Ligand source activities (1 row/activity)



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117981510 133824 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 133824 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 134628 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 134628 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 134107 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 134107 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 134050 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 134050 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 134318 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 134318 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 133933 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 133933 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 134293 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 134293 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 134344 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 134344 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 134514 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 134514 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 134803 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 134803 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 134019 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 134019 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 134459 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 134459 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 134758 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 134758 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 134785 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 134785 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 134484 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 134484 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 133811 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 133811 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 133997 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 133997 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 133714 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 133714 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 134546 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 134546 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 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 555 7 0 13 4.6 COc1cc(OCc2csc(N3CCC4(CC3)OCCO4)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3714842 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 555 7 0 13 4.6 COc1cc(OCc2csc(N3CCC4(CC3)OCCO4)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
117981465 133936 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 133936 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 134815 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 134815 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 133934 3 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 133934 3 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 134027 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 134027 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 134393 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 134393 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 134548 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 134548 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 134644 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 134644 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 133943 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 133943 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 134166 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 134166 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 134192 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 134192 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 134245 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 134245 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 134764 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 134764 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 133677 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 133677 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 133845 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 133845 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 134782 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 134782 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 134173 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 134173 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 134072 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 134072 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 134271 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 134271 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 134880 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 134880 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 134947 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 134947 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 133948 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 133948 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 134020 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 512 7 1 11 5.4 COc1cc(OCc2csc(C3(O)CCCCC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3716144 134020 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 512 7 1 11 5.4 COc1cc(OCc2csc(C3(O)CCCCC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72190586 134204 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 134204 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 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 575 8 0 12 4.4 COc1cc(OCc2csc(C3CCN(S(C)(=O)=O)CC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3717435 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 575 8 0 12 4.4 COc1cc(OCc2csc(C3CCN(S(C)(=O)=O)CC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
72192725 134899 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 134899 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 133720 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 133720 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 134046 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 134046 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 134725 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 134725 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 133733 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 133733 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 134227 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 134227 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 134607 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 134607 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 134015 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 134015 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 134097 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 134097 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 134924 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 134924 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 133864 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 133864 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 133954 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 133954 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 134334 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 134334 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 134765 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 134765 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 134773 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 134773 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 679 29 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 679 29 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 679 29 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 133953 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 133953 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 134326 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 134326 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 134556 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 134556 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 134579 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 134579 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 134410 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 134410 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 134891 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 134891 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 684 11 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 684 11 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 684 11 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 684 11 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 133801 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 133801 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 133813 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 133813 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 134463 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 134463 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 134555 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 134555 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 133825 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 133825 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 134209 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 134209 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 134701 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 134701 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 133745 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 133745 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 133830 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 133830 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 134001 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 134001 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 134042 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 134042 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 133659 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 133659 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 133675 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 133675 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 133963 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 133963 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 133977 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 133977 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 134836 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 134836 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 134981 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 134981 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 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 544 7 1 11 5.6 COc1cc(OCc2nc(C3(O)CCOCC3)sc2C)c2cc(-c3cn4nc([C@H](C)F)sc4n3)oc2c1 nan
CHEMBL3715953 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 544 7 1 11 5.6 COc1cc(OCc2nc(C3(O)CCOCC3)sc2C)c2cc(-c3cn4nc([C@H](C)F)sc4n3)oc2c1 nan
72189345 134006 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 134006 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 134666 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 134666 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 134397 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 134397 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 134460 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 134460 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 134946 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 134946 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 133710 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 133710 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 134045 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 134045 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 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 603 11 0 11 6.8 CCCN(CC)C(=O)c1ccc(-c2nc(COc3cc(OC)cc4oc(-c5cn6nc(OC)sc6n5)cc34)cs2)cc1 nan
CHEMBL3716676 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 603 11 0 11 6.8 CCCN(CC)C(=O)c1ccc(-c2nc(COc3cc(OC)cc4oc(-c5cn6nc(OC)sc6n5)cc34)cs2)cc1 nan
117981582 133923 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 133923 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 134028 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 134028 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 133641 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 133641 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 134491 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 134491 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 133711 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 133711 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 134150 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 134150 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 134828 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 134828 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 134379 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 134379 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 134882 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 134882 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 133806 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 133806 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 133987 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 133987 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 134560 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 134560 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 134826 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 134826 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 134929 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 134929 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 134315 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 134315 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 134710 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 134710 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 133868 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 133868 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 134638 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 134638 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 134679 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 134679 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 134843 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 134843 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 133646 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 133646 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 133855 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 133855 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 133935 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 133935 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 134431 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 134431 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 133707 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 133707 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 133982 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 133982 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 133999 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 133999 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 134886 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 134886 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 134781 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 134781 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 134784 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 134784 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 133772 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 133772 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 133827 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 133827 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 134623 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 134623 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 134788 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 134788 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 134501 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 134501 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 134600 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 134600 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 134756 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 134756 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 134168 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 134168 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 134316 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 134316 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 134430 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 134430 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 134933 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 134933 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 133666 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 133666 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 133896 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 133896 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 133917 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 133917 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 134322 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 134322 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 134439 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 134439 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 134477 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 134477 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 134684 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 134684 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 133706 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 133706 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 134291 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 134291 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 133796 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 133796 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 134535 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 134535 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 134757 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 134757 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 134953 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 134953 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 134385 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 134385 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 134937 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 134937 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 134584 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 134584 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 134931 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 134931 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 133642 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 133642 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 133670 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 133670 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 133891 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 133891 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 133730 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 133730 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 134539 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 134539 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 133765 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 133765 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 