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 133301 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 133301 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 134105 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 134105 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 133584 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 133584 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 133527 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 133527 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 133795 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 133795 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 133410 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 133410 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 133770 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 133770 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 133821 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 133821 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 133991 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 133991 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 134280 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 134280 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 133496 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 133496 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 133936 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 133936 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 134235 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 134235 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 134262 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 134262 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 133961 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 133961 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 133288 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 133288 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 133474 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 133474 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 133191 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 133191 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 134023 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 134023 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 133127 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 133127 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 133413 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 133413 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 134292 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 134292 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 133411 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 133411 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 133504 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 133504 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 133870 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 133870 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 134025 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 134025 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 134121 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 134121 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 133420 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 133420 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 133643 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 133643 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 133669 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 133669 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 133722 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 133722 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 134241 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 134241 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 133154 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 133154 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 133322 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 133322 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 134259 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 134259 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 133650 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 133650 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 133549 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 133549 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 133748 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 133748 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 134357 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 134357 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 134424 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 134424 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 133425 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 133425 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 133497 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 133497 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 133681 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 133681 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 133878 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 133878 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 134376 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 134376 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 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 482 9 0 10 5.6 COc1cc(OCc2csc(CCC3CC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3715066 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 482 9 0 10 5.6 COc1cc(OCc2csc(CCC3CC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
89879356 133523 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 133523 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 134202 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 134202 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 133210 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 133210 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 133704 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 133704 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 134084 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 134084 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 133492 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 133492 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 133574 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 133574 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 134401 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 134401 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 133341 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 133341 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 133431 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 133431 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 133811 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 133811 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 134242 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 134242 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 134250 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 134250 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 672 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 672 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 672 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 133430 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 133430 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 133803 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 133803 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 134033 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 134033 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 134056 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 134056 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 133887 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 133887 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 134368 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 134368 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 677 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 677 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 677 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 677 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 133278 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 133278 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 133290 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 133290 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 133940 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 133940 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 134032 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 134032 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 133302 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 133302 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 133686 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 133686 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 134178 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 134178 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 133222 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 133222 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 133307 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 133307 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 133478 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 133478 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 133519 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 133519 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 133136 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 133136 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 133152 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 133152 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 133440 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 133440 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 133454 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 133454 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 134313 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 134313 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 134458 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 134458 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 133445 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 133445 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 133483 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 133483 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 134143 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 134143 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 133874 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 133874 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 133937 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 133937 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 134423 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 134423 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 133187 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 133187 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 133522 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 133522 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 133655 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 133655 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 133400 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 133400 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 133505 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 133505 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 133118 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 133118 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 133968 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 133968 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 133188 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 133188 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 133627 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 133627 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 134305 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 134305 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 133856 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 133856 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 134359 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 134359 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 133283 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 133283 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 133464 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 133464 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 134037 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 134037 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 134303 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 134303 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 134406 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 134406 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 133792 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 133792 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 134187 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 134187 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 133345 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 133345 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 134115 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 134115 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 134156 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 134156 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 134320 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 134320 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 133123 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 133123 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 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 515 7 0 11 5.8 COc1cc(OCc2csc(-c3cccc(C#N)c3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3715590 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 515 7 0 11 5.8 COc1cc(OCc2csc(-c3cccc(C#N)c3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
89878694 133412 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 133412 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 133908 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 133908 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 133184 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 133184 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 133459 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 133459 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 133476 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 133476 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 134363 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 134363 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 134258 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 134258 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 134261 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 134261 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 133249 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 133249 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 133304 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 133304 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 134100 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 134100 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 134265 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 134265 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 133978 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 133978 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 134077 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 134077 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 134233 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 134233 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 133645 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 133645 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 133793 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 133793 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 133907 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 133907 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 134410 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 134410 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 133143 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 133143 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 133373 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 133373 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 133394 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 133394 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 133799 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 133799 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 133916 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 133916 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 133954 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 133954 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 134161 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 134161 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 133183 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 133183 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 133768 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 133768 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 133273 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 133273 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 134012 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 134012 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 134234 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 134234 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 134430 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 134430 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 133862 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 133862 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 134414 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 134414 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 134061 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 134061 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 134408 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 134408 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 133119 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 133119 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 133147 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 133147 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 133368 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 133368 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 133207 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 133207 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 134016 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 134016 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 133242 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 133242 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 133401 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 133401 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 133882 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 133882 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 134136 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 134136 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 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 512 7 0 11 