Ligand source activities (1 row/activity)





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DOI

44627488 20945 0 None 2187 2 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production
ChEMBL 418 6 6 9 -1.1 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)CP(=O)(O)O)[C@@H](O)[C@H]2O)c(=S)[nH]1 10.1021/jm901432g
CHEMBL1198696 20945 0 None 2187 2 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production
ChEMBL 418 6 6 9 -1.1 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)CP(=O)(O)O)[C@@H](O)[C@H]2O)c(=S)[nH]1 10.1021/jm901432g
CHEMBL611791 20945 0 None 2187 2 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production
ChEMBL 418 6 6 9 -1.1 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)CP(=O)(O)O)[C@@H](O)[C@H]2O)c(=S)[nH]1 10.1021/jm901432g
16082712 6877 1 None 85 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production
ChEMBL 420 6 6 10 -1.2 O[C@@H]1[C@@H](COP(=O)(OP(=O)(O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=S 10.1021/jm901432g
6202 6877 1 None 85 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production
ChEMBL 420 6 6 10 -1.2 O[C@@H]1[C@@H](COP(=O)(OP(=O)(O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=S 10.1021/jm901432g
CHEMBL216011 6877 1 None 85 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production
ChEMBL 420 6 6 10 -1.2 O[C@@H]1[C@@H](COP(=O)(OP(=O)(O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=S 10.1021/jm901432g
1748 9436 1 None 51 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production
ChEMBL 402 6 6 9 -2.5 O[C@@H]1[C@@H](COP(=O)(CP(=O)(O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm901432g
44585949 9436 1 None 51 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production
ChEMBL 402 6 6 9 -2.5 O[C@@H]1[C@@H](COP(=O)(CP(=O)(O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm901432g
CHEMBL507060 9436 1 None 51 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production
ChEMBL 402 6 6 9 -2.5 O[C@@H]1[C@@H](COP(=O)(CP(=O)(O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm901432g
44627599 20946 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production
ChEMBL 472 9 5 11 -0.2 C#CCCOP(=O)(O)OP(=O)(O)OC[C@H]1O[C@@H](n2ccc(=O)[nH]c2=S)[C@H](O)[C@@H]1O 10.1021/jm901432g
CHEMBL1198697 20946 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production
ChEMBL 472 9 5 11 -0.2 C#CCCOP(=O)(O)OP(=O)(O)OC[C@H]1O[C@@H](n2ccc(=O)[nH]c2=S)[C@H](O)[C@@H]1O 10.1021/jm901432g
CHEMBL611792 20946 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production
ChEMBL 472 9 5 11 -0.2 C#CCCOP(=O)(O)OP(=O)(O)OC[C@H]1O[C@@H](n2ccc(=O)[nH]c2=S)[C@H](O)[C@@H]1O 10.1021/jm901432g
16220889 143730 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production
ChEMBL 582 9 9 16 -3.4 O=c1[nH]c(=S)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)O[C@H]2O[C@H](CO)[C@@H](O)[C@H](O)[C@H]2O)[C@@H](O)[C@H]1O 10.1021/jm901432g
CHEMBL374384 143730 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production
ChEMBL 582 9 9 16 -3.4 O=c1[nH]c(=S)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)O[C@H]2O[C@H](CO)[C@@H](O)[C@H](O)[C@H]2O)[C@@H](O)[C@H]1O 10.1021/jm901432g
1748 9436 1 None 51 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human recombinant P2Y14 receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y14 receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation proximity assay
ChEMBL 402 6 6 9 -2.5 O[C@@H]1[C@@H](COP(=O)(CP(=O)(O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm100287t
44585949 9436 1 None 51 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human recombinant P2Y14 receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y14 receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation proximity assay
ChEMBL 402 6 6 9 -2.5 O[C@@H]1[C@@H](COP(=O)(CP(=O)(O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm100287t
CHEMBL507060 9436 1 None 51 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human recombinant P2Y14 receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y14 receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation proximity assay
ChEMBL 402 6 6 9 -2.5 O[C@@H]1[C@@H](COP(=O)(CP(=O)(O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm100287t
46890713 20985 0 None -1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant P2Y14 receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y14 receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation proximity assay
ChEMBL 528 6 6 9 -1.9 O=c1[nH]c(=O)n([C@@H]2O[C@H](COP(=O)(O)CP(=O)(O)O)[C@@H](O)[C@H]2O)cc1I 10.1021/jm100287t
CHEMBL1085561 20985 0 None -1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant P2Y14 receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y14 receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation proximity assay
ChEMBL 528 6 6 9 -1.9 O=c1[nH]c(=O)n([C@@H]2O[C@H](COP(=O)(O)CP(=O)(O)O)[C@@H](O)[C@H]2O)cc1I 10.1021/jm100287t
CHEMBL1198914 20985 0 None -1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant P2Y14 receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y14 receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation proximity assay
ChEMBL 528 6 6 9 -1.9 O=c1[nH]c(=O)n([C@@H]2O[C@H](COP(=O)(O)CP(=O)(O)O)[C@@H](O)[C@H]2O)cc1I 10.1021/jm100287t
CHEMBL4851033 20985 0 None -1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant P2Y14 receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y14 receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation proximity assay
ChEMBL 528 6 6 9 -1.9 O=c1[nH]c(=O)n([C@@H]2O[C@H](COP(=O)(O)CP(=O)(O)O)[C@@H](O)[C@H]2O)cc1I 10.1021/jm100287t
45485237 203785 0 None -1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production
ChEMBL 564 6 6 9 -1.3 O=c1[nH]c(=O)n([C@@H]2O[C@H](COP(=O)(O)C(F)(F)P(=O)(O)O)[C@@H](O)[C@H]2O)cc1I 10.1021/jm901432g
CHEMBL566925 203785 0 None -1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production
ChEMBL 564 6 6 9 -1.3 O=c1[nH]c(=O)n([C@@H]2O[C@H](COP(=O)(O)C(F)(F)P(=O)(O)O)[C@@H](O)[C@H]2O)cc1I 10.1021/jm901432g
44627802 20956 0 None 1 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production
ChEMBL 525 9 5 13 -0.6 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)Oc3ccc([N+](=O)[O-])cc3)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm901432g
CHEMBL1198725 20956 0 None 1 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production
ChEMBL 525 9 5 13 -0.6 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)Oc3ccc([N+](=O)[O-])cc3)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm901432g
CHEMBL612119 20956 0 None 1 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production
ChEMBL 525 9 5 13 -0.6 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)Oc3ccc([N+](=O)[O-])cc3)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm901432g
146015339 10694 32 None 1 7 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production
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/jm901432g
1749 10694 32 None 1 7 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production
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/jm901432g
6031 10694 32 None 1 7 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production
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/jm901432g
CHEMBL130266 10694 32 None 1 7 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production
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/jm901432g
DB03435 10694 32 None 1 7 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production
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/jm901432g
146015339 10694 32 None 1 7 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant P2Y14 receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y14 receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production 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/jm100287t
1749 10694 32 None 1 7 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant P2Y14 receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y14 receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production 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/jm100287t
6031 10694 32 None 1 7 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant P2Y14 receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y14 receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production 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/jm100287t
CHEMBL130266 10694 32 None 1 7 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant P2Y14 receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y14 receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production 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/jm100287t
DB03435 10694 32 None 1 7 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant P2Y14 receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y14 receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production 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/jm100287t
44627690 21053 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production
ChEMBL 478 10 7 13 -3.2 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OCC(O)CO)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm901432g
CHEMBL1162560 21053 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production
ChEMBL 478 10 7 13 -3.2 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OCC(O)CO)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm901432g
CHEMBL1199753 21053 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production
ChEMBL 478 10 7 13 -3.2 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OCC(O)CO)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm901432g
44627692 20955 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production
ChEMBL 478 10 7 13 -3.2 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OC(CO)CO)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm901432g
CHEMBL1198717 20955 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production
ChEMBL 478 10 7 13 -3.2 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OC(CO)CO)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm901432g
CHEMBL612065 20955 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production
ChEMBL 478 10 7 13 -3.2 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OC(CO)CO)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm901432g
44627804 21124 0 None 4 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production
ChEMBL 514 8 5 11 0.1 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)Oc3cccc(Cl)c3)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm901432g
CHEMBL1162561 21124 0 None 4 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production
ChEMBL 514 8 5 11 0.1 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)Oc3cccc(Cl)c3)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm901432g
CHEMBL1200114 21124 0 None 4 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production
ChEMBL 514 8 5 11 0.1 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)Oc3cccc(Cl)c3)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm901432g
16221095 150625 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human P2Y14 expressed in COS7 cells assessed as stimulation of PLC-mediated [3H]inositol hydrolysisAgonist activity at human P2Y14 expressed in COS7 cells assessed as stimulation of PLC-mediated [3H]inositol hydrolysis
ChEMBL 566 8 10 16 -5.4 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)O[C@@H]3[C@@H](O)[C@H](O)[C@@H](O)[C@H](O)[C@H]3O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm061222w
CHEMBL390160 150625 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human P2Y14 expressed in COS7 cells assessed as stimulation of PLC-mediated [3H]inositol hydrolysisAgonist activity at human P2Y14 expressed in COS7 cells assessed as stimulation of PLC-mediated [3H]inositol hydrolysis
ChEMBL 566 8 10 16 -5.4 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)O[C@@H]3[C@@H](O)[C@H](O)[C@@H](O)[C@H](O)[C@H]3O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm061222w
46226448 206489 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human P2Y14 receptor expressed in human COS7 cellsAgonist activity at human P2Y14 receptor expressed in human COS7 cells
ChEMBL 566 8 10 16 -5.4 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)O[C@H]3[C@H](O)[C@@H](O)[C@H](O)[C@@H](O)[C@H]3O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1016/j.bmc.2009.05.024
CHEMBL593346 206489 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human P2Y14 receptor expressed in human COS7 cellsAgonist activity at human P2Y14 receptor expressed in human COS7 cells
ChEMBL 566 8 10 16 -5.4 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)O[C@H]3[C@H](O)[C@@H](O)[C@H](O)[C@@H](O)[C@H]3O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1016/j.bmc.2009.05.024
44627806 21054 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production
ChEMBL 510 9 5 12 -0.5 COc1ccc(OP(=O)(O)OP(=O)(O)OC[C@H]2O[C@@H](n3ccc(=O)[nH]c3=O)[C@H](O)[C@@H]2O)cc1 10.1021/jm901432g
CHEMBL1162562 21054 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production
ChEMBL 510 9 5 12 -0.5 COc1ccc(OP(=O)(O)OP(=O)(O)OC[C@H]2O[C@@H](n3ccc(=O)[nH]c3=O)[C@H](O)[C@@H]2O)cc1 10.1021/jm901432g
CHEMBL1199754 21054 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production
ChEMBL 510 9 5 12 -0.5 COc1ccc(OP(=O)(O)OP(=O)(O)OC[C@H]2O[C@@H](n3ccc(=O)[nH]c3=O)[C@H](O)[C@@H]2O)cc1 10.1021/jm901432g
46226460 206807 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human P2Y14 receptor expressed in human COS7 cellsAgonist activity at human P2Y14 receptor expressed in human COS7 cells
ChEMBL 536 9 8 15 -4.2 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OC[C@H]3O[C@H](O)[C@H](O)[C@@H]3O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1016/j.bmc.2009.05.024
CHEMBL595467 206807 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human P2Y14 receptor expressed in human COS7 cellsAgonist activity at human P2Y14 receptor expressed in human COS7 cells
ChEMBL 536 9 8 15 -4.2 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OC[C@H]3O[C@H](O)[C@H](O)[C@@H]3O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1016/j.bmc.2009.05.024
448923 206550 9 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human P2Y14 receptor expressed in human COS7 cellsAgonist activity at human P2Y14 receptor expressed in human COS7 cells
ChEMBL 568 9 8 15 -3.8 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)O[C@H]3O[C@H](CO)[C@@H](O)[C@H](O)[C@H]3F)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1016/j.bmc.2009.05.024
CHEMBL593830 206550 9 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human P2Y14 receptor expressed in human COS7 cellsAgonist activity at human P2Y14 receptor expressed in human COS7 cells
ChEMBL 568 9 8 15 -3.8 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)O[C@H]3O[C@H](CO)[C@@H](O)[C@H](O)[C@H]3F)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1016/j.bmc.2009.05.024
44627694 21038 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production
ChEMBL 460 7 5 11 -0.8 CC(C)(C)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/jm901432g
CHEMBL1162552 21038 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production
ChEMBL 460 7 5 11 -0.8 CC(C)(C)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/jm901432g
CHEMBL1199701 21038 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production
ChEMBL 460 7 5 11 -0.8 CC(C)(C)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/jm901432g
46226445 208352 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human P2Y14 receptor expressed in human COS7 cellsAgonist activity at human P2Y14 receptor expressed in human COS7 cells
ChEMBL 622 11 10 17 -5.7 NCCNC(=O)[C@H]1O[C@H](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 10.1016/j.bmc.2009.05.024
CHEMBL605512 208352 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human P2Y14 receptor expressed in human COS7 cellsAgonist activity at human P2Y14 receptor expressed in human COS7 cells
ChEMBL 622 11 10 17 -5.7 NCCNC(=O)[C@H]1O[C@H](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 10.1016/j.bmc.2009.05.024
1783 10697 25 None -13 7 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human P2Y14 receptor expressed in human COS7 cellsAgonist activity at human P2Y14 receptor expressed in human COS7 cells
ChEMBL 566 9 9 16 -4.8 OC[C@H]1O[C@H](OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)[C@@H]([C@H]([C@@H]1O)O)O 10.1016/j.bmc.2009.05.024
8629 10697 25 None -13 7 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human P2Y14 receptor expressed in human COS7 cellsAgonist activity at human P2Y14 receptor expressed in human COS7 cells
ChEMBL 566 9 9 16 -4.8 OC[C@H]1O[C@H](OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)[C@@H]([C@H]([C@@H]1O)O)O 10.1016/j.bmc.2009.05.024
CHEMBL375951 10697 25 None -13 7 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human P2Y14 receptor expressed in human COS7 cellsAgonist activity at human P2Y14 receptor expressed in human COS7 cells
ChEMBL 566 9 9 16 -4.8 OC[C@H]1O[C@H](OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)[C@@H]([C@H]([C@@H]1O)O)O 10.1016/j.bmc.2009.05.024
DB01861 10697 25 None -13 7 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human P2Y14 receptor expressed in human COS7 cellsAgonist activity at human P2Y14 receptor expressed in human COS7 cells
ChEMBL 566 9 9 16 -4.8 OC[C@H]1O[C@H](OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)[C@@H]([C@H]([C@@H]1O)O)O 10.1016/j.bmc.2009.05.024
25245106 21084 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production
ChEMBL 418 7 5 11 -2.0 COP(=O)(O)OP(=O)(O)OC[C@H]1O[C@@H](n2ccc(=O)[nH]c2=O)[C@H](O)[C@@H]1O 10.1021/jm901432g
CHEMBL1162554 21084 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production
ChEMBL 418 7 5 11 -2.0 COP(=O)(O)OP(=O)(O)OC[C@H]1O[C@@H](n2ccc(=O)[nH]c2=O)[C@H](O)[C@@H]1O 10.1021/jm901432g
CHEMBL1199939 21084 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production
ChEMBL 418 7 5 11 -2.0 COP(=O)(O)OP(=O)(O)OC[C@H]1O[C@@H](n2ccc(=O)[nH]c2=O)[C@H](O)[C@@H]1O 10.1021/jm901432g
16220889 143730 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human P2Y14 receptor expressed in human COS7 cellsAgonist activity at human P2Y14 receptor expressed in human COS7 cells
ChEMBL 582 9 9 16 -3.4 O=c1[nH]c(=S)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)O[C@H]2O[C@H](CO)[C@@H](O)[C@H](O)[C@H]2O)[C@@H](O)[C@H]1O 10.1016/j.bmc.2009.05.024
CHEMBL374384 143730 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human P2Y14 receptor expressed in human COS7 cellsAgonist activity at human P2Y14 receptor expressed in human COS7 cells
ChEMBL 582 9 9 16 -3.4 O=c1[nH]c(=S)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)O[C@H]2O[C@H](CO)[C@@H](O)[C@H](O)[C@H]2O)[C@@H](O)[C@H]1O 10.1016/j.bmc.2009.05.024
44627696 21045 0 None 64 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production
ChEMBL 476 7 5 11 0.6 CC(C)(C)OP(=O)(O)OP(=O)(O)OC[C@H]1O[C@@H](n2ccc(=O)[nH]c2=S)[C@H](O)[C@@H]1O 10.1021/jm901432g
CHEMBL1162556 21045 0 None 64 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production
ChEMBL 476 7 5 11 0.6 CC(C)(C)OP(=O)(O)OP(=O)(O)OC[C@H]1O[C@@H](n2ccc(=O)[nH]c2=S)[C@H](O)[C@@H]1O 10.1021/jm901432g
CHEMBL1199732 21045 0 None 64 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production
ChEMBL 476 7 5 11 0.6 CC(C)(C)OP(=O)(O)OP(=O)(O)OC[C@H]1O[C@@H](n2ccc(=O)[nH]c2=S)[C@H](O)[C@@H]1O 10.1021/jm901432g
22838429 148364 2 None 1 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production
ChEMBL 420 6 6 10 -1.2 O=c1[nH]c(=S)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm901432g
CHEMBL384992 148364 2 None 1 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production
ChEMBL 420 6 6 10 -1.2 O=c1[nH]c(=S)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]1O 10.1021/jm901432g
46226447 208186 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human P2Y14 receptor expressed in human COS7 cellsAgonist activity at human P2Y14 receptor expressed in human COS7 cells
ChEMBL 566 10 9 16 -4.8 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OC[C@H]3O[C@](O)(CO)[C@@H](O)[C@@H]3O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1016/j.bmc.2009.05.024
CHEMBL604676 208186 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human P2Y14 receptor expressed in human COS7 cellsAgonist activity at human P2Y14 receptor expressed in human COS7 cells
ChEMBL 566 10 9 16 -4.8 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OC[C@H]3O[C@](O)(CO)[C@@H](O)[C@@H]3O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1016/j.bmc.2009.05.024
45485253 205806 0 None -6 4 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production
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/jm901432g
CHEMBL1084020 205806 0 None -6 4 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production
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/jm901432g
CHEMBL1204010 205806 0 None -6 4 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production
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/jm901432g
CHEMBL4846821 205806 0 None -6 4 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production
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/jm901432g
CHEMBL585870 205806 0 None -6 4 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production
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/jm901432g
45485253 205806 0 None -6 4 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human recombinant P2Y14 receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y14 receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation proximity assay
ChEMBL 433 7 6 11 -2.5 CO/N=c1/ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm100287t
CHEMBL1084020 205806 0 None -6 4 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human recombinant P2Y14 receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y14 receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation proximity assay
ChEMBL 433 7 6 11 -2.5 CO/N=c1/ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm100287t
CHEMBL1204010 205806 0 None -6 4 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human recombinant P2Y14 receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y14 receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation proximity assay
ChEMBL 433 7 6 11 -2.5 CO/N=c1/ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm100287t
CHEMBL4846821 205806 0 None -6 4 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human recombinant P2Y14 receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y14 receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation proximity assay
ChEMBL 433 7 6 11 -2.5 CO/N=c1/ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm100287t
CHEMBL585870 205806 0 None -6 4 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human recombinant P2Y14 receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y14 receptor expressed in HEK293 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
1783 10697 25 None -13 7 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human P2Y14 expressed in COS7 cells assessed as stimulation of PLC-mediated [3H]inositol hydrolysisAgonist activity at human P2Y14 expressed in COS7 cells assessed as stimulation of PLC-mediated [3H]inositol hydrolysis
ChEMBL 566 9 9 16 -4.8 OC[C@H]1O[C@H](OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)[C@@H]([C@H]([C@@H]1O)O)O 10.1021/jm061222w
8629 10697 25 None -13 7 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human P2Y14 expressed in COS7 cells assessed as stimulation of PLC-mediated [3H]inositol hydrolysisAgonist activity at human P2Y14 expressed in COS7 cells assessed as stimulation of PLC-mediated [3H]inositol hydrolysis
ChEMBL 566 9 9 16 -4.8 OC[C@H]1O[C@H](OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)[C@@H]([C@H]([C@@H]1O)O)O 10.1021/jm061222w
CHEMBL375951 10697 25 None -13 7 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human P2Y14 expressed in COS7 cells assessed as stimulation of PLC-mediated [3H]inositol hydrolysisAgonist activity at human P2Y14 expressed in COS7 cells assessed as stimulation of PLC-mediated [3H]inositol hydrolysis
ChEMBL 566 9 9 16 -4.8 OC[C@H]1O[C@H](OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)[C@@H]([C@H]([C@@H]1O)O)O 10.1021/jm061222w
DB01861 10697 25 None -13 7 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human P2Y14 expressed in COS7 cells assessed as stimulation of PLC-mediated [3H]inositol hydrolysisAgonist activity at human P2Y14 expressed in COS7 cells assessed as stimulation of PLC-mediated [3H]inositol hydrolysis
ChEMBL 566 9 9 16 -4.8 OC[C@H]1O[C@H](OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)[C@@H]([C@H]([C@@H]1O)O)O 10.1021/jm061222w
16220889 143730 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human P2Y14 expressed in COS7 cells assessed as stimulation of PLC-mediated [3H]inositol hydrolysisAgonist activity at human P2Y14 expressed in COS7 cells assessed as stimulation of PLC-mediated [3H]inositol hydrolysis
ChEMBL 582 9 9 16 -3.4 O=c1[nH]c(=S)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)O[C@H]2O[C@H](CO)[C@@H](O)[C@H](O)[C@H]2O)[C@@H](O)[C@H]1O 10.1021/jm061222w
CHEMBL374384 143730 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human P2Y14 expressed in COS7 cells assessed as stimulation of PLC-mediated [3H]inositol hydrolysisAgonist activity at human P2Y14 expressed in COS7 cells assessed as stimulation of PLC-mediated [3H]inositol hydrolysis
ChEMBL 582 9 9 16 -3.4 O=c1[nH]c(=S)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)O[C@H]2O[C@H](CO)[C@@H](O)[C@H](O)[C@H]2O)[C@@H](O)[C@H]1O 10.1021/jm061222w
1783 10697 25 None -13 7 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human P2Y14 receptor expressed in COS7 cells assessed as stimulation of PLCAgonist activity at human P2Y14 receptor expressed in COS7 cells assessed as stimulation of PLC
ChEMBL 566 9 9 16 -4.8 OC[C@H]1O[C@H](OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)[C@@H]([C@H]([C@@H]1O)O)O 10.1016/j.bmcl.2006.10.081
8629 10697 25 None -13 7 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human P2Y14 receptor expressed in COS7 cells assessed as stimulation of PLCAgonist activity at human P2Y14 receptor expressed in COS7 cells assessed as stimulation of PLC
ChEMBL 566 9 9 16 -4.8 OC[C@H]1O[C@H](OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)[C@@H]([C@H]([C@@H]1O)O)O 10.1016/j.bmcl.2006.10.081
CHEMBL375951 10697 25 None -13 7 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human P2Y14 receptor expressed in COS7 cells assessed as stimulation of PLCAgonist activity at human P2Y14 receptor expressed in COS7 cells assessed as stimulation of PLC
ChEMBL 566 9 9 16 -4.8 OC[C@H]1O[C@H](OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)[C@@H]([C@H]([C@@H]1O)O)O 10.1016/j.bmcl.2006.10.081
DB01861 10697 25 None -13 7 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human P2Y14 receptor expressed in COS7 cells assessed as stimulation of PLCAgonist activity at human P2Y14 receptor expressed in COS7 cells assessed as stimulation of PLC
ChEMBL 566 9 9 16 -4.8 OC[C@H]1O[C@H](OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)[C@@H]([C@H]([C@@H]1O)O)O 10.1016/j.bmcl.2006.10.081
24858471 206584 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human P2Y14 receptor expressed in human COS7 cellsAgonist activity at human P2Y14 receptor expressed in human COS7 cells
ChEMBL 568 9 8 15 -3.8 O=c1ccn([C@@H]2O[C@H](COP(=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 10.1016/j.bmc.2009.05.024
CHEMBL594064 206584 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human P2Y14 receptor expressed in human COS7 cellsAgonist activity at human P2Y14 receptor expressed in human COS7 cells
ChEMBL 568 9 8 15 -3.8 O=c1ccn([C@@H]2O[C@H](COP(=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 10.1016/j.bmc.2009.05.024
17473 10698 18 None -2 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human P2Y14 expressed in COS7 cells assessed as stimulation of PLC-mediated [3H]inositol hydrolysisAgonist activity at human P2Y14 expressed in COS7 cells assessed as stimulation of PLC-mediated [3H]inositol hydrolysis
ChEMBL 580 9 9 16 -4.7 O[C@@H]1[C@@H](COP(=O)(OP(=O)(O[C@H]2O[C@H](C(=O)O)[C@H]([C@@H]([C@H]2O)O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm061222w
1784 10698 18 None -2 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human P2Y14 expressed in COS7 cells assessed as stimulation of PLC-mediated [3H]inositol hydrolysisAgonist activity at human P2Y14 expressed in COS7 cells assessed as stimulation of PLC-mediated [3H]inositol hydrolysis
ChEMBL 580 9 9 16 -4.7 O[C@@H]1[C@@H](COP(=O)(OP(=O)(O[C@H]2O[C@H](C(=O)O)[C@H]([C@@H]([C@H]2O)O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm061222w
CHEMBL228057 10698 18 None -2 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human P2Y14 expressed in COS7 cells assessed as stimulation of PLC-mediated [3H]inositol hydrolysisAgonist activity at human P2Y14 expressed in COS7 cells assessed as stimulation of PLC-mediated [3H]inositol hydrolysis
ChEMBL 580 9 9 16 -4.7 O[C@@H]1[C@@H](COP(=O)(OP(=O)(O[C@H]2O[C@H](C(=O)O)[C@H]([C@@H]([C@H]2O)O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm061222w
DB03041 10698 18 None -2 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human P2Y14 expressed in COS7 cells assessed as stimulation of PLC-mediated [3H]inositol hydrolysisAgonist activity at human P2Y14 expressed in COS7 cells assessed as stimulation of PLC-mediated [3H]inositol hydrolysis
ChEMBL 580 9 9 16 -4.7 O[C@@H]1[C@@H](COP(=O)(OP(=O)(O[C@H]2O[C@H](C(=O)O)[C@H]([C@@H]([C@H]2O)O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1021/jm061222w
44440209 17101 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human P2Y14 receptor expressed in COS7 cells assessed as stimulation of PLCAgonist activity at human P2Y14 receptor expressed in COS7 cells assessed as stimulation of PLC
ChEMBL 580 9 9 16 -4.7 O=C(O)[C@@H]1O[C@@H](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 10.1016/j.bmcl.2006.10.081
CHEMBL1162071 17101 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human P2Y14 receptor expressed in COS7 cells assessed as stimulation of PLCAgonist activity at human P2Y14 receptor expressed in COS7 cells assessed as stimulation of PLC
ChEMBL 580 9 9 16 -4.7 O=C(O)[C@@H]1O[C@@H](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 10.1016/j.bmcl.2006.10.081
17473 10698 18 None -2 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human P2Y14 receptor expressed in human COS7 cellsAgonist activity at human P2Y14 receptor expressed in human COS7 cells
ChEMBL 580 9 9 16 -4.7 O[C@@H]1[C@@H](COP(=O)(OP(=O)(O[C@H]2O[C@H](C(=O)O)[C@H]([C@@H]([C@H]2O)O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1016/j.bmc.2009.05.024
1784 10698 18 None -2 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human P2Y14 receptor expressed in human COS7 cellsAgonist activity at human P2Y14 receptor expressed in human COS7 cells
ChEMBL 580 9 9 16 -4.7 O[C@@H]1[C@@H](COP(=O)(OP(=O)(O[C@H]2O[C@H](C(=O)O)[C@H]([C@@H]([C@H]2O)O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1016/j.bmc.2009.05.024
CHEMBL228057 10698 18 None -2 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human P2Y14 receptor expressed in human COS7 cellsAgonist activity at human P2Y14 receptor expressed in human COS7 cells
ChEMBL 580 9 9 16 -4.7 O[C@@H]1[C@@H](COP(=O)(OP(=O)(O[C@H]2O[C@H](C(=O)O)[C@H]([C@@H]([C@H]2O)O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1016/j.bmc.2009.05.024
DB03041 10698 18 None -2 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human P2Y14 receptor expressed in human COS7 cellsAgonist activity at human P2Y14 receptor expressed in human COS7 cells
ChEMBL 580 9 9 16 -4.7 O[C@@H]1[C@@H](COP(=O)(OP(=O)(O[C@H]2O[C@H](C(=O)O)[C@H]([C@@H]([C@H]2O)O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1016/j.bmc.2009.05.024
46226454 206585 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human P2Y14 receptor expressed in human COS7 cellsAgonist activity at human P2Y14 receptor expressed in human COS7 cells
ChEMBL 566 9 9 16 -4.8 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OC[C@H]3O[C@H](O)[C@H](O)[C@@H](O)[C@@H]3O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1016/j.bmc.2009.05.024
CHEMBL594065 206585 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human P2Y14 receptor expressed in human COS7 cellsAgonist activity at human P2Y14 receptor expressed in human COS7 cells
ChEMBL 566 9 9 16 -4.8 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OC[C@H]3O[C@H](O)[C@H](O)[C@@H](O)[C@@H]3O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1016/j.bmc.2009.05.024
44627591 21058 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production
ChEMBL 448 8 5 11 -0.2 CCOP(=O)(O)OP(=O)(O)OC[C@H]1O[C@@H](n2ccc(=O)[nH]c2=S)[C@H](O)[C@@H]1O 10.1021/jm901432g
CHEMBL1162563 21058 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production
ChEMBL 448 8 5 11 -0.2 CCOP(=O)(O)OP(=O)(O)OC[C@H]1O[C@@H](n2ccc(=O)[nH]c2=S)[C@H](O)[C@@H]1O 10.1021/jm901432g
CHEMBL1199783 21058 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production
ChEMBL 448 8 5 11 -0.2 CCOP(=O)(O)OP(=O)(O)OC[C@H]1O[C@@H](n2ccc(=O)[nH]c2=S)[C@H](O)[C@@H]1O 10.1021/jm901432g
44627593 21039 0 None 229 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production
ChEMBL 462 9 5 11 0.2 CCCOP(=O)(O)OP(=O)(O)OC[C@H]1O[C@@H](n2ccc(=O)[nH]c2=S)[C@H](O)[C@@H]1O 10.1021/jm901432g
CHEMBL1162553 21039 0 None 229 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production
ChEMBL 462 9 5 11 0.2 CCCOP(=O)(O)OP(=O)(O)OC[C@H]1O[C@@H](n2ccc(=O)[nH]c2=S)[C@H](O)[C@@H]1O 10.1021/jm901432g
CHEMBL1199702 21039 0 None 229 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production
ChEMBL 462 9 5 11 0.2 CCCOP(=O)(O)OP(=O)(O)OC[C@H]1O[C@@H](n2ccc(=O)[nH]c2=S)[C@H](O)[C@@H]1O 10.1021/jm901432g
1783 10697 25 None -13 7 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production
ChEMBL 566 9 9 16 -4.8 OC[C@H]1O[C@H](OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)[C@@H]([C@H]([C@@H]1O)O)O 10.1021/jm901432g
8629 10697 25 None -13 7 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production
ChEMBL 566 9 9 16 -4.8 OC[C@H]1O[C@H](OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)[C@@H]([C@H]([C@@H]1O)O)O 10.1021/jm901432g
CHEMBL375951 10697 25 None -13 7 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production
ChEMBL 566 9 9 16 -4.8 OC[C@H]1O[C@H](OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)[C@@H]([C@H]([C@@H]1O)O)O 10.1021/jm901432g
DB01861 10697 25 None -13 7 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production
ChEMBL 566 9 9 16 -4.8 OC[C@H]1O[C@H](OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)[C@@H]([C@H]([C@@H]1O)O)O 10.1021/jm901432g
44422899 148784 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human P2Y14 expressed in COS7 cells assessed as stimulation of PLC-mediated [3H]inositol hydrolysisAgonist activity at human P2Y14 expressed in COS7 cells assessed as stimulation of PLC-mediated [3H]inositol hydrolysis
ChEMBL 596 9 9 16 -3.3 O=C(O)[C@H]1O[C@H](OP(=O)(O)OP(=O)(O)OC[C@H]2O[C@@H](n3ccc(=O)[nH]c3=S)[C@H](O)[C@@H]2O)[C@H](O)[C@@H](O)[C@@H]1O 10.1021/jm061222w
CHEMBL387520 148784 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human P2Y14 expressed in COS7 cells assessed as stimulation of PLC-mediated [3H]inositol hydrolysisAgonist activity at human P2Y14 expressed in COS7 cells assessed as stimulation of PLC-mediated [3H]inositol hydrolysis
ChEMBL 596 9 9 16 -3.3 O=C(O)[C@H]1O[C@H](OP(=O)(O)OP(=O)(O)OC[C@H]2O[C@@H](n3ccc(=O)[nH]c3=S)[C@H](O)[C@@H]2O)[C@H](O)[C@@H](O)[C@@H]1O 10.1021/jm061222w
44440213 17102 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human P2Y14 expressed in COS7 cells assessed as stimulation of PLC-mediated [3H]inositol hydrolysisAgonist activity at human P2Y14 expressed in COS7 cells assessed as stimulation of PLC-mediated [3H]inositol hydrolysis
ChEMBL 607 10 9 16 -4.7 CC(=O)N[C@@H]1[C@H](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/jm061222w
CHEMBL1162072 17102 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human P2Y14 expressed in COS7 cells assessed as stimulation of PLC-mediated [3H]inositol hydrolysisAgonist activity at human P2Y14 expressed in COS7 cells assessed as stimulation of PLC-mediated [3H]inositol hydrolysis
ChEMBL 607 10 9 16 -4.7 CC(=O)N[C@@H]1[C@H](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/jm061222w
44440213 17102 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human P2Y14 receptor expressed in COS7 cells assessed as stimulation of PLCAgonist activity at human P2Y14 receptor expressed in COS7 cells assessed as stimulation of PLC
ChEMBL 607 10 9 16 -4.7 CC(=O)N[C@@H]1[C@H](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 10.1016/j.bmcl.2006.10.081
CHEMBL1162072 17102 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human P2Y14 receptor expressed in COS7 cells assessed as stimulation of PLCAgonist activity at human P2Y14 receptor expressed in COS7 cells assessed as stimulation of PLC
ChEMBL 607 10 9 16 -4.7 CC(=O)N[C@@H]1[C@H](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 10.1016/j.bmcl.2006.10.081
44440213 17102 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human P2Y14 receptor expressed in human COS7 cellsAgonist activity at human P2Y14 receptor expressed in human COS7 cells
ChEMBL 607 10 9 16 -4.7 CC(=O)N[C@@H]1[C@H](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 10.1016/j.bmc.2009.05.024
CHEMBL1162072 17102 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human P2Y14 receptor expressed in human COS7 cellsAgonist activity at human P2Y14 receptor expressed in human COS7 cells
ChEMBL 607 10 9 16 -4.7 CC(=O)N[C@@H]1[C@H](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 10.1016/j.bmc.2009.05.024
44627486 20953 0 None 1 2 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production
ChEMBL 402 6 5 10 -1.9 CP(=O)(O)OP(=O)(O)OC[C@H]1O[C@@H](n2ccc(=O)[nH]c2=O)[C@H](O)[C@@H]1O 10.1021/jm901432g
CHEMBL1198715 20953 0 None 1 2 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production
ChEMBL 402 6 5 10 -1.9 CP(=O)(O)OP(=O)(O)OC[C@H]1O[C@@H](n2ccc(=O)[nH]c2=O)[C@H](O)[C@@H]1O 10.1021/jm901432g
CHEMBL612063 20953 0 None 1 2 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production
ChEMBL 402 6 5 10 -1.9 CP(=O)(O)OP(=O)(O)OC[C@H]1O[C@@H](n2ccc(=O)[nH]c2=O)[C@H](O)[C@@H]1O 10.1021/jm901432g
46226477 206555 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human P2Y14 receptor expressed in human COS7 cellsAgonist activity at human P2Y14 receptor expressed in human COS7 cells
ChEMBL 536 9 8 15 -4.2 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OC[C@H]3O[C@H](O)[C@@H](O)[C@@H]3O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1016/j.bmc.2009.05.024
CHEMBL593842 206555 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human P2Y14 receptor expressed in human COS7 cellsAgonist activity at human P2Y14 receptor expressed in human COS7 cells
ChEMBL 536 9 8 15 -4.2 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OC[C@H]3O[C@H](O)[C@@H](O)[C@@H]3O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1016/j.bmc.2009.05.024
44627597 20954 0 None 3 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production
ChEMBL 456 9 5 11 -1.6 C#CCCOP(=O)(O)OP(=O)(O)OC[C@H]1O[C@@H](n2ccc(=O)[nH]c2=O)[C@H](O)[C@@H]1O 10.1021/jm901432g
CHEMBL1198716 20954 0 None 3 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production
ChEMBL 456 9 5 11 -1.6 C#CCCOP(=O)(O)OP(=O)(O)OC[C@H]1O[C@@H](n2ccc(=O)[nH]c2=O)[C@H](O)[C@@H]1O 10.1021/jm901432g
CHEMBL612064 20954 0 None 3 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production
ChEMBL 456 9 5 11 -1.6 C#CCCOP(=O)(O)OP(=O)(O)OC[C@H]1O[C@@H](n2ccc(=O)[nH]c2=O)[C@H](O)[C@@H]1O 10.1021/jm901432g
44422870 92352 4 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human P2Y14 expressed in COS7 cells assessed as stimulation of PLC-mediated [3H]inositol hydrolysisAgonist activity at human P2Y14 expressed in COS7 cells assessed as stimulation of PLC-mediated [3H]inositol hydrolysis
ChEMBL 582 9 9 16 -3.4 O=c1ccn([C@@H]2O[C@H](COP(=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(=S)[nH]1 10.1021/jm061222w
CHEMBL228111 92352 4 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human P2Y14 expressed in COS7 cells assessed as stimulation of PLC-mediated [3H]inositol hydrolysisAgonist activity at human P2Y14 expressed in COS7 cells assessed as stimulation of PLC-mediated [3H]inositol hydrolysis
ChEMBL 582 9 9 16 -3.4 O=c1ccn([C@@H]2O[C@H](COP(=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(=S)[nH]1 10.1021/jm061222w
44422870 92352 4 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human P2Y14 receptor expressed in human COS7 cellsAgonist activity at human P2Y14 receptor expressed in human COS7 cells
ChEMBL 582 9 9 16 -3.4 O=c1ccn([C@@H]2O[C@H](COP(=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(=S)[nH]1 10.1016/j.bmc.2009.05.024
CHEMBL228111 92352 4 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human P2Y14 receptor expressed in human COS7 cellsAgonist activity at human P2Y14 receptor expressed in human COS7 cells
ChEMBL 582 9 9 16 -3.4 O=c1ccn([C@@H]2O[C@H](COP(=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(=S)[nH]1 10.1016/j.bmc.2009.05.024
46226446 206744 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human P2Y14 receptor expressed in human COS7 cellsAgonist activity at human P2Y14 receptor expressed in human COS7 cells
ChEMBL 664 12 10 17 -5.5 CC(=O)NCCNC(=O)[C@H]1O[C@H](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 10.1016/j.bmc.2009.05.024
CHEMBL595076 206744 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human P2Y14 receptor expressed in human COS7 cellsAgonist activity at human P2Y14 receptor expressed in human COS7 cells
ChEMBL 664 12 10 17 -5.5 CC(=O)NCCNC(=O)[C@H]1O[C@H](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 10.1016/j.bmc.2009.05.024
44627698 21046 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production
ChEMBL 486 8 5 11 -0.3 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OC3CCCCC3)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm901432g
CHEMBL1162558 21046 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production
ChEMBL 486 8 5 11 -0.3 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OC3CCCCC3)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm901432g
CHEMBL1199733 21046 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production
ChEMBL 486 8 5 11 -0.3 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OC3CCCCC3)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm901432g
44627491 21097 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production
ChEMBL 434 7 5 11 -0.6 COP(=O)(O)OP(=O)(O)OC[C@H]1O[C@@H](n2ccc(=O)[nH]c2=S)[C@H](O)[C@@H]1O 10.1021/jm901432g
CHEMBL1162557 21097 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production
ChEMBL 434 7 5 11 -0.6 COP(=O)(O)OP(=O)(O)OC[C@H]1O[C@@H](n2ccc(=O)[nH]c2=S)[C@H](O)[C@@H]1O 10.1021/jm901432g
CHEMBL1200008 21097 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production
ChEMBL 434 7 5 11 -0.6 COP(=O)(O)OP(=O)(O)OC[C@H]1O[C@@H](n2ccc(=O)[nH]c2=S)[C@H](O)[C@@H]1O 10.1021/jm901432g
11146048 206867 1 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human P2Y14 receptor expressed in human COS7 cellsAgonist activity at human P2Y14 receptor expressed in human COS7 cells
ChEMBL 550 8 8 15 -3.8 C[C@H]1O[C@H](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 10.1016/j.bmc.2009.05.024
CHEMBL595940 206867 1 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human P2Y14 receptor expressed in human COS7 cellsAgonist activity at human P2Y14 receptor expressed in human COS7 cells
ChEMBL 550 8 8 15 -3.8 C[C@H]1O[C@H](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 10.1016/j.bmc.2009.05.024
448872 206462 4 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human P2Y14 receptor expressed in human COS7 cellsAgonist activity at human P2Y14 receptor expressed in human COS7 cells
ChEMBL 568 9 8 15 -3.8 O=c1ccn([C@@H]2O[C@H](COP(=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 10.1016/j.bmc.2009.05.024
CHEMBL593125 206462 4 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human P2Y14 receptor expressed in human COS7 cellsAgonist activity at human P2Y14 receptor expressed in human COS7 cells
ChEMBL 568 9 8 15 -3.8 O=c1ccn([C@@H]2O[C@H](COP(=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 10.1016/j.bmc.2009.05.024
46226441 206768 2 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human P2Y14 receptor expressed in human COS7 cellsAgonist activity at human P2Y14 receptor expressed in human COS7 cells
ChEMBL 566 9 9 16 -4.8 O=c1ccn([C@@H]2O[C@H](COP(=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.2009.05.024
CHEMBL595216 206768 2 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human P2Y14 receptor expressed in human COS7 cellsAgonist activity at human P2Y14 receptor expressed in human COS7 cells
ChEMBL 566 9 9 16 -4.8 O=c1ccn([C@@H]2O[C@H](COP(=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.2009.05.024
44585948 193430 2 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production
ChEMBL 438 6 6 9 -1.9 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)C(F)(F)P(=O)(O)O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm901432g
CHEMBL488133 193430 2 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production
ChEMBL 438 6 6 9 -1.9 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)C(F)(F)P(=O)(O)O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm901432g
46226456 206898 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human P2Y14 receptor expressed in human COS7 cellsAgonist activity at human P2Y14 receptor expressed in human COS7 cells
ChEMBL 566 9 9 16 -4.8 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OC[C@H]3O[C@H](O)[C@@H](O)[C@@H](O)[C@@H]3O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1016/j.bmc.2009.05.024
CHEMBL596145 206898 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human P2Y14 receptor expressed in human COS7 cellsAgonist activity at human P2Y14 receptor expressed in human COS7 cells
ChEMBL 566 9 9 16 -4.8 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OC[C@H]3O[C@H](O)[C@@H](O)[C@@H](O)[C@@H]3O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1016/j.bmc.2009.05.024
1782 10696 16 None -10 5 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human P2Y14 expressed in COS7 cells assessed as stimulation of PLC-mediated [3H]inositol hydrolysisAgonist activity at human P2Y14 expressed in COS7 cells assessed as stimulation of PLC-mediated [3H]inositol hydrolysis
ChEMBL 566 9 9 16 -4.8 OC[C@H]1O[C@H](OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)[C@@H]([C@H]([C@H]1O)O)O 10.1021/jm061222w
18068 10696 16 None -10 5 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human P2Y14 expressed in COS7 cells assessed as stimulation of PLC-mediated [3H]inositol hydrolysisAgonist activity at human P2Y14 expressed in COS7 cells assessed as stimulation of PLC-mediated [3H]inositol hydrolysis
ChEMBL 566 9 9 16 -4.8 OC[C@H]1O[C@H](OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)[C@@H]([C@H]([C@H]1O)O)O 10.1021/jm061222w
CHEMBL439009 10696 16 None -10 5 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human P2Y14 expressed in COS7 cells assessed as stimulation of PLC-mediated [3H]inositol hydrolysisAgonist activity at human P2Y14 expressed in COS7 cells assessed as stimulation of PLC-mediated [3H]inositol hydrolysis
ChEMBL 566 9 9 16 -4.8 OC[C@H]1O[C@H](OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)[C@@H]([C@H]([C@H]1O)O)O 10.1021/jm061222w
DB03501 10696 16 None -10 5 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human P2Y14 expressed in COS7 cells assessed as stimulation of PLC-mediated [3H]inositol hydrolysisAgonist activity at human P2Y14 expressed in COS7 cells assessed as stimulation of PLC-mediated [3H]inositol hydrolysis
ChEMBL 566 9 9 16 -4.8 OC[C@H]1O[C@H](OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)[C@@H]([C@H]([C@H]1O)O)O 10.1021/jm061222w
1782 10696 16 None -10 5 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human P2Y14 receptor expressed in human COS7 cellsAgonist activity at human P2Y14 receptor expressed in human COS7 cells
ChEMBL 566 9 9 16 -4.8 OC[C@H]1O[C@H](OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)[C@@H]([C@H]([C@H]1O)O)O 10.1016/j.bmc.2009.05.024
18068 10696 16 None -10 5 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human P2Y14 receptor expressed in human COS7 cellsAgonist activity at human P2Y14 receptor expressed in human COS7 cells
ChEMBL 566 9 9 16 -4.8 OC[C@H]1O[C@H](OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)[C@@H]([C@H]([C@H]1O)O)O 10.1016/j.bmc.2009.05.024
CHEMBL439009 10696 16 None -10 5 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human P2Y14 receptor expressed in human COS7 cellsAgonist activity at human P2Y14 receptor expressed in human COS7 cells
ChEMBL 566 9 9 16 -4.8 OC[C@H]1O[C@H](OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)[C@@H]([C@H]([C@H]1O)O)O 10.1016/j.bmc.2009.05.024
DB03501 10696 16 None -10 5 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human P2Y14 receptor expressed in human COS7 cellsAgonist activity at human P2Y14 receptor expressed in human COS7 cells
ChEMBL 566 9 9 16 -4.8 OC[C@H]1O[C@H](OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)[C@@H]([C@H]([C@H]1O)O)O 10.1016/j.bmc.2009.05.024
