-c3ccco3)nc(N)nc21 10.1021/jm800961g
162676957 183536 None 0 Human Binding pKi = 5.6 5.6 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 306 4 2 4 2.7 CC1=C(C(=O)OCC2CCC2)C(c2cccs2)NC(=O)N1 10.1021/acs.jmedchem.0c01431
CHEMBL4800019 183536 None 0 Human Binding pKi = 5.6 5.6 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 306 4 2 4 2.7 CC1=C(C(=O)OCC2CCC2)C(c2cccs2)NC(=O)N1 10.1021/acs.jmedchem.0c01431
10993916 57156 None 0 Human Binding pKi = 6.5 6.5 -12 4
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 235-347Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 235-347
ChEMBL 442 3 2 8 3.9 Cn1cc2c(nc(NC(=O)Nc3ccc(C(F)(F)F)cc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm0109614
CHEMBL164686 57156 None 0 Human Binding pKi = 6.5 6.5 -12 4
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 235-347Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 235-347
ChEMBL 442 3 2 8 3.9 Cn1cc2c(nc(NC(=O)Nc3ccc(C(F)(F)F)cc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm0109614
750351 189302 None 13 Human Binding pKi = 6.5 6.5 5 2
Displacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cells
ChEMBL 271 1 2 5 0.9 Cn1c(=O)c2[nH]c(-c3ccccc3)c(O)c2n(C)c1=O 10.1016/j.bmc.2008.09.067
CHEMBL512216 189302 None 13 Human Binding pKi = 6.5 6.5 5 2
Displacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cells
ChEMBL 271 1 2 5 0.9 Cn1c(=O)c2[nH]c(-c3ccccc3)c(O)c2n(C)c1=O 10.1016/j.bmc.2008.09.067
11660427 73398 None 0 Human Binding pKi = 6.5 6.5 6 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 357 5 1 7 1.2 CCOC(=O)COc1ccc(-c2cc3c([nH]2)c(=O)n(C)c(=O)n3C)cc1 10.1021/jm0506221
CHEMBL201548 73398 None 0 Human Binding pKi = 6.5 6.5 6 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 357 5 1 7 1.2 CCOC(=O)COc1ccc(-c2cc3c([nH]2)c(=O)n(C)c(=O)n3C)cc1 10.1021/jm0506221
12391837 9728 None 1 Human Binding pKi = 6.5 6.5 - 1
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 299 2 1 6 0.7 CN(C)c1ccc(-c2nc3c(=O)n(C)c(=O)n(C)c3[nH]2)cc1 10.1021/jm0104318
CHEMBL11332 9728 None 1 Human Binding pKi = 6.5 6.5 - 1
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 299 2 1 6 0.7 CN(C)c1ccc(-c2nc3c(=O)n(C)c(=O)n(C)c3[nH]2)cc1 10.1021/jm0104318
25027416 64479 None 0 Human Binding pKi = 5.5 5.5 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by liquid scintillation countingDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by liquid scintillation counting
ChEMBL 281 2 2 4 2.8 O=C(Nc1ccc(O)cc1)c1coc2ccccc2c1=O 10.1016/j.ejmech.2012.05.033
CHEMBL1814064 64479 None 0 Human Binding pKi = 5.5 5.5 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by liquid scintillation countingDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by liquid scintillation counting
ChEMBL 281 2 2 4 2.8 O=C(Nc1ccc(O)cc1)c1coc2ccccc2c1=O 10.1016/j.ejmech.2012.05.033
44236566 158979 None 0 Human Binding pKi = 7.5 7.5 - 1
Displacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 minsDisplacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 mins
ChEMBL 484 6 1 7 3.6 CCCn1c(=O)c2[nH]c(-c3cnn(CC#Cc4ccccc4C(F)(F)F)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2017.04.014
CHEMBL4096238 158979 None 0 Human Binding pKi = 7.5 7.5 - 1
Displacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 minsDisplacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 mins
ChEMBL 484 6 1 7 3.6 CCCn1c(=O)c2[nH]c(-c3cnn(CC#Cc4ccccc4C(F)(F)F)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2017.04.014
16070220 58024 None 0 Human Binding pKi = 7.5 7.5 3 3
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 307 4 1 6 2.5 O=C(Nc1cnc(-c2ccncn2)c(-c2ccco2)n1)C1CC1 10.1021/ml100249e
CHEMBL1672626 58024 None 0 Human Binding pKi = 7.5 7.5 3 3
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 307 4 1 6 2.5 O=C(Nc1cnc(-c2ccncn2)c(-c2ccco2)n1)C1CC1 10.1021/ml100249e
11532717 77785 None 0 Human Binding pKi = 7.5 7.5 2 3
Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cellsDisplacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells
ChEMBL 460 7 1 7 3.9 CCCn1c(=O)c2nc(-c3cnn(Cc4cc(Cl)ccc4Cl)c3)[nH]c2n(CCC)c1=O 10.1021/jm051268+
CHEMBL209174 77785 None 0 Human Binding pKi = 7.5 7.5 2 3
Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cellsDisplacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells
ChEMBL 460 7 1 7 3.9 CCCn1c(=O)c2nc(-c3cnn(Cc4cc(Cl)ccc4Cl)c3)[nH]c2n(CCC)c1=O 10.1021/jm051268+
155524137 170882 None 0 Human Binding pKi = 7.5 7.5 - 1
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 391 3 1 6 4.4 CC1=C(C(=O)OC(C)C(F)(F)F)C(c2ccco2)n2c(nc3ccccc32)N1 10.1016/j.ejmech.2021.113907
CHEMBL4454378 170882 None 0 Human Binding pKi = 7.5 7.5 - 1
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 391 3 1 6 4.4 CC1=C(C(=O)OC(C)C(F)(F)F)C(c2ccco2)n2c(nc3ccccc32)N1 10.1016/j.ejmech.2021.113907
127030364 139139 None 0 Human Binding pKi = 7.5 7.5 - 1
Displacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting methodDisplacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting method
ChEMBL 353 3 1 6 4.3 CC1=C(C(=O)OC(C)C)C(c2ccsc2)n2c(nc3ccccc32)N1 10.1021/acs.jmedchem.0c00564
CHEMBL3787034 139139 None 0 Human Binding pKi = 7.5 7.5 - 1
Displacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting methodDisplacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting method
ChEMBL 353 3 1 6 4.3 CC1=C(C(=O)OC(C)C)C(c2ccsc2)n2c(nc3ccccc32)N1 10.1021/acs.jmedchem.0c00564
127030364 139139 None 0 Human Binding pKi = 7.5 7.5 - 1
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 minsDisplacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 mins
ChEMBL 353 3 1 6 4.3 CC1=C(C(=O)OC(C)C)C(c2ccsc2)n2c(nc3ccccc32)N1 10.1021/acs.jmedchem.5b01586
CHEMBL3787034 139139 None 0 Human Binding pKi = 7.5 7.5 - 1
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 minsDisplacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 mins
ChEMBL 353 3 1 6 4.3 CC1=C(C(=O)OC(C)C)C(c2ccsc2)n2c(nc3ccccc32)N1 10.1021/acs.jmedchem.5b01586
127030364 139139 None 0 Human Binding pKi = 7.5 7.5 - 1
Displacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assayDisplacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assay
ChEMBL 353 3 1 6 4.3 CC1=C(C(=O)OC(C)C)C(c2ccsc2)n2c(nc3ccccc32)N1 10.1021/acs.jmedchem.9b01340
CHEMBL3787034 139139 None 0 Human Binding pKi = 7.5 7.5 - 1
Displacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assayDisplacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assay
ChEMBL 353 3 1 6 4.3 CC1=C(C(=O)OC(C)C)C(c2ccsc2)n2c(nc3ccccc32)N1 10.1021/acs.jmedchem.9b01340
156017721 177844 None 0 Human Binding pKi = 7.5 7.5 - 1
Displacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting methodDisplacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting method
ChEMBL 338 3 1 7 3.3 CC1=C(C(=O)OC(C)C)C(c2cnoc2)n2c(nc3ccccc32)N1 10.1021/acs.jmedchem.0c00564
CHEMBL4644103 177844 None 0 Human Binding pKi = 7.5 7.5 - 1
Displacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting methodDisplacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting method
ChEMBL 338 3 1 7 3.3 CC1=C(C(=O)OC(C)C)C(c2cnoc2)n2c(nc3ccccc32)N1 10.1021/acs.jmedchem.0c00564
155524137 170882 None 0 Human Binding pKi = 7.5 7.5 - 1
Displacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assayDisplacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assay
ChEMBL 391 3 1 6 4.4 CC1=C(C(=O)OC(C)C(F)(F)F)C(c2ccco2)n2c(nc3ccccc32)N1 10.1021/acs.jmedchem.9b01340
CHEMBL4454378 170882 None 0 Human Binding pKi = 7.5 7.5 - 1
Displacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assayDisplacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assay
ChEMBL 391 3 1 6 4.4 CC1=C(C(=O)OC(C)C(F)(F)F)C(c2ccco2)n2c(nc3ccccc32)N1 10.1021/acs.jmedchem.9b01340
CHEMBL5082973 214834 None 0 Human Binding pKi = 7.5 7.5 -1 2
Displacement of [3H]DPCPX from human A2BAR expressed in HEK293 cell membrane incubated for 30 mins by microbeta trilux scintillation counter analysisDisplacement of [3H]DPCPX from human A2BAR expressed in HEK293 cell membrane incubated for 30 mins by microbeta trilux scintillation counter analysis
ChEMBL None None None N#Cc1c(-c2ccccc2)nc(Nc2ccccc2)nc1-c1cccnc1 10.1021/acs.jmedchem.1c01636
127033325 139004 None 0 Human Binding pKi = 7.5 7.5 - 1
Displacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting methodDisplacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting method
ChEMBL 339 3 1 6 4.0 CCOC(=O)C1=C(C)Nc2nc3ccccc3n2C1c1ccsc1 10.1021/acs.jmedchem.0c00564
CHEMBL3785618 139004 None 0 Human Binding pKi = 7.5 7.5 - 1
Displacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting methodDisplacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting method
ChEMBL 339 3 1 6 4.0 CCOC(=O)C1=C(C)Nc2nc3ccccc3n2C1c1ccsc1 10.1021/acs.jmedchem.0c00564
127033325 139004 None 0 Human Binding pKi = 7.5 7.5 - 1
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 minsDisplacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 mins
ChEMBL 339 3 1 6 4.0 CCOC(=O)C1=C(C)Nc2nc3ccccc3n2C1c1ccsc1 10.1021/acs.jmedchem.5b01586
CHEMBL3785618 139004 None 0 Human Binding pKi = 7.5 7.5 - 1
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 minsDisplacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 mins
ChEMBL 339 3 1 6 4.0 CCOC(=O)C1=C(C)Nc2nc3ccccc3n2C1c1ccsc1 10.1021/acs.jmedchem.5b01586
127033325 139004 None 0 Human Binding pKi = 7.5 7.5 - 1
Displacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assayDisplacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assay
ChEMBL 339 3 1 6 4.0 CCOC(=O)C1=C(C)Nc2nc3ccccc3n2C1c1ccsc1 10.1021/acs.jmedchem.9b01340
CHEMBL3785618 139004 None 0 Human Binding pKi = 7.5 7.5 - 1
Displacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assayDisplacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assay
ChEMBL 339 3 1 6 4.0 CCOC(=O)C1=C(C)Nc2nc3ccccc3n2C1c1ccsc1 10.1021/acs.jmedchem.9b01340
10046145 2683 None 18 Human Binding pKi = 5.5 5.5 -575 6
Inhibition of human recombinant adenosine receptor A2bInhibition of human recombinant adenosine receptor A2b
ChEMBL 394 7 1 8 1.1 OCCCn1c(=O)n(CC#C)c(=O)c2c1nc(n2C)/C=C/c1cccc(c1)OC 10.1021/jm4011669
5610 2683 None 18 Human Binding pKi = 5.5 5.5 -575 6
Inhibition of human recombinant adenosine receptor A2bInhibition of human recombinant adenosine receptor A2b
ChEMBL 394 7 1 8 1.1 OCCCn1c(=O)n(CC#C)c(=O)c2c1nc(n2C)/C=C/c1cccc(c1)OC 10.1021/jm4011669
CHEMBL413079 2683 None 18 Human Binding pKi = 5.5 5.5 -575 6
Inhibition of human recombinant adenosine receptor A2bInhibition of human recombinant adenosine receptor A2b
ChEMBL 394 7 1 8 1.1 OCCCn1c(=O)n(CC#C)c(=O)c2c1nc(n2C)/C=C/c1cccc(c1)OC 10.1021/jm4011669
52946159 19293 None 0 Human Binding pKi = 6.5 6.5 4 2
Displacement of [3H]ZM241385 from human adenosine A2B receptor transfected in CHO cells after 60 mins by scintillation countingDisplacement of [3H]ZM241385 from human adenosine A2B receptor transfected in CHO cells after 60 mins by scintillation counting
ChEMBL 493 9 2 4 5.7 O=C(CCc1ccccc1)NCc1ccc2[nH]c(=O)c(-c3nccs3)c(CCc3ccccc3)c2c1 10.1016/j.bmcl.2010.10.030
CHEMBL1290435 19293 None 0 Human Binding pKi = 6.5 6.5 4 2
Displacement of [3H]ZM241385 from human adenosine A2B receptor transfected in CHO cells after 60 mins by scintillation countingDisplacement of [3H]ZM241385 from human adenosine A2B receptor transfected in CHO cells after 60 mins by scintillation counting
ChEMBL 493 9 2 4 5.7 O=C(CCc1ccccc1)NCc1ccc2[nH]c(=O)c(-c3nccs3)c(CCc3ccccc3)c2c1 10.1016/j.bmcl.2010.10.030
11995649 141537 None 0 Human Binding pKi = 6.5 6.5 -2 2
Displacement of [125I]3-(4-aminobenzyl)-8-phenyloxyacetate-1-propyl-xanthine from human adenosine A2B receptor expressed in HEK cellsDisplacement of [125I]3-(4-aminobenzyl)-8-phenyloxyacetate-1-propyl-xanthine from human adenosine A2B receptor expressed in HEK cells
ChEMBL 473 8 1 8 1.9 CCCn1c(=O)c2nc([C@]34CC[C@](C(=O)N(C)CC(=O)OC)(CC3)CC4)[nH]c2n(CCC)c1=O 10.1021/jm0605381
CHEMBL384705 141537 None 0 Human Binding pKi = 6.5 6.5 -2 2
Displacement of [125I]3-(4-aminobenzyl)-8-phenyloxyacetate-1-propyl-xanthine from human adenosine A2B receptor expressed in HEK cellsDisplacement of [125I]3-(4-aminobenzyl)-8-phenyloxyacetate-1-propyl-xanthine from human adenosine A2B receptor expressed in HEK cells
ChEMBL 473 8 1 8 1.9 CCCn1c(=O)c2nc([C@]34CC[C@](C(=O)N(C)CC(=O)OC)(CC3)CC4)[nH]c2n(CCC)c1=O 10.1021/jm0605381
44417669 141653 None 0 Human Binding pKi = 6.5 6.5 -37 4
Displacement of [125I]3-(4-aminobenzyl)-8-phenyloxyacetate-1-propyl-xanthine from human adenosine A2B receptor expressed in HEK cellsDisplacement of [125I]3-(4-aminobenzyl)-8-phenyloxyacetate-1-propyl-xanthine from human adenosine A2B receptor expressed in HEK cells
ChEMBL 356 5 1 5 2.8 CCCn1c(=O)c2nc(C34CC5CC(C3)C(C5)C4)[nH]c2n(CCC)c1=O 10.1021/jm0605381
CHEMBL385372 141653 None 0 Human Binding pKi = 6.5 6.5 -37 4
Displacement of [125I]3-(4-aminobenzyl)-8-phenyloxyacetate-1-propyl-xanthine from human adenosine A2B receptor expressed in HEK cellsDisplacement of [125I]3-(4-aminobenzyl)-8-phenyloxyacetate-1-propyl-xanthine from human adenosine A2B receptor expressed in HEK cells
ChEMBL 356 5 1 5 2.8 CCCn1c(=O)c2nc(C34CC5CC(C3)C(C5)C4)[nH]c2n(CCC)c1=O 10.1021/jm0605381
11037972 57456 None 0 Human Binding pKi = 6.5 6.5 -25 4
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 261-336Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 261-336
ChEMBL 466 4 2 8 4.2 CCn1cc2c(nc(NC(=O)Nc3ccc(Br)cc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm0109614
CHEMBL165600 57456 None 0 Human Binding pKi = 6.5 6.5 -25 4
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 261-336Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 261-336
ChEMBL 466 4 2 8 4.2 CCn1cc2c(nc(NC(=O)Nc3ccc(Br)cc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm0109614
5604 3368 None 35 Human Binding pKi = 6.5 6.5 -1995 10
Displacement of [3H]PSB-603 from human adenosine receptor A2B expressed in CHO cell membranes incubated for 75 mins by radioligand competition assayDisplacement of [3H]PSB-603 from human adenosine receptor A2B expressed in CHO cell membranes incubated for 75 mins by radioligand competition assay
ChEMBL 356 5 1 5 2.8 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C12CC3CC2CC(C1)C3 10.1016/j.ejmech.2019.111879
64627 3368 None 35 Human Binding pKi = 6.5 6.5 -1995 10
Displacement of [3H]PSB-603 from human adenosine receptor A2B expressed in CHO cell membranes incubated for 75 mins by radioligand competition assayDisplacement of [3H]PSB-603 from human adenosine receptor A2B expressed in CHO cell membranes incubated for 75 mins by radioligand competition assay
ChEMBL 356 5 1 5 2.8 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C12CC3CC2CC(C1)C3 10.1016/j.ejmech.2019.111879
CHEMBL52333 3368 None 35 Human Binding pKi = 6.5 6.5 -1995 10
Displacement of [3H]PSB-603 from human adenosine receptor A2B expressed in CHO cell membranes incubated for 75 mins by radioligand competition assayDisplacement of [3H]PSB-603 from human adenosine receptor A2B expressed in CHO cell membranes incubated for 75 mins by radioligand competition assay
ChEMBL 356 5 1 5 2.8 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C12CC3CC2CC(C1)C3 10.1016/j.ejmech.2019.111879
DB05360 3368 None 35 Human Binding pKi = 6.5 6.5 -1995 10
Displacement of [3H]PSB-603 from human adenosine receptor A2B expressed in CHO cell membranes incubated for 75 mins by radioligand competition assayDisplacement of [3H]PSB-603 from human adenosine receptor A2B expressed in CHO cell membranes incubated for 75 mins by radioligand competition assay
ChEMBL 356 5 1 5 2.8 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C12CC3CC2CC(C1)C3 10.1016/j.ejmech.2019.111879
18171064 103850 None 3 Human Binding pKi = 5.5 5.5 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by Scatchard plot analysisDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by Scatchard plot analysis
ChEMBL 280 3 1 4 2.3 CCOC(=O)C1=C(C)N(C)C(=O)NC1c1ccsc1 10.1021/ml400185v
CHEMBL3091706 103850 None 3 Human Binding pKi = 5.5 5.5 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by Scatchard plot analysisDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by Scatchard plot analysis
ChEMBL 280 3 1 4 2.3 CCOC(=O)C1=C(C)N(C)C(=O)NC1c1ccsc1 10.1021/ml400185v
145979018 166622 None 0 Human Binding pKi = 6.5 6.5 -1 3
Displacement of [3H]PSB-602 from human adenosine A2B receptor expressed in CHO cell membranesDisplacement of [3H]PSB-602 from human adenosine A2B receptor expressed in CHO cell membranes
ChEMBL 609 15 1 11 2.2 CCCCn1c(=O)c2c(nc3n2CCCN3CCc2ccc(OCC(=O)NCCN3CCOCC3)cc2)n(CCCC)c1=O 10.1039/C8MD00070K
CHEMBL4280776 166622 None 0 Human Binding pKi = 6.5 6.5 -1 3
Displacement of [3H]PSB-602 from human adenosine A2B receptor expressed in CHO cell membranesDisplacement of [3H]PSB-602 from human adenosine A2B receptor expressed in CHO cell membranes
ChEMBL 609 15 1 11 2.2 CCCCn1c(=O)c2c(nc3n2CCCN3CCc2ccc(OCC(=O)NCCN3CCOCC3)cc2)n(CCCC)c1=O 10.1039/C8MD00070K
57429618 159078 None 0 Human Binding pKi = 8.5 8.5 - 1
Displacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 minsDisplacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 mins
ChEMBL 392 4 2 6 1.9 CCCn1c(=O)[nH]c2nc(-c3cnn(CC#Cc4cccc(F)c4)c3)[nH]c2c1=O 10.1016/j.ejmech.2017.04.014
CHEMBL4097296 159078 None 0 Human Binding pKi = 8.5 8.5 - 1
Displacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 minsDisplacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 mins
ChEMBL 392 4 2 6 1.9 CCCn1c(=O)[nH]c2nc(-c3cnn(CC#Cc4cccc(F)c4)c3)[nH]c2c1=O 10.1016/j.ejmech.2017.04.014
69029783 156327 None 0 Human Binding pKi = 8.5 8.5 3 2
Displacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting methodDisplacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting method
ChEMBL 570 9 1 8 4.2 CCCn1c(=O)c2[nH]c(-c3ccc(OCC4CC(=O)N(c5ccc(C(F)(F)F)cc5)C4)nc3)nc2n(CCC)c1=O 10.1016/j.ejmech.2016.11.007
CHEMBL4065717 156327 None 0 Human Binding pKi = 8.5 8.5 3 2
Displacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting methodDisplacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting method
ChEMBL 570 9 1 8 4.2 CCCn1c(=O)c2[nH]c(-c3ccc(OCC4CC(=O)N(c5ccc(C(F)(F)F)cc5)C4)nc3)nc2n(CCC)c1=O 10.1016/j.ejmech.2016.11.007
44446477 155559 None 0 Human Binding pKi = 8.5 8.5 331 2
Displacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranesDisplacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranes
ChEMBL 430 5 2 6 2.8 O=c1[nH]c2nc(-c3cnn(Cc4cccc(C(F)(F)F)c4)c3)[nH]c2c(=O)n1CC1CC1 10.1016/j.bmcl.2008.01.008
CHEMBL404349 155559 None 0 Human Binding pKi = 8.5 8.5 331 2
Displacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranesDisplacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranes
ChEMBL 430 5 2 6 2.8 O=c1[nH]c2nc(-c3cnn(Cc4cccc(C(F)(F)F)c4)c3)[nH]c2c(=O)n1CC1CC1 10.1016/j.bmcl.2008.01.008
44451330 96184 None 0 Human Binding pKi = 8.5 8.5 53 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 507 5 1 7 2.6 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCN(c5cccc(Cl)c5)CC4)cc3)cc2n(C)c1=O 10.1016/j.bmc.2008.01.002
CHEMBL260693 96184 None 0 Human Binding pKi = 8.5 8.5 53 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 507 5 1 7 2.6 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCN(c5cccc(Cl)c5)CC4)cc3)cc2n(C)c1=O 10.1016/j.bmc.2008.01.002
11952564 6046 None 0 Human Binding pKi = 8.5 8.5 26 3
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 279 2 2 5 2.0 O=c1[nH][nH]c2nc(-c3ccco3)c(-c3ccncn3)cc12 10.1016/j.bmcl.2010.01.077
CHEMBL1080497 6046 None 0 Human Binding pKi = 8.5 8.5 26 3
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 279 2 2 5 2.0 O=c1[nH][nH]c2nc(-c3ccco3)c(-c3ccncn3)cc12 10.1016/j.bmcl.2010.01.077
16072022 58013 None 0 Human Binding pKi = 8.5 8.5 5 4
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 320 4 1 5 3.5 O=C(Nc1cnc(-c2ccncc2)c(-c2ccco2)n1)C1CCC1 10.1021/ml100249e
CHEMBL1672615 58013 None 0 Human Binding pKi = 8.5 8.5 5 4
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 320 4 1 5 3.5 O=C(Nc1cnc(-c2ccncc2)c(-c2ccco2)n1)C1CCC1 10.1021/ml100249e
45271361 195369 None 0 Human Binding pKi = 8.5 8.5 6 4
Binding affinity to human adenosine A2b receptor expressed in HEK293 cellsBinding affinity to human adenosine A2b receptor expressed in HEK293 cells
ChEMBL 495 10 2 8 2.8 CCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(F)cc4)cc3)nc2n(CCCOC)c1=O 10.1016/j.bmc.2009.03.029
CHEMBL551904 195369 None 0 Human Binding pKi = 8.5 8.5 6 4
Binding affinity to human adenosine A2b receptor expressed in HEK293 cellsBinding affinity to human adenosine A2b receptor expressed in HEK293 cells
ChEMBL 495 10 2 8 2.8 CCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(F)cc4)cc3)nc2n(CCCOC)c1=O 10.1016/j.bmc.2009.03.029
45269707 196073 None 0 Human Binding pKi = 8.5 8.5 12 4
Binding affinity to human adenosine A2b receptor expressed in HEK293 cellsBinding affinity to human adenosine A2b receptor expressed in HEK293 cells
ChEMBL 477 10 2 8 2.6 CCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccccc4)cc3)nc2n(CCCOC)c1=O 10.1016/j.bmc.2009.03.029
CHEMBL560624 196073 None 0 Human Binding pKi = 8.5 8.5 12 4
Binding affinity to human adenosine A2b receptor expressed in HEK293 cellsBinding affinity to human adenosine A2b receptor expressed in HEK293 cells
ChEMBL 477 10 2 8 2.6 CCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccccc4)cc3)nc2n(CCCOC)c1=O 10.1016/j.bmc.2009.03.029
11568001 72630 None 0 Human Binding pKi = 8.5 8.5 3 4
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 422 5 2 6 2.4 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(F)cc4)cc3)cc2n(C)c1=O 10.1021/jm0506221
CHEMBL199446 72630 None 0 Human Binding pKi = 8.5 8.5 3 4
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 422 5 2 6 2.4 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(F)cc4)cc3)cc2n(C)c1=O 10.1021/jm0506221
44185936 185534 None 0 Human Binding pKi = 8.5 8.5 12 6
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 522 8 3 7 2.4 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)NC4CCN(Cc5ccccc5)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
CHEMBL486282 185534 None 0 Human Binding pKi = 8.5 8.5 12 6
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 522 8 3 7 2.4 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)NC4CCN(Cc5ccccc5)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
449 2643 None 52 Mouse Binding pKi = 8.5 8.5 -2 9
Displacement of [3H]PSB-603 from recombinant mouse A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant mouse A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins by liquid scintillation counting method
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10.1021/acs.jmedchem.9b00071
453 2643 None 52 Mouse Binding pKi = 8.5 8.5 -2 9
Displacement of [3H]PSB-603 from recombinant mouse A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant mouse A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins by liquid scintillation counting method
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10.1021/acs.jmedchem.9b00071
6603931 2643 None 52 Mouse Binding pKi = 8.5 8.5 -2 9
Displacement of [3H]PSB-603 from recombinant mouse A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant mouse A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins by liquid scintillation counting method
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10.1021/acs.jmedchem.9b00071
CHEMBL273807 2643 None 52 Mouse Binding pKi = 8.5 8.5 -2 9
Displacement of [3H]PSB-603 from recombinant mouse A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant mouse A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins by liquid scintillation counting method
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10.1021/acs.jmedchem.9b00071
11583705 73598 None 0 Human Binding pKi = 8.5 8.5 28 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 474 10 2 6 3.7 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)NCc4ccccc4)cc3)cc2n(CCC)c1=O 10.1021/jm0506221
CHEMBL201773 73598 None 0 Human Binding pKi = 8.5 8.5 28 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 474 10 2 6 3.7 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)NCc4ccccc4)cc3)cc2n(CCC)c1=O 10.1021/jm0506221
11503616 74696 None 0 Human Binding pKi = 8.5 8.5 41 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 463 8 2 8 2.5 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(OC)nc4)cc3)cc2n(C)c1=O 10.1021/jm0506221
CHEMBL203037 74696 None 0 Human Binding pKi = 8.5 8.5 41 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 463 8 2 8 2.5 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(OC)nc4)cc3)cc2n(C)c1=O 10.1021/jm0506221
9912816 98434 None 0 Human Binding pKi = 8.5 8.5 1 6
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 475 10 2 7 3.1 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)NCc4ccccc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm0506221
CHEMBL275605 98434 None 0 Human Binding pKi = 8.5 8.5 1 6
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 475 10 2 7 3.1 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)NCc4ccccc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm0506221
11511593 141151 None 0 Human Binding pKi = 8.5 8.5 10 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 494 9 2 6 4.6 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(Cl)cc4)cc3)cc2n(CCC)c1=O 10.1021/jm0506221
CHEMBL382764 141151 None 0 Human Binding pKi = 8.5 8.5 10 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 494 9 2 6 4.6 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(Cl)cc4)cc3)cc2n(CCC)c1=O 10.1021/jm0506221
44574168 178734 None 0 Human Binding pKi = 8.5 8.5 5 2
Displacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells by beta scintillation counterDisplacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells by beta scintillation counter
ChEMBL 394 4 2 7 2.6 Cn1c(=O)c2[nH]c(-c3ccc(COC(=O)Nc4ccco4)cc3)cc2n(C)c1=O 10.1016/j.bmc.2009.03.062
CHEMBL468506 178734 None 0 Human Binding pKi = 8.5 8.5 5 2
Displacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells by beta scintillation counterDisplacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells by beta scintillation counter
ChEMBL 394 4 2 7 2.6 Cn1c(=O)c2[nH]c(-c3ccc(COC(=O)Nc4ccco4)cc3)cc2n(C)c1=O 10.1016/j.bmc.2009.03.062
155531727 171666 None 0 Human Binding pKi = 8.5 8.5 - 1
Displacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 512 6 2 7 2.1 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(c5ccccc5F)CC4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
CHEMBL4466211 171666 None 0 Human Binding pKi = 8.5 8.5 - 1
Displacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 512 6 2 7 2.1 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(c5ccccc5F)CC4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
11627336 140373 None 0 Human Binding pKi = 8.5 8.5 18 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 492 9 2 6 4.5 CCCn1c(=O)c2[nH]c(-c3ccc(OC(C)C(=O)Nc4ccc(F)cc4)cc3)cc2n(CCC)c1=O 10.1021/jm0506221
CHEMBL380847 140373 None 0 Human Binding pKi = 8.5 8.5 18 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 492 9 2 6 4.5 CCCn1c(=O)c2[nH]c(-c3ccc(OC(C)C(=O)Nc4ccc(F)cc4)cc3)cc2n(CCC)c1=O 10.1021/jm0506221
168287172 191650 None 0 Human Binding pKi = 8.5 8.5 - 1
Displacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cell membrane preincubated for 4 hrs followed by [3H]PSB-603 addition and measured after 0.5 hrs by radioligand displacement assayDisplacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cell membrane preincubated for 4 hrs followed by [3H]PSB-603 addition and measured after 0.5 hrs by radioligand displacement assay
ChEMBL 369 6 1 7 3.1 CCCn1c(=O)c2[nH]c(-c3ccc(N=C=S)cc3)nc2n(CCC)c1=O 10.1039/d2md00132b
CHEMBL5196082 191650 None 0 Human Binding pKi = 8.5 8.5 - 1
Displacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cell membrane preincubated for 4 hrs followed by [3H]PSB-603 addition and measured after 0.5 hrs by radioligand displacement assayDisplacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cell membrane preincubated for 4 hrs followed by [3H]PSB-603 addition and measured after 0.5 hrs by radioligand displacement assay
ChEMBL 369 6 1 7 3.1 CCCn1c(=O)c2[nH]c(-c3ccc(N=C=S)cc3)nc2n(CCC)c1=O 10.1039/d2md00132b
145970075 164803 None 0 Human Binding pKi = 8.5 8.5 8 4
Displacement of [3H]PSB-603 from recombinant human adenosine A2B receptor expressed in CHO cell membranes after 75 mins by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human adenosine A2B receptor expressed in CHO cell membranes after 75 mins by liquid scintillation counting method
ChEMBL 475 11 3 6 3.0 CCCn1c(=O)[nH]c2nc(-c3ccc(OCC(=O)NCCCCc4ccccc4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.7b01627
CHEMBL4218460 164803 None 0 Human Binding pKi = 8.5 8.5 8 4
Displacement of [3H]PSB-603 from recombinant human adenosine A2B receptor expressed in CHO cell membranes after 75 mins by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human adenosine A2B receptor expressed in CHO cell membranes after 75 mins by liquid scintillation counting method
ChEMBL 475 11 3 6 3.0 CCCn1c(=O)[nH]c2nc(-c3ccc(OCC(=O)NCCCCc4ccccc4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.7b01627
11677313 73295 None 0 Human Binding pKi = 8.5 8.5 3 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 478 9 2 6 4.1 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(F)cc4)cc3)cc2n(CCC)c1=O 10.1021/jm0506221
CHEMBL201281 73295 None 0 Human Binding pKi = 8.5 8.5 3 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 478 9 2 6 4.1 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(F)cc4)cc3)cc2n(CCC)c1=O 10.1021/jm0506221
44451306 96265 None 0 Human Binding pKi = 8.5 8.5 117 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 507 5 1 7 2.6 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCN(c5ccc(Cl)cc5)CC4)cc3)cc2n(C)c1=O 10.1016/j.bmc.2008.01.002
CHEMBL261056 96265 None 0 Human Binding pKi = 8.5 8.5 117 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 507 5 1 7 2.6 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCN(c5ccc(Cl)cc5)CC4)cc3)cc2n(C)c1=O 10.1016/j.bmc.2008.01.002
449 2643 None 52 Mouse Binding pKi = 8.5 8.5 -2 9
Binding affinity to mouse adenosine A2B receptorBinding affinity to mouse adenosine A2B receptor
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10.1021/jm900413e
453 2643 None 52 Mouse Binding pKi = 8.5 8.5 -2 9
Binding affinity to mouse adenosine A2B receptorBinding affinity to mouse adenosine A2B receptor
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10.1021/jm900413e
6603931 2643 None 52 Mouse Binding pKi = 8.5 8.5 -2 9
Binding affinity to mouse adenosine A2B receptorBinding affinity to mouse adenosine A2B receptor
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10.1021/jm900413e
CHEMBL273807 2643 None 52 Mouse Binding pKi = 8.5 8.5 -2 9
Binding affinity to mouse adenosine A2B receptorBinding affinity to mouse adenosine A2B receptor
ChEMBL 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10.1021/jm900413e
11642035 73544 None 0 Human Binding pKi = 8.5 8.5 7 5
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 512 6 2 7 3.0 COc1cc(OCC(=O)Nc2ccc(Br)cc2)ccc1-c1cc2c([nH]1)c(=O)n(C)c(=O)n2C 10.1021/jm0506221
CHEMBL201750 73544 None 0 Human Binding pKi = 8.5 8.5 7 5
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 512 6 2 7 3.0 COc1cc(OCC(=O)Nc2ccc(Br)cc2)ccc1-c1cc2c([nH]1)c(=O)n(C)c(=O)n2C 10.1021/jm0506221
11642035 73544 None 0 Human Binding pKi = 8.5 8.5 7 5
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 512 6 2 7 3.0 COc1cc(OCC(=O)Nc2ccc(Br)cc2)ccc1-c1cc2c([nH]1)c(=O)n(C)c(=O)n2C 10.1016/j.bmc.2008.01.002
CHEMBL201750 73544 None 0 Human Binding pKi = 8.5 8.5 7 5
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 512 6 2 7 3.0 COc1cc(OCC(=O)Nc2ccc(Br)cc2)ccc1-c1cc2c([nH]1)c(=O)n(C)c(=O)n2C 10.1016/j.bmc.2008.01.002
44451305 160345 None 0 Human Binding pKi = 8.5 8.5 33 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 551 5 1 7 2.7 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCN(c5ccc(Br)cc5)CC4)cc3)cc2n(C)c1=O 10.1016/j.bmc.2008.01.002
CHEMBL411075 160345 None 0 Human Binding pKi = 8.5 8.5 33 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 551 5 1 7 2.7 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCN(c5ccc(Br)cc5)CC4)cc3)cc2n(C)c1=O 10.1016/j.bmc.2008.01.002
11223 2077 None 24 Human Binding pKi = 8.5 8.5 -1 4
Displacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting methodDisplacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting method
ChEMBL 337 3 1 6 3.9 CC(OC(=O)C1=C(C)Nc2n(C1c1ccco1)c1ccccc1n2)C 10.1021/acs.jmedchem.0c00564
17198004 2077 None 24 Human Binding pKi = 8.5 8.5 -1 4
Displacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting methodDisplacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting method
ChEMBL 337 3 1 6 3.9 CC(OC(=O)C1=C(C)Nc2n(C1c1ccco1)c1ccccc1n2)C 10.1021/acs.jmedchem.0c00564
CHEMBL3787197 2077 None 24 Human Binding pKi = 8.5 8.5 -1 4
Displacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting methodDisplacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting method
ChEMBL 337 3 1 6 3.9 CC(OC(=O)C1=C(C)Nc2n(C1c1ccco1)c1ccccc1n2)C 10.1021/acs.jmedchem.0c00564
11223 2077 None 24 Human Binding pKi = 8.5 8.5 -1 4
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 minsDisplacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 mins
ChEMBL 337 3 1 6 3.9 CC(OC(=O)C1=C(C)Nc2n(C1c1ccco1)c1ccccc1n2)C 10.1021/acs.jmedchem.5b01586
17198004 2077 None 24 Human Binding pKi = 8.5 8.5 -1 4
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 minsDisplacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 mins
ChEMBL 337 3 1 6 3.9 CC(OC(=O)C1=C(C)Nc2n(C1c1ccco1)c1ccccc1n2)C 10.1021/acs.jmedchem.5b01586
CHEMBL3787197 2077 None 24 Human Binding pKi = 8.5 8.5 -1 4
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 minsDisplacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 mins
ChEMBL 337 3 1 6 3.9 CC(OC(=O)C1=C(C)Nc2n(C1c1ccco1)c1ccccc1n2)C 10.1021/acs.jmedchem.5b01586
11223 2077 None 24 Human Binding pKi = 8.5 8.5 -1 4
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 337 3 1 6 3.9 CC(OC(=O)C1=C(C)Nc2n(C1c1ccco1)c1ccccc1n2)C 10.1021/acs.jmedchem.0c01431
17198004 2077 None 24 Human Binding pKi = 8.5 8.5 -1 4
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 337 3 1 6 3.9 CC(OC(=O)C1=C(C)Nc2n(C1c1ccco1)c1ccccc1n2)C 10.1021/acs.jmedchem.0c01431
CHEMBL3787197 2077 None 24 Human Binding pKi = 8.5 8.5 -1 4
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 337 3 1 6 3.9 CC(OC(=O)C1=C(C)Nc2n(C1c1ccco1)c1ccccc1n2)C 10.1021/acs.jmedchem.0c01431
11223 2077 None 24 Human Binding pKi = 8.5 8.5 -1 4
Displacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assayDisplacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assay
ChEMBL 337 3 1 6 3.9 CC(OC(=O)C1=C(C)Nc2n(C1c1ccco1)c1ccccc1n2)C 10.1021/acs.jmedchem.9b01340
17198004 2077 None 24 Human Binding pKi = 8.5 8.5 -1 4
Displacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assayDisplacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assay
ChEMBL 337 3 1 6 3.9 CC(OC(=O)C1=C(C)Nc2n(C1c1ccco1)c1ccccc1n2)C 10.1021/acs.jmedchem.9b01340
CHEMBL3787197 2077 None 24 Human Binding pKi = 8.5 8.5 -1 4
Displacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assayDisplacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assay
ChEMBL 337 3 1 6 3.9 CC(OC(=O)C1=C(C)Nc2n(C1c1ccco1)c1ccccc1n2)C 10.1021/acs.jmedchem.9b01340
57429605 157183 None 0 Human Binding pKi = 8.5 8.5 - 1
Displacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 minsDisplacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 mins
ChEMBL 488 8 1 9 2.8 CCCn1c(=O)c2[nH]c(-c3cnn(CC#Cc4ccc(C(=O)OCC)cc4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2017.04.014
CHEMBL4075650 157183 None 0 Human Binding pKi = 8.5 8.5 - 1
Displacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 minsDisplacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 mins
ChEMBL 488 8 1 9 2.8 CCCn1c(=O)c2[nH]c(-c3cnn(CC#Cc4ccc(C(=O)OCC)cc4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2017.04.014
16072020 58011 None 0 Human Binding pKi = 8.5 8.5 12 4
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 294 4 1 5 3.1 CCC(=O)Nc1cnc(-c2ccncc2)c(-c2ccco2)n1 10.1021/ml100249e
CHEMBL1672613 58011 None 0 Human Binding pKi = 8.5 8.5 12 4
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 294 4 1 5 3.1 CCC(=O)Nc1cnc(-c2ccncc2)c(-c2ccco2)n1 10.1021/ml100249e
136042339 71165 None 0 Human Binding pKi = 8.5 8.5 19 2
Displacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation countingDisplacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation counting
ChEMBL 483 8 2 9 3.5 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5cc(Cl)ccc5[nH]4)no3)nc2n(CCC)c1=O 10.1021/jm201292w
CHEMBL1955915 71165 None 0 Human Binding pKi = 8.5 8.5 19 2
Displacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation countingDisplacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation counting
ChEMBL 483 8 2 9 3.5 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5cc(Cl)ccc5[nH]4)no3)nc2n(CCC)c1=O 10.1021/jm201292w
11590411 169091 None 0 Human Binding pKi = 8.5 8.5 - 1
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 446 6 2 7 2.5 CC(=O)c1ccc(NC(=O)COc2ccc(-c3cc4c([nH]3)c(=O)n(C)c(=O)n4C)cc2)cc1 10.1021/jm0506221
CHEMBL439868 169091 None 0 Human Binding pKi = 8.5 8.5 - 1
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 446 6 2 7 2.5 CC(=O)c1ccc(NC(=O)COc2ccc(-c3cc4c([nH]3)c(=O)n(C)c(=O)n4C)cc2)cc1 10.1021/jm0506221
46837705 10624 None 0 Human Binding pKi = 8.5 8.5 -2 2
Displacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells after 30 minsDisplacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells after 30 mins
ChEMBL 496 7 3 5 3.9 CCCn1c(=O)[nH]c2cc(-c3ccc(OCC(=O)Nc4ccc(Br)cc4)cc3)[nH]c2c1=O 10.1016/j.ejmech.2010.03.011
CHEMBL1170167 10624 None 0 Human Binding pKi = 8.5 8.5 -2 2
Displacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells after 30 minsDisplacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells after 30 mins
ChEMBL 496 7 3 5 3.9 CCCn1c(=O)[nH]c2cc(-c3ccc(OCC(=O)Nc4ccc(Br)cc4)cc3)[nH]c2c1=O 10.1016/j.ejmech.2010.03.011
155549264 173820 None 0 Human Binding pKi = 8.5 8.5 26 2
Displacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 544 6 3 8 2.4 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(c5ccc(O)c(Cl)c5)CC4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
CHEMBL4538468 173820 None 0 Human Binding pKi = 8.5 8.5 26 2
Displacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 544 6 3 8 2.4 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(c5ccc(O)c(Cl)c5)CC4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
11605883 79952 None 6 Human Binding pKi = 8.4 8.4 42 6
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 508 7 2 7 2.0 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccccc5)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
CHEMBL212625 79952 None 6 Human Binding pKi = 8.4 8.4 42 6
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 508 7 2 7 2.0 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccccc5)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
57429602 157239 None 0 Human Binding pKi = 8.4 8.4 - 1
Displacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 minsDisplacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 mins
ChEMBL 500 7 1 8 3.5 CCCn1c(=O)c2[nH]c(-c3cnn(CC#Cc4cccc(OC(F)(F)F)c4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2017.04.014
CHEMBL4076435 157239 None 0 Human Binding pKi = 8.4 8.4 - 1
Displacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 minsDisplacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 mins
ChEMBL 500 7 1 8 3.5 CCCn1c(=O)c2[nH]c(-c3cnn(CC#Cc4cccc(OC(F)(F)F)c4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2017.04.014
57988777 157091 None 0 Human Binding pKi = 8.4 8.4 - 1
Displacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting methodDisplacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting method
ChEMBL 529 8 1 8 4.1 CCCn1c(=O)c2[nH]c(-c3cnn(CC4CCN(c5cccc(C(F)(F)F)c5)C4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2016.11.007
CHEMBL4074412 157091 None 0 Human Binding pKi = 8.4 8.4 - 1
Displacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting methodDisplacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting method
ChEMBL 529 8 1 8 4.1 CCCn1c(=O)c2[nH]c(-c3cnn(CC4CCN(c5cccc(C(F)(F)F)c5)C4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2016.11.007
50940969 57251 None 0 Human Binding pKi = 8.4 8.4 1 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in human HEK293 cells at 1 uM incubated for 30 mins by fluorescence polarization binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in human HEK293 cells at 1 uM incubated for 30 mins by fluorescence polarization binding assay
ChEMBL 363 6 1 5 4.2 CCC(=O)Nc1cc(-c2ccc(OC)cc2)nc(-c2ccc(OC)cc2)n1 10.1021/acsmedchemlett.1c00598
CHEMBL1650356 57251 None 0 Human Binding pKi = 8.4 8.4 1 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in human HEK293 cells at 1 uM incubated for 30 mins by fluorescence polarization binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in human HEK293 cells at 1 uM incubated for 30 mins by fluorescence polarization binding assay
ChEMBL 363 6 1 5 4.2 CCC(=O)Nc1cc(-c2ccc(OC)cc2)nc(-c2ccc(OC)cc2)n1 10.1021/acsmedchemlett.1c00598
11605883 79952 None 6 Human Binding pKi = 8.4 8.4 42 6
Displacement of [3H]PSB298 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB298 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 508 7 2 7 2.0 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccccc5)CC4)cc3)[nH]c2c1=O 10.1021/jm060277v
CHEMBL212625 79952 None 6 Human Binding pKi = 8.4 8.4 42 6
Displacement of [3H]PSB298 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB298 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 508 7 2 7 2.0 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccccc5)CC4)cc3)[nH]c2c1=O 10.1021/jm060277v
11525283 79665 None 0 Human Binding pKi = 8.4 8.4 2 5
Displacement of [3H]PSB298 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB298 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 453 8 3 6 2.0 CCCn1c(=O)[nH]c2[nH]c(-c3ccc(S(=O)(=O)NCCc4ccccc4)cc3)nc2c1=O 10.1021/jm060277v
CHEMBL211521 79665 None 0 Human Binding pKi = 8.4 8.4 2 5
Displacement of [3H]PSB298 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB298 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 453 8 3 6 2.0 CCCn1c(=O)[nH]c2[nH]c(-c3ccc(S(=O)(=O)NCCc4ccccc4)cc3)nc2c1=O 10.1021/jm060277v
44451303 169154 None 0 Human Binding pKi = 8.4 8.4 50 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 564 5 1 9 3.2 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCN(c5nc6cc(Cl)ccc6s5)CC4)cc3)cc2n(C)c1=O 10.1016/j.bmc.2008.01.002
CHEMBL440418 169154 None 0 Human Binding pKi = 8.4 8.4 50 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 564 5 1 9 3.2 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCN(c5nc6cc(Cl)ccc6s5)CC4)cc3)cc2n(C)c1=O 10.1016/j.bmc.2008.01.002
156019075 177881 None 0 Human Binding pKi = 8.4 8.4 - 1
Displacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting methodDisplacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting method
ChEMBL 324 3 1 7 2.9 CCOC(=O)C1=C(C)Nc2nc3ccccc3n2[C@@H]1c1cocn1 10.1021/acs.jmedchem.0c00564
CHEMBL4644677 177881 None 0 Human Binding pKi = 8.4 8.4 - 1
Displacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting methodDisplacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting method
ChEMBL 324 3 1 7 2.9 CCOC(=O)C1=C(C)Nc2nc3ccccc3n2[C@@H]1c1cocn1 10.1021/acs.jmedchem.0c00564
57429607 159742 None 0 Human Binding pKi = 8.4 8.4 - 1
Displacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 minsDisplacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 mins
ChEMBL 441 6 1 8 2.5 CCCn1c(=O)c2[nH]c(-c3cnn(CC#Cc4cccc(C#N)c4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2017.04.014
CHEMBL4104876 159742 None 0 Human Binding pKi = 8.4 8.4 - 1
Displacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 minsDisplacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 mins
ChEMBL 441 6 1 8 2.5 CCCn1c(=O)c2[nH]c(-c3cnn(CC#Cc4cccc(C#N)c4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2017.04.014
10926422 99644 None 0 Human Binding pKi = 8.4 8.4 4 4
Inhibition of [3H]ZM-241385 binding to human adenosine A2B receptorInhibition of [3H]ZM-241385 binding to human adenosine A2B receptor
ChEMBL 358 6 2 7 1.0 CCCn1c(=O)[nH]c2[nH]c(-c3ccc(OCC(=O)OC)cc3)nc2c1=O 10.1021/jm011049y
CHEMBL284288 99644 None 0 Human Binding pKi = 8.4 8.4 4 4
Inhibition of [3H]ZM-241385 binding to human adenosine A2B receptorInhibition of [3H]ZM-241385 binding to human adenosine A2B receptor
ChEMBL 358 6 2 7 1.0 CCCn1c(=O)[nH]c2[nH]c(-c3ccc(OCC(=O)OC)cc3)nc2c1=O 10.1021/jm011049y
456 349 None 59 Human Binding pKi = 8.4 8.4 15 3
Binding affinity towards human Adenosine A2b receptor expressed in HEK293 cells using 5 nM [3H]DPCPXBinding affinity towards human Adenosine A2b receptor expressed in HEK293 cells using 5 nM [3H]DPCPX
ChEMBL 214 0 2 4 0.2 O=c1[nH]c2nc3ccccc3nc2c(=O)[nH]1 10.1021/jm058018d
5372720 349 None 59 Human Binding pKi = 8.4 8.4 15 3
Binding affinity towards human Adenosine A2b receptor expressed in HEK293 cells using 5 nM [3H]DPCPXBinding affinity towards human Adenosine A2b receptor expressed in HEK293 cells using 5 nM [3H]DPCPX
ChEMBL 214 0 2 4 0.2 O=c1[nH]c2nc3ccccc3nc2c(=O)[nH]1 10.1021/jm058018d
CHEMBL68500 349 None 59 Human Binding pKi = 8.4 8.4 15 3
Binding affinity towards human Adenosine A2b receptor expressed in HEK293 cells using 5 nM [3H]DPCPXBinding affinity towards human Adenosine A2b receptor expressed in HEK293 cells using 5 nM [3H]DPCPX
ChEMBL 214 0 2 4 0.2 O=c1[nH]c2nc3ccccc3nc2c(=O)[nH]1 10.1021/jm058018d
11143648 154851 None 0 Human Binding pKi = 8.4 8.4 1 3
Inhibition of [3H]ZM-241385 binding to human adenosine A2B receptorInhibition of [3H]ZM-241385 binding to human adenosine A2B receptor
ChEMBL 390 5 1 5 3.1 CCCn1c(=O)c2nc(-c3ccc(Br)cc3)[nH]c2n(CCC)c1=O 10.1021/jm011049y
CHEMBL40055 154851 None 0 Human Binding pKi = 8.4 8.4 1 3
Inhibition of [3H]ZM-241385 binding to human adenosine A2B receptorInhibition of [3H]ZM-241385 binding to human adenosine A2B receptor
ChEMBL 390 5 1 5 3.1 CCCn1c(=O)c2nc(-c3ccc(Br)cc3)[nH]c2n(CCC)c1=O 10.1021/jm011049y
11640539 140899 None 0 Human Binding pKi = 8.4 8.4 -1 4
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 429 5 2 7 2.1 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(C#N)cc4)cc3)cc2n(C)c1=O 10.1021/jm0506221
CHEMBL382135 140899 None 0 Human Binding pKi = 8.4 8.4 -1 4
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 429 5 2 7 2.1 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(C#N)cc4)cc3)cc2n(C)c1=O 10.1021/jm0506221
11618962 72641 None 0 Human Binding pKi = 8.4 8.4 - 1
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 436 5 2 6 2.8 CC(Oc1ccc(-c2cc3c([nH]2)c(=O)n(C)c(=O)n3C)cc1)C(=O)Nc1ccc(F)cc1 10.1021/jm0506221
CHEMBL199486 72641 None 0 Human Binding pKi = 8.4 8.4 - 1
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 436 5 2 6 2.8 CC(Oc1ccc(-c2cc3c([nH]2)c(=O)n(C)c(=O)n3C)cc1)C(=O)Nc1ccc(F)cc1 10.1021/jm0506221
10917575 81144 None 0 Human Binding pKi = 7.5 7.5 -7 4
Displacement of [3H]- DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]- DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 463 5 1 11 2.9 CSc1c2c(nc(NC(=O)Cc3ccc4c(c3)OCO4)n3nc(-c4ccco4)nc23)nn1C 10.1021/jm021023m
CHEMBL21572 81144 None 0 Human Binding pKi = 7.5 7.5 -7 4
Displacement of [3H]- DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]- DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 463 5 1 11 2.9 CSc1c2c(nc(NC(=O)Cc3ccc4c(c3)OCO4)n3nc(-c4ccco4)nc23)nn1C 10.1021/jm021023m
21958745 94731 None 0 Human Binding pKi = 7.5 7.5 - 1
Displacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranesDisplacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranes
ChEMBL 432 6 2 6 3.1 CCCCn1c(=O)[nH]c2nc(-c3cnn(Cc4cccc(C(F)(F)F)c4)c3)[nH]c2c1=O 10.1016/j.bmcl.2008.01.008
CHEMBL253049 94731 None 0 Human Binding pKi = 7.5 7.5 - 1
Displacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranesDisplacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranes
ChEMBL 432 6 2 6 3.1 CCCCn1c(=O)[nH]c2nc(-c3cnn(Cc4cccc(C(F)(F)F)c4)c3)[nH]c2c1=O 10.1016/j.bmcl.2008.01.008
10225178 32937 None 0 Human Binding pKi = 7.5 7.5 -5 4
Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 23-40Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 23-40
ChEMBL 438 3 2 6 5.5 O=C(Nc1cccc(Cl)c1)Nc1nc2ccc(Cl)cc2c2nc(-c3ccco3)nn12 10.1021/jm001047y
CHEMBL141550 32937 None 0 Human Binding pKi = 7.5 7.5 -5 4
Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 23-40Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 23-40
ChEMBL 438 3 2 6 5.5 O=C(Nc1cccc(Cl)c1)Nc1nc2ccc(Cl)cc2c2nc(-c3ccco3)nn12 10.1021/jm001047y
10225178 32937 None 0 Human Binding pKi = 7.5 7.5 -5 4
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells
ChEMBL 438 3 2 6 5.5 O=C(Nc1cccc(Cl)c1)Nc1nc2ccc(Cl)cc2c2nc(-c3ccco3)nn12 10.1021/jm0109614
CHEMBL141550 32937 None 0 Human Binding pKi = 7.5 7.5 -5 4
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells
ChEMBL 438 3 2 6 5.5 O=C(Nc1cccc(Cl)c1)Nc1nc2ccc(Cl)cc2c2nc(-c3ccco3)nn12 10.1021/jm0109614
11762982 26205 None 0 Human Binding pKi = 7.5 7.5 1 4
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 513 7 1 8 5.3 O=C(Cc1cccc2ccccc12)Nc1nc2nn(CCc3ccccc3)cc2c2nc(-c3ccco3)nn12 10.1021/jm030852k
CHEMBL135719 26205 None 0 Human Binding pKi = 7.5 7.5 1 4
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 513 7 1 8 5.3 O=C(Cc1cccc2ccccc12)Nc1nc2nn(CCc3ccccc3)cc2c2nc(-c3ccco3)nn12 10.1021/jm030852k
46880470 6076 None 0 Human Binding pKi = 7.5 7.5 20 3
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 306 4 1 5 3.1 O=C(Nc1ccc(-c2ccncc2)c(-c2cnco2)n1)C1CC1 10.1016/j.bmcl.2010.01.045
CHEMBL1080676 6076 None 0 Human Binding pKi = 7.5 7.5 20 3
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 306 4 1 5 3.1 O=C(Nc1ccc(-c2ccncc2)c(-c2cnco2)n1)C1CC1 10.1016/j.bmcl.2010.01.045
46880506 6385 None 0 Human Binding pKi = 7.5 7.5 1 4
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 307 3 1 3 3.9 CC(=O)Nc1ccc(-c2ccncc2)c(-c2cccc(F)c2)n1 10.1016/j.bmcl.2010.01.045
CHEMBL1082208 6385 None 0 Human Binding pKi = 7.5 7.5 1 4
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 307 3 1 3 3.9 CC(=O)Nc1ccc(-c2ccncc2)c(-c2cccc(F)c2)n1 10.1016/j.bmcl.2010.01.045
136042349 71149 None 0 Human Binding pKi = 7.5 7.5 21 2
Displacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation countingDisplacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation counting
ChEMBL 480 8 2 9 2.7 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5cc(F)ccc5[nH]4)nn3C)nc2n(CCC)c1=O 10.1021/jm201292w
CHEMBL1955898 71149 None 0 Human Binding pKi = 7.5 7.5 21 2
Displacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation countingDisplacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation counting
ChEMBL 480 8 2 9 2.7 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5cc(F)ccc5[nH]4)nn3C)nc2n(CCC)c1=O 10.1021/jm201292w
2690 903 None 66 Human Binding pKi = 7.5 7.5 -30 9
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 285 1 1 6 2.8 Clc1ccc2c(c1)c1nc(nn1c(n2)N)c1ccco1 10.1021/jm900413e
384 903 None 66 Human Binding pKi = 7.5 7.5 -30 9
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 285 1 1 6 2.8 Clc1ccc2c(c1)c1nc(nn1c(n2)N)c1ccco1 10.1021/jm900413e
CHEMBL16687 903 None 66 Human Binding pKi = 7.5 7.5 -30 9
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 285 1 1 6 2.8 Clc1ccc2c(c1)c1nc(nn1c(n2)N)c1ccco1 10.1021/jm900413e
21958724 96201 None 0 Human Binding pKi = 7.5 7.5 8 3
Displacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 378 6 1 7 2.1 CCCCn1c(=O)c2[nH]c(-c3cnn(Cc4ccccc4)c3)nc2n(C)c1=O 10.1021/jm7014815
CHEMBL260763 96201 None 0 Human Binding pKi = 7.5 7.5 8 3
Displacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 378 6 1 7 2.1 CCCCn1c(=O)c2[nH]c(-c3cnn(Cc4ccccc4)c3)nc2n(C)c1=O 10.1021/jm7014815
176407 4148 None 84 Human Binding pKi = 7.5 7.5 -34 6
Selectivity for recombinant human adenosine A2b receptorSelectivity for recombinant human adenosine A2b receptor
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1021/jm0498405
405 4148 None 84 Human Binding pKi = 7.5 7.5 -34 6
Selectivity for recombinant human adenosine A2b receptorSelectivity for recombinant human adenosine A2b receptor
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1021/jm0498405
CHEMBL113142 4148 None 84 Human Binding pKi = 7.5 7.5 -34 6
Selectivity for recombinant human adenosine A2b receptorSelectivity for recombinant human adenosine A2b receptor
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1021/jm0498405
DB08770 4148 None 84 Human Binding pKi = 7.5 7.5 -34 6
Selectivity for recombinant human adenosine A2b receptorSelectivity for recombinant human adenosine A2b receptor
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1021/jm0498405
44450903 96096 None 0 Human Binding pKi = 7.5 7.5 28 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 532 7 1 8 3.0 COc1ccc(C2CCN(C(=O)COc3ccc(-c4cc5c([nH]4)c(=O)n(C)c(=O)n5C)cc3OC)CC2)cc1 10.1016/j.bmc.2008.01.002
CHEMBL260179 96096 None 0 Human Binding pKi = 7.5 7.5 28 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 532 7 1 8 3.0 COc1ccc(C2CCN(C(=O)COc3ccc(-c4cc5c([nH]4)c(=O)n(C)c(=O)n5C)cc3OC)CC2)cc1 10.1016/j.bmc.2008.01.002
46837839 10756 None 0 Human Binding pKi = 7.5 7.5 - 1
Displacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells after 30 minsDisplacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells after 30 mins
ChEMBL 464 7 1 7 3.3 CCCn1c(=O)c2c(cc(-c3ccc(OCC(=O)Nc4ccc(F)cc4)cc3)n2C)n(C)c1=O 10.1016/j.ejmech.2010.03.011
CHEMBL1171380 10756 None 0 Human Binding pKi = 7.5 7.5 - 1
Displacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells after 30 minsDisplacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells after 30 mins
ChEMBL 464 7 1 7 3.3 CCCn1c(=O)c2c(cc(-c3ccc(OCC(=O)Nc4ccc(F)cc4)cc3)n2C)n(C)c1=O 10.1016/j.ejmech.2010.03.011
16109435 2379 None 10 Human Binding pKi = 6.5 6.5 -338 4
Displacement of [3H]MRS1754 from human adenosine A2B receptorDisplacement of [3H]MRS1754 from human adenosine A2B receptor
ChEMBL 353 3 1 2 6.3 C1CCC(CC1)c1nc2c([nH]1)nc(cc2c1ccccc1)c1ccccc1 10.1021/jm0607956
5607 2379 None 10 Human Binding pKi = 6.5 6.5 -338 4
Displacement of [3H]MRS1754 from human adenosine A2B receptorDisplacement of [3H]MRS1754 from human adenosine A2B receptor
ChEMBL 353 3 1 2 6.3 C1CCC(CC1)c1nc2c([nH]1)nc(cc2c1ccccc1)c1ccccc1 10.1021/jm0607956
CHEMBL219160 2379 None 10 Human Binding pKi = 6.5 6.5 -338 4
Displacement of [3H]MRS1754 from human adenosine A2B receptorDisplacement of [3H]MRS1754 from human adenosine A2B receptor
ChEMBL 353 3 1 2 6.3 C1CCC(CC1)c1nc2c([nH]1)nc(cc2c1ccccc1)c1ccccc1 10.1021/jm0607956
16109430 83420 None 1 Human Binding pKi = 6.5 6.5 -489 3
Displacement of [3H]MRS1754 from human adenosine A2B receptorDisplacement of [3H]MRS1754 from human adenosine A2B receptor
ChEMBL 339 3 1 2 6.0 c1ccc(-c2cc(-c3ccccc3)c3nc(C4CCCC4)[nH]c3n2)cc1 10.1021/jm0607956
CHEMBL219625 83420 None 1 Human Binding pKi = 6.5 6.5 -489 3
Displacement of [3H]MRS1754 from human adenosine A2B receptorDisplacement of [3H]MRS1754 from human adenosine A2B receptor
ChEMBL 339 3 1 2 6.0 c1ccc(-c2cc(-c3ccccc3)c3nc(C4CCCC4)[nH]c3n2)cc1 10.1021/jm0607956
16109428 84280 None 1 Human Binding pKi = 6.5 6.5 -489 4
Displacement of [3H]MRS1754 from human adenosine A2B receptorDisplacement of [3H]MRS1754 from human adenosine A2B receptor
ChEMBL 313 3 1 2 5.4 CC(C)c1nc2c(-c3ccccc3)cc(-c3ccccc3)nc2[nH]1 10.1021/jm0607956
CHEMBL221343 84280 None 1 Human Binding pKi = 6.5 6.5 -489 4
Displacement of [3H]MRS1754 from human adenosine A2B receptorDisplacement of [3H]MRS1754 from human adenosine A2B receptor
ChEMBL 313 3 1 2 5.4 CC(C)c1nc2c(-c3ccccc3)cc(-c3ccccc3)nc2[nH]1 10.1021/jm0607956
44418996 84305 None 1 Human Binding pKi = 6.5 6.5 -549 4
Displacement of [3H]MRS1754 from human adenosine A2B receptorDisplacement of [3H]MRS1754 from human adenosine A2B receptor
ChEMBL 327 4 1 2 5.5 CC(C)Cc1nc2c(-c3ccccc3)cc(-c3ccccc3)nc2[nH]1 10.1021/jm0607956
CHEMBL221486 84305 None 1 Human Binding pKi = 6.5 6.5 -549 4
Displacement of [3H]MRS1754 from human adenosine A2B receptorDisplacement of [3H]MRS1754 from human adenosine A2B receptor
ChEMBL 327 4 1 2 5.5 CC(C)Cc1nc2c(-c3ccccc3)cc(-c3ccccc3)nc2[nH]1 10.1021/jm0607956
16109429 141608 None 1 Human Binding pKi = 6.5 6.5 -346 4
Displacement of [3H]MRS1754 from human adenosine A2B receptorDisplacement of [3H]MRS1754 from human adenosine A2B receptor
ChEMBL 341 5 1 2 6.2 CCC(CC)c1nc2c(-c3ccccc3)cc(-c3ccccc3)nc2[nH]1 10.1021/jm0607956
CHEMBL385109 141608 None 1 Human Binding pKi = 6.5 6.5 -346 4
Displacement of [3H]MRS1754 from human adenosine A2B receptorDisplacement of [3H]MRS1754 from human adenosine A2B receptor
ChEMBL 341 5 1 2 6.2 CCC(CC)c1nc2c(-c3ccccc3)cc(-c3ccccc3)nc2[nH]1 10.1021/jm0607956
11533237 77696 None 0 Human Binding pKi = 6.5 6.5 10 3
Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cellsDisplacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells
ChEMBL 488 7 1 7 4.1 CC(C)Cn1c(=O)c2nc(-c3cnn(Cc4cccc(C(F)(F)F)c4)c3)[nH]c2n(CC(C)C)c1=O 10.1021/jm051268+
CHEMBL208920 77696 None 0 Human Binding pKi = 6.5 6.5 10 3
Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cellsDisplacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells
ChEMBL 488 7 1 7 4.1 CC(C)Cn1c(=O)c2nc(-c3cnn(Cc4cccc(C(F)(F)F)c4)c3)[nH]c2n(CC(C)C)c1=O 10.1021/jm051268+
135401232 3206 None 5 Human Binding pKi = 4.5 4.5 -24547 7
Displacement of [3H]PSB-603 from human adenosine receptor A2B expressed in CHO cell membranes incubated for 75 mins by radioligand competition assayDisplacement of [3H]PSB-603 from human adenosine receptor A2B expressed in CHO cell membranes incubated for 75 mins by radioligand competition assay
ChEMBL 397 2 1 3 4.4 CC[C@H]1N=c2n(C1)c(=O)n(c1c2[nH]c(n1)c1cc(Cl)cc(c1Cl)Cl)C 10.1016/j.ejmech.2019.111879
5619 3206 None 5 Human Binding pKi = 4.5 4.5 -24547 7
Displacement of [3H]PSB-603 from human adenosine receptor A2B expressed in CHO cell membranes incubated for 75 mins by radioligand competition assayDisplacement of [3H]PSB-603 from human adenosine receptor A2B expressed in CHO cell membranes incubated for 75 mins by radioligand competition assay
ChEMBL 397 2 1 3 4.4 CC[C@H]1N=c2n(C1)c(=O)n(c1c2[nH]c(n1)c1cc(Cl)cc(c1Cl)Cl)C 10.1016/j.ejmech.2019.111879
CHEMBL1562432 3206 None 5 Human Binding pKi = 4.5 4.5 -24547 7
Displacement of [3H]PSB-603 from human adenosine receptor A2B expressed in CHO cell membranes incubated for 75 mins by radioligand competition assayDisplacement of [3H]PSB-603 from human adenosine receptor A2B expressed in CHO cell membranes incubated for 75 mins by radioligand competition assay
ChEMBL 397 2 1 3 4.4 CC[C@H]1N=c2n(C1)c(=O)n(c1c2[nH]c(n1)c1cc(Cl)cc(c1Cl)Cl)C 10.1016/j.ejmech.2019.111879
2519 779 None 86 Rat Binding pKi = 4.5 4.5 -47 12
Displacement of [3H]PSB-603 from recombinant rat adenosine A2B receptor expressed in CHO cell membranes after 75 mins by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant rat adenosine A2B receptor expressed in CHO cell membranes after 75 mins by liquid scintillation counting method
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1021/acs.jmedchem.7b01627
2519.0 779 None 86 Rat Binding pKi = 4.5 4.5 -47 12
Displacement of [3H]PSB-603 from recombinant rat adenosine A2B receptor expressed in CHO cell membranes after 75 mins by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant rat adenosine A2B receptor expressed in CHO cell membranes after 75 mins by liquid scintillation counting method
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1021/acs.jmedchem.7b01627
407 779 None 86 Rat Binding pKi = 4.5 4.5 -47 12
Displacement of [3H]PSB-603 from recombinant rat adenosine A2B receptor expressed in CHO cell membranes after 75 mins by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant rat adenosine A2B receptor expressed in CHO cell membranes after 75 mins by liquid scintillation counting method
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1021/acs.jmedchem.7b01627
463 779 None 86 Rat Binding pKi = 4.5 4.5 -47 12
Displacement of [3H]PSB-603 from recombinant rat adenosine A2B receptor expressed in CHO cell membranes after 75 mins by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant rat adenosine A2B receptor expressed in CHO cell membranes after 75 mins by liquid scintillation counting method
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1021/acs.jmedchem.7b01627
CHEMBL113 779 None 86 Rat Binding pKi = 4.5 4.5 -47 12
Displacement of [3H]PSB-603 from recombinant rat adenosine A2B receptor expressed in CHO cell membranes after 75 mins by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant rat adenosine A2B receptor expressed in CHO cell membranes after 75 mins by liquid scintillation counting method
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1021/acs.jmedchem.7b01627
DB00201 779 None 86 Rat Binding pKi = 4.5 4.5 -47 12
Displacement of [3H]PSB-603 from recombinant rat adenosine A2B receptor expressed in CHO cell membranes after 75 mins by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant rat adenosine A2B receptor expressed in CHO cell membranes after 75 mins by liquid scintillation counting method
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1021/acs.jmedchem.7b01627
10457445 103193 None 0 Rat Binding pKi = 6.5 6.5 -93 3
Compound was tested for its binding affinity against Alpha-2 adrenergic receptorCompound was tested for its binding affinity against Alpha-2 adrenergic receptor
ChEMBL 470 14 4 6 5.0 CCCN(CCCCCCN1CCC[C@@H]1Cc1ccc(O)c(O)c1)CCc1ccc(O)c(O)c1 10.1016/0960-894X(95)00413-N
CHEMBL308295 103193 None 0 Rat Binding pKi = 6.5 6.5 -93 3
Compound was tested for its binding affinity against Alpha-2 adrenergic receptorCompound was tested for its binding affinity against Alpha-2 adrenergic receptor
ChEMBL 470 14 4 6 5.0 CCCN(CCCCCCN1CCC[C@@H]1Cc1ccc(O)c(O)c1)CCc1ccc(O)c(O)c1 10.1016/0960-894X(95)00413-N
10905184 120140 None 0 Human Binding pKi = 6.5 6.5 -30 4
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 244-373Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 244-373
ChEMBL 388 3 2 8 3.2 Cc1ccc(NC(=O)Nc2nc3nn(C)cc3c3nc(-c4ccco4)nn23)cc1 10.1021/jm0109614
CHEMBL351285 120140 None 0 Human Binding pKi = 6.5 6.5 -30 4
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 244-373Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 244-373
ChEMBL 388 3 2 8 3.2 Cc1ccc(NC(=O)Nc2nc3nn(C)cc3c3nc(-c4ccco4)nn23)cc1 10.1021/jm0109614
50940966 57284 None 0 Human Binding pKi = 6.5 6.5 -30 3
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 269 3 1 5 3.0 CC(=O)Nc1cc(-c2ccoc2)nc(-c2ccoc2)n1 10.1021/jm100843z
CHEMBL1650390 57284 None 0 Human Binding pKi = 6.5 6.5 -30 3
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 269 3 1 5 3.0 CC(=O)Nc1cc(-c2ccoc2)nc(-c2ccoc2)n1 10.1021/jm100843z
71680734 90213 None 0 Human Binding pKi = 6.5 6.5 -13 6
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells after 75 mins by liquid scintillation counting analysisDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells after 75 mins by liquid scintillation counting analysis
ChEMBL 354 6 1 5 3.6 COc1cccc(CCCC(=O)Nc2nc3ccccc3c(=O)s2)c1 10.1021/jm400336x
CHEMBL2382435 90213 None 0 Human Binding pKi = 6.5 6.5 -13 6
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells after 75 mins by liquid scintillation counting analysisDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells after 75 mins by liquid scintillation counting analysis
ChEMBL 354 6 1 5 3.6 COc1cccc(CCCC(=O)Nc2nc3ccccc3c(=O)s2)c1 10.1021/jm400336x
135486118 111357 None 0 Human Binding pKi = 6.5 6.5 1 2
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 511 9 2 9 2.8 CC(C)Cn1c(=O)c2nc(-c3cc(OCC(=O)Nc4ccc(F)cc4)nn3C)[nH]c2n(CC(C)C)c1=O 10.1021/jm0309654
CHEMBL32697 111357 None 0 Human Binding pKi = 6.5 6.5 1 2
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 511 9 2 9 2.8 CC(C)Cn1c(=O)c2nc(-c3cc(OCC(=O)Nc4ccc(F)cc4)nn3C)[nH]c2n(CC(C)C)c1=O 10.1021/jm0309654
10623248 112640 None 0 Human Binding pKi = 6.5 6.5 -29 4
Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 260-352Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 260-352
ChEMBL 446 7 2 9 4.2 CCCCn1cc2c(nc(NC(=O)Nc3ccc(OC)cc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm001047y
CHEMBL330286 112640 None 0 Human Binding pKi = 6.5 6.5 -29 4
Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 260-352Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 260-352
ChEMBL 446 7 2 9 4.2 CCCCn1cc2c(nc(NC(=O)Nc3ccc(OC)cc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm001047y
10623248 112640 None 0 Human Binding pKi = 6.5 6.5 -29 4
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells
ChEMBL 446 7 2 9 4.2 CCCCn1cc2c(nc(NC(=O)Nc3ccc(OC)cc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm010818a
CHEMBL330286 112640 None 0 Human Binding pKi = 6.5 6.5 -29 4
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells
ChEMBL 446 7 2 9 4.2 CCCCn1cc2c(nc(NC(=O)Nc3ccc(OC)cc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm010818a
10623248 112640 None 0 Human Binding pKi = 6.5 6.5 -29 4
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 262-352Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 262-352
ChEMBL 446 7 2 9 4.2 CCCCn1cc2c(nc(NC(=O)Nc3ccc(OC)cc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm0109614
CHEMBL330286 112640 None 0 Human Binding pKi = 6.5 6.5 -29 4
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 262-352Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 262-352
ChEMBL 446 7 2 9 4.2 CCCCn1cc2c(nc(NC(=O)Nc3ccc(OC)cc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm0109614
155522786 170752 None 0 Human Binding pKi = 6.5 6.5 - 1
Displacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assayDisplacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assay
ChEMBL 318 3 2 4 2.4 CC1=C(C(=O)OC(C)C(F)(F)F)C(c2ccco2)NC(=O)N1 10.1021/acs.jmedchem.9b01340
CHEMBL4452495 170752 None 0 Human Binding pKi = 6.5 6.5 - 1
Displacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assayDisplacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assay
ChEMBL 318 3 2 4 2.4 CC1=C(C(=O)OC(C)C(F)(F)F)C(c2ccco2)NC(=O)N1 10.1021/acs.jmedchem.9b01340
10884803 120783 None 0 Human Binding pKi = 6.5 6.5 -11 4
Displacement of [3H]DPCPX binding at human Adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX binding at human Adenosine A2B receptor expressed in HEK293 cells
ChEMBL 447 6 2 10 3.7 CCCn1cc2c(nc(NC(=O)Nc3ccc([N+](=O)[O-])cc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm0109614
CHEMBL355415 120783 None 0 Human Binding pKi = 6.5 6.5 -11 4
Displacement of [3H]DPCPX binding at human Adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX binding at human Adenosine A2B receptor expressed in HEK293 cells
ChEMBL 447 6 2 10 3.7 CCCn1cc2c(nc(NC(=O)Nc3ccc([N+](=O)[O-])cc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm0109614
145991489 166840 None 0 Human Binding pKi = 6.5 6.5 -2 4
Displacement of [3H]PSB-602 from human adenosine A2B receptor expressed in CHO cell membranesDisplacement of [3H]PSB-602 from human adenosine A2B receptor expressed in CHO cell membranes
ChEMBL 607 15 2 10 3.4 CCCn1c(=O)c2c(nc3n2CCCN3CCc2ccc(OCC(=O)NCCCNC3CCCCC3)cc2)n(CCC)c1=O 10.1039/C8MD00070K
CHEMBL4285218 166840 None 0 Human Binding pKi = 6.5 6.5 -2 4
Displacement of [3H]PSB-602 from human adenosine A2B receptor expressed in CHO cell membranesDisplacement of [3H]PSB-602 from human adenosine A2B receptor expressed in CHO cell membranes
ChEMBL 607 15 2 10 3.4 CCCn1c(=O)c2c(nc3n2CCCN3CCc2ccc(OCC(=O)NCCCNC3CCCCC3)cc2)n(CCC)c1=O 10.1039/C8MD00070K
162665544 182263 None 0 Human Binding pKi = 6.5 6.5 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 276 3 2 4 2.0 CC1=C(C(=O)OC2CCC2)C(c2ccoc2)NC(=O)N1 10.1021/acs.jmedchem.0c01431
CHEMBL4783746 182263 None 0 Human Binding pKi = 6.5 6.5 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 276 3 2 4 2.0 CC1=C(C(=O)OC2CCC2)C(c2ccoc2)NC(=O)N1 10.1021/acs.jmedchem.0c01431
50940926 57234 None 0 Human Binding pKi = 6.5 6.5 -6 4
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 339 4 1 3 4.4 CCC(=O)Nc1nc(-c2ccccc2F)cc(-c2ccccc2F)n1 10.1021/jm100843z
CHEMBL1650164 57234 None 0 Human Binding pKi = 6.5 6.5 -6 4
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 339 4 1 3 4.4 CCC(=O)Nc1nc(-c2ccccc2F)cc(-c2ccccc2F)n1 10.1021/jm100843z
10884000 75547 None 0 Human Binding pKi = 7.5 7.5 -1 3
Displacement of [3H]- DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]- DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 405 6 1 9 3.7 CSc1c2c(nc(N)n3nc(-c4ccco4)nc23)nn1CCCc1ccccc1 10.1021/jm021023m
CHEMBL20445 75547 None 0 Human Binding pKi = 7.5 7.5 -1 3
Displacement of [3H]- DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]- DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 405 6 1 9 3.7 CSc1c2c(nc(N)n3nc(-c4ccco4)nc23)nn1CCCc1ccccc1 10.1021/jm021023m
11081189 120375 None 0 Human Binding pKi = 7.5 7.5 2 4
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 25-40Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 25-40
ChEMBL 470 5 2 8 5.1 CCCn1cc2c(nc(NC(=O)Nc3ccc(Cl)c(Cl)c3)n3nc(-c4ccco4)nc23)n1 10.1021/jm0109614
CHEMBL353299 120375 None 0 Human Binding pKi = 7.5 7.5 2 4
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 25-40Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 25-40
ChEMBL 470 5 2 8 5.1 CCCn1cc2c(nc(NC(=O)Nc3ccc(Cl)c(Cl)c3)n3nc(-c4ccco4)nc23)n1 10.1021/jm0109614
11080491 22796 None 0 Human Binding pKi = 7.5 7.5 1 4
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 429 7 1 8 4.0 CC(C)CCn1cc2c(nc(NC(=O)Cc3ccccc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm030852k
CHEMBL132806 22796 None 0 Human Binding pKi = 7.5 7.5 1 4
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 429 7 1 8 4.0 CC(C)CCn1cc2c(nc(NC(=O)Cc3ccccc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm030852k
21916357 96393 None 0 Human Binding pKi = 7.5 7.5 10 4
Displacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 410 6 1 7 2.6 CCn1c(=O)n(CC(C)C)c(=O)c2[nH]c(-c3cnn(Cc4cccc(F)c4)c3)nc21 10.1021/jm7014815
CHEMBL261819 96393 None 0 Human Binding pKi = 7.5 7.5 10 4
Displacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 410 6 1 7 2.6 CCn1c(=O)n(CC(C)C)c(=O)c2[nH]c(-c3cnn(Cc4cccc(F)c4)c3)nc21 10.1021/jm7014815
21958764 96834 None 0 Human Binding pKi = 7.5 7.5 8 3
Displacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 378 6 1 7 2.2 CCCn1c(=O)c2[nH]c(-c3cnn(Cc4ccccc4)c3)nc2n(CC)c1=O 10.1021/jm7014815
CHEMBL265212 96834 None 0 Human Binding pKi = 7.5 7.5 8 3
Displacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 378 6 1 7 2.2 CCCn1c(=O)c2[nH]c(-c3cnn(Cc4ccccc4)c3)nc2n(CC)c1=O 10.1021/jm7014815
CHEMBL5086406 215027 None 3 Human Binding pKi = 7.5 7.5 -14 3
Displacement of [3H]DPCPX from human A2BAR expressed in HEK293 cell membrane incubated for 30 mins by microbeta trilux scintillation counter analysisDisplacement of [3H]DPCPX from human A2BAR expressed in HEK293 cell membrane incubated for 30 mins by microbeta trilux scintillation counter analysis
ChEMBL None None None COc1cccc(-c2nc(N)nc(-c3ccccc3)c2C#N)c1 10.1021/acs.jmedchem.1c01636
156009568 177161 None 0 Human Binding pKi = 7.5 7.5 - 1
Displacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting methodDisplacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting method
ChEMBL 336 3 2 5 3.6 CC1=C(C(=O)OC(C)C)C(c2ccc[nH]2)n2c(nc3ccccc32)N1 10.1021/acs.jmedchem.0c00564
CHEMBL4634269 177161 None 0 Human Binding pKi = 7.5 7.5 - 1
Displacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting methodDisplacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting method
ChEMBL 336 3 2 5 3.6 CC1=C(C(=O)OC(C)C)C(c2ccc[nH]2)n2c(nc3ccccc32)N1 10.1021/acs.jmedchem.0c00564
11568060 77879 None 0 Human Binding pKi = 7.5 7.5 -17 3
Displacement of [3H]PSB298 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB298 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 425 6 3 6 2.3 CCCn1c(=O)[nH]c2[nH]c(-c3ccc(S(=O)(=O)Nc4ccccc4)cc3)nc2c1=O 10.1021/jm060277v
CHEMBL209366 77879 None 0 Human Binding pKi = 7.5 7.5 -17 3
Displacement of [3H]PSB298 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB298 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 425 6 3 6 2.3 CCCn1c(=O)[nH]c2[nH]c(-c3ccc(S(=O)(=O)Nc4ccccc4)cc3)nc2c1=O 10.1021/jm060277v
44451483 161127 None 0 Human Binding pKi = 7.5 7.5 5 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 501 5 1 7 2.7 Cn1c(=O)c2[nH]c(-c3ccc(OC(C)(C)C(=O)N4CCN(c5ccccc5)CC4)cc3)cc2n(C)c1=O 10.1016/j.bmc.2008.01.002
CHEMBL411720 161127 None 0 Human Binding pKi = 7.5 7.5 5 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 501 5 1 7 2.7 Cn1c(=O)c2[nH]c(-c3ccc(OC(C)(C)C(=O)N4CCN(c5ccccc5)CC4)cc3)cc2n(C)c1=O 10.1016/j.bmc.2008.01.002
49798135 10875 None 0 Human Binding pKi = 7.5 7.5 - 1
Displacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells after 30 minsDisplacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells after 30 mins
ChEMBL 521 7 2 7 4.5 CCCn1c(=O)[nH]c2cc(-c3ccc(OCc4nc(-c5ccc(Br)cc5)no4)cc3)[nH]c2c1=O 10.1016/j.ejmech.2010.03.011
CHEMBL1172502 10875 None 0 Human Binding pKi = 7.5 7.5 - 1
Displacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells after 30 minsDisplacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells after 30 mins
ChEMBL 521 7 2 7 4.5 CCCn1c(=O)[nH]c2cc(-c3ccc(OCc4nc(-c5ccc(Br)cc5)no4)cc3)[nH]c2c1=O 10.1016/j.ejmech.2010.03.011
44308520 103598 None 0 Human Binding pKi = 6.5 6.5 - 1
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 348 5 1 5 2.7 CCCn1c(=O)c2nc(-c3c(F)cccc3F)[nH]c2n(CCC)c1=O 10.1021/jm0104318
CHEMBL308660 103598 None 0 Human Binding pKi = 6.5 6.5 - 1
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 348 5 1 5 2.7 CCCn1c(=O)c2nc(-c3c(F)cccc3F)[nH]c2n(CCC)c1=O 10.1021/jm0104318
11545341 78024 None 0 Human Binding pKi = 6.5 6.5 1 3
Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cellsDisplacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells
ChEMBL 378 6 1 7 2.6 CCCn1c(=O)c2nc(-c3cnn(-c4ccccc4)c3)[nH]c2n(CCC)c1=O 10.1021/jm051268+
CHEMBL209831 78024 None 0 Human Binding pKi = 6.5 6.5 1 3
Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cellsDisplacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells
ChEMBL 378 6 1 7 2.6 CCCn1c(=O)c2nc(-c3cnn(-c4ccccc4)c3)[nH]c2n(CCC)c1=O 10.1021/jm051268+
135428653 81569 None 0 Human Binding pKi = 5.5 5.5 -295 4
Displacement of [125I]3-(4-aminobenzyl)-8-phenyloxyacetate-1-propyl-xanthine from human adenosine A2B receptorDisplacement of [125I]3-(4-aminobenzyl)-8-phenyloxyacetate-1-propyl-xanthine from human adenosine A2B receptor
ChEMBL 441 7 2 4 4.3 CCCN1C(=O)N2C[C@@H](C(C)C)N=C2c2[nH]c(C34CCC(CCC(=O)O)(CC3)CC4)nc21 10.1021/jm060539t
CHEMBL216200 81569 None 0 Human Binding pKi = 5.5 5.5 -295 4
Displacement of [125I]3-(4-aminobenzyl)-8-phenyloxyacetate-1-propyl-xanthine from human adenosine A2B receptorDisplacement of [125I]3-(4-aminobenzyl)-8-phenyloxyacetate-1-propyl-xanthine from human adenosine A2B receptor
ChEMBL 441 7 2 4 4.3 CCCN1C(=O)N2C[C@@H](C(C)C)N=C2c2[nH]c(C34CCC(CCC(=O)O)(CC3)CC4)nc21 10.1021/jm060539t
11257336 201870 None 0 Human Binding pKi = 5.5 5.5 -380 3
Inhibition of [3H]PSB-298 binding to adenosine A2b receptorInhibition of [3H]PSB-298 binding to adenosine A2b receptor
ChEMBL 374 5 1 6 2.3 CCCn1c(=O)c2nc(C3=CC(C)(C)N([O])C3(C)C)[nH]c2n(CCC)c1=O 10.1021/jm049513x
CHEMBL607302 201870 None 0 Human Binding pKi = 5.5 5.5 -380 3
Inhibition of [3H]PSB-298 binding to adenosine A2b receptorInhibition of [3H]PSB-298 binding to adenosine A2b receptor
ChEMBL 374 5 1 6 2.3 CCCn1c(=O)c2nc(C3=CC(C)(C)N([O])C3(C)C)[nH]c2n(CCC)c1=O 10.1021/jm049513x
11067937 203621 None 0 Human Binding pKi = 6.5 6.5 5 3
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 344 5 0 6 2.0 C=CCn1c(=O)c2c(nc(-c3ccccc3)n2CCCl)n(C)c1=O 10.1021/jm0104318
CHEMBL67110 203621 None 0 Human Binding pKi = 6.5 6.5 5 3
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 344 5 0 6 2.0 C=CCn1c(=O)c2c(nc(-c3ccccc3)n2CCCl)n(C)c1=O 10.1021/jm0104318
76309932 103842 None 0 Human Binding pKi = 5.5 5.5 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by Scatchard plot analysisDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by Scatchard plot analysis
ChEMBL 292 3 1 5 1.7 CCOC(=O)C1=C(C)NC(=O)N(C(C)=O)C1c1ccco1 10.1021/ml400185v
CHEMBL3091696 103842 None 0 Human Binding pKi = 5.5 5.5 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by Scatchard plot analysisDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by Scatchard plot analysis
ChEMBL 292 3 1 5 1.7 CCOC(=O)C1=C(C)NC(=O)N(C(C)=O)C1c1ccco1 10.1021/ml400185v
3286 3209 None 31 Rat Binding pKi = 5.5 5.5 -26 9
Displacement of [3H]PSB-603 from recombinant rat A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant rat A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins by liquid scintillation counting method
ChEMBL 350 4 3 6 0.7 CCCn1c(=O)[nH]c2c(c1=O)nc([nH]2)c1ccc(cc1)S(=O)(=O)O 10.1021/acs.jmedchem.9b00071
5311479 3209 None 31 Rat Binding pKi = 5.5 5.5 -26 9
Displacement of [3H]PSB-603 from recombinant rat A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant rat A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins by liquid scintillation counting method
ChEMBL 350 4 3 6 0.7 CCCn1c(=O)[nH]c2c(c1=O)nc([nH]2)c1ccc(cc1)S(=O)(=O)O 10.1021/acs.jmedchem.9b00071
CHEMBL8565 3209 None 31 Rat Binding pKi = 5.5 5.5 -26 9
Displacement of [3H]PSB-603 from recombinant rat A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant rat A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins by liquid scintillation counting method
ChEMBL 350 4 3 6 0.7 CCCn1c(=O)[nH]c2c(c1=O)nc([nH]2)c1ccc(cc1)S(=O)(=O)O 10.1021/acs.jmedchem.9b00071
47104774 103849 None 0 Human Binding pKi = 6.5 6.5 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 296 3 2 4 2.5 CC1=C(C(=O)OC(C)C)C(c2ccsc2)NC(=S)N1 10.1021/acs.jmedchem.0c01431
CHEMBL3091705 103849 None 0 Human Binding pKi = 6.5 6.5 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 296 3 2 4 2.5 CC1=C(C(=O)OC(C)C)C(c2ccsc2)NC(=S)N1 10.1021/acs.jmedchem.0c01431
46227993 199697 None 0 Human Binding pKi = 6.5 6.5 1 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 326 4 1 7 1.2 Cn1c(=O)c2[nH]c(Cc3ccco3)nc2n(Cc2ccco2)c1=O 10.1016/j.bmc.2009.07.034
CHEMBL593216 199697 None 0 Human Binding pKi = 6.5 6.5 1 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 326 4 1 7 1.2 Cn1c(=O)c2[nH]c(Cc3ccco3)nc2n(Cc2ccco2)c1=O 10.1016/j.bmc.2009.07.034
395949 72505 None 18 Human Binding pKi = 6.5 6.5 -3 3
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by beta scintillation countingDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by beta scintillation counting
ChEMBL 218 2 2 4 1.0 COc1cccc2cc(C(N)=O)c(=N)oc12 10.1016/j.ejmech.2012.05.009
CHEMBL1990267 72505 None 18 Human Binding pKi = 6.5 6.5 -3 3
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by beta scintillation countingDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by beta scintillation counting
ChEMBL 218 2 2 4 1.0 COc1cccc2cc(C(N)=O)c(=N)oc12 10.1016/j.ejmech.2012.05.009
3288 1855 None 40 Human Binding pKi = 4.5 4.5 -10232 5
Agonist activity at Homo sapiens (human) adenosine A2b receptor expressed in CHO cellsAgonist activity at Homo sapiens (human) adenosine A2b receptor expressed in CHO cells
ChEMBL 351 4 5 10 -1.2 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N[C@H]1CCC[C@@H]1O 10.1007/s00044-004-0013-y
9884817 1855 None 40 Human Binding pKi = 4.5 4.5 -10232 5
Agonist activity at Homo sapiens (human) adenosine A2b receptor expressed in CHO cellsAgonist activity at Homo sapiens (human) adenosine A2b receptor expressed in CHO cells
ChEMBL 351 4 5 10 -1.2 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N[C@H]1CCC[C@@H]1O 10.1007/s00044-004-0013-y
CHEMBL2163568 1855 None 40 Human Binding pKi = 4.5 4.5 -10232 5
Agonist activity at Homo sapiens (human) adenosine A2b receptor expressed in CHO cellsAgonist activity at Homo sapiens (human) adenosine A2b receptor expressed in CHO cells
ChEMBL 351 4 5 10 -1.2 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N[C@H]1CCC[C@@H]1O 10.1007/s00044-004-0013-y
2519 779 None 86 Human Binding pKi = 4.5 4.5 -11 12
Inhibition of human A2b adenosine receptorInhibition of human A2b adenosine receptor
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1021/acs.jmedchem.1c00261
2519.0 779 None 86 Human Binding pKi = 4.5 4.5 -11 12
Inhibition of human A2b adenosine receptorInhibition of human A2b adenosine receptor
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1021/acs.jmedchem.1c00261
407 779 None 86 Human Binding pKi = 4.5 4.5 -11 12
Inhibition of human A2b adenosine receptorInhibition of human A2b adenosine receptor
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1021/acs.jmedchem.1c00261
463 779 None 86 Human Binding pKi = 4.5 4.5 -11 12
Inhibition of human A2b adenosine receptorInhibition of human A2b adenosine receptor
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1021/acs.jmedchem.1c00261
CHEMBL113 779 None 86 Human Binding pKi = 4.5 4.5 -11 12
Inhibition of human A2b adenosine receptorInhibition of human A2b adenosine receptor
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1021/acs.jmedchem.1c00261
DB00201 779 None 86 Human Binding pKi = 4.5 4.5 -11 12
Inhibition of human A2b adenosine receptorInhibition of human A2b adenosine receptor
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1021/acs.jmedchem.1c00261
2519 779 None 86 Human Binding pKi = 4.5 4.5 -11 12
Inhibition of human A2b adenosine receptor assessed as inhibition constantInhibition of human A2b adenosine receptor assessed as inhibition constant
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1021/acs.jmedchem.1c00261
2519.0 779 None 86 Human Binding pKi = 4.5 4.5 -11 12
Inhibition of human A2b adenosine receptor assessed as inhibition constantInhibition of human A2b adenosine receptor assessed as inhibition constant
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1021/acs.jmedchem.1c00261
407 779 None 86 Human Binding pKi = 4.5 4.5 -11 12
Inhibition of human A2b adenosine receptor assessed as inhibition constantInhibition of human A2b adenosine receptor assessed as inhibition constant
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1021/acs.jmedchem.1c00261
463 779 None 86 Human Binding pKi = 4.5 4.5 -11 12
Inhibition of human A2b adenosine receptor assessed as inhibition constantInhibition of human A2b adenosine receptor assessed as inhibition constant
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1021/acs.jmedchem.1c00261
CHEMBL113 779 None 86 Human Binding pKi = 4.5 4.5 -11 12
Inhibition of human A2b adenosine receptor assessed as inhibition constantInhibition of human A2b adenosine receptor assessed as inhibition constant
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1021/acs.jmedchem.1c00261
DB00201 779 None 86 Human Binding pKi = 4.5 4.5 -11 12
Inhibition of human A2b adenosine receptor assessed as inhibition constantInhibition of human A2b adenosine receptor assessed as inhibition constant
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1021/acs.jmedchem.1c00261
44520976 202191 None 4 Human Binding pKi = 5.5 5.5 -1258 4
Displacement of radioligand from human adenosine A2B receptor expressed in cells by topcount microplate scintillation countingDisplacement of radioligand from human adenosine A2B receptor expressed in cells by topcount microplate scintillation counting
ChEMBL 323 4 2 6 2.3 Cc1cccc(CNC(=O)c2cc(-c3ccc(C)o3)nc(N)n2)n1 10.1016/j.bmc.2009.07.078
CHEMBL609578 202191 None 4 Human Binding pKi = 5.5 5.5 -1258 4
Displacement of radioligand from human adenosine A2B receptor expressed in cells by topcount microplate scintillation countingDisplacement of radioligand from human adenosine A2B receptor expressed in cells by topcount microplate scintillation counting
ChEMBL 323 4 2 6 2.3 Cc1cccc(CNC(=O)c2cc(-c3ccc(C)o3)nc(N)n2)n1 10.1016/j.bmc.2009.07.078
44520976 202191 None 4 Human Binding pKi = 5.5 5.5 -1258 4
Inhibition of human recombinant adenosine receptor A2bInhibition of human recombinant adenosine receptor A2b
ChEMBL 323 4 2 6 2.3 Cc1cccc(CNC(=O)c2cc(-c3ccc(C)o3)nc(N)n2)n1 10.1021/jm4011669
CHEMBL609578 202191 None 4 Human Binding pKi = 5.5 5.5 -1258 4
Inhibition of human recombinant adenosine receptor A2bInhibition of human recombinant adenosine receptor A2b
ChEMBL 323 4 2 6 2.3 Cc1cccc(CNC(=O)c2cc(-c3ccc(C)o3)nc(N)n2)n1 10.1021/jm4011669
135529386 489 None 0 Human Binding pKi = 7.5 7.5 - 1
Binding affinity of compound for displacement of [3H]DPCPX binding in HEK293 membranes expressing human A2B adenosine receptorsBinding affinity of compound for displacement of [3H]DPCPX binding in HEK293 membranes expressing human A2B adenosine receptors
ChEMBL 537 10 2 12 0.4 CCOC(=O)c1ccc(cc1)NC(=O)COc1c/c(=C\2/N=c3c(=N2)c(=O)n(c(=O)n3CCC)CCC)/n([nH]1)C 10.1021/jm0309654
440 489 None 0 Human Binding pKi = 7.5 7.5 - 1
Binding affinity of compound for displacement of [3H]DPCPX binding in HEK293 membranes expressing human A2B adenosine receptorsBinding affinity of compound for displacement of [3H]DPCPX binding in HEK293 membranes expressing human A2B adenosine receptors
ChEMBL 537 10 2 12 0.4 CCOC(=O)c1ccc(cc1)NC(=O)COc1c/c(=C\2/N=c3c(=N2)c(=O)n(c(=O)n3CCC)CCC)/n([nH]1)C 10.1021/jm0309654
CHEMBL284615 489 None 0 Human Binding pKi = 7.5 7.5 - 1
Binding affinity of compound for displacement of [3H]DPCPX binding in HEK293 membranes expressing human A2B adenosine receptorsBinding affinity of compound for displacement of [3H]DPCPX binding in HEK293 membranes expressing human A2B adenosine receptors
ChEMBL 537 10 2 12 0.4 CCOC(=O)c1ccc(cc1)NC(=O)COc1c/c(=C\2/N=c3c(=N2)c(=O)n(c(=O)n3CCC)CCC)/n([nH]1)C 10.1021/jm0309654
135529386 489 None 0 Human Binding pKi = 7.5 7.5 - 1
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 537 10 2 12 0.4 CCOC(=O)c1ccc(cc1)NC(=O)COc1c/c(=C\2/N=c3c(=N2)c(=O)n(c(=O)n3CCC)CCC)/n([nH]1)C 10.1021/jm0309654
440 489 None 0 Human Binding pKi = 7.5 7.5 - 1
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 537 10 2 12 0.4 CCOC(=O)c1ccc(cc1)NC(=O)COc1c/c(=C\2/N=c3c(=N2)c(=O)n(c(=O)n3CCC)CCC)/n([nH]1)C 10.1021/jm0309654
CHEMBL284615 489 None 0 Human Binding pKi = 7.5 7.5 - 1
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 537 10 2 12 0.4 CCOC(=O)c1ccc(cc1)NC(=O)COc1c/c(=C\2/N=c3c(=N2)c(=O)n(c(=O)n3CCC)CCC)/n([nH]1)C 10.1021/jm0309654
46880422 6047 None 0 Human Binding pKi = 7.5 7.5 22 3
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 306 4 1 5 3.1 O=C(Nc1ccc(-c2ccncc2)c(-c2ncco2)n1)C1CC1 10.1016/j.bmcl.2010.01.045
CHEMBL1080500 6047 None 0 Human Binding pKi = 7.5 7.5 22 3
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 306 4 1 5 3.1 O=C(Nc1ccc(-c2ccncc2)c(-c2ncco2)n1)C1CC1 10.1016/j.bmcl.2010.01.045
16070448 58020 None 0 Human Binding pKi = 7.5 7.5 9 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 317 4 1 5 2.9 O=C(Nc1cnc(-c2ccncc2)c(-c2ccncc2)n1)C1CC1 10.1021/ml100249e
CHEMBL1672622 58020 None 0 Human Binding pKi = 7.5 7.5 9 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 317 4 1 5 2.9 O=C(Nc1cnc(-c2ccncc2)c(-c2ccncc2)n1)C1CC1 10.1021/ml100249e
44406643 133160 None 0 Human Binding pKi = 7.5 7.5 15 3
Displacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cellsDisplacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cells
ChEMBL 494 8 1 10 3.3 CCCn1c(=O)c2nc(-c3cnn(Cc4nc(-c5cccc(Cl)c5)no4)c3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2005.10.002
CHEMBL370380 133160 None 0 Human Binding pKi = 7.5 7.5 15 3
Displacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cellsDisplacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cells
ChEMBL 494 8 1 10 3.3 CCCn1c(=O)c2nc(-c3cnn(Cc4nc(-c5cccc(Cl)c5)no4)c3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2005.10.002
44451482 166886 None 0 Human Binding pKi = 7.5 7.5 16 3
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 503 6 1 8 2.0 COc1cc(OCC(=O)N2CCN(c3ccccc3)CC2)ccc1-c1cc2c([nH]1)c(=O)n(C)c(=O)n2C 10.1016/j.bmc.2008.01.002
CHEMBL428605 166886 None 0 Human Binding pKi = 7.5 7.5 16 3
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 503 6 1 8 2.0 COc1cc(OCC(=O)N2CCN(c3ccccc3)CC2)ccc1-c1cc2c([nH]1)c(=O)n(C)c(=O)n2C 10.1016/j.bmc.2008.01.002
46227984 201294 None 0 Human Binding pKi = 7.5 7.5 4 3
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 340 4 0 8 1.3 Cn1c(=O)c2c(nc(Cc3ccco3)n2C)n(Cc2ccco2)c1=O 10.1016/j.bmc.2009.07.034
CHEMBL604075 201294 None 0 Human Binding pKi = 7.5 7.5 4 3
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 340 4 0 8 1.3 Cn1c(=O)c2c(nc(Cc3ccco3)n2C)n(Cc2ccco2)c1=O 10.1016/j.bmc.2009.07.034
9843101 199103 None 0 Human Binding pKi = 5.5 5.5 -7943 4
Displacement of [3H]PSB-603 from human adenosine receptor A2B expressed in CHO cell membranes incubated for 75 mins by radioligand competition assayDisplacement of [3H]PSB-603 from human adenosine receptor A2B expressed in CHO cell membranes incubated for 75 mins by radioligand competition assay
ChEMBL 385 6 1 7 3.9 COc1cc(-c2nc(NC(C)=O)sc2-c2ccncc2)cc(OC)c1OC 10.1016/j.ejmech.2019.111879
CHEMBL589080 199103 None 0 Human Binding pKi = 5.5 5.5 -7943 4
Displacement of [3H]PSB-603 from human adenosine receptor A2B expressed in CHO cell membranes incubated for 75 mins by radioligand competition assayDisplacement of [3H]PSB-603 from human adenosine receptor A2B expressed in CHO cell membranes incubated for 75 mins by radioligand competition assay
ChEMBL 385 6 1 7 3.9 COc1cc(-c2nc(NC(C)=O)sc2-c2ccncc2)cc(OC)c1OC 10.1016/j.ejmech.2019.111879
45268927 196145 None 0 Human Binding pKi = 6.5 6.5 1 2
Binding affinity to human adenosine A2b receptor expressed in HEK293 cellsBinding affinity to human adenosine A2b receptor expressed in HEK293 cells
ChEMBL 342 7 1 6 2.0 CCCn1c(=O)c2[nH]c(-c3ccccc3)nc2n(CCCOC)c1=O 10.1016/j.bmc.2009.03.029
CHEMBL561167 196145 None 0 Human Binding pKi = 6.5 6.5 1 2
Binding affinity to human adenosine A2b receptor expressed in HEK293 cellsBinding affinity to human adenosine A2b receptor expressed in HEK293 cells
ChEMBL 342 7 1 6 2.0 CCCn1c(=O)c2[nH]c(-c3ccccc3)nc2n(CCCOC)c1=O 10.1016/j.bmc.2009.03.029
2732424 22192 None 29 Human Binding pKi = 5.5 5.5 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 282 3 2 5 2.5 CCOC(=O)C1=C(C)N=C(S)NC1c1cccs1 10.1021/acs.jmedchem.0c01431
CHEMBL1322729 22192 None 29 Human Binding pKi = 5.5 5.5 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 282 3 2 5 2.5 CCOC(=O)C1=C(C)N=C(S)NC1c1cccs1 10.1021/acs.jmedchem.0c01431
44390559 65579 None 0 Human Binding pKi = 6.5 6.5 1 3
Binding affinity for adenosine A2b receptor by using as [3H]ZM-241385 (14 nM) radioligand in membranes from HEK-A2B cellsBinding affinity for adenosine A2b receptor by using as [3H]ZM-241385 (14 nM) radioligand in membranes from HEK-A2B cells
ChEMBL 554 9 1 9 5.0 CCCn1c(=O)c2nc(-c3ccc(OCc4nc(-c5ccccc5C(F)(F)F)no4)cc3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2004.11.044
CHEMBL183183 65579 None 0 Human Binding pKi = 6.5 6.5 1 3
Binding affinity for adenosine A2b receptor by using as [3H]ZM-241385 (14 nM) radioligand in membranes from HEK-A2B cellsBinding affinity for adenosine A2b receptor by using as [3H]ZM-241385 (14 nM) radioligand in membranes from HEK-A2B cells
ChEMBL 554 9 1 9 5.0 CCCn1c(=O)c2nc(-c3ccc(OCc4nc(-c5ccccc5C(F)(F)F)no4)cc3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2004.11.044
50940932 57243 None 0 Human Binding pKi = 5.5 5.5 -8 4
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 315 4 1 5 4.3 CCC(=O)Nc1nc(-c2ccsc2)cc(-c2ccsc2)n1 10.1021/jm100843z
CHEMBL1650347 57243 None 0 Human Binding pKi = 5.5 5.5 -8 4
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 315 4 1 5 4.3 CCC(=O)Nc1nc(-c2ccsc2)cc(-c2ccsc2)n1 10.1021/jm100843z
162675258 183355 None 0 Human Binding pKi = 6.5 6.5 9 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 278 4 2 4 2.1 CC1=C(C(=O)OCC(C)C)C(c2ccoc2)NC(=O)N1 10.1021/acs.jmedchem.0c01431
CHEMBL4797674 183355 None 0 Human Binding pKi = 6.5 6.5 9 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 278 4 2 4 2.1 CC1=C(C(=O)OCC(C)C)C(c2ccoc2)NC(=O)N1 10.1021/acs.jmedchem.0c01431
46880509 6156 None 0 Human Binding pKi = 7.5 7.5 44 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 316 4 1 4 3.6 O=C(Nc1ccc(-c2ccncc2)c(-c2cccnc2)n1)C1CC1 10.1016/j.bmcl.2010.01.045
CHEMBL1081040 6156 None 0 Human Binding pKi = 7.5 7.5 44 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 316 4 1 4 3.6 O=C(Nc1ccc(-c2ccncc2)c(-c2cccnc2)n1)C1CC1 10.1016/j.bmcl.2010.01.045
11495161 78289 None 0 Human Binding pKi = 7.5 7.5 -1 3
Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cellsDisplacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells
ChEMBL 406 7 1 7 2.9 CCCn1c(=O)c2nc(-c3cnn(Cc4ccccc4C)c3)[nH]c2n(CCC)c1=O 10.1021/jm051268+
CHEMBL210747 78289 None 0 Human Binding pKi = 7.5 7.5 -1 3
Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cellsDisplacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells
ChEMBL 406 7 1 7 2.9 CCCn1c(=O)c2nc(-c3cnn(Cc4ccccc4C)c3)[nH]c2n(CCC)c1=O 10.1021/jm051268+
541615 97525 None 1 Human Binding pKi = 7.5 7.5 -2 4
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 385 8 2 7 1.2 CCCn1c(=O)c2nc(-c3ccc(OCC(N)=O)cc3)[nH]c2n(CCC)c1=O 10.1021/jm0506221
CHEMBL27043 97525 None 1 Human Binding pKi = 7.5 7.5 -2 4
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 385 8 2 7 1.2 CCCn1c(=O)c2nc(-c3ccc(OCC(N)=O)cc3)[nH]c2n(CCC)c1=O 10.1021/jm0506221
45271363 195432 None 0 Human Binding pKi = 7.5 7.5 2 4
Binding affinity to human adenosine A2b receptor expressed in HEK293 cellsBinding affinity to human adenosine A2b receptor expressed in HEK293 cells
ChEMBL 478 10 2 9 2.0 CCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4cccnc4)cc3)nc2n(CCCOC)c1=O 10.1016/j.bmc.2009.03.029
CHEMBL552304 195432 None 0 Human Binding pKi = 7.5 7.5 2 4
Binding affinity to human adenosine A2b receptor expressed in HEK293 cellsBinding affinity to human adenosine A2b receptor expressed in HEK293 cells
ChEMBL 478 10 2 9 2.0 CCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4cccnc4)cc3)nc2n(CCCOC)c1=O 10.1016/j.bmc.2009.03.029
11569877 133445 None 0 Human Binding pKi = 7.5 7.5 6 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 518 11 3 7 3.6 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(CC(=O)O)cc4)cc3)cc2n(CCC)c1=O 10.1021/jm0506221
CHEMBL370629 133445 None 0 Human Binding pKi = 7.5 7.5 6 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 518 11 3 7 3.6 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(CC(=O)O)cc4)cc3)cc2n(CCC)c1=O 10.1021/jm0506221
137639632 156921 None 0 Human Binding pKi = 6.5 6.5 - 1
Displacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 minsDisplacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 mins
ChEMBL 439 7 1 9 0.9 CCCn1c(=O)c2[nH]c(-c3cnn(CC#CCN4CCOCC4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2017.04.014
CHEMBL4072350 156921 None 0 Human Binding pKi = 6.5 6.5 - 1
Displacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 minsDisplacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 mins
ChEMBL 439 7 1 9 0.9 CCCn1c(=O)c2[nH]c(-c3cnn(CC#CCN4CCOCC4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2017.04.014
CHEMBL5089580 215214 None 0 Human Binding pKi = 6.5 6.5 -1174 4
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells by liquid scintillation counting analysisDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells by liquid scintillation counting analysis
ChEMBL None None None Nc1nc(-c2ccc(OCCCN3CCCCC3)cc2)c2c(n1)-c1ccccc1C2=O 10.1021/acs.jmedchem.0c00914
164617060 185409 None 0 Human Binding pKi = 5.5 5.5 -363 4
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK cell membrane incubated for 30 mins by microplate beta scintillation counting based radioligand inhibition assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK cell membrane incubated for 30 mins by microplate beta scintillation counting based radioligand inhibition assay
ChEMBL 440 9 4 9 1.0 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCCCCc4ccccc4)ncnc32)[C@H](O)[C@@H]1O 10.1016/j.ejmech.2021.113607
CHEMBL4861092 185409 None 0 Human Binding pKi = 5.5 5.5 -363 4
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK cell membrane incubated for 30 mins by microplate beta scintillation counting based radioligand inhibition assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK cell membrane incubated for 30 mins by microplate beta scintillation counting based radioligand inhibition assay
ChEMBL 440 9 4 9 1.0 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCCCCc4ccccc4)ncnc32)[C@H](O)[C@@H]1O 10.1016/j.ejmech.2021.113607
22266740 96285 None 0 Human Binding pKi = 6.5 6.5 - 1
Displacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 480 7 1 10 2.9 CCCn1c(=O)c2[nH]c(-c3cnn(Cc4noc(-c5ccc(Cl)cc5)n4)c3)nc2n(CC)c1=O 10.1021/jm7014815
CHEMBL261182 96285 None 0 Human Binding pKi = 6.5 6.5 - 1
Displacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 480 7 1 10 2.9 CCCn1c(=O)c2[nH]c(-c3cnn(Cc4noc(-c5ccc(Cl)cc5)n4)c3)nc2n(CC)c1=O 10.1021/jm7014815
10861697 103038 None 0 Rat Binding pKi = 5.5 5.5 -4 4
Inhibition of [125I]-APOBX binding to rat Adenosine A2B receptor expressed in HEK cellsInhibition of [125I]-APOBX binding to rat Adenosine A2B receptor expressed in HEK cells
ChEMBL 374 7 0 6 3.1 CCCn1c(=O)c2c(nc(-c3ccccc3)n2CCCl)n(CCC)c1=O 10.1021/jm0104318
CHEMBL307105 103038 None 0 Rat Binding pKi = 5.5 5.5 -4 4
Inhibition of [125I]-APOBX binding to rat Adenosine A2B receptor expressed in HEK cellsInhibition of [125I]-APOBX binding to rat Adenosine A2B receptor expressed in HEK cells
ChEMBL 374 7 0 6 3.1 CCCn1c(=O)c2c(nc(-c3ccccc3)n2CCCl)n(CCC)c1=O 10.1021/jm0104318
1241166 199284 None 21 Human Binding pKi = 6.5 6.5 2 2
Displacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cells
ChEMBL 356 5 1 4 5.8 O=C(c1ccccc1)c1sc(Nc2ccccc2)nc1-c1ccccc1 10.1016/j.bmc.2010.01.072
CHEMBL590302 199284 None 21 Human Binding pKi = 6.5 6.5 2 2
Displacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cells
ChEMBL 356 5 1 4 5.8 O=C(c1ccccc1)c1sc(Nc2ccccc2)nc1-c1ccccc1 10.1016/j.bmc.2010.01.072
127043829 141218 None 0 Human Binding pKi = 6.5 6.5 -1 4
Displacement of [3H]PSB-603 from recombinant human adenosine receptor A2b expressed in CHO cell membranesDisplacement of [3H]PSB-603 from recombinant human adenosine receptor A2b expressed in CHO cell membranes
ChEMBL 552 13 0 10 3.1 CCCCn1c(=O)c2c(nc3n2CCCN3CCc2ccc(OCCN3CCOCC3)cc2)n(CCCC)c1=O 10.1016/j.bmc.2016.07.028
CHEMBL3828555 141218 None 0 Human Binding pKi = 6.5 6.5 -1 4
Displacement of [3H]PSB-603 from recombinant human adenosine receptor A2b expressed in CHO cell membranesDisplacement of [3H]PSB-603 from recombinant human adenosine receptor A2b expressed in CHO cell membranes
ChEMBL 552 13 0 10 3.1 CCCCn1c(=O)c2c(nc3n2CCCN3CCc2ccc(OCCN3CCOCC3)cc2)n(CCCC)c1=O 10.1016/j.bmc.2016.07.028
44587954 174433 None 0 Human Binding pKi = 6.5 6.5 2 2
Displacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cells
ChEMBL 371 6 3 6 2.4 CCCn1c(=O)c2[nH]c(-c3ccc(C(=O)O)cc3)c(O)c2n(CCC)c1=O 10.1016/j.bmc.2008.09.067
CHEMBL455315 174433 None 0 Human Binding pKi = 6.5 6.5 2 2
Displacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cells
ChEMBL 371 6 3 6 2.4 CCCn1c(=O)c2[nH]c(-c3ccc(C(=O)O)cc3)c(O)c2n(CCC)c1=O 10.1016/j.bmc.2008.09.067
127043664 141207 None 0 Human Binding pKi = 6.5 6.5 1 4
Displacement of [3H]PSB-603 from recombinant human adenosine receptor A2b expressed in CHO cell membranesDisplacement of [3H]PSB-603 from recombinant human adenosine receptor A2b expressed in CHO cell membranes
ChEMBL 510 13 0 9 3.4 CCCn1c(=O)c2c(nc3n2CCCN3CCc2ccc(OCCN(CC)CC)cc2)n(CCC)c1=O 10.1016/j.bmc.2016.07.028
CHEMBL3828401 141207 None 0 Human Binding pKi = 6.5 6.5 1 4
Displacement of [3H]PSB-603 from recombinant human adenosine receptor A2b expressed in CHO cell membranesDisplacement of [3H]PSB-603 from recombinant human adenosine receptor A2b expressed in CHO cell membranes
ChEMBL 510 13 0 9 3.4 CCCn1c(=O)c2c(nc3n2CCCN3CCc2ccc(OCCN(CC)CC)cc2)n(CCC)c1=O 10.1016/j.bmc.2016.07.028
