Ligand source activities (1 row/activity)



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Ligands Receptor Assay information Chemical information
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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 110414 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 110414 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 3903 45 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 3903 45 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 3903 45 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 3903 45 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 3903 45 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 130 8 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 130 8 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 130 8 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 110415 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 110415 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 62591 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 62591 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 183566 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 183566 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 110417 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 110417 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 14086 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 14086 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 14086 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 14086 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 14086 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 14086 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 14086 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 14086 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 141073 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 141073 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 141073 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 141073 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 191996 0 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 191996 0 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 110426 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 110426 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 1410 19 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 1410 19 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 1410 19 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 1410 19 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 1410 19 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 1410 19 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 1410 19 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 1410 19 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 1410 19 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 1410 19 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 1410 19 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 1410 19 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 1410 19 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 1410 19 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 1410 19 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 1340 6 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 1340 6 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 1340 6 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 1340 6 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 3859 30 None -158 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 3859 30 None -158 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 3859 30 None -158 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 3859 30 None -158 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 3859 30 None -158 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 110416 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 110416 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 61009 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 61009 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 207404 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 90 4 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 90 4 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 90 4 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 169419 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 169419 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 169419 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 169419 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 14084 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 14084 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 14084 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 516 63 None -13 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 516 63 None -13 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
91 516 63 None -13 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 516 63 None -13 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 516 63 None -13 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 62588 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 62588 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 183716 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 183716 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 183716 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 183716 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 110424 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 110424 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 112310 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 112310 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 112310 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 90839 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 90839 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 187626 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 187626 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 187626 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 187626 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 62593 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 62593 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 62594 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 62594 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 62531 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 62531 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 108937 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 108937 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 62600 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 62600 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 125 9 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 125 9 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 125 9 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 110421 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 110421 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 125 9 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 125 9 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 125 9 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 2627 2 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 2627 2 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 2627 2 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 2618 5 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 2618 5 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 2618 5 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 2618 5 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 2618 5 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 2618 5 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 14081 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 14081 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 14081 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 14081 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 14081 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 14081 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 110423 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 110423 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 3903 45 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 3903 45 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 3903 45 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 3903 45 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 3903 45 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 183693 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 183693 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 62599 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 62599 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 3903 45 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 3903 45 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 3903 45 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 3903 45 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 3903 45 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 191299 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 191299 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 191299 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 191299 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 191992 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 191992 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 80743 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 80743 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 110422 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 110422 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 14077 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 14077 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 14077 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 116645 12 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 116645 12 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 62530 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 62530 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 14065 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 14065 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 14065 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 108942 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 108942 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 130 8 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 130 8 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 130 8 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 90 4 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 90 4 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 90 4 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 90 4 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 90 4 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 90 4 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 90 4 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 90 4 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 90 4 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 197698 3 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 197698 3 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 108934 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 108934 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 153915 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 153915 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 191206 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 191206 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 3903 45 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 3903 45 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 3903 45 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 3903 45 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 3903 45 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 3903 45 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 3903 45 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 3903 45 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 3903 45 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 3903 45 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 83816 3 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 83816 3 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 60759 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 60759 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 82024 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 82024 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 110428 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 110428 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 1410 19 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 1410 19 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 1410 19 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 1410 19 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 1410 19 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 14688 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 14688 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 14688 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 110425 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 110425 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 91536 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 91536 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 146884 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 146884 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 110413 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 110413 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 516 63 None -812 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 516 63 None -812 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
91 516 63 None -812 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 516 63 None -812 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 516 63 None -812 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 173418 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 173418 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 61017 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 61017 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 62589 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 62589 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 61013 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 61013 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 183649 9 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 183649 9 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 183747 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 183747 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 110427 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 110427 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 110411 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 110411 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 172026 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 172026 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 3903 45 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 3903 45 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 3903 45 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 3903 45 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 3903 45 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 3903 45 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 3903 45 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 3903 45 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 3903 45 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 3903 45 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 199998 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 199998 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 61010 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 61010 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 53 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 53 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 53 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 14081 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 14081 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 14081 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 3903 45 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 3903 45 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 3903 45 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 3903 45 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 3903 45 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 183535 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 183535 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 183501 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 183501 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 110412 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 110412 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 188173 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 188173 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 183502 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 183502 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 6537 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 6537 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 61011 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 61011 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 61555 13 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 61555 13 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 62601 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 62601 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 62590 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 62590 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 14119 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 14119 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 14119 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 187752 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 187752 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 108939 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 108939 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 197349 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 197349 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 197349 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 197349 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 197349 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 62529 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 62529 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 2628 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 2628 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 2628 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 147054 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 147054 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 188460 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 188460 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 80075 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 80075 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 3903 45 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 3903 45 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 3903 45 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 3903 45 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 3903 45 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 2852 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 2852 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 2852 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 60756 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 60756 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 183649 9 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 183649 9 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 108935 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 108935 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 60757 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 60757 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 14074 2 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 14074 2 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 14074 2 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 14074 2 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 14074 2 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 14074 2 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 14074 2 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 14074 2 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 183780 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 183780 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 188089 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 188089 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 3903 45 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 3903 45 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 3903 45 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 3903 45 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 3903 45 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 1340 6 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 1340 6 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 1340 6 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 1340 6 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 183746 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 183746 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 83840 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 83840 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 110420 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 110420 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 6674 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 6674 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 199998 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 199998 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 3903 45 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 3903 45 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 3903 45 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 3903 45 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 3903 45 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 1410 19 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 1410 19 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 1410 19 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 1410 19 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 1410 19 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 90284 0 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 90284 0 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 90284 0 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 90284 0 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 90284 0 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 90284 0 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 3903 45 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 3903 45 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 3903 45 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 3903 45 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 3903 45 