Ligand source activities (1 row/activity)





Ligands Receptor Assay information Chemical information
Sel. page Common
name
GPCRdb ID #Vendors Reference
ligand
Fold selectivity
(Potency)
# tested GPCRs
(Potency)
Species p-value
(-log)
Type Activity
Relation
Activity
Value
Assay Type Assay Description Source Mol
weight
Rot
Bonds
H don H acc LogP Smiles DOI
145971909 171479 0 None 11 3 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at recombinant human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIAAgonist activity at recombinant human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIA
ChEMBL 411 11 2 6 4.8 CCCC[C@](C)(O)C/C=C/[C@H]1CCC(=O)[C@@H]1CCSc1nc(C(=O)O)cs1 10.1016/j.bmc.2017.11.035
CHEMBL4217198 171479 0 None 11 3 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at recombinant human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIAAgonist activity at recombinant human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIA
ChEMBL 411 11 2 6 4.8 CCCC[C@](C)(O)C/C=C/[C@H]1CCC(=O)[C@@H]1CCSc1nc(C(=O)O)cs1 10.1016/j.bmc.2017.11.035
66978356 170487 0 None 10 3 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at recombinant human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIAAgonist activity at recombinant human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIA
ChEMBL 425 12 2 6 5.2 CCCCC[C@](C)(O)C/C=C/[C@H]1CCC(=O)[C@@H]1CCSc1nc(C(=O)O)cs1 10.1016/j.bmc.2017.11.035
CHEMBL4204996 170487 0 None 10 3 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at recombinant human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIAAgonist activity at recombinant human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIA
ChEMBL 425 12 2 6 5.2 CCCCC[C@](C)(O)C/C=C/[C@H]1CCC(=O)[C@@H]1CCSc1nc(C(=O)O)cs1 10.1016/j.bmc.2017.11.035
127027876 146254 0 None - 1 Human 10.0 pEC50 = 10.0 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assayAgonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assay
ChEMBL 477 5 2 6 4.8 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3COc3ccc(Cl)c(C(F)(F)F)c3)O2)n1 10.1016/j.bmcl.2016.03.110
CHEMBL3794302 146254 0 None - 1 Human 10.0 pEC50 = 10.0 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assayAgonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assay
ChEMBL 477 5 2 6 4.8 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3COc3ccc(Cl)c(C(F)(F)F)c3)O2)n1 10.1016/j.bmcl.2016.03.110
145978309 170531 0 None 27 3 Human 10.0 pEC50 = 10.0 Functional
Agonist activity at recombinant human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIAAgonist activity at recombinant human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIA
ChEMBL 429 12 2 6 4.8 C[C@@](O)(C/C=C/[C@H]1CCC(=O)[C@@H]1CCSc1nc(C(=O)O)cs1)CCCCF 10.1016/j.bmc.2017.11.035
CHEMBL4205480 170531 0 None 27 3 Human 10.0 pEC50 = 10.0 Functional
Agonist activity at recombinant human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIAAgonist activity at recombinant human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIA
ChEMBL 429 12 2 6 4.8 C[C@@](O)(C/C=C/[C@H]1CCC(=O)[C@@H]1CCSc1nc(C(=O)O)cs1)CCCCF 10.1016/j.bmc.2017.11.035
127029692 146182 0 None - 1 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assayAgonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assay
ChEMBL 423 5 2 6 4.1 Cc1cc(OC[C@H]2[C@@H](O)C[C@@H]3O[C@@H](c4nc(C(=O)O)cs4)CC[C@@H]32)ccc1Cl 10.1016/j.bmcl.2016.03.110
CHEMBL3793515 146182 0 None - 1 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assayAgonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assay
ChEMBL 423 5 2 6 4.1 Cc1cc(OC[C@H]2[C@@H](O)C[C@@H]3O[C@@H](c4nc(C(=O)O)cs4)CC[C@@H]32)ccc1Cl 10.1016/j.bmcl.2016.03.110
11855868 159323 0 None 24 3 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assayAgonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assay
ChEMBL 429 11 2 4 5.6 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2CCCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3971632 159323 0 None 24 3 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assayAgonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assay
ChEMBL 429 11 2 4 5.6 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2CCCc2ccc(C(=O)O)s2)cc1 nan
11855865 160056 0 None 35 3 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assayAgonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assay
ChEMBL 445 12 2 5 5.2 CCCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3977724 160056 0 None 35 3 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assayAgonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assay
ChEMBL 445 12 2 5 5.2 CCCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
127026955 146228 0 None - 1 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assayAgonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assay
ChEMBL 437 5 2 6 4.4 Cc1cc(OC[C@H]2[C@H](O)C[C@@H]3O[C@@H](c4nc(C(=O)O)cs4)CC[C@@H]32)cc(C)c1Cl 10.1016/j.bmcl.2016.03.110
CHEMBL3794016 146228 0 None - 1 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assayAgonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assay
ChEMBL 437 5 2 6 4.4 Cc1cc(OC[C@H]2[C@H](O)C[C@@H]3O[C@@H](c4nc(C(=O)O)cs4)CC[C@@H]32)cc(C)c1Cl 10.1016/j.bmcl.2016.03.110
1883 9856 75 None -2 12 Rat 9.7 pEC50 = 9.7 Functional
Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP releaseAgonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmcl.2009.01.059
1916 9856 75 None -2 12 Rat 9.7 pEC50 = 9.7 Functional
Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP releaseAgonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmcl.2009.01.059
5280360 9856 75 None -2 12 Rat 9.7 pEC50 = 9.7 Functional
Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP releaseAgonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmcl.2009.01.059
913 9856 75 None -2 12 Rat 9.7 pEC50 = 9.7 Functional
Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP releaseAgonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmcl.2009.01.059
CHEMBL548 9856 75 None -2 12 Rat 9.7 pEC50 = 9.7 Functional
Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP releaseAgonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmcl.2009.01.059
DB00917 9856 75 None -2 12 Rat 9.7 pEC50 = 9.7 Functional
Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP releaseAgonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmcl.2009.01.059
18376258 202681 0 None - 1 Rat 9.7 pEC50 = 9.7 Functional
Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP releaseAgonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release
ChEMBL 465 9 1 3 5.4 CC(C)(C)c1ccc(CN(Cc2cccc(CCC(=O)O)c2)S(=O)(=O)c2ccccc2)cc1 10.1016/j.bmcl.2009.01.059
CHEMBL559065 202681 0 None - 1 Rat 9.7 pEC50 = 9.7 Functional
Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP releaseAgonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release
ChEMBL 465 9 1 3 5.4 CC(C)(C)c1ccc(CN(Cc2cccc(CCC(=O)O)c2)S(=O)(=O)c2ccccc2)cc1 10.1016/j.bmcl.2009.01.059
127026956 146204 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assayAgonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assay
ChEMBL 477 5 2 6 5.1 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3COc3cc(Cl)c(Cl)cc3Cl)O2)n1 10.1016/j.bmcl.2016.03.110
CHEMBL3793862 146204 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assayAgonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assay
ChEMBL 477 5 2 6 5.1 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3COc3cc(Cl)c(Cl)cc3Cl)O2)n1 10.1016/j.bmcl.2016.03.110
126495400 146099 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assayAgonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assay
ChEMBL 477 5 2 6 5.1 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3COc3ccc(Cl)c(Cl)c3Cl)O2)n1 10.1016/j.bmcl.2016.03.110
CHEMBL3792632 146099 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assayAgonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assay
ChEMBL 477 5 2 6 5.1 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3COc3ccc(Cl)c(Cl)c3Cl)O2)n1 10.1016/j.bmcl.2016.03.110
1929 8386 55 None 2 2 Rat 9.5 pEC50 = 9.5 Functional
Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP releaseAgonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release
ChEMBL 468 9 1 5 4.2 OC(=O)COc1cccc(c1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)C(C)(C)C 10.1016/j.bmcl.2009.01.059
9890801 8386 55 None 2 2 Rat 9.5 pEC50 = 9.5 Functional
Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP releaseAgonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release
ChEMBL 468 9 1 5 4.2 OC(=O)COc1cccc(c1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)C(C)(C)C 10.1016/j.bmcl.2009.01.059
CHEMBL563646 8386 55 None 2 2 Rat 9.5 pEC50 = 9.5 Functional
Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP releaseAgonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release
ChEMBL 468 9 1 5 4.2 OC(=O)COc1cccc(c1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)C(C)(C)C 10.1016/j.bmcl.2009.01.059
DB12022 8386 55 None 2 2 Rat 9.5 pEC50 = 9.5 Functional
Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP releaseAgonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release
ChEMBL 468 9 1 5 4.2 OC(=O)COc1cccc(c1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)C(C)(C)C 10.1016/j.bmcl.2009.01.059
67082748 171142 0 None 9 3 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at recombinant human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIAAgonist activity at recombinant human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIA
ChEMBL 451 10 2 6 5.0 C[C@@](O)(C/C=C/[C@H]1CCC(=O)[C@@H]1CCSc1nc(C(=O)O)cs1)CCC(F)(F)F 10.1016/j.bmc.2017.11.035
CHEMBL4212770 171142 0 None 9 3 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at recombinant human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIAAgonist activity at recombinant human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIA
ChEMBL 451 10 2 6 5.0 C[C@@](O)(C/C=C/[C@H]1CCC(=O)[C@@H]1CCSc1nc(C(=O)O)cs1)CCC(F)(F)F 10.1016/j.bmc.2017.11.035
15979081 170619 0 None 5 3 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at recombinant human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIAAgonist activity at recombinant human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIA
ChEMBL 425 12 2 6 5.2 CCCCCC(C)(O)C/C=C/[C@H]1CCC(=O)[C@@H]1CCSc1nc(C(=O)O)cs1 10.1016/j.bmc.2017.11.035
CHEMBL4206444 170619 0 None 5 3 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at recombinant human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIAAgonist activity at recombinant human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIA
ChEMBL 425 12 2 6 5.2 CCCCCC(C)(O)C/C=C/[C@H]1CCC(=O)[C@@H]1CCSc1nc(C(=O)O)cs1 10.1016/j.bmc.2017.11.035
127051063 147100 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
ChEMBL 443 5 2 6 4.2 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3COc3ccccc3C(F)(F)F)O2)n1 10.1021/acsmedchemlett.5b00455
CHEMBL3806284 147100 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
ChEMBL 443 5 2 6 4.2 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3COc3ccccc3C(F)(F)F)O2)n1 10.1021/acsmedchemlett.5b00455
127027877 146197 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assayAgonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assay
ChEMBL 443 5 2 6 4.4 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3COc3ccc(Cl)c(Cl)c3)O2)n1 10.1016/j.bmcl.2016.03.110
CHEMBL3793802 146197 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assayAgonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assay
ChEMBL 443 5 2 6 4.4 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3COc3ccc(Cl)c(Cl)c3)O2)n1 10.1016/j.bmcl.2016.03.110
16725337 156380 0 None 4 4 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assayAgonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assay
ChEMBL 443 12 2 4 6.0 CCCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2CCCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3947001 156380 0 None 4 4 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assayAgonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assay
ChEMBL 443 12 2 4 6.0 CCCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2CCCc2ccc(C(=O)O)s2)cc1 nan
11294085 144030 0 None 1 3 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at recombinant human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIAAgonist activity at recombinant human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIA
ChEMBL 458 12 2 7 4.0 O=C(O)c1csc(SCCN2C(=O)OC[C@@H]2/C=C/[C@@H](O)C2(CCCCF)CCC2)n1 10.1016/j.bmc.2017.11.035
CHEMBL3751951 144030 0 None 1 3 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at recombinant human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIAAgonist activity at recombinant human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIA
ChEMBL 458 12 2 7 4.0 O=C(O)c1csc(SCCN2C(=O)OC[C@@H]2/C=C/[C@@H](O)C2(CCCCF)CCC2)n1 10.1016/j.bmc.2017.11.035
127028169 146268 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assayAgonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assay
ChEMBL 437 6 2 6 4.4 CCc1cc(OC[C@H]2[C@H](O)C[C@@H]3O[C@@H](c4nc(C(=O)O)cs4)CC[C@@H]32)ccc1Cl 10.1016/j.bmcl.2016.03.110
CHEMBL3794466 146268 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assayAgonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assay
ChEMBL 437 6 2 6 4.4 CCc1cc(OC[C@H]2[C@H](O)C[C@@H]3O[C@@H](c4nc(C(=O)O)cs4)CC[C@@H]32)ccc1Cl 10.1016/j.bmcl.2016.03.110
118352160 146207 0 None 7079 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assayAgonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assay
ChEMBL 423 5 2 6 4.1 Cc1cc(OC[C@H]2[C@H](O)C[C@@H]3O[C@@H](c4nc(C(=O)O)cs4)CC[C@@H]32)ccc1Cl 10.1016/j.bmcl.2016.03.110
CHEMBL3793892 146207 0 None 7079 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assayAgonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assay
ChEMBL 423 5 2 6 4.1 Cc1cc(OC[C@H]2[C@H](O)C[C@@H]3O[C@@H](c4nc(C(=O)O)cs4)CC[C@@H]32)ccc1Cl 10.1016/j.bmcl.2016.03.110
127027874 146141 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assayAgonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assay
ChEMBL 443 5 2 6 4.2 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3COc3cccc(C(F)(F)F)c3)O2)n1 10.1016/j.bmcl.2016.03.110
CHEMBL3793045 146141 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assayAgonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assay
ChEMBL 443 5 2 6 4.2 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3COc3cccc(C(F)(F)F)c3)O2)n1 10.1016/j.bmcl.2016.03.110
127027874 146141 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
ChEMBL 443 5 2 6 4.2 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3COc3cccc(C(F)(F)F)c3)O2)n1 10.1021/acsmedchemlett.5b00455
CHEMBL3793045 146141 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
ChEMBL 443 5 2 6 4.2 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3COc3cccc(C(F)(F)F)c3)O2)n1 10.1021/acsmedchemlett.5b00455
127051656 147072 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
ChEMBL 459 6 2 7 4.0 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3COc3cccc(OC(F)(F)F)c3)O2)n1 10.1021/acsmedchemlett.5b00455
CHEMBL3805981 147072 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
ChEMBL 459 6 2 7 4.0 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3COc3cccc(OC(F)(F)F)c3)O2)n1 10.1021/acsmedchemlett.5b00455
89443871 158224 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 423 8 2 4 5.5 COc1c(C)cc(-c2cccc(F)c2)cc1CNc1c(C)ccc(OCC(=O)O)c1C nan
CHEMBL3961932 158224 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 423 8 2 4 5.5 COc1c(C)cc(-c2cccc(F)c2)cc1CNc1c(C)ccc(OCC(=O)O)c1C nan
89443827 150891 0 None - 1 Human 9.0 pEC50 = 9 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 395 7 3 4 4.9 Cc1ccc(OCC(=O)O)c(C)c1NCc1cc(O)cc(-c2cccc(F)c2)c1 nan
CHEMBL3903635 150891 0 None - 1 Human 9.0 pEC50 = 9 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 395 7 3 4 4.9 Cc1ccc(OCC(=O)O)c(C)c1NCc1cc(O)cc(-c2cccc(F)c2)c1 nan
18376082 201702 0 None - 1 Rat 9.0 pEC50 = 9.0 Functional
Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP releaseAgonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release
ChEMBL 472 9 1 5 4.8 CC(C)(C)c1ccc(CN(Cc2cccc(CCC(=O)O)c2)S(=O)(=O)c2nccs2)cc1 10.1016/j.bmcl.2009.01.059
CHEMBL541517 201702 0 None - 1 Rat 9.0 pEC50 = 9.0 Functional
Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP releaseAgonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release
ChEMBL 472 9 1 5 4.8 CC(C)(C)c1ccc(CN(Cc2cccc(CCC(=O)O)c2)S(=O)(=O)c2nccs2)cc1 10.1016/j.bmcl.2009.01.059
145977227 170786 0 None -1 4 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at recombinant human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIAAgonist activity at recombinant human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIA
ChEMBL 437 10 2 6 5.2 C[C@@](O)(C/C=C/[C@H]1CCC(=O)[C@@H]1CCSc1nc(C(=O)O)cs1)CC1CCCC1 10.1016/j.bmc.2017.11.035
CHEMBL4208379 170786 0 None -1 4 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at recombinant human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIAAgonist activity at recombinant human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIA
ChEMBL 437 10 2 6 5.2 C[C@@](O)(C/C=C/[C@H]1CCC(=O)[C@@H]1CCSc1nc(C(=O)O)cs1)CC1CCCC1 10.1016/j.bmc.2017.11.035
10315 9700 28 None 1659 2 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 478 10 2 8 2.6 OC(=O)CNc1cccc(n1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)n1cccn1 10.1021/acs.jmedchem.8b00808
44230575 9700 28 None 1659 2 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 478 10 2 8 2.6 OC(=O)CNc1cccc(n1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)n1cccn1 10.1021/acs.jmedchem.8b00808
CHEMBL3707245 9700 28 None 1659 2 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 478 10 2 8 2.6 OC(=O)CNc1cccc(n1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)n1cccn1 10.1021/acs.jmedchem.8b00808
126495463 147085 0 None 69 3 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
ChEMBL 389 6 2 6 3.5 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3CCOc3ccccc3)O2)n1 10.1021/acsmedchemlett.5b00455
CHEMBL3806130 147085 0 None 69 3 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
ChEMBL 389 6 2 6 3.5 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3CCOc3ccccc3)O2)n1 10.1021/acsmedchemlett.5b00455
11502897 149571 0 None 43 3 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assayAgonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assay
ChEMBL 431 11 2 5 4.8 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3892847 149571 0 None 43 3 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assayAgonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assay
ChEMBL 431 11 2 5 4.8 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
11855870 153058 0 None 467 3 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assayAgonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assay
ChEMBL 427 11 1 4 5.7 CCCCCC(=O)c1ccc(N2C(=O)CC[C@@H]2CCCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3920756 153058 0 None 467 3 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assayAgonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assay
ChEMBL 427 11 1 4 5.7 CCCCCC(=O)c1ccc(N2C(=O)CC[C@@H]2CCCc2ccc(C(=O)O)s2)cc1 nan
11855868 159323 0 None 24 3 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 429 11 2 4 5.6 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2CCCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3971632 159323 0 None 24 3 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 429 11 2 4 5.6 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2CCCc2ccc(C(=O)O)s2)cc1 nan
11855865 160056 0 None 35 3 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 445 12 2 5 5.2 CCCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3977724 160056 0 None 35 3 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 445 12 2 5 5.2 CCCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
44230722 178508 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 489 10 2 7 3.4 O=C(O)CNc1cccc(CN(Cc2ccc(-c3ccccn3)cc2)S(=O)(=O)c2cccnc2)n1 10.1021/acs.jmedchem.8b00808
CHEMBL4467099 178508 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 489 10 2 7 3.4 O=C(O)CNc1cccc(CN(Cc2ccc(-c3ccccn3)cc2)S(=O)(=O)c2cccnc2)n1 10.1021/acs.jmedchem.8b00808
11855868 159323 0 None 24 3 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assayAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assay
ChEMBL 429 11 2 4 5.6 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2CCCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3971632 159323 0 None 24 3 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assayAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assay
ChEMBL 429 11 2 4 5.6 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2CCCc2ccc(C(=O)O)s2)cc1 nan
127026953 146277 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assayAgonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assay
ChEMBL 439 6 2 7 3.8 COc1cc(OC[C@H]2[C@H](O)C[C@@H]3O[C@@H](c4nc(C(=O)O)cs4)CC[C@@H]32)ccc1Cl 10.1016/j.bmcl.2016.03.110
CHEMBL3794585 146277 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assayAgonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assay
ChEMBL 439 6 2 7 3.8 COc1cc(OC[C@H]2[C@H](O)C[C@@H]3O[C@@H](c4nc(C(=O)O)cs4)CC[C@@H]32)ccc1Cl 10.1016/j.bmcl.2016.03.110
1883 9856 75 None -6 12 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/acsmedchemlett.5b00455
1916 9856 75 None -6 12 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/acsmedchemlett.5b00455
5280360 9856 75 None -6 12 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/acsmedchemlett.5b00455
913 9856 75 None -6 12 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/acsmedchemlett.5b00455
CHEMBL548 9856 75 None -6 12 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/acsmedchemlett.5b00455
DB00917 9856 75 None -6 12 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/acsmedchemlett.5b00455
126495398 146989 0 None 416 3 Human 8.0 pEC50 = 8 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
ChEMBL 403 7 2 6 3.9 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3CCCOc3ccccc3)O2)n1 10.1021/acsmedchemlett.5b00455
CHEMBL3805044 146989 0 None 416 3 Human 8.0 pEC50 = 8 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
ChEMBL 403 7 2 6 3.9 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3CCCOc3ccccc3)O2)n1 10.1021/acsmedchemlett.5b00455
89443586 152463 0 None - 1 Human 8.0 pEC50 = 8 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 401 7 2 3 5.2 Cc1c(OCC(=O)O)ccc(F)c1NCc1cc(-c2cccc(F)c2)ccc1F nan
CHEMBL3916133 152463 0 None - 1 Human 8.0 pEC50 = 8 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 401 7 2 3 5.2 Cc1c(OCC(=O)O)ccc(F)c1NCc1cc(-c2cccc(F)c2)ccc1F nan
118517489 150469 0 None -18 3 Human 8.0 pEC50 = 8 Functional
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
ChEMBL 414 8 2 3 4.4 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2cc(F)ccc2F)cc1 nan
CHEMBL3900245 150469 0 None -18 3 Human 8.0 pEC50 = 8 Functional
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
ChEMBL 414 8 2 3 4.4 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2cc(F)ccc2F)cc1 nan
92135977 159675 0 None -141 4 Human 8.0 pEC50 = 8 Functional
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
ChEMBL 396 8 2 3 4.2 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2cccc(F)c2)cc1 nan
CHEMBL3974652 159675 0 None -141 4 Human 8.0 pEC50 = 8 Functional
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
ChEMBL 396 8 2 3 4.2 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2cccc(F)c2)cc1 nan
8541 9718 2 None -66069 4 Human 5.0 pEC50 = 5 Functional
Agonist activity at human EP2 receptor expressed in HEK293T/17 cells assessed as increase in intracellular cAMP level incubated for 30 mins by ELISAAgonist activity at human EP2 receptor expressed in HEK293T/17 cells assessed as increase in intracellular cAMP level incubated for 30 mins by ELISA
ChEMBL 436 13 3 6 2.8 COCc1cccc(c1)C[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCSCCCC(=O)O)O 10.1021/acs.jmedchem.9b00336
9824353 9718 2 None -66069 4 Human 5.0 pEC50 = 5 Functional
Agonist activity at human EP2 receptor expressed in HEK293T/17 cells assessed as increase in intracellular cAMP level incubated for 30 mins by ELISAAgonist activity at human EP2 receptor expressed in HEK293T/17 cells assessed as increase in intracellular cAMP level incubated for 30 mins by ELISA
ChEMBL 436 13 3 6 2.8 COCc1cccc(c1)C[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCSCCCC(=O)O)O 10.1021/acs.jmedchem.9b00336
CHEMBL292964 9718 2 None -66069 4 Human 5.0 pEC50 = 5 Functional
Agonist activity at human EP2 receptor expressed in HEK293T/17 cells assessed as increase in intracellular cAMP level incubated for 30 mins by ELISAAgonist activity at human EP2 receptor expressed in HEK293T/17 cells assessed as increase in intracellular cAMP level incubated for 30 mins by ELISA
ChEMBL 436 13 3 6 2.8 COCc1cccc(c1)C[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCSCCCC(=O)O)O 10.1021/acs.jmedchem.9b00336
59465571 153063 0 None -1 2 Human 6.0 pEC50 = 6 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 386 12 2 3 5.6 CCCCCC(O)c1ccc([C@H]2CCC(=O)[C@@H]2C/C=C\CCCC(=O)O)cc1 nan
CHEMBL3920796 153063 0 None -1 2 Human 6.0 pEC50 = 6 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 386 12 2 3 5.6 CCCCCC(O)c1ccc([C@H]2CCC(=O)[C@@H]2C/C=C\CCCC(=O)O)cc1 nan
118517361 160149 0 None -107 3 Human 6.0 pEC50 = 6.0 Functional
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
ChEMBL 446 8 2 3 5.1 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2cccc(C(F)(F)F)c2)cc1 nan
CHEMBL3978590 160149 0 None -107 3 Human 6.0 pEC50 = 6.0 Functional
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
ChEMBL 446 8 2 3 5.1 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2cccc(C(F)(F)F)c2)cc1 nan
11955384 154316 0 None 33 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 360 8 2 3 4.4 CC(C)(C)c1ccc([C@H]2[C@H](O)CC(=O)[C@@H]2CCCCCCC(=O)O)cc1 nan
CHEMBL3930718 154316 0 None 33 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 360 8 2 3 4.4 CC(C)(C)c1ccc([C@H]2[C@H](O)CC(=O)[C@@H]2CCCCCCC(=O)O)cc1 nan
45268715 202755 0 None - 1 Rat 7.0 pEC50 = 7.0 Functional
Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP releaseAgonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release
ChEMBL 403 11 1 3 4.4 CCCCc1ccc(CN(c2ccccc2CCCC(=O)O)S(C)(=O)=O)cc1 10.1016/j.bmcl.2009.01.059
CHEMBL559760 202755 0 None - 1 Rat 7.0 pEC50 = 7.0 Functional
Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP releaseAgonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release
ChEMBL 403 11 1 3 4.4 CCCCc1ccc(CN(c2ccccc2CCCC(=O)O)S(C)(=O)=O)cc1 10.1016/j.bmcl.2009.01.059
16750455 158051 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 342 7 1 2 5.2 CC(C)(C)c1ccc([C@H]2CCC(=O)[C@@H]2C/C=C\CCCC(=O)O)cc1 nan
CHEMBL3960352 158051 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 342 7 1 2 5.2 CC(C)(C)c1ccc([C@H]2CCC(=O)[C@@H]2C/C=C\CCCC(=O)O)cc1 nan
53259980 183148 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 468 9 2 6 3.7 CC(C)(C)c1cccc(CN(Cc2cccc(NCC(=O)O)n2)S(=O)(=O)c2cccnc2)c1 10.1021/acs.jmedchem.8b00808
CHEMBL4566584 183148 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 468 9 2 6 3.7 CC(C)(C)c1cccc(CN(Cc2cccc(NCC(=O)O)n2)S(=O)(=O)c2cccnc2)c1 10.1021/acs.jmedchem.8b00808
CHEMBL4595789 183148 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 468 9 2 6 3.7 CC(C)(C)c1cccc(CN(Cc2cccc(NCC(=O)O)n2)S(=O)(=O)c2cccnc2)c1 10.1021/acs.jmedchem.8b00808
126495507 146157 0 None 154 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assayAgonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assay
ChEMBL 425 5 1 5 5.1 Cc1cc(OC[C@H]2[C@@H](F)C[C@@H]3O[C@@H](c4nc(C(=O)O)cs4)CC[C@@H]32)ccc1Cl 10.1016/j.bmcl.2016.03.110
CHEMBL3793167 146157 0 None 154 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assayAgonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assay
ChEMBL 425 5 1 5 5.1 Cc1cc(OC[C@H]2[C@@H](F)C[C@@H]3O[C@@H](c4nc(C(=O)O)cs4)CC[C@@H]32)ccc1Cl 10.1016/j.bmcl.2016.03.110
71515776 161135 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 419 7 2 3 5.5 CC(Nc1c(F)ccc(OCC(=O)O)c1F)c1cc(-c2cccc(F)c2)ccc1F nan
CHEMBL3986985 161135 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 419 7 2 3 5.5 CC(Nc1c(F)ccc(OCC(=O)O)c1F)c1cc(-c2cccc(F)c2)ccc1F nan
44304164 210013 0 None - 1 Mouse 8.0 pEC50 = 8.0 Functional
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptor
ChEMBL 378 11 3 4 3.6 CCC1([C@@H](O)C/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2C/C=C\CCCC(=O)O)CCC1 10.1016/s0960-894x(01)00359-6
CHEMBL64483 210013 0 None - 1 Mouse 8.0 pEC50 = 8.0 Functional
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptor
ChEMBL 378 11 3 4 3.6 CCC1([C@@H](O)C/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2C/C=C\CCCC(=O)O)CCC1 10.1016/s0960-894x(01)00359-6
118517485 149528 0 None -3 4 Human 8.0 pEC50 = 8.0 Functional
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
ChEMBL 396 8 2 3 4.2 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2ccc(F)cc2)cc1 nan
CHEMBL3892492 149528 0 None -3 4 Human 8.0 pEC50 = 8.0 Functional
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
ChEMBL 396 8 2 3 4.2 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2ccc(F)cc2)cc1 nan
71515515 157783 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 369 7 2 3 4.7 O=C(O)COc1cccc(NCc2cc(-c3cccc(F)c3)ccc2F)c1 nan
CHEMBL3958411 157783 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 369 7 2 3 4.7 O=C(O)COc1cccc(NCc2cc(-c3cccc(F)c3)ccc2F)c1 nan
126495427 146244 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assayAgonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assay
ChEMBL 422 5 2 5 4.7 Cc1cc(OC[C@H]2[C@H](O)C[C@@H]3O[C@@H](c4csc(C(=O)O)c4)CC[C@@H]32)ccc1Cl 10.1016/j.bmcl.2016.03.110
CHEMBL3794185 146244 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assayAgonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assay
ChEMBL 422 5 2 5 4.7 Cc1cc(OC[C@H]2[C@H](O)C[C@@H]3O[C@@H](c4csc(C(=O)O)c4)CC[C@@H]32)ccc1Cl 10.1016/j.bmcl.2016.03.110
11955193 150362 0 None 10 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 378 7 2 2 5.3 CC(C)(C)c1ccc([C@H]2[C@H](O)C[C@@H](Cl)[C@@H]2C/C=C\CCCC(=O)O)cc1 nan
CHEMBL3899346 150362 0 None 10 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 378 7 2 2 5.3 CC(C)(C)c1ccc([C@H]2[C@H](O)C[C@@H](Cl)[C@@H]2C/C=C\CCCC(=O)O)cc1 nan
155550016 183461 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 468 13 2 6 3.6 O=C(O)CNc1cccc(CN(CCCCCc2ccccc2)S(=O)(=O)c2cccnc2)n1 10.1021/acs.jmedchem.8b00808
CHEMBL4539881 183461 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 468 13 2 6 3.6 O=C(O)CNc1cccc(CN(CCCCCc2ccccc2)S(=O)(=O)c2cccnc2)n1 10.1021/acs.jmedchem.8b00808
CHEMBL4598324 183461 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 468 13 2 6 3.6 O=C(O)CNc1cccc(CN(CCCCCc2ccccc2)S(=O)(=O)c2cccnc2)n1 10.1021/acs.jmedchem.8b00808
53260150 183311 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 480 9 2 6 3.4 O=C(O)CNc1cccc(CN(Cc2ccc(C(F)(F)F)cc2)S(=O)(=O)c2cccnc2)n1 10.1021/acs.jmedchem.8b00808
CHEMBL4451786 183311 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 480 9 2 6 3.4 O=C(O)CNc1cccc(CN(Cc2ccc(C(F)(F)F)cc2)S(=O)(=O)c2cccnc2)n1 10.1021/acs.jmedchem.8b00808
CHEMBL4597091 183311 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 480 9 2 6 3.4 O=C(O)CNc1cccc(CN(Cc2ccc(C(F)(F)F)cc2)S(=O)(=O)c2cccnc2)n1 10.1021/acs.jmedchem.8b00808
11855590 151152 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assayAgonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assay
ChEMBL 387 8 2 5 3.4 CC(C)C(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)o2)cc1 nan
CHEMBL3905811 151152 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assayAgonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assay
ChEMBL 387 8 2 5 3.4 CC(C)C(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)o2)cc1 nan
11855591 151214 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 435 9 2 5 4.0 O=C(O)c1ccc(COC[C@H]2CCC(=O)N2c2ccc(C(O)Cc3ccccc3)cc2)o1 nan
CHEMBL3906402 151214 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 435 9 2 5 4.0 O=C(O)c1ccc(COC[C@H]2CCC(=O)N2c2ccc(C(O)Cc3ccccc3)cc2)o1 nan
11855591 151214 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assayAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assay
ChEMBL 435 9 2 5 4.0 O=C(O)c1ccc(COC[C@H]2CCC(=O)N2c2ccc(C(O)Cc3ccccc3)cc2)o1 nan
CHEMBL3906402 151214 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assayAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assay
ChEMBL 435 9 2 5 4.0 O=C(O)c1ccc(COC[C@H]2CCC(=O)N2c2ccc(C(O)Cc3ccccc3)cc2)o1 nan
118517360 150753 0 None -61 3 Human 6.9 pEC50 = 6.9 Functional
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
ChEMBL 412 8 2 3 4.7 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2cccc(Cl)c2)cc1 nan
CHEMBL3902700 150753 0 None -61 3 Human 6.9 pEC50 = 6.9 Functional
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
ChEMBL 412 8 2 3 4.7 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2cccc(Cl)c2)cc1 nan
118517489 150469 0 None -18 3 Human 6.9 pEC50 = 6.9 Functional
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
ChEMBL 414 8 2 3 4.4 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2cc(F)ccc2F)cc1 nan
CHEMBL3900245 150469 0 None -18 3 Human 6.9 pEC50 = 6.9 Functional
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
ChEMBL 414 8 2 3 4.4 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2cc(F)ccc2F)cc1 nan
11955257 160665 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 410 9 3 3 5.3 CC(C)(C)C(O)c1ccc([C@H]2[C@H](O)C[C@@H](Cl)[C@@H]2CCCCCCC(=O)O)cc1 nan
CHEMBL3983069 160665 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 410 9 3 3 5.3 CC(C)(C)C(O)c1ccc([C@H]2[C@H](O)C[C@@H](Cl)[C@@H]2CCCCCCC(=O)O)cc1 nan
118352211 146163 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assayAgonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assay
ChEMBL 375 5 2 6 3.1 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3COc3ccccc3)O2)n1 10.1016/j.bmcl.2016.03.110
CHEMBL3793209 146163 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assayAgonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assay
ChEMBL 375 5 2 6 3.1 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3COc3ccccc3)O2)n1 10.1016/j.bmcl.2016.03.110
118352211 146163 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
ChEMBL 375 5 2 6 3.1 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3COc3ccccc3)O2)n1 10.1021/acsmedchemlett.5b00455
CHEMBL3793209 146163 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
ChEMBL 375 5 2 6 3.1 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3COc3ccccc3)O2)n1 10.1021/acsmedchemlett.5b00455
126495491 147003 0 None 28 4 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
ChEMBL 429 8 2 6 4.5 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3/C=C/CCCOc3ccccc3)O2)n1 10.1021/acsmedchemlett.5b00455
CHEMBL3805169 147003 0 None 28 4 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
ChEMBL 429 8 2 6 4.5 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3/C=C/CCCOc3ccccc3)O2)n1 10.1021/acsmedchemlett.5b00455
127050452 147022 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
ChEMBL 443 5 2 6 4.2 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3COc3ccc(C(F)(F)F)cc3)O2)n1 10.1021/acsmedchemlett.5b00455
CHEMBL3805408 147022 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
ChEMBL 443 5 2 6 4.2 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3COc3ccc(C(F)(F)F)cc3)O2)n1 10.1021/acsmedchemlett.5b00455
53260293 182992 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 494 11 2 6 4.2 CCC1(c2ccc(CN(Cc3cccc(NCC(=O)O)n3)S(=O)(=O)c3cccnc3)cc2)CCC1 10.1021/acs.jmedchem.8b00808
CHEMBL4594090 182992 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 494 11 2 6 4.2 CCC1(c2ccc(CN(Cc3cccc(NCC(=O)O)n3)S(=O)(=O)c3cccnc3)cc2)CCC1 10.1021/acs.jmedchem.8b00808
89443700 159365 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 419 7 2 3 5.3 Cc1cc(-c2cccc(F)c2)cc(CNc2c(F)ccc(OCC(=O)O)c2F)c1F nan
CHEMBL3971868 159365 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 419 7 2 3 5.3 Cc1cc(-c2cccc(F)c2)cc(CNc2c(F)ccc(OCC(=O)O)c2F)c1F nan
89444072 155723 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 419 7 2 3 5.3 Cc1c(-c2cccc(F)c2)ccc(F)c1CNc1c(F)ccc(OCC(=O)O)c1F nan
CHEMBL3941975 155723 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 419 7 2 3 5.3 Cc1c(-c2cccc(F)c2)ccc(F)c1CNc1c(F)ccc(OCC(=O)O)c1F nan
44303952 107663 0 None - 1 Mouse 6.9 pEC50 = 6.9 Functional
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptor
ChEMBL 420 14 3 4 4.8 CCCCCC1([C@@H](O)C/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2C/C=C\CCCC(=O)O)CCC1 10.1016/s0960-894x(01)00359-6
CHEMBL293697 107663 0 None - 1 Mouse 6.9 pEC50 = 6.9 Functional
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptor
ChEMBL 420 14 3 4 4.8 CCCCCC1([C@@H](O)C/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2C/C=C\CCCC(=O)O)CCC1 10.1016/s0960-894x(01)00359-6
10270893 101003 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human prostaglandin EP2 receptorAgonist activity at human prostaglandin EP2 receptor
ChEMBL 376 12 2 4 3.1 CCCCCC(O)CCCN1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.09.074
CHEMBL249954 101003 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human prostaglandin EP2 receptorAgonist activity at human prostaglandin EP2 receptor
ChEMBL 376 12 2 4 3.1 CCCCCC(O)CCCN1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.09.074
9885481 202162 0 None 14 2 Rat 6.9 pEC50 = 6.9 Functional
Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP releaseAgonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release
ChEMBL 365 16 2 4 3.0 CCCCCC(O)CCCN(CCCCCCC(=O)O)S(C)(=O)=O 10.1016/j.bmcl.2009.01.059
CHEMBL551951 202162 0 None 14 2 Rat 6.9 pEC50 = 6.9 Functional
Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP releaseAgonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release
ChEMBL 365 16 2 4 3.0 CCCCCC(O)CCCN(CCCCCCC(=O)O)S(C)(=O)=O 10.1016/j.bmcl.2009.01.059
11855325 151469 0 None 19 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 387 6 1 4 4.5 CC(C)(C)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3908484 151469 0 None 19 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 387 6 1 4 4.5 CC(C)(C)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
11855325 151469 0 None 19 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assayAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assay
ChEMBL 387 6 1 4 4.5 CC(C)(C)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3908484 151469 0 None 19 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assayAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assay
ChEMBL 387 6 1 4 4.5 CC(C)(C)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
127050451 146999 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
ChEMBL 459 6 2 7 4.0 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3COc3ccc(OC(F)(F)F)cc3)O2)n1 10.1021/acsmedchemlett.5b00455
CHEMBL3805122 146999 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
ChEMBL 459 6 2 7 4.0 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3COc3ccc(OC(F)(F)F)cc3)O2)n1 10.1021/acsmedchemlett.5b00455
89443781 156057 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 423 7 2 3 5.1 O=C(O)COc1ccc(F)c(NCc2cc(-c3ccc(F)c(F)c3)ccc2F)c1F nan
CHEMBL3944601 156057 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 423 7 2 3 5.1 O=C(O)COc1ccc(F)c(NCc2cc(-c3ccc(F)c(F)c3)ccc2F)c1F nan
10481859 81942 0 None -67 2 Rat 5.9 pEC50 = 5.9 Functional
Agonist activity at rat EP2 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP2 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
ChEMBL 522 10 2 6 5.4 Cc1ccc(-c2cccc(C[C@H](O)/C=C/[C@H]3CCC(=O)N3CCSc3nc(C(=O)O)cs3)c2)cc1C 10.1016/j.bmc.2012.04.008
CHEMBL2036321 81942 0 None -67 2 Rat 5.9 pEC50 = 5.9 Functional
Agonist activity at rat EP2 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP2 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
ChEMBL 522 10 2 6 5.4 Cc1ccc(-c2cccc(C[C@H](O)/C=C/[C@H]3CCC(=O)N3CCSc3nc(C(=O)O)cs3)c2)cc1C 10.1016/j.bmc.2012.04.008
44303627 209984 0 None - 1 Mouse 5.9 pEC50 = 5.9 Functional
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptor
ChEMBL 364 11 3 3 4.5 CCC1([C@@H](O)C/C=C/[C@H]2[C@H](O)CC[C@@H]2C/C=C\CCCC(=O)O)CCC1 10.1016/s0960-894x(01)00359-6
CHEMBL64358 209984 0 None - 1 Mouse 5.9 pEC50 = 5.9 Functional
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptor
ChEMBL 364 11 3 3 4.5 CCC1([C@@H](O)C/C=C/[C@H]2[C@H](O)CC[C@@H]2C/C=C\CCCC(=O)O)CCC1 10.1016/s0960-894x(01)00359-6
134146425 155982 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 394 12 2 2 6.4 CCCCC(O)c1ccc([C@H]2CC[C@@H](Cl)[C@@H]2CCCCCCC(=O)O)cc1 nan
CHEMBL3943966 155982 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 394 12 2 2 6.4 CCCCC(O)c1ccc([C@H]2CC[C@@H](Cl)[C@@H]2CCCCCCC(=O)O)cc1 nan
11855591 151214 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assayAgonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assay
ChEMBL 435 9 2 5 4.0 O=C(O)c1ccc(COC[C@H]2CCC(=O)N2c2ccc(C(O)Cc3ccccc3)cc2)o1 nan
CHEMBL3906402 151214 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assayAgonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assay
ChEMBL 435 9 2 5 4.0 O=C(O)c1ccc(COC[C@H]2CCC(=O)N2c2ccc(C(O)Cc3ccccc3)cc2)o1 nan
10291963 91483 0 None -32 4 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human EP2 receptor by cAMP assayAgonist activity at human EP2 receptor by cAMP assay
ChEMBL 359 10 2 3 3.4 CCCCC[C@H](O)/C=C/[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.11.020
CHEMBL222715 91483 0 None -32 4 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human EP2 receptor by cAMP assayAgonist activity at human EP2 receptor by cAMP assay
ChEMBL 359 10 2 3 3.4 CCCCC[C@H](O)/C=C/[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.11.020
127029402 146136 0 None 524 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assayAgonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assay
ChEMBL 407 5 2 6 3.6 Cc1cc(OC[C@H]2[C@H](O)C[C@@H]3O[C@@H](c4nc(C(=O)O)co4)CC[C@@H]32)ccc1Cl 10.1016/j.bmcl.2016.03.110
CHEMBL3793009 146136 0 None 524 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assayAgonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assay
ChEMBL 407 5 2 6 3.6 Cc1cc(OC[C@H]2[C@H](O)C[C@@H]3O[C@@H](c4nc(C(=O)O)co4)CC[C@@H]32)ccc1Cl 10.1016/j.bmcl.2016.03.110
24760052 157964 0 None 24 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assayAgonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assay
ChEMBL 427 10 2 4 5.4 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2/C=C/Cc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3959769 157964 0 None 24 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assayAgonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assay
ChEMBL 427 10 2 4 5.4 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2/C=C/Cc2ccc(C(=O)O)s2)cc1 nan
17751059 155047 0 None 3 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 440 12 2 2 6.8 CCCCCC(O)c1ccc([C@H]2[C@H](Cl)C[C@@H](Cl)[C@@H]2C/C=C\CCCC(=O)O)cc1 nan
CHEMBL3936540 155047 0 None 3 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 440 12 2 2 6.8 CCCCCC(O)c1ccc([C@H]2[C@H](Cl)C[C@@H](Cl)[C@@H]2C/C=C\CCCC(=O)O)cc1 nan
89444124 150209 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 397 7 2 3 5.3 Cc1cc(-c2ccccc2)cc(CNc2c(F)ccc(OCC(=O)O)c2F)c1C nan
CHEMBL3898152 150209 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 397 7 2 3 5.3 Cc1cc(-c2ccccc2)cc(CNc2c(F)ccc(OCC(=O)O)c2F)c1C nan
156014791 184363 0 None -309 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human EP2 receptor expressed in HEK293 cells by calcium-5 dye based FLIPR assayAgonist activity at human EP2 receptor expressed in HEK293 cells by calcium-5 dye based FLIPR assay
ChEMBL 439 11 2 4 5.0 CCCCCC(O)CCc1c(Cl)cc(Cl)c(=O)n1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2020.127104
CHEMBL4640635 184363 0 None -309 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human EP2 receptor expressed in HEK293 cells by calcium-5 dye based FLIPR assayAgonist activity at human EP2 receptor expressed in HEK293 cells by calcium-5 dye based FLIPR assay
ChEMBL 439 11 2 4 5.0 CCCCCC(O)CCc1c(Cl)cc(Cl)c(=O)n1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2020.127104
57464006 81943 0 None -288 2 Rat 5.8 pEC50 = 5.8 Functional
Agonist activity at rat EP2 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP2 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
ChEMBL 534 10 2 7 5.5 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(-c3cc4ccccc4o3)c2)n1 10.1016/j.bmc.2012.04.008
CHEMBL2036322 81943 0 None -288 2 Rat 5.8 pEC50 = 5.8 Functional
Agonist activity at rat EP2 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP2 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
ChEMBL 534 10 2 7 5.5 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(-c3cc4ccccc4o3)c2)n1 10.1016/j.bmc.2012.04.008
10269242 162354 0 None -54 2 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human prostaglandin EP2 receptorAgonist activity at human prostaglandin EP2 receptor
ChEMBL 348 9 2 4 2.2 CC(C)CC(O)CCN1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.09.074
CHEMBL404413 162354 0 None -54 2 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human prostaglandin EP2 receptorAgonist activity at human prostaglandin EP2 receptor
ChEMBL 348 9 2 4 2.2 CC(C)CC(O)CCN1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.09.074
59465577 149967 0 None - 1 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 408 13 2 2 6.8 CCCCCC(O)c1ccc([C@H]2CC[C@@H](Cl)[C@@H]2CCCCCCC(=O)O)cc1 nan
CHEMBL3896183 149967 0 None - 1 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 408 13 2 2 6.8 CCCCCC(O)c1ccc([C@H]2CC[C@@H](Cl)[C@@H]2CCCCCCC(=O)O)cc1 nan
59465570 150037 0 None - 1 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 392 13 2 2 6.6 CCCCCC(O)c1ccc([C@H]2CC[C@@H](F)[C@@H]2CCCCCCC(=O)O)cc1 nan
CHEMBL3896693 150037 0 None - 1 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 392 13 2 2 6.6 CCCCCC(O)c1ccc([C@H]2CC[C@@H](F)[C@@H]2CCCCCCC(=O)O)cc1 nan
134143292 152006 0 None - 1 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 408 12 1 3 6.5 CCCCC(O)c1ccc([C@H]2CC[C@@H](Cl)[C@@H]2CCCCCCC(=O)OC)cc1 nan
CHEMBL3912658 152006 0 None - 1 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 408 12 1 3 6.5 CCCCC(O)c1ccc([C@H]2CC[C@@H](Cl)[C@@H]2CCCCCCC(=O)OC)cc1 nan
59465574 152723 0 None 1 2 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 400 12 1 4 5.7 CCCCCC(O)c1ccc([C@H]2CCC(=O)[C@@H]2C/C=C\CCCC(=O)OC)cc1 nan
CHEMBL3918084 152723 0 None 1 2 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 400 12 1 4 5.7 CCCCCC(O)c1ccc([C@H]2CCC(=O)[C@@H]2C/C=C\CCCC(=O)OC)cc1 nan
59465601 156673 0 None - 1 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 402 13 1 4 5.4 CCCCC(O)Cc1ccc([C@H]2CCC(=O)[C@@H]2CCCCCCC(=O)OC)cc1 nan
CHEMBL3949271 156673 0 None - 1 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 402 13 1 4 5.4 CCCCC(O)Cc1ccc([C@H]2CCC(=O)[C@@H]2CCCCCCC(=O)OC)cc1 nan
58681356 157150 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 434 7 3 4 3.9 O=C(O)COCC#CCC1[C@@H](c2ccc(C(O)C3CCCCC3)cc2)[C@H](O)C[C@H]1Cl nan
CHEMBL3953307 157150 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 434 7 3 4 3.9 O=C(O)COCC#CCC1[C@@H](c2ccc(C(O)C3CCCCC3)cc2)[C@H](O)C[C@H]1Cl nan
44442327 101234 0 None -891 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at EP2 receptor expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at EP2 receptor expressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 345 9 2 3 3.0 CCCC[C@H](O)/C=C/[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.05.025
CHEMBL251294 101234 0 None -891 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at EP2 receptor expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at EP2 receptor expressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 345 9 2 3 3.0 CCCC[C@H](O)/C=C/[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.05.025
11855870 153058 0 None 467 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 427 11 1 4 5.7 CCCCCC(=O)c1ccc(N2C(=O)CC[C@@H]2CCCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3920756 153058 0 None 467 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 427 11 1 4 5.7 CCCCCC(=O)c1ccc(N2C(=O)CC[C@@H]2CCCc2ccc(C(=O)O)s2)cc1 nan
11855870 153058 0 None 467 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assayAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assay
ChEMBL 427 11 1 4 5.7 CCCCCC(=O)c1ccc(N2C(=O)CC[C@@H]2CCCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3920756 153058 0 None 467 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assayAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assay
ChEMBL 427 11 1 4 5.7 CCCCCC(=O)c1ccc(N2C(=O)CC[C@@H]2CCCc2ccc(C(=O)O)s2)cc1 nan
71515516 155085 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 387 7 2 3 4.8 O=C(O)COc1ccc(F)c(NCc2cccc(-c3cccc(F)c3)c2)c1F nan
CHEMBL3936868 155085 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 387 7 2 3 4.8 O=C(O)COc1ccc(F)c(NCc2cccc(-c3cccc(F)c3)c2)c1F nan
71516448 159339 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 421 7 3 4 4.7 O=C(O)COc1ccc(F)c(NCc2cc(O)cc(-c3cccc(F)c3)c2F)c1F nan
CHEMBL3971730 159339 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 421 7 3 4 4.7 O=C(O)COc1ccc(F)c(NCc2cc(O)cc(-c3cccc(F)c3)c2F)c1F nan
57893848 81944 0 None -724 2 Rat 5.8 pEC50 = 5.8 Functional
Agonist activity at rat EP2 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP2 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
ChEMBL 535 10 2 8 4.9 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(-c3nc4ccccc4o3)c2)n1 10.1016/j.bmc.2012.04.008
CHEMBL2036323 81944 0 None -724 2 Rat 5.8 pEC50 = 5.8 Functional
Agonist activity at rat EP2 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP2 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
ChEMBL 535 10 2 8 4.9 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(-c3nc4ccccc4o3)c2)n1 10.1016/j.bmc.2012.04.008
118517488 160490 0 None -14 3 Human 6.8 pEC50 = 6.8 Functional
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
ChEMBL 414 8 2 3 4.4 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2cccc(F)c2F)cc1 nan
CHEMBL3981554 160490 0 None -14 3 Human 6.8 pEC50 = 6.8 Functional
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
ChEMBL 414 8 2 3 4.4 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2cccc(F)c2F)cc1 nan
58708286 161123 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 398 9 2 3 5.6 O=C(O)CCC/C=C\C[C@H]1C(=O)CC[C@@H]1c1ccc([C@H](O)C2CCCCC2)cc1 nan
CHEMBL3986874 161123 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 398 9 2 3 5.6 O=C(O)CCC/C=C\C[C@H]1C(=O)CC[C@@H]1c1ccc([C@H](O)C2CCCCC2)cc1 nan
1929 8386 55 None -2 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 468 9 1 5 4.2 OC(=O)COc1cccc(c1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)C(C)(C)C 10.1021/acs.jmedchem.8b00808
9890801 8386 55 None -2 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 468 9 1 5 4.2 OC(=O)COc1cccc(c1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)C(C)(C)C 10.1021/acs.jmedchem.8b00808
CHEMBL563646 8386 55 None -2 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 468 9 1 5 4.2 OC(=O)COc1cccc(c1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)C(C)(C)C 10.1021/acs.jmedchem.8b00808
DB12022 8386 55 None -2 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 468 9 1 5 4.2 OC(=O)COc1cccc(c1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)C(C)(C)C 10.1021/acs.jmedchem.8b00808
89444254 149558 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 423 7 2 3 5.1 O=C(O)COc1ccc(F)c(NCc2c(F)ccc(-c3cccc(F)c3)c2F)c1F nan
CHEMBL3892751 149558 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 423 7 2 3 5.1 O=C(O)COc1ccc(F)c(NCc2c(F)ccc(-c3cccc(F)c3)c2F)c1F nan
89443784 149684 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 431 8 2 4 5.2 COc1c(C)cc(-c2cccc(F)c2)cc1CNc1c(F)ccc(OCC(=O)O)c1F nan
CHEMBL3893770 149684 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 431 8 2 4 5.2 COc1c(C)cc(-c2cccc(F)c2)cc1CNc1c(F)ccc(OCC(=O)O)c1F nan
89444126 154166 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 403 7 3 4 4.6 O=C(O)COc1ccc(F)c(NCc2cc(O)cc(-c3cccc(F)c3)c2)c1F nan
CHEMBL3929662 154166 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 403 7 3 4 4.6 O=C(O)COc1ccc(F)c(NCc2cc(O)cc(-c3cccc(F)c3)c2)c1F nan
11955383 149311 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 358 7 2 3 4.2 CC(C)(C)c1ccc([C@H]2[C@H](O)CC(=O)[C@@H]2C/C=C\CCCC(=O)O)cc1 nan
CHEMBL3890808 149311 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 358 7 2 3 4.2 CC(C)(C)c1ccc([C@H]2[C@H](O)CC(=O)[C@@H]2C/C=C\CCCC(=O)O)cc1 nan
53260155 178183 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 494 11 2 6 4.1 CC(C)C1(c2ccc(CN(Cc3cccc(NCC(=O)O)n3)S(=O)(=O)c3cccnc3)cc2)CC1 10.1021/acs.jmedchem.8b00808
CHEMBL4462507 178183 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 494 11 2 6 4.1 CC(C)C1(c2ccc(CN(Cc3cccc(NCC(=O)O)n3)S(=O)(=O)c3cccnc3)cc2)CC1 10.1021/acs.jmedchem.8b00808
117703250 150417 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 419 7 2 3 5.5 C[C@@H](Nc1c(F)ccc(OCC(=O)O)c1F)c1cc(-c2cccc(F)c2)ccc1F nan
CHEMBL3899837 150417 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 419 7 2 3 5.5 C[C@@H](Nc1c(F)ccc(OCC(=O)O)c1F)c1cc(-c2cccc(F)c2)ccc1F nan
89444132 150644 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 417 8 2 4 4.9 COc1cc(CNc2c(F)ccc(OCC(=O)O)c2F)cc(-c2cccc(F)c2)c1 nan
CHEMBL3901709 150644 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 417 8 2 4 4.9 COc1cc(CNc2c(F)ccc(OCC(=O)O)c2F)cc(-c2cccc(F)c2)c1 nan
89443635 158683 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 415 7 2 3 5.5 Cc1cc(OCC(=O)O)c(C)c(NCc2cc(-c3cccc(F)c3)ccc2F)c1F nan
CHEMBL3965998 158683 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 415 7 2 3 5.5 Cc1cc(OCC(=O)O)c(C)c(NCc2cc(-c3cccc(F)c3)ccc2F)c1F nan
57394893 78081 0 None -223 2 Rat 5.8 pEC50 = 5.8 Functional
Agonist activity at rat EP2 receptorAgonist activity at rat EP2 receptor
ChEMBL 494 10 2 6 4.8 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(-c3ccccc3)c2)n1 10.1016/j.bmc.2012.02.018
CHEMBL1957435 78081 0 None -223 2 Rat 5.8 pEC50 = 5.8 Functional
Agonist activity at rat EP2 receptorAgonist activity at rat EP2 receptor
ChEMBL 494 10 2 6 4.8 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(-c3ccccc3)c2)n1 10.1016/j.bmc.2012.02.018
10291963 91483 0 None -3801 4 Rat 5.8 pEC50 = 5.8 Functional
Agonist activity at rat EP2 receptorAgonist activity at rat EP2 receptor
ChEMBL 359 10 2 3 3.4 CCCCC[C@H](O)/C=C/[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmc.2012.02.018
CHEMBL222715 91483 0 None -3801 4 Rat 5.8 pEC50 = 5.8 Functional
Agonist activity at rat EP2 receptorAgonist activity at rat EP2 receptor
ChEMBL 359 10 2 3 3.4 CCCCC[C@H](O)/C=C/[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmc.2012.02.018
57394893 78081 0 None -223 2 Rat 5.8 pEC50 = 5.8 Functional
Agonist activity at rat EP2 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP2 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
ChEMBL 494 10 2 6 4.8 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(-c3ccccc3)c2)n1 10.1016/j.bmc.2012.04.008
CHEMBL1957435 78081 0 None -223 2 Rat 5.8 pEC50 = 5.8 Functional
Agonist activity at rat EP2 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP2 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
ChEMBL 494 10 2 6 4.8 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(-c3ccccc3)c2)n1 10.1016/j.bmc.2012.04.008
11855867 152761 0 None 10 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 389 8 2 5 3.6 CCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3918349 152761 0 None 10 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 389 8 2 5 3.6 CCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
11855867 152761 0 None 10 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assayAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assay
ChEMBL 389 8 2 5 3.6 CCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3918349 152761 0 None 10 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assayAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assay
ChEMBL 389 8 2 5 3.6 CCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
44455115 102337 0 None -6 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human EP2 receptor by cAMP assayAgonist activity at human EP2 receptor by cAMP assay
ChEMBL 387 10 2 3 4.1 CCCCC(C)(C)[C@H](O)/C=C/[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.11.020
CHEMBL257658 102337 0 None -6 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human EP2 receptor by cAMP assayAgonist activity at human EP2 receptor by cAMP assay
ChEMBL 387 10 2 3 4.1 CCCCC(C)(C)[C@H](O)/C=C/[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.11.020
1883 9856 75 None -2 12 Rat 7.7 pEC50 = 7.7 Functional
Agonist activity at rat EP2 receptorAgonist activity at rat EP2 receptor
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmc.2012.02.018
1916 9856 75 None -2 12 Rat 7.7 pEC50 = 7.7 Functional
Agonist activity at rat EP2 receptorAgonist activity at rat EP2 receptor
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmc.2012.02.018
5280360 9856 75 None -2 12 Rat 7.7 pEC50 = 7.7 Functional
Agonist activity at rat EP2 receptorAgonist activity at rat EP2 receptor
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmc.2012.02.018
913 9856 75 None -2 12 Rat 7.7 pEC50 = 7.7 Functional
Agonist activity at rat EP2 receptorAgonist activity at rat EP2 receptor
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmc.2012.02.018
CHEMBL548 9856 75 None -2 12 Rat 7.7 pEC50 = 7.7 Functional
Agonist activity at rat EP2 receptorAgonist activity at rat EP2 receptor
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmc.2012.02.018
DB00917 9856 75 None -2 12 Rat 7.7 pEC50 = 7.7 Functional
Agonist activity at rat EP2 receptorAgonist activity at rat EP2 receptor
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmc.2012.02.018
53259985 183256 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 497 10 2 6 4.3 COc1ccc(S(=O)(=O)N(Cc2ccc(C(C)(C)C)cc2)Cc2cccc(NCC(=O)O)n2)cc1 10.1021/acs.jmedchem.8b00808
CHEMBL4548451 183256 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 497 10 2 6 4.3 COc1ccc(S(=O)(=O)N(Cc2ccc(C(C)(C)C)cc2)Cc2cccc(NCC(=O)O)n2)cc1 10.1021/acs.jmedchem.8b00808
CHEMBL4596602 183256 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 497 10 2 6 4.3 COc1ccc(S(=O)(=O)N(Cc2ccc(C(C)(C)C)cc2)Cc2cccc(NCC(=O)O)n2)cc1 10.1021/acs.jmedchem.8b00808
44442332 101302 0 None -97 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at EP2 receptor expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at EP2 receptor expressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 341 9 1 2 4.2 CCCC/C=C\C=C\[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.05.025
CHEMBL251709 101302 0 None -97 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at EP2 receptor expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at EP2 receptor expressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 341 9 1 2 4.2 CCCC/C=C\C=C\[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.05.025
127026952 146139 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assayAgonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assay
ChEMBL 451 6 2 6 4.9 CC(C)c1cc(OC[C@H]2[C@H](O)C[C@@H]3O[C@@H](c4nc(C(=O)O)cs4)CC[C@@H]32)ccc1Cl 10.1016/j.bmcl.2016.03.110
CHEMBL3793020 146139 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assayAgonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assay
ChEMBL 451 6 2 6 4.9 CC(C)c1cc(OC[C@H]2[C@H](O)C[C@@H]3O[C@@H](c4nc(C(=O)O)cs4)CC[C@@H]32)ccc1Cl 10.1016/j.bmcl.2016.03.110
59465581 150890 0 None 22 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 428 11 2 4 6.1 CCCCCC(O)c1ccc([C@H]2CCC(=O)[C@@H]2CCCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3903611 150890 0 None 22 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 428 11 2 4 6.1 CCCCCC(O)c1ccc([C@H]2CCC(=O)[C@@H]2CCCc2ccc(C(=O)O)s2)cc1 nan
145966519 171178 0 None 15 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at recombinant human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIAAgonist activity at recombinant human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIA
ChEMBL 437 10 2 6 5.2 C[C@](O)(C/C=C/[C@H]1CCC(=O)[C@@H]1CCSc1nc(C(=O)O)cs1)CC1CCCC1 10.1016/j.bmc.2017.11.035
CHEMBL4213312 171178 0 None 15 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at recombinant human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIAAgonist activity at recombinant human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIA
ChEMBL 437 10 2 6 5.2 C[C@](O)(C/C=C/[C@H]1CCC(=O)[C@@H]1CCSc1nc(C(=O)O)cs1)CC1CCCC1 10.1016/j.bmc.2017.11.035
44230429 183107 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 488 10 2 6 4.0 O=C(O)CNc1cccc(CN(Cc2ccc(-c3ccccc3)cc2)S(=O)(=O)c2cccnc2)n1 10.1021/acs.jmedchem.8b00808
CHEMBL4471378 183107 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 488 10 2 6 4.0 O=C(O)CNc1cccc(CN(Cc2ccc(-c3ccccc3)cc2)S(=O)(=O)c2cccnc2)n1 10.1021/acs.jmedchem.8b00808
CHEMBL4595426 183107 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 488 10 2 6 4.0 O=C(O)CNc1cccc(CN(Cc2ccc(-c3ccccc3)cc2)S(=O)(=O)c2cccnc2)n1 10.1021/acs.jmedchem.8b00808
89443841 152673 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 407 7 2 3 5.8 Cc1cc(-c2cccc(F)c2)cc(CNc2c(C)ccc(OCC(=O)O)c2C)c1C nan
CHEMBL3917749 152673 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 407 7 2 3 5.8 Cc1cc(-c2cccc(F)c2)cc(CNc2c(C)ccc(OCC(=O)O)c2C)c1C nan
89444231 152891 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 415 7 2 3 5.5 Cc1cc(-c2cccc(F)c2)cc(CNc2c(F)ccc(OCC(=O)O)c2F)c1C nan
CHEMBL3919482 152891 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 415 7 2 3 5.5 Cc1cc(-c2cccc(F)c2)cc(CNc2c(F)ccc(OCC(=O)O)c2F)c1C nan
89443843 155576 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 433 7 2 3 5.6 Cc1cc(-c2ccc(F)c(F)c2)cc(CNc2c(F)ccc(OCC(=O)O)c2F)c1C nan
CHEMBL3940781 155576 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 433 7 2 3 5.6 Cc1cc(-c2ccc(F)c(F)c2)cc(CNc2c(F)ccc(OCC(=O)O)c2F)c1C nan
89443583 157257 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 415 7 2 3 5.5 Cc1cc(-c2cccc(F)c2)cc(CNc2c(F)ccc(OCC(=O)O)c2C)c1F nan
CHEMBL3954347 157257 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 415 7 2 3 5.5 Cc1cc(-c2cccc(F)c2)cc(CNc2c(F)ccc(OCC(=O)O)c2C)c1F nan
66857988 170901 0 None 1 3 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at recombinant human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIAAgonist activity at recombinant human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIA
ChEMBL 428 12 2 7 4.0 CCCCCC(C)(O)C/C=C/[C@H]1COC(=O)N1CCSc1nc(C(=O)O)cs1 10.1016/j.bmc.2017.11.035
CHEMBL4209929 170901 0 None 1 3 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at recombinant human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIAAgonist activity at recombinant human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIA
ChEMBL 428 12 2 7 4.0 CCCCCC(C)(O)C/C=C/[C@H]1COC(=O)N1CCSc1nc(C(=O)O)cs1 10.1016/j.bmc.2017.11.035
5283086 210089 24 None -10 4 Mouse 8.7 pEC50 = 8.7 Functional
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptor
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](O)/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O 10.1016/s0960-894x(01)00359-6
CHEMBL64804 210089 24 None -10 4 Mouse 8.7 pEC50 = 8.7 Functional
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptor
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](O)/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O 10.1016/s0960-894x(01)00359-6
118352285 146247 0 None 2398 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assayAgonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assay
ChEMBL 406 5 2 5 4.2 Cc1cc(OC[C@H]2[C@H](O)C[C@@H]3O[C@@H](c4ccc(C(=O)O)o4)CC[C@@H]32)ccc1Cl 10.1016/j.bmcl.2016.03.110
CHEMBL3794226 146247 0 None 2398 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assayAgonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assay
ChEMBL 406 5 2 5 4.2 Cc1cc(OC[C@H]2[C@H](O)C[C@@H]3O[C@@H](c4ccc(C(=O)O)o4)CC[C@@H]32)ccc1Cl 10.1016/j.bmcl.2016.03.110
18376196 201701 0 None - 1 Rat 8.6 pEC50 = 8.6 Functional
Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP releaseAgonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release
ChEMBL 466 9 1 4 4.8 CC(C)(C)c1ccc(CN(Cc2cccc(CCC(=O)O)c2)S(=O)(=O)c2ccccn2)cc1 10.1016/j.bmcl.2009.01.059
CHEMBL541516 201701 0 None - 1 Rat 8.6 pEC50 = 8.6 Functional
Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP releaseAgonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release
ChEMBL 466 9 1 4 4.8 CC(C)(C)c1ccc(CN(Cc2cccc(CCC(=O)O)c2)S(=O)(=O)c2ccccn2)cc1 10.1016/j.bmcl.2009.01.059
70815687 183325 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 466 10 2 6 3.4 CC1(c2ccc(CN(Cc3cccc(NCC(=O)O)n3)S(=O)(=O)c3cccnc3)cc2)CC1 10.1021/acs.jmedchem.8b00808
CHEMBL4515583 183325 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 466 10 2 6 3.4 CC1(c2ccc(CN(Cc3cccc(NCC(=O)O)n3)S(=O)(=O)c3cccnc3)cc2)CC1 10.1021/acs.jmedchem.8b00808
CHEMBL4597208 183325 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 466 10 2 6 3.4 CC1(c2ccc(CN(Cc3cccc(NCC(=O)O)n3)S(=O)(=O)c3cccnc3)cc2)CC1 10.1021/acs.jmedchem.8b00808
138 9855 88 None -1 10 Mouse 8.6 pEC50 = 8.6 Functional
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptor
ChEMBL 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 10.1016/s0960-894x(01)00359-6
149351 9855 88 None -1 10 Mouse 8.6 pEC50 = 8.6 Functional
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptor
ChEMBL 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 10.1016/s0960-894x(01)00359-6
1882 9855 88 None -1 10 Mouse 8.6 pEC50 = 8.6 Functional
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptor
ChEMBL 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 10.1016/s0960-894x(01)00359-6
5280723 9855 88 None -1 10 Mouse 8.6 pEC50 = 8.6 Functional
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptor
ChEMBL 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 10.1016/s0960-894x(01)00359-6
CHEMBL495 9855 88 None -1 10 Mouse 8.6 pEC50 = 8.6 Functional
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptor
ChEMBL 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 10.1016/s0960-894x(01)00359-6
DB00770 9855 88 None -1 10 Mouse 8.6 pEC50 = 8.6 Functional
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptor
ChEMBL 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 10.1016/s0960-894x(01)00359-6
53260134 183041 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 485 9 2 5 4.4 CC(C)(C)c1ccc(CN(Cc2cccc(NCC(=O)O)n2)S(=O)(=O)c2ccc(F)cc2)cc1 10.1021/acs.jmedchem.8b00808
CHEMBL4466224 183041 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 485 9 2 5 4.4 CC(C)(C)c1ccc(CN(Cc2cccc(NCC(=O)O)n2)S(=O)(=O)c2ccc(F)cc2)cc1 10.1021/acs.jmedchem.8b00808
CHEMBL4594970 183041 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 485 9 2 5 4.4 CC(C)(C)c1ccc(CN(Cc2cccc(NCC(=O)O)n2)S(=O)(=O)c2ccc(F)cc2)cc1 10.1021/acs.jmedchem.8b00808
53259986 183299 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 468 9 2 6 3.7 CC(C)(C)c1ccc(CN(Cc2cccc(NCC(=O)O)n2)S(=O)(=O)c2ccccn2)cc1 10.1021/acs.jmedchem.8b00808
CHEMBL4442505 183299 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 468 9 2 6 3.7 CC(C)(C)c1ccc(CN(Cc2cccc(NCC(=O)O)n2)S(=O)(=O)c2ccccn2)cc1 10.1021/acs.jmedchem.8b00808
CHEMBL4596979 183299 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 468 9 2 6 3.7 CC(C)(C)c1ccc(CN(Cc2cccc(NCC(=O)O)n2)S(=O)(=O)c2ccccn2)cc1 10.1021/acs.jmedchem.8b00808
53259987 183277 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 468 9 2 6 3.7 CC(C)(C)c1ccc(CN(Cc2cccc(NCC(=O)O)n2)S(=O)(=O)c2cccnc2)cc1 10.1021/acs.jmedchem.8b00808
CHEMBL4591201 183277 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 468 9 2 6 3.7 CC(C)(C)c1ccc(CN(Cc2cccc(NCC(=O)O)n2)S(=O)(=O)c2cccnc2)cc1 10.1021/acs.jmedchem.8b00808
CHEMBL4596748 183277 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 468 9 2 6 3.7 CC(C)(C)c1ccc(CN(Cc2cccc(NCC(=O)O)n2)S(=O)(=O)c2cccnc2)cc1 10.1021/acs.jmedchem.8b00808
9807448 209951 0 None 1 2 Mouse 8.6 pEC50 = 8.6 Functional
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptor
ChEMBL 398 11 3 3 4.7 CCC1([C@@H](O)C/C=C/[C@H]2[C@H](O)C[C@@H](Cl)[C@@H]2C/C=C\CCCC(=O)O)CCC1 10.1016/s0960-894x(01)00359-6
CHEMBL64246 209951 0 None 1 2 Mouse 8.6 pEC50 = 8.6 Functional
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptor
ChEMBL 398 11 3 3 4.7 CCC1([C@@H](O)C/C=C/[C@H]2[C@H](O)C[C@@H](Cl)[C@@H]2C/C=C\CCCC(=O)O)CCC1 10.1016/s0960-894x(01)00359-6
118352215 146195 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assayAgonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assay
ChEMBL 403 5 2 6 3.8 Cc1ccc(OC[C@H]2[C@H](O)C[C@@H]3O[C@@H](c4nc(C(=O)O)cs4)CC[C@@H]32)cc1C 10.1016/j.bmcl.2016.03.110
CHEMBL3793797 146195 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assayAgonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assay
ChEMBL 403 5 2 6 3.8 Cc1ccc(OC[C@H]2[C@H](O)C[C@@H]3O[C@@H](c4nc(C(=O)O)cs4)CC[C@@H]32)cc1C 10.1016/j.bmcl.2016.03.110
11855865 160056 0 None 35 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assayAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assay
ChEMBL 445 12 2 5 5.2 CCCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3977724 160056 0 None 35 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assayAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assay
ChEMBL 445 12 2 5 5.2 CCCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
10126807 201877 0 None - 1 Rat 6.7 pEC50 = 6.7 Functional
Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP releaseAgonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release
ChEMBL 405 8 1 4 3.4 CC(C)(C)c1ccc(CN(Cc2cccc(OCC(=O)O)c2)S(C)(=O)=O)cc1 10.1016/j.bmcl.2009.01.059
CHEMBL549869 201877 0 None - 1 Rat 6.7 pEC50 = 6.7 Functional
Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP releaseAgonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release
ChEMBL 405 8 1 4 3.4 CC(C)(C)c1ccc(CN(Cc2cccc(OCC(=O)O)c2)S(C)(=O)=O)cc1 10.1016/j.bmcl.2009.01.059
11955273 159566 0 None - 1 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 438 10 3 4 4.6 O=C(O)COCCCC[C@@H]1[C@@H](c2ccc(C(O)C3CCCCC3)cc2)[C@H](O)C[C@H]1Cl nan
CHEMBL3973644 159566 0 None - 1 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 438 10 3 4 4.6 O=C(O)COCCCC[C@@H]1[C@@H](c2ccc(C(O)C3CCCCC3)cc2)[C@H](O)C[C@H]1Cl nan
138107701 194243 46 None -1348 7 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human EP2 expressed in HEK293 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysisAgonist activity at human EP2 expressed in HEK293 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysis
ChEMBL 360 8 3 3 3.5 CC#CCC(C)[C@H](O)/C=C/[C@@H]1[C@H]2C/C(=C/CCCC(=O)O)C[C@H]2C[C@H]1O 10.1016/j.ejmech.2022.114154
5311181 194243 46 None -1348 7 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human EP2 expressed in HEK293 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysisAgonist activity at human EP2 expressed in HEK293 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysis
ChEMBL 360 8 3 3 3.5 CC#CCC(C)[C@H](O)/C=C/[C@@H]1[C@H]2C/C(=C/CCCC(=O)O)C[C@H]2C[C@H]1O 10.1016/j.ejmech.2022.114154
CHEMBL494 194243 46 None -1348 7 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human EP2 expressed in HEK293 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysisAgonist activity at human EP2 expressed in HEK293 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysis
ChEMBL 360 8 3 3 3.5 CC#CCC(C)[C@H](O)/C=C/[C@@H]1[C@H]2C/C(=C/CCCC(=O)O)C[C@H]2C[C@H]1O 10.1016/j.ejmech.2022.114154
DB01088 194243 46 None -1348 7 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human EP2 expressed in HEK293 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysisAgonist activity at human EP2 expressed in HEK293 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysis
ChEMBL 360 8 3 3 3.5 CC#CCC(C)[C@H](O)/C=C/[C@@H]1[C@H]2C/C(=C/CCCC(=O)O)C[C@H]2C[C@H]1O 10.1016/j.ejmech.2022.114154
59465583 150052 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 398 9 2 3 5.6 O=C(O)CCC/C=C\C[C@H]1C(=O)CC[C@@H]1c1ccc(C(O)C2CCCCC2)cc1 nan
CHEMBL3896863 150052 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 398 9 2 3 5.6 O=C(O)CCC/C=C\C[C@H]1C(=O)CC[C@@H]1c1ccc(C(O)C2CCCCC2)cc1 nan
11855594 159759 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 417 10 2 5 4.4 CCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3975238 159759 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 417 10 2 5 4.4 CCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
11855594 159759 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assayAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assay
ChEMBL 417 10 2 5 4.4 CCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3975238 159759 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assayAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assay
ChEMBL 417 10 2 5 4.4 CCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
11855871 153186 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 429 11 1 5 4.9 CCCCCC(=O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3921784 153186 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 429 11 1 5 4.9 CCCCCC(=O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
11855871 153186 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assayAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assay
ChEMBL 429 11 1 5 4.9 CCCCCC(=O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3921784 153186 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assayAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assay
ChEMBL 429 11 1 5 4.9 CCCCCC(=O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
54013831 153238 0 None 1 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 402 13 1 4 5.9 CCCCCC(O)c1ccc([C@H]2CCC(=O)[C@@H]2CCCCCCC(=O)OC)cc1 nan
CHEMBL3922151 153238 0 None 1 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 402 13 1 4 5.9 CCCCCC(O)c1ccc([C@H]2CCC(=O)[C@@H]2CCCCCCC(=O)OC)cc1 nan
10363130 107812 1 None - 1 Mouse 6.7 pEC50 = 6.7 Functional
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptor
ChEMBL 392 12 3 4 4.0 CCCC1([C@@H](O)C/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2C/C=C\CCCC(=O)O)CCC1 10.1016/s0960-894x(01)00359-6
CHEMBL294585 107812 1 None - 1 Mouse 6.7 pEC50 = 6.7 Functional
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptor
ChEMBL 392 12 3 4 4.0 CCCC1([C@@H](O)C/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2C/C=C\CCCC(=O)O)CCC1 10.1016/s0960-894x(01)00359-6
9975502 101264 0 None -14 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at EP2 receptor expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at EP2 receptor expressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 355 9 1 2 4.6 CCCC/C(C)=C/C=C/[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.05.025
CHEMBL251504 101264 0 None -14 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at EP2 receptor expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at EP2 receptor expressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 355 9 1 2 4.6 CCCC/C(C)=C/C=C/[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.05.025
24760052 157964 0 None 24 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 427 10 2 4 5.4 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2/C=C/Cc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3959769 157964 0 None 24 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 427 10 2 4 5.4 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2/C=C/Cc2ccc(C(=O)O)s2)cc1 nan
70667255 158253 0 None 24 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assayAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assay
ChEMBL 427 10 2 4 5.4 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2C=CCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3962183 158253 0 None 24 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assayAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assay
ChEMBL 427 10 2 4 5.4 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2C=CCc2ccc(C(=O)O)s2)cc1 nan
72950089 157370 0 None -4365 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human EP2 receptor expressed in HEK293T/17 cells assessed as increase in GalphaS-mediated CREB activation measured after 6 to 24 hrs by SEAP reporter gene-based chemiluminescence assayAgonist activity at human EP2 receptor expressed in HEK293T/17 cells assessed as increase in GalphaS-mediated CREB activation measured after 6 to 24 hrs by SEAP reporter gene-based chemiluminescence assay
ChEMBL 375 13 2 3 3.8 CCCCC[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCCCCC(=O)O 10.1021/acs.jmedchem.9b00336
CHEMBL3955128 157370 0 None -4365 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human EP2 receptor expressed in HEK293T/17 cells assessed as increase in GalphaS-mediated CREB activation measured after 6 to 24 hrs by SEAP reporter gene-based chemiluminescence assayAgonist activity at human EP2 receptor expressed in HEK293T/17 cells assessed as increase in GalphaS-mediated CREB activation measured after 6 to 24 hrs by SEAP reporter gene-based chemiluminescence assay
ChEMBL 375 13 2 3 3.8 CCCCC[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCCCCC(=O)O 10.1021/acs.jmedchem.9b00336
11955180 158439 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 448 11 3 3 6.0 CCCC1(C(O)c2ccc([C@H]3[C@H](O)C[C@@H](Cl)[C@@H]3C/C=C\CCCC(=O)O)cc2)CCC1 nan
CHEMBL3963968 158439 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 448 11 3 3 6.0 CCCC1(C(O)c2ccc([C@H]3[C@H](O)C[C@@H](Cl)[C@@H]3C/C=C\CCCC(=O)O)cc2)CCC1 nan
10089562 161201 0 None -1 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at EP2 receptor expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at EP2 receptor expressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 355 9 1 2 4.6 CCCC/C=C(C)/C=C/[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.05.025
CHEMBL398948 161201 0 None -1 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at EP2 receptor expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at EP2 receptor expressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 355 9 1 2 4.6 CCCC/C=C(C)/C=C/[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.05.025
118352177 146190 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assayAgonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assay
ChEMBL 437 6 1 6 4.8 CO[C@H]1C[C@@H]2O[C@@H](c3nc(C(=O)O)cs3)CC[C@@H]2[C@H]1COc1ccc(Cl)c(C)c1 10.1016/j.bmcl.2016.03.110
CHEMBL3793724 146190 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assayAgonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assay
ChEMBL 437 6 1 6 4.8 CO[C@H]1C[C@@H]2O[C@@H](c3nc(C(=O)O)cs3)CC[C@@H]2[C@H]1COc1ccc(Cl)c(C)c1 10.1016/j.bmcl.2016.03.110
127051064 147077 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
ChEMBL 393 5 2 6 3.3 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3COc3ccccc3F)O2)n1 10.1021/acsmedchemlett.5b00455
CHEMBL3806060 147077 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
ChEMBL 393 5 2 6 3.3 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3COc3ccccc3F)O2)n1 10.1021/acsmedchemlett.5b00455
89443417 158371 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 421 7 2 3 5.5 O=C(O)COc1ccc(F)c(NCc2cc(-c3cccc(F)c3)ccc2Cl)c1F nan
CHEMBL3963438 158371 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 421 7 2 3 5.5 O=C(O)COc1ccc(F)c(NCc2cc(-c3cccc(F)c3)ccc2Cl)c1F nan
44455046 102502 0 None -8317 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human EP2 receptor by cAMP assayAgonist activity at human EP2 receptor by cAMP assay
ChEMBL 413 8 2 3 3.7 O=C(O)c1ccc(CCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2007.11.020
CHEMBL258332 102502 0 None -8317 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human EP2 receptor by cAMP assayAgonist activity at human EP2 receptor by cAMP assay
ChEMBL 413 8 2 3 3.7 O=C(O)c1ccc(CCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2007.11.020
56839536 149947 0 None -141 7 Human 5.6 pEC50 = 5.6 Functional
Cell Based Assay: Ca2+ signaling studies were performed using a FLIPR TETRA system (Molecular Devices, Sunnyvale, Calif., USA) in the 384-format. This is a high-throughput instrument for cell-based assays to monitor Ca2+ signaling associated with GPCRs and ion channels. Cells were seeded at a density of 5×104 cells/well in BioCoat poly-D-lysine coated, black wall, clear bottom 384-well plates (BD Biosciences, Franklin lakes, NJ, USA) and allowed to attach overnight in an incubator at 37° C. The cells were then washed twice with HBSS-HEPES buffer (Hanks' balanced salt solution without bicarbonate and phenol red, 20 mM HEPES, pH 7.4) using an ELx405 Select CW Microplate Washer (BioTek, Winooski, Vt., USA). After 60 min of dye-loading in the dark using the Ca2+-sensitive dye Fluo-4AM (Invitrogen, Carlsbad, Calif., USA), at a final concentration of 2×10^−6M, the plates were washed 4 times with HBSS-HEPES buffer to remove excess dye and leaving 50 μl of buffer in each well. The plates were then placed in the FLIPR TETRA instrument and allowed to equilibrate at 37° C. AGN-211377 was added in a 25 μl volume to each well to give final concentrations of 0.1 μM, 0.3 μM, 1 μM, 3 μM, 10 μM, and 30 μM; or 0.067 μM, 0.1 μM, 0.2 μM, 0.3 μM, 0.67 μM, and 1 μM for cells over-expressing TP receptors. After 4.5 minutes, a 7-point serial dilution of the standard agonist for the corresponding receptor, in a 25 μl volume was injected at the final concentrations from 10^−11M to 10^−5M in 10-fold serial dilution increments for cells expressing human recombinant DP1, EP1, EP2, EP3, EP4, FP, and IP receptors. The dose range for the standard agonist for human recombinant TP receptors was from 10^−12M to 10^−6M. HBSS-HEPES buffer was used as the negative control for the standard agonists. Cells were excited with LED (light emitting diode) excitation at 470-495 nm and emission was measured through an emission filter at 515-575 nm. Assay plates were read for 3.5 minutes using the FLIPRTETRA.Cell Based Assay: Ca2+ signaling studies were performed using a FLIPR TETRA system (Molecular Devices, Sunnyvale, Calif., USA) in the 384-format. This is a high-throughput instrument for cell-based assays to monitor Ca2+ signaling associated with GPCRs and ion channels. Cells were seeded at a density of 5×104 cells/well in BioCoat poly-D-lysine coated, black wall, clear bottom 384-well plates (BD Biosciences, Franklin lakes, NJ, USA) and allowed to attach overnight in an incubator at 37° C. The cells were then washed twice with HBSS-HEPES buffer (Hanks' balanced salt solution without bicarbonate and phenol red, 20 mM HEPES, pH 7.4) using an ELx405 Select CW Microplate Washer (BioTek, Winooski, Vt., USA). After 60 min of dye-loading in the dark using the Ca2+-sensitive dye Fluo-4AM (Invitrogen, Carlsbad, Calif., USA), at a final concentration of 2×10^−6M, the plates were washed 4 times with HBSS-HEPES buffer to remove excess dye and leaving 50 μl of buffer in each well. The plates were then placed in the FLIPR TETRA instrument and allowed to equilibrate at 37° C. AGN-211377 was added in a 25 μl volume to each well to give final concentrations of 0.1 μM, 0.3 μM, 1 μM, 3 μM, 10 μM, and 30 μM; or 0.067 μM, 0.1 μM, 0.2 μM, 0.3 μM, 0.67 μM, and 1 μM for cells over-expressing TP receptors. After 4.5 minutes, a 7-point serial dilution of the standard agonist for the corresponding receptor, in a 25 μl volume was injected at the final concentrations from 10^−11M to 10^−5M in 10-fold serial dilution increments for cells expressing human recombinant DP1, EP1, EP2, EP3, EP4, FP, and IP receptors. The dose range for the standard agonist for human recombinant TP receptors was from 10^−12M to 10^−6M. HBSS-HEPES buffer was used as the negative control for the standard agonists. Cells were excited with LED (light emitting diode) excitation at 470-495 nm and emission was measured through an emission filter at 515-575 nm. Assay plates were read for 3.5 minutes using the FLIPRTETRA.
ChEMBL 604 15 2 7 5.1 CCCCCCCCNC(=O)c1coc([C@@H]2CCCN2Cc2cc(F)ccc2CCC(=O)NS(=O)(=O)C(F)(F)F)n1 nan
CHEMBL3896035 149947 0 None -141 7 Human 5.6 pEC50 = 5.6 Functional
Cell Based Assay: Ca2+ signaling studies were performed using a FLIPR TETRA system (Molecular Devices, Sunnyvale, Calif., USA) in the 384-format. This is a high-throughput instrument for cell-based assays to monitor Ca2+ signaling associated with GPCRs and ion channels. Cells were seeded at a density of 5×104 cells/well in BioCoat poly-D-lysine coated, black wall, clear bottom 384-well plates (BD Biosciences, Franklin lakes, NJ, USA) and allowed to attach overnight in an incubator at 37° C. The cells were then washed twice with HBSS-HEPES buffer (Hanks' balanced salt solution without bicarbonate and phenol red, 20 mM HEPES, pH 7.4) using an ELx405 Select CW Microplate Washer (BioTek, Winooski, Vt., USA). After 60 min of dye-loading in the dark using the Ca2+-sensitive dye Fluo-4AM (Invitrogen, Carlsbad, Calif., USA), at a final concentration of 2×10^−6M, the plates were washed 4 times with HBSS-HEPES buffer to remove excess dye and leaving 50 μl of buffer in each well. The plates were then placed in the FLIPR TETRA instrument and allowed to equilibrate at 37° C. AGN-211377 was added in a 25 μl volume to each well to give final concentrations of 0.1 μM, 0.3 μM, 1 μM, 3 μM, 10 μM, and 30 μM; or 0.067 μM, 0.1 μM, 0.2 μM, 0.3 μM, 0.67 μM, and 1 μM for cells over-expressing TP receptors. After 4.5 minutes, a 7-point serial dilution of the standard agonist for the corresponding receptor, in a 25 μl volume was injected at the final concentrations from 10^−11M to 10^−5M in 10-fold serial dilution increments for cells expressing human recombinant DP1, EP1, EP2, EP3, EP4, FP, and IP receptors. The dose range for the standard agonist for human recombinant TP receptors was from 10^−12M to 10^−6M. HBSS-HEPES buffer was used as the negative control for the standard agonists. Cells were excited with LED (light emitting diode) excitation at 470-495 nm and emission was measured through an emission filter at 515-575 nm. Assay plates were read for 3.5 minutes using the FLIPRTETRA.Cell Based Assay: Ca2+ signaling studies were performed using a FLIPR TETRA system (Molecular Devices, Sunnyvale, Calif., USA) in the 384-format. This is a high-throughput instrument for cell-based assays to monitor Ca2+ signaling associated with GPCRs and ion channels. Cells were seeded at a density of 5×104 cells/well in BioCoat poly-D-lysine coated, black wall, clear bottom 384-well plates (BD Biosciences, Franklin lakes, NJ, USA) and allowed to attach overnight in an incubator at 37° C. The cells were then washed twice with HBSS-HEPES buffer (Hanks' balanced salt solution without bicarbonate and phenol red, 20 mM HEPES, pH 7.4) using an ELx405 Select CW Microplate Washer (BioTek, Winooski, Vt., USA). After 60 min of dye-loading in the dark using the Ca2+-sensitive dye Fluo-4AM (Invitrogen, Carlsbad, Calif., USA), at a final concentration of 2×10^−6M, the plates were washed 4 times with HBSS-HEPES buffer to remove excess dye and leaving 50 μl of buffer in each well. The plates were then placed in the FLIPR TETRA instrument and allowed to equilibrate at 37° C. AGN-211377 was added in a 25 μl volume to each well to give final concentrations of 0.1 μM, 0.3 μM, 1 μM, 3 μM, 10 μM, and 30 μM; or 0.067 μM, 0.1 μM, 0.2 μM, 0.3 μM, 0.67 μM, and 1 μM for cells over-expressing TP receptors. After 4.5 minutes, a 7-point serial dilution of the standard agonist for the corresponding receptor, in a 25 μl volume was injected at the final concentrations from 10^−11M to 10^−5M in 10-fold serial dilution increments for cells expressing human recombinant DP1, EP1, EP2, EP3, EP4, FP, and IP receptors. The dose range for the standard agonist for human recombinant TP receptors was from 10^−12M to 10^−6M. HBSS-HEPES buffer was used as the negative control for the standard agonists. Cells were excited with LED (light emitting diode) excitation at 470-495 nm and emission was measured through an emission filter at 515-575 nm. Assay plates were read for 3.5 minutes using the FLIPRTETRA.