52950000 19126 None 0 Human Binding pKi = 6.5 6.5 2 2
Displacement of [3H]ZM241385 from human adenosine A2B receptor transfected in CHO cells after 60 mins by scintillation countingDisplacement of [3H]ZM241385 from human adenosine A2B receptor transfected in CHO cells after 60 mins by scintillation counting
ChEMBL 505 8 2 4 5.2 N#Cc1c(CCc2ccccc2)c2cc(OCC(=O)NCc3ccc(Cl)c(Cl)c3)ccc2[nH]c1=O 10.1016/j.bmcl.2010.10.030
CHEMBL1289344 19126 None 0 Human Binding pKi = 6.5 6.5 2 2
Displacement of [3H]ZM241385 from human adenosine A2B receptor transfected in CHO cells after 60 mins by scintillation countingDisplacement of [3H]ZM241385 from human adenosine A2B receptor transfected in CHO cells after 60 mins by scintillation counting
ChEMBL 505 8 2 4 5.2 N#Cc1c(CCc2ccccc2)c2cc(OCC(=O)NCc3ccc(Cl)c(Cl)c3)ccc2[nH]c1=O 10.1016/j.bmcl.2010.10.030
2519 779 None 86 Human Binding pKi = 4.5 4.5 -11 12
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1016/j.bmc.2013.09.044
2519.0 779 None 86 Human Binding pKi = 4.5 4.5 -11 12
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1016/j.bmc.2013.09.044
407 779 None 86 Human Binding pKi = 4.5 4.5 -11 12
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1016/j.bmc.2013.09.044
463 779 None 86 Human Binding pKi = 4.5 4.5 -11 12
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1016/j.bmc.2013.09.044
CHEMBL113 779 None 86 Human Binding pKi = 4.5 4.5 -11 12
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1016/j.bmc.2013.09.044
DB00201 779 None 86 Human Binding pKi = 4.5 4.5 -11 12
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1016/j.bmc.2013.09.044
2519 779 None 86 Human Binding pKi = 4.5 4.5 -11 12
Binding affinity to human adenosine A2B receptor by radioligand displacement assayBinding affinity to human adenosine A2B receptor by radioligand displacement assay
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1039/C8MD00070K
2519.0 779 None 86 Human Binding pKi = 4.5 4.5 -11 12
Binding affinity to human adenosine A2B receptor by radioligand displacement assayBinding affinity to human adenosine A2B receptor by radioligand displacement assay
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1039/C8MD00070K
407 779 None 86 Human Binding pKi = 4.5 4.5 -11 12
Binding affinity to human adenosine A2B receptor by radioligand displacement assayBinding affinity to human adenosine A2B receptor by radioligand displacement assay
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1039/C8MD00070K
463 779 None 86 Human Binding pKi = 4.5 4.5 -11 12
Binding affinity to human adenosine A2B receptor by radioligand displacement assayBinding affinity to human adenosine A2B receptor by radioligand displacement assay
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1039/C8MD00070K
CHEMBL113 779 None 86 Human Binding pKi = 4.5 4.5 -11 12
Binding affinity to human adenosine A2B receptor by radioligand displacement assayBinding affinity to human adenosine A2B receptor by radioligand displacement assay
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1039/C8MD00070K
DB00201 779 None 86 Human Binding pKi = 4.5 4.5 -11 12
Binding affinity to human adenosine A2B receptor by radioligand displacement assayBinding affinity to human adenosine A2B receptor by radioligand displacement assay
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1039/C8MD00070K
2519 779 None 86 Human Binding pKi = 4.5 4.5 -11 12
Displacement of [125I]-ABOPX from human recombinant Adenosine A2B receptor expressed in HEK293 cells after 3 hrsDisplacement of [125I]-ABOPX from human recombinant Adenosine A2B receptor expressed in HEK293 cells after 3 hrs
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1021/acs.jmedchem.5b01586
2519.0 779 None 86 Human Binding pKi = 4.5 4.5 -11 12
Displacement of [125I]-ABOPX from human recombinant Adenosine A2B receptor expressed in HEK293 cells after 3 hrsDisplacement of [125I]-ABOPX from human recombinant Adenosine A2B receptor expressed in HEK293 cells after 3 hrs
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1021/acs.jmedchem.5b01586
407 779 None 86 Human Binding pKi = 4.5 4.5 -11 12
Displacement of [125I]-ABOPX from human recombinant Adenosine A2B receptor expressed in HEK293 cells after 3 hrsDisplacement of [125I]-ABOPX from human recombinant Adenosine A2B receptor expressed in HEK293 cells after 3 hrs
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1021/acs.jmedchem.5b01586
463 779 None 86 Human Binding pKi = 4.5 4.5 -11 12
Displacement of [125I]-ABOPX from human recombinant Adenosine A2B receptor expressed in HEK293 cells after 3 hrsDisplacement of [125I]-ABOPX from human recombinant Adenosine A2B receptor expressed in HEK293 cells after 3 hrs
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1021/acs.jmedchem.5b01586
CHEMBL113 779 None 86 Human Binding pKi = 4.5 4.5 -11 12
Displacement of [125I]-ABOPX from human recombinant Adenosine A2B receptor expressed in HEK293 cells after 3 hrsDisplacement of [125I]-ABOPX from human recombinant Adenosine A2B receptor expressed in HEK293 cells after 3 hrs
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1021/acs.jmedchem.5b01586
DB00201 779 None 86 Human Binding pKi = 4.5 4.5 -11 12
Displacement of [125I]-ABOPX from human recombinant Adenosine A2B receptor expressed in HEK293 cells after 3 hrsDisplacement of [125I]-ABOPX from human recombinant Adenosine A2B receptor expressed in HEK293 cells after 3 hrs
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1021/acs.jmedchem.5b01586
2519 779 None 86 Human Binding pKi = 4.5 4.5 -11 12
Displacement of [3H]PSB-603 from human A2B receptor expressed in CHO cell membraneDisplacement of [3H]PSB-603 from human A2B receptor expressed in CHO cell membrane
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1016/j.bmc.2016.09.003
2519.0 779 None 86 Human Binding pKi = 4.5 4.5 -11 12
Displacement of [3H]PSB-603 from human A2B receptor expressed in CHO cell membraneDisplacement of [3H]PSB-603 from human A2B receptor expressed in CHO cell membrane
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1016/j.bmc.2016.09.003
407 779 None 86 Human Binding pKi = 4.5 4.5 -11 12
Displacement of [3H]PSB-603 from human A2B receptor expressed in CHO cell membraneDisplacement of [3H]PSB-603 from human A2B receptor expressed in CHO cell membrane
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1016/j.bmc.2016.09.003
463 779 None 86 Human Binding pKi = 4.5 4.5 -11 12
Displacement of [3H]PSB-603 from human A2B receptor expressed in CHO cell membraneDisplacement of [3H]PSB-603 from human A2B receptor expressed in CHO cell membrane
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1016/j.bmc.2016.09.003
CHEMBL113 779 None 86 Human Binding pKi = 4.5 4.5 -11 12
Displacement of [3H]PSB-603 from human A2B receptor expressed in CHO cell membraneDisplacement of [3H]PSB-603 from human A2B receptor expressed in CHO cell membrane
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1016/j.bmc.2016.09.003
DB00201 779 None 86 Human Binding pKi = 4.5 4.5 -11 12
Displacement of [3H]PSB-603 from human A2B receptor expressed in CHO cell membraneDisplacement of [3H]PSB-603 from human A2B receptor expressed in CHO cell membrane
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1016/j.bmc.2016.09.003
2519 779 None 86 Human Binding pKi = 4.5 4.5 -11 12
Displacement of [3H]PSB-603 from human adenosine A2B receptorDisplacement of [3H]PSB-603 from human adenosine A2B receptor
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1016/j.bmc.2013.09.044
2519.0 779 None 86 Human Binding pKi = 4.5 4.5 -11 12
Displacement of [3H]PSB-603 from human adenosine A2B receptorDisplacement of [3H]PSB-603 from human adenosine A2B receptor
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1016/j.bmc.2013.09.044
407 779 None 86 Human Binding pKi = 4.5 4.5 -11 12
Displacement of [3H]PSB-603 from human adenosine A2B receptorDisplacement of [3H]PSB-603 from human adenosine A2B receptor
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1016/j.bmc.2013.09.044
463 779 None 86 Human Binding pKi = 4.5 4.5 -11 12
Displacement of [3H]PSB-603 from human adenosine A2B receptorDisplacement of [3H]PSB-603 from human adenosine A2B receptor
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1016/j.bmc.2013.09.044
CHEMBL113 779 None 86 Human Binding pKi = 4.5 4.5 -11 12
Displacement of [3H]PSB-603 from human adenosine A2B receptorDisplacement of [3H]PSB-603 from human adenosine A2B receptor
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1016/j.bmc.2013.09.044
DB00201 779 None 86 Human Binding pKi = 4.5 4.5 -11 12
Displacement of [3H]PSB-603 from human adenosine A2B receptorDisplacement of [3H]PSB-603 from human adenosine A2B receptor
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1016/j.bmc.2013.09.044
2519 779 None 86 Human Binding pKi = 4.5 4.5 -11 12
Displacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cells
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1016/j.bmc.2010.01.072
2519.0 779 None 86 Human Binding pKi = 4.5 4.5 -11 12
Displacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cells
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1016/j.bmc.2010.01.072
407 779 None 86 Human Binding pKi = 4.5 4.5 -11 12
Displacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cells
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1016/j.bmc.2010.01.072
463 779 None 86 Human Binding pKi = 4.5 4.5 -11 12
Displacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cells
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1016/j.bmc.2010.01.072
CHEMBL113 779 None 86 Human Binding pKi = 4.5 4.5 -11 12
Displacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cells
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1016/j.bmc.2010.01.072
DB00201 779 None 86 Human Binding pKi = 4.5 4.5 -11 12
Displacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cells
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1016/j.bmc.2010.01.072
2519 779 None 86 Human Binding pKi = 4.5 4.5 -11 12
Displacement of [3H]PSB-603 from human adenosine receptor A2B expressed in CHO cell membranes incubated for 75 mins by radioligand competition assayDisplacement of [3H]PSB-603 from human adenosine receptor A2B expressed in CHO cell membranes incubated for 75 mins by radioligand competition assay
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1016/j.ejmech.2019.111879
2519.0 779 None 86 Human Binding pKi = 4.5 4.5 -11 12
Displacement of [3H]PSB-603 from human adenosine receptor A2B expressed in CHO cell membranes incubated for 75 mins by radioligand competition assayDisplacement of [3H]PSB-603 from human adenosine receptor A2B expressed in CHO cell membranes incubated for 75 mins by radioligand competition assay
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1016/j.ejmech.2019.111879
407 779 None 86 Human Binding pKi = 4.5 4.5 -11 12
Displacement of [3H]PSB-603 from human adenosine receptor A2B expressed in CHO cell membranes incubated for 75 mins by radioligand competition assayDisplacement of [3H]PSB-603 from human adenosine receptor A2B expressed in CHO cell membranes incubated for 75 mins by radioligand competition assay
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1016/j.ejmech.2019.111879
463 779 None 86 Human Binding pKi = 4.5 4.5 -11 12
Displacement of [3H]PSB-603 from human adenosine receptor A2B expressed in CHO cell membranes incubated for 75 mins by radioligand competition assayDisplacement of [3H]PSB-603 from human adenosine receptor A2B expressed in CHO cell membranes incubated for 75 mins by radioligand competition assay
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1016/j.ejmech.2019.111879
CHEMBL113 779 None 86 Human Binding pKi = 4.5 4.5 -11 12
Displacement of [3H]PSB-603 from human adenosine receptor A2B expressed in CHO cell membranes incubated for 75 mins by radioligand competition assayDisplacement of [3H]PSB-603 from human adenosine receptor A2B expressed in CHO cell membranes incubated for 75 mins by radioligand competition assay
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1016/j.ejmech.2019.111879
DB00201 779 None 86 Human Binding pKi = 4.5 4.5 -11 12
Displacement of [3H]PSB-603 from human adenosine receptor A2B expressed in CHO cell membranes incubated for 75 mins by radioligand competition assayDisplacement of [3H]PSB-603 from human adenosine receptor A2B expressed in CHO cell membranes incubated for 75 mins by radioligand competition assay
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1016/j.ejmech.2019.111879
2519 779 None 86 Human Binding pKi = 4.5 4.5 -11 12
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1021/jm900413e
2519.0 779 None 86 Human Binding pKi = 4.5 4.5 -11 12
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1021/jm900413e
407 779 None 86 Human Binding pKi = 4.5 4.5 -11 12
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1021/jm900413e
463 779 None 86 Human Binding pKi = 4.5 4.5 -11 12
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1021/jm900413e
CHEMBL113 779 None 86 Human Binding pKi = 4.5 4.5 -11 12
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1021/jm900413e
DB00201 779 None 86 Human Binding pKi = 4.5 4.5 -11 12
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1021/jm900413e
2519 779 None 86 Human Binding pKi = 4.5 4.5 -11 12
Displacement of [3H]PSB603 from recombinant human adenosine A2b receptor expressed in HEK293 cellsDisplacement of [3H]PSB603 from recombinant human adenosine A2b receptor expressed in HEK293 cells
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1016/j.bmc.2019.02.004
2519.0 779 None 86 Human Binding pKi = 4.5 4.5 -11 12
Displacement of [3H]PSB603 from recombinant human adenosine A2b receptor expressed in HEK293 cellsDisplacement of [3H]PSB603 from recombinant human adenosine A2b receptor expressed in HEK293 cells
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1016/j.bmc.2019.02.004
407 779 None 86 Human Binding pKi = 4.5 4.5 -11 12
Displacement of [3H]PSB603 from recombinant human adenosine A2b receptor expressed in HEK293 cellsDisplacement of [3H]PSB603 from recombinant human adenosine A2b receptor expressed in HEK293 cells
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1016/j.bmc.2019.02.004
463 779 None 86 Human Binding pKi = 4.5 4.5 -11 12
Displacement of [3H]PSB603 from recombinant human adenosine A2b receptor expressed in HEK293 cellsDisplacement of [3H]PSB603 from recombinant human adenosine A2b receptor expressed in HEK293 cells
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1016/j.bmc.2019.02.004
CHEMBL113 779 None 86 Human Binding pKi = 4.5 4.5 -11 12
Displacement of [3H]PSB603 from recombinant human adenosine A2b receptor expressed in HEK293 cellsDisplacement of [3H]PSB603 from recombinant human adenosine A2b receptor expressed in HEK293 cells
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1016/j.bmc.2019.02.004
DB00201 779 None 86 Human Binding pKi = 4.5 4.5 -11 12
Displacement of [3H]PSB603 from recombinant human adenosine A2b receptor expressed in HEK293 cellsDisplacement of [3H]PSB603 from recombinant human adenosine A2b receptor expressed in HEK293 cells
ChEMBL 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 10.1016/j.bmc.2019.02.004
44459941 96698 None 4 Human Binding pKi = 5.5 5.5 1 3
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 246 4 0 6 0.3 C=CCn1c(=O)c2c(ncn2C)n(CC=C)c1=O 10.1021/jm0104318
CHEMBL26406 96698 None 4 Human Binding pKi = 5.5 5.5 1 3
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 246 4 0 6 0.3 C=CCn1c(=O)c2c(ncn2C)n(CC=C)c1=O 10.1021/jm0104318
10563436 135230 None 0 Human Binding pKi = 7.5 7.5 -3 3
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 262 3 2 4 1.5 CCCn1c(=O)[nH]c2[nH]c(C3CCCC3)nc2c1=O 10.1021/jm0104318
CHEMBL37243 135230 None 0 Human Binding pKi = 7.5 7.5 -3 3
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 262 3 2 4 1.5 CCCn1c(=O)[nH]c2[nH]c(C3CCCC3)nc2c1=O 10.1021/jm0104318
136002186 109701 None 0 Human Binding pKi = 7.5 7.5 1 2
Binding affinity of compound for displacement of [3H]DPCPX binding in HEK293 membranes expressing human A2B adenosine receptorsBinding affinity of compound for displacement of [3H]DPCPX binding in HEK293 membranes expressing human A2B adenosine receptors
ChEMBL 449 8 2 8 2.3 CCCn1c(=O)c2nc(-c3cc(NC(=O)Cc4ccccc4)n(C)n3)[nH]c2n(CCC)c1=O 10.1021/jm0309654
CHEMBL32281 109701 None 0 Human Binding pKi = 7.5 7.5 1 2
Binding affinity of compound for displacement of [3H]DPCPX binding in HEK293 membranes expressing human A2B adenosine receptorsBinding affinity of compound for displacement of [3H]DPCPX binding in HEK293 membranes expressing human A2B adenosine receptors
ChEMBL 449 8 2 8 2.3 CCCn1c(=O)c2nc(-c3cc(NC(=O)Cc4ccccc4)n(C)n3)[nH]c2n(CCC)c1=O 10.1021/jm0309654
136002186 109701 None 0 Human Binding pKi = 7.5 7.5 1 2
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 449 8 2 8 2.3 CCCn1c(=O)c2nc(-c3cc(NC(=O)Cc4ccccc4)n(C)n3)[nH]c2n(CCC)c1=O 10.1021/jm0309654
CHEMBL32281 109701 None 0 Human Binding pKi = 7.5 7.5 1 2
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 449 8 2 8 2.3 CCCn1c(=O)c2nc(-c3cc(NC(=O)Cc4ccccc4)n(C)n3)[nH]c2n(CCC)c1=O 10.1021/jm0309654
21958725 94562 None 0 Human Binding pKi = 7.5 7.5 3 4
Displacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranesDisplacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranes
ChEMBL 364 6 2 6 2.1 CCCCn1c(=O)[nH]c2nc(-c3cnn(Cc4ccccc4)c3)[nH]c2c1=O 10.1016/j.bmcl.2008.01.008
CHEMBL251874 94562 None 0 Human Binding pKi = 7.5 7.5 3 4
Displacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranesDisplacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranes
ChEMBL 364 6 2 6 2.1 CCCCn1c(=O)[nH]c2nc(-c3cnn(Cc4ccccc4)c3)[nH]c2c1=O 10.1016/j.bmcl.2008.01.008
11667107 144393 None 0 Human Binding pKi = 7.5 7.5 - 1
Displacement of [3H]DPCPX from human A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human A2B receptor expressed in HEK293 cells
ChEMBL 332 4 1 7 2.6 [O-][n+]1cccc(Nc2ncc(-c3ccncn3)c(-c3ccco3)n2)c1 10.1021/jm061333v
CHEMBL390600 144393 None 0 Human Binding pKi = 7.5 7.5 - 1
Displacement of [3H]DPCPX from human A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human A2B receptor expressed in HEK293 cells
ChEMBL 332 4 1 7 2.6 [O-][n+]1cccc(Nc2ncc(-c3ccncn3)c(-c3ccco3)n2)c1 10.1021/jm061333v
11812897 120299 None 0 Human Binding pKi = 7.5 7.5 3 4
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 26-45Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 26-45
ChEMBL 484 6 2 8 5.5 CCCCn1cc2c(nc(NC(=O)Nc3ccc(Cl)c(Cl)c3)n3nc(-c4ccco4)nc23)n1 10.1021/jm0109614
CHEMBL352707 120299 None 0 Human Binding pKi = 7.5 7.5 3 4
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 26-45Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 26-45
ChEMBL 484 6 2 8 5.5 CCCCn1cc2c(nc(NC(=O)Nc3ccc(Cl)c(Cl)c3)n3nc(-c4ccco4)nc23)n1 10.1021/jm0109614
2817165 188821 None 5 Human Binding pKi = 7.5 7.5 -91 3
Displacement of [3H]MRS1754 from human adenosine A2B receptor expressed in CHO cell membraneDisplacement of [3H]MRS1754 from human adenosine A2B receptor expressed in CHO cell membrane
ChEMBL 251 2 1 5 3.1 N#Cc1c(-c2ccco2)cc(-c2ccco2)nc1N 10.1021/jm701594y
CHEMBL506250 188821 None 5 Human Binding pKi = 7.5 7.5 -91 3
Displacement of [3H]MRS1754 from human adenosine A2B receptor expressed in CHO cell membraneDisplacement of [3H]MRS1754 from human adenosine A2B receptor expressed in CHO cell membrane
ChEMBL 251 2 1 5 3.1 N#Cc1c(-c2ccco2)cc(-c2ccco2)nc1N 10.1021/jm701594y
11524637 78087 None 0 Human Binding pKi = 7.5 7.5 -1 3
Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cellsDisplacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells
ChEMBL 422 8 1 8 2.6 CCCn1c(=O)c2nc(-c3cnn(Cc4cccc(OC)c4)c3)[nH]c2n(CCC)c1=O 10.1021/jm051268+
CHEMBL210150 78087 None 0 Human Binding pKi = 7.5 7.5 -1 3
Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cellsDisplacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells
ChEMBL 422 8 1 8 2.6 CCCn1c(=O)c2nc(-c3cnn(Cc4cccc(OC)c4)c3)[nH]c2n(CCC)c1=O 10.1021/jm051268+
2690 903 None 66 Human Binding pKi = 7.5 7.5 -30 9
Displacement of [3H]MRS-1754 from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]MRS-1754 from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 285 1 1 6 2.8 Clc1ccc2c(c1)c1nc(nn1c(n2)N)c1ccco1 10.1021/jm900413e
384 903 None 66 Human Binding pKi = 7.5 7.5 -30 9
Displacement of [3H]MRS-1754 from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]MRS-1754 from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 285 1 1 6 2.8 Clc1ccc2c(c1)c1nc(nn1c(n2)N)c1ccco1 10.1021/jm900413e
CHEMBL16687 903 None 66 Human Binding pKi = 7.5 7.5 -30 9
Displacement of [3H]MRS-1754 from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]MRS-1754 from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 285 1 1 6 2.8 Clc1ccc2c(c1)c1nc(nn1c(n2)N)c1ccco1 10.1021/jm900413e
10563436 135230 None 0 Human Binding pKi = 7.5 7.5 -3 3
Inhibition of [3H]ZM-241385 binding to human adenosine A2B receptorInhibition of [3H]ZM-241385 binding to human adenosine A2B receptor
ChEMBL 262 3 2 4 1.5 CCCn1c(=O)[nH]c2[nH]c(C3CCCC3)nc2c1=O 10.1021/jm011049y
CHEMBL37243 135230 None 0 Human Binding pKi = 7.5 7.5 -3 3
Inhibition of [3H]ZM-241385 binding to human adenosine A2B receptorInhibition of [3H]ZM-241385 binding to human adenosine A2B receptor
ChEMBL 262 3 2 4 1.5 CCCn1c(=O)[nH]c2[nH]c(C3CCCC3)nc2c1=O 10.1021/jm011049y
CHEMBL5088749 215176 None 0 Human Binding pKi = 7.5 7.5 -11 3
Displacement of [3H]DPCPX from human A2BAR expressed in HEK293 cell membrane incubated for 30 mins by microbeta trilux scintillation counter analysisDisplacement of [3H]DPCPX from human A2BAR expressed in HEK293 cell membrane incubated for 30 mins by microbeta trilux scintillation counter analysis
ChEMBL None None None CNc1nc(-c2ccccc2)c(C#N)c(-c2cccc(C#N)c2)n1 10.1021/acs.jmedchem.1c01636
11656950 72284 None 0 Human Binding pKi = 7.5 7.5 2 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 557 10 2 8 4.6 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(C5=NC(C)(C)CO5)cc4)cc3)cc2n(CCC)c1=O 10.1021/jm0506221
CHEMBL198294 72284 None 0 Human Binding pKi = 7.5 7.5 2 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 557 10 2 8 4.6 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(C5=NC(C)(C)CO5)cc4)cc3)cc2n(CCC)c1=O 10.1021/jm0506221
11569133 72612 None 0 Human Binding pKi = 7.5 7.5 1 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 476 9 3 7 3.7 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(O)cc4)cc3)cc2n(CCC)c1=O 10.1021/jm0506221
CHEMBL199399 72612 None 0 Human Binding pKi = 7.5 7.5 1 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 476 9 3 7 3.7 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(O)cc4)cc3)cc2n(CCC)c1=O 10.1021/jm0506221
156019760 177948 None 0 Human Binding pKi = 6.5 6.5 -40 2
Displacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting methodDisplacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting method
ChEMBL 337 3 2 6 3.0 CC1=C(C(=O)OC(C)C)C(c2cn[nH]c2)n2c(nc3ccccc32)N1 10.1021/acs.jmedchem.0c00564
CHEMBL4645687 177948 None 0 Human Binding pKi = 6.5 6.5 -40 2
Displacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting methodDisplacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting method
ChEMBL 337 3 2 6 3.0 CC1=C(C(=O)OC(C)C)C(c2cn[nH]c2)n2c(nc3ccccc32)N1 10.1021/acs.jmedchem.0c00564
145986838 167083 None 0 Human Binding pKi = 6.5 6.5 -2 3
Displacement of [3H]PSB-602 from human adenosine A2B receptor expressed in CHO cell membranesDisplacement of [3H]PSB-602 from human adenosine A2B receptor expressed in CHO cell membranes
ChEMBL 581 16 1 10 2.9 CCCn1c(=O)c2c(nc3n2CCCN3CCc2ccc(OCC(=O)NCCCN(CC)CC)cc2)n(CCC)c1=O 10.1039/C8MD00070K
CHEMBL4289660 167083 None 0 Human Binding pKi = 6.5 6.5 -2 3
Displacement of [3H]PSB-602 from human adenosine A2B receptor expressed in CHO cell membranesDisplacement of [3H]PSB-602 from human adenosine A2B receptor expressed in CHO cell membranes
ChEMBL 581 16 1 10 2.9 CCCn1c(=O)c2c(nc3n2CCCN3CCc2ccc(OCC(=O)NCCCN(CC)CC)cc2)n(CCC)c1=O 10.1039/C8MD00070K
135465784 162862 None 0 Human Binding pKi = 6.5 6.5 - 1
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 495 9 3 10 2.0 CCCn1c(=O)c2nc(-c3cc(NC(=O)Cc4ccc(O)c(OC)c4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
CHEMBL417312 162862 None 0 Human Binding pKi = 6.5 6.5 - 1
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 495 9 3 10 2.0 CCCn1c(=O)c2nc(-c3cc(NC(=O)Cc4ccc(O)c(OC)c4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
72546540 103841 None 1 Human Binding pKi = 5.5 5.5 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by Scatchard plot analysisDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by Scatchard plot analysis
ChEMBL 248 3 1 5 1.5 CCOC(=O)c1c(-c2ccco2)nc(=O)[nH]c1C 10.1021/ml400185v
CHEMBL3091695 103841 None 1 Human Binding pKi = 5.5 5.5 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by Scatchard plot analysisDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by Scatchard plot analysis
ChEMBL 248 3 1 5 1.5 CCOC(=O)c1c(-c2ccco2)nc(=O)[nH]c1C 10.1021/ml400185v
137652737 158589 None 0 Human Binding pKi = 6.5 6.5 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes after 30 minsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes after 30 mins
ChEMBL 304 3 2 5 2.0 CC1=C(C(=O)OC(C)C)C(c2cccs2)N/C(=N/C#N)N1 10.1021/acs.jmedchem.7b00138
CHEMBL4092030 158589 None 0 Human Binding pKi = 6.5 6.5 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes after 30 minsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes after 30 mins
ChEMBL 304 3 2 5 2.0 CC1=C(C(=O)OC(C)C)C(c2cccs2)N/C(=N/C#N)N1 10.1021/acs.jmedchem.7b00138
CHEMBL5076343 214429 None 3 Human Binding pKi = 6.5 6.5 -158 3
Displacement of [3H]DPCPX from human adenosine A2B receptor membrane (unknown origin) measured after 60 mins by scintillation counting analysisDisplacement of [3H]DPCPX from human adenosine A2B receptor membrane (unknown origin) measured after 60 mins by scintillation counting analysis
ChEMBL None None None Nc1ccccc1NC(=O)c1ccc(CCn2ncc3c2nc(N)n2nc(-c4ccco4)nc32)cc1 10.1021/acs.jmedchem.1c01155
135493268 110486 None 0 Human Binding pKi = 7.5 7.5 25 2
Binding affinity of compound for displacement of [3H]DPCPX binding in HEK293 membranes expressing human A2B adenosine receptorsBinding affinity of compound for displacement of [3H]DPCPX binding in HEK293 membranes expressing human A2B adenosine receptors
ChEMBL 449 8 2 8 2.3 CCCn1c(=O)c2nc(-c3cc(NC(=O)Cc4ccccc4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
CHEMBL32481 110486 None 0 Human Binding pKi = 7.5 7.5 25 2
Binding affinity of compound for displacement of [3H]DPCPX binding in HEK293 membranes expressing human A2B adenosine receptorsBinding affinity of compound for displacement of [3H]DPCPX binding in HEK293 membranes expressing human A2B adenosine receptors
ChEMBL 449 8 2 8 2.3 CCCn1c(=O)c2nc(-c3cc(NC(=O)Cc4ccccc4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
135493268 110486 None 0 Human Binding pKi = 7.5 7.5 25 2
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 449 8 2 8 2.3 CCCn1c(=O)c2nc(-c3cc(NC(=O)Cc4ccccc4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
CHEMBL32481 110486 None 0 Human Binding pKi = 7.5 7.5 25 2
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 449 8 2 8 2.3 CCCn1c(=O)c2nc(-c3cc(NC(=O)Cc4ccccc4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
10926253 81058 None 0 Human Binding pKi = 7.5 7.5 1 3
Displacement of [3H]- DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]- DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 353 2 1 10 0.6 CN1CCN(c2c3c(nc(N)n4nc(-c5ccco5)nc34)nn2C)CC1 10.1021/jm021023m
CHEMBL21541 81058 None 0 Human Binding pKi = 7.5 7.5 1 3
Displacement of [3H]- DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]- DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 353 2 1 10 0.6 CN1CCN(c2c3c(nc(N)n4nc(-c5ccco5)nc34)nn2C)CC1 10.1021/jm021023m
CHEMBL553587 81058 None 0 Human Binding pKi = 7.5 7.5 1 3
Displacement of [3H]- DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]- DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 353 2 1 10 0.6 CN1CCN(c2c3c(nc(N)n4nc(-c5ccco5)nc34)nn2C)CC1 10.1021/jm021023m
11733496 24905 None 0 Human Binding pKi = 7.5 7.5 1 4
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 477 8 1 8 4.5 O=C(Cc1ccccc1)Nc1nc2nn(CCCc3ccccc3)cc2c2nc(-c3ccco3)nn12 10.1021/jm030852k
CHEMBL134566 24905 None 0 Human Binding pKi = 7.5 7.5 1 4
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 477 8 1 8 4.5 O=C(Cc1ccccc1)Nc1nc2nn(CCCc3ccccc3)cc2c2nc(-c3ccco3)nn12 10.1021/jm030852k
10994216 194919 None 0 Human Binding pKi = 7.5 7.5 -2 4
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 463 7 1 8 4.2 O=C(Cc1ccccc1)Nc1nc2nn(CCc3ccccc3)cc2c2nc(-c3ccco3)nn12 10.1021/jm030852k
CHEMBL541455 194919 None 0 Human Binding pKi = 7.5 7.5 -2 4
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 463 7 1 8 4.2 O=C(Cc1ccccc1)Nc1nc2nn(CCc3ccccc3)cc2c2nc(-c3ccco3)nn12 10.1021/jm030852k
44587955 188947 None 0 Human Binding pKi = 7.5 7.5 11 2
Displacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cells
ChEMBL 397 7 2 8 1.8 CCCn1c(=O)c2[nH]c(-c3ccco3)c(OS(=O)(=O)O)c2n(CCC)c1=O 10.1016/j.bmc.2008.09.067
CHEMBL508090 188947 None 0 Human Binding pKi = 7.5 7.5 11 2
Displacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cells
ChEMBL 397 7 2 8 1.8 CCCn1c(=O)c2[nH]c(-c3ccco3)c(OS(=O)(=O)O)c2n(CCC)c1=O 10.1016/j.bmc.2008.09.067
136042342 71168 None 0 Human Binding pKi = 7.5 7.5 8 2
Displacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation countingDisplacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation counting
ChEMBL 479 9 2 10 2.8 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5cc(OC)ccc5[nH]4)no3)nc2n(CCC)c1=O 10.1021/jm201292w
CHEMBL1955918 71168 None 0 Human Binding pKi = 7.5 7.5 8 2
Displacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation countingDisplacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation counting
ChEMBL 479 9 2 10 2.8 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5cc(OC)ccc5[nH]4)no3)nc2n(CCC)c1=O 10.1021/jm201292w
135874415 95894 None 0 Human Binding pKi = 7.5 7.5 - 1
Displacement of [3H]MRE2029F20 from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]MRE2029F20 from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 527 8 2 8 3.3 CCCn1c(=O)c2[nH]c(-c3cc(C)n(CC(=O)Nc4ccc(Br)cc4)n3)nc2n(CCC)c1=O 10.1016/j.bmc.2007.11.058
CHEMBL259177 95894 None 0 Human Binding pKi = 7.5 7.5 - 1
Displacement of [3H]MRE2029F20 from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]MRE2029F20 from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 527 8 2 8 3.3 CCCn1c(=O)c2[nH]c(-c3cc(C)n(CC(=O)Nc4ccc(Br)cc4)n3)nc2n(CCC)c1=O 10.1016/j.bmc.2007.11.058
11956193 94577 None 9 Human Binding pKi = 7.5 7.5 -12 5
Displacement of [3H]MRS1754 from human adenosine A2B receptorDisplacement of [3H]MRS1754 from human adenosine A2B receptor
ChEMBL 367 5 1 8 1.1 CN1CCN(CC(=O)Nc2cc(-n3cccn3)nc(-c3ccco3)n2)CC1 10.1021/jm070623o
CHEMBL251975 94577 None 9 Human Binding pKi = 7.5 7.5 -12 5
Displacement of [3H]MRS1754 from human adenosine A2B receptorDisplacement of [3H]MRS1754 from human adenosine A2B receptor
ChEMBL 367 5 1 8 1.1 CN1CCN(CC(=O)Nc2cc(-n3cccn3)nc(-c3ccco3)n2)CC1 10.1021/jm070623o
24828457 96835 None 0 Human Binding pKi = 7.5 7.5 27 4
Displacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 396 6 1 7 2.4 CCCn1c(=O)c2[nH]c(-c3cnn(Cc4cccc(F)c4)c3)nc2n(CC)c1=O 10.1021/jm7014815
CHEMBL265213 96835 None 0 Human Binding pKi = 7.5 7.5 27 4
Displacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 396 6 1 7 2.4 CCCn1c(=O)c2[nH]c(-c3cnn(Cc4cccc(F)c4)c3)nc2n(CC)c1=O 10.1021/jm7014815
11647607 78094 None 0 Human Binding pKi = 7.5 7.5 4 3
Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cellsDisplacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells
ChEMBL 428 7 1 7 2.9 CCCn1c(=O)c2nc(-c3cnn(Cc4ccc(F)c(F)c4)c3)[nH]c2n(CCC)c1=O 10.1021/jm051268+
CHEMBL210212 78094 None 0 Human Binding pKi = 7.5 7.5 4 3
Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cellsDisplacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells
ChEMBL 428 7 1 7 2.9 CCCn1c(=O)c2nc(-c3cnn(Cc4ccc(F)c(F)c4)c3)[nH]c2n(CCC)c1=O 10.1021/jm051268+
1153 1628 None 58 Rat Binding pKi = 7.5 7.5 -5 10
Compound was tested for its binding affinity against Alpha-2 adrenergic receptorCompound was tested for its binding affinity against Alpha-2 adrenergic receptor
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1016/0960-894X(95)00413-N
12668023 1628 None 58 Rat Binding pKi = 7.5 7.5 -5 10
Compound was tested for its binding affinity against Alpha-2 adrenergic receptorCompound was tested for its binding affinity against Alpha-2 adrenergic receptor
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1016/0960-894X(95)00413-N
30026874 1628 None 58 Rat Binding pKi = 7.5 7.5 -5 10
Compound was tested for its binding affinity against Alpha-2 adrenergic receptorCompound was tested for its binding affinity against Alpha-2 adrenergic receptor
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1016/0960-894X(95)00413-N
30026875 1628 None 58 Rat Binding pKi = 7.5 7.5 -5 10
Compound was tested for its binding affinity against Alpha-2 adrenergic receptorCompound was tested for its binding affinity against Alpha-2 adrenergic receptor
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1016/0960-894X(95)00413-N
3341 1628 None 58 Rat Binding pKi = 7.5 7.5 -5 10
Compound was tested for its binding affinity against Alpha-2 adrenergic receptorCompound was tested for its binding affinity against Alpha-2 adrenergic receptor
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1016/0960-894X(95)00413-N
3341.0 1628 None 58 Rat Binding pKi = 7.5 7.5 -5 10
Compound was tested for its binding affinity against Alpha-2 adrenergic receptorCompound was tested for its binding affinity against Alpha-2 adrenergic receptor
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1016/0960-894X(95)00413-N
6603851 1628 None 58 Rat Binding pKi = 7.5 7.5 -5 10
Compound was tested for its binding affinity against Alpha-2 adrenergic receptorCompound was tested for its binding affinity against Alpha-2 adrenergic receptor
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1016/0960-894X(95)00413-N
933 1628 None 58 Rat Binding pKi = 7.5 7.5 -5 10
Compound was tested for its binding affinity against Alpha-2 adrenergic receptorCompound was tested for its binding affinity against Alpha-2 adrenergic receptor
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1016/0960-894X(95)00413-N
939 1628 None 58 Rat Binding pKi = 7.5 7.5 -5 10
Compound was tested for its binding affinity against Alpha-2 adrenergic receptorCompound was tested for its binding affinity against Alpha-2 adrenergic receptor
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1016/0960-894X(95)00413-N
985 1628 None 58 Rat Binding pKi = 7.5 7.5 -5 10
Compound was tested for its binding affinity against Alpha-2 adrenergic receptorCompound was tested for its binding affinity against Alpha-2 adrenergic receptor
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1016/0960-894X(95)00413-N
CHEMBL1160786 1628 None 58 Rat Binding pKi = 7.5 7.5 -5 10
Compound was tested for its binding affinity against Alpha-2 adrenergic receptorCompound was tested for its binding affinity against Alpha-2 adrenergic receptor
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1016/0960-894X(95)00413-N
CHEMBL1161520 1628 None 58 Rat Binding pKi = 7.5 7.5 -5 10
Compound was tested for its binding affinity against Alpha-2 adrenergic receptorCompound was tested for its binding affinity against Alpha-2 adrenergic receptor
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1016/0960-894X(95)00413-N
CHEMBL588 1628 None 58 Rat Binding pKi = 7.5 7.5 -5 10
Compound was tested for its binding affinity against Alpha-2 adrenergic receptorCompound was tested for its binding affinity against Alpha-2 adrenergic receptor
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1016/0960-894X(95)00413-N
DB00800 1628 None 58 Rat Binding pKi = 7.5 7.5 -5 10
Compound was tested for its binding affinity against Alpha-2 adrenergic receptorCompound was tested for its binding affinity against Alpha-2 adrenergic receptor
ChEMBL 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O 10.1016/0960-894X(95)00413-N
46227951 199945 None 0 Human Binding pKi = 7.5 7.5 2 3
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 396 6 0 8 2.6 Cn1c(Cc2cccs2)nc2c1c(=O)n(CC1CC1)c(=O)n2Cc1ccco1 10.1016/j.bmc.2009.07.034
CHEMBL594963 199945 None 0 Human Binding pKi = 7.5 7.5 2 3
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 396 6 0 8 2.6 Cn1c(Cc2cccs2)nc2c1c(=O)n(CC1CC1)c(=O)n2Cc1ccco1 10.1016/j.bmc.2009.07.034
46233377 201258 None 0 Human Binding pKi = 7.5 7.5 2 3
Displacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells by microplate beta scintillation counterDisplacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells by microplate beta scintillation counter
ChEMBL 386 5 0 8 2.7 CCn1c(=O)c2c(nc(Cc3cccs3)n2C)n(Cc2cccs2)c1=O 10.1016/j.bmc.2010.01.028
CHEMBL603878 201258 None 0 Human Binding pKi = 7.5 7.5 2 3
Displacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells by microplate beta scintillation counterDisplacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells by microplate beta scintillation counter
ChEMBL 386 5 0 8 2.7 CCn1c(=O)c2c(nc(Cc3cccs3)n2C)n(Cc2cccs2)c1=O 10.1016/j.bmc.2010.01.028
135423046 37704 None 0 Human Binding pKi = 6.5 6.5 -77 4
Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 332-369Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 332-369
ChEMBL 390 4 3 8 2.9 COc1ccc(NC(=O)Nc2nc3n[nH]cc3c3nc(-c4ccco4)nn23)cc1 10.1021/jm001047y
CHEMBL145767 37704 None 0 Human Binding pKi = 6.5 6.5 -77 4
Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 332-369Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 332-369
ChEMBL 390 4 3 8 2.9 COc1ccc(NC(=O)Nc2nc3n[nH]cc3c3nc(-c4ccco4)nn23)cc1 10.1021/jm001047y
11642231 77493 None 0 Human Binding pKi = 6.5 6.5 - 1
Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cellsDisplacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells
ChEMBL 528 7 1 7 4.7 CCCn1c(=O)c2nc(-c3cnn(Cc4cc(C(F)(F)F)cc(C(F)(F)F)c4)c3)[nH]c2n(CCC)c1=O 10.1021/jm051268+
CHEMBL208723 77493 None 0 Human Binding pKi = 6.5 6.5 - 1
Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cellsDisplacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells
ChEMBL 528 7 1 7 4.7 CCCn1c(=O)c2nc(-c3cnn(Cc4cc(C(F)(F)F)cc(C(F)(F)F)c4)c3)[nH]c2n(CCC)c1=O 10.1021/jm051268+
135633268 138974 None 8 Human Binding pKi = 6.5 6.5 - 1
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 minsDisplacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 mins
ChEMBL 288 3 1 7 2.1 CC1=C(C(=O)OC(C)C)C(c2ccoc2)n2ncnc2N1 10.1021/acs.jmedchem.5b01586
CHEMBL3785325 138974 None 8 Human Binding pKi = 6.5 6.5 - 1
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 minsDisplacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 mins
ChEMBL 288 3 1 7 2.1 CC1=C(C(=O)OC(C)C)C(c2ccoc2)n2ncnc2N1 10.1021/acs.jmedchem.5b01586
5613 3685 None 35 Human Binding pKi = 6.5 6.5 -45 4
Inhibition of human recombinant adenosine receptor A2bInhibition of human recombinant adenosine receptor A2b
ChEMBL 272 4 1 8 0.9 CCCCc1nc(N)c2c(n1)n(C)c(n2)n1nccn1 10.1021/jm4011669
9860294 3685 None 35 Human Binding pKi = 6.5 6.5 -45 4
Inhibition of human recombinant adenosine receptor A2bInhibition of human recombinant adenosine receptor A2b
ChEMBL 272 4 1 8 0.9 CCCCc1nc(N)c2c(n1)n(C)c(n2)n1nccn1 10.1021/jm4011669
CHEMBL197669 3685 None 35 Human Binding pKi = 6.5 6.5 -45 4
Inhibition of human recombinant adenosine receptor A2bInhibition of human recombinant adenosine receptor A2b
ChEMBL 272 4 1 8 0.9 CCCCc1nc(N)c2c(n1)n(C)c(n2)n1nccn1 10.1021/jm4011669
5613 3685 None 35 Human Binding pKi = 6.5 6.5 -45 4
Binding affinity towards human Adenosine A2b receptor expressed in HEK293 cells using 5 nM [3H]DPCPXBinding affinity towards human Adenosine A2b receptor expressed in HEK293 cells using 5 nM [3H]DPCPX
ChEMBL 272 4 1 8 0.9 CCCCc1nc(N)c2c(n1)n(C)c(n2)n1nccn1 10.1021/jm058018d
9860294 3685 None 35 Human Binding pKi = 6.5 6.5 -45 4
Binding affinity towards human Adenosine A2b receptor expressed in HEK293 cells using 5 nM [3H]DPCPXBinding affinity towards human Adenosine A2b receptor expressed in HEK293 cells using 5 nM [3H]DPCPX
ChEMBL 272 4 1 8 0.9 CCCCc1nc(N)c2c(n1)n(C)c(n2)n1nccn1 10.1021/jm058018d
CHEMBL197669 3685 None 35 Human Binding pKi = 6.5 6.5 -45 4
Binding affinity towards human Adenosine A2b receptor expressed in HEK293 cells using 5 nM [3H]DPCPXBinding affinity towards human Adenosine A2b receptor expressed in HEK293 cells using 5 nM [3H]DPCPX
ChEMBL 272 4 1 8 0.9 CCCCc1nc(N)c2c(n1)n(C)c(n2)n1nccn1 10.1021/jm058018d
72697652 104016 None 0 Human Binding pKi = 5.5 5.5 -26 5
Displacement of [3H]PSB-603 from human adenosine A2B receptorDisplacement of [3H]PSB-603 from human adenosine A2B receptor
ChEMBL 349 3 0 7 0.9 C#CCn1c(=O)c2c(nc3n2CCCN3Cc2ccccc2)n(C)c1=O 10.1016/j.bmc.2013.09.044
CHEMBL3093310 104016 None 0 Human Binding pKi = 5.5 5.5 -26 5
Displacement of [3H]PSB-603 from human adenosine A2B receptorDisplacement of [3H]PSB-603 from human adenosine A2B receptor
ChEMBL 349 3 0 7 0.9 C#CCn1c(=O)c2c(nc3n2CCCN3Cc2ccccc2)n(C)c1=O 10.1016/j.bmc.2013.09.044
10254700 203526 None 6 Human Binding pKi = 5.5 5.5 -478 8
Displacement of [3H]- ZM-241385 from human adenosine A2B receptor expressed in HEK cellsDisplacement of [3H]- ZM-241385 from human adenosine A2B receptor expressed in HEK cells
ChEMBL 483 5 4 9 0.7 OC[C@H]1O[C@@H](n2cnc3c(NCc4cccc(I)c4)ncnc32)[C@H](O)[C@@H]1O 10.1021/jm9905965
CHEMBL66393 203526 None 6 Human Binding pKi = 5.5 5.5 -478 8
Displacement of [3H]- ZM-241385 from human adenosine A2B receptor expressed in HEK cellsDisplacement of [3H]- ZM-241385 from human adenosine A2B receptor expressed in HEK cells
ChEMBL 483 5 4 9 0.7 OC[C@H]1O[C@@H](n2cnc3c(NCc4cccc(I)c4)ncnc32)[C@H](O)[C@@H]1O 10.1021/jm9905965
CHEMBL5078609 214569 None 0 Human Binding pKi = 6.5 6.5 -12 2
Displacement of [3H]DPCPX from human A2BAR expressed in HEK293 cell membrane incubated for 30 mins by microbeta trilux scintillation counter analysisDisplacement of [3H]DPCPX from human A2BAR expressed in HEK293 cell membrane incubated for 30 mins by microbeta trilux scintillation counter analysis
ChEMBL None None None CNc1nc(-c2ccccc2)c(C#N)c(-c2cccc(F)c2)n1 10.1021/acs.jmedchem.1c01636
135443359 490 None 0 Human Binding pKi = 7.4 7.4 - 1
Binding affinity of compound for displacement of [3H]DPCPX binding in HEK293 membranes expressing human A2B adenosine receptorsBinding affinity of compound for displacement of [3H]DPCPX binding in HEK293 membranes expressing human A2B adenosine receptors
ChEMBL 509 9 3 11 -0.1 CCCn1c2=N/C(=c\3/cc([nH]n3C)OCC(=O)Nc3ccc(cc3)C(=O)O)/N=c2c(=O)n(c1=O)CCC 10.1021/jm0309654
441 490 None 0 Human Binding pKi = 7.4 7.4 - 1
Binding affinity of compound for displacement of [3H]DPCPX binding in HEK293 membranes expressing human A2B adenosine receptorsBinding affinity of compound for displacement of [3H]DPCPX binding in HEK293 membranes expressing human A2B adenosine receptors
ChEMBL 509 9 3 11 -0.1 CCCn1c2=N/C(=c\3/cc([nH]n3C)OCC(=O)Nc3ccc(cc3)C(=O)O)/N=c2c(=O)n(c1=O)CCC 10.1021/jm0309654
CHEMBL431703 490 None 0 Human Binding pKi = 7.4 7.4 - 1
Binding affinity of compound for displacement of [3H]DPCPX binding in HEK293 membranes expressing human A2B adenosine receptorsBinding affinity of compound for displacement of [3H]DPCPX binding in HEK293 membranes expressing human A2B adenosine receptors
ChEMBL 509 9 3 11 -0.1 CCCn1c2=N/C(=c\3/cc([nH]n3C)OCC(=O)Nc3ccc(cc3)C(=O)O)/N=c2c(=O)n(c1=O)CCC 10.1021/jm0309654
135443359 490 None 0 Human Binding pKi = 7.4 7.4 - 1
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 509 9 3 11 -0.1 CCCn1c2=N/C(=c\3/cc([nH]n3C)OCC(=O)Nc3ccc(cc3)C(=O)O)/N=c2c(=O)n(c1=O)CCC 10.1021/jm0309654
441 490 None 0 Human Binding pKi = 7.4 7.4 - 1
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 509 9 3 11 -0.1 CCCn1c2=N/C(=c\3/cc([nH]n3C)OCC(=O)Nc3ccc(cc3)C(=O)O)/N=c2c(=O)n(c1=O)CCC 10.1021/jm0309654
CHEMBL431703 490 None 0 Human Binding pKi = 7.4 7.4 - 1
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 509 9 3 11 -0.1 CCCn1c2=N/C(=c\3/cc([nH]n3C)OCC(=O)Nc3ccc(cc3)C(=O)O)/N=c2c(=O)n(c1=O)CCC 10.1021/jm0309654
10859484 77658 None 0 Human Binding pKi = 7.4 7.4 -5 4
Displacement of [3H]- DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]- DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 298 3 2 9 1.3 CCNc1c2c(nc(N)n3nc(-c4ccco4)nc23)nn1C 10.1021/jm021023m
CHEMBL20888 77658 None 0 Human Binding pKi = 7.4 7.4 -5 4
Displacement of [3H]- DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]- DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 298 3 2 9 1.3 CCNc1c2c(nc(N)n3nc(-c4ccco4)nc23)nn1C 10.1021/jm021023m
CHEMBL544678 77658 None 0 Human Binding pKi = 7.4 7.4 -5 4
Displacement of [3H]- DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]- DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 298 3 2 9 1.3 CCNc1c2c(nc(N)n3nc(-c4ccco4)nc23)nn1C 10.1021/jm021023m
11560510 139014 None 0 Human Binding pKi = 7.4 7.4 1 3
Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cellsDisplacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells
ChEMBL 406 7 1 7 2.9 CCCn1c(=O)c2nc(-c3cnn(Cc4cccc(C)c4)c3)[nH]c2n(CCC)c1=O 10.1021/jm051268+
CHEMBL378570 139014 None 0 Human Binding pKi = 7.4 7.4 1 3
Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cellsDisplacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells
ChEMBL 406 7 1 7 2.9 CCCn1c(=O)c2nc(-c3cnn(Cc4cccc(C)c4)c3)[nH]c2n(CCC)c1=O 10.1021/jm051268+
44307827 203520 None 0 Human Binding pKi = 7.4 7.4 1 2
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 369 6 2 6 2.3 CCCn1c(=O)c2nc(-c3ccc(NC(C)=O)cc3)[nH]c2n(CCC)c1=O 10.1021/jm0104318
CHEMBL66337 203520 None 0 Human Binding pKi = 7.4 7.4 1 2
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 369 6 2 6 2.3 CCCn1c(=O)c2nc(-c3ccc(NC(C)=O)cc3)[nH]c2n(CCC)c1=O 10.1021/jm0104318
CHEMBL5088622 215165 None 0 Human Binding pKi = 7.4 7.4 -5 7
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells by liquid scintillation counting analysisDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells by liquid scintillation counting analysis
ChEMBL None None None Nc1nc(-c2ccccc2)c2c(n1)-c1cc(OCCCN3CCCC3)ccc1C2 10.1021/acs.jmedchem.0c00914
128525 154724 None 10 Human Binding pKi = 6.4 6.4 5 6
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 194 2 2 4 -0.2 CCCn1c(=O)[nH]c2[nH]cnc2c1=O 10.1021/jm0104318
CHEMBL39986 154724 None 10 Human Binding pKi = 6.4 6.4 5 6
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 194 2 2 4 -0.2 CCCn1c(=O)[nH]c2[nH]cnc2c1=O 10.1021/jm0104318
11713241 78236 None 0 Human Binding pKi = 6.4 6.4 - 1
Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cellsDisplacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells
ChEMBL 512 7 1 7 4.4 CCCn1c(=O)c2nc(-c3cnn(Cc4cc(C(F)(F)F)cc(Cl)c4F)c3)[nH]c2n(CCC)c1=O 10.1021/jm051268+
CHEMBL210614 78236 None 0 Human Binding pKi = 6.4 6.4 - 1
Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cellsDisplacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells
ChEMBL 512 7 1 7 4.4 CCCn1c(=O)c2nc(-c3cnn(Cc4cc(C(F)(F)F)cc(Cl)c4F)c3)[nH]c2n(CCC)c1=O 10.1021/jm051268+
71681203 90208 None 0 Human Binding pKi = 6.4 6.4 -10 5
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells after 75 mins by liquid scintillation counting analysisDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells after 75 mins by liquid scintillation counting analysis
ChEMBL 330 5 1 5 3.7 O=C(CCCc1ccccc1)Nc1nc2sccc2c(=O)s1 10.1021/jm400336x
CHEMBL2382425 90208 None 0 Human Binding pKi = 6.4 6.4 -10 5
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells after 75 mins by liquid scintillation counting analysisDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells after 75 mins by liquid scintillation counting analysis
ChEMBL 330 5 1 5 3.7 O=C(CCCc1ccccc1)Nc1nc2sccc2c(=O)s1 10.1021/jm400336x
71683091 89937 None 0 Human Binding pKi = 6.4 6.4 -4 6
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells after 75 mins by liquid scintillation counting analysisDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells after 75 mins by liquid scintillation counting analysis
ChEMBL 310 4 1 4 3.2 O=C(CCc1ccccc1)Nc1nc2ccccc2c(=O)s1 10.1021/jm400336x
CHEMBL2380385 89937 None 0 Human Binding pKi = 6.4 6.4 -4 6
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells after 75 mins by liquid scintillation counting analysisDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells after 75 mins by liquid scintillation counting analysis
ChEMBL 310 4 1 4 3.2 O=C(CCc1ccccc1)Nc1nc2ccccc2c(=O)s1 10.1021/jm400336x
52945064 19091 None 0 Human Binding pKi = 5.4 5.4 1 2
Displacement of [3H]ZM241385 from human adenosine A2B receptor transfected in CHO cells after 60 mins by scintillation countingDisplacement of [3H]ZM241385 from human adenosine A2B receptor transfected in CHO cells after 60 mins by scintillation counting
ChEMBL 538 9 1 4 6.0 Cn1c(=O)c(-c2ccc(F)cc2F)c(CCc2ccccc2)c2cc(OCC(=O)NCc3ccccc3)ccc21 10.1016/j.bmcl.2010.10.030
CHEMBL1289108 19091 None 0 Human Binding pKi = 5.4 5.4 1 2
Displacement of [3H]ZM241385 from human adenosine A2B receptor transfected in CHO cells after 60 mins by scintillation countingDisplacement of [3H]ZM241385 from human adenosine A2B receptor transfected in CHO cells after 60 mins by scintillation counting
ChEMBL 538 9 1 4 6.0 Cn1c(=O)c(-c2ccc(F)cc2F)c(CCc2ccccc2)c2cc(OCC(=O)NCc3ccccc3)ccc21 10.1016/j.bmcl.2010.10.030
21958639 64303 None 0 Human Binding pKi = 5.4 5.4 - 1
Binding affinity for adenosine A2b receptor by using as [3H]ZM-241385 (14 nM) radioligand in membranes from HEK-A2B cellsBinding affinity for adenosine A2b receptor by using as [3H]ZM-241385 (14 nM) radioligand in membranes from HEK-A2B cells
ChEMBL 520 9 1 9 4.7 CCCn1c(=O)c2nc(-c3ccc(OCc4noc(-c5ccc(Cl)cc5)n4)cc3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2004.11.044
CHEMBL181062 64303 None 0 Human Binding pKi = 5.4 5.4 - 1
Binding affinity for adenosine A2b receptor by using as [3H]ZM-241385 (14 nM) radioligand in membranes from HEK-A2B cellsBinding affinity for adenosine A2b receptor by using as [3H]ZM-241385 (14 nM) radioligand in membranes from HEK-A2B cells
ChEMBL 520 9 1 9 4.7 CCCn1c(=O)c2nc(-c3ccc(OCc4noc(-c5ccc(Cl)cc5)n4)cc3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2004.11.044
11386951 66885 None 0 Human Binding pKi = 5.4 5.4 -75 3
Inhibition of [3H]DPCPX binding to human adenosine A2B receptor expressed in HEK293 cellsInhibition of [3H]DPCPX binding to human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 527 9 5 16 -0.7 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(N[C@H](CO)Cc5ccc([N+](=O)[O-])cc5)nc43)[C@H](O)[C@@H]2O)n1 10.1021/jm031143+
CHEMBL186403 66885 None 0 Human Binding pKi = 5.4 5.4 -75 3
Inhibition of [3H]DPCPX binding to human adenosine A2B receptor expressed in HEK293 cellsInhibition of [3H]DPCPX binding to human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 527 9 5 16 -0.7 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(N[C@H](CO)Cc5ccc([N+](=O)[O-])cc5)nc43)[C@H](O)[C@@H]2O)n1 10.1021/jm031143+
46880418 6339 None 0 Human Binding pKi = 5.4 5.4 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 281 4 1 4 2.7 CC(=O)c1nc(NC(=O)C2CC2)ccc1-c1ccncc1 10.1016/j.bmcl.2010.01.045
CHEMBL1082004 6339 None 0 Human Binding pKi = 5.4 5.4 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 281 4 1 4 2.7 CC(=O)c1nc(NC(=O)C2CC2)ccc1-c1ccncc1 10.1016/j.bmcl.2010.01.045
10379032 7521 None 0 Human Binding pKi = 7.4 7.4 4 4
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 282 3 1 5 1.3 C=CCn1c(=O)c2[nH]c(-c3ccccc3)nc2n(C)c1=O 10.1021/jm0104318
CHEMBL10873 7521 None 0 Human Binding pKi = 7.4 7.4 4 4
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 282 3 1 5 1.3 C=CCn1c(=O)c2[nH]c(-c3ccccc3)nc2n(C)c1=O 10.1021/jm0104318
10961304 76012 None 0 Human Binding pKi = 7.4 7.4 -2 4
Displacement of [3H]- DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]- DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 447 6 3 10 3.4 CCNc1c2c(nc(NC(=O)Nc3ccc(OC)cc3)n3nc(-c4ccco4)nc23)nn1C 10.1021/jm021023m
CHEMBL20555 76012 None 0 Human Binding pKi = 7.4 7.4 -2 4
Displacement of [3H]- DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]- DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 447 6 3 10 3.4 CCNc1c2c(nc(NC(=O)Nc3ccc(OC)cc3)n3nc(-c4ccco4)nc23)nn1C 10.1021/jm021023m
CHEMBL554955 76012 None 0 Human Binding pKi = 7.4 7.4 -2 4
Displacement of [3H]- DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]- DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 447 6 3 10 3.4 CCNc1c2c(nc(NC(=O)Nc3ccc(OC)cc3)n3nc(-c4ccco4)nc23)nn1C 10.1021/jm021023m
21958681 94561 None 0 Human Binding pKi = 7.4 7.4 40 4
Displacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranesDisplacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranes
ChEMBL 336 4 2 6 1.3 CCn1c(=O)[nH]c2nc(-c3cnn(Cc4ccccc4)c3)[nH]c2c1=O 10.1016/j.bmcl.2008.01.008
CHEMBL251873 94561 None 0 Human Binding pKi = 7.4 7.4 40 4
Displacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranesDisplacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranes
ChEMBL 336 4 2 6 1.3 CCn1c(=O)[nH]c2nc(-c3cnn(Cc4ccccc4)c3)[nH]c2c1=O 10.1016/j.bmcl.2008.01.008
52944930 19294 None 0 Human Binding pKi = 7.4 7.4 2 3
Displacement of [3H]ZM241385 from human adenosine A2B receptor transfected in CHO cells after 60 mins by scintillation countingDisplacement of [3H]ZM241385 from human adenosine A2B receptor transfected in CHO cells after 60 mins by scintillation counting
ChEMBL 495 9 2 5 5.1 O=C(COc1ccc2[nH]c(=O)c(-c3nccs3)c(CCc3ccccc3)c2c1)NCc1ccccc1 10.1016/j.bmcl.2010.10.030
CHEMBL1290436 19294 None 0 Human Binding pKi = 7.4 7.4 2 3
Displacement of [3H]ZM241385 from human adenosine A2B receptor transfected in CHO cells after 60 mins by scintillation countingDisplacement of [3H]ZM241385 from human adenosine A2B receptor transfected in CHO cells after 60 mins by scintillation counting
ChEMBL 495 9 2 5 5.1 O=C(COc1ccc2[nH]c(=O)c(-c3nccs3)c(CCc3ccccc3)c2c1)NCc1ccccc1 10.1016/j.bmcl.2010.10.030
11612320 77281 None 0 Human Binding pKi = 7.4 7.4 1 3
Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cellsDisplacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells
ChEMBL 460 7 1 7 3.6 CCCn1c(=O)c2nc(-c3cnn(Cc4ccccc4C(F)(F)F)c3)[nH]c2n(CCC)c1=O 10.1021/jm051268+
CHEMBL208110 77281 None 0 Human Binding pKi = 7.4 7.4 1 3
Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cellsDisplacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells
ChEMBL 460 7 1 7 3.6 CCCn1c(=O)c2nc(-c3cnn(Cc4ccccc4C(F)(F)F)c3)[nH]c2n(CCC)c1=O 10.1021/jm051268+
11633189 78257 None 0 Human Binding pKi = 7.4 7.4 1 3
Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cellsDisplacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells
ChEMBL 422 8 1 8 2.6 CCCn1c(=O)c2nc(-c3cnn(Cc4ccc(OC)cc4)c3)[nH]c2n(CCC)c1=O 10.1021/jm051268+
CHEMBL210683 78257 None 0 Human Binding pKi = 7.4 7.4 1 3
Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cellsDisplacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells
ChEMBL 422 8 1 8 2.6 CCCn1c(=O)c2nc(-c3cnn(Cc4ccc(OC)cc4)c3)[nH]c2n(CCC)c1=O 10.1021/jm051268+
11582578 140139 None 0 Human Binding pKi = 7.4 7.4 1 3
Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cellsDisplacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells
ChEMBL 422 8 1 8 2.6 CCCn1c(=O)c2nc(-c3cnn(Cc4ccccc4OC)c3)[nH]c2n(CCC)c1=O 10.1021/jm051268+
CHEMBL380219 140139 None 0 Human Binding pKi = 7.4 7.4 1 3
Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cellsDisplacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells
ChEMBL 422 8 1 8 2.6 CCCn1c(=O)c2nc(-c3cnn(Cc4ccccc4OC)c3)[nH]c2n(CCC)c1=O 10.1021/jm051268+
11656185 72596 None 0 Human Binding pKi = 7.4 7.4 1 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 494 9 2 6 4.6 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccccc4)cc3)c(Cl)c2n(CCC)c1=O 10.1021/jm0506221
CHEMBL199327 72596 None 0 Human Binding pKi = 7.4 7.4 1 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 494 9 2 6 4.6 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccccc4)cc3)c(Cl)c2n(CCC)c1=O 10.1021/jm0506221
155531922 171730 None 0 Human Binding pKi = 7.4 7.4 - 1
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 377 3 1 6 4.0 CCOC(=O)C1=C(C(F)(F)F)Nc2nc3ccccc3n2C1c1ccoc1 10.1016/j.ejmech.2021.113907
CHEMBL4467152 171730 None 0 Human Binding pKi = 7.4 7.4 - 1
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 377 3 1 6 4.0 CCOC(=O)C1=C(C(F)(F)F)Nc2nc3ccccc3n2C1c1ccoc1 10.1016/j.ejmech.2021.113907
155531922 171730 None 0 Human Binding pKi = 7.4 7.4 - 1
Displacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assayDisplacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assay
ChEMBL 377 3 1 6 4.0 CCOC(=O)C1=C(C(F)(F)F)Nc2nc3ccccc3n2C1c1ccoc1 10.1021/acs.jmedchem.9b01340
CHEMBL4467152 171730 None 0 Human Binding pKi = 7.4 7.4 - 1
Displacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assayDisplacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assay
ChEMBL 377 3 1 6 4.0 CCOC(=O)C1=C(C(F)(F)F)Nc2nc3ccccc3n2C1c1ccoc1 10.1021/acs.jmedchem.9b01340
135949027 178609 None 0 Human Binding pKi = 6.4 6.4 -9 3
Displacement of [3H]MRS1754 from human adenosine A2B receptor expressed in CHO cell membraneDisplacement of [3H]MRS1754 from human adenosine A2B receptor expressed in CHO cell membrane
ChEMBL 277 2 2 5 3.2 N#Cc1c(-c2ccc(O)cc2)cc(-c2ccco2)nc1N 10.1021/jm701594y
CHEMBL467366 178609 None 0 Human Binding pKi = 6.4 6.4 -9 3
Displacement of [3H]MRS1754 from human adenosine A2B receptor expressed in CHO cell membraneDisplacement of [3H]MRS1754 from human adenosine A2B receptor expressed in CHO cell membrane
ChEMBL 277 2 2 5 3.2 N#Cc1c(-c2ccc(O)cc2)cc(-c2ccco2)nc1N 10.1021/jm701594y
135433658 3207 None 3 Human Binding pKi = 5.4 5.4 -371 8
Displacement of [3H]PSB-603 from human adenosine receptor A2B expressed in CHO cell membranes incubated for 75 mins by radioligand competition assayDisplacement of [3H]PSB-603 from human adenosine receptor A2B expressed in CHO cell membranes incubated for 75 mins by radioligand competition assay
ChEMBL 295 2 1 3 2.5 CC[C@@H]1Cn2c(=N1)c1[nH]c(nc1n(c2=O)C)c1ccccc1 10.1016/j.ejmech.2019.111879
5620 3207 None 3 Human Binding pKi = 5.4 5.4 -371 8
Displacement of [3H]PSB-603 from human adenosine receptor A2B expressed in CHO cell membranes incubated for 75 mins by radioligand competition assayDisplacement of [3H]PSB-603 from human adenosine receptor A2B expressed in CHO cell membranes incubated for 75 mins by radioligand competition assay
ChEMBL 295 2 1 3 2.5 CC[C@@H]1Cn2c(=N1)c1[nH]c(nc1n(c2=O)C)c1ccccc1 10.1016/j.ejmech.2019.111879
9882625 3207 None 3 Human Binding pKi = 5.4 5.4 -371 8
Displacement of [3H]PSB-603 from human adenosine receptor A2B expressed in CHO cell membranes incubated for 75 mins by radioligand competition assayDisplacement of [3H]PSB-603 from human adenosine receptor A2B expressed in CHO cell membranes incubated for 75 mins by radioligand competition assay
ChEMBL 295 2 1 3 2.5 CC[C@@H]1Cn2c(=N1)c1[nH]c(nc1n(c2=O)C)c1ccccc1 10.1016/j.ejmech.2019.111879
CHEMBL1625681 3207 None 3 Human Binding pKi = 5.4 5.4 -371 8
Displacement of [3H]PSB-603 from human adenosine receptor A2B expressed in CHO cell membranes incubated for 75 mins by radioligand competition assayDisplacement of [3H]PSB-603 from human adenosine receptor A2B expressed in CHO cell membranes incubated for 75 mins by radioligand competition assay
ChEMBL 295 2 1 3 2.5 CC[C@@H]1Cn2c(=N1)c1[nH]c(nc1n(c2=O)C)c1ccccc1 10.1016/j.ejmech.2019.111879
135414399 78154 None 0 Human Binding pKi = 5.4 5.4 - 1
Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cellsDisplacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells
ChEMBL 330 5 1 7 1.4 CCCn1c(=O)c2nc(-c3cc(C)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm051268+
CHEMBL210389 78154 None 0 Human Binding pKi = 5.4 5.4 - 1
Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cellsDisplacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells
ChEMBL 330 5 1 7 1.4 CCCn1c(=O)c2nc(-c3cc(C)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm051268+
17198003 138978 None 2 Human Binding pKi = 6.4 6.4 - 1
Displacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting methodDisplacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting method
ChEMBL 353 3 1 6 4.3 CC1=C(C(=O)OC(C)C)C(c2cccs2)n2c(nc3ccccc32)N1 10.1021/acs.jmedchem.0c00564
CHEMBL3785353 138978 None 2 Human Binding pKi = 6.4 6.4 - 1
Displacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting methodDisplacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting method
ChEMBL 353 3 1 6 4.3 CC1=C(C(=O)OC(C)C)C(c2cccs2)n2c(nc3ccccc32)N1 10.1021/acs.jmedchem.0c00564
17198003 138978 None 2 Human Binding pKi = 6.4 6.4 - 1
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 minsDisplacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 mins
ChEMBL 353 3 1 6 4.3 CC1=C(C(=O)OC(C)C)C(c2cccs2)n2c(nc3ccccc32)N1 10.1021/acs.jmedchem.5b01586
CHEMBL3785353 138978 None 2 Human Binding pKi = 6.4 6.4 - 1
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 minsDisplacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 mins
ChEMBL 353 3 1 6 4.3 CC1=C(C(=O)OC(C)C)C(c2cccs2)n2c(nc3ccccc32)N1 10.1021/acs.jmedchem.5b01586
17198003 138978 None 2 Human Binding pKi = 6.4 6.4 - 1
Displacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assayDisplacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assay
ChEMBL 353 3 1 6 4.3 CC1=C(C(=O)OC(C)C)C(c2cccs2)n2c(nc3ccccc32)N1 10.1021/acs.jmedchem.9b01340
CHEMBL3785353 138978 None 2 Human Binding pKi = 6.4 6.4 - 1
Displacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assayDisplacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assay
ChEMBL 353 3 1 6 4.3 CC1=C(C(=O)OC(C)C)C(c2cccs2)n2c(nc3ccccc32)N1 10.1021/acs.jmedchem.9b01340
11553439 72685 None 0 Human Binding pKi = 6.4 6.4 5 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 415 9 1 8 1.7 CCOC(=O)COc1ccc(-c2cc3c([nH]2)c(=O)n(C)c(=O)n3CCCOC)cc1 10.1021/jm0506221
CHEMBL199664 72685 None 0 Human Binding pKi = 6.4 6.4 5 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 415 9 1 8 1.7 CCOC(=O)COc1ccc(-c2cc3c([nH]2)c(=O)n(C)c(=O)n3CCCOC)cc1 10.1021/jm0506221
46233347 200297 None 0 Human Binding pKi = 6.4 6.4 1 3
Displacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells by microplate beta scintillation counterDisplacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells by microplate beta scintillation counter
ChEMBL 380 5 0 7 2.6 CCn1c(=O)c2c(nc(Cc3cccs3)n2C)n(Cc2ccccc2)c1=O 10.1016/j.bmc.2010.01.028
CHEMBL597354 200297 None 0 Human Binding pKi = 6.4 6.4 1 3
Displacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells by microplate beta scintillation counterDisplacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells by microplate beta scintillation counter
ChEMBL 380 5 0 7 2.6 CCn1c(=O)c2c(nc(Cc3cccs3)n2C)n(Cc2ccccc2)c1=O 10.1016/j.bmc.2010.01.028
CHEMBL5088305 215151 None 0 Human Binding pKi = 6.4 6.4 1 4
Displacement of [3H]PSB-603 from human A2B receptor expressed in CHO cell membranes measured after 3 hrs by radioligand binding assayDisplacement of [3H]PSB-603 from human A2B receptor expressed in CHO cell membranes measured after 3 hrs by radioligand binding assay
ChEMBL None None None N#Cc1c(-c2ccccc2)cc(SCc2ncc[nH]2)nc1N 10.1021/acs.jmedchem.0c01856
10980845 137875 None 0 Human Binding pKi = 6.4 6.4 -2 2
Inhibition of [3H]ZM-241385 binding to human adenosine A2B receptorInhibition of [3H]ZM-241385 binding to human adenosine A2B receptor
ChEMBL 344 6 3 6 1.0 CCCn1c(=O)[nH]c2[nH]c(-c3ccc(OCC(=O)O)cc3)nc2c1=O 10.1021/jm011049y
CHEMBL37621 137875 None 0 Human Binding pKi = 6.4 6.4 -2 2
Inhibition of [3H]ZM-241385 binding to human adenosine A2B receptorInhibition of [3H]ZM-241385 binding to human adenosine A2B receptor
ChEMBL 344 6 3 6 1.0 CCCn1c(=O)[nH]c2[nH]c(-c3ccc(OCC(=O)O)cc3)nc2c1=O 10.1021/jm011049y
50940921 57233 None 0 Human Binding pKi = 6.4 6.4 -2 4
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 395 6 1 5 5.6 CCC(=O)Nc1nc(-c2ccc(SC)cc2)cc(-c2ccc(SC)cc2)n1 10.1021/jm100843z
CHEMBL1650152 57233 None 0 Human Binding pKi = 6.4 6.4 -2 4
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 395 6 1 5 5.6 CCC(=O)Nc1nc(-c2ccc(SC)cc2)cc(-c2ccc(SC)cc2)n1 10.1021/jm100843z
10475082 74 None 23 Human Binding pKi = 4.4 4.4 -1995 6
Binding affinity for human adenosine A2b receptor subtype expressed in CHO cellsBinding affinity for human adenosine A2b receptor subtype expressed in CHO cells
ChEMBL 383 4 4 9 0.8 OC[C@H]1O[C@H]([C@]([C@@H]1O)(C)O)n1cnc2c1nc(Cl)nc2NC1CCCC1 10.1021/jm049408n
5591 74 None 23 Human Binding pKi = 4.4 4.4 -1995 6
Binding affinity for human adenosine A2b receptor subtype expressed in CHO cellsBinding affinity for human adenosine A2b receptor subtype expressed in CHO cells
ChEMBL 383 4 4 9 0.8 OC[C@H]1O[C@H]([C@]([C@@H]1O)(C)O)n1cnc2c1nc(Cl)nc2NC1CCCC1 10.1021/jm049408n
CHEMBL251997 74 None 23 Human Binding pKi = 4.4 4.4 -1995 6
Binding affinity for human adenosine A2b receptor subtype expressed in CHO cellsBinding affinity for human adenosine A2b receptor subtype expressed in CHO cells
ChEMBL 383 4 4 9 0.8 OC[C@H]1O[C@H]([C@]([C@@H]1O)(C)O)n1cnc2c1nc(Cl)nc2NC1CCCC1 10.1021/jm049408n
135546657 157698 None 0 Human Binding pKi = 7.4 7.4 - 1
Binding affinity of compound for displacement of [3H]DPCPX binding in HEK293 membranes expressing human A2B adenosine receptorsBinding affinity of compound for displacement of [3H]DPCPX binding in HEK293 membranes expressing human A2B adenosine receptors
ChEMBL 509 10 2 10 2.3 CCCn1c(=O)c2[nH]c(-c3cc(NC(=O)Cc4ccc(OC)c(OC)c4)nn3C)nc2n(CCC)c1=O 10.1021/jm0309654
CHEMBL408186 157698 None 0 Human Binding pKi = 7.4 7.4 - 1
Binding affinity of compound for displacement of [3H]DPCPX binding in HEK293 membranes expressing human A2B adenosine receptorsBinding affinity of compound for displacement of [3H]DPCPX binding in HEK293 membranes expressing human A2B adenosine receptors
ChEMBL 509 10 2 10 2.3 CCCn1c(=O)c2[nH]c(-c3cc(NC(=O)Cc4ccc(OC)c(OC)c4)nn3C)nc2n(CCC)c1=O 10.1021/jm0309654
135546657 157698 None 0 Human Binding pKi = 7.4 7.4 - 1
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 509 10 2 10 2.3 CCCn1c(=O)c2[nH]c(-c3cc(NC(=O)Cc4ccc(OC)c(OC)c4)nn3C)nc2n(CCC)c1=O 10.1021/jm0309654
CHEMBL408186 157698 None 0 Human Binding pKi = 7.4 7.4 - 1
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 509 10 2 10 2.3 CCCn1c(=O)c2[nH]c(-c3cc(NC(=O)Cc4ccc(OC)c(OC)c4)nn3C)nc2n(CCC)c1=O 10.1021/jm0309654
135546657 157698 None 0 Human Binding pKi = 7.4 7.4 - 1
Displacement of [3H]MRE2029F20 from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]MRE2029F20 from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 509 10 2 10 2.3 CCCn1c(=O)c2[nH]c(-c3cc(NC(=O)Cc4ccc(OC)c(OC)c4)nn3C)nc2n(CCC)c1=O 10.1016/j.bmc.2007.11.058
CHEMBL408186 157698 None 0 Human Binding pKi = 7.4 7.4 - 1
Displacement of [3H]MRE2029F20 from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]MRE2029F20 from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 509 10 2 10 2.3 CCCn1c(=O)c2[nH]c(-c3cc(NC(=O)Cc4ccc(OC)c(OC)c4)nn3C)nc2n(CCC)c1=O 10.1016/j.bmc.2007.11.058
44406607 72703 None 0 Human Binding pKi = 7.4 7.4 8 4
Displacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cellsDisplacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cells
ChEMBL 494 8 1 10 3.3 CCCn1c(=O)c2nc(-c3cnn(Cc4noc(-c5ccccc5Cl)n4)c3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2005.10.002
CHEMBL199732 72703 None 0 Human Binding pKi = 7.4 7.4 8 4
Displacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cellsDisplacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cells
ChEMBL 494 8 1 10 3.3 CCCn1c(=O)c2nc(-c3cnn(Cc4noc(-c5ccccc5Cl)n4)c3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2005.10.002
21958536 167564 None 0 Human Binding pKi = 7.4 7.4 1 3
Displacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 300 4 2 6 0.7 CCn1c(=O)n(CC2CC2)c(=O)c2[nH]c(-c3cn[nH]c3)nc21 10.1021/jm7014815
CHEMBL430050 167564 None 0 Human Binding pKi = 7.4 7.4 1 3
Displacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 300 4 2 6 0.7 CCn1c(=O)n(CC2CC2)c(=O)c2[nH]c(-c3cn[nH]c3)nc21 10.1021/jm7014815
135546657 157698 None 0 Human Binding pKi = 7.4 7.4 - 1
Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cellsDisplacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells
ChEMBL 509 10 2 10 2.3 CCCn1c(=O)c2[nH]c(-c3cc(NC(=O)Cc4ccc(OC)c(OC)c4)nn3C)nc2n(CCC)c1=O 10.1021/jm051268+
CHEMBL408186 157698 None 0 Human Binding pKi = 7.4 7.4 - 1
Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cellsDisplacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells
ChEMBL 509 10 2 10 2.3 CCCn1c(=O)c2[nH]c(-c3cc(NC(=O)Cc4ccc(OC)c(OC)c4)nn3C)nc2n(CCC)c1=O 10.1021/jm051268+
11555329 73239 None 0 Human Binding pKi = 7.4 7.4 2 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 512 6 2 7 3.0 COc1cc(-c2cc3c([nH]2)c(=O)n(C)c(=O)n3C)ccc1OCC(=O)Nc1ccc(Br)cc1 10.1021/jm0506221
CHEMBL201243 73239 None 0 Human Binding pKi = 7.4 7.4 2 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 512 6 2 7 3.0 COc1cc(-c2cc3c([nH]2)c(=O)n(C)c(=O)n3C)ccc1OCC(=O)Nc1ccc(Br)cc1 10.1021/jm0506221
44451200 96130 None 0 Human Binding pKi = 7.4 7.4 3 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 587 10 1 8 3.8 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCN(C(=O)OCc5ccccc5)CC4)cc3)cc2n(CCC)c1=O 10.1016/j.bmc.2008.01.002
CHEMBL260433 96130 None 0 Human Binding pKi = 7.4 7.4 3 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 587 10 1 8 3.8 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCN(C(=O)OCc5ccccc5)CC4)cc3)cc2n(CCC)c1=O 10.1016/j.bmc.2008.01.002
46227974 201252 None 0 Human Binding pKi = 7.4 7.4 5 3
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 430 7 0 8 2.1 COCCn1c(=O)c2c(nc(Cc3c(F)cccc3F)n2C)n(Cc2ccco2)c1=O 10.1016/j.bmc.2009.07.034
CHEMBL603861 201252 None 0 Human Binding pKi = 7.4 7.4 5 3
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 430 7 0 8 2.1 COCCn1c(=O)c2c(nc(Cc3c(F)cccc3F)n2C)n(Cc2ccco2)c1=O 10.1016/j.bmc.2009.07.034
46880331 6228 None 0 Human Binding pKi = 6.4 6.4 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 281 3 1 6 2.2 CC(=O)Nc1ncc(-c2ccncn2)c(-c2ccco2)n1 10.1016/j.bmcl.2010.01.045
CHEMBL1081458 6228 None 0 Human Binding pKi = 6.4 6.4 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 281 3 1 6 2.2 CC(=O)Nc1ncc(-c2ccncn2)c(-c2ccco2)n1 10.1016/j.bmcl.2010.01.045
46880417 6338 None 0 Human Binding pKi = 6.4 6.4 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 273 3 1 3 3.1 O=C(Nc1ccc(-c2ccncc2)c(Cl)n1)C1CC1 10.1016/j.bmcl.2010.01.045
CHEMBL1082003 6338 None 0 Human Binding pKi = 6.4 6.4 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 273 3 1 3 3.1 O=C(Nc1ccc(-c2ccncc2)c(Cl)n1)C1CC1 10.1016/j.bmcl.2010.01.045
2817023 181356 None 6 Human Binding pKi = 6.4 6.4 -31 3
Displacement of [3H]MRS1754 from human adenosine A2B receptor expressed in CHO cell membraneDisplacement of [3H]MRS1754 from human adenosine A2B receptor expressed in CHO cell membrane
ChEMBL 267 2 1 5 3.5 N#Cc1c(-c2ccco2)cc(-c2cccs2)nc1N 10.1021/jm701594y
CHEMBL476310 181356 None 6 Human Binding pKi = 6.4 6.4 -31 3
Displacement of [3H]MRS1754 from human adenosine A2B receptor expressed in CHO cell membraneDisplacement of [3H]MRS1754 from human adenosine A2B receptor expressed in CHO cell membrane
ChEMBL 267 2 1 5 3.5 N#Cc1c(-c2ccco2)cc(-c2cccs2)nc1N 10.1021/jm701594y
9880921 190182 None 0 Human Binding pKi = 6.4 6.4 -57 4
Displacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation countingDisplacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation counting
ChEMBL 337 4 1 9 2.0 Nc1nc(-c2ccco2)c2nnn(Cc3ccccc3[N+](=O)[O-])c2n1 10.1021/jm800961g
CHEMBL517418 190182 None 0 Human Binding pKi = 6.4 6.4 -57 4
Displacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation countingDisplacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation counting
ChEMBL 337 4 1 9 2.0 Nc1nc(-c2ccco2)c2nnn(Cc3ccccc3[N+](=O)[O-])c2n1 10.1021/jm800961g
CHEMBL5083146 214846 None 0 Human Binding pKi = 6.4 6.4 -69 3
Displacement of [3H]DPCPX from human A2BAR expressed in HEK293 cell membrane incubated for 30 mins by microbeta trilux scintillation counter analysisDisplacement of [3H]DPCPX from human A2BAR expressed in HEK293 cell membrane incubated for 30 mins by microbeta trilux scintillation counter analysis
ChEMBL None None None N#Cc1c(-c2cccc(Cl)c2)nc(N)nc1-c1ccc2c(c1)OCO2 10.1021/acs.jmedchem.1c01636
72697649 104037 None 0 Human Binding pKi = 5.4 5.4 -13 4
Displacement of [3H]PSB-603 from human adenosine A2B receptorDisplacement of [3H]PSB-603 from human adenosine A2B receptor
ChEMBL 413 2 0 7 1.8 C#CCn1c(=O)c2c(nc3n2CCCN3c2cccc(Br)c2)n(C)c1=O 10.1016/j.bmc.2013.09.044
CHEMBL3093331 104037 None 0 Human Binding pKi = 5.4 5.4 -13 4
Displacement of [3H]PSB-603 from human adenosine A2B receptorDisplacement of [3H]PSB-603 from human adenosine A2B receptor
ChEMBL 413 2 0 7 1.8 C#CCn1c(=O)c2c(nc3n2CCCN3c2cccc(Br)c2)n(C)c1=O 10.1016/j.bmc.2013.09.044
44410409 75972 None 0 Human Binding pKi = 5.4 5.4 -1949 4
Displacement of [125I]ABOPX from human adenosine A2B receptor in HEK cellsDisplacement of [125I]ABOPX from human adenosine A2B receptor in HEK cells
ChEMBL 496 7 5 11 0.1 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC)nc(C#CC(O)c4ccccc4OC)nc32)[C@H](O)[C@@H]1O 10.1016/j.bmcl.2006.01.110
CHEMBL205327 75972 None 0 Human Binding pKi = 5.4 5.4 -1949 4
Displacement of [125I]ABOPX from human adenosine A2B receptor in HEK cellsDisplacement of [125I]ABOPX from human adenosine A2B receptor in HEK cells
ChEMBL 496 7 5 11 0.1 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC)nc(C#CC(O)c4ccccc4OC)nc32)[C@H](O)[C@@H]1O 10.1016/j.bmcl.2006.01.110
156010696 177157 None 0 Human Binding pKi = 6.4 6.4 -128 2
Displacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting methodDisplacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting method
ChEMBL 340 3 1 7 3.3 CCOC(=O)C1=C(C)Nc2nc3ccccc3n2C1c1nccs1 10.1021/acs.jmedchem.0c00564
CHEMBL4634105 177157 None 0 Human Binding pKi = 6.4 6.4 -128 2
Displacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting methodDisplacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting method
ChEMBL 340 3 1 7 3.3 CCOC(=O)C1=C(C)Nc2nc3ccccc3n2C1c1nccs1 10.1021/acs.jmedchem.0c00564
135443353 110594 None 0 Human Binding pKi = 7.4 7.4 11 2
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 484 7 3 8 3.4 CCCn1c(=O)c2nc(-c3cc(NC(=O)Nc4cccc(Cl)c4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
CHEMBL32552 110594 None 0 Human Binding pKi = 7.4 7.4 11 2
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 484 7 3 8 3.4 CCCn1c(=O)c2nc(-c3cc(NC(=O)Nc4cccc(Cl)c4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
10779327 119409 None 0 Human Binding pKi = 7.4 7.4 -15 6
Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 35-45Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 35-45
ChEMBL 283 3 1 8 1.7 CCCn1cc2c(nc(N)n3nc(-c4ccco4)nc23)n1 10.1021/jm001047y
CHEMBL344706 119409 None 0 Human Binding pKi = 7.4 7.4 -15 6
Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 35-45Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 35-45
ChEMBL 283 3 1 8 1.7 CCCn1cc2c(nc(N)n3nc(-c4ccco4)nc23)n1 10.1021/jm001047y
16720105 85381 None 0 Human Binding pKi = 7.4 7.4 - 1
Displacement of [3H]DPCPX from human A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human A2B receptor expressed in HEK293 cells
ChEMBL 347 5 1 9 2.7 COc1ncc(Nc2ncc(-c3ccncn3)c(-c3ccco3)n2)cn1 10.1021/jm061333v
CHEMBL226236 85381 None 0 Human Binding pKi = 7.4 7.4 - 1
Displacement of [3H]DPCPX from human A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human A2B receptor expressed in HEK293 cells
ChEMBL 347 5 1 9 2.7 COc1ncc(Nc2ncc(-c3ccncn3)c(-c3ccco3)n2)cn1 10.1021/jm061333v
11698898 140362 None 0 Human Binding pKi = 7.4 7.4 74 2
Displacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cellsDisplacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cells
ChEMBL 494 8 1 10 3.3 CCCn1c(=O)c2nc(-c3cnn(Cc4noc(-c5ccc(Cl)cc5)n4)c3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2005.10.002
CHEMBL380821 140362 None 0 Human Binding pKi = 7.4 7.4 74 2
Displacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cellsDisplacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cells
ChEMBL 494 8 1 10 3.3 CCCn1c(=O)c2nc(-c3cnn(Cc4noc(-c5ccc(Cl)cc5)n4)c3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2005.10.002
655439 47396 None 16 Human Binding pKi = 7.4 7.4 - 1
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 minsDisplacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 mins
ChEMBL 250 3 2 4 1.5 CCOC(=O)C1=C(C)NC(=O)NC1c1ccoc1 10.1021/acs.jmedchem.5b01586
CHEMBL1544856 47396 None 16 Human Binding pKi = 7.4 7.4 - 1
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 minsDisplacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 mins
ChEMBL 250 3 2 4 1.5 CCOC(=O)C1=C(C)NC(=O)NC1c1ccoc1 10.1021/acs.jmedchem.5b01586
655439 47396 None 16 Human Binding pKi = 7.4 7.4 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes after 30 minsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes after 30 mins
ChEMBL 250 3 2 4 1.5 CCOC(=O)C1=C(C)NC(=O)NC1c1ccoc1 10.1021/acs.jmedchem.7b00138
CHEMBL1544856 47396 None 16 Human Binding pKi = 7.4 7.4 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes after 30 minsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes after 30 mins
ChEMBL 250 3 2 4 1.5 CCOC(=O)C1=C(C)NC(=O)NC1c1ccoc1 10.1021/acs.jmedchem.7b00138
655439 47396 None 16 Human Binding pKi = 7.4 7.4 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 250 3 2 4 1.5 CCOC(=O)C1=C(C)NC(=O)NC1c1ccoc1 10.1021/acs.jmedchem.0c01431
CHEMBL1544856 47396 None 16 Human Binding pKi = 7.4 7.4 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 250 3 2 4 1.5 CCOC(=O)C1=C(C)NC(=O)NC1c1ccoc1 10.1021/acs.jmedchem.0c01431
655439 47396 None 16 Human Binding pKi = 7.4 7.4 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by Scatchard plot analysisDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by Scatchard plot analysis
ChEMBL 250 3 2 4 1.5 CCOC(=O)C1=C(C)NC(=O)NC1c1ccoc1 10.1021/ml400185v
CHEMBL1544856 47396 None 16 Human Binding pKi = 7.4 7.4 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by Scatchard plot analysisDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by Scatchard plot analysis
ChEMBL 250 3 2 4 1.5 CCOC(=O)C1=C(C)NC(=O)NC1c1ccoc1 10.1021/ml400185v
655439 47396 None 16 Human Binding pKi = 7.4 7.4 - 1
Displacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assayDisplacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assay
ChEMBL 250 3 2 4 1.5 CCOC(=O)C1=C(C)NC(=O)NC1c1ccoc1 10.1021/acs.jmedchem.9b01340
CHEMBL1544856 47396 None 16 Human Binding pKi = 7.4 7.4 - 1
Displacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assayDisplacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assay
ChEMBL 250 3 2 4 1.5 CCOC(=O)C1=C(C)NC(=O)NC1c1ccoc1 10.1021/acs.jmedchem.9b01340
126079 4100 None 31 Human Binding pKi = 7.4 7.4 -2 8
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 386 8 2 7 1.8 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)O 10.1021/jm0506221
451 4100 None 31 Human Binding pKi = 7.4 7.4 -2 8
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 386 8 2 7 1.8 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)O 10.1021/jm0506221
CHEMBL27041 4100 None 31 Human Binding pKi = 7.4 7.4 -2 8
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 386 8 2 7 1.8 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)O 10.1021/jm0506221
11174953 16762 None 1 Human Binding pKi = 7.4 7.4 -3 4
Displacement of [3H]PSB-603 from human A2B receptor expressed in CHO cell membranes measured after 3 hrs by radioligand binding assayDisplacement of [3H]PSB-603 from human A2B receptor expressed in CHO cell membranes measured after 3 hrs by radioligand binding assay
ChEMBL 332 4 2 6 3.1 N#Cc1c(N)nc(SCc2ncc[nH]2)c(C#N)c1-c1ccccc1 10.1021/acs.jmedchem.0c01856
CHEMBL124345 16762 None 1 Human Binding pKi = 7.4 7.4 -3 4
Displacement of [3H]PSB-603 from human A2B receptor expressed in CHO cell membranes measured after 3 hrs by radioligand binding assayDisplacement of [3H]PSB-603 from human A2B receptor expressed in CHO cell membranes measured after 3 hrs by radioligand binding assay
ChEMBL 332 4 2 6 3.1 N#Cc1c(N)nc(SCc2ncc[nH]2)c(C#N)c1-c1ccccc1 10.1021/acs.jmedchem.0c01856
53354632 74286 None 0 Human Binding pKi = 7.4 7.4 -2 3
Inhibition of adenosine A2B receptorInhibition of adenosine A2B receptor
ChEMBL 316 2 1 4 4.1 Nc1nnc(-c2cc(Cl)cc(Cl)c2)c(-c2ccccc2)n1 10.1021/jm201376w
CHEMBL2024112 74286 None 0 Human Binding pKi = 7.4 7.4 -2 3
Inhibition of adenosine A2B receptorInhibition of adenosine A2B receptor
ChEMBL 316 2 1 4 4.1 Nc1nnc(-c2cc(Cl)cc(Cl)c2)c(-c2ccccc2)n1 10.1021/jm201376w
11560981 78311 None 0 Human Binding pKi = 6.4 6.4 - 1
Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cellsDisplacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells
ChEMBL 428 7 1 7 2.9 CCCn1c(=O)c2nc(-c3cnn(Cc4c(F)cccc4F)c3)[nH]c2n(CCC)c1=O 10.1021/jm051268+
CHEMBL210890 78311 None 0 Human Binding pKi = 6.4 6.4 - 1
Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cellsDisplacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells
ChEMBL 428 7 1 7 2.9 CCCn1c(=O)c2nc(-c3cnn(Cc4c(F)cccc4F)c3)[nH]c2n(CCC)c1=O 10.1021/jm051268+
7315331 201129 None 1 Human Binding pKi = 6.4 6.4 -5 4
Displacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cells
ChEMBL 352 5 1 5 4.6 CCOC(=O)Nc1nc(-c2ccccc2)c(C(=O)c2ccccc2)s1 10.1016/j.bmc.2010.01.072
CHEMBL603129 201129 None 1 Human Binding pKi = 6.4 6.4 -5 4
Displacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cells
ChEMBL 352 5 1 5 4.6 CCOC(=O)Nc1nc(-c2ccccc2)c(C(=O)c2ccccc2)s1 10.1016/j.bmc.2010.01.072
10085373 10428 None 6 Human Binding pKi = 6.4 6.4 -616 2
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 286 2 1 6 0.6 COc1ccc(-c2nc3c(=O)n(C)c(=O)n(C)c3[nH]2)cc1 10.1021/jm0104318
CHEMBL11635 10428 None 6 Human Binding pKi = 6.4 6.4 -616 2
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 286 2 1 6 0.6 COc1ccc(-c2nc3c(=O)n(C)c(=O)n(C)c3[nH]2)cc1 10.1021/jm0104318
21874613 176179 None 0 Human Binding pKi = 6.4 6.4 -263 4
Displacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation countingDisplacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation counting
ChEMBL 349 4 2 8 2.8 CC(C)c1cc(Cn2nnc3c(-c4ccco4)nc(N)nc32)ccc1N 10.1021/jm800961g
CHEMBL459322 176179 None 0 Human Binding pKi = 6.4 6.4 -263 4
Displacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation countingDisplacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation counting
ChEMBL 349 4 2 8 2.8 CC(C)c1cc(Cn2nnc3c(-c4ccco4)nc(N)nc32)ccc1N 10.1021/jm800961g
72697931 103819 None 0 Human Binding pKi = 5.4 5.4 -17 5
Displacement of [3H]PSB-603 from human adenosine A2B receptorDisplacement of [3H]PSB-603 from human adenosine A2B receptor
ChEMBL 313 2 0 7 0.3 C#CCn1c(=O)c2c(nc3n2CCCN3C2CCC2)n(C)c1=O 10.1016/j.bmc.2013.09.044
CHEMBL3091482 103819 None 0 Human Binding pKi = 5.4 5.4 -17 5
Displacement of [3H]PSB-603 from human adenosine A2B receptorDisplacement of [3H]PSB-603 from human adenosine A2B receptor
ChEMBL 313 2 0 7 0.3 C#CCn1c(=O)c2c(nc3n2CCCN3C2CCC2)n(C)c1=O 10.1016/j.bmc.2013.09.044
10190 935 None 45 Human Binding pKi = 5.4 5.4 -1174 4
Displacement of [3H]-ZM241385 from human adenosine 2B receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]-ZM241385 from human adenosine 2B receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 407 6 1 10 2.1 Nc1nc(c2ccc(o2)C)c2c(n1)n(nn2)Cc1cccc(n1)CO[C@@H]1COCC1 10.1021/acs.jmedchem.0c00237
44537963 935 None 45 Human Binding pKi = 5.4 5.4 -1174 4
Displacement of [3H]-ZM241385 from human adenosine 2B receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]-ZM241385 from human adenosine 2B receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 407 6 1 10 2.1 Nc1nc(c2ccc(o2)C)c2c(n1)n(nn2)Cc1cccc(n1)CO[C@@H]1COCC1 10.1021/acs.jmedchem.0c00237
44537963.0 935 None 45 Human Binding pKi = 5.4 5.4 -1174 4
Displacement of [3H]-ZM241385 from human adenosine 2B receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]-ZM241385 from human adenosine 2B receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 407 6 1 10 2.1 Nc1nc(c2ccc(o2)C)c2c(n1)n(nn2)Cc1cccc(n1)CO[C@@H]1COCC1 10.1021/acs.jmedchem.0c00237
CHEMBL4297184 935 None 45 Human Binding pKi = 5.4 5.4 -1174 4
Displacement of [3H]-ZM241385 from human adenosine 2B receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]-ZM241385 from human adenosine 2B receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 407 6 1 10 2.1 Nc1nc(c2ccc(o2)C)c2c(n1)n(nn2)Cc1cccc(n1)CO[C@@H]1COCC1 10.1021/acs.jmedchem.0c00237
DB16125 935 None 45 Human Binding pKi = 5.4 5.4 -1174 4
Displacement of [3H]-ZM241385 from human adenosine 2B receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting methodDisplacement of [3H]-ZM241385 from human adenosine 2B receptor expressed in HEK-293 cells incubated for 60 mins by scintillation counting method
ChEMBL 407 6 1 10 2.1 Nc1nc(c2ccc(o2)C)c2c(n1)n(nn2)Cc1cccc(n1)CO[C@@H]1COCC1 10.1021/acs.jmedchem.0c00237
3281 1370 None 54 Human Binding pKi = 5.4 5.4 -4265 7
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 308 3 3 4 3.3 O[C@@H]1CC[C@H](CC1)Nc1nc(nc2c1cc[nH]2)c1ccccc1 10.1016/j.bmc.2010.01.072
9953065 1370 None 54 Human Binding pKi = 5.4 5.4 -4265 7
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 308 3 3 4 3.3 O[C@@H]1CC[C@H](CC1)Nc1nc(nc2c1cc[nH]2)c1ccccc1 10.1016/j.bmc.2010.01.072
CHEMBL4204703 1370 None 54 Human Binding pKi = 5.4 5.4 -4265 7
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 308 3 3 4 3.3 O[C@@H]1CC[C@H](CC1)Nc1nc(nc2c1cc[nH]2)c1ccccc1 10.1016/j.bmc.2010.01.072
CHEMBL592435 1370 None 54 Human Binding pKi = 5.4 5.4 -4265 7
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 308 3 3 4 3.3 O[C@@H]1CC[C@H](CC1)Nc1nc(nc2c1cc[nH]2)c1ccccc1 10.1016/j.bmc.2010.01.072
DB12446 1370 None 54 Human Binding pKi = 5.4 5.4 -4265 7
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 308 3 3 4 3.3 O[C@@H]1CC[C@H](CC1)Nc1nc(nc2c1cc[nH]2)c1ccccc1 10.1016/j.bmc.2010.01.072
57429645 157008 None 0 Human Binding pKi = 8.4 8.4 - 1
Displacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting methodDisplacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting method
ChEMBL 557 8 1 8 4.2 CCCn1c(=O)c2[nH]c(-c3cnn(C(C)C4CC(=O)N(c5cccc(C(F)(F)F)c5)C4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2016.11.007
CHEMBL4073346 157008 None 0 Human Binding pKi = 8.4 8.4 - 1
Displacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting methodDisplacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting method
ChEMBL 557 8 1 8 4.2 CCCn1c(=O)c2[nH]c(-c3cnn(C(C)C4CC(=O)N(c5cccc(C(F)(F)F)c5)C4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2016.11.007
69031481 157077 None 0 Human Binding pKi = 8.4 8.4 81 3
Displacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting methodDisplacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting method
ChEMBL 529 7 1 8 3.3 CCCn1c(=O)c2[nH]c(-c3cnn(CC4CC(=O)N(c5ccc(C(F)(F)F)cc5)C4)c3)nc2n(CC)c1=O 10.1016/j.ejmech.2016.11.007
CHEMBL4074253 157077 None 0 Human Binding pKi = 8.4 8.4 81 3
Displacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting methodDisplacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting method
ChEMBL 529 7 1 8 3.3 CCCn1c(=O)c2[nH]c(-c3cnn(CC4CC(=O)N(c5ccc(C(F)(F)F)cc5)C4)c3)nc2n(CC)c1=O 10.1016/j.ejmech.2016.11.007
69029798 158210 None 0 Human Binding pKi = 8.4 8.4 - 1
Displacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting methodDisplacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting method
ChEMBL 520 9 1 8 3.3 CCCn1c(=O)c2[nH]c(-c3ccc(OCC4CC(=O)N(c5ccc(F)cc5)C4)nc3)nc2n(CCC)c1=O 10.1016/j.ejmech.2016.11.007
CHEMBL4088043 158210 None 0 Human Binding pKi = 8.4 8.4 - 1
Displacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting methodDisplacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting method
ChEMBL 520 9 1 8 3.3 CCCn1c(=O)c2[nH]c(-c3ccc(OCC4CC(=O)N(c5ccc(F)cc5)C4)nc3)nc2n(CCC)c1=O 10.1016/j.ejmech.2016.11.007
66893509 158500 None 0 Human Binding pKi = 8.4 8.4 - 1
Displacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting methodDisplacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting method
ChEMBL 559 9 1 9 3.5 CCCn1c(=O)c2[nH]c(-c3cnn(CC4CC(=O)N(c5ccc(OC(F)(F)F)cc5)C4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2016.11.007
CHEMBL4091110 158500 None 0 Human Binding pKi = 8.4 8.4 - 1
Displacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting methodDisplacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting method
ChEMBL 559 9 1 9 3.5 CCCn1c(=O)c2[nH]c(-c3cnn(CC4CC(=O)N(c5ccc(OC(F)(F)F)cc5)C4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2016.11.007
46880507 6154 None 0 Human Binding pKi = 8.4 8.4 8 3
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 333 4 1 3 4.3 O=C(Nc1ccc(-c2ccncc2)c(-c2ccc(F)cc2)n1)C1CC1 10.1016/j.bmcl.2010.01.045
CHEMBL1081038 6154 None 0 Human Binding pKi = 8.4 8.4 8 3
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 333 4 1 3 4.3 O=C(Nc1ccc(-c2ccncc2)c(-c2ccc(F)cc2)n1)C1CC1 10.1016/j.bmcl.2010.01.045
46866592 6331 None 0 Human Binding pKi = 8.4 8.4 60 4
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 306 4 1 5 3.1 O=C(Nc1ccc(-c2ccncn2)c(-c2ccco2)n1)C1CC1 10.1016/j.bmcl.2010.01.045
46866592 6331 None 0 Human Binding pKi = 8.4 8.4 60 4
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 306 4 1 5 3.1 O=C(Nc1ccc(-c2ccncn2)c(-c2ccco2)n1)C1CC1 10.1016/j.bmcl.2010.01.077
CHEMBL1081971 6331 None 0 Human Binding pKi = 8.4 8.4 60 4
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 306 4 1 5 3.1 O=C(Nc1ccc(-c2ccncn2)c(-c2ccco2)n1)C1CC1 10.1016/j.bmcl.2010.01.045
CHEMBL1081971 6331 None 0 Human Binding pKi = 8.4 8.4 60 4
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 306 4 1 5 3.1 O=C(Nc1ccc(-c2ccncn2)c(-c2ccco2)n1)C1CC1 10.1016/j.bmcl.2010.01.077
56924646 71172 None 0 Human Binding pKi = 8.4 8.4 186 2
Displacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation countingDisplacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation counting
ChEMBL 332 5 2 7 0.4 CCCn1c(=O)c2[nH]c(-c3cc(=O)[nH]n3C)nc2n(CCC)c1=O 10.1021/jm201292w
CHEMBL1955922 71172 None 0 Human Binding pKi = 8.4 8.4 186 2
Displacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation countingDisplacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation counting
ChEMBL 332 5 2 7 0.4 CCCn1c(=O)c2[nH]c(-c3cc(=O)[nH]n3C)nc2n(CCC)c1=O 10.1021/jm201292w
49797905 10743 None 0 Human Binding pKi = 8.4 8.4 -1 3
Displacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cells after 1 hrDisplacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cells after 1 hr
ChEMBL 517 7 1 7 5.2 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3cnn(Cc4cccc(C(F)(F)F)c4)c3)sc12 10.1016/j.bmcl.2011.02.053
CHEMBL1171164 10743 None 0 Human Binding pKi = 8.4 8.4 -1 3
Displacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cells after 1 hrDisplacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cells after 1 hr
ChEMBL 517 7 1 7 5.2 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3cnn(Cc4cccc(C(F)(F)F)c4)c3)sc12 10.1016/j.bmcl.2011.02.053
49797748 10620 None 0 Human Binding pKi = 8.4 8.4 25 3
Displacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cells after 1 hr by scintillation countingDisplacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 480 6 1 6 4.6 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(C(=O)N4CCCCC4)cc3)sc12 10.1016/j.bmcl.2010.05.056
CHEMBL1170135 10620 None 0 Human Binding pKi = 8.4 8.4 25 3
Displacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cells after 1 hr by scintillation countingDisplacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 480 6 1 6 4.6 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(C(=O)N4CCCCC4)cc3)sc12 10.1016/j.bmcl.2010.05.056
49797905 10743 None 0 Human Binding pKi = 8.4 8.4 -1 3
Displacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cells after 1 hr by scintillation countingDisplacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 517 7 1 7 5.2 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3cnn(Cc4cccc(C(F)(F)F)c4)c3)sc12 10.1016/j.bmcl.2010.05.056
CHEMBL1171164 10743 None 0 Human Binding pKi = 8.4 8.4 -1 3
Displacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cells after 1 hr by scintillation countingDisplacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 517 7 1 7 5.2 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3cnn(Cc4cccc(C(F)(F)F)c4)c3)sc12 10.1016/j.bmcl.2010.05.056
49797773 10857 None 0 Human Binding pKi = 8.4 8.4 17 3
Displacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cells after 1 hr by scintillation countingDisplacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 490 8 1 7 3.3 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(CN(C)S(C)(=O)=O)cc3)sc12 10.1016/j.bmcl.2010.05.056
CHEMBL1172277 10857 None 0 Human Binding pKi = 8.4 8.4 17 3
Displacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cells after 1 hr by scintillation countingDisplacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 490 8 1 7 3.3 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(CN(C)S(C)(=O)=O)cc3)sc12 10.1016/j.bmcl.2010.05.056
11555462 73036 None 0 Human Binding pKi = 8.4 8.4 11 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 522 10 2 6 4.7 CCCn1c(=O)c2[nH]c(-c3ccc(OC(C)C(=O)NCc4ccc(Cl)cc4)cc3)cc2n(CCC)c1=O 10.1021/jm0506221
CHEMBL201028 73036 None 0 Human Binding pKi = 8.4 8.4 11 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 522 10 2 6 4.7 CCCn1c(=O)c2[nH]c(-c3ccc(OC(C)C(=O)NCc4ccc(Cl)cc4)cc3)cc2n(CCC)c1=O 10.1021/jm0506221
136042340 71166 None 0 Human Binding pKi = 8.4 8.4 21 2
Displacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation countingDisplacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation counting
ChEMBL 527 8 2 9 3.6 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5cc(Br)ccc5[nH]4)no3)nc2n(CCC)c1=O 10.1021/jm201292w
CHEMBL1955916 71166 None 0 Human Binding pKi = 8.4 8.4 21 2
Displacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation countingDisplacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation counting
ChEMBL 527 8 2 9 3.6 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5cc(Br)ccc5[nH]4)no3)nc2n(CCC)c1=O 10.1021/jm201292w
46229141 199131 None 0 Human Binding pKi = 8.4 8.4 23 2
Displacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cell membraneDisplacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cell membrane
ChEMBL 614 25 1 10 4.8 C=CCCCCCCCCCCOCCOCCOCCOCCOc1ccc(-c2nc3c([nH]2)c(=O)n(C)c(=O)n3C)cc1 10.1016/j.bmc.2010.02.014
CHEMBL589251 199131 None 0 Human Binding pKi = 8.4 8.4 23 2
Displacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cell membraneDisplacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cell membrane
ChEMBL 614 25 1 10 4.8 C=CCCCCCCCCCCOCCOCCOCCOCCOc1ccc(-c2nc3c([nH]2)c(=O)n(C)c(=O)n3C)cc1 10.1016/j.bmc.2010.02.014
44451053 96104 None 0 Human Binding pKi = 8.4 8.4 41 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 597 9 1 7 4.7 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCN(c5ccc(C(F)(F)F)cc5)CC4)cc3)cc2n(CCC)c1=O 10.1016/j.bmc.2008.01.002
CHEMBL260221 96104 None 0 Human Binding pKi = 8.4 8.4 41 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 597 9 1 7 4.7 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCN(c5ccc(C(F)(F)F)cc5)CC4)cc3)cc2n(CCC)c1=O 10.1016/j.bmc.2008.01.002
44451285 161272 None 0 Human Binding pKi = 8.4 8.4 31 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 541 5 1 7 3.0 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCN(c5ccc(C(F)(F)F)cc5)CC4)cc3)cc2n(C)c1=O 10.1016/j.bmc.2008.01.002
CHEMBL412063 161272 None 0 Human Binding pKi = 8.4 8.4 31 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 541 5 1 7 3.0 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCN(c5ccc(C(F)(F)F)cc5)CC4)cc3)cc2n(C)c1=O 10.1016/j.bmc.2008.01.002
44451126 166885 None 0 Human Binding pKi = 8.4 8.4 134 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 529 7 1 7 3.6 CCCn1c(=O)n(C)c(=O)c2[nH]c(-c3ccc(OC(C)(C)C(=O)N4CCN(c5ccccc5)CC4)cc3)cc21 10.1016/j.bmc.2008.01.002
CHEMBL428604 166885 None 0 Human Binding pKi = 8.4 8.4 134 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 529 7 1 7 3.6 CCCn1c(=O)n(C)c(=O)c2[nH]c(-c3ccc(OC(C)(C)C(=O)N4CCN(c5ccccc5)CC4)cc3)cc21 10.1016/j.bmc.2008.01.002
11690712 77792 None 0 Human Binding pKi = 8.4 8.4 1 5
Displacement of [3H]PSB298 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB298 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 439 7 3 6 2.0 CCCn1c(=O)[nH]c2[nH]c(-c3ccc(S(=O)(=O)NCc4ccccc4)cc3)nc2c1=O 10.1021/jm060277v
CHEMBL209230 77792 None 0 Human Binding pKi = 8.4 8.4 1 5
Displacement of [3H]PSB298 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB298 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 439 7 3 6 2.0 CCCn1c(=O)[nH]c2[nH]c(-c3ccc(S(=O)(=O)NCc4ccccc4)cc3)nc2c1=O 10.1021/jm060277v
44451123 95838 None 0 Human Binding pKi = 8.4 8.4 151 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 570 7 1 8 3.5 CCCn1c(=O)n(C)c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCN(c5c(Cl)cncc5Cl)CC4)cc3)cc21 10.1016/j.bmc.2008.01.002
CHEMBL258948 95838 None 0 Human Binding pKi = 8.4 8.4 151 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 570 7 1 8 3.5 CCCn1c(=O)n(C)c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCN(c5c(Cl)cncc5Cl)CC4)cc3)cc21 10.1016/j.bmc.2008.01.002
155562182 175716 None 0 Human Binding pKi = 8.4 8.4 22 3
Displacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 510 6 3 8 1.7 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(c5ccc(O)cc5)CC4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
CHEMBL4582353 175716 None 0 Human Binding pKi = 8.4 8.4 22 3
Displacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 510 6 3 8 1.7 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(c5ccc(O)cc5)CC4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
155553575 174187 None 0 Human Binding pKi = 8.4 8.4 75 2
Displacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 556 7 1 8 3.1 CCCn1c(=O)c2[nH]c(-c3ccc(S(=O)(=O)N4CCN(c5ccc(Cl)cc5)CC4)cc3)nc2n(CC)c1=O 10.1021/acs.jmedchem.9b00071
CHEMBL4547661 174187 None 0 Human Binding pKi = 8.4 8.4 75 2
Displacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 556 7 1 8 3.1 CCCn1c(=O)c2[nH]c(-c3ccc(S(=O)(=O)N4CCN(c5ccc(Cl)cc5)CC4)cc3)nc2n(CC)c1=O 10.1021/acs.jmedchem.9b00071
10970127 121072 None 0 Human Binding pKi = 8.4 8.4 4 4
Inhibition of [3H]ZM-241385 binding to human adenosine A2B receptorInhibition of [3H]ZM-241385 binding to human adenosine A2B receptor
ChEMBL 348 3 2 4 2.3 CCCn1c(=O)[nH]c2[nH]c(-c3ccc(Br)cc3)nc2c1=O 10.1021/jm011049y
CHEMBL35701 121072 None 0 Human Binding pKi = 8.4 8.4 4 4
Inhibition of [3H]ZM-241385 binding to human adenosine A2B receptorInhibition of [3H]ZM-241385 binding to human adenosine A2B receptor
ChEMBL 348 3 2 4 2.3 CCCn1c(=O)[nH]c2[nH]c(-c3ccc(Br)cc3)nc2c1=O 10.1021/jm011049y
11568359 78226 None 0 Human Binding pKi = 8.4 8.4 2 6
Displacement of [3H]PSB298 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB298 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 439 6 2 7 1.1 Cn1c(=O)c2nc(-c3ccc(S(=O)(=O)NCCc4ccccc4)cc3)[nH]c2n(C)c1=O 10.1021/jm060277v
CHEMBL210585 78226 None 0 Human Binding pKi = 8.4 8.4 2 6
Displacement of [3H]PSB298 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB298 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 439 6 2 7 1.1 Cn1c(=O)c2nc(-c3ccc(S(=O)(=O)NCCc4ccccc4)cc3)[nH]c2n(C)c1=O 10.1021/jm060277v
69030381 158841 None 0 Human Binding pKi = 8.4 8.4 - 1
Displacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting methodDisplacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting method
ChEMBL 529 7 1 8 3.3 CCCn1c(=O)c2[nH]c(-c3cnn(CC4CC(=O)N(c5cccc(C(F)(F)F)c5)C4)c3)nc2n(CC)c1=O 10.1016/j.ejmech.2016.11.007