54584734 67081 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human P2Y14 receptor expressed in COS7 cells assessed as stimulation of PLCAgonist activity at human P2Y14 receptor expressed in COS7 cells assessed as stimulation of PLC
ChEMBL 566 9 10 15 -4.7 O=c1cc([C@@H]2O[C@H](COP(=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)[nH]c(=O)[nH]1 10.1016/j.bmcl.2006.10.081
CHEMBL1743884 67081 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human P2Y14 receptor expressed in COS7 cells assessed as stimulation of PLCAgonist activity at human P2Y14 receptor expressed in COS7 cells assessed as stimulation of PLC
ChEMBL 566 9 10 15 -4.7 O=c1cc([C@@H]2O[C@H](COP(=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)[nH]c(=O)[nH]1 10.1016/j.bmcl.2006.10.081
44627595 21040 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production
ChEMBL 457 9 5 12 -1.7 N#CCCOP(=O)(O)OP(=O)(O)OC[C@H]1O[C@@H](n2ccc(=O)[nH]c2=O)[C@H](O)[C@@H]1O 10.1021/jm901432g
CHEMBL1162555 21040 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production
ChEMBL 457 9 5 12 -1.7 N#CCCOP(=O)(O)OP(=O)(O)OC[C@H]1O[C@@H](n2ccc(=O)[nH]c2=O)[C@H](O)[C@@H]1O 10.1021/jm901432g
CHEMBL1199703 21040 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production
ChEMBL 457 9 5 12 -1.7 N#CCCOP(=O)(O)OP(=O)(O)OC[C@H]1O[C@@H](n2ccc(=O)[nH]c2=O)[C@H](O)[C@@H]1O 10.1021/jm901432g
449409 21047 2 None 9 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production
ChEMBL 480 8 5 11 -0.5 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)Oc3ccccc3)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm901432g
CHEMBL1162559 21047 2 None 9 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production
ChEMBL 480 8 5 11 -0.5 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)Oc3ccccc3)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm901432g
CHEMBL1199734 21047 2 None 9 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production
ChEMBL 480 8 5 11 -0.5 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)Oc3ccccc3)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm901432g
44440213 17102 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human P2Y14 expressed in COS7 cells assessed as stimulation of PLC-mediated [3H]inositol hydrolysisAgonist activity at human P2Y14 expressed in COS7 cells assessed as stimulation of PLC-mediated [3H]inositol hydrolysis
ChEMBL 607 10 9 16 -4.7 CC(=O)N[C@@H]1[C@H](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/jm061222w
CHEMBL1162072 17102 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human P2Y14 expressed in COS7 cells assessed as stimulation of PLC-mediated [3H]inositol hydrolysisAgonist activity at human P2Y14 expressed in COS7 cells assessed as stimulation of PLC-mediated [3H]inositol hydrolysis
ChEMBL 607 10 9 16 -4.7 CC(=O)N[C@@H]1[C@H](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/jm061222w
44440213 17102 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human P2Y14 receptor expressed in human COS7 cellsAgonist activity at human P2Y14 receptor expressed in human COS7 cells
ChEMBL 607 10 9 16 -4.7 CC(=O)N[C@@H]1[C@H](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 10.1016/j.bmc.2009.05.024
CHEMBL1162072 17102 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human P2Y14 receptor expressed in human COS7 cellsAgonist activity at human P2Y14 receptor expressed in human COS7 cells
ChEMBL 607 10 9 16 -4.7 CC(=O)N[C@@H]1[C@H](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 10.1016/j.bmc.2009.05.024
16220801 92239 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human P2Y14 expressed in COS7 cells assessed as stimulation of PLC-mediated [3H]inositol hydrolysisAgonist activity at human P2Y14 expressed in COS7 cells assessed as stimulation of PLC-mediated [3H]inositol hydrolysis
ChEMBL 566 10 9 16 -4.8 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OC[C@@]3(O)O[C@H](CO)[C@@H](O)[C@@H]3O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm061222w
CHEMBL226713 92239 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human P2Y14 expressed in COS7 cells assessed as stimulation of PLC-mediated [3H]inositol hydrolysisAgonist activity at human P2Y14 expressed in COS7 cells assessed as stimulation of PLC-mediated [3H]inositol hydrolysis
ChEMBL 566 10 9 16 -4.8 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OC[C@@]3(O)O[C@H](CO)[C@@H](O)[C@@H]3O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1021/jm061222w
16220801 92239 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human P2Y14 receptor expressed in human COS7 cellsAgonist activity at human P2Y14 receptor expressed in human COS7 cells
ChEMBL 566 10 9 16 -4.8 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OC[C@@]3(O)O[C@H](CO)[C@@H](O)[C@@H]3O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1016/j.bmc.2009.05.024
CHEMBL226713 92239 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human P2Y14 receptor expressed in human COS7 cellsAgonist activity at human P2Y14 receptor expressed in human COS7 cells
ChEMBL 566 10 9 16 -4.8 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OC[C@@]3(O)O[C@H](CO)[C@@H](O)[C@@H]3O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1016/j.bmc.2009.05.024
46226455 206463 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human P2Y14 receptor expressed in human COS7 cellsAgonist activity at human P2Y14 receptor expressed in human COS7 cells
ChEMBL 568 9 8 15 -3.8 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)O[C@H]3O[C@H](CF)[C@@H](O)[C@H](O)[C@H]3O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1016/j.bmc.2009.05.024
CHEMBL593126 206463 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human P2Y14 receptor expressed in human COS7 cellsAgonist activity at human P2Y14 receptor expressed in human COS7 cells
ChEMBL 568 9 8 15 -3.8 O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)O[C@H]3O[C@H](CF)[C@@H](O)[C@H](O)[C@H]3O)[C@@H](O)[C@H]2O)c(=O)[nH]1 10.1016/j.bmc.2009.05.024
448873 92311 2 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human P2Y14 expressed in COS7 cells assessed as stimulation of PLC-mediated [3H]inositol hydrolysisAgonist activity at human P2Y14 expressed in COS7 cells assessed as stimulation of PLC-mediated [3H]inositol hydrolysis
ChEMBL 566 9 9 16 -4.8 O=c1ccn([C@@H]2O[C@H](COP(=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/jm061222w
CHEMBL227711 92311 2 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human P2Y14 expressed in COS7 cells assessed as stimulation of PLC-mediated [3H]inositol hydrolysisAgonist activity at human P2Y14 expressed in COS7 cells assessed as stimulation of PLC-mediated [3H]inositol hydrolysis
ChEMBL 566 9 9 16 -4.8 O=c1ccn([C@@H]2O[C@H](COP(=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/jm061222w
448873 92311 2 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human P2Y14 receptor expressed in human COS7 cellsAgonist activity at human P2Y14 receptor expressed in human COS7 cells
ChEMBL 566 9 9 16 -4.8 O=c1ccn([C@@H]2O[C@H](COP(=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.2009.05.024
CHEMBL227711 92311 2 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human P2Y14 receptor expressed in human COS7 cellsAgonist activity at human P2Y14 receptor expressed in human COS7 cells
ChEMBL 566 9 9 16 -4.8 O=c1ccn([C@@H]2O[C@H](COP(=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.2009.05.024
46226463 206680 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human P2Y14 receptor expressed in human COS7 cellsAgonist activity at human P2Y14 receptor expressed in human COS7 cells
ChEMBL 722 12 10 18 -4.1 CC(C)(C)OC(=O)NCCNC(=O)[C@H]1O[C@H](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 10.1016/j.bmc.2009.05.024
CHEMBL594703 206680 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human P2Y14 receptor expressed in human COS7 cellsAgonist activity at human P2Y14 receptor expressed in human COS7 cells
ChEMBL 722 12 10 18 -4.1 CC(C)(C)OC(=O)NCCNC(=O)[C@H]1O[C@H](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 10.1016/j.bmc.2009.05.024
42611190 9930 12 None 5 2 Human 9.4 pIC50 = 9.4 Functional
Antagonist activity at P2Y14R (unknown origin) expressed in rat C6 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 15 mins in presence of IBMX by chromatographyAntagonist activity at P2Y14R (unknown origin) expressed in rat C6 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 15 mins in presence of IBMX by chromatography
ChEMBL 475 4 2 2 7.4 OC(=O)c1cc2cc(ccc2c(c1)c1ccc(cc1)C1CCNCC1)c1ccc(cc1)C(F)(F)F 10.1021/acs.jmedchem.2c01632
5802 9930 12 None 5 2 Human 9.4 pIC50 = 9.4 Functional
Antagonist activity at P2Y14R (unknown origin) expressed in rat C6 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 15 mins in presence of IBMX by chromatographyAntagonist activity at P2Y14R (unknown origin) expressed in rat C6 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 15 mins in presence of IBMX by chromatography
ChEMBL 475 4 2 2 7.4 OC(=O)c1cc2cc(ccc2c(c1)c1ccc(cc1)C1CCNCC1)c1ccc(cc1)C(F)(F)F 10.1021/acs.jmedchem.2c01632
CHEMBL1800685 9930 12 None 5 2 Human 9.4 pIC50 = 9.4 Functional
Antagonist activity at P2Y14R (unknown origin) expressed in rat C6 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 15 mins in presence of IBMX by chromatographyAntagonist activity at P2Y14R (unknown origin) expressed in rat C6 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 15 mins in presence of IBMX by chromatography
ChEMBL 475 4 2 2 7.4 OC(=O)c1cc2cc(ccc2c(c1)c1ccc(cc1)C1CCNCC1)c1ccc(cc1)C(F)(F)F 10.1021/acs.jmedchem.2c01632
42611190 9930 12 None 5 2 Human 9.4 pIC50 = 9.4 Functional
Antagonist activity human P2Y14R expressed in African green monkey COS7 cells assessed as inhibition of UDPG-induced [3H]inositol phosphate accumulation after 30 mins by liquid scintillation counting methodAntagonist activity human P2Y14R expressed in African green monkey COS7 cells assessed as inhibition of UDPG-induced [3H]inositol phosphate accumulation after 30 mins by liquid scintillation counting method
ChEMBL 475 4 2 2 7.4 OC(=O)c1cc2cc(ccc2c(c1)c1ccc(cc1)C1CCNCC1)c1ccc(cc1)C(F)(F)F 10.1021/acs.jmedchem.6b00044
5802 9930 12 None 5 2 Human 9.4 pIC50 = 9.4 Functional
Antagonist activity human P2Y14R expressed in African green monkey COS7 cells assessed as inhibition of UDPG-induced [3H]inositol phosphate accumulation after 30 mins by liquid scintillation counting methodAntagonist activity human P2Y14R expressed in African green monkey COS7 cells assessed as inhibition of UDPG-induced [3H]inositol phosphate accumulation after 30 mins by liquid scintillation counting method
ChEMBL 475 4 2 2 7.4 OC(=O)c1cc2cc(ccc2c(c1)c1ccc(cc1)C1CCNCC1)c1ccc(cc1)C(F)(F)F 10.1021/acs.jmedchem.6b00044
CHEMBL1800685 9930 12 None 5 2 Human 9.4 pIC50 = 9.4 Functional
Antagonist activity human P2Y14R expressed in African green monkey COS7 cells assessed as inhibition of UDPG-induced [3H]inositol phosphate accumulation after 30 mins by liquid scintillation counting methodAntagonist activity human P2Y14R expressed in African green monkey COS7 cells assessed as inhibition of UDPG-induced [3H]inositol phosphate accumulation after 30 mins by liquid scintillation counting method
ChEMBL 475 4 2 2 7.4 OC(=O)c1cc2cc(ccc2c(c1)c1ccc(cc1)C1CCNCC1)c1ccc(cc1)C(F)(F)F 10.1021/acs.jmedchem.6b00044
54584537 68458 0 None - 1 Mouse 9.0 pIC50 = 9 Functional
Antagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assayAntagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assay
ChEMBL 475 4 1 6 4.9 CCc1cccc(NC(=O)N2CCc3nc(-c4cnc(C#N)nc4)nc(-c4ccccc4C)c3C2)c1 10.1016/j.bmcl.2011.03.084
CHEMBL1771459 68458 0 None - 1 Mouse 9.0 pIC50 = 9 Functional
Antagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assayAntagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assay
ChEMBL 475 4 1 6 4.9 CCc1cccc(NC(=O)N2CCc3nc(-c4cnc(C#N)nc4)nc(-c4ccccc4C)c3C2)c1 10.1016/j.bmcl.2011.03.084
155512121 176404 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at P2Y14 (unknown origin) expressed in HEK293 cells assessed as reduction in cAMP production incubated for 30 mins by ADP-glo assayAntagonist activity at P2Y14 (unknown origin) expressed in HEK293 cells assessed as reduction in cAMP production incubated for 30 mins by ADP-glo assay
ChEMBL 414 5 3 3 5.1 Cc1ccc(C(=O)Nc2cc(C(=O)O)cc(-c3ccc(C4CCNCC4)cc3)c2)cc1 10.1016/j.ejmech.2021.113313
CHEMBL4436879 176404 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at P2Y14 (unknown origin) expressed in HEK293 cells assessed as reduction in cAMP production incubated for 30 mins by ADP-glo assayAntagonist activity at P2Y14 (unknown origin) expressed in HEK293 cells assessed as reduction in cAMP production incubated for 30 mins by ADP-glo assay
ChEMBL 414 5 3 3 5.1 Cc1ccc(C(=O)Nc2cc(C(=O)O)cc(-c3ccc(C4CCNCC4)cc3)c2)cc1 10.1016/j.ejmech.2021.113313
155512121 176404 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human P2Y14R stably expressed in human forskolin treated THP1 cells assessed as reduction in P2Y14R agonist UDPG-induced inhibition of cAMP production incubated for 15 mins by competitive enzyme-linked immunoassayAntagonist activity at human P2Y14R stably expressed in human forskolin treated THP1 cells assessed as reduction in P2Y14R agonist UDPG-induced inhibition of cAMP production incubated for 15 mins by competitive enzyme-linked immunoassay
ChEMBL 414 5 3 3 5.1 Cc1ccc(C(=O)Nc2cc(C(=O)O)cc(-c3ccc(C4CCNCC4)cc3)c2)cc1 10.1016/j.ejmech.2019.111564
CHEMBL4436879 176404 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human P2Y14R stably expressed in human forskolin treated THP1 cells assessed as reduction in P2Y14R agonist UDPG-induced inhibition of cAMP production incubated for 15 mins by competitive enzyme-linked immunoassayAntagonist activity at human P2Y14R stably expressed in human forskolin treated THP1 cells assessed as reduction in P2Y14R agonist UDPG-induced inhibition of cAMP production incubated for 15 mins by competitive enzyme-linked immunoassay
ChEMBL 414 5 3 3 5.1 Cc1ccc(C(=O)Nc2cc(C(=O)O)cc(-c3ccc(C4CCNCC4)cc3)c2)cc1 10.1016/j.ejmech.2019.111564
154636989 199200 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assayAntagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assay
ChEMBL 353 5 2 4 3.3 Cc1ccc(C(=O)Nc2cc(C(=O)O)nn2Cc2ccc(F)cc2)cc1 10.1021/acs.jmedchem.2c01632
CHEMBL5208130 199200 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assayAntagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assay
ChEMBL 353 5 2 4 3.3 Cc1ccc(C(=O)Nc2cc(C(=O)O)nn2Cc2ccc(F)cc2)cc1 10.1021/acs.jmedchem.2c01632
42611190 9930 12 None 5 2 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at P2Y14 (unknown origin) expressed in HEK293 cells assessed as reduction in cAMP production incubated for 30 mins by ADP-glo assayAntagonist activity at P2Y14 (unknown origin) expressed in HEK293 cells assessed as reduction in cAMP production incubated for 30 mins by ADP-glo assay
ChEMBL 475 4 2 2 7.4 OC(=O)c1cc2cc(ccc2c(c1)c1ccc(cc1)C1CCNCC1)c1ccc(cc1)C(F)(F)F 10.1016/j.ejmech.2021.113313
5802 9930 12 None 5 2 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at P2Y14 (unknown origin) expressed in HEK293 cells assessed as reduction in cAMP production incubated for 30 mins by ADP-glo assayAntagonist activity at P2Y14 (unknown origin) expressed in HEK293 cells assessed as reduction in cAMP production incubated for 30 mins by ADP-glo assay
ChEMBL 475 4 2 2 7.4 OC(=O)c1cc2cc(ccc2c(c1)c1ccc(cc1)C1CCNCC1)c1ccc(cc1)C(F)(F)F 10.1016/j.ejmech.2021.113313
CHEMBL1800685 9930 12 None 5 2 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at P2Y14 (unknown origin) expressed in HEK293 cells assessed as reduction in cAMP production incubated for 30 mins by ADP-glo assayAntagonist activity at P2Y14 (unknown origin) expressed in HEK293 cells assessed as reduction in cAMP production incubated for 30 mins by ADP-glo assay
ChEMBL 475 4 2 2 7.4 OC(=O)c1cc2cc(ccc2c(c1)c1ccc(cc1)C1CCNCC1)c1ccc(cc1)C(F)(F)F 10.1016/j.ejmech.2021.113313
42611190 9930 12 None 5 2 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assayAntagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assay
ChEMBL 475 4 2 2 7.4 OC(=O)c1cc2cc(ccc2c(c1)c1ccc(cc1)C1CCNCC1)c1ccc(cc1)C(F)(F)F 10.1021/acs.jmedchem.2c01632
5802 9930 12 None 5 2 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assayAntagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assay
ChEMBL 475 4 2 2 7.4 OC(=O)c1cc2cc(ccc2c(c1)c1ccc(cc1)C1CCNCC1)c1ccc(cc1)C(F)(F)F 10.1021/acs.jmedchem.2c01632
CHEMBL1800685 9930 12 None 5 2 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assayAntagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assay
ChEMBL 475 4 2 2 7.4 OC(=O)c1cc2cc(ccc2c(c1)c1ccc(cc1)C1CCNCC1)c1ccc(cc1)C(F)(F)F 10.1021/acs.jmedchem.2c01632
42611190 9930 12 None 5 2 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human P2Y14R stably expressed in human forskolin treated THP1 cells assessed as reduction in P2Y14R agonist UDPG-induced inhibition of cAMP production incubated for 15 mins by competitive enzyme-linked immunoassayAntagonist activity at human P2Y14R stably expressed in human forskolin treated THP1 cells assessed as reduction in P2Y14R agonist UDPG-induced inhibition of cAMP production incubated for 15 mins by competitive enzyme-linked immunoassay
ChEMBL 475 4 2 2 7.4 OC(=O)c1cc2cc(ccc2c(c1)c1ccc(cc1)C1CCNCC1)c1ccc(cc1)C(F)(F)F 10.1016/j.ejmech.2019.111564
5802 9930 12 None 5 2 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human P2Y14R stably expressed in human forskolin treated THP1 cells assessed as reduction in P2Y14R agonist UDPG-induced inhibition of cAMP production incubated for 15 mins by competitive enzyme-linked immunoassayAntagonist activity at human P2Y14R stably expressed in human forskolin treated THP1 cells assessed as reduction in P2Y14R agonist UDPG-induced inhibition of cAMP production incubated for 15 mins by competitive enzyme-linked immunoassay
ChEMBL 475 4 2 2 7.4 OC(=O)c1cc2cc(ccc2c(c1)c1ccc(cc1)C1CCNCC1)c1ccc(cc1)C(F)(F)F 10.1016/j.ejmech.2019.111564
CHEMBL1800685 9930 12 None 5 2 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human P2Y14R stably expressed in human forskolin treated THP1 cells assessed as reduction in P2Y14R agonist UDPG-induced inhibition of cAMP production incubated for 15 mins by competitive enzyme-linked immunoassayAntagonist activity at human P2Y14R stably expressed in human forskolin treated THP1 cells assessed as reduction in P2Y14R agonist UDPG-induced inhibition of cAMP production incubated for 15 mins by competitive enzyme-linked immunoassay
ChEMBL 475 4 2 2 7.4 OC(=O)c1cc2cc(ccc2c(c1)c1ccc(cc1)C1CCNCC1)c1ccc(cc1)C(F)(F)F 10.1016/j.ejmech.2019.111564
53234015 68455 0 None - 1 Mouse 8.0 pIC50 = 8 Functional
Antagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assayAntagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assay
ChEMBL 492 4 1 5 6.0 CCc1cccc(NC(=O)N2CCc3nc(-c4ccc5c(c4)OCO5)nc(-c4ccccc4C)c3C2)c1 10.1016/j.bmcl.2011.03.084
CHEMBL1771456 68455 0 None - 1 Mouse 8.0 pIC50 = 8 Functional
Antagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assayAntagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assay
ChEMBL 492 4 1 5 6.0 CCc1cccc(NC(=O)N2CCc3nc(-c4ccc5c(c4)OCO5)nc(-c4ccccc4C)c3C2)c1 10.1016/j.bmcl.2011.03.084
153526199 196743 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human P2Y14R expressed in human HEK293 cells assessed as inhibition of cAMP level incubated for 30 mins by cAMP-glo assayAntagonist activity at human P2Y14R expressed in human HEK293 cells assessed as inhibition of cAMP level incubated for 30 mins by cAMP-glo assay
ChEMBL 396 4 1 3 5.7 O=C(Cc1ccc(C(F)(F)F)cc1)Nc1cccc(-c2nc3ccccc3o2)c1 10.1016/j.ejmech.2021.113933
CHEMBL5170675 196743 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human P2Y14R expressed in human HEK293 cells assessed as inhibition of cAMP level incubated for 30 mins by cAMP-glo assayAntagonist activity at human P2Y14R expressed in human HEK293 cells assessed as inhibition of cAMP level incubated for 30 mins by cAMP-glo assay
ChEMBL 396 4 1 3 5.7 O=C(Cc1ccc(C(F)(F)F)cc1)Nc1cccc(-c2nc3ccccc3o2)c1 10.1016/j.ejmech.2021.113933
54584878 68831 0 None - 1 Mouse 7.0 pIC50 = 7.0 Functional
Antagonist activity at mouse P2Y14 receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAntagonist activity at mouse P2Y14 receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 382 5 1 2 6.4 Cc1cccc(C)c1COc1ccc2c(-c3ccccc3)cc(C(=O)O)cc2c1 10.1016/j.bmcl.2011.03.081
CHEMBL1774887 68831 0 None - 1 Mouse 7.0 pIC50 = 7.0 Functional
Antagonist activity at mouse P2Y14 receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAntagonist activity at mouse P2Y14 receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 382 5 1 2 6.4 Cc1cccc(C)c1COc1ccc2c(-c3ccccc3)cc(C(=O)O)cc2c1 10.1016/j.bmcl.2011.03.081
54583936 68834 0 None - 1 Mouse 7.0 pIC50 = 7.0 Functional
Antagonist activity at mouse P2Y14 receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAntagonist activity at mouse P2Y14 receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 412 7 1 3 6.3 Cc1cccc(C)c1COc1ccc2c(OCc3ccccc3)cc(C(=O)O)cc2c1 10.1016/j.bmcl.2011.03.081
CHEMBL1774890 68834 0 None - 1 Mouse 7.0 pIC50 = 7.0 Functional
Antagonist activity at mouse P2Y14 receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAntagonist activity at mouse P2Y14 receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 412 7 1 3 6.3 Cc1cccc(C)c1COc1ccc2c(OCc3ccccc3)cc(C(=O)O)cc2c1 10.1016/j.bmcl.2011.03.081
168276760 197407 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assayAntagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assay
ChEMBL 353 5 2 4 3.3 Cc1ccc(C(=O)Nc2cc(C(=O)O)nn2Cc2ccccc2F)cc1 10.1021/acs.jmedchem.2c01632
CHEMBL5181115 197407 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assayAntagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assay
ChEMBL 353 5 2 4 3.3 Cc1ccc(C(=O)Nc2cc(C(=O)O)nn2Cc2ccccc2F)cc1 10.1021/acs.jmedchem.2c01632
54583556 68439 0 None - 1 Mouse 6.0 pIC50 = 6.0 Functional
Antagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assayAntagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assay
ChEMBL 465 5 2 5 4.9 CCc1cccc(NC(=O)N2CCc3nc(-c4cccnc4)nc(-c4ccccc4CO)c3C2)c1 10.1016/j.bmcl.2011.03.084
CHEMBL1771438 68439 0 None - 1 Mouse 6.0 pIC50 = 6.0 Functional
Antagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assayAntagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assay
ChEMBL 465 5 2 5 4.9 CCc1cccc(NC(=O)N2CCc3nc(-c4cccnc4)nc(-c4ccccc4CO)c3C2)c1 10.1016/j.bmcl.2011.03.084
25157642 68457 0 None - 1 Mouse 7.9 pIC50 = 7.9 Functional
Antagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assayAntagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assay
ChEMBL 450 4 1 5 5.1 CCc1cccc(NC(=O)N2CCc3nc(-c4cncnc4)nc(-c4ccccc4C)c3C2)c1 10.1016/j.bmcl.2011.03.084
CHEMBL1771458 68457 0 None - 1 Mouse 7.9 pIC50 = 7.9 Functional
Antagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assayAntagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assay
ChEMBL 450 4 1 5 5.1 CCc1cccc(NC(=O)N2CCc3nc(-c4cncnc4)nc(-c4ccccc4C)c3C2)c1 10.1016/j.bmcl.2011.03.084
153526158 198616 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human P2Y14R expressed in human HEK293 cells assessed as inhibition of cAMP level incubated for 30 mins by cAMP-glo assayAntagonist activity at human P2Y14R expressed in human HEK293 cells assessed as inhibition of cAMP level incubated for 30 mins by cAMP-glo assay
ChEMBL 358 5 1 4 4.7 COc1ccccc1CC(=O)Nc1cccc(-c2nc3ccccc3o2)c1 10.1016/j.ejmech.2021.113933
CHEMBL5198913 198616 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human P2Y14R expressed in human HEK293 cells assessed as inhibition of cAMP level incubated for 30 mins by cAMP-glo assayAntagonist activity at human P2Y14R expressed in human HEK293 cells assessed as inhibition of cAMP level incubated for 30 mins by cAMP-glo assay
ChEMBL 358 5 1 4 4.7 COc1ccccc1CC(=O)Nc1cccc(-c2nc3ccccc3o2)c1 10.1016/j.ejmech.2021.113933
153526164 196994 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human P2Y14R expressed in human HEK293 cells assessed as inhibition of cAMP level incubated for 30 mins by cAMP-glo assayAntagonist activity at human P2Y14R expressed in human HEK293 cells assessed as inhibition of cAMP level incubated for 30 mins by cAMP-glo assay
ChEMBL 400 8 1 4 5.9 CCCCOc1ccc(CC(=O)Nc2cccc(-c3nc4ccccc4o3)c2)cc1 10.1016/j.ejmech.2021.113933
CHEMBL5174678 196994 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human P2Y14R expressed in human HEK293 cells assessed as inhibition of cAMP level incubated for 30 mins by cAMP-glo assayAntagonist activity at human P2Y14R expressed in human HEK293 cells assessed as inhibition of cAMP level incubated for 30 mins by cAMP-glo assay
ChEMBL 400 8 1 4 5.9 CCCCOc1ccc(CC(=O)Nc2cccc(-c3nc4ccccc4o3)c2)cc1 10.1016/j.ejmech.2021.113933
153526194 197621 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human P2Y14R expressed in human HEK293 cells assessed as inhibition of cAMP level incubated for 30 mins by cAMP-glo assayAntagonist activity at human P2Y14R expressed in human HEK293 cells assessed as inhibition of cAMP level incubated for 30 mins by cAMP-glo assay
ChEMBL 446 5 1 4 6.2 O=C(Cc1cccc(OC(F)(F)F)c1)Nc1cccc(-c2nc3cc(Cl)ccc3o2)c1 10.1016/j.ejmech.2021.113933
CHEMBL5184355 197621 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human P2Y14R expressed in human HEK293 cells assessed as inhibition of cAMP level incubated for 30 mins by cAMP-glo assayAntagonist activity at human P2Y14R expressed in human HEK293 cells assessed as inhibition of cAMP level incubated for 30 mins by cAMP-glo assay
ChEMBL 446 5 1 4 6.2 O=C(Cc1cccc(OC(F)(F)F)c1)Nc1cccc(-c2nc3cc(Cl)ccc3o2)c1 10.1016/j.ejmech.2021.113933
54584497 68399 0 None - 1 Mouse 5.9 pIC50 = 5.9 Functional
Antagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assayAntagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assay
ChEMBL 447 4 1 4 5.7 C=Cc1cccc(NC(=O)N2CCc3nc(-c4cccnc4)nc(-c4ccccc4C)c3C2)c1 10.1016/j.bmcl.2011.03.084
CHEMBL1771240 68399 0 None - 1 Mouse 5.9 pIC50 = 5.9 Functional
Antagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assayAntagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assay
ChEMBL 447 4 1 4 5.7 C=Cc1cccc(NC(=O)N2CCc3nc(-c4cccnc4)nc(-c4ccccc4C)c3C2)c1 10.1016/j.bmcl.2011.03.084
54586408 68400 0 None - 1 Mouse 5.9 pIC50 = 5.9 Functional
Antagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assayAntagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assay
ChEMBL 461 4 1 4 6.0 Cc1ccccc1-c1nc(-c2cccnc2)nc2c1CN(C(=O)Nc1cccc(C3CC3)c1)CC2 10.1016/j.bmcl.2011.03.084
CHEMBL1771241 68400 0 None - 1 Mouse 5.9 pIC50 = 5.9 Functional
Antagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assayAntagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assay
ChEMBL 461 4 1 4 6.0 Cc1ccccc1-c1nc(-c2cccnc2)nc2c1CN(C(=O)Nc1cccc(C3CC3)c1)CC2 10.1016/j.bmcl.2011.03.084
54585444 68408 0 None - 1 Mouse 4.9 pIC50 = 4.9 Functional
Antagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assayAntagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assay
ChEMBL 469 4 1 4 6.0 CCc1cccc(NC(=O)N2CCc3nc(-c4cccnc4)nc(-c4cccc(Cl)c4)c3C2)c1 10.1016/j.bmcl.2011.03.084
CHEMBL1771249 68408 0 None - 1 Mouse 4.9 pIC50 = 4.9 Functional
Antagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assayAntagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assay
ChEMBL 469 4 1 4 6.0 CCc1cccc(NC(=O)N2CCc3nc(-c4cccnc4)nc(-c4cccc(Cl)c4)c3C2)c1 10.1016/j.bmcl.2011.03.084
54583559 68454 0 None - 1 Mouse 7.9 pIC50 = 7.9 Functional
Antagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assayAntagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assay
ChEMBL 499 4 1 4 6.8 CCc1cccc(NC(=O)N2CCc3nc(-c4cnc5ccccc5c4)nc(-c4ccccc4C)c3C2)c1 10.1016/j.bmcl.2011.03.084
CHEMBL1771455 68454 0 None - 1 Mouse 7.9 pIC50 = 7.9 Functional
Antagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assayAntagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assay
ChEMBL 499 4 1 4 6.8 CCc1cccc(NC(=O)N2CCc3nc(-c4cnc5ccccc5c4)nc(-c4ccccc4C)c3C2)c1 10.1016/j.bmcl.2011.03.084
54586809 68844 0 None - 1 Mouse 7.9 pIC50 = 7.9 Functional
Antagonist activity at mouse P2Y14 receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAntagonist activity at mouse P2Y14 receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 490 4 2 2 7.5 O=C(O)c1cc(-c2ccc(C(O)C(F)(F)F)cc2)c2ccc(-c3ccc(C(F)(F)F)cc3)cc2c1 10.1016/j.bmcl.2011.03.081
CHEMBL1774900 68844 0 None - 1 Mouse 7.9 pIC50 = 7.9 Functional
Antagonist activity at mouse P2Y14 receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAntagonist activity at mouse P2Y14 receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 490 4 2 2 7.5 O=C(O)c1cc(-c2ccc(C(O)C(F)(F)F)cc2)c2ccc(-c3ccc(C(F)(F)F)cc3)cc2c1 10.1016/j.bmcl.2011.03.081
153526172 197179 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human P2Y14R expressed in human HEK293 cells assessed as inhibition of cAMP level incubated for 30 mins by cAMP-glo assayAntagonist activity at human P2Y14R expressed in human HEK293 cells assessed as inhibition of cAMP level incubated for 30 mins by cAMP-glo assay
ChEMBL 396 4 1 3 6.0 O=C(Cc1cccc(Cl)c1)Nc1cccc(-c2nc3cc(Cl)ccc3o2)c1 10.1016/j.ejmech.2021.113933
CHEMBL5177634 197179 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human P2Y14R expressed in human HEK293 cells assessed as inhibition of cAMP level incubated for 30 mins by cAMP-glo assayAntagonist activity at human P2Y14R expressed in human HEK293 cells assessed as inhibition of cAMP level incubated for 30 mins by cAMP-glo assay
ChEMBL 396 4 1 3 6.0 O=C(Cc1cccc(Cl)c1)Nc1cccc(-c2nc3cc(Cl)ccc3o2)c1 10.1016/j.ejmech.2021.113933
54580588 68447 0 None - 1 Mouse 5.9 pIC50 = 5.9 Functional
Antagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assayAntagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assay
ChEMBL 462 4 1 3 6.6 CCc1cccc(NC(=O)N2CCc3nc(-c4cccc(C)c4)nc(-c4ccccc4C)c3C2)c1 10.1016/j.bmcl.2011.03.084
CHEMBL1771447 68447 0 None - 1 Mouse 5.9 pIC50 = 5.9 Functional
Antagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assayAntagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assay
ChEMBL 462 4 1 3 6.6 CCc1cccc(NC(=O)N2CCc3nc(-c4cccc(C)c4)nc(-c4ccccc4C)c3C2)c1 10.1016/j.bmcl.2011.03.084
54584879 68839 0 None - 1 Mouse 5.9 pIC50 = 5.9 Functional
Antagonist activity at mouse P2Y14 receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAntagonist activity at mouse P2Y14 receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 430 4 2 4 6.5 O=C(O)c1cc2cc(-c3ccc(OC(F)(F)F)cc3)ccc2c(-c2ccsc2)c1O 10.1016/j.bmcl.2011.03.081
CHEMBL1774895 68839 0 None - 1 Mouse 5.9 pIC50 = 5.9 Functional
Antagonist activity at mouse P2Y14 receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAntagonist activity at mouse P2Y14 receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 430 4 2 4 6.5 O=C(O)c1cc2cc(-c3ccc(OC(F)(F)F)cc3)ccc2c(-c2ccsc2)c1O 10.1016/j.bmcl.2011.03.081
54580937 68833 0 None - 1 Mouse 4.9 pIC50 = 4.9 Functional
Antagonist activity at mouse P2Y14 receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAntagonist activity at mouse P2Y14 receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 306 4 1 2 4.7 Cc1cccc(C)c1COc1ccc2ccc(C(=O)O)cc2c1 10.1016/j.bmcl.2011.03.081
CHEMBL1774889 68833 0 None - 1 Mouse 4.9 pIC50 = 4.9 Functional
Antagonist activity at mouse P2Y14 receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAntagonist activity at mouse P2Y14 receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 306 4 1 2 4.7 Cc1cccc(C)c1COc1ccc2ccc(C(=O)O)cc2c1 10.1016/j.bmcl.2011.03.081
168283280 198012 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assayAntagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assay
ChEMBL 341 5 2 4 3.7 Cc1ccc(C(=O)Nc2cc(C(=O)O)nn2CC2CCCCC2)cc1 10.1021/acs.jmedchem.2c01632
CHEMBL5189945 198012 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assayAntagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assay
ChEMBL 341 5 2 4 3.7 Cc1ccc(C(=O)Nc2cc(C(=O)O)nn2CC2CCCCC2)cc1 10.1021/acs.jmedchem.2c01632
42628974 68836 0 None - 1 Mouse 7.9 pIC50 = 7.9 Functional
Antagonist activity at mouse P2Y14 receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAntagonist activity at mouse P2Y14 receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 406 5 1 3 6.6 Cc1cc(F)cc(C)c1COc1ccc2c(-c3ccsc3)cc(C(=O)O)cc2c1 10.1016/j.bmcl.2011.03.081
CHEMBL1774892 68836 0 None - 1 Mouse 7.9 pIC50 = 7.9 Functional
Antagonist activity at mouse P2Y14 receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAntagonist activity at mouse P2Y14 receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 406 5 1 3 6.6 Cc1cc(F)cc(C)c1COc1ccc2c(-c3ccsc3)cc(C(=O)O)cc2c1 10.1016/j.bmcl.2011.03.081
154636992 196658 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assayAntagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assay
ChEMBL 367 6 2 4 3.3 Cc1ccc(C(=O)Nc2cc(CC(=O)O)nn2Cc2ccc(F)cc2)cc1 10.1021/acs.jmedchem.2c01632
CHEMBL5169372 196658 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assayAntagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assay
ChEMBL 367 6 2 4 3.3 Cc1ccc(C(=O)Nc2cc(CC(=O)O)nn2Cc2ccc(F)cc2)cc1 10.1021/acs.jmedchem.2c01632
54585479 68449 0 None - 1 Mouse 6.9 pIC50 = 6.9 Functional
Antagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assayAntagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assay
ChEMBL 473 4 1 4 6.1 CCc1cccc(NC(=O)N2CCc3nc(-c4cccc(C#N)c4)nc(-c4ccccc4C)c3C2)c1 10.1016/j.bmcl.2011.03.084
CHEMBL1771450 68449 0 None - 1 Mouse 6.9 pIC50 = 6.9 Functional
Antagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assayAntagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assay
ChEMBL 473 4 1 4 6.1 CCc1cccc(NC(=O)N2CCc3nc(-c4cccc(C#N)c4)nc(-c4ccccc4C)c3C2)c1 10.1016/j.bmcl.2011.03.084
25157951 68444 0 None - 1 Mouse 5.9 pIC50 = 5.9 Functional
Antagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assayAntagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assay
ChEMBL 449 4 1 4 5.7 CCc1cccc(NC(=O)N2CCc3nc(-c4ccncc4)nc(-c4ccccc4C)c3C2)c1 10.1016/j.bmcl.2011.03.084
CHEMBL1771444 68444 0 None - 1 Mouse 5.9 pIC50 = 5.9 Functional
Antagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assayAntagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assay
ChEMBL 449 4 1 4 5.7 CCc1cccc(NC(=O)N2CCc3nc(-c4ccncc4)nc(-c4ccccc4C)c3C2)c1 10.1016/j.bmcl.2011.03.084
168282149 197601 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assayAntagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assay
ChEMBL 403 5 2 4 4.2 Cc1ccc(C(=O)Nc2cc(C(=O)O)nn2Cc2cccc(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.2c01632
CHEMBL5183974 197601 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assayAntagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assay
ChEMBL 403 5 2 4 4.2 Cc1ccc(C(=O)Nc2cc(C(=O)O)nn2Cc2cccc(C(F)(F)F)c2)cc1 10.1021/acs.jmedchem.2c01632
54584496 68397 0 None - 1 Mouse 6.8 pIC50 = 6.8 Functional
Antagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assayAntagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assay
ChEMBL 463 5 1 4 6.1 CCCc1cccc(NC(=O)N2CCc3nc(-c4cccnc4)nc(-c4ccccc4C)c3C2)c1 10.1016/j.bmcl.2011.03.084
CHEMBL1771239 68397 0 None - 1 Mouse 6.8 pIC50 = 6.8 Functional
Antagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assayAntagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assay
ChEMBL 463 5 1 4 6.1 CCCc1cccc(NC(=O)N2CCc3nc(-c4cccnc4)nc(-c4ccccc4C)c3C2)c1 10.1016/j.bmcl.2011.03.084
54581597 68450 0 None - 1 Mouse 7.8 pIC50 = 7.8 Functional
Antagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assayAntagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assay
ChEMBL 473 4 1 4 6.1 CCc1cccc(NC(=O)N2CCc3nc(-c4ccc(C#N)cc4)nc(-c4ccccc4C)c3C2)c1 10.1016/j.bmcl.2011.03.084
CHEMBL1771451 68450 0 None - 1 Mouse 7.8 pIC50 = 7.8 Functional
Antagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assayAntagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assay
ChEMBL 473 4 1 4 6.1 CCc1cccc(NC(=O)N2CCc3nc(-c4ccc(C#N)cc4)nc(-c4ccccc4C)c3C2)c1 10.1016/j.bmcl.2011.03.084
153526195 198123 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human P2Y14R expressed in human HEK293 cells assessed as inhibition of cAMP level incubated for 30 mins by cAMP-glo assayAntagonist activity at human P2Y14R expressed in human HEK293 cells assessed as inhibition of cAMP level incubated for 30 mins by cAMP-glo assay
ChEMBL 412 5 1 4 5.6 O=C(Cc1cccc(OC(F)(F)F)c1)Nc1cccc(-c2nc3ccccc3o2)c1 10.1016/j.ejmech.2021.113933
CHEMBL5191737 198123 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human P2Y14R expressed in human HEK293 cells assessed as inhibition of cAMP level incubated for 30 mins by cAMP-glo assayAntagonist activity at human P2Y14R expressed in human HEK293 cells assessed as inhibition of cAMP level incubated for 30 mins by cAMP-glo assay
ChEMBL 412 5 1 4 5.6 O=C(Cc1cccc(OC(F)(F)F)c1)Nc1cccc(-c2nc3ccccc3o2)c1 10.1016/j.ejmech.2021.113933
54585443 68405 0 None - 1 Mouse 6.8 pIC50 = 6.8 Functional
Antagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assayAntagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assay
ChEMBL 483 4 1 4 6.3 CCc1cc(Cl)cc(NC(=O)N2CCc3nc(-c4cccnc4)nc(-c4ccccc4C)c3C2)c1 10.1016/j.bmcl.2011.03.084
CHEMBL1771246 68405 0 None - 1 Mouse 6.8 pIC50 = 6.8 Functional
Antagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assayAntagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assay
ChEMBL 483 4 1 4 6.3 CCc1cc(Cl)cc(NC(=O)N2CCc3nc(-c4cccnc4)nc(-c4ccccc4C)c3C2)c1 10.1016/j.bmcl.2011.03.084
153526157 197796 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human P2Y14R expressed in human HEK293 cells assessed as inhibition of cAMP level incubated for 30 mins by cAMP-glo assayAntagonist activity at human P2Y14R expressed in human HEK293 cells assessed as inhibition of cAMP level incubated for 30 mins by cAMP-glo assay
ChEMBL 392 5 1 4 5.3 COc1ccccc1CC(=O)Nc1cccc(-c2nc3cc(Cl)ccc3o2)c1 10.1016/j.ejmech.2021.113933
CHEMBL5186756 197796 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human P2Y14R expressed in human HEK293 cells assessed as inhibition of cAMP level incubated for 30 mins by cAMP-glo assayAntagonist activity at human P2Y14R expressed in human HEK293 cells assessed as inhibition of cAMP level incubated for 30 mins by cAMP-glo assay
ChEMBL 392 5 1 4 5.3 COc1ccccc1CC(=O)Nc1cccc(-c2nc3cc(Cl)ccc3o2)c1 10.1016/j.ejmech.2021.113933
168271053 196716 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assayAntagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assay
ChEMBL 335 5 2 4 3.2 Cc1ccc(C(=O)Nc2cc(C(=O)O)nn2Cc2ccccc2)cc1 10.1021/acs.jmedchem.2c01632
CHEMBL5170216 196716 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assayAntagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assay
ChEMBL 335 5 2 4 3.2 Cc1ccc(C(=O)Nc2cc(C(=O)O)nn2Cc2ccccc2)cc1 10.1021/acs.jmedchem.2c01632
153526204 198047 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human P2Y14R expressed in human HEK293 cells assessed as inhibition of cAMP level incubated for 30 mins by cAMP-glo assayAntagonist activity at human P2Y14R expressed in human HEK293 cells assessed as inhibition of cAMP level incubated for 30 mins by cAMP-glo assay
ChEMBL 356 4 1 3 5.3 Cc1ccc(CC(=O)Nc2cccc(-c3nc4cc(C)ccc4o3)c2)cc1 10.1016/j.ejmech.2021.113933
CHEMBL5190464 198047 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human P2Y14R expressed in human HEK293 cells assessed as inhibition of cAMP level incubated for 30 mins by cAMP-glo assayAntagonist activity at human P2Y14R expressed in human HEK293 cells assessed as inhibition of cAMP level incubated for 30 mins by cAMP-glo assay
ChEMBL 356 4 1 3 5.3 Cc1ccc(CC(=O)Nc2cccc(-c3nc4cc(C)ccc4o3)c2)cc1 10.1016/j.ejmech.2021.113933
54584877 68830 0 None - 1 Mouse 6.7 pIC50 = 6.7 Functional
Antagonist activity at mouse P2Y14 receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAntagonist activity at mouse P2Y14 receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 422 5 1 2 7.1 O=C(O)c1cc(-c2ccccc2)c2ccc(OCc3c(Cl)cccc3Cl)cc2c1 10.1016/j.bmcl.2011.03.081
CHEMBL1774886 68830 0 None - 1 Mouse 6.7 pIC50 = 6.7 Functional
Antagonist activity at mouse P2Y14 receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAntagonist activity at mouse P2Y14 receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 422 5 1 2 7.1 O=C(O)c1cc(-c2ccccc2)c2ccc(OCc3c(Cl)cccc3Cl)cc2c1 10.1016/j.bmcl.2011.03.081
54583937 68842 0 None - 1 Mouse 6.7 pIC50 = 6.7 Functional
Antagonist activity at mouse P2Y14 receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAntagonist activity at mouse P2Y14 receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 476 4 1 4 6.4 CS(=O)(=O)c1cscc1-c1cc(C(=O)O)cc2cc(-c3ccc(C(F)(F)F)cc3)ccc12 10.1016/j.bmcl.2011.03.081
CHEMBL1774898 68842 0 None - 1 Mouse 6.7 pIC50 = 6.7 Functional
Antagonist activity at mouse P2Y14 receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAntagonist activity at mouse P2Y14 receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 476 4 1 4 6.4 CS(=O)(=O)c1cscc1-c1cc(C(=O)O)cc2cc(-c3ccc(C(F)(F)F)cc3)ccc12 10.1016/j.bmcl.2011.03.081
54583516 68395 0 None - 1 Mouse 5.7 pIC50 = 5.7 Functional
Antagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assayAntagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assay
ChEMBL 435 3 1 4 5.4 Cc1cccc(NC(=O)N2CCc3nc(-c4cccnc4)nc(-c4ccccc4C)c3C2)c1 10.1016/j.bmcl.2011.03.084
CHEMBL1771237 68395 0 None - 1 Mouse 5.7 pIC50 = 5.7 Functional
Antagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assayAntagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assay
ChEMBL 435 3 1 4 5.4 Cc1cccc(NC(=O)N2CCc3nc(-c4cccnc4)nc(-c4ccccc4C)c3C2)c1 10.1016/j.bmcl.2011.03.084
1341154 197776 11 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human P2Y14R expressed in human HEK293 cells assessed as inhibition of cAMP level incubated for 30 mins by cAMP-glo assayAntagonist activity at human P2Y14R expressed in human HEK293 cells assessed as inhibition of cAMP level incubated for 30 mins by cAMP-glo assay
ChEMBL 358 5 1 4 4.7 COc1ccc(CC(=O)Nc2cccc(-c3nc4ccccc4o3)c2)cc1 10.1016/j.ejmech.2021.113933
CHEMBL5186555 197776 11 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human P2Y14R expressed in human HEK293 cells assessed as inhibition of cAMP level incubated for 30 mins by cAMP-glo assayAntagonist activity at human P2Y14R expressed in human HEK293 cells assessed as inhibition of cAMP level incubated for 30 mins by cAMP-glo assay
ChEMBL 358 5 1 4 4.7 COc1ccc(CC(=O)Nc2cccc(-c3nc4ccccc4o3)c2)cc1 10.1016/j.ejmech.2021.113933
164614593 191786 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at P2Y14 (unknown origin) expressed in HEK293 cells assessed as reduction in cAMP production incubated for 30 mins by ADP-glo assayAntagonist activity at P2Y14 (unknown origin) expressed in HEK293 cells assessed as reduction in cAMP production incubated for 30 mins by ADP-glo assay
ChEMBL 321 4 2 3 4.2 Cc1ccc(C(=O)Nc2cc(C(=O)O)cc(-c3ccoc3)c2)cc1 10.1016/j.ejmech.2021.113313
CHEMBL4854775 191786 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at P2Y14 (unknown origin) expressed in HEK293 cells assessed as reduction in cAMP production incubated for 30 mins by ADP-glo assayAntagonist activity at P2Y14 (unknown origin) expressed in HEK293 cells assessed as reduction in cAMP production incubated for 30 mins by ADP-glo assay
ChEMBL 321 4 2 3 4.2 Cc1ccc(C(=O)Nc2cc(C(=O)O)cc(-c3ccoc3)c2)cc1 10.1016/j.ejmech.2021.113313
164611449 192022 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at P2Y14 (unknown origin) expressed in HEK293 cells assessed as reduction in cAMP production incubated for 30 mins by ADP-glo assayAntagonist activity at P2Y14 (unknown origin) expressed in HEK293 cells assessed as reduction in cAMP production incubated for 30 mins by ADP-glo assay
ChEMBL 321 4 3 3 3.3 Cc1ccc(C(=O)Nc2cc(C(=O)O)cc(-c3cc[nH]n3)c2)cc1 10.1016/j.ejmech.2021.113313
CHEMBL4858280 192022 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at P2Y14 (unknown origin) expressed in HEK293 cells assessed as reduction in cAMP production incubated for 30 mins by ADP-glo assayAntagonist activity at P2Y14 (unknown origin) expressed in HEK293 cells assessed as reduction in cAMP production incubated for 30 mins by ADP-glo assay
ChEMBL 321 4 3 3 3.3 Cc1ccc(C(=O)Nc2cc(C(=O)O)cc(-c3cc[nH]n3)c2)cc1 10.1016/j.ejmech.2021.113313
164627664 193161 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at P2Y14 (unknown origin) expressed in HEK293 cells assessed as reduction in cAMP production incubated for 30 mins by ADP-glo assayAntagonist activity at P2Y14 (unknown origin) expressed in HEK293 cells assessed as reduction in cAMP production incubated for 30 mins by ADP-glo assay
ChEMBL 350 4 2 4 4.2 Cc1ccc(C(=O)Nc2cc(C(=O)O)cc(-c3c(C)noc3C)c2)cc1 10.1016/j.ejmech.2021.113313
CHEMBL4875670 193161 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at P2Y14 (unknown origin) expressed in HEK293 cells assessed as reduction in cAMP production incubated for 30 mins by ADP-glo assayAntagonist activity at P2Y14 (unknown origin) expressed in HEK293 cells assessed as reduction in cAMP production incubated for 30 mins by ADP-glo assay
ChEMBL 350 4 2 4 4.2 Cc1ccc(C(=O)Nc2cc(C(=O)O)cc(-c3c(C)noc3C)c2)cc1 10.1016/j.ejmech.2021.113313
54585843 68843 0 None - 1 Mouse 7.7 pIC50 = 7.7 Functional
Antagonist activity at mouse P2Y14 receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAntagonist activity at mouse P2Y14 receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 470 4 1 3 6.3 CS(=O)(=O)c1ccc(-c2cc(C(=O)O)cc3cc(-c4ccc(C(F)(F)F)cc4)ccc23)cc1 10.1016/j.bmcl.2011.03.081
CHEMBL1774899 68843 0 None - 1 Mouse 7.7 pIC50 = 7.7 Functional
Antagonist activity at mouse P2Y14 receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAntagonist activity at mouse P2Y14 receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 470 4 1 3 6.3 CS(=O)(=O)c1ccc(-c2cc(C(=O)O)cc3cc(-c4ccc(C(F)(F)F)cc4)ccc23)cc1 10.1016/j.bmcl.2011.03.081
153526165 197202 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human P2Y14R expressed in human HEK293 cells assessed as inhibition of cAMP level incubated for 30 mins by cAMP-glo assayAntagonist activity at human P2Y14R expressed in human HEK293 cells assessed as inhibition of cAMP level incubated for 30 mins by cAMP-glo assay
ChEMBL 342 4 1 3 5.0 Cc1cccc(CC(=O)Nc2cccc(-c3nc4ccccc4o3)c2)c1 10.1016/j.ejmech.2021.113933
CHEMBL5177972 197202 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human P2Y14R expressed in human HEK293 cells assessed as inhibition of cAMP level incubated for 30 mins by cAMP-glo assayAntagonist activity at human P2Y14R expressed in human HEK293 cells assessed as inhibition of cAMP level incubated for 30 mins by cAMP-glo assay
ChEMBL 342 4 1 3 5.0 Cc1cccc(CC(=O)Nc2cccc(-c3nc4ccccc4o3)c2)c1 10.1016/j.ejmech.2021.113933
54582931 68832 0 None - 1 Mouse 5.7 pIC50 = 5.7 Functional
Antagonist activity at mouse P2Y14 receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAntagonist activity at mouse P2Y14 receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 382 5 1 2 6.4 Cc1cccc(C)c1OCc1ccc2c(-c3ccccc3)cc(C(=O)O)cc2c1 10.1016/j.bmcl.2011.03.081
CHEMBL1774888 68832 0 None - 1 Mouse 5.7 pIC50 = 5.7 Functional
Antagonist activity at mouse P2Y14 receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAntagonist activity at mouse P2Y14 receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 382 5 1 2 6.4 Cc1cccc(C)c1OCc1ccc2c(-c3ccccc3)cc(C(=O)O)cc2c1 10.1016/j.bmcl.2011.03.081
168279045 197962 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assayAntagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assay
ChEMBL 369 5 2 4 3.8 Cc1ccc(C(=O)Nc2cc(C(=O)O)nn2Cc2cccc(Cl)c2)cc1 10.1021/acs.jmedchem.2c01632
CHEMBL5189099 197962 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assayAntagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assay
ChEMBL 369 5 2 4 3.8 Cc1ccc(C(=O)Nc2cc(C(=O)O)nn2Cc2cccc(Cl)c2)cc1 10.1021/acs.jmedchem.2c01632
153526161 198191 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human P2Y14R expressed in human HEK293 cells assessed as inhibition of cAMP level incubated for 30 mins by cAMP-glo assayAntagonist activity at human P2Y14R expressed in human HEK293 cells assessed as inhibition of cAMP level incubated for 30 mins by cAMP-glo assay
ChEMBL 392 5 1 4 5.3 COc1cccc(CC(=O)Nc2cccc(-c3nc4cc(Cl)ccc4o3)c2)c1 10.1016/j.ejmech.2021.113933
CHEMBL5192666 198191 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human P2Y14R expressed in human HEK293 cells assessed as inhibition of cAMP level incubated for 30 mins by cAMP-glo assayAntagonist activity at human P2Y14R expressed in human HEK293 cells assessed as inhibition of cAMP level incubated for 30 mins by cAMP-glo assay
ChEMBL 392 5 1 4 5.3 COc1cccc(CC(=O)Nc2cccc(-c3nc4cc(Cl)ccc4o3)c2)c1 10.1016/j.ejmech.2021.113933
16911458 197371 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human P2Y14R expressed in human HEK293 cells assessed as inhibition of cAMP level incubated for 30 mins by cAMP-glo assayAntagonist activity at human P2Y14R expressed in human HEK293 cells assessed as inhibition of cAMP level incubated for 30 mins by cAMP-glo assay
ChEMBL 358 5 1 4 4.7 COc1cccc(CC(=O)Nc2cccc(-c3nc4ccccc4o3)c2)c1 10.1016/j.ejmech.2021.113933