ChEMBL 604 15 2 7 5.1 CCCCCCCCNC(=O)c1coc([C@@H]2CCCN2Cc2cc(F)ccc2CCC(=O)NS(=O)(=O)C(F)(F)F)n1 nan
57529188 153973 0 None 19 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assayAgonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assay
ChEMBL 415 11 2 5 4.3 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)o2)cc1 nan
CHEMBL3928130 153973 0 None 19 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assayAgonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assay
ChEMBL 415 11 2 5 4.3 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)o2)cc1 nan
89443813 158517 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 397 7 2 3 5.3 Cc1ccc(OCC(=O)O)c(C)c1NCc1cc(-c2cccc(F)c2)ccc1F nan
CHEMBL3964577 158517 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 397 7 2 3 5.3 Cc1ccc(OCC(=O)O)c(C)c1NCc1cc(-c2cccc(F)c2)ccc1F nan
118517359 151174 0 None -79 4 Human 7.6 pEC50 = 7.6 Functional
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
ChEMBL 456 8 2 3 4.8 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2cccc(Br)c2)cc1 nan
CHEMBL3906016 151174 0 None -79 4 Human 7.6 pEC50 = 7.6 Functional
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
ChEMBL 456 8 2 3 4.8 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2cccc(Br)c2)cc1 nan
57384034 78082 0 None -9 2 Rat 6.6 pEC50 = 6.6 Functional
Agonist activity at rat EP2 receptorAgonist activity at rat EP2 receptor
ChEMBL 528 10 2 6 5.4 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(-c3ccc(Cl)cc3)c2)n1 10.1016/j.bmc.2012.02.018
CHEMBL1957436 78082 0 None -9 2 Rat 6.6 pEC50 = 6.6 Functional
Agonist activity at rat EP2 receptorAgonist activity at rat EP2 receptor
ChEMBL 528 10 2 6 5.4 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(-c3ccc(Cl)cc3)c2)n1 10.1016/j.bmc.2012.02.018
57384034 78082 0 None -9 2 Rat 6.6 pEC50 = 6.6 Functional
Agonist activity at rat EP2 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP2 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
ChEMBL 528 10 2 6 5.4 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(-c3ccc(Cl)cc3)c2)n1 10.1016/j.bmc.2012.04.008
CHEMBL1957436 78082 0 None -9 2 Rat 6.6 pEC50 = 6.6 Functional
Agonist activity at rat EP2 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP2 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
ChEMBL 528 10 2 6 5.4 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(-c3ccc(Cl)cc3)c2)n1 10.1016/j.bmc.2012.04.008
11955194 157782 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 380 8 2 2 5.5 CC(C)(C)c1ccc([C@H]2[C@H](O)C[C@@H](Cl)[C@@H]2CCCCCCC(=O)O)cc1 nan
CHEMBL3958410 157782 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 380 8 2 2 5.5 CC(C)(C)c1ccc([C@H]2[C@H](O)C[C@@H](Cl)[C@@H]2CCCCCCC(=O)O)cc1 nan
58708282 159903 0 None 1 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 412 11 2 3 6.0 CCCC1([C@@H](O)c2cccc([C@H]3CCC(=O)[C@@H]3C/C=C\CCCC(=O)O)c2)CCC1 nan
CHEMBL3976452 159903 0 None 1 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 412 11 2 3 6.0 CCCC1([C@@H](O)c2cccc([C@H]3CCC(=O)[C@@H]3C/C=C\CCCC(=O)O)c2)CCC1 nan
58681352 161118 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 486 10 3 4 5.5 CCCC1(C(O)c2cccc([C@H]3[C@H](O)C[C@@H](Cl)[C@@H]3Cc3cccc(OCC(=O)O)c3)c2)CCC1 nan
CHEMBL3986829 161118 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 486 10 3 4 5.5 CCCC1(C(O)c2cccc([C@H]3[C@H](O)C[C@@H](Cl)[C@@H]3Cc3cccc(OCC(=O)O)c3)c2)CCC1 nan
126495360 147012 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
ChEMBL 389 5 2 6 3.4 Cc1ccc(OC[C@H]2[C@H](O)C[C@@H]3O[C@@H](c4nc(C(=O)O)cs4)CC[C@@H]32)cc1 10.1021/acsmedchemlett.5b00455
CHEMBL3805316 147012 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
ChEMBL 389 5 2 6 3.4 Cc1ccc(OC[C@H]2[C@H](O)C[C@@H]3O[C@@H](c4nc(C(=O)O)cs4)CC[C@@H]32)cc1 10.1021/acsmedchemlett.5b00455
11855866 151380 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assayAgonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assay
ChEMBL 403 9 2 5 4.0 CCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3907809 151380 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assayAgonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assay
ChEMBL 403 9 2 5 4.0 CCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
89443595 151739 5 None - 1 Human 7.6 pEC50 = 7.6 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 412 7 2 4 4.7 N#Cc1cc(CNc2c(F)ccc(OCC(=O)O)c2F)cc(-c2cccc(F)c2)c1 nan
CHEMBL3910551 151739 5 None - 1 Human 7.6 pEC50 = 7.6 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 412 7 2 4 4.7 N#Cc1cc(CNc2c(F)ccc(OCC(=O)O)c2F)cc(-c2cccc(F)c2)c1 nan
57894053 81945 0 None -208 2 Rat 5.6 pEC50 = 5.6 Functional
Agonist activity at rat EP2 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP2 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
ChEMBL 551 10 2 8 5.4 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(-c3nc4ccccc4s3)c2)n1 10.1016/j.bmc.2012.04.008
CHEMBL2036324 81945 0 None -208 2 Rat 5.6 pEC50 = 5.6 Functional
Agonist activity at rat EP2 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP2 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
ChEMBL 551 10 2 8 5.4 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(-c3nc4ccccc4s3)c2)n1 10.1016/j.bmc.2012.04.008
118517359 151174 0 None -79 4 Human 6.6 pEC50 = 6.6 Functional
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
ChEMBL 456 8 2 3 4.8 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2cccc(Br)c2)cc1 nan
CHEMBL3906016 151174 0 None -79 4 Human 6.6 pEC50 = 6.6 Functional
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
ChEMBL 456 8 2 3 4.8 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2cccc(Br)c2)cc1 nan
126495420 147027 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
ChEMBL 431 9 2 6 4.7 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3CCCCCOc3ccccc3)O2)n1 10.1021/acsmedchemlett.5b00455
CHEMBL3805455 147027 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
ChEMBL 431 9 2 6 4.7 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3CCCCCOc3ccccc3)O2)n1 10.1021/acsmedchemlett.5b00455
11855324 149383 0 None 14 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assayAgonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assay
ChEMBL 371 6 1 4 4.0 CC(C)(C)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)o2)cc1 nan
CHEMBL3891401 149383 0 None 14 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assayAgonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assay
ChEMBL 371 6 1 4 4.0 CC(C)(C)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)o2)cc1 nan
71515514 154404 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 405 7 2 3 5.0 O=C(O)COc1ccc(F)c(NCc2cc(-c3cccc(F)c3)ccc2F)c1F nan
CHEMBL3931335 154404 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 405 7 2 3 5.0 O=C(O)COc1ccc(F)c(NCc2cc(-c3cccc(F)c3)ccc2F)c1F nan
11955198 154021 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 436 10 3 3 5.8 O=C(O)CCCCCC[C@@H]1[C@@H](c2ccc(C(O)C3CCCCC3)cc2)[C@H](O)C[C@H]1Cl nan
CHEMBL3928466 154021 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 436 10 3 3 5.8 O=C(O)CCCCCC[C@@H]1[C@@H](c2ccc(C(O)C3CCCCC3)cc2)[C@H](O)C[C@H]1Cl nan
155541719 183161 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 482 9 1 6 3.7 CN(CC(=O)O)c1cccc(CN(Cc2ccc(C(C)(C)C)cc2)S(=O)(=O)c2cccnc2)n1 10.1021/acs.jmedchem.8b00808
CHEMBL4519118 183161 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 482 9 1 6 3.7 CN(CC(=O)O)c1cccc(CN(Cc2ccc(C(C)(C)C)cc2)S(=O)(=O)c2cccnc2)n1 10.1021/acs.jmedchem.8b00808
CHEMBL4595870 183161 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 482 9 1 6 3.7 CN(CC(=O)O)c1cccc(CN(Cc2ccc(C(C)(C)C)cc2)S(=O)(=O)c2cccnc2)n1 10.1021/acs.jmedchem.8b00808
132836 66469 23 None -3 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 388 13 2 3 5.8 CCCCCC(O)c1ccc([C@H]2CCC(=O)[C@@H]2CCCCCCC(=O)O)cc1 nan
CHEMBL1722929 66469 23 None -3 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 388 13 2 3 5.8 CCCCCC(O)c1ccc([C@H]2CCC(=O)[C@@H]2CCCCCCC(=O)O)cc1 nan
155532079 178468 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 494 10 2 6 4.4 O=C(O)CNc1cccc(CN(Cc2ccc(C3CCCCC3)cc2)S(=O)(=O)c2cccnc2)n1 10.1021/acs.jmedchem.8b00808
CHEMBL4466523 178468 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 494 10 2 6 4.4 O=C(O)CNc1cccc(CN(Cc2ccc(C3CCCCC3)cc2)S(=O)(=O)c2cccnc2)n1 10.1021/acs.jmedchem.8b00808
44455084 104643 0 None -10 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human EP2 receptor by cAMP assayAgonist activity at human EP2 receptor by cAMP assay
ChEMBL 399 10 2 3 4.2 CCCCC1([C@@H](O)/C=C/[C@H]2CCC(=O)N2CCc2ccc(C(=O)O)cc2)CCC1 10.1016/j.bmcl.2007.11.020
CHEMBL272277 104643 0 None -10 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human EP2 receptor by cAMP assayAgonist activity at human EP2 receptor by cAMP assay
ChEMBL 399 10 2 3 4.2 CCCCC1([C@@H](O)/C=C/[C@H]2CCC(=O)N2CCc2ccc(C(=O)O)cc2)CCC1 10.1016/j.bmcl.2007.11.020
59465581 150890 0 None 22 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assayAgonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assay
ChEMBL 428 11 2 4 6.1 CCCCCC(O)c1ccc([C@H]2CCC(=O)[C@@H]2CCCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3903611 150890 0 None 22 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assayAgonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assay
ChEMBL 428 11 2 4 6.1 CCCCCC(O)c1ccc([C@H]2CCC(=O)[C@@H]2CCCc2ccc(C(=O)O)s2)cc1 nan
89443767 152490 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 409 8 2 4 5.2 COc1cc(CNc2c(C)ccc(OCC(=O)O)c2C)cc(-c2cccc(F)c2)c1 nan
CHEMBL3916293 152490 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 409 8 2 4 5.2 COc1cc(CNc2c(C)ccc(OCC(=O)O)c2C)cc(-c2cccc(F)c2)c1 nan
89443716 153804 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 397 7 2 3 5.3 Cc1cc(CNc2c(F)ccc(OCC(=O)O)c2C)cc(-c2cccc(F)c2)c1 nan
CHEMBL3926711 153804 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 397 7 2 3 5.3 Cc1cc(CNc2c(F)ccc(OCC(=O)O)c2C)cc(-c2cccc(F)c2)c1 nan
89443671 154616 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 419 7 2 3 5.3 Cc1c(F)cc(-c2cccc(F)c2)cc1CNc1c(F)ccc(OCC(=O)O)c1F nan
CHEMBL3932999 154616 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 419 7 2 3 5.3 Cc1c(F)cc(-c2cccc(F)c2)cc1CNc1c(F)ccc(OCC(=O)O)c1F nan
89445501 159055 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 411 7 2 3 5.6 Cc1ccc(OCC(=O)O)c(C)c1NCc1cc(-c2cccc(F)c2)cc(F)c1C nan
CHEMBL3969269 159055 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 411 7 2 3 5.6 Cc1ccc(OCC(=O)O)c(C)c1NCc1cc(-c2cccc(F)c2)cc(F)c1C nan
89443873 160719 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 411 7 2 3 5.6 Cc1cc(CNc2c(C)ccc(OCC(=O)O)c2C)c(F)c(-c2cccc(F)c2)c1 nan
CHEMBL3983500 160719 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 411 7 2 3 5.6 Cc1cc(CNc2c(C)ccc(OCC(=O)O)c2C)c(F)c(-c2cccc(F)c2)c1 nan
127051062 147052 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
ChEMBL 409 5 2 6 3.8 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3COc3ccccc3Cl)O2)n1 10.1021/acsmedchemlett.5b00455
CHEMBL3805767 147052 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
ChEMBL 409 5 2 6 3.8 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3COc3ccccc3Cl)O2)n1 10.1021/acsmedchemlett.5b00455
46931421 183042 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 468 9 2 7 3.6 O=C(O)CNc1cccc(CN(Cc2cc3ccccc3s2)S(=O)(=O)c2cccnc2)n1 10.1021/acs.jmedchem.8b00808
CHEMBL4476670 183042 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 468 9 2 7 3.6 O=C(O)CNc1cccc(CN(Cc2cc3ccccc3s2)S(=O)(=O)c2cccnc2)n1 10.1021/acs.jmedchem.8b00808
CHEMBL4594971 183042 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 468 9 2 7 3.6 O=C(O)CNc1cccc(CN(Cc2cc3ccccc3s2)S(=O)(=O)c2cccnc2)n1 10.1021/acs.jmedchem.8b00808
126495424 147033 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
ChEMBL 389 5 2 6 3.4 Cc1cccc(OC[C@H]2[C@H](O)C[C@@H]3O[C@@H](c4nc(C(=O)O)cs4)CC[C@@H]32)c1 10.1021/acsmedchemlett.5b00455
CHEMBL3805554 147033 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
ChEMBL 389 5 2 6 3.4 Cc1cccc(OC[C@H]2[C@H](O)C[C@@H]3O[C@@H](c4nc(C(=O)O)cs4)CC[C@@H]32)c1 10.1021/acsmedchemlett.5b00455
127052615 147048 0 None 181 3 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
ChEMBL 401 6 2 6 3.7 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3/C=C/COc3ccccc3)O2)n1 10.1021/acsmedchemlett.5b00455
CHEMBL3805693 147048 0 None 181 3 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
ChEMBL 401 6 2 6 3.7 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3/C=C/COc3ccccc3)O2)n1 10.1021/acsmedchemlett.5b00455
127027875 146194 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assayAgonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assay
ChEMBL 409 5 2 6 3.8 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3COc3ccc(Cl)cc3)O2)n1 10.1016/j.bmcl.2016.03.110
CHEMBL3793786 146194 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assayAgonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assay
ChEMBL 409 5 2 6 3.8 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3COc3ccc(Cl)cc3)O2)n1 10.1016/j.bmcl.2016.03.110
127026954 146198 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assayAgonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assay
ChEMBL 457 5 2 6 4.5 Cc1cc(OC[C@H]2[C@H](O)C[C@@H]3O[C@@H](c4nc(C(=O)O)cs4)CC[C@@H]32)ccc1C(F)(F)F 10.1016/j.bmcl.2016.03.110
CHEMBL3793809 146198 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assayAgonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assay
ChEMBL 457 5 2 6 4.5 Cc1cc(OC[C@H]2[C@H](O)C[C@@H]3O[C@@H](c4nc(C(=O)O)cs4)CC[C@@H]32)ccc1C(F)(F)F 10.1016/j.bmcl.2016.03.110
127027875 146194 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
ChEMBL 409 5 2 6 3.8 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3COc3ccc(Cl)cc3)O2)n1 10.1021/acsmedchemlett.5b00455
CHEMBL3793786 146194 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
ChEMBL 409 5 2 6 3.8 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3COc3ccc(Cl)cc3)O2)n1 10.1021/acsmedchemlett.5b00455
127052614 147004 0 None 40 6 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
ChEMBL 415 7 2 6 4.1 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3/C=C/CCOc3ccccc3)O2)n1 10.1021/acsmedchemlett.5b00455
CHEMBL3805176 147004 0 None 40 6 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
ChEMBL 415 7 2 6 4.1 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3/C=C/CCOc3ccccc3)O2)n1 10.1021/acsmedchemlett.5b00455
118517490 159934 0 None -12 4 Human 7.5 pEC50 = 7.5 Functional
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
ChEMBL 414 8 2 3 4.4 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2ccc(F)c(F)c2)cc1 nan
CHEMBL3976710 159934 0 None -12 4 Human 7.5 pEC50 = 7.5 Functional
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
ChEMBL 414 8 2 3 4.4 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2ccc(F)c(F)c2)cc1 nan
44230723 183284 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 490 10 2 8 2.8 O=C(O)CNc1cccc(CN(Cc2ccc(-c3ccnnc3)cc2)S(=O)(=O)c2cccnc2)n1 10.1021/acs.jmedchem.8b00808
CHEMBL4473407 183284 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 490 10 2 8 2.8 O=C(O)CNc1cccc(CN(Cc2ccc(-c3ccnnc3)cc2)S(=O)(=O)c2cccnc2)n1 10.1021/acs.jmedchem.8b00808
CHEMBL4596867 183284 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 490 10 2 8 2.8 O=C(O)CNc1cccc(CN(Cc2ccc(-c3ccnnc3)cc2)S(=O)(=O)c2cccnc2)n1 10.1021/acs.jmedchem.8b00808
134155748 157948 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 400 12 2 4 4.7 CCCCCC(=O)c1ccc([C@H]2[C@H](O)CC(=O)[C@@H]2C/C=C\CCCC(=O)O)cc1 nan
CHEMBL3959653 157948 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 400 12 2 4 4.7 CCCCCC(=O)c1ccc([C@H]2[C@H](O)CC(=O)[C@@H]2C/C=C\CCCC(=O)O)cc1 nan
145965248 171009 0 None -9 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at recombinant human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIAAgonist activity at recombinant human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIA
ChEMBL 439 10 2 6 5.4 CC(C)(C)CC[C@](C)(O)C/C=C/[C@H]1CCC(=O)[C@@H]1CCSc1nc(C(=O)O)cs1 10.1016/j.bmc.2017.11.035
CHEMBL4211120 171009 0 None -9 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at recombinant human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIAAgonist activity at recombinant human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIA
ChEMBL 439 10 2 6 5.4 CC(C)(C)CC[C@](C)(O)C/C=C/[C@H]1CCC(=O)[C@@H]1CCSc1nc(C(=O)O)cs1 10.1016/j.bmc.2017.11.035
11855867 152761 0 None 10 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assayAgonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assay
ChEMBL 389 8 2 5 3.6 CCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3918349 152761 0 None 10 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assayAgonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assay
ChEMBL 389 8 2 5 3.6 CCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
58681361 151459 0 None -33 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 318 8 2 3 3.5 Cc1ccc([C@H]2[C@H](O)CC(=O)[C@@H]2CCCCCCC(=O)O)cc1 nan
CHEMBL3908432 151459 0 None -33 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 318 8 2 3 3.5 Cc1ccc([C@H]2[C@H](O)CC(=O)[C@@H]2CCCCCCC(=O)O)cc1 nan
44304181 210052 0 None -1 2 Mouse 7.5 pEC50 = 7.5 Functional
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptor
ChEMBL 394 13 3 4 4.3 CCCC1([C@@H](O)C/C=C/C2[C@H](O)CC(=O)[C@@H]2CCCCCCC(=O)O)CCC1 10.1016/s0960-894x(01)00359-6
CHEMBL64663 210052 0 None -1 2 Mouse 7.5 pEC50 = 7.5 Functional
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptor
ChEMBL 394 13 3 4 4.3 CCCC1([C@@H](O)C/C=C/C2[C@H](O)CC(=O)[C@@H]2CCCCCCC(=O)O)CCC1 10.1016/s0960-894x(01)00359-6
58932683 82062 0 None -1995 2 Rat 5.5 pEC50 = 5.5 Functional
Agonist activity at rat EP2 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP2 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
ChEMBL 549 10 2 8 5.2 Cc1ccc2nc(-c3cccc(C[C@H](O)/C=C/[C@H]4CCC(=O)N4CCSc4nc(C(=O)O)cs4)c3)oc2c1 10.1016/j.bmc.2012.04.008
CHEMBL2037289 82062 0 None -1995 2 Rat 5.5 pEC50 = 5.5 Functional
Agonist activity at rat EP2 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP2 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
ChEMBL 549 10 2 8 5.2 Cc1ccc2nc(-c3cccc(C[C@H](O)/C=C/[C@H]4CCC(=O)N4CCSc4nc(C(=O)O)cs4)c3)oc2c1 10.1016/j.bmc.2012.04.008
11955178 160566 0 None 1 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 448 11 3 3 6.0 CCCC1(C(O)c2cccc([C@H]3[C@H](O)C[C@@H](Cl)[C@@H]3C/C=C\CCCC(=O)O)c2)CCC1 nan
CHEMBL3982222 160566 0 None 1 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 448 11 3 3 6.0 CCCC1(C(O)c2cccc([C@H]3[C@H](O)C[C@@H](Cl)[C@@H]3C/C=C\CCCC(=O)O)c2)CCC1 nan
44303980 174853 0 None 1 2 Mouse 7.5 pEC50 = 7.5 Functional
Effective concentration which increases intracellular c-AMP production in mouse EP2- receptorEffective concentration which increases intracellular c-AMP production in mouse EP2- receptor
ChEMBL 408 13 2 5 4.3 CCCC1([C@@H](O)C/C=C/C2[C@H](O)CC(=O)[C@@H]2CCCCCCC(=O)OC)CCC1 10.1016/s0960-894x(01)00359-6
CHEMBL432522 174853 0 None 1 2 Mouse 7.5 pEC50 = 7.5 Functional
Effective concentration which increases intracellular c-AMP production in mouse EP2- receptorEffective concentration which increases intracellular c-AMP production in mouse EP2- receptor
ChEMBL 408 13 2 5 4.3 CCCC1([C@@H](O)C/C=C/C2[C@H](O)CC(=O)[C@@H]2CCCCCCC(=O)OC)CCC1 10.1016/s0960-894x(01)00359-6
1883 9856 75 None -6 12 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human EP2 receptor expressed in HEK293T/17 cells assessed as increase in intracellular cAMP level incubated for 30 mins by ELISAAgonist activity at human EP2 receptor expressed in HEK293T/17 cells assessed as increase in intracellular cAMP level incubated for 30 mins by ELISA
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/acs.jmedchem.9b00336
1916 9856 75 None -6 12 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human EP2 receptor expressed in HEK293T/17 cells assessed as increase in intracellular cAMP level incubated for 30 mins by ELISAAgonist activity at human EP2 receptor expressed in HEK293T/17 cells assessed as increase in intracellular cAMP level incubated for 30 mins by ELISA
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/acs.jmedchem.9b00336
5280360 9856 75 None -6 12 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human EP2 receptor expressed in HEK293T/17 cells assessed as increase in intracellular cAMP level incubated for 30 mins by ELISAAgonist activity at human EP2 receptor expressed in HEK293T/17 cells assessed as increase in intracellular cAMP level incubated for 30 mins by ELISA
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/acs.jmedchem.9b00336
913 9856 75 None -6 12 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human EP2 receptor expressed in HEK293T/17 cells assessed as increase in intracellular cAMP level incubated for 30 mins by ELISAAgonist activity at human EP2 receptor expressed in HEK293T/17 cells assessed as increase in intracellular cAMP level incubated for 30 mins by ELISA
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/acs.jmedchem.9b00336
CHEMBL548 9856 75 None -6 12 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human EP2 receptor expressed in HEK293T/17 cells assessed as increase in intracellular cAMP level incubated for 30 mins by ELISAAgonist activity at human EP2 receptor expressed in HEK293T/17 cells assessed as increase in intracellular cAMP level incubated for 30 mins by ELISA
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/acs.jmedchem.9b00336
DB00917 9856 75 None -6 12 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human EP2 receptor expressed in HEK293T/17 cells assessed as increase in intracellular cAMP level incubated for 30 mins by ELISAAgonist activity at human EP2 receptor expressed in HEK293T/17 cells assessed as increase in intracellular cAMP level incubated for 30 mins by ELISA
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/acs.jmedchem.9b00336
17757350 159533 0 None 870 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 413 12 3 4 5.1 CCCCCC(O)c1ccc([C@@H]2[C@@H](C/C=C\CCCC(=O)O)[C@H](C#N)C[C@H]2O)cc1 nan
CHEMBL3973347 159533 0 None 870 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 413 12 3 4 5.1 CCCCCC(O)c1ccc([C@@H]2[C@@H](C/C=C\CCCC(=O)O)[C@H](C#N)C[C@H]2O)cc1 nan
89444121 154210 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 421 7 2 3 5.5 O=C(O)COc1ccc(F)c(NCc2cc(-c3cccc(F)c3)ccc2F)c1Cl nan
CHEMBL3929987 154210 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 421 7 2 3 5.5 O=C(O)COc1ccc(F)c(NCc2cc(-c3cccc(F)c3)ccc2F)c1Cl nan
45271237 201878 0 None - 1 Rat 7.5 pEC50 = 7.5 Functional
Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP releaseAgonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release
ChEMBL 403 11 1 3 4.0 CCCCc1ccc(CN(Cc2cccc(CCC(=O)O)c2)S(C)(=O)=O)cc1 10.1016/j.bmcl.2009.01.059
CHEMBL549870 201878 0 None - 1 Rat 7.5 pEC50 = 7.5 Functional
Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP releaseAgonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release
ChEMBL 403 11 1 3 4.0 CCCCc1ccc(CN(Cc2cccc(CCC(=O)O)c2)S(C)(=O)=O)cc1 10.1016/j.bmcl.2009.01.059
66858036 170670 0 None -93 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at recombinant human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIAAgonist activity at recombinant human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIA
ChEMBL 468 10 2 7 4.8 C[C@@H]1OC(=O)N(CCSc2nc(C(=O)O)cs2)[C@H]1/C=C/CC(C)(O)CC1CCCCC1 10.1016/j.bmc.2017.11.035
CHEMBL4207054 170670 0 None -93 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at recombinant human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIAAgonist activity at recombinant human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIA
ChEMBL 468 10 2 7 4.8 C[C@@H]1OC(=O)N(CCSc2nc(C(=O)O)cs2)[C@H]1/C=C/CC(C)(O)CC1CCCCC1 10.1016/j.bmc.2017.11.035
59465599 153339 0 None 1 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 414 12 2 3 6.2 CCCC1(C(O)c2cccc([C@H]3CCC(=O)[C@@H]3CCCCCCC(=O)O)c2)CCC1 nan
CHEMBL3922856 153339 0 None 1 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 414 12 2 3 6.2 CCCC1(C(O)c2cccc([C@H]3CCC(=O)[C@@H]3CCCCCCC(=O)O)c2)CCC1 nan
59465600 158477 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 388 13 2 3 5.3 CCCCC(O)Cc1ccc([C@H]2CCC(=O)[C@@H]2CCCCCCC(=O)O)cc1 nan
CHEMBL3964261 158477 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 388 13 2 3 5.3 CCCCC(O)Cc1ccc([C@H]2CCC(=O)[C@@H]2CCCCCCC(=O)O)cc1 nan
58681358 157438 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 420 10 2 2 6.3 O=C(O)CCCCCC[C@@H]1[C@@H](c2ccc(CC3CCCCC3)cc2)[C@H](O)C[C@H]1Cl nan
CHEMBL3955642 157438 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 420 10 2 2 6.3 O=C(O)CCCCCC[C@@H]1[C@@H](c2ccc(CC3CCCCC3)cc2)[C@H](O)C[C@H]1Cl nan
44442331 101265 0 None -346 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at EP2 receptor expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at EP2 receptor expressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 355 9 1 2 4.6 CCCC/C(C)=C\C=C\[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.05.025
CHEMBL251505 101265 0 None -346 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at EP2 receptor expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at EP2 receptor expressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 355 9 1 2 4.6 CCCC/C(C)=C\C=C\[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.05.025
44230430 183149 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 506 10 2 6 4.2 O=C(O)CNc1cccc(CN(Cc2ccc(-c3ccc(F)cc3)cc2)S(=O)(=O)c2cccnc2)n1 10.1021/acs.jmedchem.8b00808
CHEMBL4449902 183149 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 506 10 2 6 4.2 O=C(O)CNc1cccc(CN(Cc2ccc(-c3ccc(F)cc3)cc2)S(=O)(=O)c2cccnc2)n1 10.1021/acs.jmedchem.8b00808
CHEMBL4595790 183149 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 506 10 2 6 4.2 O=C(O)CNc1cccc(CN(Cc2ccc(-c3ccc(F)cc3)cc2)S(=O)(=O)c2cccnc2)n1 10.1021/acs.jmedchem.8b00808
71515518 149584 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 401 7 2 3 5.2 Cc1cc(CNc2c(F)ccc(OCC(=O)O)c2F)cc(-c2cccc(F)c2)c1 nan
CHEMBL3892911 149584 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 401 7 2 3 5.2 Cc1cc(CNc2c(F)ccc(OCC(=O)O)c2F)cc(-c2cccc(F)c2)c1 nan
89443584 151955 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 415 7 2 3 5.5 Cc1cc(CNc2c(F)ccc(OCC(=O)O)c2C)c(F)c(-c2cccc(F)c2)c1 nan
CHEMBL3912323 151955 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 415 7 2 3 5.5 Cc1cc(CNc2c(F)ccc(OCC(=O)O)c2C)c(F)c(-c2cccc(F)c2)c1 nan
118517361 160149 0 None -107 3 Human 7.5 pEC50 = 7.5 Functional
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
ChEMBL 446 8 2 3 5.1 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2cccc(C(F)(F)F)c2)cc1 nan
CHEMBL3978590 160149 0 None -107 3 Human 7.5 pEC50 = 7.5 Functional
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
ChEMBL 446 8 2 3 5.1 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2cccc(C(F)(F)F)c2)cc1 nan
155542681 183379 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 474 9 2 7 3.7 CC(C)(C)c1ccc(CN(Cc2csc(NCC(=O)O)n2)S(=O)(=O)c2cccnc2)cc1 10.1021/acs.jmedchem.8b00808
CHEMBL4521659 183379 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 474 9 2 7 3.7 CC(C)(C)c1ccc(CN(Cc2csc(NCC(=O)O)n2)S(=O)(=O)c2cccnc2)cc1 10.1021/acs.jmedchem.8b00808
CHEMBL4597685 183379 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 474 9 2 7 3.7 CC(C)(C)c1ccc(CN(Cc2csc(NCC(=O)O)n2)S(=O)(=O)c2cccnc2)cc1 10.1021/acs.jmedchem.8b00808
11955156 155233 1 None -2 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 428 11 3 4 4.9 CCCC1(C(O)c2cccc([C@H]3[C@H](O)CC(=O)[C@@H]3C/C=C\CCCC(=O)O)c2)CCC1 nan
CHEMBL3937945 155233 1 None -2 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 428 11 3 4 4.9 CCCC1(C(O)c2cccc([C@H]3[C@H](O)CC(=O)[C@@H]3C/C=C\CCCC(=O)O)c2)CCC1 nan
118689427 158631 0 None -8 2 Human 7.4 pEC50 = 7.4 Functional
cAMP Assay: EP4 receptors couple to Gs and mediate elevations in cAMP concentration, although they do participate in other pathways as well. There are some redundancies in function between EP2 and EP4 receptors. For example, both receptors induce PGE2-mediated RANKL through cAMP.cAMP Assay: EP4 receptors couple to Gs and mediate elevations in cAMP concentration, although they do participate in other pathways as well. There are some redundancies in function between EP2 and EP4 receptors. For example, both receptors induce PGE2-mediated RANKL through cAMP.
ChEMBL 519 10 2 6 3.8 O=C(O)c1ccc(CCCN2[C@@H](/C=C/C(O)Cc3cccc(OC(F)(F)F)c3)CCS2(=O)=O)s1 nan
CHEMBL3965497 158631 0 None -8 2 Human 7.4 pEC50 = 7.4 Functional
cAMP Assay: EP4 receptors couple to Gs and mediate elevations in cAMP concentration, although they do participate in other pathways as well. There are some redundancies in function between EP2 and EP4 receptors. For example, both receptors induce PGE2-mediated RANKL through cAMP.cAMP Assay: EP4 receptors couple to Gs and mediate elevations in cAMP concentration, although they do participate in other pathways as well. There are some redundancies in function between EP2 and EP4 receptors. For example, both receptors induce PGE2-mediated RANKL through cAMP.
ChEMBL 519 10 2 6 3.8 O=C(O)c1ccc(CCCN2[C@@H](/C=C/C(O)Cc3cccc(OC(F)(F)F)c3)CCS2(=O)=O)s1 nan
57893982 81939 0 None -25 2 Rat 6.4 pEC50 = 6.4 Functional
Agonist activity at rat EP2 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP2 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
ChEMBL 508 10 2 6 5.1 Cc1ccc(-c2cccc(C[C@H](O)/C=C/[C@H]3CCC(=O)N3CCSc3nc(C(=O)O)cs3)c2)cc1 10.1016/j.bmc.2012.04.008
CHEMBL2036318 81939 0 None -25 2 Rat 6.4 pEC50 = 6.4 Functional
Agonist activity at rat EP2 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP2 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
ChEMBL 508 10 2 6 5.1 Cc1ccc(-c2cccc(C[C@H](O)/C=C/[C@H]3CCC(=O)N3CCSc3nc(C(=O)O)cs3)c2)cc1 10.1016/j.bmc.2012.04.008
11955259 153537 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 436 9 3 4 4.4 O=C(O)COC/C=C\C[C@@H]1[C@@H](c2ccc(C(O)C3CCCCC3)cc2)[C@H](O)C[C@H]1Cl nan
CHEMBL3924405 153537 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 436 9 3 4 4.4 O=C(O)COC/C=C\C[C@@H]1[C@@H](c2ccc(C(O)C3CCCCC3)cc2)[C@H](O)C[C@H]1Cl nan
57529188 153973 0 None 19 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 415 11 2 5 4.3 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)o2)cc1 nan
CHEMBL3928130 153973 0 None 19 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 415 11 2 5 4.3 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)o2)cc1 nan
57529188 153973 0 None 19 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assayAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assay
ChEMBL 415 11 2 5 4.3 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)o2)cc1 nan
CHEMBL3928130 153973 0 None 19 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assayAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assay
ChEMBL 415 11 2 5 4.3 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)o2)cc1 nan
44303626 174961 0 None - 1 Mouse 7.4 pEC50 = 7.4 Functional
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptor
ChEMBL 398 11 3 3 4.7 CCC1([C@@H](O)C/C=C/[C@H]2[C@H](O)C[C@H](Cl)[C@@H]2C/C=C\CCCC(=O)O)CCC1 10.1016/s0960-894x(01)00359-6
CHEMBL433249 174961 0 None - 1 Mouse 7.4 pEC50 = 7.4 Functional
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptor
ChEMBL 398 11 3 3 4.7 CCC1([C@@H](O)C/C=C/[C@H]2[C@H](O)C[C@H](Cl)[C@@H]2C/C=C\CCCC(=O)O)CCC1 10.1016/s0960-894x(01)00359-6
56839344 158830 0 None -12882 8 Human 5.4 pEC50 = 5.4 Functional
Cell Based Assay: Ca2+ signaling studies were performed using a FLIPR TETRA system (Molecular Devices, Sunnyvale, Calif., USA) in the 384-format. This is a high-throughput instrument for cell-based assays to monitor Ca2+ signaling associated with GPCRs and ion channels. Cells were seeded at a density of 5×104 cells/well in BioCoat poly-D-lysine coated, black wall, clear bottom 384-well plates (BD Biosciences, Franklin lakes, NJ, USA) and allowed to attach overnight in an incubator at 37° C. The cells were then washed twice with HBSS-HEPES buffer (Hanks' balanced salt solution without bicarbonate and phenol red, 20 mM HEPES, pH 7.4) using an ELx405 Select CW Microplate Washer (BioTek, Winooski, Vt., USA). After 60 min of dye-loading in the dark using the Ca2+-sensitive dye Fluo-4AM (Invitrogen, Carlsbad, Calif., USA), at a final concentration of 2×10^−6M, the plates were washed 4 times with HBSS-HEPES buffer to remove excess dye and leaving 50 μl of buffer in each well. The plates were then placed in the FLIPR TETRA instrument and allowed to equilibrate at 37° C. AGN-211377 was added in a 25 μl volume to each well to give final concentrations of 0.1 μM, 0.3 μM, 1 μM, 3 μM, 10 μM, and 30 μM; or 0.067 μM, 0.1 μM, 0.2 μM, 0.3 μM, 0.67 μM, and 1 μM for cells over-expressing TP receptors. After 4.5 minutes, a 7-point serial dilution of the standard agonist for the corresponding receptor, in a 25 μl volume was injected at the final concentrations from 10^−11M to 10^−5M in 10-fold serial dilution increments for cells expressing human recombinant DP1, EP1, EP2, EP3, EP4, FP, and IP receptors. The dose range for the standard agonist for human recombinant TP receptors was from 10^−12M to 10^−6M. HBSS-HEPES buffer was used as the negative control for the standard agonists. Cells were excited with LED (light emitting diode) excitation at 470-495 nm and emission was measured through an emission filter at 515-575 nm. Assay plates were read for 3.5 minutes using the FLIPRTETRA.Cell Based Assay: Ca2+ signaling studies were performed using a FLIPR TETRA system (Molecular Devices, Sunnyvale, Calif., USA) in the 384-format. This is a high-throughput instrument for cell-based assays to monitor Ca2+ signaling associated with GPCRs and ion channels. Cells were seeded at a density of 5×104 cells/well in BioCoat poly-D-lysine coated, black wall, clear bottom 384-well plates (BD Biosciences, Franklin lakes, NJ, USA) and allowed to attach overnight in an incubator at 37° C. The cells were then washed twice with HBSS-HEPES buffer (Hanks' balanced salt solution without bicarbonate and phenol red, 20 mM HEPES, pH 7.4) using an ELx405 Select CW Microplate Washer (BioTek, Winooski, Vt., USA). After 60 min of dye-loading in the dark using the Ca2+-sensitive dye Fluo-4AM (Invitrogen, Carlsbad, Calif., USA), at a final concentration of 2×10^−6M, the plates were washed 4 times with HBSS-HEPES buffer to remove excess dye and leaving 50 μl of buffer in each well. The plates were then placed in the FLIPR TETRA instrument and allowed to equilibrate at 37° C. AGN-211377 was added in a 25 μl volume to each well to give final concentrations of 0.1 μM, 0.3 μM, 1 μM, 3 μM, 10 μM, and 30 μM; or 0.067 μM, 0.1 μM, 0.2 μM, 0.3 μM, 0.67 μM, and 1 μM for cells over-expressing TP receptors. After 4.5 minutes, a 7-point serial dilution of the standard agonist for the corresponding receptor, in a 25 μl volume was injected at the final concentrations from 10^−11M to 10^−5M in 10-fold serial dilution increments for cells expressing human recombinant DP1, EP1, EP2, EP3, EP4, FP, and IP receptors. The dose range for the standard agonist for human recombinant TP receptors was from 10^−12M to 10^−6M. HBSS-HEPES buffer was used as the negative control for the standard agonists. Cells were excited with LED (light emitting diode) excitation at 470-495 nm and emission was measured through an emission filter at 515-575 nm. Assay plates were read for 3.5 minutes using the FLIPRTETRA.
ChEMBL 656 13 2 9 5.1 O=C(CCc1cc2c(cc1CN1CCC[C@H]1c1nc(C(=O)NCCCCC3CCCCC3)co1)OCO2)NS(=O)(=O)C(F)(F)F nan
CHEMBL3967284 158830 0 None -12882 8 Human 5.4 pEC50 = 5.4 Functional
Cell Based Assay: Ca2+ signaling studies were performed using a FLIPR TETRA system (Molecular Devices, Sunnyvale, Calif., USA) in the 384-format. This is a high-throughput instrument for cell-based assays to monitor Ca2+ signaling associated with GPCRs and ion channels. Cells were seeded at a density of 5×104 cells/well in BioCoat poly-D-lysine coated, black wall, clear bottom 384-well plates (BD Biosciences, Franklin lakes, NJ, USA) and allowed to attach overnight in an incubator at 37° C. The cells were then washed twice with HBSS-HEPES buffer (Hanks' balanced salt solution without bicarbonate and phenol red, 20 mM HEPES, pH 7.4) using an ELx405 Select CW Microplate Washer (BioTek, Winooski, Vt., USA). After 60 min of dye-loading in the dark using the Ca2+-sensitive dye Fluo-4AM (Invitrogen, Carlsbad, Calif., USA), at a final concentration of 2×10^−6M, the plates were washed 4 times with HBSS-HEPES buffer to remove excess dye and leaving 50 μl of buffer in each well. The plates were then placed in the FLIPR TETRA instrument and allowed to equilibrate at 37° C. AGN-211377 was added in a 25 μl volume to each well to give final concentrations of 0.1 μM, 0.3 μM, 1 μM, 3 μM, 10 μM, and 30 μM; or 0.067 μM, 0.1 μM, 0.2 μM, 0.3 μM, 0.67 μM, and 1 μM for cells over-expressing TP receptors. After 4.5 minutes, a 7-point serial dilution of the standard agonist for the corresponding receptor, in a 25 μl volume was injected at the final concentrations from 10^−11M to 10^−5M in 10-fold serial dilution increments for cells expressing human recombinant DP1, EP1, EP2, EP3, EP4, FP, and IP receptors. The dose range for the standard agonist for human recombinant TP receptors was from 10^−12M to 10^−6M. HBSS-HEPES buffer was used as the negative control for the standard agonists. Cells were excited with LED (light emitting diode) excitation at 470-495 nm and emission was measured through an emission filter at 515-575 nm. Assay plates were read for 3.5 minutes using the FLIPRTETRA.Cell Based Assay: Ca2+ signaling studies were performed using a FLIPR TETRA system (Molecular Devices, Sunnyvale, Calif., USA) in the 384-format. This is a high-throughput instrument for cell-based assays to monitor Ca2+ signaling associated with GPCRs and ion channels. Cells were seeded at a density of 5×104 cells/well in BioCoat poly-D-lysine coated, black wall, clear bottom 384-well plates (BD Biosciences, Franklin lakes, NJ, USA) and allowed to attach overnight in an incubator at 37° C. The cells were then washed twice with HBSS-HEPES buffer (Hanks' balanced salt solution without bicarbonate and phenol red, 20 mM HEPES, pH 7.4) using an ELx405 Select CW Microplate Washer (BioTek, Winooski, Vt., USA). After 60 min of dye-loading in the dark using the Ca2+-sensitive dye Fluo-4AM (Invitrogen, Carlsbad, Calif., USA), at a final concentration of 2×10^−6M, the plates were washed 4 times with HBSS-HEPES buffer to remove excess dye and leaving 50 μl of buffer in each well. The plates were then placed in the FLIPR TETRA instrument and allowed to equilibrate at 37° C. AGN-211377 was added in a 25 μl volume to each well to give final concentrations of 0.1 μM, 0.3 μM, 1 μM, 3 μM, 10 μM, and 30 μM; or 0.067 μM, 0.1 μM, 0.2 μM, 0.3 μM, 0.67 μM, and 1 μM for cells over-expressing TP receptors. After 4.5 minutes, a 7-point serial dilution of the standard agonist for the corresponding receptor, in a 25 μl volume was injected at the final concentrations from 10^−11M to 10^−5M in 10-fold serial dilution increments for cells expressing human recombinant DP1, EP1, EP2, EP3, EP4, FP, and IP receptors. The dose range for the standard agonist for human recombinant TP receptors was from 10^−12M to 10^−6M. HBSS-HEPES buffer was used as the negative control for the standard agonists. Cells were excited with LED (light emitting diode) excitation at 470-495 nm and emission was measured through an emission filter at 515-575 nm. Assay plates were read for 3.5 minutes using the FLIPRTETRA.
ChEMBL 656 13 2 9 5.1 O=C(CCc1cc2c(cc1CN1CCC[C@H]1c1nc(C(=O)NCCCCC3CCCCC3)co1)OCO2)NS(=O)(=O)C(F)(F)F nan
11955196 151200 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 434 9 3 3 5.6 O=C(O)CCC/C=C\C[C@@H]1[C@@H](c2ccc(C(O)C3CCCCC3)cc2)[C@H](O)C[C@H]1Cl nan
CHEMBL3906280 151200 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 434 9 3 3 5.6 O=C(O)CCC/C=C\C[C@@H]1[C@@H](c2ccc(C(O)C3CCCCC3)cc2)[C@H](O)C[C@H]1Cl nan
44444722 101031 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human prostaglandin EP2 receptorAgonist activity at human prostaglandin EP2 receptor
ChEMBL 402 11 2 4 3.5 CCCC1(C(O)CCCN2CCC(=O)N2CCc2ccc(C(=O)O)cc2)CCC1 10.1016/j.bmcl.2007.09.074
CHEMBL250153 101031 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human prostaglandin EP2 receptorAgonist activity at human prostaglandin EP2 receptor
ChEMBL 402 11 2 4 3.5 CCCC1(C(O)CCCN2CCC(=O)N2CCc2ccc(C(=O)O)cc2)CCC1 10.1016/j.bmcl.2007.09.074
17751059 155047 0 None 3 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assayAgonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assay
ChEMBL 440 12 2 2 6.8 CCCCCC(O)c1ccc([C@H]2[C@H](Cl)C[C@@H](Cl)[C@@H]2C/C=C\CCCC(=O)O)cc1 nan
CHEMBL3936540 155047 0 None 3 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assayAgonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assay
ChEMBL 440 12 2 2 6.8 CCCCCC(O)c1ccc([C@H]2[C@H](Cl)C[C@@H](Cl)[C@@H]2C/C=C\CCCC(=O)O)cc1 nan
17757350 159533 0 None 870 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assayAgonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assay
ChEMBL 413 12 3 4 5.1 CCCCCC(O)c1ccc([C@@H]2[C@@H](C/C=C\CCCC(=O)O)[C@H](C#N)C[C@H]2O)cc1 nan
CHEMBL3973347 159533 0 None 870 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assayAgonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assay
ChEMBL 413 12 3 4 5.1 CCCCCC(O)c1ccc([C@@H]2[C@@H](C/C=C\CCCC(=O)O)[C@H](C#N)C[C@H]2O)cc1 nan
89444221 151058 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 430 8 3 4 3.9 NC(=O)c1cc(CNc2c(F)ccc(OCC(=O)O)c2F)cc(-c2cccc(F)c2)c1 nan
CHEMBL3904996 151058 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 430 8 3 4 3.9 NC(=O)c1cc(CNc2c(F)ccc(OCC(=O)O)c2F)cc(-c2cccc(F)c2)c1 nan
53259981 183129 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 467 9 2 5 4.3 CC(C)(C)c1ccc(CN(Cc2cccc(NCC(=O)O)n2)S(=O)(=O)c2ccccc2)cc1 10.1021/acs.jmedchem.8b00808
CHEMBL4456588 183129 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 467 9 2 5 4.3 CC(C)(C)c1ccc(CN(Cc2cccc(NCC(=O)O)n2)S(=O)(=O)c2ccccc2)cc1 10.1021/acs.jmedchem.8b00808
CHEMBL4595646 183129 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 467 9 2 5 4.3 CC(C)(C)c1ccc(CN(Cc2cccc(NCC(=O)O)n2)S(=O)(=O)c2ccccc2)cc1 10.1021/acs.jmedchem.8b00808
53259984 183314 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 501 9 2 5 4.9 CC(C)(C)c1ccc(CN(Cc2cccc(NCC(=O)O)n2)S(=O)(=O)c2ccc(Cl)cc2)cc1 10.1021/acs.jmedchem.8b00808
CHEMBL4447271 183314 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 501 9 2 5 4.9 CC(C)(C)c1ccc(CN(Cc2cccc(NCC(=O)O)n2)S(=O)(=O)c2ccc(Cl)cc2)cc1 10.1021/acs.jmedchem.8b00808
CHEMBL4597100 183314 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 501 9 2 5 4.9 CC(C)(C)c1ccc(CN(Cc2cccc(NCC(=O)O)n2)S(=O)(=O)c2ccc(Cl)cc2)cc1 10.1021/acs.jmedchem.8b00808
53260154 177910 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 480 11 2 6 3.8 CCC1(c2ccc(CN(Cc3cccc(NCC(=O)O)n3)S(=O)(=O)c3cccnc3)cc2)CC1 10.1021/acs.jmedchem.8b00808
CHEMBL4458330 177910 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 480 11 2 6 3.8 CCC1(c2ccc(CN(Cc3cccc(NCC(=O)O)n3)S(=O)(=O)c3cccnc3)cc2)CC1 10.1021/acs.jmedchem.8b00808
11955276 157530 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 358 7 3 4 2.9 O=C(O)CCC/C=C\C[C@H]1C(=O)C[C@@H](O)[C@@H]1c1ccc2c(c1)CCC2O nan
CHEMBL3956391 157530 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 358 7 3 4 2.9 O=C(O)CCC/C=C\C[C@H]1C(=O)C[C@@H](O)[C@@H]1c1ccc2c(c1)CCC2O nan
22246893 202731 0 None - 1 Rat 6.4 pEC50 = 6.4 Functional
Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP releaseAgonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release
ChEMBL 371 13 1 4 2.7 CCCCc1ccc(CN(CCCCOCC(=O)O)S(C)(=O)=O)cc1 10.1016/j.bmcl.2009.01.059
CHEMBL559561 202731 0 None - 1 Rat 6.4 pEC50 = 6.4 Functional
Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP releaseAgonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release
ChEMBL 371 13 1 4 2.7 CCCCc1ccc(CN(CCCCOCC(=O)O)S(C)(=O)=O)cc1 10.1016/j.bmcl.2009.01.059
11855588 154135 0 None 12 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 345 8 1 2 4.9 CC(C)(C)c1ccc(N2C(=O)CC[C@@H]2CCCCCCC(=O)O)cc1 nan
CHEMBL3929446 154135 0 None 12 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 345 8 1 2 4.9 CC(C)(C)c1ccc(N2C(=O)CC[C@@H]2CCCCCCC(=O)O)cc1 nan
11855588 154135 0 None 12 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assayAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assay
ChEMBL 345 8 1 2 4.9 CC(C)(C)c1ccc(N2C(=O)CC[C@@H]2CCCCCCC(=O)O)cc1 nan
CHEMBL3929446 154135 0 None 12 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assayAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assay
ChEMBL 345 8 1 2 4.9 CC(C)(C)c1ccc(N2C(=O)CC[C@@H]2CCCCCCC(=O)O)cc1 nan
22246765 201977 0 None - 1 Rat 6.4 pEC50 = 6.4 Functional
Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP releaseAgonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release
ChEMBL 403 11 1 3 3.7 CCCCc1ccc(CN(CCc2ccc(CC(=O)O)cc2)S(C)(=O)=O)cc1 10.1016/j.bmcl.2009.01.059
CHEMBL550619 201977 0 None - 1 Rat 6.4 pEC50 = 6.4 Functional
Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP releaseAgonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release
ChEMBL 403 11 1 3 3.7 CCCCc1ccc(CN(CCc2ccc(CC(=O)O)cc2)S(C)(=O)=O)cc1 10.1016/j.bmcl.2009.01.059
22246895 202343 0 None - 1 Rat 6.4 pEC50 = 6.4 Functional
Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP releaseAgonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release
ChEMBL 399 14 2 4 3.7 CCCCC(O)c1ccc(CN(CCCCCCC(=O)O)S(C)(=O)=O)cc1 10.1016/j.bmcl.2009.01.059
CHEMBL554823 202343 0 None - 1 Rat 6.4 pEC50 = 6.4 Functional
Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP releaseAgonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release
ChEMBL 399 14 2 4 3.7 CCCCC(O)c1ccc(CN(CCCCCCC(=O)O)S(C)(=O)=O)cc1 10.1016/j.bmcl.2009.01.059
11855866 151380 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 403 9 2 5 4.0 CCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3907809 151380 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 403 9 2 5 4.0 CCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
11855866 151380 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assayAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assay
ChEMBL 403 9 2 5 4.0 CCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3907809 151380 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assayAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assay
ChEMBL 403 9 2 5 4.0 CCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
57564500 157989 0 None 2 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 440 12 2 2 6.8 CCCCCC(O)c1ccc([C@H]2[C@@H](Cl)C[C@@H](Cl)[C@@H]2C/C=C\CCCC(=O)O)cc1 nan
CHEMBL3959926 157989 0 None 2 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 440 12 2 2 6.8 CCCCCC(O)c1ccc([C@H]2[C@@H](Cl)C[C@@H](Cl)[C@@H]2C/C=C\CCCC(=O)O)cc1 nan
44230997 177316 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 479 10 2 9 1.9 O=C(O)CNc1cccc(CN(Cc2ccc(-n3cncn3)cc2)S(=O)(=O)c2cccnc2)n1 10.1021/acs.jmedchem.8b00808
CHEMBL4449855 177316 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 479 10 2 9 1.9 O=C(O)CNc1cccc(CN(Cc2ccc(-n3cncn3)cc2)S(=O)(=O)c2cccnc2)n1 10.1021/acs.jmedchem.8b00808
44304199 107594 0 None - 1 Mouse 7.4 pEC50 = 7.4 Functional
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptor
ChEMBL 392 12 3 4 4.0 CCCC1([C@@H](O)C/C=C/C2[C@H](O)CC(=O)[C@@H]2C/C=C/CCCC(=O)O)CCC1 10.1016/s0960-894x(01)00359-6
CHEMBL293242 107594 0 None - 1 Mouse 7.4 pEC50 = 7.4 Functional
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptor
ChEMBL 392 12 3 4 4.0 CCCC1([C@@H](O)C/C=C/C2[C@H](O)CC(=O)[C@@H]2C/C=C/CCCC(=O)O)CCC1 10.1016/s0960-894x(01)00359-6
9821171 104642 0 None -14454 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human EP2 receptor by cAMP assayAgonist activity at human EP2 receptor by cAMP assay
ChEMBL 379 8 2 3 3.1 O=C(O)c1ccc(CCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2ccccc2)cc1 10.1016/j.bmcl.2007.11.020
CHEMBL272276 104642 0 None -14454 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human EP2 receptor by cAMP assayAgonist activity at human EP2 receptor by cAMP assay
ChEMBL 379 8 2 3 3.1 O=C(O)c1ccc(CCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2ccccc2)cc1 10.1016/j.bmcl.2007.11.020
10223499 203120 0 None - 1 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP releaseAgonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release
ChEMBL 413 15 2 4 4.1 CCCCCC(O)c1ccc(CN(CCCCCCC(=O)O)S(C)(=O)=O)cc1 10.1016/j.bmcl.2009.01.059
CHEMBL562411 203120 0 None - 1 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP releaseAgonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release
ChEMBL 413 15 2 4 4.1 CCCCCC(O)c1ccc(CN(CCCCCCC(=O)O)S(C)(=O)=O)cc1 10.1016/j.bmcl.2009.01.059
11855324 149383 0 None 14 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 371 6 1 4 4.0 CC(C)(C)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)o2)cc1 nan
CHEMBL3891401 149383 0 None 14 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 371 6 1 4 4.0 CC(C)(C)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)o2)cc1 nan
11855324 149383 0 None 14 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assayAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assay
ChEMBL 371 6 1 4 4.0 CC(C)(C)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)o2)cc1 nan
CHEMBL3891401 149383 0 None 14 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assayAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assay
ChEMBL 371 6 1 4 4.0 CC(C)(C)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)o2)cc1 nan
53259982 183214 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 485 9 2 5 4.4 CC(C)(C)c1ccc(CN(Cc2cccc(NCC(=O)O)n2)S(=O)(=O)c2ccccc2F)cc1 10.1021/acs.jmedchem.8b00808
CHEMBL4561017 183214 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 485 9 2 5 4.4 CC(C)(C)c1ccc(CN(Cc2cccc(NCC(=O)O)n2)S(=O)(=O)c2ccccc2F)cc1 10.1021/acs.jmedchem.8b00808
CHEMBL4596258 183214 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 485 9 2 5 4.4 CC(C)(C)c1ccc(CN(Cc2cccc(NCC(=O)O)n2)S(=O)(=O)c2ccccc2F)cc1 10.1021/acs.jmedchem.8b00808
89443872 152619 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 437 7 2 3 6.0 O=C(O)COc1ccc(Cl)c(NCc2cc(-c3cccc(F)c3)ccc2F)c1Cl nan
CHEMBL3917219 152619 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 437 7 2 3 6.0 O=C(O)COc1ccc(Cl)c(NCc2cc(-c3cccc(F)c3)ccc2F)c1Cl nan
44304124 109400 0 None - 1 Mouse 7.4 pEC50 = 7.4 Functional
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptor
ChEMBL 406 12 3 4 4.3 CC(C)CC1([C@@H](O)C/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2C/C=C\CCCC(=O)O)CCC1 10.1016/s0960-894x(01)00359-6
CHEMBL304225 109400 0 None - 1 Mouse 7.4 pEC50 = 7.4 Functional
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptor
ChEMBL 406 12 3 4 4.3 CC(C)CC1([C@@H](O)C/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2C/C=C\CCCC(=O)O)CCC1 10.1016/s0960-894x(01)00359-6
11955297 156666 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 416 10 3 4 4.8 O=C(O)CCCCCC[C@H]1C(=O)C[C@@H](O)[C@@H]1c1ccc(C(O)C2CCCCC2)cc1 nan
CHEMBL3949225 156666 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 416 10 3 4 4.8 O=C(O)CCCCCC[C@H]1C(=O)C[C@@H](O)[C@@H]1c1ccc(C(O)C2CCCCC2)cc1 nan
22246983 202641 0 None - 1 Rat 6.3 pEC50 = 6.3 Functional
Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP releaseAgonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release
ChEMBL 389 11 1 3 4.2 CS(=O)(=O)N(CCCCCCC(=O)O)Cc1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2009.01.059
CHEMBL558671 202641 0 None - 1 Rat 6.3 pEC50 = 6.3 Functional
Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP releaseAgonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release
ChEMBL 389 11 1 3 4.2 CS(=O)(=O)N(CCCCCCC(=O)O)Cc1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2009.01.059
23729077 84993 31 None - 1 Human 7.3 pEC50 = 7.3 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 520 11 0 8 4.0 CC(C)OC(=O)COc1cccc(CN(Cc2ccc(-n3cccn3)cc2)S(=O)(=O)c2cccnc2)c1 nan
CHEMBL2105692 84993 31 None - 1 Human 7.3 pEC50 = 7.3 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 520 11 0 8 4.0 CC(C)OC(=O)COc1cccc(CN(Cc2ccc(-n3cccn3)cc2)S(=O)(=O)c2cccnc2)c1 nan
57894063 81940 0 None -301 2 Rat 5.3 pEC50 = 5.3 Functional
Agonist activity at rat EP2 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP2 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
ChEMBL 524 11 2 7 4.8 COc1ccc(-c2cccc(C[C@H](O)/C=C/[C@H]3CCC(=O)N3CCSc3nc(C(=O)O)cs3)c2)cc1 10.1016/j.bmc.2012.04.008
CHEMBL2036319 81940 0 None -301 2 Rat 5.3 pEC50 = 5.3 Functional
Agonist activity at rat EP2 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP2 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
ChEMBL 524 11 2 7 4.8 COc1ccc(-c2cccc(C[C@H](O)/C=C/[C@H]3CCC(=O)N3CCSc3nc(C(=O)O)cs3)c2)cc1 10.1016/j.bmc.2012.04.008
156010583 183857 0 None -162 2 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human EP2 receptor expressed in HEK293 cells by calcium-5 dye based FLIPR assayAgonist activity at human EP2 receptor expressed in HEK293 cells by calcium-5 dye based FLIPR assay
ChEMBL 451 10 2 4 5.4 CCCCCC(C)(O)/C=C/c1c(Cl)cc(Cl)c(=O)n1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2020.127104
CHEMBL4633041 183857 0 None -162 2 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human EP2 receptor expressed in HEK293 cells by calcium-5 dye based FLIPR assayAgonist activity at human EP2 receptor expressed in HEK293 cells by calcium-5 dye based FLIPR assay
ChEMBL 451 10 2 4 5.4 CCCCCC(C)(O)/C=C/c1c(Cl)cc(Cl)c(=O)n1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2020.127104
45271238 202420 0 None - 1 Rat 7.3 pEC50 = 7.3 Functional
Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP releaseAgonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release
ChEMBL 403 8 1 3 4.0 CC(C)(C)c1ccc(CN(Cc2cccc(CCC(=O)O)c2)S(C)(=O)=O)cc1 10.1016/j.bmcl.2009.01.059
CHEMBL556333 202420 0 None - 1 Rat 7.3 pEC50 = 7.3 Functional
Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP releaseAgonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release
ChEMBL 403 8 1 3 4.0 CC(C)(C)c1ccc(CN(Cc2cccc(CCC(=O)O)c2)S(C)(=O)=O)cc1 10.1016/j.bmcl.2009.01.059
59465587 151968 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 372 13 2 2 6.5 CCCCCC(O)c1ccc([C@H]2CCC=C2CCCCCCC(=O)O)cc1 nan
CHEMBL3912391 151968 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 372 13 2 2 6.5 CCCCCC(O)c1ccc([C@H]2CCC=C2CCCCCCC(=O)O)cc1 nan
11955315 150569 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 394 9 3 3 4.6 CC(C)C(O)c1ccc([C@H]2[C@H](O)C[C@@H](Cl)[C@@H]2C/C=C\CCCC(=O)O)cc1 nan
CHEMBL3901088 150569 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 394 9 3 3 4.6 CC(C)C(O)c1ccc([C@H]2[C@H](O)C[C@@H](Cl)[C@@H]2C/C=C\CCCC(=O)O)cc1 nan
11955256 150094 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 424 9 2 4 5.4 COC(=O)CCCCCC[C@@H]1[C@@H](c2ccc(C(O)C(C)(C)C)cc2)[C@H](O)C[C@H]1Cl nan
CHEMBL3897181 150094 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 424 9 2 4 5.4 COC(=O)CCCCCC[C@@H]1[C@@H](c2ccc(C(O)C(C)(C)C)cc2)[C@H](O)C[C@H]1Cl nan
16725337 156380 0 None 4 4 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 443 12 2 4 6.0 CCCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2CCCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3947001 156380 0 None 4 4 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 443 12 2 4 6.0 CCCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2CCCc2ccc(C(=O)O)s2)cc1 nan
16725337 156380 0 None 4 4 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assayAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assay
ChEMBL 443 12 2 4 6.0 CCCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2CCCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3947001 156380 0 None 4 4 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assayAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assay
ChEMBL 443 12 2 4 6.0 CCCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2CCCc2ccc(C(=O)O)s2)cc1 nan
89443809 154924 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 427 8 2 4 5.3 COc1c(C)cc(-c2cccc(F)c2)cc1CNc1c(F)ccc(OCC(=O)O)c1C nan
CHEMBL3935521 154924 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 427 8 2 4 5.3 COc1c(C)cc(-c2cccc(F)c2)cc1CNc1c(F)ccc(OCC(=O)O)c1C nan
89443631 155444 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 415 7 2 3 5.5 Cc1c(F)cc(-c2cccc(F)c2)cc1CNc1c(F)ccc(OCC(=O)O)c1C nan
CHEMBL3939716 155444 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 415 7 2 3 5.5 Cc1c(F)cc(-c2cccc(F)c2)cc1CNc1c(F)ccc(OCC(=O)O)c1C nan
127050450 147078 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
ChEMBL 393 5 2 6 3.3 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3COc3cccc(F)c3)O2)n1 10.1021/acsmedchemlett.5b00455
CHEMBL3806076 147078 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
ChEMBL 393 5 2 6 3.3 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3COc3cccc(F)c3)O2)n1 10.1021/acsmedchemlett.5b00455
57395059 76249 0 None -11 3 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
ChEMBL 418 9 2 6 3.1 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2ccccc2)n1 10.1021/acsmedchemlett.5b00455
CHEMBL1933725 76249 0 None -11 3 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
ChEMBL 418 9 2 6 3.1 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2ccccc2)n1 10.1021/acsmedchemlett.5b00455
44229605 183433 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 452 9 2 7 3.1 O=C(O)CNc1cccc(CN(Cc2cc3ccccc3o2)S(=O)(=O)c2cccnc2)n1 10.1021/acs.jmedchem.8b00808
CHEMBL4470479 183433 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 452 9 2 7 3.1 O=C(O)CNc1cccc(CN(Cc2cc3ccccc3o2)S(=O)(=O)c2cccnc2)n1 10.1021/acs.jmedchem.8b00808
CHEMBL4598070 183433 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 452 9 2 7 3.1 O=C(O)CNc1cccc(CN(Cc2cc3ccccc3o2)S(=O)(=O)c2cccnc2)n1 10.1021/acs.jmedchem.8b00808
89443989 155447 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 419 7 2 3 5.3 Cc1cc(OCC(=O)O)c(F)c(NCc2cc(-c3cccc(F)c3)ccc2F)c1F nan
CHEMBL3939740 155447 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 419 7 2 3 5.3 Cc1cc(OCC(=O)O)c(F)c(NCc2cc(-c3cccc(F)c3)ccc2F)c1F nan
44444714 100913 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human prostaglandin EP2 receptorAgonist activity at human prostaglandin EP2 receptor
ChEMBL 362 10 2 4 2.6 CCCC(C)C(O)CCN1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.09.074
CHEMBL249341 100913 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human prostaglandin EP2 receptorAgonist activity at human prostaglandin EP2 receptor
ChEMBL 362 10 2 4 2.6 CCCC(C)C(O)CCN1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.09.074
59465588 150304 0 None - 1 Human 4.3 pEC50 = 4.3 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 422 13 1 3 6.9 CCCCCC(O)c1ccc([C@H]2CC[C@@H](Cl)[C@@H]2CCCCCCC(=O)OC)cc1 nan
CHEMBL3898887 150304 0 None - 1 Human 4.3 pEC50 = 4.3 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 422 13 1 3 6.9 CCCCCC(O)c1ccc([C@H]2CC[C@@H](Cl)[C@@H]2CCCCCCC(=O)OC)cc1 nan
59465575 151845 0 None - 1 Human 4.3 pEC50 = 4.3 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 402 13 1 4 5.9 CCCCCC(O)c1cccc([C@H]2CCC(=O)[C@@H]2CCCCCCC(=O)OC)c1 nan
CHEMBL3911438 151845 0 None - 1 Human 4.3 pEC50 = 4.3 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 402 13 1 4 5.9 CCCCCC(O)c1cccc([C@H]2CCC(=O)[C@@H]2CCCCCCC(=O)OC)c1 nan
59465595 152201 0 None - 1 Human 4.3 pEC50 = 4.3 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 388 13 2 3 5.8 CCCCCC(O)c1cccc([C@H]2CCC(=O)[C@@H]2CCCCCCC(=O)O)c1 nan
CHEMBL3914108 152201 0 None - 1 Human 4.3 pEC50 = 4.3 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 388 13 2 3 5.8 CCCCCC(O)c1cccc([C@H]2CCC(=O)[C@@H]2CCCCCCC(=O)O)c1 nan
59465592 156481 0 None - 1 Human 4.3 pEC50 = 4.3 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 386 13 1 3 6.6 CCCCCC(O)c1ccc([C@H]2CCC=C2CCCCCCC(=O)OC)cc1 nan
CHEMBL3947785 156481 0 None - 1 Human 4.3 pEC50 = 4.3 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 386 13 1 3 6.6 CCCCCC(O)c1ccc([C@H]2CCC=C2CCCCCCC(=O)OC)cc1 nan
59465590 157724 0 None - 1 Human 4.3 pEC50 = 4.3 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 406 13 1 3 6.6 CCCCCC(O)c1ccc([C@H]2CC[C@@H](F)[C@@H]2CCCCCCC(=O)OC)cc1 nan
CHEMBL3957958 157724 0 None - 1 Human 4.3 pEC50 = 4.3 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 406 13 1 3 6.6 CCCCCC(O)c1ccc([C@H]2CC[C@@H](F)[C@@H]2CCCCCCC(=O)OC)cc1 nan
59465584 158209 0 None - 1 Human 4.3 pEC50 = 4.3 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 394 13 2 2 6.7 CCCCCC(O)c1ccc([C@H]2CC[C@@H](Cl)[C@@H]2CCCCCCCO)cc1 nan
CHEMBL3961847 158209 0 None - 1 Human 4.3 pEC50 = 4.3 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 394 13 2 2 6.7 CCCCCC(O)c1ccc([C@H]2CC[C@@H](Cl)[C@@H]2CCCCCCCO)cc1 nan
11855325 151469 0 None 19 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assayAgonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assay
ChEMBL 387 6 1 4 4.5 CC(C)(C)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3908484 151469 0 None 19 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assayAgonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assay
ChEMBL 387 6 1 4 4.5 CC(C)(C)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
11955233 152371 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 392 8 3 3 4.3 O=C(O)CCC/C=C\C[C@@H]1[C@@H](c2ccc(C3(O)CCC3)cc2)[C@H](O)C[C@H]1Cl nan
CHEMBL3915426 152371 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 392 8 3 3 4.3 O=C(O)CCC/C=C\C[C@@H]1[C@@H](c2ccc(C3(O)CCC3)cc2)[C@H](O)C[C@H]1Cl nan
11855593 153612 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assayAgonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assay
ChEMBL 425 11 2 4 4.7 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2cccc(C(=O)O)c2)cc1 nan
CHEMBL3924987 153612 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assayAgonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assay
ChEMBL 425 11 2 4 4.7 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2cccc(C(=O)O)c2)cc1 nan
89444078 152852 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 405 7 2 3 5.0 O=C(O)COc1ccc(F)c(NCc2cc(F)cc(-c3cccc(F)c3)c2)c1F nan
CHEMBL3919144 152852 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 405 7 2 3 5.0 O=C(O)COc1ccc(F)c(NCc2cc(F)cc(-c3cccc(F)c3)c2)c1F nan
11955406 152882 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 376 10 3 4 3.4 CC(C)(CO)c1ccc([C@H]2[C@H](O)CC(=O)[C@@H]2CCCCCCC(=O)O)cc1 nan
CHEMBL3919393 152882 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 376 10 3 4 3.4 CC(C)(CO)c1ccc([C@H]2[C@H](O)CC(=O)[C@@H]2CCCCCCC(=O)O)cc1 nan
11955294 151546 0 None 1 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 380 8 3 3 4.2 O=C(O)CCCCCC[C@@H]1[C@@H](c2ccc3c(c2)CCC3O)[C@H](O)C[C@H]1Cl nan
CHEMBL3909111 151546 0 None 1 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 380 8 3 3 4.2 O=C(O)CCCCCC[C@@H]1[C@@H](c2ccc3c(c2)CCC3O)[C@H](O)C[C@H]1Cl nan
44303889 209996 0 None - 1 Mouse 7.3 pEC50 = 7.3 Functional
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptor
ChEMBL 414 10 3 4 4.2 CCCC1([C@@H](O)C/C=C/C2[C@H](O)CC(=O)[C@@H]2CCc2ccc(C(=O)O)cc2)CCC1 10.1016/s0960-894x(01)00359-6
CHEMBL64423 209996 0 None - 1 Mouse 7.3 pEC50 = 7.3 Functional
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptor
ChEMBL 414 10 3 4 4.2 CCCC1([C@@H](O)C/C=C/C2[C@H](O)CC(=O)[C@@H]2CCc2ccc(C(=O)O)cc2)CCC1 10.1016/s0960-894x(01)00359-6
11955179 153260 0 None 5 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 450 12 3 3 6.2 CCCC1(C(O)c2cccc([C@H]3[C@H](O)C[C@@H](Cl)[C@@H]3CCCCCCC(=O)O)c2)CCC1 nan
CHEMBL3922332 153260 0 None 5 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 450 12 3 3 6.2 CCCC1(C(O)c2cccc([C@H]3[C@H](O)C[C@@H](Cl)[C@@H]3CCCCCCC(=O)O)c2)CCC1 nan
11855588 154135 0 None 12 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assayAgonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assay
ChEMBL 345 8 1 2 4.9 CC(C)(C)c1ccc(N2C(=O)CC[C@@H]2CCCCCCC(=O)O)cc1 nan
CHEMBL3929446 154135 0 None 12 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assayAgonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assay
ChEMBL 345 8 1 2 4.9 CC(C)(C)c1ccc(N2C(=O)CC[C@@H]2CCCCCCC(=O)O)cc1 nan
126495432 146102 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assayAgonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assay
ChEMBL 406 5 2 5 4.2 Cc1cc(OC[C@H]2[C@H](O)C[C@@H]3O[C@@H](c4coc(C(=O)O)c4)CC[C@@H]32)ccc1Cl 10.1016/j.bmcl.2016.03.110
CHEMBL3792668 146102 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assayAgonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assay
ChEMBL 406 5 2 5 4.2 Cc1cc(OC[C@H]2[C@H](O)C[C@@H]3O[C@@H](c4coc(C(=O)O)c4)CC[C@@H]32)ccc1Cl 10.1016/j.bmcl.2016.03.110
71515517 154861 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 419 7 2 3 5.3 Cc1cc(CNc2c(F)ccc(OCC(=O)O)c2F)c(F)c(-c2cccc(F)c2)c1 nan
CHEMBL3934986 154861 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 419 7 2 3 5.3 Cc1cc(CNc2c(F)ccc(OCC(=O)O)c2F)c(F)c(-c2cccc(F)c2)c1 nan
56839343 151057 0 None -147 6 Human 5.3 pEC50 = 5.3 Functional
Cell Based Assay: Ca2+ signaling studies were performed using a FLIPR TETRA system (Molecular Devices, Sunnyvale, Calif., USA) in the 384-format. This is a high-throughput instrument for cell-based assays to monitor Ca2+ signaling associated with GPCRs and ion channels. Cells were seeded at a density of 5×104 cells/well in BioCoat poly-D-lysine coated, black wall, clear bottom 384-well plates (BD Biosciences, Franklin lakes, NJ, USA) and allowed to attach overnight in an incubator at 37° C. The cells were then washed twice with HBSS-HEPES buffer (Hanks' balanced salt solution without bicarbonate and phenol red, 20 mM HEPES, pH 7.4) using an ELx405 Select CW Microplate Washer (BioTek, Winooski, Vt., USA). After 60 min of dye-loading in the dark using the Ca2+-sensitive dye Fluo-4AM (Invitrogen, Carlsbad, Calif., USA), at a final concentration of 2×10^−6M, the plates were washed 4 times with HBSS-HEPES buffer to remove excess dye and leaving 50 μl of buffer in each well. The plates were then placed in the FLIPR TETRA instrument and allowed to equilibrate at 37° C. AGN-211377 was added in a 25 μl volume to each well to give final concentrations of 0.1 μM, 0.3 μM, 1 μM, 3 μM, 10 μM, and 30 μM; or 0.067 μM, 0.1 μM, 0.2 μM, 0.3 μM, 0.67 μM, and 1 μM for cells over-expressing TP receptors. After 4.5 minutes, a 7-point serial dilution of the standard agonist for the corresponding receptor, in a 25 μl volume was injected at the final concentrations from 10^−11M to 10^−5M in 10-fold serial dilution increments for cells expressing human recombinant DP1, EP1, EP2, EP3, EP4, FP, and IP receptors. The dose range for the standard agonist for human recombinant TP receptors was from 10^−12M to 10^−6M. HBSS-HEPES buffer was used as the negative control for the standard agonists. Cells were excited with LED (light emitting diode) excitation at 470-495 nm and emission was measured through an emission filter at 515-575 nm. Assay plates were read for 3.5 minutes using the FLIPRTETRA.Cell Based Assay: Ca2+ signaling studies were performed using a FLIPR TETRA system (Molecular Devices, Sunnyvale, Calif., USA) in the 384-format. This is a high-throughput instrument for cell-based assays to monitor Ca2+ signaling associated with GPCRs and ion channels. Cells were seeded at a density of 5×104 cells/well in BioCoat poly-D-lysine coated, black wall, clear bottom 384-well plates (BD Biosciences, Franklin lakes, NJ, USA) and allowed to attach overnight in an incubator at 37° C. The cells were then washed twice with HBSS-HEPES buffer (Hanks' balanced salt solution without bicarbonate and phenol red, 20 mM HEPES, pH 7.4) using an ELx405 Select CW Microplate Washer (BioTek, Winooski, Vt., USA). After 60 min of dye-loading in the dark using the Ca2+-sensitive dye Fluo-4AM (Invitrogen, Carlsbad, Calif., USA), at a final concentration of 2×10^−6M, the plates were washed 4 times with HBSS-HEPES buffer to remove excess dye and leaving 50 μl of buffer in each well. The plates were then placed in the FLIPR TETRA instrument and allowed to equilibrate at 37° C. AGN-211377 was added in a 25 μl volume to each well to give final concentrations of 0.1 μM, 0.3 μM, 1 μM, 3 μM, 10 μM, and 30 μM; or 0.067 μM, 0.1 μM, 0.2 μM, 0.3 μM, 0.67 μM, and 1 μM for cells over-expressing TP receptors. After 4.5 minutes, a 7-point serial dilution of the standard agonist for the corresponding receptor, in a 25 μl volume was injected at the final concentrations from 10^−11M to 10^−5M in 10-fold serial dilution increments for cells expressing human recombinant DP1, EP1, EP2, EP3, EP4, FP, and IP receptors. The dose range for the standard agonist for human recombinant TP receptors was from 10^−12M to 10^−6M. HBSS-HEPES buffer was used as the negative control for the standard agonists. Cells were excited with LED (light emitting diode) excitation at 470-495 nm and emission was measured through an emission filter at 515-575 nm. Assay plates were read for 3.5 minutes using the FLIPRTETRA.
ChEMBL 642 14 2 8 5.4 COc1ccc(CCC(=O)NS(=O)(=O)C(F)(F)F)c(CN2CCC[C@H]2c2nc(C(=O)NCCCCC3CCCCC3)co2)c1 nan
CHEMBL3904989 151057 0 None -147 6 Human 5.3 pEC50 = 5.3 Functional
Cell Based Assay: Ca2+ signaling studies were performed using a FLIPR TETRA system (Molecular Devices, Sunnyvale, Calif., USA) in the 384-format. This is a high-throughput instrument for cell-based assays to monitor Ca2+ signaling associated with GPCRs and ion channels. Cells were seeded at a density of 5×104 cells/well in BioCoat poly-D-lysine coated, black wall, clear bottom 384-well plates (BD Biosciences, Franklin lakes, NJ, USA) and allowed to attach overnight in an incubator at 37° C. The cells were then washed twice with HBSS-HEPES buffer (Hanks' balanced salt solution without bicarbonate and phenol red, 20 mM HEPES, pH 7.4) using an ELx405 Select CW Microplate Washer (BioTek, Winooski, Vt., USA). After 60 min of dye-loading in the dark using the Ca2+-sensitive dye Fluo-4AM (Invitrogen, Carlsbad, Calif., USA), at a final concentration of 2×10^−6M, the plates were washed 4 times with HBSS-HEPES buffer to remove excess dye and leaving 50 μl of buffer in each well. The plates were then placed in the FLIPR TETRA instrument and allowed to equilibrate at 37° C. AGN-211377 was added in a 25 μl volume to each well to give final concentrations of 0.1 μM, 0.3 μM, 1 μM, 3 μM, 10 μM, and 30 μM; or 0.067 μM, 0.1 μM, 0.2 μM, 0.3 μM, 0.67 μM, and 1 μM for cells over-expressing TP receptors. After 4.5 minutes, a 7-point serial dilution of the standard agonist for the corresponding receptor, in a 25 μl volume was injected at the final concentrations from 10^−11M to 10^−5M in 10-fold serial dilution increments for cells expressing human recombinant DP1, EP1, EP2, EP3, EP4, FP, and IP receptors. The dose range for the standard agonist for human recombinant TP receptors was from 10^−12M to 10^−6M. HBSS-HEPES buffer was used as the negative control for the standard agonists. Cells were excited with LED (light emitting diode) excitation at 470-495 nm and emission was measured through an emission filter at 515-575 nm. Assay plates were read for 3.5 minutes using the FLIPRTETRA.Cell Based Assay: Ca2+ signaling studies were performed using a FLIPR TETRA system (Molecular Devices, Sunnyvale, Calif., USA) in the 384-format. This is a high-throughput instrument for cell-based assays to monitor Ca2+ signaling associated with GPCRs and ion channels. Cells were seeded at a density of 5×104 cells/well in BioCoat poly-D-lysine coated, black wall, clear bottom 384-well plates (BD Biosciences, Franklin lakes, NJ, USA) and allowed to attach overnight in an incubator at 37° C. The cells were then washed twice with HBSS-HEPES buffer (Hanks' balanced salt solution without bicarbonate and phenol red, 20 mM HEPES, pH 7.4) using an ELx405 Select CW Microplate Washer (BioTek, Winooski, Vt., USA). After 60 min of dye-loading in the dark using the Ca2+-sensitive dye Fluo-4AM (Invitrogen, Carlsbad, Calif., USA), at a final concentration of 2×10^−6M, the plates were washed 4 times with HBSS-HEPES buffer to remove excess dye and leaving 50 μl of buffer in each well. The plates were then placed in the FLIPR TETRA instrument and allowed to equilibrate at 37° C. AGN-211377 was added in a 25 μl volume to each well to give final concentrations of 0.1 μM, 0.3 μM, 1 μM, 3 μM, 10 μM, and 30 μM; or 0.067 μM, 0.1 μM, 0.2 μM, 0.3 μM, 0.67 μM, and 1 μM for cells over-expressing TP receptors. After 4.5 minutes, a 7-point serial dilution of the standard agonist for the corresponding receptor, in a 25 μl volume was injected at the final concentrations from 10^−11M to 10^−5M in 10-fold serial dilution increments for cells expressing human recombinant DP1, EP1, EP2, EP3, EP4, FP, and IP receptors. The dose range for the standard agonist for human recombinant TP receptors was from 10^−12M to 10^−6M. HBSS-HEPES buffer was used as the negative control for the standard agonists. Cells were excited with LED (light emitting diode) excitation at 470-495 nm and emission was measured through an emission filter at 515-575 nm. Assay plates were read for 3.5 minutes using the FLIPRTETRA.
ChEMBL 642 14 2 8 5.4 COc1ccc(CCC(=O)NS(=O)(=O)C(F)(F)F)c(CN2CCC[C@H]2c2nc(C(=O)NCCCCC3CCCCC3)co2)c1 nan
45266955 202424 0 None - 1 Rat 7.2 pEC50 = 7.2 Functional
Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP releaseAgonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release
ChEMBL 485 10 1 6 3.7 Cn1ccnc1CS(=O)(=O)N(Cc1ccc(C(C)(C)C)cc1)Cc1cccc(OCC(=O)O)c1 10.1016/j.bmcl.2009.01.059
CHEMBL556416 202424 0 None - 1 Rat 7.2 pEC50 = 7.2 Functional
Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP releaseAgonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release
ChEMBL 485 10 1 6 3.7 Cn1ccnc1CS(=O)(=O)N(Cc1ccc(C(C)(C)C)cc1)Cc1cccc(OCC(=O)O)c1 10.1016/j.bmcl.2009.01.059
57564500 157989 0 None 2 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assayAgonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assay
ChEMBL 440 12 2 2 6.8 CCCCCC(O)c1ccc([C@H]2[C@@H](Cl)C[C@@H](Cl)[C@@H]2C/C=C\CCCC(=O)O)cc1 nan
CHEMBL3959926 157989 0 None 2 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assayAgonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assay
ChEMBL 440 12 2 2 6.8 CCCCCC(O)c1ccc([C@H]2[C@@H](Cl)C[C@@H](Cl)[C@@H]2C/C=C\CCCC(=O)O)cc1 nan
44303723 209714 0 None - 1 Mouse 6.2 pEC50 = 6.2 Functional
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptor
ChEMBL 406 12 3 4 4.4 CCCC1([C@@H](O)C/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2C/C=C\CCCC(=O)O)CCCC1 10.1016/s0960-894x(01)00359-6
CHEMBL62885 209714 0 None - 1 Mouse 6.2 pEC50 = 6.2 Functional
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptor
ChEMBL 406 12 3 4 4.4 CCCC1([C@@H](O)C/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2C/C=C\CCCC(=O)O)CCCC1 10.1016/s0960-894x(01)00359-6
45269576 202762 0 None - 1 Rat 6.2 pEC50 = 6.2 Functional
Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP releaseAgonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release
ChEMBL 403 11 1 3 4.4 CCCCc1ccc(CN(c2ccc(CCCC(=O)O)cc2)S(C)(=O)=O)cc1 10.1016/j.bmcl.2009.01.059
CHEMBL559820 202762 0 None - 1 Rat 6.2 pEC50 = 6.2 Functional
Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP releaseAgonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release
ChEMBL 403 11 1 3 4.4 CCCCc1ccc(CN(c2ccc(CCCC(=O)O)cc2)S(C)(=O)=O)cc1 10.1016/j.bmcl.2009.01.059
9863804 100873 0 None -120 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human prostaglandin EP2 receptorAgonist activity at human prostaglandin EP2 receptor
ChEMBL 362 11 2 4 2.7 CCCCCC(O)CCN1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.09.074
CHEMBL249136 100873 0 None -120 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human prostaglandin EP2 receptorAgonist activity at human prostaglandin EP2 receptor
ChEMBL 362 11 2 4 2.7 CCCCCC(O)CCN1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.09.074
89444271 158687 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 411 7 2 3 5.6 Cc1cc(-c2cccc(F)c2)cc(CNc2c(F)ccc(OCC(=O)O)c2C)c1C nan
CHEMBL3966050 158687 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 411 7 2 3 5.6 Cc1cc(-c2cccc(F)c2)cc(CNc2c(F)ccc(OCC(=O)O)c2C)c1C nan
53259983 183080 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 485 9 2 5 4.4 CC(C)(C)c1ccc(CN(Cc2cccc(NCC(=O)O)n2)S(=O)(=O)c2cccc(F)c2)cc1 10.1021/acs.jmedchem.8b00808
CHEMBL4587628 183080 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 485 9 2 5 4.4 CC(C)(C)c1ccc(CN(Cc2cccc(NCC(=O)O)n2)S(=O)(=O)c2cccc(F)c2)cc1 10.1021/acs.jmedchem.8b00808
CHEMBL4595199 183080 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 485 9 2 5 4.4 CC(C)(C)c1ccc(CN(Cc2cccc(NCC(=O)O)n2)S(=O)(=O)c2cccc(F)c2)cc1 10.1021/acs.jmedchem.8b00808
2720 10626 59 None -10 5 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human EP2 expressed in HEK293 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysisAgonist activity at human EP2 expressed in HEK293 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysis
ChEMBL 390 10 3 4 3.6 CCCCC[C@@H](CC[C@H]1[C@H](O)C[C@H]2[C@@H]1Cc1cccc(c1C2)OCC(=O)O)O 10.1016/j.ejmech.2022.114154
5820 10626 59 None -10 5 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human EP2 expressed in HEK293 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysisAgonist activity at human EP2 expressed in HEK293 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysis
ChEMBL 390 10 3 4 3.6 CCCCC[C@@H](CC[C@H]1[C@H](O)C[C@H]2[C@@H]1Cc1cccc(c1C2)OCC(=O)O)O 10.1016/j.ejmech.2022.114154
6918140 10626 59 None -10 5 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human EP2 expressed in HEK293 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysisAgonist activity at human EP2 expressed in HEK293 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysis
ChEMBL 390 10 3 4 3.6 CCCCC[C@@H](CC[C@H]1[C@H](O)C[C@H]2[C@@H]1Cc1cccc(c1C2)OCC(=O)O)O 10.1016/j.ejmech.2022.114154
CHEMBL1237119 10626 59 None -10 5 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human EP2 expressed in HEK293 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysisAgonist activity at human EP2 expressed in HEK293 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysis
ChEMBL 390 10 3 4 3.6 CCCCC[C@@H](CC[C@H]1[C@H](O)C[C@H]2[C@@H]1Cc1cccc(c1C2)OCC(=O)O)O 10.1016/j.ejmech.2022.114154
DB00374 10626 59 None -10 5 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human EP2 expressed in HEK293 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysisAgonist activity at human EP2 expressed in HEK293 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysis
ChEMBL 390 10 3 4 3.6 CCCCC[C@@H](CC[C@H]1[C@H](O)C[C@H]2[C@@H]1Cc1cccc(c1C2)OCC(=O)O)O 10.1016/j.ejmech.2022.114154
127052577 147038 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
ChEMBL 409 5 2 6 3.8 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3COc3cccc(Cl)c3)O2)n1 10.1021/acsmedchemlett.5b00455
CHEMBL3805596 147038 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
ChEMBL 409 5 2 6 3.8 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3COc3cccc(Cl)c3)O2)n1 10.1021/acsmedchemlett.5b00455
67082722 171407 0 None 2 3 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at recombinant human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIAAgonist activity at recombinant human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIA
ChEMBL 425 12 2 6 5.2 CCCCC[C@@](C)(O)C/C=C/[C@H]1CCC(=O)[C@@H]1CCSc1nc(C(=O)O)cs1 10.1016/j.bmc.2017.11.035
CHEMBL4216182 171407 0 None 2 3 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at recombinant human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIAAgonist activity at recombinant human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIA
ChEMBL 425 12 2 6 5.2 CCCCC[C@@](C)(O)C/C=C/[C@H]1CCC(=O)[C@@H]1CCSc1nc(C(=O)O)cs1 10.1016/j.bmc.2017.11.035
8541 9718 2 None -66069 4 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human EP2 receptor expressed in HEK293T/17 cells assessed as increase in GalphaS-mediated CREB activation measured after 6 to 24 hrs by SEAP reporter gene-based chemiluminescence assayAgonist activity at human EP2 receptor expressed in HEK293T/17 cells assessed as increase in GalphaS-mediated CREB activation measured after 6 to 24 hrs by SEAP reporter gene-based chemiluminescence assay
ChEMBL 436 13 3 6 2.8 COCc1cccc(c1)C[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCSCCCC(=O)O)O 10.1021/acs.jmedchem.9b00336
9824353 9718 2 None -66069 4 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human EP2 receptor expressed in HEK293T/17 cells assessed as increase in GalphaS-mediated CREB activation measured after 6 to 24 hrs by SEAP reporter gene-based chemiluminescence assayAgonist activity at human EP2 receptor expressed in HEK293T/17 cells assessed as increase in GalphaS-mediated CREB activation measured after 6 to 24 hrs by SEAP reporter gene-based chemiluminescence assay
ChEMBL 436 13 3 6 2.8 COCc1cccc(c1)C[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCSCCCC(=O)O)O 10.1021/acs.jmedchem.9b00336
CHEMBL292964 9718 2 None -66069 4 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human EP2 receptor expressed in HEK293T/17 cells assessed as increase in GalphaS-mediated CREB activation measured after 6 to 24 hrs by SEAP reporter gene-based chemiluminescence assayAgonist activity at human EP2 receptor expressed in HEK293T/17 cells assessed as increase in GalphaS-mediated CREB activation measured after 6 to 24 hrs by SEAP reporter gene-based chemiluminescence assay
ChEMBL 436 13 3 6 2.8 COCc1cccc(c1)C[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCSCCCC(=O)O)O 10.1021/acs.jmedchem.9b00336
155527947 183313 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 501 9 2 5 4.9 CC(C)(C)c1ccc(CN(Cc2cccc(NCC(=O)O)n2)S(=O)(=O)c2cccc(Cl)c2)cc1 10.1021/acs.jmedchem.8b00808
CHEMBL4460294 183313 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 501 9 2 5 4.9 CC(C)(C)c1ccc(CN(Cc2cccc(NCC(=O)O)n2)S(=O)(=O)c2cccc(Cl)c2)cc1 10.1021/acs.jmedchem.8b00808
CHEMBL4597099 183313 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 501 9 2 5 4.9 CC(C)(C)c1ccc(CN(Cc2cccc(NCC(=O)O)n2)S(=O)(=O)c2cccc(Cl)c2)cc1 10.1021/acs.jmedchem.8b00808
11955157 159422 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 430 12 3 4 5.1 CCCC1(C(O)c2cccc([C@H]3[C@H](O)CC(=O)[C@@H]3CCCCCCC(=O)O)c2)CCC1 nan
CHEMBL3972401 159422 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 430 12 3 4 5.1 CCCC1(C(O)c2cccc([C@H]3[C@H](O)CC(=O)[C@@H]3CCCCCCC(=O)O)c2)CCC1 nan
56649302 159445 0 None -169 6 Human 5.2 pEC50 = 5.2 Functional
Cell Based Assay: Ca2+ signaling studies were performed using a FLIPR TETRA system (Molecular Devices, Sunnyvale, Calif., USA) in the 384-format. This is a high-throughput instrument for cell-based assays to monitor Ca2+ signaling associated with GPCRs and ion channels. Cells were seeded at a density of 5×104 cells/well in BioCoat poly-D-lysine coated, black wall, clear bottom 384-well plates (BD Biosciences, Franklin lakes, NJ, USA) and allowed to attach overnight in an incubator at 37° C. The cells were then washed twice with HBSS-HEPES buffer (Hanks' balanced salt solution without bicarbonate and phenol red, 20 mM HEPES, pH 7.4) using an ELx405 Select CW Microplate Washer (BioTek, Winooski, Vt., USA). After 60 min of dye-loading in the dark using the Ca2+-sensitive dye Fluo-4AM (Invitrogen, Carlsbad, Calif., USA), at a final concentration of 2×10^−6M, the plates were washed 4 times with HBSS-HEPES buffer to remove excess dye and leaving 50 μl of buffer in each well. The plates were then placed in the FLIPR TETRA instrument and allowed to equilibrate at 37° C. AGN-211377 was added in a 25 μl volume to each well to give final concentrations of 0.1 μM, 0.3 μM, 1 μM, 3 μM, 10 μM, and 30 μM; or 0.067 μM, 0.1 μM, 0.2 μM, 0.3 μM, 0.67 μM, and 1 μM for cells over-expressing TP receptors. After 4.5 minutes, a 7-point serial dilution of the standard agonist for the corresponding receptor, in a 25 μl volume was injected at the final concentrations from 10^−11M to 10^−5M in 10-fold serial dilution increments for cells expressing human recombinant DP1, EP1, EP2, EP3, EP4, FP, and IP receptors. The dose range for the standard agonist for human recombinant TP receptors was from 10^−12M to 10^−6M. HBSS-HEPES buffer was used as the negative control for the standard agonists. Cells were excited with LED (light emitting diode) excitation at 470-495 nm and emission was measured through an emission filter at 515-575 nm. Assay plates were read for 3.5 minutes using the FLIPRTETRA.Cell Based Assay: Ca2+ signaling studies were performed using a FLIPR TETRA system (Molecular Devices, Sunnyvale, Calif., USA) in the 384-format. This is a high-throughput instrument for cell-based assays to monitor Ca2+ signaling associated with GPCRs and ion channels. Cells were seeded at a density of 5×104 cells/well in BioCoat poly-D-lysine coated, black wall, clear bottom 384-well plates (BD Biosciences, Franklin lakes, NJ, USA) and allowed to attach overnight in an incubator at 37° C. The cells were then washed twice with HBSS-HEPES buffer (Hanks' balanced salt solution without bicarbonate and phenol red, 20 mM HEPES, pH 7.4) using an ELx405 Select CW Microplate Washer (BioTek, Winooski, Vt., USA). After 60 min of dye-loading in the dark using the Ca2+-sensitive dye Fluo-4AM (Invitrogen, Carlsbad, Calif., USA), at a final concentration of 2×10^−6M, the plates were washed 4 times with HBSS-HEPES buffer to remove excess dye and leaving 50 μl of buffer in each well. The plates were then placed in the FLIPR TETRA instrument and allowed to equilibrate at 37° C. AGN-211377 was added in a 25 μl volume to each well to give final concentrations of 0.1 μM, 0.3 μM, 1 μM, 3 μM, 10 μM, and 30 μM; or 0.067 μM, 0.1 μM, 0.2 μM, 0.3 μM, 0.67 μM, and 1 μM for cells over-expressing TP receptors. After 4.5 minutes, a 7-point serial dilution of the standard agonist for the corresponding receptor, in a 25 μl volume was injected at the final concentrations from 10^−11M to 10^−5M in 10-fold serial dilution increments for cells expressing human recombinant DP1, EP1, EP2, EP3, EP4, FP, and IP receptors. The dose range for the standard agonist for human recombinant TP receptors was from 10^−12M to 10^−6M. HBSS-HEPES buffer was used as the negative control for the standard agonists. Cells were excited with LED (light emitting diode) excitation at 470-495 nm and emission was measured through an emission filter at 515-575 nm. Assay plates were read for 3.5 minutes using the FLIPRTETRA.
ChEMBL 630 13 2 7 5.5 O=C(CCc1ccc(F)cc1CN1CCC[C@H]1c1nc(C(=O)NCCCCC2CCCCC2)co1)NS(=O)(=O)C(F)(F)F nan
CHEMBL3972583 159445 0 None -169 6 Human 5.2 pEC50 = 5.2 Functional
Cell Based Assay: Ca2+ signaling studies were performed using a FLIPR TETRA system (Molecular Devices, Sunnyvale, Calif., USA) in the 384-format. This is a high-throughput instrument for cell-based assays to monitor Ca2+ signaling associated with GPCRs and ion channels. Cells were seeded at a density of 5×104 cells/well in BioCoat poly-D-lysine coated, black wall, clear bottom 384-well plates (BD Biosciences, Franklin lakes, NJ, USA) and allowed to attach overnight in an incubator at 37° C. The cells were then washed twice with HBSS-HEPES buffer (Hanks' balanced salt solution without bicarbonate and phenol red, 20 mM HEPES, pH 7.4) using an ELx405 Select CW Microplate Washer (BioTek, Winooski, Vt., USA). After 60 min of dye-loading in the dark using the Ca2+-sensitive dye Fluo-4AM (Invitrogen, Carlsbad, Calif., USA), at a final concentration of 2×10^−6M, the plates were washed 4 times with HBSS-HEPES buffer to remove excess dye and leaving 50 μl of buffer in each well. The plates were then placed in the FLIPR TETRA instrument and allowed to equilibrate at 37° C. AGN-211377 was added in a 25 μl volume to each well to give final concentrations of 0.1 μM, 0.3 μM, 1 μM, 3 μM, 10 μM, and 30 μM; or 0.067 μM, 0.1 μM, 0.2 μM, 0.3 μM, 0.67 μM, and 1 μM for cells over-expressing TP receptors. After 4.5 minutes, a 7-point serial dilution of the standard agonist for the corresponding receptor, in a 25 μl volume was injected at the final concentrations from 10^−11M to 10^−5M in 10-fold serial dilution increments for cells expressing human recombinant DP1, EP1, EP2, EP3, EP4, FP, and IP receptors. The dose range for the standard agonist for human recombinant TP receptors was from 10^−12M to 10^−6M. HBSS-HEPES buffer was used as the negative control for the standard agonists. Cells were excited with LED (light emitting diode) excitation at 470-495 nm and emission was measured through an emission filter at 515-575 nm. Assay plates were read for 3.5 minutes using the FLIPRTETRA.Cell Based Assay: Ca2+ signaling studies were performed using a FLIPR TETRA system (Molecular Devices, Sunnyvale, Calif., USA) in the 384-format. This is a high-throughput instrument for cell-based assays to monitor Ca2+ signaling associated with GPCRs and ion channels. Cells were seeded at a density of 5×104 cells/well in BioCoat poly-D-lysine coated, black wall, clear bottom 384-well plates (BD Biosciences, Franklin lakes, NJ, USA) and allowed to attach overnight in an incubator at 37° C. The cells were then washed twice with HBSS-HEPES buffer (Hanks' balanced salt solution without bicarbonate and phenol red, 20 mM HEPES, pH 7.4) using an ELx405 Select CW Microplate Washer (BioTek, Winooski, Vt., USA). After 60 min of dye-loading in the dark using the Ca2+-sensitive dye Fluo-4AM (Invitrogen, Carlsbad, Calif., USA), at a final concentration of 2×10^−6M, the plates were washed 4 times with HBSS-HEPES buffer to remove excess dye and leaving 50 μl of buffer in each well. The plates were then placed in the FLIPR TETRA instrument and allowed to equilibrate at 37° C. AGN-211377 was added in a 25 μl volume to each well to give final concentrations of 0.1 μM, 0.3 μM, 1 μM, 3 μM, 10 μM, and 30 μM; or 0.067 μM, 0.1 μM, 0.2 μM, 0.3 μM, 0.67 μM, and 1 μM for cells over-expressing TP receptors. After 4.5 minutes, a 7-point serial dilution of the standard agonist for the corresponding receptor, in a 25 μl volume was injected at the final concentrations from 10^−11M to 10^−5M in 10-fold serial dilution increments for cells expressing human recombinant DP1, EP1, EP2, EP3, EP4, FP, and IP receptors. The dose range for the standard agonist for human recombinant TP receptors was from 10^−12M to 10^−6M. HBSS-HEPES buffer was used as the negative control for the standard agonists. Cells were excited with LED (light emitting diode) excitation at 470-495 nm and emission was measured through an emission filter at 515-575 nm. Assay plates were read for 3.5 minutes using the FLIPRTETRA.
ChEMBL 630 13 2 7 5.5 O=C(CCc1ccc(F)cc1CN1CCC[C@H]1c1nc(C(=O)NCCCCC2CCCCC2)co1)NS(=O)(=O)C(F)(F)F nan
155539238 183260 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 474 9 2 6 4.0 CC(C)(C)C1CCC(CN(Cc2cccc(NCC(=O)O)n2)S(=O)(=O)c2cccnc2)CC1 10.1021/acs.jmedchem.8b00808
CHEMBL4514124 183260 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 474 9 2 6 4.0 CC(C)(C)C1CCC(CN(Cc2cccc(NCC(=O)O)n2)S(=O)(=O)c2cccnc2)CC1 10.1021/acs.jmedchem.8b00808
CHEMBL4596631 183260 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 474 9 2 6 4.0 CC(C)(C)C1CCC(CN(Cc2cccc(NCC(=O)O)n2)S(=O)(=O)c2cccnc2)CC1 10.1021/acs.jmedchem.8b00808
71516449 156215 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 401 7 2 3 5.2 Cc1ccc(-c2cccc(F)c2)cc1CNc1c(F)ccc(OCC(=O)O)c1F nan
CHEMBL3945923 156215 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 401 7 2 3 5.2 Cc1ccc(-c2cccc(F)c2)cc1CNc1c(F)ccc(OCC(=O)O)c1F nan
127050766 146991 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
ChEMBL 393 5 2 6 3.3 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3COc3ccc(F)cc3)O2)n1 10.1021/acsmedchemlett.5b00455
CHEMBL3805075 146991 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
ChEMBL 393 5 2 6 3.3 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3COc3ccc(F)cc3)O2)n1 10.1021/acsmedchemlett.5b00455
89443614 157368 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 393 7 2 3 5.5 Cc1cc(CNc2c(C)ccc(OCC(=O)O)c2C)cc(-c2cccc(F)c2)c1 nan
CHEMBL3955120 157368 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 393 7 2 3 5.5 Cc1cc(CNc2c(C)ccc(OCC(=O)O)c2C)cc(-c2cccc(F)c2)c1 nan
127052613 146984 0 None -10 6 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
ChEMBL 431 7 3 7 3.1 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3/C=C/[C@@H](O)COc3ccccc3)O2)n1 10.1021/acsmedchemlett.5b00455
CHEMBL3804978 146984 0 None -10 6 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
ChEMBL 431 7 3 7 3.1 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3/C=C/[C@@H](O)COc3ccccc3)O2)n1 10.1021/acsmedchemlett.5b00455
11955236 153234 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 396 10 3 3 4.5 CC(C)(CO)c1ccc([C@H]2[C@H](O)C[C@@H](Cl)[C@@H]2CCCCCCC(=O)O)cc1 nan
CHEMBL3922121 153234 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 396 10 3 3 4.5 CC(C)(CO)c1ccc([C@H]2[C@H](O)C[C@@H](Cl)[C@@H]2CCCCCCC(=O)O)cc1 nan
44303711 109129 0 None - 1 Mouse 7.2 pEC50 = 7.2 Functional
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptor
ChEMBL 406 13 3 4 4.4 CCCCC1([C@@H](O)C/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2C/C=C\CCCC(=O)O)CCC1 10.1016/s0960-894x(01)00359-6
CHEMBL303763 109129 0 None - 1 Mouse 7.2 pEC50 = 7.2 Functional
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptor
ChEMBL 406 13 3 4 4.4 CCCCC1([C@@H](O)C/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2C/C=C\CCCC(=O)O)CCC1 10.1016/s0960-894x(01)00359-6
67245477 151661 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 428 13 1 4 7.0 CCCCCC(O)c1ccc([C@H]2CC[C@@H](Cl)[C@@H]2CCCCCCC(=O)OC)s1 nan
CHEMBL3909989 151661 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 428 13 1 4 7.0 CCCCCC(O)c1ccc([C@H]2CC[C@@H](Cl)[C@@H]2CCCCCCC(=O)OC)s1 nan
24760055 150666 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 411 10 2 4 4.6 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COc2ccc(C(=O)O)cc2)cc1 nan
CHEMBL3901873 150666 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 411 10 2 4 4.6 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COc2ccc(C(=O)O)cc2)cc1 nan
24760055 150666 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assayAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assay
ChEMBL 411 10 2 4 4.6 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COc2ccc(C(=O)O)cc2)cc1 nan
CHEMBL3901873 150666 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assayAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assay
ChEMBL 411 10 2 4 4.6 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COc2ccc(C(=O)O)cc2)cc1 nan
89443736 158133 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 421 7 2 3 5.5 O=C(O)COc1ccc(Cl)c(NCc2cc(-c3cccc(F)c3)ccc2F)c1F nan
CHEMBL3961188 158133 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 421 7 2 3 5.5 O=C(O)COc1ccc(Cl)c(NCc2cc(-c3cccc(F)c3)ccc2F)c1F nan
12521 8978 0 None -23988 2 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human EP2 receptor expressed in HEK293T/17 cells assessed as increase in GalphaS-mediated CREB activation measured after 6 to 24 hrs by SEAP reporter gene-based chemiluminescence assayAgonist activity at human EP2 receptor expressed in HEK293T/17 cells assessed as increase in GalphaS-mediated CREB activation measured after 6 to 24 hrs by SEAP reporter gene-based chemiluminescence assay
ChEMBL 399 11 2 3 3.6 FC1(C(N([C@H](C1)/C=C/[C@H]([C@H](CC#CCC)C)O)CCCCCCC(=O)O)=O)F 10.1021/acs.jmedchem.9b00336
72722131 8978 0 None -23988 2 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human EP2 receptor expressed in HEK293T/17 cells assessed as increase in GalphaS-mediated CREB activation measured after 6 to 24 hrs by SEAP reporter gene-based chemiluminescence assayAgonist activity at human EP2 receptor expressed in HEK293T/17 cells assessed as increase in GalphaS-mediated CREB activation measured after 6 to 24 hrs by SEAP reporter gene-based chemiluminescence assay
ChEMBL 399 11 2 3 3.6 FC1(C(N([C@H](C1)/C=C/[C@H]([C@H](CC#CCC)C)O)CCCCCCC(=O)O)=O)F 10.1021/acs.jmedchem.9b00336
CHEMBL3918816 8978 0 None -23988 2 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human EP2 receptor expressed in HEK293T/17 cells assessed as increase in GalphaS-mediated CREB activation measured after 6 to 24 hrs by SEAP reporter gene-based chemiluminescence assayAgonist activity at human EP2 receptor expressed in HEK293T/17 cells assessed as increase in GalphaS-mediated CREB activation measured after 6 to 24 hrs by SEAP reporter gene-based chemiluminescence assay
ChEMBL 399 11 2 3 3.6 FC1(C(N([C@H](C1)/C=C/[C@H]([C@H](CC#CCC)C)O)CCCCCCC(=O)O)=O)F 10.1021/acs.jmedchem.9b00336
11955234 158996 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 394 9 3 3 4.6 O=C(O)CCCCCC[C@@H]1[C@@H](c2ccc(C3(O)CCC3)cc2)[C@H](O)C[C@H]1Cl nan
CHEMBL3968751 158996 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 394 9 3 3 4.6 O=C(O)CCCCCC[C@@H]1[C@@H](c2ccc(C3(O)CCC3)cc2)[C@H](O)C[C@H]1Cl nan
44230431 183432 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 522 10 2 6 4.7 O=C(O)CNc1cccc(CN(Cc2ccc(-c3ccc(Cl)cc3)cc2)S(=O)(=O)c2cccnc2)n1 10.1021/acs.jmedchem.8b00808
CHEMBL4531171 183432 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 522 10 2 6 4.7 O=C(O)CNc1cccc(CN(Cc2ccc(-c3ccc(Cl)cc3)cc2)S(=O)(=O)c2cccnc2)n1 10.1021/acs.jmedchem.8b00808
CHEMBL4598069 183432 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 522 10 2 6 4.7 O=C(O)CNc1cccc(CN(Cc2ccc(-c3ccc(Cl)cc3)cc2)S(=O)(=O)c2cccnc2)n1 10.1021/acs.jmedchem.8b00808
118517483 151049 0 None -22 3 Human 7.1 pEC50 = 7.1 Functional
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
ChEMBL 396 8 2 3 4.2 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2ccccc2F)cc1 nan
CHEMBL3904946 151049 0 None -22 3 Human 7.1 pEC50 = 7.1 Functional
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
ChEMBL 396 8 2 3 4.2 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2ccccc2F)cc1 nan
11855590 151152 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 387 8 2 5 3.4 CC(C)C(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)o2)cc1 nan
CHEMBL3905811 151152 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 387 8 2 5 3.4 CC(C)C(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)o2)cc1 nan
11855590 151152 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assayAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assay
ChEMBL 387 8 2 5 3.4 CC(C)C(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)o2)cc1 nan
CHEMBL3905811 151152 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assayAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assay
ChEMBL 387 8 2 5 3.4 CC(C)C(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)o2)cc1 nan
134147021 156803 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 414 13 2 3 6.9 CCCCCC(O)c1ccc([C@H]2CC[C@@H](Cl)[C@@H]2CCCCCCC(=O)O)s1 nan
CHEMBL3950412 156803 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 414 13 2 3 6.9 CCCCCC(O)c1ccc([C@H]2CC[C@@H](Cl)[C@@H]2CCCCCCC(=O)O)s1 nan
11955255 153035 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 408 8 3 3 5.0 CC(C)(C)C(O)c1ccc([C@H]2[C@H](O)C[C@@H](Cl)[C@@H]2C/C=C\CCCC(=O)O)cc1 nan
CHEMBL3920560 153035 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 408 8 3 3 5.0 CC(C)(C)C(O)c1ccc([C@H]2[C@H](O)C[C@@H](Cl)[C@@H]2C/C=C\CCCC(=O)O)cc1 nan
92135977 159675 0 None -141 4 Human 7.1 pEC50 = 7.1 Functional
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
ChEMBL 396 8 2 3 4.2 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2cccc(F)c2)cc1 nan
CHEMBL3974652 159675 0 None -141 4 Human 7.1 pEC50 = 7.1 Functional
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
ChEMBL 396 8 2 3 4.2 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2cccc(F)c2)cc1 nan
5819 7799 29 None 1 2 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at EP2 receptor (unknown origin) by cAMP assayAgonist activity at EP2 receptor (unknown origin) by cAMP assay
ChEMBL 333 4 1 5 4.0 CCOC(=O)c1c(sc2c1CCCCC2)NC(=O)c1ccco1 10.1021/jm401431x
673766 7799 29 None 1 2 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at EP2 receptor (unknown origin) by cAMP assayAgonist activity at EP2 receptor (unknown origin) by cAMP assay
ChEMBL 333 4 1 5 4.0 CCOC(=O)c1c(sc2c1CCCCC2)NC(=O)c1ccco1 10.1021/jm401431x
CHEMBL1578948 7799 29 None 1 2 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at EP2 receptor (unknown origin) by cAMP assayAgonist activity at EP2 receptor (unknown origin) by cAMP assay
ChEMBL 333 4 1 5 4.0 CCOC(=O)c1c(sc2c1CCCCC2)NC(=O)c1ccco1 10.1021/jm401431x
11855871 153186 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assayAgonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assay
ChEMBL 429 11 1 5 4.9 CCCCCC(=O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3921784 153186 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assayAgonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assay
ChEMBL 429 11 1 5 4.9 CCCCCC(=O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
11855594 159759 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assayAgonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assay
ChEMBL 417 10 2 5 4.4 CCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3975238 159759 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assayAgonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assay
ChEMBL 417 10 2 5 4.4 CCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
11502897 149571 0 None 43 3 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 431 11 2 5 4.8 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3892847 149571 0 None 43 3 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 431 11 2 5 4.8 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
11502897 149571 0 None 43 3 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assayAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assay
ChEMBL 431 11 2 5 4.8 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3892847 149571 0 None 43 3 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assayAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assay
ChEMBL 431 11 2 5 4.8 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
89443779 155518 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 399 7 3 4 4.7 Cc1c(OCC(=O)O)ccc(F)c1NCc1cc(O)cc(-c2cccc(F)c2)c1 nan
CHEMBL3940318 155518 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 399 7 3 4 4.7 Cc1c(OCC(=O)O)ccc(F)c1NCc1cc(O)cc(-c2cccc(F)c2)c1 nan
89443711 157758 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 433 7 2 3 5.6 Cc1cc(-c2cc(F)cc(F)c2)cc(CNc2c(F)ccc(OCC(=O)O)c2F)c1C nan
CHEMBL3958279 157758 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 433 7 2 3 5.6 Cc1cc(-c2cc(F)cc(F)c2)cc(CNc2c(F)ccc(OCC(=O)O)c2F)c1C nan
118517483 151049 0 None -22 3 Human 8.1 pEC50 = 8.1 Functional
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
ChEMBL 396 8 2 3 4.2 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2ccccc2F)cc1 nan
CHEMBL3904946 151049 0 None -22 3 Human 8.1 pEC50 = 8.1 Functional
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
ChEMBL 396 8 2 3 4.2 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2ccccc2F)cc1 nan
118517359 151174 0 None -79 4 Human 8.1 pEC50 = 8.1 Functional
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
ChEMBL 456 8 2 3 4.8 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2cccc(Br)c2)cc1 nan
CHEMBL3906016 151174 0 None -79 4 Human 8.1 pEC50 = 8.1 Functional
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
ChEMBL 456 8 2 3 4.8 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2cccc(Br)c2)cc1 nan
118517488 160490 0 None -14 3 Human 8.1 pEC50 = 8.1 Functional
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
ChEMBL 414 8 2 3 4.4 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2cccc(F)c2F)cc1 nan
CHEMBL3981554 160490 0 None -14 3 Human 8.1 pEC50 = 8.1 Functional
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
ChEMBL 414 8 2 3 4.4 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2cccc(F)c2F)cc1 nan
44442327 101234 0 None -891 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human EP2 receptor by cAMP assayAgonist activity at human EP2 receptor by cAMP assay
ChEMBL 345 9 2 3 3.0 CCCC[C@H](O)/C=C/[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.11.020
CHEMBL251294 101234 0 None -891 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human EP2 receptor by cAMP assayAgonist activity at human EP2 receptor by cAMP assay
ChEMBL 345 9 2 3 3.0 CCCC[C@H](O)/C=C/[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.11.020
11955358 159861 0 None -11 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 364 8 2 2 4.7 O=C(O)CCCCCC[C@@H]1[C@@H](c2ccc3c(c2)CCC3)[C@H](O)C[C@H]1Cl nan
CHEMBL3976116 159861 0 None -11 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 364 8 2 2 4.7 O=C(O)CCCCCC[C@@H]1[C@@H](c2ccc3c(c2)CCC3)[C@H](O)C[C@H]1Cl nan
155521507 183228 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 482 10 2 6 4.1 CC(C)(C)c1ccc(CN(Cc2cccc(NCCC(=O)O)n2)S(=O)(=O)c2cccnc2)cc1 10.1021/acs.jmedchem.8b00808
CHEMBL4451941 183228 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 482 10 2 6 4.1 CC(C)(C)c1ccc(CN(Cc2cccc(NCCC(=O)O)n2)S(=O)(=O)c2cccnc2)cc1 10.1021/acs.jmedchem.8b00808
CHEMBL4596396 183228 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 482 10 2 6 4.1 CC(C)(C)c1ccc(CN(Cc2cccc(NCCC(=O)O)n2)S(=O)(=O)c2cccnc2)cc1 10.1021/acs.jmedchem.8b00808
56839342 155786 0 None -83 7 Human 6.1 pEC50 = 6.1 Functional
Cell Based Assay: Ca2+ signaling studies were performed using a FLIPR TETRA system (Molecular Devices, Sunnyvale, Calif., USA) in the 384-format. This is a high-throughput instrument for cell-based assays to monitor Ca2+ signaling associated with GPCRs and ion channels. Cells were seeded at a density of 5×104 cells/well in BioCoat poly-D-lysine coated, black wall, clear bottom 384-well plates (BD Biosciences, Franklin lakes, NJ, USA) and allowed to attach overnight in an incubator at 37° C. The cells were then washed twice with HBSS-HEPES buffer (Hanks' balanced salt solution without bicarbonate and phenol red, 20 mM HEPES, pH 7.4) using an ELx405 Select CW Microplate Washer (BioTek, Winooski, Vt., USA). After 60 min of dye-loading in the dark using the Ca2+-sensitive dye Fluo-4AM (Invitrogen, Carlsbad, Calif., USA), at a final concentration of 2×10^−6M, the plates were washed 4 times with HBSS-HEPES buffer to remove excess dye and leaving 50 μl of buffer in each well. The plates were then placed in the FLIPR TETRA instrument and allowed to equilibrate at 37° C. AGN-211377 was added in a 25 μl volume to each well to give final concentrations of 0.1 μM, 0.3 μM, 1 μM, 3 μM, 10 μM, and 30 μM; or 0.067 μM, 0.1 μM, 0.2 μM, 0.3 μM, 0.67 μM, and 1 μM for cells over-expressing TP receptors. After 4.5 minutes, a 7-point serial dilution of the standard agonist for the corresponding receptor, in a 25 μl volume was injected at the final concentrations from 10^−11M to 10^−5M in 10-fold serial dilution increments for cells expressing human recombinant DP1, EP1, EP2, EP3, EP4, FP, and IP receptors. The dose range for the standard agonist for human recombinant TP receptors was from 10^−12M to 10^−6M. HBSS-HEPES buffer was used as the negative control for the standard agonists. Cells were excited with LED (light emitting diode) excitation at 470-495 nm and emission was measured through an emission filter at 515-575 nm. Assay plates were read for 3.5 minutes using the FLIPRTETRA.Cell Based Assay: Ca2+ signaling studies were performed using a FLIPR TETRA system (Molecular Devices, Sunnyvale, Calif., USA) in the 384-format. This is a high-throughput instrument for cell-based assays to monitor Ca2+ signaling associated with GPCRs and ion channels. Cells were seeded at a density of 5×104 cells/well in BioCoat poly-D-lysine coated, black wall, clear bottom 384-well plates (BD Biosciences, Franklin lakes, NJ, USA) and allowed to attach overnight in an incubator at 37° C. The cells were then washed twice with HBSS-HEPES buffer (Hanks' balanced salt solution without bicarbonate and phenol red, 20 mM HEPES, pH 7.4) using an ELx405 Select CW Microplate Washer (BioTek, Winooski, Vt., USA). After 60 min of dye-loading in the dark using the Ca2+-sensitive dye Fluo-4AM (Invitrogen, Carlsbad, Calif., USA), at a final concentration of 2×10^−6M, the plates were washed 4 times with HBSS-HEPES buffer to remove excess dye and leaving 50 μl of buffer in each well. The plates were then placed in the FLIPR TETRA instrument and allowed to equilibrate at 37° C. AGN-211377 was added in a 25 μl volume to each well to give final concentrations of 0.1 μM, 0.3 μM, 1 μM, 3 μM, 10 μM, and 30 μM; or 0.067 μM, 0.1 μM, 0.2 μM, 0.3 μM, 0.67 μM, and 1 μM for cells over-expressing TP receptors. After 4.5 minutes, a 7-point serial dilution of the standard agonist for the corresponding receptor, in a 25 μl volume was injected at the final concentrations from 10^−11M to 10^−5M in 10-fold serial dilution increments for cells expressing human recombinant DP1, EP1, EP2, EP3, EP4, FP, and IP receptors. The dose range for the standard agonist for human recombinant TP receptors was from 10^−12M to 10^−6M. HBSS-HEPES buffer was used as the negative control for the standard agonists. Cells were excited with LED (light emitting diode) excitation at 470-495 nm and emission was measured through an emission filter at 515-575 nm. Assay plates were read for 3.5 minutes using the FLIPRTETRA.
