Ligand source activities (1 row/activity)



Get vendors


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
90656213 117680 0 None 1 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation counting
ChEMBL 635 13 7 13 -0.3 O=c1[nH]/c(=N\OCCCc2cccc(F)c2)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm500367e
CHEMBL3261362 117680 0 None 1 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation counting
ChEMBL 635 13 7 13 -0.3 O=c1[nH]/c(=N\OCCCc2cccc(F)c2)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm500367e
1734 10738 50 None -1 7 Human 7.0 pEC50 = 7 Functional
Agonist activity evaluated as change in the level of cytosolic calcium in 1321N astrocytoma cells infected with a retrovirus encoding the human P2Y4 receptorAgonist activity evaluated as change in the level of cytosolic calcium in 1321N astrocytoma cells infected with a retrovirus encoding the human P2Y4 receptor
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1016/s0960-894x(00)00612-0
3639 10738 50 None -1 7 Human 7.0 pEC50 = 7 Functional
Agonist activity evaluated as change in the level of cytosolic calcium in 1321N astrocytoma cells infected with a retrovirus encoding the human P2Y4 receptorAgonist activity evaluated as change in the level of cytosolic calcium in 1321N astrocytoma cells infected with a retrovirus encoding the human P2Y4 receptor
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1016/s0960-894x(00)00612-0
6133 10738 50 None -1 7 Human 7.0 pEC50 = 7 Functional
Agonist activity evaluated as change in the level of cytosolic calcium in 1321N astrocytoma cells infected with a retrovirus encoding the human P2Y4 receptorAgonist activity evaluated as change in the level of cytosolic calcium in 1321N astrocytoma cells infected with a retrovirus encoding the human P2Y4 receptor
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1016/s0960-894x(00)00612-0
CHEMBL336296 10738 50 None -1 7 Human 7.0 pEC50 = 7 Functional
Agonist activity evaluated as change in the level of cytosolic calcium in 1321N astrocytoma cells infected with a retrovirus encoding the human P2Y4 receptorAgonist activity evaluated as change in the level of cytosolic calcium in 1321N astrocytoma cells infected with a retrovirus encoding the human P2Y4 receptor
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1016/s0960-894x(00)00612-0
DB04005 10738 50 None -1 7 Human 7.0 pEC50 = 7 Functional
Agonist activity evaluated as change in the level of cytosolic calcium in 1321N astrocytoma cells infected with a retrovirus encoding the human P2Y4 receptorAgonist activity evaluated as change in the level of cytosolic calcium in 1321N astrocytoma cells infected with a retrovirus encoding the human P2Y4 receptor
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1016/s0960-894x(00)00612-0
1731 6918 11 None -10 3 Human 5.0 pEC50 = 5 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as calcium elevation by fura2/AM assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as calcium elevation by fura2/AM assay
ChEMBL 562 8 7 12 -1.7 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cc(Br)c(=O)[nH]c1=O 10.1021/jm901450d
9872620 6918 11 None -10 3 Human 5.0 pEC50 = 5 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as calcium elevation by fura2/AM assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as calcium elevation by fura2/AM assay
ChEMBL 562 8 7 12 -1.7 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cc(Br)c(=O)[nH]c1=O 10.1021/jm901450d
CHEMBL384527 6918 11 None -10 3 Human 5.0 pEC50 = 5 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as calcium elevation by fura2/AM assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as calcium elevation by fura2/AM assay
ChEMBL 562 8 7 12 -1.7 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cc(Br)c(=O)[nH]c1=O 10.1021/jm901450d
90656214 117681 0 None 5 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation counting
ChEMBL 635 13 7 13 -0.3 O=c1[nH]/c(=N\OCCCc2ccc(F)cc2)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm500367e
CHEMBL3261363 117681 0 None 5 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation counting
ChEMBL 635 13 7 13 -0.3 O=c1[nH]/c(=N\OCCCc2ccc(F)cc2)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm500367e
54584406 69694 0 None 4 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human P2Y4Agonist activity at human P2Y4
ChEMBL 509 9 6 12 -1.2 [N-]=[N+]=N[C@@H]1[C@H](O)[C@@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)O[C@H]1n1ccc(=O)[nH]c1=O 10.1021/jm101591j
CHEMBL1784888 69694 0 None 4 2 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human P2Y4Agonist activity at human P2Y4
ChEMBL 509 9 6 12 -1.2 [N-]=[N+]=N[C@@H]1[C@H](O)[C@@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)O[C@H]1n1ccc(=O)[nH]c1=O 10.1021/jm101591j
44586045 190927 0 None 1 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 638 14 9 17 -3.0 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)OCC(O)CO)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1016/j.bmc.2008.05.013
CHEMBL482895 190927 0 None 1 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 638 14 9 17 -3.0 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)OCC(O)CO)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1016/j.bmc.2008.05.013
90656216 117683 0 None 2 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation counting
ChEMBL 743 13 7 13 0.2 O=c1[nH]/c(=N\OCCCc2cccc(I)c2)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm500367e
CHEMBL3261365 117683 0 None 2 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation counting
ChEMBL 743 13 7 13 0.2 O=c1[nH]/c(=N\OCCCc2cccc(I)c2)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm500367e
46831686 20973 0 None -3 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assay
ChEMBL 509 9 6 11 -0.9 O=c1[nH]/c(=N\OCc2ccccc2)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm100287t
CHEMBL1084612 20973 0 None -3 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assay
ChEMBL 509 9 6 11 -0.9 O=c1[nH]/c(=N\OCc2ccccc2)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm100287t
CHEMBL1198872 20973 0 None -3 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assay
ChEMBL 509 9 6 11 -0.9 O=c1[nH]/c(=N\OCc2ccccc2)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm100287t
CHEMBL4866937 20973 0 None -3 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assay
ChEMBL 509 9 6 11 -0.9 O=c1[nH]/c(=N\OCc2ccccc2)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm100287t
46831686 20973 0 None -3 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells using [3H]inositol as substrate assessed as [3H]inositol phosphate formation after 30 mins by liquid scintillation counting analysisAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells using [3H]inositol as substrate assessed as [3H]inositol phosphate formation after 30 mins by liquid scintillation counting analysis
ChEMBL 509 9 6 11 -0.9 O=c1[nH]/c(=N\OCc2ccccc2)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1039/c3md00132f
CHEMBL1084612 20973 0 None -3 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells using [3H]inositol as substrate assessed as [3H]inositol phosphate formation after 30 mins by liquid scintillation counting analysisAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells using [3H]inositol as substrate assessed as [3H]inositol phosphate formation after 30 mins by liquid scintillation counting analysis
ChEMBL 509 9 6 11 -0.9 O=c1[nH]/c(=N\OCc2ccccc2)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1039/c3md00132f
CHEMBL1198872 20973 0 None -3 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells using [3H]inositol as substrate assessed as [3H]inositol phosphate formation after 30 mins by liquid scintillation counting analysisAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells using [3H]inositol as substrate assessed as [3H]inositol phosphate formation after 30 mins by liquid scintillation counting analysis
ChEMBL 509 9 6 11 -0.9 O=c1[nH]/c(=N\OCc2ccccc2)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1039/c3md00132f
CHEMBL4866937 20973 0 None -3 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells using [3H]inositol as substrate assessed as [3H]inositol phosphate formation after 30 mins by liquid scintillation counting analysisAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells using [3H]inositol as substrate assessed as [3H]inositol phosphate formation after 30 mins by liquid scintillation counting analysis
ChEMBL 509 9 6 11 -0.9 O=c1[nH]/c(=N\OCc2ccccc2)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1039/c3md00132f
11525909 148383 5 None -19 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 483 8 7 12 -2.5 N[C@@H]1[C@H](O)[C@@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)O[C@H]1n1ccc(=O)[nH]c1=O 10.1016/j.bmc.2008.05.013
CHEMBL385098 148383 5 None -19 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 483 8 7 12 -2.5 N[C@@H]1[C@H](O)[C@@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)O[C@H]1n1ccc(=O)[nH]c1=O 10.1016/j.bmc.2008.05.013
11525909 148383 5 None -19 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase CAgonist activity at human recombinant P2Y4 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase C
ChEMBL 483 8 7 12 -2.5 N[C@@H]1[C@H](O)[C@@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)O[C@H]1n1ccc(=O)[nH]c1=O 10.1021/jm060903o
CHEMBL385098 148383 5 None -19 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase CAgonist activity at human recombinant P2Y4 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase C
ChEMBL 483 8 7 12 -2.5 N[C@@H]1[C@H](O)[C@@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)O[C@H]1n1ccc(=O)[nH]c1=O 10.1021/jm060903o
44586007 199374 1 None 1 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 498 8 7 12 -2.1 C[C@@]1(O)[C@H](O)[C@@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)O[C@H]1n1ccc(=O)[nH]c1=O 10.1016/j.bmc.2008.05.013
CHEMBL521487 199374 1 None 1 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 498 8 7 12 -2.1 C[C@@]1(O)[C@H](O)[C@@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)O[C@H]1n1ccc(=O)[nH]c1=O 10.1016/j.bmc.2008.05.013
90656225 117692 0 None -1 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation counting
ChEMBL 667 13 7 13 0.8 O=c1[nH]/c(=N\OCCCc2ccc3ccccc3c2)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm500367e
CHEMBL3261374 117692 0 None -1 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation counting
ChEMBL 667 13 7 13 0.8 O=c1[nH]/c(=N\OCCCc2ccc3ccccc3c2)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm500367e
148197 8220 23 None -1 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 790 14 10 21 -4.2 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1016/j.bmc.2008.05.013
1736 8220 23 None -1 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 790 14 10 21 -4.2 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1016/j.bmc.2008.05.013
4900 8220 23 None -1 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 790 14 10 21 -4.2 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1016/j.bmc.2008.05.013
CHEMBL221326 8220 23 None -1 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 790 14 10 21 -4.2 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1016/j.bmc.2008.05.013
DB15919 8220 23 None -1 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 790 14 10 21 -4.2 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1016/j.bmc.2008.05.013
nan 8220 23 None -1 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 790 14 10 21 -4.2 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1016/j.bmc.2008.05.013
148197 8220 23 None -1 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase CAgonist activity at human recombinant P2Y4 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase C
ChEMBL 790 14 10 21 -4.2 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm060903o
1736 8220 23 None -1 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase CAgonist activity at human recombinant P2Y4 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase C
ChEMBL 790 14 10 21 -4.2 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm060903o
4900 8220 23 None -1 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase CAgonist activity at human recombinant P2Y4 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase C
ChEMBL 790 14 10 21 -4.2 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm060903o
CHEMBL221326 8220 23 None -1 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase CAgonist activity at human recombinant P2Y4 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase C
ChEMBL 790 14 10 21 -4.2 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm060903o
DB15919 8220 23 None -1 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase CAgonist activity at human recombinant P2Y4 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase C
ChEMBL 790 14 10 21 -4.2 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm060903o
nan 8220 23 None -1 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase CAgonist activity at human recombinant P2Y4 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase C
ChEMBL 790 14 10 21 -4.2 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm060903o
148197 8220 23 None -1 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 790 14 10 21 -4.2 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm101591j
1736 8220 23 None -1 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 790 14 10 21 -4.2 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm101591j
4900 8220 23 None -1 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 790 14 10 21 -4.2 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm101591j
CHEMBL221326 8220 23 None -1 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 790 14 10 21 -4.2 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm101591j
DB15919 8220 23 None -1 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 790 14 10 21 -4.2 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm101591j
nan 8220 23 None -1 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 790 14 10 21 -4.2 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm101591j
1737 8149 7 None -2 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 773 14 9 21 -2.9 Nc1ccn(c(=O)n1)[C@@H]1O[C@@H]([C@H](C1)O)COP(=O)(OP(=O)(OP(=O)(OP(=O)(OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1ccc(=O)[nH]c1=O)O)O)O)O 10.1016/j.bmc.2008.05.013
9875516 8149 7 None -2 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 773 14 9 21 -2.9 Nc1ccn(c(=O)n1)[C@@H]1O[C@@H]([C@H](C1)O)COP(=O)(OP(=O)(OP(=O)(OP(=O)(OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1ccc(=O)[nH]c1=O)O)O)O)O 10.1016/j.bmc.2008.05.013
CHEMBL507282 8149 7 None -2 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 773 14 9 21 -2.9 Nc1ccn(c(=O)n1)[C@@H]1O[C@@H]([C@H](C1)O)COP(=O)(OP(=O)(OP(=O)(OP(=O)(OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1ccc(=O)[nH]c1=O)O)O)O)O 10.1016/j.bmc.2008.05.013
DB04983 8149 7 None -2 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 773 14 9 21 -2.9 Nc1ccn(c(=O)n1)[C@@H]1O[C@@H]([C@H](C1)O)COP(=O)(OP(=O)(OP(=O)(OP(=O)(OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1ccc(=O)[nH]c1=O)O)O)O)O 10.1016/j.bmc.2008.05.013
146015339 10694 32 None -234 7 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assay
ChEMBL 404 6 6 10 -2.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm1016297
1749 10694 32 None -234 7 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assay
ChEMBL 404 6 6 10 -2.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm1016297
6031 10694 32 None -234 7 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assay
ChEMBL 404 6 6 10 -2.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm1016297
CHEMBL130266 10694 32 None -234 7 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assay
ChEMBL 404 6 6 10 -2.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm1016297
DB03435 10694 32 None -234 7 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assay
ChEMBL 404 6 6 10 -2.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm1016297
90656215 117682 0 None 1 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation counting
ChEMBL 695 13 7 13 0.4 O=c1[nH]/c(=N\OCCCc2ccc(Br)cc2)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm500367e
CHEMBL3261364 117682 0 None 1 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation counting
ChEMBL 695 13 7 13 0.4 O=c1[nH]/c(=N\OCCCc2ccc(Br)cc2)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm500367e
52952280 68112 0 None -2 3 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assay
ChEMBL 434 7 5 11 -1.2 CSc1nc(=O)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm1016297
CHEMBL1767410 68112 0 None -2 3 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assay
ChEMBL 434 7 5 11 -1.2 CSc1nc(=O)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm1016297
CHEMBL2029010 215927 0 None -1 3 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human P2Y purinoceptor 4 expressed in human 1321N1 cells assessed as increase in intracellular calcium concentration by spectrofluorimetryAgonist activity at human P2Y purinoceptor 4 expressed in human 1321N1 cells assessed as increase in intracellular calcium concentration by spectrofluorimetry
ChEMBL None None None BP(=O)(OC[C@H]1O[C@@H](n2ccc(=O)[nH]c2=O)[C@H](O)[C@@H]1O)OP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]1O[C@@H](n2ccc(=O)[nH]c2=O)[C@H](O)[C@@H]1O.CCCCN(CCCC)CCCC.CCCCN(CCCC)CCCC.CCCCN(CCCC)CCCC.CCCCN(CCCC)CCCC 10.1021/jm2013198
10174453 6878 5 None -17 3 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human P2Y4 receptor expressed in 1321N1 cells assessed as IP accumulation by SPAAgonist activity at human P2Y4 receptor expressed in 1321N1 cells assessed as IP accumulation by SPA
ChEMBL 500 8 7 12 -1.1 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=S 10.1021/jm060848j
3398 6878 5 None -17 3 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human P2Y4 receptor expressed in 1321N1 cells assessed as IP accumulation by SPAAgonist activity at human P2Y4 receptor expressed in 1321N1 cells assessed as IP accumulation by SPA
ChEMBL 500 8 7 12 -1.1 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=S 10.1021/jm060848j
CHEMBL217803 6878 5 None -17 3 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human P2Y4 receptor expressed in 1321N1 cells assessed as IP accumulation by SPAAgonist activity at human P2Y4 receptor expressed in 1321N1 cells assessed as IP accumulation by SPA
ChEMBL 500 8 7 12 -1.1 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=S 10.1021/jm060848j
44585519 176765 0 None 1 3 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 726 13 11 20 -4.6 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)O[C@H]3O[C@H](CO)[C@H](O)[C@H](O)[C@H]3O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1016/j.bmc.2008.05.013
CHEMBL444212 176765 0 None 1 3 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 726 13 11 20 -4.6 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)O[C@H]3O[C@H](CO)[C@H](O)[C@H](O)[C@H]3O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1016/j.bmc.2008.05.013
44585519 176765 0 None 1 3 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 726 13 11 20 -4.6 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)O[C@H]3O[C@H](CO)[C@H](O)[C@H](O)[C@H]3O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm101591j
CHEMBL444212 176765 0 None 1 3 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 726 13 11 20 -4.6 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)O[C@H]3O[C@H](CO)[C@H](O)[C@H](O)[C@H]3O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm101591j
46831384 20971 0 None 1 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assay
ChEMBL 447 8 6 11 -2.1 CCO/N=c1/ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm100287t
CHEMBL1084295 20971 0 None 1 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assay
ChEMBL 447 8 6 11 -2.1 CCO/N=c1/ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm100287t
CHEMBL1198862 20971 0 None 1 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assay
ChEMBL 447 8 6 11 -2.1 CCO/N=c1/ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm100287t
1713 7308 68 None -20 10 Rat 5.8 pEC50 = 5.8 Functional
The compound was evaluated for agonist activity against phospholipase C coupled recombinant rat P2Y purinoceptor 4 (P2Y4)The compound was evaluated for agonist activity against phospholipase C coupled recombinant rat P2Y purinoceptor 4 (P2Y4)
ChEMBL 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N 10.1021/jm020046y
5957 7308 68 None -20 10 Rat 5.8 pEC50 = 5.8 Functional
The compound was evaluated for agonist activity against phospholipase C coupled recombinant rat P2Y purinoceptor 4 (P2Y4)The compound was evaluated for agonist activity against phospholipase C coupled recombinant rat P2Y purinoceptor 4 (P2Y4)
ChEMBL 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N 10.1021/jm020046y
91 7308 68 None -20 10 Rat 5.8 pEC50 = 5.8 Functional
The compound was evaluated for agonist activity against phospholipase C coupled recombinant rat P2Y purinoceptor 4 (P2Y4)The compound was evaluated for agonist activity against phospholipase C coupled recombinant rat P2Y purinoceptor 4 (P2Y4)
ChEMBL 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N 10.1021/jm020046y
CHEMBL14249 7308 68 None -20 10 Rat 5.8 pEC50 = 5.8 Functional
The compound was evaluated for agonist activity against phospholipase C coupled recombinant rat P2Y purinoceptor 4 (P2Y4)The compound was evaluated for agonist activity against phospholipase C coupled recombinant rat P2Y purinoceptor 4 (P2Y4)
ChEMBL 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N 10.1021/jm020046y
DB00171 7308 68 None -20 10 Rat 5.8 pEC50 = 5.8 Functional
The compound was evaluated for agonist activity against phospholipase C coupled recombinant rat P2Y purinoceptor 4 (P2Y4)The compound was evaluated for agonist activity against phospholipase C coupled recombinant rat P2Y purinoceptor 4 (P2Y4)
ChEMBL 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N 10.1021/jm020046y
53309244 69691 0 None 4 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 726 13 11 20 -4.6 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)O[C@H]3O[C@H](CO)[C@@H](O)[C@@H](O)[C@H]3O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm101591j
CHEMBL1784885 69691 0 None 4 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 726 13 11 20 -4.6 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)O[C@H]3O[C@H](CO)[C@@H](O)[C@@H](O)[C@H]3O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm101591j
44586044 191077 0 None -1 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 617 13 7 16 -1.4 N#CCCOP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]1O[C@@H](n2ccc(=O)[nH]c2=O)[C@H](O)[C@@H]1O 10.1016/j.bmc.2008.05.013
CHEMBL484105 191077 0 None -1 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 617 13 7 16 -1.4 N#CCCOP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]1O[C@@H](n2ccc(=O)[nH]c2=O)[C@H](O)[C@@H]1O 10.1016/j.bmc.2008.05.013
44586044 191077 0 None -1 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 617 13 7 16 -1.4 N#CCCOP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]1O[C@@H](n2ccc(=O)[nH]c2=O)[C@H](O)[C@@H]1O 10.1021/jm101591j
CHEMBL484105 191077 0 None -1 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 617 13 7 16 -1.4 N#CCCOP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]1O[C@@H](n2ccc(=O)[nH]c2=O)[C@H](O)[C@@H]1O 10.1021/jm101591j
90656223 117690 0 None 5 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation counting
ChEMBL 623 13 7 14 -0.3 O=c1[nH]/c(=N\OCCCc2ccsc2)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm500367e
CHEMBL3261372 117690 0 None 5 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation counting
ChEMBL 623 13 7 14 -0.3 O=c1[nH]/c(=N\OCCCc2ccsc2)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm500367e
90656229 119584 0 None 1 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation counting
ChEMBL 1400 31 14 27 1.7 N=c1ccc2c(-c3ccc(C(=O)NCCCCCCn4cc(CCNC(=O)COc5ccc(CCCO/N=c6/ccn([C@@H]7O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]7O)c(=O)[nH]6)cc5)nn4)cc3C(=O)O)c3ccc(N)c(S(=O)(=O)O)c3oc-2c1S(=O)(=O)O 10.1021/jm500367e
CHEMBL3261377 119584 0 None 1 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation counting
