Ligand source activities (1 row/activity)





Ligands Receptor Assay information Chemical information
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name
GPCRdb ID #Vendors Reference
ligand
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Type Activity
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Activity
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Assay Type Assay Description Source Mol
weight
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H don H acc LogP Smiles DOI
117981510 133288 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 487 6 0 9 5.7 COc1cc(OCc2csc(-c3ccc(F)nc3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
CHEMBL3715479 133288 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 487 6 0 9 5.7 COc1cc(OCc2csc(-c3ccc(F)nc3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
117981393 134092 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 471 8 0 11 4.3 COc1cc(OCc2csc(CN(C)C)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3718225 134092 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 471 8 0 11 4.3 COc1cc(OCc2csc(CN(C)C)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
117981415 133571 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 520 8 1 11 5.4 COc1cc(OCc2csc(-c3ccc(CO)cc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3716420 133571 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 520 8 1 11 5.4 COc1cc(OCc2csc(-c3ccc(CO)cc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
117981401 133514 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 513 7 0 12 4.5 COc1cc(OCc2csc(N3CCCOCC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3716230 133514 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 513 7 0 12 4.5 COc1cc(OCc2csc(N3CCCOCC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72190588 133782 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 576 8 0 13 3.3 COc1cc(OCc2csc(N3CCN(S(C)(=O)=O)CC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3717127 133782 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 576 8 0 13 3.3 COc1cc(OCc2csc(N3CCN(S(C)(=O)=O)CC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72189039 133397 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 547 8 1 11 5.3 CNC(=O)c1ccc(-c2nc(COc3cc(OC)cc4oc(-c5cn6nc(OC)sc6n5)cc34)cs2)cc1 nan
CHEMBL3715840 133397 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 547 8 1 11 5.3 CNC(=O)c1ccc(-c2nc(COc3cc(OC)cc4oc(-c5cn6nc(OC)sc6n5)cc34)cs2)cc1 nan
117981472 133757 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 524 9 1 11 5.3 COc1cc(OCc2csc(C(O)(C3CC3)C3CC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3717042 133757 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 524 9 1 11 5.3 COc1cc(OCc2csc(C(O)(C3CC3)C3CC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
89878842 133808 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 533 8 1 11 5.0 COc1cc(OCc2csc(-c3ccc(C(N)=O)cc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3717235 133808 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 533 8 1 11 5.0 COc1cc(OCc2csc(-c3ccc(C(N)=O)cc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
117981394 133978 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 527 7 0 12 4.9 COc1cc(OCc2csc(N3C[C@H](C)O[C@H](C)C3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3717808 133978 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 527 7 0 12 4.9 COc1cc(OCc2csc(N3C[C@H](C)O[C@H](C)C3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
89873043 134267 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 512 7 0 11 5.3 COc1cc(OCc2csc(C3(C)CCOCC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3718763 134267 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 512 7 0 11 5.3 COc1cc(OCc2csc(C3(C)CCOCC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
89872927 133483 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 633 9 1 13 5.0 COc1cc(OCc2csc(C3(NS(=O)(=O)C(C)(C)C)CCOCC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3716142 133483 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 633 9 1 13 5.0 COc1cc(OCc2csc(C3(NS(=O)(=O)C(C)(C)C)CCOCC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72189948 133923 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 557 8 1 13 4.3 COc1cc(OCc2nc(N3CCOCC3)sc2C(C)(C)O)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3717618 133923 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 557 8 1 13 4.3 COc1cc(OCc2nc(N3CCOCC3)sc2C(C)(C)O)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
117981574 134222 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 614 11 0 12 6.3 CCN(CCC#N)C(=O)c1ccc(-c2nc(COc3cc(OC)cc4oc(-c5cn6nc(OC)sc6n5)cc34)cs2)cc1 nan
CHEMBL3718631 134222 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 614 11 0 12 6.3 CCN(CCC#N)C(=O)c1ccc(-c2nc(COc3cc(OC)cc4oc(-c5cn6nc(OC)sc6n5)cc34)cs2)cc1 nan
72191818 134249 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 542 7 1 12 5.0 COc1cc(OCc2csc(C3(O)CC(C)OC(C)C3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3718707 134249 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 542 7 1 12 5.0 COc1cc(OCc2csc(C3(O)CC(C)OC(C)C3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
89873110 133948 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 546 7 0 11 6.2 COc1cc(OCc2csc(C3CCOc4ccccc43)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3717706 133948 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 546 7 0 11 6.2 COc1cc(OCc2csc(C3CCOc4ccccc43)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
89873293 133275 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 494 6 0 9 5.5 COc1cc(OCc2csc(C3(F)CCOCC3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
CHEMBL3715442 133275 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 494 6 0 9 5.5 COc1cc(OCc2csc(C3(F)CCOCC3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
72192133 133461 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 528 7 1 12 4.6 COc1cc(OCc2nc(C3(O)CCOCC3)sc2C)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3716059 133461 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 528 7 1 12 4.6 COc1cc(OCc2nc(C3(O)CCOCC3)sc2C)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
89873157 133178 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 591 7 0 10 6.9 COc1nn2cc(-c3cc4c(OCc5csc(-c6ccc(C(=O)N(C)C(C)(C)C)cc6)n5)cc(F)cc4o3)nc2s1 nan
CHEMBL3715043 133178 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 591 7 0 10 6.9 COc1nn2cc(-c3cc4c(OCc5csc(-c6ccc(C(=O)N(C)C(C)(C)C)cc6)n5)cc(F)cc4o3)nc2s1 nan
72189642 134010 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 567 7 0 12 5.1 COc1cc(OCc2nc(N3CCOCC3)sc2C(F)(F)F)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3717937 134010 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 567 7 0 12 5.1 COc1cc(OCc2nc(N3CCOCC3)sc2C(F)(F)F)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72190891 133114 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 555 7 0 13 4.6 COc1cc(OCc2csc(N3CCC4(CC3)OCCO4)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3714842 133114 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 555 7 0 13 4.6 COc1cc(OCc2csc(N3CCC4(CC3)OCCO4)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
117981465 133400 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 540 8 1 11 6.0 COc1cc(OCc2csc(C(C)(O)C3CCCCC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3715853 133400 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 540 8 1 11 6.0 COc1cc(OCc2csc(C(C)(O)C3CCCCC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
117981511 134279 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 501 6 0 9 6.0 COc1cc(OCc2nc(-c3ccnc(F)c3)sc2C)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
CHEMBL3718801 134279 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 501 6 0 9 6.0 COc1cc(OCc2nc(-c3ccnc(F)c3)sc2C)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
71769562 133398 1 None - 1 Human 9.5 pEC50 = 9.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 490 7 0 10 5.9 COc1cc(OCc2csc(-c3ccccc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3715848 133398 1 None - 1 Human 9.5 pEC50 = 9.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 490 7 0 10 5.9 COc1cc(OCc2csc(-c3ccccc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
89878645 133491 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 508 7 0 10 6.1 COc1cc(OCc2csc(-c3ccc(F)cc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3716160 133491 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 508 7 0 10 6.1 COc1cc(OCc2csc(-c3ccc(F)cc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72191507 133857 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 481 7 0 12 4.9 COc1cc(OCc2csc(-c3ccno3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3717419 133857 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 481 7 0 12 4.9 COc1cc(OCc2csc(-c3ccno3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
89878659 134012 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 491 7 0 11 5.3 COc1cc(OCc2csc(-c3ccncc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3717956 134012 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 491 7 0 11 5.3 COc1cc(OCc2csc(-c3ccncc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
89872950 134108 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 527 8 0 12 4.7 CCc1sc(N2CCOCC2)nc1COc1cc(OC)cc2oc(-c3cn4nc(OC)sc4n3)cc12 nan
CHEMBL3718267 134108 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 527 8 0 12 4.7 CCc1sc(N2CCOCC2)nc1COc1cc(OC)cc2oc(-c3cn4nc(OC)sc4n3)cc12 nan
72189947 133407 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 543 9 0 13 4.2 COCc1sc(N2CCOCC2)nc1COc1cc(OC)cc2oc(-c3cn4nc(OC)sc4n3)cc12 nan
CHEMBL3715876 133407 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 543 9 0 13 4.2 COCc1sc(N2CCOCC2)nc1COc1cc(OC)cc2oc(-c3cn4nc(OC)sc4n3)cc12 nan
72191815 133630 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 514 7 1 12 4.3 COc1cc(OCc2csc(C3(O)CCOCC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3716623 133630 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 514 7 1 12 4.3 COc1cc(OCc2csc(C3(O)CCOCC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
117981405 133656 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 510 8 0 10 5.8 COc1cc(OCc2csc(CCC(F)(F)F)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3716723 133656 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 510 8 0 10 5.8 COc1cc(OCc2csc(CCC(F)(F)F)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72192135 133709 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 570 7 1 13 4.8 COc1cc(OCc2csc(C3(O)CCC4(CC3)OCCO4)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3716904 133709 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 570 7 1 13 4.8 COc1cc(OCc2csc(C3(O)CCC4(CC3)OCCO4)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72191505 134228 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 532 7 0 10 6.6 COc1cc(OCc2csc(C3CCC(F)(F)CC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3718639 134228 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 532 7 0 10 6.6 COc1cc(OCc2csc(C3CCC(F)(F)CC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
117981413 133141 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 509 7 0 11 5.5 COc1cc(OCc2csc(-c3ccnc(F)c3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3714941 133141 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 509 7 0 11 5.5 COc1cc(OCc2csc(-c3ccnc(F)c3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
89879334 133309 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 532 7 0 10 6.3 COc1cc(OCc2csc(C3(F)CCOCC3)n2)c2cc(-c3cn4nc([C@H](C)F)sc4n3)oc2c1 nan
CHEMBL3715557 133309 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 532 7 0 10 6.3 COc1cc(OCc2csc(C3(F)CCOCC3)n2)c2cc(-c3cn4nc([C@H](C)F)sc4n3)oc2c1 nan
72189042 134246 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 551 8 0 11 6.6 COc1cc(OCc2nc(-c3ccnc(F)c3)sc2C(C)C)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3718692 134246 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 551 8 0 11 6.6 COc1cc(OCc2nc(-c3ccnc(F)c3)sc2C(C)C)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72192425 133637 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 526 7 1 12 4.6 COc1cc(OCc2csc(C3(O)CCC(=O)CC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3716638 133637 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 526 7 1 12 4.6 COc1cc(OCc2csc(C3(O)CCC(=O)CC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
89879331 133536 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 575 7 0 10 6.3 COc1nn2cc(-c3cc4c(OCc5csc(-c6ccc(C(=O)N7CCCC7)cc6)n5)cc(F)cc4o3)nc2s1 nan
CHEMBL3716290 133536 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 575 7 0 10 6.3 COc1nn2cc(-c3cc4c(OCc5csc(-c6ccc(C(=O)N7CCCC7)cc6)n5)cc(F)cc4o3)nc2s1 nan
72190589 133735 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 663 9 0 14 4.6 COc1cc(OCc2csc(N3CCN(S(=O)(=O)c4ccc(C#N)cc4)CC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3716986 133735 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 663 9 0 14 4.6 COc1cc(OCc2csc(N3CCN(S(=O)(=O)c4ccc(C#N)cc4)CC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
117981398 134344 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 547 7 0 13 3.5 COc1cc(OCc2csc(N3CCS(=O)(=O)CC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3719034 134344 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 547 7 0 13 3.5 COc1cc(OCc2csc(N3CCS(=O)(=O)CC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
117981576 134411 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 600 10 0 12 5.9 CCN(CC#N)C(=O)c1ccc(-c2nc(COc3cc(OC)cc4oc(-c5cn6nc(OC)sc6n5)cc34)cs2)cc1 nan
CHEMBL3719256 134411 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 600 10 0 12 5.9 CCN(CC#N)C(=O)c1ccc(-c2nc(COc3cc(OC)cc4oc(-c5cn6nc(OC)sc6n5)cc34)cs2)cc1 nan
117981596 133412 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 601 10 0 11 6.4 COc1cc(OCc2csc(-c3ccc(C(=O)N(C)CC4CC4)cc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3715900 133412 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 601 10 0 11 6.4 COc1cc(OCc2csc(-c3ccc(C(=O)N(C)CC4CC4)cc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72192721 133484 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 512 7 1 11 5.4 COc1cc(OCc2csc(C3(O)CCCCC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3716144 133484 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 512 7 1 11 5.4 COc1cc(OCc2csc(C3(O)CCCCC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72190586 133668 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 509 7 0 12 4.2 COc1cc(OCc2coc(N3CC4CCC(C3)O4)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3716763 133668 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 509 7 0 12 4.2 COc1cc(OCc2coc(N3CC4CCC(C3)O4)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72191203 133865 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 575 8 0 12 4.4 COc1cc(OCc2csc(C3CCN(S(C)(=O)=O)CC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3717435 133865 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 575 8 0 12 4.4 COc1cc(OCc2csc(C3CCN(S(C)(=O)=O)CC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72192725 134363 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 594 8 0 12 6.8 COc1cc(OCc2csc(C3=CCC(C(=O)OC(C)(C)C)CC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3719085 134363 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 594 8 0 12 6.8 COc1cc(OCc2csc(C3=CCC(C(=O)OC(C)(C)C)CC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
117981406 133184 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 482 9 0 10 5.6 COc1cc(OCc2csc(CCC3CC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3715066 133184 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 482 9 0 10 5.6 COc1cc(OCc2csc(CCC3CC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
89879356 133510 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 574 8 0 11 5.7 COc1nn2cc(-c3cc4c(OCc5csc(-c6ccc(C(=O)N(C)CC#N)cc6)n5)cc(F)cc4o3)nc2s1 nan
CHEMBL3716212 133510 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 574 8 0 11 5.7 COc1nn2cc(-c3cc4c(OCc5csc(-c6ccc(C(=O)N(C)CC#N)cc6)n5)cc(F)cc4o3)nc2s1 nan
117981467 134189 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 526 7 1 11 5.0 COc1cc(OCc2csc(C(C)(O)C(F)(F)F)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3718540 134189 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 526 7 1 11 5.0 COc1cc(OCc2csc(C(C)(O)C(F)(F)F)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
117981578 133197 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 603 9 0 12 5.4 COc1cc(OCc2csc(-c3ccc(C(=O)N4CC(OC)C4)cc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3715100 133197 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 603 9 0 12 5.4 COc1cc(OCc2csc(-c3ccc(C(=O)N4CC(OC)C4)cc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72192427 133691 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 617 8 1 12 5.4 COc1cc(OCc2csc(C3(O)CCN(C(=O)c4ccccc4)CC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3716844 133691 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 617 8 1 12 5.4 COc1cc(OCc2csc(C3(O)CCN(C(=O)c4ccccc4)CC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
117981419 134071 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 523 7 0 11 5.8 COc1cc(OCc2nc(-c3cccnc3F)sc2C)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3718152 134071 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 523 7 0 11 5.8 COc1cc(OCc2nc(-c3cccnc3F)sc2C)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
89873238 133479 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 604 9 0 12 6.4 COc1ccc(C2(c3nc(COc4cc(OC)cc5oc(-c6cn7nc(OC)sc7n6)cc45)cs3)CCOCC2)cc1 nan
CHEMBL3716135 133479 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 604 9 0 12 6.4 COc1ccc(C2(c3nc(COc4cc(OC)cc5oc(-c6cn7nc(OC)sc7n6)cc45)cs3)CCOCC2)cc1 nan
117981463 133561 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 542 8 0 10 6.4 CCC(F)(c1nc(COc2cc(OC)cc3oc(-c4cn5nc(OC)sc5n4)cc23)cs1)C(F)(F)F nan
CHEMBL3716372 133561 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 542 8 0 10 6.4 CCC(F)(c1nc(COc2cc(OC)cc3oc(-c4cn5nc(OC)sc5n4)cc23)cs1)C(F)(F)F nan
89873140 134388 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 549 7 0 10 5.8 COc1nn2cc(-c3cc4c(OCc5csc(-c6ccc(C(=O)N(C)C)cc6)n5)cc(F)cc4o3)nc2s1 nan
CHEMBL3719195 134388 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 549 7 0 10 5.8 COc1nn2cc(-c3cc4c(OCc5csc(-c6ccc(C(=O)N(C)C)cc6)n5)cc(F)cc4o3)nc2s1 nan
117981418 133328 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 576 9 0 12 6.3 COc1cc(OCc2nc(-c3cccc(COC(C)=O)c3)sc2C)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3715612 133328 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 576 9 0 12 6.3 COc1cc(OCc2nc(-c3cccc(COC(C)=O)c3)sc2C)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
117974661 133418 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 558 7 1 11 6.1 COc1cc(OCc2csc(C3(O)CC(C)OC(C)C3)n2)c2cc(-c3cn4nc([C@H](C)F)sc4n3)oc2c1 nan
CHEMBL3715913 133418 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 558 7 1 11 6.1 COc1cc(OCc2csc(C3(O)CC(C)OC(C)C3)n2)c2cc(-c3cn4nc([C@H](C)F)sc4n3)oc2c1 nan
117981583 133798 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 591 10 1 12 5.0 COc1cc(OCc2csc(-c3ccc(C(=O)N(C)CCO)cc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3717186 133798 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 591 10 1 12 5.0 COc1cc(OCc2csc(-c3ccc(C(=O)N(C)CCO)cc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
117981530 134229 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 554 7 0 12 4.6 COc1cc(OCc2csc(N3CCN(c4cnccn4)CC3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
CHEMBL3718641 134229 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 554 7 0 12 4.6 COc1cc(OCc2csc(N3CCN(c4cnccn4)CC3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
72193010 134237 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 482 6 0 10 5.3 COc1cc(OCc2csc(C(F)(F)F)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3718657 134237 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 482 6 0 10 5.3 COc1cc(OCc2csc(C(F)(F)F)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
10269 671 21 None - 1 Human 9.4 pEC50 = 9.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 513 7 0 12 4.4 COc1cc(OCc2nc(sc2C)N2CCOCC2)c2c(c1)oc(c2)c1cn2c(n1)sc(n2)OC nan
72190270 671 21 None - 1 Human 9.4 pEC50 = 9.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 513 7 0 12 4.4 COc1cc(OCc2nc(sc2C)N2CCOCC2)c2c(c1)oc(c2)c1cn2c(n1)sc(n2)OC nan
CHEMBL3716726 671 21 None - 1 Human 9.4 pEC50 = 9.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 513 7 0 12 4.4 COc1cc(OCc2nc(sc2C)N2CCOCC2)c2c(c1)oc(c2)c1cn2c(n1)sc(n2)OC nan
72191508 133417 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 481 7 0 12 4.9 COc1cc(OCc2csc(-c3cnco3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3715912 133417 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 481 7 0 12 4.9 COc1cc(OCc2csc(-c3cnco3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72191504 133790 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 637 9 0 12 5.8 COc1cc(OCc2csc(C3CCN(S(=O)(=O)c4ccccc4)CC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3717160 133790 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 637 9 0 12 5.8 COc1cc(OCc2csc(C3CCN(S(=O)(=O)c4ccccc4)CC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
117981595 134020 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 643 12 0 11 7.6 CCCN(C(=O)c1ccc(-c2nc(COc3cc(OC)cc4oc(-c5cn6nc(OC)sc6n5)cc34)cs2)cc1)C(C)C1CC1 nan
CHEMBL3717974 134020 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 643 12 0 11 7.6 CCCN(C(=O)c1ccc(-c2nc(COc3cc(OC)cc4oc(-c5cn6nc(OC)sc6n5)cc34)cs2)cc1)C(C)C1CC1 nan
89878648 134043 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 497 7 0 11 5.2 COc1cc(OCc2csc(N3CCCCC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3718059 134043 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 497 7 0 11 5.2 COc1cc(OCc2csc(N3CCCCC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
117981517 133874 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 511 6 0 9 5.7 COc1cc(OCc2csc(N3CCC(F)(F)CC3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
CHEMBL3717467 133874 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 511 6 0 9 5.7 COc1cc(OCc2csc(N3CCC(F)(F)CC3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
117981584 134355 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 615 8 0 11 6.8 COc1cc(OCc2csc(-c3ccc(C(=O)N4CCC(C)CC4)cc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3719068 134355 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 615 8 0 11 6.8 COc1cc(OCc2csc(-c3ccc(C(=O)N4CCC(C)CC4)cc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
12038 676 7 None - 1 Human 9.4 pEC50 = 9.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 561 8 0 11 5.6 COc1nn2cc(nc2s1)c1cc2c(o1)cc(OC)cc2OCc1csc(n1)c1ccc(cc1)C(=O)N(C)C nan
72188743 676 7 None - 1 Human 9.4 pEC50 = 9.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 561 8 0 11 5.6 COc1nn2cc(nc2s1)c1cc2c(o1)cc(OC)cc2OCc1csc(n1)c1ccc(cc1)C(=O)N(C)C nan
CHEMBL3716552 676 7 None - 1 Human 9.4 pEC50 = 9.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 561 8 0 11 5.6 COc1nn2cc(nc2s1)c1cc2c(o1)cc(OC)cc2OCc1csc(n1)c1ccc(cc1)C(=O)N(C)C nan
DB14942 676 7 None - 1 Human 9.4 pEC50 = 9.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 561 8 0 11 5.6 COc1nn2cc(nc2s1)c1cc2c(o1)cc(OC)cc2OCc1csc(n1)c1ccc(cc1)C(=O)N(C)C nan
117981468 133265 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 622 8 1 11 6.7 COc1cc(OCc2csc(C(O)(c3ccc(Cl)cc3)C(F)(F)F)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3715391 133265 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 622 8 1 11 6.7 COc1cc(OCc2csc(C(O)(c3ccc(Cl)cc3)C(F)(F)F)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72191817 133277 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 528 8 0 12 4.9 COc1cc(OCc2csc(C3(OC)CCOCC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3715446 133277 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 528 8 0 12 4.9 COc1cc(OCc2csc(C3(OC)CCOCC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72188744 133927 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 548 8 0 12 5.7 COC(=O)c1ccc(-c2nc(COc3cc(OC)cc4oc(-c5cn6nc(OC)sc6n5)cc34)cs2)cc1 nan
CHEMBL3717638 133927 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 548 8 0 12 5.7 COC(=O)c1ccc(-c2nc(COc3cc(OC)cc4oc(-c5cn6nc(OC)sc6n5)cc34)cs2)cc1 nan
89879019 134019 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 539 7 0 12 4.9 COc1cc(OCc2nc(N3CC4CCC(C3)O4)sc2C)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3717972 134019 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 539 7 0 12 4.9 COc1cc(OCc2nc(N3CC4CCC(C3)O4)sc2C)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
89879382 133289 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 530 7 1 11 5.3 COc1cc(OCc2csc(C3(O)CCOCC3)n2)c2cc(-c3cn4nc([C@H](C)F)sc4n3)oc2c1 nan
CHEMBL3715485 133289 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 530 7 1 11 5.3 COc1cc(OCc2csc(C3(O)CCOCC3)n2)c2cc(-c3cn4nc([C@H](C)F)sc4n3)oc2c1 nan
117981417 133673 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 523 7 0 11 5.8 COc1cc(OCc2nc(-c3ccnc(F)c3)sc2C)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3716787 133673 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 523 7 0 11 5.8 COc1cc(OCc2nc(-c3ccnc(F)c3)sc2C)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72188746 134165 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 605 11 0 12 5.6 COCCN(C)C(=O)c1ccc(-c2nc(COc3cc(OC)cc4oc(-c5cn6nc(OC)sc6n5)cc34)cs2)cc1 nan
CHEMBL3718433 134165 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 605 11 0 12 5.6 COCCN(C)C(=O)c1ccc(-c2nc(COc3cc(OC)cc4oc(-c5cn6nc(OC)sc6n5)cc34)cs2)cc1 nan
127024748 133209 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 518 6 1 11 4.9 COc1nn2cc(-c3cc4c(OCc5csc(C6(O)CCOCC6)n5)cc(Cl)cc4o3)nc2s1 nan
CHEMBL3715154 133209 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 518 6 1 11 4.9 COc1nn2cc(-c3cc4c(OCc5csc(C6(O)CCOCC6)n5)cc(Cl)cc4o3)nc2s1 nan
89879340 133294 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 602 10 0 11 6.4 CCN(CCC#N)C(=O)c1ccc(-c2nc(COc3cc(F)cc4oc(-c5cn6nc(OC)sc6n5)cc34)cs2)cc1 nan
CHEMBL3715502 133294 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 602 10 0 11 6.4 CCN(CCC#N)C(=O)c1ccc(-c2nc(COc3cc(F)cc4oc(-c5cn6nc(OC)sc6n5)cc34)cs2)cc1 nan
117981404 133465 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 514 7 0 11 5.9 COc1cc(OCc2csc(C3CCSCC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3716066 133465 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 514 7 0 11 5.9 COc1cc(OCc2csc(C3CCSCC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
117981466 133506 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 502 9 0 10 6.2 CCC(F)(CC)c1nc(COc2cc(OC)cc3oc(-c4cn5nc(OC)sc5n4)cc23)cs1 nan
CHEMBL3716197 133506 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 502 9 0 10 6.2 CCC(F)(CC)c1nc(COc2cc(OC)cc3oc(-c4cn5nc(OC)sc5n4)cc23)cs1 nan
117981571 133123 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 603 10 0 11 6.8 CCN(C(=O)c1ccc(-c2nc(COc3cc(OC)cc4oc(-c5cn6nc(OC)sc6n5)cc34)cs2)cc1)C(C)C nan
CHEMBL3714888 133123 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 603 10 0 11 6.8 CCN(C(=O)c1ccc(-c2nc(COc3cc(OC)cc4oc(-c5cn6nc(OC)sc6n5)cc34)cs2)cc1)C(C)C nan
117981408 133139 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 548 8 0 12 5.8 COc1cc(OCc2csc(-c3cccc(OC(C)=O)c3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3714934 133139 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 548 8 0 12 5.8 COc1cc(OCc2csc(-c3cccc(OC(C)=O)c3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
117981414 133427 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 562 9 0 12 6.0 COc1cc(OCc2csc(-c3ccc(COC(C)=O)cc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3715945 133427 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 562 9 0 12 6.0 COc1cc(OCc2csc(-c3ccc(COC(C)=O)cc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72191506 133441 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 629 8 0 12 5.3 COc1cc(OCc2csc(C3CCN(S(=O)(=O)C(F)(F)F)CC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3715995 133441 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 629 8 0 12 5.3 COc1cc(OCc2csc(C3CCN(S(=O)(=O)C(F)(F)F)CC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72192132 134300 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 500 7 1 12 3.9 COc1cc(OCc2csc(C3(O)CCOC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3718853 134300 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 500 7 1 12 3.9 COc1cc(OCc2csc(C3(O)CCOC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
89873005 134445 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 632 9 0 13 6.1 COC(=O)c1ccc(C2(c3nc(COc4cc(OC)cc5oc(-c6cn7nc(OC)sc7n6)cc45)cs3)CCOCC2)cc1 nan
CHEMBL3719375 134445 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 632 9 0 13 6.1 COC(=O)c1ccc(C2(c3nc(COc4cc(OC)cc5oc(-c6cn7nc(OC)sc7n6)cc45)cs3)CCOCC2)cc1 nan
117974678 133432 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 544 7 1 11 5.6 COc1cc(OCc2nc(C3(O)CCOCC3)sc2C)c2cc(-c3cn4nc([C@H](C)F)sc4n3)oc2c1 nan
CHEMBL3715953 133432 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 544 7 1 11 5.6 COc1cc(OCc2nc(C3(O)CCOCC3)sc2C)c2cc(-c3cn4nc([C@H](C)F)sc4n3)oc2c1 nan
72189345 133470 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 600 9 0 12 5.8 COc1cc(OCc2nc(-c3ccc(C(=O)N(C)CC#N)cc3)sc2C)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3716096 133470 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 600 9 0 12 5.8 COc1cc(OCc2nc(-c3ccc(C(=O)N(C)CC#N)cc3)sc2C)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
117981395 134130 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 456 7 0 10 5.4 COc1cc(OCc2csc(C(C)C)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3718313 134130 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 456 7 0 10 5.4 COc1cc(OCc2csc(C(C)C)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
117981581 133861 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 603 8 0 11 6.8 COc1cc(OCc2csc(-c3ccc(C(=O)N(C)C(C)(C)C)cc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3717425 133861 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 603 8 0 11 6.8 COc1cc(OCc2csc(-c3ccc(C(=O)N(C)C(C)(C)C)cc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72193337 133924 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 592 8 0 11 6.5 COc1cc(OCc2csc(C3(c4ccccc4F)CCOCC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3717630 133924 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 592 8 0 11 6.5 COc1cc(OCc2csc(C3(c4ccccc4F)CCOCC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
117981397 134410 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 515 7 0 12 4.8 COc1cc(OCc2csc(N3CCSCC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3719255 134410 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 515 7 0 12 4.8 COc1cc(OCc2csc(N3CCSCC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
117981590 133174 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 589 9 0 11 6.4 COc1cc(OCc2csc(-c3ccc(C(=O)N(C)C(C)C)cc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3715035 133174 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 589 9 0 11 6.4 COc1cc(OCc2csc(-c3ccc(C(=O)N(C)C(C)C)cc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
117981505 133509 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 553 7 0 9 6.2 COc1cc(OCc2nc(-c3ccc(C(=O)N(C)C)cc3)sc2C)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
CHEMBL3716211 133509 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 553 7 0 9 6.2 COc1cc(OCc2nc(-c3ccc(C(=O)N(C)C)cc3)sc2C)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
117981592 133642 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 603 11 0 11 6.8 CCCN(CC)C(=O)c1ccc(-c2nc(COc3cc(OC)cc4oc(-c5cn6nc(OC)sc6n5)cc34)cs2)cc1 nan
CHEMBL3716676 133642 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 603 11 0 11 6.8 CCCN(CC)C(=O)c1ccc(-c2nc(COc3cc(OC)cc4oc(-c5cn6nc(OC)sc6n5)cc34)cs2)cc1 nan
117981582 133387 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 601 10 0 11 6.5 CCN(C(=O)c1ccc(-c2nc(COc3cc(OC)cc4oc(-c5cn6nc(OC)sc6n5)cc34)cs2)cc1)C1CC1 nan
CHEMBL3715784 133387 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 601 10 0 11 6.5 CCN(C(=O)c1ccc(-c2nc(COc3cc(OC)cc4oc(-c5cn6nc(OC)sc6n5)cc34)cs2)cc1)C1CC1 nan
89878696 133492 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 508 7 0 10 6.1 COc1cc(OCc2csc(-c3cccc(F)c3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3716163 133492 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 508 7 0 10 6.1 COc1cc(OCc2csc(-c3cccc(F)c3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
117981497 133105 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 491 6 0 10 4.7 COc1cc(OCc2csc(N3CCCOCC3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
CHEMBL3714814 133105 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 491 6 0 10 4.7 COc1cc(OCc2csc(N3CCCOCC3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
89878888 133955 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 505 7 0 11 5.6 COc1cc(OCc2csc(-c3ccc(C)nc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3717746 133955 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 505 7 0 11 5.6 COc1cc(OCc2csc(-c3ccc(C)nc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
117981521 133175 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 510 6 0 8 6.8 COc1cc(OCc2csc(C3CCC(F)(F)CC3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
CHEMBL3715038 133175 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 510 6 0 8 6.8 COc1cc(OCc2csc(C3CCC(F)(F)CC3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
117981544 133614 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 489 6 0 9 5.7 COc1cc(OCc2csc(N3CCC(C)CC3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
CHEMBL3716564 133614 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 489 6 0 9 5.7 COc1cc(OCc2csc(N3CCC(C)CC3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
89879347 134292 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 549 7 1 10 5.7 CNC(=O)c1ccc(-c2nc(COc3cc(F)cc4oc(-c5cn6nc(OC)sc6n5)cc34)c(C)s2)cc1 nan
CHEMBL3718829 134292 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 549 7 1 10 5.7 CNC(=O)c1ccc(-c2nc(COc3cc(F)cc4oc(-c5cn6nc(OC)sc6n5)cc34)c(C)s2)cc1 nan
89878698 133843 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 533 7 0 11 5.5 COc1cc(OCc2csc(N3CCC(F)(F)CC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3717354 133843 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 533 7 0 11 5.5 COc1cc(OCc2csc(N3CCC(F)(F)CC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
117981525 134346 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 566 7 0 9 6.9 COc1cc(OCc2csc(C3(c4ccc(C)cc4)CCOCC3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
CHEMBL3719044 134346 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 566 7 0 9 6.9 COc1cc(OCc2csc(C3(c4ccc(C)cc4)CCOCC3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
117981573 133270 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 589 8 1 12 4.7 COc1cc(OCc2csc(-c3ccc(C(=O)N4CC(O)C4)cc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3715406 133270 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 589 8 1 12 4.7 COc1cc(OCc2csc(-c3ccc(C(=O)N4CC(O)C4)cc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
117981565 133451 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 540 7 1 11 6.8 COc1cc(OCc2csc(Nc3ccc4scnc4c3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
CHEMBL3716027 133451 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 540 7 1 11 6.8 COc1cc(OCc2csc(Nc3ccc4scnc4c3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
117981499 134024 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 493 6 0 10 5.0 COc1cc(OCc2csc(N3CCSCC3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
CHEMBL3717982 134024 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 493 6 0 10 5.0 COc1cc(OCc2csc(N3CCSCC3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
89873120 134290 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 545 8 0 11 6.1 COc1cc(OCc2csc(C3(c4cccnc4)CCC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3718827 134290 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 545 8 0 11 6.1 COc1cc(OCc2csc(C3(c4cccnc4)CCC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
86700890 134393 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 499 7 0 12 4.1 COc1cc(OCc2csc(N3CCOCC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3719215 134393 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 499 7 0 12 4.1 COc1cc(OCc2csc(N3CCOCC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
117981503 133779 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 539 7 0 9 5.9 COc1cc(OCc2csc(-c3ccc(C(=O)N(C)C)cc3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
CHEMBL3717115 133779 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 539 7 0 9 5.9 COc1cc(OCc2csc(-c3ccc(C(=O)N(C)C)cc3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
72193336 134174 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 608 8 0 11 7.0 COc1cc(OCc2csc(C3(c4cccc(Cl)c4)CCOCC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3718481 134174 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 608 8 0 11 7.0 COc1cc(OCc2csc(C3(c4cccc(Cl)c4)CCOCC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72190269 133332 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 525 7 0 12 4.6 COc1cc(OCc2csc(N3CC4CCC(C3)O4)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3715632 133332 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 525 7 0 12 4.6 COc1cc(OCc2csc(N3CC4CCC(C3)O4)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
117981409 134102 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 506 7 1 11 5.6 COc1cc(OCc2csc(-c3cccc(O)c3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3718254 134102 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 506 7 1 11 5.6 COc1cc(OCc2csc(-c3cccc(O)c3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
89878899 134143 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 587 8 0 11 6.2 COc1cc(OCc2csc(-c3ccc(C(=O)N4CCCC4)cc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3718360 134143 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 587 8 0 11 6.2 COc1cc(OCc2csc(-c3ccc(C(=O)N4CCCC4)cc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72190273 134307 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 497 7 0 12 3.9 COc1cc(OCc2nc(N3CCOCC3)oc2C)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3718867 134307 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 497 7 0 12 3.9 COc1cc(OCc2nc(N3CCOCC3)oc2C)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72190272 133110 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 483 7 0 12 3.6 COc1cc(OCc2coc(N3CCOCC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3714821 133110 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 483 7 0 12 3.6 COc1cc(OCc2coc(N3CCOCC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
117981407 133319 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 515 7 0 11 5.8 COc1cc(OCc2csc(-c3cccc(C#N)c3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3715590 133319 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 515 7 0 11 5.8 COc1cc(OCc2csc(-c3cccc(C#N)c3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
89878694 133399 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 442 7 0 10 4.8 CCc1nc(COc2cc(OC)cc3oc(-c4cn5nc(OC)sc5n4)cc23)cs1 nan
CHEMBL3715852 133399 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 442 7 0 10 4.8 CCc1nc(COc2cc(OC)cc3oc(-c4cn5nc(OC)sc5n4)cc23)cs1 nan
117981593 133895 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 575 9 0 11 6.0 CCN(C)C(=O)c1ccc(-c2nc(COc3cc(OC)cc4oc(-c5cn6nc(OC)sc6n5)cc34)cs2)cc1 nan
CHEMBL3717544 133895 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 575 9 0 11 6.0 CCN(C)C(=O)c1ccc(-c2nc(COc3cc(OC)cc4oc(-c5cn6nc(OC)sc6n5)cc34)cs2)cc1 nan
117981591 133171 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 600 10 0 12 5.9 COc1cc(OCc2csc(-c3ccc(C(=O)N(C)CCC#N)cc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3715025 133171 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 600 10 0 12 5.9 COc1cc(OCc2csc(-c3ccc(C(=O)N(C)CCC#N)cc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
89878657 133446 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 491 7 0 11 5.3 COc1cc(OCc2csc(-c3cccnc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3716019 133446 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 491 7 0 11 5.3 COc1cc(OCc2csc(-c3cccnc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
117981575 133463 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 623 8 0 11 6.4 COc1cc(OCc2csc(-c3ccc(C(=O)N4CCC(F)(F)C4)cc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3716064 133463 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 623 8 0 11 6.4 COc1cc(OCc2csc(-c3ccc(C(=O)N4CCC(F)(F)C4)cc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
117981502 134350 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 484 6 1 9 5.9 COc1cc(OCc2csc(-c3cccc(O)c3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
CHEMBL3719053 134350 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 484 6 1 9 5.9 COc1cc(OCc2csc(-c3cccc(O)c3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
117981516 134245 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 546 7 0 10 5.6 COc1cc(OCc2csc(-c3ccc(S(C)(=O)=O)cc3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
CHEMBL3718689 134245 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 546 7 0 10 5.6 COc1cc(OCc2csc(-c3ccc(S(C)(=O)=O)cc3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
72192428 134248 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 582 7 1 12 5.3 COc1cc(OCc2nc(C3(O)CCOCC3)sc2C(F)(F)F)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3718695 134248 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 582 7 1 12 5.3 COc1cc(OCc2nc(C3(O)CCOCC3)sc2C(F)(F)F)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
89873143 133236 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 574 8 0 11 6.4 COc1cc(OCc2csc(C3(c4ccccc4)CCOCC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3715261 133236 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 574 8 0 11 6.4 COc1cc(OCc2csc(C3(c4ccccc4)CCOCC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
117981402 133291 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 534 7 0 12 5.7 COc1cc(OCc2csc(-c3ccc4c(c3)OCO4)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3715491 133291 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 534 7 0 12 5.7 COc1cc(OCc2csc(-c3ccc4c(c3)OCO4)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
89879309 134087 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 670 10 2 14 4.9 COc1cc(OCc2csc(C3(NC(=O)CNC(=O)OC(C)(C)C)CCOCC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3718195 134087 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 670 10 2 14 4.9 COc1cc(OCc2csc(C3(NC(=O)CNC(=O)OC(C)(C)C)CCOCC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
117981461 134252 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 500 9 1 11 5.3 CCC(O)(CC)c1nc(COc2cc(OC)cc3oc(-c4cn5nc(OC)sc5n4)cc23)cs1 nan
CHEMBL3718712 134252 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 500 9 1 11 5.3 CCC(O)(CC)c1nc(COc2cc(OC)cc3oc(-c4cn5nc(OC)sc5n4)cc23)cs1 nan
72190892 133965 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 511 7 0 12 4.1 COc1cc(OCc2csc(N3CC4(COC4)C3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3717779 133965 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 511 7 0 12 4.1 COc1cc(OCc2csc(N3CC4(COC4)C3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72193330 134064 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 502 11 0 12 4.4 COCCOCc1nc(COc2cc(OC)cc3oc(-c4cn5nc(OC)sc5n4)cc23)cs1 nan
CHEMBL3718116 134064 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 502 11 0 12 4.4 COCCOCc1nc(COc2cc(OC)cc3oc(-c4cn5nc(OC)sc5n4)cc23)cs1 nan
72193014 134220 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 608 9 1 13 4.6 COc1cc(OCc2csc(C3(O)CCC(C(=O)N(C)CC#N)CC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3718626 134220 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 608 9 1 13 4.6 COc1cc(OCc2csc(C3(O)CCC(C(=O)N(C)CC#N)CC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72191200 133632 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 597 7 0 12 6.4 COc1cc(OCc2csc(C3CCN(C(=O)OC(C)(C)C)CC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3716630 133632 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 597 7 0 12 6.4 COc1cc(OCc2csc(C3CCN(C(=O)OC(C)(C)C)CC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72189946 133780 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 529 8 1 13 3.6 COc1cc(OCc2nc(N3CCOCC3)sc2CO)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3717116 133780 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 529 8 1 13 3.6 COc1cc(OCc2nc(N3CCOCC3)sc2CO)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
89878693 133894 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 512 7 0 12 4.0 COc1cc(OCc2csc(N3CCN(C)CC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3717535 133894 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 512 7 0 12 4.0 COc1cc(OCc2csc(N3CCN(C)CC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
89872973 134397 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 645 9 0 12 6.1 COc1cc(OCc2csc(C3(c4ccc(C(=O)N(C)C)cc4)CCOCC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3719223 134397 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 645 9 0 12 6.1 COc1cc(OCc2csc(C3(c4ccc(C(=O)N(C)C)cc4)CCOCC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
89873104 133130 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 469 6 0 9 5.6 COc1cc(OCc2csc(-c3ccncc3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
CHEMBL3714914 133130 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 469 6 0 9 5.6 COc1cc(OCc2csc(-c3ccncc3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
89873256 133360 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 492 6 0 9 6.1 COc1cc(OCc2csc(C3CCSCC3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
CHEMBL3715716 133360 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 492 6 0 9 6.1 COc1cc(OCc2csc(C3CCSCC3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
117981577 133381 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 577 10 2 12 4.6 COc1cc(OCc2csc(-c3ccc(C(=O)NCCO)cc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3715770 133381 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 577 10 2 12 4.6 COc1cc(OCc2csc(-c3ccc(C(=O)NCCO)cc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
89879381 133786 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 603 8 1 10 6.3 COc1nn2cc(-c3cc4c(OCc5csc(-c6ccc(C(=O)NCC(F)(F)F)cc6)n5)cc(F)cc4o3)nc2s1 nan
CHEMBL3717136 133786 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 603 8 1 10 6.3 COc1nn2cc(-c3cc4c(OCc5csc(-c6ccc(C(=O)NCC(F)(F)F)cc6)n5)cc(F)cc4o3)nc2s1 nan
72191819 133903 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 544 7 0 11 6.0 COc1cc(OCc2csc(C3(F)CC(C)OC(C)C3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3717571 133903 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 544 7 0 11 6.0 COc1cc(OCc2csc(C3(F)CC(C)OC(C)C3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
117981500 133941 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 545 6 0 10 5.4 COc1cc(OCc2nc(N3CCOCC3)sc2C(F)(F)F)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
CHEMBL3717688 133941 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 545 6 0 10 5.4 COc1cc(OCc2nc(N3CCOCC3)sc2C(F)(F)F)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
72191816 134148 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 516 7 0 11 5.2 COc1cc(OCc2csc(C3(F)CCOCC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3718380 134148 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 516 7 0 11 5.2 COc1cc(OCc2csc(C3(F)CCOCC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
117981520 133170 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 505 7 0 10 4.9 CCc1sc(N2CCOCC2)nc1COc1cc(OC)cc2oc(-c3cn4nc(C)ccc4n3)cc12 nan
CHEMBL3715021 133170 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 505 7 0 10 4.9 CCc1sc(N2CCOCC2)nc1COc1cc(OC)cc2oc(-c3cn4nc(C)ccc4n3)cc12 nan
117981469 133755 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 594 8 1 11 6.6 COc1cc(OCc2csc(C(O)(C3CCCCC3)C(F)(F)F)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3717034 133755 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 594 8 1 11 6.6 COc1cc(OCc2csc(C(O)(C3CCCCC3)C(F)(F)F)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
117981422 133260 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 525 7 0 11 6.0 COc1cc(OCc2csc(-c3ccc(Cl)nc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3715367 133260 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 525 7 0 11 6.0 COc1cc(OCc2csc(-c3ccc(Cl)nc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
117981412 133999 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 575 8 0 11 5.9 COc1cc(OCc2nc(-c3ccc(C(=O)N(C)C)cc3)sc2C)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3717891 133999 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 575 8 0 11 5.9 COc1cc(OCc2nc(-c3ccc(C(=O)N(C)C)cc3)sc2C)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
117981504 134221 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 493 6 0 9 6.0 COc1cc(OCc2csc(-c3ccc(C#N)cc3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
CHEMBL3718629 134221 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 493 6 0 9 6.0 COc1cc(OCc2csc(-c3ccc(C#N)cc3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
117981546 134417 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 552 7 0 10 5.8 COc1cc(OCc2csc(N3CCN(c4ccccc4)CC3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
CHEMBL3719271 134417 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 552 7 0 10 5.8 COc1cc(OCc2csc(N3CCN(c4ccccc4)CC3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
86700918 133849 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 468 6 0 8 6.2 COc1cc(OCc2csc(-c3ccccc3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
CHEMBL3717386 133849 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 468 6 0 8 6.2 COc1cc(OCc2csc(-c3ccccc3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
117981512 134401 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 554 8 0 10 6.5 COc1cc(OCc2nc(-c3cccc(COC(C)=O)c3)sc2C)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
CHEMBL3719230 134401 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 554 8 0 10 6.5 COc1cc(OCc2nc(-c3cccc(COC(C)=O)c3)sc2C)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
117981594 134048 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 615 11 0 11 6.8 CCN(CC1CC1)C(=O)c1ccc(-c2nc(COc3cc(OC)cc4oc(-c5cn6nc(OC)sc6n5)cc34)cs2)cc1 nan
CHEMBL3718074 134048 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 615 11 0 11 6.8 CCN(CC1CC1)C(=O)c1ccc(-c2nc(COc3cc(OC)cc4oc(-c5cn6nc(OC)sc6n5)cc34)cs2)cc1 nan
72189344 134395 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 629 9 1 11 6.5 COc1cc(OCc2nc(-c3ccc(C(=O)NCC(F)(F)F)cc3)sc2C)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3719217 134395 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 629 9 1 11 6.5 COc1cc(OCc2nc(-c3ccc(C(=O)NCC(F)(F)F)cc3)sc2C)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72191201 133106 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 601 8 0 11 6.3 COc1cc(OCc2csc(C3CCN(C(=O)c4ccccc4)CC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3714816 133106 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 601 8 0 11 6.3 COc1cc(OCc2csc(C3CCN(C(=O)c4ccccc4)CC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
117981399 133134 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 531 7 0 12 3.8 COc1cc(OCc2csc(N3CC[S+]([O-])CC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3714921 133134 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 531 7 0 12 3.8 COc1cc(OCc2csc(N3CC[S+]([O-])CC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72192723 133355 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 548 7 1 11 5.7 COc1cc(OCc2csc(C3(O)CCC(F)(F)CC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3715693 133355 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 548 7 1 11 5.7 COc1cc(OCc2csc(C3(O)CCC(F)(F)CC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
117981411 133194 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 561 8 0 11 5.6 COc1cc(OCc2csc(-c3cccc(C(=O)N(C)C)c3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3715093 133194 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 561 8 0 11 5.6 COc1cc(OCc2csc(-c3cccc(C(=O)N(C)C)c3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
117981506 134003 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 540 8 0 10 6.2 COc1cc(OCc2csc(-c3ccc(COC(C)=O)cc3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
CHEMBL3717915 134003 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 540 8 0 10 6.2 COc1cc(OCc2csc(-c3ccc(COC(C)=O)cc3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
72189639 133229 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 561 8 1 11 5.6 CNC(=O)c1ccc(-c2nc(COc3cc(OC)cc4oc(-c5cn6nc(OC)sc6n5)cc34)c(C)s2)cc1 nan
CHEMBL3715215 133229 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 561 8 1 11 5.6 CNC(=O)c1ccc(-c2nc(COc3cc(OC)cc4oc(-c5cn6nc(OC)sc6n5)cc34)c(C)s2)cc1 nan
89873167 133388 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 594 8 0 11 6.6 COc1cc(OCc2csc(C3(c4ccc(Cl)cc4)CCOC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3715798 133388 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 594 8 0 11 6.6 COc1cc(OCc2csc(C3(c4ccc(Cl)cc4)CCOC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
89878891 133869 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 540 8 1 11 5.4 CCC(O)(c1nc(COc2cc(OC)cc3oc(-c4cn5nc(OC)sc5n4)cc23)cs1)C(F)(F)F nan
CHEMBL3717451 133869 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 540 8 1 11 5.4 CCC(O)(c1nc(COc2cc(OC)cc3oc(-c4cn5nc(OC)sc5n4)cc23)cs1)C(F)(F)F nan
89872969 134123 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 536 6 0 8 7.2 COc1cc(OCc2csc(-c3ccc(C(F)(F)F)cc3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
CHEMBL3718293 134123 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 536 6 0 8 7.2 COc1cc(OCc2csc(-c3ccc(C(F)(F)F)cc3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
72190271 134110 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 512 7 0 11 5.5 COc1cc(OCc2nc(C3CCOCC3)sc2C)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3718272 134110 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 512 7 0 11 5.5 COc1cc(OCc2nc(C3CCOCC3)sc2C)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72190587 133772 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 598 7 0 13 5.3 COc1cc(OCc2csc(N3CCN(C(=O)OC(C)(C)C)CC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3717097 133772 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 598 7 0 13 5.3 COc1cc(OCc2csc(N3CCN(C(=O)OC(C)(C)C)CC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72193013 134176 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 609 8 1 12 5.3 COc1cc(OCc2csc(C3(O)CCC(C(=O)N4CCCC4)CC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3718490 134176 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 609 8 1 12 5.3 COc1cc(OCc2csc(C3(O)CCC(C(=O)N4CCCC4)CC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
117981423 133298 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 568 8 0 12 5.3 COc1cc(OCc2csc(-c3ccc(S(C)(=O)=O)cc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3715516 133298 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 568 8 0 12 5.3 COc1cc(OCc2csc(-c3ccc(S(C)(=O)=O)cc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
117981585 133841 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 615 8 0 11 6.9 COc1cc(OCc2csc(-c3ccc(C(=O)N4CCCCCC4)cc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3717348 133841 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 615 8 0 11 6.9 COc1cc(OCc2csc(-c3ccc(C(=O)N4CCCCCC4)cc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
89879364 133968 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 528 6 0 9 7.2 COc1nn2cc(-c3cc4c(OCc5csc(-c6ccc(Cl)cc6)n5)cc(Cl)cc4o3)nc2s1 nan
CHEMBL3717785 133968 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 528 6 0 9 7.2 COc1nn2cc(-c3cc4c(OCc5csc(-c6ccc(Cl)cc6)n5)cc(Cl)cc4o3)nc2s1 nan
72191202 133729 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 603 9 0 12 5.2 COc1cc(OCc2csc(C3CCN(S(=O)(=O)C(C)C)CC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3716956 133729 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 603 9 0 12 5.2 COc1cc(OCc2csc(C3CCN(S(=O)(=O)C(C)C)CC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
89873055 133852 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 552 7 0 9 7.1 COc1cc(OCc2csc(-c3ccc(OC(F)(F)F)cc3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
CHEMBL3717407 133852 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 552 7 0 9 7.1 COc1cc(OCc2csc(-c3ccc(OC(F)(F)F)cc3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
89873109 134091 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 518 8 0 12 5.1 C=C(c1cncnc1)c1nc(COc2cc(OC)cc3oc(-c4cn5nc(OC)sc5n4)cc23)cs1 nan
CHEMBL3718220 134091 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 518 8 0 12 5.1 C=C(c1cncnc1)c1nc(COc2cc(OC)cc3oc(-c4cn5nc(OC)sc5n4)cc23)cs1 nan
117981586 134281 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 575 9 1 11 6.1 COc1cc(OCc2csc(-c3ccc(C(=O)NC(C)C)cc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3718803 134281 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 575 9 1 11 6.1 COc1cc(OCc2csc(-c3ccc(C(=O)NC(C)C)cc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
117981416 133546 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 547 8 1 11 5.3 COc1cc(OCc2nc(-c3ccc(C(N)=O)cc3)sc2C)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3716328 133546 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 547 8 1 11 5.3 COc1cc(OCc2nc(-c3ccc(C(N)=O)cc3)sc2C)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72189040 133537 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 589 8 1 11 6.5 COc1cc(OCc2csc(-c3ccc(C(=O)NC(C)(C)C)cc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3716294 133537 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 589 8 1 11 6.5 COc1cc(OCc2csc(-c3ccc(C(=O)NC(C)(C)C)cc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
89872925 134409 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 589 9 0 11 6.2 CCc1sc(-c2ccc(C(=O)N(C)C)cc2)nc1COc1cc(OC)cc2oc(-c3cn4nc(OC)sc4n3)cc12 nan
CHEMBL3719253 134409 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 589 9 0 11 6.2 CCc1sc(-c2ccc(C(=O)N(C)C)cc2)nc1COc1cc(OC)cc2oc(-c3cn4nc(OC)sc4n3)cc12 nan
89879363 133684 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 515 7 0 11 5.1 COc1cc(OCc2csc(N3CCOCC3)n2)c2cc(-c3cn4nc([C@H](C)F)sc4n3)oc2c1 nan
CHEMBL3716819 133684 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 515 7 0 11 5.1 COc1cc(OCc2csc(N3CCOCC3)n2)c2cc(-c3cn4nc([C@H](C)F)sc4n3)oc2c1 nan
72193012 133990 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 556 8 2 12 4.7 COc1cc(OCc2csc(C3(O)CCC(C(=O)O)CC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3717858 133990 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 556 8 2 12 4.7 COc1cc(OCc2csc(C3(O)CCC(C(=O)O)CC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
89872960 134498 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 513 7 1 12 4.2 COc1cc(OCc2csc(C3(N)CCOCC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3714802 134498 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 513 7 1 12 4.2 COc1cc(OCc2csc(C3(N)CCOCC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3719447 134498 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 513 7 1 12 4.2 COc1cc(OCc2csc(C3(N)CCOCC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
117981599 133370 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 613 10 0 11 6.7 COc1cc(OCc2csc(-c3ccc(C(=O)N(C4CC4)C4CC4)cc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3715739 133370 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 613 10 0 11 6.7 COc1cc(OCc2csc(-c3ccc(C(=O)N(C4CC4)C4CC4)cc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72188747 133601 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 604 9 0 12 6.4 COc1cccc(C2(c3nc(COc4cc(OC)cc5oc(-c6cn7nc(OC)sc7n6)cc45)cs3)CCOCC2)c1 nan
CHEMBL3716525 133601 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 604 9 0 12 6.4 COc1cccc(C2(c3nc(COc4cc(OC)cc5oc(-c6cn7nc(OC)sc7n6)cc45)cs3)CCOCC2)c1 nan
117981470 133640 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 518 10 0 11 5.5 COCCC(C)(F)c1nc(COc2cc(OC)cc3oc(-c4cn5nc(OC)sc5n4)cc23)cs1 nan
CHEMBL3716648 133640 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 518 10 0 11 5.5 COCCC(C)(F)c1nc(COc2cc(OC)cc3oc(-c4cn5nc(OC)sc5n4)cc23)cs1 nan
72192426 134241 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 613 7 1 13 5.5 COc1cc(OCc2csc(C3(O)CCN(C(=O)OC(C)(C)C)CC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3718672 134241 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 613 7 1 13 5.5 COc1cc(OCc2csc(C3(O)CCN(C(=O)OC(C)(C)C)CC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
89878932 133568 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 533 7 0 12 4.7 COc1cc(OCc2nc(N3CCOCC3)sc2Cl)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3716402 133568 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 533 7 0 12 4.7 COc1cc(OCc2nc(N3CCOCC3)sc2Cl)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
89879306 134407 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 578 8 0 11 6.1 COc1cc(OCc2csc(C3(c4ccccc4F)CCOC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3719245 134407 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 578 8 0 11 6.1 COc1cc(OCc2csc(C3(c4ccccc4F)CCOC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72190894 133217 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 496 9 0 12 4.6 COc1cc(OCc2csc(N(C)CCC#N)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3715170 133217 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 496 9 0 12 4.6 COc1cc(OCc2csc(N(C)CCC#N)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
117981496 133862 0 None - 1 Human 9.0 pEC50 = 9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 505 6 0 10 5.1 COc1cc(OCc2csc(N3C[C@H](C)O[C@H](C)C3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
CHEMBL3717427 133862 0 None - 1 Human 9.0 pEC50 = 9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 505 6 0 10 5.1 COc1cc(OCc2csc(N3C[C@H](C)O[C@H](C)C3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
89878894 134381 0 None - 1 Human 9.0 pEC50 = 9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 603 9 0 12 5.4 COc1cc(OCc2csc(-c3ccc(C(=O)N(C)C4COC4)cc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3719156 134381 0 None - 1 Human 9.0 pEC50 = 9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 603 9 0 12 5.4 COc1cc(OCc2csc(-c3ccc(C(=O)N(C)C4COC4)cc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
86700903 133284 0 None - 1 Human 9.0 pEC50 = 9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 478 6 0 9 6.1 COc1nn2cc(-c3cc4c(OCc5csc(-c6ccccc6)n5)cc(F)cc4o3)nc2s1 nan
CHEMBL3715465 133284 0 None - 1 Human 9.0 pEC50 = 9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 478 6 0 9 6.1 COc1nn2cc(-c3cc4c(OCc5csc(-c6ccccc6)n5)cc(F)cc4o3)nc2s1 nan
117981498 133638 0 None - 1 Human 9.0 pEC50 = 9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 512 6 0 10 5.9 COc1cc(OCc2csc(-c3ccc4c(c3)OCO4)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
CHEMBL3716644 133638 0 None - 1 Human 9.0 pEC50 = 9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 512 6 0 10 5.9 COc1cc(OCc2csc(-c3ccc4c(c3)OCO4)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
89878646 133753 0 None - 1 Human 9.0 pEC50 = 9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 520 8 0 11 5.9 COc1cc(OCc2csc(-c3ccccc3OC)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3717028 133753 0 None - 1 Human 9.0 pEC50 = 9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 520 8 0 11 5.9 COc1cc(OCc2csc(-c3ccccc3OC)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
117981420 133997 0 None - 1 Human 9.0 pEC50 = 9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 534 8 1 11 5.7 COc1cc(OCc2nc(-c3cccc(CO)c3)sc2C)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3717885 133997 0 None - 1 Human 9.0 pEC50 = 9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 534 8 1 11 5.7 COc1cc(OCc2nc(-c3cccc(CO)c3)sc2C)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