133924 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 133924 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 134405 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 134405 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 134659 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 134659 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 134646 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 134646 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 134308 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 134308 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 134712 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 134712 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 133834 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 133834 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 134377 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 134377 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 134504 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 134504 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 134265 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 134265 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 134388 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 134388 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 134627 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 134627 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 134817 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 134817 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 134082 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 134082 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 134073 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 134073 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 134945 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 134945 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 134220 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 134220 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 134526 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 134526 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 135034 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 135034 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 135034 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 133906 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 133906 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 134137 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 134137 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 134176 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 134176 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 134777 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 134777 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 134104 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 134104 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 134943 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 134943 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 133753 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 133753 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 134398 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 134398 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 134917 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 134917 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 133820 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 133820 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 134174 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 134174 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 134289 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 134289 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 134533 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 134533 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 134887 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 134887 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 133774 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 133774 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 133780 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 133780 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 133903 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 133903 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 134144 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 134144 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 134221 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 134221 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 134298 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 134298 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 134383 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 134383 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 134541 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 134541 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 134676 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 134676 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 134940 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 134940 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 134966 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 134966 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 133750 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 133750 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 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 573 8 0 11 5.8 COc1cc(OCc2csc(-c3ccc(C(=O)N4CCC4)cc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3715492 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 573 8 0 11 5.8 COc1cc(OCc2csc(-c3ccc(C(=O)N4CCC4)cc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
117981494 133915 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 133915 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 134154 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 134154 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 134200 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 134200 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 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 550 7 0 10 6.6 COc1cc(OCc2csc(C3(F)CCC(F)(F)CC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3717023 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 550 7 0 10 6.6 COc1cc(OCc2csc(C3(F)CCC(F)(F)CC3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
117981460 134351 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 134351 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 134389 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 134389 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 134506 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 134506 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 134516 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 134516 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 134833 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 134833 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 134848 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 134848 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 134892 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 134892 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 133649 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 133649 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 133742 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 133742 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 133879 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 133879 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 133932 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 133932 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 133964 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 133964 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 134023 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 134023 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 134128 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 134128 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 134141 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 134141 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 134188 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 134188 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 134418 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 134418 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 134630 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 134630 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 134720 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 134720 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 134810 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 134810 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 134905 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 134905 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 133905 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 133905 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 134511 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 134511 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 134801 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 134801 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 134923 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 134923 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 134444 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 134444 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 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 615 8 0 11 6.9 COc1cc(OCc2csc(-c3ccc(C(=O)N4C(C)CCC4C)cc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3715559 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 615 8 0 11 6.9 COc1cc(OCc2csc(-c3ccc(C(=O)N4C(C)CCC4C)cc3)n2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
86700913 134008 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 134008 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 134252 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 134252 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 134333 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 134333 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 134370 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 134370 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 133692 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 133692 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 133788 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 133788 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 133853 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 133853 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 134206 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 134206 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 134674 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 134674 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 133841 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 133841 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 133871 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 133871 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 134438 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 134438 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 133631 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 133631 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 133885 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 133885 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 134390 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 134390 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 134039 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 134039 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 134671 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 134671 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 134029 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 134029 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 134136 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 134136 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 134637 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 134637 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 134554 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 134554 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 134058 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 493 6 0 9 5.4 COc1cc(OCc2csc(N3CCC(F)CC3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
CHEMBL3716259 134058 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assay
ChEMBL 493 6 0 9 5.4 COc1cc(OCc2csc(N3CCC(F)CC3)n2)c2cc(-c3cn4nc(C)ccc4n3)oc2c1 nan
89878653 134840 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 134840 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 134594 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 134594 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 133836 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 133836 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 134335 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 134335 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 134234 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 134234 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 133859 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 133859 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 134336 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 134336 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 134706 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 134706 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 134861 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 134861 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 134432 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 134432 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 134465 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 134465 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 134581 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 134581 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 133638 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 133638 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 133890 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 133890 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 134605 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 134605 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 134794 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 134794 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 134057 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 134057 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 134133 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 134133 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 134427 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 134427 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 134850 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 134850 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 134081 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 134081 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 134544 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 134544 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 133686 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 133686 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 134285 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 134285 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 133886 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 133886 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 133904 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 133904 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 134111 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 134111 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 134365 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 134365 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 134369 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 134369 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 134893 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 134893 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 134911 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 134911 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 133713 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 133713 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 133789 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 133789 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 134182 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 134182 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 134920 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 134920 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 134567 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 134567 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 134952 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 134952 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 134461 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 134461 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 133784 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 133784 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 134875 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 134875 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 134428 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 134428 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 134085 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 134085 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 134033 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 134033 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 134140 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 134140 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 133674 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 133674 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 134670 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 134670 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 133991 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 133991 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 133799 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 133799 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 133895 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 133895 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 134984 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 134984 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 133989 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 133989 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 134522 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 134522 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 134337 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 134337 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 133682 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 133682 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 134050 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 134050 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 133701 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 133701 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 134244 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 134244 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 134360 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 134360 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 133934 3 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 133934 3 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 134344 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 134344 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 134546 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 134546 