ChEMBL 646 13 2 7 6.0 O=C(CCc1ccc(Cl)cc1CN1CCC[C@H]1c1nc(C(=O)NCCCCC2CCCCC2)co1)NS(=O)(=O)C(F)(F)F nan
CHEMBL3942394 155786 0 None -83 7 Human 6.1 pEC50 = 6.1 Functional
Cell Based Assay: Ca2+ signaling studies were performed using a FLIPR TETRA system (Molecular Devices, Sunnyvale, Calif., USA) in the 384-format. This is a high-throughput instrument for cell-based assays to monitor Ca2+ signaling associated with GPCRs and ion channels. Cells were seeded at a density of 5×104 cells/well in BioCoat poly-D-lysine coated, black wall, clear bottom 384-well plates (BD Biosciences, Franklin lakes, NJ, USA) and allowed to attach overnight in an incubator at 37° C. The cells were then washed twice with HBSS-HEPES buffer (Hanks' balanced salt solution without bicarbonate and phenol red, 20 mM HEPES, pH 7.4) using an ELx405 Select CW Microplate Washer (BioTek, Winooski, Vt., USA). After 60 min of dye-loading in the dark using the Ca2+-sensitive dye Fluo-4AM (Invitrogen, Carlsbad, Calif., USA), at a final concentration of 2×10^−6M, the plates were washed 4 times with HBSS-HEPES buffer to remove excess dye and leaving 50 μl of buffer in each well. The plates were then placed in the FLIPR TETRA instrument and allowed to equilibrate at 37° C. AGN-211377 was added in a 25 μl volume to each well to give final concentrations of 0.1 μM, 0.3 μM, 1 μM, 3 μM, 10 μM, and 30 μM; or 0.067 μM, 0.1 μM, 0.2 μM, 0.3 μM, 0.67 μM, and 1 μM for cells over-expressing TP receptors. After 4.5 minutes, a 7-point serial dilution of the standard agonist for the corresponding receptor, in a 25 μl volume was injected at the final concentrations from 10^−11M to 10^−5M in 10-fold serial dilution increments for cells expressing human recombinant DP1, EP1, EP2, EP3, EP4, FP, and IP receptors. The dose range for the standard agonist for human recombinant TP receptors was from 10^−12M to 10^−6M. HBSS-HEPES buffer was used as the negative control for the standard agonists. Cells were excited with LED (light emitting diode) excitation at 470-495 nm and emission was measured through an emission filter at 515-575 nm. Assay plates were read for 3.5 minutes using the FLIPRTETRA.Cell Based Assay: Ca2+ signaling studies were performed using a FLIPR TETRA system (Molecular Devices, Sunnyvale, Calif., USA) in the 384-format. This is a high-throughput instrument for cell-based assays to monitor Ca2+ signaling associated with GPCRs and ion channels. Cells were seeded at a density of 5×104 cells/well in BioCoat poly-D-lysine coated, black wall, clear bottom 384-well plates (BD Biosciences, Franklin lakes, NJ, USA) and allowed to attach overnight in an incubator at 37° C. The cells were then washed twice with HBSS-HEPES buffer (Hanks' balanced salt solution without bicarbonate and phenol red, 20 mM HEPES, pH 7.4) using an ELx405 Select CW Microplate Washer (BioTek, Winooski, Vt., USA). After 60 min of dye-loading in the dark using the Ca2+-sensitive dye Fluo-4AM (Invitrogen, Carlsbad, Calif., USA), at a final concentration of 2×10^−6M, the plates were washed 4 times with HBSS-HEPES buffer to remove excess dye and leaving 50 μl of buffer in each well. The plates were then placed in the FLIPR TETRA instrument and allowed to equilibrate at 37° C. AGN-211377 was added in a 25 μl volume to each well to give final concentrations of 0.1 μM, 0.3 μM, 1 μM, 3 μM, 10 μM, and 30 μM; or 0.067 μM, 0.1 μM, 0.2 μM, 0.3 μM, 0.67 μM, and 1 μM for cells over-expressing TP receptors. After 4.5 minutes, a 7-point serial dilution of the standard agonist for the corresponding receptor, in a 25 μl volume was injected at the final concentrations from 10^−11M to 10^−5M in 10-fold serial dilution increments for cells expressing human recombinant DP1, EP1, EP2, EP3, EP4, FP, and IP receptors. The dose range for the standard agonist for human recombinant TP receptors was from 10^−12M to 10^−6M. HBSS-HEPES buffer was used as the negative control for the standard agonists. Cells were excited with LED (light emitting diode) excitation at 470-495 nm and emission was measured through an emission filter at 515-575 nm. Assay plates were read for 3.5 minutes using the FLIPRTETRA.
ChEMBL 646 13 2 7 6.0 O=C(CCc1ccc(Cl)cc1CN1CCC[C@H]1c1nc(C(=O)NCCCCC2CCCCC2)co1)NS(=O)(=O)C(F)(F)F nan
58932678 82063 0 None -301 2 Rat 5.1 pEC50 = 5.1 Functional
Agonist activity at rat EP2 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP2 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
ChEMBL 549 10 2 8 5.2 Cc1cccc2oc(-c3cccc(C[C@H](O)/C=C/[C@H]4CCC(=O)N4CCSc4nc(C(=O)O)cs4)c3)nc12 10.1016/j.bmc.2012.04.008
CHEMBL2037290 82063 0 None -301 2 Rat 5.1 pEC50 = 5.1 Functional
Agonist activity at rat EP2 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP2 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
ChEMBL 549 10 2 8 5.2 Cc1cccc2oc(-c3cccc(C[C@H](O)/C=C/[C@H]4CCC(=O)N4CCSc4nc(C(=O)O)cs4)c3)nc12 10.1016/j.bmc.2012.04.008
22246956 203098 0 None - 1 Rat 6.1 pEC50 = 6.1 Functional
Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP releaseAgonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release
ChEMBL 411 15 1 4 4.2 CCCCCC(=O)c1ccc(CN(CCCCCCC(=O)O)S(C)(=O)=O)cc1 10.1016/j.bmcl.2009.01.059
CHEMBL562291 203098 0 None - 1 Rat 6.1 pEC50 = 6.1 Functional
Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP releaseAgonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release
ChEMBL 411 15 1 4 4.2 CCCCCC(=O)c1ccc(CN(CCCCCCC(=O)O)S(C)(=O)=O)cc1 10.1016/j.bmcl.2009.01.059
69753740 147000 0 None -2454 5 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
ChEMBL 390 9 3 5 2.8 O=C(O)CCC[C@H]1CC[C@H]2[C@H](C[C@@H](O)[C@@H]2/C=C/[C@@H](O)COc2ccccc2)O1 10.1021/acsmedchemlett.5b00455
CHEMBL3805134 147000 0 None -2454 5 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
ChEMBL 390 9 3 5 2.8 O=C(O)CCC[C@H]1CC[C@H]2[C@H](C[C@@H](O)[C@@H]2/C=C/[C@@H](O)COc2ccccc2)O1 10.1021/acsmedchemlett.5b00455
134155748 157948 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assayAgonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assay
ChEMBL 400 12 2 4 4.7 CCCCCC(=O)c1ccc([C@H]2[C@H](O)CC(=O)[C@@H]2C/C=C\CCCC(=O)O)cc1 nan
CHEMBL3959653 157948 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assayAgonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assay
ChEMBL 400 12 2 4 4.7 CCCCCC(=O)c1ccc([C@H]2[C@H](O)CC(=O)[C@@H]2C/C=C\CCCC(=O)O)cc1 nan
89443669 153990 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 417 7 3 4 4.9 Cc1cc(-c2cccc(F)c2)cc(CNc2c(F)ccc(OCC(=O)O)c2F)c1O nan
CHEMBL3928263 153990 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 417 7 3 4 4.9 Cc1cc(-c2cccc(F)c2)cc(CNc2c(F)ccc(OCC(=O)O)c2F)c1O nan
89443662 159667 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 412 7 2 4 4.7 N#Cc1c(OCC(=O)O)ccc(F)c1NCc1cc(-c2cccc(F)c2)ccc1F nan
CHEMBL3974557 159667 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 412 7 2 4 4.7 N#Cc1c(OCC(=O)O)ccc(F)c1NCc1cc(-c2cccc(F)c2)ccc1F nan
1883 9856 75 None -6 12 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human EP2 receptor expressed in HEK293T/17 cells assessed as increase in GalphaS-mediated CREB activation measured after 6 to 24 hrs by SEAP reporter gene-based chemiluminescence assayAgonist activity at human EP2 receptor expressed in HEK293T/17 cells assessed as increase in GalphaS-mediated CREB activation measured after 6 to 24 hrs by SEAP reporter gene-based chemiluminescence assay
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/acs.jmedchem.9b00336
1916 9856 75 None -6 12 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human EP2 receptor expressed in HEK293T/17 cells assessed as increase in GalphaS-mediated CREB activation measured after 6 to 24 hrs by SEAP reporter gene-based chemiluminescence assayAgonist activity at human EP2 receptor expressed in HEK293T/17 cells assessed as increase in GalphaS-mediated CREB activation measured after 6 to 24 hrs by SEAP reporter gene-based chemiluminescence assay
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/acs.jmedchem.9b00336
5280360 9856 75 None -6 12 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human EP2 receptor expressed in HEK293T/17 cells assessed as increase in GalphaS-mediated CREB activation measured after 6 to 24 hrs by SEAP reporter gene-based chemiluminescence assayAgonist activity at human EP2 receptor expressed in HEK293T/17 cells assessed as increase in GalphaS-mediated CREB activation measured after 6 to 24 hrs by SEAP reporter gene-based chemiluminescence assay
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/acs.jmedchem.9b00336
913 9856 75 None -6 12 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human EP2 receptor expressed in HEK293T/17 cells assessed as increase in GalphaS-mediated CREB activation measured after 6 to 24 hrs by SEAP reporter gene-based chemiluminescence assayAgonist activity at human EP2 receptor expressed in HEK293T/17 cells assessed as increase in GalphaS-mediated CREB activation measured after 6 to 24 hrs by SEAP reporter gene-based chemiluminescence assay
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/acs.jmedchem.9b00336
CHEMBL548 9856 75 None -6 12 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human EP2 receptor expressed in HEK293T/17 cells assessed as increase in GalphaS-mediated CREB activation measured after 6 to 24 hrs by SEAP reporter gene-based chemiluminescence assayAgonist activity at human EP2 receptor expressed in HEK293T/17 cells assessed as increase in GalphaS-mediated CREB activation measured after 6 to 24 hrs by SEAP reporter gene-based chemiluminescence assay
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/acs.jmedchem.9b00336
DB00917 9856 75 None -6 12 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human EP2 receptor expressed in HEK293T/17 cells assessed as increase in GalphaS-mediated CREB activation measured after 6 to 24 hrs by SEAP reporter gene-based chemiluminescence assayAgonist activity at human EP2 receptor expressed in HEK293T/17 cells assessed as increase in GalphaS-mediated CREB activation measured after 6 to 24 hrs by SEAP reporter gene-based chemiluminescence assay
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/acs.jmedchem.9b00336
56835070 76246 0 None -112 2 Rat 7.1 pEC50 = 7.1 Functional
Agonist activity at rat EP2 receptorAgonist activity at rat EP2 receptor
ChEMBL 432 9 2 6 3.4 Cc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=O)N2CCSc2nc(C(=O)O)cs2)c1 10.1016/j.bmc.2012.02.018
CHEMBL1933722 76246 0 None -112 2 Rat 7.1 pEC50 = 7.1 Functional
Agonist activity at rat EP2 receptorAgonist activity at rat EP2 receptor
ChEMBL 432 9 2 6 3.4 Cc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=O)N2CCSc2nc(C(=O)O)cs2)c1 10.1016/j.bmc.2012.02.018
56835070 76246 0 None -112 2 Rat 7.1 pEC50 = 7.1 Functional
Agonist activity at rat EP2 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP2 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
ChEMBL 432 9 2 6 3.4 Cc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=O)N2CCSc2nc(C(=O)O)cs2)c1 10.1016/j.bmc.2012.04.008
CHEMBL1933722 76246 0 None -112 2 Rat 7.1 pEC50 = 7.1 Functional
Agonist activity at rat EP2 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP2 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
ChEMBL 432 9 2 6 3.4 Cc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=O)N2CCSc2nc(C(=O)O)cs2)c1 10.1016/j.bmc.2012.04.008
51036042 183120 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 405 8 2 5 2.8 CC(C)(C)c1ccc(CN(Cc2cccc(NCC(=O)O)n2)S(C)(=O)=O)cc1 10.1021/acs.jmedchem.8b00808
CHEMBL4554216 183120 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 405 8 2 5 2.8 CC(C)(C)c1ccc(CN(Cc2cccc(NCC(=O)O)n2)S(C)(=O)=O)cc1 10.1021/acs.jmedchem.8b00808
CHEMBL4595541 183120 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 405 8 2 5 2.8 CC(C)(C)c1ccc(CN(Cc2cccc(NCC(=O)O)n2)S(C)(=O)=O)cc1 10.1021/acs.jmedchem.8b00808
66857975 171267 0 None -10 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at recombinant human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIAAgonist activity at recombinant human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIA
ChEMBL 454 10 2 7 4.4 CC(O)(C/C=C/[C@H]1COC(=O)N1CCSc1nc(C(=O)O)cs1)CC1CCCCC1 10.1016/j.bmc.2017.11.035
CHEMBL4214346 171267 0 None -10 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at recombinant human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIAAgonist activity at recombinant human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIA
ChEMBL 454 10 2 7 4.4 CC(O)(C/C=C/[C@H]1COC(=O)N1CCSc1nc(C(=O)O)cs1)CC1CCCCC1 10.1016/j.bmc.2017.11.035
11955133 152427 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 374 8 1 4 4.5 COC(=O)CCCCCC[C@H]1C(=O)C[C@@H](O)[C@@H]1c1ccc(C(C)(C)C)cc1 nan
CHEMBL3915820 152427 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 374 8 1 4 4.5 COC(=O)CCCCCC[C@H]1C(=O)C[C@@H](O)[C@@H]1c1ccc(C(C)(C)C)cc1 nan
9820676 201824 0 None - 1 Rat 7.0 pEC50 = 7.0 Functional
Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP releaseAgonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release
ChEMBL 369 13 1 3 3.8 CCCCc1ccc(CN(CCCCCCC(=O)O)S(C)(=O)=O)cc1 10.1016/j.bmcl.2009.01.059
CHEMBL549461 201824 0 None - 1 Rat 7.0 pEC50 = 7.0 Functional
Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP releaseAgonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release
ChEMBL 369 13 1 3 3.8 CCCCc1ccc(CN(CCCCCCC(=O)O)S(C)(=O)=O)cc1 10.1016/j.bmcl.2009.01.059
89444029 155873 0 None - 1 Human 7.0 pEC50 = 7 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 401 7 2 3 5.2 Cc1ccc(OCC(=O)O)c(F)c1NCc1cc(-c2cccc(F)c2)ccc1F nan
CHEMBL3943109 155873 0 None - 1 Human 7.0 pEC50 = 7 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 401 7 2 3 5.2 Cc1ccc(OCC(=O)O)c(F)c1NCc1cc(-c2cccc(F)c2)ccc1F nan
122180297 128425 0 None 4466 2 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 437 3 1 4 4.9 C[C@@H]1COc2c(Cl)cc(-n3ccc4cc(F)ccc43)cc2CN1Cc1cc[nH]c(=O)c1 10.1021/acs.jmedchem.5b00567
CHEMBL3586362 128425 0 None 4466 2 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 437 3 1 4 4.9 C[C@@H]1COc2c(Cl)cc(-n3ccc4cc(F)ccc43)cc2CN1Cc1cc[nH]c(=O)c1 10.1021/acs.jmedchem.5b00567
122180261 128391 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 426 4 0 5 5.8 COc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1cccc(C#N)c1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586324 128391 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 426 4 0 5 5.8 COc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1cccc(C#N)c1)C2 10.1021/acs.jmedchem.5b00567
122180274 128401 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 385 4 0 5 4.4 COc1cc(-n2ccc3ccccc32)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586337 128401 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 385 4 0 5 4.4 COc1cc(-n2ccc3ccccc32)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
122180288 128416 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 386 3 0 4 5.7 Cc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586352 128416 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 386 3 0 4 5.7 Cc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
122180250 128380 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 432 5 0 6 5.4 COc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1cccnc1OC)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586313 128380 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 432 5 0 6 5.4 COc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1cccnc1OC)C2 10.1021/acs.jmedchem.5b00567
122180267 128395 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 360 4 0 4 4.5 COc1cc(-c2cccc(C)c2)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586330 128395 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 360 4 0 4 4.5 COc1cc(-c2cccc(C)c2)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
122180251 128381 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 432 5 0 6 5.4 COc1ccc(CN2CCOc3c(cc(-c4csc5ccccc45)cc3OC)C2)cn1 10.1021/acs.jmedchem.5b00567
CHEMBL3586314 128381 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 432 5 0 6 5.4 COc1ccc(CN2CCOc3c(cc(-c4csc5ccccc45)cc3OC)C2)cn1 10.1021/acs.jmedchem.5b00567
122180273 128400 0 None - 1 Human 4.8 pIC50 = 4.8 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 386 4 0 6 3.8 COc1cc(-n2cnc3ccccc32)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586336 128400 0 None - 1 Human 4.8 pIC50 = 4.8 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 386 4 0 6 3.8 COc1cc(-n2cnc3ccccc32)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
1987175 10566 31 None 1 5 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human EP2 receptor overexpressed in rat C6 cells assessed as inhibition of PGE2-induced cAMP accumulation incubated for 10 mins prior to PGE2 addition measured after 40 mins by TR-FRET assayAntagonist activity at human EP2 receptor overexpressed in rat C6 cells assessed as inhibition of PGE2-induced cAMP accumulation incubated for 10 mins prior to PGE2 addition measured after 40 mins by TR-FRET assay
ChEMBL 491 7 3 7 3.6 CCc1nnc(s1)NS(=O)(=O)c1ccc(cc1)NC(=S)NC(=O)/C=C/c1ccc(cc1)F 10.1021/ml400112h
9283 10566 31 None 1 5 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human EP2 receptor overexpressed in rat C6 cells assessed as inhibition of PGE2-induced cAMP accumulation incubated for 10 mins prior to PGE2 addition measured after 40 mins by TR-FRET assayAntagonist activity at human EP2 receptor overexpressed in rat C6 cells assessed as inhibition of PGE2-induced cAMP accumulation incubated for 10 mins prior to PGE2 addition measured after 40 mins by TR-FRET assay
ChEMBL 491 7 3 7 3.6 CCc1nnc(s1)NS(=O)(=O)c1ccc(cc1)NC(=S)NC(=O)/C=C/c1ccc(cc1)F 10.1021/ml400112h
CHEMBL1372836 10566 31 None 1 5 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human EP2 receptor overexpressed in rat C6 cells assessed as inhibition of PGE2-induced cAMP accumulation incubated for 10 mins prior to PGE2 addition measured after 40 mins by TR-FRET assayAntagonist activity at human EP2 receptor overexpressed in rat C6 cells assessed as inhibition of PGE2-induced cAMP accumulation incubated for 10 mins prior to PGE2 addition measured after 40 mins by TR-FRET assay
ChEMBL 491 7 3 7 3.6 CCc1nnc(s1)NS(=O)(=O)c1ccc(cc1)NC(=S)NC(=O)/C=C/c1ccc(cc1)F 10.1021/ml400112h
122180270 128397 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 380 4 0 4 4.8 COc1cc(-c2cccc(Cl)c2)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586333 128397 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 380 4 0 4 4.8 COc1cc(-c2cccc(Cl)c2)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
122180282 128409 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 410 4 0 6 4.3 COc1cc(-n2ccc3cc(C#N)ccc32)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586345 128409 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 410 4 0 6 4.3 COc1cc(-n2ccc3cc(C#N)ccc32)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
122180295 128422 0 None 281 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 422 3 1 4 5.3 O=c1cc(CN2CCOc3c(Cl)cc(-c4csc5ccccc45)cc3C2)cc[nH]1 10.1021/acs.jmedchem.5b00567
CHEMBL3586359 128422 0 None 281 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 422 3 1 4 5.3 O=c1cc(CN2CCOc3c(Cl)cc(-c4csc5ccccc45)cc3C2)cc[nH]1 10.1021/acs.jmedchem.5b00567
122180296 128424 0 None 758 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 436 3 1 4 5.7 C[C@@H]1COc2c(Cl)cc(-c3csc4ccccc34)cc2CN1Cc1cc[nH]c(=O)c1 10.1021/acs.jmedchem.5b00567
CHEMBL3586361 128424 0 None 758 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 436 3 1 4 5.7 C[C@@H]1COc2c(Cl)cc(-c3csc4ccccc34)cc2CN1Cc1cc[nH]c(=O)c1 10.1021/acs.jmedchem.5b00567
122180265 128394 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 396 4 0 4 5.3 COc1cc(-c2cccc3ccccc23)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586328 128394 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 396 4 0 4 5.3 COc1cc(-c2cccc3ccccc23)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
122180276 128403 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 399 4 0 5 4.6 COc1cc(-c2cn(C)c3ccccc23)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586339 128403 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 399 4 0 5 4.6 COc1cc(-c2cn(C)c3ccccc23)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
122180289 128417 0 None 7 2 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 406 3 0 4 6.0 Clc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586353 128417 0 None 7 2 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 406 3 0 4 6.0 Clc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
56927669 128423 0 None -2 4 Rat 7.5 pIC50 = 7.5 Functional
Antagonist activity at rat EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at rat EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 423 3 1 4 4.5 O=c1cc(CN2CCOc3c(Cl)cc(-n4ccc5cc(F)ccc54)cc3C2)cc[nH]1 10.1021/acs.jmedchem.5b00567
CHEMBL3586360 128423 0 None -2 4 Rat 7.5 pIC50 = 7.5 Functional
Antagonist activity at rat EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at rat EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 423 3 1 4 4.5 O=c1cc(CN2CCOc3c(Cl)cc(-n4ccc5cc(F)ccc54)cc3C2)cc[nH]1 10.1021/acs.jmedchem.5b00567
30897313 128376 0 None -2 5 Rat 6.5 pIC50 = 6.5 Functional
Antagonist activity at rat EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at rat EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 402 4 0 5 5.4 COc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586309 128376 0 None -2 5 Rat 6.5 pIC50 = 6.5 Functional
Antagonist activity at rat EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at rat EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 402 4 0 5 5.4 COc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
42484632 128377 5 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 402 4 0 5 5.4 COc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1ccccn1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586310 128377 5 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 402 4 0 5 5.4 COc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1ccccn1)C2 10.1021/acs.jmedchem.5b00567
122180275 128402 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 385 4 1 4 4.6 COc1cc(-c2c[nH]c3ccccc23)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586338 128402 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 385 4 1 4 4.6 COc1cc(-c2c[nH]c3ccccc23)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
122180278 128405 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 419 4 0 5 5.1 COc1cc(-n2ccc3c(Cl)cccc32)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586341 128405 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 419 4 0 5 5.1 COc1cc(-n2ccc3c(Cl)cccc32)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
122180286 128413 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 388 3 1 5 5.1 Oc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586349 128413 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 388 3 1 5 5.1 Oc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
56927669 128423 0 None 2 4 Mouse 8.4 pIC50 = 8.4 Functional
Antagonist activity at mouse EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at mouse EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 423 3 1 4 4.5 O=c1cc(CN2CCOc3c(Cl)cc(-n4ccc5cc(F)ccc54)cc3C2)cc[nH]1 10.1021/acs.jmedchem.5b00567
CHEMBL3586360 128423 0 None 2 4 Mouse 8.4 pIC50 = 8.4 Functional
Antagonist activity at mouse EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at mouse EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 423 3 1 4 4.5 O=c1cc(CN2CCOc3c(Cl)cc(-n4ccc5cc(F)ccc54)cc3C2)cc[nH]1 10.1021/acs.jmedchem.5b00567
122180283 128410 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 403 4 0 5 4.6 COc1cc(-n2ccc3cc(F)ccc32)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586346 128410 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 403 4 0 5 4.6 COc1cc(-n2ccc3cc(F)ccc32)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
122180280 128407 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 419 4 0 5 5.1 COc1cc(-n2ccc3ccc(Cl)cc32)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586343 128407 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 419 4 0 5 5.1 COc1cc(-n2ccc3ccc(Cl)cc32)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
122180263 128392 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 402 4 0 5 5.4 COc1cc(-c2cc3ccccc3s2)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586326 128392 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 402 4 0 5 5.4 COc1cc(-c2cc3ccccc3s2)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
56927669 128423 0 None -3 4 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 423 3 1 4 4.5 O=c1cc(CN2CCOc3c(Cl)cc(-n4ccc5cc(F)ccc54)cc3C2)cc[nH]1 10.1021/acs.jmedchem.5b00567
CHEMBL3586360 128423 0 None -3 4 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 423 3 1 4 4.5 O=c1cc(CN2CCOc3c(Cl)cc(-n4ccc5cc(F)ccc54)cc3C2)cc[nH]1 10.1021/acs.jmedchem.5b00567
122180252 128382 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 418 4 1 5 4.7 COc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1ccc(=O)[nH]c1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586315 128382 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 418 4 1 5 4.7 COc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1ccc(=O)[nH]c1)C2 10.1021/acs.jmedchem.5b00567
122180284 128411 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 421 4 0 5 4.8 COc1cc(N2CCc3cc(Cl)ccc32)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586347 128411 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 421 4 0 5 4.8 COc1cc(N2CCc3cc(Cl)ccc32)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
30897313 128376 0 None 2 5 Mouse 7.2 pIC50 = 7.2 Functional
Antagonist activity at mouse EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at mouse EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 402 4 0 5 5.4 COc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586309 128376 0 None 2 5 Mouse 7.2 pIC50 = 7.2 Functional
Antagonist activity at mouse EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at mouse EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 402 4 0 5 5.4 COc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
30897313 128376 0 None -2 5 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 402 4 0 5 5.4 COc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586309 128376 0 None -2 5 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 402 4 0 5 5.4 COc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
122180272 128399 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 403 4 0 6 4.8 COc1cc(-c2nsc3ccccc23)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586335 128399 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 403 4 0 6 4.8 COc1cc(-c2nsc3ccccc23)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
122180279 128406 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 419 4 0 5 5.1 COc1cc(-n2ccc3cc(Cl)ccc32)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586342 128406 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 419 4 0 5 5.1 COc1cc(-n2ccc3cc(Cl)ccc32)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
122180249 128379 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 403 4 0 6 4.8 COc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1cncnc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586312 128379 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 403 4 0 6 4.8 COc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1cncnc1)C2 10.1021/acs.jmedchem.5b00567
30956824 128378 4 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 402 4 0 5 5.4 COc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1ccncc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586311 128378 4 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 402 4 0 5 5.4 COc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1ccncc1)C2 10.1021/acs.jmedchem.5b00567
122180277 128404 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 419 4 0 5 5.1 COc1cc(-n2cc(Cl)c3ccccc32)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586340 128404 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 419 4 0 5 5.1 COc1cc(-n2cc(Cl)c3ccccc32)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
44365207 47470 0 None - 0 Human 6.6 pKd = 6.6 Functional
Compound was tested for antagonism of Prostaglandin E2 receptor activity in guinea pig ileum assay based on the dose ratio at 3 uMCompound was tested for antagonism of Prostaglandin E2 receptor activity in guinea pig ileum assay based on the dose ratio at 3 uM
ChEMBL 489 5 2 6 3.8 O=C(CCS(=O)(=O)Cc1ccco1)NNC(=O)N1Cc2ccccc2Oc2ccc(Cl)cc21 10.1016/0960-894X(94)80027-8
CHEMBL148449 47470 0 None - 0 Human 6.6 pKd = 6.6 Functional
Compound was tested for antagonism of Prostaglandin E2 receptor activity in guinea pig ileum assay based on the dose ratio at 3 uMCompound was tested for antagonism of Prostaglandin E2 receptor activity in guinea pig ileum assay based on the dose ratio at 3 uM
ChEMBL 489 5 2 6 3.8 O=C(CCS(=O)(=O)Cc1ccco1)NNC(=O)N1Cc2ccccc2Oc2ccc(Cl)cc21 10.1016/0960-894X(94)80027-8
38191 16685 16 None - 0 Human 6.2 pKd = 6.2 Functional
Compound was tested for antagonism of Prostaglandin E2 receptor activity in guinea pig ileum assay based on the dose ratio at 3 uMCompound was tested for antagonism of Prostaglandin E2 receptor activity in guinea pig ileum assay based on the dose ratio at 3 uM
ChEMBL 407 4 2 3 4.6 O=C(CCCCCl)NNC(=O)N1Cc2ccccc2Oc2ccc(Cl)cc21 10.1016/0960-894X(94)80027-8
CHEMBL114395 16685 16 None - 0 Human 6.2 pKd = 6.2 Functional
Compound was tested for antagonism of Prostaglandin E2 receptor activity in guinea pig ileum assay based on the dose ratio at 3 uMCompound was tested for antagonism of Prostaglandin E2 receptor activity in guinea pig ileum assay based on the dose ratio at 3 uM
ChEMBL 407 4 2 3 4.6 O=C(CCCCCl)NNC(=O)N1Cc2ccccc2Oc2ccc(Cl)cc21 10.1016/0960-894X(94)80027-8
44365227 128764 0 None - 0 Human 6.2 pKd = 6.2 Functional
Compound was tested for antagonism of Prostaglandin E2 receptor activity in guinea pig ileum assay based on the dose ratio at 3 uMCompound was tested for antagonism of Prostaglandin E2 receptor activity in guinea pig ileum assay based on the dose ratio at 3 uM
ChEMBL 473 5 2 5 4.1 O=C(CC[S+]([O-])Cc1ccco1)NNC(=O)N1Cc2ccccc2Oc2ccc(Cl)cc21 10.1016/0960-894X(94)80027-8
CHEMBL359231 128764 0 None - 0 Human 6.2 pKd = 6.2 Functional
Compound was tested for antagonism of Prostaglandin E2 receptor activity in guinea pig ileum assay based on the dose ratio at 3 uMCompound was tested for antagonism of Prostaglandin E2 receptor activity in guinea pig ileum assay based on the dose ratio at 3 uM
ChEMBL 473 5 2 5 4.1 O=C(CC[S+]([O-])Cc1ccco1)NNC(=O)N1Cc2ccccc2Oc2ccc(Cl)cc21 10.1016/0960-894X(94)80027-8
1924 10315 39 None - 0 Human 8.1 pKd = 8.1 Functional
Compound was tested for antagonism of Prostaglandin E2 receptor activity in guinea pig ileum assay based on the dose ratio at 3 uMCompound was tested for antagonism of Prostaglandin E2 receptor activity in guinea pig ileum assay based on the dose ratio at 3 uM
ChEMBL 457 5 2 5 5.1 O=C(NNC(=O)N1Cc2ccccc2Oc2c1cc(Cl)cc2)CCSCc1ccco1 10.1016/0960-894X(94)80027-8
9933831 10315 39 None - 0 Human 8.1 pKd = 8.1 Functional
Compound was tested for antagonism of Prostaglandin E2 receptor activity in guinea pig ileum assay based on the dose ratio at 3 uMCompound was tested for antagonism of Prostaglandin E2 receptor activity in guinea pig ileum assay based on the dose ratio at 3 uM
ChEMBL 457 5 2 5 5.1 O=C(NNC(=O)N1Cc2ccccc2Oc2c1cc(Cl)cc2)CCSCc1ccco1 10.1016/0960-894X(94)80027-8
CHEMBL358653 10315 39 None - 0 Human 8.1 pKd = 8.1 Functional
Compound was tested for antagonism of Prostaglandin E2 receptor activity in guinea pig ileum assay based on the dose ratio at 3 uMCompound was tested for antagonism of Prostaglandin E2 receptor activity in guinea pig ileum assay based on the dose ratio at 3 uM
ChEMBL 457 5 2 5 5.1 O=C(NNC(=O)N1Cc2ccccc2Oc2c1cc(Cl)cc2)CCSCc1ccco1 10.1016/0960-894X(94)80027-8
119461 7108 72 None - 0 Human 5.9 pKi = 5.9 Functional
Antagonist activity at EP2 receptor (unknown origin) by functional cAMP assayAntagonist activity at EP2 receptor (unknown origin) by functional cAMP assay
ChEMBL 298 3 1 4 3.4 CC(Oc1ccc2c(c1)oc1c(c2=O)cc(cc1)C(=O)O)C 10.1021/jm401431x
1896 7108 72 None - 0 Human 5.9 pKi = 5.9 Functional
Antagonist activity at EP2 receptor (unknown origin) by functional cAMP assayAntagonist activity at EP2 receptor (unknown origin) by functional cAMP assay
ChEMBL 298 3 1 4 3.4 CC(Oc1ccc2c(c1)oc1c(c2=O)cc(cc1)C(=O)O)C 10.1021/jm401431x
CHEMBL1317823 7108 72 None - 0 Human 5.9 pKi = 5.9 Functional
Antagonist activity at EP2 receptor (unknown origin) by functional cAMP assayAntagonist activity at EP2 receptor (unknown origin) by functional cAMP assay
ChEMBL 298 3 1 4 3.4 CC(Oc1ccc2c(c1)oc1c(c2=O)cc(cc1)C(=O)O)C 10.1021/jm401431x
9817405 172182 5 None - 0 Human 4.9 pKi = 4.9 Functional
Antagonistic activity at Prostanoid EP2 receptor in human was determinedAntagonistic activity at Prostanoid EP2 receptor in human was determined
ChEMBL 288 4 1 1 4.5 O=C(O)/C=C/c1ccccc1Cc1ccc2ccccc2c1 10.1016/s0960-894x(01)00056-7
CHEMBL423815 172182 5 None - 0 Human 4.9 pKi = 4.9 Functional
Antagonistic activity at Prostanoid EP2 receptor in human was determinedAntagonistic activity at Prostanoid EP2 receptor in human was determined
ChEMBL 288 4 1 1 4.5 O=C(O)/C=C/c1ccccc1Cc1ccc2ccccc2c1 10.1016/s0960-894x(01)00056-7
10402929 64317 0 None - 0 Human 4.9 pKi = 4.9 Functional
Antagonistic activity at Prostanoid EP2 receptor in human was determinedAntagonistic activity at Prostanoid EP2 receptor in human was determined
ChEMBL 306 4 1 1 4.7 O=C(O)/C=C/c1ccccc1Cc1ccc(Cl)c(Cl)c1 10.1016/s0960-894x(01)00056-7
CHEMBL166351 64317 0 None - 0 Human 4.9 pKi = 4.9 Functional
Antagonistic activity at Prostanoid EP2 receptor in human was determinedAntagonistic activity at Prostanoid EP2 receptor in human was determined
ChEMBL 306 4 1 1 4.7 O=C(O)/C=C/c1ccccc1Cc1ccc(Cl)c(Cl)c1 10.1016/s0960-894x(01)00056-7
44377464 126863 0 None - 0 Human 5.4 pKi = 5.4 Functional
Antagonistic activity at Prostanoid EP2 receptor in human was determinedAntagonistic activity at Prostanoid EP2 receptor in human was determined
ChEMBL 306 4 1 1 4.7 O=C(O)/C=C/c1ccccc1Cc1ccc(Cl)cc1Cl 10.1016/s0960-894x(01)00056-7
CHEMBL350832 126863 0 None - 0 Human 5.4 pKi = 5.4 Functional
Antagonistic activity at Prostanoid EP2 receptor in human was determinedAntagonistic activity at Prostanoid EP2 receptor in human was determined
ChEMBL 306 4 1 1 4.7 O=C(O)/C=C/c1ccccc1Cc1ccc(Cl)cc1Cl 10.1016/s0960-894x(01)00056-7
9817292 64001 0 None - 0 Human 4.4 pKi = 4.4 Functional
Antagonistic activity at Prostanoid EP2 receptor in human was determinedAntagonistic activity at Prostanoid EP2 receptor in human was determined
ChEMBL 284 5 1 2 4.1 CSc1ccc(Cc2ccccc2/C=C/C(=O)O)cc1 10.1016/s0960-894x(01)00056-7
CHEMBL165010 64001 0 None - 0 Human 4.4 pKi = 4.4 Functional
Antagonistic activity at Prostanoid EP2 receptor in human was determinedAntagonistic activity at Prostanoid EP2 receptor in human was determined
ChEMBL 284 5 1 2 4.1 CSc1ccc(Cc2ccccc2/C=C/C(=O)O)cc1 10.1016/s0960-894x(01)00056-7
10483360 206007 28 None - 4 Human 4.4 pKi = 4.4 Functional
Inhibition of EP2 expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP productionInhibition of EP2 expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP production
ChEMBL 580 12 3 6 5.8 CCCCNC(=O)c1ccc(Oc2ccc(CC(=O)O)cc2OC)c(NS(=O)(=O)c2ccc(Cl)cc2Cl)c1 10.1016/j.bmcl.2009.09.052
CHEMBL589973 206007 28 None - 4 Human 4.4 pKi = 4.4 Functional
Inhibition of EP2 expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP productionInhibition of EP2 expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP production
ChEMBL 580 12 3 6 5.8 CCCCNC(=O)c1ccc(Oc2ccc(CC(=O)O)cc2OC)c(NS(=O)(=O)c2ccc(Cl)cc2Cl)c1 10.1016/j.bmcl.2009.09.052
138 9855 88 None -4 10 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O None
149351 9855 88 None -4 10 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O None
1882 9855 88 None -4 10 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O None
5280723 9855 88 None -4 10 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O None
CHEMBL495 9855 88 None -4 10 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O None
DB00770 9855 88 None -4 10 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O None
44230999 174225 26 None - 1 Human 8.1 pEC50 = 8.1 Functional
activity measured for the active metabolite (omidenepag)activity measured for the active metabolite (omidenepag)
Drug Central 520 11 1 9 3.4 CC(C)OC(=O)CNc1cccc(CN(Cc2ccc(-n3cccn3)cc2)S(=O)(=O)c2cccnc2)n1 None
CHEMBL4297666 174225 26 None - 1 Human 8.1 pEC50 = 8.1 Functional
activity measured for the active metabolite (omidenepag)activity measured for the active metabolite (omidenepag)
Drug Central 520 11 1 9 3.4 CC(C)OC(=O)CNc1cccc(CN(Cc2ccc(-n3cccn3)cc2)S(=O)(=O)c2cccnc2)n1 None
DB15071 174225 26 None - 1 Human 8.1 pEC50 = 8.1 Functional
activity measured for the active metabolite (omidenepag)activity measured for the active metabolite (omidenepag)
Drug Central 520 11 1 9 3.4 CC(C)OC(=O)CNc1cccc(CN(Cc2ccc(-n3cccn3)cc2)S(=O)(=O)c2cccnc2)n1 None
1929 8386 55 None 2 2 Rat 9.5 pEC50 = 9.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 468 9 1 5 4.2 OC(=O)COc1cccc(c1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)C(C)(C)C 19250823
9890801 8386 55 None 2 2 Rat 9.5 pEC50 = 9.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 468 9 1 5 4.2 OC(=O)COc1cccc(c1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)C(C)(C)C 19250823
CHEMBL563646 8386 55 None 2 2 Rat 9.5 pEC50 = 9.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 468 9 1 5 4.2 OC(=O)COc1cccc(c1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)C(C)(C)C 19250823
DB12022 8386 55 None 2 2 Rat 9.5 pEC50 = 9.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 468 9 1 5 4.2 OC(=O)COc1cccc(c1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)C(C)(C)C 19250823
1883 9856 75 None -2 12 Rat 8.1 pIC50 = 8.1 Functional
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
Drug Central 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O None
1916 9856 75 None -2 12 Rat 8.1 pIC50 = 8.1 Functional
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
Drug Central 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O None
5280360 9856 75 None -2 12 Rat 8.1 pIC50 = 8.1 Functional
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
Drug Central 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O None
913 9856 75 None -2 12 Rat 8.1 pIC50 = 8.1 Functional
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
Drug Central 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O None
CHEMBL548 9856 75 None -2 12 Rat 8.1 pIC50 = 8.1 Functional
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
Drug Central 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O None
DB00917 9856 75 None -2 12 Rat 8.1 pIC50 = 8.1 Functional
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
Drug Central 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O None
1929 8386 55 None 2 2 Rat 7.3 pIC50 = 7.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 468 9 1 5 4.2 OC(=O)COc1cccc(c1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)C(C)(C)C 19250823
9890801 8386 55 None 2 2 Rat 7.3 pIC50 = 7.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 468 9 1 5 4.2 OC(=O)COc1cccc(c1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)C(C)(C)C 19250823
CHEMBL563646 8386 55 None 2 2 Rat 7.3 pIC50 = 7.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 468 9 1 5 4.2 OC(=O)COc1cccc(c1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)C(C)(C)C 19250823
DB12022 8386 55 None 2 2 Rat 7.3 pIC50 = 7.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 468 9 1 5 4.2 OC(=O)COc1cccc(c1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)C(C)(C)C 19250823
18376177 10525 50 None -1 2 Human 8.0 pIC50 = 8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 478 10 1 7 3.1 OC(=O)COc1cccc(c1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)n1cccn1 21376717
5816 10525 50 None -1 2 Human 8.0 pIC50 = 8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 478 10 1 7 3.1 OC(=O)COc1cccc(c1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)n1cccn1 21376717
CHEMBL2107783 10525 50 None -1 2 Human 8.0 pIC50 = 8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 478 10 1 7 3.1 OC(=O)COc1cccc(c1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)n1cccn1 21376717
DB12623 10525 50 None -1 2 Human 8.0 pIC50 = 8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 478 10 1 7 3.1 OC(=O)COc1cccc(c1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)n1cccn1 21376717
18376177 10525 50 None 1 2 Rat 8.3 pIC50 = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 478 10 1 7 3.1 OC(=O)COc1cccc(c1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)n1cccn1 21376717
5816 10525 50 None 1 2 Rat 8.3 pIC50 = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 478 10 1 7 3.1 OC(=O)COc1cccc(c1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)n1cccn1 21376717
CHEMBL2107783 10525 50 None 1 2 Rat 8.3 pIC50 = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 478 10 1 7 3.1 OC(=O)COc1cccc(c1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)n1cccn1 21376717
DB12623 10525 50 None 1 2 Rat 8.3 pIC50 = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 478 10 1 7 3.1 OC(=O)COc1cccc(c1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)n1cccn1 21376717
12520 10568 0 None - 1 Human 7.9 pKB = 7.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 344 5 3 2 3.8 CC1=C(CCNC(=O)C2=CC=C(C=C2)C3=CNC=N3)C4=C(N1)C=CC=C4 35187419
12520 10568 0 None - 1 Human 7.9 pKB = 7.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 344 5 3 2 3.8 CC1=C(CCNC(=O)C2=CC=C(C=C2)C3=CNC=N3)C4=C(N1)C=CC=C4 36654746
155128767 10568 0 None - 1 Human 7.9 pKB = 7.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 344 5 3 2 3.8 CC1=C(CCNC(=O)C2=CC=C(C=C2)C3=CNC=N3)C4=C(N1)C=CC=C4 35187419
155128767 10568 0 None - 1 Human 7.9 pKB = 7.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 344 5 3 2 3.8 CC1=C(CCNC(=O)C2=CC=C(C=C2)C3=CNC=N3)C4=C(N1)C=CC=C4 36654746
10603 10564 0 None 537 3 Human 8.0 pKB = 8.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 400 6 3 5 4.0 Cc1cc(Nc2ncc(cn2)C(=O)NCCc2c(C)[nH]c3c2cccc3)nc(c1)C 31904232
145996528 10564 0 None 537 3 Human 8.0 pKB = 8.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 400 6 3 5 4.0 Cc1cc(Nc2ncc(cn2)C(=O)NCCc2c(C)[nH]c3c2cccc3)nc(c1)C 31904232
CHEMBL4552900 10564 0 None 537 3 Human 8.0 pKB = 8.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 400 6 3 5 4.0 Cc1cc(Nc2ncc(cn2)C(=O)NCCc2c(C)[nH]c3c2cccc3)nc(c1)C 31904232
1987175 10566 31 None 1 5 Human 8.1 pKB = 8.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 491 7 3 7 3.6 CCc1nnc(s1)NS(=O)(=O)c1ccc(cc1)NC(=S)NC(=O)/C=C/c1ccc(cc1)F 23914286
9283 10566 31 None 1 5 Human 8.1 pKB = 8.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 491 7 3 7 3.6 CCc1nnc(s1)NS(=O)(=O)c1ccc(cc1)NC(=S)NC(=O)/C=C/c1ccc(cc1)F 23914286
CHEMBL1372836 10566 31 None 1 5 Human 8.1 pKB = 8.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 491 7 3 7 3.6 CCc1nnc(s1)NS(=O)(=O)c1ccc(cc1)NC(=S)NC(=O)/C=C/c1ccc(cc1)F 23914286
25114442 9835 56 None -1 3 Human 8.3 pKB = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 409 6 1 4 3.6 COc1ccc2c(c1)ccc(c2)OCC1(CN(C1)C(=O)c1ccc(cc1)F)C(=O)O 21595651
25114442 9835 56 None -1 3 Human 8.3 pKB = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 409 6 1 4 3.6 COc1ccc2c(c1)ccc(c2)OCC1(CN(C1)C(=O)c1ccc(cc1)F)C(=O)O 22747912
5817 9835 56 None -1 3 Human 8.3 pKB = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 409 6 1 4 3.6 COc1ccc2c(c1)ccc(c2)OCC1(CN(C1)C(=O)c1ccc(cc1)F)C(=O)O 21595651
5817 9835 56 None -1 3 Human 8.3 pKB = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 409 6 1 4 3.6 COc1ccc2c(c1)ccc(c2)OCC1(CN(C1)C(=O)c1ccc(cc1)F)C(=O)O 22747912
CHEMBL3286797 9835 56 None -1 3 Human 8.3 pKB = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 409 6 1 4 3.6 COc1ccc2c(c1)ccc(c2)OCC1(CN(C1)C(=O)c1ccc(cc1)F)C(=O)O 21595651
CHEMBL3286797 9835 56 None -1 3 Human 8.3 pKB = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 409 6 1 4 3.6 COc1ccc2c(c1)ccc(c2)OCC1(CN(C1)C(=O)c1ccc(cc1)F)C(=O)O 22747912
DB12024 9835 56 None -1 3 Human 8.3 pKB = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 409 6 1 4 3.6 COc1ccc2c(c1)ccc(c2)OCC1(CN(C1)C(=O)c1ccc(cc1)F)C(=O)O 21595651
DB12024 9835 56 None -1 3 Human 8.3 pKB = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 409 6 1 4 3.6 COc1ccc2c(c1)ccc(c2)OCC1(CN(C1)C(=O)c1ccc(cc1)F)C(=O)O 22747912
25114442 9835 56 None 1 3 Mouse 8.3 pKB = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 409 6 1 4 3.6 COc1ccc2c(c1)ccc(c2)OCC1(CN(C1)C(=O)c1ccc(cc1)F)C(=O)O 22747912
5817 9835 56 None 1 3 Mouse 8.3 pKB = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 409 6 1 4 3.6 COc1ccc2c(c1)ccc(c2)OCC1(CN(C1)C(=O)c1ccc(cc1)F)C(=O)O 22747912
CHEMBL3286797 9835 56 None 1 3 Mouse 8.3 pKB = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 409 6 1 4 3.6 COc1ccc2c(c1)ccc(c2)OCC1(CN(C1)C(=O)c1ccc(cc1)F)C(=O)O 22747912
DB12024 9835 56 None 1 3 Mouse 8.3 pKB = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 409 6 1 4 3.6 COc1ccc2c(c1)ccc(c2)OCC1(CN(C1)C(=O)c1ccc(cc1)F)C(=O)O 22747912
46213069 9837 0 None - 1 Human 8.5 pKB = 8.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 456 7 1 5 4.2 COc1ccc(cc1)C(=O)N1CCC(C1)(COc1ccc(cc1)c1ccc(cc1)C#N)C(=O)O 23786281
8538 9837 0 None - 1 Human 8.5 pKB = 8.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 456 7 1 5 4.2 COc1ccc(cc1)C(=O)N1CCC(C1)(COc1ccc(cc1)c1ccc(cc1)C#N)C(=O)O 23786281
CHEMBL5285583 9837 0 None - 1 Human 8.5 pKB = 8.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 456 7 1 5 4.2 COc1ccc(cc1)C(=O)N1CCC(C1)(COc1ccc(cc1)c1ccc(cc1)C#N)C(=O)O 23786281
8546 10567 0 None - 1 Human 8.6 pKB = 8.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 377 9 1 3 4.5 CCN(c1ccc(cc1)CC(=O)NCCCn1c(C)cc2c1cccc2)CC 24937185
91827368 10567 0 None - 1 Human 8.6 pKB = 8.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 377 9 1 3 4.5 CCN(c1ccc(cc1)CC(=O)NCCCn1c(C)cc2c1cccc2)CC 24937185
5818 10565 47 None 1096 2 Human 8.6 pKB = 8.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 394 8 1 5 3.8 COc1cc(/C=C/C(=O)NCCn2c(C)cc3c2cccc3)cc(c1OC)OC 22323596
5886965 10565 47 None 1096 2 Human 8.6 pKB = 8.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 394 8 1 5 3.8 COc1cc(/C=C/C(=O)NCCn2c(C)cc3c2cccc3)cc(c1OC)OC 22323596
CHEMBL1368005 10565 47 None 1096 2 Human 8.6 pKB = 8.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 394 8 1 5 3.8 COc1cc(/C=C/C(=O)NCCn2c(C)cc3c2cccc3)cc(c1OC)OC 22323596




Ligands Receptor Assay information Chemical information
Sel. page Common
name
GPCRdb ID #Vendors Reference
ligand
Fold selectivity
(Affinity)
# tested GPCRs
(Affinity)
Species p-value
(-log)
Type Activity
Relation
Activity
Value
Assay Type Assay Description Source Mol
weight
Rot
Bonds
H don H acc LogP Smiles DOI
11855868 159323 0 None - 1 Human 9.8 pEC50 = 9.8 Binding
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulationAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulation
ChEMBL 429 11 2 4 5.6 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2CCCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3971632 159323 0 None - 1 Human 9.8 pEC50 = 9.8 Binding
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulationAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulation
ChEMBL 429 11 2 4 5.6 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2CCCc2ccc(C(=O)O)s2)cc1 nan
127037150 144338 0 None - 0 Human 9.4 pEC50 = 9.4 Binding
Agonist activity at human EP2 receptorAgonist activity at human EP2 receptor
ChEMBL 426 12 2 6 4.1 CCCC[C@H](C)C[C@H](O)/C=C/[C@H]1CCC(=O)N1CCSc1nc(C(=O)O)cs1 10.1016/j.bmcl.2015.12.039
CHEMBL3754586 144338 0 None - 0 Human 9.4 pEC50 = 9.4 Binding
Agonist activity at human EP2 receptorAgonist activity at human EP2 receptor
ChEMBL 426 12 2 6 4.1 CCCC[C@H](C)C[C@H](O)/C=C/[C@H]1CCC(=O)N1CCSc1nc(C(=O)O)cs1 10.1016/j.bmcl.2015.12.039
16725337 156380 0 None - 1 Human 9.2 pEC50 = 9.2 Binding
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulationAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulation
ChEMBL 443 12 2 4 6.0 CCCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2CCCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3947001 156380 0 None - 1 Human 9.2 pEC50 = 9.2 Binding
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulationAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulation
ChEMBL 443 12 2 4 6.0 CCCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2CCCc2ccc(C(=O)O)s2)cc1 nan
59554827 144071 0 None - 0 Human 9.0 pEC50 = 9.0 Binding
Agonist activity at human EP2 receptorAgonist activity at human EP2 receptor
ChEMBL 426 11 2 6 4.1 CCCCC(C)(C)[C@H](O)/C=C/[C@H]1CCC(=O)N1CCSc1nc(C(=O)O)cs1 10.1016/j.bmcl.2015.12.039
CHEMBL3752377 144071 0 None - 0 Human 9.0 pEC50 = 9.0 Binding
Agonist activity at human EP2 receptorAgonist activity at human EP2 receptor
ChEMBL 426 11 2 6 4.1 CCCCC(C)(C)[C@H](O)/C=C/[C@H]1CCC(=O)N1CCSc1nc(C(=O)O)cs1 10.1016/j.bmcl.2015.12.039
11502897 149571 0 None - 1 Human 8.8 pEC50 = 8.8 Binding
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulationAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulation
ChEMBL 431 11 2 5 4.8 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3892847 149571 0 None - 1 Human 8.8 pEC50 = 8.8 Binding
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulationAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulation
ChEMBL 431 11 2 5 4.8 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
11855865 160056 0 None - 1 Human 8.8 pEC50 = 8.8 Binding
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulationAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulation
ChEMBL 445 12 2 5 5.2 CCCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3977724 160056 0 None - 1 Human 8.8 pEC50 = 8.8 Binding
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulationAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulation
ChEMBL 445 12 2 5 5.2 CCCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
11855870 153058 0 None - 1 Human 8.8 pEC50 = 8.8 Binding
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulationAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulation
ChEMBL 427 11 1 4 5.7 CCCCCC(=O)c1ccc(N2C(=O)CC[C@@H]2CCCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3920756 153058 0 None - 1 Human 8.8 pEC50 = 8.8 Binding
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulationAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulation
ChEMBL 427 11 1 4 5.7 CCCCCC(=O)c1ccc(N2C(=O)CC[C@@H]2CCCc2ccc(C(=O)O)s2)cc1 nan
1932 9716 5 None 1 6 Human 8.7 pEC50 = 8.7 Binding
Agonist activity at EP2 receptor (unknown origin) by functional assayAgonist activity at EP2 receptor (unknown origin) by functional assay
ChEMBL 410 12 3 3 4.8 C=CCC1(CCC1)[C@H](C/C=C/[C@H]1[C@H](O)C[C@H]([C@@H]1C/C=C\CCCC(=O)O)Cl)O 10.1021/jm401431x
5311228 9716 5 None 1 6 Human 8.7 pEC50 = 8.7 Binding
Agonist activity at EP2 receptor (unknown origin) by functional assayAgonist activity at EP2 receptor (unknown origin) by functional assay
ChEMBL 410 12 3 3 4.8 C=CCC1(CCC1)[C@H](C/C=C/[C@H]1[C@H](O)C[C@H]([C@@H]1C/C=C\CCCC(=O)O)Cl)O 10.1021/jm401431x
CHEMBL3286796 9716 5 None 1 6 Human 8.7 pEC50 = 8.7 Binding
Agonist activity at EP2 receptor (unknown origin) by functional assayAgonist activity at EP2 receptor (unknown origin) by functional assay
ChEMBL 410 12 3 3 4.8 C=CCC1(CCC1)[C@H](C/C=C/[C@H]1[C@H](O)C[C@H]([C@@H]1C/C=C\CCCC(=O)O)Cl)O 10.1021/jm401431x
90054482 150695 0 None - 0 Human 6.0 pEC50 = 6 Binding
SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.
ChEMBL 463 10 2 4 4.4 C[C@@H](Cc1ccccc1)[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCc1ccc(C(=O)O)s1 nan
CHEMBL3902065 150695 0 None - 0 Human 6.0 pEC50 = 6 Binding
SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.
ChEMBL 463 10 2 4 4.4 C[C@@H](Cc1ccccc1)[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCc1ccc(C(=O)O)s1 nan
90054490 158969 0 None - 0 Human 6.0 pEC50 = 6.0 Binding
SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.
ChEMBL 519 14 2 4 6.0 C[C@@H](CCCCCc1ccccc1)[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCc1ccc(C(=O)O)s1 nan
CHEMBL3968443 158969 0 None - 0 Human 6.0 pEC50 = 6.0 Binding
SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.
ChEMBL 519 14 2 4 6.0 C[C@@H](CCCCCc1ccccc1)[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCc1ccc(C(=O)O)s1 nan
127051063 147100 0 None - 0 Human 8.0 pEC50 = 8.0 Binding
Agonist activity at PK2-tagged human EP2 receptor expressed in HEK293 cells assessed as induction of EA-tagged beta-arrestin recruitment incubated for 90 mins by beta-galactosidase reporter gene assayAgonist activity at PK2-tagged human EP2 receptor expressed in HEK293 cells assessed as induction of EA-tagged beta-arrestin recruitment incubated for 90 mins by beta-galactosidase reporter gene assay
ChEMBL 443 5 2 6 4.2 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3COc3ccccc3C(F)(F)F)O2)n1 10.1021/acsmedchemlett.5b00455
CHEMBL3806284 147100 0 None - 0 Human 8.0 pEC50 = 8.0 Binding
Agonist activity at PK2-tagged human EP2 receptor expressed in HEK293 cells assessed as induction of EA-tagged beta-arrestin recruitment incubated for 90 mins by beta-galactosidase reporter gene assayAgonist activity at PK2-tagged human EP2 receptor expressed in HEK293 cells assessed as induction of EA-tagged beta-arrestin recruitment incubated for 90 mins by beta-galactosidase reporter gene assay
ChEMBL 443 5 2 6 4.2 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3COc3ccccc3C(F)(F)F)O2)n1 10.1021/acsmedchemlett.5b00455
11855590 151152 0 None - 0 Human 5.9 pEC50 = 5.9 Binding
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulationAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulation
ChEMBL 387 8 2 5 3.4 CC(C)C(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)o2)cc1 nan
CHEMBL3905811 151152 0 None - 0 Human 5.9 pEC50 = 5.9 Binding
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulationAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulation
ChEMBL 387 8 2 5 3.4 CC(C)C(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)o2)cc1 nan
90054450 150554 0 None - 0 Human 5.9 pEC50 = 5.9 Binding
SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.
ChEMBL 493 13 2 4 5.4 C[C@@H](CCCc1ccccc1)[C@H](O)CC[C@H]1CC(F)(F)C(=O)N1CCCc1ccc(C(=O)O)s1 nan
CHEMBL3900979 150554 0 None - 0 Human 5.9 pEC50 = 5.9 Binding
SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.
ChEMBL 493 13 2 4 5.4 C[C@@H](CCCc1ccccc1)[C@H](O)CC[C@H]1CC(F)(F)C(=O)N1CCCc1ccc(C(=O)O)s1 nan
11855591 151214 0 None - 1 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulationAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulation
ChEMBL 435 9 2 5 4.0 O=C(O)c1ccc(COC[C@H]2CCC(=O)N2c2ccc(C(O)Cc3ccccc3)cc2)o1 nan
CHEMBL3906402 151214 0 None - 1 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulationAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulation
ChEMBL 435 9 2 5 4.0 O=C(O)c1ccc(COC[C@H]2CCC(=O)N2c2ccc(C(O)Cc3ccccc3)cc2)o1 nan
72948479 159812 0 None - 1 Human 6.8 pEC50 = 6.8 Binding
SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.
ChEMBL 491 12 2 4 5.2 C[C@@H](CCCc1ccccc1)[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCc1ccc(C(=O)O)s1 nan
CHEMBL3975743 159812 0 None - 1 Human 6.8 pEC50 = 6.8 Binding
SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.
ChEMBL 491 12 2 4 5.2 C[C@@H](CCCc1ccccc1)[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCc1ccc(C(=O)O)s1 nan
70667255 158253 0 None - 1 Human 7.8 pEC50 = 7.8 Binding
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulationAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulation
ChEMBL 427 10 2 4 5.4 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2C=CCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3962183 158253 0 None - 1 Human 7.8 pEC50 = 7.8 Binding
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulationAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulation
ChEMBL 427 10 2 4 5.4 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2C=CCc2ccc(C(=O)O)s2)cc1 nan
90054430 156143 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.
ChEMBL 505 13 2 4 5.6 C[C@@H](CCCCc1ccccc1)[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCc1ccc(C(=O)O)s1 nan
CHEMBL3945327 156143 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.
ChEMBL 505 13 2 4 5.6 C[C@@H](CCCCc1ccccc1)[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCc1ccc(C(=O)O)s1 nan
5283056 209639 34 None - 0 Human 7.8 pEC50 = 7.8 Binding
SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.
ChEMBL 354 13 3 4 3.5 CCCCC[C@@H](O)/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O nan
CHEMBL62570 209639 34 None - 0 Human 7.8 pEC50 = 7.8 Binding
SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.
ChEMBL 354 13 3 4 3.5 CCCCC[C@@H](O)/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O nan
66858111 144229 0 None - 1 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human EP2 receptorAgonist activity at human EP2 receptor
ChEMBL 488 11 2 7 4.5 O=C(O)c1csc(SCCN2C(=O)OC[C@@H]2/C=C/[C@@H](O)C2(CCc3ccccc3)CCC2)n1 10.1016/j.bmcl.2015.12.039
CHEMBL3753622 144229 0 None - 1 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human EP2 receptorAgonist activity at human EP2 receptor
ChEMBL 488 11 2 7 4.5 O=C(O)c1csc(SCCN2C(=O)OC[C@@H]2/C=C/[C@@H](O)C2(CCc3ccccc3)CCC2)n1 10.1016/j.bmcl.2015.12.039
72950425 149828 0 None - 1 Human 5.8 pEC50 = 5.8 Binding
SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.
ChEMBL 419 8 2 3 3.5 CCC#CC[C@H](C)[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCc1ccc(C(=O)O)cc1 nan
CHEMBL3895047 149828 0 None - 1 Human 5.8 pEC50 = 5.8 Binding
SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.
ChEMBL 419 8 2 3 3.5 CCC#CC[C@H](C)[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCc1ccc(C(=O)O)cc1 nan
11328569 144246 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Agonist activity at human EP2 receptorAgonist activity at human EP2 receptor
ChEMBL 456 12 2 8 3.3 COCCCC1([C@H](O)/C=C/[C@H]2COC(=O)N2CCSc2nc(C(=O)O)cs2)CCC1 10.1016/j.bmcl.2015.12.039
CHEMBL3753788 144246 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Agonist activity at human EP2 receptorAgonist activity at human EP2 receptor
ChEMBL 456 12 2 8 3.3 COCCCC1([C@H](O)/C=C/[C@H]2COC(=O)N2CCSc2nc(C(=O)O)cs2)CCC1 10.1016/j.bmcl.2015.12.039
11855324 149383 0 None - 1 Human 6.7 pEC50 = 6.7 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 6.0 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 6.0 membranes incubated for 60 mins
ChEMBL 371 6 1 4 4.0 CC(C)(C)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)o2)cc1 nan
CHEMBL3891401 149383 0 None - 1 Human 6.7 pEC50 = 6.7 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 6.0 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 6.0 membranes incubated for 60 mins
ChEMBL 371 6 1 4 4.0 CC(C)(C)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)o2)cc1 nan
72950929 153360 0 None - 1 Human 5.7 pEC50 = 5.7 Binding
SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.
ChEMBL 395 10 2 3 3.7 CCCCC[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCc1ccc(C(=O)O)cc1 nan
CHEMBL3923027 153360 0 None - 1 Human 5.7 pEC50 = 5.7 Binding
SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.
ChEMBL 395 10 2 3 3.7 CCCCC[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCc1ccc(C(=O)O)cc1 nan
1883 9856 75 None -6 24 Human 8.7 pEC50 = 8.7 Binding
Agonist activity at EP2 receptor (unknown origin) by functional assayAgonist activity at EP2 receptor (unknown origin) by functional assay
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/jm401431x
1916 9856 75 None -6 24 Human 8.7 pEC50 = 8.7 Binding
Agonist activity at EP2 receptor (unknown origin) by functional assayAgonist activity at EP2 receptor (unknown origin) by functional assay
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/jm401431x
5280360 9856 75 None -6 24 Human 8.7 pEC50 = 8.7 Binding
Agonist activity at EP2 receptor (unknown origin) by functional assayAgonist activity at EP2 receptor (unknown origin) by functional assay
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/jm401431x
913 9856 75 None -6 24 Human 8.7 pEC50 = 8.7 Binding
Agonist activity at EP2 receptor (unknown origin) by functional assayAgonist activity at EP2 receptor (unknown origin) by functional assay
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/jm401431x
CHEMBL548 9856 75 None -6 24 Human 8.7 pEC50 = 8.7 Binding
Agonist activity at EP2 receptor (unknown origin) by functional assayAgonist activity at EP2 receptor (unknown origin) by functional assay
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/jm401431x
DB00917 9856 75 None -6 24 Human 8.7 pEC50 = 8.7 Binding
Agonist activity at EP2 receptor (unknown origin) by functional assayAgonist activity at EP2 receptor (unknown origin) by functional assay
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/jm401431x
126495400 146099 0 None - 0 Human 8.6 pEC50 = 8.6 Binding
Agonist activity at human EP2 receptor expressed in HEK293 cells after 24 hrs beta-arrestin recruitment assayAgonist activity at human EP2 receptor expressed in HEK293 cells after 24 hrs beta-arrestin recruitment assay
ChEMBL 477 5 2 6 5.1 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3COc3ccc(Cl)c(Cl)c3Cl)O2)n1 10.1016/j.bmcl.2016.03.110
CHEMBL3792632 146099 0 None - 0 Human 8.6 pEC50 = 8.6 Binding
Agonist activity at human EP2 receptor expressed in HEK293 cells after 24 hrs beta-arrestin recruitment assayAgonist activity at human EP2 receptor expressed in HEK293 cells after 24 hrs beta-arrestin recruitment assay
ChEMBL 477 5 2 6 5.1 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3COc3ccc(Cl)c(Cl)c3Cl)O2)n1 10.1016/j.bmcl.2016.03.110
127026955 146228 0 None - 0 Human 8.6 pEC50 = 8.6 Binding
Agonist activity at human EP2 receptor expressed in HEK293 cells after 24 hrs beta-arrestin recruitment assayAgonist activity at human EP2 receptor expressed in HEK293 cells after 24 hrs beta-arrestin recruitment assay
ChEMBL 437 5 2 6 4.4 Cc1cc(OC[C@H]2[C@H](O)C[C@@H]3O[C@@H](c4nc(C(=O)O)cs4)CC[C@@H]32)cc(C)c1Cl 10.1016/j.bmcl.2016.03.110
CHEMBL3794016 146228 0 None - 0 Human 8.6 pEC50 = 8.6 Binding
Agonist activity at human EP2 receptor expressed in HEK293 cells after 24 hrs beta-arrestin recruitment assayAgonist activity at human EP2 receptor expressed in HEK293 cells after 24 hrs beta-arrestin recruitment assay
ChEMBL 437 5 2 6 4.4 Cc1cc(OC[C@H]2[C@H](O)C[C@@H]3O[C@@H](c4nc(C(=O)O)cs4)CC[C@@H]32)cc(C)c1Cl 10.1016/j.bmcl.2016.03.110
18376177 10525 50 None - 1 Human 8.6 pEC50 = 8.6 Binding
Agonist activity at EP2 receptor (unknown origin) by functional assayAgonist activity at EP2 receptor (unknown origin) by functional assay
ChEMBL 478 10 1 7 3.1 OC(=O)COc1cccc(c1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)n1cccn1 10.1021/jm401431x
5816 10525 50 None - 1 Human 8.6 pEC50 = 8.6 Binding
Agonist activity at EP2 receptor (unknown origin) by functional assayAgonist activity at EP2 receptor (unknown origin) by functional assay
ChEMBL 478 10 1 7 3.1 OC(=O)COc1cccc(c1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)n1cccn1 10.1021/jm401431x
CHEMBL2107783 10525 50 None - 1 Human 8.6 pEC50 = 8.6 Binding
Agonist activity at EP2 receptor (unknown origin) by functional assayAgonist activity at EP2 receptor (unknown origin) by functional assay
ChEMBL 478 10 1 7 3.1 OC(=O)COc1cccc(c1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)n1cccn1 10.1021/jm401431x
DB12623 10525 50 None - 1 Human 8.6 pEC50 = 8.6 Binding
Agonist activity at EP2 receptor (unknown origin) by functional assayAgonist activity at EP2 receptor (unknown origin) by functional assay
ChEMBL 478 10 1 7 3.1 OC(=O)COc1cccc(c1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)n1cccn1 10.1021/jm401431x
11294085 144030 0 None - 1 Human 8.5 pEC50 = 8.5 Binding
Agonist activity at human EP2 receptorAgonist activity at human EP2 receptor
ChEMBL 458 12 2 7 4.0 O=C(O)c1csc(SCCN2C(=O)OC[C@@H]2/C=C/[C@@H](O)C2(CCCCF)CCC2)n1 10.1016/j.bmcl.2015.12.039
CHEMBL3751951 144030 0 None - 1 Human 8.5 pEC50 = 8.5 Binding
Agonist activity at human EP2 receptorAgonist activity at human EP2 receptor
ChEMBL 458 12 2 7 4.0 O=C(O)c1csc(SCCN2C(=O)OC[C@@H]2/C=C/[C@@H](O)C2(CCCCF)CCC2)n1 10.1016/j.bmcl.2015.12.039
59554822 144172 0 None - 1 Human 8.5 pEC50 = 8.5 Binding
Agonist activity at human EP2 receptorAgonist activity at human EP2 receptor
ChEMBL 440 11 2 7 4.0 CCCCC1([C@H](O)/C=C/[C@H]2COC(=O)N2CCSc2nc(C(=O)O)cs2)CCC1 10.1016/j.bmcl.2015.12.039
CHEMBL3753221 144172 0 None - 1 Human 8.5 pEC50 = 8.5 Binding
Agonist activity at human EP2 receptorAgonist activity at human EP2 receptor
ChEMBL 440 11 2 7 4.0 CCCCC1([C@H](O)/C=C/[C@H]2COC(=O)N2CCSc2nc(C(=O)O)cs2)CCC1 10.1016/j.bmcl.2015.12.039
127051062 147052 0 None - 0 Human 6.7 pEC50 = 6.7 Binding
Agonist activity at PK2-tagged human EP2 receptor expressed in HEK293 cells assessed as induction of EA-tagged beta-arrestin recruitment incubated for 90 mins by beta-galactosidase reporter gene assayAgonist activity at PK2-tagged human EP2 receptor expressed in HEK293 cells assessed as induction of EA-tagged beta-arrestin recruitment incubated for 90 mins by beta-galactosidase reporter gene assay
ChEMBL 409 5 2 6 3.8 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3COc3ccccc3Cl)O2)n1 10.1021/acsmedchemlett.5b00455
CHEMBL3805767 147052 0 None - 0 Human 6.7 pEC50 = 6.7 Binding
Agonist activity at PK2-tagged human EP2 receptor expressed in HEK293 cells assessed as induction of EA-tagged beta-arrestin recruitment incubated for 90 mins by beta-galactosidase reporter gene assayAgonist activity at PK2-tagged human EP2 receptor expressed in HEK293 cells assessed as induction of EA-tagged beta-arrestin recruitment incubated for 90 mins by beta-galactosidase reporter gene assay
ChEMBL 409 5 2 6 3.8 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3COc3ccccc3Cl)O2)n1 10.1021/acsmedchemlett.5b00455
72950089 157370 0 None -1621 3 Human 6.7 pEC50 = 6.7 Binding
SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.
ChEMBL 375 13 2 3 3.8 CCCCC[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCCCCC(=O)O nan
CHEMBL3955128 157370 0 None -1621 3 Human 6.7 pEC50 = 6.7 Binding
SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.
ChEMBL 375 13 2 3 3.8 CCCCC[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCCCCC(=O)O nan
66857670 144179 0 None - 1 Human 7.7 pEC50 = 7.7 Binding
Agonist activity at human EP2 receptorAgonist activity at human EP2 receptor
ChEMBL 436 9 2 7 3.3 CC#CCC1([C@H](O)/C=C/[C@H]2COC(=O)N2CCSc2nc(C(=O)O)cs2)CCC1 10.1016/j.bmcl.2015.12.039
CHEMBL3753268 144179 0 None - 1 Human 7.7 pEC50 = 7.7 Binding
Agonist activity at human EP2 receptorAgonist activity at human EP2 receptor
ChEMBL 436 9 2 7 3.3 CC#CCC1([C@H](O)/C=C/[C@H]2COC(=O)N2CCSc2nc(C(=O)O)cs2)CCC1 10.1016/j.bmcl.2015.12.039
57529188 153973 0 None - 1 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulationAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulation
ChEMBL 415 11 2 5 4.3 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)o2)cc1 nan
CHEMBL3928130 153973 0 None - 1 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulationAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulation
ChEMBL 415 11 2 5 4.3 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)o2)cc1 nan
11855866 151380 0 None - 1 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulationAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulation
ChEMBL 403 9 2 5 4.0 CCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3907809 151380 0 None - 1 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulationAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulation
ChEMBL 403 9 2 5 4.0 CCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
11855325 151469 0 None - 1 Human 7.6 pEC50 = 7.6 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 6.0 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 6.0 membranes incubated for 60 mins
ChEMBL 387 6 1 4 4.5 CC(C)(C)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3908484 151469 0 None - 1 Human 7.6 pEC50 = 7.6 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 6.0 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 6.0 membranes incubated for 60 mins
ChEMBL 387 6 1 4 4.5 CC(C)(C)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
11855324 149383 0 None - 1 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulationAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulation
ChEMBL 371 6 1 4 4.0 CC(C)(C)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)o2)cc1 nan
CHEMBL3891401 149383 0 None - 1 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulationAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulation
ChEMBL 371 6 1 4 4.0 CC(C)(C)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)o2)cc1 nan
127026652 144260 0 None - 1 Human 7.5 pEC50 = 7.5 Binding
Agonist activity at human EP2 receptorAgonist activity at human EP2 receptor
ChEMBL 456 12 2 8 3.3 CCOCCC1([C@H](O)/C=C/[C@H]2COC(=O)N2CCSc2nc(C(=O)O)cs2)CCC1 10.1016/j.bmcl.2015.12.039
CHEMBL3753898 144260 0 None - 1 Human 7.5 pEC50 = 7.5 Binding
Agonist activity at human EP2 receptorAgonist activity at human EP2 receptor
ChEMBL 456 12 2 8 3.3 CCOCCC1([C@H](O)/C=C/[C@H]2COC(=O)N2CCSc2nc(C(=O)O)cs2)CCC1 10.1016/j.bmcl.2015.12.039
127026956 146204 0 None - 0 Human 8.4 pEC50 = 8.4 Binding
Agonist activity at human EP2 receptor expressed in HEK293 cells after 24 hrs beta-arrestin recruitment assayAgonist activity at human EP2 receptor expressed in HEK293 cells after 24 hrs beta-arrestin recruitment assay
ChEMBL 477 5 2 6 5.1 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3COc3cc(Cl)c(Cl)cc3Cl)O2)n1 10.1016/j.bmcl.2016.03.110
CHEMBL3793862 146204 0 None - 0 Human 8.4 pEC50 = 8.4 Binding
Agonist activity at human EP2 receptor expressed in HEK293 cells after 24 hrs beta-arrestin recruitment assayAgonist activity at human EP2 receptor expressed in HEK293 cells after 24 hrs beta-arrestin recruitment assay
ChEMBL 477 5 2 6 5.1 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3COc3cc(Cl)c(Cl)cc3Cl)O2)n1 10.1016/j.bmcl.2016.03.110
9807448 209951 0 None 1 4 Human 8.4 pEC50 = 8.4 Binding
Agonist activity at EP2 receptor (unknown origin) by functional assayAgonist activity at EP2 receptor (unknown origin) by functional assay
ChEMBL 398 11 3 3 4.7 CCC1([C@@H](O)C/C=C/[C@H]2[C@H](O)C[C@@H](Cl)[C@@H]2C/C=C\CCCC(=O)O)CCC1 10.1021/jm401431x
CHEMBL64246 209951 0 None 1 4 Human 8.4 pEC50 = 8.4 Binding
Agonist activity at EP2 receptor (unknown origin) by functional assayAgonist activity at EP2 receptor (unknown origin) by functional assay
ChEMBL 398 11 3 3 4.7 CCC1([C@@H](O)C/C=C/[C@H]2[C@H](O)C[C@@H](Cl)[C@@H]2C/C=C\CCCC(=O)O)CCC1 10.1021/jm401431x
11855867 152761 0 None - 1 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulationAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulation
ChEMBL 389 8 2 5 3.6 CCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3918349 152761 0 None - 1 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulationAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulation
ChEMBL 389 8 2 5 3.6 CCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
1892 7534 20 None -2 9 Human 7.5 pEC50 = 7.5 Binding
Agonist activity at EP2 receptor (unknown origin) by functional assayAgonist activity at EP2 receptor (unknown origin) by functional assay
ChEMBL 394 13 3 4 4.3 CCCC1(CCC1)[C@H](C/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 10.1021/jm401431x
25886893 7534 20 None -2 9 Human 7.5 pEC50 = 7.5 Binding
Agonist activity at EP2 receptor (unknown origin) by functional assayAgonist activity at EP2 receptor (unknown origin) by functional assay
ChEMBL 394 13 3 4 4.3 CCCC1(CCC1)[C@H](C/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 10.1021/jm401431x
CHEMBL1628262 7534 20 None -2 9 Human 7.5 pEC50 = 7.5 Binding
Agonist activity at EP2 receptor (unknown origin) by functional assayAgonist activity at EP2 receptor (unknown origin) by functional assay
ChEMBL 394 13 3 4 4.3 CCCC1(CCC1)[C@H](C/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 10.1021/jm401431x
72948663 152512 0 None - 1 Human 6.5 pEC50 = 6.5 Binding
SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.
ChEMBL 415 11 2 4 4.1 CCCCC[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCc1ccc(C(=O)O)s1 nan
CHEMBL3916499 152512 0 None - 1 Human 6.5 pEC50 = 6.5 Binding
SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.
ChEMBL 415 11 2 4 4.1 CCCCC[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCc1ccc(C(=O)O)s1 nan
5311035 104579 29 None -4 9 Human 7.5 pEC50 = 7.5 Binding
Agonist activity at EP2 receptor (unknown origin) by functional assayAgonist activity at EP2 receptor (unknown origin) by functional assay
ChEMBL 408 13 2 5 4.3 CCCC1([C@H](O)C/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2CCCCCCC(=O)OC)CCC1 10.1021/jm401431x
CHEMBL271896 104579 29 None -4 9 Human 7.5 pEC50 = 7.5 Binding
Agonist activity at EP2 receptor (unknown origin) by functional assayAgonist activity at EP2 receptor (unknown origin) by functional assay
ChEMBL 408 13 2 5 4.3 CCCC1([C@H](O)C/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2CCCCCCC(=O)OC)CCC1 10.1021/jm401431x
1883 9856 75 None -6 24 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at PK2-tagged human EP2 receptor expressed in HEK293 cells assessed as induction of EA-tagged beta-arrestin recruitment incubated for 90 mins by beta-galactosidase reporter gene assayAgonist activity at PK2-tagged human EP2 receptor expressed in HEK293 cells assessed as induction of EA-tagged beta-arrestin recruitment incubated for 90 mins by beta-galactosidase reporter gene assay
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/acsmedchemlett.5b00455
1916 9856 75 None -6 24 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at PK2-tagged human EP2 receptor expressed in HEK293 cells assessed as induction of EA-tagged beta-arrestin recruitment incubated for 90 mins by beta-galactosidase reporter gene assayAgonist activity at PK2-tagged human EP2 receptor expressed in HEK293 cells assessed as induction of EA-tagged beta-arrestin recruitment incubated for 90 mins by beta-galactosidase reporter gene assay
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/acsmedchemlett.5b00455
5280360 9856 75 None -6 24 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at PK2-tagged human EP2 receptor expressed in HEK293 cells assessed as induction of EA-tagged beta-arrestin recruitment incubated for 90 mins by beta-galactosidase reporter gene assayAgonist activity at PK2-tagged human EP2 receptor expressed in HEK293 cells assessed as induction of EA-tagged beta-arrestin recruitment incubated for 90 mins by beta-galactosidase reporter gene assay
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/acsmedchemlett.5b00455
913 9856 75 None -6 24 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at PK2-tagged human EP2 receptor expressed in HEK293 cells assessed as induction of EA-tagged beta-arrestin recruitment incubated for 90 mins by beta-galactosidase reporter gene assayAgonist activity at PK2-tagged human EP2 receptor expressed in HEK293 cells assessed as induction of EA-tagged beta-arrestin recruitment incubated for 90 mins by beta-galactosidase reporter gene assay
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/acsmedchemlett.5b00455
CHEMBL548 9856 75 None -6 24 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at PK2-tagged human EP2 receptor expressed in HEK293 cells assessed as induction of EA-tagged beta-arrestin recruitment incubated for 90 mins by beta-galactosidase reporter gene assayAgonist activity at PK2-tagged human EP2 receptor expressed in HEK293 cells assessed as induction of EA-tagged beta-arrestin recruitment incubated for 90 mins by beta-galactosidase reporter gene assay
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/acsmedchemlett.5b00455
DB00917 9856 75 None -6 24 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at PK2-tagged human EP2 receptor expressed in HEK293 cells assessed as induction of EA-tagged beta-arrestin recruitment incubated for 90 mins by beta-galactosidase reporter gene assayAgonist activity at PK2-tagged human EP2 receptor expressed in HEK293 cells assessed as induction of EA-tagged beta-arrestin recruitment incubated for 90 mins by beta-galactosidase reporter gene assay
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/acsmedchemlett.5b00455
66857738 144078 0 None - 1 Human 5.4 pEC50 = 5.4 Binding
Agonist activity at human EP2 receptorAgonist activity at human EP2 receptor
ChEMBL 468 10 2 7 4.7 CC(C)(C)CCC1([C@H](O)/C=C/[C@H]2COC(=O)N2CCSc2nc(C(=O)O)cs2)CCC1 10.1016/j.bmcl.2015.12.039
CHEMBL3752435 144078 0 None - 1 Human 5.4 pEC50 = 5.4 Binding
Agonist activity at human EP2 receptorAgonist activity at human EP2 receptor
ChEMBL 468 10 2 7 4.7 CC(C)(C)CCC1([C@H](O)/C=C/[C@H]2COC(=O)N2CCSc2nc(C(=O)O)cs2)CCC1 10.1016/j.bmcl.2015.12.039
127050451 146999 0 None - 0 Human 5.4 pEC50 = 5.4 Binding
Agonist activity at PK2-tagged human EP2 receptor expressed in HEK293 cells assessed as induction of EA-tagged beta-arrestin recruitment incubated for 90 mins by beta-galactosidase reporter gene assayAgonist activity at PK2-tagged human EP2 receptor expressed in HEK293 cells assessed as induction of EA-tagged beta-arrestin recruitment incubated for 90 mins by beta-galactosidase reporter gene assay
ChEMBL 459 6 2 7 4.0 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3COc3ccc(OC(F)(F)F)cc3)O2)n1 10.1021/acsmedchemlett.5b00455
CHEMBL3805122 146999 0 None - 0 Human 5.4 pEC50 = 5.4 Binding
Agonist activity at PK2-tagged human EP2 receptor expressed in HEK293 cells assessed as induction of EA-tagged beta-arrestin recruitment incubated for 90 mins by beta-galactosidase reporter gene assayAgonist activity at PK2-tagged human EP2 receptor expressed in HEK293 cells assessed as induction of EA-tagged beta-arrestin recruitment incubated for 90 mins by beta-galactosidase reporter gene assay
ChEMBL 459 6 2 7 4.0 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3COc3ccc(OC(F)(F)F)cc3)O2)n1 10.1021/acsmedchemlett.5b00455
1929 8386 55 None -11 2 Human 8.3 pEC50 = 8.3 Binding
Agonist activity at EP2 receptor (unknown origin) by functional assayAgonist activity at EP2 receptor (unknown origin) by functional assay
ChEMBL 468 9 1 5 4.2 OC(=O)COc1cccc(c1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)C(C)(C)C 10.1021/jm401431x
9890801 8386 55 None -11 2 Human 8.3 pEC50 = 8.3 Binding
Agonist activity at EP2 receptor (unknown origin) by functional assayAgonist activity at EP2 receptor (unknown origin) by functional assay
ChEMBL 468 9 1 5 4.2 OC(=O)COc1cccc(c1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)C(C)(C)C 10.1021/jm401431x
CHEMBL563646 8386 55 None -11 2 Human 8.3 pEC50 = 8.3 Binding
Agonist activity at EP2 receptor (unknown origin) by functional assayAgonist activity at EP2 receptor (unknown origin) by functional assay
ChEMBL 468 9 1 5 4.2 OC(=O)COc1cccc(c1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)C(C)(C)C 10.1021/jm401431x
DB12022 8386 55 None -11 2 Human 8.3 pEC50 = 8.3 Binding
Agonist activity at EP2 receptor (unknown origin) by functional assayAgonist activity at EP2 receptor (unknown origin) by functional assay
ChEMBL 468 9 1 5 4.2 OC(=O)COc1cccc(c1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)C(C)(C)C 10.1021/jm401431x
11362836 144074 0 None - 1 Human 8.2 pEC50 = 8.2 Binding
Agonist activity at human EP2 receptorAgonist activity at human EP2 receptor
ChEMBL 446 12 2 7 3.8 CC(C)(CCCCF)[C@H](O)/C=C/[C@H]1COC(=O)N1CCSc1nc(C(=O)O)cs1 10.1016/j.bmcl.2015.12.039
CHEMBL3752406 144074 0 None - 1 Human 8.2 pEC50 = 8.2 Binding
Agonist activity at human EP2 receptorAgonist activity at human EP2 receptor
ChEMBL 446 12 2 7 3.8 CC(C)(CCCCF)[C@H](O)/C=C/[C@H]1COC(=O)N1CCSc1nc(C(=O)O)cs1 10.1016/j.bmcl.2015.12.039
11855325 151469 0 None - 1 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulationAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulation
ChEMBL 387 6 1 4 4.5 CC(C)(C)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3908484 151469 0 None - 1 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulationAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulation
ChEMBL 387 6 1 4 4.5 CC(C)(C)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
11855593 153612 0 None - 0 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulationAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulation
ChEMBL 425 11 2 4 4.7 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2cccc(C(=O)O)c2)cc1 nan
CHEMBL3924987 153612 0 None - 0 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulationAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulation
ChEMBL 425 11 2 4 4.7 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2cccc(C(=O)O)c2)cc1 nan
11855588 154135 0 None - 0 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulationAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulation
ChEMBL 345 8 1 2 4.9 CC(C)(C)c1ccc(N2C(=O)CC[C@@H]2CCCCCCC(=O)O)cc1 nan
CHEMBL3929446 154135 0 None - 0 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulationAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulation
ChEMBL 345 8 1 2 4.9 CC(C)(C)c1ccc(N2C(=O)CC[C@@H]2CCCCCCC(=O)O)cc1 nan
5283086 210089 24 None - 5 Human 7.2 pEC50 = 7.2 Binding
SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](O)/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O nan
CHEMBL64804 210089 24 None - 5 Human 7.2 pEC50 = 7.2 Binding
SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](O)/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O nan
11156167 144298 0 None - 1 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at human EP2 receptorAgonist activity at human EP2 receptor
ChEMBL 494 11 2 7 5.2 O=C(O)c1csc(SCCN2C(=O)OC[C@@H]2/C=C/[C@@H](O)C2(CCC3CCCCC3)CCC2)n1 10.1016/j.bmcl.2015.12.039
CHEMBL3754197 144298 0 None - 1 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at human EP2 receptorAgonist activity at human EP2 receptor
ChEMBL 494 11 2 7 5.2 O=C(O)c1csc(SCCN2C(=O)OC[C@@H]2/C=C/[C@@H](O)C2(CCC3CCCCC3)CCC2)n1 10.1016/j.bmcl.2015.12.039
90054537 155182 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.
ChEMBL 491 12 2 4 5.2 C[C@@H](CCCc1ccccc1)[C@@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCc1ccc(C(=O)O)s1 nan
CHEMBL3937596 155182 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.
ChEMBL 491 12 2 4 5.2 C[C@@H](CCCc1ccccc1)[C@@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCc1ccc(C(=O)O)s1 nan
127051656 147072 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at PK2-tagged human EP2 receptor expressed in HEK293 cells assessed as induction of EA-tagged beta-arrestin recruitment incubated for 90 mins by beta-galactosidase reporter gene assayAgonist activity at PK2-tagged human EP2 receptor expressed in HEK293 cells assessed as induction of EA-tagged beta-arrestin recruitment incubated for 90 mins by beta-galactosidase reporter gene assay
ChEMBL 459 6 2 7 4.0 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3COc3cccc(OC(F)(F)F)c3)O2)n1 10.1021/acsmedchemlett.5b00455
CHEMBL3805981 147072 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at PK2-tagged human EP2 receptor expressed in HEK293 cells assessed as induction of EA-tagged beta-arrestin recruitment incubated for 90 mins by beta-galactosidase reporter gene assayAgonist activity at PK2-tagged human EP2 receptor expressed in HEK293 cells assessed as induction of EA-tagged beta-arrestin recruitment incubated for 90 mins by beta-galactosidase reporter gene assay
ChEMBL 459 6 2 7 4.0 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3COc3cccc(OC(F)(F)F)c3)O2)n1 10.1021/acsmedchemlett.5b00455
59554824 144253 0 None - 1 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at human EP2 receptorAgonist activity at human EP2 receptor
ChEMBL 428 11 2 7 3.9 CCCCC(C)(C)[C@H](O)/C=C/[C@H]1COC(=O)N1CCSc1nc(C(=O)O)cs1 10.1016/j.bmcl.2015.12.039
CHEMBL3753853 144253 0 None - 1 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at human EP2 receptorAgonist activity at human EP2 receptor
ChEMBL 428 11 2 7 3.9 CCCCC(C)(C)[C@H](O)/C=C/[C@H]1COC(=O)N1CCSc1nc(C(=O)O)cs1 10.1016/j.bmcl.2015.12.039
90054519 158765 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.
ChEMBL 477 11 2 4 4.8 C[C@@H](CCc1ccccc1)[C@@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCc1ccc(C(=O)O)s1 nan
CHEMBL3966743 158765 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.
ChEMBL 477 11 2 4 4.8 C[C@@H](CCc1ccccc1)[C@@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCc1ccc(C(=O)O)s1 nan
72948294 156736 0 None - 1 Human 6.1 pEC50 = 6.1 Binding
SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.
ChEMBL 439 9 2 4 4.0 CCC#CC[C@H](C)[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCc1ccc(C(=O)O)s1 nan
CHEMBL3949856 156736 0 None - 1 Human 6.1 pEC50 = 6.1 Binding
SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.
ChEMBL 439 9 2 4 4.0 CCC#CC[C@H](C)[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCc1ccc(C(=O)O)s1 nan
90054392 149696 0 None - 0 Human 4.1 pEC50 = 4.1 Binding
SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.
ChEMBL 519 14 2 4 6.0 C[C@@H](CCCCCc1ccccc1)[C@@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCc1ccc(C(=O)O)s1 nan
CHEMBL3893847 149696 0 None - 0 Human 4.1 pEC50 = 4.1 Binding
SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.
ChEMBL 519 14 2 4 6.0 C[C@@H](CCCCCc1ccccc1)[C@@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCc1ccc(C(=O)O)s1 nan
11855871 153186 0 None - 1 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulationAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulation
ChEMBL 429 11 1 5 4.9 CCCCCC(=O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3921784 153186 0 None - 1 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulationAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulation
ChEMBL 429 11 1 5 4.9 CCCCCC(=O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
11855594 159759 0 None - 1 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulationAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulation
ChEMBL 417 10 2 5 4.4 CCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3975238 159759 0 None - 1 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulationAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulation
ChEMBL 417 10 2 5 4.4 CCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
127027874 146141 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at PK2-tagged human EP2 receptor expressed in HEK293 cells assessed as induction of EA-tagged beta-arrestin recruitment incubated for 90 mins by beta-galactosidase reporter gene assayAgonist activity at PK2-tagged human EP2 receptor expressed in HEK293 cells assessed as induction of EA-tagged beta-arrestin recruitment incubated for 90 mins by beta-galactosidase reporter gene assay
ChEMBL 443 5 2 6 4.2 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3COc3cccc(C(F)(F)F)c3)O2)n1 10.1021/acsmedchemlett.5b00455
CHEMBL3793045 146141 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at PK2-tagged human EP2 receptor expressed in HEK293 cells assessed as induction of EA-tagged beta-arrestin recruitment incubated for 90 mins by beta-galactosidase reporter gene assayAgonist activity at PK2-tagged human EP2 receptor expressed in HEK293 cells assessed as induction of EA-tagged beta-arrestin recruitment incubated for 90 mins by beta-galactosidase reporter gene assay
ChEMBL 443 5 2 6 4.2 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3COc3cccc(C(F)(F)F)c3)O2)n1 10.1021/acsmedchemlett.5b00455
127027874 146141 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at human EP2 receptor expressed in HEK293 cells after 24 hrs beta-arrestin recruitment assayAgonist activity at human EP2 receptor expressed in HEK293 cells after 24 hrs beta-arrestin recruitment assay
ChEMBL 443 5 2 6 4.2 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3COc3cccc(C(F)(F)F)c3)O2)n1 10.1016/j.bmcl.2016.03.110
CHEMBL3793045 146141 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at human EP2 receptor expressed in HEK293 cells after 24 hrs beta-arrestin recruitment assayAgonist activity at human EP2 receptor expressed in HEK293 cells after 24 hrs beta-arrestin recruitment assay
ChEMBL 443 5 2 6 4.2 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3COc3cccc(C(F)(F)F)c3)O2)n1 10.1016/j.bmcl.2016.03.110
10339756 149863 0 None - 0 Human 6.0 pEC50 = 6.0 Binding
Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.
ChEMBL 380 12 3 4 3.9 CCCCC[C@H](O)/C=C/[C@H]1[C@H](O)C(C)(C)C(=O)[C@@H]1C/C=C\CCCC(=O)O nan
CHEMBL3895324 149863 0 None - 0 Human 6.0 pEC50 = 6.0 Binding
Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.
ChEMBL 380 12 3 4 3.9 CCCCC[C@H](O)/C=C/[C@H]1[C@H](O)C(C)(C)C(=O)[C@@H]1C/C=C\CCCC(=O)O nan
118689427 158631 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10N HCl is added to achieve a pH of 7.4). The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 °C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H−] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations were for 60 min at 25 °C. and were terminated by the addition of 4 ml of ice-cold 50 mM TRIS-HCl, followed by rapid filtration through Whatman GF/B filters and three additional 4 ml washes in a cell harvester (Brandel). Competition studies were performed using a final concentration of 5 nM [3H]-PGE2, or 5 nM [3H] 17-phenyl PGF2a and non-specific binding determined with 10^−5M of unlabeled PGE2, or 17-phenyl PGF2a, according to receptor subtype studied.Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10N HCl is added to achieve a pH of 7.4). The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 °C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H−] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations were for 60 min at 25 °C. and were terminated by the addition of 4 ml of ice-cold 50 mM TRIS-HCl, followed by rapid filtration through Whatman GF/B filters and three additional 4 ml washes in a cell harvester (Brandel). Competition studies were performed using a final concentration of 5 nM [3H]-PGE2, or 5 nM [3H] 17-phenyl PGF2a and non-specific binding determined with 10^−5M of unlabeled PGE2, or 17-phenyl PGF2a, according to receptor subtype studied.
ChEMBL 519 10 2 6 3.8 O=C(O)c1ccc(CCCN2[C@@H](/C=C/C(O)Cc3cccc(OC(F)(F)F)c3)CCS2(=O)=O)s1 nan
CHEMBL3965497 158631 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10N HCl is added to achieve a pH of 7.4). The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 °C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H−] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations were for 60 min at 25 °C. and were terminated by the addition of 4 ml of ice-cold 50 mM TRIS-HCl, followed by rapid filtration through Whatman GF/B filters and three additional 4 ml washes in a cell harvester (Brandel). Competition studies were performed using a final concentration of 5 nM [3H]-PGE2, or 5 nM [3H] 17-phenyl PGF2a and non-specific binding determined with 10^−5M of unlabeled PGE2, or 17-phenyl PGF2a, according to receptor subtype studied.Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10N HCl is added to achieve a pH of 7.4). The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 °C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H−] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations were for 60 min at 25 °C. and were terminated by the addition of 4 ml of ice-cold 50 mM TRIS-HCl, followed by rapid filtration through Whatman GF/B filters and three additional 4 ml washes in a cell harvester (Brandel). Competition studies were performed using a final concentration of 5 nM [3H]-PGE2, or 5 nM [3H] 17-phenyl PGF2a and non-specific binding determined with 10^−5M of unlabeled PGE2, or 17-phenyl PGF2a, according to receptor subtype studied.