5.5 COc1cc(OCc2nc(C3CCOCC3)sc2C)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3718272 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 512 7 0 11 5.5 COc1cc(OCc2nc(C3CCOCC3)sc2C)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72190587 133785 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 133785 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 134189 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 134189 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 133311 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 133311 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 133854 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 133854 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 133981 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 133981 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 133742 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 133742 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 133865 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 133865 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 134104 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 134104 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 134294 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 134294 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 133559 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 133559 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 133550 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 133550 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 134422 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 134422 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 133697 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 133697 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 134003 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 134003 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 134511 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 134511 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 134511 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 133383 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 133383 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 133614 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 133614 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 133653 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 133653 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 134254 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 134254 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 133581 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 133581 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 134420 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 134420 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 133230 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 133230 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 133875 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 133875 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 134394 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 134394 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 133297 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 133297 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 133651 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 133651 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 133766 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 133766 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 134010 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 134010 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 134364 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 134364 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 133251 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 133251 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 133257 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 133257 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 133380 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 133380 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 133621 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 133621 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 133698 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 133698 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 133775 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 133775 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 133860 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 133860 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 134018 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 134018 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 134153 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 134153 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 134417 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 134417 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 134443 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 134443 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 133227 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 133227 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 133305 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 133305 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 133392 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 133392 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 133631 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 133631 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 133677 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 133677 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 133764 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 133764 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 133828 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 133828 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 133866 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 133866 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 133983 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 133983 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 133993 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 133993 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 134310 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 134310 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 134325 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 134325 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 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 498 7 0 11 5.2 COc1cc(OCc2csc(C3CCOCC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3719069 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 498 7 0 11 5.2 COc1cc(OCc2csc(C3CCOCC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72189342 133126 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 133126 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 133219 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 133219 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 133356 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 133356 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 133409 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 133409 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 133441 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 133441 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 133500 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 133500 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 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 544 7 0 11 6.1 COc1cc(OCc2csc(C3=CCOc4ccccc43)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3716498 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 544 7 0 11 6.1 COc1cc(OCc2csc(C3=CCOc4ccccc43)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72190895 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 527 9 0 12 4.9 COC[C@@H]1CCCN1c1nc(COc2cc(OC)cc3oc(-c4cn5nc(OC)sc5n4)cc23)cs1 nan
CHEMBL3716539 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 527 9 0 12 4.9 COC[C@@H]1CCCN1c1nc(COc2cc(OC)cc3oc(-c4cn5nc(OC)sc5n4)cc23)cs1 nan
89878650 133665 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 133665 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 133895 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 133895 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 134107 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 134107 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 134197 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 134197 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 134287 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 134287 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 134382 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 134382 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 133382 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 133382 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 133988 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 133988 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 134278 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 134278 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 134400 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 134400 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 133921 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 133921 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 133324 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 133324 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 133485 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 133485 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 133729 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 133729 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 133810 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 133810 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 133847 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 133847 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 133169 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 133169 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 133265 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 133265 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 133330 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 133330 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 133683 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 133683 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 134151 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 134151 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 133318 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 133318 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 133348 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 133348 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 133915 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 133915 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 133108 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 133108 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 133362 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 133362 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 133867 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 133867 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 133516 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 133516 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 134148 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 134148 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 133506 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 133506 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 133613 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 133613 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 134114 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 134114 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 134031 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 134031 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 133535 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 133535 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 134317 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 134317 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 134071 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 134071 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 133313 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 133313 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 133812 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 133812 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 133711 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 133711 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 133336 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 133336 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 133813 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 133813 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 134183 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 134183 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 134338 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 134338 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 133909 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 133909 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 133942 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 133942 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 134058 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 134058 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 133115 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 133115 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 133367 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 133367 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 134082 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 134082 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 134271 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 134271 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 133534 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 133534 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 133610 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 133610 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 133904 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 133904 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 134327 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 134327 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 133558 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 133558 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 134021 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 134021 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 133163 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 133163 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 133762 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 133762 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 133363 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 133363 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 133381 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 133381 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 133588 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 133588 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 133842 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 133842 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 133846 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 133846 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 134370 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 134370 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 134388 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 134388 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 133190 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 133190 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 133266 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 133266 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 133659 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 133659 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 134397 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 134397 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 134044 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 134044 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 134429 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 134429 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 133938 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 133938 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 133261 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 133261 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 134352 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 134352 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 133905 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 133905 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 133562 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 133562 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 133510 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 133510 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 133617 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 133617 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 133151 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 133151 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 134147 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 134147 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 133468 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 133468 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 133276 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 133276 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 133372 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 133372 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 134461 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 134461 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 133466 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 133466 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 133999 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 133999 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 133814 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 133814 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 133159 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 133159 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 133527 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 133527 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 133178 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 133178 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 133721 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 133721 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 133837 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 133837 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 133411 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 133411 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 133821 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 133821 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 134023 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 134023 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 134241 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 134241 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 134155 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 134155 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 135548 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 