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 134764 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 134764 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 134678 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 134678 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 136071 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 136071 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 134400 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 134400 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 133691 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 133691 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 134426 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 134426 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 134894 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 134894 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 134837 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 134837 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 134847 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 134847 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 679 29 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 679 29 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 679 29 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 684 11 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 684 11 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 684 11 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 684 11 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 133933 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 133933 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 134579 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 134579 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 191211 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 191211 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 192295 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 192295 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 134155 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 134155 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 134146 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 134146 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 134535 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 134535 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 134735 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 134735 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 134906 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 134906 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 133900 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 133900 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 134864 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 134864 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 133900 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 133900 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 134001 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 134001 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 134666 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 134666 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 134735 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 134735 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 134906 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 134906 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 134099 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 134099 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 185378 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 185378 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 133862 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 133862 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 133928 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 133928 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 679 29 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 679 29 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 679 29 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 133976 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 133976 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 134241 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 134241 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 135796 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 135796 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 134171 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 134171 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 133646 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 133646 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 133868 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 133868 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 133935 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 133935 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 133999 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 133999 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 134171 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 134171 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 134679 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 134679 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 134929 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 134929 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 190370 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 190370 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 190858 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 190858 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 134313 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 134313 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 134769 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 134769 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 134120 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 134120 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 134452 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 134452 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 134550 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 134550 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 134430 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 134430 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 134452 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 134452 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 189996 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 189996 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 679 29 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 679 29 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 679 29 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 134083 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 134083 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 134122 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 134122 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 134343 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 134343 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 135567 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 135567 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 135321 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 135321 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 134219 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 134219 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 134483 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 134483 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 135900 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 135900 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 133897 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 133897 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 133730 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 133730 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 133834 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 133834 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 134292 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 134292 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 190168 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 190168 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 174379 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 174379 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 134101 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 134101 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 134884 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 134884 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 135453 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 135453 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 135903 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 135903 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 171405 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 171405 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 134950 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 134950 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 134950 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 134950 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 133796 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 133796 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 134853 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 134853 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 134491 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 134491 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 171070 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 171070 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 135523 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 135523 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 135523 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 135523 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 134947 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 134947 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 134942 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 134942 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 182124 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 182124 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 133694 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 133694 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 134131 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 134131 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 133699 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 133699 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 133919 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 133919 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 134968 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 134968 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 134521 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 134521 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 134971 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 134971 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 135520 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 135520 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 134080 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 134080 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 133774 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 133774 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 134968 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 134968 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 192234 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 192234 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 171106 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 171106 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 134288 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 134288 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 135996 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 135996 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 135767 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 135767 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 136099 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 136099 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 134619 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 134619 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 134006 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 134006 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 135475 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 135475 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 171329 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 171329 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 185081 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 185081 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 133808 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 133808 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 134088 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 134088 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 135475 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 135475 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 135867 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 135867 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 136273 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 136273 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 136272 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 136272 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 133986 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 133986 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 135669 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 135669 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 134532 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 134532 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 134630 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 134630 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 134892 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 134892 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 170329 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 170329 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 133738 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 133738 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 135837 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 135837 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 134879 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 134879 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 134190 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 134190 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 135908 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 135908 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 133844 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 133844 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 133901 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 133901 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 134354 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 134354 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 136113 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 136113 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 134761 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 134761 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 134354 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 134354 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 134444 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 134444 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 134348 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 134348 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 134957 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 134957 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 133939 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 133939 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 133834 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 133834 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 134548 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 134548 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 136081 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 136081 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 170722 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 170722 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 173876 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 173876 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 134973 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 134973 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 135608 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 135608 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 135969 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 135969 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 134009 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 134009 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 135397 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 135397 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 134360 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 134360 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 135956 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 135956 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 136018 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 136018 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 133908 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 133908 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 191174 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 191174 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 134441 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 134441 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 135770 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 135770 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 134483 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 134483 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 133871 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 133871 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 175614 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 175614 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 135730 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 135730 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 134292 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 134292 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 134211 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 134211 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 134027 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 134027 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 134245 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 134245 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 134533 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 134533 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 134679 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 134679 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 135649 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 135649 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 136189 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 136189 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 135526 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 135526 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 135681 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 135681 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 136038 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 