ChEMBL 1400 31 14 27 1.7 N=c1ccc2c(-c3ccc(C(=O)NCCCCCCn4cc(CCNC(=O)COc5ccc(CCCO/N=c6/ccn([C@@H]7O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]7O)c(=O)[nH]6)cc5)nn4)cc3C(=O)O)c3ccc(N)c(S(=O)(=O)O)c3oc-2c1S(=O)(=O)O 10.1021/jm500367e
CHEMBL3306844 119584 0 None 1 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation counting
ChEMBL 1400 31 14 27 1.7 N=c1ccc2c(-c3ccc(C(=O)NCCCCCCn4cc(CCNC(=O)COc5ccc(CCCO/N=c6/ccn([C@@H]7O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]7O)c(=O)[nH]6)cc5)nn4)cc3C(=O)O)c3ccc(N)c(S(=O)(=O)O)c3oc-2c1S(=O)(=O)O 10.1021/jm500367e
44439758 98045 0 None -1995 2 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human cloned P2Y4 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human cloned P2Y4 receptor expressed in human 1321N1 by FLIPR assay
ChEMBL 551 8 6 11 0.6 O=c1c2cc(Cl)ccc2ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1016/j.bmcl.2006.09.017
CHEMBL240201 98045 0 None -1995 2 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human cloned P2Y4 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human cloned P2Y4 receptor expressed in human 1321N1 by FLIPR assay
ChEMBL 551 8 6 11 0.6 O=c1c2cc(Cl)ccc2ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1016/j.bmcl.2006.09.017
44585518 194988 0 None -6 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 726 13 11 20 -4.6 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)O[C@H]3O[C@H](CO)[C@@H](O)[C@H](O)[C@H]3O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1016/j.bmc.2008.05.013
CHEMBL499138 194988 0 None -6 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 726 13 11 20 -4.6 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)O[C@H]3O[C@H](CO)[C@@H](O)[C@H](O)[C@H]3O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1016/j.bmc.2008.05.013
44585518 194988 0 None -6 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 726 13 11 20 -4.6 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)O[C@H]3O[C@H](CO)[C@@H](O)[C@H](O)[C@H]3O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm101591j
CHEMBL499138 194988 0 None -6 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 726 13 11 20 -4.6 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)O[C@H]3O[C@H](CO)[C@@H](O)[C@H](O)[C@H]3O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm101591j
53308826 69696 0 None 3 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 527 10 7 13 -2.0 CCO/N=c1/ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm101591j
CHEMBL1784890 69696 0 None 3 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 527 10 7 13 -2.0 CCO/N=c1/ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm101591j
53308961 69697 0 None -1 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 555 9 7 13 -1.2 CC(C)(C)O/N=c1/ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm101591j
CHEMBL1784891 69697 0 None -1 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 555 9 7 13 -1.2 CC(C)(C)O/N=c1/ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm101591j
53309530 69634 0 None 2 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 728 13 10 19 -3.6 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)O[C@H]3O[C@H](CO)[C@@H](F)[C@H](O)[C@H]3O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm101591j
CHEMBL1784293 69634 0 None 2 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 728 13 10 19 -3.6 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)O[C@H]3O[C@H](CO)[C@@H](F)[C@H](O)[C@H]3O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm101591j
90666793 116202 0 None -53 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells using [3H]inositol as substrate assessed as [3H]inositol phosphate formation after 30 mins by liquid scintillation counting analysisAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells using [3H]inositol as substrate assessed as [3H]inositol phosphate formation after 30 mins by liquid scintillation counting analysis
ChEMBL 554 10 6 13 -1.0 O=c1[nH]/c(=N\OCc2ccc([N+](=O)[O-])cc2)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1039/c3md00132f
CHEMBL3220050 116202 0 None -53 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells using [3H]inositol as substrate assessed as [3H]inositol phosphate formation after 30 mins by liquid scintillation counting analysisAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells using [3H]inositol as substrate assessed as [3H]inositol phosphate formation after 30 mins by liquid scintillation counting analysis
ChEMBL 554 10 6 13 -1.0 O=c1[nH]/c(=N\OCc2ccc([N+](=O)[O-])cc2)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1039/c3md00132f
53309381 69703 0 None 2 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 740 13 11 20 -4.5 O=C(O)[C@H]1O[C@H](OP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]2O[C@@H](n3ccc(=O)[nH]c3=O)[C@H](O)[C@@H]2O)[C@H](O)[C@@H](O)[C@@H]1O 10.1021/jm101591j
CHEMBL1784902 69703 0 None 2 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 740 13 11 20 -4.5 O=C(O)[C@H]1O[C@H](OP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]2O[C@@H](n3ccc(=O)[nH]c3=O)[C@H](O)[C@@H]2O)[C@H](O)[C@@H](O)[C@@H]1O 10.1021/jm101591j
1730 6913 10 None 3 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at P2Y4 receptorAgonist activity at P2Y4 receptor
ChEMBL 500 8 7 12 -1.1 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=S)[nH]c1=O 10.1021/jm1016297
3033941 6913 10 None 3 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at P2Y4 receptorAgonist activity at P2Y4 receptor
ChEMBL 500 8 7 12 -1.1 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=S)[nH]c1=O 10.1021/jm1016297
CHEMBL1767409 6913 10 None 3 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at P2Y4 receptorAgonist activity at P2Y4 receptor
ChEMBL 500 8 7 12 -1.1 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=S)[nH]c1=O 10.1021/jm1016297
90656220 117687 0 None 2 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation counting
ChEMBL 647 14 7 14 -0.4 COc1ccc(CCCO/N=c2/ccn([C@@H]3O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]3O)c(=O)[nH]2)cc1 10.1021/jm500367e
CHEMBL3261369 117687 0 None 2 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation counting
ChEMBL 647 14 7 14 -0.4 COc1ccc(CCCO/N=c2/ccn([C@@H]3O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]3O)c(=O)[nH]2)cc1 10.1021/jm500367e
1730 6913 10 None 3 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assay
ChEMBL 500 8 7 12 -1.1 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=S)[nH]c1=O 10.1021/jm1016297
3033941 6913 10 None 3 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assay
ChEMBL 500 8 7 12 -1.1 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=S)[nH]c1=O 10.1021/jm1016297
CHEMBL1767409 6913 10 None 3 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assay
ChEMBL 500 8 7 12 -1.1 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=S)[nH]c1=O 10.1021/jm1016297
4044 9443 3 None 26 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 617 13 7 13 -0.4 O[C@@H]1[C@H](O)[C@H](O[C@H]1n1cc/c(=N/OCCCc2ccccc2)/[nH]c1=O)COP(=O)(OP(=O)(OP(=O)(O)O)O)O 10.1021/jm101591j
53262902 9443 3 None 26 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 617 13 7 13 -0.4 O[C@@H]1[C@H](O)[C@H](O[C@H]1n1cc/c(=N/OCCCc2ccccc2)/[nH]c1=O)COP(=O)(OP(=O)(OP(=O)(O)O)O)O 10.1021/jm101591j
CHEMBL1784894 9443 3 None 26 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 617 13 7 13 -0.4 O[C@@H]1[C@H](O)[C@H](O[C@H]1n1cc/c(=N/OCCCc2ccccc2)/[nH]c1=O)COP(=O)(OP(=O)(OP(=O)(O)O)O)O 10.1021/jm101591j
16116566 9434 10 None -301 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 499 8 7 12 -1.2 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1N)n1ccc(=O)[nH]c1=S 10.1016/j.bmc.2008.05.013
1733 9434 10 None -301 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 499 8 7 12 -1.2 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1N)n1ccc(=O)[nH]c1=S 10.1016/j.bmc.2008.05.013
CHEMBL373780 9434 10 None -301 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 499 8 7 12 -1.2 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1N)n1ccc(=O)[nH]c1=S 10.1016/j.bmc.2008.05.013
16116566 9434 10 None -301 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase CAgonist activity at human recombinant P2Y4 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase C
ChEMBL 499 8 7 12 -1.2 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1N)n1ccc(=O)[nH]c1=S 10.1021/jm060903o
1733 9434 10 None -301 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase CAgonist activity at human recombinant P2Y4 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase C
ChEMBL 499 8 7 12 -1.2 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1N)n1ccc(=O)[nH]c1=S 10.1021/jm060903o
CHEMBL373780 9434 10 None -301 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase CAgonist activity at human recombinant P2Y4 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase C
ChEMBL 499 8 7 12 -1.2 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1N)n1ccc(=O)[nH]c1=S 10.1021/jm060903o
46831692 20968 0 None 1 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 513 9 7 13 -2.4 CO/N=c1\ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm101591j
CHEMBL1083764 20968 0 None 1 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 513 9 7 13 -2.4 CO/N=c1\ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm101591j
CHEMBL1198849 20968 0 None 1 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 513 9 7 13 -2.4 CO/N=c1\ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm101591j
46831692 20968 0 None 1 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells using [3H]inositol as substrate assessed as [3H]inositol phosphate formation after 30 mins by liquid scintillation counting analysisAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells using [3H]inositol as substrate assessed as [3H]inositol phosphate formation after 30 mins by liquid scintillation counting analysis
ChEMBL 513 9 7 13 -2.4 CO/N=c1\ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1039/c3md00132f
CHEMBL1083764 20968 0 None 1 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells using [3H]inositol as substrate assessed as [3H]inositol phosphate formation after 30 mins by liquid scintillation counting analysisAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells using [3H]inositol as substrate assessed as [3H]inositol phosphate formation after 30 mins by liquid scintillation counting analysis
ChEMBL 513 9 7 13 -2.4 CO/N=c1\ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1039/c3md00132f
CHEMBL1198849 20968 0 None 1 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells using [3H]inositol as substrate assessed as [3H]inositol phosphate formation after 30 mins by liquid scintillation counting analysisAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells using [3H]inositol as substrate assessed as [3H]inositol phosphate formation after 30 mins by liquid scintillation counting analysis
ChEMBL 513 9 7 13 -2.4 CO/N=c1\ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1039/c3md00132f
90656222 117689 0 None 1 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation counting
ChEMBL 618 13 7 14 -1.0 O=c1[nH]/c(=N\OCCCc2ccncc2)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm500367e
CHEMBL3261371 117689 0 None 1 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation counting
ChEMBL 618 13 7 14 -1.0 O=c1[nH]/c(=N\OCCCc2ccncc2)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm500367e
1734 10738 50 None -1 7 Human 5.6 pEC50 = 5.6 Functional
The compound was evaluated for antagonist activity against phospholipase C coupled recombinant human P2Y purinoceptor 4 (P2Y4)The compound was evaluated for antagonist activity against phospholipase C coupled recombinant human P2Y purinoceptor 4 (P2Y4)
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm020046y
3639 10738 50 None -1 7 Human 5.6 pEC50 = 5.6 Functional
The compound was evaluated for antagonist activity against phospholipase C coupled recombinant human P2Y purinoceptor 4 (P2Y4)The compound was evaluated for antagonist activity against phospholipase C coupled recombinant human P2Y purinoceptor 4 (P2Y4)
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm020046y
6133 10738 50 None -1 7 Human 5.6 pEC50 = 5.6 Functional
The compound was evaluated for antagonist activity against phospholipase C coupled recombinant human P2Y purinoceptor 4 (P2Y4)The compound was evaluated for antagonist activity against phospholipase C coupled recombinant human P2Y purinoceptor 4 (P2Y4)
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm020046y
CHEMBL336296 10738 50 None -1 7 Human 5.6 pEC50 = 5.6 Functional
The compound was evaluated for antagonist activity against phospholipase C coupled recombinant human P2Y purinoceptor 4 (P2Y4)The compound was evaluated for antagonist activity against phospholipase C coupled recombinant human P2Y purinoceptor 4 (P2Y4)
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm020046y
DB04005 10738 50 None -1 7 Human 5.6 pEC50 = 5.6 Functional
The compound was evaluated for antagonist activity against phospholipase C coupled recombinant human P2Y purinoceptor 4 (P2Y4)The compound was evaluated for antagonist activity against phospholipase C coupled recombinant human P2Y purinoceptor 4 (P2Y4)
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm020046y
44586043 191054 0 None 1 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 562 10 7 14 -1.7 CP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]1O[C@@H](n2ccc(=O)[nH]c2=O)[C@H](O)[C@@H]1O 10.1016/j.bmc.2008.05.013
CHEMBL483913 191054 0 None 1 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 562 10 7 14 -1.7 CP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]1O[C@@H](n2ccc(=O)[nH]c2=O)[C@H](O)[C@@H]1O 10.1016/j.bmc.2008.05.013
53309242 69702 0 None 1 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 685 13 7 17 -0.4 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)Oc3cccc([N+](=O)[O-])c3)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm101591j
CHEMBL1784900 69702 0 None 1 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 685 13 7 17 -0.4 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)Oc3cccc([N+](=O)[O-])c3)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm101591j
1734 10738 50 None -3 7 Rat 5.6 pEC50 = 5.6 Functional
The compound was evaluated for antagonist activity against phospholipase C coupled recombinant rat P2Y purinoceptor 4 (P2Y4)The compound was evaluated for antagonist activity against phospholipase C coupled recombinant rat P2Y purinoceptor 4 (P2Y4)
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm020046y
3639 10738 50 None -3 7 Rat 5.6 pEC50 = 5.6 Functional
The compound was evaluated for antagonist activity against phospholipase C coupled recombinant rat P2Y purinoceptor 4 (P2Y4)The compound was evaluated for antagonist activity against phospholipase C coupled recombinant rat P2Y purinoceptor 4 (P2Y4)
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm020046y
6133 10738 50 None -3 7 Rat 5.6 pEC50 = 5.6 Functional
The compound was evaluated for antagonist activity against phospholipase C coupled recombinant rat P2Y purinoceptor 4 (P2Y4)The compound was evaluated for antagonist activity against phospholipase C coupled recombinant rat P2Y purinoceptor 4 (P2Y4)
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm020046y
CHEMBL336296 10738 50 None -3 7 Rat 5.6 pEC50 = 5.6 Functional
The compound was evaluated for antagonist activity against phospholipase C coupled recombinant rat P2Y purinoceptor 4 (P2Y4)The compound was evaluated for antagonist activity against phospholipase C coupled recombinant rat P2Y purinoceptor 4 (P2Y4)
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm020046y
DB04005 10738 50 None -3 7 Rat 5.6 pEC50 = 5.6 Functional
The compound was evaluated for antagonist activity against phospholipase C coupled recombinant rat P2Y purinoceptor 4 (P2Y4)The compound was evaluated for antagonist activity against phospholipase C coupled recombinant rat P2Y purinoceptor 4 (P2Y4)
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm020046y
44586042 198675 0 None 1 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 578 11 7 15 -1.7 COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]1O[C@@H](n2ccc(=O)[nH]c2=O)[C@H](O)[C@@H]1O 10.1016/j.bmc.2008.05.013
CHEMBL519991 198675 0 None 1 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 578 11 7 15 -1.7 COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]1O[C@@H](n2ccc(=O)[nH]c2=O)[C@H](O)[C@@H]1O 10.1016/j.bmc.2008.05.013
44586042 198675 0 None 1 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 578 11 7 15 -1.7 COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]1O[C@@H](n2ccc(=O)[nH]c2=O)[C@H](O)[C@@H]1O 10.1021/jm101591j
CHEMBL519991 198675 0 None 1 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 578 11 7 15 -1.7 COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]1O[C@@H](n2ccc(=O)[nH]c2=O)[C@H](O)[C@@H]1O 10.1021/jm101591j
44586026 199370 1 None -4 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 580 10 8 14 -1.0 O=c1[nH]c(=S)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1016/j.bmc.2008.05.013
CHEMBL521451 199370 1 None -4 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 580 10 8 14 -1.0 O=c1[nH]c(=S)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1016/j.bmc.2008.05.013
44417696 87930 0 None -5 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human P2Y4 receptor expressed in 1321N1 cells assessed as IP accumulation by SPAAgonist activity at human P2Y4 receptor expressed in 1321N1 cells assessed as IP accumulation by SPA
ChEMBL 498 8 6 13 -2.5 Cn1c(=O)ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c1=O 10.1021/jm060848j
CHEMBL215783 87930 0 None -5 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human P2Y4 receptor expressed in 1321N1 cells assessed as IP accumulation by SPAAgonist activity at human P2Y4 receptor expressed in 1321N1 cells assessed as IP accumulation by SPA
ChEMBL 498 8 6 13 -2.5 Cn1c(=O)ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c1=O 10.1021/jm060848j
90656221 117688 0 None 1 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation counting
ChEMBL 618 13 7 14 -1.0 O=c1[nH]/c(=N\OCCCc2cccnc2)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm500367e
CHEMBL3261370 117688 0 None 1 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation counting
ChEMBL 618 13 7 14 -1.0 O=c1[nH]/c(=N\OCCCc2cccnc2)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm500367e
46890063 20964 0 None -3 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assay
ChEMBL 494 8 7 11 -2.1 O=c1ccn([C@@]23C[C@H]2[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]3O)c(=O)[nH]1 10.1021/jm100287t
CHEMBL1083148 20964 0 None -3 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assay
ChEMBL 494 8 7 11 -2.1 O=c1ccn([C@@]23C[C@H]2[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]3O)c(=O)[nH]1 10.1021/jm100287t
CHEMBL1198833 20964 0 None -3 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assay
ChEMBL 494 8 7 11 -2.1 O=c1ccn([C@@]23C[C@H]2[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]3O)c(=O)[nH]1 10.1021/jm100287t
21706 123925 15 None -5 2 Rat 5.5 pEC50 = 5.5 Functional
The compound was evaluated for antagonist activity against phospholipase C coupled recombinant rat P2Y purinoceptor 4 (P2Y4)The compound was evaluated for antagonist activity against phospholipase C coupled recombinant rat P2Y purinoceptor 4 (P2Y4)
ChEMBL 836 14 10 25 -2.4 Nc1ncnc2c1ncn2[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]2O[C@@H](n3cnc4c(N)ncnc43)[C@H](O)[C@@H]2O)[C@@H](O)[C@H]1O 10.1021/jm020046y
CHEMBL339385 123925 15 None -5 2 Rat 5.5 pEC50 = 5.5 Functional
The compound was evaluated for antagonist activity against phospholipase C coupled recombinant rat P2Y purinoceptor 4 (P2Y4)The compound was evaluated for antagonist activity against phospholipase C coupled recombinant rat P2Y purinoceptor 4 (P2Y4)
ChEMBL 836 14 10 25 -2.4 Nc1ncnc2c1ncn2[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]2O[C@@H](n3cnc4c(N)ncnc43)[C@H](O)[C@@H]2O)[C@@H](O)[C@H]1O 10.1021/jm020046y
53309529 69633 0 None 1 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 757 14 10 20 -3.5 CO/N=c1/ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)O[C@H]3O[C@H](CO)[C@@H](O)[C@H](F)[C@H]3O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm101591j
CHEMBL1784292 69633 0 None 1 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 757 14 10 20 -3.5 CO/N=c1/ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)O[C@H]3O[C@H](CO)[C@@H](O)[C@H](F)[C@H]3O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm101591j
15485121 20952 0 None -3 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in 1321N1 cells assessed as PLC-mediated [3H]IP productionAgonist activity at human recombinant P2Y4 receptor expressed in 1321N1 cells assessed as PLC-mediated [3H]IP production
ChEMBL 388 6 5 9 -1.6 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)O)C[C@H]2O)c(=O)[nH]1 10.1021/jm060485n
CHEMBL1198709 20952 0 None -3 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in 1321N1 cells assessed as PLC-mediated [3H]IP productionAgonist activity at human recombinant P2Y4 receptor expressed in 1321N1 cells assessed as PLC-mediated [3H]IP production
ChEMBL 388 6 5 9 -1.6 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)O)C[C@H]2O)c(=O)[nH]1 10.1021/jm060485n
CHEMBL612021 20952 0 None -3 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in 1321N1 cells assessed as PLC-mediated [3H]IP productionAgonist activity at human recombinant P2Y4 receptor expressed in 1321N1 cells assessed as PLC-mediated [3H]IP production
ChEMBL 388 6 5 9 -1.6 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)O)C[C@H]2O)c(=O)[nH]1 10.1021/jm060485n
90666802 116207 0 None -3 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells using [3H]inositol as substrate assessed as [3H]inositol phosphate formation after 30 mins by liquid scintillation counting analysisAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells using [3H]inositol as substrate assessed as [3H]inositol phosphate formation after 30 mins by liquid scintillation counting analysis
ChEMBL 769 18 7 18 -0.8 CC(=O)NCCn1cc(CCOP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]2O[C@@H](n3cc/c(=N/OCc4ccccc4)[nH]c3=O)[C@H](O)[C@@H]2O)nn1 10.1039/c3md00132f
CHEMBL3220058 116207 0 None -3 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells using [3H]inositol as substrate assessed as [3H]inositol phosphate formation after 30 mins by liquid scintillation counting analysisAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells using [3H]inositol as substrate assessed as [3H]inositol phosphate formation after 30 mins by liquid scintillation counting analysis
ChEMBL 769 18 7 18 -0.8 CC(=O)NCCn1cc(CCOP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]2O[C@@H](n3cc/c(=N/OCc4ccccc4)[nH]c3=O)[C@H](O)[C@@H]2O)nn1 10.1039/c3md00132f
1731 6918 11 None -10 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human P2Y4 receptor expressed in 1321N1 cells assessed as IP accumulation by SPAAgonist activity at human P2Y4 receptor expressed in 1321N1 cells assessed as IP accumulation by SPA
ChEMBL 562 8 7 12 -1.7 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cc(Br)c(=O)[nH]c1=O 10.1021/jm060848j
9872620 6918 11 None -10 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human P2Y4 receptor expressed in 1321N1 cells assessed as IP accumulation by SPAAgonist activity at human P2Y4 receptor expressed in 1321N1 cells assessed as IP accumulation by SPA
ChEMBL 562 8 7 12 -1.7 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cc(Br)c(=O)[nH]c1=O 10.1021/jm060848j
CHEMBL384527 6918 11 None -10 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human P2Y4 receptor expressed in 1321N1 cells assessed as IP accumulation by SPAAgonist activity at human P2Y4 receptor expressed in 1321N1 cells assessed as IP accumulation by SPA
ChEMBL 562 8 7 12 -1.7 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cc(Br)c(=O)[nH]c1=O 10.1021/jm060848j
10174453 6878 5 None -17 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 500 8 7 12 -1.1 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=S 10.1016/j.bmc.2008.05.013
3398 6878 5 None -17 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 500 8 7 12 -1.1 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=S 10.1016/j.bmc.2008.05.013
CHEMBL217803 6878 5 None -17 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 500 8 7 12 -1.1 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=S 10.1016/j.bmc.2008.05.013