135548 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 133877 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 133877 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 133168 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 133168 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 133903 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 133903 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 134371 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 134371 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 134314 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 134314 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 134324 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 134324 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 672 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 672 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 672 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 677 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 677 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 677 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 677 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 133410 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 133410 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 134056 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 134056 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 190617 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 190617 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 191697 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 191697 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 133632 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 133632 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 133623 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 133623 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 134012 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 134012 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 134212 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 134212 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 134383 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 134383 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 133377 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 133377 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 134341 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 134341 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 133377 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 133377 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 133478 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 133478 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 134143 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 134143 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 134212 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 134212 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 134383 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 134383 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 133576 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 133576 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 184796 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 184796 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 133339 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 133339 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 133405 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 133405 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 672 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 672 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 672 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 133453 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 133453 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 133718 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 133718 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 135273 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 135273 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 133648 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 133648 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 133123 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 133123 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 133345 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 133345 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 133412 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 133412 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 133476 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 133476 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 133648 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 133648 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 134156 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 134156 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 134406 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 134406 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 189776 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 189776 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 190264 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 190264 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 133790 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 133790 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 134246 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 134246 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 133597 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 133597 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 133929 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 133929 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 134027 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 134027 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 133907 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 133907 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 133929 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 133929 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 189403 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 189403 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 672 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 672 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 672 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 133560 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 133560 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 133599 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 133599 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 133820 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 133820 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 135044 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 135044 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 134798 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 134798 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 133696 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 133696 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 133960 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 133960 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 135377 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 135377 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 133374 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 133374 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 133207 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 133207 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 133311 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 133311 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 133769 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 133769 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 189575 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 189575 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 173807 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 173807 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 133578 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 133578 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 134361 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 134361 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 134930 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 134930 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 135380 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 135380 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 170839 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 170839 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 134427 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 134427 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 134427 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 134427 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 133273 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 133273 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 134330 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 134330 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 133968 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 133968 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 170503 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 170503 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 135000 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 135000 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 135000 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 135000 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 134424 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 134424 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 134419 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 134419 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 181542 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 181542 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 133171 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 133171 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 133608 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 133608 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 133176 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 133176 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 133396 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 133396 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 134445 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 134445 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 133998 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 133998 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 134448 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 134448 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 134997 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 134997 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 133557 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 133557 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 133251 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 133251 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 134445 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 134445 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 191636 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 191636 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 170540 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 170540 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 133765 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 133765 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 135473 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 135473 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 135244 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 135244 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 135576 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 135576 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 134096 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 134096 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 133483 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 133483 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 134952 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 134952 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 170763 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 170763 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 184498 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 184498 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 133285 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 133285 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 133565 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 133565 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 134952 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 134952 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 135344 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 135344 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 135750 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 135750 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 135749 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 135749 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 133463 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 133463 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 135146 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 135146 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 134009 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 134009 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 134107 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 134107 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 134369 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 134369 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 169761 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 169761 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 133215 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 133215 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 135314 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 135314 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 134356 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 134356 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 133667 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 133667 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 135385 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 135385 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 133321 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 133321 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 133378 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 133378 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 133831 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 133831 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 135590 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 135590 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 134238 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 134238 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 133831 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 133831 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 133921 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 133921 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 133825 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 133825 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 134434 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 134434 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 133416 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 133416 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 133311 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 133311 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 134025 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 134025 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 135558 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 135558 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 170155 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 170155 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 173304 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 173304 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 134450 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 134450 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 135085 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 135085 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 135446 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 135446 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 133486 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 133486 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 134874 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 134874 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 133837 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 133837 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 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 541 9 0 9 7.0 COc1cc(OCc2cccc(OCc3cc(C)cc(C)c3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3731383 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 541 9 0 9 7.0 COc1cc(OCc2cccc(OCc3cc(C)cc(C)c3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118068392 135495 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 135495 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 133385 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 133385 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 190580 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 190580 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 133918 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 133918 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 135247 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 135247 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 133960 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 133960 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 133348 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 133348 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 175041 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 175041 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 135207 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 135207 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 133769 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 133769 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 133688 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 133688 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 133504 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 133504 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 133722 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 133722 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 134010 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 134010 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 134156 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 134156 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 135126 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 135126 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 135666 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 135666 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 135003 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 135003 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 135158 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 135158 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 