CHEMBL4094755 158841 None 0 Human Binding pKi = 8.4 8.4 - 1
Displacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting methodDisplacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting method
ChEMBL 529 7 1 8 3.3 CCCn1c(=O)c2[nH]c(-c3cnn(CC4CC(=O)N(c5cccc(C(F)(F)F)c5)C4)c3)nc2n(CC)c1=O 10.1016/j.ejmech.2016.11.007
69031242 155808 None 0 Human Binding pKi = 8.3 8.3 - 1
Displacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting methodDisplacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting method
ChEMBL 520 9 1 8 3.3 CCCn1c(=O)c2[nH]c(-c3ccc(OCC4CC(=O)N(c5cccc(F)c5)C4)nc3)nc2n(CCC)c1=O 10.1016/j.ejmech.2016.11.007
CHEMBL4059759 155808 None 0 Human Binding pKi = 8.3 8.3 - 1
Displacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting methodDisplacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting method
ChEMBL 520 9 1 8 3.3 CCCn1c(=O)c2[nH]c(-c3ccc(OCC4CC(=O)N(c5cccc(F)c5)C4)nc3)nc2n(CCC)c1=O 10.1016/j.ejmech.2016.11.007
11663068 72737 None 0 Human Binding pKi = 8.3 8.3 3 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 484 9 2 6 4.0 O=C(COc1ccc(-c2cc3c([nH]2)c(=O)n(CC2CC2)c(=O)n3CC2CC2)cc1)Nc1ccccc1 10.1021/jm0506221
CHEMBL199862 72737 None 0 Human Binding pKi = 8.3 8.3 3 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 484 9 2 6 4.0 O=C(COc1ccc(-c2cc3c([nH]2)c(=O)n(CC2CC2)c(=O)n3CC2CC2)cc1)Nc1ccccc1 10.1021/jm0506221
44450849 161305 None 0 Human Binding pKi = 8.3 8.3 33 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 514 8 1 6 4.3 CCCn1c(=O)c2[nH]c(-c3ccc(OC(C)C(=O)N4CCc5ccccc5C4)cc3)cc2n(CCC)c1=O 10.1016/j.bmc.2008.01.002
CHEMBL412293 161305 None 0 Human Binding pKi = 8.3 8.3 33 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 514 8 1 6 4.3 CCCn1c(=O)c2[nH]c(-c3ccc(OC(C)C(=O)N4CCc5ccccc5C4)cc3)cc2n(CCC)c1=O 10.1016/j.bmc.2008.01.002
15627855 98307 None 0 Human Binding pKi = 8.3 8.3 9 3
Binding affinity for human adenosine A2B receptor using [3H]ZM-241385 in CHO cell membranesBinding affinity for human adenosine A2B receptor using [3H]ZM-241385 in CHO cell membranes
ChEMBL 270 3 2 4 1.5 CCCn1c(=O)[nH]c2[nH]c(-c3ccccc3)nc2c1=O 10.1021/jm0310030
CHEMBL274855 98307 None 0 Human Binding pKi = 8.3 8.3 9 3
Binding affinity for human adenosine A2B receptor using [3H]ZM-241385 in CHO cell membranesBinding affinity for human adenosine A2B receptor using [3H]ZM-241385 in CHO cell membranes
ChEMBL 270 3 2 4 1.5 CCCn1c(=O)[nH]c2[nH]c(-c3ccccc3)nc2c1=O 10.1021/jm0310030
15627855 98307 None 0 Human Binding pKi = 8.3 8.3 9 3
Inhibition of [3H]ZM-241385 binding to human adenosine A2B receptorInhibition of [3H]ZM-241385 binding to human adenosine A2B receptor
ChEMBL 270 3 2 4 1.5 CCCn1c(=O)[nH]c2[nH]c(-c3ccccc3)nc2c1=O 10.1021/jm011049y
CHEMBL274855 98307 None 0 Human Binding pKi = 8.3 8.3 9 3
Inhibition of [3H]ZM-241385 binding to human adenosine A2B receptorInhibition of [3H]ZM-241385 binding to human adenosine A2B receptor
ChEMBL 270 3 2 4 1.5 CCCn1c(=O)[nH]c2[nH]c(-c3ccccc3)nc2c1=O 10.1021/jm011049y
11553509 72672 None 0 Human Binding pKi = 8.3 8.3 1 4
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 418 5 2 6 2.6 CC(Oc1ccc(-c2cc3c([nH]2)c(=O)n(C)c(=O)n3C)cc1)C(=O)Nc1ccccc1 10.1021/jm0506221
CHEMBL199611 72672 None 0 Human Binding pKi = 8.3 8.3 1 4
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 418 5 2 6 2.6 CC(Oc1ccc(-c2cc3c([nH]2)c(=O)n(C)c(=O)n3C)cc1)C(=O)Nc1ccccc1 10.1021/jm0506221
11649117 140548 None 0 Human Binding pKi = 8.3 8.3 3 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 506 10 2 6 4.9 CCCn1c(=O)c2[nH]c(-c3ccc(OC(CC)C(=O)Nc4ccc(F)cc4)cc3)cc2n(CCC)c1=O 10.1021/jm0506221
CHEMBL381091 140548 None 0 Human Binding pKi = 8.3 8.3 3 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 506 10 2 6 4.9 CCCn1c(=O)c2[nH]c(-c3ccc(OC(CC)C(=O)Nc4ccc(F)cc4)cc3)cc2n(CCC)c1=O 10.1021/jm0506221
44451021 95866 None 0 Human Binding pKi = 8.3 8.3 33 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 529 9 1 7 3.7 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCN(c5ccccc5)CC4)cc3)cc2n(CCC)c1=O 10.1016/j.bmc.2008.01.002
CHEMBL259057 95866 None 0 Human Binding pKi = 8.3 8.3 33 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 529 9 1 7 3.7 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCN(c5ccccc5)CC4)cc3)cc2n(CCC)c1=O 10.1016/j.bmc.2008.01.002
11590537 75005 None 0 Human Binding pKi = 8.3 8.3 4 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 452 6 2 6 2.6 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)NCc4ccc(Cl)cc4)cc3)cc2n(C)c1=O 10.1021/jm0506221
CHEMBL203305 75005 None 0 Human Binding pKi = 8.3 8.3 4 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 452 6 2 6 2.6 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)NCc4ccc(Cl)cc4)cc3)cc2n(C)c1=O 10.1021/jm0506221
44451099 96294 None 0 Human Binding pKi = 8.3 8.3 81 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 561 11 1 9 2.2 COCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCN(c5ccccc5)CC4)cc3)cc2n(CCOC)c1=O 10.1016/j.bmc.2008.01.002
CHEMBL261212 96294 None 0 Human Binding pKi = 8.3 8.3 81 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 561 11 1 9 2.2 COCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCN(c5ccccc5)CC4)cc3)cc2n(CCOC)c1=O 10.1016/j.bmc.2008.01.002
57429603 157381 None 0 Human Binding pKi = 8.3 8.3 - 1
Displacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 minsDisplacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 mins
ChEMBL 484 6 1 7 3.6 CCCn1c(=O)c2[nH]c(-c3cnn(CC#Cc4cccc(C(F)(F)F)c4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2017.04.014
CHEMBL4078183 157381 None 0 Human Binding pKi = 8.3 8.3 - 1
Displacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 minsDisplacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 mins
ChEMBL 484 6 1 7 3.6 CCCn1c(=O)c2[nH]c(-c3cnn(CC#Cc4cccc(C(F)(F)F)c4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2017.04.014
76314450 105513 None 0 Human Binding pKi = 8.3 8.3 -12 4
Binding affinity to human recombinant adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated adenylyl cyclase activity after 20 minsBinding affinity to human recombinant adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated adenylyl cyclase activity after 20 mins
ChEMBL 343 5 1 7 0.6 CN(C)CCOc1ccc(-c2nc3c([nH]2)c(=O)n(C)c(=O)n3C)cc1 10.1016/j.ejmech.2014.01.045
CHEMBL3121720 105513 None 0 Human Binding pKi = 8.3 8.3 -12 4
Binding affinity to human recombinant adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated adenylyl cyclase activity after 20 minsBinding affinity to human recombinant adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated adenylyl cyclase activity after 20 mins
ChEMBL 343 5 1 7 0.6 CN(C)CCOc1ccc(-c2nc3c([nH]2)c(=O)n(C)c(=O)n3C)cc1 10.1016/j.ejmech.2014.01.045
126079 4100 None 31 Human Binding pKi = 7.4 7.4 -2 8
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 386 8 2 7 1.8 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)O 10.1021/jm0104318
451 4100 None 31 Human Binding pKi = 7.4 7.4 -2 8
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 386 8 2 7 1.8 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)O 10.1021/jm0104318
CHEMBL27041 4100 None 31 Human Binding pKi = 7.4 7.4 -2 8
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 386 8 2 7 1.8 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)O 10.1021/jm0104318
10863425 56738 None 0 Human Binding pKi = 7.4 7.4 2 4
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 32-51Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 32-51
ChEMBL 456 4 2 8 4.7 CCn1cc2c(nc(NC(=O)Nc3ccc(Cl)c(Cl)c3)n3nc(-c4ccco4)nc23)n1 10.1021/jm0109614
CHEMBL164275 56738 None 0 Human Binding pKi = 7.4 7.4 2 4
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 32-51Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 32-51
ChEMBL 456 4 2 8 4.7 CCn1cc2c(nc(NC(=O)Nc3ccc(Cl)c(Cl)c3)n3nc(-c4ccco4)nc23)n1 10.1021/jm0109614
135874430 160130 None 0 Human Binding pKi = 7.4 7.4 - 1
Displacement of [3H]MRE2029F20 from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]MRE2029F20 from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 517 8 2 8 3.8 CCCn1c(=O)c2[nH]c(-c3cc(C)n(CC(=O)Nc4ccc(Cl)c(Cl)c4)n3)nc2n(CCC)c1=O 10.1016/j.bmc.2007.11.058
CHEMBL410895 160130 None 0 Human Binding pKi = 7.4 7.4 - 1
Displacement of [3H]MRE2029F20 from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]MRE2029F20 from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 517 8 2 8 3.8 CCCn1c(=O)c2[nH]c(-c3cc(C)n(CC(=O)Nc4ccc(Cl)c(Cl)c4)n3)nc2n(CCC)c1=O 10.1016/j.bmc.2007.11.058
11596614 77099 None 0 Human Binding pKi = 7.4 7.4 -1 3
Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cellsDisplacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells
ChEMBL 406 7 1 7 2.9 CCCn1c(=O)c2nc(-c3cnn(Cc4ccc(C)cc4)c3)[nH]c2n(CCC)c1=O 10.1021/jm051268+
CHEMBL207524 77099 None 0 Human Binding pKi = 7.4 7.4 -1 3
Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cellsDisplacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells
ChEMBL 406 7 1 7 2.9 CCCn1c(=O)c2nc(-c3cnn(Cc4ccc(C)cc4)c3)[nH]c2n(CCC)c1=O 10.1021/jm051268+
CHEMBL5094532 215501 None 0 Human Binding pKi = 7.4 7.4 -2 3
Displacement of [3H]DPCPX from human A2BAR expressed in HEK293 cell membrane incubated for 30 mins by microbeta trilux scintillation counter analysisDisplacement of [3H]DPCPX from human A2BAR expressed in HEK293 cell membrane incubated for 30 mins by microbeta trilux scintillation counter analysis
ChEMBL None None None N#Cc1c(-c2ccccc2)nc(N)nc1-c1cccs1 10.1021/acs.jmedchem.1c01636
163215620 190343 None 0 Human Binding pKi = 7.4 7.4 -398 4
Displacement of [3H]DPCPX from human A2BAR expressed in HEK293 cells membrane assessed as inhibition constant preincubated for 5 mins followed by [3H]DPCPX addition and measured after 1.5 hrs by TopCount scintillation counting methodDisplacement of [3H]DPCPX from human A2BAR expressed in HEK293 cells membrane assessed as inhibition constant preincubated for 5 mins followed by [3H]DPCPX addition and measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 318 3 2 6 1.8 Nc1nc(C(=O)NCc2ccccn2)cn2c1nc1ccccc12 10.1021/acs.jmedchem.2c00101
CHEMBL5176737 190343 None 0 Human Binding pKi = 7.4 7.4 -398 4
Displacement of [3H]DPCPX from human A2BAR expressed in HEK293 cells membrane assessed as inhibition constant preincubated for 5 mins followed by [3H]DPCPX addition and measured after 1.5 hrs by TopCount scintillation counting methodDisplacement of [3H]DPCPX from human A2BAR expressed in HEK293 cells membrane assessed as inhibition constant preincubated for 5 mins followed by [3H]DPCPX addition and measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 318 3 2 6 1.8 Nc1nc(C(=O)NCc2ccccn2)cn2c1nc1ccccc12 10.1021/acs.jmedchem.2c00101
CHEMBL5203105 190343 None 0 Human Binding pKi = 7.4 7.4 -398 4
Displacement of [3H]DPCPX from human A2BAR expressed in HEK293 cells membrane assessed as inhibition constant preincubated for 5 mins followed by [3H]DPCPX addition and measured after 1.5 hrs by TopCount scintillation counting methodDisplacement of [3H]DPCPX from human A2BAR expressed in HEK293 cells membrane assessed as inhibition constant preincubated for 5 mins followed by [3H]DPCPX addition and measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 318 3 2 6 1.8 Nc1nc(C(=O)NCc2ccccn2)cn2c1nc1ccccc12 10.1021/acs.jmedchem.2c00101
49798161 10755 None 0 Human Binding pKi = 7.4 7.4 4 3
Displacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells after 30 minsDisplacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells after 30 mins
ChEMBL 537 6 1 9 3.6 COc1cc(OCc2nc(-c3ccc(Br)cc3)no2)ccc1-c1cc2c([nH]1)c(=O)n(C)c(=O)n2C 10.1016/j.ejmech.2010.03.011
CHEMBL1171379 10755 None 0 Human Binding pKi = 7.4 7.4 4 3
Displacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells after 30 minsDisplacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells after 30 mins
ChEMBL 537 6 1 9 3.6 COc1cc(OCc2nc(-c3ccc(Br)cc3)no2)ccc1-c1cc2c([nH]1)c(=O)n(C)c(=O)n2C 10.1016/j.ejmech.2010.03.011
2748294 41377 None 21 Human Binding pKi = 7.4 7.4 - 1
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 minsDisplacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 mins
ChEMBL 264 3 2 4 1.9 CC1=C(C(=O)OC(C)C)C(c2ccco2)NC(=O)N1 10.1021/acs.jmedchem.5b01586
CHEMBL1490082 41377 None 21 Human Binding pKi = 7.4 7.4 - 1
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 minsDisplacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 mins
ChEMBL 264 3 2 4 1.9 CC1=C(C(=O)OC(C)C)C(c2ccco2)NC(=O)N1 10.1021/acs.jmedchem.5b01586
2748294 41377 None 21 Human Binding pKi = 7.4 7.4 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes after 30 minsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes after 30 mins
ChEMBL 264 3 2 4 1.9 CC1=C(C(=O)OC(C)C)C(c2ccco2)NC(=O)N1 10.1021/acs.jmedchem.7b00138
CHEMBL1490082 41377 None 21 Human Binding pKi = 7.4 7.4 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes after 30 minsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes after 30 mins
ChEMBL 264 3 2 4 1.9 CC1=C(C(=O)OC(C)C)C(c2ccco2)NC(=O)N1 10.1021/acs.jmedchem.7b00138
2748294 41377 None 21 Human Binding pKi = 7.4 7.4 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 264 3 2 4 1.9 CC1=C(C(=O)OC(C)C)C(c2ccco2)NC(=O)N1 10.1021/acs.jmedchem.0c01431
CHEMBL1490082 41377 None 21 Human Binding pKi = 7.4 7.4 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 264 3 2 4 1.9 CC1=C(C(=O)OC(C)C)C(c2ccco2)NC(=O)N1 10.1021/acs.jmedchem.0c01431
2748294 41377 None 21 Human Binding pKi = 7.4 7.4 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by Scatchard plot analysisDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by Scatchard plot analysis
ChEMBL 264 3 2 4 1.9 CC1=C(C(=O)OC(C)C)C(c2ccco2)NC(=O)N1 10.1021/ml400185v
CHEMBL1490082 41377 None 21 Human Binding pKi = 7.4 7.4 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by Scatchard plot analysisDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by Scatchard plot analysis
ChEMBL 264 3 2 4 1.9 CC1=C(C(=O)OC(C)C)C(c2ccco2)NC(=O)N1 10.1021/ml400185v
2748294 41377 None 21 Human Binding pKi = 7.4 7.4 - 1
Displacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assayDisplacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assay
ChEMBL 264 3 2 4 1.9 CC1=C(C(=O)OC(C)C)C(c2ccco2)NC(=O)N1 10.1021/acs.jmedchem.9b01340
CHEMBL1490082 41377 None 21 Human Binding pKi = 7.4 7.4 - 1
Displacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assayDisplacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assay
ChEMBL 264 3 2 4 1.9 CC1=C(C(=O)OC(C)C)C(c2ccco2)NC(=O)N1 10.1021/acs.jmedchem.9b01340
10661707 161839 None 0 Human Binding pKi = 6.4 6.4 -8 4
Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 343-468Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 343-468
ChEMBL 297 1 1 8 2.1 CC(C)(C)n1cc2c(nc(N)n3nc(-c4ccco4)nc23)n1 10.1021/jm001047y
CHEMBL414620 161839 None 0 Human Binding pKi = 6.4 6.4 -8 4
Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 343-468Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 343-468
ChEMBL 297 1 1 8 2.1 CC(C)(C)n1cc2c(nc(N)n3nc(-c4ccco4)nc23)n1 10.1021/jm001047y
11162618 195502 None 0 Human Binding pKi = 6.4 6.4 -154 4
Binding affinity to adenosine A2B receptorBinding affinity to adenosine A2B receptor
ChEMBL 308 4 2 5 2.6 Cc1cccc(CNC(=O)c2cc(-c3ccco3)nc(N)n2)c1 10.1016/j.bmcl.2009.03.142
CHEMBL553449 195502 None 0 Human Binding pKi = 6.4 6.4 -154 4
Binding affinity to adenosine A2B receptorBinding affinity to adenosine A2B receptor
ChEMBL 308 4 2 5 2.6 Cc1cccc(CNC(=O)c2cc(-c3ccco3)nc(N)n2)c1 10.1016/j.bmcl.2009.03.142
156010620 177035 None 0 Human Binding pKi = 6.4 6.4 -79 2
Displacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting methodDisplacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting method
ChEMBL 323 3 2 6 2.6 CCOC(=O)C1=C(C)Nc2nc3ccccc3n2C1c1ncc[nH]1 10.1021/acs.jmedchem.0c00564
CHEMBL4632427 177035 None 0 Human Binding pKi = 6.4 6.4 -79 2
Displacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting methodDisplacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting method
ChEMBL 323 3 2 6 2.6 CCOC(=O)C1=C(C)Nc2nc3ccccc3n2C1c1ncc[nH]1 10.1021/acs.jmedchem.0c00564
162665941 182378 None 0 Human Binding pKi = 6.4 6.4 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 292 3 2 4 2.5 CC1=C(C(=O)OC2CCC2)C(c2ccsc2)NC(=O)N1 10.1021/acs.jmedchem.0c01431
CHEMBL4785137 182378 None 0 Human Binding pKi = 6.4 6.4 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 292 3 2 4 2.5 CC1=C(C(=O)OC2CCC2)C(c2ccsc2)NC(=O)N1 10.1021/acs.jmedchem.0c01431
14969717 203757 None 0 Human Binding pKi = 6.4 6.4 18 3
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 256 3 2 4 0.7 O=c1[nH]c2[nH]cnc2c(=O)n1CCc1ccccc1 10.1021/jm0104318
CHEMBL67949 203757 None 0 Human Binding pKi = 6.4 6.4 18 3
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 256 3 2 4 0.7 O=c1[nH]c2[nH]cnc2c(=O)n1CCc1ccccc1 10.1021/jm0104318
71681051 90205 None 0 Human Binding pKi = 6.4 6.4 -4 5
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells after 75 mins by liquid scintillation counting analysisDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells after 75 mins by liquid scintillation counting analysis
ChEMBL 338 5 1 4 3.9 Cc1ccc2nc(NC(=O)CCCc3ccccc3)sc(=O)c2c1 10.1021/jm400336x
CHEMBL2382420 90205 None 0 Human Binding pKi = 6.4 6.4 -4 5
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells after 75 mins by liquid scintillation counting analysisDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells after 75 mins by liquid scintillation counting analysis
ChEMBL 338 5 1 4 3.9 Cc1ccc2nc(NC(=O)CCCc3ccccc3)sc(=O)c2c1 10.1021/jm400336x
135440168 99955 None 0 Human Binding pKi = 7.4 7.4 23 2
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 466 9 2 10 1.5 CCCn1c(=O)c2nc(-c3cc(OCC(=O)Nc4ccncc4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
CHEMBL286420 99955 None 0 Human Binding pKi = 7.4 7.4 23 2
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 466 9 2 10 1.5 CCCn1c(=O)c2nc(-c3cc(OCC(=O)Nc4ccncc4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
66894243 158587 None 0 Human Binding pKi = 7.4 7.4 - 1
Displacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting methodDisplacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting method
ChEMBL 493 8 1 8 2.8 CCCn1c(=O)c2[nH]c(-c3cnn(CC4CC(=O)N(c5cccc(F)c5)C4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2016.11.007
CHEMBL4092017 158587 None 0 Human Binding pKi = 7.4 7.4 - 1
Displacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting methodDisplacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting method
ChEMBL 493 8 1 8 2.8 CCCn1c(=O)c2[nH]c(-c3cnn(CC4CC(=O)N(c5cccc(F)c5)C4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2016.11.007
46880373 5937 None 0 Human Binding pKi = 7.4 7.4 -3 4
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 253 3 1 4 2.6 N#Cc1ccc(NC(=O)C2CC2)nc1-c1ccco1 10.1016/j.bmcl.2010.01.045
CHEMBL1079801 5937 None 0 Human Binding pKi = 7.4 7.4 -3 4
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 253 3 1 4 2.6 N#Cc1ccc(NC(=O)C2CC2)nc1-c1ccco1 10.1016/j.bmcl.2010.01.045
11656109 78380 None 0 Human Binding pKi = 6.4 6.4 - 1
Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cellsDisplacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells
ChEMBL 490 8 1 8 3.6 CCCn1c(=O)c2nc(-c3cnn(Cc4ccc(OC)c(C(F)(F)F)c4)c3)[nH]c2n(CCC)c1=O 10.1021/jm051268+
CHEMBL211038 78380 None 0 Human Binding pKi = 6.4 6.4 - 1
Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cellsDisplacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells
ChEMBL 490 8 1 8 3.6 CCCn1c(=O)c2nc(-c3cnn(Cc4ccc(OC)c(C(F)(F)F)c4)c3)[nH]c2n(CCC)c1=O 10.1021/jm051268+
9893136 98759 None 0 Human Binding pKi = 4.4 4.4 -19498 6
Displacement of [3H]- ZM-241385 from human adenosine A2B receptor expressed in HEK cellsDisplacement of [3H]- ZM-241385 from human adenosine A2B receptor expressed in HEK cells
ChEMBL 527 5 4 8 2.0 OC[C@@]12C[C@@H]1[C@@H](n1cnc3c(NCc4cccc(I)c4)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1021/jm9905965
CHEMBL27809 98759 None 0 Human Binding pKi = 4.4 4.4 -19498 6
Displacement of [3H]- ZM-241385 from human adenosine A2B receptor expressed in HEK cellsDisplacement of [3H]- ZM-241385 from human adenosine A2B receptor expressed in HEK cells
ChEMBL 527 5 4 8 2.0 OC[C@@]12C[C@@H]1[C@@H](n1cnc3c(NCc4cccc(I)c4)nc(Cl)nc31)[C@H](O)[C@@H]2O 10.1021/jm9905965
99562 99301 None 61 Human Binding pKi = 5.4 5.4 1 4
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 218 1 0 6 -0.9 C#CCn1c(=O)c2c(ncn2C)n(C)c1=O 10.1021/jm0104318
CHEMBL282038 99301 None 61 Human Binding pKi = 5.4 5.4 1 4
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 218 1 0 6 -0.9 C#CCn1c(=O)c2c(ncn2C)n(C)c1=O 10.1021/jm0104318
99562 99301 None 61 Human Binding pKi = 5.4 5.4 1 4
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 218 1 0 6 -0.9 C#CCn1c(=O)c2c(ncn2C)n(C)c1=O 10.1016/j.bmc.2013.09.044
CHEMBL282038 99301 None 61 Human Binding pKi = 5.4 5.4 1 4
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 218 1 0 6 -0.9 C#CCn1c(=O)c2c(ncn2C)n(C)c1=O 10.1016/j.bmc.2013.09.044
99562 99301 None 61 Human Binding pKi = 5.4 5.4 1 4
Displacement of [3H]PSB-603 from human adenosine A2B receptorDisplacement of [3H]PSB-603 from human adenosine A2B receptor
ChEMBL 218 1 0 6 -0.9 C#CCn1c(=O)c2c(ncn2C)n(C)c1=O 10.1016/j.bmc.2013.09.044
CHEMBL282038 99301 None 61 Human Binding pKi = 5.4 5.4 1 4
Displacement of [3H]PSB-603 from human adenosine A2B receptorDisplacement of [3H]PSB-603 from human adenosine A2B receptor
ChEMBL 218 1 0 6 -0.9 C#CCn1c(=O)c2c(ncn2C)n(C)c1=O 10.1016/j.bmc.2013.09.044
1922 202818 None 44 Human Binding pKi = 6.4 6.4 -26 6
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 256 1 1 5 0.6 Cn1c(=O)c2nc(-c3ccccc3)[nH]c2n(C)c1=O 10.1021/jm0104318
CHEMBL62350 202818 None 44 Human Binding pKi = 6.4 6.4 -26 6
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 256 1 1 5 0.6 Cn1c(=O)c2nc(-c3ccccc3)[nH]c2n(C)c1=O 10.1021/jm0104318
1922 202818 None 44 Human Binding pKi = 6.4 6.4 -26 6
Binding affinity for human HEK293 adenosine A2B receptor using [125I]ABOPX in CHO cell membranesBinding affinity for human HEK293 adenosine A2B receptor using [125I]ABOPX in CHO cell membranes
ChEMBL 256 1 1 5 0.6 Cn1c(=O)c2nc(-c3ccccc3)[nH]c2n(C)c1=O 10.1021/jm0310030
CHEMBL62350 202818 None 44 Human Binding pKi = 6.4 6.4 -26 6
Binding affinity for human HEK293 adenosine A2B receptor using [125I]ABOPX in CHO cell membranesBinding affinity for human HEK293 adenosine A2B receptor using [125I]ABOPX in CHO cell membranes
ChEMBL 256 1 1 5 0.6 Cn1c(=O)c2nc(-c3ccccc3)[nH]c2n(C)c1=O 10.1021/jm0310030
47104774 103849 None 0 Human Binding pKi = 6.4 6.4 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by Scatchard plot analysisDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by Scatchard plot analysis
ChEMBL 296 3 2 4 2.5 CC1=C(C(=O)OC(C)C)C(c2ccsc2)NC(=S)N1 10.1021/ml400185v
CHEMBL3091705 103849 None 0 Human Binding pKi = 6.4 6.4 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by Scatchard plot analysisDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by Scatchard plot analysis
ChEMBL 296 3 2 4 2.5 CC1=C(C(=O)OC(C)C)C(c2ccsc2)NC(=S)N1 10.1021/ml400185v
21958526 130708 None 0 Human Binding pKi = 7.4 7.4 -6 3
Binding affinity for adenosine A2b receptor by using as [3H]ZM-241385 (14 nM) radioligand in membranes from HEK-A2B cellsBinding affinity for adenosine A2b receptor by using as [3H]ZM-241385 (14 nM) radioligand in membranes from HEK-A2B cells
ChEMBL 520 9 1 9 4.7 CCCn1c(=O)c2nc(-c3ccc(OCc4nc(-c5cccc(Cl)c5)no4)cc3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2004.11.044
CHEMBL368442 130708 None 0 Human Binding pKi = 7.4 7.4 -6 3
Binding affinity for adenosine A2b receptor by using as [3H]ZM-241385 (14 nM) radioligand in membranes from HEK-A2B cellsBinding affinity for adenosine A2b receptor by using as [3H]ZM-241385 (14 nM) radioligand in membranes from HEK-A2B cells
ChEMBL 520 9 1 9 4.7 CCCn1c(=O)c2nc(-c3ccc(OCc4nc(-c5cccc(Cl)c5)no4)cc3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2004.11.044
46880420 6341 None 0 Human Binding pKi = 7.4 7.4 7 3
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 322 4 1 5 3.6 O=C(Nc1ccc(-c2ccncc2)c(-c2nccs2)n1)C1CC1 10.1016/j.bmcl.2010.01.045
CHEMBL1082006 6341 None 0 Human Binding pKi = 7.4 7.4 7 3
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 322 4 1 5 3.6 O=C(Nc1ccc(-c2ccncc2)c(-c2nccs2)n1)C1CC1 10.1016/j.bmcl.2010.01.045
90654601 110034 None 0 Human Binding pKi = 7.4 7.4 -4 2
Displacement of [3H]PSB603 from human adenosine A2B receptor expressed in CHO cell membranes after 2 hrs by beta scintillation counting analysisDisplacement of [3H]PSB603 from human adenosine A2B receptor expressed in CHO cell membranes after 2 hrs by beta scintillation counting analysis
ChEMBL 369 4 1 9 3.1 N#Cc1c(N)nc(SCc2cscn2)nc1-c1ccc2c(c1)OCO2 10.1021/jm401643m
CHEMBL3234965 110034 None 0 Human Binding pKi = 7.4 7.4 -4 2
Displacement of [3H]PSB603 from human adenosine A2B receptor expressed in CHO cell membranes after 2 hrs by beta scintillation counting analysisDisplacement of [3H]PSB603 from human adenosine A2B receptor expressed in CHO cell membranes after 2 hrs by beta scintillation counting analysis
ChEMBL 369 4 1 9 3.1 N#Cc1c(N)nc(SCc2cscn2)nc1-c1ccc2c(c1)OCO2 10.1021/jm401643m
44406617 72636 None 0 Human Binding pKi = 7.4 7.4 22 3
Displacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cellsDisplacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cells
ChEMBL 528 8 1 10 3.7 CCCn1c(=O)c2nc(-c3cnn(Cc4nc(-c5cccc(C(F)(F)F)c5)no4)c3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2005.10.002
CHEMBL199471 72636 None 0 Human Binding pKi = 7.4 7.4 22 3
Displacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cellsDisplacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cells
ChEMBL 528 8 1 10 3.7 CCCn1c(=O)c2nc(-c3cnn(Cc4nc(-c5cccc(C(F)(F)F)c5)no4)c3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2005.10.002
11420226 96350 None 0 Human Binding pKi = 7.4 7.4 4 3
Displacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 479 7 1 9 3.5 CCCn1c(=O)c2[nH]c(-c3cnn(Cc4cc(-c5ccc(Cl)cc5)on4)c3)nc2n(CC)c1=O 10.1021/jm7014815
CHEMBL261554 96350 None 0 Human Binding pKi = 7.4 7.4 4 3
Displacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 479 7 1 9 3.5 CCCn1c(=O)c2[nH]c(-c3cnn(Cc4cc(-c5ccc(Cl)cc5)on4)c3)nc2n(CC)c1=O 10.1021/jm7014815
24828056 156508 None 0 Human Binding pKi = 7.4 7.4 9 3
Displacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 288 3 2 6 0.5 CC(C)Cn1c(=O)c2[nH]c(-c3cn[nH]c3)nc2n(C)c1=O 10.1021/jm7014815
CHEMBL406775 156508 None 0 Human Binding pKi = 7.4 7.4 9 3
Displacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 288 3 2 6 0.5 CC(C)Cn1c(=O)c2[nH]c(-c3cn[nH]c3)nc2n(C)c1=O 10.1021/jm7014815
9970296 120469 None 0 Human Binding pKi = 7.4 7.4 -1 5
Inhibition of [3H]ZM-241385 binding to human adenosine A2B receptorInhibition of [3H]ZM-241385 binding to human adenosine A2B receptor
ChEMBL 269 3 2 3 2.1 CCCn1c(=O)[nH]c2cc(-c3ccccc3)[nH]c2c1=O 10.1021/jm011049y
CHEMBL35415 120469 None 0 Human Binding pKi = 7.4 7.4 -1 5
Inhibition of [3H]ZM-241385 binding to human adenosine A2B receptorInhibition of [3H]ZM-241385 binding to human adenosine A2B receptor
ChEMBL 269 3 2 3 2.1 CCCn1c(=O)[nH]c2cc(-c3ccccc3)[nH]c2c1=O 10.1021/jm011049y
155555919 174424 None 0 Human Binding pKi = 7.4 7.4 - 1
Displacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assayDisplacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assay
ChEMBL 377 3 1 6 4.0 CC1=C(C(=O)OCC(F)(F)F)C(c2ccoc2)n2c(nc3ccccc32)N1 10.1021/acs.jmedchem.9b01340
CHEMBL4552910 174424 None 0 Human Binding pKi = 7.4 7.4 - 1
Displacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assayDisplacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assay
ChEMBL 377 3 1 6 4.0 CC1=C(C(=O)OCC(F)(F)F)C(c2ccoc2)n2c(nc3ccccc32)N1 10.1021/acs.jmedchem.9b01340
11278089 84709 None 5 Human Binding pKi = 7.4 7.4 -1 4
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 303 4 1 3 4.2 CCC(=O)Nc1nc(-c2ccccc2)cc(-c2ccccc2)n1 10.1021/jm100843z
CHEMBL222718 84709 None 5 Human Binding pKi = 7.4 7.4 -1 4
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 303 4 1 3 4.2 CCC(=O)Nc1nc(-c2ccccc2)cc(-c2ccccc2)n1 10.1021/jm100843z
11568517 74496 None 0 Human Binding pKi = 7.4 7.4 20 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 446 7 1 6 2.7 CCN(Cc1ccccc1)C(=O)COc1ccc(-c2cc3c([nH]2)c(=O)n(C)c(=O)n3C)cc1 10.1021/jm0506221
CHEMBL202876 74496 None 0 Human Binding pKi = 7.4 7.4 20 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 446 7 1 6 2.7 CCN(Cc1ccccc1)C(=O)COc1ccc(-c2cc3c([nH]2)c(=O)n(C)c(=O)n3C)cc1 10.1021/jm0506221
44574281 178536 None 0 Human Binding pKi = 7.4 7.4 1 2
Displacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells by beta scintillation counterDisplacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells by beta scintillation counter
ChEMBL 547 8 1 7 4.6 CCCn1c(=O)c2[nH]c(-c3ccc(COC(=O)N4CCN(c5ccc(F)cc5)CC4)cc3)cc2n(CCC)c1=O 10.1016/j.bmc.2009.03.062
CHEMBL466828 178536 None 0 Human Binding pKi = 7.4 7.4 1 2
Displacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells by beta scintillation counterDisplacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells by beta scintillation counter
ChEMBL 547 8 1 7 4.6 CCCn1c(=O)c2[nH]c(-c3ccc(COC(=O)N4CCN(c5ccc(F)cc5)CC4)cc3)cc2n(CCC)c1=O 10.1016/j.bmc.2009.03.062
14969715 203794 None 2 Human Binding pKi = 6.4 6.4 -91 5
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 208 3 2 4 0.2 CCCCn1c(=O)[nH]c2[nH]cnc2c1=O 10.1021/jm0104318
CHEMBL68278 203794 None 2 Human Binding pKi = 6.4 6.4 -91 5
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 208 3 2 4 0.2 CCCCn1c(=O)[nH]c2[nH]cnc2c1=O 10.1021/jm0104318
9858577 178672 None 0 Human Binding pKi = 6.4 6.4 -13 4
Displacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation countingDisplacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation counting
ChEMBL 327 3 1 8 2.1 Nc1nc(-c2cncs2)c2nnn(Cc3ccccc3F)c2n1 10.1021/jm800961g
CHEMBL467867 178672 None 0 Human Binding pKi = 6.4 6.4 -13 4
Displacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation countingDisplacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation counting
ChEMBL 327 3 1 8 2.1 Nc1nc(-c2cncs2)c2nnn(Cc3ccccc3F)c2n1 10.1021/jm800961g
76331767 103847 None 0 Human Binding pKi = 5.4 5.4 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 264 3 1 4 1.8 CCOC(=O)C1=C(C)N(C)C(=O)NC1c1ccoc1 10.1021/acs.jmedchem.0c01431
CHEMBL3091702 103847 None 0 Human Binding pKi = 5.4 5.4 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 264 3 1 4 1.8 CCOC(=O)C1=C(C)N(C)C(=O)NC1c1ccoc1 10.1021/acs.jmedchem.0c01431
76331767 103847 None 0 Human Binding pKi = 5.4 5.4 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by Scatchard plot analysisDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by Scatchard plot analysis
ChEMBL 264 3 1 4 1.8 CCOC(=O)C1=C(C)N(C)C(=O)NC1c1ccoc1 10.1021/ml400185v
CHEMBL3091702 103847 None 0 Human Binding pKi = 5.4 5.4 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by Scatchard plot analysisDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by Scatchard plot analysis
ChEMBL 264 3 1 4 1.8 CCOC(=O)C1=C(C)N(C)C(=O)NC1c1ccoc1 10.1021/ml400185v
162672711 183229 None 0 Human Binding pKi = 6.4 6.4 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 276 4 2 4 1.9 CC1=C(C(=O)OCC2CC2)C(c2ccoc2)NC(=O)N1 10.1021/acs.jmedchem.0c01431
CHEMBL4796169 183229 None 0 Human Binding pKi = 6.4 6.4 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 276 4 2 4 1.9 CC1=C(C(=O)OCC2CC2)C(c2ccoc2)NC(=O)N1 10.1021/acs.jmedchem.0c01431
44452514 95820 None 0 Human Binding pKi = 6.4 6.4 -5 3
Displacement of [3]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 323 6 1 7 3.0 COCCCNc1nc2ccccc2n2nc(-c3ccco3)nc12 10.1016/j.bmc.2007.10.103
CHEMBL258848 95820 None 0 Human Binding pKi = 6.4 6.4 -5 3
Displacement of [3]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 323 6 1 7 3.0 COCCCNc1nc2ccccc2n2nc(-c3ccco3)nc12 10.1016/j.bmc.2007.10.103
10834513 38798 None 0 Human Binding pKi = 5.4 5.4 -12 4
Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 3828-4817Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 3828-4817
ChEMBL 395 4 1 8 3.7 Nc1nc2nn(CCc3cccc4ccccc34)cc2c2nc(-c3ccco3)nn12 10.1021/jm001047y
CHEMBL146658 38798 None 0 Human Binding pKi = 5.4 5.4 -12 4
Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 3828-4817Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 3828-4817
ChEMBL 395 4 1 8 3.7 Nc1nc2nn(CCc3cccc4ccccc34)cc2c2nc(-c3ccco3)nn12 10.1021/jm001047y
11420910 96939 None 0 Human Binding pKi = 7.4 7.4 -9 4
Binding affinity for human adenosine A2B receptor using [3H]-PSB-298 in CHO cell membranesBinding affinity for human adenosine A2B receptor using [3H]-PSB-298 in CHO cell membranes
ChEMBL 513 9 1 10 3.0 CCCn1c(=O)c2nc(-c3ccc(S(=O)(=O)Oc4cccc([N+](=O)[O-])c4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm0310030
CHEMBL266099 96939 None 0 Human Binding pKi = 7.4 7.4 -9 4
Binding affinity for human adenosine A2B receptor using [3H]-PSB-298 in CHO cell membranesBinding affinity for human adenosine A2B receptor using [3H]-PSB-298 in CHO cell membranes
ChEMBL 513 9 1 10 3.0 CCCn1c(=O)c2nc(-c3ccc(S(=O)(=O)Oc4cccc([N+](=O)[O-])c4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm0310030
66894271 157460 None 0 Human Binding pKi = 7.4 7.4 - 1
Displacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting methodDisplacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting method
ChEMBL 493 8 1 8 2.8 CCCn1c(=O)c2[nH]c(-c3cnn(CC4CCN(c5cccc(F)c5)C4=O)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2016.11.007
CHEMBL4079189 157460 None 0 Human Binding pKi = 7.4 7.4 - 1
Displacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting methodDisplacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting method
ChEMBL 493 8 1 8 2.8 CCCn1c(=O)c2[nH]c(-c3cnn(CC4CCN(c5cccc(F)c5)C4=O)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2016.11.007
53325341 58023 None 0 Human Binding pKi = 7.4 7.4 14 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 307 4 1 6 2.5 O=C(Nc1cnc(-c2ccncc2)c(-c2cnco2)n1)C1CC1 10.1021/ml100249e
CHEMBL1672625 58023 None 0 Human Binding pKi = 7.4 7.4 14 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 307 4 1 6 2.5 O=C(Nc1cnc(-c2ccncc2)c(-c2cnco2)n1)C1CC1 10.1021/ml100249e
21874661 190473 None 0 Human Binding pKi = 7.4 7.4 -60 4
Displacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation countingDisplacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation counting
ChEMBL 325 3 2 8 1.8 Nc1nc(-c2ccco2)c2nnn(Cc3ccc(N)c(F)c3)c2n1 10.1021/jm800961g
CHEMBL517886 190473 None 0 Human Binding pKi = 7.4 7.4 -60 4
Displacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation countingDisplacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation counting
ChEMBL 325 3 2 8 1.8 Nc1nc(-c2ccco2)c2nnn(Cc3ccc(N)c(F)c3)c2n1 10.1021/jm800961g
76324530 103845 None 0 Human Binding pKi = 7.4 7.4 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 266 3 2 4 1.6 CCOC(=O)C1=C(C)NC(=S)NC1c1ccoc1 10.1021/acs.jmedchem.0c01431
CHEMBL3091700 103845 None 0 Human Binding pKi = 7.4 7.4 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 266 3 2 4 1.6 CCOC(=O)C1=C(C)NC(=S)NC1c1ccoc1 10.1021/acs.jmedchem.0c01431
76324530 103845 None 0 Human Binding pKi = 7.4 7.4 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by Scatchard plot analysisDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by Scatchard plot analysis
ChEMBL 266 3 2 4 1.6 CCOC(=O)C1=C(C)NC(=S)NC1c1ccoc1 10.1021/ml400185v
CHEMBL3091700 103845 None 0 Human Binding pKi = 7.4 7.4 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by Scatchard plot analysisDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by Scatchard plot analysis
ChEMBL 266 3 2 4 1.6 CCOC(=O)C1=C(C)NC(=S)NC1c1ccoc1 10.1021/ml400185v
44451790 95988 None 0 Human Binding pKi = 7.4 7.4 -24 3
Displacement of [3H]DPCPX from human A2BAR expressed in HEK293 cell membrane incubated for 30 mins by microbeta trilux scintillation counter analysisDisplacement of [3H]DPCPX from human A2BAR expressed in HEK293 cell membrane incubated for 30 mins by microbeta trilux scintillation counter analysis
ChEMBL 316 2 1 6 3.0 N#Cc1c(-c2ccccc2)nc(N)nc1-c1ccc2c(c1)OCO2 10.1021/acs.jmedchem.1c01636
CHEMBL259607 95988 None 0 Human Binding pKi = 7.4 7.4 -24 3
Displacement of [3H]DPCPX from human A2BAR expressed in HEK293 cell membrane incubated for 30 mins by microbeta trilux scintillation counter analysisDisplacement of [3H]DPCPX from human A2BAR expressed in HEK293 cell membrane incubated for 30 mins by microbeta trilux scintillation counter analysis
ChEMBL 316 2 1 6 3.0 N#Cc1c(-c2ccccc2)nc(N)nc1-c1ccc2c(c1)OCO2 10.1021/acs.jmedchem.1c01636
156019165 177996 None 0 Human Binding pKi = 7.4 7.4 - 1
Displacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting methodDisplacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting method
ChEMBL 338 3 1 7 3.3 CC1=C(C(=O)OC(C)C)C(c2cocn2)n2c(nc3ccccc32)N1 10.1021/acs.jmedchem.0c00564
CHEMBL4646279 177996 None 0 Human Binding pKi = 7.4 7.4 - 1
Displacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting methodDisplacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting method
ChEMBL 338 3 1 7 3.3 CC1=C(C(=O)OC(C)C)C(c2cocn2)n2c(nc3ccccc32)N1 10.1021/acs.jmedchem.0c00564
CHEMBL5082650 214815 None 0 Human Binding pKi = 7.4 7.4 -10 7
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells by liquid scintillation counting analysisDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells by liquid scintillation counting analysis
ChEMBL None None None Nc1nc(-c2ccccc2)c2c(n1)-c1cc(OCCCN3CCCCC3)ccc1C2=O 10.1021/acs.jmedchem.0c00914
11595592 72310 None 0 Human Binding pKi = 7.4 7.4 93 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 357 6 2 6 1.6 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)O)cc3)cc2n(C)c1=O 10.1021/jm0506221
CHEMBL198345 72310 None 0 Human Binding pKi = 7.4 7.4 93 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 357 6 2 6 1.6 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)O)cc3)cc2n(C)c1=O 10.1021/jm0506221
11611016 72695 None 0 Human Binding pKi = 7.4 7.4 22 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 399 8 2 6 2.8 CCCn1c(=O)c2[nH]c(-c3ccc(OC(C)C(=O)O)cc3)cc2n(CCC)c1=O 10.1021/jm0506221
CHEMBL199697 72695 None 0 Human Binding pKi = 7.4 7.4 22 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 399 8 2 6 2.8 CCCn1c(=O)c2[nH]c(-c3ccc(OC(C)C(=O)O)cc3)cc2n(CCC)c1=O 10.1021/jm0506221
44451224 159388 None 0 Human Binding pKi = 7.4 7.4 6 3
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 474 5 1 7 2.2 COc1cc(OCC(=O)N2CCc3ccccc3C2)ccc1-c1cc2c([nH]1)c(=O)n(C)c(=O)n2C 10.1016/j.bmc.2008.01.002
CHEMBL410066 159388 None 0 Human Binding pKi = 7.4 7.4 6 3
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 474 5 1 7 2.2 COc1cc(OCC(=O)N2CCc3ccccc3C2)ccc1-c1cc2c([nH]1)c(=O)n(C)c(=O)n2C 10.1016/j.bmc.2008.01.002
11143352 200149 None 0 Human Binding pKi = 7.4 7.4 -1 3
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 378 6 0 7 2.5 CCCn1c(=O)c2c(nc(Cc3ccccc3)n2C)n(Cc2ccco2)c1=O 10.1016/j.bmc.2009.07.034
CHEMBL596346 200149 None 0 Human Binding pKi = 7.4 7.4 -1 3
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 378 6 0 7 2.5 CCCn1c(=O)c2c(nc(Cc3ccccc3)n2C)n(Cc2ccco2)c1=O 10.1016/j.bmc.2009.07.034
9950776 83197 None 0 Human Binding pKi = 6.4 6.4 -707 4
Displacement of [125I]3-(4-aminobenzyl)-8-phenyloxyacetate-1-propyl-xanthine from human adenosine A2B receptorDisplacement of [125I]3-(4-aminobenzyl)-8-phenyloxyacetate-1-propyl-xanthine from human adenosine A2B receptor
ChEMBL 360 5 2 6 2.0 CCCn1c(=O)c2nc(C34CCC(O)(CC3)CC4)[nH]c2n(CCC)c1=O 10.1021/jm060539t
CHEMBL218458 83197 None 0 Human Binding pKi = 6.4 6.4 -707 4
Displacement of [125I]3-(4-aminobenzyl)-8-phenyloxyacetate-1-propyl-xanthine from human adenosine A2B receptorDisplacement of [125I]3-(4-aminobenzyl)-8-phenyloxyacetate-1-propyl-xanthine from human adenosine A2B receptor
ChEMBL 360 5 2 6 2.0 CCCn1c(=O)c2nc(C34CCC(O)(CC3)CC4)[nH]c2n(CCC)c1=O 10.1021/jm060539t
21958522 64695 None 0 Human Binding pKi = 6.4 6.4 - 1
Binding affinity for adenosine A2b receptor by using as [3H]ZM-241385 (14 nM) radioligand in membranes from HEK-A2B cellsBinding affinity for adenosine A2b receptor by using as [3H]ZM-241385 (14 nM) radioligand in membranes from HEK-A2B cells
ChEMBL 500 9 1 9 4.3 CCCn1c(=O)c2nc(-c3ccc(OCc4noc(-c5ccccc5C)n4)cc3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2004.11.044
CHEMBL181873 64695 None 0 Human Binding pKi = 6.4 6.4 - 1
Binding affinity for adenosine A2b receptor by using as [3H]ZM-241385 (14 nM) radioligand in membranes from HEK-A2B cellsBinding affinity for adenosine A2b receptor by using as [3H]ZM-241385 (14 nM) radioligand in membranes from HEK-A2B cells
ChEMBL 500 9 1 9 4.3 CCCn1c(=O)c2nc(-c3ccc(OCc4noc(-c5ccccc5C)n4)cc3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2004.11.044
44588439 175555 None 0 Human Binding pKi = 7.4 7.4 1 2
Displacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cells
ChEMBL 327 5 2 5 2.7 CCCn1c(=O)c2[nH]c(-c3ccc(O)cc3)cc2n(CCC)c1=O 10.1016/j.bmc.2008.09.067
CHEMBL457881 175555 None 0 Human Binding pKi = 7.4 7.4 1 2
Displacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cells
ChEMBL 327 5 2 5 2.7 CCCn1c(=O)c2[nH]c(-c3ccc(O)cc3)cc2n(CCC)c1=O 10.1016/j.bmc.2008.09.067
11611580 78235 None 0 Human Binding pKi = 7.4 7.4 8 3
Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cellsDisplacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells
ChEMBL 424 7 1 7 3.1 CCCn1c(=O)c2nc(-c3cnn(Cc4cccc(C)c4F)c3)[nH]c2n(CCC)c1=O 10.1021/jm051268+
CHEMBL210609 78235 None 0 Human Binding pKi = 7.4 7.4 8 3
Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cellsDisplacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells
ChEMBL 424 7 1 7 3.1 CCCn1c(=O)c2nc(-c3cnn(Cc4cccc(C)c4F)c3)[nH]c2n(CCC)c1=O 10.1021/jm051268+
2690 903 None 66 Human Binding pKi = 7.4 7.4 -30 9
Inhibition of human recombinant adenosine receptor A2bInhibition of human recombinant adenosine receptor A2b
ChEMBL 285 1 1 6 2.8 Clc1ccc2c(c1)c1nc(nn1c(n2)N)c1ccco1 10.1021/jm4011669
384 903 None 66 Human Binding pKi = 7.4 7.4 -30 9
Inhibition of human recombinant adenosine receptor A2bInhibition of human recombinant adenosine receptor A2b
ChEMBL 285 1 1 6 2.8 Clc1ccc2c(c1)c1nc(nn1c(n2)N)c1ccco1 10.1021/jm4011669
CHEMBL16687 903 None 66 Human Binding pKi = 7.4 7.4 -30 9
Inhibition of human recombinant adenosine receptor A2bInhibition of human recombinant adenosine receptor A2b
ChEMBL 285 1 1 6 2.8 Clc1ccc2c(c1)c1nc(nn1c(n2)N)c1ccco1 10.1021/jm4011669
11663050 141090 None 0 Human Binding pKi = 7.4 7.4 1 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 482 5 2 6 3.0 Cn1c(=O)c2[nH]c(-c3cccc(OCC(=O)Nc4ccc(Br)cc4)c3)cc2n(C)c1=O 10.1021/jm0506221
CHEMBL382663 141090 None 0 Human Binding pKi = 7.4 7.4 1 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 482 5 2 6 3.0 Cn1c(=O)c2[nH]c(-c3cccc(OCC(=O)Nc4ccc(Br)cc4)c3)cc2n(C)c1=O 10.1021/jm0506221
24950846 170512 None 0 Human Binding pKi = 6.4 6.4 -28 3
Displacement of [3H]MRS1754 from human adenosine A2B receptor expressed in CHO cell membraneDisplacement of [3H]MRS1754 from human adenosine A2B receptor expressed in CHO cell membrane
ChEMBL 265 2 1 5 3.4 Cc1ccc(-c2cc(-c3ccco3)nc(N)c2C#N)o1 10.1021/jm701594y
CHEMBL444953 170512 None 0 Human Binding pKi = 6.4 6.4 -28 3
Displacement of [3H]MRS1754 from human adenosine A2B receptor expressed in CHO cell membraneDisplacement of [3H]MRS1754 from human adenosine A2B receptor expressed in CHO cell membrane
ChEMBL 265 2 1 5 3.4 Cc1ccc(-c2cc(-c3ccco3)nc(N)c2C#N)o1 10.1021/jm701594y
21874692 188805 None 0 Human Binding pKi = 6.4 6.4 -15 4
Displacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation countingDisplacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation counting
ChEMBL 337 4 1 9 2.0 Nc1nc(-c2ccco2)c2nnn(Cc3ccc([N+](=O)[O-])cc3)c2n1 10.1021/jm800961g
CHEMBL505977 188805 None 0 Human Binding pKi = 6.4 6.4 -15 4
Displacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation countingDisplacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation counting
ChEMBL 337 4 1 9 2.0 Nc1nc(-c2ccco2)c2nnn(Cc3ccc([N+](=O)[O-])cc3)c2n1 10.1021/jm800961g
142609112 182140 None 0 Human Binding pKi = 6.4 6.4 -131 4
Inhibition of FRET-labelled CA200645 binding to human adenosine 2B receptor expressed in CHO cells incubated for 2 hr by TR-FRET assayInhibition of FRET-labelled CA200645 binding to human adenosine 2B receptor expressed in CHO cells incubated for 2 hr by TR-FRET assay
ChEMBL 309 4 2 6 2.0 Cc1cccnc1CNC(=O)c1cnc(-c2ccco2)nc1N 10.1021/acs.jmedchem.0c00237
CHEMBL4782266 182140 None 0 Human Binding pKi = 6.4 6.4 -131 4
Inhibition of FRET-labelled CA200645 binding to human adenosine 2B receptor expressed in CHO cells incubated for 2 hr by TR-FRET assayInhibition of FRET-labelled CA200645 binding to human adenosine 2B receptor expressed in CHO cells incubated for 2 hr by TR-FRET assay
ChEMBL 309 4 2 6 2.0 Cc1cccnc1CNC(=O)c1cnc(-c2ccco2)nc1N 10.1021/acs.jmedchem.0c00237
21874764 189211 None 0 Human Binding pKi = 6.4 6.4 -3 4
Displacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation countingDisplacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation counting
ChEMBL 349 4 2 8 2.1 CC(=O)Nc1ccc(Cn2nnc3c(-c4ccco4)nc(N)nc32)cc1 10.1021/jm800961g
CHEMBL511413 189211 None 0 Human Binding pKi = 6.4 6.4 -3 4
Displacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation countingDisplacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation counting
ChEMBL 349 4 2 8 2.1 CC(=O)Nc1ccc(Cn2nnc3c(-c4ccco4)nc(N)nc32)cc1 10.1021/jm800961g
11808022 183563 None 0 Human Binding pKi = 5.4 5.4 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 278 2 2 4 2.2 CC1=C(C(=O)OC(C)(C)C)C(c2ccoc2)NC(=O)N1 10.1021/acs.jmedchem.0c01431
CHEMBL4800327 183563 None 0 Human Binding pKi = 5.4 5.4 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 278 2 2 4 2.2 CC1=C(C(=O)OC(C)(C)C)C(c2ccoc2)NC(=O)N1 10.1021/acs.jmedchem.0c01431
11289861 195291 None 0 Human Binding pKi = 6.4 6.4 -63 4
Binding affinity to adenosine A2B receptorBinding affinity to adenosine A2B receptor
ChEMBL 310 4 3 7 1.2 Nc1cccc(CNC(=O)c2cc(-c3ccco3)nc(N)n2)n1 10.1016/j.bmcl.2009.03.142
CHEMBL551373 195291 None 0 Human Binding pKi = 6.4 6.4 -63 4
Binding affinity to adenosine A2B receptorBinding affinity to adenosine A2B receptor
ChEMBL 310 4 3 7 1.2 Nc1cccc(CNC(=O)c2cc(-c3ccco3)nc(N)n2)n1 10.1016/j.bmcl.2009.03.142
4314924 177817 None 4 Human Binding pKi = 6.4 6.4 - 1
Displacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting methodDisplacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting method
ChEMBL 322 3 2 5 3.2 CCOC(=O)C1=C(C)Nc2nc3ccccc3n2C1c1cc[nH]c1 10.1021/acs.jmedchem.0c00564
CHEMBL4643705 177817 None 4 Human Binding pKi = 6.4 6.4 - 1
Displacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting methodDisplacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting method
ChEMBL 322 3 2 5 3.2 CCOC(=O)C1=C(C)Nc2nc3ccccc3n2C1c1cc[nH]c1 10.1021/acs.jmedchem.0c00564
11091600 83320 None 0 Human Binding pKi = 7.4 7.4 -2 3
Displacement of [3H]- DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]- DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 449 6 1 10 3.2 COc1ccc(CC(=O)Nc2nc3nn(C)c(SC)c3c3nc(-c4ccco4)nn23)cc1 10.1021/jm021023m
CHEMBL21910 83320 None 0 Human Binding pKi = 7.4 7.4 -2 3
Displacement of [3H]- DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]- DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 449 6 1 10 3.2 COc1ccc(CC(=O)Nc2nc3nn(C)c(SC)c3c3nc(-c4ccco4)nn23)cc1 10.1021/jm021023m
24827552 96229 None 0 Human Binding pKi = 7.4 7.4 6 4
Displacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 379 5 1 8 1.9 CCCn1c(=O)c2[nH]c(-c3cnn(-c4ccc(C)nc4)c3)nc2n(CC)c1=O 10.1021/jm7014815
CHEMBL260878 96229 None 0 Human Binding pKi = 7.4 7.4 6 4
Displacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 379 5 1 8 1.9 CCCn1c(=O)c2[nH]c(-c3cnn(-c4ccc(C)nc4)c3)nc2n(CC)c1=O 10.1021/jm7014815
CHEMBL5088876 215184 None 0 Human Binding pKi = 7.4 7.4 -25 3
Displacement of [3H]DPCPX from human A2BAR expressed in HEK293 cell membrane incubated for 30 mins by microbeta trilux scintillation counter analysisDisplacement of [3H]DPCPX from human A2BAR expressed in HEK293 cell membrane incubated for 30 mins by microbeta trilux scintillation counter analysis
ChEMBL None None None COc1cc(OC)cc(-c2nc(N)nc(-c3ccccc3)c2C#N)c1 10.1021/acs.jmedchem.1c01636
11508721 72266 None 0 Human Binding pKi = 7.3 7.3 16 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 357 6 2 6 1.6 CCCn1c(=O)n(C)c(=O)c2[nH]c(-c3ccc(OCC(=O)O)cc3)cc21 10.1021/jm0506221
CHEMBL198243 72266 None 0 Human Binding pKi = 7.3 7.3 16 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 357 6 2 6 1.6 CCCn1c(=O)n(C)c(=O)c2[nH]c(-c3ccc(OCC(=O)O)cc3)cc21 10.1021/jm0506221
9890003 119411 None 0 Human Binding pKi = 6.4 6.4 -5 4
Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 432-469Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 432-469
ChEMBL 450 3 2 8 4.8 CC(C)(C)n1cc2c(nc(NC(=O)Nc3cccc(Cl)c3)n3nc(-c4ccco4)nc23)n1 10.1021/jm001047y
CHEMBL344724 119411 None 0 Human Binding pKi = 6.4 6.4 -5 4
Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 432-469Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 432-469
ChEMBL 450 3 2 8 4.8 CC(C)(C)n1cc2c(nc(NC(=O)Nc3cccc(Cl)c3)n3nc(-c4ccco4)nc23)n1 10.1021/jm001047y
145981689 166582 None 0 Human Binding pKi = 6.3 6.3 -3 3
Displacement of [3H]PSB-602 from human adenosine A2B receptor expressed in CHO cell membranesDisplacement of [3H]PSB-602 from human adenosine A2B receptor expressed in CHO cell membranes
ChEMBL 579 14 1 10 2.6 CCCn1c(=O)c2c(nc3n2CCCN3CCc2ccc(OCC(=O)NCCCN3CCCC3)cc2)n(CCC)c1=O 10.1039/C8MD00070K
CHEMBL4280069 166582 None 0 Human Binding pKi = 6.3 6.3 -3 3
Displacement of [3H]PSB-602 from human adenosine A2B receptor expressed in CHO cell membranesDisplacement of [3H]PSB-602 from human adenosine A2B receptor expressed in CHO cell membranes
ChEMBL 579 14 1 10 2.6 CCCn1c(=O)c2c(nc3n2CCCN3CCc2ccc(OCC(=O)NCCCN3CCCC3)cc2)n(CCC)c1=O 10.1039/C8MD00070K
44390551 168339 None 0 Human Binding pKi = 5.3 5.3 - 1
Binding affinity for adenosine A2b receptor by using as [3H]ZM-241385 (14 nM) radioligand in membranes from HEK-A2B cellsBinding affinity for adenosine A2b receptor by using as [3H]ZM-241385 (14 nM) radioligand in membranes from HEK-A2B cells
ChEMBL 511 9 1 10 3.9 CCCn1c(=O)c2nc(-c3ccc(OCc4nc(-c5ccc(C#N)cc5)no4)cc3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2004.11.044
CHEMBL434334 168339 None 0 Human Binding pKi = 5.3 5.3 - 1
Binding affinity for adenosine A2b receptor by using as [3H]ZM-241385 (14 nM) radioligand in membranes from HEK-A2B cellsBinding affinity for adenosine A2b receptor by using as [3H]ZM-241385 (14 nM) radioligand in membranes from HEK-A2B cells
ChEMBL 511 9 1 10 3.9 CCCn1c(=O)c2nc(-c3ccc(OCc4nc(-c5ccc(C#N)cc5)no4)cc3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2004.11.044
2882256 31908 None 12 Human Binding pKi = 5.3 5.3 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 342 4 1 4 3.5 CC1=C(C(=O)OCc2ccccc2)C(c2ccsc2)NC(=O)N1C 10.1021/acs.jmedchem.0c01431
CHEMBL1407320 31908 None 12 Human Binding pKi = 5.3 5.3 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 342 4 1 4 3.5 CC1=C(C(=O)OCc2ccccc2)C(c2ccsc2)NC(=O)N1C 10.1021/acs.jmedchem.0c01431
12267228 176936 None 0 Human Binding pKi = 6.3 6.3 -3 2
Displacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cells
ChEMBL 269 1 1 4 1.5 Cc1ccc(-c2cc3c([nH]2)c(=O)n(C)c(=O)n3C)cc1 10.1016/j.bmc.2008.09.067
CHEMBL462095 176936 None 0 Human Binding pKi = 6.3 6.3 -3 2
Displacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cells
ChEMBL 269 1 1 4 1.5 Cc1ccc(-c2cc3c([nH]2)c(=O)n(C)c(=O)n3C)cc1 10.1016/j.bmc.2008.09.067
10938608 120111 None 0 Human Binding pKi = 7.3 7.3 -3 4
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 34-62Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 34-62
ChEMBL 416 5 2 8 4.1 CCCn1cc2c(nc(NC(=O)Nc3ccc(C)cc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm0109614
CHEMBL351075 120111 None 0 Human Binding pKi = 7.3 7.3 -3 4
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 34-62Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 34-62
ChEMBL 416 5 2 8 4.1 CCCn1cc2c(nc(NC(=O)Nc3ccc(C)cc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm0109614
24827443 96343 None 0 Human Binding pKi = 7.3 7.3 8 3
Displacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 365 5 1 8 1.6 CCCn1c(=O)c2[nH]c(-c3cnn(-c4ccccn4)c3)nc2n(CC)c1=O 10.1021/jm7014815
CHEMBL261525 96343 None 0 Human Binding pKi = 7.3 7.3 8 3
Displacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 365 5 1 8 1.6 CCCn1c(=O)c2[nH]c(-c3cnn(-c4ccccn4)c3)nc2n(CC)c1=O 10.1021/jm7014815
21874686 176819 None 0 Human Binding pKi = 7.3 7.3 -30 4
Displacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation countingDisplacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation counting
ChEMBL 307 3 2 8 1.7 Nc1ccc(Cn2nnc3c(-c4ccco4)nc(N)nc32)cc1 10.1021/jm800961g
CHEMBL460975 176819 None 0 Human Binding pKi = 7.3 7.3 -30 4
Displacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation countingDisplacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation counting
ChEMBL 307 3 2 8 1.7 Nc1ccc(Cn2nnc3c(-c4ccco4)nc(N)nc32)cc1 10.1021/jm800961g
136044105 120051 None 0 Human Binding pKi = 7.3 7.3 -1 3
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 358 6 2 7 2.1 CCCn1c(=O)c2[nH]c(-c3ccc(OC)cc3O)nc2n(CCC)c1=O 10.1021/jm0104318
CHEMBL350469 120051 None 0 Human Binding pKi = 7.3 7.3 -1 3
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 358 6 2 7 2.1 CCCn1c(=O)c2[nH]c(-c3ccc(OC)cc3O)nc2n(CCC)c1=O 10.1021/jm0104318
46228004 200057 None 0 Human Binding pKi = 7.3 7.3 2 3
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 426 6 0 7 2.8 Cn1c(Cc2c(F)cccc2F)nc2c1c(=O)n(CC1CC1)c(=O)n2Cc1ccco1 10.1016/j.bmc.2009.07.034
CHEMBL595657 200057 None 0 Human Binding pKi = 7.3 7.3 2 3
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 426 6 0 7 2.8 Cn1c(Cc2c(F)cccc2F)nc2c1c(=O)n(CC1CC1)c(=O)n2Cc1ccco1 10.1016/j.bmc.2009.07.034
11739282 196658 None 0 Human Binding pKi = 6.3 6.3 -269 4
Binding affinity to adenosine A2B receptorBinding affinity to adenosine A2B receptor
ChEMBL 339 6 2 7 1.8 COCc1cccc(CNC(=O)c2cc(-c3ccco3)nc(N)n2)n1 10.1016/j.bmcl.2009.03.142
CHEMBL564473 196658 None 0 Human Binding pKi = 6.3 6.3 -269 4
Binding affinity to adenosine A2B receptorBinding affinity to adenosine A2B receptor
ChEMBL 339 6 2 7 1.8 COCc1cccc(CNC(=O)c2cc(-c3ccco3)nc(N)n2)n1 10.1016/j.bmcl.2009.03.142
11739282 196658 None 0 Human Binding pKi = 6.3 6.3 -269 4
Inhibition of human recombinant adenosine receptor A2bInhibition of human recombinant adenosine receptor A2b
ChEMBL 339 6 2 7 1.8 COCc1cccc(CNC(=O)c2cc(-c3ccco3)nc(N)n2)n1 10.1021/jm4011669
CHEMBL564473 196658 None 0 Human Binding pKi = 6.3 6.3 -269 4
Inhibition of human recombinant adenosine receptor A2bInhibition of human recombinant adenosine receptor A2b
ChEMBL 339 6 2 7 1.8 COCc1cccc(CNC(=O)c2cc(-c3ccco3)nc(N)n2)n1 10.1021/jm4011669
14969716 203591 None 2 Human Binding pKi = 6.3 6.3 32 3
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 192 2 2 4 -0.4 C=CCn1c(=O)[nH]c2[nH]cnc2c1=O 10.1021/jm0104318
CHEMBL66899 203591 None 2 Human Binding pKi = 6.3 6.3 32 3
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 192 2 2 4 -0.4 C=CCn1c(=O)[nH]c2[nH]cnc2c1=O 10.1021/jm0104318
137650340 157520 None 0 Human Binding pKi = 6.3 6.3 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes after 30 minsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes after 30 mins
ChEMBL 290 3 2 5 1.7 CCOC(=O)C1=C(C)N/C(=N\C#N)NC1c1ccsc1 10.1021/acs.jmedchem.7b00138
CHEMBL4079899 157520 None 0 Human Binding pKi = 6.3 6.3 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes after 30 minsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes after 30 mins
ChEMBL 290 3 2 5 1.7 CCOC(=O)C1=C(C)N/C(=N\C#N)NC1c1ccsc1 10.1021/acs.jmedchem.7b00138
49870828 18792 None 0 Human Binding pKi = 5.3 5.3 -54 3
Displacement of [3H]DPCPX from human adenosine A2b receptor expressed in HEK293 cells after 30 minsDisplacement of [3H]DPCPX from human adenosine A2b receptor expressed in HEK293 cells after 30 mins
ChEMBL 373 3 0 7 3.5 Cc1nn(Cc2ccccc2)c(=O)c2ncn3nc(-c4ccsc4)cc3c12 10.1016/j.bmc.2010.09.043
CHEMBL1278102 18792 None 0 Human Binding pKi = 5.3 5.3 -54 3
Displacement of [3H]DPCPX from human adenosine A2b receptor expressed in HEK293 cells after 30 minsDisplacement of [3H]DPCPX from human adenosine A2b receptor expressed in HEK293 cells after 30 mins
ChEMBL 373 3 0 7 3.5 Cc1nn(Cc2ccccc2)c(=O)c2ncn3nc(-c4ccsc4)cc3c12 10.1016/j.bmc.2010.09.043
135465785 488 None 0 Human Binding pKi = 7.3 7.3 - 1
Binding affinity of compound for displacement of [3H]DPCPX binding in HEK293 membranes expressing human A2B adenosine receptorsBinding affinity of compound for displacement of [3H]DPCPX binding in HEK293 membranes expressing human A2B adenosine receptors
ChEMBL 496 8 2 12 0.0 CCCn1c2=N/C(=c/3\o[nH]c(c3)OCC(=O)Nc3ccc4c(c3)OCO4)/N=c2c(=O)n(c1=O)CCC 10.1021/jm0309654
439 488 None 0 Human Binding pKi = 7.3 7.3 - 1
Binding affinity of compound for displacement of [3H]DPCPX binding in HEK293 membranes expressing human A2B adenosine receptorsBinding affinity of compound for displacement of [3H]DPCPX binding in HEK293 membranes expressing human A2B adenosine receptors
ChEMBL 496 8 2 12 0.0 CCCn1c2=N/C(=c/3\o[nH]c(c3)OCC(=O)Nc3ccc4c(c3)OCO4)/N=c2c(=O)n(c1=O)CCC 10.1021/jm0309654
CHEMBL32582 488 None 0 Human Binding pKi = 7.3 7.3 - 1
Binding affinity of compound for displacement of [3H]DPCPX binding in HEK293 membranes expressing human A2B adenosine receptorsBinding affinity of compound for displacement of [3H]DPCPX binding in HEK293 membranes expressing human A2B adenosine receptors
ChEMBL 496 8 2 12 0.0 CCCn1c2=N/C(=c/3\o[nH]c(c3)OCC(=O)Nc3ccc4c(c3)OCO4)/N=c2c(=O)n(c1=O)CCC 10.1021/jm0309654
135465785 488 None 0 Human Binding pKi = 7.3 7.3 - 1
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 496 8 2 12 0.0 CCCn1c2=N/C(=c/3\o[nH]c(c3)OCC(=O)Nc3ccc4c(c3)OCO4)/N=c2c(=O)n(c1=O)CCC 10.1021/jm0309654
439 488 None 0 Human Binding pKi = 7.3 7.3 - 1
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 496 8 2 12 0.0 CCCn1c2=N/C(=c/3\o[nH]c(c3)OCC(=O)Nc3ccc4c(c3)OCO4)/N=c2c(=O)n(c1=O)CCC 10.1021/jm0309654
CHEMBL32582 488 None 0 Human Binding pKi = 7.3 7.3 - 1
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 496 8 2 12 0.0 CCCn1c2=N/C(=c/3\o[nH]c(c3)OCC(=O)Nc3ccc4c(c3)OCO4)/N=c2c(=O)n(c1=O)CCC 10.1021/jm0309654
46880508 6155 None 0 Human Binding pKi = 7.3 7.3 18 3
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 316 4 1 4 3.6 O=C(Nc1ccc(-c2ccncc2)c(-c2ccccn2)n1)C1CC1 10.1016/j.bmcl.2010.01.045
CHEMBL1081039 6155 None 0 Human Binding pKi = 7.3 7.3 18 3
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 316 4 1 4 3.6 O=C(Nc1ccc(-c2ccncc2)c(-c2ccccn2)n1)C1CC1 10.1016/j.bmcl.2010.01.045
46880332 6229 None 0 Human Binding pKi = 7.3 7.3 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 280 3 1 5 2.8 CC(=O)Nc1ccc(-c2ccncn2)c(-c2ccco2)n1 10.1016/j.bmcl.2010.01.045
CHEMBL1081459 6229 None 0 Human Binding pKi = 7.3 7.3 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 280 3 1 5 2.8 CC(=O)Nc1ccc(-c2ccncn2)c(-c2ccco2)n1 10.1016/j.bmcl.2010.01.045
CHEMBL5082920 214832 None 0 Human Binding pKi = 7.3 7.3 -7 5
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells by liquid scintillation counting analysisDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells by liquid scintillation counting analysis
ChEMBL None None None Nc1nc(-c2ccccc2)c2c(n1)-c1cc(OCCCN3CCCC3)ccc1C2=O 10.1021/acs.jmedchem.0c00914
CHEMBL5083244 214854 None 0 Human Binding pKi = 7.3 7.3 -1 2
Displacement of [3H]DPCPX from human A2BAR expressed in HEK293 cell membrane incubated for 30 mins by microbeta trilux scintillation counter analysisDisplacement of [3H]DPCPX from human A2BAR expressed in HEK293 cell membrane incubated for 30 mins by microbeta trilux scintillation counter analysis
ChEMBL None None None CNc1nc(-c2ccccc2)c(C#N)c(-c2ccccc2F)n1 10.1021/acs.jmedchem.1c01636
1676 98984 None 61 Human Binding pKi = 5.3 5.3 -3 10
Displacement of [125I]ABOPX from human adenosine receptor A2b expressed in HEK293 cell membranes after 3 hrs by fluorescence assayDisplacement of [125I]ABOPX from human adenosine receptor A2b expressed in HEK293 cell membranes after 3 hrs by fluorescence assay
ChEMBL 194 2 2 4 -0.2 CCCn1c(=O)[nH]c(=O)c2[nH]cnc21 10.1016/j.ejmech.2016.11.007
CHEMBL279898 98984 None 61 Human Binding pKi = 5.3 5.3 -3 10
Displacement of [125I]ABOPX from human adenosine receptor A2b expressed in HEK293 cell membranes after 3 hrs by fluorescence assayDisplacement of [125I]ABOPX from human adenosine receptor A2b expressed in HEK293 cell membranes after 3 hrs by fluorescence assay
ChEMBL 194 2 2 4 -0.2 CCCn1c(=O)[nH]c(=O)c2[nH]cnc21 10.1016/j.ejmech.2016.11.007
1676 98984 None 61 Human Binding pKi = 5.3 5.3 -3 10
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 194 2 2 4 -0.2 CCCn1c(=O)[nH]c(=O)c2[nH]cnc21 10.1021/jm0104318
CHEMBL279898 98984 None 61 Human Binding pKi = 5.3 5.3 -3 10
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 194 2 2 4 -0.2 CCCn1c(=O)[nH]c(=O)c2[nH]cnc21 10.1021/jm0104318
1676 98984 None 61 Human Binding pKi = 5.3 5.3 -3 10
Displacement of [3H]DPX from human recombinant Adenosine A2B receptor expressed in HEK293 cells after 3 hrsDisplacement of [3H]DPX from human recombinant Adenosine A2B receptor expressed in HEK293 cells after 3 hrs
ChEMBL 194 2 2 4 -0.2 CCCn1c(=O)[nH]c(=O)c2[nH]cnc21 10.1021/acs.jmedchem.5b01586
CHEMBL279898 98984 None 61 Human Binding pKi = 5.3 5.3 -3 10
Displacement of [3H]DPX from human recombinant Adenosine A2B receptor expressed in HEK293 cells after 3 hrsDisplacement of [3H]DPX from human recombinant Adenosine A2B receptor expressed in HEK293 cells after 3 hrs
ChEMBL 194 2 2 4 -0.2 CCCn1c(=O)[nH]c(=O)c2[nH]cnc21 10.1021/acs.jmedchem.5b01586
1676 98984 None 61 Human Binding pKi = 5.3 5.3 -3 10
Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cellsDisplacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells
ChEMBL 194 2 2 4 -0.2 CCCn1c(=O)[nH]c(=O)c2[nH]cnc21 10.1021/jm051268+
CHEMBL279898 98984 None 61 Human Binding pKi = 5.3 5.3 -3 10
Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cellsDisplacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells
ChEMBL 194 2 2 4 -0.2 CCCn1c(=O)[nH]c(=O)c2[nH]cnc21 10.1021/jm051268+
65269 188227 None 36 Human Binding pKi = 4.3 4.3 -21 4
Displacement of [3H]- ZM-241385 from human adenosine A2B receptor expressed in HEK cellsDisplacement of [3H]- ZM-241385 from human adenosine A2B receptor expressed in HEK cells
ChEMBL 265 2 4 8 -1.3 Nc1ncnc2c1ncn2[C@@H]1C[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm9905965
CHEMBL49935 188227 None 36 Human Binding pKi = 4.3 4.3 -21 4
Displacement of [3H]- ZM-241385 from human adenosine A2B receptor expressed in HEK cellsDisplacement of [3H]- ZM-241385 from human adenosine A2B receptor expressed in HEK cells
ChEMBL 265 2 4 8 -1.3 Nc1ncnc2c1ncn2[C@@H]1C[C@H](CO)[C@@H](O)[C@H]1O 10.1021/jm9905965
CHEMBL5091545 215313 None 0 Human Binding pKi = 6.3 6.3 -16 2
Displacement of [3H]DPCPX from human A2BAR expressed in HEK293 cell membrane incubated for 30 mins by microbeta trilux scintillation counter analysisDisplacement of [3H]DPCPX from human A2BAR expressed in HEK293 cell membrane incubated for 30 mins by microbeta trilux scintillation counter analysis
ChEMBL None None None CNc1nc(-c2ccccc2)c(C#N)c(-c2ccc(C)cc2)n1 10.1021/acs.jmedchem.1c01636
44451105 160633 None 0 Human Binding pKi = 6.3 6.3 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 537 6 1 8 2.6 COc1cc(OCC(=O)N2CCN(c3ccc(Cl)cc3)CC2)ccc1-c1cc2c([nH]1)c(=O)n(C)c(=O)n2C 10.1016/j.bmc.2008.01.002
CHEMBL411314 160633 None 0 Human Binding pKi = 6.3 6.3 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 537 6 1 8 2.6 COc1cc(OCC(=O)N2CCN(c3ccc(Cl)cc3)CC2)ccc1-c1cc2c([nH]1)c(=O)n(C)c(=O)n2C 10.1016/j.bmc.2008.01.002
46233214 200277 None 0 Human Binding pKi = 6.3 6.3 -3 3
Displacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells by microplate beta scintillation counterDisplacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells by microplate beta scintillation counter
ChEMBL 344 6 1 6 2.3 CCSCCn1c(=O)n(CC)c(=O)c2[nH]c(-c3ccccc3)nc21 10.1016/j.bmc.2010.01.028
CHEMBL597169 200277 None 0 Human Binding pKi = 6.3 6.3 -3 3
Displacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells by microplate beta scintillation counterDisplacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells by microplate beta scintillation counter
ChEMBL 344 6 1 6 2.3 CCSCCn1c(=O)n(CC)c(=O)c2[nH]c(-c3ccccc3)nc21 10.1016/j.bmc.2010.01.028
44588473 175244 None 0 Human Binding pKi = 6.3 6.3 1 2
Displacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cells
ChEMBL 357 6 1 7 2.7 CCCn1c(=O)c2c(cc(-c3ccc(OC)cc3)n2O)n(CCC)c1=O 10.1016/j.bmc.2008.09.067
CHEMBL457209 175244 None 0 Human Binding pKi = 6.3 6.3 1 2
Displacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cells
ChEMBL 357 6 1 7 2.7 CCCn1c(=O)c2c(cc(-c3ccc(OC)cc3)n2O)n(CCC)c1=O 10.1016/j.bmc.2008.09.067
404 4098 None 33 Human Binding pKi = 7.3 7.3 -154 11
Binding affinity towards human Adenosine A2B receptorBinding affinity towards human Adenosine A2B receptor
ChEMBL 428 10 3 8 0.8 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)NCCN 10.1021/jm011049y
432 4098 None 33 Human Binding pKi = 7.3 7.3 -154 11
Binding affinity towards human Adenosine A2B receptorBinding affinity towards human Adenosine A2B receptor
ChEMBL 428 10 3 8 0.8 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)NCCN 10.1021/jm011049y
5697 4098 None 33 Human Binding pKi = 7.3 7.3 -154 11
Binding affinity towards human Adenosine A2B receptorBinding affinity towards human Adenosine A2B receptor
ChEMBL 428 10 3 8 0.8 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)NCCN 10.1021/jm011049y
CHEMBL273094 4098 None 33 Human Binding pKi = 7.3 7.3 -154 11
Binding affinity towards human Adenosine A2B receptorBinding affinity towards human Adenosine A2B receptor
ChEMBL 428 10 3 8 0.8 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)NCCN 10.1021/jm011049y
57429621 159174 None 0 Human Binding pKi = 7.3 7.3 - 1
Displacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 minsDisplacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 mins
ChEMBL 418 5 3 7 1.4 CCCn1c(=O)[nH]c2nc(-c3cnn(CC#Cc4cccc(C(=O)O)c4)c3)[nH]c2c1=O 10.1016/j.ejmech.2017.04.014
CHEMBL4098369 159174 None 0 Human Binding pKi = 7.3 7.3 - 1
Displacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 minsDisplacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 mins
ChEMBL 418 5 3 7 1.4 CCCn1c(=O)[nH]c2nc(-c3cnn(CC#Cc4cccc(C(=O)O)c4)c3)[nH]c2c1=O 10.1016/j.ejmech.2017.04.014
22266756 94595 None 0 Human Binding pKi = 7.3 7.3 - 1
Displacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranesDisplacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranes
ChEMBL 464 6 2 9 2.4 O=c1[nH]c2nc(-c3cnn(Cc4noc(-c5ccc(Cl)cc5)n4)c3)[nH]c2c(=O)n1CC1CC1 10.1016/j.bmcl.2008.01.008
CHEMBL252074 94595 None 0 Human Binding pKi = 7.3 7.3 - 1
Displacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranesDisplacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranes
ChEMBL 464 6 2 9 2.4 O=c1[nH]c2nc(-c3cnn(Cc4noc(-c5ccc(Cl)cc5)n4)c3)[nH]c2c(=O)n1CC1CC1 10.1016/j.bmcl.2008.01.008
11112849 57304 None 0 Human Binding pKi = 7.3 7.3 -177 4
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 37-63Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 37-63
ChEMBL 432 4 2 10 3.1 CCn1cc2c(nc(NC(=O)Nc3ccc4c(c3)OCO4)n3nc(-c4ccco4)nc23)n1 10.1021/jm0109614
CHEMBL165083 57304 None 0 Human Binding pKi = 7.3 7.3 -177 4
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 37-63Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 37-63
ChEMBL 432 4 2 10 3.1 CCn1cc2c(nc(NC(=O)Nc3ccc4c(c3)OCO4)n3nc(-c4ccco4)nc23)n1 10.1021/jm0109614
135874421 168958 None 0 Human Binding pKi = 7.3 7.3 - 1
Displacement of [3H]MRE2029F20 from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]MRE2029F20 from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 477 8 2 8 3.1 CCCn1c(=O)c2[nH]c(-c3cc(C)n(CC(=O)Nc4ccc(C)c(C)c4)n3)nc2n(CCC)c1=O 10.1016/j.bmc.2007.11.058
CHEMBL438938 168958 None 0 Human Binding pKi = 7.3 7.3 - 1
Displacement of [3H]MRE2029F20 from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]MRE2029F20 from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 477 8 2 8 3.1 CCCn1c(=O)c2[nH]c(-c3cc(C)n(CC(=O)Nc4ccc(C)c(C)c4)n3)nc2n(CCC)c1=O 10.1016/j.bmc.2007.11.058
11466670 72919 None 0 Human Binding pKi = 7.3 7.3 25 4
Displacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cellsDisplacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cells
ChEMBL 527 8 1 9 4.3 CCCn1c(=O)c2nc(-c3cnn(Cc4cc(-c5ccc(C(F)(F)F)cc5)on4)c3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2005.10.002
CHEMBL200451 72919 None 0 Human Binding pKi = 7.3 7.3 25 4
Displacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cellsDisplacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cells
ChEMBL 527 8 1 9 4.3 CCCn1c(=O)c2nc(-c3cnn(Cc4cc(-c5ccc(C(F)(F)F)cc5)on4)c3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2005.10.002
52946584 201826 None 0 Human Binding pKi = 7.3 7.3 -3 4
Inhibition of [3H]PSB-298 binding to adenosine A2b receptorInhibition of [3H]PSB-298 binding to adenosine A2b receptor
ChEMBL 496 7 3 6 3.5 CCCC1C(=O)Nc2nc(-c3ccc(OCC(=O)NC4CC(C)(C)N([O])C(C)(C)C4)cc3)[nH]c2C1=O 10.1021/jm049513x
CHEMBL607025 201826 None 0 Human Binding pKi = 7.3 7.3 -3 4
Inhibition of [3H]PSB-298 binding to adenosine A2b receptorInhibition of [3H]PSB-298 binding to adenosine A2b receptor
ChEMBL 496 7 3 6 3.5 CCCC1C(=O)Nc2nc(-c3ccc(OCC(=O)NC4CC(C)(C)N([O])C(C)(C)C4)cc3)[nH]c2C1=O 10.1021/jm049513x
155524516 170967 None 0 Human Binding pKi = 7.3 7.3 2 3
Displacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 432 5 2 7 0.4 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(C)CC4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
CHEMBL4455937 170967 None 0 Human Binding pKi = 7.3 7.3 2 3
Displacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 432 5 2 7 0.4 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(C)CC4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
45268873 196750 None 0 Human Binding pKi = 7.3 7.3 2 3
Binding affinity to human adenosine A2b receptor expressed in HEK293 cellsBinding affinity to human adenosine A2b receptor expressed in HEK293 cells
ChEMBL 532 10 2 9 2.1 CCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)NN4CCc5ccccc5C4)cc3)nc2n(CCCOC)c1=O 10.1016/j.bmc.2009.03.029
CHEMBL565192 196750 None 0 Human Binding pKi = 7.3 7.3 2 3
Binding affinity to human adenosine A2b receptor expressed in HEK293 cellsBinding affinity to human adenosine A2b receptor expressed in HEK293 cells
ChEMBL 532 10 2 9 2.1 CCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)NN4CCc5ccccc5C4)cc3)nc2n(CCCOC)c1=O 10.1016/j.bmc.2009.03.029
136042335 71162 None 0 Human Binding pKi = 7.3 7.3 - 1
Displacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation countingDisplacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation counting
ChEMBL 490 8 2 10 1.9 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc(=O)c5ccccc5[nH]4)nn3C)nc2n(CCC)c1=O 10.1021/jm201292w
CHEMBL1955911 71162 None 0 Human Binding pKi = 7.3 7.3 - 1
Displacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation countingDisplacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation counting
ChEMBL 490 8 2 10 1.9 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc(=O)c5ccccc5[nH]4)nn3C)nc2n(CCC)c1=O 10.1021/jm201292w
168273637 190316 None 0 Human Binding pKi = 7.3 7.3 - 1
Displacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cell membrane and measured after 0.5 hrs by radioligand displacement assayDisplacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cell membrane and measured after 0.5 hrs by radioligand displacement assay
ChEMBL 410 7 1 8 2.0 CCCn1c(=O)c2[nH]c(-c3ccc(OS(=O)(=O)F)cc3)nc2n(CCC)c1=O 10.1039/d2md00132b
CHEMBL5176227 190316 None 0 Human Binding pKi = 7.3 7.3 - 1
Displacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cell membrane and measured after 0.5 hrs by radioligand displacement assayDisplacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cell membrane and measured after 0.5 hrs by radioligand displacement assay
ChEMBL 410 7 1 8 2.0 CCCn1c(=O)c2[nH]c(-c3ccc(OS(=O)(=O)F)cc3)nc2n(CCC)c1=O 10.1039/d2md00132b
168272084 190282 None 0 Human Binding pKi = 7.3 7.3 - 1
Displacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cell membrane preincubated for 4 hrs followed by [3H]PSB-603 addition and measured after 0.5 hrs by radioligand displacement assayDisplacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cell membrane preincubated for 4 hrs followed by [3H]PSB-603 addition and measured after 0.5 hrs by radioligand displacement assay
ChEMBL 369 6 1 7 3.1 CCCn1c(=O)c2[nH]c(-c3cccc(N=C=S)c3)nc2n(CCC)c1=O 10.1039/d2md00132b
CHEMBL5175698 190282 None 0 Human Binding pKi = 7.3 7.3 - 1
Displacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cell membrane preincubated for 4 hrs followed by [3H]PSB-603 addition and measured after 0.5 hrs by radioligand displacement assayDisplacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cell membrane preincubated for 4 hrs followed by [3H]PSB-603 addition and measured after 0.5 hrs by radioligand displacement assay
ChEMBL 369 6 1 7 3.1 CCCn1c(=O)c2[nH]c(-c3cccc(N=C=S)c3)nc2n(CCC)c1=O 10.1039/d2md00132b
11662264 77283 None 0 Human Binding pKi = 5.3 5.3 - 1
Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cellsDisplacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells
ChEMBL 444 7 1 7 3.4 CCCn1c(=O)c2nc(-c3cnn(Cc4cc(F)ccc4Cl)c3)[nH]c2n(CCC)c1=O 10.1021/jm051268+
CHEMBL208143 77283 None 0 Human Binding pKi = 5.3 5.3 - 1
Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cellsDisplacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells
ChEMBL 444 7 1 7 3.4 CCCn1c(=O)c2nc(-c3cnn(Cc4cc(F)ccc4Cl)c3)[nH]c2n(CCC)c1=O 10.1021/jm051268+
2980395 139007 None 13 Human Binding pKi = 6.3 6.3 - 1
Displacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting methodDisplacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting method
ChEMBL 339 3 1 6 4.0 CCOC(=O)C1=C(C)Nc2nc3ccccc3n2C1c1cccs1 10.1021/acs.jmedchem.0c00564
CHEMBL3785635 139007 None 13 Human Binding pKi = 6.3 6.3 - 1
Displacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting methodDisplacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting method
ChEMBL 339 3 1 6 4.0 CCOC(=O)C1=C(C)Nc2nc3ccccc3n2C1c1cccs1 10.1021/acs.jmedchem.0c00564
2980395 139007 None 13 Human Binding pKi = 6.3 6.3 - 1
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 minsDisplacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 mins
ChEMBL 339 3 1 6 4.0 CCOC(=O)C1=C(C)Nc2nc3ccccc3n2C1c1cccs1 10.1021/acs.jmedchem.5b01586
CHEMBL3785635 139007 None 13 Human Binding pKi = 6.3 6.3 - 1
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 minsDisplacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 mins
ChEMBL 339 3 1 6 4.0 CCOC(=O)C1=C(C)Nc2nc3ccccc3n2C1c1cccs1 10.1021/acs.jmedchem.5b01586
2980395 139007 None 13 Human Binding pKi = 6.3 6.3 - 1
Displacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assayDisplacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assay
ChEMBL 339 3 1 6 4.0 CCOC(=O)C1=C(C)Nc2nc3ccccc3n2C1c1cccs1 10.1021/acs.jmedchem.9b01340
CHEMBL3785635 139007 None 13 Human Binding pKi = 6.3 6.3 - 1
Displacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assayDisplacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assay
ChEMBL 339 3 1 6 4.0 CCOC(=O)C1=C(C)Nc2nc3ccccc3n2C1c1cccs1 10.1021/acs.jmedchem.9b01340
44390528 122614 None 0 Human Binding pKi = 6.3 6.3 2 2
Binding affinity for adenosine A2b receptor by using as [3H]ZM-241385 (14 nM) radioligand in membranes from HEK-A2B cellsBinding affinity for adenosine A2b receptor by using as [3H]ZM-241385 (14 nM) radioligand in membranes from HEK-A2B cells
ChEMBL 554 9 1 9 5.0 CCCn1c(=O)c2nc(-c3ccc(OCc4nc(-c5ccc(C(F)(F)F)cc5)no4)cc3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2004.11.044
CHEMBL360280 122614 None 0 Human Binding pKi = 6.3 6.3 2 2
Binding affinity for adenosine A2b receptor by using as [3H]ZM-241385 (14 nM) radioligand in membranes from HEK-A2B cellsBinding affinity for adenosine A2b receptor by using as [3H]ZM-241385 (14 nM) radioligand in membranes from HEK-A2B cells
ChEMBL 554 9 1 9 5.0 CCCn1c(=O)c2nc(-c3ccc(OCc4nc(-c5ccc(C(F)(F)F)cc5)no4)cc3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2004.11.044
52941244 19251 None 0 Human Binding pKi = 6.3 6.3 -1 2
Displacement of [3H]ZM241385 from human adenosine A2B receptor transfected in CHO cells after 60 mins by scintillation countingDisplacement of [3H]ZM241385 from human adenosine A2B receptor transfected in CHO cells after 60 mins by scintillation counting
ChEMBL 509 9 2 5 5.7 C[C@@H](NC(=O)COc1ccc2[nH]c(=O)c(-c3nccs3)c(CCc3ccccc3)c2c1)c1ccccc1 10.1016/j.bmcl.2010.10.030
CHEMBL1290209 19251 None 0 Human Binding pKi = 6.3 6.3 -1 2
Displacement of [3H]ZM241385 from human adenosine A2B receptor transfected in CHO cells after 60 mins by scintillation countingDisplacement of [3H]ZM241385 from human adenosine A2B receptor transfected in CHO cells after 60 mins by scintillation counting
ChEMBL 509 9 2 5 5.7 C[C@@H](NC(=O)COc1ccc2[nH]c(=O)c(-c3nccs3)c(CCc3ccccc3)c2c1)c1ccccc1 10.1016/j.bmcl.2010.10.030
45273099 195626 None 0 Human Binding pKi = 6.3 6.3 10 2
Binding affinity to human adenosine A2b receptor expressed in HEK293 cellsBinding affinity to human adenosine A2b receptor expressed in HEK293 cells
ChEMBL 378 9 1 8 1.9 CCSCCn1c(=O)c2[nH]c(-c3ccco3)nc2n(CCCOC)c1=O 10.1016/j.bmc.2009.03.029
CHEMBL556264 195626 None 0 Human Binding pKi = 6.3 6.3 10 2
Binding affinity to human adenosine A2b receptor expressed in HEK293 cellsBinding affinity to human adenosine A2b receptor expressed in HEK293 cells
ChEMBL 378 9 1 8 1.9 CCSCCn1c(=O)c2[nH]c(-c3ccco3)nc2n(CCCOC)c1=O 10.1016/j.bmc.2009.03.029
10219934 96288 None 8 Human Binding pKi = 5.3 5.3 1 3
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 208 1 1 5 0.0 CC(C)n1c(=O)n(C)c(=O)c2[nH]cnc21 10.1021/jm0104318
CHEMBL26119 96288 None 8 Human Binding pKi = 5.3 5.3 1 3
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 208 1 1 5 0.0 CC(C)n1c(=O)n(C)c(=O)c2[nH]cnc21 10.1021/jm0104318
10737168 165335 None 0 Human Binding pKi = 7.3 7.3 -288 6
Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 38-63Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 38-63
ChEMBL 359 5 1 8 2.9 Nc1nc2nn(CCCc3ccccc3)cc2c2nc(-c3ccco3)nn12 10.1021/jm001047y
CHEMBL423542 165335 None 0 Human Binding pKi = 7.3 7.3 -288 6
Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 38-63Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 38-63
ChEMBL 359 5 1 8 2.9 Nc1nc2nn(CCCc3ccccc3)cc2c2nc(-c3ccco3)nn12 10.1021/jm001047y
50940980 57285 None 2 Human Binding pKi = 7.3 7.3 -3 4
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 283 4 1 5 3.3 CCC(=O)Nc1cc(-c2ccoc2)nc(-c2ccoc2)n1 10.1021/jm100843z
CHEMBL1650391 57285 None 2 Human Binding pKi = 7.3 7.3 -3 4
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 283 4 1 5 3.3 CCC(=O)Nc1cc(-c2ccoc2)nc(-c2ccoc2)n1 10.1021/jm100843z
136042335 71162 None 0 Human Binding pKi = 7.3 7.3 - 1
Displacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation countingDisplacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation counting
ChEMBL 490 8 2 10 1.9 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc(=O)c5ccccc5[nH]4)nn3C)nc2n(CCC)c1=O 10.1021/jm201292w
CHEMBL1955911 71162 None 0 Human Binding pKi = 7.3 7.3 - 1
Displacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation countingDisplacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation counting
ChEMBL 490 8 2 10 1.9 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc(=O)c5ccccc5[nH]4)nn3C)nc2n(CCC)c1=O 10.1021/jm201292w
21958762 155780 None 0 Human Binding pKi = 7.3 7.3 3 3
Displacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 288 4 2 6 0.7 CCCn1c(=O)c2[nH]c(-c3cn[nH]c3)nc2n(CC)c1=O 10.1021/jm7014815
CHEMBL405901 155780 None 0 Human Binding pKi = 7.3 7.3 3 3
Displacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 288 4 2 6 0.7 CCCn1c(=O)c2[nH]c(-c3cn[nH]c3)nc2n(CC)c1=O 10.1021/jm7014815
155511760 169610 None 0 Human Binding pKi = 7.3 7.3 - 1
Displacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assayDisplacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assay
ChEMBL 391 3 1 6 4.4 CC(C)OC(=O)C1=C(C(F)(F)F)Nc2nc3ccccc3n2C1c1ccoc1 10.1021/acs.jmedchem.9b01340
CHEMBL4436567 169610 None 0 Human Binding pKi = 7.3 7.3 - 1
Displacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assayDisplacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assay
ChEMBL 391 3 1 6 4.4 CC(C)OC(=O)C1=C(C(F)(F)F)Nc2nc3ccccc3n2C1c1ccoc1 10.1021/acs.jmedchem.9b01340
122227309 177664 None 0 Human Binding pKi = 7.3 7.3 - 1
Displacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting methodDisplacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting method
ChEMBL 322 3 2 5 3.2 CCOC(=O)C1=C(C)Nc2nc3ccccc3n2C1c1ccc[nH]1 10.1021/acs.jmedchem.0c00564
CHEMBL4641601 177664 None 0 Human Binding pKi = 7.3 7.3 - 1
Displacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting methodDisplacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting method
ChEMBL 322 3 2 5 3.2 CCOC(=O)C1=C(C)Nc2nc3ccccc3n2C1c1ccc[nH]1 10.1021/acs.jmedchem.0c00564
44588472 172612 None 0 Human Binding pKi = 6.3 6.3 -2 2
Displacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cells
ChEMBL 341 6 1 5 3.0 CCCn1c(=O)c2[nH]c(-c3ccc(OC)cc3)cc2n(CCC)c1=O 10.1016/j.bmc.2008.09.067
CHEMBL449133 172612 None 0 Human Binding pKi = 6.3 6.3 -2 2
Displacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cells
ChEMBL 341 6 1 5 3.0 CCCn1c(=O)c2[nH]c(-c3ccc(OC)cc3)cc2n(CCC)c1=O 10.1016/j.bmc.2008.09.067
CHEMBL5075422 214372 None 3 Human Binding pKi = 6.3 6.3 -87 4
Displacement of [3H] DPCPX from human recombinant A2B adenosine receptor expressed in HEK293 cells incubated for 30 mins by radioligand binding competition assayDisplacement of [3H] DPCPX from human recombinant A2B adenosine receptor expressed in HEK293 cells incubated for 30 mins by radioligand binding competition assay
ChEMBL None None None Cn1cc(-c2cnc(N)n3nc(-c4ccco4)nc23)ccc1=O 10.1021/acsmedchemlett.1c00599
71570366 86151 None 0 Human Binding pKi = 6.3 6.3 -11 3
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK-293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK-293 cells
ChEMBL 409 7 1 7 3.8 COc1cccc(-c2cc(NC(C)=O)nc(-c3cccc(OC)c3OC)n2)c1OC 10.1016/j.ejmech.2012.11.010
CHEMBL2311745 86151 None 0 Human Binding pKi = 6.3 6.3 -11 3
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK-293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK-293 cells
ChEMBL 409 7 1 7 3.8 COc1cccc(-c2cc(NC(C)=O)nc(-c3cccc(OC)c3OC)n2)c1OC 10.1016/j.ejmech.2012.11.010
44236567 157302 None 0 Human Binding pKi = 8.3 8.3 - 1
Displacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 minsDisplacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 mins
ChEMBL 430 6 1 7 2.9 CCCn1c(=O)c2[nH]c(-c3cnn(CC#Cc4cccc(C)c4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2017.04.014
CHEMBL4077090 157302 None 0 Human Binding pKi = 8.3 8.3 - 1
Displacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 minsDisplacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 mins
ChEMBL 430 6 1 7 2.9 CCCn1c(=O)c2[nH]c(-c3cnn(CC#Cc4cccc(C)c4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2017.04.014
44236420 156235 None 0 Human Binding pKi = 8.3 8.3 - 1
Displacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting methodDisplacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting method
ChEMBL 518 8 1 9 2.2 CCCn1c(=O)c2[nH]c(-c3cnn(CC(=O)N4CCN(c5ccc(C)cc5)CC4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2016.11.007
CHEMBL4064755 156235 None 0 Human Binding pKi = 8.3 8.3 - 1
Displacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting methodDisplacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting method
ChEMBL 518 8 1 9 2.2 CCCn1c(=O)c2[nH]c(-c3cnn(CC(=O)N4CCN(c5ccc(C)cc5)CC4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2016.11.007
21958775 94773 None 0 Human Binding pKi = 8.3 8.3 19 3
Displacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranesDisplacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranes
ChEMBL 380 5 2 6 1.9 O=c1[nH]c2nc(-c3cnn(Cc4cccc(F)c4)c3)[nH]c2c(=O)n1CC1CC1 10.1016/j.bmcl.2008.01.008
CHEMBL253252 94773 None 0 Human Binding pKi = 8.3 8.3 19 3
Displacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranesDisplacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranes
ChEMBL 380 5 2 6 1.9 O=c1[nH]c2nc(-c3cnn(Cc4cccc(F)c4)c3)[nH]c2c(=O)n1CC1CC1 10.1016/j.bmcl.2008.01.008
10246959 58764 None 0 Human Binding pKi = 8.3 8.3 -15 6
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 345 4 1 8 2.6 Nc1nc2nn(CCc3ccccc3)cc2c2nc(-c3ccco3)nn12 10.1021/jm030852k
CHEMBL16867 58764 None 0 Human Binding pKi = 8.3 8.3 -15 6
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 345 4 1 8 2.6 Nc1nc2nn(CCc3ccccc3)cc2c2nc(-c3ccco3)nn12 10.1021/jm030852k
46880375 5939 None 0 Human Binding pKi = 8.3 8.3 29 4
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 339 4 1 4 4.4 O=C(Nc1ccc(-c2ccncc2Cl)c(-c2ccco2)n1)C1CC1 10.1016/j.bmcl.2010.01.045
CHEMBL1079803 5939 None 0 Human Binding pKi = 8.3 8.3 29 4
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 339 4 1 4 4.4 O=C(Nc1ccc(-c2ccncc2Cl)c(-c2ccco2)n1)C1CC1 10.1016/j.bmcl.2010.01.045
46880419 6340 None 0 Human Binding pKi = 8.3 8.3 2 4
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 319 4 1 4 4.1 Cc1ccc(-c2nc(NC(=O)C3CC3)ccc2-c2ccncc2)o1 10.1016/j.bmcl.2010.01.045
CHEMBL1082005 6340 None 0 Human Binding pKi = 8.3 8.3 2 4
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 319 4 1 4 4.1 Cc1ccc(-c2nc(NC(=O)C3CC3)ccc2-c2ccncc2)o1 10.1016/j.bmcl.2010.01.045
136042350 71150 None 0 Human Binding pKi = 8.3 8.3 30 2
Displacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation countingDisplacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation counting
ChEMBL 496 8 2 9 3.2 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5cc(Cl)ccc5[nH]4)nn3C)nc2n(CCC)c1=O 10.1021/jm201292w
CHEMBL1955899 71150 None 0 Human Binding pKi = 8.3 8.3 30 2
Displacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation countingDisplacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation counting
ChEMBL 496 8 2 9 3.2 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5cc(Cl)ccc5[nH]4)nn3C)nc2n(CCC)c1=O 10.1021/jm201292w
11610638 166194 None 0 Human Binding pKi = 8.3 8.3 57 3
Displacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 382 5 1 7 2.0 CCn1c(=O)c2nc(-c3cnn(Cc4cccc(F)c4)c3)[nH]c2n(CC)c1=O 10.1021/jm7014815
CHEMBL426504 166194 None 0 Human Binding pKi = 8.3 8.3 57 3
Displacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 382 5 1 7 2.0 CCn1c(=O)c2nc(-c3cnn(Cc4cccc(F)c4)c3)[nH]c2n(CC)c1=O 10.1021/jm7014815
53248700 60734 None 0 Human Binding pKi = 8.3 8.3 3 3
Displacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cells after 1 hrDisplacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cells after 1 hr
ChEMBL 536 5 2 6 5.2 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)N3CCC(O)(c4cccc(C(F)(F)F)c4)CC3)sc12 10.1016/j.bmcl.2011.02.053
CHEMBL1760899 60734 None 0 Human Binding pKi = 8.3 8.3 3 3
Displacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cells after 1 hrDisplacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cells after 1 hr
ChEMBL 536 5 2 6 5.2 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)N3CCC(O)(c4cccc(C(F)(F)F)c4)CC3)sc12 10.1016/j.bmcl.2011.02.053
11610638 166194 None 0 Human Binding pKi = 8.3 8.3 57 3
Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cellsDisplacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells
ChEMBL 382 5 1 7 2.0 CCn1c(=O)c2nc(-c3cnn(Cc4cccc(F)c4)c3)[nH]c2n(CC)c1=O 10.1021/jm051268+
CHEMBL426504 166194 None 0 Human Binding pKi = 8.3 8.3 57 3
Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cellsDisplacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells
ChEMBL 382 5 1 7 2.0 CCn1c(=O)c2nc(-c3cnn(Cc4cccc(F)c4)c3)[nH]c2n(CC)c1=O 10.1021/jm051268+
10246959 58764 None 0 Human Binding pKi = 8.3 8.3 -15 6
Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 3.9-6.7Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 3.9-6.7
ChEMBL 345 4 1 8 2.6 Nc1nc2nn(CCc3ccccc3)cc2c2nc(-c3ccco3)nn12 10.1021/jm001047y
CHEMBL16867 58764 None 0 Human Binding pKi = 8.3 8.3 -15 6
Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 3.9-6.7Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 3.9-6.7
ChEMBL 345 4 1 8 2.6 Nc1nc2nn(CCc3ccccc3)cc2c2nc(-c3ccco3)nn12 10.1021/jm001047y
11576491 74448 None 0 Human Binding pKi = 8.3 8.3 20 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 474 9 2 6 4.4 CCCn1c(=O)c2[nH]c(-c3ccc(OC(C)C(=O)Nc4ccccc4)cc3)cc2n(CCC)c1=O 10.1021/jm0506221
CHEMBL202766 74448 None 0 Human Binding pKi = 8.3 8.3 20 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 474 9 2 6 4.4 CCCn1c(=O)c2[nH]c(-c3ccc(OC(C)C(=O)Nc4ccccc4)cc3)cc2n(CCC)c1=O 10.1021/jm0506221
11497055 74449 None 0 Human Binding pKi = 8.3 8.3 7 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 504 10 2 7 4.4 CCCn1c(=O)c2[nH]c(-c3ccc(OC(C)C(=O)Nc4ccc(OC)cc4)cc3)cc2n(CCC)c1=O 10.1021/jm0506221
CHEMBL202767 74449 None 0 Human Binding pKi = 8.3 8.3 7 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 504 10 2 7 4.4 CCCn1c(=O)c2[nH]c(-c3ccc(OC(C)C(=O)Nc4ccc(OC)cc4)cc3)cc2n(CCC)c1=O 10.1021/jm0506221
11649145 135204 None 0 Human Binding pKi = 8.3 8.3 1 5
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 508 8 2 6 4.8 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(-c5ccccc5)cc4)cc3)cc2n(C)c1=O 10.1021/jm0506221
CHEMBL372148 135204 None 0 Human Binding pKi = 8.3 8.3 1 5
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 508 8 2 6 4.8 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(-c5ccccc5)cc4)cc3)cc2n(C)c1=O 10.1021/jm0506221
44451283 96463 None 0 Human Binding pKi = 8.3 8.3 20 4
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 473 5 1 7 2.0 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCN(c5ccccc5)CC4)cc3)cc2n(C)c1=O 10.1016/j.bmc.2008.01.002
CHEMBL262332 96463 None 0 Human Binding pKi = 8.3 8.3 20 4
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 473 5 1 7 2.0 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCN(c5ccccc5)CC4)cc3)cc2n(C)c1=O 10.1016/j.bmc.2008.01.002
44236539 156792 None 0 Human Binding pKi = 8.3 8.3 - 1
Displacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 minsDisplacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 mins
ChEMBL 460 7 2 8 2.3 CCCn1c(=O)c2[nH]c(-c3cnn(CC#Cc4cccc(C(=O)O)c4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2017.04.014
CHEMBL4070936 156792 None 0 Human Binding pKi = 8.3 8.3 - 1
Displacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 minsDisplacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 mins
ChEMBL 460 7 2 8 2.3 CCCn1c(=O)c2[nH]c(-c3cnn(CC#Cc4cccc(C(=O)O)c4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2017.04.014
71452718 78923 None 0 Human Binding pKi = 8.3 8.3 7 4
Inhibition of [3H]ZM-241380 binding to adenosine A2b receptorInhibition of [3H]ZM-241380 binding to adenosine A2b receptor
ChEMBL 491 10 4 7 2.5 CCCCn1c(=O)[nH]c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(CC(=O)O)cc4)cc3)nc2c1=O 10.1021/jm049513x
CHEMBL2112962 78923 None 0 Human Binding pKi = 8.3 8.3 7 4
Inhibition of [3H]ZM-241380 binding to adenosine A2b receptorInhibition of [3H]ZM-241380 binding to adenosine A2b receptor
ChEMBL 491 10 4 7 2.5 CCCCn1c(=O)[nH]c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(CC(=O)O)cc4)cc3)nc2c1=O 10.1021/jm049513x
10863910 140839 None 0 Human Binding pKi = 8.3 8.3 7 4
Inhibition of [3H]ZM-241385 binding to human adenosine A2B receptorInhibition of [3H]ZM-241385 binding to human adenosine A2B receptor
ChEMBL 491 9 3 8 2.7 CCCCn1c(=O)[nH]c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(C(=O)OC)cc4)cc3)nc2c1=O 10.1021/jm011049y
CHEMBL38193 140839 None 0 Human Binding pKi = 8.3 8.3 7 4
Inhibition of [3H]ZM-241385 binding to human adenosine A2B receptorInhibition of [3H]ZM-241385 binding to human adenosine A2B receptor
ChEMBL 491 9 3 8 2.7 CCCCn1c(=O)[nH]c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(C(=O)OC)cc4)cc3)nc2c1=O 10.1021/jm011049y
10050439 206336 None 0 Human Binding pKi = 8.3 8.3 -1 3
Binding affinity for human adenosine A2B receptor using [3H]-PSB-298 in CHO cell membranesBinding affinity for human adenosine A2B receptor using [3H]-PSB-298 in CHO cell membranes
ChEMBL 471 7 2 9 2.2 CCCn1c(=O)[nH]c2[nH]c(-c3ccc(S(=O)(=O)Oc4ccc([N+](=O)[O-])cc4)cc3)nc2c1=O 10.1021/jm0310030
CHEMBL8732 206336 None 0 Human Binding pKi = 8.3 8.3 -1 3
Binding affinity for human adenosine A2B receptor using [3H]-PSB-298 in CHO cell membranesBinding affinity for human adenosine A2B receptor using [3H]-PSB-298 in CHO cell membranes
ChEMBL 471 7 2 9 2.2 CCCn1c(=O)[nH]c2[nH]c(-c3ccc(S(=O)(=O)Oc4ccc([N+](=O)[O-])cc4)cc3)nc2c1=O 10.1021/jm0310030
57988776 156659 None 0 Human Binding pKi = 8.3 8.3 - 1
Displacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting methodDisplacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting method
ChEMBL 519 9 1 7 3.9 CCCn1c(=O)c2[nH]c(-c3ccc(OCC4CC(=O)N(c5ccc(F)cc5)C4)cc3)nc2n(CCC)c1=O 10.1016/j.ejmech.2016.11.007
CHEMBL4069458 156659 None 0 Human Binding pKi = 8.3 8.3 - 1
Displacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting methodDisplacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting method
ChEMBL 519 9 1 7 3.9 CCCn1c(=O)c2[nH]c(-c3ccc(OCC4CC(=O)N(c5ccc(F)cc5)C4)cc3)nc2n(CCC)c1=O 10.1016/j.ejmech.2016.11.007
162650047 180068 None 0 Human Binding pKi = 8.3 8.3 -69 2
Inhibition of FRET-labelled CA200645 binding to human adenosine 2B receptor expressed in CHO cells incubated for 2 hr by TR-FRET assayInhibition of FRET-labelled CA200645 binding to human adenosine 2B receptor expressed in CHO cells incubated for 2 hr by TR-FRET assay
ChEMBL 393 5 2 7 3.0 COc1nc(-c2ncco2)nc(N)c1C(=O)NCc1c(Cl)cccc1Cl 10.1021/acs.jmedchem.0c00237
CHEMBL4747929 180068 None 0 Human Binding pKi = 8.3 8.3 -69 2
Inhibition of FRET-labelled CA200645 binding to human adenosine 2B receptor expressed in CHO cells incubated for 2 hr by TR-FRET assayInhibition of FRET-labelled CA200645 binding to human adenosine 2B receptor expressed in CHO cells incubated for 2 hr by TR-FRET assay
ChEMBL 393 5 2 7 3.0 COc1nc(-c2ncco2)nc(N)c1C(=O)NCc1c(Cl)cccc1Cl 10.1021/acs.jmedchem.0c00237
44185934 186710 None 0 Human Binding pKi = 8.3 8.3 14 4
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 403 4 2 6 1.3 CCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCCCC4)cc3)[nH]c2c1=O 10.1021/jm900413e
CHEMBL488542 186710 None 0 Human Binding pKi = 8.3 8.3 14 4
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 403 4 2 6 1.3 CCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCCCC4)cc3)[nH]c2c1=O 10.1021/jm900413e
168297138 192241 None 0 Human Binding pKi = 8.3 8.3 - 1
Displacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cell membrane preincubated for 4 hrs followed by [3H]PSB-603 addition and measured after 0.5 hrs by radioligand displacement assayDisplacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cell membrane preincubated for 4 hrs followed by [3H]PSB-603 addition and measured after 0.5 hrs by radioligand displacement assay
ChEMBL 368 5 2 7 1.1 CCCn1c(=O)[nH]c2nc(-c3ccc(OS(=O)(=O)F)cc3)[nH]c2c1=O 10.1039/d2md00132b
CHEMBL5205220 192241 None 0 Human Binding pKi = 8.3 8.3 - 1
Displacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cell membrane preincubated for 4 hrs followed by [3H]PSB-603 addition and measured after 0.5 hrs by radioligand displacement assayDisplacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cell membrane preincubated for 4 hrs followed by [3H]PSB-603 addition and measured after 0.5 hrs by radioligand displacement assay
ChEMBL 368 5 2 7 1.1 CCCn1c(=O)[nH]c2nc(-c3ccc(OS(=O)(=O)F)cc3)[nH]c2c1=O 10.1039/d2md00132b
135484064 2616 None 4 Human Binding pKi = 8.3 8.3 21 4
Binding affinity of compound for displacement of [3H]DPCPX binding in HEK293 membranes expressing human A2B adenosine receptorsBinding affinity of compound for displacement of [3H]DPCPX binding in HEK293 membranes expressing human A2B adenosine receptors
ChEMBL 509 9 2 11 1.9 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)Nc1ccc2c(c1)OCO2 10.1021/jm0309654
390 2616 None 4 Human Binding pKi = 8.3 8.3 21 4
Binding affinity of compound for displacement of [3H]DPCPX binding in HEK293 membranes expressing human A2B adenosine receptorsBinding affinity of compound for displacement of [3H]DPCPX binding in HEK293 membranes expressing human A2B adenosine receptors
ChEMBL 509 9 2 11 1.9 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)Nc1ccc2c(c1)OCO2 10.1021/jm0309654
CHEMBL260331 2616 None 4 Human Binding pKi = 8.3 8.3 21 4
Binding affinity of compound for displacement of [3H]DPCPX binding in HEK293 membranes expressing human A2B adenosine receptorsBinding affinity of compound for displacement of [3H]DPCPX binding in HEK293 membranes expressing human A2B adenosine receptors
ChEMBL 509 9 2 11 1.9 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)Nc1ccc2c(c1)OCO2 10.1021/jm0309654
135484064 2616 None 4 Human Binding pKi = 8.3 8.3 21 4
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 509 9 2 11 1.9 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)Nc1ccc2c(c1)OCO2 10.1021/jm0309654
390 2616 None 4 Human Binding pKi = 8.3 8.3 21 4
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 509 9 2 11 1.9 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)Nc1ccc2c(c1)OCO2 10.1021/jm0309654
CHEMBL260331 2616 None 4 Human Binding pKi = 8.3 8.3 21 4
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 509 9 2 11 1.9 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)Nc1ccc2c(c1)OCO2 10.1021/jm0309654
135484064 2616 None 4 Human Binding pKi = 8.3 8.3 21 4
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 509 9 2 11 1.9 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)Nc1ccc2c(c1)OCO2 10.1021/jm900413e
390 2616 None 4 Human Binding pKi = 8.3 8.3 21 4
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 509 9 2 11 1.9 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)Nc1ccc2c(c1)OCO2 10.1021/jm900413e
CHEMBL260331 2616 None 4 Human Binding pKi = 8.3 8.3 21 4
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 509 9 2 11 1.9 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)Nc1ccc2c(c1)OCO2 10.1021/jm900413e
135484064 2616 None 4 Human Binding pKi = 8.3 8.3 21 4
Displacement of [3H] DPCPX from human recombinant Adenosine A2B receptor expressed in HEK293 cells after 60 minsDisplacement of [3H] DPCPX from human recombinant Adenosine A2B receptor expressed in HEK293 cells after 60 mins
ChEMBL 509 9 2 11 1.9 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)Nc1ccc2c(c1)OCO2 10.1021/acs.jmedchem.5b01586
390 2616 None 4 Human Binding pKi = 8.3 8.3 21 4
Displacement of [3H] DPCPX from human recombinant Adenosine A2B receptor expressed in HEK293 cells after 60 minsDisplacement of [3H] DPCPX from human recombinant Adenosine A2B receptor expressed in HEK293 cells after 60 mins
ChEMBL 509 9 2 11 1.9 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)Nc1ccc2c(c1)OCO2 10.1021/acs.jmedchem.5b01586
CHEMBL260331 2616 None 4 Human Binding pKi = 8.3 8.3 21 4
Displacement of [3H] DPCPX from human recombinant Adenosine A2B receptor expressed in HEK293 cells after 60 minsDisplacement of [3H] DPCPX from human recombinant Adenosine A2B receptor expressed in HEK293 cells after 60 mins
ChEMBL 509 9 2 11 1.9 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)Nc1ccc2c(c1)OCO2 10.1021/acs.jmedchem.5b01586