10174453 6878 5 None -17 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase CAgonist activity at human recombinant P2Y4 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase C
ChEMBL 500 8 7 12 -1.1 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=S 10.1021/jm060903o
3398 6878 5 None -17 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase CAgonist activity at human recombinant P2Y4 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase C
ChEMBL 500 8 7 12 -1.1 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=S 10.1021/jm060903o
CHEMBL217803 6878 5 None -17 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase CAgonist activity at human recombinant P2Y4 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase C
ChEMBL 500 8 7 12 -1.1 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=S 10.1021/jm060903o
10174453 6878 5 None -17 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 500 8 7 12 -1.1 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=S 10.1021/jm101591j
3398 6878 5 None -17 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 500 8 7 12 -1.1 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=S 10.1021/jm101591j
CHEMBL217803 6878 5 None -17 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 500 8 7 12 -1.1 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=S 10.1021/jm101591j
10432343 206158 4 None -1 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as concentration required to 50% maximal response of compound 3 at 10 uM by fura2/AM assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as concentration required to 50% maximal response of compound 3 at 10 uM by fura2/AM assay
ChEMBL 422 6 6 10 -2.5 O=c1[nH]c(=O)n([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)cc1F 10.1021/jm901450d
CHEMBL590981 206158 4 None -1 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as concentration required to 50% maximal response of compound 3 at 10 uM by fura2/AM assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as concentration required to 50% maximal response of compound 3 at 10 uM by fura2/AM assay
ChEMBL 422 6 6 10 -2.5 O=c1[nH]c(=O)n([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)cc1F 10.1021/jm901450d
90666790 116199 0 None -18 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells using [3H]inositol as substrate assessed as [3H]inositol phosphate formation after 30 mins by liquid scintillation counting analysisAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells using [3H]inositol as substrate assessed as [3H]inositol phosphate formation after 30 mins by liquid scintillation counting analysis
ChEMBL 635 9 6 11 -0.3 O=c1[nH]/c(=N\OCc2cccc(I)c2)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1039/c3md00132f
CHEMBL3220047 116199 0 None -18 3 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells using [3H]inositol as substrate assessed as [3H]inositol phosphate formation after 30 mins by liquid scintillation counting analysisAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells using [3H]inositol as substrate assessed as [3H]inositol phosphate formation after 30 mins by liquid scintillation counting analysis
ChEMBL 635 9 6 11 -0.3 O=c1[nH]/c(=N\OCc2cccc(I)c2)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1039/c3md00132f
44439757 161231 0 None -707 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human cloned P2Y4 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human cloned P2Y4 receptor expressed in human 1321N1 by FLIPR assay
ChEMBL 535 8 6 11 0.1 O=c1c2cc(F)ccc2ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1016/j.bmcl.2006.09.017
CHEMBL399017 161231 0 None -707 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human cloned P2Y4 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human cloned P2Y4 receptor expressed in human 1321N1 by FLIPR assay
ChEMBL 535 8 6 11 0.1 O=c1c2cc(F)ccc2ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1016/j.bmcl.2006.09.017
44585987 198581 0 None 2 3 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assay
ChEMBL 566 8 7 11 0.1 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)C(Cl)(Cl)P(=O)(O)O)[C@@H](O)[C@H]2O)c(=S)[nH]1 10.1021/jm1016297
CHEMBL519835 198581 0 None 2 3 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assay
ChEMBL 566 8 7 11 0.1 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)C(Cl)(Cl)P(=O)(O)O)[C@@H](O)[C@H]2O)c(=S)[nH]1 10.1021/jm1016297
1734 10738 50 None -1 7 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human cloned P2Y4 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human cloned P2Y4 receptor expressed in human 1321N1 by FLIPR assay
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1016/j.bmcl.2006.09.017
1734 10738 50 None -1 7 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human cloned P2Y4 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human cloned P2Y4 receptor expressed in human 1321N1 by FLIPR assay
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1016/j.bmcl.2006.10.038
3639 10738 50 None -1 7 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human cloned P2Y4 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human cloned P2Y4 receptor expressed in human 1321N1 by FLIPR assay
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1016/j.bmcl.2006.09.017
3639 10738 50 None -1 7 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human cloned P2Y4 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human cloned P2Y4 receptor expressed in human 1321N1 by FLIPR assay
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1016/j.bmcl.2006.10.038
6133 10738 50 None -1 7 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human cloned P2Y4 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human cloned P2Y4 receptor expressed in human 1321N1 by FLIPR assay
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1016/j.bmcl.2006.09.017
6133 10738 50 None -1 7 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human cloned P2Y4 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human cloned P2Y4 receptor expressed in human 1321N1 by FLIPR assay
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1016/j.bmcl.2006.10.038
CHEMBL336296 10738 50 None -1 7 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human cloned P2Y4 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human cloned P2Y4 receptor expressed in human 1321N1 by FLIPR assay
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1016/j.bmcl.2006.09.017
CHEMBL336296 10738 50 None -1 7 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human cloned P2Y4 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human cloned P2Y4 receptor expressed in human 1321N1 by FLIPR assay
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1016/j.bmcl.2006.10.038
DB04005 10738 50 None -1 7 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human cloned P2Y4 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human cloned P2Y4 receptor expressed in human 1321N1 by FLIPR assay
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1016/j.bmcl.2006.09.017
DB04005 10738 50 None -1 7 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human cloned P2Y4 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human cloned P2Y4 receptor expressed in human 1321N1 by FLIPR assay
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1016/j.bmcl.2006.10.038
451388 91006 6 None -27 3 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase CAgonist activity at human recombinant P2Y4 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase C
ChEMBL 498 8 7 12 -2.2 Cc1cn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c(=O)[nH]c1=O 10.1021/jm060903o
CHEMBL220940 91006 6 None -27 3 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase CAgonist activity at human recombinant P2Y4 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase C
ChEMBL 498 8 7 12 -2.2 Cc1cn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c(=O)[nH]c1=O 10.1021/jm060903o
52952604 67859 0 None -3 3 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assay
ChEMBL 636 11 6 13 -0.4 O=C(Cn1c(=O)ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)C(F)(F)P(=O)(O)O)[C@@H](O)[C@H]2O)c1=O)c1ccccc1 10.1021/jm1016297
CHEMBL1765118 67859 0 None -3 3 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assay
ChEMBL 636 11 6 13 -0.4 O=C(Cn1c(=O)ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)C(F)(F)P(=O)(O)O)[C@@H](O)[C@H]2O)c1=O)c1ccccc1 10.1021/jm1016297
11993891 89211 0 None -33 3 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human P2Y4 receptor expressed in 1321N1 cells assessed as IP accumulation by SPAAgonist activity at human P2Y4 receptor expressed in 1321N1 cells assessed as IP accumulation by SPA
ChEMBL 628 8 7 11 -0.5 O=c1[nH]c(=O)n([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)C(Cl)(Cl)P(=O)(O)O)[C@@H](O)[C@H]2O)cc1Br 10.1021/jm060848j
CHEMBL217467 89211 0 None -33 3 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human P2Y4 receptor expressed in 1321N1 cells assessed as IP accumulation by SPAAgonist activity at human P2Y4 receptor expressed in 1321N1 cells assessed as IP accumulation by SPA
ChEMBL 628 8 7 11 -0.5 O=c1[nH]c(=O)n([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)C(Cl)(Cl)P(=O)(O)O)[C@@H](O)[C@H]2O)cc1Br 10.1021/jm060848j
90656227 117694 0 None 2 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation counting
ChEMBL 742 18 8 15 -0.9 C#CCCNC(=O)COc1ccc(CCCO/N=c2/ccn([C@@H]3O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]3O)c(=O)[nH]2)cc1 10.1021/jm500367e
CHEMBL3261376 117694 0 None 2 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation counting
ChEMBL 742 18 8 15 -0.9 C#CCCNC(=O)COc1ccc(CCCO/N=c2/ccn([C@@H]3O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]3O)c(=O)[nH]2)cc1 10.1021/jm500367e
148197 8220 23 None -1 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at P2Y4 receptorAgonist activity at P2Y4 receptor
ChEMBL 790 14 10 21 -4.2 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm1016297
1736 8220 23 None -1 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at P2Y4 receptorAgonist activity at P2Y4 receptor
ChEMBL 790 14 10 21 -4.2 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm1016297
4900 8220 23 None -1 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at P2Y4 receptorAgonist activity at P2Y4 receptor
ChEMBL 790 14 10 21 -4.2 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm1016297
CHEMBL221326 8220 23 None -1 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at P2Y4 receptorAgonist activity at P2Y4 receptor
ChEMBL 790 14 10 21 -4.2 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm1016297
DB15919 8220 23 None -1 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at P2Y4 receptorAgonist activity at P2Y4 receptor
ChEMBL 790 14 10 21 -4.2 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm1016297
nan 8220 23 None -1 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at P2Y4 receptorAgonist activity at P2Y4 receptor
ChEMBL 790 14 10 21 -4.2 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm1016297
44457427 21629 0 None -6 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity evaluated as change in the level of cytosolic calcium in 1321N astrocytoma cells infected with a retrovirus encoding the human P2Y4 receptorAgonist activity evaluated as change in the level of cytosolic calcium in 1321N astrocytoma cells infected with a retrovirus encoding the human P2Y4 receptor
ChEMBL 790 14 10 21 -4.2 O=c1ccn([C@H]2O[C@@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]3O[C@@H](n4ccc(=O)[nH]c4=O)[C@H](O)[C@@H]3O)[C@H](O)[C@@H]2O)c(=O)[nH]1 10.1016/s0960-894x(00)00612-0
CHEMBL1207447 21629 0 None -6 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity evaluated as change in the level of cytosolic calcium in 1321N astrocytoma cells infected with a retrovirus encoding the human P2Y4 receptorAgonist activity evaluated as change in the level of cytosolic calcium in 1321N astrocytoma cells infected with a retrovirus encoding the human P2Y4 receptor
ChEMBL 790 14 10 21 -4.2 O=c1ccn([C@H]2O[C@@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]3O[C@@H](n4ccc(=O)[nH]c4=O)[C@H](O)[C@@H]3O)[C@H](O)[C@@H]2O)c(=O)[nH]1 10.1016/s0960-894x(00)00612-0
CHEMBL406266 21629 0 None -6 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity evaluated as change in the level of cytosolic calcium in 1321N astrocytoma cells infected with a retrovirus encoding the human P2Y4 receptorAgonist activity evaluated as change in the level of cytosolic calcium in 1321N astrocytoma cells infected with a retrovirus encoding the human P2Y4 receptor
ChEMBL 790 14 10 21 -4.2 O=c1ccn([C@H]2O[C@@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]3O[C@@H](n4ccc(=O)[nH]c4=O)[C@H](O)[C@@H]3O)[C@H](O)[C@@H]2O)c(=O)[nH]1 10.1016/s0960-894x(00)00612-0
90656224 117691 0 None -2 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation counting
ChEMBL 565 12 7 13 -1.6 C#CCCCO/N=c1/ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm500367e
CHEMBL3261373 117691 0 None -2 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation counting
ChEMBL 565 12 7 13 -1.6 C#CCCCO/N=c1/ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm500367e
10303040 98743 0 None -190 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human cloned P2Y4 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human cloned P2Y4 receptor expressed in human 1321N1 by FLIPR assay
ChEMBL 507 8 6 11 0.8 O=P(O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]1O[C@@H](c2nc3ccccc3s2)[C@H](O)[C@@H]1O 10.1016/j.bmcl.2006.10.038
CHEMBL241481 98743 0 None -190 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human cloned P2Y4 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human cloned P2Y4 receptor expressed in human 1321N1 by FLIPR assay
ChEMBL 507 8 6 11 0.8 O=P(O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]1O[C@@H](c2nc3ccccc3s2)[C@H](O)[C@@H]1O 10.1016/j.bmcl.2006.10.038
10191162 154195 0 None -602 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human cloned P2Y4 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human cloned P2Y4 receptor expressed in human 1321N1 by FLIPR assay
ChEMBL 559 8 6 11 1.6 O=P(O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]1O[C@@H](c2nc3c(F)cc(Cl)cc3s2)[C@H](O)[C@@H]1O 10.1016/j.bmcl.2006.10.038
CHEMBL392989 154195 0 None -602 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human cloned P2Y4 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human cloned P2Y4 receptor expressed in human 1321N1 by FLIPR assay
ChEMBL 559 8 6 11 1.6 O=P(O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]1O[C@@H](c2nc3c(F)cc(Cl)cc3s2)[C@H](O)[C@@H]1O 10.1016/j.bmcl.2006.10.038
90656212 117679 0 None 4 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation counting
ChEMBL 619 13 7 14 -1.0 O=c1[nH]/c(=N\OCCOc2ccccc2)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm500367e
CHEMBL3261361 117679 0 None 4 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation counting
ChEMBL 619 13 7 14 -1.0 O=c1[nH]/c(=N\OCCOc2ccccc2)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm500367e
1713 7308 68 None -630 10 Human 4.4 pEC50 = 4.4 Functional
The compound was evaluated for antagonist activity against phospholipase C coupled recombinant human P2Y purinoceptor 4 (P2Y4)The compound was evaluated for antagonist activity against phospholipase C coupled recombinant human P2Y purinoceptor 4 (P2Y4)
ChEMBL 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N 10.1021/jm020046y
5957 7308 68 None -630 10 Human 4.4 pEC50 = 4.4 Functional
The compound was evaluated for antagonist activity against phospholipase C coupled recombinant human P2Y purinoceptor 4 (P2Y4)The compound was evaluated for antagonist activity against phospholipase C coupled recombinant human P2Y purinoceptor 4 (P2Y4)
ChEMBL 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N 10.1021/jm020046y
91 7308 68 None -630 10 Human 4.4 pEC50 = 4.4 Functional
The compound was evaluated for antagonist activity against phospholipase C coupled recombinant human P2Y purinoceptor 4 (P2Y4)The compound was evaluated for antagonist activity against phospholipase C coupled recombinant human P2Y purinoceptor 4 (P2Y4)
ChEMBL 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N 10.1021/jm020046y
CHEMBL14249 7308 68 None -630 10 Human 4.4 pEC50 = 4.4 Functional
The compound was evaluated for antagonist activity against phospholipase C coupled recombinant human P2Y purinoceptor 4 (P2Y4)The compound was evaluated for antagonist activity against phospholipase C coupled recombinant human P2Y purinoceptor 4 (P2Y4)
ChEMBL 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N 10.1021/jm020046y
DB00171 7308 68 None -630 10 Human 4.4 pEC50 = 4.4 Functional
The compound was evaluated for antagonist activity against phospholipase C coupled recombinant human P2Y purinoceptor 4 (P2Y4)The compound was evaluated for antagonist activity against phospholipase C coupled recombinant human P2Y purinoceptor 4 (P2Y4)
ChEMBL 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N 10.1021/jm020046y
44585521 180769 0 None -1 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 710 13 10 19 -3.5 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]3OC(O)C[C@@H](O)[C@@H]3O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1016/j.bmc.2008.05.013
CHEMBL454230 180769 0 None -1 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 710 13 10 19 -3.5 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]3OC(O)C[C@@H](O)[C@@H]3O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1016/j.bmc.2008.05.013
52952395 68120 0 None -2 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assay
ChEMBL 368 6 4 9 -0.9 CCSc1nc(=O)ccn1[C@@H]1O[C@H](COP(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm1016297
CHEMBL1767418 68120 0 None -2 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assay
ChEMBL 368 6 4 9 -0.9 CCSc1nc(=O)ccn1[C@@H]1O[C@H](COP(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm1016297
53309245 69692 0 None -1 3 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 726 13 11 20 -4.6 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)O[C@H]3O[C@H](CO)[C@@H](O)[C@H](O)[C@@H]3O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm101591j
CHEMBL1784886 69692 0 None -1 3 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 726 13 11 20 -4.6 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)O[C@H]3O[C@H](CO)[C@@H](O)[C@H](O)[C@@H]3O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm101591j
52952391 68116 0 None -4 3 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assay
ChEMBL 418 7 5 11 -1.9 COc1nc(=O)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm1016297
CHEMBL1767414 68116 0 None -4 3 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assay
ChEMBL 418 7 5 11 -1.9 COc1nc(=O)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm1016297
189010 191010 12 None -1 3 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 564 10 8 14 -2.4 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1016/j.bmc.2008.05.013
CHEMBL483502 191010 12 None -1 3 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 564 10 8 14 -2.4 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1016/j.bmc.2008.05.013
44586005 191108 0 None -2 2 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 526 9 8 12 -2.8 NC(=O)N[C@@H]1[C@H](O)[C@@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)O[C@H]1n1ccc(=O)[nH]c1=O 10.1016/j.bmc.2008.05.013
CHEMBL484295 191108 0 None -2 2 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 526 9 8 12 -2.8 NC(=O)N[C@@H]1[C@H](O)[C@@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)O[C@H]1n1ccc(=O)[nH]c1=O 10.1016/j.bmc.2008.05.013
90656226 117693 0 None 3 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation counting
ChEMBL 718 14 7 14 0.9 N#CC(CCO/N=c1/ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c(=O)[nH]1)(c1ccccc1)c1ccccc1 10.1021/jm500367e
CHEMBL3261375 117693 0 None 3 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation counting
ChEMBL 718 14 7 14 0.9 N#CC(CCO/N=c1/ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c(=O)[nH]1)(c1ccccc1)c1ccccc1 10.1021/jm500367e
90656210 117677 0 None -1 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation counting
ChEMBL 585 13 8 14 -2.2 O=C(O)CCCO/N=c1/ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm500367e
CHEMBL3261359 117677 0 None -1 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation counting
ChEMBL 585 13 8 14 -2.2 O=C(O)CCCO/N=c1/ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm500367e
44585516 179374 0 None -2 2 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 696 13 10 19 -3.9 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@@H]3OC(O)[C@@H](O)[C@H]3O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1016/j.bmc.2008.05.013
CHEMBL448985 179374 0 None -2 2 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 696 13 10 19 -3.9 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@@H]3OC(O)[C@@H](O)[C@H]3O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1016/j.bmc.2008.05.013
1734 10738 50 None -1 7 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human P2Y purinoceptor 4 expressed in human 1321N1 cells assessed as increase in intracellular calcium concentration by spectrofluorimetryAgonist activity at human P2Y purinoceptor 4 expressed in human 1321N1 cells assessed as increase in intracellular calcium concentration by spectrofluorimetry
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm2013198
3639 10738 50 None -1 7 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human P2Y purinoceptor 4 expressed in human 1321N1 cells assessed as increase in intracellular calcium concentration by spectrofluorimetryAgonist activity at human P2Y purinoceptor 4 expressed in human 1321N1 cells assessed as increase in intracellular calcium concentration by spectrofluorimetry
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm2013198
6133 10738 50 None -1 7 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human P2Y purinoceptor 4 expressed in human 1321N1 cells assessed as increase in intracellular calcium concentration by spectrofluorimetryAgonist activity at human P2Y purinoceptor 4 expressed in human 1321N1 cells assessed as increase in intracellular calcium concentration by spectrofluorimetry
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm2013198
CHEMBL336296 10738 50 None -1 7 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human P2Y purinoceptor 4 expressed in human 1321N1 cells assessed as increase in intracellular calcium concentration by spectrofluorimetryAgonist activity at human P2Y purinoceptor 4 expressed in human 1321N1 cells assessed as increase in intracellular calcium concentration by spectrofluorimetry
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm2013198
DB04005 10738 50 None -1 7 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human P2Y purinoceptor 4 expressed in human 1321N1 cells assessed as increase in intracellular calcium concentration by spectrofluorimetryAgonist activity at human P2Y purinoceptor 4 expressed in human 1321N1 cells assessed as increase in intracellular calcium concentration by spectrofluorimetry
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm2013198
1734 10738 50 None -1 7 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium concentration by dual-excitation spectrofluorimetric analysisAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium concentration by dual-excitation spectrofluorimetric analysis
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1016/j.ejmech.2008.07.015
3639 10738 50 None -1 7 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium concentration by dual-excitation spectrofluorimetric analysisAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium concentration by dual-excitation spectrofluorimetric analysis
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1016/j.ejmech.2008.07.015
6133 10738 50 None -1 7 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium concentration by dual-excitation spectrofluorimetric analysisAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium concentration by dual-excitation spectrofluorimetric analysis
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1016/j.ejmech.2008.07.015
CHEMBL336296 10738 50 None -1 7 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium concentration by dual-excitation spectrofluorimetric analysisAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium concentration by dual-excitation spectrofluorimetric analysis