135515 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 135515 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 135277 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 135277 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 135531 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 135531 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 135116 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 135116 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 134804 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 134804 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 134941 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 134941 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 135606 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 135606 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 135223 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 135223 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 134884 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 134884 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 135407 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 135407 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 135376 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 135376 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 133560 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 133560 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 135385 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 135385 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 135455 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 135455 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 135610 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 135610 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 185414 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 185414 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 135692 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 135692 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 134874 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 134874 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 135523 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 135523 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 134804 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 134804 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 134963 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 134963 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 170318 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 170318 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 135010 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 135010 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 135682 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 135682 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 135305 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 135305 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 135660 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 135660 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 135100 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 135100 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 134854 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 134854 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 134960 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 134960 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 135224 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 135224 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 135628 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 135628 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 135179 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 135179 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 135420 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 135420 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 135174 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 135174 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 179557 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 179557 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 135537 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 135537 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 135029 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 135029 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 135470 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 135470 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 134793 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 134793 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 135662 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 135662 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 135393 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 135393 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 135103 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 135103 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 134929 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 134929 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 135013 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 135013 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 135683 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 135683 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 134284 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 134284 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 135340 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 135340 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 135695 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 135695 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 134943 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 134943 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 133498 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 133498 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 135544 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 135544 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 135248 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 135248 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 135181 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 135181 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 134963 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 134963 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 135700 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 135700 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 135039 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 135039 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 135697 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 135697 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 135226 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 135226 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 134901 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 134901 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 135622 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 135622 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 135106 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 135106 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 134963 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 134963 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 135333 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 135333 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 135215 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 135215 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 135624 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 135624 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 135495 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 135495 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 135123 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 135123 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 134896 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 134896 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 135102 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 135102 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 135613 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 135613 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 135026 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 135026 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 135716 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 135716 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 134977 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 134977 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 135219 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 135219 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 134870 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 134870 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 135652 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 135652 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 135162 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 135162 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 134162 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 134162 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 134953 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 134953 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 135488 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 135488 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 135735 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 135735 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 135319 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 135319 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 134844 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 134844 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 135168 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 135168 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 135369 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 135369 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 135527 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 135527 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 135364 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 135364 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 135339 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 135339 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 135490 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 135490 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 135167 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 135167 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 184739 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 184739 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 135050 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 135050 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 134792 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 134792 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 134872 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 134872 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 135519 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 135519 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 135635 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 135635 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 135635 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 135635 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 134949 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 134949 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 134859 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 134859 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 135031 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 135031 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 169659 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 169659 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 135267 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 135267 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 135136 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 135136 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 135009 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 135009 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 135160 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 135160 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 135266 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 135266 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 184796 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 184796 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 135355 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 135355 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 135368 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 135368 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 168973 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 168973 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 135564 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 135564 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 135316 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 135316 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 133184 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 133184 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 134364 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 134364 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 134422 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 134422 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 135482 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 135482 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 133461 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 133461 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 133238 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 133238 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 135406 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 135406 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 677 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 677 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 677 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 677 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 134178 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 134178 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 135454 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 135454 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 135189 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 135189 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 133944 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 133944 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 135282 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 135282 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 133133 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 133133 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 133579 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 133579 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 133154 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 133154 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 133556 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 133556 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 135426 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 135426 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 135599 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 135599 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 135277 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 135277 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 135325 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 135325 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 135111 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 135111 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 135220 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 135220 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 135505 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 135505 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 173207 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 173207 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 134326 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 134326 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 3858 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 3858 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 3858 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 133813 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 133813 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 3858 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 3858 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 3858 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 169394 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 169394 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 179076 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 179076 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 3858 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 3858 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 3858 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 133788 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 133788 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 134837 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 134837 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 135394 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 135394 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 135748 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 135748 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 134866 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 134866 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 135672 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 135672 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 134988 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 134988 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 134912 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 134912 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 190947 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 190947 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 135595 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 135595 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 135706 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 135706 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 134212 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 134212 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 133903 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 133903 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 135177 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 135177 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 135395 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 135395 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 135000 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 135000 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 134894 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 134894 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 135747 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 135747 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 134077 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 134077 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 135012 