ChEMBL 519 10 2 6 3.8 O=C(O)c1ccc(CCCN2[C@@H](/C=C/C(O)Cc3cccc(OC(F)(F)F)c3)CCS2(=O)=O)s1 nan
56927669 128423 0 None - 0 Mouse 8.0 pIC50 = 8 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from mouse EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 423 3 1 4 4.5 O=c1cc(CN2CCOc3c(Cl)cc(-n4ccc5cc(F)ccc54)cc3C2)cc[nH]1 10.1021/acs.jmedchem.5b00567
CHEMBL3586360 128423 0 None - 0 Mouse 8.0 pIC50 = 8 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from mouse EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 423 3 1 4 4.5 O=c1cc(CN2CCOc3c(Cl)cc(-n4ccc5cc(F)ccc54)cc3C2)cc[nH]1 10.1021/acs.jmedchem.5b00567
56927669 128423 0 None - 0 Rat 8.0 pIC50 = 8 Binding
Displacement of [3H]-PGE2 from rat EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from rat EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 423 3 1 4 4.5 O=c1cc(CN2CCOc3c(Cl)cc(-n4ccc5cc(F)ccc54)cc3C2)cc[nH]1 10.1021/acs.jmedchem.5b00567
CHEMBL3586360 128423 0 None - 0 Rat 8.0 pIC50 = 8 Binding
Displacement of [3H]-PGE2 from rat EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from rat EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 423 3 1 4 4.5 O=c1cc(CN2CCOc3c(Cl)cc(-n4ccc5cc(F)ccc54)cc3C2)cc[nH]1 10.1021/acs.jmedchem.5b00567
10315 9700 28 None - 1 Human 8.0 pIC50 = 8 Binding
Displacement of [3H]prostaglandin E2 from human EP2 receptor expressed in HEK293 cell membranes after 60 mins by liquid scintillation countingDisplacement of [3H]prostaglandin E2 from human EP2 receptor expressed in HEK293 cell membranes after 60 mins by liquid scintillation counting
ChEMBL 478 10 2 8 2.6 OC(=O)CNc1cccc(n1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)n1cccn1 10.1021/acs.jmedchem.8b00808
44230575 9700 28 None - 1 Human 8.0 pIC50 = 8 Binding
Displacement of [3H]prostaglandin E2 from human EP2 receptor expressed in HEK293 cell membranes after 60 mins by liquid scintillation countingDisplacement of [3H]prostaglandin E2 from human EP2 receptor expressed in HEK293 cell membranes after 60 mins by liquid scintillation counting
ChEMBL 478 10 2 8 2.6 OC(=O)CNc1cccc(n1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)n1cccn1 10.1021/acs.jmedchem.8b00808
CHEMBL3707245 9700 28 None - 1 Human 8.0 pIC50 = 8 Binding
Displacement of [3H]prostaglandin E2 from human EP2 receptor expressed in HEK293 cell membranes after 60 mins by liquid scintillation countingDisplacement of [3H]prostaglandin E2 from human EP2 receptor expressed in HEK293 cell membranes after 60 mins by liquid scintillation counting
ChEMBL 478 10 2 8 2.6 OC(=O)CNc1cccc(n1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)n1cccn1 10.1021/acs.jmedchem.8b00808
122180251 128381 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 432 5 0 6 5.4 COc1ccc(CN2CCOc3c(cc(-c4csc5ccccc45)cc3OC)C2)cn1 10.1021/acs.jmedchem.5b00567
CHEMBL3586314 128381 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 432 5 0 6 5.4 COc1ccc(CN2CCOc3c(cc(-c4csc5ccccc45)cc3OC)C2)cn1 10.1021/acs.jmedchem.5b00567
122180259 128389 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 479 5 0 6 5.4 COc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1ccc(S(C)(=O)=O)cc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586322 128389 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 479 5 0 6 5.4 COc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1ccc(S(C)(=O)=O)cc1)C2 10.1021/acs.jmedchem.5b00567
122180261 128391 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 426 4 0 5 5.8 COc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1cccc(C#N)c1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586324 128391 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 426 4 0 5 5.8 COc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1cccc(C#N)c1)C2 10.1021/acs.jmedchem.5b00567
122180282 128409 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 410 4 0 6 4.3 COc1cc(-n2ccc3cc(C#N)ccc32)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586345 128409 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 410 4 0 6 4.3 COc1cc(-n2ccc3cc(C#N)ccc32)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
30897313 128376 0 None - 0 Mouse 7.0 pIC50 = 7 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from mouse EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 402 4 0 5 5.4 COc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586309 128376 0 None - 0 Mouse 7.0 pIC50 = 7 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from mouse EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 402 4 0 5 5.4 COc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
30897313 128376 0 None - 0 Rat 7.0 pIC50 = 7 Binding
Displacement of [3H]-PGE2 from rat EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from rat EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 402 4 0 5 5.4 COc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586309 128376 0 None - 0 Rat 7.0 pIC50 = 7 Binding
Displacement of [3H]-PGE2 from rat EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from rat EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 402 4 0 5 5.4 COc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
122180253 128383 0 None - 0 Human 5.0 pIC50 = 5 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 401 4 0 4 6.0 COc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1ccccc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586316 128383 0 None - 0 Human 5.0 pIC50 = 5 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 401 4 0 4 6.0 COc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1ccccc1)C2 10.1021/acs.jmedchem.5b00567
122180271 128398 0 None - 0 Human 5.0 pIC50 = 5 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 380 4 0 4 4.8 COc1cc(-c2ccc(Cl)cc2)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586334 128398 0 None - 0 Human 5.0 pIC50 = 5 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 380 4 0 4 4.8 COc1cc(-c2ccc(Cl)cc2)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
44564990 199429 0 None - 0 Human 5.0 pIC50 = 5 Binding
Displacement of radioligand from EP2 receptorDisplacement of radioligand from EP2 receptor
ChEMBL 538 6 1 5 5.7 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2cc(F)c(F)cc2F)c2c(Oc3ccc(Cl)c(F)c3)cccc21 10.1016/j.bmcl.2008.12.112
CHEMBL521777 199429 0 None - 0 Human 5.0 pIC50 = 5 Binding
Displacement of radioligand from EP2 receptorDisplacement of radioligand from EP2 receptor
ChEMBL 538 6 1 5 5.7 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2cc(F)c(F)cc2F)c2c(Oc3ccc(Cl)c(F)c3)cccc21 10.1016/j.bmcl.2008.12.112
122180276 128403 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 399 4 0 5 4.6 COc1cc(-c2cn(C)c3ccccc23)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586339 128403 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 399 4 0 5 4.6 COc1cc(-c2cn(C)c3ccccc23)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
122180285 128412 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 372 3 0 4 5.4 c1cncc(CN2CCOc3ccc(-c4csc5ccccc45)cc3C2)c1 10.1021/acs.jmedchem.5b00567
CHEMBL3586348 128412 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 372 3 0 4 5.4 c1cncc(CN2CCOc3ccc(-c4csc5ccccc45)cc3C2)c1 10.1021/acs.jmedchem.5b00567
44409693 172877 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Binding affinity to rat EP2 receptor expressed in HEK293 cellsBinding affinity to rat EP2 receptor expressed in HEK293 cells
ChEMBL 429 11 2 4 4.3 CCc1ccc(CC(O)CC[C@H]2CCC(=O)N2CCCc2ccc(C(=O)O)s2)cc1 10.1016/j.bmcl.2006.01.018
CHEMBL425950 172877 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Binding affinity to rat EP2 receptor expressed in HEK293 cellsBinding affinity to rat EP2 receptor expressed in HEK293 cells
ChEMBL 429 11 2 4 4.3 CCc1ccc(CC(O)CC[C@H]2CCC(=O)N2CCCc2ccc(C(=O)O)s2)cc1 10.1016/j.bmcl.2006.01.018
122180269 128396 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 380 4 0 4 4.8 COc1cc(-c2ccccc2Cl)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586332 128396 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 380 4 0 4 4.8 COc1cc(-c2ccccc2Cl)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
44409907 83825 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Binding affinity to rat EP2 receptor expressed in HEK293 cellsBinding affinity to rat EP2 receptor expressed in HEK293 cells
ChEMBL 419 10 2 4 3.9 O=C(O)c1ccc(CCCN2C(=O)CC[C@@H]2CC[C@@H](O)Cc2ccc(F)cc2)s1 10.1016/j.bmcl.2006.01.018
CHEMBL207237 83825 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Binding affinity to rat EP2 receptor expressed in HEK293 cellsBinding affinity to rat EP2 receptor expressed in HEK293 cells
ChEMBL 419 10 2 4 3.9 O=C(O)c1ccc(CCCN2C(=O)CC[C@@H]2CC[C@@H](O)Cc2ccc(F)cc2)s1 10.1016/j.bmcl.2006.01.018
44570000 185429 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Displacement of [3H]PGE2 from human EP2 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP2 receptor after 1 hr by liquid scintillation counting
ChEMBL 544 7 2 5 6.2 O=C(COc1cccc2[nH]cc(Cc3ccc4ccccc4c3)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1021/jm9005912
CHEMBL467632 185429 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Displacement of [3H]PGE2 from human EP2 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP2 receptor after 1 hr by liquid scintillation counting
ChEMBL 544 7 2 5 6.2 O=C(COc1cccc2[nH]cc(Cc3ccc4ccccc4c3)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1021/jm9005912
44409739 146438 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Binding affinity to rat EP2 receptor expressed in HEK293 cellsBinding affinity to rat EP2 receptor expressed in HEK293 cells
ChEMBL 477 11 2 4 5.4 O=C(O)c1ccc(CCCN2C(=O)CC[C@@H]2CCC(O)Cc2ccccc2-c2ccccc2)s1 10.1016/j.bmcl.2006.01.018
CHEMBL379785 146438 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Binding affinity to rat EP2 receptor expressed in HEK293 cellsBinding affinity to rat EP2 receptor expressed in HEK293 cells
ChEMBL 477 11 2 4 5.4 O=C(O)c1ccc(CCCN2C(=O)CC[C@@H]2CCC(O)Cc2ccccc2-c2ccccc2)s1 10.1016/j.bmcl.2006.01.018
44157014 199396 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Displacement of radioligand from EP2 receptorDisplacement of radioligand from EP2 receptor
ChEMBL 518 6 1 5 5.9 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2ccc(F)c(F)c2)c2c(Oc3ccc4ccccc4c3)cccc21 10.1016/j.bmcl.2008.12.112
CHEMBL521609 199396 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Displacement of radioligand from EP2 receptorDisplacement of radioligand from EP2 receptor
ChEMBL 518 6 1 5 5.9 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2ccc(F)c(F)c2)c2c(Oc3ccc4ccccc4c3)cccc21 10.1016/j.bmcl.2008.12.112
58905349 163057 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Antagonist activity at human EP2 receptorAntagonist activity at human EP2 receptor
ChEMBL 400 6 2 4 4.3 O=C(O)c1ccc(CNC(=O)c2cc(Cl)cnc2Oc2ccc(F)cc2)cc1 10.1016/j.bmcl.2017.01.067
CHEMBL4065183 163057 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Antagonist activity at human EP2 receptorAntagonist activity at human EP2 receptor
ChEMBL 400 6 2 4 4.3 O=C(O)c1ccc(CNC(=O)c2cc(Cl)cnc2Oc2ccc(F)cc2)cc1 10.1016/j.bmcl.2017.01.067
CHEMBL4552554 220780 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Affinity Biochemical interaction (Enzymatic inhibition assay) EUB0000342a PTGER2Affinity Biochemical interaction (Enzymatic inhibition assay) EUB0000342a PTGER2
ChEMBL None None None O=C(c1ccc(F)cc1)N1CC(COc2ccc(Br)cc2)(C(=O)O)C1 10.6019/CHEMBL5210307
10047541 139288 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Affinity for Prostanoid EP2 receptor expressed in CHO cellsAffinity for Prostanoid EP2 receptor expressed in CHO cells
ChEMBL 416 13 4 6 3.8 O=C(O)CCCCCC[C@H]1[C@@H](O)C[C@@H](O)[C@@H]1CCC(O)CSc1cccs1 10.1021/jm990542v
CHEMBL369797 139288 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Affinity for Prostanoid EP2 receptor expressed in CHO cellsAffinity for Prostanoid EP2 receptor expressed in CHO cells
ChEMBL 416 13 4 6 3.8 O=C(O)CCCCCC[C@H]1[C@@H](O)C[C@@H](O)[C@@H]1CCC(O)CSc1cccs1 10.1021/jm990542v
122180293 128421 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 416 4 0 5 4.9 COc1cc(-c2csc3ccccc23)cc2c1OCC(=O)N(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586357 128421 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 416 4 0 5 4.9 COc1cc(-c2csc3ccccc23)cc2c1OCC(=O)N(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
11955294 151546 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 380 8 3 3 4.2 O=C(O)CCCCCC[C@@H]1[C@@H](c2ccc3c(c2)CCC3O)[C@H](O)C[C@H]1Cl nan
CHEMBL3909111 151546 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 380 8 3 3 4.2 O=C(O)CCCCCC[C@@H]1[C@@H](c2ccc3c(c2)CCC3O)[C@H](O)C[C@H]1Cl nan
11955240 154768 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 352 8 3 3 3.5 O=C(O)CCC/C=C\C[C@@H]1[C@@H](c2ccc(CO)cc2)[C@H](O)C[C@H]1Cl nan
CHEMBL3934202 154768 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 352 8 3 3 3.5 O=C(O)CCC/C=C\C[C@@H]1[C@@H](c2ccc(CO)cc2)[C@H](O)C[C@H]1Cl nan
44409910 147687 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Binding affinity to rat EP2 receptor expressed in HEK293 cellsBinding affinity to rat EP2 receptor expressed in HEK293 cells
ChEMBL 477 11 2 4 5.4 O=C(O)c1ccc(CCCN2C(=O)CC[C@@H]2CCC(O)Cc2cccc(-c3ccccc3)c2)s1 10.1016/j.bmcl.2006.01.018
CHEMBL382197 147687 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Binding affinity to rat EP2 receptor expressed in HEK293 cellsBinding affinity to rat EP2 receptor expressed in HEK293 cells
ChEMBL 477 11 2 4 5.4 O=C(O)c1ccc(CCCN2C(=O)CC[C@@H]2CCC(O)Cc2cccc(-c3ccccc3)c2)s1 10.1016/j.bmcl.2006.01.018
25195248 189714 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Binding affinity to human EP2 receptor by radioligand binding assayBinding affinity to human EP2 receptor by radioligand binding assay
ChEMBL 540 6 1 4 4.6 CC12CCCC(/C=C/C(=O)NS(=O)(=O)c3cc(F)c(F)cc3F)=C1N(Cc1ccc(F)c(F)c1)C(=O)C2 10.1016/j.bmcl.2008.12.027
CHEMBL479263 189714 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Binding affinity to human EP2 receptor by radioligand binding assayBinding affinity to human EP2 receptor by radioligand binding assay
ChEMBL 540 6 1 4 4.6 CC12CCCC(/C=C/C(=O)NS(=O)(=O)c3cc(F)c(F)cc3F)=C1N(Cc1ccc(F)c(F)c1)C(=O)C2 10.1016/j.bmcl.2008.12.027
118756024 128415 4 None - 0 Human 4.9 pIC50 = 4.9 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 416 5 0 5 5.8 CCOc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586350 128415 4 None - 0 Human 4.9 pIC50 = 4.9 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 416 5 0 5 5.8 CCOc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
122180286 128413 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 388 3 1 5 5.1 Oc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586349 128413 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 388 3 1 5 5.1 Oc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
10339756 149863 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.
ChEMBL 380 12 3 4 3.9 CCCCC[C@H](O)/C=C/[C@H]1[C@H](O)C(C)(C)C(=O)[C@@H]1C/C=C\CCCC(=O)O nan
CHEMBL3895324 149863 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.
ChEMBL 380 12 3 4 3.9 CCCCC[C@H](O)/C=C/[C@H]1[C@H](O)C(C)(C)C(=O)[C@@H]1C/C=C\CCCC(=O)O nan
122180264 128393 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 346 4 0 4 4.2 COc1cc(-c2ccccc2)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586327 128393 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 346 4 0 4 4.2 COc1cc(-c2ccccc2)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
122180267 128395 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 360 4 0 4 4.5 COc1cc(-c2cccc(C)c2)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586330 128395 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 360 4 0 4 4.5 COc1cc(-c2cccc(C)c2)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
11955255 153035 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 408 8 3 3 5.0 CC(C)(C)C(O)c1ccc([C@H]2[C@H](O)C[C@@H](Cl)[C@@H]2C/C=C\CCCC(=O)O)cc1 nan
CHEMBL3920560 153035 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 408 8 3 3 5.0 CC(C)(C)C(O)c1ccc([C@H]2[C@H](O)C[C@@H](Cl)[C@@H]2C/C=C\CCCC(=O)O)cc1 nan
11495634 21677 13 None - 4 Human 5.8 pIC50 = 5.8 Binding
Inhibition of EP2 receptorInhibition of EP2 receptor
ChEMBL 405 6 1 3 5.4 O=C(O)c1cccc(Cc2cc(Cl)ccc2OCc2ccc(Cl)cc2F)n1 10.1016/j.bmcl.2009.02.112
CHEMBL1207972 21677 13 None - 4 Human 5.8 pIC50 = 5.8 Binding
Inhibition of EP2 receptorInhibition of EP2 receptor
ChEMBL 405 6 1 3 5.4 O=C(O)c1cccc(Cc2cc(Cl)ccc2OCc2ccc(Cl)cc2F)n1 10.1016/j.bmcl.2009.02.112
CHEMBL467114 21677 13 None - 4 Human 5.8 pIC50 = 5.8 Binding
Inhibition of EP2 receptorInhibition of EP2 receptor
ChEMBL 405 6 1 3 5.4 O=C(O)c1cccc(Cc2cc(Cl)ccc2OCc2ccc(Cl)cc2F)n1 10.1016/j.bmcl.2009.02.112
9820676 201824 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
ChEMBL 369 13 1 3 3.8 CCCCc1ccc(CN(CCCCCCC(=O)O)S(C)(=O)=O)cc1 10.1016/j.bmcl.2009.01.059
CHEMBL549461 201824 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
ChEMBL 369 13 1 3 3.8 CCCCc1ccc(CN(CCCCCCC(=O)O)S(C)(=O)=O)cc1 10.1016/j.bmcl.2009.01.059
122180290 128418 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 370 3 0 3 5.9 c1cncc(CN2CCCc3ccc(-c4csc5ccccc45)cc3C2)c1 10.1021/acs.jmedchem.5b00567
CHEMBL3586354 128418 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 370 3 0 3 5.9 c1cncc(CN2CCCc3ccc(-c4csc5ccccc45)cc3C2)c1 10.1021/acs.jmedchem.5b00567
11575201 164201 0 None - 1 Human 5.8 pIC50 = 5.8 Binding
Antagonist activity at human EP2 receptorAntagonist activity at human EP2 receptor
ChEMBL 413 6 2 3 5.5 C[C@H](NC(=O)c1cc(Cl)ccc1Oc1cccc(F)c1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2017.01.067
CHEMBL4078648 164201 0 None - 1 Human 5.8 pIC50 = 5.8 Binding
Antagonist activity at human EP2 receptorAntagonist activity at human EP2 receptor
ChEMBL 413 6 2 3 5.5 C[C@H](NC(=O)c1cc(Cl)ccc1Oc1cccc(F)c1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2017.01.067
72695027 113043 0 None -28 2 Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]-PGE2 from human EP2 receptor by liquid scintillation counting analysisDisplacement of [3H]-PGE2 from human EP2 receptor by liquid scintillation counting analysis
ChEMBL 396 8 2 4 3.5 C[C@H](NC(=O)[C@H]1CCCCN1CCOc1ccccc1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2015.05.091
CHEMBL3115074 113043 0 None -28 2 Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]-PGE2 from human EP2 receptor by liquid scintillation counting analysisDisplacement of [3H]-PGE2 from human EP2 receptor by liquid scintillation counting analysis
ChEMBL 396 8 2 4 3.5 C[C@H](NC(=O)[C@H]1CCCCN1CCOc1ccccc1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2015.05.091
CHEMBL3138992 113043 0 None -28 2 Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]-PGE2 from human EP2 receptor by liquid scintillation counting analysisDisplacement of [3H]-PGE2 from human EP2 receptor by liquid scintillation counting analysis
ChEMBL 396 8 2 4 3.5 C[C@H](NC(=O)[C@H]1CCCCN1CCOc1ccccc1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2015.05.091
122180256 128386 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 431 5 0 5 6.0 COc1ccc(CN2CCOc3c(cc(-c4csc5ccccc45)cc3OC)C2)cc1 10.1021/acs.jmedchem.5b00567
CHEMBL3586319 128386 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 431 5 0 5 6.0 COc1ccc(CN2CCOc3c(cc(-c4csc5ccccc45)cc3OC)C2)cc1 10.1021/acs.jmedchem.5b00567
11955406 152882 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 376 10 3 4 3.4 CC(C)(CO)c1ccc([C@H]2[C@H](O)CC(=O)[C@@H]2CCCCCCC(=O)O)cc1 nan
CHEMBL3919393 152882 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 376 10 3 4 3.4 CC(C)(CO)c1ccc([C@H]2[C@H](O)CC(=O)[C@@H]2CCCCCCC(=O)O)cc1 nan
44409738 146384 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Binding affinity to rat EP2 receptor expressed in HEK293 cellsBinding affinity to rat EP2 receptor expressed in HEK293 cells
ChEMBL 435 10 2 4 4.4 O=C(O)c1ccc(CCCN2C(=O)CC[C@@H]2CC[C@@H](O)Cc2cccc(Cl)c2)s1 10.1016/j.bmcl.2006.01.018
CHEMBL379746 146384 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Binding affinity to rat EP2 receptor expressed in HEK293 cellsBinding affinity to rat EP2 receptor expressed in HEK293 cells
ChEMBL 435 10 2 4 4.4 O=C(O)c1ccc(CCCN2C(=O)CC[C@@H]2CC[C@@H](O)Cc2cccc(Cl)c2)s1 10.1016/j.bmcl.2006.01.018
11577792 166097 19 None -1819 5 Human 5.7 pIC50 = 5.7 Binding
Antagonist activity at human EP2 receptorAntagonist activity at human EP2 receptor
ChEMBL 414 6 2 4 4.9 C[C@H](NC(=O)c1cc(Cl)cnc1Oc1cccc(F)c1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2017.01.067
CHEMBL4099851 166097 19 None -1819 5 Human 5.7 pIC50 = 5.7 Binding
Antagonist activity at human EP2 receptorAntagonist activity at human EP2 receptor
ChEMBL 414 6 2 4 4.9 C[C@H](NC(=O)c1cc(Cl)cnc1Oc1cccc(F)c1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2017.01.067
46879894 12953 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Binding affinity to human EP2 receptor by radioligand displacement assayBinding affinity to human EP2 receptor by radioligand displacement assay
ChEMBL 565 6 1 5 7.2 Cc1cn(Cc2ccc(Cl)cc2Cl)c2c(-c3cc(NS(=O)(=O)c4ccc(F)c(F)c4)no3)cc(F)cc12 10.1016/j.bmcl.2009.09.084
CHEMBL1081186 12953 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Binding affinity to human EP2 receptor by radioligand displacement assayBinding affinity to human EP2 receptor by radioligand displacement assay
ChEMBL 565 6 1 5 7.2 Cc1cn(Cc2ccc(Cl)cc2Cl)c2c(-c3cc(NS(=O)(=O)c4ccc(F)c(F)c4)no3)cc(F)cc12 10.1016/j.bmcl.2009.09.084
122180297 128425 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 437 3 1 4 4.9 C[C@@H]1COc2c(Cl)cc(-n3ccc4cc(F)ccc43)cc2CN1Cc1cc[nH]c(=O)c1 10.1021/acs.jmedchem.5b00567
CHEMBL3586362 128425 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 437 3 1 4 4.9 C[C@@H]1COc2c(Cl)cc(-n3ccc4cc(F)ccc43)cc2CN1Cc1cc[nH]c(=O)c1 10.1021/acs.jmedchem.5b00567
1883 9856 75 None -6 24 Human 8.7 pIC50 = 8.7 Binding
Binding affinity to human EP2 receptor (unknown origin) by radioligand displacement assayBinding affinity to human EP2 receptor (unknown origin) by radioligand displacement assay
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmc.2013.03.016
1916 9856 75 None -6 24 Human 8.7 pIC50 = 8.7 Binding
Binding affinity to human EP2 receptor (unknown origin) by radioligand displacement assayBinding affinity to human EP2 receptor (unknown origin) by radioligand displacement assay
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmc.2013.03.016
5280360 9856 75 None -6 24 Human 8.7 pIC50 = 8.7 Binding
Binding affinity to human EP2 receptor (unknown origin) by radioligand displacement assayBinding affinity to human EP2 receptor (unknown origin) by radioligand displacement assay
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmc.2013.03.016
913 9856 75 None -6 24 Human 8.7 pIC50 = 8.7 Binding
Binding affinity to human EP2 receptor (unknown origin) by radioligand displacement assayBinding affinity to human EP2 receptor (unknown origin) by radioligand displacement assay
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmc.2013.03.016
CHEMBL548 9856 75 None -6 24 Human 8.7 pIC50 = 8.7 Binding
Binding affinity to human EP2 receptor (unknown origin) by radioligand displacement assayBinding affinity to human EP2 receptor (unknown origin) by radioligand displacement assay
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmc.2013.03.016
DB00917 9856 75 None -6 24 Human 8.7 pIC50 = 8.7 Binding
Binding affinity to human EP2 receptor (unknown origin) by radioligand displacement assayBinding affinity to human EP2 receptor (unknown origin) by radioligand displacement assay
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmc.2013.03.016
1883 9856 75 None -6 24 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]PGE2 from human recombinant EP2 receptor expressed in HEK293 cells measured after 120 mins by scintillation counting methodDisplacement of [3H]PGE2 from human recombinant EP2 receptor expressed in HEK293 cells measured after 120 mins by scintillation counting method
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmc.2016.11.014
1916 9856 75 None -6 24 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]PGE2 from human recombinant EP2 receptor expressed in HEK293 cells measured after 120 mins by scintillation counting methodDisplacement of [3H]PGE2 from human recombinant EP2 receptor expressed in HEK293 cells measured after 120 mins by scintillation counting method
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmc.2016.11.014
5280360 9856 75 None -6 24 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]PGE2 from human recombinant EP2 receptor expressed in HEK293 cells measured after 120 mins by scintillation counting methodDisplacement of [3H]PGE2 from human recombinant EP2 receptor expressed in HEK293 cells measured after 120 mins by scintillation counting method
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmc.2016.11.014
913 9856 75 None -6 24 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]PGE2 from human recombinant EP2 receptor expressed in HEK293 cells measured after 120 mins by scintillation counting methodDisplacement of [3H]PGE2 from human recombinant EP2 receptor expressed in HEK293 cells measured after 120 mins by scintillation counting method
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmc.2016.11.014
CHEMBL548 9856 75 None -6 24 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]PGE2 from human recombinant EP2 receptor expressed in HEK293 cells measured after 120 mins by scintillation counting methodDisplacement of [3H]PGE2 from human recombinant EP2 receptor expressed in HEK293 cells measured after 120 mins by scintillation counting method
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmc.2016.11.014
DB00917 9856 75 None -6 24 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]PGE2 from human recombinant EP2 receptor expressed in HEK293 cells measured after 120 mins by scintillation counting methodDisplacement of [3H]PGE2 from human recombinant EP2 receptor expressed in HEK293 cells measured after 120 mins by scintillation counting method
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmc.2016.11.014
1883 9856 75 None -6 24 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]PGE2 from human recombinant prostanoid EP2 receptor expressed in HEK293 cellsDisplacement of [3H]PGE2 from human recombinant prostanoid EP2 receptor expressed in HEK293 cells
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmc.2016.03.006
1916 9856 75 None -6 24 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]PGE2 from human recombinant prostanoid EP2 receptor expressed in HEK293 cellsDisplacement of [3H]PGE2 from human recombinant prostanoid EP2 receptor expressed in HEK293 cells
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmc.2016.03.006
5280360 9856 75 None -6 24 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]PGE2 from human recombinant prostanoid EP2 receptor expressed in HEK293 cellsDisplacement of [3H]PGE2 from human recombinant prostanoid EP2 receptor expressed in HEK293 cells
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmc.2016.03.006
913 9856 75 None -6 24 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]PGE2 from human recombinant prostanoid EP2 receptor expressed in HEK293 cellsDisplacement of [3H]PGE2 from human recombinant prostanoid EP2 receptor expressed in HEK293 cells
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmc.2016.03.006
CHEMBL548 9856 75 None -6 24 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]PGE2 from human recombinant prostanoid EP2 receptor expressed in HEK293 cellsDisplacement of [3H]PGE2 from human recombinant prostanoid EP2 receptor expressed in HEK293 cells
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmc.2016.03.006
DB00917 9856 75 None -6 24 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]PGE2 from human recombinant prostanoid EP2 receptor expressed in HEK293 cellsDisplacement of [3H]PGE2 from human recombinant prostanoid EP2 receptor expressed in HEK293 cells
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmc.2016.03.006
122180249 128379 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 403 4 0 6 4.8 COc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1cncnc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586312 128379 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 403 4 0 6 4.8 COc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1cncnc1)C2 10.1021/acs.jmedchem.5b00567
122180295 128422 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 422 3 1 4 5.3 O=c1cc(CN2CCOc3c(Cl)cc(-c4csc5ccccc45)cc3C2)cc[nH]1 10.1021/acs.jmedchem.5b00567
CHEMBL3586359 128422 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 422 3 1 4 5.3 O=c1cc(CN2CCOc3c(Cl)cc(-c4csc5ccccc45)cc3C2)cc[nH]1 10.1021/acs.jmedchem.5b00567
30956824 128378 4 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 402 4 0 5 5.4 COc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1ccncc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586311 128378 4 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 402 4 0 5 5.4 COc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1ccncc1)C2 10.1021/acs.jmedchem.5b00567
122180250 128380 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 432 5 0 6 5.4 COc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1cccnc1OC)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586313 128380 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 432 5 0 6 5.4 COc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1cccnc1OC)C2 10.1021/acs.jmedchem.5b00567
122180252 128382 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 418 4 1 5 4.7 COc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1ccc(=O)[nH]c1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586315 128382 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 418 4 1 5 4.7 COc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1ccc(=O)[nH]c1)C2 10.1021/acs.jmedchem.5b00567
122180288 128416 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 386 3 0 4 5.7 Cc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586352 128416 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 386 3 0 4 5.7 Cc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
9885481 202162 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
ChEMBL 365 16 2 4 3.0 CCCCCC(O)CCCN(CCCCCCC(=O)O)S(C)(=O)=O 10.1016/j.bmcl.2009.01.059
CHEMBL551951 202162 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
ChEMBL 365 16 2 4 3.0 CCCCCC(O)CCCN(CCCCCCC(=O)O)S(C)(=O)=O 10.1016/j.bmcl.2009.01.059
11955276 157530 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 358 7 3 4 2.9 O=C(O)CCC/C=C\C[C@H]1C(=O)C[C@@H](O)[C@@H]1c1ccc2c(c1)CCC2O nan
CHEMBL3956391 157530 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 358 7 3 4 2.9 O=C(O)CCC/C=C\C[C@H]1C(=O)C[C@@H](O)[C@@H]1c1ccc2c(c1)CCC2O nan
44570666 190049 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity to human EP2 receptor by radioligand binding assayBinding affinity to human EP2 receptor by radioligand binding assay
ChEMBL 522 6 1 4 4.5 CC12CCCC(/C=C/C(=O)NS(=O)(=O)c3ccc(F)c(F)c3)=C1N(Cc1ccc(F)c(F)c1)C(=O)C2 10.1016/j.bmcl.2008.12.027
CHEMBL479664 190049 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity to human EP2 receptor by radioligand binding assayBinding affinity to human EP2 receptor by radioligand binding assay
ChEMBL 522 6 1 4 4.5 CC12CCCC(/C=C/C(=O)NS(=O)(=O)c3ccc(F)c(F)c3)=C1N(Cc1ccc(F)c(F)c1)C(=O)C2 10.1016/j.bmcl.2008.12.027
58905388 165445 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity at human EP2 receptorAntagonist activity at human EP2 receptor
ChEMBL 383 6 2 3 4.4 O=C(O)c1ccc(CNC(=O)c2cc(F)ccc2Oc2ccc(F)cc2)cc1 10.1016/j.bmcl.2017.01.067
CHEMBL4092846 165445 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity at human EP2 receptorAntagonist activity at human EP2 receptor
ChEMBL 383 6 2 3 4.4 O=C(O)c1ccc(CNC(=O)c2cc(F)ccc2Oc2ccc(F)cc2)cc1 10.1016/j.bmcl.2017.01.067
10670992 66830 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Affinity for Prostanoid EP2 receptor expressed in CHO cellsAffinity for Prostanoid EP2 receptor expressed in CHO cells
ChEMBL 444 13 4 5 4.4 O=C(O)CCCCCC[C@H]1[C@@H](O)C[C@@H](O)[C@@H]1CCC(O)CSc1cccc(Cl)c1 10.1021/jm990542v
CHEMBL173680 66830 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Affinity for Prostanoid EP2 receptor expressed in CHO cellsAffinity for Prostanoid EP2 receptor expressed in CHO cells
ChEMBL 444 13 4 5 4.4 O=C(O)CCCCCC[C@H]1[C@@H](O)C[C@@H](O)[C@@H]1CCC(O)CSc1cccc(Cl)c1 10.1021/jm990542v
15486806 107263 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Affinity for Prostanoid EP2 receptor expressed in CHO cellsAffinity for Prostanoid EP2 receptor expressed in CHO cells
ChEMBL 392 13 4 4 3.5 O=C(O)CCCCCC[C@H]1[C@@H](O)C[C@@H](O)[C@@H]1CC[C@@H](O)CCc1ccccc1 10.1021/jm990542v
CHEMBL290969 107263 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Affinity for Prostanoid EP2 receptor expressed in CHO cellsAffinity for Prostanoid EP2 receptor expressed in CHO cells
ChEMBL 392 13 4 4 3.5 O=C(O)CCCCCC[C@H]1[C@@H](O)C[C@@H](O)[C@@H]1CC[C@@H](O)CCc1ccccc1 10.1021/jm990542v
45270403 201896 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
ChEMBL 351 14 2 4 2.5 CC(C)CC(O)CCCN(CCCCCCC(=O)O)S(C)(=O)=O 10.1016/j.bmcl.2009.01.059
CHEMBL550015 201896 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
ChEMBL 351 14 2 4 2.5 CC(C)CC(O)CCCN(CCCCCCC(=O)O)S(C)(=O)=O 10.1016/j.bmcl.2009.01.059
10180 10364 58 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of beta-arrestin binding to recombinant human prostanoid EP2 receptor expressed in HEK293 cell membranes by beta-lactamase complementation assayInhibition of beta-arrestin binding to recombinant human prostanoid EP2 receptor expressed in HEK293 cell membranes by beta-lactamase complementation assay
ChEMBL 402 3 1 3 4.2 Fc1ccc2c(c1)c1CN(CCc1n2CC(=O)O)C(=O)c1cccc2c1cccc2 10.1021/jm400122f
49843471 10364 58 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of beta-arrestin binding to recombinant human prostanoid EP2 receptor expressed in HEK293 cell membranes by beta-lactamase complementation assayInhibition of beta-arrestin binding to recombinant human prostanoid EP2 receptor expressed in HEK293 cell membranes by beta-lactamase complementation assay
ChEMBL 402 3 1 3 4.2 Fc1ccc2c(c1)c1CN(CCc1n2CC(=O)O)C(=O)c1cccc2c1cccc2 10.1021/jm400122f
CHEMBL2386081 10364 58 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of beta-arrestin binding to recombinant human prostanoid EP2 receptor expressed in HEK293 cell membranes by beta-lactamase complementation assayInhibition of beta-arrestin binding to recombinant human prostanoid EP2 receptor expressed in HEK293 cell membranes by beta-lactamase complementation assay
ChEMBL 402 3 1 3 4.2 Fc1ccc2c(c1)c1CN(CCc1n2CC(=O)O)C(=O)c1cccc2c1cccc2 10.1021/jm400122f
DB12562 10364 58 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of beta-arrestin binding to recombinant human prostanoid EP2 receptor expressed in HEK293 cell membranes by beta-lactamase complementation assayInhibition of beta-arrestin binding to recombinant human prostanoid EP2 receptor expressed in HEK293 cell membranes by beta-lactamase complementation assay
ChEMBL 402 3 1 3 4.2 Fc1ccc2c(c1)c1CN(CCc1n2CC(=O)O)C(=O)c1cccc2c1cccc2 10.1021/jm400122f
45271237 201878 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
ChEMBL 403 11 1 3 4.0 CCCCc1ccc(CN(Cc2cccc(CCC(=O)O)c2)S(C)(=O)=O)cc1 10.1016/j.bmcl.2009.01.059
CHEMBL549870 201878 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
ChEMBL 403 11 1 3 4.0 CCCCc1ccc(CN(Cc2cccc(CCC(=O)O)c2)S(C)(=O)=O)cc1 10.1016/j.bmcl.2009.01.059
122180275 128402 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 385 4 1 4 4.6 COc1cc(-c2c[nH]c3ccccc23)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586338 128402 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 385 4 1 4 4.6 COc1cc(-c2c[nH]c3ccccc23)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
71733910 97110 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of beta-arrestin binding to recombinant human prostanoid EP2 receptor expressed in HEK293 cell membranes by beta-lactamase complementation assayInhibition of beta-arrestin binding to recombinant human prostanoid EP2 receptor expressed in HEK293 cell membranes by beta-lactamase complementation assay
ChEMBL 436 3 1 3 4.9 O=C(O)Cn1c2c(c3cc(F)cc(Cl)c31)CN(C(=O)c1cccc3ccccc13)CC2 10.1021/jm400122f
CHEMBL2385900 97110 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of beta-arrestin binding to recombinant human prostanoid EP2 receptor expressed in HEK293 cell membranes by beta-lactamase complementation assayInhibition of beta-arrestin binding to recombinant human prostanoid EP2 receptor expressed in HEK293 cell membranes by beta-lactamase complementation assay
ChEMBL 436 3 1 3 4.9 O=C(O)Cn1c2c(c3cc(F)cc(Cl)c31)CN(C(=O)c1cccc3ccccc13)CC2 10.1021/jm400122f
18376258 202681 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
ChEMBL 465 9 1 3 5.4 CC(C)(C)c1ccc(CN(Cc2cccc(CCC(=O)O)c2)S(=O)(=O)c2ccccc2)cc1 10.1016/j.bmcl.2009.01.059
CHEMBL559065 202681 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
ChEMBL 465 9 1 3 5.4 CC(C)(C)c1ccc(CN(Cc2cccc(CCC(=O)O)c2)S(=O)(=O)c2ccccc2)cc1 10.1016/j.bmcl.2009.01.059
122180263 128392 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 402 4 0 5 5.4 COc1cc(-c2cc3ccccc3s2)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586326 128392 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 402 4 0 5 5.4 COc1cc(-c2cc3ccccc3s2)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
22246983 202641 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
ChEMBL 389 11 1 3 4.2 CS(=O)(=O)N(CCCCCCC(=O)O)Cc1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2009.01.059
CHEMBL558671 202641 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
ChEMBL 389 11 1 3 4.2 CS(=O)(=O)N(CCCCCCC(=O)O)Cc1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2009.01.059
1883 9856 75 None -6 24 Human 8.5 pIC50 = 8.5 Binding
Binding affinity to human prostanoid EP2 receptor by radioligand displacement assayBinding affinity to human prostanoid EP2 receptor by radioligand displacement assay
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.ejmech.2013.01.044
1916 9856 75 None -6 24 Human 8.5 pIC50 = 8.5 Binding
Binding affinity to human prostanoid EP2 receptor by radioligand displacement assayBinding affinity to human prostanoid EP2 receptor by radioligand displacement assay
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.ejmech.2013.01.044
5280360 9856 75 None -6 24 Human 8.5 pIC50 = 8.5 Binding
Binding affinity to human prostanoid EP2 receptor by radioligand displacement assayBinding affinity to human prostanoid EP2 receptor by radioligand displacement assay
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.ejmech.2013.01.044
913 9856 75 None -6 24 Human 8.5 pIC50 = 8.5 Binding
Binding affinity to human prostanoid EP2 receptor by radioligand displacement assayBinding affinity to human prostanoid EP2 receptor by radioligand displacement assay
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.ejmech.2013.01.044
CHEMBL548 9856 75 None -6 24 Human 8.5 pIC50 = 8.5 Binding
Binding affinity to human prostanoid EP2 receptor by radioligand displacement assayBinding affinity to human prostanoid EP2 receptor by radioligand displacement assay
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.ejmech.2013.01.044
DB00917 9856 75 None -6 24 Human 8.5 pIC50 = 8.5 Binding
Binding affinity to human prostanoid EP2 receptor by radioligand displacement assayBinding affinity to human prostanoid EP2 receptor by radioligand displacement assay
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.ejmech.2013.01.044
122180284 128411 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 421 4 0 5 4.8 COc1cc(N2CCc3cc(Cl)ccc32)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586347 128411 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 421 4 0 5 4.8 COc1cc(N2CCc3cc(Cl)ccc32)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
122180265 128394 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 396 4 0 4 5.3 COc1cc(-c2cccc3ccccc23)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586328 128394 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 396 4 0 4 5.3 COc1cc(-c2cccc3ccccc23)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
122180274 128401 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 385 4 0 5 4.4 COc1cc(-n2ccc3ccccc32)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586337 128401 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 385 4 0 5 4.4 COc1cc(-n2ccc3ccccc32)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
122180254 128384 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 435 4 0 4 6.6 COc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1ccc(Cl)cc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586317 128384 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 435 4 0 4 6.6 COc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1ccc(Cl)cc1)C2 10.1021/acs.jmedchem.5b00567
122180255 128385 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 415 4 0 4 6.3 COc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1ccc(C)cc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586318 128385 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 415 4 0 4 6.3 COc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1ccc(C)cc1)C2 10.1021/acs.jmedchem.5b00567
122180260 128390 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 435 4 0 4 6.6 COc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1cccc(Cl)c1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586323 128390 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 435 4 0 4 6.6 COc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1cccc(Cl)c1)C2 10.1021/acs.jmedchem.5b00567
45269575 203184 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
ChEMBL 419 12 1 4 4.0 CCCCc1ccc(CN(CCCOc2cccc(C(=O)O)c2)S(C)(=O)=O)cc1 10.1016/j.bmcl.2009.01.059
CHEMBL562825 203184 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
ChEMBL 419 12 1 4 4.0 CCCCc1ccc(CN(CCCOc2cccc(C(=O)O)c2)S(C)(=O)=O)cc1 10.1016/j.bmcl.2009.01.059
45271234 201862 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
ChEMBL 405 11 1 4 3.5 CCCCc1ccc(CN(Cc2ccccc2OCC(=O)O)S(C)(=O)=O)cc1 10.1016/j.bmcl.2009.01.059
CHEMBL549663 201862 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
ChEMBL 405 11 1 4 3.5 CCCCc1ccc(CN(Cc2ccccc2OCC(=O)O)S(C)(=O)=O)cc1 10.1016/j.bmcl.2009.01.059
45268716 202777 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
ChEMBL 389 10 1 3 4.0 CCCCc1ccc(CN(c2cccc(CCC(=O)O)c2)S(C)(=O)=O)cc1 10.1016/j.bmcl.2009.01.059
CHEMBL559955 202777 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
ChEMBL 389 10 1 3 4.0 CCCCc1ccc(CN(c2cccc(CCC(=O)O)c2)S(C)(=O)=O)cc1 10.1016/j.bmcl.2009.01.059
16664733 161606 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Inhibition of human recombinant EP2 receptor expressed in 293EBNA cellsInhibition of human recombinant EP2 receptor expressed in 293EBNA cells
ChEMBL 483 9 3 5 4.3 CC(=O)Nc1cccc(-c2ccc(Cc3ocnc3C(=O)N[C@@H](Cc3ccccc3)C(=O)O)cc2)c1 10.1016/j.bmcl.2006.12.025
CHEMBL400404 161606 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Inhibition of human recombinant EP2 receptor expressed in 293EBNA cellsInhibition of human recombinant EP2 receptor expressed in 293EBNA cells
ChEMBL 483 9 3 5 4.3 CC(=O)Nc1cccc(-c2ccc(Cc3ocnc3C(=O)N[C@@H](Cc3ccccc3)C(=O)O)cc2)c1 10.1016/j.bmcl.2006.12.025
45266955 202424 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
ChEMBL 485 10 1 6 3.7 Cn1ccnc1CS(=O)(=O)N(Cc1ccc(C(C)(C)C)cc1)Cc1cccc(OCC(=O)O)c1 10.1016/j.bmcl.2009.01.059
CHEMBL556416 202424 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
ChEMBL 485 10 1 6 3.7 Cn1ccnc1CS(=O)(=O)N(Cc1ccc(C(C)(C)C)cc1)Cc1cccc(OCC(=O)O)c1 10.1016/j.bmcl.2009.01.059
44627515 203616 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Displacement of [3H]PGE2 from human EP2 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP2 receptor after 1 hr by liquid scintillation counting
ChEMBL 572 6 1 5 7.2 Cc1cn(Cc2ccc3ccccc3c2)c2c(/C=C/C(=O)NS(=O)(=O)c3cc(Cl)c(Cl)s3)cc(F)cc12 10.1021/jm9005912
CHEMBL565799 203616 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Displacement of [3H]PGE2 from human EP2 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP2 receptor after 1 hr by liquid scintillation counting
ChEMBL 572 6 1 5 7.2 Cc1cn(Cc2ccc3ccccc3c2)c2c(/C=C/C(=O)NS(=O)(=O)c3cc(Cl)c(Cl)s3)cc(F)cc12 10.1021/jm9005912
11618662 165601 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Antagonist activity at human EP2 receptorAntagonist activity at human EP2 receptor
ChEMBL 421 6 2 5 4.6 C[C@H](NC(=O)c1cc(Cl)cnc1Oc1cccc(C#N)c1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2017.01.067
CHEMBL4094572 165601 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Antagonist activity at human EP2 receptorAntagonist activity at human EP2 receptor
ChEMBL 421 6 2 5 4.6 C[C@H](NC(=O)c1cc(Cl)cnc1Oc1cccc(C#N)c1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2017.01.067
11955257 160665 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 410 9 3 3 5.3 CC(C)(C)C(O)c1ccc([C@H]2[C@H](O)C[C@@H](Cl)[C@@H]2CCCCCCC(=O)O)cc1 nan
CHEMBL3983069 160665 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 410 9 3 3 5.3 CC(C)(C)C(O)c1ccc([C@H]2[C@H](O)C[C@@H](Cl)[C@@H]2CCCCCCC(=O)O)cc1 nan
1883 9856 75 None -6 24 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/jm9018756
1916 9856 75 None -6 24 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/jm9018756
5280360 9856 75 None -6 24 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/jm9018756
913 9856 75 None -6 24 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/jm9018756
CHEMBL548 9856 75 None -6 24 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/jm9018756
DB00917 9856 75 None -6 24 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/jm9018756
1894 7744 41 None - 5 Human 5.4 pIC50 = 5.4 Binding
Affinity for Prostanoid EP2 receptor expressed in CHO cellsAffinity for Prostanoid EP2 receptor expressed in CHO cells
ChEMBL 424 11 4 5 3.2 OC(=O)CCC/C=C\C[C@H]1[C@@H](O)C[C@H]([C@@H]1/C=C/[C@H](COc1cccc(c1)Cl)O)O 10.1021/jm990542v
5311053 7744 41 None - 5 Human 5.4 pIC50 = 5.4 Binding
Affinity for Prostanoid EP2 receptor expressed in CHO cellsAffinity for Prostanoid EP2 receptor expressed in CHO cells
ChEMBL 424 11 4 5 3.2 OC(=O)CCC/C=C\C[C@H]1[C@@H](O)C[C@H]([C@@H]1/C=C/[C@H](COc1cccc(c1)Cl)O)O 10.1021/jm990542v
CHEMBL37853 7744 41 None - 5 Human 5.4 pIC50 = 5.4 Binding
Affinity for Prostanoid EP2 receptor expressed in CHO cellsAffinity for Prostanoid EP2 receptor expressed in CHO cells
ChEMBL 424 11 4 5 3.2 OC(=O)CCC/C=C\C[C@H]1[C@@H](O)C[C@H]([C@@H]1/C=C/[C@H](COc1cccc(c1)Cl)O)O 10.1021/jm990542v
DB11507 7744 41 None - 5 Human 5.4 pIC50 = 5.4 Binding
Affinity for Prostanoid EP2 receptor expressed in CHO cellsAffinity for Prostanoid EP2 receptor expressed in CHO cells
ChEMBL 424 11 4 5 3.2 OC(=O)CCC/C=C\C[C@H]1[C@@H](O)C[C@H]([C@@H]1/C=C/[C@H](COc1cccc(c1)Cl)O)O 10.1021/jm990542v
118175009 143463 0 None -812 2 Human 5.4 pIC50 = 5.4 Binding
Antagonist activity at human EP2 receptorAntagonist activity at human EP2 receptor
ChEMBL 429 4 2 2 6.7 Cc1ccc(C(=O)O)c(C)c1NC(=O)c1cc(-c2cccc(Cl)c2)cc2ccccc12 10.1016/j.bmcl.2015.11.023
CHEMBL3740325 143463 0 None -812 2 Human 5.4 pIC50 = 5.4 Binding
Antagonist activity at human EP2 receptorAntagonist activity at human EP2 receptor
ChEMBL 429 4 2 2 6.7 Cc1ccc(C(=O)O)c(C)c1NC(=O)c1cc(-c2cccc(Cl)c2)cc2ccccc12 10.1016/j.bmcl.2015.11.023
45271238 202420 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
ChEMBL 403 8 1 3 4.0 CC(C)(C)c1ccc(CN(Cc2cccc(CCC(=O)O)c2)S(C)(=O)=O)cc1 10.1016/j.bmcl.2009.01.059
CHEMBL556333 202420 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
ChEMBL 403 8 1 3 4.0 CC(C)(C)c1ccc(CN(Cc2cccc(CCC(=O)O)c2)S(C)(=O)=O)cc1 10.1016/j.bmcl.2009.01.059
1883 9856 75 None -6 24 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]prostaglandin E2 from human EP2 receptor expressed in HEK293 cell membranes after 60 mins by liquid scintillation countingDisplacement of [3H]prostaglandin E2 from human EP2 receptor expressed in HEK293 cell membranes after 60 mins by liquid scintillation counting
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/acs.jmedchem.8b00808
1916 9856 75 None -6 24 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]prostaglandin E2 from human EP2 receptor expressed in HEK293 cell membranes after 60 mins by liquid scintillation countingDisplacement of [3H]prostaglandin E2 from human EP2 receptor expressed in HEK293 cell membranes after 60 mins by liquid scintillation counting
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/acs.jmedchem.8b00808
5280360 9856 75 None -6 24 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]prostaglandin E2 from human EP2 receptor expressed in HEK293 cell membranes after 60 mins by liquid scintillation countingDisplacement of [3H]prostaglandin E2 from human EP2 receptor expressed in HEK293 cell membranes after 60 mins by liquid scintillation counting
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/acs.jmedchem.8b00808
913 9856 75 None -6 24 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]prostaglandin E2 from human EP2 receptor expressed in HEK293 cell membranes after 60 mins by liquid scintillation countingDisplacement of [3H]prostaglandin E2 from human EP2 receptor expressed in HEK293 cell membranes after 60 mins by liquid scintillation counting
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/acs.jmedchem.8b00808
CHEMBL548 9856 75 None -6 24 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]prostaglandin E2 from human EP2 receptor expressed in HEK293 cell membranes after 60 mins by liquid scintillation countingDisplacement of [3H]prostaglandin E2 from human EP2 receptor expressed in HEK293 cell membranes after 60 mins by liquid scintillation counting
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/acs.jmedchem.8b00808
DB00917 9856 75 None -6 24 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]prostaglandin E2 from human EP2 receptor expressed in HEK293 cell membranes after 60 mins by liquid scintillation countingDisplacement of [3H]prostaglandin E2 from human EP2 receptor expressed in HEK293 cell membranes after 60 mins by liquid scintillation counting
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/acs.jmedchem.8b00808
122180272 128399 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 403 4 0 6 4.8 COc1cc(-c2nsc3ccccc23)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586335 128399 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 403 4 0 6 4.8 COc1cc(-c2nsc3ccccc23)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
122180278 128405 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 419 4 0 5 5.1 COc1cc(-n2ccc3c(Cl)cccc32)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586341 128405 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 419 4 0 5 5.1 COc1cc(-n2ccc3c(Cl)cccc32)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
122180292 128420 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 385 3 0 4 5.4 CN1CCN(Cc2cccnc2)Cc2cc(-c3csc4ccccc34)ccc21 10.1021/acs.jmedchem.5b00567
CHEMBL3586356 128420 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 385 3 0 4 5.4 CN1CCN(Cc2cccnc2)Cc2cc(-c3csc4ccccc34)ccc21 10.1021/acs.jmedchem.5b00567
11296282 8191 32 None - 1 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]PGE2 from human EP2 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP2 receptor after 1 hr by liquid scintillation counting
ChEMBL 590 6 1 5 7.3 Clc1ccc(c(c1)Cl)Cn1cc(c2c1c(/C=C/C(=O)NS(=O)(=O)c1sc(c(c1)Cl)Cl)cc(c2)F)C 10.1021/jm9005912
5822 8191 32 None - 1 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]PGE2 from human EP2 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP2 receptor after 1 hr by liquid scintillation counting
ChEMBL 590 6 1 5 7.3 Clc1ccc(c(c1)Cl)Cn1cc(c2c1c(/C=C/C(=O)NS(=O)(=O)c1sc(c(c1)Cl)Cl)cc(c2)F)C 10.1021/jm9005912
CHEMBL565591 8191 32 None - 1 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]PGE2 from human EP2 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP2 receptor after 1 hr by liquid scintillation counting
ChEMBL 590 6 1 5 7.3 Clc1ccc(c(c1)Cl)Cn1cc(c2c1c(/C=C/C(=O)NS(=O)(=O)c1sc(c(c1)Cl)Cl)cc(c2)F)C 10.1021/jm9005912
44230999 174225 26 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]prostaglandin E2 from human EP2 receptor expressed in HEK293 cell membranes after 60 mins by liquid scintillation countingDisplacement of [3H]prostaglandin E2 from human EP2 receptor expressed in HEK293 cell membranes after 60 mins by liquid scintillation counting
ChEMBL 520 11 1 9 3.4 CC(C)OC(=O)CNc1cccc(CN(Cc2ccc(-n3cccn3)cc2)S(=O)(=O)c2cccnc2)n1 10.1021/acs.jmedchem.8b00808
CHEMBL4297666 174225 26 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]prostaglandin E2 from human EP2 receptor expressed in HEK293 cell membranes after 60 mins by liquid scintillation countingDisplacement of [3H]prostaglandin E2 from human EP2 receptor expressed in HEK293 cell membranes after 60 mins by liquid scintillation counting
ChEMBL 520 11 1 9 3.4 CC(C)OC(=O)CNc1cccc(CN(Cc2ccc(-n3cccn3)cc2)S(=O)(=O)c2cccnc2)n1 10.1021/acs.jmedchem.8b00808
DB15071 174225 26 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]prostaglandin E2 from human EP2 receptor expressed in HEK293 cell membranes after 60 mins by liquid scintillation countingDisplacement of [3H]prostaglandin E2 from human EP2 receptor expressed in HEK293 cell membranes after 60 mins by liquid scintillation counting
ChEMBL 520 11 1 9 3.4 CC(C)OC(=O)CNc1cccc(CN(Cc2ccc(-n3cccn3)cc2)S(=O)(=O)c2cccnc2)n1 10.1021/acs.jmedchem.8b00808
11955235 159530 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 394 9 3 3 4.2 CC(C)(CO)c1ccc([C@H]2[C@H](O)C[C@@H](Cl)[C@@H]2C/C=C\CCCC(=O)O)cc1 nan
CHEMBL3973312 159530 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 394 9 3 3 4.2 CC(C)(CO)c1ccc([C@H]2[C@H](O)C[C@@H](Cl)[C@@H]2C/C=C\CCCC(=O)O)cc1 nan
44564571 193594 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of radioligand from EP2 receptorDisplacement of radioligand from EP2 receptor
ChEMBL 536 6 1 5 6.1 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2ccc(F)c(F)c2)c2c(Oc3ccc(Cl)c(Cl)c3)cccc21 10.1016/j.bmcl.2008.12.112
CHEMBL489310 193594 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of radioligand from EP2 receptorDisplacement of radioligand from EP2 receptor
ChEMBL 536 6 1 5 6.1 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2ccc(F)c(F)c2)c2c(Oc3ccc(Cl)c(Cl)c3)cccc21 10.1016/j.bmcl.2008.12.112
11683088 165757 0 None - 1 Human 5.4 pIC50 = 5.4 Binding
Antagonist activity at human EP2 receptorAntagonist activity at human EP2 receptor
ChEMBL 414 6 2 4 4.9 C[C@H](NC(=O)c1cc(Cl)cnc1Oc1ccc(F)cc1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2017.01.067
CHEMBL4096216 165757 0 None - 1 Human 5.4 pIC50 = 5.4 Binding
Antagonist activity at human EP2 receptorAntagonist activity at human EP2 receptor
ChEMBL 414 6 2 4 4.9 C[C@H](NC(=O)c1cc(Cl)cnc1Oc1ccc(F)cc1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2017.01.067
162671048 189586 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]prostaglandin E2 from full-length recombinant human EP2 receptor expressed in HEK293 cell membranes measured after 120 mins by scintillation counting methodDisplacement of [3H]prostaglandin E2 from full-length recombinant human EP2 receptor expressed in HEK293 cell membranes measured after 120 mins by scintillation counting method
ChEMBL 451 5 1 4 5.4 Cc1c(-c2cccs2)nc2ccc(Br)cc2c1C(=O)NCCc1cccnc1 10.1021/acs.jmedchem.0c00834
CHEMBL4790821 189586 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]prostaglandin E2 from full-length recombinant human EP2 receptor expressed in HEK293 cell membranes measured after 120 mins by scintillation counting methodDisplacement of [3H]prostaglandin E2 from full-length recombinant human EP2 receptor expressed in HEK293 cell membranes measured after 120 mins by scintillation counting method
ChEMBL 451 5 1 4 5.4 Cc1c(-c2cccs2)nc2ccc(Br)cc2c1C(=O)NCCc1cccnc1 10.1021/acs.jmedchem.0c00834
9934368 145699 11 None - 1 Rat 6.3 pIC50 = 6.3 Binding
Binding affinity to rat EP2 receptorBinding affinity to rat EP2 receptor
ChEMBL 469 10 2 4 4.8 O=C(O)c1ccc(CCCN2C(=O)CC[C@@H]2CC[C@@H](O)Cc2cccc(C(F)(F)F)c2)s1 10.1021/jm9018756
CHEMBL378376 145699 11 None - 1 Rat 6.3 pIC50 = 6.3 Binding
Binding affinity to rat EP2 receptorBinding affinity to rat EP2 receptor
ChEMBL 469 10 2 4 4.8 O=C(O)c1ccc(CCCN2C(=O)CC[C@@H]2CC[C@@H](O)Cc2cccc(C(F)(F)F)c2)s1 10.1021/jm9018756
9934368 145699 11 None - 1 Rat 6.3 pIC50 = 6.3 Binding
Binding affinity to rat EP2 receptor expressed in HEK293 cellsBinding affinity to rat EP2 receptor expressed in HEK293 cells
ChEMBL 469 10 2 4 4.8 O=C(O)c1ccc(CCCN2C(=O)CC[C@@H]2CC[C@@H](O)Cc2cccc(C(F)(F)F)c2)s1 10.1016/j.bmcl.2006.01.018
CHEMBL378376 145699 11 None - 1 Rat 6.3 pIC50 = 6.3 Binding
Binding affinity to rat EP2 receptor expressed in HEK293 cellsBinding affinity to rat EP2 receptor expressed in HEK293 cells
ChEMBL 469 10 2 4 4.8 O=C(O)c1ccc(CCCN2C(=O)CC[C@@H]2CC[C@@H](O)Cc2cccc(C(F)(F)F)c2)s1 10.1016/j.bmcl.2006.01.018
44627395 203651 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [3H]PGE2 from human EP2 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP2 receptor after 1 hr by liquid scintillation counting
ChEMBL 563 7 1 7 5.6 O=C(COc1cccc2ncn(Cc3ccc(Cl)cc3Cl)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1021/jm9005912
CHEMBL565992 203651 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [3H]PGE2 from human EP2 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP2 receptor after 1 hr by liquid scintillation counting
ChEMBL 563 7 1 7 5.6 O=C(COc1cccc2ncn(Cc3ccc(Cl)cc3Cl)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1021/jm9005912
11955410 159308 0 None - 0 Human 4.3 pIC50 = 4.3 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 408 9 2 4 4.3 COC(=O)CCC/C=C\C[C@@H]1[C@@H](c2ccc(C(C)(C)CO)cc2)[C@H](O)C[C@H]1Cl nan
CHEMBL3971493 159308 0 None - 0 Human 4.3 pIC50 = 4.3 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 408 9 2 4 4.3 COC(=O)CCC/C=C\C[C@@H]1[C@@H](c2ccc(C(C)(C)CO)cc2)[C@H](O)C[C@H]1Cl nan
5311239 137396 31 None - 0 Human 5.3 pIC50 = 5.3 Binding
Affinity for Prostanoid EP2 receptor expressed in CHO cellsAffinity for Prostanoid EP2 receptor expressed in CHO cells
ChEMBL 358 14 4 4 3.5 CCCCC[C@H](O)CC[C@H]1[C@H](O)C[C@H](O)[C@@H]1CCCCCCC(=O)O 10.1021/jm990542v
CHEMBL36817 137396 31 None - 0 Human 5.3 pIC50 = 5.3 Binding
Affinity for Prostanoid EP2 receptor expressed in CHO cellsAffinity for Prostanoid EP2 receptor expressed in CHO cells
ChEMBL 358 14 4 4 3.5 CCCCC[C@H](O)CC[C@H]1[C@H](O)C[C@H](O)[C@@H]1CCCCCCC(=O)O 10.1021/jm990542v
45268715 202755 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
ChEMBL 403 11 1 3 4.4 CCCCc1ccc(CN(c2ccccc2CCCC(=O)O)S(C)(=O)=O)cc1 10.1016/j.bmcl.2009.01.059
CHEMBL559760 202755 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
ChEMBL 403 11 1 3 4.4 CCCCc1ccc(CN(c2ccccc2CCCC(=O)O)S(C)(=O)=O)cc1 10.1016/j.bmcl.2009.01.059
25114442 9835 56 None - 1 Human 8.3 pIC50 = 8.3 Binding
Affinity Biochemical interaction (Enzymatic inhibition assay) EUB0000351a PTGER2Affinity Biochemical interaction (Enzymatic inhibition assay) EUB0000351a PTGER2
ChEMBL 409 6 1 4 3.6 COc1ccc2c(c1)ccc(c2)OCC1(CN(C1)C(=O)c1ccc(cc1)F)C(=O)O 10.6019/CHEMBL5210307
5817 9835 56 None - 1 Human 8.3 pIC50 = 8.3 Binding
Affinity Biochemical interaction (Enzymatic inhibition assay) EUB0000351a PTGER2Affinity Biochemical interaction (Enzymatic inhibition assay) EUB0000351a PTGER2
ChEMBL 409 6 1 4 3.6 COc1ccc2c(c1)ccc(c2)OCC1(CN(C1)C(=O)c1ccc(cc1)F)C(=O)O 10.6019/CHEMBL5210307
CHEMBL3286797 9835 56 None - 1 Human 8.3 pIC50 = 8.3 Binding
Affinity Biochemical interaction (Enzymatic inhibition assay) EUB0000351a PTGER2Affinity Biochemical interaction (Enzymatic inhibition assay) EUB0000351a PTGER2
ChEMBL 409 6 1 4 3.6 COc1ccc2c(c1)ccc(c2)OCC1(CN(C1)C(=O)c1ccc(cc1)F)C(=O)O 10.6019/CHEMBL5210307
DB12024 9835 56 None - 1 Human 8.3 pIC50 = 8.3 Binding
Affinity Biochemical interaction (Enzymatic inhibition assay) EUB0000351a PTGER2Affinity Biochemical interaction (Enzymatic inhibition assay) EUB0000351a PTGER2
ChEMBL 409 6 1 4 3.6 COc1ccc2c(c1)ccc(c2)OCC1(CN(C1)C(=O)c1ccc(cc1)F)C(=O)O 10.6019/CHEMBL5210307
1883 9856 75 None -7 24 Rat 8.3 pIC50 = 8.3 Binding
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmcl.2009.01.059
1916 9856 75 None -7 24 Rat 8.3 pIC50 = 8.3 Binding
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmcl.2009.01.059
5280360 9856 75 None -7 24 Rat 8.3 pIC50 = 8.3 Binding
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmcl.2009.01.059
913 9856 75 None -7 24 Rat 8.3 pIC50 = 8.3 Binding
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmcl.2009.01.059
CHEMBL548 9856 75 None -7 24 Rat 8.3 pIC50 = 8.3 Binding
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmcl.2009.01.059
DB00917 9856 75 None -7 24 Rat 8.3 pIC50 = 8.3 Binding
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmcl.2009.01.059
1929 8386 55 None - 2 Rat 7.3 pIC50 = 7.3 Binding
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
ChEMBL 468 9 1 5 4.2 OC(=O)COc1cccc(c1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)C(C)(C)C 10.1016/j.bmcl.2009.01.059
9890801 8386 55 None - 2 Rat 7.3 pIC50 = 7.3 Binding
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
ChEMBL 468 9 1 5 4.2 OC(=O)COc1cccc(c1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)C(C)(C)C 10.1016/j.bmcl.2009.01.059
CHEMBL563646 8386 55 None - 2 Rat 7.3 pIC50 = 7.3 Binding
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
ChEMBL 468 9 1 5 4.2 OC(=O)COc1cccc(c1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)C(C)(C)C 10.1016/j.bmcl.2009.01.059
DB12022 8386 55 None - 2 Rat 7.3 pIC50 = 7.3 Binding
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
ChEMBL 468 9 1 5 4.2 OC(=O)COc1cccc(c1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)C(C)(C)C 10.1016/j.bmcl.2009.01.059
22246895 202343 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
ChEMBL 399 14 2 4 3.7 CCCCC(O)c1ccc(CN(CCCCCCC(=O)O)S(C)(=O)=O)cc1 10.1016/j.bmcl.2009.01.059
CHEMBL554823 202343 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
ChEMBL 399 14 2 4 3.7 CCCCC(O)c1ccc(CN(CCCCCCC(=O)O)S(C)(=O)=O)cc1 10.1016/j.bmcl.2009.01.059
18376196 201701 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
ChEMBL 466 9 1 4 4.8 CC(C)(C)c1ccc(CN(Cc2cccc(CCC(=O)O)c2)S(=O)(=O)c2ccccn2)cc1 10.1016/j.bmcl.2009.01.059
CHEMBL541516 201701 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
ChEMBL 466 9 1 4 4.8 CC(C)(C)c1ccc(CN(Cc2cccc(CCC(=O)O)c2)S(=O)(=O)c2ccccn2)cc1 10.1016/j.bmcl.2009.01.059
58681352 161118 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 486 10 3 4 5.5 CCCC1(C(O)c2cccc([C@H]3[C@H](O)C[C@@H](Cl)[C@@H]3Cc3cccc(OCC(=O)O)c3)c2)CCC1 nan
CHEMBL3986829 161118 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 486 10 3 4 5.5 CCCC1(C(O)c2cccc([C@H]3[C@H](O)C[C@@H](Cl)[C@@H]3Cc3cccc(OCC(=O)O)c3)c2)CCC1 nan
122180281 128408 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 419 4 0 5 5.1 COc1cc(-n2ccc3cccc(Cl)c32)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586344 128408 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 419 4 0 5 5.1 COc1cc(-n2ccc3cccc(Cl)c32)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
16048029 202283 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
ChEMBL 369 10 1 3 3.8 CC(C)(C)c1ccc(CN(CCCCCCC(=O)O)S(C)(=O)=O)cc1 10.1016/j.bmcl.2009.01.059
CHEMBL553468 202283 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
ChEMBL 369 10 1 3 3.8 CC(C)(C)c1ccc(CN(CCCCCCC(=O)O)S(C)(=O)=O)cc1 10.1016/j.bmcl.2009.01.059
122180277 128404 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 419 4 0 5 5.1 COc1cc(-n2cc(Cl)c3ccccc32)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586340 128404 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 419 4 0 5 5.1 COc1cc(-n2cc(Cl)c3ccccc32)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
122180257 128387 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 459 5 0 6 5.8 COC(=O)c1ccc(CN2CCOc3c(cc(-c4csc5ccccc45)cc3OC)C2)cc1 10.1021/acs.jmedchem.5b00567
CHEMBL3586320 128387 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 459 5 0 6 5.8 COC(=O)c1ccc(CN2CCOc3c(cc(-c4csc5ccccc45)cc3OC)C2)cc1 10.1021/acs.jmedchem.5b00567
122180258 128388 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 426 4 0 5 5.8 COc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1ccc(C#N)cc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586321 128388 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 426 4 0 5 5.8 COc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1ccc(C#N)cc1)C2 10.1021/acs.jmedchem.5b00567
122180291 128419 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 371 3 1 4 5.4 c1cncc(CN2CCNc3ccc(-c4csc5ccccc45)cc3C2)c1 10.1021/acs.jmedchem.5b00567
CHEMBL3586355 128419 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 371 3 1 4 5.4 c1cncc(CN2CCNc3ccc(-c4csc5ccccc45)cc3C2)c1 10.1021/acs.jmedchem.5b00567
11955358 159861 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 364 8 2 2 4.7 O=C(O)CCCCCC[C@@H]1[C@@H](c2ccc3c(c2)CCC3)[C@H](O)C[C@H]1Cl nan
CHEMBL3976116 159861 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 364 8 2 2 4.7 O=C(O)CCCCCC[C@@H]1[C@@H](c2ccc3c(c2)CCC3)[C@H](O)C[C@H]1Cl nan
18376082 201702 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
ChEMBL 472 9 1 5 4.8 CC(C)(C)c1ccc(CN(Cc2cccc(CCC(=O)O)c2)S(=O)(=O)c2nccs2)cc1 10.1016/j.bmcl.2009.01.059
CHEMBL541517 201702 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
ChEMBL 472 9 1 5 4.8 CC(C)(C)c1ccc(CN(Cc2cccc(CCC(=O)O)c2)S(=O)(=O)c2nccs2)cc1 10.1016/j.bmcl.2009.01.059
22246956 203098 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
ChEMBL 411 15 1 4 4.2 CCCCCC(=O)c1ccc(CN(CCCCCCC(=O)O)S(C)(=O)=O)cc1 10.1016/j.bmcl.2009.01.059
CHEMBL562291 203098 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
ChEMBL 411 15 1 4 4.2 CCCCCC(=O)c1ccc(CN(CCCCCCC(=O)O)S(C)(=O)=O)cc1 10.1016/j.bmcl.2009.01.059
44409917 146028 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Binding affinity to rat EP2 receptor expressed in HEK293 cellsBinding affinity to rat EP2 receptor expressed in HEK293 cells
ChEMBL 419 10 2 4 3.9 O=C(O)c1ccc(CCCN2C(=O)CC[C@@H]2CCC(O)Cc2cccc(F)c2)s1 10.1016/j.bmcl.2006.01.018
CHEMBL378968 146028 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Binding affinity to rat EP2 receptor expressed in HEK293 cellsBinding affinity to rat EP2 receptor expressed in HEK293 cells
ChEMBL 419 10 2 4 3.9 O=C(O)c1ccc(CCCN2C(=O)CC[C@@H]2CCC(O)Cc2cccc(F)c2)s1 10.1016/j.bmcl.2006.01.018
122180273 128400 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 386 4 0 6 3.8 COc1cc(-n2cnc3ccccc32)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586336 128400 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 386 4 0 6 3.8 COc1cc(-n2cnc3ccccc32)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
11539410 97114 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of beta-arrestin binding to recombinant human prostanoid EP2 receptor expressed in HEK293 cell membranes by beta-lactamase complementation assayInhibition of beta-arrestin binding to recombinant human prostanoid EP2 receptor expressed in HEK293 cell membranes by beta-lactamase complementation assay
ChEMBL 438 5 1 3 5.2 CCc1ccc(-c2ccc(C(=O)N3CCc4c(c5ccccc5n4CC(=O)O)C3)cc2)cc1 10.1021/jm400122f
CHEMBL2385904 97114 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of beta-arrestin binding to recombinant human prostanoid EP2 receptor expressed in HEK293 cell membranes by beta-lactamase complementation assayInhibition of beta-arrestin binding to recombinant human prostanoid EP2 receptor expressed in HEK293 cell membranes by beta-lactamase complementation assay
ChEMBL 438 5 1 3 5.2 CCc1ccc(-c2ccc(C(=O)N3CCc4c(c5ccccc5n4CC(=O)O)C3)cc2)cc1 10.1021/jm400122f
45269576 202762 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
ChEMBL 403 11 1 3 4.4 CCCCc1ccc(CN(c2ccc(CCCC(=O)O)cc2)S(C)(=O)=O)cc1 10.1016/j.bmcl.2009.01.059
CHEMBL559820 202762 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
ChEMBL 403 11 1 3 4.4 CCCCc1ccc(CN(c2ccc(CCCC(=O)O)cc2)S(C)(=O)=O)cc1 10.1016/j.bmcl.2009.01.059
11653874 97134 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of beta-arrestin binding to recombinant human prostanoid EP2 receptor expressed in HEK293 cell membranes by beta-lactamase complementation assayInhibition of beta-arrestin binding to recombinant human prostanoid EP2 receptor expressed in HEK293 cell membranes by beta-lactamase complementation assay
ChEMBL 384 3 1 3 4.1 O=C(O)Cn1c2c(c3ccccc31)CN(C(=O)c1cccc3ccccc13)CC2 10.1021/jm400122f
CHEMBL2386079 97134 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of beta-arrestin binding to recombinant human prostanoid EP2 receptor expressed in HEK293 cell membranes by beta-lactamase complementation assayInhibition of beta-arrestin binding to recombinant human prostanoid EP2 receptor expressed in HEK293 cell membranes by beta-lactamase complementation assay
ChEMBL 384 3 1 3 4.1 O=C(O)Cn1c2c(c3ccccc31)CN(C(=O)c1cccc3ccccc13)CC2 10.1021/jm400122f
1955 6805 1 None - 0 Human 5.2 pIC50 = 5.2 Binding
Affinity for Prostanoid EP2 receptor expressed in CHO cellsAffinity for Prostanoid EP2 receptor expressed in CHO cells
ChEMBL 428 13 4 5 3.6 O[C@@H](COc1cccc(c1)Cl)CC[C@H]1[C@H](O)C[C@@H]([C@@H]1CCCCCCC(=O)O)O 10.1021/jm990542v
5311240 6805 1 None - 0 Human 5.2 pIC50 = 5.2 Binding
Affinity for Prostanoid EP2 receptor expressed in CHO cellsAffinity for Prostanoid EP2 receptor expressed in CHO cells
ChEMBL 428 13 4 5 3.6 O[C@@H](COc1cccc(c1)Cl)CC[C@H]1[C@H](O)C[C@@H]([C@@H]1CCCCCCC(=O)O)O 10.1021/jm990542v
CHEMBL36041 6805 1 None - 0 Human 5.2 pIC50 = 5.2 Binding
Affinity for Prostanoid EP2 receptor expressed in CHO cellsAffinity for Prostanoid EP2 receptor expressed in CHO cells
ChEMBL 428 13 4 5 3.6 O[C@@H](COc1cccc(c1)Cl)CC[C@H]1[C@H](O)C[C@@H]([C@@H]1CCCCCCC(=O)O)O 10.1021/jm990542v
44409733 147662 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Binding affinity to rat EP2 receptor expressed in HEK293 cellsBinding affinity to rat EP2 receptor expressed in HEK293 cells
ChEMBL 401 10 2 4 3.8 O=C(O)c1ccc(CCCN2C(=O)CC[C@@H]2CCC(O)Cc2ccccc2)s1 10.1016/j.bmcl.2006.01.018
CHEMBL382029 147662 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Binding affinity to rat EP2 receptor expressed in HEK293 cellsBinding affinity to rat EP2 receptor expressed in HEK293 cells
ChEMBL 401 10 2 4 3.8 O=C(O)c1ccc(CCCN2C(=O)CC[C@@H]2CCC(O)Cc2ccccc2)s1 10.1016/j.bmcl.2006.01.018
30897313 128376 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 402 4 0 5 5.4 COc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586309 128376 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 402 4 0 5 5.4 COc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
42484632 128377 5 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 402 4 0 5 5.4 COc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1ccccn1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586310 128377 5 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 402 4 0 5 5.4 COc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1ccccn1)C2 10.1021/acs.jmedchem.5b00567
122180270 128397 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 380 4 0 4 4.8 COc1cc(-c2cccc(Cl)c2)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586333 128397 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 380 4 0 4 4.8 COc1cc(-c2cccc(Cl)c2)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
22246893 202731 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
ChEMBL 371 13 1 4 2.7 CCCCc1ccc(CN(CCCCOCC(=O)O)S(C)(=O)=O)cc1 10.1016/j.bmcl.2009.01.059
CHEMBL559561 202731 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
ChEMBL 371 13 1 4 2.7 CCCCc1ccc(CN(CCCCOCC(=O)O)S(C)(=O)=O)cc1 10.1016/j.bmcl.2009.01.059
11524454 7733 55 None - 1 Human 6.2 pIC50 = 6.2 Binding
Antagonist activity at human EP2 receptorAntagonist activity at human EP2 receptor
ChEMBL 413 6 2 3 5.5 Clc1ccc(c(c1)C(=O)N[C@H](c1ccc(cc1)C(=O)O)C)Oc1ccc(cc1)F 10.1016/j.bmcl.2017.01.067
5857 7733 55 None - 1 Human 6.2 pIC50 = 6.2 Binding
Antagonist activity at human EP2 receptorAntagonist activity at human EP2 receptor
ChEMBL 413 6 2 3 5.5 Clc1ccc(c(c1)C(=O)N[C@H](c1ccc(cc1)C(=O)O)C)Oc1ccc(cc1)F 10.1016/j.bmcl.2017.01.067
CHEMBL591666 7733 55 None - 1 Human 6.2 pIC50 = 6.2 Binding
Antagonist activity at human EP2 receptorAntagonist activity at human EP2 receptor
ChEMBL 413 6 2 3 5.5 Clc1ccc(c(c1)C(=O)N[C@H](c1ccc(cc1)C(=O)O)C)Oc1ccc(cc1)F 10.1016/j.bmcl.2017.01.067
68505327 97135 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of beta-arrestin binding to recombinant human prostanoid EP2 receptor expressed in HEK293 cell membranes by beta-lactamase complementation assayInhibition of beta-arrestin binding to recombinant human prostanoid EP2 receptor expressed in HEK293 cell membranes by beta-lactamase complementation assay
ChEMBL 418 3 1 3 4.7 O=C(O)Cn1c2c(c3cc(Cl)ccc31)CN(C(=O)c1cccc3ccccc13)CC2 10.1021/jm400122f
CHEMBL2386080 97135 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of beta-arrestin binding to recombinant human prostanoid EP2 receptor expressed in HEK293 cell membranes by beta-lactamase complementation assayInhibition of beta-arrestin binding to recombinant human prostanoid EP2 receptor expressed in HEK293 cell membranes by beta-lactamase complementation assay
ChEMBL 418 3 1 3 4.7 O=C(O)Cn1c2c(c3cc(Cl)ccc31)CN(C(=O)c1cccc3ccccc13)CC2 10.1021/jm400122f
44564892 187301 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of radioligand from EP2 receptorDisplacement of radioligand from EP2 receptor
ChEMBL 554 6 1 5 6.2 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2cc(F)c(F)cc2F)c2c(Oc3ccc(Cl)c(Cl)c3)cccc21 10.1016/j.bmcl.2008.12.112
CHEMBL475348 187301 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of radioligand from EP2 receptorDisplacement of radioligand from EP2 receptor
ChEMBL 554 6 1 5 6.2 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2cc(F)c(F)cc2F)c2c(Oc3ccc(Cl)c(Cl)c3)cccc21 10.1016/j.bmcl.2008.12.112
10126807 201877 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
ChEMBL 405 8 1 4 3.4 CC(C)(C)c1ccc(CN(Cc2cccc(OCC(=O)O)c2)S(C)(=O)=O)cc1 10.1016/j.bmcl.2009.01.059
CHEMBL549869 201877 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
ChEMBL 405 8 1 4 3.4 CC(C)(C)c1ccc(CN(Cc2cccc(OCC(=O)O)c2)S(C)(=O)=O)cc1 10.1016/j.bmcl.2009.01.059
56927669 128423 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 423 3 1 4 4.5 O=c1cc(CN2CCOc3c(Cl)cc(-n4ccc5cc(F)ccc54)cc3C2)cc[nH]1 10.1021/acs.jmedchem.5b00567
CHEMBL3586360 128423 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 423 3 1 4 4.5 O=c1cc(CN2CCOc3c(Cl)cc(-n4ccc5cc(F)ccc54)cc3C2)cc[nH]1 10.1021/acs.jmedchem.5b00567
122180296 128424 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 436 3 1 4 5.7 C[C@@H]1COc2c(Cl)cc(-c3csc4ccccc34)cc2CN1Cc1cc[nH]c(=O)c1 10.1021/acs.jmedchem.5b00567
CHEMBL3586361 128424 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 436 3 1 4 5.7 C[C@@H]1COc2c(Cl)cc(-c3csc4ccccc34)cc2CN1Cc1cc[nH]c(=O)c1 10.1021/acs.jmedchem.5b00567
122180279 128406 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 419 4 0 5 5.1 COc1cc(-n2ccc3cc(Cl)ccc32)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586342 128406 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 419 4 0 5 5.1 COc1cc(-n2ccc3cc(Cl)ccc32)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
122180289 128417 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 406 3 0 4 6.0 Clc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586353 128417 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 406 3 0 4 6.0 Clc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
122180280 128407 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 419 4 0 5 5.1 COc1cc(-n2ccc3ccc(Cl)cc32)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586343 128407 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 419 4 0 5 5.1 COc1cc(-n2ccc3ccc(Cl)cc32)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
22246765 201977 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
ChEMBL 403 11 1 3 3.7 CCCCc1ccc(CN(CCc2ccc(CC(=O)O)cc2)S(C)(=O)=O)cc1 10.1016/j.bmcl.2009.01.059
CHEMBL550619 201977 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
ChEMBL 403 11 1 3 3.7 CCCCc1ccc(CN(CCc2ccc(CC(=O)O)cc2)S(C)(=O)=O)cc1 10.1016/j.bmcl.2009.01.059
44409918 172752 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Binding affinity to rat EP2 receptor expressed in HEK293 cellsBinding affinity to rat EP2 receptor expressed in HEK293 cells
ChEMBL 435 10 2 4 4.4 O=C(O)c1ccc(CCCN2C(=O)CC[C@@H]2CCC(O)Cc2ccc(Cl)cc2)s1 10.1016/j.bmcl.2006.01.018
CHEMBL425243 172752 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Binding affinity to rat EP2 receptor expressed in HEK293 cellsBinding affinity to rat EP2 receptor expressed in HEK293 cells
ChEMBL 435 10 2 4 4.4 O=C(O)c1ccc(CCCN2C(=O)CC[C@@H]2CCC(O)Cc2ccc(Cl)cc2)s1 10.1016/j.bmcl.2006.01.018
11955236 153234 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 396 10 3 3 4.5 CC(C)(CO)c1ccc([C@H]2[C@H](O)C[C@@H](Cl)[C@@H]2CCCCCCC(=O)O)cc1 nan
CHEMBL3922121 153234 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 396 10 3 3 4.5 CC(C)(CO)c1ccc([C@H]2[C@H](O)C[C@@H](Cl)[C@@H]2CCCCCCC(=O)O)cc1 nan
122180283 128410 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 403 4 0 5 4.6 COc1cc(-n2ccc3cc(F)ccc32)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586346 128410 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 403 4 0 5 4.6 COc1cc(-n2ccc3cc(F)ccc32)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
45268713 202730 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
ChEMBL 351 15 2 4 2.6 CCCCCC(O)CCCN(CCCCCC(=O)O)S(C)(=O)=O 10.1016/j.bmcl.2009.01.059
CHEMBL559560 202730 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
ChEMBL 351 15 2 4 2.6 CCCCCC(O)CCCN(CCCCCC(=O)O)S(C)(=O)=O 10.1016/j.bmcl.2009.01.059
10223499 203120 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
ChEMBL 413 15 2 4 4.1 CCCCCC(O)c1ccc(CN(CCCCCCC(=O)O)S(C)(=O)=O)cc1 10.1016/j.bmcl.2009.01.059
CHEMBL562411 203120 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
ChEMBL 413 15 2 4 4.1 CCCCCC(O)c1ccc(CN(CCCCCCC(=O)O)S(C)(=O)=O)cc1 10.1016/j.bmcl.2009.01.059
44564893 187302 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Displacement of radioligand from EP2 receptorDisplacement of radioligand from EP2 receptor
ChEMBL 554 6 1 5 6.2 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2cc(F)c(F)cc2F)c2c(Oc3ccc(Cl)cc3Cl)cccc21 10.1016/j.bmcl.2008.12.112
CHEMBL475349 187302 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Displacement of radioligand from EP2 receptorDisplacement of radioligand from EP2 receptor
ChEMBL 554 6 1 5 6.2 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2cc(F)c(F)cc2F)c2c(Oc3ccc(Cl)cc3Cl)cccc21 10.1016/j.bmcl.2008.12.112
71733912 97113 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Inhibition of beta-arrestin binding to recombinant human prostanoid EP2 receptor expressed in HEK293 cell membranes by beta-lactamase complementation assayInhibition of beta-arrestin binding to recombinant human prostanoid EP2 receptor expressed in HEK293 cell membranes by beta-lactamase complementation assay
ChEMBL 430 5 1 3 4.5 O=C(O)Cn1c2c(c3cc(F)ccc31)CN(C(=O)CCc1cccc3ccccc13)CC2 10.1021/jm400122f
CHEMBL2385903 97113 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Inhibition of beta-arrestin binding to recombinant human prostanoid EP2 receptor expressed in HEK293 cell membranes by beta-lactamase complementation assayInhibition of beta-arrestin binding to recombinant human prostanoid EP2 receptor expressed in HEK293 cell membranes by beta-lactamase complementation assay
ChEMBL 430 5 1 3 4.5 O=C(O)Cn1c2c(c3cc(F)ccc31)CN(C(=O)CCc1cccc3ccccc13)CC2 10.1021/jm400122f
44564804 183479 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Displacement of radioligand from EP2 receptorDisplacement of radioligand from EP2 receptor
ChEMBL 536 6 1 5 6.1 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2ccc(F)c(F)c2)c2c(Oc3ccc(Cl)cc3Cl)cccc21 10.1016/j.bmcl.2008.12.112
CHEMBL459885 183479 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Displacement of radioligand from EP2 receptorDisplacement of radioligand from EP2 receptor
ChEMBL 536 6 1 5 6.1 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2ccc(F)c(F)c2)c2c(Oc3ccc(Cl)cc3Cl)cccc21 10.1016/j.bmcl.2008.12.112
25114442 9835 56 None - 1 Human 8.7 pKd = 8.7 Binding
Affinity On-target Cellular interaction (Functional reporter assay (prostaglandin E2 (PGE2)-induced increase in cAMP in CHO cells expressing EP2 receptors)) EUB0000351a PTGER2Affinity On-target Cellular interaction (Functional reporter assay (prostaglandin E2 (PGE2)-induced increase in cAMP in CHO cells expressing EP2 receptors)) EUB0000351a PTGER2
ChEMBL 409 6 1 4 3.6 COc1ccc2c(c1)ccc(c2)OCC1(CN(C1)C(=O)c1ccc(cc1)F)C(=O)O 10.6019/CHEMBL5210121
5817 9835 56 None - 1 Human 8.7 pKd = 8.7 Binding
Affinity On-target Cellular interaction (Functional reporter assay (prostaglandin E2 (PGE2)-induced increase in cAMP in CHO cells expressing EP2 receptors)) EUB0000351a PTGER2Affinity On-target Cellular interaction (Functional reporter assay (prostaglandin E2 (PGE2)-induced increase in cAMP in CHO cells expressing EP2 receptors)) EUB0000351a PTGER2
ChEMBL 409 6 1 4 3.6 COc1ccc2c(c1)ccc(c2)OCC1(CN(C1)C(=O)c1ccc(cc1)F)C(=O)O 10.6019/CHEMBL5210121
CHEMBL3286797 9835 56 None - 1 Human 8.7 pKd = 8.7 Binding
Affinity On-target Cellular interaction (Functional reporter assay (prostaglandin E2 (PGE2)-induced increase in cAMP in CHO cells expressing EP2 receptors)) EUB0000351a PTGER2Affinity On-target Cellular interaction (Functional reporter assay (prostaglandin E2 (PGE2)-induced increase in cAMP in CHO cells expressing EP2 receptors)) EUB0000351a PTGER2
ChEMBL 409 6 1 4 3.6 COc1ccc2c(c1)ccc(c2)OCC1(CN(C1)C(=O)c1ccc(cc1)F)C(=O)O 10.6019/CHEMBL5210121
DB12024 9835 56 None - 1 Human 8.7 pKd = 8.7 Binding
Affinity On-target Cellular interaction (Functional reporter assay (prostaglandin E2 (PGE2)-induced increase in cAMP in CHO cells expressing EP2 receptors)) EUB0000351a PTGER2Affinity On-target Cellular interaction (Functional reporter assay (prostaglandin E2 (PGE2)-induced increase in cAMP in CHO cells expressing EP2 receptors)) EUB0000351a PTGER2
ChEMBL 409 6 1 4 3.6 COc1ccc2c(c1)ccc(c2)OCC1(CN(C1)C(=O)c1ccc(cc1)F)C(=O)O 10.6019/CHEMBL5210121
CHEMBL5281349 200889 0 None - 1 Human 7.9 pKd = 7.9 Binding
Binding affinity to human recombinant PTGER2 assessed as dissociation constant by high throughput fluorescence polarization assayBinding affinity to human recombinant PTGER2 assessed as dissociation constant by high throughput fluorescence polarization assay
ChEMBL 1581 31 10 14 8.1 CC(C)C[C@H]1CN(CC(=O)NCCC(=O)N[C@@H](CCCCNC(=S)Nc2ccccc2)C(N)=O)C(=O)CCSCc2ccc(cc2)C(=O)N[C@@H](CC(C)C)CN(C(=O)CC2CC2)CC(=O)N[C@@H](CCCCN)CN(C(=O)CCc2ccccc2)CC(=O)N[C@@H](Cc2ccccc2)CN(C(=O)CCC2CCCCC2)CC(=O)N1 10.1016/j.bmcl.2023.129255
CHEMBL5279002 200788 0 None - 1 Human 7.8 pKd = 7.8 Binding
Binding affinity to human recombinant PTGER2 assessed as dissociation constant by high throughput fluorescence polarization assayBinding affinity to human recombinant PTGER2 assessed as dissociation constant by high throughput fluorescence polarization assay
ChEMBL 1921 33 12 18 12.0 CC(C)C[C@H]1CN(CC(=O)NCCC(=O)N[C@@H](CCCCNC(=S)Nc2ccc(-c3c4ccc(=O)cc-4oc4cc(O)ccc34)c(C(=O)O)c2)C(N)=O)C(=O)CCSCc2ccc(cc2)C(=O)N[C@@H](CCCCN)CN(C(=O)CCc2ccccc2)CC(=O)N[C@@H](CC(C)C)CN(C(=O)CCC2CCCCC2)CC(=O)N[C@@H](Cc2ccccc2)CN(C(=O)Cc2ccc3ccccc3c2)CC(=O)N1 10.1016/j.bmcl.2023.129255
46213069 9837 0 None 1905 3 Human 9.2 pKi = 9.2 Binding
Binding affinity to EP2 receptor in human mast cell assessed as inhibition constantBinding affinity to EP2 receptor in human mast cell assessed as inhibition constant
ChEMBL 456 7 1 5 4.2 COc1ccc(cc1)C(=O)N1CCC(C1)(COc1ccc(cc1)c1ccc(cc1)C#N)C(=O)O 10.1021/acs.jmedchem.1c00816
8538 9837 0 None 1905 3 Human 9.2 pKi = 9.2 Binding
Binding affinity to EP2 receptor in human mast cell assessed as inhibition constantBinding affinity to EP2 receptor in human mast cell assessed as inhibition constant
ChEMBL 456 7 1 5 4.2 COc1ccc(cc1)C(=O)N1CCC(C1)(COc1ccc(cc1)c1ccc(cc1)C#N)C(=O)O 10.1021/acs.jmedchem.1c00816
CHEMBL5285583 9837 0 None 1905 3 Human 9.2 pKi = 9.2 Binding
Binding affinity to EP2 receptor in human mast cell assessed as inhibition constantBinding affinity to EP2 receptor in human mast cell assessed as inhibition constant
ChEMBL 456 7 1 5 4.2 COc1ccc(cc1)C(=O)N1CCC(C1)(COc1ccc(cc1)c1ccc(cc1)C#N)C(=O)O 10.1021/acs.jmedchem.1c00816
9807448 209951 0 None 1 4 Human 9.1 pKi = 9.1 Binding
Compound was evaluated for its competitive binding affinity towards human Prostanoid EP2 receptor in CHO cells expressing prostanoid receptorCompound was evaluated for its competitive binding affinity towards human Prostanoid EP2 receptor in CHO cells expressing prostanoid receptor
ChEMBL 398 11 3 3 4.7 CCC1([C@@H](O)C/C=C/[C@H]2[C@H](O)C[C@@H](Cl)[C@@H]2C/C=C\CCCC(=O)O)CCC1 10.1016/s0960-894x(01)00359-6
CHEMBL64246 209951 0 None 1 4 Human 9.1 pKi = 9.1 Binding
Compound was evaluated for its competitive binding affinity towards human Prostanoid EP2 receptor in CHO cells expressing prostanoid receptorCompound was evaluated for its competitive binding affinity towards human Prostanoid EP2 receptor in CHO cells expressing prostanoid receptor
ChEMBL 398 11 3 3 4.7 CCC1([C@@H](O)C/C=C/[C@H]2[C@H](O)C[C@@H](Cl)[C@@H]2C/C=C\CCCC(=O)O)CCC1 10.1016/s0960-894x(01)00359-6
1883 9856 75 None -6 24 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]PGE2 from human recombinant EP2 receptor expressed in HEK293 cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]PGE2 from human recombinant EP2 receptor expressed in HEK293 cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/acs.jmedchem.9b00336
1916 9856 75 None -6 24 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]PGE2 from human recombinant EP2 receptor expressed in HEK293 cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]PGE2 from human recombinant EP2 receptor expressed in HEK293 cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/acs.jmedchem.9b00336
5280360 9856 75 None -6 24 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]PGE2 from human recombinant EP2 receptor expressed in HEK293 cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]PGE2 from human recombinant EP2 receptor expressed in HEK293 cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/acs.jmedchem.9b00336
913 9856 75 None -6 24 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]PGE2 from human recombinant EP2 receptor expressed in HEK293 cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]PGE2 from human recombinant EP2 receptor expressed in HEK293 cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/acs.jmedchem.9b00336
CHEMBL548 9856 75 None -6 24 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]PGE2 from human recombinant EP2 receptor expressed in HEK293 cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]PGE2 from human recombinant EP2 receptor expressed in HEK293 cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/acs.jmedchem.9b00336
DB00917 9856 75 None -6 24 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]PGE2 from human recombinant EP2 receptor expressed in HEK293 cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]PGE2 from human recombinant EP2 receptor expressed in HEK293 cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/acs.jmedchem.9b00336
51039069 135981 0 None - 1 Human 9.0 pKi = 9.0 Binding
Binding Assay: Measurement of EP2 receptor binding affinity was carried out according to the method of Abramovitz et al. (Biochimica et Biophysica Acta, 1483, 285 (2000)). A test compound dissolved in dimethylsulfoxide and [3H]PGE2 (NET-428, available from PerkinElmer Inc.) (final concentration: 10 nM) were added to a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2, 1 mM EDTA) in which 10 μg of a membrane fraction (ES-562-M, available from Euroscreen S.A.) of HEK293 cells expressing human EP2 receptor had been suspended, followed by incubation at 30° C. for 60 minutes. The membrane fraction was recovered on glass fiber filter paper (GF/B, available from Whatman PLC) using a cell harvester (M30R, available from Brandel Inc.), and after washing with a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2), radioactivity was measured with a liquid scintillation analyzer (2000CA, available from Packard).Binding Assay: Measurement of EP2 receptor binding affinity was carried out according to the method of Abramovitz et al. (Biochimica et Biophysica Acta, 1483, 285 (2000)). A test compound dissolved in dimethylsulfoxide and [3H]PGE2 (NET-428, available from PerkinElmer Inc.) (final concentration: 10 nM) were added to a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2, 1 mM EDTA) in which 10 μg of a membrane fraction (ES-562-M, available from Euroscreen S.A.) of HEK293 cells expressing human EP2 receptor had been suspended, followed by incubation at 30° C. for 60 minutes. The membrane fraction was recovered on glass fiber filter paper (GF/B, available from Whatman PLC) using a cell harvester (M30R, available from Brandel Inc.), and after washing with a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2), radioactivity was measured with a liquid scintillation analyzer (2000CA, available from Packard).
ChEMBL 419 6 4 4 4.1 O=C(NO)c1ccc(CNC(=O)c2[nH]c(-c3ccoc3)cc2-c2ccc(F)cc2)cc1 nan
CHEMBL3670659 135981 0 None - 1 Human 9.0 pKi = 9.0 Binding
Binding Assay: Measurement of EP2 receptor binding affinity was carried out according to the method of Abramovitz et al. (Biochimica et Biophysica Acta, 1483, 285 (2000)). A test compound dissolved in dimethylsulfoxide and [3H]PGE2 (NET-428, available from PerkinElmer Inc.) (final concentration: 10 nM) were added to a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2, 1 mM EDTA) in which 10 μg of a membrane fraction (ES-562-M, available from Euroscreen S.A.) of HEK293 cells expressing human EP2 receptor had been suspended, followed by incubation at 30° C. for 60 minutes. The membrane fraction was recovered on glass fiber filter paper (GF/B, available from Whatman PLC) using a cell harvester (M30R, available from Brandel Inc.), and after washing with a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2), radioactivity was measured with a liquid scintillation analyzer (2000CA, available from Packard).Binding Assay: Measurement of EP2 receptor binding affinity was carried out according to the method of Abramovitz et al. (Biochimica et Biophysica Acta, 1483, 285 (2000)). A test compound dissolved in dimethylsulfoxide and [3H]PGE2 (NET-428, available from PerkinElmer Inc.) (final concentration: 10 nM) were added to a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2, 1 mM EDTA) in which 10 μg of a membrane fraction (ES-562-M, available from Euroscreen S.A.) of HEK293 cells expressing human EP2 receptor had been suspended, followed by incubation at 30° C. for 60 minutes. The membrane fraction was recovered on glass fiber filter paper (GF/B, available from Whatman PLC) using a cell harvester (M30R, available from Brandel Inc.), and after washing with a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2), radioactivity was measured with a liquid scintillation analyzer (2000CA, available from Packard).
ChEMBL 419 6 4 4 4.1 O=C(NO)c1ccc(CNC(=O)c2[nH]c(-c3ccoc3)cc2-c2ccc(F)cc2)cc1 nan
51039071 135985 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding Assay: Measurement of EP2 receptor binding affinity was carried out according to the method of Abramovitz et al. (Biochimica et Biophysica Acta, 1483, 285 (2000)). A test compound dissolved in dimethylsulfoxide and [3H]PGE2 (NET-428, available from PerkinElmer Inc.) (final concentration: 10 nM) were added to a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2, 1 mM EDTA) in which 10 μg of a membrane fraction (ES-562-M, available from Euroscreen S.A.) of HEK293 cells expressing human EP2 receptor had been suspended, followed by incubation at 30° C. for 60 minutes. The membrane fraction was recovered on glass fiber filter paper (GF/B, available from Whatman PLC) using a cell harvester (M30R, available from Brandel Inc.), and after washing with a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2), radioactivity was measured with a liquid scintillation analyzer (2000CA, available from Packard).Binding Assay: Measurement of EP2 receptor binding affinity was carried out according to the method of Abramovitz et al. (Biochimica et Biophysica Acta, 1483, 285 (2000)). A test compound dissolved in dimethylsulfoxide and [3H]PGE2 (NET-428, available from PerkinElmer Inc.) (final concentration: 10 nM) were added to a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2, 1 mM EDTA) in which 10 μg of a membrane fraction (ES-562-M, available from Euroscreen S.A.) of HEK293 cells expressing human EP2 receptor had been suspended, followed by incubation at 30° C. for 60 minutes. The membrane fraction was recovered on glass fiber filter paper (GF/B, available from Whatman PLC) using a cell harvester (M30R, available from Brandel Inc.), and after washing with a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2), radioactivity was measured with a liquid scintillation analyzer (2000CA, available from Packard).
ChEMBL 419 6 4 4 4.1 O=C(NO)c1ccc(CNC(=O)c2[nH]c(-c3ccccc3)cc2-c2ccc(F)cc2)o1 nan
CHEMBL3670663 135985 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding Assay: Measurement of EP2 receptor binding affinity was carried out according to the method of Abramovitz et al. (Biochimica et Biophysica Acta, 1483, 285 (2000)). A test compound dissolved in dimethylsulfoxide and [3H]PGE2 (NET-428, available from PerkinElmer Inc.) (final concentration: 10 nM) were added to a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2, 1 mM EDTA) in which 10 μg of a membrane fraction (ES-562-M, available from Euroscreen S.A.) of HEK293 cells expressing human EP2 receptor had been suspended, followed by incubation at 30° C. for 60 minutes. The membrane fraction was recovered on glass fiber filter paper (GF/B, available from Whatman PLC) using a cell harvester (M30R, available from Brandel Inc.), and after washing with a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2), radioactivity was measured with a liquid scintillation analyzer (2000CA, available from Packard).Binding Assay: Measurement of EP2 receptor binding affinity was carried out according to the method of Abramovitz et al. (Biochimica et Biophysica Acta, 1483, 285 (2000)). A test compound dissolved in dimethylsulfoxide and [3H]PGE2 (NET-428, available from PerkinElmer Inc.) (final concentration: 10 nM) were added to a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2, 1 mM EDTA) in which 10 μg of a membrane fraction (ES-562-M, available from Euroscreen S.A.) of HEK293 cells expressing human EP2 receptor had been suspended, followed by incubation at 30° C. for 60 minutes. The membrane fraction was recovered on glass fiber filter paper (GF/B, available from Whatman PLC) using a cell harvester (M30R, available from Brandel Inc.), and after washing with a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2), radioactivity was measured with a liquid scintillation analyzer (2000CA, available from Packard).
ChEMBL 419 6 4 4 4.1 O=C(NO)c1ccc(CNC(=O)c2[nH]c(-c3ccccc3)cc2-c2ccc(F)cc2)o1 nan
10481859 81942 0 None -4 3 Mouse 8.8 pKi = 8.8 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 522 10 2 6 5.4 Cc1ccc(-c2cccc(C[C@H](O)/C=C/[C@H]3CCC(=O)N3CCSc3nc(C(=O)O)cs3)c2)cc1C 10.1016/j.bmc.2012.04.008
CHEMBL2036321 81942 0 None -4 3 Mouse 8.8 pKi = 8.8 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 522 10 2 6 5.4 Cc1ccc(-c2cccc(C[C@H](O)/C=C/[C@H]3CCC(=O)N3CCSc3nc(C(=O)O)cs3)c2)cc1C 10.1016/j.bmc.2012.04.008
1932 9716 5 None 1 6 Human 8.8 pKi = 8.8 Binding
Binding affinity to EP2 receptor (unknown origin) by competitive binding assayBinding affinity to EP2 receptor (unknown origin) by competitive binding assay
ChEMBL 410 12 3 3 4.8 C=CCC1(CCC1)[C@H](C/C=C/[C@H]1[C@H](O)C[C@H]([C@@H]1C/C=C\CCCC(=O)O)Cl)O 10.1021/jm401431x
5311228 9716 5 None 1 6 Human 8.8 pKi = 8.8 Binding
Binding affinity to EP2 receptor (unknown origin) by competitive binding assayBinding affinity to EP2 receptor (unknown origin) by competitive binding assay
ChEMBL 410 12 3 3 4.8 C=CCC1(CCC1)[C@H](C/C=C/[C@H]1[C@H](O)C[C@H]([C@@H]1C/C=C\CCCC(=O)O)Cl)O 10.1021/jm401431x
CHEMBL3286796 9716 5 None 1 6 Human 8.8 pKi = 8.8 Binding
Binding affinity to EP2 receptor (unknown origin) by competitive binding assayBinding affinity to EP2 receptor (unknown origin) by competitive binding assay
ChEMBL 410 12 3 3 4.8 C=CCC1(CCC1)[C@H](C/C=C/[C@H]1[C@H](O)C[C@H]([C@@H]1C/C=C\CCCC(=O)O)Cl)O 10.1021/jm401431x
1883 9856 75 None -6 24 Human 8.8 pKi = 8.8 Binding
Binding affinity to human prostanoid EP2 receptor by radioligand displacement assayBinding affinity to human prostanoid EP2 receptor by radioligand displacement assay
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.ejmech.2013.01.044
1916 9856 75 None -6 24 Human 8.8 pKi = 8.8 Binding
Binding affinity to human prostanoid EP2 receptor by radioligand displacement assayBinding affinity to human prostanoid EP2 receptor by radioligand displacement assay
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.ejmech.2013.01.044
5280360 9856 75 None -6 24 Human 8.8 pKi = 8.8 Binding
Binding affinity to human prostanoid EP2 receptor by radioligand displacement assayBinding affinity to human prostanoid EP2 receptor by radioligand displacement assay
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.ejmech.2013.01.044
913 9856 75 None -6 24 Human 8.8 pKi = 8.8 Binding
Binding affinity to human prostanoid EP2 receptor by radioligand displacement assayBinding affinity to human prostanoid EP2 receptor by radioligand displacement assay
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.ejmech.2013.01.044
CHEMBL548 9856 75 None -6 24 Human 8.8 pKi = 8.8 Binding
Binding affinity to human prostanoid EP2 receptor by radioligand displacement assayBinding affinity to human prostanoid EP2 receptor by radioligand displacement assay
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.ejmech.2013.01.044
DB00917 9856 75 None -6 24 Human 8.8 pKi = 8.8 Binding
Binding affinity to human prostanoid EP2 receptor by radioligand displacement assayBinding affinity to human prostanoid EP2 receptor by radioligand displacement assay
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.ejmech.2013.01.044
57384034 78082 0 None -2 3 Mouse 8.8 pKi = 8.8 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 528 10 2 6 5.4 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(-c3ccc(Cl)cc3)c2)n1 10.1016/j.bmc.2012.02.018
CHEMBL1957436 78082 0 None -2 3 Mouse 8.8 pKi = 8.8 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 528 10 2 6 5.4 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(-c3ccc(Cl)cc3)c2)n1 10.1016/j.bmc.2012.02.018
57384034 78082 0 None -2 3 Mouse 8.8 pKi = 8.8 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 528 10 2 6 5.4 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(-c3ccc(Cl)cc3)c2)n1 10.1016/j.bmc.2012.04.008
CHEMBL1957436 78082 0 None -2 3 Mouse 8.8 pKi = 8.8 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 528 10 2 6 5.4 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(-c3ccc(Cl)cc3)c2)n1 10.1016/j.bmc.2012.04.008
67078793 135975 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding Assay: Measurement of EP2 receptor binding affinity was carried out according to the method of Abramovitz et al. (Biochimica et Biophysica Acta, 1483, 285 (2000)). A test compound dissolved in dimethylsulfoxide and [3H]PGE2 (NET-428, available from PerkinElmer Inc.) (final concentration: 10 nM) were added to a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2, 1 mM EDTA) in which 10 μg of a membrane fraction (ES-562-M, available from Euroscreen S.A.) of HEK293 cells expressing human EP2 receptor had been suspended, followed by incubation at 30° C. for 60 minutes. The membrane fraction was recovered on glass fiber filter paper (GF/B, available from Whatman PLC) using a cell harvester (M30R, available from Brandel Inc.), and after washing with a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2), radioactivity was measured with a liquid scintillation analyzer (2000CA, available from Packard).Binding Assay: Measurement of EP2 receptor binding affinity was carried out according to the method of Abramovitz et al. (Biochimica et Biophysica Acta, 1483, 285 (2000)). A test compound dissolved in dimethylsulfoxide and [3H]PGE2 (NET-428, available from PerkinElmer Inc.) (final concentration: 10 nM) were added to a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2, 1 mM EDTA) in which 10 μg of a membrane fraction (ES-562-M, available from Euroscreen S.A.) of HEK293 cells expressing human EP2 receptor had been suspended, followed by incubation at 30° C. for 60 minutes. The membrane fraction was recovered on glass fiber filter paper (GF/B, available from Whatman PLC) using a cell harvester (M30R, available from Brandel Inc.), and after washing with a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2), radioactivity was measured with a liquid scintillation analyzer (2000CA, available from Packard).