136038 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 135800 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 135800 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 136054 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 136054 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 135639 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 135639 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 135327 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 135327 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 135464 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 135464 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 136129 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 136129 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 135746 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 135746 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 135407 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 135407 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 135930 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 135930 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 135899 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 135899 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 134083 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 134083 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 135908 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 135908 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 135978 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 135978 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 136133 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 136133 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 185996 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 185996 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 136215 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 136215 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 135397 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 135397 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 136046 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 136046 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 135327 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 135327 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 135486 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 135486 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 170885 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 170885 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 135533 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 135533 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 136205 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 136205 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 135828 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 135828 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 136183 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 136183 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 135623 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 135623 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 135377 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 135377 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 135483 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 135483 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 135747 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 135747 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 136151 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 136151 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 135702 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 135702 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 135943 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 135943 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 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 630 9 1 11 5.9 CSc1nn2cc(-c3nc4c(OC[C@@H]5CCCN5C(=O)[C@H](NC(=O)c5cccs5)c5ccccc5)cccc4o3)nc2s1 nan
CHEMBL3729809 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 630 9 1 11 5.9 CSc1nn2cc(-c3nc4c(OC[C@@H]5CCCN5C(=O)[C@H](NC(=O)c5cccs5)c5ccccc5)cccc4o3)nc2s1 nan
126507530 180137 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 180137 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 136060 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 136060 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 135552 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 135552 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 135993 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 135993 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 135316 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 135316 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 136185 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 136185 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 135916 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 135916 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 135626 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 135626 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 135452 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 135452 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 135536 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 135536 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 136206 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 136206 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 134807 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 134807 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 135863 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 135863 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 136218 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 136218 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 135466 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 135466 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 134021 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 134021 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 136067 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 136067 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 135771 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 135771 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 135704 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 135704 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 135486 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 135486 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 136223 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 136223 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 135562 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 135562 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 136220 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 136220 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 135749 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 135749 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 135424 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 135424 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 136145 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 136145 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 135629 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 135629 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 135486 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 135486 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 135856 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 135856 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 135738 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 135738 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 136147 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 136147 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 136018 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 136018 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 135646 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 135646 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 135419 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 135419 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 135625 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 135625 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 136136 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 136136 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 135549 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 135549 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 136239 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 136239 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 135500 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 135500 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 135742 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 135742 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 135393 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 135393 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 136175 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 136175 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 135685 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 135685 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 134685 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 134685 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 135476 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 135476 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 136011 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 136011 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 136258 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 136258 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 135842 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 135842 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 135367 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 135367 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 135691 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 135691 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 135892 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 135892 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 136050 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 136050 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 135887 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 135887 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 135862 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 135862 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 136013 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 136013 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 135690 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 135690 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 185321 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 185321 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 135573 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 135573 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 135315 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 135315 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 135395 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 135395 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 136042 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 136042 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 136158 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 136158 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 136158 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 136158 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 135472 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 135472 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 135382 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 135382 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 135554 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 135554 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 170226 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 170226 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 135790 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 135790 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 135659 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 135659 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 135532 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 135532 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 135683 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 135683 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 135789 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 135789 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 185378 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 185378 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 135878 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 135878 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 135891 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 135891 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 169540 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 169540 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 136087 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 136087 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 135839 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 135839 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 133707 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 133707 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 134887 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 134887 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 134945 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 134945 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 136005 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 136005 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 133984 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 133984 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 133761 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 133761 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 135929 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 135929 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 684 11 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 684 11 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 684 11 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 684 11 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 134701 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 134701 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 135977 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 135977 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 135712 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 135712 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 134467 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 134467 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 135805 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 135805 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 133656 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 133656 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 134102 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 134102 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 133677 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 133677 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 134079 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 134079 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 135949 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 135949 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 136122 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 136122 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 135800 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 135800 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 135848 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 135848 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 135634 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 135634 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 135743 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 135743 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 136028 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 136028 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 173779 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 173779 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 134849 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 134849 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 3921 7 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 3921 7 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 3921 7 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 134336 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 134336 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 3921 7 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 3921 7 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 3921 7 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 169961 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 169961 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 179656 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 179656 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 3921 7 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 3921 7 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 3921 7 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 134311 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 134311 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 135360 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 135360 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 135917 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 135917 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 136271 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 136271 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 135389 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 135389 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 136195 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 136195 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 135511 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 135511 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 135435 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 135435 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 191543 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 191543 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 136118 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 136118 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 136229 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 136229 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 134735 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 134735 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 134426 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 134426 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 135700 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 135700 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 135918 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 135918 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 135523 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 135523 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 135417 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 135417 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 136270 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 136270 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 134600 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 134600 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 135535 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 135535 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 136105 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 136105 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 136092 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 136092 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 135885 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 135885 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 135445 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 135445 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 135713 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 135713 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 135709 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 301 2 0 6 4.2 CSc1nn2cc(-c3cc4cccc(C)c4o3)nc2s1 nan