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1016/j.ejmech.2008.07.015
DB04005 10738 50 None -1 7 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium concentration by dual-excitation spectrofluorimetric analysisAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium concentration by dual-excitation spectrofluorimetric analysis
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1016/j.ejmech.2008.07.015
10929115 208462 0 None -5 2 Human 7.3 pEC50 = 7.3 Functional
Measure of Agonist Potency at human P2Y purinoceptor 4 (hP2Y4) stably expressed in 131N1 astrocytoma cellMeasure of Agonist Potency at human P2Y purinoceptor 4 (hP2Y4) stably expressed in 131N1 astrocytoma cell
ChEMBL 494 8 7 11 -1.8 O=c1ccn([C@H]2[C@H](O)[C@H](O)[C@]3(COP(=O)(O)OP(=O)(O)OP(=O)(O)O)C[C@H]23)c(=O)[nH]1 10.1021/jm010369e
CHEMBL606210 208462 0 None -5 2 Human 7.3 pEC50 = 7.3 Functional
Measure of Agonist Potency at human P2Y purinoceptor 4 (hP2Y4) stably expressed in 131N1 astrocytoma cellMeasure of Agonist Potency at human P2Y purinoceptor 4 (hP2Y4) stably expressed in 131N1 astrocytoma cell
ChEMBL 494 8 7 11 -1.8 O=c1ccn([C@H]2[C@H](O)[C@H](O)[C@]3(COP(=O)(O)OP(=O)(O)OP(=O)(O)O)C[C@H]23)c(=O)[nH]1 10.1021/jm010369e
52952281 68113 0 None -4 2 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assay
ChEMBL 462 9 5 11 -0.4 CCCSc1nc(=O)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm1016297
CHEMBL1767411 68113 0 None -4 2 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assay
ChEMBL 462 9 5 11 -0.4 CCCSc1nc(=O)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm1016297
49867142 6841 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assay
ChEMBL 323 4 5 9 -2.4 O[C@@H]1[C@H](O)[C@H](O[C@H]1n1ccc(=O)nc1N)COP(=O)(O)O 10.1021/jm1016297
6201 6841 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assay
ChEMBL 323 4 5 9 -2.4 O[C@@H]1[C@H](O)[C@H](O[C@H]1n1ccc(=O)nc1N)COP(=O)(O)O 10.1021/jm1016297
CHEMBL1233534 6841 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assay
ChEMBL 323 4 5 9 -2.4 O[C@@H]1[C@H](O)[C@H](O[C@H]1n1ccc(=O)nc1N)COP(=O)(O)O 10.1021/jm1016297
46831692 20968 0 None 1 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assay
ChEMBL 513 9 7 13 -2.4 CO/N=c1\ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm100287t
CHEMBL1083764 20968 0 None 1 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assay
ChEMBL 513 9 7 13 -2.4 CO/N=c1\ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm100287t
CHEMBL1198849 20968 0 None 1 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assay
ChEMBL 513 9 7 13 -2.4 CO/N=c1\ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm100287t
1734 10738 50 None -1 7 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as calcium elevation by fura2/AM assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as calcium elevation by fura2/AM assay
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm901450d
3639 10738 50 None -1 7 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as calcium elevation by fura2/AM assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as calcium elevation by fura2/AM assay
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm901450d
6133 10738 50 None -1 7 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as calcium elevation by fura2/AM assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as calcium elevation by fura2/AM assay
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm901450d
CHEMBL336296 10738 50 None -1 7 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as calcium elevation by fura2/AM assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as calcium elevation by fura2/AM assay
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm901450d
DB04005 10738 50 None -1 7 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as calcium elevation by fura2/AM assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as calcium elevation by fura2/AM assay
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm901450d
44586027 190896 1 None -9 3 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 660 12 9 16 -0.9 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c(=S)[nH]1 10.1016/j.bmc.2008.05.013
CHEMBL482683 190896 1 None -9 3 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 660 12 9 16 -0.9 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c(=S)[nH]1 10.1016/j.bmc.2008.05.013
44585988 190862 0 None -5 2 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 530 9 6 13 0.3 CSc1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c(=S)n1 10.1016/j.bmc.2008.05.013
CHEMBL482472 190862 0 None -5 2 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 530 9 6 13 0.3 CSc1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c(=S)n1 10.1016/j.bmc.2008.05.013
90656211 117678 0 None 3 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation counting
ChEMBL 631 14 7 13 -0.0 O=c1[nH]/c(=N\OCCCCc2ccccc2)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm500367e
CHEMBL3261360 117678 0 None 3 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation counting
ChEMBL 631 14 7 13 -0.0 O=c1[nH]/c(=N\OCCCCc2ccccc2)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm500367e
135528590 195538 0 None -3 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 813 14 10 22 -3.0 Nc1nc(=O)c2ncn([C@H]3C[C@H](O)[C@@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]4O[C@@H](n5ccc(=O)[nH]c5=O)[C@H](O)[C@@H]4O)O3)c2[nH]1 10.1016/j.bmc.2008.05.013
CHEMBL505403 195538 0 None -3 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 813 14 10 22 -3.0 Nc1nc(=O)c2ncn([C@H]3C[C@H](O)[C@@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]4O[C@@H](n5ccc(=O)[nH]c5=O)[C@H](O)[C@@H]4O)O3)c2[nH]1 10.1016/j.bmc.2008.05.013
44586025 190863 1 None -9 3 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 580 10 8 14 -1.0 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c(=S)[nH]1 10.1016/j.bmc.2008.05.013
CHEMBL482485 190863 1 None -9 3 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 580 10 8 14 -1.0 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c(=S)[nH]1 10.1016/j.bmc.2008.05.013
46830492 13387 0 None -8 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assay
ChEMBL 768 14 9 21 -4.1 CO/N=c1/ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]3O[C@@H](n4cc/c(=N/OC)[nH]c4=O)[C@H](O)[C@@H]3O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm100287t
CHEMBL1083257 13387 0 None -8 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assay
ChEMBL 768 14 9 21 -4.1 CO/N=c1/ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]3O[C@@H](n4cc/c(=N/OC)[nH]c4=O)[C@H](O)[C@@H]3O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm100287t
52952282 68114 0 None 1 3 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assay
ChEMBL 510 9 5 11 0.4 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c(SCc2ccccc2)n1 10.1021/jm1016297
CHEMBL1767412 68114 0 None 1 3 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assay
ChEMBL 510 9 5 11 0.4 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c(SCc2ccccc2)n1 10.1021/jm1016297
10255482 68658 18 None 10 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as concentration required to 50% maximal response of compound 3 at 10 uM by fura2/AM assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as concentration required to 50% maximal response of compound 3 at 10 uM by fura2/AM assay
ChEMBL 502 8 7 12 -2.4 O=c1[nH]c(=O)n([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)cc1F 10.1021/jm901450d
CHEMBL1774 68658 18 None 10 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as concentration required to 50% maximal response of compound 3 at 10 uM by fura2/AM assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as concentration required to 50% maximal response of compound 3 at 10 uM by fura2/AM assay
ChEMBL 502 8 7 12 -2.4 O=c1[nH]c(=O)n([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)cc1F 10.1021/jm901450d
53262904 69704 0 None 11 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 728 13 10 19 -3.6 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)O[C@H]3O[C@H](CO)[C@@H](O)[C@H](F)[C@H]3O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm101591j
CHEMBL1784904 69704 0 None 11 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 728 13 10 19 -3.6 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)O[C@H]3O[C@H](CO)[C@@H](O)[C@H](F)[C@H]3O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm101591j
53309379 69693 0 None 4 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 696 12 10 19 -3.9 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)O[C@H]3OC[C@@H](O)[C@H](O)[C@H]3O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm101591j
CHEMBL1784887 69693 0 None 4 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 696 12 10 19 -3.9 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)O[C@H]3OC[C@@H](O)[C@H](O)[C@H]3O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm101591j
46831386 21006 0 None -1 3 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assay
ChEMBL 475 7 6 11 -1.3 CC(C)(C)O/N=c1/ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm100287t
CHEMBL1084296 21006 0 None -1 3 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assay
ChEMBL 475 7 6 11 -1.3 CC(C)(C)O/N=c1/ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm100287t
CHEMBL1199210 21006 0 None -1 3 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assay
ChEMBL 475 7 6 11 -1.3 CC(C)(C)O/N=c1/ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm100287t
44585517 195115 0 None -1 2 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 724 14 10 19 -3.1 CC[C@]1(O)O[C@@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]2O[C@@H](n3ccc(=O)[nH]c3=O)[C@H](O)[C@@H]2O)[C@H](O)[C@H]1O 10.1016/j.bmc.2008.05.013
CHEMBL500840 195115 0 None -1 2 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 724 14 10 19 -3.1 CC[C@]1(O)O[C@@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]2O[C@@H](n3ccc(=O)[nH]c3=O)[C@H](O)[C@@H]2O)[C@H](O)[C@H]1O 10.1016/j.bmc.2008.05.013
90666798 116204 0 None -5 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells using [3H]inositol as substrate assessed as [3H]inositol phosphate formation after 30 mins by liquid scintillation counting analysisAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells using [3H]inositol as substrate assessed as [3H]inositol phosphate formation after 30 mins by liquid scintillation counting analysis
ChEMBL 815 15 9 20 -2.6 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]3O[C@@H](n4cc/c(=N/OCc5ccccc5)[nH]c4=O)[C@H](O)[C@@H]3O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1039/c3md00132f
CHEMBL3220054 116204 0 None -5 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells using [3H]inositol as substrate assessed as [3H]inositol phosphate formation after 30 mins by liquid scintillation counting analysisAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells using [3H]inositol as substrate assessed as [3H]inositol phosphate formation after 30 mins by liquid scintillation counting analysis
ChEMBL 815 15 9 20 -2.6 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]3O[C@@H](n4cc/c(=N/OCc5ccccc5)[nH]c4=O)[C@H](O)[C@@H]3O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1039/c3md00132f
45485253 205806 0 None -12 4 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assay
ChEMBL 433 7 6 11 -2.5 CO/N=c1/ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm100287t
CHEMBL1084020 205806 0 None -12 4 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assay
ChEMBL 433 7 6 11 -2.5 CO/N=c1/ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm100287t
CHEMBL1204010 205806 0 None -12 4 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assay
ChEMBL 433 7 6 11 -2.5 CO/N=c1/ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm100287t
CHEMBL4846821 205806 0 None -12 4 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assay
ChEMBL 433 7 6 11 -2.5 CO/N=c1/ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm100287t
CHEMBL585870 205806 0 None -12 4 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assay
ChEMBL 433 7 6 11 -2.5 CO/N=c1/ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm100287t
53309528 69632 0 None 3 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 833 16 10 20 -1.9 O=c1[nH]/c(=N\OCc2ccccc2)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)O[C@H]2O[C@H](CO)[C@@H](O)[C@H](F)[C@H]2O)[C@@H](O)[C@H]1O 10.1021/jm101591j
CHEMBL1784291 69632 0 None 3 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 833 16 10 20 -1.9 O=c1[nH]/c(=N\OCc2ccccc2)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)O[C@H]2O[C@H](CO)[C@@H](O)[C@H](F)[C@H]2O)[C@@H](O)[C@H]1O 10.1021/jm101591j
90656230 9444 0 None -3 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation counting
ChEMBL 1387 36 10 24 4.5 O=C(COc1ccc(cc1)CCCONc1ccn(c(=O)n1)[C@@H]1O[C@@H]([C@H]([C@H]1O)O)COP(=O)(OP(=O)(OP(=O)(O)O)O)O)NCCc1nnn(c1)CCCNC(=O)CCCCCNC(=O)COc1ccc(cc1)/C=C/c1ccc2n1[B-](F)(F)[N+]1=C(C=CC1=C2)c1cccs1 10.1021/jm500367e
9469 9444 0 None -3 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation counting
ChEMBL 1387 36 10 24 4.5 O=C(COc1ccc(cc1)CCCONc1ccn(c(=O)n1)[C@@H]1O[C@@H]([C@H]([C@H]1O)O)COP(=O)(OP(=O)(OP(=O)(O)O)O)O)NCCc1nnn(c1)CCCNC(=O)CCCCCNC(=O)COc1ccc(cc1)/C=C/c1ccc2n1[B-](F)(F)[N+]1=C(C=CC1=C2)c1cccs1 10.1021/jm500367e
CHEMBL3261378 9444 0 None -3 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation counting
ChEMBL 1387 36 10 24 4.5 O=C(COc1ccc(cc1)CCCONc1ccn(c(=O)n1)[C@@H]1O[C@@H]([C@H]([C@H]1O)O)COP(=O)(OP(=O)(OP(=O)(O)O)O)O)NCCc1nnn(c1)CCCNC(=O)CCCCCNC(=O)COc1ccc(cc1)/C=C/c1ccc2n1[B-](F)(F)[N+]1=C(C=CC1=C2)c1cccs1 10.1021/jm500367e
44439743 154365 0 None -229 2 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human cloned P2Y4 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human cloned P2Y4 receptor expressed in human 1321N1 by FLIPR assay
ChEMBL 517 8 6 11 -0.0 O=c1c2ccccc2ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1016/j.bmcl.2006.09.017
CHEMBL393100 154365 0 None -229 2 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human cloned P2Y4 receptor expressed in human 1321N1 by FLIPR assayAgonist activity at human cloned P2Y4 receptor expressed in human 1321N1 by FLIPR assay
ChEMBL 517 8 6 11 -0.0 O=c1c2ccccc2ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1016/j.bmcl.2006.09.017
24857827 195826 0 None -8 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 789 14 9 21 -1.5 Nc1ccn([C@H]2C[C@H](O)[C@@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]3O[C@@H](n4ccc(=O)[nH]c4=S)[C@H](O)[C@@H]3O)O2)c(=O)n1 10.1016/j.bmc.2008.05.013
CHEMBL509434 195826 0 None -8 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 789 14 9 21 -1.5 Nc1ccn([C@H]2C[C@H](O)[C@@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]3O[C@@H](n4ccc(=O)[nH]c4=S)[C@H](O)[C@@H]3O)O2)c(=O)n1 10.1016/j.bmc.2008.05.013
23379800 87261 0 None -56 4 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human P2Y4 receptor expressed in 1321N1 cells assessed as IP accumulation by SPAAgonist activity at human P2Y4 receptor expressed in 1321N1 cells assessed as IP accumulation by SPA
ChEMBL 482 6 6 10 -1.9 O=c1[nH]c(=O)n([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)cc1Br 10.1021/jm060848j
CHEMBL214698 87261 0 None -56 4 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human P2Y4 receptor expressed in 1321N1 cells assessed as IP accumulation by SPAAgonist activity at human P2Y4 receptor expressed in 1321N1 cells assessed as IP accumulation by SPA
ChEMBL 482 6 6 10 -1.9 O=c1[nH]c(=O)n([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)cc1Br 10.1021/jm060848j
1734 10738 50 None -1 7 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase CAgonist activity at human recombinant P2Y4 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase C
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm060903o
3639 10738 50 None -1 7 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase CAgonist activity at human recombinant P2Y4 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase C
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm060903o
6133 10738 50 None -1 7 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase CAgonist activity at human recombinant P2Y4 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase C
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm060903o
CHEMBL336296 10738 50 None -1 7 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase CAgonist activity at human recombinant P2Y4 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase C
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm060903o
DB04005 10738 50 None -1 7 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase CAgonist activity at human recombinant P2Y4 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase C
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm060903o
53262890 9671 0 None 16 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 603 12 7 13 -0.8 O[C@@H]1[C@H](O)[C@H](O[C@H]1n1cc/c(=N/OCCc2ccccc2)/[nH]c1=O)COP(=O)(OP(=O)(OP(=O)(O)O)O)O 10.1021/jm101591j
6200 9671 0 None 16 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 603 12 7 13 -0.8 O[C@@H]1[C@H](O)[C@H](O[C@H]1n1cc/c(=N/OCCc2ccccc2)/[nH]c1=O)COP(=O)(OP(=O)(OP(=O)(O)O)O)O 10.1021/jm101591j
CHEMBL1784893 9671 0 None 16 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 603 12 7 13 -0.8 O[C@@H]1[C@H](O)[C@H](O[C@H]1n1cc/c(=N/OCCc2ccccc2)/[nH]c1=O)COP(=O)(OP(=O)(OP(=O)(O)O)O)O 10.1021/jm101591j
52952497 67856 0 None -51 3 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assay
ChEMBL 668 11 6 13 0.1 O=C(Cn1c(=O)ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)C(Cl)(Cl)P(=O)(O)O)[C@@H](O)[C@H]2O)c1=O)c1ccccc1 10.1021/jm1016297
CHEMBL1765115 67856 0 None -51 3 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assay
ChEMBL 668 11 6 13 0.1 O=C(Cn1c(=O)ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)C(Cl)(Cl)P(=O)(O)O)[C@@H](O)[C@H]2O)c1=O)c1ccccc1 10.1021/jm1016297
189010 191010 12 None -1 3 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 564 10 8 14 -2.4 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm101591j
CHEMBL483502 191010 12 None -1 3 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 564 10 8 14 -2.4 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm101591j
90666791 116200 0 None -234 3 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells using [3H]inositol as substrate assessed as [3H]inositol phosphate formation after 30 mins by liquid scintillation counting analysisAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells using [3H]inositol as substrate assessed as [3H]inositol phosphate formation after 30 mins by liquid scintillation counting analysis
ChEMBL 587 9 6 11 -0.2 O=c1[nH]/c(=N\OCc2ccc(Br)cc2)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1039/c3md00132f
CHEMBL3220048 116200 0 None -234 3 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells using [3H]inositol as substrate assessed as [3H]inositol phosphate formation after 30 mins by liquid scintillation counting analysisAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells using [3H]inositol as substrate assessed as [3H]inositol phosphate formation after 30 mins by liquid scintillation counting analysis
ChEMBL 587 9 6 11 -0.2 O=c1[nH]/c(=N\OCc2ccc(Br)cc2)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1039/c3md00132f
52952603 67857 0 None -4 3 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assay
ChEMBL 566 8 7 11 0.1 O=c1[nH]c(=S)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)C(Cl)(Cl)P(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm1016297
CHEMBL1765116 67857 0 None -4 3 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assay
ChEMBL 566 8 7 11 0.1 O=c1[nH]c(=S)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)C(Cl)(Cl)P(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm1016297
46830491 20961 4 None -6 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assay
ChEMBL 739 13 9 20 -4.2 CO/N=c1/ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]3O[C@@H](n4ccc(=O)[nH]c4=O)[C@H](O)[C@@H]3O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm100287t
CHEMBL1083256 20961 4 None -6 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assay
ChEMBL 739 13 9 20 -4.2 CO/N=c1/ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]3O[C@@H](n4ccc(=O)[nH]c4=O)[C@H](O)[C@@H]3O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm100287t
CHEMBL1198754 20961 4 None -6 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assay
ChEMBL 739 13 9 20 -4.2 CO/N=c1/ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]3O[C@@H](n4ccc(=O)[nH]c4=O)[C@H](O)[C@@H]3O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm100287t
CHEMBL4279296 20961 4 None -6 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assay
ChEMBL 739 13 9 20 -4.2 CO/N=c1/ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]3O[C@@H](n4ccc(=O)[nH]c4=O)[C@H](O)[C@@H]3O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm100287t
46830491 20961 4 None -6 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells using [3H]inositol as substrate assessed as [3H]inositol phosphate formation after 30 mins by liquid scintillation counting analysisAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells using [3H]inositol as substrate assessed as [3H]inositol phosphate formation after 30 mins by liquid scintillation counting analysis
ChEMBL 739 13 9 20 -4.2 CO/N=c1/ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]3O[C@@H](n4ccc(=O)[nH]c4=O)[C@H](O)[C@@H]3O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1039/c3md00132f
CHEMBL1083256 20961 4 None -6 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells using [3H]inositol as substrate assessed as [3H]inositol phosphate formation after 30 mins by liquid scintillation counting analysisAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells using [3H]inositol as substrate assessed as [3H]inositol phosphate formation after 30 mins by liquid scintillation counting analysis
ChEMBL 739 13 9 20 -4.2 CO/N=c1/ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]3O[C@@H](n4ccc(=O)[nH]c4=O)[C@H](O)[C@@H]3O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1039/c3md00132f
CHEMBL1198754 20961 4 None -6 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells using [3H]inositol as substrate assessed as [3H]inositol phosphate formation after 30 mins by liquid scintillation counting analysisAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells using [3H]inositol as substrate assessed as [3H]inositol phosphate formation after 30 mins by liquid scintillation counting analysis
ChEMBL 739 13 9 20 -4.2 CO/N=c1/ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]3O[C@@H](n4ccc(=O)[nH]c4=O)[C@H](O)[C@@H]3O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1039/c3md00132f
CHEMBL4279296 20961 4 None -6 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells using [3H]inositol as substrate assessed as [3H]inositol phosphate formation after 30 mins by liquid scintillation counting analysisAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells using [3H]inositol as substrate assessed as [3H]inositol phosphate formation after 30 mins by liquid scintillation counting analysis
ChEMBL 739 13 9 20 -4.2 CO/N=c1/ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]3O[C@@H](n4ccc(=O)[nH]c4=O)[C@H](O)[C@@H]3O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1039/c3md00132f
44586006 191141 0 None -56 2 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 500 8 7 12 -1.1 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@@H]2O)c(=S)[nH]1 10.1016/j.bmc.2008.05.013
CHEMBL484494 191141 0 None -56 2 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 500 8 7 12 -1.1 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@@H]2O)c(=S)[nH]1 10.1016/j.bmc.2008.05.013
9853990 195453 0 None -2 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 822 14 10 21 -1.5 O=c1[nH]c(=S)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]2O[C@@H](n3ccc(=S)[nH]c3=O)[C@H](O)[C@@H]2O)[C@@H](O)[C@H]1O 10.1016/j.bmc.2008.05.013
CHEMBL503798 195453 0 None -2 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 822 14 10 21 -1.5 O=c1[nH]c(=S)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]2O[C@@H](n3ccc(=S)[nH]c3=O)[C@H](O)[C@@H]2O)[C@@H](O)[C@H]1O 10.1016/j.bmc.2008.05.013
1734 10738 50 None -1 7 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm101591j
3639 10738 50 None -1 7 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm101591j