117981587 134351 0 None - 1 Human 9.0 pEC50 = 9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 615 9 1 11 6.2 COc1cc(OCc2csc(-c3ccc(C(=O)NCC(F)(F)F)cc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3719060 134351 0 None - 1 Human 9.0 pEC50 = 9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 615 9 1 11 6.2 COc1cc(OCc2csc(-c3ccc(C(=O)NCC(F)(F)F)cc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72193329 133238 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 490 7 0 10 5.9 COc1cc(OCc2nc(-c3ccccc3)cs2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3715264 133238 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 490 7 0 10 5.9 COc1cc(OCc2nc(-c3ccccc3)cs2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
89879362 133244 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 560 7 0 10 7.0 COc1cc(OCc2csc(C3(F)CC(C)OC(C)C3)n2)c2cc(-c3cn4nc([C@H](C)F)sc4n3)oc2c1 nan
CHEMBL3715289 133244 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 560 7 0 10 7.0 COc1cc(OCc2csc(C3(F)CC(C)OC(C)C3)n2)c2cc(-c3cn4nc([C@H](C)F)sc4n3)oc2c1 nan
89872882 133367 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 594 8 0 11 6.6 COc1cc(OCc2csc(C3(c4cccc(Cl)c4)CCOC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3715726 133367 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 594 8 0 11 6.6 COc1cc(OCc2csc(C3(c4cccc(Cl)c4)CCOC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72193335 133608 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 608 8 0 11 7.0 COc1cc(OCc2csc(C3(c4ccc(Cl)cc4)CCOCC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3716551 133608 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 608 8 0 11 7.0 COc1cc(OCc2csc(C3(c4ccc(Cl)cc4)CCOCC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72189640 133685 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 504 7 0 10 6.5 COc1cc(OC(C)c2csc(-c3ccccc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3716823 133685 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 504 7 0 10 6.5 COc1cc(OC(C)c2csc(-c3ccccc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
89878649 133762 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 558 7 0 10 6.9 COc1cc(OCc2csc(-c3cccc(C(F)(F)F)c3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3717068 133762 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 558 7 0 10 6.9 COc1cc(OCc2csc(-c3cccc(C(F)(F)F)c3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
117981569 133847 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 587 7 0 11 5.9 COc1cc(OCc2csc(N3CCN(c4cccc(Cl)n4)CC3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
CHEMBL3717364 133847 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 587 7 0 11 5.9 COc1cc(OCc2csc(N3CCN(c4cccc(Cl)n4)CC3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
72189641 134005 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 524 7 0 10 6.6 COc1cc(OCc2nc(-c3ccccc3)sc2Cl)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3717923 134005 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 524 7 0 10 6.6 COc1cc(OCc2nc(-c3ccccc3)sc2Cl)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
117981561 134140 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 491 6 0 10 4.7 COc1cc(OCc2csc(N3CCOC(C)C3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
CHEMBL3718352 134140 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 491 6 0 10 4.7 COc1cc(OCc2csc(N3CCOC(C)C3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
89878660 134404 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 496 7 0 10 6.3 COc1cc(OCc2csc(C3CCCCC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3719238 134404 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 496 7 0 10 6.3 COc1cc(OCc2csc(C3CCCCC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
89878695 134430 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 526 7 0 10 6.2 COc1cc(OCc2csc(-c3ccc(F)cc3F)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3719316 134430 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 526 7 0 10 6.2 COc1cc(OCc2csc(-c3ccc(F)cc3F)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72191199 133214 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 597 8 1 11 7.1 COc1cc(OCc2csc(Nc3ccc(Br)cc3C)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3715161 133214 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 597 8 1 11 7.1 COc1cc(OCc2csc(Nc3ccc(Br)cc3C)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
117981572 133292 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 573 8 0 11 5.8 COc1cc(OCc2csc(-c3ccc(C(=O)N4CCC4)cc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3715492 133292 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 573 8 0 11 5.8 COc1cc(OCc2csc(-c3ccc(C(=O)N4CCC4)cc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
117981494 133379 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 498 7 0 9 6.2 COc1ccc(-c2nc(COc3cc(OC)cc4oc(-c5cn6nc(C)ccc6n5)cc34)cs2)cc1 nan
CHEMBL3715762 133379 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 498 7 0 9 6.2 COc1ccc(-c2nc(COc3cc(OC)cc4oc(-c5cn6nc(C)ccc6n5)cc34)cs2)cc1 nan
117981547 133618 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 553 7 0 11 5.2 COc1cc(OCc2csc(N3CCN(c4ccccn4)CC3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
CHEMBL3716572 133618 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 553 7 0 11 5.2 COc1cc(OCc2csc(N3CCN(c4ccccn4)CC3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
89872881 133664 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 502 6 0 8 6.8 COc1cc(OCc2csc(-c3ccc(Cl)cc3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
CHEMBL3716754 133664 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 502 6 0 8 6.8 COc1cc(OCc2csc(-c3ccc(Cl)cc3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
72192724 133751 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 550 7 0 10 6.6 COc1cc(OCc2csc(C3(F)CCC(F)(F)CC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3717023 133751 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 550 7 0 10 6.6 COc1cc(OCc2csc(C3(F)CCC(F)(F)CC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
117981460 133815 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 588 8 1 11 6.1 COc1cc(OCc2csc(C(O)(c3ccccc3)C(F)(F)F)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3717259 133815 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 588 8 1 11 6.1 COc1cc(OCc2csc(C(O)(c3ccccc3)C(F)(F)F)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
117981588 133853 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 561 9 1 11 5.7 CCNC(=O)c1ccc(-c2nc(COc3cc(OC)cc4oc(-c5cn6nc(OC)sc6n5)cc34)cs2)cc1 nan
CHEMBL3717411 133853 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 561 9 1 11 5.7 CCNC(=O)c1ccc(-c2nc(COc3cc(OC)cc4oc(-c5cn6nc(OC)sc6n5)cc34)cs2)cc1 nan
89878701 133970 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 414 6 0 10 4.3 COc1cc(OCc2cscn2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3717789 133970 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 414 6 0 10 4.3 COc1cc(OCc2cscn2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
117981501 133980 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 526 7 0 10 6.1 COc1cc(OCc2csc(-c3cccc(OC(C)=O)c3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
CHEMBL3717814 133980 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 526 7 0 10 6.1 COc1cc(OCc2csc(-c3cccc(OC(C)=O)c3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
72192722 134297 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 514 7 0 10 6.4 COc1cc(OCc2csc(C3(F)CCCCC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3718840 134297 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 514 7 0 10 6.4 COc1cc(OCc2csc(C3(F)CCCCC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
117981523 134312 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 572 7 0 9 6.9 COc1cc(OCc2csc(C3(c4ccc(Cl)cc4)CCOC3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
CHEMBL3718885 134312 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 572 7 0 9 6.9 COc1cc(OCc2csc(C3(c4ccc(Cl)cc4)CCOC3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
89878655 134356 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 498 7 0 11 5.2 COc1cc(OCc2csc(C3CCOCC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3719069 134356 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 498 7 0 11 5.2 COc1cc(OCc2csc(C3CCOCC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72189342 133113 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 604 8 0 12 7.2 COc1cc(OCc2nc(-c3ccc(C(=O)OC(C)(C)C)cc3)sc2C)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3714836 133113 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 604 8 0 12 7.2 COc1cc(OCc2nc(-c3ccc(C(=O)OC(C)(C)C)cc3)sc2C)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
89873006 133206 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 574 8 0 11 6.3 COc1cc(OCc2csc(C3(c4ccc(C)cc4)CCOC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3715137 133206 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 574 8 0 11 6.3 COc1cc(OCc2csc(C3(c4ccc(C)cc4)CCOC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
89872908 133343 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 566 8 0 10 7.2 COc1cc(OCc2csc(C(C)(C)c3ccc(Cl)cc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3715659 133343 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 566 8 0 10 7.2 COc1cc(OCc2csc(C(C)(C)c3ccc(Cl)cc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
89878647 133396 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 492 7 0 12 4.7 COc1cc(OCc2csc(-c3cnccn3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3715839 133396 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 492 7 0 12 4.7 COc1cc(OCc2csc(-c3cnccn3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
117981597 133428 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 573 9 1 11 5.8 COc1cc(OCc2csc(-c3ccc(C(=O)NC4CC4)cc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3715947 133428 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 573 9 1 11 5.8 COc1cc(OCc2csc(-c3ccc(C(=O)NC4CC4)cc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
89878642 133487 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 494 6 0 8 7.1 C[C@H](F)c1nn2cc(-c3cc4c(OCc5csc(-c6ccccc6)n5)cc(F)cc4o3)nc2s1 nan
CHEMBL3716150 133487 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 494 6 0 8 7.1 C[C@H](F)c1nn2cc(-c3cc4c(OCc5csc(-c6ccccc6)n5)cc(F)cc4o3)nc2s1 nan
89873018 133592 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 544 7 0 11 6.1 COc1cc(OCc2csc(C3=CCOc4ccccc43)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3716498 133592 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 544 7 0 11 6.1 COc1cc(OCc2csc(C3=CCOc4ccccc43)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72190895 133605 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 527 9 0 12 4.9 COC[C@@H]1CCCN1c1nc(COc2cc(OC)cc3oc(-c4cn5nc(OC)sc5n4)cc23)cs1 nan
CHEMBL3716539 133605 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 527 9 0 12 4.9 COC[C@@H]1CCCN1c1nc(COc2cc(OC)cc3oc(-c4cn5nc(OC)sc5n4)cc23)cs1 nan
89878650 133652 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 504 7 0 10 6.2 COc1cc(OCc2csc(-c3cccc(C)c3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3716709 133652 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 504 7 0 10 6.2 COc1cc(OCc2csc(-c3cccc(C)c3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
89878700 133882 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 492 6 0 10 5.0 COc1cc(OCc2csc(Br)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3717486 133882 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 492 6 0 10 5.0 COc1cc(OCc2csc(Br)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
89878692 134094 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 558 7 0 10 6.9 COc1cc(OCc2csc(-c3ccc(C(F)(F)F)cc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3718231 134094 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 558 7 0 10 6.9 COc1cc(OCc2csc(-c3ccc(C(F)(F)F)cc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
89872977 134184 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 508 6 0 9 6.9 COc1nn2cc(-c3cc4c(OCc5csc(-c6cccc(C)c6)n5)cc(Cl)cc4o3)nc2s1 nan
CHEMBL3718509 134184 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 508 6 0 9 6.9 COc1nn2cc(-c3cc4c(OCc5csc(-c6cccc(C)c6)n5)cc(Cl)cc4o3)nc2s1 nan
117981556 134274 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 503 7 0 9 6.1 CCC1CCN(c2nc(COc3cc(OC)cc4oc(-c5cn6nc(C)ccc6n5)cc34)cs2)CC1 nan
CHEMBL3718781 134274 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 503 7 0 9 6.1 CCC1CCN(c2nc(COc3cc(OC)cc4oc(-c5cn6nc(C)ccc6n5)cc34)cs2)CC1 nan
117981513 134369 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 512 7 1 9 6.0 COc1cc(OCc2nc(-c3cccc(CO)c3)sc2C)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
CHEMBL3719105 134369 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 512 7 1 9 6.0 COc1cc(OCc2nc(-c3cccc(CO)c3)sc2C)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
117981562 133369 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 501 6 0 9 5.9 COc1cc(OCc2csc(N3CCC4(CC3)CC4)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
CHEMBL3715736 133369 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 501 6 0 9 5.9 COc1cc(OCc2csc(N3CCC4(CC3)CC4)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
89873113 133975 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 532 8 0 10 6.6 COc1cc(OCc2csc(C(C)(C)c3ccccc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3717802 133975 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 532 8 0 10 6.6 COc1cc(OCc2csc(C(C)(C)c3ccccc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
89878699 134265 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 574 8 0 11 6.8 COc1cc(OCc2csc(-c3ccc(OC(F)(F)F)cc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3718755 134265 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 574 8 0 11 6.8 COc1cc(OCc2csc(-c3ccc(OC(F)(F)F)cc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
117981529 134387 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 523 12 0 11 4.6 COCCN(CCOC)c1nc(COc2cc(OC)cc3oc(-c4cn5nc(C)ccc5n4)cc23)cs1 nan
CHEMBL3719181 134387 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 523 12 0 11 4.6 COCCN(CCOC)c1nc(COc2cc(OC)cc3oc(-c4cn5nc(C)ccc5n4)cc23)cs1 nan
72193331 133908 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 491 7 0 11 5.3 COc1cc(OCc2nsc(-c3ccccc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3717580 133908 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 491 7 0 11 5.3 COc1cc(OCc2nsc(-c3ccccc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
117981598 133311 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 615 8 0 11 6.9 COc1cc(OCc2csc(-c3ccc(C(=O)N4C(C)CCC4C)cc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3715559 133311 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 615 8 0 11 6.9 COc1cc(OCc2csc(-c3ccc(C(=O)N4C(C)CCC4C)cc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
86700913 133472 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 494 6 0 9 6.6 COc1nn2cc(-c3cc4c(OCc5csc(-c6ccccc6)n5)cc(Cl)cc4o3)nc2s1 nan
CHEMBL3716103 133472 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 494 6 0 9 6.6 COc1nn2cc(-c3cc4c(OCc5csc(-c6ccccc6)n5)cc(Cl)cc4o3)nc2s1 nan
89878654 133716 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 524 7 0 10 6.6 COc1cc(OCc2csc(-c3ccc(Cl)cc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3716917 133716 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 524 7 0 10 6.6 COc1cc(OCc2csc(-c3ccc(Cl)cc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
89878893 133797 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 577 8 0 10 6.6 COc1cc(OCc2csc(-c3ccc(C(=O)N(C)C)cc3)n2)c2cc(-c3cn4nc([C@H](C)F)sc4n3)oc2c1 nan
CHEMBL3717182 133797 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 577 8 0 10 6.6 COc1cc(OCc2csc(-c3ccc(C(=O)N(C)C)cc3)n2)c2cc(-c3cn4nc([C@H](C)F)sc4n3)oc2c1 nan
127024445 133834 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 554 7 0 12 5.7 COc1cc(OCc2csc(C3CCC4(CC3)OCCO4)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3717332 133834 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 554 7 0 12 5.7 COc1cc(OCc2csc(C3CCC4(CC3)OCCO4)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
117981552 133156 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 586 7 0 10 6.5 COc1cc(OCc2csc(N3CCN(c4cccc(Cl)c4)CC3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
CHEMBL3714991 133156 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 586 7 0 10 6.5 COc1cc(OCc2csc(N3CCN(c4cccc(Cl)c4)CC3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
117981540 133252 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 449 7 1 9 5.3 COc1cc(OCc2csc(NC(C)C)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
CHEMBL3715333 133252 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 449 7 1 9 5.3 COc1cc(OCc2csc(NC(C)C)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
89878640 133317 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 495 7 0 12 5.2 COc1cc(OCc2csc(-c3cc(C)on3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3715578 133317 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 495 7 0 12 5.2 COc1cc(OCc2csc(-c3cc(C)on3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
89872998 133670 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 617 9 1 13 5.3 COc1cc(OCc2csc(C3(N[S@+]([O-])C(C)(C)C)CCOCC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3716780 133670 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 617 9 1 13 5.3 COc1cc(OCc2csc(C3(N[S@+]([O-])C(C)(C)C)CCOCC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72193334 134138 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 652 8 0 11 7.1 COc1cc(OCc2csc(C3(c4ccc(Br)cc4)CCOCC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3718346 134138 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 652 8 0 11 7.1 COc1cc(OCc2csc(C3(c4ccc(Br)cc4)CCOCC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
117981514 133305 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 483 6 0 9 5.9 COc1cc(OCc2csc(-c3ccc(C)nc3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
CHEMBL3715545 133305 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 483 6 0 9 5.9 COc1cc(OCc2csc(-c3ccc(C)nc3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
72193009 133335 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 428 6 0 10 4.6 COc1cc(OCc2csc(C)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3715642 133335 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 428 6 0 10 4.6 COc1cc(OCc2csc(C)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
89878697 133902 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 508 7 0 10 6.1 COc1cc(OCc2csc(-c3ccccc3F)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3717567 133902 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 508 7 0 10 6.1 COc1cc(OCc2csc(-c3ccccc3F)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
117981518 133095 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 554 7 0 11 3.6 COc1cc(OCc2csc(N3CCN(S(C)(=O)=O)CC3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
CHEMBL3714777 133095 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 554 7 0 11 3.6 COc1cc(OCc2csc(N3CCN(S(C)(=O)=O)CC3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
89872701 133349 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 506 7 0 9 6.9 COc1cc(OCc2csc(-c3ccccc3)n2)c2cc(-c3cn4nc([C@H](C)F)sc4n3)oc2c1 nan
CHEMBL3715685 133349 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 506 7 0 9 6.9 COc1cc(OCc2csc(-c3ccccc3)n2)c2cc(-c3cn4nc([C@H](C)F)sc4n3)oc2c1 nan
72192429 133854 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 584 7 0 11 6.3 COc1cc(OCc2nc(C3(F)CCOCC3)sc2C(F)(F)F)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3717413 133854 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 584 7 0 11 6.3 COc1cc(OCc2nc(C3(F)CCOCC3)sc2C(F)(F)F)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
117981537 133503 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 465 9 1 10 4.6 COCCNc1nc(COc2cc(OC)cc3oc(-c4cn5nc(C)ccc5n4)cc23)cs1 nan
CHEMBL3716189 133503 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 465 9 1 10 4.6 COCCNc1nc(COc2cc(OC)cc3oc(-c4cn5nc(C)ccc5n4)cc23)cs1 nan
117981570 134135 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 560 7 0 11 4.8 COc1cc(OCc2csc(N3CCN(C4CCOCC4)CC3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
CHEMBL3718335 134135 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 560 7 0 11 4.8 COc1cc(OCc2csc(N3CCN(C4CCOCC4)CC3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
89873126 133493 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 426 5 0 8 5.1 COc1cc(OCc2csc(Cl)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
CHEMBL3716164 133493 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 426 5 0 8 5.1 COc1cc(OCc2csc(Cl)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
117981532 133600 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 465 8 1 10 3.9 COc1cc(OCc2csc(N(C)CCO)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
CHEMBL3716524 133600 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 465 8 1 10 3.9 COc1cc(OCc2csc(N(C)CCO)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
117981550 134101 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 515 7 1 9 6.7 COc1cc(OCc2csc(Nc3cc(C)ccc3F)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
CHEMBL3718248 134101 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 515 7 1 9 6.7 COc1cc(OCc2csc(Nc3cc(C)ccc3F)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
117981539 134018 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 532 10 1 10 4.9 COc1cc(OCc2csc(NCCCN3CCCC3=O)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
CHEMBL3717970 134018 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 532 10 1 10 4.9 COc1cc(OCc2csc(NCCCN3CCCC3=O)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
117981558 133522 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 493 6 0 9 5.4 COc1cc(OCc2csc(N3CCC(F)CC3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
CHEMBL3716259 133522 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 493 6 0 9 5.4 COc1cc(OCc2csc(N3CCC(F)CC3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
89878653 134304 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 504 7 0 10 6.2 COc1cc(OCc2nc(-c3ccccc3)sc2C)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3718860 134304 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 504 7 0 10 6.2 COc1cc(OCc2nc(-c3ccccc3)sc2C)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
117981580 134058 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 587 10 0 11 6.2 C=CCN(C)C(=O)c1ccc(-c2nc(COc3cc(OC)cc4oc(-c5cn6nc(OC)sc6n5)cc34)cs2)cc1 nan
CHEMBL3718108 134058 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 587 10 0 11 6.2 C=CCN(C)C(=O)c1ccc(-c2nc(COc3cc(OC)cc4oc(-c5cn6nc(OC)sc6n5)cc34)cs2)cc1 nan
117981410 133300 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 515 7 0 11 5.8 COc1cc(OCc2csc(-c3ccc(C#N)cc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3715528 133300 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 515 7 0 11 5.8 COc1cc(OCc2csc(-c3ccc(C#N)cc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72190590 133799 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 604 9 0 13 4.1 COc1cc(OCc2csc(N3CCN(S(=O)(=O)C(C)C)CC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3717188 133799 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 604 9 0 13 4.1 COc1cc(OCc2csc(N3CCN(S(=O)(=O)C(C)C)CC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72189343 133698 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 548 8 1 11 5.9 COc1cc(OCc2nc(-c3ccc(C(=O)O)cc3)sc2C)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3716864 133698 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 548 8 1 11 5.9 COc1cc(OCc2nc(-c3ccc(C(=O)O)cc3)sc2C)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
89878661 133323 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 520 8 0 11 5.9 COc1ccc(-c2nc(COc3cc(OC)cc4oc(-c5cn6nc(OC)sc6n5)cc34)cs2)cc1 nan
CHEMBL3715600 133323 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 520 8 0 11 5.9 COc1ccc(-c2nc(COc3cc(OC)cc4oc(-c5cn6nc(OC)sc6n5)cc34)cs2)cc1 nan
72188745 133800 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 548 8 1 11 6.2 COc1cc(OCc2csc(-c3ccc(C(C)(C)O)cc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3717195 133800 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 548 8 1 11 6.2 COc1cc(OCc2csc(-c3ccc(C(C)(C)O)cc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
117981553 134170 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 540 9 1 10 6.2 COc1cc(OCc2csc(NCc3cccc(N(C)C)c3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
CHEMBL3718462 134170 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 540 9 1 10 6.2 COc1cc(OCc2csc(NCc3cccc(N(C)C)c3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
89873035 134325 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 603 9 0 11 6.7 COc1cc(OCc2nc(-c3ccc(C(=O)N(C)C)cc3)sc2C(C)C)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3718970 134325 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 603 9 0 11 6.7 COc1cc(OCc2nc(-c3ccc(C(=O)N(C)C)cc3)sc2C(C)C)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
86700915 133896 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 460 6 0 9 5.9 COc1nn2cc(-c3cc4c(OCc5csc(-c6ccccc6)n5)cccc4o3)nc2s1 nan
CHEMBL3717546 133896 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 460 6 0 9 5.9 COc1nn2cc(-c3cc4c(OCc5csc(-c6ccccc6)n5)cccc4o3)nc2s1 nan
117981421 133929 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 521 8 0 12 5.3 COc1cncc(-c2nc(COc3cc(OC)cc4oc(-c5cn6nc(OC)sc6n5)cc34)cs2)c1 nan
CHEMBL3717642 133929 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 521 8 0 12 5.3 COc1cncc(-c2nc(COc3cc(OC)cc4oc(-c5cn6nc(OC)sc6n5)cc34)cs2)c1 nan
117981515 134045 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 503 6 0 9 6.2 COc1cc(OCc2csc(-c3ccc(Cl)nc3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
CHEMBL3718063 134045 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 503 6 0 9 6.2 COc1cc(OCc2csc(-c3ccc(Cl)nc3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
72189945 133102 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 527 8 0 13 3.9 COc1cc(OCc2nc(N3CCOCC3)sc2C=O)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3714807 133102 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 527 8 0 13 3.9 COc1cc(OCc2nc(N3CCOCC3)sc2C=O)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
117981566 133354 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 567 7 0 11 5.5 COc1cc(OCc2csc(N3CCN(c4ccc(C)cn4)CC3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
CHEMBL3715692 133354 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 567 7 0 11 5.5 COc1cc(OCc2csc(N3CCN(c4ccc(C)cn4)CC3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
117981568 134069 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 513 8 1 10 6.2 COc1cccc(Nc2nc(COc3cc(OC)cc4oc(-c5cn6nc(C)ccc6n5)cc34)cs2)c1 nan
CHEMBL3718142 134069 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 513 8 1 10 6.2 COc1cccc(Nc2nc(COc3cc(OC)cc4oc(-c5cn6nc(C)ccc6n5)cc34)cs2)c1 nan
117981548 134258 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 512 7 1 10 6.3 COc1cc(OCc2csc(Nc3cc(C)cc(C)n3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
CHEMBL3718733 134258 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 512 7 1 10 6.3 COc1cc(OCc2csc(Nc3cc(C)cc(C)n3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
89872988 133521 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 598 10 1 13 3.9 COc1cc(OCc2csc(C3(NC(=O)CN(C)C)CCOCC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3716255 133521 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 598 10 1 13 3.9 COc1cc(OCc2csc(C3(NC(=O)CN(C)C)CCOCC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
117981589 133597 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 604 11 1 12 5.2 COc1cc(OCc2csc(-c3ccc(C(=O)NCCN(C)C)cc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3716517 133597 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 604 11 1 12 5.2 COc1cc(OCc2csc(-c3ccc(C(=O)NCCN(C)C)cc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
117981560 133891 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 504 6 0 10 4.6 COc1cc(OCc2csc(N3CCN(C)C(C)C3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
CHEMBL3717527 133891 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 504 6 0 10 4.6 COc1cc(OCc2csc(N3CCN(C)C(C)C3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
72189643 134314 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 443 6 1 11 4.1 COc1cc(OCc2nc(N)sc2C)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3718893 134314 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 443 6 1 11 4.1 COc1cc(OCc2nc(N)sc2C)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
117981531 133545 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 526 8 1 10 6.3 COc1cc(OCc2csc(Nc3cccc(N(C)C)c3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
CHEMBL3716324 133545 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 526 8 1 10 6.3 COc1cc(OCc2csc(Nc3cccc(N(C)C)c3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
117981495 134008 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 477 6 0 10 4.3 COc1cc(OCc2csc(N3CCOCC3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
CHEMBL3717931 134008 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 477 6 0 10 4.3 COc1cc(OCc2csc(N3CCOCC3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
89878641 133150 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 524 7 0 10 6.6 COc1cc(OCc2csc(-c3ccccc3Cl)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3714977 133150 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 524 7 0 10 6.6 COc1cc(OCc2csc(-c3ccccc3Cl)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
117981557 133749 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 475 6 0 9 5.5 COc1cc(OCc2csc(N3CCC[C@@H]3C)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
CHEMBL3717011 133749 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 475 6 0 9 5.5 COc1cc(OCc2csc(N3CCC[C@@H]3C)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
89873106 133350 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 470 5 0 8 5.3 COc1cc(OCc2csc(Br)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
CHEMBL3715686 133350 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 470 5 0 8 5.3 COc1cc(OCc2csc(Br)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
72188742 133368 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 474 7 0 11 4.4 COc1cc(OCc2cnnn2-c2ccccc2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3715728 133368 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 474 7 0 11 4.4 COc1cc(OCc2cnnn2-c2ccccc2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
117981519 133575 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 641 8 0 12 4.9 COc1cc(OCc2csc(N3CCN(S(=O)(=O)c4ccc(C#N)cc4)CC3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
CHEMBL3716435 133575 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 641 8 0 12 4.9 COc1cc(OCc2csc(N3CCN(S(=O)(=O)c4ccc(C#N)cc4)CC3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
89872952 133829 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 588 8 0 11 6.7 COc1cc(OCc2csc(C3(c4ccc(C)cc4)CCOCC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3717319 133829 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 588 8 0 11 6.7 COc1cc(OCc2csc(C3(c4ccc(C)cc4)CCOCC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
117981533 133833 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 474 8 0 10 4.8 COc1cc(OCc2csc(N(C)CCC#N)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
CHEMBL3717327 133833 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 474 8 0 10 4.8 COc1cc(OCc2csc(N(C)CCC#N)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
117981493 134357 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 476 6 0 9 5.4 COc1cc(OCc2csc(C3CCOCC3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
CHEMBL3719070 134357 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 476 6 0 9 5.4 COc1cc(OCc2csc(C3CCOCC3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
72193332 134375 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 491 7 0 11 5.3 COc1cc(OCc2nnc(-c3ccccc3)s2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3719133 134375 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 491 7 0 11 5.3 COc1cc(OCc2nnc(-c3ccccc3)s2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
117981526 133177 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 520 8 1 11 3.6 COc1cc(OCc2csc(N3CCN(CCO)CC3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
CHEMBL3715042 133177 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 520 8 1 11 3.6 COc1cc(OCc2csc(N3CCN(CCO)CC3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
117981567 133253 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 516 7 1 10 6.1 COc1cc(OCc2csc(Nc3ccc(F)c(C)n3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
CHEMBL3715336 133253 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 516 7 1 10 6.1 COc1cc(OCc2csc(Nc3ccc(F)c(C)n3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
117981545 133646 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 522 7 2 9 6.7 COc1cc(OCc2csc(Nc3ccc4[nH]ccc4c3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
CHEMBL3716687 133646 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 522 7 2 9 6.7 COc1cc(OCc2csc(Nc3ccc4[nH]ccc4c3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
72193011 134384 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 612 8 1 13 6.0 COc1cc(OCc2csc(C3(O)CCC(C(=O)OC(C)(C)C)CC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3719172 134384 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 612 8 1 13 6.0 COc1cc(OCc2csc(C3(O)CCC(C(=O)OC(C)(C)C)CC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
117981559 134031 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 475 6 0 9 5.5 COc1cc(OCc2csc(N3CCC[C@H]3C)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
CHEMBL3718007 134031 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 475 6 0 9 5.5 COc1cc(OCc2csc(N3CCC[C@H]3C)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
117981551 134416 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 497 7 1 9 6.5 COc1cc(OCc2csc(Nc3cccc(C)c3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
CHEMBL3719267 134416 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 497 7 1 9 6.5 COc1cc(OCc2csc(Nc3cccc(C)c3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
89873029 133925 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 495 6 0 9 6.4 CC(F)(F)c1nn2cc(-c3cc4c(OCc5csc(-c6ccccc6)n5)nccc4o3)nc2s1 nan
CHEMBL3717633 133925 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 495 6 0 9 6.4 CC(F)(F)c1nn2cc(-c3cc4c(OCc5csc(-c6ccccc6)n5)nccc4o3)nc2s1 nan
117981549 133248 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 519 7 1 9 6.5 COc1cc(OCc2csc(Nc3cc(F)ccc3F)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
CHEMBL3715312 133248 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 519 7 1 9 6.5 COc1cc(OCc2csc(Nc3cc(F)ccc3F)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
72193333 134339 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 474 7 0 11 4.4 COc1cc(OCc2cn(-c3ccccc3)nn2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3719018 134339 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 474 7 0 11 4.4 COc1cc(OCc2cn(-c3ccccc3)nn2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
117981528 133892 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 498 8 1 10 5.5 COc1cc(OCc2csc(NCc3cccnc3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
CHEMBL3717529 133892 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 498 8 1 10 5.5 COc1cc(OCc2csc(NCc3cccnc3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
117981554 133549 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 567 8 0 11 5.2 COc1cc(OCc2csc(N3CCN(Cc4cccnc4)CC3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
CHEMBL3716336 133549 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 567 8 0 11 5.2 COc1cc(OCc2csc(N3CCN(Cc4cccnc4)CC3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
117981555 133497 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 560 7 0 11 4.8 COc1cc(OCc2csc(N3CCC(N4CCOCC4)CC3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
CHEMBL3716173 133497 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 560 7 0 11 4.8 COc1cc(OCc2csc(N3CCC(N4CCOCC4)CC3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
117981563 133604 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 463 7 0 9 5.3 COc1cc(OCc2csc(N(C)C(C)C)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
CHEMBL3716534 133604 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 463 7 0 9 5.3 COc1cc(OCc2csc(N(C)C(C)C)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
117981522 133138 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 586 7 0 9 7.2 COc1cc(OCc2csc(C3(c4cccc(Cl)c4)CCOCC3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
CHEMBL3714932 133138 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 586 7 0 9 7.2 COc1cc(OCc2csc(C3(c4cccc(Cl)c4)CCOCC3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
117981543 134134 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 508 7 1 10 6.1 COc1cc(OCc2csc(Nc3cccc(C#N)c3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
CHEMBL3718333 134134 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 508 7 1 10 6.1 COc1cc(OCc2csc(Nc3cccc(C#N)c3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
117981564 133455 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 435 6 0 9 4.6 COc1cc(OCc2csc(N(C)C)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
CHEMBL3716037 133455 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 435 6 0 9 4.6 COc1cc(OCc2csc(N(C)C)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
117981542 133263 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 447 6 0 9 4.7 COc1cc(OCc2csc(N3CCC3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
CHEMBL3715374 133263 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 447 6 0 9 4.7 COc1cc(OCc2csc(N3CCC3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
89873207 133359 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 490 6 0 10 4.2 COc1cc(OCc2csc(N3CCN(C)CC3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
CHEMBL3715711 133359 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 490 6 0 10 4.2 COc1cc(OCc2csc(N3CCN(C)CC3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
117981541 134448 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 491 8 1 10 5.1 COc1cc(OCc2csc(NCC3CCCO3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
CHEMBL3719385 134448 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 491 8 1 10 5.1 COc1cc(OCc2csc(NCC3CCCO3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
117981536 133453 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 518 7 0 10 5.0 COc1cc(OCc2csc(N3CCC(N(C)C)CC3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
CHEMBL3716035 133453 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 518 7 0 10 5.0 COc1cc(OCc2csc(N3CCC(N(C)C)CC3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
117981538 133986 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 477 6 1 10 4.1 COc1cc(OCc2csc(N3CC[C@@H](O)C3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
CHEMBL3717842 133986 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 477 6 1 10 4.1 COc1cc(OCc2csc(N3CC[C@@H](O)C3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
117981527 133801 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 520 9 1 11 4.2 COc1cc(OCc2csc(NCCN3CCOCC3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
CHEMBL3717199 133801 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 520 9 1 11 4.2 COc1cc(OCc2csc(NCCN3CCOCC3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
117981579 133146 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 589 9 1 12 5.1 COc1cc(OCc2csc(-c3ccc(C(=O)NC4COC4)cc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3714962 133146 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 589 9 1 12 5.1 COc1cc(OCc2csc(-c3ccc(C(=O)NC4COC4)cc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
117981401 133514 0 None - 1 Human 9.7 pIC50 = 9.7 Functional
Antagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR methodAntagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR method
ChEMBL 513 7 0 12 4.5 COc1cc(OCc2csc(N3CCCOCC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.2c00359
CHEMBL3716230 133514 0 None - 1 Human 9.7 pIC50 = 9.7 Functional
Antagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR methodAntagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR method
ChEMBL 513 7 0 12 4.5 COc1cc(OCc2csc(N3CCCOCC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.2c00359
72191813 133165 0 None - 1 Human 9.6 pIC50 = 9.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 555 8 0 10 5.6 COc1cc(OCc2cccc(-c3ccc(C(=O)N(C)C)cc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3715013 133165 0 None - 1 Human 9.6 pIC50 = 9.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 555 8 0 10 5.6 COc1cc(OCc2cccc(-c3ccc(C(=O)N(C)C)cc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72192122 133708 0 None - 1 Human 9.6 pIC50 = 9.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 522 8 0 11 4.8 COc1cc(OCc2cccc(C3(OC)CCOCC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3716902 133708 0 None - 1 Human 9.6 pIC50 = 9.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 522 8 0 11 4.8 COc1cc(OCc2cccc(C3(OC)CCOCC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72192127 133824 0 None - 1 Human 9.5 pIC50 = 9.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 556 8 0 11 5.0 COc1cc(OCc2ccnc(-c3ccc(C(=O)N(C)C)cc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3717308 133824 0 None - 1 Human 9.5 pIC50 = 9.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 556 8 0 11 5.0 COc1cc(OCc2ccnc(-c3ccc(C(=O)N(C)C)cc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
71769562 133398 1 None - 1 Human 9.5 pIC50 = 9.5 Functional
Antagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR methodAntagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR method
ChEMBL 490 7 0 10 5.9 COc1cc(OCc2csc(-c3ccccc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.2c00359
CHEMBL3715848 133398 1 None - 1 Human 9.5 pIC50 = 9.5 Functional
Antagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR methodAntagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR method
ChEMBL 490 7 0 10 5.9 COc1cc(OCc2csc(-c3ccccc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.2c00359
89878842 133808 0 None - 1 Human 9.5 pIC50 = 9.5 Functional
Antagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR methodAntagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR method
ChEMBL 533 8 1 11 5.0 COc1cc(OCc2csc(-c3ccc(C(N)=O)cc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.2c00359
CHEMBL3717235 133808 0 None - 1 Human 9.5 pIC50 = 9.5 Functional
Antagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR methodAntagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR method
ChEMBL 533 8 1 11 5.0 COc1cc(OCc2csc(-c3ccc(C(N)=O)cc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.2c00359
72189642 134010 0 None - 1 Human 9.5 pIC50 = 9.5 Functional
Antagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR methodAntagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR method
ChEMBL 567 7 0 12 5.1 COc1cc(OCc2nc(N3CCOCC3)sc2C(F)(F)F)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.2c00359
CHEMBL3717937 134010 0 None - 1 Human 9.5 pIC50 = 9.5 Functional
Antagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR methodAntagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR method
ChEMBL 567 7 0 12 5.1 COc1cc(OCc2nc(N3CCOCC3)sc2C(F)(F)F)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.2c00359
72191505 134228 0 None - 1 Human 9.5 pIC50 = 9.5 Functional
Antagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR methodAntagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR method
ChEMBL 532 7 0 10 6.6 COc1cc(OCc2csc(C3CCC(F)(F)CC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.2c00359
CHEMBL3718639 134228 0 None - 1 Human 9.5 pIC50 = 9.5 Functional
Antagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR methodAntagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR method
ChEMBL 532 7 0 10 6.6 COc1cc(OCc2csc(C3CCC(F)(F)CC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.2c00359
72192123 134142 0 None - 1 Human 9.5 pIC50 = 9.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 526 7 0 9 6.2 COc1cc(OCc2cccc(C3(F)CCOCC3)n2)c2cc(-c3cn4nc([C@H](C)F)sc4n3)oc2c1 nan
CHEMBL3718355 134142 0 None - 1 Human 9.5 pIC50 = 9.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 526 7 0 9 6.2 COc1cc(OCc2cccc(C3(F)CCOCC3)n2)c2cc(-c3cn4nc([C@H](C)F)sc4n3)oc2c1 nan
72203402 135535 0 None - 1 Human 9.5 pIC50 = 9.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 547 9 0 9 7.0 COc1cc(OCc2cccc(OCc3cccc(Cl)c3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3732089 135535 0 None - 1 Human 9.5 pIC50 = 9.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 547 9 0 9 7.0 COc1cc(OCc2cccc(OCc3cccc(Cl)c3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72192124 133864 0 None - 1 Human 9.5 pIC50 = 9.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 510 7 0 10 5.2 COc1cc(OCc2cccc(C3(F)CCOCC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3717430 133864 0 None - 1 Human 9.5 pIC50 = 9.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 510 7 0 10 5.2 COc1cc(OCc2cccc(C3(F)CCOCC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72192125 133155 0 None - 1 Human 9.4 pIC50 = 9.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 538 8 0 10 5.9 COc1cc(OCc2cccc(C3(OC)CCOCC3)n2)c2cc(-c3cn4nc([C@H](C)F)sc4n3)oc2c1 nan
CHEMBL3714990 133155 0 None - 1 Human 9.4 pIC50 = 9.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 538 8 0 10 5.9 COc1cc(OCc2cccc(C3(OC)CCOCC3)n2)c2cc(-c3cn4nc([C@H](C)F)sc4n3)oc2c1 nan
72191814 133890 0 None - 1 Human 9.4 pIC50 = 9.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 504 7 0 11 4.8 COc1cc(OCc2ccnc(-c3ccnc(F)c3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3717518 133890 0 None - 1 Human 9.4 pIC50 = 9.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 504 7 0 11 4.8 COc1cc(OCc2ccnc(-c3ccnc(F)c3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118042464 134358 0 None - 1 Human 9.4 pIC50 = 9.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 543 10 0 11 6.0 CCCOc1ncc(-c2cccc(COc3cc(OC)cc4oc(-c5cn6nc(OC)sc6n5)cc34)c2)cn1 nan
CHEMBL3719074 134358 0 None - 1 Human 9.4 pIC50 = 9.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 543 10 0 11 6.0 CCCOc1ncc(-c2cccc(COc3cc(OC)cc4oc(-c5cn6nc(OC)sc6n5)cc34)c2)cn1 nan
72188739 134301 0 None - 1 Human 9.4 pIC50 = 9.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 518 7 0 9 6.5 COc1cc(OCc2cccc(-c3ccc(Cl)cn3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3718854 134301 0 None - 1 Human 9.4 pIC50 = 9.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 518 7 0 9 6.5 COc1cc(OCc2cccc(-c3ccc(Cl)cn3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72191194 134311 0 None - 1 Human 9.4 pIC50 = 9.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 533 8 0 11 5.4 COc1cc(OCc2cc(F)cc(-c3cnc(OC)nc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3718880 134311 0 None - 1 Human 9.4 pIC50 = 9.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 533 8 0 11 5.4 COc1cc(OCc2cc(F)cc(-c3cnc(OC)nc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
10269 671 21 None - 1 Human 9.4 pIC50 = 9.4 Functional
Antagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR methodAntagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR method
ChEMBL 513 7 0 12 4.4 COc1cc(OCc2nc(sc2C)N2CCOCC2)c2c(c1)oc(c2)c1cn2c(n1)sc(n2)OC 10.1021/acs.jmedchem.2c00359
72190270 671 21 None - 1 Human 9.4 pIC50 = 9.4 Functional
Antagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR methodAntagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR method
ChEMBL 513 7 0 12 4.4 COc1cc(OCc2nc(sc2C)N2CCOCC2)c2c(c1)oc(c2)c1cn2c(n1)sc(n2)OC 10.1021/acs.jmedchem.2c00359
CHEMBL3716726 671 21 None - 1 Human 9.4 pIC50 = 9.4 Functional
Antagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR methodAntagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR method
ChEMBL 513 7 0 12 4.4 COc1cc(OCc2nc(sc2C)N2CCOCC2)c2c(c1)oc(c2)c1cn2c(n1)sc(n2)OC 10.1021/acs.jmedchem.2c00359
12038 676 7 None - 1 Human 9.4 pIC50 = 9.4 Functional
Antagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR methodAntagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR method
ChEMBL 561 8 0 11 5.6 COc1nn2cc(nc2s1)c1cc2c(o1)cc(OC)cc2OCc1csc(n1)c1ccc(cc1)C(=O)N(C)C 10.1021/acs.jmedchem.2c00359
72188743 676 7 None - 1 Human 9.4 pIC50 = 9.4 Functional
Antagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR methodAntagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR method
ChEMBL 561 8 0 11 5.6 COc1nn2cc(nc2s1)c1cc2c(o1)cc(OC)cc2OCc1csc(n1)c1ccc(cc1)C(=O)N(C)C 10.1021/acs.jmedchem.2c00359
CHEMBL3716552 676 7 None - 1 Human 9.4 pIC50 = 9.4 Functional
Antagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR methodAntagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR method
ChEMBL 561 8 0 11 5.6 COc1nn2cc(nc2s1)c1cc2c(o1)cc(OC)cc2OCc1csc(n1)c1ccc(cc1)C(=O)N(C)C 10.1021/acs.jmedchem.2c00359
DB14942 676 7 None - 1 Human 9.4 pIC50 = 9.4 Functional
Antagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR methodAntagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR method
ChEMBL 561 8 0 11 5.6 COc1nn2cc(nc2s1)c1cc2c(o1)cc(OC)cc2OCc1csc(n1)c1ccc(cc1)C(=O)N(C)C 10.1021/acs.jmedchem.2c00359
72189039 133397 0 None - 1 Human 9.4 pIC50 = 9.4 Functional
Antagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR methodAntagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR method
ChEMBL 547 8 1 11 5.3 CNC(=O)c1ccc(-c2nc(COc3cc(OC)cc4oc(-c5cn6nc(OC)sc6n5)cc34)cs2)cc1 10.1021/acs.jmedchem.2c00359
CHEMBL3715840 133397 0 None - 1 Human 9.4 pIC50 = 9.4 Functional
Antagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR methodAntagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR method
ChEMBL 547 8 1 11 5.3 CNC(=O)c1ccc(-c2nc(COc3cc(OC)cc4oc(-c5cn6nc(OC)sc6n5)cc34)cs2)cc1 10.1021/acs.jmedchem.2c00359
89878648 134043 0 None - 1 Human 9.4 pIC50 = 9.4 Functional
Antagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR methodAntagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR method
ChEMBL 497 7 0 11 5.2 COc1cc(OCc2csc(N3CCCCC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.2c00359
CHEMBL3718059 134043 0 None - 1 Human 9.4 pIC50 = 9.4 Functional
Antagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR methodAntagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR method
ChEMBL 497 7 0 11 5.2 COc1cc(OCc2csc(N3CCCCC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.2c00359
168282821 190607 0 None - 1 Human 9.4 pIC50 = 9.4 Functional
Antagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR methodAntagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR method
ChEMBL 494 7 0 12 3.4 COc1cc(OCc2ccnc(N3CCOCC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.2c00359
CHEMBL5189522 190607 0 None - 1 Human 9.4 pIC50 = 9.4 Functional
Antagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR methodAntagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR method
ChEMBL 494 7 0 12 3.4 COc1cc(OCc2ccnc(N3CCOCC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.2c00359
130375610 191687 0 None - 1 Human 9.4 pIC50 = 9.4 Functional
Antagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR methodAntagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR method
ChEMBL 456 8 0 10 5.2 CCCc1nc(COc2cc(OC)cc3oc(-c4cn5nc(OC)sc5n4)cc23)cs1 10.1021/acs.jmedchem.2c00359
CHEMBL5206065 191687 0 None - 1 Human 9.4 pIC50 = 9.4 Functional
Antagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR methodAntagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR method
ChEMBL 456 8 0 10 5.2 CCCc1nc(COc2cc(OC)cc3oc(-c4cn5nc(OC)sc5n4)cc23)cs1 10.1021/acs.jmedchem.2c00359
72192126 133619 0 None - 1 Human 9.4 pIC50 = 9.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 524 7 1 10 5.2 COc1cc(OCc2cccc(C3(O)CCOCC3)n2)c2cc(-c3cn4nc([C@H](C)F)sc4n3)oc2c1 nan
CHEMBL3716576 133619 0 None - 1 Human 9.4 pIC50 = 9.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 524 7 1 10 5.2 COc1cc(OCc2cccc(C3(O)CCOCC3)n2)c2cc(-c3cn4nc([C@H](C)F)sc4n3)oc2c1 nan
89873549 133610 0 None - 1 Human 9.4 pIC50 = 9.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 508 7 1 11 4.2 COc1cc(OCc2cccc(C3(O)CCOCC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3716555 133610 0 None - 1 Human 9.4 pIC50 = 9.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 508 7 1 11 4.2 COc1cc(OCc2cccc(C3(O)CCOCC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
117981412 133999 0 None - 1 Human 9.4 pIC50 = 9.4 Functional
Inhibition of human PAR4 expressed in HEK293 cells assessed as Ala-(L-4-F-Phe)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-induced inhibition of calcium mobilization preincubated for 30 mins followed by Ala-(L-4-F-Phe)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly stimulation by FLIPR methodInhibition of human PAR4 expressed in HEK293 cells assessed as Ala-(L-4-F-Phe)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-induced inhibition of calcium mobilization preincubated for 30 mins followed by Ala-(L-4-F-Phe)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly stimulation by FLIPR method
ChEMBL 575 8 0 11 5.9 COc1cc(OCc2nc(-c3ccc(C(=O)N(C)C)cc3)sc2C)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1016/j.ejmech.2020.112893
CHEMBL3717891 133999 0 None - 1 Human 9.4 pIC50 = 9.4 Functional
Inhibition of human PAR4 expressed in HEK293 cells assessed as Ala-(L-4-F-Phe)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-induced inhibition of calcium mobilization preincubated for 30 mins followed by Ala-(L-4-F-Phe)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly stimulation by FLIPR methodInhibition of human PAR4 expressed in HEK293 cells assessed as Ala-(L-4-F-Phe)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-induced inhibition of calcium mobilization preincubated for 30 mins followed by Ala-(L-4-F-Phe)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly stimulation by FLIPR method
ChEMBL 575 8 0 11 5.9 COc1cc(OCc2nc(-c3ccc(C(=O)N(C)C)cc3)sc2C)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1016/j.ejmech.2020.112893
72189034 134199 0 None - 1 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 514 8 0 10 5.9 COc1ccc(-c2cccc(COc3cc(OC)cc4oc(-c5cn6nc(OC)sc6n5)cc34)c2)nc1 nan
CHEMBL3718564 134199 0 None - 1 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 514 8 0 10 5.9 COc1ccc(-c2cccc(COc3cc(OC)cc4oc(-c5cn6nc(OC)sc6n5)cc34)c2)nc1 nan
89884103 134370 0 None - 1 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 514 8 0 10 5.9 COc1cc(OCc2cccc(-c3ccc(OC)nc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3719106 134370 0 None - 1 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 514 8 0 10 5.9 COc1cc(OCc2cccc(-c3ccc(OC)nc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118042463 133364 0 None - 1 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 509 7 0 10 5.7 COc1cc(OCc2cccc(-c3ccc(C#N)cn3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3715722 133364 0 None - 1 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 509 7 0 10 5.7 COc1cc(OCc2cccc(-c3ccc(C#N)cn3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72190582 134328 0 None - 1 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 545 9 0 12 5.3 COc1cc(COc2cc(OC)cc3oc(-c4cn5nc(OC)sc5n4)cc23)cc(-c2cnc(OC)nc2)c1 nan
CHEMBL3718990 134328 0 None - 1 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 545 9 0 12 5.3 COc1cc(COc2cc(OC)cc3oc(-c4cn5nc(OC)sc5n4)cc23)cc(-c2cnc(OC)nc2)c1 nan
118042463 133364 0 None - 1 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR methodAntagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR method
ChEMBL 509 7 0 10 5.7 COc1cc(OCc2cccc(-c3ccc(C#N)cn3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.2c00359
CHEMBL3715722 133364 0 None - 1 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR methodAntagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR method
ChEMBL 509 7 0 10 5.7 COc1cc(OCc2cccc(-c3ccc(C#N)cn3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.2c00359
117981404 133465 0 None - 1 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR methodAntagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR method
ChEMBL 514 7 0 11 5.9 COc1cc(OCc2csc(C3CCSCC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.2c00359
CHEMBL3716066 133465 0 None - 1 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR methodAntagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR method
ChEMBL 514 7 0 11 5.9 COc1cc(OCc2csc(C3CCSCC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.2c00359
117981395 134130 0 None - 1 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR methodAntagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR method
ChEMBL 456 7 0 10 5.4 COc1cc(OCc2csc(C(C)C)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.2c00359
CHEMBL3718313 134130 0 None - 1 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR methodAntagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR method
ChEMBL 456 7 0 10 5.4 COc1cc(OCc2csc(C(C)C)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.2c00359
72189034 134199 0 None - 1 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR methodAntagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR method
ChEMBL 514 8 0 10 5.9 COc1ccc(-c2cccc(COc3cc(OC)cc4oc(-c5cn6nc(OC)sc6n5)cc34)c2)nc1 10.1021/acs.jmedchem.2c00359
CHEMBL3718564 134199 0 None - 1 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR methodAntagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR method
ChEMBL 514 8 0 10 5.9 COc1ccc(-c2cccc(COc3cc(OC)cc4oc(-c5cn6nc(OC)sc6n5)cc34)c2)nc1 10.1021/acs.jmedchem.2c00359
89884103 134370 0 None - 1 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR methodAntagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR method
ChEMBL 514 8 0 10 5.9 COc1cc(OCc2cccc(-c3ccc(OC)nc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.2c00359
CHEMBL3719106 134370 0 None - 1 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR methodAntagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR method
ChEMBL 514 8 0 10 5.9 COc1cc(OCc2cccc(-c3ccc(OC)nc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.2c00359
118042466 133563 0 None - 1 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 516 7 0 9 6.3 COc1cc(OCc2cccc(-c3ccc(C)nc3F)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3716388 133563 0 None - 1 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 516 7 0 9 6.3 COc1cc(OCc2cccc(-c3ccc(C)nc3F)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
164612042 184786 0 None 25 2 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity at human PAR4 expressed in Ga15-HEK293 cells assessed as reduction in PAR4 AP AYPGKF-NH2-induced cytosolic calcium incubated for 24 hrs by FLIPR - calcium mobilization assayAntagonist activity at human PAR4 expressed in Ga15-HEK293 cells assessed as reduction in PAR4 AP AYPGKF-NH2-induced cytosolic calcium incubated for 24 hrs by FLIPR - calcium mobilization assay
ChEMBL 371 2 0 6 4.2 COc1cc(Cl)c2nc(-c3cc(C)cc4c(=O)n(C)cnc34)sc2c1 10.1016/j.ejmech.2021.113764
CHEMBL4860533 184786 0 None 25 2 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity at human PAR4 expressed in Ga15-HEK293 cells assessed as reduction in PAR4 AP AYPGKF-NH2-induced cytosolic calcium incubated for 24 hrs by FLIPR - calcium mobilization assayAntagonist activity at human PAR4 expressed in Ga15-HEK293 cells assessed as reduction in PAR4 AP AYPGKF-NH2-induced cytosolic calcium incubated for 24 hrs by FLIPR - calcium mobilization assay
ChEMBL 371 2 0 6 4.2 COc1cc(Cl)c2nc(-c3cc(C)cc4c(=O)n(C)cnc34)sc2c1 10.1016/j.ejmech.2021.113764
72193007 133326 0 None - 1 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 532 7 0 9 6.8 COc1cc(OCc2cccc(-c3ncc(Cl)cc3C)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3715604 133326 0 None - 1 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 532 7 0 9 6.8 COc1cc(OCc2cccc(-c3ncc(Cl)cc3C)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72191197 133392 0 None - 1 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 612 10 0 11 7.5 COc1cc(OCc2cccc(-c3ccc(C(C)OC4CCCCO4)cn3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3715826 133392 0 None - 1 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 612 10 0 11 7.5 COc1cc(OCc2cccc(-c3ccc(C(C)OC4CCCCO4)cn3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
10269 671 21 None - 1 Human 9.3 pIC50 = 9.3 Functional
Inhibition of human PAR4 expressed in HEK293 cells assessed as Ala-(L-4-F-Phe)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-induced inhibition of calcium mobilization preincubated for 30 mins followed by Ala-(L-4-F-Phe)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly stimulation by FLIPR methodInhibition of human PAR4 expressed in HEK293 cells assessed as Ala-(L-4-F-Phe)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-induced inhibition of calcium mobilization preincubated for 30 mins followed by Ala-(L-4-F-Phe)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly stimulation by FLIPR method
ChEMBL 513 7 0 12 4.4 COc1cc(OCc2nc(sc2C)N2CCOCC2)c2c(c1)oc(c2)c1cn2c(n1)sc(n2)OC 10.1016/j.ejmech.2020.112893
72190270 671 21 None - 1 Human 9.3 pIC50 = 9.3 Functional
Inhibition of human PAR4 expressed in HEK293 cells assessed as Ala-(L-4-F-Phe)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-induced inhibition of calcium mobilization preincubated for 30 mins followed by Ala-(L-4-F-Phe)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly stimulation by FLIPR methodInhibition of human PAR4 expressed in HEK293 cells assessed as Ala-(L-4-F-Phe)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-induced inhibition of calcium mobilization preincubated for 30 mins followed by Ala-(L-4-F-Phe)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly stimulation by FLIPR method
ChEMBL 513 7 0 12 4.4 COc1cc(OCc2nc(sc2C)N2CCOCC2)c2c(c1)oc(c2)c1cn2c(n1)sc(n2)OC 10.1016/j.ejmech.2020.112893
CHEMBL3716726 671 21 None - 1 Human 9.3 pIC50 = 9.3 Functional
Inhibition of human PAR4 expressed in HEK293 cells assessed as Ala-(L-4-F-Phe)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-induced inhibition of calcium mobilization preincubated for 30 mins followed by Ala-(L-4-F-Phe)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly stimulation by FLIPR methodInhibition of human PAR4 expressed in HEK293 cells assessed as Ala-(L-4-F-Phe)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-induced inhibition of calcium mobilization preincubated for 30 mins followed by Ala-(L-4-F-Phe)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly stimulation by FLIPR method
ChEMBL 513 7 0 12 4.4 COc1cc(OCc2nc(sc2C)N2CCOCC2)c2c(c1)oc(c2)c1cn2c(n1)sc(n2)OC 10.1016/j.ejmech.2020.112893
72190265 133440 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 548 8 0 10 6.5 COc1cc(COc2cc(OC)cc3oc(-c4cn5nc(OC)sc5n4)cc23)cc(-c2ccc(Cl)nc2)c1 nan
CHEMBL3715991 133440 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 548 8 0 10 6.5 COc1cc(COc2cc(OC)cc3oc(-c4cn5nc(OC)sc5n4)cc23)cc(-c2ccc(Cl)nc2)c1 nan
72188737 133705 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 516 7 0 9 6.3 COc1cc(OCc2cccc(-c3ccc(F)c(C)n3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3716899 133705 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 516 7 0 9 6.3 COc1cc(OCc2cccc(-c3ccc(F)c(C)n3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118068683 135260 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 534 9 0 11 6.1 COc1cc(OCc2cccc(OCc3csc(C)n3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3730431 135260 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 534 9 0 11 6.1 COc1cc(OCc2cccc(OCc3csc(C)n3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
89884107 133635 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 552 7 0 9 6.9 COc1cc(OCc2cccc(-c3ccc(C(F)(F)F)cn3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3716636 133635 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 552 7 0 9 6.9 COc1cc(OCc2cccc(-c3ccc(C(F)(F)F)cn3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72190272 133110 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR methodAntagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR method
ChEMBL 483 7 0 12 3.6 COc1cc(OCc2coc(N3CCOCC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.2c00359
CHEMBL3714821 133110 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR methodAntagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR method
ChEMBL 483 7 0 12 3.6 COc1cc(OCc2coc(N3CCOCC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.2c00359
72190269 133332 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR methodAntagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR method
ChEMBL 525 7 0 12 4.6 COc1cc(OCc2csc(N3CC4CCC(C3)O4)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.2c00359
CHEMBL3715632 133332 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR methodAntagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR method