CHEMBL5180500 197371 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human P2Y14R expressed in human HEK293 cells assessed as inhibition of cAMP level incubated for 30 mins by cAMP-glo assayAntagonist activity at human P2Y14R expressed in human HEK293 cells assessed as inhibition of cAMP level incubated for 30 mins by cAMP-glo assay
ChEMBL 358 5 1 4 4.7 COc1cccc(CC(=O)Nc2cccc(-c3nc4ccccc4o3)c2)c1 10.1016/j.ejmech.2021.113933
168285041 198339 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assayAntagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assay
ChEMBL 369 5 2 4 3.8 Cc1ccc(C(=O)Nc2cc(C(=O)O)nn2Cc2ccccc2Cl)cc1 10.1021/acs.jmedchem.2c01632
CHEMBL5194765 198339 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assayAntagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assay
ChEMBL 369 5 2 4 3.8 Cc1ccc(C(=O)Nc2cc(C(=O)O)nn2Cc2ccccc2Cl)cc1 10.1021/acs.jmedchem.2c01632
54583558 68451 0 None - 1 Mouse 7.6 pIC50 = 7.6 Functional
Antagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assayAntagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assay
ChEMBL 466 4 1 3 6.4 CCc1cccc(NC(=O)N2CCc3nc(-c4ccc(F)cc4)nc(-c4ccccc4C)c3C2)c1 10.1016/j.bmcl.2011.03.084
CHEMBL1771452 68451 0 None - 1 Mouse 7.6 pIC50 = 7.6 Functional
Antagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assayAntagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assay
ChEMBL 466 4 1 3 6.4 CCc1cccc(NC(=O)N2CCc3nc(-c4ccc(F)cc4)nc(-c4ccccc4C)c3C2)c1 10.1016/j.bmcl.2011.03.084
153526196 196911 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human P2Y14R expressed in human HEK293 cells assessed as inhibition of cAMP level incubated for 30 mins by cAMP-glo assayAntagonist activity at human P2Y14R expressed in human HEK293 cells assessed as inhibition of cAMP level incubated for 30 mins by cAMP-glo assay
ChEMBL 406 4 1 3 5.4 O=C(Cc1cccc(Br)c1)Nc1cccc(-c2nc3ccccc3o2)c1 10.1016/j.ejmech.2021.113933
CHEMBL5173454 196911 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human P2Y14R expressed in human HEK293 cells assessed as inhibition of cAMP level incubated for 30 mins by cAMP-glo assayAntagonist activity at human P2Y14R expressed in human HEK293 cells assessed as inhibition of cAMP level incubated for 30 mins by cAMP-glo assay
ChEMBL 406 4 1 3 5.4 O=C(Cc1cccc(Br)c1)Nc1cccc(-c2nc3ccccc3o2)c1 10.1016/j.ejmech.2021.113933
54581994 68835 0 None - 1 Mouse 7.6 pIC50 = 7.6 Functional
Antagonist activity at mouse P2Y14 receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAntagonist activity at mouse P2Y14 receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 388 5 1 3 6.5 Cc1cccc(C)c1COc1ccc2c(-c3ccsc3)cc(C(=O)O)cc2c1 10.1016/j.bmcl.2011.03.081
CHEMBL1774891 68835 0 None - 1 Mouse 7.6 pIC50 = 7.6 Functional
Antagonist activity at mouse P2Y14 receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAntagonist activity at mouse P2Y14 receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 388 5 1 3 6.5 Cc1cccc(C)c1COc1ccc2c(-c3ccsc3)cc(C(=O)O)cc2c1 10.1016/j.bmcl.2011.03.081
153526190 197764 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human P2Y14R expressed in human HEK293 cells assessed as inhibition of cAMP level incubated for 30 mins by cAMP-glo assayAntagonist activity at human P2Y14R expressed in human HEK293 cells assessed as inhibition of cAMP level incubated for 30 mins by cAMP-glo assay
ChEMBL 430 4 1 3 6.3 O=C(Cc1cccc(C(F)(F)F)c1)Nc1cccc(-c2nc3cc(Cl)ccc3o2)c1 10.1016/j.ejmech.2021.113933
CHEMBL5186266 197764 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human P2Y14R expressed in human HEK293 cells assessed as inhibition of cAMP level incubated for 30 mins by cAMP-glo assayAntagonist activity at human P2Y14R expressed in human HEK293 cells assessed as inhibition of cAMP level incubated for 30 mins by cAMP-glo assay
ChEMBL 430 4 1 3 6.3 O=C(Cc1cccc(C(F)(F)F)c1)Nc1cccc(-c2nc3cc(Cl)ccc3o2)c1 10.1016/j.ejmech.2021.113933
54585477 68443 0 None - 1 Mouse 5.6 pIC50 = 5.6 Functional
Antagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assayAntagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assay
ChEMBL 465 4 1 4 4.9 CCc1cccc(NC(=O)N2CCc3nc(-c4ccc[n+]([O-])c4)nc(-c4ccccc4C)c3C2)c1 10.1016/j.bmcl.2011.03.084
CHEMBL1771442 68443 0 None - 1 Mouse 5.6 pIC50 = 5.6 Functional
Antagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assayAntagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assay
ChEMBL 465 4 1 4 4.9 CCc1cccc(NC(=O)N2CCc3nc(-c4ccc[n+]([O-])c4)nc(-c4ccccc4C)c3C2)c1 10.1016/j.bmcl.2011.03.084
54583517 68403 0 None - 1 Mouse 7.5 pIC50 = 7.5 Functional
Antagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assayAntagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assay
ChEMBL 467 4 1 4 6.1 Cc1ccccc1-c1nc(-c2cccnc2)nc2c1CN(C(=O)Nc1cccc(C(C)F)c1)CC2 10.1016/j.bmcl.2011.03.084
CHEMBL1771244 68403 0 None - 1 Mouse 7.5 pIC50 = 7.5 Functional
Antagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assayAntagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assay
ChEMBL 467 4 1 4 6.1 Cc1ccccc1-c1nc(-c2cccnc2)nc2c1CN(C(=O)Nc1cccc(C(C)F)c1)CC2 10.1016/j.bmcl.2011.03.084
54585480 68456 0 None - 1 Mouse 8.5 pIC50 = 8.5 Functional
Antagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assayAntagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assay
ChEMBL 474 4 1 5 5.5 CCc1cccc(NC(=O)N2CCc3nc(-c4cnccc4C#N)nc(-c4ccccc4C)c3C2)c1 10.1016/j.bmcl.2011.03.084
CHEMBL1771457 68456 0 None - 1 Mouse 8.5 pIC50 = 8.5 Functional
Antagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assayAntagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assay
ChEMBL 474 4 1 5 5.5 CCc1cccc(NC(=O)N2CCc3nc(-c4cnccc4C#N)nc(-c4ccccc4C)c3C2)c1 10.1016/j.bmcl.2011.03.084
155564566 182271 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human P2Y14R stably expressed in human forskolin treated THP1 cells assessed as reduction in P2Y14R agonist UDPG-induced inhibition of cAMP production incubated for 15 mins by competitive enzyme-linked immunoassayAntagonist activity at human P2Y14R stably expressed in human forskolin treated THP1 cells assessed as reduction in P2Y14R agonist UDPG-induced inhibition of cAMP production incubated for 15 mins by competitive enzyme-linked immunoassay
ChEMBL 401 5 3 4 4.2 O=C(O)c1cc(NC(=O)c2ccncc2)cc(-c2ccc(C3CCNCC3)cc2)c1 10.1016/j.ejmech.2019.111564
CHEMBL4577585 182271 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human P2Y14R stably expressed in human forskolin treated THP1 cells assessed as reduction in P2Y14R agonist UDPG-induced inhibition of cAMP production incubated for 15 mins by competitive enzyme-linked immunoassayAntagonist activity at human P2Y14R stably expressed in human forskolin treated THP1 cells assessed as reduction in P2Y14R agonist UDPG-induced inhibition of cAMP production incubated for 15 mins by competitive enzyme-linked immunoassay
ChEMBL 401 5 3 4 4.2 O=C(O)c1cc(NC(=O)c2ccncc2)cc(-c2ccc(C3CCNCC3)cc2)c1 10.1016/j.ejmech.2019.111564
168293389 198906 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assayAntagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assay
ChEMBL 381 6 2 5 3.2 CC(=O)c1ccc(C(=O)Nc2cc(C(=O)O)nn2Cc2ccc(F)cc2)cc1 10.1021/acs.jmedchem.2c01632
CHEMBL5203559 198906 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assayAntagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assay
ChEMBL 381 6 2 5 3.2 CC(=O)c1ccc(C(=O)Nc2cc(C(=O)O)nn2Cc2ccc(F)cc2)cc1 10.1021/acs.jmedchem.2c01632
154636998 198346 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assayAntagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assay
ChEMBL 403 5 2 4 4.2 Cc1ccc(C(=O)Nc2cc(C(=O)O)nn2Cc2ccc(C(F)(F)F)cc2)cc1 10.1021/acs.jmedchem.2c01632
CHEMBL5194881 198346 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assayAntagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assay
ChEMBL 403 5 2 4 4.2 Cc1ccc(C(=O)Nc2cc(C(=O)O)nn2Cc2ccc(C(F)(F)F)cc2)cc1 10.1021/acs.jmedchem.2c01632
54586445 68452 0 None - 1 Mouse 7.5 pIC50 = 7.5 Functional
Antagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assayAntagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assay
ChEMBL 466 4 1 3 6.4 CCc1cccc(NC(=O)N2CCc3nc(-c4cccc(F)c4)nc(-c4ccccc4C)c3C2)c1 10.1016/j.bmcl.2011.03.084
CHEMBL1771453 68452 0 None - 1 Mouse 7.5 pIC50 = 7.5 Functional
Antagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assayAntagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assay
ChEMBL 466 4 1 3 6.4 CCc1cccc(NC(=O)N2CCc3nc(-c4cccc(F)c4)nc(-c4ccccc4C)c3C2)c1 10.1016/j.bmcl.2011.03.084
153526166 198094 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human P2Y14R expressed in human HEK293 cells assessed as inhibition of cAMP level incubated for 30 mins by cAMP-glo assayAntagonist activity at human P2Y14R expressed in human HEK293 cells assessed as inhibition of cAMP level incubated for 30 mins by cAMP-glo assay
ChEMBL 440 4 1 3 6.1 O=C(Cc1ccccc1Br)Nc1cccc(-c2nc3cc(Cl)ccc3o2)c1 10.1016/j.ejmech.2021.113933
CHEMBL5191340 198094 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human P2Y14R expressed in human HEK293 cells assessed as inhibition of cAMP level incubated for 30 mins by cAMP-glo assayAntagonist activity at human P2Y14R expressed in human HEK293 cells assessed as inhibition of cAMP level incubated for 30 mins by cAMP-glo assay
ChEMBL 440 4 1 3 6.1 O=C(Cc1ccccc1Br)Nc1cccc(-c2nc3cc(Cl)ccc3o2)c1 10.1016/j.ejmech.2021.113933
54585842 68841 0 None - 1 Mouse 6.5 pIC50 = 6.5 Functional
Antagonist activity at mouse P2Y14 receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAntagonist activity at mouse P2Y14 receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 492 5 1 5 6.2 CS(=O)(=O)c1cscc1-c1cc(C(=O)O)cc2cc(-c3ccc(OC(F)(F)F)cc3)ccc12 10.1016/j.bmcl.2011.03.081
CHEMBL1774897 68841 0 None - 1 Mouse 6.5 pIC50 = 6.5 Functional
Antagonist activity at mouse P2Y14 receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAntagonist activity at mouse P2Y14 receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 492 5 1 5 6.2 CS(=O)(=O)c1cscc1-c1cc(C(=O)O)cc2cc(-c3ccc(OC(F)(F)F)cc3)ccc12 10.1016/j.bmcl.2011.03.081
54582583 68437 0 None - 1 Mouse 5.5 pIC50 = 5.5 Functional
Antagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assayAntagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assay
ChEMBL 465 5 1 5 5.4 CCc1cccc(NC(=O)N2CCc3nc(-c4cccnc4)nc(-c4ccccc4OC)c3C2)c1 10.1016/j.bmcl.2011.03.084
CHEMBL1771436 68437 0 None - 1 Mouse 5.5 pIC50 = 5.5 Functional
Antagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assayAntagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assay
ChEMBL 465 5 1 5 5.4 CCc1cccc(NC(=O)N2CCc3nc(-c4cccnc4)nc(-c4ccccc4OC)c3C2)c1 10.1016/j.bmcl.2011.03.084
153526192 197020 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human P2Y14R expressed in human HEK293 cells assessed as inhibition of cAMP level incubated for 30 mins by cAMP-glo assayAntagonist activity at human P2Y14R expressed in human HEK293 cells assessed as inhibition of cAMP level incubated for 30 mins by cAMP-glo assay
ChEMBL 410 4 1 3 6.0 Cc1ccc2oc(-c3cccc(NC(=O)Cc4ccc(C(F)(F)F)cc4)c3)nc2c1 10.1016/j.ejmech.2021.113933
CHEMBL5175099 197020 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human P2Y14R expressed in human HEK293 cells assessed as inhibition of cAMP level incubated for 30 mins by cAMP-glo assayAntagonist activity at human P2Y14R expressed in human HEK293 cells assessed as inhibition of cAMP level incubated for 30 mins by cAMP-glo assay
ChEMBL 410 4 1 3 6.0 Cc1ccc2oc(-c3cccc(NC(=O)Cc4ccc(C(F)(F)F)cc4)c3)nc2c1 10.1016/j.ejmech.2021.113933
54584880 68840 0 None - 1 Mouse 6.5 pIC50 = 6.5 Functional
Antagonist activity at mouse P2Y14 receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAntagonist activity at mouse P2Y14 receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 580 5 2 4 8.1 O=C(O)c1cc(-c2cscc2C(O)(C(F)(F)F)C(F)(F)F)c2ccc(-c3ccc(OC(F)(F)F)cc3)cc2c1 10.1016/j.bmcl.2011.03.081
CHEMBL1774896 68840 0 None - 1 Mouse 6.5 pIC50 = 6.5 Functional
Antagonist activity at mouse P2Y14 receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAntagonist activity at mouse P2Y14 receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 580 5 2 4 8.1 O=C(O)c1cc(-c2cscc2C(O)(C(F)(F)F)C(F)(F)F)c2ccc(-c3ccc(OC(F)(F)F)cc3)cc2c1 10.1016/j.bmcl.2011.03.081
19027172 68828 0 None -1 2 Mouse 5.5 pIC50 = 5.5 Functional
Antagonist activity at mouse P2Y14 receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAntagonist activity at mouse P2Y14 receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 354 5 1 2 5.8 O=C(O)c1cc(-c2ccccc2)c2ccc(OCc3ccccc3)cc2c1 10.1016/j.bmcl.2011.03.081
CHEMBL1774882 68828 0 None -1 2 Mouse 5.5 pIC50 = 5.5 Functional
Antagonist activity at mouse P2Y14 receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAntagonist activity at mouse P2Y14 receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 354 5 1 2 5.8 O=C(O)c1cc(-c2ccccc2)c2ccc(OCc3ccccc3)cc2c1 10.1016/j.bmcl.2011.03.081
168294899 199105 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assayAntagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assay
ChEMBL 313 5 2 4 2.9 Cc1ccc(C(=O)Nc2cc(C(=O)O)nn2CC2CCC2)cc1 10.1021/acs.jmedchem.2c01632
CHEMBL5206480 199105 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assayAntagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assay
ChEMBL 313 5 2 4 2.9 Cc1ccc(C(=O)Nc2cc(C(=O)O)nn2CC2CCC2)cc1 10.1021/acs.jmedchem.2c01632
54580548 68407 0 None - 1 Mouse 5.4 pIC50 = 5.4 Functional
Antagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assayAntagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assay
ChEMBL 453 4 1 4 5.5 CCc1cccc(NC(=O)N2CCc3nc(-c4cccnc4)nc(-c4ccccc4F)c3C2)c1 10.1016/j.bmcl.2011.03.084
CHEMBL1771248 68407 0 None - 1 Mouse 5.4 pIC50 = 5.4 Functional
Antagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assayAntagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assay
ChEMBL 453 4 1 4 5.5 CCc1cccc(NC(=O)N2CCc3nc(-c4cccnc4)nc(-c4ccccc4F)c3C2)c1 10.1016/j.bmcl.2011.03.084
54582932 68838 0 None - 1 Mouse 6.4 pIC50 = 6.4 Functional
Antagonist activity at mouse P2Y14 receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAntagonist activity at mouse P2Y14 receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 432 4 1 3 7.0 O=C(O)c1cc2cc(-c3ccc(OC(F)(F)F)cc3)ccc2c(-c2ccsc2)c1F 10.1016/j.bmcl.2011.03.081
CHEMBL1774894 68838 0 None - 1 Mouse 6.4 pIC50 = 6.4 Functional
Antagonist activity at mouse P2Y14 receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAntagonist activity at mouse P2Y14 receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 432 4 1 3 7.0 O=C(O)c1cc2cc(-c3ccc(OC(F)(F)F)cc3)ccc2c(-c2ccsc2)c1F 10.1016/j.bmcl.2011.03.081
54585446 68410 0 None - 1 Mouse 6.4 pIC50 = 6.4 Functional
Antagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assayAntagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assay
ChEMBL 463 5 1 4 5.9 CCc1cccc(NC(=O)N2CCc3nc(-c4cccnc4)nc(-c4ccccc4CC)c3C2)c1 10.1016/j.bmcl.2011.03.084
CHEMBL1771251 68410 0 None - 1 Mouse 6.4 pIC50 = 6.4 Functional
Antagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assayAntagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assay
ChEMBL 463 5 1 4 5.9 CCc1cccc(NC(=O)N2CCc3nc(-c4cccnc4)nc(-c4ccccc4CC)c3C2)c1 10.1016/j.bmcl.2011.03.084
25110840 68459 0 None - 1 Mouse 8.4 pIC50 = 8.4 Functional
Antagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assayAntagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assay
ChEMBL 467 4 1 5 5.9 CCc1cccc(NC(=O)N2CCc3nc(-c4c(C)noc4C)nc(-c4ccccc4C)c3C2)c1 10.1016/j.bmcl.2011.03.084
CHEMBL1771460 68459 0 None - 1 Mouse 8.4 pIC50 = 8.4 Functional
Antagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assayAntagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assay
ChEMBL 467 4 1 5 5.9 CCc1cccc(NC(=O)N2CCc3nc(-c4c(C)noc4C)nc(-c4ccccc4C)c3C2)c1 10.1016/j.bmcl.2011.03.084
42630802 68845 0 None - 1 Mouse 8.4 pIC50 = 8.4 Functional
Antagonist activity at mouse P2Y14 receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAntagonist activity at mouse P2Y14 receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 490 4 2 2 7.5 O=C(O)c1cc(-c2ccc([C@@H](O)C(F)(F)F)cc2)c2ccc(-c3ccc(C(F)(F)F)cc3)cc2c1 10.1016/j.bmcl.2011.03.081
CHEMBL1774901 68845 0 None - 1 Mouse 8.4 pIC50 = 8.4 Functional
Antagonist activity at mouse P2Y14 receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAntagonist activity at mouse P2Y14 receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 490 4 2 2 7.5 O=C(O)c1cc(-c2ccc([C@@H](O)C(F)(F)F)cc2)c2ccc(-c3ccc(C(F)(F)F)cc3)cc2c1 10.1016/j.bmcl.2011.03.081
168279771 197499 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assayAntagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assay
ChEMBL 389 5 2 4 3.6 Cc1ccc(C(=O)Nc2cc(C(=O)O)nn2Cc2cc(F)c(F)c(F)c2)cc1 10.1021/acs.jmedchem.2c01632
CHEMBL5182459 197499 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assayAntagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assay
ChEMBL 389 5 2 4 3.6 Cc1ccc(C(=O)Nc2cc(C(=O)O)nn2Cc2cc(F)c(F)c(F)c2)cc1 10.1021/acs.jmedchem.2c01632
168276085 197030 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assayAntagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assay
ChEMBL 371 5 2 4 3.5 Cc1ccc(C(=O)Nc2cc(C(=O)O)nn2Cc2ccc(F)c(F)c2)cc1 10.1021/acs.jmedchem.2c01632
CHEMBL5175291 197030 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assayAntagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assay
ChEMBL 371 5 2 4 3.5 Cc1ccc(C(=O)Nc2cc(C(=O)O)nn2Cc2ccc(F)c(F)c2)cc1 10.1021/acs.jmedchem.2c01632
155549217 180602 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human P2Y14R stably expressed in human forskolin treated THP1 cells assessed as reduction in P2Y14R agonist UDPG-induced inhibition of cAMP production incubated for 15 mins by competitive enzyme-linked immunoassayAntagonist activity at human P2Y14R stably expressed in human forskolin treated THP1 cells assessed as reduction in P2Y14R agonist UDPG-induced inhibition of cAMP production incubated for 15 mins by competitive enzyme-linked immunoassay
ChEMBL 402 5 3 5 3.6 O=C(O)c1cc(NC(=O)c2cnccn2)cc(-c2ccc(C3CCNCC3)cc2)c1 10.1016/j.ejmech.2019.111564
CHEMBL4538561 180602 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human P2Y14R stably expressed in human forskolin treated THP1 cells assessed as reduction in P2Y14R agonist UDPG-induced inhibition of cAMP production incubated for 15 mins by competitive enzyme-linked immunoassayAntagonist activity at human P2Y14R stably expressed in human forskolin treated THP1 cells assessed as reduction in P2Y14R agonist UDPG-induced inhibition of cAMP production incubated for 15 mins by competitive enzyme-linked immunoassay
ChEMBL 402 5 3 5 3.6 O=C(O)c1cc(NC(=O)c2cnccn2)cc(-c2ccc(C3CCNCC3)cc2)c1 10.1016/j.ejmech.2019.111564
155525228 177711 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human P2Y14R stably expressed in human forskolin treated THP1 cells assessed as reduction in P2Y14R agonist UDPG-induced inhibition of cAMP production incubated for 15 mins by competitive enzyme-linked immunoassayAntagonist activity at human P2Y14R stably expressed in human forskolin treated THP1 cells assessed as reduction in P2Y14R agonist UDPG-induced inhibition of cAMP production incubated for 15 mins by competitive enzyme-linked immunoassay
ChEMBL 425 5 3 4 4.6 N#Cc1ccc(C(=O)Nc2cc(C(=O)O)cc(-c3ccc(C4CCNCC4)cc3)c2)cc1 10.1016/j.ejmech.2019.111564
CHEMBL4455311 177711 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human P2Y14R stably expressed in human forskolin treated THP1 cells assessed as reduction in P2Y14R agonist UDPG-induced inhibition of cAMP production incubated for 15 mins by competitive enzyme-linked immunoassayAntagonist activity at human P2Y14R stably expressed in human forskolin treated THP1 cells assessed as reduction in P2Y14R agonist UDPG-induced inhibition of cAMP production incubated for 15 mins by competitive enzyme-linked immunoassay
ChEMBL 425 5 3 4 4.6 N#Cc1ccc(C(=O)Nc2cc(C(=O)O)cc(-c3ccc(C4CCNCC4)cc3)c2)cc1 10.1016/j.ejmech.2019.111564
168280360 197973 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assayAntagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assay
ChEMBL 367 6 2 4 3.6 CCc1ccc(C(=O)Nc2cc(C(=O)O)nn2Cc2ccc(F)cc2)cc1 10.1021/acs.jmedchem.2c01632
CHEMBL5189241 197973 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assayAntagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assay
ChEMBL 367 6 2 4 3.6 CCc1ccc(C(=O)Nc2cc(C(=O)O)nn2Cc2ccc(F)cc2)cc1 10.1021/acs.jmedchem.2c01632
168286955 198145 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assayAntagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assay
ChEMBL 360 5 2 5 3.1 Cc1ccc(C(=O)Nc2cc(C(=O)O)nn2Cc2ccc(C#N)cc2)cc1 10.1021/acs.jmedchem.2c01632
CHEMBL5192153 198145 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assayAntagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assay
ChEMBL 360 5 2 5 3.1 Cc1ccc(C(=O)Nc2cc(C(=O)O)nn2Cc2ccc(C#N)cc2)cc1 10.1021/acs.jmedchem.2c01632
153526201 198224 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human P2Y14R expressed in human HEK293 cells assessed as inhibition of cAMP level incubated for 30 mins by cAMP-glo assayAntagonist activity at human P2Y14R expressed in human HEK293 cells assessed as inhibition of cAMP level incubated for 30 mins by cAMP-glo assay
ChEMBL 412 5 1 4 5.6 O=C(Cc1ccc(OC(F)(F)F)cc1)Nc1cccc(-c2nc3ccccc3o2)c1 10.1016/j.ejmech.2021.113933
CHEMBL5193065 198224 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human P2Y14R expressed in human HEK293 cells assessed as inhibition of cAMP level incubated for 30 mins by cAMP-glo assayAntagonist activity at human P2Y14R expressed in human HEK293 cells assessed as inhibition of cAMP level incubated for 30 mins by cAMP-glo assay
ChEMBL 412 5 1 4 5.6 O=C(Cc1ccc(OC(F)(F)F)cc1)Nc1cccc(-c2nc3ccccc3o2)c1 10.1016/j.ejmech.2021.113933
168278836 197674 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assayAntagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assay
ChEMBL 403 5 2 4 4.2 Cc1ccc(C(=O)Nc2cc(C(=O)O)nn2Cc2ccccc2C(F)(F)F)cc1 10.1021/acs.jmedchem.2c01632
CHEMBL5185002 197674 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assayAntagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assay
ChEMBL 403 5 2 4 4.2 Cc1ccc(C(=O)Nc2cc(C(=O)O)nn2Cc2ccccc2C(F)(F)F)cc1 10.1021/acs.jmedchem.2c01632
164611926 191960 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at P2Y14 (unknown origin) expressed in HEK293 cells assessed as reduction in cAMP production incubated for 30 mins by ADP-glo assayAntagonist activity at P2Y14 (unknown origin) expressed in HEK293 cells assessed as reduction in cAMP production incubated for 30 mins by ADP-glo assay
ChEMBL 331 4 2 2 4.6 Cc1ccc(C(=O)Nc2cc(C(=O)O)cc(-c3ccccc3)c2)cc1 10.1016/j.ejmech.2021.113313
CHEMBL4857372 191960 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at P2Y14 (unknown origin) expressed in HEK293 cells assessed as reduction in cAMP production incubated for 30 mins by ADP-glo assayAntagonist activity at P2Y14 (unknown origin) expressed in HEK293 cells assessed as reduction in cAMP production incubated for 30 mins by ADP-glo assay
ChEMBL 331 4 2 2 4.6 Cc1ccc(C(=O)Nc2cc(C(=O)O)cc(-c3ccccc3)c2)cc1 10.1016/j.ejmech.2021.113313
155526332 177951 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human P2Y14R stably expressed in human forskolin treated THP1 cells assessed as reduction in P2Y14R agonist UDPG-induced inhibition of cAMP production incubated for 15 mins by competitive enzyme-linked immunoassayAntagonist activity at human P2Y14R stably expressed in human forskolin treated THP1 cells assessed as reduction in P2Y14R agonist UDPG-induced inhibition of cAMP production incubated for 15 mins by competitive enzyme-linked immunoassay
ChEMBL 400 5 3 3 4.8 O=C(O)c1cc(NC(=O)c2ccccc2)cc(-c2ccc(C3CCNCC3)cc2)c1 10.1016/j.ejmech.2019.111564
CHEMBL4458922 177951 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human P2Y14R stably expressed in human forskolin treated THP1 cells assessed as reduction in P2Y14R agonist UDPG-induced inhibition of cAMP production incubated for 15 mins by competitive enzyme-linked immunoassayAntagonist activity at human P2Y14R stably expressed in human forskolin treated THP1 cells assessed as reduction in P2Y14R agonist UDPG-induced inhibition of cAMP production incubated for 15 mins by competitive enzyme-linked immunoassay
ChEMBL 400 5 3 3 4.8 O=C(O)c1cc(NC(=O)c2ccccc2)cc(-c2ccc(C3CCNCC3)cc2)c1 10.1016/j.ejmech.2019.111564
168297588 199036 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assayAntagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assay
ChEMBL 371 5 2 4 3.5 Cc1ccc(C(=O)Nc2cc(C(=O)O)nn2Cc2cc(F)cc(F)c2)cc1 10.1021/acs.jmedchem.2c01632
CHEMBL5205552 199036 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assayAntagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assay
ChEMBL 371 5 2 4 3.5 Cc1ccc(C(=O)Nc2cc(C(=O)O)nn2Cc2cc(F)cc(F)c2)cc1 10.1021/acs.jmedchem.2c01632
153523840 198621 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human P2Y14R expressed in human HEK293 cells assessed as inhibition of cAMP level incubated for 30 mins by cAMP-glo assayAntagonist activity at human P2Y14R expressed in human HEK293 cells assessed as inhibition of cAMP level incubated for 30 mins by cAMP-glo assay
ChEMBL 341 4 1 2 5.6 Cc1ccc(CC(=O)Nc2ccc(-c3cc4ccccc4o3)cc2)cc1 10.1016/j.ejmech.2021.113933
CHEMBL5198960 198621 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human P2Y14R expressed in human HEK293 cells assessed as inhibition of cAMP level incubated for 30 mins by cAMP-glo assayAntagonist activity at human P2Y14R expressed in human HEK293 cells assessed as inhibition of cAMP level incubated for 30 mins by cAMP-glo assay
ChEMBL 341 4 1 2 5.6 Cc1ccc(CC(=O)Nc2ccc(-c3cc4ccccc4o3)cc2)cc1 10.1016/j.ejmech.2021.113933
54580547 68393 0 None - 1 Mouse 6.4 pIC50 = 6.4 Functional
Antagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assayAntagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assay
ChEMBL 465 5 1 5 5.5 CCOc1cccc(NC(=O)N2CCc3nc(-c4cccnc4)nc(-c4ccccc4C)c3C2)c1 10.1016/j.bmcl.2011.03.084
CHEMBL1771235 68393 0 None - 1 Mouse 6.4 pIC50 = 6.4 Functional
Antagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assayAntagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assay
ChEMBL 465 5 1 5 5.5 CCOc1cccc(NC(=O)N2CCc3nc(-c4cccnc4)nc(-c4ccccc4C)c3C2)c1 10.1016/j.bmcl.2011.03.084
54586410 68406 0 None - 1 Mouse 6.4 pIC50 = 6.4 Functional
Antagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assayAntagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assay
ChEMBL 469 4 1 4 6.0 CCc1cccc(NC(=O)N2CCc3nc(-c4cccnc4)nc(-c4ccccc4Cl)c3C2)c1 10.1016/j.bmcl.2011.03.084
CHEMBL1771247 68406 0 None - 1 Mouse 6.4 pIC50 = 6.4 Functional
Antagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assayAntagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assay
ChEMBL 469 4 1 4 6.0 CCc1cccc(NC(=O)N2CCc3nc(-c4cccnc4)nc(-c4ccccc4Cl)c3C2)c1 10.1016/j.bmcl.2011.03.084
54585441 68389 0 None - 1 Mouse 5.3 pIC50 = 5.3 Functional
Antagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assayAntagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assay
ChEMBL 421 3 1 4 5.1 Cc1ccccc1-c1nc(-c2cccnc2)nc2c1CN(C(=O)Nc1ccccc1)CC2 10.1016/j.bmcl.2011.03.084
CHEMBL1771230 68389 0 None - 1 Mouse 5.3 pIC50 = 5.3 Functional
Antagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assayAntagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assay
ChEMBL 421 3 1 4 5.1 Cc1ccccc1-c1nc(-c2cccnc2)nc2c1CN(C(=O)Nc1ccccc1)CC2 10.1016/j.bmcl.2011.03.084
54581993 68829 0 None - 1 Mouse 5.3 pIC50 = 5.3 Functional
Antagonist activity at mouse P2Y14 receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAntagonist activity at mouse P2Y14 receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 340 4 1 2 6.0 O=C(O)c1cc(-c2ccccc2)c2ccc(Oc3ccccc3)cc2c1 10.1016/j.bmcl.2011.03.081
CHEMBL1774884 68829 0 None - 1 Mouse 5.3 pIC50 = 5.3 Functional
Antagonist activity at mouse P2Y14 receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAntagonist activity at mouse P2Y14 receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 340 4 1 2 6.0 O=C(O)c1cc(-c2ccccc2)c2ccc(Oc3ccccc3)cc2c1 10.1016/j.bmcl.2011.03.081
168285071 198373 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assayAntagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assay
ChEMBL 380 6 2 6 3.1 Cc1ccc(C(=O)Nc2cc(C(=O)O)nn2Cc2ccc([N+](=O)[O-])cc2)cc1 10.1021/acs.jmedchem.2c01632
CHEMBL5195243 198373 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assayAntagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assay
ChEMBL 380 6 2 6 3.1 Cc1ccc(C(=O)Nc2cc(C(=O)O)nn2Cc2ccc([N+](=O)[O-])cc2)cc1 10.1021/acs.jmedchem.2c01632
155544120 180116 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human P2Y14R stably expressed in human forskolin treated THP1 cells assessed as reduction in P2Y14R agonist UDPG-induced inhibition of cAMP production incubated for 15 mins by competitive enzyme-linked immunoassayAntagonist activity at human P2Y14R stably expressed in human forskolin treated THP1 cells assessed as reduction in P2Y14R agonist UDPG-induced inhibition of cAMP production incubated for 15 mins by competitive enzyme-linked immunoassay
ChEMBL 445 6 3 5 4.7 O=C(O)c1cc(NC(=O)c2ccc([N+](=O)[O-])cc2)cc(-c2ccc(C3CCNCC3)cc2)c1 10.1016/j.ejmech.2019.111564
CHEMBL4526840 180116 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human P2Y14R stably expressed in human forskolin treated THP1 cells assessed as reduction in P2Y14R agonist UDPG-induced inhibition of cAMP production incubated for 15 mins by competitive enzyme-linked immunoassayAntagonist activity at human P2Y14R stably expressed in human forskolin treated THP1 cells assessed as reduction in P2Y14R agonist UDPG-induced inhibition of cAMP production incubated for 15 mins by competitive enzyme-linked immunoassay
ChEMBL 445 6 3 5 4.7 O=C(O)c1cc(NC(=O)c2ccc([N+](=O)[O-])cc2)cc(-c2ccc(C3CCNCC3)cc2)c1 10.1016/j.ejmech.2019.111564
168293652 198938 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assayAntagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assay
ChEMBL 353 5 2 4 3.3 Cc1ccc(C(=O)Nc2cc(C(=O)O)nn2Cc2cccc(F)c2)cc1 10.1021/acs.jmedchem.2c01632
CHEMBL5203936 198938 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assayAntagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assay
ChEMBL 353 5 2 4 3.3 Cc1ccc(C(=O)Nc2cc(C(=O)O)nn2Cc2cccc(F)c2)cc1 10.1021/acs.jmedchem.2c01632
168274334 197483 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assayAntagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assay
ChEMBL 363 5 2 4 3.8 Cc1ccc(C(=O)Nc2cc(C(=O)O)nn2Cc2cc(C)cc(C)c2)cc1 10.1021/acs.jmedchem.2c01632
CHEMBL5182261 197483 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assayAntagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assay
ChEMBL 363 5 2 4 3.8 Cc1ccc(C(=O)Nc2cc(C(=O)O)nn2Cc2cc(C)cc(C)c2)cc1 10.1021/acs.jmedchem.2c01632
54582584 68441 0 None - 1 Mouse 7.3 pIC50 = 7.3 Functional
Antagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assayAntagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assay
ChEMBL 483 4 1 4 6.3 CCc1cccc(NC(=O)N2CCc3nc(-c4cccnc4)nc(-c4c(C)cccc4Cl)c3C2)c1 10.1016/j.bmcl.2011.03.084
CHEMBL1771440 68441 0 None - 1 Mouse 7.3 pIC50 = 7.3 Functional
Antagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assayAntagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assay
ChEMBL 483 4 1 4 6.3 CCc1cccc(NC(=O)N2CCc3nc(-c4cccnc4)nc(-c4c(C)cccc4Cl)c3C2)c1 10.1016/j.bmcl.2011.03.084
54580587 68442 0 None - 1 Mouse 7.3 pIC50 = 7.3 Functional
Antagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assayAntagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assay
ChEMBL 503 4 1 4 6.7 CCc1cccc(NC(=O)N2CCc3nc(-c4cccnc4)nc(-c4c(Cl)cccc4Cl)c3C2)c1 10.1016/j.bmcl.2011.03.084
CHEMBL1771441 68442 0 None - 1 Mouse 7.3 pIC50 = 7.3 Functional
Antagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assayAntagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assay
ChEMBL 503 4 1 4 6.7 CCc1cccc(NC(=O)N2CCc3nc(-c4cccnc4)nc(-c4c(Cl)cccc4Cl)c3C2)c1 10.1016/j.bmcl.2011.03.084
54581995 68846 0 None - 1 Mouse 7.3 pIC50 = 7.3 Functional
Antagonist activity at mouse P2Y14 receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAntagonist activity at mouse P2Y14 receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 490 4 2 2 7.5 O=C(O)c1cc(-c2ccc([C@H](O)C(F)(F)F)cc2)c2ccc(-c3ccc(C(F)(F)F)cc3)cc2c1 10.1016/j.bmcl.2011.03.081
CHEMBL1774902 68846 0 None - 1 Mouse 7.3 pIC50 = 7.3 Functional
Antagonist activity at mouse P2Y14 receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAntagonist activity at mouse P2Y14 receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 490 4 2 2 7.5 O=C(O)c1cc(-c2ccc([C@H](O)C(F)(F)F)cc2)c2ccc(-c3ccc(C(F)(F)F)cc3)cc2c1 10.1016/j.bmcl.2011.03.081
54582545 68392 0 None - 1 Mouse 5.3 pIC50 = 5.3 Functional
Antagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assayAntagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assay
ChEMBL 451 4 1 5 5.1 COc1cccc(NC(=O)N2CCc3nc(-c4cccnc4)nc(-c4ccccc4C)c3C2)c1 10.1016/j.bmcl.2011.03.084
CHEMBL1771234 68392 0 None - 1 Mouse 5.3 pIC50 = 5.3 Functional
Antagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assayAntagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assay
ChEMBL 451 4 1 5 5.1 COc1cccc(NC(=O)N2CCc3nc(-c4cccnc4)nc(-c4ccccc4C)c3C2)c1 10.1016/j.bmcl.2011.03.084
168296742 199051 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assayAntagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assay
ChEMBL 349 5 2 4 3.5 Cc1ccc(C(=O)Nc2cc(C(=O)O)nn2Cc2ccccc2C)cc1 10.1021/acs.jmedchem.2c01632
CHEMBL5205688 199051 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assayAntagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assay
ChEMBL 349 5 2 4 3.5 Cc1ccc(C(=O)Nc2cc(C(=O)O)nn2Cc2ccccc2C)cc1 10.1021/acs.jmedchem.2c01632
42630806 68837 0 None - 1 Mouse 7.3 pIC50 = 7.3 Functional
Antagonist activity at mouse P2Y14 receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAntagonist activity at mouse P2Y14 receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 414 4 1 3 6.8 O=C(O)c1cc(-c2ccsc2)c2ccc(-c3ccc(OC(F)(F)F)cc3)cc2c1 10.1016/j.bmcl.2011.03.081
CHEMBL1774893 68837 0 None - 1 Mouse 7.3 pIC50 = 7.3 Functional
Antagonist activity at mouse P2Y14 receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAntagonist activity at mouse P2Y14 receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 414 4 1 3 6.8 O=C(O)c1cc(-c2ccsc2)c2ccc(-c3ccc(OC(F)(F)F)cc3)cc2c1 10.1016/j.bmcl.2011.03.081
126720243 177695 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human P2Y14R expressed in CHO cells assessed as inhibition of UDPG-mediated reduction of forskolin-induced cAMP production after 15 mins by by competitive enzyme-linked immunoassayAntagonist activity at human P2Y14R expressed in CHO cells assessed as inhibition of UDPG-mediated reduction of forskolin-induced cAMP production after 15 mins by by competitive enzyme-linked immunoassay
ChEMBL 449 3 2 2 5.9 O=C(O)c1cc(C#Cc2ccc(C(F)(F)F)cc2)cc(-c2ccc(C3CCNCC3)cc2)c1 10.1021/acs.jmedchem.6b00044
CHEMBL4455037 177695 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human P2Y14R expressed in CHO cells assessed as inhibition of UDPG-mediated reduction of forskolin-induced cAMP production after 15 mins by by competitive enzyme-linked immunoassayAntagonist activity at human P2Y14R expressed in CHO cells assessed as inhibition of UDPG-mediated reduction of forskolin-induced cAMP production after 15 mins by by competitive enzyme-linked immunoassay
ChEMBL 449 3 2 2 5.9 O=C(O)c1cc(C#Cc2ccc(C(F)(F)F)cc2)cc(-c2ccc(C3CCNCC3)cc2)c1 10.1021/acs.jmedchem.6b00044
54587430 68390 0 None - 1 Mouse 6.2 pIC50 = 6.2 Functional
Antagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assayAntagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assay
ChEMBL 455 3 1 4 5.8 Cc1ccccc1-c1nc(-c2cccnc2)nc2c1CN(C(=O)Nc1cccc(Cl)c1)CC2 10.1016/j.bmcl.2011.03.084
CHEMBL1771232 68390 0 None - 1 Mouse 6.2 pIC50 = 6.2 Functional
Antagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assayAntagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assay
ChEMBL 455 3 1 4 5.8 Cc1ccccc1-c1nc(-c2cccnc2)nc2c1CN(C(=O)Nc1cccc(Cl)c1)CC2 10.1016/j.bmcl.2011.03.084
54583514 68391 0 None - 1 Mouse 5.2 pIC50 = 5.2 Functional
Antagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assayAntagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assay
ChEMBL 455 3 1 4 5.8 Cc1ccccc1-c1nc(-c2cccnc2)nc2c1CN(C(=O)Nc1ccc(Cl)cc1)CC2 10.1016/j.bmcl.2011.03.084
CHEMBL1771233 68391 0 None - 1 Mouse 5.2 pIC50 = 5.2 Functional
Antagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assayAntagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assay
ChEMBL 455 3 1 4 5.8 Cc1ccccc1-c1nc(-c2cccnc2)nc2c1CN(C(=O)Nc1ccc(Cl)cc1)CC2 10.1016/j.bmcl.2011.03.084
153526173 197993 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human P2Y14R expressed in human HEK293 cells assessed as inhibition of cAMP level incubated for 30 mins by cAMP-glo assayAntagonist activity at human P2Y14R expressed in human HEK293 cells assessed as inhibition of cAMP level incubated for 30 mins by cAMP-glo assay
ChEMBL 430 4 1 3 6.3 O=C(Cc1ccc(C(F)(F)F)cc1)Nc1cccc(-c2nc3cc(Cl)ccc3o2)c1 10.1016/j.ejmech.2021.113933
CHEMBL5189611 197993 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human P2Y14R expressed in human HEK293 cells assessed as inhibition of cAMP level incubated for 30 mins by cAMP-glo assayAntagonist activity at human P2Y14R expressed in human HEK293 cells assessed as inhibition of cAMP level incubated for 30 mins by cAMP-glo assay
ChEMBL 430 4 1 3 6.3 O=C(Cc1ccc(C(F)(F)F)cc1)Nc1cccc(-c2nc3cc(Cl)ccc3o2)c1 10.1016/j.ejmech.2021.113933
153526188 197014 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human P2Y14R expressed in human HEK293 cells assessed as inhibition of cAMP level incubated for 30 mins by cAMP-glo assayAntagonist activity at human P2Y14R expressed in human HEK293 cells assessed as inhibition of cAMP level incubated for 30 mins by cAMP-glo assay
ChEMBL 376 4 1 3 5.6 Cc1ccc(CC(=O)Nc2cccc(-c3nc4cc(Cl)ccc4o3)c2)cc1 10.1016/j.ejmech.2021.113933
CHEMBL5175004 197014 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human P2Y14R expressed in human HEK293 cells assessed as inhibition of cAMP level incubated for 30 mins by cAMP-glo assayAntagonist activity at human P2Y14R expressed in human HEK293 cells assessed as inhibition of cAMP level incubated for 30 mins by cAMP-glo assay
ChEMBL 376 4 1 3 5.6 Cc1ccc(CC(=O)Nc2cccc(-c3nc4cc(Cl)ccc4o3)c2)cc1 10.1016/j.ejmech.2021.113933
168293347 198925 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assayAntagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assay
ChEMBL 365 6 2 5 3.2 COc1cccc(Cn2nc(C(=O)O)cc2NC(=O)c2ccc(C)cc2)c1 10.1021/acs.jmedchem.2c01632
CHEMBL5203764 198925 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assayAntagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assay
ChEMBL 365 6 2 5 3.2 COc1cccc(Cn2nc(C(=O)O)cc2NC(=O)c2ccc(C)cc2)c1 10.1021/acs.jmedchem.2c01632
54583557 68446 0 None - 1 Mouse 7.2 pIC50 = 7.2 Functional
Antagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assayAntagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assay
ChEMBL 462 4 1 3 6.6 CCc1cccc(NC(=O)N2CCc3nc(-c4ccc(C)cc4)nc(-c4ccccc4C)c3C2)c1 10.1016/j.bmcl.2011.03.084
CHEMBL1771446 68446 0 None - 1 Mouse 7.2 pIC50 = 7.2 Functional
Antagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assayAntagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assay
ChEMBL 462 4 1 3 6.6 CCc1cccc(NC(=O)N2CCc3nc(-c4ccc(C)cc4)nc(-c4ccccc4C)c3C2)c1 10.1016/j.bmcl.2011.03.084
54582546 68404 0 None - 1 Mouse 6.2 pIC50 = 6.2 Functional
Antagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assayAntagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assay
ChEMBL 485 4 1 4 6.2 Cc1ccccc1-c1nc(-c2cccnc2)nc2c1CN(C(=O)Nc1cccc(C(C)(F)F)c1)CC2 10.1016/j.bmcl.2011.03.084
CHEMBL1771245 68404 0 None - 1 Mouse 6.2 pIC50 = 6.2 Functional
Antagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assayAntagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assay
ChEMBL 485 4 1 4 6.2 Cc1ccccc1-c1nc(-c2cccnc2)nc2c1CN(C(=O)Nc1cccc(C(C)(F)F)c1)CC2 10.1016/j.bmcl.2011.03.084
54583515 68394 0 None - 1 Mouse 6.2 pIC50 = 6.2 Functional
Antagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assayAntagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assay
ChEMBL 467 4 1 5 5.8 CSc1cccc(NC(=O)N2CCc3nc(-c4cccnc4)nc(-c4ccccc4C)c3C2)c1 10.1016/j.bmcl.2011.03.084
CHEMBL1771236 68394 0 None - 1 Mouse 6.2 pIC50 = 6.2 Functional
Antagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assayAntagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assay
ChEMBL 467 4 1 5 5.8 CSc1cccc(NC(=O)N2CCc3nc(-c4cccnc4)nc(-c4ccccc4C)c3C2)c1 10.1016/j.bmcl.2011.03.084
54586409 68401 0 None - 1 Mouse 5.2 pIC50 = 5.2 Functional
Antagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assayAntagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assay
ChEMBL 463 4 1 5 5.3 CC(=O)c1cccc(NC(=O)N2CCc3nc(-c4cccnc4)nc(-c4ccccc4C)c3C2)c1 10.1016/j.bmcl.2011.03.084
CHEMBL1771242 68401 0 None - 1 Mouse 5.2 pIC50 = 5.2 Functional
Antagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assayAntagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assay
ChEMBL 463 4 1 5 5.3 CC(=O)c1cccc(NC(=O)N2CCc3nc(-c4cccnc4)nc(-c4ccccc4C)c3C2)c1 10.1016/j.bmcl.2011.03.084
136088963 68438 0 None - 1 Mouse 5.2 pIC50 = 5.2 Functional
Antagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assayAntagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assay
ChEMBL 451 4 2 5 5.1 CCc1cccc(NC(=O)N2CCc3nc(-c4cccnc4)nc(-c4ccccc4O)c3C2)c1 10.1016/j.bmcl.2011.03.084
CHEMBL1771437 68438 0 None - 1 Mouse 5.2 pIC50 = 5.2 Functional
Antagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assayAntagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assay
ChEMBL 451 4 2 5 5.1 CCc1cccc(NC(=O)N2CCc3nc(-c4cccnc4)nc(-c4ccccc4O)c3C2)c1 10.1016/j.bmcl.2011.03.084
168278286 197903 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assayAntagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assay
ChEMBL 377 6 2 5 3.4 CC(=O)c1ccc(Cn2nc(C(=O)O)cc2NC(=O)c2ccc(C)cc2)cc1 10.1021/acs.jmedchem.2c01632
CHEMBL5188038 197903 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assayAntagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assay
ChEMBL 377 6 2 5 3.4 CC(=O)c1ccc(Cn2nc(C(=O)O)cc2NC(=O)c2ccc(C)cc2)cc1 10.1021/acs.jmedchem.2c01632
168295924 199216 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assayAntagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assay
ChEMBL 369 5 2 4 3.8 Cc1ccc(C(=O)Nc2cc(C(=O)O)nn2Cc2ccc(Cl)cc2)cc1 10.1021/acs.jmedchem.2c01632
CHEMBL5208342 199216 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assayAntagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assay
ChEMBL 369 5 2 4 3.8 Cc1ccc(C(=O)Nc2cc(C(=O)O)nn2Cc2ccc(Cl)cc2)cc1 10.1021/acs.jmedchem.2c01632
54585445 68409 0 None - 1 Mouse 5.2 pIC50 = 5.2 Functional
Antagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assayAntagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assay
ChEMBL 483 4 1 4 6.3 CCc1cccc(NC(=O)N2CCc3nc(-c4cccnc4)nc(-c4ccc(Cl)cc4C)c3C2)c1 10.1016/j.bmcl.2011.03.084
CHEMBL1771250 68409 0 None - 1 Mouse 5.2 pIC50 = 5.2 Functional
Antagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assayAntagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assay
ChEMBL 483 4 1 4 6.3 CCc1cccc(NC(=O)N2CCc3nc(-c4cccnc4)nc(-c4ccc(Cl)cc4C)c3C2)c1 10.1016/j.bmcl.2011.03.084
54582586 68448 0 None - 1 Mouse 5.1 pIC50 = 5.1 Functional
Antagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assayAntagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assay
ChEMBL 516 4 1 3 7.3 CCc1cccc(NC(=O)N2CCc3nc(-c4ccc(C(F)(F)F)cc4)nc(-c4ccccc4C)c3C2)c1 10.1016/j.bmcl.2011.03.084
CHEMBL1771449 68448 0 None - 1 Mouse 5.1 pIC50 = 5.1 Functional
Antagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assayAntagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assay
ChEMBL 516 4 1 3 7.3 CCc1cccc(NC(=O)N2CCc3nc(-c4ccc(C(F)(F)F)cc4)nc(-c4ccccc4C)c3C2)c1 10.1016/j.bmcl.2011.03.084
42630568 68847 0 None - 1 Mouse 8.1 pIC50 = 8.1 Functional
Antagonist activity at mouse P2Y14 receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAntagonist activity at mouse P2Y14 receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 472 5 2 2 7.2 O=C(O)c1cc(-c2ccc([C@@H](O)C(F)F)cc2)c2ccc(-c3ccc(C(F)(F)F)cc3)cc2c1 10.1016/j.bmcl.2011.03.081
CHEMBL1774903 68847 0 None - 1 Mouse 8.1 pIC50 = 8.1 Functional
Antagonist activity at mouse P2Y14 receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assayAntagonist activity at mouse P2Y14 receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay
ChEMBL 472 5 2 2 7.2 O=C(O)c1cc(-c2ccc([C@@H](O)C(F)F)cc2)c2ccc(-c3ccc(C(F)(F)F)cc3)cc2c1 10.1016/j.bmcl.2011.03.081
41616259 198129 2 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human P2Y14R expressed in human HEK293 cells assessed as inhibition of cAMP level incubated for 30 mins by cAMP-glo assayAntagonist activity at human P2Y14R expressed in human HEK293 cells assessed as inhibition of cAMP level incubated for 30 mins by cAMP-glo assay
ChEMBL 342 4 1 3 5.0 Cc1ccc(CC(=O)Nc2cccc(-c3nc4ccccc4o3)c2)cc1 10.1016/j.ejmech.2021.113933
CHEMBL5191983 198129 2 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human P2Y14R expressed in human HEK293 cells assessed as inhibition of cAMP level incubated for 30 mins by cAMP-glo assayAntagonist activity at human P2Y14R expressed in human HEK293 cells assessed as inhibition of cAMP level incubated for 30 mins by cAMP-glo assay
ChEMBL 342 4 1 3 5.0 Cc1ccc(CC(=O)Nc2cccc(-c3nc4ccccc4o3)c2)cc1 10.1016/j.ejmech.2021.113933
54581547 68396 0 None - 1 Mouse 7.1 pIC50 = 7.1 Functional
Antagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assayAntagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assay
ChEMBL 449 4 1 4 5.7 CCc1cccc(NC(=O)N2CCc3nc(-c4cccnc4)nc(-c4ccccc4C)c3C2)c1 10.1016/j.bmcl.2011.03.084
CHEMBL1771238 68396 0 None - 1 Mouse 7.1 pIC50 = 7.1 Functional
Antagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assayAntagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assay
ChEMBL 449 4 1 4 5.7 CCc1cccc(NC(=O)N2CCc3nc(-c4cccnc4)nc(-c4ccccc4C)c3C2)c1 10.1016/j.bmcl.2011.03.084
54585442 68402 0 None - 1 Mouse 5.1 pIC50 = 5.1 Functional
Antagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assayAntagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assay
ChEMBL 465 4 2 5 5.2 Cc1ccccc1-c1nc(-c2cccnc2)nc2c1CN(C(=O)Nc1cccc(C(C)O)c1)CC2 10.1016/j.bmcl.2011.03.084
CHEMBL1771243 68402 0 None - 1 Mouse 5.1 pIC50 = 5.1 Functional
Antagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assayAntagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assay
ChEMBL 465 4 2 5 5.2 Cc1ccccc1-c1nc(-c2cccnc2)nc2c1CN(C(=O)Nc1cccc(C(C)O)c1)CC2 10.1016/j.bmcl.2011.03.084
54582585 68445 0 None - 1 Mouse 7.1 pIC50 = 7.1 Functional
Antagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assayAntagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assay
ChEMBL 448 4 1 3 6.3 CCc1cccc(NC(=O)N2CCc3nc(-c4ccccc4)nc(-c4ccccc4C)c3C2)c1 10.1016/j.bmcl.2011.03.084
CHEMBL1771445 68445 0 None - 1 Mouse 7.1 pIC50 = 7.1 Functional
Antagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assayAntagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assay
ChEMBL 448 4 1 3 6.3 CCc1cccc(NC(=O)N2CCc3nc(-c4ccccc4)nc(-c4ccccc4C)c3C2)c1 10.1016/j.bmcl.2011.03.084
54580589 68453 0 None - 1 Mouse 6.1 pIC50 = 6.1 Functional
Antagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assayAntagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assay
ChEMBL 498 4 1 3 7.4 CCc1cccc(NC(=O)N2CCc3nc(-c4ccc5ccccc5c4)nc(-c4ccccc4C)c3C2)c1 10.1016/j.bmcl.2011.03.084
CHEMBL1771454 68453 0 None - 1 Mouse 6.1 pIC50 = 6.1 Functional
Antagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assayAntagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assay
ChEMBL 498 4 1 3 7.4 CCc1cccc(NC(=O)N2CCc3nc(-c4ccc5ccccc5c4)nc(-c4ccccc4C)c3C2)c1 10.1016/j.bmcl.2011.03.084
54586443 68440 0 None - 1 Mouse 8.1 pIC50 = 8.1 Functional
Antagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assayAntagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assay
ChEMBL 463 4 1 4 6.0 CCc1cccc(NC(=O)N2CCc3nc(-c4cccnc4)nc(-c4c(C)cccc4C)c3C2)c1 10.1016/j.bmcl.2011.03.084
CHEMBL1771439 68440 0 None - 1 Mouse 8.1 pIC50 = 8.1 Functional
Antagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assayAntagonist activity at mouse P2Y14 expressed in human HEK cells coexpressing Galphai5 assessed as inhibition of UDP-glucose stimulated calcium release by FLIPR assay
ChEMBL 463 4 1 4 6.0 CCc1cccc(NC(=O)N2CCc3nc(-c4cccnc4)nc(-c4c(C)cccc4C)c3C2)c1 10.1016/j.bmcl.2011.03.084
2972254 196850 9 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human P2Y14R expressed in human HEK293 cells assessed as inhibition of cAMP level incubated for 30 mins by cAMP-glo assayAntagonist activity at human P2Y14R expressed in human HEK293 cells assessed as inhibition of cAMP level incubated for 30 mins by cAMP-glo assay
ChEMBL 392 5 1 4 5.3 COc1ccc(CC(=O)Nc2cccc(-c3nc4cc(Cl)ccc4o3)c2)cc1 10.1016/j.ejmech.2021.113933
CHEMBL5172530 196850 9 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human P2Y14R expressed in human HEK293 cells assessed as inhibition of cAMP level incubated for 30 mins by cAMP-glo assayAntagonist activity at human P2Y14R expressed in human HEK293 cells assessed as inhibition of cAMP level incubated for 30 mins by cAMP-glo assay