6133 10738 50 None -1 7 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm101591j
CHEMBL336296 10738 50 None -1 7 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm101591j
DB04005 10738 50 None -1 7 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm101591j
1737 8149 7 None -2 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at P2Y4 receptorAgonist activity at P2Y4 receptor
ChEMBL 773 14 9 21 -2.9 Nc1ccn(c(=O)n1)[C@@H]1O[C@@H]([C@H](C1)O)COP(=O)(OP(=O)(OP(=O)(OP(=O)(OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1ccc(=O)[nH]c1=O)O)O)O)O 10.1021/jm1016297
9875516 8149 7 None -2 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at P2Y4 receptorAgonist activity at P2Y4 receptor
ChEMBL 773 14 9 21 -2.9 Nc1ccn(c(=O)n1)[C@@H]1O[C@@H]([C@H](C1)O)COP(=O)(OP(=O)(OP(=O)(OP(=O)(OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1ccc(=O)[nH]c1=O)O)O)O)O 10.1021/jm1016297
CHEMBL507282 8149 7 None -2 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at P2Y4 receptorAgonist activity at P2Y4 receptor
ChEMBL 773 14 9 21 -2.9 Nc1ccn(c(=O)n1)[C@@H]1O[C@@H]([C@H](C1)O)COP(=O)(OP(=O)(OP(=O)(OP(=O)(OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1ccc(=O)[nH]c1=O)O)O)O)O 10.1021/jm1016297
DB04983 8149 7 None -2 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at P2Y4 receptorAgonist activity at P2Y4 receptor
ChEMBL 773 14 9 21 -2.9 Nc1ccn(c(=O)n1)[C@@H]1O[C@@H]([C@H](C1)O)COP(=O)(OP(=O)(OP(=O)(OP(=O)(OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1ccc(=O)[nH]c1=O)O)O)O)O 10.1021/jm1016297
44585986 191107 0 None -5 3 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 534 8 7 11 -0.4 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)C(F)(F)P(=O)(O)O)[C@@H](O)[C@H]2O)c(=S)[nH]1 10.1016/j.bmc.2008.05.013
CHEMBL484290 191107 0 None -5 3 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 534 8 7 11 -0.4 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)C(F)(F)P(=O)(O)O)[C@@H](O)[C@H]2O)c(=S)[nH]1 10.1016/j.bmc.2008.05.013
44420650 91031 0 None -17 2 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase CAgonist activity at human recombinant P2Y4 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase C
ChEMBL 583 9 7 12 0.0 CC(C)(C)C(=O)N[C@@H]1[C@H](O)[C@@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)O[C@H]1n1ccc(=O)[nH]c1=S 10.1021/jm060903o
CHEMBL221162 91031 0 None -17 2 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase CAgonist activity at human recombinant P2Y4 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase C
ChEMBL 583 9 7 12 0.0 CC(C)(C)C(=O)N[C@@H]1[C@H](O)[C@@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)O[C@H]1n1ccc(=O)[nH]c1=S 10.1021/jm060903o
90656219 117686 0 None 5 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation counting
ChEMBL 662 14 7 15 -0.5 O=c1[nH]/c(=N\OCCCc2ccc([N+](=O)[O-])cc2)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm500367e
CHEMBL3261368 117686 0 None 5 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation counting
ChEMBL 662 14 7 15 -0.5 O=c1[nH]/c(=N\OCCCc2ccc([N+](=O)[O-])cc2)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm500367e
46890111 13524 0 None -5 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assay
ChEMBL 478 8 6 10 -0.8 O=c1ccn([C@H]2C[C@H](O)[C@@]3(COP(=O)(O)OP(=O)(O)OP(=O)(O)O)C[C@H]23)c(=O)[nH]1 10.1021/jm100287t
CHEMBL1083763 13524 0 None -5 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assay
ChEMBL 478 8 6 10 -0.8 O=c1ccn([C@H]2C[C@H](O)[C@@]3(COP(=O)(O)OP(=O)(O)OP(=O)(O)O)C[C@H]23)c(=O)[nH]1 10.1021/jm100287t
10929115 208462 0 None -5 2 Human 7.1 pEC50 = 7.1 Functional
Measure of Agonist Potency at human P2Y purinoceptor 4 (hP2Y4) stably expressed in 131N1 astrocytoma cellMeasure of Agonist Potency at human P2Y purinoceptor 4 (hP2Y4) stably expressed in 131N1 astrocytoma cell
ChEMBL 494 8 7 11 -1.8 O=c1ccn([C@H]2[C@H](O)[C@H](O)[C@]3(COP(=O)(O)OP(=O)(O)OP(=O)(O)O)C[C@H]23)c(=O)[nH]1 10.1021/jm010369e
CHEMBL606210 208462 0 None -5 2 Human 7.1 pEC50 = 7.1 Functional
Measure of Agonist Potency at human P2Y purinoceptor 4 (hP2Y4) stably expressed in 131N1 astrocytoma cellMeasure of Agonist Potency at human P2Y purinoceptor 4 (hP2Y4) stably expressed in 131N1 astrocytoma cell
ChEMBL 494 8 7 11 -1.8 O=c1ccn([C@H]2[C@H](O)[C@H](O)[C@]3(COP(=O)(O)OP(=O)(O)OP(=O)(O)O)C[C@H]23)c(=O)[nH]1 10.1021/jm010369e
1734 10738 50 None -1 7 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human P2Y4 receptor expressed in 1321N1 cells assessed as IP accumulation by SPAAgonist activity at human P2Y4 receptor expressed in 1321N1 cells assessed as IP accumulation by SPA
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm060848j
3639 10738 50 None -1 7 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human P2Y4 receptor expressed in 1321N1 cells assessed as IP accumulation by SPAAgonist activity at human P2Y4 receptor expressed in 1321N1 cells assessed as IP accumulation by SPA
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm060848j
6133 10738 50 None -1 7 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human P2Y4 receptor expressed in 1321N1 cells assessed as IP accumulation by SPAAgonist activity at human P2Y4 receptor expressed in 1321N1 cells assessed as IP accumulation by SPA
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm060848j
CHEMBL336296 10738 50 None -1 7 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human P2Y4 receptor expressed in 1321N1 cells assessed as IP accumulation by SPAAgonist activity at human P2Y4 receptor expressed in 1321N1 cells assessed as IP accumulation by SPA
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm060848j
DB04005 10738 50 None -1 7 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human P2Y4 receptor expressed in 1321N1 cells assessed as IP accumulation by SPAAgonist activity at human P2Y4 receptor expressed in 1321N1 cells assessed as IP accumulation by SPA
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm060848j
148197 8220 23 None -1 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human P2Y4Agonist activity at human P2Y4
ChEMBL 790 14 10 21 -4.2 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm101591j
1736 8220 23 None -1 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human P2Y4Agonist activity at human P2Y4
ChEMBL 790 14 10 21 -4.2 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm101591j
4900 8220 23 None -1 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human P2Y4Agonist activity at human P2Y4
ChEMBL 790 14 10 21 -4.2 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm101591j
CHEMBL221326 8220 23 None -1 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human P2Y4Agonist activity at human P2Y4
ChEMBL 790 14 10 21 -4.2 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm101591j
DB15919 8220 23 None -1 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human P2Y4Agonist activity at human P2Y4
ChEMBL 790 14 10 21 -4.2 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm101591j
nan 8220 23 None -1 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human P2Y4Agonist activity at human P2Y4
ChEMBL 790 14 10 21 -4.2 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm101591j
9875011 97490 1 None -3 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 710 12 9 19 -4.3 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]3O[C@@H](n4ccc(=O)[nH]c4=O)[C@H](O)[C@@H]3O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1016/j.bmc.2008.05.013
CHEMBL239151 97490 1 None -3 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 710 12 9 19 -4.3 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]3O[C@@H](n4ccc(=O)[nH]c4=O)[C@H](O)[C@@H]3O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1016/j.bmc.2008.05.013
9875011 97490 1 None -3 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assay
ChEMBL 710 12 9 19 -4.3 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]3O[C@@H](n4ccc(=O)[nH]c4=O)[C@H](O)[C@@H]3O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm100287t
CHEMBL239151 97490 1 None -3 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assay
ChEMBL 710 12 9 19 -4.3 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]3O[C@@H](n4ccc(=O)[nH]c4=O)[C@H](O)[C@@H]3O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm100287t
9875011 97490 1 None -3 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells using [3H]inositol as substrate assessed as [3H]inositol phosphate formation after 30 mins by liquid scintillation counting analysisAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells using [3H]inositol as substrate assessed as [3H]inositol phosphate formation after 30 mins by liquid scintillation counting analysis
ChEMBL 710 12 9 19 -4.3 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]3O[C@@H](n4ccc(=O)[nH]c4=O)[C@H](O)[C@@H]3O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1039/c3md00132f
CHEMBL239151 97490 1 None -3 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells using [3H]inositol as substrate assessed as [3H]inositol phosphate formation after 30 mins by liquid scintillation counting analysisAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells using [3H]inositol as substrate assessed as [3H]inositol phosphate formation after 30 mins by liquid scintillation counting analysis
ChEMBL 710 12 9 19 -4.3 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]3O[C@@H](n4ccc(=O)[nH]c4=O)[C@H](O)[C@@H]3O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1039/c3md00132f
1734 10738 50 None -1 7 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assay
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm1016297
3639 10738 50 None -1 7 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assay
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm1016297
6133 10738 50 None -1 7 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assay
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm1016297
CHEMBL336296 10738 50 None -1 7 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assay
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm1016297
DB04005 10738 50 None -1 7 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assay
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm1016297
1734 10738 50 None -1 7 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human P2Y4Agonist activity at human P2Y4
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm101591j
3639 10738 50 None -1 7 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human P2Y4Agonist activity at human P2Y4
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm101591j
6133 10738 50 None -1 7 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human P2Y4Agonist activity at human P2Y4
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm101591j
CHEMBL336296 10738 50 None -1 7 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human P2Y4Agonist activity at human P2Y4
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm101591j
DB04005 10738 50 None -1 7 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human P2Y4Agonist activity at human P2Y4
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm101591j
1734 10738 50 None -1 7 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1016/j.bmc.2008.05.013
3639 10738 50 None -1 7 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1016/j.bmc.2008.05.013
6133 10738 50 None -1 7 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1016/j.bmc.2008.05.013
CHEMBL336296 10738 50 None -1 7 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1016/j.bmc.2008.05.013
DB04005 10738 50 None -1 7 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1016/j.bmc.2008.05.013
44585987 198581 0 None 2 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 566 8 7 11 0.1 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)C(Cl)(Cl)P(=O)(O)O)[C@@H](O)[C@H]2O)c(=S)[nH]1 10.1016/j.bmc.2008.05.013
CHEMBL519835 198581 0 None 2 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate accumulation by scintillation proximity assay
ChEMBL 566 8 7 11 0.1 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)C(Cl)(Cl)P(=O)(O)O)[C@@H](O)[C@H]2O)c(=S)[nH]1 10.1016/j.bmc.2008.05.013
1734 10738 50 None -1 7 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assay
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm100287t
3639 10738 50 None -1 7 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assay
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm100287t
6133 10738 50 None -1 7 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assay
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm100287t
CHEMBL336296 10738 50 None -1 7 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assay
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm100287t
DB04005 10738 50 None -1 7 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production by scintillation proximity assay
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm100287t
1734 10738 50 None -1 7 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GFP-tagged P2Y4 receptor expressed in human 1321N1 cells assessed as intracellular calcium mobilization by fura2/AM-based fluorescence spectrophotometryAgonist activity at human GFP-tagged P2Y4 receptor expressed in human 1321N1 cells assessed as intracellular calcium mobilization by fura2/AM-based fluorescence spectrophotometry
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1016/j.bmc.2012.07.042
3639 10738 50 None -1 7 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GFP-tagged P2Y4 receptor expressed in human 1321N1 cells assessed as intracellular calcium mobilization by fura2/AM-based fluorescence spectrophotometryAgonist activity at human GFP-tagged P2Y4 receptor expressed in human 1321N1 cells assessed as intracellular calcium mobilization by fura2/AM-based fluorescence spectrophotometry
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1016/j.bmc.2012.07.042
6133 10738 50 None -1 7 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GFP-tagged P2Y4 receptor expressed in human 1321N1 cells assessed as intracellular calcium mobilization by fura2/AM-based fluorescence spectrophotometryAgonist activity at human GFP-tagged P2Y4 receptor expressed in human 1321N1 cells assessed as intracellular calcium mobilization by fura2/AM-based fluorescence spectrophotometry
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1016/j.bmc.2012.07.042
CHEMBL336296 10738 50 None -1 7 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GFP-tagged P2Y4 receptor expressed in human 1321N1 cells assessed as intracellular calcium mobilization by fura2/AM-based fluorescence spectrophotometryAgonist activity at human GFP-tagged P2Y4 receptor expressed in human 1321N1 cells assessed as intracellular calcium mobilization by fura2/AM-based fluorescence spectrophotometry
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1016/j.bmc.2012.07.042
DB04005 10738 50 None -1 7 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human GFP-tagged P2Y4 receptor expressed in human 1321N1 cells assessed as intracellular calcium mobilization by fura2/AM-based fluorescence spectrophotometryAgonist activity at human GFP-tagged P2Y4 receptor expressed in human 1321N1 cells assessed as intracellular calcium mobilization by fura2/AM-based fluorescence spectrophotometry
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1016/j.bmc.2012.07.042
90656217 117684 0 None -1 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation counting
ChEMBL 743 13 7 13 0.2 O=c1[nH]/c(=N\OCCCc2ccc(I)cc2)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm500367e
CHEMBL3261366 117684 0 None -1 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation counting
ChEMBL 743 13 7 13 0.2 O=c1[nH]/c(=N\OCCCc2ccc(I)cc2)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm500367e
53309380 69695 0 None 2 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 767 14 11 20 -4.4 CC(=O)N[C@H]1[C@@H](OP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]2O[C@@H](n3ccc(=O)[nH]c3=O)[C@H](O)[C@@H]2O)O[C@H](CO)[C@@H](O)[C@@H]1O 10.1021/jm101591j
CHEMBL1784889 69695 0 None 2 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 767 14 11 20 -4.4 CC(=O)N[C@H]1[C@@H](OP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]2O[C@@H](n3ccc(=O)[nH]c3=O)[C@H](O)[C@@H]2O)O[C@H](CO)[C@@H](O)[C@@H]1O 10.1021/jm101591j
52952605 9982 10 None -70 3 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assay
ChEMBL 534 8 7 11 -0.4 O[C@@H]1[C@@H](COP(=O)(OP(=O)(C(P(=O)(O)O)(F)F)O)O)O[C@H]([C@@H]1O)n1ccc(=S)[nH]c1=O 10.1021/jm1016297
5902 9982 10 None -70 3 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assay
ChEMBL 534 8 7 11 -0.4 O[C@@H]1[C@@H](COP(=O)(OP(=O)(C(P(=O)(O)O)(F)F)O)O)O[C@H]([C@@H]1O)n1ccc(=S)[nH]c1=O 10.1021/jm1016297
CHEMBL1765119 9982 10 None -70 3 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate intracellular accumulation by scintillation proximity assay
ChEMBL 534 8 7 11 -0.4 O[C@@H]1[C@@H](COP(=O)(OP(=O)(C(P(=O)(O)O)(F)F)O)O)O[C@H]([C@@H]1O)n1ccc(=S)[nH]c1=O 10.1021/jm1016297
CHEMBL2029010 215927 0 None -1 3 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human P2Y purinoceptor 4 expressed in human 1321N1 cells assessed as increase in intracellular calcium concentration by spectrofluorimetryAgonist activity at human P2Y purinoceptor 4 expressed in human 1321N1 cells assessed as increase in intracellular calcium concentration by spectrofluorimetry
ChEMBL None None None BP(=O)(OC[C@H]1O[C@@H](n2ccc(=O)[nH]c2=O)[C@H](O)[C@@H]1O)OP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]1O[C@@H](n2ccc(=O)[nH]c2=O)[C@H](O)[C@@H]1O.CCCCN(CCCC)CCCC.CCCCN(CCCC)CCCC.CCCCN(CCCC)CCCC.CCCCN(CCCC)CCCC 10.1021/jm2013198
90656218 117685 0 None 4 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation counting
ChEMBL 662 14 7 15 -0.5 O=c1[nH]/c(=N\OCCCc2cccc([N+](=O)[O-])c2)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm500367e
CHEMBL3261367 117685 0 None 4 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation countingAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as stimulation of [3H]inositol phosphate accumulation by liquid scintillation counting
ChEMBL 662 14 7 15 -0.5 O=c1[nH]/c(=N\OCCCc2cccc([N+](=O)[O-])c2)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm500367e
90666794 116203 0 None -9 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells using [3H]inositol as substrate assessed as [3H]inositol phosphate formation after 30 mins by liquid scintillation counting analysisAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells using [3H]inositol as substrate assessed as [3H]inositol phosphate formation after 30 mins by liquid scintillation counting analysis
ChEMBL 585 10 6 11 -0.2 C#CCCC#Cc1cccc(CO/N=c2/ccn([C@@H]3O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]3O)c(=O)[nH]2)c1 10.1039/c3md00132f
CHEMBL3220051 116203 0 None -9 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells using [3H]inositol as substrate assessed as [3H]inositol phosphate formation after 30 mins by liquid scintillation counting analysisAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells using [3H]inositol as substrate assessed as [3H]inositol phosphate formation after 30 mins by liquid scintillation counting analysis
ChEMBL 585 10 6 11 -0.2 C#CCCC#Cc1cccc(CO/N=c2/ccn([C@@H]3O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]3O)c(=O)[nH]2)c1 10.1039/c3md00132f
53308272 69698 0 None 2 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 589 11 7 13 -0.8 O=c1[nH]/c(=N\OCc2ccccc2)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm101591j
CHEMBL1784892 69698 0 None 2 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assayAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells assessed as [3H]inositol phosphate production after 30 mins by scintillation proximity assay
ChEMBL 589 11 7 13 -0.8 O=c1[nH]/c(=N\OCc2ccccc2)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm101591j
53308272 69698 0 None 2 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells using [3H]inositol as substrate assessed as [3H]inositol phosphate formation after 30 mins by liquid scintillation counting analysisAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells using [3H]inositol as substrate assessed as [3H]inositol phosphate formation after 30 mins by liquid scintillation counting analysis
ChEMBL 589 11 7 13 -0.8 O=c1[nH]/c(=N\OCc2ccccc2)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1039/c3md00132f
CHEMBL1784892 69698 0 None 2 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells using [3H]inositol as substrate assessed as [3H]inositol phosphate formation after 30 mins by liquid scintillation counting analysisAgonist activity at human recombinant P2Y4 receptor expressed in human 1321N1 cells using [3H]inositol as substrate assessed as [3H]inositol phosphate formation after 30 mins by liquid scintillation counting analysis
ChEMBL 589 11 7 13 -0.8 O=c1[nH]/c(=N\OCc2ccccc2)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1039/c3md00132f
25125168 21690 0 None 1 3 Human 5.0 pIC50 = 5 Functional
Antagonist activity against human P2Y4 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assayAntagonist activity against human P2Y4 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assay
ChEMBL 556 5 4 10 4.3 Nc1c(S(=O)(=O)O)cc(Nc2ccc(Nc3nc(Cl)nc(Cl)n3)cc2)c2c1C(=O)c1ccccc1C2=O 10.1021/jm1012193
CHEMBL1208098 21690 0 None 1 3 Human 5.0 pIC50 = 5 Functional
Antagonist activity against human P2Y4 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assayAntagonist activity against human P2Y4 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assay
ChEMBL 556 5 4 10 4.3 Nc1c(S(=O)(=O)O)cc(Nc2ccc(Nc3nc(Cl)nc(Cl)n3)cc2)c2c1C(=O)c1ccccc1C2=O 10.1021/jm1012193
CHEMBL496401 21690 0 None 1 3 Human 5.0 pIC50 = 5 Functional
Antagonist activity against human P2Y4 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assayAntagonist activity against human P2Y4 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assay
ChEMBL 556 5 4 10 4.3 Nc1c(S(=O)(=O)O)cc(Nc2ccc(Nc3nc(Cl)nc(Cl)n3)cc2)c2c1C(=O)c1ccccc1C2=O 10.1021/jm1012193
3018777 67024 6 None 2 2 Human 5.0 pIC50 = 5 Functional
Antagonist activity against human P2Y4 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assayAntagonist activity against human P2Y4 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assay
ChEMBL 424 4 3 7 3.0 COc1cccc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)c1 10.1021/jm1012193
CHEMBL1671995 67024 6 None 2 2 Human 5.0 pIC50 = 5 Functional
Antagonist activity against human P2Y4 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assayAntagonist activity against human P2Y4 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assay
ChEMBL 424 4 3 7 3.0 COc1cccc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)c1 10.1021/jm1012193
CHEMBL1741070 67024 6 None 2 2 Human 5.0 pIC50 = 5 Functional
Antagonist activity against human P2Y4 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assayAntagonist activity against human P2Y4 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assay
ChEMBL 424 4 3 7 3.0 COc1cccc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)c1 10.1021/jm1012193
53308119 67030 0 None 2 2 Human 5.0 pIC50 = 5 Functional
Antagonist activity against human P2Y4 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assayAntagonist activity against human P2Y4 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assay
ChEMBL 556 5 4 10 4.3 Nc1c(S(=O)(=O)O)cc(Nc2cccc(Nc3nc(Cl)nc(Cl)n3)c2)c2c1C(=O)c1ccccc1C2=O 10.1021/jm1012193
CHEMBL1672105 67030 0 None 2 2 Human 5.0 pIC50 = 5 Functional
Antagonist activity against human P2Y4 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assayAntagonist activity against human P2Y4 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assay
ChEMBL 556 5 4 10 4.3 Nc1c(S(=O)(=O)O)cc(Nc2cccc(Nc3nc(Cl)nc(Cl)n3)c2)c2c1C(=O)c1ccccc1C2=O 10.1021/jm1012193
CHEMBL1741085 67030 0 None 2 2 Human 5.0 pIC50 = 5 Functional
Antagonist activity against human P2Y4 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assayAntagonist activity against human P2Y4 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assay
ChEMBL 556 5 4 10 4.3 Nc1c(S(=O)(=O)O)cc(Nc2cccc(Nc3nc(Cl)nc(Cl)n3)c2)c2c1C(=O)c1ccccc1C2=O 10.1021/jm1012193
53326685 67031 0 None 3 2 Human 5.0 pIC50 = 5 Functional
Antagonist activity against human P2Y4 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assayAntagonist activity against human P2Y4 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assay