ChEMBL 287 3 2 2 4.2 O=C(O)c1[nH]c(-c2cccs2)cc1-c1ccc(F)cc1 nan
CHEMBL3670653 135975 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding Assay: Measurement of EP2 receptor binding affinity was carried out according to the method of Abramovitz et al. (Biochimica et Biophysica Acta, 1483, 285 (2000)). A test compound dissolved in dimethylsulfoxide and [3H]PGE2 (NET-428, available from PerkinElmer Inc.) (final concentration: 10 nM) were added to a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2, 1 mM EDTA) in which 10 μg of a membrane fraction (ES-562-M, available from Euroscreen S.A.) of HEK293 cells expressing human EP2 receptor had been suspended, followed by incubation at 30° C. for 60 minutes. The membrane fraction was recovered on glass fiber filter paper (GF/B, available from Whatman PLC) using a cell harvester (M30R, available from Brandel Inc.), and after washing with a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2), radioactivity was measured with a liquid scintillation analyzer (2000CA, available from Packard).Binding Assay: Measurement of EP2 receptor binding affinity was carried out according to the method of Abramovitz et al. (Biochimica et Biophysica Acta, 1483, 285 (2000)). A test compound dissolved in dimethylsulfoxide and [3H]PGE2 (NET-428, available from PerkinElmer Inc.) (final concentration: 10 nM) were added to a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2, 1 mM EDTA) in which 10 μg of a membrane fraction (ES-562-M, available from Euroscreen S.A.) of HEK293 cells expressing human EP2 receptor had been suspended, followed by incubation at 30° C. for 60 minutes. The membrane fraction was recovered on glass fiber filter paper (GF/B, available from Whatman PLC) using a cell harvester (M30R, available from Brandel Inc.), and after washing with a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2), radioactivity was measured with a liquid scintillation analyzer (2000CA, available from Packard).
ChEMBL 287 3 2 2 4.2 O=C(O)c1[nH]c(-c2cccs2)cc1-c1ccc(F)cc1 nan
18376177 10525 50 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity to EP2 receptor (unknown origin) by competitive binding assayBinding affinity to EP2 receptor (unknown origin) by competitive binding assay
ChEMBL 478 10 1 7 3.1 OC(=O)COc1cccc(c1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)n1cccn1 10.1021/jm401431x
5816 10525 50 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity to EP2 receptor (unknown origin) by competitive binding assayBinding affinity to EP2 receptor (unknown origin) by competitive binding assay
ChEMBL 478 10 1 7 3.1 OC(=O)COc1cccc(c1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)n1cccn1 10.1021/jm401431x
CHEMBL2107783 10525 50 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity to EP2 receptor (unknown origin) by competitive binding assayBinding affinity to EP2 receptor (unknown origin) by competitive binding assay
ChEMBL 478 10 1 7 3.1 OC(=O)COc1cccc(c1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)n1cccn1 10.1021/jm401431x
DB12623 10525 50 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity to EP2 receptor (unknown origin) by competitive binding assayBinding affinity to EP2 receptor (unknown origin) by competitive binding assay
ChEMBL 478 10 1 7 3.1 OC(=O)COc1cccc(c1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)n1cccn1 10.1021/jm401431x
11855865 160056 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 445 12 2 5 5.2 CCCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3977724 160056 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 445 12 2 5 5.2 CCCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
10116114 132664 0 None -28 8 Mouse 7.0 pKi = 7 Binding
Ability to inhibit the binding of [3H]-PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP2Ability to inhibit the binding of [3H]-PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP2
ChEMBL 470 6 1 6 4.5 Cc1cc2c(CC(=O)O)cccc2n1C(=O)c1ccc(OC[C@@H]2CN(C)c3ccccc3O2)cc1 10.1016/j.bmcl.2004.07.039
CHEMBL364841 132664 0 None -28 8 Mouse 7.0 pKi = 7 Binding
Ability to inhibit the binding of [3H]-PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP2Ability to inhibit the binding of [3H]-PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP2
ChEMBL 470 6 1 6 4.5 Cc1cc2c(CC(=O)O)cccc2n1C(=O)c1ccc(OC[C@@H]2CN(C)c3ccccc3O2)cc1 10.1016/j.bmcl.2004.07.039
13231966 107728 0 None -141 5 Mouse 7.0 pKi = 7 Binding
Affinity for mouse Prostanoid EP2 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP2 receptor expressed in CHO cells
ChEMBL 372 13 3 5 3.2 CCCCC[C@H](O)/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1SCCCCCC(=O)O 10.1016/s0960-894x(01)00365-1
CHEMBL294108 107728 0 None -141 5 Mouse 7.0 pKi = 7 Binding
Affinity for mouse Prostanoid EP2 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP2 receptor expressed in CHO cells
ChEMBL 372 13 3 5 3.2 CCCCC[C@H](O)/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1SCCCCCC(=O)O 10.1016/s0960-894x(01)00365-1
13231966 107728 0 None -141 5 Mouse 7.0 pKi = 7 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptor
ChEMBL 372 13 3 5 3.2 CCCCC[C@H](O)/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1SCCCCCC(=O)O 10.1016/s0960-894x(01)00364-x
CHEMBL294108 107728 0 None -141 5 Mouse 7.0 pKi = 7 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptor
ChEMBL 372 13 3 5 3.2 CCCCC[C@H](O)/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1SCCCCCC(=O)O 10.1016/s0960-894x(01)00364-x
44455046 102502 0 None -50118 2 Human 6.0 pKi = 6 Binding
Displacement of [3H]PGE2 from human EP2 receptorDisplacement of [3H]PGE2 from human EP2 receptor
ChEMBL 413 8 2 3 3.7 O=C(O)c1ccc(CCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2007.11.020
CHEMBL258332 102502 0 None -50118 2 Human 6.0 pKi = 6 Binding
Displacement of [3H]PGE2 from human EP2 receptorDisplacement of [3H]PGE2 from human EP2 receptor
ChEMBL 413 8 2 3 3.7 O=C(O)c1ccc(CCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2007.11.020
44304057 210038 0 None -288 4 Mouse 6.0 pKi = 6 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptor
ChEMBL 390 13 3 6 2.6 CCCCC[C@H](O)/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CSCCSCC(=O)O 10.1016/s0960-894x(01)00364-x
CHEMBL64598 210038 0 None -288 4 Mouse 6.0 pKi = 6 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptor
ChEMBL 390 13 3 6 2.6 CCCCC[C@H](O)/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CSCCSCC(=O)O 10.1016/s0960-894x(01)00364-x
10181606 213130 0 None -645 7 Human 5.0 pKi = 5 Binding
Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 437 5 1 4 5.2 O=C(/C=C/c1ccccc1-c1ccc(Cl)c(Cl)c1)NS(=O)(=O)c1cccs1 10.1016/s0960-894x(03)00794-7
CHEMBL87371 213130 0 None -645 7 Human 5.0 pKi = 5 Binding
Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 437 5 1 4 5.2 O=C(/C=C/c1ccccc1-c1ccc(Cl)c(Cl)c1)NS(=O)(=O)c1cccs1 10.1016/s0960-894x(03)00794-7
118517483 151049 0 None -93 2 Human 6.0 pKi = 6.0 Binding
Radioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations wRadioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations w
ChEMBL 396 8 2 3 4.2 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2ccccc2F)cc1 nan
CHEMBL3904946 151049 0 None -93 2 Human 6.0 pKi = 6.0 Binding
Radioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations wRadioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations w
ChEMBL 396 8 2 3 4.2 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2ccccc2F)cc1 nan
71455094 88656 0 None -407 4 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]PGE2 from human EP2R expressed in chem1 cells after 2hrs by beta countingDisplacement of [3H]PGE2 from human EP2R expressed in chem1 cells after 2hrs by beta counting
ChEMBL 623 12 1 8 6.4 COc1cc(C/C=C/c2ccccc2/C=C/C(=O)NS(=O)(=O)c2cccs2)ccc1OCCn1cc2ccccc2c1C#N 10.1021/ml300191g
CHEMBL2164609 88656 0 None -407 4 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]PGE2 from human EP2R expressed in chem1 cells after 2hrs by beta countingDisplacement of [3H]PGE2 from human EP2R expressed in chem1 cells after 2hrs by beta counting
ChEMBL 623 12 1 8 6.4 COc1cc(C/C=C/c2ccccc2/C=C/C(=O)NS(=O)(=O)c2cccs2)ccc1OCCn1cc2ccccc2c1C#N 10.1021/ml300191g
44303627 209984 0 None 467 2 Mouse 8.0 pKi = 8.0 Binding
Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.
ChEMBL 364 11 3 3 4.5 CCC1([C@@H](O)C/C=C/[C@H]2[C@H](O)CC[C@@H]2C/C=C\CCCC(=O)O)CCC1 10.1016/s0960-894x(01)00359-6
CHEMBL64358 209984 0 None 467 2 Mouse 8.0 pKi = 8.0 Binding
Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.
ChEMBL 364 11 3 3 4.5 CCC1([C@@H](O)C/C=C/[C@H]2[C@H](O)CC[C@@H]2C/C=C\CCCC(=O)O)CCC1 10.1016/s0960-894x(01)00359-6
5311035 104579 29 None -4 9 Human 7.0 pKi = 7.0 Binding
Binding affinity at human prostaglandin EP2 receptorBinding affinity at human prostaglandin EP2 receptor
ChEMBL 408 13 2 5 4.3 CCCC1([C@H](O)C/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2CCCCCCC(=O)OC)CCC1 10.1016/j.bmcl.2007.09.074
CHEMBL271896 104579 29 None -4 9 Human 7.0 pKi = 7.0 Binding
Binding affinity at human prostaglandin EP2 receptorBinding affinity at human prostaglandin EP2 receptor
ChEMBL 408 13 2 5 4.3 CCCC1([C@H](O)C/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2CCCCCCC(=O)OC)CCC1 10.1016/j.bmcl.2007.09.074
52941778 23314 0 None -1 3 Human 7.0 pKi = 7.0 Binding
Binding affinity for human prostanoid EP2 receptorBinding affinity for human prostanoid EP2 receptor
ChEMBL 712 14 2 4 11.7 O=C(O)/C=C/c1ccccc1/C=C/Cc1ccccc1Oc1ccccc1.O=C(O)/C=C/c1ccccc1C/C=C\c1ccccc1Oc1ccccc1 10.1016/j.bmcl.2004.11.051
CHEMBL1237304 23314 0 None -1 3 Human 7.0 pKi = 7.0 Binding
Binding affinity for human prostanoid EP2 receptorBinding affinity for human prostanoid EP2 receptor
ChEMBL 712 14 2 4 11.7 O=C(O)/C=C/c1ccccc1/C=C/Cc1ccccc1Oc1ccccc1.O=C(O)/C=C/c1ccccc1C/C=C\c1ccccc1Oc1ccccc1 10.1016/j.bmcl.2004.11.051
5311035 104579 29 None -4 9 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]PGE2 from human EP2 receptorDisplacement of [3H]PGE2 from human EP2 receptor
ChEMBL 408 13 2 5 4.3 CCCC1([C@H](O)C/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2CCCCCCC(=O)OC)CCC1 10.1016/j.bmcl.2007.11.020
CHEMBL271896 104579 29 None -4 9 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]PGE2 from human EP2 receptorDisplacement of [3H]PGE2 from human EP2 receptor
ChEMBL 408 13 2 5 4.3 CCCC1([C@H](O)C/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2CCCCCCC(=O)OC)CCC1 10.1016/j.bmcl.2007.11.020
44390782 71377 0 None -57 3 Human 6.0 pKi = 6.0 Binding
Binding affinity for human prostanoid EP2 receptorBinding affinity for human prostanoid EP2 receptor
ChEMBL 402 10 1 3 5.5 COc1cccc(CCCc2ccccc2/C=C/C(=O)O)c1OCc1ccccc1 10.1016/j.bmcl.2004.11.051
CHEMBL181691 71377 0 None -57 3 Human 6.0 pKi = 6.0 Binding
Binding affinity for human prostanoid EP2 receptorBinding affinity for human prostanoid EP2 receptor
ChEMBL 402 10 1 3 5.5 COc1cccc(CCCc2ccccc2/C=C/C(=O)O)c1OCc1ccccc1 10.1016/j.bmcl.2004.11.051
44303907 209520 0 None - 1 Mouse 6.0 pKi = 6.0 Binding
Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.
ChEMBL 390 10 3 4 3.5 CCCC1([C@@H](O)C/C=C/C2[C@H](O)CC(=O)[C@@H]2CC#CCCCC(=O)O)CCC1 10.1016/s0960-894x(01)00359-6
CHEMBL61925 209520 0 None - 1 Mouse 6.0 pKi = 6.0 Binding
Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.
ChEMBL 390 10 3 4 3.5 CCCC1([C@@H](O)C/C=C/C2[C@H](O)CC(=O)[C@@H]2CC#CCCCC(=O)O)CCC1 10.1016/s0960-894x(01)00359-6
10431288 76141 0 None -1318 3 Mouse 6.0 pKi = 6.0 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counterDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counter
ChEMBL 403 12 2 3 4.5 CCc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=S)N2CCCCCCC(=O)O)c1 10.1016/j.bmc.2011.12.009
CHEMBL1929546 76141 0 None -1318 3 Mouse 6.0 pKi = 6.0 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counterDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counter
ChEMBL 403 12 2 3 4.5 CCc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=S)N2CCCCCCC(=O)O)c1 10.1016/j.bmc.2011.12.009
46201043 207361 0 None -5011 3 Mouse 6.0 pKi = 6.0 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 453 9 2 3 5.9 C[C@@H](NC(=O)c1cc(COc2ccccc2)ccc1CCC(=O)O)c1cccc2ccccc12 10.1016/j.bmc.2009.11.023
CHEMBL599154 207361 0 None -5011 3 Mouse 6.0 pKi = 6.0 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 453 9 2 3 5.9 C[C@@H](NC(=O)c1cc(COc2ccccc2)ccc1CCC(=O)O)c1cccc2ccccc12 10.1016/j.bmc.2009.11.023
9939791 168697 0 None -912 8 Human 5.0 pKi = 5.0 Binding
Affinity at human EP2 receptor.Affinity at human EP2 receptor.
ChEMBL 684 8 1 5 7.2 CO[C@](C(=O)NS(=O)(=O)c1ccccc1-c1ccc(CN2C(=O)c3ccccc3CCc3ccccc32)cc1)(c1ccccc1)C(F)(F)F 10.1016/s0960-894x(99)00465-5
CHEMBL415310 168697 0 None -912 8 Human 5.0 pKi = 5.0 Binding
Affinity at human EP2 receptor.Affinity at human EP2 receptor.
ChEMBL 684 8 1 5 7.2 CO[C@](C(=O)NS(=O)(=O)c1ccccc1-c1ccc(CN2C(=O)c3ccccc3CCc3ccccc32)cc1)(c1ccccc1)C(F)(F)F 10.1016/s0960-894x(99)00465-5
9873528 213709 0 None -72 4 Human 5.0 pKi = 5.0 Binding
Affinity at human EP2 receptor.Affinity at human EP2 receptor.
ChEMBL 602 7 1 5 6.9 O=C(NS(=O)(=O)c1ccccc1-c1ccc(CN2C(=O)c3ccccc3CCc3ccccc32)cc1)OCc1ccccc1 10.1016/s0960-894x(99)00465-5
CHEMBL91063 213709 0 None -72 4 Human 5.0 pKi = 5.0 Binding
Affinity at human EP2 receptor.Affinity at human EP2 receptor.
ChEMBL 602 7 1 5 6.9 O=C(NS(=O)(=O)c1ccccc1-c1ccc(CN2C(=O)c3ccccc3CCc3ccccc32)cc1)OCc1ccccc1 10.1016/s0960-894x(99)00465-5
134155748 157948 0 None 25 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 400 12 2 4 4.7 CCCCCC(=O)c1ccc([C@H]2[C@H](O)CC(=O)[C@@H]2C/C=C\CCCC(=O)O)cc1 nan
CHEMBL3959653 157948 0 None 25 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 400 12 2 4 4.7 CCCCCC(=O)c1ccc([C@H]2[C@H](O)CC(=O)[C@@H]2C/C=C\CCCC(=O)O)cc1 nan
11502897 149571 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 mins
ChEMBL 431 11 2 5 4.8 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3892847 149571 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 mins
ChEMBL 431 11 2 5 4.8 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
11502897 149571 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 431 11 2 5 4.8 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3892847 149571 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 431 11 2 5 4.8 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
119461 7108 72 None -3 10 Human 5.9 pKi = 5.9 Binding
Inhibition of EP2 receptor (unknown origin) by competitive binding assayInhibition of EP2 receptor (unknown origin) by competitive binding assay
ChEMBL 298 3 1 4 3.4 CC(Oc1ccc2c(c1)oc1c(c2=O)cc(cc1)C(=O)O)C 10.1021/jm401431x
1896 7108 72 None -3 10 Human 5.9 pKi = 5.9 Binding
Inhibition of EP2 receptor (unknown origin) by competitive binding assayInhibition of EP2 receptor (unknown origin) by competitive binding assay
ChEMBL 298 3 1 4 3.4 CC(Oc1ccc2c(c1)oc1c(c2=O)cc(cc1)C(=O)O)C 10.1021/jm401431x
CHEMBL1317823 7108 72 None -3 10 Human 5.9 pKi = 5.9 Binding
Inhibition of EP2 receptor (unknown origin) by competitive binding assayInhibition of EP2 receptor (unknown origin) by competitive binding assay
ChEMBL 298 3 1 4 3.4 CC(Oc1ccc2c(c1)oc1c(c2=O)cc(cc1)C(=O)O)C 10.1021/jm401431x
118517359 151174 0 None -114 2 Human 5.9 pKi = 5.9 Binding
Radioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations wRadioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations w
ChEMBL 456 8 2 3 4.8 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2cccc(Br)c2)cc1 nan
CHEMBL3906016 151174 0 None -114 2 Human 5.9 pKi = 5.9 Binding
Radioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations wRadioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations w
ChEMBL 456 8 2 3 4.8 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2cccc(Br)c2)cc1 nan
24952927 208010 0 None -851 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]PGE2 from human EP2 receptor expressed in HEK293-EBNA cells by scintillation countingDisplacement of [3H]PGE2 from human EP2 receptor expressed in HEK293-EBNA cells by scintillation counting
ChEMBL 461 6 2 3 6.2 Cc1sc(C)c(C(=O)N[C@@H](C)c2ccc(C(=O)O)cc2)c1Cc1ccc(C(F)(F)F)cc1 10.1021/jm901771h
CHEMBL603690 208010 0 None -851 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]PGE2 from human EP2 receptor expressed in HEK293-EBNA cells by scintillation countingDisplacement of [3H]PGE2 from human EP2 receptor expressed in HEK293-EBNA cells by scintillation counting
ChEMBL 461 6 2 3 6.2 Cc1sc(C)c(C(=O)N[C@@H](C)c2ccc(C(=O)O)cc2)c1Cc1ccc(C(F)(F)F)cc1 10.1021/jm901771h
44304404 107357 0 None -23 4 Mouse 7.9 pKi = 7.9 Binding
Affinity for mouse Prostanoid EP2 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP2 receptor expressed in CHO cells
ChEMBL 436 12 3 4 4.1 COCc1cccc(C[C@H](O)/C=C/[C@H]2[C@H](O)C[C@@H](Cl)[C@@H]2C/C=C/CCCC(=O)O)c1 10.1016/s0960-894x(01)00365-1
CHEMBL291630 107357 0 None -23 4 Mouse 7.9 pKi = 7.9 Binding
Affinity for mouse Prostanoid EP2 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP2 receptor expressed in CHO cells
ChEMBL 436 12 3 4 4.1 COCc1cccc(C[C@H](O)/C=C/[C@H]2[C@H](O)C[C@@H](Cl)[C@@H]2C/C=C/CCCC(=O)O)c1 10.1016/s0960-894x(01)00365-1
10291963 91483 0 None -74 6 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]PGE2 from human EP2 receptorDisplacement of [3H]PGE2 from human EP2 receptor
ChEMBL 359 10 2 3 3.4 CCCCC[C@H](O)/C=C/[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.11.020
CHEMBL222715 91483 0 None -74 6 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]PGE2 from human EP2 receptorDisplacement of [3H]PGE2 from human EP2 receptor
ChEMBL 359 10 2 3 3.4 CCCCC[C@H](O)/C=C/[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.11.020
44520989 206543 0 None -2 3 Mouse 5.9 pKi = 5.9 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 396 6 2 4 5.0 Cc1c(C)c2c(c(C)c1O)CCC(C)(CCOc1ccccc1/C=C/C(=O)O)O2 10.1016/j.bmc.2009.08.007
CHEMBL593764 206543 0 None -2 3 Mouse 5.9 pKi = 5.9 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 396 6 2 4 5.0 Cc1c(C)c2c(c(C)c1O)CCC(C)(CCOc1ccccc1/C=C/C(=O)O)O2 10.1016/j.bmc.2009.08.007
23016719 207999 0 None -1 2 Mouse 5.9 pKi = 5.9 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 424 9 1 3 6.1 O=C(O)/C=C/c1ccc(OCc2ccccc2)cc1OCCc1ccc2ccccc2c1 10.1016/j.bmc.2009.08.007
CHEMBL603625 207999 0 None -1 2 Mouse 5.9 pKi = 5.9 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 424 9 1 3 6.1 O=C(O)/C=C/c1ccc(OCc2ccccc2)cc1OCCc1ccc2ccccc2c1 10.1016/j.bmc.2009.08.007
44304055 109500 0 None -371 4 Mouse 5.9 pKi = 5.9 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptor
ChEMBL 390 13 3 6 2.7 CCCCC[C@H](O)/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1SCCSCCC(=O)O 10.1016/s0960-894x(01)00364-x
CHEMBL304887 109500 0 None -371 4 Mouse 5.9 pKi = 5.9 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptor
ChEMBL 390 13 3 6 2.7 CCCCC[C@H](O)/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1SCCSCCC(=O)O 10.1016/s0960-894x(01)00364-x
44304034 207373 0 None -165 3 Mouse 5.9 pKi = 5.9 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptor
ChEMBL 424 11 3 6 2.7 Cc1ccc(C[C@H](O)/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2SCCCSCC(=O)O)cc1 10.1016/s0960-894x(01)00364-x
CHEMBL59921 207373 0 None -165 3 Mouse 5.9 pKi = 5.9 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptor
ChEMBL 424 11 3 6 2.7 Cc1ccc(C[C@H](O)/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2SCCCSCC(=O)O)cc1 10.1016/s0960-894x(01)00364-x
9817405 172182 5 None -165 6 Human 4.9 pKi = 4.9 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 288 4 1 1 4.5 O=C(O)/C=C/c1ccccc1Cc1ccc2ccccc2c1 10.1016/j.bmcl.2006.08.025
CHEMBL423815 172182 5 None -165 6 Human 4.9 pKi = 4.9 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 288 4 1 1 4.5 O=C(O)/C=C/c1ccccc1Cc1ccc2ccccc2c1 10.1016/j.bmcl.2006.08.025
72695027 113043 0 None -28 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-PGE2 from human EP2 receptor by liquid scintillation counting analysisDisplacement of [3H]-PGE2 from human EP2 receptor by liquid scintillation counting analysis
ChEMBL 396 8 2 4 3.5 C[C@H](NC(=O)[C@H]1CCCCN1CCOc1ccccc1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2015.05.091
CHEMBL3115074 113043 0 None -28 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-PGE2 from human EP2 receptor by liquid scintillation counting analysisDisplacement of [3H]-PGE2 from human EP2 receptor by liquid scintillation counting analysis
ChEMBL 396 8 2 4 3.5 C[C@H](NC(=O)[C@H]1CCCCN1CCOc1ccccc1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2015.05.091
CHEMBL3138992 113043 0 None -28 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-PGE2 from human EP2 receptor by liquid scintillation counting analysisDisplacement of [3H]-PGE2 from human EP2 receptor by liquid scintillation counting analysis
ChEMBL 396 8 2 4 3.5 C[C@H](NC(=O)[C@H]1CCCCN1CCOc1ccccc1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2015.05.091
72706947 181443 20 None -5128 3 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]PGE2 from human recombinant EP2 receptor expressed in HEK293 cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]PGE2 from human recombinant EP2 receptor expressed in HEK293 cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 363 11 2 3 3.4 CCC#CC[C@H](C)[C@H](O)/C=C/[C@H]1CCC(=O)N1CCCCCCC(=O)O 10.1021/acs.jmedchem.9b00336
CHEMBL4558749 181443 20 None -5128 3 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]PGE2 from human recombinant EP2 receptor expressed in HEK293 cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]PGE2 from human recombinant EP2 receptor expressed in HEK293 cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 363 11 2 3 3.4 CCC#CC[C@H](C)[C@H](O)/C=C/[C@H]1CCC(=O)N1CCCCCCC(=O)O 10.1021/acs.jmedchem.9b00336
118517488 160490 0 None -56 2 Human 5.9 pKi = 5.9 Binding
Radioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations wRadioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations w
ChEMBL 414 8 2 3 4.4 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2cccc(F)c2F)cc1 nan
CHEMBL3981554 160490 0 None -56 2 Human 5.9 pKi = 5.9 Binding
Radioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations wRadioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations w
ChEMBL 414 8 2 3 4.4 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2cccc(F)c2F)cc1 nan
44442327 101234 0 None -147 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]PGE2 from human EP2 receptor expressed in HEK293 cellsDisplacement of [3H]PGE2 from human EP2 receptor expressed in HEK293 cells
ChEMBL 345 9 2 3 3.0 CCCC[C@H](O)/C=C/[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.05.025
CHEMBL251294 101234 0 None -147 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]PGE2 from human EP2 receptor expressed in HEK293 cellsDisplacement of [3H]PGE2 from human EP2 receptor expressed in HEK293 cells
ChEMBL 345 9 2 3 3.0 CCCC[C@H](O)/C=C/[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.05.025
17757350 159533 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 413 12 3 4 5.1 CCCCCC(O)c1ccc([C@@H]2[C@@H](C/C=C\CCCC(=O)O)[C@H](C#N)C[C@H]2O)cc1 nan
CHEMBL3973347 159533 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 413 12 3 4 5.1 CCCCCC(O)c1ccc([C@@H]2[C@@H](C/C=C\CCCC(=O)O)[C@H](C#N)C[C@H]2O)cc1 nan
10112412 76243 0 None -208 3 Mouse 6.9 pKi = 6.9 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 413 9 2 4 3.8 Cc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=O)N2CCCc2ccc(C(=O)O)s2)c1 10.1016/j.bmcl.2011.10.109
CHEMBL1933719 76243 0 None -208 3 Mouse 6.9 pKi = 6.9 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 413 9 2 4 3.8 Cc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=O)N2CCCc2ccc(C(=O)O)s2)c1 10.1016/j.bmcl.2011.10.109
10112412 76243 0 None -208 3 Mouse 6.9 pKi = 6.9 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 413 9 2 4 3.8 Cc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=O)N2CCCc2ccc(C(=O)O)s2)c1 10.1016/j.bmc.2012.02.018
CHEMBL1933719 76243 0 None -208 3 Mouse 6.9 pKi = 6.9 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 413 9 2 4 3.8 Cc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=O)N2CCCc2ccc(C(=O)O)s2)c1 10.1016/j.bmc.2012.02.018
118517489 150469 0 None -44 2 Human 5.9 pKi = 5.9 Binding
Radioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations wRadioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations w
ChEMBL 414 8 2 3 4.4 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2cc(F)ccc2F)cc1 nan
CHEMBL3900245 150469 0 None -44 2 Human 5.9 pKi = 5.9 Binding
Radioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations wRadioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations w
ChEMBL 414 8 2 3 4.4 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2cc(F)ccc2F)cc1 nan
51039070 135982 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Measurement of EP2 receptor binding affinity was carried out according to the method of Abramovitz et al. (Biochimica et Biophysica Acta, 1483, 285 (2000)). A test compound dissolved in dimethylsulfoxide and [3H]PGE2 (NET-428, available from PerkinElmer Inc.) (final concentration: 10 nM) were added to a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2, 1 mM EDTA) in which 10 μg of a membrane fraction (ES-562-M, available from Euroscreen S.A.) of HEK293 cells expressing human EP2 receptor had been suspended, followed by incubation at 30° C. for 60 minutes. The membrane fraction was recovered on glass fiber filter paper (GF/B, available from Whatman PLC) using a cell harvester (M30R, available from Brandel Inc.), and after washing with a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2), radioactivity was measured with a liquid scintillation analyzer (2000CA, available from Packard).Binding Assay: Measurement of EP2 receptor binding affinity was carried out according to the method of Abramovitz et al. (Biochimica et Biophysica Acta, 1483, 285 (2000)). A test compound dissolved in dimethylsulfoxide and [3H]PGE2 (NET-428, available from PerkinElmer Inc.) (final concentration: 10 nM) were added to a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2, 1 mM EDTA) in which 10 μg of a membrane fraction (ES-562-M, available from Euroscreen S.A.) of HEK293 cells expressing human EP2 receptor had been suspended, followed by incubation at 30° C. for 60 minutes. The membrane fraction was recovered on glass fiber filter paper (GF/B, available from Whatman PLC) using a cell harvester (M30R, available from Brandel Inc.), and after washing with a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2), radioactivity was measured with a liquid scintillation analyzer (2000CA, available from Packard).
ChEMBL 433 6 5 5 4.2 O=C(NO)c1ccc(CNC(=O)c2[nH]c(-c3cccs3)cc2-c2ccc(O)cc2)cc1 nan
CHEMBL3670660 135982 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Measurement of EP2 receptor binding affinity was carried out according to the method of Abramovitz et al. (Biochimica et Biophysica Acta, 1483, 285 (2000)). A test compound dissolved in dimethylsulfoxide and [3H]PGE2 (NET-428, available from PerkinElmer Inc.) (final concentration: 10 nM) were added to a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2, 1 mM EDTA) in which 10 μg of a membrane fraction (ES-562-M, available from Euroscreen S.A.) of HEK293 cells expressing human EP2 receptor had been suspended, followed by incubation at 30° C. for 60 minutes. The membrane fraction was recovered on glass fiber filter paper (GF/B, available from Whatman PLC) using a cell harvester (M30R, available from Brandel Inc.), and after washing with a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2), radioactivity was measured with a liquid scintillation analyzer (2000CA, available from Packard).Binding Assay: Measurement of EP2 receptor binding affinity was carried out according to the method of Abramovitz et al. (Biochimica et Biophysica Acta, 1483, 285 (2000)). A test compound dissolved in dimethylsulfoxide and [3H]PGE2 (NET-428, available from PerkinElmer Inc.) (final concentration: 10 nM) were added to a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2, 1 mM EDTA) in which 10 μg of a membrane fraction (ES-562-M, available from Euroscreen S.A.) of HEK293 cells expressing human EP2 receptor had been suspended, followed by incubation at 30° C. for 60 minutes. The membrane fraction was recovered on glass fiber filter paper (GF/B, available from Whatman PLC) using a cell harvester (M30R, available from Brandel Inc.), and after washing with a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2), radioactivity was measured with a liquid scintillation analyzer (2000CA, available from Packard).
ChEMBL 433 6 5 5 4.2 O=C(NO)c1ccc(CNC(=O)c2[nH]c(-c3cccs3)cc2-c2ccc(O)cc2)cc1 nan
44303626 174961 0 None - 1 Mouse 7.9 pKi = 7.9 Binding
Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.
ChEMBL 398 11 3 3 4.7 CCC1([C@@H](O)C/C=C/[C@H]2[C@H](O)C[C@H](Cl)[C@@H]2C/C=C\CCCC(=O)O)CCC1 10.1016/s0960-894x(01)00359-6
CHEMBL433249 174961 0 None - 1 Mouse 7.9 pKi = 7.9 Binding
Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.
ChEMBL 398 11 3 3 4.7 CCC1([C@@H](O)C/C=C/[C@H]2[C@H](O)C[C@H](Cl)[C@@H]2C/C=C\CCCC(=O)O)CCC1 10.1016/s0960-894x(01)00359-6
57400249 76252 0 None 3 3 Mouse 7.9 pKi = 7.9 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 410 9 2 6 3.4 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)CC2CCCC2)n1 10.1016/j.bmcl.2011.10.109
CHEMBL1933728 76252 0 None 3 3 Mouse 7.9 pKi = 7.9 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 410 9 2 6 3.4 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)CC2CCCC2)n1 10.1016/j.bmcl.2011.10.109
10291963 91483 0 None -74 6 Human 6.9 pKi = 6.9 Binding
Binding affinity to human EP2 receptorBinding affinity to human EP2 receptor
ChEMBL 359 10 2 3 3.4 CCCCC[C@H](O)/C=C/[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1021/jm049290a
CHEMBL222715 91483 0 None -74 6 Human 6.9 pKi = 6.9 Binding
Binding affinity to human EP2 receptorBinding affinity to human EP2 receptor
ChEMBL 359 10 2 3 3.4 CCCCC[C@H](O)/C=C/[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1021/jm049290a
11315933 130072 4 None -707 5 Mouse 5.9 pKi = 5.9 Binding
Ability to inhibit the binding of [3H]-PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP2Ability to inhibit the binding of [3H]-PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP2
ChEMBL 413 7 1 4 4.9 Cc1cc2c(CC(=O)O)cccc2n1C(=O)c1ccc(OCCc2ccccc2)cc1 10.1016/j.bmcl.2004.07.039
CHEMBL361457 130072 4 None -707 5 Mouse 5.9 pKi = 5.9 Binding
Ability to inhibit the binding of [3H]-PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP2Ability to inhibit the binding of [3H]-PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP2
ChEMBL 413 7 1 4 4.9 Cc1cc2c(CC(=O)O)cccc2n1C(=O)c1ccc(OCCc2ccccc2)cc1 10.1016/j.bmcl.2004.07.039
44394432 134104 0 None -10 5 Mouse 5.9 pKi = 5.9 Binding
Ability to inhibit the binding of [3H]-PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP2Ability to inhibit the binding of [3H]-PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP2
ChEMBL 457 6 1 6 4.5 Cc1cc2c(CC(=O)O)cccc2n1C(=O)c1ccc(OC[C@H]2COc3ccccc3O2)cc1 10.1016/j.bmcl.2004.07.039
CHEMBL365908 134104 0 None -10 5 Mouse 5.9 pKi = 5.9 Binding
Ability to inhibit the binding of [3H]-PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP2Ability to inhibit the binding of [3H]-PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP2
ChEMBL 457 6 1 6 4.5 Cc1cc2c(CC(=O)O)cccc2n1C(=O)c1ccc(OC[C@H]2COc3ccccc3O2)cc1 10.1016/j.bmcl.2004.07.039
23017109 206853 0 None -6 2 Mouse 5.9 pKi = 5.9 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 416 10 1 5 4.3 O=C(O)COCc1ccc(Cn2cccn2)cc1OCCc1ccc2ccccc2c1 10.1016/j.bmc.2009.08.007
CHEMBL595830 206853 0 None -6 2 Mouse 5.9 pKi = 5.9 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 416 10 1 5 4.3 O=C(O)COCc1ccc(Cn2cccn2)cc1OCCc1ccc2ccccc2c1 10.1016/j.bmc.2009.08.007
15907747 213802 0 None -257 4 Human 4.9 pKi = 4.9 Binding
Affinity at human EP2 receptor.Affinity at human EP2 receptor.
ChEMBL 684 8 1 5 7.2 CO[C@@](C(=O)NS(=O)(=O)c1ccccc1-c1ccc(CN2C(=O)c3ccccc3CCc3ccccc32)cc1)(c1ccccc1)C(F)(F)F 10.1016/s0960-894x(99)00465-5
CHEMBL91537 213802 0 None -257 4 Human 4.9 pKi = 4.9 Binding
Affinity at human EP2 receptor.Affinity at human EP2 receptor.
ChEMBL 684 8 1 5 7.2 CO[C@@](C(=O)NS(=O)(=O)c1ccccc1-c1ccc(CN2C(=O)c3ccccc3CCc3ccccc32)cc1)(c1ccccc1)C(F)(F)F 10.1016/s0960-894x(99)00465-5
118517361 160149 0 None -218 2 Human 5.9 pKi = 5.9 Binding
Radioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations wRadioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations w
ChEMBL 446 8 2 3 5.1 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2cccc(C(F)(F)F)c2)cc1 nan
CHEMBL3978590 160149 0 None -218 2 Human 5.9 pKi = 5.9 Binding
Radioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations wRadioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations w
ChEMBL 446 8 2 3 5.1 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2cccc(C(F)(F)F)c2)cc1 nan
9975502 101264 0 None 1 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]PGE2 from human EP2 receptor expressed in HEK293 cellsDisplacement of [3H]PGE2 from human EP2 receptor expressed in HEK293 cells
ChEMBL 355 9 1 2 4.6 CCCC/C(C)=C/C=C/[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.05.025
CHEMBL251504 101264 0 None 1 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]PGE2 from human EP2 receptor expressed in HEK293 cellsDisplacement of [3H]PGE2 from human EP2 receptor expressed in HEK293 cells
ChEMBL 355 9 1 2 4.6 CCCC/C(C)=C/C=C/[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.05.025
3356 9060 73 None -53 8 Human 6.9 pKi = 6.9 Binding
Binding affinity to human EP2 receptor expressed in HEK293 cellsBinding affinity to human EP2 receptor expressed in HEK293 cells
ChEMBL 435 5 1 4 4.4 OC(=O)C[C@H]1CCc2c1n(Cc1ccc(cc1)Cl)c1c2cc(cc1S(=O)(=O)C)F 10.1021/jm0603668
4326 9060 73 None -53 8 Human 6.9 pKi = 6.9 Binding
Binding affinity to human EP2 receptor expressed in HEK293 cellsBinding affinity to human EP2 receptor expressed in HEK293 cells
ChEMBL 435 5 1 4 4.4 OC(=O)C[C@H]1CCc2c1n(Cc1ccc(cc1)Cl)c1c2cc(cc1S(=O)(=O)C)F 10.1021/jm0603668
9867642 9060 73 None -53 8 Human 6.9 pKi = 6.9 Binding
Binding affinity to human EP2 receptor expressed in HEK293 cellsBinding affinity to human EP2 receptor expressed in HEK293 cells
ChEMBL 435 5 1 4 4.4 OC(=O)C[C@H]1CCc2c1n(Cc1ccc(cc1)Cl)c1c2cc(cc1S(=O)(=O)C)F 10.1021/jm0603668
CHEMBL426559 9060 73 None -53 8 Human 6.9 pKi = 6.9 Binding
Binding affinity to human EP2 receptor expressed in HEK293 cellsBinding affinity to human EP2 receptor expressed in HEK293 cells
ChEMBL 435 5 1 4 4.4 OC(=O)C[C@H]1CCc2c1n(Cc1ccc(cc1)Cl)c1c2cc(cc1S(=O)(=O)C)F 10.1021/jm0603668
DB11629 9060 73 None -53 8 Human 6.9 pKi = 6.9 Binding
Binding affinity to human EP2 receptor expressed in HEK293 cellsBinding affinity to human EP2 receptor expressed in HEK293 cells
ChEMBL 435 5 1 4 4.4 OC(=O)C[C@H]1CCc2c1n(Cc1ccc(cc1)Cl)c1c2cc(cc1S(=O)(=O)C)F 10.1021/jm0603668
70667255 158253 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 mins
ChEMBL 427 10 2 4 5.4 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2C=CCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3962183 158253 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 mins
ChEMBL 427 10 2 4 5.4 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2C=CCc2ccc(C(=O)O)s2)cc1 nan
24760052 157964 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 427 10 2 4 5.4 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2/C=C/Cc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3959769 157964 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 427 10 2 4 5.4 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2/C=C/Cc2ccc(C(=O)O)s2)cc1 nan
44304436 210099 0 None -35 5 Mouse 7.9 pKi = 7.9 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptor
ChEMBL 400 14 3 5 3.8 CCCC[C@H](C)C[C@H](O)/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1SCCCCCC(=O)O 10.1016/s0960-894x(01)00364-x
CHEMBL64854 210099 0 None -35 5 Mouse 7.9 pKi = 7.9 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptor
ChEMBL 400 14 3 5 3.8 CCCC[C@H](C)C[C@H](O)/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1SCCCCCC(=O)O 10.1016/s0960-894x(01)00364-x
44320373 213029 0 None 5 4 Human 6.9 pKi = 6.9 Binding
Binding affinity at human Prostanoid EP2 receptor.Binding affinity at human Prostanoid EP2 receptor.
ChEMBL 376 9 1 2 5.8 O=C(O)CCc1ccccc1-c1ccc(CSCCc2ccccc2)cc1 10.1016/s0960-894x(02)00518-8
CHEMBL86799 213029 0 None 5 4 Human 6.9 pKi = 6.9 Binding
Binding affinity at human Prostanoid EP2 receptor.Binding affinity at human Prostanoid EP2 receptor.
ChEMBL 376 9 1 2 5.8 O=C(O)CCc1ccccc1-c1ccc(CSCCc2ccccc2)cc1 10.1016/s0960-894x(02)00518-8
52947851 23317 0 None -14 3 Human 5.9 pKi = 5.9 Binding
Binding affinity for human prostanoid EP2 receptorBinding affinity for human prostanoid EP2 receptor
ChEMBL 528 10 2 2 8.1 O=C(O)/C=C/c1ccccc1/C=C/Cc1ccccc1.O=C(O)/C=C/c1ccccc1C/C=C/c1ccccc1 10.1016/j.bmcl.2004.11.051
CHEMBL1237315 23317 0 None -14 3 Human 5.9 pKi = 5.9 Binding
Binding affinity for human prostanoid EP2 receptorBinding affinity for human prostanoid EP2 receptor
ChEMBL 528 10 2 2 8.1 O=C(O)/C=C/c1ccccc1/C=C/Cc1ccccc1.O=C(O)/C=C/c1ccccc1C/C=C/c1ccccc1 10.1016/j.bmcl.2004.11.051
52947851 23317 0 None -14 3 Human 5.9 pKi = 5.9 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 528 10 2 2 8.1 O=C(O)/C=C/c1ccccc1/C=C/Cc1ccccc1.O=C(O)/C=C/c1ccccc1C/C=C/c1ccccc1 10.1016/j.bmcl.2006.08.025
CHEMBL1237315 23317 0 None -14 3 Human 5.9 pKi = 5.9 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 528 10 2 2 8.1 O=C(O)/C=C/c1ccccc1/C=C/Cc1ccccc1.O=C(O)/C=C/c1ccccc1C/C=C/c1ccccc1 10.1016/j.bmcl.2006.08.025
9813912 144660 0 None -14 3 Human 5.9 pKi = 5.9 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 264 5 1 1 4.0 O=C(O)/C=C/c1ccccc1C/C=C/c1ccccc1 10.1016/j.bmcl.2006.08.025
CHEMBL376282 144660 0 None -14 3 Human 5.9 pKi = 5.9 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 264 5 1 1 4.0 O=C(O)/C=C/c1ccccc1C/C=C/c1ccccc1 10.1016/j.bmcl.2006.08.025
57394140 76146 0 None -707 3 Mouse 5.9 pKi = 5.9 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counterDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counter
ChEMBL 419 13 2 4 4.1 COCc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=S)N2CCCCCCC(=O)O)c1 10.1016/j.bmc.2011.12.009
CHEMBL1929550 76146 0 None -707 3 Mouse 5.9 pKi = 5.9 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counterDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counter
ChEMBL 419 13 2 4 4.1 COCc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=S)N2CCCCCCC(=O)O)c1 10.1016/j.bmc.2011.12.009
134146425 155982 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 394 12 2 2 6.4 CCCCC(O)c1ccc([C@H]2CC[C@@H](Cl)[C@@H]2CCCCCCC(=O)O)cc1 nan
CHEMBL3943966 155982 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 394 12 2 2 6.4 CCCCC(O)c1ccc([C@H]2CC[C@@H](Cl)[C@@H]2CCCCCCC(=O)O)cc1 nan
11519006 109263 0 None -229 6 Human 5.9 pKi = 5.9 Binding
Inhibition of [3H]PGE-2 binding to Prostanoid EP2 receptorInhibition of [3H]PGE-2 binding to Prostanoid EP2 receptor
ChEMBL 481 8 1 5 6.1 O=C(O)COc1cccc(C[C@@H]2CCC[C@H]3O[C@]23c2nc(-c3ccccc3)c(-c3ccccc3)o2)c1 10.1016/j.bmcl.2005.04.076
CHEMBL2373410 109263 0 None -229 6 Human 5.9 pKi = 5.9 Binding
Inhibition of [3H]PGE-2 binding to Prostanoid EP2 receptorInhibition of [3H]PGE-2 binding to Prostanoid EP2 receptor
ChEMBL 481 8 1 5 6.1 O=C(O)COc1cccc(C[C@@H]2CCC[C@H]3O[C@]23c2nc(-c3ccccc3)c(-c3ccccc3)o2)c1 10.1016/j.bmcl.2005.04.076
CHEMBL3040272 109263 0 None -229 6 Human 5.9 pKi = 5.9 Binding
Inhibition of [3H]PGE-2 binding to Prostanoid EP2 receptorInhibition of [3H]PGE-2 binding to Prostanoid EP2 receptor
ChEMBL 481 8 1 5 6.1 O=C(O)COc1cccc(C[C@@H]2CCC[C@H]3O[C@]23c2nc(-c3ccccc3)c(-c3ccccc3)o2)c1 10.1016/j.bmcl.2005.04.076
9808508 118337 0 None -245 3 Human 4.9 pKi = 4.9 Binding
Affinity at human EP2 receptor.Affinity at human EP2 receptor.
ChEMBL 586 7 1 4 6.3 O=C(Cc1ccccc1)NS(=O)(=O)c1ccccc1-c1ccc(CN2C(=O)c3ccccc3CCc3ccccc32)cc1 10.1016/s0960-894x(99)00465-5
CHEMBL328067 118337 0 None -245 3 Human 4.9 pKi = 4.9 Binding
Affinity at human EP2 receptor.Affinity at human EP2 receptor.
ChEMBL 586 7 1 4 6.3 O=C(Cc1ccccc1)NS(=O)(=O)c1ccccc1-c1ccc(CN2C(=O)c3ccccc3CCc3ccccc32)cc1 10.1016/s0960-894x(99)00465-5
44455115 102337 0 None -15 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]PGE2 from human EP2 receptorDisplacement of [3H]PGE2 from human EP2 receptor
ChEMBL 387 10 2 3 4.1 CCCCC(C)(C)[C@H](O)/C=C/[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.11.020
CHEMBL257658 102337 0 None -15 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]PGE2 from human EP2 receptorDisplacement of [3H]PGE2 from human EP2 receptor
ChEMBL 387 10 2 3 4.1 CCCCC(C)(C)[C@H](O)/C=C/[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.11.020
118517359 151174 0 None -114 2 Human 5.8 pKi = 5.8 Binding
Radioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations wRadioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations w
ChEMBL 456 8 2 3 4.8 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2cccc(Br)c2)cc1 nan
CHEMBL3906016 151174 0 None -114 2 Human 5.8 pKi = 5.8 Binding
Radioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations wRadioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations w
ChEMBL 456 8 2 3 4.8 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2cccc(Br)c2)cc1 nan
44289922 170303 0 None -954 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]PGE2 from human recombinant EP2 receptor expressed in HEK293 cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]PGE2 from human recombinant EP2 receptor expressed in HEK293 cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 339 13 2 3 3.5 CCCCC[C@H](O)/C=C/[C@H]1CCC(=O)N1CCCCCCC(=O)O 10.1021/acs.jmedchem.9b00336
CHEMBL42027 170303 0 None -954 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]PGE2 from human recombinant EP2 receptor expressed in HEK293 cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]PGE2 from human recombinant EP2 receptor expressed in HEK293 cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 339 13 2 3 3.5 CCCCC[C@H](O)/C=C/[C@H]1CCC(=O)N1CCCCCCC(=O)O 10.1021/acs.jmedchem.9b00336
11855868 159323 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 mins
ChEMBL 429 11 2 4 5.6 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2CCCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3971632 159323 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 mins
ChEMBL 429 11 2 4 5.6 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2CCCc2ccc(C(=O)O)s2)cc1 nan
57393340 76250 0 None -10 4 Mouse 7.8 pKi = 7.8 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 530 12 2 7 4.2 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(COCC(F)(F)F)c2)n1 10.1016/j.bmcl.2011.10.109
CHEMBL1933726 76250 0 None -10 4 Mouse 7.8 pKi = 7.8 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 530 12 2 7 4.2 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(COCC(F)(F)F)c2)n1 10.1016/j.bmcl.2011.10.109
11855868 159323 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 429 11 2 4 5.6 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2CCCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3971632 159323 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 429 11 2 4 5.6 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2CCCc2ccc(C(=O)O)s2)cc1 nan
57894053 81945 0 None -79 3 Mouse 7.8 pKi = 7.8 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 551 10 2 8 5.4 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(-c3nc4ccccc4s3)c2)n1 10.1016/j.bmc.2012.04.008
CHEMBL2036324 81945 0 None -79 3 Mouse 7.8 pKi = 7.8 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 551 10 2 8 5.4 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(-c3nc4ccccc4s3)c2)n1 10.1016/j.bmc.2012.04.008
155516303 176856 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]prostaglandin E2 from human EP2 receptor expressed in HEK293 cell membranes after 60 mins by liquid scintillation countingDisplacement of [3H]prostaglandin E2 from human EP2 receptor expressed in HEK293 cell membranes after 60 mins by liquid scintillation counting
ChEMBL 478 7 1 5 5.2 CC(C)(C)c1ccc(CN(Cc2cccc3oc(C(=O)O)cc23)S(=O)(=O)c2cccnc2)cc1 10.1021/acs.jmedchem.8b00808
CHEMBL4443289 176856 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]prostaglandin E2 from human EP2 receptor expressed in HEK293 cell membranes after 60 mins by liquid scintillation countingDisplacement of [3H]prostaglandin E2 from human EP2 receptor expressed in HEK293 cell membranes after 60 mins by liquid scintillation counting
ChEMBL 478 7 1 5 5.2 CC(C)(C)c1ccc(CN(Cc2cccc3oc(C(=O)O)cc23)S(=O)(=O)c2cccnc2)cc1 10.1021/acs.jmedchem.8b00808
18973764 23419 0 None 1 4 Human 6.8 pKi = 6.8 Binding
Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 346 8 1 2 5.1 O=C(O)c1ccc(CCCc2ccccc2OCc2ccccc2)cc1 10.1016/s0960-894x(03)00794-7
CHEMBL124199 23419 0 None 1 4 Human 6.8 pKi = 6.8 Binding
Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 346 8 1 2 5.1 O=C(O)c1ccc(CCCc2ccccc2OCc2ccccc2)cc1 10.1016/s0960-894x(03)00794-7
44304058 209956 0 None -66 5 Mouse 6.8 pKi = 6.8 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptor
ChEMBL 374 13 3 6 2.0 CCCCC[C@H](O)/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1SCCCOCC(=O)O 10.1016/s0960-894x(01)00364-x
CHEMBL64254 209956 0 None -66 5 Mouse 6.8 pKi = 6.8 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptor
ChEMBL 374 13 3 6 2.0 CCCCC[C@H](O)/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1SCCCOCC(=O)O 10.1016/s0960-894x(01)00364-x
23017216 205938 0 None -1380 4 Mouse 5.8 pKi = 5.8 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 439 9 2 3 5.4 O=C(O)CCc1ccc(COc2ccccc2)cc1C(=O)NCc1cccc2ccccc12 10.1016/j.bmc.2009.11.023
CHEMBL589411 205938 0 None -1380 4 Mouse 5.8 pKi = 5.8 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 439 9 2 3 5.4 O=C(O)CCc1ccc(COc2ccccc2)cc1C(=O)NCc1cccc2ccccc12 10.1016/j.bmc.2009.11.023
44304051 109537 0 None -213 4 Mouse 5.8 pKi = 5.8 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptor
ChEMBL 440 12 3 7 2.4 COc1ccc(C[C@H](O)/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2SCCCSCC(=O)O)cc1 10.1016/s0960-894x(01)00364-x
CHEMBL305126 109537 0 None -213 4 Mouse 5.8 pKi = 5.8 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptor
ChEMBL 440 12 3 7 2.4 COc1ccc(C[C@H](O)/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2SCCCSCC(=O)O)cc1 10.1016/s0960-894x(01)00364-x
134143292 152006 0 None - 1 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 408 12 1 3 6.5 CCCCC(O)c1ccc([C@H]2CC[C@@H](Cl)[C@@H]2CCCCCCC(=O)OC)cc1 nan
CHEMBL3912658 152006 0 None - 1 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 408 12 1 3 6.5 CCCCC(O)c1ccc([C@H]2CC[C@@H](Cl)[C@@H]2CCCCCCC(=O)OC)cc1 nan
59465595 152201 0 None - 1 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 388 13 2 3 5.8 CCCCCC(O)c1cccc([C@H]2CCC(=O)[C@@H]2CCCCCCC(=O)O)c1 nan
CHEMBL3914108 152201 0 None - 1 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 388 13 2 3 5.8 CCCCCC(O)c1cccc([C@H]2CCC(=O)[C@@H]2CCCCCCC(=O)O)c1 nan
59465574 152723 0 None 1 2 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 400 12 1 4 5.7 CCCCCC(O)c1ccc([C@H]2CCC(=O)[C@@H]2C/C=C\CCCC(=O)OC)cc1 nan
CHEMBL3918084 152723 0 None 1 2 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 400 12 1 4 5.7 CCCCCC(O)c1ccc([C@H]2CCC(=O)[C@@H]2C/C=C\CCCC(=O)OC)cc1 nan
118517490 159934 0 None -125 2 Human 5.8 pKi = 5.8 Binding
Radioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations wRadioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations w
ChEMBL 414 8 2 3 4.4 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2ccc(F)c(F)c2)cc1 nan
CHEMBL3976710 159934 0 None -125 2 Human 5.8 pKi = 5.8 Binding
Radioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations wRadioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations w
ChEMBL 414 8 2 3 4.4 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2ccc(F)c(F)c2)cc1 nan
72695027 113043 0 None -28 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cell membranes after 90 mins by topcount scintillation counting analysisDisplacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cell membranes after 90 mins by topcount scintillation counting analysis
ChEMBL 396 8 2 4 3.5 C[C@H](NC(=O)[C@H]1CCCCN1CCOc1ccccc1)c1ccc(C(=O)O)cc1 10.1021/ml5000367
CHEMBL3115074 113043 0 None -28 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cell membranes after 90 mins by topcount scintillation counting analysisDisplacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cell membranes after 90 mins by topcount scintillation counting analysis
ChEMBL 396 8 2 4 3.5 C[C@H](NC(=O)[C@H]1CCCCN1CCOc1ccccc1)c1ccc(C(=O)O)cc1 10.1021/ml5000367
CHEMBL3138992 113043 0 None -28 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cell membranes after 90 mins by topcount scintillation counting analysisDisplacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cell membranes after 90 mins by topcount scintillation counting analysis
ChEMBL 396 8 2 4 3.5 C[C@H](NC(=O)[C@H]1CCCCN1CCOc1ccccc1)c1ccc(C(=O)O)cc1 10.1021/ml5000367
72695027 113043 0 None -28 2 Human 5.8 pKi = 5.8 Binding
In Vitro Binding Assay: hEP1 and hEP4 membranes are prepared from recombinant HEK293 cells stably expressing the human EP1 (Genbank accession number AY275470) or EP4 (Genbank accession number AY429109) receptors. hEP2 and hEP3 membranes are prepared from HEK293 cells transiently transfected with EP2 (Genbank accession number AY275471) or EP3 (isoform VI: Genbank accession number AY429108) receptor plasmids. Frozen cell pellets are homogenized in homogenization buffer using a Teflon/glass homogenizer. Membrane protein is aliquoted and quick frozen on dry ice prior to storage at -80 C. Homogenization buffer contained 10 mM Tris-HCl, pH 7.4, 250 mM sucrose, 1 mM EDTA, 0.3 mM indomethacin and plus Complete, with EDTA, obtained from Roche Molecular Biochemicals (Catalog Number 1 697 498).Kd values for [3H]-PGE2 binding to each receptor are determined by saturation binding studies or homologous competition. Compounds are tested in a 96-well format using a three-fold dilution series.In Vitro Binding Assay: hEP1 and hEP4 membranes are prepared from recombinant HEK293 cells stably expressing the human EP1 (Genbank accession number AY275470) or EP4 (Genbank accession number AY429109) receptors. hEP2 and hEP3 membranes are prepared from HEK293 cells transiently transfected with EP2 (Genbank accession number AY275471) or EP3 (isoform VI: Genbank accession number AY429108) receptor plasmids. Frozen cell pellets are homogenized in homogenization buffer using a Teflon/glass homogenizer. Membrane protein is aliquoted and quick frozen on dry ice prior to storage at -80 C. Homogenization buffer contained 10 mM Tris-HCl, pH 7.4, 250 mM sucrose, 1 mM EDTA, 0.3 mM indomethacin and plus Complete, with EDTA, obtained from Roche Molecular Biochemicals (Catalog Number 1 697 498).Kd values for [3H]-PGE2 binding to each receptor are determined by saturation binding studies or homologous competition. Compounds are tested in a 96-well format using a three-fold dilution series.
ChEMBL 396 8 2 4 3.5 C[C@H](NC(=O)[C@H]1CCCCN1CCOc1ccccc1)c1ccc(C(=O)O)cc1 nan
CHEMBL3115074 113043 0 None -28 2 Human 5.8 pKi = 5.8 Binding
In Vitro Binding Assay: hEP1 and hEP4 membranes are prepared from recombinant HEK293 cells stably expressing the human EP1 (Genbank accession number AY275470) or EP4 (Genbank accession number AY429109) receptors. hEP2 and hEP3 membranes are prepared from HEK293 cells transiently transfected with EP2 (Genbank accession number AY275471) or EP3 (isoform VI: Genbank accession number AY429108) receptor plasmids. Frozen cell pellets are homogenized in homogenization buffer using a Teflon/glass homogenizer. Membrane protein is aliquoted and quick frozen on dry ice prior to storage at -80 C. Homogenization buffer contained 10 mM Tris-HCl, pH 7.4, 250 mM sucrose, 1 mM EDTA, 0.3 mM indomethacin and plus Complete, with EDTA, obtained from Roche Molecular Biochemicals (Catalog Number 1 697 498).Kd values for [3H]-PGE2 binding to each receptor are determined by saturation binding studies or homologous competition. Compounds are tested in a 96-well format using a three-fold dilution series.In Vitro Binding Assay: hEP1 and hEP4 membranes are prepared from recombinant HEK293 cells stably expressing the human EP1 (Genbank accession number AY275470) or EP4 (Genbank accession number AY429109) receptors. hEP2 and hEP3 membranes are prepared from HEK293 cells transiently transfected with EP2 (Genbank accession number AY275471) or EP3 (isoform VI: Genbank accession number AY429108) receptor plasmids. Frozen cell pellets are homogenized in homogenization buffer using a Teflon/glass homogenizer. Membrane protein is aliquoted and quick frozen on dry ice prior to storage at -80 C. Homogenization buffer contained 10 mM Tris-HCl, pH 7.4, 250 mM sucrose, 1 mM EDTA, 0.3 mM indomethacin and plus Complete, with EDTA, obtained from Roche Molecular Biochemicals (Catalog Number 1 697 498).Kd values for [3H]-PGE2 binding to each receptor are determined by saturation binding studies or homologous competition. Compounds are tested in a 96-well format using a three-fold dilution series.
ChEMBL 396 8 2 4 3.5 C[C@H](NC(=O)[C@H]1CCCCN1CCOc1ccccc1)c1ccc(C(=O)O)cc1 nan
CHEMBL3138992 113043 0 None -28 2 Human 5.8 pKi = 5.8 Binding
In Vitro Binding Assay: hEP1 and hEP4 membranes are prepared from recombinant HEK293 cells stably expressing the human EP1 (Genbank accession number AY275470) or EP4 (Genbank accession number AY429109) receptors. hEP2 and hEP3 membranes are prepared from HEK293 cells transiently transfected with EP2 (Genbank accession number AY275471) or EP3 (isoform VI: Genbank accession number AY429108) receptor plasmids. Frozen cell pellets are homogenized in homogenization buffer using a Teflon/glass homogenizer. Membrane protein is aliquoted and quick frozen on dry ice prior to storage at -80 C. Homogenization buffer contained 10 mM Tris-HCl, pH 7.4, 250 mM sucrose, 1 mM EDTA, 0.3 mM indomethacin and plus Complete, with EDTA, obtained from Roche Molecular Biochemicals (Catalog Number 1 697 498).Kd values for [3H]-PGE2 binding to each receptor are determined by saturation binding studies or homologous competition. Compounds are tested in a 96-well format using a three-fold dilution series.In Vitro Binding Assay: hEP1 and hEP4 membranes are prepared from recombinant HEK293 cells stably expressing the human EP1 (Genbank accession number AY275470) or EP4 (Genbank accession number AY429109) receptors. hEP2 and hEP3 membranes are prepared from HEK293 cells transiently transfected with EP2 (Genbank accession number AY275471) or EP3 (isoform VI: Genbank accession number AY429108) receptor plasmids. Frozen cell pellets are homogenized in homogenization buffer using a Teflon/glass homogenizer. Membrane protein is aliquoted and quick frozen on dry ice prior to storage at -80 C. Homogenization buffer contained 10 mM Tris-HCl, pH 7.4, 250 mM sucrose, 1 mM EDTA, 0.3 mM indomethacin and plus Complete, with EDTA, obtained from Roche Molecular Biochemicals (Catalog Number 1 697 498).Kd values for [3H]-PGE2 binding to each receptor are determined by saturation binding studies or homologous competition. Compounds are tested in a 96-well format using a three-fold dilution series.
ChEMBL 396 8 2 4 3.5 C[C@H](NC(=O)[C@H]1CCCCN1CCOc1ccccc1)c1ccc(C(=O)O)cc1 nan
24952577 207340 0 None -2 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]PGE2 from human EP2 receptor expressed in HEK293-EBNA cells by scintillation countingDisplacement of [3H]PGE2 from human EP2 receptor expressed in HEK293-EBNA cells by scintillation counting
ChEMBL 399 6 2 3 5.2 C[C@H](NC(=O)c1cscc1Cc1cccc(Cl)c1)c1ccc(C(=O)O)cc1 10.1021/jm901771h
CHEMBL599051 207340 0 None -2 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]PGE2 from human EP2 receptor expressed in HEK293-EBNA cells by scintillation countingDisplacement of [3H]PGE2 from human EP2 receptor expressed in HEK293-EBNA cells by scintillation counting
ChEMBL 399 6 2 3 5.2 C[C@H](NC(=O)c1cscc1Cc1cccc(Cl)c1)c1ccc(C(=O)O)cc1 10.1021/jm901771h
1929 8386 55 None -11 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]prostaglandin E2 from human EP2 receptor expressed in HEK293 cell membranes after 60 mins by liquid scintillation countingDisplacement of [3H]prostaglandin E2 from human EP2 receptor expressed in HEK293 cell membranes after 60 mins by liquid scintillation counting
ChEMBL 468 9 1 5 4.2 OC(=O)COc1cccc(c1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)C(C)(C)C 10.1021/acs.jmedchem.8b00808
9890801 8386 55 None -11 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]prostaglandin E2 from human EP2 receptor expressed in HEK293 cell membranes after 60 mins by liquid scintillation countingDisplacement of [3H]prostaglandin E2 from human EP2 receptor expressed in HEK293 cell membranes after 60 mins by liquid scintillation counting
ChEMBL 468 9 1 5 4.2 OC(=O)COc1cccc(c1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)C(C)(C)C 10.1021/acs.jmedchem.8b00808
CHEMBL563646 8386 55 None -11 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]prostaglandin E2 from human EP2 receptor expressed in HEK293 cell membranes after 60 mins by liquid scintillation countingDisplacement of [3H]prostaglandin E2 from human EP2 receptor expressed in HEK293 cell membranes after 60 mins by liquid scintillation counting
ChEMBL 468 9 1 5 4.2 OC(=O)COc1cccc(c1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)C(C)(C)C 10.1021/acs.jmedchem.8b00808
DB12022 8386 55 None -11 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]prostaglandin E2 from human EP2 receptor expressed in HEK293 cell membranes after 60 mins by liquid scintillation countingDisplacement of [3H]prostaglandin E2 from human EP2 receptor expressed in HEK293 cell membranes after 60 mins by liquid scintillation counting
ChEMBL 468 9 1 5 4.2 OC(=O)COc1cccc(c1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)C(C)(C)C 10.1021/acs.jmedchem.8b00808
44349503 175169 0 None -100 4 Human 5.8 pKi = 5.8 Binding
Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 553 10 1 5 7.1 O=C(CCc1ccccc1-c1cccc(-c2ccccc2OCc2ccccc2)c1)NS(=O)(=O)c1cccs1 10.1016/s0960-894x(03)00794-7
CHEMBL434637 175169 0 None -100 4 Human 5.8 pKi = 5.8 Binding
Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 553 10 1 5 7.1 O=C(CCc1ccccc1-c1cccc(-c2ccccc2OCc2ccccc2)c1)NS(=O)(=O)c1cccs1 10.1016/s0960-894x(03)00794-7
44419351 90918 0 None -28 4 Human 5.8 pKi = 5.8 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 533 12 1 5 6.2 Cc1ccc(OCc2ccccc2)c(CCCc2ccccc2CCC(=O)NS(=O)(=O)c2cccs2)c1 10.1016/j.bmcl.2006.08.025
CHEMBL220821 90918 0 None -28 4 Human 5.8 pKi = 5.8 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 533 12 1 5 6.2 Cc1ccc(OCc2ccccc2)c(CCCc2ccccc2CCC(=O)NS(=O)(=O)c2cccs2)c1 10.1016/j.bmcl.2006.08.025
44324368 103293 0 None -3 4 Human 4.8 pKi = 4.8 Binding
Affinity at human EP2 receptor.Affinity at human EP2 receptor.
ChEMBL 587 6 2 4 6.8 O=C(Nc1ccccc1)NS(=O)(=O)c1ccccc1-c1ccc(CN2C(=O)c3ccccc3CCc3ccccc32)cc1 10.1016/s0960-894x(99)00465-5
CHEMBL262690 103293 0 None -3 4 Human 4.8 pKi = 4.8 Binding
Affinity at human EP2 receptor.Affinity at human EP2 receptor.
ChEMBL 587 6 2 4 6.8 O=C(Nc1ccccc1)NS(=O)(=O)c1ccccc1-c1ccc(CN2C(=O)c3ccccc3CCc3ccccc32)cc1 10.1016/s0960-894x(99)00465-5
10144273 212613 0 None -131 4 Human 4.8 pKi = 4.8 Binding
Binding affinity at human Prostanoid EP2 receptor.Binding affinity at human Prostanoid EP2 receptor.
ChEMBL 558 8 1 5 7.2 O=C(CCc1ccccc1-c1cccc(/C=C/c2ccc3ccc(Cl)cc3n2)c1)NS(=O)(=O)c1cccs1 10.1016/s0960-894x(02)00518-8
CHEMBL83450 212613 0 None -131 4 Human 4.8 pKi = 4.8 Binding
Binding affinity at human Prostanoid EP2 receptor.Binding affinity at human Prostanoid EP2 receptor.
ChEMBL 558 8 1 5 7.2 O=C(CCc1ccccc1-c1cccc(/C=C/c2ccc3ccc(Cl)cc3n2)c1)NS(=O)(=O)c1cccs1 10.1016/s0960-894x(02)00518-8
11855871 153186 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 mins
ChEMBL 429 11 1 5 4.9 CCCCCC(=O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3921784 153186 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 mins
ChEMBL 429 11 1 5 4.9 CCCCCC(=O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
11855871 153186 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 429 11 1 5 4.9 CCCCCC(=O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3921784 153186 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 429 11 1 5 4.9 CCCCCC(=O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
11855866 151380 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 mins
ChEMBL 403 9 2 5 4.0 CCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3907809 151380 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 mins
ChEMBL 403 9 2 5 4.0 CCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
11855866 151380 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 403 9 2 5 4.0 CCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3907809 151380 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 403 9 2 5 4.0 CCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
53494965 71587 0 None -5 3 Mouse 6.8 pKi = 6.8 Binding
Displacement of [3H]PGE2 from mouse prostaglandin EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]PGE2 from mouse prostaglandin EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 460 7 2 5 4.5 Cc1ccc(CC(=O)O)cc1NC(=O)c1ccc(OC[C@@H]2CN(C)c3ccccc3O2)cc1C 10.1016/j.bmc.2011.08.007
CHEMBL1819611 71587 0 None -5 3 Mouse 6.8 pKi = 6.8 Binding
Displacement of [3H]PGE2 from mouse prostaglandin EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]PGE2 from mouse prostaglandin EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 460 7 2 5 4.5 Cc1ccc(CC(=O)O)cc1NC(=O)c1ccc(OC[C@@H]2CN(C)c3ccccc3O2)cc1C 10.1016/j.bmc.2011.08.007
52947847 23310 0 None 1 3 Human 5.8 pKi = 5.8 Binding
Binding affinity for human prostanoid EP2 receptorBinding affinity for human prostanoid EP2 receptor
ChEMBL 768 16 2 4 11.9 Cc1cccc(/C=C/Cc2ccc(/C=C/C(=O)O)cc2)c1OCc1ccccc1.Cc1cccc(C/C=C\c2ccc(/C=C/C(=O)O)cc2)c1OCc1ccccc1 10.1016/j.bmcl.2004.11.051
CHEMBL1237300 23310 0 None 1 3 Human 5.8 pKi = 5.8 Binding
Binding affinity for human prostanoid EP2 receptorBinding affinity for human prostanoid EP2 receptor
ChEMBL 768 16 2 4 11.9 Cc1cccc(/C=C/Cc2ccc(/C=C/C(=O)O)cc2)c1OCc1ccccc1.Cc1cccc(C/C=C\c2ccc(/C=C/C(=O)O)cc2)c1OCc1ccccc1 10.1016/j.bmcl.2004.11.051
11314979 72883 0 None -11 4 Mouse 5.8 pKi = 5.8 Binding
Binding affinity for mouse Prostanoid EP2 receptorBinding affinity for mouse Prostanoid EP2 receptor
ChEMBL 379 7 1 4 4.8 CCCCOc1ccc(C(=O)n2c(C)c(CC(=O)O)c3cc(C)ccc32)cc1 10.1016/j.bmcl.2004.06.006
CHEMBL183933 72883 0 None -11 4 Mouse 5.8 pKi = 5.8 Binding
Binding affinity for mouse Prostanoid EP2 receptorBinding affinity for mouse Prostanoid EP2 receptor
ChEMBL 379 7 1 4 4.8 CCCCOc1ccc(C(=O)n2c(C)c(CC(=O)O)c3cc(C)ccc32)cc1 10.1016/j.bmcl.2004.06.006
11234840 131833 0 None -4 2 Mouse 5.8 pKi = 5.8 Binding
Binding affinity for mouse Prostanoid EP2 receptorBinding affinity for mouse Prostanoid EP2 receptor
ChEMBL 395 8 1 5 4.5 CCCCOc1cccc(C(=O)n2c(C)c(CC(=O)O)c3cc(OC)ccc32)c1 10.1016/j.bmcl.2004.06.006
CHEMBL364421 131833 0 None -4 2 Mouse 5.8 pKi = 5.8 Binding
Binding affinity for mouse Prostanoid EP2 receptorBinding affinity for mouse Prostanoid EP2 receptor
ChEMBL 395 8 1 5 4.5 CCCCOc1cccc(C(=O)n2c(C)c(CC(=O)O)c3cc(OC)ccc32)c1 10.1016/j.bmcl.2004.06.006
56949973 76147 0 None -3388 4 Mouse 5.8 pKi = 5.8 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counterDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counter
ChEMBL 407 11 2 4 3.8 Cc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=S)N2CCSCCCC(=O)O)c1 10.1016/j.bmc.2011.12.009
CHEMBL1929551 76147 0 None -3388 4 Mouse 5.8 pKi = 5.8 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counterDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counter
ChEMBL 407 11 2 4 3.8 Cc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=S)N2CCSCCCC(=O)O)c1 10.1016/j.bmc.2011.12.009
57894092 81933 0 None -8511 3 Mouse 5.8 pKi = 5.8 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 494 12 2 6 4.5 O=C(O)CCCSCCN1C(=O)CC[C@@H]1/C=C/[C@@H](O)Cc1cccc(-c2nc3ccccc3o2)c1 10.1016/j.bmc.2012.04.008
CHEMBL2036312 81933 0 None -8511 3 Mouse 5.8 pKi = 5.8 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 494 12 2 6 4.5 O=C(O)CCCSCCN1C(=O)CC[C@@H]1/C=C/[C@@H](O)Cc1cccc(-c2nc3ccccc3o2)c1 10.1016/j.bmc.2012.04.008
10157810 70561 0 None 3 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]PGE2 from human EP2R expressed in chem1 cells after 2hrs by beta countingDisplacement of [3H]PGE2 from human EP2R expressed in chem1 cells after 2hrs by beta counting
ChEMBL 400 9 1 3 5.6 COc1cc(C/C=C/c2ccccc2/C=C/C(=O)O)ccc1OCc1ccccc1 10.1021/ml300191g
CHEMBL180191 70561 0 None 3 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]PGE2 from human EP2R expressed in chem1 cells after 2hrs by beta countingDisplacement of [3H]PGE2 from human EP2R expressed in chem1 cells after 2hrs by beta counting
ChEMBL 400 9 1 3 5.6 COc1cc(C/C=C/c2ccccc2/C=C/C(=O)O)ccc1OCc1ccccc1 10.1021/ml300191g
44442334 101303 0 None -7 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]PGE2 from human EP2 receptor expressed in HEK293 cellsDisplacement of [3H]PGE2 from human EP2 receptor expressed in HEK293 cells
ChEMBL 327 7 1 2 3.8 CC/C(C)=C\C=C\[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.05.025
CHEMBL251710 101303 0 None -7 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]PGE2 from human EP2 receptor expressed in HEK293 cellsDisplacement of [3H]PGE2 from human EP2 receptor expressed in HEK293 cells
ChEMBL 327 7 1 2 3.8 CC/C(C)=C\C=C\[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.05.025
11495634 21677 13 None -218 4 Mouse 5.8 pKi = 5.8 Binding
Antagonist activity at mouse EP2 receptorAntagonist activity at mouse EP2 receptor
ChEMBL 405 6 1 3 5.4 O=C(O)c1cccc(Cc2cc(Cl)ccc2OCc2ccc(Cl)cc2F)n1 10.1016/j.bmcl.2012.11.046
CHEMBL1207972 21677 13 None -218 4 Mouse 5.8 pKi = 5.8 Binding
Antagonist activity at mouse EP2 receptorAntagonist activity at mouse EP2 receptor
ChEMBL 405 6 1 3 5.4 O=C(O)c1cccc(Cc2cc(Cl)ccc2OCc2ccc(Cl)cc2F)n1 10.1016/j.bmcl.2012.11.046
CHEMBL467114 21677 13 None -218 4 Mouse 5.8 pKi = 5.8 Binding
Antagonist activity at mouse EP2 receptorAntagonist activity at mouse EP2 receptor
ChEMBL 405 6 1 3 5.4 O=C(O)c1cccc(Cc2cc(Cl)ccc2OCc2ccc(Cl)cc2F)n1 10.1016/j.bmcl.2012.11.046
92135977 159675 0 None -275 2 Human 5.8 pKi = 5.8 Binding
Radioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations wRadioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations w
ChEMBL 396 8 2 3 4.2 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2cccc(F)c2)cc1 nan
CHEMBL3974652 159675 0 None -275 2 Human 5.8 pKi = 5.8 Binding
Radioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations wRadioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations w
ChEMBL 396 8 2 3 4.2 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2cccc(F)c2)cc1 nan
52945421 23308 0 None 2 4 Human 7.8 pKi = 7.8 Binding
Binding affinity for human prostanoid EP2 receptorBinding affinity for human prostanoid EP2 receptor
ChEMBL 740 16 2 4 11.2 O=C(O)/C=C/c1ccccc1/C=C/Cc1cccc(OCc2ccccc2)c1.O=C(O)/C=C/c1ccccc1C/C=C\c1cccc(OCc2ccccc2)c1 10.1016/j.bmcl.2004.11.051
CHEMBL1237298 23308 0 None 2 4 Human 7.8 pKi = 7.8 Binding
Binding affinity for human prostanoid EP2 receptorBinding affinity for human prostanoid EP2 receptor
ChEMBL 740 16 2 4 11.2 O=C(O)/C=C/c1ccccc1/C=C/Cc1cccc(OCc2ccccc2)c1.O=C(O)/C=C/c1ccccc1C/C=C\c1cccc(OCc2ccccc2)c1 10.1016/j.bmcl.2004.11.051
21362912 177954 0 None -8 4 Human 5.8 pKi = 5.8 Binding
Binding affinity at human Prostanoid EP2 receptor.Binding affinity at human Prostanoid EP2 receptor.
ChEMBL 535 12 1 5 6.7 O=C(CCCc1ccccc1-c1ccc(CSCCc2ccccc2)cc1)NS(=O)(=O)c1cccs1 10.1016/s0960-894x(02)00518-8
CHEMBL445895 177954 0 None -8 4 Human 5.8 pKi = 5.8 Binding
Binding affinity at human Prostanoid EP2 receptor.Binding affinity at human Prostanoid EP2 receptor.
ChEMBL 535 12 1 5 6.7 O=C(CCCc1ccccc1-c1ccc(CSCCc2ccccc2)cc1)NS(=O)(=O)c1cccs1 10.1016/s0960-894x(02)00518-8
23017362 206757 0 None -45 4 Mouse 5.8 pKi = 5.8 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 414 10 1 4 5.1 O=C(O)CCCc1ccc(Cn2cccn2)cc1OCCc1ccc2ccccc2c1 10.1016/j.bmc.2009.08.007
CHEMBL595157 206757 0 None -45 4 Mouse 5.8 pKi = 5.8 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 414 10 1 4 5.1 O=C(O)CCCc1ccc(Cn2cccn2)cc1OCCc1ccc2ccccc2c1 10.1016/j.bmc.2009.08.007
11577792 166097 19 None -1819 5 Human 5.7 pKi = 5.7 Binding
Antagonist activity at human EP2 receptorAntagonist activity at human EP2 receptor
ChEMBL 414 6 2 4 4.9 C[C@H](NC(=O)c1cc(Cl)cnc1Oc1cccc(F)c1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2017.01.067
CHEMBL4099851 166097 19 None -1819 5 Human 5.7 pKi = 5.7 Binding
Antagonist activity at human EP2 receptorAntagonist activity at human EP2 receptor
ChEMBL 414 6 2 4 4.9 C[C@H](NC(=O)c1cc(Cl)cnc1Oc1cccc(F)c1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2017.01.067
10448293 161200 0 None -41 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]PGE2 from human EP2 receptor expressed in HEK293 cellsDisplacement of [3H]PGE2 from human EP2 receptor expressed in HEK293 cells
ChEMBL 313 6 1 2 3.4 CC(C)=C/C=C/[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.05.025
CHEMBL398947 161200 0 None -41 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]PGE2 from human EP2 receptor expressed in HEK293 cellsDisplacement of [3H]PGE2 from human EP2 receptor expressed in HEK293 cells
ChEMBL 313 6 1 2 3.4 CC(C)=C/C=C/[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.05.025
11855324 149383 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells at pH 6 after 60 minsDisplacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells at pH 6 after 60 mins
ChEMBL 371 6 1 4 4.0 CC(C)(C)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)o2)cc1 nan
CHEMBL3891401 149383 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells at pH 6 after 60 minsDisplacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells at pH 6 after 60 mins
ChEMBL 371 6 1 4 4.0 CC(C)(C)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)o2)cc1 nan
57395059 76249 0 None -12 3 Mouse 7.7 pKi = 7.7 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 418 9 2 6 3.1 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2ccccc2)n1 10.1016/j.bmcl.2011.10.109
CHEMBL1933725 76249 0 None -12 3 Mouse 7.7 pKi = 7.7 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 418 9 2 6 3.1 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2ccccc2)n1 10.1016/j.bmcl.2011.10.109
57395059 76249 0 None -12 3 Mouse 7.7 pKi = 7.7 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 418 9 2 6 3.1 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2ccccc2)n1 10.1016/j.bmc.2012.02.018
CHEMBL1933725 76249 0 None -12 3 Mouse 7.7 pKi = 7.7 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 418 9 2 6 3.1 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2ccccc2)n1 10.1016/j.bmc.2012.02.018
11855865 160056 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 mins
ChEMBL 445 12 2 5 5.2 CCCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3977724 160056 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 mins
ChEMBL 445 12 2 5 5.2 CCCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
57403612 78080 0 None -239 3 Mouse 6.7 pKi = 6.7 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 433 9 2 4 4.2 O=C(O)c1ccc(CCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(Cl)c2)s1 10.1016/j.bmc.2012.02.018
CHEMBL1957434 78080 0 None -239 3 Mouse 6.7 pKi = 6.7 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 433 9 2 4 4.2 O=C(O)c1ccc(CCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(Cl)c2)s1 10.1016/j.bmc.2012.02.018
15948325 9304 45 None -1548 6 Human 5.7 pKi = 5.7 Binding
Binding affinity to human EP2 receptor expressed in HEK293 cellsBinding affinity to human EP2 receptor expressed in HEK293 cells
ChEMBL 603 11 1 8 4.7 CCOc1c2CN(C(=O)c2c(c2c1nccc2)OCC)c1ccc(cc1C)CS(=O)(=O)NC(=O)Cc1ccccc1OC 10.1016/j.bmcl.2008.01.103
5856 9304 45 None -1548 6 Human 5.7 pKi = 5.7 Binding
Binding affinity to human EP2 receptor expressed in HEK293 cellsBinding affinity to human EP2 receptor expressed in HEK293 cells
ChEMBL 603 11 1 8 4.7 CCOc1c2CN(C(=O)c2c(c2c1nccc2)OCC)c1ccc(cc1C)CS(=O)(=O)NC(=O)Cc1ccccc1OC 10.1016/j.bmcl.2008.01.103
CHEMBL402162 9304 45 None -1548 6 Human 5.7 pKi = 5.7 Binding
Binding affinity to human EP2 receptor expressed in HEK293 cellsBinding affinity to human EP2 receptor expressed in HEK293 cells
ChEMBL 603 11 1 8 4.7 CCOc1c2CN(C(=O)c2c(c2c1nccc2)OCC)c1ccc(cc1C)CS(=O)(=O)NC(=O)Cc1ccccc1OC 10.1016/j.bmcl.2008.01.103
59465577 149967 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 408 13 2 2 6.8 CCCCCC(O)c1ccc([C@H]2CC[C@@H](Cl)[C@@H]2CCCCCCC(=O)O)cc1 nan
CHEMBL3896183 149967 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 408 13 2 2 6.8 CCCCCC(O)c1ccc([C@H]2CC[C@@H](Cl)[C@@H]2CCCCCCC(=O)O)cc1 nan
57893982 81939 0 None -4 3 Mouse 8.7 pKi = 8.7 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 508 10 2 6 5.1 Cc1ccc(-c2cccc(C[C@H](O)/C=C/[C@H]3CCC(=O)N3CCSc3nc(C(=O)O)cs3)c2)cc1 10.1016/j.bmc.2012.04.008
CHEMBL2036318 81939 0 None -4 3 Mouse 8.7 pKi = 8.7 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 508 10 2 6 5.1 Cc1ccc(-c2cccc(C[C@H](O)/C=C/[C@H]3CCC(=O)N3CCSc3nc(C(=O)O)cs3)c2)cc1 10.1016/j.bmc.2012.04.008
57464006 81943 0 None -17 4 Mouse 8.7 pKi = 8.7 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 534 10 2 7 5.5 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(-c3cc4ccccc4o3)c2)n1 10.1016/j.bmc.2012.04.008
CHEMBL2036322 81943 0 None -17 4 Mouse 8.7 pKi = 8.7 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 534 10 2 7 5.5 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(-c3cc4ccccc4o3)c2)n1 10.1016/j.bmc.2012.04.008
9807448 209951 0 None -1 4 Mouse 8.7 pKi = 8.7 Binding
Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.
ChEMBL 398 11 3 3 4.7 CCC1([C@@H](O)C/C=C/[C@H]2[C@H](O)C[C@@H](Cl)[C@@H]2C/C=C\CCCC(=O)O)CCC1 10.1016/s0960-894x(01)00359-6
CHEMBL64246 209951 0 None -1 4 Mouse 8.7 pKi = 8.7 Binding
Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.
ChEMBL 398 11 3 3 4.7 CCC1([C@@H](O)C/C=C/[C@H]2[C@H](O)C[C@@H](Cl)[C@@H]2C/C=C\CCCC(=O)O)CCC1 10.1016/s0960-894x(01)00359-6
67078538 135976 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding Assay: Measurement of EP2 receptor binding affinity was carried out according to the method of Abramovitz et al. (Biochimica et Biophysica Acta, 1483, 285 (2000)). A test compound dissolved in dimethylsulfoxide and [3H]PGE2 (NET-428, available from PerkinElmer Inc.) (final concentration: 10 nM) were added to a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2, 1 mM EDTA) in which 10 μg of a membrane fraction (ES-562-M, available from Euroscreen S.A.) of HEK293 cells expressing human EP2 receptor had been suspended, followed by incubation at 30° C. for 60 minutes. The membrane fraction was recovered on glass fiber filter paper (GF/B, available from Whatman PLC) using a cell harvester (M30R, available from Brandel Inc.), and after washing with a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2), radioactivity was measured with a liquid scintillation analyzer (2000CA, available from Packard).Binding Assay: Measurement of EP2 receptor binding affinity was carried out according to the method of Abramovitz et al. (Biochimica et Biophysica Acta, 1483, 285 (2000)). A test compound dissolved in dimethylsulfoxide and [3H]PGE2 (NET-428, available from PerkinElmer Inc.) (final concentration: 10 nM) were added to a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2, 1 mM EDTA) in which 10 μg of a membrane fraction (ES-562-M, available from Euroscreen S.A.) of HEK293 cells expressing human EP2 receptor had been suspended, followed by incubation at 30° C. for 60 minutes. The membrane fraction was recovered on glass fiber filter paper (GF/B, available from Whatman PLC) using a cell harvester (M30R, available from Brandel Inc.), and after washing with a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2), radioactivity was measured with a liquid scintillation analyzer (2000CA, available from Packard).
ChEMBL 269 3 3 3 3.3 O=C(O)c1[nH]c(-c2ccoc2)cc1-c1ccc(O)cc1 nan
CHEMBL3670654 135976 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding Assay: Measurement of EP2 receptor binding affinity was carried out according to the method of Abramovitz et al. (Biochimica et Biophysica Acta, 1483, 285 (2000)). A test compound dissolved in dimethylsulfoxide and [3H]PGE2 (NET-428, available from PerkinElmer Inc.) (final concentration: 10 nM) were added to a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2, 1 mM EDTA) in which 10 μg of a membrane fraction (ES-562-M, available from Euroscreen S.A.) of HEK293 cells expressing human EP2 receptor had been suspended, followed by incubation at 30° C. for 60 minutes. The membrane fraction was recovered on glass fiber filter paper (GF/B, available from Whatman PLC) using a cell harvester (M30R, available from Brandel Inc.), and after washing with a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2), radioactivity was measured with a liquid scintillation analyzer (2000CA, available from Packard).Binding Assay: Measurement of EP2 receptor binding affinity was carried out according to the method of Abramovitz et al. (Biochimica et Biophysica Acta, 1483, 285 (2000)). A test compound dissolved in dimethylsulfoxide and [3H]PGE2 (NET-428, available from PerkinElmer Inc.) (final concentration: 10 nM) were added to a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2, 1 mM EDTA) in which 10 μg of a membrane fraction (ES-562-M, available from Euroscreen S.A.) of HEK293 cells expressing human EP2 receptor had been suspended, followed by incubation at 30° C. for 60 minutes. The membrane fraction was recovered on glass fiber filter paper (GF/B, available from Whatman PLC) using a cell harvester (M30R, available from Brandel Inc.), and after washing with a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2), radioactivity was measured with a liquid scintillation analyzer (2000CA, available from Packard).
ChEMBL 269 3 3 3 3.3 O=C(O)c1[nH]c(-c2ccoc2)cc1-c1ccc(O)cc1 nan
44303952 107663 0 None 41 4 Mouse 7.7 pKi = 7.7 Binding
Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.
ChEMBL 420 14 3 4 4.8 CCCCCC1([C@@H](O)C/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2C/C=C\CCCC(=O)O)CCC1 10.1016/s0960-894x(01)00359-6
CHEMBL293697 107663 0 None 41 4 Mouse 7.7 pKi = 7.7 Binding
Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.
ChEMBL 420 14 3 4 4.8 CCCCCC1([C@@H](O)C/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2C/C=C\CCCC(=O)O)CCC1 10.1016/s0960-894x(01)00359-6
10361472 71982 0 None -199 3 Mouse 5.7 pKi = 5.7 Binding
Ability to inhibit the binding of [3H]-PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP2Ability to inhibit the binding of [3H]-PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP2
ChEMBL 365 7 1 4 4.4 CCCCOc1ccc(C(=O)n2c(C)cc3c(CC(=O)O)cccc32)cc1 10.1016/j.bmcl.2004.07.039
CHEMBL182555 71982 0 None -199 3 Mouse 5.7 pKi = 5.7 Binding
Ability to inhibit the binding of [3H]-PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP2Ability to inhibit the binding of [3H]-PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP2
ChEMBL 365 7 1 4 4.4 CCCCOc1ccc(C(=O)n2c(C)cc3c(CC(=O)O)cccc32)cc1 10.1016/j.bmcl.2004.07.039
10118889 213052 0 None -74 4 Human 5.7 pKi = 5.7 Binding
Binding affinity at human Prostanoid EP2 receptor.Binding affinity at human Prostanoid EP2 receptor.
ChEMBL 521 11 1 5 6.3 O=C(CCc1ccccc1-c1cccc(CSCCc2ccccc2)c1)NS(=O)(=O)c1cccs1 10.1016/s0960-894x(02)00518-8
CHEMBL86933 213052 0 None -74 4 Human 5.7 pKi = 5.7 Binding
Binding affinity at human Prostanoid EP2 receptor.Binding affinity at human Prostanoid EP2 receptor.
ChEMBL 521 11 1 5 6.3 O=C(CCc1ccccc1-c1cccc(CSCCc2ccccc2)c1)NS(=O)(=O)c1cccs1 10.1016/s0960-894x(02)00518-8
11187675 71988 0 None -61 4 Mouse 5.7 pKi = 5.7 Binding
Binding affinity for mouse Prostanoid EP2 receptorBinding affinity for mouse Prostanoid EP2 receptor
ChEMBL 365 7 1 4 4.4 CCCCOc1ccc(C(=O)n2c(C)c(CC(=O)O)c3ccccc32)cc1 10.1016/j.bmcl.2004.06.006
CHEMBL182572 71988 0 None -61 4 Mouse 5.7 pKi = 5.7 Binding
Binding affinity for mouse Prostanoid EP2 receptorBinding affinity for mouse Prostanoid EP2 receptor
ChEMBL 365 7 1 4 4.4 CCCCOc1ccc(C(=O)n2c(C)c(CC(=O)O)c3ccccc32)cc1 10.1016/j.bmcl.2004.06.006
12002527 81935 0 None -19952 2 Mouse 5.7 pKi = 5.7 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 493 12 2 5 5.1 O=C(O)CCCSCCN1C(=O)CC[C@@H]1/C=C/[C@@H](O)Cc1cccc(-c2cc3ccccc3o2)c1 10.1016/j.bmc.2012.04.008
CHEMBL2036314 81935 0 None -19952 2 Mouse 5.7 pKi = 5.7 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 493 12 2 5 5.1 O=C(O)CCCSCCN1C(=O)CC[C@@H]1/C=C/[C@@H](O)Cc1cccc(-c2cc3ccccc3o2)c1 10.1016/j.bmc.2012.04.008
24953628 207382 0 None -63 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]PGE2 from human EP2 receptor expressed in HEK293-EBNA cells by scintillation countingDisplacement of [3H]PGE2 from human EP2 receptor expressed in HEK293-EBNA cells by scintillation counting
ChEMBL 427 6 2 3 5.8 Cc1sc(C)c(C(=O)N[C@@H](C)c2ccc(C(=O)O)cc2)c1Cc1ccc(Cl)cc1 10.1021/jm901771h
CHEMBL599262 207382 0 None -63 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]PGE2 from human EP2 receptor expressed in HEK293-EBNA cells by scintillation countingDisplacement of [3H]PGE2 from human EP2 receptor expressed in HEK293-EBNA cells by scintillation counting
ChEMBL 427 6 2 3 5.8 Cc1sc(C)c(C(=O)N[C@@H](C)c2ccc(C(=O)O)cc2)c1Cc1ccc(Cl)cc1 10.1021/jm901771h
57529188 153973 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 mins
ChEMBL 415 11 2 5 4.3 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)o2)cc1 nan
CHEMBL3928130 153973 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 mins
ChEMBL 415 11 2 5 4.3 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)o2)cc1 nan
57529188 153973 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 415 11 2 5 4.3 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)o2)cc1 nan
CHEMBL3928130 153973 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 415 11 2 5 4.3 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)o2)cc1 nan
44444721 161185 0 None -77 2 Human 5.7 pKi = 5.7 Binding
Binding affinity at human prostaglandin EP2 receptorBinding affinity at human prostaglandin EP2 receptor
ChEMBL 508 9 2 4 3.0 O=C(O)c1ccc(CCN2C(=O)CCN2CC[C@@H](O)Cc2cccc(I)c2)cc1 10.1016/j.bmcl.2007.09.074
CHEMBL398827 161185 0 None -77 2 Human 5.7 pKi = 5.7 Binding
Binding affinity at human prostaglandin EP2 receptorBinding affinity at human prostaglandin EP2 receptor
ChEMBL 508 9 2 4 3.0 O=C(O)c1ccc(CCN2C(=O)CCN2CC[C@@H](O)Cc2cccc(I)c2)cc1 10.1016/j.bmcl.2007.09.074
44455084 104643 0 None -10 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]PGE2 from human EP2 receptorDisplacement of [3H]PGE2 from human EP2 receptor
ChEMBL 399 10 2 3 4.2 CCCCC1([C@@H](O)/C=C/[C@H]2CCC(=O)N2CCc2ccc(C(=O)O)cc2)CCC1 10.1016/j.bmcl.2007.11.020
CHEMBL272277 104643 0 None -10 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]PGE2 from human EP2 receptorDisplacement of [3H]PGE2 from human EP2 receptor
ChEMBL 399 10 2 3 4.2 CCCCC1([C@@H](O)/C=C/[C@H]2CCC(=O)N2CCc2ccc(C(=O)O)cc2)CCC1 10.1016/j.bmcl.2007.11.020
58932681 81947 0 None -100 3 Mouse 7.7 pKi = 7.7 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 549 10 2 8 5.2 Cc1ccc2oc(-c3cccc(C[C@H](O)/C=C/[C@H]4CCC(=O)N4CCSc4nc(C(=O)O)cs4)c3)nc2c1 10.1016/j.bmc.2012.04.008
CHEMBL2036326 81947 0 None -100 3 Mouse 7.7 pKi = 7.7 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 549 10 2 8 5.2 Cc1ccc2oc(-c3cccc(C[C@H](O)/C=C/[C@H]4CCC(=O)N4CCSc4nc(C(=O)O)cs4)c3)nc2c1 10.1016/j.bmc.2012.04.008
10116116 71185 0 None -26 5 Mouse 6.7 pKi = 6.7 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 470 6 1 6 4.5 Cc1c(CC(=O)O)c2ccccc2n1C(=O)c1ccc(OC[C@@H]2CN(C)c3ccccc3O2)cc1 10.1016/j.bmc.2011.06.014
CHEMBL1813115 71185 0 None -26 5 Mouse 6.7 pKi = 6.7 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 470 6 1 6 4.5 Cc1c(CC(=O)O)c2ccccc2n1C(=O)c1ccc(OC[C@@H]2CN(C)c3ccccc3O2)cc1 10.1016/j.bmc.2011.06.014
10206535 73346 0 None -398 4 Mouse 5.7 pKi = 5.7 Binding
Ability to inhibit the binding of [3H]-PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP2Ability to inhibit the binding of [3H]-PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP2
ChEMBL 488 6 1 6 4.7 Cc1cc2c(CC(=O)O)cccc2n1C(=O)c1ccc(OC[C@@H]2CN(C)c3ccc(F)cc3O2)cc1 10.1016/j.bmcl.2004.07.039
CHEMBL185251 73346 0 None -398 4 Mouse 5.7 pKi = 5.7 Binding
Ability to inhibit the binding of [3H]-PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP2Ability to inhibit the binding of [3H]-PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP2
ChEMBL 488 6 1 6 4.7 Cc1cc2c(CC(=O)O)cccc2n1C(=O)c1ccc(OC[C@@H]2CN(C)c3ccc(F)cc3O2)cc1 10.1016/j.bmcl.2004.07.039
44320126 213191 0 None -17 4 Human 5.7 pKi = 5.7 Binding
Binding affinity at human Prostanoid EP2 receptor.Binding affinity at human Prostanoid EP2 receptor.
ChEMBL 537 11 1 7 6.2 Cc1cccc(OCCCOc2ccc(-c3ccccc3COC(=O)NS(=O)(=O)c3cccs3)cc2)c1 10.1016/s0960-894x(02)00518-8
CHEMBL87816 213191 0 None -17 4 Human 5.7 pKi = 5.7 Binding
Binding affinity at human Prostanoid EP2 receptor.Binding affinity at human Prostanoid EP2 receptor.
ChEMBL 537 11 1 7 6.2 Cc1cccc(OCCCOc2ccc(-c3ccccc3COC(=O)NS(=O)(=O)c3cccs3)cc2)c1 10.1016/s0960-894x(02)00518-8
22009011 70847 0 None -208 4 Human 5.7 pKi = 5.7 Binding
Binding affinity for human prostanoid EP2 receptorBinding affinity for human prostanoid EP2 receptor
ChEMBL 468 8 2 3 6.7 Cc1cccc(/C=C/C(O)c2ccccc2/C=C/C(=O)O)c1OCc1c(Cl)cccc1Cl 10.1016/j.bmcl.2004.11.051
CHEMBL180742 70847 0 None -208 4 Human 5.7 pKi = 5.7 Binding
Binding affinity for human prostanoid EP2 receptorBinding affinity for human prostanoid EP2 receptor
ChEMBL 468 8 2 3 6.7 Cc1cccc(/C=C/C(O)c2ccccc2/C=C/C(=O)O)c1OCc1c(Cl)cccc1Cl 10.1016/j.bmcl.2004.11.051
11187675 71988 0 None -61 4 Mouse 5.7 pKi = 5.7 Binding
Binding affinity for mouse Prostanoid EP2 receptorBinding affinity for mouse Prostanoid EP2 receptor
ChEMBL 365 7 1 4 4.4 CCCCOc1ccc(C(=O)n2c(C)c(CC(=O)O)c3ccccc32)cc1 10.1016/j.bmcl.2004.06.006
CHEMBL182572 71988 0 None -61 4 Mouse 5.7 pKi = 5.7 Binding
Binding affinity for mouse Prostanoid EP2 receptorBinding affinity for mouse Prostanoid EP2 receptor
ChEMBL 365 7 1 4 4.4 CCCCOc1ccc(C(=O)n2c(C)c(CC(=O)O)c3ccccc32)cc1 10.1016/j.bmcl.2004.06.006
44419380 89854 0 None -208 4 Human 5.7 pKi = 5.7 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 529 10 1 5 6.4 Cc1ccc(OCc2ccccc2)c(/C=C/Cc2ccccc2/C=C/C(=O)NS(=O)(=O)c2cccs2)c1 10.1016/j.bmcl.2006.08.025
CHEMBL218178 89854 0 None -208 4 Human 5.7 pKi = 5.7 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 529 10 1 5 6.4 Cc1ccc(OCc2ccccc2)c(/C=C/Cc2ccccc2/C=C/C(=O)NS(=O)(=O)c2cccs2)c1 10.1016/j.bmcl.2006.08.025
44419384 89855 0 None -208 4 Human 5.7 pKi = 5.7 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 529 10 1 5 6.4 Cc1ccc(OCc2ccccc2)c(C/C=C/c2ccccc2/C=C/C(=O)NS(=O)(=O)c2cccs2)c1 10.1016/j.bmcl.2006.08.025
CHEMBL218179 89855 0 None -208 4 Human 5.7 pKi = 5.7 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 529 10 1 5 6.4 Cc1ccc(OCc2ccccc2)c(C/C=C/c2ccccc2/C=C/C(=O)NS(=O)(=O)c2cccs2)c1 10.1016/j.bmcl.2006.08.025
57894081 81929 0 None -3467 2 Mouse 5.7 pKi = 5.7 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 503 12 2 4 5.6 O=C(O)CCCSCCN1C(=O)CC[C@@H]1/C=C/[C@@H](O)Cc1cccc(-c2ccc3ccccc3c2)c1 10.1016/j.bmc.2012.04.008
CHEMBL2036308 81929 0 None -3467 2 Mouse 5.7 pKi = 5.7 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 503 12 2 4 5.6 O=C(O)CCCSCCN1C(=O)CC[C@@H]1/C=C/[C@@H](O)Cc1cccc(-c2ccc3ccccc3c2)c1 10.1016/j.bmc.2012.04.008
23017746 206628 0 None -13 3 Mouse 5.7 pKi = 5.7 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 414 8 1 3 6.2 O=C(O)/C=C/c1ccc(Cc2cccs2)cc1OCCc1ccc2ccccc2c1 10.1016/j.bmc.2009.08.007
CHEMBL594365 206628 0 None -13 3 Mouse 5.7 pKi = 5.7 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 414 8 1 3 6.2 O=C(O)/C=C/c1ccc(Cc2cccs2)cc1OCCc1ccc2ccccc2c1 10.1016/j.bmc.2009.08.007
9846782 107682 7 None -676 3 Mouse 5.7 pKi = 5.7 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptor
ChEMBL 454 13 3 7 2.6 COCc1cccc(C[C@H](O)/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2SCCCSCC(=O)O)c1 10.1016/s0960-894x(01)00364-x
CHEMBL293856 107682 7 None -676 3 Mouse 5.7 pKi = 5.7 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptor
ChEMBL 454 13 3 7 2.6 COCc1cccc(C[C@H](O)/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2SCCCSCC(=O)O)c1 10.1016/s0960-894x(01)00364-x
15907748 118241 0 None -147 4 Human 4.7 pKi = 4.7 Binding
Affinity at human EP2 receptor.Affinity at human EP2 receptor.