ChEMBL 392 5 1 4 5.3 COc1ccc(CC(=O)Nc2cccc(-c3nc4cc(Cl)ccc4o3)c2)cc1 10.1016/j.ejmech.2021.113933
153526185 199005 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human P2Y14R expressed in human HEK293 cells assessed as inhibition of cAMP level incubated for 30 mins by cAMP-glo assayAntagonist activity at human P2Y14R expressed in human HEK293 cells assessed as inhibition of cAMP level incubated for 30 mins by cAMP-glo assay
ChEMBL 342 4 1 3 5.0 Cc1ccccc1CC(=O)Nc1cccc(-c2nc3ccccc3o2)c1 10.1016/j.ejmech.2021.113933
CHEMBL5204942 199005 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human P2Y14R expressed in human HEK293 cells assessed as inhibition of cAMP level incubated for 30 mins by cAMP-glo assayAntagonist activity at human P2Y14R expressed in human HEK293 cells assessed as inhibition of cAMP level incubated for 30 mins by cAMP-glo assay
ChEMBL 342 4 1 3 5.0 Cc1ccccc1CC(=O)Nc1cccc(-c2nc3ccccc3o2)c1 10.1016/j.ejmech.2021.113933
168271452 197386 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human P2Y14R expressed in human HEK293 cells assessed as inhibition of cAMP level incubated for 30 mins by cAMP-glo assayAntagonist activity at human P2Y14R expressed in human HEK293 cells assessed as inhibition of cAMP level incubated for 30 mins by cAMP-glo assay
ChEMBL 390 4 1 3 5.9 Cc1cccc(CC(=O)Nc2cc(C)cc(-c3nc4cc(Cl)ccc4o3)c2)c1 10.1016/j.ejmech.2021.113933
CHEMBL5180780 197386 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human P2Y14R expressed in human HEK293 cells assessed as inhibition of cAMP level incubated for 30 mins by cAMP-glo assayAntagonist activity at human P2Y14R expressed in human HEK293 cells assessed as inhibition of cAMP level incubated for 30 mins by cAMP-glo assay
ChEMBL 390 4 1 3 5.9 Cc1cccc(CC(=O)Nc2cc(C)cc(-c3nc4cc(Cl)ccc4o3)c2)c1 10.1016/j.ejmech.2021.113933
164621154 192857 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at P2Y14 (unknown origin) expressed in HEK293 cells assessed as reduction in cAMP production incubated for 30 mins by ADP-glo assayAntagonist activity at P2Y14 (unknown origin) expressed in HEK293 cells assessed as reduction in cAMP production incubated for 30 mins by ADP-glo assay
ChEMBL 337 4 2 3 4.7 Cc1ccc(C(=O)Nc2cc(C(=O)O)cc(-c3ccsc3)c2)cc1 10.1016/j.ejmech.2021.113313
CHEMBL4871413 192857 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at P2Y14 (unknown origin) expressed in HEK293 cells assessed as reduction in cAMP production incubated for 30 mins by ADP-glo assayAntagonist activity at P2Y14 (unknown origin) expressed in HEK293 cells assessed as reduction in cAMP production incubated for 30 mins by ADP-glo assay
ChEMBL 337 4 2 3 4.7 Cc1ccc(C(=O)Nc2cc(C(=O)O)cc(-c3ccsc3)c2)cc1 10.1016/j.ejmech.2021.113313
153526180 197748 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human P2Y14R expressed in human HEK293 cells assessed as inhibition of cAMP level incubated for 30 mins by cAMP-glo assayAntagonist activity at human P2Y14R expressed in human HEK293 cells assessed as inhibition of cAMP level incubated for 30 mins by cAMP-glo assay
ChEMBL 446 5 1 4 6.2 O=C(Cc1ccc(OC(F)(F)F)cc1)Nc1cccc(-c2nc3cc(Cl)ccc3o2)c1 10.1016/j.ejmech.2021.113933
CHEMBL5186024 197748 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human P2Y14R expressed in human HEK293 cells assessed as inhibition of cAMP level incubated for 30 mins by cAMP-glo assayAntagonist activity at human P2Y14R expressed in human HEK293 cells assessed as inhibition of cAMP level incubated for 30 mins by cAMP-glo assay
ChEMBL 446 5 1 4 6.2 O=C(Cc1ccc(OC(F)(F)F)cc1)Nc1cccc(-c2nc3cc(Cl)ccc3o2)c1 10.1016/j.ejmech.2021.113933
168296672 199302 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assayAntagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assay
ChEMBL 327 5 2 4 3.3 Cc1ccc(C(=O)Nc2cc(C(=O)O)nn2CC2CCCC2)cc1 10.1021/acs.jmedchem.2c01632
CHEMBL5209515 199302 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assayAntagonist activity at P2Y14R (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated in presence of IBMX by cAMP-glo assay
ChEMBL 327 5 2 4 3.3 Cc1ccc(C(=O)Nc2cc(C(=O)O)nn2CC2CCCC2)cc1 10.1021/acs.jmedchem.2c01632
124221650 9445 0 None - 0 Human 10.1 pKi = 10.1 Functional
Antagonist activity at human P2Y14R expressed in CHO cells assessed as inhibition of UDPG-mediated reduction of forskolin-induced [3H]cAMP production measured after 15 mins in presence of phosphodiesterase inhibitor IBMX by chromatographic methodAntagonist activity at human P2Y14R expressed in CHO cells assessed as inhibition of UDPG-mediated reduction of forskolin-induced [3H]cAMP production measured after 15 mins in presence of phosphodiesterase inhibitor IBMX by chromatographic method
ChEMBL 1213 21 6 14 9.3 O=C(c1ccc(c(c1)C(=O)O)c1c2ccc(c(c2oc2c1ccc(=[NH2+])c2S(=O)(=O)[O-])S(=O)(=O)O)N)NCCCCCCn1nnc(c1)CCCCN1CCC(CC1)c1ccc(cc1)c1cc(cc2c1ccc(c2)c1ccc(cc1)C(F)(F)F)C(=O)O 10.1021/acs.jmedchem.6b00044
124221651 9445 0 None - 0 Human 10.1 pKi = 10.1 Functional
Antagonist activity at human P2Y14R expressed in CHO cells assessed as inhibition of UDPG-mediated reduction of forskolin-induced [3H]cAMP production measured after 15 mins in presence of phosphodiesterase inhibitor IBMX by chromatographic methodAntagonist activity at human P2Y14R expressed in CHO cells assessed as inhibition of UDPG-mediated reduction of forskolin-induced [3H]cAMP production measured after 15 mins in presence of phosphodiesterase inhibitor IBMX by chromatographic method
ChEMBL 1213 21 6 14 9.3 O=C(c1ccc(c(c1)C(=O)O)c1c2ccc(c(c2oc2c1ccc(=[NH2+])c2S(=O)(=O)[O-])S(=O)(=O)O)N)NCCCCCCn1nnc(c1)CCCCN1CCC(CC1)c1ccc(cc1)c1cc(cc2c1ccc(c2)c1ccc(cc1)C(F)(F)F)C(=O)O 10.1021/acs.jmedchem.6b00044
9470 9445 0 None - 0 Human 10.1 pKi = 10.1 Functional
Antagonist activity at human P2Y14R expressed in CHO cells assessed as inhibition of UDPG-mediated reduction of forskolin-induced [3H]cAMP production measured after 15 mins in presence of phosphodiesterase inhibitor IBMX by chromatographic methodAntagonist activity at human P2Y14R expressed in CHO cells assessed as inhibition of UDPG-mediated reduction of forskolin-induced [3H]cAMP production measured after 15 mins in presence of phosphodiesterase inhibitor IBMX by chromatographic method
ChEMBL 1213 21 6 14 9.3 O=C(c1ccc(c(c1)C(=O)O)c1c2ccc(c(c2oc2c1ccc(=[NH2+])c2S(=O)(=O)[O-])S(=O)(=O)O)N)NCCCCCCn1nnc(c1)CCCCN1CCC(CC1)c1ccc(cc1)c1cc(cc2c1ccc(c2)c1ccc(cc1)C(F)(F)F)C(=O)O 10.1021/acs.jmedchem.6b00044
CHEMBL4447162 9445 0 None - 0 Human 10.1 pKi = 10.1 Functional
Antagonist activity at human P2Y14R expressed in CHO cells assessed as inhibition of UDPG-mediated reduction of forskolin-induced [3H]cAMP production measured after 15 mins in presence of phosphodiesterase inhibitor IBMX by chromatographic methodAntagonist activity at human P2Y14R expressed in CHO cells assessed as inhibition of UDPG-mediated reduction of forskolin-induced [3H]cAMP production measured after 15 mins in presence of phosphodiesterase inhibitor IBMX by chromatographic method
ChEMBL 1213 21 6 14 9.3 O=C(c1ccc(c(c1)C(=O)O)c1c2ccc(c(c2oc2c1ccc(=[NH2+])c2S(=O)(=O)[O-])S(=O)(=O)O)N)NCCCCCCn1nnc(c1)CCCCN1CCC(CC1)c1ccc(cc1)c1cc(cc2c1ccc(c2)c1ccc(cc1)C(F)(F)F)C(=O)O 10.1021/acs.jmedchem.6b00044
42611190 9930 12 None 5 2 Human 9.4 pKi = 9.4 Functional
Antagonist activity at human P2Y14 expressed in CHO cells assessed as inhibition of forskolin-induced increase of cAMP accumulation incubated for 15 mins in presence of IBMXAntagonist activity at human P2Y14 expressed in CHO cells assessed as inhibition of forskolin-induced increase of cAMP accumulation incubated for 15 mins in presence of IBMX
ChEMBL 475 4 2 2 7.4 OC(=O)c1cc2cc(ccc2c(c1)c1ccc(cc1)C1CCNCC1)c1ccc(cc1)C(F)(F)F 10.1021/acs.jmedchem.1c01964
5802 9930 12 None 5 2 Human 9.4 pKi = 9.4 Functional
Antagonist activity at human P2Y14 expressed in CHO cells assessed as inhibition of forskolin-induced increase of cAMP accumulation incubated for 15 mins in presence of IBMXAntagonist activity at human P2Y14 expressed in CHO cells assessed as inhibition of forskolin-induced increase of cAMP accumulation incubated for 15 mins in presence of IBMX
ChEMBL 475 4 2 2 7.4 OC(=O)c1cc2cc(ccc2c(c1)c1ccc(cc1)C1CCNCC1)c1ccc(cc1)C(F)(F)F 10.1021/acs.jmedchem.1c01964
CHEMBL1800685 9930 12 None 5 2 Human 9.4 pKi = 9.4 Functional
Antagonist activity at human P2Y14 expressed in CHO cells assessed as inhibition of forskolin-induced increase of cAMP accumulation incubated for 15 mins in presence of IBMXAntagonist activity at human P2Y14 expressed in CHO cells assessed as inhibition of forskolin-induced increase of cAMP accumulation incubated for 15 mins in presence of IBMX
ChEMBL 475 4 2 2 7.4 OC(=O)c1cc2cc(ccc2c(c1)c1ccc(cc1)C1CCNCC1)c1ccc(cc1)C(F)(F)F 10.1021/acs.jmedchem.1c01964
124221652 9446 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Measuring inhibition of forskolin-stimulated cAMP formation in CHO cells expressing the human P2Y<sub>14</sub> receptorMeasuring inhibition of forskolin-stimulated cAMP formation in CHO cells expressing the human P2Y<sub>14</sub> receptor
Guide to Pharmacology 1070 20 10 20 -0.1 O=C(COc1ccc(cc1)C1=[N+]2C(=Cc3n([B-]2(F)F)c(cc3)c2cccs2)C=C1)NCCCCCNC(=O)[C@H]1O[C@H](OP(=O)(OP(=O)(OCC2OC(C(C2O)O)n2ccc(=O)[nH]c2=O)O)O)[C@@H]([C@H]([C@@H]1O)O)O 26303895
9471 9446 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Measuring inhibition of forskolin-stimulated cAMP formation in CHO cells expressing the human P2Y<sub>14</sub> receptorMeasuring inhibition of forskolin-stimulated cAMP formation in CHO cells expressing the human P2Y<sub>14</sub> receptor
Guide to Pharmacology 1070 20 10 20 -0.1 O=C(COc1ccc(cc1)C1=[N+]2C(=Cc3n([B-]2(F)F)c(cc3)c2cccs2)C=C1)NCCCCCNC(=O)[C@H]1O[C@H](OP(=O)(OP(=O)(OCC2OC(C(C2O)O)n2ccc(=O)[nH]c2=O)O)O)[C@@H]([C@H]([C@@H]1O)O)O 26303895
126456135 9432 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 626 11 7 18 -3.2 OC[C@H]1O[C@H](OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=S)O[Na])O[Na])[C@@H]([C@H]([C@@H]1O)O)O 17407275
126456135 9432 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 626 11 7 18 -3.2 OC[C@H]1O[C@H](OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=S)O[Na])O[Na])[C@@H]([C@H]([C@@H]1O)O)O 22825617
3337 9432 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 626 11 7 18 -3.2 OC[C@H]1O[C@H](OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=S)O[Na])O[Na])[C@@H]([C@H]([C@@H]1O)O)O 17407275
3337 9432 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 626 11 7 18 -3.2 OC[C@H]1O[C@H](OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=S)O[Na])O[Na])[C@@H]([C@H]([C@@H]1O)O)O 22825617
73755042 9432 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 626 11 7 18 -3.2 OC[C@H]1O[C@H](OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=S)O[Na])O[Na])[C@@H]([C@H]([C@@H]1O)O)O 17407275
73755042 9432 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 626 11 7 18 -3.2 OC[C@H]1O[C@H](OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=S)O[Na])O[Na])[C@@H]([C@H]([C@@H]1O)O)O 22825617
90488784 9432 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 626 11 7 18 -3.2 OC[C@H]1O[C@H](OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=S)O[Na])O[Na])[C@@H]([C@H]([C@@H]1O)O)O 17407275
90488784 9432 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 626 11 7 18 -3.2 OC[C@H]1O[C@H](OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=S)O[Na])O[Na])[C@@H]([C@H]([C@@H]1O)O)O 22825617
1782 10696 16 None -10 5 Human 7.0 pEC50 = 7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 566 9 9 16 -4.8 OC[C@H]1O[C@H](OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)[C@@H]([C@H]([C@H]1O)O)O 10753868
18068 10696 16 None -10 5 Human 7.0 pEC50 = 7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 566 9 9 16 -4.8 OC[C@H]1O[C@H](OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)[C@@H]([C@H]([C@H]1O)O)O 10753868
CHEMBL439009 10696 16 None -10 5 Human 7.0 pEC50 = 7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 566 9 9 16 -4.8 OC[C@H]1O[C@H](OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)[C@@H]([C@H]([C@H]1O)O)O 10753868
DB03501 10696 16 None -10 5 Human 7.0 pEC50 = 7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 566 9 9 16 -4.8 OC[C@H]1O[C@H](OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)[C@@H]([C@H]([C@H]1O)O)O 10753868
146015339 10694 32 None 1 7 Human 7.1 pEC50 = 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 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 19759354
1749 10694 32 None 1 7 Human 7.1 pEC50 = 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 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 19759354
6031 10694 32 None 1 7 Human 7.1 pEC50 = 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 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 19759354
CHEMBL130266 10694 32 None 1 7 Human 7.1 pEC50 = 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 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 19759354
DB03435 10694 32 None 1 7 Human 7.1 pEC50 = 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 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 19759354
5909 9437 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 438 6 6 9 -1.9 O[C@H]1[C@@H](COP(=O)(C(P(=O)(O)O)(F)F)O)O[C@H]([C@H]1O)n1ccc(=O)[nH]c1=O 19902968
91827349 9437 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 438 6 6 9 -1.9 O[C@H]1[C@@H](COP(=O)(C(P(=O)(O)O)(F)F)O)O[C@H]([C@H]1O)n1ccc(=O)[nH]c1=O 19902968
16082712 6877 1 None 85 2 Human 8.7 pEC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 420 6 6 10 -1.2 O[C@@H]1[C@@H](COP(=O)(OP(=O)(O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=S 19902968
6202 6877 1 None 85 2 Human 8.7 pEC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 420 6 6 10 -1.2 O[C@@H]1[C@@H](COP(=O)(OP(=O)(O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=S 19902968
CHEMBL216011 6877 1 None 85 2 Human 8.7 pEC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 420 6 6 10 -1.2 O[C@@H]1[C@@H](COP(=O)(OP(=O)(O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=S 19902968
5908 9438 0 None - 1 Human 9.0 pEC50 = 9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 432 7 6 9 -1.1 O[C@H]1[C@@H](COP(=O)(CCP(=O)(O)O)O)O[C@H]([C@H]1O)n1ccc(=O)[nH]c1=S 21484092
91827348 9438 0 None - 1 Human 9.0 pEC50 = 9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 432 7 6 9 -1.1 O[C@H]1[C@@H](COP(=O)(CCP(=O)(O)O)O)O[C@H]([C@H]1O)n1ccc(=O)[nH]c1=S 21484092
6203 7143 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 414 6 4 7 1.4 C[C@@H]1[C@@H](COP(=O)(CP(=O)(O)O)O)O[C@H]([C@@H]1C)n1ccc(=O)[nH]c1=S 19902968
73755188 7143 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 414 6 4 7 1.4 C[C@@H]1[C@@H](COP(=O)(CP(=O)(O)O)O)O[C@H]([C@@H]1C)n1ccc(=O)[nH]c1=S 19902968
1779 10699 0 None -10 3 Human 6.0 pEC50 None 6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 607 10 9 16 -4.7 OC[C@H]1O[C@H](OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)[C@@H]([C@H]([C@@H]1O)O)NC(=O)C 19339661
445675 10699 0 None -10 3 Human 6.0 pEC50 None 6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 607 10 9 16 -4.7 OC[C@H]1O[C@H](OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)[C@@H]([C@H]([C@@H]1O)O)NC(=O)C 19339661
CHEMBL388154 10699 0 None -10 3 Human 6.0 pEC50 None 6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 607 10 9 16 -4.7 OC[C@H]1O[C@H](OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)[C@@H]([C@H]([C@@H]1O)O)NC(=O)C 19339661
DB03397 10699 0 None -10 3 Human 6.0 pEC50 None 6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 607 10 9 16 -4.7 OC[C@H]1O[C@H](OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)[C@@H]([C@H]([C@@H]1O)O)NC(=O)C 19339661
1779 10699 0 None -1 3 Rat 6.8 pEC50 None 6.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 607 10 9 16 -4.7 OC[C@H]1O[C@H](OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)[C@@H]([C@H]([C@@H]1O)O)NC(=O)C 11735218
445675 10699 0 None -1 3 Rat 6.8 pEC50 None 6.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 607 10 9 16 -4.7 OC[C@H]1O[C@H](OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)[C@@H]([C@H]([C@@H]1O)O)NC(=O)C 11735218
CHEMBL388154 10699 0 None -1 3 Rat 6.8 pEC50 None 6.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 607 10 9 16 -4.7 OC[C@H]1O[C@H](OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)[C@@H]([C@H]([C@@H]1O)O)NC(=O)C 11735218
DB03397 10699 0 None -1 3 Rat 6.8 pEC50 None 6.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 607 10 9 16 -4.7 OC[C@H]1O[C@H](OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)[C@@H]([C@H]([C@@H]1O)O)NC(=O)C 11735218
17473 10698 18 None -1 3 Rat 7.0 pEC50 None 7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 580 9 9 16 -4.7 O[C@@H]1[C@@H](COP(=O)(OP(=O)(O[C@H]2O[C@H](C(=O)O)[C@H]([C@@H]([C@H]2O)O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 11735218
1784 10698 18 None -1 3 Rat 7.0 pEC50 None 7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 580 9 9 16 -4.7 O[C@@H]1[C@@H](COP(=O)(OP(=O)(O[C@H]2O[C@H](C(=O)O)[C@H]([C@@H]([C@H]2O)O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 11735218
CHEMBL228057 10698 18 None -1 3 Rat 7.0 pEC50 None 7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 580 9 9 16 -4.7 O[C@@H]1[C@@H](COP(=O)(OP(=O)(O[C@H]2O[C@H](C(=O)O)[C@H]([C@@H]([C@H]2O)O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 11735218
DB03041 10698 18 None -1 3 Rat 7.0 pEC50 None 7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 580 9 9 16 -4.7 O[C@@H]1[C@@H](COP(=O)(OP(=O)(O[C@H]2O[C@H](C(=O)O)[C@H]([C@@H]([C@H]2O)O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 11735218
1779 10699 0 None 1 3 Mouse 7.0 pEC50 None 7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 607 10 9 16 -4.7 OC[C@H]1O[C@H](OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)[C@@H]([C@H]([C@@H]1O)O)NC(=O)C 11735218
445675 10699 0 None 1 3 Mouse 7.0 pEC50 None 7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 607 10 9 16 -4.7 OC[C@H]1O[C@H](OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)[C@@H]([C@H]([C@@H]1O)O)NC(=O)C 11735218
CHEMBL388154 10699 0 None 1 3 Mouse 7.0 pEC50 None 7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 607 10 9 16 -4.7 OC[C@H]1O[C@H](OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)[C@@H]([C@H]([C@@H]1O)O)NC(=O)C 11735218
DB03397 10699 0 None 1 3 Mouse 7.0 pEC50 None 7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 607 10 9 16 -4.7 OC[C@H]1O[C@H](OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)[C@@H]([C@H]([C@@H]1O)O)NC(=O)C 11735218
1782 10696 16 None -3 5 Rat 7.1 pEC50 None 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 566 9 9 16 -4.8 OC[C@H]1O[C@H](OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)[C@@H]([C@H]([C@H]1O)O)O 11735218
18068 10696 16 None -3 5 Rat 7.1 pEC50 None 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 566 9 9 16 -4.8 OC[C@H]1O[C@H](OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)[C@@H]([C@H]([C@H]1O)O)O 11735218
CHEMBL439009 10696 16 None -3 5 Rat 7.1 pEC50 None 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 566 9 9 16 -4.8 OC[C@H]1O[C@H](OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)[C@@H]([C@H]([C@H]1O)O)O 11735218
DB03501 10696 16 None -3 5 Rat 7.1 pEC50 None 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 566 9 9 16 -4.8 OC[C@H]1O[C@H](OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)[C@@H]([C@H]([C@H]1O)O)O 11735218
17473 10698 18 None -2 3 Human 7.2 pEC50 None 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 580 9 9 16 -4.7 O[C@@H]1[C@@H](COP(=O)(OP(=O)(O[C@H]2O[C@H](C(=O)O)[C@H]([C@@H]([C@H]2O)O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 19339661
17473 10698 18 None 1 3 Mouse 7.2 pEC50 None 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 580 9 9 16 -4.7 O[C@@H]1[C@@H](COP(=O)(OP(=O)(O[C@H]2O[C@H](C(=O)O)[C@H]([C@@H]([C@H]2O)O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 11735218
1784 10698 18 None -2 3 Human 7.2 pEC50 None 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 580 9 9 16 -4.7 O[C@@H]1[C@@H](COP(=O)(OP(=O)(O[C@H]2O[C@H](C(=O)O)[C@H]([C@@H]([C@H]2O)O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 19339661
1784 10698 18 None 1 3 Mouse 7.2 pEC50 None 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 580 9 9 16 -4.7 O[C@@H]1[C@@H](COP(=O)(OP(=O)(O[C@H]2O[C@H](C(=O)O)[C@H]([C@@H]([C@H]2O)O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 11735218
CHEMBL228057 10698 18 None -2 3 Human 7.2 pEC50 None 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 580 9 9 16 -4.7 O[C@@H]1[C@@H](COP(=O)(OP(=O)(O[C@H]2O[C@H](C(=O)O)[C@H]([C@@H]([C@H]2O)O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 19339661
CHEMBL228057 10698 18 None 1 3 Mouse 7.2 pEC50 None 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 580 9 9 16 -4.7 O[C@@H]1[C@@H](COP(=O)(OP(=O)(O[C@H]2O[C@H](C(=O)O)[C@H]([C@@H]([C@H]2O)O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 11735218
DB03041 10698 18 None -2 3 Human 7.2 pEC50 None 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 580 9 9 16 -4.7 O[C@@H]1[C@@H](COP(=O)(OP(=O)(O[C@H]2O[C@H](C(=O)O)[C@H]([C@@H]([C@H]2O)O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 19339661
DB03041 10698 18 None 1 3 Mouse 7.2 pEC50 None 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 580 9 9 16 -4.7 O[C@@H]1[C@@H](COP(=O)(OP(=O)(O[C@H]2O[C@H](C(=O)O)[C@H]([C@@H]([C@H]2O)O)O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 11735218
1782 10696 16 None 1 5 Mouse 7.6 pEC50 None 7.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 566 9 9 16 -4.8 OC[C@H]1O[C@H](OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)[C@@H]([C@H]([C@H]1O)O)O 11735218
18068 10696 16 None 1 5 Mouse 7.6 pEC50 None 7.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 566 9 9 16 -4.8 OC[C@H]1O[C@H](OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)[C@@H]([C@H]([C@H]1O)O)O 11735218
CHEMBL439009 10696 16 None 1 5 Mouse 7.6 pEC50 None 7.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 566 9 9 16 -4.8 OC[C@H]1O[C@H](OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)[C@@H]([C@H]([C@H]1O)O)O 11735218
DB03501 10696 16 None 1 5 Mouse 7.6 pEC50 None 7.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 566 9 9 16 -4.8 OC[C@H]1O[C@H](OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)[C@@H]([C@H]([C@H]1O)O)O 11735218
1783 10697 25 None -1 7 Rat 7.6 pEC50 None 7.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 566 9 9 16 -4.8 OC[C@H]1O[C@H](OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)[C@@H]([C@H]([C@@H]1O)O)O 11735218
8629 10697 25 None -1 7 Rat 7.6 pEC50 None 7.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 566 9 9 16 -4.8 OC[C@H]1O[C@H](OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)[C@@H]([C@H]([C@@H]1O)O)O 11735218
CHEMBL375951 10697 25 None -1 7 Rat 7.6 pEC50 None 7.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 566 9 9 16 -4.8 OC[C@H]1O[C@H](OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)[C@@H]([C@H]([C@@H]1O)O)O 11735218
DB01861 10697 25 None -1 7 Rat 7.6 pEC50 None 7.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 566 9 9 16 -4.8 OC[C@H]1O[C@H](OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)[C@@H]([C@H]([C@@H]1O)O)O 11735218
1783 10697 25 None -1 7 Mouse 7.7 pEC50 None 7.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 566 9 9 16 -4.8 OC[C@H]1O[C@H](OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)[C@@H]([C@H]([C@@H]1O)O)O 11735218
8629 10697 25 None -1 7 Mouse 7.7 pEC50 None 7.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 566 9 9 16 -4.8 OC[C@H]1O[C@H](OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)[C@@H]([C@H]([C@@H]1O)O)O 11735218
CHEMBL375951 10697 25 None -1 7 Mouse 7.7 pEC50 None 7.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 566 9 9 16 -4.8 OC[C@H]1O[C@H](OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)[C@@H]([C@H]([C@@H]1O)O)O 11735218
DB01861 10697 25 None -1 7 Mouse 7.7 pEC50 None 7.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 566 9 9 16 -4.8 OC[C@H]1O[C@H](OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)[C@@H]([C@H]([C@@H]1O)O)O 11735218
134611896 9448 4 None 3 2 Human 6.6 pIC50 = 6.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 452 5 2 5 4.4 OC(=O)c1cc(cc(c1)n1nnc(c1)c1ccc(cc1)C(F)(F)F)c1ccc(cc1)C(=O)N 29767967
9999 9448 4 None 3 2 Human 6.6 pIC50 = 6.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 452 5 2 5 4.4 OC(=O)c1cc(cc(c1)n1nnc(c1)c1ccc(cc1)C(F)(F)F)c1ccc(cc1)C(=O)N 29767967
CHEMBL4299805 9448 4 None 3 2 Human 6.6 pIC50 = 6.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 452 5 2 5 4.4 OC(=O)c1cc(cc(c1)n1nnc(c1)c1ccc(cc1)C(F)(F)F)c1ccc(cc1)C(=O)N 29767967
134611895 9447 4 None 2 2 Human 6.8 pIC50 = 6.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 515 8 3 7 4.5 NCCCNC(=O)c1ccc(s1)c1cc(cc(c1)n1nnc(c1)c1ccc(cc1)C(F)(F)F)C(=O)O 29767967
9998 9447 4 None 2 2 Human 6.8 pIC50 = 6.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 515 8 3 7 4.5 NCCCNC(=O)c1ccc(s1)c1cc(cc(c1)n1nnc(c1)c1ccc(cc1)C(F)(F)F)C(=O)O 29767967
CHEMBL4212721 9447 4 None 2 2 Human 6.8 pIC50 = 6.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 515 8 3 7 4.5 NCCCNC(=O)c1ccc(s1)c1cc(cc(c1)n1nnc(c1)c1ccc(cc1)C(F)(F)F)C(=O)O 29767967
1783 10697 25 None -13 7 Human 7.1 pIC50 = 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 566 9 9 16 -4.8 OC[C@H]1O[C@H](OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)[C@@H]([C@H]([C@@H]1O)O)O 19339661
8629 10697 25 None -13 7 Human 7.1 pIC50 = 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 566 9 9 16 -4.8 OC[C@H]1O[C@H](OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)[C@@H]([C@H]([C@@H]1O)O)O 19339661
CHEMBL375951 10697 25 None -13 7 Human 7.1 pIC50 = 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 566 9 9 16 -4.8 OC[C@H]1O[C@H](OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)[C@@H]([C@H]([C@@H]1O)O)O 19339661
DB01861 10697 25 None -13 7 Human 7.1 pIC50 = 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 566 9 9 16 -4.8 OC[C@H]1O[C@H](OP(=O)(OP(=O)(OC[C@H]2O[C@H]([C@@H]([C@@H]2O)O)n2ccc(=O)[nH]c2=O)O)O)[C@@H]([C@H]([C@@H]1O)O)O 19339661
11453 9449 0 None -1 2 Mouse 7.5 pIC50 = 7.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 505 5 1 3 7.6 CON1CCC(CC1)c1ccc(cc1)c1cc(cc2c1ccc(c2)c1ccc(cc1)C(F)(F)F)C(=O)O 32551012
155817521 9449 0 None -1 2 Mouse 7.5 pIC50 = 7.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 505 5 1 3 7.6 CON1CCC(CC1)c1ccc(cc1)c1cc(cc2c1ccc(c2)c1ccc(cc1)C(F)(F)F)C(=O)O 32551012
11453 9449 0 None 1 2 Human 7.6 pIC50 = 7.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 505 5 1 3 7.6 CON1CCC(CC1)c1ccc(cc1)c1cc(cc2c1ccc(c2)c1ccc(cc1)C(F)(F)F)C(=O)O 32551012
155817521 9449 0 None 1 2 Human 7.6 pIC50 = 7.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 505 5 1 3 7.6 CON1CCC(CC1)c1ccc(cc1)c1cc(cc2c1ccc(c2)c1ccc(cc1)C(F)(F)F)C(=O)O 32551012
13422 9760 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 345 4 2 3 3.3 C1=CC(=CC=C1OCC(=O)NC2=CC3=C(C=C2)N=CN3)Br 38874515
146015339 10694 32 None -5 7 Rat 6.5 pIC50 None 6.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 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 18252808
1749 10694 32 None -5 7 Rat 6.5 pIC50 None 6.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 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 18252808
6031 10694 32 None -5 7 Rat 6.5 pIC50 None 6.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 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 18252808
CHEMBL130266 10694 32 None -5 7 Rat 6.5 pIC50 None 6.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 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 18252808
DB03435 10694 32 None -5 7 Rat 6.5 pIC50 None 6.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 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 18252808




Ligands (move mouse cursor over ligand name to see structure) Receptor Assay information Chemical information
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DOI

44422870 92352 4 None - 0 Human 5.0 pEC50 = 5.0 Binding
Agonist activity at recombinant human P2Y14 receptor expressed in African green monkey COS7 cells co-transfected with Galphaqi assessed as stimulation of phospholipase CbetaAgonist activity at recombinant human P2Y14 receptor expressed in African green monkey COS7 cells co-transfected with Galphaqi assessed as stimulation of phospholipase Cbeta
ChEMBL 582 9 9 16 -3.4 O=c1ccn([C@@H]2O[C@H](COP(=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(=S)[nH]1 10.1016/j.bmc.2015.03.042
CHEMBL228111 92352 4 None - 0 Human 5.0 pEC50 = 5.0 Binding
Agonist activity at recombinant human P2Y14 receptor expressed in African green monkey COS7 cells co-transfected with Galphaqi assessed as stimulation of phospholipase CbetaAgonist activity at recombinant human P2Y14 receptor expressed in African green monkey COS7 cells co-transfected with Galphaqi assessed as stimulation of phospholipase Cbeta
ChEMBL 582 9 9 16 -3.4 O=c1ccn([C@@H]2O[C@H](COP(=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(=S)[nH]1 10.1016/j.bmc.2015.03.042
146015339 10694 32 None - 0 Human 7.5 pEC50 = 7.5 Binding
Agonist activity at human P2Y14 expressed in rat C6 cellsAgonist activity at human P2Y14 expressed in rat C6 cells
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/acs.jmedchem.5b01972
1749 10694 32 None - 0 Human 7.5 pEC50 = 7.5 Binding
Agonist activity at human P2Y14 expressed in rat C6 cellsAgonist activity at human P2Y14 expressed in rat C6 cells
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/acs.jmedchem.5b01972
6031 10694 32 None - 0 Human 7.5 pEC50 = 7.5 Binding
Agonist activity at human P2Y14 expressed in rat C6 cellsAgonist activity at human P2Y14 expressed in rat C6 cells
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/acs.jmedchem.5b01972
CHEMBL130266 10694 32 None - 0 Human 7.5 pEC50 = 7.5 Binding
Agonist activity at human P2Y14 expressed in rat C6 cellsAgonist activity at human P2Y14 expressed in rat C6 cells
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/acs.jmedchem.5b01972
DB03435 10694 32 None - 0 Human 7.5 pEC50 = 7.5 Binding
Agonist activity at human P2Y14 expressed in rat C6 cellsAgonist activity at human P2Y14 expressed in rat C6 cells
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/acs.jmedchem.5b01972
146015339 10694 32 None - 0 Human 7.5 pEC50 = 7.5 Binding
Agonist activity at human P2Y14 expressed in rat CHO cellsAgonist activity at human P2Y14 expressed in rat CHO cells
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/acs.jmedchem.5b01972
1749 10694 32 None - 0 Human 7.5 pEC50 = 7.5 Binding
Agonist activity at human P2Y14 expressed in rat CHO cellsAgonist activity at human P2Y14 expressed in rat CHO cells
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/acs.jmedchem.5b01972
6031 10694 32 None - 0 Human 7.5 pEC50 = 7.5 Binding
Agonist activity at human P2Y14 expressed in rat CHO cellsAgonist activity at human P2Y14 expressed in rat CHO cells
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/acs.jmedchem.5b01972
CHEMBL130266 10694 32 None - 0 Human 7.5 pEC50 = 7.5 Binding
Agonist activity at human P2Y14 expressed in rat CHO cellsAgonist activity at human P2Y14 expressed in rat CHO cells
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/acs.jmedchem.5b01972
DB03435 10694 32 None - 0 Human 7.5 pEC50 = 7.5 Binding
Agonist activity at human P2Y14 expressed in rat CHO cellsAgonist activity at human P2Y14 expressed in rat CHO cells
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/acs.jmedchem.5b01972
146015339 10694 32 None - 0 Rat 6.5 pEC50 = 6.5 Binding
Antagonist activity at rat P2Y14Antagonist activity at rat P2Y14
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/acs.jmedchem.5b01972
1749 10694 32 None - 0 Rat 6.5 pEC50 = 6.5 Binding
Antagonist activity at rat P2Y14Antagonist activity at rat P2Y14
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/acs.jmedchem.5b01972
6031 10694 32 None - 0 Rat 6.5 pEC50 = 6.5 Binding
Antagonist activity at rat P2Y14Antagonist activity at rat P2Y14
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/acs.jmedchem.5b01972
CHEMBL130266 10694 32 None - 0 Rat 6.5 pEC50 = 6.5 Binding
Antagonist activity at rat P2Y14Antagonist activity at rat P2Y14
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/acs.jmedchem.5b01972
DB03435 10694 32 None - 0 Rat 6.5 pEC50 = 6.5 Binding
Antagonist activity at rat P2Y14Antagonist activity at rat P2Y14
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/acs.jmedchem.5b01972
146015339 10694 32 None - 0 Human 7.1 pEC50 = 7.1 Binding
Agonist activity at human P2Y14 expressed in HEK293 cellsAgonist activity at human P2Y14 expressed in HEK293 cells
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/acs.jmedchem.5b01972
1749 10694 32 None - 0 Human 7.1 pEC50 = 7.1 Binding
Agonist activity at human P2Y14 expressed in HEK293 cellsAgonist activity at human P2Y14 expressed in HEK293 cells
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/acs.jmedchem.5b01972
6031 10694 32 None - 0 Human 7.1 pEC50 = 7.1 Binding
Agonist activity at human P2Y14 expressed in HEK293 cellsAgonist activity at human P2Y14 expressed in HEK293 cells
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/acs.jmedchem.5b01972
CHEMBL130266 10694 32 None - 0 Human 7.1 pEC50 = 7.1 Binding
Agonist activity at human P2Y14 expressed in HEK293 cellsAgonist activity at human P2Y14 expressed in HEK293 cells
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/acs.jmedchem.5b01972
DB03435 10694 32 None - 0 Human 7.1 pEC50 = 7.1 Binding
Agonist activity at human P2Y14 expressed in HEK293 cellsAgonist activity at human P2Y14 expressed in HEK293 cells
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/acs.jmedchem.5b01972
42611190 9930 12 None -1 5 Human 9.3 pIC50 = 9.3 Binding
Affinity Biochemical interaction (FLIPR assay) EUB0000274bCl P2RY14Affinity Biochemical interaction (FLIPR assay) EUB0000274bCl P2RY14
ChEMBL 475 4 2 2 7.4 OC(=O)c1cc2cc(ccc2c(c1)c1ccc(cc1)C1CCNCC1)c1ccc(cc1)C(F)(F)F 10.6019/CHEMBL5210307
5802 9930 12 None -1 5 Human 9.3 pIC50 = 9.3 Binding
Affinity Biochemical interaction (FLIPR assay) EUB0000274bCl P2RY14Affinity Biochemical interaction (FLIPR assay) EUB0000274bCl P2RY14
ChEMBL 475 4 2 2 7.4 OC(=O)c1cc2cc(ccc2c(c1)c1ccc(cc1)C1CCNCC1)c1ccc(cc1)C(F)(F)F 10.6019/CHEMBL5210307
CHEMBL1800685 9930 12 None -1 5 Human 9.3 pIC50 = 9.3 Binding
Affinity Biochemical interaction (FLIPR assay) EUB0000274bCl P2RY14Affinity Biochemical interaction (FLIPR assay) EUB0000274bCl P2RY14
ChEMBL 475 4 2 2 7.4 OC(=O)c1cc2cc(ccc2c(c1)c1ccc(cc1)C1CCNCC1)c1ccc(cc1)C(F)(F)F 10.6019/CHEMBL5210307
CHEMBL5083619 221654 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Inhibition of fluorescent antagonist binding to human P2Y14R expressed in CHO cells preincubated for 30 mins followed by 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy 6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate addition and measured after 30 mins by BD FACSCalibur flow cytometry analysisInhibition of fluorescent antagonist binding to human P2Y14R expressed in CHO cells preincubated for 30 mins followed by 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy 6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate addition and measured after 30 mins by BD FACSCalibur flow cytometry analysis
ChEMBL None None None N[C@@H]1C[C@H](CO)[C@@H](c2ccc(-c3cc(C(=O)O)cc4cc(-c5ccc(C(F)(F)F)cc5)ccc34)cc2)C1 10.1021/acs.jmedchem.1c01964
CHEMBL5093569 222211 0 None - 0 Human 7.0 pIC50 = 7 Binding
Inhibition of fluorescent antagonist binding to human P2Y14R expressed in CHO cells preincubated for 30 mins followed by 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy 6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate addition and measured after 30 mins by BD FACSCalibur flow cytometry analysisInhibition of fluorescent antagonist binding to human P2Y14R expressed in CHO cells preincubated for 30 mins followed by 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy 6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate addition and measured after 30 mins by BD FACSCalibur flow cytometry analysis
ChEMBL None None None N[C@@H]1C[C@H](CO)C[C@H]1c1ccc(-c2cc(C(=O)O)cc3cc(-c4ccc(C(F)(F)F)cc4)ccc23)cc1 10.1021/acs.jmedchem.1c01964
CHEMBL5081782 221548 0 None - 0 Human 7.0 pIC50 = 7 Binding
Inhibition of fluorescent antagonist binding to human P2Y14R expressed in CHO cells preincubated for 30 mins followed by 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy 6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate addition and measured after 30 mins by BD FACSCalibur flow cytometry analysisInhibition of fluorescent antagonist binding to human P2Y14R expressed in CHO cells preincubated for 30 mins followed by 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy 6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate addition and measured after 30 mins by BD FACSCalibur flow cytometry analysis
ChEMBL None None None O=C(O)c1cc(-c2ccc([C@H]3C[C@H]4C[C@@H]3C(=O)N4)cc2)c2ccc(-c3ccc(C(F)(F)F)cc3)cc2c1 10.1021/acs.jmedchem.1c01964
CHEMBL5079515 221400 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibition of fluorescent antagonist binding to human P2Y14R expressed in CHO cells preincubated for 30 mins followed by 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy 6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate addition and measured after 30 mins by BD FACSCalibur flow cytometry analysisInhibition of fluorescent antagonist binding to human P2Y14R expressed in CHO cells preincubated for 30 mins followed by 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy 6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate addition and measured after 30 mins by BD FACSCalibur flow cytometry analysis
ChEMBL None None None N[C@H]1C[C@@H](C(=O)O)[C@H](c2ccc(-c3cc(C(=O)O)cc4cc(-c5ccc(C(F)(F)F)cc5)ccc34)cc2)C1 10.1021/acs.jmedchem.1c01964
CHEMBL5093465 222208 0 None - 0 Mouse 7.0 pIC50 = 7.0 Binding
Inhibition of fluorescent antagonist binding to mouse P2Y14R expressed in HEK293 cells preincubated for 30 mins followed by addition of 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy-6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate incubated for 30 mins by BD FACSCalibur flow cytometry analysisInhibition of fluorescent antagonist binding to mouse P2Y14R expressed in HEK293 cells preincubated for 30 mins followed by addition of 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy-6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate incubated for 30 mins by BD FACSCalibur flow cytometry analysis
ChEMBL None None None CC(=O)N1C[C@H]2C[C@@H]1C[C@@H]2c1ccc(-c2cc(C(=O)O)cc3cc(-c4ccc(C(F)(F)F)cc4)ccc23)cc1 10.1021/acs.jmedchem.1c01964
CHEMBL5090079 222020 0 None - 0 Mouse 7.0 pIC50 = 7.0 Binding
Inhibition of fluorescent antagonist binding to mouse P2Y14R expressed in HEK293 cells preincubated for 30 mins followed by addition of 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy-6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate incubated for 30 mins by BD FACSCalibur flow cytometry analysisInhibition of fluorescent antagonist binding to mouse P2Y14R expressed in HEK293 cells preincubated for 30 mins followed by addition of 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy-6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate incubated for 30 mins by BD FACSCalibur flow cytometry analysis
ChEMBL None None None CS(=O)(=O)C1C[C@H]2C[C@@H]1C[C@@H]2c1ccc(-c2cc(C(=O)O)cc3cc(-c4ccc(C(F)(F)F)cc4)ccc23)cc1 10.1021/acs.jmedchem.1c01964
156019395 184788 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7.4 by flow cytomtery based competitive fluorescence assayInhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7.4 by flow cytomtery based competitive fluorescence assay
ChEMBL 518 5 1 5 6.1 O=C(O)c1cc(-c2ccc(C34CCN(CC3)CC4)cc2)cc(-n2cc(-c3ccc(C(F)(F)F)cc3)nn2)c1 10.1021/acs.jmedchem.0c00745
CHEMBL4646514 184788 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7.4 by flow cytomtery based competitive fluorescence assayInhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7.4 by flow cytomtery based competitive fluorescence assay
ChEMBL 518 5 1 5 6.1 O=C(O)c1cc(-c2ccc(C34CCN(CC3)CC4)cc2)cc(-n2cc(-c3ccc(C(F)(F)F)cc3)nn2)c1 10.1021/acs.jmedchem.0c00745
145978515 170467 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Displacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric methodDisplacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric method
ChEMBL 499 8 3 7 4.0 NCCCNC(=O)c1ccc(-c2cc(C(=O)O)cc(-n3cc(-c4ccc(C(F)(F)F)cc4)nn3)c2)o1 10.1021/acs.jmedchem.8b00168
CHEMBL4204811 170467 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Displacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric methodDisplacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric method
ChEMBL 499 8 3 7 4.0 NCCCNC(=O)c1ccc(-c2cc(C(=O)O)cc(-n3cc(-c4ccc(C(F)(F)F)cc4)nn3)c2)o1 10.1021/acs.jmedchem.8b00168
1748 9436 1 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding affinity to human P2Y14 expressed in CHO cellsBinding affinity to human P2Y14 expressed in CHO cells
ChEMBL 402 6 6 9 -2.5 O[C@@H]1[C@@H](COP(=O)(CP(=O)(O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1016/j.bmcl.2021.128137
44585949 9436 1 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding affinity to human P2Y14 expressed in CHO cellsBinding affinity to human P2Y14 expressed in CHO cells
ChEMBL 402 6 6 9 -2.5 O[C@@H]1[C@@H](COP(=O)(CP(=O)(O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1016/j.bmcl.2021.128137
CHEMBL507060 9436 1 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding affinity to human P2Y14 expressed in CHO cellsBinding affinity to human P2Y14 expressed in CHO cells
ChEMBL 402 6 6 9 -2.5 O[C@@H]1[C@@H](COP(=O)(CP(=O)(O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O 10.1016/j.bmcl.2021.128137
156012972 184293 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Inhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7.4 by flow cytomtery based competitive fluorescence assayInhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7.4 by flow cytomtery based competitive fluorescence assay
ChEMBL 481 5 3 5 5.1 O=C(O)c1[nH]c(-c2ccc(C3CCNCC3)cc2)cc1-c1cn(-c2ccc(C(F)(F)F)cc2)nn1 10.1021/acs.jmedchem.0c00745
CHEMBL4639693 184293 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Inhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7.4 by flow cytomtery based competitive fluorescence assayInhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7.4 by flow cytomtery based competitive fluorescence assay
ChEMBL 481 5 3 5 5.1 O=C(O)c1[nH]c(-c2ccc(C3CCNCC3)cc2)cc1-c1cn(-c2ccc(C(F)(F)F)cc2)nn1 10.1021/acs.jmedchem.0c00745
CHEMBL5074788 221112 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of fluorescent antagonist binding to human P2Y14R expressed in CHO cells preincubated for 30 mins followed by 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy 6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate addition and measured after 30 mins by BD FACSCalibur flow cytometry analysisInhibition of fluorescent antagonist binding to human P2Y14R expressed in CHO cells preincubated for 30 mins followed by 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy 6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate addition and measured after 30 mins by BD FACSCalibur flow cytometry analysis
ChEMBL None None None O=C(O)c1cc(-c2ccc([C@]3(O)C[C@H]4CC[C@@H]3CN4)cc2)c2ccc(-c3ccc(C(F)(F)F)cc3)cc2c1 10.1021/acs.jmedchem.1c01964
135357071 178414 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of 6-Amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy-6-(4-(trifluoromethyl)phenyl)-naphthalen-1-yl)phenyl)piperidin-1-yl)-butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)-phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate from human P2Y14R expressed in CHO cells measured after 15 mins by flow cytometric analysisDisplacement of 6-Amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy-6-(4-(trifluoromethyl)phenyl)-naphthalen-1-yl)phenyl)piperidin-1-yl)-butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)-phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate from human P2Y14R expressed in CHO cells measured after 15 mins by flow cytometric analysis
ChEMBL 502 5 2 5 5.5 O=C(O)c1cc(-c2ccc(C3CCNCC3)cc2)cc(-n2cc(-c3ccc(Br)cc3)nn2)c1 10.1021/acs.jmedchem.6b00044
CHEMBL4465763 178414 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of 6-Amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy-6-(4-(trifluoromethyl)phenyl)-naphthalen-1-yl)phenyl)piperidin-1-yl)-butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)-phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate from human P2Y14R expressed in CHO cells measured after 15 mins by flow cytometric analysisDisplacement of 6-Amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy-6-(4-(trifluoromethyl)phenyl)-naphthalen-1-yl)phenyl)piperidin-1-yl)-butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)-phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate from human P2Y14R expressed in CHO cells measured after 15 mins by flow cytometric analysis
ChEMBL 502 5 2 5 5.5 O=C(O)c1cc(-c2ccc(C3CCNCC3)cc2)cc(-n2cc(-c3ccc(Br)cc3)nn2)c1 10.1021/acs.jmedchem.6b00044
139392339 184106 0 None - 1 Mouse 5.9 pIC50 = 5.9 Binding
Inhibition of MRS4174 binding to mouse P2Y14R expressed in HEK293 cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins by flow cytomtery based competitive fluorescence assayInhibition of MRS4174 binding to mouse P2Y14R expressed in HEK293 cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins by flow cytomtery based competitive fluorescence assay
ChEMBL 504 5 2 5 5.6 O=C(O)c1cc(-c2ccc(C34CCNCC3C4)cc2)cc(-n2cc(-c3ccc(C(F)(F)F)cc3)nn2)c1 10.1021/acs.jmedchem.0c00745
CHEMBL4637158 184106 0 None - 1 Mouse 5.9 pIC50 = 5.9 Binding
Inhibition of MRS4174 binding to mouse P2Y14R expressed in HEK293 cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins by flow cytomtery based competitive fluorescence assayInhibition of MRS4174 binding to mouse P2Y14R expressed in HEK293 cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins by flow cytomtery based competitive fluorescence assay
ChEMBL 504 5 2 5 5.6 O=C(O)c1cc(-c2ccc(C34CCNCC3C4)cc2)cc(-n2cc(-c3ccc(C(F)(F)F)cc3)nn2)c1 10.1021/acs.jmedchem.0c00745
CHEMBL5083835 221665 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of fluorescent antagonist binding to human P2Y14R expressed in CHO cells preincubated for 30 mins followed by 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy 6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate addition and measured after 30 mins by BD FACSCalibur flow cytometry analysisInhibition of fluorescent antagonist binding to human P2Y14R expressed in CHO cells preincubated for 30 mins followed by 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy 6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate addition and measured after 30 mins by BD FACSCalibur flow cytometry analysis
ChEMBL None None None O=C(O)c1cc(-c2ccc([C@@]3(O)C[C@H]4CC[C@@H](C3)N4)cc2)c2ccc(-c3ccc(C(F)(F)F)cc3)cc2c1 10.1021/acs.jmedchem.1c01964
145966990 171171 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric methodDisplacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric method
ChEMBL 539 8 3 9 3.9 NCCCNC(=O)c1ccc(-c2cc(-c3nnn[nH]3)cc(-n3cc(-c4ccc(C(F)(F)F)cc4)nn3)c2)s1 10.1021/acs.jmedchem.8b00168
CHEMBL4213231 171171 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric methodDisplacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric method
ChEMBL 539 8 3 9 3.9 NCCCNC(=O)c1ccc(-c2cc(-c3nnn[nH]3)cc(-n3cc(-c4ccc(C(F)(F)F)cc4)nn3)c2)s1 10.1021/acs.jmedchem.8b00168
CHEMBL5085145 221730 0 None - 2 Human 7.9 pIC50 = 7.9 Binding
Inhibition of fluorescent antagonist binding to human P2Y14R expressed in CHO cells preincubated for 30 mins followed by 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy 6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate addition and measured after 30 mins by BD FACSCalibur flow cytometry analysisInhibition of fluorescent antagonist binding to human P2Y14R expressed in CHO cells preincubated for 30 mins followed by 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy 6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate addition and measured after 30 mins by BD FACSCalibur flow cytometry analysis
ChEMBL None None None N[C@H]1C[C@@H](CO)[C@H](c2ccc(-c3cc(C(=O)O)cc4cc(-c5ccc(C(F)(F)F)cc5)ccc34)cc2)C1 10.1021/acs.jmedchem.1c01964
CHEMBL5077574 221286 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of fluorescent antagonist binding to human P2Y14R expressed in CHO cells preincubated for 30 mins followed by 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy 6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate addition and measured after 30 mins by BD FACSCalibur flow cytometry analysisInhibition of fluorescent antagonist binding to human P2Y14R expressed in CHO cells preincubated for 30 mins followed by 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy 6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate addition and measured after 30 mins by BD FACSCalibur flow cytometry analysis
ChEMBL None None None N[C@H]1C[C@@H](CO)C[C@@H]1c1ccc(-c2cc(C(=O)O)cc3cc(-c4ccc(C(F)(F)F)cc4)ccc23)cc1 10.1021/acs.jmedchem.1c01964