ChEMBL 525 7 0 12 4.6 COc1cc(OCc2csc(N3CC4CCC(C3)O4)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.2c00359
89878694 133399 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR methodAntagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR method
ChEMBL 442 7 0 10 4.8 CCc1nc(COc2cc(OC)cc3oc(-c4cn5nc(OC)sc5n4)cc23)cs1 10.1021/acs.jmedchem.2c00359
CHEMBL3715852 133399 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR methodAntagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR method
ChEMBL 442 7 0 10 4.8 CCc1nc(COc2cc(OC)cc3oc(-c4cn5nc(OC)sc5n4)cc23)cs1 10.1021/acs.jmedchem.2c00359
117981575 133463 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR methodAntagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR method
ChEMBL 623 8 0 11 6.4 COc1cc(OCc2csc(-c3ccc(C(=O)N4CCC(F)(F)C4)cc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.2c00359
CHEMBL3716064 133463 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR methodAntagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR method
ChEMBL 623 8 0 11 6.4 COc1cc(OCc2csc(-c3ccc(C(=O)N4CCC(F)(F)C4)cc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.2c00359
89884107 133635 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR methodAntagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR method
ChEMBL 552 7 0 9 6.9 COc1cc(OCc2cccc(-c3ccc(C(F)(F)F)cn3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.2c00359
CHEMBL3716636 133635 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR methodAntagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR method
ChEMBL 552 7 0 9 6.9 COc1cc(OCc2cccc(-c3ccc(C(F)(F)F)cn3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.2c00359
89878899 134143 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR methodAntagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR method
ChEMBL 587 8 0 11 6.2 COc1cc(OCc2csc(-c3ccc(C(=O)N4CCCC4)cc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.2c00359
CHEMBL3718360 134143 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR methodAntagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR method
ChEMBL 587 8 0 11 6.2 COc1cc(OCc2csc(-c3ccc(C(=O)N4CCCC4)cc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.2c00359
86700890 134393 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR methodAntagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR method
ChEMBL 499 7 0 12 4.1 COc1cc(OCc2csc(N3CCOCC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.2c00359
CHEMBL3719215 134393 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR methodAntagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR method
ChEMBL 499 7 0 12 4.1 COc1cc(OCc2csc(N3CCOCC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.2c00359
168273671 189766 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR methodAntagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR method
ChEMBL 493 7 0 11 4.0 COc1cc(OCc2cccc(N3CCOCC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.2c00359
CHEMBL5177223 189766 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR methodAntagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR method
ChEMBL 493 7 0 11 4.0 COc1cc(OCc2cccc(N3CCOCC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.2c00359
168279555 190254 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR methodAntagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR method
ChEMBL 505 7 0 9 5.8 COc1cc(COc2cc(OC)cc3oc(-c4cn5nc(OC)sc5n4)cc23)cc(C(F)(F)F)c1 10.1021/acs.jmedchem.2c00359
CHEMBL5184586 190254 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR methodAntagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR method
ChEMBL 505 7 0 9 5.8 COc1cc(COc2cc(OC)cc3oc(-c4cn5nc(OC)sc5n4)cc23)cc(C(F)(F)F)c1 10.1021/acs.jmedchem.2c00359
72188738 133777 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 520 7 0 9 6.1 COc1cc(OCc2cccc(-c3ncc(F)cc3F)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3717105 133777 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 520 7 0 9 6.1 COc1cc(OCc2cccc(-c3ncc(F)cc3F)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118042465 134233 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 516 7 0 9 6.3 COc1cc(OCc2cccc(-c3cnc(F)c(C)c3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3718647 134233 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 516 7 0 9 6.3 COc1cc(OCc2cccc(-c3cnc(F)c(C)c3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72191812 133584 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 489 7 0 8 6.8 COc1cc(OCc2cccc(C3CCCCC3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3716460 133584 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 489 7 0 8 6.8 COc1cc(OCc2cccc(C3CCCCC3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72189037 133916 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 515 8 0 11 5.3 COc1cc(OCc2cccc(-c3cnc(OC)nc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3717597 133916 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 515 8 0 11 5.3 COc1cc(OCc2cccc(-c3cnc(OC)nc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72189634 134014 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 502 7 0 9 6.0 COc1cc(OCc2cccc(-c3ccnc(F)c3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3717959 134014 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 502 7 0 9 6.0 COc1cc(OCc2cccc(-c3ccnc(F)c3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
89878693 133894 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR methodAntagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR method
ChEMBL 512 7 0 12 4.0 COc1cc(OCc2csc(N3CCN(C)CC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.2c00359
CHEMBL3717535 133894 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR methodAntagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR method
ChEMBL 512 7 0 12 4.0 COc1cc(OCc2csc(N3CCN(C)CC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.2c00359
72189037 133916 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR methodAntagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR method
ChEMBL 515 8 0 11 5.3 COc1cc(OCc2cccc(-c3cnc(OC)nc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.2c00359
CHEMBL3717597 133916 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR methodAntagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR method
ChEMBL 515 8 0 11 5.3 COc1cc(OCc2cccc(-c3cnc(OC)nc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.2c00359
168269004 189393 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR methodAntagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR method
ChEMBL 492 7 0 10 4.6 COc1cc(OCc2cccc(N3CCOCC3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.2c00359
CHEMBL5171201 189393 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR methodAntagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR method
ChEMBL 492 7 0 10 4.6 COc1cc(OCc2cccc(N3CCOCC3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.2c00359
10269 671 21 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at human PAR4 expressed in Ga15-HEK293 cells assessed as reduction in PAR4 AP AYPGKF-NH2-induced cytosolic calcium incubated for 24 hrs by FLIPR - calcium mobilization assayAntagonist activity at human PAR4 expressed in Ga15-HEK293 cells assessed as reduction in PAR4 AP AYPGKF-NH2-induced cytosolic calcium incubated for 24 hrs by FLIPR - calcium mobilization assay
ChEMBL 513 7 0 12 4.4 COc1cc(OCc2nc(sc2C)N2CCOCC2)c2c(c1)oc(c2)c1cn2c(n1)sc(n2)OC 10.1016/j.ejmech.2021.113764
72190270 671 21 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at human PAR4 expressed in Ga15-HEK293 cells assessed as reduction in PAR4 AP AYPGKF-NH2-induced cytosolic calcium incubated for 24 hrs by FLIPR - calcium mobilization assayAntagonist activity at human PAR4 expressed in Ga15-HEK293 cells assessed as reduction in PAR4 AP AYPGKF-NH2-induced cytosolic calcium incubated for 24 hrs by FLIPR - calcium mobilization assay
ChEMBL 513 7 0 12 4.4 COc1cc(OCc2nc(sc2C)N2CCOCC2)c2c(c1)oc(c2)c1cn2c(n1)sc(n2)OC 10.1016/j.ejmech.2021.113764
CHEMBL3716726 671 21 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at human PAR4 expressed in Ga15-HEK293 cells assessed as reduction in PAR4 AP AYPGKF-NH2-induced cytosolic calcium incubated for 24 hrs by FLIPR - calcium mobilization assayAntagonist activity at human PAR4 expressed in Ga15-HEK293 cells assessed as reduction in PAR4 AP AYPGKF-NH2-induced cytosolic calcium incubated for 24 hrs by FLIPR - calcium mobilization assay
ChEMBL 513 7 0 12 4.4 COc1cc(OCc2nc(sc2C)N2CCOCC2)c2c(c1)oc(c2)c1cn2c(n1)sc(n2)OC 10.1016/j.ejmech.2021.113764
72191810 133547 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 489 7 0 9 5.6 COc1cc(OCc2cccc(C3=CCOCC3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3716332 133547 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 489 7 0 9 5.6 COc1cc(OCc2cccc(C3=CCOCC3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72192131 133586 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 506 7 0 12 5.0 COc1cc(OCc2ccnc(-c3csc(C)n3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3716464 133586 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 506 7 0 12 5.0 COc1cc(OCc2ccnc(-c3csc(C)n3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72191503 133807 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 491 7 0 9 5.7 COc1cc(OCc2cccc(C3CCOCC3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3717220 133807 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 491 7 0 9 5.7 COc1cc(OCc2cccc(C3CCOCC3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118068646 135031 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 549 9 0 9 6.7 COc1cc(OCc2cccc(OCc3cccc(F)c3F)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3729018 135031 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 549 9 0 9 6.7 COc1cc(OCc2cccc(OCc3cccc(F)c3F)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118068698 134785 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 573 11 0 11 6.4 COc1cc(OCc2cccc(OCc3ccc(OC)c(OC)c3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3727531 134785 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 573 11 0 11 6.4 COc1cc(OCc2cccc(OCc3ccc(OC)c(OC)c3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72189635 133683 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 518 7 0 9 6.5 COc1cc(OCc2cccc(-c3ccc(Cl)nc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3716818 133683 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 518 7 0 9 6.5 COc1cc(OCc2cccc(-c3ccc(Cl)nc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72192129 133947 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 515 8 0 11 5.3 COc1ccc(-c2nccc(COc3cc(OC)cc4oc(-c5cn6nc(OC)sc6n5)cc34)n2)cc1 nan
CHEMBL3717703 133947 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 515 8 0 11 5.3 COc1ccc(-c2nccc(COc3cc(OC)cc4oc(-c5cn6nc(OC)sc6n5)cc34)n2)cc1 nan
118068397 135364 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 531 9 0 9 6.5 COc1cc(OCc2cc(F)cc(OCc3ccccc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3731050 135364 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 531 9 0 9 6.5 COc1cc(OCc2cc(F)cc(OCc3ccccc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72191500 133361 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 584 9 0 11 6.8 COc1cc(OCc2cccc(-c3ccc(OC4CCCCO4)cn3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3715717 133361 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 584 9 0 11 6.8 COc1cc(OCc2cccc(-c3ccc(OC4CCCCO4)cn3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
117981411 133194 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR methodAntagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR method
ChEMBL 561 8 0 11 5.6 COc1cc(OCc2csc(-c3cccc(C(=O)N(C)C)c3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.2c00359
CHEMBL3715093 133194 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR methodAntagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR method
ChEMBL 561 8 0 11 5.6 COc1cc(OCc2csc(-c3cccc(C(=O)N(C)C)c3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.2c00359
117981423 133298 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR methodAntagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR method
ChEMBL 568 8 0 12 5.3 COc1cc(OCc2csc(-c3ccc(S(C)(=O)=O)cc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.2c00359
CHEMBL3715516 133298 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR methodAntagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR method
ChEMBL 568 8 0 12 5.3 COc1cc(OCc2csc(-c3ccc(S(C)(=O)=O)cc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.2c00359
89884100 133756 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR methodAntagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR method
ChEMBL 473 7 0 9 6.1 COc1cc(OCc2cccc(-c3ccoc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.2c00359
CHEMBL3717040 133756 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR methodAntagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR method
ChEMBL 473 7 0 9 6.1 COc1cc(OCc2cccc(-c3ccoc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.2c00359
168273516 189565 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR methodAntagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR method
ChEMBL 521 8 0 12 5.3 COc1cc(OCc2csc(-c3ccc(OC)nc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.2c00359
CHEMBL5173906 189565 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR methodAntagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR method
ChEMBL 521 8 0 12 5.3 COc1cc(OCc2csc(-c3ccc(OC)nc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.2c00359
155555810 173797 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assayAntagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assay
ChEMBL 437 8 0 9 4.7 COc1cc(OCCOc2ccccc2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.9b00186
CHEMBL4551932 173797 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assayAntagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assay
ChEMBL 437 8 0 9 4.7 COc1cc(OCCOc2ccccc2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.9b00186
72189942 133565 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 532 8 0 10 6.0 COc1ccc(-c2cc(F)cc(COc3cc(OC)cc4oc(-c5cn6nc(OC)sc6n5)cc34)c2)nc1 nan
CHEMBL3716397 133565 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 532 8 0 10 6.0 COc1ccc(-c2cc(F)cc(COc3cc(OC)cc4oc(-c5cn6nc(OC)sc6n5)cc34)c2)nc1 nan
72192421 134348 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 543 7 0 12 5.1 COc1cc(OCc2ccnc(C3COc4ccccc4O3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3719049 134348 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 543 7 0 12 5.1 COc1cc(OCc2ccnc(C3COc4ccccc4O3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118068633 134917 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 529 9 0 9 7.1 COc1cc(OCc2cccc(OCc3ccccc3)c2)c2cc(-c3cn4nc(SC)sc4n3)oc2c1 nan
CHEMBL3728326 134917 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 529 9 0 9 7.1 COc1cc(OCc2cccc(OCc3ccccc3)c2)c2cc(-c3cn4nc(SC)sc4n3)oc2c1 nan
72202285 135367 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 431 6 0 10 3.8 COc1cc(OC[C@@H]2COC(C)(C)O2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3731063 135367 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 431 6 0 10 3.8 COc1cc(OC[C@@H]2COC(C)(C)O2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
155529126 170829 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assayAntagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assay
ChEMBL 515 8 0 9 7.0 COc1cc(OCc2cccc(Sc3ccccc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.9b00186
CHEMBL4462511 170829 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assayAntagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assay
ChEMBL 515 8 0 9 7.0 COc1cc(OCc2cccc(Sc3ccccc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.9b00186
72192130 134414 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR methodAntagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR method
ChEMBL 485 7 0 10 5.3 COc1cc(OCc2ccnc(-c3ccccc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.2c00359
CHEMBL3719264 134414 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR methodAntagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR method
ChEMBL 485 7 0 10 5.3 COc1cc(OCc2ccnc(-c3ccccc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.2c00359
72192130 134414 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 485 7 0 10 5.3 COc1cc(OCc2ccnc(-c3ccccc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3719264 134414 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 485 7 0 10 5.3 COc1cc(OCc2ccnc(-c3ccccc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
117981422 133260 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 525 7 0 11 6.0 COc1cc(OCc2csc(-c3ccc(Cl)nc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3715367 133260 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 525 7 0 11 6.0 COc1cc(OCc2csc(-c3ccc(Cl)nc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72190886 134317 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 514 8 0 10 5.9 COc1ccc(-c2cccc(COc3cc(OC)cc4oc(-c5cn6nc(OC)sc6n5)cc34)n2)cc1 nan
CHEMBL3718901 134317 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 514 8 0 10 5.9 COc1ccc(-c2cccc(COc3cc(OC)cc4oc(-c5cn6nc(OC)sc6n5)cc34)n2)cc1 nan
89878888 133955 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 505 7 0 11 5.6 COc1cc(OCc2csc(-c3ccc(C)nc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3717746 133955 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 505 7 0 11 5.6 COc1cc(OCc2csc(-c3ccc(C)nc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
89880942 170493 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assayAntagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assay
ChEMBL 432 6 0 9 4.7 COc1cc(OCc2cccc(C#N)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.9b00186
CHEMBL4457190 170493 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assayAntagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assay
ChEMBL 432 6 0 9 4.7 COc1cc(OCc2cccc(C#N)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.9b00186
118068442 134987 0 None - 1 Human 9.0 pIC50 = 9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 331 4 0 8 3.2 COc1cc(OC)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3728724 134987 0 None - 1 Human 9.0 pIC50 = 9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 331 4 0 8 3.2 COc1cc(OC)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118068442 134987 0 None - 1 Human 9.0 pIC50 = 9 Functional
Antagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assayAntagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assay
ChEMBL 331 4 0 8 3.2 COc1cc(OC)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.9b00186
CHEMBL3728724 134987 0 None - 1 Human 9.0 pIC50 = 9 Functional
Antagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assayAntagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assay
ChEMBL 331 4 0 8 3.2 COc1cc(OC)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.9b00186
117981576 134411 0 None - 1 Human 9.0 pIC50 = 9 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 600 10 0 12 5.9 CCN(CC#N)C(=O)c1ccc(-c2nc(COc3cc(OC)cc4oc(-c5cn6nc(OC)sc6n5)cc34)cs2)cc1 nan
CHEMBL3719256 134411 0 None - 1 Human 9.0 pIC50 = 9 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 600 10 0 12 5.9 CCN(CC#N)C(=O)c1ccc(-c2nc(COc3cc(OC)cc4oc(-c5cn6nc(OC)sc6n5)cc34)cs2)cc1 nan
72189941 134406 0 None - 1 Human 9.0 pIC50 = 9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 648 12 0 11 8.1 COc1ccc(COC(C)c2ccc(-c3cccc(COc4cc(OC)cc5oc(-c6cn7nc(OC)sc7n6)cc45)c3)nc2)cc1 nan
CHEMBL3719244 134406 0 None - 1 Human 9.0 pIC50 = 9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 648 12 0 11 8.1 COc1ccc(COC(C)c2ccc(-c3cccc(COc4cc(OC)cc5oc(-c6cn7nc(OC)sc7n6)cc45)c3)nc2)cc1 nan
139388463 181532 0 None - 1 Human 9.0 pIC50 = 9 Functional
Inhibition of human PAR4 expressed in HEK293 cells assessed as Ala-(L-4-F-Phe)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-induced inhibition of calcium mobilization preincubated for 30 mins followed by Ala-(L-4-F-Phe)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly stimulation by FLIPR methodInhibition of human PAR4 expressed in HEK293 cells assessed as Ala-(L-4-F-Phe)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-induced inhibition of calcium mobilization preincubated for 30 mins followed by Ala-(L-4-F-Phe)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly stimulation by FLIPR method
ChEMBL 399 4 1 6 5.3 Cc1cc(-c2nc(C)c(-c3cccc(O)c3)s2)c2ncc(OC(F)F)nc2c1 10.1016/j.ejmech.2020.112893
CHEMBL4782079 181532 0 None - 1 Human 9.0 pIC50 = 9 Functional
Inhibition of human PAR4 expressed in HEK293 cells assessed as Ala-(L-4-F-Phe)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-induced inhibition of calcium mobilization preincubated for 30 mins followed by Ala-(L-4-F-Phe)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly stimulation by FLIPR methodInhibition of human PAR4 expressed in HEK293 cells assessed as Ala-(L-4-F-Phe)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-induced inhibition of calcium mobilization preincubated for 30 mins followed by Ala-(L-4-F-Phe)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly stimulation by FLIPR method
ChEMBL 399 4 1 6 5.3 Cc1cc(-c2nc(C)c(-c3cccc(O)c3)s2)c2ncc(OC(F)F)nc2c1 10.1016/j.ejmech.2020.112893
72189038 133158 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 490 7 0 10 5.9 COc1cc(OCc2cccc(-c3cnsc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3714996 133158 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 490 7 0 10 5.9 COc1cc(OCc2cccc(-c3cnsc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118042467 133595 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 502 7 0 9 6.0 COc1cc(OCc2cccc(-c3cccnc3F)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3716502 133595 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 502 7 0 9 6.0 COc1cc(OCc2cccc(-c3cccnc3F)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72189036 133163 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 510 7 0 11 5.1 COc1cc(OCc2cccc(-c3cnc(C#N)cn3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3715007 133163 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 510 7 0 11 5.1 COc1cc(OCc2cccc(-c3cnc(C#N)cn3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72192422 133383 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 525 8 0 10 5.7 COc1cc(OCc2ccnc(C3(c4ccccc4)CC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3715775 133383 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 525 8 0 10 5.7 COc1cc(OCc2ccnc(C3(c4ccccc4)CC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72192415 134432 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 485 7 0 10 5.3 COc1cc(OCc2cccc(-c3cncnc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3719331 134432 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 485 7 0 10 5.3 COc1cc(OCc2cccc(-c3cncnc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72190264 133985 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 474 7 0 10 5.5 COc1cc(OCc2cncc(-c3ccoc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3717838 133985 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 474 7 0 10 5.5 COc1cc(OCc2cncc(-c3ccoc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72192424 134435 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 519 7 0 10 5.9 COc1ncc(-c2cccc(COc3cc(Cl)cc4oc(-c5cn6nc(OC)sc6n5)cc34)c2)cn1 nan
CHEMBL3719340 134435 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 519 7 0 10 5.9 COc1ncc(-c2cccc(COc3cc(Cl)cc4oc(-c5cn6nc(OC)sc6n5)cc34)c2)cn1 nan
72202582 134984 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 549 10 0 9 7.0 COc1nn2cc(-c3cc4c(OCc5cccc(OCc6ccccc6)c5)cc(OC(F)F)cc4o3)nc2s1 nan
CHEMBL3728707 134984 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 549 10 0 9 7.0 COc1nn2cc(-c3cc4c(OCc5cccc(OCc6ccccc6)c5)cc(OC(F)F)cc4o3)nc2s1 nan
72191499 133544 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 583 9 0 10 7.4 COc1cc(OCc2cccc(-c3ccc(OC4CCCCO4)cc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3716323 133544 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 583 9 0 10 7.4 COc1cc(OCc2cccc(-c3ccc(OC4CCCCO4)cc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72193329 133238 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR methodAntagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR method
ChEMBL 490 7 0 10 5.9 COc1cc(OCc2nc(-c3ccccc3)cs2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.2c00359
CHEMBL3715264 133238 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR methodAntagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR method
ChEMBL 490 7 0 10 5.9 COc1cc(OCc2nc(-c3ccccc3)cs2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.2c00359
72192415 134432 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR methodAntagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR method
ChEMBL 485 7 0 10 5.3 COc1cc(OCc2cccc(-c3cncnc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.2c00359
CHEMBL3719331 134432 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR methodAntagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR method
ChEMBL 485 7 0 10 5.3 COc1cc(OCc2cccc(-c3cncnc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.2c00359
89873081 191626 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR methodAntagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR method
ChEMBL 534 8 1 11 5.6 COc1cc(OCc2csc(-c3ccc(C(=O)O)cc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.2c00359
CHEMBL5205126 191626 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR methodAntagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR method
ChEMBL 534 8 1 11 5.6 COc1cc(OCc2csc(-c3ccc(C(=O)O)cc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.2c00359
155525561 170530 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assayAntagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assay
ChEMBL 421 7 0 8 4.8 COc1cc(OCCc2ccccc2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.9b00186
CHEMBL4457819 170530 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assayAntagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assay
ChEMBL 421 7 0 8 4.8 COc1cc(OCCc2ccccc2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.9b00186
72191198 133752 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 528 8 1 10 5.9 COc1cc(OCc2cccc(-c3ccc(C(C)O)cn3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3717026 133752 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 528 8 1 10 5.9 COc1cc(OCc2cccc(-c3ccc(C(C)O)cn3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118068661 135460 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 603 12 0 12 6.4 COc1cc(OCc2cccc(OCc3cc(OC)c(OC)c(OC)c3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3731644 135460 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 603 12 0 12 6.4 COc1cc(OCc2cccc(OCc3cc(OC)c(OC)c(OC)c3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118068702 135231 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 561 8 0 8 7.1 COc1cc(OCc2cccc(OCc3ccccc3)c2)c2cc(-c3cn4nc(Br)sc4n3)oc2c1 nan
CHEMBL3730244 135231 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 561 8 0 8 7.1 COc1cc(OCc2cccc(OCc3ccccc3)c2)c2cc(-c3cn4nc(Br)sc4n3)oc2c1 nan
118068684 135563 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 529 9 0 8 7.4 COc1cc(OCc2cccc(OCc3ccccc3)c2)c2cc(-c3cn4nc([C@H](C)F)sc4n3)oc2c1 nan
CHEMBL3732266 135563 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 529 9 0 8 7.4 COc1cc(OCc2cccc(OCc3ccccc3)c2)c2cc(-c3cn4nc([C@H](C)F)sc4n3)oc2c1 nan
72189339 134083 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 528 8 0 10 6.2 COc1cc(OCc2cccc(-c3cnc(OC)cc3C)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3718187 134083 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 528 8 0 10 6.2 COc1cc(OCc2cccc(-c3cnc(OC)cc3C)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72189345 133470 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 600 9 0 12 5.8 COc1cc(OCc2nc(-c3ccc(C(=O)N(C)CC#N)cc3)sc2C)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3716096 133470 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 600 9 0 12 5.8 COc1cc(OCc2nc(-c3ccc(C(=O)N(C)CC#N)cc3)sc2C)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118068437 134939 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assayAntagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assay
ChEMBL 301 3 0 7 3.2 COc1ccc2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.9b00186
CHEMBL3728462 134939 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assayAntagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assay
ChEMBL 301 3 0 7 3.2 COc1ccc2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.9b00186
155528420 170753 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assayAntagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assay
ChEMBL 499 8 0 9 6.6 COc1cc(OCc2cccc(Oc3ccccc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.9b00186
CHEMBL4461217 170753 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assayAntagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assay
ChEMBL 499 8 0 9 6.6 COc1cc(OCc2cccc(Oc3ccccc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.9b00186
164610234 184488 0 None 60 2 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at human PAR4 expressed in Ga15-HEK293 cells assessed as reduction in PAR4 AP AYPGKF-NH2-induced cytosolic calcium incubated for 24 hrs by FLIPR - calcium mobilization assayAntagonist activity at human PAR4 expressed in Ga15-HEK293 cells assessed as reduction in PAR4 AP AYPGKF-NH2-induced cytosolic calcium incubated for 24 hrs by FLIPR - calcium mobilization assay
ChEMBL 608 7 1 8 5.5 Cc1cc(-c2nc3c(Cl)cc(OCCNS(=O)(=O)c4ccc(C(F)(F)F)cc4)cc3s2)c2ncn(C)c(=O)c2c1 10.1016/j.ejmech.2021.113764
CHEMBL4855875 184488 0 None 60 2 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at human PAR4 expressed in Ga15-HEK293 cells assessed as reduction in PAR4 AP AYPGKF-NH2-induced cytosolic calcium incubated for 24 hrs by FLIPR - calcium mobilization assayAntagonist activity at human PAR4 expressed in Ga15-HEK293 cells assessed as reduction in PAR4 AP AYPGKF-NH2-induced cytosolic calcium incubated for 24 hrs by FLIPR - calcium mobilization assay
ChEMBL 608 7 1 8 5.5 Cc1cc(-c2nc3c(Cl)cc(OCCNS(=O)(=O)c4ccc(C(F)(F)F)cc4)cc3s2)c2ncn(C)c(=O)c2c1 10.1016/j.ejmech.2021.113764
118042468 133272 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 502 7 0 9 6.0 COc1cc(OCc2cccc(-c3ncccc3F)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3715416 133272 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 502 7 0 9 6.0 COc1cc(OCc2cccc(-c3ncccc3F)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72189637 133552 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 545 10 0 12 5.2 COCOc1cnc(-c2cccc(COc3cc(OC)cc4oc(-c5cn6nc(OC)sc6n5)cc34)c2)cn1 nan
CHEMBL3716344 133552 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 545 10 0 12 5.2 COCOc1cnc(-c2cccc(COc3cc(OC)cc4oc(-c5cn6nc(OC)sc6n5)cc34)c2)cn1 nan
118068437 134939 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 301 3 0 7 3.2 COc1ccc2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3728462 134939 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 301 3 0 7 3.2 COc1ccc2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118070682 135331 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 347 4 0 8 3.9 COc1cc(OC)c2cc(-c3cn4nc(SC)sc4n3)oc2c1 nan
CHEMBL3730863 135331 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 347 4 0 8 3.9 COc1cc(OC)c2cc(-c3cn4nc(SC)sc4n3)oc2c1 nan
118068652 135737 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 543 10 0 10 6.4 COc1cc(OCc2cccc(OCc3ccccc3OC)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3733324 135737 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 543 10 0 10 6.4 COc1cc(OCc2cccc(OCc3ccccc3OC)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118068655 135736 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 547 9 0 9 7.0 COc1cc(OCc2cccc(OCc3ccccc3Cl)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3733319 135736 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 547 9 0 9 7.0 COc1cc(OCc2cccc(OCc3ccccc3Cl)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72192712 133450 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 489 7 0 9 6.5 COc1cc(OCc2cccc(-c3ccsc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3716026 133450 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 489 7 0 9 6.5 COc1cc(OCc2cccc(-c3ccsc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118068689 135133 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 577 10 0 10 7.0 COc1cc(Cl)cc(COc2cccc(COc3cc(OC)cc4oc(-c5cn6nc(OC)sc6n5)cc34)c2)c1 nan
CHEMBL3729641 135133 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 577 10 0 10 7.0 COc1cc(Cl)cc(COc2cccc(COc3cc(OC)cc4oc(-c5cn6nc(OC)sc6n5)cc34)c2)c1 nan
72192419 133996 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 502 7 0 9 6.0 COc1cc(OCc2cccc(-c3ccc(F)nc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3717884 133996 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 502 7 0 9 6.0 COc1cc(OCc2cccc(-c3ccc(F)nc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
89878692 134094 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR methodAntagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR method
ChEMBL 558 7 0 10 6.9 COc1cc(OCc2csc(-c3ccc(C(F)(F)F)cc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.2c00359
CHEMBL3718231 134094 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR methodAntagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR method
ChEMBL 558 7 0 10 6.9 COc1cc(OCc2csc(-c3ccc(C(F)(F)F)cc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.2c00359
89878655 134356 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR methodAntagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR method
ChEMBL 498 7 0 11 5.2 COc1cc(OCc2csc(C3CCOCC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.2c00359
CHEMBL3719069 134356 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR methodAntagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR method
ChEMBL 498 7 0 11 5.2 COc1cc(OCc2csc(C3CCOCC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.2c00359
118068383 169750 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assayAntagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assay
ChEMBL 513 9 0 9 6.4 COc1cc(OCc2ccc(OCc3ccccc3)cc2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.9b00186
CHEMBL4447049 169750 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assayAntagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assay
ChEMBL 513 9 0 9 6.4 COc1cc(OCc2ccc(OCc3ccccc3)cc2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.9b00186
72190890 133202 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 493 7 0 9 5.5 COc1cc(OCc2cccc(-c3cnc(OC)nc3)c2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
CHEMBL3715116 133202 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 493 7 0 9 5.5 COc1cc(OCc2cccc(-c3cnc(OC)nc3)c2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
118068639 135301 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 607 11 0 11 7.1 COc1cc(OCc2cccc(OCc3ccc(OC)c(OC)c3Cl)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3730688 135301 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 607 11 0 11 7.1 COc1cc(OCc2cccc(OCc3ccc(OC)c(OC)c3Cl)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72192420 134343 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 449 7 0 10 4.5 COc1cc(OCc2ccnc(C3CC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3719033 134343 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 449 7 0 10 4.5 COc1cc(OCc2ccnc(C3CC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72192716 133654 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 519 7 0 10 5.9 COc1cnc(-c2cccc(COc3cc(Cl)cc4oc(-c5cn6nc(OC)sc6n5)cc34)c2)cn1 nan
CHEMBL3716719 133654 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 519 7 0 10 5.9 COc1cnc(-c2cccc(COc3cc(Cl)cc4oc(-c5cn6nc(OC)sc6n5)cc34)c2)cn1 nan
118068714 135372 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 543 10 0 10 6.4 COc1ccc(COc2cccc(COc3cc(OC)cc4oc(-c5cn6nc(OC)sc6n5)cc34)c2)cc1 nan
CHEMBL3731102 135372 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 543 10 0 10 6.4 COc1ccc(COc2cccc(COc3cc(OC)cc4oc(-c5cn6nc(OC)sc6n5)cc34)c2)cc1 nan
72189341 133308 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 552 7 0 9 7.2 COc1cc(OCc2cccc(-c3ncc(Cl)cc3Cl)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3715555 133308 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 552 7 0 9 7.2 COc1cc(OCc2cccc(-c3ncc(Cl)cc3Cl)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72190581 133365 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 538 7 0 9 6.3 COc1cc(OCc2cc(F)cc(-c3ncc(F)cc3F)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3715723 133365 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 538 7 0 9 6.3 COc1cc(OCc2cc(F)cc(-c3ncc(F)cc3F)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72189340 133818 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 515 8 0 11 5.3 COc1cc(OCc2cccc(-c3cnc(OC)cn3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3717275 133818 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 515 8 0 11 5.3 COc1cc(OCc2cccc(-c3cnc(OC)cn3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118068669 135577 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 565 9 0 9 7.2 COc1cc(OCc2cccc(OCc3ccc(Cl)cc3F)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3732358 135577 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 565 9 0 9 7.2 COc1cc(OCc2cccc(OCc3ccc(Cl)cc3F)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72191196 134225 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 599 11 0 11 5.6 COCCN(C)C(=O)c1ccc(-c2cccc(COc3cc(OC)cc4oc(-c5cn6nc(OC)sc6n5)cc34)c2)cn1 nan
CHEMBL3718635 134225 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 599 11 0 11 5.6 COCCN(C)C(=O)c1ccc(-c2cccc(COc3cc(OC)cc4oc(-c5cn6nc(OC)sc6n5)cc34)c2)cn1 nan
72189340 133818 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR methodAntagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR method
ChEMBL 515 8 0 11 5.3 COc1cc(OCc2cccc(-c3cnc(OC)cn3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.2c00359
CHEMBL3717275 133818 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR methodAntagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR method
ChEMBL 515 8 0 11 5.3 COc1cc(OCc2cccc(-c3cnc(OC)cn3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.2c00359
72193331 133908 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR methodAntagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR method
ChEMBL 491 7 0 11 5.3 COc1cc(OCc2nsc(-c3ccccc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.2c00359
CHEMBL3717580 133908 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR methodAntagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR method
ChEMBL 491 7 0 11 5.3 COc1cc(OCc2nsc(-c3ccccc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.2c00359
89884101 133812 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 502 7 0 9 6.0 COc1cc(OCc2cccc(-c3ccc(F)cn3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3717253 133812 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 502 7 0 9 6.0 COc1cc(OCc2cccc(-c3ccc(F)cn3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72193006 134421 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 519 7 0 10 5.9 COc1cc(OCc2cncc(-c3ccc(Cl)nc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3719287 134421 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 519 7 0 10 5.9 COc1cc(OCc2cncc(-c3ccc(Cl)nc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72192423 133403 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 534 8 1 11 5.7 COc1cc(OCc2cccc(-c3nc(CO)c(C)s3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3715863 133403 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 534 8 1 11 5.7 COc1cc(OCc2cccc(-c3nc(CO)c(C)s3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
117981423 133298 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 568 8 0 12 5.3 COc1cc(OCc2csc(-c3ccc(S(C)(=O)=O)cc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3715516 133298 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 568 8 0 12 5.3 COc1cc(OCc2csc(-c3ccc(S(C)(=O)=O)cc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
89878659 134012 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 491 7 0 11 5.3 COc1cc(OCc2csc(-c3ccncc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3717956 134012 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 491 7 0 11 5.3 COc1cc(OCc2csc(-c3ccncc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118068699 135545 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 573 11 0 11 6.4 COc1cc(COc2cccc(COc3cc(OC)cc4oc(-c5cn6nc(OC)sc6n5)cc34)c2)cc(OC)c1 nan
CHEMBL3732151 135545 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 573 11 0 11 6.4 COc1cc(COc2cccc(COc3cc(OC)cc4oc(-c5cn6nc(OC)sc6n5)cc34)c2)cc(OC)c1 nan
155521862 170145 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assayAntagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assay
ChEMBL 421 6 0 8 5.1 COc1cc(OCc2ccccc2C)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.9b00186
CHEMBL4452111 170145 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assayAntagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assay
ChEMBL 421 6 0 8 5.1 COc1cc(OCc2ccccc2C)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.9b00186
155549758 173294 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assayAntagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assay
ChEMBL 437 7 0 9 4.8 COc1ccc(COc2cc(OC)cc3oc(-c4cn5nc(OC)sc5n4)cc23)cc1 10.1021/acs.jmedchem.9b00186
CHEMBL4539616 173294 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assayAntagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assay
ChEMBL 437 7 0 9 4.8 COc1ccc(COc2cc(OC)cc3oc(-c4cn5nc(OC)sc5n4)cc23)cc1 10.1021/acs.jmedchem.9b00186
118042469 134437 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 509 7 0 10 5.7 COc1cc(OCc2cccc(-c3ncccc3C#N)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3719349 134437 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 509 7 0 10 5.7 COc1cc(OCc2cccc(-c3ncccc3C#N)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118068387 135072 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 567 9 0 9 6.8 COc1cc(OCc2cccc(OCc3ccc(F)c(F)c3F)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3729253 135072 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 567 9 0 9 6.8 COc1cc(OCc2cccc(OCc3ccc(F)c(F)c3F)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118068628 135433 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 527 8 0 10 6.0 COc1cc(OCc2cccc(OC(=O)c3ccccc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3731476 135433 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 527 8 0 10 6.0 COc1cc(OCc2cccc(OC(=O)c3ccccc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72189636 133473 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 597 8 0 11 5.3 COc1cc(OCc2cccc(-c3ccc(C(=O)N4CCOCC4)nc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3716120 133473 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 597 8 0 11 5.3 COc1cc(OCc2cccc(-c3ccc(C(=O)N4CCOCC4)nc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118068638 134861 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 599 9 0 9 7.5 COc1cc(OCc2cccc(OCc3cc(F)cc(C(F)(F)F)c3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3728013 134861 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 599 9 0 9 7.5 COc1cc(OCc2cccc(OCc3cc(F)cc(C(F)(F)F)c3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72192127 133824 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 556 8 0 11 5.0 COc1cc(OCc2ccnc(-c3ccc(C(=O)N(C)C)cc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3717308 133824 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 556 8 0 11 5.0 COc1cc(OCc2ccnc(-c3ccc(C(=O)N(C)C)cc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118068697 135420 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 541 9 0 9 7.0 COc1cc(OCc2cccc(OCc3cc(C)cc(C)c3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3731383 135420 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 541 9 0 9 7.0 COc1cc(OCc2cccc(OCc3cc(C)cc(C)c3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118068392 135482 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 531 9 0 9 6.5 COc1cc(OCc2cccc(OCc3ccc(F)cc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3731766 135482 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 531 9 0 9 6.5 COc1cc(OCc2cccc(OCc3ccc(F)cc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72192711 133372 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 527 8 0 9 6.8 COc1ccc(-c2cccc(COc3cc(OC)cc4oc(-c5cn6nc(OC)sc6n5)cc34)c2)c(C)c1 nan
CHEMBL3715746 133372 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 527 8 0 9 6.8 COc1ccc(-c2cccc(COc3cc(OC)cc4oc(-c5cn6nc(OC)sc6n5)cc34)c2)c(C)c1 nan
168279438 190570 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR methodAntagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR method
ChEMBL 513 7 0 12 3.6 COc1cc(OCc2csc(N3CCOCC3=O)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.2c00359
CHEMBL5188943 190570 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR methodAntagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR method
ChEMBL 513 7 0 12 3.6 COc1cc(OCc2csc(N3CCOCC3=O)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.2c00359
71770954 133905 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 509 7 0 10 5.7 COc1cc(OCc2cccc(-c3ccc(C#N)nc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3717574 133905 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 509 7 0 10 5.7 COc1cc(OCc2cccc(-c3ccc(C#N)nc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118068398 135234 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 527 9 0 9 6.7 COc1cc(OCc2cccc(OCc3cccc(C)c3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3730270 135234 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 527 9 0 9 6.7 COc1cc(OCc2cccc(OCc3cccc(C)c3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72192129 133947 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 515 8 0 11 5.3 COc1ccc(-c2nccc(COc3cc(OC)cc4oc(-c5cn6nc(OC)sc6n5)cc34)n2)cc1 nan
CHEMBL3717703 133947 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 515 8 0 11 5.3 COc1ccc(-c2nccc(COc3cc(OC)cc4oc(-c5cn6nc(OC)sc6n5)cc34)n2)cc1 nan
72193009 133335 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR methodAntagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR method
ChEMBL 428 6 0 10 4.6 COc1cc(OCc2csc(C)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.2c00359
CHEMBL3715642 133335 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR methodAntagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR method
ChEMBL 428 6 0 10 4.6 COc1cc(OCc2csc(C)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.2c00359
155565675 175031 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assayAntagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assay
ChEMBL 451 9 0 9 4.8 COc1cc(OCCOCc2ccccc2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.9b00186
CHEMBL4580391 175031 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assayAntagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assay
ChEMBL 451 9 0 9 4.8 COc1cc(OCCOCc2ccccc2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.9b00186
72202435 135194 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 483 8 0 8 6.4 COc1nn2cc(-c3cc4c(OCc5cccc(OCc6ccccc6)c5)cccc4o3)nc2s1 nan
CHEMBL3730035 135194 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 483 8 0 8 6.4 COc1nn2cc(-c3cc4c(OCc5cccc(OCc6ccccc6)c5)cccc4o3)nc2s1 nan
89884100 133756 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 473 7 0 9 6.1 COc1cc(OCc2cccc(-c3ccoc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3717040 133756 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 473 7 0 9 6.1 COc1cc(OCc2cccc(-c3ccoc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72189338 133675 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 536 7 0 9 6.7 COc1cc(OCc2cccc(-c3ncc(Cl)cc3F)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3716806 133675 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 536 7 0 9 6.7 COc1cc(OCc2cccc(-c3ncc(Cl)cc3F)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
89878645 133491 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 508 7 0 10 6.1 COc1cc(OCc2csc(-c3ccc(F)cc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3716160 133491 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 508 7 0 10 6.1 COc1cc(OCc2csc(-c3ccc(F)cc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72192135 133709 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 570 7 1 13 4.8 COc1cc(OCc2csc(C3(O)CCC4(CC3)OCCO4)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3716904 133709 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 570 7 1 13 4.8 COc1cc(OCc2csc(C3(O)CCC4(CC3)OCCO4)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
117981420 133997 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 534 8 1 11 5.7 COc1cc(OCc2nc(-c3cccc(CO)c3)sc2C)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3717885 133997 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 534 8 1 11 5.7 COc1cc(OCc2nc(-c3cccc(CO)c3)sc2C)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
89878899 134143 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 587 8 0 11 6.2 COc1cc(OCc2csc(-c3ccc(C(=O)N4CCCC4)cc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3718360 134143 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 587 8 0 11 6.2 COc1cc(OCc2csc(-c3ccc(C(=O)N4CCCC4)cc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118068728 135113 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 501 8 0 8 6.5 COc1nn2cc(-c3cc4c(OCc5cccc(OCc6ccccc6)c5)cc(F)cc4o3)nc2s1 nan
CHEMBL3729530 135113 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 501 8 0 8 6.5 COc1nn2cc(-c3cc4c(OCc5cccc(OCc6ccccc6)c5)cc(F)cc4o3)nc2s1 nan
118068406 135653 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 531 9 0 9 6.5 COc1cc(OCc2cccc(OCc3ccccc3F)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3732786 135653 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 531 9 0 9 6.5 COc1cc(OCc2cccc(OCc3ccccc3F)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
89880960 134990 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 355 2 0 5 5.5 C[C@H](F)c1nn2cc(-c3cc4c(Cl)cc(Cl)cc4o3)nc2s1 nan
CHEMBL3728747 134990 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 355 2 0 5 5.5 C[C@H](F)c1nn2cc(-c3cc4c(Cl)cc(Cl)cc4o3)nc2s1 nan
118068472 135145 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 306 2 0 7 3.5 CSc1nn2cc(-c3nc4cc(F)ccc4o3)nc2s1 nan
CHEMBL3729720 135145 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 306 2 0 7 3.5 CSc1nn2cc(-c3nc4cc(F)ccc4o3)nc2s1 nan
118068694 135502 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 617 12 0 9 8.2 COc1cc(OCc2cccc(OCc3ccccc3CCc3ccccc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3731888 135502 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 617 12 0 9 8.2 COc1cc(OCc2cccc(OCc3ccccc3CCc3ccccc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118068403 135264 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 573 11 0 11 6.4 COc1cc(OCc2cccc(OCc3cccc(OC)c3OC)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3730469 135264 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 573 11 0 11 6.4 COc1cc(OCc2cccc(OCc3cccc(OC)c3OC)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72201420 135518 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 424 6 0 9 4.9 COc1cc(OCc2ccccc2)c2nc(-c3cn4nc(SC)sc4n3)oc2c1 nan
CHEMBL3732006 135518 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 424 6 0 9 4.9 COc1cc(OCc2ccccc2)c2nc(-c3cn4nc(SC)sc4n3)oc2c1 nan
118068463 135103 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 313 3 0 6 4.3 COc1nn2cc(-c3cc4cccc(C(C)C)c4o3)nc2s1 nan
CHEMBL3729475 135103 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 313 3 0 6 4.3 COc1nn2cc(-c3cc4cccc(C(C)C)c4o3)nc2s1 nan
118068468 134791 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 331 4 0 8 3.2 COc1nn2cc(-c3cc4c(OC)ccc(OC)c4o3)nc2s1 nan
CHEMBL3727598 134791 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 331 4 0 8 3.2 COc1nn2cc(-c3cc4c(OC)ccc(OC)c4o3)nc2s1 nan
118068448 134928 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 410 5 0 7 5.4 CCc1nn2cc(-c3nc4ccc(OCc5ccc(Cl)cc5)cc4o3)nc2s1 nan
CHEMBL3728380 134928 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 410 5 0 7 5.4 CCc1nn2cc(-c3nc4ccc(OCc5ccc(Cl)cc5)cc4o3)nc2s1 nan
118068386 135593 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 528 9 0 10 6.1 COc1cc(OCc2cccc(OCc3cccc(C)n3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3732437 135593 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 528 9 0 10 6.1 COc1cc(OCc2cccc(OCc3cccc(C)n3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118068450 135210 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 406 6 0 8 4.7 CCc1nn2cc(-c3nc4ccc(OCc5ccc(OC)cc5)cc4o3)nc2s1 nan
CHEMBL3730124 135210 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 406 6 0 8 4.7 CCc1nn2cc(-c3nc4ccc(OCc5ccc(OC)cc5)cc4o3)nc2s1 nan
118068514 134871 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 419 5 0 9 4.8 CSc1nn2cc(-c3nc4c(OCc5cccc(C#N)c5)cccc4o3)nc2s1 nan
CHEMBL3728088 134871 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 419 5 0 9 4.8 CSc1nn2cc(-c3nc4c(OCc5cccc(C#N)c5)cccc4o3)nc2s1 nan
118068435 135394 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 376 5 0 7 4.7 CCc1nn2cc(-c3nc4ccc(OCc5ccccc5)cc4o3)nc2s1 nan
CHEMBL3731210 135394 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 376 5 0 7 4.7 CCc1nn2cc(-c3nc4ccc(OCc5ccccc5)cc4o3)nc2s1 nan
118068533 135363 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 354 1 0 6 4.0 Fc1ccc2sc(-c3cn4nc(Br)sc4n3)nc2c1 nan
CHEMBL3731049 135363 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 354 1 0 6 4.0 Fc1ccc2sc(-c3cn4nc(Br)sc4n3)nc2c1 nan
72191810 133547 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 489 7 0 9 5.6 COc1cc(OCc2cccc(C3=CCOCC3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3716332 133547 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 489 7 0 9 5.6 COc1cc(OCc2cccc(C3=CCOCC3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118068714 135372 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 543 10 0 10 6.4 COc1ccc(COc2cccc(COc3cc(OC)cc4oc(-c5cn6nc(OC)sc6n5)cc34)c2)cc1 nan
CHEMBL3731102 135372 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 543 10 0 10 6.4 COc1ccc(COc2cccc(COc3cc(OC)cc4oc(-c5cn6nc(OC)sc6n5)cc34)c2)cc1 nan
118070612 135442 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 302 2 0 7 3.4 COc1nn2cc(-c3nc4ccc(C)cc4s3)nc2s1 nan
CHEMBL3731529 135442 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 302 2 0 7 3.4 COc1nn2cc(-c3nc4ccc(C)cc4s3)nc2s1 nan
118068594 135597 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 347 1 0 5 4.6 Cc1cc(C)c2cc(-c3cn4nc(Br)sc4n3)oc2c1 nan
CHEMBL3732453 135597 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 347 1 0 5 4.6 Cc1cc(C)c2cc(-c3cn4nc(Br)sc4n3)oc2c1 nan
164619381 185404 0 None 6 2 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at PAR4 in human platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in human platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 415 5 0 7 4.6 CCOCn1cnc2c(-c3nc4c(Cl)cc(OC)cc4s3)cc(C)cc2c1=O 10.1016/j.ejmech.2021.113764
CHEMBL4870185 185404 0 None 6 2 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at PAR4 in human platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in human platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 415 5 0 7 4.6 CCOCn1cnc2c(-c3nc4c(Cl)cc(OC)cc4s3)cc(C)cc2c1=O 10.1016/j.ejmech.2021.113764
118068478 135679 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 358 4 0 7 5.0 CCC(C)(C)c1ccc2oc(-c3cn4nc(SC)sc4n3)nc2c1 nan
CHEMBL3732953 135679 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 358 4 0 7 5.0 CCC(C)(C)c1ccc2oc(-c3cn4nc(SC)sc4n3)nc2c1 nan
118068638 134861 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 599 9 0 9 7.5 COc1cc(OCc2cccc(OCc3cc(F)cc(C(F)(F)F)c3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3728013 134861 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 599 9 0 9 7.5 COc1cc(OCc2cccc(OCc3cc(F)cc(C(F)(F)F)c3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118068651 135510 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 402 1 0 6 4.7 Cc1cc(C(F)(F)F)c2cc(-c3cn4nc(Br)sc4n3)oc2n1 nan
CHEMBL3731940 135510 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 402 1 0 6 4.7 Cc1cc(C(F)(F)F)c2cc(-c3cn4nc(Br)sc4n3)oc2n1 nan
118068468 134791 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assayAntagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assay
ChEMBL 331 4 0 8 3.2 COc1nn2cc(-c3cc4c(OC)ccc(OC)c4o3)nc2s1 10.1021/acs.jmedchem.9b00186
CHEMBL3727598 134791 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assayAntagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assay
ChEMBL 331 4 0 8 3.2 COc1nn2cc(-c3cc4c(OC)ccc(OC)c4o3)nc2s1 10.1021/acs.jmedchem.9b00186
72203403 134950 1 None 9 2 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assayAntagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assay
ChEMBL 287 2 0 6 3.9 CSc1nn2cc(-c3cc4ccccc4o3)nc2s1 10.1021/acs.jmedchem.9b00186
CHEMBL3728507 134950 1 None 9 2 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assayAntagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assay
ChEMBL 287 2 0 6 3.9 CSc1nn2cc(-c3cc4ccccc4o3)nc2s1 10.1021/acs.jmedchem.9b00186
155523812 170308 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assayAntagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assay
ChEMBL 441 6 0 8 5.5 COc1cc(OCc2ccc(Cl)cc2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.9b00186
CHEMBL4454407 170308 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assayAntagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assay
ChEMBL 441 6 0 8 5.5 COc1cc(OCc2ccc(Cl)cc2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.9b00186
89873374 134997 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 317 3 0 7 3.9 COc1cccc2oc(-c3cn4nc(SC)sc4n3)cc12 nan
CHEMBL3728788 134997 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 317 3 0 7 3.9 COc1cccc2oc(-c3cn4nc(SC)sc4n3)cc12 nan
118068467 135669 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 347 4 0 8 3.9 COc1ccc(OC)c2oc(-c3cn4nc(SC)sc4n3)cc12 nan
CHEMBL3732887 135669 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 347 4 0 8 3.9 COc1ccc(OC)c2oc(-c3cn4nc(SC)sc4n3)cc12 nan
89880970 135292 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assayAntagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assay
ChEMBL 270 2 1 6 3.2 CNc1nn2cc(-c3cc4ccccc4o3)nc2s1 10.1021/acs.jmedchem.9b00186
CHEMBL3730643 135292 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assayAntagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assay
ChEMBL 270 2 1 6 3.2 CNc1nn2cc(-c3cc4ccccc4o3)nc2s1 10.1021/acs.jmedchem.9b00186
72201855 135647 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 287 2 1 7 2.9 COc1nn2cc(-c3cc4c(O)cccc4o3)nc2s1 nan
CHEMBL3732750 135647 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 287 2 1 7 2.9 COc1nn2cc(-c3cc4c(O)cccc4o3)nc2s1 nan
72201424 135087 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 351 3 0 8 3.6 CC(F)(F)c1nn2cc(-c3nc4c([N+](=O)[O-])cccc4o3)nc2s1 nan
CHEMBL3729358 135087 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 351 3 0 8 3.6 CC(F)(F)c1nn2cc(-c3nc4c([N+](=O)[O-])cccc4o3)nc2s1 nan
118070670 134841 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 483 8 0 8 6.4 COc1nn2cc(-c3cc4c(OCc5ccccc5)cc(OCc5ccccc5)cc4o3)nc2s1 nan
CHEMBL3727848 134841 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 483 8 0 8 6.4 COc1nn2cc(-c3cc4c(OCc5ccccc5)cc(OCc5ccccc5)cc4o3)nc2s1 nan
118068601 134947 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 319 2 0 5 4.6 Cc1cccc2cc(-c3cn4nc(C(C)(F)F)sc4n3)oc12 nan
CHEMBL3728503 134947 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 319 2 0 5 4.6 Cc1cccc2cc(-c3cn4nc(C(C)(F)F)sc4n3)oc12 nan
118070614 135211 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 499 8 0 8 7.1 CSc1nn2cc(-c3cc4c(OCc5ccccc5)cc(OCc5ccccc5)cc4o3)nc2s1 nan
CHEMBL3730129 135211 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 499 8 0 8 7.1 CSc1nn2cc(-c3cc4c(OCc5ccccc5)cc(OCc5ccccc5)cc4o3)nc2s1 nan
118068589 135615 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 351 3 0 6 4.9 COc1cc2oc(-c3cn4nc([C@@H](C)F)sc4n3)cc2cc1Cl nan
CHEMBL3732564 135615 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 351 3 0 6 4.9 COc1cc2oc(-c3cn4nc([C@@H](C)F)sc4n3)cc2cc1Cl nan
118068505 135166 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 417 6 0 10 3.0 CSc1nn2cc(-c3nc4c(OCCN5CCOCC5)cccc4o3)nc2s1 nan
CHEMBL3729837 135166 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 417 6 0 10 3.0 CSc1nn2cc(-c3nc4c(OCCN5CCOCC5)cccc4o3)nc2s1 nan
118068527 135407 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 424 6 0 9 4.9 COc1ccc(COc2ccc3nc(-c4cn5nc(SC)sc5n4)oc3c2)cc1 nan
CHEMBL3731275 135407 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 424 6 0 9 4.9 COc1ccc(COc2ccc3nc(-c4cn5nc(SC)sc5n4)oc3c2)cc1 nan
72202284 135161 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 630 9 1 11 5.9 CSc1nn2cc(-c3nc4c(OC[C@@H]5CCCN5C(=O)[C@H](NC(=O)c5cccs5)c5ccccc5)cccc4o3)nc2s1 nan
CHEMBL3729809 135161 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 630 9 1 11 5.9 CSc1nn2cc(-c3nc4c(OC[C@@H]5CCCN5C(=O)[C@H](NC(=O)c5cccs5)c5ccccc5)cccc4o3)nc2s1 nan
126507530 179547 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Inhibition of human PAR4 expressed in HEK293 cells assessed as Ala-(L-4-F-Phe)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-induced inhibition of calcium mobilization preincubated for 30 mins followed by Ala-(L-4-F-Phe)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly stimulation by FLIPR methodInhibition of human PAR4 expressed in HEK293 cells assessed as Ala-(L-4-F-Phe)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-induced inhibition of calcium mobilization preincubated for 30 mins followed by Ala-(L-4-F-Phe)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly stimulation by FLIPR method
ChEMBL 354 3 0 3 5.5 Cc1cc(-c2ccc(Cl)cc2Cl)c2ncc(OC(F)F)nc2c1 10.1016/j.ejmech.2020.112893
CHEMBL4748806 179547 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Inhibition of human PAR4 expressed in HEK293 cells assessed as Ala-(L-4-F-Phe)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-induced inhibition of calcium mobilization preincubated for 30 mins followed by Ala-(L-4-F-Phe)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly stimulation by FLIPR methodInhibition of human PAR4 expressed in HEK293 cells assessed as Ala-(L-4-F-Phe)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-induced inhibition of calcium mobilization preincubated for 30 mins followed by Ala-(L-4-F-Phe)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly stimulation by FLIPR method
ChEMBL 354 3 0 3 5.5 Cc1cc(-c2ccc(Cl)cc2Cl)c2ncc(OC(F)F)nc2c1 10.1016/j.ejmech.2020.112893
118070618 135524 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 315 2 0 6 4.5 CSc1nn2cc(-c3cc4c(C)cc(C)cc4o3)nc2s1 nan
CHEMBL3732032 135524 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 315 2 0 6 4.5 CSc1nn2cc(-c3cc4c(C)cc(C)cc4o3)nc2s1 nan
118068726 135016 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 543 10 0 10 6.6 CSc1nn2cc(-c3cc4c(OCc5cccc(OCc6ccccc6)c5)cc(OC=O)cc4o3)nc2s1 nan
CHEMBL3728882 135016 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 543 10 0 10 6.6 CSc1nn2cc(-c3cc4c(OCc5cccc(OCc6ccccc6)c5)cc(OC=O)cc4o3)nc2s1 nan
72201993 135457 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 322 2 0 7 4.0 CSc1nn2cc(-c3cc4c(Cl)nccc4o3)nc2s1 nan
CHEMBL3731628 135457 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 322 2 0 7 4.0 CSc1nn2cc(-c3cc4c(Cl)nccc4o3)nc2s1 nan
72203406 134780 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 304 2 0 7 3.8 CSc1nn2cc(-c3nc4ccccc4s3)nc2s1 nan
CHEMBL3727495 134780 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 304 2 0 7 3.8 CSc1nn2cc(-c3nc4ccccc4s3)nc2s1 nan
118068456 135649 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 299 3 0 6 3.8 CCc1cccc2cc(-c3cn4nc(OC)sc4n3)oc12 nan
CHEMBL3732777 135649 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 299 3 0 6 3.8 CCc1cccc2cc(-c3cn4nc(OC)sc4n3)oc12 nan
118068566 135380 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 337 1 0 5 4.1 Fc1cccc2oc(-c3cn4nc(Br)sc4n3)cc12 nan
CHEMBL3731148 135380 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 337 1 0 5 4.1 Fc1cccc2oc(-c3cn4nc(Br)sc4n3)cc12 nan
118068559 135090 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 393 5 0 7 4.0 COCCOc1cccc2oc(-c3cn4nc(Br)sc4n3)cc12 nan
CHEMBL3729385 135090 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 393 5 0 7 4.0 COCCOc1cccc2oc(-c3cn4nc(Br)sc4n3)cc12 nan
118068451 134916 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 377 5 0 8 4.1 CCc1nn2cc(-c3nc4ccc(OCc5ccncc5)cc4o3)nc2s1 nan
CHEMBL3728319 134916 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 377 5 0 8 4.1 CCc1nn2cc(-c3nc4ccc(OCc5ccncc5)cc4o3)nc2s1 nan