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 135012 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 135582 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 135582 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 135569 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 135569 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 135362 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 135362 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 134922 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 134922 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 135190 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 135190 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 135186 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 135186 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 135035 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 135035 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 135242 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 135242 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 133666 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 133666 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 135646 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 135646 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 135612 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 135612 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 135394 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 135394 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 135371 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 135371 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 135513 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 135513 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 135288 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 135288 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 135513 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 135513 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 134111 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 134111 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 134836 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 134836 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 135722 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 135722 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 134996 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 134996 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 133527 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 133527 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 133677 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 133677 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 133828 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 133828 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 135674 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 135674 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 135623 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 135623 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 134442 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 134442 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 134934 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 134934 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 135193 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 135193 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 133983 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 133983 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 135457 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 135457 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 133367 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 133367 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 135032 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 135032 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 133169 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 133169 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 135297 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 135297 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 133363 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 133363 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 135269 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 135269 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 133127 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 133127 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 133519 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 133519 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 135359 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 135359 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 135654 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 135654 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 134923 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 134923 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 135359 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 135359 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 133637 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 133637 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 3858 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 3858 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 3858 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 134904 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 134904 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 134073 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 134073 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 135669 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 135669 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 133643 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 133643 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 133651 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 133651 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 135001 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 135001 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 135528 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 135528 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 134987 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 134987 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 135367 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 135367 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 135594 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 135594 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 133574 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 133574 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 134189 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 134189 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 135489 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 135489 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 135489 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 135489 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 135156 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 135156 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 134044 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 134044 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 135711 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 135711 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 133635 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 133635 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 135452 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 135452 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 134032 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 134032 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 134262 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 134262 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 134410 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 134410 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 172881 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 172881 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 135320 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 135320 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 135040 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 135040 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 135680 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 135680 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 133381 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 133381 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 135642 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 135642 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 135500 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 135500 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 134791 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 134791 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 133718 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 133718 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 133362 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 133362 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 134233 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 134233 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 134241 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 134241 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 134808 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 134808 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 134957 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 134957 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 185197 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 185197 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 135705 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 135705 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 135113 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 135113 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 135280 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 135280 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 133278 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 133278 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 134879 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 134879 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 134819 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 134819 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 134800 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 134800 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 169578 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 169578 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 135536 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 135536 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 135674 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 135674 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 134865 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 134865 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 133354 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 133354 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 135057 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 135057 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 171944 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 171944 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 172647 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 172647 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 135068 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 135068 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 135475 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 135475 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 135449 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 135449 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 171022 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 171022 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 172846 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 172846 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 185473 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 185473 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 135634 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 135634 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 171683 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 171683 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 135698 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 135698 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 677 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 677 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 677 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 677 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 135278 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 135278 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 134111 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 134111 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 134965 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 134965 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 171799 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 171799 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 135432 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 135432 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 134995 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 134995 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 135212 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 135212 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 135675 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 135675 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 134020 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 134020 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 135645 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 135645 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 135137 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 135137 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 133663 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 133663 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 135684 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 135684 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 133336 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 133336 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 134341 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 134341 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 134818 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 134818 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 133831 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 133831 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 133564 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 133564 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 134991 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 134991 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 134081 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 134081 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 133448 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 133448 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 135460 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 135460 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 134388 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 134388 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 135457 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 135457 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 135065 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 135065 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 134955 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 134955 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 135655 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 135655 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 134794 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 134794 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 135608 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 135608 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 135325 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 135325 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 135094 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 135094 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 133905 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 133905 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 133524 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 133524 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 135611 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 135611 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 135438 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 135438 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 135326 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 135326 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 135753 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 135753 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 135439 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 135439 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 135023 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 135023 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 134850 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 134850 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 135446 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 135446 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 135663 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 135663 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 135580 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 135580 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 135145 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 135145 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 135300 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 135300 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 135111 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 135111 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 135651 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 135651 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 134947 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 134947 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 135001 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 135001 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 134790 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 134790 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 135666 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 135666 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 135151 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 135151 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 134811 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 134811 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 134948 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 134948 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 134872 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 134872 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 135334 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 135334 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 135398 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 135398 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 135122 