145971541 171250 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Displacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric methodDisplacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric method
ChEMBL 527 5 2 7 4.4 O=C(O)c1cc(-c2ccc(C(=O)N3CCNCC3)s2)cc(-n2cc(-c3ccc(C(F)(F)F)cc3)nn2)c1 10.1021/acs.jmedchem.8b00168
CHEMBL4214132 171250 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Displacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric methodDisplacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric method
ChEMBL 527 5 2 7 4.4 O=C(O)c1cc(-c2ccc(C(=O)N3CCNCC3)s2)cc(-n2cc(-c3ccc(C(F)(F)F)cc3)nn2)c1 10.1021/acs.jmedchem.8b00168
164585459 191750 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysisInhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysis
ChEMBL 466 6 2 5 4.3 NC(=O)Cc1ccc(-c2cc(C(=O)O)cc(-n3cc(-c4ccc(C(F)(F)F)cc4)nn3)c2)cc1 10.1021/acs.jmedchem.1c00164
CHEMBL4854060 191750 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysisInhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysis
ChEMBL 466 6 2 5 4.3 NC(=O)Cc1ccc(-c2cc(C(=O)O)cc(-n3cc(-c4ccc(C(F)(F)F)cc4)nn3)c2)cc1 10.1021/acs.jmedchem.1c00164
CHEMBL5074765 221111 0 None - 2 Mouse 7.9 pIC50 = 7.9 Binding
Inhibition of fluorescent antagonist binding to mouse P2Y14R expressed in HEK293 cells preincubated for 30 mins followed by addition of 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy-6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate incubated for 30 mins by BD FACSCalibur flow cytometry analysisInhibition of fluorescent antagonist binding to mouse P2Y14R expressed in HEK293 cells preincubated for 30 mins followed by addition of 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy-6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate incubated for 30 mins by BD FACSCalibur flow cytometry analysis
ChEMBL None None None O=C(O)c1cc(-c2ccc([C@@H]3C[C@@H]4C[C@H]3CN4)cc2)c2ccc(-c3ccc(C(F)(F)F)cc3)cc2c1 10.1021/acs.jmedchem.1c01964
139392057 171110 0 None - 0 Mouse 6.9 pIC50 = 6.9 Binding
Displacement of Alexafluor488 labeled 4-(4-(1-(4-(1-(6-(4-(6-amino-3-imino-4,5-disulfo-3H-xanthen-9-yl)-3-carboxybenzamido)hexyl)-1H-1,2,3-triazol-4-yl)butyl)piperidin-4-yl)phenyl)-7-(4-(trifluoromethyl)phenyl)-2-naphthoic acid from HA-tagged mouse P2Y14 expressed in HEK293 cells measured after 30 mins by FACScalibur flow cytometry analysisDisplacement of Alexafluor488 labeled 4-(4-(1-(4-(1-(6-(4-(6-amino-3-imino-4,5-disulfo-3H-xanthen-9-yl)-3-carboxybenzamido)hexyl)-1H-1,2,3-triazol-4-yl)butyl)piperidin-4-yl)phenyl)-7-(4-(trifluoromethyl)phenyl)-2-naphthoic acid from HA-tagged mouse P2Y14 expressed in HEK293 cells measured after 30 mins by FACScalibur flow cytometry analysis
ChEMBL 555 8 1 2 8.9 C#CCCCCN1CCC(c2ccc(-c3cc(C(=O)O)cc4cc(-c5ccc(C(F)(F)F)cc5)ccc34)cc2)CC1 10.1021/acsmedchemlett.0c00115
CHEMBL4212441 171110 0 None - 0 Mouse 6.9 pIC50 = 6.9 Binding
Displacement of Alexafluor488 labeled 4-(4-(1-(4-(1-(6-(4-(6-amino-3-imino-4,5-disulfo-3H-xanthen-9-yl)-3-carboxybenzamido)hexyl)-1H-1,2,3-triazol-4-yl)butyl)piperidin-4-yl)phenyl)-7-(4-(trifluoromethyl)phenyl)-2-naphthoic acid from HA-tagged mouse P2Y14 expressed in HEK293 cells measured after 30 mins by FACScalibur flow cytometry analysisDisplacement of Alexafluor488 labeled 4-(4-(1-(4-(1-(6-(4-(6-amino-3-imino-4,5-disulfo-3H-xanthen-9-yl)-3-carboxybenzamido)hexyl)-1H-1,2,3-triazol-4-yl)butyl)piperidin-4-yl)phenyl)-7-(4-(trifluoromethyl)phenyl)-2-naphthoic acid from HA-tagged mouse P2Y14 expressed in HEK293 cells measured after 30 mins by FACScalibur flow cytometry analysis
ChEMBL 555 8 1 2 8.9 C#CCCCCN1CCC(c2ccc(-c3cc(C(=O)O)cc4cc(-c5ccc(C(F)(F)F)cc5)ccc34)cc2)CC1 10.1021/acsmedchemlett.0c00115
139392057 171110 0 None - 0 Mouse 6.9 pIC50 = 6.9 Binding
Inhibition of MRS4174 binding to mouse P2Y14R expressed in HEK293 cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins by flow cytomtery based competitive fluorescence assayInhibition of MRS4174 binding to mouse P2Y14R expressed in HEK293 cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins by flow cytomtery based competitive fluorescence assay
ChEMBL 555 8 1 2 8.9 C#CCCCCN1CCC(c2ccc(-c3cc(C(=O)O)cc4cc(-c5ccc(C(F)(F)F)cc5)ccc34)cc2)CC1 10.1021/acs.jmedchem.0c00745
CHEMBL4212441 171110 0 None - 0 Mouse 6.9 pIC50 = 6.9 Binding
Inhibition of MRS4174 binding to mouse P2Y14R expressed in HEK293 cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins by flow cytomtery based competitive fluorescence assayInhibition of MRS4174 binding to mouse P2Y14R expressed in HEK293 cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins by flow cytomtery based competitive fluorescence assay
ChEMBL 555 8 1 2 8.9 C#CCCCCN1CCC(c2ccc(-c3cc(C(=O)O)cc4cc(-c5ccc(C(F)(F)F)cc5)ccc34)cc2)CC1 10.1021/acs.jmedchem.0c00745
155525420 177898 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of 6-Amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy-6-(4-(trifluoromethyl)phenyl)-naphthalen-1-yl)phenyl)piperidin-1-yl)-butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)-phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate from human P2Y14R expressed in CHO cells measured after 15 mins by flow cytometric analysisDisplacement of 6-Amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy-6-(4-(trifluoromethyl)phenyl)-naphthalen-1-yl)phenyl)piperidin-1-yl)-butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)-phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate from human P2Y14R expressed in CHO cells measured after 15 mins by flow cytometric analysis
ChEMBL 508 6 2 6 5.7 O=C(O)c1cc(-c2ccc(C3CCNCC3)cc2)cc(-n2cc(-c3ccc(OC(F)(F)F)cc3)nn2)c1 10.1021/acs.jmedchem.6b00044
CHEMBL4458050 177898 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of 6-Amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy-6-(4-(trifluoromethyl)phenyl)-naphthalen-1-yl)phenyl)piperidin-1-yl)-butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)-phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate from human P2Y14R expressed in CHO cells measured after 15 mins by flow cytometric analysisDisplacement of 6-Amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy-6-(4-(trifluoromethyl)phenyl)-naphthalen-1-yl)phenyl)piperidin-1-yl)-butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)-phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate from human P2Y14R expressed in CHO cells measured after 15 mins by flow cytometric analysis
ChEMBL 508 6 2 6 5.7 O=C(O)c1cc(-c2ccc(C3CCNCC3)cc2)cc(-n2cc(-c3ccc(OC(F)(F)F)cc3)nn2)c1 10.1021/acs.jmedchem.6b00044
139392365 184836 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7.4 by flow cytomtery based competitive fluorescence assayInhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7.4 by flow cytomtery based competitive fluorescence assay
ChEMBL 559 9 1 2 9.7 CCCCCCN1CCC(c2ccc(-c3cc(C(=O)O)cc4cc(-c5ccc(C(F)(F)F)cc5)ccc34)cc2)CC1 10.1021/acs.jmedchem.0c00745
CHEMBL4647290 184836 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7.4 by flow cytomtery based competitive fluorescence assayInhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7.4 by flow cytomtery based competitive fluorescence assay
ChEMBL 559 9 1 2 9.7 CCCCCCN1CCC(c2ccc(-c3cc(C(=O)O)cc4cc(-c5ccc(C(F)(F)F)cc5)ccc34)cc2)CC1 10.1021/acs.jmedchem.0c00745
145973771 171498 0 None - 7 Human 6.9 pIC50 = 6.9 Binding
Displacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric methodDisplacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric method
ChEMBL 797 16 2 7 10.8 CC(C)(C)OC(=O)NCCCCCCn1cc(CCCCN2CCC(c3ccc(-c4cc(C(=O)O)cc5cc(-c6ccc(C(F)(F)F)cc6)ccc45)cc3)CC2)nn1 10.1021/acs.jmedchem.8b00168
CHEMBL4217398 171498 0 None - 7 Human 6.9 pIC50 = 6.9 Binding
Displacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric methodDisplacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric method
ChEMBL 797 16 2 7 10.8 CC(C)(C)OC(=O)NCCCCCCn1cc(CCCCN2CCC(c3ccc(-c4cc(C(=O)O)cc5cc(-c6ccc(C(F)(F)F)cc6)ccc45)cc3)CC2)nn1 10.1021/acs.jmedchem.8b00168
139392135 184740 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7.4 by flow cytomtery based competitive fluorescence assayInhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7.4 by flow cytomtery based competitive fluorescence assay
ChEMBL 517 6 1 2 8.5 CCCN1CCC(c2ccc(-c3cc(C(=O)O)cc4cc(-c5ccc(C(F)(F)F)cc5)ccc34)cc2)CC1 10.1021/acs.jmedchem.0c00745
CHEMBL4645854 184740 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7.4 by flow cytomtery based competitive fluorescence assayInhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7.4 by flow cytomtery based competitive fluorescence assay
ChEMBL 517 6 1 2 8.5 CCCN1CCC(c2ccc(-c3cc(C(=O)O)cc4cc(-c5ccc(C(F)(F)F)cc5)ccc34)cc2)CC1 10.1021/acs.jmedchem.0c00745
145965191 170876 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Displacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric methodDisplacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric method
ChEMBL 665 11 3 9 6.0 CC(C)(C)OC(=O)NCCCCNS(=O)(=O)c1ccc(-c2cc(C(=O)O)cc(-n3cc(-c4ccc(C(F)(F)F)cc4)nn3)c2)s1 10.1021/acs.jmedchem.8b00168
CHEMBL4209607 170876 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Displacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric methodDisplacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric method
ChEMBL 665 11 3 9 6.0 CC(C)(C)OC(=O)NCCCCNS(=O)(=O)c1ccc(-c2cc(C(=O)O)cc(-n3cc(-c4ccc(C(F)(F)F)cc4)nn3)c2)s1 10.1021/acs.jmedchem.8b00168
139392069 184237 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7.4 by flow cytomtery based competitive fluorescence assayInhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7.4 by flow cytomtery based competitive fluorescence assay
ChEMBL 513 5 1 2 7.7 C#CCN1CCC(c2ccc(-c3cc(C(=O)O)cc4cc(-c5ccc(C(F)(F)F)cc5)ccc34)cc2)CC1 10.1021/acs.jmedchem.0c00745
CHEMBL4638909 184237 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7.4 by flow cytomtery based competitive fluorescence assayInhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7.4 by flow cytomtery based competitive fluorescence assay
ChEMBL 513 5 1 2 7.7 C#CCN1CCC(c2ccc(-c3cc(C(=O)O)cc4cc(-c5ccc(C(F)(F)F)cc5)ccc34)cc2)CC1 10.1021/acs.jmedchem.0c00745
42628974 68836 0 None - 0 Mouse 7.9 pIC50 = 7.9 Binding
Inhibition of mouse P2Y14 receptorInhibition of mouse P2Y14 receptor
ChEMBL 406 5 1 3 6.6 Cc1cc(F)cc(C)c1COc1ccc2c(-c3ccsc3)cc(C(=O)O)cc2c1 10.1016/j.ejmech.2019.04.068
CHEMBL1774892 68836 0 None - 0 Mouse 7.9 pIC50 = 7.9 Binding
Inhibition of mouse P2Y14 receptorInhibition of mouse P2Y14 receptor
ChEMBL 406 5 1 3 6.6 Cc1cc(F)cc(C)c1COc1ccc2c(-c3ccsc3)cc(C(=O)O)cc2c1 10.1016/j.ejmech.2019.04.068
42611190 9930 12 None -1 5 Human 7.8 pIC50 = 7.8 Binding
Inhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 6.5 by flow cytomtery based competitive fluorescence assayInhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 6.5 by flow cytomtery based competitive fluorescence assay
ChEMBL 475 4 2 2 7.4 OC(=O)c1cc2cc(ccc2c(c1)c1ccc(cc1)C1CCNCC1)c1ccc(cc1)C(F)(F)F 10.1021/acs.jmedchem.0c00745
5802 9930 12 None -1 5 Human 7.8 pIC50 = 7.8 Binding
Inhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 6.5 by flow cytomtery based competitive fluorescence assayInhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 6.5 by flow cytomtery based competitive fluorescence assay
ChEMBL 475 4 2 2 7.4 OC(=O)c1cc2cc(ccc2c(c1)c1ccc(cc1)C1CCNCC1)c1ccc(cc1)C(F)(F)F 10.1021/acs.jmedchem.0c00745
CHEMBL1800685 9930 12 None -1 5 Human 7.8 pIC50 = 7.8 Binding
Inhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 6.5 by flow cytomtery based competitive fluorescence assayInhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 6.5 by flow cytomtery based competitive fluorescence assay
ChEMBL 475 4 2 2 7.4 OC(=O)c1cc2cc(ccc2c(c1)c1ccc(cc1)C1CCNCC1)c1ccc(cc1)C(F)(F)F 10.1021/acs.jmedchem.0c00745
145946839 174364 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric methodDisplacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric method
ChEMBL 453 5 2 6 3.8 NC(=O)c1ccc(-c2cc(C(=O)O)cc(-n3cc(-c4ccc(C(F)(F)F)cc4)nn3)c2)cn1 10.1021/acs.jmedchem.8b00168
CHEMBL4207803 174364 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric methodDisplacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric method
ChEMBL 453 5 2 6 3.8 NC(=O)c1ccc(-c2cc(C(=O)O)cc(-n3cc(-c4ccc(C(F)(F)F)cc4)nn3)c2)cn1 10.1021/acs.jmedchem.8b00168
CHEMBL4300744 174364 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric methodDisplacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric method
ChEMBL 453 5 2 6 3.8 NC(=O)c1ccc(-c2cc(C(=O)O)cc(-n3cc(-c4ccc(C(F)(F)F)cc4)nn3)c2)cn1 10.1021/acs.jmedchem.8b00168
156021071 184944 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7.4 by flow cytomtery based competitive fluorescence assayInhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7.4 by flow cytomtery based competitive fluorescence assay
ChEMBL 825 25 1 9 7.7 COCCOCCOCCOCCOCCOCCOCCC(=O)N1CCC(c2ccc(-c3cc(C(=O)O)cc4cc(-c5ccc(C(F)(F)F)cc5)ccc34)cc2)CC1 10.1021/acs.jmedchem.0c00745
CHEMBL4649076 184944 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7.4 by flow cytomtery based competitive fluorescence assayInhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7.4 by flow cytomtery based competitive fluorescence assay
ChEMBL 825 25 1 9 7.7 COCCOCCOCCOCCOCCOCCOCCC(=O)N1CCC(c2ccc(-c3cc(C(=O)O)cc4cc(-c5ccc(C(F)(F)F)cc5)ccc34)cc2)CC1 10.1021/acs.jmedchem.0c00745
164585355 192089 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Inhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysisInhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysis
ChEMBL 464 5 2 5 5.3 NC1(c2ccc(-c3cc(C(=O)O)cc(-n4cc(-c5ccc(C(F)(F)F)cc5)nn4)c3)cc2)CC1 10.1021/acs.jmedchem.1c00164
CHEMBL4859398 192089 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Inhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysisInhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysis
ChEMBL 464 5 2 5 5.3 NC1(c2ccc(-c3cc(C(=O)O)cc(-n4cc(-c5ccc(C(F)(F)F)cc5)nn4)c3)cc2)CC1 10.1021/acs.jmedchem.1c00164
132280527 177674 1 None - 0 Mouse 6.9 pIC50 = 6.9 Binding
Displacement of Alexafluor488 labeled 4-(4-(1-(4-(1-(6-(4-(6-amino-3-imino-4,5-disulfo-3H-xanthen-9-yl)-3-carboxybenzamido)hexyl)-1H-1,2,3-triazol-4-yl)butyl)piperidin-4-yl)phenyl)-7-(4-(trifluoromethyl)phenyl)-2-naphthoic acid from HA-tagged mouse P2Y14 expressed in HEK293 cells measured after 30 mins by FACScalibur flow cytometry analysisDisplacement of Alexafluor488 labeled 4-(4-(1-(4-(1-(6-(4-(6-amino-3-imino-4,5-disulfo-3H-xanthen-9-yl)-3-carboxybenzamido)hexyl)-1H-1,2,3-triazol-4-yl)butyl)piperidin-4-yl)phenyl)-7-(4-(trifluoromethyl)phenyl)-2-naphthoic acid from HA-tagged mouse P2Y14 expressed in HEK293 cells measured after 30 mins by FACScalibur flow cytometry analysis
ChEMBL 492 5 2 5 5.8 O=C(O)c1cc(-c2ccc(C3CCNCC3)cc2)cc(-n2cc(-c3ccc(C(F)(F)F)cc3)nn2)c1 10.1021/acsmedchemlett.0c00115
CHEMBL4454538 177674 1 None - 0 Mouse 6.9 pIC50 = 6.9 Binding
Displacement of Alexafluor488 labeled 4-(4-(1-(4-(1-(6-(4-(6-amino-3-imino-4,5-disulfo-3H-xanthen-9-yl)-3-carboxybenzamido)hexyl)-1H-1,2,3-triazol-4-yl)butyl)piperidin-4-yl)phenyl)-7-(4-(trifluoromethyl)phenyl)-2-naphthoic acid from HA-tagged mouse P2Y14 expressed in HEK293 cells measured after 30 mins by FACScalibur flow cytometry analysisDisplacement of Alexafluor488 labeled 4-(4-(1-(4-(1-(6-(4-(6-amino-3-imino-4,5-disulfo-3H-xanthen-9-yl)-3-carboxybenzamido)hexyl)-1H-1,2,3-triazol-4-yl)butyl)piperidin-4-yl)phenyl)-7-(4-(trifluoromethyl)phenyl)-2-naphthoic acid from HA-tagged mouse P2Y14 expressed in HEK293 cells measured after 30 mins by FACScalibur flow cytometry analysis
ChEMBL 492 5 2 5 5.8 O=C(O)c1cc(-c2ccc(C3CCNCC3)cc2)cc(-n2cc(-c3ccc(C(F)(F)F)cc3)nn2)c1 10.1021/acsmedchemlett.0c00115
132280527 177674 1 None - 0 Mouse 6.9 pIC50 = 6.9 Binding
Inhibition of MRS4174 binding to mouse P2Y14R expressed in HEK293 cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins by flow cytomtery based competitive fluorescence assayInhibition of MRS4174 binding to mouse P2Y14R expressed in HEK293 cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins by flow cytomtery based competitive fluorescence assay
ChEMBL 492 5 2 5 5.8 O=C(O)c1cc(-c2ccc(C3CCNCC3)cc2)cc(-n2cc(-c3ccc(C(F)(F)F)cc3)nn2)c1 10.1021/acs.jmedchem.0c00745
CHEMBL4454538 177674 1 None - 0 Mouse 6.9 pIC50 = 6.9 Binding
Inhibition of MRS4174 binding to mouse P2Y14R expressed in HEK293 cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins by flow cytomtery based competitive fluorescence assayInhibition of MRS4174 binding to mouse P2Y14R expressed in HEK293 cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins by flow cytomtery based competitive fluorescence assay
ChEMBL 492 5 2 5 5.8 O=C(O)c1cc(-c2ccc(C3CCNCC3)cc2)cc(-n2cc(-c3ccc(C(F)(F)F)cc3)nn2)c1 10.1021/acs.jmedchem.0c00745
164585341 193289 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysisInhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysis
ChEMBL 424 4 2 5 4.9 Nc1ccc(-c2cc(C(=O)O)cc(-n3cc(-c4ccc(C(F)(F)F)cc4)nn3)c2)cc1 10.1021/acs.jmedchem.1c00164
CHEMBL4877496 193289 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysisInhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysis
ChEMBL 424 4 2 5 4.9 Nc1ccc(-c2cc(C(=O)O)cc(-n3cc(-c4ccc(C(F)(F)F)cc4)nn3)c2)cc1 10.1021/acs.jmedchem.1c00164
145946622 174340 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric methodDisplacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric method
ChEMBL 494 7 2 5 5.5 CCCNC(=O)c1ccc(-c2cc(C(=O)O)cc(-n3cc(-c4ccc(C(F)(F)F)cc4)nn3)c2)cc1 10.1021/acs.jmedchem.8b00168
CHEMBL4216270 174340 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric methodDisplacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric method
ChEMBL 494 7 2 5 5.5 CCCNC(=O)c1ccc(-c2cc(C(=O)O)cc(-n3cc(-c4ccc(C(F)(F)F)cc4)nn3)c2)cc1 10.1021/acs.jmedchem.8b00168
CHEMBL4300426 174340 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric methodDisplacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric method
ChEMBL 494 7 2 5 5.5 CCCNC(=O)c1ccc(-c2cc(C(=O)O)cc(-n3cc(-c4ccc(C(F)(F)F)cc4)nn3)c2)cc1 10.1021/acs.jmedchem.8b00168
164585602 192418 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysisInhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysis
ChEMBL 489 5 2 4 7.0 O=C(O)c1cc(-c2ccc(-c3cc(CO)on3)cc2)c2ccc(-c3ccc(C(F)(F)F)cc3)cc2c1 10.1021/acs.jmedchem.1c00164
CHEMBL4864408 192418 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysisInhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysis
ChEMBL 489 5 2 4 7.0 O=C(O)c1cc(-c2ccc(-c3cc(CO)on3)cc2)c2ccc(-c3ccc(C(F)(F)F)cc3)cc2c1 10.1021/acs.jmedchem.1c00164
CHEMBL5079102 221386 0 None - 0 Mouse 7.8 pIC50 = 7.8 Binding
Inhibition of fluorescent antagonist binding to mouse P2Y14R expressed in HEK293 cells preincubated for 30 mins followed by addition of 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy-6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate incubated for 30 mins by BD FACSCalibur flow cytometry analysisInhibition of fluorescent antagonist binding to mouse P2Y14R expressed in HEK293 cells preincubated for 30 mins followed by addition of 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy-6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate incubated for 30 mins by BD FACSCalibur flow cytometry analysis
ChEMBL None None None O=C(O)c1cc(-c2ccc(C3(O)[C@H]4CC[C@H]3CNC4)cc2)c2ccc(-c3ccc(C(F)(F)F)cc3)cc2c1 10.1021/acs.jmedchem.1c01964
CHEMBL5092515 222153 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of fluorescent antagonist binding to human P2Y14R expressed in CHO cells preincubated for 30 mins followed by 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy 6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate addition and measured after 30 mins by BD FACSCalibur flow cytometry analysisInhibition of fluorescent antagonist binding to human P2Y14R expressed in CHO cells preincubated for 30 mins followed by 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy 6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate addition and measured after 30 mins by BD FACSCalibur flow cytometry analysis
ChEMBL None None None O=C(O)c1cc(-c2ccc([C@@]3(O)C[C@H]4CC[C@@H]3CN4)cc2)c2ccc(-c3ccc(C(F)(F)F)cc3)cc2c1 10.1021/acs.jmedchem.1c01964
145968000 171580 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric methodDisplacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric method
ChEMBL 563 6 2 8 4.0 O=C(O)c1cc(-c2ccc(S(=O)(=O)N3CCNCC3)s2)cc(-n2cc(-c3ccc(C(F)(F)F)cc3)nn2)c1 10.1021/acs.jmedchem.8b00168
CHEMBL4218414 171580 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric methodDisplacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric method
ChEMBL 563 6 2 8 4.0 O=C(O)c1cc(-c2ccc(S(=O)(=O)N3CCNCC3)s2)cc(-n2cc(-c3ccc(C(F)(F)F)cc3)nn2)c1 10.1021/acs.jmedchem.8b00168
164585437 192960 0 None - 1 Mouse 6.8 pIC50 = 6.8 Binding
Inhibition of fluorescent antagonist binding to mouse P2Y14 receptor expressed in HEK293 cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysisInhibition of fluorescent antagonist binding to mouse P2Y14 receptor expressed in HEK293 cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysis
ChEMBL 535 6 3 6 5.3 O=C(O)c1cc(-c2ccc(NC(=O)C3CCNCC3)cc2)cc(-n2cc(-c3ccc(C(F)(F)F)cc3)nn2)c1 10.1021/acs.jmedchem.1c00164
CHEMBL4872692 192960 0 None - 1 Mouse 6.8 pIC50 = 6.8 Binding
Inhibition of fluorescent antagonist binding to mouse P2Y14 receptor expressed in HEK293 cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysisInhibition of fluorescent antagonist binding to mouse P2Y14 receptor expressed in HEK293 cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysis
ChEMBL 535 6 3 6 5.3 O=C(O)c1cc(-c2ccc(NC(=O)C3CCNCC3)cc2)cc(-n2cc(-c3ccc(C(F)(F)F)cc3)nn2)c1 10.1021/acs.jmedchem.1c00164
145978299 170505 0 None - 0 Mouse 5.8 pIC50 = 5.8 Binding
Displacement of Alexafluor488 labeled 4-(4-(1-(4-(1-(6-(4-(6-amino-3-imino-4,5-disulfo-3H-xanthen-9-yl)-3-carboxybenzamido)hexyl)-1H-1,2,3-triazol-4-yl)butyl)piperidin-4-yl)phenyl)-7-(4-(trifluoromethyl)phenyl)-2-naphthoic acid from HA-tagged mouse P2Y14 expressed in HEK293 cells measured after 30 mins by FACScalibur flow cytometry analysisDisplacement of Alexafluor488 labeled 4-(4-(1-(4-(1-(6-(4-(6-amino-3-imino-4,5-disulfo-3H-xanthen-9-yl)-3-carboxybenzamido)hexyl)-1H-1,2,3-triazol-4-yl)butyl)piperidin-4-yl)phenyl)-7-(4-(trifluoromethyl)phenyl)-2-naphthoic acid from HA-tagged mouse P2Y14 expressed in HEK293 cells measured after 30 mins by FACScalibur flow cytometry analysis
ChEMBL 332 2 2 2 4.9 O=C(O)c1cc(O)c2ccc(-c3ccc(C(F)(F)F)cc3)cc2c1 10.1021/acsmedchemlett.0c00115
CHEMBL4205190 170505 0 None - 0 Mouse 5.8 pIC50 = 5.8 Binding
Displacement of Alexafluor488 labeled 4-(4-(1-(4-(1-(6-(4-(6-amino-3-imino-4,5-disulfo-3H-xanthen-9-yl)-3-carboxybenzamido)hexyl)-1H-1,2,3-triazol-4-yl)butyl)piperidin-4-yl)phenyl)-7-(4-(trifluoromethyl)phenyl)-2-naphthoic acid from HA-tagged mouse P2Y14 expressed in HEK293 cells measured after 30 mins by FACScalibur flow cytometry analysisDisplacement of Alexafluor488 labeled 4-(4-(1-(4-(1-(6-(4-(6-amino-3-imino-4,5-disulfo-3H-xanthen-9-yl)-3-carboxybenzamido)hexyl)-1H-1,2,3-triazol-4-yl)butyl)piperidin-4-yl)phenyl)-7-(4-(trifluoromethyl)phenyl)-2-naphthoic acid from HA-tagged mouse P2Y14 expressed in HEK293 cells measured after 30 mins by FACScalibur flow cytometry analysis
ChEMBL 332 2 2 2 4.9 O=C(O)c1cc(O)c2ccc(-c3ccc(C(F)(F)F)cc3)cc2c1 10.1021/acsmedchemlett.0c00115
135356877 182712 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of 6-Amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy-6-(4-(trifluoromethyl)phenyl)-naphthalen-1-yl)phenyl)piperidin-1-yl)-butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)-phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate from human P2Y14R expressed in CHO cells measured after 15 mins by flow cytometric analysisDisplacement of 6-Amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy-6-(4-(trifluoromethyl)phenyl)-naphthalen-1-yl)phenyl)piperidin-1-yl)-butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)-phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate from human P2Y14R expressed in CHO cells measured after 15 mins by flow cytometric analysis
ChEMBL 510 10 2 6 6.3 CCCCCOc1ccc(-c2cn(-c3cc(C(=O)O)cc(-c4ccc(C5CCNCC5)cc4)c3)nn2)cc1 10.1021/acs.jmedchem.6b00044
CHEMBL4587611 182712 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of 6-Amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy-6-(4-(trifluoromethyl)phenyl)-naphthalen-1-yl)phenyl)piperidin-1-yl)-butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)-phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate from human P2Y14R expressed in CHO cells measured after 15 mins by flow cytometric analysisDisplacement of 6-Amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy-6-(4-(trifluoromethyl)phenyl)-naphthalen-1-yl)phenyl)piperidin-1-yl)-butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)-phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate from human P2Y14R expressed in CHO cells measured after 15 mins by flow cytometric analysis
ChEMBL 510 10 2 6 6.3 CCCCCOc1ccc(-c2cn(-c3cc(C(=O)O)cc(-c4ccc(C5CCNCC5)cc4)c3)nn2)cc1 10.1021/acs.jmedchem.6b00044
145974993 171540 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric methodDisplacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric method
ChEMBL 557 6 2 7 3.9 O=C(O)c1cc(-c2ccc(S(=O)(=O)N3CCNCC3)cc2)cc(-n2cc(-c3ccc(C(F)(F)F)cc3)nn2)c1 10.1021/acs.jmedchem.8b00168
CHEMBL4217880 171540 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric methodDisplacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric method
ChEMBL 557 6 2 7 3.9 O=C(O)c1cc(-c2ccc(S(=O)(=O)N3CCNCC3)cc2)cc(-n2cc(-c3ccc(C(F)(F)F)cc3)nn2)c1 10.1021/acs.jmedchem.8b00168
145977566 170432 1 None - 0 Human 4.8 pIC50 = 4.8 Binding
Displacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric methodDisplacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric method
ChEMBL 349 3 2 5 3.4 O=C(O)c1cc(O)cc(-n2cc(-c3ccc(C(F)(F)F)cc3)nn2)c1 10.1021/acs.jmedchem.8b00168
CHEMBL4204323 170432 1 None - 0 Human 4.8 pIC50 = 4.8 Binding
Displacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric methodDisplacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric method
ChEMBL 349 3 2 5 3.4 O=C(O)c1cc(O)cc(-n2cc(-c3ccc(C(F)(F)F)cc3)nn2)c1 10.1021/acs.jmedchem.8b00168
CHEMBL5087161 221852 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibition of fluorescent antagonist binding to human P2Y14R expressed in CHO cells preincubated for 30 mins followed by 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy 6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate addition and measured after 30 mins by BD FACSCalibur flow cytometry analysisInhibition of fluorescent antagonist binding to human P2Y14R expressed in CHO cells preincubated for 30 mins followed by 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy 6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate addition and measured after 30 mins by BD FACSCalibur flow cytometry analysis
ChEMBL None None None N[C@@H]1C[C@H](C(=O)O)C[C@H]1c1ccc(-c2cc(C(=O)O)cc3cc(-c4ccc(C(F)(F)F)cc4)ccc23)cc1 10.1021/acs.jmedchem.1c01964
155549257 180590 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Binding affinity to human P2Y14 expressed in CHO cellsBinding affinity to human P2Y14 expressed in CHO cells
ChEMBL 436 6 6 9 -1.9 O=c1[nH]c(=O)n([C@@H]2O[C@H](COP(=O)(O)CP(=O)(O)O)[C@@H](O)[C@H]2O)cc1Cl 10.1016/j.bmcl.2021.128137
CHEMBL4538320 180590 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Binding affinity to human P2Y14 expressed in CHO cellsBinding affinity to human P2Y14 expressed in CHO cells
ChEMBL 436 6 6 9 -1.9 O=c1[nH]c(=O)n([C@@H]2O[C@H](COP(=O)(O)CP(=O)(O)O)[C@@H](O)[C@H]2O)cc1Cl 10.1016/j.bmcl.2021.128137
CHEMBL4849188 180590 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Binding affinity to human P2Y14 expressed in CHO cellsBinding affinity to human P2Y14 expressed in CHO cells
ChEMBL 436 6 6 9 -1.9 O=c1[nH]c(=O)n([C@@H]2O[C@H](COP(=O)(O)CP(=O)(O)O)[C@@H](O)[C@H]2O)cc1Cl 10.1016/j.bmcl.2021.128137
139406866 184490 0 None - 1 Human 5.8 pIC50 = 5.8 Binding
Inhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7.4 by flow cytomtery based competitive fluorescence assayInhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7.4 by flow cytomtery based competitive fluorescence assay
ChEMBL 452 5 2 5 4.4 NC(=O)c1ccc(-c2cc(C(=O)O)cc(-c3cn(-c4ccc(C(F)(F)F)cc4)nn3)c2)cc1 10.1021/acs.jmedchem.0c00745
CHEMBL4642215 184490 0 None - 1 Human 5.8 pIC50 = 5.8 Binding
Inhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7.4 by flow cytomtery based competitive fluorescence assayInhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7.4 by flow cytomtery based competitive fluorescence assay
ChEMBL 452 5 2 5 4.4 NC(=O)c1ccc(-c2cc(C(=O)O)cc(-c3cn(-c4ccc(C(F)(F)F)cc4)nn3)c2)cc1 10.1021/acs.jmedchem.0c00745
134611895 9447 4 None - 2 Human 6.8 pIC50 = 6.8 Binding
Displacement of Alexafluor488 labeled 4-(4-(1-(4-(1-(6-(4-(6-amino-3-imino-4,5-disulfo-3H-xanthen-9-yl)-3-carboxybenzamido)hexyl)-1H-1,2,3-triazol-4-yl)butyl)piperidin-4-yl)phenyl)-7-(4-(trifluoromethyl)phenyl)-2-naphthoic acid from human P2Y14 expressed in CHO cells measured after 30 mins by FACScalibur flow cytometry analysisDisplacement of Alexafluor488 labeled 4-(4-(1-(4-(1-(6-(4-(6-amino-3-imino-4,5-disulfo-3H-xanthen-9-yl)-3-carboxybenzamido)hexyl)-1H-1,2,3-triazol-4-yl)butyl)piperidin-4-yl)phenyl)-7-(4-(trifluoromethyl)phenyl)-2-naphthoic acid from human P2Y14 expressed in CHO cells measured after 30 mins by FACScalibur flow cytometry analysis
ChEMBL 515 8 3 7 4.5 NCCCNC(=O)c1ccc(s1)c1cc(cc(c1)n1nnc(c1)c1ccc(cc1)C(F)(F)F)C(=O)O 10.1021/acsmedchemlett.0c00115
9998 9447 4 None - 2 Human 6.8 pIC50 = 6.8 Binding
Displacement of Alexafluor488 labeled 4-(4-(1-(4-(1-(6-(4-(6-amino-3-imino-4,5-disulfo-3H-xanthen-9-yl)-3-carboxybenzamido)hexyl)-1H-1,2,3-triazol-4-yl)butyl)piperidin-4-yl)phenyl)-7-(4-(trifluoromethyl)phenyl)-2-naphthoic acid from human P2Y14 expressed in CHO cells measured after 30 mins by FACScalibur flow cytometry analysisDisplacement of Alexafluor488 labeled 4-(4-(1-(4-(1-(6-(4-(6-amino-3-imino-4,5-disulfo-3H-xanthen-9-yl)-3-carboxybenzamido)hexyl)-1H-1,2,3-triazol-4-yl)butyl)piperidin-4-yl)phenyl)-7-(4-(trifluoromethyl)phenyl)-2-naphthoic acid from human P2Y14 expressed in CHO cells measured after 30 mins by FACScalibur flow cytometry analysis
ChEMBL 515 8 3 7 4.5 NCCCNC(=O)c1ccc(s1)c1cc(cc(c1)n1nnc(c1)c1ccc(cc1)C(F)(F)F)C(=O)O 10.1021/acsmedchemlett.0c00115
CHEMBL4212721 9447 4 None - 2 Human 6.8 pIC50 = 6.8 Binding
Displacement of Alexafluor488 labeled 4-(4-(1-(4-(1-(6-(4-(6-amino-3-imino-4,5-disulfo-3H-xanthen-9-yl)-3-carboxybenzamido)hexyl)-1H-1,2,3-triazol-4-yl)butyl)piperidin-4-yl)phenyl)-7-(4-(trifluoromethyl)phenyl)-2-naphthoic acid from human P2Y14 expressed in CHO cells measured after 30 mins by FACScalibur flow cytometry analysisDisplacement of Alexafluor488 labeled 4-(4-(1-(4-(1-(6-(4-(6-amino-3-imino-4,5-disulfo-3H-xanthen-9-yl)-3-carboxybenzamido)hexyl)-1H-1,2,3-triazol-4-yl)butyl)piperidin-4-yl)phenyl)-7-(4-(trifluoromethyl)phenyl)-2-naphthoic acid from human P2Y14 expressed in CHO cells measured after 30 mins by FACScalibur flow cytometry analysis
ChEMBL 515 8 3 7 4.5 NCCCNC(=O)c1ccc(s1)c1cc(cc(c1)n1nnc(c1)c1ccc(cc1)C(F)(F)F)C(=O)O 10.1021/acsmedchemlett.0c00115
134611895 9447 4 None - 2 Human 6.8 pIC50 = 6.8 Binding
Displacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric methodDisplacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric method
ChEMBL 515 8 3 7 4.5 NCCCNC(=O)c1ccc(s1)c1cc(cc(c1)n1nnc(c1)c1ccc(cc1)C(F)(F)F)C(=O)O 10.1021/acs.jmedchem.8b00168
9998 9447 4 None - 2 Human 6.8 pIC50 = 6.8 Binding
Displacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric methodDisplacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric method
ChEMBL 515 8 3 7 4.5 NCCCNC(=O)c1ccc(s1)c1cc(cc(c1)n1nnc(c1)c1ccc(cc1)C(F)(F)F)C(=O)O 10.1021/acs.jmedchem.8b00168
CHEMBL4212721 9447 4 None - 2 Human 6.8 pIC50 = 6.8 Binding
Displacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric methodDisplacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric method
ChEMBL 515 8 3 7 4.5 NCCCNC(=O)c1ccc(s1)c1cc(cc(c1)n1nnc(c1)c1ccc(cc1)C(F)(F)F)C(=O)O 10.1021/acs.jmedchem.8b00168
164585582 192806 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysisInhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysis
ChEMBL 493 5 2 6 5.2 O=C(O)c1cc(-c2ccc(C3CCNCC3)cc2)cc(-n2cc(-c3ccc(C(F)(F)F)cc3)nn2)n1 10.1021/acs.jmedchem.1c00164
CHEMBL4870627 192806 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysisInhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysis
ChEMBL 493 5 2 6 5.2 O=C(O)c1cc(-c2ccc(C3CCNCC3)cc2)cc(-n2cc(-c3ccc(C(F)(F)F)cc3)nn2)n1 10.1021/acs.jmedchem.1c00164
CHEMBL5086827 221830 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of fluorescent antagonist binding to human P2Y14R expressed in CHO cells preincubated for 30 mins followed by 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy 6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate addition and measured after 30 mins by BD FACSCalibur flow cytometry analysisInhibition of fluorescent antagonist binding to human P2Y14R expressed in CHO cells preincubated for 30 mins followed by 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy 6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate addition and measured after 30 mins by BD FACSCalibur flow cytometry analysis
ChEMBL None None None CC1CC(c2ccc(-c3cc(C(=O)O)cc4cc(-c5ccc(C(F)(F)F)cc5)ccc34)cc2)CCN1 10.1021/acs.jmedchem.1c01964
CHEMBL5083619 221654 0 None - 0 Mouse 7.8 pIC50 = 7.8 Binding
Inhibition of fluorescent antagonist binding to mouse P2Y14R expressed in HEK293 cells preincubated for 30 mins followed by addition of 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy-6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate incubated for 30 mins by BD FACSCalibur flow cytometry analysisInhibition of fluorescent antagonist binding to mouse P2Y14R expressed in HEK293 cells preincubated for 30 mins followed by addition of 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy-6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate incubated for 30 mins by BD FACSCalibur flow cytometry analysis
ChEMBL None None None N[C@@H]1C[C@H](CO)[C@@H](c2ccc(-c3cc(C(=O)O)cc4cc(-c5ccc(C(F)(F)F)cc5)ccc34)cc2)C1 10.1021/acs.jmedchem.1c01964
145977136 170602 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric methodDisplacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric method
ChEMBL 515 8 3 7 4.5 NCCCNC(=O)c1cc(-c2cc(C(=O)O)cc(-n3cc(-c4ccc(C(F)(F)F)cc4)nn3)c2)cs1 10.1021/acs.jmedchem.8b00168
CHEMBL4206291 170602 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric methodDisplacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric method
ChEMBL 515 8 3 7 4.5 NCCCNC(=O)c1cc(-c2cc(C(=O)O)cc(-n3cc(-c4ccc(C(F)(F)F)cc4)nn3)c2)cs1 10.1021/acs.jmedchem.8b00168
164585426 193294 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Inhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysisInhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysis
ChEMBL 462 6 1 5 5.8 N#CCCc1ccc(-c2cc(C(=O)O)cc(-n3cc(-c4ccc(C(F)(F)F)cc4)nn3)c2)cc1 10.1021/acs.jmedchem.1c00164
CHEMBL4877577 193294 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Inhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysisInhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysis
ChEMBL 462 6 1 5 5.8 N#CCCc1ccc(-c2cc(C(=O)O)cc(-n3cc(-c4ccc(C(F)(F)F)cc4)nn3)c2)cc1 10.1021/acs.jmedchem.1c00164
139392457 184629 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7.4 by flow cytomtery based competitive fluorescence assayInhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7.4 by flow cytomtery based competitive fluorescence assay
ChEMBL 473 4 2 2 7.3 O=C(O)c1cc(-c2ccc(C3=CCNCC3)cc2)c2ccc(-c3ccc(C(F)(F)F)cc3)cc2c1 10.1021/acs.jmedchem.0c00745
CHEMBL4644135 184629 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7.4 by flow cytomtery based competitive fluorescence assayInhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7.4 by flow cytomtery based competitive fluorescence assay
ChEMBL 473 4 2 2 7.3 O=C(O)c1cc(-c2ccc(C3=CCNCC3)cc2)c2ccc(-c3ccc(C(F)(F)F)cc3)cc2c1 10.1021/acs.jmedchem.0c00745
164585602 192418 0 None - 0 Mouse 7.7 pIC50 = 7.7 Binding
Inhibition of fluorescent antagonist binding to mouse P2Y14 receptor expressed in HEK293 cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysisInhibition of fluorescent antagonist binding to mouse P2Y14 receptor expressed in HEK293 cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysis
ChEMBL 489 5 2 4 7.0 O=C(O)c1cc(-c2ccc(-c3cc(CO)on3)cc2)c2ccc(-c3ccc(C(F)(F)F)cc3)cc2c1 10.1021/acs.jmedchem.1c00164
CHEMBL4864408 192418 0 None - 0 Mouse 7.7 pIC50 = 7.7 Binding
Inhibition of fluorescent antagonist binding to mouse P2Y14 receptor expressed in HEK293 cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysisInhibition of fluorescent antagonist binding to mouse P2Y14 receptor expressed in HEK293 cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysis
ChEMBL 489 5 2 4 7.0 O=C(O)c1cc(-c2ccc(-c3cc(CO)on3)cc2)c2ccc(-c3ccc(C(F)(F)F)cc3)cc2c1 10.1021/acs.jmedchem.1c00164
164585622 191707 0 None - 2 Mouse 6.7 pIC50 = 6.7 Binding
Inhibition of fluorescent antagonist binding to mouse P2Y14 receptor expressed in HEK293 cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysisInhibition of fluorescent antagonist binding to mouse P2Y14 receptor expressed in HEK293 cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysis
ChEMBL 506 6 2 7 5.5 O=C(O)c1cc(-c2ccc(-c3cc(CO)on3)cc2)cc(-n2cc(-c3ccc(C(F)(F)F)cc3)nn2)c1 10.1021/acs.jmedchem.1c00164
CHEMBL4853466 191707 0 None - 2 Mouse 6.7 pIC50 = 6.7 Binding
Inhibition of fluorescent antagonist binding to mouse P2Y14 receptor expressed in HEK293 cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysisInhibition of fluorescent antagonist binding to mouse P2Y14 receptor expressed in HEK293 cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysis
ChEMBL 506 6 2 7 5.5 O=C(O)c1cc(-c2ccc(-c3cc(CO)on3)cc2)cc(-n2cc(-c3ccc(C(F)(F)F)cc3)nn2)c1 10.1021/acs.jmedchem.1c00164
164585463 191550 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysisInhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysis
ChEMBL 528 6 2 5 6.6 O=C(O)c1cc(-c2ccc(NC(=O)c3ccccc3)cc2)cc(-n2cc(-c3ccc(C(F)(F)F)cc3)nn2)c1 10.1021/acs.jmedchem.1c00164
CHEMBL4851241 191550 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysisInhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysis
ChEMBL 528 6 2 5 6.6 O=C(O)c1cc(-c2ccc(NC(=O)c3ccccc3)cc2)cc(-n2cc(-c3ccc(C(F)(F)F)cc3)nn2)c1 10.1021/acs.jmedchem.1c00164
164585509 191810 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Inhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysisInhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysis
ChEMBL 578 7 2 6 6.9 CC(C)(C)OC(=O)NCC1(c2ccc(-c3cc(C(=O)O)cc(-n4cc(-c5ccc(C(F)(F)F)cc5)nn4)c3)cc2)CC1 10.1021/acs.jmedchem.1c00164
CHEMBL4855087 191810 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Inhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysisInhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysis
ChEMBL 578 7 2 6 6.9 CC(C)(C)OC(=O)NCC1(c2ccc(-c3cc(C(=O)O)cc(-n4cc(-c5ccc(C(F)(F)F)cc5)nn4)c3)cc2)CC1 10.1021/acs.jmedchem.1c00164
42611190 9930 12 None -1 5 Human 7.7 pIC50 = 7.7 Binding
Inhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 6 by flow cytomtery based competitive fluorescence assayInhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 6 by flow cytomtery based competitive fluorescence assay
ChEMBL 475 4 2 2 7.4 OC(=O)c1cc2cc(ccc2c(c1)c1ccc(cc1)C1CCNCC1)c1ccc(cc1)C(F)(F)F 10.1021/acs.jmedchem.0c00745
5802 9930 12 None -1 5 Human 7.7 pIC50 = 7.7 Binding
Inhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 6 by flow cytomtery based competitive fluorescence assayInhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 6 by flow cytomtery based competitive fluorescence assay
ChEMBL 475 4 2 2 7.4 OC(=O)c1cc2cc(ccc2c(c1)c1ccc(cc1)C1CCNCC1)c1ccc(cc1)C(F)(F)F 10.1021/acs.jmedchem.0c00745
CHEMBL1800685 9930 12 None -1 5 Human 7.7 pIC50 = 7.7 Binding
Inhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 6 by flow cytomtery based competitive fluorescence assayInhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 6 by flow cytomtery based competitive fluorescence assay
ChEMBL 475 4 2 2 7.4 OC(=O)c1cc2cc(ccc2c(c1)c1ccc(cc1)C1CCNCC1)c1ccc(cc1)C(F)(F)F 10.1021/acs.jmedchem.0c00745
139392488 184990 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7.4 by flow cytomtery based competitive fluorescence assayInhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7.4 by flow cytomtery based competitive fluorescence assay
ChEMBL 489 4 1 2 7.7 CN1CCC(c2ccc(-c3cc(C(=O)O)cc4cc(-c5ccc(C(F)(F)F)cc5)ccc34)cc2)CC1 10.1021/acs.jmedchem.0c00745
CHEMBL4649700 184990 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7.4 by flow cytomtery based competitive fluorescence assayInhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7.4 by flow cytomtery based competitive fluorescence assay
ChEMBL 489 4 1 2 7.7 CN1CCC(c2ccc(-c3cc(C(=O)O)cc4cc(-c5ccc(C(F)(F)F)cc5)ccc34)cc2)CC1 10.1021/acs.jmedchem.0c00745
145977780 170377 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric methodDisplacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric method
ChEMBL 513 6 2 7 4.8 O=C(O)c1cc(-c2ccc(CN3CCNCC3)s2)cc(-n2cc(-c3ccc(C(F)(F)F)cc3)nn2)c1 10.1021/acs.jmedchem.8b00168
CHEMBL4203557 170377 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric methodDisplacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric method
ChEMBL 513 6 2 7 4.8 O=C(O)c1cc(-c2ccc(CN3CCNCC3)s2)cc(-n2cc(-c3ccc(C(F)(F)F)cc3)nn2)c1 10.1021/acs.jmedchem.8b00168
164585437 192960 0 None - 1 Human 6.7 pIC50 = 6.7 Binding
Inhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysisInhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysis
ChEMBL 535 6 3 6 5.3 O=C(O)c1cc(-c2ccc(NC(=O)C3CCNCC3)cc2)cc(-n2cc(-c3ccc(C(F)(F)F)cc3)nn2)c1 10.1021/acs.jmedchem.1c00164
CHEMBL4872692 192960 0 None - 1 Human 6.7 pIC50 = 6.7 Binding
Inhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysisInhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysis
ChEMBL 535 6 3 6 5.3 O=C(O)c1cc(-c2ccc(NC(=O)C3CCNCC3)cc2)cc(-n2cc(-c3ccc(C(F)(F)F)cc3)nn2)c1 10.1021/acs.jmedchem.1c00164
139392013 184694 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7.4 by flow cytomtery based competitive fluorescence assayInhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7.4 by flow cytomtery based competitive fluorescence assay
ChEMBL 501 4 1 2 7.6 O=C(O)c1cc(-c2ccc(C34CCN(CC3)CC4)cc2)c2ccc(-c3ccc(C(F)(F)F)cc3)cc2c1 10.1021/acs.jmedchem.0c00745
CHEMBL4645216 184694 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7.4 by flow cytomtery based competitive fluorescence assayInhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7.4 by flow cytomtery based competitive fluorescence assay
ChEMBL 501 4 1 2 7.6 O=C(O)c1cc(-c2ccc(C34CCN(CC3)CC4)cc2)c2ccc(-c3ccc(C(F)(F)F)cc3)cc2c1 10.1021/acs.jmedchem.0c00745
139392013 184694 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibition of fluorescent antagonist binding to human P2Y14R expressed in CHO cells preincubated for 30 mins followed by 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy 6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate addition and measured after 30 mins by BD FACSCalibur flow cytometry analysisInhibition of fluorescent antagonist binding to human P2Y14R expressed in CHO cells preincubated for 30 mins followed by 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy 6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate addition and measured after 30 mins by BD FACSCalibur flow cytometry analysis
ChEMBL 501 4 1 2 7.6 O=C(O)c1cc(-c2ccc(C34CCN(CC3)CC4)cc2)c2ccc(-c3ccc(C(F)(F)F)cc3)cc2c1 10.1021/acs.jmedchem.1c01964
CHEMBL4645216 184694 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibition of fluorescent antagonist binding to human P2Y14R expressed in CHO cells preincubated for 30 mins followed by 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy 6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate addition and measured after 30 mins by BD FACSCalibur flow cytometry analysisInhibition of fluorescent antagonist binding to human P2Y14R expressed in CHO cells preincubated for 30 mins followed by 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy 6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate addition and measured after 30 mins by BD FACSCalibur flow cytometry analysis
ChEMBL 501 4 1 2 7.6 O=C(O)c1cc(-c2ccc(C34CCN(CC3)CC4)cc2)c2ccc(-c3ccc(C(F)(F)F)cc3)cc2c1 10.1021/acs.jmedchem.1c01964
CHEMBL5078197 221322 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibition of fluorescent antagonist binding to human P2Y14R expressed in CHO cells preincubated for 30 mins followed by 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy 6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate addition and measured after 30 mins by BD FACSCalibur flow cytometry analysisInhibition of fluorescent antagonist binding to human P2Y14R expressed in CHO cells preincubated for 30 mins followed by 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy 6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate addition and measured after 30 mins by BD FACSCalibur flow cytometry analysis
ChEMBL None None None CC1CNCCC1c1ccc(-c2cc(C(=O)O)cc3cc(-c4ccc(C(F)(F)F)cc4)ccc23)cc1 10.1021/acs.jmedchem.1c01964
164585536 191948 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysisInhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysis
ChEMBL 478 5 2 5 5.7 NC1(c2ccc(-c3cc(C(=O)O)cc(-n4cc(-c5ccc(C(F)(F)F)cc5)nn4)c3)cc2)CCC1 10.1021/acs.jmedchem.1c00164
CHEMBL4857222 191948 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysisInhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysis
ChEMBL 478 5 2 5 5.7 NC1(c2ccc(-c3cc(C(=O)O)cc(-n4cc(-c5ccc(C(F)(F)F)cc5)nn4)c3)cc2)CCC1 10.1021/acs.jmedchem.1c00164
156020616 184909 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7.4 by flow cytomtery based competitive fluorescence assayInhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7.4 by flow cytomtery based competitive fluorescence assay
ChEMBL 467 5 4 3 4.9 NC(=O)c1ccc(-c2cc(C(=O)O)cc(C(=O)Nc3cc4ccc(C(F)(F)F)cc4[nH]3)c2)cc1 10.1021/acs.jmedchem.0c00745
CHEMBL4648409 184909 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7.4 by flow cytomtery based competitive fluorescence assayInhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7.4 by flow cytomtery based competitive fluorescence assay
ChEMBL 467 5 4 3 4.9 NC(=O)c1ccc(-c2cc(C(=O)O)cc(C(=O)Nc3cc4ccc(C(F)(F)F)cc4[nH]3)c2)cc1 10.1021/acs.jmedchem.0c00745
145978641 170759 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Displacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric methodDisplacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric method
ChEMBL 532 5 2 7 5.3 CC(C)(C)NC(=O)c1ccc(-c2cc(-c3nnn[nH]3)cc(-n3cc(-c4ccc(C(F)(F)F)cc4)nn3)c2)cc1 10.1021/acs.jmedchem.8b00168
CHEMBL4208014 170759 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Displacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric methodDisplacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric method
ChEMBL 532 5 2 7 5.3 CC(C)(C)NC(=O)c1ccc(-c2cc(-c3nnn[nH]3)cc(-n3cc(-c4ccc(C(F)(F)F)cc4)nn3)c2)cc1 10.1021/acs.jmedchem.8b00168
CHEMBL5079102 221386 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibition of fluorescent antagonist binding to human P2Y14R expressed in CHO cells preincubated for 30 mins followed by 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy 6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate addition and measured after 30 mins by BD FACSCalibur flow cytometry analysisInhibition of fluorescent antagonist binding to human P2Y14R expressed in CHO cells preincubated for 30 mins followed by 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy 6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate addition and measured after 30 mins by BD FACSCalibur flow cytometry analysis
ChEMBL None None None O=C(O)c1cc(-c2ccc(C3(O)[C@H]4CC[C@H]3CNC4)cc2)c2ccc(-c3ccc(C(F)(F)F)cc3)cc2c1 10.1021/acs.jmedchem.1c01964
139392013 184694 0 None - 0 Mouse 7.7 pIC50 = 7.7 Binding
Inhibition of MRS4174 binding to mouse P2Y14R expressed in HEK293 cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins by flow cytomtery based competitive fluorescence assayInhibition of MRS4174 binding to mouse P2Y14R expressed in HEK293 cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins by flow cytomtery based competitive fluorescence assay
ChEMBL 501 4 1 2 7.6 O=C(O)c1cc(-c2ccc(C34CCN(CC3)CC4)cc2)c2ccc(-c3ccc(C(F)(F)F)cc3)cc2c1 10.1021/acs.jmedchem.0c00745
CHEMBL4645216 184694 0 None - 0 Mouse 7.7 pIC50 = 7.7 Binding
Inhibition of MRS4174 binding to mouse P2Y14R expressed in HEK293 cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins by flow cytomtery based competitive fluorescence assayInhibition of MRS4174 binding to mouse P2Y14R expressed in HEK293 cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins by flow cytomtery based competitive fluorescence assay
ChEMBL 501 4 1 2 7.6 O=C(O)c1cc(-c2ccc(C34CCN(CC3)CC4)cc2)c2ccc(-c3ccc(C(F)(F)F)cc3)cc2c1 10.1021/acs.jmedchem.0c00745
42611190 9930 12 None -87 5 Mouse 7.7 pIC50 = 7.7 Binding