ChEMBL 520 5 6 12 2.4 Nc1c(S(=O)(=O)O)cc(Nc2ccc(Nc3nc(O)nc(O)n3)cc2)c2c1C(=O)c1ccccc1C2=O 10.1021/jm1012193
CHEMBL1672106 67031 0 None 3 2 Human 5.0 pIC50 = 5 Functional
Antagonist activity against human P2Y4 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assayAntagonist activity against human P2Y4 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assay
ChEMBL 520 5 6 12 2.4 Nc1c(S(=O)(=O)O)cc(Nc2ccc(Nc3nc(O)nc(O)n3)cc2)c2c1C(=O)c1ccccc1C2=O 10.1021/jm1012193
CHEMBL1741086 67031 0 None 3 2 Human 5.0 pIC50 = 5 Functional
Antagonist activity against human P2Y4 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assayAntagonist activity against human P2Y4 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assay
ChEMBL 520 5 6 12 2.4 Nc1c(S(=O)(=O)O)cc(Nc2ccc(Nc3nc(O)nc(O)n3)cc2)c2c1C(=O)c1ccccc1C2=O 10.1021/jm1012193
137648293 164354 0 None - 1 Human 4.0 pIC50 = 4 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 390 3 3 5 3.9 Cc1cc(Nc2ccc(F)cc2C(=O)O)c2c(c1N)C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL4080560 164354 0 None - 1 Human 4.0 pIC50 = 4 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 390 3 3 5 3.9 Cc1cc(Nc2ccc(F)cc2C(=O)O)c2c(c1N)C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
25124826 21698 2 None -1 3 Human 5.0 pIC50 = 5 Functional
Antagonist activity at human P2Y4 receptor expressed in astrocytoma cells assessed as inhibition of intracellular calcium mobilizationAntagonist activity at human P2Y4 receptor expressed in astrocytoma cells assessed as inhibition of intracellular calcium mobilization
ChEMBL 444 3 3 6 4.2 Nc1c(S(=O)(=O)O)cc(Nc2cccc3ccccc23)c2c1C(=O)c1ccccc1C2=O 10.1021/jm901851t
CHEMBL1208118 21698 2 None -1 3 Human 5.0 pIC50 = 5 Functional
Antagonist activity at human P2Y4 receptor expressed in astrocytoma cells assessed as inhibition of intracellular calcium mobilizationAntagonist activity at human P2Y4 receptor expressed in astrocytoma cells assessed as inhibition of intracellular calcium mobilization
ChEMBL 444 3 3 6 4.2 Nc1c(S(=O)(=O)O)cc(Nc2cccc3ccccc23)c2c1C(=O)c1ccccc1C2=O 10.1021/jm901851t
CHEMBL498423 21698 2 None -1 3 Human 5.0 pIC50 = 5 Functional
Antagonist activity at human P2Y4 receptor expressed in astrocytoma cells assessed as inhibition of intracellular calcium mobilizationAntagonist activity at human P2Y4 receptor expressed in astrocytoma cells assessed as inhibition of intracellular calcium mobilization
ChEMBL 444 3 3 6 4.2 Nc1c(S(=O)(=O)O)cc(Nc2cccc3ccccc23)c2c1C(=O)c1ccccc1C2=O 10.1021/jm901851t
44152335 21502 1 None 1 3 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 422 3 3 6 3.7 Cc1ccc(C)c(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)c1 10.1021/acs.jmedchem.7b00030
CHEMBL1206280 21502 1 None 1 3 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 422 3 3 6 3.7 Cc1ccc(C)c(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)c1 10.1021/acs.jmedchem.7b00030
CHEMBL256689 21502 1 None 1 3 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 422 3 3 6 3.7 Cc1ccc(C)c(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)c1 10.1021/acs.jmedchem.7b00030
136677322 10069 24 None -158 9 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 773 9 7 15 3.9 OS(=O)(=O)c1cc(Nc2ccc(c(c2)S(=O)(=O)O)Nc2nc(Cl)nc(n2)Nc2cccc(c2)S(=O)(=O)O)c2c(c1N)C(=O)c1c(C2=O)cccc1 10.1021/acs.jmedchem.7b00030
1739 10069 24 None -158 9 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 773 9 7 15 3.9 OS(=O)(=O)c1cc(Nc2ccc(c(c2)S(=O)(=O)O)Nc2nc(Cl)nc(n2)Nc2cccc(c2)S(=O)(=O)O)c2c(c1N)C(=O)c1c(C2=O)cccc1 10.1021/acs.jmedchem.7b00030
656725 10069 24 None -158 9 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 773 9 7 15 3.9 OS(=O)(=O)c1cc(Nc2ccc(c(c2)S(=O)(=O)O)Nc2nc(Cl)nc(n2)Nc2cccc(c2)S(=O)(=O)O)c2c(c1N)C(=O)c1c(C2=O)cccc1 10.1021/acs.jmedchem.7b00030
CHEMBL1160031 10069 24 None -158 9 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 773 9 7 15 3.9 OS(=O)(=O)c1cc(Nc2ccc(c(c2)S(=O)(=O)O)Nc2nc(Cl)nc(n2)Nc2cccc(c2)S(=O)(=O)O)c2c(c1N)C(=O)c1c(C2=O)cccc1 10.1021/acs.jmedchem.7b00030
25128135 21691 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 502 5 3 7 5.2 Nc1c(S(=O)(=O)O)cc(Nc2ccc(Sc3ccccc3)cc2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL1208102 21691 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 502 5 3 7 5.2 Nc1c(S(=O)(=O)O)cc(Nc2ccc(Sc3ccccc3)cc2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL496620 21691 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 502 5 3 7 5.2 Nc1c(S(=O)(=O)O)cc(Nc2ccc(Sc3ccccc3)cc2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
51050135 67029 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 430 3 3 6 3.3 Nc1c(S(=O)(=O)O)cc(Nc2cc(F)cc(F)c2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL1672099 67029 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 430 3 3 6 3.3 Nc1c(S(=O)(=O)O)cc(Nc2cc(F)cc(F)c2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL1741083 67029 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 430 3 3 6 3.3 Nc1c(S(=O)(=O)O)cc(Nc2cc(F)cc(F)c2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
46504926 198111 31 None - 1 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at human P2Y4R expressed in HEK293 cells assessed as inhibition of UTP-induced IP3 production preincubated for 0.5 hrs followed by UTP stimulation by ELISAAntagonist activity at human P2Y4R expressed in HEK293 cells assessed as inhibition of UTP-induced IP3 production preincubated for 0.5 hrs followed by UTP stimulation by ELISA
ChEMBL 522 4 1 3 5.2 O=C(C1CC1)N1CCc2cc(Br)c(S(=O)(=O)Nc3ccc(Cl)c(C(F)(F)F)c3)cc21 10.1021/acs.jmedchem.2c01632
CHEMBL5191550 198111 31 None - 1 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at human P2Y4R expressed in HEK293 cells assessed as inhibition of UTP-induced IP3 production preincubated for 0.5 hrs followed by UTP stimulation by ELISAAntagonist activity at human P2Y4R expressed in HEK293 cells assessed as inhibition of UTP-induced IP3 production preincubated for 0.5 hrs followed by UTP stimulation by ELISA
ChEMBL 522 4 1 3 5.2 O=C(C1CC1)N1CCc2cc(Br)c(S(=O)(=O)Nc3ccc(Cl)c(C(F)(F)F)c3)cc21 10.1021/acs.jmedchem.2c01632
51050133 67035 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 412 3 3 6 3.2 Nc1c(S(=O)(=O)O)cc(Nc2cccc(F)c2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL1671997 67035 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 412 3 3 6 3.2 Nc1c(S(=O)(=O)O)cc(Nc2cccc(F)c2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL1741100 67035 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 412 3 3 6 3.2 Nc1c(S(=O)(=O)O)cc(Nc2cccc(F)c2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
20658940 21695 0 None - 1 Human 4.8 pIC50 = 4.8 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 408 4 3 6 2.9 Nc1c(S(=O)(=O)O)cc(NCc2ccccc2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL1208114 21695 0 None - 1 Human 4.8 pIC50 = 4.8 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 408 4 3 6 2.9 Nc1c(S(=O)(=O)O)cc(NCc2ccccc2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL498223 21695 0 None - 1 Human 4.8 pIC50 = 4.8 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 408 4 3 6 2.9 Nc1c(S(=O)(=O)O)cc(NCc2ccccc2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
25124828 21703 0 None 1 3 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity against human P2Y4 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assayAntagonist activity against human P2Y4 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assay
ChEMBL 600 6 5 11 4.0 Nc1c(S(=O)(=O)O)cc(Nc2cc(Nc3nc(Cl)nc(Cl)n3)cc(C(=O)O)c2)c2c1C(=O)c1ccccc1C2=O 10.1021/jm1012193
CHEMBL1208131 21703 0 None 1 3 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity against human P2Y4 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assayAntagonist activity against human P2Y4 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assay
ChEMBL 600 6 5 11 4.0 Nc1c(S(=O)(=O)O)cc(Nc2cc(Nc3nc(Cl)nc(Cl)n3)cc(C(=O)O)c2)c2c1C(=O)c1ccccc1C2=O 10.1021/jm1012193
CHEMBL499580 21703 0 None 1 3 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity against human P2Y4 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assayAntagonist activity against human P2Y4 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assay
ChEMBL 600 6 5 11 4.0 Nc1c(S(=O)(=O)O)cc(Nc2cc(Nc3nc(Cl)nc(Cl)n3)cc(C(=O)O)c2)c2c1C(=O)c1ccccc1C2=O 10.1021/jm1012193
51050129 67027 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 422 4 3 6 3.6 CCc1cccc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)c1 10.1021/acs.jmedchem.7b00030
CHEMBL1671993 67027 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 422 4 3 6 3.6 CCc1cccc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)c1 10.1021/acs.jmedchem.7b00030
CHEMBL1741081 67027 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 422 4 3 6 3.6 CCc1cccc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)c1 10.1021/acs.jmedchem.7b00030
137630446 167844 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 442 4 3 7 3.2 COc1cc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)ccc1F 10.1021/acs.jmedchem.7b00030
CHEMBL4090513 167844 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 442 4 3 7 3.2 COc1cc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)ccc1F 10.1021/acs.jmedchem.7b00030
CHEMBL4116637 167844 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 442 4 3 7 3.2 COc1cc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)ccc1F 10.1021/acs.jmedchem.7b00030
137631028 167925 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 442 3 3 6 4.0 Cc1cc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)ccc1Cl 10.1021/acs.jmedchem.7b00030
CHEMBL4082692 167925 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 442 3 3 6 4.0 Cc1cc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)ccc1Cl 10.1021/acs.jmedchem.7b00030
CHEMBL4117312 167925 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 442 3 3 6 4.0 Cc1cc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)ccc1Cl 10.1021/acs.jmedchem.7b00030
137630150 167831 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 504 5 3 7 5.0 Nc1c(S(=O)(=O)O)cc(Nc2ccc(Oc3ccc(F)cc3)cc2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL4074456 167831 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 504 5 3 7 5.0 Nc1c(S(=O)(=O)O)cc(Nc2ccc(Oc3ccc(F)cc3)cc2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL4116573 167831 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 504 5 3 7 5.0 Nc1c(S(=O)(=O)O)cc(Nc2ccc(Oc3ccc(F)cc3)cc2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
3018777 67024 6 None 2 2 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 424 4 3 7 3.0 COc1cccc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)c1 10.1021/acs.jmedchem.7b00030
CHEMBL1671995 67024 6 None 2 2 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 424 4 3 7 3.0 COc1cccc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)c1 10.1021/acs.jmedchem.7b00030
CHEMBL1741070 67024 6 None 2 2 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 424 4 3 7 3.0 COc1cccc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)c1 10.1021/acs.jmedchem.7b00030
137630536 167858 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 564 5 3 7 5.6 Nc1c(S(=O)(=O)O)cc(Nc2ccc(Oc3ccc(Br)cc3)cc2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL4065831 167858 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 564 5 3 7 5.6 Nc1c(S(=O)(=O)O)cc(Nc2ccc(Oc3ccc(Br)cc3)cc2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL4116759 167858 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 564 5 3 7 5.6 Nc1c(S(=O)(=O)O)cc(Nc2ccc(Oc3ccc(Br)cc3)cc2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
25123180 21606 0 None 2 3 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 485 5 4 7 4.8 Nc1c(S(=O)(=O)O)cc(Nc2ccc(Nc3ccccc3)cc2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL1207384 21606 0 None 2 3 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 485 5 4 7 4.8 Nc1c(S(=O)(=O)O)cc(Nc2ccc(Nc3ccccc3)cc2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL401859 21606 0 None 2 3 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 485 5 4 7 4.8 Nc1c(S(=O)(=O)O)cc(Nc2ccc(Nc3ccccc3)cc2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
25127814 21723 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 486 5 3 7 4.8 Nc1c(S(=O)(=O)O)cc(Nc2ccc(Oc3ccccc3)cc2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL1208433 21723 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 486 5 3 7 4.8 Nc1c(S(=O)(=O)O)cc(Nc2ccc(Oc3ccccc3)cc2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL597203 21723 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 486 5 3 7 4.8 Nc1c(S(=O)(=O)O)cc(Nc2ccc(Oc3ccccc3)cc2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
22916 21497 22 None -2 6 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 394 3 3 6 3.0 Nc1c(S(=O)(=O)O)cc(Nc2ccccc2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL1206272 21497 22 None -2 6 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 394 3 3 6 3.0 Nc1c(S(=O)(=O)O)cc(Nc2ccccc2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL256057 21497 22 None -2 6 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 394 3 3 6 3.0 Nc1c(S(=O)(=O)O)cc(Nc2ccccc2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
137629896 167796 0 None - 1 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 454 4 5 8 2.4 Nc1c(S(=O)(=O)O)cc(Nc2ccc(O)cc2C(=O)O)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL4067679 167796 0 None - 1 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 454 4 5 8 2.4 Nc1c(S(=O)(=O)O)cc(Nc2ccc(O)cc2C(=O)O)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL4116314 167796 0 None - 1 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 454 4 5 8 2.4 Nc1c(S(=O)(=O)O)cc(Nc2ccc(O)cc2C(=O)O)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
25124484 21522 0 None 3 2 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity against human P2Y4 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assayAntagonist activity against human P2Y4 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assay
ChEMBL 428 3 3 6 3.7 Nc1c(S(=O)(=O)O)cc(Nc2cccc(Cl)c2)c2c1C(=O)c1ccccc1C2=O 10.1021/jm1012193
CHEMBL1206415 21522 0 None 3 2 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity against human P2Y4 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assayAntagonist activity against human P2Y4 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assay
ChEMBL 428 3 3 6 3.7 Nc1c(S(=O)(=O)O)cc(Nc2cccc(Cl)c2)c2c1C(=O)c1ccccc1C2=O 10.1021/jm1012193
CHEMBL271672 21522 0 None 3 2 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity against human P2Y4 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assayAntagonist activity against human P2Y4 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assay
ChEMBL 428 3 3 6 3.7 Nc1c(S(=O)(=O)O)cc(Nc2cccc(Cl)c2)c2c1C(=O)c1ccccc1C2=O 10.1021/jm1012193
71531032 167785 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 442 3 3 6 4.0 Cc1cc(Cl)ccc1Nc1cc(S(=O)(=O)O)c(N)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL4060811 167785 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 442 3 3 6 4.0 Cc1cc(Cl)ccc1Nc1cc(S(=O)(=O)O)c(N)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL4116227 167785 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 442 3 3 6 4.0 Cc1cc(Cl)ccc1Nc1cc(S(=O)(=O)O)c(N)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
106250 21688 6 None 1 4 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity against human P2Y4 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assayAntagonist activity against human P2Y4 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assay
ChEMBL 410 3 4 7 2.7 Nc1c(S(=O)(=O)O)cc(Nc2ccc(O)cc2)c2c1C(=O)c1ccccc1C2=O 10.1021/jm1012193
CHEMBL1208092 21688 6 None 1 4 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity against human P2Y4 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assayAntagonist activity against human P2Y4 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assay
ChEMBL 410 3 4 7 2.7 Nc1c(S(=O)(=O)O)cc(Nc2ccc(O)cc2)c2c1C(=O)c1ccccc1C2=O 10.1021/jm1012193
CHEMBL496030 21688 6 None 1 4 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity against human P2Y4 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assayAntagonist activity against human P2Y4 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assay
ChEMBL 410 3 4 7 2.7 Nc1c(S(=O)(=O)O)cc(Nc2ccc(O)cc2)c2c1C(=O)c1ccccc1C2=O 10.1021/jm1012193
21130371 21659 0 None 1 4 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 408 3 3 6 3.3 Cc1cccc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)c1 10.1021/acs.jmedchem.7b00030
CHEMBL1207842 21659 0 None 1 4 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 408 3 3 6 3.3 Cc1cccc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)c1 10.1021/acs.jmedchem.7b00030
CHEMBL445413 21659 0 None 1 4 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 408 3 3 6 3.3 Cc1cccc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)c1 10.1021/acs.jmedchem.7b00030
137630000 167809 0 None 10 5 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 530 5 3 7 5.8 Cc1ccc(Sc2ccc(Nc3cc(S(=O)(=O)O)c(N)c4c3C(=O)c3ccccc3C4=O)cc2)c(C)c1 10.1021/acs.jmedchem.7b00030
CHEMBL4087247 167809 0 None 10 5 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 530 5 3 7 5.8 Cc1ccc(Sc2ccc(Nc3cc(S(=O)(=O)O)c(N)c4c3C(=O)c3ccccc3C4=O)cc2)c(C)c1 10.1021/acs.jmedchem.7b00030
CHEMBL4116405 167809 0 None 10 5 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 530 5 3 7 5.8 Cc1ccc(Sc2ccc(Nc3cc(S(=O)(=O)O)c(N)c4c3C(=O)c3ccccc3C4=O)cc2)c(C)c1 10.1021/acs.jmedchem.7b00030
25124484 21522 0 None 3 2 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 428 3 3 6 3.7 Nc1c(S(=O)(=O)O)cc(Nc2cccc(Cl)c2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL1206415 21522 0 None 3 2 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 428 3 3 6 3.7 Nc1c(S(=O)(=O)O)cc(Nc2cccc(Cl)c2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL271672 21522 0 None 3 2 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 428 3 3 6 3.7 Nc1c(S(=O)(=O)O)cc(Nc2cccc(Cl)c2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
11970419 21725 0 None - 1 Human 4.6 pIC50 = 4.6 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 438 4 4 7 2.7 Nc1c(S(=O)(=O)O)cc(Nc2cccc(C(=O)O)c2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL1208450 21725 0 None - 1 Human 4.6 pIC50 = 4.6 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 438 4 4 7 2.7 Nc1c(S(=O)(=O)O)cc(Nc2cccc(C(=O)O)c2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL598857 21725 0 None - 1 Human 4.6 pIC50 = 4.6 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 438 4 4 7 2.7 Nc1c(S(=O)(=O)O)cc(Nc2cccc(C(=O)O)c2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
106250 21688 6 None 1 4 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human P2Y4 receptor expressed in astrocytoma cells assessed as inhibition of intracellular calcium mobilizationAntagonist activity at human P2Y4 receptor expressed in astrocytoma cells assessed as inhibition of intracellular calcium mobilization
ChEMBL 410 3 4 7 2.7 Nc1c(S(=O)(=O)O)cc(Nc2ccc(O)cc2)c2c1C(=O)c1ccccc1C2=O 10.1021/jm901851t
CHEMBL1208092 21688 6 None 1 4 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human P2Y4 receptor expressed in astrocytoma cells assessed as inhibition of intracellular calcium mobilizationAntagonist activity at human P2Y4 receptor expressed in astrocytoma cells assessed as inhibition of intracellular calcium mobilization
ChEMBL 410 3 4 7 2.7 Nc1c(S(=O)(=O)O)cc(Nc2ccc(O)cc2)c2c1C(=O)c1ccccc1C2=O 10.1021/jm901851t
CHEMBL496030 21688 6 None 1 4 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human P2Y4 receptor expressed in astrocytoma cells assessed as inhibition of intracellular calcium mobilizationAntagonist activity at human P2Y4 receptor expressed in astrocytoma cells assessed as inhibition of intracellular calcium mobilization
ChEMBL 410 3 4 7 2.7 Nc1c(S(=O)(=O)O)cc(Nc2ccc(O)cc2)c2c1C(=O)c1ccccc1C2=O 10.1021/jm901851t
22916 21497 22 None -2 6 Human 4.6 pIC50 = 4.6 Functional
Antagonist activity against human P2Y4 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assayAntagonist activity against human P2Y4 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assay
ChEMBL 394 3 3 6 3.0 Nc1c(S(=O)(=O)O)cc(Nc2ccccc2)c2c1C(=O)c1ccccc1C2=O 10.1021/jm1012193
CHEMBL1206272 21497 22 None -2 6 Human 4.6 pIC50 = 4.6 Functional
Antagonist activity against human P2Y4 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assayAntagonist activity against human P2Y4 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assay
ChEMBL 394 3 3 6 3.0 Nc1c(S(=O)(=O)O)cc(Nc2ccccc2)c2c1C(=O)c1ccccc1C2=O 10.1021/jm1012193
CHEMBL256057 21497 22 None -2 6 Human 4.6 pIC50 = 4.6 Functional
Antagonist activity against human P2Y4 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assayAntagonist activity against human P2Y4 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assay
ChEMBL 394 3 3 6 3.0 Nc1c(S(=O)(=O)O)cc(Nc2ccccc2)c2c1C(=O)c1ccccc1C2=O 10.1021/jm1012193
22916 21497 22 None -2 6 Human 4.6 pIC50 = 4.6 Functional
Antagonist activity at human P2Y4 receptor expressed in astrocytoma cells assessed as inhibition of intracellular calcium mobilizationAntagonist activity at human P2Y4 receptor expressed in astrocytoma cells assessed as inhibition of intracellular calcium mobilization
ChEMBL 394 3 3 6 3.0 Nc1c(S(=O)(=O)O)cc(Nc2ccccc2)c2c1C(=O)c1ccccc1C2=O 10.1021/jm901851t
CHEMBL1206272 21497 22 None -2 6 Human 4.6 pIC50 = 4.6 Functional
Antagonist activity at human P2Y4 receptor expressed in astrocytoma cells assessed as inhibition of intracellular calcium mobilizationAntagonist activity at human P2Y4 receptor expressed in astrocytoma cells assessed as inhibition of intracellular calcium mobilization
ChEMBL 394 3 3 6 3.0 Nc1c(S(=O)(=O)O)cc(Nc2ccccc2)c2c1C(=O)c1ccccc1C2=O 10.1021/jm901851t
CHEMBL256057 21497 22 None -2 6 Human 4.6 pIC50 = 4.6 Functional
Antagonist activity at human P2Y4 receptor expressed in astrocytoma cells assessed as inhibition of intracellular calcium mobilizationAntagonist activity at human P2Y4 receptor expressed in astrocytoma cells assessed as inhibition of intracellular calcium mobilization
ChEMBL 394 3 3 6 3.0 Nc1c(S(=O)(=O)O)cc(Nc2ccccc2)c2c1C(=O)c1ccccc1C2=O 10.1021/jm901851t
108643 9989 6 None 3 3 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 424 4 3 7 3.0 COc1ccc(cc1)Nc1cc(c(c2c1C(=O)c1ccccc1C2=O)N)S(=O)(=O)O 10.1021/acs.jmedchem.7b00030
9468 9989 6 None 3 3 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 424 4 3 7 3.0 COc1ccc(cc1)Nc1cc(c(c2c1C(=O)c1ccccc1C2=O)N)S(=O)(=O)O 10.1021/acs.jmedchem.7b00030
CHEMBL1207381 9989 6 None 3 3 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 424 4 3 7 3.0 COc1ccc(cc1)Nc1cc(c(c2c1C(=O)c1ccccc1C2=O)N)S(=O)(=O)O 10.1021/acs.jmedchem.7b00030
44456166 21608 0 None 3 3 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 422 3 3 6 3.7 Cc1cccc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)c1C 10.1021/acs.jmedchem.7b00030
CHEMBL1207392 21608 0 None 3 3 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 422 3 3 6 3.7 Cc1cccc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)c1C 10.1021/acs.jmedchem.7b00030
CHEMBL402239 21608 0 None 3 3 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 422 3 3 6 3.7 Cc1cccc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)c1C 10.1021/acs.jmedchem.7b00030
16120270 21716 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 472 4 4 7 3.4 Nc1c(S(=O)(=O)O)cc(Nc2cc(Cl)ccc2C(=O)O)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL1208282 21716 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 472 4 4 7 3.4 Nc1c(S(=O)(=O)O)cc(Nc2cc(Cl)ccc2C(=O)O)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL522053 21716 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 472 4 4 7 3.4 Nc1c(S(=O)(=O)O)cc(Nc2cc(Cl)ccc2C(=O)O)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
117532 21623 8 None 8 3 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 408 3 3 6 3.3 Cc1ccc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)cc1 10.1021/acs.jmedchem.7b00030
CHEMBL1207421 21623 8 None 8 3 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 408 3 3 6 3.3 Cc1ccc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)cc1 10.1021/acs.jmedchem.7b00030
CHEMBL404450 21623 8 None 8 3 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 408 3 3 6 3.3 Cc1ccc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)cc1 10.1021/acs.jmedchem.7b00030