ChEMBL 615 7 2 4 7.0 C[C@H](NC(=O)NS(=O)(=O)c1ccccc1-c1ccc(CN2C(=O)c3ccccc3CCc3ccccc32)cc1)c1ccccc1 10.1016/s0960-894x(99)00465-5
CHEMBL327597 118241 0 None -147 4 Human 4.7 pKi = 4.7 Binding
Affinity at human EP2 receptor.Affinity at human EP2 receptor.
ChEMBL 615 7 2 4 7.0 C[C@H](NC(=O)NS(=O)(=O)c1ccccc1-c1ccc(CN2C(=O)c3ccccc3CCc3ccccc32)cc1)c1ccccc1 10.1016/s0960-894x(99)00465-5
138 9855 88 None -19 18 Mouse 7.7 pKi = 7.7 Binding
Affinity for mouse Prostanoid EP2 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP2 receptor expressed in CHO cells
ChEMBL 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 10.1016/s0960-894x(01)00365-1
149351 9855 88 None -19 18 Mouse 7.7 pKi = 7.7 Binding
Affinity for mouse Prostanoid EP2 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP2 receptor expressed in CHO cells
ChEMBL 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 10.1016/s0960-894x(01)00365-1
1882 9855 88 None -19 18 Mouse 7.7 pKi = 7.7 Binding
Affinity for mouse Prostanoid EP2 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP2 receptor expressed in CHO cells
ChEMBL 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 10.1016/s0960-894x(01)00365-1
5280723 9855 88 None -19 18 Mouse 7.7 pKi = 7.7 Binding
Affinity for mouse Prostanoid EP2 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP2 receptor expressed in CHO cells
ChEMBL 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 10.1016/s0960-894x(01)00365-1
CHEMBL495 9855 88 None -19 18 Mouse 7.7 pKi = 7.7 Binding
Affinity for mouse Prostanoid EP2 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP2 receptor expressed in CHO cells
ChEMBL 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 10.1016/s0960-894x(01)00365-1
DB00770 9855 88 None -19 18 Mouse 7.7 pKi = 7.7 Binding
Affinity for mouse Prostanoid EP2 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP2 receptor expressed in CHO cells
ChEMBL 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 10.1016/s0960-894x(01)00365-1
1883 9856 75 None -15 24 Mouse 7.7 pKi = 7.7 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmcl.2011.10.109
1916 9856 75 None -15 24 Mouse 7.7 pKi = 7.7 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmcl.2011.10.109
5280360 9856 75 None -15 24 Mouse 7.7 pKi = 7.7 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmcl.2011.10.109
913 9856 75 None -15 24 Mouse 7.7 pKi = 7.7 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmcl.2011.10.109
CHEMBL548 9856 75 None -15 24 Mouse 7.7 pKi = 7.7 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmcl.2011.10.109
DB00917 9856 75 None -15 24 Mouse 7.7 pKi = 7.7 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmcl.2011.10.109
1883 9856 75 None -15 24 Mouse 7.7 pKi = 7.7 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmc.2012.02.018
1916 9856 75 None -15 24 Mouse 7.7 pKi = 7.7 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmc.2012.02.018
5280360 9856 75 None -15 24 Mouse 7.7 pKi = 7.7 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmc.2012.02.018
913 9856 75 None -15 24 Mouse 7.7 pKi = 7.7 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmc.2012.02.018
CHEMBL548 9856 75 None -15 24 Mouse 7.7 pKi = 7.7 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmc.2012.02.018
DB00917 9856 75 None -15 24 Mouse 7.7 pKi = 7.7 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmc.2012.02.018
57396660 78083 0 None -1819 2 Mouse 7.7 pKi = 7.7 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 544 10 2 6 5.9 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(-c3ccc4ccccc4c3)c2)n1 10.1016/j.bmc.2012.02.018
CHEMBL1957437 78083 0 None -1819 2 Mouse 7.7 pKi = 7.7 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 544 10 2 6 5.9 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(-c3ccc4ccccc4c3)c2)n1 10.1016/j.bmc.2012.02.018
57396660 78083 0 None -1819 2 Mouse 7.7 pKi = 7.7 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 544 10 2 6 5.9 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(-c3ccc4ccccc4c3)c2)n1 10.1016/j.bmc.2012.04.008
CHEMBL1957437 78083 0 None -1819 2 Mouse 7.7 pKi = 7.7 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 544 10 2 6 5.9 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(-c3ccc4ccccc4c3)c2)n1 10.1016/j.bmc.2012.04.008
10348321 81946 0 None -87 3 Mouse 7.7 pKi = 7.7 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 585 10 2 8 6.0 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(-c3nc4cc(Cl)ccc4s3)c2)n1 10.1016/j.bmc.2012.04.008
CHEMBL2036325 81946 0 None -87 3 Mouse 7.7 pKi = 7.7 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 585 10 2 8 6.0 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(-c3nc4cc(Cl)ccc4s3)c2)n1 10.1016/j.bmc.2012.04.008
58932678 82063 0 None -104 3 Mouse 7.7 pKi = 7.7 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 549 10 2 8 5.2 Cc1cccc2oc(-c3cccc(C[C@H](O)/C=C/[C@H]4CCC(=O)N4CCSc4nc(C(=O)O)cs4)c3)nc12 10.1016/j.bmc.2012.04.008
CHEMBL2037290 82063 0 None -104 3 Mouse 7.7 pKi = 7.7 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 549 10 2 8 5.2 Cc1cccc2oc(-c3cccc(C[C@H](O)/C=C/[C@H]4CCC(=O)N4CCSc4nc(C(=O)O)cs4)c3)nc12 10.1016/j.bmc.2012.04.008
56672020 71599 0 None -1 2 Mouse 7.7 pKi = 7.7 Binding
Displacement of [3H]PGE2 from mouse prostaglandin EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]PGE2 from mouse prostaglandin EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 484 7 2 5 4.6 CN1C[C@@H](COc2ccc(C(=O)Nc3cc(CC(=O)O)ccc3F)c(Cl)c2)Oc2ccccc21 10.1016/j.bmc.2011.08.007
CHEMBL1819623 71599 0 None -1 2 Mouse 7.7 pKi = 7.7 Binding
Displacement of [3H]PGE2 from mouse prostaglandin EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]PGE2 from mouse prostaglandin EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 484 7 2 5 4.6 CN1C[C@@H](COc2ccc(C(=O)Nc3cc(CC(=O)O)ccc3F)c(Cl)c2)Oc2ccccc21 10.1016/j.bmc.2011.08.007
11337782 91718 0 None -12 3 Human 6.7 pKi = 6.7 Binding
Binding affinity to human EP2 receptorBinding affinity to human EP2 receptor
ChEMBL 373 10 2 3 3.6 O=C(O)c1ccc(CCN2C(=O)CC[C@@H]2CC[C@@H](O)CCC2CCC2)cc1 10.1021/jm049290a
CHEMBL223744 91718 0 None -12 3 Human 6.7 pKi = 6.7 Binding
Binding affinity to human EP2 receptorBinding affinity to human EP2 receptor
ChEMBL 373 10 2 3 3.6 O=C(O)c1ccc(CCN2C(=O)CC[C@@H]2CC[C@@H](O)CCC2CCC2)cc1 10.1021/jm049290a
9863804 100873 0 None -8 2 Human 5.7 pKi = 5.7 Binding
Binding affinity at human prostaglandin EP2 receptorBinding affinity at human prostaglandin EP2 receptor
ChEMBL 362 11 2 4 2.7 CCCCCC(O)CCN1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.09.074
CHEMBL249136 100873 0 None -8 2 Human 5.7 pKi = 5.7 Binding
Binding affinity at human prostaglandin EP2 receptorBinding affinity at human prostaglandin EP2 receptor
ChEMBL 362 11 2 4 2.7 CCCCCC(O)CCN1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.09.074
9938669 174837 0 None -154 4 Human 4.7 pKi = 4.7 Binding
Affinity at human EP2 receptor.Affinity at human EP2 receptor.
ChEMBL 602 8 1 5 6.2 O=C(COc1ccccc1)NS(=O)(=O)c1ccccc1-c1ccc(CN2C(=O)c3ccccc3CCc3ccccc32)cc1 10.1016/s0960-894x(99)00465-5
CHEMBL432380 174837 0 None -154 4 Human 4.7 pKi = 4.7 Binding
Affinity at human EP2 receptor.Affinity at human EP2 receptor.
ChEMBL 602 8 1 5 6.2 O=C(COc1ccccc1)NS(=O)(=O)c1ccccc1-c1ccc(CN2C(=O)c3ccccc3CCc3ccccc32)cc1 10.1016/s0960-894x(99)00465-5
10113454 184280 0 None -1380 3 Human 4.7 pKi = 4.7 Binding
Binding affinity was determined against prostanoid EP2 receptorBinding affinity was determined against prostanoid EP2 receptor
ChEMBL 429 12 2 3 4.4 O=C(O)CCCCCCN1C(=O)CC[C@@H]1CC[C@@H](O)Cc1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2004.01.063
CHEMBL46395 184280 0 None -1380 3 Human 4.7 pKi = 4.7 Binding
Binding affinity was determined against prostanoid EP2 receptorBinding affinity was determined against prostanoid EP2 receptor
ChEMBL 429 12 2 3 4.4 O=C(O)CCCCCCN1C(=O)CC[C@@H]1CC[C@@H](O)Cc1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2004.01.063
118517483 151049 0 None -93 2 Human 5.7 pKi = 5.7 Binding
Radioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations wRadioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations w
ChEMBL 396 8 2 3 4.2 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2ccccc2F)cc1 nan
CHEMBL3904946 151049 0 None -93 2 Human 5.7 pKi = 5.7 Binding
Radioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations wRadioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations w
ChEMBL 396 8 2 3 4.2 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2ccccc2F)cc1 nan
11488860 26063 0 None -5370 8 Human 5.6 pKi = 5.6 Binding
Binding affinity to prostanoid receptor EP2 receptorBinding affinity to prostanoid receptor EP2 receptor
ChEMBL 497 5 1 4 5.7 C[C@@H](c1ccc(C(F)(F)F)cc1)n1c2c(c3cc(F)cc(S(C)(=O)=O)c31)CCC[C@@H]2CC(=O)O 10.1016/j.bmcl.2010.10.018
CHEMBL1290413 26063 0 None -5370 8 Human 5.6 pKi = 5.6 Binding
Binding affinity to prostanoid receptor EP2 receptorBinding affinity to prostanoid receptor EP2 receptor
ChEMBL 497 5 1 4 5.7 C[C@@H](c1ccc(C(F)(F)F)cc1)n1c2c(c3cc(F)cc(S(C)(=O)=O)c31)CCC[C@@H]2CC(=O)O 10.1016/j.bmcl.2010.10.018
24760055 150666 0 None -2 2 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 mins
ChEMBL 411 10 2 4 4.6 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COc2ccc(C(=O)O)cc2)cc1 nan
CHEMBL3901873 150666 0 None -2 2 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 mins
ChEMBL 411 10 2 4 4.6 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COc2ccc(C(=O)O)cc2)cc1 nan
24760055 150666 0 None -2 2 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 411 10 2 4 4.6 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COc2ccc(C(=O)O)cc2)cc1 nan
CHEMBL3901873 150666 0 None -2 2 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 411 10 2 4 4.6 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COc2ccc(C(=O)O)cc2)cc1 nan
11855591 151214 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 mins
ChEMBL 435 9 2 5 4.0 O=C(O)c1ccc(COC[C@H]2CCC(=O)N2c2ccc(C(O)Cc3ccccc3)cc2)o1 nan
CHEMBL3906402 151214 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 mins
ChEMBL 435 9 2 5 4.0 O=C(O)c1ccc(COC[C@H]2CCC(=O)N2c2ccc(C(O)Cc3ccccc3)cc2)o1 nan
11855591 151214 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 435 9 2 5 4.0 O=C(O)c1ccc(COC[C@H]2CCC(=O)N2c2ccc(C(O)Cc3ccccc3)cc2)o1 nan
CHEMBL3906402 151214 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 435 9 2 5 4.0 O=C(O)c1ccc(COC[C@H]2CCC(=O)N2c2ccc(C(O)Cc3ccccc3)cc2)o1 nan
10414412 81941 0 None -6 3 Mouse 7.6 pKi = 7.6 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 522 10 2 6 5.4 Cc1ccc(-c2cccc(C[C@H](O)/C=C/[C@H]3CCC(=O)N3CCSc3nc(C(=O)O)cs3)c2)c(C)c1 10.1016/j.bmc.2012.04.008
CHEMBL2036320 81941 0 None -6 3 Mouse 7.6 pKi = 7.6 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 522 10 2 6 5.4 Cc1ccc(-c2cccc(C[C@H](O)/C=C/[C@H]3CCC(=O)N3CCSc3nc(C(=O)O)cs3)c2)c(C)c1 10.1016/j.bmc.2012.04.008
11408533 148105 0 None -89 3 Human 6.6 pKi = 6.6 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 459 6 1 5 4.5 CC(=O)c1cc(S(C)(=O)=O)cc2c3c(n(Cc4ccc(Cl)cc4)c12)[C@@H](CC(=O)O)CC3 10.1016/j.bmcl.2006.02.062
CHEMBL383484 148105 0 None -89 3 Human 6.6 pKi = 6.6 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 459 6 1 5 4.5 CC(=O)c1cc(S(C)(=O)=O)cc2c3c(n(Cc4ccc(Cl)cc4)c12)[C@@H](CC(=O)O)CC3 10.1016/j.bmcl.2006.02.062
11408533 148105 0 None -89 3 Human 6.6 pKi = 6.6 Binding
Binding affinity to human EP2 receptor expressed in HEK293 cellsBinding affinity to human EP2 receptor expressed in HEK293 cells
ChEMBL 459 6 1 5 4.5 CC(=O)c1cc(S(C)(=O)=O)cc2c3c(n(Cc4ccc(Cl)cc4)c12)[C@@H](CC(=O)O)CC3 10.1021/jm0603668
CHEMBL383484 148105 0 None -89 3 Human 6.6 pKi = 6.6 Binding
Binding affinity to human EP2 receptor expressed in HEK293 cellsBinding affinity to human EP2 receptor expressed in HEK293 cells
ChEMBL 459 6 1 5 4.5 CC(=O)c1cc(S(C)(=O)=O)cc2c3c(n(Cc4ccc(Cl)cc4)c12)[C@@H](CC(=O)O)CC3 10.1021/jm0603668
11743212 23936 0 None -758 7 Human 5.6 pKi = 5.6 Binding
Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 426 7 1 3 6.8 O=C(O)C1CC1c1ccccc1-c1csc(-c2ccccc2OCc2ccccc2)c1 10.1016/s0960-894x(03)00794-7
CHEMBL125588 23936 0 None -758 7 Human 5.6 pKi = 5.6 Binding
Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 426 7 1 3 6.8 O=C(O)C1CC1c1ccccc1-c1csc(-c2ccccc2OCc2ccccc2)c1 10.1016/s0960-894x(03)00794-7
56658143 71579 0 None -16 6 Mouse 5.6 pKi = 5.6 Binding
Displacement of [3H]PGE2 from mouse prostaglandin EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]PGE2 from mouse prostaglandin EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 468 8 2 6 3.4 CN1C[C@@H](COc2ccc(S(=O)(=O)Nc3cccc(CC(=O)O)c3)cc2)Oc2ccccc21 10.1016/j.bmc.2011.08.007
CHEMBL1819604 71579 0 None -16 6 Mouse 5.6 pKi = 5.6 Binding
Displacement of [3H]PGE2 from mouse prostaglandin EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]PGE2 from mouse prostaglandin EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 468 8 2 6 3.4 CN1C[C@@H](COc2ccc(S(=O)(=O)Nc3cccc(CC(=O)O)c3)cc2)Oc2ccccc21 10.1016/j.bmc.2011.08.007
9809136 113666 0 None -2290 8 Human 4.6 pKi = 4.6 Binding
Affinity at human EP2 receptor.Affinity at human EP2 receptor.
ChEMBL 614 7 1 4 7.1 CC(C)(C(=O)NS(=O)(=O)c1ccccc1-c1ccc(CN2C(=O)c3ccccc3CCc3ccccc32)cc1)c1ccccc1 10.1016/s0960-894x(99)00465-5
CHEMBL314533 113666 0 None -2290 8 Human 4.6 pKi = 4.6 Binding
Affinity at human EP2 receptor.Affinity at human EP2 receptor.
ChEMBL 614 7 1 4 7.1 CC(C)(C(=O)NS(=O)(=O)c1ccccc1-c1ccc(CN2C(=O)c3ccccc3CCc3ccccc32)cc1)c1ccccc1 10.1016/s0960-894x(99)00465-5
9874010 213969 0 None -1348 8 Human 4.6 pKi = 4.6 Binding
Affinity at human EP2 receptor.Affinity at human EP2 receptor.
ChEMBL 629 8 1 4 6.9 CN(CCc1ccccc1)C(=O)NS(=O)(=O)c1ccccc1-c1ccc(CN2C(=O)c3ccccc3CCc3ccccc32)cc1 10.1016/s0960-894x(99)00465-5
CHEMBL92539 213969 0 None -1348 8 Human 4.6 pKi = 4.6 Binding
Affinity at human EP2 receptor.Affinity at human EP2 receptor.
ChEMBL 629 8 1 4 6.9 CN(CCc1ccccc1)C(=O)NS(=O)(=O)c1ccccc1-c1ccc(CN2C(=O)c3ccccc3CCc3ccccc32)cc1 10.1016/s0960-894x(99)00465-5
10229201 162355 0 None -87 2 Human 5.6 pKi = 5.6 Binding
Binding affinity at human prostaglandin EP2 receptorBinding affinity at human prostaglandin EP2 receptor
ChEMBL 508 9 2 4 3.0 O=C(O)c1ccc(CCN2C(=O)CCN2CCC(O)Cc2cccc(I)c2)cc1 10.1016/j.bmcl.2007.09.074
CHEMBL404414 162355 0 None -87 2 Human 5.6 pKi = 5.6 Binding
Binding affinity at human prostaglandin EP2 receptorBinding affinity at human prostaglandin EP2 receptor
ChEMBL 508 9 2 4 3.0 O=C(O)c1ccc(CCN2C(=O)CCN2CCC(O)Cc2cccc(I)c2)cc1 10.1016/j.bmcl.2007.09.074
10076580 82064 0 None -158 3 Mouse 7.6 pKi = 7.6 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 563 10 2 8 5.5 Cc1cc(C)c2oc(-c3cccc(C[C@H](O)/C=C/[C@H]4CCC(=O)N4CCSc4nc(C(=O)O)cs4)c3)nc2c1 10.1016/j.bmc.2012.04.008
CHEMBL2037291 82064 0 None -158 3 Mouse 7.6 pKi = 7.6 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 563 10 2 8 5.5 Cc1cc(C)c2oc(-c3cccc(C[C@H](O)/C=C/[C@H]4CCC(=O)N4CCSc4nc(C(=O)O)cs4)c3)nc2c1 10.1016/j.bmc.2012.04.008
132836 66469 23 None 1 3 Human 6.6 pKi = 6.6 Binding
Binding affinity to EP2 receptor (unknown origin) by competitive binding assayBinding affinity to EP2 receptor (unknown origin) by competitive binding assay
ChEMBL 388 13 2 3 5.8 CCCCCC(O)c1ccc([C@H]2CCC(=O)[C@@H]2CCCCCCC(=O)O)cc1 10.1021/jm401431x
CHEMBL1722929 66469 23 None 1 3 Human 6.6 pKi = 6.6 Binding
Binding affinity to EP2 receptor (unknown origin) by competitive binding assayBinding affinity to EP2 receptor (unknown origin) by competitive binding assay
ChEMBL 388 13 2 3 5.8 CCCCCC(O)c1ccc([C@H]2CCC(=O)[C@@H]2CCCCCCC(=O)O)cc1 10.1021/jm401431x
57403799 76244 0 None -6 2 Mouse 6.6 pKi = 6.6 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 398 9 2 5 2.8 Cc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=O)N2CCCc2nc(C(=O)O)co2)c1 10.1016/j.bmcl.2011.10.109
CHEMBL1933720 76244 0 None -6 2 Mouse 6.6 pKi = 6.6 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 398 9 2 5 2.8 Cc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=O)N2CCCc2nc(C(=O)O)co2)c1 10.1016/j.bmcl.2011.10.109
57403799 76244 0 None -6 2 Mouse 6.6 pKi = 6.6 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 398 9 2 5 2.8 Cc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=O)N2CCCc2nc(C(=O)O)co2)c1 10.1016/j.bmc.2012.02.018
CHEMBL1933720 76244 0 None -6 2 Mouse 6.6 pKi = 6.6 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 398 9 2 5 2.8 Cc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=O)N2CCCc2nc(C(=O)O)co2)c1 10.1016/j.bmc.2012.02.018
5311035 104579 29 None -4 9 Human 5.6 pKi = 5.6 Binding
Binding affinity to EP2 receptor (unknown origin) by competitive binding assayBinding affinity to EP2 receptor (unknown origin) by competitive binding assay
ChEMBL 408 13 2 5 4.3 CCCC1([C@H](O)C/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2CCCCCCC(=O)OC)CCC1 10.1021/jm401431x
CHEMBL271896 104579 29 None -4 9 Human 5.6 pKi = 5.6 Binding
Binding affinity to EP2 receptor (unknown origin) by competitive binding assayBinding affinity to EP2 receptor (unknown origin) by competitive binding assay
ChEMBL 408 13 2 5 4.3 CCCC1([C@H](O)C/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2CCCCCCC(=O)OC)CCC1 10.1021/jm401431x
44303980 174853 0 None - 1 Mouse 5.6 pKi = 5.6 Binding
Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.
ChEMBL 408 13 2 5 4.3 CCCC1([C@@H](O)C/C=C/C2[C@H](O)CC(=O)[C@@H]2CCCCCCC(=O)OC)CCC1 10.1016/s0960-894x(01)00359-6
CHEMBL432522 174853 0 None - 1 Mouse 5.6 pKi = 5.6 Binding
Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.
ChEMBL 408 13 2 5 4.3 CCCC1([C@@H](O)C/C=C/C2[C@H](O)CC(=O)[C@@H]2CCCCCCC(=O)OC)CCC1 10.1016/s0960-894x(01)00359-6
22009004 148529 0 None -2884 4 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]PGE2 from human EP2R expressed in chem1 cells after 2hrs by beta countingDisplacement of [3H]PGE2 from human EP2R expressed in chem1 cells after 2hrs by beta counting
ChEMBL 545 11 1 6 6.1 COc1cc(C/C=C/c2ccccc2/C=C/C(=O)NS(=O)(=O)c2cccs2)ccc1OCc1ccccc1 10.1021/ml300191g
CHEMBL385955 148529 0 None -2884 4 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]PGE2 from human EP2R expressed in chem1 cells after 2hrs by beta countingDisplacement of [3H]PGE2 from human EP2R expressed in chem1 cells after 2hrs by beta counting
ChEMBL 545 11 1 6 6.1 COc1cc(C/C=C/c2ccccc2/C=C/C(=O)NS(=O)(=O)c2cccs2)ccc1OCc1ccccc1 10.1021/ml300191g
10270893 101003 0 None -1 2 Human 5.6 pKi = 5.6 Binding
Binding affinity at human prostaglandin EP2 receptorBinding affinity at human prostaglandin EP2 receptor
ChEMBL 376 12 2 4 3.1 CCCCCC(O)CCCN1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.09.074
CHEMBL249954 101003 0 None -1 2 Human 5.6 pKi = 5.6 Binding
Binding affinity at human prostaglandin EP2 receptorBinding affinity at human prostaglandin EP2 receptor
ChEMBL 376 12 2 4 3.1 CCCCCC(O)CCCN1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.09.074
44303889 209996 0 None - 1 Mouse 7.6 pKi = 7.6 Binding
Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.
ChEMBL 414 10 3 4 4.2 CCCC1([C@@H](O)C/C=C/C2[C@H](O)CC(=O)[C@@H]2CCc2ccc(C(=O)O)cc2)CCC1 10.1016/s0960-894x(01)00359-6
CHEMBL64423 209996 0 None - 1 Mouse 7.6 pKi = 7.6 Binding
Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.
ChEMBL 414 10 3 4 4.2 CCCC1([C@@H](O)C/C=C/C2[C@H](O)CC(=O)[C@@H]2CCc2ccc(C(=O)O)cc2)CCC1 10.1016/s0960-894x(01)00359-6
17751059 155047 0 None 56 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 440 12 2 2 6.8 CCCCCC(O)c1ccc([C@H]2[C@H](Cl)C[C@@H](Cl)[C@@H]2C/C=C\CCCC(=O)O)cc1 nan
CHEMBL3936540 155047 0 None 56 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 440 12 2 2 6.8 CCCCCC(O)c1ccc([C@H]2[C@H](Cl)C[C@@H](Cl)[C@@H]2C/C=C\CCCC(=O)O)cc1 nan
21974328 73044 0 None -26 5 Mouse 6.6 pKi = 6.6 Binding
Ability to inhibit the binding of [3H]-PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP2Ability to inhibit the binding of [3H]-PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP2
ChEMBL 443 6 1 6 4.4 Cc1cc2c(CC(=O)O)cccc2n1C(=O)c1ccc(OCC2Oc3ccccc3O2)cc1 10.1016/j.bmcl.2004.07.039
CHEMBL184684 73044 0 None -26 5 Mouse 6.6 pKi = 6.6 Binding
Ability to inhibit the binding of [3H]-PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP2Ability to inhibit the binding of [3H]-PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP2
ChEMBL 443 6 1 6 4.4 Cc1cc2c(CC(=O)O)cccc2n1C(=O)c1ccc(OCC2Oc3ccccc3O2)cc1 10.1016/j.bmcl.2004.07.039
10228100 71188 0 None -43 5 Mouse 6.6 pKi = 6.6 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 488 6 1 6 4.7 Cc1c(CC(=O)O)c2cc(F)ccc2n1C(=O)c1ccc(OC[C@@H]2CN(C)c3ccccc3O2)cc1 10.1016/j.bmc.2011.06.014
CHEMBL1813118 71188 0 None -43 5 Mouse 6.6 pKi = 6.6 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 488 6 1 6 4.7 Cc1c(CC(=O)O)c2cc(F)ccc2n1C(=O)c1ccc(OC[C@@H]2CN(C)c3ccccc3O2)cc1 10.1016/j.bmc.2011.06.014
44349551 23586 0 None -47 4 Human 5.6 pKi = 5.6 Binding
Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 415 8 2 4 6.2 O=C(O)CNc1ccccc1-c1csc(-c2ccccc2OCc2ccccc2)c1 10.1016/s0960-894x(03)00794-7
CHEMBL124675 23586 0 None -47 4 Human 5.6 pKi = 5.6 Binding
Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 415 8 2 4 6.2 O=C(O)CNc1ccccc1-c1csc(-c2ccccc2OCc2ccccc2)c1 10.1016/s0960-894x(03)00794-7
10158725 23600 0 None -109 4 Human 5.6 pKi = 5.6 Binding
Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 414 8 1 3 6.7 O=C(O)CCc1ccccc1-c1csc(-c2ccccc2OCc2ccccc2)c1 10.1016/s0960-894x(03)00794-7
CHEMBL124738 23600 0 None -109 4 Human 5.6 pKi = 5.6 Binding
Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 414 8 1 3 6.7 O=C(O)CCc1ccccc1-c1csc(-c2ccccc2OCc2ccccc2)c1 10.1016/s0960-894x(03)00794-7
44320405 112942 0 None -5 4 Human 5.6 pKi = 5.6 Binding
Binding affinity at human Prostanoid EP2 receptor.Binding affinity at human Prostanoid EP2 receptor.
ChEMBL 521 11 1 5 6.2 O=C(NS(=O)(=O)CCc1ccccc1-c1ccc(CSCCc2ccccc2)cc1)c1cccs1 10.1016/s0960-894x(02)00518-8
CHEMBL313700 112942 0 None -5 4 Human 5.6 pKi = 5.6 Binding
Binding affinity at human Prostanoid EP2 receptor.Binding affinity at human Prostanoid EP2 receptor.
ChEMBL 521 11 1 5 6.2 O=C(NS(=O)(=O)CCc1ccccc1-c1ccc(CSCCc2ccccc2)cc1)c1cccs1 10.1016/s0960-894x(02)00518-8
52944194 23315 0 None -194 4 Human 5.6 pKi = 5.6 Binding
Binding affinity for human prostanoid EP2 receptorBinding affinity for human prostanoid EP2 receptor
ChEMBL 936 18 4 6 12.8 O=C(O)/C=C/c1ccccc1/C=C/Cc1cccc(CO)c1OCc1c(Cl)cccc1Cl.O=C(O)/C=C/c1ccccc1C/C=C/c1cccc(CO)c1OCc1c(Cl)cccc1Cl 10.1016/j.bmcl.2004.11.051
CHEMBL1237305 23315 0 None -194 4 Human 5.6 pKi = 5.6 Binding
Binding affinity for human prostanoid EP2 receptorBinding affinity for human prostanoid EP2 receptor
ChEMBL 936 18 4 6 12.8 O=C(O)/C=C/c1ccccc1/C=C/Cc1cccc(CO)c1OCc1c(Cl)cccc1Cl.O=C(O)/C=C/c1ccccc1C/C=C/c1cccc(CO)c1OCc1c(Cl)cccc1Cl 10.1016/j.bmcl.2004.11.051
52947852 23318 0 None -37 3 Human 5.6 pKi = 5.6 Binding
Binding affinity for human prostanoid EP2 receptorBinding affinity for human prostanoid EP2 receptor
ChEMBL 588 12 2 4 8.1 COc1ccc(/C=C/Cc2ccccc2/C=C/C(=O)O)cc1.COc1ccc(C/C=C/c2ccccc2/C=C/C(=O)O)cc1 10.1016/j.bmcl.2004.11.051
CHEMBL1237316 23318 0 None -37 3 Human 5.6 pKi = 5.6 Binding
Binding affinity for human prostanoid EP2 receptorBinding affinity for human prostanoid EP2 receptor
ChEMBL 588 12 2 4 8.1 COc1ccc(/C=C/Cc2ccccc2/C=C/C(=O)O)cc1.COc1ccc(C/C=C/c2ccccc2/C=C/C(=O)O)cc1 10.1016/j.bmcl.2004.11.051
52947852 23318 0 None -37 3 Human 5.6 pKi = 5.6 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 588 12 2 4 8.1 COc1ccc(/C=C/Cc2ccccc2/C=C/C(=O)O)cc1.COc1ccc(C/C=C/c2ccccc2/C=C/C(=O)O)cc1 10.1016/j.bmcl.2006.08.025
CHEMBL1237316 23318 0 None -37 3 Human 5.6 pKi = 5.6 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 588 12 2 4 8.1 COc1ccc(/C=C/Cc2ccccc2/C=C/C(=O)O)cc1.COc1ccc(C/C=C/c2ccccc2/C=C/C(=O)O)cc1 10.1016/j.bmcl.2006.08.025
44419388 90190 0 None -37 3 Human 5.6 pKi = 5.6 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 294 6 1 2 4.0 COc1ccc(/C=C/Cc2ccccc2/C=C/C(=O)O)cc1 10.1016/j.bmcl.2006.08.025
CHEMBL219590 90190 0 None -37 3 Human 5.6 pKi = 5.6 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 294 6 1 2 4.0 COc1ccc(/C=C/Cc2ccccc2/C=C/C(=O)O)cc1 10.1016/j.bmcl.2006.08.025
11339240 91503 0 None -3548 2 Human 5.6 pKi = 5.6 Binding
Binding affinity to human EP2 receptorBinding affinity to human EP2 receptor
ChEMBL 423 10 2 4 3.2 COCc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=O)N2CCc2ccc(C(=O)O)cc2)c1 10.1021/jm049290a
CHEMBL222834 91503 0 None -3548 2 Human 5.6 pKi = 5.6 Binding
Binding affinity to human EP2 receptorBinding affinity to human EP2 receptor
ChEMBL 423 10 2 4 3.2 COCc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=O)N2CCc2ccc(C(=O)O)cc2)c1 10.1021/jm049290a
9885106 91548 0 None -1258 6 Mouse 5.6 pKi = 5.6 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 357 13 2 4 3.1 CCCCC[C@H](O)/C=C/[C@H]1CCC(=O)N1CCSCCCC(=O)O 10.1016/j.bmcl.2011.10.109
CHEMBL223151 91548 0 None -1258 6 Mouse 5.6 pKi = 5.6 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 357 13 2 4 3.1 CCCCC[C@H](O)/C=C/[C@H]1CCC(=O)N1CCSCCCC(=O)O 10.1016/j.bmcl.2011.10.109
9885106 91548 0 None -1258 6 Mouse 5.6 pKi = 5.6 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 357 13 2 4 3.1 CCCCC[C@H](O)/C=C/[C@H]1CCC(=O)N1CCSCCCC(=O)O 10.1016/j.bmc.2012.02.018
CHEMBL223151 91548 0 None -1258 6 Mouse 5.6 pKi = 5.6 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 357 13 2 4 3.1 CCCCC[C@H](O)/C=C/[C@H]1CCC(=O)N1CCSCCCC(=O)O 10.1016/j.bmc.2012.02.018
44304258 109133 0 None -114 3 Mouse 5.6 pKi = 5.6 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptor
ChEMBL 424 11 3 6 2.7 Cc1ccccc1C[C@H](O)/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1SCCCSCC(=O)O 10.1016/s0960-894x(01)00364-x
CHEMBL303787 109133 0 None -114 3 Mouse 5.6 pKi = 5.6 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptor
ChEMBL 424 11 3 6 2.7 Cc1ccccc1C[C@H](O)/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1SCCCSCC(=O)O 10.1016/s0960-894x(01)00364-x
44455158 104497 0 None -933 2 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]PGE2 from human EP2 receptorDisplacement of [3H]PGE2 from human EP2 receptor
ChEMBL 331 8 2 3 2.6 CCC[C@H](O)/C=C/[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.11.020
CHEMBL271488 104497 0 None -933 2 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]PGE2 from human EP2 receptorDisplacement of [3H]PGE2 from human EP2 receptor
ChEMBL 331 8 2 3 2.6 CCC[C@H](O)/C=C/[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.11.020
9821171 104642 0 None -51286 2 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]PGE2 from human EP2 receptorDisplacement of [3H]PGE2 from human EP2 receptor
ChEMBL 379 8 2 3 3.1 O=C(O)c1ccc(CCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2ccccc2)cc1 10.1016/j.bmcl.2007.11.020
CHEMBL272276 104642 0 None -51286 2 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]PGE2 from human EP2 receptorDisplacement of [3H]PGE2 from human EP2 receptor
ChEMBL 379 8 2 3 3.1 O=C(O)c1ccc(CCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2ccccc2)cc1 10.1016/j.bmcl.2007.11.020
44304011 209587 0 None -83 3 Mouse 5.6 pKi = 5.6 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptor
ChEMBL 440 12 3 7 2.4 COc1ccccc1C[C@H](O)/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1SCCCSCC(=O)O 10.1016/s0960-894x(01)00364-x
CHEMBL62305 209587 0 None -83 3 Mouse 5.6 pKi = 5.6 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptor
ChEMBL 440 12 3 7 2.4 COc1ccccc1C[C@H](O)/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1SCCCSCC(=O)O 10.1016/s0960-894x(01)00364-x
44290263 108106 0 None -3235 2 Human 4.6 pKi = 4.6 Binding
Binding affinity was determined against prostanoid EP2 receptorBinding affinity was determined against prostanoid EP2 receptor
ChEMBL 453 12 3 4 5.2 Cc1cc(O)ccc1-c1cccc([C@H](O)CC[C@H]2CCC(=O)N2CCCCCCC(=O)O)c1 10.1016/j.bmcl.2004.01.063
CHEMBL296715 108106 0 None -3235 2 Human 4.6 pKi = 4.6 Binding
Binding affinity was determined against prostanoid EP2 receptorBinding affinity was determined against prostanoid EP2 receptor
ChEMBL 453 12 3 4 5.2 Cc1cc(O)ccc1-c1cccc([C@H](O)CC[C@H]2CCC(=O)N2CCCCCCC(=O)O)c1 10.1016/j.bmcl.2004.01.063
77050677 135362 0 None -588 2 Human 6.6 pKi = 6.6 Binding
In Vitro Binding Assay: hEP1 and hEP4 membranes are prepared from recombinant HEK293 cells stably expressing the human EP1 (Genbank accession number AY275470) or EP4 (Genbank accession number AY429109) receptors. hEP2 and hEP3 membranes are prepared from HEK293 cells transiently transfected with EP2 (Genbank accession number AY275471) or EP3 (isoform VI: Genbank accession number AY429108) receptor plasmids. Frozen cell pellets are homogenized in homogenization buffer using a Teflon/glass homogenizer. Membrane protein is aliquoted and quick frozen on dry ice prior to storage at -80 C. Homogenization buffer contained 10 mM Tris-HCl, pH 7.4, 250 mM sucrose, 1 mM EDTA, 0.3 mM indomethacin and plus Complete, with EDTA, obtained from Roche Molecular Biochemicals (Catalog Number 1 697 498).Kd values for [3]H-PGE2 binding to each receptor are determined by saturation binding studies or homologous competition. Compounds are tested in a 96-well format using a three-fold dilution series.In Vitro Binding Assay: hEP1 and hEP4 membranes are prepared from recombinant HEK293 cells stably expressing the human EP1 (Genbank accession number AY275470) or EP4 (Genbank accession number AY429109) receptors. hEP2 and hEP3 membranes are prepared from HEK293 cells transiently transfected with EP2 (Genbank accession number AY275471) or EP3 (isoform VI: Genbank accession number AY429108) receptor plasmids. Frozen cell pellets are homogenized in homogenization buffer using a Teflon/glass homogenizer. Membrane protein is aliquoted and quick frozen on dry ice prior to storage at -80 C. Homogenization buffer contained 10 mM Tris-HCl, pH 7.4, 250 mM sucrose, 1 mM EDTA, 0.3 mM indomethacin and plus Complete, with EDTA, obtained from Roche Molecular Biochemicals (Catalog Number 1 697 498).Kd values for [3]H-PGE2 binding to each receptor are determined by saturation binding studies or homologous competition. Compounds are tested in a 96-well format using a three-fold dilution series.
ChEMBL 385 10 2 4 3.7 CC(C)[C@@H](OCCOc1ccccc1)C(=O)N[C@@H](C)c1ccc(C(=O)O)cc1 nan
CHEMBL3667607 135362 0 None -588 2 Human 6.6 pKi = 6.6 Binding
In Vitro Binding Assay: hEP1 and hEP4 membranes are prepared from recombinant HEK293 cells stably expressing the human EP1 (Genbank accession number AY275470) or EP4 (Genbank accession number AY429109) receptors. hEP2 and hEP3 membranes are prepared from HEK293 cells transiently transfected with EP2 (Genbank accession number AY275471) or EP3 (isoform VI: Genbank accession number AY429108) receptor plasmids. Frozen cell pellets are homogenized in homogenization buffer using a Teflon/glass homogenizer. Membrane protein is aliquoted and quick frozen on dry ice prior to storage at -80 C. Homogenization buffer contained 10 mM Tris-HCl, pH 7.4, 250 mM sucrose, 1 mM EDTA, 0.3 mM indomethacin and plus Complete, with EDTA, obtained from Roche Molecular Biochemicals (Catalog Number 1 697 498).Kd values for [3]H-PGE2 binding to each receptor are determined by saturation binding studies or homologous competition. Compounds are tested in a 96-well format using a three-fold dilution series.In Vitro Binding Assay: hEP1 and hEP4 membranes are prepared from recombinant HEK293 cells stably expressing the human EP1 (Genbank accession number AY275470) or EP4 (Genbank accession number AY429109) receptors. hEP2 and hEP3 membranes are prepared from HEK293 cells transiently transfected with EP2 (Genbank accession number AY275471) or EP3 (isoform VI: Genbank accession number AY429108) receptor plasmids. Frozen cell pellets are homogenized in homogenization buffer using a Teflon/glass homogenizer. Membrane protein is aliquoted and quick frozen on dry ice prior to storage at -80 C. Homogenization buffer contained 10 mM Tris-HCl, pH 7.4, 250 mM sucrose, 1 mM EDTA, 0.3 mM indomethacin and plus Complete, with EDTA, obtained from Roche Molecular Biochemicals (Catalog Number 1 697 498).Kd values for [3]H-PGE2 binding to each receptor are determined by saturation binding studies or homologous competition. Compounds are tested in a 96-well format using a three-fold dilution series.
ChEMBL 385 10 2 4 3.7 CC(C)[C@@H](OCCOc1ccccc1)C(=O)N[C@@H](C)c1ccc(C(=O)O)cc1 nan
11855325 151469 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells at pH 6 after 60 minsDisplacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells at pH 6 after 60 mins
ChEMBL 387 6 1 4 4.5 CC(C)(C)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3908484 151469 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells at pH 6 after 60 minsDisplacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells at pH 6 after 60 mins
ChEMBL 387 6 1 4 4.5 CC(C)(C)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
21362900 212619 0 None -58 4 Human 5.6 pKi = 5.6 Binding
Binding affinity at human Prostanoid EP2 receptor.Binding affinity at human Prostanoid EP2 receptor.
ChEMBL 521 11 1 5 6.3 O=C(CCc1ccccc1-c1ccc(CSCCc2ccccc2)cc1)NS(=O)(=O)c1cccs1 10.1016/s0960-894x(02)00518-8
CHEMBL83518 212619 0 None -58 4 Human 5.6 pKi = 5.6 Binding
Binding affinity at human Prostanoid EP2 receptor.Binding affinity at human Prostanoid EP2 receptor.
ChEMBL 521 11 1 5 6.3 O=C(CCc1ccccc1-c1ccc(CSCCc2ccccc2)cc1)NS(=O)(=O)c1cccs1 10.1016/s0960-894x(02)00518-8
11418818 73436 0 None -14 4 Mouse 5.6 pKi = 5.6 Binding
Binding affinity for mouse Prostanoid EP2 receptorBinding affinity for mouse Prostanoid EP2 receptor
ChEMBL 423 10 1 5 5.2 CCCCOc1ccc(C(=O)n2c(C)c(CCCC(=O)O)c3cc(OC)ccc32)cc1 10.1016/j.bmcl.2004.06.006
CHEMBL185369 73436 0 None -14 4 Mouse 5.6 pKi = 5.6 Binding
Binding affinity for mouse Prostanoid EP2 receptorBinding affinity for mouse Prostanoid EP2 receptor
ChEMBL 423 10 1 5 5.2 CCCCOc1ccc(C(=O)n2c(C)c(CCCC(=O)O)c3cc(OC)ccc32)cc1 10.1016/j.bmcl.2004.06.006
53358921 71215 0 None -562 6 Mouse 5.6 pKi = 5.6 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 482 7 1 5 5.4 CCN1c2ccccc2C[C@@H]1COc1ccc(C(=O)n2c(C)c(CC(=O)O)c3ccccc32)c(C)c1 10.1016/j.bmc.2011.06.014
CHEMBL1813287 71215 0 None -562 6 Mouse 5.6 pKi = 5.6 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 482 7 1 5 5.4 CCN1c2ccccc2C[C@@H]1COc1ccc(C(=O)n2c(C)c(CC(=O)O)c3ccccc32)c(C)c1 10.1016/j.bmc.2011.06.014
10181606 213130 0 None -645 7 Human 4.6 pKi = 4.6 Binding
Binding affinity at human Prostanoid EP2 receptor.Binding affinity at human Prostanoid EP2 receptor.
ChEMBL 437 5 1 4 5.2 O=C(/C=C/c1ccccc1-c1ccc(Cl)c(Cl)c1)NS(=O)(=O)c1cccs1 10.1016/s0960-894x(02)00518-8
CHEMBL87371 213130 0 None -645 7 Human 4.6 pKi = 4.6 Binding
Binding affinity at human Prostanoid EP2 receptor.Binding affinity at human Prostanoid EP2 receptor.
ChEMBL 437 5 1 4 5.2 O=C(/C=C/c1ccccc1-c1ccc(Cl)c(Cl)c1)NS(=O)(=O)c1cccs1 10.1016/s0960-894x(02)00518-8
118517360 150753 0 None -1380 2 Human 5.6 pKi = 5.6 Binding
Radioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations wRadioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations w
ChEMBL 412 8 2 3 4.7 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2cccc(Cl)c2)cc1 nan
CHEMBL3902700 150753 0 None -1380 2 Human 5.6 pKi = 5.6 Binding
Radioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations wRadioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations w
ChEMBL 412 8 2 3 4.7 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2cccc(Cl)c2)cc1 nan
44444714 100913 0 None 2 2 Human 5.6 pKi = 5.6 Binding
Binding affinity at human prostaglandin EP2 receptorBinding affinity at human prostaglandin EP2 receptor
ChEMBL 362 10 2 4 2.6 CCCC(C)C(O)CCN1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.09.074
CHEMBL249341 100913 0 None 2 2 Human 5.6 pKi = 5.6 Binding
Binding affinity at human prostaglandin EP2 receptorBinding affinity at human prostaglandin EP2 receptor
ChEMBL 362 10 2 4 2.6 CCCC(C)C(O)CCN1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.09.074
57893848 81944 0 None -234 2 Mouse 7.6 pKi = 7.6 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 535 10 2 8 4.9 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(-c3nc4ccccc4o3)c2)n1 10.1016/j.bmc.2012.04.008
CHEMBL2036323 81944 0 None -234 2 Mouse 7.6 pKi = 7.6 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 535 10 2 8 4.9 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(-c3nc4ccccc4o3)c2)n1 10.1016/j.bmc.2012.04.008
21974362 128822 0 None -1 4 Mouse 6.6 pKi = 6.6 Binding
Ability to inhibit the binding of [3H]-PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP2Ability to inhibit the binding of [3H]-PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP2
ChEMBL 455 6 1 5 4.9 Cc1cc2c(CC(=O)O)cccc2n1C(=O)c1ccc(OCC2COc3ccccc3C2)cc1 10.1016/j.bmcl.2004.07.039
CHEMBL359564 128822 0 None -1 4 Mouse 6.6 pKi = 6.6 Binding
Ability to inhibit the binding of [3H]-PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP2Ability to inhibit the binding of [3H]-PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP2
ChEMBL 455 6 1 5 4.9 Cc1cc2c(CC(=O)O)cccc2n1C(=O)c1ccc(OCC2COc3ccccc3C2)cc1 10.1016/j.bmcl.2004.07.039
9886718 209942 0 None -398 4 Mouse 6.6 pKi = 6.6 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptor
ChEMBL 390 13 3 6 2.7 CCCCC[C@H](O)/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1SCCCSCC(=O)O 10.1016/s0960-894x(01)00364-x
CHEMBL64217 209942 0 None -398 4 Mouse 6.6 pKi = 6.6 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptor
ChEMBL 390 13 3 6 2.7 CCCCC[C@H](O)/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1SCCCSCC(=O)O 10.1016/s0960-894x(01)00364-x
118175009 143463 0 None -812 2 Human 5.6 pKi = 5.6 Binding
Antagonist activity at human EP2 receptorAntagonist activity at human EP2 receptor
ChEMBL 429 4 2 2 6.7 Cc1ccc(C(=O)O)c(C)c1NC(=O)c1cc(-c2cccc(Cl)c2)cc2ccccc12 10.1016/j.bmcl.2015.11.023
CHEMBL3740325 143463 0 None -812 2 Human 5.6 pKi = 5.6 Binding
Antagonist activity at human EP2 receptorAntagonist activity at human EP2 receptor
ChEMBL 429 4 2 2 6.7 Cc1ccc(C(=O)O)c(C)c1NC(=O)c1cc(-c2cccc(Cl)c2)cc2ccccc12 10.1016/j.bmcl.2015.11.023
10157813 208395 0 None -177 4 Mouse 5.6 pKi = 5.6 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 400 9 1 4 4.7 O=C(O)CCc1ccc(Cn2cccn2)cc1OCCc1ccc2ccccc2c1 10.1016/j.bmc.2009.08.007
CHEMBL605833 208395 0 None -177 4 Mouse 5.6 pKi = 5.6 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 400 9 1 4 4.7 O=C(O)CCc1ccc(Cn2cccn2)cc1OCCc1ccc2ccccc2c1 10.1016/j.bmc.2009.08.007
59465587 151968 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 372 13 2 2 6.5 CCCCCC(O)c1ccc([C@H]2CCC=C2CCCCCCC(=O)O)cc1 nan
CHEMBL3912391 151968 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 372 13 2 2 6.5 CCCCCC(O)c1ccc([C@H]2CCC=C2CCCCCCC(=O)O)cc1 nan
10205205 100943 0 None -47 2 Human 5.6 pKi = 5.6 Binding
Binding affinity at human prostaglandin EP2 receptorBinding affinity at human prostaglandin EP2 receptor
ChEMBL 466 10 2 5 3.3 O=C(O)c1ccc(CCN2C(=O)CCN2CCC(O)Cc2cccc(OC(F)(F)F)c2)cc1 10.1016/j.bmcl.2007.09.074
CHEMBL249539 100943 0 None -47 2 Human 5.6 pKi = 5.6 Binding
Binding affinity at human prostaglandin EP2 receptorBinding affinity at human prostaglandin EP2 receptor
ChEMBL 466 10 2 5 3.3 O=C(O)c1ccc(CCN2C(=O)CCN2CCC(O)Cc2cccc(OC(F)(F)F)c2)cc1 10.1016/j.bmcl.2007.09.074
10089562 161201 0 None 5 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]PGE2 from human EP2 receptor expressed in HEK293 cellsDisplacement of [3H]PGE2 from human EP2 receptor expressed in HEK293 cells
ChEMBL 355 9 1 2 4.6 CCCC/C=C(C)/C=C/[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.05.025
CHEMBL398948 161201 0 None 5 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]PGE2 from human EP2 receptor expressed in HEK293 cellsDisplacement of [3H]PGE2 from human EP2 receptor expressed in HEK293 cells
ChEMBL 355 9 1 2 4.6 CCCC/C=C(C)/C=C/[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.05.025
44304335 209757 0 None -37 4 Mouse 6.5 pKi = 6.5 Binding
Affinity for mouse Prostanoid EP2 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP2 receptor expressed in CHO cells
ChEMBL 422 10 4 4 4.0 Cc1cc(C[C@H](O)/C=C/[C@H]2[C@H](O)C[C@@H](Cl)[C@@H]2C/C=C/CCCC(=O)O)ccc1O 10.1016/s0960-894x(01)00365-1
CHEMBL63061 209757 0 None -37 4 Mouse 6.5 pKi = 6.5 Binding
Affinity for mouse Prostanoid EP2 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP2 receptor expressed in CHO cells
ChEMBL 422 10 4 4 4.0 Cc1cc(C[C@H](O)/C=C/[C@H]2[C@H](O)C[C@@H](Cl)[C@@H]2C/C=C/CCCC(=O)O)ccc1O 10.1016/s0960-894x(01)00365-1
21362879 23340 0 None -107 4 Human 5.5 pKi = 5.5 Binding
Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 414 8 1 3 6.7 O=C(O)CCc1ccccc1-c1cc(-c2ccccc2OCc2ccccc2)cs1 10.1016/s0960-894x(03)00794-7
CHEMBL123855 23340 0 None -107 4 Human 5.5 pKi = 5.5 Binding
Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 414 8 1 3 6.7 O=C(O)CCc1ccccc1-c1cc(-c2ccccc2OCc2ccccc2)cs1 10.1016/s0960-894x(03)00794-7
21362853 25304 0 None -32 4 Human 5.5 pKi = 5.5 Binding
Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 408 8 1 2 6.6 O=C(O)CCc1ccccc1-c1cccc(-c2ccccc2COc2ccccc2)c1 10.1016/s0960-894x(03)00794-7
CHEMBL127482 25304 0 None -32 4 Human 5.5 pKi = 5.5 Binding
Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 408 8 1 2 6.6 O=C(O)CCc1ccccc1-c1cccc(-c2ccccc2COc2ccccc2)c1 10.1016/s0960-894x(03)00794-7
12112239 113337 0 None -8 4 Human 5.5 pKi = 5.5 Binding
Binding affinity at human Prostanoid EP2 receptor.Binding affinity at human Prostanoid EP2 receptor.
ChEMBL 549 12 1 6 6.3 Cc1cccc(OCCCOc2ccc(-c3ccccc3CC(C)C(=O)NS(=O)(=O)c3cccs3)cc2)c1 10.1016/s0960-894x(02)00518-8
CHEMBL314200 113337 0 None -8 4 Human 5.5 pKi = 5.5 Binding
Binding affinity at human Prostanoid EP2 receptor.Binding affinity at human Prostanoid EP2 receptor.
ChEMBL 549 12 1 6 6.3 Cc1cccc(OCCCOc2ccc(-c3ccccc3CC(C)C(=O)NS(=O)(=O)c3cccs3)cc2)c1 10.1016/s0960-894x(02)00518-8
21362893 213106 0 None -54 4 Human 5.5 pKi = 5.5 Binding
Binding affinity at human Prostanoid EP2 receptor.Binding affinity at human Prostanoid EP2 receptor.
ChEMBL 535 12 1 6 6.0 Cc1cccc(OCCCOc2ccc(-c3ccccc3CCC(=O)NS(=O)(=O)c3cccs3)cc2)c1 10.1016/s0960-894x(02)00518-8
CHEMBL87263 213106 0 None -54 4 Human 5.5 pKi = 5.5 Binding
Binding affinity at human Prostanoid EP2 receptor.Binding affinity at human Prostanoid EP2 receptor.
ChEMBL 535 12 1 6 6.0 Cc1cccc(OCCCOc2ccc(-c3ccccc3CCC(=O)NS(=O)(=O)c3cccs3)cc2)c1 10.1016/s0960-894x(02)00518-8
44320321 213213 0 None -6 4 Human 5.5 pKi = 5.5 Binding
Binding affinity at human Prostanoid EP2 receptor.Binding affinity at human Prostanoid EP2 receptor.
ChEMBL 563 12 1 6 6.6 Cc1cccc(OCCCOc2ccc(-c3ccccc3CC(C)(C)C(=O)NS(=O)(=O)c3cccs3)cc2)c1 10.1016/s0960-894x(02)00518-8
CHEMBL87975 213213 0 None -6 4 Human 5.5 pKi = 5.5 Binding
Binding affinity at human Prostanoid EP2 receptor.Binding affinity at human Prostanoid EP2 receptor.
ChEMBL 563 12 1 6 6.6 Cc1cccc(OCCCOc2ccc(-c3ccccc3CC(C)(C)C(=O)NS(=O)(=O)c3cccs3)cc2)c1 10.1016/s0960-894x(02)00518-8
52941777 23312 0 None 1 4 Human 5.5 pKi = 5.5 Binding
Binding affinity for human prostanoid EP2 receptorBinding affinity for human prostanoid EP2 receptor
ChEMBL 744 16 2 4 10.9 Cc1cccc(/C=C/Cc2ccccc2CC(=O)O)c1OCc1ccccc1.Cc1cccc(C/C=C/c2ccccc2CC(=O)O)c1OCc1ccccc1 10.1016/j.bmcl.2004.11.051
CHEMBL1237302 23312 0 None 1 4 Human 5.5 pKi = 5.5 Binding
Binding affinity for human prostanoid EP2 receptorBinding affinity for human prostanoid EP2 receptor
ChEMBL 744 16 2 4 10.9 Cc1cccc(/C=C/Cc2ccccc2CC(=O)O)c1OCc1ccccc1.Cc1cccc(C/C=C/c2ccccc2CC(=O)O)c1OCc1ccccc1 10.1016/j.bmcl.2004.11.051
44393681 73635 0 None -1 3 Mouse 5.5 pKi = 5.5 Binding
Binding affinity for mouse Prostanoid EP2 receptorBinding affinity for mouse Prostanoid EP2 receptor
ChEMBL 409 9 1 5 5.2 CCCCOc1ccc(C(=O)n2c(CCC)c(C(=O)O)c3cc(OC)ccc32)cc1 10.1016/j.bmcl.2004.06.006
CHEMBL186244 73635 0 None -1 3 Mouse 5.5 pKi = 5.5 Binding
Binding affinity for mouse Prostanoid EP2 receptorBinding affinity for mouse Prostanoid EP2 receptor
ChEMBL 409 9 1 5 5.2 CCCCOc1ccc(C(=O)n2c(CCC)c(C(=O)O)c3cc(OC)ccc32)cc1 10.1016/j.bmcl.2004.06.006
10202765 179466 0 None -18197 3 Human 4.5 pKi = 4.5 Binding
Binding affinity was determined against prostanoid EP2 receptorBinding affinity was determined against prostanoid EP2 receptor
ChEMBL 427 11 2 3 4.2 O=C(O)CCCCCCN1C(=O)CC[C@@H]1/C=C/[C@@H](O)Cc1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2004.01.063
CHEMBL45008 179466 0 None -18197 3 Human 4.5 pKi = 4.5 Binding
Binding affinity was determined against prostanoid EP2 receptorBinding affinity was determined against prostanoid EP2 receptor
ChEMBL 427 11 2 3 4.2 O=C(O)CCCCCCN1C(=O)CC[C@@H]1/C=C/[C@@H](O)Cc1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2004.01.063
71458758 127640 0 None -21 4 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]PGE2 from human EP2R expressed in chem1 cells after 2hrs by beta countingDisplacement of [3H]PGE2 from human EP2R expressed in chem1 cells after 2hrs by beta counting
ChEMBL 615 14 1 4 7.8 COc1cc(C/C=C/c2ccccc2/C=C/C(=O)O)ccc1OCC[n+]1c(C)cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc1C 10.1021/ml300191g
CHEMBL2164612 127640 0 None -21 4 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]PGE2 from human EP2R expressed in chem1 cells after 2hrs by beta countingDisplacement of [3H]PGE2 from human EP2R expressed in chem1 cells after 2hrs by beta counting
ChEMBL 615 14 1 4 7.8 COc1cc(C/C=C/c2ccccc2/C=C/C(=O)O)ccc1OCC[n+]1c(C)cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc1C 10.1021/ml300191g
CHEMBL3558858 127640 0 None -21 4 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]PGE2 from human EP2R expressed in chem1 cells after 2hrs by beta countingDisplacement of [3H]PGE2 from human EP2R expressed in chem1 cells after 2hrs by beta counting
ChEMBL 615 14 1 4 7.8 COc1cc(C/C=C/c2ccccc2/C=C/C(=O)O)ccc1OCC[n+]1c(C)cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc1C 10.1021/ml300191g
57396825 76248 0 None -6 4 Mouse 8.5 pKi = 8.5 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 398 11 2 6 3.4 CCCCC[C@H](O)/C=C/[C@H]1CCC(=O)N1CCSc1nc(C(=O)O)cs1 10.1016/j.bmcl.2011.10.109
CHEMBL1933724 76248 0 None -6 4 Mouse 8.5 pKi = 8.5 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 398 11 2 6 3.4 CCCCC[C@H](O)/C=C/[C@H]1CCC(=O)N1CCSc1nc(C(=O)O)cs1 10.1016/j.bmcl.2011.10.109
57396825 76248 0 None -6 4 Mouse 8.5 pKi = 8.5 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 398 11 2 6 3.4 CCCCC[C@H](O)/C=C/[C@H]1CCC(=O)N1CCSc1nc(C(=O)O)cs1 10.1016/j.bmc.2012.02.018
CHEMBL1933724 76248 0 None -6 4 Mouse 8.5 pKi = 8.5 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 398 11 2 6 3.4 CCCCC[C@H](O)/C=C/[C@H]1CCC(=O)N1CCSc1nc(C(=O)O)cs1 10.1016/j.bmc.2012.02.018
57394893 78081 0 None -3 4 Mouse 8.5 pKi = 8.5 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 494 10 2 6 4.8 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(-c3ccccc3)c2)n1 10.1016/j.bmc.2012.02.018
CHEMBL1957435 78081 0 None -3 4 Mouse 8.5 pKi = 8.5 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 494 10 2 6 4.8 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(-c3ccccc3)c2)n1 10.1016/j.bmc.2012.02.018
57394893 78081 0 None -3 4 Mouse 8.5 pKi = 8.5 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 494 10 2 6 4.8 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(-c3ccccc3)c2)n1 10.1016/j.bmc.2012.04.008
CHEMBL1957435 78081 0 None -3 4 Mouse 8.5 pKi = 8.5 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 494 10 2 6 4.8 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(-c3ccccc3)c2)n1 10.1016/j.bmc.2012.04.008
51039072 135984 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding Assay: Measurement of EP2 receptor binding affinity was carried out according to the method of Abramovitz et al. (Biochimica et Biophysica Acta, 1483, 285 (2000)). A test compound dissolved in dimethylsulfoxide and [3H]PGE2 (NET-428, available from PerkinElmer Inc.) (final concentration: 10 nM) were added to a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2, 1 mM EDTA) in which 10 μg of a membrane fraction (ES-562-M, available from Euroscreen S.A.) of HEK293 cells expressing human EP2 receptor had been suspended, followed by incubation at 30° C. for 60 minutes. The membrane fraction was recovered on glass fiber filter paper (GF/B, available from Whatman PLC) using a cell harvester (M30R, available from Brandel Inc.), and after washing with a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2), radioactivity was measured with a liquid scintillation analyzer (2000CA, available from Packard).Binding Assay: Measurement of EP2 receptor binding affinity was carried out according to the method of Abramovitz et al. (Biochimica et Biophysica Acta, 1483, 285 (2000)). A test compound dissolved in dimethylsulfoxide and [3H]PGE2 (NET-428, available from PerkinElmer Inc.) (final concentration: 10 nM) were added to a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2, 1 mM EDTA) in which 10 μg of a membrane fraction (ES-562-M, available from Euroscreen S.A.) of HEK293 cells expressing human EP2 receptor had been suspended, followed by incubation at 30° C. for 60 minutes. The membrane fraction was recovered on glass fiber filter paper (GF/B, available from Whatman PLC) using a cell harvester (M30R, available from Brandel Inc.), and after washing with a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2), radioactivity was measured with a liquid scintillation analyzer (2000CA, available from Packard).
ChEMBL 417 6 4 5 4.3 COc1ccc(-c2cc(-c3ccccc3)[nH]c2C(=O)Nc2ccc(C(=O)NO)o2)cc1 nan
CHEMBL3670662 135984 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding Assay: Measurement of EP2 receptor binding affinity was carried out according to the method of Abramovitz et al. (Biochimica et Biophysica Acta, 1483, 285 (2000)). A test compound dissolved in dimethylsulfoxide and [3H]PGE2 (NET-428, available from PerkinElmer Inc.) (final concentration: 10 nM) were added to a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2, 1 mM EDTA) in which 10 μg of a membrane fraction (ES-562-M, available from Euroscreen S.A.) of HEK293 cells expressing human EP2 receptor had been suspended, followed by incubation at 30° C. for 60 minutes. The membrane fraction was recovered on glass fiber filter paper (GF/B, available from Whatman PLC) using a cell harvester (M30R, available from Brandel Inc.), and after washing with a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2), radioactivity was measured with a liquid scintillation analyzer (2000CA, available from Packard).Binding Assay: Measurement of EP2 receptor binding affinity was carried out according to the method of Abramovitz et al. (Biochimica et Biophysica Acta, 1483, 285 (2000)). A test compound dissolved in dimethylsulfoxide and [3H]PGE2 (NET-428, available from PerkinElmer Inc.) (final concentration: 10 nM) were added to a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2, 1 mM EDTA) in which 10 μg of a membrane fraction (ES-562-M, available from Euroscreen S.A.) of HEK293 cells expressing human EP2 receptor had been suspended, followed by incubation at 30° C. for 60 minutes. The membrane fraction was recovered on glass fiber filter paper (GF/B, available from Whatman PLC) using a cell harvester (M30R, available from Brandel Inc.), and after washing with a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2), radioactivity was measured with a liquid scintillation analyzer (2000CA, available from Packard).
ChEMBL 417 6 4 5 4.3 COc1ccc(-c2cc(-c3ccccc3)[nH]c2C(=O)Nc2ccc(C(=O)NO)o2)cc1 nan
9807448 209951 0 None 1 4 Human 8.5 pKi = 8.5 Binding
Binding affinity to EP2 receptor (unknown origin) by competitive binding assayBinding affinity to EP2 receptor (unknown origin) by competitive binding assay
ChEMBL 398 11 3 3 4.7 CCC1([C@@H](O)C/C=C/[C@H]2[C@H](O)C[C@@H](Cl)[C@@H]2C/C=C\CCCC(=O)O)CCC1 10.1021/jm401431x
CHEMBL64246 209951 0 None 1 4 Human 8.5 pKi = 8.5 Binding
Binding affinity to EP2 receptor (unknown origin) by competitive binding assayBinding affinity to EP2 receptor (unknown origin) by competitive binding assay
ChEMBL 398 11 3 3 4.7 CCC1([C@@H](O)C/C=C/[C@H]2[C@H](O)C[C@@H](Cl)[C@@H]2C/C=C\CCCC(=O)O)CCC1 10.1021/jm401431x
10315 9700 28 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to EP2 (unknown origin) assessed as inhibition constantBinding affinity to EP2 (unknown origin) assessed as inhibition constant
ChEMBL 478 10 2 8 2.6 OC(=O)CNc1cccc(n1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)n1cccn1 10.1016/j.ejmech.2021.113842
44230575 9700 28 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to EP2 (unknown origin) assessed as inhibition constantBinding affinity to EP2 (unknown origin) assessed as inhibition constant
ChEMBL 478 10 2 8 2.6 OC(=O)CNc1cccc(n1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)n1cccn1 10.1016/j.ejmech.2021.113842
CHEMBL3707245 9700 28 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to EP2 (unknown origin) assessed as inhibition constantBinding affinity to EP2 (unknown origin) assessed as inhibition constant
ChEMBL 478 10 2 8 2.6 OC(=O)CNc1cccc(n1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)n1cccn1 10.1016/j.ejmech.2021.113842
67078580 135978 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding Assay: Measurement of EP2 receptor binding affinity was carried out according to the method of Abramovitz et al. (Biochimica et Biophysica Acta, 1483, 285 (2000)). A test compound dissolved in dimethylsulfoxide and [3H]PGE2 (NET-428, available from PerkinElmer Inc.) (final concentration: 10 nM) were added to a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2, 1 mM EDTA) in which 10 μg of a membrane fraction (ES-562-M, available from Euroscreen S.A.) of HEK293 cells expressing human EP2 receptor had been suspended, followed by incubation at 30° C. for 60 minutes. The membrane fraction was recovered on glass fiber filter paper (GF/B, available from Whatman PLC) using a cell harvester (M30R, available from Brandel Inc.), and after washing with a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2), radioactivity was measured with a liquid scintillation analyzer (2000CA, available from Packard).Binding Assay: Measurement of EP2 receptor binding affinity was carried out according to the method of Abramovitz et al. (Biochimica et Biophysica Acta, 1483, 285 (2000)). A test compound dissolved in dimethylsulfoxide and [3H]PGE2 (NET-428, available from PerkinElmer Inc.) (final concentration: 10 nM) were added to a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2, 1 mM EDTA) in which 10 μg of a membrane fraction (ES-562-M, available from Euroscreen S.A.) of HEK293 cells expressing human EP2 receptor had been suspended, followed by incubation at 30° C. for 60 minutes. The membrane fraction was recovered on glass fiber filter paper (GF/B, available from Whatman PLC) using a cell harvester (M30R, available from Brandel Inc.), and after washing with a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2), radioactivity was measured with a liquid scintillation analyzer (2000CA, available from Packard).
ChEMBL 435 6 2 5 4.7 COC(=O)c1ccc(CNC(=O)c2[nH]c(-c3cccs3)cc2-c2ccc(F)cc2)nc1 nan
CHEMBL3670656 135978 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding Assay: Measurement of EP2 receptor binding affinity was carried out according to the method of Abramovitz et al. (Biochimica et Biophysica Acta, 1483, 285 (2000)). A test compound dissolved in dimethylsulfoxide and [3H]PGE2 (NET-428, available from PerkinElmer Inc.) (final concentration: 10 nM) were added to a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2, 1 mM EDTA) in which 10 μg of a membrane fraction (ES-562-M, available from Euroscreen S.A.) of HEK293 cells expressing human EP2 receptor had been suspended, followed by incubation at 30° C. for 60 minutes. The membrane fraction was recovered on glass fiber filter paper (GF/B, available from Whatman PLC) using a cell harvester (M30R, available from Brandel Inc.), and after washing with a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2), radioactivity was measured with a liquid scintillation analyzer (2000CA, available from Packard).Binding Assay: Measurement of EP2 receptor binding affinity was carried out according to the method of Abramovitz et al. (Biochimica et Biophysica Acta, 1483, 285 (2000)). A test compound dissolved in dimethylsulfoxide and [3H]PGE2 (NET-428, available from PerkinElmer Inc.) (final concentration: 10 nM) were added to a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2, 1 mM EDTA) in which 10 μg of a membrane fraction (ES-562-M, available from Euroscreen S.A.) of HEK293 cells expressing human EP2 receptor had been suspended, followed by incubation at 30° C. for 60 minutes. The membrane fraction was recovered on glass fiber filter paper (GF/B, available from Whatman PLC) using a cell harvester (M30R, available from Brandel Inc.), and after washing with a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2), radioactivity was measured with a liquid scintillation analyzer (2000CA, available from Packard).
ChEMBL 435 6 2 5 4.7 COC(=O)c1ccc(CNC(=O)c2[nH]c(-c3cccs3)cc2-c2ccc(F)cc2)nc1 nan
51039068 135980 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding Assay: Measurement of EP2 receptor binding affinity was carried out according to the method of Abramovitz et al. (Biochimica et Biophysica Acta, 1483, 285 (2000)). A test compound dissolved in dimethylsulfoxide and [3H]PGE2 (NET-428, available from PerkinElmer Inc.) (final concentration: 10 nM) were added to a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2, 1 mM EDTA) in which 10 μg of a membrane fraction (ES-562-M, available from Euroscreen S.A.) of HEK293 cells expressing human EP2 receptor had been suspended, followed by incubation at 30° C. for 60 minutes. The membrane fraction was recovered on glass fiber filter paper (GF/B, available from Whatman PLC) using a cell harvester (M30R, available from Brandel Inc.), and after washing with a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2), radioactivity was measured with a liquid scintillation analyzer (2000CA, available from Packard).Binding Assay: Measurement of EP2 receptor binding affinity was carried out according to the method of Abramovitz et al. (Biochimica et Biophysica Acta, 1483, 285 (2000)). A test compound dissolved in dimethylsulfoxide and [3H]PGE2 (NET-428, available from PerkinElmer Inc.) (final concentration: 10 nM) were added to a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2, 1 mM EDTA) in which 10 μg of a membrane fraction (ES-562-M, available from Euroscreen S.A.) of HEK293 cells expressing human EP2 receptor had been suspended, followed by incubation at 30° C. for 60 minutes. The membrane fraction was recovered on glass fiber filter paper (GF/B, available from Whatman PLC) using a cell harvester (M30R, available from Brandel Inc.), and after washing with a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2), radioactivity was measured with a liquid scintillation analyzer (2000CA, available from Packard).
ChEMBL 436 6 4 5 4.0 O=C(NO)c1ccc(CNC(=O)c2[nH]c(-c3cccs3)cc2-c2ccc(F)cc2)nc1 nan
CHEMBL3670658 135980 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding Assay: Measurement of EP2 receptor binding affinity was carried out according to the method of Abramovitz et al. (Biochimica et Biophysica Acta, 1483, 285 (2000)). A test compound dissolved in dimethylsulfoxide and [3H]PGE2 (NET-428, available from PerkinElmer Inc.) (final concentration: 10 nM) were added to a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2, 1 mM EDTA) in which 10 μg of a membrane fraction (ES-562-M, available from Euroscreen S.A.) of HEK293 cells expressing human EP2 receptor had been suspended, followed by incubation at 30° C. for 60 minutes. The membrane fraction was recovered on glass fiber filter paper (GF/B, available from Whatman PLC) using a cell harvester (M30R, available from Brandel Inc.), and after washing with a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2), radioactivity was measured with a liquid scintillation analyzer (2000CA, available from Packard).Binding Assay: Measurement of EP2 receptor binding affinity was carried out according to the method of Abramovitz et al. (Biochimica et Biophysica Acta, 1483, 285 (2000)). A test compound dissolved in dimethylsulfoxide and [3H]PGE2 (NET-428, available from PerkinElmer Inc.) (final concentration: 10 nM) were added to a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2, 1 mM EDTA) in which 10 μg of a membrane fraction (ES-562-M, available from Euroscreen S.A.) of HEK293 cells expressing human EP2 receptor had been suspended, followed by incubation at 30° C. for 60 minutes. The membrane fraction was recovered on glass fiber filter paper (GF/B, available from Whatman PLC) using a cell harvester (M30R, available from Brandel Inc.), and after washing with a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2), radioactivity was measured with a liquid scintillation analyzer (2000CA, available from Packard).
ChEMBL 436 6 4 5 4.0 O=C(NO)c1ccc(CNC(=O)c2[nH]c(-c3cccs3)cc2-c2ccc(F)cc2)nc1 nan
44304164 210013 0 None - 1 Mouse 7.5 pKi = 7.5 Binding
Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.
ChEMBL 378 11 3 4 3.6 CCC1([C@@H](O)C/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2C/C=C\CCCC(=O)O)CCC1 10.1016/s0960-894x(01)00359-6
CHEMBL64483 210013 0 None - 1 Mouse 7.5 pKi = 7.5 Binding
Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.
ChEMBL 378 11 3 4 3.6 CCC1([C@@H](O)C/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2C/C=C\CCCC(=O)O)CCC1 10.1016/s0960-894x(01)00359-6
15947857 162292 7 None -269 7 Human 6.5 pKi = 6.5 Binding
Binding affinity to human EP2 receptor expressed in HEK293 cellsBinding affinity to human EP2 receptor expressed in HEK293 cells
ChEMBL 767 12 1 9 6.3 COc1cccc(OC)c1C1(C(=O)NS(=O)(=O)Cc2ccc(N3Cc4c(c(OCC(F)(F)F)c5cccnc5c4OCC(F)(F)F)C3=O)c(C)c2)CC1 10.1016/j.bmcl.2008.01.103
CHEMBL404199 162292 7 None -269 7 Human 6.5 pKi = 6.5 Binding
Binding affinity to human EP2 receptor expressed in HEK293 cellsBinding affinity to human EP2 receptor expressed in HEK293 cells
ChEMBL 767 12 1 9 6.3 COc1cccc(OC)c1C1(C(=O)NS(=O)(=O)Cc2ccc(N3Cc4c(c(OCC(F)(F)F)c5cccnc5c4OCC(F)(F)F)C3=O)c(C)c2)CC1 10.1016/j.bmcl.2008.01.103
44320294 112784 0 None -4 4 Human 5.5 pKi = 5.5 Binding
Binding affinity at human Prostanoid EP2 receptor.Binding affinity at human Prostanoid EP2 receptor.
ChEMBL 557 12 1 6 5.7 O=S(=O)(CCc1ccccc1-c1ccc(CSCCc2ccccc2)cc1)NS(=O)(=O)c1cccs1 10.1016/s0960-894x(02)00518-8
CHEMBL313266 112784 0 None -4 4 Human 5.5 pKi = 5.5 Binding
Binding affinity at human Prostanoid EP2 receptor.Binding affinity at human Prostanoid EP2 receptor.
ChEMBL 557 12 1 6 5.7 O=S(=O)(CCc1ccccc1-c1ccc(CSCCc2ccccc2)cc1)NS(=O)(=O)c1cccs1 10.1016/s0960-894x(02)00518-8
230826 100206 32 None -19 3 Human 5.5 pKi = 5.5 Binding
Binding affinity at prostanoid EP2 receptorBinding affinity at prostanoid EP2 receptor
ChEMBL 268 4 1 2 3.9 O=C(O)COc1ccc(Cl)cc1C1CCCCC1 10.1016/j.bmcl.2007.05.019
CHEMBL245908 100206 32 None -19 3 Human 5.5 pKi = 5.5 Binding
Binding affinity at prostanoid EP2 receptorBinding affinity at prostanoid EP2 receptor
ChEMBL 268 4 1 2 3.9 O=C(O)COc1ccc(Cl)cc1C1CCCCC1 10.1016/j.bmcl.2007.05.019
44269516 50407 30 None -87 3 Human 5.5 pKi = 5.5 Binding
Binding affinity towards EP2 receptor expressed in HEK293 ebna cells recombinantly expressing the corresponding human prostanoid cDNAsBinding affinity towards EP2 receptor expressed in HEK293 ebna cells recombinantly expressing the corresponding human prostanoid cDNAs
ChEMBL 341 14 2 3 3.7 CCCCCC(O)CCC1CCC(=O)N1CCCCCCC(=O)O 10.1016/s0960-894x(03)00042-8
CHEMBL15096 50407 30 None -87 3 Human 5.5 pKi = 5.5 Binding
Binding affinity towards EP2 receptor expressed in HEK293 ebna cells recombinantly expressing the corresponding human prostanoid cDNAsBinding affinity towards EP2 receptor expressed in HEK293 ebna cells recombinantly expressing the corresponding human prostanoid cDNAs
ChEMBL 341 14 2 3 3.7 CCCCCC(O)CCC1CCC(=O)N1CCCCCCC(=O)O 10.1016/s0960-894x(03)00042-8
10413147 15852 0 None -13182 3 Mouse 5.5 pKi = 5.5 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 486 10 3 3 7.2 Cc1cc(C)cc(Nc2ccc(CCC(=O)O)c(C(=O)N[C@H](CC(C)C)c3cc(C)cc(C)c3)c2)c1 10.1016/j.bmc.2010.03.028
CHEMBL1099047 15852 0 None -13182 3 Mouse 5.5 pKi = 5.5 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 486 10 3 3 7.2 Cc1cc(C)cc(Nc2ccc(CCC(=O)O)c(C(=O)N[C@H](CC(C)C)c3cc(C)cc(C)c3)c2)c1 10.1016/j.bmc.2010.03.028
44444720 101002 0 None -239 2 Human 5.5 pKi = 5.5 Binding
Binding affinity at human prostaglandin EP2 receptorBinding affinity at human prostaglandin EP2 receptor
ChEMBL 460 9 2 4 3.1 O=C(O)c1ccc(CCN2C(=O)CCN2CC[C@@H](O)Cc2cccc(Br)c2)cc1 10.1016/j.bmcl.2007.09.074
CHEMBL249953 101002 0 None -239 2 Human 5.5 pKi = 5.5 Binding
Binding affinity at human prostaglandin EP2 receptorBinding affinity at human prostaglandin EP2 receptor
ChEMBL 460 9 2 4 3.1 O=C(O)c1ccc(CCN2C(=O)CCN2CC[C@@H](O)Cc2cccc(Br)c2)cc1 10.1016/j.bmcl.2007.09.074
11855870 153058 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 mins
ChEMBL 427 11 1 4 5.7 CCCCCC(=O)c1ccc(N2C(=O)CC[C@@H]2CCCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3920756 153058 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 mins
ChEMBL 427 11 1 4 5.7 CCCCCC(=O)c1ccc(N2C(=O)CC[C@@H]2CCCc2ccc(C(=O)O)s2)cc1 nan
11855870 153058 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 427 11 1 4 5.7 CCCCCC(=O)c1ccc(N2C(=O)CC[C@@H]2CCCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3920756 153058 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 427 11 1 4 5.7 CCCCCC(=O)c1ccc(N2C(=O)CC[C@@H]2CCCc2ccc(C(=O)O)s2)cc1 nan
11269563 148388 0 None -281 5 Human 6.5 pKi = 6.5 Binding
Binding affinity to human EP2 receptor expressed in HEK293 cellsBinding affinity to human EP2 receptor expressed in HEK293 cells
ChEMBL 399 5 1 3 5.2 CC(=O)c1cc(F)cc2c3c(n(Cc4ccc(Cl)cc4)c12)[C@@H](CC(=O)O)CC3 10.1021/jm0603668
CHEMBL385126 148388 0 None -281 5 Human 6.5 pKi = 6.5 Binding
Binding affinity to human EP2 receptor expressed in HEK293 cellsBinding affinity to human EP2 receptor expressed in HEK293 cells
ChEMBL 399 5 1 3 5.2 CC(=O)c1cc(F)cc2c3c(n(Cc4ccc(Cl)cc4)c12)[C@@H](CC(=O)O)CC3 10.1021/jm0603668
10185382 71189 0 None -30 5 Mouse 6.5 pKi = 6.5 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 500 7 1 7 4.6 COc1ccc2c(c1)c(CC(=O)O)c(C)n2C(=O)c1ccc(OC[C@@H]2CN(C)c3ccccc3O2)cc1 10.1016/j.bmc.2011.06.014
CHEMBL1813119 71189 0 None -30 5 Mouse 6.5 pKi = 6.5 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 500 7 1 7 4.6 COc1ccc2c(c1)c(CC(=O)O)c(C)n2C(=O)c1ccc(OC[C@@H]2CN(C)c3ccccc3O2)cc1 10.1016/j.bmc.2011.06.014
9867899 209903 0 None -97 3 Mouse 5.5 pKi = 5.5 Binding
Affinity for mouse Prostanoid EP2 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP2 receptor expressed in CHO cells
ChEMBL 440 13 3 5 3.6 COCc1cccc(C[C@H](O)/C=C/[C@H]2[C@H](O)C[C@@H](F)[C@@H]2CCSCCCC(=O)O)c1 10.1016/s0960-894x(01)00365-1
CHEMBL64072 209903 0 None -97 3 Mouse 5.5 pKi = 5.5 Binding
Affinity for mouse Prostanoid EP2 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP2 receptor expressed in CHO cells
ChEMBL 440 13 3 5 3.6 COCc1cccc(C[C@H](O)/C=C/[C@H]2[C@H](O)C[C@@H](F)[C@@H]2CCSCCCC(=O)O)c1 10.1016/s0960-894x(01)00365-1
44303590 209690 0 None -363 3 Mouse 5.5 pKi = 5.5 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptor
ChEMBL 468 14 3 7 2.6 COCCc1cccc(C[C@H](O)/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2SCCCSCC(=O)O)c1 10.1016/s0960-894x(01)00364-x
CHEMBL62779 209690 0 None -363 3 Mouse 5.5 pKi = 5.5 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptor
ChEMBL 468 14 3 7 2.6 COCCc1cccc(C[C@H](O)/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2SCCCSCC(=O)O)c1 10.1016/s0960-894x(01)00364-x
21362867 113879 0 None -128 4 Human 4.5 pKi = 4.5 Binding
Binding affinity at human Prostanoid EP2 receptor.Binding affinity at human Prostanoid EP2 receptor.
ChEMBL 417 7 1 5 4.6 CSc1cccc(-c2ccccc2CCC(=O)NS(=O)(=O)c2cccs2)c1 10.1016/s0960-894x(02)00518-8
CHEMBL315974 113879 0 None -128 4 Human 4.5 pKi = 4.5 Binding
Binding affinity at human Prostanoid EP2 receptor.Binding affinity at human Prostanoid EP2 receptor.
ChEMBL 417 7 1 5 4.6 CSc1cccc(-c2ccccc2CCC(=O)NS(=O)(=O)c2cccs2)c1 10.1016/s0960-894x(02)00518-8
44269544 42026 0 None -7762 3 Human 4.5 pKi = 4.5 Binding
Binding affinity was determined against prostanoid EP2 receptorBinding affinity was determined against prostanoid EP2 receptor
ChEMBL 359 11 2 3 3.2 O=C(O)CCCCCCN1C(=O)CC[C@@H]1/C=C/C(O)Cc1ccccc1 10.1016/j.bmcl.2004.01.063
CHEMBL14359 42026 0 None -7762 3 Human 4.5 pKi = 4.5 Binding
Binding affinity was determined against prostanoid EP2 receptorBinding affinity was determined against prostanoid EP2 receptor
ChEMBL 359 11 2 3 3.2 O=C(O)CCCCCCN1C(=O)CC[C@@H]1/C=C/C(O)Cc1ccccc1 10.1016/j.bmcl.2004.01.063
118517488 160490 0 None -56 2 Human 5.5 pKi = 5.5 Binding
Radioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations wRadioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations w
ChEMBL 414 8 2 3 4.4 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2cccc(F)c2F)cc1 nan
CHEMBL3981554 160490 0 None -56 2 Human 5.5 pKi = 5.5 Binding
Radioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations wRadioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations w
ChEMBL 414 8 2 3 4.4 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2cccc(F)c2F)cc1 nan
118517361 160149 0 None -218 2 Human 5.5 pKi = 5.5 Binding
Radioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations wRadioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations w
ChEMBL 446 8 2 3 5.1 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2cccc(C(F)(F)F)c2)cc1 nan
CHEMBL3978590 160149 0 None -218 2 Human 5.5 pKi = 5.5 Binding
Radioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations wRadioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations w
ChEMBL 446 8 2 3 5.1 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2cccc(C(F)(F)F)c2)cc1 nan
57393339 76247 0 None -57 2 Mouse 6.5 pKi = 6.5 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 432 9 2 6 3.4 Cc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=O)N2CCSc2ncc(C(=O)O)s2)c1 10.1016/j.bmcl.2011.10.109
CHEMBL1933723 76247 0 None -57 2 Mouse 6.5 pKi = 6.5 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 432 9 2 6 3.4 Cc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=O)N2CCSc2ncc(C(=O)O)s2)c1 10.1016/j.bmcl.2011.10.109
57393339 76247 0 None -57 2 Mouse 6.5 pKi = 6.5 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 432 9 2 6 3.4 Cc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=O)N2CCSc2ncc(C(=O)O)s2)c1 10.1016/j.bmc.2012.02.018
CHEMBL1933723 76247 0 None -57 2 Mouse 6.5 pKi = 6.5 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 432 9 2 6 3.4 Cc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=O)N2CCSc2ncc(C(=O)O)s2)c1 10.1016/j.bmc.2012.02.018
44290312 185699 0 None -87 2 Human 4.5 pKi = 4.5 Binding
Binding affinity was determined against prostanoid EP2 receptorBinding affinity was determined against prostanoid EP2 receptor
ChEMBL 421 11 2 3 5.0 O=C(O)CCCCCCN1C(=O)CC[C@@H]1/C=C/C(O)c1cccc(-c2ccccc2)c1 10.1016/j.bmcl.2004.01.063
CHEMBL47018 185699 0 None -87 2 Human 4.5 pKi = 4.5 Binding
Binding affinity was determined against prostanoid EP2 receptorBinding affinity was determined against prostanoid EP2 receptor
ChEMBL 421 11 2 3 5.0 O=C(O)CCCCCCN1C(=O)CC[C@@H]1/C=C/C(O)c1cccc(-c2ccccc2)c1 10.1016/j.bmcl.2004.01.063
72950089 157370 0 None -1621 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]PGE2 from human recombinant EP2 receptor expressed in HEK293 cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]PGE2 from human recombinant EP2 receptor expressed in HEK293 cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 375 13 2 3 3.8 CCCCC[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCCCCC(=O)O 10.1021/acs.jmedchem.9b00336
CHEMBL3955128 157370 0 None -1621 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]PGE2 from human recombinant EP2 receptor expressed in HEK293 cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]PGE2 from human recombinant EP2 receptor expressed in HEK293 cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 375 13 2 3 3.8 CCCCC[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCCCCC(=O)O 10.1021/acs.jmedchem.9b00336
21974331 133324 0 None -5 4 Mouse 6.5 pKi = 6.5 Binding
Ability to inhibit the binding of [3H]-PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP2Ability to inhibit the binding of [3H]-PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP2
ChEMBL 399 6 1 4 4.8 Cc1cc2c(CC(=O)O)cccc2n1C(=O)c1ccc(OCc2ccccc2)cc1 10.1016/j.bmcl.2004.07.039
CHEMBL365243 133324 0 None -5 4 Mouse 6.5 pKi = 6.5 Binding
Ability to inhibit the binding of [3H]-PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP2Ability to inhibit the binding of [3H]-PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP2
ChEMBL 399 6 1 4 4.8 Cc1cc2c(CC(=O)O)cccc2n1C(=O)c1ccc(OCc2ccccc2)cc1 10.1016/j.bmcl.2004.07.039
10363130 107812 1 None 3 2 Mouse 6.5 pKi = 6.5 Binding
Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.
ChEMBL 392 12 3 4 4.0 CCCC1([C@@H](O)C/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2C/C=C\CCCC(=O)O)CCC1 10.1016/s0960-894x(01)00359-6
CHEMBL294585 107812 1 None 3 2 Mouse 6.5 pKi = 6.5 Binding
Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.
ChEMBL 392 12 3 4 4.0 CCCC1([C@@H](O)C/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2C/C=C\CCCC(=O)O)CCC1 10.1016/s0960-894x(01)00359-6
10185612 71187 0 None -11 4 Mouse 6.5 pKi = 6.5 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 504 6 1 6 5.2 Cc1c(CC(=O)O)c2cc(Cl)ccc2n1C(=O)c1ccc(OC[C@@H]2CN(C)c3ccccc3O2)cc1 10.1016/j.bmc.2011.06.014
CHEMBL1813117 71187 0 None -11 4 Mouse 6.5 pKi = 6.5 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 504 6 1 6 5.2 Cc1c(CC(=O)O)c2cc(Cl)ccc2n1C(=O)c1ccc(OC[C@@H]2CN(C)c3ccccc3O2)cc1 10.1016/j.bmc.2011.06.014
11338015 72892 0 None -1 2 Mouse 5.5 pKi = 5.5 Binding
Binding affinity for mouse Prostanoid EP2 receptorBinding affinity for mouse Prostanoid EP2 receptor
ChEMBL 381 7 2 5 4.2 CCCCOc1ccc(C(=O)n2c(C)c(CC(=O)O)c3cc(O)ccc32)cc1 10.1016/j.bmcl.2004.06.006
CHEMBL183983 72892 0 None -1 2 Mouse 5.5 pKi = 5.5 Binding
Binding affinity for mouse Prostanoid EP2 receptorBinding affinity for mouse Prostanoid EP2 receptor
ChEMBL 381 7 2 5 4.2 CCCCOc1ccc(C(=O)n2c(C)c(CC(=O)O)c3cc(O)ccc32)cc1 10.1016/j.bmcl.2004.06.006
44303967 209737 0 None - 1 Mouse 5.5 pKi = 5.5 Binding
Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.
ChEMBL 420 12 3 4 4.8 CCCC1([C@@H](O)C/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2C/C=C\CCCC(=O)O)CCCCC1 10.1016/s0960-894x(01)00359-6
CHEMBL62987 209737 0 None - 1 Mouse 5.5 pKi = 5.5 Binding
Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.
ChEMBL 420 12 3 4 4.8 CCCC1([C@@H](O)C/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2C/C=C\CCCC(=O)O)CCCCC1 10.1016/s0960-894x(01)00359-6
10294290 206832 0 None -275 4 Mouse 5.5 pKi = 5.5 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 398 8 1 4 4.8 O=C(O)/C=C/c1ccc(Cn2cccn2)cc1OCCc1ccc2ccccc2c1 10.1016/j.bmc.2009.08.007
CHEMBL595632 206832 0 None -275 4 Mouse 5.5 pKi = 5.5 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 398 8 1 4 4.8 O=C(O)/C=C/c1ccc(Cn2cccn2)cc1OCCc1ccc2ccccc2c1 10.1016/j.bmc.2009.08.007
50898361 63647 0 None -2630 4 Human 5.5 pKi = 5.5 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 549 7 2 5 5.4 Cc1ccc(S(=O)(=O)NC(=O)NCCc2ccc(-c3c(C(=O)N(C)C)sc4c(C)cc(C)cc34)cc2)cc1 10.1016/j.bmcl.2010.11.118
CHEMBL1644003 63647 0 None -2630 4 Human 5.5 pKi = 5.5 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 549 7 2 5 5.4 Cc1ccc(S(=O)(=O)NC(=O)NCCc2ccc(-c3c(C(=O)N(C)C)sc4c(C)cc(C)cc34)cc2)cc1 10.1016/j.bmcl.2010.11.118
44304474 209710 0 None -91 5 Mouse 6.5 pKi = 6.5 Binding
Affinity for mouse Prostanoid EP2 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP2 receptor expressed in CHO cells
ChEMBL 372 13 3 5 3.0 CCCCC[C@H](O)/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCSCCC(=O)O 10.1016/s0960-894x(01)00365-1
CHEMBL62868 209710 0 None -91 5 Mouse 6.5 pKi = 6.5 Binding
Affinity for mouse Prostanoid EP2 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP2 receptor expressed in CHO cells
ChEMBL 372 13 3 5 3.0 CCCCC[C@H](O)/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCSCCC(=O)O 10.1016/s0960-894x(01)00365-1
10277744 71186 0 None -12 7 Mouse 6.5 pKi = 6.5 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 484 6 1 6 4.9 Cc1ccc2c(c1)c(CC(=O)O)c(C)n2C(=O)c1ccc(OC[C@@H]2CN(C)c3ccccc3O2)cc1 10.1016/j.bmc.2011.06.014
CHEMBL1813116 71186 0 None -12 7 Mouse 6.5 pKi = 6.5 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 484 6 1 6 4.9 Cc1ccc2c(c1)c(CC(=O)O)c(C)n2C(=O)c1ccc(OC[C@@H]2CN(C)c3ccccc3O2)cc1 10.1016/j.bmc.2011.06.014
10291963 91483 0 None -199 6 Mouse 6.5 pKi = 6.5 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 359 10 2 3 3.4 CCCCC[C@H](O)/C=C/[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2011.10.109
CHEMBL222715 91483 0 None -199 6 Mouse 6.5 pKi = 6.5 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 359 10 2 3 3.4 CCCCC[C@H](O)/C=C/[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2011.10.109
11476788 168053 0 None -23 6 Human 5.5 pKi = 5.5 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 463 5 1 5 4.4 CS(=O)(=O)c1cc(F)cc2c1c(C(=O)c1ccc(Cl)cc1)c1n2CCC[C@@H]1CC(=O)O 10.1016/j.bmcl.2008.03.015
CHEMBL412070 168053 0 None -23 6 Human 5.5 pKi = 5.5 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 463 5 1 5 4.4 CS(=O)(=O)c1cc(F)cc2c1c(C(=O)c1ccc(Cl)cc1)c1n2CCC[C@@H]1CC(=O)O 10.1016/j.bmcl.2008.03.015
92135977 159675 0 None -275 2 Human 5.5 pKi = 5.5 Binding
Radioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations wRadioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations w
ChEMBL 396 8 2 3 4.2 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2cccc(F)c2)cc1 nan
CHEMBL3974652 159675 0 None -275 2 Human 5.5 pKi = 5.5 Binding
Radioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations wRadioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations w
ChEMBL 396 8 2 3 4.2 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2cccc(F)c2)cc1 nan
11405770 144686 0 None -2 3 Human 7.5 pKi = 7.5 Binding
Binding affinity to human EP2 receptorBinding affinity to human EP2 receptor
ChEMBL 361 11 2 3 3.6 CCCCC[C@H](O)CC[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1021/jm049290a
CHEMBL376347 144686 0 None -2 3 Human 7.5 pKi = 7.5 Binding
Binding affinity to human EP2 receptorBinding affinity to human EP2 receptor
ChEMBL 361 11 2 3 3.6 CCCCC[C@H](O)CC[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1021/jm049290a
21362910 23697 0 None -5 4 Human 5.5 pKi = 5.5 Binding
Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 422 9 1 2 7.0 O=C(O)CCCc1ccccc1-c1cccc(-c2ccccc2OCc2ccccc2)c1 10.1016/s0960-894x(03)00794-7
CHEMBL125269 23697 0 None -5 4 Human 5.5 pKi = 5.5 Binding
Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 422 9 1 2 7.0 O=C(O)CCCc1ccccc1-c1cccc(-c2ccccc2OCc2ccccc2)c1 10.1016/s0960-894x(03)00794-7
57893867 81932 0 None -12302 2 Mouse 5.5 pKi = 5.5 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 492 12 3 4 4.9 O=C(O)CCCSCCN1C(=O)CC[C@@H]1/C=C/[C@@H](O)Cc1cccc(-c2ccc3[nH]ccc3c2)c1 10.1016/j.bmc.2012.04.008
CHEMBL2036311 81932 0 None -12302 2 Mouse 5.5 pKi = 5.5 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 492 12 3 4 4.9 O=C(O)CCCSCCN1C(=O)CC[C@@H]1/C=C/[C@@H](O)Cc1cccc(-c2ccc3[nH]ccc3c2)c1 10.1016/j.bmc.2012.04.008
56658144 71580 0 None 1 2 Mouse 5.5 pKi = 5.5 Binding
Displacement of [3H]PGE2 from mouse prostaglandin EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]PGE2 from mouse prostaglandin EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 432 7 2 5 3.8 CN1C[C@@H](COc2ccc(NC(=O)c3cccc(CC(=O)O)c3)cc2)Oc2ccccc21 10.1016/j.bmc.2011.08.007
CHEMBL1819605 71580 0 None 1 2 Mouse 5.5 pKi = 5.5 Binding
Displacement of [3H]PGE2 from mouse prostaglandin EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]PGE2 from mouse prostaglandin EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 432 7 2 5 3.8 CN1C[C@@H](COc2ccc(NC(=O)c3cccc(CC(=O)O)c3)cc2)Oc2ccccc21 10.1016/j.bmc.2011.08.007
44349531 23337 0 None -3 4 Human 5.4 pKi = 5.4 Binding
Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 394 7 1 2 6.2 O=C(O)Cc1ccccc1-c1cccc(-c2ccccc2OCc2ccccc2)c1 10.1016/s0960-894x(03)00794-7
CHEMBL123844 23337 0 None -3 4 Human 5.4 pKi = 5.4 Binding
Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 394 7 1 2 6.2 O=C(O)Cc1ccccc1-c1cccc(-c2ccccc2OCc2ccccc2)c1 10.1016/s0960-894x(03)00794-7
21362849 175107 0 None -4 4 Human 5.4 pKi = 5.4 Binding
Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 422 8 1 2 6.9 CC(Cc1ccccc1-c1cccc(-c2ccccc2OCc2ccccc2)c1)C(=O)O 10.1016/s0960-894x(03)00794-7
CHEMBL434247 175107 0 None -4 4 Human 5.4 pKi = 5.4 Binding
Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 422 8 1 2 6.9 CC(Cc1ccccc1-c1cccc(-c2ccccc2OCc2ccccc2)c1)C(=O)O 10.1016/s0960-894x(03)00794-7
44269464 41251 0 None -3 3 Human 5.4 pKi = 5.4 Binding
Binding affinity towards EP2 receptor expressed in HEK293 ebna cells recombinantly expressing the corresponding human prostanoid cDNAsBinding affinity towards EP2 receptor expressed in HEK293 ebna cells recombinantly expressing the corresponding human prostanoid cDNAs
ChEMBL 341 14 2 3 3.7 CCCCCC(O)CC[C@@H]1CCC(=O)N1CCCCCCC(=O)O 10.1016/s0960-894x(03)00042-8
CHEMBL14286 41251 0 None -3 3 Human 5.4 pKi = 5.4 Binding
Binding affinity towards EP2 receptor expressed in HEK293 ebna cells recombinantly expressing the corresponding human prostanoid cDNAsBinding affinity towards EP2 receptor expressed in HEK293 ebna cells recombinantly expressing the corresponding human prostanoid cDNAs
ChEMBL 341 14 2 3 3.7 CCCCCC(O)CC[C@@H]1CCC(=O)N1CCCCCCC(=O)O 10.1016/s0960-894x(03)00042-8
118517489 150469 0 None -44 2 Human 5.4 pKi = 5.4 Binding
Radioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations wRadioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations w
ChEMBL 414 8 2 3 4.4 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2cc(F)ccc2F)cc1 nan
CHEMBL3900245 150469 0 None -44 2 Human 5.4 pKi = 5.4 Binding
Radioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations wRadioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations w
ChEMBL 414 8 2 3 4.4 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2cc(F)ccc2F)cc1 nan
44304417 208889 0 None -138 4 Mouse 6.4 pKi = 6.4 Binding
Affinity for mouse Prostanoid EP2 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP2 receptor expressed in CHO cells
ChEMBL 438 13 3 4 4.3 COCc1cccc(C[C@H](O)/C=C/[C@H]2[C@H](O)C[C@@H](Cl)[C@@H]2CCCCCCC(=O)O)c1 10.1016/s0960-894x(01)00365-1
CHEMBL60894 208889 0 None -138 4 Mouse 6.4 pKi = 6.4 Binding
Affinity for mouse Prostanoid EP2 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP2 receptor expressed in CHO cells
ChEMBL 438 13 3 4 4.3 COCc1cccc(C[C@H](O)/C=C/[C@H]2[C@H](O)C[C@@H](Cl)[C@@H]2CCCCCCC(=O)O)c1 10.1016/s0960-894x(01)00365-1
44303723 209714 0 None - 1 Mouse 6.4 pKi = 6.4 Binding
Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.
ChEMBL 406 12 3 4 4.4 CCCC1([C@@H](O)C/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2C/C=C\CCCC(=O)O)CCCC1 10.1016/s0960-894x(01)00359-6
CHEMBL62885 209714 0 None - 1 Mouse 6.4 pKi = 6.4 Binding
Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.