Displacement of Alexafluor488 labeled 4-(4-(1-(4-(1-(6-(4-(6-amino-3-imino-4,5-disulfo-3H-xanthen-9-yl)-3-carboxybenzamido)hexyl)-1H-1,2,3-triazol-4-yl)butyl)piperidin-4-yl)phenyl)-7-(4-(trifluoromethyl)phenyl)-2-naphthoic acid from HA-tagged mouse P2Y14 expressed in HEK293 cells measured after 30 mins by FACScalibur flow cytometry analysisDisplacement of Alexafluor488 labeled 4-(4-(1-(4-(1-(6-(4-(6-amino-3-imino-4,5-disulfo-3H-xanthen-9-yl)-3-carboxybenzamido)hexyl)-1H-1,2,3-triazol-4-yl)butyl)piperidin-4-yl)phenyl)-7-(4-(trifluoromethyl)phenyl)-2-naphthoic acid from HA-tagged mouse P2Y14 expressed in HEK293 cells measured after 30 mins by FACScalibur flow cytometry analysis
ChEMBL 475 4 2 2 7.4 OC(=O)c1cc2cc(ccc2c(c1)c1ccc(cc1)C1CCNCC1)c1ccc(cc1)C(F)(F)F 10.1021/acsmedchemlett.0c00115
5802 9930 12 None -87 5 Mouse 7.7 pIC50 = 7.7 Binding
Displacement of Alexafluor488 labeled 4-(4-(1-(4-(1-(6-(4-(6-amino-3-imino-4,5-disulfo-3H-xanthen-9-yl)-3-carboxybenzamido)hexyl)-1H-1,2,3-triazol-4-yl)butyl)piperidin-4-yl)phenyl)-7-(4-(trifluoromethyl)phenyl)-2-naphthoic acid from HA-tagged mouse P2Y14 expressed in HEK293 cells measured after 30 mins by FACScalibur flow cytometry analysisDisplacement of Alexafluor488 labeled 4-(4-(1-(4-(1-(6-(4-(6-amino-3-imino-4,5-disulfo-3H-xanthen-9-yl)-3-carboxybenzamido)hexyl)-1H-1,2,3-triazol-4-yl)butyl)piperidin-4-yl)phenyl)-7-(4-(trifluoromethyl)phenyl)-2-naphthoic acid from HA-tagged mouse P2Y14 expressed in HEK293 cells measured after 30 mins by FACScalibur flow cytometry analysis
ChEMBL 475 4 2 2 7.4 OC(=O)c1cc2cc(ccc2c(c1)c1ccc(cc1)C1CCNCC1)c1ccc(cc1)C(F)(F)F 10.1021/acsmedchemlett.0c00115
CHEMBL1800685 9930 12 None -87 5 Mouse 7.7 pIC50 = 7.7 Binding
Displacement of Alexafluor488 labeled 4-(4-(1-(4-(1-(6-(4-(6-amino-3-imino-4,5-disulfo-3H-xanthen-9-yl)-3-carboxybenzamido)hexyl)-1H-1,2,3-triazol-4-yl)butyl)piperidin-4-yl)phenyl)-7-(4-(trifluoromethyl)phenyl)-2-naphthoic acid from HA-tagged mouse P2Y14 expressed in HEK293 cells measured after 30 mins by FACScalibur flow cytometry analysisDisplacement of Alexafluor488 labeled 4-(4-(1-(4-(1-(6-(4-(6-amino-3-imino-4,5-disulfo-3H-xanthen-9-yl)-3-carboxybenzamido)hexyl)-1H-1,2,3-triazol-4-yl)butyl)piperidin-4-yl)phenyl)-7-(4-(trifluoromethyl)phenyl)-2-naphthoic acid from HA-tagged mouse P2Y14 expressed in HEK293 cells measured after 30 mins by FACScalibur flow cytometry analysis
ChEMBL 475 4 2 2 7.4 OC(=O)c1cc2cc(ccc2c(c1)c1ccc(cc1)C1CCNCC1)c1ccc(cc1)C(F)(F)F 10.1021/acsmedchemlett.0c00115
42611190 9930 12 None -87 5 Mouse 7.7 pIC50 = 7.7 Binding
Inhibition of MRS4174 binding to mouse P2Y14R expressed in HEK293 cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins by flow cytomtery based competitive fluorescence assayInhibition of MRS4174 binding to mouse P2Y14R expressed in HEK293 cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins by flow cytomtery based competitive fluorescence assay
ChEMBL 475 4 2 2 7.4 OC(=O)c1cc2cc(ccc2c(c1)c1ccc(cc1)C1CCNCC1)c1ccc(cc1)C(F)(F)F 10.1021/acs.jmedchem.0c00745
5802 9930 12 None -87 5 Mouse 7.7 pIC50 = 7.7 Binding
Inhibition of MRS4174 binding to mouse P2Y14R expressed in HEK293 cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins by flow cytomtery based competitive fluorescence assayInhibition of MRS4174 binding to mouse P2Y14R expressed in HEK293 cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins by flow cytomtery based competitive fluorescence assay
ChEMBL 475 4 2 2 7.4 OC(=O)c1cc2cc(ccc2c(c1)c1ccc(cc1)C1CCNCC1)c1ccc(cc1)C(F)(F)F 10.1021/acs.jmedchem.0c00745
CHEMBL1800685 9930 12 None -87 5 Mouse 7.7 pIC50 = 7.7 Binding
Inhibition of MRS4174 binding to mouse P2Y14R expressed in HEK293 cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins by flow cytomtery based competitive fluorescence assayInhibition of MRS4174 binding to mouse P2Y14R expressed in HEK293 cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins by flow cytomtery based competitive fluorescence assay
ChEMBL 475 4 2 2 7.4 OC(=O)c1cc2cc(ccc2c(c1)c1ccc(cc1)C1CCNCC1)c1ccc(cc1)C(F)(F)F 10.1021/acs.jmedchem.0c00745
CHEMBL5089848 222009 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of fluorescent antagonist binding to human P2Y14R expressed in CHO cells preincubated for 30 mins followed by 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy 6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate addition and measured after 30 mins by BD FACSCalibur flow cytometry analysisInhibition of fluorescent antagonist binding to human P2Y14R expressed in CHO cells preincubated for 30 mins followed by 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy 6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate addition and measured after 30 mins by BD FACSCalibur flow cytometry analysis
ChEMBL None None None O=C(O)c1cc(-c2ccc(C34CCNCC3C4(F)F)cc2)c2ccc(-c3ccc(C(F)(F)F)cc3)cc2c1 10.1021/acs.jmedchem.1c01964
155534564 178735 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Binding affinity to human P2Y14 expressed in CHO cellsBinding affinity to human P2Y14 expressed in CHO cells
ChEMBL 525 9 6 10 -0.7 O=c1[nH]/c(=N/OCc2ccccc2)c(F)cn1[C@@H]1O[C@H](COP(=O)(O)CP(=O)(O)O)[C@@H](O)[C@H]1O 10.1016/j.bmcl.2021.128137
CHEMBL4470616 178735 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Binding affinity to human P2Y14 expressed in CHO cellsBinding affinity to human P2Y14 expressed in CHO cells
ChEMBL 525 9 6 10 -0.7 O=c1[nH]/c(=N/OCc2ccccc2)c(F)cn1[C@@H]1O[C@H](COP(=O)(O)CP(=O)(O)O)[C@@H](O)[C@H]1O 10.1016/j.bmcl.2021.128137
CHEMBL4871928 178735 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Binding affinity to human P2Y14 expressed in CHO cellsBinding affinity to human P2Y14 expressed in CHO cells
ChEMBL 525 9 6 10 -0.7 O=c1[nH]/c(=N/OCc2ccccc2)c(F)cn1[C@@H]1O[C@H](COP(=O)(O)CP(=O)(O)O)[C@@H](O)[C@H]1O 10.1016/j.bmcl.2021.128137
145975592 170460 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric methodDisplacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric method
ChEMBL 565 10 3 8 4.4 NCCCCNS(=O)(=O)c1ccc(-c2cc(C(=O)O)cc(-n3cc(-c4ccc(C(F)(F)F)cc4)nn3)c2)s1 10.1021/acs.jmedchem.8b00168
CHEMBL4204741 170460 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric methodDisplacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric method
ChEMBL 565 10 3 8 4.4 NCCCCNS(=O)(=O)c1ccc(-c2cc(C(=O)O)cc(-n3cc(-c4ccc(C(F)(F)F)cc4)nn3)c2)s1 10.1021/acs.jmedchem.8b00168
164585335 193219 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysisInhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysis
ChEMBL 476 5 1 6 6.0 O=C(O)c1cc(-c2ccc(-c3ccon3)cc2)cc(-n2cc(-c3ccc(C(F)(F)F)cc3)nn2)c1 10.1021/acs.jmedchem.1c00164
CHEMBL4876369 193219 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysisInhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysis
ChEMBL 476 5 1 6 6.0 O=C(O)c1cc(-c2ccc(-c3ccon3)cc2)cc(-n2cc(-c3ccc(C(F)(F)F)cc3)nn2)c1 10.1021/acs.jmedchem.1c00164
135356798 178179 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of 6-Amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy-6-(4-(trifluoromethyl)phenyl)-naphthalen-1-yl)phenyl)piperidin-1-yl)-butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)-phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate from human P2Y14R expressed in CHO cells measured after 15 mins by flow cytometric analysisDisplacement of 6-Amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy-6-(4-(trifluoromethyl)phenyl)-naphthalen-1-yl)phenyl)piperidin-1-yl)-butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)-phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate from human P2Y14R expressed in CHO cells measured after 15 mins by flow cytometric analysis
ChEMBL 480 5 2 5 6.1 CC(C)(C)c1ccc(-c2cn(-c3cc(C(=O)O)cc(-c4ccc(C5CCNCC5)cc4)c3)nn2)cc1 10.1021/acs.jmedchem.6b00044
CHEMBL4462380 178179 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of 6-Amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy-6-(4-(trifluoromethyl)phenyl)-naphthalen-1-yl)phenyl)piperidin-1-yl)-butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)-phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate from human P2Y14R expressed in CHO cells measured after 15 mins by flow cytometric analysisDisplacement of 6-Amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy-6-(4-(trifluoromethyl)phenyl)-naphthalen-1-yl)phenyl)piperidin-1-yl)-butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)-phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate from human P2Y14R expressed in CHO cells measured after 15 mins by flow cytometric analysis
ChEMBL 480 5 2 5 6.1 CC(C)(C)c1ccc(-c2cn(-c3cc(C(=O)O)cc(-c4ccc(C5CCNCC5)cc4)c3)nn2)cc1 10.1021/acs.jmedchem.6b00044
164585399 191970 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Inhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysisInhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysis
ChEMBL 635 6 2 7 6.9 CC(C)(C)OC(=O)N1CCC(C(=O)Nc2ccc(-c3cc(C(=O)O)cc(-n4cc(-c5ccc(C(F)(F)F)cc5)nn4)c3)cc2)CC1 10.1021/acs.jmedchem.1c00164
CHEMBL4857504 191970 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Inhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysisInhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysis
ChEMBL 635 6 2 7 6.9 CC(C)(C)OC(=O)N1CCC(C(=O)Nc2ccc(-c3cc(C(=O)O)cc(-n4cc(-c5ccc(C(F)(F)F)cc5)nn4)c3)cc2)CC1 10.1021/acs.jmedchem.1c00164
145965887 170867 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric methodDisplacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric method
ChEMBL 537 8 3 8 3.6 NCCNS(=O)(=O)c1ccc(-c2cc(C(=O)O)cc(-n3cc(-c4ccc(C(F)(F)F)cc4)nn3)c2)s1 10.1021/acs.jmedchem.8b00168
CHEMBL4209538 170867 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric methodDisplacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric method
ChEMBL 537 8 3 8 3.6 NCCNS(=O)(=O)c1ccc(-c2cc(C(=O)O)cc(-n3cc(-c4ccc(C(F)(F)F)cc4)nn3)c2)s1 10.1021/acs.jmedchem.8b00168
135356790 181863 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of 6-Amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy-6-(4-(trifluoromethyl)phenyl)-naphthalen-1-yl)phenyl)piperidin-1-yl)-butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)-phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate from human P2Y14R expressed in CHO cells measured after 15 mins by flow cytometric analysisDisplacement of 6-Amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy-6-(4-(trifluoromethyl)phenyl)-naphthalen-1-yl)phenyl)piperidin-1-yl)-butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)-phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate from human P2Y14R expressed in CHO cells measured after 15 mins by flow cytometric analysis
ChEMBL 460 5 2 5 5.0 O=C(O)c1cc(-c2ccc(C3CCNCC3)cc2)cc(-n2cc(-c3ccc(F)c(F)c3)nn2)c1 10.1021/acs.jmedchem.6b00044
CHEMBL4568641 181863 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of 6-Amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy-6-(4-(trifluoromethyl)phenyl)-naphthalen-1-yl)phenyl)piperidin-1-yl)-butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)-phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate from human P2Y14R expressed in CHO cells measured after 15 mins by flow cytometric analysisDisplacement of 6-Amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy-6-(4-(trifluoromethyl)phenyl)-naphthalen-1-yl)phenyl)piperidin-1-yl)-butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)-phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate from human P2Y14R expressed in CHO cells measured after 15 mins by flow cytometric analysis
ChEMBL 460 5 2 5 5.0 O=C(O)c1cc(-c2ccc(C3CCNCC3)cc2)cc(-n2cc(-c3ccc(F)c(F)c3)nn2)c1 10.1021/acs.jmedchem.6b00044
145965747 171050 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric methodDisplacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric method
ChEMBL 615 9 3 8 6.0 CC(C)(C)OC(=O)NCCCNC(=O)c1ccc(-c2cc(C(=O)O)cc(-n3cc(-c4ccc(C(F)(F)F)cc4)nn3)c2)s1 10.1021/acs.jmedchem.8b00168
CHEMBL4211740 171050 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric methodDisplacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric method
ChEMBL 615 9 3 8 6.0 CC(C)(C)OC(=O)NCCCNC(=O)c1ccc(-c2cc(C(=O)O)cc(-n3cc(-c4ccc(C(F)(F)F)cc4)nn3)c2)s1 10.1021/acs.jmedchem.8b00168
CHEMBL5084539 221701 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibition of fluorescent antagonist binding to human P2Y14R expressed in CHO cells preincubated for 30 mins followed by 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy 6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate addition and measured after 30 mins by BD FACSCalibur flow cytometry analysisInhibition of fluorescent antagonist binding to human P2Y14R expressed in CHO cells preincubated for 30 mins followed by 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy 6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate addition and measured after 30 mins by BD FACSCalibur flow cytometry analysis
ChEMBL None None None O=C(O)c1cc(-c2ccc(C3=C[C@H]4CC[C@@H]3CN4)cc2)c2ccc(-c3ccc(C(F)(F)F)cc3)cc2c1 10.1021/acs.jmedchem.1c01964
139392022 184749 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7.4 by flow cytomtery based competitive fluorescence assayInhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7.4 by flow cytomtery based competitive fluorescence assay
ChEMBL 493 5 2 6 4.7 O=C(O)c1cc(-c2ccc(N3CCNCC3)cc2)cc(-n2cc(-c3ccc(C(F)(F)F)cc3)nn2)c1 10.1021/acs.jmedchem.0c00745
CHEMBL4645987 184749 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7.4 by flow cytomtery based competitive fluorescence assayInhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7.4 by flow cytomtery based competitive fluorescence assay
ChEMBL 493 5 2 6 4.7 O=C(O)c1cc(-c2ccc(N3CCNCC3)cc2)cc(-n2cc(-c3ccc(C(F)(F)F)cc3)nn2)c1 10.1021/acs.jmedchem.0c00745
135356965 176864 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of 6-Amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy-6-(4-(trifluoromethyl)phenyl)-naphthalen-1-yl)phenyl)piperidin-1-yl)-butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)-phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate from human P2Y14R expressed in CHO cells measured after 15 mins by flow cytometric analysisDisplacement of 6-Amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy-6-(4-(trifluoromethyl)phenyl)-naphthalen-1-yl)phenyl)piperidin-1-yl)-butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)-phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate from human P2Y14R expressed in CHO cells measured after 15 mins by flow cytometric analysis
ChEMBL 438 5 2 5 5.1 Cc1ccc(-c2cn(-c3cc(C(=O)O)cc(-c4ccc(C5CCNCC5)cc4)c3)nn2)cc1 10.1021/acs.jmedchem.6b00044
CHEMBL4443391 176864 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of 6-Amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy-6-(4-(trifluoromethyl)phenyl)-naphthalen-1-yl)phenyl)piperidin-1-yl)-butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)-phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate from human P2Y14R expressed in CHO cells measured after 15 mins by flow cytometric analysisDisplacement of 6-Amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy-6-(4-(trifluoromethyl)phenyl)-naphthalen-1-yl)phenyl)piperidin-1-yl)-butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)-phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate from human P2Y14R expressed in CHO cells measured after 15 mins by flow cytometric analysis
ChEMBL 438 5 2 5 5.1 Cc1ccc(-c2cn(-c3cc(C(=O)O)cc(-c4ccc(C5CCNCC5)cc4)c3)nn2)cc1 10.1021/acs.jmedchem.6b00044
164585482 192851 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysisInhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysis
ChEMBL 571 4 1 2 8.2 O=C(O)c1cc(-c2ccc(C3CCN(C(=O)C(F)(F)F)CC3)cc2)c2ccc(-c3ccc(C(F)(F)F)cc3)cc2c1 10.1021/acs.jmedchem.1c00164
CHEMBL4871298 192851 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysisInhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysis
ChEMBL 571 4 1 2 8.2 O=C(O)c1cc(-c2ccc(C3CCN(C(=O)C(F)(F)F)CC3)cc2)c2ccc(-c3ccc(C(F)(F)F)cc3)cc2c1 10.1021/acs.jmedchem.1c00164
145970281 170755 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric methodDisplacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric method
ChEMBL 476 5 2 7 3.9 NC(=O)c1ccc(-c2cc(-c3nnn[nH]3)cc(-n3cc(-c4ccc(C(F)(F)F)cc4)nn3)c2)cc1 10.1021/acs.jmedchem.8b00168
CHEMBL4207940 170755 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric methodDisplacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric method
ChEMBL 476 5 2 7 3.9 NC(=O)c1ccc(-c2cc(-c3nnn[nH]3)cc(-n3cc(-c4ccc(C(F)(F)F)cc4)nn3)c2)cc1 10.1021/acs.jmedchem.8b00168
156014504 184023 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7.4 by flow cytomtery based competitive fluorescence assayInhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7.4 by flow cytomtery based competitive fluorescence assay
ChEMBL 467 5 4 3 4.9 NC(=O)c1ccc(-c2cc(C(=O)O)cc(C(=O)Nc3cc4cc(C(F)(F)F)ccc4[nH]3)c2)cc1 10.1021/acs.jmedchem.0c00745
CHEMBL4635846 184023 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7.4 by flow cytomtery based competitive fluorescence assayInhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7.4 by flow cytomtery based competitive fluorescence assay
ChEMBL 467 5 4 3 4.9 NC(=O)c1ccc(-c2cc(C(=O)O)cc(C(=O)Nc3cc4cc(C(F)(F)F)ccc4[nH]3)c2)cc1 10.1021/acs.jmedchem.0c00745
59590494 184412 2 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7.4 by flow cytomtery based competitive fluorescence assayInhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7.4 by flow cytomtery based competitive fluorescence assay
ChEMBL 575 4 1 3 9.0 CC(C)(C)OC(=O)N1CCC(c2ccc(-c3cc(C(=O)O)cc4cc(-c5ccc(C(F)(F)F)cc5)ccc34)cc2)CC1 10.1021/acs.jmedchem.0c00745
CHEMBL4641243 184412 2 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7.4 by flow cytomtery based competitive fluorescence assayInhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7.4 by flow cytomtery based competitive fluorescence assay
ChEMBL 575 4 1 3 9.0 CC(C)(C)OC(=O)N1CCC(c2ccc(-c3cc(C(=O)O)cc4cc(-c5ccc(C(F)(F)F)cc5)ccc34)cc2)CC1 10.1021/acs.jmedchem.0c00745
156018952 184657 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Inhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7.4 by flow cytomtery based competitive fluorescence assayInhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7.4 by flow cytomtery based competitive fluorescence assay
ChEMBL 468 5 4 4 4.3 NC(=O)c1ccc(-c2cc(C(=O)O)cc(C(=O)Nc3nc4cc(C(F)(F)F)ccc4[nH]3)c2)cc1 10.1021/acs.jmedchem.0c00745
CHEMBL4644647 184657 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Inhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7.4 by flow cytomtery based competitive fluorescence assayInhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7.4 by flow cytomtery based competitive fluorescence assay
ChEMBL 468 5 4 4 4.3 NC(=O)c1ccc(-c2cc(C(=O)O)cc(C(=O)Nc3nc4cc(C(F)(F)F)ccc4[nH]3)c2)cc1 10.1021/acs.jmedchem.0c00745
139406787 183924 0 None - 4 Mouse 6.6 pIC50 = 6.6 Binding
Displacement of Alexafluor488 labeled 4-(4-(1-(4-(1-(6-(4-(6-amino-3-imino-4,5-disulfo-3H-xanthen-9-yl)-3-carboxybenzamido)hexyl)-1H-1,2,3-triazol-4-yl)butyl)piperidin-4-yl)phenyl)-7-(4-(trifluoromethyl)phenyl)-2-naphthoic acid from HA-tagged mouse P2Y14 expressed in HEK293 cells measured after 30 mins by FACScalibur flow cytometry analysisDisplacement of Alexafluor488 labeled 4-(4-(1-(4-(1-(6-(4-(6-amino-3-imino-4,5-disulfo-3H-xanthen-9-yl)-3-carboxybenzamido)hexyl)-1H-1,2,3-triazol-4-yl)butyl)piperidin-4-yl)phenyl)-7-(4-(trifluoromethyl)phenyl)-2-naphthoic acid from HA-tagged mouse P2Y14 expressed in HEK293 cells measured after 30 mins by FACScalibur flow cytometry analysis
ChEMBL 492 5 2 5 5.8 O=C(O)c1cc(-c2ccc(C3CCNCC3)cc2)cc(-c2cn(-c3ccc(C(F)(F)F)cc3)nn2)c1 10.1021/acsmedchemlett.0c00115
CHEMBL4633982 183924 0 None - 4 Mouse 6.6 pIC50 = 6.6 Binding
Displacement of Alexafluor488 labeled 4-(4-(1-(4-(1-(6-(4-(6-amino-3-imino-4,5-disulfo-3H-xanthen-9-yl)-3-carboxybenzamido)hexyl)-1H-1,2,3-triazol-4-yl)butyl)piperidin-4-yl)phenyl)-7-(4-(trifluoromethyl)phenyl)-2-naphthoic acid from HA-tagged mouse P2Y14 expressed in HEK293 cells measured after 30 mins by FACScalibur flow cytometry analysisDisplacement of Alexafluor488 labeled 4-(4-(1-(4-(1-(6-(4-(6-amino-3-imino-4,5-disulfo-3H-xanthen-9-yl)-3-carboxybenzamido)hexyl)-1H-1,2,3-triazol-4-yl)butyl)piperidin-4-yl)phenyl)-7-(4-(trifluoromethyl)phenyl)-2-naphthoic acid from HA-tagged mouse P2Y14 expressed in HEK293 cells measured after 30 mins by FACScalibur flow cytometry analysis
ChEMBL 492 5 2 5 5.8 O=C(O)c1cc(-c2ccc(C3CCNCC3)cc2)cc(-c2cn(-c3ccc(C(F)(F)F)cc3)nn2)c1 10.1021/acsmedchemlett.0c00115
139406787 183924 0 None - 4 Mouse 6.6 pIC50 = 6.6 Binding
Inhibition of MRS4174 binding to mouse P2Y14R expressed in HEK293 cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins by flow cytomtery based competitive fluorescence assayInhibition of MRS4174 binding to mouse P2Y14R expressed in HEK293 cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins by flow cytomtery based competitive fluorescence assay
ChEMBL 492 5 2 5 5.8 O=C(O)c1cc(-c2ccc(C3CCNCC3)cc2)cc(-c2cn(-c3ccc(C(F)(F)F)cc3)nn2)c1 10.1021/acs.jmedchem.0c00745
CHEMBL4633982 183924 0 None - 4 Mouse 6.6 pIC50 = 6.6 Binding
Inhibition of MRS4174 binding to mouse P2Y14R expressed in HEK293 cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins by flow cytomtery based competitive fluorescence assayInhibition of MRS4174 binding to mouse P2Y14R expressed in HEK293 cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins by flow cytomtery based competitive fluorescence assay
ChEMBL 492 5 2 5 5.8 O=C(O)c1cc(-c2ccc(C3CCNCC3)cc2)cc(-c2cn(-c3ccc(C(F)(F)F)cc3)nn2)c1 10.1021/acs.jmedchem.0c00745
CHEMBL5074947 221120 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibition of fluorescent antagonist binding to human P2Y14R expressed in CHO cells preincubated for 30 mins followed by 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy 6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate addition and measured after 30 mins by BD FACSCalibur flow cytometry analysisInhibition of fluorescent antagonist binding to human P2Y14R expressed in CHO cells preincubated for 30 mins followed by 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy 6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate addition and measured after 30 mins by BD FACSCalibur flow cytometry analysis
ChEMBL None None None O=C(O)c1cc(-c2ccc(C3CC4CCC3CN4)cc2)c2ccc(-c3ccc(C(F)(F)F)cc3)cc2c1 10.1021/acs.jmedchem.1c01964
126720252 171454 0 None - 12 Human 7.6 pIC50 = 7.6 Binding
Displacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric methodDisplacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric method
ChEMBL 697 15 2 6 9.2 NCCCCCCn1cc(CCCCN2CCC(c3ccc(-c4cc(C(=O)O)cc5cc(-c6ccc(C(F)(F)F)cc6)ccc45)cc3)CC2)nn1 10.1021/acs.jmedchem.8b00168
CHEMBL4216870 171454 0 None - 12 Human 7.6 pIC50 = 7.6 Binding
Displacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric methodDisplacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric method
ChEMBL 697 15 2 6 9.2 NCCCCCCn1cc(CCCCN2CCC(c3ccc(-c4cc(C(=O)O)cc5cc(-c6ccc(C(F)(F)F)cc6)ccc45)cc3)CC2)nn1 10.1021/acs.jmedchem.8b00168
CHEMBL5091500 222090 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibition of fluorescent antagonist binding to human P2Y14R expressed in CHO cells preincubated for 30 mins followed by 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy 6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate addition and measured after 30 mins by BD FACSCalibur flow cytometry analysisInhibition of fluorescent antagonist binding to human P2Y14R expressed in CHO cells preincubated for 30 mins followed by 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy 6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate addition and measured after 30 mins by BD FACSCalibur flow cytometry analysis
ChEMBL None None None O=C(O)c1cc(-c2ccc([C@H]3C[C@@H]4CN[C@H]3C4)cc2)c2ccc(-c3ccc(C(F)(F)F)cc3)cc2c1 10.1021/acs.jmedchem.1c01964
CHEMBL5076127 221194 0 None - 0 Mouse 7.6 pIC50 = 7.6 Binding
Inhibition of fluorescent antagonist binding to mouse P2Y14R expressed in HEK293 cells preincubated for 30 mins followed by addition of 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy-6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate incubated for 30 mins by BD FACSCalibur flow cytometry analysisInhibition of fluorescent antagonist binding to mouse P2Y14R expressed in HEK293 cells preincubated for 30 mins followed by addition of 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy-6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate incubated for 30 mins by BD FACSCalibur flow cytometry analysis
ChEMBL None None None O=C(O)c1cc(-c2ccc([C@@H]3C[C@@H]4C[C@H]3C(=O)N4)cc2)c2ccc(-c3ccc(C(F)(F)F)cc3)cc2c1 10.1021/acs.jmedchem.1c01964
156021006 184816 0 None - 1 Human 5.6 pIC50 = 5.6 Binding
Inhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7.4 by flow cytomtery based competitive fluorescence assayInhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7.4 by flow cytomtery based competitive fluorescence assay
ChEMBL 509 8 3 6 4.4 NCCCNC(=O)c1ccc(-c2cc(C(=O)O)cc(-c3cn(-c4ccc(C(F)(F)F)cc4)nn3)c2)cc1 10.1021/acs.jmedchem.0c00745
CHEMBL4647020 184816 0 None - 1 Human 5.6 pIC50 = 5.6 Binding
Inhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7.4 by flow cytomtery based competitive fluorescence assayInhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7.4 by flow cytomtery based competitive fluorescence assay
ChEMBL 509 8 3 6 4.4 NCCCNC(=O)c1ccc(-c2cc(C(=O)O)cc(-c3cn(-c4ccc(C(F)(F)F)cc4)nn3)c2)cc1 10.1021/acs.jmedchem.0c00745
145974515 171530 1 None - 0 Human 4.6 pIC50 = 4.6 Binding
Displacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric methodDisplacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric method
ChEMBL 411 3 1 4 4.4 O=C(O)c1cc(Br)cc(-n2cc(-c3ccc(C(F)(F)F)cc3)nn2)c1 10.1021/acs.jmedchem.8b00168
CHEMBL4217776 171530 1 None - 0 Human 4.6 pIC50 = 4.6 Binding
Displacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric methodDisplacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric method
ChEMBL 411 3 1 4 4.4 O=C(O)c1cc(Br)cc(-n2cc(-c3ccc(C(F)(F)F)cc3)nn2)c1 10.1021/acs.jmedchem.8b00168
134611896 9448 4 None - 1 Human 6.6 pIC50 = 6.6 Binding
Displacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric methodDisplacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric method
ChEMBL 452 5 2 5 4.4 OC(=O)c1cc(cc(c1)n1nnc(c1)c1ccc(cc1)C(F)(F)F)c1ccc(cc1)C(=O)N 10.1021/acs.jmedchem.8b00168
9999 9448 4 None - 1 Human 6.6 pIC50 = 6.6 Binding
Displacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric methodDisplacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric method
ChEMBL 452 5 2 5 4.4 OC(=O)c1cc(cc(c1)n1nnc(c1)c1ccc(cc1)C(F)(F)F)c1ccc(cc1)C(=O)N 10.1021/acs.jmedchem.8b00168
CHEMBL4299805 9448 4 None - 1 Human 6.6 pIC50 = 6.6 Binding
Displacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric methodDisplacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric method
ChEMBL 452 5 2 5 4.4 OC(=O)c1cc(cc(c1)n1nnc(c1)c1ccc(cc1)C(F)(F)F)c1ccc(cc1)C(=O)N 10.1021/acs.jmedchem.8b00168
CHEMBL5086761 221826 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of fluorescent antagonist binding to human P2Y14R expressed in CHO cells preincubated for 30 mins followed by 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy 6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate addition and measured after 30 mins by BD FACSCalibur flow cytometry analysisInhibition of fluorescent antagonist binding to human P2Y14R expressed in CHO cells preincubated for 30 mins followed by 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy 6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate addition and measured after 30 mins by BD FACSCalibur flow cytometry analysis
ChEMBL None None None N[C@H]1C[C@@H](C(=O)O)C[C@@H]1c1ccc(-c2cc(C(=O)O)cc3cc(-c4ccc(C(F)(F)F)cc4)ccc23)cc1 10.1021/acs.jmedchem.1c01964
155770281 184526 0 None - 9 Human 7.6 pIC50 = 7.6 Binding
Displacement of Alexafluor488 labeled 4-(4-(1-(4-(1-(6-(4-(6-amino-3-imino-4,5-disulfo-3H-xanthen-9-yl)-3-carboxybenzamido)hexyl)-1H-1,2,3-triazol-4-yl)butyl)piperidin-4-yl)phenyl)-7-(4-(trifluoromethyl)phenyl)-2-naphthoic acid from human P2Y14 expressed in CHO cells measured after 30 mins by FACScalibur flow cytometry analysisDisplacement of Alexafluor488 labeled 4-(4-(1-(4-(1-(6-(4-(6-amino-3-imino-4,5-disulfo-3H-xanthen-9-yl)-3-carboxybenzamido)hexyl)-1H-1,2,3-triazol-4-yl)butyl)piperidin-4-yl)phenyl)-7-(4-(trifluoromethyl)phenyl)-2-naphthoic acid from human P2Y14 expressed in CHO cells measured after 30 mins by FACScalibur flow cytometry analysis
ChEMBL 517 4 1 2 7.6 CC(=O)N1CCC(c2ccc(-c3cc(C(=O)O)cc4cc(-c5ccc(C(F)(F)F)cc5)ccc34)cc2)CC1 10.1021/acsmedchemlett.0c00115
CHEMBL4642592 184526 0 None - 9 Human 7.6 pIC50 = 7.6 Binding
Displacement of Alexafluor488 labeled 4-(4-(1-(4-(1-(6-(4-(6-amino-3-imino-4,5-disulfo-3H-xanthen-9-yl)-3-carboxybenzamido)hexyl)-1H-1,2,3-triazol-4-yl)butyl)piperidin-4-yl)phenyl)-7-(4-(trifluoromethyl)phenyl)-2-naphthoic acid from human P2Y14 expressed in CHO cells measured after 30 mins by FACScalibur flow cytometry analysisDisplacement of Alexafluor488 labeled 4-(4-(1-(4-(1-(6-(4-(6-amino-3-imino-4,5-disulfo-3H-xanthen-9-yl)-3-carboxybenzamido)hexyl)-1H-1,2,3-triazol-4-yl)butyl)piperidin-4-yl)phenyl)-7-(4-(trifluoromethyl)phenyl)-2-naphthoic acid from human P2Y14 expressed in CHO cells measured after 30 mins by FACScalibur flow cytometry analysis
ChEMBL 517 4 1 2 7.6 CC(=O)N1CCC(c2ccc(-c3cc(C(=O)O)cc4cc(-c5ccc(C(F)(F)F)cc5)ccc34)cc2)CC1 10.1021/acsmedchemlett.0c00115
156021465 184820 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7.4 by flow cytomtery based competitive fluorescence assayInhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7.4 by flow cytomtery based competitive fluorescence assay
ChEMBL 954 28 2 11 8.6 CC(C)(C)OC(=O)NCCOCCOCCOCCOCCOCCOCCOCCC(=O)N1CCC(c2ccc(-c3cc(C(=O)O)cc4cc(-c5ccc(C(F)(F)F)cc5)ccc34)cc2)CC1 10.1021/acs.jmedchem.0c00745
CHEMBL4647092 184820 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7.4 by flow cytomtery based competitive fluorescence assayInhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7.4 by flow cytomtery based competitive fluorescence assay
ChEMBL 954 28 2 11 8.6 CC(C)(C)OC(=O)NCCOCCOCCOCCOCCOCCOCCOCCC(=O)N1CCC(c2ccc(-c3cc(C(=O)O)cc4cc(-c5ccc(C(F)(F)F)cc5)ccc34)cc2)CC1 10.1021/acs.jmedchem.0c00745
164585460 192673 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysisInhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysis
ChEMBL 495 6 2 6 4.6 O=C(O)c1cc(-c2ccc(C3(CO)COC3)cc2)cc(-n2cc(-c3ccc(C(F)(F)F)cc3)nn2)c1 10.1021/acs.jmedchem.1c00164
CHEMBL4868552 192673 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysisInhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysis
ChEMBL 495 6 2 6 4.6 O=C(O)c1cc(-c2ccc(C3(CO)COC3)cc2)cc(-n2cc(-c3ccc(C(F)(F)F)cc3)nn2)c1 10.1021/acs.jmedchem.1c00164
CHEMBL5075741 221175 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibition of fluorescent antagonist binding to human P2Y14R expressed in CHO cells preincubated for 30 mins followed by 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy 6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate addition and measured after 30 mins by BD FACSCalibur flow cytometry analysisInhibition of fluorescent antagonist binding to human P2Y14R expressed in CHO cells preincubated for 30 mins followed by 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy 6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate addition and measured after 30 mins by BD FACSCalibur flow cytometry analysis
ChEMBL None None None CC(=O)N1C[C@@H]2C[C@H]1C[C@H]2c1ccc(-c2cc(C(=O)O)cc3cc(-c4ccc(C(F)(F)F)cc4)ccc23)cc1 10.1021/acs.jmedchem.1c01964
155770281 184526 0 None - 9 Mouse 7.5 pIC50 = 7.5 Binding
Displacement of Alexafluor488 labeled 4-(4-(1-(4-(1-(6-(4-(6-amino-3-imino-4,5-disulfo-3H-xanthen-9-yl)-3-carboxybenzamido)hexyl)-1H-1,2,3-triazol-4-yl)butyl)piperidin-4-yl)phenyl)-7-(4-(trifluoromethyl)phenyl)-2-naphthoic acid from HA-tagged mouse P2Y14 expressed in HEK293 cells measured after 30 mins by FACScalibur flow cytometry analysisDisplacement of Alexafluor488 labeled 4-(4-(1-(4-(1-(6-(4-(6-amino-3-imino-4,5-disulfo-3H-xanthen-9-yl)-3-carboxybenzamido)hexyl)-1H-1,2,3-triazol-4-yl)butyl)piperidin-4-yl)phenyl)-7-(4-(trifluoromethyl)phenyl)-2-naphthoic acid from HA-tagged mouse P2Y14 expressed in HEK293 cells measured after 30 mins by FACScalibur flow cytometry analysis
ChEMBL 517 4 1 2 7.6 CC(=O)N1CCC(c2ccc(-c3cc(C(=O)O)cc4cc(-c5ccc(C(F)(F)F)cc5)ccc34)cc2)CC1 10.1021/acsmedchemlett.0c00115
CHEMBL4642592 184526 0 None - 9 Mouse 7.5 pIC50 = 7.5 Binding
Displacement of Alexafluor488 labeled 4-(4-(1-(4-(1-(6-(4-(6-amino-3-imino-4,5-disulfo-3H-xanthen-9-yl)-3-carboxybenzamido)hexyl)-1H-1,2,3-triazol-4-yl)butyl)piperidin-4-yl)phenyl)-7-(4-(trifluoromethyl)phenyl)-2-naphthoic acid from HA-tagged mouse P2Y14 expressed in HEK293 cells measured after 30 mins by FACScalibur flow cytometry analysisDisplacement of Alexafluor488 labeled 4-(4-(1-(4-(1-(6-(4-(6-amino-3-imino-4,5-disulfo-3H-xanthen-9-yl)-3-carboxybenzamido)hexyl)-1H-1,2,3-triazol-4-yl)butyl)piperidin-4-yl)phenyl)-7-(4-(trifluoromethyl)phenyl)-2-naphthoic acid from HA-tagged mouse P2Y14 expressed in HEK293 cells measured after 30 mins by FACScalibur flow cytometry analysis
ChEMBL 517 4 1 2 7.6 CC(=O)N1CCC(c2ccc(-c3cc(C(=O)O)cc4cc(-c5ccc(C(F)(F)F)cc5)ccc34)cc2)CC1 10.1021/acsmedchemlett.0c00115
155770281 184526 0 None - 9 Mouse 7.5 pIC50 = 7.5 Binding
Inhibition of MRS4174 binding to mouse P2Y14R expressed in HEK293 cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins by flow cytomtery based competitive fluorescence assayInhibition of MRS4174 binding to mouse P2Y14R expressed in HEK293 cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins by flow cytomtery based competitive fluorescence assay
ChEMBL 517 4 1 2 7.6 CC(=O)N1CCC(c2ccc(-c3cc(C(=O)O)cc4cc(-c5ccc(C(F)(F)F)cc5)ccc34)cc2)CC1 10.1021/acs.jmedchem.0c00745
CHEMBL4642592 184526 0 None - 9 Mouse 7.5 pIC50 = 7.5 Binding
Inhibition of MRS4174 binding to mouse P2Y14R expressed in HEK293 cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins by flow cytomtery based competitive fluorescence assayInhibition of MRS4174 binding to mouse P2Y14R expressed in HEK293 cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins by flow cytomtery based competitive fluorescence assay
ChEMBL 517 4 1 2 7.6 CC(=O)N1CCC(c2ccc(-c3cc(C(=O)O)cc4cc(-c5ccc(C(F)(F)F)cc5)ccc34)cc2)CC1 10.1021/acs.jmedchem.0c00745
135357363 181274 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of 6-Amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy-6-(4-(trifluoromethyl)phenyl)-naphthalen-1-yl)phenyl)piperidin-1-yl)-butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)-phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate from human P2Y14R expressed in CHO cells measured after 15 mins by flow cytometric analysisDisplacement of 6-Amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy-6-(4-(trifluoromethyl)phenyl)-naphthalen-1-yl)phenyl)piperidin-1-yl)-butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)-phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate from human P2Y14R expressed in CHO cells measured after 15 mins by flow cytometric analysis
ChEMBL 458 5 2 5 5.4 O=C(O)c1cc(-c2ccc(C3CCNCC3)cc2)cc(-n2cc(-c3ccc(Cl)cc3)nn2)c1 10.1021/acs.jmedchem.6b00044
CHEMBL4554777 181274 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of 6-Amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy-6-(4-(trifluoromethyl)phenyl)-naphthalen-1-yl)phenyl)piperidin-1-yl)-butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)-phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate from human P2Y14R expressed in CHO cells measured after 15 mins by flow cytometric analysisDisplacement of 6-Amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy-6-(4-(trifluoromethyl)phenyl)-naphthalen-1-yl)phenyl)piperidin-1-yl)-butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)-phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate from human P2Y14R expressed in CHO cells measured after 15 mins by flow cytometric analysis
ChEMBL 458 5 2 5 5.4 O=C(O)c1cc(-c2ccc(C3CCNCC3)cc2)cc(-n2cc(-c3ccc(Cl)cc3)nn2)c1 10.1021/acs.jmedchem.6b00044
164585439 192665 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysisInhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysis
ChEMBL 466 7 2 5 5.2 NCCCc1ccc(-c2cc(C(=O)O)cc(-n3cc(-c4ccc(C(F)(F)F)cc4)nn3)c2)cc1 10.1021/acs.jmedchem.1c00164
CHEMBL4868306 192665 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysisInhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysis
ChEMBL 466 7 2 5 5.2 NCCCc1ccc(-c2cc(C(=O)O)cc(-n3cc(-c4ccc(C(F)(F)F)cc4)nn3)c2)cc1 10.1021/acs.jmedchem.1c00164
164585348 191431 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysisInhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysis
ChEMBL 493 5 2 6 5.2 O=C(O)c1cc(-n2cc(-c3ccc(C(F)(F)F)cc3)nn2)cc(-c2ccc(C3CCNCC3)cc2)n1 10.1021/acs.jmedchem.1c00164
CHEMBL4849653 191431 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysisInhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysis
ChEMBL 493 5 2 6 5.2 O=C(O)c1cc(-n2cc(-c3ccc(C(F)(F)F)cc3)nn2)cc(-c2ccc(C3CCNCC3)cc2)n1 10.1021/acs.jmedchem.1c00164
164585622 191707 0 None - 2 Human 6.5 pIC50 = 6.5 Binding
Inhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysisInhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysis
ChEMBL 506 6 2 7 5.5 O=C(O)c1cc(-c2ccc(-c3cc(CO)on3)cc2)cc(-n2cc(-c3ccc(C(F)(F)F)cc3)nn2)c1 10.1021/acs.jmedchem.1c00164
CHEMBL4853466 191707 0 None - 2 Human 6.5 pIC50 = 6.5 Binding
Inhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysisInhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysis
ChEMBL 506 6 2 7 5.5 O=C(O)c1cc(-c2ccc(-c3cc(CO)on3)cc2)cc(-n2cc(-c3ccc(C(F)(F)F)cc3)nn2)c1 10.1021/acs.jmedchem.1c00164
CHEMBL5085823 221771 4 None - 0 Human 8.5 pIC50 = 8.5 Binding
Inhibition of fluorescent antagonist binding to human P2Y14R expressed in CHO cells preincubated for 30 mins followed by 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy 6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate addition and measured after 30 mins by BD FACSCalibur flow cytometry analysisInhibition of fluorescent antagonist binding to human P2Y14R expressed in CHO cells preincubated for 30 mins followed by 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy 6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate addition and measured after 30 mins by BD FACSCalibur flow cytometry analysis
ChEMBL None None None O=C(O)c1cc(-c2ccc([C@H]3C[C@H]4C[C@@H]3CN4)cc2)c2ccc(-c3ccc(C(F)(F)F)cc3)cc2c1 10.1021/acs.jmedchem.1c01964
139406810 184006 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7.4 by flow cytomtery based competitive fluorescence assayInhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7.4 by flow cytomtery based competitive fluorescence assay
ChEMBL 428 5 3 3 4.4 NC(=O)c1ccc(-c2cc(NC(=O)c3ccc(C(F)(F)F)cc3)cc(C(=O)O)c2)cc1 10.1021/acs.jmedchem.0c00745
CHEMBL4635586 184006 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7.4 by flow cytomtery based competitive fluorescence assayInhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7.4 by flow cytomtery based competitive fluorescence assay
ChEMBL 428 5 3 3 4.4 NC(=O)c1ccc(-c2cc(NC(=O)c3ccc(C(F)(F)F)cc3)cc(C(=O)O)c2)cc1 10.1021/acs.jmedchem.0c00745
164585347 192518 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysisInhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysis
ChEMBL 462 4 2 5 4.6 NCC#Cc1ccc(-c2cc(C(=O)O)cc(-n3cc(-c4ccc(C(F)(F)F)cc4)nn3)c2)cc1 10.1021/acs.jmedchem.1c00164
CHEMBL4866107 192518 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysisInhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysis
ChEMBL 462 4 2 5 4.6 NCC#Cc1ccc(-c2cc(C(=O)O)cc(-n3cc(-c4ccc(C(F)(F)F)cc4)nn3)c2)cc1 10.1021/acs.jmedchem.1c00164
CHEMBL5094130 222255 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibition of fluorescent antagonist binding to human P2Y14R expressed in CHO cells preincubated for 30 mins followed by 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy 6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate addition and measured after 30 mins by BD FACSCalibur flow cytometry analysisInhibition of fluorescent antagonist binding to human P2Y14R expressed in CHO cells preincubated for 30 mins followed by 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy 6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate addition and measured after 30 mins by BD FACSCalibur flow cytometry analysis
ChEMBL None None None O=C(O)c1cc(-c2ccc(C3CCNC3)cc2)c2ccc(-c3ccc(C(F)(F)F)cc3)cc2c1 10.1021/acs.jmedchem.1c01964
132280527 177674 1 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of 6-Amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy-6-(4-(trifluoromethyl)phenyl)-naphthalen-1-yl)phenyl)piperidin-1-yl)-butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)-phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate from human P2Y14R expressed in CHO cells measured after 15 mins by flow cytometric analysisDisplacement of 6-Amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy-6-(4-(trifluoromethyl)phenyl)-naphthalen-1-yl)phenyl)piperidin-1-yl)-butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)-phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate from human P2Y14R expressed in CHO cells measured after 15 mins by flow cytometric analysis
ChEMBL 492 5 2 5 5.8 O=C(O)c1cc(-c2ccc(C3CCNCC3)cc2)cc(-n2cc(-c3ccc(C(F)(F)F)cc3)nn2)c1 10.1021/acs.jmedchem.6b00044
CHEMBL4454538 177674 1 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of 6-Amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy-6-(4-(trifluoromethyl)phenyl)-naphthalen-1-yl)phenyl)piperidin-1-yl)-butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)-phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate from human P2Y14R expressed in CHO cells measured after 15 mins by flow cytometric analysisDisplacement of 6-Amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy-6-(4-(trifluoromethyl)phenyl)-naphthalen-1-yl)phenyl)piperidin-1-yl)-butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)-phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate from human P2Y14R expressed in CHO cells measured after 15 mins by flow cytometric analysis
ChEMBL 492 5 2 5 5.8 O=C(O)c1cc(-c2ccc(C3CCNCC3)cc2)cc(-n2cc(-c3ccc(C(F)(F)F)cc3)nn2)c1 10.1021/acs.jmedchem.6b00044
132280527 177674 1 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of Alexafluor488 labeled 4-(4-(1-(4-(1-(6-(4-(6-amino-3-imino-4,5-disulfo-3H-xanthen-9-yl)-3-carboxybenzamido)hexyl)-1H-1,2,3-triazol-4-yl)butyl)piperidin-4-yl)phenyl)-7-(4-(trifluoromethyl)phenyl)-2-naphthoic acid from human P2Y14 expressed in CHO cells measured after 30 mins by FACScalibur flow cytometry analysisDisplacement of Alexafluor488 labeled 4-(4-(1-(4-(1-(6-(4-(6-amino-3-imino-4,5-disulfo-3H-xanthen-9-yl)-3-carboxybenzamido)hexyl)-1H-1,2,3-triazol-4-yl)butyl)piperidin-4-yl)phenyl)-7-(4-(trifluoromethyl)phenyl)-2-naphthoic acid from human P2Y14 expressed in CHO cells measured after 30 mins by FACScalibur flow cytometry analysis
ChEMBL 492 5 2 5 5.8 O=C(O)c1cc(-c2ccc(C3CCNCC3)cc2)cc(-n2cc(-c3ccc(C(F)(F)F)cc3)nn2)c1 10.1021/acsmedchemlett.0c00115
CHEMBL4454538 177674 1 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of Alexafluor488 labeled 4-(4-(1-(4-(1-(6-(4-(6-amino-3-imino-4,5-disulfo-3H-xanthen-9-yl)-3-carboxybenzamido)hexyl)-1H-1,2,3-triazol-4-yl)butyl)piperidin-4-yl)phenyl)-7-(4-(trifluoromethyl)phenyl)-2-naphthoic acid from human P2Y14 expressed in CHO cells measured after 30 mins by FACScalibur flow cytometry analysisDisplacement of Alexafluor488 labeled 4-(4-(1-(4-(1-(6-(4-(6-amino-3-imino-4,5-disulfo-3H-xanthen-9-yl)-3-carboxybenzamido)hexyl)-1H-1,2,3-triazol-4-yl)butyl)piperidin-4-yl)phenyl)-7-(4-(trifluoromethyl)phenyl)-2-naphthoic acid from human P2Y14 expressed in CHO cells measured after 30 mins by FACScalibur flow cytometry analysis
ChEMBL 492 5 2 5 5.8 O=C(O)c1cc(-c2ccc(C3CCNCC3)cc2)cc(-n2cc(-c3ccc(C(F)(F)F)cc3)nn2)c1 10.1021/acsmedchemlett.0c00115
145946347 174288 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric methodDisplacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric method
ChEMBL 442 5 2 6 4.0 NC(=O)c1ccc(-c2cc(C(=O)O)cc(-n3cc(-c4ccc(C(F)(F)F)cc4)nn3)c2)o1 10.1021/acs.jmedchem.8b00168
CHEMBL4209732 174288 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric methodDisplacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric method
ChEMBL 442 5 2 6 4.0 NC(=O)c1ccc(-c2cc(C(=O)O)cc(-n3cc(-c4ccc(C(F)(F)F)cc4)nn3)c2)o1 10.1021/acs.jmedchem.8b00168
CHEMBL4299839 174288 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric methodDisplacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric method
ChEMBL 442 5 2 6 4.0 NC(=O)c1ccc(-c2cc(C(=O)O)cc(-n3cc(-c4ccc(C(F)(F)F)cc4)nn3)c2)o1 10.1021/acs.jmedchem.8b00168
164585603 192390 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysisInhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysis
ChEMBL 524 5 2 6 6.7 CC(C)(C)OC(=O)Nc1ccc(-c2cc(C(=O)O)cc(-n3cc(-c4ccc(C(F)(F)F)cc4)nn3)c2)cc1 10.1021/acs.jmedchem.1c00164
CHEMBL4863984 192390 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysisInhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysis
ChEMBL 524 5 2 6 6.7 CC(C)(C)OC(=O)Nc1ccc(-c2cc(C(=O)O)cc(-n3cc(-c4ccc(C(F)(F)F)cc4)nn3)c2)cc1 10.1021/acs.jmedchem.1c00164
145978299 170505 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of Alexafluor488 labeled 4-(4-(1-(4-(1-(6-(4-(6-amino-3-imino-4,5-disulfo-3H-xanthen-9-yl)-3-carboxybenzamido)hexyl)-1H-1,2,3-triazol-4-yl)butyl)piperidin-4-yl)phenyl)-7-(4-(trifluoromethyl)phenyl)-2-naphthoic acid from human P2Y14 expressed in CHO cells measured after 30 mins by FACScalibur flow cytometry analysisDisplacement of Alexafluor488 labeled 4-(4-(1-(4-(1-(6-(4-(6-amino-3-imino-4,5-disulfo-3H-xanthen-9-yl)-3-carboxybenzamido)hexyl)-1H-1,2,3-triazol-4-yl)butyl)piperidin-4-yl)phenyl)-7-(4-(trifluoromethyl)phenyl)-2-naphthoic acid from human P2Y14 expressed in CHO cells measured after 30 mins by FACScalibur flow cytometry analysis
ChEMBL 332 2 2 2 4.9 O=C(O)c1cc(O)c2ccc(-c3ccc(C(F)(F)F)cc3)cc2c1 10.1021/acsmedchemlett.0c00115
CHEMBL4205190 170505 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of Alexafluor488 labeled 4-(4-(1-(4-(1-(6-(4-(6-amino-3-imino-4,5-disulfo-3H-xanthen-9-yl)-3-carboxybenzamido)hexyl)-1H-1,2,3-triazol-4-yl)butyl)piperidin-4-yl)phenyl)-7-(4-(trifluoromethyl)phenyl)-2-naphthoic acid from human P2Y14 expressed in CHO cells measured after 30 mins by FACScalibur flow cytometry analysisDisplacement of Alexafluor488 labeled 4-(4-(1-(4-(1-(6-(4-(6-amino-3-imino-4,5-disulfo-3H-xanthen-9-yl)-3-carboxybenzamido)hexyl)-1H-1,2,3-triazol-4-yl)butyl)piperidin-4-yl)phenyl)-7-(4-(trifluoromethyl)phenyl)-2-naphthoic acid from human P2Y14 expressed in CHO cells measured after 30 mins by FACScalibur flow cytometry analysis
ChEMBL 332 2 2 2 4.9 O=C(O)c1cc(O)c2ccc(-c3ccc(C(F)(F)F)cc3)cc2c1 10.1021/acsmedchemlett.0c00115
145978299 170505 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric methodDisplacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric method
ChEMBL 332 2 2 2 4.9 O=C(O)c1cc(O)c2ccc(-c3ccc(C(F)(F)F)cc3)cc2c1 10.1021/acs.jmedchem.8b00168
CHEMBL4205190 170505 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric methodDisplacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric method
ChEMBL 332 2 2 2 4.9 O=C(O)c1cc(O)c2ccc(-c3ccc(C(F)(F)F)cc3)cc2c1 10.1021/acs.jmedchem.8b00168
CHEMBL5085823 221771 4 None - 0 Mouse 7.5 pIC50 = 7.5 Binding
Inhibition of fluorescent antagonist binding to mouse P2Y14R expressed in HEK293 cells preincubated for 30 mins followed by addition of 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy-6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate incubated for 30 mins by BD FACSCalibur flow cytometry analysisInhibition of fluorescent antagonist binding to mouse P2Y14R expressed in HEK293 cells preincubated for 30 mins followed by addition of 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy-6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate incubated for 30 mins by BD FACSCalibur flow cytometry analysis
ChEMBL None None None O=C(O)c1cc(-c2ccc([C@H]3C[C@H]4C[C@@H]3CN4)cc2)c2ccc(-c3ccc(C(F)(F)F)cc3)cc2c1 10.1021/acs.jmedchem.1c01964
145964454 171237 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Displacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric methodDisplacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric method
ChEMBL 435 3 1 6 3.9 FC(F)(F)c1ccc(-c2cn(-c3cc(Br)cc(-c4nnn[nH]4)c3)nn2)cc1 10.1021/acs.jmedchem.8b00168
CHEMBL4214014 171237 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Displacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric methodDisplacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric method
ChEMBL 435 3 1 6 3.9 FC(F)(F)c1ccc(-c2cn(-c3cc(Br)cc(-c4nnn[nH]4)c3)nn2)cc1 10.1021/acs.jmedchem.8b00168
CHEMBL5078289 221328 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibition of fluorescent antagonist binding to human P2Y14R expressed in CHO cells preincubated for 30 mins followed by 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy 6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate addition and measured after 30 mins by BD FACSCalibur flow cytometry analysisInhibition of fluorescent antagonist binding to human P2Y14R expressed in CHO cells preincubated for 30 mins followed by 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy 6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate addition and measured after 30 mins by BD FACSCalibur flow cytometry analysis