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 3903 45 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 3903 45 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 3903 45 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 3903 45 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 3903 45 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 3903 45 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 3903 45 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 3903 45 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 3903 45 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 3903 45 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 191206 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 191206 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 3903 45 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 3903 45 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 3903 45 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 3903 45 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 3903 45 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 3903 45 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 3903 45 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 3903 45 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 3903 45 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 3903 45 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 110418 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 110418 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 62592 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 62592 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 3159 9 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 3159 9 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 3159 9 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 207404 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 110419 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 110419 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 108938 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 108938 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 62595 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 62595 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 62595 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 62595 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 14749 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 14749 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 14749 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 59934 5 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 59934 5 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 59934 5 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 59940 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 59940 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 59940 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 59941 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 59941 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 59941 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 157033 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 157033 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 14757 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 14757 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 14757 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 14561 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 14561 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 14561 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 3244 22 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 3244 22 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 3244 22 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 3244 22 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 14750 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 14750 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 14750 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 59939 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 59939 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 59939 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 190738 26 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 190738 26 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 59945 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 59945 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 59945 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 14754 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 14754 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 14754 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 14762 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 14762 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 14762 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 59937 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 59937 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 59937 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 160518 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 160518 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 160518 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 160599 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 160599 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 160599 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 160505 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 160505 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 160505 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 59934 5 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 59934 5 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 59934 5 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 160532 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 160532 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 160532 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 14665 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 14665 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 14665 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 14782 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 14782 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 14782 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 14556 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 14556 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 14556 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 160470 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 160470 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 160470 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 14581 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 14581 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 14581 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 160459 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 160459 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 160459 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 14747 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 14747 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 14747 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 14718 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 14718 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 14718 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 160483 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 160483 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 160483 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 14581 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 14581 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 14581 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 14784 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 14784 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 14784 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 14747 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 14747 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 14747 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 14556 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 14556 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 14556 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 14556 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 14556 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 14556 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 3166 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 3166 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 3166 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 14667 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 14667 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 14667 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 14775 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 14775 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 14775 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 14682 9 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 14682 9 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 14682 9 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 160560 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 160560 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 160560 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 14787 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 14787 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 14787 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 59945 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 59945 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 59945 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 14582 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 14582 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 14582 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 14747 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 14747 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 14747 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 160559 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 160559 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 160559 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 14785 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 14785 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 14785 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 160539 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 160539 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 160539 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 14744 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 14744 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 14744 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 14563 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 14563 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 14563 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 14666 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 14666 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 14666 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 14560 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 14560 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 14560 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 160471 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 160471 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 160471 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 160540 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 160540 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 160540 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 14568 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 14568 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 14568 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 14786 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 14786 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 14786 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 160530 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 160530 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 160530 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 160586 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 160586 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 160586 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 3162 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 3162 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 3162 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 160673 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 160673 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 160673 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 14568 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 14568 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 14568 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 3244 22 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 3244 22 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 3244 22 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 3244 22 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 14777 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 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 14777 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 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 14777 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 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 10116 5 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 10116 5 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 10116 5 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 10116 5 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 59943 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 59943 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 59943 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 59938 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 59938 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 59938 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 14755 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 14755 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 14755 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 54684 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 54684 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 54684 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 14757 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 14757 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 14757 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 160566 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 160566 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 160566 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 59935 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 59935 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 59935 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 160660 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 160660 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 160660 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 3244 22 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 3244 22 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 3244 22 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 3244 22 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 3244 22 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 3244 22 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 3244 22 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 3244 22 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 3903 45 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 3903 45 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 3903 45 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 3903 45 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 3903 45 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 516 63 None -13 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 516 63 None -13 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
91 516 63 None -13 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 516 63 None -13 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 516 63 None -13 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 3903 45 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 3903 45 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 3903 45 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 3903 45 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 3903 45 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 1410 19 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 1410 19 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 1410 19 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 1410 19 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 1410 19 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 3104 14 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 3104 14 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 3104 14 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 3104 14 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 53 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 53 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 53 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 516 63 None -812 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 516 63 None -812 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
91 516 63 None -812 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 516 63 None -812 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 516 63 None -812 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 516 63 None -13 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 516 63 None -13 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 516 63 None -13 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 516 63 None -13 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 516 63 None -13 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 516 63 None -13 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
91 516 63 None -13 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
91 516 63 None -13 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
91 516 63 None -13 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 516 63 None -13 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 516 63 None -13 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 516 63 None -13 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 516 63 None -13 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 516 63 None -13 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 516 63 None -13 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 1340 6 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 1340 6 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 1340 6 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 1340 6 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 3903 45 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 3903 45 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 3903 45 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 3903 45 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 3903 45 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 1410 19 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 1410 19 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 1410 19 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 1410 19 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 1410 19 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 2791 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 2791 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 2852 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 2852 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 2852 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 2623 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 2623 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 2627 2 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 2627 2 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 2627 2 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 1192 55 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 1192 55 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 1192 55 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 1192 55 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 2070 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 2070 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 2070 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 1859 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 1859 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 1859 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 1859 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 1859 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 1859 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 1859 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 1859 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 3903 45 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 3903 45 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 3903 45 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 3903 45 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 3903 45 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 2070 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 2070 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 2070 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 2070 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 2070 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 2070 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 446 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 446 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 3244 22 None -794 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 3244 22 None -794 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 3244 22 None -794 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 3244 22 None -794 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 3162 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 3162 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 3162 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


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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
90656232 110430 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 110430 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
90656231 110429 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 110429 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 516 63 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 516 63 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
91 516 63 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 516 63 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 516 63 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 516 63 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 516 63 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
91 516 63 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 516 63 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 516 63 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