44236601 157581 None 0 Human Binding pKi = 8.3 8.3 - 1
Displacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 minsDisplacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 mins
ChEMBL 500 7 1 8 3.5 CCCn1c(=O)c2[nH]c(-c3cnn(CC#Cc4ccc(OC(F)(F)F)cc4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2017.04.014
CHEMBL4080646 157581 None 0 Human Binding pKi = 8.3 8.3 - 1
Displacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 minsDisplacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 mins
ChEMBL 500 7 1 8 3.5 CCCn1c(=O)c2[nH]c(-c3cnn(CC#Cc4ccc(OC(F)(F)F)cc4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2017.04.014
44450982 100975 None 0 Human Binding pKi = 8.3 8.3 120 4
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 576 8 1 6 5.1 CCCn1c(=O)n(C)c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCC(c5ccccc5)(c5ccccc5)CC4)cc3)cc21 10.1016/j.bmc.2008.01.002
CHEMBL294223 100975 None 0 Human Binding pKi = 8.3 8.3 120 4
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 576 8 1 6 5.1 CCCn1c(=O)n(C)c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCC(c5ccccc5)(c5ccccc5)CC4)cc3)cc21 10.1016/j.bmc.2008.01.002
135484064 2616 None 4 Human Binding pKi = 8.3 8.3 21 4
Displacement of [3H]DPCPX from human adenosine receptor A2b expressed in HEK293 cell membranesDisplacement of [3H]DPCPX from human adenosine receptor A2b expressed in HEK293 cell membranes
ChEMBL 509 9 2 11 1.9 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)Nc1ccc2c(c1)OCO2 10.1016/j.ejmech.2016.11.007
390 2616 None 4 Human Binding pKi = 8.3 8.3 21 4
Displacement of [3H]DPCPX from human adenosine receptor A2b expressed in HEK293 cell membranesDisplacement of [3H]DPCPX from human adenosine receptor A2b expressed in HEK293 cell membranes
ChEMBL 509 9 2 11 1.9 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)Nc1ccc2c(c1)OCO2 10.1016/j.ejmech.2016.11.007
CHEMBL260331 2616 None 4 Human Binding pKi = 8.3 8.3 21 4
Displacement of [3H]DPCPX from human adenosine receptor A2b expressed in HEK293 cell membranesDisplacement of [3H]DPCPX from human adenosine receptor A2b expressed in HEK293 cell membranes
ChEMBL 509 9 2 11 1.9 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)Nc1ccc2c(c1)OCO2 10.1016/j.ejmech.2016.11.007
10226014 94591 None 0 Human Binding pKi = 8.3 8.3 - 1
Displacement of [3H]DPCPX to human A2B adenosine receptor derived from HEK cells assessed as inhibition constantDisplacement of [3H]DPCPX to human A2B adenosine receptor derived from HEK cells assessed as inhibition constant
ChEMBL 452 6 2 9 2.4 CCCn1c(=O)[nH]c2nc(-c3cnn(Cc4noc(-c5ccc(Cl)cc5)n4)c3)[nH]c2c1=O 10.1021/acs.jmedchem.1c00261
CHEMBL252048 94591 None 0 Human Binding pKi = 8.3 8.3 - 1
Displacement of [3H]DPCPX to human A2B adenosine receptor derived from HEK cells assessed as inhibition constantDisplacement of [3H]DPCPX to human A2B adenosine receptor derived from HEK cells assessed as inhibition constant
ChEMBL 452 6 2 9 2.4 CCCn1c(=O)[nH]c2nc(-c3cnn(Cc4noc(-c5ccc(Cl)cc5)n4)c3)[nH]c2c1=O 10.1021/acs.jmedchem.1c00261
135484064 2616 None 4 Human Binding pKi = 8.3 8.3 21 4
Displacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 509 9 2 11 1.9 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)Nc1ccc2c(c1)OCO2 10.1021/jm201292w
390 2616 None 4 Human Binding pKi = 8.3 8.3 21 4
Displacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 509 9 2 11 1.9 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)Nc1ccc2c(c1)OCO2 10.1021/jm201292w
CHEMBL260331 2616 None 4 Human Binding pKi = 8.3 8.3 21 4
Displacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 509 9 2 11 1.9 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)Nc1ccc2c(c1)OCO2 10.1021/jm201292w
135484064 2616 None 4 Human Binding pKi = 8.3 8.3 21 4
Displacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation countingDisplacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation counting
ChEMBL 509 9 2 11 1.9 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)Nc1ccc2c(c1)OCO2 10.1021/jm201292w
390 2616 None 4 Human Binding pKi = 8.3 8.3 21 4
Displacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation countingDisplacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation counting
ChEMBL 509 9 2 11 1.9 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)Nc1ccc2c(c1)OCO2 10.1021/jm201292w
CHEMBL260331 2616 None 4 Human Binding pKi = 8.3 8.3 21 4
Displacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation countingDisplacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation counting
ChEMBL 509 9 2 11 1.9 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)Nc1ccc2c(c1)OCO2 10.1021/jm201292w
136042343 71169 None 0 Human Binding pKi = 8.3 8.3 11 2
Displacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation countingDisplacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation counting
ChEMBL 501 8 2 9 3.6 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5cc(Cl)c(F)cc5[nH]4)no3)nc2n(CCC)c1=O 10.1021/jm201292w
CHEMBL1955919 71169 None 0 Human Binding pKi = 8.3 8.3 11 2
Displacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation countingDisplacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation counting
ChEMBL 501 8 2 9 3.6 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5cc(Cl)c(F)cc5[nH]4)no3)nc2n(CCC)c1=O 10.1021/jm201292w
135484064 2616 None 4 Human Binding pKi = 8.3 8.3 21 4
Displacement of [3H]MRE2029F20 from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]MRE2029F20 from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 509 9 2 11 1.9 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)Nc1ccc2c(c1)OCO2 10.1016/j.bmc.2007.11.058
390 2616 None 4 Human Binding pKi = 8.3 8.3 21 4
Displacement of [3H]MRE2029F20 from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]MRE2029F20 from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 509 9 2 11 1.9 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)Nc1ccc2c(c1)OCO2 10.1016/j.bmc.2007.11.058
CHEMBL260331 2616 None 4 Human Binding pKi = 8.3 8.3 21 4
Displacement of [3H]MRE2029F20 from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]MRE2029F20 from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 509 9 2 11 1.9 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)Nc1ccc2c(c1)OCO2 10.1016/j.bmc.2007.11.058
10895702 139180 None 0 Human Binding pKi = 8.3 8.3 3 3
Inhibition of [3H]ZM-241380 binding to adenosine A2b receptorInhibition of [3H]ZM-241380 binding to adenosine A2b receptor
ChEMBL 454 8 2 7 1.4 CCCCn1c(=O)[nH]c2[nH]c(-c3ccc(OCC(=O)N4CCN(CC)CC4)cc3)nc2c1=O 10.1021/jm049513x
CHEMBL37875 139180 None 0 Human Binding pKi = 8.3 8.3 3 3
Inhibition of [3H]ZM-241380 binding to adenosine A2b receptorInhibition of [3H]ZM-241380 binding to adenosine A2b receptor
ChEMBL 454 8 2 7 1.4 CCCCn1c(=O)[nH]c2[nH]c(-c3ccc(OCC(=O)N4CCN(CC)CC4)cc3)nc2c1=O 10.1021/jm049513x
10895702 139180 None 0 Human Binding pKi = 8.3 8.3 3 3
Inhibition of [3H]ZM-241385 binding to human adenosine A2B receptorInhibition of [3H]ZM-241385 binding to human adenosine A2B receptor
ChEMBL 454 8 2 7 1.4 CCCCn1c(=O)[nH]c2[nH]c(-c3ccc(OCC(=O)N4CCN(CC)CC4)cc3)nc2c1=O 10.1021/jm011049y
CHEMBL37875 139180 None 0 Human Binding pKi = 8.3 8.3 3 3
Inhibition of [3H]ZM-241385 binding to human adenosine A2B receptorInhibition of [3H]ZM-241385 binding to human adenosine A2B receptor
ChEMBL 454 8 2 7 1.4 CCCCn1c(=O)[nH]c2[nH]c(-c3ccc(OCC(=O)N4CCN(CC)CC4)cc3)nc2c1=O 10.1021/jm011049y
11510702 73118 None 0 Human Binding pKi = 8.3 8.3 11 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 450 7 2 6 3.3 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(F)cc4)cc3)cc2n(C)c1=O 10.1021/jm0506221
CHEMBL201127 73118 None 0 Human Binding pKi = 8.3 8.3 11 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 450 7 2 6 3.3 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(F)cc4)cc3)cc2n(C)c1=O 10.1021/jm0506221
44450982 100975 None 0 Human Binding pKi = 8.3 8.3 120 4
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 576 8 1 6 5.1 CCCn1c(=O)n(C)c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCC(c5ccccc5)(c5ccccc5)CC4)cc3)cc21 10.1016/j.bmc.2008.01.002
CHEMBL294223 100975 None 0 Human Binding pKi = 8.3 8.3 120 4
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 576 8 1 6 5.1 CCCn1c(=O)n(C)c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCC(c5ccccc5)(c5ccccc5)CC4)cc3)cc21 10.1016/j.bmc.2008.01.002
155552405 174055 None 0 Human Binding pKi = 8.2 8.2 25 2
Displacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 522 6 2 7 1.6 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(C(=O)c5ccccc5)CC4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
CHEMBL4543948 174055 None 0 Human Binding pKi = 8.2 8.2 25 2
Displacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 522 6 2 7 1.6 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(C(=O)c5ccccc5)CC4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
44451100 156886 None 0 Human Binding pKi = 8.2 8.2 109 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 592 7 1 9 4.1 CCCn1c(=O)n(C)c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCN(c5nc6ccc(Cl)cc6s5)CC4)cc3)cc21 10.1016/j.bmc.2008.01.002
CHEMBL407202 156886 None 0 Human Binding pKi = 8.2 8.2 109 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 592 7 1 9 4.1 CCCn1c(=O)n(C)c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCN(c5nc6ccc(Cl)cc6s5)CC4)cc3)cc21 10.1016/j.bmc.2008.01.002
11621020 72794 None 0 Human Binding pKi = 8.2 8.2 - 1
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 558 7 2 6 3.7 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(I)cc4)cc3)cc2n(C)c1=O 10.1021/jm0506221
CHEMBL200052 72794 None 0 Human Binding pKi = 8.2 8.2 - 1
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 558 7 2 6 3.7 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(I)cc4)cc3)cc2n(C)c1=O 10.1021/jm0506221
44236503 158059 None 0 Human Binding pKi = 8.2 8.2 - 1
Displacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 minsDisplacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 mins
ChEMBL 434 6 1 7 2.8 CCCn1c(=O)c2[nH]c(-c3cnn(CC#Cc4ccc(F)cc4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2017.04.014
CHEMBL4086077 158059 None 0 Human Binding pKi = 8.2 8.2 - 1
Displacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 minsDisplacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 mins
ChEMBL 434 6 1 7 2.8 CCCn1c(=O)c2[nH]c(-c3cnn(CC#Cc4ccc(F)cc4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2017.04.014
44574252 178482 None 0 Human Binding pKi = 8.2 8.2 1 2
Displacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells by beta scintillation counterDisplacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells by beta scintillation counter
ChEMBL 450 8 3 7 3.5 CCCn1c(=O)c2[nH]c(-c3ccc(COC(=O)Nc4cc[nH]n4)cc3)cc2n(CCC)c1=O 10.1016/j.bmc.2009.03.062
CHEMBL466453 178482 None 0 Human Binding pKi = 8.2 8.2 1 2
Displacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells by beta scintillation counterDisplacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells by beta scintillation counter
ChEMBL 450 8 3 7 3.5 CCCn1c(=O)c2[nH]c(-c3ccc(COC(=O)Nc4cc[nH]n4)cc3)cc2n(CCC)c1=O 10.1016/j.bmc.2009.03.062
145967791 164822 None 0 Human Binding pKi = 8.2 8.2 10 6
Displacement of [3H]PSB-603 from recombinant human adenosine A2B receptor expressed in CHO cell membranes after 75 mins by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human adenosine A2B receptor expressed in CHO cell membranes after 75 mins by liquid scintillation counting method
ChEMBL 659 12 3 7 5.0 CCCn1c(=O)[nH]c2nc(-c3ccc(OCC(=O)NCCCCCC4=C5C(C)=CC(C)=[N+]5[B-](F)(F)n5c(C)cc(C)c54)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.7b01627
CHEMBL4218673 164822 None 0 Human Binding pKi = 8.2 8.2 10 6
Displacement of [3H]PSB-603 from recombinant human adenosine A2B receptor expressed in CHO cell membranes after 75 mins by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human adenosine A2B receptor expressed in CHO cell membranes after 75 mins by liquid scintillation counting method
ChEMBL 659 12 3 7 5.0 CCCn1c(=O)[nH]c2nc(-c3ccc(OCC(=O)NCCCCCC4=C5C(C)=CC(C)=[N+]5[B-](F)(F)n5c(C)cc(C)c54)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.7b01627
10196114 63973 None 11 Human Binding pKi = 7.3 7.3 - 1
Binding affinity for adenosine A2b receptor by using as [3H]ZM-241385 (14 nM) radioligand in membranes from HEK-A2B cellsBinding affinity for adenosine A2b receptor by using as [3H]ZM-241385 (14 nM) radioligand in membranes from HEK-A2B cells
ChEMBL 516 10 1 10 4.0 CCCn1c(=O)c2nc(-c3ccc(OCc4noc(-c5cccc(OC)c5)n4)cc3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2004.11.044
CHEMBL180693 63973 None 11 Human Binding pKi = 7.3 7.3 - 1
Binding affinity for adenosine A2b receptor by using as [3H]ZM-241385 (14 nM) radioligand in membranes from HEK-A2B cellsBinding affinity for adenosine A2b receptor by using as [3H]ZM-241385 (14 nM) radioligand in membranes from HEK-A2B cells
ChEMBL 516 10 1 10 4.0 CCCn1c(=O)c2nc(-c3ccc(OCc4noc(-c5cccc(OC)c5)n4)cc3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2004.11.044
135465774 111479 None 0 Human Binding pKi = 7.3 7.3 64 2
Binding affinity of compound for displacement of [3H]DPCPX binding in HEK293 membranes expressing human A2B adenosine receptorsBinding affinity of compound for displacement of [3H]DPCPX binding in HEK293 membranes expressing human A2B adenosine receptors
ChEMBL 467 8 2 8 2.4 CCCn1c(=O)c2nc(-c3cc(NC(=O)Cc4cccc(F)c4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
CHEMBL32770 111479 None 0 Human Binding pKi = 7.3 7.3 64 2
Binding affinity of compound for displacement of [3H]DPCPX binding in HEK293 membranes expressing human A2B adenosine receptorsBinding affinity of compound for displacement of [3H]DPCPX binding in HEK293 membranes expressing human A2B adenosine receptors
ChEMBL 467 8 2 8 2.4 CCCn1c(=O)c2nc(-c3cc(NC(=O)Cc4cccc(F)c4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
135465774 111479 None 0 Human Binding pKi = 7.3 7.3 64 2
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 467 8 2 8 2.4 CCCn1c(=O)c2nc(-c3cc(NC(=O)Cc4cccc(F)c4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
CHEMBL32770 111479 None 0 Human Binding pKi = 7.3 7.3 64 2
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 467 8 2 8 2.4 CCCn1c(=O)c2nc(-c3cc(NC(=O)Cc4cccc(F)c4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
10196114 63973 None 11 Human Binding pKi = 7.3 7.3 - 1
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 516 10 1 10 4.0 CCCn1c(=O)c2nc(-c3ccc(OCc4noc(-c5cccc(OC)c5)n4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm201292w
CHEMBL180693 63973 None 11 Human Binding pKi = 7.3 7.3 - 1
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 516 10 1 10 4.0 CCCn1c(=O)c2nc(-c3ccc(OCc4noc(-c5cccc(OC)c5)n4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm201292w
10905799 119910 None 0 Human Binding pKi = 7.3 7.3 -7 4
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 43-58Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 43-58
ChEMBL 416 6 2 8 4.2 CCCCn1cc2c(nc(NC(=O)Nc3ccccc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm0109614
CHEMBL349240 119910 None 0 Human Binding pKi = 7.3 7.3 -7 4
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 43-58Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 43-58
ChEMBL 416 6 2 8 4.2 CCCCn1cc2c(nc(NC(=O)Nc3ccccc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm0109614
44588515 175157 None 0 Human Binding pKi = 7.3 7.3 2 2
Displacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cells
ChEMBL 372 6 2 7 2.6 CCCn1c(=O)c2[nH]c(-c3ccc([N+](=O)[O-])cc3)c(O)c2n(CCC)c1=O 10.1016/j.bmc.2008.09.067
CHEMBL457014 175157 None 0 Human Binding pKi = 7.3 7.3 2 2
Displacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cells
ChEMBL 372 6 2 7 2.6 CCCn1c(=O)c2[nH]c(-c3ccc([N+](=O)[O-])cc3)c(O)c2n(CCC)c1=O 10.1016/j.bmc.2008.09.067
176407 4148 None 84 Human Binding pKi = 7.3 7.3 -34 6
Inhibition of human adenosine 2B receptorInhibition of human adenosine 2B receptor
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1021/acs.jmedchem.0c00237
405 4148 None 84 Human Binding pKi = 7.3 7.3 -34 6
Inhibition of human adenosine 2B receptorInhibition of human adenosine 2B receptor
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1021/acs.jmedchem.0c00237
CHEMBL113142 4148 None 84 Human Binding pKi = 7.3 7.3 -34 6
Inhibition of human adenosine 2B receptorInhibition of human adenosine 2B receptor
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1021/acs.jmedchem.0c00237
DB08770 4148 None 84 Human Binding pKi = 7.3 7.3 -34 6
Inhibition of human adenosine 2B receptorInhibition of human adenosine 2B receptor
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1021/acs.jmedchem.0c00237
176407 4148 None 84 Human Binding pKi = 7.3 7.3 -34 6
Inhibition of human recombinant adenosine receptor A2bInhibition of human recombinant adenosine receptor A2b
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1021/jm4011669
405 4148 None 84 Human Binding pKi = 7.3 7.3 -34 6
Inhibition of human recombinant adenosine receptor A2bInhibition of human recombinant adenosine receptor A2b
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1021/jm4011669
CHEMBL113142 4148 None 84 Human Binding pKi = 7.3 7.3 -34 6
Inhibition of human recombinant adenosine receptor A2bInhibition of human recombinant adenosine receptor A2b
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1021/jm4011669
DB08770 4148 None 84 Human Binding pKi = 7.3 7.3 -34 6
Inhibition of human recombinant adenosine receptor A2bInhibition of human recombinant adenosine receptor A2b
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1021/jm4011669
CHEMBL5084351 214910 None 4 Human Binding pKi = 7.3 7.3 -33 3
Displacement of [3H]DPCPX from human A2BAR expressed in HEK293 cell membrane incubated for 30 mins by microbeta trilux scintillation counter analysisDisplacement of [3H]DPCPX from human A2BAR expressed in HEK293 cell membrane incubated for 30 mins by microbeta trilux scintillation counter analysis
ChEMBL None None None N#Cc1c(-c2ccccc2)nc(N)nc1-c1cccc(O)c1 10.1021/acs.jmedchem.1c01636
56844240 1109 None 0 Human Binding pKi = 7.3 7.3 -11 3
Inhibition of adenosine A2B receptorInhibition of adenosine A2B receptor
ChEMBL 277 2 1 5 2.8 Nc1nnc(c(n1)c1ccccc1)c1cc(C)nc(c1)C 10.1021/jm201376w
9236 1109 None 0 Human Binding pKi = 7.3 7.3 -11 3
Inhibition of adenosine A2B receptorInhibition of adenosine A2B receptor
ChEMBL 277 2 1 5 2.8 Nc1nnc(c(n1)c1ccccc1)c1cc(C)nc(c1)C 10.1021/jm201376w
CHEMBL2024115 1109 None 0 Human Binding pKi = 7.3 7.3 -11 3
Inhibition of adenosine A2B receptorInhibition of adenosine A2B receptor
ChEMBL 277 2 1 5 2.8 Nc1nnc(c(n1)c1ccccc1)c1cc(C)nc(c1)C 10.1021/jm201376w
137636304 156201 None 0 Human Binding pKi = 6.3 6.3 -691 3
Displacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes measured after 90 minsDisplacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes measured after 90 mins
ChEMBL 419 4 2 7 3.4 COc1ccc(N2CCOCC2)c2sc(NC(=O)C3(C)CCC(C)(O)CC3)nc12 10.1021/acs.jmedchem.6b01584
CHEMBL4064207 156201 None 0 Human Binding pKi = 6.3 6.3 -691 3
Displacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes measured after 90 minsDisplacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes measured after 90 mins
ChEMBL 419 4 2 7 3.4 COc1ccc(N2CCOCC2)c2sc(NC(=O)C3(C)CCC(C)(O)CC3)nc12 10.1021/acs.jmedchem.6b01584
132941757 158899 None 0 Human Binding pKi = 6.3 6.3 -870 3
Displacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes measured after 90 minsDisplacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes measured after 90 mins
ChEMBL 460 7 1 7 4.4 CCN(CC)C1CCC(C)(C(=O)Nc2nc3c(OC)ccc(N4CCOCC4)c3s2)CC1 10.1021/acs.jmedchem.6b01584
CHEMBL4095355 158899 None 0 Human Binding pKi = 6.3 6.3 -870 3
Displacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes measured after 90 minsDisplacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes measured after 90 mins
ChEMBL 460 7 1 7 4.4 CCN(CC)C1CCC(C)(C(=O)Nc2nc3c(OC)ccc(N4CCOCC4)c3s2)CC1 10.1021/acs.jmedchem.6b01584
145973260 164598 None 0 Human Binding pKi = 5.3 5.3 -11481 4
Displacement of [3H]-MRS-1754 from human A2B receptor expressed in HEK293 cell membranes after 90 mins radioligand binding assayDisplacement of [3H]-MRS-1754 from human A2B receptor expressed in HEK293 cell membranes after 90 mins radioligand binding assay
ChEMBL 568 9 1 14 1.5 COCCOc1ccc(N2CCN(CCn3c(=O)n(C)c4c3nc(N)n3nc(-c5nccs5)nc43)CC2)cc1F 10.1021/acsmedchemlett.7b00175
CHEMBL4215754 164598 None 0 Human Binding pKi = 5.3 5.3 -11481 4
Displacement of [3H]-MRS-1754 from human A2B receptor expressed in HEK293 cell membranes after 90 mins radioligand binding assayDisplacement of [3H]-MRS-1754 from human A2B receptor expressed in HEK293 cell membranes after 90 mins radioligand binding assay
ChEMBL 568 9 1 14 1.5 COCCOc1ccc(N2CCN(CCn3c(=O)n(C)c4c3nc(N)n3nc(-c5nccs5)nc43)CC2)cc1F 10.1021/acsmedchemlett.7b00175
11618368 3847 None 77 Human Binding pKi = 5.3 5.3 -501 5
Displacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes measured after 90 minsDisplacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes measured after 90 mins
ChEMBL 406 3 2 7 2.5 COc1ccc(c2c1nc(s2)NC(=O)N1CCC(CC1)(C)O)N1CCOCC1 10.1021/acs.jmedchem.6b01584
5611 3847 None 77 Human Binding pKi = 5.3 5.3 -501 5
Displacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes measured after 90 minsDisplacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes measured after 90 mins
ChEMBL 406 3 2 7 2.5 COc1ccc(c2c1nc(s2)NC(=O)N1CCC(CC1)(C)O)N1CCOCC1 10.1021/acs.jmedchem.6b01584
CHEMBL2105747 3847 None 77 Human Binding pKi = 5.3 5.3 -501 5
Displacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes measured after 90 minsDisplacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes measured after 90 mins
ChEMBL 406 3 2 7 2.5 COc1ccc(c2c1nc(s2)NC(=O)N1CCC(CC1)(C)O)N1CCOCC1 10.1021/acs.jmedchem.6b01584
DB12203 3847 None 77 Human Binding pKi = 5.3 5.3 -501 5
Displacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes measured after 90 minsDisplacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes measured after 90 mins
ChEMBL 406 3 2 7 2.5 COc1ccc(c2c1nc(s2)NC(=O)N1CCC(CC1)(C)O)N1CCOCC1 10.1021/acs.jmedchem.6b01584
137634085 156289 None 0 Human Binding pKi = 5.3 5.3 -1258 4
Displacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes measured after 90 minsDisplacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes measured after 90 mins
ChEMBL 463 6 1 7 4.2 COc1ccc(N2CCOCC2)c2sc(NC(=O)C(C)(C)Oc3ccc(F)c(F)c3)nc12 10.1021/acs.jmedchem.6b01584
CHEMBL4065326 156289 None 0 Human Binding pKi = 5.3 5.3 -1258 4
Displacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes measured after 90 minsDisplacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes measured after 90 mins
ChEMBL 463 6 1 7 4.2 COc1ccc(N2CCOCC2)c2sc(NC(=O)C(C)(C)Oc3ccc(F)c(F)c3)nc12 10.1021/acs.jmedchem.6b01584
44574223 178711 None 0 Human Binding pKi = 6.3 6.3 6 2
Displacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells by beta scintillation counterDisplacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells by beta scintillation counter
ChEMBL 466 8 2 7 4.8 CCCn1c(=O)c2[nH]c(-c3ccc(COC(=O)Nc4ccsc4)cc3)cc2n(CCC)c1=O 10.1016/j.bmc.2009.03.062
CHEMBL468306 178711 None 0 Human Binding pKi = 6.3 6.3 6 2
Displacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells by beta scintillation counterDisplacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells by beta scintillation counter
ChEMBL 466 8 2 7 4.8 CCCn1c(=O)c2[nH]c(-c3ccc(COC(=O)Nc4ccsc4)cc3)cc2n(CCC)c1=O 10.1016/j.bmc.2009.03.062
44452435 96612 None 0 Human Binding pKi = 6.3 6.3 -39 4
Displacement of [3]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 383 5 1 6 4.1 O=C(CCc1ccccc1)Nc1nc2ccccc2n2nc(-c3ccco3)nc12 10.1016/j.bmc.2007.10.103
CHEMBL263372 96612 None 0 Human Binding pKi = 6.3 6.3 -39 4
Displacement of [3]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 383 5 1 6 4.1 O=C(CCc1ccccc1)Nc1nc2ccccc2n2nc(-c3ccco3)nc12 10.1016/j.bmc.2007.10.103
10346511 103047 None 5 Human Binding pKi = 5.3 5.3 -2754 8
Displacement of [3H]- ZM-241385 from human adenosine A2B receptor expressed in HEK cellsDisplacement of [3H]- ZM-241385 from human adenosine A2B receptor expressed in HEK cells
ChEMBL 517 5 4 9 1.3 OC[C@H]1O[C@@H](n2cnc3c(NCc4cccc(I)c4)nc(Cl)nc32)[C@H](O)[C@@H]1O 10.1021/jm9905965
CHEMBL307199 103047 None 5 Human Binding pKi = 5.3 5.3 -2754 8
Displacement of [3H]- ZM-241385 from human adenosine A2B receptor expressed in HEK cellsDisplacement of [3H]- ZM-241385 from human adenosine A2B receptor expressed in HEK cells
ChEMBL 517 5 4 9 1.3 OC[C@H]1O[C@@H](n2cnc3c(NCc4cccc(I)c4)nc(Cl)nc32)[C@H](O)[C@@H]1O 10.1021/jm9905965
11995448 141459 None 0 Human Binding pKi = 6.3 6.3 -22 3
Displacement of [125I]3-(4-aminobenzyl)-8-phenyloxyacetate-1-propyl-xanthine from human adenosine A2B receptor expressed in HEK cellsDisplacement of [125I]3-(4-aminobenzyl)-8-phenyloxyacetate-1-propyl-xanthine from human adenosine A2B receptor expressed in HEK cells
ChEMBL 473 9 2 8 2.0 CCCn1c(=O)c2nc([C@]34CC[C@](C(=O)NCCC(=O)OC)(CC3)CC4)[nH]c2n(CCC)c1=O 10.1021/jm0605381
CHEMBL384257 141459 None 0 Human Binding pKi = 6.3 6.3 -22 3
Displacement of [125I]3-(4-aminobenzyl)-8-phenyloxyacetate-1-propyl-xanthine from human adenosine A2B receptor expressed in HEK cellsDisplacement of [125I]3-(4-aminobenzyl)-8-phenyloxyacetate-1-propyl-xanthine from human adenosine A2B receptor expressed in HEK cells
ChEMBL 473 9 2 8 2.0 CCCn1c(=O)c2nc([C@]34CC[C@](C(=O)NCCC(=O)OC)(CC3)CC4)[nH]c2n(CCC)c1=O 10.1021/jm0605381
24827556 159780 None 0 Human Binding pKi = 6.3 6.3 2 3
Displacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 381 5 1 8 0.8 CCCn1c(=O)c2[nH]c(-c3cnn(-c4ccc[n+]([O-])c4)c3)nc2n(CC)c1=O 10.1021/jm7014815
CHEMBL410529 159780 None 0 Human Binding pKi = 6.3 6.3 2 3
Displacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 381 5 1 8 0.8 CCCn1c(=O)c2[nH]c(-c3cnn(-c4ccc[n+]([O-])c4)c3)nc2n(CC)c1=O 10.1021/jm7014815
156015785 177617 None 0 Human Binding pKi = 6.3 6.3 -2 4
Displacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting methodDisplacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting method
ChEMBL 324 3 1 7 2.9 CCOC(=O)C1=C(C)Nc2nc3ccccc3n2C1c1cnco1 10.1021/acs.jmedchem.0c00564
CHEMBL4640980 177617 None 0 Human Binding pKi = 6.3 6.3 -2 4
Displacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting methodDisplacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting method
ChEMBL 324 3 1 7 2.9 CCOC(=O)C1=C(C)Nc2nc3ccccc3n2C1c1cnco1 10.1021/acs.jmedchem.0c00564
135493292 100278 None 0 Human Binding pKi = 7.3 7.3 - 1
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 512 11 2 11 2.4 CCCn1c(=O)c2nc(-c3cc(OCC(=O)Nc4ccc(OC)c(OC)c4)no3)[nH]c2n(CCC)c1=O 10.1021/jm0309654
CHEMBL289002 100278 None 0 Human Binding pKi = 7.3 7.3 - 1
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 512 11 2 11 2.4 CCCn1c(=O)c2nc(-c3cc(OCC(=O)Nc4ccc(OC)c(OC)c4)no3)[nH]c2n(CCC)c1=O 10.1021/jm0309654
135485985 98579 None 43 Human Binding pKi = 7.3 7.3 -2 6
Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 44-58Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 44-58
ChEMBL 241 1 2 7 0.8 Nc1nc2n[nH]cc2c2nc(-c3ccco3)nn12 10.1021/jm001047y
CHEMBL276738 98579 None 43 Human Binding pKi = 7.3 7.3 -2 6
Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 44-58Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 44-58
ChEMBL 241 1 2 7 0.8 Nc1nc2n[nH]cc2c2nc(-c3ccco3)nn12 10.1021/jm001047y
137650430 157199 None 0 Human Binding pKi = 7.3 7.3 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes after 30 minsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes after 30 mins
ChEMBL 290 3 2 5 1.7 CCOC(=O)C1=C(C)N/C(=N\C#N)NC1c1cccs1 10.1021/acs.jmedchem.7b00138
CHEMBL4075899 157199 None 0 Human Binding pKi = 7.3 7.3 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes after 30 minsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes after 30 mins
ChEMBL 290 3 2 5 1.7 CCOC(=O)C1=C(C)N/C(=N\C#N)NC1c1cccs1 10.1021/acs.jmedchem.7b00138
1329 1472 None 86 Human Binding pKi = 7.3 7.3 -1288 14
Displacement of [3H]DPCPX from human adenosine A2b receptor expressed in HEK293 cells after 30 minsDisplacement of [3H]DPCPX from human adenosine A2b receptor expressed in HEK293 cells after 30 mins
ChEMBL 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 10.1016/j.bmc.2010.09.043
386 1472 None 86 Human Binding pKi = 7.3 7.3 -1288 14
Displacement of [3H]DPCPX from human adenosine A2b receptor expressed in HEK293 cells after 30 minsDisplacement of [3H]DPCPX from human adenosine A2b receptor expressed in HEK293 cells after 30 mins
ChEMBL 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 10.1016/j.bmc.2010.09.043
CHEMBL183 1472 None 86 Human Binding pKi = 7.3 7.3 -1288 14
Displacement of [3H]DPCPX from human adenosine A2b receptor expressed in HEK293 cells after 30 minsDisplacement of [3H]DPCPX from human adenosine A2b receptor expressed in HEK293 cells after 30 mins
ChEMBL 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 10.1016/j.bmc.2010.09.043
DB12946 1472 None 86 Human Binding pKi = 7.3 7.3 -1288 14
Displacement of [3H]DPCPX from human adenosine A2b receptor expressed in HEK293 cells after 30 minsDisplacement of [3H]DPCPX from human adenosine A2b receptor expressed in HEK293 cells after 30 mins
ChEMBL 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 10.1016/j.bmc.2010.09.043
1329 1472 None 86 Human Binding pKi = 7.3 7.3 -1288 14
Inhibition of [3H]ZM-241,385 binding to adenosine A2b receptorInhibition of [3H]ZM-241,385 binding to adenosine A2b receptor
ChEMBL 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 10.1021/jm049513x
386 1472 None 86 Human Binding pKi = 7.3 7.3 -1288 14
Inhibition of [3H]ZM-241,385 binding to adenosine A2b receptorInhibition of [3H]ZM-241,385 binding to adenosine A2b receptor
ChEMBL 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 10.1021/jm049513x
CHEMBL183 1472 None 86 Human Binding pKi = 7.3 7.3 -1288 14
Inhibition of [3H]ZM-241,385 binding to adenosine A2b receptorInhibition of [3H]ZM-241,385 binding to adenosine A2b receptor
ChEMBL 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 10.1021/jm049513x
DB12946 1472 None 86 Human Binding pKi = 7.3 7.3 -1288 14
Inhibition of [3H]ZM-241,385 binding to adenosine A2b receptorInhibition of [3H]ZM-241,385 binding to adenosine A2b receptor
ChEMBL 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 10.1021/jm049513x
1329 1472 None 86 Human Binding pKi = 7.3 7.3 -1288 14
Inhibition of [3H]ZM-241385 binding to human adenosine A2B receptorInhibition of [3H]ZM-241385 binding to human adenosine A2B receptor
ChEMBL 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 10.1021/jm011049y
386 1472 None 86 Human Binding pKi = 7.3 7.3 -1288 14
Inhibition of [3H]ZM-241385 binding to human adenosine A2B receptorInhibition of [3H]ZM-241385 binding to human adenosine A2B receptor
ChEMBL 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 10.1021/jm011049y
CHEMBL183 1472 None 86 Human Binding pKi = 7.3 7.3 -1288 14
Inhibition of [3H]ZM-241385 binding to human adenosine A2B receptorInhibition of [3H]ZM-241385 binding to human adenosine A2B receptor
ChEMBL 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 10.1021/jm011049y
DB12946 1472 None 86 Human Binding pKi = 7.3 7.3 -1288 14
Inhibition of [3H]ZM-241385 binding to human adenosine A2B receptorInhibition of [3H]ZM-241385 binding to human adenosine A2B receptor
ChEMBL 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 10.1021/jm011049y
137660466 159287 None 0 Human Binding pKi = 7.3 7.3 -2 3
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes after 30 minsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes after 30 mins
ChEMBL 288 3 1 2 4.4 CC(=O)Nc1cc(-c2ccccc2)cc(-c2ccccc2)n1 10.1021/acs.jmedchem.7b00860
CHEMBL4099480 159287 None 0 Human Binding pKi = 7.3 7.3 -2 3
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes after 30 minsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes after 30 mins
ChEMBL 288 3 1 2 4.4 CC(=O)Nc1cc(-c2ccccc2)cc(-c2ccccc2)n1 10.1021/acs.jmedchem.7b00860
11495410 72693 None 0 Human Binding pKi = 7.3 7.3 3 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 418 6 2 6 1.9 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)NCc4ccccc4)cc3)cc2n(C)c1=O 10.1021/jm0506221
CHEMBL199688 72693 None 0 Human Binding pKi = 7.3 7.3 3 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 418 6 2 6 1.9 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)NCc4ccccc4)cc3)cc2n(C)c1=O 10.1021/jm0506221
11590453 72724 None 0 Human Binding pKi = 7.3 7.3 6 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 448 7 2 7 1.9 COc1cccc(CNC(=O)COc2ccc(-c3cc4c([nH]3)c(=O)n(C)c(=O)n4C)cc2)c1 10.1021/jm0506221
CHEMBL199826 72724 None 0 Human Binding pKi = 7.3 7.3 6 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 448 7 2 7 1.9 COc1cccc(CNC(=O)COc2ccc(-c3cc4c([nH]3)c(=O)n(C)c(=O)n4C)cc2)c1 10.1021/jm0506221
44451480 95806 None 0 Human Binding pKi = 7.3 7.3 45 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 503 6 1 8 2.0 COc1ccccc1N1CCN(C(=O)COc2ccc(-c3cc4c([nH]3)c(=O)n(C)c(=O)n4C)cc2)CC1 10.1016/j.bmc.2008.01.002
CHEMBL258778 95806 None 0 Human Binding pKi = 7.3 7.3 45 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 503 6 1 8 2.0 COc1ccccc1N1CCN(C(=O)COc2ccc(-c3cc4c([nH]3)c(=O)n(C)c(=O)n4C)cc2)CC1 10.1016/j.bmc.2008.01.002
44451201 96131 None 0 Human Binding pKi = 7.3 7.3 30 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 619 11 1 7 5.3 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCN(C(c5ccccc5)c5ccccc5)CC4)cc3)cc2n(CCC)c1=O 10.1016/j.bmc.2008.01.002
CHEMBL260434 96131 None 0 Human Binding pKi = 7.3 7.3 30 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 619 11 1 7 5.3 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCN(C(c5ccccc5)c5ccccc5)CC4)cc3)cc2n(CCC)c1=O 10.1016/j.bmc.2008.01.002
168273637 190316 None 0 Human Binding pKi = 7.3 7.3 - 1
Displacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cell membrane preincubated for 4 hrs followed by [3H]PSB-603 addition and measured after 0.5 hrs by radioligand displacement assayDisplacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cell membrane preincubated for 4 hrs followed by [3H]PSB-603 addition and measured after 0.5 hrs by radioligand displacement assay
ChEMBL 410 7 1 8 2.0 CCCn1c(=O)c2[nH]c(-c3ccc(OS(=O)(=O)F)cc3)nc2n(CCC)c1=O 10.1039/d2md00132b
CHEMBL5176227 190316 None 0 Human Binding pKi = 7.3 7.3 - 1
Displacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cell membrane preincubated for 4 hrs followed by [3H]PSB-603 addition and measured after 0.5 hrs by radioligand displacement assayDisplacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cell membrane preincubated for 4 hrs followed by [3H]PSB-603 addition and measured after 0.5 hrs by radioligand displacement assay
ChEMBL 410 7 1 8 2.0 CCCn1c(=O)c2[nH]c(-c3ccc(OS(=O)(=O)F)cc3)nc2n(CCC)c1=O 10.1039/d2md00132b
CHEMBL5079596 214625 None 0 Human Binding pKi = 7.3 7.3 -1 2
Displacement of [3H]DPCPX from human A2BAR expressed in HEK293 cell membrane incubated for 30 mins by microbeta trilux scintillation counter analysisDisplacement of [3H]DPCPX from human A2BAR expressed in HEK293 cell membrane incubated for 30 mins by microbeta trilux scintillation counter analysis
ChEMBL None None None N#Cc1c(-c2ccccc2)nc(Nc2ccccc2)nc1-c1ccc(F)cc1 10.1021/acs.jmedchem.1c01636
14978313 102655 None 0 Human Binding pKi = 6.3 6.3 4 5
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 204 1 1 5 -0.9 C#CCn1c(=O)c2[nH]cnc2n(C)c1=O 10.1021/jm0104318
CHEMBL304455 102655 None 0 Human Binding pKi = 6.3 6.3 4 5
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 204 1 1 5 -0.9 C#CCn1c(=O)c2[nH]cnc2n(C)c1=O 10.1021/jm0104318
165412580 192002 None 4 Human Binding pKi = 6.3 6.3 -50 3
Displacement of [3H]DPCPX from human A2BAR incubated for 60 mins by scintillation counter analysisDisplacement of [3H]DPCPX from human A2BAR incubated for 60 mins by scintillation counter analysis
ChEMBL 450 11 3 9 3.6 Nc1nc(-c2ccco2)c2cnn(Cc3cccc(OCCCCCCC(=O)NO)c3)c2n1 10.1016/j.ejmech.2022.114326
CHEMBL5201523 192002 None 4 Human Binding pKi = 6.3 6.3 -50 3
Displacement of [3H]DPCPX from human A2BAR incubated for 60 mins by scintillation counter analysisDisplacement of [3H]DPCPX from human A2BAR incubated for 60 mins by scintillation counter analysis
ChEMBL 450 11 3 9 3.6 Nc1nc(-c2ccco2)c2cnn(Cc3cccc(OCCCCCCC(=O)NO)c3)c2n1 10.1016/j.ejmech.2022.114326
12351799 189320 None 0 Human Binding pKi = 6.3 6.3 4 2
Displacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cells
ChEMBL 285 1 2 5 1.2 Cc1ccc(-c2[nH]c3c(=O)n(C)c(=O)n(C)c3c2O)cc1 10.1016/j.bmc.2008.09.067
CHEMBL512388 189320 None 0 Human Binding pKi = 6.3 6.3 4 2
Displacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cells
ChEMBL 285 1 2 5 1.2 Cc1ccc(-c2[nH]c3c(=O)n(C)c(=O)n(C)c3c2O)cc1 10.1016/j.bmc.2008.09.067
11313850 111575 None 0 Human Binding pKi = 6.3 6.3 - 1
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 341 5 1 7 2.0 CCCn1c(=O)c2c(nc(-c3ccc(N)cc3)n2C)n(CCC)c1=O 10.1021/jm0309654
CHEMBL32814 111575 None 0 Human Binding pKi = 6.3 6.3 - 1
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 341 5 1 7 2.0 CCCn1c(=O)c2c(nc(-c3ccc(N)cc3)n2C)n(CCC)c1=O 10.1021/jm0309654
156020536 178149 None 0 Human Binding pKi = 6.3 6.3 - 1
Displacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting methodDisplacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting method
ChEMBL 336 3 2 5 3.6 CC1=C(C(=O)OC(C)C)C(c2cc[nH]c2)n2c(nc3ccccc32)N1 10.1021/acs.jmedchem.0c00564
CHEMBL4648862 178149 None 0 Human Binding pKi = 6.3 6.3 - 1
Displacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting methodDisplacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting method
ChEMBL 336 3 2 5 3.6 CC1=C(C(=O)OC(C)C)C(c2cc[nH]c2)n2c(nc3ccccc32)N1 10.1021/acs.jmedchem.0c00564
21958721 64133 None 0 Human Binding pKi = 5.3 5.3 - 1
Binding affinity for adenosine A2b receptor by using as [3H]ZM-241385 (14 nM) radioligand in membranes from HEK-A2B cellsBinding affinity for adenosine A2b receptor by using as [3H]ZM-241385 (14 nM) radioligand in membranes from HEK-A2B cells
ChEMBL 520 9 1 9 4.7 CCCn1c(=O)c2nc(-c3ccc(OCc4nc(-c5ccc(Cl)cc5)no4)cc3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2004.11.044
CHEMBL180832 64133 None 0 Human Binding pKi = 5.3 5.3 - 1
Binding affinity for adenosine A2b receptor by using as [3H]ZM-241385 (14 nM) radioligand in membranes from HEK-A2B cellsBinding affinity for adenosine A2b receptor by using as [3H]ZM-241385 (14 nM) radioligand in membranes from HEK-A2B cells
ChEMBL 520 9 1 9 4.7 CCCn1c(=O)c2nc(-c3ccc(OCc4nc(-c5ccc(Cl)cc5)no4)cc3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2004.11.044
11494318 72256 None 0 Human Binding pKi = 6.3 6.3 -10 3
Binding affinity towards human Adenosine A2b receptor expressed in HEK293 cells using 5 nM [3H]DPCPXBinding affinity towards human Adenosine A2b receptor expressed in HEK293 cells using 5 nM [3H]DPCPX
ChEMBL 215 1 1 7 0.1 Cn1c(-n2nccn2)nc2c(N)nccc21 10.1021/jm058018d
CHEMBL198200 72256 None 0 Human Binding pKi = 6.3 6.3 -10 3
Binding affinity towards human Adenosine A2b receptor expressed in HEK293 cells using 5 nM [3H]DPCPXBinding affinity towards human Adenosine A2b receptor expressed in HEK293 cells using 5 nM [3H]DPCPX
ChEMBL 215 1 1 7 0.1 Cn1c(-n2nccn2)nc2c(N)nccc21 10.1021/jm058018d
2099 3046 None 81 Human Binding pKi = 5.3 5.3 19 3
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 278 5 0 7 0.2 CC(=O)CCCCn1c(=O)c2n(C)cnc2n(c1=O)C 10.1021/jm0104318
4740 3046 None 81 Human Binding pKi = 5.3 5.3 19 3
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 278 5 0 7 0.2 CC(=O)CCCCn1c(=O)c2n(C)cnc2n(c1=O)C 10.1021/jm0104318
4740.0 3046 None 81 Human Binding pKi = 5.3 5.3 19 3
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 278 5 0 7 0.2 CC(=O)CCCCn1c(=O)c2n(C)cnc2n(c1=O)C 10.1021/jm0104318
7095 3046 None 81 Human Binding pKi = 5.3 5.3 19 3
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 278 5 0 7 0.2 CC(=O)CCCCn1c(=O)c2n(C)cnc2n(c1=O)C 10.1021/jm0104318
CHEMBL628 3046 None 81 Human Binding pKi = 5.3 5.3 19 3
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 278 5 0 7 0.2 CC(=O)CCCCn1c(=O)c2n(C)cnc2n(c1=O)C 10.1021/jm0104318
DB00806 3046 None 81 Human Binding pKi = 5.3 5.3 19 3
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 278 5 0 7 0.2 CC(=O)CCCCn1c(=O)c2n(C)cnc2n(c1=O)C 10.1021/jm0104318
10928649 58146 None 0 Human Binding pKi = 7.3 7.3 -3 4
Displacement of [3H]DPCPX binding at human Adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX binding at human Adenosine A2B receptor expressed in HEK293 cells
ChEMBL 461 7 2 10 4.1 CCCCn1cc2c(nc(NC(=O)Nc3ccc([N+](=O)[O-])cc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm0109614
CHEMBL167915 58146 None 0 Human Binding pKi = 7.3 7.3 -3 4
Displacement of [3H]DPCPX binding at human Adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX binding at human Adenosine A2B receptor expressed in HEK293 cells
ChEMBL 461 7 2 10 4.1 CCCCn1cc2c(nc(NC(=O)Nc3ccc([N+](=O)[O-])cc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm0109614
155560449 175083 None 0 Human Binding pKi = 7.3 7.3 - 1
Displacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assayDisplacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assay
ChEMBL 391 3 1 6 4.4 CC1=C(C(=O)OC(C)C(F)(F)F)C(c2ccoc2)n2c(nc3ccccc32)N1 10.1021/acs.jmedchem.9b01340
CHEMBL4568571 175083 None 0 Human Binding pKi = 7.3 7.3 - 1
Displacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assayDisplacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assay
ChEMBL 391 3 1 6 4.4 CC1=C(C(=O)OC(C)C(F)(F)F)C(c2ccoc2)n2c(nc3ccccc32)N1 10.1021/acs.jmedchem.9b01340
11613517 72728 None 0 Human Binding pKi = 7.3 7.3 1 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 536 10 2 7 4.9 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(C(C)=O)cc4)cc3)c(Cl)c2n(CCC)c1=O 10.1021/jm0506221
CHEMBL199834 72728 None 0 Human Binding pKi = 7.3 7.3 1 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 536 10 2 7 4.9 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(C(C)=O)cc4)cc3)c(Cl)c2n(CCC)c1=O 10.1021/jm0506221
10421804 99746 None 0 Human Binding pKi = 6.3 6.3 -5 4
Inhibition of [3H]ZM-241385 binding to human adenosine A2B receptorInhibition of [3H]ZM-241385 binding to human adenosine A2B receptor
ChEMBL 241 1 2 3 1.2 Cn1c(=O)[nH]c2cc(-c3ccccc3)[nH]c2c1=O 10.1021/jm011049y
CHEMBL284991 99746 None 0 Human Binding pKi = 6.3 6.3 -5 4
Inhibition of [3H]ZM-241385 binding to human adenosine A2B receptorInhibition of [3H]ZM-241385 binding to human adenosine A2B receptor
ChEMBL 241 1 2 3 1.2 Cn1c(=O)[nH]c2cc(-c3ccccc3)[nH]c2c1=O 10.1021/jm011049y
155533281 171832 None 0 Human Binding pKi = 6.3 6.3 - 1
Displacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assayDisplacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assay
ChEMBL 304 3 2 4 2.0 CCOC(=O)C1=C(C(F)(F)F)NC(=O)NC1c1ccoc1 10.1021/acs.jmedchem.9b01340
CHEMBL4468661 171832 None 0 Human Binding pKi = 6.3 6.3 - 1
Displacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assayDisplacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assay
ChEMBL 304 3 2 4 2.0 CCOC(=O)C1=C(C(F)(F)F)NC(=O)NC1c1ccoc1 10.1021/acs.jmedchem.9b01340
168276821 190107 None 0 Human Binding pKi = 6.3 6.3 - 1
Displacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cell membrane preincubated for 4 hrs followed by [3H]PSB-603 addition and measured after 0.5 hrs by radioligand displacement assayDisplacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cell membrane preincubated for 4 hrs followed by [3H]PSB-603 addition and measured after 0.5 hrs by radioligand displacement assay
ChEMBL 410 7 1 8 2.0 CCCn1c(=O)c2[nH]c(-c3cccc(OS(=O)(=O)F)c3)nc2n(CCC)c1=O 10.1039/d2md00132b
CHEMBL5172969 190107 None 0 Human Binding pKi = 6.3 6.3 - 1
Displacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cell membrane preincubated for 4 hrs followed by [3H]PSB-603 addition and measured after 0.5 hrs by radioligand displacement assayDisplacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cell membrane preincubated for 4 hrs followed by [3H]PSB-603 addition and measured after 0.5 hrs by radioligand displacement assay
ChEMBL 410 7 1 8 2.0 CCCn1c(=O)c2[nH]c(-c3cccc(OS(=O)(=O)F)c3)nc2n(CCC)c1=O 10.1039/d2md00132b
52949755 19238 None 0 Human Binding pKi = 5.3 5.3 -1 2
Displacement of [3H]ZM241385 from human adenosine A2B receptor transfected in CHO cells after 60 mins by scintillation countingDisplacement of [3H]ZM241385 from human adenosine A2B receptor transfected in CHO cells after 60 mins by scintillation counting
ChEMBL 468 6 2 5 3.2 Cc1c(S(C)(=O)=O)c(=O)[nH]c2ccc(OCC(=O)NCc3ccc(Cl)c(Cl)c3)cc12 10.1016/j.bmcl.2010.10.030
CHEMBL1290103 19238 None 0 Human Binding pKi = 5.3 5.3 -1 2
Displacement of [3H]ZM241385 from human adenosine A2B receptor transfected in CHO cells after 60 mins by scintillation countingDisplacement of [3H]ZM241385 from human adenosine A2B receptor transfected in CHO cells after 60 mins by scintillation counting
ChEMBL 468 6 2 5 3.2 Cc1c(S(C)(=O)=O)c(=O)[nH]c2ccc(OCC(=O)NCc3ccc(Cl)c(Cl)c3)cc12 10.1016/j.bmcl.2010.10.030
21958676 63909 None 0 Human Binding pKi = 6.3 6.3 1 2
Binding affinity for adenosine A2b receptor by using as [3H]ZM-241385 (14 nM) radioligand in membranes from HEK-A2B cellsBinding affinity for adenosine A2b receptor by using as [3H]ZM-241385 (14 nM) radioligand in membranes from HEK-A2B cells
ChEMBL 500 9 1 9 4.3 CCCn1c(=O)c2nc(-c3ccc(OCc4nc(-c5ccc(C)cc5)no4)cc3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2004.11.044
CHEMBL180559 63909 None 0 Human Binding pKi = 6.3 6.3 1 2
Binding affinity for adenosine A2b receptor by using as [3H]ZM-241385 (14 nM) radioligand in membranes from HEK-A2B cellsBinding affinity for adenosine A2b receptor by using as [3H]ZM-241385 (14 nM) radioligand in membranes from HEK-A2B cells
ChEMBL 500 9 1 9 4.3 CCCn1c(=O)c2nc(-c3ccc(OCc4nc(-c5ccc(C)cc5)no4)cc3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2004.11.044
135529372 110111 None 0 Human Binding pKi = 7.3 7.3 - 1
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 482 10 2 10 2.4 CCCn1c(=O)c2nc(-c3cc(OCC(=O)Nc4ccc(OC)cc4)no3)[nH]c2n(CCC)c1=O 10.1021/jm0309654
CHEMBL32359 110111 None 0 Human Binding pKi = 7.3 7.3 - 1
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 482 10 2 10 2.4 CCCn1c(=O)c2nc(-c3cc(OCC(=O)Nc4ccc(OC)cc4)no3)[nH]c2n(CCC)c1=O 10.1021/jm0309654
10637742 58952 None 0 Human Binding pKi = 7.3 7.3 -33 6
Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 40-69Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 40-69
ChEMBL 297 4 1 8 2.1 CCCCn1cc2c(nc(N)n3nc(-c4ccco4)nc23)n1 10.1021/jm001047y
CHEMBL16894 58952 None 0 Human Binding pKi = 7.3 7.3 -33 6
Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 40-69Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 40-69
ChEMBL 297 4 1 8 2.1 CCCCn1cc2c(nc(N)n3nc(-c4ccco4)nc23)n1 10.1021/jm001047y
10939224 57536 None 0 Human Binding pKi = 7.3 7.3 -173 4
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 40-69Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 40-69
ChEMBL 446 5 2 10 3.5 CCCn1cc2c(nc(NC(=O)Nc3ccc4c(c3)OCO4)n3nc(-c4ccco4)nc23)n1 10.1021/jm0109614
CHEMBL166301 57536 None 0 Human Binding pKi = 7.3 7.3 -173 4
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 40-69Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 40-69
ChEMBL 446 5 2 10 3.5 CCCn1cc2c(nc(NC(=O)Nc3ccc4c(c3)OCO4)n3nc(-c4ccco4)nc23)n1 10.1021/jm0109614
9902563 188790 None 0 Human Binding pKi = 7.3 7.3 -23 4
Displacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation countingDisplacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation counting
ChEMBL 341 3 1 8 2.4 Cc1csc(-c2nc(N)nc3c2nnn3Cc2ccccc2F)n1 10.1021/jm800961g
CHEMBL505787 188790 None 0 Human Binding pKi = 7.3 7.3 -23 4
Displacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation countingDisplacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation counting
ChEMBL 341 3 1 8 2.4 Cc1csc(-c2nc(N)nc3c2nnn3Cc2ccccc2F)n1 10.1021/jm800961g
3286 3209 None 31 Human Binding pKi = 7.3 7.3 4 9
Antagonist activity at human A2B receptorAntagonist activity at human A2B receptor
ChEMBL 350 4 3 6 0.7 CCCn1c(=O)[nH]c2c(c1=O)nc([nH]2)c1ccc(cc1)S(=O)(=O)O 10.1021/acs.jmedchem.0c01431
5311479 3209 None 31 Human Binding pKi = 7.3 7.3 4 9
Antagonist activity at human A2B receptorAntagonist activity at human A2B receptor
ChEMBL 350 4 3 6 0.7 CCCn1c(=O)[nH]c2c(c1=O)nc([nH]2)c1ccc(cc1)S(=O)(=O)O 10.1021/acs.jmedchem.0c01431
CHEMBL8565 3209 None 31 Human Binding pKi = 7.3 7.3 4 9
Antagonist activity at human A2B receptorAntagonist activity at human A2B receptor
ChEMBL 350 4 3 6 0.7 CCCn1c(=O)[nH]c2c(c1=O)nc([nH]2)c1ccc(cc1)S(=O)(=O)O 10.1021/acs.jmedchem.0c01431
11416002 98488 None 2 Human Binding pKi = 7.3 7.3 40 3
Binding affinity for human adenosine A2B receptor using [3H]ZM-241385 in CHO cell membranesBinding affinity for human adenosine A2B receptor using [3H]ZM-241385 in CHO cell membranes
ChEMBL 322 2 3 6 -0.1 Cn1c(=O)[nH]c2[nH]c(-c3ccc(S(=O)(=O)O)cc3)nc2c1=O 10.1021/jm0310030
CHEMBL275987 98488 None 2 Human Binding pKi = 7.3 7.3 40 3
Binding affinity for human adenosine A2B receptor using [3H]ZM-241385 in CHO cell membranesBinding affinity for human adenosine A2B receptor using [3H]ZM-241385 in CHO cell membranes
ChEMBL 322 2 3 6 -0.1 Cn1c(=O)[nH]c2[nH]c(-c3ccc(S(=O)(=O)O)cc3)nc2c1=O 10.1021/jm0310030
3286 3209 None 31 Human Binding pKi = 7.3 7.3 4 9
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 350 4 3 6 0.7 CCCn1c(=O)[nH]c2c(c1=O)nc([nH]2)c1ccc(cc1)S(=O)(=O)O 10.1021/jm900413e
5311479 3209 None 31 Human Binding pKi = 7.3 7.3 4 9
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 350 4 3 6 0.7 CCCn1c(=O)[nH]c2c(c1=O)nc([nH]2)c1ccc(cc1)S(=O)(=O)O 10.1021/jm900413e
CHEMBL8565 3209 None 31 Human Binding pKi = 7.3 7.3 4 9
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 350 4 3 6 0.7 CCCn1c(=O)[nH]c2c(c1=O)nc([nH]2)c1ccc(cc1)S(=O)(=O)O 10.1021/jm900413e
3286 3209 None 31 Human Binding pKi = 7.3 7.3 4 9
Displacement of [125I]IABOPX to human A2B receptor assessed as inhibition constant by fluorescence based assayDisplacement of [125I]IABOPX to human A2B receptor assessed as inhibition constant by fluorescence based assay
ChEMBL 350 4 3 6 0.7 CCCn1c(=O)[nH]c2c(c1=O)nc([nH]2)c1ccc(cc1)S(=O)(=O)O 10.1021/acs.jmedchem.1c00261
5311479 3209 None 31 Human Binding pKi = 7.3 7.3 4 9
Displacement of [125I]IABOPX to human A2B receptor assessed as inhibition constant by fluorescence based assayDisplacement of [125I]IABOPX to human A2B receptor assessed as inhibition constant by fluorescence based assay
ChEMBL 350 4 3 6 0.7 CCCn1c(=O)[nH]c2c(c1=O)nc([nH]2)c1ccc(cc1)S(=O)(=O)O 10.1021/acs.jmedchem.1c00261
CHEMBL8565 3209 None 31 Human Binding pKi = 7.3 7.3 4 9
Displacement of [125I]IABOPX to human A2B receptor assessed as inhibition constant by fluorescence based assayDisplacement of [125I]IABOPX to human A2B receptor assessed as inhibition constant by fluorescence based assay
ChEMBL 350 4 3 6 0.7 CCCn1c(=O)[nH]c2c(c1=O)nc([nH]2)c1ccc(cc1)S(=O)(=O)O 10.1021/acs.jmedchem.1c00261
3286 3209 None 31 Human Binding pKi = 7.3 7.3 4 9
Displacement of [125I]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [125I]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 350 4 3 6 0.7 CCCn1c(=O)[nH]c2c(c1=O)nc([nH]2)c1ccc(cc1)S(=O)(=O)O 10.1021/jm900413e
5311479 3209 None 31 Human Binding pKi = 7.3 7.3 4 9
Displacement of [125I]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [125I]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 350 4 3 6 0.7 CCCn1c(=O)[nH]c2c(c1=O)nc([nH]2)c1ccc(cc1)S(=O)(=O)O 10.1021/jm900413e
CHEMBL8565 3209 None 31 Human Binding pKi = 7.3 7.3 4 9
Displacement of [125I]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [125I]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 350 4 3 6 0.7 CCCn1c(=O)[nH]c2c(c1=O)nc([nH]2)c1ccc(cc1)S(=O)(=O)O 10.1021/jm900413e
3286 3209 None 31 Human Binding pKi = 7.3 7.3 4 9
Displacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 350 4 3 6 0.7 CCCn1c(=O)[nH]c2c(c1=O)nc([nH]2)c1ccc(cc1)S(=O)(=O)O 10.1021/jm060277v
5311479 3209 None 31 Human Binding pKi = 7.3 7.3 4 9
Displacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 350 4 3 6 0.7 CCCn1c(=O)[nH]c2c(c1=O)nc([nH]2)c1ccc(cc1)S(=O)(=O)O 10.1021/jm060277v
CHEMBL8565 3209 None 31 Human Binding pKi = 7.3 7.3 4 9
Displacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 350 4 3 6 0.7 CCCn1c(=O)[nH]c2c(c1=O)nc([nH]2)c1ccc(cc1)S(=O)(=O)O 10.1021/jm060277v
3286 3209 None 31 Human Binding pKi = 7.3 7.3 4 9
Displacement of [3H]ZM241385 from human recombinant Adenosine A2B receptorDisplacement of [3H]ZM241385 from human recombinant Adenosine A2B receptor
ChEMBL 350 4 3 6 0.7 CCCn1c(=O)[nH]c2c(c1=O)nc([nH]2)c1ccc(cc1)S(=O)(=O)O 10.1021/acs.jmedchem.5b01586
5311479 3209 None 31 Human Binding pKi = 7.3 7.3 4 9
Displacement of [3H]ZM241385 from human recombinant Adenosine A2B receptorDisplacement of [3H]ZM241385 from human recombinant Adenosine A2B receptor
ChEMBL 350 4 3 6 0.7 CCCn1c(=O)[nH]c2c(c1=O)nc([nH]2)c1ccc(cc1)S(=O)(=O)O 10.1021/acs.jmedchem.5b01586
CHEMBL8565 3209 None 31 Human Binding pKi = 7.3 7.3 4 9
Displacement of [3H]ZM241385 from human recombinant Adenosine A2B receptorDisplacement of [3H]ZM241385 from human recombinant Adenosine A2B receptor
ChEMBL 350 4 3 6 0.7 CCCn1c(=O)[nH]c2c(c1=O)nc([nH]2)c1ccc(cc1)S(=O)(=O)O 10.1021/acs.jmedchem.5b01586
3286 3209 None 31 Human Binding pKi = 7.3 7.3 4 9
Displacement of [3H]ZM241385 from human recombinant adenosine A2B receptorDisplacement of [3H]ZM241385 from human recombinant adenosine A2B receptor
ChEMBL 350 4 3 6 0.7 CCCn1c(=O)[nH]c2c(c1=O)nc([nH]2)c1ccc(cc1)S(=O)(=O)O 10.1021/acs.jmedchem.7b00138
5311479 3209 None 31 Human Binding pKi = 7.3 7.3 4 9
Displacement of [3H]ZM241385 from human recombinant adenosine A2B receptorDisplacement of [3H]ZM241385 from human recombinant adenosine A2B receptor
ChEMBL 350 4 3 6 0.7 CCCn1c(=O)[nH]c2c(c1=O)nc([nH]2)c1ccc(cc1)S(=O)(=O)O 10.1021/acs.jmedchem.7b00138
CHEMBL8565 3209 None 31 Human Binding pKi = 7.3 7.3 4 9
Displacement of [3H]ZM241385 from human recombinant adenosine A2B receptorDisplacement of [3H]ZM241385 from human recombinant adenosine A2B receptor
ChEMBL 350 4 3 6 0.7 CCCn1c(=O)[nH]c2c(c1=O)nc([nH]2)c1ccc(cc1)S(=O)(=O)O 10.1021/acs.jmedchem.7b00138
3286 3209 None 31 Human Binding pKi = 7.3 7.3 4 9
Displacement of [3H]ZM241385 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 30 mins by scintillation counting methodDisplacement of [3H]ZM241385 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 30 mins by scintillation counting method
ChEMBL 350 4 3 6 0.7 CCCn1c(=O)[nH]c2c(c1=O)nc([nH]2)c1ccc(cc1)S(=O)(=O)O 10.1021/acs.jmedchem.9b00071
5311479 3209 None 31 Human Binding pKi = 7.3 7.3 4 9
Displacement of [3H]ZM241385 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 30 mins by scintillation counting methodDisplacement of [3H]ZM241385 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 30 mins by scintillation counting method
ChEMBL 350 4 3 6 0.7 CCCn1c(=O)[nH]c2c(c1=O)nc([nH]2)c1ccc(cc1)S(=O)(=O)O 10.1021/acs.jmedchem.9b00071
CHEMBL8565 3209 None 31 Human Binding pKi = 7.3 7.3 4 9
Displacement of [3H]ZM241385 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 30 mins by scintillation counting methodDisplacement of [3H]ZM241385 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 30 mins by scintillation counting method
ChEMBL 350 4 3 6 0.7 CCCn1c(=O)[nH]c2c(c1=O)nc([nH]2)c1ccc(cc1)S(=O)(=O)O 10.1021/acs.jmedchem.9b00071
3286 3209 None 31 Human Binding pKi = 7.3 7.3 4 9
Inhibition of [3H]ZM-241385 binding to human adenosine A2B receptorInhibition of [3H]ZM-241385 binding to human adenosine A2B receptor
ChEMBL 350 4 3 6 0.7 CCCn1c(=O)[nH]c2c(c1=O)nc([nH]2)c1ccc(cc1)S(=O)(=O)O 10.1021/jm011049y
5311479 3209 None 31 Human Binding pKi = 7.3 7.3 4 9
Inhibition of [3H]ZM-241385 binding to human adenosine A2B receptorInhibition of [3H]ZM-241385 binding to human adenosine A2B receptor
ChEMBL 350 4 3 6 0.7 CCCn1c(=O)[nH]c2c(c1=O)nc([nH]2)c1ccc(cc1)S(=O)(=O)O 10.1021/jm011049y
CHEMBL8565 3209 None 31 Human Binding pKi = 7.3 7.3 4 9
Inhibition of [3H]ZM-241385 binding to human adenosine A2B receptorInhibition of [3H]ZM-241385 binding to human adenosine A2B receptor
ChEMBL 350 4 3 6 0.7 CCCn1c(=O)[nH]c2c(c1=O)nc([nH]2)c1ccc(cc1)S(=O)(=O)O 10.1021/jm011049y
44451171 96048 None 0 Human Binding pKi = 7.3 7.3 28 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 487 6 1 7 2.0 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCN(Cc5ccccc5)CC4)cc3)cc2n(C)c1=O 10.1016/j.bmc.2008.01.002
CHEMBL259913 96048 None 0 Human Binding pKi = 7.3 7.3 28 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 487 6 1 7 2.0 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCN(Cc5ccccc5)CC4)cc3)cc2n(C)c1=O 10.1016/j.bmc.2008.01.002
11640619 138385 None 0 Human Binding pKi = 7.3 7.3 -9 3
Displacement of [3H]PSB298 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB298 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 433 9 2 6 2.3 CCCN(CCC)S(=O)(=O)c1ccc(-c2nc3c(=O)n(CCC)c(=O)[nH]c3[nH]2)cc1 10.1021/jm060277v
CHEMBL377246 138385 None 0 Human Binding pKi = 7.3 7.3 -9 3
Displacement of [3H]PSB298 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB298 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 433 9 2 6 2.3 CCCN(CCC)S(=O)(=O)c1ccc(-c2nc3c(=O)n(CCC)c(=O)[nH]c3[nH]2)cc1 10.1021/jm060277v
1882 90652 None 66 Rat Binding pKi = 5.3 5.3 -3 5
Inhibition of [125I]-APOBX binding to rat Adenosine A2B receptor expressed in HEK cellsInhibition of [125I]-APOBX binding to rat Adenosine A2B receptor expressed in HEK cells
ChEMBL 242 2 0 6 -0.3 Cn1c(=O)c2c(ncn2CCCl)n(C)c1=O 10.1021/jm0104318
CHEMBL23903 90652 None 66 Rat Binding pKi = 5.3 5.3 -3 5
Inhibition of [125I]-APOBX binding to rat Adenosine A2B receptor expressed in HEK cellsInhibition of [125I]-APOBX binding to rat Adenosine A2B receptor expressed in HEK cells
ChEMBL 242 2 0 6 -0.3 Cn1c(=O)c2c(ncn2CCCl)n(C)c1=O 10.1021/jm0104318
11798195 121692 None 0 Human Binding pKi = 7.3 7.3 1 4
Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 45-64Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 45-64
ChEMBL 460 7 2 9 4.4 COc1ccc(NC(=O)Nc2nc3nn(CCC(C)C)cc3c3nc(-c4ccco4)nn23)cc1 10.1021/jm001047y
CHEMBL358735 121692 None 0 Human Binding pKi = 7.3 7.3 1 4
Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 45-64Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 45-64
ChEMBL 460 7 2 9 4.4 COc1ccc(NC(=O)Nc2nc3nn(CCC(C)C)cc3c3nc(-c4ccco4)nn23)cc1 10.1021/jm001047y
44588395 189784 None 0 Human Binding pKi = 7.3 7.3 -1 4
Displacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cells
ChEMBL 327 5 2 5 2.7 CCCn1c(=O)c2[nH]c(-c3ccccc3)c(O)c2n(CCC)c1=O 10.1016/j.bmc.2008.09.067
CHEMBL516154 189784 None 0 Human Binding pKi = 7.3 7.3 -1 4
Displacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cells
ChEMBL 327 5 2 5 2.7 CCCn1c(=O)c2[nH]c(-c3ccccc3)c(O)c2n(CCC)c1=O 10.1016/j.bmc.2008.09.067
21958758 72884 None 0 Human Binding pKi = 7.3 7.3 48 4
Displacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cellsDisplacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cells
ChEMBL 474 8 1 10 3.0 CCCn1c(=O)c2nc(-c3cnn(Cc4nc(-c5ccc(C)cc5)no4)c3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2005.10.002
CHEMBL200349 72884 None 0 Human Binding pKi = 7.3 7.3 48 4
Displacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cellsDisplacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cells
ChEMBL 474 8 1 10 3.0 CCCn1c(=O)c2nc(-c3cnn(Cc4nc(-c5ccc(C)cc5)no4)c3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2005.10.002
11517635 74948 None 0 Human Binding pKi = 7.3 7.3 18 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 432 6 1 6 2.3 CN(Cc1ccccc1)C(=O)COc1ccc(-c2cc3c([nH]2)c(=O)n(C)c(=O)n3C)cc1 10.1021/jm0506221
CHEMBL203196 74948 None 0 Human Binding pKi = 7.3 7.3 18 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 432 6 1 6 2.3 CN(Cc1ccccc1)C(=O)COc1ccc(-c2cc3c([nH]2)c(=O)n(C)c(=O)n3C)cc1 10.1021/jm0506221
71681055 90207 None 0 Human Binding pKi = 6.3 6.3 - 1
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells after 75 mins by liquid scintillation counting analysisDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells after 75 mins by liquid scintillation counting analysis
ChEMBL 330 5 1 5 3.7 O=C(CCCc1ccccc1)Nc1nc2ccsc2c(=O)s1 10.1021/jm400336x
CHEMBL2382424 90207 None 0 Human Binding pKi = 6.3 6.3 - 1
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells after 75 mins by liquid scintillation counting analysisDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells after 75 mins by liquid scintillation counting analysis
ChEMBL 330 5 1 5 3.7 O=C(CCCc1ccccc1)Nc1nc2ccsc2c(=O)s1 10.1021/jm400336x
46227980 201890 None 0 Human Binding pKi = 6.3 6.3 2 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 368 6 1 7 2.4 C=CCn1c(=O)c2[nH]c(Cc3cccs3)nc2n(Cc2ccco2)c1=O 10.1016/j.bmc.2009.07.034
CHEMBL607371 201890 None 0 Human Binding pKi = 6.3 6.3 2 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 368 6 1 7 2.4 C=CCn1c(=O)c2[nH]c(Cc3cccs3)nc2n(Cc2ccco2)c1=O 10.1016/j.bmc.2009.07.034
135522391 117094 None 0 Human Binding pKi = 7.3 7.3 - 1
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 552 9 1 10 2.0 CCCn1c(=O)c2nc(-c3cc(OCC(=O)N4CCN(c5ccc(F)cc5)CC4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
CHEMBL33930 117094 None 0 Human Binding pKi = 7.3 7.3 - 1
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 552 9 1 10 2.0 CCCn1c(=O)c2nc(-c3cc(OCC(=O)N4CCN(c5ccc(F)cc5)CC4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
135915277 157351 None 0 Human Binding pKi = 7.3 7.3 - 1
Displacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 minsDisplacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 mins
ChEMBL 451 7 1 8 2.9 CCCn1c(=O)c2[nH]c(-c3cc(OCC#Cc4cccc(F)c4)no3)nc2n(CCC)c1=O 10.1016/j.ejmech.2017.04.014
CHEMBL4077765 157351 None 0 Human Binding pKi = 7.3 7.3 - 1
Displacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 minsDisplacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 mins
ChEMBL 451 7 1 8 2.9 CCCn1c(=O)c2[nH]c(-c3cc(OCC#Cc4cccc(F)c4)no3)nc2n(CCC)c1=O 10.1016/j.ejmech.2017.04.014
44406639 72592 None 0 Human Binding pKi = 7.3 7.3 23 3
Displacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cellsDisplacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cells
ChEMBL 528 8 1 10 3.7 CCCn1c(=O)c2nc(-c3cnn(Cc4nc(-c5ccc(C(F)(F)F)cc5)no4)c3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2005.10.002
CHEMBL199309 72592 None 0 Human Binding pKi = 7.3 7.3 23 3
Displacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cellsDisplacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cells
ChEMBL 528 8 1 10 3.7 CCCn1c(=O)c2nc(-c3cnn(Cc4nc(-c5ccc(C(F)(F)F)cc5)no4)c3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2005.10.002
135805568 139128 None 2 Human Binding pKi = 7.3 7.3 - 1
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 minsDisplacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 mins
ChEMBL 288 3 1 7 2.1 CC1=C(C(=O)OC(C)C)C(c2ccco2)n2ncnc2N1 10.1021/acs.jmedchem.5b01586
CHEMBL3786944 139128 None 2 Human Binding pKi = 7.3 7.3 - 1
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 minsDisplacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 mins
ChEMBL 288 3 1 7 2.1 CC1=C(C(=O)OC(C)C)C(c2ccco2)n2ncnc2N1 10.1021/acs.jmedchem.5b01586
11153 2008 None 46 Human Binding pKi = 7.3 7.3 -35 4
Displacement of [3H]DPCPX from human A2BAR expressed in HEK293 cells membrane assessed as inhibition constant preincubated for 5 mins followed by [3H]DPCPX addition and measured after 1.5 hrs by TopCount scintillation counting methodDisplacement of [3H]DPCPX from human A2BAR expressed in HEK293 cells membrane assessed as inhibition constant preincubated for 5 mins followed by [3H]DPCPX addition and measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 315 2 1 5 3.3 Nc1nnc(c(n1)c1ccc(cc1)F)c1cc(C)nc(c1)Cl 10.1021/acs.jmedchem.2c00101
86676119 2008 None 46 Human Binding pKi = 7.3 7.3 -35 4
Displacement of [3H]DPCPX from human A2BAR expressed in HEK293 cells membrane assessed as inhibition constant preincubated for 5 mins followed by [3H]DPCPX addition and measured after 1.5 hrs by TopCount scintillation counting methodDisplacement of [3H]DPCPX from human A2BAR expressed in HEK293 cells membrane assessed as inhibition constant preincubated for 5 mins followed by [3H]DPCPX addition and measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 315 2 1 5 3.3 Nc1nnc(c(n1)c1ccc(cc1)F)c1cc(C)nc(c1)Cl 10.1021/acs.jmedchem.2c00101
CHEMBL4594442 2008 None 46 Human Binding pKi = 7.3 7.3 -35 4
Displacement of [3H]DPCPX from human A2BAR expressed in HEK293 cells membrane assessed as inhibition constant preincubated for 5 mins followed by [3H]DPCPX addition and measured after 1.5 hrs by TopCount scintillation counting methodDisplacement of [3H]DPCPX from human A2BAR expressed in HEK293 cells membrane assessed as inhibition constant preincubated for 5 mins followed by [3H]DPCPX addition and measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 315 2 1 5 3.3 Nc1nnc(c(n1)c1ccc(cc1)F)c1cc(C)nc(c1)Cl 10.1021/acs.jmedchem.2c00101
DB16192 2008 None 46 Human Binding pKi = 7.3 7.3 -35 4
Displacement of [3H]DPCPX from human A2BAR expressed in HEK293 cells membrane assessed as inhibition constant preincubated for 5 mins followed by [3H]DPCPX addition and measured after 1.5 hrs by TopCount scintillation counting methodDisplacement of [3H]DPCPX from human A2BAR expressed in HEK293 cells membrane assessed as inhibition constant preincubated for 5 mins followed by [3H]DPCPX addition and measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 315 2 1 5 3.3 Nc1nnc(c(n1)c1ccc(cc1)F)c1cc(C)nc(c1)Cl 10.1021/acs.jmedchem.2c00101
10219753 203673 None 2 Human Binding pKi = 6.3 6.3 5 3
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 190 1 2 4 -1.0 C#CCn1c(=O)[nH]c2[nH]cnc2c1=O 10.1021/jm0104318
CHEMBL67415 203673 None 2 Human Binding pKi = 6.3 6.3 5 3
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 190 1 2 4 -1.0 C#CCn1c(=O)[nH]c2[nH]cnc2c1=O 10.1021/jm0104318
13525048 98179 None 0 Human Binding pKi = 5.3 5.3 2 3
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 300 2 2 6 0.3 Cn1c(=O)c2nc(-c3cccc(C(=O)O)c3)[nH]c2n(C)c1=O 10.1021/jm0104318
CHEMBL273953 98179 None 0 Human Binding pKi = 5.3 5.3 2 3
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 300 2 2 6 0.3 Cn1c(=O)c2nc(-c3cccc(C(=O)O)c3)[nH]c2n(C)c1=O 10.1021/jm0104318
10869347 203644 None 0 Rat Binding pKi = 5.3 5.3 -8 4
Inhibition of [125I]-APOBX binding to rat Adenosine A2B receptor expressed in HEK cellsInhibition of [125I]-APOBX binding to rat Adenosine A2B receptor expressed in HEK cells
ChEMBL 270 3 1 5 0.7 Cn1c(=O)n(CCc2ccccc2)c(=O)c2[nH]cnc21 10.1021/jm0104318
CHEMBL67228 203644 None 0 Rat Binding pKi = 5.3 5.3 -8 4
Inhibition of [125I]-APOBX binding to rat Adenosine A2B receptor expressed in HEK cellsInhibition of [125I]-APOBX binding to rat Adenosine A2B receptor expressed in HEK cells
ChEMBL 270 3 1 5 0.7 Cn1c(=O)n(CCc2ccccc2)c(=O)c2[nH]cnc21 10.1021/jm0104318
44410403 76009 None 0 Human Binding pKi = 5.3 5.3 -2884 4
Displacement of [125I]ABOPX from human adenosine A2B receptor in HEK cellsDisplacement of [125I]ABOPX from human adenosine A2B receptor in HEK cells
ChEMBL 458 5 5 10 0.1 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC)nc(C#CC4(O)CCCCC4)nc32)[C@H](O)[C@@H]1O 10.1016/j.bmcl.2006.01.110
CHEMBL205531 76009 None 0 Human Binding pKi = 5.3 5.3 -2884 4
Displacement of [125I]ABOPX from human adenosine A2B receptor in HEK cellsDisplacement of [125I]ABOPX from human adenosine A2B receptor in HEK cells
ChEMBL 458 5 5 10 0.1 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC)nc(C#CC4(O)CCCCC4)nc32)[C@H](O)[C@@H]1O 10.1016/j.bmcl.2006.01.110
44390583 64289 None 0 Human Binding pKi = 6.3 6.3 - 1
Binding affinity for adenosine A2b receptor by using as [3H]ZM-241385 (14 nM) radioligand in membranes from HEK-A2B cellsBinding affinity for adenosine A2b receptor by using as [3H]ZM-241385 (14 nM) radioligand in membranes from HEK-A2B cells
ChEMBL 516 10 1 10 4.0 CCCn1c(=O)c2nc(-c3ccc(OCc4nc(-c5ccccc5OC)no4)cc3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2004.11.044
CHEMBL181005 64289 None 0 Human Binding pKi = 6.3 6.3 - 1
Binding affinity for adenosine A2b receptor by using as [3H]ZM-241385 (14 nM) radioligand in membranes from HEK-A2B cellsBinding affinity for adenosine A2b receptor by using as [3H]ZM-241385 (14 nM) radioligand in membranes from HEK-A2B cells
ChEMBL 516 10 1 10 4.0 CCCn1c(=O)c2nc(-c3ccc(OCc4nc(-c5ccccc5OC)no4)cc3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2004.11.044
135529391 481 None 0 Human Binding pKi = 7.3 7.3 - 1
Binding affinity of compound for displacement of [3H]DPCPX binding in HEK293 membranes expressing human A2B adenosine receptorsBinding affinity of compound for displacement of [3H]DPCPX binding in HEK293 membranes expressing human A2B adenosine receptors
ChEMBL 555 10 2 10 1.5 CCCn1c2=N/C(=c\3/cc([nH]n3C)NC(=O)Cc3ccc(cc3)OCc3ccccc3)/N=c2c(=O)n(c1=O)CCC 10.1021/jm0309654
438 481 None 0 Human Binding pKi = 7.3 7.3 - 1
Binding affinity of compound for displacement of [3H]DPCPX binding in HEK293 membranes expressing human A2B adenosine receptorsBinding affinity of compound for displacement of [3H]DPCPX binding in HEK293 membranes expressing human A2B adenosine receptors
ChEMBL 555 10 2 10 1.5 CCCn1c2=N/C(=c\3/cc([nH]n3C)NC(=O)Cc3ccc(cc3)OCc3ccccc3)/N=c2c(=O)n(c1=O)CCC 10.1021/jm0309654
CHEMBL285900 481 None 0 Human Binding pKi = 7.3 7.3 - 1
Binding affinity of compound for displacement of [3H]DPCPX binding in HEK293 membranes expressing human A2B adenosine receptorsBinding affinity of compound for displacement of [3H]DPCPX binding in HEK293 membranes expressing human A2B adenosine receptors
ChEMBL 555 10 2 10 1.5 CCCn1c2=N/C(=c\3/cc([nH]n3C)NC(=O)Cc3ccc(cc3)OCc3ccccc3)/N=c2c(=O)n(c1=O)CCC 10.1021/jm0309654
135529391 481 None 0 Human Binding pKi = 7.3 7.3 - 1
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 555 10 2 10 1.5 CCCn1c2=N/C(=c\3/cc([nH]n3C)NC(=O)Cc3ccc(cc3)OCc3ccccc3)/N=c2c(=O)n(c1=O)CCC 10.1021/jm0309654
438 481 None 0 Human Binding pKi = 7.3 7.3 - 1
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 555 10 2 10 1.5 CCCn1c2=N/C(=c\3/cc([nH]n3C)NC(=O)Cc3ccc(cc3)OCc3ccccc3)/N=c2c(=O)n(c1=O)CCC 10.1021/jm0309654
CHEMBL285900 481 None 0 Human Binding pKi = 7.3 7.3 - 1
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 555 10 2 10 1.5 CCCn1c2=N/C(=c\3/cc([nH]n3C)NC(=O)Cc3ccc(cc3)OCc3ccccc3)/N=c2c(=O)n(c1=O)CCC 10.1021/jm0309654
16071780 58022 None 0 Human Binding pKi = 7.3 7.3 15 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 307 4 1 6 2.5 O=C(Nc1cnc(-c2ccncc2)c(-c2ncco2)n1)C1CC1 10.1021/ml100249e
CHEMBL1672624 58022 None 0 Human Binding pKi = 7.3 7.3 15 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 307 4 1 6 2.5 O=C(Nc1cnc(-c2ccncc2)c(-c2ncco2)n1)C1CC1 10.1021/ml100249e
135874431 96256 None 0 Human Binding pKi = 7.3 7.3 - 1
Displacement of [3H]MRE2029F20 from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]MRE2029F20 from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 463 8 2 8 2.8 CCCn1c(=O)c2[nH]c(-c3cc(C)n(CC(=O)Nc4ccc(C)cc4)n3)nc2n(CCC)c1=O 10.1016/j.bmc.2007.11.058
CHEMBL261028 96256 None 0 Human Binding pKi = 7.3 7.3 - 1
Displacement of [3H]MRE2029F20 from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]MRE2029F20 from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 463 8 2 8 2.8 CCCn1c(=O)c2[nH]c(-c3cc(C)n(CC(=O)Nc4ccc(C)cc4)n3)nc2n(CCC)c1=O 10.1016/j.bmc.2007.11.058
1329 1472 None 86 Human Binding pKi = 7.3 7.3 -1288 14
Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cellsDisplacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells
ChEMBL 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 10.1021/jm051268+
386 1472 None 86 Human Binding pKi = 7.3 7.3 -1288 14
Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cellsDisplacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells
ChEMBL 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 10.1021/jm051268+
CHEMBL183 1472 None 86 Human Binding pKi = 7.3 7.3 -1288 14
Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cellsDisplacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells
ChEMBL 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 10.1021/jm051268+
DB12946 1472 None 86 Human Binding pKi = 7.3 7.3 -1288 14
Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cellsDisplacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells
ChEMBL 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 10.1021/jm051268+
11519405 72754 None 0 Human Binding pKi = 7.3 7.3 1 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 532 11 2 8 4.2 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(C(=O)OCC)cc4)cc3)cc2n(CCC)c1=O 10.1021/jm0506221
CHEMBL199898 72754 None 0 Human Binding pKi = 7.3 7.3 1 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 532 11 2 8 4.2 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(C(=O)OCC)cc4)cc3)cc2n(CCC)c1=O 10.1021/jm0506221
18079460 103848 None 0 Human Binding pKi = 7.3 7.3 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 280 3 2 4 2.3 CC1=C(C(=O)OC(C)C)C(c2ccsc2)NC(=O)N1 10.1021/acs.jmedchem.0c01431
CHEMBL3091704 103848 None 0 Human Binding pKi = 7.3 7.3 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 280 3 2 4 2.3 CC1=C(C(=O)OC(C)C)C(c2ccsc2)NC(=O)N1 10.1021/acs.jmedchem.0c01431
18079460 103848 None 0 Human Binding pKi = 7.3 7.3 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by Scatchard plot analysisDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by Scatchard plot analysis
ChEMBL 280 3 2 4 2.3 CC1=C(C(=O)OC(C)C)C(c2ccsc2)NC(=O)N1 10.1021/ml400185v
CHEMBL3091704 103848 None 0 Human Binding pKi = 7.3 7.3 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by Scatchard plot analysisDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by Scatchard plot analysis
ChEMBL 280 3 2 4 2.3 CC1=C(C(=O)OC(C)C)C(c2ccsc2)NC(=O)N1 10.1021/ml400185v
18079460 103848 None 0 Human Binding pKi = 7.3 7.3 - 1
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 minsDisplacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 mins
ChEMBL 280 3 2 4 2.3 CC1=C(C(=O)OC(C)C)C(c2ccsc2)NC(=O)N1 10.1021/acs.jmedchem.5b01586
CHEMBL3091704 103848 None 0 Human Binding pKi = 7.3 7.3 - 1
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 minsDisplacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 mins
ChEMBL 280 3 2 4 2.3 CC1=C(C(=O)OC(C)C)C(c2ccsc2)NC(=O)N1 10.1021/acs.jmedchem.5b01586
18079460 103848 None 0 Human Binding pKi = 7.3 7.3 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes after 30 minsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes after 30 mins
ChEMBL 280 3 2 4 2.3 CC1=C(C(=O)OC(C)C)C(c2ccsc2)NC(=O)N1 10.1021/acs.jmedchem.7b00138
CHEMBL3091704 103848 None 0 Human Binding pKi = 7.3 7.3 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes after 30 minsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes after 30 mins
ChEMBL 280 3 2 4 2.3 CC1=C(C(=O)OC(C)C)C(c2ccsc2)NC(=O)N1 10.1021/acs.jmedchem.7b00138
18079460 103848 None 0 Human Binding pKi = 7.3 7.3 - 1
Displacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assayDisplacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assay
ChEMBL 280 3 2 4 2.3 CC1=C(C(=O)OC(C)C)C(c2ccsc2)NC(=O)N1 10.1021/acs.jmedchem.9b01340
CHEMBL3091704 103848 None 0 Human Binding pKi = 7.3 7.3 - 1
Displacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assayDisplacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assay
ChEMBL 280 3 2 4 2.3 CC1=C(C(=O)OC(C)C)C(c2ccsc2)NC(=O)N1 10.1021/acs.jmedchem.9b01340
162675859 183322 None 0 Human Binding pKi = 6.3 6.3 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 290 4 2 4 2.3 CC1=C(C(=O)OCC2CCC2)C(c2ccco2)NC(=O)N1 10.1021/acs.jmedchem.0c01431
CHEMBL4797364 183322 None 0 Human Binding pKi = 6.3 6.3 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 290 4 2 4 2.3 CC1=C(C(=O)OCC2CCC2)C(c2ccco2)NC(=O)N1 10.1021/acs.jmedchem.0c01431
168276821 190107 None 0 Human Binding pKi = 6.3 6.3 - 1
Displacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cell membrane and measured after 0.5 hrs by radioligand displacement assayDisplacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cell membrane and measured after 0.5 hrs by radioligand displacement assay
ChEMBL 410 7 1 8 2.0 CCCn1c(=O)c2[nH]c(-c3cccc(OS(=O)(=O)F)c3)nc2n(CCC)c1=O 10.1039/d2md00132b
CHEMBL5172969 190107 None 0 Human Binding pKi = 6.3 6.3 - 1
Displacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cell membrane and measured after 0.5 hrs by radioligand displacement assayDisplacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cell membrane and measured after 0.5 hrs by radioligand displacement assay
ChEMBL 410 7 1 8 2.0 CCCn1c(=O)c2[nH]c(-c3cccc(OS(=O)(=O)F)c3)nc2n(CCC)c1=O 10.1039/d2md00132b
76011 203657 None 8 Human Binding pKi = 5.3 5.3 2 3
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 256 3 0 6 0.1 Cn1c(=O)c2c(ncn2CCCCl)n(C)c1=O 10.1021/jm0104318
CHEMBL67323 203657 None 8 Human Binding pKi = 5.3 5.3 2 3
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 256 3 0 6 0.1 Cn1c(=O)c2c(ncn2CCCCl)n(C)c1=O 10.1021/jm0104318
135443324 111440 None 0 Human Binding pKi = 6.3 6.3 - 1
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 393 4 2 8 0.5 Cn1nc(NC(=O)Cc2ccccc2)cc1-c1nc2c(=O)n(C)c(=O)n(C)c2[nH]1 10.1021/jm0309654
CHEMBL32750 111440 None 0 Human Binding pKi = 6.3 6.3 - 1
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 393 4 2 8 0.5 Cn1nc(NC(=O)Cc2ccccc2)cc1-c1nc2c(=O)n(C)c(=O)n(C)c2[nH]1 10.1021/jm0309654
9910926 29331 None 0 Human Binding pKi = 7.2 7.2 -11 5
Displacement of [3H]-DPCPX from Adenosine A2b receptor expressed in CHO cells; range 50-63Displacement of [3H]-DPCPX from Adenosine A2b receptor expressed in CHO cells; range 50-63
ChEMBL 436 5 2 8 4.4 CCCn1cc2c(nc(NC(=O)Nc3cccc(Cl)c3)n3nc(-c4ccco4)nc23)n1 10.1021/jm001047y
CHEMBL138332 29331 None 0 Human Binding pKi = 7.2 7.2 -11 5
Displacement of [3H]-DPCPX from Adenosine A2b receptor expressed in CHO cells; range 50-63Displacement of [3H]-DPCPX from Adenosine A2b receptor expressed in CHO cells; range 50-63
ChEMBL 436 5 2 8 4.4 CCCn1cc2c(nc(NC(=O)Nc3cccc(Cl)c3)n3nc(-c4ccco4)nc23)n1 10.1021/jm001047y
9910926 29331 None 0 Human Binding pKi = 7.2 7.2 -11 5
Displacement of [3H]-DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 50-63Displacement of [3H]-DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 50-63
ChEMBL 436 5 2 8 4.4 CCCn1cc2c(nc(NC(=O)Nc3cccc(Cl)c3)n3nc(-c4ccco4)nc23)n1 10.1021/jm0109614
CHEMBL138332 29331 None 0 Human Binding pKi = 7.2 7.2 -11 5
Displacement of [3H]-DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 50-63Displacement of [3H]-DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 50-63
ChEMBL 436 5 2 8 4.4 CCCn1cc2c(nc(NC(=O)Nc3cccc(Cl)c3)n3nc(-c4ccco4)nc23)n1 10.1021/jm0109614
9869262 104861 None 0 Rat Binding pKi = 7.2 7.2 -9 3
Compound was tested for its binding affinity against Alpha-2 adrenergic receptorCompound was tested for its binding affinity against Alpha-2 adrenergic receptor
ChEMBL 468 11 4 6 4.8 Oc1ccc(C[C@H]2CCCN2CCCCCCN2CCC[C@@H]2Cc2ccc(O)c(O)c2)cc1O 10.1016/0960-894X(95)00413-N
CHEMBL310997 104861 None 0 Rat Binding pKi = 7.2 7.2 -9 3
Compound was tested for its binding affinity against Alpha-2 adrenergic receptorCompound was tested for its binding affinity against Alpha-2 adrenergic receptor
ChEMBL 468 11 4 6 4.8 Oc1ccc(C[C@H]2CCCN2CCCCCCN2CCC[C@@H]2Cc2ccc(O)c(O)c2)cc1O 10.1016/0960-894X(95)00413-N
44451169 96047 None 0 Human Binding pKi = 7.2 7.2 25 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 503 6 1 8 2.0 COc1cc(-c2cc3c([nH]2)c(=O)n(C)c(=O)n3C)ccc1OCC(=O)N1CCN(c2ccccc2)CC1 10.1016/j.bmc.2008.01.002
CHEMBL259912 96047 None 0 Human Binding pKi = 7.2 7.2 25 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 503 6 1 8 2.0 COc1cc(-c2cc3c([nH]2)c(=O)n(C)c(=O)n3C)ccc1OCC(=O)N1CCN(c2ccccc2)CC1 10.1016/j.bmc.2008.01.002
377 2758 None 53 Human Binding pKi = 6.2 6.2 -1479 15
Displacement of [3H]MRS-1754 from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]MRS-1754 from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm900413e
425 2758 None 53 Human Binding pKi = 6.2 6.2 -1479 15
Displacement of [3H]MRS-1754 from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]MRS-1754 from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm900413e
448222 2758 None 53 Human Binding pKi = 6.2 6.2 -1479 15
Displacement of [3H]MRS-1754 from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]MRS-1754 from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm900413e
CHEMBL464859 2758 None 53 Human Binding pKi = 6.2 6.2 -1479 15
Displacement of [3H]MRS-1754 from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]MRS-1754 from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm900413e
155531946 171745 None 0 Human Binding pKi = 6.2 6.2 - 1
Displacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assayDisplacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assay
ChEMBL 320 3 2 4 2.5 CCOC(=O)C1=C(C(F)(F)F)NC(=O)NC1c1ccsc1 10.1021/acs.jmedchem.9b01340
CHEMBL4467283 171745 None 0 Human Binding pKi = 6.2 6.2 - 1
Displacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assayDisplacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assay
ChEMBL 320 3 2 4 2.5 CCOC(=O)C1=C(C(F)(F)F)NC(=O)NC1c1ccsc1 10.1021/acs.jmedchem.9b01340
162643792 181756 None 0 Human Binding pKi = 6.2 6.2 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 290 3 2 4 2.4 CC1=C(C(=O)OC2CCCC2)C(c2ccco2)NC(=O)N1 10.1021/acs.jmedchem.0c01431
CHEMBL4777520 181756 None 0 Human Binding pKi = 6.2 6.2 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 290 3 2 4 2.4 CC1=C(C(=O)OC2CCCC2)C(c2ccco2)NC(=O)N1 10.1021/acs.jmedchem.0c01431
145989810 167193 None 0 Human Binding pKi = 6.2 6.2 -1 4
Displacement of [3H]PSB-602 from human adenosine A2B receptor expressed in CHO cell membranesDisplacement of [3H]PSB-602 from human adenosine A2B receptor expressed in CHO cell membranes
ChEMBL 586 14 1 9 4.1 CCCCn1c(=O)c2c(nc3n2CCCN3CCc2ccc(OCC(=O)NCc3ccccc3)cc2)n(CCCC)c1=O 10.1039/C8MD00070K
CHEMBL4291422 167193 None 0 Human Binding pKi = 6.2 6.2 -1 4
Displacement of [3H]PSB-602 from human adenosine A2B receptor expressed in CHO cell membranesDisplacement of [3H]PSB-602 from human adenosine A2B receptor expressed in CHO cell membranes
ChEMBL 586 14 1 9 4.1 CCCCn1c(=O)c2c(nc3n2CCCN3CCc2ccc(OCC(=O)NCc3ccccc3)cc2)n(CCCC)c1=O 10.1039/C8MD00070K
137637685 155797 None 0 Human Binding pKi = 6.2 6.2 -1 3
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes after 30 minsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes after 30 mins
ChEMBL 408 7 1 6 4.4 COc1cccc(-c2cc(NC(C)=O)nc(-c3cccc(OC)c3OC)c2)c1OC 10.1021/acs.jmedchem.7b00860
CHEMBL4059638 155797 None 0 Human Binding pKi = 6.2 6.2 -1 3
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes after 30 minsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes after 30 mins
ChEMBL 408 7 1 6 4.4 COc1cccc(-c2cc(NC(C)=O)nc(-c3cccc(OC)c3OC)c2)c1OC 10.1021/acs.jmedchem.7b00860
44281738 110645 None 0 Human Binding pKi = 7.2 7.2 20 2
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 476 8 3 7 4.0 CCCn1c(=O)c2nc(-c3ccc(NC(=O)Nc4cccc(OC)c4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm0309654
CHEMBL32581 110645 None 0 Human Binding pKi = 7.2 7.2 20 2
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 476 8 3 7 4.0 CCCn1c(=O)c2nc(-c3ccc(NC(=O)Nc4cccc(OC)c4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm0309654
135493238 116672 None 0 Human Binding pKi = 7.2 7.2 2 2
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 331 5 2 8 0.7 CCCn1c(=O)c2nc(-c3cc(N)n(C)n3)[nH]c2n(CCC)c1=O 10.1021/jm0309654
CHEMBL33709 116672 None 0 Human Binding pKi = 7.2 7.2 2 2
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 331 5 2 8 0.7 CCCn1c(=O)c2nc(-c3cc(N)n(C)n3)[nH]c2n(CCC)c1=O 10.1021/jm0309654
9868763 34558 None 0 Human Binding pKi = 7.2 7.2 5 4
Displacement of [3H]-DPCPX from Adenosine A2b receptor expressed in CHO cells; range 52-65Displacement of [3H]-DPCPX from Adenosine A2b receptor expressed in CHO cells; range 52-65
ChEMBL 458 6 2 9 4.4 COc1ccc(NC(=O)Nc2nc3nn(CC=C(C)C)cc3c3nc(-c4ccco4)nn23)cc1 10.1021/jm001047y
CHEMBL142926 34558 None 0 Human Binding pKi = 7.2 7.2 5 4
Displacement of [3H]-DPCPX from Adenosine A2b receptor expressed in CHO cells; range 52-65Displacement of [3H]-DPCPX from Adenosine A2b receptor expressed in CHO cells; range 52-65
ChEMBL 458 6 2 9 4.4 COc1ccc(NC(=O)Nc2nc3nn(CC=C(C)C)cc3c3nc(-c4ccco4)nn23)cc1 10.1021/jm001047y
11503200 78095 None 0 Human Binding pKi = 7.2 7.2 9 3
Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cellsDisplacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells
ChEMBL 444 7 1 7 3.4 CCCn1c(=O)c2nc(-c3cnn(Cc4cccc(Cl)c4F)c3)[nH]c2n(CCC)c1=O 10.1021/jm051268+
CHEMBL210213 78095 None 0 Human Binding pKi = 7.2 7.2 9 3
Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cellsDisplacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells
ChEMBL 444 7 1 7 3.4 CCCn1c(=O)c2nc(-c3cnn(Cc4cccc(Cl)c4F)c3)[nH]c2n(CCC)c1=O 10.1021/jm051268+
CHEMBL5084903 214938 None 0 Human Binding pKi = 7.2 7.2 -12 5
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells by liquid scintillation counting analysisDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells by liquid scintillation counting analysis
ChEMBL None None None Nc1nc(-c2ccccc2)c2c(n1)-c1cc(OCCCN3CCCCC3)ccc1C2 10.1021/acs.jmedchem.0c00914
44451129 96145 None 0 Human Binding pKi = 7.2 7.2 12 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 474 5 1 8 1.4 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCN(c5ccccn5)CC4)cc3)cc2n(C)c1=O 10.1016/j.bmc.2008.01.002
CHEMBL260495 96145 None 0 Human Binding pKi = 7.2 7.2 12 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 474 5 1 8 1.4 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCN(c5ccccn5)CC4)cc3)cc2n(C)c1=O 10.1016/j.bmc.2008.01.002
CHEMBL5076643 214456 None 0 Human Binding pKi = 7.2 7.2 -2 3
Displacement of [3H] DPCPX from human recombinant A2B adenosine receptor expressed in HEK293 cells incubated for 30 mins by radioligand binding competition assayDisplacement of [3H] DPCPX from human recombinant A2B adenosine receptor expressed in HEK293 cells incubated for 30 mins by radioligand binding competition assay
ChEMBL None None None Cn1cc(-c2cnc(N)nc2-c2ccco2)ccc1=O 10.1021/acsmedchemlett.1c00599
135428645 172703 None 0 Human Binding pKi = 6.2 6.2 -204 5
Displacement of [125I]3-(4-aminobenzyl)-8-phenyloxyacetate-1-propyl-xanthine from human adenosine A2B receptorDisplacement of [125I]3-(4-aminobenzyl)-8-phenyloxyacetate-1-propyl-xanthine from human adenosine A2B receptor
ChEMBL 371 4 2 4 2.9 CCCN1C(=O)N2C[C@@H](CC)N=C2c2[nH]c(C34CCC(O)(CC3)CC4)nc21 10.1021/jm060539t
CHEMBL450341 172703 None 0 Human Binding pKi = 6.2 6.2 -204 5
Displacement of [125I]3-(4-aminobenzyl)-8-phenyloxyacetate-1-propyl-xanthine from human adenosine A2B receptorDisplacement of [125I]3-(4-aminobenzyl)-8-phenyloxyacetate-1-propyl-xanthine from human adenosine A2B receptor
ChEMBL 371 4 2 4 2.9 CCCN1C(=O)N2C[C@@H](CC)N=C2c2[nH]c(C34CCC(O)(CC3)CC4)nc21 10.1021/jm060539t
25027417 64480 None 0 Human Binding pKi = 5.2 5.2 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by liquid scintillation countingDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by liquid scintillation counting
ChEMBL 311 3 2 5 2.8 COc1ccc(NC(=O)c2coc3ccccc3c2=O)cc1O 10.1016/j.ejmech.2012.05.033
CHEMBL1814065 64480 None 0 Human Binding pKi = 5.2 5.2 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by liquid scintillation countingDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by liquid scintillation counting
ChEMBL 311 3 2 5 2.8 COc1ccc(NC(=O)c2coc3ccccc3c2=O)cc1O 10.1016/j.ejmech.2012.05.033
21958720 63488 None 0 Human Binding pKi = 5.2 5.2 - 1
Binding affinity for adenosine A2b receptor by using as [3H]ZM-241385 (14 nM) radioligand in membranes from HEK-A2B cellsBinding affinity for adenosine A2b receptor by using as [3H]ZM-241385 (14 nM) radioligand in membranes from HEK-A2B cells
ChEMBL 520 9 1 9 4.7 CCCn1c(=O)c2nc(-c3ccc(OCc4noc(-c5ccccc5Cl)n4)cc3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2004.11.044
CHEMBL179935 63488 None 0 Human Binding pKi = 5.2 5.2 - 1
Binding affinity for adenosine A2b receptor by using as [3H]ZM-241385 (14 nM) radioligand in membranes from HEK-A2B cellsBinding affinity for adenosine A2b receptor by using as [3H]ZM-241385 (14 nM) radioligand in membranes from HEK-A2B cells
ChEMBL 520 9 1 9 4.7 CCCn1c(=O)c2nc(-c3ccc(OCc4noc(-c5ccccc5Cl)n4)cc3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2004.11.044
613506 54085 None 17 Human Binding pKi = 6.2 6.2 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 250 3 2 4 1.5 CCOC(=O)C1=C(C)NC(=O)NC1c1ccco1 10.1021/acs.jmedchem.0c01431
CHEMBL1606497 54085 None 17 Human Binding pKi = 6.2 6.2 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 250 3 2 4 1.5 CCOC(=O)C1=C(C)NC(=O)NC1c1ccco1 10.1021/acs.jmedchem.0c01431
613506 54085 None 17 Human Binding pKi = 6.2 6.2 - 1
Displacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assayDisplacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assay
ChEMBL 250 3 2 4 1.5 CCOC(=O)C1=C(C)NC(=O)NC1c1ccco1 10.1021/acs.jmedchem.9b01340
CHEMBL1606497 54085 None 17 Human Binding pKi = 6.2 6.2 - 1
Displacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assayDisplacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assay
ChEMBL 250 3 2 4 1.5 CCOC(=O)C1=C(C)NC(=O)NC1c1ccco1 10.1021/acs.jmedchem.9b01340
613506 54085 None 17 Human Binding pKi = 6.2 6.2 - 1
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 minsDisplacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 mins
ChEMBL 250 3 2 4 1.5 CCOC(=O)C1=C(C)NC(=O)NC1c1ccco1 10.1021/acs.jmedchem.5b01586
CHEMBL1606497 54085 None 17 Human Binding pKi = 6.2 6.2 - 1
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 minsDisplacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 mins
ChEMBL 250 3 2 4 1.5 CCOC(=O)C1=C(C)NC(=O)NC1c1ccco1 10.1021/acs.jmedchem.5b01586
613506 54085 None 17 Human Binding pKi = 6.2 6.2 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes after 30 minsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes after 30 mins
ChEMBL 250 3 2 4 1.5 CCOC(=O)C1=C(C)NC(=O)NC1c1ccco1 10.1021/acs.jmedchem.7b00138
CHEMBL1606497 54085 None 17 Human Binding pKi = 6.2 6.2 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes after 30 minsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes after 30 mins
ChEMBL 250 3 2 4 1.5 CCOC(=O)C1=C(C)NC(=O)NC1c1ccco1 10.1021/acs.jmedchem.7b00138
613506 54085 None 17 Human Binding pKi = 6.2 6.2 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by Scatchard plot analysisDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by Scatchard plot analysis
ChEMBL 250 3 2 4 1.5 CCOC(=O)C1=C(C)NC(=O)NC1c1ccco1 10.1021/ml400185v
CHEMBL1606497 54085 None 17 Human Binding pKi = 6.2 6.2 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by Scatchard plot analysisDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by Scatchard plot analysis
ChEMBL 250 3 2 4 1.5 CCOC(=O)C1=C(C)NC(=O)NC1c1ccco1 10.1021/ml400185v
11380878 197754 None 0 Human Binding pKi = 5.2 5.2 -630 4
Binding affinity to adenosine A2B receptorBinding affinity to adenosine A2B receptor
ChEMBL 295 4 2 6 1.6 Nc1nc(C(=O)NCc2cccnc2)cc(-c2ccco2)n1 10.1016/j.bmcl.2009.03.142
CHEMBL571672 197754 None 0 Human Binding pKi = 5.2 5.2 -630 4
Binding affinity to adenosine A2B receptorBinding affinity to adenosine A2B receptor
ChEMBL 295 4 2 6 1.6 Nc1nc(C(=O)NCc2cccnc2)cc(-c2ccco2)n1 10.1016/j.bmcl.2009.03.142
155513258 169725 None 0 Human Binding pKi = 6.2 6.2 - 1
Displacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assayDisplacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assay
ChEMBL 304 3 2 4 2.0 CC1=C(C(=O)OCC(F)(F)F)C(c2ccoc2)NC(=O)N1 10.1021/acs.jmedchem.9b01340
CHEMBL4438396 169725 None 0 Human Binding pKi = 6.2 6.2 - 1
Displacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assayDisplacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assay
ChEMBL 304 3 2 4 2.0 CC1=C(C(=O)OCC(F)(F)F)C(c2ccoc2)NC(=O)N1 10.1021/acs.jmedchem.9b01340
46233380 200681 None 0 Human Binding pKi = 6.2 6.2 -3 3
Displacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells by microplate beta scintillation counterDisplacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells by microplate beta scintillation counter
ChEMBL 374 7 1 6 1.7 CCCn1c(=O)c2[nH]c(-c3ccccc3)nc2n(CC[S+]([O-])CC)c1=O 10.1016/j.bmc.2010.01.028
CHEMBL599817 200681 None 0 Human Binding pKi = 6.2 6.2 -3 3
Displacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells by microplate beta scintillation counterDisplacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells by microplate beta scintillation counter
ChEMBL 374 7 1 6 1.7 CCCn1c(=O)c2[nH]c(-c3ccccc3)nc2n(CC[S+]([O-])CC)c1=O 10.1016/j.bmc.2010.01.028
44406930 73032 None 0 Human Binding pKi = 5.2 5.2 -2754 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 572 9 1 7 4.2 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)c4ccc(I)cc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm0506221
CHEMBL201022 73032 None 0 Human Binding pKi = 5.2 5.2 -2754 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 572 9 1 7 4.2 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)c4ccc(I)cc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm0506221
44588396 175439 None 0 Human Binding pKi = 6.2 6.2 -1 2
Displacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cells
ChEMBL 341 5 1 6 3.0 CCCn1c(=O)c2c(cc(-c3ccc(C)cc3)n2O)n(CCC)c1=O 10.1016/j.bmc.2008.09.067
CHEMBL457659 175439 None 0 Human Binding pKi = 6.2 6.2 -1 2
Displacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cells
ChEMBL 341 5 1 6 3.0 CCCn1c(=O)c2c(cc(-c3ccc(C)cc3)n2O)n(CCC)c1=O 10.1016/j.bmc.2008.09.067
135493286 109764 None 0 Human Binding pKi = 7.2 7.2 40 2
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 493 8 3 9 2.8 CCCn1c(=O)c2nc(-c3cc(NC(=O)Nc4ccc(N(C)C)cc4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
CHEMBL32311 109764 None 0 Human Binding pKi = 7.2 7.2 40 2
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 493 8 3 9 2.8 CCCn1c(=O)c2nc(-c3cc(NC(=O)Nc4ccc(N(C)C)cc4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
21874675 178702 None 0 Human Binding pKi = 7.2 7.2 -53 4
Displacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation countingDisplacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation counting
ChEMBL 331 3 2 7 2.6 Nc1nc(-c2ccco2)c2nnn(Cc3ccc4[nH]ccc4c3)c2n1 10.1021/jm800961g
CHEMBL468256 178702 None 0 Human Binding pKi = 7.2 7.2 -53 4
Displacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation countingDisplacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation counting
ChEMBL 331 3 2 7 2.6 Nc1nc(-c2ccco2)c2nnn(Cc3ccc4[nH]ccc4c3)c2n1 10.1021/jm800961g
137658586 159309 None 0 Human Binding pKi = 7.2 7.2 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes after 30 minsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes after 30 mins
ChEMBL 288 3 2 5 1.6 CC1=C(C(=O)OC(C)C)C(c2ccoc2)N/C(=N/C#N)N1 10.1021/acs.jmedchem.7b00138
CHEMBL4099777 159309 None 0 Human Binding pKi = 7.2 7.2 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes after 30 minsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes after 30 mins
ChEMBL 288 3 2 5 1.6 CC1=C(C(=O)OC(C)C)C(c2ccoc2)N/C(=N/C#N)N1 10.1021/acs.jmedchem.7b00138
44308481 204016 None 0 Human Binding pKi = 7.2 7.2 -1 3
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 374 6 3 8 1.8 CCCn1c(=O)c2nc(-c3cc(O)c(OC)c(O)c3)[nH]c2n(CCC)c1=O 10.1021/jm0104318
CHEMBL69701 204016 None 0 Human Binding pKi = 7.2 7.2 -1 3
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 374 6 3 8 1.8 CCCn1c(=O)c2nc(-c3cc(O)c(OC)c(O)c3)[nH]c2n(CCC)c1=O 10.1021/jm0104318
10927361 90868 None 0 Human Binding pKi = 6.2 6.2 1 4
Displacement of [3H]ZM-241385 from human adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]ZM-241385 from human adenosine A2B receptor expressed in CHO cells
ChEMBL 395 7 0 7 2.6 CCCn1c(=O)c2c(nc3n2CCCN3CCc2ccccc2)n(CCC)c1=O 10.1016/j.bmc.2007.07.051
CHEMBL239233 90868 None 0 Human Binding pKi = 6.2 6.2 1 4
Displacement of [3H]ZM-241385 from human adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]ZM-241385 from human adenosine A2B receptor expressed in CHO cells
ChEMBL 395 7 0 7 2.6 CCCn1c(=O)c2c(nc3n2CCCN3CCc2ccccc2)n(CCC)c1=O 10.1016/j.bmc.2007.07.051
21874602 176782 None 0 Human Binding pKi = 6.2 6.2 -54 4
Displacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation countingDisplacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation counting
ChEMBL 377 5 2 8 2.3 CC(C)NC(=O)c1cccc(Cn2nnc3c(-c4ccco4)nc(N)nc32)c1 10.1021/jm800961g
CHEMBL460596 176782 None 0 Human Binding pKi = 6.2 6.2 -54 4
Displacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation countingDisplacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation counting
ChEMBL 377 5 2 8 2.3 CC(C)NC(=O)c1cccc(Cn2nnc3c(-c4ccco4)nc(N)nc32)c1 10.1021/jm800961g
10158974 155506 None 0 Human Binding pKi = 8.2 8.2 -1 3
Antagonist activity at human A2B receptorAntagonist activity at human A2B receptor
ChEMBL 418 5 2 6 2.8 CCCn1c(=O)[nH]c2nc(-c3cnn(Cc4cccc(C(F)(F)F)c4)c3)[nH]c2c1=O 10.1021/acs.jmedchem.0c01431
CHEMBL404168 155506 None 0 Human Binding pKi = 8.2 8.2 -1 3
Antagonist activity at human A2B receptorAntagonist activity at human A2B receptor
ChEMBL 418 5 2 6 2.8 CCCn1c(=O)[nH]c2nc(-c3cnn(Cc4cccc(C(F)(F)F)c4)c3)[nH]c2c1=O 10.1021/acs.jmedchem.0c01431
66892382 159152 None 0 Human Binding pKi = 8.2 8.2 1 3
Displacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting methodDisplacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting method
ChEMBL 559 9 1 9 3.5 CCCn1c(=O)c2[nH]c(-c3cnn(CC4CCN(c5ccc(OC(F)(F)F)cc5)C4=O)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2016.11.007
CHEMBL4098127 159152 None 0 Human Binding pKi = 8.2 8.2 1 3
Displacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting methodDisplacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting method
ChEMBL 559 9 1 9 3.5 CCCn1c(=O)c2[nH]c(-c3cnn(CC4CCN(c5ccc(OC(F)(F)F)cc5)C4=O)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2016.11.007
57429661 159626 None 0 Human Binding pKi = 8.2 8.2 - 1
Displacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting methodDisplacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting method
ChEMBL 543 8 1 8 3.6 CCCn1c(=O)c2[nH]c(-c3cnn(CC4CCN(c5cccc(C(F)(F)F)c5)C4=O)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2016.11.007
CHEMBL4103446 159626 None 0 Human Binding pKi = 8.2 8.2 - 1
Displacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting methodDisplacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting method
ChEMBL 543 8 1 8 3.6 CCCn1c(=O)c2[nH]c(-c3cnn(CC4CCN(c5cccc(C(F)(F)F)c5)C4=O)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2016.11.007
11774068 94564 None 0 Human Binding pKi = 8.2 8.2 - 1
Displacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranesDisplacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranes
ChEMBL 404 4 2 6 2.4 CCn1c(=O)[nH]c2nc(-c3cnn(Cc4cccc(C(F)(F)F)c4)c3)[nH]c2c1=O 10.1016/j.bmcl.2008.01.008
CHEMBL251876 94564 None 0 Human Binding pKi = 8.2 8.2 - 1
Displacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranesDisplacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranes
ChEMBL 404 4 2 6 2.4 CCn1c(=O)[nH]c2nc(-c3cnn(Cc4cccc(C(F)(F)F)c4)c3)[nH]c2c1=O 10.1016/j.bmcl.2008.01.008
21958524 94594 None 0 Human Binding pKi = 8.2 8.2 29 4
Displacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranesDisplacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranes
ChEMBL 362 5 2 6 1.7 O=c1[nH]c2nc(-c3cnn(Cc4ccccc4)c3)[nH]c2c(=O)n1CC1CC1 10.1016/j.bmcl.2008.01.008
CHEMBL252069 94594 None 0 Human Binding pKi = 8.2 8.2 29 4
Displacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranesDisplacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranes
ChEMBL 362 5 2 6 1.7 O=c1[nH]c2nc(-c3cnn(Cc4ccccc4)c3)[nH]c2c(=O)n1CC1CC1 10.1016/j.bmcl.2008.01.008
11953248 5522 None 0 Human Binding pKi = 8.2 8.2 52 3
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 279 2 2 5 2.0 O=c1[nH]c2cc(-c3ccncn3)c(-c3ccco3)nc2[nH]1 10.1016/j.bmcl.2010.01.077
CHEMBL1076563 5522 None 0 Human Binding pKi = 8.2 8.2 52 3
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 279 2 2 5 2.0 O=c1[nH]c2cc(-c3ccncn3)c(-c3ccco3)nc2[nH]1 10.1016/j.bmcl.2010.01.077
16072019 58010 None 0 Human Binding pKi = 8.2 8.2 75 4
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 280 3 1 5 2.8 CC(=O)Nc1cnc(-c2ccncc2)c(-c2ccco2)n1 10.1021/ml100249e
CHEMBL1672612 58010 None 0 Human Binding pKi = 8.2 8.2 75 4
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 280 3 1 5 2.8 CC(=O)Nc1cnc(-c2ccncc2)c(-c2ccco2)n1 10.1021/ml100249e
53322692 58030 None 0 Human Binding pKi = 8.2 8.2 67 3
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 325 4 1 6 2.7 O=C(Nc1cnc(-c2ccncc2F)c(-c2ncco2)n1)C1CC1 10.1021/ml100249e
CHEMBL1672632 58030 None 0 Human Binding pKi = 8.2 8.2 67 3
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 325 4 1 6 2.7 O=C(Nc1cnc(-c2ccncc2F)c(-c2ncco2)n1)C1CC1 10.1021/ml100249e
21958619 95935 None 0 Human Binding pKi = 8.2 8.2 38 4
Displacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 418 4 1 7 2.4 CCn1c(=O)c2[nH]c(-c3cnn(Cc4cccc(C(F)(F)F)c4)c3)nc2n(C)c1=O 10.1021/jm7014815
CHEMBL259342 95935 None 0 Human Binding pKi = 8.2 8.2 38 4
Displacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 418 4 1 7 2.4 CCn1c(=O)c2[nH]c(-c3cnn(Cc4cccc(C(F)(F)F)c4)c3)nc2n(C)c1=O 10.1021/jm7014815
11508923 96144 None 0 Human Binding pKi = 8.2 8.2 38 4
Displacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 368 4 1 7 1.5 CCn1c(=O)c2[nH]c(-c3cnn(Cc4cccc(F)c4)c3)nc2n(C)c1=O 10.1021/jm7014815
CHEMBL260490 96144 None 0 Human Binding pKi = 8.2 8.2 38 4
Displacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 368 4 1 7 1.5 CCn1c(=O)c2[nH]c(-c3cnn(Cc4cccc(F)c4)c3)nc2n(C)c1=O 10.1021/jm7014815
49797906 10744 None 0 Human Binding pKi = 8.2 8.2 -1 3
Displacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cells after 1 hr by scintillation countingDisplacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 467 7 1 7 4.3 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3cnn(Cc4cccc(F)c4)c3)sc12 10.1016/j.bmcl.2010.05.056
CHEMBL1171165 10744 None 0 Human Binding pKi = 8.2 8.2 -1 3
Displacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cells after 1 hr by scintillation countingDisplacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 467 7 1 7 4.3 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3cnn(Cc4cccc(F)c4)c3)sc12 10.1016/j.bmcl.2010.05.056
21874647 176914 None 0 Human Binding pKi = 8.2 8.2 -2 4
Displacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation countingDisplacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation counting
ChEMBL 324 3 1 7 2.6 Cc1ccc(-c2nc(N)nc3c2nnn3Cc2ccccc2F)o1 10.1021/jm800961g
CHEMBL461857 176914 None 0 Human Binding pKi = 8.2 8.2 -2 4
Displacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation countingDisplacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation counting
ChEMBL 324 3 1 7 2.6 Cc1ccc(-c2nc(N)nc3c2nnn3Cc2ccccc2F)o1 10.1021/jm800961g
135418454 16527 None 0 Human Binding pKi = 8.2 8.2 -7 4
Inhibition of [3H]DPCPX binding to human Adenosine A2B receptor expressed in HEK cells at 10000 nMInhibition of [3H]DPCPX binding to human Adenosine A2B receptor expressed in HEK cells at 10000 nM
ChEMBL 360 4 1 5 4.0 CCCCc1nc2[nH]cnc2c2nc(-c3ccc(C(F)(F)F)cc3)nn12 10.1021/jm010570p
CHEMBL123705 16527 None 0 Human Binding pKi = 8.2 8.2 -7 4
Inhibition of [3H]DPCPX binding to human Adenosine A2B receptor expressed in HEK cells at 10000 nMInhibition of [3H]DPCPX binding to human Adenosine A2B receptor expressed in HEK cells at 10000 nM
ChEMBL 360 4 1 5 4.0 CCCCc1nc2[nH]cnc2c2nc(-c3ccc(C(F)(F)F)cc3)nn12 10.1021/jm010570p
11555968 73387 None 0 Human Binding pKi = 8.2 8.2 5 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 566 10 2 6 5.5 CCCn1c(=O)c2[nH]c(-c3ccc(OC(CC)C(=O)Nc4ccc(Br)cc4)cc3)cc2n(CCC)c1=O 10.1021/jm0506221
CHEMBL201493 73387 None 0 Human Binding pKi = 8.2 8.2 5 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 566 10 2 6 5.5 CCCn1c(=O)c2[nH]c(-c3ccc(OC(CC)C(=O)Nc4ccc(Br)cc4)cc3)cc2n(CCC)c1=O 10.1021/jm0506221
44451074 158809 None 0 Human Binding pKi = 8.2 8.2 79 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 535 7 1 7 3.5 CCCn1c(=O)n(C)c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCN(c5cccc(Cl)c5)CC4)cc3)cc21 10.1016/j.bmc.2008.01.002
CHEMBL409443 158809 None 0 Human Binding pKi = 8.2 8.2 79 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 535 7 1 7 3.5 CCCn1c(=O)n(C)c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCN(c5cccc(Cl)c5)CC4)cc3)cc21 10.1016/j.bmc.2008.01.002
155518147 170255 None 0 Human Binding pKi = 8.2 8.2 27 2
Displacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 554 9 3 9 1.4 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(c5ccc(OCCO)cc5)CC4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
CHEMBL4445941 170255 None 0 Human Binding pKi = 8.2 8.2 27 2
Displacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 554 9 3 9 1.4 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(c5ccc(OCCO)cc5)CC4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
11730776 139390 None 0 Human Binding pKi = 8.2 8.2 3 3
Inhibition of [3H]ZM-241385 binding to human adenosine A2B receptorInhibition of [3H]ZM-241385 binding to human adenosine A2B receptor
ChEMBL 498 8 2 8 1.6 CCCCn1c(=O)[nH]c2[nH]c(-c3ccc(OCC(=O)N4CCN(C(=O)OCC)CC4)cc3)nc2c1=O 10.1021/jm011049y
CHEMBL37933 139390 None 0 Human Binding pKi = 8.2 8.2 3 3
Inhibition of [3H]ZM-241385 binding to human adenosine A2B receptorInhibition of [3H]ZM-241385 binding to human adenosine A2B receptor
ChEMBL 498 8 2 8 1.6 CCCCn1c(=O)[nH]c2[nH]c(-c3ccc(OCC(=O)N4CCN(C(=O)OCC)CC4)cc3)nc2c1=O 10.1021/jm011049y
44450979 95889 None 0 Human Binding pKi = 8.2 8.2 66 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 530 8 1 7 3.9 CCCn1c(=O)n(C)c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCC(c5ccccc5OC)CC4)cc3)cc21 10.1016/j.bmc.2008.01.002
CHEMBL259151 95889 None 0 Human Binding pKi = 8.2 8.2 66 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 530 8 1 7 3.9 CCCn1c(=O)n(C)c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCC(c5ccccc5OC)CC4)cc3)cc21 10.1016/j.bmc.2008.01.002
44450983 158881 None 0 Human Binding pKi = 8.2 8.2 6 3
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 543 10 1 7 3.7 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCN(Cc5ccccc5)CC4)cc3)cc2n(CCC)c1=O 10.1016/j.bmc.2008.01.002
CHEMBL409514 158881 None 0 Human Binding pKi = 8.2 8.2 6 3
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 543 10 1 7 3.7 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCN(Cc5ccccc5)CC4)cc3)cc2n(CCC)c1=O 10.1016/j.bmc.2008.01.002
44450983 158881 None 0 Human Binding pKi = 8.2 8.2 6 3
Displacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cells
ChEMBL 543 10 1 7 3.7 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCN(Cc5ccccc5)CC4)cc3)cc2n(CCC)c1=O 10.1016/j.bmc.2008.09.067
CHEMBL409514 158881 None 0 Human Binding pKi = 8.2 8.2 6 3
Displacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cells
ChEMBL 543 10 1 7 3.7 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCN(Cc5ccccc5)CC4)cc3)cc2n(CCC)c1=O 10.1016/j.bmc.2008.09.067
44236505 159639 None 0 Human Binding pKi = 8.2 8.2 - 1
Displacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 minsDisplacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 mins
ChEMBL 446 7 1 8 2.6 CCCn1c(=O)c2[nH]c(-c3cnn(CC#Cc4cccc(OC)c4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2017.04.014
CHEMBL4103585 159639 None 0 Human Binding pKi = 8.2 8.2 - 1
Displacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 minsDisplacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 mins
ChEMBL 446 7 1 8 2.6 CCCn1c(=O)c2[nH]c(-c3cnn(CC#Cc4cccc(OC)c4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2017.04.014
7052992 183327 None 2 Human Binding pKi = 8.2 8.2 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 280 3 2 4 2.0 CC1=C(C(=O)OC(C)C)[C@@H](c2ccco2)NC(=S)N1 10.1021/acs.jmedchem.0c01431
CHEMBL4797393 183327 None 2 Human Binding pKi = 8.2 8.2 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 280 3 2 4 2.0 CC1=C(C(=O)OC(C)C)[C@@H](c2ccco2)NC(=S)N1 10.1021/acs.jmedchem.0c01431
44451284 96464 None 0 Human Binding pKi = 8.2 8.2 56 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 507 5 1 7 2.6 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCN(c5ccccc5Cl)CC4)cc3)cc2n(C)c1=O 10.1016/j.bmc.2008.01.002
CHEMBL262333 96464 None 0 Human Binding pKi = 8.2 8.2 56 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 507 5 1 7 2.6 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCN(c5ccccc5Cl)CC4)cc3)cc2n(C)c1=O 10.1016/j.bmc.2008.01.002
44451272 159586 None 0 Human Binding pKi = 8.2 8.2 56 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 498 5 1 8 1.8 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCN(c5ccc(C#N)cc5)CC4)cc3)cc2n(C)c1=O 10.1016/j.bmc.2008.01.002
CHEMBL410297 159586 None 0 Human Binding pKi = 8.2 8.2 56 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 498 5 1 8 1.8 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCN(c5ccc(C#N)cc5)CC4)cc3)cc2n(C)c1=O 10.1016/j.bmc.2008.01.002
44224278 156370 None 0 Human Binding pKi = 8.2 8.2 - 1
Displacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 minsDisplacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 mins
ChEMBL 430 6 1 7 2.9 CCCn1c(=O)c2[nH]c(-c3cnn(CC#Cc4ccc(C)cc4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2017.04.014
CHEMBL4066128 156370 None 0 Human Binding pKi = 8.2 8.2 - 1
Displacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 minsDisplacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 mins
ChEMBL 430 6 1 7 2.9 CCCn1c(=O)c2[nH]c(-c3cnn(CC#Cc4ccc(C)cc4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2017.04.014
66893874 159308 None 0 Human Binding pKi = 8.2 8.2 - 1
Displacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting methodDisplacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting method
ChEMBL 543 8 1 8 3.6 CCCn1c(=O)c2[nH]c(-c3cnn(CC4CC(=O)N(c5cccc(C(F)(F)F)c5)C4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2016.11.007
CHEMBL4099762 159308 None 0 Human Binding pKi = 8.2 8.2 - 1
Displacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting methodDisplacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting method
ChEMBL 543 8 1 8 3.6 CCCn1c(=O)c2[nH]c(-c3cnn(CC4CC(=O)N(c5cccc(C(F)(F)F)c5)C4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2016.11.007
44588516 188913 None 0 Human Binding pKi = 8.2 8.2 4 4
Displacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cells
ChEMBL 405 6 2 7 2.1 CCCn1c(=O)c2[nH]c(-c3ccc(S(C)(=O)=O)cc3)c(O)c2n(CCC)c1=O 10.1016/j.bmc.2008.09.067
CHEMBL507754 188913 None 0 Human Binding pKi = 8.2 8.2 4 4
Displacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cells
ChEMBL 405 6 2 7 2.1 CCCn1c(=O)c2[nH]c(-c3ccc(S(C)(=O)=O)cc3)c(O)c2n(CCC)c1=O 10.1016/j.bmc.2008.09.067
10863622 133411 None 0 Human Binding pKi = 8.2 8.2 4 3
Inhibition of [3H]ZM-241385 binding to human adenosine A2B receptorInhibition of [3H]ZM-241385 binding to human adenosine A2B receptor
ChEMBL 468 7 2 7 1.0 CCCCn1c(=O)[nH]c2[nH]c(-c3ccc(OCC(=O)N4CCN(C(C)=O)CC4)cc3)nc2c1=O 10.1021/jm011049y
CHEMBL37050 133411 None 0 Human Binding pKi = 8.2 8.2 4 3
Inhibition of [3H]ZM-241385 binding to human adenosine A2B receptorInhibition of [3H]ZM-241385 binding to human adenosine A2B receptor
ChEMBL 468 7 2 7 1.0 CCCCn1c(=O)[nH]c2[nH]c(-c3ccc(OCC(=O)N4CCN(C(C)=O)CC4)cc3)nc2c1=O 10.1021/jm011049y
44450933 96039 None 0 Human Binding pKi = 8.2 8.2 36 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 543 9 1 7 4.1 CCCn1c(=O)c2[nH]c(-c3ccc(OC(C)C(=O)N4CCN(c5ccccc5)CC4)cc3)cc2n(CCC)c1=O 10.1016/j.bmc.2008.01.002
CHEMBL259871 96039 None 0 Human Binding pKi = 8.2 8.2 36 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 543 9 1 7 4.1 CCCn1c(=O)c2[nH]c(-c3ccc(OC(C)C(=O)N4CCN(c5ccccc5)CC4)cc3)cc2n(CCC)c1=O 10.1016/j.bmc.2008.01.002
44236659 159672 None 0 Human Binding pKi = 8.2 8.2 - 1
Displacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 minsDisplacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 mins
ChEMBL 434 6 1 7 2.8 CCCn1c(=O)c2[nH]c(-c3cnn(CC#Cc4cccc(F)c4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2017.04.014
CHEMBL4103997 159672 None 0 Human Binding pKi = 8.2 8.2 - 1
Displacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 minsDisplacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 mins
ChEMBL 434 6 1 7 2.8 CCCn1c(=O)c2[nH]c(-c3cnn(CC#Cc4cccc(F)c4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2017.04.014
52945195 19179 None 0 Human Binding pKi = 8.2 8.2 3 3
Displacement of [3H]ZM241385 from human adenosine A2B receptor transfected in CHO cells after 60 mins by scintillation countingDisplacement of [3H]ZM241385 from human adenosine A2B receptor transfected in CHO cells after 60 mins by scintillation counting
ChEMBL 525 10 3 6 4.7 O=C(COc1ccc2[nH]c(=O)c(-c3nccs3)c(CCc3ccccc3)c2c1)N[C@@H](CO)c1ccccc1 10.1016/j.bmcl.2010.10.030
CHEMBL1289676 19179 None 0 Human Binding pKi = 8.2 8.2 3 3
Displacement of [3H]ZM241385 from human adenosine A2B receptor transfected in CHO cells after 60 mins by scintillation countingDisplacement of [3H]ZM241385 from human adenosine A2B receptor transfected in CHO cells after 60 mins by scintillation counting
ChEMBL 525 10 3 6 4.7 O=C(COc1ccc2[nH]c(=O)c(-c3nccs3)c(CCc3ccccc3)c2c1)N[C@@H](CO)c1ccccc1 10.1016/j.bmcl.2010.10.030
11046203 99972 None 3 Human Binding pKi = 8.2 8.2 8 4
Inhibition of [3H]ZM-241385 binding to human adenosine A2B receptorInhibition of [3H]ZM-241385 binding to human adenosine A2B receptor
ChEMBL 344 2 2 4 1.5 C#CCn1c(=O)[nH]c2[nH]c(-c3ccc(Br)cc3)nc2c1=O 10.1021/jm011049y
CHEMBL286527 99972 None 3 Human Binding pKi = 8.2 8.2 8 4
Inhibition of [3H]ZM-241385 binding to human adenosine A2B receptorInhibition of [3H]ZM-241385 binding to human adenosine A2B receptor
ChEMBL 344 2 2 4 1.5 C#CCn1c(=O)[nH]c2[nH]c(-c3ccc(Br)cc3)nc2c1=O 10.1021/jm011049y
155531840 171642 None 0 Human Binding pKi = 8.2 8.2 - 1
Displacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assayDisplacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assay
ChEMBL 391 3 1 6 4.4 CC1=C(C(=O)O[C@H](C)C(F)(F)F)[C@@H](c2ccco2)n2c(nc3ccccc32)N1 10.1021/acs.jmedchem.9b01340
CHEMBL4465889 171642 None 0 Human Binding pKi = 8.2 8.2 - 1
Displacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assayDisplacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assay
ChEMBL 391 3 1 6 4.4 CC1=C(C(=O)O[C@H](C)C(F)(F)F)[C@@H](c2ccco2)n2c(nc3ccccc32)N1 10.1021/acs.jmedchem.9b01340
11533996 73237 None 0 Human Binding pKi = 8.2 8.2 15 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 544 10 2 7 4.9 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(OC(F)(F)F)cc4)cc3)cc2n(CCC)c1=O 10.1021/jm0506221
CHEMBL201239 73237 None 0 Human Binding pKi = 8.2 8.2 15 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 544 10 2 7 4.9 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(OC(F)(F)F)cc4)cc3)cc2n(CCC)c1=O 10.1021/jm0506221
11554182 140569 None 0 Human Binding pKi = 8.2 8.2 11 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 449 6 2 8 2.2 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc([N+](=O)[O-])cc4)cc3)cc2n(C)c1=O 10.1021/jm0506221
CHEMBL381214 140569 None 0 Human Binding pKi = 8.2 8.2 11 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 449 6 2 8 2.2 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc([N+](=O)[O-])cc4)cc3)cc2n(C)c1=O 10.1021/jm0506221
44450932 96038 None 0 Human Binding pKi = 8.2 8.2 5 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 563 9 1 7 4.4 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCN(c5ccccc5Cl)CC4)cc3)cc2n(CCC)c1=O 10.1016/j.bmc.2008.01.002
CHEMBL259870 96038 None 0 Human Binding pKi = 8.2 8.2 5 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 563 9 1 7 4.4 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCN(c5ccccc5Cl)CC4)cc3)cc2n(CCC)c1=O 10.1016/j.bmc.2008.01.002
CHEMBL5074665 214324 None 0 Human Binding pKi = 7.2 7.2 -5 3
Displacement of [3H]DPCPX from human A2BAR expressed in HEK293 cell membrane incubated for 30 mins by microbeta trilux scintillation counter analysisDisplacement of [3H]DPCPX from human A2BAR expressed in HEK293 cell membrane incubated for 30 mins by microbeta trilux scintillation counter analysis
ChEMBL None None None CNc1nc(-c2ccccc2)c(C#N)c(-c2cc(OC)cc(OC)c2)n1 10.1021/acs.jmedchem.1c01636
135874422 159085 None 0 Human Binding pKi = 7.2 7.2 - 1
Displacement of [3H]MRE2029F20 from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]MRE2029F20 from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 509 10 2 10 2.5 CCCn1c(=O)c2[nH]c(-c3cc(C)n(CC(=O)Nc4ccc(OC)c(OC)c4)n3)nc2n(CCC)c1=O 10.1016/j.bmc.2007.11.058
CHEMBL409736 159085 None 0 Human Binding pKi = 7.2 7.2 - 1
Displacement of [3H]MRE2029F20 from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]MRE2029F20 from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 509 10 2 10 2.5 CCCn1c(=O)c2[nH]c(-c3cc(C)n(CC(=O)Nc4ccc(OC)c(OC)c4)n3)nc2n(CCC)c1=O 10.1016/j.bmc.2007.11.058
21916398 95885 None 0 Human Binding pKi = 7.2 7.2 1 4
Displacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 396 5 1 7 2.1 CC(C)Cn1c(=O)c2[nH]c(-c3cnn(Cc4cccc(F)c4)c3)nc2n(C)c1=O 10.1021/jm7014815
CHEMBL259130 95885 None 0 Human Binding pKi = 7.2 7.2 1 4
Displacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 396 5 1 7 2.1 CC(C)Cn1c(=O)c2[nH]c(-c3cnn(Cc4cccc(F)c4)c3)nc2n(C)c1=O 10.1021/jm7014815
443 755 None 10 Human Binding pKi = 7.2 7.2 -3 7
Inhibition of [3H]ZM-241385 binding to human adenosine A2B receptorInhibition of [3H]ZM-241385 binding to human adenosine A2B receptor
ChEMBL 382 7 2 6 2.5 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)/C=C/C(=O)O 10.1021/jm011049y
6439089 755 None 10 Human Binding pKi = 7.2 7.2 -3 7
Inhibition of [3H]ZM-241385 binding to human adenosine A2B receptorInhibition of [3H]ZM-241385 binding to human adenosine A2B receptor
ChEMBL 382 7 2 6 2.5 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)/C=C/C(=O)O 10.1021/jm011049y
CHEMBL16997 755 None 10 Human Binding pKi = 7.2 7.2 -3 7
Inhibition of [3H]ZM-241385 binding to human adenosine A2B receptorInhibition of [3H]ZM-241385 binding to human adenosine A2B receptor
ChEMBL 382 7 2 6 2.5 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)/C=C/C(=O)O 10.1021/jm011049y
11713673 72702 None 0 Human Binding pKi = 7.2 7.2 3 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 546 12 2 8 4.1 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(CC(=O)OCC)cc4)cc3)cc2n(CCC)c1=O 10.1021/jm0506221
CHEMBL199722 72702 None 0 Human Binding pKi = 7.2 7.2 3 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 546 12 2 8 4.1 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(CC(=O)OCC)cc4)cc3)cc2n(CCC)c1=O 10.1021/jm0506221
11634901 73512 None 0 Human Binding pKi = 7.2 7.2 4 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 512 9 2 6 4.8 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4cccc(F)c4)cc3)c(Cl)c2n(CCC)c1=O 10.1021/jm0506221
CHEMBL201679 73512 None 0 Human Binding pKi = 7.2 7.2 4 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 512 9 2 6 4.8 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4cccc(F)c4)cc3)c(Cl)c2n(CCC)c1=O 10.1021/jm0506221
168271107 190069 None 0 Human Binding pKi = 7.2 7.2 - 1
Displacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cell membrane and measured after 0.5 hrs by radioligand displacement assayDisplacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cell membrane and measured after 0.5 hrs by radioligand displacement assay
ChEMBL 394 6 1 7 2.0 CCCn1c(=O)c2[nH]c(-c3ccc(S(=O)(=O)F)cc3)nc2n(CCC)c1=O 10.1039/d2md00132b
CHEMBL5172513 190069 None 0 Human Binding pKi = 7.2 7.2 - 1
Displacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cell membrane and measured after 0.5 hrs by radioligand displacement assayDisplacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cell membrane and measured after 0.5 hrs by radioligand displacement assay
ChEMBL 394 6 1 7 2.0 CCCn1c(=O)c2[nH]c(-c3ccc(S(=O)(=O)F)cc3)nc2n(CCC)c1=O 10.1039/d2md00132b
935972 97534 None 10 Human Binding pKi = 7.2 7.2 -1 3
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 272 1 2 6 0.3 Cn1c(=O)c2nc(-c3ccc(O)cc3)[nH]c2n(C)c1=O 10.1021/jm0104318
CHEMBL27047 97534 None 10 Human Binding pKi = 7.2 7.2 -1 3
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 272 1 2 6 0.3 Cn1c(=O)c2nc(-c3ccc(O)cc3)[nH]c2n(C)c1=O 10.1021/jm0104318
44574224 178592 None 0 Human Binding pKi = 6.2 6.2 3 2
Displacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells by beta scintillation counterDisplacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells by beta scintillation counter
ChEMBL 466 8 2 7 4.8 CCCn1c(=O)c2[nH]c(-c3ccc(COC(=O)Nc4cccs4)cc3)cc2n(CCC)c1=O 10.1016/j.bmc.2009.03.062
CHEMBL467270 178592 None 0 Human Binding pKi = 6.2 6.2 3 2
Displacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells by beta scintillation counterDisplacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells by beta scintillation counter
ChEMBL 466 8 2 7 4.8 CCCn1c(=O)c2[nH]c(-c3ccc(COC(=O)Nc4cccs4)cc3)cc2n(CCC)c1=O 10.1016/j.bmc.2009.03.062
135633267 139147 None 15 Human Binding pKi = 6.2 6.2 - 1
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 minsDisplacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 mins
ChEMBL 274 3 1 7 1.7 CCOC(=O)C1=C(C)Nc2ncnn2C1c1ccoc1 10.1021/acs.jmedchem.5b01586
CHEMBL3787123 139147 None 15 Human Binding pKi = 6.2 6.2 - 1
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 minsDisplacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 mins
ChEMBL 274 3 1 7 1.7 CCOC(=O)C1=C(C)Nc2ncnn2C1c1ccoc1 10.1021/acs.jmedchem.5b01586
2748280 20133 None 32 Human Binding pKi = 6.2 6.2 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 266 3 2 5 2.0 CCOC(=O)C1=C(C)N=C(S)NC1c1ccco1 10.1021/acs.jmedchem.0c01431
CHEMBL1304358 20133 None 32 Human Binding pKi = 6.2 6.2 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 266 3 2 5 2.0 CCOC(=O)C1=C(C)N=C(S)NC1c1ccco1 10.1021/acs.jmedchem.0c01431
2748280 20133 None 32 Human Binding pKi = 6.2 6.2 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by Scatchard plot analysisDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by Scatchard plot analysis
ChEMBL 266 3 2 5 2.0 CCOC(=O)C1=C(C)N=C(S)NC1c1ccco1 10.1021/ml400185v
CHEMBL1304358 20133 None 32 Human Binding pKi = 6.2 6.2 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by Scatchard plot analysisDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by Scatchard plot analysis
ChEMBL 266 3 2 5 2.0 CCOC(=O)C1=C(C)N=C(S)NC1c1ccco1 10.1021/ml400185v
11798368 121925 None 0 Human Binding pKi = 7.2 7.2 1 4
Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 55-68Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 55-68
ChEMBL 464 6 2 8 5.1 CC(C)CCn1cc2c(nc(NC(=O)Nc3cccc(Cl)c3)n3nc(-c4ccco4)nc23)n1 10.1021/jm001047y
CHEMBL359044 121925 None 0 Human Binding pKi = 7.2 7.2 1 4
Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 55-68Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 55-68
ChEMBL 464 6 2 8 5.1 CC(C)CCn1cc2c(nc(NC(=O)Nc3cccc(Cl)c3)n3nc(-c4ccco4)nc23)n1 10.1021/jm001047y
10982985 120002 None 0 Human Binding pKi = 7.2 7.2 -2 4
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 49-77Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 49-77
ChEMBL 436 5 2 8 4.4 CCCn1cc2c(nc(NC(=O)Nc3ccccc3Cl)n3nc(-c4ccco4)nc23)n1 10.1021/jm0109614
CHEMBL350042 120002 None 0 Human Binding pKi = 7.2 7.2 -2 4
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 49-77Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 49-77
ChEMBL 436 5 2 8 4.4 CCCn1cc2c(nc(NC(=O)Nc3ccccc3Cl)n3nc(-c4ccco4)nc23)n1 10.1021/jm0109614
136042337 71163 None 0 Human Binding pKi = 7.2 7.2 - 1
Displacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation countingDisplacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation counting
ChEMBL 520 10 1 12 2.7 CCCn1c(=O)c2[nH]c(-c3cc(OCc4noc(-c5cccc(OC)c5)n4)nn3C)nc2n(CCC)c1=O 10.1021/jm201292w
CHEMBL1955913 71163 None 0 Human Binding pKi = 7.2 7.2 - 1
Displacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation countingDisplacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation counting
ChEMBL 520 10 1 12 2.7 CCCn1c(=O)c2[nH]c(-c3cc(OCc4noc(-c5cccc(OC)c5)n4)nn3C)nc2n(CCC)c1=O 10.1021/jm201292w
155522786 170752 None 0 Human Binding pKi = 7.2 7.2 - 1
Displacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assayDisplacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assay
ChEMBL 318 3 2 4 2.4 CC1=C(C(=O)OC(C)C(F)(F)F)C(c2ccco2)NC(=O)N1 10.1021/acs.jmedchem.9b01340
CHEMBL4452495 170752 None 0 Human Binding pKi = 7.2 7.2 - 1
Displacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assayDisplacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assay
ChEMBL 318 3 2 4 2.4 CC1=C(C(=O)OC(C)C(F)(F)F)C(c2ccco2)NC(=O)N1 10.1021/acs.jmedchem.9b01340
46227959 201728 None 0 Human Binding pKi = 7.2 7.2 2 3
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 394 7 0 8 1.8 COCCn1c(=O)c2c(nc(Cc3ccccc3)n2C)n(Cc2ccco2)c1=O 10.1016/j.bmc.2009.07.034
CHEMBL606535 201728 None 0 Human Binding pKi = 7.2 7.2 2 3
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 394 7 0 8 1.8 COCCn1c(=O)c2c(nc(Cc3ccccc3)n2C)n(Cc2ccco2)c1=O 10.1016/j.bmc.2009.07.034
44417680 82140 None 0 Human Binding pKi = 6.2 6.2 -870 6
Displacement of [125I]3-(4-aminobenzyl)-8-phenyloxyacetate-1-propyl-xanthine from human adenosine A2B receptor expressed in HEK cellsDisplacement of [125I]3-(4-aminobenzyl)-8-phenyloxyacetate-1-propyl-xanthine from human adenosine A2B receptor expressed in HEK cells
ChEMBL 344 5 1 6 1.6 CCCn1c(=O)c2nc([C@H]3CC4C[C@@H]3[C@H]3O[C@@H]43)[nH]c2n(CCC)c1=O 10.1021/jm0605381
CHEMBL216750 82140 None 0 Human Binding pKi = 6.2 6.2 -870 6
Displacement of [125I]3-(4-aminobenzyl)-8-phenyloxyacetate-1-propyl-xanthine from human adenosine A2B receptor expressed in HEK cellsDisplacement of [125I]3-(4-aminobenzyl)-8-phenyloxyacetate-1-propyl-xanthine from human adenosine A2B receptor expressed in HEK cells
ChEMBL 344 5 1 6 1.6 CCCn1c(=O)c2nc([C@H]3CC4C[C@@H]3[C@H]3O[C@@H]43)[nH]c2n(CCC)c1=O 10.1021/jm0605381
168272084 190282 None 0 Human Binding pKi = 6.2 6.2 - 1
Displacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cell membrane and measured after 0.5 hrs by radioligand displacement assayDisplacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cell membrane and measured after 0.5 hrs by radioligand displacement assay
ChEMBL 369 6 1 7 3.1 CCCn1c(=O)c2[nH]c(-c3cccc(N=C=S)c3)nc2n(CCC)c1=O 10.1039/d2md00132b
CHEMBL5175698 190282 None 0 Human Binding pKi = 6.2 6.2 - 1
Displacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cell membrane and measured after 0.5 hrs by radioligand displacement assayDisplacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cell membrane and measured after 0.5 hrs by radioligand displacement assay
ChEMBL 369 6 1 7 3.1 CCCn1c(=O)c2[nH]c(-c3cccc(N=C=S)c3)nc2n(CCC)c1=O 10.1039/d2md00132b
1328 1369 None 35 Human Binding pKi = 7.2 7.2 -7 4
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 284 3 1 5 1.6 CCn1c2nc([nH]c2c(=O)n(c1=O)CC)c1ccccc1 10.1021/jm0104318
445 1369 None 35 Human Binding pKi = 7.2 7.2 -7 4
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 284 3 1 5 1.6 CCn1c2nc([nH]c2c(=O)n(c1=O)CC)c1ccccc1 10.1021/jm0104318
CHEMBL11348 1369 None 35 Human Binding pKi = 7.2 7.2 -7 4
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 284 3 1 5 1.6 CCn1c2nc([nH]c2c(=O)n(c1=O)CC)c1ccccc1 10.1021/jm0104318
57988794 156833 None 0 Human Binding pKi = 7.2 7.2 - 1
Displacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 minsDisplacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 mins
ChEMBL 340 6 1 7 1.2 C#CCn1cc(-c2nc3c([nH]2)c(=O)n(CCC)c(=O)n3CCC)cn1 10.1016/j.ejmech.2017.04.014
CHEMBL4071331 156833 None 0 Human Binding pKi = 7.2 7.2 - 1
Displacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 minsDisplacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 mins
ChEMBL 340 6 1 7 1.2 C#CCn1cc(-c2nc3c([nH]2)c(=O)n(CCC)c(=O)n3CCC)cn1 10.1016/j.ejmech.2017.04.014
24950690 178615 None 0 Human Binding pKi = 6.2 6.2 -9 3
Displacement of [3H]MRS1754 from human adenosine A2B receptor expressed in CHO cell membraneDisplacement of [3H]MRS1754 from human adenosine A2B receptor expressed in CHO cell membrane
ChEMBL 275 2 1 4 3.8 Cc1cccc(-c2cc(-c3ccco3)nc(N)c2C#N)c1 10.1021/jm701594y
CHEMBL467386 178615 None 0 Human Binding pKi = 6.2 6.2 -9 3
Displacement of [3H]MRS1754 from human adenosine A2B receptor expressed in CHO cell membraneDisplacement of [3H]MRS1754 from human adenosine A2B receptor expressed in CHO cell membrane
ChEMBL 275 2 1 4 3.8 Cc1cccc(-c2cc(-c3ccco3)nc(N)c2C#N)c1 10.1021/jm701594y
11352497 122967 None 0 Human Binding pKi = 6.2 6.2 -123 4
Inhibition of [3H]DPCPX binding to human adenosine A2B receptor expressed in HEK293 cellsInhibition of [3H]DPCPX binding to human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 498 8 6 15 -0.9 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(N[C@H](CO)Cc5ccc(O)cc5)nc43)[C@H](O)[C@@H]2O)n1 10.1021/jm031143+
CHEMBL360837 122967 None 0 Human Binding pKi = 6.2 6.2 -123 4
Inhibition of [3H]DPCPX binding to human adenosine A2B receptor expressed in HEK293 cellsInhibition of [3H]DPCPX binding to human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 498 8 6 15 -0.9 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(N[C@H](CO)Cc5ccc(O)cc5)nc43)[C@H](O)[C@@H]2O)n1 10.1021/jm031143+
152034 76545 None 8 Human Binding pKi = 5.2 5.2 -1 2
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 278 5 1 5 1.6 CC(C)CCn1c(=O)c2nc[nH]c2n(CC(C)C)c1=O 10.1021/jm0104318
CHEMBL20613 76545 None 8 Human Binding pKi = 5.2 5.2 -1 2
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 278 5 1 5 1.6 CC(C)CCn1c(=O)c2nc[nH]c2n(CC(C)C)c1=O 10.1021/jm0104318
2732424 22192 None 29 Human Binding pKi = 5.2 5.2 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by Scatchard plot analysisDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by Scatchard plot analysis
ChEMBL 282 3 2 5 2.5 CCOC(=O)C1=C(C)N=C(S)NC1c1cccs1 10.1021/ml400185v
CHEMBL1322729 22192 None 29 Human Binding pKi = 5.2 5.2 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by Scatchard plot analysisDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by Scatchard plot analysis
ChEMBL 282 3 2 5 2.5 CCOC(=O)C1=C(C)N=C(S)NC1c1cccs1 10.1021/ml400185v
16070216 58015 None 0 Human Binding pKi = 7.2 7.2 16 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 360 4 1 5 4.2 O=C(Nc1cnc(-c2ccncc2)c(-c2ccco2)n1)c1ccc(F)cc1 10.1021/ml100249e
CHEMBL1672617 58015 None 0 Human Binding pKi = 7.2 7.2 16 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 360 4 1 5 4.2 O=C(Nc1cnc(-c2ccncc2)c(-c2ccco2)n1)c1ccc(F)cc1 10.1021/ml100249e
44406328 134126 None 0 Human Binding pKi = 7.2 7.2 31 3
Displacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cellsDisplacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cells
ChEMBL 489 9 1 10 3.3 CCCn1c(=O)c2nc(-c3cnn(Cc4cc(-c5ccc(OC)cc5)on4)c3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2005.10.002
CHEMBL371649 134126 None 0 Human Binding pKi = 7.2 7.2 31 3
Displacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cellsDisplacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cells
ChEMBL 489 9 1 10 3.3 CCCn1c(=O)c2nc(-c3cnn(Cc4cc(-c5ccc(OC)cc5)on4)c3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2005.10.002
21874557 3996 None 51 Human Binding pKi = 7.2 7.2 -52 4
Displacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation countingDisplacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation counting
ChEMBL 321 3 2 8 2.0 Nc1nc(c2ccco2)c2c(n1)n(nn2)Cc1ccc(c(c1)C)N 10.1021/jm800961g
5612 3996 None 51 Human Binding pKi = 7.2 7.2 -52 4
Displacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation countingDisplacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation counting
ChEMBL 321 3 2 8 2.0 Nc1nc(c2ccco2)c2c(n1)n(nn2)Cc1ccc(c(c1)C)N 10.1021/jm800961g
CHEMBL447664 3996 None 51 Human Binding pKi = 7.2 7.2 -52 4
Displacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation countingDisplacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation counting
ChEMBL 321 3 2 8 2.0 Nc1nc(c2ccco2)c2c(n1)n(nn2)Cc1ccc(c(c1)C)N 10.1021/jm800961g
DB06625 3996 None 51 Human Binding pKi = 7.2 7.2 -52 4
Displacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation countingDisplacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation counting
ChEMBL 321 3 2 8 2.0 Nc1nc(c2ccco2)c2c(n1)n(nn2)Cc1ccc(c(c1)C)N 10.1021/jm800961g
21874557 3996 None 51 Human Binding pKi = 7.2 7.2 -52 4
Inhibition of human recombinant adenosine receptor A2bInhibition of human recombinant adenosine receptor A2b
ChEMBL 321 3 2 8 2.0 Nc1nc(c2ccco2)c2c(n1)n(nn2)Cc1ccc(c(c1)C)N 10.1021/jm4011669
5612 3996 None 51 Human Binding pKi = 7.2 7.2 -52 4
Inhibition of human recombinant adenosine receptor A2bInhibition of human recombinant adenosine receptor A2b
ChEMBL 321 3 2 8 2.0 Nc1nc(c2ccco2)c2c(n1)n(nn2)Cc1ccc(c(c1)C)N 10.1021/jm4011669
CHEMBL447664 3996 None 51 Human Binding pKi = 7.2 7.2 -52 4
Inhibition of human recombinant adenosine receptor A2bInhibition of human recombinant adenosine receptor A2b
ChEMBL 321 3 2 8 2.0 Nc1nc(c2ccco2)c2c(n1)n(nn2)Cc1ccc(c(c1)C)N 10.1021/jm4011669
DB06625 3996 None 51 Human Binding pKi = 7.2 7.2 -52 4
Inhibition of human recombinant adenosine receptor A2bInhibition of human recombinant adenosine receptor A2b
ChEMBL 321 3 2 8 2.0 Nc1nc(c2ccco2)c2c(n1)n(nn2)Cc1ccc(c(c1)C)N 10.1021/jm4011669
11576751 73033 None 0 Human Binding pKi = 7.2 7.2 7 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 488 10 2 7 3.8 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(C=O)cc4)cc3)cc2n(CCC)c1=O 10.1021/jm0506221
CHEMBL201024 73033 None 0 Human Binding pKi = 7.2 7.2 7 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 488 10 2 7 3.8 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(C=O)cc4)cc3)cc2n(CCC)c1=O 10.1021/jm0506221
1329 1472 None 86 Human Binding pKi = 7.2 7.2 -1288 14
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 10.1021/jm0104318
386 1472 None 86 Human Binding pKi = 7.2 7.2 -1288 14
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 10.1021/jm0104318
CHEMBL183 1472 None 86 Human Binding pKi = 7.2 7.2 -1288 14
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 10.1021/jm0104318
DB12946 1472 None 86 Human Binding pKi = 7.2 7.2 -1288 14
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 10.1021/jm0104318
9901497 190181 None 0 Human Binding pKi = 6.2 6.2 -162 4
Displacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation countingDisplacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation counting
ChEMBL 317 3 1 8 2.0 N#Cc1cccc(Cn2nnc3c(-c4ccco4)nc(N)nc32)c1 10.1021/jm800961g
CHEMBL517417 190181 None 0 Human Binding pKi = 6.2 6.2 -162 4
Displacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation countingDisplacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation counting
ChEMBL 317 3 1 8 2.0 N#Cc1cccc(Cn2nnc3c(-c4ccco4)nc(N)nc32)c1 10.1021/jm800961g
70696536 75448 None 0 Human Binding pKi = 6.2 6.2 -5 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by beta scintillation countingDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by beta scintillation counting
ChEMBL 338 5 3 5 2.6 COc1cccc2cc(C(=O)NCCc3ccc(O)cc3)c(=N)oc12 10.1016/j.ejmech.2012.05.009
CHEMBL2042073 75448 None 0 Human Binding pKi = 6.2 6.2 -5 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by beta scintillation countingDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by beta scintillation counting
ChEMBL 338 5 3 5 2.6 COc1cccc2cc(C(=O)NCCc3ccc(O)cc3)c(=N)oc12 10.1016/j.ejmech.2012.05.009
21874771 178564 None 0 Human Binding pKi = 6.2 6.2 -74 4
Displacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation countingDisplacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation counting
ChEMBL 298 3 1 7 2.6 Nc1nc(-c2ccco2)c2nnn(CC3CCCCC3)c2n1 10.1021/jm800961g
CHEMBL467035 178564 None 0 Human Binding pKi = 6.2 6.2 -74 4
Displacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation countingDisplacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation counting
ChEMBL 298 3 1 7 2.6 Nc1nc(-c2ccco2)c2nnn(CC3CCCCC3)c2n1 10.1021/jm800961g
162673363 182998 None 0 Human Binding pKi = 6.2 6.2 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 280 3 2 4 2.6 CC1=C(C(=O)SC(C)C)C(c2ccoc2)NC(=O)N1 10.1021/acs.jmedchem.0c01431
CHEMBL4793548 182998 None 0 Human Binding pKi = 6.2 6.2 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 280 3 2 4 2.6 CC1=C(C(=O)SC(C)C)C(c2ccoc2)NC(=O)N1 10.1021/acs.jmedchem.0c01431
25027418 64482 None 0 Human Binding pKi = 5.2 5.2 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by liquid scintillation countingDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by liquid scintillation counting
ChEMBL 325 4 1 5 3.1 COc1ccc(NC(=O)c2coc3ccccc3c2=O)cc1OC 10.1016/j.ejmech.2012.05.033
CHEMBL1814067 64482 None 0 Human Binding pKi = 5.2 5.2 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by liquid scintillation countingDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by liquid scintillation counting
ChEMBL 325 4 1 5 3.1 COc1ccc(NC(=O)c2coc3ccccc3c2=O)cc1OC 10.1016/j.ejmech.2012.05.033
67364057 74289 None 0 Human Binding pKi = 7.2 7.2 -15 3
Antagonist activity at human adenosine A2b receptor expressed in HEK293T cells by radioligand competition binding assayAntagonist activity at human adenosine A2b receptor expressed in HEK293T cells by radioligand competition binding assay
ChEMBL 295 2 1 5 2.9 Cc1cc(-c2nnc(N)nc2-c2ccc(F)cc2)cc(C)n1 10.1021/acs.jmedchem.0c00237
CHEMBL2024116 74289 None 0 Human Binding pKi = 7.2 7.2 -15 3
Antagonist activity at human adenosine A2b receptor expressed in HEK293T cells by radioligand competition binding assayAntagonist activity at human adenosine A2b receptor expressed in HEK293T cells by radioligand competition binding assay
ChEMBL 295 2 1 5 2.9 Cc1cc(-c2nnc(N)nc2-c2ccc(F)cc2)cc(C)n1 10.1021/acs.jmedchem.0c00237
CHEMBL5076254 214423 None 0 Human Binding pKi = 7.2 7.2 -3 2
Displacement of [3H]DPCPX from human A2BAR expressed in HEK293 cell membrane incubated for 30 mins by microbeta trilux scintillation counter analysisDisplacement of [3H]DPCPX from human A2BAR expressed in HEK293 cell membrane incubated for 30 mins by microbeta trilux scintillation counter analysis
ChEMBL None None None COc1cc(OC)cc(-c2nc(Nc3ccccc3)nc(-c3ccccc3)c2C#N)c1 10.1021/acs.jmedchem.1c01636
44588517 175159 None 0 Human Binding pKi = 7.2 7.2 3 3
Displacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cells
ChEMBL 377 4 2 7 1.2 CCCn1c(=O)c2[nH]c(-c3ccc(S(C)(=O)=O)cc3)c(O)c2n(C)c1=O 10.1016/j.bmc.2008.09.067
CHEMBL457015 175159 None 0 Human Binding pKi = 7.2 7.2 3 3
Displacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cells
ChEMBL 377 4 2 7 1.2 CCCn1c(=O)c2[nH]c(-c3ccc(S(C)(=O)=O)cc3)c(O)c2n(C)c1=O 10.1016/j.bmc.2008.09.067
22266784 141233 None 0 Human Binding pKi = 7.2 7.2 27 2
Displacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cellsDisplacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cells
ChEMBL 528 8 1 10 3.7 CCCn1c(=O)c2nc(-c3cnn(Cc4noc(-c5cccc(C(F)(F)F)c5)n4)c3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2005.10.002
CHEMBL382929 141233 None 0 Human Binding pKi = 7.2 7.2 27 2
Displacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cellsDisplacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cells
ChEMBL 528 8 1 10 3.7 CCCn1c(=O)c2nc(-c3cnn(Cc4noc(-c5cccc(C(F)(F)F)c5)n4)c3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2005.10.002
11698623 78184 None 0 Human Binding pKi = 6.2 6.2 - 1
Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cellsDisplacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells
ChEMBL 478 7 1 7 3.8 CCCn1c(=O)c2nc(-c3cnn(Cc4ccc(F)c(C(F)(F)F)c4)c3)[nH]c2n(CCC)c1=O 10.1021/jm051268+
CHEMBL210482 78184 None 0 Human Binding pKi = 6.2 6.2 - 1
Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cellsDisplacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells
ChEMBL 478 7 1 7 3.8 CCCn1c(=O)c2nc(-c3cnn(Cc4ccc(F)c(C(F)(F)F)c4)c3)[nH]c2n(CCC)c1=O 10.1021/jm051268+
1676 98984 None 61 Human Binding pKi = 5.2 5.2 -3 10
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 194 2 2 4 -0.2 CCCn1c(=O)[nH]c(=O)c2[nH]cnc21 10.1021/jm900413e
CHEMBL279898 98984 None 61 Human Binding pKi = 5.2 5.2 -3 10
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 194 2 2 4 -0.2 CCCn1c(=O)[nH]c(=O)c2[nH]cnc21 10.1021/jm900413e
155517938 170227 None 0 Human Binding pKi = 6.2 6.2 - 1
Displacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assayDisplacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assay
ChEMBL 334 3 2 4 2.9 CC1=C(C(=O)OC(C)C(F)(F)F)C(c2ccsc2)NC(=O)N1 10.1021/acs.jmedchem.9b01340
CHEMBL4445568 170227 None 0 Human Binding pKi = 6.2 6.2 - 1
Displacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assayDisplacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assay
ChEMBL 334 3 2 4 2.9 CC1=C(C(=O)OC(C)C(F)(F)F)C(c2ccsc2)NC(=O)N1 10.1021/acs.jmedchem.9b01340
9901700 190892 None 0 Human Binding pKi = 6.2 6.2 -354 4
Displacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation countingDisplacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation counting
ChEMBL 322 4 1 8 2.1 COc1cccc(Cn2nnc3c(-c4ccco4)nc(N)nc32)c1 10.1021/jm800961g
CHEMBL518497 190892 None 0 Human Binding pKi = 6.2 6.2 -354 4
Displacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation countingDisplacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation counting
ChEMBL 322 4 1 8 2.1 COc1cccc(Cn2nnc3c(-c4ccco4)nc(N)nc32)c1 10.1021/jm800961g
21958565 64459 None 0 Human Binding pKi = 6.2 6.2 - 1
Binding affinity for adenosine A2b receptor by using as [3H]ZM-241385 (14 nM) radioligand in membranes from HEK-A2B cellsBinding affinity for adenosine A2b receptor by using as [3H]ZM-241385 (14 nM) radioligand in membranes from HEK-A2B cells
ChEMBL 504 9 1 9 4.1 CCCn1c(=O)c2nc(-c3ccc(OCc4noc(-c5ccccc5F)n4)cc3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2004.11.044
CHEMBL181346 64459 None 0 Human Binding pKi = 6.2 6.2 - 1
Binding affinity for adenosine A2b receptor by using as [3H]ZM-241385 (14 nM) radioligand in membranes from HEK-A2B cellsBinding affinity for adenosine A2b receptor by using as [3H]ZM-241385 (14 nM) radioligand in membranes from HEK-A2B cells
ChEMBL 504 9 1 9 4.1 CCCn1c(=O)c2nc(-c3ccc(OCc4noc(-c5ccccc5F)n4)cc3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2004.11.044
46228017 199801 None 0 Human Binding pKi = 6.2 6.2 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 400 8 1 8 2.5 CCSCCn1c(=O)c2[nH]c(Cc3ccco3)nc2n(Cc2ccco2)c1=O 10.1016/j.bmc.2009.07.034
CHEMBL594046 199801 None 0 Human Binding pKi = 6.2 6.2 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 400 8 1 8 2.5 CCSCCn1c(=O)c2[nH]c(Cc3ccco3)nc2n(Cc2ccco2)c1=O 10.1016/j.bmc.2009.07.034
10869347 203644 None 0 Human Binding pKi = 6.2 6.2 8 4
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 270 3 1 5 0.7 Cn1c(=O)n(CCc2ccccc2)c(=O)c2[nH]cnc21 10.1021/jm0104318
CHEMBL67228 203644 None 0 Human Binding pKi = 6.2 6.2 8 4
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 270 3 1 5 0.7 Cn1c(=O)n(CCc2ccccc2)c(=O)c2[nH]cnc21 10.1021/jm0104318
9967620 188977 None 0 Human Binding pKi = 6.2 6.2 -173 4
Displacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation countingDisplacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation counting
ChEMBL 337 4 1 9 2.0 Nc1nc(-c2ccco2)c2nnn(Cc3cccc([N+](=O)[O-])c3)c2n1 10.1021/jm800961g
CHEMBL508451 188977 None 0 Human Binding pKi = 6.2 6.2 -173 4
Displacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation countingDisplacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation counting
ChEMBL 337 4 1 9 2.0 Nc1nc(-c2ccco2)c2nnn(Cc3cccc([N+](=O)[O-])c3)c2n1 10.1021/jm800961g
137656644 159683 None 0 Human Binding pKi = 6.2 6.2 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes after 30 minsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes after 30 mins
ChEMBL 304 3 2 5 2.0 CC1=C(C(=O)OC(C)C)C(c2ccsc2)N/C(=N/C#N)N1 10.1021/acs.jmedchem.7b00138
CHEMBL4104142 159683 None 0 Human Binding pKi = 6.2 6.2 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes after 30 minsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes after 30 mins
ChEMBL 304 3 2 5 2.0 CC1=C(C(=O)OC(C)C)C(c2ccsc2)N/C(=N/C#N)N1 10.1021/acs.jmedchem.7b00138
44281684 110414 None 0 Human Binding pKi = 6.2 6.2 - 1
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 445 8 2 6 3.6 CCCn1c(=O)c2nc(-c3ccc(NC(=O)Cc4ccccc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm0309654
CHEMBL32447 110414 None 0 Human Binding pKi = 6.2 6.2 - 1
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 445 8 2 6 3.6 CCCn1c(=O)c2nc(-c3ccc(NC(=O)Cc4ccccc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm0309654
11091783 84221 None 0 Human Binding pKi = 7.2 7.2 -1 4
Displacement of [3H]- DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]- DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 460 6 2 11 2.6 CCNc1c2c(nc(NC(=O)Cc3ccc4c(c3)OCO4)n3nc(-c4ccco4)nc23)nn1C 10.1021/jm021023m
CHEMBL22085 84221 None 0 Human Binding pKi = 7.2 7.2 -1 4
Displacement of [3H]- DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]- DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 460 6 2 11 2.6 CCNc1c2c(nc(NC(=O)Cc3ccc4c(c3)OCO4)n3nc(-c4ccco4)nc23)nn1C 10.1021/jm021023m
10659581 28805 None 0 Human Binding pKi = 7.2 7.2 -33 6
Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 56-75Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 56-75
ChEMBL 269 2 1 8 1.3 CCn1cc2c(nc(N)n3nc(-c4ccco4)nc23)n1 10.1021/jm001047y
CHEMBL137879 28805 None 0 Human Binding pKi = 7.2 7.2 -33 6
Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 56-75Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 56-75
ChEMBL 269 2 1 8 1.3 CCn1cc2c(nc(N)n3nc(-c4ccco4)nc23)n1 10.1021/jm001047y
135874428 167562 None 0 Human Binding pKi = 7.2 7.2 7 2
Displacement of [3H]MRE2029F20 from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]MRE2029F20 from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 479 9 2 9 2.5 CCCn1c(=O)c2[nH]c(-c3cc(C)n(CC(=O)Nc4cccc(OC)c4)n3)nc2n(CCC)c1=O 10.1016/j.bmc.2007.11.058
CHEMBL430044 167562 None 0 Human Binding pKi = 7.2 7.2 7 2
Displacement of [3H]MRE2029F20 from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]MRE2029F20 from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 479 9 2 9 2.5 CCCn1c(=O)c2[nH]c(-c3cc(C)n(CC(=O)Nc4cccc(OC)c4)n3)nc2n(CCC)c1=O 10.1016/j.bmc.2007.11.058
176407 4148 None 84 Human Binding pKi = 7.2 7.2 -34 6
Displacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting methodDisplacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting method
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1021/acs.jmedchem.0c00564
405 4148 None 84 Human Binding pKi = 7.2 7.2 -34 6
Displacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting methodDisplacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting method
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1021/acs.jmedchem.0c00564
CHEMBL113142 4148 None 84 Human Binding pKi = 7.2 7.2 -34 6
Displacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting methodDisplacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting method
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1021/acs.jmedchem.0c00564
DB08770 4148 None 84 Human Binding pKi = 7.2 7.2 -34 6
Displacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting methodDisplacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting method
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1021/acs.jmedchem.0c00564
176407 4148 None 84 Human Binding pKi = 7.2 7.2 -34 6
Displacement of [3H]DPCPX from human A2BAR expressed in HEK293 cell membrane incubated for 30 mins by microbeta trilux scintillation counter analysisDisplacement of [3H]DPCPX from human A2BAR expressed in HEK293 cell membrane incubated for 30 mins by microbeta trilux scintillation counter analysis
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1021/acs.jmedchem.1c01636
405 4148 None 84 Human Binding pKi = 7.2 7.2 -34 6
Displacement of [3H]DPCPX from human A2BAR expressed in HEK293 cell membrane incubated for 30 mins by microbeta trilux scintillation counter analysisDisplacement of [3H]DPCPX from human A2BAR expressed in HEK293 cell membrane incubated for 30 mins by microbeta trilux scintillation counter analysis
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1021/acs.jmedchem.1c01636
CHEMBL113142 4148 None 84 Human Binding pKi = 7.2 7.2 -34 6
Displacement of [3H]DPCPX from human A2BAR expressed in HEK293 cell membrane incubated for 30 mins by microbeta trilux scintillation counter analysisDisplacement of [3H]DPCPX from human A2BAR expressed in HEK293 cell membrane incubated for 30 mins by microbeta trilux scintillation counter analysis
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1021/acs.jmedchem.1c01636
DB08770 4148 None 84 Human Binding pKi = 7.2 7.2 -34 6
Displacement of [3H]DPCPX from human A2BAR expressed in HEK293 cell membrane incubated for 30 mins by microbeta trilux scintillation counter analysisDisplacement of [3H]DPCPX from human A2BAR expressed in HEK293 cell membrane incubated for 30 mins by microbeta trilux scintillation counter analysis
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1021/acs.jmedchem.1c01636
176407 4148 None 84 Human Binding pKi = 7.2 7.2 -34 6
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 minsDisplacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 mins
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1021/acs.jmedchem.5b01586
405 4148 None 84 Human Binding pKi = 7.2 7.2 -34 6
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 minsDisplacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 mins
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1021/acs.jmedchem.5b01586
CHEMBL113142 4148 None 84 Human Binding pKi = 7.2 7.2 -34 6
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 minsDisplacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 mins
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1021/acs.jmedchem.5b01586
DB08770 4148 None 84 Human Binding pKi = 7.2 7.2 -34 6
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 minsDisplacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 mins
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1021/acs.jmedchem.5b01586
176407 4148 None 84 Human Binding pKi = 7.2 7.2 -34 6
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes after 30 minsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes after 30 mins
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1021/acs.jmedchem.7b00138
405 4148 None 84 Human Binding pKi = 7.2 7.2 -34 6
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes after 30 minsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes after 30 mins
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1021/acs.jmedchem.7b00138
CHEMBL113142 4148 None 84 Human Binding pKi = 7.2 7.2 -34 6
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes after 30 minsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes after 30 mins
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1021/acs.jmedchem.7b00138
DB08770 4148 None 84 Human Binding pKi = 7.2 7.2 -34 6
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes after 30 minsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes after 30 mins
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1021/acs.jmedchem.7b00138
176407 4148 None 84 Human Binding pKi = 7.2 7.2 -34 6
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1021/acs.jmedchem.0c01431
405 4148 None 84 Human Binding pKi = 7.2 7.2 -34 6
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1021/acs.jmedchem.0c01431
CHEMBL113142 4148 None 84 Human Binding pKi = 7.2 7.2 -34 6
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1021/acs.jmedchem.0c01431
DB08770 4148 None 84 Human Binding pKi = 7.2 7.2 -34 6
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1021/acs.jmedchem.0c01431
176407 4148 None 84 Human Binding pKi = 7.2 7.2 -34 6
Displacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assayDisplacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assay
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1021/acs.jmedchem.9b01340
405 4148 None 84 Human Binding pKi = 7.2 7.2 -34 6
Displacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assayDisplacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assay
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1021/acs.jmedchem.9b01340
CHEMBL113142 4148 None 84 Human Binding pKi = 7.2 7.2 -34 6
Displacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assayDisplacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assay
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1021/acs.jmedchem.9b01340
DB08770 4148 None 84 Human Binding pKi = 7.2 7.2 -34 6
Displacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assayDisplacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assay
ChEMBL 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10.1021/acs.jmedchem.9b01340
11496023 138737 None 0 Human Binding pKi = 6.2 6.2 - 1
Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cellsDisplacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells
ChEMBL 446 7 1 7 3.0 CCCn1c(=O)c2nc(-c3cnn(Cc4c(F)cc(F)cc4F)c3)[nH]c2n(CCC)c1=O 10.1021/jm051268+
CHEMBL378020 138737 None 0 Human Binding pKi = 6.2 6.2 - 1
Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cellsDisplacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells
ChEMBL 446 7 1 7 3.0 CCCn1c(=O)c2nc(-c3cnn(Cc4c(F)cc(F)cc4F)c3)[nH]c2n(CCC)c1=O 10.1021/jm051268+
155563730 175408 None 0 Human Binding pKi = 6.2 6.2 - 1
Displacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assayDisplacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assay
ChEMBL 334 3 2 4 2.9 CC(C)OC(=O)C1=C(C(F)(F)F)NC(=O)NC1c1ccsc1 10.1021/acs.jmedchem.9b01340
CHEMBL4575695 175408 None 0 Human Binding pKi = 6.2 6.2 - 1
Displacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assayDisplacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assay
ChEMBL 334 3 2 4 2.9 CC(C)OC(=O)C1=C(C(F)(F)F)NC(=O)NC1c1ccsc1 10.1021/acs.jmedchem.9b01340
44284710 100453 None 0 Human Binding pKi = 5.2 5.2 -15 2
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 376 6 1 6 3.0 CCCn1c(=O)c2nc(-c3ccc(Cl)cc3OC)[nH]c2n(CCC)c1=O 10.1021/jm0104318
CHEMBL290643 100453 None 0 Human Binding pKi = 5.2 5.2 -15 2
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 376 6 1 6 3.0 CCCn1c(=O)c2nc(-c3ccc(Cl)cc3OC)[nH]c2n(CCC)c1=O 10.1021/jm0104318
4675559 103855 None 5 Human Binding pKi = 5.2 5.2 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 264 3 1 4 1.8 CCOC(=O)C1=C(C)N(C)C(=O)NC1c1ccco1 10.1021/acs.jmedchem.0c01431
CHEMBL3091714 103855 None 5 Human Binding pKi = 5.2 5.2 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 264 3 1 4 1.8 CCOC(=O)C1=C(C)N(C)C(=O)NC1c1ccco1 10.1021/acs.jmedchem.0c01431
4675559 103855 None 5 Human Binding pKi = 5.2 5.2 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by Scatchard plot analysisDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by Scatchard plot analysis
ChEMBL 264 3 1 4 1.8 CCOC(=O)C1=C(C)N(C)C(=O)NC1c1ccco1 10.1021/ml400185v
CHEMBL3091714 103855 None 5 Human Binding pKi = 5.2 5.2 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by Scatchard plot analysisDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by Scatchard plot analysis
ChEMBL 264 3 1 4 1.8 CCOC(=O)C1=C(C)N(C)C(=O)NC1c1ccco1 10.1021/ml400185v
162663283 181964 None 0 Human Binding pKi = 6.2 6.2 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 306 3 2 4 2.9 CC1=C(C(=O)OC2CCCC2)C(c2ccsc2)NC(=O)N1 10.1021/acs.jmedchem.0c01431
CHEMBL4780036 181964 None 0 Human Binding pKi = 6.2 6.2 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 306 3 2 4 2.9 CC1=C(C(=O)OC2CCCC2)C(c2ccsc2)NC(=O)N1 10.1021/acs.jmedchem.0c01431
135529396 116577 None 0 Human Binding pKi = 7.2 7.2 -1 2
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 571 9 2 9 3.4 CC(C)Cn1c(=O)c2nc(-c3cc(OCC(=O)Nc4ccc(Br)cc4)n(C)n3)[nH]c2n(CC(C)C)c1=O 10.1021/jm0309654
CHEMBL33653 116577 None 0 Human Binding pKi = 7.2 7.2 -1 2
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 571 9 2 9 3.4 CC(C)Cn1c(=O)c2nc(-c3cc(OCC(=O)Nc4ccc(Br)cc4)n(C)n3)[nH]c2n(CC(C)C)c1=O 10.1021/jm0309654
11590025 73415 None 0 Human Binding pKi = 7.2 7.2 6 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 429 10 1 8 2.2 CCOC(=O)COc1ccc(-c2cc3c([nH]2)c(=O)n(CC)c(=O)n3CCCOC)cc1 10.1021/jm0506221
CHEMBL201650 73415 None 0 Human Binding pKi = 7.2 7.2 6 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 429 10 1 8 2.2 CCOC(=O)COc1ccc(-c2cc3c([nH]2)c(=O)n(CC)c(=O)n3CCCOC)cc1 10.1021/jm0506221
145993107 166910 None 0 Human Binding pKi = 7.2 7.2 -1 4
Displacement of [3H]PSB-602 from human adenosine A2B receptor expressed in CHO cell membranesDisplacement of [3H]PSB-602 from human adenosine A2B receptor expressed in CHO cell membranes
ChEMBL 593 15 1 10 3.0 CCCCn1c(=O)c2c(nc3n2CCCN3CCc2ccc(OCC(=O)NCCN3CCCC3)cc2)n(CCCC)c1=O 10.1039/C8MD00070K
CHEMBL4286455 166910 None 0 Human Binding pKi = 7.2 7.2 -1 4
Displacement of [3H]PSB-602 from human adenosine A2B receptor expressed in CHO cell membranesDisplacement of [3H]PSB-602 from human adenosine A2B receptor expressed in CHO cell membranes
ChEMBL 593 15 1 10 3.0 CCCCn1c(=O)c2c(nc3n2CCCN3CCc2ccc(OCC(=O)NCCN3CCCC3)cc2)n(CCCC)c1=O 10.1039/C8MD00070K
127043663 141225 None 0 Human Binding pKi = 6.2 6.2 -1 3
Displacement of [3H]PSB-603 from recombinant human adenosine receptor A2b expressed in CHO cell membranesDisplacement of [3H]PSB-603 from recombinant human adenosine receptor A2b expressed in CHO cell membranes
ChEMBL 411 7 1 8 2.3 CCCn1c(=O)c2c(nc3n2CCCN3CCc2ccc(O)cc2)n(CCC)c1=O 10.1016/j.bmc.2016.07.028
CHEMBL3828658 141225 None 0 Human Binding pKi = 6.2 6.2 -1 3
Displacement of [3H]PSB-603 from recombinant human adenosine receptor A2b expressed in CHO cell membranesDisplacement of [3H]PSB-603 from recombinant human adenosine receptor A2b expressed in CHO cell membranes
ChEMBL 411 7 1 8 2.3 CCCn1c(=O)c2c(nc3n2CCCN3CCc2ccc(O)cc2)n(CCC)c1=O 10.1016/j.bmc.2016.07.028
162667742 182404 None 0 Human Binding pKi = 5.2 5.2 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 312 4 2 4 2.7 CC1=C(C(=O)OCc2ccccc2)C(c2ccoc2)NC(=O)N1 10.1021/acs.jmedchem.0c01431
CHEMBL4785576 182404 None 0 Human Binding pKi = 5.2 5.2 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 312 4 2 4 2.7 CC1=C(C(=O)OCc2ccccc2)C(c2ccoc2)NC(=O)N1 10.1021/acs.jmedchem.0c01431
135409793 16472 None 0 Human Binding pKi = 5.2 5.2 -5248 4
Inhibition of [3H]DPCPX binding to human Adenosine A2B receptor expressed in HEK cells; Range 3580-12400Inhibition of [3H]DPCPX binding to human Adenosine A2B receptor expressed in HEK cells; Range 3580-12400
ChEMBL 335 5 1 6 3.1 CCCCc1nc2[nH]cnc2c2nc(-c3ccc(N(C)C)cc3)nn12 10.1021/jm010570p
CHEMBL123462 16472 None 0 Human Binding pKi = 5.2 5.2 -5248 4
Inhibition of [3H]DPCPX binding to human Adenosine A2B receptor expressed in HEK cells; Range 3580-12400Inhibition of [3H]DPCPX binding to human Adenosine A2B receptor expressed in HEK cells; Range 3580-12400
ChEMBL 335 5 1 6 3.1 CCCCc1nc2[nH]cnc2c2nc(-c3ccc(N(C)C)cc3)nn12 10.1021/jm010570p
11483771 195718 None 0 Human Binding pKi = 7.2 7.2 -19 4
Binding affinity to adenosine A2B receptorBinding affinity to adenosine A2B receptor
ChEMBL 312 4 2 5 2.4 Nc1nc(C(=O)NCc2ccccc2F)cc(-c2ccco2)n1 10.1016/j.bmcl.2009.03.142
CHEMBL557084 195718 None 0 Human Binding pKi = 7.2 7.2 -19 4
Binding affinity to adenosine A2B receptorBinding affinity to adenosine A2B receptor
ChEMBL 312 4 2 5 2.4 Nc1nc(C(=O)NCc2ccccc2F)cc(-c2ccco2)n1 10.1016/j.bmcl.2009.03.142
71570217 86147 None 0 Human Binding pKi = 7.2 7.2 -23 4
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK-293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK-293 cells
ChEMBL 349 5 1 5 3.8 COc1cccc(-c2cc(NC(C)=O)nc(-c3cccc(OC)c3)n2)c1 10.1016/j.ejmech.2012.11.010
CHEMBL2311741 86147 None 0 Human Binding pKi = 7.2 7.2 -23 4
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK-293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK-293 cells
ChEMBL 349 5 1 5 3.8 COc1cccc(-c2cc(NC(C)=O)nc(-c3cccc(OC)c3)n2)c1 10.1016/j.ejmech.2012.11.010
44452536 95895 None 0 Human Binding pKi = 7.2 7.2 -16 4
Displacement of [3]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 309 4 2 7 2.3 CC(O)CNc1nc2ccccc2n2nc(-c3ccco3)nc12 10.1016/j.bmc.2007.10.103
CHEMBL259178 95895 None 0 Human Binding pKi = 7.2 7.2 -16 4
Displacement of [3]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 309 4 2 7 2.3 CC(O)CNc1nc2ccccc2n2nc(-c3ccco3)nc12 10.1016/j.bmc.2007.10.103
44588394 175349 None 0 Human Binding pKi = 6.2 6.2 -26 2
Displacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cells
ChEMBL 327 5 1 6 2.7 CCCn1c(=O)c2c(cc(-c3ccccc3)n2O)n(CCC)c1=O 10.1016/j.bmc.2008.09.067
CHEMBL457441 175349 None 0 Human Binding pKi = 6.2 6.2 -26 2
Displacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cells
ChEMBL 327 5 1 6 2.7 CCCn1c(=O)c2c(cc(-c3ccccc3)n2O)n(CCC)c1=O 10.1016/j.bmc.2008.09.067
52948671 19313 None 0 Human Binding pKi = 6.2 6.2 5 2
Displacement of [3H]ZM241385 from human adenosine A2B receptor transfected in CHO cells after 60 mins by scintillation countingDisplacement of [3H]ZM241385 from human adenosine A2B receptor transfected in CHO cells after 60 mins by scintillation counting
ChEMBL 520 11 1 5 4.8 COCCCNC(=O)COc1ccc2c(c1)c(CCc1ccccc1)c(-c1ccc(F)cc1F)c(=O)n2C 10.1016/j.bmcl.2010.10.030
CHEMBL1290544 19313 None 0 Human Binding pKi = 6.2 6.2 5 2
Displacement of [3H]ZM241385 from human adenosine A2B receptor transfected in CHO cells after 60 mins by scintillation countingDisplacement of [3H]ZM241385 from human adenosine A2B receptor transfected in CHO cells after 60 mins by scintillation counting
ChEMBL 520 11 1 5 4.8 COCCCNC(=O)COc1ccc2c(c1)c(CCc1ccccc1)c(-c1ccc(F)cc1F)c(=O)n2C 10.1016/j.bmcl.2010.10.030
71680730 90210 None 0 Human Binding pKi = 6.2 6.2 -10 4
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells after 75 mins by liquid scintillation counting analysisDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells after 75 mins by liquid scintillation counting analysis
ChEMBL 338 4 1 5 3.3 COc1cccc(/C=C/C(=O)Nc2nc3ccccc3c(=O)s2)c1 10.1021/jm400336x
CHEMBL2382431 90210 None 0 Human Binding pKi = 6.2 6.2 -10 4
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells after 75 mins by liquid scintillation counting analysisDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells after 75 mins by liquid scintillation counting analysis
ChEMBL 338 4 1 5 3.3 COc1cccc(/C=C/C(=O)Nc2nc3ccccc3c(=O)s2)c1 10.1021/jm400336x
44588393 176339 None 0 Human Binding pKi = 7.2 7.2 10 2
Displacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cells
ChEMBL 349 2 2 7 0.3 Cn1c(=O)c2[nH]c(-c3ccc(S(C)(=O)=O)cc3)c(O)c2n(C)c1=O 10.1016/j.bmc.2008.09.067
CHEMBL459553 176339 None 0 Human Binding pKi = 7.2 7.2 10 2
Displacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cells
ChEMBL 349 2 2 7 0.3 Cn1c(=O)c2[nH]c(-c3ccc(S(C)(=O)=O)cc3)c(O)c2n(C)c1=O 10.1016/j.bmc.2008.09.067
156014270 177217 None 0 Human Binding pKi = 7.2 7.2 - 1
Displacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting methodDisplacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting method
ChEMBL 354 3 1 7 3.7 CC1=C(C(=O)OC(C)C)C(c2cncs2)n2c(nc3ccccc32)N1 10.1021/acs.jmedchem.0c00564
CHEMBL4635502 177217 None 0 Human Binding pKi = 7.2 7.2 - 1
Displacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting methodDisplacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting method
ChEMBL 354 3 1 7 3.7 CC1=C(C(=O)OC(C)C)C(c2cncs2)n2c(nc3ccccc32)N1 10.1021/acs.jmedchem.0c00564
127038752 136745 None 0 Human Binding pKi = 6.2 6.2 -74 4
Displacement of [3H]-DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by liquid scintillation counting analysis
ChEMBL 466 7 4 13 0.5 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(NC(C)Cc5ccccc5)nc43)[C@H](O)[C@@H]2O)n1 10.1039/C5MD00086F
CHEMBL3740959 136745 None 0 Human Binding pKi = 6.2 6.2 -74 4
Displacement of [3H]-DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by liquid scintillation counting analysis
ChEMBL 466 7 4 13 0.5 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(NC(C)Cc5ccccc5)nc43)[C@H](O)[C@@H]2O)n1 10.1039/C5MD00086F
10065148 99115 None 0 Human Binding pKi = 7.2 7.2 -33 4
Displacement of [3H]- DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]- DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 329 4 1 9 2.4 CCCSc1c2c(nc(N)n3nc(-c4ccco4)nc23)nn1C 10.1021/jm021023m
CHEMBL280888 99115 None 0 Human Binding pKi = 7.2 7.2 -33 4
Displacement of [3H]- DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]- DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 329 4 1 9 2.4 CCCSc1c2c(nc(N)n3nc(-c4ccco4)nc23)nn1C 10.1021/jm021023m
136383804 158096 None 0 Human Binding pKi = 7.2 7.2 - 1
Displacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting methodDisplacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting method
ChEMBL 560 9 1 9 3.8 CCCn1c(=O)c2[nH]c(-c3cc(OCC4CC(=O)N(c5cccc(C(F)(F)F)c5)C4)no3)nc2n(CCC)c1=O 10.1016/j.ejmech.2016.11.007
CHEMBL4086551 158096 None 0 Human Binding pKi = 7.2 7.2 - 1
Displacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting methodDisplacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting method
ChEMBL 560 9 1 9 3.8 CCCn1c(=O)c2[nH]c(-c3cc(OCC4CC(=O)N(c5cccc(C(F)(F)F)c5)C4)no3)nc2n(CCC)c1=O 10.1016/j.ejmech.2016.11.007
11537425 85382 None 0 Human Binding pKi = 7.2 7.2 - 1
Displacement of [3H]DPCPX from human A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human A2B receptor expressed in HEK293 cells
ChEMBL 341 4 1 8 3.2 N#Cc1cncc(Nc2ncc(-c3ccncn3)c(-c3ccco3)n2)c1 10.1021/jm061333v
CHEMBL226237 85382 None 0 Human Binding pKi = 7.2 7.2 - 1
Displacement of [3H]DPCPX from human A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human A2B receptor expressed in HEK293 cells
ChEMBL 341 4 1 8 3.2 N#Cc1cncc(Nc2ncc(-c3ccncn3)c(-c3ccco3)n2)c1 10.1021/jm061333v
11711753 166223 None 0 Human Binding pKi = 7.2 7.2 15 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 434 6 2 7 2.3 COc1cc(OCC(=O)Nc2ccccc2)ccc1-c1cc2c([nH]1)c(=O)n(C)c(=O)n2C 10.1021/jm0506221
CHEMBL426660 166223 None 0 Human Binding pKi = 7.2 7.2 15 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 434 6 2 7 2.3 COc1cc(OCC(=O)Nc2ccccc2)ccc1-c1cc2c([nH]1)c(=O)n(C)c(=O)n2C 10.1021/jm0506221
44451018 160586 None 0 Human Binding pKi = 7.2 7.2 3 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 535 7 1 7 3.5 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCN(c5ccccc5Cl)CC4)cc3)cc2n(C)c1=O 10.1016/j.bmc.2008.01.002
CHEMBL411275 160586 None 0 Human Binding pKi = 7.2 7.2 3 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 535 7 1 7 3.5 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCN(c5ccccc5Cl)CC4)cc3)cc2n(C)c1=O 10.1016/j.bmc.2008.01.002
10861697 103038 None 0 Human Binding pKi = 6.2 6.2 2 4
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 374 7 0 6 3.1 CCCn1c(=O)c2c(nc(-c3ccccc3)n2CCCl)n(CCC)c1=O 10.1021/jm0104318
CHEMBL307105 103038 None 0 Human Binding pKi = 6.2 6.2 2 4
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 374 7 0 6 3.1 CCCn1c(=O)c2c(nc(-c3ccccc3)n2CCCl)n(CCC)c1=O 10.1021/jm0104318
265603 162585 None 9 Human Binding pKi = 5.2 5.2 - 1
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 301 2 1 7 0.5 Cn1c(=O)c2nc(-c3ccc([N+](=O)[O-])cc3)[nH]c2n(C)c1=O 10.1021/jm0104318
CHEMBL416884 162585 None 9 Human Binding pKi = 5.2 5.2 - 1
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 301 2 1 7 0.5 Cn1c(=O)c2nc(-c3ccc([N+](=O)[O-])cc3)[nH]c2n(C)c1=O 10.1021/jm0104318
137175186 139155 None 0 Human Binding pKi = 6.2 6.2 - 1
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 minsDisplacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 mins
ChEMBL 290 3 1 7 2.2 CCOC(=O)C1=C(C)Nc2ncnn2C1c1ccsc1 10.1021/acs.jmedchem.5b01586
CHEMBL3787179 139155 None 0 Human Binding pKi = 6.2 6.2 - 1
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 minsDisplacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 mins
ChEMBL 290 3 1 7 2.2 CCOC(=O)C1=C(C)Nc2ncnn2C1c1ccsc1 10.1021/acs.jmedchem.5b01586
10226014 94591 None 0 Human Binding pKi = 8.2 8.2 - 1
Displacement of 3H-ZM214385 from human Adenosine A2B receptor expressed in HEK293 cells after 90 minsDisplacement of 3H-ZM214385 from human Adenosine A2B receptor expressed in HEK293 cells after 90 mins
ChEMBL 452 6 2 9 2.4 CCCn1c(=O)[nH]c2nc(-c3cnn(Cc4noc(-c5ccc(Cl)cc5)n4)c3)[nH]c2c1=O 10.1021/acs.jmedchem.5b01586
CHEMBL252048 94591 None 0 Human Binding pKi = 8.2 8.2 - 1
Displacement of 3H-ZM214385 from human Adenosine A2B receptor expressed in HEK293 cells after 90 minsDisplacement of 3H-ZM214385 from human Adenosine A2B receptor expressed in HEK293 cells after 90 mins
ChEMBL 452 6 2 9 2.4 CCCn1c(=O)[nH]c2nc(-c3cnn(Cc4noc(-c5ccc(Cl)cc5)n4)c3)[nH]c2c1=O 10.1021/acs.jmedchem.5b01586
10226014 94591 None 0 Human Binding pKi = 8.2 8.2 - 1
Displacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranesDisplacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranes
ChEMBL 452 6 2 9 2.4 CCCn1c(=O)[nH]c2nc(-c3cnn(Cc4noc(-c5ccc(Cl)cc5)n4)c3)[nH]c2c1=O 10.1016/j.bmcl.2008.01.008
CHEMBL252048 94591 None 0 Human Binding pKi = 8.2 8.2 - 1
Displacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranesDisplacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranes
ChEMBL 452 6 2 9 2.4 CCCn1c(=O)[nH]c2nc(-c3cnn(Cc4noc(-c5ccc(Cl)cc5)n4)c3)[nH]c2c1=O 10.1016/j.bmcl.2008.01.008
46880333 6305 None 0 Human Binding pKi = 8.2 8.2 29 4
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 279 3 1 4 3.4 CC(=O)Nc1ccc(-c2ccncc2)c(-c2ccco2)n1 10.1016/j.bmcl.2010.01.045
CHEMBL1081811 6305 None 0 Human Binding pKi = 8.2 8.2 29 4
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 279 3 1 4 3.4 CC(=O)Nc1ccc(-c2ccncc2)c(-c2ccco2)n1 10.1016/j.bmcl.2010.01.045
135678052 95777 None 0 Human Binding pKi = 8.2 8.2 - 1
Displacement of [3H]MRE2029F20 from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]MRE2029F20 from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 483 8 2 8 3.2 CCCn1c(=O)c2[nH]c(-c3cc(C)n(CC(=O)Nc4ccc(Cl)cc4)n3)nc2n(CCC)c1=O 10.1016/j.bmc.2007.11.058
CHEMBL258571 95777 None 0 Human Binding pKi = 8.2 8.2 - 1
Displacement of [3H]MRE2029F20 from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]MRE2029F20 from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 483 8 2 8 3.2 CCCn1c(=O)c2[nH]c(-c3cc(C)n(CC(=O)Nc4ccc(Cl)cc4)n3)nc2n(CCC)c1=O 10.1016/j.bmc.2007.11.058
145964662 164438 None 0 Human Binding pKi = 8.2 8.2 3 3
Displacement of [3H]PSB-603 from recombinant human adenosine A2B receptor expressed in CHO cell membranes after 75 mins by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human adenosine A2B receptor expressed in CHO cell membranes after 75 mins by liquid scintillation counting method
ChEMBL 433 8 3 6 2.2 CCCn1c(=O)[nH]c2nc(-c3ccc(OCC(=O)NCc4ccccc4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.7b01627
CHEMBL4213768 164438 None 0 Human Binding pKi = 8.2 8.2 3 3
Displacement of [3H]PSB-603 from recombinant human adenosine A2B receptor expressed in CHO cell membranes after 75 mins by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human adenosine A2B receptor expressed in CHO cell membranes after 75 mins by liquid scintillation counting method
ChEMBL 433 8 3 6 2.2 CCCn1c(=O)[nH]c2nc(-c3ccc(OCC(=O)NCc4ccccc4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.7b01627
21916389 95926 None 0 Human Binding pKi = 8.2 8.2 4 4
Displacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 394 5 1 7 1.9 Cn1c(=O)n(CC2CC2)c(=O)c2[nH]c(-c3cnn(Cc4cccc(F)c4)c3)nc21 10.1021/jm7014815
CHEMBL259300 95926 None 0 Human Binding pKi = 8.2 8.2 4 4
Displacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]ZM-241385 from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 394 5 1 7 1.9 Cn1c(=O)n(CC2CC2)c(=O)c2[nH]c(-c3cnn(Cc4cccc(F)c4)c3)nc21 10.1021/jm7014815
49797747 10619 None 0 Human Binding pKi = 8.2 8.2 10 3
Displacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cells after 1 hr by scintillation countingDisplacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 482 6 1 7 3.4 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(C(=O)N4CCOCC4)cc3)sc12 10.1016/j.bmcl.2010.05.056
CHEMBL1170134 10619 None 0 Human Binding pKi = 8.2 8.2 10 3
Displacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cells after 1 hr by scintillation countingDisplacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 482 6 1 7 3.4 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(C(=O)N4CCOCC4)cc3)sc12 10.1016/j.bmcl.2010.05.056
155551750 175388 None 0 Human Binding pKi = 8.2 8.2 44 3
Displacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 626 14 2 10 2.0 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc(OCCOCCOC)cc5)CC4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
CHEMBL4575279 175388 None 0 Human Binding pKi = 8.2 8.2 44 3
Displacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 626 14 2 10 2.0 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc(OCCOCCOC)cc5)CC4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
44451271 95775 None 0 Human Binding pKi = 8.2 8.2 45 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 542 5 1 8 2.7 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCN(c5c(Cl)cncc5Cl)CC4)cc3)cc2n(C)c1=O 10.1016/j.bmc.2008.01.002
CHEMBL258568 95775 None 0 Human Binding pKi = 8.2 8.2 45 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 542 5 1 8 2.7 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCN(c5c(Cl)cncc5Cl)CC4)cc3)cc2n(C)c1=O 10.1016/j.bmc.2008.01.002
44574194 178428 None 0 Human Binding pKi = 8.2 8.2 2 4
Displacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells by beta scintillation counterDisplacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells by beta scintillation counter
ChEMBL 460 8 2 6 4.7 CCCn1c(=O)c2[nH]c(-c3ccc(COC(=O)Nc4ccccc4)cc3)cc2n(CCC)c1=O 10.1016/j.bmc.2009.03.062
CHEMBL466021 178428 None 0 Human Binding pKi = 8.2 8.2 2 4
Displacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells by beta scintillation counterDisplacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells by beta scintillation counter
ChEMBL 460 8 2 6 4.7 CCCn1c(=O)c2[nH]c(-c3ccc(COC(=O)Nc4ccccc4)cc3)cc2n(CCC)c1=O 10.1016/j.bmc.2009.03.062
155566764 175873 None 0 Human Binding pKi = 8.2 8.2 41 2
Displacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 508 6 2 7 2.4 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(c5ccccc5)C(C)C4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
CHEMBL4586090 175873 None 0 Human Binding pKi = 8.2 8.2 41 2
Displacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 508 6 2 7 2.4 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(c5ccccc5)C(C)C4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
44450828 157695 None 0 Human Binding pKi = 8.1 8.1 44 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 472 6 1 6 3.1 CCCn1c(=O)n(C)c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCc5ccccc5C4)cc3)cc21 10.1016/j.bmc.2008.01.002
CHEMBL408185 157695 None 0 Human Binding pKi = 8.1 8.1 44 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 472 6 1 6 3.1 CCCn1c(=O)n(C)c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCc5ccccc5C4)cc3)cc21 10.1016/j.bmc.2008.01.002
44236602 159034 None 0 Human Binding pKi = 8.1 8.1 - 1
Displacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 minsDisplacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 mins
ChEMBL 420 5 1 7 2.4 CCCn1c(=O)c2[nH]c(-c3cnn(CC#Cc4ccc(F)cc4)c3)nc2n(CC)c1=O 10.1016/j.ejmech.2017.04.014
CHEMBL4096746 159034 None 0 Human Binding pKi = 8.1 8.1 - 1
Displacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 minsDisplacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 mins
ChEMBL 420 5 1 7 2.4 CCCn1c(=O)c2[nH]c(-c3cnn(CC#Cc4ccc(F)cc4)c3)nc2n(CC)c1=O 10.1016/j.ejmech.2017.04.014
44236571 155816 None 0 Human Binding pKi = 8.1 8.1 - 1
Displacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 minsDisplacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 mins
ChEMBL 420 5 1 7 2.4 CCCn1c(=O)c2[nH]c(-c3cnn(CC#Cc4cccc(F)c4)c3)nc2n(CC)c1=O 10.1016/j.ejmech.2017.04.014
CHEMBL4059836 155816 None 0 Human Binding pKi = 8.1 8.1 - 1
Displacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 minsDisplacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 mins
ChEMBL 420 5 1 7 2.4 CCCn1c(=O)c2[nH]c(-c3cnn(CC#Cc4cccc(F)c4)c3)nc2n(CC)c1=O 10.1016/j.ejmech.2017.04.014
44451072 96040 None 0 Human Binding pKi = 8.1 8.1 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 543 9 1 7 4.0 CCCn1c(=O)n(CC(C)C)c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCN(c5ccccc5)CC4)cc3)cc21 10.1016/j.bmc.2008.01.002
CHEMBL259874 96040 None 0 Human Binding pKi = 8.1 8.1 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 543 9 1 7 4.0 CCCn1c(=O)n(CC(C)C)c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCN(c5ccccc5)CC4)cc3)cc21 10.1016/j.bmc.2008.01.002
44551168 201775 None 0 Human Binding pKi = 8.1 8.1 11 3
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 370 5 0 8 2.2 CCn1c(=O)c2c(nc(Cc3cccs3)n2C)n(Cc2ccco2)c1=O 10.1016/j.bmc.2009.07.034
CHEMBL606753 201775 None 0 Human Binding pKi = 8.1 8.1 11 3
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 370 5 0 8 2.2 CCn1c(=O)c2c(nc(Cc3cccs3)n2C)n(Cc2ccco2)c1=O 10.1016/j.bmc.2009.07.034
145976828 163678 None 0 Human Binding pKi = 8.1 8.1 1 2
Displacement of [3H]PSB-603 from recombinant human adenosine A2B receptor expressed in CHO cell membranes after 75 mins by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human adenosine A2B receptor expressed in CHO cell membranes after 75 mins by liquid scintillation counting method
ChEMBL 447 9 3 6 2.2 CCCn1c(=O)[nH]c2nc(-c3ccc(OCC(=O)NCCc4ccccc4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.7b01627
CHEMBL4204683 163678 None 0 Human Binding pKi = 8.1 8.1 1 2
Displacement of [3H]PSB-603 from recombinant human adenosine A2B receptor expressed in CHO cell membranes after 75 mins by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human adenosine A2B receptor expressed in CHO cell membranes after 75 mins by liquid scintillation counting method
ChEMBL 447 9 3 6 2.2 CCCn1c(=O)[nH]c2nc(-c3ccc(OCC(=O)NCCc4ccccc4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.7b01627
44185932 191619 None 0 Human Binding pKi = 8.1 8.1 11 4
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 508 7 2 7 1.6 CCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(CCc5ccccc5)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
CHEMBL519556 191619 None 0 Human Binding pKi = 8.1 8.1 11 4
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 508 7 2 7 1.6 CCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(CCc5ccccc5)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
66894103 156561 None 0 Human Binding pKi = 8.1 8.1 - 1
Displacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting methodDisplacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting method
ChEMBL 569 9 1 7 4.8 CCCn1c(=O)c2[nH]c(-c3ccc(OCC4CC(=O)N(c5cccc(C(F)(F)F)c5)C4)cc3)nc2n(CCC)c1=O 10.1016/j.ejmech.2016.11.007
CHEMBL4068421 156561 None 0 Human Binding pKi = 8.1 8.1 - 1
Displacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting methodDisplacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting method
ChEMBL 569 9 1 7 4.8 CCCn1c(=O)c2[nH]c(-c3ccc(OCC4CC(=O)N(c5cccc(C(F)(F)F)c5)C4)cc3)nc2n(CCC)c1=O 10.1016/j.ejmech.2016.11.007
56951623 71173 None 0 Human Binding pKi = 8.1 8.1 18 3
Displacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation countingDisplacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation counting
ChEMBL 331 5 2 6 1.0 CCCn1c(=O)c2[nH]c(-c3cc(=O)[nH]n3C)cc2n(CCC)c1=O 10.1021/jm201292w
CHEMBL1955923 71173 None 0 Human Binding pKi = 8.1 8.1 18 3
Displacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation countingDisplacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation counting
ChEMBL 331 5 2 6 1.0 CCCn1c(=O)c2[nH]c(-c3cc(=O)[nH]n3C)cc2n(CCC)c1=O 10.1021/jm201292w
44185933 186709 None 0 Human Binding pKi = 8.1 8.1 35 5
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 522 8 2 7 2.0 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(CCc5ccccc5)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
CHEMBL488541 186709 None 0 Human Binding pKi = 8.1 8.1 35 5
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 522 8 2 7 2.0 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(CCc5ccccc5)CC4)cc3)[nH]c2c1=O 10.1021/jm900413e
44450850 95847 None 0 Human Binding pKi = 8.1 8.1 9 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 598 9 1 8 4.4 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCN(c5c(Cl)cncc5Cl)CC4)cc3)cc2n(CCC)c1=O 10.1016/j.bmc.2008.01.002
CHEMBL258979 95847 None 0 Human Binding pKi = 8.1 8.1 9 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 598 9 1 8 4.4 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCN(c5c(Cl)cncc5Cl)CC4)cc3)cc2n(CCC)c1=O 10.1016/j.bmc.2008.01.002
11498113 73029 None 0 Human Binding pKi = 8.1 8.1 6 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 607 12 2 8 3.9 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(CS(=O)(=O)N5CCCC5)cc4)cc3)cc2n(CCC)c1=O 10.1021/jm0506221
CHEMBL201008 73029 None 0 Human Binding pKi = 8.1 8.1 6 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 607 12 2 8 3.9 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(CS(=O)(=O)N5CCCC5)cc4)cc3)cc2n(CCC)c1=O 10.1021/jm0506221
11664137 73299 None 0 Human Binding pKi = 8.1 8.1 4 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 565 10 2 6 4.3 CCCn1c(=O)c2[nH]c(-c3ccc(N(C=O)CC(=O)Nc4ccc(Br)cc4)cc3)cc2n(CCC)c1=O 10.1021/jm0506221
CHEMBL201293 73299 None 0 Human Binding pKi = 8.1 8.1 4 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 565 10 2 6 4.3 CCCn1c(=O)c2[nH]c(-c3ccc(N(C=O)CC(=O)Nc4ccc(Br)cc4)cc3)cc2n(CCC)c1=O 10.1021/jm0506221
11604435 75025 None 0 Human Binding pKi = 8.1 8.1 23 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 432 7 2 6 3.2 CCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccccc4)cc3)cc2n(CC)c1=O 10.1021/jm0506221
CHEMBL203413 75025 None 0 Human Binding pKi = 8.1 8.1 23 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 432 7 2 6 3.2 CCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccccc4)cc3)cc2n(CC)c1=O 10.1021/jm0506221
137640112 156682 None 0 Human Binding pKi = 8.1 8.1 - 1
Displacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 minsDisplacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 mins
ChEMBL 488 8 1 9 2.8 CCCn1c(=O)c2[nH]c(-c3cnn(CC#Cc4ccccc4C(=O)OCC)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2017.04.014
CHEMBL4069730 156682 None 0 Human Binding pKi = 8.1 8.1 - 1
Displacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 minsDisplacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 mins
ChEMBL 488 8 1 9 2.8 CCCn1c(=O)c2[nH]c(-c3cnn(CC#Cc4ccccc4C(=O)OCC)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2017.04.014
44574225 178593 None 0 Human Binding pKi = 8.1 8.1 4 2
Displacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells by beta scintillation counterDisplacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells by beta scintillation counter
ChEMBL 462 8 2 8 3.5 CCCn1c(=O)c2[nH]c(-c3ccc(COC(=O)Nc4cnccn4)cc3)cc2n(CCC)c1=O 10.1016/j.bmc.2009.03.062
CHEMBL467271 178593 None 0 Human Binding pKi = 8.1 8.1 4 2
Displacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells by beta scintillation counterDisplacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells by beta scintillation counter
ChEMBL 462 8 2 8 3.5 CCCn1c(=O)c2[nH]c(-c3ccc(COC(=O)Nc4cnccn4)cc3)cc2n(CCC)c1=O 10.1016/j.bmc.2009.03.062
145973326 164724 None 0 Human Binding pKi = 8.1 8.1 29 3
Displacement of [3H]PSB-603 from recombinant human adenosine A2B receptor expressed in CHO cell membranes after 75 mins by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human adenosine A2B receptor expressed in CHO cell membranes after 75 mins by liquid scintillation counting method
ChEMBL 729 17 3 7 7.0 CCCn1c(=O)[nH]c2nc(-c3ccc(OCC(=O)NCCCCCCCCCCC4=C5C(C)=CC(C)=[N+]5[B-](F)(F)n5c(C)cc(C)c54)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.7b01627
CHEMBL4217459 164724 None 0 Human Binding pKi = 8.1 8.1 29 3
Displacement of [3H]PSB-603 from recombinant human adenosine A2B receptor expressed in CHO cell membranes after 75 mins by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human adenosine A2B receptor expressed in CHO cell membranes after 75 mins by liquid scintillation counting method
ChEMBL 729 17 3 7 7.0 CCCn1c(=O)[nH]c2nc(-c3ccc(OCC(=O)NCCCCCCCCCCC4=C5C(C)=CC(C)=[N+]5[B-](F)(F)n5c(C)cc(C)c54)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.7b01627
11562203 73150 None 0 Human Binding pKi = 8.1 8.1 6 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 488 9 2 6 4.8 CCCn1c(=O)c2[nH]c(-c3ccc(OC(C)(C)C(=O)Nc4ccccc4)cc3)cc2n(CCC)c1=O 10.1021/jm0506221
CHEMBL201157 73150 None 0 Human Binding pKi = 8.1 8.1 6 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 488 9 2 6 4.8 CCCn1c(=O)c2[nH]c(-c3ccc(OC(C)(C)C(=O)Nc4ccccc4)cc3)cc2n(CCC)c1=O 10.1021/jm0506221
44406891 73543 None 0 Human Binding pKi = 8.1 8.1 10 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 516 9 2 6 5.3 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(C(C)(C)C)cc4)cc3)cc2n(CCC)c1=O 10.1021/jm0506221
CHEMBL201749 73543 None 0 Human Binding pKi = 8.1 8.1 10 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 516 9 2 6 5.3 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(C(C)(C)C)cc4)cc3)cc2n(CCC)c1=O 10.1021/jm0506221
10720065 98397 None 0 Human Binding pKi = 8.1 8.1 1 6
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 495 9 2 7 4.0 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccc(Cl)cc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm0506221
CHEMBL275427 98397 None 0 Human Binding pKi = 8.1 8.1 1 6
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 495 9 2 7 4.0 CCCn1c(=O)c2nc(-c3ccc(OCC(=O)Nc4ccc(Cl)cc4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm0506221
168296088 192366 None 1 Human Binding pKi = 8.1 8.1 - 1
Displacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cell membrane and measured after 0.5 hrs by radioligand displacement assayDisplacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cell membrane and measured after 0.5 hrs by radioligand displacement assay
ChEMBL 352 4 2 6 1.1 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)F)cc3)[nH]c2c1=O 10.1039/d2md00132b
CHEMBL5207290 192366 None 1 Human Binding pKi = 8.1 8.1 - 1
Displacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cell membrane and measured after 0.5 hrs by radioligand displacement assayDisplacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cell membrane and measured after 0.5 hrs by radioligand displacement assay
ChEMBL 352 4 2 6 1.1 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)F)cc3)[nH]c2c1=O 10.1039/d2md00132b
11784407 97232 None 0 Human Binding pKi = 7.2 7.2 6 3
Binding affinity for human adenosine A2B receptor using [3H]ZM-241385 in CHO cell membranesBinding affinity for human adenosine A2B receptor using [3H]ZM-241385 in CHO cell membranes
ChEMBL 364 5 3 6 1.1 CCCCn1c(=O)[nH]c2[nH]c(-c3ccc(S(=O)(=O)O)cc3)nc2c1=O 10.1021/jm0310030
CHEMBL268617 97232 None 0 Human Binding pKi = 7.2 7.2 6 3
Binding affinity for human adenosine A2B receptor using [3H]ZM-241385 in CHO cell membranesBinding affinity for human adenosine A2B receptor using [3H]ZM-241385 in CHO cell membranes
ChEMBL 364 5 3 6 1.1 CCCCn1c(=O)[nH]c2[nH]c(-c3ccc(S(=O)(=O)O)cc3)nc2c1=O 10.1021/jm0310030
CHEMBL36952 97232 None 0 Human Binding pKi = 7.2 7.2 6 3
Binding affinity for human adenosine A2B receptor using [3H]ZM-241385 in CHO cell membranesBinding affinity for human adenosine A2B receptor using [3H]ZM-241385 in CHO cell membranes
ChEMBL 364 5 3 6 1.1 CCCCn1c(=O)[nH]c2[nH]c(-c3ccc(S(=O)(=O)O)cc3)nc2c1=O 10.1021/jm0310030
135465776 99720 None 0 Human Binding pKi = 7.2 7.2 - 1
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 470 9 2 9 2.5 CCCn1c(=O)c2nc(-c3cc(OCC(=O)Nc4ccc(F)cc4)no3)[nH]c2n(CCC)c1=O 10.1021/jm0309654
CHEMBL284789 99720 None 0 Human Binding pKi = 7.2 7.2 - 1
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 470 9 2 9 2.5 CCCn1c(=O)c2nc(-c3cc(OCC(=O)Nc4ccc(F)cc4)no3)[nH]c2n(CCC)c1=O 10.1021/jm0309654
10647227 165454 None 0 Human Binding pKi = 7.2 7.2 -3 4
Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 56-89Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 56-89
ChEMBL 450 6 2 8 4.8 CCCCn1cc2c(nc(NC(=O)Nc3cccc(Cl)c3)n3nc(-c4ccco4)nc23)n1 10.1021/jm001047y
CHEMBL423934 165454 None 0 Human Binding pKi = 7.2 7.2 -3 4
Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 56-89Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 56-89
ChEMBL 450 6 2 8 4.8 CCCCn1cc2c(nc(NC(=O)Nc3cccc(Cl)c3)n3nc(-c4ccco4)nc23)n1 10.1021/jm001047y
10647227 165454 None 0 Human Binding pKi = 7.2 7.2 -3 4
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 56-89Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 56-89
ChEMBL 450 6 2 8 4.8 CCCCn1cc2c(nc(NC(=O)Nc3cccc(Cl)c3)n3nc(-c4ccco4)nc23)n1 10.1021/jm0109614
CHEMBL423934 165454 None 0 Human Binding pKi = 7.2 7.2 -3 4
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 56-89Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 56-89
ChEMBL 450 6 2 8 4.8 CCCCn1cc2c(nc(NC(=O)Nc3cccc(Cl)c3)n3nc(-c4ccco4)nc23)n1 10.1021/jm0109614
52946114 19273 None 0 Human Binding pKi = 7.2 7.2 2 2
Displacement of [3H]ZM241385 from human adenosine A2B receptor transfected in CHO cells after 60 mins by scintillation countingDisplacement of [3H]ZM241385 from human adenosine A2B receptor transfected in CHO cells after 60 mins by scintillation counting
ChEMBL 525 9 2 6 5.7 CC(C)(NC(=O)COc1ccc2[nH]c(=O)c(-c3nccs3)c(COc3ccccc3)c2c1)c1ccccc1 10.1016/j.bmcl.2010.10.030
CHEMBL1290325 19273 None 0 Human Binding pKi = 7.2 7.2 2 2
Displacement of [3H]ZM241385 from human adenosine A2B receptor transfected in CHO cells after 60 mins by scintillation countingDisplacement of [3H]ZM241385 from human adenosine A2B receptor transfected in CHO cells after 60 mins by scintillation counting
ChEMBL 525 9 2 6 5.7 CC(C)(NC(=O)COc1ccc2[nH]c(=O)c(-c3nccs3)c(COc3ccccc3)c2c1)c1ccccc1 10.1016/j.bmcl.2010.10.030
52945098 19353 None 0 Human Binding pKi = 7.2 7.2 -1 2
Displacement of [3H]ZM241385 from human adenosine A2B receptor transfected in CHO cells after 60 mins by scintillation countingDisplacement of [3H]ZM241385 from human adenosine A2B receptor transfected in CHO cells after 60 mins by scintillation counting
ChEMBL 504 9 1 6 3.4 Cn1c(=O)c(S(C)(=O)=O)c(CCc2ccccc2)c2cc(OCC(=O)NCc3ccccc3)ccc21 10.1016/j.bmcl.2010.10.030
CHEMBL1290782 19353 None 0 Human Binding pKi = 7.2 7.2 -1 2
Displacement of [3H]ZM241385 from human adenosine A2B receptor transfected in CHO cells after 60 mins by scintillation countingDisplacement of [3H]ZM241385 from human adenosine A2B receptor transfected in CHO cells after 60 mins by scintillation counting
ChEMBL 504 9 1 6 3.4 Cn1c(=O)c(S(C)(=O)=O)c(CCc2ccccc2)c2cc(OCC(=O)NCc3ccccc3)ccc21 10.1016/j.bmcl.2010.10.030
11784407 97232 None 0 Human Binding pKi = 7.2 7.2 6 3
Inhibition of [3H]ZM-241385 binding to human adenosine A2B receptorInhibition of [3H]ZM-241385 binding to human adenosine A2B receptor
ChEMBL 364 5 3 6 1.1 CCCCn1c(=O)[nH]c2[nH]c(-c3ccc(S(=O)(=O)O)cc3)nc2c1=O 10.1021/jm011049y
CHEMBL268617 97232 None 0 Human Binding pKi = 7.2 7.2 6 3
Inhibition of [3H]ZM-241385 binding to human adenosine A2B receptorInhibition of [3H]ZM-241385 binding to human adenosine A2B receptor
ChEMBL 364 5 3 6 1.1 CCCCn1c(=O)[nH]c2[nH]c(-c3ccc(S(=O)(=O)O)cc3)nc2c1=O 10.1021/jm011049y
CHEMBL36952 97232 None 0 Human Binding pKi = 7.2 7.2 6 3
Inhibition of [3H]ZM-241385 binding to human adenosine A2B receptorInhibition of [3H]ZM-241385 binding to human adenosine A2B receptor
ChEMBL 364 5 3 6 1.1 CCCCn1c(=O)[nH]c2[nH]c(-c3ccc(S(=O)(=O)O)cc3)nc2c1=O 10.1021/jm011049y
135515507 34124 None 0 Human Binding pKi = 7.2 7.2 -4 4
Tested for inhibitory activity against Adenosine A2b receptor by displacement of [3H]DPCPX expressed in CHO cells; value ranges from 61-80Tested for inhibitory activity against Adenosine A2b receptor by displacement of [3H]DPCPX expressed in CHO cells; value ranges from 61-80
ChEMBL 394 3 3 7 3.6 O=C(Nc1cccc(Cl)c1)Nc1nc2n[nH]cc2c2nc(-c3ccco3)nn12 10.1021/jm001047y
CHEMBL142562 34124 None 0 Human Binding pKi = 7.2 7.2 -4 4
Tested for inhibitory activity against Adenosine A2b receptor by displacement of [3H]DPCPX expressed in CHO cells; value ranges from 61-80Tested for inhibitory activity against Adenosine A2b receptor by displacement of [3H]DPCPX expressed in CHO cells; value ranges from 61-80
ChEMBL 394 3 3 7 3.6 O=C(Nc1cccc(Cl)c1)Nc1nc2n[nH]cc2c2nc(-c3ccco3)nn12 10.1021/jm001047y
45269769 196573 None 0 Human Binding pKi = 7.2 7.2 7 2
Binding affinity to human adenosine A2b receptor expressed in HEK293 cellsBinding affinity to human adenosine A2b receptor expressed in HEK293 cells
ChEMBL 404 7 1 6 3.3 CCn1c(=O)c2[nH]c(-c3ccc(-c4ccccc4)cc3)nc2n(CCCOC)c1=O 10.1016/j.bmc.2009.03.029
CHEMBL563889 196573 None 0 Human Binding pKi = 7.2 7.2 7 2
Binding affinity to human adenosine A2b receptor expressed in HEK293 cellsBinding affinity to human adenosine A2b receptor expressed in HEK293 cells
ChEMBL 404 7 1 6 3.3 CCn1c(=O)c2[nH]c(-c3ccc(-c4ccccc4)cc3)nc2n(CCCOC)c1=O 10.1016/j.bmc.2009.03.029
11567699 73655 None 0 Human Binding pKi = 7.2 7.2 4 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 408 6 2 7 1.5 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)NCc4ccco4)cc3)cc2n(C)c1=O 10.1021/jm0506221
CHEMBL201796 73655 None 0 Human Binding pKi = 7.2 7.2 4 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 408 6 2 7 1.5 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)NCc4ccco4)cc3)cc2n(C)c1=O 10.1021/jm0506221
44451128 161301 None 0 Human Binding pKi = 7.2 7.2 10 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 521 5 1 7 3.0 CC(Oc1ccc(-c2cc3c([nH]2)c(=O)n(C)c(=O)n3C)cc1)C(=O)N1CCN(c2ccccc2Cl)CC1 10.1016/j.bmc.2008.01.002
CHEMBL412275 161301 None 0 Human Binding pKi = 7.2 7.2 10 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 521 5 1 7 3.0 CC(Oc1ccc(-c2cc3c([nH]2)c(=O)n(C)c(=O)n3C)cc1)C(=O)N1CCN(c2ccccc2Cl)CC1 10.1016/j.bmc.2008.01.002
168281755 190905 None 0 Human Binding pKi = 7.2 7.2 - 1
Displacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cell membrane preincubated for 4 hrs followed by [3H]PSB-603 addition and measured after 0.5 hrs by radioligand displacement assayDisplacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cell membrane preincubated for 4 hrs followed by [3H]PSB-603 addition and measured after 0.5 hrs by radioligand displacement assay
ChEMBL 368 5 2 7 1.1 CCCn1c(=O)[nH]c2nc(-c3cccc(OS(=O)(=O)F)c3)[nH]c2c1=O 10.1039/d2md00132b
CHEMBL5185103 190905 None 0 Human Binding pKi = 7.2 7.2 - 1
Displacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cell membrane preincubated for 4 hrs followed by [3H]PSB-603 addition and measured after 0.5 hrs by radioligand displacement assayDisplacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cell membrane preincubated for 4 hrs followed by [3H]PSB-603 addition and measured after 0.5 hrs by radioligand displacement assay
ChEMBL 368 5 2 7 1.1 CCCn1c(=O)[nH]c2nc(-c3cccc(OS(=O)(=O)F)c3)[nH]c2c1=O 10.1039/d2md00132b
21958702 129655 None 0 Human Binding pKi = 6.2 6.2 - 1
Binding affinity for adenosine A2b receptor by using as [3H]ZM-241385 (14 nM) radioligand in membranes from HEK-A2B cellsBinding affinity for adenosine A2b receptor by using as [3H]ZM-241385 (14 nM) radioligand in membranes from HEK-A2B cells
ChEMBL 500 9 1 9 4.3 CCCn1c(=O)c2nc(-c3ccc(OCc4noc(-c5cccc(C)c5)n4)cc3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2004.11.044
CHEMBL367351 129655 None 0 Human Binding pKi = 6.2 6.2 - 1
Binding affinity for adenosine A2b receptor by using as [3H]ZM-241385 (14 nM) radioligand in membranes from HEK-A2B cellsBinding affinity for adenosine A2b receptor by using as [3H]ZM-241385 (14 nM) radioligand in membranes from HEK-A2B cells
ChEMBL 500 9 1 9 4.3 CCCn1c(=O)c2nc(-c3ccc(OCc4noc(-c5cccc(C)c5)n4)cc3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2004.11.044
11495641 139264 None 0 Human Binding pKi = 6.2 6.2 - 1
Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cellsDisplacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells
ChEMBL 428 7 1 7 2.9 CCCn1c(=O)c2nc(-c3cnn(Cc4ccc(F)cc4F)c3)[nH]c2n(CCC)c1=O 10.1021/jm051268+
CHEMBL379032 139264 None 0 Human Binding pKi = 6.2 6.2 - 1
Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cellsDisplacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells
ChEMBL 428 7 1 7 2.9 CCCn1c(=O)c2nc(-c3cnn(Cc4ccc(F)cc4F)c3)[nH]c2n(CCC)c1=O 10.1021/jm051268+
11618368 3847 None 77 Human Binding pKi = 6.2 6.2 -501 5
Inhibition of human adenosine 2B receptorInhibition of human adenosine 2B receptor
ChEMBL 406 3 2 7 2.5 COc1ccc(c2c1nc(s2)NC(=O)N1CCC(CC1)(C)O)N1CCOCC1 10.1021/acs.jmedchem.0c00237
5611 3847 None 77 Human Binding pKi = 6.2 6.2 -501 5
Inhibition of human adenosine 2B receptorInhibition of human adenosine 2B receptor
ChEMBL 406 3 2 7 2.5 COc1ccc(c2c1nc(s2)NC(=O)N1CCC(CC1)(C)O)N1CCOCC1 10.1021/acs.jmedchem.0c00237
CHEMBL2105747 3847 None 77 Human Binding pKi = 6.2 6.2 -501 5
Inhibition of human adenosine 2B receptorInhibition of human adenosine 2B receptor
ChEMBL 406 3 2 7 2.5 COc1ccc(c2c1nc(s2)NC(=O)N1CCC(CC1)(C)O)N1CCOCC1 10.1021/acs.jmedchem.0c00237
DB12203 3847 None 77 Human Binding pKi = 6.2 6.2 -501 5
Inhibition of human adenosine 2B receptorInhibition of human adenosine 2B receptor
ChEMBL 406 3 2 7 2.5 COc1ccc(c2c1nc(s2)NC(=O)N1CCC(CC1)(C)O)N1CCOCC1 10.1021/acs.jmedchem.0c00237
11618368 3847 None 77 Human Binding pKi = 6.2 6.2 -501 5
Inhibition of human recombinant adenosine receptor A2bInhibition of human recombinant adenosine receptor A2b
ChEMBL 406 3 2 7 2.5 COc1ccc(c2c1nc(s2)NC(=O)N1CCC(CC1)(C)O)N1CCOCC1 10.1021/jm4011669
5611 3847 None 77 Human Binding pKi = 6.2 6.2 -501 5
Inhibition of human recombinant adenosine receptor A2bInhibition of human recombinant adenosine receptor A2b
ChEMBL 406 3 2 7 2.5 COc1ccc(c2c1nc(s2)NC(=O)N1CCC(CC1)(C)O)N1CCOCC1 10.1021/jm4011669
CHEMBL2105747 3847 None 77 Human Binding pKi = 6.2 6.2 -501 5
Inhibition of human recombinant adenosine receptor A2bInhibition of human recombinant adenosine receptor A2b
ChEMBL 406 3 2 7 2.5 COc1ccc(c2c1nc(s2)NC(=O)N1CCC(CC1)(C)O)N1CCOCC1 10.1021/jm4011669
DB12203 3847 None 77 Human Binding pKi = 6.2 6.2 -501 5
Inhibition of human recombinant adenosine receptor A2bInhibition of human recombinant adenosine receptor A2b
ChEMBL 406 3 2 7 2.5 COc1ccc(c2c1nc(s2)NC(=O)N1CCC(CC1)(C)O)N1CCOCC1 10.1021/jm4011669
2153 3800 None 115 Human Binding pKi = 5.2 5.2 -21 14
Binding affinity for adenosine A2b receptor by using as [3H]ZM-241385 radioligand in membranes from HEK-A2B cellsBinding affinity for adenosine A2b receptor by using as [3H]ZM-241385 radioligand in membranes from HEK-A2B cells
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1016/j.bmcl.2004.11.044
2153.0 3800 None 115 Human Binding pKi = 5.2 5.2 -21 14
Binding affinity for adenosine A2b receptor by using as [3H]ZM-241385 radioligand in membranes from HEK-A2B cellsBinding affinity for adenosine A2b receptor by using as [3H]ZM-241385 radioligand in membranes from HEK-A2B cells
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1016/j.bmcl.2004.11.044
2620 3800 None 115 Human Binding pKi = 5.2 5.2 -21 14