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 135122 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 133330 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 133330 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 135089 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 135089 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 135668 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 135668 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 134837 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 134837 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 135124 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 135124 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 135213 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 135213 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 135233 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 135233 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 135257 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 135257 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 135373 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 135373 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 135691 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 135691 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 135554 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 135554 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 135589 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 135589 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 134809 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 134809 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 134812 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 134812 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 190870 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 190870 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 147154 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 147154 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 134073 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 134073 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 135644 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 135644 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 135383 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 135383 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 134883 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 134883 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 133624 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 133624 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 135613 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 135613 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 135613 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 135613 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 135093 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 135093 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 134049 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 134049 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 170186 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 170186 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 133873 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 133873 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 135629 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 135629 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 133873 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 133873 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 134795 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 134795 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 134994 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 134994 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 135530 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 135530 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 135125 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 135125 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 135726 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 135726 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 133193 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 133193 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 135195 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 135195 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 135321 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 135321 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 135676 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 135676 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 133411 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 133411 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 135577 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 135577 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 133635 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 133635 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 135740 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 135740 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 135441 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 135441 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 133918 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 133918 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 133902 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 133902 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 134907 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 134907 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 135273 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 135273 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 135142 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 135142 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 184059 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 184059 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 135549 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 135549 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 135305 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 135305 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 135499 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 135499 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 135453 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 135453 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 135525 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 135525 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 135269 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 135269 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 135264 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 135264 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 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 388 3 0 8 4.7 CSc1nn2cc(-c3nc4c(OC(F)(F)F)cccc4s3)nc2s1 nan
CHEMBL3728211 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 388 3 0 8 4.7 CSc1nn2cc(-c3nc4c(OC(F)(F)F)cccc4s3)nc2s1 nan
118068620 134985 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 134985 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 134856 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 134856 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 134924 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 134924 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 133873 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 133873 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 135180 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 135180 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 134833 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 134833 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 135028 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 135028 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 135442 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 135442 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 135436 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 135436 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 135576 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 135576 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 135183 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 135183 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 135614 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 135614 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 134916 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 134916 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 135295 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 135295 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 135688 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 135688 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 135222 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 135222 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 133702 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 133702 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 135127 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 135127 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 135232 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 135232 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 135356 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 135356 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 134412 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 134412 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 134250 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 134250 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 135149 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 135149 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 135345 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 135345 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 133638 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 133638 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 133666 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 133666 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 133411 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 133411 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 134820 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 134820 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 135323 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 135323 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 135387 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 135387 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 134898 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 134898 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 135652 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 135652 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 135104 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 135104 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 135329 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 135329 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 135326 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 135326 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 134333 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 134333 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 185197 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 185197 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 135418 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 135418 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 135243 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 135243 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 135391 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 135391 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 135486 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 135486 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 135214 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 135214 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 135702 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 135702 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 135741 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 135741 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 135693 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 135693 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 134850 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 134850 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 134887 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 134887 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 135691 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 135691 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 134894 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 134894 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 135389 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 135389 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 135247 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 135247 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 135427 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 135427 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 135321 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 135321 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 135364 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 135364 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 135047 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 135047 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 135345 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 135345 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 135559 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 135559 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 135361 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 135361 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 135354 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 135354 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 135195 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 135195 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 135387 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 135387 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 135649 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 135649 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 134909 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 134909 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 135461 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 135461 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 134988 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 134988 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 135515 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 135515 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 135724 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 135724 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 134926 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 134926 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 134897 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 134897 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 134870 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 134870 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 134221 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 134221 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 134221 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 134221 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 133150 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 133150 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 184498 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 184498 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 135119 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 135119 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 133447 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 133447 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 135494 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 135494 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 184059 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 184059 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 135025 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 135025 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 135291 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 135291 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 135605 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 135605 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 135191 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 135191 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 134991 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 134991 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 134878 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 134878 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 134829 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 134829 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 135135 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 135135 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 135275 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 135275 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 134036 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 134036 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 133897 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 133897 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 133171 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 133171 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 135664 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 135664 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 135083 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 135083 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 135282 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 135282 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 134893 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 134893 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 134088 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 134088 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 134088 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 134088 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 135618 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 135618 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 135089 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 135089 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 134903 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 134903 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 134843 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 134843 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 134835 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 134835 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 134020 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 134020 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 134787 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 134787 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 135447 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 135447 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 134881 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 134881 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 134848 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 134848 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 135131 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 