ChEMBL None None None O=C(O)c1cc(-c2ccc(C3=CC4CCC(C3)N4)cc2)c2ccc(-c3ccc(C(F)(F)F)cc3)cc2c1 10.1021/acs.jmedchem.1c01964
19027172 68828 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Antagonist activity at human P2Y14 using UDP-Glc as substrateAntagonist activity at human P2Y14 using UDP-Glc as substrate
ChEMBL 354 5 1 2 5.8 O=C(O)c1cc(-c2ccccc2)c2ccc(OCc3ccccc3)cc2c1 10.1021/acs.jmedchem.5b01972
CHEMBL1774882 68828 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Antagonist activity at human P2Y14 using UDP-Glc as substrateAntagonist activity at human P2Y14 using UDP-Glc as substrate
ChEMBL 354 5 1 2 5.8 O=C(O)c1cc(-c2ccccc2)c2ccc(OCc3ccccc3)cc2c1 10.1021/acs.jmedchem.5b01972
139392339 184106 0 None - 1 Human 6.5 pIC50 = 6.5 Binding
Inhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7.4 by flow cytomtery based competitive fluorescence assayInhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7.4 by flow cytomtery based competitive fluorescence assay
ChEMBL 504 5 2 5 5.6 O=C(O)c1cc(-c2ccc(C34CCNCC3C4)cc2)cc(-n2cc(-c3ccc(C(F)(F)F)cc3)nn2)c1 10.1021/acs.jmedchem.0c00745
CHEMBL4637158 184106 0 None - 1 Human 6.5 pIC50 = 6.5 Binding
Inhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7.4 by flow cytomtery based competitive fluorescence assayInhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7.4 by flow cytomtery based competitive fluorescence assay
ChEMBL 504 5 2 5 5.6 O=C(O)c1cc(-c2ccc(C34CCNCC3C4)cc2)cc(-n2cc(-c3ccc(C(F)(F)F)cc3)nn2)c1 10.1021/acs.jmedchem.0c00745
164585473 191341 0 None - 5 Human 7.4 pIC50 = 7.4 Binding
Inhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysisInhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysis
ChEMBL 503 5 1 2 7.2 O=CN1CCC(c2ccc(-c3cc(C(=O)O)cc4cc(-c5ccc(C(F)(F)F)cc5)ccc34)cc2)CC1 10.1021/acs.jmedchem.1c00164
CHEMBL4848380 191341 0 None - 5 Human 7.4 pIC50 = 7.4 Binding
Inhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysisInhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysis
ChEMBL 503 5 1 2 7.2 O=CN1CCC(c2ccc(-c3cc(C(=O)O)cc4cc(-c5ccc(C(F)(F)F)cc5)ccc34)cc2)CC1 10.1021/acs.jmedchem.1c00164
122185397 129693 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity to human P2Y14 expressed in CHO cellsBinding affinity to human P2Y14 expressed in CHO cells
ChEMBL 420 6 6 9 -2.4 O=c1[nH]c(=O)n([C@@H]2O[C@H](COP(=O)(O)CP(=O)(O)O)[C@@H](O)[C@H]2O)cc1F 10.1016/j.bmcl.2021.128137
CHEMBL3606064 129693 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity to human P2Y14 expressed in CHO cellsBinding affinity to human P2Y14 expressed in CHO cells
ChEMBL 420 6 6 9 -2.4 O=c1[nH]c(=O)n([C@@H]2O[C@H](COP(=O)(O)CP(=O)(O)O)[C@@H](O)[C@H]2O)cc1F 10.1016/j.bmcl.2021.128137
CHEMBL4875504 129693 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity to human P2Y14 expressed in CHO cellsBinding affinity to human P2Y14 expressed in CHO cells
ChEMBL 420 6 6 9 -2.4 O=c1[nH]c(=O)n([C@@H]2O[C@H](COP(=O)(O)CP(=O)(O)O)[C@@H](O)[C@H]2O)cc1F 10.1016/j.bmcl.2021.128137
122185397 129693 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of 6-Amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy-6-(4-(trifluoromethyl)phenyl)-naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)-phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate from recombinant human P2Y14 receptor expressed in CHO cells preincubated for 30 mins followed by tracer addition and measured after 30 mins by flow cytometryDisplacement of 6-Amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy-6-(4-(trifluoromethyl)phenyl)-naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)-phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate from recombinant human P2Y14 receptor expressed in CHO cells preincubated for 30 mins followed by tracer addition and measured after 30 mins by flow cytometry
ChEMBL 420 6 6 9 -2.4 O=c1[nH]c(=O)n([C@@H]2O[C@H](COP(=O)(O)CP(=O)(O)O)[C@@H](O)[C@H]2O)cc1F 10.1021/acs.jmedchem.9b00164
CHEMBL3606064 129693 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of 6-Amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy-6-(4-(trifluoromethyl)phenyl)-naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)-phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate from recombinant human P2Y14 receptor expressed in CHO cells preincubated for 30 mins followed by tracer addition and measured after 30 mins by flow cytometryDisplacement of 6-Amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy-6-(4-(trifluoromethyl)phenyl)-naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)-phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate from recombinant human P2Y14 receptor expressed in CHO cells preincubated for 30 mins followed by tracer addition and measured after 30 mins by flow cytometry
ChEMBL 420 6 6 9 -2.4 O=c1[nH]c(=O)n([C@@H]2O[C@H](COP(=O)(O)CP(=O)(O)O)[C@@H](O)[C@H]2O)cc1F 10.1021/acs.jmedchem.9b00164
CHEMBL4875504 129693 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of 6-Amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy-6-(4-(trifluoromethyl)phenyl)-naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)-phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate from recombinant human P2Y14 receptor expressed in CHO cells preincubated for 30 mins followed by tracer addition and measured after 30 mins by flow cytometryDisplacement of 6-Amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy-6-(4-(trifluoromethyl)phenyl)-naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)-phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate from recombinant human P2Y14 receptor expressed in CHO cells preincubated for 30 mins followed by tracer addition and measured after 30 mins by flow cytometry
ChEMBL 420 6 6 9 -2.4 O=c1[nH]c(=O)n([C@@H]2O[C@H](COP(=O)(O)CP(=O)(O)O)[C@@H](O)[C@H]2O)cc1F 10.1021/acs.jmedchem.9b00164
CHEMBL5083773 221660 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of fluorescent antagonist binding to human P2Y14R expressed in CHO cells preincubated for 30 mins followed by 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy 6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate addition and measured after 30 mins by BD FACSCalibur flow cytometry analysisInhibition of fluorescent antagonist binding to human P2Y14R expressed in CHO cells preincubated for 30 mins followed by 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy 6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate addition and measured after 30 mins by BD FACSCalibur flow cytometry analysis
ChEMBL None None None O=C(O)c1cc(-c2ccc([C@@H]3C[C@@H]4C[C@H]3NC4=O)cc2)c2ccc(-c3ccc(C(F)(F)F)cc3)cc2c1 10.1021/acs.jmedchem.1c01964
164585347 192518 0 None - 0 Mouse 6.4 pIC50 = 6.4 Binding
Inhibition of fluorescent antagonist binding to mouse P2Y14 receptor expressed in HEK293 cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysisInhibition of fluorescent antagonist binding to mouse P2Y14 receptor expressed in HEK293 cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysis
ChEMBL 462 4 2 5 4.6 NCC#Cc1ccc(-c2cc(C(=O)O)cc(-n3cc(-c4ccc(C(F)(F)F)cc4)nn3)c2)cc1 10.1021/acs.jmedchem.1c00164
CHEMBL4866107 192518 0 None - 0 Mouse 6.4 pIC50 = 6.4 Binding
Inhibition of fluorescent antagonist binding to mouse P2Y14 receptor expressed in HEK293 cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysisInhibition of fluorescent antagonist binding to mouse P2Y14 receptor expressed in HEK293 cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysis
ChEMBL 462 4 2 5 4.6 NCC#Cc1ccc(-c2cc(C(=O)O)cc(-n3cc(-c4ccc(C(F)(F)F)cc4)nn3)c2)cc1 10.1021/acs.jmedchem.1c00164
155770279 185001 0 None - 0 Mouse 7.4 pIC50 = 7.4 Binding
Displacement of Alexafluor488 labeled 4-(4-(1-(4-(1-(6-(4-(6-amino-3-imino-4,5-disulfo-3H-xanthen-9-yl)-3-carboxybenzamido)hexyl)-1H-1,2,3-triazol-4-yl)butyl)piperidin-4-yl)phenyl)-7-(4-(trifluoromethyl)phenyl)-2-naphthoic acid from HA-tagged mouse P2Y14 expressed in HEK293 cells measured after 30 mins by FACScalibur flow cytometry analysisDisplacement of Alexafluor488 labeled 4-(4-(1-(4-(1-(6-(4-(6-amino-3-imino-4,5-disulfo-3H-xanthen-9-yl)-3-carboxybenzamido)hexyl)-1H-1,2,3-triazol-4-yl)butyl)piperidin-4-yl)phenyl)-7-(4-(trifluoromethyl)phenyl)-2-naphthoic acid from HA-tagged mouse P2Y14 expressed in HEK293 cells measured after 30 mins by FACScalibur flow cytometry analysis
ChEMBL 531 5 1 2 8.0 CCC(=O)N1CCC(c2ccc(-c3cc(C(=O)O)cc4cc(-c5ccc(C(F)(F)F)cc5)ccc34)cc2)CC1 10.1021/acsmedchemlett.0c00115
CHEMBL4649855 185001 0 None - 0 Mouse 7.4 pIC50 = 7.4 Binding
Displacement of Alexafluor488 labeled 4-(4-(1-(4-(1-(6-(4-(6-amino-3-imino-4,5-disulfo-3H-xanthen-9-yl)-3-carboxybenzamido)hexyl)-1H-1,2,3-triazol-4-yl)butyl)piperidin-4-yl)phenyl)-7-(4-(trifluoromethyl)phenyl)-2-naphthoic acid from HA-tagged mouse P2Y14 expressed in HEK293 cells measured after 30 mins by FACScalibur flow cytometry analysisDisplacement of Alexafluor488 labeled 4-(4-(1-(4-(1-(6-(4-(6-amino-3-imino-4,5-disulfo-3H-xanthen-9-yl)-3-carboxybenzamido)hexyl)-1H-1,2,3-triazol-4-yl)butyl)piperidin-4-yl)phenyl)-7-(4-(trifluoromethyl)phenyl)-2-naphthoic acid from HA-tagged mouse P2Y14 expressed in HEK293 cells measured after 30 mins by FACScalibur flow cytometry analysis
ChEMBL 531 5 1 2 8.0 CCC(=O)N1CCC(c2ccc(-c3cc(C(=O)O)cc4cc(-c5ccc(C(F)(F)F)cc5)ccc34)cc2)CC1 10.1021/acsmedchemlett.0c00115
139392013 184694 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7 by flow cytomtery based competitive fluorescence assayInhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7 by flow cytomtery based competitive fluorescence assay
ChEMBL 501 4 1 2 7.6 O=C(O)c1cc(-c2ccc(C34CCN(CC3)CC4)cc2)c2ccc(-c3ccc(C(F)(F)F)cc3)cc2c1 10.1021/acs.jmedchem.0c00745
CHEMBL4645216 184694 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7 by flow cytomtery based competitive fluorescence assayInhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7 by flow cytomtery based competitive fluorescence assay
ChEMBL 501 4 1 2 7.6 O=C(O)c1cc(-c2ccc(C34CCN(CC3)CC4)cc2)c2ccc(-c3ccc(C(F)(F)F)cc3)cc2c1 10.1021/acs.jmedchem.0c00745
156015426 184334 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7.4 by flow cytomtery based competitive fluorescence assayInhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7.4 by flow cytomtery based competitive fluorescence assay
ChEMBL 516 4 1 1 7.8 C[N+]12CCC(c3ccc(-c4cc(C(=O)O)cc5cc(-c6ccc(C(F)(F)F)cc6)ccc45)cc3)(CC1)CC2 10.1021/acs.jmedchem.0c00745
CHEMBL4640370 184334 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7.4 by flow cytomtery based competitive fluorescence assayInhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7.4 by flow cytomtery based competitive fluorescence assay
ChEMBL 516 4 1 1 7.8 C[N+]12CCC(c3ccc(-c4cc(C(=O)O)cc5cc(-c6ccc(C(F)(F)F)cc6)ccc45)cc3)(CC1)CC2 10.1021/acs.jmedchem.0c00745
CHEMBL5078543 221340 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of fluorescent antagonist binding to human P2Y14R expressed in CHO cells preincubated for 30 mins followed by 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy 6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate addition and measured after 30 mins by BD FACSCalibur flow cytometry analysisInhibition of fluorescent antagonist binding to human P2Y14R expressed in CHO cells preincubated for 30 mins followed by 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy 6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate addition and measured after 30 mins by BD FACSCalibur flow cytometry analysis
ChEMBL None None None O=C(O)c1cc(-c2ccc(C3CC4CCC(C3)N4)cc2)c2ccc(-c3ccc(C(F)(F)F)cc3)cc2c1 10.1021/acs.jmedchem.1c01964
134611895 9447 4 None - 2 Mouse 6.4 pIC50 = 6.4 Binding
Displacement of Alexafluor488 labeled 4-(4-(1-(4-(1-(6-(4-(6-amino-3-imino-4,5-disulfo-3H-xanthen-9-yl)-3-carboxybenzamido)hexyl)-1H-1,2,3-triazol-4-yl)butyl)piperidin-4-yl)phenyl)-7-(4-(trifluoromethyl)phenyl)-2-naphthoic acid from HA-tagged mouse P2Y14 expressed in HEK293 cells measured after 30 mins by FACScalibur flow cytometry analysisDisplacement of Alexafluor488 labeled 4-(4-(1-(4-(1-(6-(4-(6-amino-3-imino-4,5-disulfo-3H-xanthen-9-yl)-3-carboxybenzamido)hexyl)-1H-1,2,3-triazol-4-yl)butyl)piperidin-4-yl)phenyl)-7-(4-(trifluoromethyl)phenyl)-2-naphthoic acid from HA-tagged mouse P2Y14 expressed in HEK293 cells measured after 30 mins by FACScalibur flow cytometry analysis
ChEMBL 515 8 3 7 4.5 NCCCNC(=O)c1ccc(s1)c1cc(cc(c1)n1nnc(c1)c1ccc(cc1)C(F)(F)F)C(=O)O 10.1021/acsmedchemlett.0c00115
9998 9447 4 None - 2 Mouse 6.4 pIC50 = 6.4 Binding
Displacement of Alexafluor488 labeled 4-(4-(1-(4-(1-(6-(4-(6-amino-3-imino-4,5-disulfo-3H-xanthen-9-yl)-3-carboxybenzamido)hexyl)-1H-1,2,3-triazol-4-yl)butyl)piperidin-4-yl)phenyl)-7-(4-(trifluoromethyl)phenyl)-2-naphthoic acid from HA-tagged mouse P2Y14 expressed in HEK293 cells measured after 30 mins by FACScalibur flow cytometry analysisDisplacement of Alexafluor488 labeled 4-(4-(1-(4-(1-(6-(4-(6-amino-3-imino-4,5-disulfo-3H-xanthen-9-yl)-3-carboxybenzamido)hexyl)-1H-1,2,3-triazol-4-yl)butyl)piperidin-4-yl)phenyl)-7-(4-(trifluoromethyl)phenyl)-2-naphthoic acid from HA-tagged mouse P2Y14 expressed in HEK293 cells measured after 30 mins by FACScalibur flow cytometry analysis
ChEMBL 515 8 3 7 4.5 NCCCNC(=O)c1ccc(s1)c1cc(cc(c1)n1nnc(c1)c1ccc(cc1)C(F)(F)F)C(=O)O 10.1021/acsmedchemlett.0c00115
CHEMBL4212721 9447 4 None - 2 Mouse 6.4 pIC50 = 6.4 Binding
Displacement of Alexafluor488 labeled 4-(4-(1-(4-(1-(6-(4-(6-amino-3-imino-4,5-disulfo-3H-xanthen-9-yl)-3-carboxybenzamido)hexyl)-1H-1,2,3-triazol-4-yl)butyl)piperidin-4-yl)phenyl)-7-(4-(trifluoromethyl)phenyl)-2-naphthoic acid from HA-tagged mouse P2Y14 expressed in HEK293 cells measured after 30 mins by FACScalibur flow cytometry analysisDisplacement of Alexafluor488 labeled 4-(4-(1-(4-(1-(6-(4-(6-amino-3-imino-4,5-disulfo-3H-xanthen-9-yl)-3-carboxybenzamido)hexyl)-1H-1,2,3-triazol-4-yl)butyl)piperidin-4-yl)phenyl)-7-(4-(trifluoromethyl)phenyl)-2-naphthoic acid from HA-tagged mouse P2Y14 expressed in HEK293 cells measured after 30 mins by FACScalibur flow cytometry analysis
ChEMBL 515 8 3 7 4.5 NCCCNC(=O)c1ccc(s1)c1cc(cc(c1)n1nnc(c1)c1ccc(cc1)C(F)(F)F)C(=O)O 10.1021/acsmedchemlett.0c00115
134611895 9447 4 None - 2 Mouse 6.4 pIC50 = 6.4 Binding
Inhibition of MRS4174 binding to mouse P2Y14R expressed in HEK293 cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins by flow cytomtery based competitive fluorescence assayInhibition of MRS4174 binding to mouse P2Y14R expressed in HEK293 cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins by flow cytomtery based competitive fluorescence assay
ChEMBL 515 8 3 7 4.5 NCCCNC(=O)c1ccc(s1)c1cc(cc(c1)n1nnc(c1)c1ccc(cc1)C(F)(F)F)C(=O)O 10.1021/acs.jmedchem.0c00745
9998 9447 4 None - 2 Mouse 6.4 pIC50 = 6.4 Binding
Inhibition of MRS4174 binding to mouse P2Y14R expressed in HEK293 cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins by flow cytomtery based competitive fluorescence assayInhibition of MRS4174 binding to mouse P2Y14R expressed in HEK293 cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins by flow cytomtery based competitive fluorescence assay
ChEMBL 515 8 3 7 4.5 NCCCNC(=O)c1ccc(s1)c1cc(cc(c1)n1nnc(c1)c1ccc(cc1)C(F)(F)F)C(=O)O 10.1021/acs.jmedchem.0c00745
CHEMBL4212721 9447 4 None - 2 Mouse 6.4 pIC50 = 6.4 Binding
Inhibition of MRS4174 binding to mouse P2Y14R expressed in HEK293 cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins by flow cytomtery based competitive fluorescence assayInhibition of MRS4174 binding to mouse P2Y14R expressed in HEK293 cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins by flow cytomtery based competitive fluorescence assay
ChEMBL 515 8 3 7 4.5 NCCCNC(=O)c1ccc(s1)c1cc(cc(c1)n1nnc(c1)c1ccc(cc1)C(F)(F)F)C(=O)O 10.1021/acs.jmedchem.0c00745
164585384 191283 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysisInhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysis
ChEMBL 520 7 2 7 5.5 O=C(O)c1cc(-c2ccc(-c3cc(CCO)on3)cc2)cc(-n2cc(-c3ccc(C(F)(F)F)cc3)nn2)c1 10.1021/acs.jmedchem.1c00164
CHEMBL4847409 191283 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysisInhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysis
ChEMBL 520 7 2 7 5.5 O=C(O)c1cc(-c2ccc(-c3cc(CCO)on3)cc2)cc(-n2cc(-c3ccc(C(F)(F)F)cc3)nn2)c1 10.1021/acs.jmedchem.1c00164
CHEMBL5076127 221194 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of fluorescent antagonist binding to human P2Y14R expressed in CHO cells preincubated for 30 mins followed by 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy 6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate addition and measured after 30 mins by BD FACSCalibur flow cytometry analysisInhibition of fluorescent antagonist binding to human P2Y14R expressed in CHO cells preincubated for 30 mins followed by 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy 6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate addition and measured after 30 mins by BD FACSCalibur flow cytometry analysis
ChEMBL None None None O=C(O)c1cc(-c2ccc([C@@H]3C[C@@H]4C[C@H]3C(=O)N4)cc2)c2ccc(-c3ccc(C(F)(F)F)cc3)cc2c1 10.1021/acs.jmedchem.1c01964
CHEMBL5076678 221236 0 None - 0 Mouse 7.4 pIC50 = 7.4 Binding
Inhibition of fluorescent antagonist binding to mouse P2Y14R expressed in HEK293 cells preincubated for 30 mins followed by addition of 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy-6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate incubated for 30 mins by BD FACSCalibur flow cytometry analysisInhibition of fluorescent antagonist binding to mouse P2Y14R expressed in HEK293 cells preincubated for 30 mins followed by addition of 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy-6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate incubated for 30 mins by BD FACSCalibur flow cytometry analysis
ChEMBL None None None N[C@@H]1C[C@H](C(=O)O)[C@@H](c2ccc(-c3cc(C(=O)O)cc4cc(-c5ccc(C(F)(F)F)cc5)ccc34)cc2)C1 10.1021/acs.jmedchem.1c01964
155770279 185001 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of Alexafluor488 labeled 4-(4-(1-(4-(1-(6-(4-(6-amino-3-imino-4,5-disulfo-3H-xanthen-9-yl)-3-carboxybenzamido)hexyl)-1H-1,2,3-triazol-4-yl)butyl)piperidin-4-yl)phenyl)-7-(4-(trifluoromethyl)phenyl)-2-naphthoic acid from human P2Y14 expressed in CHO cells measured after 30 mins by FACScalibur flow cytometry analysisDisplacement of Alexafluor488 labeled 4-(4-(1-(4-(1-(6-(4-(6-amino-3-imino-4,5-disulfo-3H-xanthen-9-yl)-3-carboxybenzamido)hexyl)-1H-1,2,3-triazol-4-yl)butyl)piperidin-4-yl)phenyl)-7-(4-(trifluoromethyl)phenyl)-2-naphthoic acid from human P2Y14 expressed in CHO cells measured after 30 mins by FACScalibur flow cytometry analysis
ChEMBL 531 5 1 2 8.0 CCC(=O)N1CCC(c2ccc(-c3cc(C(=O)O)cc4cc(-c5ccc(C(F)(F)F)cc5)ccc34)cc2)CC1 10.1021/acsmedchemlett.0c00115
CHEMBL4649855 185001 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of Alexafluor488 labeled 4-(4-(1-(4-(1-(6-(4-(6-amino-3-imino-4,5-disulfo-3H-xanthen-9-yl)-3-carboxybenzamido)hexyl)-1H-1,2,3-triazol-4-yl)butyl)piperidin-4-yl)phenyl)-7-(4-(trifluoromethyl)phenyl)-2-naphthoic acid from human P2Y14 expressed in CHO cells measured after 30 mins by FACScalibur flow cytometry analysisDisplacement of Alexafluor488 labeled 4-(4-(1-(4-(1-(6-(4-(6-amino-3-imino-4,5-disulfo-3H-xanthen-9-yl)-3-carboxybenzamido)hexyl)-1H-1,2,3-triazol-4-yl)butyl)piperidin-4-yl)phenyl)-7-(4-(trifluoromethyl)phenyl)-2-naphthoic acid from human P2Y14 expressed in CHO cells measured after 30 mins by FACScalibur flow cytometry analysis
ChEMBL 531 5 1 2 8.0 CCC(=O)N1CCC(c2ccc(-c3cc(C(=O)O)cc4cc(-c5ccc(C(F)(F)F)cc5)ccc34)cc2)CC1 10.1021/acsmedchemlett.0c00115
CHEMBL5081216 221513 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of fluorescent antagonist binding to human P2Y14R expressed in CHO cells preincubated for 30 mins followed by 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy 6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate addition and measured after 30 mins by BD FACSCalibur flow cytometry analysisInhibition of fluorescent antagonist binding to human P2Y14R expressed in CHO cells preincubated for 30 mins followed by 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy 6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate addition and measured after 30 mins by BD FACSCalibur flow cytometry analysis
ChEMBL None None None O=C(O)c1cc(-c2ccc([C@H]3CCN[C@@H]4C[C@H]34)cc2)c2ccc(-c3ccc(C(F)(F)F)cc3)cc2c1 10.1021/acs.jmedchem.1c01964
CHEMBL5083773 221660 0 None - 0 Mouse 7.4 pIC50 = 7.4 Binding
Inhibition of fluorescent antagonist binding to mouse P2Y14R expressed in HEK293 cells preincubated for 30 mins followed by addition of 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy-6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate incubated for 30 mins by BD FACSCalibur flow cytometry analysisInhibition of fluorescent antagonist binding to mouse P2Y14R expressed in HEK293 cells preincubated for 30 mins followed by addition of 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy-6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate incubated for 30 mins by BD FACSCalibur flow cytometry analysis
ChEMBL None None None O=C(O)c1cc(-c2ccc([C@@H]3C[C@@H]4C[C@H]3NC4=O)cc2)c2ccc(-c3ccc(C(F)(F)F)cc3)cc2c1 10.1021/acs.jmedchem.1c01964
139406783 184267 0 None - 0 Human 4.4 pIC50 = 4.4 Binding
Inhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7.4 by flow cytomtery based competitive fluorescence assayInhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7.4 by flow cytomtery based competitive fluorescence assay
ChEMBL 473 4 1 5 6.0 N#Cc1cc(-c2ccc(C3CCNCC3)cc2)cc(-n2cc(-c3ccc(C(F)(F)F)cc3)nn2)c1 10.1021/acs.jmedchem.0c00745
CHEMBL4639356 184267 0 None - 0 Human 4.4 pIC50 = 4.4 Binding
Inhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7.4 by flow cytomtery based competitive fluorescence assayInhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7.4 by flow cytomtery based competitive fluorescence assay
ChEMBL 473 4 1 5 6.0 N#Cc1cc(-c2ccc(C3CCNCC3)cc2)cc(-n2cc(-c3ccc(C(F)(F)F)cc3)nn2)c1 10.1021/acs.jmedchem.0c00745
164585342 192739 0 None - 0 Human 4.4 pIC50 = 4.4 Binding
Inhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysisInhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysis
ChEMBL 566 8 2 6 6.8 CC(C)(C)OC(=O)NCCCc1ccc(-c2cc(C(=O)O)cc(-n3cc(-c4ccc(C(F)(F)F)cc4)nn3)c2)cc1 10.1021/acs.jmedchem.1c00164
CHEMBL4869611 192739 0 None - 0 Human 4.4 pIC50 = 4.4 Binding
Inhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysisInhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysis
ChEMBL 566 8 2 6 6.8 CC(C)(C)OC(=O)NCCCc1ccc(-c2cc(C(=O)O)cc(-n3cc(-c4ccc(C(F)(F)F)cc4)nn3)c2)cc1 10.1021/acs.jmedchem.1c00164
CHEMBL4566600 220793 0 None -4 6 Human 5.4 pIC50 = 5.4 Binding
Affinity Biochemical interaction (FLIPR assay) EUB0000337aCl P2RY14Affinity Biochemical interaction (FLIPR assay) EUB0000337aCl P2RY14
ChEMBL None None None Cc1c(C(=O)O)cc(-c2ccc(C3CCNCC3)cc2)c2ccc(-c3ccc(C(F)(F)F)cc3)cc12 10.6019/CHEMBL5210307
CHEMBL4745071 220793 0 None -4 6 Human 5.4 pIC50 = 5.4 Binding
Affinity Biochemical interaction (FLIPR assay) EUB0000337aCl P2RY14Affinity Biochemical interaction (FLIPR assay) EUB0000337aCl P2RY14
ChEMBL None None None Cc1c(C(=O)O)cc(-c2ccc(C3CCNCC3)cc2)c2ccc(-c3ccc(C(F)(F)F)cc3)cc12 10.6019/CHEMBL5210307
CHEMBL5079780 221419 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of fluorescent antagonist binding to human P2Y14R expressed in CHO cells preincubated for 30 mins followed by 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy 6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate addition and measured after 30 mins by BD FACSCalibur flow cytometry analysisInhibition of fluorescent antagonist binding to human P2Y14R expressed in CHO cells preincubated for 30 mins followed by 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy 6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate addition and measured after 30 mins by BD FACSCalibur flow cytometry analysis
ChEMBL None None None COC1(c2ccc(-c3cc(C(=O)O)cc4cc(-c5ccc(C(F)(F)F)cc5)ccc34)cc2)[C@H]2CC[C@H]1CNC2 10.1021/acs.jmedchem.1c01964
CHEMBL5081827 221550 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of fluorescent antagonist binding to human P2Y14R expressed in CHO cells preincubated for 30 mins followed by 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy 6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate addition and measured after 30 mins by BD FACSCalibur flow cytometry analysisInhibition of fluorescent antagonist binding to human P2Y14R expressed in CHO cells preincubated for 30 mins followed by 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy 6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate addition and measured after 30 mins by BD FACSCalibur flow cytometry analysis
ChEMBL None None None CCOC(=O)N1C[C@H]2C[C@@H]1C[C@@H]2c1ccc(-c2cc(C(=O)O)cc3cc(-c4ccc(C(F)(F)F)cc4)ccc23)cc1 10.1021/acs.jmedchem.1c01964
CHEMBL5077557 221282 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibition of fluorescent antagonist binding to human P2Y14R expressed in CHO cells preincubated for 30 mins followed by 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy 6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate addition and measured after 30 mins by BD FACSCalibur flow cytometry analysisInhibition of fluorescent antagonist binding to human P2Y14R expressed in CHO cells preincubated for 30 mins followed by 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy 6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate addition and measured after 30 mins by BD FACSCalibur flow cytometry analysis
ChEMBL None None None O=C(O)c1cc(-c2ccc(C34CCNCC3C4)cc2)c2ccc(-c3ccc(C(F)(F)F)cc3)cc2c1 10.1021/acs.jmedchem.1c01964
CHEMBL5075522 221161 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of fluorescent antagonist binding to human P2Y14R expressed in CHO cells preincubated for 30 mins followed by 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy 6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate addition and measured after 30 mins by BD FACSCalibur flow cytometry analysisInhibition of fluorescent antagonist binding to human P2Y14R expressed in CHO cells preincubated for 30 mins followed by 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy 6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate addition and measured after 30 mins by BD FACSCalibur flow cytometry analysis
ChEMBL None None None O=C(O)c1cc(-c2ccc(C3(O)[C@H]4CC[C@H]3CN(Cc3ccccc3)C4)cc2)c2ccc(-c3ccc(C(F)(F)F)cc3)cc2c1 10.1021/acs.jmedchem.1c01964
135356879 181449 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of 6-Amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy-6-(4-(trifluoromethyl)phenyl)-naphthalen-1-yl)phenyl)piperidin-1-yl)-butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)-phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate from human P2Y14R expressed in CHO cells measured after 15 mins by flow cytometric analysisDisplacement of 6-Amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy-6-(4-(trifluoromethyl)phenyl)-naphthalen-1-yl)phenyl)piperidin-1-yl)-butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)-phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate from human P2Y14R expressed in CHO cells measured after 15 mins by flow cytometric analysis
ChEMBL 466 6 2 5 5.9 CC(C)c1ccc(-c2cn(-c3cc(C(=O)O)cc(-c4ccc(C5CCNCC5)cc4)c3)nn2)cc1 10.1021/acs.jmedchem.6b00044
CHEMBL4558911 181449 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of 6-Amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy-6-(4-(trifluoromethyl)phenyl)-naphthalen-1-yl)phenyl)piperidin-1-yl)-butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)-phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate from human P2Y14R expressed in CHO cells measured after 15 mins by flow cytometric analysisDisplacement of 6-Amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy-6-(4-(trifluoromethyl)phenyl)-naphthalen-1-yl)phenyl)piperidin-1-yl)-butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)-phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate from human P2Y14R expressed in CHO cells measured after 15 mins by flow cytometric analysis
ChEMBL 466 6 2 5 5.9 CC(C)c1ccc(-c2cn(-c3cc(C(=O)O)cc(-c4ccc(C5CCNCC5)cc4)c3)nn2)cc1 10.1021/acs.jmedchem.6b00044
156020230 184953 0 None - 0 Mouse 6.3 pIC50 = 6.3 Binding
Inhibition of MRS4174 binding to mouse P2Y14R expressed in HEK293 cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins by flow cytomtery based competitive fluorescence assayInhibition of MRS4174 binding to mouse P2Y14R expressed in HEK293 cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins by flow cytomtery based competitive fluorescence assay
ChEMBL 854 27 2 10 7.1 NCCOCCOCCOCCOCCOCCOCCOCCC(=O)N1CCC(c2ccc(-c3cc(C(=O)O)cc4cc(-c5ccc(C(F)(F)F)cc5)ccc34)cc2)CC1 10.1021/acs.jmedchem.0c00745
CHEMBL4649194 184953 0 None - 0 Mouse 6.3 pIC50 = 6.3 Binding
Inhibition of MRS4174 binding to mouse P2Y14R expressed in HEK293 cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins by flow cytomtery based competitive fluorescence assayInhibition of MRS4174 binding to mouse P2Y14R expressed in HEK293 cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins by flow cytomtery based competitive fluorescence assay
ChEMBL 854 27 2 10 7.1 NCCOCCOCCOCCOCCOCCOCCOCCC(=O)N1CCC(c2ccc(-c3cc(C(=O)O)cc4cc(-c5ccc(C(F)(F)F)cc5)ccc34)cc2)CC1 10.1021/acs.jmedchem.0c00745
CHEMBL5076678 221236 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibition of fluorescent antagonist binding to human P2Y14R expressed in CHO cells preincubated for 30 mins followed by 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy 6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate addition and measured after 30 mins by BD FACSCalibur flow cytometry analysisInhibition of fluorescent antagonist binding to human P2Y14R expressed in CHO cells preincubated for 30 mins followed by 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy 6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate addition and measured after 30 mins by BD FACSCalibur flow cytometry analysis
ChEMBL None None None N[C@@H]1C[C@H](C(=O)O)[C@@H](c2ccc(-c3cc(C(=O)O)cc4cc(-c5ccc(C(F)(F)F)cc5)ccc34)cc2)C1 10.1021/acs.jmedchem.1c01964
164585561 192690 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysisInhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysis
ChEMBL 493 5 2 6 5.2 O=C(O)c1cc(-c2ccc(C3CCNCC3)cc2)nc(-n2cc(-c3ccc(C(F)(F)F)cc3)nn2)c1 10.1021/acs.jmedchem.1c00164
CHEMBL4868823 192690 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysisInhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysis
ChEMBL 493 5 2 6 5.2 O=C(O)c1cc(-c2ccc(C3CCNCC3)cc2)nc(-n2cc(-c3ccc(C(F)(F)F)cc3)nn2)c1 10.1021/acs.jmedchem.1c00164
CHEMBL5090079 222020 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of fluorescent antagonist binding to human P2Y14R expressed in CHO cells preincubated for 30 mins followed by 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy 6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate addition and measured after 30 mins by BD FACSCalibur flow cytometry analysisInhibition of fluorescent antagonist binding to human P2Y14R expressed in CHO cells preincubated for 30 mins followed by 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy 6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate addition and measured after 30 mins by BD FACSCalibur flow cytometry analysis
ChEMBL None None None CS(=O)(=O)C1C[C@H]2C[C@@H]1C[C@@H]2c1ccc(-c2cc(C(=O)O)cc3cc(-c4ccc(C(F)(F)F)cc4)ccc23)cc1 10.1021/acs.jmedchem.1c01964
139392022 184749 0 None - 0 Mouse 6.3 pIC50 = 6.3 Binding
Inhibition of MRS4174 binding to mouse P2Y14R expressed in HEK293 cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins by flow cytomtery based competitive fluorescence assayInhibition of MRS4174 binding to mouse P2Y14R expressed in HEK293 cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins by flow cytomtery based competitive fluorescence assay
ChEMBL 493 5 2 6 4.7 O=C(O)c1cc(-c2ccc(N3CCNCC3)cc2)cc(-n2cc(-c3ccc(C(F)(F)F)cc3)nn2)c1 10.1021/acs.jmedchem.0c00745
CHEMBL4645987 184749 0 None - 0 Mouse 6.3 pIC50 = 6.3 Binding
Inhibition of MRS4174 binding to mouse P2Y14R expressed in HEK293 cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins by flow cytomtery based competitive fluorescence assayInhibition of MRS4174 binding to mouse P2Y14R expressed in HEK293 cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins by flow cytomtery based competitive fluorescence assay
ChEMBL 493 5 2 6 4.7 O=C(O)c1cc(-c2ccc(N3CCNCC3)cc2)cc(-n2cc(-c3ccc(C(F)(F)F)cc3)nn2)c1 10.1021/acs.jmedchem.0c00745
CHEMBL5085823 221771 4 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibition of fluorescent antagonist binding to human P2Y14R expressed in CHO cells preincubated for 30 mins followed by 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy 6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate addition and measured after 30 mins by BD FACSCalibur flow cytometry analysisInhibition of fluorescent antagonist binding to human P2Y14R expressed in CHO cells preincubated for 30 mins followed by 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy 6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate addition and measured after 30 mins by BD FACSCalibur flow cytometry analysis
ChEMBL None None None O=C(O)c1cc(-c2ccc([C@H]3C[C@H]4C[C@@H]3CN4)cc2)c2ccc(-c3ccc(C(F)(F)F)cc3)cc2c1 10.1021/acs.jmedchem.1c01964
145946301 174285 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric methodDisplacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric method
ChEMBL 453 5 2 6 3.8 NC(=O)c1ccc(-c2cc(C(=O)O)cc(-n3cc(-c4ccc(C(F)(F)F)cc4)nn3)c2)nc1 10.1021/acs.jmedchem.8b00168
CHEMBL4211172 174285 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric methodDisplacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric method
ChEMBL 453 5 2 6 3.8 NC(=O)c1ccc(-c2cc(C(=O)O)cc(-n3cc(-c4ccc(C(F)(F)F)cc4)nn3)c2)nc1 10.1021/acs.jmedchem.8b00168
CHEMBL4299823 174285 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric methodDisplacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric method
ChEMBL 453 5 2 6 3.8 NC(=O)c1ccc(-c2cc(C(=O)O)cc(-n3cc(-c4ccc(C(F)(F)F)cc4)nn3)c2)nc1 10.1021/acs.jmedchem.8b00168
145977351 170512 0 None - 0 Human 4.3 pIC50 = 4.3 Binding
Displacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric methodDisplacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric method
ChEMBL 627 5 1 8 6.1 CC(C)(C)OC(=O)N1CCN(C(=O)c2ccc(-c3cc(C(=O)O)cc(-n4cc(-c5ccc(C(F)(F)F)cc5)nn4)c3)s2)CC1 10.1021/acs.jmedchem.8b00168
CHEMBL4205258 170512 0 None - 0 Human 4.3 pIC50 = 4.3 Binding
Displacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric methodDisplacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric method
ChEMBL 627 5 1 8 6.1 CC(C)(C)OC(=O)N1CCN(C(=O)c2ccc(-c3cc(C(=O)O)cc(-n4cc(-c5ccc(C(F)(F)F)cc5)nn4)c3)s2)CC1 10.1021/acs.jmedchem.8b00168
145978183 170764 0 None - 0 Human 4.3 pIC50 = 4.3 Binding
Displacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric methodDisplacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric method
ChEMBL 663 6 1 9 5.6 CC(C)(C)OC(=O)N1CCN(S(=O)(=O)c2ccc(-c3cc(C(=O)O)cc(-n4cc(-c5ccc(C(F)(F)F)cc5)nn4)c3)s2)CC1 10.1021/acs.jmedchem.8b00168
CHEMBL4208103 170764 0 None - 0 Human 4.3 pIC50 = 4.3 Binding
Displacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric methodDisplacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric method
ChEMBL 663 6 1 9 5.6 CC(C)(C)OC(=O)N1CCN(S(=O)(=O)c2ccc(-c3cc(C(=O)O)cc(-n4cc(-c5ccc(C(F)(F)F)cc5)nn4)c3)s2)CC1 10.1021/acs.jmedchem.8b00168
156015426 184334 0 None - 0 Mouse 7.3 pIC50 = 7.3 Binding
Inhibition of MRS4174 binding to mouse P2Y14R expressed in HEK293 cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins by flow cytomtery based competitive fluorescence assayInhibition of MRS4174 binding to mouse P2Y14R expressed in HEK293 cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins by flow cytomtery based competitive fluorescence assay
ChEMBL 516 4 1 1 7.8 C[N+]12CCC(c3ccc(-c4cc(C(=O)O)cc5cc(-c6ccc(C(F)(F)F)cc6)ccc45)cc3)(CC1)CC2 10.1021/acs.jmedchem.0c00745
CHEMBL4640370 184334 0 None - 0 Mouse 7.3 pIC50 = 7.3 Binding
Inhibition of MRS4174 binding to mouse P2Y14R expressed in HEK293 cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins by flow cytomtery based competitive fluorescence assayInhibition of MRS4174 binding to mouse P2Y14R expressed in HEK293 cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins by flow cytomtery based competitive fluorescence assay
ChEMBL 516 4 1 1 7.8 C[N+]12CCC(c3ccc(-c4cc(C(=O)O)cc5cc(-c6ccc(C(F)(F)F)cc6)ccc45)cc3)(CC1)CC2 10.1021/acs.jmedchem.0c00745
145946517 174346 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric methodDisplacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric method
ChEMBL 466 5 2 5 4.7 CNC(=O)c1ccc(-c2cc(C(=O)O)cc(-n3cc(-c4ccc(C(F)(F)F)cc4)nn3)c2)cc1 10.1021/acs.jmedchem.8b00168
CHEMBL4204183 174346 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric methodDisplacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric method
ChEMBL 466 5 2 5 4.7 CNC(=O)c1ccc(-c2cc(C(=O)O)cc(-n3cc(-c4ccc(C(F)(F)F)cc4)nn3)c2)cc1 10.1021/acs.jmedchem.8b00168
CHEMBL4300528 174346 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric methodDisplacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric method
ChEMBL 466 5 2 5 4.7 CNC(=O)c1ccc(-c2cc(C(=O)O)cc(-n3cc(-c4ccc(C(F)(F)F)cc4)nn3)c2)cc1 10.1021/acs.jmedchem.8b00168
145947443 174451 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric methodDisplacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric method
ChEMBL 454 5 2 7 3.2 NC(=O)c1cnc(-c2cc(C(=O)O)cc(-n3cc(-c4ccc(C(F)(F)F)cc4)nn3)c2)cn1 10.1021/acs.jmedchem.8b00168
CHEMBL4213423 174451 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric methodDisplacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric method
ChEMBL 454 5 2 7 3.2 NC(=O)c1cnc(-c2cc(C(=O)O)cc(-n3cc(-c4ccc(C(F)(F)F)cc4)nn3)c2)cn1 10.1021/acs.jmedchem.8b00168
CHEMBL4301976 174451 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric methodDisplacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric method
ChEMBL 454 5 2 7 3.2 NC(=O)c1cnc(-c2cc(C(=O)O)cc(-n3cc(-c4ccc(C(F)(F)F)cc4)nn3)c2)cn1 10.1021/acs.jmedchem.8b00168
139392013 184694 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 6.5 by flow cytomtery based competitive fluorescence assayInhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 6.5 by flow cytomtery based competitive fluorescence assay
ChEMBL 501 4 1 2 7.6 O=C(O)c1cc(-c2ccc(C34CCN(CC3)CC4)cc2)c2ccc(-c3ccc(C(F)(F)F)cc3)cc2c1 10.1021/acs.jmedchem.0c00745
CHEMBL4645216 184694 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 6.5 by flow cytomtery based competitive fluorescence assayInhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 6.5 by flow cytomtery based competitive fluorescence assay
ChEMBL 501 4 1 2 7.6 O=C(O)c1cc(-c2ccc(C34CCN(CC3)CC4)cc2)c2ccc(-c3ccc(C(F)(F)F)cc3)cc2c1 10.1021/acs.jmedchem.0c00745
CHEMBL5079653 221410 0 None - 1 Human 7.2 pIC50 = 7.2 Binding
Inhibition of fluorescent antagonist binding to human P2Y14R expressed in CHO cells preincubated for 30 mins followed by 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy 6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate addition and measured after 30 mins by BD FACSCalibur flow cytometry analysisInhibition of fluorescent antagonist binding to human P2Y14R expressed in CHO cells preincubated for 30 mins followed by 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy 6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate addition and measured after 30 mins by BD FACSCalibur flow cytometry analysis
ChEMBL None None None O=C(O)c1cc(-c2ccc([C@H]3C[C@H]4C[C@@H]3NC4=O)cc2)c2ccc(-c3ccc(C(F)(F)F)cc3)cc2c1 10.1021/acs.jmedchem.1c01964
164585567 192758 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysisInhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysis
ChEMBL 509 8 3 6 4.4 NCCCNC(=O)c1ccc(-c2cc(C(=O)O)cc(-n3cc(-c4ccc(C(F)(F)F)cc4)nn3)c2)cc1 10.1021/acs.jmedchem.1c00164
CHEMBL4869802 192758 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysisInhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysis
ChEMBL 509 8 3 6 4.4 NCCCNC(=O)c1ccc(-c2cc(C(=O)O)cc(-n3cc(-c4ccc(C(F)(F)F)cc4)nn3)c2)cc1 10.1021/acs.jmedchem.1c00164
145976578 170456 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric methodDisplacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric method
ChEMBL 637 9 3 9 5.2 CC(C)(C)OC(=O)NCCNS(=O)(=O)c1ccc(-c2cc(C(=O)O)cc(-n3cc(-c4ccc(C(F)(F)F)cc4)nn3)c2)s1 10.1021/acs.jmedchem.8b00168
CHEMBL4204678 170456 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric methodDisplacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric method
ChEMBL 637 9 3 9 5.2 CC(C)(C)OC(=O)NCCNS(=O)(=O)c1ccc(-c2cc(C(=O)O)cc(-n3cc(-c4ccc(C(F)(F)F)cc4)nn3)c2)s1 10.1021/acs.jmedchem.8b00168
42611190 9930 12 None -1 5 Human 8.2 pIC50 = 8.2 Binding
Displacement of 6-Amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy-6-(4-(trifluoromethyl)phenyl)-naphthalen-1-yl)phenyl)piperidin-1-yl)-butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)-phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate from human P2Y14R expressed in CHO cells measured after 15 mins by flow cytometric analysisDisplacement of 6-Amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy-6-(4-(trifluoromethyl)phenyl)-naphthalen-1-yl)phenyl)piperidin-1-yl)-butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)-phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate from human P2Y14R expressed in CHO cells measured after 15 mins by flow cytometric analysis
ChEMBL 475 4 2 2 7.4 OC(=O)c1cc2cc(ccc2c(c1)c1ccc(cc1)C1CCNCC1)c1ccc(cc1)C(F)(F)F 10.1021/acs.jmedchem.6b00044
5802 9930 12 None -1 5 Human 8.2 pIC50 = 8.2 Binding
Displacement of 6-Amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy-6-(4-(trifluoromethyl)phenyl)-naphthalen-1-yl)phenyl)piperidin-1-yl)-butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)-phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate from human P2Y14R expressed in CHO cells measured after 15 mins by flow cytometric analysisDisplacement of 6-Amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy-6-(4-(trifluoromethyl)phenyl)-naphthalen-1-yl)phenyl)piperidin-1-yl)-butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)-phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate from human P2Y14R expressed in CHO cells measured after 15 mins by flow cytometric analysis
ChEMBL 475 4 2 2 7.4 OC(=O)c1cc2cc(ccc2c(c1)c1ccc(cc1)C1CCNCC1)c1ccc(cc1)C(F)(F)F 10.1021/acs.jmedchem.6b00044
CHEMBL1800685 9930 12 None -1 5 Human 8.2 pIC50 = 8.2 Binding
Displacement of 6-Amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy-6-(4-(trifluoromethyl)phenyl)-naphthalen-1-yl)phenyl)piperidin-1-yl)-butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)-phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate from human P2Y14R expressed in CHO cells measured after 15 mins by flow cytometric analysisDisplacement of 6-Amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy-6-(4-(trifluoromethyl)phenyl)-naphthalen-1-yl)phenyl)piperidin-1-yl)-butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)-phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate from human P2Y14R expressed in CHO cells measured after 15 mins by flow cytometric analysis
ChEMBL 475 4 2 2 7.4 OC(=O)c1cc2cc(ccc2c(c1)c1ccc(cc1)C1CCNCC1)c1ccc(cc1)C(F)(F)F 10.1021/acs.jmedchem.6b00044
42611190 9930 12 None -1 5 Human 8.2 pIC50 = 8.2 Binding
Displacement of Alexafluor488 labeled 4-(4-(1-(4-(1-(6-(4-(6-amino-3-imino-4,5-disulfo-3H-xanthen-9-yl)-3-carboxybenzamido)hexyl)-1H-1,2,3-triazol-4-yl)butyl)piperidin-4-yl)phenyl)-7-(4-(trifluoromethyl)phenyl)-2-naphthoic acid from human P2Y14 expressed in CHO cells measured after 30 mins by FACScalibur flow cytometry analysisDisplacement of Alexafluor488 labeled 4-(4-(1-(4-(1-(6-(4-(6-amino-3-imino-4,5-disulfo-3H-xanthen-9-yl)-3-carboxybenzamido)hexyl)-1H-1,2,3-triazol-4-yl)butyl)piperidin-4-yl)phenyl)-7-(4-(trifluoromethyl)phenyl)-2-naphthoic acid from human P2Y14 expressed in CHO cells measured after 30 mins by FACScalibur flow cytometry analysis
ChEMBL 475 4 2 2 7.4 OC(=O)c1cc2cc(ccc2c(c1)c1ccc(cc1)C1CCNCC1)c1ccc(cc1)C(F)(F)F 10.1021/acsmedchemlett.0c00115
5802 9930 12 None -1 5 Human 8.2 pIC50 = 8.2 Binding
Displacement of Alexafluor488 labeled 4-(4-(1-(4-(1-(6-(4-(6-amino-3-imino-4,5-disulfo-3H-xanthen-9-yl)-3-carboxybenzamido)hexyl)-1H-1,2,3-triazol-4-yl)butyl)piperidin-4-yl)phenyl)-7-(4-(trifluoromethyl)phenyl)-2-naphthoic acid from human P2Y14 expressed in CHO cells measured after 30 mins by FACScalibur flow cytometry analysisDisplacement of Alexafluor488 labeled 4-(4-(1-(4-(1-(6-(4-(6-amino-3-imino-4,5-disulfo-3H-xanthen-9-yl)-3-carboxybenzamido)hexyl)-1H-1,2,3-triazol-4-yl)butyl)piperidin-4-yl)phenyl)-7-(4-(trifluoromethyl)phenyl)-2-naphthoic acid from human P2Y14 expressed in CHO cells measured after 30 mins by FACScalibur flow cytometry analysis
ChEMBL 475 4 2 2 7.4 OC(=O)c1cc2cc(ccc2c(c1)c1ccc(cc1)C1CCNCC1)c1ccc(cc1)C(F)(F)F 10.1021/acsmedchemlett.0c00115
CHEMBL1800685 9930 12 None -1 5 Human 8.2 pIC50 = 8.2 Binding
Displacement of Alexafluor488 labeled 4-(4-(1-(4-(1-(6-(4-(6-amino-3-imino-4,5-disulfo-3H-xanthen-9-yl)-3-carboxybenzamido)hexyl)-1H-1,2,3-triazol-4-yl)butyl)piperidin-4-yl)phenyl)-7-(4-(trifluoromethyl)phenyl)-2-naphthoic acid from human P2Y14 expressed in CHO cells measured after 30 mins by FACScalibur flow cytometry analysisDisplacement of Alexafluor488 labeled 4-(4-(1-(4-(1-(6-(4-(6-amino-3-imino-4,5-disulfo-3H-xanthen-9-yl)-3-carboxybenzamido)hexyl)-1H-1,2,3-triazol-4-yl)butyl)piperidin-4-yl)phenyl)-7-(4-(trifluoromethyl)phenyl)-2-naphthoic acid from human P2Y14 expressed in CHO cells measured after 30 mins by FACScalibur flow cytometry analysis
ChEMBL 475 4 2 2 7.4 OC(=O)c1cc2cc(ccc2c(c1)c1ccc(cc1)C1CCNCC1)c1ccc(cc1)C(F)(F)F 10.1021/acsmedchemlett.0c00115
139392279 184542 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7.4 by flow cytomtery based competitive fluorescence assayInhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7.4 by flow cytomtery based competitive fluorescence assay
ChEMBL 428 5 3 3 4.4 NC(=O)c1ccc(-c2cc(C(=O)O)cc(C(=O)Nc3ccc(C(F)(F)F)cc3)c2)cc1 10.1021/acs.jmedchem.0c00745
CHEMBL4642765 184542 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7.4 by flow cytomtery based competitive fluorescence assayInhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7.4 by flow cytomtery based competitive fluorescence assay
ChEMBL 428 5 3 3 4.4 NC(=O)c1ccc(-c2cc(C(=O)O)cc(C(=O)Nc3ccc(C(F)(F)F)cc3)c2)cc1 10.1021/acs.jmedchem.0c00745
164585597 193396 0 None - 0 Human 4.2 pIC50 = 4.2 Binding
Inhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysisInhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysis
ChEMBL 558 7 3 6 5.7 O=P(O)(O)OCc1cc(-c2ccc(C3CCNCC3)cc2)cc(-n2cc(-c3ccc(C(F)(F)F)cc3)nn2)c1 10.1021/acs.jmedchem.1c00164
CHEMBL4879099 193396 0 None - 0 Human 4.2 pIC50 = 4.2 Binding
Inhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysisInhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysis
ChEMBL 558 7 3 6 5.7 O=P(O)(O)OCc1cc(-c2ccc(C3CCNCC3)cc2)cc(-n2cc(-c3ccc(C(F)(F)F)cc3)nn2)c1 10.1021/acs.jmedchem.1c00164
145946659 174329 0 None - 1 Human 6.2 pIC50 = 6.2 Binding
Displacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric methodDisplacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric method
ChEMBL 488 5 2 6 4.0 NS(=O)(=O)c1ccc(-c2cc(C(=O)O)cc(-n3cc(-c4ccc(C(F)(F)F)cc4)nn3)c2)cc1 10.1021/acs.jmedchem.8b00168
CHEMBL4214536 174329 0 None - 1 Human 6.2 pIC50 = 6.2 Binding
Displacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric methodDisplacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric method
ChEMBL 488 5 2 6 4.0 NS(=O)(=O)c1ccc(-c2cc(C(=O)O)cc(-n3cc(-c4ccc(C(F)(F)F)cc4)nn3)c2)cc1 10.1021/acs.jmedchem.8b00168
CHEMBL4300303 174329 0 None - 1 Human 6.2 pIC50 = 6.2 Binding
Displacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric methodDisplacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric method
ChEMBL 488 5 2 6 4.0 NS(=O)(=O)c1ccc(-c2cc(C(=O)O)cc(-n3cc(-c4ccc(C(F)(F)F)cc4)nn3)c2)cc1 10.1021/acs.jmedchem.8b00168
CHEMBL5080028 221439 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibition of fluorescent antagonist binding to human P2Y14R expressed in CHO cells preincubated for 30 mins followed by 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy 6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate addition and measured after 30 mins by BD FACSCalibur flow cytometry analysisInhibition of fluorescent antagonist binding to human P2Y14R expressed in CHO cells preincubated for 30 mins followed by 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy 6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate addition and measured after 30 mins by BD FACSCalibur flow cytometry analysis
ChEMBL None None None O=C(O)c1cc(-c2ccc([C@@H]3CCN[C@@H]4C[C@@H]43)cc2)c2ccc(-c3ccc(C(F)(F)F)cc3)cc2c1 10.1021/acs.jmedchem.1c01964