Binding affinity for adenosine A2b receptor by using as [3H]ZM-241385 radioligand in membranes from HEK-A2B cellsBinding affinity for adenosine A2b receptor by using as [3H]ZM-241385 radioligand in membranes from HEK-A2B cells
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1016/j.bmcl.2004.11.044
413 3800 None 115 Human Binding pKi = 5.2 5.2 -21 14
Binding affinity for adenosine A2b receptor by using as [3H]ZM-241385 radioligand in membranes from HEK-A2B cellsBinding affinity for adenosine A2b receptor by using as [3H]ZM-241385 radioligand in membranes from HEK-A2B cells
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1016/j.bmcl.2004.11.044
CHEMBL190 3800 None 115 Human Binding pKi = 5.2 5.2 -21 14
Binding affinity for adenosine A2b receptor by using as [3H]ZM-241385 radioligand in membranes from HEK-A2B cellsBinding affinity for adenosine A2b receptor by using as [3H]ZM-241385 radioligand in membranes from HEK-A2B cells
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1016/j.bmcl.2004.11.044
DB00277 3800 None 115 Human Binding pKi = 5.2 5.2 -21 14
Binding affinity for adenosine A2b receptor by using as [3H]ZM-241385 radioligand in membranes from HEK-A2B cellsBinding affinity for adenosine A2b receptor by using as [3H]ZM-241385 radioligand in membranes from HEK-A2B cells
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1016/j.bmcl.2004.11.044
156014687 177260 None 0 Human Binding pKi = 6.2 6.2 - 1
Displacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting methodDisplacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting method
ChEMBL 323 3 2 6 2.6 CCOC(=O)C1=C(C)Nc2nc3ccccc3n2C1c1cc[nH]n1 10.1021/acs.jmedchem.0c00564
CHEMBL4636116 177260 None 0 Human Binding pKi = 6.2 6.2 - 1
Displacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting methodDisplacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting method
ChEMBL 323 3 2 6 2.6 CCOC(=O)C1=C(C)Nc2nc3ccccc3n2C1c1cc[nH]n1 10.1021/acs.jmedchem.0c00564
456309 160652 None 17 Human Binding pKi = 5.2 5.2 -114 4
Inhibition of human recombinant adenosine receptor A2bInhibition of human recombinant adenosine receptor A2b
ChEMBL 378 2 2 3 4.4 O[C@H](c1cc(C(F)(F)F)nc2c(C(F)(F)F)cccc12)[C@@H]1CCCCN1 10.1021/jm4011669
CHEMBL411329 160652 None 17 Human Binding pKi = 5.2 5.2 -114 4
Inhibition of human recombinant adenosine receptor A2bInhibition of human recombinant adenosine receptor A2b
ChEMBL 378 2 2 3 4.4 O[C@H](c1cc(C(F)(F)F)nc2c(C(F)(F)F)cccc12)[C@@H]1CCCCN1 10.1021/jm4011669
156009812 177060 None 0 Human Binding pKi = 6.2 6.2 -707 2
Displacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting methodDisplacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting method
ChEMBL 338 3 1 7 3.3 CC1=C(C(=O)OC(C)C)C(c2ncco2)n2c(nc3ccccc32)N1 10.1021/acs.jmedchem.0c00564
CHEMBL4632760 177060 None 0 Human Binding pKi = 6.2 6.2 -707 2
Displacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting methodDisplacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting method
ChEMBL 338 3 1 7 3.3 CC1=C(C(=O)OC(C)C)C(c2ncco2)n2c(nc3ccccc32)N1 10.1021/acs.jmedchem.0c00564
44588514 175067 None 0 Human Binding pKi = 7.2 7.2 4 2
Displacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cells
ChEMBL 369 6 2 6 2.9 CCCn1c(=O)c2[nH]c(-c3ccc(C(C)=O)cc3)c(O)c2n(CCC)c1=O 10.1016/j.bmc.2008.09.067
CHEMBL456816 175067 None 0 Human Binding pKi = 7.2 7.2 4 2
Displacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cells
ChEMBL 369 6 2 6 2.9 CCCn1c(=O)c2[nH]c(-c3ccc(C(C)=O)cc3)c(O)c2n(CCC)c1=O 10.1016/j.bmc.2008.09.067
52949999 19125 None 0 Human Binding pKi = 6.2 6.2 -1 2
Displacement of [3H]ZM241385 from human adenosine A2B receptor transfected in CHO cells after 60 mins by scintillation countingDisplacement of [3H]ZM241385 from human adenosine A2B receptor transfected in CHO cells after 60 mins by scintillation counting
ChEMBL 572 9 1 5 5.1 CN(Cc1ccc(Cl)c(Cl)c1)C(=O)COc1ccc2[nH]c(=O)c(S(C)(=O)=O)c(CCc3ccccc3)c2c1 10.1016/j.bmcl.2010.10.030
CHEMBL1289343 19125 None 0 Human Binding pKi = 6.2 6.2 -1 2
Displacement of [3H]ZM241385 from human adenosine A2B receptor transfected in CHO cells after 60 mins by scintillation countingDisplacement of [3H]ZM241385 from human adenosine A2B receptor transfected in CHO cells after 60 mins by scintillation counting
ChEMBL 572 9 1 5 5.1 CN(Cc1ccc(Cl)c(Cl)c1)C(=O)COc1ccc2[nH]c(=O)c(S(C)(=O)=O)c(CCc3ccccc3)c2c1 10.1016/j.bmcl.2010.10.030
156015964 177624 None 0 Human Binding pKi = 6.2 6.2 - 1
Displacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting methodDisplacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting method
ChEMBL 324 3 1 7 2.9 CCOC(=O)C1=C(C)Nc2nc3ccccc3n2C1c1ccno1 10.1021/acs.jmedchem.0c00564
CHEMBL4641123 177624 None 0 Human Binding pKi = 6.2 6.2 - 1
Displacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting methodDisplacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting method
ChEMBL 324 3 1 7 2.9 CCOC(=O)C1=C(C)Nc2nc3ccccc3n2C1c1ccno1 10.1021/acs.jmedchem.0c00564
72546298 103852 None 0 Human Binding pKi = 6.2 6.2 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by Scatchard plot analysisDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by Scatchard plot analysis
ChEMBL 264 4 2 4 1.9 CCOC(=O)C1=C(CC)NC(=O)NC1c1ccco1 10.1021/ml400185v
CHEMBL3091710 103852 None 0 Human Binding pKi = 6.2 6.2 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by Scatchard plot analysisDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by Scatchard plot analysis
ChEMBL 264 4 2 4 1.9 CCOC(=O)C1=C(CC)NC(=O)NC1c1ccco1 10.1021/ml400185v
46880473 6079 None 0 Human Binding pKi = 7.1 7.1 19 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 305 4 1 5 2.7 O=C(Nc1ccc(-c2ccncc2)c(-n2cccn2)n1)C1CC1 10.1016/j.bmcl.2010.01.045
CHEMBL1080679 6079 None 0 Human Binding pKi = 7.1 7.1 19 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 305 4 1 5 2.7 O=C(Nc1ccc(-c2ccncc2)c(-n2cccn2)n1)C1CC1 10.1016/j.bmcl.2010.01.045
11531449 72251 None 0 Human Binding pKi = 7.1 7.1 12 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 401 9 2 7 1.7 CCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)O)cc3)cc2n(CCCOC)c1=O 10.1021/jm0506221
CHEMBL198191 72251 None 0 Human Binding pKi = 7.1 7.1 12 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 401 9 2 7 1.7 CCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)O)cc3)cc2n(CCCOC)c1=O 10.1021/jm0506221
44437214 169254 None 0 Human Binding pKi = 5.1 5.1 -31 6
Displacement of [3H]ZM-241385 from human adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]ZM-241385 from human adenosine A2B receptor expressed in CHO cells
ChEMBL 355 3 1 8 0.6 Cn1c(=O)c2c(nc3n2CCCN3CCc2ccc(O)cc2)n(C)c1=O 10.1016/j.bmc.2007.07.051
CHEMBL441145 169254 None 0 Human Binding pKi = 5.1 5.1 -31 6
Displacement of [3H]ZM-241385 from human adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]ZM-241385 from human adenosine A2B receptor expressed in CHO cells
ChEMBL 355 3 1 8 0.6 Cn1c(=O)c2c(nc3n2CCCN3CCc2ccc(O)cc2)n(C)c1=O 10.1016/j.bmc.2007.07.051
9834769 157246 None 2 Human Binding pKi = 6.1 6.1 -457 4
Binding affinity at human adenosine A2B receptorBinding affinity at human adenosine A2B receptor
ChEMBL 247 2 0 5 3.4 CCc1nc(-c2nccs2)c2sccc2n1 10.1016/j.bmcl.2008.03.076
CHEMBL407650 157246 None 2 Human Binding pKi = 6.1 6.1 -457 4
Binding affinity at human adenosine A2B receptorBinding affinity at human adenosine A2B receptor
ChEMBL 247 2 0 5 3.4 CCc1nc(-c2nccs2)c2sccc2n1 10.1016/j.bmcl.2008.03.076
156019063 177837 None 0 Human Binding pKi = 6.1 6.1 - 1
Displacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting methodDisplacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting method
ChEMBL 338 3 1 7 3.3 CC1=C(C(=O)OC(C)C)C(c2ccon2)n2c(nc3ccccc32)N1 10.1021/acs.jmedchem.0c00564
CHEMBL4644043 177837 None 0 Human Binding pKi = 6.1 6.1 - 1
Displacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting methodDisplacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting method
ChEMBL 338 3 1 7 3.3 CC1=C(C(=O)OC(C)C)C(c2ccon2)n2c(nc3ccccc32)N1 10.1021/acs.jmedchem.0c00564
162667072 182409 None 0 Human Binding pKi = 6.1 6.1 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 292 4 2 4 2.3 CC1=C(C(=O)OCC2CC2)C(c2ccsc2)NC(=O)N1 10.1021/acs.jmedchem.0c01431
CHEMBL4785646 182409 None 0 Human Binding pKi = 6.1 6.1 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 292 4 2 4 2.3 CC1=C(C(=O)OCC2CC2)C(c2ccsc2)NC(=O)N1 10.1021/acs.jmedchem.0c01431
127030660 139030 None 0 Human Binding pKi = 6.1 6.1 - 1
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 minsDisplacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 mins
ChEMBL 303 3 1 6 3.2 CC1=C(C(=O)OC(C)C)C(c2cccs2)n2ccnc2N1 10.1021/acs.jmedchem.5b01586
CHEMBL3785876 139030 None 0 Human Binding pKi = 6.1 6.1 - 1
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 minsDisplacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 mins
ChEMBL 303 3 1 6 3.2 CC1=C(C(=O)OC(C)C)C(c2cccs2)n2ccnc2N1 10.1021/acs.jmedchem.5b01586
22266730 94563 None 0 Human Binding pKi = 7.1 7.1 29 2
Displacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranesDisplacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranes
ChEMBL 354 4 2 6 1.5 CCn1c(=O)[nH]c2nc(-c3cnn(Cc4cccc(F)c4)c3)[nH]c2c1=O 10.1016/j.bmcl.2008.01.008
CHEMBL251875 94563 None 0 Human Binding pKi = 7.1 7.1 29 2
Displacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranesDisplacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranes
ChEMBL 354 4 2 6 1.5 CCn1c(=O)[nH]c2nc(-c3cnn(Cc4cccc(F)c4)c3)[nH]c2c1=O 10.1016/j.bmcl.2008.01.008
1329 1472 None 86 Human Binding pKi = 7.1 7.1 -1288 14
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes after 30 minsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes after 30 mins
ChEMBL 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 10.1021/acs.jmedchem.7b00138
386 1472 None 86 Human Binding pKi = 7.1 7.1 -1288 14
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes after 30 minsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes after 30 mins
ChEMBL 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 10.1021/acs.jmedchem.7b00138
CHEMBL183 1472 None 86 Human Binding pKi = 7.1 7.1 -1288 14
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes after 30 minsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes after 30 mins
ChEMBL 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 10.1021/acs.jmedchem.7b00138
DB12946 1472 None 86 Human Binding pKi = 7.1 7.1 -1288 14
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes after 30 minsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes after 30 mins
ChEMBL 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 10.1021/acs.jmedchem.7b00138
15667089 4617 None 0 Human Binding pKi = 7.1 7.1 -33 5
Displacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assayDisplacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assay
ChEMBL 276 3 1 5 1.6 CCn1c(=O)c2nc(C3CCCC3)[nH]c2n(CC)c1=O 10.1021/acs.jmedchem.9b01340
CHEMBL102859 4617 None 0 Human Binding pKi = 7.1 7.1 -33 5
Displacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assayDisplacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assay
ChEMBL 276 3 1 5 1.6 CCn1c(=O)c2nc(C3CCCC3)[nH]c2n(CC)c1=O 10.1021/acs.jmedchem.9b01340
1329 1472 None 86 Human Binding pKi = 7.1 7.1 -1288 14
Displacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting methodDisplacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting method
ChEMBL 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 10.1021/acs.jmedchem.0c00564
386 1472 None 86 Human Binding pKi = 7.1 7.1 -1288 14
Displacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting methodDisplacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting method
ChEMBL 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 10.1021/acs.jmedchem.0c00564
CHEMBL183 1472 None 86 Human Binding pKi = 7.1 7.1 -1288 14
Displacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting methodDisplacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting method
ChEMBL 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 10.1021/acs.jmedchem.0c00564
DB12946 1472 None 86 Human Binding pKi = 7.1 7.1 -1288 14
Displacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting methodDisplacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting method
ChEMBL 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 10.1021/acs.jmedchem.0c00564
1329 1472 None 86 Human Binding pKi = 7.1 7.1 -1288 14
Displacement of [3H]DPCPX from human A2BAR expressed in HEK293 cell membrane incubated for 30 mins by microbeta trilux scintillation counter analysisDisplacement of [3H]DPCPX from human A2BAR expressed in HEK293 cell membrane incubated for 30 mins by microbeta trilux scintillation counter analysis
ChEMBL 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 10.1021/acs.jmedchem.1c01636
386 1472 None 86 Human Binding pKi = 7.1 7.1 -1288 14
Displacement of [3H]DPCPX from human A2BAR expressed in HEK293 cell membrane incubated for 30 mins by microbeta trilux scintillation counter analysisDisplacement of [3H]DPCPX from human A2BAR expressed in HEK293 cell membrane incubated for 30 mins by microbeta trilux scintillation counter analysis
ChEMBL 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 10.1021/acs.jmedchem.1c01636
CHEMBL183 1472 None 86 Human Binding pKi = 7.1 7.1 -1288 14
Displacement of [3H]DPCPX from human A2BAR expressed in HEK293 cell membrane incubated for 30 mins by microbeta trilux scintillation counter analysisDisplacement of [3H]DPCPX from human A2BAR expressed in HEK293 cell membrane incubated for 30 mins by microbeta trilux scintillation counter analysis
ChEMBL 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 10.1021/acs.jmedchem.1c01636
DB12946 1472 None 86 Human Binding pKi = 7.1 7.1 -1288 14
Displacement of [3H]DPCPX from human A2BAR expressed in HEK293 cell membrane incubated for 30 mins by microbeta trilux scintillation counter analysisDisplacement of [3H]DPCPX from human A2BAR expressed in HEK293 cell membrane incubated for 30 mins by microbeta trilux scintillation counter analysis
ChEMBL 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 10.1021/acs.jmedchem.1c01636
1329 1472 None 86 Human Binding pKi = 7.1 7.1 -1288 14
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 minsDisplacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 mins
ChEMBL 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 10.1021/acs.jmedchem.5b01586
386 1472 None 86 Human Binding pKi = 7.1 7.1 -1288 14
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 minsDisplacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 mins
ChEMBL 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 10.1021/acs.jmedchem.5b01586
CHEMBL183 1472 None 86 Human Binding pKi = 7.1 7.1 -1288 14
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 minsDisplacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 mins
ChEMBL 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 10.1021/acs.jmedchem.5b01586
DB12946 1472 None 86 Human Binding pKi = 7.1 7.1 -1288 14
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 minsDisplacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 mins
ChEMBL 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 10.1021/acs.jmedchem.5b01586
CHEMBL5074986 214348 None 0 Human Binding pKi = 7.1 7.1 -15 3
Displacement of [3H]DPCPX from human A2BAR expressed in HEK293 cell membrane incubated for 30 mins by microbeta trilux scintillation counter analysisDisplacement of [3H]DPCPX from human A2BAR expressed in HEK293 cell membrane incubated for 30 mins by microbeta trilux scintillation counter analysis
ChEMBL None None None N#Cc1c(-c2cccc(Cl)c2)nc(N)nc1-c1cccc(Cl)c1 10.1021/acs.jmedchem.1c01636
155542822 173167 None 0 Human Binding pKi = 6.1 6.1 - 1
Displacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assayDisplacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assay
ChEMBL 377 3 1 6 4.0 CCOC(=O)C1=C(C(F)(F)F)Nc2nc3ccccc3n2C1c1ccco1 10.1021/acs.jmedchem.9b01340
CHEMBL4521818 173167 None 0 Human Binding pKi = 6.1 6.1 - 1
Displacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assayDisplacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assay
ChEMBL 377 3 1 6 4.0 CCOC(=O)C1=C(C(F)(F)F)Nc2nc3ccccc3n2C1c1ccco1 10.1021/acs.jmedchem.9b01340
1329 1472 None 86 Human Binding pKi = 5.1 5.1 -1288 14
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 10.1021/acs.jmedchem.0c01431
386 1472 None 86 Human Binding pKi = 5.1 5.1 -1288 14
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 10.1021/acs.jmedchem.0c01431
CHEMBL183 1472 None 86 Human Binding pKi = 5.1 5.1 -1288 14
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 10.1021/acs.jmedchem.0c01431
DB12946 1472 None 86 Human Binding pKi = 5.1 5.1 -1288 14
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 10.1021/acs.jmedchem.0c01431
162671640 182855 None 0 Human Binding pKi = 6.1 6.1 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 290 4 2 4 2.3 CC1=C(C(=O)OCC2CCC2)C(c2ccoc2)NC(=O)N1 10.1021/acs.jmedchem.0c01431
CHEMBL4791578 182855 None 0 Human Binding pKi = 6.1 6.1 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 290 4 2 4 2.3 CC1=C(C(=O)OCC2CCC2)C(c2ccoc2)NC(=O)N1 10.1021/acs.jmedchem.0c01431
135421366 108967 None 0 Human Binding pKi = 7.1 7.1 13 2
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 521 11 2 9 3.6 CCCn1c(=O)c2nc(-c3cc(OCC(=O)Nc4ccc(C(C)CC)cc4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
CHEMBL32118 108967 None 0 Human Binding pKi = 7.1 7.1 13 2
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 521 11 2 9 3.6 CCCn1c(=O)c2nc(-c3cc(OCC(=O)Nc4ccc(C(C)CC)cc4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
44406592 72872 None 0 Human Binding pKi = 7.1 7.1 4 3
Displacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cellsDisplacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cells
ChEMBL 528 8 1 10 3.7 CCCn1c(=O)c2nc(-c3cnn(Cc4nc(-c5ccccc5C(F)(F)F)no4)c3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2005.10.002
CHEMBL200313 72872 None 0 Human Binding pKi = 7.1 7.1 4 3
Displacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cellsDisplacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cells
ChEMBL 528 8 1 10 3.7 CCCn1c(=O)c2nc(-c3cnn(Cc4nc(-c5ccccc5C(F)(F)F)no4)c3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2005.10.002
11711190 77791 None 0 Human Binding pKi = 7.1 7.1 -4 3
Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cellsDisplacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells
ChEMBL 406 8 1 7 2.8 CCCn1c(=O)c2nc(-c3cnn(CCc4ccccc4)c3)[nH]c2n(CCC)c1=O 10.1021/jm051268+
CHEMBL209217 77791 None 0 Human Binding pKi = 7.1 7.1 -4 3
Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cellsDisplacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells
ChEMBL 406 8 1 7 2.8 CCCn1c(=O)c2nc(-c3cnn(CCc4ccccc4)c3)[nH]c2n(CCC)c1=O 10.1021/jm051268+
21874581 169615 None 0 Human Binding pKi = 6.1 6.1 -138 4
Displacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation countingDisplacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation counting
ChEMBL 322 4 1 8 2.1 COc1ccccc1Cn1nnc2c(-c3ccco3)nc(N)nc21 10.1021/jm800961g
CHEMBL443665 169615 None 0 Human Binding pKi = 6.1 6.1 -138 4
Displacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation countingDisplacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation counting
ChEMBL 322 4 1 8 2.1 COc1ccccc1Cn1nnc2c(-c3ccco3)nc(N)nc21 10.1021/jm800961g
9497523 181359 None 0 Human Binding pKi = 7.1 7.1 -53 3
Displacement of [3H]MRS1754 from human adenosine A2B receptor expressed in CHO cell membraneDisplacement of [3H]MRS1754 from human adenosine A2B receptor expressed in CHO cell membrane
ChEMBL 267 2 1 5 3.5 N#Cc1c(-c2cccs2)cc(-c2ccco2)nc1N 10.1021/jm701594y
CHEMBL476311 181359 None 0 Human Binding pKi = 7.1 7.1 -53 3
Displacement of [3H]MRS1754 from human adenosine A2B receptor expressed in CHO cell membraneDisplacement of [3H]MRS1754 from human adenosine A2B receptor expressed in CHO cell membrane
ChEMBL 267 2 1 5 3.5 N#Cc1c(-c2cccs2)cc(-c2ccco2)nc1N 10.1021/jm701594y
156020575 178065 None 0 Human Binding pKi = 6.1 6.1 - 1
Displacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting methodDisplacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting method
ChEMBL 354 3 1 7 3.7 CC1=C(C(=O)OC(C)C)C(c2nccs2)n2c(nc3ccccc32)N1 10.1021/acs.jmedchem.0c00564
CHEMBL4647365 178065 None 0 Human Binding pKi = 6.1 6.1 - 1
Displacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting methodDisplacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting method
ChEMBL 354 3 1 7 3.7 CC1=C(C(=O)OC(C)C)C(c2nccs2)n2c(nc3ccccc32)N1 10.1021/acs.jmedchem.0c00564
11426423 195101 None 0 Human Binding pKi = 6.1 6.1 -177 4
Binding affinity to adenosine A2B receptorBinding affinity to adenosine A2B receptor
ChEMBL 295 4 2 6 1.6 Nc1nc(C(=O)NCc2ccccn2)cc(-c2ccco2)n1 10.1016/j.bmcl.2009.03.142
CHEMBL549885 195101 None 0 Human Binding pKi = 6.1 6.1 -177 4
Binding affinity to adenosine A2B receptorBinding affinity to adenosine A2B receptor
ChEMBL 295 4 2 6 1.6 Nc1nc(C(=O)NCc2ccccn2)cc(-c2ccco2)n1 10.1016/j.bmcl.2009.03.142
11850015 80160 None 0 Human Binding pKi = 5.1 5.1 -72 2
Displacement of [3H]DPCPX from human adenosine A2b receptor expressed in HEK293 cells after 30 minsDisplacement of [3H]DPCPX from human adenosine A2b receptor expressed in HEK293 cells after 30 mins
ChEMBL 367 3 0 6 3.5 Cc1nn(Cc2ccccc2)c(=O)c2ncn3nc(-c4ccccc4)cc3c12 10.1016/j.bmc.2010.09.043
CHEMBL213425 80160 None 0 Human Binding pKi = 5.1 5.1 -72 2
Displacement of [3H]DPCPX from human adenosine A2b receptor expressed in HEK293 cells after 30 minsDisplacement of [3H]DPCPX from human adenosine A2b receptor expressed in HEK293 cells after 30 mins
ChEMBL 367 3 0 6 3.5 Cc1nn(Cc2ccccc2)c(=O)c2ncn3nc(-c4ccccc4)cc3c12 10.1016/j.bmc.2010.09.043
19074239 203856 None 6 Human Binding pKi = 5.1 5.1 -6 2
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 320 10 1 5 3.0 CCCCCCn1c(=O)c2nc[nH]c2n(CCCCCC)c1=O 10.1021/jm0104318
CHEMBL68660 203856 None 6 Human Binding pKi = 5.1 5.1 -6 2
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 320 10 1 5 3.0 CCCCCCn1c(=O)c2nc[nH]c2n(CCCCCC)c1=O 10.1021/jm0104318
135522362 100021 None 0 Human Binding pKi = 7.1 7.1 - 1
Binding affinity of compound for displacement of [3H]DPCPX binding in HEK293 membranes expressing human A2B adenosine receptorsBinding affinity of compound for displacement of [3H]DPCPX binding in HEK293 membranes expressing human A2B adenosine receptors
ChEMBL 472 8 1 10 0.3 CCCn1c(=O)c2nc(-c3cc(OCC(=O)N4CCN(C)CC4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
CHEMBL286838 100021 None 0 Human Binding pKi = 7.1 7.1 - 1
Binding affinity of compound for displacement of [3H]DPCPX binding in HEK293 membranes expressing human A2B adenosine receptorsBinding affinity of compound for displacement of [3H]DPCPX binding in HEK293 membranes expressing human A2B adenosine receptors
ChEMBL 472 8 1 10 0.3 CCCn1c(=O)c2nc(-c3cc(OCC(=O)N4CCN(C)CC4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
135522362 100021 None 0 Human Binding pKi = 7.1 7.1 - 1
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 472 8 1 10 0.3 CCCn1c(=O)c2nc(-c3cc(OCC(=O)N4CCN(C)CC4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
CHEMBL286838 100021 None 0 Human Binding pKi = 7.1 7.1 - 1
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 472 8 1 10 0.3 CCCn1c(=O)c2nc(-c3cc(OCC(=O)N4CCN(C)CC4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
10895416 57185 None 0 Human Binding pKi = 7.1 7.1 -7 4
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 56-103Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 56-103
ChEMBL 436 5 2 8 4.4 CCCn1cc2c(nc(NC(=O)Nc3ccc(Cl)cc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm0109614
CHEMBL164905 57185 None 0 Human Binding pKi = 7.1 7.1 -7 4
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 56-103Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 56-103
ChEMBL 436 5 2 8 4.4 CCCn1cc2c(nc(NC(=O)Nc3ccc(Cl)cc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm0109614
136042345 71171 None 0 Human Binding pKi = 7.1 7.1 - 1
Displacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation countingDisplacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation counting
ChEMBL 585 8 2 9 4.9 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5c(C(F)(F)F)cc(C(F)(F)F)cc5[nH]4)no3)nc2n(CCC)c1=O 10.1021/jm201292w
CHEMBL1955921 71171 None 0 Human Binding pKi = 7.1 7.1 - 1
Displacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation countingDisplacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation counting
ChEMBL 585 8 2 9 4.9 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5c(C(F)(F)F)cc(C(F)(F)F)cc5[nH]4)no3)nc2n(CCC)c1=O 10.1021/jm201292w
11438116 84667 None 4 Human Binding pKi = 7.1 7.1 -5 4
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 303 4 1 3 4.2 CCC(=O)Nc1cc(-c2ccccc2)nc(-c2ccccc2)n1 10.1021/jm100843z
CHEMBL222474 84667 None 4 Human Binding pKi = 7.1 7.1 -5 4
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 303 4 1 3 4.2 CCC(=O)Nc1cc(-c2ccccc2)nc(-c2ccccc2)n1 10.1021/jm100843z
377 2758 None 53 Human Binding pKi = 6.1 6.1 -1479 15
Inhibition of [3H]DPCPX binding to human adenosine A2B receptor expressed in HEK293 cellsInhibition of [3H]DPCPX binding to human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm031143+
425 2758 None 53 Human Binding pKi = 6.1 6.1 -1479 15
Inhibition of [3H]DPCPX binding to human adenosine A2B receptor expressed in HEK293 cellsInhibition of [3H]DPCPX binding to human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm031143+
448222 2758 None 53 Human Binding pKi = 6.1 6.1 -1479 15
Inhibition of [3H]DPCPX binding to human adenosine A2B receptor expressed in HEK293 cellsInhibition of [3H]DPCPX binding to human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm031143+
CHEMBL464859 2758 None 53 Human Binding pKi = 6.1 6.1 -1479 15
Inhibition of [3H]DPCPX binding to human adenosine A2B receptor expressed in HEK293 cellsInhibition of [3H]DPCPX binding to human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1021/jm031143+
44410550 76260 None 0 Human Binding pKi = 5.1 5.1 -5888 4
Displacement of [125I]ABOPX from human adenosine A2B receptor in HEK cellsDisplacement of [125I]ABOPX from human adenosine A2B receptor in HEK cells
ChEMBL 511 7 5 12 0.0 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC)nc(C#CC(O)c4ccccc4[N+](=O)[O-])nc32)[C@H](O)[C@@H]1O 10.1016/j.bmcl.2006.01.110
CHEMBL205850 76260 None 0 Human Binding pKi = 5.1 5.1 -5888 4
Displacement of [125I]ABOPX from human adenosine A2B receptor in HEK cellsDisplacement of [125I]ABOPX from human adenosine A2B receptor in HEK cells
ChEMBL 511 7 5 12 0.0 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC)nc(C#CC(O)c4ccccc4[N+](=O)[O-])nc32)[C@H](O)[C@@H]1O 10.1016/j.bmcl.2006.01.110
156019196 177953 None 0 Human Binding pKi = 6.1 6.1 -389 2
Displacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting methodDisplacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting method
ChEMBL 324 3 1 7 2.9 CCOC(=O)C1=C(C)Nc2nc3ccccc3n2C1c1ncco1 10.1021/acs.jmedchem.0c00564
CHEMBL4645754 177953 None 0 Human Binding pKi = 6.1 6.1 -389 2
Displacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting methodDisplacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting method
ChEMBL 324 3 1 7 2.9 CCOC(=O)C1=C(C)Nc2nc3ccccc3n2C1c1ncco1 10.1021/acs.jmedchem.0c00564
66892978 159228 None 0 Human Binding pKi = 7.1 7.1 - 1
Displacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting methodDisplacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting method
ChEMBL 519 9 2 9 2.3 CCCn1c(=O)c2[nH]c(-c3cnn(CC4CC(=O)N(c5ccc(C(=O)O)cc5)C4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2016.11.007
CHEMBL4098853 159228 None 0 Human Binding pKi = 7.1 7.1 - 1
Displacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting methodDisplacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting method
ChEMBL 519 9 2 9 2.3 CCCn1c(=O)c2[nH]c(-c3cnn(CC4CC(=O)N(c5ccc(C(=O)O)cc5)C4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2016.11.007
45269706 196072 None 0 Human Binding pKi = 7.1 7.1 1 2
Binding affinity to human adenosine A2b receptor expressed in HEK293 cellsBinding affinity to human adenosine A2b receptor expressed in HEK293 cells
ChEMBL 469 10 2 8 2.0 CCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)NC4CCCC4)cc3)nc2n(CCCOC)c1=O 10.1016/j.bmc.2009.03.029
CHEMBL560623 196072 None 0 Human Binding pKi = 7.1 7.1 1 2
Binding affinity to human adenosine A2b receptor expressed in HEK293 cellsBinding affinity to human adenosine A2b receptor expressed in HEK293 cells
ChEMBL 469 10 2 8 2.0 CCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)NC4CCCC4)cc3)nc2n(CCCOC)c1=O 10.1016/j.bmc.2009.03.029
11555937 140422 None 0 Human Binding pKi = 7.1 7.1 - 1
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 564 11 2 7 5.2 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(C(=O)c5ccccc5)cc4)cc3)cc2n(CCC)c1=O 10.1021/jm0506221
CHEMBL380901 140422 None 0 Human Binding pKi = 7.1 7.1 - 1
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 564 11 2 7 5.2 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(C(=O)c5ccccc5)cc4)cc3)cc2n(CCC)c1=O 10.1021/jm0506221
135416050 100106 None 0 Human Binding pKi = 7.1 7.1 - 1
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 494 9 2 10 2.2 CCCn1c(=O)c2nc(-c3cc(NC(=O)Cc4ccc([N+](=O)[O-])cc4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
CHEMBL287493 100106 None 0 Human Binding pKi = 7.1 7.1 - 1
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 494 9 2 10 2.2 CCCn1c(=O)c2nc(-c3cc(NC(=O)Cc4ccc([N+](=O)[O-])cc4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
135529373 112367 None 0 Human Binding pKi = 7.1 7.1 24 2
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 485 8 2 8 2.6 CCCn1c(=O)c2nc(-c3cc(NC(=O)Cc4ccc(F)c(F)c4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
CHEMBL32950 112367 None 0 Human Binding pKi = 7.1 7.1 24 2
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 485 8 2 8 2.6 CCCn1c(=O)c2nc(-c3cc(NC(=O)Cc4ccc(F)c(F)c4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
10994183 120232 None 0 Human Binding pKi = 7.1 7.1 -154 4
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 57-105Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 57-105
ChEMBL 460 6 2 10 3.9 CCCCn1cc2c(nc(NC(=O)Nc3ccc4c(c3)OCO4)n3nc(-c4ccco4)nc23)n1 10.1021/jm0109614
CHEMBL352192 120232 None 0 Human Binding pKi = 7.1 7.1 -154 4
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 57-105Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 57-105
ChEMBL 460 6 2 10 3.9 CCCCn1cc2c(nc(NC(=O)Nc3ccc4c(c3)OCO4)n3nc(-c4ccco4)nc23)n1 10.1021/jm0109614
11091632 119959 None 0 Human Binding pKi = 7.1 7.1 -2 4
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 65-94Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 65-94
ChEMBL 450 6 2 8 4.8 CCCCn1cc2c(nc(NC(=O)Nc3ccccc3Cl)n3nc(-c4ccco4)nc23)n1 10.1021/jm0109614
CHEMBL349716 119959 None 0 Human Binding pKi = 7.1 7.1 -2 4
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 65-94Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 65-94
ChEMBL 450 6 2 8 4.8 CCCCn1cc2c(nc(NC(=O)Nc3ccccc3Cl)n3nc(-c4ccco4)nc23)n1 10.1021/jm0109614
46880421 6373 None 0 Human Binding pKi = 7.1 7.1 4 4
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 322 4 1 5 3.6 O=C(Nc1ccc(-c2ccncc2)c(-c2cncs2)n1)C1CC1 10.1016/j.bmcl.2010.01.045
CHEMBL1082171 6373 None 0 Human Binding pKi = 7.1 7.1 4 4
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 322 4 1 5 3.6 O=C(Nc1ccc(-c2ccncc2)c(-c2cncs2)n1)C1CC1 10.1016/j.bmcl.2010.01.045
2153 3800 None 115 Human Binding pKi = 5.1 5.1 -21 14
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1021/jm900413e
2153.0 3800 None 115 Human Binding pKi = 5.1 5.1 -21 14
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1021/jm900413e
2620 3800 None 115 Human Binding pKi = 5.1 5.1 -21 14
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1021/jm900413e
413 3800 None 115 Human Binding pKi = 5.1 5.1 -21 14
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1021/jm900413e
CHEMBL190 3800 None 115 Human Binding pKi = 5.1 5.1 -21 14
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1021/jm900413e
DB00277 3800 None 115 Human Binding pKi = 5.1 5.1 -21 14
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1021/jm900413e
156018198 177831 None 0 Human Binding pKi = 6.1 6.1 - 1
Displacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting methodDisplacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting method
ChEMBL 324 3 1 7 2.9 CCOC(=O)C1=C(C)Nc2nc3ccccc3n2C1c1ccon1 10.1021/acs.jmedchem.0c00564
CHEMBL4643944 177831 None 0 Human Binding pKi = 6.1 6.1 - 1
Displacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting methodDisplacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting method
ChEMBL 324 3 1 7 2.9 CCOC(=O)C1=C(C)Nc2nc3ccccc3n2C1c1ccon1 10.1021/acs.jmedchem.0c00564
137645670 157999 None 0 Human Binding pKi = 7.1 7.1 - 1
Displacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 minsDisplacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 mins
ChEMBL 424 6 2 8 1.9 CCCn1c(=O)c2[nH]c(-c3cnn(CC#CC4(O)CCCC4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2017.04.014
CHEMBL4085353 157999 None 0 Human Binding pKi = 7.1 7.1 - 1
Displacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 minsDisplacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 mins
ChEMBL 424 6 2 8 1.9 CCCn1c(=O)c2[nH]c(-c3cnn(CC#CC4(O)CCCC4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2017.04.014
21874603 178586 None 0 Human Binding pKi = 7.1 7.1 -34 4
Displacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation countingDisplacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation counting
ChEMBL 328 3 1 7 2.4 Nc1nc(-c2ccco2)c2nnn(Cc3cccc(F)c3F)c2n1 10.1021/jm800961g
CHEMBL467244 178586 None 0 Human Binding pKi = 7.1 7.1 -34 4
Displacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation countingDisplacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation counting
ChEMBL 328 3 1 7 2.4 Nc1nc(-c2ccco2)c2nnn(Cc3cccc(F)c3F)c2n1 10.1021/jm800961g
11561747 73090 None 0 Human Binding pKi = 7.1 7.1 6 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 463 8 2 6 3.2 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)O)cc3)c(Br)c2n(CCC)c1=O 10.1021/jm0506221
CHEMBL201108 73090 None 0 Human Binding pKi = 7.1 7.1 6 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 463 8 2 6 3.2 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)O)cc3)c(Br)c2n(CCC)c1=O 10.1021/jm0506221
11524078 73542 None 0 Human Binding pKi = 7.1 7.1 8 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 396 5 2 6 1.7 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)NC4CCCC4)cc3)cc2n(C)c1=O 10.1021/jm0506221
CHEMBL201745 73542 None 0 Human Binding pKi = 7.1 7.1 8 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 396 5 2 6 1.7 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)NC4CCCC4)cc3)cc2n(C)c1=O 10.1021/jm0506221
155525396 171090 None 0 Human Binding pKi = 7.1 7.1 -7 4
Displacement of [3H]DPCPX from human A2B receptor expressed in HEK-293-A2B cells incubated for 30 mins by scintillation counting method based radioligand competitive binding assayDisplacement of [3H]DPCPX from human A2B receptor expressed in HEK-293-A2B cells incubated for 30 mins by scintillation counting method based radioligand competitive binding assay
ChEMBL 295 2 2 5 2.7 Oc1ccc(-c2nc(N3CCCCC3)c3nc[nH]c3n2)cc1 10.1016/j.bmc.2019.06.034
CHEMBL4457537 171090 None 0 Human Binding pKi = 7.1 7.1 -7 4
Displacement of [3H]DPCPX from human A2B receptor expressed in HEK-293-A2B cells incubated for 30 mins by scintillation counting method based radioligand competitive binding assayDisplacement of [3H]DPCPX from human A2B receptor expressed in HEK-293-A2B cells incubated for 30 mins by scintillation counting method based radioligand competitive binding assay
ChEMBL 295 2 2 5 2.7 Oc1ccc(-c2nc(N3CCCCC3)c3nc[nH]c3n2)cc1 10.1016/j.bmc.2019.06.034
46837703 10593 None 0 Human Binding pKi = 7.1 7.1 - 1
Displacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells after 30 minsDisplacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells after 30 mins
ChEMBL 458 6 2 5 3.1 CCCn1c(=O)[nH]c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCc5ccccc5C4)cc3)cc21 10.1016/j.ejmech.2010.03.011
CHEMBL1169972 10593 None 0 Human Binding pKi = 7.1 7.1 - 1
Displacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells after 30 minsDisplacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells after 30 mins
ChEMBL 458 6 2 5 3.1 CCCn1c(=O)[nH]c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCc5ccccc5C4)cc3)cc21 10.1016/j.ejmech.2010.03.011
14000474 51000 None 0 Human Binding pKi = 7.1 7.1 - 1
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 314 5 1 7 1.2 CCCn1c(=O)c2nc(-c3cnccn3)[nH]c2n(CCC)c1=O 10.1021/jm0104318
CHEMBL157836 51000 None 0 Human Binding pKi = 7.1 7.1 - 1
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 314 5 1 7 1.2 CCCn1c(=O)c2nc(-c3cnccn3)[nH]c2n(CCC)c1=O 10.1021/jm0104318
44410697 77285 None 0 Human Binding pKi = 5.1 5.1 -4265 4
Displacement of [125I]ABOPX from human adenosine A2B receptor in HEK cellsDisplacement of [125I]ABOPX from human adenosine A2B receptor in HEK cells
ChEMBL 458 6 5 10 -0.1 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC)nc(C#CC(O)C4CCCC4)nc32)[C@H](O)[C@@H]1O 10.1016/j.bmcl.2006.01.110
CHEMBL208160 77285 None 0 Human Binding pKi = 5.1 5.1 -4265 4
Displacement of [125I]ABOPX from human adenosine A2B receptor in HEK cellsDisplacement of [125I]ABOPX from human adenosine A2B receptor in HEK cells
ChEMBL 458 6 5 10 -0.1 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC)nc(C#CC(O)C4CCCC4)nc32)[C@H](O)[C@@H]1O 10.1016/j.bmcl.2006.01.110
44520982 199848 None 0 Human Binding pKi = 6.1 6.1 -794 4
Displacement of radioligand from human adenosine A2B receptor expressed in cells by topcount microplate scintillation countingDisplacement of radioligand from human adenosine A2B receptor expressed in cells by topcount microplate scintillation counting
ChEMBL 298 4 3 6 1.3 Cc1ccc(-c2cc(C(=O)NCc3ncc[nH]3)nc(N)n2)o1 10.1016/j.bmc.2009.07.078
CHEMBL594363 199848 None 0 Human Binding pKi = 6.1 6.1 -794 4
Displacement of radioligand from human adenosine A2B receptor expressed in cells by topcount microplate scintillation countingDisplacement of radioligand from human adenosine A2B receptor expressed in cells by topcount microplate scintillation counting
ChEMBL 298 4 3 6 1.3 Cc1ccc(-c2cc(C(=O)NCc3ncc[nH]3)nc(N)n2)o1 10.1016/j.bmc.2009.07.078
69030489 159446 None 0 Human Binding pKi = 8.1 8.1 - 1
Displacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting methodDisplacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting method
ChEMBL 489 8 1 8 2.9 CCCn1c(=O)c2[nH]c(-c3cnn(CC4CC(=O)N(c5ccc(C)cc5)C4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2016.11.007
CHEMBL4101208 159446 None 0 Human Binding pKi = 8.1 8.1 - 1
Displacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting methodDisplacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting method
ChEMBL 489 8 1 8 2.9 CCCn1c(=O)c2[nH]c(-c3cnn(CC4CC(=O)N(c5ccc(C)cc5)C4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2016.11.007
10158974 155506 None 0 Human Binding pKi = 8.1 8.1 -1 3
Displacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranesDisplacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranes
ChEMBL 418 5 2 6 2.8 CCCn1c(=O)[nH]c2nc(-c3cnn(Cc4cccc(C(F)(F)F)c4)c3)[nH]c2c1=O 10.1016/j.bmcl.2008.01.008
CHEMBL404168 155506 None 0 Human Binding pKi = 8.1 8.1 -1 3
Displacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranesDisplacement of [3H]-ZM241385 from human A2B receptor expressed in HEK293 cell membranes
ChEMBL 418 5 2 6 2.8 CCCn1c(=O)[nH]c2nc(-c3cnn(Cc4cccc(C(F)(F)F)c4)c3)[nH]c2c1=O 10.1016/j.bmcl.2008.01.008
11952670 6336 None 0 Human Binding pKi = 8.1 8.1 44 3
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 278 2 2 6 2.3 Nc1n[nH]c2nc(-c3ccco3)c(-c3ccncn3)cc12 10.1016/j.bmcl.2010.01.077
CHEMBL1082001 6336 None 0 Human Binding pKi = 8.1 8.1 44 3
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 278 2 2 6 2.3 Nc1n[nH]c2nc(-c3ccco3)c(-c3ccncn3)cc12 10.1016/j.bmcl.2010.01.077
46911060 10648 None 0 Human Binding pKi = 8.1 8.1 6 4
Displacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cells after 1 hrDisplacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cells after 1 hr
ChEMBL 373 5 1 7 2.7 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccnn3C)sc12 10.1016/j.bmcl.2011.02.053
CHEMBL1170367 10648 None 0 Human Binding pKi = 8.1 8.1 6 4
Displacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cells after 1 hrDisplacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cells after 1 hr
ChEMBL 373 5 1 7 2.7 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccnn3C)sc12 10.1016/j.bmcl.2011.02.053
46911060 10648 None 0 Human Binding pKi = 8.1 8.1 6 4
Displacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cells after 1 hr by scintillation countingDisplacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 373 5 1 7 2.7 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccnn3C)sc12 10.1016/j.bmcl.2010.05.056
CHEMBL1170367 10648 None 0 Human Binding pKi = 8.1 8.1 6 4
Displacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cells after 1 hr by scintillation countingDisplacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 373 5 1 7 2.7 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccnn3C)sc12 10.1016/j.bmcl.2010.05.056
49797771 10855 None 0 Human Binding pKi = 8.1 8.1 9 3
Displacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cells after 1 hr by scintillation countingDisplacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 435 6 1 7 4.1 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(-n4ccnc4)cc3)sc12 10.1016/j.bmcl.2010.05.056
CHEMBL1172275 10855 None 0 Human Binding pKi = 8.1 8.1 9 3
Displacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cells after 1 hr by scintillation countingDisplacement of [3H]ZM241385 from human adenosine A2B receptor expressed in CHO cells after 1 hr by scintillation counting
ChEMBL 435 6 1 7 4.1 CCN(C(C)=O)c1ccc(OC)c2nc(NC(=O)c3ccc(-n4ccnc4)cc3)sc12 10.1016/j.bmcl.2010.05.056
156012446 177336 None 0 Human Binding pKi = 8.1 8.1 - 1
Displacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting methodDisplacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting method
ChEMBL 324 3 1 7 2.9 CCOC(=O)C1=C(C)Nc2nc3ccccc3n2C1c1cocn1 10.1021/acs.jmedchem.0c00564
CHEMBL4637285 177336 None 0 Human Binding pKi = 8.1 8.1 - 1
Displacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting methodDisplacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting method
ChEMBL 324 3 1 7 2.9 CCOC(=O)C1=C(C)Nc2nc3ccccc3n2C1c1cocn1 10.1021/acs.jmedchem.0c00564
136042353 71153 None 0 Human Binding pKi = 8.1 8.1 70 2
Displacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation countingDisplacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation counting
ChEMBL 530 8 2 9 3.6 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5cc(C(F)(F)F)ccc5[nH]4)nn3C)nc2n(CCC)c1=O 10.1021/jm201292w
CHEMBL1955902 71153 None 0 Human Binding pKi = 8.1 8.1 70 2
Displacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation countingDisplacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation counting
ChEMBL 530 8 2 9 3.6 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5cc(C(F)(F)F)ccc5[nH]4)nn3C)nc2n(CCC)c1=O 10.1021/jm201292w
44451269 96266 None 0 Human Binding pKi = 8.1 8.1 33 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 565 5 1 7 3.1 CC(Oc1ccc(-c2cc3c([nH]2)c(=O)n(C)c(=O)n3C)cc1)C(=O)N1CCN(c2ccc(Br)cc2)CC1 10.1016/j.bmc.2008.01.002
CHEMBL261068 96266 None 0 Human Binding pKi = 8.1 8.1 33 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 565 5 1 7 3.1 CC(Oc1ccc(-c2cc3c([nH]2)c(=O)n(C)c(=O)n3C)cc1)C(=O)N1CCN(c2ccc(Br)cc2)CC1 10.1016/j.bmc.2008.01.002
11270783 1226 None 35 Human Binding pKi = 8.1 8.1 67 4
Displacement of [125I]-ABOPX from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [125I]-ABOPX from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 446 6 1 7 3.2 CCCn1c(=O)c2nc([nH]c2n(c1=O)CC)c1cnn(c1)Cc1cccc(c1)C(F)(F)F 10.1021/jm201292w
5615 1226 None 35 Human Binding pKi = 8.1 8.1 67 4
Displacement of [125I]-ABOPX from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [125I]-ABOPX from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 446 6 1 7 3.2 CCCn1c(=O)c2nc([nH]c2n(c1=O)CC)c1cnn(c1)Cc1cccc(c1)C(F)(F)F 10.1021/jm201292w
CHEMBL260933 1226 None 35 Human Binding pKi = 8.1 8.1 67 4
Displacement of [125I]-ABOPX from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [125I]-ABOPX from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 446 6 1 7 3.2 CCCn1c(=O)c2nc([nH]c2n(c1=O)CC)c1cnn(c1)Cc1cccc(c1)C(F)(F)F 10.1021/jm201292w
DB05936 1226 None 35 Human Binding pKi = 8.1 8.1 67 4
Displacement of [125I]-ABOPX from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [125I]-ABOPX from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 446 6 1 7 3.2 CCCn1c(=O)c2nc([nH]c2n(c1=O)CC)c1cnn(c1)Cc1cccc(c1)C(F)(F)F 10.1021/jm201292w
155565911 175777 None 0 Human Binding pKi = 8.1 8.1 - 1
Displacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 522 7 2 7 2.6 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(C(C)c5ccccc5)CC4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
CHEMBL4583860 175777 None 0 Human Binding pKi = 8.1 8.1 - 1
Displacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 522 7 2 7 2.6 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(C(C)c5ccccc5)CC4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
155548264 173768 None 0 Mouse Binding pKi = 8.1 8.1 -4 3
Displacement of [3H]PSB-603 from recombinant mouse A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant mouse A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 542 6 1 8 2.7 CCCn1c(=O)c2[nH]c(-c3ccc(S(=O)(=O)N4CCN(c5ccc(Cl)cc5)CC4)cc3)nc2n(C)c1=O 10.1021/acs.jmedchem.9b00071
CHEMBL4537196 173768 None 0 Mouse Binding pKi = 8.1 8.1 -4 3
Displacement of [3H]PSB-603 from recombinant mouse A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant mouse A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 542 6 1 8 2.7 CCCn1c(=O)c2[nH]c(-c3ccc(S(=O)(=O)N4CCN(c5ccc(Cl)cc5)CC4)cc3)nc2n(C)c1=O 10.1021/acs.jmedchem.9b00071
66894029 158134 None 0 Human Binding pKi = 8.1 8.1 - 1
Displacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting methodDisplacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting method
ChEMBL 570 9 1 8 4.2 CCCn1c(=O)c2[nH]c(-c3ccc(OCC4CC(=O)N(c5cccc(C(F)(F)F)c5)C4)nc3)nc2n(CCC)c1=O 10.1016/j.ejmech.2016.11.007
CHEMBL4087139 158134 None 0 Human Binding pKi = 8.1 8.1 - 1
Displacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting methodDisplacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting method
ChEMBL 570 9 1 8 4.2 CCCn1c(=O)c2[nH]c(-c3ccc(OCC4CC(=O)N(c5cccc(C(F)(F)F)c5)C4)nc3)nc2n(CCC)c1=O 10.1016/j.ejmech.2016.11.007
44450829 95877 None 0 Human Binding pKi = 8.1 8.1 41 4
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 444 4 1 6 2.2 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCc5ccccc5C4)cc3)cc2n(C)c1=O 10.1016/j.bmc.2008.01.002
CHEMBL259105 95877 None 0 Human Binding pKi = 8.1 8.1 41 4
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 444 4 1 6 2.2 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCc5ccccc5C4)cc3)cc2n(C)c1=O 10.1016/j.bmc.2008.01.002
154701278 169905 None 1 Human Binding pKi = 8.1 8.1 - 1
Displacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assayDisplacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assay
ChEMBL 391 3 1 6 4.4 CC1=C(C(=O)O[C@@H](C)C(F)(F)F)[C@@H](c2ccco2)n2c(nc3ccccc32)N1 10.1021/acs.jmedchem.9b01340
CHEMBL4440908 169905 None 1 Human Binding pKi = 8.1 8.1 - 1
Displacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assayDisplacement of [3H]DPCPX from human recombinant A2B receptor expressed in human HEK293 cell membranes incubated for 30 mins by radioligand binding competition assay
ChEMBL 391 3 1 6 4.4 CC1=C(C(=O)O[C@@H](C)C(F)(F)F)[C@@H](c2ccco2)n2c(nc3ccccc32)N1 10.1021/acs.jmedchem.9b01340
11313397 174709 None 0 Human Binding pKi = 8.1 8.1 18 2
Displacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cells
ChEMBL 326 5 2 5 2.6 CCCn1c(=O)c2[nH]c(-c3ccc(N)cc3)cc2n(CCC)c1=O 10.1016/j.bmc.2008.09.067
CHEMBL455986 174709 None 0 Human Binding pKi = 8.1 8.1 18 2
Displacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cells
ChEMBL 326 5 2 5 2.6 CCCn1c(=O)c2[nH]c(-c3ccc(N)cc3)cc2n(CCC)c1=O 10.1016/j.bmc.2008.09.067
11677816 73119 None 0 Human Binding pKi = 8.1 8.1 1 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 506 9 2 6 4.9 CCCn1c(=O)c2[nH]c(-c3ccc(OC(C)(C)C(=O)Nc4ccc(F)cc4)cc3)cc2n(CCC)c1=O 10.1021/jm0506221
CHEMBL201128 73119 None 0 Human Binding pKi = 8.1 8.1 1 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 506 9 2 6 4.9 CCCn1c(=O)c2[nH]c(-c3ccc(OC(C)(C)C(=O)Nc4ccc(F)cc4)cc3)cc2n(CCC)c1=O 10.1021/jm0506221
11541413 138491 None 0 Human Binding pKi = 8.1 8.1 2 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 566 12 2 7 5.6 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(OCc5ccccc5)cc4)cc3)cc2n(CCC)c1=O 10.1021/jm0506221
CHEMBL377485 138491 None 0 Human Binding pKi = 8.1 8.1 2 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 566 12 2 7 5.6 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(OCc5ccccc5)cc4)cc3)cc2n(CCC)c1=O 10.1021/jm0506221
54768602 80999 None 0 Human Binding pKi = 6.1 6.1 -2 3
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 331 1 0 7 1.4 Cn1c(=O)c2c(nc3n2CCN3C2CCCCCCC2)n(C)c1=O 10.1016/j.ejmech.2011.05.023
CHEMBL2153629 80999 None 0 Human Binding pKi = 6.1 6.1 -2 3
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 331 1 0 7 1.4 Cn1c(=O)c2c(nc3n2CCN3C2CCCCCCC2)n(C)c1=O 10.1016/j.ejmech.2011.05.023
162664296 182080 None 0 Human Binding pKi = 6.1 6.1 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 259 2 2 4 2.4 CC1=C(c2ncc(C)o2)C(c2ccoc2)NC(=O)N1 10.1021/acs.jmedchem.0c01431
CHEMBL4781559 182080 None 0 Human Binding pKi = 6.1 6.1 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 259 2 2 4 2.4 CC1=C(c2ncc(C)o2)C(c2ccoc2)NC(=O)N1 10.1021/acs.jmedchem.0c01431
71683094 90209 None 0 Human Binding pKi = 6.1 6.1 2 2
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells after 75 mins by liquid scintillation counting analysisDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells after 75 mins by liquid scintillation counting analysis
ChEMBL 328 4 1 4 3.4 O=C(CCc1ccccc1F)Nc1nc2ccccc2c(=O)s1 10.1021/jm400336x
CHEMBL2382428 90209 None 0 Human Binding pKi = 6.1 6.1 2 2
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells after 75 mins by liquid scintillation counting analysisDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells after 75 mins by liquid scintillation counting analysis
ChEMBL 328 4 1 4 3.4 O=C(CCc1ccccc1F)Nc1nc2ccccc2c(=O)s1 10.1021/jm400336x
10505816 30354 None 0 Human Binding pKi = 6.1 6.1 -3 5
Displacement of [3H]-DPCPX from Adenosine A2b receptor expressed in CHO cells; range 719-895Displacement of [3H]-DPCPX from Adenosine A2b receptor expressed in CHO cells; range 719-895
ChEMBL 508 8 2 9 5.0 COc1ccc(NC(=O)Nc2nc3nn(CCCc4ccccc4)cc3c3nc(-c4ccco4)nn23)cc1 10.1021/jm001047y
CHEMBL139182 30354 None 0 Human Binding pKi = 6.1 6.1 -3 5
Displacement of [3H]-DPCPX from Adenosine A2b receptor expressed in CHO cells; range 719-895Displacement of [3H]-DPCPX from Adenosine A2b receptor expressed in CHO cells; range 719-895
ChEMBL 508 8 2 9 5.0 COc1ccc(NC(=O)Nc2nc3nn(CCCc4ccccc4)cc3c3nc(-c4ccco4)nn23)cc1 10.1021/jm001047y
162673763 183077 None 0 Human Binding pKi = 6.1 6.1 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 248 4 2 3 2.3 CCCC(=O)C1=C(C)NC(=O)NC1c1ccco1 10.1021/acs.jmedchem.0c01431
CHEMBL4794386 183077 None 0 Human Binding pKi = 6.1 6.1 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 248 4 2 3 2.3 CCCC(=O)C1=C(C)NC(=O)NC1c1ccco1 10.1021/acs.jmedchem.0c01431
135522364 99909 None 0 Human Binding pKi = 7.1 7.1 17 2
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 480 8 3 9 2.8 CCCn1c(=O)c2nc(-c3cc(NC(=O)Nc4ccc(OC)cc4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
CHEMBL286102 99909 None 0 Human Binding pKi = 7.1 7.1 17 2
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 480 8 3 9 2.8 CCCn1c(=O)c2nc(-c3cc(NC(=O)Nc4ccc(OC)cc4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
10859484 77658 None 0 Human Binding pKi = 7.1 7.1 -5 4
Displacement of [3H]- DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]- DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 298 3 2 9 1.3 CCNc1c2c(nc(N)n3nc(-c4ccco4)nc23)nn1C 10.1021/jm021023m
CHEMBL20888 77658 None 0 Human Binding pKi = 7.1 7.1 -5 4
Displacement of [3H]- DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]- DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 298 3 2 9 1.3 CCNc1c2c(nc(N)n3nc(-c4ccco4)nc23)nn1C 10.1021/jm021023m
CHEMBL544678 77658 None 0 Human Binding pKi = 7.1 7.1 -5 4
Displacement of [3H]- DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]- DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 298 3 2 9 1.3 CCNc1c2c(nc(N)n3nc(-c4ccco4)nc23)nn1C 10.1021/jm021023m
9868991 118989 None 0 Human Binding pKi = 7.1 7.1 1 4
Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 70-94Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 70-94
ChEMBL 462 5 2 8 5.0 CC(C)=CCn1cc2c(nc(NC(=O)Nc3cccc(Cl)c3)n3nc(-c4ccco4)nc23)n1 10.1021/jm001047y
CHEMBL342500 118989 None 0 Human Binding pKi = 7.1 7.1 1 4
Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 70-94Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 70-94
ChEMBL 462 5 2 8 5.0 CC(C)=CCn1cc2c(nc(NC(=O)Nc3cccc(Cl)c3)n3nc(-c4ccco4)nc23)n1 10.1021/jm001047y
10791347 165164 None 0 Human Binding pKi = 7.1 7.1 -7 6
Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 70-94Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 70-94
ChEMBL 494 7 2 9 4.6 COc1ccc(NC(=O)Nc2nc3nn(CCc4ccccc4)cc3c3nc(-c4ccco4)nn23)cc1 10.1021/jm001047y
CHEMBL422820 165164 None 0 Human Binding pKi = 7.1 7.1 -7 6
Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 70-94Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 70-94
ChEMBL 494 7 2 9 4.6 COc1ccc(NC(=O)Nc2nc3nn(CCc4ccccc4)cc3c3nc(-c4ccco4)nn23)cc1 10.1021/jm001047y
44574167 178706 None 0 Human Binding pKi = 7.1 7.1 6 2
Displacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells by beta scintillation counterDisplacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells by beta scintillation counter
ChEMBL 405 4 2 7 2.4 Cn1c(=O)c2[nH]c(-c3ccc(COC(=O)Nc4ccccn4)cc3)cc2n(C)c1=O 10.1016/j.bmc.2009.03.062
CHEMBL468296 178706 None 0 Human Binding pKi = 7.1 7.1 6 2
Displacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells by beta scintillation counterDisplacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells by beta scintillation counter
ChEMBL 405 4 2 7 2.4 Cn1c(=O)c2[nH]c(-c3ccc(COC(=O)Nc4ccccn4)cc3)cc2n(C)c1=O 10.1016/j.bmc.2009.03.062
12295530 99777 None 15 Human Binding pKi = 6.1 6.1 3 3
Inhibition of [3H]ZM-241385 binding to human adenosine A2B receptorInhibition of [3H]ZM-241385 binding to human adenosine A2B receptor
ChEMBL 228 1 3 3 0.6 O=c1[nH]c(=O)c2[nH]c(-c3ccccc3)nc2[nH]1 10.1021/jm011049y
CHEMBL285191 99777 None 15 Human Binding pKi = 6.1 6.1 3 3
Inhibition of [3H]ZM-241385 binding to human adenosine A2B receptorInhibition of [3H]ZM-241385 binding to human adenosine A2B receptor
ChEMBL 228 1 3 3 0.6 O=c1[nH]c(=O)c2[nH]c(-c3ccccc3)nc2[nH]1 10.1021/jm011049y
45486932 197016 None 3 Human Binding pKi = 5.1 5.1 -6 3
Binding affinity to adenosine A2B receptor (unknown origin)Binding affinity to adenosine A2B receptor (unknown origin)
ChEMBL 267 5 1 5 2.5 CCn1cnc2c(NCCc3ccccc3)ncnc21 10.1039/C5MD00034C
CHEMBL567012 197016 None 3 Human Binding pKi = 5.1 5.1 -6 3
Binding affinity to adenosine A2B receptor (unknown origin)Binding affinity to adenosine A2B receptor (unknown origin)
ChEMBL 267 5 1 5 2.5 CCn1cnc2c(NCCc3ccccc3)ncnc21 10.1039/C5MD00034C
137175187 138966 None 0 Human Binding pKi = 6.1 6.1 - 1
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 minsDisplacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 mins
ChEMBL 304 3 1 7 2.6 CC1=C(C(=O)OC(C)C)C(c2ccsc2)n2ncnc2N1 10.1021/acs.jmedchem.5b01586
CHEMBL3785256 138966 None 0 Human Binding pKi = 6.1 6.1 - 1
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 minsDisplacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 mins
ChEMBL 304 3 1 7 2.6 CC1=C(C(=O)OC(C)C)C(c2ccsc2)n2ncnc2N1 10.1021/acs.jmedchem.5b01586
44406555 72863 None 0 Human Binding pKi = 7.1 7.1 5 4
Displacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cellsDisplacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cells
ChEMBL 490 9 1 11 2.7 CCCn1c(=O)c2nc(-c3cnn(Cc4nc(-c5ccccc5OC)no4)c3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2005.10.002
CHEMBL200278 72863 None 0 Human Binding pKi = 7.1 7.1 5 4
Displacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cellsDisplacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cells
ChEMBL 490 9 1 11 2.7 CCCn1c(=O)c2nc(-c3cnn(Cc4nc(-c5ccccc5OC)no4)c3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2005.10.002
44406562 134202 None 0 Human Binding pKi = 7.1 7.1 7 3
Displacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cellsDisplacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cells
ChEMBL 490 9 1 11 2.7 CCCn1c(=O)c2nc(-c3cnn(Cc4nc(-c5cccc(OC)c5)no4)c3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2005.10.002
CHEMBL371676 134202 None 0 Human Binding pKi = 7.1 7.1 7 3
Displacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cellsDisplacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cells
ChEMBL 490 9 1 11 2.7 CCCn1c(=O)c2nc(-c3cnn(Cc4nc(-c5cccc(OC)c5)no4)c3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2005.10.002
22266738 166284 None 0 Human Binding pKi = 7.1 7.1 6 4
Displacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cellsDisplacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cells
ChEMBL 493 8 1 9 3.9 CCCn1c(=O)c2nc(-c3cnn(Cc4cc(-c5ccc(Cl)cc5)on4)c3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2005.10.002
CHEMBL427016 166284 None 0 Human Binding pKi = 7.1 7.1 6 4
Displacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cellsDisplacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cells
ChEMBL 493 8 1 9 3.9 CCCn1c(=O)c2nc(-c3cnn(Cc4cc(-c5ccc(Cl)cc5)on4)c3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2005.10.002
5353365 1210 None 32 Human Binding pKi = 5.1 5.1 -263 6
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 330 2 0 6 1.8 Clc1cccc(c1)/C=C/c1nc2c(n1C)c(=O)n(c(=O)n2C)C 10.1021/jm400336x
5609 1210 None 32 Human Binding pKi = 5.1 5.1 -263 6
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 330 2 0 6 1.8 Clc1cccc(c1)/C=C/c1nc2c(n1C)c(=O)n(c(=O)n2C)C 10.1021/jm400336x
CHEMBL26138 1210 None 32 Human Binding pKi = 5.1 5.1 -263 6
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cellsDisplacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells
ChEMBL 330 2 0 6 1.8 Clc1cccc(c1)/C=C/c1nc2c(n1C)c(=O)n(c(=O)n2C)C 10.1021/jm400336x
44236417 158692 None 0 Human Binding pKi = 7.1 7.1 - 1
Displacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 minsDisplacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 mins
ChEMBL 452 7 1 9 0.8 CCCn1c(=O)c2[nH]c(-c3cnn(CC#CCN4CCN(C)CC4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2017.04.014
CHEMBL4093116 158692 None 0 Human Binding pKi = 7.1 7.1 - 1
Displacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 minsDisplacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 mins
ChEMBL 452 7 1 9 0.8 CCCn1c(=O)c2[nH]c(-c3cnn(CC#CCN4CCN(C)CC4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2017.04.014
21958814 135644 None 0 Human Binding pKi = 7.1 7.1 11 3
Displacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cellsDisplacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cells
ChEMBL 490 9 1 11 2.7 CCCn1c(=O)c2nc(-c3cnn(Cc4noc(-c5ccccc5OC)n4)c3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2005.10.002
CHEMBL372951 135644 None 0 Human Binding pKi = 7.1 7.1 11 3
Displacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cellsDisplacement of [3H]ZM-241385 from Adenosine A2B receptor expressed in HEK cells
ChEMBL 490 9 1 11 2.7 CCCn1c(=O)c2nc(-c3cnn(Cc4noc(-c5ccccc5OC)n4)c3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2005.10.002
11706151 72036 None 0 Human Binding pKi = 7.1 7.1 -1 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 508 10 2 6 4.3 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)NCc4ccccc4)cc3)c(Cl)c2n(CCC)c1=O 10.1021/jm0506221
CHEMBL197605 72036 None 0 Human Binding pKi = 7.1 7.1 -1 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 508 10 2 6 4.3 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)NCc4ccccc4)cc3)c(Cl)c2n(CCC)c1=O 10.1021/jm0506221
11519361 75012 None 0 Human Binding pKi = 7.1 7.1 3 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 528 9 2 6 5.3 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccccc4Cl)cc3)c(Cl)c2n(CCC)c1=O 10.1021/jm0506221
CHEMBL203359 75012 None 0 Human Binding pKi = 7.1 7.1 3 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 528 9 2 6 5.3 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccccc4Cl)cc3)c(Cl)c2n(CCC)c1=O 10.1021/jm0506221
46228016 201867 None 0 Human Binding pKi = 6.1 6.1 -2 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 410 8 1 7 2.9 CCSCCn1c(=O)c2[nH]c(Cc3ccccc3)nc2n(Cc2ccco2)c1=O 10.1016/j.bmc.2009.07.034
CHEMBL607258 201867 None 0 Human Binding pKi = 6.1 6.1 -2 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 410 8 1 7 2.9 CCSCCn1c(=O)c2[nH]c(Cc3ccccc3)nc2n(Cc2ccco2)c1=O 10.1016/j.bmc.2009.07.034
12150 2333 None 2 Human Binding pKi = 6.1 6.1 -100 4
Displacement of [3H]MRS1754 from A2BAR (unknown origin) expressed in HEK293 cells assessed as inhibition constant by competitive binding assayDisplacement of [3H]MRS1754 from A2BAR (unknown origin) expressed in HEK293 cells assessed as inhibition constant by competitive binding assay
ChEMBL 399 4 3 9 1.9 O[C@H]1[C@@H](O)[C@H](n2c3nc(C#CCCCC)nc(N)c3nc2c2cccs2)OC1 10.1021/acs.jmedchem.2c00462
164885960 2333 None 2 Human Binding pKi = 6.1 6.1 -100 4
Displacement of [3H]MRS1754 from A2BAR (unknown origin) expressed in HEK293 cells assessed as inhibition constant by competitive binding assayDisplacement of [3H]MRS1754 from A2BAR (unknown origin) expressed in HEK293 cells assessed as inhibition constant by competitive binding assay
ChEMBL 399 4 3 9 1.9 O[C@H]1[C@@H](O)[C@H](n2c3nc(C#CCCCC)nc(N)c3nc2c2cccs2)OC1 10.1021/acs.jmedchem.2c00462
CHEMBL5203469 2333 None 2 Human Binding pKi = 6.1 6.1 -100 4
Displacement of [3H]MRS1754 from A2BAR (unknown origin) expressed in HEK293 cells assessed as inhibition constant by competitive binding assayDisplacement of [3H]MRS1754 from A2BAR (unknown origin) expressed in HEK293 cells assessed as inhibition constant by competitive binding assay
ChEMBL 399 4 3 9 1.9 O[C@H]1[C@@H](O)[C@H](n2c3nc(C#CCCCC)nc(N)c3nc2c2cccs2)OC1 10.1021/acs.jmedchem.2c00462
25188209 178759 None 0 Human Binding pKi = 6.1 6.1 -20 4
Displacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation countingDisplacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation counting
ChEMBL 311 3 1 8 1.6 Nc1nc(-c2ncco2)c2nnn(Cc3ccccc3F)c2n1 10.1021/jm800961g
CHEMBL468701 178759 None 0 Human Binding pKi = 6.1 6.1 -20 4
Displacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation countingDisplacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation counting
ChEMBL 311 3 1 8 1.6 Nc1nc(-c2ncco2)c2nnn(Cc3ccccc3F)c2n1 10.1021/jm800961g
135543600 16330 None 0 Human Binding pKi = 6.1 6.1 -933 4
Inhibition of [3H]DPCPX binding to human Adenosine A2B receptor expressed in HEK cells; range 640-1100Inhibition of [3H]DPCPX binding to human Adenosine A2B receptor expressed in HEK cells; range 640-1100
ChEMBL 336 6 1 6 3.4 CCCCc1nc2[nH]cnc2c2nc(-c3ccc(OCC)cc3)nn12 10.1021/jm010570p
CHEMBL122819 16330 None 0 Human Binding pKi = 6.1 6.1 -933 4
Inhibition of [3H]DPCPX binding to human Adenosine A2B receptor expressed in HEK cells; range 640-1100Inhibition of [3H]DPCPX binding to human Adenosine A2B receptor expressed in HEK cells; range 640-1100
ChEMBL 336 6 1 6 3.4 CCCCc1nc2[nH]cnc2c2nc(-c3ccc(OCC)cc3)nn12 10.1021/jm010570p
21874641 189857 None 0 Human Binding pKi = 7.1 7.1 -52 4
Displacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation countingDisplacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation counting
ChEMBL 323 3 3 9 1.4 Nc1nc(-c2ccco2)c2nnn(Cc3ccc(N)c(O)c3)c2n1 10.1021/jm800961g
CHEMBL516770 189857 None 0 Human Binding pKi = 7.1 7.1 -52 4
Displacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation countingDisplacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation counting
ChEMBL 323 3 3 9 1.4 Nc1nc(-c2ccco2)c2nnn(Cc3ccc(N)c(O)c3)c2n1 10.1021/jm800961g
2748297 181702 None 12 Human Binding pKi = 7.1 7.1 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 278 4 2 4 2.2 CCC(C)OC(=O)C1=C(C)NC(=O)NC1c1ccco1 10.1021/acs.jmedchem.0c01431
CHEMBL4776764 181702 None 12 Human Binding pKi = 7.1 7.1 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 278 4 2 4 2.2 CCC(C)OC(=O)C1=C(C)NC(=O)NC1c1ccco1 10.1021/acs.jmedchem.0c01431
127030064 138976 None 0 Human Binding pKi = 6.1 6.1 - 1
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 minsDisplacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 mins
ChEMBL 303 3 1 6 3.2 CC1=C(C(=O)OC(C)C)C(c2ccsc2)n2ccnc2N1 10.1021/acs.jmedchem.5b01586
CHEMBL3785334 138976 None 0 Human Binding pKi = 6.1 6.1 - 1
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 minsDisplacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 mins
ChEMBL 303 3 1 6 3.2 CC1=C(C(=O)OC(C)C)C(c2ccsc2)n2ccnc2N1 10.1021/acs.jmedchem.5b01586
44410691 138187 None 0 Human Binding pKi = 5.1 5.1 -15848 4
Displacement of [125I]ABOPX from human adenosine A2B receptor in HEK cellsDisplacement of [125I]ABOPX from human adenosine A2B receptor in HEK cells
ChEMBL 460 9 5 10 0.3 CCCCC[C@H](O)C#Cc1nc(NCC)c2ncn([C@@H]3O[C@H](C(=O)NCC)[C@@H](O)[C@H]3O)c2n1 10.1016/j.bmcl.2006.01.110
CHEMBL376968 138187 None 0 Human Binding pKi = 5.1 5.1 -15848 4
Displacement of [125I]ABOPX from human adenosine A2B receptor in HEK cellsDisplacement of [125I]ABOPX from human adenosine A2B receptor in HEK cells
ChEMBL 460 9 5 10 0.3 CCCCC[C@H](O)C#Cc1nc(NCC)c2ncn([C@@H]3O[C@H](C(=O)NCC)[C@@H](O)[C@H]3O)c2n1 10.1016/j.bmcl.2006.01.110
135430228 110318 None 0 Human Binding pKi = 7.1 7.1 9 2
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 548 10 1 10 1.8 CCCn1c(=O)c2nc(-c3cc(OCC(=O)N4CCN(Cc5ccccc5)CC4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
CHEMBL32388 110318 None 0 Human Binding pKi = 7.1 7.1 9 2
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 548 10 1 10 1.8 CCCn1c(=O)c2nc(-c3cc(OCC(=O)N4CCN(Cc5ccccc5)CC4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
11122708 120214 None 0 Human Binding pKi = 7.1 7.1 -13 4
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 68-105Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 68-105
ChEMBL 422 4 2 8 4.1 CCn1cc2c(nc(NC(=O)Nc3ccc(Cl)cc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm0109614
CHEMBL352073 120214 None 0 Human Binding pKi = 7.1 7.1 -13 4
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 68-105Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 68-105
ChEMBL 422 4 2 8 4.1 CCn1cc2c(nc(NC(=O)Nc3ccc(Cl)cc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm0109614
16071781 58026 None 0 Human Binding pKi = 7.1 7.1 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 351 4 1 5 3.6 O=C(Nc1cnc(-c2ccncc2Cl)c(-c2cccnc2)n1)C1CC1 10.1021/ml100249e
CHEMBL1672628 58026 None 0 Human Binding pKi = 7.1 7.1 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assayDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 60 mins by filtration binding assay
ChEMBL 351 4 1 5 3.6 O=C(Nc1cnc(-c2ccncc2Cl)c(-c2cccnc2)n1)C1CC1 10.1021/ml100249e
45268921 196115 None 0 Human Binding pKi = 7.1 7.1 2 2
Binding affinity to human adenosine A2b receptor expressed in HEK293 cellsBinding affinity to human adenosine A2b receptor expressed in HEK293 cells
ChEMBL 317 6 2 6 0.9 CCn1c(=O)c2[nH]c(-c3ccc[nH]3)nc2n(CCCOC)c1=O 10.1016/j.bmc.2009.03.029
CHEMBL560967 196115 None 0 Human Binding pKi = 7.1 7.1 2 2
Binding affinity to human adenosine A2b receptor expressed in HEK293 cellsBinding affinity to human adenosine A2b receptor expressed in HEK293 cells
ChEMBL 317 6 2 6 0.9 CCn1c(=O)c2[nH]c(-c3ccc[nH]3)nc2n(CCCOC)c1=O 10.1016/j.bmc.2009.03.029
127034214 138980 None 0 Human Binding pKi = 7.1 7.1 - 1
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 minsDisplacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 mins
ChEMBL 287 3 1 6 2.7 CC1=C(C(=O)OC(C)C)C(c2ccco2)n2ccnc2N1 10.1021/acs.jmedchem.5b01586
CHEMBL3785381 138980 None 0 Human Binding pKi = 7.1 7.1 - 1
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 minsDisplacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 mins
ChEMBL 287 3 1 6 2.7 CC1=C(C(=O)OC(C)C)C(c2ccco2)n2ccnc2N1 10.1021/acs.jmedchem.5b01586
12654835 56757 None 2 Human Binding pKi = 5.1 5.1 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by liquid scintillation countingDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by liquid scintillation counting
ChEMBL 265 2 1 3 3.0 O=C(Nc1ccccc1)c1coc2ccccc2c1=O 10.1016/j.ejmech.2012.05.033
CHEMBL1643120 56757 None 2 Human Binding pKi = 5.1 5.1 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by liquid scintillation countingDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by liquid scintillation counting
ChEMBL 265 2 1 3 3.0 O=C(Nc1ccccc1)c1coc2ccccc2c1=O 10.1016/j.ejmech.2012.05.033
127043668 141171 None 0 Human Binding pKi = 6.1 6.1 - 1
Displacement of [3H]PSB-603 from recombinant human adenosine receptor A2b expressed in CHO cell membranesDisplacement of [3H]PSB-603 from recombinant human adenosine receptor A2b expressed in CHO cell membranes
ChEMBL 524 11 0 10 2.3 CCCn1c(=O)c2c(nc3n2CCCN3CCc2ccc(OCCN3CCOCC3)cc2)n(CCC)c1=O 10.1016/j.bmc.2016.07.028
CHEMBL3827920 141171 None 0 Human Binding pKi = 6.1 6.1 - 1
Displacement of [3H]PSB-603 from recombinant human adenosine receptor A2b expressed in CHO cell membranesDisplacement of [3H]PSB-603 from recombinant human adenosine receptor A2b expressed in CHO cell membranes
ChEMBL 524 11 0 10 2.3 CCCn1c(=O)c2c(nc3n2CCCN3CCc2ccc(OCCN3CCOCC3)cc2)n(CCC)c1=O 10.1016/j.bmc.2016.07.028
45267987 194789 None 0 Human Binding pKi = 6.1 6.1 -112 4
Binding affinity to adenosine A2B receptorBinding affinity to adenosine A2B receptor
ChEMBL 294 4 2 5 2.2 Nc1nc(C(=O)NCc2ccccc2)cc(-c2ccco2)n1 10.1016/j.bmcl.2009.03.142
CHEMBL538629 194789 None 0 Human Binding pKi = 6.1 6.1 -112 4
Binding affinity to adenosine A2B receptorBinding affinity to adenosine A2B receptor
ChEMBL 294 4 2 5 2.2 Nc1nc(C(=O)NCc2ccccc2)cc(-c2ccco2)n1 10.1016/j.bmcl.2009.03.142
44442019 154314 None 0 Human Binding pKi = 5.1 5.1 -269 3
Binding affinity to adenosine A2B receptorBinding affinity to adenosine A2B receptor
ChEMBL 618 8 6 11 3.5 CC(C)(C)c1cc(C(=O)NCCc2ccc(Nc3ncnc4c3ncn4[C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)cc2)cc(C(C)(C)C)c1O 10.1016/j.bmcl.2007.07.035
CHEMBL398669 154314 None 0 Human Binding pKi = 5.1 5.1 -269 3
Binding affinity to adenosine A2B receptorBinding affinity to adenosine A2B receptor
ChEMBL 618 8 6 11 3.5 CC(C)(C)c1cc(C(=O)NCCc2ccc(Nc3ncnc4c3ncn4[C@@H]3O[C@H](CO)[C@@H](O)[C@H]3O)cc2)cc(C(C)(C)C)c1O 10.1016/j.bmcl.2007.07.035
135448286 109711 None 0 Human Binding pKi = 7.1 7.1 - 1
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 507 10 2 10 2.3 CCCn1c(=O)c2nc(-c3cc(OCC(=O)Nc4ccc(C(C)=O)cc4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
CHEMBL32288 109711 None 0 Human Binding pKi = 7.1 7.1 - 1
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 507 10 2 10 2.3 CCCn1c(=O)c2nc(-c3cc(OCC(=O)Nc4ccc(C(C)=O)cc4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
135522390 119141 None 0 Human Binding pKi = 7.1 7.1 - 1
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 550 10 2 11 2.0 CCCn1c(=O)c2nc(-c3cc(OCC(=O)Nc4ccc(N5CCOCC5)cc4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
CHEMBL34281 119141 None 0 Human Binding pKi = 7.1 7.1 - 1
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 550 10 2 11 2.0 CCCn1c(=O)c2nc(-c3cc(OCC(=O)Nc4ccc(N5CCOCC5)cc4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
145993331 166919 None 0 Human Binding pKi = 6.1 6.1 -1 4
Displacement of [3H]PSB-602 from human adenosine A2B receptor expressed in CHO cell membranesDisplacement of [3H]PSB-602 from human adenosine A2B receptor expressed in CHO cell membranes
ChEMBL 576 14 1 11 2.4 CCCn1c(=O)c2c(nc3n2CCCN3CCc2ccc(OCC(=O)NCCCn3ccnc3)cc2)n(CCC)c1=O 10.1039/C8MD00070K
CHEMBL4286634 166919 None 0 Human Binding pKi = 6.1 6.1 -1 4
Displacement of [3H]PSB-602 from human adenosine A2B receptor expressed in CHO cell membranesDisplacement of [3H]PSB-602 from human adenosine A2B receptor expressed in CHO cell membranes
ChEMBL 576 14 1 11 2.4 CCCn1c(=O)c2c(nc3n2CCCN3CCc2ccc(OCC(=O)NCCCn3ccnc3)cc2)n(CCC)c1=O 10.1039/C8MD00070K
9860013 156983 None 0 Human Binding pKi = 6.1 6.1 -616 4
Binding affinity at human adenosine A2B receptorBinding affinity at human adenosine A2B receptor
ChEMBL 261 2 0 5 3.9 CC(C)c1nc(-c2nccs2)c2sccc2n1 10.1016/j.bmcl.2008.03.076
CHEMBL407307 156983 None 0 Human Binding pKi = 6.1 6.1 -616 4
Binding affinity at human adenosine A2B receptorBinding affinity at human adenosine A2B receptor
ChEMBL 261 2 0 5 3.9 CC(C)c1nc(-c2nccs2)c2sccc2n1 10.1016/j.bmcl.2008.03.076
9860013 156983 None 0 Human Binding pKi = 6.1 6.1 -616 4
Inhibition of human recombinant adenosine receptor A2bInhibition of human recombinant adenosine receptor A2b
ChEMBL 261 2 0 5 3.9 CC(C)c1nc(-c2nccs2)c2sccc2n1 10.1021/jm4011669
CHEMBL407307 156983 None 0 Human Binding pKi = 6.1 6.1 -616 4
Inhibition of human recombinant adenosine receptor A2bInhibition of human recombinant adenosine receptor A2b
ChEMBL 261 2 0 5 3.9 CC(C)c1nc(-c2nccs2)c2sccc2n1 10.1021/jm4011669
11037739 165544 None 0 Human Binding pKi = 7.1 7.1 -6 4
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 76-98Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 76-98
ChEMBL 450 6 2 8 4.8 CCCCn1cc2c(nc(NC(=O)Nc3ccc(Cl)cc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm0109614
CHEMBL424161 165544 None 0 Human Binding pKi = 7.1 7.1 -6 4
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 76-98Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 76-98
ChEMBL 450 6 2 8 4.8 CCCCn1cc2c(nc(NC(=O)Nc3ccc(Cl)cc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm0109614
136042348 71176 None 0 Human Binding pKi = 7.1 7.1 -1 2
Displacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation countingDisplacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation counting
ChEMBL 508 9 2 10 2.5 CCCn1c(=O)c2[nH]c(-c3cc(OCC(=O)Nc4ccc5c(c4)OCO5)nn3C)cc2n(CCC)c1=O 10.1021/jm201292w
CHEMBL1955926 71176 None 0 Human Binding pKi = 7.1 7.1 -1 2
Displacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation countingDisplacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation counting
ChEMBL 508 9 2 10 2.5 CCCn1c(=O)c2[nH]c(-c3cc(OCC(=O)Nc4ccc5c(c4)OCO5)nn3C)cc2n(CCC)c1=O 10.1021/jm201292w
44308015 103379 None 0 Human Binding pKi = 5.1 5.1 - 1
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 266 3 0 8 -1.0 CC(=O)OCCn1c(=O)c2c(ncn2C)n(C)c1=O 10.1021/jm0104318
CHEMBL308464 103379 None 0 Human Binding pKi = 5.1 5.1 - 1
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 266 3 0 8 -1.0 CC(=O)OCCn1c(=O)c2c(ncn2C)n(C)c1=O 10.1021/jm0104318
135546648 109714 None 0 Human Binding pKi = 7.1 7.1 2 2
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 467 8 2 8 2.4 CCCn1c(=O)c2nc(-c3cc(NC(=O)Cc4ccc(F)cc4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
CHEMBL32289 109714 None 0 Human Binding pKi = 7.1 7.1 2 2
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 467 8 2 8 2.4 CCCn1c(=O)c2nc(-c3cc(NC(=O)Cc4ccc(F)cc4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
11728808 120313 None 0 Human Binding pKi = 7.1 7.1 -15 4
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 67-115Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 67-115
ChEMBL 388 4 2 8 3.4 CCn1cc2c(nc(NC(=O)Nc3ccccc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm0109614
CHEMBL352796 120313 None 0 Human Binding pKi = 7.1 7.1 -15 4
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 67-115Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 67-115
ChEMBL 388 4 2 8 3.4 CCn1cc2c(nc(NC(=O)Nc3ccccc3)n3nc(-c4ccco4)nc23)n1 10.1021/jm0109614
136042330 71156 None 0 Human Binding pKi = 7.1 7.1 52 2
Displacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation countingDisplacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation counting
ChEMBL 506 9 3 10 2.3 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5cc(C(=O)O)ccc5[nH]4)nn3C)nc2n(CCC)c1=O 10.1021/jm201292w
CHEMBL1955905 71156 None 0 Human Binding pKi = 7.1 7.1 52 2
Displacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation countingDisplacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation counting
ChEMBL 506 9 3 10 2.3 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5cc(C(=O)O)ccc5[nH]4)nn3C)nc2n(CCC)c1=O 10.1021/jm201292w
21874782 176806 None 0 Human Binding pKi = 7.1 7.1 -38 4
Displacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation countingDisplacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation counting
ChEMBL 298 3 1 8 2.2 Nc1nc(-c2ccco2)c2nnn(Cc3cccs3)c2n1 10.1021/jm800961g
CHEMBL460799 176806 None 0 Human Binding pKi = 7.1 7.1 -38 4
Displacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation countingDisplacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation counting
ChEMBL 298 3 1 8 2.2 Nc1nc(-c2ccco2)c2nnn(Cc3cccs3)c2n1 10.1021/jm800961g
377 2758 None 53 Human Binding pKi = 6.1 6.1 -1479 15
Displacement of [125I]ABOPX from human adenosine A2B receptor in HEK cellsDisplacement of [125I]ABOPX from human adenosine A2B receptor in HEK cells
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1016/j.bmcl.2006.01.110
425 2758 None 53 Human Binding pKi = 6.1 6.1 -1479 15
Displacement of [125I]ABOPX from human adenosine A2B receptor in HEK cellsDisplacement of [125I]ABOPX from human adenosine A2B receptor in HEK cells
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1016/j.bmcl.2006.01.110
448222 2758 None 53 Human Binding pKi = 6.1 6.1 -1479 15
Displacement of [125I]ABOPX from human adenosine A2B receptor in HEK cellsDisplacement of [125I]ABOPX from human adenosine A2B receptor in HEK cells
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1016/j.bmcl.2006.01.110
CHEMBL464859 2758 None 53 Human Binding pKi = 6.1 6.1 -1479 15
Displacement of [125I]ABOPX from human adenosine A2B receptor in HEK cellsDisplacement of [125I]ABOPX from human adenosine A2B receptor in HEK cells
ChEMBL 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10.1016/j.bmcl.2006.01.110
10267860 176823 None 0 Human Binding pKi = 6.1 6.1 -12 4
Displacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation countingDisplacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation counting
ChEMBL 317 3 1 8 2.0 N#Cc1ccc(Cn2nnc3c(-c4ccco4)nc(N)nc32)cc1 10.1021/jm800961g
CHEMBL461007 176823 None 0 Human Binding pKi = 6.1 6.1 -12 4
Displacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation countingDisplacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation counting
ChEMBL 317 3 1 8 2.0 N#Cc1ccc(Cn2nnc3c(-c4ccco4)nc(N)nc32)cc1 10.1021/jm800961g
2748301 172287 None 8 Human Binding pKi = 6.1 6.1 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 312 4 2 4 2.7 CC1=C(C(=O)OCc2ccccc2)C(c2ccco2)NC(=O)N1 10.1021/acs.jmedchem.0c01431
CHEMBL4474844 172287 None 8 Human Binding pKi = 6.1 6.1 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 312 4 2 4 2.7 CC1=C(C(=O)OCc2ccccc2)C(c2ccco2)NC(=O)N1 10.1021/acs.jmedchem.0c01431
44588436 174708 None 0 Human Binding pKi = 7.1 7.1 -1 2
Displacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cells
ChEMBL 341 5 2 5 3.0 CCCn1c(=O)c2[nH]c(-c3ccc(C)cc3)c(O)c2n(CCC)c1=O 10.1016/j.bmc.2008.09.067
CHEMBL455985 174708 None 0 Human Binding pKi = 7.1 7.1 -1 2
Displacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human cloned adenosine A2B receptor expressed in HEK293 cells
ChEMBL 341 5 2 5 3.0 CCCn1c(=O)c2[nH]c(-c3ccc(C)cc3)c(O)c2n(CCC)c1=O 10.1016/j.bmc.2008.09.067
46227950 199905 None 0 Human Binding pKi = 7.1 7.1 4 3
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 396 5 1 6 2.0 C#CCn1c(=O)c2[nH]c(Cc3c(F)cccc3F)nc2n(Cc2ccco2)c1=O 10.1016/j.bmc.2009.07.034
CHEMBL594728 199905 None 0 Human Binding pKi = 7.1 7.1 4 3
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 396 5 1 6 2.0 C#CCn1c(=O)c2[nH]c(Cc3c(F)cccc3F)nc2n(Cc2ccco2)c1=O 10.1016/j.bmc.2009.07.034
46227995 201444 None 0 Human Binding pKi = 7.1 7.1 1 3
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 430 8 0 9 2.9 CCSCCn1c(=O)c2c(nc(Cc3cccs3)n2C)n(Cc2ccco2)c1=O 10.1016/j.bmc.2009.07.034
CHEMBL604885 201444 None 0 Human Binding pKi = 7.1 7.1 1 3
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 430 8 0 9 2.9 CCSCCn1c(=O)c2c(nc(Cc3cccs3)n2C)n(Cc2ccco2)c1=O 10.1016/j.bmc.2009.07.034
44450875 96830 None 0 Human Binding pKi = 6.1 6.1 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 502 6 1 7 3.0 COc1cc(OCC(=O)N2CCC(c3ccccc3)CC2)ccc1-c1cc2c([nH]1)c(=O)n(C)c(=O)n2C 10.1016/j.bmc.2008.01.002
CHEMBL265182 96830 None 0 Human Binding pKi = 6.1 6.1 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 502 6 1 7 3.0 COc1cc(OCC(=O)N2CCC(c3ccccc3)CC2)ccc1-c1cc2c([nH]1)c(=O)n(C)c(=O)n2C 10.1016/j.bmc.2008.01.002
44410406 75559 None 0 Human Binding pKi = 5.1 5.1 -6760 4
Displacement of [125I]ABOPX from human adenosine A2B receptor in HEK cellsDisplacement of [125I]ABOPX from human adenosine A2B receptor in HEK cells
ChEMBL 472 6 5 10 0.3 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC)nc(C#CC(O)C4CCCCC4)nc32)[C@H](O)[C@@H]1O 10.1016/j.bmcl.2006.01.110
CHEMBL204526 75559 None 0 Human Binding pKi = 5.1 5.1 -6760 4
Displacement of [125I]ABOPX from human adenosine A2B receptor in HEK cellsDisplacement of [125I]ABOPX from human adenosine A2B receptor in HEK cells
ChEMBL 472 6 5 10 0.3 CCNC(=O)[C@H]1O[C@@H](n2cnc3c(NCC)nc(C#CC(O)C4CCCCC4)nc32)[C@H](O)[C@@H]1O 10.1016/j.bmcl.2006.01.110
11198201 110677 None 7 Human Binding pKi = 8.1 8.1 3 3
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 327 5 2 6 2.0 CCCn1c(=O)c2nc(-c3ccc(N)cc3)[nH]c2n(CCC)c1=O 10.1021/jm0309654
CHEMBL32598 110677 None 7 Human Binding pKi = 8.1 8.1 3 3
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 327 5 2 6 2.0 CCCn1c(=O)c2nc(-c3ccc(N)cc3)[nH]c2n(CCC)c1=O 10.1021/jm0309654
66894327 155974 None 0 Human Binding pKi = 8.1 8.1 - 1
Displacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting methodDisplacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting method
ChEMBL 559 9 1 9 3.5 CCCn1c(=O)c2[nH]c(-c3cnn(CC4CC(=O)N(c5cccc(OC(F)(F)F)c5)C4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2016.11.007
CHEMBL4061490 155974 None 0 Human Binding pKi = 8.1 8.1 - 1
Displacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting methodDisplacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting method
ChEMBL 559 9 1 9 3.5 CCCn1c(=O)c2[nH]c(-c3cnn(CC4CC(=O)N(c5cccc(OC(F)(F)F)c5)C4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2016.11.007
66894035 156203 None 0 Human Binding pKi = 8.1 8.1 - 1
Displacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting methodDisplacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting method
ChEMBL 505 9 1 9 2.6 CCCn1c(=O)c2[nH]c(-c3cnn(CC4CC(=O)N(c5ccc(OC)cc5)C4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2016.11.007
CHEMBL4064289 156203 None 0 Human Binding pKi = 8.1 8.1 - 1
Displacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting methodDisplacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting method
ChEMBL 505 9 1 9 2.6 CCCn1c(=O)c2[nH]c(-c3cnn(CC4CC(=O)N(c5ccc(OC)cc5)C4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2016.11.007
66894143 158442 None 0 Human Binding pKi = 8.1 8.1 - 1
Displacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting methodDisplacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting method
ChEMBL 519 9 1 7 3.9 CCCn1c(=O)c2[nH]c(-c3ccc(OCC4CC(=O)N(c5cccc(F)c5)C4)cc3)nc2n(CCC)c1=O 10.1016/j.ejmech.2016.11.007
CHEMBL4090483 158442 None 0 Human Binding pKi = 8.1 8.1 - 1
Displacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting methodDisplacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting method
ChEMBL 519 9 1 7 3.9 CCCn1c(=O)c2[nH]c(-c3ccc(OCC4CC(=O)N(c5cccc(F)c5)C4)cc3)nc2n(CCC)c1=O 10.1016/j.ejmech.2016.11.007
9839378 140131 None 0 Human Binding pKi = 8.1 8.1 2 4
Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cellsDisplacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells
ChEMBL 302 5 2 6 1.1 CCCn1c(=O)c2nc(-c3cn[nH]c3)[nH]c2n(CCC)c1=O 10.1021/jm051268+
CHEMBL380176 140131 None 0 Human Binding pKi = 8.1 8.1 2 4
Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cellsDisplacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells
ChEMBL 302 5 2 6 1.1 CCCn1c(=O)c2nc(-c3cn[nH]c3)[nH]c2n(CCC)c1=O 10.1021/jm051268+
10852506 106981 None 0 Human Binding pKi = 8.0 8.0 -11 6
Displacement of [3H]-DPCPX from Adenosine A2b receptor expressed in CHO cells; range 7.4-11.3Displacement of [3H]-DPCPX from Adenosine A2b receptor expressed in CHO cells; range 7.4-11.3
ChEMBL 311 4 1 8 2.4 CC(C)CCn1cc2c(nc(N)n3nc(-c4ccco4)nc23)n1 10.1021/jm001047y
CHEMBL315150 106981 None 0 Human Binding pKi = 8.0 8.0 -11 6
Displacement of [3H]-DPCPX from Adenosine A2b receptor expressed in CHO cells; range 7.4-11.3Displacement of [3H]-DPCPX from Adenosine A2b receptor expressed in CHO cells; range 7.4-11.3
ChEMBL 311 4 1 8 2.4 CC(C)CCn1cc2c(nc(N)n3nc(-c4ccco4)nc23)n1 10.1021/jm001047y
44219684 195768 None 0 Human Binding pKi = 8.0 8.0 12 4
Binding affinity to human adenosine A2b receptor expressed in HEK293 cellsBinding affinity to human adenosine A2b receptor expressed in HEK293 cells
ChEMBL 502 10 2 9 2.5 CCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(C#N)cc4)cc3)nc2n(CCCOC)c1=O 10.1016/j.bmc.2009.03.029
CHEMBL557694 195768 None 0 Human Binding pKi = 8.0 8.0 12 4
Binding affinity to human adenosine A2b receptor expressed in HEK293 cellsBinding affinity to human adenosine A2b receptor expressed in HEK293 cells
ChEMBL 502 10 2 9 2.5 CCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(C#N)cc4)cc3)nc2n(CCCOC)c1=O 10.1016/j.bmc.2009.03.029
44450955 167389 None 0 Human Binding pKi = 8.0 8.0 43 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 530 8 1 7 3.9 CCCn1c(=O)n(C)c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCC(c5ccc(OC)cc5)CC4)cc3)cc21 10.1016/j.bmc.2008.01.002
CHEMBL429512 167389 None 0 Human Binding pKi = 8.0 8.0 43 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 530 8 1 7 3.9 CCCn1c(=O)n(C)c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCC(c5ccc(OC)cc5)CC4)cc3)cc21 10.1016/j.bmc.2008.01.002
10204847 74426 None 0 Human Binding pKi = 8.0 8.0 23 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 460 9 2 6 4.0 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccccc4)cc3)cc2n(CCC)c1=O 10.1021/jm0506221
CHEMBL202665 74426 None 0 Human Binding pKi = 8.0 8.0 23 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 460 9 2 6 4.0 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccccc4)cc3)cc2n(CCC)c1=O 10.1021/jm0506221
136002248 71158 None 0 Human Binding pKi = 8.0 8.0 269 2
Displacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation countingDisplacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation counting
ChEMBL 564 8 2 9 4.2 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5c(Cl)cc(C(F)(F)F)cc5[nH]4)nn3C)nc2n(CCC)c1=O 10.1021/jm201292w
CHEMBL1955907 71158 None 0 Human Binding pKi = 8.0 8.0 269 2
Displacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation countingDisplacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation counting
ChEMBL 564 8 2 9 4.2 CCCn1c(=O)c2[nH]c(-c3cc(OCc4nc5c(Cl)cc(C(F)(F)F)cc5[nH]4)nn3C)nc2n(CCC)c1=O 10.1021/jm201292w
44574118 178806 None 0 Human Binding pKi = 8.0 8.0 1 4
Displacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells by beta scintillation counterDisplacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells by beta scintillation counter
ChEMBL 422 4 2 6 3.1 Cn1c(=O)c2[nH]c(-c3ccc(COC(=O)Nc4ccc(F)cc4)cc3)cc2n(C)c1=O 10.1016/j.bmc.2009.03.062
CHEMBL469119 178806 None 0 Human Binding pKi = 8.0 8.0 1 4
Displacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells by beta scintillation counterDisplacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells by beta scintillation counter
ChEMBL 422 4 2 6 3.1 Cn1c(=O)c2[nH]c(-c3ccc(COC(=O)Nc4ccc(F)cc4)cc3)cc2n(C)c1=O 10.1016/j.bmc.2009.03.062
11612118 140689 None 0 Human Binding pKi = 8.0 8.0 11 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 450 7 2 6 3.3 CCCn1c(=O)n(C)c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(F)cc4)cc3)cc21 10.1021/jm0506221
CHEMBL381538 140689 None 0 Human Binding pKi = 8.0 8.0 11 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 450 7 2 6 3.3 CCCn1c(=O)n(C)c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc(F)cc4)cc3)cc21 10.1021/jm0506221
44450826 95876 None 0 Human Binding pKi = 8.0 8.0 25 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 524 8 1 6 3.9 O=C(COc1ccc(-c2cc3c([nH]2)c(=O)n(CC2CC2)c(=O)n3CC2CC2)cc1)N1CCc2ccccc2C1 10.1016/j.bmc.2008.01.002
CHEMBL259104 95876 None 0 Human Binding pKi = 8.0 8.0 25 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 524 8 1 6 3.9 O=C(COc1ccc(-c2cc3c([nH]2)c(=O)n(CC2CC2)c(=O)n3CC2CC2)cc1)N1CCc2ccccc2C1 10.1016/j.bmc.2008.01.002
44451253 96015 None 0 Human Binding pKi = 8.0 8.0 33 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 491 5 1 7 2.1 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCN(c5ccc(F)cc5)CC4)cc3)cc2n(C)c1=O 10.1016/j.bmc.2008.01.002
CHEMBL259733 96015 None 0 Human Binding pKi = 8.0 8.0 33 2
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 491 5 1 7 2.1 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCN(c5ccc(F)cc5)CC4)cc3)cc2n(C)c1=O 10.1016/j.bmc.2008.01.002
44450958 96051 None 0 Human Binding pKi = 8.0 8.0 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 548 6 1 6 4.2 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCC(c5ccccc5)(c5ccccc5)CC4)cc3)cc2n(C)c1=O 10.1016/j.bmc.2008.01.002
CHEMBL259931 96051 None 0 Human Binding pKi = 8.0 8.0 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 548 6 1 6 4.2 Cn1c(=O)c2[nH]c(-c3ccc(OCC(=O)N4CCC(c5ccccc5)(c5ccccc5)CC4)cc3)cc2n(C)c1=O 10.1016/j.bmc.2008.01.002
66893166 156964 None 0 Human Binding pKi = 8.0 8.0 - 1
Displacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting methodDisplacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting method
ChEMBL 493 8 1 8 2.8 CCCn1c(=O)c2[nH]c(-c3cnn(CC4CC(=O)N(c5ccc(F)cc5)C4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2016.11.007
CHEMBL4072877 156964 None 0 Human Binding pKi = 8.0 8.0 - 1
Displacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting methodDisplacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting method
ChEMBL 493 8 1 8 2.8 CCCn1c(=O)c2[nH]c(-c3cnn(CC4CC(=O)N(c5ccc(F)cc5)C4)c3)nc2n(CCC)c1=O 10.1016/j.ejmech.2016.11.007
11656075 72308 None 0 Human Binding pKi = 8.0 8.0 2 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 488 10 2 6 4.8 CCCn1c(=O)c2[nH]c(-c3ccc(OC(CC)C(=O)Nc4ccccc4)cc3)cc2n(CCC)c1=O 10.1021/jm0506221
CHEMBL198338 72308 None 0 Human Binding pKi = 8.0 8.0 2 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 488 10 2 6 4.8 CCCn1c(=O)c2[nH]c(-c3ccc(OC(CC)C(=O)Nc4ccccc4)cc3)cc2n(CCC)c1=O 10.1021/jm0506221
2690 903 None 66 Human Binding pKi = 8.0 8.0 -30 9
Displacement of [3H]MRE-2029F20 from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]MRE-2029F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 285 1 1 6 2.8 Clc1ccc2c(c1)c1nc(nn1c(n2)N)c1ccco1 10.1021/jm900413e
384 903 None 66 Human Binding pKi = 8.0 8.0 -30 9
Displacement of [3H]MRE-2029F20 from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]MRE-2029F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 285 1 1 6 2.8 Clc1ccc2c(c1)c1nc(nn1c(n2)N)c1ccco1 10.1021/jm900413e
CHEMBL16687 903 None 66 Human Binding pKi = 8.0 8.0 -30 9
Displacement of [3H]MRE-2029F20 from human recombinant adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]MRE-2029F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells
ChEMBL 285 1 1 6 2.8 Clc1ccc2c(c1)c1nc(nn1c(n2)N)c1ccco1 10.1021/jm900413e
57429610 158849 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 minsDisplacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 mins
ChEMBL 486 6 1 8 3.1 CCCn1c(=O)c2[nH]c(-c3cnn(CC#Cc4ccc(OC(F)(F)F)cc4)c3)nc2n(CC)c1=O 10.1016/j.ejmech.2017.04.014
CHEMBL4094840 158849 None 0 Human Binding pKi = 8 8.0 - 1
Displacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 minsDisplacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes after 90 mins
ChEMBL 486 6 1 8 3.1 CCCn1c(=O)c2[nH]c(-c3cnn(CC#Cc4ccc(OC(F)(F)F)cc4)c3)nc2n(CC)c1=O 10.1016/j.ejmech.2017.04.014
135499926 99923 None 0 Human Binding pKi = 7.1 7.1 1 2
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 623 11 2 9 4.9 CCCn1c(=O)c2nc(-c3cc(NC(=O)Cc4ccc(OCc5cccc(C(F)(F)F)c5)cc4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
CHEMBL286212 99923 None 0 Human Binding pKi = 7.1 7.1 1 2
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 623 11 2 9 4.9 CCCn1c(=O)c2nc(-c3cc(NC(=O)Cc4ccc(OCc5cccc(C(F)(F)F)c5)cc4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
135465778 100403 None 0 Human Binding pKi = 7.1 7.1 22 2
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 480 8 3 9 2.8 CCCn1c(=O)c2nc(-c3cc(NC(=O)Nc4cccc(OC)c4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
CHEMBL290105 100403 None 0 Human Binding pKi = 7.1 7.1 22 2
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 480 8 3 9 2.8 CCCn1c(=O)c2nc(-c3cc(NC(=O)Nc4cccc(OC)c4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
216466 3845 None 32 Human Binding pKi = 7.1 7.1 -123 6
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 416 8 2 6 3.2 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C12CCC(CC1)(CC2)CCC(=O)O 10.1016/j.bmc.2010.01.072
5605 3845 None 32 Human Binding pKi = 7.1 7.1 -123 6
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 416 8 2 6 3.2 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C12CCC(CC1)(CC2)CCC(=O)O 10.1016/j.bmc.2010.01.072
CHEMBL386974 3845 None 32 Human Binding pKi = 7.1 7.1 -123 6
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 416 8 2 6 3.2 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C12CCC(CC1)(CC2)CCC(=O)O 10.1016/j.bmc.2010.01.072
CHEMBL414157 3845 None 32 Human Binding pKi = 7.1 7.1 -123 6
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 416 8 2 6 3.2 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C12CCC(CC1)(CC2)CCC(=O)O 10.1016/j.bmc.2010.01.072
DB12569 3845 None 32 Human Binding pKi = 7.1 7.1 -123 6
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 416 8 2 6 3.2 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C12CCC(CC1)(CC2)CCC(=O)O 10.1016/j.bmc.2010.01.072
216466 3845 None 32 Human Binding pKi = 7.1 7.1 -123 6
Displacement of [125I]3-(4-aminobenzyl)-8-phenyloxyacetate-1-propyl-xanthine from human adenosine A2B receptorDisplacement of [125I]3-(4-aminobenzyl)-8-phenyloxyacetate-1-propyl-xanthine from human adenosine A2B receptor
ChEMBL 416 8 2 6 3.2 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C12CCC(CC1)(CC2)CCC(=O)O 10.1021/jm060539t
5605 3845 None 32 Human Binding pKi = 7.1 7.1 -123 6
Displacement of [125I]3-(4-aminobenzyl)-8-phenyloxyacetate-1-propyl-xanthine from human adenosine A2B receptorDisplacement of [125I]3-(4-aminobenzyl)-8-phenyloxyacetate-1-propyl-xanthine from human adenosine A2B receptor
ChEMBL 416 8 2 6 3.2 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C12CCC(CC1)(CC2)CCC(=O)O 10.1021/jm060539t
CHEMBL386974 3845 None 32 Human Binding pKi = 7.1 7.1 -123 6
Displacement of [125I]3-(4-aminobenzyl)-8-phenyloxyacetate-1-propyl-xanthine from human adenosine A2B receptorDisplacement of [125I]3-(4-aminobenzyl)-8-phenyloxyacetate-1-propyl-xanthine from human adenosine A2B receptor
ChEMBL 416 8 2 6 3.2 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C12CCC(CC1)(CC2)CCC(=O)O 10.1021/jm060539t
CHEMBL414157 3845 None 32 Human Binding pKi = 7.1 7.1 -123 6
Displacement of [125I]3-(4-aminobenzyl)-8-phenyloxyacetate-1-propyl-xanthine from human adenosine A2B receptorDisplacement of [125I]3-(4-aminobenzyl)-8-phenyloxyacetate-1-propyl-xanthine from human adenosine A2B receptor
ChEMBL 416 8 2 6 3.2 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C12CCC(CC1)(CC2)CCC(=O)O 10.1021/jm060539t
DB12569 3845 None 32 Human Binding pKi = 7.1 7.1 -123 6
Displacement of [125I]3-(4-aminobenzyl)-8-phenyloxyacetate-1-propyl-xanthine from human adenosine A2B receptorDisplacement of [125I]3-(4-aminobenzyl)-8-phenyloxyacetate-1-propyl-xanthine from human adenosine A2B receptor
ChEMBL 416 8 2 6 3.2 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C12CCC(CC1)(CC2)CCC(=O)O 10.1021/jm060539t
216466 3845 None 32 Human Binding pKi = 7.1 7.1 -123 6
Displacement of [125I]3-(4-aminobenzyl)-8-phenyloxyacetate-1-propyl-xanthine from human adenosine A2B receptor expressed in HEK cellsDisplacement of [125I]3-(4-aminobenzyl)-8-phenyloxyacetate-1-propyl-xanthine from human adenosine A2B receptor expressed in HEK cells
ChEMBL 416 8 2 6 3.2 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C12CCC(CC1)(CC2)CCC(=O)O 10.1021/jm0605381
5605 3845 None 32 Human Binding pKi = 7.1 7.1 -123 6
Displacement of [125I]3-(4-aminobenzyl)-8-phenyloxyacetate-1-propyl-xanthine from human adenosine A2B receptor expressed in HEK cellsDisplacement of [125I]3-(4-aminobenzyl)-8-phenyloxyacetate-1-propyl-xanthine from human adenosine A2B receptor expressed in HEK cells
ChEMBL 416 8 2 6 3.2 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C12CCC(CC1)(CC2)CCC(=O)O 10.1021/jm0605381
CHEMBL386974 3845 None 32 Human Binding pKi = 7.1 7.1 -123 6
Displacement of [125I]3-(4-aminobenzyl)-8-phenyloxyacetate-1-propyl-xanthine from human adenosine A2B receptor expressed in HEK cellsDisplacement of [125I]3-(4-aminobenzyl)-8-phenyloxyacetate-1-propyl-xanthine from human adenosine A2B receptor expressed in HEK cells
ChEMBL 416 8 2 6 3.2 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C12CCC(CC1)(CC2)CCC(=O)O 10.1021/jm0605381
CHEMBL414157 3845 None 32 Human Binding pKi = 7.1 7.1 -123 6
Displacement of [125I]3-(4-aminobenzyl)-8-phenyloxyacetate-1-propyl-xanthine from human adenosine A2B receptor expressed in HEK cellsDisplacement of [125I]3-(4-aminobenzyl)-8-phenyloxyacetate-1-propyl-xanthine from human adenosine A2B receptor expressed in HEK cells
ChEMBL 416 8 2 6 3.2 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C12CCC(CC1)(CC2)CCC(=O)O 10.1021/jm0605381
DB12569 3845 None 32 Human Binding pKi = 7.1 7.1 -123 6
Displacement of [125I]3-(4-aminobenzyl)-8-phenyloxyacetate-1-propyl-xanthine from human adenosine A2B receptor expressed in HEK cellsDisplacement of [125I]3-(4-aminobenzyl)-8-phenyloxyacetate-1-propyl-xanthine from human adenosine A2B receptor expressed in HEK cells
ChEMBL 416 8 2 6 3.2 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C12CCC(CC1)(CC2)CCC(=O)O 10.1021/jm0605381
136414898 157426 None 0 Human Binding pKi = 7.1 7.1 - 1
Displacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting methodDisplacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting method
ChEMBL 510 9 1 9 2.9 CCCn1c(=O)c2[nH]c(-c3cc(OCC4CC(=O)N(c5cccc(F)c5)C4)no3)nc2n(CCC)c1=O 10.1016/j.ejmech.2016.11.007
CHEMBL4078707 157426 None 0 Human Binding pKi = 7.1 7.1 - 1
Displacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting methodDisplacement of [3H]-MRS-1754 from human adenosine receptor A2b expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting method