ChEMBL 406 12 3 4 4.4 CCCC1([C@@H](O)C/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2C/C=C\CCCC(=O)O)CCCC1 10.1016/s0960-894x(01)00359-6
53358922 71204 0 None -70 6 Mouse 6.4 pKi = 6.4 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 522 6 1 6 5.3 Cc1c(CC(=O)O)c2cc(F)ccc2n1C(=O)c1ccc(OC[C@@H]2CN(C)c3ccccc3O2)cc1Cl 10.1016/j.bmc.2011.06.014
CHEMBL1813276 71204 0 None -70 6 Mouse 6.4 pKi = 6.4 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 522 6 1 6 5.3 Cc1c(CC(=O)O)c2cc(F)ccc2n1C(=O)c1ccc(OC[C@@H]2CN(C)c3ccccc3O2)cc1Cl 10.1016/j.bmc.2011.06.014
21362851 123682 0 None -67 4 Human 5.4 pKi = 5.4 Binding
Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 408 8 1 2 6.6 O=C(O)CCc1ccccc1-c1cccc(-c2ccccc2OCc2ccccc2)c1 10.1016/s0960-894x(03)00794-7
CHEMBL338388 123682 0 None -67 4 Human 5.4 pKi = 5.4 Binding
Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 408 8 1 2 6.6 O=C(O)CCc1ccccc1-c1cccc(-c2ccccc2OCc2ccccc2)c1 10.1016/s0960-894x(03)00794-7
10109445 91918 0 None -537 2 Human 5.4 pKi = 5.4 Binding
Binding affinity to human EP2 receptorBinding affinity to human EP2 receptor
ChEMBL 365 10 2 4 3.5 CCCCC[C@H](O)/C=C/[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)s1 10.1021/jm049290a
CHEMBL224970 91918 0 None -537 2 Human 5.4 pKi = 5.4 Binding
Binding affinity to human EP2 receptorBinding affinity to human EP2 receptor
ChEMBL 365 10 2 4 3.5 CCCCC[C@H](O)/C=C/[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)s1 10.1021/jm049290a
1883 9856 75 None -6 24 Human 7.4 pKi = 7.4 Binding
Binding affinity to EP2 receptor (unknown origin) by competitive binding assayBinding affinity to EP2 receptor (unknown origin) by competitive binding assay
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/jm401431x
1916 9856 75 None -6 24 Human 7.4 pKi = 7.4 Binding
Binding affinity to EP2 receptor (unknown origin) by competitive binding assayBinding affinity to EP2 receptor (unknown origin) by competitive binding assay
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/jm401431x
5280360 9856 75 None -6 24 Human 7.4 pKi = 7.4 Binding
Binding affinity to EP2 receptor (unknown origin) by competitive binding assayBinding affinity to EP2 receptor (unknown origin) by competitive binding assay
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/jm401431x
913 9856 75 None -6 24 Human 7.4 pKi = 7.4 Binding
Binding affinity to EP2 receptor (unknown origin) by competitive binding assayBinding affinity to EP2 receptor (unknown origin) by competitive binding assay
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/jm401431x
CHEMBL548 9856 75 None -6 24 Human 7.4 pKi = 7.4 Binding
Binding affinity to EP2 receptor (unknown origin) by competitive binding assayBinding affinity to EP2 receptor (unknown origin) by competitive binding assay
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/jm401431x
DB00917 9856 75 None -6 24 Human 7.4 pKi = 7.4 Binding
Binding affinity to EP2 receptor (unknown origin) by competitive binding assayBinding affinity to EP2 receptor (unknown origin) by competitive binding assay
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/jm401431x
5283086 210089 24 None -269 5 Mouse 7.4 pKi = 7.4 Binding
Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](O)/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O 10.1016/s0960-894x(01)00359-6
CHEMBL64804 210089 24 None -269 5 Mouse 7.4 pKi = 7.4 Binding
Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](O)/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O 10.1016/s0960-894x(01)00359-6
10271490 172672 0 None -29 3 Human 6.4 pKi = 6.4 Binding
Binding affinity for human prostanoid EP2 receptorBinding affinity for human prostanoid EP2 receptor
ChEMBL 386 9 1 2 5.8 Cc1cccc(CCCc2ccccc2/C=C/C(=O)O)c1OCc1ccccc1 10.1016/j.bmcl.2004.11.051
CHEMBL424975 172672 0 None -29 3 Human 6.4 pKi = 6.4 Binding
Binding affinity for human prostanoid EP2 receptorBinding affinity for human prostanoid EP2 receptor
ChEMBL 386 9 1 2 5.8 Cc1cccc(CCCc2ccccc2/C=C/C(=O)O)c1OCc1ccccc1 10.1016/j.bmcl.2004.11.051
44320433 174722 0 None -45 4 Human 5.4 pKi = 5.4 Binding
Binding affinity at human Prostanoid EP2 receptor.Binding affinity at human Prostanoid EP2 receptor.
ChEMBL 521 11 1 5 6.3 O=C(CCc1ccccc1-c1ccccc1CSCCc1ccccc1)NS(=O)(=O)c1cccs1 10.1016/s0960-894x(02)00518-8
CHEMBL431612 174722 0 None -45 4 Human 5.4 pKi = 5.4 Binding
Binding affinity at human Prostanoid EP2 receptor.Binding affinity at human Prostanoid EP2 receptor.
ChEMBL 521 11 1 5 6.3 O=C(CCc1ccccc1-c1ccccc1CSCCc1ccccc1)NS(=O)(=O)c1cccs1 10.1016/s0960-894x(02)00518-8
24953283 206227 0 None -426 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]PGE2 from human EP2 receptor expressed in HEK293-EBNA cells by scintillation countingDisplacement of [3H]PGE2 from human EP2 receptor expressed in HEK293-EBNA cells by scintillation counting
ChEMBL 467 6 2 3 6.5 C[C@@H](NC(=O)c1c(Cl)sc(Cl)c1Cc1cccc(Cl)c1)c1ccc(C(=O)O)cc1 10.1021/jm901771h
CHEMBL591431 206227 0 None -426 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]PGE2 from human EP2 receptor expressed in HEK293-EBNA cells by scintillation countingDisplacement of [3H]PGE2 from human EP2 receptor expressed in HEK293-EBNA cells by scintillation counting
ChEMBL 467 6 2 3 6.5 C[C@@H](NC(=O)c1c(Cl)sc(Cl)c1Cc1cccc(Cl)c1)c1ccc(C(=O)O)cc1 10.1021/jm901771h
11855594 159759 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 mins
ChEMBL 417 10 2 5 4.4 CCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3975238 159759 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 mins
ChEMBL 417 10 2 5 4.4 CCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
11855594 159759 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 417 10 2 5 4.4 CCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3975238 159759 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 417 10 2 5 4.4 CCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
11294166 83820 0 None -213 3 Human 6.4 pKi = 6.4 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 461 6 2 5 4.3 CC(O)c1cc(S(C)(=O)=O)cc2c3c(n(Cc4ccc(Cl)cc4)c12)[C@@H](CC(=O)O)CC3 10.1016/j.bmcl.2006.02.062
CHEMBL207203 83820 0 None -213 3 Human 6.4 pKi = 6.4 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 461 6 2 5 4.3 CC(O)c1cc(S(C)(=O)=O)cc2c3c(n(Cc4ccc(Cl)cc4)c12)[C@@H](CC(=O)O)CC3 10.1016/j.bmcl.2006.02.062
11294166 83820 0 None -213 3 Human 6.4 pKi = 6.4 Binding
Binding affinity to human EP2 receptor expressed in HEK293 cellsBinding affinity to human EP2 receptor expressed in HEK293 cells
ChEMBL 461 6 2 5 4.3 CC(O)c1cc(S(C)(=O)=O)cc2c3c(n(Cc4ccc(Cl)cc4)c12)[C@@H](CC(=O)O)CC3 10.1021/jm0603668
CHEMBL207203 83820 0 None -213 3 Human 6.4 pKi = 6.4 Binding
Binding affinity to human EP2 receptor expressed in HEK293 cellsBinding affinity to human EP2 receptor expressed in HEK293 cells
ChEMBL 461 6 2 5 4.3 CC(O)c1cc(S(C)(=O)=O)cc2c3c(n(Cc4ccc(Cl)cc4)c12)[C@@H](CC(=O)O)CC3 10.1021/jm0603668
22009003 129394 0 None -436 4 Human 5.4 pKi = 5.4 Binding
Binding affinity for human prostanoid EP2 receptorBinding affinity for human prostanoid EP2 receptor
ChEMBL 468 8 2 3 6.7 Cc1cccc(C(O)/C=C/c2ccccc2/C=C/C(=O)O)c1OCc1c(Cl)cccc1Cl 10.1016/j.bmcl.2004.11.051
CHEMBL360290 129394 0 None -436 4 Human 5.4 pKi = 5.4 Binding
Binding affinity for human prostanoid EP2 receptorBinding affinity for human prostanoid EP2 receptor
ChEMBL 468 8 2 3 6.7 Cc1cccc(C(O)/C=C/c2ccccc2/C=C/C(=O)O)c1OCc1c(Cl)cccc1Cl 10.1016/j.bmcl.2004.11.051
44304008 210021 0 None -549 4 Mouse 5.4 pKi = 5.4 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptor
ChEMBL 410 11 3 6 2.4 O=C(O)CSCCCS[C@H]1C(=O)C[C@@H](O)[C@@H]1/C=C/[C@@H](O)Cc1ccccc1 10.1016/s0960-894x(01)00364-x
CHEMBL64542 210021 0 None -549 4 Mouse 5.4 pKi = 5.4 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptor
ChEMBL 410 11 3 6 2.4 O=C(O)CSCCCS[C@H]1C(=O)C[C@@H](O)[C@@H]1/C=C/[C@@H](O)Cc1ccccc1 10.1016/s0960-894x(01)00364-x
44138108 191064 0 None -12302 6 Human 5.4 pKi = 5.4 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 434 5 1 4 6.6 CC(C)c1nccc2c1c(Sc1ccc(Cl)c(Cl)c1)c1n2CC[C@@H]1CC(=O)O 10.1016/j.bmcl.2009.03.010
CHEMBL483991 191064 0 None -12302 6 Human 5.4 pKi = 5.4 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 434 5 1 4 6.6 CC(C)c1nccc2c1c(Sc1ccc(Cl)c(Cl)c1)c1n2CC[C@@H]1CC(=O)O 10.1016/j.bmcl.2009.03.010
51039064 135979 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding Assay: Measurement of EP2 receptor binding affinity was carried out according to the method of Abramovitz et al. (Biochimica et Biophysica Acta, 1483, 285 (2000)). A test compound dissolved in dimethylsulfoxide and [3H]PGE2 (NET-428, available from PerkinElmer Inc.) (final concentration: 10 nM) were added to a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2, 1 mM EDTA) in which 10 μg of a membrane fraction (ES-562-M, available from Euroscreen S.A.) of HEK293 cells expressing human EP2 receptor had been suspended, followed by incubation at 30° C. for 60 minutes. The membrane fraction was recovered on glass fiber filter paper (GF/B, available from Whatman PLC) using a cell harvester (M30R, available from Brandel Inc.), and after washing with a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2), radioactivity was measured with a liquid scintillation analyzer (2000CA, available from Packard).Binding Assay: Measurement of EP2 receptor binding affinity was carried out according to the method of Abramovitz et al. (Biochimica et Biophysica Acta, 1483, 285 (2000)). A test compound dissolved in dimethylsulfoxide and [3H]PGE2 (NET-428, available from PerkinElmer Inc.) (final concentration: 10 nM) were added to a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2, 1 mM EDTA) in which 10 μg of a membrane fraction (ES-562-M, available from Euroscreen S.A.) of HEK293 cells expressing human EP2 receptor had been suspended, followed by incubation at 30° C. for 60 minutes. The membrane fraction was recovered on glass fiber filter paper (GF/B, available from Whatman PLC) using a cell harvester (M30R, available from Brandel Inc.), and after washing with a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2), radioactivity was measured with a liquid scintillation analyzer (2000CA, available from Packard).
ChEMBL 417 6 5 5 3.7 O=C(NO)c1ccc(CNC(=O)c2[nH]c(-c3ccoc3)cc2-c2ccc(O)cc2)cc1 nan
CHEMBL3670657 135979 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding Assay: Measurement of EP2 receptor binding affinity was carried out according to the method of Abramovitz et al. (Biochimica et Biophysica Acta, 1483, 285 (2000)). A test compound dissolved in dimethylsulfoxide and [3H]PGE2 (NET-428, available from PerkinElmer Inc.) (final concentration: 10 nM) were added to a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2, 1 mM EDTA) in which 10 μg of a membrane fraction (ES-562-M, available from Euroscreen S.A.) of HEK293 cells expressing human EP2 receptor had been suspended, followed by incubation at 30° C. for 60 minutes. The membrane fraction was recovered on glass fiber filter paper (GF/B, available from Whatman PLC) using a cell harvester (M30R, available from Brandel Inc.), and after washing with a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2), radioactivity was measured with a liquid scintillation analyzer (2000CA, available from Packard).Binding Assay: Measurement of EP2 receptor binding affinity was carried out according to the method of Abramovitz et al. (Biochimica et Biophysica Acta, 1483, 285 (2000)). A test compound dissolved in dimethylsulfoxide and [3H]PGE2 (NET-428, available from PerkinElmer Inc.) (final concentration: 10 nM) were added to a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2, 1 mM EDTA) in which 10 μg of a membrane fraction (ES-562-M, available from Euroscreen S.A.) of HEK293 cells expressing human EP2 receptor had been suspended, followed by incubation at 30° C. for 60 minutes. The membrane fraction was recovered on glass fiber filter paper (GF/B, available from Whatman PLC) using a cell harvester (M30R, available from Brandel Inc.), and after washing with a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2), radioactivity was measured with a liquid scintillation analyzer (2000CA, available from Packard).
ChEMBL 417 6 5 5 3.7 O=C(NO)c1ccc(CNC(=O)c2[nH]c(-c3ccoc3)cc2-c2ccc(O)cc2)cc1 nan
1883 9856 75 None -6 24 Human 8.3 pKi = 8.3 Binding
Binding affinity at human prostaglandin EP2 receptorBinding affinity at human prostaglandin EP2 receptor
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmcl.2007.09.074
1916 9856 75 None -6 24 Human 8.3 pKi = 8.3 Binding
Binding affinity at human prostaglandin EP2 receptorBinding affinity at human prostaglandin EP2 receptor
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmcl.2007.09.074
5280360 9856 75 None -6 24 Human 8.3 pKi = 8.3 Binding
Binding affinity at human prostaglandin EP2 receptorBinding affinity at human prostaglandin EP2 receptor
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmcl.2007.09.074
913 9856 75 None -6 24 Human 8.3 pKi = 8.3 Binding
Binding affinity at human prostaglandin EP2 receptorBinding affinity at human prostaglandin EP2 receptor
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmcl.2007.09.074
CHEMBL548 9856 75 None -6 24 Human 8.3 pKi = 8.3 Binding
Binding affinity at human prostaglandin EP2 receptorBinding affinity at human prostaglandin EP2 receptor
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmcl.2007.09.074
DB00917 9856 75 None -6 24 Human 8.3 pKi = 8.3 Binding
Binding affinity at human prostaglandin EP2 receptorBinding affinity at human prostaglandin EP2 receptor
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmcl.2007.09.074
1883 9856 75 None -6 24 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]PGE2 from human EP2 receptorDisplacement of [3H]PGE2 from human EP2 receptor
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmcl.2007.11.020
1916 9856 75 None -6 24 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]PGE2 from human EP2 receptorDisplacement of [3H]PGE2 from human EP2 receptor
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmcl.2007.11.020
5280360 9856 75 None -6 24 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]PGE2 from human EP2 receptorDisplacement of [3H]PGE2 from human EP2 receptor
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmcl.2007.11.020
913 9856 75 None -6 24 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]PGE2 from human EP2 receptorDisplacement of [3H]PGE2 from human EP2 receptor
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmcl.2007.11.020
CHEMBL548 9856 75 None -6 24 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]PGE2 from human EP2 receptorDisplacement of [3H]PGE2 from human EP2 receptor
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmcl.2007.11.020
DB00917 9856 75 None -6 24 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]PGE2 from human EP2 receptorDisplacement of [3H]PGE2 from human EP2 receptor
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmcl.2007.11.020
1883 9856 75 None -6 24 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]PGE2 from human EP2 receptor expressed in HEK293 cellsDisplacement of [3H]PGE2 from human EP2 receptor expressed in HEK293 cells
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmcl.2007.05.025
1916 9856 75 None -6 24 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]PGE2 from human EP2 receptor expressed in HEK293 cellsDisplacement of [3H]PGE2 from human EP2 receptor expressed in HEK293 cells
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmcl.2007.05.025
5280360 9856 75 None -6 24 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]PGE2 from human EP2 receptor expressed in HEK293 cellsDisplacement of [3H]PGE2 from human EP2 receptor expressed in HEK293 cells
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmcl.2007.05.025
913 9856 75 None -6 24 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]PGE2 from human EP2 receptor expressed in HEK293 cellsDisplacement of [3H]PGE2 from human EP2 receptor expressed in HEK293 cells
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmcl.2007.05.025
CHEMBL548 9856 75 None -6 24 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]PGE2 from human EP2 receptor expressed in HEK293 cellsDisplacement of [3H]PGE2 from human EP2 receptor expressed in HEK293 cells
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmcl.2007.05.025
DB00917 9856 75 None -6 24 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]PGE2 from human EP2 receptor expressed in HEK293 cellsDisplacement of [3H]PGE2 from human EP2 receptor expressed in HEK293 cells
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmcl.2007.05.025
44304124 109400 0 None - 1 Mouse 7.4 pKi = 7.4 Binding
Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.
ChEMBL 406 12 3 4 4.3 CC(C)CC1([C@@H](O)C/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2C/C=C\CCCC(=O)O)CCC1 10.1016/s0960-894x(01)00359-6
CHEMBL304225 109400 0 None - 1 Mouse 7.4 pKi = 7.4 Binding
Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.
ChEMBL 406 12 3 4 4.3 CC(C)CC1([C@@H](O)C/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2C/C=C\CCCC(=O)O)CCC1 10.1016/s0960-894x(01)00359-6
11855324 149383 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 mins
ChEMBL 371 6 1 4 4.0 CC(C)(C)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)o2)cc1 nan
CHEMBL3891401 149383 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 mins
ChEMBL 371 6 1 4 4.0 CC(C)(C)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)o2)cc1 nan
11855324 149383 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 371 6 1 4 4.0 CC(C)(C)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)o2)cc1 nan
CHEMBL3891401 149383 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 371 6 1 4 4.0 CC(C)(C)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)o2)cc1 nan
44269486 173621 0 None -144 3 Human 5.4 pKi = 5.4 Binding
Binding affinity towards EP2 receptor expressed in HEK293 ebna cells recombinantly expressing the corresponding human prostanoid cDNAsBinding affinity towards EP2 receptor expressed in HEK293 ebna cells recombinantly expressing the corresponding human prostanoid cDNAs
ChEMBL 341 14 2 3 3.7 CCCCCC(O)CC[C@H]1CCC(=O)N1CCCCCCC(=O)O 10.1016/s0960-894x(03)00042-8
CHEMBL428524 173621 0 None -144 3 Human 5.4 pKi = 5.4 Binding
Binding affinity towards EP2 receptor expressed in HEK293 ebna cells recombinantly expressing the corresponding human prostanoid cDNAsBinding affinity towards EP2 receptor expressed in HEK293 ebna cells recombinantly expressing the corresponding human prostanoid cDNAs
ChEMBL 341 14 2 3 3.7 CCCCCC(O)CC[C@H]1CCC(=O)N1CCCCCCC(=O)O 10.1016/s0960-894x(03)00042-8
138 9855 88 None -19 18 Mouse 7.4 pKi = 7.4 Binding
Affinity for mouse Prostanoid EP2 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP2 receptor expressed in CHO cells
ChEMBL 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 10.1016/s0960-894x(01)00365-1
149351 9855 88 None -19 18 Mouse 7.4 pKi = 7.4 Binding
Affinity for mouse Prostanoid EP2 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP2 receptor expressed in CHO cells
ChEMBL 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 10.1016/s0960-894x(01)00365-1
1882 9855 88 None -19 18 Mouse 7.4 pKi = 7.4 Binding
Affinity for mouse Prostanoid EP2 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP2 receptor expressed in CHO cells
ChEMBL 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 10.1016/s0960-894x(01)00365-1
5280723 9855 88 None -19 18 Mouse 7.4 pKi = 7.4 Binding
Affinity for mouse Prostanoid EP2 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP2 receptor expressed in CHO cells
ChEMBL 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 10.1016/s0960-894x(01)00365-1
CHEMBL495 9855 88 None -19 18 Mouse 7.4 pKi = 7.4 Binding
Affinity for mouse Prostanoid EP2 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP2 receptor expressed in CHO cells
ChEMBL 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 10.1016/s0960-894x(01)00365-1
DB00770 9855 88 None -19 18 Mouse 7.4 pKi = 7.4 Binding
Affinity for mouse Prostanoid EP2 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP2 receptor expressed in CHO cells
ChEMBL 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 10.1016/s0960-894x(01)00365-1
138 9855 88 None -19 18 Mouse 7.4 pKi = 7.4 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptor
ChEMBL 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 10.1016/s0960-894x(01)00364-x
149351 9855 88 None -19 18 Mouse 7.4 pKi = 7.4 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptor
ChEMBL 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 10.1016/s0960-894x(01)00364-x
1882 9855 88 None -19 18 Mouse 7.4 pKi = 7.4 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptor
ChEMBL 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 10.1016/s0960-894x(01)00364-x
5280723 9855 88 None -19 18 Mouse 7.4 pKi = 7.4 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptor
ChEMBL 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 10.1016/s0960-894x(01)00364-x
CHEMBL495 9855 88 None -19 18 Mouse 7.4 pKi = 7.4 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptor
ChEMBL 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 10.1016/s0960-894x(01)00364-x
DB00770 9855 88 None -19 18 Mouse 7.4 pKi = 7.4 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptor
ChEMBL 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 10.1016/s0960-894x(01)00364-x
10183680 133944 0 None -2 3 Mouse 6.4 pKi = 6.4 Binding
Ability to inhibit the binding of [3H]-PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP2Ability to inhibit the binding of [3H]-PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP2
ChEMBL 470 6 1 6 4.5 Cc1cc2c(CC(=O)O)cccc2n1C(=O)c1ccc(OC[C@H]2CN(C)c3ccccc3O2)cc1 10.1016/j.bmcl.2004.07.039
CHEMBL365696 133944 0 None -2 3 Mouse 6.4 pKi = 6.4 Binding
Ability to inhibit the binding of [3H]-PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP2Ability to inhibit the binding of [3H]-PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP2
ChEMBL 470 6 1 6 4.5 Cc1cc2c(CC(=O)O)cccc2n1C(=O)c1ccc(OC[C@H]2CN(C)c3ccccc3O2)cc1 10.1016/j.bmcl.2004.07.039
11597294 172955 4 None -489 8 Human 6.4 pKi = 6.4 Binding
Binding affinity to human EP2 receptor expressed in HEK293 cellsBinding affinity to human EP2 receptor expressed in HEK293 cells
ChEMBL 435 4 1 2 5.7 O=C(O)C[C@H]1CCc2c1n(Cc1ccc(Cl)cc1)c1c(Br)cc(F)cc21 10.1021/jm0603668
CHEMBL426387 172955 4 None -489 8 Human 6.4 pKi = 6.4 Binding
Binding affinity to human EP2 receptor expressed in HEK293 cellsBinding affinity to human EP2 receptor expressed in HEK293 cells
ChEMBL 435 4 1 2 5.7 O=C(O)C[C@H]1CCc2c1n(Cc1ccc(Cl)cc1)c1c(Br)cc(F)cc21 10.1021/jm0603668
57391585 76242 0 None -457 2 Mouse 6.4 pKi = 6.4 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 393 8 2 3 3.4 Cc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=O)N2CCc2ccc(C(=O)O)cc2)c1 10.1016/j.bmcl.2011.10.109
CHEMBL1933718 76242 0 None -457 2 Mouse 6.4 pKi = 6.4 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 393 8 2 3 3.4 Cc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=O)N2CCc2ccc(C(=O)O)cc2)c1 10.1016/j.bmcl.2011.10.109
57391585 76242 0 None -457 2 Mouse 6.4 pKi = 6.4 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 393 8 2 3 3.4 Cc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=O)N2CCc2ccc(C(=O)O)cc2)c1 10.1016/j.bmc.2012.02.018
CHEMBL1933718 76242 0 None -457 2 Mouse 6.4 pKi = 6.4 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 393 8 2 3 3.4 Cc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=O)N2CCc2ccc(C(=O)O)cc2)c1 10.1016/j.bmc.2012.02.018
10112486 23673 0 None -7 4 Human 5.4 pKi = 5.4 Binding
Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 414 8 1 3 6.7 O=C(O)CCc1ccccc1-c1ccc(-c2ccccc2OCc2ccccc2)s1 10.1016/s0960-894x(03)00794-7
CHEMBL125110 23673 0 None -7 4 Human 5.4 pKi = 5.4 Binding
Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 414 8 1 3 6.7 O=C(O)CCc1ccccc1-c1ccc(-c2ccccc2OCc2ccccc2)s1 10.1016/s0960-894x(03)00794-7
44390831 70411 0 None -575 4 Human 5.4 pKi = 5.4 Binding
Binding affinity for human prostanoid EP2 receptorBinding affinity for human prostanoid EP2 receptor
ChEMBL 402 8 1 2 6.1 Cc1cccc(/C=C/Cc2ccccc2/C=C/C(=O)O)c1OCc1ccc(F)cc1 10.1016/j.bmcl.2004.11.051
CHEMBL180089 70411 0 None -575 4 Human 5.4 pKi = 5.4 Binding
Binding affinity for human prostanoid EP2 receptorBinding affinity for human prostanoid EP2 receptor
ChEMBL 402 8 1 2 6.1 Cc1cccc(/C=C/Cc2ccccc2/C=C/C(=O)O)c1OCc1ccc(F)cc1 10.1016/j.bmcl.2004.11.051
44289969 108155 0 None -17 2 Human 4.4 pKi = 4.4 Binding
Binding affinity was determined against prostanoid EP2 receptorBinding affinity was determined against prostanoid EP2 receptor
ChEMBL 345 10 2 3 3.3 O=C(O)CCCCCCN1C(=O)CC[C@@H]1/C=C/C(O)c1ccccc1 10.1016/j.bmcl.2004.01.063
CHEMBL297139 108155 0 None -17 2 Human 4.4 pKi = 4.4 Binding
Binding affinity was determined against prostanoid EP2 receptorBinding affinity was determined against prostanoid EP2 receptor
ChEMBL 345 10 2 3 3.3 O=C(O)CCCCCCN1C(=O)CC[C@@H]1/C=C/C(O)c1ccccc1 10.1016/j.bmcl.2004.01.063
57398586 76251 0 None -53 3 Mouse 7.4 pKi = 7.4 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 422 9 2 7 3.0 Cc1ccc(C[C@H](O)/C=C/[C@H]2CCC(=O)N2CCSc2nc(C(=O)O)cs2)o1 10.1016/j.bmcl.2011.10.109
CHEMBL1933727 76251 0 None -53 3 Mouse 7.4 pKi = 7.4 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 422 9 2 7 3.0 Cc1ccc(C[C@H](O)/C=C/[C@H]2CCC(=O)N2CCSc2nc(C(=O)O)cs2)o1 10.1016/j.bmcl.2011.10.109
44290262 185298 0 None -10 2 Human 5.4 pKi = 5.4 Binding
Binding affinity was determined against prostanoid EP2 receptorBinding affinity was determined against prostanoid EP2 receptor
ChEMBL 455 11 2 3 5.6 O=C(O)CCCCCCN1C(=O)CC[C@@H]1/C=C/C(O)c1cccc(-c2ccc(Cl)cc2)c1 10.1016/j.bmcl.2004.01.063
CHEMBL46671 185298 0 None -10 2 Human 5.4 pKi = 5.4 Binding
Binding affinity was determined against prostanoid EP2 receptorBinding affinity was determined against prostanoid EP2 receptor
ChEMBL 455 11 2 3 5.6 O=C(O)CCCCCCN1C(=O)CC[C@@H]1/C=C/C(O)c1cccc(-c2ccc(Cl)cc2)c1 10.1016/j.bmcl.2004.01.063
44290272 108220 0 None -6760 2 Human 4.4 pKi = 4.4 Binding
Binding affinity was determined against prostanoid EP2 receptorBinding affinity was determined against prostanoid EP2 receptor
ChEMBL 455 11 2 3 5.6 O=C(O)CCCCCCN1C(=O)CC[C@@H]1/C=C/C(O)c1cccc(-c2ccccc2Cl)c1 10.1016/j.bmcl.2004.01.063
CHEMBL297578 108220 0 None -6760 2 Human 4.4 pKi = 4.4 Binding
Binding affinity was determined against prostanoid EP2 receptorBinding affinity was determined against prostanoid EP2 receptor
ChEMBL 455 11 2 3 5.6 O=C(O)CCCCCCN1C(=O)CC[C@@H]1/C=C/C(O)c1cccc(-c2ccccc2Cl)c1 10.1016/j.bmcl.2004.01.063
44442327 101234 0 None -147 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]PGE2 from human EP2 receptorDisplacement of [3H]PGE2 from human EP2 receptor
ChEMBL 345 9 2 3 3.0 CCCC[C@H](O)/C=C/[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.11.020
CHEMBL251294 101234 0 None -147 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]PGE2 from human EP2 receptorDisplacement of [3H]PGE2 from human EP2 receptor
ChEMBL 345 9 2 3 3.0 CCCC[C@H](O)/C=C/[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.11.020
71462285 88655 0 None -239 4 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]PGE2 from human EP2R expressed in chem1 cells after 2hrs by beta countingDisplacement of [3H]PGE2 from human EP2R expressed in chem1 cells after 2hrs by beta counting
ChEMBL 478 10 1 5 6.0 COc1cc(C/C=C/c2ccccc2/C=C/C(=O)O)ccc1OCCn1cc2ccccc2c1C#N 10.1021/ml300191g
CHEMBL2164608 88655 0 None -239 4 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]PGE2 from human EP2R expressed in chem1 cells after 2hrs by beta countingDisplacement of [3H]PGE2 from human EP2R expressed in chem1 cells after 2hrs by beta counting
ChEMBL 478 10 1 5 6.0 COc1cc(C/C=C/c2ccccc2/C=C/C(=O)O)ccc1OCCn1cc2ccccc2c1C#N 10.1021/ml300191g
44303711 109129 0 None 18 3 Mouse 7.4 pKi = 7.4 Binding
Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.
ChEMBL 406 13 3 4 4.4 CCCCC1([C@@H](O)C/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2C/C=C\CCCC(=O)O)CCC1 10.1016/s0960-894x(01)00359-6
CHEMBL303763 109129 0 None 18 3 Mouse 7.4 pKi = 7.4 Binding
Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.
ChEMBL 406 13 3 4 4.4 CCCCC1([C@@H](O)C/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2C/C=C\CCCC(=O)O)CCC1 10.1016/s0960-894x(01)00359-6
24953285 207648 0 None -53 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]PGE2 from human EP2 receptor expressed in HEK293-EBNA cells by scintillation countingDisplacement of [3H]PGE2 from human EP2 receptor expressed in HEK293-EBNA cells by scintillation counting
ChEMBL 453 6 2 3 5.9 O=C(O)c1ccc(CNC(=O)c2c(Cl)sc(Cl)c2Cc2cccc(Cl)c2)cc1 10.1021/jm901771h
CHEMBL601299 207648 0 None -53 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]PGE2 from human EP2 receptor expressed in HEK293-EBNA cells by scintillation countingDisplacement of [3H]PGE2 from human EP2 receptor expressed in HEK293-EBNA cells by scintillation counting
ChEMBL 453 6 2 3 5.9 O=C(O)c1ccc(CNC(=O)c2c(Cl)sc(Cl)c2Cc2cccc(Cl)c2)cc1 10.1021/jm901771h
155520370 177255 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]prostaglandin E2 from human EP2 receptor expressed in HEK293 cell membranes after 60 mins by liquid scintillation countingDisplacement of [3H]prostaglandin E2 from human EP2 receptor expressed in HEK293 cell membranes after 60 mins by liquid scintillation counting
ChEMBL 478 7 1 5 5.2 CC(C)(C)c1ccc(CN(Cc2ccc3cc(C(=O)O)oc3c2)S(=O)(=O)c2cccnc2)cc1 10.1021/acs.jmedchem.8b00808
CHEMBL4448995 177255 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]prostaglandin E2 from human EP2 receptor expressed in HEK293 cell membranes after 60 mins by liquid scintillation countingDisplacement of [3H]prostaglandin E2 from human EP2 receptor expressed in HEK293 cell membranes after 60 mins by liquid scintillation counting
ChEMBL 478 7 1 5 5.2 CC(C)(C)c1ccc(CN(Cc2ccc3cc(C(=O)O)oc3c2)S(=O)(=O)c2cccnc2)cc1 10.1021/acs.jmedchem.8b00808
56665068 71598 0 None -3 4 Mouse 7.4 pKi = 7.4 Binding
Displacement of [3H]PGE2 from mouse prostaglandin EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]PGE2 from mouse prostaglandin EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 500 7 2 5 5.1 CN1C[C@@H](COc2ccc(C(=O)Nc3cc(CC(=O)O)ccc3Cl)c(Cl)c2)Oc2ccccc21 10.1016/j.bmc.2011.08.007
CHEMBL1819622 71598 0 None -3 4 Mouse 7.4 pKi = 7.4 Binding
Displacement of [3H]PGE2 from mouse prostaglandin EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]PGE2 from mouse prostaglandin EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 500 7 2 5 5.1 CN1C[C@@H](COc2ccc(C(=O)Nc3cc(CC(=O)O)ccc3Cl)c(Cl)c2)Oc2ccccc21 10.1016/j.bmc.2011.08.007
10269242 162354 0 None -2 2 Human 5.4 pKi = 5.4 Binding
Binding affinity at human prostaglandin EP2 receptorBinding affinity at human prostaglandin EP2 receptor
ChEMBL 348 9 2 4 2.2 CC(C)CC(O)CCN1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.09.074
CHEMBL404413 162354 0 None -2 2 Human 5.4 pKi = 5.4 Binding
Binding affinity at human prostaglandin EP2 receptorBinding affinity at human prostaglandin EP2 receptor
ChEMBL 348 9 2 4 2.2 CC(C)CC(O)CCN1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.09.074
21974528 131228 0 None -22 5 Mouse 6.4 pKi = 6.4 Binding
Ability to inhibit the binding of [3H]-PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP2Ability to inhibit the binding of [3H]-PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP2
ChEMBL 441 6 1 5 4.6 Cc1cc2c(CC(=O)O)cccc2n1C(=O)c1ccc(OCC2Cc3ccccc3O2)cc1 10.1016/j.bmcl.2004.07.039
CHEMBL363984 131228 0 None -22 5 Mouse 6.4 pKi = 6.4 Binding
Ability to inhibit the binding of [3H]-PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP2Ability to inhibit the binding of [3H]-PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP2
ChEMBL 441 6 1 5 4.6 Cc1cc2c(CC(=O)O)cccc2n1C(=O)c1ccc(OCC2Cc3ccccc3O2)cc1 10.1016/j.bmcl.2004.07.039
44289922 170303 0 None -954 5 Human 5.4 pKi = 5.4 Binding
Binding affinity was determined against prostanoid EP2 receptorBinding affinity was determined against prostanoid EP2 receptor
ChEMBL 339 13 2 3 3.5 CCCCC[C@H](O)/C=C/[C@H]1CCC(=O)N1CCCCCCC(=O)O 10.1016/j.bmcl.2004.01.063
CHEMBL42027 170303 0 None -954 5 Human 5.4 pKi = 5.4 Binding
Binding affinity was determined against prostanoid EP2 receptorBinding affinity was determined against prostanoid EP2 receptor
ChEMBL 339 13 2 3 3.5 CCCCC[C@H](O)/C=C/[C@H]1CCC(=O)N1CCCCCCC(=O)O 10.1016/j.bmcl.2004.01.063
10227492 23670 0 None -218 4 Human 5.3 pKi = 5.3 Binding
Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 476 8 1 2 7.9 O=C(O)CCc1ccccc1-c1cccc(-c2ccccc2OCc2c(Cl)cccc2Cl)c1 10.1016/s0960-894x(03)00794-7
CHEMBL125087 23670 0 None -218 4 Human 5.3 pKi = 5.3 Binding
Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 476 8 1 2 7.9 O=C(O)CCc1ccccc1-c1cccc(-c2ccccc2OCc2c(Cl)cccc2Cl)c1 10.1016/s0960-894x(03)00794-7
44349528 120578 0 None -131 4 Human 5.3 pKi = 5.3 Binding
Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 428 8 1 3 7.2 CC(CC(=O)O)c1ccccc1-c1csc(-c2ccccc2OCc2ccccc2)c1 10.1016/s0960-894x(03)00794-7
CHEMBL332446 120578 0 None -131 4 Human 5.3 pKi = 5.3 Binding
Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 428 8 1 3 7.2 CC(CC(=O)O)c1ccccc1-c1csc(-c2ccccc2OCc2ccccc2)c1 10.1016/s0960-894x(03)00794-7
59465601 156673 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 402 13 1 4 5.4 CCCCC(O)Cc1ccc([C@H]2CCC(=O)[C@@H]2CCCCCCC(=O)OC)cc1 nan
CHEMBL3949271 156673 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 402 13 1 4 5.4 CCCCC(O)Cc1ccc([C@H]2CCC(=O)[C@@H]2CCCCCCC(=O)OC)cc1 nan
24953286 208163 0 None -151 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]PGE2 from human EP2 receptor expressed in HEK293-EBNA cells by scintillation countingDisplacement of [3H]PGE2 from human EP2 receptor expressed in HEK293-EBNA cells by scintillation counting
ChEMBL 427 6 2 3 5.8 Cc1sc(C)c(C(=O)N[C@@H](C)c2ccc(C(=O)O)cc2)c1Cc1cccc(Cl)c1 10.1021/jm901771h
CHEMBL604546 208163 0 None -151 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]PGE2 from human EP2 receptor expressed in HEK293-EBNA cells by scintillation countingDisplacement of [3H]PGE2 from human EP2 receptor expressed in HEK293-EBNA cells by scintillation counting
ChEMBL 427 6 2 3 5.8 Cc1sc(C)c(C(=O)N[C@@H](C)c2ccc(C(=O)O)cc2)c1Cc1cccc(Cl)c1 10.1021/jm901771h
54013831 153238 0 None 3 2 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 402 13 1 4 5.9 CCCCCC(O)c1ccc([C@H]2CCC(=O)[C@@H]2CCCCCCC(=O)OC)cc1 nan
CHEMBL3922151 153238 0 None 3 2 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 402 13 1 4 5.9 CCCCCC(O)c1ccc([C@H]2CCC(=O)[C@@H]2CCCCCCC(=O)OC)cc1 nan
9845064 76123 0 None -194 3 Mouse 6.3 pKi = 6.3 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counterDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counter
ChEMBL 420 13 2 5 3.9 COCc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=O)[C@@H]2CCSCCCC(=O)O)c1 10.1016/j.bmc.2011.12.009
CHEMBL1929528 76123 0 None -194 3 Mouse 6.3 pKi = 6.3 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counterDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counter
ChEMBL 420 13 2 5 3.9 COCc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=O)[C@@H]2CCSCCCC(=O)O)c1 10.1016/j.bmc.2011.12.009
11395329 130625 0 None -17 2 Mouse 5.3 pKi = 5.3 Binding
Binding affinity for mouse Prostanoid EP2 receptorBinding affinity for mouse Prostanoid EP2 receptor
ChEMBL 395 8 1 5 4.5 CCCCOc1ccc(C(=O)n2c(C)c(CC(=O)O)c3cc(OC)ccc32)cc1 10.1016/j.bmcl.2004.06.006
CHEMBL362541 130625 0 None -17 2 Mouse 5.3 pKi = 5.3 Binding
Binding affinity for mouse Prostanoid EP2 receptorBinding affinity for mouse Prostanoid EP2 receptor
ChEMBL 395 8 1 5 4.5 CCCCOc1ccc(C(=O)n2c(C)c(CC(=O)O)c3cc(OC)ccc32)cc1 10.1016/j.bmcl.2004.06.006
9885106 91548 0 None -2344 6 Human 5.3 pKi = 5.3 Binding
Binding affinity to human EP2 receptorBinding affinity to human EP2 receptor
ChEMBL 357 13 2 4 3.1 CCCCC[C@H](O)/C=C/[C@H]1CCC(=O)N1CCSCCCC(=O)O 10.1021/jm049290a
CHEMBL223151 91548 0 None -2344 6 Human 5.3 pKi = 5.3 Binding
Binding affinity to human EP2 receptorBinding affinity to human EP2 receptor
ChEMBL 357 13 2 4 3.1 CCCCC[C@H](O)/C=C/[C@H]1CCC(=O)N1CCSCCCC(=O)O 10.1021/jm049290a
44304389 209932 0 None -40 4 Mouse 7.3 pKi = 7.3 Binding
Affinity for mouse Prostanoid EP2 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP2 receptor expressed in CHO cells
ChEMBL 372 13 3 5 3.0 CCCCC[C@H](O)/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCSCC(=O)O 10.1016/s0960-894x(01)00365-1
CHEMBL64188 209932 0 None -40 4 Mouse 7.3 pKi = 7.3 Binding
Affinity for mouse Prostanoid EP2 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP2 receptor expressed in CHO cells
ChEMBL 372 13 3 5 3.0 CCCCC[C@H](O)/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCSCC(=O)O 10.1016/s0960-894x(01)00365-1
10168694 213128 0 None -309 4 Human 5.3 pKi = 5.3 Binding
Binding affinity at human Prostanoid EP2 receptor.Binding affinity at human Prostanoid EP2 receptor.
ChEMBL 671 17 1 7 8.2 O=C(CCc1ccccc1-c1ccc(OCCCOc2cccc(CSCCc3ccccc3)c2)cc1)NS(=O)(=O)c1cccs1 10.1016/s0960-894x(02)00518-8
CHEMBL87366 213128 0 None -309 4 Human 5.3 pKi = 5.3 Binding
Binding affinity at human Prostanoid EP2 receptor.Binding affinity at human Prostanoid EP2 receptor.
ChEMBL 671 17 1 7 8.2 O=C(CCc1ccccc1-c1ccc(OCCCOc2cccc(CSCCc3ccccc3)c2)cc1)NS(=O)(=O)c1cccs1 10.1016/s0960-894x(02)00518-8
12521 8978 0 None -20892 4 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]PGE2 from human recombinant EP2 receptor expressed in HEK293 cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]PGE2 from human recombinant EP2 receptor expressed in HEK293 cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 399 11 2 3 3.6 FC1(C(N([C@H](C1)/C=C/[C@H]([C@H](CC#CCC)C)O)CCCCCCC(=O)O)=O)F 10.1021/acs.jmedchem.9b00336
72722131 8978 0 None -20892 4 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]PGE2 from human recombinant EP2 receptor expressed in HEK293 cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]PGE2 from human recombinant EP2 receptor expressed in HEK293 cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 399 11 2 3 3.6 FC1(C(N([C@H](C1)/C=C/[C@H]([C@H](CC#CCC)C)O)CCCCCCC(=O)O)=O)F 10.1021/acs.jmedchem.9b00336
CHEMBL3918816 8978 0 None -20892 4 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]PGE2 from human recombinant EP2 receptor expressed in HEK293 cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]PGE2 from human recombinant EP2 receptor expressed in HEK293 cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 399 11 2 3 3.6 FC1(C(N([C@H](C1)/C=C/[C@H]([C@H](CC#CCC)C)O)CCCCCCC(=O)O)=O)F 10.1021/acs.jmedchem.9b00336
1929 8386 55 None -11 2 Human 7.3 pKi = 7.3 Binding
Binding affinity to EP2 receptor (unknown origin) by competitive binding assayBinding affinity to EP2 receptor (unknown origin) by competitive binding assay
ChEMBL 468 9 1 5 4.2 OC(=O)COc1cccc(c1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)C(C)(C)C 10.1021/jm401431x
9890801 8386 55 None -11 2 Human 7.3 pKi = 7.3 Binding
Binding affinity to EP2 receptor (unknown origin) by competitive binding assayBinding affinity to EP2 receptor (unknown origin) by competitive binding assay
ChEMBL 468 9 1 5 4.2 OC(=O)COc1cccc(c1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)C(C)(C)C 10.1021/jm401431x
CHEMBL563646 8386 55 None -11 2 Human 7.3 pKi = 7.3 Binding
Binding affinity to EP2 receptor (unknown origin) by competitive binding assayBinding affinity to EP2 receptor (unknown origin) by competitive binding assay
ChEMBL 468 9 1 5 4.2 OC(=O)COc1cccc(c1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)C(C)(C)C 10.1021/jm401431x
DB12022 8386 55 None -11 2 Human 7.3 pKi = 7.3 Binding
Binding affinity to EP2 receptor (unknown origin) by competitive binding assayBinding affinity to EP2 receptor (unknown origin) by competitive binding assay
ChEMBL 468 9 1 5 4.2 OC(=O)COc1cccc(c1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)C(C)(C)C 10.1021/jm401431x
10299717 71191 0 None -144 6 Mouse 6.3 pKi = 6.3 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 484 6 1 6 4.9 Cc1cc(OC[C@@H]2CN(C)c3ccccc3O2)ccc1C(=O)n1c(C)c(CC(=O)O)c2ccccc21 10.1016/j.bmc.2011.06.014
CHEMBL1813120 71191 0 None -144 6 Mouse 6.3 pKi = 6.3 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 484 6 1 6 4.9 Cc1cc(OC[C@@H]2CN(C)c3ccccc3O2)ccc1C(=O)n1c(C)c(CC(=O)O)c2ccccc21 10.1016/j.bmc.2011.06.014
59465588 150304 0 None - 1 Human 4.3 pKi = 4.3 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 422 13 1 3 6.9 CCCCCC(O)c1ccc([C@H]2CC[C@@H](Cl)[C@@H]2CCCCCCC(=O)OC)cc1 nan
CHEMBL3898887 150304 0 None - 1 Human 4.3 pKi = 4.3 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 422 13 1 3 6.9 CCCCCC(O)c1ccc([C@H]2CC[C@@H](Cl)[C@@H]2CCCCCCC(=O)OC)cc1 nan
59465575 151845 0 None - 1 Human 4.3 pKi = 4.3 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 402 13 1 4 5.9 CCCCCC(O)c1cccc([C@H]2CCC(=O)[C@@H]2CCCCCCC(=O)OC)c1 nan
CHEMBL3911438 151845 0 None - 1 Human 4.3 pKi = 4.3 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 402 13 1 4 5.9 CCCCCC(O)c1cccc([C@H]2CCC(=O)[C@@H]2CCCCCCC(=O)OC)c1 nan
59465592 156481 0 None - 1 Human 4.3 pKi = 4.3 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 386 13 1 3 6.6 CCCCCC(O)c1ccc([C@H]2CCC=C2CCCCCCC(=O)OC)cc1 nan
CHEMBL3947785 156481 0 None - 1 Human 4.3 pKi = 4.3 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 386 13 1 3 6.6 CCCCCC(O)c1ccc([C@H]2CCC=C2CCCCCCC(=O)OC)cc1 nan
59465590 157724 0 None - 1 Human 4.3 pKi = 4.3 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 406 13 1 3 6.6 CCCCCC(O)c1ccc([C@H]2CC[C@@H](F)[C@@H]2CCCCCCC(=O)OC)cc1 nan
CHEMBL3957958 157724 0 None - 1 Human 4.3 pKi = 4.3 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 406 13 1 3 6.6 CCCCCC(O)c1ccc([C@H]2CC[C@@H](F)[C@@H]2CCCCCCC(=O)OC)cc1 nan
59465584 158209 0 None - 1 Human 4.3 pKi = 4.3 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 394 13 2 2 6.7 CCCCCC(O)c1ccc([C@H]2CC[C@@H](Cl)[C@@H]2CCCCCCCO)cc1 nan
CHEMBL3961847 158209 0 None - 1 Human 4.3 pKi = 4.3 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 394 13 2 2 6.7 CCCCCC(O)c1ccc([C@H]2CC[C@@H](Cl)[C@@H]2CCCCCCCO)cc1 nan
11855325 151469 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 mins
ChEMBL 387 6 1 4 4.5 CC(C)(C)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3908484 151469 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 mins
ChEMBL 387 6 1 4 4.5 CC(C)(C)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
11855325 151469 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 387 6 1 4 4.5 CC(C)(C)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3908484 151469 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 387 6 1 4 4.5 CC(C)(C)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
57564500 157989 0 None 4 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 440 12 2 2 6.8 CCCCCC(O)c1ccc([C@H]2[C@@H](Cl)C[C@@H](Cl)[C@@H]2C/C=C\CCCC(=O)O)cc1 nan
CHEMBL3959926 157989 0 None 4 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 440 12 2 2 6.8 CCCCCC(O)c1ccc([C@H]2[C@@H](Cl)C[C@@H](Cl)[C@@H]2C/C=C\CCCC(=O)O)cc1 nan
12137443 91478 0 None -5495 4 Human 5.3 pKi = 5.3 Binding
Binding affinity to human EP2 receptorBinding affinity to human EP2 receptor
ChEMBL 491 9 2 3 6.1 Cc1cc(Cl)ccc1-c1cccc([C@H](O)CC[C@H]2CCC(=O)N2CCc2ccc(C(=O)O)cc2)c1 10.1021/jm049290a
CHEMBL222677 91478 0 None -5495 4 Human 5.3 pKi = 5.3 Binding
Binding affinity to human EP2 receptorBinding affinity to human EP2 receptor
ChEMBL 491 9 2 3 6.1 Cc1cc(Cl)ccc1-c1cccc([C@H](O)CC[C@H]2CCC(=O)N2CCc2ccc(C(=O)O)cc2)c1 10.1021/jm049290a
11224239 71578 0 None -1 4 Mouse 6.3 pKi = 6.3 Binding
Displacement of [3H]PGE2 from mouse prostaglandin EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]PGE2 from mouse prostaglandin EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 432 7 2 5 3.8 CN1C[C@@H](COc2ccc(C(=O)Nc3cccc(CC(=O)O)c3)cc2)Oc2ccccc21 10.1016/j.bmc.2011.08.007
CHEMBL1819603 71578 0 None -1 4 Mouse 6.3 pKi = 6.3 Binding
Displacement of [3H]PGE2 from mouse prostaglandin EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]PGE2 from mouse prostaglandin EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 432 7 2 5 3.8 CN1C[C@@H](COc2ccc(C(=O)Nc3cccc(CC(=O)O)c3)cc2)Oc2ccccc21 10.1016/j.bmc.2011.08.007
11282034 73404 0 None -13 3 Mouse 5.3 pKi = 5.3 Binding
Binding affinity for mouse Prostanoid EP2 receptorBinding affinity for mouse Prostanoid EP2 receptor
ChEMBL 437 11 1 5 5.6 CCCCOc1ccc(C(=O)n2c(C)c(CCCCC(=O)O)c3cc(OC)ccc32)cc1 10.1016/j.bmcl.2004.06.006
CHEMBL185277 73404 0 None -13 3 Mouse 5.3 pKi = 5.3 Binding
Binding affinity for mouse Prostanoid EP2 receptorBinding affinity for mouse Prostanoid EP2 receptor
ChEMBL 437 11 1 5 5.6 CCCCOc1ccc(C(=O)n2c(C)c(CCCCC(=O)O)c3cc(OC)ccc32)cc1 10.1016/j.bmcl.2004.06.006
46887240 15526 0 None -13489 3 Mouse 5.3 pKi = 5.3 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 472 10 3 3 6.9 Cc1cccc(Nc2ccc(CCC(=O)O)c(C(=O)N[C@H](CC(C)C)c3cc(C)cc(C)c3)c2)c1 10.1016/j.bmc.2010.03.028
CHEMBL1096382 15526 0 None -13489 3 Mouse 5.3 pKi = 5.3 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 472 10 3 3 6.9 Cc1cccc(Nc2ccc(CCC(=O)O)c(C(=O)N[C@H](CC(C)C)c3cc(C)cc(C)c3)c2)c1 10.1016/j.bmc.2010.03.028
52945419 23306 0 None -478 4 Human 5.3 pKi = 5.3 Binding
Binding affinity for human prostanoid EP2 receptorBinding affinity for human prostanoid EP2 receptor
ChEMBL 772 16 4 6 10.7 O=C(O)/C=C/c1ccccc1/C=C/Cc1cccc(O)c1OCc1ccccc1.O=C(O)/C=C/c1ccccc1C/C=C\c1cccc(O)c1OCc1ccccc1 10.1016/j.bmcl.2004.11.051
CHEMBL1237296 23306 0 None -478 4 Human 5.3 pKi = 5.3 Binding
Binding affinity for human prostanoid EP2 receptorBinding affinity for human prostanoid EP2 receptor
ChEMBL 772 16 4 6 10.7 O=C(O)/C=C/c1ccccc1/C=C/Cc1cccc(O)c1OCc1ccccc1.O=C(O)/C=C/c1ccccc1C/C=C\c1cccc(O)c1OCc1ccccc1 10.1016/j.bmcl.2004.11.051
56672018 71581 0 None -6 3 Mouse 5.3 pKi = 5.3 Binding
Displacement of [3H]PGE2 from mouse prostaglandin EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]PGE2 from mouse prostaglandin EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 446 7 1 5 3.9 CN1C[C@@H](COc2ccc(C(=O)N(C)c3cccc(CC(=O)O)c3)cc2)Oc2ccccc21 10.1016/j.bmc.2011.08.007
CHEMBL1819606 71581 0 None -6 3 Mouse 5.3 pKi = 5.3 Binding
Displacement of [3H]PGE2 from mouse prostaglandin EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]PGE2 from mouse prostaglandin EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 446 7 1 5 3.9 CN1C[C@@H](COc2ccc(C(=O)N(C)c3cccc(CC(=O)O)c3)cc2)Oc2ccccc21 10.1016/j.bmc.2011.08.007
44303709 209979 0 None -870 3 Mouse 5.3 pKi = 5.3 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptor
ChEMBL 470 13 3 7 3.3 CSCc1cccc(C[C@H](O)/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2SCCCSCC(=O)O)c1 10.1016/s0960-894x(01)00364-x
CHEMBL64338 209979 0 None -870 3 Mouse 5.3 pKi = 5.3 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptor
ChEMBL 470 13 3 7 3.3 CSCc1cccc(C[C@H](O)/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2SCCCSCC(=O)O)c1 10.1016/s0960-894x(01)00364-x
59465581 150890 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 428 11 2 4 6.1 CCCCCC(O)c1ccc([C@H]2CCC(=O)[C@@H]2CCCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3903611 150890 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 428 11 2 4 6.1 CCCCCC(O)c1ccc([C@H]2CCC(=O)[C@@H]2CCCc2ccc(C(=O)O)s2)cc1 nan
44455236 102250 0 None -53 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]PGE2 from human EP2 receptorDisplacement of [3H]PGE2 from human EP2 receptor
ChEMBL 373 11 2 3 3.8 CCCCCC[C@H](O)/C=C/[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.11.020
CHEMBL257217 102250 0 None -53 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]PGE2 from human EP2 receptorDisplacement of [3H]PGE2 from human EP2 receptor
ChEMBL 373 11 2 3 3.8 CCCCCC[C@H](O)/C=C/[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.11.020
21974448 73737 0 None -53 4 Mouse 6.3 pKi = 6.3 Binding
Ability to inhibit the binding of [3H]-PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP2Ability to inhibit the binding of [3H]-PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP2
ChEMBL 429 8 1 5 4.7 Cc1cc2c(CC(=O)O)cccc2n1C(=O)c1ccc(OCCOc2ccccc2)cc1 10.1016/j.bmcl.2004.07.039
CHEMBL186735 73737 0 None -53 4 Mouse 6.3 pKi = 6.3 Binding
Ability to inhibit the binding of [3H]-PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP2Ability to inhibit the binding of [3H]-PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP2
ChEMBL 429 8 1 5 4.7 Cc1cc2c(CC(=O)O)cccc2n1C(=O)c1ccc(OCCOc2ccccc2)cc1 10.1016/j.bmcl.2004.07.039
11155228 72880 0 None -1778 4 Human 5.3 pKi = 5.3 Binding
Binding affinity for human prostanoid EP2 receptorBinding affinity for human prostanoid EP2 receptor
ChEMBL 452 8 1 2 7.2 Cc1cccc(/C=C/Cc2ccccc2/C=C/C(=O)O)c1OCc1c(Cl)cccc1Cl 10.1016/j.bmcl.2004.11.051
CHEMBL183919 72880 0 None -1778 4 Human 5.3 pKi = 5.3 Binding
Binding affinity for human prostanoid EP2 receptorBinding affinity for human prostanoid EP2 receptor
ChEMBL 452 8 1 2 7.2 Cc1cccc(/C=C/Cc2ccccc2/C=C/C(=O)O)c1OCc1c(Cl)cccc1Cl 10.1016/j.bmcl.2004.11.051
44419347 89550 0 None -1778 4 Human 5.3 pKi = 5.3 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 452 8 1 2 7.2 Cc1ccc(OCc2c(Cl)cccc2Cl)c(/C=C/Cc2ccccc2/C=C/C(=O)O)c1 10.1016/j.bmcl.2006.08.025
CHEMBL217988 89550 0 None -1778 4 Human 5.3 pKi = 5.3 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 452 8 1 2 7.2 Cc1ccc(OCc2c(Cl)cccc2Cl)c(/C=C/Cc2ccccc2/C=C/C(=O)O)c1 10.1016/j.bmcl.2006.08.025
10298293 100942 0 None -426 2 Human 5.3 pKi = 5.3 Binding
Binding affinity at human prostaglandin EP2 receptorBinding affinity at human prostaglandin EP2 receptor
ChEMBL 460 9 2 4 3.1 O=C(O)c1ccc(CCN2C(=O)CCN2CCC(O)Cc2cccc(Br)c2)cc1 10.1016/j.bmcl.2007.09.074
CHEMBL249538 100942 0 None -426 2 Human 5.3 pKi = 5.3 Binding
Binding affinity at human prostaglandin EP2 receptorBinding affinity at human prostaglandin EP2 receptor
ChEMBL 460 9 2 4 3.1 O=C(O)c1ccc(CCN2C(=O)CCN2CCC(O)Cc2cccc(Br)c2)cc1 10.1016/j.bmcl.2007.09.074
52944193 23305 0 None -63 4 Human 6.3 pKi = 6.3 Binding
Binding affinity for human prostanoid EP2 receptorBinding affinity for human prostanoid EP2 receptor
ChEMBL 768 16 2 4 11.9 Cc1cccc(/C=C/Cc2ccccc2/C=C/C(=O)O)c1OCc1ccccc1.Cc1cccc(C/C=C/c2ccccc2/C=C/C(=O)O)c1OCc1ccccc1 10.1016/j.bmcl.2004.11.051
CHEMBL1237295 23305 0 None -63 4 Human 6.3 pKi = 6.3 Binding
Binding affinity for human prostanoid EP2 receptorBinding affinity for human prostanoid EP2 receptor
ChEMBL 768 16 2 4 11.9 Cc1cccc(/C=C/Cc2ccccc2/C=C/C(=O)O)c1OCc1ccccc1.Cc1cccc(C/C=C/c2ccccc2/C=C/C(=O)O)c1OCc1ccccc1 10.1016/j.bmcl.2004.11.051
21362905 178086 0 None -8 4 Human 5.3 pKi = 5.3 Binding
Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 428 8 1 3 6.9 CC(Cc1ccccc1-c1csc(-c2ccccc2OCc2ccccc2)c1)C(=O)O 10.1016/s0960-894x(03)00794-7
CHEMBL446098 178086 0 None -8 4 Human 5.3 pKi = 5.3 Binding
Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 428 8 1 3 6.9 CC(Cc1ccccc1-c1csc(-c2ccccc2OCc2ccccc2)c1)C(=O)O 10.1016/s0960-894x(03)00794-7
58932683 82062 0 None -354 3 Mouse 7.3 pKi = 7.3 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 549 10 2 8 5.2 Cc1ccc2nc(-c3cccc(C[C@H](O)/C=C/[C@H]4CCC(=O)N4CCSc4nc(C(=O)O)cs4)c3)oc2c1 10.1016/j.bmc.2012.04.008
CHEMBL2037289 82062 0 None -354 3 Mouse 7.3 pKi = 7.3 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 549 10 2 8 5.2 Cc1ccc2nc(-c3cccc(C[C@H](O)/C=C/[C@H]4CCC(=O)N4CCSc4nc(C(=O)O)cs4)c3)oc2c1 10.1016/j.bmc.2012.04.008
44444716 161616 0 None -12 2 Human 6.3 pKi = 6.3 Binding
Binding affinity at human prostaglandin EP2 receptorBinding affinity at human prostaglandin EP2 receptor
ChEMBL 484 12 1 3 5.4 CC(CCN1CCC(=O)N1CCc1ccc(C(=O)O)cc1)Cc1cccc(CCc2ccccc2)c1 10.1016/j.bmcl.2007.09.074
CHEMBL400447 161616 0 None -12 2 Human 6.3 pKi = 6.3 Binding
Binding affinity at human prostaglandin EP2 receptorBinding affinity at human prostaglandin EP2 receptor
ChEMBL 484 12 1 3 5.4 CC(CCN1CCC(=O)N1CCc1ccc(C(=O)O)cc1)Cc1cccc(CCc2ccccc2)c1 10.1016/j.bmcl.2007.09.074
10295421 100972 0 None -316 2 Human 5.3 pKi = 5.3 Binding
Binding affinity at human prostaglandin EP2 receptorBinding affinity at human prostaglandin EP2 receptor
ChEMBL 416 9 2 4 3.0 O=C(O)c1ccc(CCN2C(=O)CCN2CCC(O)Cc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2007.09.074
CHEMBL249744 100972 0 None -316 2 Human 5.3 pKi = 5.3 Binding
Binding affinity at human prostaglandin EP2 receptorBinding affinity at human prostaglandin EP2 receptor
ChEMBL 416 9 2 4 3.0 O=C(O)c1ccc(CCN2C(=O)CCN2CCC(O)Cc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2007.09.074
44234032 154703 0 None -81 6 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-PGE2 from recombinant human EP2 receptor expressed in HEK293 cell membranes incubated for 1 hrDisplacement of [3H]-PGE2 from recombinant human EP2 receptor expressed in HEK293 cell membranes incubated for 1 hr
ChEMBL 415 8 1 4 5.0 O=C(O)COC[C@H]1CC[C@H](COC(=O)N(c2ccccc2)c2cccc(F)c2)CC1 10.1021/acs.jmedchem.6b00871
CHEMBL3933704 154703 0 None -81 6 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-PGE2 from recombinant human EP2 receptor expressed in HEK293 cell membranes incubated for 1 hrDisplacement of [3H]-PGE2 from recombinant human EP2 receptor expressed in HEK293 cell membranes incubated for 1 hr
ChEMBL 415 8 1 4 5.0 O=C(O)COC[C@H]1CC[C@H](COC(=O)N(c2ccccc2)c2cccc(F)c2)CC1 10.1021/acs.jmedchem.6b00871
11165749 172738 0 None -20 3 Mouse 5.2 pKi = 5.2 Binding
Binding affinity for mouse Prostanoid EP2 receptorBinding affinity for mouse Prostanoid EP2 receptor
ChEMBL 409 9 1 5 4.8 CCCCOc1ccc(C(=O)n2c(C)c(CCC(=O)O)c3cc(OC)ccc32)cc1 10.1016/j.bmcl.2004.06.006
CHEMBL425167 172738 0 None -20 3 Mouse 5.2 pKi = 5.2 Binding
Binding affinity for mouse Prostanoid EP2 receptorBinding affinity for mouse Prostanoid EP2 receptor
ChEMBL 409 9 1 5 4.8 CCCCOc1ccc(C(=O)n2c(C)c(CCC(=O)O)c3cc(OC)ccc32)cc1 10.1016/j.bmcl.2004.06.006
44520990 206632 0 None -6 3 Mouse 5.2 pKi = 5.2 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 410 6 2 4 5.3 Cc1ccc(/C=C/C(=O)O)c(OCCC2(C)CCc3c(C)c(O)c(C)c(C)c3O2)c1 10.1016/j.bmc.2009.08.007
CHEMBL594423 206632 0 None -6 3 Mouse 5.2 pKi = 5.2 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 410 6 2 4 5.3 Cc1ccc(/C=C/C(=O)O)c(OCCC2(C)CCc3c(C)c(O)c(C)c(C)c3O2)c1 10.1016/j.bmc.2009.08.007
11855867 152761 0 None - 1 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 mins
ChEMBL 389 8 2 5 3.6 CCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3918349 152761 0 None - 1 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 mins
ChEMBL 389 8 2 5 3.6 CCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
11855867 152761 0 None - 1 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 389 8 2 5 3.6 CCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3918349 152761 0 None - 1 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 389 8 2 5 3.6 CCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
44304403 175876 0 None -16 4 Mouse 7.2 pKi = 7.2 Binding
Affinity for mouse Prostanoid EP2 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP2 receptor expressed in CHO cells
ChEMBL 420 12 3 4 3.8 COCc1cccc(C[C@H](O)/C=C/[C@H]2[C@H](O)C[C@@H](F)[C@@H]2C/C=C/CCCC(=O)O)c1 10.1016/s0960-894x(01)00365-1
CHEMBL439934 175876 0 None -16 4 Mouse 7.2 pKi = 7.2 Binding
Affinity for mouse Prostanoid EP2 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP2 receptor expressed in CHO cells
ChEMBL 420 12 3 4 3.8 COCc1cccc(C[C@H](O)/C=C/[C@H]2[C@H](O)C[C@@H](F)[C@@H]2C/C=C/CCCC(=O)O)c1 10.1016/s0960-894x(01)00365-1
44290314 180753 0 None -5754 3 Human 4.2 pKi = 4.2 Binding
Binding affinity was determined against prostanoid EP2 receptorBinding affinity was determined against prostanoid EP2 receptor
ChEMBL 403 10 2 4 3.9 O=C(O)CCCCCCN1C(=O)CC[C@@H]1/C=C/C(O)c1ccc(C(F)(F)F)o1 10.1016/j.bmcl.2004.01.063
CHEMBL45418 180753 0 None -5754 3 Human 4.2 pKi = 4.2 Binding
Binding affinity was determined against prostanoid EP2 receptorBinding affinity was determined against prostanoid EP2 receptor
ChEMBL 403 10 2 4 3.9 O=C(O)CCCCCCN1C(=O)CC[C@@H]1/C=C/C(O)c1ccc(C(F)(F)F)o1 10.1016/j.bmcl.2004.01.063
44320272 213041 0 None -1 4 Human 6.2 pKi = 6.2 Binding
Binding affinity at human Prostanoid EP2 receptor.Binding affinity at human Prostanoid EP2 receptor.
ChEMBL 507 10 1 5 5.9 O=C(Cc1ccccc1-c1ccc(CSCCc2ccccc2)cc1)NS(=O)(=O)c1cccs1 10.1016/s0960-894x(02)00518-8
CHEMBL86886 213041 0 None -1 4 Human 6.2 pKi = 6.2 Binding
Binding affinity at human Prostanoid EP2 receptor.Binding affinity at human Prostanoid EP2 receptor.
ChEMBL 507 10 1 5 5.9 O=C(Cc1ccccc1-c1ccc(CSCCc2ccccc2)cc1)NS(=O)(=O)c1cccs1 10.1016/s0960-894x(02)00518-8
24952929 9332 42 None -9332 5 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]PGE2 from human EP2 receptor expressed in HEK293-EBNA cells by scintillation countingDisplacement of [3H]PGE2 from human EP2 receptor expressed in HEK293-EBNA cells by scintillation counting
ChEMBL 473 6 2 3 6.1 OC(=O)c1ccc(cc1)C1(CC1)NC(=O)c1c(C)sc(c1Cc1ccc(cc1)C(F)(F)F)C 10.1021/jm901771h
4041 9332 42 None -9332 5 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]PGE2 from human EP2 receptor expressed in HEK293-EBNA cells by scintillation countingDisplacement of [3H]PGE2 from human EP2 receptor expressed in HEK293-EBNA cells by scintillation counting
ChEMBL 473 6 2 3 6.1 OC(=O)c1ccc(cc1)C1(CC1)NC(=O)c1c(C)sc(c1Cc1ccc(cc1)C(F)(F)F)C 10.1021/jm901771h
CHEMBL597997 9332 42 None -9332 5 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]PGE2 from human EP2 receptor expressed in HEK293-EBNA cells by scintillation countingDisplacement of [3H]PGE2 from human EP2 receptor expressed in HEK293-EBNA cells by scintillation counting
ChEMBL 473 6 2 3 6.1 OC(=O)c1ccc(cc1)C1(CC1)NC(=O)c1c(C)sc(c1Cc1ccc(cc1)C(F)(F)F)C 10.1021/jm901771h
10295336 208225 0 None -53 4 Mouse 5.2 pKi = 5.2 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 415 8 1 3 4.7 O=C(O)/C=C/c1ccc(CN2CCCC2=O)cc1OCCc1ccc2ccccc2c1 10.1016/j.bmc.2009.08.007
CHEMBL604897 208225 0 None -53 4 Mouse 5.2 pKi = 5.2 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 415 8 1 3 4.7 O=C(O)/C=C/c1ccc(CN2CCCC2=O)cc1OCCc1ccc2ccccc2c1 10.1016/j.bmc.2009.08.007
44290266 168487 0 None -8 4 Human 8.2 pKi = 8.2 Binding
Binding affinity was determined against prostanoid EP2 receptorBinding affinity was determined against prostanoid EP2 receptor
ChEMBL 353 12 3 4 2.3 CCCCC[C@H](O)/C=C/[C@H]1[C@H](O)CC(=O)N1C/C=C/CCCC(=O)O 10.1016/j.bmcl.2004.01.063
CHEMBL413509 168487 0 None -8 4 Human 8.2 pKi = 8.2 Binding
Binding affinity was determined against prostanoid EP2 receptorBinding affinity was determined against prostanoid EP2 receptor
ChEMBL 353 12 3 4 2.3 CCCCC[C@H](O)/C=C/[C@H]1[C@H](O)CC(=O)N1C/C=C/CCCC(=O)O 10.1016/j.bmcl.2004.01.063
44394380 132207 0 None -6 4 Mouse 7.2 pKi = 7.2 Binding
Ability to inhibit the binding of [3H]-PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP2Ability to inhibit the binding of [3H]-PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP2
ChEMBL 457 6 1 6 4.5 Cc1cc2c(CC(=O)O)cccc2n1C(=O)c1ccc(OC[C@@H]2COc3ccccc3O2)cc1 10.1016/j.bmcl.2004.07.039
CHEMBL364593 132207 0 None -6 4 Mouse 7.2 pKi = 7.2 Binding
Ability to inhibit the binding of [3H]-PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP2Ability to inhibit the binding of [3H]-PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP2
ChEMBL 457 6 1 6 4.5 Cc1cc2c(CC(=O)O)cccc2n1C(=O)c1ccc(OC[C@@H]2COc3ccccc3O2)cc1 10.1016/j.bmcl.2004.07.039
44442337 100782 0 None 1 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]PGE2 from human EP2 receptor expressed in HEK293 cellsDisplacement of [3H]PGE2 from human EP2 receptor expressed in HEK293 cells
ChEMBL 381 8 1 2 5.0 C/C(=C/C=C/[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1)CC1CCCC1 10.1016/j.bmcl.2007.05.025
CHEMBL248678 100782 0 None 1 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]PGE2 from human EP2 receptor expressed in HEK293 cellsDisplacement of [3H]PGE2 from human EP2 receptor expressed in HEK293 cells
ChEMBL 381 8 1 2 5.0 C/C(=C/C=C/[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1)CC1CCCC1 10.1016/j.bmcl.2007.05.025
44442331 101265 0 None -15 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]PGE2 from human EP2 receptor expressed in HEK293 cellsDisplacement of [3H]PGE2 from human EP2 receptor expressed in HEK293 cells
ChEMBL 355 9 1 2 4.6 CCCC/C(C)=C\C=C\[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.05.025
CHEMBL251505 101265 0 None -15 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]PGE2 from human EP2 receptor expressed in HEK293 cellsDisplacement of [3H]PGE2 from human EP2 receptor expressed in HEK293 cells
ChEMBL 355 9 1 2 4.6 CCCC/C(C)=C\C=C\[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.05.025
10278907 71192 0 None -138 3 Mouse 6.2 pKi = 6.2 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 504 6 1 6 5.2 Cc1c(CC(=O)O)c2ccccc2n1C(=O)c1ccc(OC[C@@H]2CN(C)c3ccccc3O2)cc1Cl 10.1016/j.bmc.2011.06.014
CHEMBL1813121 71192 0 None -138 3 Mouse 6.2 pKi = 6.2 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 504 6 1 6 5.2 Cc1c(CC(=O)O)c2ccccc2n1C(=O)c1ccc(OC[C@@H]2CN(C)c3ccccc3O2)cc1Cl 10.1016/j.bmc.2011.06.014
59465570 150037 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 392 13 2 2 6.6 CCCCCC(O)c1ccc([C@H]2CC[C@@H](F)[C@@H]2CCCCCCC(=O)O)cc1 nan
CHEMBL3896693 150037 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 392 13 2 2 6.6 CCCCCC(O)c1ccc([C@H]2CC[C@@H](F)[C@@H]2CCCCCCC(=O)O)cc1 nan
134147021 156803 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 414 13 2 3 6.9 CCCCCC(O)c1ccc([C@H]2CC[C@@H](Cl)[C@@H]2CCCCCCC(=O)O)s1 nan
CHEMBL3950412 156803 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 414 13 2 3 6.9 CCCCCC(O)c1ccc([C@H]2CC[C@@H](Cl)[C@@H]2CCCCCCC(=O)O)s1 nan
10204257 100944 0 None -104 2 Human 5.2 pKi = 5.2 Binding
Binding affinity at human prostaglandin EP2 receptorBinding affinity at human prostaglandin EP2 receptor
ChEMBL 450 9 2 4 3.4 O=C(O)c1ccc(CCN2C(=O)CCN2CCC(O)Cc2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2007.09.074
CHEMBL249540 100944 0 None -104 2 Human 5.2 pKi = 5.2 Binding
Binding affinity at human prostaglandin EP2 receptorBinding affinity at human prostaglandin EP2 receptor
ChEMBL 450 9 2 4 3.4 O=C(O)c1ccc(CCN2C(=O)CCN2CCC(O)Cc2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2007.09.074
44219292 119359 38 None -204 7 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-PGE2 from recombinant human EP2 receptor expressed in HEK293 cell membranes incubated for 1 hrDisplacement of [3H]-PGE2 from recombinant human EP2 receptor expressed in HEK293 cell membranes incubated for 1 hr
ChEMBL 431 8 1 4 5.5 O=C(O)COC[C@H]1CC[C@H](COC(=O)N(c2ccccc2)c2ccc(Cl)cc2)CC1 10.1021/acs.jmedchem.6b00871
CHEMBL3301604 119359 38 None -204 7 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-PGE2 from recombinant human EP2 receptor expressed in HEK293 cell membranes incubated for 1 hrDisplacement of [3H]-PGE2 from recombinant human EP2 receptor expressed in HEK293 cell membranes incubated for 1 hr
ChEMBL 431 8 1 4 5.5 O=C(O)COC[C@H]1CC[C@H](COC(=O)N(c2ccccc2)c2ccc(Cl)cc2)CC1 10.1021/acs.jmedchem.6b00871
CHEMBL3919269 119359 38 None -204 7 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-PGE2 from recombinant human EP2 receptor expressed in HEK293 cell membranes incubated for 1 hrDisplacement of [3H]-PGE2 from recombinant human EP2 receptor expressed in HEK293 cell membranes incubated for 1 hr
ChEMBL 431 8 1 4 5.5 O=C(O)COC[C@H]1CC[C@H](COC(=O)N(c2ccccc2)c2ccc(Cl)cc2)CC1 10.1021/acs.jmedchem.6b00871
DB12462 119359 38 None -204 7 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-PGE2 from recombinant human EP2 receptor expressed in HEK293 cell membranes incubated for 1 hrDisplacement of [3H]-PGE2 from recombinant human EP2 receptor expressed in HEK293 cell membranes incubated for 1 hr
ChEMBL 431 8 1 4 5.5 O=C(O)COC[C@H]1CC[C@H](COC(=O)N(c2ccccc2)c2ccc(Cl)cc2)CC1 10.1021/acs.jmedchem.6b00871
57400087 78077 0 None -2 2 Mouse 5.2 pKi = 5.2 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 413 8 2 3 4.0 O=C(O)CCc1cccc(N2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(Cl)c2)c1 10.1016/j.bmc.2012.02.018
CHEMBL1957431 78077 0 None -2 2 Mouse 5.2 pKi = 5.2 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 413 8 2 3 4.0 O=C(O)CCc1cccc(N2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(Cl)c2)c1 10.1016/j.bmc.2012.02.018
57893916 81930 0 None -1288 2 Mouse 5.2 pKi = 5.2 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 454 12 2 5 3.8 O=C(O)CCCSCCN1C(=O)CC[C@@H]1/C=C/[C@@H](O)Cc1cccc(-c2ccccn2)c1 10.1016/j.bmc.2012.04.008
CHEMBL2036309 81930 0 None -1288 2 Mouse 5.2 pKi = 5.2 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 454 12 2 5 3.8 O=C(O)CCCSCCN1C(=O)CC[C@@H]1/C=C/[C@@H](O)Cc1cccc(-c2ccccn2)c1 10.1016/j.bmc.2012.04.008
56672019 71588 0 None -7 4 Mouse 7.2 pKi = 7.2 Binding
Displacement of [3H]PGE2 from mouse prostaglandin EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]PGE2 from mouse prostaglandin EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 460 7 2 5 4.5 Cc1cc(CC(=O)O)cc(NC(=O)c2ccc(OC[C@@H]3CN(C)c4ccccc4O3)cc2C)c1 10.1016/j.bmc.2011.08.007
CHEMBL1819612 71588 0 None -7 4 Mouse 7.2 pKi = 7.2 Binding
Displacement of [3H]PGE2 from mouse prostaglandin EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]PGE2 from mouse prostaglandin EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 460 7 2 5 4.5 Cc1cc(CC(=O)O)cc(NC(=O)c2ccc(OC[C@@H]3CN(C)c4ccccc4O3)cc2C)c1 10.1016/j.bmc.2011.08.007
8541 9718 2 None -1548 4 Mouse 6.2 pKi = 6.2 Binding
Affinity for mouse Prostanoid EP2 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP2 receptor expressed in CHO cells
ChEMBL 436 13 3 6 2.8 COCc1cccc(c1)C[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCSCCCC(=O)O)O 10.1016/s0960-894x(01)00365-1
9824353 9718 2 None -1548 4 Mouse 6.2 pKi = 6.2 Binding
Affinity for mouse Prostanoid EP2 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP2 receptor expressed in CHO cells
ChEMBL 436 13 3 6 2.8 COCc1cccc(c1)C[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCSCCCC(=O)O)O 10.1016/s0960-894x(01)00365-1
CHEMBL292964 9718 2 None -1548 4 Mouse 6.2 pKi = 6.2 Binding
Affinity for mouse Prostanoid EP2 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP2 receptor expressed in CHO cells
ChEMBL 436 13 3 6 2.8 COCc1cccc(c1)C[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCSCCCC(=O)O)O 10.1016/s0960-894x(01)00365-1
8541 9718 2 None -1548 4 Mouse 6.2 pKi = 6.2 Binding
Binding affinity to mouse EP2 receptor by competitive binding assayBinding affinity to mouse EP2 receptor by competitive binding assay
ChEMBL 436 13 3 6 2.8 COCc1cccc(c1)C[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCSCCCC(=O)O)O 10.1021/jm9018756
9824353 9718 2 None -1548 4 Mouse 6.2 pKi = 6.2 Binding
Binding affinity to mouse EP2 receptor by competitive binding assayBinding affinity to mouse EP2 receptor by competitive binding assay
ChEMBL 436 13 3 6 2.8 COCc1cccc(c1)C[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCSCCCC(=O)O)O 10.1021/jm9018756
CHEMBL292964 9718 2 None -1548 4 Mouse 6.2 pKi = 6.2 Binding
Binding affinity to mouse EP2 receptor by competitive binding assayBinding affinity to mouse EP2 receptor by competitive binding assay
ChEMBL 436 13 3 6 2.8 COCc1cccc(c1)C[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCSCCCC(=O)O)O 10.1021/jm9018756
8541 9718 2 None -1548 4 Mouse 6.2 pKi = 6.2 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counterDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counter
ChEMBL 436 13 3 6 2.8 COCc1cccc(c1)C[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCSCCCC(=O)O)O 10.1016/j.bmc.2011.12.009
9824353 9718 2 None -1548 4 Mouse 6.2 pKi = 6.2 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counterDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counter
ChEMBL 436 13 3 6 2.8 COCc1cccc(c1)C[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCSCCCC(=O)O)O 10.1016/j.bmc.2011.12.009
CHEMBL292964 9718 2 None -1548 4 Mouse 6.2 pKi = 6.2 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counterDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counter
ChEMBL 436 13 3 6 2.8 COCc1cccc(c1)C[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCSCCCC(=O)O)O 10.1016/j.bmc.2011.12.009
10221497 100914 0 None -91 2 Human 5.2 pKi = 5.2 Binding
Binding affinity at human prostaglandin EP2 receptorBinding affinity at human prostaglandin EP2 receptor
ChEMBL 382 9 2 4 2.4 O=C(O)c1ccc(CCN2C(=O)CCN2CCC(O)Cc2ccccc2)cc1 10.1016/j.bmcl.2007.09.074
CHEMBL249342 100914 0 None -91 2 Human 5.2 pKi = 5.2 Binding
Binding affinity at human prostaglandin EP2 receptorBinding affinity at human prostaglandin EP2 receptor
ChEMBL 382 9 2 4 2.4 O=C(O)c1ccc(CCN2C(=O)CCN2CCC(O)Cc2ccccc2)cc1 10.1016/j.bmcl.2007.09.074
10272306 161615 0 None -173 2 Human 5.2 pKi = 5.2 Binding
Binding affinity at human prostaglandin EP2 receptorBinding affinity at human prostaglandin EP2 receptor
ChEMBL 400 9 2 4 2.5 O=C(O)c1ccc(CCN2C(=O)CCN2CCC(O)Cc2cccc(F)c2)cc1 10.1016/j.bmcl.2007.09.074
CHEMBL400446 161615 0 None -173 2 Human 5.2 pKi = 5.2 Binding
Binding affinity at human prostaglandin EP2 receptorBinding affinity at human prostaglandin EP2 receptor
ChEMBL 400 9 2 4 2.5 O=C(O)c1ccc(CCN2C(=O)CCN2CCC(O)Cc2cccc(F)c2)cc1 10.1016/j.bmcl.2007.09.074
71452690 85400 0 None 15 4 Human 7.2 pKi = 7.2 Binding
Binding affinity at human Prostanoid EP2 receptor.Binding affinity at human Prostanoid EP2 receptor.
ChEMBL 400 9 1 4 5.1 c1ccc(CCSCc2ccc(-c3ccccc3CCc3nnn[nH]3)cc2)cc1 10.1016/s0960-894x(02)00518-8
CHEMBL2112332 85400 0 None 15 4 Human 7.2 pKi = 7.2 Binding
Binding affinity at human Prostanoid EP2 receptor.Binding affinity at human Prostanoid EP2 receptor.
ChEMBL 400 9 1 4 5.1 c1ccc(CCSCc2ccc(-c3ccccc3CCc3nnn[nH]3)cc2)cc1 10.1016/s0960-894x(02)00518-8
52950151 23309 0 None 3 4 Human 6.2 pKi = 6.2 Binding
Binding affinity for human prostanoid EP2 receptorBinding affinity for human prostanoid EP2 receptor
ChEMBL 768 16 2 4 11.9 Cc1cccc(/C=C/Cc2cccc(/C=C/C(=O)O)c2)c1OCc1ccccc1.Cc1cccc(C/C=C/c2cccc(/C=C/C(=O)O)c2)c1OCc1ccccc1 10.1016/j.bmcl.2004.11.051
CHEMBL1237299 23309 0 None 3 4 Human 6.2 pKi = 6.2 Binding
Binding affinity for human prostanoid EP2 receptorBinding affinity for human prostanoid EP2 receptor
ChEMBL 768 16 2 4 11.9 Cc1cccc(/C=C/Cc2cccc(/C=C/C(=O)O)c2)c1OCc1ccccc1.Cc1cccc(C/C=C/c2cccc(/C=C/C(=O)O)c2)c1OCc1ccccc1 10.1016/j.bmcl.2004.11.051
22008967 89924 0 None -2691 4 Human 5.2 pKi = 5.2 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 439 8 1 5 4.5 COc1ccc(/C=C/Cc2ccccc2/C=C/C(=O)NS(=O)(=O)c2cccs2)cc1 10.1016/j.bmcl.2006.08.025
CHEMBL218228 89924 0 None -2691 4 Human 5.2 pKi = 5.2 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 439 8 1 5 4.5 COc1ccc(/C=C/Cc2ccccc2/C=C/C(=O)NS(=O)(=O)c2cccs2)cc1 10.1016/j.bmcl.2006.08.025
22008966 89925 0 None -2691 4 Human 5.2 pKi = 5.2 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 439 8 1 5 4.5 COc1ccc(C/C=C/c2ccccc2/C=C/C(=O)NS(=O)(=O)c2cccs2)cc1 10.1016/j.bmcl.2006.08.025
CHEMBL218229 89925 0 None -2691 4 Human 5.2 pKi = 5.2 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 439 8 1 5 4.5 COc1ccc(C/C=C/c2ccccc2/C=C/C(=O)NS(=O)(=O)c2cccs2)cc1 10.1016/j.bmcl.2006.08.025
13230981 41841 0 None -1122 3 Human 5.2 pKi = 5.2 Binding
Binding affinity towards EP2 receptor expressed in HEK293 ebna cells recombinantly expressing the corresponding human prostanoid cDNAsBinding affinity towards EP2 receptor expressed in HEK293 ebna cells recombinantly expressing the corresponding human prostanoid cDNAs
ChEMBL 339 13 2 3 3.5 CCCCCC(O)/C=C/[C@H]1CCC(=O)N1CCCCCCC(=O)O 10.1016/s0960-894x(03)00042-8
CHEMBL14334 41841 0 None -1122 3 Human 5.2 pKi = 5.2 Binding
Binding affinity towards EP2 receptor expressed in HEK293 ebna cells recombinantly expressing the corresponding human prostanoid cDNAsBinding affinity towards EP2 receptor expressed in HEK293 ebna cells recombinantly expressing the corresponding human prostanoid cDNAs
ChEMBL 339 13 2 3 3.5 CCCCCC(O)/C=C/[C@H]1CCC(=O)N1CCCCCCC(=O)O 10.1016/s0960-894x(03)00042-8
10348006 82065 0 None -338 3 Mouse 7.2 pKi = 7.2 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 569 10 2 8 5.5 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(-c3nc4cc(Cl)ccc4o3)c2)n1 10.1016/j.bmc.2012.04.008
CHEMBL2037292 82065 0 None -338 3 Mouse 7.2 pKi = 7.2 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 569 10 2 8 5.5 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(-c3nc4cc(Cl)ccc4o3)c2)n1 10.1016/j.bmc.2012.04.008
52943000 23307 0 None -26 4 Human 6.2 pKi = 6.2 Binding
Binding affinity for human prostanoid EP2 receptorBinding affinity for human prostanoid EP2 receptor
ChEMBL 740 16 2 4 11.2 O=C(O)/C=C/c1ccccc1/C=C/Cc1ccccc1OCc1ccccc1.O=C(O)/C=C/c1ccccc1C/C=C\c1ccccc1OCc1ccccc1 10.1016/j.bmcl.2004.11.051
CHEMBL1237297 23307 0 None -26 4 Human 6.2 pKi = 6.2 Binding
Binding affinity for human prostanoid EP2 receptorBinding affinity for human prostanoid EP2 receptor
ChEMBL 740 16 2 4 11.2 O=C(O)/C=C/c1ccccc1/C=C/Cc1ccccc1OCc1ccccc1.O=C(O)/C=C/c1ccccc1C/C=C\c1ccccc1OCc1ccccc1 10.1016/j.bmcl.2004.11.051
10319835 76142 0 None -16982 3 Mouse 5.2 pKi = 5.2 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counterDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counter
ChEMBL 417 13 2 3 4.9 CCCc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=S)N2CCCCCCC(=O)O)c1 10.1016/j.bmc.2011.12.009
CHEMBL1929547 76142 0 None -16982 3 Mouse 5.2 pKi = 5.2 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counterDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counter
ChEMBL 417 13 2 3 4.9 CCCc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=S)N2CCCCCCC(=O)O)c1 10.1016/j.bmc.2011.12.009
44520991 206481 0 None -7 2 Mouse 5.2 pKi = 5.2 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 426 7 2 5 5.0 COc1ccc(/C=C/C(=O)O)c(OCCC2(C)CCc3c(C)c(O)c(C)c(C)c3O2)c1 10.1016/j.bmc.2009.08.007
CHEMBL593260 206481 0 None -7 2 Mouse 5.2 pKi = 5.2 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 426 7 2 5 5.0 COc1ccc(/C=C/C(=O)O)c(OCCC2(C)CCc3c(C)c(O)c(C)c(C)c3O2)c1 10.1016/j.bmc.2009.08.007
44289977 169538 0 None -478 2 Human 4.2 pKi = 4.2 Binding
Binding affinity was determined against prostanoid EP2 receptorBinding affinity was determined against prostanoid EP2 receptor
ChEMBL 413 10 2 3 4.3 O=C(O)CCCCCCN1C(=O)CC[C@@H]1/C=C/C(O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2004.01.063
CHEMBL417171 169538 0 None -478 2 Human 4.2 pKi = 4.2 Binding
Binding affinity was determined against prostanoid EP2 receptorBinding affinity was determined against prostanoid EP2 receptor
ChEMBL 413 10 2 3 4.3 O=C(O)CCCCCCN1C(=O)CC[C@@H]1/C=C/C(O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2004.01.063
12003887 78074 0 None -776 2 Mouse 5.2 pKi = 5.2 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 411 11 2 4 3.4 O=C(O)CCCSCCN1C(=O)CC[C@@H]1/C=C/[C@@H](O)Cc1cccc(Cl)c1 10.1016/j.bmc.2012.02.018
CHEMBL1957308 78074 0 None -776 2 Mouse 5.2 pKi = 5.2 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 411 11 2 4 3.4 O=C(O)CCCSCCN1C(=O)CC[C@@H]1/C=C/[C@@H](O)Cc1cccc(Cl)c1 10.1016/j.bmc.2012.02.018
67078970 135977 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: Measurement of EP2 receptor binding affinity was carried out according to the method of Abramovitz et al. (Biochimica et Biophysica Acta, 1483, 285 (2000)). A test compound dissolved in dimethylsulfoxide and [3H]PGE2 (NET-428, available from PerkinElmer Inc.) (final concentration: 10 nM) were added to a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2, 1 mM EDTA) in which 10 μg of a membrane fraction (ES-562-M, available from Euroscreen S.A.) of HEK293 cells expressing human EP2 receptor had been suspended, followed by incubation at 30° C. for 60 minutes. The membrane fraction was recovered on glass fiber filter paper (GF/B, available from Whatman PLC) using a cell harvester (M30R, available from Brandel Inc.), and after washing with a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2), radioactivity was measured with a liquid scintillation analyzer (2000CA, available from Packard).Binding Assay: Measurement of EP2 receptor binding affinity was carried out according to the method of Abramovitz et al. (Biochimica et Biophysica Acta, 1483, 285 (2000)). A test compound dissolved in dimethylsulfoxide and [3H]PGE2 (NET-428, available from PerkinElmer Inc.) (final concentration: 10 nM) were added to a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2, 1 mM EDTA) in which 10 μg of a membrane fraction (ES-562-M, available from Euroscreen S.A.) of HEK293 cells expressing human EP2 receptor had been suspended, followed by incubation at 30° C. for 60 minutes. The membrane fraction was recovered on glass fiber filter paper (GF/B, available from Whatman PLC) using a cell harvester (M30R, available from Brandel Inc.), and after washing with a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2), radioactivity was measured with a liquid scintillation analyzer (2000CA, available from Packard).
ChEMBL 416 6 3 5 4.4 COC(=O)c1ccc(CNC(=O)c2[nH]c(-c3ccoc3)cc2-c2ccc(O)cc2)cc1 nan
CHEMBL3670655 135977 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: Measurement of EP2 receptor binding affinity was carried out according to the method of Abramovitz et al. (Biochimica et Biophysica Acta, 1483, 285 (2000)). A test compound dissolved in dimethylsulfoxide and [3H]PGE2 (NET-428, available from PerkinElmer Inc.) (final concentration: 10 nM) were added to a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2, 1 mM EDTA) in which 10 μg of a membrane fraction (ES-562-M, available from Euroscreen S.A.) of HEK293 cells expressing human EP2 receptor had been suspended, followed by incubation at 30° C. for 60 minutes. The membrane fraction was recovered on glass fiber filter paper (GF/B, available from Whatman PLC) using a cell harvester (M30R, available from Brandel Inc.), and after washing with a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2), radioactivity was measured with a liquid scintillation analyzer (2000CA, available from Packard).Binding Assay: Measurement of EP2 receptor binding affinity was carried out according to the method of Abramovitz et al. (Biochimica et Biophysica Acta, 1483, 285 (2000)). A test compound dissolved in dimethylsulfoxide and [3H]PGE2 (NET-428, available from PerkinElmer Inc.) (final concentration: 10 nM) were added to a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2, 1 mM EDTA) in which 10 μg of a membrane fraction (ES-562-M, available from Euroscreen S.A.) of HEK293 cells expressing human EP2 receptor had been suspended, followed by incubation at 30° C. for 60 minutes. The membrane fraction was recovered on glass fiber filter paper (GF/B, available from Whatman PLC) using a cell harvester (M30R, available from Brandel Inc.), and after washing with a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2), radioactivity was measured with a liquid scintillation analyzer (2000CA, available from Packard).
ChEMBL 416 6 3 5 4.4 COC(=O)c1ccc(CNC(=O)c2[nH]c(-c3ccoc3)cc2-c2ccc(O)cc2)cc1 nan
25114442 9835 56 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to human EP2 receptor expressed in CHO cells assessed as inhibition constantBinding affinity to human EP2 receptor expressed in CHO cells assessed as inhibition constant
ChEMBL 409 6 1 4 3.6 COc1ccc2c(c1)ccc(c2)OCC1(CN(C1)C(=O)c1ccc(cc1)F)C(=O)O 10.1021/acs.jmedchem.1c00816
5817 9835 56 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to human EP2 receptor expressed in CHO cells assessed as inhibition constantBinding affinity to human EP2 receptor expressed in CHO cells assessed as inhibition constant
ChEMBL 409 6 1 4 3.6 COc1ccc2c(c1)ccc(c2)OCC1(CN(C1)C(=O)c1ccc(cc1)F)C(=O)O 10.1021/acs.jmedchem.1c00816
CHEMBL3286797 9835 56 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to human EP2 receptor expressed in CHO cells assessed as inhibition constantBinding affinity to human EP2 receptor expressed in CHO cells assessed as inhibition constant
ChEMBL 409 6 1 4 3.6 COc1ccc2c(c1)ccc(c2)OCC1(CN(C1)C(=O)c1ccc(cc1)F)C(=O)O 10.1021/acs.jmedchem.1c00816
DB12024 9835 56 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to human EP2 receptor expressed in CHO cells assessed as inhibition constantBinding affinity to human EP2 receptor expressed in CHO cells assessed as inhibition constant
ChEMBL 409 6 1 4 3.6 COc1ccc2c(c1)ccc(c2)OCC1(CN(C1)C(=O)c1ccc(cc1)F)C(=O)O 10.1021/acs.jmedchem.1c00816
59465571 153063 0 None 21 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 386 12 2 3 5.6 CCCCCC(O)c1ccc([C@H]2CCC(=O)[C@@H]2C/C=C\CCCC(=O)O)cc1 nan
CHEMBL3920796 153063 0 None 21 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 386 12 2 3 5.6 CCCCCC(O)c1ccc([C@H]2CCC(=O)[C@@H]2C/C=C\CCCC(=O)O)cc1 nan
59465600 158477 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 388 13 2 3 5.3 CCCCC(O)Cc1ccc([C@H]2CCC(=O)[C@@H]2CCCCCCC(=O)O)cc1 nan
CHEMBL3964261 158477 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 388 13 2 3 5.3 CCCCC(O)Cc1ccc([C@H]2CCC(=O)[C@@H]2CCCCCCC(=O)O)cc1 nan
21362845 113680 0 None -630 4 Human 4.2 pKi = 4.2 Binding
Binding affinity at human Prostanoid EP2 receptor.Binding affinity at human Prostanoid EP2 receptor.
ChEMBL 556 7 1 5 7.3 O=C(/C=C/c1ccccc1-c1cccc(/C=C/c2ccc3ccc(Cl)cc3n2)c1)NS(=O)(=O)c1cccs1 10.1016/s0960-894x(02)00518-8
CHEMBL314616 113680 0 None -630 4 Human 4.2 pKi = 4.2 Binding
Binding affinity at human Prostanoid EP2 receptor.Binding affinity at human Prostanoid EP2 receptor.
ChEMBL 556 7 1 5 7.3 O=C(/C=C/c1ccccc1-c1cccc(/C=C/c2ccc3ccc(Cl)cc3n2)c1)NS(=O)(=O)c1cccs1 10.1016/s0960-894x(02)00518-8
52943002 23311 0 None -2 4 Human 5.2 pKi = 5.2 Binding
Binding affinity for human prostanoid EP2 receptorBinding affinity for human prostanoid EP2 receptor
ChEMBL 716 14 2 4 11.1 Cc1cccc(/C=C\Cc2ccccc2C(=O)O)c1OCc1ccccc1.Cc1cccc(C/C=C/c2ccccc2C(=O)O)c1OCc1ccccc1 10.1016/j.bmcl.2004.11.051
CHEMBL1237301 23311 0 None -2 4 Human 5.2 pKi = 5.2 Binding
Binding affinity for human prostanoid EP2 receptorBinding affinity for human prostanoid EP2 receptor
ChEMBL 716 14 2 4 11.1 Cc1cccc(/C=C\Cc2ccccc2C(=O)O)c1OCc1ccccc1.Cc1cccc(C/C=C/c2ccccc2C(=O)O)c1OCc1ccccc1 10.1016/j.bmcl.2004.11.051
67245477 151661 0 None - 1 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 428 13 1 4 7.0 CCCCCC(O)c1ccc([C@H]2CC[C@@H](Cl)[C@@H]2CCCCCCC(=O)OC)s1 nan
CHEMBL3909989 151661 0 None - 1 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 428 13 1 4 7.0 CCCCCC(O)c1ccc([C@H]2CC[C@@H](Cl)[C@@H]2CCCCCCC(=O)OC)s1 nan
44289921 171150 0 None -9332 3 Human 4.2 pKi = 4.2 Binding
Binding affinity was determined against prostanoid EP2 receptorBinding affinity was determined against prostanoid EP2 receptor
ChEMBL 365 11 2 3 3.9 O=C(O)CCCCCCN1C(=O)CC[C@@H]1/C=C/[C@@H](O)CC1CCCCC1 10.1016/j.bmcl.2004.01.063
CHEMBL42129 171150 0 None -9332 3 Human 4.2 pKi = 4.2 Binding
Binding affinity was determined against prostanoid EP2 receptorBinding affinity was determined against prostanoid EP2 receptor
ChEMBL 365 11 2 3 3.9 O=C(O)CCCCCCN1C(=O)CC[C@@H]1/C=C/[C@@H](O)CC1CCCCC1 10.1016/j.bmcl.2004.01.063
57893891 81934 0 None -1995 2 Mouse 6.1 pKi = 6.1 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 510 12 2 6 5.0 O=C(O)CCCSCCN1C(=O)CC[C@@H]1/C=C/[C@@H](O)Cc1cccc(-c2nc3ccccc3s2)c1 10.1016/j.bmc.2012.04.008
CHEMBL2036313 81934 0 None -1995 2 Mouse 6.1 pKi = 6.1 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 510 12 2 6 5.0 O=C(O)CCCSCCN1C(=O)CC[C@@H]1/C=C/[C@@H](O)Cc1cccc(-c2nc3ccccc3s2)c1 10.1016/j.bmc.2012.04.008
24952929 9332 42 None -11481 5 Rat 5.1 pKi = 5.1 Binding
Displacement of [3H]PGE2 from rat EP2 receptor expressed in HEK293-EBNA cells by scintillation countingDisplacement of [3H]PGE2 from rat EP2 receptor expressed in HEK293-EBNA cells by scintillation counting
ChEMBL 473 6 2 3 6.1 OC(=O)c1ccc(cc1)C1(CC1)NC(=O)c1c(C)sc(c1Cc1ccc(cc1)C(F)(F)F)C 10.1021/jm901771h
4041 9332 42 None -11481 5 Rat 5.1 pKi = 5.1 Binding
Displacement of [3H]PGE2 from rat EP2 receptor expressed in HEK293-EBNA cells by scintillation countingDisplacement of [3H]PGE2 from rat EP2 receptor expressed in HEK293-EBNA cells by scintillation counting
ChEMBL 473 6 2 3 6.1 OC(=O)c1ccc(cc1)C1(CC1)NC(=O)c1c(C)sc(c1Cc1ccc(cc1)C(F)(F)F)C 10.1021/jm901771h
CHEMBL597997 9332 42 None -11481 5 Rat 5.1 pKi = 5.1 Binding
Displacement of [3H]PGE2 from rat EP2 receptor expressed in HEK293-EBNA cells by scintillation countingDisplacement of [3H]PGE2 from rat EP2 receptor expressed in HEK293-EBNA cells by scintillation counting
ChEMBL 473 6 2 3 6.1 OC(=O)c1ccc(cc1)C1(CC1)NC(=O)c1c(C)sc(c1Cc1ccc(cc1)C(F)(F)F)C 10.1021/jm901771h
1892 7534 20 None -2 9 Human 7.1 pKi = 7.1 Binding
Binding affinity to EP2 receptor (unknown origin) by competitive binding assayBinding affinity to EP2 receptor (unknown origin) by competitive binding assay
ChEMBL 394 13 3 4 4.3 CCCC1(CCC1)[C@H](C/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 10.1021/jm401431x
25886893 7534 20 None -2 9 Human 7.1 pKi = 7.1 Binding
Binding affinity to EP2 receptor (unknown origin) by competitive binding assayBinding affinity to EP2 receptor (unknown origin) by competitive binding assay
ChEMBL 394 13 3 4 4.3 CCCC1(CCC1)[C@H](C/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 10.1021/jm401431x
CHEMBL1628262 7534 20 None -2 9 Human 7.1 pKi = 7.1 Binding
Binding affinity to EP2 receptor (unknown origin) by competitive binding assayBinding affinity to EP2 receptor (unknown origin) by competitive binding assay
ChEMBL 394 13 3 4 4.3 CCCC1(CCC1)[C@H](C/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 10.1021/jm401431x
44304181 210052 0 None 12 2 Mouse 7.1 pKi = 7.1 Binding
Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.
ChEMBL 394 13 3 4 4.3 CCCC1([C@@H](O)C/C=C/C2[C@H](O)CC(=O)[C@@H]2CCCCCCC(=O)O)CCC1 10.1016/s0960-894x(01)00359-6
CHEMBL64663 210052 0 None 12 2 Mouse 7.1 pKi = 7.1 Binding
Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.