118068421 135000 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 304 2 0 6 3.8 CCc1nn2cc(-c3nc4ccc(Cl)cc4o3)nc2s1 nan
CHEMBL3728803 135000 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 304 2 0 6 3.8 CCc1nn2cc(-c3nc4ccc(Cl)cc4o3)nc2s1 nan
118068405 135670 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 514 9 0 10 5.8 COc1cc(OCc2cccc(OCc3ccccn3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3732890 135670 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 514 9 0 10 5.8 COc1cc(OCc2cccc(OCc3ccccn3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72193327 134271 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 526 7 0 9 6.5 COc1cc(OCc2cccc(-c3ccc(C#N)c(F)c3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3718775 134271 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 526 7 0 9 6.5 COc1cc(OCc2cccc(-c3ccc(C#N)c(F)c3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72201711 135327 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 305 2 0 5 4.3 CC(F)(F)c1nn2cc(-c3cc4ccccc4o3)nc2s1 nan
CHEMBL3730850 135327 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 305 2 0 5 4.3 CC(F)(F)c1nn2cc(-c3cc4ccccc4o3)nc2s1 nan
72201991 135682 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 331 3 1 7 3.6 CSc1nn2cc(-c3cc4c(C(=O)O)cccc4o3)nc2s1 nan
CHEMBL3732971 135682 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 331 3 1 7 3.6 CSc1nn2cc(-c3cc4c(C(=O)O)cccc4o3)nc2s1 nan
72201422 134930 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 408 6 0 9 4.2 COc1cc(OCc2ccccc2)c2nc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3728392 134930 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 408 6 0 9 4.2 COc1cc(OCc2ccccc2)c2nc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72190268 133485 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 518 7 0 8 7.0 COc1cc(OCc2cccc(-c3ccc(F)cn3)c2)c2cc(-c3cn4nc([C@H](C)F)sc4n3)oc2c1 nan
CHEMBL3716146 133485 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 518 7 0 8 7.0 COc1cc(OCc2cccc(-c3ccc(F)cn3)c2)c2cc(-c3cn4nc([C@H](C)F)sc4n3)oc2c1 nan
118070664 135531 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 354 2 0 7 3.9 COc1nn2cc(-c3cc4c(C(F)(F)F)cc(C)nc4o3)nc2s1 nan
CHEMBL3732079 135531 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 354 2 0 7 3.9 COc1nn2cc(-c3cc4c(C(F)(F)F)cc(C)nc4o3)nc2s1 nan
118068502 135235 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 318 3 0 8 3.3 COc1cccc2oc(-c3cn4nc(SC)sc4n3)nc12 nan
CHEMBL3730275 135235 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 318 3 0 8 3.3 COc1cccc2oc(-c3cn4nc(SC)sc4n3)nc12 nan
118068464 135168 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 331 3 0 7 4.2 COc1ccc2c(C)c(-c3cn4nc(SC)sc4n3)oc2c1 nan
CHEMBL3729859 135168 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 331 3 0 7 4.2 COc1ccc2c(C)c(-c3cn4nc(SC)sc4n3)oc2c1 nan
72203403 134950 1 None 9 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 287 2 0 6 3.9 CSc1nn2cc(-c3cc4ccccc4o3)nc2s1 nan
CHEMBL3728507 134950 1 None 9 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 287 2 0 6 3.9 CSc1nn2cc(-c3cc4ccccc4o3)nc2s1 nan
118070648 135687 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 402 5 0 8 4.7 COc1nn2cc(-c3cc4c(OCc5cccc(C#N)c5)cccc4o3)nc2s1 nan
CHEMBL3732993 135687 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 402 5 0 8 4.7 COc1nn2cc(-c3cc4c(OCc5cccc(C#N)c5)cccc4o3)nc2s1 nan
118068419 135026 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 304 2 0 6 3.8 CCc1nn2cc(-c3nc4cc(Cl)ccc4o3)nc2s1 nan
CHEMBL3728966 135026 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 304 2 0 6 3.8 CCc1nn2cc(-c3nc4cc(Cl)ccc4o3)nc2s1 nan
118068443 135684 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 356 6 0 7 4.6 CCc1nn2cc(-c3nc4ccc(OCCC(C)C)cc4o3)nc2s1 nan
CHEMBL3732986 135684 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 356 6 0 7 4.6 CCc1nn2cc(-c3nc4ccc(OCCC(C)C)cc4o3)nc2s1 nan
126729464 135213 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 319 2 0 6 4.2 COc1nn2cc(-c3cc4cc(Cl)c(C)cc4o3)nc2s1 nan
CHEMBL3730143 135213 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 319 2 0 6 4.2 COc1nn2cc(-c3cc4cc(Cl)c(C)cc4o3)nc2s1 nan
118070603 134888 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 395 3 0 7 4.7 COc1cc(Br)cc2cc(-c3cn4nc(SC)sc4n3)oc12 nan
CHEMBL3728167 134888 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 395 3 0 7 4.7 COc1cc(Br)cc2cc(-c3cn4nc(SC)sc4n3)oc12 nan
118068496 135609 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 395 5 0 9 4.3 CSc1nn2cc(-c3nc4c(OCc5ccccn5)cccc4o3)nc2s1 nan
CHEMBL3732521 135609 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 395 5 0 9 4.3 CSc1nn2cc(-c3nc4c(OCc5ccccn5)cccc4o3)nc2s1 nan
72203547 135093 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 272 2 0 7 2.6 COc1nn2cc(-c3nc4ccccc4o3)nc2s1 nan
CHEMBL3729406 135093 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 272 2 0 7 2.6 COc1nn2cc(-c3nc4ccccc4o3)nc2s1 nan
72203403 134950 1 None 9 2 Human 7.9 pIC50 = 7.9 Functional
Inhibition of human PAR4 expressed in HEK293 cells assessed as Ala-(L-4-F-Phe)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-induced inhibition of calcium mobilization preincubated for 30 mins followed by Ala-(L-4-F-Phe)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly stimulation by FLIPR methodInhibition of human PAR4 expressed in HEK293 cells assessed as Ala-(L-4-F-Phe)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-induced inhibition of calcium mobilization preincubated for 30 mins followed by Ala-(L-4-F-Phe)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly stimulation by FLIPR method
ChEMBL 287 2 0 6 3.9 CSc1nn2cc(-c3cc4ccccc4o3)nc2s1 10.1016/j.ejmech.2020.112893
CHEMBL3728507 134950 1 None 9 2 Human 7.9 pIC50 = 7.9 Functional
Inhibition of human PAR4 expressed in HEK293 cells assessed as Ala-(L-4-F-Phe)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-induced inhibition of calcium mobilization preincubated for 30 mins followed by Ala-(L-4-F-Phe)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly stimulation by FLIPR methodInhibition of human PAR4 expressed in HEK293 cells assessed as Ala-(L-4-F-Phe)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-induced inhibition of calcium mobilization preincubated for 30 mins followed by Ala-(L-4-F-Phe)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly stimulation by FLIPR method
ChEMBL 287 2 0 6 3.9 CSc1nn2cc(-c3cc4ccccc4o3)nc2s1 10.1016/j.ejmech.2020.112893
89880974 135320 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 321 2 0 6 4.6 CSc1nn2cc(-c3cc4cccc(Cl)c4o3)nc2s1 nan
CHEMBL3730812 135320 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 321 2 0 6 4.6 CSc1nn2cc(-c3cc4cccc(Cl)c4o3)nc2s1 nan
118070613 135202 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 342 4 0 8 3.8 CSc1nn2cc(-c3cc4c(OCC#N)cccc4o3)nc2s1 nan
CHEMBL3730079 135202 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 342 4 0 8 3.8 CSc1nn2cc(-c3cc4c(OCC#N)cccc4o3)nc2s1 nan
72203545 135611 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 313 4 0 6 4.2 CCOc1cccc2cc(-c3cn4nc(CC)sc4n3)oc12 nan
CHEMBL3732531 135611 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 313 4 0 6 4.2 CCOc1cccc2cc(-c3cn4nc(CC)sc4n3)oc12 nan
118068392 135482 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 531 9 0 9 6.5 COc1cc(OCc2cccc(OCc3ccc(F)cc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3731766 135482 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 531 9 0 9 6.5 COc1cc(OCc2cccc(OCc3ccc(F)cc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118070666 135110 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 427 10 0 8 5.3 CCOC(=O)CCCCCOc1cccc2cc(-c3cn4nc(CC)sc4n3)oc12 nan
CHEMBL3729522 135110 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 427 10 0 8 5.3 CCOC(=O)CCCCCOc1cccc2cc(-c3cn4nc(CC)sc4n3)oc12 nan
89880976 134883 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 315 4 0 7 3.6 CCOc1cccc2cc(-c3cn4nc(OC)sc4n3)oc12 nan
CHEMBL3728147 134883 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 315 4 0 7 3.6 CCOc1cccc2cc(-c3cn4nc(OC)sc4n3)oc12 nan
118068425 135089 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 324 4 0 7 3.7 CCc1nn2cc(-c3cc4cccc(OCC#N)c4o3)nc2s1 nan
CHEMBL3729379 135089 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 324 4 0 7 3.7 CCc1nn2cc(-c3cc4cccc(OCC#N)c4o3)nc2s1 nan
72201708 135600 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 407 6 0 8 4.8 COc1cc(OCc2ccccc2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3732490 135600 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 407 6 0 8 4.8 COc1cc(OCc2ccccc2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118068721 135013 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 543 10 0 9 7.5 CCOc1cc(OCc2cccc(OCc3ccccc3)c2)c2cc(-c3cn4nc(SC)sc4n3)oc2c1 nan
CHEMBL3728869 135013 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 543 10 0 9 7.5 CCOc1cc(OCc2cccc(OCc3ccccc3)c2)c2cc(-c3cn4nc(SC)sc4n3)oc2c1 nan
72203549 135703 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 302 2 0 7 3.6 CSc1nn2cc(-c3nc4cc(C)ccc4o3)nc2s1 nan
CHEMBL3733105 135703 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 302 2 0 7 3.6 CSc1nn2cc(-c3nc4cc(C)ccc4o3)nc2s1 nan
118068504 134964 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 302 3 0 8 2.6 COc1ccc2nc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3728563 134964 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 302 3 0 8 2.6 COc1ccc2nc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118068396 135206 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 319 2 0 5 4.6 Cc1ccc2cc(-c3cn4nc(C(C)(F)F)sc4n3)oc2c1 nan
CHEMBL3730090 135206 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 319 2 0 5 4.6 Cc1ccc2cc(-c3cn4nc(C(C)(F)F)sc4n3)oc2c1 nan
72202583 134857 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 547 9 0 9 7.0 COc1cc(OCc2cc(Cl)cc(OCc3ccccc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3728008 134857 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 547 9 0 9 7.0 COc1cc(OCc2cc(Cl)cc(OCc3ccccc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118068709 135639 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 565 9 0 9 7.2 COc1cc(OCc2cccc(OCc3c(F)cccc3Cl)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3732678 135639 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 565 9 0 9 7.2 COc1cc(OCc2cccc(OCc3c(F)cccc3Cl)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118068583 135149 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 319 2 0 5 4.6 Cc1ccc2oc(-c3cn4nc(C(C)(F)F)sc4n3)cc2c1 nan
CHEMBL3729754 135149 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 319 2 0 5 4.6 Cc1ccc2oc(-c3cn4nc(C(C)(F)F)sc4n3)cc2c1 nan
89873174 134149 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 507 7 0 11 6.0 COc1cc(OCc2csc(-c3ccccc3)n2)c2nc(-c3cn4nc(SC)sc4n3)oc2c1 nan
CHEMBL3718382 134149 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 507 7 0 11 6.0 COc1cc(OCc2csc(-c3ccccc3)n2)c2nc(-c3cn4nc(SC)sc4n3)oc2c1 nan
118068602 134940 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 339 2 0 5 5.0 CC(F)(F)c1nn2cc(-c3cc4cc(Cl)ccc4o3)nc2s1 nan
CHEMBL3728466 134940 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 339 2 0 5 5.0 CC(F)(F)c1nn2cc(-c3cc4cc(Cl)ccc4o3)nc2s1 nan
118068432 135475 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 341 6 0 6 4.9 CCCCOc1cccc2cc(-c3cn4nc(CC)sc4n3)oc12 nan
CHEMBL3731719 135475 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 341 6 0 6 4.9 CCCCOc1cccc2cc(-c3cn4nc(CC)sc4n3)oc12 nan
72201858 135722 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 347 5 0 8 3.9 COCOc1cccc2oc(-c3cn4nc(SC)sc4n3)cc12 nan
CHEMBL3733239 135722 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 347 5 0 8 3.9 COCOc1cccc2oc(-c3cn4nc(SC)sc4n3)cc12 nan
118068656 135306 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 619 12 0 10 8.0 COc1cc(OCc2cccc(OCc3ccc(OCc4ccccc4)cc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3730704 135306 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 619 12 0 10 8.0 COc1cc(OCc2cccc(OCc3ccc(OCc4ccccc4)cc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118068431 134831 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 299 3 0 6 3.8 CCc1nn2cc(-c3cc4cc(OC)ccc4o3)nc2s1 nan
CHEMBL3727806 134831 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 299 3 0 6 3.8 CCc1nn2cc(-c3cc4cc(OC)ccc4o3)nc2s1 nan
118068503 135155 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 428 5 0 8 5.6 CSc1nn2cc(-c3nc4c(OCc5ccc(Cl)cc5)cccc4o3)nc2s1 nan
CHEMBL3729775 135155 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 428 5 0 8 5.6 CSc1nn2cc(-c3nc4c(OCc5ccc(Cl)cc5)cccc4o3)nc2s1 nan
118068507 135356 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 358 5 0 8 4.1 CSc1nn2cc(-c3nc4ccc(OCC5CC5)cc4o3)nc2s1 nan
CHEMBL3731014 135356 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 358 5 0 8 4.1 CSc1nn2cc(-c3nc4ccc(OCC5CC5)cc4o3)nc2s1 nan
89880947 135514 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 345 4 0 8 3.5 COc1nn2cc(-c3oc4c(OC)c(OC)ccc4c3C)nc2s1 nan
CHEMBL3731960 135514 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 345 4 0 8 3.5 COc1nn2cc(-c3oc4c(OC)c(OC)ccc4c3C)nc2s1 nan
43337113 135351 2 None - 1 Human 4.8 pIC50 = 4.8 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 319 1 0 5 4.0 Brc1nn2cc(-c3cc4ccccc4o3)nc2s1 nan
CHEMBL3730981 135351 2 None - 1 Human 4.8 pIC50 = 4.8 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 319 1 0 5 4.0 Brc1nn2cc(-c3cc4ccccc4o3)nc2s1 nan
118068487 135326 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 302 2 0 7 3.6 CSc1nn2cc(-c3nc4c(C)cccc4o3)nc2s1 nan
CHEMBL3730848 135326 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 302 2 0 7 3.6 CSc1nn2cc(-c3nc4c(C)cccc4o3)nc2s1 nan
72201709 135477 2 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 317 3 1 8 2.9 COc1cc(O)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3731736 135477 2 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 317 3 1 8 2.9 COc1cc(O)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118068525 135154 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 348 5 0 9 3.3 COCOc1ccc2nc(-c3cn4nc(SC)sc4n3)oc2c1 nan
CHEMBL3729770 135154 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 348 5 0 9 3.3 COCOc1ccc2nc(-c3cn4nc(SC)sc4n3)oc2c1 nan
164610439 184729 0 None 7 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at PAR4 in human platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in human platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 318 1 0 3 4.2 Cc1cc(-c2ccc(Cl)cc2Cl)c2ncn(C)c(=O)c2c1 10.1016/j.ejmech.2021.113764
CHEMBL4859532 184729 0 None 7 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at PAR4 in human platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in human platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 318 1 0 3 4.2 Cc1cc(-c2ccc(Cl)cc2Cl)c2ncn(C)c(=O)c2c1 10.1016/j.ejmech.2021.113764
118070627 135037 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 302 3 0 7 3.5 CCOc1nn2cc(-c3nc4ccccc4s3)nc2s1 nan
CHEMBL3729067 135037 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 302 3 0 7 3.5 CCOc1nn2cc(-c3nc4ccccc4s3)nc2s1 nan
118068614 134779 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 323 2 0 5 4.5 CC(F)(F)c1nn2cc(-c3cc4c(F)cccc4o3)nc2s1 nan
CHEMBL3727486 134779 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 323 2 0 5 4.5 CC(F)(F)c1nn2cc(-c3cc4c(F)cccc4o3)nc2s1 nan
89880953 134859 1 None 69 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 255 1 0 5 3.5 Cc1nn2cc(-c3cc4ccccc4o3)nc2s1 nan
CHEMBL3728010 134859 1 None 69 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 255 1 0 5 3.5 Cc1nn2cc(-c3cc4ccccc4o3)nc2s1 nan
118070523 135506 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 375 5 0 8 4.7 COc1cc(OC(C)C)c2cc(-c3cn4nc(SC)sc4n3)oc2c1 nan
CHEMBL3731917 135506 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 375 5 0 8 4.7 COc1cc(OC(C)C)c2cc(-c3cn4nc(SC)sc4n3)oc2c1 nan
89873584 135622 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assayAntagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assay
ChEMBL 331 4 0 8 3.2 COc1nn2cc(-c3cc4ccc(OC)c(OC)c4o3)nc2s1 10.1021/acs.jmedchem.9b00186
CHEMBL3732594 135622 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assayAntagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assay
ChEMBL 331 4 0 8 3.2 COc1nn2cc(-c3cc4ccc(OC)c(OC)c4o3)nc2s1 10.1021/acs.jmedchem.9b00186
89873584 135622 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 331 4 0 8 3.2 COc1nn2cc(-c3cc4ccc(OC)c(OC)c4o3)nc2s1 nan
CHEMBL3732594 135622 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 331 4 0 8 3.2 COc1nn2cc(-c3cc4ccc(OC)c(OC)c4o3)nc2s1 nan
118068644 134936 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 528 9 0 10 6.1 COc1cc(OCc2cccc(OCc3cccnc3C)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3728431 134936 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 528 9 0 10 6.1 COc1cc(OCc2cccc(OCc3cccnc3C)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118068461 134846 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 355 3 0 7 4.1 COc1nn2cc(-c3cc4cc(OC(F)(F)F)ccc4o3)nc2s1 nan
CHEMBL3727889 134846 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 355 3 0 7 4.1 COc1nn2cc(-c3cc4cc(OC(F)(F)F)ccc4o3)nc2s1 nan
72201562 135018 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 388 3 0 8 4.7 CSc1nn2cc(-c3nc4ccc(OC(F)(F)F)cc4s3)nc2s1 nan
CHEMBL3728886 135018 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 388 3 0 8 4.7 CSc1nn2cc(-c3nc4ccc(OC(F)(F)F)cc4s3)nc2s1 nan
155517852 169648 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assayAntagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assay
ChEMBL 437 7 0 9 4.8 COc1cc(OCc2ccccc2OC)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.9b00186
CHEMBL4445561 169648 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assayAntagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assay
ChEMBL 437 7 0 9 4.8 COc1cc(OCc2ccccc2OC)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.9b00186
118068454 135254 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 305 2 0 6 3.9 COc1nn2cc(-c3cc4cc(Cl)ccc4o3)nc2s1 nan
CHEMBL3730387 135254 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 305 2 0 6 3.9 COc1nn2cc(-c3cc4cc(Cl)ccc4o3)nc2s1 nan
72201563 135123 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 322 2 0 7 3.9 CSc1nn2cc(-c3nc4cc(F)ccc4s3)nc2s1 nan
CHEMBL3729596 135123 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 322 2 0 7 3.9 CSc1nn2cc(-c3nc4cc(F)ccc4s3)nc2s1 nan
118070597 134996 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 411 5 0 7 5.6 CSc1nn2cc(-c3cc4c(OCc5ccc(F)cc5)cccc4o3)nc2s1 nan
CHEMBL3728779 134996 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 411 5 0 7 5.6 CSc1nn2cc(-c3cc4c(OCc5ccc(F)cc5)cccc4o3)nc2s1 nan
118068650 135147 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 335 3 0 6 4.3 COc1ccc2cc(-c3cn4nc(C(C)(F)F)sc4n3)oc2c1 nan
CHEMBL3729726 135147 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 335 3 0 6 4.3 COc1ccc2cc(-c3cn4nc(C(C)(F)F)sc4n3)oc2c1 nan
118068641 135253 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 379 3 0 7 4.0 COc1cc(OC)c2cc(-c3cn4nc(Br)sc4n3)oc2c1 nan
CHEMBL3730384 135253 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 379 3 0 7 4.0 COc1cc(OC)c2cc(-c3cn4nc(Br)sc4n3)oc2c1 nan
164612042 184786 0 None 25 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at PAR4 in human platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in human platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 371 2 0 6 4.2 COc1cc(Cl)c2nc(-c3cc(C)cc4c(=O)n(C)cnc34)sc2c1 10.1016/j.ejmech.2021.113764
CHEMBL4860533 184786 0 None 25 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at PAR4 in human platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in human platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 371 2 0 6 4.2 COc1cc(Cl)c2nc(-c3cc(C)cc4c(=O)n(C)cnc34)sc2c1 10.1016/j.ejmech.2021.113764
118068489 135342 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 316 2 0 7 3.9 CSc1nn2cc(-c3nc4cc(C)c(C)cc4o3)nc2s1 nan
CHEMBL3730935 135342 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 316 2 0 7 3.9 CSc1nn2cc(-c3nc4cc(C)c(C)cc4o3)nc2s1 nan
72201419 135355 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 350 5 0 8 3.7 CSc1nn2cc(-c3nc4ccc(OCCF)cc4o3)nc2s1 nan
CHEMBL3731010 135355 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 350 5 0 8 3.7 CSc1nn2cc(-c3nc4ccc(OCCF)cc4o3)nc2s1 nan
155511382 168962 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assayAntagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assay
ChEMBL 349 3 0 6 5.4 c1ccc(Sc2nn3cc(-c4cc5ccccc5o4)nc3s2)cc1 10.1021/acs.jmedchem.9b00186
CHEMBL4435447 168962 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assayAntagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assay
ChEMBL 349 3 0 6 5.4 c1ccc(Sc2nn3cc(-c4cc5ccccc5o4)nc3s2)cc1 10.1021/acs.jmedchem.9b00186
118068643 135551 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 473 5 0 7 5.7 COc1cc(OCc2ccc(F)cc2)c2cc(-c3cn4nc(Br)sc4n3)oc2c1 nan
CHEMBL3732187 135551 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 473 5 0 7 5.7 COc1cc(OCc2ccc(F)cc2)c2cc(-c3cn4nc(Br)sc4n3)oc2c1 nan
118068591 135303 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 353 2 0 5 5.3 Cc1cc2oc(-c3cn4nc(C(C)(F)F)sc4n3)cc2cc1Cl nan
CHEMBL3730692 135303 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 353 2 0 5 5.3 Cc1cc2oc(-c3cn4nc(C(C)(F)F)sc4n3)cc2cc1Cl nan
117981591 133171 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 600 10 0 12 5.9 COc1cc(OCc2csc(-c3ccc(C(=O)N(C)CCC#N)cc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3715025 133171 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 600 10 0 12 5.9 COc1cc(OCc2csc(-c3ccc(C(=O)N(C)CCC#N)cc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
117981587 134351 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 615 9 1 11 6.2 COc1cc(OCc2csc(-c3ccc(C(=O)NCC(F)(F)F)cc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3719060 134351 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 615 9 1 11 6.2 COc1cc(OCc2csc(-c3ccc(C(=O)NCC(F)(F)F)cc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
89872925 134409 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 589 9 0 11 6.2 CCc1sc(-c2ccc(C(=O)N(C)C)cc2)nc1COc1cc(OC)cc2oc(-c3cn4nc(OC)sc4n3)cc12 nan
CHEMBL3719253 134409 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 589 9 0 11 6.2 CCc1sc(-c2ccc(C(=O)N(C)C)cc2)nc1COc1cc(OC)cc2oc(-c3cn4nc(OC)sc4n3)cc12 nan
89879103 135469 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 345 5 0 8 3.6 CCOc1cc(OC)cc2oc(-c3cn4nc(OC)sc4n3)cc12 nan
CHEMBL3731684 135469 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 345 5 0 8 3.6 CCOc1cc(OC)cc2oc(-c3cn4nc(OC)sc4n3)cc12 nan
72189337 133448 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 527 8 0 10 5.9 COc1cc(OCc2cccc(-c3ccc(N(C)C)nc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3716023 133448 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 527 8 0 10 5.9 COc1cc(OCc2cccc(-c3ccc(N(C)C)nc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
89884102 133225 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 498 7 0 9 6.2 COc1cc(OCc2cccc(-c3ccc(C)cn3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3715196 133225 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 498 7 0 9 6.2 COc1cc(OCc2cccc(-c3ccc(C)cn3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118068627 135393 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 609 9 0 9 7.3 COc1cc(OCc2cccc(OCc3ccc(Br)cc3F)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3731203 135393 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 609 9 0 9 7.3 COc1cc(OCc2cccc(OCc3ccc(Br)cc3F)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
12038 676 7 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 561 8 0 11 5.6 COc1nn2cc(nc2s1)c1cc2c(o1)cc(OC)cc2OCc1csc(n1)c1ccc(cc1)C(=O)N(C)C nan
72188743 676 7 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 561 8 0 11 5.6 COc1nn2cc(nc2s1)c1cc2c(o1)cc(OC)cc2OCc1csc(n1)c1ccc(cc1)C(=O)N(C)C nan
CHEMBL3716552 676 7 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 561 8 0 11 5.6 COc1nn2cc(nc2s1)c1cc2c(o1)cc(OC)cc2OCc1csc(n1)c1ccc(cc1)C(=O)N(C)C nan
DB14942 676 7 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 561 8 0 11 5.6 COc1nn2cc(nc2s1)c1cc2c(o1)cc(OC)cc2OCc1csc(n1)c1ccc(cc1)C(=O)N(C)C nan
72188746 134165 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 605 11 0 12 5.6 COCCN(C)C(=O)c1ccc(-c2nc(COc3cc(OC)cc4oc(-c5cn6nc(OC)sc6n5)cc34)cs2)cc1 nan
CHEMBL3718433 134165 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 605 11 0 12 5.6 COCCN(C)C(=O)c1ccc(-c2nc(COc3cc(OC)cc4oc(-c5cn6nc(OC)sc6n5)cc34)cs2)cc1 nan
118068596 135441 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 555 10 0 9 7.5 COc1cc(OCc2cccc(OCc3ccc(C(C)C)cc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3731508 135441 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 555 10 0 9 7.5 COc1cc(OCc2cccc(OCc3ccc(C(C)C)cc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118068645 135176 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 541 9 0 9 7.0 COc1cc(OCc2cccc(OCc3ccc(C)cc3C)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3729919 135176 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 541 9 0 9 7.0 COc1cc(OCc2cccc(OCc3ccc(C)cc3C)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72190585 133931 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 516 8 0 12 4.7 COc1cc(OCc2cncc(-c3cnc(OC)nc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3717651 133931 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 516 8 0 12 4.7 COc1cc(OCc2cncc(-c3cnc(OC)nc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118068693 135269 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 514 9 0 10 5.8 COc1cc(OCc2cccc(OCc3cccnc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3730494 135269 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 514 9 0 10 5.8 COc1cc(OCc2cccc(OCc3cccnc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
89884106 133120 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 516 8 0 12 4.7 COc1cc(OCc2cccc(-c3cnc(OC)nc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3714876 133120 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 516 8 0 12 4.7 COc1cc(OCc2cccc(-c3cnc(OC)nc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72190888 133566 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 514 8 0 10 5.9 COc1ccc(-c2cncc(COc3cc(OC)cc4oc(-c5cn6nc(OC)sc6n5)cc34)c2)cc1 nan
CHEMBL3716398 133566 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 514 8 0 10 5.9 COc1ccc(-c2cncc(COc3cc(OC)cc4oc(-c5cn6nc(OC)sc6n5)cc34)c2)cc1 nan
117981413 133141 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 509 7 0 11 5.5 COc1cc(OCc2csc(-c3ccnc(F)c3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3714941 133141 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 509 7 0 11 5.5 COc1cc(OCc2csc(-c3ccnc(F)c3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72191811 133543 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 487 7 0 8 6.8 COc1cc(OCc2cccc(C3=CCCCC3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3716313 133543 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 487 7 0 8 6.8 COc1cc(OCc2cccc(C3=CCCCC3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118068632 135413 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 500 6 0 10 5.0 COc1cc(OC[C@H]2CCCN2C(=O)OC(C)(C)C)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3731346 135413 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 500 6 0 10 5.0 COc1cc(OC[C@H]2CCCN2C(=O)OC(C)(C)C)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118068637 135586 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 543 10 0 10 6.4 COc1cc(OCc2ccc(OC)c(OCc3ccccc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3732411 135586 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 543 10 0 10 6.4 COc1cc(OCc2ccc(OC)c(OCc3ccccc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118068403 135264 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 573 11 0 11 6.4 COc1cc(OCc2cccc(OCc3cccc(OC)c3OC)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3730469 135264 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 573 11 0 11 6.4 COc1cc(OCc2cccc(OCc3cccc(OC)c3OC)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118068677 135312 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 527 10 0 9 6.8 CCOc1nn2cc(-c3cc4c(OCc5cccc(OCc6ccccc6)c5)cc(OC)cc4o3)nc2s1 nan
CHEMBL3730719 135312 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 527 10 0 9 6.8 CCOc1nn2cc(-c3cc4c(OCc5cccc(OCc6ccccc6)c5)cc(OC)cc4o3)nc2s1 nan
118068682 135098 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 605 11 0 10 8.2 COc1cc(OCc2cccc(OCc3ccc(Oc4ccccc4)cc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3729435 135098 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 605 11 0 10 8.2 COc1cc(OCc2cccc(OCc3ccc(Oc4ccccc4)cc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118068659 135207 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 549 9 0 9 6.7 COc1cc(OCc2cccc(OCc3ccc(F)cc3F)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3730097 135207 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 549 9 0 9 6.7 COc1cc(OCc2cccc(OCc3ccc(F)cc3F)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118068687 135492 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 632 11 1 10 7.6 COc1cc(OCc2cccc(OCc3cccc(NC(=O)c4ccccc4)c3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3731836 135492 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 632 11 1 10 7.6 COc1cc(OCc2cccc(OCc3cccc(NC(=O)c4ccccc4)c3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
155548776 173197 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assayAntagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assay
ChEMBL 441 6 0 8 5.5 COc1cc(OCc2ccccc2Cl)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.9b00186
CHEMBL4537548 173197 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assayAntagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assay
ChEMBL 441 6 0 8 5.5 COc1cc(OCc2ccccc2Cl)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.9b00186
72192418 134313 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 502 7 0 10 6.1 COc1cc(OCc2cccc(-c3c(C)noc3C)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3718892 134313 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 502 7 0 10 6.1 COc1cc(OCc2cccc(-c3c(C)noc3C)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
10442 3846 3 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR methodAntagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR method
ChEMBL 513 9 0 9 6.4 COc1cc(OCc2cccc(c2)OCc2ccccc2)c2c(c1)oc(c2)c1cn2c(n1)sc(n2)OC 10.1021/acs.jmedchem.2c00359
71770951 3846 3 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR methodAntagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR method
ChEMBL 513 9 0 9 6.4 COc1cc(OCc2cccc(c2)OCc2ccccc2)c2c(c1)oc(c2)c1cn2c(n1)sc(n2)OC 10.1021/acs.jmedchem.2c00359
CHEMBL3728620 3846 3 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR methodAntagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR method
ChEMBL 513 9 0 9 6.4 COc1cc(OCc2cccc(c2)OCc2ccccc2)c2c(c1)oc(c2)c1cn2c(n1)sc(n2)OC 10.1021/acs.jmedchem.2c00359
72188745 133800 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR methodAntagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR method
ChEMBL 548 8 1 11 6.2 COc1cc(OCc2csc(-c3ccc(C(C)(C)O)cc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.2c00359
CHEMBL3717195 133800 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR methodAntagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR method
ChEMBL 548 8 1 11 6.2 COc1cc(OCc2csc(-c3ccc(C(C)(C)O)cc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.2c00359
10442 3846 3 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assayAntagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assay
ChEMBL 513 9 0 9 6.4 COc1cc(OCc2cccc(c2)OCc2ccccc2)c2c(c1)oc(c2)c1cn2c(n1)sc(n2)OC 10.1021/acs.jmedchem.9b00186
71770951 3846 3 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assayAntagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assay
ChEMBL 513 9 0 9 6.4 COc1cc(OCc2cccc(c2)OCc2ccccc2)c2c(c1)oc(c2)c1cn2c(n1)sc(n2)OC 10.1021/acs.jmedchem.9b00186
CHEMBL3728620 3846 3 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assayAntagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assay
ChEMBL 513 9 0 9 6.4 COc1cc(OCc2cccc(c2)OCc2ccccc2)c2c(c1)oc(c2)c1cn2c(n1)sc(n2)OC 10.1021/acs.jmedchem.9b00186
155515625 169383 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assayAntagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assay
ChEMBL 511 9 0 8 6.6 COc1cc(OCc2cccc(CCc3ccccc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.9b00186
CHEMBL4441723 169383 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assayAntagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assay
ChEMBL 511 9 0 8 6.6 COc1cc(OCc2cccc(CCc3ccccc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.9b00186
162646586 179066 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Inhibition of human PAR4 expressed in HEK293 cells assessed as Ala-(L-4-F-Phe)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-induced inhibition of calcium mobilization preincubated for 30 mins followed by Ala-(L-4-F-Phe)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly stimulation by FLIPR methodInhibition of human PAR4 expressed in HEK293 cells assessed as Ala-(L-4-F-Phe)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-induced inhibition of calcium mobilization preincubated for 30 mins followed by Ala-(L-4-F-Phe)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly stimulation by FLIPR method
ChEMBL 588 6 1 10 6.6 COc1cnc2c(-c3nc4cc(F)c(O[C@@H]5CCC(C)(C)[C@@H]5OC(=O)Nc5ccnc(C)n5)cc4s3)cc(C)cc2n1 10.1016/j.ejmech.2020.112893
CHEMBL4743197 179066 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Inhibition of human PAR4 expressed in HEK293 cells assessed as Ala-(L-4-F-Phe)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-induced inhibition of calcium mobilization preincubated for 30 mins followed by Ala-(L-4-F-Phe)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly stimulation by FLIPR methodInhibition of human PAR4 expressed in HEK293 cells assessed as Ala-(L-4-F-Phe)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-induced inhibition of calcium mobilization preincubated for 30 mins followed by Ala-(L-4-F-Phe)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly stimulation by FLIPR method
ChEMBL 588 6 1 10 6.6 COc1cnc2c(-c3nc4cc(F)c(O[C@@H]5CCC(C)(C)[C@@H]5OC(=O)Nc5ccnc(C)n5)cc4s3)cc(C)cc2n1 10.1016/j.ejmech.2020.112893
10442 3846 3 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 513 9 0 9 6.4 COc1cc(OCc2cccc(c2)OCc2ccccc2)c2c(c1)oc(c2)c1cn2c(n1)sc(n2)OC nan
71770951 3846 3 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 513 9 0 9 6.4 COc1cc(OCc2cccc(c2)OCc2ccccc2)c2c(c1)oc(c2)c1cn2c(n1)sc(n2)OC nan
CHEMBL3728620 3846 3 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 513 9 0 9 6.4 COc1cc(OCc2cccc(c2)OCc2ccccc2)c2c(c1)oc(c2)c1cn2c(n1)sc(n2)OC nan
72193002 133775 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 545 9 0 12 5.3 COc1cc(OCc2cccc(-c3cnc(OC)nc3OC)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3717102 133775 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 545 9 0 12 5.3 COc1cc(OCc2cccc(-c3cnc(OC)nc3OC)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118068394 134824 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 527 9 0 9 6.7 COc1cc(OCc2cccc(OCc3ccccc3C)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3727781 134824 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 527 9 0 9 6.7 COc1cc(OCc2cccc(OCc3ccccc3C)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72202725 135381 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 543 10 0 10 6.4 COc1cc(COc2cc(OC)cc3oc(-c4cn5nc(OC)sc5n4)cc23)cc(OCc2ccccc2)c1 nan
CHEMBL3731160 135381 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 543 10 0 10 6.4 COc1cc(COc2cc(OC)cc3oc(-c4cn5nc(OC)sc5n4)cc23)cc(OCc2ccccc2)c1 nan
118068690 135735 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 591 9 0 9 7.1 COc1cc(OCc2cccc(OCc3ccccc3Br)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3733315 135735 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 591 9 0 9 7.1 COc1cc(OCc2cccc(OCc3ccccc3Br)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118068703 134853 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 581 9 0 9 7.4 COc1cc(OCc2cccc(OCc3cccc(C(F)(F)F)c3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3727965 134853 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 581 9 0 9 7.4 COc1cc(OCc2cccc(OCc3cccc(C(F)(F)F)c3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118068630 135659 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 567 9 0 9 6.8 COc1cc(OCc2cccc(OCc3c(F)ccc(F)c3F)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3732805 135659 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 567 9 0 9 6.8 COc1cc(OCc2cccc(OCc3c(F)ccc(F)c3F)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118068634 134975 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 547 9 0 8 7.5 COc1cc(OCc2cccc(OCc3ccccc3)c2)c2cc(-c3cn4nc(C(C)(F)F)sc4n3)oc2c1 nan
CHEMBL3728638 134975 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 547 9 0 8 7.5 COc1cc(OCc2cccc(OCc3ccccc3)c2)c2cc(-c3cn4nc(C(C)(F)F)sc4n3)oc2c1 nan
118068707 134899 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 541 9 0 9 7.0 COc1cc(OCc2cccc(OCc3ccc(C)c(C)c3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3728215 134899 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 541 9 0 9 7.0 COc1cc(OCc2cccc(OCc3ccc(C)c(C)c3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
168284282 190937 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR methodAntagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR method
ChEMBL 490 7 0 10 5.9 COc1cc(OCc2ncc(-c3ccccc3)s2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.2c00359
CHEMBL5194507 190937 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR methodAntagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR method
ChEMBL 490 7 0 10 5.9 COc1cc(OCc2ncc(-c3ccccc3)s2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.2c00359
89873480 135582 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assayAntagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assay
ChEMBL 301 3 0 7 3.2 COc1nn2cc(-c3cc4cccc(OC)c4o3)nc2s1 10.1021/acs.jmedchem.9b00186
CHEMBL3732386 135582 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assayAntagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assay
ChEMBL 301 3 0 7 3.2 COc1nn2cc(-c3cc4cccc(OC)c4o3)nc2s1 10.1021/acs.jmedchem.9b00186
89880975 135693 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 361 4 0 8 4.3 COc1ccc2c(C)c(-c3cn4nc(SC)sc4n3)oc2c1OC nan
CHEMBL3733053 135693 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 361 4 0 8 4.3 COc1ccc2c(C)c(-c3cn4nc(SC)sc4n3)oc2c1OC nan
72189034 134199 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 514 8 0 10 5.9 COc1ccc(-c2cccc(COc3cc(OC)cc4oc(-c5cn6nc(OC)sc6n5)cc34)c2)nc1 nan
CHEMBL3718564 134199 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 514 8 0 10 5.9 COc1ccc(-c2cccc(COc3cc(OC)cc4oc(-c5cn6nc(OC)sc6n5)cc34)c2)nc1 nan
72191814 133890 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 504 7 0 11 4.8 COc1cc(OCc2ccnc(-c3ccnc(F)c3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3717518 133890 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 504 7 0 11 4.8 COc1cc(OCc2ccnc(-c3ccnc(F)c3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118068658 135164 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 565 9 0 9 7.2 COc1cc(OCc2cccc(OCc3ccc(F)cc3Cl)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3729823 135164 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 565 9 0 9 7.2 COc1cc(OCc2cccc(OCc3ccc(F)cc3Cl)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118070616 135382 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 289 2 0 6 3.4 COc1nn2cc(-c3cc4cccc(F)c4o3)nc2s1 nan
CHEMBL3731161 135382 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 289 2 0 6 3.4 COc1nn2cc(-c3cc4cccc(F)c4o3)nc2s1 nan
118068442 134987 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of tissue factor-induced platelet aggregation pre-incubated for 2 mins before Cacl2 and tissue factor addition by optical or impedance aggregometryAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of tissue factor-induced platelet aggregation pre-incubated for 2 mins before Cacl2 and tissue factor addition by optical or impedance aggregometry
ChEMBL 331 4 0 8 3.2 COc1cc(OC)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3728724 134987 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of tissue factor-induced platelet aggregation pre-incubated for 2 mins before Cacl2 and tissue factor addition by optical or impedance aggregometryAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of tissue factor-induced platelet aggregation pre-incubated for 2 mins before Cacl2 and tissue factor addition by optical or impedance aggregometry
ChEMBL 331 4 0 8 3.2 COc1cc(OC)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
89881089 134881 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 281 2 0 5 4.1 c1ccc2oc(-c3cn4nc(C5CC5)sc4n3)cc2c1 nan
CHEMBL3728130 134881 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 281 2 0 5 4.1 c1ccc2oc(-c3cn4nc(C5CC5)sc4n3)cc2c1 nan
118070592 135734 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 318 2 0 7 4.1 CSc1nn2cc(-c3nc4ccc(C)cc4s3)nc2s1 nan
CHEMBL3733313 135734 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 318 2 0 7 4.1 CSc1nn2cc(-c3nc4ccc(C)cc4s3)nc2s1 nan
72193330 134064 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 502 11 0 12 4.4 COCCOCc1nc(COc2cc(OC)cc3oc(-c4cn5nc(OC)sc5n4)cc23)cs1 nan
CHEMBL3718116 134064 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 502 11 0 12 4.4 COCCOCc1nc(COc2cc(OC)cc3oc(-c4cn5nc(OC)sc5n4)cc23)cs1 nan
118068471 134999 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 322 2 0 7 4.0 CSc1nn2cc(-c3nc4cc(Cl)ccc4o3)nc2s1 nan
CHEMBL3728800 134999 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 322 2 0 7 4.0 CSc1nn2cc(-c3nc4cc(Cl)ccc4o3)nc2s1 nan
72203550 135569 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 401 6 0 9 3.8 CSc1nn2cc(-c3nc4ccc(OCCN5CCCC5)cc4o3)nc2s1 nan
CHEMBL3732304 135569 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 401 6 0 9 3.8 CSc1nn2cc(-c3nc4ccc(OCCN5CCCC5)cc4o3)nc2s1 nan
118068722 135556 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 565 10 0 9 7.7 CSc1nn2cc(-c3cc4c(OCc5cccc(OCc6ccccc6)c5)cc(OC(F)F)cc4o3)nc2s1 nan
CHEMBL3732202 135556 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 565 10 0 9 7.7 CSc1nn2cc(-c3cc4c(OCc5cccc(OCc6ccccc6)c5)cc(OC(F)F)cc4o3)nc2s1 nan
72201995 135349 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 306 2 0 7 3.3 COc1nn2cc(-c3cc4c(Cl)nccc4o3)nc2s1 nan
CHEMBL3730974 135349 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 306 2 0 7 3.3 COc1nn2cc(-c3cc4c(Cl)nccc4o3)nc2s1 nan
118070607 134909 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 361 6 0 8 4.0 COCCOc1cccc2oc(-c3cn4nc(SC)sc4n3)cc12 nan
CHEMBL3728283 134909 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 361 6 0 8 4.0 COCCOc1cccc2oc(-c3cn4nc(SC)sc4n3)cc12 nan
72203546 135177 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 288 2 0 7 3.3 CSc1nn2cc(-c3nc4ccccc4o3)nc2s1 nan
CHEMBL3729938 135177 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 288 2 0 7 3.3 CSc1nn2cc(-c3nc4ccccc4o3)nc2s1 nan
89880971 135173 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 301 2 0 6 4.2 CSc1nn2cc(-c3cc4cccc(C)c4o3)nc2s1 nan
CHEMBL3729892 135173 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 301 2 0 6 4.2 CSc1nn2cc(-c3cc4cccc(C)c4o3)nc2s1 nan
118070611 135022 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 364 4 0 9 3.8 COc1cc(OC)c2nc(-c3cn4nc(SC)sc4n3)sc2c1 nan
CHEMBL3728936 135022 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 364 4 0 9 3.8 COc1cc(OC)c2nc(-c3cn4nc(SC)sc4n3)sc2c1 nan
118068679 135229 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 522 7 0 9 5.0 COc1cc(OC[C@H]2CCCN2C(=O)c2ccc(F)cc2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3730239 135229 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 522 7 0 9 5.0 COc1cc(OC[C@H]2CCCN2C(=O)c2ccc(F)cc2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72190889 133653 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 444 6 0 9 5.4 COc1nn2cc(-c3nc4c(OCc5cccc(-c6ccoc6)c5)cccc4o3)nc2s1 nan
CHEMBL3716715 133653 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 444 6 0 9 5.4 COc1nn2cc(-c3nc4c(OCc5cccc(-c6ccoc6)c5)cccc4o3)nc2s1 nan
89881053 135633 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 301 2 0 6 4.2 CSc1nn2cc(-c3cc4ccc(C)cc4o3)nc2s1 nan
CHEMBL3732642 135633 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 301 2 0 6 4.2 CSc1nn2cc(-c3cc4ccc(C)cc4o3)nc2s1 nan
118068555 135599 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 323 2 0 5 4.5 CC(F)(F)c1nn2cc(-c3cc4ccc(F)cc4o3)nc2s1 nan
CHEMBL3732482 135599 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 323 2 0 5 4.5 CC(F)(F)c1nn2cc(-c3cc4ccc(F)cc4o3)nc2s1 nan
72202725 135381 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 543 10 0 10 6.4 COc1cc(COc2cc(OC)cc3oc(-c4cn5nc(OC)sc5n4)cc23)cc(OCc2ccccc2)c1 nan
CHEMBL3731160 135381 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 543 10 0 10 6.4 COc1cc(COc2cc(OC)cc3oc(-c4cn5nc(OC)sc5n4)cc23)cc(OCc2ccccc2)c1 nan
126729406 135358 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 339 2 0 6 4.5 COc1nn2cc(-c3cc4c(Cl)cc(Cl)cc4o3)nc2s1 nan
CHEMBL3731032 135358 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 339 2 0 6 4.5 COc1nn2cc(-c3cc4c(Cl)cc(Cl)cc4o3)nc2s1 nan
118068455 135500 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assayAntagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assay
ChEMBL 301 3 0 7 3.2 COc1ccc2oc(-c3cn4nc(OC)sc4n3)cc2c1 10.1021/acs.jmedchem.9b00186
CHEMBL3731871 135500 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assayAntagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assay
ChEMBL 301 3 0 7 3.2 COc1ccc2oc(-c3cn4nc(OC)sc4n3)cc2c1 10.1021/acs.jmedchem.9b00186
89880948 135275 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 300 3 0 7 3.2 CCc1nn2cc(-c3nc4ccc(OC)cc4o3)nc2s1 nan
CHEMBL3730518 135275 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 300 3 0 7 3.2 CCc1nn2cc(-c3nc4ccc(OC)cc4o3)nc2s1 nan
118068455 135500 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 301 3 0 7 3.2 COc1ccc2oc(-c3cn4nc(OC)sc4n3)cc2c1 nan
CHEMBL3731871 135500 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 301 3 0 7 3.2 COc1ccc2oc(-c3cn4nc(OC)sc4n3)cc2c1 nan
72190267 134098 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 536 7 0 8 7.1 COc1cc(OCc2cccc(-c3ccc(F)nc3)c2)c2cc(-c3cn4nc(C(C)(F)F)sc4n3)oc2c1 nan
CHEMBL3718243 134098 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 536 7 0 8 7.1 COc1cc(OCc2cccc(-c3ccc(F)nc3)c2)c2cc(-c3cn4nc(C(C)(F)F)sc4n3)oc2c1 nan
118068494 134823 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 394 5 0 8 4.9 CSc1nn2cc(-c3nc4c(OCc5ccccc5)cccc4o3)nc2s1 nan
CHEMBL3727779 134823 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 394 5 0 8 4.9 CSc1nn2cc(-c3nc4c(OCc5ccccc5)cccc4o3)nc2s1 nan
118068531 135709 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 334 2 0 6 4.3 Cc1cc2nc(-c3cn4nc(C(C)(F)F)sc4n3)oc2cc1C nan
CHEMBL3733155 135709 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 334 2 0 6 4.3 Cc1cc2nc(-c3cn4nc(C(C)(F)F)sc4n3)oc2cc1C nan
118070608 134983 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 393 5 0 7 5.5 CSc1nn2cc(-c3cc4cc(OCc5ccccc5)ccc4o3)nc2s1 nan
CHEMBL3728702 134983 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 393 5 0 7 5.5 CSc1nn2cc(-c3cc4cc(OCc5ccccc5)ccc4o3)nc2s1 nan
117981401 133514 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 513 7 0 12 4.5 COc1cc(OCc2csc(N3CCCOCC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3716230 133514 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 513 7 0 12 4.5 COc1cc(OCc2csc(N3CCCOCC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
89872881 133664 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 502 6 0 8 6.8 COc1cc(OCc2csc(-c3ccc(Cl)cc3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
CHEMBL3716754 133664 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 502 6 0 8 6.8 COc1cc(OCc2csc(-c3ccc(Cl)cc3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
117981460 133815 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 588 8 1 11 6.1 COc1cc(OCc2csc(C(O)(c3ccccc3)C(F)(F)F)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3717259 133815 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 588 8 1 11 6.1 COc1cc(OCc2csc(C(O)(c3ccccc3)C(F)(F)F)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118070605 135661 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 441 6 0 8 5.7 COc1cc(OCc2ccc(F)cc2)c2cc(-c3cn4nc(SC)sc4n3)oc2c1 nan
CHEMBL3732817 135661 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 441 6 0 8 5.7 COc1cc(OCc2ccc(F)cc2)c2cc(-c3cn4nc(SC)sc4n3)oc2c1 nan
118068592 135610 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 427 2 0 6 4.7 COc1cc2oc(-c3cn4nc(Br)sc4n3)cc2cc1Br nan
CHEMBL3732525 135610 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 427 2 0 6 4.7 COc1cc2oc(-c3cn4nc(Br)sc4n3)cc2cc1Br nan
72193005 134429 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 524 7 0 11 5.5 COc1cc(OCc2cccc(-c3ccc4nncn4c3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3719309 134429 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 524 7 0 11 5.5 COc1cc(OCc2cccc(-c3ccc4nncn4c3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118068481 134921 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 324 2 0 7 3.6 CSc1nn2cc(-c3nc4cc(F)c(F)cc4o3)nc2s1 nan
CHEMBL3728343 134921 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 324 2 0 7 3.6 CSc1nn2cc(-c3nc4cc(F)c(F)cc4o3)nc2s1 nan
118068585 135180 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 393 5 0 6 5.8 CC(F)c1nn2cc(-c3cc4c(OCc5ccccc5)cccc4o3)nc2s1 nan
CHEMBL3729955 135180 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 393 5 0 6 5.8 CC(F)c1nn2cc(-c3cc4c(OCc5ccccc5)cccc4o3)nc2s1 nan
89878701 133970 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 414 6 0 10 4.3 COc1cc(OCc2cscn2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3717789 133970 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 414 6 0 10 4.3 COc1cc(OCc2cscn2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118068438 135444 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 345 4 0 8 3.5 COc1cc(OC)c2c(C)c(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3731542 135444 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 345 4 0 8 3.5 COc1cc(OC)c2c(C)c(-c3cn4nc(OC)sc4n3)oc2c1 nan
117981566 133354 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 567 7 0 11 5.5 COc1cc(OCc2csc(N3CCN(c4ccc(C)cn4)CC3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
CHEMBL3715692 133354 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 567 7 0 11 5.5 COc1cc(OCc2csc(N3CCN(c4ccc(C)cn4)CC3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
118068529 135019 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 306 2 0 6 3.7 CC(F)(F)c1nn2cc(-c3nc4ccccc4o3)nc2s1 nan
CHEMBL3728918 135019 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 306 2 0 6 3.7 CC(F)(F)c1nn2cc(-c3nc4ccccc4o3)nc2s1 nan
117981552 133156 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 586 7 0 10 6.5 COc1cc(OCc2csc(N3CCN(c4cccc(Cl)c4)CC3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
CHEMBL3714991 133156 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 586 7 0 10 6.5 COc1cc(OCc2csc(N3CCN(c4cccc(Cl)c4)CC3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
72202140 135284 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 620 8 1 11 6.0 CSc1nn2cc(-c3nc4c(OC[C@@H]5CCCN5C(=O)[C@H](NC(=O)OC(C)(C)C)c5ccccc5)cccc4o3)nc2s1 nan
CHEMBL3730595 135284 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 620 8 1 11 6.0 CSc1nn2cc(-c3nc4c(OC[C@@H]5CCCN5C(=O)[C@H](NC(=O)OC(C)(C)C)c5ccccc5)cccc4o3)nc2s1 nan
89873106 133350 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 470 5 0 8 5.3 COc1cc(OCc2csc(Br)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
CHEMBL3715686 133350 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 470 5 0 8 5.3 COc1cc(OCc2csc(Br)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
118068712 135256 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 617 11 0 9 8.3 COc1nn2cc(-c3cc4c(OCc5cccc(OCc6cccc(C)c6)c5)c(Cc5ccccc5)c(OC)cc4o3)nc2s1 nan
CHEMBL3730410 135256 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 617 11 0 9 8.3 COc1nn2cc(-c3cc4c(OCc5cccc(OCc6cccc(C)c6)c5)c(Cc5ccccc5)c(OC)cc4o3)nc2s1 nan
72190891 133114 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 555 7 0 13 4.6 COc1cc(OCc2csc(N3CCC4(CC3)OCCO4)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3714842 133114 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 555 7 0 13 4.6 COc1cc(OCc2csc(N3CCC4(CC3)OCCO4)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
117981466 133506 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 502 9 0 10 6.2 CCC(F)(CC)c1nc(COc2cc(OC)cc3oc(-c4cn5nc(OC)sc5n4)cc23)cs1 nan
CHEMBL3716197 133506 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 502 9 0 10 6.2 CCC(F)(CC)c1nc(COc2cc(OC)cc3oc(-c4cn5nc(OC)sc5n4)cc23)cs1 nan
72201854 135346 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assayAntagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assay
ChEMBL 377 5 0 7 4.8 COc1nn2cc(-c3cc4c(OCc5ccccc5)cccc4o3)nc2s1 10.1021/acs.jmedchem.9b00186
CHEMBL3730957 135346 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assayAntagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assay
ChEMBL 377 5 0 7 4.8 COc1nn2cc(-c3cc4c(OCc5ccccc5)cccc4o3)nc2s1 10.1021/acs.jmedchem.9b00186
126729364 135641 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 379 3 0 7 4.0 COc1nn2cc(-c3cc4cc(Br)cc(OC)c4o3)nc2s1 nan
CHEMBL3732698 135641 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 379 3 0 7 4.0 COc1nn2cc(-c3cc4cc(Br)cc(OC)c4o3)nc2s1 nan
118068719 134910 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 515 8 1 9 6.8 CSc1nn2cc(-c3cc4c(OCc5cccc(OCc6ccccc6)c5)cc(O)cc4o3)nc2s1 nan
CHEMBL3728285 134910 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 515 8 1 9 6.8 CSc1nn2cc(-c3cc4c(OCc5cccc(OCc6ccccc6)c5)cc(O)cc4o3)nc2s1 nan
72201854 135346 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 377 5 0 7 4.8 COc1nn2cc(-c3cc4c(OCc5ccccc5)cccc4o3)nc2s1 nan
CHEMBL3730957 135346 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 377 5 0 7 4.8 COc1nn2cc(-c3cc4c(OCc5ccccc5)cccc4o3)nc2s1 nan
72193326 133624 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 529 8 0 11 5.8 COc1cc(OCc2cccc(-c3ccc([N+](=O)[O-])nc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3716601 133624 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 529 8 0 11 5.8 COc1cc(OCc2cccc(-c3ccc([N+](=O)[O-])nc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
10442 3846 3 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 513 9 0 9 6.4 COc1cc(OCc2cccc(c2)OCc2ccccc2)c2c(c1)oc(c2)c1cn2c(n1)sc(n2)OC nan
71770951 3846 3 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 513 9 0 9 6.4 COc1cc(OCc2cccc(c2)OCc2ccccc2)c2c(c1)oc(c2)c1cn2c(n1)sc(n2)OC nan
CHEMBL3728620 3846 3 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 513 9 0 9 6.4 COc1cc(OCc2cccc(c2)OCc2ccccc2)c2c(c1)oc(c2)c1cn2c(n1)sc(n2)OC nan
118070677 134891 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 372 3 0 8 4.0 COc1nn2cc(-c3nc4c(OC(F)(F)F)cccc4s3)nc2s1 nan
CHEMBL3728188 134891 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 372 3 0 8 4.0 COc1nn2cc(-c3nc4c(OC(F)(F)F)cccc4s3)nc2s1 nan
72189943 134060 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 519 7 0 9 6.4 COc1cc(OCc2cccc(-c3cncnc3)c2)c2cc(-c3cn4nc(C(C)(F)F)sc4n3)oc2c1 nan
CHEMBL3718111 134060 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 519 7 0 9 6.4 COc1cc(OCc2cccc(-c3cncnc3)c2)c2cc(-c3cn4nc(C(C)(F)F)sc4n3)oc2c1 nan
118068705 135656 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 649 13 0 11 8.0 COc1cc(COc2cccc(COc3cc(OC)cc4oc(-c5cn6nc(OC)sc6n5)cc34)c2)cc(OCc2ccccc2)c1 nan
CHEMBL3732797 135656 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 649 13 0 11 8.0 COc1cc(COc2cccc(COc3cc(OC)cc4oc(-c5cn6nc(OC)sc6n5)cc34)c2)cc(OCc2ccccc2)c1 nan
72191815 133630 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 514 7 1 12 4.3 COc1cc(OCc2csc(C3(O)CCOCC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3716623 133630 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 514 7 1 12 4.3 COc1cc(OCc2csc(C3(O)CCOCC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
117981498 133638 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 512 6 0 10 5.9 COc1cc(OCc2csc(-c3ccc4c(c3)OCO4)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
CHEMBL3716644 133638 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 512 6 0 10 5.9 COc1cc(OCc2csc(-c3ccc4c(c3)OCO4)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
118068685 134988 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 569 9 0 9 7.7 COc1cc(OCc2cccc(OCc3ccc(C(C)(C)C)cc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3728728 134988 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 569 9 0 9 7.7 COc1cc(OCc2cccc(OCc3ccc(C(C)(C)C)cc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72201568 135515 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 304 2 0 6 4.1 CC(F)c1nn2cc(-c3nc4ccccc4s3)nc2s1 nan
CHEMBL3731961 135515 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 304 2 0 6 4.1 CC(F)c1nn2cc(-c3nc4ccccc4s3)nc2s1 nan
72202139 134974 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 487 5 0 10 5.1 CSc1nn2cc(-c3nc4c(OC[C@@H]5CCCN5C(=O)OC(C)(C)C)cccc4o3)nc2s1 nan
CHEMBL3728637 134974 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 487 5 0 10 5.1 CSc1nn2cc(-c3nc4c(OC[C@@H]5CCCN5C(=O)OC(C)(C)C)cccc4o3)nc2s1 nan
118068676 135354 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 500 6 0 10 5.0 COc1cc(OC[C@@H]2CCCN2C(=O)OC(C)(C)C)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3731003 135354 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 500 6 0 10 5.0 COc1cc(OC[C@@H]2CCCN2C(=O)OC(C)(C)C)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118068660 135581 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 653 12 0 10 8.6 COc1cc(OCc2cccc(OCc3cccc(OCc4cccc(Cl)c4)c3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3732373 135581 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 653 12 0 10 8.6 COc1cc(OCc2cccc(OCc3cccc(OCc4cccc(Cl)c4)c3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
117981463 133561 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 542 8 0 10 6.4 CCC(F)(c1nc(COc2cc(OC)cc3oc(-c4cn5nc(OC)sc5n4)cc23)cs1)C(F)(F)F nan
CHEMBL3716372 133561 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 542 8 0 10 6.4 CCC(F)(c1nc(COc2cc(OC)cc3oc(-c4cn5nc(OC)sc5n4)cc23)cs1)C(F)(F)F nan
72193013 134176 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 609 8 1 12 5.3 COc1cc(OCc2csc(C3(O)CCC(C(=O)N4CCCC4)CC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3718490 134176 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 609 8 1 12 5.3 COc1cc(OCc2csc(C3(O)CCC(C(=O)N4CCCC4)CC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118068465 135476 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assayAntagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assay
ChEMBL 377 5 0 7 4.8 COc1nn2cc(-c3cc4ccc(OCc5ccccc5)cc4o3)nc2s1 10.1021/acs.jmedchem.9b00186
CHEMBL3731720 135476 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assayAntagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assay
ChEMBL 377 5 0 7 4.8 COc1nn2cc(-c3cc4ccc(OCc5ccccc5)cc4o3)nc2s1 10.1021/acs.jmedchem.9b00186
118068465 135476 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 377 5 0 7 4.8 COc1nn2cc(-c3cc4ccc(OCc5ccccc5)cc4o3)nc2s1 nan
CHEMBL3731720 135476 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 377 5 0 7 4.8 COc1nn2cc(-c3cc4ccc(OCc5ccccc5)cc4o3)nc2s1 nan
118070629 135143 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 352 6 0 7 4.4 CCc1nn2cc(-c3cc4cccc(OCCCC#N)c4o3)nc2s1 nan
CHEMBL3729701 135143 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 352 6 0 7 4.4 CCc1nn2cc(-c3cc4cccc(OCCCC#N)c4o3)nc2s1 nan
117981559 134031 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 475 6 0 9 5.5 COc1cc(OCc2csc(N3CCC[C@H]3C)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
CHEMBL3718007 134031 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 475 6 0 9 5.5 COc1cc(OCc2csc(N3CCC[C@H]3C)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
118068649 135698 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 411 5 0 6 5.9 CC(F)(F)c1nn2cc(-c3cc4c(OCc5ccccc5)cccc4o3)nc2s1 nan
CHEMBL3733083 135698 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 411 5 0 6 5.9 CC(F)(F)c1nn2cc(-c3cc4c(OCc5ccccc5)cccc4o3)nc2s1 nan
72189638 133622 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 569 8 0 11 5.7 COc1cc(OCc2cccc(-c3ccc(N4CCOCC4)nc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3716595 133622 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 569 8 0 11 5.7 COc1cc(OCc2cccc(-c3ccc(N4CCOCC4)nc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118068535 135439 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 336 2 0 6 4.5 Cc1ccc2nc(-c3cn4nc(C(C)(F)F)sc4n3)sc2c1 nan
CHEMBL3731495 135439 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 336 2 0 6 4.5 Cc1ccc2nc(-c3cn4nc(C(C)(F)F)sc4n3)sc2c1 nan
89879019 134019 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 539 7 0 12 4.9 COc1cc(OCc2nc(N3CC4CCC(C3)O4)sc2C)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3717972 134019 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 539 7 0 12 4.9 COc1cc(OCc2nc(N3CC4CCC(C3)O4)sc2C)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72191818 134249 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 542 7 1 12 5.0 COc1cc(OCc2csc(C3(O)CC(C)OC(C)C3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3718707 134249 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 542 7 1 12 5.0 COc1cc(OCc2csc(C3(O)CC(C)OC(C)C3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
89872973 134397 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 645 9 0 12 6.1 COc1cc(OCc2csc(C3(c4ccc(C(=O)N(C)C)cc4)CCOCC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3719223 134397 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 645 9 0 12 6.1 COc1cc(OCc2csc(C3(c4ccc(C(=O)N(C)C)cc4)CCOCC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
155545221 172871 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assayAntagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assay
ChEMBL 437 7 1 9 4.3 COc1cc(OCc2cccc(CO)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.9b00186
CHEMBL4529377 172871 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assayAntagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assay
ChEMBL 437 7 1 9 4.3 COc1cc(OCc2cccc(CO)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.9b00186
118068484 135307 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 302 3 0 8 2.6 COc1ccc2oc(-c3cn4nc(OC)sc4n3)nc2c1 nan
CHEMBL3730711 135307 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 302 3 0 8 2.6 COc1ccc2oc(-c3cn4nc(OC)sc4n3)nc2c1 nan
118068474 135027 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 286 2 0 7 2.9 COc1nn2cc(-c3nc4cc(C)ccc4o3)nc2s1 nan
CHEMBL3728990 135027 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 286 2 0 7 2.9 COc1nn2cc(-c3nc4cc(C)ccc4o3)nc2s1 nan
89884104 135667 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 441 6 0 7 5.9 COc1cc(OCc2ccccc2)c2cc(-c3cn4nc(C(C)(F)F)sc4n3)oc2c1 nan
CHEMBL3732884 135667 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 441 6 0 7 5.9 COc1cc(OCc2ccccc2)c2cc(-c3cn4nc(C(C)(F)F)sc4n3)oc2c1 nan
72188742 133368 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 474 7 0 11 4.4 COc1cc(OCc2cnnn2-c2ccccc2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3715728 133368 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 474 7 0 11 4.4 COc1cc(OCc2cnnn2-c2ccccc2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118070620 135629 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 395 3 0 7 4.7 COc1cc(Br)c2oc(-c3cn4nc(SC)sc4n3)cc2c1 nan
CHEMBL3732629 135629 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 395 3 0 7 4.7 COc1cc(Br)c2oc(-c3cn4nc(SC)sc4n3)cc2c1 nan
126729471 135487 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 379 3 0 7 4.0 COc1cc(Br)c2oc(-c3cn4nc(OC)sc4n3)cc2c1 nan
CHEMBL3731802 135487 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 379 3 0 7 4.0 COc1cc(Br)c2oc(-c3cn4nc(OC)sc4n3)cc2c1 nan
118068581 134778 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 427 2 0 6 4.7 COc1cc(Br)cc2cc(-c3cn4nc(Br)sc4n3)oc12 nan
CHEMBL3727478 134778 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 427 2 0 6 4.7 COc1cc(Br)cc2cc(-c3cn4nc(Br)sc4n3)oc12 nan
72188737 133705 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 516 7 0 9 6.3 COc1cc(OCc2cccc(-c3ccc(F)c(C)n3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3716899 133705 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 516 7 0 9 6.3 COc1cc(OCc2cccc(-c3ccc(F)c(C)n3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