ChEMBL 510 9 1 9 2.9 CCCn1c(=O)c2[nH]c(-c3cc(OCC4CC(=O)N(c5cccc(F)c5)C4)no3)nc2n(CCC)c1=O 10.1016/j.ejmech.2016.11.007
10696675 28896 None 0 Human Binding pKi = 7.1 7.1 1 6
Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 81-101Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 81-101
ChEMBL 498 6 2 8 5.3 O=C(Nc1cccc(Cl)c1)Nc1nc2nn(CCc3ccccc3)cc2c2nc(-c3ccco3)nn12 10.1021/jm001047y
CHEMBL137950 28896 None 0 Human Binding pKi = 7.1 7.1 1 6
Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 81-101Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 81-101
ChEMBL 498 6 2 8 5.3 O=C(Nc1cccc(Cl)c1)Nc1nc2nn(CCc3ccccc3)cc2c2nc(-c3ccco3)nn12 10.1021/jm001047y
10587109 118785 None 0 Human Binding pKi = 7.1 7.1 -31 4
Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 81-101Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 81-101
ChEMBL 255 1 1 8 0.9 Cn1cc2c(nc(N)n3nc(-c4ccco4)nc23)n1 10.1021/jm001047y
CHEMBL342059 118785 None 0 Human Binding pKi = 7.1 7.1 -31 4
Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 81-101Displacement of [3H]DPCPX from Adenosine A2b receptor expressed in CHO cells; range 81-101
ChEMBL 255 1 1 8 0.9 Cn1cc2c(nc(N)n3nc(-c4ccco4)nc23)n1 10.1021/jm001047y
10587109 118785 None 0 Human Binding pKi = 7.1 7.1 -31 4
Displacement of [3H]DPCPX from human A2B receptor expressed in CHO cells by scintillation counterDisplacement of [3H]DPCPX from human A2B receptor expressed in CHO cells by scintillation counter
ChEMBL 255 1 1 8 0.9 Cn1cc2c(nc(N)n3nc(-c4ccco4)nc23)n1 10.1016/j.ejmech.2015.12.019
CHEMBL342059 118785 None 0 Human Binding pKi = 7.1 7.1 -31 4
Displacement of [3H]DPCPX from human A2B receptor expressed in CHO cells by scintillation counterDisplacement of [3H]DPCPX from human A2B receptor expressed in CHO cells by scintillation counter
ChEMBL 255 1 1 8 0.9 Cn1cc2c(nc(N)n3nc(-c4ccco4)nc23)n1 10.1016/j.ejmech.2015.12.019
24827594 157819 None 0 Human Binding pKi = 6.1 6.1 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes after 30 minsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes after 30 mins
ChEMBL 274 3 2 5 1.2 CCOC(=O)C1=C(C)N/C(=N\C#N)NC1c1ccco1 10.1021/acs.jmedchem.7b00138
CHEMBL4083334 157819 None 0 Human Binding pKi = 6.1 6.1 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes after 30 minsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes after 30 mins
ChEMBL 274 3 2 5 1.2 CCOC(=O)C1=C(C)N/C(=N\C#N)NC1c1ccco1 10.1021/acs.jmedchem.7b00138
2153 3800 None 115 Human Binding pKi = 5.1 5.1 -21 14
Displacement of [125I]ABOPX from human adenosine receptor A2b expressed in HEK293 cell membranes after 3 hrs by fluorescence assayDisplacement of [125I]ABOPX from human adenosine receptor A2b expressed in HEK293 cell membranes after 3 hrs by fluorescence assay
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1016/j.ejmech.2016.11.007
2153.0 3800 None 115 Human Binding pKi = 5.1 5.1 -21 14
Displacement of [125I]ABOPX from human adenosine receptor A2b expressed in HEK293 cell membranes after 3 hrs by fluorescence assayDisplacement of [125I]ABOPX from human adenosine receptor A2b expressed in HEK293 cell membranes after 3 hrs by fluorescence assay
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1016/j.ejmech.2016.11.007
2620 3800 None 115 Human Binding pKi = 5.1 5.1 -21 14
Displacement of [125I]ABOPX from human adenosine receptor A2b expressed in HEK293 cell membranes after 3 hrs by fluorescence assayDisplacement of [125I]ABOPX from human adenosine receptor A2b expressed in HEK293 cell membranes after 3 hrs by fluorescence assay
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1016/j.ejmech.2016.11.007
413 3800 None 115 Human Binding pKi = 5.1 5.1 -21 14
Displacement of [125I]ABOPX from human adenosine receptor A2b expressed in HEK293 cell membranes after 3 hrs by fluorescence assayDisplacement of [125I]ABOPX from human adenosine receptor A2b expressed in HEK293 cell membranes after 3 hrs by fluorescence assay
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1016/j.ejmech.2016.11.007
CHEMBL190 3800 None 115 Human Binding pKi = 5.1 5.1 -21 14
Displacement of [125I]ABOPX from human adenosine receptor A2b expressed in HEK293 cell membranes after 3 hrs by fluorescence assayDisplacement of [125I]ABOPX from human adenosine receptor A2b expressed in HEK293 cell membranes after 3 hrs by fluorescence assay
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1016/j.ejmech.2016.11.007
DB00277 3800 None 115 Human Binding pKi = 5.1 5.1 -21 14
Displacement of [125I]ABOPX from human adenosine receptor A2b expressed in HEK293 cell membranes after 3 hrs by fluorescence assayDisplacement of [125I]ABOPX from human adenosine receptor A2b expressed in HEK293 cell membranes after 3 hrs by fluorescence assay
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1016/j.ejmech.2016.11.007
162666447 182288 None 0 Human Binding pKi = 6.0 6.0 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 259 2 2 4 2.4 CC1=C(c2ncc(C)o2)C(c2ccco2)NC(=O)N1 10.1021/acs.jmedchem.0c01431
CHEMBL4783984 182288 None 0 Human Binding pKi = 6.0 6.0 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 259 2 2 4 2.4 CC1=C(c2ncc(C)o2)C(c2ccco2)NC(=O)N1 10.1021/acs.jmedchem.0c01431
9968253 190189 None 0 Human Binding pKi = 6.0 6.0 -223 4
Displacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation countingDisplacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation counting
ChEMBL 350 4 1 9 1.9 COC(=O)c1cccc(Cn2nnc3c(-c4ccco4)nc(N)nc32)c1 10.1021/jm800961g
CHEMBL517429 190189 None 0 Human Binding pKi = 6.0 6.0 -223 4
Displacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation countingDisplacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation counting
ChEMBL 350 4 1 9 1.9 COC(=O)c1cccc(Cn2nnc3c(-c4ccco4)nc(N)nc32)c1 10.1021/jm800961g
2153 3800 None 115 Human Binding pKi = 5.0 5.0 -21 14
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1021/jm0104318
2153.0 3800 None 115 Human Binding pKi = 5.0 5.0 -21 14
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1021/jm0104318
2620 3800 None 115 Human Binding pKi = 5.0 5.0 -21 14
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1021/jm0104318
413 3800 None 115 Human Binding pKi = 5.0 5.0 -21 14
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1021/jm0104318
CHEMBL190 3800 None 115 Human Binding pKi = 5.0 5.0 -21 14
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1021/jm0104318
DB00277 3800 None 115 Human Binding pKi = 5.0 5.0 -21 14
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1021/jm0104318
2153 3800 None 115 Human Binding pKi = 5.0 5.0 -21 14
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1016/j.bmc.2010.01.072
2153 3800 None 115 Human Binding pKi = 5.0 5.0 -21 14
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1016/j.bmc.2013.09.044
2153.0 3800 None 115 Human Binding pKi = 5.0 5.0 -21 14
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1016/j.bmc.2010.01.072
2153.0 3800 None 115 Human Binding pKi = 5.0 5.0 -21 14
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1016/j.bmc.2013.09.044
2620 3800 None 115 Human Binding pKi = 5.0 5.0 -21 14
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1016/j.bmc.2010.01.072
2620 3800 None 115 Human Binding pKi = 5.0 5.0 -21 14
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1016/j.bmc.2013.09.044
413 3800 None 115 Human Binding pKi = 5.0 5.0 -21 14
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1016/j.bmc.2010.01.072
413 3800 None 115 Human Binding pKi = 5.0 5.0 -21 14
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1016/j.bmc.2013.09.044
CHEMBL190 3800 None 115 Human Binding pKi = 5.0 5.0 -21 14
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1016/j.bmc.2010.01.072
CHEMBL190 3800 None 115 Human Binding pKi = 5.0 5.0 -21 14
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1016/j.bmc.2013.09.044
DB00277 3800 None 115 Human Binding pKi = 5.0 5.0 -21 14
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1016/j.bmc.2010.01.072
DB00277 3800 None 115 Human Binding pKi = 5.0 5.0 -21 14
Binding affinity to human adenosine A2B receptorBinding affinity to human adenosine A2B receptor
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1016/j.bmc.2013.09.044
2153 3800 None 115 Human Binding pKi = 5.0 5.0 -21 14
Binding affinity to human adenosine A2B receptor by radioligand displacement assayBinding affinity to human adenosine A2B receptor by radioligand displacement assay
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1039/C8MD00070K
2153.0 3800 None 115 Human Binding pKi = 5.0 5.0 -21 14
Binding affinity to human adenosine A2B receptor by radioligand displacement assayBinding affinity to human adenosine A2B receptor by radioligand displacement assay
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1039/C8MD00070K
2620 3800 None 115 Human Binding pKi = 5.0 5.0 -21 14
Binding affinity to human adenosine A2B receptor by radioligand displacement assayBinding affinity to human adenosine A2B receptor by radioligand displacement assay
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1039/C8MD00070K
413 3800 None 115 Human Binding pKi = 5.0 5.0 -21 14
Binding affinity to human adenosine A2B receptor by radioligand displacement assayBinding affinity to human adenosine A2B receptor by radioligand displacement assay
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1039/C8MD00070K
CHEMBL190 3800 None 115 Human Binding pKi = 5.0 5.0 -21 14
Binding affinity to human adenosine A2B receptor by radioligand displacement assayBinding affinity to human adenosine A2B receptor by radioligand displacement assay
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1039/C8MD00070K
DB00277 3800 None 115 Human Binding pKi = 5.0 5.0 -21 14
Binding affinity to human adenosine A2B receptor by radioligand displacement assayBinding affinity to human adenosine A2B receptor by radioligand displacement assay
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1039/C8MD00070K
2153 3800 None 115 Human Binding pKi = 5.0 5.0 -21 14
Displacement of [125I]-ABOPX from human recombinant Adenosine A2B receptor expressed in HEK293 cells after 3 hrsDisplacement of [125I]-ABOPX from human recombinant Adenosine A2B receptor expressed in HEK293 cells after 3 hrs
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1021/acs.jmedchem.5b01586
2153.0 3800 None 115 Human Binding pKi = 5.0 5.0 -21 14
Displacement of [125I]-ABOPX from human recombinant Adenosine A2B receptor expressed in HEK293 cells after 3 hrsDisplacement of [125I]-ABOPX from human recombinant Adenosine A2B receptor expressed in HEK293 cells after 3 hrs
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1021/acs.jmedchem.5b01586
2620 3800 None 115 Human Binding pKi = 5.0 5.0 -21 14
Displacement of [125I]-ABOPX from human recombinant Adenosine A2B receptor expressed in HEK293 cells after 3 hrsDisplacement of [125I]-ABOPX from human recombinant Adenosine A2B receptor expressed in HEK293 cells after 3 hrs
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1021/acs.jmedchem.5b01586
413 3800 None 115 Human Binding pKi = 5.0 5.0 -21 14
Displacement of [125I]-ABOPX from human recombinant Adenosine A2B receptor expressed in HEK293 cells after 3 hrsDisplacement of [125I]-ABOPX from human recombinant Adenosine A2B receptor expressed in HEK293 cells after 3 hrs
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1021/acs.jmedchem.5b01586
CHEMBL190 3800 None 115 Human Binding pKi = 5.0 5.0 -21 14
Displacement of [125I]-ABOPX from human recombinant Adenosine A2B receptor expressed in HEK293 cells after 3 hrsDisplacement of [125I]-ABOPX from human recombinant Adenosine A2B receptor expressed in HEK293 cells after 3 hrs
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1021/acs.jmedchem.5b01586
DB00277 3800 None 115 Human Binding pKi = 5.0 5.0 -21 14
Displacement of [125I]-ABOPX from human recombinant Adenosine A2B receptor expressed in HEK293 cells after 3 hrsDisplacement of [125I]-ABOPX from human recombinant Adenosine A2B receptor expressed in HEK293 cells after 3 hrs
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1021/acs.jmedchem.5b01586
2153 3800 None 115 Human Binding pKi = 5.0 5.0 -21 14
Displacement of [3H]PSB-603 from human adenosine receptor A2B expressed in CHO cell membranes incubated for 75 mins by radioligand competition assayDisplacement of [3H]PSB-603 from human adenosine receptor A2B expressed in CHO cell membranes incubated for 75 mins by radioligand competition assay
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1016/j.ejmech.2019.111879
2153.0 3800 None 115 Human Binding pKi = 5.0 5.0 -21 14
Displacement of [3H]PSB-603 from human adenosine receptor A2B expressed in CHO cell membranes incubated for 75 mins by radioligand competition assayDisplacement of [3H]PSB-603 from human adenosine receptor A2B expressed in CHO cell membranes incubated for 75 mins by radioligand competition assay
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1016/j.ejmech.2019.111879
2620 3800 None 115 Human Binding pKi = 5.0 5.0 -21 14
Displacement of [3H]PSB-603 from human adenosine receptor A2B expressed in CHO cell membranes incubated for 75 mins by radioligand competition assayDisplacement of [3H]PSB-603 from human adenosine receptor A2B expressed in CHO cell membranes incubated for 75 mins by radioligand competition assay
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1016/j.ejmech.2019.111879
413 3800 None 115 Human Binding pKi = 5.0 5.0 -21 14
Displacement of [3H]PSB-603 from human adenosine receptor A2B expressed in CHO cell membranes incubated for 75 mins by radioligand competition assayDisplacement of [3H]PSB-603 from human adenosine receptor A2B expressed in CHO cell membranes incubated for 75 mins by radioligand competition assay
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1016/j.ejmech.2019.111879
CHEMBL190 3800 None 115 Human Binding pKi = 5.0 5.0 -21 14
Displacement of [3H]PSB-603 from human adenosine receptor A2B expressed in CHO cell membranes incubated for 75 mins by radioligand competition assayDisplacement of [3H]PSB-603 from human adenosine receptor A2B expressed in CHO cell membranes incubated for 75 mins by radioligand competition assay
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1016/j.ejmech.2019.111879
DB00277 3800 None 115 Human Binding pKi = 5.0 5.0 -21 14
Displacement of [3H]PSB-603 from human adenosine receptor A2B expressed in CHO cell membranes incubated for 75 mins by radioligand competition assayDisplacement of [3H]PSB-603 from human adenosine receptor A2B expressed in CHO cell membranes incubated for 75 mins by radioligand competition assay
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1016/j.ejmech.2019.111879
2153 3800 None 115 Human Binding pKi = 5.0 5.0 -21 14
Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cellsDisplacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1021/jm051268+
2153.0 3800 None 115 Human Binding pKi = 5.0 5.0 -21 14
Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cellsDisplacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1021/jm051268+
2620 3800 None 115 Human Binding pKi = 5.0 5.0 -21 14
Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cellsDisplacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1021/jm051268+
413 3800 None 115 Human Binding pKi = 5.0 5.0 -21 14
Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cellsDisplacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1021/jm051268+
CHEMBL190 3800 None 115 Human Binding pKi = 5.0 5.0 -21 14
Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cellsDisplacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1021/jm051268+
DB00277 3800 None 115 Human Binding pKi = 5.0 5.0 -21 14
Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cellsDisplacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells
ChEMBL 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 10.1021/jm051268+
44390523 63816 None 0 Human Binding pKi = 7.0 7.0 1 3
Binding affinity for adenosine A2b receptor by using as [3H]ZM-241385 (14 nM) radioligand in membranes from HEK-A2B cellsBinding affinity for adenosine A2b receptor by using as [3H]ZM-241385 (14 nM) radioligand in membranes from HEK-A2B cells
ChEMBL 500 9 1 9 4.3 CCCn1c(=O)c2nc(-c3ccc(OCc4noc(-c5ccc(C)cc5)n4)cc3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2004.11.044
CHEMBL180236 63816 None 0 Human Binding pKi = 7.0 7.0 1 3
Binding affinity for adenosine A2b receptor by using as [3H]ZM-241385 (14 nM) radioligand in membranes from HEK-A2B cellsBinding affinity for adenosine A2b receptor by using as [3H]ZM-241385 (14 nM) radioligand in membranes from HEK-A2B cells
ChEMBL 500 9 1 9 4.3 CCCn1c(=O)c2nc(-c3ccc(OCc4noc(-c5ccc(C)cc5)n4)cc3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2004.11.044
11584408 73378 None 0 Human Binding pKi = 7.0 7.0 7 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 518 10 2 6 4.2 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc([N+](C)(C)C)cc4)cc3)cc2n(CCC)c1=O 10.1021/jm0506221
CHEMBL201447 73378 None 0 Human Binding pKi = 7.0 7.0 7 2
Binding affinity to recombinant human adenosine A2B receptorBinding affinity to recombinant human adenosine A2B receptor
ChEMBL 518 10 2 6 4.2 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4ccc([N+](C)(C)C)cc4)cc3)cc2n(CCC)c1=O 10.1021/jm0506221
25066016 96189 None 2 Human Binding pKi = 6.0 6.0 -275 4
Binding affinity at human adenosine A2B receptorBinding affinity at human adenosine A2B receptor
ChEMBL 259 2 0 5 3.7 c1csc(-c2nc(C3CC3)nc3ccsc23)n1 10.1016/j.bmcl.2008.03.076
CHEMBL260719 96189 None 2 Human Binding pKi = 6.0 6.0 -275 4
Binding affinity at human adenosine A2B receptorBinding affinity at human adenosine A2B receptor
ChEMBL 259 2 0 5 3.7 c1csc(-c2nc(C3CC3)nc3ccsc23)n1 10.1016/j.bmcl.2008.03.076
145993147 166960 None 0 Human Binding pKi = 6.0 6.0 -1 3
Displacement of [3H]PSB-602 from human adenosine A2B receptor expressed in CHO cell membranesDisplacement of [3H]PSB-602 from human adenosine A2B receptor expressed in CHO cell membranes
ChEMBL 581 13 1 11 1.5 CCCn1c(=O)c2c(nc3n2CCCN3CCc2ccc(OCC(=O)NCCN3CCOCC3)cc2)n(CCC)c1=O 10.1039/C8MD00070K
CHEMBL4287298 166960 None 0 Human Binding pKi = 6.0 6.0 -1 3
Displacement of [3H]PSB-602 from human adenosine A2B receptor expressed in CHO cell membranesDisplacement of [3H]PSB-602 from human adenosine A2B receptor expressed in CHO cell membranes
ChEMBL 581 13 1 11 1.5 CCCn1c(=O)c2c(nc3n2CCCN3CCc2ccc(OCC(=O)NCCN3CCOCC3)cc2)n(CCC)c1=O 10.1039/C8MD00070K
21874722 176820 None 0 Human Binding pKi = 6.0 6.0 -3 3
Displacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation countingDisplacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation counting
ChEMBL 321 4 2 8 1.6 NCc1ccc(Cn2nnc3c(-c4ccco4)nc(N)nc32)cc1 10.1021/jm800961g
CHEMBL460976 176820 None 0 Human Binding pKi = 6.0 6.0 -3 3
Displacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation countingDisplacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation counting
ChEMBL 321 4 2 8 1.6 NCc1ccc(Cn2nnc3c(-c4ccco4)nc(N)nc32)cc1 10.1021/jm800961g
11392671 195290 None 0 Human Binding pKi = 6.0 6.0 -416 4
Binding affinity to adenosine A2B receptorBinding affinity to adenosine A2B receptor
ChEMBL 308 4 2 5 2.6 Cc1ccccc1CNC(=O)c1cc(-c2ccco2)nc(N)n1 10.1016/j.bmcl.2009.03.142
CHEMBL551368 195290 None 0 Human Binding pKi = 6.0 6.0 -416 4
Binding affinity to adenosine A2B receptorBinding affinity to adenosine A2B receptor
ChEMBL 308 4 2 5 2.6 Cc1ccccc1CNC(=O)c1cc(-c2ccco2)nc(N)n1 10.1016/j.bmcl.2009.03.142
156020727 178106 None 0 Human Binding pKi = 7.0 7.0 -6 2
Displacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting methodDisplacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting method
ChEMBL 323 3 2 6 2.6 CCOC(=O)C1=C(C)Nc2nc3ccccc3n2C1c1cn[nH]c1 10.1021/acs.jmedchem.0c00564
CHEMBL4647965 178106 None 0 Human Binding pKi = 7.0 7.0 -6 2
Displacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting methodDisplacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting method
ChEMBL 323 3 2 6 2.6 CCOC(=O)C1=C(C)Nc2nc3ccccc3n2C1c1cn[nH]c1 10.1021/acs.jmedchem.0c00564
45270541 195200 None 0 Human Binding pKi = 6.0 6.0 -194 4
Binding affinity to adenosine A2B receptorBinding affinity to adenosine A2B receptor
ChEMBL 312 4 2 5 2.4 Nc1nc(C(=O)NCc2cccc(F)c2)cc(-c2ccco2)n1 10.1016/j.bmcl.2009.03.142
CHEMBL550636 195200 None 0 Human Binding pKi = 6.0 6.0 -194 4
Binding affinity to adenosine A2B receptorBinding affinity to adenosine A2B receptor
ChEMBL 312 4 2 5 2.4 Nc1nc(C(=O)NCc2cccc(F)c2)cc(-c2ccco2)n1 10.1016/j.bmcl.2009.03.142
135483531 78541 None 0 Human Binding pKi = 7.0 7.0 1 2
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 543 9 2 9 2.9 CCCn1c(=O)c2[nH]c(-c3cc(OCC(=O)Nc4ccc(Br)cc4)n(C)n3)nc2n(CCC)c1=O 10.1021/jm0309654
CHEMBL2112067 78541 None 0 Human Binding pKi = 7.0 7.0 1 2
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 543 9 2 9 2.9 CCCn1c(=O)c2[nH]c(-c3cc(OCC(=O)Nc4ccc(Br)cc4)n(C)n3)nc2n(CCC)c1=O 10.1021/jm0309654
45270544 195201 None 0 Human Binding pKi = 7.0 7.0 2 2
Binding affinity to human adenosine A2b receptor expressed in HEK293 cellsBinding affinity to human adenosine A2b receptor expressed in HEK293 cells
ChEMBL 517 10 3 9 2.5 CCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4nc5ccccc5[nH]4)cc3)nc2n(CCCOC)c1=O 10.1016/j.bmc.2009.03.029
CHEMBL550638 195201 None 0 Human Binding pKi = 7.0 7.0 2 2
Binding affinity to human adenosine A2b receptor expressed in HEK293 cellsBinding affinity to human adenosine A2b receptor expressed in HEK293 cells
ChEMBL 517 10 3 9 2.5 CCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)Nc4nc5ccccc5[nH]4)cc3)nc2n(CCCOC)c1=O 10.1016/j.bmc.2009.03.029
46227957 201370 None 0 Human Binding pKi = 7.0 7.0 1 3
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 402 7 1 8 2.5 CSCCn1c(=O)c2[nH]c(Cc3cccs3)nc2n(Cc2ccco2)c1=O 10.1016/j.bmc.2009.07.034
CHEMBL604492 201370 None 0 Human Binding pKi = 7.0 7.0 1 3
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cellsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cells
ChEMBL 402 7 1 8 2.5 CSCCn1c(=O)c2[nH]c(Cc3cccs3)nc2n(Cc2ccco2)c1=O 10.1016/j.bmc.2009.07.034
44316058 205537 None 0 Rat Binding pKi = 6.0 6.0 -104 3
Compound was tested for its binding affinity against Alpha-2 adrenergic receptorCompound was tested for its binding affinity against Alpha-2 adrenergic receptor
ChEMBL 468 11 4 6 4.8 Oc1ccc(C[C@@H]2CCCN2CCCCCCN2CCC[C@@H]2Cc2ccc(O)c(O)c2)cc1O 10.1016/0960-894X(95)00413-N
CHEMBL80974 205537 None 0 Rat Binding pKi = 6.0 6.0 -104 3
Compound was tested for its binding affinity against Alpha-2 adrenergic receptorCompound was tested for its binding affinity against Alpha-2 adrenergic receptor
ChEMBL 468 11 4 6 4.8 Oc1ccc(C[C@@H]2CCCN2CCCCCCN2CCC[C@@H]2Cc2ccc(O)c(O)c2)cc1O 10.1016/0960-894X(95)00413-N
21874520 176807 None 0 Human Binding pKi = 6.0 6.0 -42 4
Displacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation countingDisplacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation counting
ChEMBL 391 5 1 8 2.6 CC(C)N(C)C(=O)c1cccc(Cn2nnc3c(-c4ccco4)nc(N)nc32)c1 10.1021/jm800961g
CHEMBL460805 176807 None 0 Human Binding pKi = 6.0 6.0 -42 4
Displacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation countingDisplacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation counting
ChEMBL 391 5 1 8 2.6 CC(C)N(C)C(=O)c1cccc(Cn2nnc3c(-c4ccco4)nc(N)nc32)c1 10.1021/jm800961g
44390571 64306 None 0 Human Binding pKi = 6.0 6.0 - 1
Binding affinity for adenosine A2b receptor by using as [3H]ZM-241385 (14 nM) radioligand in membranes from HEK-A2B cellsBinding affinity for adenosine A2b receptor by using as [3H]ZM-241385 (14 nM) radioligand in membranes from HEK-A2B cells
ChEMBL 554 9 1 9 5.0 CCCn1c(=O)c2nc(-c3ccc(OCc4nc(-c5cccc(C(F)(F)F)c5)no4)cc3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2004.11.044
CHEMBL181067 64306 None 0 Human Binding pKi = 6.0 6.0 - 1
Binding affinity for adenosine A2b receptor by using as [3H]ZM-241385 (14 nM) radioligand in membranes from HEK-A2B cellsBinding affinity for adenosine A2b receptor by using as [3H]ZM-241385 (14 nM) radioligand in membranes from HEK-A2B cells
ChEMBL 554 9 1 9 5.0 CCCn1c(=O)c2nc(-c3ccc(OCc4nc(-c5cccc(C(F)(F)F)c5)no4)cc3)[nH]c2n(CCC)c1=O 10.1016/j.bmcl.2004.11.044
101422 91546 None 15 Human Binding pKi = 5.0 5.0 -2 3
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 218 1 0 6 -0.9 C#CCn1cnc2c1c(=O)n(C)c(=O)n2C 10.1021/jm0104318
CHEMBL24049 91546 None 15 Human Binding pKi = 5.0 5.0 -2 3
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 218 1 0 6 -0.9 C#CCn1cnc2c1c(=O)n(C)c(=O)n2C 10.1021/jm0104318
9794423 102178 None 1 Human Binding pKi = 5.0 5.0 - 1
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 218 1 0 6 -0.9 C#CCn1c(=O)n(C)c(=O)c2c1ncn2C 10.1021/jm0104318
CHEMBL302725 102178 None 1 Human Binding pKi = 5.0 5.0 - 1
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 218 1 0 6 -0.9 C#CCn1c(=O)n(C)c(=O)c2c1ncn2C 10.1021/jm0104318
101446 92313 None 28 Human Binding pKi = 5.0 5.0 1 3
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 220 2 0 6 -0.4 C=CCn1cnc2c1c(=O)n(C)c(=O)n2C 10.1021/jm0104318
CHEMBL24289 92313 None 28 Human Binding pKi = 5.0 5.0 1 3
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 220 2 0 6 -0.4 C=CCn1cnc2c1c(=O)n(C)c(=O)n2C 10.1021/jm0104318
44281663 168041 None 0 Human Binding pKi = 7.0 7.0 18 2
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 505 10 2 8 3.6 CCCn1c(=O)c2nc(-c3ccc(NC(=O)Cc4ccc(OC)c(OC)c4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm0309654
CHEMBL432273 168041 None 0 Human Binding pKi = 7.0 7.0 18 2
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 505 10 2 8 3.6 CCCn1c(=O)c2nc(-c3ccc(NC(=O)Cc4ccc(OC)c(OC)c4)cc3)[nH]c2n(CCC)c1=O 10.1021/jm0309654
162669067 182761 None 0 Human Binding pKi = 7.0 7.0 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 276 3 2 4 2.0 CC1=C(C(=O)OC2CCC2)C(c2ccco2)NC(=O)N1 10.1021/acs.jmedchem.0c01431
CHEMBL4790210 182761 None 0 Human Binding pKi = 7.0 7.0 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 276 3 2 4 2.0 CC1=C(C(=O)OC2CCC2)C(c2ccco2)NC(=O)N1 10.1021/acs.jmedchem.0c01431
168288152 191830 None 0 Human Binding pKi = 6.0 6.0 - 1
Displacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cell membrane and measured after 0.5 hrs by radioligand displacement assayDisplacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cell membrane and measured after 0.5 hrs by radioligand displacement assay
ChEMBL 394 6 1 7 2.0 CCCn1c(=O)c2[nH]c(-c3cccc(S(=O)(=O)F)c3)nc2n(CCC)c1=O 10.1039/d2md00132b
CHEMBL5198830 191830 None 0 Human Binding pKi = 6.0 6.0 - 1
Displacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cell membrane and measured after 0.5 hrs by radioligand displacement assayDisplacement of [3H]PSB-603 from human adenosine A2B receptor expressed in CHO cell membrane and measured after 0.5 hrs by radioligand displacement assay
ChEMBL 394 6 1 7 2.0 CCCn1c(=O)c2[nH]c(-c3cccc(S(=O)(=O)F)c3)nc2n(CCC)c1=O 10.1039/d2md00132b
135522363 170582 None 0 Human Binding pKi = 7.0 7.0 - 1
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 479 9 2 9 2.3 CCCn1c(=O)c2nc(-c3cc(NC(=O)Cc4cccc(OC)c4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
CHEMBL445056 170582 None 0 Human Binding pKi = 7.0 7.0 - 1
Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cellsBinding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells
ChEMBL 479 9 2 9 2.3 CCCn1c(=O)c2nc(-c3cc(NC(=O)Cc4cccc(OC)c4)nn3C)[nH]c2n(CCC)c1=O 10.1021/jm0309654
137649307 157285 None 0 Human Binding pKi = 7.0 7.0 -6 3
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes after 30 minsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes after 30 mins
ChEMBL 348 5 1 4 4.4 COc1cccc(-c2cc(NC(C)=O)nc(-c3cccc(OC)c3)c2)c1 10.1021/acs.jmedchem.7b00860
CHEMBL4076880 157285 None 0 Human Binding pKi = 7.0 7.0 -6 3
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes after 30 minsDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes after 30 mins
ChEMBL 348 5 1 4 4.4 COc1cccc(-c2cc(NC(C)=O)nc(-c3cccc(OC)c3)c2)c1 10.1021/acs.jmedchem.7b00860
163215620 190343 None 0 Human Binding pKi = 7.0 7.0 -398 4
Displacement of [3H]DPCPX from human A2BAR expressed in HEK293 cells membrane assessed as inhibition constant preincubated for 5 mins followed by [3H]DPCPX addition and measured after 1.5 hrs by TopCount scintillation counting methodDisplacement of [3H]DPCPX from human A2BAR expressed in HEK293 cells membrane assessed as inhibition constant preincubated for 5 mins followed by [3H]DPCPX addition and measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 318 3 2 6 1.8 Nc1nc(C(=O)NCc2ccccn2)cn2c1nc1ccccc12 10.1021/acs.jmedchem.2c00101
CHEMBL5176737 190343 None 0 Human Binding pKi = 7.0 7.0 -398 4
Displacement of [3H]DPCPX from human A2BAR expressed in HEK293 cells membrane assessed as inhibition constant preincubated for 5 mins followed by [3H]DPCPX addition and measured after 1.5 hrs by TopCount scintillation counting methodDisplacement of [3H]DPCPX from human A2BAR expressed in HEK293 cells membrane assessed as inhibition constant preincubated for 5 mins followed by [3H]DPCPX addition and measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 318 3 2 6 1.8 Nc1nc(C(=O)NCc2ccccn2)cn2c1nc1ccccc12 10.1021/acs.jmedchem.2c00101
CHEMBL5203105 190343 None 0 Human Binding pKi = 7.0 7.0 -398 4
Displacement of [3H]DPCPX from human A2BAR expressed in HEK293 cells membrane assessed as inhibition constant preincubated for 5 mins followed by [3H]DPCPX addition and measured after 1.5 hrs by TopCount scintillation counting methodDisplacement of [3H]DPCPX from human A2BAR expressed in HEK293 cells membrane assessed as inhibition constant preincubated for 5 mins followed by [3H]DPCPX addition and measured after 1.5 hrs by TopCount scintillation counting method
ChEMBL 318 3 2 6 1.8 Nc1nc(C(=O)NCc2ccccn2)cn2c1nc1ccccc12 10.1021/acs.jmedchem.2c00101
155542720 173163 None 0 Human Binding pKi = 7.0 7.0 11 2
Displacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 552 8 3 8 1.7 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc(C(=O)O)cc5)CC4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
CHEMBL4521715 173163 None 0 Human Binding pKi = 7.0 7.0 11 2
Displacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting methodDisplacement of [3H]PSB-603 from recombinant human A2B adenosine receptor expressed in CHO cell membranes measured after 75 mins in presence of adenosine deaminase by liquid scintillation counting method
ChEMBL 552 8 3 8 1.7 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc(C(=O)O)cc5)CC4)cc3)[nH]c2c1=O 10.1021/acs.jmedchem.9b00071
10998551 102117 None 0 Human Binding pKi = 6.0 6.0 -1 3
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 220 1 2 4 0.5 O=c1[nH]c2[nH]cnc2c(=O)n1C1CCCC1 10.1021/jm0104318
CHEMBL302344 102117 None 0 Human Binding pKi = 6.0 6.0 -1 3
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 220 1 2 4 0.5 O=c1[nH]c2[nH]cnc2c(=O)n1C1CCCC1 10.1021/jm0104318
11004373 120252 None 0 Human Binding pKi = 7.0 7.0 -10 4
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 67-141Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 67-141
ChEMBL 422 4 2 8 4.1 CCn1cc2c(nc(NC(=O)Nc3ccccc3Cl)n3nc(-c4ccco4)nc23)n1 10.1021/jm0109614
CHEMBL352345 120252 None 0 Human Binding pKi = 7.0 7.0 -10 4
Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 67-141Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells; range 67-141
ChEMBL 422 4 2 8 4.1 CCn1cc2c(nc(NC(=O)Nc3ccccc3Cl)n3nc(-c4ccco4)nc23)n1 10.1021/jm0109614
46837841 10625 None 0 Human Binding pKi = 7.0 7.0 - 1
Displacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells after 30 minsDisplacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells after 30 mins
ChEMBL 514 8 0 7 4.0 CCCn1c(=O)c2c(cc(-c3ccc(OCC(=O)N4CCc5ccccc5C4)cc3)n2C)n(CCC)c1=O 10.1016/j.ejmech.2010.03.011
CHEMBL1170168 10625 None 0 Human Binding pKi = 7.0 7.0 - 1
Displacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells after 30 minsDisplacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cells after 30 mins
ChEMBL 514 8 0 7 4.0 CCCn1c(=O)c2c(cc(-c3ccc(OCC(=O)N4CCc5ccccc5C4)cc3)n2C)n(CCC)c1=O 10.1016/j.ejmech.2010.03.011
56627882 118512 None 0 Human Binding pKi = 6.0 6.0 -194 5
Displacement of [3H]-DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by liquid scintillation counting analysis
ChEMBL 367 3 3 12 -0.9 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1039/C5MD00086F
CHEMBL3414937 118512 None 0 Human Binding pKi = 6.0 6.0 -194 5
Displacement of [3H]-DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by liquid scintillation counting analysisDisplacement of [3H]-DPCPX from human adenosine A2B receptor expressed in HEK293 cells after 30 mins by liquid scintillation counting analysis
ChEMBL 367 3 3 12 -0.9 CCn1nnc([C@H]2O[C@@H](n3cnc4c(N)nc(Cl)nc43)[C@H](O)[C@@H]2O)n1 10.1039/C5MD00086F
681 1465 None 72 Rat Binding pKi = 6.0 6.0 -15 39
Compound was tested for its binding affinity against Alpha-2 adrenergic receptorCompound was tested for its binding affinity against Alpha-2 adrenergic receptor
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/0960-894X(95)00413-N
681.0 1465 None 72 Rat Binding pKi = 6.0 6.0 -15 39
Compound was tested for its binding affinity against Alpha-2 adrenergic receptorCompound was tested for its binding affinity against Alpha-2 adrenergic receptor
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/0960-894X(95)00413-N
940 1465 None 72 Rat Binding pKi = 6.0 6.0 -15 39
Compound was tested for its binding affinity against Alpha-2 adrenergic receptorCompound was tested for its binding affinity against Alpha-2 adrenergic receptor
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/0960-894X(95)00413-N
947 1465 None 72 Rat Binding pKi = 6.0 6.0 -15 39
Compound was tested for its binding affinity against Alpha-2 adrenergic receptorCompound was tested for its binding affinity against Alpha-2 adrenergic receptor
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/0960-894X(95)00413-N
CHEMBL59 1465 None 72 Rat Binding pKi = 6.0 6.0 -15 39
Compound was tested for its binding affinity against Alpha-2 adrenergic receptorCompound was tested for its binding affinity against Alpha-2 adrenergic receptor
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/0960-894X(95)00413-N
DB00988 1465 None 72 Rat Binding pKi = 6.0 6.0 -15 39
Compound was tested for its binding affinity against Alpha-2 adrenergic receptorCompound was tested for its binding affinity against Alpha-2 adrenergic receptor
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1016/0960-894X(95)00413-N
156018247 177780 None 0 Human Binding pKi = 7.0 7.0 -4 2
Displacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting methodDisplacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting method
ChEMBL 340 3 1 7 3.3 CCOC(=O)C1=C(C)Nc2nc3ccccc3n2C1c1ccns1 10.1021/acs.jmedchem.0c00564
CHEMBL4643113 177780 None 0 Human Binding pKi = 7.0 7.0 -4 2
Displacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting methodDisplacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting method
ChEMBL 340 3 1 7 3.3 CCOC(=O)C1=C(C)Nc2nc3ccccc3n2C1c1ccns1 10.1021/acs.jmedchem.0c00564
11524593 141278 None 0 Human Binding pKi = 6.0 6.0 -1 3
Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cellsDisplacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells
ChEMBL 420 9 1 7 3.4 CCCCn1c(=O)c2nc(-c3cnn(Cc4ccccc4)c3)[nH]c2n(CCCC)c1=O 10.1021/jm051268+
CHEMBL383201 141278 None 0 Human Binding pKi = 6.0 6.0 -1 3
Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cellsDisplacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells
ChEMBL 420 9 1 7 3.4 CCCCn1c(=O)c2nc(-c3cnn(Cc4ccccc4)c3)[nH]c2n(CCCC)c1=O 10.1021/jm051268+
3123319 28717 None 7 Human Binding pKi = 6.0 6.0 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 252 2 2 5 1.7 COC(=O)C1=C(C)N=C(S)NC1c1ccco1 10.1021/acs.jmedchem.0c01431
CHEMBL1377918 28717 None 7 Human Binding pKi = 6.0 6.0 - 1
Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting methodDisplacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method
ChEMBL 252 2 2 5 1.7 COC(=O)C1=C(C)N=C(S)NC1c1ccco1 10.1021/acs.jmedchem.0c01431
19818540 75409 None 0 Human Binding pKi = 5 5.0 -5 2
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 354 6 1 5 3.3 CC(C)CCn1c(=O)c2nc(-c3ccccc3)[nH]c2n(CC(C)C)c1=O 10.1021/jm0104318
CHEMBL20402 75409 None 0 Human Binding pKi = 5 5.0 -5 2
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
ChEMBL 354 6 1 5 3.3 CC(C)CCn1c(=O)c2nc(-c3ccccc3)[nH]c2n(CC(C)C)c1=O 10.1021/jm0104318
11655061 139173 None 0 Human Binding pKi = 6 6.0 -1 3
Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cellsDisplacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells
ChEMBL 438 7 1 7 3.2 CC(C)Cn1c(=O)c2nc(-c3cnn(Cc4cccc(F)c4)c3)[nH]c2n(CC(C)C)c1=O 10.1021/jm051268+
CHEMBL378743 139173 None 0 Human Binding pKi = 6 6.0 -1 3
Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cellsDisplacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells
ChEMBL 438 7 1 7 3.2 CC(C)Cn1c(=O)c2nc(-c3cnn(Cc4cccc(F)c4)c3)[nH]c2n(CC(C)C)c1=O 10.1021/jm051268+
CHEMBL5079363 214615 None 0 Human Binding pKi = 5 5.0 -457 4
Displacement of [3H] DPCPX from human recombinant A2B adenosine receptor expressed in HEK293 cells incubated for 30 mins by radioligand binding competition assayDisplacement of [3H] DPCPX from human recombinant A2B adenosine receptor expressed in HEK293 cells incubated for 30 mins by radioligand binding competition assay
ChEMBL None None None Cc1cnc(-c2nc3c(-c4ccc(=O)n(C)c4)cnc(N)n3n2)s1 10.1021/acsmedchemlett.1c00599
3284 3216 None 35 Human Binding pKd = 9.4 9.4 -1 7
UnclassifiedUnclassified
Guide to Pharmacology 528 6 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)c1ccc(cc1)Cl 19569717
44185871 3216 None 35 Human Binding pKd = 9.4 9.4 -1 7
UnclassifiedUnclassified
Guide to Pharmacology 528 6 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)c1ccc(cc1)Cl 19569717
5728 3216 None 35 Human Binding pKd = 9.4 9.4 -1 7
UnclassifiedUnclassified
Guide to Pharmacology 528 6 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)c1ccc(cc1)Cl 19569717
CHEMBL483688 3216 None 35 Human Binding pKd = 9.4 9.4 -1 7
UnclassifiedUnclassified
Guide to Pharmacology 528 6 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)c1ccc(cc1)Cl 19569717
3284 3216 None 35 Human Binding pKd = 9.4 9.4 -1 7
UnclassifiedUnclassified
Guide to Pharmacology 528 6 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)c1ccc(cc1)Cl 19569717
44185871 3216 None 35 Human Binding pKd = 9.4 9.4 -1 7
UnclassifiedUnclassified
Guide to Pharmacology 528 6 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)c1ccc(cc1)Cl 19569717
5728 3216 None 35 Human Binding pKd = 9.4 9.4 -1 7
UnclassifiedUnclassified
Guide to Pharmacology 528 6 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)c1ccc(cc1)Cl 19569717
CHEMBL483688 3216 None 35 Human Binding pKd = 9.4 9.4 -1 7
UnclassifiedUnclassified
Guide to Pharmacology 528 6 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)c1ccc(cc1)Cl 19569717
3284 3216 None 35 Mouse Binding pKd = 9.5 9.5 1 7
UnclassifiedUnclassified
Guide to Pharmacology 528 6 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)c1ccc(cc1)Cl 19569717
44185871 3216 None 35 Mouse Binding pKd = 9.5 9.5 1 7
UnclassifiedUnclassified
Guide to Pharmacology 528 6 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)c1ccc(cc1)Cl 19569717
5728 3216 None 35 Mouse Binding pKd = 9.5 9.5 1 7
UnclassifiedUnclassified
Guide to Pharmacology 528 6 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)c1ccc(cc1)Cl 19569717
CHEMBL483688 3216 None 35 Mouse Binding pKd = 9.5 9.5 1 7
UnclassifiedUnclassified
Guide to Pharmacology 528 6 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)c1ccc(cc1)Cl 19569717
3284 3216 None 35 Mouse Binding pKd = 9.5 9.5 1 7
UnclassifiedUnclassified
Guide to Pharmacology 528 6 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)c1ccc(cc1)Cl 19569717
44185871 3216 None 35 Mouse Binding pKd = 9.5 9.5 1 7
UnclassifiedUnclassified
Guide to Pharmacology 528 6 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)c1ccc(cc1)Cl 19569717
5728 3216 None 35 Mouse Binding pKd = 9.5 9.5 1 7
UnclassifiedUnclassified
Guide to Pharmacology 528 6 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)c1ccc(cc1)Cl 19569717
CHEMBL483688 3216 None 35 Mouse Binding pKd = 9.5 9.5 1 7
UnclassifiedUnclassified
Guide to Pharmacology 528 6 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)c1ccc(cc1)Cl 19569717
449 2643 None 52 Human Binding pKd = 9.8 9.8 -1 9
UnclassifiedUnclassified
Guide to Pharmacology 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 11266650
453 2643 None 52 Human Binding pKd = 9.8 9.8 -1 9
UnclassifiedUnclassified
Guide to Pharmacology 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 11266650
6603931 2643 None 52 Human Binding pKd = 9.8 9.8 -1 9
UnclassifiedUnclassified
Guide to Pharmacology 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 11266650
CHEMBL273807 2643 None 52 Human Binding pKd = 9.8 9.8 -1 9
UnclassifiedUnclassified
Guide to Pharmacology 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 11266650
450 2970 None 9 Human Binding pKd None 9.8 9.8 257 4
UnclassifiedUnclassified
Guide to Pharmacology 525 10 3 6 3.6 CC(=O)NCCNc1nc(nc2c1cc([nH]2)C(=O)N1CCN(CC1)CCCc1ccccc1)c1ccccc1 15194002
454 2970 None 9 Human Binding pKd None 9.8 9.8 257 4
UnclassifiedUnclassified
Guide to Pharmacology 525 10 3 6 3.6 CC(=O)NCCNc1nc(nc2c1cc([nH]2)C(=O)N1CCN(CC1)CCCc1ccccc1)c1ccccc1 15194002
5311041 2970 None 9 Human Binding pKd None 9.8 9.8 257 4
UnclassifiedUnclassified
Guide to Pharmacology 525 10 3 6 3.6 CC(=O)NCCNc1nc(nc2c1cc([nH]2)C(=O)N1CCN(CC1)CCCc1ccccc1)c1ccccc1 15194002
CHEMBL485862 2970 None 9 Human Binding pKd None 9.8 9.8 257 4
UnclassifiedUnclassified
Guide to Pharmacology 525 10 3 6 3.6 CC(=O)NCCNc1nc(nc2c1cc([nH]2)C(=O)N1CCN(CC1)CCCc1ccccc1)c1ccccc1 15194002
44186666 185658 UNDEFINED 0 Human Binding pKi = 9.8 9.8 144 5
NoneNone
PDSP KiDatabase 562 6 2 7 2.6 CCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc(C(F)(F)F)cc5)CC4)cc3)[nH]c2c1=O None
CHEMBL486478 185658 UNDEFINED 0 Human Binding pKi = 9.8 9.8 144 5
NoneNone
PDSP KiDatabase 562 6 2 7 2.6 CCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc(C(F)(F)F)cc5)CC4)cc3)[nH]c2c1=O None
44186580 184206 UNDEFINED 0 Human Binding pKi = 9.7 9.7 30 6
NoneNone
PDSP KiDatabase 528 6 2 7 2.3 CCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc(Cl)cc5)CC4)cc3)[nH]c2c1=O None
CHEMBL483261 184206 UNDEFINED 0 Human Binding pKi = 9.7 9.7 30 6
NoneNone
PDSP KiDatabase 528 6 2 7 2.3 CCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc(Cl)cc5)CC4)cc3)[nH]c2c1=O None
44186668 191510 UNDEFINED 0 Human Binding pKi = 9.6 9.6 245 6
NoneNone
PDSP KiDatabase 562 6 2 7 2.6 CCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5cccc(C(F)(F)F)c5)CC4)cc3)[nH]c2c1=O None
CHEMBL519390 191510 UNDEFINED 0 Human Binding pKi = 9.6 9.6 245 6
NoneNone
PDSP KiDatabase 562 6 2 7 2.6 CCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5cccc(C(F)(F)F)c5)CC4)cc3)[nH]c2c1=O None
44186667 185659 UNDEFINED 0 Human Binding pKi = 9.5 9.5 478 6
NoneNone
PDSP KiDatabase 576 7 2 7 3.0 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc(C(F)(F)F)cc5)CC4)cc3)[nH]c2c1=O None
CHEMBL486479 185659 UNDEFINED 0 Human Binding pKi = 9.5 9.5 478 6
NoneNone
PDSP KiDatabase 576 7 2 7 3.0 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc(C(F)(F)F)cc5)CC4)cc3)[nH]c2c1=O None
44186581 3205 UNDEFINED 27 Human Binding pKi = 9.4 9.4 851 6
NoneNone
PDSP KiDatabase 542 7 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)Cc1ccc(cc1)Cl None
6561 3205 UNDEFINED 27 Human Binding pKi = 9.4 9.4 851 6
NoneNone
PDSP KiDatabase 542 7 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)Cc1ccc(cc1)Cl None
CHEMBL482436 3205 UNDEFINED 27 Human Binding pKi = 9.4 9.4 851 6
NoneNone
PDSP KiDatabase 542 7 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)Cc1ccc(cc1)Cl None
450 2970 UNDEFINED 9 Human Binding pKi = 9.4 9.4 257 4
NoneNone
PDSP KiDatabase 525 10 3 6 3.6 CC(=O)NCCNc1nc(nc2c1cc([nH]2)C(=O)N1CCN(CC1)CCCc1ccccc1)c1ccccc1 None
454 2970 UNDEFINED 9 Human Binding pKi = 9.4 9.4 257 4
NoneNone
PDSP KiDatabase 525 10 3 6 3.6 CC(=O)NCCNc1nc(nc2c1cc([nH]2)C(=O)N1CCN(CC1)CCCc1ccccc1)c1ccccc1 None
5311041 2970 UNDEFINED 9 Human Binding pKi = 9.4 9.4 257 4
NoneNone
PDSP KiDatabase 525 10 3 6 3.6 CC(=O)NCCNc1nc(nc2c1cc([nH]2)C(=O)N1CCN(CC1)CCCc1ccccc1)c1ccccc1 None
CHEMBL485862 2970 UNDEFINED 9 Human Binding pKi = 9.4 9.4 257 4
NoneNone
PDSP KiDatabase 525 10 3 6 3.6 CC(=O)NCCNc1nc(nc2c1cc([nH]2)C(=O)N1CCN(CC1)CCCc1ccccc1)c1ccccc1 None
44185870 184230 UNDEFINED 0 Human Binding pKi = 9.4 9.4 117 5
NoneNone
PDSP KiDatabase 514 5 2 7 2.3 CCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(c5ccc(Cl)cc5)CC4)cc3)[nH]c2c1=O None
CHEMBL483487 184230 UNDEFINED 0 Human Binding pKi = 9.4 9.4 117 5
NoneNone
PDSP KiDatabase 514 5 2 7 2.3 CCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(c5ccc(Cl)cc5)CC4)cc3)[nH]c2c1=O None
44186626 184609 UNDEFINED 0 Human Binding pKi = 9.4 9.4 245 6
NoneNone
PDSP KiDatabase 526 7 2 7 2.1 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5cccc(F)c5)CC4)cc3)[nH]c2c1=O None
CHEMBL484900 184609 UNDEFINED 0 Human Binding pKi = 9.4 9.4 245 6
NoneNone
PDSP KiDatabase 526 7 2 7 2.1 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5cccc(F)c5)CC4)cc3)[nH]c2c1=O None
44185872 191398 UNDEFINED 0 Human Binding pKi = 9.3 9.3 416 4
NoneNone
PDSP KiDatabase 524 5 2 7 1.9 C#CCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(c5ccc(Cl)cc5)CC4)cc3)[nH]c2c1=O None
CHEMBL519253 191398 UNDEFINED 0 Human Binding pKi = 9.3 9.3 416 4
NoneNone
PDSP KiDatabase 524 5 2 7 1.9 C#CCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(c5ccc(Cl)cc5)CC4)cc3)[nH]c2c1=O None
3284 3216 UNDEFINED 35 Human Binding pKi = 9.3 9.3 -1 7
NoneNone
PDSP KiDatabase 528 6 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)c1ccc(cc1)Cl None
44185871 3216 UNDEFINED 35 Human Binding pKi = 9.3 9.3 -1 7
NoneNone
PDSP KiDatabase 528 6 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)c1ccc(cc1)Cl None
5728 3216 UNDEFINED 35 Human Binding pKi = 9.3 9.3 -1 7
NoneNone
PDSP KiDatabase 528 6 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)c1ccc(cc1)Cl None
CHEMBL483688 3216 UNDEFINED 35 Human Binding pKi = 9.3 9.3 -1 7
NoneNone
PDSP KiDatabase 528 6 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)c1ccc(cc1)Cl None
44186624 192436 UNDEFINED 0 Human Binding pKi = 9.2 9.2 57 4
NoneNone
PDSP KiDatabase 526 7 2 7 2.1 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc(F)cc5)CC4)cc3)[nH]c2c1=O None
CHEMBL520830 192436 UNDEFINED 0 Human Binding pKi = 9.2 9.2 57 4
NoneNone
PDSP KiDatabase 526 7 2 7 2.1 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc(F)cc5)CC4)cc3)[nH]c2c1=O None
44186582 184113 UNDEFINED 0 Human Binding pKi = 9.2 9.2 158 4
NoneNone
PDSP KiDatabase 528 6 2 7 2.3 CCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5cccc(Cl)c5)CC4)cc3)[nH]c2c1=O None
CHEMBL482638 184113 UNDEFINED 0 Human Binding pKi = 9.2 9.2 158 4
NoneNone
PDSP KiDatabase 528 6 2 7 2.3 CCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5cccc(Cl)c5)CC4)cc3)[nH]c2c1=O None
44186625 184608 UNDEFINED 0 Human Binding pKi = 9.2 9.2 208 6
NoneNone
PDSP KiDatabase 512 6 2 7 1.7 CCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5cccc(F)c5)CC4)cc3)[nH]c2c1=O None
CHEMBL484899 184608 UNDEFINED 0 Human Binding pKi = 9.2 9.2 208 6
NoneNone
PDSP KiDatabase 512 6 2 7 1.7 CCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5cccc(F)c5)CC4)cc3)[nH]c2c1=O None
44186669 185797 UNDEFINED 0 Human Binding pKi = 9.1 9.1 354 6
NoneNone
PDSP KiDatabase 576 7 2 7 3.0 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5cccc(C(F)(F)F)c5)CC4)cc3)[nH]c2c1=O None
CHEMBL486688 185797 UNDEFINED 0 Human Binding pKi = 9.1 9.1 354 6
NoneNone
PDSP KiDatabase 576 7 2 7 3.0 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5cccc(C(F)(F)F)c5)CC4)cc3)[nH]c2c1=O None
44186622 184229 UNDEFINED 0 Human Binding pKi = 9.1 9.1 208 6
NoneNone
PDSP KiDatabase 542 7 2 7 2.7 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5cccc(Cl)c5)CC4)cc3)[nH]c2c1=O None
CHEMBL483469 184229 UNDEFINED 0 Human Binding pKi = 9.1 9.1 208 6
NoneNone
PDSP KiDatabase 542 7 2 7 2.7 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5cccc(Cl)c5)CC4)cc3)[nH]c2c1=O None
44186715 191219 UNDEFINED 0 Human Binding pKi = 9.1 9.1 54 4
NoneNone
PDSP KiDatabase 522 7 2 7 2.3 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc(C)cc5)CC4)cc3)[nH]c2c1=O None
CHEMBL518972 191219 UNDEFINED 0 Human Binding pKi = 9.1 9.1 54 4
NoneNone
PDSP KiDatabase 522 7 2 7 2.3 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc(C)cc5)CC4)cc3)[nH]c2c1=O None
44186718 184173 UNDEFINED 0 Human Binding pKi = 9.1 9.1 117 6
NoneNone
PDSP KiDatabase 538 6 2 9 1.3 CCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc6c(c5)OCO6)CC4)cc3)[nH]c2c1=O None
CHEMBL483065 184173 UNDEFINED 0 Human Binding pKi = 9.1 9.1 117 6
NoneNone
PDSP KiDatabase 538 6 2 9 1.3 CCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc6c(c5)OCO6)CC4)cc3)[nH]c2c1=O None
44186717 184145 UNDEFINED 0 Human Binding pKi = 9.0 9.0 89 6
NoneNone
PDSP KiDatabase 538 8 2 8 2.0 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc(OC)cc5)CC4)cc3)[nH]c2c1=O None
CHEMBL482855 184145 UNDEFINED 0 Human Binding pKi = 9.0 9.0 89 6
NoneNone
PDSP KiDatabase 538 8 2 8 2.0 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc(OC)cc5)CC4)cc3)[nH]c2c1=O None
44186719 185916 UNDEFINED 0 Human Binding pKi = 9.0 9.0 74 6
NoneNone
PDSP KiDatabase 552 7 2 9 1.7 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc6c(c5)OCO6)CC4)cc3)[nH]c2c1=O None
CHEMBL486893 185916 UNDEFINED 0 Human Binding pKi = 9.0 9.0 74 6
NoneNone
PDSP KiDatabase 552 7 2 9 1.7 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc6c(c5)OCO6)CC4)cc3)[nH]c2c1=O None
44186579 191784 UNDEFINED 0 Human Binding pKi = 8.9 8.9 131 6
NoneNone
PDSP KiDatabase 494 6 2 7 1.6 CCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccccc5)CC4)cc3)[nH]c2c1=O None
CHEMBL519813 191784 UNDEFINED 0 Human Binding pKi = 8.9 8.9 131 6
NoneNone
PDSP KiDatabase 494 6 2 7 1.6 CCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccccc5)CC4)cc3)[nH]c2c1=O None
44186716 184114 UNDEFINED 0 Human Binding pKi = 8.9 8.9 194 6
NoneNone
PDSP KiDatabase 524 7 2 8 1.6 CCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc(OC)cc5)CC4)cc3)[nH]c2c1=O None
CHEMBL482648 184114 UNDEFINED 0 Human Binding pKi = 8.9 8.9 194 6
NoneNone
PDSP KiDatabase 524 7 2 8 1.6 CCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc(OC)cc5)CC4)cc3)[nH]c2c1=O None
44583036 186955 UNDEFINED 0 Human Binding pKi = 8.9 8.9 7 5
NoneNone
PDSP KiDatabase 400 8 3 7 0.6 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)NCCO)cc3)cc2n(C)c1=O None
CHEMBL490262 186955 UNDEFINED 0 Human Binding pKi = 8.9 8.9 7 5
NoneNone
PDSP KiDatabase 400 8 3 7 0.6 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)NCCO)cc3)cc2n(C)c1=O None
CHEMBL521280 186955 UNDEFINED 0 Human Binding pKi = 8.9 8.9 7 5
NoneNone
PDSP KiDatabase 400 8 3 7 0.6 CCCn1c(=O)c2[nH]c(-c3ccc(OCC(=O)NCCO)cc3)cc2n(C)c1=O None
44186623 192089 UNDEFINED 0 Human Binding pKi = 8.9 8.9 31 6
NoneNone
PDSP KiDatabase 512 6 2 7 1.7 CCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc(F)cc5)CC4)cc3)[nH]c2c1=O None
CHEMBL520297 192089 UNDEFINED 0 Human Binding pKi = 8.9 8.9 31 6
NoneNone
PDSP KiDatabase 512 6 2 7 1.7 CCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc(F)cc5)CC4)cc3)[nH]c2c1=O None
11605883 79952 UNDEFINED 6 Human Binding pKi = 8.9 8.9 42 6
NoneNone
PDSP KiDatabase 508 7 2 7 2.0 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccccc5)CC4)cc3)[nH]c2c1=O None
CHEMBL212625 79952 UNDEFINED 6 Human Binding pKi = 8.9 8.9 42 6
NoneNone
PDSP KiDatabase 508 7 2 7 2.0 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccccc5)CC4)cc3)[nH]c2c1=O None
44186670 192302 UNDEFINED 0 Human Binding pKi = 8.8 8.8 24 4
NoneNone
PDSP KiDatabase 508 6 2 7 1.9 CCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc(C)cc5)CC4)cc3)[nH]c2c1=O None
CHEMBL520617 192302 UNDEFINED 0 Human Binding pKi = 8.8 8.8 24 4
NoneNone
PDSP KiDatabase 508 6 2 7 1.9 CCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccc(C)cc5)CC4)cc3)[nH]c2c1=O None
None 217134 UNDEFINED 0 Human Binding pKi = 8.7 8.7 208 4
NoneNone
PDSP KiDatabase 485 9 2 7 3.9 CCCN1C2=C(C(=O)N(C1=O)CCC)NC(=C2)C3=CC=C(C=C3)OCC(=O)NC4=CC=C(C=C4)C#N None
44185874 185660 UNDEFINED 0 Human Binding pKi = 8.7 8.7 20 5
NoneNone
PDSP KiDatabase 524 7 2 8 2.0 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(c5ccc(OC)cc5)CC4)cc3)[nH]c2c1=O None
CHEMBL486481 185660 UNDEFINED 0 Human Binding pKi = 8.7 8.7 20 5
NoneNone
PDSP KiDatabase 524 7 2 8 2.0 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(c5ccc(OC)cc5)CC4)cc3)[nH]c2c1=O None
982689 199243 UNDEFINED 9 Human Binding pKi = 6 6.0 -141 3
NoneNone
PDSP KiDatabase 414 6 1 5 5.3 COc1ccc(C(=O)c2sc(NC(=O)c3ccccc3)nc2-c2ccccc2)cc1 None
CHEMBL590033 199243 UNDEFINED 9 Human Binding pKi = 6 6.0 -141 3
NoneNone
PDSP KiDatabase 414 6 1 5 5.3 COc1ccc(C(=O)c2sc(NC(=O)c3ccccc3)nc2-c2ccccc2)cc1 None
46229302 199283 UNDEFINED 0 Human Binding pKi = 6 6.0 -14 4
NoneNone
PDSP KiDatabase 382 6 1 6 4.6 CCOC(=O)Nc1nc(-c2ccccc2)c(C(=O)c2ccc(OC)cc2)s1 None
CHEMBL590301 199283 UNDEFINED 0 Human Binding pKi = 6 6.0 -14 4
NoneNone
PDSP KiDatabase 382 6 1 6 4.6 CCOC(=O)Nc1nc(-c2ccccc2)c(C(=O)c2ccc(OC)cc2)s1 None
5033052 199484 UNDEFINED 14 Human Binding pKi = 6 6.0 -173 6
NoneNone
PDSP KiDatabase 374 5 1 5 4.9 O=C(Nc1nc(-c2ccccc2)c(C(=O)c2ccccc2)s1)c1ccco1 None
CHEMBL591710 199484 UNDEFINED 14 Human Binding pKi = 6 6.0 -173 6
NoneNone
PDSP KiDatabase 374 5 1 5 4.9 O=C(Nc1nc(-c2ccccc2)c(C(=O)c2ccccc2)s1)c1ccco1 None
46228971 199603 UNDEFINED 0 Human Binding pKi = 6 6.0 -208 5
NoneNone
PDSP KiDatabase 398 5 1 4 5.6 Cc1ccc(C(=O)c2sc(NC(=O)c3ccccc3)nc2-c2ccccc2)cc1 None
CHEMBL592679 199603 UNDEFINED 0 Human Binding pKi = 6 6.0 -208 5
NoneNone
PDSP KiDatabase 398 5 1 4 5.6 Cc1ccc(C(=O)c2sc(NC(=O)c3ccccc3)nc2-c2ccccc2)cc1 None
981611 200742 UNDEFINED 17 Human Binding pKi = 6 6.0 -104 4
NoneNone
PDSP KiDatabase 384 5 1 4 5.3 O=C(Nc1nc(-c2ccccc2)c(C(=O)c2ccccc2)s1)c1ccccc1 None
CHEMBL600232 200742 UNDEFINED 17 Human Binding pKi = 6 6.0 -104 4
NoneNone
PDSP KiDatabase 384 5 1 4 5.3 O=C(Nc1nc(-c2ccccc2)c(C(=O)c2ccccc2)s1)c1ccccc1 None
7315332 201069 UNDEFINED 5 Human Binding pKi = 6 6.0 -2 3
NoneNone
PDSP KiDatabase 386 5 1 5 5.3 CCOC(=O)Nc1nc(-c2ccccc2)c(C(=O)c2ccc(Cl)cc2)s1 None
CHEMBL602722 201069 UNDEFINED 5 Human Binding pKi = 6 6.0 -2 3
NoneNone
PDSP KiDatabase 386 5 1 5 5.3 CCOC(=O)Nc1nc(-c2ccccc2)c(C(=O)c2ccc(Cl)cc2)s1 None
46228988 201102 UNDEFINED 0 Human Binding pKi = 6 6.0 -83 3
NoneNone
PDSP KiDatabase 408 5 1 5 5.5 O=C(Nc1nc(-c2ccccc2)c(C(=O)c2ccc(Cl)cc2)s1)c1ccco1 None
CHEMBL602950 201102 UNDEFINED 0 Human Binding pKi = 6 6.0 -83 3
NoneNone
PDSP KiDatabase 408 5 1 5 5.5 O=C(Nc1nc(-c2ccccc2)c(C(=O)c2ccc(Cl)cc2)s1)c1ccco1 None
None 217572 UNDEFINED 0 Human Binding pKi = 6 6.0 1 2
NoneNone
PDSP KiDatabase 432 5 1 4 6.3 CC1=CC=C(C=C1)C(=O)NC2=NC(=C(S2)C(=O)C3=CC=C(C=C3)Cl)C4=CC=CC=C4 None
None 217573 UNDEFINED 0 Human Binding pKi = 6 6.0 1 2
NoneNone
PDSP KiDatabase 398 5 1 4 5.6 CC1=CC=C(C=C1)C(=O)NC2=NC(=C(S2)C(=O)C3=CC=CC=C3)C4=CC=CC=C4 None
None 217574 UNDEFINED 0 Human Binding pKi = 6 6.0 1 2
NoneNone
PDSP KiDatabase 462 6 1 6 4.7 CS(=O)(=O)C1=CC=C(C=C1)C(=O)C2=C(N=C(S2)NC(=O)C3=CC=CC=C3)C4=CC=CC=C4 None
None 217575 UNDEFINED 0 Human Binding pKi = 6 6.0 1 2
NoneNone
PDSP KiDatabase 434 6 1 6 5.2 CS(=O)(=O)C1=CC=C(C=C1)C(=O)C2=C(N=C(S2)NC3=CC=CC=C3)C4=CC=CC=C4 None
None 217576 UNDEFINED 0 Human Binding pKi = 6 6.0 1 2
NoneNone
PDSP KiDatabase 370 5 1 4 6.1 CC1=CC=C(C=C1)C(=O)C2=C(N=C(S2)NC3=CC=CC=C3)C4=CC=CC=C4 None
None 217577 UNDEFINED 0 Human Binding pKi = 6 6.0 1 2
NoneNone
PDSP KiDatabase 386 6 1 5 5.8 COC1=CC=C(C=C1)C(=O)C2=C(N=C(S2)NC3=CC=CC=C3)C4=CC=CC=C4 None
None 217578 UNDEFINED 0 Human Binding pKi = 6 6.0 1 2
NoneNone
PDSP KiDatabase 328 4 1 4 4.7 CNC1=NC(=C(S1)C(=O)C2=CC=C(C=C2)Cl)C3=CC=CC=C3 None
None 217579 UNDEFINED 0 Human Binding pKi = 6 6.0 1 2
NoneNone
PDSP KiDatabase 324 5 1 5 4.1 CNC1=NC(=C(S1)C(=O)C2=CC=C(C=C2)OC)C3=CC=CC=C3 None
None 217580 UNDEFINED 0 Human Binding pKi = 6 6.0 1 2
NoneNone
PDSP KiDatabase 294 4 1 4 4.1 CNC1=NC(=C(S1)C(=O)C2=CC=CC=C2)C3=CC=CC=C3 None
2519 779 UNDEFINED 86 Human Binding pKi = 5 5.0 -11 12
NoneNone
PDSP KiDatabase 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C None
2519.0 779 UNDEFINED 86 Human Binding pKi = 5 5.0 -11 12
NoneNone
PDSP KiDatabase 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C None
407 779 UNDEFINED 86 Human Binding pKi = 5 5.0 -11 12
NoneNone
PDSP KiDatabase 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C None
463 779 UNDEFINED 86 Human Binding pKi = 5 5.0 -11 12
NoneNone
PDSP KiDatabase 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C None
CHEMBL113 779 UNDEFINED 86 Human Binding pKi = 5 5.0 -11 12
NoneNone
PDSP KiDatabase 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C None
DB00201 779 UNDEFINED 86 Human Binding pKi = 5 5.0 -11 12
NoneNone
PDSP KiDatabase 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C None
380 1287 125I-ABOPX 54 Human Binding pKi = 5 5.0 -17782 13
NoneNone
PDSP KiDatabase 335 4 4 9 -0.2 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NC1CCCC1 None
657378 1287 125I-ABOPX 54 Human Binding pKi = 5 5.0 -17782 13
NoneNone
PDSP KiDatabase 335 4 4 9 -0.2 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NC1CCCC1 None
CHEMBL68738 1287 125I-ABOPX 54 Human Binding pKi = 5 5.0 -17782 13
NoneNone
PDSP KiDatabase 335 4 4 9 -0.2 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NC1CCCC1 None
11081 3217 UNDEFINED 5 Human Binding pKi = 5 5.0 -30 6
NoneNone
PDSP KiDatabase 378 3 1 7 1.4 Cn1c(=O)n(C)c(=O)c2c1nc1n2CCCN1CCc1c[nH]c2c1cccc2 None
44437220 3217 UNDEFINED 5 Human Binding pKi = 5 5.0 -30 6
NoneNone
PDSP KiDatabase 378 3 1 7 1.4 Cn1c(=O)n(C)c(=O)c2c1nc1n2CCCN1CCc1c[nH]c2c1cccc2 None
CHEMBL239232 3217 UNDEFINED 5 Human Binding pKi = 5 5.0 -30 6
NoneNone
PDSP KiDatabase 378 3 1 7 1.4 Cn1c(=O)n(C)c(=O)c2c1nc1n2CCCN1CCc1c[nH]c2c1cccc2 None
44437219 90651 UNDEFINED 0 Human Binding pKi = 5 5.0 -1 2
NoneNone
PDSP KiDatabase 340 3 0 8 0.3 Cn1c(=O)c2c(nc3n2CCCN3CCc2ccccn2)n(C)c1=O None
CHEMBL239018 90651 UNDEFINED 0 Human Binding pKi = 5 5.0 -1 2
NoneNone
PDSP KiDatabase 340 3 0 8 0.3 Cn1c(=O)c2c(nc3n2CCCN3CCc2ccccn2)n(C)c1=O None
3162488 91144 UNDEFINED 10 Human Binding pKi = 5 5.0 -31 5
NoneNone
PDSP KiDatabase 339 3 0 7 0.9 Cn1c(=O)c2c(nc3n2CCCN3CCc2ccccc2)n(C)c1=O None
CHEMBL239864 91144 UNDEFINED 10 Human Binding pKi = 5 5.0 -31 5
NoneNone
PDSP KiDatabase 339 3 0 7 0.9 Cn1c(=O)c2c(nc3n2CCCN3CCc2ccccc2)n(C)c1=O None
11003653 145838 UNDEFINED 0 Human Binding pKi = 5 5.0 -2 4
NoneNone
PDSP KiDatabase 389 4 0 8 1.4 Cn1c(=O)c2c(nc3n2CCCN3CCOc2ccc(Cl)cc2)n(C)c1=O None
CHEMBL391718 145838 UNDEFINED 0 Human Binding pKi = 5 5.0 -2 4
NoneNone
PDSP KiDatabase 389 4 0 8 1.4 Cn1c(=O)c2c(nc3n2CCCN3CCOc2ccc(Cl)cc2)n(C)c1=O None
44437233 154933 UNDEFINED 0 Human Binding pKi = 5 5.0 -1 3
NoneNone
PDSP KiDatabase 368 5 1 8 0.4 Cn1c(=O)c2c(nc3n2CCCN3CCNCc2ccccc2)n(C)c1=O None
CHEMBL401028 154933 UNDEFINED 0 Human Binding pKi = 5 5.0 -1 3
NoneNone
PDSP KiDatabase 368 5 1 8 0.4 Cn1c(=O)c2c(nc3n2CCCN3CCNCc2ccccc2)n(C)c1=O None
3668 216122 125I-ABOPX 0 Human Binding pKi = 5 5.0 -9120 10
NoneNone
PDSP KiDatabase 510 5 4 9 0.4 CNC(=O)C1C(C(C(O1)N2C=NC3=C2N=CN=C3NCC4=CC(=CC=C4)I)O)O None
None 216127 125I-ABOPX 0 Human Binding pKi = 5 5.0 -8511 5
NoneNone
PDSP KiDatabase 385 6 4 9 0.5 CC(CC1=CC=CC=C1)NC2=NC=NC3=C2N=CN3C4C(C(C(O4)CO)O)O None
None 216292 125I-ABOPX 0 Human Binding pKi = 5 5.0 -660 6
NoneNone
PDSP KiDatabase 499 10 6 11 -0.2 CCNC(=O)C1C(C(C(O1)N2C=NC3=C2N=C(N=C3N)NCCC4=CC=C(C=C4)CCC(=O)O)O)O None
235481 216294 125I-ABOPX 0 Human Binding pKi = 5 5.0 -1258 4
NoneNone
PDSP KiDatabase 301 2 4 9 -1.3 C1=NC2=C(N1C3C(C(C(O3)CO)O)O)N=C(N=C2N)Cl None
235481 216294 UNDEFINED 0 Human Binding pKi = 5 5.0 -1258 4
NoneNone
PDSP KiDatabase 301 2 4 9 -1.3 C1=NC2=C(N1C3C(C(C(O3)CO)O)O)N=C(N=C2N)Cl None
None 216295 125I-ABOPX 0 Human Binding pKi = 5 5.0 - 1
NoneNone
PDSP KiDatabase 527 6 6 11 -0.1 C1=CC(=C(C=C1CCNC2=NC3=C(C(=N2)N)N=CN3C4C(C(C(O4)CO)O)O)I)N None
44583035 172741 UNDEFINED 0 Human Binding pKi = 8.0 8.0 7 4
NoneNone
PDSP KiDatabase 593 5 1 10 3.4 Cn1c(=O)c2[nH]c(-c3ccc(OC(C)(C)C(=O)N4CCN(c5nc6cc(Cl)ccc6s5)CC4)cc3)nc2n(C)c1=O None
CHEMBL450826 172741 UNDEFINED 0 Human Binding pKi = 8.0 8.0 7 4
NoneNone
PDSP KiDatabase 593 5 1 10 3.4 Cn1c(=O)c2[nH]c(-c3ccc(OC(C)(C)C(=O)N4CCN(c5nc6cc(Cl)ccc6s5)CC4)cc3)nc2n(C)c1=O None
44185873 192487 UNDEFINED 0 Human Binding pKi = 7.9 7.9 31 3
NoneNone
PDSP KiDatabase 510 6 2 8 1.6 CCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(c5ccc(OC)cc5)CC4)cc3)[nH]c2c1=O None
CHEMBL520899 192487 UNDEFINED 0 Human Binding pKi = 7.9 7.9 31 3
NoneNone
PDSP KiDatabase 510 6 2 8 1.6 CCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(c5ccc(OC)cc5)CC4)cc3)[nH]c2c1=O None
1328 1369 125I-ABOPX 35 Human Binding pKi = 7.9 7.9 -7 4
NoneNone
PDSP KiDatabase 284 3 1 5 1.6 CCn1c2nc([nH]c2c(=O)n(c1=O)CC)c1ccccc1 None
445 1369 125I-ABOPX 35 Human Binding pKi = 7.9 7.9 -7 4
NoneNone
PDSP KiDatabase 284 3 1 5 1.6 CCn1c2nc([nH]c2c(=O)n(c1=O)CC)c1ccccc1 None
CHEMBL11348 1369 125I-ABOPX 35 Human Binding pKi = 7.9 7.9 -7 4
NoneNone
PDSP KiDatabase 284 3 1 5 1.6 CCn1c2nc([nH]c2c(=O)n(c1=O)CC)c1ccccc1 None
404 4098 3H-cAMP 33 Human Binding pKi = 7.9 7.9 -154 11
NoneNone
PDSP KiDatabase 428 10 3 8 0.8 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)NCCN None
432 4098 3H-cAMP 33 Human Binding pKi = 7.9 7.9 -154 11
NoneNone
PDSP KiDatabase 428 10 3 8 0.8 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)NCCN None
5697 4098 3H-cAMP 33 Human Binding pKi = 7.9 7.9 -154 11
NoneNone
PDSP KiDatabase 428 10 3 8 0.8 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)NCCN None
CHEMBL273094 4098 3H-cAMP 33 Human Binding pKi = 7.9 7.9 -154 11
NoneNone
PDSP KiDatabase 428 10 3 8 0.8 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)NCCN None
2690 903 UNDEFINED 66 Human Binding pKi = 7.8 7.8 -30 9
NoneNone
PDSP KiDatabase 285 1 1 6 2.8 Clc1ccc2c(c1)c1nc(nn1c(n2)N)c1ccco1 None
384 903 UNDEFINED 66 Human Binding pKi = 7.8 7.8 -30 9
NoneNone
PDSP KiDatabase 285 1 1 6 2.8 Clc1ccc2c(c1)c1nc(nn1c(n2)N)c1ccco1 None
CHEMBL16687 903 UNDEFINED 66 Human Binding pKi = 7.8 7.8 -30 9
NoneNone
PDSP KiDatabase 285 1 1 6 2.8 Clc1ccc2c(c1)c1nc(nn1c(n2)N)c1ccco1 None
377 2758 UNDEFINED 53 Human Binding pKi = 5.7 5.7 -1479 15
NoneNone
PDSP KiDatabase 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N None
425 2758 UNDEFINED 53 Human Binding pKi = 5.7 5.7 -1479 15
NoneNone
PDSP KiDatabase 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N None
448222 2758 UNDEFINED 53 Human Binding pKi = 5.7 5.7 -1479 15
NoneNone
PDSP KiDatabase 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N None
CHEMBL464859 2758 UNDEFINED 53 Human Binding pKi = 5.7 5.7 -1479 15
NoneNone
PDSP KiDatabase 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N None
44185935 185533 UNDEFINED 0 Human Binding pKi = 7.7 7.7 4 4
NoneNone
PDSP KiDatabase 417 5 2 6 1.7 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCCCC4)cc3)[nH]c2c1=O None
CHEMBL486281 185533 UNDEFINED 0 Human Binding pKi = 7.7 7.7 4 4
NoneNone
PDSP KiDatabase 417 5 2 6 1.7 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCCCC4)cc3)[nH]c2c1=O None
11270783 1226 UNDEFINED 35 Human Binding pKi = 7.7 7.7 67 4
NoneNone
PDSP KiDatabase 446 6 1 7 3.2 CCCn1c(=O)c2nc([nH]c2n(c1=O)CC)c1cnn(c1)Cc1cccc(c1)C(F)(F)F None
5615 1226 UNDEFINED 35 Human Binding pKi = 7.7 7.7 67 4
NoneNone
PDSP KiDatabase 446 6 1 7 3.2 CCCn1c(=O)c2nc([nH]c2n(c1=O)CC)c1cnn(c1)Cc1cccc(c1)C(F)(F)F None
CHEMBL260933 1226 UNDEFINED 35 Human Binding pKi = 7.7 7.7 67 4
NoneNone
PDSP KiDatabase 446 6 1 7 3.2 CCCn1c(=O)c2nc([nH]c2n(c1=O)CC)c1cnn(c1)Cc1cccc(c1)C(F)(F)F None
DB05936 1226 UNDEFINED 35 Human Binding pKi = 7.7 7.7 67 4
NoneNone
PDSP KiDatabase 446 6 1 7 3.2 CCCn1c(=O)c2nc([nH]c2n(c1=O)CC)c1cnn(c1)Cc1cccc(c1)C(F)(F)F None
None 217135 UNDEFINED 0 Human Binding pKi = 6.6 6.6 89 3
NoneNone
PDSP KiDatabase 372 4 2 7 -2.6 CCCN1C(=O)C2=C(NC1=O)N=C(N2)C3=CC=C(C=C3)S(=O)(=O)[O-].[Na+] None
377 2758 UNDEFINED 53 Human Binding pKi = 6.6 6.6 -1479 15
NoneNone
PDSP KiDatabase 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N None
425 2758 UNDEFINED 53 Human Binding pKi = 6.6 6.6 -1479 15
NoneNone
PDSP KiDatabase 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N None
448222 2758 UNDEFINED 53 Human Binding pKi = 6.6 6.6 -1479 15
NoneNone
PDSP KiDatabase 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N None
CHEMBL464859 2758 UNDEFINED 53 Human Binding pKi = 6.6 6.6 -1479 15
NoneNone
PDSP KiDatabase 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N None
44185936 185534 UNDEFINED 0 Human Binding pKi = 8.5 8.5 12 6
NoneNone
PDSP KiDatabase 522 8 3 7 2.4 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)NC4CCN(Cc5ccccc5)CC4)cc3)[nH]c2c1=O None
CHEMBL486282 185534 UNDEFINED 0 Human Binding pKi = 8.5 8.5 12 6
NoneNone
PDSP KiDatabase 522 8 3 7 2.4 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)NC4CCN(Cc5ccccc5)CC4)cc3)[nH]c2c1=O None
11605883 79952 UNDEFINED 6 Human Binding pKi = 8.4 8.4 42 6
NoneNone
PDSP KiDatabase 508 7 2 7 2.0 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccccc5)CC4)cc3)[nH]c2c1=O None
CHEMBL212625 79952 UNDEFINED 6 Human Binding pKi = 8.4 8.4 42 6
NoneNone
PDSP KiDatabase 508 7 2 7 2.0 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(Cc5ccccc5)CC4)cc3)[nH]c2c1=O None
2690 903 UNDEFINED 66 Human Binding pKi = 7.5 7.5 -30 9
NoneNone
PDSP KiDatabase 285 1 1 6 2.8 Clc1ccc2c(c1)c1nc(nn1c(n2)N)c1ccco1 None
384 903 UNDEFINED 66 Human Binding pKi = 7.5 7.5 -30 9
NoneNone
PDSP KiDatabase 285 1 1 6 2.8 Clc1ccc2c(c1)c1nc(nn1c(n2)N)c1ccco1 None
CHEMBL16687 903 UNDEFINED 66 Human Binding pKi = 7.5 7.5 -30 9
NoneNone
PDSP KiDatabase 285 1 1 6 2.8 Clc1ccc2c(c1)c1nc(nn1c(n2)N)c1ccco1 None
163889 1964 125I-ABOPX 17 Human Binding pKi = 7.5 7.5 -6 8
NoneNone
PDSP KiDatabase 575 8 3 8 2.7 CCCn1c(=O)c2[nH]c(nc2n(c1=O)Cc1ccc(c(c1)I)N)c1ccc(cc1)OCC(=O)O None
446 1964 125I-ABOPX 17 Human Binding pKi = 7.5 7.5 -6 8
NoneNone
PDSP KiDatabase 575 8 3 8 2.7 CCCn1c(=O)c2[nH]c(nc2n(c1=O)Cc1ccc(c(c1)I)N)c1ccc(cc1)OCC(=O)O None
CHEMBL355370 1964 125I-ABOPX 17 Human Binding pKi = 7.5 7.5 -6 8
NoneNone
PDSP KiDatabase 575 8 3 8 2.7 CCCn1c(=O)c2[nH]c(nc2n(c1=O)Cc1ccc(c(c1)I)N)c1ccc(cc1)OCC(=O)O None
176407 4148 125I-ABOPX 84 Human Binding pKi = 7.5 7.5 -34 6
NoneNone
PDSP KiDatabase 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 None
176407 4148 3H-MRE 3008F20 84 Human Binding pKi = 7.5 7.5 -34 6
NoneNone
PDSP KiDatabase 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 None
405 4148 125I-ABOPX 84 Human Binding pKi = 7.5 7.5 -34 6
NoneNone
PDSP KiDatabase 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 None
405 4148 3H-MRE 3008F20 84 Human Binding pKi = 7.5 7.5 -34 6
NoneNone
PDSP KiDatabase 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 None
CHEMBL113142 4148 125I-ABOPX 84 Human Binding pKi = 7.5 7.5 -34 6
NoneNone
PDSP KiDatabase 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 None
CHEMBL113142 4148 3H-MRE 3008F20 84 Human Binding pKi = 7.5 7.5 -34 6
NoneNone
PDSP KiDatabase 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 None
DB08770 4148 125I-ABOPX 84 Human Binding pKi = 7.5 7.5 -34 6
NoneNone
PDSP KiDatabase 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 None
DB08770 4148 3H-MRE 3008F20 84 Human Binding pKi = 7.5 7.5 -34 6
NoneNone
PDSP KiDatabase 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 None
176407 4148 125I-ABOPX 84 Human Binding pKi = 7.5 7.5 -34 6
NoneNone
PDSP KiDatabase 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 None
405 4148 125I-ABOPX 84 Human Binding pKi = 7.5 7.5 -34 6
NoneNone
PDSP KiDatabase 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 None
CHEMBL113142 4148 125I-ABOPX 84 Human Binding pKi = 7.5 7.5 -34 6
NoneNone
PDSP KiDatabase 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 None
DB08770 4148 125I-ABOPX 84 Human Binding pKi = 7.5 7.5 -34 6
NoneNone
PDSP KiDatabase 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 None
377 2758 125I-ABOPX 53 Human Binding pKi = 6.5 6.5 -1479 15
NoneNone
PDSP KiDatabase 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N None
425 2758 125I-ABOPX 53 Human Binding pKi = 6.5 6.5 -1479 15
NoneNone
PDSP KiDatabase 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N None
448222 2758 125I-ABOPX 53 Human Binding pKi = 6.5 6.5 -1479 15
NoneNone
PDSP KiDatabase 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N None
CHEMBL464859 2758 125I-ABOPX 53 Human Binding pKi = 6.5 6.5 -1479 15
NoneNone
PDSP KiDatabase 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N None
1241166 199284 UNDEFINED 21 Human Binding pKi = 6.5 6.5 2 2
NoneNone
PDSP KiDatabase 356 5 1 4 5.8 O=C(c1ccccc1)c1sc(Nc2ccccc2)nc1-c1ccccc1 None
CHEMBL590302 199284 UNDEFINED 21 Human Binding pKi = 6.5 6.5 2 2
NoneNone
PDSP KiDatabase 356 5 1 4 5.8 O=C(c1ccccc1)c1sc(Nc2ccccc2)nc1-c1ccccc1 None
2519 779 [ 3 H]8-(4-(4-(4-chlorophenyl)piperazine-1-sulfonyl)phenyl)-1-propylxanthine ([3H]PSB-603) 86 Human Binding pKi = 4.5 4.5 -11 12
NoneNone
PDSP KiDatabase 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C None
2519.0 779 [ 3 H]8-(4-(4-(4-chlorophenyl)piperazine-1-sulfonyl)phenyl)-1-propylxanthine ([3H]PSB-603) 86 Human Binding pKi = 4.5 4.5 -11 12
NoneNone
PDSP KiDatabase 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C None
407 779 [ 3 H]8-(4-(4-(4-chlorophenyl)piperazine-1-sulfonyl)phenyl)-1-propylxanthine ([3H]PSB-603) 86 Human Binding pKi = 4.5 4.5 -11 12
NoneNone
PDSP KiDatabase 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C None
463 779 [ 3 H]8-(4-(4-(4-chlorophenyl)piperazine-1-sulfonyl)phenyl)-1-propylxanthine ([3H]PSB-603) 86 Human Binding pKi = 4.5 4.5 -11 12
NoneNone
PDSP KiDatabase 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C None
CHEMBL113 779 [ 3 H]8-(4-(4-(4-chlorophenyl)piperazine-1-sulfonyl)phenyl)-1-propylxanthine ([3H]PSB-603) 86 Human Binding pKi = 4.5 4.5 -11 12
NoneNone
PDSP KiDatabase 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C None
DB00201 779 [ 3 H]8-(4-(4-(4-chlorophenyl)piperazine-1-sulfonyl)phenyl)-1-propylxanthine ([3H]PSB-603) 86 Human Binding pKi = 4.5 4.5 -11 12
NoneNone
PDSP KiDatabase 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C None
2690 903 UNDEFINED 66 Human Binding pKi = 7.5 7.5 -30 9
NoneNone
PDSP KiDatabase 285 1 1 6 2.8 Clc1ccc2c(c1)c1nc(nn1c(n2)N)c1ccco1 None
384 903 UNDEFINED 66 Human Binding pKi = 7.5 7.5 -30 9
NoneNone
PDSP KiDatabase 285 1 1 6 2.8 Clc1ccc2c(c1)c1nc(nn1c(n2)N)c1ccco1 None
CHEMBL16687 903 UNDEFINED 66 Human Binding pKi = 7.5 7.5 -30 9
NoneNone
PDSP KiDatabase 285 1 1 6 2.8 Clc1ccc2c(c1)c1nc(nn1c(n2)N)c1ccco1 None
7315331 201129 UNDEFINED 1 Human Binding pKi = 6.4 6.4 -5 4
NoneNone
PDSP KiDatabase 352 5 1 5 4.6 CCOC(=O)Nc1nc(-c2ccccc2)c(C(=O)c2ccccc2)s1 None
CHEMBL603129 201129 UNDEFINED 1 Human Binding pKi = 6.4 6.4 -5 4
NoneNone
PDSP KiDatabase 352 5 1 5 4.6 CCOC(=O)Nc1nc(-c2ccccc2)c(C(=O)c2ccccc2)s1 None
None 217571 UNDEFINED 0 Human Binding pKi = 5.4 5.4 -3981 4
NoneNone
PDSP KiDatabase 308 3 3 4 3.3 C1CC(CCC1NC2=NC(=NC3=C2C=CN3)C4=CC=CC=C4)O None
69550 204102 None 86 Human Binding pKi = 8.3 8.3 - 1
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
Drug Central 238 2 1 7 -1.5 Cn1c(=O)c2c(ncn2CC(=O)O)n(C)c1=O None
CHEMBL70246 204102 None 86 Human Binding pKi = 8.3 8.3 - 1
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
Drug Central 238 2 1 7 -1.5 Cn1c(=O)c2c(ncn2CC(=O)O)n(C)c1=O None
1892 204045 None 78 Human Binding pKi = 8.3 8.3 34 3
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
Drug Central 224 2 1 7 -1.6 Cn1c(=O)c2c(ncn2CCO)n(C)c1=O None
CHEMBL699 204045 None 78 Human Binding pKi = 8.3 8.3 34 3
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
Drug Central 224 2 1 7 -1.6 Cn1c(=O)c2c(ncn2CCO)n(C)c1=O None
2519 779 None 86 Human Binding pKi = 8.3 8.3 -11 12
NoneNone
Drug Central 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C None
2519.0 779 None 86 Human Binding pKi = 8.3 8.3 -11 12
NoneNone
Drug Central 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C None
407 779 None 86 Human Binding pKi = 8.3 8.3 -11 12
NoneNone
Drug Central 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C None
463 779 None 86 Human Binding pKi = 8.3 8.3 -11 12
NoneNone
Drug Central 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C None
CHEMBL113 779 None 86 Human Binding pKi = 8.3 8.3 -11 12
NoneNone
Drug Central 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C None
DB00201 779 None 86 Human Binding pKi = 8.3 8.3 -11 12
NoneNone
Drug Central 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C None
2153 3800 None 115 Rat Binding pKi = 8.3 8.3 -1 14
Inhibition of [125I]-APOBX binding to rat Adenosine A2B receptor expressed in HEK cellsInhibition of [125I]-APOBX binding to rat Adenosine A2B receptor expressed in HEK cells
Drug Central 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 None
2153.0 3800 None 115 Rat Binding pKi = 8.3 8.3 -1 14
Inhibition of [125I]-APOBX binding to rat Adenosine A2B receptor expressed in HEK cellsInhibition of [125I]-APOBX binding to rat Adenosine A2B receptor expressed in HEK cells
Drug Central 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 None
2620 3800 None 115 Rat Binding pKi = 8.3 8.3 -1 14
Inhibition of [125I]-APOBX binding to rat Adenosine A2B receptor expressed in HEK cellsInhibition of [125I]-APOBX binding to rat Adenosine A2B receptor expressed in HEK cells
Drug Central 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 None
413 3800 None 115 Rat Binding pKi = 8.3 8.3 -1 14
Inhibition of [125I]-APOBX binding to rat Adenosine A2B receptor expressed in HEK cellsInhibition of [125I]-APOBX binding to rat Adenosine A2B receptor expressed in HEK cells
Drug Central 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 None
CHEMBL190 3800 None 115 Rat Binding pKi = 8.3 8.3 -1 14
Inhibition of [125I]-APOBX binding to rat Adenosine A2B receptor expressed in HEK cellsInhibition of [125I]-APOBX binding to rat Adenosine A2B receptor expressed in HEK cells
Drug Central 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 None
DB00277 3800 None 115 Rat Binding pKi = 8.3 8.3 -1 14
Inhibition of [125I]-APOBX binding to rat Adenosine A2B receptor expressed in HEK cellsInhibition of [125I]-APOBX binding to rat Adenosine A2B receptor expressed in HEK cells
Drug Central 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 None
2519 779 None 86 Mouse Binding pKi = 8.3 8.3 -1 12
NoneNone
Drug Central 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C None
2519.0 779 None 86 Mouse Binding pKi = 8.3 8.3 -1 12
NoneNone
Drug Central 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C None
407 779 None 86 Mouse Binding pKi = 8.3 8.3 -1 12
NoneNone
Drug Central 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C None
463 779 None 86 Mouse Binding pKi = 8.3 8.3 -1 12
NoneNone
Drug Central 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C None
CHEMBL113 779 None 86 Mouse Binding pKi = 8.3 8.3 -1 12
NoneNone
Drug Central 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C None
DB00201 779 None 86 Mouse Binding pKi = 8.3 8.3 -1 12
NoneNone
Drug Central 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C None
1329 1472 3H-MRE 3008F20 86 Human Binding pKi = 7.4 7.4 -1288 14
NoneNone
PDSP KiDatabase 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 None
386 1472 3H-MRE 3008F20 86 Human Binding pKi = 7.4 7.4 -1288 14
NoneNone
PDSP KiDatabase 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 None
CHEMBL183 1472 3H-MRE 3008F20 86 Human Binding pKi = 7.4 7.4 -1288 14
NoneNone
PDSP KiDatabase 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 None
DB12946 1472 3H-MRE 3008F20 86 Human Binding pKi = 7.4 7.4 -1288 14
NoneNone
PDSP KiDatabase 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 None
163889 1964 125I-ABOPX 17 Human Binding pKi = 7.4 7.4 -6 8
NoneNone
PDSP KiDatabase 575 8 3 8 2.7 CCCn1c(=O)c2[nH]c(nc2n(c1=O)Cc1ccc(c(c1)I)N)c1ccc(cc1)OCC(=O)O None
446 1964 125I-ABOPX 17 Human Binding pKi = 7.4 7.4 -6 8
NoneNone
PDSP KiDatabase 575 8 3 8 2.7 CCCn1c(=O)c2[nH]c(nc2n(c1=O)Cc1ccc(c(c1)I)N)c1ccc(cc1)OCC(=O)O None
CHEMBL355370 1964 125I-ABOPX 17 Human Binding pKi = 7.4 7.4 -6 8
NoneNone
PDSP KiDatabase 575 8 3 8 2.7 CCCn1c(=O)c2[nH]c(nc2n(c1=O)Cc1ccc(c(c1)I)N)c1ccc(cc1)OCC(=O)O None
2690 903 3H-cAMP 66 Human Binding pKi = 7.4 7.4 -30 9
NoneNone
PDSP KiDatabase 285 1 1 6 2.8 Clc1ccc2c(c1)c1nc(nn1c(n2)N)c1ccco1 None
384 903 3H-cAMP 66 Human Binding pKi = 7.4 7.4 -30 9
NoneNone
PDSP KiDatabase 285 1 1 6 2.8 Clc1ccc2c(c1)c1nc(nn1c(n2)N)c1ccco1 None
CHEMBL16687 903 3H-cAMP 66 Human Binding pKi = 7.4 7.4 -30 9
NoneNone
PDSP KiDatabase 285 1 1 6 2.8 Clc1ccc2c(c1)c1nc(nn1c(n2)N)c1ccco1 None
2153 3800 None 115 Mouse Binding pKi = 8.3 8.3 1 14
NoneNone
Drug Central 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 None
2153.0 3800 None 115 Mouse Binding pKi = 8.3 8.3 1 14
NoneNone
Drug Central 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 None
2620 3800 None 115 Mouse Binding pKi = 8.3 8.3 1 14
NoneNone
Drug Central 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 None
413 3800 None 115 Mouse Binding pKi = 8.3 8.3 1 14
NoneNone
Drug Central 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 None
CHEMBL190 3800 None 115 Mouse Binding pKi = 8.3 8.3 1 14
NoneNone
Drug Central 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 None
DB00277 3800 None 115 Mouse Binding pKi = 8.3 8.3 1 14
NoneNone
Drug Central 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 None
2099 3046 None 81 Human Binding pKi = 8.3 8.3 19 3
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
Drug Central 278 5 0 7 0.2 CC(=O)CCCCn1c(=O)c2n(C)cnc2n(c1=O)C None
4740 3046 None 81 Human Binding pKi = 8.3 8.3 19 3
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
Drug Central 278 5 0 7 0.2 CC(=O)CCCCn1c(=O)c2n(C)cnc2n(c1=O)C None
4740.0 3046 None 81 Human Binding pKi = 8.3 8.3 19 3
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
Drug Central 278 5 0 7 0.2 CC(=O)CCCCn1c(=O)c2n(C)cnc2n(c1=O)C None
7095 3046 None 81 Human Binding pKi = 8.3 8.3 19 3
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
Drug Central 278 5 0 7 0.2 CC(=O)CCCCn1c(=O)c2n(C)cnc2n(c1=O)C None
CHEMBL628 3046 None 81 Human Binding pKi = 8.3 8.3 19 3
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
Drug Central 278 5 0 7 0.2 CC(=O)CCCCn1c(=O)c2n(C)cnc2n(c1=O)C None
DB00806 3046 None 81 Human Binding pKi = 8.3 8.3 19 3
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
Drug Central 278 5 0 7 0.2 CC(=O)CCCCn1c(=O)c2n(C)cnc2n(c1=O)C None
1676 98984 None 61 Human Binding pKi = 8.3 8.3 -3 10
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
Drug Central 194 2 2 4 -0.2 CCCn1c(=O)[nH]c(=O)c2[nH]cnc21 None
CHEMBL279898 98984 None 61 Human Binding pKi = 8.3 8.3 -3 10
Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligandBinding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand
Drug Central 194 2 2 4 -0.2 CCCn1c(=O)[nH]c(=O)c2[nH]cnc21 None
44185934 186710 UNDEFINED 0 Human Binding pKi = 8.3 8.3 14 4
NoneNone
PDSP KiDatabase 403 4 2 6 1.3 CCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCCCC4)cc3)[nH]c2c1=O None
CHEMBL488542 186710 UNDEFINED 0 Human Binding pKi = 8.3 8.3 14 4
NoneNone
PDSP KiDatabase 403 4 2 6 1.3 CCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCCCC4)cc3)[nH]c2c1=O None
None 217133 UNDEFINED 0 Human Binding pKi = 8.3 8.3 -1 11
NoneNone
PDSP KiDatabase 116 4 0 2 1.4 CCCCN(C)N=O None
2153 3800 None 115 Human Binding pKi = 8.3 8.3 -21 14
Displacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cell membraneDisplacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cell membrane
Drug Central 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 None
2153.0 3800 None 115 Human Binding pKi = 8.3 8.3 -21 14
Displacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cell membraneDisplacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cell membrane
Drug Central 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 None
2620 3800 None 115 Human Binding pKi = 8.3 8.3 -21 14
Displacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cell membraneDisplacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cell membrane
Drug Central 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 None
413 3800 None 115 Human Binding pKi = 8.3 8.3 -21 14
Displacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cell membraneDisplacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cell membrane
Drug Central 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 None
CHEMBL190 3800 None 115 Human Binding pKi = 8.3 8.3 -21 14
Displacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cell membraneDisplacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cell membrane
Drug Central 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 None
DB00277 3800 None 115 Human Binding pKi = 8.3 8.3 -21 14
Displacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cell membraneDisplacement of [3H]DPCPX from human recombinant adenosine A2B receptor expressed in HEK293 cell membrane
Drug Central 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 None
4882 2099 None 82 Human Binding pKi = 8.2 8.2 -104 6
Inhibition of human recombinant adenosine receptor A2bInhibition of human recombinant adenosine receptor A2b
Drug Central 384 6 0 8 2.1 COc1cc(/C=C/c2nc3c(n2C)c(=O)n(c(=O)n3CC)CC)ccc1OC None
5311037 2099 None 82 Human Binding pKi = 8.2 8.2 -104 6
Inhibition of human recombinant adenosine receptor A2bInhibition of human recombinant adenosine receptor A2b
Drug Central 384 6 0 8 2.1 COc1cc(/C=C/c2nc3c(n2C)c(=O)n(c(=O)n3CC)CC)ccc1OC None
5311037.0 2099 None 82 Human Binding pKi = 8.2 8.2 -104 6
Inhibition of human recombinant adenosine receptor A2bInhibition of human recombinant adenosine receptor A2b
Drug Central 384 6 0 8 2.1 COc1cc(/C=C/c2nc3c(n2C)c(=O)n(c(=O)n3CC)CC)ccc1OC None
5608 2099 None 82 Human Binding pKi = 8.2 8.2 -104 6
Inhibition of human recombinant adenosine receptor A2bInhibition of human recombinant adenosine receptor A2b
Drug Central 384 6 0 8 2.1 COc1cc(/C=C/c2nc3c(n2C)c(=O)n(c(=O)n3CC)CC)ccc1OC None
CHEMBL431770 2099 None 82 Human Binding pKi = 8.2 8.2 -104 6
Inhibition of human recombinant adenosine receptor A2bInhibition of human recombinant adenosine receptor A2b
Drug Central 384 6 0 8 2.1 COc1cc(/C=C/c2nc3c(n2C)c(=O)n(c(=O)n3CC)CC)ccc1OC None
DB11757 2099 None 82 Human Binding pKi = 8.2 8.2 -104 6
Inhibition of human recombinant adenosine receptor A2bInhibition of human recombinant adenosine receptor A2b
Drug Central 384 6 0 8 2.1 COc1cc(/C=C/c2nc3c(n2C)c(=O)n(c(=O)n3CC)CC)ccc1OC None
169317 1201 125I-ABOPX 38 Human Binding pKi = 7.3 7.3 -44 9
NoneNone
PDSP KiDatabase 236 4 1 5 0.7 CCCn1c(=O)n(CCC)c2c(c1=O)[nH]cn2 None
427 1201 125I-ABOPX 38 Human Binding pKi = 7.3 7.3 -44 9
NoneNone
PDSP KiDatabase 236 4 1 5 0.7 CCCn1c(=O)n(CCC)c2c(c1=O)[nH]cn2 None
CHEMBL157655 1201 125I-ABOPX 38 Human Binding pKi = 7.3 7.3 -44 9
NoneNone
PDSP KiDatabase 236 4 1 5 0.7 CCCn1c(=O)n(CCC)c2c(c1=O)[nH]cn2 None
176407 4148 3H-cAMP 84 Human Binding pKi = 7.3 7.3 -34 6
NoneNone
PDSP KiDatabase 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 None
405 4148 3H-cAMP 84 Human Binding pKi = 7.3 7.3 -34 6
NoneNone
PDSP KiDatabase 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 None
CHEMBL113142 4148 3H-cAMP 84 Human Binding pKi = 7.3 7.3 -34 6
NoneNone
PDSP KiDatabase 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 None
DB08770 4148 3H-cAMP 84 Human Binding pKi = 7.3 7.3 -34 6
NoneNone
PDSP KiDatabase 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 None
176408 3557 3H-MRE 3008F20 84 Human Binding pKi = 5.3 5.3 -407 7
NoneNone
PDSP KiDatabase 345 4 1 8 2.6 Nc1nc2n(CCc3ccccc3)ncc2c2n1nc(n2)c1ccco1 None
176408 3557 3H-cAMP 84 Human Binding pKi = 5.3 5.3 -407 7
NoneNone
PDSP KiDatabase 345 4 1 8 2.6 Nc1nc2n(CCc3ccccc3)ncc2c2n1nc(n2)c1ccco1 None
403 3557 3H-MRE 3008F20 84 Human Binding pKi = 5.3 5.3 -407 7
NoneNone
PDSP KiDatabase 345 4 1 8 2.6 Nc1nc2n(CCc3ccccc3)ncc2c2n1nc(n2)c1ccco1 None
403 3557 3H-cAMP 84 Human Binding pKi = 5.3 5.3 -407 7
NoneNone
PDSP KiDatabase 345 4 1 8 2.6 Nc1nc2n(CCc3ccccc3)ncc2c2n1nc(n2)c1ccco1 None
431 3557 3H-MRE 3008F20 84 Human Binding pKi = 5.3 5.3 -407 7
NoneNone
PDSP KiDatabase 345 4 1 8 2.6 Nc1nc2n(CCc3ccccc3)ncc2c2n1nc(n2)c1ccco1 None
431 3557 3H-cAMP 84 Human Binding pKi = 5.3 5.3 -407 7
NoneNone
PDSP KiDatabase 345 4 1 8 2.6 Nc1nc2n(CCc3ccccc3)ncc2c2n1nc(n2)c1ccco1 None
CHEMBL17127 3557 3H-MRE 3008F20 84 Human Binding pKi = 5.3 5.3 -407 7
NoneNone
PDSP KiDatabase 345 4 1 8 2.6 Nc1nc2n(CCc3ccccc3)ncc2c2n1nc(n2)c1ccco1 None
CHEMBL17127 3557 3H-cAMP 84 Human Binding pKi = 5.3 5.3 -407 7
NoneNone
PDSP KiDatabase 345 4 1 8 2.6 Nc1nc2n(CCc3ccccc3)ncc2c2n1nc(n2)c1ccco1 None
1329 1472 3H-PSB-298 86 Human Binding pKi = 7.3 7.3 -1288 14
NoneNone
PDSP KiDatabase 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 None
1329 1472 3H-ZM241385 86 Human Binding pKi = 7.3 7.3 -1288 14
NoneNone
PDSP KiDatabase 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 None
386 1472 3H-PSB-298 86 Human Binding pKi = 7.3 7.3 -1288 14
NoneNone
PDSP KiDatabase 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 None
386 1472 3H-ZM241385 86 Human Binding pKi = 7.3 7.3 -1288 14
NoneNone
PDSP KiDatabase 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 None
CHEMBL183 1472 3H-PSB-298 86 Human Binding pKi = 7.3 7.3 -1288 14
NoneNone
PDSP KiDatabase 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 None
CHEMBL183 1472 3H-ZM241385 86 Human Binding pKi = 7.3 7.3 -1288 14
NoneNone
PDSP KiDatabase 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 None
DB12946 1472 3H-PSB-298 86 Human Binding pKi = 7.3 7.3 -1288 14
NoneNone
PDSP KiDatabase 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 None
DB12946 1472 3H-ZM241385 86 Human Binding pKi = 7.3 7.3 -1288 14
NoneNone
PDSP KiDatabase 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 None
None 216123 125I-ABOPX 0 Human Binding pKi = 7.3 7.3 -2 5
NoneNone
PDSP KiDatabase 382 7 2 6 2.5 CCCN1C2=C(C(=O)N(C1=O)CCC)NC(=N2)C3=CC=C(C=C3)C=CC(=O)O None
None 217135 UNDEFINED 0 Human Binding pKi = 7.3 7.3 89 3
NoneNone
PDSP KiDatabase 372 4 2 7 -2.6 CCCN1C(=O)C2=C(NC1=O)N=C(N2)C3=CC=C(C=C3)S(=O)(=O)[O-].[Na+] None
169317 1201 125I-ABOPX 38 Human Binding pKi = 7.3 7.3 -44 9
NoneNone
PDSP KiDatabase 236 4 1 5 0.7 CCCn1c(=O)n(CCC)c2c(c1=O)[nH]cn2 None
427 1201 125I-ABOPX 38 Human Binding pKi = 7.3 7.3 -44 9
NoneNone
PDSP KiDatabase 236 4 1 5 0.7 CCCn1c(=O)n(CCC)c2c(c1=O)[nH]cn2 None
CHEMBL157655 1201 125I-ABOPX 38 Human Binding pKi = 7.3 7.3 -44 9
NoneNone
PDSP KiDatabase 236 4 1 5 0.7 CCCn1c(=O)n(CCC)c2c(c1=O)[nH]cn2 None
377 2758 UNDEFINED 53 Human Binding pKi = 6.2 6.2 -1479 15
NoneNone
PDSP KiDatabase 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N None
425 2758 UNDEFINED 53 Human Binding pKi = 6.2 6.2 -1479 15
NoneNone
PDSP KiDatabase 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N None
448222 2758 UNDEFINED 53 Human Binding pKi = 6.2 6.2 -1479 15
NoneNone
PDSP KiDatabase 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N None
CHEMBL464859 2758 UNDEFINED 53 Human Binding pKi = 6.2 6.2 -1479 15
NoneNone
PDSP KiDatabase 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N None
10927361 90868 UNDEFINED 0 Human Binding pKi = 6.2 6.2 1 4
NoneNone
PDSP KiDatabase 395 7 0 7 2.6 CCCn1c(=O)c2c(nc3n2CCCN3CCc2ccccc2)n(CCC)c1=O None
CHEMBL239233 90868 UNDEFINED 0 Human Binding pKi = 6.2 6.2 1 4
NoneNone
PDSP KiDatabase 395 7 0 7 2.6 CCCn1c(=O)c2c(nc3n2CCCN3CCc2ccccc2)n(CCC)c1=O None
681 1465 None 72 Rat Binding pKi = 8.2 8.2 -15 39
NoneNone
Drug Central 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
681.0 1465 None 72 Rat Binding pKi = 8.2 8.2 -15 39
NoneNone
Drug Central 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
940 1465 None 72 Rat Binding pKi = 8.2 8.2 -15 39
NoneNone
Drug Central 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
947 1465 None 72 Rat Binding pKi = 8.2 8.2 -15 39
NoneNone
Drug Central 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
CHEMBL59 1465 None 72 Rat Binding pKi = 8.2 8.2 -15 39
NoneNone
Drug Central 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
DB00988 1465 None 72 Rat Binding pKi = 8.2 8.2 -15 39
NoneNone
Drug Central 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
1676 98984 125I-ABOPX 61 Human Binding pKi = 5.2 5.2 -3 10
NoneNone
PDSP KiDatabase 194 2 2 4 -0.2 CCCn1c(=O)[nH]c(=O)c2[nH]cnc21 None
CHEMBL279898 98984 125I-ABOPX 61 Human Binding pKi = 5.2 5.2 -3 10
NoneNone
PDSP KiDatabase 194 2 2 4 -0.2 CCCn1c(=O)[nH]c(=O)c2[nH]cnc21 None
1676 98984 125I-ABOPX 61 Human Binding pKi = 5.2 5.2 -3 10
NoneNone
PDSP KiDatabase 194 2 2 4 -0.2 CCCn1c(=O)[nH]c(=O)c2[nH]cnc21 None
1676 98984 UNDEFINED 61 Human Binding pKi = 5.2 5.2 -3 10
NoneNone
PDSP KiDatabase 194 2 2 4 -0.2 CCCn1c(=O)[nH]c(=O)c2[nH]cnc21 None
CHEMBL279898 98984 125I-ABOPX 61 Human Binding pKi = 5.2 5.2 -3 10
NoneNone
PDSP KiDatabase 194 2 2 4 -0.2 CCCn1c(=O)[nH]c(=O)c2[nH]cnc21 None
CHEMBL279898 98984 UNDEFINED 61 Human Binding pKi = 5.2 5.2 -3 10
NoneNone
PDSP KiDatabase 194 2 2 4 -0.2 CCCn1c(=O)[nH]c(=O)c2[nH]cnc21 None
404 4098 125I-ABOPX 33 Human Binding pKi = 8.1 8.1 -154 11
NoneNone
PDSP KiDatabase 428 10 3 8 0.8 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)NCCN None
432 4098 125I-ABOPX 33 Human Binding pKi = 8.1 8.1 -154 11
NoneNone
PDSP KiDatabase 428 10 3 8 0.8 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)NCCN None
5697 4098 125I-ABOPX 33 Human Binding pKi = 8.1 8.1 -154 11
NoneNone
PDSP KiDatabase 428 10 3 8 0.8 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)NCCN None
CHEMBL273094 4098 125I-ABOPX 33 Human Binding pKi = 8.1 8.1 -154 11
NoneNone
PDSP KiDatabase 428 10 3 8 0.8 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)NCCN None
1153 1628 None 58 Rat Binding pKi = 8.1 8.1 -5 10
NoneNone
Drug Central 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
12668023 1628 None 58 Rat Binding pKi = 8.1 8.1 -5 10
NoneNone
Drug Central 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
30026874 1628 None 58 Rat Binding pKi = 8.1 8.1 -5 10
NoneNone
Drug Central 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
30026875 1628 None 58 Rat Binding pKi = 8.1 8.1 -5 10
NoneNone
Drug Central 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
3341 1628 None 58 Rat Binding pKi = 8.1 8.1 -5 10
NoneNone
Drug Central 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
3341.0 1628 None 58 Rat Binding pKi = 8.1 8.1 -5 10
NoneNone
Drug Central 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
6603851 1628 None 58 Rat Binding pKi = 8.1 8.1 -5 10
NoneNone
Drug Central 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
933 1628 None 58 Rat Binding pKi = 8.1 8.1 -5 10
NoneNone
Drug Central 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
939 1628 None 58 Rat Binding pKi = 8.1 8.1 -5 10
NoneNone
Drug Central 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
985 1628 None 58 Rat Binding pKi = 8.1 8.1 -5 10
NoneNone
Drug Central 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
CHEMBL1160786 1628 None 58 Rat Binding pKi = 8.1 8.1 -5 10
NoneNone
Drug Central 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
CHEMBL1161520 1628 None 58 Rat Binding pKi = 8.1 8.1 -5 10
NoneNone
Drug Central 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
CHEMBL588 1628 None 58 Rat Binding pKi = 8.1 8.1 -5 10
NoneNone
Drug Central 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
DB00800 1628 None 58 Rat Binding pKi = 8.1 8.1 -5 10
NoneNone
Drug Central 305 1 4 4 2.7 Oc1ccc(cc1)C1CNCCc2c1cc(O)c(c2Cl)O None
44185932 191619 UNDEFINED 0 Human Binding pKi = 8.1 8.1 11 4
NoneNone
PDSP KiDatabase 508 7 2 7 1.6 CCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(CCc5ccccc5)CC4)cc3)[nH]c2c1=O None
CHEMBL519556 191619 UNDEFINED 0 Human Binding pKi = 8.1 8.1 11 4
NoneNone
PDSP KiDatabase 508 7 2 7 1.6 CCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(CCc5ccccc5)CC4)cc3)[nH]c2c1=O None
44185933 186709 UNDEFINED 0 Human Binding pKi = 8.1 8.1 35 5
NoneNone
PDSP KiDatabase 522 8 2 7 2.0 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(CCc5ccccc5)CC4)cc3)[nH]c2c1=O None
CHEMBL488541 186709 UNDEFINED 0 Human Binding pKi = 8.1 8.1 35 5
NoneNone
PDSP KiDatabase 522 8 2 7 2.0 CCCn1c(=O)[nH]c2nc(-c3ccc(S(=O)(=O)N4CCN(CCc5ccccc5)CC4)cc3)[nH]c2c1=O None
44437214 169254 UNDEFINED 0 Human Binding pKi = 5.1 5.1 -31 6
NoneNone
PDSP KiDatabase 355 3 1 8 0.6 Cn1c(=O)c2c(nc3n2CCCN3CCc2ccc(O)cc2)n(C)c1=O None
CHEMBL441145 169254 UNDEFINED 0 Human Binding pKi = 5.1 5.1 -31 6
NoneNone
PDSP KiDatabase 355 3 1 8 0.6 Cn1c(=O)c2c(nc3n2CCCN3CCc2ccc(O)cc2)n(C)c1=O None
1329 1472 [3H]DPCPX 86 Human Binding pKi = 7.1 7.1 -1288 14
NoneNone
PDSP KiDatabase 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 None
386 1472 [3H]DPCPX 86 Human Binding pKi = 7.1 7.1 -1288 14
NoneNone
PDSP KiDatabase 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 None
CHEMBL183 1472 [3H]DPCPX 86 Human Binding pKi = 7.1 7.1 -1288 14
NoneNone
PDSP KiDatabase 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 None
DB12946 1472 [3H]DPCPX 86 Human Binding pKi = 7.1 7.1 -1288 14
NoneNone
PDSP KiDatabase 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 None
2153 3800 125I-ABOPX 115 Human Binding pKi = 5.1 5.1 -21 14
NoneNone
PDSP KiDatabase 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 None
2153 3800 UNDEFINED 115 Human Binding pKi = 5.1 5.1 -21 14
NoneNone
PDSP KiDatabase 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 None
2153.0 3800 125I-ABOPX 115 Human Binding pKi = 5.1 5.1 -21 14
NoneNone
PDSP KiDatabase 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 None
2153.0 3800 UNDEFINED 115 Human Binding pKi = 5.1 5.1 -21 14
NoneNone
PDSP KiDatabase 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 None
2620 3800 125I-ABOPX 115 Human Binding pKi = 5.1 5.1 -21 14
NoneNone
PDSP KiDatabase 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 None
2620 3800 UNDEFINED 115 Human Binding pKi = 5.1 5.1 -21 14
NoneNone
PDSP KiDatabase 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 None
413 3800 125I-ABOPX 115 Human Binding pKi = 5.1 5.1 -21 14
NoneNone
PDSP KiDatabase 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 None
413 3800 UNDEFINED 115 Human Binding pKi = 5.1 5.1 -21 14
NoneNone
PDSP KiDatabase 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 None
CHEMBL190 3800 125I-ABOPX 115 Human Binding pKi = 5.1 5.1 -21 14
NoneNone
PDSP KiDatabase 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 None
CHEMBL190 3800 UNDEFINED 115 Human Binding pKi = 5.1 5.1 -21 14
NoneNone
PDSP KiDatabase 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 None
DB00277 3800 125I-ABOPX 115 Human Binding pKi = 5.1 5.1 -21 14
NoneNone
PDSP KiDatabase 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 None
DB00277 3800 UNDEFINED 115 Human Binding pKi = 5.1 5.1 -21 14
NoneNone
PDSP KiDatabase 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 None
2690 903 UNDEFINED 66 Human Binding pKi = 8.0 8.0 -30 9
NoneNone
PDSP KiDatabase 285 1 1 6 2.8 Clc1ccc2c(c1)c1nc(nn1c(n2)N)c1ccco1 None
384 903 UNDEFINED 66 Human Binding pKi = 8.0 8.0 -30 9
NoneNone
PDSP KiDatabase 285 1 1 6 2.8 Clc1ccc2c(c1)c1nc(nn1c(n2)N)c1ccco1 None
CHEMBL16687 903 UNDEFINED 66 Human Binding pKi = 8.0 8.0 -30 9
NoneNone
PDSP KiDatabase 285 1 1 6 2.8 Clc1ccc2c(c1)c1nc(nn1c(n2)N)c1ccco1 None
216466 3845 UNDEFINED 32 Human Binding pKi = 7.1 7.1 -123 6
NoneNone
PDSP KiDatabase 416 8 2 6 3.2 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C12CCC(CC1)(CC2)CCC(=O)O None
5605 3845 UNDEFINED 32 Human Binding pKi = 7.1 7.1 -123 6
NoneNone
PDSP KiDatabase 416 8 2 6 3.2 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C12CCC(CC1)(CC2)CCC(=O)O None
CHEMBL386974 3845 UNDEFINED 32 Human Binding pKi = 7.1 7.1 -123 6
NoneNone
PDSP KiDatabase 416 8 2 6 3.2 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C12CCC(CC1)(CC2)CCC(=O)O None
CHEMBL414157 3845 UNDEFINED 32 Human Binding pKi = 7.1 7.1 -123 6
NoneNone
PDSP KiDatabase 416 8 2 6 3.2 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C12CCC(CC1)(CC2)CCC(=O)O None
DB12569 3845 UNDEFINED 32 Human Binding pKi = 7.1 7.1 -123 6
NoneNone
PDSP KiDatabase 416 8 2 6 3.2 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C12CCC(CC1)(CC2)CCC(=O)O None
2153 3800 UNDEFINED 115 Human Binding pKi = 5.0 5.0 -21 14
NoneNone
PDSP KiDatabase 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 None
2153.0 3800 UNDEFINED 115 Human Binding pKi = 5.0 5.0 -21 14
NoneNone
PDSP KiDatabase 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 None
2620 3800 UNDEFINED 115 Human Binding pKi = 5.0 5.0 -21 14
NoneNone
PDSP KiDatabase 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 None
413 3800 UNDEFINED 115 Human Binding pKi = 5.0 5.0 -21 14
NoneNone
PDSP KiDatabase 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 None
CHEMBL190 3800 UNDEFINED 115 Human Binding pKi = 5.0 5.0 -21 14
NoneNone
PDSP KiDatabase 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 None
DB00277 3800 UNDEFINED 115 Human Binding pKi = 5.0 5.0 -21 14
NoneNone
PDSP KiDatabase 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 None
2153 3800 125I-ABOPX 115 Human Binding pKi = 5.0 5.0 -21 14
NoneNone
PDSP KiDatabase 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 None
2153.0 3800 125I-ABOPX 115 Human Binding pKi = 5.0 5.0 -21 14
NoneNone
PDSP KiDatabase 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 None
2620 3800 125I-ABOPX 115 Human Binding pKi = 5.0 5.0 -21 14
NoneNone
PDSP KiDatabase 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 None
413 3800 125I-ABOPX 115 Human Binding pKi = 5.0 5.0 -21 14
NoneNone
PDSP KiDatabase 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 None
CHEMBL190 3800 125I-ABOPX 115 Human Binding pKi = 5.0 5.0 -21 14
NoneNone
PDSP KiDatabase 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 None
DB00277 3800 125I-ABOPX 115 Human Binding pKi = 5.0 5.0 -21 14
NoneNone
PDSP KiDatabase 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 None
11153 2008 None 46 Human Binding pKi = 7.2 7.2 -35 4
Binding affinity of AZD4635 determined in a radioligand binding competition assays with membranes prepared from HEK-293-T cells stably expressing human A2BR.Binding affinity of AZD4635 determined in a radioligand binding competition assays with membranes prepared from HEK-293-T cells stably expressing human A2BR.
Guide to Pharmacology 315 2 1 5 3.3 Nc1nnc(c(n1)c1ccc(cc1)F)c1cc(C)nc(c1)Cl 32727810
86676119 2008 None 46 Human Binding pKi = 7.2 7.2 -35 4
Binding affinity of AZD4635 determined in a radioligand binding competition assays with membranes prepared from HEK-293-T cells stably expressing human A2BR.Binding affinity of AZD4635 determined in a radioligand binding competition assays with membranes prepared from HEK-293-T cells stably expressing human A2BR.
Guide to Pharmacology 315 2 1 5 3.3 Nc1nnc(c(n1)c1ccc(cc1)F)c1cc(C)nc(c1)Cl 32727810
CHEMBL4594442 2008 None 46 Human Binding pKi = 7.2 7.2 -35 4
Binding affinity of AZD4635 determined in a radioligand binding competition assays with membranes prepared from HEK-293-T cells stably expressing human A2BR.Binding affinity of AZD4635 determined in a radioligand binding competition assays with membranes prepared from HEK-293-T cells stably expressing human A2BR.
Guide to Pharmacology 315 2 1 5 3.3 Nc1nnc(c(n1)c1ccc(cc1)F)c1cc(C)nc(c1)Cl 32727810
DB16192 2008 None 46 Human Binding pKi = 7.2 7.2 -35 4
Binding affinity of AZD4635 determined in a radioligand binding competition assays with membranes prepared from HEK-293-T cells stably expressing human A2BR.Binding affinity of AZD4635 determined in a radioligand binding competition assays with membranes prepared from HEK-293-T cells stably expressing human A2BR.