ChEMBL 394 13 3 4 4.3 CCCC1([C@@H](O)C/C=C/C2[C@H](O)CC(=O)[C@@H]2CCCCCCC(=O)O)CCC1 10.1016/s0960-894x(01)00359-6
9965922 70651 0 None -724 4 Human 5.1 pKi = 5.1 Binding
Binding affinity for human prostanoid EP2 receptorBinding affinity for human prostanoid EP2 receptor
ChEMBL 294 5 2 2 4.1 Cc1cccc(/C=C/Cc2ccccc2/C=C/C(=O)O)c1O 10.1016/j.bmcl.2004.11.051
CHEMBL180389 70651 0 None -724 4 Human 5.1 pKi = 5.1 Binding
Binding affinity for human prostanoid EP2 receptorBinding affinity for human prostanoid EP2 receptor
ChEMBL 294 5 2 2 4.1 Cc1cccc(/C=C/Cc2ccccc2/C=C/C(=O)O)c1O 10.1016/j.bmcl.2004.11.051
24765153 191308 0 None -11481 8 Human 5.1 pKi = 5.1 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 434 5 1 4 6.6 CC(C)c1nccc2c1c(Sc1ccc(Cl)c(Cl)c1)c1n2CC[C@H]1CC(=O)O 10.1016/j.bmcl.2009.03.010
CHEMBL484778 191308 0 None -11481 8 Human 5.1 pKi = 5.1 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 434 5 1 4 6.6 CC(C)c1nccc2c1c(Sc1ccc(Cl)c(Cl)c1)c1n2CC[C@H]1CC(=O)O 10.1016/j.bmcl.2009.03.010
9910141 107652 0 None -1513 3 Mouse 5.1 pKi = 5.1 Binding
Affinity for mouse Prostanoid EP2 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP2 receptor expressed in CHO cells
ChEMBL 422 11 4 6 2.7 Cc1cc(C[C@H](O)/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2CCSCCCC(=O)O)ccc1O 10.1016/s0960-894x(01)00365-1
CHEMBL293647 107652 0 None -1513 3 Mouse 5.1 pKi = 5.1 Binding
Affinity for mouse Prostanoid EP2 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP2 receptor expressed in CHO cells
ChEMBL 422 11 4 6 2.7 Cc1cc(C[C@H](O)/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2CCSCCCC(=O)O)ccc1O 10.1016/s0960-894x(01)00365-1
118517485 149528 0 None -50 2 Human 6.1 pKi = 6.1 Binding
Radioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations wRadioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations w
ChEMBL 396 8 2 3 4.2 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2ccc(F)cc2)cc1 nan
CHEMBL3892492 149528 0 None -50 2 Human 6.1 pKi = 6.1 Binding
Radioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations wRadioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations w
ChEMBL 396 8 2 3 4.2 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2ccc(F)cc2)cc1 nan
24952580 207341 0 None -575 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]PGE2 from human EP2 receptor expressed in HEK293-EBNA cells by scintillation countingDisplacement of [3H]PGE2 from human EP2 receptor expressed in HEK293-EBNA cells by scintillation counting
ChEMBL 467 6 2 3 6.5 C[C@H](NC(=O)c1c(Cl)sc(Cl)c1Cc1cccc(Cl)c1)c1ccc(C(=O)O)cc1 10.1021/jm901771h
CHEMBL599052 207341 0 None -575 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]PGE2 from human EP2 receptor expressed in HEK293-EBNA cells by scintillation countingDisplacement of [3H]PGE2 from human EP2 receptor expressed in HEK293-EBNA cells by scintillation counting
ChEMBL 467 6 2 3 6.5 C[C@H](NC(=O)c1c(Cl)sc(Cl)c1Cc1cccc(Cl)c1)c1ccc(C(=O)O)cc1 10.1021/jm901771h
10452108 100783 0 None -25 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]PGE2 from human EP2 receptor expressed in HEK293 cellsDisplacement of [3H]PGE2 from human EP2 receptor expressed in HEK293 cells
ChEMBL 375 7 1 2 4.6 C/C(=C\C=C\[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1)c1ccccc1 10.1016/j.bmcl.2007.05.025
CHEMBL248679 100783 0 None -25 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]PGE2 from human EP2 receptor expressed in HEK293 cellsDisplacement of [3H]PGE2 from human EP2 receptor expressed in HEK293 cells
ChEMBL 375 7 1 2 4.6 C/C(=C\C=C\[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1)c1ccccc1 10.1016/j.bmcl.2007.05.025
44304388 209931 0 None -151 5 Mouse 7.1 pKi = 7.1 Binding
Affinity for mouse Prostanoid EP2 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP2 receptor expressed in CHO cells
ChEMBL 372 13 3 5 3.0 CCCCC[C@H](O)/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCSCCCC(=O)O 10.1016/s0960-894x(01)00365-1
CHEMBL64187 209931 0 None -151 5 Mouse 7.1 pKi = 7.1 Binding
Affinity for mouse Prostanoid EP2 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP2 receptor expressed in CHO cells
ChEMBL 372 13 3 5 3.0 CCCCC[C@H](O)/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCSCCCC(=O)O 10.1016/s0960-894x(01)00365-1
11440167 91493 0 None -75 3 Human 7.1 pKi = 7.1 Binding
Binding affinity to human EP2 receptorBinding affinity to human EP2 receptor
ChEMBL 371 9 2 3 3.4 O=C(O)c1ccc(CCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)CCC2CCC2)cc1 10.1021/jm049290a
CHEMBL222782 91493 0 None -75 3 Human 7.1 pKi = 7.1 Binding
Binding affinity to human EP2 receptorBinding affinity to human EP2 receptor
ChEMBL 371 9 2 3 3.4 O=C(O)c1ccc(CCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)CCC2CCC2)cc1 10.1021/jm049290a
44444722 101031 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity at human prostaglandin EP2 receptorBinding affinity at human prostaglandin EP2 receptor
ChEMBL 402 11 2 4 3.5 CCCC1(C(O)CCCN2CCC(=O)N2CCc2ccc(C(=O)O)cc2)CCC1 10.1016/j.bmcl.2007.09.074
CHEMBL250153 101031 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity at human prostaglandin EP2 receptorBinding affinity at human prostaglandin EP2 receptor
ChEMBL 402 11 2 4 3.5 CCCC1(C(O)CCCN2CCC(=O)N2CCc2ccc(C(=O)O)cc2)CCC1 10.1016/j.bmcl.2007.09.074
52945294 23319 0 None -95 3 Human 6.1 pKi = 6.1 Binding
Binding affinity for human prostanoid EP2 receptorBinding affinity for human prostanoid EP2 receptor
ChEMBL 800 18 2 6 11.3 COc1cc(/C=C\Cc2ccccc2/C=C/C(=O)O)ccc1OCc1ccccc1.COc1cc(C/C=C/c2ccccc2/C=C/C(=O)O)ccc1OCc1ccccc1 10.1016/j.bmcl.2004.11.051
CHEMBL1237317 23319 0 None -95 3 Human 6.1 pKi = 6.1 Binding
Binding affinity for human prostanoid EP2 receptorBinding affinity for human prostanoid EP2 receptor
ChEMBL 800 18 2 6 11.3 COc1cc(/C=C\Cc2ccccc2/C=C/C(=O)O)ccc1OCc1ccccc1.COc1cc(C/C=C/c2ccccc2/C=C/C(=O)O)ccc1OCc1ccccc1 10.1016/j.bmcl.2004.11.051
52945294 23319 0 None -95 3 Human 6.1 pKi = 6.1 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 800 18 2 6 11.3 COc1cc(/C=C\Cc2ccccc2/C=C/C(=O)O)ccc1OCc1ccccc1.COc1cc(C/C=C/c2ccccc2/C=C/C(=O)O)ccc1OCc1ccccc1 10.1016/j.bmcl.2006.08.025
CHEMBL1237317 23319 0 None -95 3 Human 6.1 pKi = 6.1 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 800 18 2 6 11.3 COc1cc(/C=C\Cc2ccccc2/C=C/C(=O)O)ccc1OCc1ccccc1.COc1cc(C/C=C/c2ccccc2/C=C/C(=O)O)ccc1OCc1ccccc1 10.1016/j.bmcl.2006.08.025
10111602 90003 0 None -95 3 Human 6.1 pKi = 6.1 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 400 9 1 3 5.6 COc1cc(/C=C/Cc2ccccc2/C=C/C(=O)O)ccc1OCc1ccccc1 10.1016/j.bmcl.2006.08.025
CHEMBL218626 90003 0 None -95 3 Human 6.1 pKi = 6.1 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 400 9 1 3 5.6 COc1cc(/C=C/Cc2ccccc2/C=C/C(=O)O)ccc1OCc1ccccc1 10.1016/j.bmcl.2006.08.025
22990263 23565 0 None -4 3 Human 5.1 pKi = 5.1 Binding
Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 292 3 1 1 4.8 O=C(O)/C=C/c1ccccc1-c1ccc(Cl)c(Cl)c1 10.1016/s0960-894x(03)00794-7
CHEMBL124574 23565 0 None -4 3 Human 5.1 pKi = 5.1 Binding
Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 292 3 1 1 4.8 O=C(O)/C=C/c1ccccc1-c1ccc(Cl)c(Cl)c1 10.1016/s0960-894x(03)00794-7
10410111 109618 0 None -398 3 Mouse 6.1 pKi = 6.1 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptor
ChEMBL 424 11 3 6 2.7 Cc1cccc(C[C@H](O)/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2SCCCSCC(=O)O)c1 10.1016/s0960-894x(01)00364-x
CHEMBL305568 109618 0 None -398 3 Mouse 6.1 pKi = 6.1 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptor
ChEMBL 424 11 3 6 2.7 Cc1cccc(C[C@H](O)/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2SCCCSCC(=O)O)c1 10.1016/s0960-894x(01)00364-x
44304009 107512 0 None -1479 3 Mouse 5.1 pKi = 5.1 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptor
ChEMBL 482 15 3 7 3.3 CCCOCc1cccc(C[C@H](O)/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2SCCCSCC(=O)O)c1 10.1016/s0960-894x(01)00364-x
CHEMBL292717 107512 0 None -1479 3 Mouse 5.1 pKi = 5.1 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptor
ChEMBL 482 15 3 7 3.3 CCCOCc1cccc(C[C@H](O)/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2SCCCSCC(=O)O)c1 10.1016/s0960-894x(01)00364-x
11210487 71068 0 None 177 4 Human 8.1 pKi = 8.1 Binding
Binding affinity for human prostanoid EP2 receptorBinding affinity for human prostanoid EP2 receptor
ChEMBL 356 7 1 2 5.5 O=C(O)/C=C/c1ccccc1/C=C/c1ccccc1OCc1ccccc1 10.1016/j.bmcl.2004.11.051
CHEMBL181035 71068 0 None 177 4 Human 8.1 pKi = 8.1 Binding
Binding affinity for human prostanoid EP2 receptorBinding affinity for human prostanoid EP2 receptor
ChEMBL 356 7 1 2 5.5 O=C(O)/C=C/c1ccccc1/C=C/c1ccccc1OCc1ccccc1 10.1016/j.bmcl.2004.11.051
16725337 156380 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 mins
ChEMBL 443 12 2 4 6.0 CCCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2CCCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3947001 156380 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 mins
ChEMBL 443 12 2 4 6.0 CCCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2CCCc2ccc(C(=O)O)s2)cc1 nan
16725337 156380 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 443 12 2 4 6.0 CCCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2CCCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3947001 156380 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 443 12 2 4 6.0 CCCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2CCCc2ccc(C(=O)O)s2)cc1 nan
24953625 208311 0 None -323 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]PGE2 from human EP2 receptor expressed in HEK293-EBNA cells by scintillation countingDisplacement of [3H]PGE2 from human EP2 receptor expressed in HEK293-EBNA cells by scintillation counting
ChEMBL 461 6 2 3 6.2 Cc1sc(C)c(C(=O)N[C@@H](C)c2ccc(C(=O)O)cc2)c1Cc1cccc(C(F)(F)F)c1 10.1021/jm901771h
CHEMBL605330 208311 0 None -323 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]PGE2 from human EP2 receptor expressed in HEK293-EBNA cells by scintillation countingDisplacement of [3H]PGE2 from human EP2 receptor expressed in HEK293-EBNA cells by scintillation counting
ChEMBL 461 6 2 3 6.2 Cc1sc(C)c(C(=O)N[C@@H](C)c2ccc(C(=O)O)cc2)c1Cc1cccc(C(F)(F)F)c1 10.1021/jm901771h
10302378 89554 0 None -6606 4 Human 5.1 pKi = 5.1 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 539 9 1 5 6.6 O=C(/C=C/c1ccccc1Cc1ccc2cc(OCc3ccccc3)ccc2c1)NS(=O)(=O)c1cccs1 10.1016/j.bmcl.2006.08.025
CHEMBL217991 89554 0 None -6606 4 Human 5.1 pKi = 5.1 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 539 9 1 5 6.6 O=C(/C=C/c1ccccc1Cc1ccc2cc(OCc3ccccc3)ccc2c1)NS(=O)(=O)c1cccs1 10.1016/j.bmcl.2006.08.025
22009006 148342 0 None -1584 4 Human 5.1 pKi = 5.1 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 409 7 1 4 4.5 O=C(/C=C/c1ccccc1/C=C/Cc1ccccc1)NS(=O)(=O)c1cccs1 10.1016/j.bmcl.2006.08.025
CHEMBL384878 148342 0 None -1584 4 Human 5.1 pKi = 5.1 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 409 7 1 4 4.5 O=C(/C=C/c1ccccc1/C=C/Cc1ccccc1)NS(=O)(=O)c1cccs1 10.1016/j.bmcl.2006.08.025
9953337 148438 0 None -1584 4 Human 5.1 pKi = 5.1 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 409 7 1 4 4.5 O=C(/C=C/c1ccccc1C/C=C/c1ccccc1)NS(=O)(=O)c1cccs1 10.1016/j.bmcl.2006.08.025
CHEMBL385396 148438 0 None -1584 4 Human 5.1 pKi = 5.1 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 409 7 1 4 4.5 O=C(/C=C/c1ccccc1C/C=C/c1ccccc1)NS(=O)(=O)c1cccs1 10.1016/j.bmcl.2006.08.025
25003075 13610 18 None -28183 7 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]PGE2 from human prostanoid EP2 receptor expressed in HEK293-EBNA cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from human prostanoid EP2 receptor expressed in HEK293-EBNA cells after 60 mins by scintillation counting
ChEMBL 478 6 2 3 5.8 O=C(O)c1ccc(C2(NC(=O)c3cccc4ccn(Cc5ccc(C(F)(F)F)cc5)c34)CC2)cc1 10.1016/j.bmcl.2010.04.065
CHEMBL1084009 13610 18 None -28183 7 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]PGE2 from human prostanoid EP2 receptor expressed in HEK293-EBNA cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from human prostanoid EP2 receptor expressed in HEK293-EBNA cells after 60 mins by scintillation counting
ChEMBL 478 6 2 3 5.8 O=C(O)c1ccc(C2(NC(=O)c3cccc4ccn(Cc5ccc(C(F)(F)F)cc5)c34)CC2)cc1 10.1016/j.bmcl.2010.04.065
10247632 84766 0 None -1 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]PGE2 from human EP2 receptor expressed in HEK293 cellsDisplacement of [3H]PGE2 from human EP2 receptor expressed in HEK293 cells
ChEMBL 355 9 1 2 4.6 CCCC/C=C(C)/C=C\[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.05.025
CHEMBL2096894 84766 0 None -1 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]PGE2 from human EP2 receptor expressed in HEK293 cellsDisplacement of [3H]PGE2 from human EP2 receptor expressed in HEK293 cells
ChEMBL 355 9 1 2 4.6 CCCC/C=C(C)/C=C\[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.05.025
10178073 23331 0 None -1148 4 Human 5.1 pKi = 5.1 Binding
Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 384 8 1 2 5.9 Cc1cccc(/C=C/Cc2ccccc2/C=C/C(=O)O)c1OCc1ccccc1 10.1016/s0960-894x(03)00794-7
CHEMBL123794 23331 0 None -1148 4 Human 5.1 pKi = 5.1 Binding
Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 384 8 1 2 5.9 Cc1cccc(/C=C/Cc2ccccc2/C=C/C(=O)O)c1OCc1ccccc1 10.1016/s0960-894x(03)00794-7
9944231 24807 0 None -10 4 Human 5.1 pKi = 5.1 Binding
Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 302 5 1 1 5.0 O=C(O)CCc1ccccc1-c1cccc(-c2ccccc2)c1 10.1016/s0960-894x(03)00794-7
CHEMBL126472 24807 0 None -10 4 Human 5.1 pKi = 5.1 Binding
Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 302 5 1 1 5.0 O=C(O)CCc1ccccc1-c1cccc(-c2ccccc2)c1 10.1016/s0960-894x(03)00794-7
10178073 23331 0 None -1148 4 Human 5.1 pKi = 5.1 Binding
Binding affinity for human prostanoid EP2 receptorBinding affinity for human prostanoid EP2 receptor
ChEMBL 384 8 1 2 5.9 Cc1cccc(/C=C/Cc2ccccc2/C=C/C(=O)O)c1OCc1ccccc1 10.1016/j.bmcl.2004.11.051
CHEMBL123794 23331 0 None -1148 4 Human 5.1 pKi = 5.1 Binding
Binding affinity for human prostanoid EP2 receptorBinding affinity for human prostanoid EP2 receptor
ChEMBL 384 8 1 2 5.9 Cc1cccc(/C=C/Cc2ccccc2/C=C/C(=O)O)c1OCc1ccccc1 10.1016/j.bmcl.2004.11.051
12112238 124849 0 None -10 4 Human 6.1 pKi = 6.1 Binding
Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 406 7 1 2 6.7 O=C(O)/C=C/c1ccccc1-c1cccc(-c2ccccc2OCc2ccccc2)c1 10.1016/s0960-894x(03)00794-7
CHEMBL340501 124849 0 None -10 4 Human 6.1 pKi = 6.1 Binding
Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 406 7 1 2 6.7 O=C(O)/C=C/c1ccccc1-c1cccc(-c2ccccc2OCc2ccccc2)c1 10.1016/s0960-894x(03)00794-7
44444715 100973 0 None -25 2 Human 5.1 pKi = 5.1 Binding
Binding affinity at human prostaglandin EP2 receptorBinding affinity at human prostaglandin EP2 receptor
ChEMBL 450 12 2 4 3.7 O=C(O)c1ccc(CCN2C(=O)CCN2CCC(O)Cc2cccc(CCC3CC3)c2)cc1 10.1016/j.bmcl.2007.09.074
CHEMBL249745 100973 0 None -25 2 Human 5.1 pKi = 5.1 Binding
Binding affinity at human prostaglandin EP2 receptorBinding affinity at human prostaglandin EP2 receptor
ChEMBL 450 12 2 4 3.7 O=C(O)c1ccc(CCN2C(=O)CCN2CCC(O)Cc2cccc(CCC3CC3)c2)cc1 10.1016/j.bmcl.2007.09.074
57398585 76245 0 None -6 2 Mouse 7.1 pKi = 7.1 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 414 9 2 5 3.2 Cc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=O)N2CCCc2nc(C(=O)O)cs2)c1 10.1016/j.bmcl.2011.10.109
CHEMBL1933721 76245 0 None -6 2 Mouse 7.1 pKi = 7.1 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 414 9 2 5 3.2 Cc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=O)N2CCCc2nc(C(=O)O)cs2)c1 10.1016/j.bmcl.2011.10.109
57398585 76245 0 None -6 2 Mouse 7.1 pKi = 7.1 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 414 9 2 5 3.2 Cc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=O)N2CCCc2nc(C(=O)O)cs2)c1 10.1016/j.bmc.2012.02.018
CHEMBL1933721 76245 0 None -6 2 Mouse 7.1 pKi = 7.1 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 414 9 2 5 3.2 Cc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=O)N2CCCc2nc(C(=O)O)cs2)c1 10.1016/j.bmc.2012.02.018
56834112 76122 0 None -1071 2 Mouse 5.1 pKi = 5.1 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counterDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counter
ChEMBL 421 13 2 5 2.9 COCc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=O)N2CCSCCCC(=O)O)c1 10.1016/j.bmc.2011.12.009
CHEMBL1929527 76122 0 None -1071 2 Mouse 5.1 pKi = 5.1 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counterDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counter
ChEMBL 421 13 2 5 2.9 COCc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=O)N2CCSCCCC(=O)O)c1 10.1016/j.bmc.2011.12.009
44290271 185827 0 None -204 2 Human 4.1 pKi = 4.1 Binding
Binding affinity was determined against prostanoid EP2 receptorBinding affinity was determined against prostanoid EP2 receptor
ChEMBL 455 11 2 3 5.6 O=C(O)CCCCCCN1C(=O)CC[C@@H]1/C=C/C(O)c1cccc(-c2cccc(Cl)c2)c1 10.1016/j.bmcl.2004.01.063
CHEMBL47138 185827 0 None -204 2 Human 4.1 pKi = 4.1 Binding
Binding affinity was determined against prostanoid EP2 receptorBinding affinity was determined against prostanoid EP2 receptor
ChEMBL 455 11 2 3 5.6 O=C(O)CCCCCCN1C(=O)CC[C@@H]1/C=C/C(O)c1cccc(-c2cccc(Cl)c2)c1 10.1016/j.bmcl.2004.01.063
52944193 23305 0 None -63 4 Human 6.1 pKi = 6.1 Binding
Binding affinity for human prostanoid EP2 receptorBinding affinity for human prostanoid EP2 receptor
ChEMBL 768 16 2 4 11.9 Cc1cccc(/C=C/Cc2ccccc2/C=C/C(=O)O)c1OCc1ccccc1.Cc1cccc(C/C=C/c2ccccc2/C=C/C(=O)O)c1OCc1ccccc1 10.1016/j.bmcl.2004.11.051
CHEMBL1237295 23305 0 None -63 4 Human 6.1 pKi = 6.1 Binding
Binding affinity for human prostanoid EP2 receptorBinding affinity for human prostanoid EP2 receptor
ChEMBL 768 16 2 4 11.9 Cc1cccc(/C=C/Cc2ccccc2/C=C/C(=O)O)c1OCc1ccccc1.Cc1cccc(C/C=C/c2ccccc2/C=C/C(=O)O)c1OCc1ccccc1 10.1016/j.bmcl.2004.11.051
44419374 89770 0 None -95 4 Human 6.1 pKi = 6.1 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 384 8 1 2 5.9 Cc1ccc(OCc2ccccc2)c(/C=C/Cc2ccccc2/C=C/C(=O)O)c1 10.1016/j.bmcl.2006.08.025
CHEMBL218123 89770 0 None -95 4 Human 6.1 pKi = 6.1 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 384 8 1 2 5.9 Cc1ccc(OCc2ccccc2)c(/C=C/Cc2ccccc2/C=C/C(=O)O)c1 10.1016/j.bmcl.2006.08.025
44419379 144641 0 None -95 4 Human 6.1 pKi = 6.1 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 384 8 1 2 5.9 Cc1ccc(OCc2ccccc2)c(C/C=C/c2ccccc2/C=C/C(=O)O)c1 10.1016/j.bmcl.2006.08.025
CHEMBL376053 144641 0 None -95 4 Human 6.1 pKi = 6.1 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 384 8 1 2 5.9 Cc1ccc(OCc2ccccc2)c(C/C=C/c2ccccc2/C=C/C(=O)O)c1 10.1016/j.bmcl.2006.08.025
44320388 213187 0 None -56 4 Human 5.1 pKi = 5.1 Binding
Binding affinity at human Prostanoid EP2 receptor.Binding affinity at human Prostanoid EP2 receptor.
ChEMBL 536 11 2 6 5.8 Cc1cccc(OCCCOc2ccc(-c3ccccc3CNC(=O)NS(=O)(=O)c3cccs3)cc2)c1 10.1016/s0960-894x(02)00518-8
CHEMBL87797 213187 0 None -56 4 Human 5.1 pKi = 5.1 Binding
Binding affinity at human Prostanoid EP2 receptor.Binding affinity at human Prostanoid EP2 receptor.
ChEMBL 536 11 2 6 5.8 Cc1cccc(OCCCOc2ccc(-c3ccccc3CNC(=O)NS(=O)(=O)c3cccs3)cc2)c1 10.1016/s0960-894x(02)00518-8
9954562 90912 0 None -478 4 Human 5.1 pKi = 5.1 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 433 6 1 4 5.0 O=C(/C=C/c1ccccc1Cc1ccc2ccccc2c1)NS(=O)(=O)c1cccs1 10.1016/j.bmcl.2006.08.025
CHEMBL220802 90912 0 None -478 4 Human 5.1 pKi = 5.1 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 433 6 1 4 5.0 O=C(/C=C/c1ccccc1Cc1ccc2ccccc2c1)NS(=O)(=O)c1cccs1 10.1016/j.bmcl.2006.08.025
138 9855 88 None -19 18 Mouse 7.1 pKi = 7.1 Binding
Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.
ChEMBL 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 10.1016/s0960-894x(01)00359-6
149351 9855 88 None -19 18 Mouse 7.1 pKi = 7.1 Binding
Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.
ChEMBL 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 10.1016/s0960-894x(01)00359-6
1882 9855 88 None -19 18 Mouse 7.1 pKi = 7.1 Binding
Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.
ChEMBL 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 10.1016/s0960-894x(01)00359-6
5280723 9855 88 None -19 18 Mouse 7.1 pKi = 7.1 Binding
Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.
ChEMBL 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 10.1016/s0960-894x(01)00359-6
CHEMBL495 9855 88 None -19 18 Mouse 7.1 pKi = 7.1 Binding
Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.
ChEMBL 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 10.1016/s0960-894x(01)00359-6
DB00770 9855 88 None -19 18 Mouse 7.1 pKi = 7.1 Binding
Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.
ChEMBL 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 10.1016/s0960-894x(01)00359-6
52945423 23313 0 None -33 4 Human 5.1 pKi = 5.1 Binding
Binding affinity for human prostanoid EP2 receptorBinding affinity for human prostanoid EP2 receptor
ChEMBL 824 18 2 6 11.6 CC(=O)c1ccc(OCc2ccccc2)c(/C=C/Cc2ccccc2/C=C/C(=O)O)c1.CC(=O)c1ccc(OCc2ccccc2)c(C/C=C/c2ccccc2/C=C/C(=O)O)c1 10.1016/j.bmcl.2004.11.051
CHEMBL1237303 23313 0 None -33 4 Human 5.1 pKi = 5.1 Binding
Binding affinity for human prostanoid EP2 receptorBinding affinity for human prostanoid EP2 receptor
ChEMBL 824 18 2 6 11.6 CC(=O)c1ccc(OCc2ccccc2)c(/C=C/Cc2ccccc2/C=C/C(=O)O)c1.CC(=O)c1ccc(OCc2ccccc2)c(C/C=C/c2ccccc2/C=C/C(=O)O)c1 10.1016/j.bmcl.2004.11.051
22009008 89932 0 None -5495 4 Human 5.1 pKi = 5.1 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 545 11 1 6 6.1 COc1cc(/C=C/Cc2ccccc2/C=C/C(=O)NS(=O)(=O)c2cccs2)ccc1OCc1ccccc1 10.1016/j.bmcl.2006.08.025
CHEMBL218280 89932 0 None -5495 4 Human 5.1 pKi = 5.1 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 545 11 1 6 6.1 COc1cc(/C=C/Cc2ccccc2/C=C/C(=O)NS(=O)(=O)c2cccs2)ccc1OCc1ccccc1 10.1016/j.bmcl.2006.08.025
22009004 148529 0 None -2884 4 Human 5.1 pKi = 5.1 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 545 11 1 6 6.1 COc1cc(C/C=C/c2ccccc2/C=C/C(=O)NS(=O)(=O)c2cccs2)ccc1OCc1ccccc1 10.1016/j.bmcl.2006.08.025
CHEMBL385955 148529 0 None -2884 4 Human 5.1 pKi = 5.1 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 545 11 1 6 6.1 COc1cc(C/C=C/c2ccccc2/C=C/C(=O)NS(=O)(=O)c2cccs2)ccc1OCc1ccccc1 10.1016/j.bmcl.2006.08.025
132836 66469 23 None 1 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 388 13 2 3 5.8 CCCCCC(O)c1ccc([C@H]2CCC(=O)[C@@H]2CCCCCCC(=O)O)cc1 nan
CHEMBL1722929 66469 23 None 1 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 388 13 2 3 5.8 CCCCCC(O)c1ccc([C@H]2CCC(=O)[C@@H]2CCCCCCC(=O)O)cc1 nan
44442332 101302 0 None -3 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]PGE2 from human EP2 receptor expressed in HEK293 cellsDisplacement of [3H]PGE2 from human EP2 receptor expressed in HEK293 cells
ChEMBL 341 9 1 2 4.2 CCCC/C=C\C=C\[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.05.025
CHEMBL251709 101302 0 None -3 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]PGE2 from human EP2 receptor expressed in HEK293 cellsDisplacement of [3H]PGE2 from human EP2 receptor expressed in HEK293 cells
ChEMBL 341 9 1 2 4.2 CCCC/C=C\C=C\[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.05.025
44393680 73119 0 None -4 2 Mouse 5.1 pKi = 5.1 Binding
Binding affinity for mouse Prostanoid EP2 receptorBinding affinity for mouse Prostanoid EP2 receptor
ChEMBL 367 7 1 5 4.2 CCCCOc1ccc(C(=O)n2cc(C(=O)O)c3cc(OC)ccc32)cc1 10.1016/j.bmcl.2004.06.006
CHEMBL185087 73119 0 None -4 2 Mouse 5.1 pKi = 5.1 Binding
Binding affinity for mouse Prostanoid EP2 receptorBinding affinity for mouse Prostanoid EP2 receptor
ChEMBL 367 7 1 5 4.2 CCCCOc1ccc(C(=O)n2cc(C(=O)O)c3cc(OC)ccc32)cc1 10.1016/j.bmcl.2004.06.006
84973026 135986 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Measurement of EP2 receptor binding affinity was carried out according to the method of Abramovitz et al. (Biochimica et Biophysica Acta, 1483, 285 (2000)). A test compound dissolved in dimethylsulfoxide and [3H]PGE2 (NET-428, available from PerkinElmer Inc.) (final concentration: 10 nM) were added to a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2, 1 mM EDTA) in which 10 μg of a membrane fraction (ES-562-M, available from Euroscreen S.A.) of HEK293 cells expressing human EP2 receptor had been suspended, followed by incubation at 30° C. for 60 minutes. The membrane fraction was recovered on glass fiber filter paper (GF/B, available from Whatman PLC) using a cell harvester (M30R, available from Brandel Inc.), and after washing with a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2), radioactivity was measured with a liquid scintillation analyzer (2000CA, available from Packard).Binding Assay: Measurement of EP2 receptor binding affinity was carried out according to the method of Abramovitz et al. (Biochimica et Biophysica Acta, 1483, 285 (2000)). A test compound dissolved in dimethylsulfoxide and [3H]PGE2 (NET-428, available from PerkinElmer Inc.) (final concentration: 10 nM) were added to a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2, 1 mM EDTA) in which 10 μg of a membrane fraction (ES-562-M, available from Euroscreen S.A.) of HEK293 cells expressing human EP2 receptor had been suspended, followed by incubation at 30° C. for 60 minutes. The membrane fraction was recovered on glass fiber filter paper (GF/B, available from Whatman PLC) using a cell harvester (M30R, available from Brandel Inc.), and after washing with a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2), radioactivity was measured with a liquid scintillation analyzer (2000CA, available from Packard).
ChEMBL 441 7 4 4 4.7 COc1ccc(-c2cc(-c3ccccc3)[nH]c2C(=O)Nc2cccc(CC(=O)NO)c2)cc1 nan
CHEMBL3670664 135986 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Measurement of EP2 receptor binding affinity was carried out according to the method of Abramovitz et al. (Biochimica et Biophysica Acta, 1483, 285 (2000)). A test compound dissolved in dimethylsulfoxide and [3H]PGE2 (NET-428, available from PerkinElmer Inc.) (final concentration: 10 nM) were added to a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2, 1 mM EDTA) in which 10 μg of a membrane fraction (ES-562-M, available from Euroscreen S.A.) of HEK293 cells expressing human EP2 receptor had been suspended, followed by incubation at 30° C. for 60 minutes. The membrane fraction was recovered on glass fiber filter paper (GF/B, available from Whatman PLC) using a cell harvester (M30R, available from Brandel Inc.), and after washing with a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2), radioactivity was measured with a liquid scintillation analyzer (2000CA, available from Packard).Binding Assay: Measurement of EP2 receptor binding affinity was carried out according to the method of Abramovitz et al. (Biochimica et Biophysica Acta, 1483, 285 (2000)). A test compound dissolved in dimethylsulfoxide and [3H]PGE2 (NET-428, available from PerkinElmer Inc.) (final concentration: 10 nM) were added to a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2, 1 mM EDTA) in which 10 μg of a membrane fraction (ES-562-M, available from Euroscreen S.A.) of HEK293 cells expressing human EP2 receptor had been suspended, followed by incubation at 30° C. for 60 minutes. The membrane fraction was recovered on glass fiber filter paper (GF/B, available from Whatman PLC) using a cell harvester (M30R, available from Brandel Inc.), and after washing with a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2), radioactivity was measured with a liquid scintillation analyzer (2000CA, available from Packard).
ChEMBL 441 7 4 4 4.7 COc1ccc(-c2cc(-c3ccccc3)[nH]c2C(=O)Nc2cccc(CC(=O)NO)c2)cc1 nan
57894063 81940 0 None -5 3 Mouse 8.0 pKi = 8.0 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 524 11 2 7 4.8 COc1ccc(-c2cccc(C[C@H](O)/C=C/[C@H]3CCC(=O)N3CCSc3nc(C(=O)O)cs3)c2)cc1 10.1016/j.bmc.2012.04.008
CHEMBL2036319 81940 0 None -5 3 Mouse 8.0 pKi = 8.0 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 524 11 2 7 4.8 COc1ccc(-c2cccc(C[C@H](O)/C=C/[C@H]3CCC(=O)N3CCSc3nc(C(=O)O)cs3)c2)cc1 10.1016/j.bmc.2012.04.008
56835070 76246 0 None -22 3 Mouse 8.0 pKi = 8.0 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 432 9 2 6 3.4 Cc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=O)N2CCSc2nc(C(=O)O)cs2)c1 10.1016/j.bmcl.2011.10.109
CHEMBL1933722 76246 0 None -22 3 Mouse 8.0 pKi = 8.0 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 432 9 2 6 3.4 Cc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=O)N2CCSc2nc(C(=O)O)cs2)c1 10.1016/j.bmcl.2011.10.109
56835070 76246 0 None -22 3 Mouse 8.0 pKi = 8.0 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 432 9 2 6 3.4 Cc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=O)N2CCSc2nc(C(=O)O)cs2)c1 10.1016/j.bmc.2012.02.018
CHEMBL1933722 76246 0 None -22 3 Mouse 8.0 pKi = 8.0 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 432 9 2 6 3.4 Cc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=O)N2CCSc2nc(C(=O)O)cs2)c1 10.1016/j.bmc.2012.02.018
56835070 76246 0 None -22 3 Mouse 8.0 pKi = 8.0 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 432 9 2 6 3.4 Cc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=O)N2CCSc2nc(C(=O)O)cs2)c1 10.1016/j.bmc.2012.04.008
CHEMBL1933722 76246 0 None -22 3 Mouse 8.0 pKi = 8.0 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 432 9 2 6 3.4 Cc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=O)N2CCSc2nc(C(=O)O)cs2)c1 10.1016/j.bmc.2012.04.008
84973025 135983 5 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Measurement of EP2 receptor binding affinity was carried out according to the method of Abramovitz et al. (Biochimica et Biophysica Acta, 1483, 285 (2000)). A test compound dissolved in dimethylsulfoxide and [3H]PGE2 (NET-428, available from PerkinElmer Inc.) (final concentration: 10 nM) were added to a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2, 1 mM EDTA) in which 10 μg of a membrane fraction (ES-562-M, available from Euroscreen S.A.) of HEK293 cells expressing human EP2 receptor had been suspended, followed by incubation at 30° C. for 60 minutes. The membrane fraction was recovered on glass fiber filter paper (GF/B, available from Whatman PLC) using a cell harvester (M30R, available from Brandel Inc.), and after washing with a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2), radioactivity was measured with a liquid scintillation analyzer (2000CA, available from Packard).Binding Assay: Measurement of EP2 receptor binding affinity was carried out according to the method of Abramovitz et al. (Biochimica et Biophysica Acta, 1483, 285 (2000)). A test compound dissolved in dimethylsulfoxide and [3H]PGE2 (NET-428, available from PerkinElmer Inc.) (final concentration: 10 nM) were added to a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2, 1 mM EDTA) in which 10 μg of a membrane fraction (ES-562-M, available from Euroscreen S.A.) of HEK293 cells expressing human EP2 receptor had been suspended, followed by incubation at 30° C. for 60 minutes. The membrane fraction was recovered on glass fiber filter paper (GF/B, available from Whatman PLC) using a cell harvester (M30R, available from Brandel Inc.), and after washing with a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2), radioactivity was measured with a liquid scintillation analyzer (2000CA, available from Packard).
ChEMBL 417 6 5 5 3.7 O=C(NO)c1ccc(CNC(=O)c2[nH]c(-c3ccc(O)cc3)cc2-c2ccoc2)cc1 nan
CHEMBL3670661 135983 5 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Measurement of EP2 receptor binding affinity was carried out according to the method of Abramovitz et al. (Biochimica et Biophysica Acta, 1483, 285 (2000)). A test compound dissolved in dimethylsulfoxide and [3H]PGE2 (NET-428, available from PerkinElmer Inc.) (final concentration: 10 nM) were added to a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2, 1 mM EDTA) in which 10 μg of a membrane fraction (ES-562-M, available from Euroscreen S.A.) of HEK293 cells expressing human EP2 receptor had been suspended, followed by incubation at 30° C. for 60 minutes. The membrane fraction was recovered on glass fiber filter paper (GF/B, available from Whatman PLC) using a cell harvester (M30R, available from Brandel Inc.), and after washing with a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2), radioactivity was measured with a liquid scintillation analyzer (2000CA, available from Packard).Binding Assay: Measurement of EP2 receptor binding affinity was carried out according to the method of Abramovitz et al. (Biochimica et Biophysica Acta, 1483, 285 (2000)). A test compound dissolved in dimethylsulfoxide and [3H]PGE2 (NET-428, available from PerkinElmer Inc.) (final concentration: 10 nM) were added to a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2, 1 mM EDTA) in which 10 μg of a membrane fraction (ES-562-M, available from Euroscreen S.A.) of HEK293 cells expressing human EP2 receptor had been suspended, followed by incubation at 30° C. for 60 minutes. The membrane fraction was recovered on glass fiber filter paper (GF/B, available from Whatman PLC) using a cell harvester (M30R, available from Brandel Inc.), and after washing with a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2), radioactivity was measured with a liquid scintillation analyzer (2000CA, available from Packard).
ChEMBL 417 6 5 5 3.7 O=C(NO)c1ccc(CNC(=O)c2[nH]c(-c3ccc(O)cc3)cc2-c2ccoc2)cc1 nan
21974374 134025 0 None -1 5 Mouse 7.1 pKi = 7.1 Binding
Ability to inhibit the binding of [3H]-PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP2Ability to inhibit the binding of [3H]-PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP2
ChEMBL 455 6 1 5 5.0 Cc1cc2c(CC(=O)O)cccc2n1C(=O)c1ccc(OCC2CCc3ccccc3O2)cc1 10.1016/j.bmcl.2004.07.039
CHEMBL365829 134025 0 None -1 5 Mouse 7.1 pKi = 7.1 Binding
Ability to inhibit the binding of [3H]-PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP2Ability to inhibit the binding of [3H]-PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP2
ChEMBL 455 6 1 5 5.0 Cc1cc2c(CC(=O)O)cccc2n1C(=O)c1ccc(OCC2CCc3ccccc3O2)cc1 10.1016/j.bmcl.2004.07.039
44304334 208355 0 None -45 5 Mouse 7.0 pKi = 7.0 Binding
Affinity for mouse Prostanoid EP2 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP2 receptor expressed in CHO cells
ChEMBL 372 13 3 5 3.0 CCCCC[C@H](O)/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CSCCCCC(=O)O 10.1016/s0960-894x(01)00365-1
CHEMBL60555 208355 0 None -45 5 Mouse 7.0 pKi = 7.0 Binding
Affinity for mouse Prostanoid EP2 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP2 receptor expressed in CHO cells
ChEMBL 372 13 3 5 3.0 CCCCC[C@H](O)/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CSCCCCC(=O)O 10.1016/s0960-894x(01)00365-1
57396659 78076 0 None -114 3 Mouse 7.0 pKi = 7.0 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 431 9 2 5 4.0 Cc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=O)N2CCSc2ccc(C(=O)O)s2)c1 10.1016/j.bmc.2012.02.018
CHEMBL1957430 78076 0 None -114 3 Mouse 7.0 pKi = 7.0 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 431 9 2 5 4.0 Cc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=O)N2CCSc2ccc(C(=O)O)s2)c1 10.1016/j.bmc.2012.02.018
44304199 107594 0 None - 1 Mouse 7.0 pKi = 7.0 Binding
Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.
ChEMBL 392 12 3 4 4.0 CCCC1([C@@H](O)C/C=C/C2[C@H](O)CC(=O)[C@@H]2C/C=C/CCCC(=O)O)CCC1 10.1016/s0960-894x(01)00359-6
CHEMBL293242 107594 0 None - 1 Mouse 7.0 pKi = 7.0 Binding
Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.
ChEMBL 392 12 3 4 4.0 CCCC1([C@@H](O)C/C=C/C2[C@H](O)CC(=O)[C@@H]2C/C=C/CCCC(=O)O)CCC1 10.1016/s0960-894x(01)00359-6
44444719 101001 0 None -67 2 Human 5.0 pKi = 5.0 Binding
Binding affinity at human prostaglandin EP2 receptorBinding affinity at human prostaglandin EP2 receptor
ChEMBL 382 9 2 4 2.4 O=C(O)c1ccc(CCN2C(=O)CCN2CC[C@@H](O)Cc2ccccc2)cc1 10.1016/j.bmcl.2007.09.074
CHEMBL249952 101001 0 None -67 2 Human 5.0 pKi = 5.0 Binding
Binding affinity at human prostaglandin EP2 receptorBinding affinity at human prostaglandin EP2 receptor
ChEMBL 382 9 2 4 2.4 O=C(O)c1ccc(CCN2C(=O)CCN2CC[C@@H](O)Cc2ccccc2)cc1 10.1016/j.bmcl.2007.09.074
10273914 206451 0 None -70 3 Mouse 5.0 pKi = 5.0 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 424 9 1 3 6.1 O=C(O)/C=C/c1ccc(COc2ccccc2)cc1OCCc1ccc2ccccc2c1 10.1016/j.bmc.2009.08.007
CHEMBL593041 206451 0 None -70 3 Mouse 5.0 pKi = 5.0 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 424 9 1 3 6.1 O=C(O)/C=C/c1ccc(COc2ccccc2)cc1OCCc1ccc2ccccc2c1 10.1016/j.bmc.2009.08.007
46230201 207395 0 None -436 3 Mouse 5.0 pKi = 5.0 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 453 9 2 3 5.9 C[C@H](NC(=O)c1cc(COc2ccccc2)ccc1CCC(=O)O)c1cccc2ccccc12 10.1016/j.bmc.2009.11.023
CHEMBL599355 207395 0 None -436 3 Mouse 5.0 pKi = 5.0 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 453 9 2 3 5.9 C[C@H](NC(=O)c1cc(COc2ccccc2)ccc1CCC(=O)O)c1cccc2ccccc12 10.1016/j.bmc.2009.11.023
118517485 149528 0 None -50 2 Human 5.0 pKi = 5.0 Binding
Radioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations wRadioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations w
ChEMBL 396 8 2 3 4.2 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2ccc(F)cc2)cc1 nan
CHEMBL3892492 149528 0 None -50 2 Human 5.0 pKi = 5.0 Binding
Radioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations wRadioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations w
ChEMBL 396 8 2 3 4.2 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2ccc(F)cc2)cc1 nan
118517490 159934 0 None -125 2 Human 5.0 pKi = 5.0 Binding
Radioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations wRadioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations w
ChEMBL 414 8 2 3 4.4 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2ccc(F)c(F)c2)cc1 nan
CHEMBL3976710 159934 0 None -125 2 Human 5.0 pKi = 5.0 Binding
Radioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations wRadioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations w
ChEMBL 414 8 2 3 4.4 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2ccc(F)c(F)c2)cc1 nan
9865111 70639 0 None -14 4 Human 6.0 pKi = 6.0 Binding
Binding affinity for human prostanoid EP2 receptorBinding affinity for human prostanoid EP2 receptor
ChEMBL 388 10 1 2 5.8 Cc1cccc(CCCc2ccccc2CCC(=O)O)c1OCc1ccccc1 10.1016/j.bmcl.2004.11.051
CHEMBL180343 70639 0 None -14 4 Human 6.0 pKi = 6.0 Binding
Binding affinity for human prostanoid EP2 receptorBinding affinity for human prostanoid EP2 receptor
ChEMBL 388 10 1 2 5.8 Cc1cccc(CCCc2ccccc2CCC(=O)O)c1OCc1ccccc1 10.1016/j.bmcl.2004.11.051
44419350 90917 0 None -14 4 Human 6.0 pKi = 6.0 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 388 10 1 2 5.8 Cc1ccc(OCc2ccccc2)c(CCCc2ccccc2CCC(=O)O)c1 10.1016/j.bmcl.2006.08.025
CHEMBL220820 90917 0 None -14 4 Human 6.0 pKi = 6.0 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 388 10 1 2 5.8 Cc1ccc(OCc2ccccc2)c(CCCc2ccccc2CCC(=O)O)c1 10.1016/j.bmcl.2006.08.025
118517359 151174 0 None -114 2 Human 6.0 pKi = 6.0 Binding
Radioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations wRadioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations w
ChEMBL 456 8 2 3 4.8 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2cccc(Br)c2)cc1 nan
CHEMBL3906016 151174 0 None -114 2 Human 6.0 pKi = 6.0 Binding
Radioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations wRadioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations w
ChEMBL 456 8 2 3 4.8 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2cccc(Br)c2)cc1 nan
10116114 132664 0 None -28 8 Mouse 7.0 pKi = 7 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 470 6 1 6 4.5 Cc1cc2c(CC(=O)O)cccc2n1C(=O)c1ccc(OC[C@@H]2CN(C)c3ccccc3O2)cc1 10.1016/j.bmc.2011.06.014
CHEMBL364841 132664 0 None -28 8 Mouse 7.0 pKi = 7 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 470 6 1 6 4.5 Cc1cc2c(CC(=O)O)cccc2n1C(=O)c1ccc(OC[C@@H]2CN(C)c3ccccc3O2)cc1 10.1016/j.bmc.2011.06.014
10116114 132664 0 None -28 8 Mouse 7.0 pKi = 7 Binding
Displacement of [3H]PGE2 from mouse prostaglandin EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]PGE2 from mouse prostaglandin EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 470 6 1 6 4.5 Cc1cc2c(CC(=O)O)cccc2n1C(=O)c1ccc(OC[C@@H]2CN(C)c3ccccc3O2)cc1 10.1016/j.bmc.2011.08.007
CHEMBL364841 132664 0 None -28 8 Mouse 7.0 pKi = 7 Binding
Displacement of [3H]PGE2 from mouse prostaglandin EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]PGE2 from mouse prostaglandin EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 470 6 1 6 4.5 Cc1cc2c(CC(=O)O)cccc2n1C(=O)c1ccc(OC[C@@H]2CN(C)c3ccccc3O2)cc1 10.1016/j.bmc.2011.08.007
44390806 70852 0 None -24 3 Human 6.0 pKi = 6 Binding
Binding affinity for human prostanoid EP2 receptorBinding affinity for human prostanoid EP2 receptor
ChEMBL 386 8 1 2 5.9 Cc1cccc(C2CC2c2ccccc2CCC(=O)O)c1OCc1ccccc1 10.1016/j.bmcl.2004.11.051
CHEMBL180752 70852 0 None -24 3 Human 6.0 pKi = 6 Binding
Binding affinity for human prostanoid EP2 receptorBinding affinity for human prostanoid EP2 receptor
ChEMBL 386 8 1 2 5.9 Cc1cccc(C2CC2c2ccccc2CCC(=O)O)c1OCc1ccccc1 10.1016/j.bmcl.2004.11.051
1883 9856 75 None -6 24 Human 7.8 pKd = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10634944
1883 9856 75 None -6 24 Human 7.8 pKd = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 16604093
1916 9856 75 None -6 24 Human 7.8 pKd = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10634944
1916 9856 75 None -6 24 Human 7.8 pKd = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 16604093
5280360 9856 75 None -6 24 Human 7.8 pKd = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10634944
5280360 9856 75 None -6 24 Human 7.8 pKd = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 16604093
913 9856 75 None -6 24 Human 7.8 pKd = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10634944
913 9856 75 None -6 24 Human 7.8 pKd = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 16604093
CHEMBL548 9856 75 None -6 24 Human 7.8 pKd = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10634944
CHEMBL548 9856 75 None -6 24 Human 7.8 pKd = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 16604093
DB00917 9856 75 None -6 24 Human 7.8 pKd = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10634944
DB00917 9856 75 None -6 24 Human 7.8 pKd = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 16604093
1883 9856 75 None -15 24 Mouse 7.7 pKd None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 14699136
1916 9856 75 None -15 24 Mouse 7.7 pKd None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 14699136
5280360 9856 75 None -15 24 Mouse 7.7 pKd None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 14699136
913 9856 75 None -15 24 Mouse 7.7 pKd None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 14699136
CHEMBL548 9856 75 None -15 24 Mouse 7.7 pKd None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 14699136
DB00917 9856 75 None -15 24 Mouse 7.7 pKd None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 14699136
1883 9856 75 None -7 24 Rat 8.1 pKd None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 9440134
1883 9856 75 None -7 24 Rat 8.1 pKd None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 9537820
1916 9856 75 None -7 24 Rat 8.1 pKd None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 9440134
1916 9856 75 None -7 24 Rat 8.1 pKd None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 9537820
5280360 9856 75 None -7 24 Rat 8.1 pKd None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 9440134
5280360 9856 75 None -7 24 Rat 8.1 pKd None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 9537820
913 9856 75 None -7 24 Rat 8.1 pKd None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 9440134
913 9856 75 None -7 24 Rat 8.1 pKd None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 9537820
CHEMBL548 9856 75 None -7 24 Rat 8.1 pKd None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 9440134
CHEMBL548 9856 75 None -7 24 Rat 8.1 pKd None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 9537820
DB00917 9856 75 None -7 24 Rat 8.1 pKd None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 9440134
DB00917 9856 75 None -7 24 Rat 8.1 pKd None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 9537820
138 9855 88 3H-PGE2 -19 18 Mouse 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O None
149351 9855 88 3H-PGE2 -19 18 Mouse 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O None
1882 9855 88 3H-PGE2 -19 18 Mouse 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O None
5280723 9855 88 3H-PGE2 -19 18 Mouse 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O None
CHEMBL495 9855 88 3H-PGE2 -19 18 Mouse 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O None
DB00770 9855 88 3H-PGE2 -19 18 Mouse 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O None
None 222825 0 3H-PGE2 -66 3 Mouse 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 350 11 3 3 4.1 CCCCCC(C=CC1C(CC2C1CC(=C2)CCCCC(=O)O)O)O None
5090 22333 106 Functional -1348 30 Dog 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 314 3 0 4 2.6 CS(=O)(=O)c1ccc(C2=C(c3ccccc3)C(=O)OC2)cc1 None
5090 22333 106 Functional -35 30 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 314 3 0 4 2.6 CS(=O)(=O)c1ccc(C2=C(c3ccccc3)C(=O)OC2)cc1 None
CHEMBL122 22333 106 Functional -1348 30 Dog 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 314 3 0 4 2.6 CS(=O)(=O)c1ccc(C2=C(c3ccccc3)C(=O)OC2)cc1 None
CHEMBL122 22333 106 Functional -35 30 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 314 3 0 4 2.6 CS(=O)(=O)c1ccc(C2=C(c3ccccc3)C(=O)OC2)cc1 None
5311035 104579 29 3H-PGE2 4 9 Mouse 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 408 13 2 5 4.3 CCCC1([C@H](O)C/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2CCCCCCC(=O)OC)CCC1 None
CHEMBL271896 104579 29 3H-PGE2 4 9 Mouse 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 408 13 2 5 4.3 CCCC1([C@H](O)C/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2CCCCCCC(=O)OC)CCC1 None
1883 9856 75 3H-PGE2 -15 24 Mouse 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O None
1916 9856 75 3H-PGE2 -15 24 Mouse 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O None
5280360 9856 75 3H-PGE2 -15 24 Mouse 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O None
913 9856 75 3H-PGE2 -15 24 Mouse 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O None
CHEMBL548 9856 75 3H-PGE2 -15 24 Mouse 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O None
DB00917 9856 75 3H-PGE2 -15 24 Mouse 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O None
1917 7714 0 3H-PGE2 -22 9 Mouse 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 374 6 3 4 2.2 CCC#CC[C@@H]([C@@H](C#C[C@H]1[C@H](O)C[C@H]2[C@@H]1C/C(=C/COCC(=O)O)/C2)O)C None
5311044 7714 0 3H-PGE2 -22 9 Mouse 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 374 6 3 4 2.2 CCC#CC[C@@H]([C@@H](C#C[C@H]1[C@H](O)C[C@H]2[C@@H]1C/C(=C/COCC(=O)O)/C2)O)C None
631 7714 0 3H-PGE2 -22 9 Mouse 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 374 6 3 4 2.2 CCC#CC[C@@H]([C@@H](C#C[C@H]1[C@H](O)C[C@H]2[C@@H]1C/C(=C/COCC(=O)O)/C2)O)C None
CHEMBL160629 7714 0 3H-PGE2 -22 9 Mouse 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 374 6 3 4 2.2 CCC#CC[C@@H]([C@@H](C#C[C@H]1[C@H](O)C[C@H]2[C@@H]1C/C(=C/COCC(=O)O)/C2)O)C None
89077401 222823 0 3H-PGE2 -144 12 Mouse 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 360 8 3 3 3.5 CC#CCC(C)C(C=CC1C(CC2C1CC(=CCCCC(=O)O)C2)O)O None
133126726 222824 0 3H-PGE2 -151 14 Mouse 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 350 10 3 3 4.1 CCCCCC(C=CC1C(CC2C1CC(=CCCCC(=O)O)C2)O)O None
24868263 222824 0 3H-PGE2 -151 14 Mouse 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 350 10 3 3 4.1 CCCCCC(C=CC1C(CC2C1CC(=CCCCC(=O)O)C2)O)O None
1440 8808 119 Functional -9 6 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 357 4 1 4 3.9 COc1ccc2c(c1)c(CC(=O)O)c(n2C(=O)c1ccc(cc1)Cl)C None
1909 8808 119 Functional -9 6 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 357 4 1 4 3.9 COc1ccc2c(c1)c(CC(=O)O)c(n2C(=O)c1ccc(cc1)Cl)C None
3715 8808 119 Functional -9 6 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 357 4 1 4 3.9 COc1ccc2c(c1)c(CC(=O)O)c(n2C(=O)c1ccc(cc1)Cl)C None
CHEMBL6 8808 119 Functional -9 6 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 357 4 1 4 3.9 COc1ccc2c(c1)c(CC(=O)O)c(n2C(=O)c1ccc(cc1)Cl)C None
DB00328 8808 119 Functional -9 6 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 357 4 1 4 3.9 COc1ccc2c(c1)c(CC(=O)O)c(n2C(=O)c1ccc(cc1)Cl)C None
None 222822 0 3H-PGE2 -9 5 Mouse 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 366 12 2 3 5.2 CCCCCC(C=CC1CC2CC(C1CC=CCCCC(=O)O)S2)O None
None 222828 0 3H-PGE2 -2 3 Mouse 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 512 11 2 4 4.6 C1CC2C(C(C1O2)CC=CCCCC(=O)O)C=CC(COC3=CC=C(C=C3)I)O None
1928 7105 0 3H-PGE2 -3 3 Mouse 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 388 13 2 3 5.8 CCCCCC(c1ccc(cc1)C1CCC(=O)C1CCCCCCC(=O)O)O None
5310998 7105 0 3H-PGE2 -3 3 Mouse 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 388 13 2 3 5.8 CCCCCC(c1ccc(cc1)C1CCC(=O)C1CCCCCCC(=O)O)O None
1817 9320 68 3H-PGE2 -6 12 Mouse 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 382 13 2 5 4.0 CCCCC(C/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)OC)(O)C None
1936 9320 68 3H-PGE2 -6 12 Mouse 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 382 13 2 5 4.0 CCCCC(C/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)OC)(O)C None
5282381 9320 68 3H-PGE2 -6 12 Mouse 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 382 13 2 5 4.0 CCCCC(C/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)OC)(O)C None
CHEMBL606 9320 68 3H-PGE2 -6 12 Mouse 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 382 13 2 5 4.0 CCCCC(C/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)OC)(O)C None
DB00929 9320 68 3H-PGE2 -6 12 Mouse 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 382 13 2 5 4.0 CCCCC(C/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)OC)(O)C None
1440 8808 119 Functional -38 6 Dog 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 357 4 1 4 3.9 COc1ccc2c(c1)c(CC(=O)O)c(n2C(=O)c1ccc(cc1)Cl)C None
1440 8808 119 Functional -9 6 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 357 4 1 4 3.9 COc1ccc2c(c1)c(CC(=O)O)c(n2C(=O)c1ccc(cc1)Cl)C None
1909 8808 119 Functional -38 6 Dog 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 357 4 1 4 3.9 COc1ccc2c(c1)c(CC(=O)O)c(n2C(=O)c1ccc(cc1)Cl)C None
1909 8808 119 Functional -9 6 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 357 4 1 4 3.9 COc1ccc2c(c1)c(CC(=O)O)c(n2C(=O)c1ccc(cc1)Cl)C None
3715 8808 119 Functional -38 6 Dog 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 357 4 1 4 3.9 COc1ccc2c(c1)c(CC(=O)O)c(n2C(=O)c1ccc(cc1)Cl)C None
3715 8808 119 Functional -9 6 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 357 4 1 4 3.9 COc1ccc2c(c1)c(CC(=O)O)c(n2C(=O)c1ccc(cc1)Cl)C None
CHEMBL6 8808 119 Functional -38 6 Dog 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 357 4 1 4 3.9 COc1ccc2c(c1)c(CC(=O)O)c(n2C(=O)c1ccc(cc1)Cl)C None
CHEMBL6 8808 119 Functional -9 6 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 357 4 1 4 3.9 COc1ccc2c(c1)c(CC(=O)O)c(n2C(=O)c1ccc(cc1)Cl)C None
DB00328 8808 119 Functional -38 6 Dog 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 357 4 1 4 3.9 COc1ccc2c(c1)c(CC(=O)O)c(n2C(=O)c1ccc(cc1)Cl)C None
DB00328 8808 119 Functional -9 6 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 357 4 1 4 3.9 COc1ccc2c(c1)c(CC(=O)O)c(n2C(=O)c1ccc(cc1)Cl)C None
119461 7108 72 3H-PGE2 1 10 Mouse 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 298 3 1 4 3.4 CC(Oc1ccc2c(c1)oc1c(c2=O)cc(cc1)C(=O)O)C None
1896 7108 72 3H-PGE2 1 10 Mouse 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 298 3 1 4 3.4 CC(Oc1ccc2c(c1)oc1c(c2=O)cc(cc1)C(=O)O)C None
CHEMBL1317823 7108 72 3H-PGE2 1 10 Mouse 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 298 3 1 4 3.4 CC(Oc1ccc2c(c1)oc1c(c2=O)cc(cc1)C(=O)O)C None
5090 22333 106 Functional -35 30 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 314 3 0 4 2.6 CS(=O)(=O)c1ccc(C2=C(c3ccccc3)C(=O)OC2)cc1 None
CHEMBL122 22333 106 Functional -35 30 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 314 3 0 4 2.6 CS(=O)(=O)c1ccc(C2=C(c3ccccc3)C(=O)OC2)cc1 None
5090 22333 106 Functional -35 30 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 314 3 0 4 2.6 CS(=O)(=O)c1ccc(C2=C(c3ccccc3)C(=O)OC2)cc1 None
CHEMBL122 22333 106 Functional -35 30 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 314 3 0 4 2.6 CS(=O)(=O)c1ccc(C2=C(c3ccccc3)C(=O)OC2)cc1 None
5077 10351 79 None 1 4 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 496 12 1 7 3.9 O=C(NS(=O)(=O)C)COCCCCN(c1cnc(c(n1)c1ccccc1)c1ccccc1)C(C)C None
7552 10351 79 None 1 4 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 496 12 1 7 3.9 O=C(NS(=O)(=O)C)COCCCCN(c1cnc(c(n1)c1ccccc1)c1ccccc1)C(C)C None
9913767 10351 79 None 1 4 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 496 12 1 7 3.9 O=C(NS(=O)(=O)C)COCCCCN(c1cnc(c(n1)c1ccccc1)c1ccccc1)C(C)C None
CHEMBL238804 10351 79 None 1 4 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 496 12 1 7 3.9 O=C(NS(=O)(=O)C)COCCCCN(c1cnc(c(n1)c1ccccc1)c1ccccc1)C(C)C None
DB11362 10351 79 None 1 4 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 496 12 1 7 3.9 O=C(NS(=O)(=O)C)COCCCCN(c1cnc(c(n1)c1ccccc1)c1ccccc1)C(C)C None
1884 9857 52 None -36 22 Rat 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 354 12 4 4 3.0 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O None
5280363 9857 52 None -36 22 Rat 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 354 12 4 4 3.0 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O None
912 9857 52 None -36 22 Rat 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 354 12 4 4 3.0 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O None
CHEMBL815 9857 52 None -36 22 Rat 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 354 12 4 4 3.0 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O None
DB12789 9857 52 None -36 22 Rat 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 354 12 4 4 3.0 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O None
138107701 194243 46 None -5 15 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 360 8 3 3 3.5 CC#CCC(C)[C@H](O)/C=C/[C@@H]1[C@H]2C/C(=C/CCCC(=O)O)C[C@H]2C[C@H]1O None
5311181 194243 46 None -5 15 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 360 8 3 3 3.5 CC#CCC(C)[C@H](O)/C=C/[C@@H]1[C@H]2C/C(=C/CCCC(=O)O)C[C@H]2C[C@H]1O None
CHEMBL494 194243 46 None -5 15 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 360 8 3 3 3.5 CC#CCC(C)[C@H](O)/C=C/[C@@H]1[C@H]2C/C(=C/CCCC(=O)O)C[C@H]2C[C@H]1O None
DB01088 194243 46 None -5 15 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 360 8 3 3 3.5 CC#CCC(C)[C@H](O)/C=C/[C@@H]1[C@H]2C/C(=C/CCCC(=O)O)C[C@H]2C[C@H]1O None
138107701 194243 46 None -5 15 Mouse 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 360 8 3 3 3.5 CC#CCC(C)[C@H](O)/C=C/[C@@H]1[C@H]2C/C(=C/CCCC(=O)O)C[C@H]2C[C@H]1O None
5311181 194243 46 None -5 15 Mouse 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 360 8 3 3 3.5 CC#CCC(C)[C@H](O)/C=C/[C@@H]1[C@H]2C/C(=C/CCCC(=O)O)C[C@H]2C[C@H]1O None
CHEMBL494 194243 46 None -5 15 Mouse 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 360 8 3 3 3.5 CC#CCC(C)[C@H](O)/C=C/[C@@H]1[C@H]2C/C(=C/CCCC(=O)O)C[C@H]2C[C@H]1O None
DB01088 194243 46 None -5 15 Mouse 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 360 8 3 3 3.5 CC#CCC(C)[C@H](O)/C=C/[C@@H]1[C@H]2C/C(=C/CCCC(=O)O)C[C@H]2C[C@H]1O None
1917 7714 0 None -22 9 Mouse 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 374 6 3 4 2.2 CCC#CC[C@@H]([C@@H](C#C[C@H]1[C@H](O)C[C@H]2[C@@H]1C/C(=C/COCC(=O)O)/C2)O)C None
5311044 7714 0 None -22 9 Mouse 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 374 6 3 4 2.2 CCC#CC[C@@H]([C@@H](C#C[C@H]1[C@H](O)C[C@H]2[C@@H]1C/C(=C/COCC(=O)O)/C2)O)C None
631 7714 0 None -22 9 Mouse 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 374 6 3 4 2.2 CCC#CC[C@@H]([C@@H](C#C[C@H]1[C@H](O)C[C@H]2[C@@H]1C/C(=C/COCC(=O)O)/C2)O)C None
CHEMBL160629 7714 0 None -22 9 Mouse 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 374 6 3 4 2.2 CCC#CC[C@@H]([C@@H](C#C[C@H]1[C@H](O)C[C@H]2[C@@H]1C/C(=C/COCC(=O)O)/C2)O)C None
138107701 194243 46 None -5 15 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 360 8 3 3 3.5 CC#CCC(C)[C@H](O)/C=C/[C@@H]1[C@H]2C/C(=C/CCCC(=O)O)C[C@H]2C[C@H]1O None
5311181 194243 46 None -5 15 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 360 8 3 3 3.5 CC#CCC(C)[C@H](O)/C=C/[C@@H]1[C@H]2C/C(=C/CCCC(=O)O)C[C@H]2C[C@H]1O None
CHEMBL494 194243 46 None -5 15 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 360 8 3 3 3.5 CC#CCC(C)[C@H](O)/C=C/[C@@H]1[C@H]2C/C(=C/CCCC(=O)O)C[C@H]2C[C@H]1O None
DB01088 194243 46 None -5 15 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 360 8 3 3 3.5 CC#CCC(C)[C@H](O)/C=C/[C@@H]1[C@H]2C/C(=C/CCCC(=O)O)C[C@H]2C[C@H]1O None
1884 9857 52 None -37 22 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 354 12 4 4 3.0 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O None
5280363 9857 52 None -37 22 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 354 12 4 4 3.0 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O None
912 9857 52 None -37 22 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 354 12 4 4 3.0 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O None
CHEMBL815 9857 52 None -37 22 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 354 12 4 4 3.0 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O None
DB12789 9857 52 None -37 22 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 354 12 4 4 3.0 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O None
656511 224495 0 None -1 7 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 539 6 3 8 -0.2 CC1(C)S[C@@H]2[C@H](NC(=O)[C@H](NC(=O)N3CCN(C3=O)S(C)(=O)=O)C3=CC=CC=C3)C(=O)N2[C@H]1C(O)=O None
3356 9060 73 None -53 8 Human 8.2 pKi = 8.2 Binding
Binding affinity to human EP2 receptor expressed in HEK293 cellsBinding affinity to human EP2 receptor expressed in HEK293 cells
Drug Central 435 5 1 4 4.4 OC(=O)C[C@H]1CCc2c1n(Cc1ccc(cc1)Cl)c1c2cc(cc1S(=O)(=O)C)F None
4326 9060 73 None -53 8 Human 8.2 pKi = 8.2 Binding
Binding affinity to human EP2 receptor expressed in HEK293 cellsBinding affinity to human EP2 receptor expressed in HEK293 cells
Drug Central 435 5 1 4 4.4 OC(=O)C[C@H]1CCc2c1n(Cc1ccc(cc1)Cl)c1c2cc(cc1S(=O)(=O)C)F None
9867642 9060 73 None -53 8 Human 8.2 pKi = 8.2 Binding
Binding affinity to human EP2 receptor expressed in HEK293 cellsBinding affinity to human EP2 receptor expressed in HEK293 cells
Drug Central 435 5 1 4 4.4 OC(=O)C[C@H]1CCc2c1n(Cc1ccc(cc1)Cl)c1c2cc(cc1S(=O)(=O)C)F None
CHEMBL426559 9060 73 None -53 8 Human 8.2 pKi = 8.2 Binding
Binding affinity to human EP2 receptor expressed in HEK293 cellsBinding affinity to human EP2 receptor expressed in HEK293 cells
Drug Central 435 5 1 4 4.4 OC(=O)C[C@H]1CCc2c1n(Cc1ccc(cc1)Cl)c1c2cc(cc1S(=O)(=O)C)F None
DB11629 9060 73 None -53 8 Human 8.2 pKi = 8.2 Binding
Binding affinity to human EP2 receptor expressed in HEK293 cellsBinding affinity to human EP2 receptor expressed in HEK293 cells
Drug Central 435 5 1 4 4.4 OC(=O)C[C@H]1CCc2c1n(Cc1ccc(cc1)Cl)c1c2cc(cc1S(=O)(=O)C)F None
123619 223172 0 None 125 27 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 358 3 0 4 4.2 CC1=NC=C(C=C1)C2=NC=C(C=C2C3=CC=C(C=C3)S(=O)(=O)C)Cl None
5090 22333 106 None 28 30 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 314 3 0 4 2.6 CS(=O)(=O)c1ccc(C2=C(c3ccccc3)C(=O)OC2)cc1 None
CHEMBL122 22333 106 None 28 30 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 314 3 0 4 2.6 CS(=O)(=O)c1ccc(C2=C(c3ccccc3)C(=O)OC2)cc1 None
1817 9320 68 None -7 12 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 382 13 2 5 4.0 CCCCC(C/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)OC)(O)C None
1936 9320 68 None -7 12 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 382 13 2 5 4.0 CCCCC(C/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)OC)(O)C None
5282381 9320 68 None -7 12 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 382 13 2 5 4.0 CCCCC(C/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)OC)(O)C None
CHEMBL606 9320 68 None -7 12 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 382 13 2 5 4.0 CCCCC(C/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)OC)(O)C None
DB00929 9320 68 None -7 12 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 382 13 2 5 4.0 CCCCC(C/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)OC)(O)C None
138 9855 88 None -19 18 Mouse 8.1 pKi = 8.1 Binding
Affinity for mouse Prostanoid EP2 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP2 receptor expressed in CHO cells
Drug Central 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O None
149351 9855 88 None -19 18 Mouse 8.1 pKi = 8.1 Binding
Affinity for mouse Prostanoid EP2 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP2 receptor expressed in CHO cells
Drug Central 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O None
1882 9855 88 None -19 18 Mouse 8.1 pKi = 8.1 Binding
Affinity for mouse Prostanoid EP2 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP2 receptor expressed in CHO cells
Drug Central 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O None
5280723 9855 88 None -19 18 Mouse 8.1 pKi = 8.1 Binding
Affinity for mouse Prostanoid EP2 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP2 receptor expressed in CHO cells
Drug Central 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O None
CHEMBL495 9855 88 None -19 18 Mouse 8.1 pKi = 8.1 Binding
Affinity for mouse Prostanoid EP2 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP2 receptor expressed in CHO cells
Drug Central 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O None
DB00770 9855 88 None -19 18 Mouse 8.1 pKi = 8.1 Binding
Affinity for mouse Prostanoid EP2 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP2 receptor expressed in CHO cells
Drug Central 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O None
1883 9856 75 None -15 24 Mouse 8.1 pKi = 8.1 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
Drug Central 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O None
1916 9856 75 None -15 24 Mouse 8.1 pKi = 8.1 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
Drug Central 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O None
5280360 9856 75 None -15 24 Mouse 8.1 pKi = 8.1 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
Drug Central 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O None
913 9856 75 None -15 24 Mouse 8.1 pKi = 8.1 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
Drug Central 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O None
CHEMBL548 9856 75 None -15 24 Mouse 8.1 pKi = 8.1 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
Drug Central 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O None
DB00917 9856 75 None -15 24 Mouse 8.1 pKi = 8.1 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
Drug Central 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O None
1440 8808 119 None 3 6 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 357 4 1 4 3.9 COc1ccc2c(c1)c(CC(=O)O)c(n2C(=O)c1ccc(cc1)Cl)C None
1909 8808 119 None 3 6 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 357 4 1 4 3.9 COc1ccc2c(c1)c(CC(=O)O)c(n2C(=O)c1ccc(cc1)Cl)C None
3715 8808 119 None 3 6 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 357 4 1 4 3.9 COc1ccc2c(c1)c(CC(=O)O)c(n2C(=O)c1ccc(cc1)Cl)C None
CHEMBL6 8808 119 None 3 6 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 357 4 1 4 3.9 COc1ccc2c(c1)c(CC(=O)O)c(n2C(=O)c1ccc(cc1)Cl)C None
DB00328 8808 119 None 3 6 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 357 4 1 4 3.9 COc1ccc2c(c1)c(CC(=O)O)c(n2C(=O)c1ccc(cc1)Cl)C None
138 9855 88 None -8 18 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O None
149351 9855 88 None -8 18 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O None
1882 9855 88 None -8 18 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O None
5280723 9855 88 None -8 18 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O None
CHEMBL495 9855 88 None -8 18 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O None
DB00770 9855 88 None -8 18 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O None
2720 10626 59 None -1 6 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 390 10 3 4 3.6 CCCCC[C@@H](CC[C@H]1[C@H](O)C[C@H]2[C@@H]1Cc1cccc(c1C2)OCC(=O)O)O None
5820 10626 59 None -1 6 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 390 10 3 4 3.6 CCCCC[C@@H](CC[C@H]1[C@H](O)C[C@H]2[C@@H]1Cc1cccc(c1C2)OCC(=O)O)O None
6918140 10626 59 None -1 6 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 390 10 3 4 3.6 CCCCC[C@@H](CC[C@H]1[C@H](O)C[C@H]2[C@@H]1Cc1cccc(c1C2)OCC(=O)O)O None
CHEMBL1237119 10626 59 None -1 6 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 390 10 3 4 3.6 CCCCC[C@@H](CC[C@H]1[C@H](O)C[C@H]2[C@@H]1Cc1cccc(c1C2)OCC(=O)O)O None
DB00374 10626 59 None -1 6 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 390 10 3 4 3.6 CCCCC[C@@H](CC[C@H]1[C@H](O)C[C@H]2[C@@H]1Cc1cccc(c1C2)OCC(=O)O)O None
1883 9856 75 None -6 24 Human 8.1 pKi = 8.1 Binding
Binding affinity to human prostanoid EP2 receptor by radioligand displacement assayBinding affinity to human prostanoid EP2 receptor by radioligand displacement assay
Drug Central 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O None
1916 9856 75 None -6 24 Human 8.1 pKi = 8.1 Binding
Binding affinity to human prostanoid EP2 receptor by radioligand displacement assayBinding affinity to human prostanoid EP2 receptor by radioligand displacement assay
Drug Central 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O None
5280360 9856 75 None -6 24 Human 8.1 pKi = 8.1 Binding
Binding affinity to human prostanoid EP2 receptor by radioligand displacement assayBinding affinity to human prostanoid EP2 receptor by radioligand displacement assay
Drug Central 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O None
913 9856 75 None -6 24 Human 8.1 pKi = 8.1 Binding
Binding affinity to human prostanoid EP2 receptor by radioligand displacement assayBinding affinity to human prostanoid EP2 receptor by radioligand displacement assay
Drug Central 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O None
CHEMBL548 9856 75 None -6 24 Human 8.1 pKi = 8.1 Binding
Binding affinity to human prostanoid EP2 receptor by radioligand displacement assayBinding affinity to human prostanoid EP2 receptor by radioligand displacement assay
Drug Central 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O None
DB00917 9856 75 None -6 24 Human 8.1 pKi = 8.1 Binding
Binding affinity to human prostanoid EP2 receptor by radioligand displacement assayBinding affinity to human prostanoid EP2 receptor by radioligand displacement assay
Drug Central 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O None
5852 9395 55 None -288 4 Human 5.2 pKi = 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 419 11 1 5 4.9 OC(=O)COCCCCN(c1cnc(c(n1)c1ccccc1)c1ccccc1)C(C)C 17545310
9931891 9395 55 None -288 4 Human 5.2 pKi = 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 419 11 1 5 4.9 OC(=O)COCCCCN(c1cnc(c(n1)c1ccccc1)c1ccccc1)C(C)C 17545310
CHEMBL239226 9395 55 None -288 4 Human 5.2 pKi = 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 419 11 1 5 4.9 OC(=O)COCCCCN(c1cnc(c(n1)c1ccccc1)c1ccccc1)C(C)C 17545310
1895 8788 0 None -125 16 Rat 5.9 pKi = 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 360 8 3 3 3.5 CC#CCC([C@@H](/C=C/C1[C@H](O)C[C@H]2[C@@H]1C/C(=C/CCCC(=O)O)/C2)O)C 9537820
6435378 8788 0 None -125 16 Rat 5.9 pKi = 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 360 8 3 3 3.5 CC#CCC([C@@H](/C=C/C1[C@H](O)C[C@H]2[C@@H]1C/C(=C/CCCC(=O)O)/C2)O)C 9537820
CHEMBL236025 8788 0 None -125 16 Rat 5.9 pKi = 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 360 8 3 3 3.5 CC#CCC([C@@H](/C=C/C1[C@H](O)C[C@H]2[C@@H]1C/C(=C/CCCC(=O)O)/C2)O)C 9537820
DB01088 8788 0 None -125 16 Rat 5.9 pKi = 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 360 8 3 3 3.5 CC#CCC([C@@H](/C=C/C1[C@H](O)C[C@H]2[C@@H]1C/C(=C/CCCC(=O)O)/C2)O)C 9537820
1892 7534 20 None -2 9 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 394 13 3 4 4.3 CCCC1(CCC1)[C@H](C/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 10462542
1892 7534 20 None -2 9 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 394 13 3 4 4.3 CCCC1(CCC1)[C@H](C/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 10634944
25886893 7534 20 None -2 9 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 394 13 3 4 4.3 CCCC1(CCC1)[C@H](C/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 10462542
25886893 7534 20 None -2 9 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 394 13 3 4 4.3 CCCC1(CCC1)[C@H](C/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 10634944
CHEMBL1628262 7534 20 None -2 9 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 394 13 3 4 4.3 CCCC1(CCC1)[C@H](C/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 10462542
CHEMBL1628262 7534 20 None -2 9 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 394 13 3 4 4.3 CCCC1(CCC1)[C@H](C/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 10634944
1883 9856 75 None -15 24 Mouse 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10746663
1883 9856 75 None -15 24 Mouse 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 14607240
1883 9856 75 None -15 24 Mouse 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 9313928
1916 9856 75 None -15 24 Mouse 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10746663
1916 9856 75 None -15 24 Mouse 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 14607240
1916 9856 75 None -15 24 Mouse 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 9313928
5280360 9856 75 None -15 24 Mouse 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10746663
5280360 9856 75 None -15 24 Mouse 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 14607240
5280360 9856 75 None -15 24 Mouse 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 9313928
913 9856 75 None -15 24 Mouse 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10746663
913 9856 75 None -15 24 Mouse 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 14607240
913 9856 75 None -15 24 Mouse 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 9313928
CHEMBL548 9856 75 None -15 24 Mouse 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10746663
CHEMBL548 9856 75 None -15 24 Mouse 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 14607240
CHEMBL548 9856 75 None -15 24 Mouse 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 9313928
DB00917 9856 75 None -15 24 Mouse 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10746663
DB00917 9856 75 None -15 24 Mouse 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 14607240
DB00917 9856 75 None -15 24 Mouse 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 9313928
1883 9856 75 None -6 24 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10462542
1883 9856 75 None -6 24 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10634944
1883 9856 75 None -6 24 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 16604093
1916 9856 75 None -6 24 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10462542
1916 9856 75 None -6 24 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10634944
1916 9856 75 None -6 24 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 16604093
5280360 9856 75 None -6 24 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10462542
5280360 9856 75 None -6 24 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10634944
5280360 9856 75 None -6 24 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 16604093
913 9856 75 None -6 24 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10462542
913 9856 75 None -6 24 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10634944
913 9856 75 None -6 24 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 16604093
CHEMBL548 9856 75 None -6 24 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10462542
CHEMBL548 9856 75 None -6 24 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10634944
CHEMBL548 9856 75 None -6 24 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 16604093
DB00917 9856 75 None -6 24 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10462542
DB00917 9856 75 None -6 24 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10634944
DB00917 9856 75 None -6 24 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 16604093
138 9855 88 None -19 18 Mouse 8.0 pKi = 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 9313928
138 9855 88 None -8 18 Rat 8.0 pKi = 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 9537820
149351 9855 88 None -19 18 Mouse 8.0 pKi = 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 9313928
149351 9855 88 None -8 18 Rat 8.0 pKi = 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 9537820
1882 9855 88 None -19 18 Mouse 8.0 pKi = 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 9313928
1882 9855 88 None -8 18 Rat 8.0 pKi = 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 9537820
5280723 9855 88 None -19 18 Mouse 8.0 pKi = 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 9313928
5280723 9855 88 None -8 18 Rat 8.0 pKi = 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 9537820
CHEMBL495 9855 88 None -19 18 Mouse 8.0 pKi = 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 9313928
CHEMBL495 9855 88 None -8 18 Rat 8.0 pKi = 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 9537820
DB00770 9855 88 None -19 18 Mouse 8.0 pKi = 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 9313928
DB00770 9855 88 None -8 18 Rat 8.0 pKi = 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 9537820
138 9855 88 None -9 18 Human 8.0 pKi = 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 8163486
149351 9855 88 None -9 18 Human 8.0 pKi = 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 8163486
1882 9855 88 None -9 18 Human 8.0 pKi = 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 8163486
5280723 9855 88 None -9 18 Human 8.0 pKi = 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 8163486
CHEMBL495 9855 88 None -9 18 Human 8.0 pKi = 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 8163486
DB00770 9855 88 None -9 18 Human 8.0 pKi = 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 8163486
1883 9856 75 None -7 24 Rat 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 9537820
1916 9856 75 None -7 24 Rat 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 9537820
5280360 9856 75 None -7 24 Rat 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 9537820
913 9856 75 None -7 24 Rat 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 9537820
CHEMBL548 9856 75 None -7 24 Rat 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 9537820
DB00917 9856 75 None -7 24 Rat 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 9537820
10110 9861 0 None - 1 Human 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 6 2 3 4.3 OC(=O)COc1cccc(c1)NC(=O)c1cc(ccc1F)c1cccc(c1)F 30341781
59654860 9861 0 None - 1 Human 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 6 2 3 4.3 OC(=O)COc1cccc(c1)NC(=O)c1cc(ccc1F)c1cccc(c1)F 30341781
2720 10626 59 None -1 6 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 390 10 3 4 3.6 CCCCC[C@@H](CC[C@H]1[C@H](O)C[C@H]2[C@@H]1Cc1cccc(c1C2)OCC(=O)O)O 22480736
2720 10626 59 None -1 6 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 390 10 3 4 3.6 CCCCC[C@@H](CC[C@H]1[C@H](O)C[C@H]2[C@@H]1Cc1cccc(c1C2)OCC(=O)O)O 25542069
5820 10626 59 None -1 6 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 390 10 3 4 3.6 CCCCC[C@@H](CC[C@H]1[C@H](O)C[C@H]2[C@@H]1Cc1cccc(c1C2)OCC(=O)O)O 22480736
5820 10626 59 None -1 6 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 390 10 3 4 3.6 CCCCC[C@@H](CC[C@H]1[C@H](O)C[C@H]2[C@@H]1Cc1cccc(c1C2)OCC(=O)O)O 25542069
6918140 10626 59 None -1 6 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 390 10 3 4 3.6 CCCCC[C@@H](CC[C@H]1[C@H](O)C[C@H]2[C@@H]1Cc1cccc(c1C2)OCC(=O)O)O 22480736
6918140 10626 59 None -1 6 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 390 10 3 4 3.6 CCCCC[C@@H](CC[C@H]1[C@H](O)C[C@H]2[C@@H]1Cc1cccc(c1C2)OCC(=O)O)O 25542069
CHEMBL1237119 10626 59 None -1 6 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 390 10 3 4 3.6 CCCCC[C@@H](CC[C@H]1[C@H](O)C[C@H]2[C@@H]1Cc1cccc(c1C2)OCC(=O)O)O 22480736
CHEMBL1237119 10626 59 None -1 6 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 390 10 3 4 3.6 CCCCC[C@@H](CC[C@H]1[C@H](O)C[C@H]2[C@@H]1Cc1cccc(c1C2)OCC(=O)O)O 25542069
DB00374 10626 59 None -1 6 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 390 10 3 4 3.6 CCCCC[C@@H](CC[C@H]1[C@H](O)C[C@H]2[C@@H]1Cc1cccc(c1C2)OCC(=O)O)O 22480736
DB00374 10626 59 None -1 6 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 390 10 3 4 3.6 CCCCC[C@@H](CC[C@H]1[C@H](O)C[C@H]2[C@@H]1Cc1cccc(c1C2)OCC(=O)O)O 25542069
10315 9700 28 None - 1 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 478 10 2 8 2.6 OC(=O)CNc1cccc(n1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)n1cccn1 29332128
44230575 9700 28 None - 1 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 478 10 2 8 2.6 OC(=O)CNc1cccc(n1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)n1cccn1 29332128
CHEMBL3707245 9700 28 None - 1 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 478 10 2 8 2.6 OC(=O)CNc1cccc(n1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)n1cccn1 29332128
1932 9716 5 None -1 6 Mouse 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 410 12 3 3 4.8 C=CCC1(CCC1)[C@H](C/C=C/[C@H]1[C@H](O)C[C@H]([C@@H]1C/C=C\CCCC(=O)O)Cl)O 10746663
5311228 9716 5 None -1 6 Mouse 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 410 12 3 3 4.8 C=CCC1(CCC1)[C@H](C/C=C/[C@H]1[C@H](O)C[C@H]([C@@H]1C/C=C\CCCC(=O)O)Cl)O 10746663
CHEMBL3286796 9716 5 None -1 6 Mouse 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 410 12 3 3 4.8 C=CCC1(CCC1)[C@H](C/C=C/[C@H]1[C@H](O)C[C@H]([C@@H]1C/C=C\CCCC(=O)O)Cl)O 10746663
1888 10672 29 None -501 17 Human 4.9 pKi None 4.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 350 12 2 3 4.3 CCCCC[C@@H](/C=C/[C@H]1[C@@H]2OC[C@H]([C@@H]1C/C=C\CCCC(=O)O)C2)O 10634944
1974 10672 29 None -501 17 Human 4.9 pKi None 4.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 350 12 2 3 4.3 CCCCC[C@@H](/C=C/[C@H]1[C@@H]2OC[C@H]([C@@H]1C/C=C\CCCC(=O)O)C2)O 10634944
5311493 10672 29 None -501 17 Human 4.9 pKi None 4.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 350 12 2 3 4.3 CCCCC[C@@H](/C=C/[C@H]1[C@@H]2OC[C@H]([C@@H]1C/C=C\CCCC(=O)O)C2)O 10634944
CHEMBL521784 10672 29 None -501 17 Human 4.9 pKi None 4.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 350 12 2 3 4.3 CCCCC[C@@H](/C=C/[C@H]1[C@@H]2OC[C@H]([C@@H]1C/C=C\CCCC(=O)O)C2)O 10634944
1817 9320 68 None -7 12 Human 5.0 pKi None 5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 382 13 2 5 4.0 CCCCC(C/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)OC)(O)C 10634944
1936 9320 68 None -7 12 Human 5.0 pKi None 5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 382 13 2 5 4.0 CCCCC(C/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)OC)(O)C 10634944
5282381 9320 68 None -7 12 Human 5.0 pKi None 5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 382 13 2 5 4.0 CCCCC(C/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)OC)(O)C 10634944
CHEMBL606 9320 68 None -7 12 Human 5.0 pKi None 5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 382 13 2 5 4.0 CCCCC(C/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)OC)(O)C 10634944
DB00929 9320 68 None -7 12 Human 5.0 pKi None 5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 382 13 2 5 4.0 CCCCC(C/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)OC)(O)C 10634944
1881 9853 0 None -4570 21 Human 5.0 pKi None 5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1C(=O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O 10462542
1891 9853 0 None -4570 21 Human 5.0 pKi None 5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1C(=O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O 10462542
448457 9853 0 None -4570 21 Human 5.0 pKi None 5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1C(=O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O 10462542
CHEMBL1235252 9853 0 None -4570 21 Human 5.0 pKi None 5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1C(=O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O 10462542
DB02056 9853 0 None -4570 21 Human 5.0 pKi None 5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1C(=O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O 10462542
1888 10672 29 None -316 17 Rat 5.1 pKi None 5.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 350 12 2 3 4.3 CCCCC[C@@H](/C=C/[C@H]1[C@@H]2OC[C@H]([C@@H]1C/C=C\CCCC(=O)O)C2)O 9537820
1974 10672 29 None -316 17 Rat 5.1 pKi None 5.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 350 12 2 3 4.3 CCCCC[C@@H](/C=C/[C@H]1[C@@H]2OC[C@H]([C@@H]1C/C=C\CCCC(=O)O)C2)O 9537820
5311493 10672 29 None -316 17 Rat 5.1 pKi None 5.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 350 12 2 3 4.3 CCCCC[C@@H](/C=C/[C@H]1[C@@H]2OC[C@H]([C@@H]1C/C=C\CCCC(=O)O)C2)O 9537820
CHEMBL521784 10672 29 None -316 17 Rat 5.1 pKi None 5.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 350 12 2 3 4.3 CCCCC[C@@H](/C=C/[C@H]1[C@@H]2OC[C@H]([C@@H]1C/C=C\CCCC(=O)O)C2)O 9537820
1881 9853 0 None -2290 21 Rat 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1C(=O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O 9537820
1891 9853 0 None -2290 21 Rat 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1C(=O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O 9537820
448457 9853 0 None -2290 21 Rat 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1C(=O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O 9537820
CHEMBL1235252 9853 0 None -2290 21 Rat 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1C(=O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O 9537820
DB02056 9853 0 None -2290 21 Rat 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1C(=O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O 9537820
1931 9720 0 None -371 2 Mouse 5.4 pKi None 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 380 14 1 4 4.6 CCCCC[C@@H](/C=C/[C@H]1[C@H](OC)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)OC 10746663
5311229 9720 0 None -371 2 Mouse 5.4 pKi None 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 380 14 1 4 4.6 CCCCC[C@@H](/C=C/[C@H]1[C@H](OC)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)OC 10746663
1884 9857 52 None -37 22 Human 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 12 4 4 3.0 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O 10462542
1884 9857 52 None -37 22 Human 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 12 4 4 3.0 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O 10634944
5280363 9857 52 None -37 22 Human 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 12 4 4 3.0 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O 10462542
5280363 9857 52 None -37 22 Human 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 12 4 4 3.0 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O 10634944
912 9857 52 None -37 22 Human 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 12 4 4 3.0 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O 10462542
912 9857 52 None -37 22 Human 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 12 4 4 3.0 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O 10634944
CHEMBL815 9857 52 None -37 22 Human 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 12 4 4 3.0 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O 10462542
CHEMBL815 9857 52 None -37 22 Human 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 12 4 4 3.0 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O 10634944
DB12789 9857 52 None -37 22 Human 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 12 4 4 3.0 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O 10462542
DB12789 9857 52 None -37 22 Human 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 12 4 4 3.0 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O 10634944
1884 9857 52 None -36 22 Rat 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 12 4 4 3.0 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O 9537820
5280363 9857 52 None -36 22 Rat 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 12 4 4 3.0 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O 9537820
912 9857 52 None -36 22 Rat 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 12 4 4 3.0 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O 9537820
CHEMBL815 9857 52 None -36 22 Rat 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 12 4 4 3.0 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O 9537820
DB12789 9857 52 None -36 22 Rat 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 12 4 4 3.0 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O 9537820
1913 9242 0 None -15848 15 Human 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 374 12 2 4 4.0 OC(=O)CCCCCC[C@@H]1[C@@H](/C=C/[C@H](COc2ccccc2)O)CCC1=O 10462542
1913 9242 0 None -15848 15 Human 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 374 12 2 4 4.0 OC(=O)CCCCCC[C@@H]1[C@@H](/C=C/[C@H](COc2ccccc2)O)CCC1=O 10634944
5311223 9242 0 None -15848 15 Human 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 374 12 2 4 4.0 OC(=O)CCCCCC[C@@H]1[C@@H](/C=C/[C@H](COc2ccccc2)O)CCC1=O 10462542
5311223 9242 0 None -15848 15 Human 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 374 12 2 4 4.0 OC(=O)CCCCCC[C@@H]1[C@@H](/C=C/[C@H](COc2ccccc2)O)CCC1=O 10634944
1895 8788 0 None -199 16 Human 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 360 8 3 3 3.5 CC#CCC([C@@H](/C=C/C1[C@H](O)C[C@H]2[C@@H]1C/C(=C/CCCC(=O)O)/C2)O)C 10634944
6435378 8788 0 None -199 16 Human 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 360 8 3 3 3.5 CC#CCC([C@@H](/C=C/C1[C@H](O)C[C@H]2[C@@H]1C/C(=C/CCCC(=O)O)/C2)O)C 10634944
CHEMBL236025 8788 0 None -199 16 Human 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 360 8 3 3 3.5 CC#CCC([C@@H](/C=C/C1[C@H](O)C[C@H]2[C@@H]1C/C(=C/CCCC(=O)O)/C2)O)C 10634944
DB01088 8788 0 None -199 16 Human 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 360 8 3 3 3.5 CC#CCC([C@@H](/C=C/C1[C@H](O)C[C@H]2[C@@H]1C/C(=C/CCCC(=O)O)/C2)O)C 10634944
1933 9717 0 None -199 3 Mouse 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 468 14 3 7 2.9 COCc1ccccc1CC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1SCCCSCC(=O)O)O 10746663
5311230 9717 0 None -199 3 Mouse 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 468 14 3 7 2.9 COCc1ccccc1CC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1SCCCSCC(=O)O)O 10746663
1893 7582 0 None -112 13 Mouse 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 350 10 3 3 4.1 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)C[C@H]2[C@@H]1C/C(=C\CCCC(=O)O)/C2)O 9313928
5311242 7582 0 None -112 13 Mouse 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 350 10 3 3 4.1 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)C[C@H]2[C@@H]1C/C(=C\CCCC(=O)O)/C2)O 9313928
CHEMBL148319 7582 0 None -112 13 Mouse 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 350 10 3 3 4.1 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)C[C@H]2[C@@H]1C/C(=C\CCCC(=O)O)/C2)O 9313928
1895 8788 0 None -158 16 Mouse 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 360 8 3 3 3.5 CC#CCC([C@@H](/C=C/C1[C@H](O)C[C@H]2[C@@H]1C/C(=C/CCCC(=O)O)/C2)O)C 9313928
6435378 8788 0 None -158 16 Mouse 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 360 8 3 3 3.5 CC#CCC([C@@H](/C=C/C1[C@H](O)C[C@H]2[C@@H]1C/C(=C/CCCC(=O)O)/C2)O)C 9313928
CHEMBL236025 8788 0 None -158 16 Mouse 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 360 8 3 3 3.5 CC#CCC([C@@H](/C=C/C1[C@H](O)C[C@H]2[C@@H]1C/C(=C/CCCC(=O)O)/C2)O)C 9313928
DB01088 8788 0 None -158 16 Mouse 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 360 8 3 3 3.5 CC#CCC([C@@H](/C=C/C1[C@H](O)C[C@H]2[C@@H]1C/C(=C/CCCC(=O)O)/C2)O)C 9313928
1947 6817 0 None -39 3 Human 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 368 12 4 5 2.2 O[C@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)CCC[C@H](O)C 8078484
5283038 6817 0 None -39 3 Human 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 368 12 4 5 2.2 O[C@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)CCC[C@H](O)C 8078484
119461 7108 72 None -3 10 Human 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 298 3 1 4 3.4 CC(Oc1ccc2c(c1)oc1c(c2=O)cc(cc1)C(=O)O)C 10634944
1896 7108 72 None -3 10 Human 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 298 3 1 4 3.4 CC(Oc1ccc2c(c1)oc1c(c2=O)cc(cc1)C(=O)O)C 10634944
CHEMBL1317823 7108 72 None -3 10 Human 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 298 3 1 4 3.4 CC(Oc1ccc2c(c1)oc1c(c2=O)cc(cc1)C(=O)O)C 10634944
1917 7714 0 None -22 9 Mouse 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 374 6 3 4 2.2 CCC#CC[C@@H]([C@@H](C#C[C@H]1[C@H](O)C[C@H]2[C@@H]1C/C(=C/COCC(=O)O)/C2)O)C 9313928
5311044 7714 0 None -22 9 Mouse 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 374 6 3 4 2.2 CCC#CC[C@@H]([C@@H](C#C[C@H]1[C@H](O)C[C@H]2[C@@H]1C/C(=C/COCC(=O)O)/C2)O)C 9313928
631 7714 0 None -22 9 Mouse 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 374 6 3 4 2.2 CCC#CC[C@@H]([C@@H](C#C[C@H]1[C@H](O)C[C@H]2[C@@H]1C/C(=C/COCC(=O)O)/C2)O)C 9313928
CHEMBL160629 7714 0 None -22 9 Mouse 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 374 6 3 4 2.2 CCC#CC[C@@H]([C@@H](C#C[C@H]1[C@H](O)C[C@H]2[C@@H]1C/C(=C/COCC(=O)O)/C2)O)C 9313928
1913 9242 0 None -8912 15 Rat 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 374 12 2 4 4.0 OC(=O)CCCCCC[C@@H]1[C@@H](/C=C/[C@H](COc2ccccc2)O)CCC1=O 9537820
5311223 9242 0 None -8912 15 Rat 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 374 12 2 4 4.0 OC(=O)CCCCCC[C@@H]1[C@@H](/C=C/[C@H](COc2ccccc2)O)CCC1=O 9537820
1928 7105 0 None -12 3 Human 6.0 pKi None 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 388 13 2 3 5.8 CCCCCC(c1ccc(cc1)C1CCC(=O)C1CCCCCCC(=O)O)O 10462542
5310998 7105 0 None -12 3 Human 6.0 pKi None 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 388 13 2 3 5.8 CCCCCC(c1ccc(cc1)C1CCC(=O)C1CCCCCCC(=O)O)O 10462542
1893 7582 0 None -70 13 Human 6.0 pKi None 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 350 10 3 3 4.1 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)C[C@H]2[C@@H]1C/C(=C\CCCC(=O)O)/C2)O 10634944
5311242 7582 0 None -70 13 Human 6.0 pKi None 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 350 10 3 3 4.1 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)C[C@H]2[C@@H]1C/C(=C\CCCC(=O)O)/C2)O 10634944
CHEMBL148319 7582 0 None -70 13 Human 6.0 pKi None 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 350 10 3 3 4.1 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)C[C@H]2[C@@H]1C/C(=C\CCCC(=O)O)/C2)O 10634944
1934 8871 0 None -63 3 Mouse 6.0 pKi None 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 350 11 3 3 4.1 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)C[C@H]2[C@@H]1CC(=C2)CCCCC(=O)O)O 9313928
5311244 8871 0 None -63 3 Mouse 6.0 pKi None 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 350 11 3 3 4.1 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)C[C@H]2[C@@H]1CC(=C2)CCCCC(=O)O)O 9313928
CHEMBL4522827 8871 0 None -63 3 Mouse 6.0 pKi None 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 350 11 3 3 4.1 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)C[C@H]2[C@@H]1CC(=C2)CCCCC(=O)O)O 9313928
1912 6815 0 None -213 6 Rat 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 386 11 3 4 3.3 OC(=O)CCC/C=C\C[C@H]1C(=O)C[C@H]([C@@H]1/C=C/[C@H](CCc1ccccc1)O)O 9537820
5283068 6815 0 None -213 6 Rat 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 386 11 3 4 3.3 OC(=O)CCC/C=C\C[C@H]1C(=O)C[C@H]([C@@H]1/C=C/[C@H](CCc1ccccc1)O)O 9537820
CHEMBL1879970 6815 0 None -213 6 Rat 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 386 11 3 4 3.3 OC(=O)CCC/C=C\C[C@H]1C(=O)C[C@H]([C@@H]1/C=C/[C@H](CCc1ccccc1)O)O 9537820
1930 10106 25 None -999 3 Mouse 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 450 13 2 7 2.9 COCc1cccc(c1)C[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCSCCCC(=O)OC)O 11917107
9803828 10106 25 None -999 3 Mouse 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 450 13 2 7 2.9 COCc1cccc(c1)C[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCSCCCC(=O)OC)O 11917107
CHEMBL303960 10106 25 None -999 3 Mouse 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 450 13 2 7 2.9 COCc1cccc(c1)C[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCSCCCC(=O)OC)O 11917107
DB16315 10106 25 None -999 3 Mouse 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 450 13 2 7 2.9 COCc1cccc(c1)C[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCSCCCC(=O)OC)O 11917107
119461 7108 72 None -1 10 Rat 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 298 3 1 4 3.4 CC(Oc1ccc2c(c1)oc1c(c2=O)cc(cc1)C(=O)O)C 9537820
1896 7108 72 None -1 10 Rat 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 298 3 1 4 3.4 CC(Oc1ccc2c(c1)oc1c(c2=O)cc(cc1)C(=O)O)C 9537820
CHEMBL1317823 7108 72 None -1 10 Rat 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 298 3 1 4 3.4 CC(Oc1ccc2c(c1)oc1c(c2=O)cc(cc1)C(=O)O)C 9537820
119461 7108 72 None 1 10 Mouse 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 298 3 1 4 3.4 CC(Oc1ccc2c(c1)oc1c(c2=O)cc(cc1)C(=O)O)C 9313928
1896 7108 72 None 1 10 Mouse 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 298 3 1 4 3.4 CC(Oc1ccc2c(c1)oc1c(c2=O)cc(cc1)C(=O)O)C 9313928
CHEMBL1317823 7108 72 None 1 10 Mouse 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 298 3 1 4 3.4 CC(Oc1ccc2c(c1)oc1c(c2=O)cc(cc1)C(=O)O)C 9313928
1928 7105 0 None -3 3 Mouse 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 388 13 2 3 5.8 CCCCCC(c1ccc(cc1)C1CCC(=O)C1CCCCCCC(=O)O)O 9313928
5310998 7105 0 None -3 3 Mouse 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 388 13 2 3 5.8 CCCCCC(c1ccc(cc1)C1CCC(=O)C1CCCCCCC(=O)O)O 9313928
1947 6817 0 None -5 3 Rat 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 368 12 4 5 2.2 O[C@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)CCC[C@H](O)C 9537820
5283038 6817 0 None -5 3 Rat 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 368 12 4 5 2.2 O[C@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)CCC[C@H](O)C 9537820
1892 7534 20 None 2 9 Rat 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 394 13 3 4 4.3 CCCC1(CCC1)[C@H](C/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 9537820
25886893 7534 20 None 2 9 Rat 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 394 13 3 4 4.3 CCCC1(CCC1)[C@H](C/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 9537820
CHEMBL1628262 7534 20 None 2 9 Rat 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 394 13 3 4 4.3 CCCC1(CCC1)[C@H](C/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 9537820
1925 6796 0 None -39 6 Mouse 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 13 2 3 4.5 CCCCC[C@@H](/C=C/[C@H]1CCC(=O)[C@@H]1CCCCCCC(=O)O)O 9313928
5283055 6796 0 None -39 6 Mouse 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 13 2 3 4.5 CCCCC[C@@H](/C=C/[C@H]1CCC(=O)[C@@H]1CCCCCCC(=O)O)O 9313928
CHEMBL3246389 6796 0 None -39 6 Mouse 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 13 2 3 4.5 CCCCC[C@@H](/C=C/[C@H]1CCC(=O)[C@@H]1CCCCCCC(=O)O)O 9313928
1925 6796 0 None -25 6 Rat 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 13 2 3 4.5 CCCCC[C@@H](/C=C/[C@H]1CCC(=O)[C@@H]1CCCCCCC(=O)O)O 9537820
5283055 6796 0 None -25 6 Rat 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 13 2 3 4.5 CCCCC[C@@H](/C=C/[C@H]1CCC(=O)[C@@H]1CCCCCCC(=O)O)O 9537820
CHEMBL3246389 6796 0 None -25 6 Rat 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 13 2 3 4.5 CCCCC[C@@H](/C=C/[C@H]1CCC(=O)[C@@H]1CCCCCCC(=O)O)O 9537820
1935 9319 0 None -3 3 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 368 13 3 4 3.9 CCCCC(C/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)(O)C 10634944
6436406 9319 0 None -3 3 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 368 13 3 4 3.9 CCCCC(C/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)(O)C 10634944
CHEMBL1201377 9319 0 None -3 3 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 368 13 3 4 3.9 CCCCC(C/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)(O)C 10634944
1926 6813 0 None -8 3 Mouse 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 380 12 3 4 3.9 CCCCC([C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O)(C)C 9313928
5283066 6813 0 None -8 3 Mouse 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 380 12 3 4 3.9 CCCCC([C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O)(C)C 9313928
CHEMBL1221529 6813 0 None -8 3 Mouse 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 380 12 3 4 3.9 CCCCC([C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O)(C)C 9313928