89872701 133349 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 506 7 0 9 6.9 COc1cc(OCc2csc(-c3ccccc3)n2)c2cc(-c3cn4nc([C@H](C)F)sc4n3)oc2c1 nan
CHEMBL3715685 133349 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 506 7 0 9 6.9 COc1cc(OCc2csc(-c3ccccc3)n2)c2cc(-c3cn4nc([C@H](C)F)sc4n3)oc2c1 nan
72193014 134220 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 608 9 1 13 4.6 COc1cc(OCc2csc(C3(O)CCC(C(=O)N(C)CC#N)CC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3718626 134220 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 608 9 1 13 4.6 COc1cc(OCc2csc(C3(O)CCC(C(=O)N(C)CC#N)CC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72191505 134228 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 532 7 0 10 6.6 COc1cc(OCc2csc(C3CCC(F)(F)CC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3718639 134228 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 532 7 0 10 6.6 COc1cc(OCc2csc(C3CCC(F)(F)CC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118068453 134795 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 285 2 0 6 3.5 COc1nn2cc(-c3cc4cccc(C)c4o3)nc2s1 nan
CHEMBL3727623 134795 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 285 2 0 6 3.5 COc1nn2cc(-c3cc4cccc(C)c4o3)nc2s1 nan
118068495 134944 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 346 4 0 8 4.1 CSc1nn2cc(-c3nc4c(OC(C)C)cccc4o3)nc2s1 nan
CHEMBL3728491 134944 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 346 4 0 8 4.1 CSc1nn2cc(-c3nc4c(OC(C)C)cccc4o3)nc2s1 nan
164622285 185187 0 None 8 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at PAR4 in human platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in human platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 311 1 0 5 3.2 Cc1cc(-c2nc3c(s2)CCCC3)c2ncn(C)c(=O)c2c1 10.1016/j.ejmech.2021.113764
CHEMBL4866566 185187 0 None 8 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at PAR4 in human platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in human platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 311 1 0 5 3.2 Cc1cc(-c2nc3c(s2)CCCC3)c2ncn(C)c(=O)c2c1 10.1016/j.ejmech.2021.113764
118068571 135692 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 339 2 0 5 5.0 CC(F)(F)c1nn2cc(-c3cc4ccc(Cl)cc4o3)nc2s1 nan
CHEMBL3733049 135692 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 339 2 0 5 5.0 CC(F)(F)c1nn2cc(-c3cc4ccc(Cl)cc4o3)nc2s1 nan
118068501 135100 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 395 5 0 9 4.3 CSc1nn2cc(-c3nc4ccc(OCc5cccnc5)cc4o3)nc2s1 nan
CHEMBL3729464 135100 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 395 5 0 9 4.3 CSc1nn2cc(-c3nc4ccc(OCc5cccnc5)cc4o3)nc2s1 nan
89873725 135267 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 285 2 1 6 3.5 CCc1nn2cc(-c3cc4cccc(O)c4o3)nc2s1 nan
CHEMBL3730489 135267 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 285 2 1 6 3.5 CCc1nn2cc(-c3cc4cccc(O)c4o3)nc2s1 nan
117981468 133265 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 622 8 1 11 6.7 COc1cc(OCc2csc(C(O)(c3ccc(Cl)cc3)C(F)(F)F)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3715391 133265 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 622 8 1 11 6.7 COc1cc(OCc2csc(C(O)(c3ccc(Cl)cc3)C(F)(F)F)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118068613 134866 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 413 3 0 6 5.1 COc1cc2oc(-c3cn4nc(C(C)(F)F)sc4n3)cc2cc1Br nan
CHEMBL3728059 134866 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 413 3 0 6 5.1 COc1cc2oc(-c3cn4nc(C(C)(F)F)sc4n3)cc2cc1Br nan
118070649 134806 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 379 3 0 7 4.0 COc1nn2cc(-c3cc4c(Br)ccc(OC)c4o3)nc2s1 nan
CHEMBL3727674 134806 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 379 3 0 7 4.0 COc1nn2cc(-c3cc4c(Br)ccc(OC)c4o3)nc2s1 nan
118068572 134787 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 411 5 0 6 5.9 CC(F)(F)c1nn2cc(-c3cc4ccc(OCc5ccccc5)cc4o3)nc2s1 nan
CHEMBL3727533 134787 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 411 5 0 6 5.9 CC(F)(F)c1nn2cc(-c3cc4ccc(OCc5ccccc5)cc4o3)nc2s1 nan
118070586 169567 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assayAntagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assay
ChEMBL 301 3 0 6 4.3 CCSc1nn2cc(-c3cc4ccccc4o3)nc2s1 10.1021/acs.jmedchem.9b00186
CHEMBL4444227 169567 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assayAntagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assay
ChEMBL 301 3 0 6 4.3 CCSc1nn2cc(-c3cc4ccccc4o3)nc2s1 10.1021/acs.jmedchem.9b00186
118068440 135523 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 340 4 0 7 4.1 CCc1nn2cc(-c3nc4ccc(OC5CCC5)cc4o3)nc2s1 nan
CHEMBL3732020 135523 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 340 4 0 7 4.1 CCc1nn2cc(-c3nc4ccc(OC5CCC5)cc4o3)nc2s1 nan
118070605 135661 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 441 6 0 8 5.7 COc1cc(OCc2ccc(F)cc2)c2cc(-c3cn4nc(SC)sc4n3)oc2c1 nan
CHEMBL3732817 135661 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 441 6 0 8 5.7 COc1cc(OCc2ccc(F)cc2)c2cc(-c3cn4nc(SC)sc4n3)oc2c1 nan
118068664 134852 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 639 9 0 9 7.0 COc1cc(OCc2cccc(OCc3ccc(I)cc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3727956 134852 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 639 9 0 9 7.0 COc1cc(OCc2cccc(OCc3ccc(I)cc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
89873728 133341 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 485 7 0 10 5.3 COc1cc(OCc2cccc(-c3ncccn3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3715655 133341 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 485 7 0 10 5.3 COc1cc(OCc2cccc(-c3ncccn3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118068470 135044 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 305 2 0 6 3.9 COc1nn2cc(-c3cc4c(Cl)cccc4o3)nc2s1 nan
CHEMBL3729088 135044 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 305 2 0 6 3.9 COc1nn2cc(-c3cc4c(Cl)cccc4o3)nc2s1 nan
89881055 171934 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assayAntagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assay
ChEMBL 423 6 1 9 4.5 COc1cc(OCc2cccc(O)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.9b00186
CHEMBL4483493 171934 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assayAntagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assay
ChEMBL 423 6 1 9 4.5 COc1cc(OCc2cccc(O)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.9b00186
155543857 172637 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assayAntagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assay
ChEMBL 475 6 0 8 5.8 COc1cc(OCc2cccc(C(F)(F)F)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.9b00186
CHEMBL4523001 172637 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assayAntagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assay
ChEMBL 475 6 0 8 5.8 COc1cc(OCc2cccc(C(F)(F)F)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.9b00186
118068713 135055 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 573 11 0 11 6.4 COc1cc(OCc2cccc(OCc3c(OC)cccc3OC)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3729176 135055 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 573 11 0 11 6.4 COc1cc(OCc2cccc(OCc3c(OC)cccc3OC)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118068663 135462 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 599 9 0 9 7.5 COc1cc(OCc2cccc(OCc3ccc(F)cc3C(F)(F)F)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3731667 135462 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 599 9 0 9 7.5 COc1cc(OCc2cccc(OCc3ccc(F)cc3C(F)(F)F)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72201707 135436 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 351 3 0 7 4.6 COc1cc2oc(-c3cn4nc(SC)sc4n3)cc2cc1Cl nan
CHEMBL3731491 135436 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 351 3 0 7 4.6 COc1cc2oc(-c3cn4nc(SC)sc4n3)cc2cc1Cl nan
155530857 171012 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assayAntagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assay
ChEMBL 513 9 0 9 6.4 COc1cc(OCc2cccc(COc3ccccc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.9b00186
CHEMBL4465125 171012 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assayAntagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assay
ChEMBL 513 9 0 9 6.4 COc1cc(OCc2cccc(COc3ccccc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.9b00186
155544936 172836 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assayAntagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assay
ChEMBL 513 9 0 9 6.4 COc1cc(OCc2ccccc2OCc2ccccc2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.9b00186
CHEMBL4528562 172836 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assayAntagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assay
ChEMBL 513 9 0 9 6.4 COc1cc(OCc2ccccc2OCc2ccccc2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.9b00186
164623869 185463 0 None 52 2 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human PAR4 expressed in Ga15-HEK293 cells assessed as reduction in PAR4 AP AYPGKF-NH2-induced cytosolic calcium incubated for 24 hrs by FLIPR - calcium mobilization assayAntagonist activity at human PAR4 expressed in Ga15-HEK293 cells assessed as reduction in PAR4 AP AYPGKF-NH2-induced cytosolic calcium incubated for 24 hrs by FLIPR - calcium mobilization assay
ChEMBL 355 2 0 6 3.7 COc1cc(F)c2nc(-c3cc(C)cc4c(=O)n(C)cnc34)sc2c1 10.1016/j.ejmech.2021.113764
CHEMBL4871001 185463 0 None 52 2 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human PAR4 expressed in Ga15-HEK293 cells assessed as reduction in PAR4 AP AYPGKF-NH2-induced cytosolic calcium incubated for 24 hrs by FLIPR - calcium mobilization assayAntagonist activity at human PAR4 expressed in Ga15-HEK293 cells assessed as reduction in PAR4 AP AYPGKF-NH2-induced cytosolic calcium incubated for 24 hrs by FLIPR - calcium mobilization assay
ChEMBL 355 2 0 6 3.7 COc1cc(F)c2nc(-c3cc(C)cc4c(=O)n(C)cnc34)sc2c1 10.1016/j.ejmech.2021.113764
118068704 135621 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 581 9 0 9 7.7 COc1cc(OCc2cccc(OCc3ccc(Cl)c(Cl)c3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3732593 135621 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 581 9 0 9 7.7 COc1cc(OCc2cccc(OCc3ccc(Cl)c(Cl)c3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
147630030 171673 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assayAntagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assay
ChEMBL 441 6 0 8 5.5 COc1cc(OCc2cccc(Cl)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.9b00186
CHEMBL4474285 171673 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assayAntagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assay
ChEMBL 441 6 0 8 5.5 COc1cc(OCc2cccc(Cl)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.9b00186
118070609 135685 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 365 2 0 6 4.7 CSc1nn2cc(-c3cc4c(Br)cccc4o3)nc2s1 nan
CHEMBL3732987 135685 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 365 2 0 6 4.7 CSc1nn2cc(-c3cc4c(Br)cccc4o3)nc2s1 nan
12038 676 7 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at PAR4 in human platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in human platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 561 8 0 11 5.6 COc1nn2cc(nc2s1)c1cc2c(o1)cc(OC)cc2OCc1csc(n1)c1ccc(cc1)C(=O)N(C)C 10.1016/j.ejmech.2021.113764
72188743 676 7 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at PAR4 in human platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in human platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 561 8 0 11 5.6 COc1nn2cc(nc2s1)c1cc2c(o1)cc(OC)cc2OCc1csc(n1)c1ccc(cc1)C(=O)N(C)C 10.1016/j.ejmech.2021.113764
CHEMBL3716552 676 7 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at PAR4 in human platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in human platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 561 8 0 11 5.6 COc1nn2cc(nc2s1)c1cc2c(o1)cc(OC)cc2OCc1csc(n1)c1ccc(cc1)C(=O)N(C)C 10.1016/j.ejmech.2021.113764
DB14942 676 7 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at PAR4 in human platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in human platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 561 8 0 11 5.6 COc1nn2cc(nc2s1)c1cc2c(o1)cc(OC)cc2OCc1csc(n1)c1ccc(cc1)C(=O)N(C)C 10.1016/j.ejmech.2021.113764
118068604 135265 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 581 9 0 9 7.4 COc1cc(OCc2cccc(OCc3ccccc3C(F)(F)F)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3730470 135265 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 581 9 0 9 7.4 COc1cc(OCc2cccc(OCc3ccccc3C(F)(F)F)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72190267 134098 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 536 7 0 8 7.1 COc1cc(OCc2cccc(-c3ccc(F)nc3)c2)c2cc(-c3cn4nc(C(C)(F)F)sc4n3)oc2c1 nan
CHEMBL3718243 134098 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 536 7 0 8 7.1 COc1cc(OCc2cccc(-c3ccc(F)nc3)c2)c2cc(-c3cn4nc(C(C)(F)F)sc4n3)oc2c1 nan
118068565 134952 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 351 3 0 6 4.9 COc1cc2oc(-c3cn4nc([C@H](C)F)sc4n3)cc2cc1Cl nan
CHEMBL3728518 134952 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 351 3 0 6 4.9 COc1cc2oc(-c3cn4nc([C@H](C)F)sc4n3)cc2cc1Cl nan
155538309 171789 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assayAntagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assay
ChEMBL 475 6 0 8 5.8 COc1cc(OCc2ccccc2C(F)(F)F)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.9b00186
CHEMBL4476101 171789 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assayAntagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assay
ChEMBL 475 6 0 8 5.8 COc1cc(OCc2ccccc2C(F)(F)F)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.9b00186
118070522 135419 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 359 5 0 8 4.0 COc1cc(OC(C)C)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3731380 135419 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 359 5 0 8 4.0 COc1cc(OC(C)C)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118068605 134982 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 563 9 0 9 7.5 COc1cc(OCc2cccc(OCc3cccc4ccccc34)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3728697 134982 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 563 9 0 9 7.5 COc1cc(OCc2cccc(OCc3cccc4ccccc34)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118070672 135199 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 289 2 0 6 3.4 COc1nn2cc(-c3cc4c(F)cccc4o3)nc2s1 nan
CHEMBL3730069 135199 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 289 2 0 6 3.4 COc1nn2cc(-c3cc4c(F)cccc4o3)nc2s1 nan
118068459 135662 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 289 2 0 6 3.4 COc1nn2cc(-c3cc4cc(F)ccc4o3)nc2s1 nan
CHEMBL3732836 135662 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 289 2 0 6 3.4 COc1nn2cc(-c3cc4cc(F)ccc4o3)nc2s1 nan
72193001 134007 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 527 7 0 10 6.2 COc1cc(OCc2cccc(-c3ccc4c(c3)OCO4)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3717928 134007 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 527 7 0 10 6.2 COc1cc(OCc2cccc(-c3ccc4c(c3)OCO4)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118068608 135632 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 561 9 0 9 7.3 COc1cc(OCc2cccc(OCc3ccc(C)c(Cl)c3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3732637 135632 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 561 9 0 9 7.3 COc1cc(OCc2cccc(OCc3ccc(C)c(Cl)c3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
89881049 135124 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 317 3 0 7 3.9 COc1ccc2cc(-c3cn4nc(SC)sc4n3)oc2c1 nan
CHEMBL3729599 135124 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 317 3 0 7 3.9 COc1ccc2cc(-c3cn4nc(SC)sc4n3)oc2c1 nan
72192714 133650 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 487 7 0 10 5.2 COc1cc(OCc2cccc(-c3cnn(C)c3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3716704 133650 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 487 7 0 10 5.2 COc1cc(OCc2cccc(-c3cnn(C)c3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118068457 135671 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 305 2 0 6 3.9 COc1nn2cc(-c3cc4ccc(Cl)cc4o3)nc2s1 nan
CHEMBL3732891 135671 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 305 2 0 6 3.9 COc1nn2cc(-c3cc4ccc(Cl)cc4o3)nc2s1 nan
89878661 133323 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 520 8 0 11 5.9 COc1ccc(-c2nc(COc3cc(OC)cc4oc(-c5cn6nc(OC)sc6n5)cc34)cs2)cc1 nan
CHEMBL3715600 133323 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 520 8 0 11 5.9 COc1ccc(-c2nc(COc3cc(OC)cc4oc(-c5cn6nc(OC)sc6n5)cc34)cs2)cc1 nan
72190582 134328 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 545 9 0 12 5.3 COc1cc(COc2cc(OC)cc3oc(-c4cn5nc(OC)sc5n4)cc23)cc(-c2cnc(OC)nc2)c1 nan
CHEMBL3718990 134328 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 545 9 0 12 5.3 COc1cc(COc2cc(OC)cc3oc(-c4cn5nc(OC)sc5n4)cc23)cc(-c2cnc(OC)nc2)c1 nan
118068626 134805 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 527 9 0 9 6.7 COc1cc(OCc2ccc(C)c(OCc3ccccc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3727672 134805 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 527 9 0 9 6.7 COc1cc(OCc2ccc(C)c(OCc3ccccc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72189340 133818 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 515 8 0 11 5.3 COc1cc(OCc2cccc(-c3cnc(OC)cn3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3717275 133818 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 515 8 0 11 5.3 COc1cc(OCc2cccc(-c3cnc(OC)cn3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72192713 133551 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 504 7 0 10 6.2 COc1cc(OCc2cccc(-c3csc(C)n3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3716341 133551 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 504 7 0 10 6.2 COc1cc(OCc2cccc(-c3csc(C)n3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118068686 134978 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 597 10 0 10 7.3 COc1cc(OCc2cccc(OCc3ccc(OC(F)(F)F)cc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3728653 134978 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 597 10 0 10 7.3 COc1cc(OCc2cccc(OCc3ccc(OC(F)(F)F)cc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118042457 134068 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 539 7 0 9 7.7 COc1cc(OCc2cccc(-c3csc4ccccc34)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3718140 134068 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 539 7 0 9 7.7 COc1cc(OCc2cccc(-c3csc4ccccc34)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72192715 133435 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 519 7 0 8 6.7 COc1cc(OCc2cccc(-c3ccc(F)cc3F)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3715980 133435 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 519 7 0 8 6.7 COc1cc(OCc2cccc(-c3ccc(F)cc3F)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118068515 135447 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 348 4 0 9 3.3 COc1cc(OC)c2nc(-c3cn4nc(SC)sc4n3)oc2c1 nan
CHEMBL3731547 135447 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 348 4 0 9 3.3 COc1cc(OC)c2nc(-c3cn4nc(SC)sc4n3)oc2c1 nan
72193332 134375 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR methodAntagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR method
ChEMBL 491 7 0 11 5.3 COc1cc(OCc2nnc(-c3ccccc3)s2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.2c00359
CHEMBL3719133 134375 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR methodAntagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR method
ChEMBL 491 7 0 11 5.3 COc1cc(OCc2nnc(-c3ccccc3)s2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.2c00359
118068438 135444 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 345 4 0 8 3.5 COc1cc(OC)c2c(C)c(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3731542 135444 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 345 4 0 8 3.5 COc1cc(OC)c2c(C)c(-c3cn4nc(OC)sc4n3)oc2c1 nan
118068607 135052 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 548 9 0 10 6.4 COc1cc(OCc2cccc(OCc3ccnc(Cl)c3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3729143 135052 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 548 9 0 10 6.4 COc1cc(OCc2cccc(OCc3ccnc(Cl)c3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118070676 134942 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 322 2 0 7 3.9 CSc1nn2cc(-c3nc4ccc(F)cc4s3)nc2s1 nan
CHEMBL3728473 134942 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 322 2 0 7 3.9 CSc1nn2cc(-c3nc4ccc(F)cc4s3)nc2s1 nan
127024141 135642 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 429 3 1 7 4.8 COc1cc(O)c2cc(-c3cn4nc(C(C)(F)F)sc4n3)oc2c1Br nan
CHEMBL3732720 135642 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 429 3 1 7 4.8 COc1cc(O)c2cc(-c3cn4nc(C(C)(F)F)sc4n3)oc2c1Br nan
118068486 134781 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 462 5 0 8 5.9 CSc1nn2cc(-c3nc4c(OCc5ccc(C(F)(F)F)cc5)cccc4o3)nc2s1 nan
CHEMBL3727503 134781 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 462 5 0 8 5.9 CSc1nn2cc(-c3nc4c(OCc5ccc(C(F)(F)F)cc5)cccc4o3)nc2s1 nan
72201992 135595 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 420 5 1 7 4.9 CSc1nn2cc(-c3cc4ccc(C(=O)NCc5ccccc5)cc4o3)nc2s1 nan
CHEMBL3732445 135595 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 420 5 1 7 4.9 CSc1nn2cc(-c3cc4ccc(C(=O)NCc5ccccc5)cc4o3)nc2s1 nan
118068677 135312 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 527 10 0 9 6.8 CCOc1nn2cc(-c3cc4c(OCc5cccc(OCc6ccccc6)c5)cc(OC)cc4o3)nc2s1 nan
CHEMBL3730719 135312 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 527 10 0 9 6.8 CCOc1nn2cc(-c3cc4c(OCc5cccc(OCc6ccccc6)c5)cc(OC)cc4o3)nc2s1 nan
118068473 135081 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 286 2 0 7 2.9 COc1nn2cc(-c3nc4c(C)cccc4o3)nc2s1 nan
CHEMBL3729340 135081 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 286 2 0 7 2.9 COc1nn2cc(-c3nc4c(C)cccc4o3)nc2s1 nan
117981528 133892 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 498 8 1 10 5.5 COc1cc(OCc2csc(NCc3cccnc3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
CHEMBL3717529 133892 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 498 8 1 10 5.5 COc1cc(OCc2csc(NCc3cccnc3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
118042476 133511 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 470 6 0 8 6.6 CSc1nn2cc(-c3nc4c(OCc5ccccc5-c5ccccc5)cccc4o3)nc2s1 nan
CHEMBL3716224 133511 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 470 6 0 8 6.6 CSc1nn2cc(-c3nc4c(OCc5ccccc5-c5ccccc5)cccc4o3)nc2s1 nan
118068640 135598 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 427 2 0 6 4.7 COc1ccc(Br)c2cc(-c3cn4nc(Br)sc4n3)oc12 nan
CHEMBL3732471 135598 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 427 2 0 6 4.7 COc1ccc(Br)c2cc(-c3cn4nc(Br)sc4n3)oc12 nan
118068584 135425 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 393 5 0 6 5.8 CC(F)c1nn2cc(-c3cc4ccc(OCc5ccccc5)cc4o3)nc2s1 nan
CHEMBL3731418 135425 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 393 5 0 6 5.8 CC(F)c1nn2cc(-c3cc4ccc(OCc5ccccc5)cc4o3)nc2s1 nan
118070619 135313 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 425 6 0 8 4.9 COc1cc(OCc2ccc(F)cc2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3730755 135313 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 425 6 0 8 4.9 COc1cc(OCc2ccc(F)cc2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118068480 135740 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 328 2 0 7 3.9 COc1nn2cc(-c3nc4cc(C(C)(C)C)ccc4o3)nc2s1 nan
CHEMBL3733348 135740 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 328 2 0 7 3.9 COc1nn2cc(-c3nc4cc(C(C)(C)C)ccc4o3)nc2s1 nan
72201857 135426 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 303 2 1 7 3.6 CSc1nn2cc(-c3cc4c(O)cccc4o3)nc2s1 nan
CHEMBL3731424 135426 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 303 2 1 7 3.6 CSc1nn2cc(-c3cc4c(O)cccc4o3)nc2s1 nan
118068611 135010 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 337 1 0 5 4.1 Fc1cccc2cc(-c3cn4nc(Br)sc4n3)oc12 nan
CHEMBL3728858 135010 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 337 1 0 5 4.1 Fc1cccc2cc(-c3cn4nc(Br)sc4n3)oc12 nan
72202581 134837 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 547 9 0 9 7.0 COc1nn2cc(-c3cc4c(OCc5cccc(OCc6ccccc6)c5)cc(OC)c(Cl)c4o3)nc2s1 nan
CHEMBL3727827 134837 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 547 9 0 9 7.0 COc1nn2cc(-c3cc4c(OCc5cccc(OCc6ccccc6)c5)cc(OC)c(Cl)c4o3)nc2s1 nan
118068628 135433 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 527 8 0 10 6.0 COc1cc(OCc2cccc(OC(=O)c3ccccc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3731476 135433 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 527 8 0 10 6.0 COc1cc(OCc2cccc(OC(=O)c3ccccc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
89880961 135650 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 355 2 0 5 5.5 C[C@@H](F)c1nn2cc(-c3cc4c(Cl)cc(Cl)cc4o3)nc2s1 nan
CHEMBL3732780 135650 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 355 2 0 5 5.5 C[C@@H](F)c1nn2cc(-c3cc4c(Cl)cc(Cl)cc4o3)nc2s1 nan
118068466 135567 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 315 2 0 6 4.5 CSc1nn2cc(-c3cc4ccc(C)c(C)c4o3)nc2s1 nan
CHEMBL3732288 135567 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 315 2 0 6 4.5 CSc1nn2cc(-c3cc4ccc(C)c(C)c4o3)nc2s1 nan
118068498 135132 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 430 5 0 8 5.2 CSc1nn2cc(-c3nc4ccc(OCc5cc(F)cc(F)c5)cc4o3)nc2s1 nan
CHEMBL3729637 135132 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 430 5 0 8 5.2 CSc1nn2cc(-c3nc4ccc(OCc5cc(F)cc(F)c5)cc4o3)nc2s1 nan
118068441 135287 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 382 5 0 7 5.1 CCc1nn2cc(-c3nc4ccc(OCC5CCCCC5)cc4o3)nc2s1 nan
CHEMBL3730606 135287 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 382 5 0 7 5.1 CCc1nn2cc(-c3nc4ccc(OCC5CCCCC5)cc4o3)nc2s1 nan
118068682 135098 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 605 11 0 10 8.2 COc1cc(OCc2cccc(OCc3ccc(Oc4ccccc4)cc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3729435 135098 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 605 11 0 10 8.2 COc1cc(OCc2cccc(OCc3ccc(Oc4ccccc4)cc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118068499 135638 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 462 5 0 8 5.9 CSc1nn2cc(-c3nc4ccc(OCc5ccc(C(F)(F)F)cc5)cc4o3)nc2s1 nan
CHEMBL3732661 135638 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 462 5 0 8 5.9 CSc1nn2cc(-c3nc4ccc(OCc5ccc(C(F)(F)F)cc5)cc4o3)nc2s1 nan
72201561 134934 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 321 2 1 7 3.3 CC(F)(F)c1nn2cc(-c3nc4c(N)cccc4o3)nc2s1 nan
CHEMBL3728411 134934 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 321 2 1 7 3.3 CC(F)(F)c1nn2cc(-c3nc4c(N)cccc4o3)nc2s1 nan
118068685 134988 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 569 9 0 9 7.7 COc1cc(OCc2cccc(OCc3ccc(C(C)(C)C)cc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3728728 134988 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 569 9 0 9 7.7 COc1cc(OCc2cccc(OCc3ccc(C(C)(C)C)cc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
89873600 134777 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 288 2 0 7 3.1 COc1nn2cc(-c3nc4ccccc4s3)nc2s1 nan
CHEMBL3727477 134777 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 288 2 0 7 3.1 COc1nn2cc(-c3nc4ccccc4s3)nc2s1 nan
118068406 135653 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 531 9 0 9 6.5 COc1cc(OCc2cccc(OCc3ccccc3F)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3732786 135653 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 531 9 0 9 6.5 COc1cc(OCc2cccc(OCc3ccccc3F)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118068424 135138 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 288 2 0 6 3.3 CCc1nn2cc(-c3nc4cc(F)ccc4o3)nc2s1 nan
CHEMBL3729657 135138 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 288 2 0 6 3.3 CCc1nn2cc(-c3nc4cc(F)ccc4o3)nc2s1 nan
118068610 134798 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 343 2 0 5 4.6 Fc1ccc2cc(-c3cn4nc(C(F)(F)Cl)sc4n3)oc2c1 nan
CHEMBL3727642 134798 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 343 2 0 5 4.6 Fc1ccc2cc(-c3cn4nc(C(F)(F)Cl)sc4n3)oc2c1 nan
89881052 134935 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 317 3 0 7 3.9 COc1ccc2oc(-c3cn4nc(SC)sc4n3)cc2c1 nan
CHEMBL3728417 134935 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 317 3 0 7 3.9 COc1ccc2oc(-c3cn4nc(SC)sc4n3)cc2c1 nan
89880953 134859 1 None 69 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assayAntagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assay
ChEMBL 255 1 0 5 3.5 Cc1nn2cc(-c3cc4ccccc4o3)nc2s1 10.1021/acs.jmedchem.9b00186
CHEMBL3728010 134859 1 None 69 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assayAntagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assay
ChEMBL 255 1 0 5 3.5 Cc1nn2cc(-c3cc4ccccc4o3)nc2s1 10.1021/acs.jmedchem.9b00186
118068574 135321 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 337 1 0 5 4.1 Fc1ccc2cc(-c3cn4nc(Br)sc4n3)oc2c1 nan
CHEMBL3730813 135321 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 337 1 0 5 4.1 Fc1ccc2cc(-c3cn4nc(Br)sc4n3)oc2c1 nan
118068670 135385 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 531 9 0 9 6.5 COc1cc(OCc2cccc(OCc3cccc(F)c3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3731170 135385 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 531 9 0 9 6.5 COc1cc(OCc2cccc(OCc3cccc(F)c3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72202431 135109 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 513 9 0 9 6.4 COc1cc(OCc2cccc(OCc3ccccc3)c2)c2oc(-c3cn4nc(OC)sc4n3)cc2c1 nan
CHEMBL3729520 135109 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 513 9 0 9 6.4 COc1cc(OCc2cccc(OCc3ccccc3)c2)c2oc(-c3cn4nc(OC)sc4n3)cc2c1 nan
89878640 133317 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 495 7 0 12 5.2 COc1cc(OCc2csc(-c3cc(C)on3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3715578 133317 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 495 7 0 12 5.2 COc1cc(OCc2csc(-c3cc(C)on3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
89880954 135076 1 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assayAntagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assay
ChEMBL 269 2 0 5 3.8 CCc1nn2cc(-c3cc4ccccc4o3)nc2s1 10.1021/acs.jmedchem.9b00186
CHEMBL3729282 135076 1 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assayAntagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assay
ChEMBL 269 2 0 5 3.8 CCc1nn2cc(-c3cc4ccccc4o3)nc2s1 10.1021/acs.jmedchem.9b00186
123271515 135655 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 316 3 0 8 3.1 COc1nn2cc(-c3cc4ccc([N+](=O)[O-])cc4o3)nc2s1 nan
CHEMBL3732794 135655 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 316 3 0 8 3.1 COc1nn2cc(-c3cc4ccc([N+](=O)[O-])cc4o3)nc2s1 nan
118068394 134824 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 527 9 0 9 6.7 COc1cc(OCc2cccc(OCc3ccccc3C)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3727781 134824 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 527 9 0 9 6.7 COc1cc(OCc2cccc(OCc3ccccc3C)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118068700 135111 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 637 12 0 10 8.1 COc1cc(OCc2cccc(OCc3cc(F)cc(OCc4ccccc4)c3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3729523 135111 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 637 12 0 10 8.1 COc1cc(OCc2cccc(OCc3cc(F)cc(OCc4ccccc4)c3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118068479 135200 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 300 2 0 7 3.2 COc1nn2cc(-c3nc4cc(C)c(C)cc4o3)nc2s1 nan
CHEMBL3730074 135200 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 300 2 0 7 3.2 COc1nn2cc(-c3nc4cc(C)c(C)cc4o3)nc2s1 nan
72203548 135220 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 270 1 0 6 3.2 Cc1ccc2oc(-c3cn4nc(C)sc4n3)nc2c1 nan
CHEMBL3730194 135220 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 270 1 0 6 3.2 Cc1ccc2oc(-c3cn4nc(C)sc4n3)nc2c1 nan
118068557 135244 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 339 2 0 5 4.8 Cc1ccc2cc(-c3cn4nc(C(F)(F)Cl)sc4n3)oc2c1 nan
CHEMBL3730335 135244 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 339 2 0 5 4.8 Cc1ccc2cc(-c3cn4nc(C(F)(F)Cl)sc4n3)oc2c1 nan
127037106 135360 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 499 8 0 8 7.1 CSc1nn2cc(-c3cc4c(OCc5cccc(OCc6ccccc6)c5)cccc4o3)nc2s1 nan
CHEMBL3731038 135360 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 499 8 0 8 7.1 CSc1nn2cc(-c3cc4c(OCc5cccc(OCc6ccccc6)c5)cccc4o3)nc2s1 nan
118068530 135678 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 500 8 0 9 6.5 CSc1nn2cc(-c3nc4c(OCc5cccc(OCc6ccccc6)c5)cccc4o3)nc2s1 nan
CHEMBL3732951 135678 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 500 8 0 9 6.5 CSc1nn2cc(-c3nc4c(OCc5cccc(OCc6ccccc6)c5)cccc4o3)nc2s1 nan
118068526 135541 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 348 5 0 9 3.3 COCOc1cccc2oc(-c3cn4nc(SC)sc4n3)nc12 nan
CHEMBL3732137 135541 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 348 5 0 9 3.3 COCOc1cccc2oc(-c3cn4nc(SC)sc4n3)nc12 nan
118068449 135576 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 342 5 0 7 4.2 CCc1nn2cc(-c3nc4ccc(OCC(C)C)cc4o3)nc2s1 nan
CHEMBL3732354 135576 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 342 5 0 7 4.2 CCc1nn2cc(-c3nc4ccc(OCC(C)C)cc4o3)nc2s1 nan
89881085 134796 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 328 5 0 7 4.0 CCCOc1ccc2nc(-c3cn4nc(CC)sc4n3)oc2c1 nan
CHEMBL3727624 134796 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 328 5 0 7 4.0 CCCOc1ccc2nc(-c3cn4nc(CC)sc4n3)oc2c1 nan
118068436 134799 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 371 3 0 7 4.8 CSc1nn2cc(-c3cc4cccc(OC(F)(F)F)c4o3)nc2s1 nan
CHEMBL3727643 134799 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 371 3 0 7 4.8 CSc1nn2cc(-c3cc4cccc(OC(F)(F)F)c4o3)nc2s1 nan
168285337 190860 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR methodAntagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR method
ChEMBL 490 7 0 10 5.9 COc1cc(OCc2cnc(-c3ccccc3)s2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.2c00359
CHEMBL5193311 190860 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR methodAntagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR method
ChEMBL 490 7 0 10 5.9 COc1cc(OCc2cnc(-c3ccccc3)s2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.2c00359
89873469 147142 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assayAntagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assay
ChEMBL 271 2 0 6 3.2 COc1nn2cc(-c3cc4ccccc4o3)nc2s1 10.1021/acs.jmedchem.9b00186
CHEMBL3931873 147142 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assayAntagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assay
ChEMBL 271 2 0 6 3.2 COc1nn2cc(-c3cc4ccccc4o3)nc2s1 10.1021/acs.jmedchem.9b00186
72189943 134060 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 519 7 0 9 6.4 COc1cc(OCc2cccc(-c3cncnc3)c2)c2cc(-c3cn4nc(C(C)(F)F)sc4n3)oc2c1 nan
CHEMBL3718111 134060 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 519 7 0 9 6.4 COc1cc(OCc2cccc(-c3cncnc3)c2)c2cc(-c3cn4nc(C(C)(F)F)sc4n3)oc2c1 nan
118070543 135631 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 423 6 0 8 5.5 COc1cc(OCc2ccccc2)c2cc(-c3cn4nc(SC)sc4n3)oc2c1 nan
CHEMBL3732636 135631 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 423 6 0 8 5.5 COc1cc(OCc2ccccc2)c2cc(-c3cn4nc(SC)sc4n3)oc2c1 nan
118068691 135370 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 621 10 0 10 7.2 COc1cc(OCc2cccc(OCc3cc(Br)ccc3OC)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3731085 135370 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 621 10 0 10 7.2 COc1cc(OCc2cccc(OCc3cc(Br)ccc3OC)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118068668 134870 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 599 9 0 9 7.5 COc1cc(OCc2cccc(OCc3cccc(C(F)(F)F)c3F)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3728073 134870 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 599 9 0 9 7.5 COc1cc(OCc2cccc(OCc3cccc(C(F)(F)F)c3F)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72189940 133611 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 584 8 0 11 6.8 COc1cc(OCc2cccc(-c3ccc(C(=O)OC(C)(C)C)nc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3716559 133611 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 584 8 0 11 6.8 COc1cc(OCc2cccc(-c3ccc(C(=O)OC(C)(C)C)nc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72201708 135600 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR methodAntagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR method
ChEMBL 407 6 0 8 4.8 COc1cc(OCc2ccccc2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.2c00359
CHEMBL3732490 135600 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR methodAntagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR method
ChEMBL 407 6 0 8 4.8 COc1cc(OCc2ccccc2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.2c00359
72201708 135600 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assayAntagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assay
ChEMBL 407 6 0 8 4.8 COc1cc(OCc2ccccc2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.9b00186
CHEMBL3732490 135600 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assayAntagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assay
ChEMBL 407 6 0 8 4.8 COc1cc(OCc2ccccc2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.9b00186
118070615 135080 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 305 2 0 6 4.1 CSc1nn2cc(-c3cc4c(F)cccc4o3)nc2s1 nan
CHEMBL3729338 135080 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 305 2 0 6 4.1 CSc1nn2cc(-c3cc4c(F)cccc4o3)nc2s1 nan
118042461 134036 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 498 7 0 9 6.2 COc1cc(OCc2cccc(-c3ccnc(C)c3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3718033 134036 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 498 7 0 9 6.2 COc1cc(OCc2cccc(-c3ccnc(C)c3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
155523135 170176 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assayAntagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assay
ChEMBL 475 6 0 8 5.8 COc1cc(OCc2ccc(C(F)(F)F)cc2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.9b00186
CHEMBL4452516 170176 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assayAntagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assay
ChEMBL 475 6 0 8 5.8 COc1cc(OCc2ccc(C(F)(F)F)cc2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.9b00186
72192416 133860 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 551 7 0 8 7.5 COc1cc(OCc2cccc(-c3cccc(C(F)(F)F)c3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3717423 133860 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 551 7 0 8 7.5 COc1cc(OCc2cccc(-c3cccc(C(F)(F)F)c3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72201706 135616 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 335 3 0 7 3.9 COc1nn2cc(-c3cc4cc(Cl)c(OC)cc4o3)nc2s1 nan
CHEMBL3732565 135616 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 335 3 0 7 3.9 COc1nn2cc(-c3cc4cc(Cl)c(OC)cc4o3)nc2s1 nan
72192416 133860 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR methodAntagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR method
ChEMBL 551 7 0 8 7.5 COc1cc(OCc2cccc(-c3cccc(C(F)(F)F)c3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.2c00359
CHEMBL3717423 133860 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR methodAntagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR method
ChEMBL 551 7 0 8 7.5 COc1cc(OCc2cccc(-c3cccc(C(F)(F)F)c3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.2c00359
118068587 134782 1 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 349 2 0 6 4.0 COc1ccc2cc(-c3cn4nc(Br)sc4n3)oc2c1 nan
CHEMBL3727514 134782 1 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 349 2 0 6 4.0 COc1ccc2cc(-c3cn4nc(Br)sc4n3)oc2c1 nan
118068629 134981 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 567 9 0 9 6.8 COc1cc(OCc2cccc(OCc3cc(F)c(F)c(F)c3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3728680 134981 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 567 9 0 9 6.8 COc1cc(OCc2cccc(OCc3cc(F)c(F)c(F)c3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118070674 135517 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 595 9 0 9 7.7 COc1cc(OCc2cccc(OCc3cc(C(F)(F)F)ccc3C)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3731983 135517 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 595 9 0 9 7.7 COc1cc(OCc2cccc(OCc3cc(C(F)(F)F)ccc3C)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72202433 135112 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 511 9 0 8 6.9 CCc1cc(OCc2cccc(OCc3ccccc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3729525 135112 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 511 9 0 8 6.9 CCc1cc(OCc2cccc(OCc3ccccc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118070601 135713 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 395 3 0 7 4.7 COc1cc2oc(-c3cn4nc(SC)sc4n3)cc2cc1Br nan
CHEMBL3733175 135713 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 395 3 0 7 4.7 COc1cc2oc(-c3cn4nc(SC)sc4n3)cc2cc1Br nan
72190266 133180 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 536 7 0 8 7.1 COc1cc(OCc2cccc(-c3ccc(F)cn3)c2)c2cc(-c3cn4nc(C(C)(F)F)sc4n3)oc2c1 nan
CHEMBL3715054 133180 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 536 7 0 8 7.1 COc1cc(OCc2cccc(-c3ccc(F)cn3)c2)c2cc(-c3cn4nc(C(C)(F)F)sc4n3)oc2c1 nan
118068727 135182 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 527 10 0 9 6.8 CCOc1cc(OCc2cccc(OCc3ccccc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3729962 135182 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 527 10 0 9 6.8 CCOc1cc(OCc2cccc(OCc3ccccc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72202726 135308 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 517 8 0 8 7.0 COc1cc(OCc2cccc(OCc3ccccc3)c2)c2cc(-c3cn4nc(Cl)sc4n3)oc2c1 nan
CHEMBL3730712 135308 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 517 8 0 8 7.0 COc1cc(OCc2cccc(OCc3ccccc3)c2)c2cc(-c3cn4nc(Cl)sc4n3)oc2c1 nan
118068657 135663 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 581 9 0 9 7.7 COc1cc(OCc2cccc(OCc3c(Cl)cccc3Cl)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3732840 135663 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 581 9 0 9 7.7 COc1cc(OCc2cccc(OCc3c(Cl)cccc3Cl)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
71769562 133398 1 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 490 7 0 10 5.9 COc1cc(OCc2csc(-c3ccccc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3715848 133398 1 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 490 7 0 10 5.9 COc1cc(OCc2csc(-c3ccccc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118068381 135564 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 285 2 0 6 3.5 COc1nn2cc(-c3cc4ccc(C)cc4o3)nc2s1 nan
CHEMBL3732276 135564 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 285 2 0 6 3.5 COc1nn2cc(-c3cc4ccc(C)cc4o3)nc2s1 nan
72189638 133622 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 569 8 0 11 5.7 COc1cc(OCc2cccc(-c3ccc(N4CCOCC4)nc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3716595 133622 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 569 8 0 11 5.7 COc1cc(OCc2cccc(-c3ccc(N4CCOCC4)nc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118068723 135727 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 501 8 0 8 6.5 COc1nn2cc(-c3cc4c(F)cc(OCc5cccc(OCc6ccccc6)c5)cc4o3)nc2s1 nan
CHEMBL3733272 135727 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 501 8 0 8 6.5 COc1nn2cc(-c3cc4c(F)cc(OCc5cccc(OCc6ccccc6)c5)cc4o3)nc2s1 nan
118068624 135428 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 317 3 0 6 4.2 COc1ccc2cc(-c3cn4nc(C(C)F)sc4n3)oc2c1 nan
CHEMBL3731434 135428 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 317 3 0 6 4.2 COc1ccc2cc(-c3cn4nc(C(C)F)sc4n3)oc2c1 nan
71770954 133905 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 509 7 0 10 5.7 COc1cc(OCc2cccc(-c3ccc(C#N)nc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3717574 133905 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 509 7 0 10 5.7 COc1cc(OCc2cccc(-c3ccc(C#N)nc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72191501 133889 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 499 7 1 9 6.2 COc1cc(OCc2cccc(-c3ccc(O)cc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3717515 133889 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 499 7 1 9 6.2 COc1cc(OCc2cccc(-c3ccc(O)cc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118068680 134894 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 649 13 0 11 8.0 COc1cc(OCc2cccc(OCc3ccc(OCc4ccccc4)c(OC)c3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3728199 134894 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 649 13 0 11 8.0 COc1cc(OCc2cccc(OCc3ccc(OCc4ccccc4)c(OC)c3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118068683 135260 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 534 9 0 11 6.1 COc1cc(OCc2cccc(OCc3csc(C)n3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3730431 135260 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 534 9 0 11 6.1 COc1cc(OCc2cccc(OCc3csc(C)n3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118068520 135129 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 332 4 0 8 3.7 CCOc1ccc2nc(-c3cn4nc(SC)sc4n3)oc2c1 nan
CHEMBL3729621 135129 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 332 4 0 8 3.7 CCOc1ccc2nc(-c3cn4nc(SC)sc4n3)oc2c1 nan
164616125 184049 0 None 9 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at PAR4 in human platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in human platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 385 3 0 6 4.4 CCc1cc(-c2nc3c(Cl)cc(OC)cc3s2)c2ncn(C)c(=O)c2c1 10.1016/j.ejmech.2021.113764
CHEMBL4849569 184049 0 None 9 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at PAR4 in human platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in human platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 385 3 0 6 4.4 CCc1cc(-c2nc3c(Cl)cc(OC)cc3s2)c2ncn(C)c(=O)c2c1 10.1016/j.ejmech.2021.113764
72202283 135536 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 624 9 1 10 5.9 CSc1nn2cc(-c3nc4c(OC[C@@H]5CCCN5C(=O)[C@H](NC(=O)c5ccccc5)c5ccccc5)cccc4o3)nc2s1 nan
CHEMBL3732091 135536 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 624 9 1 10 5.9 CSc1nn2cc(-c3nc4c(OC[C@@H]5CCCN5C(=O)[C@H](NC(=O)c5ccccc5)c5ccccc5)cccc4o3)nc2s1 nan
89880970 135292 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 270 2 1 6 3.2 CNc1nn2cc(-c3cc4ccccc4o3)nc2s1 nan
CHEMBL3730643 135292 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 270 2 1 6 3.2 CNc1nn2cc(-c3cc4ccccc4o3)nc2s1 nan
118068483 135486 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 318 3 0 8 3.3 COc1ccc2oc(-c3cn4nc(SC)sc4n3)nc2c1 nan
CHEMBL3731794 135486 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 318 3 0 8 3.3 COc1ccc2oc(-c3cn4nc(SC)sc4n3)nc2c1 nan
118068508 135440 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 358 5 0 8 4.1 CSc1nn2cc(-c3nc4c(OCC5CC5)cccc4o3)nc2s1 nan
CHEMBL3731504 135440 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 358 5 0 8 4.1 CSc1nn2cc(-c3nc4c(OCC5CC5)cccc4o3)nc2s1 nan
118068488 135512 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 306 2 0 7 3.3 COc1nn2cc(-c3nc4cc(Cl)ccc4o3)nc2s1 nan
CHEMBL3731944 135512 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 306 2 0 7 3.3 COc1nn2cc(-c3nc4cc(Cl)ccc4o3)nc2s1 nan
118068712 135256 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 617 11 0 9 8.3 COc1nn2cc(-c3cc4c(OCc5cccc(OCc6cccc(C)c6)c5)c(Cc5ccccc5)c(OC)cc4o3)nc2s1 nan
CHEMBL3730410 135256 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 617 11 0 9 8.3 COc1nn2cc(-c3cc4c(OCc5cccc(OCc6cccc(C)c6)c5)c(Cc5ccccc5)c(OC)cc4o3)nc2s1 nan
72201565 135251 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 354 1 0 6 4.0 Fc1ccc2nc(-c3cn4nc(Br)sc4n3)sc2c1 nan
CHEMBL3730373 135251 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 354 1 0 6 4.0 Fc1ccc2nc(-c3cn4nc(Br)sc4n3)sc2c1 nan
72201564 134898 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 388 3 0 8 4.7 CSc1nn2cc(-c3nc4c(OC(F)(F)F)cccc4s3)nc2s1 nan
CHEMBL3728211 134898 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 388 3 0 8 4.7 CSc1nn2cc(-c3nc4c(OC(F)(F)F)cccc4s3)nc2s1 nan
118068620 134972 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 373 2 0 5 5.6 CC(F)(F)c1nn2cc(-c3cc4c(Cl)cc(Cl)cc4o3)nc2s1 nan
CHEMBL3728622 134972 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 373 2 0 5 5.6 CC(F)(F)c1nn2cc(-c3cc4c(Cl)cc(Cl)cc4o3)nc2s1 nan
118070671 134843 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 395 5 0 7 4.9 COc1nn2cc(-c3cc4c(OCc5ccc(F)cc5)cccc4o3)nc2s1 nan
CHEMBL3727854 134843 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 395 5 0 7 4.9 COc1nn2cc(-c3cc4c(OCc5ccc(F)cc5)cccc4o3)nc2s1 nan
72201853 134911 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 325 2 0 5 4.5 FC(F)(Cl)c1nn2cc(-c3cc4ccccc4o3)nc2s1 nan
CHEMBL3728288 134911 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 325 2 0 5 4.5 FC(F)(Cl)c1nn2cc(-c3cc4ccccc4o3)nc2s1 nan
72192416 133860 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 551 7 0 8 7.5 COc1cc(OCc2cccc(-c3cccc(C(F)(F)F)c3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3717423 133860 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 551 7 0 8 7.5 COc1cc(OCc2cccc(-c3cccc(C(F)(F)F)c3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
89873560 135167 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 409 5 0 8 4.0 COCOc1c(Br)ccc2oc(-c3cn4nc(OC)sc4n3)cc12 nan
CHEMBL3729842 135167 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 409 5 0 8 4.0 COCOc1c(Br)ccc2oc(-c3cn4nc(OC)sc4n3)cc12 nan
118068452 134820 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 328 4 0 7 3.9 CCc1nn2cc(-c3nc4ccc(OC(C)C)cc4o3)nc2s1 nan
CHEMBL3727735 134820 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 328 4 0 7 3.9 CCc1nn2cc(-c3nc4ccc(OC(C)C)cc4o3)nc2s1 nan
72201852 135015 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 341 3 0 5 4.6 FC(F)C(F)(F)c1nn2cc(-c3cc4ccccc4o3)nc2s1 nan
CHEMBL3728873 135015 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 341 3 0 5 4.6 FC(F)C(F)(F)c1nn2cc(-c3cc4ccccc4o3)nc2s1 nan
118068469 135429 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 287 2 1 7 2.9 COc1nn2cc(-c3cc4ccc(O)cc4o3)nc2s1 nan
CHEMBL3731454 135429 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 287 2 1 7 2.9 COc1nn2cc(-c3cc4ccc(O)cc4o3)nc2s1 nan
118068420 135423 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 284 2 0 6 3.5 CCc1nn2cc(-c3nc4c(C)cccc4o3)nc2s1 nan
CHEMBL3731404 135423 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 284 2 0 6 3.5 CCc1nn2cc(-c3nc4c(C)cccc4o3)nc2s1 nan
118068684 135563 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 529 9 0 8 7.4 COc1cc(OCc2cccc(OCc3ccccc3)c2)c2cc(-c3cn4nc([C@H](C)F)sc4n3)oc2c1 nan
CHEMBL3732266 135563 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 529 9 0 8 7.4 COc1cc(OCc2cccc(OCc3ccccc3)c2)c2cc(-c3cn4nc([C@H](C)F)sc4n3)oc2c1 nan
72201994 135170 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 354 1 0 6 4.0 Clc1nccc2oc(-c3cn4nc(Br)sc4n3)cc12 nan
CHEMBL3729878 135170 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 354 1 0 6 4.0 Clc1nccc2oc(-c3cn4nc(Br)sc4n3)cc12 nan
118068558 135601 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 287 2 0 5 4.2 CC(F)c1nn2cc(-c3cc4ccccc4o3)nc2s1 nan
CHEMBL3732492 135601 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 287 2 0 5 4.2 CC(F)c1nn2cc(-c3cc4ccccc4o3)nc2s1 nan
118068490 134903 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 308 2 0 7 2.9 COc1nn2cc(-c3nc4cc(F)c(F)cc4o3)nc2s1 nan
CHEMBL3728244 134903 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 308 2 0 7 2.9 COc1nn2cc(-c3nc4cc(F)c(F)cc4o3)nc2s1 nan
118068544 135282 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 356 2 0 6 4.8 CC(F)(F)c1nn2cc(-c3nc4c(Cl)cccc4s3)nc2s1 nan
CHEMBL3730564 135282 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 356 2 0 6 4.8 CC(F)(F)c1nn2cc(-c3nc4c(Cl)cccc4s3)nc2s1 nan
118068522 135675 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 430 5 0 8 5.2 CSc1nn2cc(-c3nc4c(OCc5cc(F)cc(F)c5)cccc4o3)nc2s1 nan
CHEMBL3732925 135675 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 430 5 0 8 5.2 CSc1nn2cc(-c3nc4c(OCc5cc(F)cc(F)c5)cccc4o3)nc2s1 nan
118070600 135209 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 345 6 0 8 3.2 COCCOc1cccc2oc(-c3cn4nc(OC)sc4n3)cc12 nan
CHEMBL3730121 135209 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 345 6 0 8 3.2 COCCOc1cccc2oc(-c3cn4nc(OC)sc4n3)cc12 nan
72192128 133689 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 510 7 0 11 5.1 COc1cc(OCc2ccnc(-c3cccc(C#N)c3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3716837 133689 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 510 7 0 11 5.1 COc1cc(OCc2ccnc(-c3cccc(C#N)c3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118068497 135114 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 306 2 0 7 3.5 CSc1nn2cc(-c3nc4cccc(F)c4o3)nc2s1 nan
CHEMBL3729532 135114 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 306 2 0 7 3.5 CSc1nn2cc(-c3nc4cccc(F)c4o3)nc2s1 nan
72201421 135219 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 303 2 1 8 2.9 CSc1nn2cc(-c3nc4c(N)cccc4o3)nc2s1 nan
CHEMBL3730192 135219 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 303 2 1 8 2.9 CSc1nn2cc(-c3nc4c(N)cccc4o3)nc2s1 nan
72201989 135343 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 394 5 0 8 4.9 CSc1nn2cc(-c3cc4c(OCc5cccnc5)cccc4o3)nc2s1 nan
CHEMBL3730937 135343 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 394 5 0 8 4.9 CSc1nn2cc(-c3cc4c(OCc5cccnc5)cccc4o3)nc2s1 nan
72189944 134399 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 501 7 0 9 6.3 COc1cc(OCc2cccc(-c3cncnc3)c2)c2cc(-c3cn4nc([C@H](C)F)sc4n3)oc2c1 nan
CHEMBL3719227 134399 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 501 7 0 9 6.3 COc1cc(OCc2cccc(-c3cncnc3)c2)c2cc(-c3cn4nc([C@H](C)F)sc4n3)oc2c1 nan
72193010 134237 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 482 6 0 10 5.3 COc1cc(OCc2csc(C(F)(F)F)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3718657 134237 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 482 6 0 10 5.3 COc1cc(OCc2csc(C(F)(F)F)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118068477 135136 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 290 2 0 7 2.7 COc1nn2cc(-c3nc4cc(F)ccc4o3)nc2s1 nan
CHEMBL3729647 135136 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 290 2 0 7 2.7 COc1nn2cc(-c3nc4cc(F)ccc4o3)nc2s1 nan
118070669 135332 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 395 3 0 7 4.7 COc1ccc(Br)c2cc(-c3cn4nc(SC)sc4n3)oc12 nan
CHEMBL3730866 135332 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 395 3 0 7 4.7 COc1ccc(Br)c2cc(-c3cn4nc(SC)sc4n3)oc12 nan
72193328 133625 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 541 7 0 10 6.2 COc1cc(OCc2cccc(-c3ccc4c(c3)OCCO4)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3716602 133625 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 541 7 0 10 6.2 COc1cc(OCc2cccc(-c3ccc4c(c3)OCCO4)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72190889 133653 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 444 6 0 9 5.4 COc1nn2cc(-c3nc4c(OCc5cccc(-c6ccoc6)c5)cccc4o3)nc2s1 nan
CHEMBL3716715 133653 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 444 6 0 9 5.4 COc1nn2cc(-c3nc4c(OCc5cccc(-c6ccoc6)c5)cccc4o3)nc2s1 nan
71769562 133398 1 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against PAR4 in washed human platelets assessed as inhibition of alpha-thrombin-induced platelet aggregation pre-incubated for 20 mins before alpha-thrombin addition by optical aggretometryAntagonist activity against PAR4 in washed human platelets assessed as inhibition of alpha-thrombin-induced platelet aggregation pre-incubated for 20 mins before alpha-thrombin addition by optical aggretometry
ChEMBL 490 7 0 10 5.9 COc1cc(OCc2csc(-c3ccccc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3715848 133398 1 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against PAR4 in washed human platelets assessed as inhibition of alpha-thrombin-induced platelet aggregation pre-incubated for 20 mins before alpha-thrombin addition by optical aggretometryAntagonist activity against PAR4 in washed human platelets assessed as inhibition of alpha-thrombin-induced platelet aggregation pre-incubated for 20 mins before alpha-thrombin addition by optical aggretometry
ChEMBL 490 7 0 10 5.9 COc1cc(OCc2csc(-c3ccccc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118068724 134807 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 631 10 0 11 6.6 COc1nn2cc(-c3cc4c(OCc5cccc(OCc6ccccc6)c5)cc(OS(=O)(=O)C(F)(F)F)cc4o3)nc2s1 nan
CHEMBL3727676 134807 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 631 10 0 11 6.6 COc1nn2cc(-c3cc4c(OCc5cccc(OCc6ccccc6)c5)cc(OS(=O)(=O)C(F)(F)F)cc4o3)nc2s1 nan
118068715 135310 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 508 8 0 9 6.2 COc1nn2cc(-c3cc4c(OCc5cccc(OCc6ccccc6)c5)cc(C#N)cc4o3)nc2s1 nan
CHEMBL3730715 135310 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 508 8 0 9 6.2 COc1nn2cc(-c3cc4c(OCc5cccc(OCc6ccccc6)c5)cc(C#N)cc4o3)nc2s1 nan
118068662 135374 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 605 11 0 10 8.2 COc1cc(OCc2cccc(OCc3cccc(Oc4ccccc4)c3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3731108 135374 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 605 11 0 10 8.2 COc1cc(OCc2cccc(OCc3cccc(Oc4ccccc4)c3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72202580 134885 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 517 8 0 8 7.0 COc1nn2cc(-c3cc4c(OCc5cccc(OCc6ccccc6)c5)cc(Cl)cc4o3)nc2s1 nan
CHEMBL3728158 134885 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 517 8 0 8 7.0 COc1nn2cc(-c3cc4c(OCc5cccc(OCc6ccccc6)c5)cc(Cl)cc4o3)nc2s1 nan
118068709 135639 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 565 9 0 9 7.2 COc1cc(OCc2cccc(OCc3c(F)cccc3Cl)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3732678 135639 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 565 9 0 9 7.2 COc1cc(OCc2cccc(OCc3c(F)cccc3Cl)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118068681 135091 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 571 10 0 10 7.0 COc1cc(OCc2cccc(OCc3ccc(OC)c(C)c3C)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3729386 135091 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 571 10 0 10 7.0 COc1cc(OCc2cccc(OCc3ccc(OC)c(C)c3C)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72201566 135316 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 306 2 0 7 3.2 COc1nn2cc(-c3nc4ccc(F)cc4s3)nc2s1 nan
CHEMBL3730778 135316 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 306 2 0 7 3.2 COc1nn2cc(-c3nc4ccc(F)cc4s3)nc2s1 nan
118070619 135313 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 425 6 0 8 4.9 COc1cc(OCc2ccc(F)cc2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3730755 135313 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 425 6 0 8 4.9 COc1cc(OCc2ccc(F)cc2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72192134 134320 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 530 7 0 11 5.5 COc1cc(OCc2nc(C3(F)CCOCC3)sc2C)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3718927 134320 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 530 7 0 11 5.5 COc1cc(OCc2nc(C3(F)CCOCC3)sc2C)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
164622285 185187 0 None 8 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human PAR4 expressed in Ga15-HEK293 cells assessed as reduction in PAR4 AP AYPGKF-NH2-induced cytosolic calcium incubated for 24 hrs by FLIPR - calcium mobilization assayAntagonist activity at human PAR4 expressed in Ga15-HEK293 cells assessed as reduction in PAR4 AP AYPGKF-NH2-induced cytosolic calcium incubated for 24 hrs by FLIPR - calcium mobilization assay
ChEMBL 311 1 0 5 3.2 Cc1cc(-c2nc3c(s2)CCCC3)c2ncn(C)c(=O)c2c1 10.1016/j.ejmech.2021.113764
CHEMBL4866566 185187 0 None 8 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human PAR4 expressed in Ga15-HEK293 cells assessed as reduction in PAR4 AP AYPGKF-NH2-induced cytosolic calcium incubated for 24 hrs by FLIPR - calcium mobilization assayAntagonist activity at human PAR4 expressed in Ga15-HEK293 cells assessed as reduction in PAR4 AP AYPGKF-NH2-induced cytosolic calcium incubated for 24 hrs by FLIPR - calcium mobilization assay
ChEMBL 311 1 0 5 3.2 Cc1cc(-c2nc3c(s2)CCCC3)c2ncn(C)c(=O)c2c1 10.1016/j.ejmech.2021.113764
118070655 135405 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 299 2 0 6 3.8 COc1nn2cc(-c3cc4c(C)cc(C)cc4o3)nc2s1 nan
CHEMBL3731269 135405 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 299 2 0 6 3.8 COc1nn2cc(-c3cc4c(C)cc(C)cc4o3)nc2s1 nan
118070599 135230 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 305 2 0 6 4.1 CSc1nn2cc(-c3cc4cccc(F)c4o3)nc2s1 nan
CHEMBL3730242 135230 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 305 2 0 6 4.1 CSc1nn2cc(-c3cc4cccc(F)c4o3)nc2s1 nan
118068556 135378 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 365 4 0 7 4.3 COc1cc(OC)c2cc(-c3cn4nc(C(C)(F)F)sc4n3)oc2c1 nan
CHEMBL3731134 135378 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 365 4 0 7 4.3 COc1cc(OC)c2cc(-c3cn4nc(C(C)(F)F)sc4n3)oc2c1 nan
72201856 135473 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 347 4 0 7 4.3 COc1cc(OC)c2cc(-c3cn4nc(C(C)F)sc4n3)oc2c1 nan
CHEMBL3731702 135473 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 347 4 0 7 4.3 COc1cc(OC)c2cc(-c3cn4nc(C(C)F)sc4n3)oc2c1 nan
118068446 135201 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 410 5 0 7 5.4 CCc1nn2cc(-c3nc4ccc(OCc5ccccc5Cl)cc4o3)nc2s1 nan
CHEMBL3730076 135201 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 410 5 0 7 5.4 CCc1nn2cc(-c3nc4ccc(OCc5ccccc5Cl)cc4o3)nc2s1 nan
72201423 135689 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 320 2 0 6 4.0 Cc1cccc2oc(-c3cn4nc(C(C)(F)F)sc4n3)nc12 nan
CHEMBL3733017 135689 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 320 2 0 6 4.0 Cc1cccc2oc(-c3cn4nc(C(C)(F)F)sc4n3)nc12 nan
118068718 135728 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 647 10 0 11 7.3 CSc1nn2cc(-c3cc4c(OCc5cccc(OCc6ccccc6)c5)cc(OS(=O)(=O)C(F)(F)F)cc4o3)nc2s1 nan
CHEMBL3733277 135728 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 647 10 0 11 7.3 CSc1nn2cc(-c3cc4c(OCc5cccc(OCc6ccccc6)c5)cc(OS(=O)(=O)C(F)(F)F)cc4o3)nc2s1 nan
118068615 135680 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 367 1 0 5 4.9 Cc1cc2oc(-c3cn4nc(Br)sc4n3)cc2cc1Cl nan
CHEMBL3732954 135680 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 367 1 0 5 4.9 Cc1cc2oc(-c3cn4nc(Br)sc4n3)cc2cc1Cl nan
72202581 134837 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 547 9 0 9 7.0 COc1nn2cc(-c3cc4c(OCc5cccc(OCc6ccccc6)c5)cc(OC)c(Cl)c4o3)nc2s1 nan
CHEMBL3727827 134837 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 547 9 0 9 7.0 COc1nn2cc(-c3cc4c(OCc5cccc(OCc6ccccc6)c5)cc(OC)c(Cl)c4o3)nc2s1 nan
118070647 134874 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 379 3 0 7 4.0 COc1nn2cc(-c3cc4cc(Br)c(OC)cc4o3)nc2s1 nan
CHEMBL3728096 134874 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 379 3 0 7 4.0 COc1nn2cc(-c3cc4cc(Br)c(OC)cc4o3)nc2s1 nan
118068530 135678 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 500 8 0 9 6.5 CSc1nn2cc(-c3nc4c(OCc5cccc(OCc6ccccc6)c5)cccc4o3)nc2s1 nan
CHEMBL3732951 135678 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 500 8 0 9 6.5 CSc1nn2cc(-c3nc4c(OCc5cccc(OCc6ccccc6)c5)cccc4o3)nc2s1 nan
89881089 134881 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assayAntagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assay
ChEMBL 281 2 0 5 4.1 c1ccc2oc(-c3cn4nc(C5CC5)sc4n3)cc2c1 10.1021/acs.jmedchem.9b00186
CHEMBL3728130 134881 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assayAntagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assay
ChEMBL 281 2 0 5 4.1 c1ccc2oc(-c3cn4nc(C5CC5)sc4n3)cc2c1 10.1021/acs.jmedchem.9b00186
89881062 135376 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 624 9 1 10 5.9 CSc1nn2cc(-c3nc4c(OC[C@H]5CCCN5C(=O)[C@H](NC(=O)c5ccccc5)c5ccccc5)cccc4o3)nc2s1 nan
CHEMBL3731125 135376 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 624 9 1 10 5.9 CSc1nn2cc(-c3nc4c(OC[C@H]5CCCN5C(=O)[C@H](NC(=O)c5ccccc5)c5ccccc5)cccc4o3)nc2s1 nan
118068398 135234 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 527 9 0 9 6.7 COc1cc(OCc2cccc(OCc3cccc(C)c3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3730270 135234 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 527 9 0 9 6.7 COc1cc(OCc2cccc(OCc3cccc(C)c3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118068462 135414 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 299 2 0 6 3.8 COc1nn2cc(-c3cc4ccc(C)c(C)c4o3)nc2s1 nan
CHEMBL3731355 135414 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 299 2 0 6 3.8 COc1nn2cc(-c3cc4ccc(C)c(C)c4o3)nc2s1 nan
72202726 135308 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 517 8 0 8 7.0 COc1cc(OCc2cccc(OCc3ccccc3)c2)c2cc(-c3cn4nc(Cl)sc4n3)oc2c1 nan
CHEMBL3730712 135308 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 517 8 0 8 7.0 COc1cc(OCc2cccc(OCc3ccccc3)c2)c2cc(-c3cn4nc(Cl)sc4n3)oc2c1 nan