CHEMBL3729892 135709 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 301 2 0 6 4.2 CSc1nn2cc(-c3cc4cccc(C)c4o3)nc2s1 nan
118070611 135558 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 135558 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 135765 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 135765 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 134189 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 134189 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 136169 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 136169 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 136135 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 136135 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 135917 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 135917 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 135894 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 135894 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 136036 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 136036 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 135811 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 135811 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 136036 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 136036 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 134634 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 134634 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 135359 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 135359 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 136245 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 136245 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 135519 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 135519 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 134050 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 134050 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 134200 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 134200 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 134351 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 134351 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 136197 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 136197 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 136146 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 136146 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 134965 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 134965 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 135457 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 135457 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 135716 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 135716 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 134506 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 134506 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 135980 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 135980 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 133890 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 133890 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 135555 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 135555 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 133692 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 133692 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 135820 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 135820 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 133886 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 133886 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 135792 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 135792 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 133650 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 133650 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 134042 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 134042 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 135882 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 135882 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 136177 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 136177 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 135446 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 135446 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 135882 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 135882 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 134160 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 134160 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 3921 7 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 3921 7 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 3921 7 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 135427 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 135427 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 134596 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 134596 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 136192 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 136192 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 134166 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 134166 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 134174 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 134174 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 135524 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 135524 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 136051 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 136051 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 135510 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 135510 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 135890 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 135890 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 136117 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 136117 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 134097 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 134097 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 134712 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 134712 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 136012 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 136012 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 136012 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 136012 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 135679 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 135679 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 134567 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 134567 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 136234 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 136234 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 134158 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 134158 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 135975 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 135975 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 134555 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 134555 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 134785 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 134785 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 134933 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 134933 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 173453 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 173453 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 135843 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 135843 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 135563 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 135563 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 136203 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 136203 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 133904 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 133904 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 136165 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 136165 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 136023 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 136023 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 135314 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 135314 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 134241 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 134241 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 133885 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 133885 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 134756 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 134756 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 134764 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 134764 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 135331 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 135331 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 135480 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 135480 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 185779 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 185779 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 136228 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 136228 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 135636 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 135636 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 135803 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 135803 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 133801 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 133801 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 135402 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 135402 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 135342 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 135342 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 135323 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 135323 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 170145 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 170145 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 136059 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 136059 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 136197 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 136197 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 135388 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 135388 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 133877 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 133877 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 135580 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 135580 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 172511 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 172511 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 173218 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 173218 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 135591 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 135591 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 135998 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 135998 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 135972 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 135972 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 171588 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 171588 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 173418 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 173418 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 186055 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 186055 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 136157 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 136157 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 172249 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 172249 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 136221 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 136221 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 684 11 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 684 11 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 684 11 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 684 11 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 135801 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 135801 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 134634 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 134634 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 135488 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 135488 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 172365 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 172365 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 135955 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 135955 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 135518 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 135518 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 135735 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 135735 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 136198 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 136198 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 134543 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 134543 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 136168 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 136168 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 135660 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 135660 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 134186 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 134186 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 136207 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 136207 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 133859 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 133859 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 134864 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 134864 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 135341 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 135341 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 134354 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 134354 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 134087 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 134087 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 135514 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 135514 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 134604 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 134604 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 133971 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 133971 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 135983 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 135983 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 134911 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 134911 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 135980 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 135980 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 135588 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 135588 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 135478 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 135478 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 136178 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 136178 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 135317 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 135317 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 136131 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 136131 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 135848 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 135848 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 135617 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 135617 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 134428 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 134428 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 134047 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 134047 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 136134 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 136134 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 135961 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 135961 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 135849 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 135849 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 136276 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 136276 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 135962 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 135962 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 135546 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 135546 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 135373 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 135373 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 135969 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 135969 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 136186 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 136186 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 136103 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 136103 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 135668 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 135668 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 135823 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 135823 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 135634 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 135634 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 136174 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 136174 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 135470 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 135470 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 135524 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 135524 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 135313 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 135313 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 136189 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 136189 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 135674 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 135674 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 135334 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 135334 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 135471 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 135471 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 135395 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 135395 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 135857 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 135857 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 135921 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 135921 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 135645 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 135645 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 133853 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 133853 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 135612 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 135612 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 136191 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 136191 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 135360 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 135360 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 135647 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 135647 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 135736 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 135736 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 135756 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 135756 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 135780 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 135780 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 135896 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 135896 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 136214 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 136214 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 136077 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 136077 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 136112 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 136112 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 135332 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 135332 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 135335 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 135335 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 191466 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 191466 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 147687 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 147687 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 134596 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 134596 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 136167 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 136167 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 135906 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 135906 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 135406 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 135406 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 134147 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 134147 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 136136 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 136136 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 136136 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 136136 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 135616 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 305 2 0 6 4.1 CSc1nn2cc(-c3cc4c(F)cccc4o3)nc2s1 nan