135131 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 135456 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 135456 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 135241 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 135241 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 133654 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 133654 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 135086 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 135086 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 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 581 9 0 9 7.7 COc1cc(OCc2cccc(OCc3cc(Cl)cc(Cl)c3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3727768 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 581 9 0 9 7.7 COc1cc(OCc2cccc(OCc3cc(Cl)cc(Cl)c3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72193004 134321 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 134321 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 135579 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 135579 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 135469 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 135469 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 135521 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 135521 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 135370 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 135370 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 134848 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 134848 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 672 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 672 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 672 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 169229 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 169229 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 135669 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 135669 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 135595 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 135595 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 135540 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 135540 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 135133 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 135133 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 134779 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 134779 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 134919 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 134919 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 135259 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 135259 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 135338 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 135338 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 135301 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 135301 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 135720 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 135720 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 134921 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 134921 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 135740 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 135740 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 135465 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 135465 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 135468 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 135468 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 135065 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 135065 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 174715 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 174715 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 185473 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 185473 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 135510 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 135510 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 135678 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 135678 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 135379 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 135379 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 134828 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 134828 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 135109 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 135109 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 135626 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 135626 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 135200 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 135200 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 135522 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 135522 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 135211 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 135211 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 191698 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 191698 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 134815 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 134815 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 133442 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 133442 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 134938 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 134938 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 134095 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 134095 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 134897 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 134897 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 135382 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 135382 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 135665 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 135665 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 134788 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 134788 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 135640 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 135640 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 135097 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 135097 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 135583 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 135583 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 133624 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 133624 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 135744 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 135744 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 171460 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 171460 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 135153 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 135153 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 135377 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 135377 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 135085 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 135085 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 135736 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 135736 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 133632 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 133632 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 135186 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 135186 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 135715 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 135715 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 133774 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 133774 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 135683 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 135683 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 135606 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 135606 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 133640 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 133640 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 135107 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 135107 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 170660 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 170660 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 135343 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 135343 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 134845 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 134845 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 672 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 672 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 672 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 135403 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 135403 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 135351 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 135351 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 134827 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 134827 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 135737 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 135737 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 134977 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 134977 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 134810 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 134810 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 134883 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 134883 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 133739 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 133739 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 135563 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 135563 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 135382 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 135382 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 134866 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 134866 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 135503 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 135503 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 133353 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 133353 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 134946 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 134946 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 2537 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 2537 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 2537 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 4046 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 4046 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 4046 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 3858 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 3858 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 3858 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 672 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 672 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 672 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 672 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 672 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 672 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 133411 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 133411 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 147154 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 147154 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 185273 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 185273 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 147381 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 147381 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 147381 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 147381 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 135613 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 135613 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 183796 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 183796 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 184676 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 184676 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 113985 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 113985 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 134804 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 134804 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 185509 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 185509 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 143463 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 143463 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 143463 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 143463 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 143882 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 143882 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 185197 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 185197 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 134952 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 134952 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 169394 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 169394 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 149318 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 149318 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 149318 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 149318 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 184739 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 184739 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 151030 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 151030 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 4046 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 4046 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 4046 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 4046 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 4046 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 4046 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 169229 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 169229 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 151030 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 151030 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 149478 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 149478 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 145495 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 145495 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 149478 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 149478 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 174424 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 174424 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 145495 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 145495 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 174444 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 174444 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 174444 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 174444 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 184028 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 184028 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 185239 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 185239 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 173188 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 173188 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 173188 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 173188 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 2537 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 2537 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 2537 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 144298 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 144298 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 144298 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 144298 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 143882 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 143882 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 143882 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 143882 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 174606 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 174606 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 147154 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 147154 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 174606 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 174606 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 184059 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 184059 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 135613 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 135613 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 185542 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 185542 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 184498 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 184498 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 144688 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 144688 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 144688 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 144688 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 174424 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 174424 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 174424 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 174424 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 170186 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 170186 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 135489 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 135489 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 134872 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 134872 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 183933 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 183933 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 184691 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 184691 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 147381 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 147381 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 134012 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 134012 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 147381 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 147381 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 147381 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 147381 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 147381 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 147381 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 175296 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 175296 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 147862 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 147862 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 184782 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 184782 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 147862 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 147862 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 185071 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 185071 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 175296 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 175296 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 134804 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 134804 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 135618 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 135618 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 