43337113 135351 2 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 319 1 0 5 4.0 Brc1nn2cc(-c3cc4ccccc4o3)nc2s1 nan
CHEMBL3730981 135351 2 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 319 1 0 5 4.0 Brc1nn2cc(-c3cc4ccccc4o3)nc2s1 nan
118068666 135034 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 459 6 0 7 6.0 COc1cc(OCc2ccc(F)cc2)c2cc(-c3cn4nc(C(C)(F)F)sc4n3)oc2c1 nan
CHEMBL3729033 135034 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 459 6 0 7 6.0 COc1cc(OCc2ccc(F)cc2)c2cc(-c3cn4nc(C(C)(F)F)sc4n3)oc2c1 nan
118070669 135332 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 395 3 0 7 4.7 COc1ccc(Br)c2cc(-c3cn4nc(SC)sc4n3)oc12 nan
CHEMBL3730866 135332 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 395 3 0 7 4.7 COc1ccc(Br)c2cc(-c3cn4nc(SC)sc4n3)oc12 nan
118068429 135546 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 298 2 0 6 3.8 CCc1nn2cc(-c3nc4cc(C)cc(C)c4o3)nc2s1 nan
CHEMBL3732152 135546 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 298 2 0 6 3.8 CCc1nn2cc(-c3nc4cc(C)cc(C)c4o3)nc2s1 nan
118068426 135348 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 298 2 0 6 3.8 CCc1nn2cc(-c3nc4cc(C)c(C)cc4o3)nc2s1 nan
CHEMBL3730966 135348 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 298 2 0 6 3.8 CCc1nn2cc(-c3nc4cc(C)c(C)cc4o3)nc2s1 nan
89881056 135341 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 620 8 1 11 6.0 CSc1nn2cc(-c3nc4c(OC[C@H]5CCCN5C(=O)[C@H](NC(=O)OC(C)(C)C)c5ccccc5)cccc4o3)nc2s1 nan
CHEMBL3730925 135341 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 620 8 1 11 6.0 CSc1nn2cc(-c3nc4c(OC[C@H]5CCCN5C(=O)[C@H](NC(=O)OC(C)(C)C)c5ccccc5)cccc4o3)nc2s1 nan
118068727 135182 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 527 10 0 9 6.8 CCOc1cc(OCc2cccc(OCc3ccccc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3729962 135182 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 527 10 0 9 6.8 CCOc1cc(OCc2cccc(OCc3ccccc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118068662 135374 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 605 11 0 10 8.2 COc1cc(OCc2cccc(OCc3cccc(Oc4ccccc4)c3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3731108 135374 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 605 11 0 10 8.2 COc1cc(OCc2cccc(OCc3cccc(Oc4ccccc4)c3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118068500 135636 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 395 5 0 9 4.3 CSc1nn2cc(-c3nc4c(OCc5cccnc5)cccc4o3)nc2s1 nan
CHEMBL3732656 135636 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 395 5 0 9 4.3 CSc1nn2cc(-c3nc4c(OCc5cccnc5)cccc4o3)nc2s1 nan
118068433 134896 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 326 2 0 6 4.5 CCc1nn2cc(-c3nc4cc(C(C)(C)C)ccc4o3)nc2s1 nan
CHEMBL3728202 134896 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 326 2 0 6 4.5 CCc1nn2cc(-c3nc4cc(C(C)(C)C)ccc4o3)nc2s1 nan
118068444 135448 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 404 7 0 7 5.2 CCc1nn2cc(-c3nc4ccc(OCCCc5ccccc5)cc4o3)nc2s1 nan
CHEMBL3731548 135448 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 404 7 0 7 5.2 CCc1nn2cc(-c3nc4ccc(OCCCc5ccccc5)cc4o3)nc2s1 nan
118068634 134975 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 547 9 0 8 7.5 COc1cc(OCc2cccc(OCc3ccccc3)c2)c2cc(-c3cn4nc(C(C)(F)F)sc4n3)oc2c1 nan
CHEMBL3728638 134975 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 547 9 0 8 7.5 COc1cc(OCc2cccc(OCc3ccccc3)c2)c2cc(-c3cn4nc(C(C)(F)F)sc4n3)oc2c1 nan
118068694 135502 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 617 12 0 9 8.2 COc1cc(OCc2cccc(OCc3ccccc3CCc3ccccc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3731888 135502 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 617 12 0 9 8.2 COc1cc(OCc2cccc(OCc3ccccc3CCc3ccccc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118070589 135711 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 371 6 0 8 3.7 CCOC(=O)COc1cccc2cc(-c3cn4nc(CC)sc4n3)oc12 nan
CHEMBL3733169 135711 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 371 6 0 8 3.7 CCOC(=O)COc1cccc2cc(-c3cn4nc(CC)sc4n3)oc12 nan
72202137 134913 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 485 6 0 8 5.6 COc1nn2cc(-c3cc4c(OCc5ccccc5)cc(OC)c(Br)c4o3)nc2s1 nan
CHEMBL3728293 134913 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 485 6 0 8 5.6 COc1nn2cc(-c3cc4c(OCc5ccccc5)cc(OC)c(Br)c4o3)nc2s1 nan
118068711 134884 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 619 12 0 10 8.0 COc1cc(OCc2cccc(OCc3cccc(OCc4ccccc4)c3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3728153 134884 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 619 12 0 10 8.0 COc1cc(OCc2cccc(OCc3cccc(OCc4ccccc4)c3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72202583 134857 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 547 9 0 9 7.0 COc1cc(OCc2cc(Cl)cc(OCc3ccccc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3728008 134857 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 547 9 0 9 7.0 COc1cc(OCc2cc(Cl)cc(OCc3ccccc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72193324 134208 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR methodAntagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR method
ChEMBL 514 8 0 10 5.9 COc1cc(OCc2cccc(-c3cccc(OC)n3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.2c00359
CHEMBL3718606 134208 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR methodAntagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR method
ChEMBL 514 8 0 10 5.9 COc1cc(OCc2cccc(-c3cccc(OC)n3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.2c00359
72193324 134208 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 514 8 0 10 5.9 COc1cc(OCc2cccc(-c3cccc(OC)n3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3718606 134208 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 514 8 0 10 5.9 COc1cc(OCc2cccc(-c3cccc(OC)n3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118042458 133137 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 484 7 0 9 5.9 COc1cc(OCc2cccc(-c3cccnc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3714929 133137 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 484 7 0 9 5.9 COc1cc(OCc2cccc(-c3cccnc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
164610234 184488 0 None 60 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at PAR4 in human platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in human platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 608 7 1 8 5.5 Cc1cc(-c2nc3c(Cl)cc(OCCNS(=O)(=O)c4ccc(C(F)(F)F)cc4)cc3s2)c2ncn(C)c(=O)c2c1 10.1016/j.ejmech.2021.113764
CHEMBL4855875 184488 0 None 60 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at PAR4 in human platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in human platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 608 7 1 8 5.5 Cc1cc(-c2nc3c(Cl)cc(OCCNS(=O)(=O)c4ccc(C(F)(F)F)cc4)cc3s2)c2ncn(C)c(=O)c2c1 10.1016/j.ejmech.2021.113764
72203552 135106 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 318 3 0 8 3.3 COc1ccc2nc(-c3cn4nc(SC)sc4n3)oc2c1 nan
CHEMBL3729499 135106 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 318 3 0 8 3.3 COc1ccc2nc(-c3cn4nc(SC)sc4n3)oc2c1 nan
72190584 133434 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 519 7 0 10 5.9 COc1cc(OCc2cccc(-c3ccc(Cl)nc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3715976 133434 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 519 7 0 10 5.9 COc1cc(OCc2cccc(-c3ccc(Cl)nc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118068672 135481 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 599 9 0 9 7.5 COc1cc(OCc2cccc(OCc3cc(C(F)(F)F)ccc3F)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3731752 135481 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 599 9 0 9 7.5 COc1cc(OCc2cccc(OCc3cc(C(F)(F)F)ccc3F)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
164616125 184049 0 None 9 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human PAR4 expressed in Ga15-HEK293 cells assessed as reduction in PAR4 AP AYPGKF-NH2-induced cytosolic calcium incubated for 24 hrs by FLIPR - calcium mobilization assayAntagonist activity at human PAR4 expressed in Ga15-HEK293 cells assessed as reduction in PAR4 AP AYPGKF-NH2-induced cytosolic calcium incubated for 24 hrs by FLIPR - calcium mobilization assay
ChEMBL 385 3 0 6 4.4 CCc1cc(-c2nc3c(Cl)cc(OC)cc3s2)c2ncn(C)c(=O)c2c1 10.1016/j.ejmech.2021.113764
CHEMBL4849569 184049 0 None 9 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human PAR4 expressed in Ga15-HEK293 cells assessed as reduction in PAR4 AP AYPGKF-NH2-induced cytosolic calcium incubated for 24 hrs by FLIPR - calcium mobilization assayAntagonist activity at human PAR4 expressed in Ga15-HEK293 cells assessed as reduction in PAR4 AP AYPGKF-NH2-induced cytosolic calcium incubated for 24 hrs by FLIPR - calcium mobilization assay
ChEMBL 385 3 0 6 4.4 CCc1cc(-c2nc3c(Cl)cc(OC)cc3s2)c2ncn(C)c(=O)c2c1 10.1016/j.ejmech.2021.113764
118068382 135012 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 285 2 0 6 3.5 COc1nn2cc(-c3cc4cc(C)ccc4o3)nc2s1 nan
CHEMBL3728864 135012 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 285 2 0 6 3.5 COc1nn2cc(-c3cc4cc(C)ccc4o3)nc2s1 nan
118068706 135278 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 555 9 0 9 7.3 COc1cc(OCc2cccc(OCc3c(C)cc(C)cc3C)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3730526 135278 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 555 9 0 9 7.3 COc1cc(OCc2cccc(OCc3c(C)cc(C)cc3C)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118068423 135592 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 327 5 0 6 4.6 CCCOc1cccc2cc(-c3cn4nc(CC)sc4n3)oc12 nan
CHEMBL3732433 135592 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 327 5 0 6 4.6 CCCOc1cccc2cc(-c3cn4nc(CC)sc4n3)oc12 nan
118068586 135178 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 531 7 0 7 7.1 Brc1nn2cc(-c3cc4c(OCc5ccccc5)cc(OCc5ccccc5)cc4o3)nc2s1 nan
CHEMBL3729948 135178 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 531 7 0 7 7.1 Brc1nn2cc(-c3cc4c(OCc5ccccc5)cc(OCc5ccccc5)cc4o3)nc2s1 nan
118068686 134978 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 597 10 0 10 7.3 COc1cc(OCc2cccc(OCc3ccc(OC(F)(F)F)cc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3728653 134978 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 597 10 0 10 7.3 COc1cc(OCc2cccc(OCc3ccc(OC(F)(F)F)cc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
89873594 134865 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 334 3 0 8 3.8 COc1cccc2sc(-c3cn4nc(SC)sc4n3)nc12 nan
CHEMBL3728053 134865 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 334 3 0 8 3.8 COc1cccc2sc(-c3cn4nc(SC)sc4n3)nc12 nan
118068512 134816 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 419 5 0 9 4.8 CSc1nn2cc(-c3nc4ccc(OCc5cccc(C#N)c5)cc4o3)nc2s1 nan
CHEMBL3727710 134816 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 419 5 0 9 4.8 CSc1nn2cc(-c3nc4ccc(OCc5cccc(C#N)c5)cc4o3)nc2s1 nan
118070588 135122 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 399 8 0 8 4.5 CCOC(=O)CCCOc1cccc2cc(-c3cn4nc(CC)sc4n3)oc12 nan
CHEMBL3729588 135122 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 399 8 0 8 4.5 CCOC(=O)CCCOc1cccc2cc(-c3cn4nc(CC)sc4n3)oc12 nan
72201567 135262 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 322 2 0 6 4.2 CC(F)(F)c1nn2cc(-c3nc4ccccc4s3)nc2s1 nan
CHEMBL3730440 135262 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 322 2 0 6 4.2 CC(F)(F)c1nn2cc(-c3nc4ccccc4s3)nc2s1 nan
118042460 134023 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 523 7 0 10 6.1 COc1cc(OCc2cccc(-c3ccc4nccn4c3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3717980 134023 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 523 7 0 10 6.1 COc1cc(OCc2cccc(-c3ccc4nccn4c3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72191195 133884 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 528 8 1 10 5.6 COc1cc(OCc2cccc(-c3ccc(C(=O)O)nc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3717498 133884 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 528 8 1 10 5.6 COc1cc(OCc2cccc(-c3ccc(C(=O)O)nc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72189038 133158 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 490 7 0 10 5.9 COc1cc(OCc2cccc(-c3cnsc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3714996 133158 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 490 7 0 10 5.9 COc1cc(OCc2cccc(-c3cnsc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72201418 135651 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 395 5 0 9 4.3 CSc1nn2cc(-c3nc4ccc(OCc5ccccn5)cc4o3)nc2s1 nan
CHEMBL3732783 135651 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 395 5 0 9 4.3 CSc1nn2cc(-c3nc4ccc(OCc5ccccn5)cc4o3)nc2s1 nan
118068447 135070 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 410 5 0 7 5.4 CCc1nn2cc(-c3nc4ccc(OCc5cccc(Cl)c5)cc4o3)nc2s1 nan
CHEMBL3729245 135070 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 410 5 0 7 5.4 CCc1nn2cc(-c3nc4ccc(OCc5cccc(Cl)c5)cc4o3)nc2s1 nan
118068693 135269 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 514 9 0 10 5.8 COc1cc(OCc2cccc(OCc3cccnc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3730494 135269 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 514 9 0 10 5.8 COc1cc(OCc2cccc(OCc3cccnc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
89880952 134880 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 306 2 0 6 3.4 CCc1nn2cc(-c3nc4cc(F)c(F)cc4o3)nc2s1 nan
CHEMBL3728113 134880 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 306 2 0 6 3.4 CCc1nn2cc(-c3nc4cc(F)c(F)cc4o3)nc2s1 nan
118042459 134075 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 551 7 0 8 7.5 COc1cc(OCc2cccc(-c3ccc(C(F)(F)F)cc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3718163 134075 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 551 7 0 8 7.5 COc1cc(OCc2cccc(-c3ccc(C(F)(F)F)cc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118042459 134075 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR methodAntagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR method
ChEMBL 551 7 0 8 7.5 COc1cc(OCc2cccc(-c3ccc(C(F)(F)F)cc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.2c00359
CHEMBL3718163 134075 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR methodAntagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR method
ChEMBL 551 7 0 8 7.5 COc1cc(OCc2cccc(-c3ccc(C(F)(F)F)cc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.2c00359
118070587 135605 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assayAntagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assay
ChEMBL 285 3 0 6 3.6 CCOc1nn2cc(-c3cc4ccccc4o3)nc2s1 10.1021/acs.jmedchem.9b00186
CHEMBL3732510 135605 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assayAntagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assay
ChEMBL 285 3 0 6 3.6 CCOc1nn2cc(-c3cc4ccccc4o3)nc2s1 10.1021/acs.jmedchem.9b00186
89880954 135076 1 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 269 2 0 5 3.8 CCc1nn2cc(-c3cc4ccccc4o3)nc2s1 nan
CHEMBL3729282 135076 1 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 269 2 0 5 3.8 CCc1nn2cc(-c3cc4ccccc4o3)nc2s1 nan
118068647 134890 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 389 3 0 6 5.2 CC(F)(F)c1nn2cc(-c3cc4cccc(OC(F)(F)F)c4o3)nc2s1 nan
CHEMBL3728180 134890 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 389 3 0 6 5.2 CC(F)(F)c1nn2cc(-c3cc4cccc(OC(F)(F)F)c4o3)nc2s1 nan
118068513 134830 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 428 5 0 8 5.6 CSc1nn2cc(-c3nc4ccc(OCc5ccccc5Cl)cc4o3)nc2s1 nan
CHEMBL3727802 134830 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 428 5 0 8 5.6 CSc1nn2cc(-c3nc4ccc(OCc5ccccc5Cl)cc4o3)nc2s1 nan
118068692 134822 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 581 9 0 9 7.7 COc1cc(OCc2cccc(OCc3cc(Cl)cc(Cl)c3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3727768 134822 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 581 9 0 9 7.7 COc1cc(OCc2cccc(OCc3cc(Cl)cc(Cl)c3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72193001 134007 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 527 7 0 10 6.2 COc1cc(OCc2cccc(-c3ccc4c(c3)OCO4)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3717928 134007 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 527 7 0 10 6.2 COc1cc(OCc2cccc(-c3ccc4c(c3)OCO4)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118068485 134774 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 356 3 0 8 3.5 COc1nn2cc(-c3nc4cc(OC(F)(F)F)ccc4o3)nc2s1 nan
CHEMBL3727463 134774 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 356 3 0 8 3.5 COc1nn2cc(-c3nc4cc(OC(F)(F)F)ccc4o3)nc2s1 nan
118068439 135434 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 340 5 0 7 4.0 CCc1nn2cc(-c3nc4ccc(OCC5CC5)cc4o3)nc2s1 nan
CHEMBL3731484 135434 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 340 5 0 7 4.0 CCc1nn2cc(-c3nc4ccc(OCC5CC5)cc4o3)nc2s1 nan
118068519 134868 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 332 4 0 8 3.7 CCOc1cccc2oc(-c3cn4nc(SC)sc4n3)nc12 nan
CHEMBL3728067 134868 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 332 4 0 8 3.7 CCOc1cccc2oc(-c3cn4nc(SC)sc4n3)nc12 nan
118068695 134835 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 629 13 0 11 8.0 COc1cc(OCc2cccc(OCc3cc(OC(C)C)cc(OC(C)C)c3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3727816 134835 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 629 13 0 11 8.0 COc1cc(OCc2cccc(OCc3cc(OC(C)C)cc(OC(C)C)c3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118068445 135118 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 368 4 0 7 4.9 CCc1nn2cc(-c3nc4ccc(OC5CCCCC5)cc4o3)nc2s1 nan
CHEMBL3729564 135118 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 368 4 0 7 4.9 CCc1nn2cc(-c3nc4ccc(OC5CCCCC5)cc4o3)nc2s1 nan
89880981 135443 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 331 3 0 7 4.2 COc1ccc2oc(-c3cn4nc(SC)sc4n3)c(C)c2c1 nan
CHEMBL3731536 135443 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 331 3 0 7 4.2 COc1ccc2oc(-c3cn4nc(SC)sc4n3)c(C)c2c1 nan
118068720 135228 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 665 10 0 10 7.7 CC(F)(F)c1nn2cc(-c3cc4c(OCc5cccc(OCc6ccccc6)c5)cc(OS(=O)(=O)C(F)(F)F)cc4o3)nc2s1 nan
CHEMBL3730237 135228 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 665 10 0 10 7.7 CC(F)(F)c1nn2cc(-c3cc4c(OCc5cccc(OCc6ccccc6)c5)cc(OS(=O)(=O)C(F)(F)F)cc4o3)nc2s1 nan
72190583 133641 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 484 7 0 9 5.9 COc1cc(OCc2cncc(-c3ccccc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3716664 133641 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 484 7 0 9 5.9 COc1cc(OCc2cncc(-c3ccccc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118068603 135073 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 369 3 0 6 5.0 COc1cc2oc(-c3cn4nc(C(C)(F)F)sc4n3)cc2cc1Cl nan
CHEMBL3729256 135073 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 369 3 0 6 5.0 COc1cc2oc(-c3cn4nc(C(C)(F)F)sc4n3)cc2cc1Cl nan
118068692 134822 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 581 9 0 9 7.7 COc1cc(OCc2cccc(OCc3cc(Cl)cc(Cl)c3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3727768 134822 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 581 9 0 9 7.7 COc1cc(OCc2cccc(OCc3cc(Cl)cc(Cl)c3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72193004 134308 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 523 7 0 10 6.1 COc1cc(OCc2cccc(-c3cnc4ccccn34)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3718869 134308 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 523 7 0 10 6.1 COc1cc(OCc2cccc(-c3cnc4ccccn34)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118068696 135566 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 581 9 0 9 7.7 COc1cc(OCc2cccc(OCc3ccc(Cl)cc3Cl)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3732283 135566 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 581 9 0 9 7.7 COc1cc(OCc2cccc(OCc3ccc(Cl)cc3Cl)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118068688 135456 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 581 9 0 9 7.4 COc1cc(OCc2cc(OCc3ccccc3)cc(C(F)(F)F)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3731626 135456 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 581 9 0 9 7.4 COc1cc(OCc2cc(OCc3ccccc3)cc(C(F)(F)F)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72201990 135508 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 331 5 0 8 3.2 COCOc1cccc2oc(-c3cn4nc(OC)sc4n3)cc12 nan
CHEMBL3731928 135508 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 331 5 0 8 3.2 COCOc1cccc2oc(-c3cn4nc(OC)sc4n3)cc12 nan
118068564 135357 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 393 4 0 7 4.4 CCOc1cc(OC)cc2oc(-c3cn4nc(Br)sc4n3)cc12 nan
CHEMBL3731020 135357 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 393 4 0 7 4.4 CCOc1cc(OC)cc2oc(-c3cn4nc(Br)sc4n3)cc12 nan
118068695 134835 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 629 13 0 11 8.0 COc1cc(OCc2cccc(OCc3cc(OC(C)C)cc(OC(C)C)c3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3727816 134835 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 629 13 0 11 8.0 COc1cc(OCc2cccc(OCc3cc(OC(C)C)cc(OC(C)C)c3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
10269 671 21 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 513 7 0 12 4.4 COc1cc(OCc2nc(sc2C)N2CCOCC2)c2c(c1)oc(c2)c1cn2c(n1)sc(n2)OC nan
72190270 671 21 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 513 7 0 12 4.4 COc1cc(OCc2nc(sc2C)N2CCOCC2)c2c(c1)oc(c2)c1cn2c(n1)sc(n2)OC nan
CHEMBL3716726 671 21 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 513 7 0 12 4.4 COc1cc(OCc2nc(sc2C)N2CCOCC2)c2c(c1)oc(c2)c1cn2c(n1)sc(n2)OC nan
118068374 169218 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assayAntagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assay
ChEMBL 301 3 0 7 3.2 COc1nn2cc(-c3cc4c(OC)cccc4o3)nc2s1 10.1021/acs.jmedchem.9b00186
CHEMBL4439280 169218 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assayAntagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assay
ChEMBL 301 3 0 7 3.2 COc1nn2cc(-c3cc4c(OC)cccc4o3)nc2s1 10.1021/acs.jmedchem.9b00186
118068705 135656 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 649 13 0 11 8.0 COc1cc(COc2cccc(COc3cc(OC)cc4oc(-c5cn6nc(OC)sc6n5)cc34)c2)cc(OCc2ccccc2)c1 nan
CHEMBL3732797 135656 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 649 13 0 11 8.0 COc1cc(COc2cccc(COc3cc(OC)cc4oc(-c5cn6nc(OC)sc6n5)cc34)c2)cc(OCc2ccccc2)c1 nan
89873480 135582 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 301 3 0 7 3.2 COc1nn2cc(-c3cc4cccc(OC)c4o3)nc2s1 nan
CHEMBL3732386 135582 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 301 3 0 7 3.2 COc1nn2cc(-c3cc4cccc(OC)c4o3)nc2s1 nan
72202432 135527 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 499 8 1 9 6.1 COc1nn2cc(-c3cc4c(OCc5cccc(OCc6ccccc6)c5)cc(O)cc4o3)nc2s1 nan
CHEMBL3732045 135527 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 499 8 1 9 6.1 COc1nn2cc(-c3cc4c(OCc5cccc(OCc6ccccc6)c5)cc(O)cc4o3)nc2s1 nan
118068710 135120 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 639 9 0 9 7.0 COc1cc(OCc2cccc(OCc3ccccc3I)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3729581 135120 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 639 9 0 9 7.0 COc1cc(OCc2cccc(OCc3ccccc3I)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118068458 134766 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 289 2 0 6 3.4 COc1nn2cc(-c3cc4ccc(F)cc4o3)nc2s1 nan
CHEMBL3727432 134766 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 289 2 0 6 3.4 COc1nn2cc(-c3cc4ccc(F)cc4o3)nc2s1 nan
118068506 134906 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 428 5 0 8 5.6 CSc1nn2cc(-c3nc4ccc(OCc5ccc(Cl)cc5)cc4o3)nc2s1 nan
CHEMBL3728256 134906 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 428 5 0 8 5.6 CSc1nn2cc(-c3nc4ccc(OCc5ccc(Cl)cc5)cc4o3)nc2s1 nan
118068510 135246 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 303 2 1 8 2.9 CSc1nn2cc(-c3nc4ccc(N)cc4o3)nc2s1 nan
CHEMBL3730357 135246 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 303 2 1 8 2.9 CSc1nn2cc(-c3nc4ccc(N)cc4o3)nc2s1 nan
118068460 135325 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 316 3 0 8 3.1 COc1nn2cc(-c3cc4cc([N+](=O)[O-])ccc4o3)nc2s1 nan
CHEMBL3730846 135325 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 316 3 0 8 3.1 COc1nn2cc(-c3cc4cc([N+](=O)[O-])ccc4o3)nc2s1 nan
118068674 135288 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 515 9 0 11 5.2 COc1cc(OCc2cccc(OCc3cncnc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3730607 135288 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 515 9 0 11 5.2 COc1cc(OCc2cccc(OCc3cncnc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118068648 135707 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 305 2 0 5 4.4 CC(F)c1nn2cc(-c3cc4ccc(F)cc4o3)nc2s1 nan
CHEMBL3733129 135707 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 305 2 0 5 4.4 CC(F)c1nn2cc(-c3cc4ccc(F)cc4o3)nc2s1 nan
72202434 134908 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 540 9 1 9 6.3 COc1nn2cc(-c3cc4c(OCc5cccc(OCc6ccccc6)c5)cc(NC(C)=O)cc4o3)nc2s1 nan
CHEMBL3728281 134908 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 540 9 1 9 6.3 COc1nn2cc(-c3cc4c(OCc5cccc(OCc6ccccc6)c5)cc(NC(C)=O)cc4o3)nc2s1 nan
118068723 135727 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 501 8 0 8 6.5 COc1nn2cc(-c3cc4c(F)cc(OCc5cccc(OCc6ccccc6)c5)cc4o3)nc2s1 nan
CHEMBL3733272 135727 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 501 8 0 8 6.5 COc1nn2cc(-c3cc4c(F)cc(OCc5cccc(OCc6ccccc6)c5)cc4o3)nc2s1 nan
118070617 135452 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 335 2 0 6 4.9 CSc1nn2cc(-c3cc4cc(Cl)c(C)cc4o3)nc2s1 nan
CHEMBL3731593 135452 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 335 2 0 6 4.9 CSc1nn2cc(-c3cc4cc(Cl)c(C)cc4o3)nc2s1 nan
72203551 135455 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 394 5 0 8 4.9 CSc1nn2cc(-c3nc4ccc(OCc5ccccc5)cc4o3)nc2s1 nan
CHEMBL3731621 135455 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 394 5 0 8 4.9 CSc1nn2cc(-c3nc4ccc(OCc5ccccc5)cc4o3)nc2s1 nan
118068607 135052 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 548 9 0 10 6.4 COc1cc(OCc2cccc(OCc3ccnc(Cl)c3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3729143 135052 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 548 9 0 10 6.4 COc1cc(OCc2cccc(OCc3ccnc(Cl)c3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
155563531 174705 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assayAntagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assay
ChEMBL 299 3 0 6 4.0 CC(C)Oc1nn2cc(-c3cc4ccccc4o3)nc2s1 10.1021/acs.jmedchem.9b00186
CHEMBL4572935 174705 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assayAntagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assay
ChEMBL 299 3 0 6 4.0 CC(C)Oc1nn2cc(-c3cc4ccccc4o3)nc2s1 10.1021/acs.jmedchem.9b00186
164623869 185463 0 None 52 2 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at PAR4 in human platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in human platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 355 2 0 6 3.7 COc1cc(F)c2nc(-c3cc(C)cc4c(=O)n(C)cnc34)sc2c1 10.1016/j.ejmech.2021.113764
CHEMBL4871001 185463 0 None 52 2 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at PAR4 in human platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in human platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 355 2 0 6 3.7 COc1cc(F)c2nc(-c3cc(C)cc4c(=O)n(C)cnc34)sc2c1 10.1016/j.ejmech.2021.113764
118070675 135497 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 338 2 0 7 4.4 CSc1nn2cc(-c3nc4c(Cl)cccc4s3)nc2s1 nan
CHEMBL3731858 135497 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 338 2 0 7 4.4 CSc1nn2cc(-c3nc4c(Cl)cccc4s3)nc2s1 nan
89873529 135665 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 304 2 1 8 3.0 CSc1nn2cc(-c3nc4c(O)cccc4o3)nc2s1 nan
CHEMBL3732858 135665 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 304 2 1 8 3.0 CSc1nn2cc(-c3nc4c(O)cccc4o3)nc2s1 nan
118068665 135366 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 407 4 0 7 4.8 COc1cc(OC(C)C)c2cc(-c3cn4nc(Br)sc4n3)oc2c1 nan
CHEMBL3731060 135366 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 407 4 0 7 4.8 COc1cc(OC(C)C)c2cc(-c3cn4nc(Br)sc4n3)oc2c1 nan
118068521 134815 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 395 5 0 9 4.3 CSc1nn2cc(-c3nc4c(OCc5ccncc5)cccc4o3)nc2s1 nan
CHEMBL3727709 134815 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 395 5 0 9 4.3 CSc1nn2cc(-c3nc4c(OCc5ccncc5)cccc4o3)nc2s1 nan
118068493 135096 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 346 4 0 8 4.1 CSc1nn2cc(-c3nc4ccc(OC(C)C)cc4o3)nc2s1 nan
CHEMBL3729432 135096 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 346 4 0 8 4.1 CSc1nn2cc(-c3nc4ccc(OC(C)C)cc4o3)nc2s1 nan
118070610 135613 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 322 2 0 7 3.7 COc1nn2cc(-c3nc4c(Cl)cccc4s3)nc2s1 nan
CHEMBL3732554 135613 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 322 2 0 7 3.7 COc1nn2cc(-c3nc4c(Cl)cccc4s3)nc2s1 nan
89880967 135187 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 370 2 0 7 4.6 CSc1nn2cc(-c3cc4c(C(F)(F)F)cc(C)nc4o3)nc2s1 nan
CHEMBL3729992 135187 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 370 2 0 7 4.6 CSc1nn2cc(-c3cc4c(C(F)(F)F)cc(C)nc4o3)nc2s1 nan
118070606 135509 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 355 2 0 6 5.2 CSc1nn2cc(-c3cc4c(Cl)cc(Cl)cc4o3)nc2s1 nan
CHEMBL3731932 135509 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 355 2 0 6 5.2 CSc1nn2cc(-c3cc4c(Cl)cc(Cl)cc4o3)nc2s1 nan
118068653 135198 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 589 10 0 9 8.0 COc1cc(OCc2cccc(OCc3ccccc3-c3ccccc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3730060 135198 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 589 10 0 9 8.0 COc1cc(OCc2cccc(OCc3ccccc3-c3ccccc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
168294560 191688 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR methodAntagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR method
ChEMBL 489 6 0 8 6.1 COc1cc(OCc2cc(C(F)(F)F)ccc2C)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.2c00359
CHEMBL5206095 191688 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR methodAntagonist activity at full length human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2 induced intracellular calcium mobilization pretreated with compound for 30 mins followed by agonist addition for 30 mins by FLIPR method
ChEMBL 489 6 0 8 6.1 COc1cc(OCc2cc(C(F)(F)F)ccc2C)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.2c00359
89873693 134802 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 299 3 0 6 3.8 CCc1nn2cc(-c3cc4cccc(OC)c4o3)nc2s1 nan
CHEMBL3727656 134802 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 299 3 0 6 3.8 CCc1nn2cc(-c3cc4cccc(OC)c4o3)nc2s1 nan
72193003 133429 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 541 7 0 11 6.5 COc1cc(OCc2cccc(-c3ccc4nsnc4c3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3715948 133429 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 541 7 0 11 6.5 COc1cc(OCc2cccc(-c3ccc4nsnc4c3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72201705 134925 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 383 2 0 6 4.6 COc1cc2oc(-c3cn4nc(Br)sc4n3)cc2cc1Cl nan
CHEMBL3728367 134925 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 383 2 0 6 4.6 COc1cc2oc(-c3cn4nc(Br)sc4n3)cc2cc1Cl nan
72189035 134082 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 516 8 1 10 5.2 COc1cc(OCc2cccc(-c3coc(C(N)=O)c3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3718180 134082 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 516 8 1 10 5.2 COc1cc(OCc2cccc(-c3coc(C(N)=O)c3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118068711 134884 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 619 12 0 10 8.0 COc1cc(OCc2cccc(OCc3cccc(OCc4ccccc4)c3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3728153 134884 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 619 12 0 10 8.0 COc1cc(OCc2cccc(OCc3cccc(OCc4ccccc4)c3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
89873629 135369 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 317 3 0 7 3.9 COc1cccc2cc(-c3cn4nc(SC)sc4n3)oc12 nan
CHEMBL3731072 135369 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 317 3 0 7 3.9 COc1cccc2cc(-c3cn4nc(SC)sc4n3)oc12 nan
118068606 135652 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 549 9 0 9 6.7 COc1cc(OCc2cccc(OCc3cc(F)cc(F)c3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3732785 135652 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 549 9 0 9 6.7 COc1cc(OCc2cccc(OCc3cc(F)cc(F)c3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118068667 134775 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 599 9 0 9 7.5 COc1cc(OCc2cccc(OCc3ccc(F)c(C(F)(F)F)c3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3727464 134775 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 599 9 0 9 7.5 COc1cc(OCc2cccc(OCc3ccc(F)c(C(F)(F)F)c3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118068482 135627 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 372 3 0 8 4.2 CSc1nn2cc(-c3nc4cc(OC(F)(F)F)ccc4o3)nc2s1 nan
CHEMBL3732619 135627 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 372 3 0 8 4.2 CSc1nn2cc(-c3nc4cc(OC(F)(F)F)ccc4o3)nc2s1 nan
89880973 135084 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 342 6 0 7 4.3 CCCCOc1ccc2nc(-c3cn4nc(CC)sc4n3)oc2c1 nan
CHEMBL3729347 135084 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 342 6 0 7 4.3 CCCCOc1ccc2nc(-c3cn4nc(CC)sc4n3)oc2c1 nan
118068528 135570 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 446 5 0 8 5.2 COc1nn2cc(-c3nc4ccc(OCc5ccc(C(F)(F)F)cc5)cc4o3)nc2s1 nan
CHEMBL3732314 135570 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 446 5 0 8 5.2 COc1nn2cc(-c3nc4ccc(OCc5ccc(C(F)(F)F)cc5)cc4o3)nc2s1 nan
72189940 133611 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 584 8 0 11 6.8 COc1cc(OCc2cccc(-c3ccc(C(=O)OC(C)(C)C)nc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3716559 133611 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 584 8 0 11 6.8 COc1cc(OCc2cccc(-c3ccc(C(=O)OC(C)(C)C)nc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118068509 135731 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 424 6 0 9 4.9 COc1ccc(COc2cccc3oc(-c4cn5nc(SC)sc5n4)nc23)cc1 nan
CHEMBL3733298 135731 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 424 6 0 9 4.9 COc1ccc(COc2cccc3oc(-c4cn5nc(SC)sc5n4)nc23)cc1 nan
145998086 171450 1 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assayAntagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assay
ChEMBL 319 2 0 7 2.6 CS(=O)(=O)c1nn2cc(-c3cc4ccccc4o3)nc2s1 10.1021/acs.jmedchem.9b00186
CHEMBL4471641 171450 1 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assayAntagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assay
ChEMBL 319 2 0 7 2.6 CS(=O)(=O)c1nn2cc(-c3cc4ccccc4o3)nc2s1 10.1021/acs.jmedchem.9b00186
72202138 135140 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 487 5 0 10 5.1 CSc1nn2cc(-c3nc4c(OC[C@H]5CCCN5C(=O)OC(C)(C)C)cccc4o3)nc2s1 nan
CHEMBL3729693 135140 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 487 5 0 10 5.1 CSc1nn2cc(-c3nc4c(OC[C@H]5CCCN5C(=O)OC(C)(C)C)cccc4o3)nc2s1 nan
118068397 135364 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 531 9 0 9 6.5 COc1cc(OCc2cc(F)cc(OCc3ccccc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3731050 135364 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 531 9 0 9 6.5 COc1cc(OCc2cc(F)cc(OCc3ccccc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118068387 135072 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 567 9 0 9 6.8 COc1cc(OCc2cccc(OCc3ccc(F)c(F)c3F)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3729253 135072 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 567 9 0 9 6.8 COc1cc(OCc2cccc(OCc3ccc(F)c(F)c3F)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118068476 135723 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 344 2 0 7 4.6 CSc1nn2cc(-c3nc4cc(C(C)(C)C)ccc4o3)nc2s1 nan
CHEMBL3733240 135723 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 344 2 0 7 4.6 CSc1nn2cc(-c3nc4cc(C(C)(C)C)ccc4o3)nc2s1 nan
72192126 133619 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 524 7 1 10 5.2 COc1cc(OCc2cccc(C3(O)CCOCC3)n2)c2cc(-c3cn4nc([C@H](C)F)sc4n3)oc2c1 nan
CHEMBL3716576 133619 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 524 7 1 10 5.2 COc1cc(OCc2cccc(C3(O)CCOCC3)n2)c2cc(-c3cn4nc([C@H](C)F)sc4n3)oc2c1 nan
89880971 135173 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 301 2 0 6 4.2 CSc1nn2cc(-c3cc4cccc(C)c4o3)nc2s1 nan
CHEMBL3729892 135173 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 301 2 0 6 4.2 CSc1nn2cc(-c3cc4cccc(C)c4o3)nc2s1 nan
72202282 135702 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 630 9 1 11 5.9 CSc1nn2cc(-c3nc4c(OC[C@H]5CCCN5C(=O)[C@H](NC(=O)c5cccs5)c5ccccc5)cccc4o3)nc2s1 nan
CHEMBL3733104 135702 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 630 9 1 11 5.9 CSc1nn2cc(-c3nc4c(OC[C@H]5CCCN5C(=O)[C@H](NC(=O)c5cccs5)c5ccccc5)cccc4o3)nc2s1 nan
72191502 133761 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 500 7 1 10 5.6 COc1cc(OCc2cccc(-c3ccc(O)cn3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3717065 133761 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 500 7 1 10 5.6 COc1cc(OCc2cccc(-c3ccc(O)cn3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118068405 135670 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 514 9 0 10 5.8 COc1cc(OCc2cccc(OCc3ccccn3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3732890 135670 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 514 9 0 10 5.8 COc1cc(OCc2cccc(OCc3ccccn3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118068386 135593 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 528 9 0 10 6.1 COc1cc(OCc2cccc(OCc3cccc(C)n3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3732437 135593 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 528 9 0 10 6.1 COc1cc(OCc2cccc(OCc3cccc(C)n3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72192417 133627 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 539 7 0 9 7.7 COc1cc(OCc2cccc(-c3cc4ccccc4s3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3716610 133627 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 539 7 0 9 7.7 COc1cc(OCc2cccc(-c3cc4ccccc4s3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118068717 135094 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 507 8 0 8 6.4 C#Cc1cc(OCc2cccc(OCc3ccccc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3729407 135094 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 507 8 0 8 6.4 C#Cc1cc(OCc2cccc(OCc3ccccc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
155527266 170650 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assayAntagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assay
ChEMBL 437 7 0 9 4.8 COc1cccc(COc2cc(OC)cc3oc(-c4cn5nc(OC)sc5n4)cc23)c1 10.1021/acs.jmedchem.9b00186
CHEMBL4459685 170650 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assayAntagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assay
ChEMBL 437 7 0 9 4.8 COc1cccc(COc2cc(OC)cc3oc(-c4cn5nc(OC)sc5n4)cc23)c1 10.1021/acs.jmedchem.9b00186
118068590 135330 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 351 3 0 6 4.9 COc1cc2oc(-c3cn4nc(C(C)F)sc4n3)cc2cc1Cl nan
CHEMBL3730859 135330 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 351 3 0 6 4.9 COc1cc2oc(-c3cn4nc(C(C)F)sc4n3)cc2cc1Cl nan
118070594 134832 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 306 2 0 7 3.2 COc1nn2cc(-c3nc4cc(F)ccc4s3)nc2s1 nan
CHEMBL3727807 134832 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 306 2 0 7 3.2 COc1nn2cc(-c3nc4cc(F)ccc4s3)nc2s1 nan
10269 671 21 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at PAR4 in human platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in human platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 513 7 0 12 4.4 COc1cc(OCc2nc(sc2C)N2CCOCC2)c2c(c1)oc(c2)c1cn2c(n1)sc(n2)OC 10.1016/j.ejmech.2021.113764
72190270 671 21 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at PAR4 in human platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in human platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 513 7 0 12 4.4 COc1cc(OCc2nc(sc2C)N2CCOCC2)c2c(c1)oc(c2)c1cn2c(n1)sc(n2)OC 10.1016/j.ejmech.2021.113764
CHEMBL3716726 671 21 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at PAR4 in human platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in human platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 513 7 0 12 4.4 COc1cc(OCc2nc(sc2C)N2CCOCC2)c2c(c1)oc(c2)c1cn2c(n1)sc(n2)OC 10.1016/j.ejmech.2021.113764
118068673 135390 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 597 10 0 10 7.3 COc1cc(OCc2cccc(OCc3ccccc3OC(F)(F)F)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3731190 135390 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 597 10 0 10 7.3 COc1cc(OCc2cccc(OCc3ccccc3OC(F)(F)F)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
89880949 135338 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 300 3 0 7 3.2 CCc1nn2cc(-c3nc4c(OC)cccc4o3)nc2s1 nan
CHEMBL3730914 135338 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 300 3 0 7 3.2 CCc1nn2cc(-c3nc4c(OC)cccc4o3)nc2s1 nan
118068491 134814 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 290 2 0 7 2.7 COc1nn2cc(-c3nc4cccc(F)c4o3)nc2s1 nan
CHEMBL3727707 134814 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 290 2 0 7 2.7 COc1nn2cc(-c3nc4cccc(F)c4o3)nc2s1 nan
118068492 135724 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 395 5 0 9 4.3 CSc1nn2cc(-c3nc4ccc(OCc5ccncc5)cc4o3)nc2s1 nan
CHEMBL3733243 135724 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 395 5 0 9 4.3 CSc1nn2cc(-c3nc4ccc(OCc5ccncc5)cc4o3)nc2s1 nan
118068504 134964 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 302 3 0 8 2.6 COc1ccc2nc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3728563 134964 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 302 3 0 8 2.6 COc1ccc2nc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118070645 134797 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 338 2 0 7 4.4 CSc1nn2cc(-c3nc4ccc(Cl)cc4s3)nc2s1 nan
CHEMBL3727627 134797 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 338 2 0 7 4.4 CSc1nn2cc(-c3nc4ccc(Cl)cc4s3)nc2s1 nan
118068668 134870 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 599 9 0 9 7.5 COc1cc(OCc2cccc(OCc3cccc(C(F)(F)F)c3F)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3728073 134870 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 599 9 0 9 7.5 COc1cc(OCc2cccc(OCc3cccc(C(F)(F)F)c3F)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118042462 133726 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 508 7 0 9 6.3 COc1cc(OCc2cccc(-c3ccc(C#N)cc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3716950 133726 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 508 7 0 9 6.3 COc1cc(OCc2cccc(-c3ccc(C#N)cc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118068593 135550 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 387 1 0 5 5.3 Clc1cc(Cl)c2cc(-c3cn4nc(Br)sc4n3)oc2c1 nan
CHEMBL3732170 135550 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 387 1 0 5 5.3 Clc1cc(Cl)c2cc(-c3cn4nc(Br)sc4n3)oc2c1 nan
89873629 135369 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 317 3 0 7 3.9 COc1cccc2cc(-c3cn4nc(SC)sc4n3)oc12 nan
CHEMBL3731072 135369 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 317 3 0 7 3.9 COc1cccc2cc(-c3cn4nc(SC)sc4n3)oc12 nan
118068703 134853 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 581 9 0 9 7.4 COc1cc(OCc2cccc(OCc3cccc(C(F)(F)F)c3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3727965 134853 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 581 9 0 9 7.4 COc1cc(OCc2cccc(OCc3cccc(C(F)(F)F)c3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72202135 135490 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 407 5 1 8 4.5 COc1nn2cc(-c3cc4c(O)c(Cc5ccccc5)c(OC)cc4o3)nc2s1 nan
CHEMBL3731815 135490 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 407 5 1 8 4.5 COc1nn2cc(-c3cc4c(O)c(Cc5ccccc5)c(OC)cc4o3)nc2s1 nan
72193325 133340 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 509 7 0 10 5.7 COc1cc(OCc2cccc(-c3cccnc3C#N)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3715654 133340 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assayAntagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
ChEMBL 509 7 0 10 5.7 COc1cc(OCc2cccc(-c3cccnc3C#N)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118070593 134933 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 352 2 0 7 4.8 CSc1nn2cc(-c3nc4c(C)cc(Cl)cc4s3)nc2s1 nan
CHEMBL3728406 134933 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 352 2 0 7 4.8 CSc1nn2cc(-c3nc4c(C)cc(Cl)cc4s3)nc2s1 nan
752812 2527 43 None 70 3 Human 6.9 pIC50 = 6.9 Functional
Antagonism measured in a novel PAC-1 fluorescent αIIbβ3 activation assay.Antagonism measured in a novel PAC-1 fluorescent αIIbβ3 activation assay.
Guide to Pharmacology 282 3 1 4 3.2 OCc1c(c2ccccc2)c2c(n1C)ccc(c2)[N+](=O)[O-] 25176330
9459 2527 43 None 70 3 Human 6.9 pIC50 = 6.9 Functional
Antagonism measured in a novel PAC-1 fluorescent αIIbβ3 activation assay.Antagonism measured in a novel PAC-1 fluorescent αIIbβ3 activation assay.
Guide to Pharmacology 282 3 1 4 3.2 OCc1c(c2ccccc2)c2c(n1C)ccc(c2)[N+](=O)[O-] 25176330
CHEMBL1609104 2527 43 None 70 3 Human 6.9 pIC50 = 6.9 Functional
Antagonism measured in a novel PAC-1 fluorescent αIIbβ3 activation assay.Antagonism measured in a novel PAC-1 fluorescent αIIbβ3 activation assay.
Guide to Pharmacology 282 3 1 4 3.2 OCc1c(c2ccccc2)c2c(n1C)ccc(c2)[N+](=O)[O-] 25176330
10132921 4034 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonism of PAR4-AP-stimulated human platelet aggregation.Antagonism of PAR4-AP-stimulated human platelet aggregation.
Guide to Pharmacology 356 5 0 4 4.9 CCOC(=O)c1ccc(cc1)c1nn(c2c1cccc2)Cc1ccccc1 25176330
9458 4034 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonism of PAR4-AP-stimulated human platelet aggregation.Antagonism of PAR4-AP-stimulated human platelet aggregation.
Guide to Pharmacology 356 5 0 4 4.9 CCOC(=O)c1ccc(cc1)c1nn(c2c1cccc2)Cc1ccccc1 25176330
CHEMBL125021 4034 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonism of PAR4-AP-stimulated human platelet aggregation.Antagonism of PAR4-AP-stimulated human platelet aggregation.
Guide to Pharmacology 356 5 0 4 4.9 CCOC(=O)c1ccc(cc1)c1nn(c2c1cccc2)Cc1ccccc1 25176330
10442 3846 3 None - 1 Human 8.6 pIC50 = 8.6 Functional
Measuring inhibition of PAR4 agonist-induced intracellular calcium mobilization in HEK293-PAR4 cells by FLIPR assay.Measuring inhibition of PAR4 agonist-induced intracellular calcium mobilization in HEK293-PAR4 cells by FLIPR assay.
Guide to Pharmacology 513 9 0 9 6.4 COc1cc(OCc2cccc(c2)OCc2ccccc2)c2c(c1)oc(c2)c1cn2c(n1)sc(n2)OC 31246024
71770951 3846 3 None - 1 Human 8.6 pIC50 = 8.6 Functional
Measuring inhibition of PAR4 agonist-induced intracellular calcium mobilization in HEK293-PAR4 cells by FLIPR assay.Measuring inhibition of PAR4 agonist-induced intracellular calcium mobilization in HEK293-PAR4 cells by FLIPR assay.
Guide to Pharmacology 513 9 0 9 6.4 COc1cc(OCc2cccc(c2)OCc2ccccc2)c2c(c1)oc(c2)c1cn2c(n1)sc(n2)OC 31246024
CHEMBL3728620 3846 3 None - 1 Human 8.6 pIC50 = 8.6 Functional
Measuring inhibition of PAR4 agonist-induced intracellular calcium mobilization in HEK293-PAR4 cells by FLIPR assay.Measuring inhibition of PAR4 agonist-induced intracellular calcium mobilization in HEK293-PAR4 cells by FLIPR assay.
Guide to Pharmacology 513 9 0 9 6.4 COc1cc(OCc2cccc(c2)OCc2ccccc2)c2c(c1)oc(c2)c1cn2c(n1)sc(n2)OC 31246024
10269 671 21 None - 1 Human 9.3 pIC50 = 9.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 513 7 0 12 4.4 COc1cc(OCc2nc(sc2C)N2CCOCC2)c2c(c1)oc(c2)c1cn2c(n1)sc(n2)OC 28053157
10269 671 21 None - 1 Human 9.3 pIC50 = 9.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 513 7 0 12 4.4 COc1cc(OCc2nc(sc2C)N2CCOCC2)c2c(c1)oc(c2)c1cn2c(n1)sc(n2)OC 35729784
72190270 671 21 None - 1 Human 9.3 pIC50 = 9.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 513 7 0 12 4.4 COc1cc(OCc2nc(sc2C)N2CCOCC2)c2c(c1)oc(c2)c1cn2c(n1)sc(n2)OC 28053157
72190270 671 21 None - 1 Human 9.3 pIC50 = 9.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 513 7 0 12 4.4 COc1cc(OCc2nc(sc2C)N2CCOCC2)c2c(c1)oc(c2)c1cn2c(n1)sc(n2)OC 35729784
CHEMBL3716726 671 21 None - 1 Human 9.3 pIC50 = 9.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 513 7 0 12 4.4 COc1cc(OCc2nc(sc2C)N2CCOCC2)c2c(c1)oc(c2)c1cn2c(n1)sc(n2)OC 28053157
CHEMBL3716726 671 21 None - 1 Human 9.3 pIC50 = 9.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 513 7 0 12 4.4 COc1cc(OCc2nc(sc2C)N2CCOCC2)c2c(c1)oc(c2)c1cn2c(n1)sc(n2)OC 35729784




Ligands Receptor Assay information Chemical information
Sel. page Common
name
GPCRdb ID #Vendors Reference
ligand
Fold selectivity
(Affinity)
# tested GPCRs
(Affinity)
Species p-value
(-log)
Type Activity
Relation
Activity
Value
Assay Type Assay Description Source Mol
weight
Rot
Bonds
H don H acc LogP Smiles DOI
71769562 133398 1 None - 0 Human 10.6 pIC50 = 10.6 Binding
Antagonist activity at PAR4 (unknown origin) assessed as inhibition of gamma-thrombin-induced receptor activationAntagonist activity at PAR4 (unknown origin) assessed as inhibition of gamma-thrombin-induced receptor activation
ChEMBL 490 7 0 10 5.9 COc1cc(OCc2csc(-c3ccccc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1016/j.bmcl.2016.10.020
CHEMBL3715848 133398 1 None - 0 Human 10.6 pIC50 = 10.6 Binding
Antagonist activity at PAR4 (unknown origin) assessed as inhibition of gamma-thrombin-induced receptor activationAntagonist activity at PAR4 (unknown origin) assessed as inhibition of gamma-thrombin-induced receptor activation
ChEMBL 490 7 0 10 5.9 COc1cc(OCc2csc(-c3ccccc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1016/j.bmcl.2016.10.020
89873469 147142 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Antagonist activity at PAR4 (unknown origin) assessed as inhibition of activating peptide-induced receptor activationAntagonist activity at PAR4 (unknown origin) assessed as inhibition of activating peptide-induced receptor activation
ChEMBL 271 2 0 6 3.2 COc1nn2cc(-c3cc4ccccc4o3)nc2s1 10.1016/j.bmcl.2016.10.020
CHEMBL3931873 147142 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Antagonist activity at PAR4 (unknown origin) assessed as inhibition of activating peptide-induced receptor activationAntagonist activity at PAR4 (unknown origin) assessed as inhibition of activating peptide-induced receptor activation
ChEMBL 271 2 0 6 3.2 COc1nn2cc(-c3cc4ccccc4o3)nc2s1 10.1016/j.bmcl.2016.10.020
164622799 185263 0 None - 0 Mouse 6.0 pIC50 = 6 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 401 4 0 7 4.2 COCn1cnc2c(-c3nc4c(Cl)cc(OC)cc4s3)cc(C)cc2c1=O 10.1016/j.ejmech.2021.113764
CHEMBL4867779 185263 0 None - 0 Mouse 6.0 pIC50 = 6 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 401 4 0 7 4.2 COCn1cnc2c(-c3nc4c(Cl)cc(OC)cc4s3)cc(C)cc2c1=O 10.1016/j.ejmech.2021.113764
134137936 147369 0 None - 0 Human 6.0 pIC50 = 6 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of gamma-thrombin-induced P-selectin activationAntagonist activity at PAR4 in human platelets assessed as inhibition of gamma-thrombin-induced P-selectin activation
ChEMBL 368 3 0 7 3.9 COc1nn2cc(-c3cc4cc(OC(F)(F)F)ccc4n3C)nc2s1 10.1016/j.bmcl.2016.10.020
CHEMBL3933579 147369 0 None - 0 Human 6.0 pIC50 = 6 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of gamma-thrombin-induced P-selectin activationAntagonist activity at PAR4 in human platelets assessed as inhibition of gamma-thrombin-induced P-selectin activation
ChEMBL 368 3 0 7 3.9 COc1nn2cc(-c3cc4cc(OC(F)(F)F)ccc4n3C)nc2s1 10.1016/j.bmcl.2016.10.020
134137936 147369 0 None - 0 Human 6.0 pIC50 = 6 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of gamma-thrombin-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of gamma-thrombin-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 368 3 0 7 3.9 COc1nn2cc(-c3cc4cc(OC(F)(F)F)ccc4n3C)nc2s1 10.1016/j.bmcl.2016.10.020
CHEMBL3933579 147369 0 None - 0 Human 6.0 pIC50 = 6 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of gamma-thrombin-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of gamma-thrombin-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 368 3 0 7 3.9 COc1nn2cc(-c3cc4cc(OC(F)(F)F)ccc4n3C)nc2s1 10.1016/j.bmcl.2016.10.020
72201708 135600 0 None - 0 Human 6.0 pIC50 = 6 Binding
Antagonist activity at PAR4 in human washed platelets assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured every 50 secs for up to 15 mins starting from 10 secs post gamma-thrombin addition in presence of recombinant hirudinAntagonist activity at PAR4 in human washed platelets assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured every 50 secs for up to 15 mins starting from 10 secs post gamma-thrombin addition in presence of recombinant hirudin
ChEMBL 407 6 0 8 4.8 COc1cc(OCc2ccccc2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.9b00186
CHEMBL3732490 135600 0 None - 0 Human 6.0 pIC50 = 6 Binding
Antagonist activity at PAR4 in human washed platelets assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured every 50 secs for up to 15 mins starting from 10 secs post gamma-thrombin addition in presence of recombinant hirudinAntagonist activity at PAR4 in human washed platelets assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured every 50 secs for up to 15 mins starting from 10 secs post gamma-thrombin addition in presence of recombinant hirudin
ChEMBL 407 6 0 8 4.8 COc1cc(OCc2ccccc2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.9b00186
164608789 183786 0 None - 0 Mouse 5.0 pIC50 = 5 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 315 4 0 7 3.4 COCc1cc2ccc(OC)c(-c3nn4ccnc4s3)c2o1 10.1016/j.ejmech.2021.113764
CHEMBL4845694 183786 0 None - 0 Mouse 5.0 pIC50 = 5 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 315 4 0 7 3.4 COCc1cc2ccc(OC)c(-c3nn4ccnc4s3)c2o1 10.1016/j.ejmech.2021.113764
164609914 184666 0 None - 0 Mouse 5.0 pIC50 = 5 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 329 4 0 7 3.7 COCc1cc2ccc(OC)c(-c3nn4cc(C)nc4s3)c2o1 10.1016/j.ejmech.2021.113764
CHEMBL4858534 184666 0 None - 0 Mouse 5.0 pIC50 = 5 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 329 4 0 7 3.7 COCc1cc2ccc(OC)c(-c3nn4cc(C)nc4s3)c2o1 10.1016/j.ejmech.2021.113764
118714140 113972 0 None - 0 Human 5.0 pIC50 = 5 Binding
Antagonist activity at PAR4 in PAR-4-AP-stimulated human platelets compound pretreated for 5 mins by fluorescent PAC1 integrin alpha2bb3 activation assayAntagonist activity at PAR4 in PAR-4-AP-stimulated human platelets compound pretreated for 5 mins by fluorescent PAC1 integrin alpha2bb3 activation assay
ChEMBL 429 6 1 6 4.5 COc1ccc(-c2c(CO)n(Cc3cccc(OC(F)(F)F)c3)c3ncccc23)cn1 10.1016/j.bmcl.2014.08.021
CHEMBL3334933 113972 0 None - 0 Human 5.0 pIC50 = 5 Binding
Antagonist activity at PAR4 in PAR-4-AP-stimulated human platelets compound pretreated for 5 mins by fluorescent PAC1 integrin alpha2bb3 activation assayAntagonist activity at PAR4 in PAR-4-AP-stimulated human platelets compound pretreated for 5 mins by fluorescent PAC1 integrin alpha2bb3 activation assay
ChEMBL 429 6 1 6 4.5 COc1ccc(-c2c(CO)n(Cc3cccc(OC(F)(F)F)c3)c3ncccc23)cn1 10.1016/j.bmcl.2014.08.021
118068468 134791 0 None - 0 Human 5.0 pIC50 = 5 Binding
Antagonist activity at PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured in presence of recombinant hirudinAntagonist activity at PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured in presence of recombinant hirudin
ChEMBL 331 4 0 8 3.2 COc1nn2cc(-c3cc4c(OC)ccc(OC)c4o3)nc2s1 10.1021/acs.jmedchem.9b00186
CHEMBL3727598 134791 0 None - 0 Human 5.0 pIC50 = 5 Binding
Antagonist activity at PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured in presence of recombinant hirudinAntagonist activity at PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured in presence of recombinant hirudin
ChEMBL 331 4 0 8 3.2 COc1nn2cc(-c3cc4c(OC)ccc(OC)c4o3)nc2s1 10.1021/acs.jmedchem.9b00186
164621177 185499 0 None - 0 Mouse 6.0 pIC50 = 6.0 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 574 7 1 8 5.2 Cc1cc(-c2nc3c(Cl)cc(OCCNS(=O)(=O)c4ccc(Cl)cc4)cc3s2)c2ncn(C)c(=O)c2c1 10.1016/j.ejmech.2021.113764
CHEMBL4871578 185499 0 None - 0 Mouse 6.0 pIC50 = 6.0 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 574 7 1 8 5.2 Cc1cc(-c2nc3c(Cl)cc(OCCNS(=O)(=O)c4ccc(Cl)cc4)cc3s2)c2ncn(C)c(=O)c2c1 10.1016/j.ejmech.2021.113764
132051298 143451 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of gamma-thrombin-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of gamma-thrombin-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 317 2 0 5 3.6 COc1nn2cc(-c3ccc(F)c(C(F)(F)F)c3)nc2s1 10.1016/j.bmcl.2016.10.020
CHEMBL3902806 143451 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of gamma-thrombin-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of gamma-thrombin-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 317 2 0 5 3.6 COc1nn2cc(-c3ccc(F)c(C(F)(F)F)c3)nc2s1 10.1016/j.bmcl.2016.10.020
132051298 143451 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of gamma-thrombin-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of gamma-thrombin-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 317 2 0 5 3.6 COc1nn2cc(-c3ccc(F)c(C(F)(F)F)c3)nc2s1 10.1016/j.bmcl.2016.10.020
CHEMBL3902806 143451 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of gamma-thrombin-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of gamma-thrombin-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 317 2 0 5 3.6 COc1nn2cc(-c3ccc(F)c(C(F)(F)F)c3)nc2s1 10.1016/j.bmcl.2016.10.020
132051221 143870 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced P-selectin activationAntagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced P-selectin activation
ChEMBL 299 2 0 5 3.5 COc1nn2cc(-c3ccc(C(F)(F)F)cc3)nc2s1 10.1016/j.bmcl.2016.10.020
CHEMBL3906197 143870 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced P-selectin activationAntagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced P-selectin activation
ChEMBL 299 2 0 5 3.5 COc1nn2cc(-c3ccc(C(F)(F)F)cc3)nc2s1 10.1016/j.bmcl.2016.10.020
164622285 185187 0 None - 0 Mouse 7.0 pIC50 = 7.0 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 311 1 0 5 3.2 Cc1cc(-c2nc3c(s2)CCCC3)c2ncn(C)c(=O)c2c1 10.1016/j.ejmech.2021.113764
CHEMBL4866566 185187 0 None - 0 Mouse 7.0 pIC50 = 7.0 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 311 1 0 5 3.2 Cc1cc(-c2nc3c(s2)CCCC3)c2ncn(C)c(=O)c2c1 10.1016/j.ejmech.2021.113764
118068437 134939 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at PAR4 in human washed platelets assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured every 50 secs for up to 15 mins starting from 10 secs post gamma-thrombin addition in presence of recombinant hirudinAntagonist activity at PAR4 in human washed platelets assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured every 50 secs for up to 15 mins starting from 10 secs post gamma-thrombin addition in presence of recombinant hirudin
ChEMBL 301 3 0 7 3.2 COc1ccc2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.9b00186
CHEMBL3728462 134939 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at PAR4 in human washed platelets assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured every 50 secs for up to 15 mins starting from 10 secs post gamma-thrombin addition in presence of recombinant hirudinAntagonist activity at PAR4 in human washed platelets assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured every 50 secs for up to 15 mins starting from 10 secs post gamma-thrombin addition in presence of recombinant hirudin
ChEMBL 301 3 0 7 3.2 COc1ccc2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.9b00186
155515625 169383 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Antagonist activity at PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured in presence of recombinant hirudinAntagonist activity at PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured in presence of recombinant hirudin
ChEMBL 511 9 0 8 6.6 COc1cc(OCc2cccc(CCc3ccccc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.9b00186
CHEMBL4441723 169383 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Antagonist activity at PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured in presence of recombinant hirudinAntagonist activity at PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured in presence of recombinant hirudin
ChEMBL 511 9 0 8 6.6 COc1cc(OCc2cccc(CCc3ccccc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.9b00186
132051242 149306 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 309 3 0 7 1.9 COc1nn2cc(-c3ccc(S(C)(=O)=O)cc3)nc2s1 10.1016/j.bmcl.2016.10.020
CHEMBL3948984 149306 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 309 3 0 7 1.9 COc1nn2cc(-c3ccc(S(C)(=O)=O)cc3)nc2s1 10.1016/j.bmcl.2016.10.020
132051242 149306 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 309 3 0 7 1.9 COc1nn2cc(-c3ccc(S(C)(=O)=O)cc3)nc2s1 10.1016/j.bmcl.2016.10.020
CHEMBL3948984 149306 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 309 3 0 7 1.9 COc1nn2cc(-c3ccc(S(C)(=O)=O)cc3)nc2s1 10.1016/j.bmcl.2016.10.020
164610439 184729 0 None - 0 Mouse 5.9 pIC50 = 5.9 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 318 1 0 3 4.2 Cc1cc(-c2ccc(Cl)cc2Cl)c2ncn(C)c(=O)c2c1 10.1016/j.ejmech.2021.113764
CHEMBL4859532 184729 0 None - 0 Mouse 5.9 pIC50 = 5.9 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 318 1 0 3 4.2 Cc1cc(-c2ccc(Cl)cc2Cl)c2ncn(C)c(=O)c2c1 10.1016/j.ejmech.2021.113764
132051300 151018 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 267 2 0 5 2.7 COc1nn2cc(-c3c(F)cccc3F)nc2s1 10.1016/j.bmcl.2016.10.020
CHEMBL3963226 151018 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 267 2 0 5 2.7 COc1nn2cc(-c3c(F)cccc3F)nc2s1 10.1016/j.bmcl.2016.10.020
10132921 4034 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity PAR4 (unknown origin)Antagonist activity PAR4 (unknown origin)
ChEMBL 356 5 0 4 4.9 CCOC(=O)c1ccc(cc1)c1nn(c2c1cccc2)Cc1ccccc1 10.1021/acs.jmedchem.6b00928
9458 4034 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity PAR4 (unknown origin)Antagonist activity PAR4 (unknown origin)
ChEMBL 356 5 0 4 4.9 CCOC(=O)c1ccc(cc1)c1nn(c2c1cccc2)Cc1ccccc1 10.1021/acs.jmedchem.6b00928
CHEMBL125021 4034 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity PAR4 (unknown origin)Antagonist activity PAR4 (unknown origin)
ChEMBL 356 5 0 4 4.9 CCOC(=O)c1ccc(cc1)c1nn(c2c1cccc2)Cc1ccccc1 10.1021/acs.jmedchem.6b00928
10132921 4034 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at PAR4 in PAR-4-AP-stimulated human platelets compound pretreated for 5 mins by fluorescent PAC1 integrin alpha2bb3 activation assayAntagonist activity at PAR4 in PAR-4-AP-stimulated human platelets compound pretreated for 5 mins by fluorescent PAC1 integrin alpha2bb3 activation assay
ChEMBL 356 5 0 4 4.9 CCOC(=O)c1ccc(cc1)c1nn(c2c1cccc2)Cc1ccccc1 10.1016/j.bmcl.2014.08.021
9458 4034 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at PAR4 in PAR-4-AP-stimulated human platelets compound pretreated for 5 mins by fluorescent PAC1 integrin alpha2bb3 activation assayAntagonist activity at PAR4 in PAR-4-AP-stimulated human platelets compound pretreated for 5 mins by fluorescent PAC1 integrin alpha2bb3 activation assay
ChEMBL 356 5 0 4 4.9 CCOC(=O)c1ccc(cc1)c1nn(c2c1cccc2)Cc1ccccc1 10.1016/j.bmcl.2014.08.021
CHEMBL125021 4034 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at PAR4 in PAR-4-AP-stimulated human platelets compound pretreated for 5 mins by fluorescent PAC1 integrin alpha2bb3 activation assayAntagonist activity at PAR4 in PAR-4-AP-stimulated human platelets compound pretreated for 5 mins by fluorescent PAC1 integrin alpha2bb3 activation assay
ChEMBL 356 5 0 4 4.9 CCOC(=O)c1ccc(cc1)c1nn(c2c1cccc2)Cc1ccccc1 10.1016/j.bmcl.2014.08.021
118068374 169218 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Antagonist activity at PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured in presence of recombinant hirudinAntagonist activity at PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured in presence of recombinant hirudin
ChEMBL 301 3 0 7 3.2 COc1nn2cc(-c3cc4c(OC)cccc4o3)nc2s1 10.1021/acs.jmedchem.9b00186
CHEMBL4439280 169218 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Antagonist activity at PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured in presence of recombinant hirudinAntagonist activity at PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured in presence of recombinant hirudin
ChEMBL 301 3 0 7 3.2 COc1nn2cc(-c3cc4c(OC)cccc4o3)nc2s1 10.1021/acs.jmedchem.9b00186
132051300 151018 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 267 2 0 5 2.7 COc1nn2cc(-c3c(F)cccc3F)nc2s1 10.1016/j.bmcl.2016.10.020
CHEMBL3963226 151018 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 267 2 0 5 2.7 COc1nn2cc(-c3c(F)cccc3F)nc2s1 10.1016/j.bmcl.2016.10.020
132051219 149466 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of gamma-thrombin-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of gamma-thrombin-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 299 2 0 5 3.5 COc1nn2cc(-c3cccc(C(F)(F)F)c3)nc2s1 10.1016/j.bmcl.2016.10.020