137630776 167886 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 436 5 3 6 4.0 CCCc1cccc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)c1 10.1021/acs.jmedchem.7b00030
CHEMBL4063945 167886 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 436 5 3 6 4.0 CCCc1cccc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)c1 10.1021/acs.jmedchem.7b00030
CHEMBL4117065 167886 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 436 5 3 6 4.0 CCCc1cccc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)c1 10.1021/acs.jmedchem.7b00030
25114303 21728 0 None - 1 Human 4.5 pIC50 = 4.5 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 438 4 4 7 2.7 Nc1c(S(=O)(=O)O)cc(Nc2ccc(C(=O)O)cc2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL1208486 21728 0 None - 1 Human 4.5 pIC50 = 4.5 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 438 4 4 7 2.7 Nc1c(S(=O)(=O)O)cc(Nc2ccc(C(=O)O)cc2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL604300 21728 0 None - 1 Human 4.5 pIC50 = 4.5 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 438 4 4 7 2.7 Nc1c(S(=O)(=O)O)cc(Nc2ccc(C(=O)O)cc2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
51050133 67035 0 None - 1 Human 4.5 pIC50 = 4.5 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 412 3 3 6 3.2 Nc1c(S(=O)(=O)O)cc(Nc2cccc(F)c2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL1671997 67035 0 None - 1 Human 4.5 pIC50 = 4.5 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 412 3 3 6 3.2 Nc1c(S(=O)(=O)O)cc(Nc2cccc(F)c2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL1741100 67035 0 None - 1 Human 4.5 pIC50 = 4.5 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 412 3 3 6 3.2 Nc1c(S(=O)(=O)O)cc(Nc2cccc(F)c2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
13782419 21523 2 None 1 3 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 428 3 3 6 3.7 Nc1c(S(=O)(=O)O)cc(Nc2ccc(Cl)cc2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL1206416 21523 2 None 1 3 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 428 3 3 6 3.7 Nc1c(S(=O)(=O)O)cc(Nc2ccc(Cl)cc2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL271673 21523 2 None 1 3 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 428 3 3 6 3.7 Nc1c(S(=O)(=O)O)cc(Nc2ccc(Cl)cc2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
106250 21688 6 None 1 4 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 410 3 4 7 2.7 Nc1c(S(=O)(=O)O)cc(Nc2ccc(O)cc2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL1208092 21688 6 None 1 4 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 410 3 4 7 2.7 Nc1c(S(=O)(=O)O)cc(Nc2ccc(O)cc2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL496030 21688 6 None 1 4 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 410 3 4 7 2.7 Nc1c(S(=O)(=O)O)cc(Nc2ccc(O)cc2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
56944331 167885 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 422 4 3 6 3.6 CCc1ccc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)cc1 10.1021/acs.jmedchem.7b00030
CHEMBL4078095 167885 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 422 4 3 6 3.6 CCc1ccc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)cc1 10.1021/acs.jmedchem.7b00030
CHEMBL4117064 167885 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 422 4 3 6 3.6 CCc1ccc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)cc1 10.1021/acs.jmedchem.7b00030
46228693 21726 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 472 3 3 6 3.8 Nc1c(S(=O)(=O)O)cc(Nc2ccc(Br)cc2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL1208451 21726 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 472 3 3 6 3.8 Nc1c(S(=O)(=O)O)cc(Nc2ccc(Br)cc2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL599050 21726 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 472 3 3 6 3.8 Nc1c(S(=O)(=O)O)cc(Nc2ccc(Br)cc2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
137630585 167865 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 458 4 3 7 3.7 COc1cc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)ccc1Cl 10.1021/acs.jmedchem.7b00030
CHEMBL4081964 167865 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 458 4 3 7 3.7 COc1cc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)ccc1Cl 10.1021/acs.jmedchem.7b00030
CHEMBL4116837 167865 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 458 4 3 7 3.7 COc1cc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)ccc1Cl 10.1021/acs.jmedchem.7b00030
25127813 21685 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 484 5 3 6 4.6 Nc1c(S(=O)(=O)O)cc(Nc2ccc(Cc3ccccc3)cc2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL1208083 21685 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 484 5 3 6 4.6 Nc1c(S(=O)(=O)O)cc(Nc2ccc(Cc3ccccc3)cc2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL495605 21685 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 484 5 3 6 4.6 Nc1c(S(=O)(=O)O)cc(Nc2ccc(Cc3ccccc3)cc2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
117530 21504 5 None 2 3 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 408 3 3 6 3.3 Cc1ccccc1Nc1cc(S(=O)(=O)O)c(N)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL1206282 21504 5 None 2 3 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 408 3 3 6 3.3 Cc1ccccc1Nc1cc(S(=O)(=O)O)c(N)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL256864 21504 5 None 2 3 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 408 3 3 6 3.3 Cc1ccccc1Nc1cc(S(=O)(=O)O)c(N)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
44456161 21607 0 None 2 3 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 422 4 3 6 3.6 CCc1ccccc1Nc1cc(S(=O)(=O)O)c(N)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL1207391 21607 0 None 2 3 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 422 4 3 6 3.6 CCc1ccccc1Nc1cc(S(=O)(=O)O)c(N)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL402238 21607 0 None 2 3 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 422 4 3 6 3.6 CCc1ccccc1Nc1cc(S(=O)(=O)O)c(N)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
109055 21501 1 None 1 3 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 422 3 3 6 3.7 Cc1ccc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)c(C)c1 10.1021/acs.jmedchem.7b00030
CHEMBL1206279 21501 1 None 1 3 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 422 3 3 6 3.7 Cc1ccc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)c(C)c1 10.1021/acs.jmedchem.7b00030
CHEMBL256688 21501 1 None 1 3 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 422 3 3 6 3.7 Cc1ccc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)c(C)c1 10.1021/acs.jmedchem.7b00030
137629897 167797 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 520 5 3 7 5.5 Nc1c(S(=O)(=O)O)cc(Nc2ccc(Oc3ccc(Cl)cc3)cc2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL4094930 167797 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 520 5 3 7 5.5 Nc1c(S(=O)(=O)O)cc(Nc2ccc(Oc3ccc(Cl)cc3)cc2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL4116315 167797 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 520 5 3 7 5.5 Nc1c(S(=O)(=O)O)cc(Nc2ccc(Oc3ccc(Cl)cc3)cc2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
137630586 167866 0 None 6 5 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 530 5 3 7 5.8 Cc1ccc(C)c(Sc2ccc(Nc3cc(S(=O)(=O)O)c(N)c4c3C(=O)c3ccccc3C4=O)cc2)c1 10.1021/acs.jmedchem.7b00030
CHEMBL4081274 167866 0 None 6 5 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 530 5 3 7 5.8 Cc1ccc(C)c(Sc2ccc(Nc3cc(S(=O)(=O)O)c(N)c4c3C(=O)c3ccccc3C4=O)cc2)c1 10.1021/acs.jmedchem.7b00030
CHEMBL4116838 167866 0 None 6 5 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 530 5 3 7 5.8 Cc1ccc(C)c(Sc2ccc(Nc3cc(S(=O)(=O)O)c(N)c4c3C(=O)c3ccccc3C4=O)cc2)c1 10.1021/acs.jmedchem.7b00030
3018582 21509 6 None -1 3 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 424 4 3 7 3.0 COc1ccccc1Nc1cc(S(=O)(=O)O)c(N)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL1206290 21509 6 None -1 3 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 424 4 3 7 3.0 COc1ccccc1Nc1cc(S(=O)(=O)O)c(N)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL257495 21509 6 None -1 3 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 424 4 3 7 3.0 COc1ccccc1Nc1cc(S(=O)(=O)O)c(N)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
25124160 21727 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 412 3 3 6 3.2 Nc1c(S(=O)(=O)O)cc(Nc2ccc(F)cc2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL1208485 21727 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 412 3 3 6 3.2 Nc1c(S(=O)(=O)O)cc(Nc2ccc(F)cc2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL604158 21727 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 412 3 3 6 3.2 Nc1c(S(=O)(=O)O)cc(Nc2ccc(F)cc2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
137630492 167856 0 None 8 4 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 517 6 3 8 4.7 Nc1c(S(=O)(=O)O)cc(Nc2ccc(SCc3cccnc3)cc2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL4090874 167856 0 None 8 4 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 517 6 3 8 4.7 Nc1c(S(=O)(=O)O)cc(Nc2ccc(SCc3cccnc3)cc2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL4116755 167856 0 None 8 4 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 517 6 3 8 4.7 Nc1c(S(=O)(=O)O)cc(Nc2ccc(SCc3cccnc3)cc2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
137629595 167912 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 438 4 3 7 3.4 COc1cc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)ccc1C 10.1021/acs.jmedchem.7b00030
CHEMBL4072198 167912 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 438 4 3 7 3.4 COc1cc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)ccc1C 10.1021/acs.jmedchem.7b00030
CHEMBL4117231 167912 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 438 4 3 7 3.4 COc1cc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)ccc1C 10.1021/acs.jmedchem.7b00030
11451 9985 0 None 6 5 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 530 5 3 7 5.8 Nc1c2C(=O)c3ccccc3C(=O)c2c(cc1S(=O)(=O)O)Nc1ccc(cc1)Sc1ccc(c(c1)C)C 10.1021/acs.jmedchem.7b00030
132574707 9985 0 None 6 5 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 530 5 3 7 5.8 Nc1c2C(=O)c3ccccc3C(=O)c2c(cc1S(=O)(=O)O)Nc1ccc(cc1)Sc1ccc(c(c1)C)C 10.1021/acs.jmedchem.7b00030
CHEMBL4116316 9985 0 None 6 5 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 530 5 3 7 5.8 Nc1c2C(=O)c3ccccc3C(=O)c2c(cc1S(=O)(=O)O)Nc1ccc(cc1)Sc1ccc(c(c1)C)C 10.1021/acs.jmedchem.7b00030
137635750 167999 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 454 5 3 8 3.1 COc1ccc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)cc1OC 10.1021/acs.jmedchem.7b00030
CHEMBL4063599 167999 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 454 5 3 8 3.1 COc1ccc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)cc1OC 10.1021/acs.jmedchem.7b00030
CHEMBL4117950 167999 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 454 5 3 8 3.1 COc1ccc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)cc1OC 10.1021/acs.jmedchem.7b00030
3018582 21509 6 None -1 3 Human 4.3 pIC50 = 4.3 Functional
Antagonist activity at human P2Y4 receptorAntagonist activity at human P2Y4 receptor
ChEMBL 424 4 3 7 3.0 COc1ccccc1Nc1cc(S(=O)(=O)O)c(N)c2c1C(=O)c1ccccc1C2=O 10.1016/j.bmcl.2007.10.082
CHEMBL1206290 21509 6 None -1 3 Human 4.3 pIC50 = 4.3 Functional
Antagonist activity at human P2Y4 receptorAntagonist activity at human P2Y4 receptor
ChEMBL 424 4 3 7 3.0 COc1ccccc1Nc1cc(S(=O)(=O)O)c(N)c2c1C(=O)c1ccccc1C2=O 10.1016/j.bmcl.2007.10.082
CHEMBL257495 21509 6 None -1 3 Human 4.3 pIC50 = 4.3 Functional
Antagonist activity at human P2Y4 receptorAntagonist activity at human P2Y4 receptor
ChEMBL 424 4 3 7 3.0 COc1ccccc1Nc1cc(S(=O)(=O)O)c(N)c2c1C(=O)c1ccccc1C2=O 10.1016/j.bmcl.2007.10.082
136677322 10069 24 None -158 9 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as inhibition of UTP-induced intracellular calcium mobilization by FLUOstar plate readerAntagonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as inhibition of UTP-induced intracellular calcium mobilization by FLUOstar plate reader
ChEMBL 773 9 7 15 3.9 OS(=O)(=O)c1cc(Nc2ccc(c(c2)S(=O)(=O)O)Nc2nc(Cl)nc(n2)Nc2cccc(c2)S(=O)(=O)O)c2c(c1N)C(=O)c1c(C2=O)cccc1 10.1021/jm800175e
1739 10069 24 None -158 9 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as inhibition of UTP-induced intracellular calcium mobilization by FLUOstar plate readerAntagonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as inhibition of UTP-induced intracellular calcium mobilization by FLUOstar plate reader
ChEMBL 773 9 7 15 3.9 OS(=O)(=O)c1cc(Nc2ccc(c(c2)S(=O)(=O)O)Nc2nc(Cl)nc(n2)Nc2cccc(c2)S(=O)(=O)O)c2c(c1N)C(=O)c1c(C2=O)cccc1 10.1021/jm800175e
656725 10069 24 None -158 9 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as inhibition of UTP-induced intracellular calcium mobilization by FLUOstar plate readerAntagonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as inhibition of UTP-induced intracellular calcium mobilization by FLUOstar plate reader
ChEMBL 773 9 7 15 3.9 OS(=O)(=O)c1cc(Nc2ccc(c(c2)S(=O)(=O)O)Nc2nc(Cl)nc(n2)Nc2cccc(c2)S(=O)(=O)O)c2c(c1N)C(=O)c1c(C2=O)cccc1 10.1021/jm800175e
CHEMBL1160031 10069 24 None -158 9 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as inhibition of UTP-induced intracellular calcium mobilization by FLUOstar plate readerAntagonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as inhibition of UTP-induced intracellular calcium mobilization by FLUOstar plate reader
ChEMBL 773 9 7 15 3.9 OS(=O)(=O)c1cc(Nc2ccc(c(c2)S(=O)(=O)O)Nc2nc(Cl)nc(n2)Nc2cccc(c2)S(=O)(=O)O)c2c(c1N)C(=O)c1c(C2=O)cccc1 10.1021/jm800175e
25114519 21718 1 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 438 4 4 7 2.7 Nc1c(S(=O)(=O)O)cc(Nc2ccccc2C(=O)O)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL1208288 21718 1 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 438 4 4 7 2.7 Nc1c(S(=O)(=O)O)cc(Nc2ccccc2C(=O)O)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL524064 21718 1 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 438 4 4 7 2.7 Nc1c(S(=O)(=O)O)cc(Nc2ccccc2C(=O)O)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
136677323 16984 6 None -7 3 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 773 9 7 15 3.9 Nc1c(S(=O)(=O)O)cc(Nc2ccc(Nc3nc(Cl)nc(Nc4ccc(S(=O)(=O)O)cc4)n3)c(S(=O)(=O)O)c2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
3638737 16984 6 None -7 3 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 773 9 7 15 3.9 Nc1c(S(=O)(=O)O)cc(Nc2ccc(Nc3nc(Cl)nc(Nc4ccc(S(=O)(=O)O)cc4)n3)c(S(=O)(=O)O)c2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL1160025 16984 6 None -7 3 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 773 9 7 15 3.9 Nc1c(S(=O)(=O)O)cc(Nc2ccc(Nc3nc(Cl)nc(Nc4ccc(S(=O)(=O)O)cc4)n3)c(S(=O)(=O)O)c2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL1365553 16984 6 None -7 3 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 773 9 7 15 3.9 Nc1c(S(=O)(=O)O)cc(Nc2ccc(Nc3nc(Cl)nc(Nc4ccc(S(=O)(=O)O)cc4)n3)c(S(=O)(=O)O)c2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
25124162 67033 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 422 3 3 6 3.7 Cc1cc(C)cc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)c1 10.1021/acs.jmedchem.7b00030
CHEMBL1671994 67033 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 422 3 3 6 3.7 Cc1cc(C)cc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)c1 10.1021/acs.jmedchem.7b00030
CHEMBL1741096 67033 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 422 3 3 6 3.7 Cc1cc(C)cc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)c1 10.1021/acs.jmedchem.7b00030
25124161 67028 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 472 3 3 6 3.8 Nc1c(S(=O)(=O)O)cc(Nc2cccc(Br)c2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL1672098 67028 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 472 3 3 6 3.8 Nc1c(S(=O)(=O)O)cc(Nc2cccc(Br)c2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL1741082 67028 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 472 3 3 6 3.8 Nc1c(S(=O)(=O)O)cc(Nc2cccc(Br)c2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
15404279 21696 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 422 5 3 6 2.9 Nc1c(S(=O)(=O)O)cc(NCCc2ccccc2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL1208115 21696 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 422 5 3 6 2.9 Nc1c(S(=O)(=O)O)cc(NCCc2ccccc2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL498224 21696 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 422 5 3 6 2.9 Nc1c(S(=O)(=O)O)cc(NCCc2ccccc2)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
136126658 61743 0 None -1 2 Human 4.1 pIC50 = 4.1 Functional
Antagonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as inhibition of UTP-induced intracellular calcium mobilization by FLUOstar plate readerAntagonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as inhibition of UTP-induced intracellular calcium mobilization by FLUOstar plate reader
ChEMBL 510 8 5 10 2.0 Cc1cc(/N=N/c2ccc(S(=O)(=O)O)cc2S(=O)(=O)O)c(COP(=O)(O)O)c(C=O)c1O 10.1021/jm800175e
CHEMBL1615626 61743 0 None -1 2 Human 4.1 pIC50 = 4.1 Functional
Antagonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as inhibition of UTP-induced intracellular calcium mobilization by FLUOstar plate readerAntagonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as inhibition of UTP-induced intracellular calcium mobilization by FLUOstar plate reader
ChEMBL 510 8 5 10 2.0 Cc1cc(/N=N/c2ccc(S(=O)(=O)O)cc2S(=O)(=O)O)c(COP(=O)(O)O)c(C=O)c1O 10.1021/jm800175e
CHEMBL477339 61743 0 None -1 2 Human 4.1 pIC50 = 4.1 Functional
Antagonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as inhibition of UTP-induced intracellular calcium mobilization by FLUOstar plate readerAntagonist activity at human P2Y4 receptor expressed in human 1321N1 cells assessed as inhibition of UTP-induced intracellular calcium mobilization by FLUOstar plate reader
ChEMBL 510 8 5 10 2.0 Cc1cc(/N=N/c2ccc(S(=O)(=O)O)cc2S(=O)(=O)O)c(COP(=O)(O)O)c(C=O)c1O 10.1021/jm800175e
25124826 21698 2 None -1 3 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 444 3 3 6 4.2 Nc1c(S(=O)(=O)O)cc(Nc2cccc3ccccc23)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL1208118 21698 2 None -1 3 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 444 3 3 6 4.2 Nc1c(S(=O)(=O)O)cc(Nc2cccc3ccccc23)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL498423 21698 2 None -1 3 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 444 3 3 6 4.2 Nc1c(S(=O)(=O)O)cc(Nc2cccc3ccccc23)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
137630841 167892 0 None -12 5 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 424 3 4 7 3.0 Cc1cc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)ccc1O 10.1021/acs.jmedchem.7b00030
CHEMBL4069492 167892 0 None -12 5 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 424 3 4 7 3.0 Cc1cc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)ccc1O 10.1021/acs.jmedchem.7b00030
CHEMBL4117118 167892 0 None -12 5 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 424 3 4 7 3.0 Cc1cc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)ccc1O 10.1021/acs.jmedchem.7b00030
51050131 67025 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 454 5 3 8 3.1 COc1cc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)cc(OC)c1 10.1021/acs.jmedchem.7b00030
CHEMBL1671996 67025 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 454 5 3 8 3.1 COc1cc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)cc(OC)c1 10.1021/acs.jmedchem.7b00030
CHEMBL1741071 67025 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 454 5 3 8 3.1 COc1cc(Nc2cc(S(=O)(=O)O)c(N)c3c2C(=O)c2ccccc2C3=O)cc(OC)c1 10.1021/acs.jmedchem.7b00030
137645876 167986 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 428 3 3 6 3.7 Nc1c(S(=O)(=O)O)cc(Nc2ccccc2Cl)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL4084432 167986 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 428 3 3 6 3.7 Nc1c(S(=O)(=O)O)cc(Nc2ccccc2Cl)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
CHEMBL4117856 167986 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assayAntagonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as inhibition of UTP-activated intracellular calcium mobilization preincubated for 30 mins followed by UTP addition by fluo-4-dye based fluorescence assay
ChEMBL 428 3 3 6 3.7 Nc1c(S(=O)(=O)O)cc(Nc2ccccc2Cl)c2c1C(=O)c1ccccc1C2=O 10.1021/acs.jmedchem.7b00030
136677322 10069 24 None -158 9 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity against human P2Y4 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assayAntagonist activity against human P2Y4 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assay
ChEMBL 773 9 7 15 3.9 OS(=O)(=O)c1cc(Nc2ccc(c(c2)S(=O)(=O)O)Nc2nc(Cl)nc(n2)Nc2cccc(c2)S(=O)(=O)O)c2c(c1N)C(=O)c1c(C2=O)cccc1 10.1021/jm1012193
1739 10069 24 None -158 9 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity against human P2Y4 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assayAntagonist activity against human P2Y4 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assay
ChEMBL 773 9 7 15 3.9 OS(=O)(=O)c1cc(Nc2ccc(c(c2)S(=O)(=O)O)Nc2nc(Cl)nc(n2)Nc2cccc(c2)S(=O)(=O)O)c2c(c1N)C(=O)c1c(C2=O)cccc1 10.1021/jm1012193
656725 10069 24 None -158 9 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity against human P2Y4 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assayAntagonist activity against human P2Y4 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assay
ChEMBL 773 9 7 15 3.9 OS(=O)(=O)c1cc(Nc2ccc(c(c2)S(=O)(=O)O)Nc2nc(Cl)nc(n2)Nc2cccc(c2)S(=O)(=O)O)c2c(c1N)C(=O)c1c(C2=O)cccc1 10.1021/jm1012193
CHEMBL1160031 10069 24 None -158 9 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity against human P2Y4 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assayAntagonist activity against human P2Y4 receptor expressed in 1321N1 astrocytoma cells by calcium mobilization assay
ChEMBL 773 9 7 15 3.9 OS(=O)(=O)c1cc(Nc2ccc(c(c2)S(=O)(=O)O)Nc2nc(Cl)nc(n2)Nc2cccc(c2)S(=O)(=O)O)c2c(c1N)C(=O)c1c(C2=O)cccc1 10.1021/jm1012193
136677322 10069 24 None -158 9 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at human P2Y4 receptor expressed in astrocytoma cells assessed as inhibition of intracellular calcium mobilizationAntagonist activity at human P2Y4 receptor expressed in astrocytoma cells assessed as inhibition of intracellular calcium mobilization
ChEMBL 773 9 7 15 3.9 OS(=O)(=O)c1cc(Nc2ccc(c(c2)S(=O)(=O)O)Nc2nc(Cl)nc(n2)Nc2cccc(c2)S(=O)(=O)O)c2c(c1N)C(=O)c1c(C2=O)cccc1 10.1021/jm901851t
1739 10069 24 None -158 9 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at human P2Y4 receptor expressed in astrocytoma cells assessed as inhibition of intracellular calcium mobilizationAntagonist activity at human P2Y4 receptor expressed in astrocytoma cells assessed as inhibition of intracellular calcium mobilization
ChEMBL 773 9 7 15 3.9 OS(=O)(=O)c1cc(Nc2ccc(c(c2)S(=O)(=O)O)Nc2nc(Cl)nc(n2)Nc2cccc(c2)S(=O)(=O)O)c2c(c1N)C(=O)c1c(C2=O)cccc1 10.1021/jm901851t
656725 10069 24 None -158 9 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at human P2Y4 receptor expressed in astrocytoma cells assessed as inhibition of intracellular calcium mobilizationAntagonist activity at human P2Y4 receptor expressed in astrocytoma cells assessed as inhibition of intracellular calcium mobilization
ChEMBL 773 9 7 15 3.9 OS(=O)(=O)c1cc(Nc2ccc(c(c2)S(=O)(=O)O)Nc2nc(Cl)nc(n2)Nc2cccc(c2)S(=O)(=O)O)c2c(c1N)C(=O)c1c(C2=O)cccc1 10.1021/jm901851t
CHEMBL1160031 10069 24 None -158 9 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at human P2Y4 receptor expressed in astrocytoma cells assessed as inhibition of intracellular calcium mobilizationAntagonist activity at human P2Y4 receptor expressed in astrocytoma cells assessed as inhibition of intracellular calcium mobilization
ChEMBL 773 9 7 15 3.9 OS(=O)(=O)c1cc(Nc2ccc(c(c2)S(=O)(=O)O)Nc2nc(Cl)nc(n2)Nc2cccc(c2)S(=O)(=O)O)c2c(c1N)C(=O)c1c(C2=O)cccc1 10.1021/jm901851t
1734 10738 50 None -3 7 Rat 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O None
3639 10738 50 None -3 7 Rat 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O None
6133 10738 50 None -3 7 Rat 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O None
CHEMBL336296 10738 50 None -3 7 Rat 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O None
DB04005 10738 50 None -3 7 Rat 8.3 pEC50 = 8.3 Functional
NoneNone
Drug Central 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O None