CHEMBL3729338 135616 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 305 2 0 6 4.1 CSc1nn2cc(-c3cc4c(F)cccc4o3)nc2s1 nan
118042461 134572 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 134572 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 170753 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 170753 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 134396 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 134396 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 136152 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 136152 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 134396 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 134396 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 135318 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 135318 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 135517 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 567 9 0 9 6.8 COc1cc(OCc2cccc(OCc3cc(F)c(F)c(F)c3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3728680 135517 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 567 9 0 9 6.8 COc1cc(OCc2cccc(OCc3cc(F)c(F)c(F)c3)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118070674 136053 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 136053 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 135648 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 135648 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 136249 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 136249 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 133716 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 133716 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 135718 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 135718 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 135844 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 135844 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 136199 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 136199 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 133934 3 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 133934 3 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 136100 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 136100 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 134158 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 134158 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 136263 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 136263 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 135964 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 135964 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 134441 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 134441 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 134425 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 134425 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 135430 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 135430 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 135796 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 135796 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 135665 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 135665 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 184642 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 184642 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 136072 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 136072 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 135828 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 135828 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 136022 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 136022 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 135976 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 135976 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 136048 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 136048 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 135792 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 135792 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 135787 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 135787 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 135434 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 135434 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 135508 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 135508 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 135379 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 135379 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 135447 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 135447 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 134396 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 134396 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 135703 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 135703 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 135356 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 135356 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 135551 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 135551 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 135965 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 135965 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 135959 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 135959 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 136099 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 136099 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 135706 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 135706 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 136137 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 136137 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 135439 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 135439 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 135818 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 135818 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 136211 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 136211 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 135745 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 135745 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 134225 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 134225 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 135650 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 135650 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 135755 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 135755 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 135879 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 135879 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 134935 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 134935 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 134773 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 134773 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 135672 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 135672 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 135868 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 135868 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 134161 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 134161 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 134189 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 134189 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 133934 3 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 133934 3 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 135343 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 135343 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 135846 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 135846 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 135910 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 135910 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 135421 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 135421 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 136175 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 136175 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 135627 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 135627 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 135852 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 135852 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 135849 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 135849 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 134856 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 134856 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 185779 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 185779 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 135941 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 135941 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 135766 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 135766 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 135914 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 135914 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 136009 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 136009 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 135737 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 135737 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 136225 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 136225 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 136264 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 136264 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 136216 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 136216 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 135373 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 135373 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 135410 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 135410 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 136214 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 136214 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 135417 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 135417 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 135912 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 135912 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 135770 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 135770 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 135950 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 135950 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 135844 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 135844 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 135887 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 135887 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 135570 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 135570 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 135868 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 135868 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 136082 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 136082 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 135884 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 135884 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 135877 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 135877 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 135718 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 135718 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 135910 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 135910 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 136172 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 136172 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 135432 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 135432 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 135984 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 135984 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 135511 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 135511 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 136038 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 136038 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 136247 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 136247 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 135449 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 135449 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 135420 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 135420 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 135393 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 135393 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 134744 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 134744 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 134744 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 134744 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 133673 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 133673 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 185081 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 185081 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 135642 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 135642 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 133970 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 133970 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 136017 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 136017 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 184642 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 184642 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 135548 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 135548 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 135814 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 135814 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 136128 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 136128 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 135714 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 135714 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 135514 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 135514 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 135401 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 135401 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 135352 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 135352 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 135658 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 135658 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 135798 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 135798 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 134559 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 134559 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 134420 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 134420 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 133694 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 133694 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 136187 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 136187 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 135606 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 135606 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 135805 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 135805 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 135416 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 135416 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 134611 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 134611 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 134611 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 134611 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 136141 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 136141 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 135612 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 135612 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 135426 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 135426 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 135366 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 135366 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 135358 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 135358 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 134543 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 134543 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 135310 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 135310 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 135970 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 135970 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 135404 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 135404 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 135371 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 135371 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 135654 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 135654 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 135979 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 135979 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 135764 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 135764 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 134177 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 134177 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 135609 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 135609 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 135358 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 135358 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 134844 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 134844 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 136102 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 136102 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 135992 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 135992 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 136044 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 136044 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 135893 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 135893 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 135371 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 135371 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 679 29 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 679 29 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 679 29 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 169796 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 169796 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 136192 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 136192 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 136118 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 136118 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 136063 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 136063 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 135656 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 639 9 0 9 7.0 COc1cc(OCc2cccc(OCc3ccccc3I)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