Guide to Pharmacology 315 2 1 5 3.3 Nc1nnc(c(n1)c1ccc(cc1)F)c1cc(C)nc(c1)Cl 32727810
5595 662 None 24 Human Binding pKi = 3.4 3.4 -16595 6
UnclassifiedUnclassified
Guide to Pharmacology 391 5 5 11 -0.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(N/N=C/C1CCCCC1)nc2N 16518376
9576912 662 None 24 Human Binding pKi = 3.4 3.4 -16595 6
UnclassifiedUnclassified
Guide to Pharmacology 391 5 5 11 -0.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(N/N=C/C1CCCCC1)nc2N 16518376
CHEMBL1950554 662 None 24 Human Binding pKi = 3.4 3.4 -16595 6
UnclassifiedUnclassified
Guide to Pharmacology 391 5 5 11 -0.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(N/N=C/C1CCCCC1)nc2N 16518376
DB04853 662 None 24 Human Binding pKi = 3.4 3.4 -16595 6
UnclassifiedUnclassified
Guide to Pharmacology 391 5 5 11 -0.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(N/N=C/C1CCCCC1)nc2N 16518376
423 2706 None 54 Human Binding pKi = 3.8 3.8 -89125 8
UnclassifiedUnclassified
Guide to Pharmacology 349 4 4 9 0.2 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NC1CCCCC1 6253037
9841284 2706 None 54 Human Binding pKi = 3.8 3.8 -89125 8
UnclassifiedUnclassified
Guide to Pharmacology 349 4 4 9 0.2 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NC1CCCCC1 6253037
CHEMBL45891 2706 None 54 Human Binding pKi = 3.8 3.8 -89125 8
UnclassifiedUnclassified
Guide to Pharmacology 349 4 4 9 0.2 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NC1CCCCC1 6253037
3086599 904 None 45 Human Binding pKi = 4.2 4.2 -3630 8
UnclassifiedUnclassified
Guide to Pharmacology 499 10 6 11 -0.2 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(NCCc1ccc(cc1)CCC(=O)O)nc2N 10496952
3086599 904 None 45 Human Binding pKi = 4.2 4.2 -3630 8
UnclassifiedUnclassified
Guide to Pharmacology 499 10 6 11 -0.2 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(NCCc1ccc(cc1)CCC(=O)O)nc2N 11093773
3086599 904 None 45 Human Binding pKi = 4.2 4.2 -3630 8
UnclassifiedUnclassified
Guide to Pharmacology 499 10 6 11 -0.2 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(NCCc1ccc(cc1)CCC(=O)O)nc2N 16518376
375 904 None 45 Human Binding pKi = 4.2 4.2 -3630 8
UnclassifiedUnclassified
Guide to Pharmacology 499 10 6 11 -0.2 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(NCCc1ccc(cc1)CCC(=O)O)nc2N 10496952
375 904 None 45 Human Binding pKi = 4.2 4.2 -3630 8
UnclassifiedUnclassified
Guide to Pharmacology 499 10 6 11 -0.2 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(NCCc1ccc(cc1)CCC(=O)O)nc2N 11093773
375 904 None 45 Human Binding pKi = 4.2 4.2 -3630 8
UnclassifiedUnclassified
Guide to Pharmacology 499 10 6 11 -0.2 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(NCCc1ccc(cc1)CCC(=O)O)nc2N 16518376
424 904 None 45 Human Binding pKi = 4.2 4.2 -3630 8
UnclassifiedUnclassified
Guide to Pharmacology 499 10 6 11 -0.2 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(NCCc1ccc(cc1)CCC(=O)O)nc2N 10496952
424 904 None 45 Human Binding pKi = 4.2 4.2 -3630 8
UnclassifiedUnclassified
Guide to Pharmacology 499 10 6 11 -0.2 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(NCCc1ccc(cc1)CCC(=O)O)nc2N 11093773
424 904 None 45 Human Binding pKi = 4.2 4.2 -3630 8
UnclassifiedUnclassified
Guide to Pharmacology 499 10 6 11 -0.2 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(NCCc1ccc(cc1)CCC(=O)O)nc2N 16518376
CHEMBL331372 904 None 45 Human Binding pKi = 4.2 4.2 -3630 8
UnclassifiedUnclassified
Guide to Pharmacology 499 10 6 11 -0.2 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(NCCc1ccc(cc1)CCC(=O)O)nc2N 10496952
CHEMBL331372 904 None 45 Human Binding pKi = 4.2 4.2 -3630 8
UnclassifiedUnclassified
Guide to Pharmacology 499 10 6 11 -0.2 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(NCCc1ccc(cc1)CCC(=O)O)nc2N 11093773
CHEMBL331372 904 None 45 Human Binding pKi = 4.2 4.2 -3630 8
UnclassifiedUnclassified
Guide to Pharmacology 499 10 6 11 -0.2 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(NCCc1ccc(cc1)CCC(=O)O)nc2N 16518376
2519 779 None 86 Rat Binding pKi = 4.5 4.5 -47 12
UnclassifiedUnclassified
Guide to Pharmacology 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 8135856
2519.0 779 None 86 Rat Binding pKi = 4.5 4.5 -47 12
UnclassifiedUnclassified
Guide to Pharmacology 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 8135856
407 779 None 86 Rat Binding pKi = 4.5 4.5 -47 12
UnclassifiedUnclassified
Guide to Pharmacology 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 8135856
463 779 None 86 Rat Binding pKi = 4.5 4.5 -47 12
UnclassifiedUnclassified
Guide to Pharmacology 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 8135856
CHEMBL113 779 None 86 Rat Binding pKi = 4.5 4.5 -47 12
UnclassifiedUnclassified
Guide to Pharmacology 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 8135856
DB00201 779 None 86 Rat Binding pKi = 4.5 4.5 -47 12
UnclassifiedUnclassified
Guide to Pharmacology 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 8135856
123807 871 None 54 Human Binding pKi = 4.6 4.6 -13803 13
UnclassifiedUnclassified
Guide to Pharmacology 369 4 4 9 0.4 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NC1CCCC1 10496952
123807 871 None 54 Human Binding pKi = 4.6 4.6 -13803 13
UnclassifiedUnclassified
Guide to Pharmacology 369 4 4 9 0.4 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NC1CCCC1 16518376
374 871 None 54 Human Binding pKi = 4.6 4.6 -13803 13
UnclassifiedUnclassified
Guide to Pharmacology 369 4 4 9 0.4 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NC1CCCC1 10496952
374 871 None 54 Human Binding pKi = 4.6 4.6 -13803 13
UnclassifiedUnclassified
Guide to Pharmacology 369 4 4 9 0.4 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NC1CCCC1 16518376
379 871 None 54 Human Binding pKi = 4.6 4.6 -13803 13
UnclassifiedUnclassified
Guide to Pharmacology 369 4 4 9 0.4 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NC1CCCC1 10496952
379 871 None 54 Human Binding pKi = 4.6 4.6 -13803 13
UnclassifiedUnclassified
Guide to Pharmacology 369 4 4 9 0.4 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NC1CCCC1 16518376
CHEMBL284969 871 None 54 Human Binding pKi = 4.6 4.6 -13803 13
UnclassifiedUnclassified
Guide to Pharmacology 369 4 4 9 0.4 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NC1CCCC1 10496952
CHEMBL284969 871 None 54 Human Binding pKi = 4.6 4.6 -13803 13
UnclassifiedUnclassified
Guide to Pharmacology 369 4 4 9 0.4 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NC1CCCC1 16518376
2153 3800 None 115 Human Binding pKi = 4.6 4.6 -21 14
UnclassifiedUnclassified
Guide to Pharmacology 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 11705449
2153 3800 None 115 Human Binding pKi = 4.6 4.6 -21 14
UnclassifiedUnclassified
Guide to Pharmacology 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 12014951
2153 3800 None 115 Human Binding pKi = 4.6 4.6 -21 14
UnclassifiedUnclassified
Guide to Pharmacology 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 16219300
2153 3800 None 115 Human Binding pKi = 4.6 4.6 -21 14
UnclassifiedUnclassified
Guide to Pharmacology 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 18404493
2153.0 3800 None 115 Human Binding pKi = 4.6 4.6 -21 14
UnclassifiedUnclassified
Guide to Pharmacology 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 11705449
2153.0 3800 None 115 Human Binding pKi = 4.6 4.6 -21 14
UnclassifiedUnclassified
Guide to Pharmacology 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 12014951
2153.0 3800 None 115 Human Binding pKi = 4.6 4.6 -21 14
UnclassifiedUnclassified
Guide to Pharmacology 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 16219300
2153.0 3800 None 115 Human Binding pKi = 4.6 4.6 -21 14
UnclassifiedUnclassified
Guide to Pharmacology 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 18404493
2620 3800 None 115 Human Binding pKi = 4.6 4.6 -21 14
UnclassifiedUnclassified
Guide to Pharmacology 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 11705449
2620 3800 None 115 Human Binding pKi = 4.6 4.6 -21 14
UnclassifiedUnclassified
Guide to Pharmacology 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 12014951
2620 3800 None 115 Human Binding pKi = 4.6 4.6 -21 14
UnclassifiedUnclassified
Guide to Pharmacology 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 16219300
2620 3800 None 115 Human Binding pKi = 4.6 4.6 -21 14
UnclassifiedUnclassified
Guide to Pharmacology 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 18404493
413 3800 None 115 Human Binding pKi = 4.6 4.6 -21 14
UnclassifiedUnclassified
Guide to Pharmacology 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 11705449
413 3800 None 115 Human Binding pKi = 4.6 4.6 -21 14
UnclassifiedUnclassified
Guide to Pharmacology 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 12014951
413 3800 None 115 Human Binding pKi = 4.6 4.6 -21 14
UnclassifiedUnclassified
Guide to Pharmacology 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 16219300
413 3800 None 115 Human Binding pKi = 4.6 4.6 -21 14
UnclassifiedUnclassified
Guide to Pharmacology 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 18404493
CHEMBL190 3800 None 115 Human Binding pKi = 4.6 4.6 -21 14
UnclassifiedUnclassified
Guide to Pharmacology 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 11705449
CHEMBL190 3800 None 115 Human Binding pKi = 4.6 4.6 -21 14
UnclassifiedUnclassified
Guide to Pharmacology 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 12014951
CHEMBL190 3800 None 115 Human Binding pKi = 4.6 4.6 -21 14
UnclassifiedUnclassified
Guide to Pharmacology 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 16219300
CHEMBL190 3800 None 115 Human Binding pKi = 4.6 4.6 -21 14
UnclassifiedUnclassified
Guide to Pharmacology 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 18404493
DB00277 3800 None 115 Human Binding pKi = 4.6 4.6 -21 14
UnclassifiedUnclassified
Guide to Pharmacology 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 11705449
DB00277 3800 None 115 Human Binding pKi = 4.6 4.6 -21 14
UnclassifiedUnclassified
Guide to Pharmacology 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 12014951
DB00277 3800 None 115 Human Binding pKi = 4.6 4.6 -21 14
UnclassifiedUnclassified
Guide to Pharmacology 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 16219300
DB00277 3800 None 115 Human Binding pKi = 4.6 4.6 -21 14
UnclassifiedUnclassified
Guide to Pharmacology 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 18404493
123683 3121 None 63 Human Binding pKi = 4.6 4.6 -95499 13
UnclassifiedUnclassified
Guide to Pharmacology 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10496952
123683 3121 None 63 Human Binding pKi = 4.6 4.6 -95499 13
UnclassifiedUnclassified
Guide to Pharmacology 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 16518376
422 3121 None 63 Human Binding pKi = 4.6 4.6 -95499 13
UnclassifiedUnclassified
Guide to Pharmacology 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10496952
422 3121 None 63 Human Binding pKi = 4.6 4.6 -95499 13
UnclassifiedUnclassified
Guide to Pharmacology 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 16518376
CHEMBL119709 3121 None 63 Human Binding pKi = 4.6 4.6 -95499 13
UnclassifiedUnclassified
Guide to Pharmacology 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10496952
CHEMBL119709 3121 None 63 Human Binding pKi = 4.6 4.6 -95499 13
UnclassifiedUnclassified
Guide to Pharmacology 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 16518376
DB05511 3121 None 63 Human Binding pKi = 4.6 4.6 -95499 13
UnclassifiedUnclassified
Guide to Pharmacology 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 10496952
DB05511 3121 None 63 Human Binding pKi = 4.6 4.6 -95499 13
UnclassifiedUnclassified
Guide to Pharmacology 510 5 4 9 0.4 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NCc1cccc(c1)I 16518376
380 1287 None 54 Human Binding pKi = 4.6 4.6 -17782 13
UnclassifiedUnclassified
Guide to Pharmacology 335 4 4 9 -0.2 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NC1CCCC1 10496952
380 1287 None 54 Human Binding pKi = 4.6 4.6 -17782 13
UnclassifiedUnclassified
Guide to Pharmacology 335 4 4 9 -0.2 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NC1CCCC1 16518376
657378 1287 None 54 Human Binding pKi = 4.6 4.6 -17782 13
UnclassifiedUnclassified
Guide to Pharmacology 335 4 4 9 -0.2 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NC1CCCC1 10496952
657378 1287 None 54 Human Binding pKi = 4.6 4.6 -17782 13
UnclassifiedUnclassified
Guide to Pharmacology 335 4 4 9 -0.2 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NC1CCCC1 16518376
CHEMBL68738 1287 None 54 Human Binding pKi = 4.6 4.6 -17782 13
UnclassifiedUnclassified
Guide to Pharmacology 335 4 4 9 -0.2 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NC1CCCC1 10496952
CHEMBL68738 1287 None 54 Human Binding pKi = 4.6 4.6 -17782 13
UnclassifiedUnclassified
Guide to Pharmacology 335 4 4 9 -0.2 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2NC1CCCC1 16518376
414 3382 None 33 Human Binding pKi = 4.7 4.7 -19054 12
UnclassifiedUnclassified
Guide to Pharmacology 385 6 4 9 0.5 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N[C@@H](Cc1ccccc1)C 10496952
414 3382 None 33 Human Binding pKi = 4.7 4.7 -19054 12
UnclassifiedUnclassified
Guide to Pharmacology 385 6 4 9 0.5 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N[C@@H](Cc1ccccc1)C 11093773
414 3382 None 33 Human Binding pKi = 4.7 4.7 -19054 12
UnclassifiedUnclassified
Guide to Pharmacology 385 6 4 9 0.5 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N[C@@H](Cc1ccccc1)C 11266650
414 3382 None 33 Human Binding pKi = 4.7 4.7 -19054 12
UnclassifiedUnclassified
Guide to Pharmacology 385 6 4 9 0.5 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N[C@@H](Cc1ccccc1)C 16219300
414 3382 None 33 Human Binding pKi = 4.7 4.7 -19054 12
UnclassifiedUnclassified
Guide to Pharmacology 385 6 4 9 0.5 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N[C@@H](Cc1ccccc1)C 6253037
93205 3382 None 33 Human Binding pKi = 4.7 4.7 -19054 12
UnclassifiedUnclassified
Guide to Pharmacology 385 6 4 9 0.5 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N[C@@H](Cc1ccccc1)C 10496952
93205 3382 None 33 Human Binding pKi = 4.7 4.7 -19054 12
UnclassifiedUnclassified
Guide to Pharmacology 385 6 4 9 0.5 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N[C@@H](Cc1ccccc1)C 11093773
93205 3382 None 33 Human Binding pKi = 4.7 4.7 -19054 12
UnclassifiedUnclassified
Guide to Pharmacology 385 6 4 9 0.5 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N[C@@H](Cc1ccccc1)C 11266650
93205 3382 None 33 Human Binding pKi = 4.7 4.7 -19054 12
UnclassifiedUnclassified
Guide to Pharmacology 385 6 4 9 0.5 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N[C@@H](Cc1ccccc1)C 16219300
93205 3382 None 33 Human Binding pKi = 4.7 4.7 -19054 12
UnclassifiedUnclassified
Guide to Pharmacology 385 6 4 9 0.5 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N[C@@H](Cc1ccccc1)C 6253037
CHEMBL139000 3382 None 33 Human Binding pKi = 4.7 4.7 -19054 12
UnclassifiedUnclassified
Guide to Pharmacology 385 6 4 9 0.5 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N[C@@H](Cc1ccccc1)C 10496952
CHEMBL139000 3382 None 33 Human Binding pKi = 4.7 4.7 -19054 12
UnclassifiedUnclassified
Guide to Pharmacology 385 6 4 9 0.5 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N[C@@H](Cc1ccccc1)C 11093773
CHEMBL139000 3382 None 33 Human Binding pKi = 4.7 4.7 -19054 12
UnclassifiedUnclassified
Guide to Pharmacology 385 6 4 9 0.5 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N[C@@H](Cc1ccccc1)C 11266650
CHEMBL139000 3382 None 33 Human Binding pKi = 4.7 4.7 -19054 12
UnclassifiedUnclassified
Guide to Pharmacology 385 6 4 9 0.5 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N[C@@H](Cc1ccccc1)C 16219300
CHEMBL139000 3382 None 33 Human Binding pKi = 4.7 4.7 -19054 12
UnclassifiedUnclassified
Guide to Pharmacology 385 6 4 9 0.5 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N[C@@H](Cc1ccccc1)C 6253037
2519 779 None 86 Human Binding pKi = 4.7 4.7 -11 12
UnclassifiedUnclassified
Guide to Pharmacology 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 12014951
2519 779 None 86 Human Binding pKi = 4.7 4.7 -11 12
UnclassifiedUnclassified
Guide to Pharmacology 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 18404493
2519 779 None 86 Human Binding pKi = 4.7 4.7 -11 12
UnclassifiedUnclassified
Guide to Pharmacology 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 19569717
2519.0 779 None 86 Human Binding pKi = 4.7 4.7 -11 12
UnclassifiedUnclassified
Guide to Pharmacology 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 12014951
2519.0 779 None 86 Human Binding pKi = 4.7 4.7 -11 12
UnclassifiedUnclassified
Guide to Pharmacology 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 18404493
2519.0 779 None 86 Human Binding pKi = 4.7 4.7 -11 12
UnclassifiedUnclassified
Guide to Pharmacology 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 19569717
407 779 None 86 Human Binding pKi = 4.7 4.7 -11 12
UnclassifiedUnclassified
Guide to Pharmacology 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 12014951
407 779 None 86 Human Binding pKi = 4.7 4.7 -11 12
UnclassifiedUnclassified
Guide to Pharmacology 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 18404493
407 779 None 86 Human Binding pKi = 4.7 4.7 -11 12
UnclassifiedUnclassified
Guide to Pharmacology 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 19569717
463 779 None 86 Human Binding pKi = 4.7 4.7 -11 12
UnclassifiedUnclassified
Guide to Pharmacology 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 12014951
463 779 None 86 Human Binding pKi = 4.7 4.7 -11 12
UnclassifiedUnclassified
Guide to Pharmacology 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 18404493
463 779 None 86 Human Binding pKi = 4.7 4.7 -11 12
UnclassifiedUnclassified
Guide to Pharmacology 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 19569717
CHEMBL113 779 None 86 Human Binding pKi = 4.7 4.7 -11 12
UnclassifiedUnclassified
Guide to Pharmacology 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 12014951
CHEMBL113 779 None 86 Human Binding pKi = 4.7 4.7 -11 12
UnclassifiedUnclassified
Guide to Pharmacology 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 18404493
CHEMBL113 779 None 86 Human Binding pKi = 4.7 4.7 -11 12
UnclassifiedUnclassified
Guide to Pharmacology 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 19569717
DB00201 779 None 86 Human Binding pKi = 4.7 4.7 -11 12
UnclassifiedUnclassified
Guide to Pharmacology 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 12014951
DB00201 779 None 86 Human Binding pKi = 4.7 4.7 -11 12
UnclassifiedUnclassified
Guide to Pharmacology 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 18404493
DB00201 779 None 86 Human Binding pKi = 4.7 4.7 -11 12
UnclassifiedUnclassified
Guide to Pharmacology 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 19569717
414 3382 None 33 Mouse Binding pKi = 4.7 4.7 -16218 12
UnclassifiedUnclassified
Guide to Pharmacology 385 6 4 9 0.5 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N[C@@H](Cc1ccccc1)C 8135856
93205 3382 None 33 Mouse Binding pKi = 4.7 4.7 -16218 12
UnclassifiedUnclassified
Guide to Pharmacology 385 6 4 9 0.5 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N[C@@H](Cc1ccccc1)C 8135856
CHEMBL139000 3382 None 33 Mouse Binding pKi = 4.7 4.7 -16218 12
UnclassifiedUnclassified
Guide to Pharmacology 385 6 4 9 0.5 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N[C@@H](Cc1ccccc1)C 8135856
372 58 None 103 Human Binding pKi = 4.8 4.8 -2630 9
UnclassifiedUnclassified
Guide to Pharmacology 301 2 4 9 -1.3 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2N 10496952
372 58 None 103 Human Binding pKi = 4.8 4.8 -2630 9
UnclassifiedUnclassified
Guide to Pharmacology 301 2 4 9 -1.3 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2N 11093773
372 58 None 103 Human Binding pKi = 4.8 4.8 -2630 9
UnclassifiedUnclassified
Guide to Pharmacology 301 2 4 9 -1.3 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2N 6253037
8974 58 None 103 Human Binding pKi = 4.8 4.8 -2630 9
UnclassifiedUnclassified
Guide to Pharmacology 301 2 4 9 -1.3 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2N 10496952
8974 58 None 103 Human Binding pKi = 4.8 4.8 -2630 9
UnclassifiedUnclassified
Guide to Pharmacology 301 2 4 9 -1.3 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2N 11093773
8974 58 None 103 Human Binding pKi = 4.8 4.8 -2630 9
UnclassifiedUnclassified
Guide to Pharmacology 301 2 4 9 -1.3 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2N 6253037
CHEMBL285819 58 None 103 Human Binding pKi = 4.8 4.8 -2630 9
UnclassifiedUnclassified
Guide to Pharmacology 301 2 4 9 -1.3 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2N 10496952
CHEMBL285819 58 None 103 Human Binding pKi = 4.8 4.8 -2630 9
UnclassifiedUnclassified
Guide to Pharmacology 301 2 4 9 -1.3 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2N 11093773
CHEMBL285819 58 None 103 Human Binding pKi = 4.8 4.8 -2630 9
UnclassifiedUnclassified
Guide to Pharmacology 301 2 4 9 -1.3 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2N 6253037
2844 283 None 107 Human Binding pKi = 4.8 4.8 -467 8
UnclassifiedUnclassified
Guide to Pharmacology 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 14662005
2844 283 None 107 Human Binding pKi = 4.8 4.8 -467 8
UnclassifiedUnclassified
Guide to Pharmacology 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 15822182
2844 283 None 107 Human Binding pKi = 4.8 4.8 -467 8
UnclassifiedUnclassified
Guide to Pharmacology 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 7746802
60961 283 None 107 Human Binding pKi = 4.8 4.8 -467 8
UnclassifiedUnclassified
Guide to Pharmacology 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 14662005
60961 283 None 107 Human Binding pKi = 4.8 4.8 -467 8
UnclassifiedUnclassified
Guide to Pharmacology 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 15822182
60961 283 None 107 Human Binding pKi = 4.8 4.8 -467 8
UnclassifiedUnclassified
Guide to Pharmacology 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 7746802
60961.0 283 None 107 Human Binding pKi = 4.8 4.8 -467 8
UnclassifiedUnclassified
Guide to Pharmacology 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 14662005
60961.0 283 None 107 Human Binding pKi = 4.8 4.8 -467 8
UnclassifiedUnclassified
Guide to Pharmacology 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 15822182
60961.0 283 None 107 Human Binding pKi = 4.8 4.8 -467 8
UnclassifiedUnclassified
Guide to Pharmacology 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 7746802
90 283 None 107 Human Binding pKi = 4.8 4.8 -467 8
UnclassifiedUnclassified
Guide to Pharmacology 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 14662005
90 283 None 107 Human Binding pKi = 4.8 4.8 -467 8
UnclassifiedUnclassified
Guide to Pharmacology 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 15822182
90 283 None 107 Human Binding pKi = 4.8 4.8 -467 8
UnclassifiedUnclassified
Guide to Pharmacology 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 7746802
CHEMBL477 283 None 107 Human Binding pKi = 4.8 4.8 -467 8
UnclassifiedUnclassified
Guide to Pharmacology 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 14662005
CHEMBL477 283 None 107 Human Binding pKi = 4.8 4.8 -467 8
UnclassifiedUnclassified
Guide to Pharmacology 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 15822182
CHEMBL477 283 None 107 Human Binding pKi = 4.8 4.8 -467 8
UnclassifiedUnclassified
Guide to Pharmacology 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 7746802
DB00640 283 None 107 Human Binding pKi = 4.8 4.8 -467 8
UnclassifiedUnclassified
Guide to Pharmacology 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 14662005
DB00640 283 None 107 Human Binding pKi = 4.8 4.8 -467 8
UnclassifiedUnclassified
Guide to Pharmacology 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 15822182
DB00640 283 None 107 Human Binding pKi = 4.8 4.8 -467 8
UnclassifiedUnclassified
Guide to Pharmacology 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 7746802
2519 779 None 86 Mouse Binding pKi = 4.9 4.9 -1 12
UnclassifiedUnclassified
Guide to Pharmacology 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 8135856
2519.0 779 None 86 Mouse Binding pKi = 4.9 4.9 -1 12
UnclassifiedUnclassified
Guide to Pharmacology 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 8135856
407 779 None 86 Mouse Binding pKi = 4.9 4.9 -1 12
UnclassifiedUnclassified
Guide to Pharmacology 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 8135856
463 779 None 86 Mouse Binding pKi = 4.9 4.9 -1 12
UnclassifiedUnclassified
Guide to Pharmacology 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 8135856
CHEMBL113 779 None 86 Mouse Binding pKi = 4.9 4.9 -1 12
UnclassifiedUnclassified
Guide to Pharmacology 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 8135856
DB00201 779 None 86 Mouse Binding pKi = 4.9 4.9 -1 12
UnclassifiedUnclassified
Guide to Pharmacology 194 0 0 6 -1.0 Cn1cnc2c1c(=O)n(C)c(=O)n2C 8135856
5353365 1210 None 32 Rat Binding pKi = 5.1 5.1 -263 6
UnclassifiedUnclassified
Guide to Pharmacology 330 2 0 6 1.8 Clc1cccc(c1)/C=C/c1nc2c(n1C)c(=O)n(c(=O)n2C)C None
5609 1210 None 32 Rat Binding pKi = 5.1 5.1 -263 6
UnclassifiedUnclassified
Guide to Pharmacology 330 2 0 6 1.8 Clc1cccc(c1)/C=C/c1nc2c(n1C)c(=O)n(c(=O)n2C)C None
CHEMBL26138 1210 None 32 Rat Binding pKi = 5.1 5.1 -263 6
UnclassifiedUnclassified
Guide to Pharmacology 330 2 0 6 1.8 Clc1cccc(c1)/C=C/c1nc2c(n1C)c(=O)n(c(=O)n2C)C None
2153 3800 None 115 Mouse Binding pKi = 5.3 5.3 1 14
UnclassifiedUnclassified
Guide to Pharmacology 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 19141710
2153.0 3800 None 115 Mouse Binding pKi = 5.3 5.3 1 14
UnclassifiedUnclassified
Guide to Pharmacology 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 19141710
2620 3800 None 115 Mouse Binding pKi = 5.3 5.3 1 14
UnclassifiedUnclassified
Guide to Pharmacology 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 19141710
413 3800 None 115 Mouse Binding pKi = 5.3 5.3 1 14
UnclassifiedUnclassified
Guide to Pharmacology 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 19141710
CHEMBL190 3800 None 115 Mouse Binding pKi = 5.3 5.3 1 14
UnclassifiedUnclassified
Guide to Pharmacology 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 19141710
DB00277 3800 None 115 Mouse Binding pKi = 5.3 5.3 1 14
UnclassifiedUnclassified
Guide to Pharmacology 180 0 1 5 -1.0 Cn1c(=O)n(C)c2c(c1=O)[nH]cn2 19141710
10046145 2683 None 18 Human Binding pKi = 5.3 5.3 -575 6
UnclassifiedUnclassified
Guide to Pharmacology 394 7 1 8 1.1 OCCCn1c(=O)n(CC#C)c(=O)c2c1nc(n2C)/C=C/c1cccc(c1)OC 10669571
10046145 2683 None 18 Human Binding pKi = 5.3 5.3 -575 6
UnclassifiedUnclassified
Guide to Pharmacology 394 7 1 8 1.1 OCCCn1c(=O)n(CC#C)c(=O)c2c1nc(n2C)/C=C/c1cccc(c1)OC 15696333
5610 2683 None 18 Human Binding pKi = 5.3 5.3 -575 6
UnclassifiedUnclassified
Guide to Pharmacology 394 7 1 8 1.1 OCCCn1c(=O)n(CC#C)c(=O)c2c1nc(n2C)/C=C/c1cccc(c1)OC 10669571
5610 2683 None 18 Human Binding pKi = 5.3 5.3 -575 6
UnclassifiedUnclassified
Guide to Pharmacology 394 7 1 8 1.1 OCCCn1c(=O)n(CC#C)c(=O)c2c1nc(n2C)/C=C/c1cccc(c1)OC 15696333
CHEMBL413079 2683 None 18 Human Binding pKi = 5.3 5.3 -575 6
UnclassifiedUnclassified
Guide to Pharmacology 394 7 1 8 1.1 OCCCn1c(=O)n(CC#C)c(=O)c2c1nc(n2C)/C=C/c1cccc(c1)OC 10669571
CHEMBL413079 2683 None 18 Human Binding pKi = 5.3 5.3 -575 6
UnclassifiedUnclassified
Guide to Pharmacology 394 7 1 8 1.1 OCCCn1c(=O)n(CC#C)c(=O)c2c1nc(n2C)/C=C/c1cccc(c1)OC 15696333
2844 283 None 107 Rat Binding pKi = 5.3 5.3 -158 8
UnclassifiedUnclassified
Guide to Pharmacology 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 14662005
60961 283 None 107 Rat Binding pKi = 5.3 5.3 -158 8
UnclassifiedUnclassified
Guide to Pharmacology 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 14662005
60961.0 283 None 107 Rat Binding pKi = 5.3 5.3 -158 8
UnclassifiedUnclassified
Guide to Pharmacology 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 14662005
90 283 None 107 Rat Binding pKi = 5.3 5.3 -158 8
UnclassifiedUnclassified
Guide to Pharmacology 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 14662005
CHEMBL477 283 None 107 Rat Binding pKi = 5.3 5.3 -158 8
UnclassifiedUnclassified
Guide to Pharmacology 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 14662005
DB00640 283 None 107 Rat Binding pKi = 5.3 5.3 -158 8
UnclassifiedUnclassified
Guide to Pharmacology 267 2 4 9 -2.0 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 14662005
2099 3046 None 81 Human Binding pKi = 5.3 5.3 19 3
UnclassifiedUnclassified
Guide to Pharmacology 278 5 0 7 0.2 CC(=O)CCCCn1c(=O)c2n(C)cnc2n(c1=O)C 12014951
4740 3046 None 81 Human Binding pKi = 5.3 5.3 19 3
UnclassifiedUnclassified
Guide to Pharmacology 278 5 0 7 0.2 CC(=O)CCCCn1c(=O)c2n(C)cnc2n(c1=O)C 12014951
4740.0 3046 None 81 Human Binding pKi = 5.3 5.3 19 3
UnclassifiedUnclassified
Guide to Pharmacology 278 5 0 7 0.2 CC(=O)CCCCn1c(=O)c2n(C)cnc2n(c1=O)C 12014951
7095 3046 None 81 Human Binding pKi = 5.3 5.3 19 3
UnclassifiedUnclassified
Guide to Pharmacology 278 5 0 7 0.2 CC(=O)CCCCn1c(=O)c2n(C)cnc2n(c1=O)C 12014951
CHEMBL628 3046 None 81 Human Binding pKi = 5.3 5.3 19 3
UnclassifiedUnclassified
Guide to Pharmacology 278 5 0 7 0.2 CC(=O)CCCCn1c(=O)c2n(C)cnc2n(c1=O)C 12014951
DB00806 3046 None 81 Human Binding pKi = 5.3 5.3 19 3
UnclassifiedUnclassified
Guide to Pharmacology 278 5 0 7 0.2 CC(=O)CCCCn1c(=O)c2n(C)cnc2n(c1=O)C 12014951
3281 1370 None 54 Human Binding pKi = 5.4 5.4 -4265 7
UnclassifiedUnclassified
Guide to Pharmacology 308 3 3 4 3.3 O[C@@H]1CC[C@H](CC1)Nc1nc(nc2c1cc[nH]2)c1ccccc1 17558436
9953065 1370 None 54 Human Binding pKi = 5.4 5.4 -4265 7
UnclassifiedUnclassified
Guide to Pharmacology 308 3 3 4 3.3 O[C@@H]1CC[C@H](CC1)Nc1nc(nc2c1cc[nH]2)c1ccccc1 17558436
CHEMBL4204703 1370 None 54 Human Binding pKi = 5.4 5.4 -4265 7
UnclassifiedUnclassified
Guide to Pharmacology 308 3 3 4 3.3 O[C@@H]1CC[C@H](CC1)Nc1nc(nc2c1cc[nH]2)c1ccccc1 17558436
CHEMBL592435 1370 None 54 Human Binding pKi = 5.4 5.4 -4265 7
UnclassifiedUnclassified
Guide to Pharmacology 308 3 3 4 3.3 O[C@@H]1CC[C@H](CC1)Nc1nc(nc2c1cc[nH]2)c1ccccc1 17558436
DB12446 1370 None 54 Human Binding pKi = 5.4 5.4 -4265 7
UnclassifiedUnclassified
Guide to Pharmacology 308 3 3 4 3.3 O[C@@H]1CC[C@H](CC1)Nc1nc(nc2c1cc[nH]2)c1ccccc1 17558436
135401232 3206 None 5 Mouse Binding pKi = 5.7 5.7 -1698 7
UnclassifiedUnclassified
Guide to Pharmacology 397 2 1 3 4.4 CC[C@H]1N=c2n(C1)c(=O)n(c1c2[nH]c(n1)c1cc(Cl)cc(c1Cl)Cl)C 12139454
5619 3206 None 5 Mouse Binding pKi = 5.7 5.7 -1698 7
UnclassifiedUnclassified
Guide to Pharmacology 397 2 1 3 4.4 CC[C@H]1N=c2n(C1)c(=O)n(c1c2[nH]c(n1)c1cc(Cl)cc(c1Cl)Cl)C 12139454
CHEMBL1562432 3206 None 5 Mouse Binding pKi = 5.7 5.7 -1698 7
UnclassifiedUnclassified
Guide to Pharmacology 397 2 1 3 4.4 CC[C@H]1N=c2n(C1)c(=O)n(c1c2[nH]c(n1)c1cc(Cl)cc(c1Cl)Cl)C 12139454
135433658 3207 None 3 Mouse Binding pKi = 5.7 5.7 -208 8
UnclassifiedUnclassified
Guide to Pharmacology 295 2 1 3 2.5 CC[C@@H]1Cn2c(=N1)c1[nH]c(nc1n(c2=O)C)c1ccccc1 12139454
5620 3207 None 3 Mouse Binding pKi = 5.7 5.7 -208 8
UnclassifiedUnclassified
Guide to Pharmacology 295 2 1 3 2.5 CC[C@@H]1Cn2c(=N1)c1[nH]c(nc1n(c2=O)C)c1ccccc1 12139454
9882625 3207 None 3 Mouse Binding pKi = 5.7 5.7 -208 8
UnclassifiedUnclassified
Guide to Pharmacology 295 2 1 3 2.5 CC[C@@H]1Cn2c(=N1)c1[nH]c(nc1n(c2=O)C)c1ccccc1 12139454
CHEMBL1625681 3207 None 3 Mouse Binding pKi = 5.7 5.7 -208 8
UnclassifiedUnclassified
Guide to Pharmacology 295 2 1 3 2.5 CC[C@@H]1Cn2c(=N1)c1[nH]c(nc1n(c2=O)C)c1ccccc1 12139454
377 2758 None 53 Mouse Binding pKi = 5.7 5.7 -4265 15
UnclassifiedUnclassified
Guide to Pharmacology 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N None
425 2758 None 53 Mouse Binding pKi = 5.7 5.7 -4265 15
UnclassifiedUnclassified
Guide to Pharmacology 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N None
448222 2758 None 53 Mouse Binding pKi = 5.7 5.7 -4265 15
UnclassifiedUnclassified
Guide to Pharmacology 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N None
CHEMBL464859 2758 None 53 Mouse Binding pKi = 5.7 5.7 -4265 15
UnclassifiedUnclassified
Guide to Pharmacology 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N None
459 2618 None 34 Human Binding pKi = 5.8 5.8 -389 5
UnclassifiedUnclassified
Guide to Pharmacology 432 6 2 9 3.8 CCCn1cc2c(n1)nc(n1c2nc(n1)c1ccco1)NC(=O)Nc1ccc(cc1)OC 10779381
459 2618 None 34 Human Binding pKi = 5.8 5.8 -389 5
UnclassifiedUnclassified
Guide to Pharmacology 432 6 2 9 3.8 CCCn1cc2c(n1)nc(n1c2nc(n1)c1ccco1)NC(=O)Nc1ccc(cc1)OC 16219300
459 2618 None 34 Human Binding pKi = 5.8 5.8 -389 5
UnclassifiedUnclassified
Guide to Pharmacology 432 6 2 9 3.8 CCCn1cc2c(n1)nc(n1c2nc(n1)c1ccco1)NC(=O)Nc1ccc(cc1)OC 16518376
477 2618 None 34 Human Binding pKi = 5.8 5.8 -389 5
UnclassifiedUnclassified
Guide to Pharmacology 432 6 2 9 3.8 CCCn1cc2c(n1)nc(n1c2nc(n1)c1ccco1)NC(=O)Nc1ccc(cc1)OC 10779381
477 2618 None 34 Human Binding pKi = 5.8 5.8 -389 5
UnclassifiedUnclassified
Guide to Pharmacology 432 6 2 9 3.8 CCCn1cc2c(n1)nc(n1c2nc(n1)c1ccco1)NC(=O)Nc1ccc(cc1)OC 16219300
477 2618 None 34 Human Binding pKi = 5.8 5.8 -389 5
UnclassifiedUnclassified
Guide to Pharmacology 432 6 2 9 3.8 CCCn1cc2c(n1)nc(n1c2nc(n1)c1ccco1)NC(=O)Nc1ccc(cc1)OC 16518376
5310960 2618 None 34 Human Binding pKi = 5.8 5.8 -389 5
UnclassifiedUnclassified
Guide to Pharmacology 432 6 2 9 3.8 CCCn1cc2c(n1)nc(n1c2nc(n1)c1ccco1)NC(=O)Nc1ccc(cc1)OC 10779381
5310960 2618 None 34 Human Binding pKi = 5.8 5.8 -389 5
UnclassifiedUnclassified
Guide to Pharmacology 432 6 2 9 3.8 CCCn1cc2c(n1)nc(n1c2nc(n1)c1ccco1)NC(=O)Nc1ccc(cc1)OC 16219300
5310960 2618 None 34 Human Binding pKi = 5.8 5.8 -389 5
UnclassifiedUnclassified
Guide to Pharmacology 432 6 2 9 3.8 CCCn1cc2c(n1)nc(n1c2nc(n1)c1ccco1)NC(=O)Nc1ccc(cc1)OC 16518376
CHEMBL302765 2618 None 34 Human Binding pKi = 5.8 5.8 -389 5
UnclassifiedUnclassified
Guide to Pharmacology 432 6 2 9 3.8 CCCn1cc2c(n1)nc(n1c2nc(n1)c1ccco1)NC(=O)Nc1ccc(cc1)OC 10779381
CHEMBL302765 2618 None 34 Human Binding pKi = 5.8 5.8 -389 5
UnclassifiedUnclassified
Guide to Pharmacology 432 6 2 9 3.8 CCCn1cc2c(n1)nc(n1c2nc(n1)c1ccco1)NC(=O)Nc1ccc(cc1)OC 16219300
CHEMBL302765 2618 None 34 Human Binding pKi = 5.8 5.8 -389 5
UnclassifiedUnclassified
Guide to Pharmacology 432 6 2 9 3.8 CCCn1cc2c(n1)nc(n1c2nc(n1)c1ccco1)NC(=O)Nc1ccc(cc1)OC 16518376
5606 1644 None 17 Human Binding pKi = 6.0 6.0 -1995 6
UnclassifiedUnclassified
Guide to Pharmacology 375 5 1 4 3.8 OCC[C@H]1CCCCN1C(=O)/C=C/c1c(nn2c1cccc2)c1ccccc1 16518376
6439091 1644 None 17 Human Binding pKi = 6.0 6.0 -1995 6
UnclassifiedUnclassified
Guide to Pharmacology 375 5 1 4 3.8 OCC[C@H]1CCCCN1C(=O)/C=C/c1c(nn2c1cccc2)c1ccccc1 16518376
CHEMBL440115 1644 None 17 Human Binding pKi = 6.0 6.0 -1995 6
UnclassifiedUnclassified
Guide to Pharmacology 375 5 1 4 3.8 OCC[C@H]1CCCCN1C(=O)/C=C/c1c(nn2c1cccc2)c1ccccc1 16518376
135409562 2184 None 7 Human Binding pKi = 6.2 6.2 -3090 4
UnclassifiedUnclassified
Guide to Pharmacology 373 3 1 3 3.3 CCCn1c2nc([nH]c2c2=NCCn2c1=O)c1ccc(cc1)Br 12063073
5618 2184 None 7 Human Binding pKi = 6.2 6.2 -3090 4
UnclassifiedUnclassified
Guide to Pharmacology 373 3 1 3 3.3 CCCn1c2nc([nH]c2c2=NCCn2c1=O)c1ccc(cc1)Br 12063073
CHEMBL2181965 2184 None 7 Human Binding pKi = 6.2 6.2 -3090 4
UnclassifiedUnclassified
Guide to Pharmacology 373 3 1 3 3.3 CCCn1c2nc([nH]c2c2=NCCn2c1=O)c1ccc(cc1)Br 12063073
176408 3557 None 84 Human Binding pKi = 6.3 6.3 -407 7
UnclassifiedUnclassified
Guide to Pharmacology 345 4 1 8 2.6 Nc1nc2n(CCc3ccccc3)ncc2c2n1nc(n2)c1ccco1 11093773
176408 3557 None 84 Human Binding pKi = 6.3 6.3 -407 7
UnclassifiedUnclassified
Guide to Pharmacology 345 4 1 8 2.6 Nc1nc2n(CCc3ccccc3)ncc2c2n1nc(n2)c1ccco1 16518376
403 3557 None 84 Human Binding pKi = 6.3 6.3 -407 7
UnclassifiedUnclassified
Guide to Pharmacology 345 4 1 8 2.6 Nc1nc2n(CCc3ccccc3)ncc2c2n1nc(n2)c1ccco1 11093773
403 3557 None 84 Human Binding pKi = 6.3 6.3 -407 7
UnclassifiedUnclassified
Guide to Pharmacology 345 4 1 8 2.6 Nc1nc2n(CCc3ccccc3)ncc2c2n1nc(n2)c1ccco1 16518376
431 3557 None 84 Human Binding pKi = 6.3 6.3 -407 7
UnclassifiedUnclassified
Guide to Pharmacology 345 4 1 8 2.6 Nc1nc2n(CCc3ccccc3)ncc2c2n1nc(n2)c1ccco1 11093773
431 3557 None 84 Human Binding pKi = 6.3 6.3 -407 7
UnclassifiedUnclassified
Guide to Pharmacology 345 4 1 8 2.6 Nc1nc2n(CCc3ccccc3)ncc2c2n1nc(n2)c1ccco1 16518376
CHEMBL17127 3557 None 84 Human Binding pKi = 6.3 6.3 -407 7
UnclassifiedUnclassified
Guide to Pharmacology 345 4 1 8 2.6 Nc1nc2n(CCc3ccccc3)ncc2c2n1nc(n2)c1ccco1 11093773
CHEMBL17127 3557 None 84 Human Binding pKi = 6.3 6.3 -407 7
UnclassifiedUnclassified
Guide to Pharmacology 345 4 1 8 2.6 Nc1nc2n(CCc3ccccc3)ncc2c2n1nc(n2)c1ccco1 16518376
377 2758 None 53 Human Binding pKi = 6.3 6.3 -1479 15
UnclassifiedUnclassified
Guide to Pharmacology 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10496952
377 2758 None 53 Human Binding pKi = 6.3 6.3 -1479 15
UnclassifiedUnclassified
Guide to Pharmacology 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 11093773
377 2758 None 53 Human Binding pKi = 6.3 6.3 -1479 15
UnclassifiedUnclassified
Guide to Pharmacology 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 11266650
377 2758 None 53 Human Binding pKi = 6.3 6.3 -1479 15
UnclassifiedUnclassified
Guide to Pharmacology 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 14662005
377 2758 None 53 Human Binding pKi = 6.3 6.3 -1479 15
UnclassifiedUnclassified
Guide to Pharmacology 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 15194002
377 2758 None 53 Human Binding pKi = 6.3 6.3 -1479 15
UnclassifiedUnclassified
Guide to Pharmacology 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 15267242
377 2758 None 53 Human Binding pKi = 6.3 6.3 -1479 15
UnclassifiedUnclassified
Guide to Pharmacology 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 16219300
425 2758 None 53 Human Binding pKi = 6.3 6.3 -1479 15
UnclassifiedUnclassified
Guide to Pharmacology 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10496952
425 2758 None 53 Human Binding pKi = 6.3 6.3 -1479 15
UnclassifiedUnclassified
Guide to Pharmacology 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 11093773
425 2758 None 53 Human Binding pKi = 6.3 6.3 -1479 15
UnclassifiedUnclassified
Guide to Pharmacology 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 11266650
425 2758 None 53 Human Binding pKi = 6.3 6.3 -1479 15
UnclassifiedUnclassified
Guide to Pharmacology 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 14662005
425 2758 None 53 Human Binding pKi = 6.3 6.3 -1479 15
UnclassifiedUnclassified
Guide to Pharmacology 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 15194002
425 2758 None 53 Human Binding pKi = 6.3 6.3 -1479 15
UnclassifiedUnclassified
Guide to Pharmacology 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 15267242
425 2758 None 53 Human Binding pKi = 6.3 6.3 -1479 15
UnclassifiedUnclassified
Guide to Pharmacology 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 16219300
448222 2758 None 53 Human Binding pKi = 6.3 6.3 -1479 15
UnclassifiedUnclassified
Guide to Pharmacology 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10496952
448222 2758 None 53 Human Binding pKi = 6.3 6.3 -1479 15
UnclassifiedUnclassified
Guide to Pharmacology 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 11093773
448222 2758 None 53 Human Binding pKi = 6.3 6.3 -1479 15
UnclassifiedUnclassified
Guide to Pharmacology 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 11266650
448222 2758 None 53 Human Binding pKi = 6.3 6.3 -1479 15
UnclassifiedUnclassified
Guide to Pharmacology 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 14662005
448222 2758 None 53 Human Binding pKi = 6.3 6.3 -1479 15
UnclassifiedUnclassified
Guide to Pharmacology 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 15194002
448222 2758 None 53 Human Binding pKi = 6.3 6.3 -1479 15
UnclassifiedUnclassified
Guide to Pharmacology 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 15267242
448222 2758 None 53 Human Binding pKi = 6.3 6.3 -1479 15
UnclassifiedUnclassified
Guide to Pharmacology 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 16219300
CHEMBL464859 2758 None 53 Human Binding pKi = 6.3 6.3 -1479 15
UnclassifiedUnclassified
Guide to Pharmacology 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 10496952
CHEMBL464859 2758 None 53 Human Binding pKi = 6.3 6.3 -1479 15
UnclassifiedUnclassified
Guide to Pharmacology 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 11093773
CHEMBL464859 2758 None 53 Human Binding pKi = 6.3 6.3 -1479 15
UnclassifiedUnclassified
Guide to Pharmacology 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 11266650
CHEMBL464859 2758 None 53 Human Binding pKi = 6.3 6.3 -1479 15
UnclassifiedUnclassified
Guide to Pharmacology 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 14662005
CHEMBL464859 2758 None 53 Human Binding pKi = 6.3 6.3 -1479 15
UnclassifiedUnclassified
Guide to Pharmacology 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 15194002
CHEMBL464859 2758 None 53 Human Binding pKi = 6.3 6.3 -1479 15
UnclassifiedUnclassified
Guide to Pharmacology 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 15267242
CHEMBL464859 2758 None 53 Human Binding pKi = 6.3 6.3 -1479 15
UnclassifiedUnclassified
Guide to Pharmacology 308 3 4 9 -1.8 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N 16219300
3281 1370 None 54 Rat Binding pKi = 6.3 6.3 -537 7
UnclassifiedUnclassified
Guide to Pharmacology 308 3 3 4 3.3 O[C@@H]1CC[C@H](CC1)Nc1nc(nc2c1cc[nH]2)c1ccccc1 17558436
9953065 1370 None 54 Rat Binding pKi = 6.3 6.3 -537 7
UnclassifiedUnclassified
Guide to Pharmacology 308 3 3 4 3.3 O[C@@H]1CC[C@H](CC1)Nc1nc(nc2c1cc[nH]2)c1ccccc1 17558436
CHEMBL4204703 1370 None 54 Rat Binding pKi = 6.3 6.3 -537 7
UnclassifiedUnclassified
Guide to Pharmacology 308 3 3 4 3.3 O[C@@H]1CC[C@H](CC1)Nc1nc(nc2c1cc[nH]2)c1ccccc1 17558436
CHEMBL592435 1370 None 54 Rat Binding pKi = 6.3 6.3 -537 7
UnclassifiedUnclassified
Guide to Pharmacology 308 3 3 4 3.3 O[C@@H]1CC[C@H](CC1)Nc1nc(nc2c1cc[nH]2)c1ccccc1 17558436
DB12446 1370 None 54 Rat Binding pKi = 6.3 6.3 -537 7
UnclassifiedUnclassified
Guide to Pharmacology 308 3 3 4 3.3 O[C@@H]1CC[C@H](CC1)Nc1nc(nc2c1cc[nH]2)c1ccccc1 17558436
5613 3685 None 35 Human Binding pKi = 6.5 6.5 -45 4
UnclassifiedUnclassified
Guide to Pharmacology 272 4 1 8 0.9 CCCCc1nc(N)c2c(n1)n(C)c(n2)n1nccn1 16250647
9860294 3685 None 35 Human Binding pKi = 6.5 6.5 -45 4
UnclassifiedUnclassified
Guide to Pharmacology 272 4 1 8 0.9 CCCCc1nc(N)c2c(n1)n(C)c(n2)n1nccn1 16250647
CHEMBL197669 3685 None 35 Human Binding pKi = 6.5 6.5 -45 4
UnclassifiedUnclassified
Guide to Pharmacology 272 4 1 8 0.9 CCCCc1nc(N)c2c(n1)n(C)c(n2)n1nccn1 16250647
11717831 585 None 48 Mouse Binding pKi = 6.5 6.5 -60 5
UnclassifiedUnclassified
Guide to Pharmacology 379 7 2 7 2.4 N#Cc1c(N)nc(c(c1c1ccc(cc1)OCC1CC1)C#N)SCC(=O)N 17632123
3289 585 None 48 Mouse Binding pKi = 6.5 6.5 -60 5
UnclassifiedUnclassified
Guide to Pharmacology 379 7 2 7 2.4 N#Cc1c(N)nc(c(c1c1ccc(cc1)OCC1CC1)C#N)SCC(=O)N 17632123
CHEMBL4202825 585 None 48 Mouse Binding pKi = 6.5 6.5 -60 5
UnclassifiedUnclassified
Guide to Pharmacology 379 7 2 7 2.4 N#Cc1c(N)nc(c(c1c1ccc(cc1)OCC1CC1)C#N)SCC(=O)N 17632123
5604 3368 None 35 Human Binding pKi = 6.5 6.5 -1995 10
UnclassifiedUnclassified
Guide to Pharmacology 356 5 1 5 2.8 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C12CC3CC2CC(C1)C3 17125264
64627 3368 None 35 Human Binding pKi = 6.5 6.5 -1995 10
UnclassifiedUnclassified
Guide to Pharmacology 356 5 1 5 2.8 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C12CC3CC2CC(C1)C3 17125264
CHEMBL52333 3368 None 35 Human Binding pKi = 6.5 6.5 -1995 10
UnclassifiedUnclassified
Guide to Pharmacology 356 5 1 5 2.8 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C12CC3CC2CC(C1)C3 17125264
DB05360 3368 None 35 Human Binding pKi = 6.5 6.5 -1995 10
UnclassifiedUnclassified
Guide to Pharmacology 356 5 1 5 2.8 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C12CC3CC2CC(C1)C3 17125264
1329 1472 None 86 Rat Binding pKi = 6.7 6.7 -1905 14
UnclassifiedUnclassified
Guide to Pharmacology 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 12014951
1329 1472 None 86 Rat Binding pKi = 6.7 6.7 -1905 14
UnclassifiedUnclassified
Guide to Pharmacology 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 12954362
386 1472 None 86 Rat Binding pKi = 6.7 6.7 -1905 14
UnclassifiedUnclassified
Guide to Pharmacology 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 12014951
386 1472 None 86 Rat Binding pKi = 6.7 6.7 -1905 14
UnclassifiedUnclassified
Guide to Pharmacology 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 12954362
CHEMBL183 1472 None 86 Rat Binding pKi = 6.7 6.7 -1905 14
UnclassifiedUnclassified
Guide to Pharmacology 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 12014951
CHEMBL183 1472 None 86 Rat Binding pKi = 6.7 6.7 -1905 14
UnclassifiedUnclassified
Guide to Pharmacology 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 12954362
DB12946 1472 None 86 Rat Binding pKi = 6.7 6.7 -1905 14
UnclassifiedUnclassified
Guide to Pharmacology 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 12014951
DB12946 1472 None 86 Rat Binding pKi = 6.7 6.7 -1905 14
UnclassifiedUnclassified
Guide to Pharmacology 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 12954362
11689583 3214 None 29 Human Binding pKi = 6.7 6.7 -1513 7
UnclassifiedUnclassified
Guide to Pharmacology 386 7 2 6 2.1 OCCCn1c2[nH]c(nc2c(=O)n(c1=O)CCCC)C12CC3CC2CC(C1)C3 16458010
3285 3214 None 29 Human Binding pKi = 6.7 6.7 -1513 7
UnclassifiedUnclassified
Guide to Pharmacology 386 7 2 6 2.1 OCCCn1c2[nH]c(nc2c(=O)n(c1=O)CCCC)C12CC3CC2CC(C1)C3 16458010
CHEMBL1316674 3214 None 29 Human Binding pKi = 6.7 6.7 -1513 7
UnclassifiedUnclassified
Guide to Pharmacology 386 7 2 6 2.1 OCCCn1c2[nH]c(nc2c(=O)n(c1=O)CCCC)C12CC3CC2CC(C1)C3 16458010
11224 582 None 35 Human Binding pKi = 7.0 7.0 - 1
UnclassifiedUnclassified
Guide to Pharmacology 433 4 1 7 2.1 CCn1c(=O)c2c(C)c(sc2n(c1=O)CCC(F)(F)F)C(=O)N1CCC(CC1)O 30576906
118016229 582 None 35 Human Binding pKi = 7.0 7.0 - 1
UnclassifiedUnclassified
Guide to Pharmacology 433 4 1 7 2.1 CCn1c(=O)c2c(C)c(sc2n(c1=O)CCC(F)(F)F)C(=O)N1CCC(CC1)O 30576906
CHEMBL4522981 582 None 35 Human Binding pKi = 7.0 7.0 - 1
UnclassifiedUnclassified
Guide to Pharmacology 433 4 1 7 2.1 CCn1c(=O)c2c(C)c(sc2n(c1=O)CCC(F)(F)F)C(=O)N1CCC(CC1)O 30576906
2690 903 None 66 Human Binding pKi = 7.1 7.1 -30 9
UnclassifiedUnclassified
Guide to Pharmacology 285 1 1 6 2.8 Clc1ccc2c(c1)c1nc(nn1c(n2)N)c1ccco1 10624567
2690 903 None 66 Human Binding pKi = 7.1 7.1 -30 9
UnclassifiedUnclassified
Guide to Pharmacology 285 1 1 6 2.8 Clc1ccc2c(c1)c1nc(nn1c(n2)N)c1ccco1 11266650
2690 903 None 66 Human Binding pKi = 7.1 7.1 -30 9
UnclassifiedUnclassified
Guide to Pharmacology 285 1 1 6 2.8 Clc1ccc2c(c1)c1nc(nn1c(n2)N)c1ccco1 15194002
2690 903 None 66 Human Binding pKi = 7.1 7.1 -30 9
UnclassifiedUnclassified
Guide to Pharmacology 285 1 1 6 2.8 Clc1ccc2c(c1)c1nc(nn1c(n2)N)c1ccco1 19141710
2690 903 None 66 Human Binding pKi = 7.1 7.1 -30 9
UnclassifiedUnclassified
Guide to Pharmacology 285 1 1 6 2.8 Clc1ccc2c(c1)c1nc(nn1c(n2)N)c1ccco1 9459566
2690 903 None 66 Human Binding pKi = 7.1 7.1 -30 9
UnclassifiedUnclassified
Guide to Pharmacology 285 1 1 6 2.8 Clc1ccc2c(c1)c1nc(nn1c(n2)N)c1ccco1 9933143
384 903 None 66 Human Binding pKi = 7.1 7.1 -30 9
UnclassifiedUnclassified
Guide to Pharmacology 285 1 1 6 2.8 Clc1ccc2c(c1)c1nc(nn1c(n2)N)c1ccco1 10624567
384 903 None 66 Human Binding pKi = 7.1 7.1 -30 9
UnclassifiedUnclassified
Guide to Pharmacology 285 1 1 6 2.8 Clc1ccc2c(c1)c1nc(nn1c(n2)N)c1ccco1 11266650
384 903 None 66 Human Binding pKi = 7.1 7.1 -30 9
UnclassifiedUnclassified
Guide to Pharmacology 285 1 1 6 2.8 Clc1ccc2c(c1)c1nc(nn1c(n2)N)c1ccco1 15194002
384 903 None 66 Human Binding pKi = 7.1 7.1 -30 9
UnclassifiedUnclassified
Guide to Pharmacology 285 1 1 6 2.8 Clc1ccc2c(c1)c1nc(nn1c(n2)N)c1ccco1 19141710
384 903 None 66 Human Binding pKi = 7.1 7.1 -30 9
UnclassifiedUnclassified
Guide to Pharmacology 285 1 1 6 2.8 Clc1ccc2c(c1)c1nc(nn1c(n2)N)c1ccco1 9459566
384 903 None 66 Human Binding pKi = 7.1 7.1 -30 9
UnclassifiedUnclassified
Guide to Pharmacology 285 1 1 6 2.8 Clc1ccc2c(c1)c1nc(nn1c(n2)N)c1ccco1 9933143
CHEMBL16687 903 None 66 Human Binding pKi = 7.1 7.1 -30 9
UnclassifiedUnclassified
Guide to Pharmacology 285 1 1 6 2.8 Clc1ccc2c(c1)c1nc(nn1c(n2)N)c1ccco1 10624567
CHEMBL16687 903 None 66 Human Binding pKi = 7.1 7.1 -30 9
UnclassifiedUnclassified
Guide to Pharmacology 285 1 1 6 2.8 Clc1ccc2c(c1)c1nc(nn1c(n2)N)c1ccco1 11266650
CHEMBL16687 903 None 66 Human Binding pKi = 7.1 7.1 -30 9
UnclassifiedUnclassified
Guide to Pharmacology 285 1 1 6 2.8 Clc1ccc2c(c1)c1nc(nn1c(n2)N)c1ccco1 15194002
CHEMBL16687 903 None 66 Human Binding pKi = 7.1 7.1 -30 9
UnclassifiedUnclassified
Guide to Pharmacology 285 1 1 6 2.8 Clc1ccc2c(c1)c1nc(nn1c(n2)N)c1ccco1 19141710
CHEMBL16687 903 None 66 Human Binding pKi = 7.1 7.1 -30 9
UnclassifiedUnclassified
Guide to Pharmacology 285 1 1 6 2.8 Clc1ccc2c(c1)c1nc(nn1c(n2)N)c1ccco1 9459566
CHEMBL16687 903 None 66 Human Binding pKi = 7.1 7.1 -30 9
UnclassifiedUnclassified
Guide to Pharmacology 285 1 1 6 2.8 Clc1ccc2c(c1)c1nc(nn1c(n2)N)c1ccco1 9933143
216466 3845 None 32 Human Binding pKi = 7.1 7.1 -123 6
UnclassifiedUnclassified
Guide to Pharmacology 416 8 2 6 3.2 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C12CCC(CC1)(CC2)CCC(=O)O 17125264
5605 3845 None 32 Human Binding pKi = 7.1 7.1 -123 6
UnclassifiedUnclassified
Guide to Pharmacology 416 8 2 6 3.2 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C12CCC(CC1)(CC2)CCC(=O)O 17125264
CHEMBL386974 3845 None 32 Human Binding pKi = 7.1 7.1 -123 6
UnclassifiedUnclassified
Guide to Pharmacology 416 8 2 6 3.2 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C12CCC(CC1)(CC2)CCC(=O)O 17125264
CHEMBL414157 3845 None 32 Human Binding pKi = 7.1 7.1 -123 6
UnclassifiedUnclassified
Guide to Pharmacology 416 8 2 6 3.2 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C12CCC(CC1)(CC2)CCC(=O)O 17125264
DB12569 3845 None 32 Human Binding pKi = 7.1 7.1 -123 6
UnclassifiedUnclassified
Guide to Pharmacology 416 8 2 6 3.2 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C12CCC(CC1)(CC2)CCC(=O)O 17125264
1329 1472 None 86 Mouse Binding pKi = 7.1 7.1 -870 14
UnclassifiedUnclassified
Guide to Pharmacology 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 19141710
386 1472 None 86 Mouse Binding pKi = 7.1 7.1 -870 14
UnclassifiedUnclassified
Guide to Pharmacology 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 19141710
CHEMBL183 1472 None 86 Mouse Binding pKi = 7.1 7.1 -870 14
UnclassifiedUnclassified
Guide to Pharmacology 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 19141710
DB12946 1472 None 86 Mouse Binding pKi = 7.1 7.1 -870 14
UnclassifiedUnclassified
Guide to Pharmacology 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 19141710
1329 1472 None 86 Human Binding pKi = 7.1 7.1 -1288 14
UnclassifiedUnclassified
Guide to Pharmacology 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 12014951
1329 1472 None 86 Human Binding pKi = 7.1 7.1 -1288 14
UnclassifiedUnclassified
Guide to Pharmacology 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 15194002
1329 1472 None 86 Human Binding pKi = 7.1 7.1 -1288 14
UnclassifiedUnclassified
Guide to Pharmacology 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 16020631
1329 1472 None 86 Human Binding pKi = 7.1 7.1 -1288 14
UnclassifiedUnclassified
Guide to Pharmacology 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 16902942
386 1472 None 86 Human Binding pKi = 7.1 7.1 -1288 14
UnclassifiedUnclassified
Guide to Pharmacology 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 12014951
386 1472 None 86 Human Binding pKi = 7.1 7.1 -1288 14
UnclassifiedUnclassified
Guide to Pharmacology 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 15194002
386 1472 None 86 Human Binding pKi = 7.1 7.1 -1288 14
UnclassifiedUnclassified
Guide to Pharmacology 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 16020631
386 1472 None 86 Human Binding pKi = 7.1 7.1 -1288 14
UnclassifiedUnclassified
Guide to Pharmacology 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 16902942
CHEMBL183 1472 None 86 Human Binding pKi = 7.1 7.1 -1288 14
UnclassifiedUnclassified
Guide to Pharmacology 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 12014951
CHEMBL183 1472 None 86 Human Binding pKi = 7.1 7.1 -1288 14
UnclassifiedUnclassified
Guide to Pharmacology 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 15194002
CHEMBL183 1472 None 86 Human Binding pKi = 7.1 7.1 -1288 14
UnclassifiedUnclassified
Guide to Pharmacology 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 16020631
CHEMBL183 1472 None 86 Human Binding pKi = 7.1 7.1 -1288 14
UnclassifiedUnclassified
Guide to Pharmacology 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 16902942
DB12946 1472 None 86 Human Binding pKi = 7.1 7.1 -1288 14
UnclassifiedUnclassified
Guide to Pharmacology 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 12014951
DB12946 1472 None 86 Human Binding pKi = 7.1 7.1 -1288 14
UnclassifiedUnclassified
Guide to Pharmacology 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 15194002
DB12946 1472 None 86 Human Binding pKi = 7.1 7.1 -1288 14
UnclassifiedUnclassified
Guide to Pharmacology 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 16020631
DB12946 1472 None 86 Human Binding pKi = 7.1 7.1 -1288 14
UnclassifiedUnclassified
Guide to Pharmacology 304 5 1 5 2.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)C1CCCC1 16902942
21874557 3996 None 51 Human Binding pKi = 7.2 7.2 -52 4
UnclassifiedUnclassified
Guide to Pharmacology 321 3 2 8 2.0 Nc1nc(c2ccco2)c2c(n1)n(nn2)Cc1ccc(c(c1)C)N 19072055
5612 3996 None 51 Human Binding pKi = 7.2 7.2 -52 4
UnclassifiedUnclassified
Guide to Pharmacology 321 3 2 8 2.0 Nc1nc(c2ccco2)c2c(n1)n(nn2)Cc1ccc(c(c1)C)N 19072055
CHEMBL447664 3996 None 51 Human Binding pKi = 7.2 7.2 -52 4
UnclassifiedUnclassified
Guide to Pharmacology 321 3 2 8 2.0 Nc1nc(c2ccco2)c2c(n1)n(nn2)Cc1ccc(c(c1)C)N 19072055
DB06625 3996 None 51 Human Binding pKi = 7.2 7.2 -52 4
UnclassifiedUnclassified
Guide to Pharmacology 321 3 2 8 2.0 Nc1nc(c2ccco2)c2c(n1)n(nn2)Cc1ccc(c(c1)C)N 19072055
3286 3209 None 31 Human Binding pKi = 7.3 7.3 4 9
UnclassifiedUnclassified
Guide to Pharmacology 350 4 3 6 0.7 CCCn1c(=O)[nH]c2c(c1=O)nc([nH]2)c1ccc(cc1)S(=O)(=O)O 11906291
5311479 3209 None 31 Human Binding pKi = 7.3 7.3 4 9
UnclassifiedUnclassified
Guide to Pharmacology 350 4 3 6 0.7 CCCn1c(=O)[nH]c2c(c1=O)nc([nH]2)c1ccc(cc1)S(=O)(=O)O 11906291
CHEMBL8565 3209 None 31 Human Binding pKi = 7.3 7.3 4 9
UnclassifiedUnclassified
Guide to Pharmacology 350 4 3 6 0.7 CCCn1c(=O)[nH]c2c(c1=O)nc([nH]2)c1ccc(cc1)S(=O)(=O)O 11906291
11270783 1226 None 35 Human Binding pKi = 7.7 7.7 67 4
UnclassifiedUnclassified
Guide to Pharmacology 446 6 1 7 3.2 CCCn1c(=O)c2nc([nH]c2n(c1=O)CC)c1cnn(c1)Cc1cccc(c1)C(F)(F)F 18321039
5615 1226 None 35 Human Binding pKi = 7.7 7.7 67 4
UnclassifiedUnclassified
Guide to Pharmacology 446 6 1 7 3.2 CCCn1c(=O)c2nc([nH]c2n(c1=O)CC)c1cnn(c1)Cc1cccc(c1)C(F)(F)F 18321039
CHEMBL260933 1226 None 35 Human Binding pKi = 7.7 7.7 67 4
UnclassifiedUnclassified
Guide to Pharmacology 446 6 1 7 3.2 CCCn1c(=O)c2nc([nH]c2n(c1=O)CC)c1cnn(c1)Cc1cccc(c1)C(F)(F)F 18321039
DB05936 1226 None 35 Human Binding pKi = 7.7 7.7 67 4
UnclassifiedUnclassified
Guide to Pharmacology 446 6 1 7 3.2 CCCn1c(=O)c2nc([nH]c2n(c1=O)CC)c1cnn(c1)Cc1cccc(c1)C(F)(F)F 18321039
11716665 2281 None 37 Human Binding pKi = 7.8 7.8 58 4
UnclassifiedUnclassified
Guide to Pharmacology 316 4 1 7 3.3 n1ccc(nc1)c1cnc(nc1c1ccco1)Nc1cccnc1 17469811
11716665 2281 None 37 Human Binding pKi = 7.8 7.8 58 4
UnclassifiedUnclassified
Guide to Pharmacology 316 4 1 7 3.3 n1ccc(nc1)c1cnc(nc1c1ccco1)Nc1cccnc1 20137946
5617 2281 None 37 Human Binding pKi = 7.8 7.8 58 4
UnclassifiedUnclassified
Guide to Pharmacology 316 4 1 7 3.3 n1ccc(nc1)c1cnc(nc1c1ccco1)Nc1cccnc1 17469811
5617 2281 None 37 Human Binding pKi = 7.8 7.8 58 4
UnclassifiedUnclassified
Guide to Pharmacology 316 4 1 7 3.3 n1ccc(nc1)c1cnc(nc1c1ccco1)Nc1cccnc1 20137946
CHEMBL375293 2281 None 37 Human Binding pKi = 7.8 7.8 58 4
UnclassifiedUnclassified
Guide to Pharmacology 316 4 1 7 3.3 n1ccc(nc1)c1cnc(nc1c1ccco1)Nc1cccnc1 17469811
CHEMBL375293 2281 None 37 Human Binding pKi = 7.8 7.8 58 4
UnclassifiedUnclassified
Guide to Pharmacology 316 4 1 7 3.3 n1ccc(nc1)c1cnc(nc1c1ccco1)Nc1cccnc1 20137946
449 2643 None 52 Rat Binding pKi = 7.8 7.8 -9 9
UnclassifiedUnclassified
Guide to Pharmacology 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10737749
449 2643 None 52 Rat Binding pKi = 7.8 7.8 -9 9
UnclassifiedUnclassified
Guide to Pharmacology 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 12954362
453 2643 None 52 Rat Binding pKi = 7.8 7.8 -9 9
UnclassifiedUnclassified
Guide to Pharmacology 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10737749
453 2643 None 52 Rat Binding pKi = 7.8 7.8 -9 9
UnclassifiedUnclassified
Guide to Pharmacology 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 12954362
6603931 2643 None 52 Rat Binding pKi = 7.8 7.8 -9 9
UnclassifiedUnclassified
Guide to Pharmacology 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10737749
6603931 2643 None 52 Rat Binding pKi = 7.8 7.8 -9 9
UnclassifiedUnclassified
Guide to Pharmacology 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 12954362
CHEMBL273807 2643 None 52 Rat Binding pKi = 7.8 7.8 -9 9
UnclassifiedUnclassified
Guide to Pharmacology 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10737749
CHEMBL273807 2643 None 52 Rat Binding pKi = 7.8 7.8 -9 9
UnclassifiedUnclassified
Guide to Pharmacology 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 12954362
404 4098 None 33 Human Binding pKi = 7.9 7.9 -154 11
UnclassifiedUnclassified
Guide to Pharmacology 428 10 3 8 0.8 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)NCCN 10496952
404 4098 None 33 Human Binding pKi = 7.9 7.9 -154 11
UnclassifiedUnclassified
Guide to Pharmacology 428 10 3 8 0.8 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)NCCN 10624567
404 4098 None 33 Human Binding pKi = 7.9 7.9 -154 11
UnclassifiedUnclassified
Guide to Pharmacology 428 10 3 8 0.8 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)NCCN 11093773
404 4098 None 33 Human Binding pKi = 7.9 7.9 -154 11
UnclassifiedUnclassified
Guide to Pharmacology 428 10 3 8 0.8 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)NCCN 11266650
404 4098 None 33 Human Binding pKi = 7.9 7.9 -154 11
UnclassifiedUnclassified
Guide to Pharmacology 428 10 3 8 0.8 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)NCCN 15194002
404 4098 None 33 Human Binding pKi = 7.9 7.9 -154 11
UnclassifiedUnclassified
Guide to Pharmacology 428 10 3 8 0.8 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)NCCN 9459566
432 4098 None 33 Human Binding pKi = 7.9 7.9 -154 11
UnclassifiedUnclassified
Guide to Pharmacology 428 10 3 8 0.8 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)NCCN 10496952
432 4098 None 33 Human Binding pKi = 7.9 7.9 -154 11
UnclassifiedUnclassified
Guide to Pharmacology 428 10 3 8 0.8 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)NCCN 10624567
432 4098 None 33 Human Binding pKi = 7.9 7.9 -154 11
UnclassifiedUnclassified
Guide to Pharmacology 428 10 3 8 0.8 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)NCCN 11093773
432 4098 None 33 Human Binding pKi = 7.9 7.9 -154 11
UnclassifiedUnclassified
Guide to Pharmacology 428 10 3 8 0.8 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)NCCN 11266650
432 4098 None 33 Human Binding pKi = 7.9 7.9 -154 11
UnclassifiedUnclassified
Guide to Pharmacology 428 10 3 8 0.8 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)NCCN 15194002
432 4098 None 33 Human Binding pKi = 7.9 7.9 -154 11
UnclassifiedUnclassified
Guide to Pharmacology 428 10 3 8 0.8 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)NCCN 9459566
5697 4098 None 33 Human Binding pKi = 7.9 7.9 -154 11
UnclassifiedUnclassified
Guide to Pharmacology 428 10 3 8 0.8 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)NCCN 10496952
5697 4098 None 33 Human Binding pKi = 7.9 7.9 -154 11
UnclassifiedUnclassified
Guide to Pharmacology 428 10 3 8 0.8 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)NCCN 10624567
5697 4098 None 33 Human Binding pKi = 7.9 7.9 -154 11
UnclassifiedUnclassified
Guide to Pharmacology 428 10 3 8 0.8 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)NCCN 11093773
5697 4098 None 33 Human Binding pKi = 7.9 7.9 -154 11
UnclassifiedUnclassified
Guide to Pharmacology 428 10 3 8 0.8 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)NCCN 11266650
5697 4098 None 33 Human Binding pKi = 7.9 7.9 -154 11
UnclassifiedUnclassified
Guide to Pharmacology 428 10 3 8 0.8 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)NCCN 15194002
5697 4098 None 33 Human Binding pKi = 7.9 7.9 -154 11
UnclassifiedUnclassified
Guide to Pharmacology 428 10 3 8 0.8 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)NCCN 9459566
CHEMBL273094 4098 None 33 Human Binding pKi = 7.9 7.9 -154 11
UnclassifiedUnclassified
Guide to Pharmacology 428 10 3 8 0.8 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)NCCN 10496952
CHEMBL273094 4098 None 33 Human Binding pKi = 7.9 7.9 -154 11
UnclassifiedUnclassified
Guide to Pharmacology 428 10 3 8 0.8 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)NCCN 10624567
CHEMBL273094 4098 None 33 Human Binding pKi = 7.9 7.9 -154 11
UnclassifiedUnclassified
Guide to Pharmacology 428 10 3 8 0.8 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)NCCN 11093773
CHEMBL273094 4098 None 33 Human Binding pKi = 7.9 7.9 -154 11
UnclassifiedUnclassified
Guide to Pharmacology 428 10 3 8 0.8 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)NCCN 11266650
CHEMBL273094 4098 None 33 Human Binding pKi = 7.9 7.9 -154 11
UnclassifiedUnclassified
Guide to Pharmacology 428 10 3 8 0.8 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)NCCN 15194002
CHEMBL273094 4098 None 33 Human Binding pKi = 7.9 7.9 -154 11
UnclassifiedUnclassified
Guide to Pharmacology 428 10 3 8 0.8 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)NCCN 9459566
2690 903 None 66 Mouse Binding pKi = 8.0 8.0 -11 9
UnclassifiedUnclassified
Guide to Pharmacology 285 1 1 6 2.8 Clc1ccc2c(c1)c1nc(nn1c(n2)N)c1ccco1 19141710
384 903 None 66 Mouse Binding pKi = 8.0 8.0 -11 9
UnclassifiedUnclassified
Guide to Pharmacology 285 1 1 6 2.8 Clc1ccc2c(c1)c1nc(nn1c(n2)N)c1ccco1 19141710
CHEMBL16687 903 None 66 Mouse Binding pKi = 8.0 8.0 -11 9
UnclassifiedUnclassified
Guide to Pharmacology 285 1 1 6 2.8 Clc1ccc2c(c1)c1nc(nn1c(n2)N)c1ccco1 19141710
24780383 515 None 0 Mouse Binding pKi = 8.1 8.1 -3 8
UnclassifiedUnclassified
Guide to Pharmacology 513 6 1 8 3.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)C1CC1)c1ccc(nc1)N(C(=O)c1ccc(nc1)C(F)(F)F)C 10737749
5616 515 None 0 Mouse Binding pKi = 8.1 8.1 -3 8
UnclassifiedUnclassified
Guide to Pharmacology 513 6 1 8 3.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)C1CC1)c1ccc(nc1)N(C(=O)c1ccc(nc1)C(F)(F)F)C 10737749
11717831 585 None 48 Human Binding pKi = 8.3 8.3 60 5
UnclassifiedUnclassified
Guide to Pharmacology 379 7 2 7 2.4 N#Cc1c(N)nc(c(c1c1ccc(cc1)OCC1CC1)C#N)SCC(=O)N 17353435
3289 585 None 48 Human Binding pKi = 8.3 8.3 60 5
UnclassifiedUnclassified
Guide to Pharmacology 379 7 2 7 2.4 N#Cc1c(N)nc(c(c1c1ccc(cc1)OCC1CC1)C#N)SCC(=O)N 17353435
CHEMBL4202825 585 None 48 Human Binding pKi = 8.3 8.3 60 5
UnclassifiedUnclassified
Guide to Pharmacology 379 7 2 7 2.4 N#Cc1c(N)nc(c(c1c1ccc(cc1)OCC1CC1)C#N)SCC(=O)N 17353435
135484064 2616 None 4 Human Binding pKi = 8.4 8.4 21 4
UnclassifiedUnclassified
Guide to Pharmacology 509 9 2 11 1.9 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)Nc1ccc2c(c1)OCO2 14998332
135484064 2616 None 4 Human Binding pKi = 8.4 8.4 21 4
UnclassifiedUnclassified
Guide to Pharmacology 509 9 2 11 1.9 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)Nc1ccc2c(c1)OCO2 16219300
390 2616 None 4 Human Binding pKi = 8.4 8.4 21 4
UnclassifiedUnclassified
Guide to Pharmacology 509 9 2 11 1.9 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)Nc1ccc2c(c1)OCO2 14998332
390 2616 None 4 Human Binding pKi = 8.4 8.4 21 4
UnclassifiedUnclassified
Guide to Pharmacology 509 9 2 11 1.9 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)Nc1ccc2c(c1)OCO2 16219300
CHEMBL260331 2616 None 4 Human Binding pKi = 8.4 8.4 21 4
UnclassifiedUnclassified
Guide to Pharmacology 509 9 2 11 1.9 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)Nc1ccc2c(c1)OCO2 14998332
CHEMBL260331 2616 None 4 Human Binding pKi = 8.4 8.4 21 4
UnclassifiedUnclassified
Guide to Pharmacology 509 9 2 11 1.9 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)Nc1ccc2c(c1)OCO2 16219300
11223 2077 None 24 Human Binding pKi = 8.5 8.5 -1 4
UnclassifiedUnclassified
Guide to Pharmacology 337 3 1 6 3.9 CC(OC(=O)C1=C(C)Nc2n(C1c1ccco1)c1ccccc1n2)C 26824742
17198004 2077 None 24 Human Binding pKi = 8.5 8.5 -1 4
UnclassifiedUnclassified
Guide to Pharmacology 337 3 1 6 3.9 CC(OC(=O)C1=C(C)Nc2n(C1c1ccco1)c1ccccc1n2)C 26824742
CHEMBL3787197 2077 None 24 Human Binding pKi = 8.5 8.5 -1 4
UnclassifiedUnclassified
Guide to Pharmacology 337 3 1 6 3.9 CC(OC(=O)C1=C(C)Nc2n(C1c1ccco1)c1ccccc1n2)C 26824742
449 2643 None 52 Mouse Binding pKi = 8.5 8.5 -2 9
UnclassifiedUnclassified
Guide to Pharmacology 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 19141710
453 2643 None 52 Mouse Binding pKi = 8.5 8.5 -2 9
UnclassifiedUnclassified
Guide to Pharmacology 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 19141710
6603931 2643 None 52 Mouse Binding pKi = 8.5 8.5 -2 9
UnclassifiedUnclassified
Guide to Pharmacology 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 19141710
CHEMBL273807 2643 None 52 Mouse Binding pKi = 8.5 8.5 -2 9
UnclassifiedUnclassified
Guide to Pharmacology 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 19141710
24780383 515 None 0 Human Binding pKi = 8.6 8.6 3 8
UnclassifiedUnclassified
Guide to Pharmacology 513 6 1 8 3.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)C1CC1)c1ccc(nc1)N(C(=O)c1ccc(nc1)C(F)(F)F)C 10737749
5616 515 None 0 Human Binding pKi = 8.6 8.6 3 8
UnclassifiedUnclassified
Guide to Pharmacology 513 6 1 8 3.4 CCCn1c2nc([nH]c2c(=O)n(c1=O)C1CC1)c1ccc(nc1)N(C(=O)c1ccc(nc1)C(F)(F)F)C 10737749
449 2643 None 52 Human Binding pKi = 8.8 8.8 -1 9
UnclassifiedUnclassified
Guide to Pharmacology 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10737749
449 2643 None 52 Human Binding pKi = 8.8 8.8 -1 9
UnclassifiedUnclassified
Guide to Pharmacology 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 11266650
453 2643 None 52 Human Binding pKi = 8.8 8.8 -1 9
UnclassifiedUnclassified
Guide to Pharmacology 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10737749
453 2643 None 52 Human Binding pKi = 8.8 8.8 -1 9
UnclassifiedUnclassified
Guide to Pharmacology 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 11266650
6603931 2643 None 52 Human Binding pKi = 8.8 8.8 -1 9
UnclassifiedUnclassified
Guide to Pharmacology 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10737749
6603931 2643 None 52 Human Binding pKi = 8.8 8.8 -1 9
UnclassifiedUnclassified
Guide to Pharmacology 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 11266650
CHEMBL273807 2643 None 52 Human Binding pKi = 8.8 8.8 -1 9
UnclassifiedUnclassified
Guide to Pharmacology 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 10737749
CHEMBL273807 2643 None 52 Human Binding pKi = 8.8 8.8 -1 9
UnclassifiedUnclassified
Guide to Pharmacology 486 9 2 8 3.3 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)Nc1ccc(cc1)C#N 11266650
3284 3216 None 35 Human Binding pKi = 9.3 9.3 -1 7
UnclassifiedUnclassified
Guide to Pharmacology 528 6 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)c1ccc(cc1)Cl 19569717
44185871 3216 None 35 Human Binding pKi = 9.3 9.3 -1 7
UnclassifiedUnclassified
Guide to Pharmacology 528 6 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)c1ccc(cc1)Cl 19569717
5728 3216 None 35 Human Binding pKi = 9.3 9.3 -1 7
UnclassifiedUnclassified
Guide to Pharmacology 528 6 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)c1ccc(cc1)Cl 19569717
CHEMBL483688 3216 None 35 Human Binding pKi = 9.3 9.3 -1 7
UnclassifiedUnclassified
Guide to Pharmacology 528 6 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)c1ccc(cc1)Cl 19569717
44186581 3205 None 27 Human Binding pKi = 9.4 9.4 851 6
UnclassifiedUnclassified
Guide to Pharmacology 542 7 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)Cc1ccc(cc1)Cl 19569717
6561 3205 None 27 Human Binding pKi = 9.4 9.4 851 6
UnclassifiedUnclassified
Guide to Pharmacology 542 7 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)Cc1ccc(cc1)Cl 19569717
CHEMBL482436 3205 None 27 Human Binding pKi = 9.4 9.4 851 6
UnclassifiedUnclassified
Guide to Pharmacology 542 7 2 7 2.7 CCCn1c(=O)[nH]c2c(c1=O)[nH]c(n2)c1ccc(cc1)S(=O)(=O)N1CCN(CC1)Cc1ccc(cc1)Cl 19569717
11561692 1869 None 14 Human Binding pKi > 4.3 4.3 -239 4
UnclassifiedUnclassified
Guide to Pharmacology 461 6 4 10 1.7 O[C@@H]1[C@H](O)[C@H](O[C@H]1n1cnc2c1ncnc2N[C@@H]1CCC[C@H]1O)CSc1ccccc1F 19012505
5593 1869 None 14 Human Binding pKi > 4.3 4.3 -239 4
UnclassifiedUnclassified
Guide to Pharmacology 461 6 4 10 1.7 O[C@@H]1[C@H](O)[C@H](O[C@H]1n1cnc2c1ncnc2N[C@@H]1CCC[C@H]1O)CSc1ccccc1F 19012505
CHEMBL3545011 1869 None 14 Human Binding pKi > 4.3 4.3 -239 4
UnclassifiedUnclassified
Guide to Pharmacology 461 6 4 10 1.7 O[C@@H]1[C@H](O)[C@H](O[C@H]1n1cnc2c1ncnc2N[C@@H]1CCC[C@H]1O)CSc1ccccc1F 19012505
10981286 1919 None 30 Human Binding pKi > 4.5 4.5 -28183 4
UnclassifiedUnclassified
Guide to Pharmacology 361 5 4 9 0.0 CCCCC#Cc1nc(NC)c2c(n1)n(cn2)[C@@H]1O[C@@H]([C@H]([C@H]1O)O)CO 12109910
10981286 1919 None 30 Human Binding pKi > 4.5 4.5 -28183 4
UnclassifiedUnclassified
Guide to Pharmacology 361 5 4 9 0.0 CCCCC#Cc1nc(NC)c2c(n1)n(cn2)[C@@H]1O[C@@H]([C@H]([C@H]1O)O)CO 17126322
5599 1919 None 30 Human Binding pKi > 4.5 4.5 -28183 4
UnclassifiedUnclassified
Guide to Pharmacology 361 5 4 9 0.0 CCCCC#Cc1nc(NC)c2c(n1)n(cn2)[C@@H]1O[C@@H]([C@H]([C@H]1O)O)CO 12109910
5599 1919 None 30 Human Binding pKi > 4.5 4.5 -28183 4
UnclassifiedUnclassified
Guide to Pharmacology 361 5 4 9 0.0 CCCCC#Cc1nc(NC)c2c(n1)n(cn2)[C@@H]1O[C@@H]([C@H]([C@H]1O)O)CO 17126322
5736 1919 None 30 Human Binding pKi > 4.5 4.5 -28183 4
UnclassifiedUnclassified
Guide to Pharmacology 361 5 4 9 0.0 CCCCC#Cc1nc(NC)c2c(n1)n(cn2)[C@@H]1O[C@@H]([C@H]([C@H]1O)O)CO 12109910
5736 1919 None 30 Human Binding pKi > 4.5 4.5 -28183 4
UnclassifiedUnclassified
Guide to Pharmacology 361 5 4 9 0.0 CCCCC#Cc1nc(NC)c2c(n1)n(cn2)[C@@H]1O[C@@H]([C@H]([C@H]1O)O)CO 17126322
CHEMBL260563 1919 None 30 Human Binding pKi > 4.5 4.5 -28183 4
UnclassifiedUnclassified
Guide to Pharmacology 361 5 4 9 0.0 CCCCC#Cc1nc(NC)c2c(n1)n(cn2)[C@@H]1O[C@@H]([C@H]([C@H]1O)O)CO 12109910
CHEMBL260563 1919 None 30 Human Binding pKi > 4.5 4.5 -28183 4
UnclassifiedUnclassified
Guide to Pharmacology 361 5 4 9 0.0 CCCCC#Cc1nc(NC)c2c(n1)n(cn2)[C@@H]1O[C@@H]([C@H]([C@H]1O)O)CO 17126322
3086599 904 None 45 Rat Binding pKi > 5 5.0 -575 8
UnclassifiedUnclassified
Guide to Pharmacology 499 10 6 11 -0.2 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(NCCc1ccc(cc1)CCC(=O)O)nc2N None
375 904 None 45 Rat Binding pKi > 5 5.0 -575 8
UnclassifiedUnclassified
Guide to Pharmacology 499 10 6 11 -0.2 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(NCCc1ccc(cc1)CCC(=O)O)nc2N None
424 904 None 45 Rat Binding pKi > 5 5.0 -575 8
UnclassifiedUnclassified
Guide to Pharmacology 499 10 6 11 -0.2 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(NCCc1ccc(cc1)CCC(=O)O)nc2N None
CHEMBL331372 904 None 45 Rat Binding pKi > 5 5.0 -575 8
UnclassifiedUnclassified
Guide to Pharmacology 499 10 6 11 -0.2 CCNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(NCCc1ccc(cc1)CCC(=O)O)nc2N None
3035850 951 None 73 Human Binding pKi > 5 5.0 -54954 14
UnclassifiedUnclassified
Guide to Pharmacology 544 5 4 9 1.1 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NCc1cccc(c1)I None
3035850 951 None 73 Mouse Binding pKi > 5 5.0 -54954 14
UnclassifiedUnclassified
Guide to Pharmacology 544 5 4 9 1.1 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NCc1cccc(c1)I None
3035850.0 951 None 73 Human Binding pKi > 5 5.0 -54954 14
UnclassifiedUnclassified
Guide to Pharmacology 544 5 4 9 1.1 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NCc1cccc(c1)I None
3035850.0 951 None 73 Mouse Binding pKi > 5 5.0 -54954 14
UnclassifiedUnclassified
Guide to Pharmacology 544 5 4 9 1.1 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NCc1cccc(c1)I None
457 951 None 73 Human Binding pKi > 5 5.0 -54954 14
UnclassifiedUnclassified
Guide to Pharmacology 544 5 4 9 1.1 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NCc1cccc(c1)I None
457 951 None 73 Mouse Binding pKi > 5 5.0 -54954 14
UnclassifiedUnclassified
Guide to Pharmacology 544 5 4 9 1.1 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NCc1cccc(c1)I None
CHEMBL431733 951 None 73 Human Binding pKi > 5 5.0 -54954 14
UnclassifiedUnclassified
Guide to Pharmacology 544 5 4 9 1.1 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NCc1cccc(c1)I None
CHEMBL431733 951 None 73 Mouse Binding pKi > 5 5.0 -54954 14
UnclassifiedUnclassified
Guide to Pharmacology 544 5 4 9 1.1 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NCc1cccc(c1)I None
DB12885 951 None 73 Human Binding pKi > 5 5.0 -54954 14
UnclassifiedUnclassified
Guide to Pharmacology 544 5 4 9 1.1 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NCc1cccc(c1)I None
DB12885 951 None 73 Mouse Binding pKi > 5 5.0 -54954 14
UnclassifiedUnclassified
Guide to Pharmacology 544 5 4 9 1.1 CNC(=O)[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NCc1cccc(c1)I None
4882 2099 None 82 Human Binding pKi > 5 5.0 -104 6
UnclassifiedUnclassified
Guide to Pharmacology 384 6 0 8 2.1 COc1cc(/C=C/c2nc3c(n2C)c(=O)n(c(=O)n3CC)CC)ccc1OC 21303899
5311037 2099 None 82 Human Binding pKi > 5 5.0 -104 6
UnclassifiedUnclassified
Guide to Pharmacology 384 6 0 8 2.1 COc1cc(/C=C/c2nc3c(n2C)c(=O)n(c(=O)n3CC)CC)ccc1OC 21303899
5311037.0 2099 None 82 Human Binding pKi > 5 5.0 -104 6
UnclassifiedUnclassified
Guide to Pharmacology 384 6 0 8 2.1 COc1cc(/C=C/c2nc3c(n2C)c(=O)n(c(=O)n3CC)CC)ccc1OC 21303899
5608 2099 None 82 Human Binding pKi > 5 5.0 -104 6
UnclassifiedUnclassified
Guide to Pharmacology 384 6 0 8 2.1 COc1cc(/C=C/c2nc3c(n2C)c(=O)n(c(=O)n3CC)CC)ccc1OC 21303899
CHEMBL431770 2099 None 82 Human Binding pKi > 5 5.0 -104 6
UnclassifiedUnclassified
Guide to Pharmacology 384 6 0 8 2.1 COc1cc(/C=C/c2nc3c(n2C)c(=O)n(c(=O)n3CC)CC)ccc1OC 21303899
DB11757 2099 None 82 Human Binding pKi > 5 5.0 -104 6
UnclassifiedUnclassified
Guide to Pharmacology 384 6 0 8 2.1 COc1cc(/C=C/c2nc3c(n2C)c(=O)n(c(=O)n3CC)CC)ccc1OC 21303899
393594 2636 None 42 Human Binding pKi > 5 5.0 -354 7
UnclassifiedUnclassified
Guide to Pharmacology 477 6 1 5 5.2 CCOC(=O)C1=C(C)NC(=C(C1C#Cc1ccccc1)C(=O)OCc1ccccc1)c1ccccc1 None
470 2636 None 42 Human Binding pKi > 5 5.0 -354 7
UnclassifiedUnclassified
Guide to Pharmacology 477 6 1 5 5.2 CCOC(=O)C1=C(C)NC(=C(C1C#Cc1ccccc1)C(=O)OCc1ccccc1)c1ccccc1 None
CHEMBL1995014 2636 None 42 Human Binding pKi > 5 5.0 -354 7
UnclassifiedUnclassified
Guide to Pharmacology 477 6 1 5 5.2 CCOC(=O)C1=C(C)NC(=C(C1C#Cc1ccccc1)C(=O)OCc1ccccc1)c1ccccc1 None
CHEMBL89852 2636 None 42 Human Binding pKi > 5 5.0 -354 7
UnclassifiedUnclassified
Guide to Pharmacology 477 6 1 5 5.2 CCOC(=O)C1=C(C)NC(=C(C1C#Cc1ccccc1)C(=O)OCc1ccccc1)c1ccccc1 None
3661570 2641 None 53 Human Binding pKi > 5 5.0 -102 9
UnclassifiedUnclassified
Guide to Pharmacology 399 9 0 5 5.7 CCCOC(=O)c1c(CCC)c(C(=O)SCC)c(nc1c1ccccc1)CC None
3661570 2641 None 53 Mouse Binding pKi > 5 5.0 -102 9
UnclassifiedUnclassified
Guide to Pharmacology 399 9 0 5 5.7 CCCOC(=O)c1c(CCC)c(C(=O)SCC)c(nc1c1ccccc1)CC None
474 2641 None 53 Human Binding pKi > 5 5.0 -102 9
UnclassifiedUnclassified
Guide to Pharmacology 399 9 0 5 5.7 CCCOC(=O)c1c(CCC)c(C(=O)SCC)c(nc1c1ccccc1)CC None
474 2641 None 53 Mouse Binding pKi > 5 5.0 -102 9
UnclassifiedUnclassified
Guide to Pharmacology 399 9 0 5 5.7 CCCOC(=O)c1c(CCC)c(C(=O)SCC)c(nc1c1ccccc1)CC None
CHEMBL111545 2641 None 53 Human Binding pKi > 5 5.0 -102 9
UnclassifiedUnclassified
Guide to Pharmacology 399 9 0 5 5.7 CCCOC(=O)c1c(CCC)c(C(=O)SCC)c(nc1c1ccccc1)CC None
CHEMBL111545 2641 None 53 Mouse Binding pKi > 5 5.0 -102 9
UnclassifiedUnclassified
Guide to Pharmacology 399 9 0 5 5.7 CCCOC(=O)c1c(CCC)c(C(=O)SCC)c(nc1c1ccccc1)CC None
11248240 2664 None 4 Human Binding pKi > 5 5.0 -34673 10
UnclassifiedUnclassified
Guide to Pharmacology 462 5 4 8 1.8 CNC(=O)[C@]12C[C@@H]2[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NCc1cccc(c1)Cl 16518376
5601 2664 None 4 Human Binding pKi > 5 5.0 -34673 10
UnclassifiedUnclassified
Guide to Pharmacology 462 5 4 8 1.8 CNC(=O)[C@]12C[C@@H]2[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NCc1cccc(c1)Cl 16518376
CHEMBL175543 2664 None 4 Human Binding pKi > 5 5.0 -34673 10
UnclassifiedUnclassified
Guide to Pharmacology 462 5 4 8 1.8 CNC(=O)[C@]12C[C@@H]2[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(Cl)nc2NCc1cccc(c1)Cl 16518376
219024 3300 None 65 Human Binding pKi > 5 5.0 -229 5
UnclassifiedUnclassified
Guide to Pharmacology 390 4 5 12 -2.4 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(nc2N)n1ncc(c1)C(=O)NC 16518376
219024.0 3300 None 65 Human Binding pKi > 5 5.0 -229 5
UnclassifiedUnclassified
Guide to Pharmacology 390 4 5 12 -2.4 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(nc2N)n1ncc(c1)C(=O)NC 16518376
2362 3300 None 65 Human Binding pKi > 5 5.0 -229 5
UnclassifiedUnclassified
Guide to Pharmacology 390 4 5 12 -2.4 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(nc2N)n1ncc(c1)C(=O)NC 16518376
5596 3300 None 65 Human Binding pKi > 5 5.0 -229 5
UnclassifiedUnclassified
Guide to Pharmacology 390 4 5 12 -2.4 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(nc2N)n1ncc(c1)C(=O)NC 16518376
CHEMBL317052 3300 None 65 Human Binding pKi > 5 5.0 -229 5
UnclassifiedUnclassified
Guide to Pharmacology 390 4 5 12 -2.4 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(nc2N)n1ncc(c1)C(=O)NC 16518376
DB06213 3300 None 65 Human Binding pKi > 5 5.0 -229 5
UnclassifiedUnclassified
Guide to Pharmacology 390 4 5 12 -2.4 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(nc2N)n1ncc(c1)C(=O)NC 16518376
10668061 3553 None 70 Human Binding pKi > 5 5.0 -64565 6
UnclassifiedUnclassified
Guide to Pharmacology 389 6 1 9 3.0 COc1ccc(cc1)CCCn1ncc2c1nc(N)n1c2nc(n1)c1ccco1 16518376
3283 3553 None 70 Human Binding pKi > 5 5.0 -64565 6
UnclassifiedUnclassified
Guide to Pharmacology 389 6 1 9 3.0 COc1ccc(cc1)CCCn1ncc2c1nc(N)n1c2nc(n1)c1ccco1 16518376
CHEMBL136689 3553 None 70 Human Binding pKi > 5 5.0 -64565 6
UnclassifiedUnclassified
Guide to Pharmacology 389 6 1 9 3.0 COc1ccc(cc1)CCCn1ncc2c1nc(N)n1c2nc(n1)c1ccco1 16518376
135546224 3765 None 0 Human Binding pKi > 5 5.0 -3548 4
UnclassifiedUnclassified
Guide to Pharmacology 497 7 6 11 1.8 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(N/N=N/C(=O)Nc1ccccc1)nc2NC1CCCC1 9384502
136218973 3765 None 0 Human Binding pKi > 5 5.0 -3548 4
UnclassifiedUnclassified
Guide to Pharmacology 497 7 6 11 1.8 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(N/N=N/C(=O)Nc1ccccc1)nc2NC1CCCC1 9384502
5590 3765 None 0 Human Binding pKi > 5 5.0 -3548 4
UnclassifiedUnclassified
Guide to Pharmacology 497 7 6 11 1.8 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(N/N=N/C(=O)Nc1ccccc1)nc2NC1CCCC1 9384502
CHEMBL2113457 3765 None 0 Human Binding pKi > 5 5.0 -3548 4
UnclassifiedUnclassified
Guide to Pharmacology 497 7 6 11 1.8 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(N/N=N/C(=O)Nc1ccccc1)nc2NC1CCCC1 9384502
10117987 3164 None 84 Human Binding pKi > 6 6.0 -1047 6
UnclassifiedUnclassified
Guide to Pharmacology 503 9 1 12 2.2 COCCOc1ccc(cc1)N1CCN(CC1)CCn1ncc2c1nc(N)n1c2nc(n1)c1ccco1 18221214
5614 3164 None 84 Human Binding pKi > 6 6.0 -1047 6
UnclassifiedUnclassified
Guide to Pharmacology 503 9 1 12 2.2 COCCOc1ccc(cc1)N1CCN(CC1)CCn1ncc2c1nc(N)n1c2nc(n1)c1ccco1 18221214
CHEMBL240624 3164 None 84 Human Binding pKi > 6 6.0 -1047 6
UnclassifiedUnclassified
Guide to Pharmacology 503 9 1 12 2.2 COCCOc1ccc(cc1)N1CCN(CC1)CCn1ncc2c1nc(N)n1c2nc(n1)c1ccco1 18221214
DB11864 3164 None 84 Human Binding pKi > 6 6.0 -1047 6
UnclassifiedUnclassified
Guide to Pharmacology 503 9 1 12 2.2 COCCOc1ccc(cc1)N1CCN(CC1)CCn1ncc2c1nc(N)n1c2nc(n1)c1ccco1 18221214
16109435 2379 None 10 Human Binding pKi > 6.5 6.5 -338 4
UnclassifiedUnclassified
Guide to Pharmacology 353 3 1 2 6.3 C1CCC(CC1)c1nc2c([nH]1)nc(cc2c1ccccc1)c1ccccc1 14663020
5607 2379 None 10 Human Binding pKi > 6.5 6.5 -338 4
UnclassifiedUnclassified
Guide to Pharmacology 353 3 1 2 6.3 C1CCC(CC1)c1nc2c([nH]1)nc(cc2c1ccccc1)c1ccccc1 14663020
CHEMBL219160 2379 None 10 Human Binding pKi > 6.5 6.5 -338 4
UnclassifiedUnclassified
Guide to Pharmacology 353 3 1 2 6.3 C1CCC(CC1)c1nc2c([nH]1)nc(cc2c1ccccc1)c1ccccc1 14663020
415 3651 None 12 Human Binding pKi None 4.7 4.7 -1905 9
UnclassifiedUnclassified
Guide to Pharmacology 385 6 4 9 0.5 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N[C@H](Cc1ccccc1)C 10496952
415 3651 None 12 Human Binding pKi None 4.7 4.7 -1905 9
UnclassifiedUnclassified
Guide to Pharmacology 385 6 4 9 0.5 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N[C@H](Cc1ccccc1)C 16219300
5312112 3651 None 12 Human Binding pKi None 4.7 4.7 -1905 9
UnclassifiedUnclassified
Guide to Pharmacology 385 6 4 9 0.5 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N[C@H](Cc1ccccc1)C 10496952
5312112 3651 None 12 Human Binding pKi None 4.7 4.7 -1905 9
UnclassifiedUnclassified
Guide to Pharmacology 385 6 4 9 0.5 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N[C@H](Cc1ccccc1)C 16219300
CHEMBL420705 3651 None 12 Human Binding pKi None 4.7 4.7 -1905 9
UnclassifiedUnclassified
Guide to Pharmacology 385 6 4 9 0.5 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N[C@H](Cc1ccccc1)C 10496952
CHEMBL420705 3651 None 12 Human Binding pKi None 4.7 4.7 -1905 9
UnclassifiedUnclassified
Guide to Pharmacology 385 6 4 9 0.5 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1ncnc2N[C@H](Cc1ccccc1)C 16219300
434 223 None 0 Human Binding pKi None 4.7 4.7 - 1
UnclassifiedUnclassified
Guide to Pharmacology 457 6 6 11 -0.7 CCNC(=O)C(=O)Nc1nc(Nc2ccccc2)c2c(n1)n(cn2)[C@@H]1O[C@@H]([C@H]([C@H]1O)O)CO 10496952
57340157 223 None 0 Human Binding pKi None 4.7 4.7 - 1
UnclassifiedUnclassified
Guide to Pharmacology 457 6 6 11 -0.7 CCNC(=O)C(=O)Nc1nc(Nc2ccccc2)c2c(n1)n(cn2)[C@@H]1O[C@@H]([C@H]([C@H]1O)O)CO 10496952
456 349 None 59 Human Binding pKi None 6 6.0 15 3
UnclassifiedUnclassified
Guide to Pharmacology 214 0 2 4 0.2 O=c1[nH]c2nc3ccccc3nc2c(=O)[nH]1 10624567
456 349 None 59 Human Binding pKi None 6 6.0 15 3
UnclassifiedUnclassified
Guide to Pharmacology 214 0 2 4 0.2 O=c1[nH]c2nc3ccccc3nc2c(=O)[nH]1 11266650
5372720 349 None 59 Human Binding pKi None 6 6.0 15 3
UnclassifiedUnclassified
Guide to Pharmacology 214 0 2 4 0.2 O=c1[nH]c2nc3ccccc3nc2c(=O)[nH]1 10624567
5372720 349 None 59 Human Binding pKi None 6 6.0 15 3
UnclassifiedUnclassified
Guide to Pharmacology 214 0 2 4 0.2 O=c1[nH]c2nc3ccccc3nc2c(=O)[nH]1 11266650
CHEMBL68500 349 None 59 Human Binding pKi None 6 6.0 15 3
UnclassifiedUnclassified
Guide to Pharmacology 214 0 2 4 0.2 O=c1[nH]c2nc3ccccc3nc2c(=O)[nH]1 10624567
CHEMBL68500 349 None 59 Human Binding pKi None 6 6.0 15 3
UnclassifiedUnclassified
Guide to Pharmacology 214 0 2 4 0.2 O=c1[nH]c2nc3ccccc3nc2c(=O)[nH]1 11266650
10221256 104 None 0 Human Binding pKi None 6.3 6.3 - 1
UnclassifiedUnclassified
Guide to Pharmacology 277 3 2 5 0.7 CC(Cn1c(=O)[nH]c(=O)c2c1nc([nH]2)N1CCCC1)C 11705449
447 104 None 0 Human Binding pKi None 6.3 6.3 - 1
UnclassifiedUnclassified
Guide to Pharmacology 277 3 2 5 0.7 CC(Cn1c(=O)[nH]c(=O)c2c1nc([nH]2)N1CCCC1)C 11705449
444 1333 None 0 Human Binding pKi None 6.4 6.4 - 1
UnclassifiedUnclassified
Guide to Pharmacology 314 5 1 5 2.3 C=CCn1c2nc([nH]c2c(=O)n(c1=O)CC=C)C1CCCCC1 11266650
9926882 1333 None 0 Human Binding pKi None 6.4 6.4 - 1
UnclassifiedUnclassified
Guide to Pharmacology 314 5 1 5 2.3 C=CCn1c2nc([nH]c2c(=O)n(c1=O)CC=C)C1CCCCC1 11266650
393595 2637 None 51 Human Binding pKi None 6.5 6.5 -97 6
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 6 4.4 O=C(Nc1nc2ccc(cc2c2n1nc(n2)c1ccco1)Cl)Cc1ccccc1 15194002
448 2637 None 51 Human Binding pKi None 6.5 6.5 -97 6
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 6 4.4 O=C(Nc1nc2ccc(cc2c2n1nc(n2)c1ccco1)Cl)Cc1ccccc1 15194002
CHEMBL88147 2637 None 51 Human Binding pKi None 6.5 6.5 -97 6
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 6 4.4 O=C(Nc1nc2ccc(cc2c2n1nc(n2)c1ccco1)Cl)Cc1ccccc1 15194002
164437 64 None 24 Human Binding pKi None 6.6 6.6 -114 7
UnclassifiedUnclassified
Guide to Pharmacology 388 5 4 9 -0.3 CCCCC#Cc1nc(N)c2c(n1)n(cn2)[C@@H]1O[C@@H]([C@H]([C@H]1O)O)C(=O)NCC 16219300
373 64 None 24 Human Binding pKi None 6.6 6.6 -114 7
UnclassifiedUnclassified
Guide to Pharmacology 388 5 4 9 -0.3 CCCCC#Cc1nc(N)c2c(n1)n(cn2)[C@@H]1O[C@@H]([C@H]([C@H]1O)O)C(=O)NCC 16219300
CHEMBL410873 64 None 24 Human Binding pKi None 6.6 6.6 -114 7
UnclassifiedUnclassified
Guide to Pharmacology 388 5 4 9 -0.3 CCCCC#Cc1nc(N)c2c(n1)n(cn2)[C@@H]1O[C@@H]([C@H]([C@H]1O)O)C(=O)NCC 16219300
443 755 None 10 Human Binding pKi None 7.3 7.3 -3 7
UnclassifiedUnclassified
Guide to Pharmacology 382 7 2 6 2.5 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)/C=C/C(=O)O 10496952
6439089 755 None 10 Human Binding pKi None 7.3 7.3 -3 7
UnclassifiedUnclassified
Guide to Pharmacology 382 7 2 6 2.5 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)/C=C/C(=O)O 10496952
CHEMBL16997 755 None 10 Human Binding pKi None 7.3 7.3 -3 7
UnclassifiedUnclassified
Guide to Pharmacology 382 7 2 6 2.5 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)/C=C/C(=O)O 10496952
169317 1201 None 38 Human Binding pKi None 7.3 7.3 -44 9
UnclassifiedUnclassified
Guide to Pharmacology 236 4 1 5 0.7 CCCn1c(=O)n(CCC)c2c(c1=O)[nH]cn2 10496952
169317 1201 None 38 Human Binding pKi None 7.3 7.3 -44 9
UnclassifiedUnclassified
Guide to Pharmacology 236 4 1 5 0.7 CCCn1c(=O)n(CCC)c2c(c1=O)[nH]cn2 11266650
427 1201 None 38 Human Binding pKi None 7.3 7.3 -44 9
UnclassifiedUnclassified
Guide to Pharmacology 236 4 1 5 0.7 CCCn1c(=O)n(CCC)c2c(c1=O)[nH]cn2 10496952
427 1201 None 38 Human Binding pKi None 7.3 7.3 -44 9
UnclassifiedUnclassified
Guide to Pharmacology 236 4 1 5 0.7 CCCn1c(=O)n(CCC)c2c(c1=O)[nH]cn2 11266650
CHEMBL157655 1201 None 38 Human Binding pKi None 7.3 7.3 -44 9
UnclassifiedUnclassified
Guide to Pharmacology 236 4 1 5 0.7 CCCn1c(=O)n(CCC)c2c(c1=O)[nH]cn2 10496952
CHEMBL157655 1201 None 38 Human Binding pKi None 7.3 7.3 -44 9
UnclassifiedUnclassified
Guide to Pharmacology 236 4 1 5 0.7 CCCn1c(=O)n(CCC)c2c(c1=O)[nH]cn2 11266650
126079 4100 None 31 Human Binding pKi None 7.3 7.3 -2 8
UnclassifiedUnclassified
Guide to Pharmacology 386 8 2 7 1.8 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)O 11266650
451 4100 None 31 Human Binding pKi None 7.3 7.3 -2 8
UnclassifiedUnclassified
Guide to Pharmacology 386 8 2 7 1.8 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)O 11266650
CHEMBL27041 4100 None 31 Human Binding pKi None 7.3 7.3 -2 8
UnclassifiedUnclassified
Guide to Pharmacology 386 8 2 7 1.8 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1ccc(cc1)OCC(=O)O 11266650
163889 1964 None 17 Human Binding pKi None 7.4 7.4 -6 8
UnclassifiedUnclassified
Guide to Pharmacology 575 8 3 8 2.7 CCCn1c(=O)c2[nH]c(nc2n(c1=O)Cc1ccc(c(c1)I)N)c1ccc(cc1)OCC(=O)O 10496952
446 1964 None 17 Human Binding pKi None 7.4 7.4 -6 8
UnclassifiedUnclassified
Guide to Pharmacology 575 8 3 8 2.7 CCCn1c(=O)c2[nH]c(nc2n(c1=O)Cc1ccc(c(c1)I)N)c1ccc(cc1)OCC(=O)O 10496952
CHEMBL355370 1964 None 17 Human Binding pKi None 7.4 7.4 -6 8
UnclassifiedUnclassified
Guide to Pharmacology 575 8 3 8 2.7 CCCn1c(=O)c2[nH]c(nc2n(c1=O)Cc1ccc(c(c1)I)N)c1ccc(cc1)OCC(=O)O 10496952
176407 4148 None 84 Human Binding pKi None 7.5 7.5 -34 6
UnclassifiedUnclassified
Guide to Pharmacology 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10496952
176407 4148 None 84 Human Binding pKi None 7.5 7.5 -34 6
UnclassifiedUnclassified
Guide to Pharmacology 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 11093773
176407 4148 None 84 Human Binding pKi None 7.5 7.5 -34 6
UnclassifiedUnclassified
Guide to Pharmacology 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 11266650
176407 4148 None 84 Human Binding pKi None 7.5 7.5 -34 6
UnclassifiedUnclassified
Guide to Pharmacology 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 15194002
405 4148 None 84 Human Binding pKi None 7.5 7.5 -34 6
UnclassifiedUnclassified
Guide to Pharmacology 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10496952
405 4148 None 84 Human Binding pKi None 7.5 7.5 -34 6
UnclassifiedUnclassified
Guide to Pharmacology 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 11093773
405 4148 None 84 Human Binding pKi None 7.5 7.5 -34 6
UnclassifiedUnclassified
Guide to Pharmacology 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 11266650
405 4148 None 84 Human Binding pKi None 7.5 7.5 -34 6
UnclassifiedUnclassified
Guide to Pharmacology 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 15194002
CHEMBL113142 4148 None 84 Human Binding pKi None 7.5 7.5 -34 6
UnclassifiedUnclassified
Guide to Pharmacology 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10496952
CHEMBL113142 4148 None 84 Human Binding pKi None 7.5 7.5 -34 6
UnclassifiedUnclassified
Guide to Pharmacology 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 11093773
CHEMBL113142 4148 None 84 Human Binding pKi None 7.5 7.5 -34 6
UnclassifiedUnclassified
Guide to Pharmacology 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 11266650
CHEMBL113142 4148 None 84 Human Binding pKi None 7.5 7.5 -34 6
UnclassifiedUnclassified
Guide to Pharmacology 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 15194002
DB08770 4148 None 84 Human Binding pKi None 7.5 7.5 -34 6
UnclassifiedUnclassified
Guide to Pharmacology 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 10496952
DB08770 4148 None 84 Human Binding pKi None 7.5 7.5 -34 6
UnclassifiedUnclassified
Guide to Pharmacology 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 11093773
DB08770 4148 None 84 Human Binding pKi None 7.5 7.5 -34 6
UnclassifiedUnclassified
Guide to Pharmacology 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 11266650
DB08770 4148 None 84 Human Binding pKi None 7.5 7.5 -34 6
UnclassifiedUnclassified
Guide to Pharmacology 337 5 3 9 1.7 Oc1ccc(cc1)CCNc1nc(N)n2c(n1)nc(n2)c1ccco1 15194002
135465785 488 None 0 Human Binding pKi None 7.6 7.6 - 1
UnclassifiedUnclassified
Guide to Pharmacology 496 8 2 12 0.0 CCCn1c2=N/C(=c/3\o[nH]c(c3)OCC(=O)Nc3ccc4c(c3)OCO4)/N=c2c(=O)n(c1=O)CCC 16219300
439 488 None 0 Human Binding pKi None 7.6 7.6 - 1
UnclassifiedUnclassified
Guide to Pharmacology 496 8 2 12 0.0 CCCn1c2=N/C(=c/3\o[nH]c(c3)OCC(=O)Nc3ccc4c(c3)OCO4)/N=c2c(=O)n(c1=O)CCC 16219300
CHEMBL32582 488 None 0 Human Binding pKi None 7.6 7.6 - 1
UnclassifiedUnclassified
Guide to Pharmacology 496 8 2 12 0.0 CCCn1c2=N/C(=c/3\o[nH]c(c3)OCC(=O)Nc3ccc4c(c3)OCO4)/N=c2c(=O)n(c1=O)CCC 16219300
135529391 481 None 0 Human Binding pKi None 7.7 7.7 - 1
UnclassifiedUnclassified
Guide to Pharmacology 555 10 2 10 1.5 CCCn1c2=N/C(=c\3/cc([nH]n3C)NC(=O)Cc3ccc(cc3)OCc3ccccc3)/N=c2c(=O)n(c1=O)CCC 16219300
438 481 None 0 Human Binding pKi None 7.7 7.7 - 1
UnclassifiedUnclassified
Guide to Pharmacology 555 10 2 10 1.5 CCCn1c2=N/C(=c\3/cc([nH]n3C)NC(=O)Cc3ccc(cc3)OCc3ccccc3)/N=c2c(=O)n(c1=O)CCC 16219300
CHEMBL285900 481 None 0 Human Binding pKi None 7.7 7.7 - 1
UnclassifiedUnclassified
Guide to Pharmacology 555 10 2 10 1.5 CCCn1c2=N/C(=c\3/cc([nH]n3C)NC(=O)Cc3ccc(cc3)OCc3ccccc3)/N=c2c(=O)n(c1=O)CCC 16219300
135443359 490 None 0 Human Binding pKi None 7.7 7.7 - 1
UnclassifiedUnclassified
Guide to Pharmacology 509 9 3 11 -0.1 CCCn1c2=N/C(=c\3/cc([nH]n3C)OCC(=O)Nc3ccc(cc3)C(=O)O)/N=c2c(=O)n(c1=O)CCC 16219300
441 490 None 0 Human Binding pKi None 7.7 7.7 - 1
UnclassifiedUnclassified
Guide to Pharmacology 509 9 3 11 -0.1 CCCn1c2=N/C(=c\3/cc([nH]n3C)OCC(=O)Nc3ccc(cc3)C(=O)O)/N=c2c(=O)n(c1=O)CCC 16219300
CHEMBL431703 490 None 0 Human Binding pKi None 7.7 7.7 - 1
UnclassifiedUnclassified
Guide to Pharmacology 509 9 3 11 -0.1 CCCn1c2=N/C(=c\3/cc([nH]n3C)OCC(=O)Nc3ccc(cc3)C(=O)O)/N=c2c(=O)n(c1=O)CCC 16219300
135529386 489 None 0 Human Binding pKi None 7.8 7.8 - 1
UnclassifiedUnclassified
Guide to Pharmacology 537 10 2 12 0.4 CCOC(=O)c1ccc(cc1)NC(=O)COc1c/c(=C\2/N=c3c(=N2)c(=O)n(c(=O)n3CCC)CCC)/n([nH]1)C 16219300
440 489 None 0 Human Binding pKi None 7.8 7.8 - 1
UnclassifiedUnclassified
Guide to Pharmacology 537 10 2 12 0.4 CCOC(=O)c1ccc(cc1)NC(=O)COc1c/c(=C\2/N=c3c(=N2)c(=O)n(c(=O)n3CCC)CCC)/n([nH]1)C 16219300
CHEMBL284615 489 None 0 Human Binding pKi None 7.8 7.8 - 1
UnclassifiedUnclassified
Guide to Pharmacology 537 10 2 12 0.4 CCOC(=O)c1ccc(cc1)NC(=O)COc1c/c(=C\2/N=c3c(=N2)c(=O)n(c(=O)n3CCC)CCC)/n([nH]1)C 16219300
1328 1369 None 35 Human Binding pKi None 7.9 7.9 -7 4
UnclassifiedUnclassified
Guide to Pharmacology 284 3 1 5 1.6 CCn1c2nc([nH]c2c(=O)n(c1=O)CC)c1ccccc1 10496952
445 1369 None 35 Human Binding pKi None 7.9 7.9 -7 4
UnclassifiedUnclassified
Guide to Pharmacology 284 3 1 5 1.6 CCn1c2nc([nH]c2c(=O)n(c1=O)CC)c1ccccc1 10496952
CHEMBL11348 1369 None 35 Human Binding pKi None 7.9 7.9 -7 4
UnclassifiedUnclassified
Guide to Pharmacology 284 3 1 5 1.6 CCn1c2nc([nH]c2c(=O)n(c1=O)CC)c1ccccc1 10496952
135416058 491 None 0 Human Binding pKi None 8 8.0 - 1
UnclassifiedUnclassified
Guide to Pharmacology 530 8 1 11 -0.5 C=CCn1c2=N/C(=c\3/cc([nH]n3C)OCC(=O)N3CCN(CC3)c3ccccc3)/N=c2c(=O)n(c1=O)CC=C 16219300
442 491 None 0 Human Binding pKi None 8 8.0 - 1
UnclassifiedUnclassified
Guide to Pharmacology 530 8 1 11 -0.5 C=CCn1c2=N/C(=c\3/cc([nH]n3C)OCC(=O)N3CCN(CC3)c3ccccc3)/N=c2c(=O)n(c1=O)CC=C 16219300
CHEMBL2113342 491 None 0 Human Binding pKi None 8 8.0 - 1
UnclassifiedUnclassified
Guide to Pharmacology 530 8 1 11 -0.5 C=CCn1c2=N/C(=c\3/cc([nH]n3C)OCC(=O)N3CCN(CC3)c3ccccc3)/N=c2c(=O)n(c1=O)CC=C 16219300
135443367 487 None 0 Human Binding pKi None 8.1 8.1 22 2
UnclassifiedUnclassified
Guide to Pharmacology 534 9 1 10 1.8 CCCn1c2[nH]c(nc2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)N1CCN(CC1)c1ccccc1 16219300
382 487 None 0 Human Binding pKi None 8.1 8.1 22 2
UnclassifiedUnclassified
Guide to Pharmacology 534 9 1 10 1.8 CCCn1c2[nH]c(nc2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)N1CCN(CC1)c1ccccc1 16219300
CHEMBL33455 487 None 0 Human Binding pKi None 8.1 8.1 22 2
UnclassifiedUnclassified
Guide to Pharmacology 534 9 1 10 1.8 CCCn1c2[nH]c(nc2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)N1CCN(CC1)c1ccccc1 16219300
135489238 477 None 1 Human Binding pKi None 8.2 8.2 30 2
UnclassifiedUnclassified
Guide to Pharmacology 533 9 2 9 3.4 CCCn1c2[nH]c(nc2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)Nc1ccc(c(c1)Cl)Cl 16219300
381 477 None 1 Human Binding pKi None 8.2 8.2 30 2
UnclassifiedUnclassified
Guide to Pharmacology 533 9 2 9 3.4 CCCn1c2[nH]c(nc2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)Nc1ccc(c(c1)Cl)Cl 16219300
CHEMBL32802 477 None 1 Human Binding pKi None 8.2 8.2 30 2
UnclassifiedUnclassified
Guide to Pharmacology 533 9 2 9 3.4 CCCn1c2[nH]c(nc2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)Nc1ccc(c(c1)Cl)Cl 16219300
135476605 478 None 0 Human Binding pKi None 8.4 8.4 - 1
UnclassifiedUnclassified
Guide to Pharmacology 525 10 2 13 0.2 CCCn1c2=N/C(=c\3/cc([nH]n3C)OC(=O)CNc3ccc(c(c3)OC)OC)/N=c2c(=O)n(c1=O)CCC 16219300
437 478 None 0 Human Binding pKi None 8.4 8.4 - 1
UnclassifiedUnclassified
Guide to Pharmacology 525 10 2 13 0.2 CCCn1c2=N/C(=c\3/cc([nH]n3C)OC(=O)CNc3ccc(c(c3)OC)OC)/N=c2c(=O)n(c1=O)CCC 16219300
135522368 492 None 1 Human Binding pKi None 8.4 8.4 117 2
UnclassifiedUnclassified
Guide to Pharmacology 493 9 2 9 2.7 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)Nc1ccc(c(c1)C)C 16219300
383 492 None 1 Human Binding pKi None 8.4 8.4 117 2
UnclassifiedUnclassified
Guide to Pharmacology 493 9 2 9 2.7 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)Nc1ccc(c(c1)C)C 16219300
CHEMBL33491 492 None 1 Human Binding pKi None 8.4 8.4 117 2
UnclassifiedUnclassified
Guide to Pharmacology 493 9 2 9 2.7 CCCn1c2nc([nH]c2c(=O)n(c1=O)CCC)c1cc(nn1C)OCC(=O)Nc1ccc(c(c1)C)C 16219300
450 2970 None 9 Human Binding pKi None 9.3 9.3 257 4
UnclassifiedUnclassified
Guide to Pharmacology 525 10 3 6 3.6 CC(=O)NCCNc1nc(nc2c1cc([nH]2)C(=O)N1CCN(CC1)CCCc1ccccc1)c1ccccc1 15194002
454 2970 None 9 Human Binding pKi None 9.3 9.3 257 4
UnclassifiedUnclassified
Guide to Pharmacology 525 10 3 6 3.6 CC(=O)NCCNc1nc(nc2c1cc([nH]2)C(=O)N1CCN(CC1)CCCc1ccccc1)c1ccccc1 15194002
5311041 2970 None 9 Human Binding pKi None 9.3 9.3 257 4
UnclassifiedUnclassified
Guide to Pharmacology 525 10 3 6 3.6 CC(=O)NCCNc1nc(nc2c1cc([nH]2)C(=O)N1CCN(CC1)CCCc1ccccc1)c1ccccc1 15194002
CHEMBL485862 2970 None 9 Human Binding pKi None 9.3 9.3 257 4
UnclassifiedUnclassified
Guide to Pharmacology 525 10 3 6 3.6 CC(=O)NCCNc1nc(nc2c1cc([nH]2)C(=O)N1CCN(CC1)CCCc1ccccc1)c1ccccc1 15194002