164585624 192967 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysisInhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysis
ChEMBL 453 5 2 5 5.0 O=C(O)c1ccc(-c2cc(C(=O)O)cc(-n3cc(-c4ccc(C(F)(F)F)cc4)nn3)c2)cc1 10.1021/acs.jmedchem.1c00164
CHEMBL4872737 192967 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysisInhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysis
ChEMBL 453 5 2 5 5.0 O=C(O)c1ccc(-c2cc(C(=O)O)cc(-n3cc(-c4ccc(C(F)(F)F)cc4)nn3)c2)cc1 10.1021/acs.jmedchem.1c00164
139392366 184874 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7.4 by flow cytomtery based competitive fluorescence assayInhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7.4 by flow cytomtery based competitive fluorescence assay
ChEMBL 540 5 2 5 5.8 O=C(O)c1cc(-c2ccc(C34CCNCC3C4(F)F)cc2)cc(-n2cc(-c3ccc(C(F)(F)F)cc3)nn2)c1 10.1021/acs.jmedchem.0c00745
CHEMBL4647874 184874 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7.4 by flow cytomtery based competitive fluorescence assayInhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7.4 by flow cytomtery based competitive fluorescence assay
ChEMBL 540 5 2 5 5.8 O=C(O)c1cc(-c2ccc(C34CCNCC3C4(F)F)cc2)cc(-n2cc(-c3ccc(C(F)(F)F)cc3)nn2)c1 10.1021/acs.jmedchem.0c00745
CHEMBL5075741 221175 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibition of fluorescent antagonist binding to human P2Y14R expressed in CHO cells preincubated for 30 mins followed by 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy 6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate addition and measured after 30 mins by BD FACSCalibur flow cytometry analysisInhibition of fluorescent antagonist binding to human P2Y14R expressed in CHO cells preincubated for 30 mins followed by 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy 6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate addition and measured after 30 mins by BD FACSCalibur flow cytometry analysis
ChEMBL None None None CC(=O)N1C[C@@H]2C[C@H]1C[C@H]2c1ccc(-c2cc(C(=O)O)cc3cc(-c4ccc(C(F)(F)F)cc4)ccc23)cc1 10.1021/acs.jmedchem.1c01964
145947737 174488 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric methodDisplacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric method
ChEMBL 494 5 2 7 4.0 NS(=O)(=O)c1ccc(-c2cc(C(=O)O)cc(-n3cc(-c4ccc(C(F)(F)F)cc4)nn3)c2)s1 10.1021/acs.jmedchem.8b00168
CHEMBL4213485 174488 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric methodDisplacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric method
ChEMBL 494 5 2 7 4.0 NS(=O)(=O)c1ccc(-c2cc(C(=O)O)cc(-n3cc(-c4ccc(C(F)(F)F)cc4)nn3)c2)s1 10.1021/acs.jmedchem.8b00168
CHEMBL4302471 174488 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric methodDisplacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric method
ChEMBL 494 5 2 7 4.0 NS(=O)(=O)c1ccc(-c2cc(C(=O)O)cc(-n3cc(-c4ccc(C(F)(F)F)cc4)nn3)c2)s1 10.1021/acs.jmedchem.8b00168
139406787 183924 0 None - 4 Human 6.2 pIC50 = 6.2 Binding
Displacement of Alexafluor488 labeled 4-(4-(1-(4-(1-(6-(4-(6-amino-3-imino-4,5-disulfo-3H-xanthen-9-yl)-3-carboxybenzamido)hexyl)-1H-1,2,3-triazol-4-yl)butyl)piperidin-4-yl)phenyl)-7-(4-(trifluoromethyl)phenyl)-2-naphthoic acid from human P2Y14 expressed in CHO cells measured after 30 mins by FACScalibur flow cytometry analysisDisplacement of Alexafluor488 labeled 4-(4-(1-(4-(1-(6-(4-(6-amino-3-imino-4,5-disulfo-3H-xanthen-9-yl)-3-carboxybenzamido)hexyl)-1H-1,2,3-triazol-4-yl)butyl)piperidin-4-yl)phenyl)-7-(4-(trifluoromethyl)phenyl)-2-naphthoic acid from human P2Y14 expressed in CHO cells measured after 30 mins by FACScalibur flow cytometry analysis
ChEMBL 492 5 2 5 5.8 O=C(O)c1cc(-c2ccc(C3CCNCC3)cc2)cc(-c2cn(-c3ccc(C(F)(F)F)cc3)nn2)c1 10.1021/acsmedchemlett.0c00115
CHEMBL4633982 183924 0 None - 4 Human 6.2 pIC50 = 6.2 Binding
Displacement of Alexafluor488 labeled 4-(4-(1-(4-(1-(6-(4-(6-amino-3-imino-4,5-disulfo-3H-xanthen-9-yl)-3-carboxybenzamido)hexyl)-1H-1,2,3-triazol-4-yl)butyl)piperidin-4-yl)phenyl)-7-(4-(trifluoromethyl)phenyl)-2-naphthoic acid from human P2Y14 expressed in CHO cells measured after 30 mins by FACScalibur flow cytometry analysisDisplacement of Alexafluor488 labeled 4-(4-(1-(4-(1-(6-(4-(6-amino-3-imino-4,5-disulfo-3H-xanthen-9-yl)-3-carboxybenzamido)hexyl)-1H-1,2,3-triazol-4-yl)butyl)piperidin-4-yl)phenyl)-7-(4-(trifluoromethyl)phenyl)-2-naphthoic acid from human P2Y14 expressed in CHO cells measured after 30 mins by FACScalibur flow cytometry analysis
ChEMBL 492 5 2 5 5.8 O=C(O)c1cc(-c2ccc(C3CCNCC3)cc2)cc(-c2cn(-c3ccc(C(F)(F)F)cc3)nn2)c1 10.1021/acsmedchemlett.0c00115
155540535 179279 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Binding affinity to human P2Y14 expressed in CHO cellsBinding affinity to human P2Y14 expressed in CHO cells
ChEMBL 505 8 6 10 -0.5 O=C(Nc1ccn([C@@H]2O[C@H](COP(=O)(O)CP(=O)(O)O)[C@@H](O)[C@H]2O)c(=O)n1)c1ccccc1 10.1016/j.bmcl.2021.128137
CHEMBL4483379 179279 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Binding affinity to human P2Y14 expressed in CHO cellsBinding affinity to human P2Y14 expressed in CHO cells
ChEMBL 505 8 6 10 -0.5 O=C(Nc1ccn([C@@H]2O[C@H](COP(=O)(O)CP(=O)(O)O)[C@@H](O)[C@H]2O)c(=O)n1)c1ccccc1 10.1016/j.bmcl.2021.128137
CHEMBL4860557 179279 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Binding affinity to human P2Y14 expressed in CHO cellsBinding affinity to human P2Y14 expressed in CHO cells
ChEMBL 505 8 6 10 -0.5 O=C(Nc1ccn([C@@H]2O[C@H](COP(=O)(O)CP(=O)(O)O)[C@@H](O)[C@H]2O)c(=O)n1)c1ccccc1 10.1016/j.bmcl.2021.128137
155540535 179279 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of 6-Amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy-6-(4-(trifluoromethyl)phenyl)-naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)-phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate from recombinant human P2Y14 receptor expressed in CHO cells preincubated for 30 mins followed by tracer addition and measured after 30 mins by flow cytometryDisplacement of 6-Amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy-6-(4-(trifluoromethyl)phenyl)-naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)-phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate from recombinant human P2Y14 receptor expressed in CHO cells preincubated for 30 mins followed by tracer addition and measured after 30 mins by flow cytometry
ChEMBL 505 8 6 10 -0.5 O=C(Nc1ccn([C@@H]2O[C@H](COP(=O)(O)CP(=O)(O)O)[C@@H](O)[C@H]2O)c(=O)n1)c1ccccc1 10.1021/acs.jmedchem.9b00164
CHEMBL4483379 179279 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of 6-Amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy-6-(4-(trifluoromethyl)phenyl)-naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)-phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate from recombinant human P2Y14 receptor expressed in CHO cells preincubated for 30 mins followed by tracer addition and measured after 30 mins by flow cytometryDisplacement of 6-Amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy-6-(4-(trifluoromethyl)phenyl)-naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)-phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate from recombinant human P2Y14 receptor expressed in CHO cells preincubated for 30 mins followed by tracer addition and measured after 30 mins by flow cytometry
ChEMBL 505 8 6 10 -0.5 O=C(Nc1ccn([C@@H]2O[C@H](COP(=O)(O)CP(=O)(O)O)[C@@H](O)[C@H]2O)c(=O)n1)c1ccccc1 10.1021/acs.jmedchem.9b00164
CHEMBL4860557 179279 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of 6-Amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy-6-(4-(trifluoromethyl)phenyl)-naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)-phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate from recombinant human P2Y14 receptor expressed in CHO cells preincubated for 30 mins followed by tracer addition and measured after 30 mins by flow cytometryDisplacement of 6-Amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy-6-(4-(trifluoromethyl)phenyl)-naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)-phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate from recombinant human P2Y14 receptor expressed in CHO cells preincubated for 30 mins followed by tracer addition and measured after 30 mins by flow cytometry
ChEMBL 505 8 6 10 -0.5 O=C(Nc1ccn([C@@H]2O[C@H](COP(=O)(O)CP(=O)(O)O)[C@@H](O)[C@H]2O)c(=O)n1)c1ccccc1 10.1021/acs.jmedchem.9b00164
145977870 170546 0 None - 0 Human 4.2 pIC50 = 4.2 Binding
Displacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric methodDisplacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric method
ChEMBL 613 6 1 8 6.4 CC(C)(C)OC(=O)N1CCN(Cc2ccc(-c3cc(C(=O)O)cc(-n4cc(-c5ccc(C(F)(F)F)cc5)nn4)c3)s2)CC1 10.1021/acs.jmedchem.8b00168
CHEMBL4205655 170546 0 None - 0 Human 4.2 pIC50 = 4.2 Binding
Displacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric methodDisplacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric method
ChEMBL 613 6 1 8 6.4 CC(C)(C)OC(=O)N1CCN(Cc2ccc(-c3cc(C(=O)O)cc(-n4cc(-c5ccc(C(F)(F)F)cc5)nn4)c3)s2)CC1 10.1021/acs.jmedchem.8b00168
CHEMBL5092333 222140 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of fluorescent antagonist binding to human P2Y14R expressed in CHO cells preincubated for 30 mins followed by 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy 6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate addition and measured after 30 mins by BD FACSCalibur flow cytometry analysisInhibition of fluorescent antagonist binding to human P2Y14R expressed in CHO cells preincubated for 30 mins followed by 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy 6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate addition and measured after 30 mins by BD FACSCalibur flow cytometry analysis
ChEMBL None None None O=C(O)c1cc(-c2ccc(C3[C@H]4CC[C@H]3CNC4)cc2)c2ccc(-c3ccc(C(F)(F)F)cc3)cc2c1 10.1021/acs.jmedchem.1c01964
42611190 9930 12 None -1 5 Human 8.1 pIC50 = 8.1 Binding
Displacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric methodDisplacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric method
ChEMBL 475 4 2 2 7.4 OC(=O)c1cc2cc(ccc2c(c1)c1ccc(cc1)C1CCNCC1)c1ccc(cc1)C(F)(F)F 10.1021/acs.jmedchem.8b00168
5802 9930 12 None -1 5 Human 8.1 pIC50 = 8.1 Binding
Displacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric methodDisplacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric method
ChEMBL 475 4 2 2 7.4 OC(=O)c1cc2cc(ccc2c(c1)c1ccc(cc1)C1CCNCC1)c1ccc(cc1)C(F)(F)F 10.1021/acs.jmedchem.8b00168
CHEMBL1800685 9930 12 None -1 5 Human 8.1 pIC50 = 8.1 Binding
Displacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric methodDisplacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric method
ChEMBL 475 4 2 2 7.4 OC(=O)c1cc2cc(ccc2c(c1)c1ccc(cc1)C1CCNCC1)c1ccc(cc1)C(F)(F)F 10.1021/acs.jmedchem.8b00168
135356919 176695 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of 6-Amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy-6-(4-(trifluoromethyl)phenyl)-naphthalen-1-yl)phenyl)piperidin-1-yl)-butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)-phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate from human P2Y14R expressed in CHO cells measured after 15 mins by flow cytometric analysisDisplacement of 6-Amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy-6-(4-(trifluoromethyl)phenyl)-naphthalen-1-yl)phenyl)piperidin-1-yl)-butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)-phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate from human P2Y14R expressed in CHO cells measured after 15 mins by flow cytometric analysis
ChEMBL 466 7 2 5 5.7 CCCc1ccc(-c2cn(-c3cc(C(=O)O)cc(-c4ccc(C5CCNCC5)cc4)c3)nn2)cc1 10.1021/acs.jmedchem.6b00044
CHEMBL4441075 176695 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of 6-Amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy-6-(4-(trifluoromethyl)phenyl)-naphthalen-1-yl)phenyl)piperidin-1-yl)-butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)-phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate from human P2Y14R expressed in CHO cells measured after 15 mins by flow cytometric analysisDisplacement of 6-Amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy-6-(4-(trifluoromethyl)phenyl)-naphthalen-1-yl)phenyl)piperidin-1-yl)-butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)-phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate from human P2Y14R expressed in CHO cells measured after 15 mins by flow cytometric analysis
ChEMBL 466 7 2 5 5.7 CCCc1ccc(-c2cn(-c3cc(C(=O)O)cc(-c4ccc(C5CCNCC5)cc4)c3)nn2)cc1 10.1021/acs.jmedchem.6b00044
145977176 170673 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric methodDisplacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric method
ChEMBL 515 8 3 7 4.5 NCCCNC(=O)c1csc(-c2cc(C(=O)O)cc(-n3cc(-c4ccc(C(F)(F)F)cc4)nn3)c2)c1 10.1021/acs.jmedchem.8b00168
CHEMBL4207098 170673 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric methodDisplacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric method
ChEMBL 515 8 3 7 4.5 NCCCNC(=O)c1csc(-c2cc(C(=O)O)cc(-n3cc(-c4ccc(C(F)(F)F)cc4)nn3)c2)c1 10.1021/acs.jmedchem.8b00168
164585431 191787 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysisInhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysis
ChEMBL 482 6 3 5 5.5 O=C(O)c1cc(NC(=O)c2ccc(C(F)(F)F)cc2)cc(-c2ccc(-c3cc(CO)on3)cc2)c1 10.1021/acs.jmedchem.1c00164
CHEMBL4854794 191787 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysisInhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysis
ChEMBL 482 6 3 5 5.5 O=C(O)c1cc(NC(=O)c2ccc(C(F)(F)F)cc2)cc(-c2ccc(-c3cc(CO)on3)cc2)c1 10.1021/acs.jmedchem.1c00164
145946492 174319 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric methodDisplacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric method
ChEMBL 508 5 2 5 5.8 CC(C)(C)NC(=O)c1ccc(-c2cc(C(=O)O)cc(-n3cc(-c4ccc(C(F)(F)F)cc4)nn3)c2)cc1 10.1021/acs.jmedchem.8b00168
CHEMBL4207890 174319 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric methodDisplacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric method
ChEMBL 508 5 2 5 5.8 CC(C)(C)NC(=O)c1ccc(-c2cc(C(=O)O)cc(-n3cc(-c4ccc(C(F)(F)F)cc4)nn3)c2)cc1 10.1021/acs.jmedchem.8b00168
CHEMBL4300224 174319 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric methodDisplacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric method
ChEMBL 508 5 2 5 5.8 CC(C)(C)NC(=O)c1ccc(-c2cc(C(=O)O)cc(-n3cc(-c4ccc(C(F)(F)F)cc4)nn3)c2)cc1 10.1021/acs.jmedchem.8b00168
145965286 171069 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric methodDisplacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric method
ChEMBL 551 9 3 8 4.0 NCCCNS(=O)(=O)c1ccc(-c2cc(C(=O)O)cc(-n3cc(-c4ccc(C(F)(F)F)cc4)nn3)c2)s1 10.1021/acs.jmedchem.8b00168
CHEMBL4211995 171069 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric methodDisplacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric method
ChEMBL 551 9 3 8 4.0 NCCCNS(=O)(=O)c1ccc(-c2cc(C(=O)O)cc(-n3cc(-c4ccc(C(F)(F)F)cc4)nn3)c2)s1 10.1021/acs.jmedchem.8b00168
139392057 171110 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of Alexafluor488 labeled 4-(4-(1-(4-(1-(6-(4-(6-amino-3-imino-4,5-disulfo-3H-xanthen-9-yl)-3-carboxybenzamido)hexyl)-1H-1,2,3-triazol-4-yl)butyl)piperidin-4-yl)phenyl)-7-(4-(trifluoromethyl)phenyl)-2-naphthoic acid from human P2Y14 expressed in CHO cells measured after 30 mins by FACScalibur flow cytometry analysisDisplacement of Alexafluor488 labeled 4-(4-(1-(4-(1-(6-(4-(6-amino-3-imino-4,5-disulfo-3H-xanthen-9-yl)-3-carboxybenzamido)hexyl)-1H-1,2,3-triazol-4-yl)butyl)piperidin-4-yl)phenyl)-7-(4-(trifluoromethyl)phenyl)-2-naphthoic acid from human P2Y14 expressed in CHO cells measured after 30 mins by FACScalibur flow cytometry analysis
ChEMBL 555 8 1 2 8.9 C#CCCCCN1CCC(c2ccc(-c3cc(C(=O)O)cc4cc(-c5ccc(C(F)(F)F)cc5)ccc34)cc2)CC1 10.1021/acsmedchemlett.0c00115
CHEMBL4212441 171110 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of Alexafluor488 labeled 4-(4-(1-(4-(1-(6-(4-(6-amino-3-imino-4,5-disulfo-3H-xanthen-9-yl)-3-carboxybenzamido)hexyl)-1H-1,2,3-triazol-4-yl)butyl)piperidin-4-yl)phenyl)-7-(4-(trifluoromethyl)phenyl)-2-naphthoic acid from human P2Y14 expressed in CHO cells measured after 30 mins by FACScalibur flow cytometry analysisDisplacement of Alexafluor488 labeled 4-(4-(1-(4-(1-(6-(4-(6-amino-3-imino-4,5-disulfo-3H-xanthen-9-yl)-3-carboxybenzamido)hexyl)-1H-1,2,3-triazol-4-yl)butyl)piperidin-4-yl)phenyl)-7-(4-(trifluoromethyl)phenyl)-2-naphthoic acid from human P2Y14 expressed in CHO cells measured after 30 mins by FACScalibur flow cytometry analysis
ChEMBL 555 8 1 2 8.9 C#CCCCCN1CCC(c2ccc(-c3cc(C(=O)O)cc4cc(-c5ccc(C(F)(F)F)cc5)ccc34)cc2)CC1 10.1021/acsmedchemlett.0c00115
139392057 171110 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7.4 by flow cytomtery based competitive fluorescence assayInhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7.4 by flow cytomtery based competitive fluorescence assay
ChEMBL 555 8 1 2 8.9 C#CCCCCN1CCC(c2ccc(-c3cc(C(=O)O)cc4cc(-c5ccc(C(F)(F)F)cc5)ccc34)cc2)CC1 10.1021/acs.jmedchem.0c00745
CHEMBL4212441 171110 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7.4 by flow cytomtery based competitive fluorescence assayInhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7.4 by flow cytomtery based competitive fluorescence assay
ChEMBL 555 8 1 2 8.9 C#CCCCCN1CCC(c2ccc(-c3cc(C(=O)O)cc4cc(-c5ccc(C(F)(F)F)cc5)ccc34)cc2)CC1 10.1021/acs.jmedchem.0c00745
139392057 171110 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric methodDisplacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric method
ChEMBL 555 8 1 2 8.9 C#CCCCCN1CCC(c2ccc(-c3cc(C(=O)O)cc4cc(-c5ccc(C(F)(F)F)cc5)ccc34)cc2)CC1 10.1021/acs.jmedchem.8b00168
CHEMBL4212441 171110 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric methodDisplacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric method
ChEMBL 555 8 1 2 8.9 C#CCCCCN1CCC(c2ccc(-c3cc(C(=O)O)cc4cc(-c5ccc(C(F)(F)F)cc5)ccc34)cc2)CC1 10.1021/acs.jmedchem.8b00168
42611190 9930 12 None -1 5 Human 8.1 pIC50 = 8.1 Binding
Inhibition of fluorescent antagonist binding to human P2Y14 expressed in CHO cells incubated for 30 minsInhibition of fluorescent antagonist binding to human P2Y14 expressed in CHO cells incubated for 30 mins
ChEMBL 475 4 2 2 7.4 OC(=O)c1cc2cc(ccc2c(c1)c1ccc(cc1)C1CCNCC1)c1ccc(cc1)C(F)(F)F 10.1021/acs.jmedchem.1c01964
5802 9930 12 None -1 5 Human 8.1 pIC50 = 8.1 Binding
Inhibition of fluorescent antagonist binding to human P2Y14 expressed in CHO cells incubated for 30 minsInhibition of fluorescent antagonist binding to human P2Y14 expressed in CHO cells incubated for 30 mins
ChEMBL 475 4 2 2 7.4 OC(=O)c1cc2cc(ccc2c(c1)c1ccc(cc1)C1CCNCC1)c1ccc(cc1)C(F)(F)F 10.1021/acs.jmedchem.1c01964
CHEMBL1800685 9930 12 None -1 5 Human 8.1 pIC50 = 8.1 Binding
Inhibition of fluorescent antagonist binding to human P2Y14 expressed in CHO cells incubated for 30 minsInhibition of fluorescent antagonist binding to human P2Y14 expressed in CHO cells incubated for 30 mins
ChEMBL 475 4 2 2 7.4 OC(=O)c1cc2cc(ccc2c(c1)c1ccc(cc1)C1CCNCC1)c1ccc(cc1)C(F)(F)F 10.1021/acs.jmedchem.1c01964
CHEMBL5074765 221111 0 None - 2 Human 8.1 pIC50 = 8.1 Binding
Inhibition of fluorescent antagonist binding to human P2Y14R expressed in CHO cells preincubated for 30 mins followed by 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy 6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate addition and measured after 30 mins by BD FACSCalibur flow cytometry analysisInhibition of fluorescent antagonist binding to human P2Y14R expressed in CHO cells preincubated for 30 mins followed by 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy 6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate addition and measured after 30 mins by BD FACSCalibur flow cytometry analysis
ChEMBL None None None O=C(O)c1cc(-c2ccc([C@@H]3C[C@@H]4C[C@H]3CN4)cc2)c2ccc(-c3ccc(C(F)(F)F)cc3)cc2c1 10.1021/acs.jmedchem.1c01964
164585400 191680 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysisInhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysis
ChEMBL 466 5 2 5 5.3 CC(=O)Nc1ccc(-c2cc(C(=O)O)cc(-n3cc(-c4ccc(C(F)(F)F)cc4)nn3)c2)cc1 10.1021/acs.jmedchem.1c00164
CHEMBL4853085 191680 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysisInhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysis
ChEMBL 466 5 2 5 5.3 CC(=O)Nc1ccc(-c2cc(C(=O)O)cc(-n3cc(-c4ccc(C(F)(F)F)cc4)nn3)c2)cc1 10.1021/acs.jmedchem.1c00164
145969418 171628 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric methodDisplacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric method
ChEMBL 739 16 2 6 9.4 CC(=O)NCCCCCCn1cc(CCCCN2CCC(c3ccc(-c4cc(C(=O)O)cc5cc(-c6ccc(C(F)(F)F)cc6)ccc45)cc3)CC2)nn1 10.1021/acs.jmedchem.8b00168
CHEMBL4218967 171628 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric methodDisplacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric method
ChEMBL 739 16 2 6 9.4 CC(=O)NCCCCCCn1cc(CCCCN2CCC(c3ccc(-c4cc(C(=O)O)cc5cc(-c6ccc(C(F)(F)F)cc6)ccc45)cc3)CC2)nn1 10.1021/acs.jmedchem.8b00168
139392013 184694 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 6 by flow cytomtery based competitive fluorescence assayInhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 6 by flow cytomtery based competitive fluorescence assay
ChEMBL 501 4 1 2 7.6 O=C(O)c1cc(-c2ccc(C34CCN(CC3)CC4)cc2)c2ccc(-c3ccc(C(F)(F)F)cc3)cc2c1 10.1021/acs.jmedchem.0c00745
CHEMBL4645216 184694 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 6 by flow cytomtery based competitive fluorescence assayInhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 6 by flow cytomtery based competitive fluorescence assay
ChEMBL 501 4 1 2 7.6 O=C(O)c1cc(-c2ccc(C34CCN(CC3)CC4)cc2)c2ccc(-c3ccc(C(F)(F)F)cc3)cc2c1 10.1021/acs.jmedchem.0c00745
145964225 171236 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric methodDisplacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric method
ChEMBL 566 10 3 8 4.4 O=C(O)c1cc(-c2ccc(S(=O)(=O)NCCCCO)s2)cc(-n2cc(-c3ccc(C(F)(F)F)cc3)nn2)c1 10.1021/acs.jmedchem.8b00168
CHEMBL4214011 171236 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric methodDisplacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric method
ChEMBL 566 10 3 8 4.4 O=C(O)c1cc(-c2ccc(S(=O)(=O)NCCCCO)s2)cc(-n2cc(-c3ccc(C(F)(F)F)cc3)nn2)c1 10.1021/acs.jmedchem.8b00168
156019395 184788 0 None - 0 Mouse 6.1 pIC50 = 6.1 Binding
Inhibition of MRS4174 binding to mouse P2Y14R expressed in HEK293 cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins by flow cytomtery based competitive fluorescence assayInhibition of MRS4174 binding to mouse P2Y14R expressed in HEK293 cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins by flow cytomtery based competitive fluorescence assay
ChEMBL 518 5 1 5 6.1 O=C(O)c1cc(-c2ccc(C34CCN(CC3)CC4)cc2)cc(-n2cc(-c3ccc(C(F)(F)F)cc3)nn2)c1 10.1021/acs.jmedchem.0c00745
CHEMBL4646514 184788 0 None - 0 Mouse 6.1 pIC50 = 6.1 Binding
Inhibition of MRS4174 binding to mouse P2Y14R expressed in HEK293 cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins by flow cytomtery based competitive fluorescence assayInhibition of MRS4174 binding to mouse P2Y14R expressed in HEK293 cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins by flow cytomtery based competitive fluorescence assay
ChEMBL 518 5 1 5 6.1 O=C(O)c1cc(-c2ccc(C34CCN(CC3)CC4)cc2)cc(-n2cc(-c3ccc(C(F)(F)F)cc3)nn2)c1 10.1021/acs.jmedchem.0c00745
CHEMBL5084659 221708 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of fluorescent antagonist binding to human P2Y14R expressed in CHO cells preincubated for 30 mins followed by 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy 6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate addition and measured after 30 mins by BD FACSCalibur flow cytometry analysisInhibition of fluorescent antagonist binding to human P2Y14R expressed in CHO cells preincubated for 30 mins followed by 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy 6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate addition and measured after 30 mins by BD FACSCalibur flow cytometry analysis
ChEMBL None None None O=C(O)c1cc(-c2cc(C34CCN(CC3)CC4)ccc2Br)c2ccc(-c3ccc(C(F)(F)F)cc3)cc2c1 10.1021/acs.jmedchem.1c01964
164585395 191649 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysisInhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysis
ChEMBL 478 6 2 5 5.3 NCC1(c2ccc(-c3cc(C(=O)O)cc(-n4cc(-c5ccc(C(F)(F)F)cc5)nn4)c3)cc2)CC1 10.1021/acs.jmedchem.1c00164
CHEMBL4852625 191649 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysisInhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysis
ChEMBL 478 6 2 5 5.3 NCC1(c2ccc(-c3cc(C(=O)O)cc(-n4cc(-c5ccc(C(F)(F)F)cc5)nn4)c3)cc2)CC1 10.1021/acs.jmedchem.1c00164
164585522 193307 0 None - 1 Human 6.1 pIC50 = 6.1 Binding
Inhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysisInhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysis
ChEMBL 477 5 2 7 4.5 O=C(O)c1cc(-c2ccc(-c3nnn[nH]3)cc2)cc(-n2cc(-c3ccc(C(F)(F)F)cc3)nn2)c1 10.1021/acs.jmedchem.1c00164
CHEMBL4877701 193307 0 None - 1 Human 6.1 pIC50 = 6.1 Binding
Inhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysisInhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysis
ChEMBL 477 5 2 7 4.5 O=C(O)c1cc(-c2ccc(-c3nnn[nH]3)cc2)cc(-n2cc(-c3ccc(C(F)(F)F)cc3)nn2)c1 10.1021/acs.jmedchem.1c00164
145946302 174286 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric methodDisplacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric method
ChEMBL 480 6 2 5 5.1 CCNC(=O)c1ccc(-c2cc(C(=O)O)cc(-n3cc(-c4ccc(C(F)(F)F)cc4)nn3)c2)cc1 10.1021/acs.jmedchem.8b00168
CHEMBL4212481 174286 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric methodDisplacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric method
ChEMBL 480 6 2 5 5.1 CCNC(=O)c1ccc(-c2cc(C(=O)O)cc(-n3cc(-c4ccc(C(F)(F)F)cc4)nn3)c2)cc1 10.1021/acs.jmedchem.8b00168
CHEMBL4299824 174286 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric methodDisplacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric method
ChEMBL 480 6 2 5 5.1 CCNC(=O)c1ccc(-c2cc(C(=O)O)cc(-n3cc(-c4ccc(C(F)(F)F)cc4)nn3)c2)cc1 10.1021/acs.jmedchem.8b00168
42611190 9930 12 None -1 5 Human 8.0 pIC50 = 8.0 Binding
Inhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7 by flow cytomtery based competitive fluorescence assayInhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7 by flow cytomtery based competitive fluorescence assay
ChEMBL 475 4 2 2 7.4 OC(=O)c1cc2cc(ccc2c(c1)c1ccc(cc1)C1CCNCC1)c1ccc(cc1)C(F)(F)F 10.1021/acs.jmedchem.0c00745
5802 9930 12 None -1 5 Human 8.0 pIC50 = 8.0 Binding
Inhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7 by flow cytomtery based competitive fluorescence assayInhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7 by flow cytomtery based competitive fluorescence assay
ChEMBL 475 4 2 2 7.4 OC(=O)c1cc2cc(ccc2c(c1)c1ccc(cc1)C1CCNCC1)c1ccc(cc1)C(F)(F)F 10.1021/acs.jmedchem.0c00745
CHEMBL1800685 9930 12 None -1 5 Human 8.0 pIC50 = 8.0 Binding
Inhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7 by flow cytomtery based competitive fluorescence assayInhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7 by flow cytomtery based competitive fluorescence assay
ChEMBL 475 4 2 2 7.4 OC(=O)c1cc2cc(ccc2c(c1)c1ccc(cc1)C1CCNCC1)c1ccc(cc1)C(F)(F)F 10.1021/acs.jmedchem.0c00745
CHEMBL5087295 221861 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Inhibition of fluorescent antagonist binding to human P2Y14R expressed in CHO cells preincubated for 30 mins followed by 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy 6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate addition and measured after 30 mins by BD FACSCalibur flow cytometry analysisInhibition of fluorescent antagonist binding to human P2Y14R expressed in CHO cells preincubated for 30 mins followed by 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy 6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate addition and measured after 30 mins by BD FACSCalibur flow cytometry analysis
ChEMBL None None None O=C(O)c1cc(-c2ccc([C@@H]3C[C@H]4CN[C@@H]3C4)cc2)c2ccc(-c3ccc(C(F)(F)F)cc3)cc2c1 10.1021/acs.jmedchem.1c01964
CHEMBL5087295 221861 0 None - 0 Mouse 7.0 pIC50 = 7.0 Binding
Inhibition of fluorescent antagonist binding to mouse P2Y14R expressed in HEK293 cells preincubated for 30 mins followed by addition of 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy-6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate incubated for 30 mins by BD FACSCalibur flow cytometry analysisInhibition of fluorescent antagonist binding to mouse P2Y14R expressed in HEK293 cells preincubated for 30 mins followed by addition of 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy-6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate incubated for 30 mins by BD FACSCalibur flow cytometry analysis
ChEMBL None None None O=C(O)c1cc(-c2ccc([C@@H]3C[C@H]4CN[C@@H]3C4)cc2)c2ccc(-c3ccc(C(F)(F)F)cc3)cc2c1 10.1021/acs.jmedchem.1c01964
134611896 9448 4 None - 1 Mouse 6.0 pIC50 = 6.0 Binding
Inhibition of MRS4174 binding to mouse P2Y14R expressed in HEK293 cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins by flow cytomtery based competitive fluorescence assayInhibition of MRS4174 binding to mouse P2Y14R expressed in HEK293 cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins by flow cytomtery based competitive fluorescence assay
ChEMBL 452 5 2 5 4.4 OC(=O)c1cc(cc(c1)n1nnc(c1)c1ccc(cc1)C(F)(F)F)c1ccc(cc1)C(=O)N 10.1021/acs.jmedchem.0c00745
9999 9448 4 None - 1 Mouse 6.0 pIC50 = 6.0 Binding
Inhibition of MRS4174 binding to mouse P2Y14R expressed in HEK293 cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins by flow cytomtery based competitive fluorescence assayInhibition of MRS4174 binding to mouse P2Y14R expressed in HEK293 cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins by flow cytomtery based competitive fluorescence assay
ChEMBL 452 5 2 5 4.4 OC(=O)c1cc(cc(c1)n1nnc(c1)c1ccc(cc1)C(F)(F)F)c1ccc(cc1)C(=O)N 10.1021/acs.jmedchem.0c00745
CHEMBL4299805 9448 4 None - 1 Mouse 6.0 pIC50 = 6.0 Binding
Inhibition of MRS4174 binding to mouse P2Y14R expressed in HEK293 cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins by flow cytomtery based competitive fluorescence assayInhibition of MRS4174 binding to mouse P2Y14R expressed in HEK293 cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins by flow cytomtery based competitive fluorescence assay
ChEMBL 452 5 2 5 4.4 OC(=O)c1cc(cc(c1)n1nnc(c1)c1ccc(cc1)C(F)(F)F)c1ccc(cc1)C(=O)N 10.1021/acs.jmedchem.0c00745
135357364 178879 1 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of 6-Amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy-6-(4-(trifluoromethyl)phenyl)-naphthalen-1-yl)phenyl)piperidin-1-yl)-butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)-phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate from human P2Y14R expressed in CHO cells measured after 15 mins by flow cytometric analysisDisplacement of 6-Amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy-6-(4-(trifluoromethyl)phenyl)-naphthalen-1-yl)phenyl)piperidin-1-yl)-butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)-phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate from human P2Y14R expressed in CHO cells measured after 15 mins by flow cytometric analysis
ChEMBL 508 5 2 6 5.6 O=C(O)c1cc(-c2ccc(C3CCNCC3)cc2)cc(-n2cc(-c3ccc(Br)s3)nn2)c1 10.1021/acs.jmedchem.6b00044
CHEMBL4472517 178879 1 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of 6-Amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy-6-(4-(trifluoromethyl)phenyl)-naphthalen-1-yl)phenyl)piperidin-1-yl)-butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)-phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate from human P2Y14R expressed in CHO cells measured after 15 mins by flow cytometric analysisDisplacement of 6-Amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy-6-(4-(trifluoromethyl)phenyl)-naphthalen-1-yl)phenyl)piperidin-1-yl)-butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)-phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate from human P2Y14R expressed in CHO cells measured after 15 mins by flow cytometric analysis
ChEMBL 508 5 2 6 5.6 O=C(O)c1cc(-c2ccc(C3CCNCC3)cc2)cc(-n2cc(-c3ccc(Br)s3)nn2)c1 10.1021/acs.jmedchem.6b00044
164585365 193267 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Inhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysisInhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysis
ChEMBL 481 8 2 5 5.6 O=C(O)c1cc(-c2ccc(CCCCO)cc2)cc(-n2cc(-c3ccc(C(F)(F)F)cc3)nn2)c1 10.1021/acs.jmedchem.1c00164
CHEMBL4877136 193267 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Inhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysisInhibition of fluorescent antagonist binding to human P2Y14 receptor expressed in CHO cells preincubated with compound for 30 mins followed by fluorescent antagonist addition and measured after 30 mins by flow cytometry analysis
ChEMBL 481 8 2 5 5.6 O=C(O)c1cc(-c2ccc(CCCCO)cc2)cc(-n2cc(-c3ccc(C(F)(F)F)cc3)nn2)c1 10.1021/acs.jmedchem.1c00164
145971306 171256 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Displacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric methodDisplacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric method
ChEMBL 651 10 3 9 5.6 CC(C)(C)OC(=O)NCCCNS(=O)(=O)c1ccc(-c2cc(C(=O)O)cc(-n3cc(-c4ccc(C(F)(F)F)cc4)nn3)c2)s1 10.1021/acs.jmedchem.8b00168
CHEMBL4214191 171256 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Displacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric methodDisplacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric method
ChEMBL 651 10 3 9 5.6 CC(C)(C)OC(=O)NCCCNS(=O)(=O)c1ccc(-c2cc(C(=O)O)cc(-n3cc(-c4ccc(C(F)(F)F)cc4)nn3)c2)s1 10.1021/acs.jmedchem.8b00168
145977897 170629 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric methodDisplacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric method
ChEMBL 516 5 2 7 5.3 FC(F)(F)c1ccc(-c2cn(-c3cc(-c4ccc(C5CCNCC5)cc4)cc(-c4nnn[nH]4)c3)nn2)cc1 10.1021/acs.jmedchem.8b00168
CHEMBL4206519 170629 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric methodDisplacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric method
ChEMBL 516 5 2 7 5.3 FC(F)(F)c1ccc(-c2cn(-c3cc(-c4ccc(C5CCNCC5)cc4)cc(-c4nnn[nH]4)c3)nn2)cc1 10.1021/acs.jmedchem.8b00168
156020230 184953 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7.4 by flow cytomtery based competitive fluorescence assayInhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7.4 by flow cytomtery based competitive fluorescence assay
ChEMBL 854 27 2 10 7.1 NCCOCCOCCOCCOCCOCCOCCOCCC(=O)N1CCC(c2ccc(-c3cc(C(=O)O)cc4cc(-c5ccc(C(F)(F)F)cc5)ccc34)cc2)CC1 10.1021/acs.jmedchem.0c00745
CHEMBL4649194 184953 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7.4 by flow cytomtery based competitive fluorescence assayInhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7.4 by flow cytomtery based competitive fluorescence assay
ChEMBL 854 27 2 10 7.1 NCCOCCOCCOCCOCCOCCOCCOCCC(=O)N1CCC(c2ccc(-c3cc(C(=O)O)cc4cc(-c5ccc(C(F)(F)F)cc5)ccc34)cc2)CC1 10.1021/acs.jmedchem.0c00745
156011024 183911 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7.4 by flow cytomtery based competitive fluorescence assayInhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7.4 by flow cytomtery based competitive fluorescence assay
ChEMBL 896 28 2 10 7.2 CC(=O)NCCOCCOCCOCCOCCOCCOCCOCCC(=O)N1CCC(c2ccc(-c3cc(C(=O)O)cc4cc(-c5ccc(C(F)(F)F)cc5)ccc34)cc2)CC1 10.1021/acs.jmedchem.0c00745
CHEMBL4633795 183911 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7.4 by flow cytomtery based competitive fluorescence assayInhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7.4 by flow cytomtery based competitive fluorescence assay
ChEMBL 896 28 2 10 7.2 CC(=O)NCCOCCOCCOCCOCCOCCOCCOCCC(=O)N1CCC(c2ccc(-c3cc(C(=O)O)cc4cc(-c5ccc(C(F)(F)F)cc5)ccc34)cc2)CC1 10.1021/acs.jmedchem.0c00745
CHEMBL5093465 222208 0 None - 0 Human 7.0 pIC50 = 7 Binding
Inhibition of fluorescent antagonist binding to human P2Y14R expressed in CHO cells preincubated for 30 mins followed by 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy 6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate addition and measured after 30 mins by BD FACSCalibur flow cytometry analysisInhibition of fluorescent antagonist binding to human P2Y14R expressed in CHO cells preincubated for 30 mins followed by 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy 6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate addition and measured after 30 mins by BD FACSCalibur flow cytometry analysis
ChEMBL None None None CC(=O)N1C[C@H]2C[C@@H]1C[C@@H]2c1ccc(-c2cc(C(=O)O)cc3cc(-c4ccc(C(F)(F)F)cc4)ccc23)cc1 10.1021/acs.jmedchem.1c01964
CHEMBL5271821 200479 0 None - 1 Human 10.1 pKi = 10.1 Binding
Antagonist activity at human P2Y14 expressed in CHO cells assessed as inhibition constantAntagonist activity at human P2Y14 expressed in CHO cells assessed as inhibition constant
ChEMBL 1211 21 6 14 12.0 CC(=O)c1cc(C(=O)NCCCCCCn2cc(CCCCN3CCC(c4ccc(-c5cc(C(=O)O)cc6cc(-c7ccc(C(F)(F)F)cc7)ccc56)cc4)CC3)nn2)ccc1-c1c2ccc(=N)c(S(=O)(=O)O)c-2oc2c(S(=O)(=O)O)c(N)ccc12 10.1021/acs.jmedchem.5b01972
124221650 9445 0 None - 1 Human 10.1 pKi = 10.1 Binding
Inhibition of human P2Y14 receptor expressed in CHO cells by fluorescence assayInhibition of human P2Y14 receptor expressed in CHO cells by fluorescence assay
ChEMBL 1213 21 6 14 9.3 O=C(c1ccc(c(c1)C(=O)O)c1c2ccc(c(c2oc2c1ccc(=[NH2+])c2S(=O)(=O)[O-])S(=O)(=O)O)N)NCCCCCCn1nnc(c1)CCCCN1CCC(CC1)c1ccc(cc1)c1cc(cc2c1ccc(c2)c1ccc(cc1)C(F)(F)F)C(=O)O 10.1016/j.ejmech.2019.04.068
124221651 9445 0 None - 1 Human 10.1 pKi = 10.1 Binding
Inhibition of human P2Y14 receptor expressed in CHO cells by fluorescence assayInhibition of human P2Y14 receptor expressed in CHO cells by fluorescence assay
ChEMBL 1213 21 6 14 9.3 O=C(c1ccc(c(c1)C(=O)O)c1c2ccc(c(c2oc2c1ccc(=[NH2+])c2S(=O)(=O)[O-])S(=O)(=O)O)N)NCCCCCCn1nnc(c1)CCCCN1CCC(CC1)c1ccc(cc1)c1cc(cc2c1ccc(c2)c1ccc(cc1)C(F)(F)F)C(=O)O 10.1016/j.ejmech.2019.04.068
9470 9445 0 None - 1 Human 10.1 pKi = 10.1 Binding
Inhibition of human P2Y14 receptor expressed in CHO cells by fluorescence assayInhibition of human P2Y14 receptor expressed in CHO cells by fluorescence assay
ChEMBL 1213 21 6 14 9.3 O=C(c1ccc(c(c1)C(=O)O)c1c2ccc(c(c2oc2c1ccc(=[NH2+])c2S(=O)(=O)[O-])S(=O)(=O)O)N)NCCCCCCn1nnc(c1)CCCCN1CCC(CC1)c1ccc(cc1)c1cc(cc2c1ccc(c2)c1ccc(cc1)C(F)(F)F)C(=O)O 10.1016/j.ejmech.2019.04.068
CHEMBL4447162 9445 0 None - 1 Human 10.1 pKi = 10.1 Binding
Inhibition of human P2Y14 receptor expressed in CHO cells by fluorescence assayInhibition of human P2Y14 receptor expressed in CHO cells by fluorescence assay
ChEMBL 1213 21 6 14 9.3 O=C(c1ccc(c(c1)C(=O)O)c1c2ccc(c(c2oc2c1ccc(=[NH2+])c2S(=O)(=O)[O-])S(=O)(=O)O)N)NCCCCCCn1nnc(c1)CCCCN1CCC(CC1)c1ccc(cc1)c1cc(cc2c1ccc(c2)c1ccc(cc1)C(F)(F)F)C(=O)O 10.1016/j.ejmech.2019.04.068
124221650 9445 0 None - 1 Human 10.1 pKi = 10.1 Binding
Inhibition of human P2Y14RInhibition of human P2Y14R
ChEMBL 1213 21 6 14 9.3 O=C(c1ccc(c(c1)C(=O)O)c1c2ccc(c(c2oc2c1ccc(=[NH2+])c2S(=O)(=O)[O-])S(=O)(=O)O)N)NCCCCCCn1nnc(c1)CCCCN1CCC(CC1)c1ccc(cc1)c1cc(cc2c1ccc(c2)c1ccc(cc1)C(F)(F)F)C(=O)O 10.1021/acs.jmedchem.0c00745
124221651 9445 0 None - 1 Human 10.1 pKi = 10.1 Binding
Inhibition of human P2Y14RInhibition of human P2Y14R
ChEMBL 1213 21 6 14 9.3 O=C(c1ccc(c(c1)C(=O)O)c1c2ccc(c(c2oc2c1ccc(=[NH2+])c2S(=O)(=O)[O-])S(=O)(=O)O)N)NCCCCCCn1nnc(c1)CCCCN1CCC(CC1)c1ccc(cc1)c1cc(cc2c1ccc(c2)c1ccc(cc1)C(F)(F)F)C(=O)O 10.1021/acs.jmedchem.0c00745
9470 9445 0 None - 1 Human 10.1 pKi = 10.1 Binding
Inhibition of human P2Y14RInhibition of human P2Y14R
ChEMBL 1213 21 6 14 9.3 O=C(c1ccc(c(c1)C(=O)O)c1c2ccc(c(c2oc2c1ccc(=[NH2+])c2S(=O)(=O)[O-])S(=O)(=O)O)N)NCCCCCCn1nnc(c1)CCCCN1CCC(CC1)c1ccc(cc1)c1cc(cc2c1ccc(c2)c1ccc(cc1)C(F)(F)F)C(=O)O 10.1021/acs.jmedchem.0c00745
CHEMBL4447162 9445 0 None - 1 Human 10.1 pKi = 10.1 Binding
Inhibition of human P2Y14RInhibition of human P2Y14R
ChEMBL 1213 21 6 14 9.3 O=C(c1ccc(c(c1)C(=O)O)c1c2ccc(c(c2oc2c1ccc(=[NH2+])c2S(=O)(=O)[O-])S(=O)(=O)O)N)NCCCCCCn1nnc(c1)CCCCN1CCC(CC1)c1ccc(cc1)c1cc(cc2c1ccc(c2)c1ccc(cc1)C(F)(F)F)C(=O)O 10.1021/acs.jmedchem.0c00745
42611190 9930 12 None 1 5 Rat 9.4 pKi = 9.4 Binding
Antagonist activity at P2Y14R in rat C6 cells assessed as suppression of UDP-glucose-mediated inhibition of forskolin-stimulated [3H]cyclic-AMP accumulation after 15 mins in presence of [3H]-adenineAntagonist activity at P2Y14R in rat C6 cells assessed as suppression of UDP-glucose-mediated inhibition of forskolin-stimulated [3H]cyclic-AMP accumulation after 15 mins in presence of [3H]-adenine
ChEMBL 475 4 2 2 7.4 OC(=O)c1cc2cc(ccc2c(c1)c1ccc(cc1)C1CCNCC1)c1ccc(cc1)C(F)(F)F 10.1021/acs.jmedchem.8b00168
5802 9930 12 None 1 5 Rat 9.4 pKi = 9.4 Binding
Antagonist activity at P2Y14R in rat C6 cells assessed as suppression of UDP-glucose-mediated inhibition of forskolin-stimulated [3H]cyclic-AMP accumulation after 15 mins in presence of [3H]-adenineAntagonist activity at P2Y14R in rat C6 cells assessed as suppression of UDP-glucose-mediated inhibition of forskolin-stimulated [3H]cyclic-AMP accumulation after 15 mins in presence of [3H]-adenine
ChEMBL 475 4 2 2 7.4 OC(=O)c1cc2cc(ccc2c(c1)c1ccc(cc1)C1CCNCC1)c1ccc(cc1)C(F)(F)F 10.1021/acs.jmedchem.8b00168
CHEMBL1800685 9930 12 None 1 5 Rat 9.4 pKi = 9.4 Binding
Antagonist activity at P2Y14R in rat C6 cells assessed as suppression of UDP-glucose-mediated inhibition of forskolin-stimulated [3H]cyclic-AMP accumulation after 15 mins in presence of [3H]-adenineAntagonist activity at P2Y14R in rat C6 cells assessed as suppression of UDP-glucose-mediated inhibition of forskolin-stimulated [3H]cyclic-AMP accumulation after 15 mins in presence of [3H]-adenine
ChEMBL 475 4 2 2 7.4 OC(=O)c1cc2cc(ccc2c(c1)c1ccc(cc1)C1CCNCC1)c1ccc(cc1)C(F)(F)F 10.1021/acs.jmedchem.8b00168
42630568 68847 0 None - 1 Mouse 5.9 pKi = 5.9 Binding
Inhibition of mouse P2Y14 receptor in presence of 2% HSAInhibition of mouse P2Y14 receptor in presence of 2% HSA
ChEMBL 472 5 2 2 7.2 O=C(O)c1cc(-c2ccc([C@@H](O)C(F)F)cc2)c2ccc(-c3ccc(C(F)(F)F)cc3)cc2c1 10.1016/j.ejmech.2019.04.068
CHEMBL1774903 68847 0 None - 1 Mouse 5.9 pKi = 5.9 Binding
Inhibition of mouse P2Y14 receptor in presence of 2% HSAInhibition of mouse P2Y14 receptor in presence of 2% HSA
ChEMBL 472 5 2 2 7.2 O=C(O)c1cc(-c2ccc([C@@H](O)C(F)F)cc2)c2ccc(-c3ccc(C(F)(F)F)cc3)cc2c1 10.1016/j.ejmech.2019.04.068
53234015 68455 0 None - 1 Human 6.8 pKi = 6.8 Binding
Antagonist activity at human recombinant P2Y14 assessed as inhibition constantAntagonist activity at human recombinant P2Y14 assessed as inhibition constant
ChEMBL 492 4 1 5 6.0 CCc1cccc(NC(=O)N2CCc3nc(-c4ccc5c(c4)OCO5)nc(-c4ccccc4C)c3C2)c1 10.1021/acs.jmedchem.5b01972
CHEMBL1771456 68455 0 None - 1 Human 6.8 pKi = 6.8 Binding
Antagonist activity at human recombinant P2Y14 assessed as inhibition constantAntagonist activity at human recombinant P2Y14 assessed as inhibition constant
ChEMBL 492 4 1 5 6.0 CCc1cccc(NC(=O)N2CCc3nc(-c4ccc5c(c4)OCO5)nc(-c4ccccc4C)c3C2)c1 10.1021/acs.jmedchem.5b01972
42611190 9930 12 None -1 5 Human 8.6 pKi = 8.6 Binding
Selectivity interaction (Binding assay (using HEK293 cells)) EUB0000274bCl P2RY14Selectivity interaction (Binding assay (using HEK293 cells)) EUB0000274bCl P2RY14
ChEMBL 475 4 2 2 7.4 OC(=O)c1cc2cc(ccc2c(c1)c1ccc(cc1)C1CCNCC1)c1ccc(cc1)C(F)(F)F 10.6019/CHEMBL5212743
5802 9930 12 None -1 5 Human 8.6 pKi = 8.6 Binding
Selectivity interaction (Binding assay (using HEK293 cells)) EUB0000274bCl P2RY14Selectivity interaction (Binding assay (using HEK293 cells)) EUB0000274bCl P2RY14
ChEMBL 475 4 2 2 7.4 OC(=O)c1cc2cc(ccc2c(c1)c1ccc(cc1)C1CCNCC1)c1ccc(cc1)C(F)(F)F 10.6019/CHEMBL5212743
CHEMBL1800685 9930 12 None -1 5 Human 8.6 pKi = 8.6 Binding
Selectivity interaction (Binding assay (using HEK293 cells)) EUB0000274bCl P2RY14Selectivity interaction (Binding assay (using HEK293 cells)) EUB0000274bCl P2RY14
ChEMBL 475 4 2 2 7.4 OC(=O)c1cc2cc(ccc2c(c1)c1ccc(cc1)C1CCNCC1)c1ccc(cc1)C(F)(F)F 10.6019/CHEMBL5212743
68530100 94238 0 None -117 3 Human 5.6 pKi = 5.6 Binding
Inhibition of human P2Y14 receptorInhibition of human P2Y14 receptor
ChEMBL 391 4 2 3 6.5 Cc1ccc(NC(=O)Nc2cccnc2Sc2ccccc2C(C)(C)C)cc1 10.1021/jm301708u
CHEMBL2333767 94238 0 None -117 3 Human 5.6 pKi = 5.6 Binding
Inhibition of human P2Y14 receptorInhibition of human P2Y14 receptor
ChEMBL 391 4 2 3 6.5 Cc1ccc(NC(=O)Nc2cccnc2Sc2ccccc2C(C)(C)C)cc1 10.1021/jm301708u
11510273 94242 0 None -208 3 Human 5.5 pKi = 5.5 Binding
Inhibition of human P2Y14 receptorInhibition of human P2Y14 receptor
ChEMBL 431 6 2 4 6.5 CC(C)c1ccccc1Oc1ncccc1NC(=O)Nc1ccc(OC(F)(F)F)cc1 10.1021/jm301708u
CHEMBL2333773 94242 0 None -208 3 Human 5.5 pKi = 5.5 Binding
Inhibition of human P2Y14 receptorInhibition of human P2Y14 receptor
ChEMBL 431 6 2 4 6.5 CC(C)c1ccccc1Oc1ncccc1NC(=O)Nc1ccc(OC(F)(F)F)cc1 10.1021/jm301708u
42611190 9930 12 None -87 5 Mouse 7.5 pKi = 7.5 Binding
Inhibition of mouse P2Y14 receptor in presence of 2% HSAInhibition of mouse P2Y14 receptor in presence of 2% HSA
ChEMBL 475 4 2 2 7.4 OC(=O)c1cc2cc(ccc2c(c1)c1ccc(cc1)C1CCNCC1)c1ccc(cc1)C(F)(F)F 10.1016/j.ejmech.2019.04.068
5802 9930 12 None -87 5 Mouse 7.5 pKi = 7.5 Binding
Inhibition of mouse P2Y14 receptor in presence of 2% HSAInhibition of mouse P2Y14 receptor in presence of 2% HSA
ChEMBL 475 4 2 2 7.4 OC(=O)c1cc2cc(ccc2c(c1)c1ccc(cc1)C1CCNCC1)c1ccc(cc1)C(F)(F)F 10.1016/j.ejmech.2019.04.068
CHEMBL1800685 9930 12 None -87 5 Mouse 7.5 pKi = 7.5 Binding
Inhibition of mouse P2Y14 receptor in presence of 2% HSAInhibition of mouse P2Y14 receptor in presence of 2% HSA
ChEMBL 475 4 2 2 7.4 OC(=O)c1cc2cc(ccc2c(c1)c1ccc(cc1)C1CCNCC1)c1ccc(cc1)C(F)(F)F 10.1016/j.ejmech.2019.04.068
11510579 7477 52 None -128 2 Human 5.5 pKi = 5.5 Binding
Inhibition of human P2Y14 receptorInhibition of human P2Y14 receptor
ChEMBL 445 5 2 4 6.7 O=C(Nc1cccnc1Oc1ccccc1C(C)(C)C)Nc1ccc(cc1)OC(F)(F)F 10.1021/jm301708u
5808 7477 52 None -128 2 Human 5.5 pKi = 5.5 Binding
Inhibition of human P2Y14 receptorInhibition of human P2Y14 receptor
ChEMBL 445 5 2 4 6.7 O=C(Nc1cccnc1Oc1ccccc1C(C)(C)C)Nc1ccc(cc1)OC(F)(F)F 10.1021/jm301708u
CHEMBL2333770 7477 52 None -128 2 Human 5.5 pKi = 5.5 Binding
Inhibition of human P2Y14 receptorInhibition of human P2Y14 receptor
ChEMBL 445 5 2 4 6.7 O=C(Nc1cccnc1Oc1ccccc1C(C)(C)C)Nc1ccc(cc1)OC(F)(F)F 10.1021/jm301708u
42630568 68847 0 None - 1 Mouse 8.4 pKi = 8.4 Binding
Inhibition of mouse P2Y14 receptorInhibition of mouse P2Y14 receptor
ChEMBL 472 5 2 2 7.2 O=C(O)c1cc(-c2ccc([C@@H](O)C(F)F)cc2)c2ccc(-c3ccc(C(F)(F)F)cc3)cc2c1 10.1016/j.ejmech.2019.04.068
CHEMBL1774903 68847 0 None - 1 Mouse 8.4 pKi = 8.4 Binding
Inhibition of mouse P2Y14 receptorInhibition of mouse P2Y14 receptor
ChEMBL 472 5 2 2 7.2 O=C(O)c1cc(-c2ccc([C@@H](O)C(F)F)cc2)c2ccc(-c3ccc(C(F)(F)F)cc3)cc2c1 10.1016/j.ejmech.2019.04.068
11611428 94240 0 None -758 2 Human 5.2 pKi = 5.2 Binding
Inhibition of human P2Y14 receptorInhibition of human P2Y14 receptor
ChEMBL 417 4 2 3 7.1 CC(C)(C)c1ccc(NC(=O)Nc2cccnc2Oc2ccccc2C(C)(C)C)cc1 10.1021/jm301708u
CHEMBL2333771 94240 0 None -758 2 Human 5.2 pKi = 5.2 Binding
Inhibition of human P2Y14 receptorInhibition of human P2Y14 receptor
ChEMBL 417 4 2 3 7.1 CC(C)(C)c1ccc(NC(=O)Nc2cccnc2Oc2ccccc2C(C)(C)C)cc1 10.1021/jm301708u
CHEMBL4566600 220793 0 None -4 6 Human 5.1 pKi = 5.1 Binding
Affinity On-target Cellular interaction (Binding assay in HEK293 cells) EUB0000337aCl P2RY14Affinity On-target Cellular interaction (Binding assay in HEK293 cells) EUB0000337aCl P2RY14
ChEMBL None None None Cc1c(C(=O)O)cc(-c2ccc(C3CCNCC3)cc2)c2ccc(-c3ccc(C(F)(F)F)cc3)cc12 10.6019/CHEMBL5210121
CHEMBL4745071 220793 0 None -4 6 Human 5.1 pKi = 5.1 Binding
Affinity On-target Cellular interaction (Binding assay in HEK293 cells) EUB0000337aCl P2RY14Affinity On-target Cellular interaction (Binding assay in HEK293 cells) EUB0000337aCl P2RY14
ChEMBL None None None Cc1c(C(=O)O)cc(-c2ccc(C3CCNCC3)cc2)c2ccc(-c3ccc(C(F)(F)F)cc3)cc12 10.6019/CHEMBL5210121
124221650 9445 0 None - 1 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1213 21 6 14 9.3 O=C(c1ccc(c(c1)C(=O)O)c1c2ccc(c(c2oc2c1ccc(=[NH2+])c2S(=O)(=O)[O-])S(=O)(=O)O)N)NCCCCCCn1nnc(c1)CCCCN1CCC(CC1)c1ccc(cc1)c1cc(cc2c1ccc(c2)c1ccc(cc1)C(F)(F)F)C(=O)O 25299434
124221651 9445 0 None - 1 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1213 21 6 14 9.3 O=C(c1ccc(c(c1)C(=O)O)c1c2ccc(c(c2oc2c1ccc(=[NH2+])c2S(=O)(=O)[O-])S(=O)(=O)O)N)NCCCCCCn1nnc(c1)CCCCN1CCC(CC1)c1ccc(cc1)c1cc(cc2c1ccc(c2)c1ccc(cc1)C(F)(F)F)C(=O)O 25299434
9470 9445 0 None - 1 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1213 21 6 14 9.3 O=C(c1ccc(c(c1)C(=O)O)c1c2ccc(c(c2oc2c1ccc(=[NH2+])c2S(=O)(=O)[O-])S(=O)(=O)O)N)NCCCCCCn1nnc(c1)CCCCN1CCC(CC1)c1ccc(cc1)c1cc(cc2c1ccc(c2)c1ccc(cc1)C(F)(F)F)C(=O)O 25299434
CHEMBL4447162 9445 0 None - 1 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1213 21 6 14 9.3 O=C(c1ccc(c(c1)C(=O)O)c1c2ccc(c(c2oc2c1ccc(=[NH2+])c2S(=O)(=O)[O-])S(=O)(=O)O)N)NCCCCCCn1nnc(c1)CCCCN1CCC(CC1)c1ccc(cc1)c1cc(cc2c1ccc(c2)c1ccc(cc1)C(F)(F)F)C(=O)O 25299434
42611190 9930 12 None -1 5 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 475 4 2 2 7.4 OC(=O)c1cc2cc(ccc2c(c1)c1ccc(cc1)C1CCNCC1)c1ccc(cc1)C(F)(F)F 23592514
5802 9930 12 None -1 5 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 475 4 2 2 7.4 OC(=O)c1cc2cc(ccc2c(c1)c1ccc(cc1)C1CCNCC1)c1ccc(cc1)C(F)(F)F 23592514
CHEMBL1800685 9930 12 None -1 5 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 475 4 2 2 7.4 OC(=O)c1cc2cc(ccc2c(c1)c1ccc(cc1)C1CCNCC1)c1ccc(cc1)C(F)(F)F 23592514