CHEMBL3729581 135656 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins before agonist addition by FLIPR assay
ChEMBL 639 9 0 9 7.0 COc1cc(OCc2cccc(OCc3ccccc3I)c2)c2cc(-c3cn4nc(OC)sc4n3)oc2c1 nan
118068458 135302 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 135302 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 135442 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 135442 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 135782 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 135782 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 135861 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 135861 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 135824 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 135824 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 136243 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 136243 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 135444 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 135444 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 136263 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 136263 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 135988 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 135988 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 135991 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 135991 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 135588 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 135588 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 175287 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 175287 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 186055 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 186055 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 136033 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 136033 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 136201 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 136201 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 135902 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 135902 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 135351 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 135351 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 135632 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 135632 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 136149 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 136149 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 135723 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 135723 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 136045 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 136045 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 135734 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 135734 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 192296 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 192296 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 135338 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 135338 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 133965 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 133965 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 135461 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 135461 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 134618 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 134618 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 135420 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 135420 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 135905 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 135905 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 136188 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 136188 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 135311 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 135311 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 136163 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 136163 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 135620 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 135620 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 136106 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 136106 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 134147 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 134147 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 136267 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 136267 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 172026 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 172026 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 135676 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 135676 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 135900 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 135900 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 135608 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 135608 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 136259 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 136259 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 134155 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 134155 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 135709 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 135709 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 136238 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 136238 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 134297 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 134297 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 136206 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 136206 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 136129 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 136129 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 134163 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 134163 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 135630 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 135630 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 171226 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 171226 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 135866 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 135866 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 135368 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 135368 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 679 29 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 679 29 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 679 29 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 135926 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 135926 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 135874 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 135874 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 135350 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 135350 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 136260 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 136260 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 135500 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 135500 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 135333 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 135333 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 135406 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 135406 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 134262 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 134262 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 136086 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 136086 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 135905 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 135905 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 135389 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 135389 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 136026 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 136026 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 133876 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 133876 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 135469 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 135469 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 2574 50 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 2574 50 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 2574 50 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 4109 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 4109 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 4109 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 3921 7 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 3921 7 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 3921 7 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 679 29 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 679 29 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 679 29 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 679 29 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 679 29 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 679 29 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


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Ligands (move mouse cursor over ligand name to see structure) Receptor Assay information Chemical information
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71769562 133934 3 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 133934 3 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 147687 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 147687 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 185855 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 185855 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 147914 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 147914 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 147914 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 147914 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 136136 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 136136 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 184378 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 184378 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 185258 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 185258 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 114483 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 114483 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 135327 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 135327 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 186091 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 186091 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 143995 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 143995 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 143995 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 143995 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 144415 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 144415 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 185779 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 185779 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 135475 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 135475 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 169961 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 169961 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 149850 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 149850 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 149850 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 149850 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 185321 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 185321 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 151562 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 151562 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 4109 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 4109 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 4109 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 4109 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 4109 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 4109 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 169796 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 169796 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 151562 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 151562 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 150010 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 150010 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 146028 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 146028 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 150010 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 150010 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 174996 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 174996 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 146028 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 146028 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 175016 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 175016 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 175016 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 175016 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 184611 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 184611 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 185821 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 185821 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 173760 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 173760 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 173760 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 173760 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 2574 50 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 2574 50 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 2574 50 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 144831 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 144831 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 144831 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 144831 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 144415 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 144415 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 144415 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 144415 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 175178 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 175178 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 147687 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 147687 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 175178 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 175178 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 184642 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 184642 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 136136 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 136136 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 186124 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 186124 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 185081 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 185081 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 145221 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 145221 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 145221 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 145221 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 174996 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 174996 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 174996 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 174996 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 170753 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 170753 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 136012 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 136012 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 135395 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 135395 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 184515 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 184515 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 185273 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 185273 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 147914 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 147914 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 134535 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 134535 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 147914 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 147914 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 147914 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 147914 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 147914 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 147914 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 175869 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 175869 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 148394 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 148394 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 185364 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 185364 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 148394 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 148394 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 185653 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 185653 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 175869 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 175869 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 135327 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 135327 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 136141 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 136141 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 172483 