1713 7308 68 None -20 10 Rat 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N None
5957 7308 68 None -20 10 Rat 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N None
91 7308 68 None -20 10 Rat 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N None
CHEMBL14249 7308 68 None -20 10 Rat 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N None
DB00171 7308 68 None -20 10 Rat 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N None
1734 10738 50 None -1 7 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O None
3639 10738 50 None -1 7 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O None
6133 10738 50 None -1 7 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O None
CHEMBL336296 10738 50 None -1 7 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O None
DB04005 10738 50 None -1 7 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O None
148197 8220 23 None -1 3 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 790 14 10 21 -4.2 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O None
1736 8220 23 None -1 3 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 790 14 10 21 -4.2 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O None
4900 8220 23 None -1 3 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 790 14 10 21 -4.2 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O None
CHEMBL221326 8220 23 None -1 3 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 790 14 10 21 -4.2 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O None
DB15919 8220 23 None -1 3 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 790 14 10 21 -4.2 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O None
nan 8220 23 None -1 3 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 790 14 10 21 -4.2 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O None
1725 9927 17 None -100 6 Human 3.5 pEC50 = 3.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 511 8 5 11 1.4 O=Cc1c(COP(=O)(O)O)c(/N=N/c2ccc(cc2S(=O)(=O)O)S(=O)(=O)O)nc(c1O)C 18600475
4881 9927 17 None -100 6 Human 3.5 pEC50 = 3.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 511 8 5 11 1.4 O=Cc1c(COP(=O)(O)O)c(/N=N/c2ccc(cc2S(=O)(=O)O)S(=O)(=O)O)nc(c1O)C 18600475
CHEMBL1437958 9927 17 None -100 6 Human 3.5 pEC50 = 3.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 511 8 5 11 1.4 O=Cc1c(COP(=O)(O)O)c(/N=N/c2ccc(cc2S(=O)(=O)O)S(=O)(=O)O)nc(c1O)C 18600475
CHEMBL69234 9927 17 None -100 6 Human 3.5 pEC50 = 3.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 511 8 5 11 1.4 O=Cc1c(COP(=O)(O)O)c(/N=N/c2ccc(cc2S(=O)(=O)O)S(=O)(=O)O)nc(c1O)C 18600475
49867142 6841 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 323 4 5 9 -2.4 O[C@@H]1[C@H](O)[C@H](O[C@H]1n1ccc(=O)nc1N)COP(=O)(O)O 21417463
6201 6841 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 323 4 5 9 -2.4 O[C@@H]1[C@H](O)[C@H](O[C@H]1n1ccc(=O)nc1N)COP(=O)(O)O 21417463
CHEMBL1233534 6841 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 323 4 5 9 -2.4 O[C@@H]1[C@H](O)[C@H](O[C@H]1n1ccc(=O)nc1N)COP(=O)(O)O 21417463
1713 7308 68 None -630 10 Human 5.4 pEC50 = 5.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N 21193033
5957 7308 68 None -630 10 Human 5.4 pEC50 = 5.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N 21193033
91 7308 68 None -630 10 Human 5.4 pEC50 = 5.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N 21193033
CHEMBL14249 7308 68 None -630 10 Human 5.4 pEC50 = 5.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N 21193033
DB00171 7308 68 None -630 10 Human 5.4 pEC50 = 5.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N 21193033
1713 7308 68 None -20 10 Rat 6.0 pEC50 = 6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N 10779375
1713 7308 68 None -20 10 Rat 6.0 pEC50 = 6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N 12213051
1713 7308 68 None -20 10 Rat 6.0 pEC50 = 6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N 9647463
5957 7308 68 None -20 10 Rat 6.0 pEC50 = 6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N 10779375
5957 7308 68 None -20 10 Rat 6.0 pEC50 = 6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N 12213051
5957 7308 68 None -20 10 Rat 6.0 pEC50 = 6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N 9647463
91 7308 68 None -20 10 Rat 6.0 pEC50 = 6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N 10779375
91 7308 68 None -20 10 Rat 6.0 pEC50 = 6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N 12213051
91 7308 68 None -20 10 Rat 6.0 pEC50 = 6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N 9647463
CHEMBL14249 7308 68 None -20 10 Rat 6.0 pEC50 = 6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N 10779375
CHEMBL14249 7308 68 None -20 10 Rat 6.0 pEC50 = 6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N 12213051
CHEMBL14249 7308 68 None -20 10 Rat 6.0 pEC50 = 6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N 9647463
DB00171 7308 68 None -20 10 Rat 6.0 pEC50 = 6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N 10779375
DB00171 7308 68 None -20 10 Rat 6.0 pEC50 = 6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N 12213051
DB00171 7308 68 None -20 10 Rat 6.0 pEC50 = 6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N 9647463
1737 8149 7 None -2 3 Human 6.1 pEC50 = 6.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 773 14 9 21 -2.9 Nc1ccn(c(=O)n1)[C@@H]1O[C@@H]([C@H](C1)O)COP(=O)(OP(=O)(OP(=O)(OP(=O)(OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1ccc(=O)[nH]c1=O)O)O)O)O 12183642
9875516 8149 7 None -2 3 Human 6.1 pEC50 = 6.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 773 14 9 21 -2.9 Nc1ccn(c(=O)n1)[C@@H]1O[C@@H]([C@H](C1)O)COP(=O)(OP(=O)(OP(=O)(OP(=O)(OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1ccc(=O)[nH]c1=O)O)O)O)O 12183642
CHEMBL507282 8149 7 None -2 3 Human 6.1 pEC50 = 6.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 773 14 9 21 -2.9 Nc1ccn(c(=O)n1)[C@@H]1O[C@@H]([C@H](C1)O)COP(=O)(OP(=O)(OP(=O)(OP(=O)(OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1ccc(=O)[nH]c1=O)O)O)O)O 12183642
DB04983 8149 7 None -2 3 Human 6.1 pEC50 = 6.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 773 14 9 21 -2.9 Nc1ccn(c(=O)n1)[C@@H]1O[C@@H]([C@H](C1)O)COP(=O)(OP(=O)(OP(=O)(OP(=O)(OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1ccc(=O)[nH]c1=O)O)O)O)O 12183642
1734 10738 50 None -1 7 Human 6.3 pEC50 = 6.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10779375
3639 10738 50 None -1 7 Human 6.3 pEC50 = 6.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10779375
6133 10738 50 None -1 7 Human 6.3 pEC50 = 6.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10779375
CHEMBL336296 10738 50 None -1 7 Human 6.3 pEC50 = 6.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10779375
DB04005 10738 50 None -1 7 Human 6.3 pEC50 = 6.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10779375
148197 8220 23 None -1 3 Human 6.4 pEC50 = 6.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 790 14 10 21 -4.2 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 16475938
1736 8220 23 None -1 3 Human 6.4 pEC50 = 6.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 790 14 10 21 -4.2 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 16475938
4900 8220 23 None -1 3 Human 6.4 pEC50 = 6.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 790 14 10 21 -4.2 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 16475938
CHEMBL221326 8220 23 None -1 3 Human 6.4 pEC50 = 6.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 790 14 10 21 -4.2 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 16475938
DB15919 8220 23 None -1 3 Human 6.4 pEC50 = 6.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 790 14 10 21 -4.2 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 16475938
nan 8220 23 None -1 3 Human 6.4 pEC50 = 6.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 790 14 10 21 -4.2 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 16475938
1740 9609 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 494 8 7 11 -1.8 OC1C(n2ccc(=O)[nH]c2=O)C2C(C1O)(C2)COP(=O)(OP(=O)(OP(=O)(O)O)O)O 11754592
44309485 9609 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 494 8 7 11 -1.8 OC1C(n2ccc(=O)[nH]c2=O)C2C(C1O)(C2)COP(=O)(OP(=O)(OP(=O)(O)O)O)O 11754592
53262890 9671 0 None 16 3 Human 7.1 pEC50 = 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 603 12 7 13 -0.8 O[C@@H]1[C@H](O)[C@H](O[C@H]1n1cc/c(=N/OCCc2ccccc2)/[nH]c1=O)COP(=O)(OP(=O)(OP(=O)(O)O)O)O 21528910
6200 9671 0 None 16 3 Human 7.1 pEC50 = 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 603 12 7 13 -0.8 O[C@@H]1[C@H](O)[C@H](O[C@H]1n1cc/c(=N/OCCc2ccccc2)/[nH]c1=O)COP(=O)(OP(=O)(OP(=O)(O)O)O)O 21528910
CHEMBL1784893 9671 0 None 16 3 Human 7.1 pEC50 = 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 603 12 7 13 -0.8 O[C@@H]1[C@H](O)[C@H](O[C@H]1n1cc/c(=N/OCCc2ccccc2)/[nH]c1=O)COP(=O)(OP(=O)(OP(=O)(O)O)O)O 21528910
6199 9439 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 727 13 10 18 -3.4 OC[C@H]1O[C@H](OP(=O)(OP(=O)(OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)C2C=CC(=O)NC2=O)O)O)O)O)[C@@H]([C@H]([C@@H]1O)F)O 21528910
91827350 9439 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 727 13 10 18 -3.4 OC[C@H]1O[C@H](OP(=O)(OP(=O)(OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)C2C=CC(=O)NC2=O)O)O)O)O)[C@@H]([C@H]([C@@H]1O)F)O 21528910
4044 9443 3 None 26 3 Human 7.6 pEC50 = 7.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 617 13 7 13 -0.4 O[C@@H]1[C@H](O)[C@H](O[C@H]1n1cc/c(=N/OCCCc2ccccc2)/[nH]c1=O)COP(=O)(OP(=O)(OP(=O)(O)O)O)O 21528910
53262902 9443 3 None 26 3 Human 7.6 pEC50 = 7.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 617 13 7 13 -0.4 O[C@@H]1[C@H](O)[C@H](O[C@H]1n1cc/c(=N/OCCCc2ccccc2)/[nH]c1=O)COP(=O)(OP(=O)(OP(=O)(O)O)O)O 21528910
CHEMBL1784894 9443 3 None 26 3 Human 7.6 pEC50 = 7.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 617 13 7 13 -0.4 O[C@@H]1[C@H](O)[C@H](O[C@H]1n1cc/c(=N/OCCCc2ccccc2)/[nH]c1=O)COP(=O)(OP(=O)(OP(=O)(O)O)O)O 21528910
1741 8000 62 None 4 2 Rat 5.1 pEC50 None 5.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 483 8 7 13 -2.2 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(nc1=O)N 10779375
6176 8000 62 None 4 2 Rat 5.1 pEC50 None 5.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 483 8 7 13 -2.2 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(nc1=O)N 10779375
CHEMBL223533 8000 62 None 4 2 Rat 5.1 pEC50 None 5.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 483 8 7 13 -2.2 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(nc1=O)N 10779375
DB02431 8000 62 None 4 2 Rat 5.1 pEC50 None 5.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 483 8 7 13 -2.2 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(nc1=O)N 10779375
135398643 8882 0 None -4 2 Human 5.1 pEC50 None 5.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 508 8 7 13 -1.9 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1[nH]cnc2=O 10779375
1743 8882 0 None -4 2 Human 5.1 pEC50 None 5.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 508 8 7 13 -1.9 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1[nH]cnc2=O 10779375
CHEMBL1233686 8882 0 None -4 2 Human 5.1 pEC50 None 5.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 508 8 7 13 -1.9 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1[nH]cnc2=O 10779375
135398633 8671 0 None -2 2 Human 5.2 pEC50 None 5.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 523 8 8 14 -2.3 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1[nH]c(N)nc2=O 10779375
1742 8671 0 None -2 2 Human 5.2 pEC50 None 5.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 523 8 8 14 -2.3 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1[nH]c(N)nc2=O 10779375
CHEMBL1233147 8671 0 None -2 2 Human 5.2 pEC50 None 5.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 523 8 8 14 -2.3 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1[nH]c(N)nc2=O 10779375
DB04137 8671 0 None -2 2 Human 5.2 pEC50 None 5.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 523 8 8 14 -2.3 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1[nH]c(N)nc2=O 10779375
135398633 8671 0 None 2 2 Rat 5.6 pEC50 None 5.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 523 8 8 14 -2.3 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1[nH]c(N)nc2=O 10779375
1742 8671 0 None 2 2 Rat 5.6 pEC50 None 5.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 523 8 8 14 -2.3 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1[nH]c(N)nc2=O 10779375
CHEMBL1233147 8671 0 None 2 2 Rat 5.6 pEC50 None 5.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 523 8 8 14 -2.3 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1[nH]c(N)nc2=O 10779375
DB04137 8671 0 None 2 2 Rat 5.6 pEC50 None 5.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 523 8 8 14 -2.3 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1[nH]c(N)nc2=O 10779375
1734 10738 50 None -3 7 Rat 5.6 pEC50 None 5.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 9647463
3639 10738 50 None -3 7 Rat 5.6 pEC50 None 5.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 9647463
6133 10738 50 None -3 7 Rat 5.6 pEC50 None 5.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 9647463
CHEMBL336296 10738 50 None -3 7 Rat 5.6 pEC50 None 5.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 9647463
DB04005 10738 50 None -3 7 Rat 5.6 pEC50 None 5.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 9647463
135398643 8882 0 None 4 2 Rat 5.8 pEC50 None 5.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 508 8 7 13 -1.9 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1[nH]cnc2=O 10779375
135398643 8882 0 None 4 2 Rat 5.8 pEC50 None 5.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 508 8 7 13 -1.9 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1[nH]cnc2=O 9647463
1743 8882 0 None 4 2 Rat 5.8 pEC50 None 5.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 508 8 7 13 -1.9 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1[nH]cnc2=O 10779375
1743 8882 0 None 4 2 Rat 5.8 pEC50 None 5.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 508 8 7 13 -1.9 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1[nH]cnc2=O 9647463
CHEMBL1233686 8882 0 None 4 2 Rat 5.8 pEC50 None 5.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 508 8 7 13 -1.9 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1[nH]cnc2=O 10779375
CHEMBL1233686 8882 0 None 4 2 Rat 5.8 pEC50 None 5.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 508 8 7 13 -1.9 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1[nH]cnc2=O 9647463
1732 7238 0 None -6 4 Rat 5.9 pEC50 None 5.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 832 14 6 29 -5.0 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2cnc3c2ncnc3N)[O-])[O-])[O-])[O-])O[C@H]([C@@H]1O)n1cnc2c1ncnc2N 10779375
25243905 7238 0 None -6 4 Rat 5.9 pEC50 None 5.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 832 14 6 29 -5.0 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2cnc3c2ncnc3N)[O-])[O-])[O-])[O-])O[C@H]([C@@H]1O)n1cnc2c1ncnc2N 10779375
136677322 10069 24 None -446 9 Rat 4.7 pIC50 = 4.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 773 9 7 15 3.9 OS(=O)(=O)c1cc(Nc2ccc(c(c2)S(=O)(=O)O)Nc2nc(Cl)nc(n2)Nc2cccc(c2)S(=O)(=O)O)c2c(c1N)C(=O)c1c(C2=O)cccc1 9647463
1739 10069 24 None -446 9 Rat 4.7 pIC50 = 4.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 773 9 7 15 3.9 OS(=O)(=O)c1cc(Nc2ccc(c(c2)S(=O)(=O)O)Nc2nc(Cl)nc(n2)Nc2cccc(c2)S(=O)(=O)O)c2c(c1N)C(=O)c1c(C2=O)cccc1 9647463
656725 10069 24 None -446 9 Rat 4.7 pIC50 = 4.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 773 9 7 15 3.9 OS(=O)(=O)c1cc(Nc2ccc(c(c2)S(=O)(=O)O)Nc2nc(Cl)nc(n2)Nc2cccc(c2)S(=O)(=O)O)c2c(c1N)C(=O)c1c(C2=O)cccc1 9647463
CHEMBL1160031 10069 24 None -446 9 Rat 4.7 pIC50 = 4.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 773 9 7 15 3.9 OS(=O)(=O)c1cc(Nc2ccc(c(c2)S(=O)(=O)O)Nc2nc(Cl)nc(n2)Nc2cccc(c2)S(=O)(=O)O)c2c(c1N)C(=O)c1c(C2=O)cccc1 9647463
11451 9985 0 None 6 5 Human 6.6 pIC50 = 6.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 530 5 3 7 5.8 Nc1c2C(=O)c3ccccc3C(=O)c2c(cc1S(=O)(=O)O)Nc1ccc(cc1)Sc1ccc(c(c1)C)C 28306255
132574707 9985 0 None 6 5 Human 6.6 pIC50 = 6.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 530 5 3 7 5.8 Nc1c2C(=O)c3ccccc3C(=O)c2c(cc1S(=O)(=O)O)Nc1ccc(cc1)Sc1ccc(c(c1)C)C 28306255
CHEMBL4116316 9985 0 None 6 5 Human 6.6 pIC50 = 6.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 530 5 3 7 5.8 Nc1c2C(=O)c3ccccc3C(=O)c2c(cc1S(=O)(=O)O)Nc1ccc(cc1)Sc1ccc(c(c1)C)C 28306255


Get vendors


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
1713 7308 68 None - 2 Rat 5.9 pEC50 = 5.9 Binding
Antagonist activity at rat P2Y4Antagonist activity at rat P2Y4
ChEMBL 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.5b01972
5957 7308 68 None - 2 Rat 5.9 pEC50 = 5.9 Binding
Antagonist activity at rat P2Y4Antagonist activity at rat P2Y4
ChEMBL 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.5b01972
91 7308 68 None - 2 Rat 5.9 pEC50 = 5.9 Binding
Antagonist activity at rat P2Y4Antagonist activity at rat P2Y4
ChEMBL 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.5b01972
CHEMBL14249 7308 68 None - 2 Rat 5.9 pEC50 = 5.9 Binding
Antagonist activity at rat P2Y4Antagonist activity at rat P2Y4
ChEMBL 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.5b01972
DB00171 7308 68 None - 2 Rat 5.9 pEC50 = 5.9 Binding
Antagonist activity at rat P2Y4Antagonist activity at rat P2Y4
ChEMBL 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.5b01972
90656232 117696 0 None - 0 Human 5.9 pEC50 = 5.9 Binding
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells by functional assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells by functional assay
ChEMBL 1056 24 10 23 0.0 O=c1[nH]/c(=N\OCCCc2ccccc2)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]2O[C@@H](n3cc/c(=N/OCCCc4ccccc4)[nH]c3=O)[C@H](O)[C@@H]2O)[C@@H](O)[C@H]1O 10.1021/jm500367e
CHEMBL3261380 117696 0 None - 0 Human 5.9 pEC50 = 5.9 Binding
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells by functional assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells by functional assay
ChEMBL 1056 24 10 23 0.0 O=c1[nH]/c(=N\OCCCc2ccccc2)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]2O[C@@H](n3cc/c(=N/OCCCc4ccccc4)[nH]c3=O)[C@H](O)[C@@H]2O)[C@@H](O)[C@H]1O 10.1021/jm500367e
1734 10738 50 None - 0 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at human P2Y4 transfected in human 1321N1 cellsAgonist activity at human P2Y4 transfected in human 1321N1 cells
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/acs.jmedchem.5b01972
3639 10738 50 None - 0 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at human P2Y4 transfected in human 1321N1 cellsAgonist activity at human P2Y4 transfected in human 1321N1 cells
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/acs.jmedchem.5b01972
6133 10738 50 None - 0 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at human P2Y4 transfected in human 1321N1 cellsAgonist activity at human P2Y4 transfected in human 1321N1 cells
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/acs.jmedchem.5b01972
CHEMBL336296 10738 50 None - 0 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at human P2Y4 transfected in human 1321N1 cellsAgonist activity at human P2Y4 transfected in human 1321N1 cells
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/acs.jmedchem.5b01972
DB04005 10738 50 None - 0 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at human P2Y4 transfected in human 1321N1 cellsAgonist activity at human P2Y4 transfected in human 1321N1 cells
ChEMBL 484 8 7 12 -2.5 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/acs.jmedchem.5b01972
1713 7308 68 None 257 2 Human 5.2 pEC50 = 5.2 Binding
Antagonist activity at human P2Y4Antagonist activity at human P2Y4
ChEMBL 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.5b01972
5957 7308 68 None 257 2 Human 5.2 pEC50 = 5.2 Binding
Antagonist activity at human P2Y4Antagonist activity at human P2Y4
ChEMBL 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.5b01972
91 7308 68 None 257 2 Human 5.2 pEC50 = 5.2 Binding
Antagonist activity at human P2Y4Antagonist activity at human P2Y4
ChEMBL 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.5b01972
CHEMBL14249 7308 68 None 257 2 Human 5.2 pEC50 = 5.2 Binding
Antagonist activity at human P2Y4Antagonist activity at human P2Y4
ChEMBL 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.5b01972
DB00171 7308 68 None 257 2 Human 5.2 pEC50 = 5.2 Binding
Antagonist activity at human P2Y4Antagonist activity at human P2Y4
ChEMBL 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N 10.1021/acs.jmedchem.5b01972
136677322 10069 24 None - 1 Rat 5.2 pEC50 = 5.2 Binding
Antagonist activity at rat P2Y4 transfected in xenopus oocyte cellAntagonist activity at rat P2Y4 transfected in xenopus oocyte cell
ChEMBL 773 9 7 15 3.9 OS(=O)(=O)c1cc(Nc2ccc(c(c2)S(=O)(=O)O)Nc2nc(Cl)nc(n2)Nc2cccc(c2)S(=O)(=O)O)c2c(c1N)C(=O)c1c(C2=O)cccc1 10.1021/acs.jmedchem.5b01972
1739 10069 24 None - 1 Rat 5.2 pEC50 = 5.2 Binding
Antagonist activity at rat P2Y4 transfected in xenopus oocyte cellAntagonist activity at rat P2Y4 transfected in xenopus oocyte cell
ChEMBL 773 9 7 15 3.9 OS(=O)(=O)c1cc(Nc2ccc(c(c2)S(=O)(=O)O)Nc2nc(Cl)nc(n2)Nc2cccc(c2)S(=O)(=O)O)c2c(c1N)C(=O)c1c(C2=O)cccc1 10.1021/acs.jmedchem.5b01972
656725 10069 24 None - 1 Rat 5.2 pEC50 = 5.2 Binding
Antagonist activity at rat P2Y4 transfected in xenopus oocyte cellAntagonist activity at rat P2Y4 transfected in xenopus oocyte cell
ChEMBL 773 9 7 15 3.9 OS(=O)(=O)c1cc(Nc2ccc(c(c2)S(=O)(=O)O)Nc2nc(Cl)nc(n2)Nc2cccc(c2)S(=O)(=O)O)c2c(c1N)C(=O)c1c(C2=O)cccc1 10.1021/acs.jmedchem.5b01972
CHEMBL1160031 10069 24 None - 1 Rat 5.2 pEC50 = 5.2 Binding
Antagonist activity at rat P2Y4 transfected in xenopus oocyte cellAntagonist activity at rat P2Y4 transfected in xenopus oocyte cell
ChEMBL 773 9 7 15 3.9 OS(=O)(=O)c1cc(Nc2ccc(c(c2)S(=O)(=O)O)Nc2nc(Cl)nc(n2)Nc2cccc(c2)S(=O)(=O)O)c2c(c1N)C(=O)c1c(C2=O)cccc1 10.1021/acs.jmedchem.5b01972
90656231 117695 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells by functional assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells by functional assay
ChEMBL 923 19 10 22 -2.1 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]3O[C@@H](n4cc/c(=N/OCCCc5ccccc5)[nH]c4=O)[C@H](O)[C@@H]3O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm500367e
CHEMBL3261379 117695 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at human P2Y4 receptor expressed in human 1321N1 cells by functional assayAgonist activity at human P2Y4 receptor expressed in human 1321N1 cells by functional assay
ChEMBL 923 19 10 22 -2.1 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OP(=O)(O)OP(=O)(O)OC[C@H]3O[C@@H](n4cc/c(=N/OCCCc5ccccc5)[nH]c4=O)[C@H](O)[C@@H]3O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm500367e
1713 7308 68 None 257 2 Human 6.2 pKd = 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N 10779375
5957 7308 68 None 257 2 Human 6.2 pKd = 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N 10779375
91 7308 68 None 257 2 Human 6.2 pKd = 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N 10779375
CHEMBL14249 7308 68 None 257 2 Human 6.2 pKd = 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N 10779375
DB00171 7308 68 None 257 2 Human 6.2 pKd = 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N 10779375
1713 7308 68 None 257 2 Human 8.2 pKi = 8.2 Binding
GRAC: human P2Y4 selective antagonistGRAC: human P2Y4 selective antagonist
Drug Central 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N None
5957 7308 68 None 257 2 Human 8.2 pKi = 8.2 Binding
GRAC: human P2Y4 selective antagonistGRAC: human P2Y4 selective antagonist
Drug Central 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N None
91 7308 68 None 257 2 Human 8.2 pKi = 8.2 Binding
GRAC: human P2Y4 selective antagonistGRAC: human P2Y4 selective antagonist
Drug Central 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N None
CHEMBL14249 7308 68 None 257 2 Human 8.2 pKi = 8.2 Binding
GRAC: human P2Y4 selective antagonistGRAC: human P2Y4 selective antagonist
Drug Central 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N None
DB00171 7308 68 None 257 2 Human 8.2 pKi = 8.2 Binding
GRAC: human P2Y4 selective antagonistGRAC: human P2Y4 selective antagonist
Drug Central 507 8 7 14 -1.6 O[C@@H]1[C@@H](COP(=O)(OP(=O)(OP(=O)(O)O)O)O)O[C@H]([C@@H]1O)n1cnc2c1ncnc2N None