CHEMBL3950308 149466 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of gamma-thrombin-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of gamma-thrombin-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 299 2 0 5 3.5 COc1nn2cc(-c3cccc(C(F)(F)F)c3)nc2s1 10.1016/j.bmcl.2016.10.020
132051220 145483 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 299 2 0 5 3.5 COc1nn2cc(-c3ccccc3C(F)(F)F)nc2s1 10.1016/j.bmcl.2016.10.020
CHEMBL3918711 145483 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 299 2 0 5 3.5 COc1nn2cc(-c3ccccc3C(F)(F)F)nc2s1 10.1016/j.bmcl.2016.10.020
132051219 149466 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of gamma-thrombin-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of gamma-thrombin-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 299 2 0 5 3.5 COc1nn2cc(-c3cccc(C(F)(F)F)c3)nc2s1 10.1016/j.bmcl.2016.10.020
CHEMBL3950308 149466 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of gamma-thrombin-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of gamma-thrombin-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 299 2 0 5 3.5 COc1nn2cc(-c3cccc(C(F)(F)F)c3)nc2s1 10.1016/j.bmcl.2016.10.020
118953461 174414 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity against PAR4 activating peptide domain in in human platelets assessed as inhibition of P-selectin activationAntagonist activity against PAR4 activating peptide domain in in human platelets assessed as inhibition of P-selectin activation
ChEMBL 508 6 1 8 5.5 COc1nn2cc(-c3c(CO)n(Cc4ccccc4Cl)c4ccc(OC(F)(F)F)cc34)nc2s1 10.1021/acs.jmedchem.6b00928
CHEMBL4566669 174414 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity against PAR4 activating peptide domain in in human platelets assessed as inhibition of P-selectin activationAntagonist activity against PAR4 activating peptide domain in in human platelets assessed as inhibition of P-selectin activation
ChEMBL 508 6 1 8 5.5 COc1nn2cc(-c3c(CO)n(Cc4ccccc4Cl)c4ccc(OC(F)(F)F)cc34)nc2s1 10.1021/acs.jmedchem.6b00928
132051220 145483 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 299 2 0 5 3.5 COc1nn2cc(-c3ccccc3C(F)(F)F)nc2s1 10.1016/j.bmcl.2016.10.020
CHEMBL3918711 145483 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 299 2 0 5 3.5 COc1nn2cc(-c3ccccc3C(F)(F)F)nc2s1 10.1016/j.bmcl.2016.10.020
118971366 174434 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Antagonist activity against PAR4 activating peptide domain in human platelets assessed as inhibition of alpha2bbeta3 activation level by PAC1 binding assayAntagonist activity against PAR4 activating peptide domain in human platelets assessed as inhibition of alpha2bbeta3 activation level by PAC1 binding assay
ChEMBL 481 6 1 6 5.5 CSc1ncc(-c2c(CO)n(Cc3ccc(F)cc3F)c3ccc(OC(F)(F)F)cc23)cn1 10.1021/acs.jmedchem.6b00928
CHEMBL4567147 174434 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Antagonist activity against PAR4 activating peptide domain in human platelets assessed as inhibition of alpha2bbeta3 activation level by PAC1 binding assayAntagonist activity against PAR4 activating peptide domain in human platelets assessed as inhibition of alpha2bbeta3 activation level by PAC1 binding assay
ChEMBL 481 6 1 6 5.5 CSc1ncc(-c2c(CO)n(Cc3ccc(F)cc3F)c3ccc(OC(F)(F)F)cc23)cn1 10.1021/acs.jmedchem.6b00928
118971366 174434 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Antagonist activity against PAR4 activating peptide domain in human platelets assessed as inhibition of alpha2bbeta3 activation level by PAC1 binding assayAntagonist activity against PAR4 activating peptide domain in human platelets assessed as inhibition of alpha2bbeta3 activation level by PAC1 binding assay
ChEMBL 481 6 1 6 5.5 CSc1ncc(-c2c(CO)n(Cc3ccc(F)cc3F)c3ccc(OC(F)(F)F)cc23)cn1 10.1021/acs.jmedchem.6b00928
CHEMBL4567147 174434 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Antagonist activity against PAR4 activating peptide domain in human platelets assessed as inhibition of alpha2bbeta3 activation level by PAC1 binding assayAntagonist activity against PAR4 activating peptide domain in human platelets assessed as inhibition of alpha2bbeta3 activation level by PAC1 binding assay
ChEMBL 481 6 1 6 5.5 CSc1ncc(-c2c(CO)n(Cc3ccc(F)cc3F)c3ccc(OC(F)(F)F)cc23)cn1 10.1021/acs.jmedchem.6b00928
164615515 184018 0 None - 0 Mouse 5.9 pIC50 = 5.9 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 297 1 1 4 3.2 Cc1cc(-c2nc3c(s2)CCCC3)c2nc[nH]c(=O)c2c1 10.1016/j.ejmech.2021.113764
CHEMBL4849024 184018 0 None - 0 Mouse 5.9 pIC50 = 5.9 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 297 1 1 4 3.2 Cc1cc(-c2nc3c(s2)CCCC3)c2nc[nH]c(=O)c2c1 10.1016/j.ejmech.2021.113764
164622783 185229 0 None - 0 Mouse 5.9 pIC50 = 5.9 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 413 5 0 6 5.2 CCCCc1cc(-c2nc3c(Cl)cc(OC)cc3s2)c2ncn(C)c(=O)c2c1 10.1016/j.ejmech.2021.113764
CHEMBL4867321 185229 0 None - 0 Mouse 5.9 pIC50 = 5.9 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 413 5 0 6 5.2 CCCCc1cc(-c2nc3c(Cl)cc(OC)cc3s2)c2ncn(C)c(=O)c2c1 10.1016/j.ejmech.2021.113764
118971054 173178 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Antagonist activity against PAR4 activating peptide domain in human platelets assessed as inhibition of alpha2bbeta3 activation level by PAC1 binding assayAntagonist activity against PAR4 activating peptide domain in human platelets assessed as inhibition of alpha2bbeta3 activation level by PAC1 binding assay
ChEMBL 408 6 1 5 4.9 COc1ccc2c(-c3ccc(OC)nc3)c(CO)n(Cc3ccccc3Cl)c2c1 10.1021/acs.jmedchem.6b00928
CHEMBL4537098 173178 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Antagonist activity against PAR4 activating peptide domain in human platelets assessed as inhibition of alpha2bbeta3 activation level by PAC1 binding assayAntagonist activity against PAR4 activating peptide domain in human platelets assessed as inhibition of alpha2bbeta3 activation level by PAC1 binding assay
ChEMBL 408 6 1 5 4.9 COc1ccc2c(-c3ccc(OC)nc3)c(CO)n(Cc3ccccc3Cl)c2c1 10.1021/acs.jmedchem.6b00928
118971054 173178 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Antagonist activity against PAR4 activating peptide domain in human platelets assessed as inhibition of alpha2bbeta3 activation level by PAC1 binding assayAntagonist activity against PAR4 activating peptide domain in human platelets assessed as inhibition of alpha2bbeta3 activation level by PAC1 binding assay
ChEMBL 408 6 1 5 4.9 COc1ccc2c(-c3ccc(OC)nc3)c(CO)n(Cc3ccccc3Cl)c2c1 10.1021/acs.jmedchem.6b00928
CHEMBL4537098 173178 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Antagonist activity against PAR4 activating peptide domain in human platelets assessed as inhibition of alpha2bbeta3 activation level by PAC1 binding assayAntagonist activity against PAR4 activating peptide domain in human platelets assessed as inhibition of alpha2bbeta3 activation level by PAC1 binding assay
ChEMBL 408 6 1 5 4.9 COc1ccc2c(-c3ccc(OC)nc3)c(CO)n(Cc3ccccc3Cl)c2c1 10.1021/acs.jmedchem.6b00928
752812 2527 43 None - 0 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at PAR4 in PAR-4-AP-stimulated human platelets compound pretreated for 5 mins by fluorescent PAC1 integrin alpha2bb3 activation assayAntagonist activity at PAR4 in PAR-4-AP-stimulated human platelets compound pretreated for 5 mins by fluorescent PAC1 integrin alpha2bb3 activation assay
ChEMBL 282 3 1 4 3.2 OCc1c(c2ccccc2)c2c(n1C)ccc(c2)[N+](=O)[O-] 10.1016/j.bmcl.2014.08.021
9459 2527 43 None - 0 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at PAR4 in PAR-4-AP-stimulated human platelets compound pretreated for 5 mins by fluorescent PAC1 integrin alpha2bb3 activation assayAntagonist activity at PAR4 in PAR-4-AP-stimulated human platelets compound pretreated for 5 mins by fluorescent PAC1 integrin alpha2bb3 activation assay
ChEMBL 282 3 1 4 3.2 OCc1c(c2ccccc2)c2c(n1C)ccc(c2)[N+](=O)[O-] 10.1016/j.bmcl.2014.08.021
CHEMBL1609104 2527 43 None - 0 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at PAR4 in PAR-4-AP-stimulated human platelets compound pretreated for 5 mins by fluorescent PAC1 integrin alpha2bb3 activation assayAntagonist activity at PAR4 in PAR-4-AP-stimulated human platelets compound pretreated for 5 mins by fluorescent PAC1 integrin alpha2bb3 activation assay
ChEMBL 282 3 1 4 3.2 OCc1c(c2ccccc2)c2c(n1C)ccc(c2)[N+](=O)[O-] 10.1016/j.bmcl.2014.08.021
132051238 144286 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of gamma-thrombin-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of gamma-thrombin-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 299 2 0 5 3.8 COc1nn2cc(-c3ccc(Cl)c(Cl)c3)nc2s1 10.1016/j.bmcl.2016.10.020
CHEMBL3909608 144286 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of gamma-thrombin-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of gamma-thrombin-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 299 2 0 5 3.8 COc1nn2cc(-c3ccc(Cl)c(Cl)c3)nc2s1 10.1016/j.bmcl.2016.10.020
132051238 144286 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of gamma-thrombin-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of gamma-thrombin-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 299 2 0 5 3.8 COc1nn2cc(-c3ccc(Cl)c(Cl)c3)nc2s1 10.1016/j.bmcl.2016.10.020
CHEMBL3909608 144286 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of gamma-thrombin-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of gamma-thrombin-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 299 2 0 5 3.8 COc1nn2cc(-c3ccc(Cl)c(Cl)c3)nc2s1 10.1016/j.bmcl.2016.10.020
132051221 143870 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 299 2 0 5 3.5 COc1nn2cc(-c3ccc(C(F)(F)F)cc3)nc2s1 10.1016/j.bmcl.2016.10.020
CHEMBL3906197 143870 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 299 2 0 5 3.5 COc1nn2cc(-c3ccc(C(F)(F)F)cc3)nc2s1 10.1016/j.bmcl.2016.10.020
132051221 143870 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 299 2 0 5 3.5 COc1nn2cc(-c3ccc(C(F)(F)F)cc3)nc2s1 10.1016/j.bmcl.2016.10.020
CHEMBL3906197 143870 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 299 2 0 5 3.5 COc1nn2cc(-c3ccc(C(F)(F)F)cc3)nc2s1 10.1016/j.bmcl.2016.10.020
118971373 174596 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Antagonist activity against PAR4 activating peptide domain in human platelets assessed as inhibition of alpha2bbeta3 activation level by PAC1 binding assayAntagonist activity against PAR4 activating peptide domain in human platelets assessed as inhibition of alpha2bbeta3 activation level by PAC1 binding assay
ChEMBL 463 6 1 6 5.2 COc1ncc(-c2c(CO)n(Cc3ccccc3Cl)c3ccc(OC(F)(F)F)cc23)cn1 10.1021/acs.jmedchem.6b00928
CHEMBL4570494 174596 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Antagonist activity against PAR4 activating peptide domain in human platelets assessed as inhibition of alpha2bbeta3 activation level by PAC1 binding assayAntagonist activity against PAR4 activating peptide domain in human platelets assessed as inhibition of alpha2bbeta3 activation level by PAC1 binding assay
ChEMBL 463 6 1 6 5.2 COc1ncc(-c2c(CO)n(Cc3ccccc3Cl)c3ccc(OC(F)(F)F)cc23)cn1 10.1021/acs.jmedchem.6b00928
89873469 147142 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Antagonist activity at PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured in presence of recombinant hirudinAntagonist activity at PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured in presence of recombinant hirudin
ChEMBL 271 2 0 6 3.2 COc1nn2cc(-c3cc4ccccc4o3)nc2s1 10.1021/acs.jmedchem.9b00186
CHEMBL3931873 147142 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Antagonist activity at PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured in presence of recombinant hirudinAntagonist activity at PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured in presence of recombinant hirudin
ChEMBL 271 2 0 6 3.2 COc1nn2cc(-c3cc4ccccc4o3)nc2s1 10.1021/acs.jmedchem.9b00186
118971373 174596 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Antagonist activity against PAR4 activating peptide domain in human platelets assessed as inhibition of alpha2bbeta3 activation level by PAC1 binding assayAntagonist activity against PAR4 activating peptide domain in human platelets assessed as inhibition of alpha2bbeta3 activation level by PAC1 binding assay
ChEMBL 463 6 1 6 5.2 COc1ncc(-c2c(CO)n(Cc3ccccc3Cl)c3ccc(OC(F)(F)F)cc23)cn1 10.1021/acs.jmedchem.6b00928
CHEMBL4570494 174596 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Antagonist activity against PAR4 activating peptide domain in human platelets assessed as inhibition of alpha2bbeta3 activation level by PAC1 binding assayAntagonist activity against PAR4 activating peptide domain in human platelets assessed as inhibition of alpha2bbeta3 activation level by PAC1 binding assay
ChEMBL 463 6 1 6 5.2 COc1ncc(-c2c(CO)n(Cc3ccccc3Cl)c3ccc(OC(F)(F)F)cc23)cn1 10.1021/acs.jmedchem.6b00928
164616125 184049 0 None - 0 Mouse 6.8 pIC50 = 6.8 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 385 3 0 6 4.4 CCc1cc(-c2nc3c(Cl)cc(OC)cc3s2)c2ncn(C)c(=O)c2c1 10.1016/j.ejmech.2021.113764
CHEMBL4849569 184049 0 None - 0 Mouse 6.8 pIC50 = 6.8 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 385 3 0 6 4.4 CCc1cc(-c2nc3c(Cl)cc(OC)cc3s2)c2ncn(C)c(=O)c2c1 10.1016/j.ejmech.2021.113764
72201708 135600 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Antagonist activity at PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured in presence of recombinant hirudinAntagonist activity at PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured in presence of recombinant hirudin
ChEMBL 407 6 0 8 4.8 COc1cc(OCc2ccccc2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.9b00186
CHEMBL3732490 135600 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Antagonist activity at PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured in presence of recombinant hirudinAntagonist activity at PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured in presence of recombinant hirudin
ChEMBL 407 6 0 8 4.8 COc1cc(OCc2ccccc2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.9b00186
164622974 185532 0 None - 0 Mouse 5.8 pIC50 = 5.8 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 373 4 1 5 5.0 COCc1nc2cc(C)cc(-c3nc4c(Cl)cc(OC)cc4s3)c2[nH]1 10.1016/j.ejmech.2021.113764
CHEMBL4871870 185532 0 None - 0 Mouse 5.8 pIC50 = 5.8 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 373 4 1 5 5.0 COCc1nc2cc(C)cc(-c3nc4c(Cl)cc(OC)cc4s3)c2[nH]1 10.1016/j.ejmech.2021.113764
164610234 184488 0 None - 0 Mouse 6.8 pIC50 = 6.8 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 608 7 1 8 5.5 Cc1cc(-c2nc3c(Cl)cc(OCCNS(=O)(=O)c4ccc(C(F)(F)F)cc4)cc3s2)c2ncn(C)c(=O)c2c1 10.1016/j.ejmech.2021.113764
CHEMBL4855875 184488 0 None - 0 Mouse 6.8 pIC50 = 6.8 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 608 7 1 8 5.5 Cc1cc(-c2nc3c(Cl)cc(OCCNS(=O)(=O)c4ccc(C(F)(F)F)cc4)cc3s2)c2ncn(C)c(=O)c2c1 10.1016/j.ejmech.2021.113764
132051301 144676 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 267 2 0 5 2.7 COc1nn2cc(-c3ccc(F)cc3F)nc2s1 10.1016/j.bmcl.2016.10.020
CHEMBL3912611 144676 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 267 2 0 5 2.7 COc1nn2cc(-c3ccc(F)cc3F)nc2s1 10.1016/j.bmcl.2016.10.020
132051301 144676 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 267 2 0 5 2.7 COc1nn2cc(-c3ccc(F)cc3F)nc2s1 10.1016/j.bmcl.2016.10.020
CHEMBL3912611 144676 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 267 2 0 5 2.7 COc1nn2cc(-c3ccc(F)cc3F)nc2s1 10.1016/j.bmcl.2016.10.020
118953461 174414 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Antagonist activity against PAR4 activating peptide domain in human platelets assessed as inhibition of alpha2bbeta3 activation level by PAC1 binding assayAntagonist activity against PAR4 activating peptide domain in human platelets assessed as inhibition of alpha2bbeta3 activation level by PAC1 binding assay
ChEMBL 508 6 1 8 5.5 COc1nn2cc(-c3c(CO)n(Cc4ccccc4Cl)c4ccc(OC(F)(F)F)cc34)nc2s1 10.1021/acs.jmedchem.6b00928
CHEMBL4566669 174414 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Antagonist activity against PAR4 activating peptide domain in human platelets assessed as inhibition of alpha2bbeta3 activation level by PAC1 binding assayAntagonist activity against PAR4 activating peptide domain in human platelets assessed as inhibition of alpha2bbeta3 activation level by PAC1 binding assay
ChEMBL 508 6 1 8 5.5 COc1nn2cc(-c3c(CO)n(Cc4ccccc4Cl)c4ccc(OC(F)(F)F)cc34)nc2s1 10.1021/acs.jmedchem.6b00928
118953461 174414 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Antagonist activity against PAR4 activating peptide domain in human platelets assessed as inhibition of alpha2bbeta3 activation level by PAC1 binding assayAntagonist activity against PAR4 activating peptide domain in human platelets assessed as inhibition of alpha2bbeta3 activation level by PAC1 binding assay
ChEMBL 508 6 1 8 5.5 COc1nn2cc(-c3c(CO)n(Cc4ccccc4Cl)c4ccc(OC(F)(F)F)cc34)nc2s1 10.1021/acs.jmedchem.6b00928
CHEMBL4566669 174414 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Antagonist activity against PAR4 activating peptide domain in human platelets assessed as inhibition of alpha2bbeta3 activation level by PAC1 binding assayAntagonist activity against PAR4 activating peptide domain in human platelets assessed as inhibition of alpha2bbeta3 activation level by PAC1 binding assay
ChEMBL 508 6 1 8 5.5 COc1nn2cc(-c3c(CO)n(Cc4ccccc4Cl)c4ccc(OC(F)(F)F)cc34)nc2s1 10.1021/acs.jmedchem.6b00928
155523135 170176 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Antagonist activity at PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured in presence of recombinant hirudinAntagonist activity at PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured in presence of recombinant hirudin
ChEMBL 475 6 0 8 5.8 COc1cc(OCc2ccc(C(F)(F)F)cc2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.9b00186
CHEMBL4452516 170176 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Antagonist activity at PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured in presence of recombinant hirudinAntagonist activity at PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured in presence of recombinant hirudin
ChEMBL 475 6 0 8 5.8 COc1cc(OCc2ccc(C(F)(F)F)cc2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.9b00186
118068465 135476 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Antagonist activity at PAR4 in human washed platelets assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured every 50 secs for up to 15 mins starting from 10 secs post gamma-thrombin addition in presence of recombinant hirudinAntagonist activity at PAR4 in human washed platelets assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured every 50 secs for up to 15 mins starting from 10 secs post gamma-thrombin addition in presence of recombinant hirudin
ChEMBL 377 5 0 7 4.8 COc1nn2cc(-c3cc4ccc(OCc5ccccc5)cc4o3)nc2s1 10.1021/acs.jmedchem.9b00186
CHEMBL3731720 135476 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Antagonist activity at PAR4 in human washed platelets assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured every 50 secs for up to 15 mins starting from 10 secs post gamma-thrombin addition in presence of recombinant hirudinAntagonist activity at PAR4 in human washed platelets assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured every 50 secs for up to 15 mins starting from 10 secs post gamma-thrombin addition in presence of recombinant hirudin
ChEMBL 377 5 0 7 4.8 COc1nn2cc(-c3cc4ccc(OCc5ccccc5)cc4o3)nc2s1 10.1021/acs.jmedchem.9b00186
89880953 134859 1 None - 0 Mouse 5.7 pIC50 = 5.7 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 255 1 0 5 3.5 Cc1nn2cc(-c3cc4ccccc4o3)nc2s1 10.1016/j.ejmech.2021.113764
CHEMBL3728010 134859 1 None - 0 Mouse 5.7 pIC50 = 5.7 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 255 1 0 5 3.5 Cc1nn2cc(-c3cc4ccccc4o3)nc2s1 10.1016/j.ejmech.2021.113764
164609947 183923 0 None - 0 Mouse 5.7 pIC50 = 5.7 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 372 2 0 4 4.6 COc1cc(Cl)c2nc(-c3cc(C)cc4c3CCN(C)C4=O)sc2c1 10.1016/j.ejmech.2021.113764
CHEMBL4847592 183923 0 None - 0 Mouse 5.7 pIC50 = 5.7 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 372 2 0 4 4.6 COc1cc(Cl)c2nc(-c3cc(C)cc4c3CCN(C)C4=O)sc2c1 10.1016/j.ejmech.2021.113764
164614838 184681 0 None - 0 Mouse 5.7 pIC50 = 5.7 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 385 3 0 6 4.7 CCn1cnc2c(-c3nc4c(Cl)cc(OC)cc4s3)cc(C)cc2c1=O 10.1016/j.ejmech.2021.113764
CHEMBL4858844 184681 0 None - 0 Mouse 5.7 pIC50 = 5.7 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 385 3 0 6 4.7 CCn1cnc2c(-c3nc4c(Cl)cc(OC)cc4s3)cc(C)cc2c1=O 10.1016/j.ejmech.2021.113764
134137936 147369 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced P-selectin activationAntagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced P-selectin activation
ChEMBL 368 3 0 7 3.9 COc1nn2cc(-c3cc4cc(OC(F)(F)F)ccc4n3C)nc2s1 10.1016/j.bmcl.2016.10.020
CHEMBL3933579 147369 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced P-selectin activationAntagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced P-selectin activation
ChEMBL 368 3 0 7 3.9 COc1nn2cc(-c3cc4cc(OC(F)(F)F)ccc4n3C)nc2s1 10.1016/j.bmcl.2016.10.020
117981412 133999 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Antagonist activity at PAR4 in human platelet-rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin stimulationAntagonist activity at PAR4 in human platelet-rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin stimulation
ChEMBL 575 8 0 11 5.9 COc1cc(OCc2nc(-c3ccc(C(=O)N(C)C)cc3)sc2C)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1016/j.ejmech.2020.112893
CHEMBL3717891 133999 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Antagonist activity at PAR4 in human platelet-rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin stimulationAntagonist activity at PAR4 in human platelet-rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin stimulation
ChEMBL 575 8 0 11 5.9 COc1cc(OCc2nc(-c3ccc(C(=O)N(C)C)cc3)sc2C)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1016/j.ejmech.2020.112893
134137936 147369 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced P-selectin activationAntagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced P-selectin activation
ChEMBL 368 3 0 7 3.9 COc1nn2cc(-c3cc4cc(OC(F)(F)F)ccc4n3C)nc2s1 10.1016/j.bmcl.2016.10.020
CHEMBL3933579 147369 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced P-selectin activationAntagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced P-selectin activation
ChEMBL 368 3 0 7 3.9 COc1nn2cc(-c3cc4cc(OC(F)(F)F)ccc4n3C)nc2s1 10.1016/j.bmcl.2016.10.020
134137936 147369 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 368 3 0 7 3.9 COc1nn2cc(-c3cc4cc(OC(F)(F)F)ccc4n3C)nc2s1 10.1016/j.bmcl.2016.10.020
CHEMBL3933579 147369 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 368 3 0 7 3.9 COc1nn2cc(-c3cc4cc(OC(F)(F)F)ccc4n3C)nc2s1 10.1016/j.bmcl.2016.10.020
134137936 147369 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 368 3 0 7 3.9 COc1nn2cc(-c3cc4cc(OC(F)(F)F)ccc4n3C)nc2s1 10.1016/j.bmcl.2016.10.020
CHEMBL3933579 147369 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 368 3 0 7 3.9 COc1nn2cc(-c3cc4cc(OC(F)(F)F)ccc4n3C)nc2s1 10.1016/j.bmcl.2016.10.020
118971061 175286 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity against PAR4 activating peptide domain in human platelets assessed as inhibition of alpha2bbeta3 activation level by PAC1 binding assayAntagonist activity against PAR4 activating peptide domain in human platelets assessed as inhibition of alpha2bbeta3 activation level by PAC1 binding assay
ChEMBL 479 6 1 6 5.9 CSc1ncc(-c2c(CO)n(Cc3ccccc3Cl)c3cc(OC(F)(F)F)ccc23)cn1 10.1021/acs.jmedchem.6b00928
CHEMBL4586027 175286 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity against PAR4 activating peptide domain in human platelets assessed as inhibition of alpha2bbeta3 activation level by PAC1 binding assayAntagonist activity against PAR4 activating peptide domain in human platelets assessed as inhibition of alpha2bbeta3 activation level by PAC1 binding assay
ChEMBL 479 6 1 6 5.9 CSc1ncc(-c2c(CO)n(Cc3ccccc3Cl)c3cc(OC(F)(F)F)ccc23)cn1 10.1021/acs.jmedchem.6b00928
132051307 147850 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 276 3 0 7 2.4 COc1nn2cc(-c3ccc([N+](=O)[O-])cc3)nc2s1 10.1016/j.bmcl.2016.10.020
CHEMBL3937549 147850 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 276 3 0 7 2.4 COc1nn2cc(-c3ccc([N+](=O)[O-])cc3)nc2s1 10.1016/j.bmcl.2016.10.020
164618138 184772 0 None - 0 Mouse 5.7 pIC50 = 5.7 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 500 5 1 8 5.1 Cc1cc(-c2nc3c(Cl)cc(OCCNC(=O)OC(C)(C)C)cc3s2)c2ncn(C)c(=O)c2c1 10.1016/j.ejmech.2021.113764
CHEMBL4860348 184772 0 None - 0 Mouse 5.7 pIC50 = 5.7 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 500 5 1 8 5.1 Cc1cc(-c2nc3c(Cl)cc(OCCNC(=O)OC(C)(C)C)cc3s2)c2ncn(C)c(=O)c2c1 10.1016/j.ejmech.2021.113764
132051307 147850 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 276 3 0 7 2.4 COc1nn2cc(-c3ccc([N+](=O)[O-])cc3)nc2s1 10.1016/j.bmcl.2016.10.020
CHEMBL3937549 147850 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 276 3 0 7 2.4 COc1nn2cc(-c3ccc([N+](=O)[O-])cc3)nc2s1 10.1016/j.bmcl.2016.10.020
164622683 185061 0 None - 0 Mouse 5.7 pIC50 = 5.7 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 385 2 0 6 4.5 COc1cc(Cl)c2nc(-c3cc(C)cc4c(=O)n(C)c(C)nc34)sc2c1 10.1016/j.ejmech.2021.113764
CHEMBL4864730 185061 0 None - 0 Mouse 5.7 pIC50 = 5.7 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 385 2 0 6 4.5 COc1cc(Cl)c2nc(-c3cc(C)cc4c(=O)n(C)c(C)nc34)sc2c1 10.1016/j.ejmech.2021.113764
118971061 175286 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity against PAR4 activating peptide domain in human platelets assessed as inhibition of alpha2bbeta3 activation level by PAC1 binding assayAntagonist activity against PAR4 activating peptide domain in human platelets assessed as inhibition of alpha2bbeta3 activation level by PAC1 binding assay
ChEMBL 479 6 1 6 5.9 CSc1ncc(-c2c(CO)n(Cc3ccccc3Cl)c3cc(OC(F)(F)F)ccc23)cn1 10.1021/acs.jmedchem.6b00928
CHEMBL4586027 175286 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity against PAR4 activating peptide domain in human platelets assessed as inhibition of alpha2bbeta3 activation level by PAC1 binding assayAntagonist activity against PAR4 activating peptide domain in human platelets assessed as inhibition of alpha2bbeta3 activation level by PAC1 binding assay
ChEMBL 479 6 1 6 5.9 CSc1ncc(-c2c(CO)n(Cc3ccccc3Cl)c3cc(OC(F)(F)F)ccc23)cn1 10.1021/acs.jmedchem.6b00928
118068468 134791 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Antagonist activity at PAR4 in human washed platelets assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured every 50 secs for up to 15 mins starting from 10 secs post gamma-thrombin addition in presence of recombinant hirudinAntagonist activity at PAR4 in human washed platelets assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured every 50 secs for up to 15 mins starting from 10 secs post gamma-thrombin addition in presence of recombinant hirudin
ChEMBL 331 4 0 8 3.2 COc1nn2cc(-c3cc4c(OC)ccc(OC)c4o3)nc2s1 10.1021/acs.jmedchem.9b00186
CHEMBL3727598 134791 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Antagonist activity at PAR4 in human washed platelets assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured every 50 secs for up to 15 mins starting from 10 secs post gamma-thrombin addition in presence of recombinant hirudinAntagonist activity at PAR4 in human washed platelets assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured every 50 secs for up to 15 mins starting from 10 secs post gamma-thrombin addition in presence of recombinant hirudin
ChEMBL 331 4 0 8 3.2 COc1nn2cc(-c3cc4c(OC)ccc(OC)c4o3)nc2s1 10.1021/acs.jmedchem.9b00186
118070587 135605 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Antagonist activity at PAR4 in human washed platelets assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured every 50 secs for up to 15 mins starting from 10 secs post gamma-thrombin addition in presence of recombinant hirudinAntagonist activity at PAR4 in human washed platelets assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured every 50 secs for up to 15 mins starting from 10 secs post gamma-thrombin addition in presence of recombinant hirudin
ChEMBL 285 3 0 6 3.6 CCOc1nn2cc(-c3cc4ccccc4o3)nc2s1 10.1021/acs.jmedchem.9b00186
CHEMBL3732510 135605 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Antagonist activity at PAR4 in human washed platelets assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured every 50 secs for up to 15 mins starting from 10 secs post gamma-thrombin addition in presence of recombinant hirudinAntagonist activity at PAR4 in human washed platelets assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured every 50 secs for up to 15 mins starting from 10 secs post gamma-thrombin addition in presence of recombinant hirudin
ChEMBL 285 3 0 6 3.6 CCOc1nn2cc(-c3cc4ccccc4o3)nc2s1 10.1021/acs.jmedchem.9b00186
118967085 171906 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Antagonist activity against PAR4 activating peptide domain in human platelets assessed as inhibition of alpha2bbeta3 activation level by PAC1 binding assayAntagonist activity against PAR4 activating peptide domain in human platelets assessed as inhibition of alpha2bbeta3 activation level by PAC1 binding assay
ChEMBL 506 6 1 5 5.9 COc1ccc(-c2c(CO)n(Cc3cccc(Br)c3)c3ccc(OC(F)(F)F)cc23)cn1 10.1021/acs.jmedchem.6b00928
CHEMBL4483019 171906 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Antagonist activity against PAR4 activating peptide domain in human platelets assessed as inhibition of alpha2bbeta3 activation level by PAC1 binding assayAntagonist activity against PAR4 activating peptide domain in human platelets assessed as inhibition of alpha2bbeta3 activation level by PAC1 binding assay
ChEMBL 506 6 1 5 5.9 COc1ccc(-c2c(CO)n(Cc3cccc(Br)c3)c3ccc(OC(F)(F)F)cc23)cn1 10.1021/acs.jmedchem.6b00928
118967085 171906 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Antagonist activity against PAR4 activating peptide domain in human platelets assessed as inhibition of alpha2bbeta3 activation level by PAC1 binding assayAntagonist activity against PAR4 activating peptide domain in human platelets assessed as inhibition of alpha2bbeta3 activation level by PAC1 binding assay
ChEMBL 506 6 1 5 5.9 COc1ccc(-c2c(CO)n(Cc3cccc(Br)c3)c3ccc(OC(F)(F)F)cc23)cn1 10.1021/acs.jmedchem.6b00928
CHEMBL4483019 171906 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Antagonist activity against PAR4 activating peptide domain in human platelets assessed as inhibition of alpha2bbeta3 activation level by PAC1 binding assayAntagonist activity against PAR4 activating peptide domain in human platelets assessed as inhibition of alpha2bbeta3 activation level by PAC1 binding assay
ChEMBL 506 6 1 5 5.9 COc1ccc(-c2c(CO)n(Cc3cccc(Br)c3)c3ccc(OC(F)(F)F)cc23)cn1 10.1021/acs.jmedchem.6b00928
132051314 147715 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of gamma-thrombin-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of gamma-thrombin-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 315 3 0 6 3.4 COc1nn2cc(-c3ccc(OC(F)(F)F)cc3)nc2s1 10.1016/j.bmcl.2016.10.020
CHEMBL3936444 147715 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of gamma-thrombin-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of gamma-thrombin-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 315 3 0 6 3.4 COc1nn2cc(-c3ccc(OC(F)(F)F)cc3)nc2s1 10.1016/j.bmcl.2016.10.020
164621380 185121 0 None - 0 Mouse 5.6 pIC50 = 5.6 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 341 3 0 6 3.3 COCn1cnc2c(-c3nc4c(s3)CCCC4)cc(C)cc2c1=O 10.1016/j.ejmech.2021.113764
CHEMBL4865655 185121 0 None - 0 Mouse 5.6 pIC50 = 5.6 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 341 3 0 6 3.3 COCn1cnc2c(-c3nc4c(s3)CCCC4)cc(C)cc2c1=O 10.1016/j.ejmech.2021.113764
89873480 135582 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity at PAR4 in human washed platelets assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured every 50 secs for up to 15 mins starting from 10 secs post gamma-thrombin addition in presence of recombinant hirudinAntagonist activity at PAR4 in human washed platelets assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured every 50 secs for up to 15 mins starting from 10 secs post gamma-thrombin addition in presence of recombinant hirudin
ChEMBL 301 3 0 7 3.2 COc1nn2cc(-c3cc4cccc(OC)c4o3)nc2s1 10.1021/acs.jmedchem.9b00186
CHEMBL3732386 135582 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity at PAR4 in human washed platelets assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured every 50 secs for up to 15 mins starting from 10 secs post gamma-thrombin addition in presence of recombinant hirudinAntagonist activity at PAR4 in human washed platelets assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured every 50 secs for up to 15 mins starting from 10 secs post gamma-thrombin addition in presence of recombinant hirudin
ChEMBL 301 3 0 7 3.2 COc1nn2cc(-c3cc4cccc(OC)c4o3)nc2s1 10.1021/acs.jmedchem.9b00186
89873469 147142 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity at PAR4 in human washed platelets assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured every 50 secs for up to 15 mins starting from 10 secs post gamma-thrombin addition in presence of recombinant hirudinAntagonist activity at PAR4 in human washed platelets assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured every 50 secs for up to 15 mins starting from 10 secs post gamma-thrombin addition in presence of recombinant hirudin
ChEMBL 271 2 0 6 3.2 COc1nn2cc(-c3cc4ccccc4o3)nc2s1 10.1021/acs.jmedchem.9b00186
CHEMBL3931873 147142 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity at PAR4 in human washed platelets assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured every 50 secs for up to 15 mins starting from 10 secs post gamma-thrombin addition in presence of recombinant hirudinAntagonist activity at PAR4 in human washed platelets assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured every 50 secs for up to 15 mins starting from 10 secs post gamma-thrombin addition in presence of recombinant hirudin
ChEMBL 271 2 0 6 3.2 COc1nn2cc(-c3cc4ccccc4o3)nc2s1 10.1021/acs.jmedchem.9b00186
89880954 135076 1 None - 0 Human 5.6 pIC50 = 5.6 Binding
Antagonist activity at PAR4 in human washed platelets assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured every 50 secs for up to 15 mins starting from 10 secs post gamma-thrombin addition in presence of recombinant hirudinAntagonist activity at PAR4 in human washed platelets assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured every 50 secs for up to 15 mins starting from 10 secs post gamma-thrombin addition in presence of recombinant hirudin
ChEMBL 269 2 0 5 3.8 CCc1nn2cc(-c3cc4ccccc4o3)nc2s1 10.1021/acs.jmedchem.9b00186
CHEMBL3729282 135076 1 None - 0 Human 5.6 pIC50 = 5.6 Binding
Antagonist activity at PAR4 in human washed platelets assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured every 50 secs for up to 15 mins starting from 10 secs post gamma-thrombin addition in presence of recombinant hirudinAntagonist activity at PAR4 in human washed platelets assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured every 50 secs for up to 15 mins starting from 10 secs post gamma-thrombin addition in presence of recombinant hirudin
ChEMBL 269 2 0 5 3.8 CCc1nn2cc(-c3cc4ccccc4o3)nc2s1 10.1021/acs.jmedchem.9b00186
132051314 147715 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of gamma-thrombin-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of gamma-thrombin-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 315 3 0 6 3.4 COc1nn2cc(-c3ccc(OC(F)(F)F)cc3)nc2s1 10.1016/j.bmcl.2016.10.020
CHEMBL3936444 147715 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of gamma-thrombin-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of gamma-thrombin-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 315 3 0 6 3.4 COc1nn2cc(-c3ccc(OC(F)(F)F)cc3)nc2s1 10.1016/j.bmcl.2016.10.020
10442 3846 3 None - 1 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity at PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured in presence of recombinant hirudinAntagonist activity at PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured in presence of recombinant hirudin
ChEMBL 513 9 0 9 6.4 COc1cc(OCc2cccc(c2)OCc2ccccc2)c2c(c1)oc(c2)c1cn2c(n1)sc(n2)OC 10.1021/acs.jmedchem.9b00186
71770951 3846 3 None - 1 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity at PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured in presence of recombinant hirudinAntagonist activity at PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured in presence of recombinant hirudin
ChEMBL 513 9 0 9 6.4 COc1cc(OCc2cccc(c2)OCc2ccccc2)c2c(c1)oc(c2)c1cn2c(n1)sc(n2)OC 10.1021/acs.jmedchem.9b00186
CHEMBL3728620 3846 3 None - 1 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity at PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured in presence of recombinant hirudinAntagonist activity at PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured in presence of recombinant hirudin
ChEMBL 513 9 0 9 6.4 COc1cc(OCc2cccc(c2)OCc2ccccc2)c2c(c1)oc(c2)c1cn2c(n1)sc(n2)OC 10.1021/acs.jmedchem.9b00186
155544936 172836 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Antagonist activity at PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured in presence of recombinant hirudinAntagonist activity at PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured in presence of recombinant hirudin
ChEMBL 513 9 0 9 6.4 COc1cc(OCc2ccccc2OCc2ccccc2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.9b00186
CHEMBL4528562 172836 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Antagonist activity at PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured in presence of recombinant hirudinAntagonist activity at PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured in presence of recombinant hirudin
ChEMBL 513 9 0 9 6.4 COc1cc(OCc2ccccc2OCc2ccccc2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.9b00186
132051310 152261 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of gamma-thrombin-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of gamma-thrombin-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 297 4 0 6 3.1 COc1nn2cc(-c3ccc(OC(F)F)cc3)nc2s1 10.1016/j.bmcl.2016.10.020
CHEMBL3973767 152261 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of gamma-thrombin-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of gamma-thrombin-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 297 4 0 6 3.1 COc1nn2cc(-c3ccc(OC(F)F)cc3)nc2s1 10.1016/j.bmcl.2016.10.020
164616976 184689 0 None - 0 Mouse 5.6 pIC50 = 5.6 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 540 7 1 8 4.5 Cc1cc(-c2nc3c(Cl)cc(OCCNS(=O)(=O)c4ccccc4)cc3s2)c2ncn(C)c(=O)c2c1 10.1016/j.ejmech.2021.113764
CHEMBL4859012 184689 0 None - 0 Mouse 5.6 pIC50 = 5.6 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 540 7 1 8 4.5 Cc1cc(-c2nc3c(Cl)cc(OCCNS(=O)(=O)c4ccccc4)cc3s2)c2ncn(C)c(=O)c2c1 10.1016/j.ejmech.2021.113764
132051310 152261 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of gamma-thrombin-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of gamma-thrombin-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 297 4 0 6 3.1 COc1nn2cc(-c3ccc(OC(F)F)cc3)nc2s1 10.1016/j.bmcl.2016.10.020
CHEMBL3973767 152261 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of gamma-thrombin-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of gamma-thrombin-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 297 4 0 6 3.1 COc1nn2cc(-c3ccc(OC(F)F)cc3)nc2s1 10.1016/j.bmcl.2016.10.020
132051314 147715 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced P-selectin activationAntagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced P-selectin activation
ChEMBL 315 3 0 6 3.4 COc1nn2cc(-c3ccc(OC(F)(F)F)cc3)nc2s1 10.1016/j.bmcl.2016.10.020
CHEMBL3936444 147715 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced P-selectin activationAntagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced P-selectin activation
ChEMBL 315 3 0 6 3.4 COc1nn2cc(-c3ccc(OC(F)(F)F)cc3)nc2s1 10.1016/j.bmcl.2016.10.020
132051314 147715 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 315 3 0 6 3.4 COc1nn2cc(-c3ccc(OC(F)(F)F)cc3)nc2s1 10.1016/j.bmcl.2016.10.020
CHEMBL3936444 147715 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 315 3 0 6 3.4 COc1nn2cc(-c3ccc(OC(F)(F)F)cc3)nc2s1 10.1016/j.bmcl.2016.10.020
72203403 134950 1 None - 0 Human 5.6 pIC50 = 5.6 Binding
Antagonist activity at PAR4 in human platelet-rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin stimulationAntagonist activity at PAR4 in human platelet-rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin stimulation
ChEMBL 287 2 0 6 3.9 CSc1nn2cc(-c3cc4ccccc4o3)nc2s1 10.1016/j.ejmech.2020.112893
CHEMBL3728507 134950 1 None - 0 Human 5.6 pIC50 = 5.6 Binding
Antagonist activity at PAR4 in human platelet-rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin stimulationAntagonist activity at PAR4 in human platelet-rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin stimulation
ChEMBL 287 2 0 6 3.9 CSc1nn2cc(-c3cc4ccccc4o3)nc2s1 10.1016/j.ejmech.2020.112893
164624419 184897 0 None - 0 Mouse 5.6 pIC50 = 5.6 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 297 1 0 5 2.9 Cn1cnc2c(-c3nc4c(s3)CCCC4)cccc2c1=O 10.1016/j.ejmech.2021.113764
CHEMBL4862300 184897 0 None - 0 Mouse 5.6 pIC50 = 5.6 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 297 1 0 5 2.9 Cn1cnc2c(-c3nc4c(s3)CCCC4)cccc2c1=O 10.1016/j.ejmech.2021.113764
164611833 184440 0 None - 0 Mouse 5.6 pIC50 = 5.6 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 375 1 0 5 4.8 Cc1cc(-c2nc3c(Cl)cc(Cl)cc3s2)c2ncn(C)c(=O)c2c1 10.1016/j.ejmech.2021.113764
CHEMBL4855122 184440 0 None - 0 Mouse 5.6 pIC50 = 5.6 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 375 1 0 5 4.8 Cc1cc(-c2nc3c(Cl)cc(Cl)cc3s2)c2ncn(C)c(=O)c2c1 10.1016/j.ejmech.2021.113764
132051314 147715 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 315 3 0 6 3.4 COc1nn2cc(-c3ccc(OC(F)(F)F)cc3)nc2s1 10.1016/j.bmcl.2016.10.020
CHEMBL3936444 147715 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 315 3 0 6 3.4 COc1nn2cc(-c3ccc(OC(F)(F)F)cc3)nc2s1 10.1016/j.bmcl.2016.10.020
72203403 134950 1 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity at PAR4 in human washed platelets assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured every 50 secs for up to 15 mins starting from 10 secs post gamma-thrombin addition in presence of recombinant hirudinAntagonist activity at PAR4 in human washed platelets assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured every 50 secs for up to 15 mins starting from 10 secs post gamma-thrombin addition in presence of recombinant hirudin
ChEMBL 287 2 0 6 3.9 CSc1nn2cc(-c3cc4ccccc4o3)nc2s1 10.1021/acs.jmedchem.9b00186
CHEMBL3728507 134950 1 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity at PAR4 in human washed platelets assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured every 50 secs for up to 15 mins starting from 10 secs post gamma-thrombin addition in presence of recombinant hirudinAntagonist activity at PAR4 in human washed platelets assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured every 50 secs for up to 15 mins starting from 10 secs post gamma-thrombin addition in presence of recombinant hirudin
ChEMBL 287 2 0 6 3.9 CSc1nn2cc(-c3cc4ccccc4o3)nc2s1 10.1021/acs.jmedchem.9b00186
89881055 171934 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Antagonist activity at PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured in presence of recombinant hirudinAntagonist activity at PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured in presence of recombinant hirudin
ChEMBL 423 6 1 9 4.5 COc1cc(OCc2cccc(O)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.9b00186
CHEMBL4483493 171934 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Antagonist activity at PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured in presence of recombinant hirudinAntagonist activity at PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured in presence of recombinant hirudin
ChEMBL 423 6 1 9 4.5 COc1cc(OCc2cccc(O)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.9b00186
118714146 113978 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity at PAR4 in PAR-4-AP-stimulated human platelets compound pretreated for 5 mins by fluorescent PAC1 integrin alpha2bb3 activation assayAntagonist activity at PAR4 in PAR-4-AP-stimulated human platelets compound pretreated for 5 mins by fluorescent PAC1 integrin alpha2bb3 activation assay
ChEMBL 323 6 1 4 4.3 CCCNCc1c(-c2ccccc2)c2cc([N+](=O)[O-])ccc2n1C 10.1016/j.bmcl.2014.08.021
CHEMBL3334944 113978 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity at PAR4 in PAR-4-AP-stimulated human platelets compound pretreated for 5 mins by fluorescent PAC1 integrin alpha2bb3 activation assayAntagonist activity at PAR4 in PAR-4-AP-stimulated human platelets compound pretreated for 5 mins by fluorescent PAC1 integrin alpha2bb3 activation assay
ChEMBL 323 6 1 4 4.3 CCCNCc1c(-c2ccccc2)c2cc([N+](=O)[O-])ccc2n1C 10.1016/j.bmcl.2014.08.021
132051238 144286 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 299 2 0 5 3.8 COc1nn2cc(-c3ccc(Cl)c(Cl)c3)nc2s1 10.1016/j.bmcl.2016.10.020
CHEMBL3909608 144286 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 299 2 0 5 3.8 COc1nn2cc(-c3ccc(Cl)c(Cl)c3)nc2s1 10.1016/j.bmcl.2016.10.020
132051238 144286 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 299 2 0 5 3.8 COc1nn2cc(-c3ccc(Cl)c(Cl)c3)nc2s1 10.1016/j.bmcl.2016.10.020
CHEMBL3909608 144286 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 299 2 0 5 3.8 COc1nn2cc(-c3ccc(Cl)c(Cl)c3)nc2s1 10.1016/j.bmcl.2016.10.020
132051237 153389 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced P-selectin activationAntagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced P-selectin activation
ChEMBL 265 2 0 5 3.1 COc1nn2cc(-c3ccc(Cl)cc3)nc2s1 10.1016/j.bmcl.2016.10.020
CHEMBL3983476 153389 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced P-selectin activationAntagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced P-selectin activation
ChEMBL 265 2 0 5 3.1 COc1nn2cc(-c3ccc(Cl)cc3)nc2s1 10.1016/j.bmcl.2016.10.020
164609962 183954 0 None - 0 Mouse 5.5 pIC50 = 5.5 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 296 1 0 6 2.6 Cc1cc(-c2nn3ccnc3s2)c2ccn(C)c(=O)c2c1 10.1016/j.ejmech.2021.113764
CHEMBL4848044 183954 0 None - 0 Mouse 5.5 pIC50 = 5.5 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 296 1 0 6 2.6 Cc1cc(-c2nn3ccnc3s2)c2ccn(C)c(=O)c2c1 10.1016/j.ejmech.2021.113764
164616136 184085 0 None - 0 Mouse 5.5 pIC50 = 5.5 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 400 4 1 7 3.5 Cc1cc(-c2nc3c(Cl)cc(OCCN)cc3s2)c2ncn(C)c(=O)c2c1 10.1016/j.ejmech.2021.113764
CHEMBL4849962 184085 0 None - 0 Mouse 5.5 pIC50 = 5.5 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 400 4 1 7 3.5 Cc1cc(-c2nc3c(Cl)cc(OCCN)cc3s2)c2ncn(C)c(=O)c2c1 10.1016/j.ejmech.2021.113764
72201854 135346 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Antagonist activity at PAR4 in human washed platelets assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured every 50 secs for up to 15 mins starting from 10 secs post gamma-thrombin addition in presence of recombinant hirudinAntagonist activity at PAR4 in human washed platelets assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured every 50 secs for up to 15 mins starting from 10 secs post gamma-thrombin addition in presence of recombinant hirudin
ChEMBL 377 5 0 7 4.8 COc1nn2cc(-c3cc4c(OCc5ccccc5)cccc4o3)nc2s1 10.1021/acs.jmedchem.9b00186
CHEMBL3730957 135346 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Antagonist activity at PAR4 in human washed platelets assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured every 50 secs for up to 15 mins starting from 10 secs post gamma-thrombin addition in presence of recombinant hirudinAntagonist activity at PAR4 in human washed platelets assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured every 50 secs for up to 15 mins starting from 10 secs post gamma-thrombin addition in presence of recombinant hirudin
ChEMBL 377 5 0 7 4.8 COc1nn2cc(-c3cc4c(OCc5ccccc5)cccc4o3)nc2s1 10.1021/acs.jmedchem.9b00186
164609668 184437 0 None - 0 Mouse 5.5 pIC50 = 5.5 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 313 3 1 6 3.1 COCc1nc2cc(C)cc(-c3nn4cc(C)nc4s3)c2[nH]1 10.1016/j.ejmech.2021.113764
CHEMBL4855079 184437 0 None - 0 Mouse 5.5 pIC50 = 5.5 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 313 3 1 6 3.1 COCc1nc2cc(C)cc(-c3nn4cc(C)nc4s3)c2[nH]1 10.1016/j.ejmech.2021.113764
164620157 185216 0 None - 0 Mouse 5.5 pIC50 = 5.5 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 310 1 0 6 2.9 Cc1cc(-c2nn3cc(C)nc3s2)c2ccn(C)c(=O)c2c1 10.1016/j.ejmech.2021.113764
CHEMBL4867000 185216 0 None - 0 Mouse 5.5 pIC50 = 5.5 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 310 1 0 6 2.9 Cc1cc(-c2nn3cc(C)nc3s2)c2ccn(C)c(=O)c2c1 10.1016/j.ejmech.2021.113764
71148622 113975 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Antagonist activity at PAR4 in PAR-4-AP-stimulated human platelets compound pretreated for 5 mins by fluorescent PAC1 integrin alpha2bb3 activation assayAntagonist activity at PAR4 in PAR-4-AP-stimulated human platelets compound pretreated for 5 mins by fluorescent PAC1 integrin alpha2bb3 activation assay
ChEMBL 372 6 0 4 5.5 Cn1c(COCc2ccccc2)c(-c2ccccc2)c2cc([N+](=O)[O-])ccc21 10.1016/j.bmcl.2014.08.021
CHEMBL3334941 113975 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Antagonist activity at PAR4 in PAR-4-AP-stimulated human platelets compound pretreated for 5 mins by fluorescent PAC1 integrin alpha2bb3 activation assayAntagonist activity at PAR4 in PAR-4-AP-stimulated human platelets compound pretreated for 5 mins by fluorescent PAC1 integrin alpha2bb3 activation assay
ChEMBL 372 6 0 4 5.5 Cn1c(COCc2ccccc2)c(-c2ccccc2)c2cc([N+](=O)[O-])ccc21 10.1016/j.bmcl.2014.08.021
164614403 184070 0 None - 0 Mouse 5.5 pIC50 = 5.5 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 335 2 0 5 3.3 C#CCn1cnc2c(-c3nc4c(s3)CCCC4)cc(C)cc2c1=O 10.1016/j.ejmech.2021.113764
CHEMBL4849742 184070 0 None - 0 Mouse 5.5 pIC50 = 5.5 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 335 2 0 5 3.3 C#CCn1cnc2c(-c3nc4c(s3)CCCC4)cc(C)cc2c1=O 10.1016/j.ejmech.2021.113764
134135549 143795 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 280 2 0 5 2.8 CN(C)c1nn2cc(-c3c(F)cccc3F)nc2s1 10.1016/j.bmcl.2016.10.020
CHEMBL3905565 143795 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 280 2 0 5 2.8 CN(C)c1nn2cc(-c3c(F)cccc3F)nc2s1 10.1016/j.bmcl.2016.10.020
164623754 185189 0 None - 0 Mouse 5.5 pIC50 = 5.5 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 299 3 0 6 3.7 COCc1cc2cc(C)cc(-c3nn4ccnc4s3)c2o1 10.1016/j.ejmech.2021.113764
CHEMBL4866596 185189 0 None - 0 Mouse 5.5 pIC50 = 5.5 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 299 3 0 6 3.7 COCc1cc2cc(C)cc(-c3nn4ccnc4s3)c2o1 10.1016/j.ejmech.2021.113764
132051221 143870 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of gamma-thrombin-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of gamma-thrombin-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 299 2 0 5 3.5 COc1nn2cc(-c3ccc(C(F)(F)F)cc3)nc2s1 10.1016/j.bmcl.2016.10.020
CHEMBL3906197 143870 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of gamma-thrombin-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of gamma-thrombin-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 299 2 0 5 3.5 COc1nn2cc(-c3ccc(C(F)(F)F)cc3)nc2s1 10.1016/j.bmcl.2016.10.020
132051221 143870 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of gamma-thrombin-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of gamma-thrombin-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 299 2 0 5 3.5 COc1nn2cc(-c3ccc(C(F)(F)F)cc3)nc2s1 10.1016/j.bmcl.2016.10.020
CHEMBL3906197 143870 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of gamma-thrombin-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of gamma-thrombin-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 299 2 0 5 3.5 COc1nn2cc(-c3ccc(C(F)(F)F)cc3)nc2s1 10.1016/j.bmcl.2016.10.020
118068374 169218 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Antagonist activity at PAR4 in human washed platelets assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured every 50 secs for up to 15 mins starting from 10 secs post gamma-thrombin addition in presence of recombinant hirudinAntagonist activity at PAR4 in human washed platelets assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured every 50 secs for up to 15 mins starting from 10 secs post gamma-thrombin addition in presence of recombinant hirudin
ChEMBL 301 3 0 7 3.2 COc1nn2cc(-c3cc4c(OC)cccc4o3)nc2s1 10.1021/acs.jmedchem.9b00186
CHEMBL4439280 169218 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Antagonist activity at PAR4 in human washed platelets assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured every 50 secs for up to 15 mins starting from 10 secs post gamma-thrombin addition in presence of recombinant hirudinAntagonist activity at PAR4 in human washed platelets assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured every 50 secs for up to 15 mins starting from 10 secs post gamma-thrombin addition in presence of recombinant hirudin
ChEMBL 301 3 0 7 3.2 COc1nn2cc(-c3cc4c(OC)cccc4o3)nc2s1 10.1021/acs.jmedchem.9b00186
89873480 135582 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Antagonist activity at PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured in presence of recombinant hirudinAntagonist activity at PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured in presence of recombinant hirudin
ChEMBL 301 3 0 7 3.2 COc1nn2cc(-c3cc4cccc(OC)c4o3)nc2s1 10.1021/acs.jmedchem.9b00186
CHEMBL3732386 135582 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Antagonist activity at PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured in presence of recombinant hirudinAntagonist activity at PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured in presence of recombinant hirudin
ChEMBL 301 3 0 7 3.2 COc1nn2cc(-c3cc4cccc(OC)c4o3)nc2s1 10.1021/acs.jmedchem.9b00186
132051314 147715 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of gamma-thrombin-induced P-selectin activationAntagonist activity at PAR4 in human platelets assessed as inhibition of gamma-thrombin-induced P-selectin activation
ChEMBL 315 3 0 6 3.4 COc1nn2cc(-c3ccc(OC(F)(F)F)cc3)nc2s1 10.1016/j.bmcl.2016.10.020
CHEMBL3936444 147715 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of gamma-thrombin-induced P-selectin activationAntagonist activity at PAR4 in human platelets assessed as inhibition of gamma-thrombin-induced P-selectin activation
ChEMBL 315 3 0 6 3.4 COc1nn2cc(-c3ccc(OC(F)(F)F)cc3)nc2s1 10.1016/j.bmcl.2016.10.020
164627193 185731 0 None - 0 Mouse 5.5 pIC50 = 5.5 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 325 2 0 5 3.5 CCc1cc(-c2nc3c(s2)CCCC3)c2ncn(C)c(=O)c2c1 10.1016/j.ejmech.2021.113764
CHEMBL4874764 185731 0 None - 0 Mouse 5.5 pIC50 = 5.5 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 325 2 0 5 3.5 CCc1cc(-c2nc3c(s2)CCCC3)c2ncn(C)c(=O)c2c1 10.1016/j.ejmech.2021.113764
132051219 149466 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 299 2 0 5 3.5 COc1nn2cc(-c3cccc(C(F)(F)F)c3)nc2s1 10.1016/j.bmcl.2016.10.020
CHEMBL3950308 149466 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 299 2 0 5 3.5 COc1nn2cc(-c3cccc(C(F)(F)F)c3)nc2s1 10.1016/j.bmcl.2016.10.020
132051219 149466 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 299 2 0 5 3.5 COc1nn2cc(-c3cccc(C(F)(F)F)c3)nc2s1 10.1016/j.bmcl.2016.10.020
CHEMBL3950308 149466 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 299 2 0 5 3.5 COc1nn2cc(-c3cccc(C(F)(F)F)c3)nc2s1 10.1016/j.bmcl.2016.10.020
155521862 170145 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Antagonist activity at PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured in presence of recombinant hirudinAntagonist activity at PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured in presence of recombinant hirudin
ChEMBL 421 6 0 8 5.1 COc1cc(OCc2ccccc2C)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.9b00186
CHEMBL4452111 170145 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Antagonist activity at PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured in presence of recombinant hirudinAntagonist activity at PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured in presence of recombinant hirudin
ChEMBL 421 6 0 8 5.1 COc1cc(OCc2ccccc2C)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.9b00186
164620347 185624 0 None - 0 Mouse 5.4 pIC50 = 5.4 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 257 1 0 5 2.4 Cc1cc(-c2nccs2)c2ncn(C)c(=O)c2c1 10.1016/j.ejmech.2021.113764
CHEMBL4873173 185624 0 None - 0 Mouse 5.4 pIC50 = 5.4 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 257 1 0 5 2.4 Cc1cc(-c2nccs2)c2ncn(C)c(=O)c2c1 10.1016/j.ejmech.2021.113764
164610457 183925 0 None - 0 Mouse 5.4 pIC50 = 5.4 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 318 1 0 3 4.2 Cc1cc(-c2cccc(Cl)c2Cl)c2ncn(C)c(=O)c2c1 10.1016/j.ejmech.2021.113764
CHEMBL4847606 183925 0 None - 0 Mouse 5.4 pIC50 = 5.4 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 318 1 0 3 4.2 Cc1cc(-c2cccc(Cl)c2Cl)c2ncn(C)c(=O)c2c1 10.1016/j.ejmech.2021.113764
118971050 174622 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Antagonist activity against PAR4 activating peptide domain in human platelets assessed as inhibition of alpha2bbeta3 activation level by PAC1 binding assayAntagonist activity against PAR4 activating peptide domain in human platelets assessed as inhibition of alpha2bbeta3 activation level by PAC1 binding assay
ChEMBL 422 7 1 5 5.3 CCOc1ccc2c(-c3ccc(OC)nc3)c(CO)n(Cc3ccccc3Cl)c2c1 10.1021/acs.jmedchem.6b00928
CHEMBL4571068 174622 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Antagonist activity against PAR4 activating peptide domain in human platelets assessed as inhibition of alpha2bbeta3 activation level by PAC1 binding assayAntagonist activity against PAR4 activating peptide domain in human platelets assessed as inhibition of alpha2bbeta3 activation level by PAC1 binding assay
ChEMBL 422 7 1 5 5.3 CCOc1ccc2c(-c3ccc(OC)nc3)c(CO)n(Cc3ccccc3Cl)c2c1 10.1021/acs.jmedchem.6b00928
164621537 185408 0 None - 0 Mouse 5.4 pIC50 = 5.4 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 325 2 0 5 3.7 CCn1cnc2c(-c3nc4c(s3)CCCC4)cc(C)cc2c1=O 10.1016/j.ejmech.2021.113764
CHEMBL4870259 185408 0 None - 0 Mouse 5.4 pIC50 = 5.4 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 325 2 0 5 3.7 CCn1cnc2c(-c3nc4c(s3)CCCC4)cc(C)cc2c1=O 10.1016/j.ejmech.2021.113764
118971050 174622 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Antagonist activity against PAR4 activating peptide domain in human platelets assessed as inhibition of alpha2bbeta3 activation level by PAC1 binding assayAntagonist activity against PAR4 activating peptide domain in human platelets assessed as inhibition of alpha2bbeta3 activation level by PAC1 binding assay
ChEMBL 422 7 1 5 5.3 CCOc1ccc2c(-c3ccc(OC)nc3)c(CO)n(Cc3ccccc3Cl)c2c1 10.1021/acs.jmedchem.6b00928
CHEMBL4571068 174622 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Antagonist activity against PAR4 activating peptide domain in human platelets assessed as inhibition of alpha2bbeta3 activation level by PAC1 binding assayAntagonist activity against PAR4 activating peptide domain in human platelets assessed as inhibition of alpha2bbeta3 activation level by PAC1 binding assay
ChEMBL 422 7 1 5 5.3 CCOc1ccc2c(-c3ccc(OC)nc3)c(CO)n(Cc3ccccc3Cl)c2c1 10.1021/acs.jmedchem.6b00928
126961335 533 31 None - 1 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at human PAR4Antagonist activity at human PAR4
ChEMBL 570 5 1 6 7.5 N#Cc1ccc(cc1)NC(=O)c1ccc2c(c1)nc(n2[C@H](C1CCCCC1)C)c1cc2OCOc2cc1Br 10.1021/acs.jmedchem.7b01844
9560 533 31 None - 1 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at human PAR4Antagonist activity at human PAR4
ChEMBL 570 5 1 6 7.5 N#Cc1ccc(cc1)NC(=O)c1ccc2c(c1)nc(n2[C@H](C1CCCCC1)C)c1cc2OCOc2cc1Br 10.1021/acs.jmedchem.7b01844
CHEMBL4128763 533 31 None - 1 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at human PAR4Antagonist activity at human PAR4
ChEMBL 570 5 1 6 7.5 N#Cc1ccc(cc1)NC(=O)c1ccc2c(c1)nc(n2[C@H](C1CCCCC1)C)c1cc2OCOc2cc1Br 10.1021/acs.jmedchem.7b01844
132051237 153389 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 265 2 0 5 3.1 COc1nn2cc(-c3ccc(Cl)cc3)nc2s1 10.1016/j.bmcl.2016.10.020
CHEMBL3983476 153389 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 265 2 0 5 3.1 COc1nn2cc(-c3ccc(Cl)cc3)nc2s1 10.1016/j.bmcl.2016.10.020
132051237 153389 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 265 2 0 5 3.1 COc1nn2cc(-c3ccc(Cl)cc3)nc2s1 10.1016/j.bmcl.2016.10.020
CHEMBL3983476 153389 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 265 2 0 5 3.1 COc1nn2cc(-c3ccc(Cl)cc3)nc2s1 10.1016/j.bmcl.2016.10.020
155528420 170753 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured in presence of recombinant hirudinAntagonist activity at PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured in presence of recombinant hirudin
ChEMBL 499 8 0 9 6.6 COc1cc(OCc2cccc(Oc3ccccc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.9b00186
CHEMBL4461217 170753 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured in presence of recombinant hirudinAntagonist activity at PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured in presence of recombinant hirudin
ChEMBL 499 8 0 9 6.6 COc1cc(OCc2cccc(Oc3ccccc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.9b00186
132051221 143870 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of gamma-thrombin-induced P-selectin activationAntagonist activity at PAR4 in human platelets assessed as inhibition of gamma-thrombin-induced P-selectin activation
ChEMBL 299 2 0 5 3.5 COc1nn2cc(-c3ccc(C(F)(F)F)cc3)nc2s1 10.1016/j.bmcl.2016.10.020
CHEMBL3906197 143870 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of gamma-thrombin-induced P-selectin activationAntagonist activity at PAR4 in human platelets assessed as inhibition of gamma-thrombin-induced P-selectin activation
ChEMBL 299 2 0 5 3.5 COc1nn2cc(-c3ccc(C(F)(F)F)cc3)nc2s1 10.1016/j.bmcl.2016.10.020
132051372 148957 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 249 2 0 5 2.6 COc1nn2cc(-c3ccc(F)cc3)nc2s1 10.1016/j.bmcl.2016.10.020
CHEMBL3946410 148957 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 249 2 0 5 2.6 COc1nn2cc(-c3ccc(F)cc3)nc2s1 10.1016/j.bmcl.2016.10.020
132051372 148957 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 249 2 0 5 2.6 COc1nn2cc(-c3ccc(F)cc3)nc2s1 10.1016/j.bmcl.2016.10.020
CHEMBL3946410 148957 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 249 2 0 5 2.6 COc1nn2cc(-c3ccc(F)cc3)nc2s1 10.1016/j.bmcl.2016.10.020
155529126 170829 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured in presence of recombinant hirudinAntagonist activity at PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured in presence of recombinant hirudin
ChEMBL 515 8 0 9 7.0 COc1cc(OCc2cccc(Sc3ccccc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.9b00186
CHEMBL4462511 170829 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured in presence of recombinant hirudinAntagonist activity at PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured in presence of recombinant hirudin
ChEMBL 515 8 0 9 7.0 COc1cc(OCc2cccc(Sc3ccccc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.9b00186
72201854 135346 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Antagonist activity at PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured in presence of recombinant hirudinAntagonist activity at PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured in presence of recombinant hirudin
ChEMBL 377 5 0 7 4.8 COc1nn2cc(-c3cc4c(OCc5ccccc5)cccc4o3)nc2s1 10.1021/acs.jmedchem.9b00186
CHEMBL3730957 135346 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Antagonist activity at PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured in presence of recombinant hirudinAntagonist activity at PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured in presence of recombinant hirudin
ChEMBL 377 5 0 7 4.8 COc1nn2cc(-c3cc4c(OCc5ccccc5)cccc4o3)nc2s1 10.1021/acs.jmedchem.9b00186
118971381 172345 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Antagonist activity against PAR4 activating peptide domain in human platelets assessed as inhibition of alpha2bbeta3 activation level by PAC1 binding assayAntagonist activity against PAR4 activating peptide domain in human platelets assessed as inhibition of alpha2bbeta3 activation level by PAC1 binding assay
ChEMBL 425 6 1 6 5.0 COc1ccc2c(-c3cnc(SC)nc3)c(CO)n(Cc3ccccc3Cl)c2c1 10.1021/acs.jmedchem.6b00928
CHEMBL4516569 172345 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Antagonist activity against PAR4 activating peptide domain in human platelets assessed as inhibition of alpha2bbeta3 activation level by PAC1 binding assayAntagonist activity against PAR4 activating peptide domain in human platelets assessed as inhibition of alpha2bbeta3 activation level by PAC1 binding assay
ChEMBL 425 6 1 6 5.0 COc1ccc2c(-c3cnc(SC)nc3)c(CO)n(Cc3ccccc3Cl)c2c1 10.1021/acs.jmedchem.6b00928