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 172483 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 172483 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 172483 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 148259 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 148259 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 185713 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 185713 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 136118 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 136118 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 147687 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 147687 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 135612 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 135612 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 148259 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 148259 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 3921 7 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 3921 7 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 3921 7 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 173418 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 173418 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 152805 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 152805 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 185281 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 185281 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 152805 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 152805 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 148259 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 148259 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 148259 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 148259 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 135486 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 135486 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 185489 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 185489 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 185033 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 185033 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 148259 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 148259 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 135486 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 135486 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 172511 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 172511 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 114489 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 114489 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 144831 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 144831 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 144831 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 144831 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 153935 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 153935 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 184547 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 184547 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 184678 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 184678 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 135882 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 135882 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 185030 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 185030 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 185808 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 185808 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 114486 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 114486 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 184663 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 184663 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 144339 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 144339 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 185781 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 185781 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 144415 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 144415 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 144415 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 144415 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 169796 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 169796 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 136118 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 136118 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 148259 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 148259 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 186323 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 186323 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 150010 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 150010 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 150010 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 150010 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 170722 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 170722 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 186216 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 186216 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 184517 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 184517 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 175204 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 175204 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 186000 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 186000 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 175204 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 175204 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 538 35 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 538 35 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 538 35 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 153935 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 153935 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 153935 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 153935 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 171329 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 171329 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 144415 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 144415 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 149501 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 149501 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 149501 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 149501 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 171405 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 171405 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 135882 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 135882 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 172924 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 172924 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 172924 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 172924 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 186493 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 186493 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 184389 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 184389 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 186311 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 186311 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 174630 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 174630 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 174996 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 174996 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 143007 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 143007 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 143007 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 143007 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 173218 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 173218 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 174630 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 174630 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 185629 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 185629 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 174066 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 174066 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 146797 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 146797 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 135475 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 135475 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 174379 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 174379 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 174066 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 174066 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 186043 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 186043 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 146797 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 146797 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 173431 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 173431 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 174630 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 174630 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 172823 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 172823 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 173431 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 173431 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 172823 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 172823 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 175614 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 175614 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 172854 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 172854 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 172854 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 172854 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 114488 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 114488 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 147120 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 147120 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 147120 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 147120 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 185050 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 185050 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 150585 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 150585 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 150585 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 150585 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 135523 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 135523 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 186045 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 186045 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 184987 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 184987 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 184888 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 184888 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 170329 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 170329 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 185801 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 185801 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 147120 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 147120 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 147120 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 147120 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 146527 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 146527 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 146527 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 146527 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 147687 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 147687 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 144108 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 144108 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 144108 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 144108 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 171588 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 171588 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 153935 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 153935 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 153935 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 153935 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 153935 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 153935 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 185577 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 185577 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 114485 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 114485 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 185996 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 185996 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 114482 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 114482 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 114482 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 114482 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 185348 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 185348 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 152235 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 152235 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 152235 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 152235 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 185241 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 185241 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 143995 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 143995 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 172249 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 172249 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 143995 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 143995 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 679 29 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 679 29 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 679 29 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 186519 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 186519 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 142477 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 142477 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 142477 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 142477 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 186415 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 186415 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 135523 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 135523 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 149603 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 149603 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 149603 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 149603 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 184475 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 184475 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 171106 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 171106 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 114484 17 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 114484 17 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 185223 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 185223 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 114487 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 114487 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 3921 7 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 3921 7 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 3921 7 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 172945 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 172945 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 172945 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 172945 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 171070 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 171070 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 185208 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 185208 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 186024 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 186024 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 152805 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 152805 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 152805 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 152805 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 186055 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 186055 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 185378 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 185378 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 186358 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 186358 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 679 29 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 679 29 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 679 29 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 153008 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 153008 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 153008 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 153008 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 135486 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 135486 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 174630 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 174630 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 184633 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 184633 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 147914 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 147914 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 186263 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 186263 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 185806 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 185806 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 186471 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 186471 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 679 29 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 679 29 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 679 29 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 684 11 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 684 11 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 684 11 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 684 11 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 679 29 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 679 29 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 679 29 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 684 11 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 684 11 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 684 11 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 684 11 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 3921 7 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 3921 7 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 3921 7 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 3921 7 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 3921 7 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 3921 7 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 684 11 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 684 11 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 684 11 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 684 11 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