171916 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 171916 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 171916 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 171916 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 147727 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 147727 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 185131 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 185131 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 135595 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 135595 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 147154 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 147154 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 135089 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 135089 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 147727 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 147727 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 3858 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 3858 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 3858 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 172846 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 172846 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 152273 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 152273 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 184699 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 184699 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 152273 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 152273 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 147727 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 147727 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 147727 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 147727 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 134963 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 134963 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 184907 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 184907 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 184450 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 184450 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 147727 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 147727 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 134963 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 134963 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 171944 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 171944 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 113991 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 113991 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 144298 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 144298 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 144298 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 144298 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 153401 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 153401 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 183964 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 183964 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 184095 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 184095 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 135359 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 135359 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 184447 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 184447 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 185226 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 185226 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 113988 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 113988 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 184080 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 184080 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 143807 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 143807 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 185199 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 185199 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 143882 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 143882 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 143882 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 143882 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 169229 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 169229 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 135595 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 135595 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 147727 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 147727 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 185741 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 185741 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 149478 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 149478 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 149478 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 149478 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 170155 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 170155 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 185634 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 185634 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 183935 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 183935 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 174632 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 174632 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 185418 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 185418 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 174632 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 174632 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 153401 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 153401 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 153401 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 153401 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 170763 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 170763 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 143882 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 143882 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 148969 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 148969 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 148969 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 148969 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 170839 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 170839 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 135359 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 135359 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 172355 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 172355 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 172355 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 172355 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 185911 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 185911 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 183807 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 183807 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 185729 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 185729 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 174058 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 174058 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 174424 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 174424 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 142475 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 142475 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 142475 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 142475 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 172647 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 172647 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 174058 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 174058 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 185047 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 185047 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 173494 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 173494 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 146264 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 146264 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 134952 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 134952 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 173807 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 173807 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 173494 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 173494 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 185461 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 185461 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 146264 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 146264 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 172859 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 172859 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 174058 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 174058 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 172254 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 172254 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 172859 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 172859 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 172254 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 172254 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 175041 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 175041 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 172285 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 172285 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 172285 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 172285 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 113990 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 113990 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 146587 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 146587 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 146587 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 146587 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 184467 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 184467 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 150052 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 150052 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 150052 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 150052 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 135000 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 135000 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 185463 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 185463 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 184404 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 184404 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 184305 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 184305 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 169761 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 169761 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 185219 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 185219 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 146587 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 146587 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 146587 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 146587 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 145994 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 145994 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 145994 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 145994 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 147154 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 147154 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 143576 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 143576 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 143576 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 143576 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 171022 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 171022 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 153401 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 153401 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 153401 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 153401 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 153401 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 153401 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 184995 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 184995 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 113987 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 113987 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 185414 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 185414 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 113984 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 113984 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 113984 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 113984 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 184766 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 184766 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 151703 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 151703 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 151703 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 151703 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 184659 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 184659 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 143463 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 143463 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 171683 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 171683 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 143463 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 143463 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 672 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 672 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 672 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 185937 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 185937 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 141945 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 141945 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 141945 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 141945 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 185833 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 185833 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 135000 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 135000 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 149071 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 149071 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 149071 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 149071 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 183893 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 183893 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 170540 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 170540 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 113986 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 113986 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 184640 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 184640 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 113989 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 113989 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 3858 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 3858 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 3858 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 172376 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 172376 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 172376 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 172376 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 170503 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 170503 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 184625 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 184625 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 185442 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 185442 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 152273 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 152273 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 152273 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 152273 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 185473 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 185473 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 184796 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 184796 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 185776 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 185776 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 672 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 672 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 672 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 152474 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 152474 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 152474 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 152474 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 134963 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 134963 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 174058 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 174058 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 184050 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 184050 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 147381 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 147381 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 185681 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 185681 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 185224 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 185224 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 185889 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 185889 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 672 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 672 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 672 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 677 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 677 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 677 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 677 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 672 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 672 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 672 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 677 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 677 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 677 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 677 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 3858 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 3858 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 3858 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 3858 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 3858 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 3858 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 677 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 677 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 677 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 677 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