118971381 172345 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Antagonist activity against PAR4 activating peptide domain in human platelets assessed as inhibition of alpha2bbeta3 activation level by PAC1 binding assayAntagonist activity against PAR4 activating peptide domain in human platelets assessed as inhibition of alpha2bbeta3 activation level by PAC1 binding assay
ChEMBL 425 6 1 6 5.0 COc1ccc2c(-c3cnc(SC)nc3)c(CO)n(Cc3ccccc3Cl)c2c1 10.1021/acs.jmedchem.6b00928
CHEMBL4516569 172345 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Antagonist activity against PAR4 activating peptide domain in human platelets assessed as inhibition of alpha2bbeta3 activation level by PAC1 binding assayAntagonist activity against PAR4 activating peptide domain in human platelets assessed as inhibition of alpha2bbeta3 activation level by PAC1 binding assay
ChEMBL 425 6 1 6 5.0 COc1ccc2c(-c3cnc(SC)nc3)c(CO)n(Cc3ccccc3Cl)c2c1 10.1021/acs.jmedchem.6b00928
164627731 185901 0 None - 0 Mouse 5.4 pIC50 = 5.4 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 379 3 0 6 3.8 C#CCn1cnc2c(-c3nc4c(F)cc(OC)cc4s3)cc(C)cc2c1=O 10.1016/j.ejmech.2021.113764
CHEMBL4877231 185901 0 None - 0 Mouse 5.4 pIC50 = 5.4 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 379 3 0 6 3.8 C#CCn1cnc2c(-c3nc4c(F)cc(OC)cc4s3)cc(C)cc2c1=O 10.1016/j.ejmech.2021.113764
164609245 183797 0 None - 0 Mouse 5.4 pIC50 = 5.4 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 290 1 0 4 3.7 Cc1cc(-c2cc3ccccc3o2)c2ncn(C)c(=O)c2c1 10.1016/j.ejmech.2021.113764
CHEMBL4845780 183797 0 None - 0 Mouse 5.4 pIC50 = 5.4 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 290 1 0 4 3.7 Cc1cc(-c2cc3ccccc3o2)c2ncn(C)c(=O)c2c1 10.1016/j.ejmech.2021.113764
164627887 185719 0 None - 0 Mouse 5.4 pIC50 = 5.4 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 395 3 0 6 4.3 C#CCn1cnc2c(-c3nc4c(Cl)cc(OC)cc4s3)cc(C)cc2c1=O 10.1016/j.ejmech.2021.113764
CHEMBL4874590 185719 0 None - 0 Mouse 5.4 pIC50 = 5.4 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 395 3 0 6 4.3 C#CCn1cnc2c(-c3nc4c(Cl)cc(OC)cc4s3)cc(C)cc2c1=O 10.1016/j.ejmech.2021.113764
118967091 174048 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity against PAR4 activating peptide domain in in human platelets assessed as inhibition of P-selectin activationAntagonist activity against PAR4 activating peptide domain in in human platelets assessed as inhibition of P-selectin activation
ChEMBL 462 6 1 5 5.8 COc1ccc(-c2c(CO)n(Cc3ccccc3Cl)c3ccc(OC(F)(F)F)cc23)cn1 10.1021/acs.jmedchem.6b00928
CHEMBL4557930 174048 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity against PAR4 activating peptide domain in in human platelets assessed as inhibition of P-selectin activationAntagonist activity against PAR4 activating peptide domain in in human platelets assessed as inhibition of P-selectin activation
ChEMBL 462 6 1 5 5.8 COc1ccc(-c2c(CO)n(Cc3ccccc3Cl)c3ccc(OC(F)(F)F)cc23)cn1 10.1021/acs.jmedchem.6b00928
118953461 174414 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Antagonist activity at PAR4 TL domain in human platelets assessed as gamma-thrombin-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC based flow cytometric analysisAntagonist activity at PAR4 TL domain in human platelets assessed as gamma-thrombin-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC based flow cytometric analysis
ChEMBL 508 6 1 8 5.5 COc1nn2cc(-c3c(CO)n(Cc4ccccc4Cl)c4ccc(OC(F)(F)F)cc34)nc2s1 10.1021/acs.jmedchem.6b00928
CHEMBL4566669 174414 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Antagonist activity at PAR4 TL domain in human platelets assessed as gamma-thrombin-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC based flow cytometric analysisAntagonist activity at PAR4 TL domain in human platelets assessed as gamma-thrombin-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC based flow cytometric analysis
ChEMBL 508 6 1 8 5.5 COc1nn2cc(-c3c(CO)n(Cc4ccccc4Cl)c4ccc(OC(F)(F)F)cc34)nc2s1 10.1021/acs.jmedchem.6b00928
132051239 142463 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 265 2 0 5 3.1 COc1nn2cc(-c3ccccc3Cl)nc2s1 10.1016/j.bmcl.2016.10.020
CHEMBL3894648 142463 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 265 2 0 5 3.1 COc1nn2cc(-c3ccccc3Cl)nc2s1 10.1016/j.bmcl.2016.10.020
132051239 142463 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 265 2 0 5 3.1 COc1nn2cc(-c3ccccc3Cl)nc2s1 10.1016/j.bmcl.2016.10.020
CHEMBL3894648 142463 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 265 2 0 5 3.1 COc1nn2cc(-c3ccccc3Cl)nc2s1 10.1016/j.bmcl.2016.10.020
155543857 172637 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured in presence of recombinant hirudinAntagonist activity at PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured in presence of recombinant hirudin
ChEMBL 475 6 0 8 5.8 COc1cc(OCc2cccc(C(F)(F)F)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.9b00186
CHEMBL4523001 172637 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured in presence of recombinant hirudinAntagonist activity at PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured in presence of recombinant hirudin
ChEMBL 475 6 0 8 5.8 COc1cc(OCc2cccc(C(F)(F)F)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.9b00186
118967091 174048 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity against PAR4 activating peptide domain in human platelets assessed as inhibition of alpha2bbeta3 activation level by PAC1 binding assayAntagonist activity against PAR4 activating peptide domain in human platelets assessed as inhibition of alpha2bbeta3 activation level by PAC1 binding assay
ChEMBL 462 6 1 5 5.8 COc1ccc(-c2c(CO)n(Cc3ccccc3Cl)c3ccc(OC(F)(F)F)cc23)cn1 10.1021/acs.jmedchem.6b00928
CHEMBL4557930 174048 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity against PAR4 activating peptide domain in human platelets assessed as inhibition of alpha2bbeta3 activation level by PAC1 binding assayAntagonist activity against PAR4 activating peptide domain in human platelets assessed as inhibition of alpha2bbeta3 activation level by PAC1 binding assay
ChEMBL 462 6 1 5 5.8 COc1ccc(-c2c(CO)n(Cc3ccccc3Cl)c3ccc(OC(F)(F)F)cc23)cn1 10.1021/acs.jmedchem.6b00928
164623197 185037 0 None - 0 Mouse 5.3 pIC50 = 5.3 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 355 4 0 6 3.7 CCOCn1cnc2c(-c3nc4c(s3)CCCC4)cc(C)cc2c1=O 10.1016/j.ejmech.2021.113764
CHEMBL4864292 185037 0 None - 0 Mouse 5.3 pIC50 = 5.3 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 355 4 0 6 3.7 CCOCn1cnc2c(-c3nc4c(s3)CCCC4)cc(C)cc2c1=O 10.1016/j.ejmech.2021.113764
118967132 173484 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Antagonist activity against PAR4 activating peptide domain in human platelets assessed as inhibition of alpha2bbeta3 activation level by PAC1 binding assayAntagonist activity against PAR4 activating peptide domain in human platelets assessed as inhibition of alpha2bbeta3 activation level by PAC1 binding assay
ChEMBL 496 6 1 5 6.2 COc1ccc(-c2c(CO)n(Cc3cccc(C(F)(F)F)c3)c3ccc(OC(F)(F)F)cc23)cn1 10.1021/acs.jmedchem.6b00928
CHEMBL4544189 173484 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Antagonist activity against PAR4 activating peptide domain in human platelets assessed as inhibition of alpha2bbeta3 activation level by PAC1 binding assayAntagonist activity against PAR4 activating peptide domain in human platelets assessed as inhibition of alpha2bbeta3 activation level by PAC1 binding assay
ChEMBL 496 6 1 5 6.2 COc1ccc(-c2c(CO)n(Cc3cccc(C(F)(F)F)c3)c3ccc(OC(F)(F)F)cc23)cn1 10.1021/acs.jmedchem.6b00928
132051226 146252 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 276 3 0 7 2.4 COc1nn2cc(-c3ccccc3[N+](=O)[O-])nc2s1 10.1016/j.bmcl.2016.10.020
CHEMBL3924666 146252 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 276 3 0 7 2.4 COc1nn2cc(-c3ccccc3[N+](=O)[O-])nc2s1 10.1016/j.bmcl.2016.10.020
118068437 134939 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Antagonist activity at PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured in presence of recombinant hirudinAntagonist activity at PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured in presence of recombinant hirudin
ChEMBL 301 3 0 7 3.2 COc1ccc2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.9b00186
CHEMBL3728462 134939 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Antagonist activity at PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured in presence of recombinant hirudinAntagonist activity at PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured in presence of recombinant hirudin
ChEMBL 301 3 0 7 3.2 COc1ccc2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.9b00186
155555810 173797 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Antagonist activity at PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured in presence of recombinant hirudinAntagonist activity at PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured in presence of recombinant hirudin
ChEMBL 437 8 0 9 4.7 COc1cc(OCCOc2ccccc2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.9b00186
CHEMBL4551932 173797 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Antagonist activity at PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured in presence of recombinant hirudinAntagonist activity at PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured in presence of recombinant hirudin
ChEMBL 437 8 0 9 4.7 COc1cc(OCCOc2ccccc2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.9b00186
118967132 173484 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Antagonist activity against PAR4 activating peptide domain in human platelets assessed as inhibition of alpha2bbeta3 activation level by PAC1 binding assayAntagonist activity against PAR4 activating peptide domain in human platelets assessed as inhibition of alpha2bbeta3 activation level by PAC1 binding assay
ChEMBL 496 6 1 5 6.2 COc1ccc(-c2c(CO)n(Cc3cccc(C(F)(F)F)c3)c3ccc(OC(F)(F)F)cc23)cn1 10.1021/acs.jmedchem.6b00928
CHEMBL4544189 173484 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Antagonist activity against PAR4 activating peptide domain in human platelets assessed as inhibition of alpha2bbeta3 activation level by PAC1 binding assayAntagonist activity against PAR4 activating peptide domain in human platelets assessed as inhibition of alpha2bbeta3 activation level by PAC1 binding assay
ChEMBL 496 6 1 5 6.2 COc1ccc(-c2c(CO)n(Cc3cccc(C(F)(F)F)c3)c3ccc(OC(F)(F)F)cc23)cn1 10.1021/acs.jmedchem.6b00928
164622438 185451 0 None - 0 Mouse 5.3 pIC50 = 5.3 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 313 3 0 6 4.0 COCc1cc2cc(C)cc(-c3nn4cc(C)nc4s3)c2o1 10.1016/j.ejmech.2021.113764
CHEMBL4870778 185451 0 None - 0 Mouse 5.3 pIC50 = 5.3 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 313 3 0 6 4.0 COCc1cc2cc(C)cc(-c3nn4cc(C)nc4s3)c2o1 10.1016/j.ejmech.2021.113764
132051226 146252 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 276 3 0 7 2.4 COc1nn2cc(-c3ccccc3[N+](=O)[O-])nc2s1 10.1016/j.bmcl.2016.10.020
CHEMBL3924666 146252 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 276 3 0 7 2.4 COc1nn2cc(-c3ccccc3[N+](=O)[O-])nc2s1 10.1016/j.bmcl.2016.10.020
118971057 172849 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Antagonist activity against PAR4 activating peptide domain in human platelets assessed as inhibition of alpha2bbeta3 activation level by PAC1 binding assayAntagonist activity against PAR4 activating peptide domain in human platelets assessed as inhibition of alpha2bbeta3 activation level by PAC1 binding assay
ChEMBL 479 6 1 6 5.9 CSc1ncc(-c2c(CO)n(Cc3ccccc3Cl)c3ccc(OC(F)(F)F)cc23)cn1 10.1021/acs.jmedchem.6b00928
CHEMBL4528799 172849 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Antagonist activity against PAR4 activating peptide domain in human platelets assessed as inhibition of alpha2bbeta3 activation level by PAC1 binding assayAntagonist activity against PAR4 activating peptide domain in human platelets assessed as inhibition of alpha2bbeta3 activation level by PAC1 binding assay
ChEMBL 479 6 1 6 5.9 CSc1ncc(-c2c(CO)n(Cc3ccccc3Cl)c3ccc(OC(F)(F)F)cc23)cn1 10.1021/acs.jmedchem.6b00928
118967091 174048 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Antagonist activity against PAR4 activating peptide domain in human platelets assessed as inhibition of alpha2bbeta3 activation level by PAC1 binding assayAntagonist activity against PAR4 activating peptide domain in human platelets assessed as inhibition of alpha2bbeta3 activation level by PAC1 binding assay
ChEMBL 462 6 1 5 5.8 COc1ccc(-c2c(CO)n(Cc3ccccc3Cl)c3ccc(OC(F)(F)F)cc23)cn1 10.1021/acs.jmedchem.6b00928
CHEMBL4557930 174048 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Antagonist activity against PAR4 activating peptide domain in human platelets assessed as inhibition of alpha2bbeta3 activation level by PAC1 binding assayAntagonist activity against PAR4 activating peptide domain in human platelets assessed as inhibition of alpha2bbeta3 activation level by PAC1 binding assay
ChEMBL 462 6 1 5 5.8 COc1ccc(-c2c(CO)n(Cc3ccccc3Cl)c3ccc(OC(F)(F)F)cc23)cn1 10.1021/acs.jmedchem.6b00928
118971059 172244 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Antagonist activity against PAR4 activating peptide domain in human platelets assessed as inhibition of alpha2bbeta3 activation level by PAC1 binding assayAntagonist activity against PAR4 activating peptide domain in human platelets assessed as inhibition of alpha2bbeta3 activation level by PAC1 binding assay
ChEMBL 477 7 1 6 5.6 CCOc1ncc(-c2c(CO)n(Cc3ccccc3Cl)c3ccc(OC(F)(F)F)cc23)cn1 10.1021/acs.jmedchem.6b00928
CHEMBL4514069 172244 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Antagonist activity against PAR4 activating peptide domain in human platelets assessed as inhibition of alpha2bbeta3 activation level by PAC1 binding assayAntagonist activity against PAR4 activating peptide domain in human platelets assessed as inhibition of alpha2bbeta3 activation level by PAC1 binding assay
ChEMBL 477 7 1 6 5.6 CCOc1ncc(-c2c(CO)n(Cc3ccccc3Cl)c3ccc(OC(F)(F)F)cc23)cn1 10.1021/acs.jmedchem.6b00928
118971057 172849 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Antagonist activity against PAR4 activating peptide domain in human platelets assessed as inhibition of alpha2bbeta3 activation level by PAC1 binding assayAntagonist activity against PAR4 activating peptide domain in human platelets assessed as inhibition of alpha2bbeta3 activation level by PAC1 binding assay
ChEMBL 479 6 1 6 5.9 CSc1ncc(-c2c(CO)n(Cc3ccccc3Cl)c3ccc(OC(F)(F)F)cc23)cn1 10.1021/acs.jmedchem.6b00928
CHEMBL4528799 172849 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Antagonist activity against PAR4 activating peptide domain in human platelets assessed as inhibition of alpha2bbeta3 activation level by PAC1 binding assayAntagonist activity against PAR4 activating peptide domain in human platelets assessed as inhibition of alpha2bbeta3 activation level by PAC1 binding assay
ChEMBL 479 6 1 6 5.9 CSc1ncc(-c2c(CO)n(Cc3ccccc3Cl)c3ccc(OC(F)(F)F)cc23)cn1 10.1021/acs.jmedchem.6b00928
118971059 172244 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Antagonist activity against PAR4 activating peptide domain in human platelets assessed as inhibition of alpha2bbeta3 activation level by PAC1 binding assayAntagonist activity against PAR4 activating peptide domain in human platelets assessed as inhibition of alpha2bbeta3 activation level by PAC1 binding assay
ChEMBL 477 7 1 6 5.6 CCOc1ncc(-c2c(CO)n(Cc3ccccc3Cl)c3ccc(OC(F)(F)F)cc23)cn1 10.1021/acs.jmedchem.6b00928
CHEMBL4514069 172244 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Antagonist activity against PAR4 activating peptide domain in human platelets assessed as inhibition of alpha2bbeta3 activation level by PAC1 binding assayAntagonist activity against PAR4 activating peptide domain in human platelets assessed as inhibition of alpha2bbeta3 activation level by PAC1 binding assay
ChEMBL 477 7 1 6 5.6 CCOc1ncc(-c2c(CO)n(Cc3ccccc3Cl)c3ccc(OC(F)(F)F)cc23)cn1 10.1021/acs.jmedchem.6b00928
155565675 175031 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Antagonist activity at PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured in presence of recombinant hirudinAntagonist activity at PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured in presence of recombinant hirudin
ChEMBL 451 9 0 9 4.8 COc1cc(OCCOCc2ccccc2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.9b00186
CHEMBL4580391 175031 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Antagonist activity at PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured in presence of recombinant hirudinAntagonist activity at PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured in presence of recombinant hirudin
ChEMBL 451 9 0 9 4.8 COc1cc(OCCOCc2ccccc2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.9b00186
118967130 172275 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Antagonist activity against PAR4 activating peptide domain in human platelets assessed as inhibition of alpha2bbeta3 activation level by PAC1 binding assayAntagonist activity against PAR4 activating peptide domain in human platelets assessed as inhibition of alpha2bbeta3 activation level by PAC1 binding assay
ChEMBL 464 6 1 5 5.4 COc1ccc(-c2c(CO)n(Cc3ccc(F)cc3F)c3ccc(OC(F)(F)F)cc23)cn1 10.1021/acs.jmedchem.6b00928
CHEMBL4514977 172275 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Antagonist activity against PAR4 activating peptide domain in human platelets assessed as inhibition of alpha2bbeta3 activation level by PAC1 binding assayAntagonist activity against PAR4 activating peptide domain in human platelets assessed as inhibition of alpha2bbeta3 activation level by PAC1 binding assay
ChEMBL 464 6 1 5 5.4 COc1ccc(-c2c(CO)n(Cc3ccc(F)cc3F)c3ccc(OC(F)(F)F)cc23)cn1 10.1021/acs.jmedchem.6b00928
118967130 172275 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Antagonist activity against PAR4 activating peptide domain in human platelets assessed as inhibition of alpha2bbeta3 activation level by PAC1 binding assayAntagonist activity against PAR4 activating peptide domain in human platelets assessed as inhibition of alpha2bbeta3 activation level by PAC1 binding assay
ChEMBL 464 6 1 5 5.4 COc1ccc(-c2c(CO)n(Cc3ccc(F)cc3F)c3ccc(OC(F)(F)F)cc23)cn1 10.1021/acs.jmedchem.6b00928
CHEMBL4514977 172275 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Antagonist activity against PAR4 activating peptide domain in human platelets assessed as inhibition of alpha2bbeta3 activation level by PAC1 binding assayAntagonist activity against PAR4 activating peptide domain in human platelets assessed as inhibition of alpha2bbeta3 activation level by PAC1 binding assay
ChEMBL 464 6 1 5 5.4 COc1ccc(-c2c(CO)n(Cc3ccc(F)cc3F)c3ccc(OC(F)(F)F)cc23)cn1 10.1021/acs.jmedchem.6b00928
71148620 113977 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Antagonist activity at PAR4 in PAR-4-AP-stimulated human platelets compound pretreated for 5 mins by fluorescent PAC1 integrin alpha2bb3 activation assayAntagonist activity at PAR4 in PAR-4-AP-stimulated human platelets compound pretreated for 5 mins by fluorescent PAC1 integrin alpha2bb3 activation assay
ChEMBL 340 7 0 5 3.9 COCCOCc1c(-c2ccccc2)c2cc([N+](=O)[O-])ccc2n1C 10.1016/j.bmcl.2014.08.021
CHEMBL3334943 113977 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Antagonist activity at PAR4 in PAR-4-AP-stimulated human platelets compound pretreated for 5 mins by fluorescent PAC1 integrin alpha2bb3 activation assayAntagonist activity at PAR4 in PAR-4-AP-stimulated human platelets compound pretreated for 5 mins by fluorescent PAC1 integrin alpha2bb3 activation assay
ChEMBL 340 7 0 5 3.9 COCCOCc1c(-c2ccccc2)c2cc([N+](=O)[O-])ccc2n1C 10.1016/j.bmcl.2014.08.021
132051319 146575 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 367 2 0 5 4.5 COc1nn2cc(-c3cc(C(F)(F)F)cc(C(F)(F)F)c3)nc2s1 10.1016/j.bmcl.2016.10.020
CHEMBL3927486 146575 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 367 2 0 5 4.5 COc1nn2cc(-c3cc(C(F)(F)F)cc(C(F)(F)F)c3)nc2s1 10.1016/j.bmcl.2016.10.020
132051319 146575 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 367 2 0 5 4.5 COc1nn2cc(-c3cc(C(F)(F)F)cc(C(F)(F)F)c3)nc2s1 10.1016/j.bmcl.2016.10.020
CHEMBL3927486 146575 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 367 2 0 5 4.5 COc1nn2cc(-c3cc(C(F)(F)F)cc(C(F)(F)F)c3)nc2s1 10.1016/j.bmcl.2016.10.020
164609686 184457 0 None - 0 Mouse 6.3 pIC50 = 6.3 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 554 7 1 8 4.8 Cc1ccc(S(=O)(=O)NCCOc2cc(Cl)c3nc(-c4cc(C)cc5c(=O)n(C)cnc45)sc3c2)cc1 10.1016/j.ejmech.2021.113764
CHEMBL4855377 184457 0 None - 0 Mouse 6.3 pIC50 = 6.3 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 554 7 1 8 4.8 Cc1ccc(S(=O)(=O)NCCOc2cc(Cl)c3nc(-c4cc(C)cc5c(=O)n(C)cnc45)sc3c2)cc1 10.1016/j.ejmech.2021.113764
132051315 150040 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 249 2 0 5 2.6 COc1nn2cc(-c3ccccc3F)nc2s1 10.1016/j.bmcl.2016.10.020
CHEMBL3955095 150040 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 249 2 0 5 2.6 COc1nn2cc(-c3ccccc3F)nc2s1 10.1016/j.bmcl.2016.10.020
132051315 150040 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 249 2 0 5 2.6 COc1nn2cc(-c3ccccc3F)nc2s1 10.1016/j.bmcl.2016.10.020
CHEMBL3955095 150040 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 249 2 0 5 2.6 COc1nn2cc(-c3ccccc3F)nc2s1 10.1016/j.bmcl.2016.10.020
118068442 134987 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Antagonist activity at PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured in presence of recombinant hirudinAntagonist activity at PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured in presence of recombinant hirudin
ChEMBL 331 4 0 8 3.2 COc1cc(OC)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.9b00186
CHEMBL3728724 134987 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Antagonist activity at PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured in presence of recombinant hirudinAntagonist activity at PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured in presence of recombinant hirudin
ChEMBL 331 4 0 8 3.2 COc1cc(OC)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.9b00186
164624691 185453 0 None - 0 Mouse 5.3 pIC50 = 5.3 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 341 2 0 6 3.4 COc1cc(F)c2nc(-c3cccc4c(=O)n(C)cnc34)sc2c1 10.1016/j.ejmech.2021.113764
CHEMBL4870833 185453 0 None - 0 Mouse 5.3 pIC50 = 5.3 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 341 2 0 6 3.4 COc1cc(F)c2nc(-c3cccc4c(=O)n(C)cnc34)sc2c1 10.1016/j.ejmech.2021.113764
164612316 184394 0 None - 0 Mouse 5.3 pIC50 = 5.3 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 369 2 0 6 4.0 COc1cc(F)c2nc(-c3cc(C)cc4c(=O)n(C)c(C)nc34)sc2c1 10.1016/j.ejmech.2021.113764
CHEMBL4854301 184394 0 None - 0 Mouse 5.3 pIC50 = 5.3 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 369 2 0 6 4.0 COc1cc(F)c2nc(-c3cc(C)cc4c(=O)n(C)c(C)nc34)sc2c1 10.1016/j.ejmech.2021.113764
164610678 184295 0 None - 0 Mouse 5.3 pIC50 = 5.3 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 268 1 0 3 3.0 Cc1cc(-c2ccccc2F)c2ncn(C)c(=O)c2c1 10.1016/j.ejmech.2021.113764
CHEMBL4852886 184295 0 None - 0 Mouse 5.3 pIC50 = 5.3 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 268 1 0 3 3.0 Cc1cc(-c2ccccc2F)c2ncn(C)c(=O)c2c1 10.1016/j.ejmech.2021.113764
118068383 169750 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Antagonist activity at PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured in presence of recombinant hirudinAntagonist activity at PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured in presence of recombinant hirudin
ChEMBL 513 9 0 9 6.4 COc1cc(OCc2ccc(OCc3ccccc3)cc2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.9b00186
CHEMBL4447049 169750 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Antagonist activity at PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured in presence of recombinant hirudinAntagonist activity at PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured in presence of recombinant hirudin
ChEMBL 513 9 0 9 6.4 COc1cc(OCc2ccc(OCc3ccccc3)cc2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.9b00186
164625638 185209 0 None - 0 Mouse 5.3 pIC50 = 5.3 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 399 1 0 7 3.9 Cc1cc(-c2nc3c(Cl)cc4c(c3s2)OCCO4)c2ncn(C)c(=O)c2c1 10.1016/j.ejmech.2021.113764
CHEMBL4866947 185209 0 None - 0 Mouse 5.3 pIC50 = 5.3 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 399 1 0 7 3.9 Cc1cc(-c2nc3c(Cl)cc4c(c3s2)OCCO4)c2ncn(C)c(=O)c2c1 10.1016/j.ejmech.2021.113764
132051319 146575 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of gamma-thrombin-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of gamma-thrombin-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 367 2 0 5 4.5 COc1nn2cc(-c3cc(C(F)(F)F)cc(C(F)(F)F)c3)nc2s1 10.1016/j.bmcl.2016.10.020
CHEMBL3927486 146575 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of gamma-thrombin-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of gamma-thrombin-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 367 2 0 5 4.5 COc1nn2cc(-c3cc(C(F)(F)F)cc(C(F)(F)F)c3)nc2s1 10.1016/j.bmcl.2016.10.020
132051319 146575 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of gamma-thrombin-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of gamma-thrombin-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 367 2 0 5 4.5 COc1nn2cc(-c3cc(C(F)(F)F)cc(C(F)(F)F)c3)nc2s1 10.1016/j.bmcl.2016.10.020
CHEMBL3927486 146575 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of gamma-thrombin-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of gamma-thrombin-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 367 2 0 5 4.5 COc1nn2cc(-c3cc(C(F)(F)F)cc(C(F)(F)F)c3)nc2s1 10.1016/j.bmcl.2016.10.020
132051234 145982 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 245 2 0 5 2.8 COc1nn2cc(-c3ccc(C)cc3)nc2s1 10.1016/j.bmcl.2016.10.020
CHEMBL3922644 145982 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 245 2 0 5 2.8 COc1nn2cc(-c3ccc(C)cc3)nc2s1 10.1016/j.bmcl.2016.10.020
132051234 145982 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 245 2 0 5 2.8 COc1nn2cc(-c3ccc(C)cc3)nc2s1 10.1016/j.bmcl.2016.10.020
CHEMBL3922644 145982 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 245 2 0 5 2.8 COc1nn2cc(-c3ccc(C)cc3)nc2s1 10.1016/j.bmcl.2016.10.020
89873469 147142 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity at PAR4 (unknown origin) assessed as inhibition of gamma-thrombin-induced receptor activationAntagonist activity at PAR4 (unknown origin) assessed as inhibition of gamma-thrombin-induced receptor activation
ChEMBL 271 2 0 6 3.2 COc1nn2cc(-c3cc4ccccc4o3)nc2s1 10.1016/j.bmcl.2016.10.020
CHEMBL3931873 147142 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity at PAR4 (unknown origin) assessed as inhibition of gamma-thrombin-induced receptor activationAntagonist activity at PAR4 (unknown origin) assessed as inhibition of gamma-thrombin-induced receptor activation
ChEMBL 271 2 0 6 3.2 COc1nn2cc(-c3cc4ccccc4o3)nc2s1 10.1016/j.bmcl.2016.10.020
132051232 143564 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 261 3 0 6 2.5 COc1ccc(-c2cn3nc(OC)sc3n2)cc1 10.1016/j.bmcl.2016.10.020
CHEMBL3903596 143564 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 261 3 0 6 2.5 COc1ccc(-c2cn3nc(OC)sc3n2)cc1 10.1016/j.bmcl.2016.10.020
132051232 143564 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 261 3 0 6 2.5 COc1ccc(-c2cn3nc(OC)sc3n2)cc1 10.1016/j.bmcl.2016.10.020
CHEMBL3903596 143564 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 261 3 0 6 2.5 COc1ccc(-c2cn3nc(OC)sc3n2)cc1 10.1016/j.bmcl.2016.10.020
155530857 171012 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Antagonist activity at PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured in presence of recombinant hirudinAntagonist activity at PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured in presence of recombinant hirudin
ChEMBL 513 9 0 9 6.4 COc1cc(OCc2cccc(COc3ccccc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.9b00186
CHEMBL4465125 171012 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Antagonist activity at PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured in presence of recombinant hirudinAntagonist activity at PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured in presence of recombinant hirudin
ChEMBL 513 9 0 9 6.4 COc1cc(OCc2cccc(COc3ccccc3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.9b00186
132051237 153389 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of gamma-thrombin-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of gamma-thrombin-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 265 2 0 5 3.1 COc1nn2cc(-c3ccc(Cl)cc3)nc2s1 10.1016/j.bmcl.2016.10.020
CHEMBL3983476 153389 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of gamma-thrombin-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of gamma-thrombin-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 265 2 0 5 3.1 COc1nn2cc(-c3ccc(Cl)cc3)nc2s1 10.1016/j.bmcl.2016.10.020
132051237 153389 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of gamma-thrombin-induced P-selectin activationAntagonist activity at PAR4 in human platelets assessed as inhibition of gamma-thrombin-induced P-selectin activation
ChEMBL 265 2 0 5 3.1 COc1nn2cc(-c3ccc(Cl)cc3)nc2s1 10.1016/j.bmcl.2016.10.020
CHEMBL3983476 153389 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of gamma-thrombin-induced P-selectin activationAntagonist activity at PAR4 in human platelets assessed as inhibition of gamma-thrombin-induced P-selectin activation
ChEMBL 265 2 0 5 3.1 COc1nn2cc(-c3ccc(Cl)cc3)nc2s1 10.1016/j.bmcl.2016.10.020
132051237 153389 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of gamma-thrombin-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of gamma-thrombin-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 265 2 0 5 3.1 COc1nn2cc(-c3ccc(Cl)cc3)nc2s1 10.1016/j.bmcl.2016.10.020
CHEMBL3983476 153389 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of gamma-thrombin-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of gamma-thrombin-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 265 2 0 5 3.1 COc1nn2cc(-c3ccc(Cl)cc3)nc2s1 10.1016/j.bmcl.2016.10.020
164625471 184985 0 None - 0 Mouse 5.2 pIC50 = 5.2 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 367 5 0 5 4.8 CCCCc1cc(-c2nc3c(s2)CCCC3)c2ncn(CC)c(=O)c2c1 10.1016/j.ejmech.2021.113764
CHEMBL4863438 184985 0 None - 0 Mouse 5.2 pIC50 = 5.2 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 367 5 0 5 4.8 CCCCc1cc(-c2nc3c(s2)CCCC3)c2ncn(CC)c(=O)c2c1 10.1016/j.ejmech.2021.113764
71148612 113974 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Antagonist activity at PAR4 in PAR-4-AP-stimulated human platelets compound pretreated for 5 mins by fluorescent PAC1 integrin alpha2bb3 activation assayAntagonist activity at PAR4 in PAR-4-AP-stimulated human platelets compound pretreated for 5 mins by fluorescent PAC1 integrin alpha2bb3 activation assay
ChEMBL 324 6 0 4 4.7 CCCOCc1c(-c2ccccc2)c2cc([N+](=O)[O-])ccc2n1C 10.1016/j.bmcl.2014.08.021
CHEMBL3334940 113974 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Antagonist activity at PAR4 in PAR-4-AP-stimulated human platelets compound pretreated for 5 mins by fluorescent PAC1 integrin alpha2bb3 activation assayAntagonist activity at PAR4 in PAR-4-AP-stimulated human platelets compound pretreated for 5 mins by fluorescent PAC1 integrin alpha2bb3 activation assay
ChEMBL 324 6 0 4 4.7 CCCOCc1c(-c2ccccc2)c2cc([N+](=O)[O-])ccc2n1C 10.1016/j.bmcl.2014.08.021
164619381 185404 0 None - 0 Mouse 6.2 pIC50 = 6.2 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 415 5 0 7 4.6 CCOCn1cnc2c(-c3nc4c(Cl)cc(OC)cc4s3)cc(C)cc2c1=O 10.1016/j.ejmech.2021.113764
CHEMBL4870185 185404 0 None - 0 Mouse 6.2 pIC50 = 6.2 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 415 5 0 7 4.6 CCOCn1cnc2c(-c3nc4c(Cl)cc(OC)cc4s3)cc(C)cc2c1=O 10.1016/j.ejmech.2021.113764
118714099 113971 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity at PAR4 in PAR-4-AP-stimulated human platelets compound pretreated for 5 mins by fluorescent PAC1 integrin alpha2bb3 activation assayAntagonist activity at PAR4 in PAR-4-AP-stimulated human platelets compound pretreated for 5 mins by fluorescent PAC1 integrin alpha2bb3 activation assay
ChEMBL 355 5 0 3 5.5 CCOC(=O)c1ccc(-c2cn(Cc3ccccc3)c3ccccc23)cc1 10.1016/j.bmcl.2014.08.021
CHEMBL3334887 113971 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity at PAR4 in PAR-4-AP-stimulated human platelets compound pretreated for 5 mins by fluorescent PAC1 integrin alpha2bb3 activation assayAntagonist activity at PAR4 in PAR-4-AP-stimulated human platelets compound pretreated for 5 mins by fluorescent PAC1 integrin alpha2bb3 activation assay
ChEMBL 355 5 0 3 5.5 CCOC(=O)c1ccc(-c2cn(Cc3ccccc3)c3ccccc23)cc1 10.1016/j.bmcl.2014.08.021
118714099 113971 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity at PAR4 in human platelets after 10 mins by flow cytometric analysisAntagonist activity at PAR4 in human platelets after 10 mins by flow cytometric analysis
ChEMBL 355 5 0 3 5.5 CCOC(=O)c1ccc(-c2cn(Cc3ccccc3)c3ccccc23)cc1 10.1021/acs.jmedchem.6b00928
CHEMBL3334887 113971 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity at PAR4 in human platelets after 10 mins by flow cytometric analysisAntagonist activity at PAR4 in human platelets after 10 mins by flow cytometric analysis
ChEMBL 355 5 0 3 5.5 CCOC(=O)c1ccc(-c2cn(Cc3ccccc3)c3ccccc23)cc1 10.1021/acs.jmedchem.6b00928
164613710 184756 0 None - 0 Mouse 5.2 pIC50 = 5.2 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 383 3 0 6 4.7 COc1cc(F)c2nc(-c3cc(C)cc4c(=O)n(C(C)C)cnc34)sc2c1 10.1016/j.ejmech.2021.113764
CHEMBL4860078 184756 0 None - 0 Mouse 5.2 pIC50 = 5.2 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 383 3 0 6 4.7 COc1cc(F)c2nc(-c3cc(C)cc4c(=O)n(C(C)C)cnc34)sc2c1 10.1016/j.ejmech.2021.113764
132051309 151691 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 249 2 0 5 2.6 COc1nn2cc(-c3cccc(F)c3)nc2s1 10.1016/j.bmcl.2016.10.020
CHEMBL3968857 151691 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 249 2 0 5 2.6 COc1nn2cc(-c3cccc(F)c3)nc2s1 10.1016/j.bmcl.2016.10.020
132051309 151691 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 249 2 0 5 2.6 COc1nn2cc(-c3cccc(F)c3)nc2s1 10.1016/j.bmcl.2016.10.020
CHEMBL3968857 151691 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 249 2 0 5 2.6 COc1nn2cc(-c3cccc(F)c3)nc2s1 10.1016/j.bmcl.2016.10.020
164609894 184649 0 None - 0 Mouse 5.2 pIC50 = 5.2 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 357 2 0 6 3.9 COc1cc(Cl)c2nc(-c3cccc4c(=O)n(C)cnc34)sc2c1 10.1016/j.ejmech.2021.113764
CHEMBL4858255 184649 0 None - 0 Mouse 5.2 pIC50 = 5.2 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 357 2 0 6 3.9 COc1cc(Cl)c2nc(-c3cccc4c(=O)n(C)cnc34)sc2c1 10.1016/j.ejmech.2021.113764
132051298 143451 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 317 2 0 5 3.6 COc1nn2cc(-c3ccc(F)c(C(F)(F)F)c3)nc2s1 10.1016/j.bmcl.2016.10.020
CHEMBL3902806 143451 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 317 2 0 5 3.6 COc1nn2cc(-c3ccc(F)c(C(F)(F)F)c3)nc2s1 10.1016/j.bmcl.2016.10.020
147630030 171673 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Antagonist activity at PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured in presence of recombinant hirudinAntagonist activity at PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured in presence of recombinant hirudin
ChEMBL 441 6 0 8 5.5 COc1cc(OCc2cccc(Cl)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.9b00186
CHEMBL4474285 171673 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Antagonist activity at PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured in presence of recombinant hirudinAntagonist activity at PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured in presence of recombinant hirudin
ChEMBL 441 6 0 8 5.5 COc1cc(OCc2cccc(Cl)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.9b00186
132051298 143451 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 317 2 0 5 3.6 COc1nn2cc(-c3ccc(F)c(C(F)(F)F)c3)nc2s1 10.1016/j.bmcl.2016.10.020
CHEMBL3902806 143451 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 317 2 0 5 3.6 COc1nn2cc(-c3ccc(F)c(C(F)(F)F)c3)nc2s1 10.1016/j.bmcl.2016.10.020
10269 671 21 None - 1 Human 8.1 pIC50 = 8.1 Binding
Antagonist activity at PAR4 in human platelet-rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin stimulationAntagonist activity at PAR4 in human platelet-rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin stimulation
ChEMBL 513 7 0 12 4.4 COc1cc(OCc2nc(sc2C)N2CCOCC2)c2c(c1)oc(c2)c1cn2c(n1)sc(n2)OC 10.1016/j.ejmech.2020.112893
72190270 671 21 None - 1 Human 8.1 pIC50 = 8.1 Binding
Antagonist activity at PAR4 in human platelet-rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin stimulationAntagonist activity at PAR4 in human platelet-rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin stimulation
ChEMBL 513 7 0 12 4.4 COc1cc(OCc2nc(sc2C)N2CCOCC2)c2c(c1)oc(c2)c1cn2c(n1)sc(n2)OC 10.1016/j.ejmech.2020.112893
CHEMBL3716726 671 21 None - 1 Human 8.1 pIC50 = 8.1 Binding
Antagonist activity at PAR4 in human platelet-rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin stimulationAntagonist activity at PAR4 in human platelet-rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin stimulation
ChEMBL 513 7 0 12 4.4 COc1cc(OCc2nc(sc2C)N2CCOCC2)c2c(c1)oc(c2)c1cn2c(n1)sc(n2)OC 10.1016/j.ejmech.2020.112893
164626855 185927 0 None - 0 Mouse 5.2 pIC50 = 5.2 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 353 4 0 5 4.3 CCCCc1cc(-c2nc3c(s2)CCCC3)c2ncn(C)c(=O)c2c1 10.1016/j.ejmech.2021.113764
CHEMBL4877639 185927 0 None - 0 Mouse 5.2 pIC50 = 5.2 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 353 4 0 5 4.3 CCCCc1cc(-c2nc3c(s2)CCCC3)c2ncn(C)c(=O)c2c1 10.1016/j.ejmech.2021.113764
132051312 141933 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 265 2 0 5 3.1 COc1nn2cc(-c3cccc(Cl)c3)nc2s1 10.1016/j.bmcl.2016.10.020
CHEMBL3890362 141933 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 265 2 0 5 3.1 COc1nn2cc(-c3cccc(Cl)c3)nc2s1 10.1016/j.bmcl.2016.10.020
132051312 141933 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 265 2 0 5 3.1 COc1nn2cc(-c3cccc(Cl)c3)nc2s1 10.1016/j.bmcl.2016.10.020
CHEMBL3890362 141933 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 265 2 0 5 3.1 COc1nn2cc(-c3cccc(Cl)c3)nc2s1 10.1016/j.bmcl.2016.10.020
164627429 185823 0 None - 0 Mouse 5.1 pIC50 = 5.1 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 280 2 0 4 2.9 COc1ccccc1-c1cc(C)cc2c(=O)n(C)cnc12 10.1016/j.ejmech.2021.113764
CHEMBL4876067 185823 0 None - 0 Mouse 5.1 pIC50 = 5.1 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 280 2 0 4 2.9 COc1ccccc1-c1cc(C)cc2c(=O)n(C)cnc12 10.1016/j.ejmech.2021.113764
118068442 134987 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at PAR4 in human washed platelets assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured every 50 secs for up to 15 mins starting from 10 secs post gamma-thrombin addition in presence of recombinant hirudinAntagonist activity at PAR4 in human washed platelets assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured every 50 secs for up to 15 mins starting from 10 secs post gamma-thrombin addition in presence of recombinant hirudin
ChEMBL 331 4 0 8 3.2 COc1cc(OC)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.9b00186
CHEMBL3728724 134987 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at PAR4 in human washed platelets assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured every 50 secs for up to 15 mins starting from 10 secs post gamma-thrombin addition in presence of recombinant hirudinAntagonist activity at PAR4 in human washed platelets assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured every 50 secs for up to 15 mins starting from 10 secs post gamma-thrombin addition in presence of recombinant hirudin
ChEMBL 331 4 0 8 3.2 COc1cc(OC)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.9b00186
132051302 149059 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 231 2 0 5 2.5 COc1nn2cc(-c3ccccc3)nc2s1 10.1016/j.bmcl.2016.10.020
CHEMBL3947023 149059 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 231 2 0 5 2.5 COc1nn2cc(-c3ccccc3)nc2s1 10.1016/j.bmcl.2016.10.020
132051302 149059 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 231 2 0 5 2.5 COc1nn2cc(-c3ccccc3)nc2s1 10.1016/j.bmcl.2016.10.020
CHEMBL3947023 149059 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 231 2 0 5 2.5 COc1nn2cc(-c3ccccc3)nc2s1 10.1016/j.bmcl.2016.10.020
164609311 183883 0 None - 0 Mouse 5.1 pIC50 = 5.1 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 255 1 0 5 3.5 Cc1cn2nc(-c3cccc4ccoc34)sc2n1 10.1016/j.ejmech.2021.113764
CHEMBL4846976 183883 0 None - 0 Mouse 5.1 pIC50 = 5.1 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 255 1 0 5 3.5 Cc1cn2nc(-c3cccc4ccoc34)sc2n1 10.1016/j.ejmech.2021.113764
155525561 170530 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Antagonist activity at PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured in presence of recombinant hirudinAntagonist activity at PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured in presence of recombinant hirudin
ChEMBL 421 7 0 8 4.8 COc1cc(OCCc2ccccc2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.9b00186
CHEMBL4457819 170530 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Antagonist activity at PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured in presence of recombinant hirudinAntagonist activity at PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured in presence of recombinant hirudin
ChEMBL 421 7 0 8 4.8 COc1cc(OCCc2ccccc2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.9b00186
748659 113973 16 None - 0 Human 6.1 pIC50 = 6.1 Binding
Antagonist activity at PAR4 in PAR-4-AP-stimulated human platelets compound pretreated for 5 mins by fluorescent PAC1 integrin alpha2bb3 activation assayAntagonist activity at PAR4 in PAR-4-AP-stimulated human platelets compound pretreated for 5 mins by fluorescent PAC1 integrin alpha2bb3 activation assay
ChEMBL 296 4 0 4 3.9 COCc1c(-c2ccccc2)c2cc([N+](=O)[O-])ccc2n1C 10.1016/j.bmcl.2014.08.021
CHEMBL3334939 113973 16 None - 0 Human 6.1 pIC50 = 6.1 Binding
Antagonist activity at PAR4 in PAR-4-AP-stimulated human platelets compound pretreated for 5 mins by fluorescent PAC1 integrin alpha2bb3 activation assayAntagonist activity at PAR4 in PAR-4-AP-stimulated human platelets compound pretreated for 5 mins by fluorescent PAC1 integrin alpha2bb3 activation assay
ChEMBL 296 4 0 4 3.9 COCc1c(-c2ccccc2)c2cc([N+](=O)[O-])ccc2n1C 10.1016/j.bmcl.2014.08.021
134181023 184630 0 None - 0 Mouse 6.1 pIC50 = 6.1 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 385 4 0 6 5.0 COCc1cnc2c(-c3nc4c(Cl)cc(OC)cc4s3)cc(C)cc2n1 10.1016/j.ejmech.2021.113764
CHEMBL4857938 184630 0 None - 0 Mouse 6.1 pIC50 = 6.1 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 385 4 0 6 5.0 COCc1cnc2c(-c3nc4c(Cl)cc(OC)cc4s3)cc(C)cc2n1 10.1016/j.ejmech.2021.113764
71148609 113976 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Antagonist activity at PAR4 in PAR-4-AP-stimulated human platelets compound pretreated for 5 mins by fluorescent PAC1 integrin alpha2bb3 activation assayAntagonist activity at PAR4 in PAR-4-AP-stimulated human platelets compound pretreated for 5 mins by fluorescent PAC1 integrin alpha2bb3 activation assay
ChEMBL 295 4 1 4 3.5 CNCc1c(-c2ccccc2)c2cc([N+](=O)[O-])ccc2n1C 10.1016/j.bmcl.2014.08.021
CHEMBL3334942 113976 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Antagonist activity at PAR4 in PAR-4-AP-stimulated human platelets compound pretreated for 5 mins by fluorescent PAC1 integrin alpha2bb3 activation assayAntagonist activity at PAR4 in PAR-4-AP-stimulated human platelets compound pretreated for 5 mins by fluorescent PAC1 integrin alpha2bb3 activation assay
ChEMBL 295 4 1 4 3.5 CNCc1c(-c2ccccc2)c2cc([N+](=O)[O-])ccc2n1C 10.1016/j.bmcl.2014.08.021
10442 3846 3 None - 1 Human 8.1 pIC50 = 8.1 Binding
Antagonist activity at PAR4 in human washed platelets assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured every 50 secs for up to 15 mins starting from 10 secs post gamma-thrombin addition in presence of recombinant hirudinAntagonist activity at PAR4 in human washed platelets assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured every 50 secs for up to 15 mins starting from 10 secs post gamma-thrombin addition in presence of recombinant hirudin
ChEMBL 513 9 0 9 6.4 COc1cc(OCc2cccc(c2)OCc2ccccc2)c2c(c1)oc(c2)c1cn2c(n1)sc(n2)OC 10.1021/acs.jmedchem.9b00186
71770951 3846 3 None - 1 Human 8.1 pIC50 = 8.1 Binding
Antagonist activity at PAR4 in human washed platelets assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured every 50 secs for up to 15 mins starting from 10 secs post gamma-thrombin addition in presence of recombinant hirudinAntagonist activity at PAR4 in human washed platelets assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured every 50 secs for up to 15 mins starting from 10 secs post gamma-thrombin addition in presence of recombinant hirudin
ChEMBL 513 9 0 9 6.4 COc1cc(OCc2cccc(c2)OCc2ccccc2)c2c(c1)oc(c2)c1cn2c(n1)sc(n2)OC 10.1021/acs.jmedchem.9b00186
CHEMBL3728620 3846 3 None - 1 Human 8.1 pIC50 = 8.1 Binding
Antagonist activity at PAR4 in human washed platelets assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured every 50 secs for up to 15 mins starting from 10 secs post gamma-thrombin addition in presence of recombinant hirudinAntagonist activity at PAR4 in human washed platelets assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured every 50 secs for up to 15 mins starting from 10 secs post gamma-thrombin addition in presence of recombinant hirudin
ChEMBL 513 9 0 9 6.4 COc1cc(OCc2cccc(c2)OCc2ccccc2)c2c(c1)oc(c2)c1cn2c(n1)sc(n2)OC 10.1021/acs.jmedchem.9b00186
118971371 172366 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Antagonist activity against PAR4 activating peptide domain in human platelets assessed as inhibition of alpha2bbeta3 activation level by PAC1 binding assayAntagonist activity against PAR4 activating peptide domain in human platelets assessed as inhibition of alpha2bbeta3 activation level by PAC1 binding assay
ChEMBL 462 6 1 5 5.8 COc1ccc(-c2c(CO)n(Cc3ccccc3Cl)c3cc(OC(F)(F)F)ccc23)cn1 10.1021/acs.jmedchem.6b00928
CHEMBL4517009 172366 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Antagonist activity against PAR4 activating peptide domain in human platelets assessed as inhibition of alpha2bbeta3 activation level by PAC1 binding assayAntagonist activity against PAR4 activating peptide domain in human platelets assessed as inhibition of alpha2bbeta3 activation level by PAC1 binding assay
ChEMBL 462 6 1 5 5.8 COc1ccc(-c2c(CO)n(Cc3ccccc3Cl)c3cc(OC(F)(F)F)ccc23)cn1 10.1021/acs.jmedchem.6b00928
118971371 172366 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Antagonist activity against PAR4 activating peptide domain in human platelets assessed as inhibition of alpha2bbeta3 activation level by PAC1 binding assayAntagonist activity against PAR4 activating peptide domain in human platelets assessed as inhibition of alpha2bbeta3 activation level by PAC1 binding assay
ChEMBL 462 6 1 5 5.8 COc1ccc(-c2c(CO)n(Cc3ccccc3Cl)c3cc(OC(F)(F)F)ccc23)cn1 10.1021/acs.jmedchem.6b00928
CHEMBL4517009 172366 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Antagonist activity against PAR4 activating peptide domain in human platelets assessed as inhibition of alpha2bbeta3 activation level by PAC1 binding assayAntagonist activity against PAR4 activating peptide domain in human platelets assessed as inhibition of alpha2bbeta3 activation level by PAC1 binding assay
ChEMBL 462 6 1 5 5.8 COc1ccc(-c2c(CO)n(Cc3ccccc3Cl)c3cc(OC(F)(F)F)ccc23)cn1 10.1021/acs.jmedchem.6b00928
89880942 170493 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Antagonist activity at PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured in presence of recombinant hirudinAntagonist activity at PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured in presence of recombinant hirudin
ChEMBL 432 6 0 9 4.7 COc1cc(OCc2cccc(C#N)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.9b00186
CHEMBL4457190 170493 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Antagonist activity at PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured in presence of recombinant hirudinAntagonist activity at PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation preincubated for 5 mins followed by gamma-thrombin addition and measured in presence of recombinant hirudin
ChEMBL 432 6 0 9 4.7 COc1cc(OCc2cccc(C#N)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 10.1021/acs.jmedchem.9b00186
164614705 184615 0 None - 0 Mouse 5.1 pIC50 = 5.1 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 325 1 0 5 3.6 Cc1cc(-c2nc3c(s2)CCCC3)c2nc(C)n(C)c(=O)c2c1 10.1016/j.ejmech.2021.113764
CHEMBL4857661 184615 0 None - 0 Mouse 5.1 pIC50 = 5.1 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 325 1 0 5 3.6 Cc1cc(-c2nc3c(s2)CCCC3)c2nc(C)n(C)c(=O)c2c1 10.1016/j.ejmech.2021.113764
164622925 185432 0 None - 0 Mouse 5.1 pIC50 = 5.1 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 558 7 1 8 4.7 Cc1cc(-c2nc3c(Cl)cc(OCCNS(=O)(=O)c4ccc(F)cc4)cc3s2)c2ncn(C)c(=O)c2c1 10.1016/j.ejmech.2021.113764
CHEMBL4870598 185432 0 None - 0 Mouse 5.1 pIC50 = 5.1 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 558 7 1 8 4.7 Cc1cc(-c2nc3c(Cl)cc(OCCNS(=O)(=O)c4ccc(F)cc4)cc3s2)c2ncn(C)c(=O)c2c1 10.1016/j.ejmech.2021.113764
132051310 152261 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 297 4 0 6 3.1 COc1nn2cc(-c3ccc(OC(F)F)cc3)nc2s1 10.1016/j.bmcl.2016.10.020
CHEMBL3973767 152261 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 297 4 0 6 3.1 COc1nn2cc(-c3ccc(OC(F)F)cc3)nc2s1 10.1016/j.bmcl.2016.10.020
132051310 152261 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 297 4 0 6 3.1 COc1nn2cc(-c3ccc(OC(F)F)cc3)nc2s1 10.1016/j.bmcl.2016.10.020
CHEMBL3973767 152261 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 297 4 0 6 3.1 COc1nn2cc(-c3ccc(OC(F)F)cc3)nc2s1 10.1016/j.bmcl.2016.10.020
164623869 185463 0 None - 0 Mouse 6.1 pIC50 = 6.1 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 355 2 0 6 3.7 COc1cc(F)c2nc(-c3cc(C)cc4c(=O)n(C)cnc34)sc2c1 10.1016/j.ejmech.2021.113764
CHEMBL4871001 185463 0 None - 0 Mouse 6.1 pIC50 = 6.1 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 355 2 0 6 3.7 COc1cc(F)c2nc(-c3cc(C)cc4c(=O)n(C)cnc34)sc2c1 10.1016/j.ejmech.2021.113764
164612042 184786 0 None - 0 Mouse 7.1 pIC50 = 7.1 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 371 2 0 6 4.2 COc1cc(Cl)c2nc(-c3cc(C)cc4c(=O)n(C)cnc34)sc2c1 10.1016/j.ejmech.2021.113764
CHEMBL4860533 184786 0 None - 0 Mouse 7.1 pIC50 = 7.1 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 371 2 0 6 4.2 COc1cc(Cl)c2nc(-c3cc(C)cc4c(=O)n(C)cnc34)sc2c1 10.1016/j.ejmech.2021.113764
164628469 185766 0 None - 0 Mouse 5.1 pIC50 = 5.1 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 312 1 0 5 2.7 Cc1cc2c(c(-c3nn4cc(C)nc4s3)c1)CCN(C)C2=O 10.1016/j.ejmech.2021.113764
CHEMBL4875309 185766 0 None - 0 Mouse 5.1 pIC50 = 5.1 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 312 1 0 5 2.7 Cc1cc2c(c(-c3nn4cc(C)nc4s3)c1)CCN(C)C2=O 10.1016/j.ejmech.2021.113764
10269 671 21 None - 1 Human 8.0 pIC50 = 8.0 Binding
Antagonist activity at PAR4 in human whole blood assessed as inhibition of Ala-(L-4-F-Phe)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-induced platelet aggregation preincubated for 10 mins followed by Ala-(L-4-F-Phe)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly stimulationAntagonist activity at PAR4 in human whole blood assessed as inhibition of Ala-(L-4-F-Phe)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-induced platelet aggregation preincubated for 10 mins followed by Ala-(L-4-F-Phe)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly stimulation
ChEMBL 513 7 0 12 4.4 COc1cc(OCc2nc(sc2C)N2CCOCC2)c2c(c1)oc(c2)c1cn2c(n1)sc(n2)OC 10.1016/j.ejmech.2020.112893
72190270 671 21 None - 1 Human 8.0 pIC50 = 8.0 Binding
Antagonist activity at PAR4 in human whole blood assessed as inhibition of Ala-(L-4-F-Phe)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-induced platelet aggregation preincubated for 10 mins followed by Ala-(L-4-F-Phe)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly stimulationAntagonist activity at PAR4 in human whole blood assessed as inhibition of Ala-(L-4-F-Phe)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-induced platelet aggregation preincubated for 10 mins followed by Ala-(L-4-F-Phe)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly stimulation
ChEMBL 513 7 0 12 4.4 COc1cc(OCc2nc(sc2C)N2CCOCC2)c2c(c1)oc(c2)c1cn2c(n1)sc(n2)OC 10.1016/j.ejmech.2020.112893
CHEMBL3716726 671 21 None - 1 Human 8.0 pIC50 = 8.0 Binding
Antagonist activity at PAR4 in human whole blood assessed as inhibition of Ala-(L-4-F-Phe)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-induced platelet aggregation preincubated for 10 mins followed by Ala-(L-4-F-Phe)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly stimulationAntagonist activity at PAR4 in human whole blood assessed as inhibition of Ala-(L-4-F-Phe)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-induced platelet aggregation preincubated for 10 mins followed by Ala-(L-4-F-Phe)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly stimulation
ChEMBL 513 7 0 12 4.4 COc1cc(OCc2nc(sc2C)N2CCOCC2)c2c(c1)oc(c2)c1cn2c(n1)sc(n2)OC 10.1016/j.ejmech.2020.112893
132051243 152462 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 256 2 0 6 2.3 COc1nn2cc(-c3ccc(C#N)cc3)nc2s1 10.1016/j.bmcl.2016.10.020
CHEMBL3975497 152462 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 256 2 0 6 2.3 COc1nn2cc(-c3ccc(C#N)cc3)nc2s1 10.1016/j.bmcl.2016.10.020
132051243 152462 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 256 2 0 6 2.3 COc1nn2cc(-c3ccc(C#N)cc3)nc2s1 10.1016/j.bmcl.2016.10.020
CHEMBL3975497 152462 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 256 2 0 6 2.3 COc1nn2cc(-c3ccc(C#N)cc3)nc2s1 10.1016/j.bmcl.2016.10.020
72203403 134950 1 None - 0 Mouse 6.0 pIC50 = 6.0 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 287 2 0 6 3.9 CSc1nn2cc(-c3cc4ccccc4o3)nc2s1 10.1016/j.ejmech.2021.113764
CHEMBL3728507 134950 1 None - 0 Mouse 6.0 pIC50 = 6.0 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 287 2 0 6 3.9 CSc1nn2cc(-c3cc4ccccc4o3)nc2s1 10.1016/j.ejmech.2021.113764
118967091 174048 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Antagonist activity at PAR4 TL domain in human platelets assessed as gamma-thrombin-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC based flow cytometric analysisAntagonist activity at PAR4 TL domain in human platelets assessed as gamma-thrombin-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC based flow cytometric analysis
ChEMBL 462 6 1 5 5.8 COc1ccc(-c2c(CO)n(Cc3ccccc3Cl)c3ccc(OC(F)(F)F)cc23)cn1 10.1021/acs.jmedchem.6b00928
CHEMBL4557930 174048 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Antagonist activity at PAR4 TL domain in human platelets assessed as gamma-thrombin-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC based flow cytometric analysisAntagonist activity at PAR4 TL domain in human platelets assessed as gamma-thrombin-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC based flow cytometric analysis
ChEMBL 462 6 1 5 5.8 COc1ccc(-c2c(CO)n(Cc3ccccc3Cl)c3ccc(OC(F)(F)F)cc23)cn1 10.1021/acs.jmedchem.6b00928
164612120 184040 0 None - 0 Mouse 6.0 pIC50 = 6.0 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 608 7 1 8 5.8 Cc1cc(-c2nc3c(Cl)cc(OCCNS(=O)(=O)c4ccc(Cl)cc4Cl)cc3s2)c2ncn(C)c(=O)c2c1 10.1016/j.ejmech.2021.113764
CHEMBL4849478 184040 0 None - 0 Mouse 6.0 pIC50 = 6.0 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 608 7 1 8 5.8 Cc1cc(-c2nc3c(Cl)cc(OCCNS(=O)(=O)c4ccc(Cl)cc4Cl)cc3s2)c2ncn(C)c(=O)c2c1 10.1016/j.ejmech.2021.113764
134137936 147369 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of gamma-thrombin-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of gamma-thrombin-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 368 3 0 7 3.9 COc1nn2cc(-c3cc4cc(OC(F)(F)F)ccc4n3C)nc2s1 10.1016/j.bmcl.2016.10.020
CHEMBL3933579 147369 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Antagonist activity at PAR4 in human platelets assessed as inhibition of gamma-thrombin-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of gamma-thrombin-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
ChEMBL 368 3 0 7 3.9 COc1nn2cc(-c3cc4cc(OC(F)(F)F)ccc4n3C)nc2s1 10.1016/j.bmcl.2016.10.020
164619889 185671 0 None - 0 Mouse 5.0 pIC50 = 5.0 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 399 3 0 6 5.2 COc1cc(Cl)c2nc(-c3cc(C)cc4c(=O)n(C(C)C)cnc34)sc2c1 10.1016/j.ejmech.2021.113764
CHEMBL4873863 185671 0 None - 0 Mouse 5.0 pIC50 = 5.0 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 399 3 0 6 5.2 COc1cc(Cl)c2nc(-c3cc(C)cc4c(=O)n(C(C)C)cnc34)sc2c1 10.1016/j.ejmech.2021.113764
164619673 185214 0 None - 0 Mouse 6.0 pIC50 = 6.0 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 370 2 0 5 4.8 COc1cc(Cl)c2nc(-c3cc(C)cc4c(=O)n(C)ccc34)sc2c1 10.1016/j.ejmech.2021.113764
CHEMBL4866983 185214 0 None - 0 Mouse 6.0 pIC50 = 6.0 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 370 2 0 5 4.8 COc1cc(Cl)c2nc(-c3cc(C)cc4c(=O)n(C)ccc34)sc2c1 10.1016/j.ejmech.2021.113764
164625765 185879 0 None - 0 Mouse 5.0 pIC50 = 5 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 369 3 0 6 4.1 CCn1cnc2c(-c3nc4c(F)cc(OC)cc4s3)cc(C)cc2c1=O 10.1016/j.ejmech.2021.113764
CHEMBL4876763 185879 0 None - 0 Mouse 5.0 pIC50 = 5 Binding
Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
ChEMBL 369 3 0 6 4.1 CCn1cnc2c(-c3nc4c(F)cc(OC)cc4s3)cc(C)cc2c1=O 10.1016/j.ejmech.2021.113764
10269 671 21 None - 1 Human 10.2 pKd = 10.2 Binding
Binding affinity to PAR4 (unknown origin) assessed as association constantBinding affinity to PAR4 (unknown origin) assessed as association constant
ChEMBL 513 7 0 12 4.4 COc1cc(OCc2nc(sc2C)N2CCOCC2)c2c(c1)oc(c2)c1cn2c(n1)sc(n2)OC 10.1021/acs.jmedchem.2c00359
72190270 671 21 None - 1 Human 10.2 pKd = 10.2 Binding
Binding affinity to PAR4 (unknown origin) assessed as association constantBinding affinity to PAR4 (unknown origin) assessed as association constant
ChEMBL 513 7 0 12 4.4 COc1cc(OCc2nc(sc2C)N2CCOCC2)c2c(c1)oc(c2)c1cn2c(n1)sc(n2)OC 10.1021/acs.jmedchem.2c00359
CHEMBL3716726 671 21 None - 1 Human 10.2 pKd = 10.2 Binding
Binding affinity to PAR4 (unknown origin) assessed as association constantBinding affinity to PAR4 (unknown origin) assessed as association constant
ChEMBL 513 7 0 12 4.4 COc1cc(OCc2nc(sc2C)N2CCOCC2)c2c(c1)oc(c2)c1cn2c(n1)sc(n2)OC 10.1021/acs.jmedchem.2c00359
12038 676 7 None - 1 Human 10.1 pKd = 10.1 Binding
Binding affinity to PAR4 (unknown origin) assessed as association constantBinding affinity to PAR4 (unknown origin) assessed as association constant
ChEMBL 561 8 0 11 5.6 COc1nn2cc(nc2s1)c1cc2c(o1)cc(OC)cc2OCc1csc(n1)c1ccc(cc1)C(=O)N(C)C 10.1021/acs.jmedchem.2c00359
72188743 676 7 None - 1 Human 10.1 pKd = 10.1 Binding
Binding affinity to PAR4 (unknown origin) assessed as association constantBinding affinity to PAR4 (unknown origin) assessed as association constant
ChEMBL 561 8 0 11 5.6 COc1nn2cc(nc2s1)c1cc2c(o1)cc(OC)cc2OCc1csc(n1)c1ccc(cc1)C(=O)N(C)C 10.1021/acs.jmedchem.2c00359
CHEMBL3716552 676 7 None - 1 Human 10.1 pKd = 10.1 Binding
Binding affinity to PAR4 (unknown origin) assessed as association constantBinding affinity to PAR4 (unknown origin) assessed as association constant
ChEMBL 561 8 0 11 5.6 COc1nn2cc(nc2s1)c1cc2c(o1)cc(OC)cc2OCc1csc(n1)c1ccc(cc1)C(=O)N(C)C 10.1021/acs.jmedchem.2c00359
DB14942 676 7 None - 1 Human 10.1 pKd = 10.1 Binding
Binding affinity to PAR4 (unknown origin) assessed as association constantBinding affinity to PAR4 (unknown origin) assessed as association constant
ChEMBL 561 8 0 11 5.6 COc1nn2cc(nc2s1)c1cc2c(o1)cc(OC)cc2OCc1csc(n1)c1ccc(cc1)C(=O)N(C)C 10.1021/acs.jmedchem.2c00359
10269 671 21 None - 1 Human 10.0 pKd = 10.0 Binding
Binding affinity to PAR4 (unknown origin) assessed as saturation bindingBinding affinity to PAR4 (unknown origin) assessed as saturation binding
ChEMBL 513 7 0 12 4.4 COc1cc(OCc2nc(sc2C)N2CCOCC2)c2c(c1)oc(c2)c1cn2c(n1)sc(n2)OC 10.1021/acs.jmedchem.2c00359
72190270 671 21 None - 1 Human 10.0 pKd = 10.0 Binding
Binding affinity to PAR4 (unknown origin) assessed as saturation bindingBinding affinity to PAR4 (unknown origin) assessed as saturation binding
ChEMBL 513 7 0 12 4.4 COc1cc(OCc2nc(sc2C)N2CCOCC2)c2c(c1)oc(c2)c1cn2c(n1)sc(n2)OC 10.1021/acs.jmedchem.2c00359
CHEMBL3716726 671 21 None - 1 Human 10.0 pKd = 10.0 Binding
Binding affinity to PAR4 (unknown origin) assessed as saturation bindingBinding affinity to PAR4 (unknown origin) assessed as saturation binding
ChEMBL 513 7 0 12 4.4 COc1cc(OCc2nc(sc2C)N2CCOCC2)c2c(c1)oc(c2)c1cn2c(n1)sc(n2)OC 10.1021/acs.jmedchem.2c00359
12038 676 7 None - 1 Human 10.0 pKd = 10 Binding
Binding affinity to PAR4 (unknown origin) assessed as saturation bindingBinding affinity to PAR4 (unknown origin) assessed as saturation binding
ChEMBL 561 8 0 11 5.6 COc1nn2cc(nc2s1)c1cc2c(o1)cc(OC)cc2OCc1csc(n1)c1ccc(cc1)C(=O)N(C)C 10.1021/acs.jmedchem.2c00359
72188743 676 7 None - 1 Human 10.0 pKd = 10 Binding
Binding affinity to PAR4 (unknown origin) assessed as saturation bindingBinding affinity to PAR4 (unknown origin) assessed as saturation binding
ChEMBL 561 8 0 11 5.6 COc1nn2cc(nc2s1)c1cc2c(o1)cc(OC)cc2OCc1csc(n1)c1ccc(cc1)C(=O)N(C)C 10.1021/acs.jmedchem.2c00359
CHEMBL3716552 676 7 None - 1 Human 10.0 pKd = 10 Binding
Binding affinity to PAR4 (unknown origin) assessed as saturation bindingBinding affinity to PAR4 (unknown origin) assessed as saturation binding
ChEMBL 561 8 0 11 5.6 COc1nn2cc(nc2s1)c1cc2c(o1)cc(OC)cc2OCc1csc(n1)c1ccc(cc1)C(=O)N(C)C 10.1021/acs.jmedchem.2c00359
DB14942 676 7 None - 1 Human 10.0 pKd = 10 Binding
Binding affinity to PAR4 (unknown origin) assessed as saturation bindingBinding affinity to PAR4 (unknown origin) assessed as saturation binding
ChEMBL 561 8 0 11 5.6 COc1nn2cc(nc2s1)c1cc2c(o1)cc(OC)cc2OCc1csc(n1)c1ccc(cc1)C(=O)N(C)C 10.1021/acs.jmedchem.2c00359
10442 3846 3 None - 1 Human 8.9 pKd = 8.9 Binding
Displacement of [3H]BMS-986120 from His-tagged human PAR4 expressed in HEK293 cell membranes measured after 2 hrsDisplacement of [3H]BMS-986120 from His-tagged human PAR4 expressed in HEK293 cell membranes measured after 2 hrs
ChEMBL 513 9 0 9 6.4 COc1cc(OCc2cccc(c2)OCc2ccccc2)c2c(c1)oc(c2)c1cn2c(n1)sc(n2)OC 10.1021/acs.jmedchem.9b00186
71770951 3846 3 None - 1 Human 8.9 pKd = 8.9 Binding
Displacement of [3H]BMS-986120 from His-tagged human PAR4 expressed in HEK293 cell membranes measured after 2 hrsDisplacement of [3H]BMS-986120 from His-tagged human PAR4 expressed in HEK293 cell membranes measured after 2 hrs
ChEMBL 513 9 0 9 6.4 COc1cc(OCc2cccc(c2)OCc2ccccc2)c2c(c1)oc(c2)c1cn2c(n1)sc(n2)OC 10.1021/acs.jmedchem.9b00186
CHEMBL3728620 3846 3 None - 1 Human 8.9 pKd = 8.9 Binding
Displacement of [3H]BMS-986120 from His-tagged human PAR4 expressed in HEK293 cell membranes measured after 2 hrsDisplacement of [3H]BMS-986120 from His-tagged human PAR4 expressed in HEK293 cell membranes measured after 2 hrs
ChEMBL 513 9 0 9 6.4 COc1cc(OCc2cccc(c2)OCc2ccccc2)c2c(c1)oc(c2)c1cn2c(n1)sc(n2)OC 10.1021/acs.jmedchem.9b00186
10442 3846 3 None - 1 Human 8.5 pKd = 8.5 Binding
Displacement of [3H]BMS-986120 from His-tagged human PAR4 expressed in HEK293 cell membranesDisplacement of [3H]BMS-986120 from His-tagged human PAR4 expressed in HEK293 cell membranes
ChEMBL 513 9 0 9 6.4 COc1cc(OCc2cccc(c2)OCc2ccccc2)c2c(c1)oc(c2)c1cn2c(n1)sc(n2)OC 10.1021/acs.jmedchem.9b00186
71770951 3846 3 None - 1 Human 8.5 pKd = 8.5 Binding
Displacement of [3H]BMS-986120 from His-tagged human PAR4 expressed in HEK293 cell membranesDisplacement of [3H]BMS-986120 from His-tagged human PAR4 expressed in HEK293 cell membranes
ChEMBL 513 9 0 9 6.4 COc1cc(OCc2cccc(c2)OCc2ccccc2)c2c(c1)oc(c2)c1cn2c(n1)sc(n2)OC 10.1021/acs.jmedchem.9b00186
CHEMBL3728620 3846 3 None - 1 Human 8.5 pKd = 8.5 Binding
Displacement of [3H]BMS-986120 from His-tagged human PAR4 expressed in HEK293 cell membranesDisplacement of [3H]BMS-986120 from His-tagged human PAR4 expressed in HEK293 cell membranes
ChEMBL 513 9 0 9 6.4 COc1cc(OCc2cccc(c2)OCc2ccccc2)c2c(c1)oc(c2)c1cn2c(n1)sc(n2)OC 10.1021/acs.jmedchem.9b00186
12038 676 7 None - 1 Human 9.3 pIC50 = 9.3 Binding
Affinity determined by saturation binding assay.Affinity determined by saturation binding assay.
Guide to Pharmacology 561 8 0 11 5.6 COc1nn2cc(nc2s1)c1cc2c(o1)cc(OC)cc2OCc1csc(n1)c1ccc(cc1)C(=O)N(C)C 35729784
72188743 676 7 None - 1 Human 9.3 pIC50 = 9.3 Binding
Affinity determined by saturation binding assay.Affinity determined by saturation binding assay.
Guide to Pharmacology 561 8 0 11 5.6 COc1nn2cc(nc2s1)c1cc2c(o1)cc(OC)cc2OCc1csc(n1)c1ccc(cc1)C(=O)N(C)C 35729784
CHEMBL3716552 676 7 None - 1 Human 9.3 pIC50 = 9.3 Binding
Affinity determined by saturation binding assay.Affinity determined by saturation binding assay.
Guide to Pharmacology 561 8 0 11 5.6 COc1nn2cc(nc2s1)c1cc2c(o1)cc(OC)cc2OCc1csc(n1)c1ccc(cc1)C(=O)N(C)C 35729784
DB14942 676 7 None - 1 Human 9.3 pIC50 = 9.3 Binding
Affinity determined by saturation binding assay.Affinity determined by saturation binding assay.
Guide to Pharmacology 561 8 0 11 5.6 COc1nn2cc(nc2s1)c1cc2c(o1)cc(OC)cc2OCc1csc(n1)c1ccc(cc1)C(=O)N(C)C 35729784