Ligand source activities (1 row/activity)
| Ligands (move mouse cursor over ligand name to see structure) | Receptor | Activity | Chemical information | |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Sel. page | Common name
| GPCRdb ID
| Reference ligand
| Vendors | Species
| Assay Type
| Activity Type
| Activity Relation
| Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description
| Source
| Mol weight | Rot Bonds | H don | H acc | LogP | Smiles
| DOI
| |
Ligands (move mouse cursor over ligand name to see structure)
| Receptor
| Activity
| Chemical information
| |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Sel. page | Common name
| GPCRdb ID
| Reference ligand
| Vendors | Species
| Assay Type
| Activity Type
| Activity Relation
| Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description
| Source
| Mol weight | Rot Bonds | H don | H acc | LogP | Smiles
| DOI
| |
| 117981510 | 133893 | None | 0 | Human | Functional | pEC50 | = | 9.7 | 9.7 | - | 1 | Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-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 | 133893 | None | 0 | Human | Functional | pEC50 | = | 9.7 | 9.7 | - | 1 | Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-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 | 134697 | None | 0 | Human | Functional | pEC50 | = | 9.7 | 9.7 | - | 1 | Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-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 | 134697 | None | 0 | Human | Functional | pEC50 | = | 9.7 | 9.7 | - | 1 | Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-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 | 134176 | None | 0 | Human | Functional | pEC50 | = | 9.6 | 9.6 | - | 1 | Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-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 | 134176 | None | 0 | Human | Functional | pEC50 | = | 9.6 | 9.6 | - | 1 | Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-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 | 134119 | None | 0 | Human | Functional | pEC50 | = | 9.6 | 9.6 | - | 1 | Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-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 | 134119 | None | 0 | Human | Functional | pEC50 | = | 9.6 | 9.6 | - | 1 | Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-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 | 134387 | None | 0 | Human | Functional | pEC50 | = | 9.6 | 9.6 | - | 1 | Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-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 | 134387 | None | 0 | Human | Functional | pEC50 | = | 9.6 | 9.6 | - | 1 | Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-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 | 134002 | None | 0 | Human | Functional | pEC50 | = | 9.6 | 9.6 | - | 1 | Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-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 | 134002 | None | 0 | Human | Functional | pEC50 | = | 9.6 | 9.6 | - | 1 | Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-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 | 134362 | None | 0 | Human | Functional | pEC50 | = | 9.6 | 9.6 | - | 1 | Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-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 | 134362 | None | 0 | Human | Functional | pEC50 | = | 9.6 | 9.6 | - | 1 | Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-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 | 134413 | None | 0 | Human | Functional | pEC50 | = | 9.6 | 9.6 | - | 1 | Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-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 | 134413 | None | 0 | Human | Functional | pEC50 | = | 9.6 | 9.6 | - | 1 | Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-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 | 134583 | None | 0 | Human | Functional | pEC50 | = | 9.6 | 9.6 | - | 1 | Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-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 | 134583 | None | 0 | Human | Functional | pEC50 | = | 9.6 | 9.6 | - | 1 | Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-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 | 134872 | None | 0 | Human | Functional | pEC50 | = | 9.6 | 9.6 | - | 1 | Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-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 | 134872 | None | 0 | Human | Functional | pEC50 | = | 9.6 | 9.6 | - | 1 | Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-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 | 134088 | None | 0 | Human | Functional | pEC50 | = | 9.6 | 9.6 | - | 1 | Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-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 | 134088 | None | 0 | Human | Functional | pEC50 | = | 9.6 | 9.6 | - | 1 | Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-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 | 134528 | None | 0 | Human | Functional | pEC50 | = | 9.6 | 9.6 | - | 1 | Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-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 | 134528 | None | 0 | Human | Functional | pEC50 | = | 9.6 | 9.6 | - | 1 | Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-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 | 134827 | None | 0 | Human | Functional | pEC50 | = | 9.6 | 9.6 | - | 1 | Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-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 | 134827 | None | 0 | Human | Functional | pEC50 | = | 9.6 | 9.6 | - | 1 | Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-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 | 134854 | None | 0 | Human | Functional | pEC50 | = | 9.6 | 9.6 | - | 1 | Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-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 | 134854 | None | 0 | Human | Functional | pEC50 | = | 9.6 | 9.6 | - | 1 | Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-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 | 134553 | None | 0 | Human | Functional | pEC50 | = | 9.6 | 9.6 | - | 1 | Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-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 | 134553 | None | 0 | Human | Functional | pEC50 | = | 9.6 | 9.6 | - | 1 | Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-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 | 133880 | None | 0 | Human | Functional | pEC50 | = | 9.5 | 9.5 | - | 1 | Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-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 | 133880 | None | 0 | Human | Functional | pEC50 | = | 9.5 | 9.5 | - | 1 | Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-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 | 134066 | None | 0 | Human | Functional | pEC50 | = | 9.5 | 9.5 | - | 1 | Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-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 | 134066 | None | 0 | Human | Functional | pEC50 | = | 9.5 | 9.5 | - | 1 | Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-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 | 133783 | None | 0 | Human | Functional | pEC50 | = | 9.5 | 9.5 | - | 1 | Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-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 | 133783 | None | 0 | Human | Functional | pEC50 | = | 9.5 | 9.5 | - | 1 | Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-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 | 134615 | None | 0 | Human | Functional | pEC50 | = | 9.5 | 9.5 | - | 1 | Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-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 | 134615 | None | 0 | Human | Functional | pEC50 | = | 9.5 | 9.5 | - | 1 | Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-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 | 133719 | None | 0 | Human | Functional | pEC50 | = | 9.5 | 9.5 | - | 1 | Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-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 | 133719 | None | 0 | Human | Functional | pEC50 | = | 9.5 | 9.5 | - | 1 | Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-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 | 134005 | None | 0 | Human | Functional | pEC50 | = | 9.5 | 9.5 | - | 1 | Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-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 | 134005 | None | 0 | Human | Functional | pEC50 | = | 9.5 | 9.5 | - | 1 | Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-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 | 134884 | None | 0 | Human | Functional | pEC50 | = | 9.5 | 9.5 | - | 1 | Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-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 | 134884 | None | 0 | Human | Functional | pEC50 | = | 9.5 | 9.5 | - | 1 | Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-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 | 134003 | None | 3 | Human | Functional | pEC50 | = | 9.5 | 9.5 | - | 1 | Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-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 | 134003 | None | 3 | Human | Functional | pEC50 | = | 9.5 | 9.5 | - | 1 | Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-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 | 134096 | None | 0 | Human | Functional | pEC50 | = | 9.5 | 9.5 | - | 1 | Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-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 | 134096 | None | 0 | Human | Functional | pEC50 | = | 9.5 | 9.5 | - | 1 | Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-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 | 134462 | None | 0 | Human | Functional | pEC50 | = | 9.5 | 9.5 | - | 1 | Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-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 | 134462 | None | 0 | Human | Functional | pEC50 | = | 9.5 | 9.5 | - | 1 | Antagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-Phe(4-F)-Pro-Gly-Trp-Leu-Val-Lys-Asn-Gly-NH2-induced intracellular calcium mobilization incubated for 30 mins by FLIPR assayAntagonist activity against human PAR4 expressed in HEK293 cells assessed as reduction in H-Ala-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 | ||
Showing 1 to 50 of 2,148 entries
| Ligands (move mouse cursor over ligand name to see structure) | Receptor | Activity | Chemical information | |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Sel. page | Common name
| GPCRdb ID
| Reference ligand
| Vendors | Species
| Assay Type
| Activity Type
| Activity Relation
| Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description
| Source
| Mol weight | Rot Bonds | H don | H acc | LogP | Smiles
| DOI
| |
Ligands (move mouse cursor over ligand name to see structure)
| Receptor
| Activity
| Chemical information
| |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Sel. page | Common name
| GPCRdb ID
| Reference ligand
| Vendors | Species
| Assay Type
| Activity Type
| Activity Relation
| Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description
| Source
| Mol weight | Rot Bonds | H don | H acc | LogP | Smiles
| DOI
| |
| 71769562 | 134003 | None | 3 | Human | Binding | pIC50 | = | 10.6 | 10.6 | - | 0 | 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 | 134003 | None | 3 | Human | Binding | pIC50 | = | 10.6 | 10.6 | - | 0 | 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 | 147775 | None | 0 | Human | Binding | pIC50 | = | 8.8 | 8.8 | - | 0 | 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 | 147775 | None | 0 | Human | Binding | pIC50 | = | 8.8 | 8.8 | - | 0 | 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 | 185961 | None | 0 | Mouse | Binding | pIC50 | = | 6 | 6.0 | - | 0 | Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity 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 | 185961 | None | 0 | Mouse | Binding | pIC50 | = | 6 | 6.0 | - | 0 | Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity 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 | 148002 | None | 0 | Human | Binding | pIC50 | = | 6 | 6.0 | - | 0 | 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 | 148002 | None | 0 | Human | Binding | pIC50 | = | 6 | 6.0 | - | 0 | 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 | 148002 | None | 0 | Human | Binding | pIC50 | = | 6 | 6.0 | - | 0 | 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 | 148002 | None | 0 | Human | Binding | pIC50 | = | 6 | 6.0 | - | 0 | 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 | 136220 | None | 0 | Human | Binding | pIC50 | = | 6 | 6.0 | - | 0 | 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 | 136220 | None | 0 | Human | Binding | pIC50 | = | 6 | 6.0 | - | 0 | 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 | 184484 | None | 0 | Mouse | Binding | pIC50 | = | 5 | 5.0 | - | 0 | Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity 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 | 184484 | None | 0 | Mouse | Binding | pIC50 | = | 5 | 5.0 | - | 0 | Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity 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 | 185364 | None | 0 | Mouse | Binding | pIC50 | = | 5 | 5.0 | - | 0 | Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity 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 | 185364 | None | 0 | Mouse | Binding | pIC50 | = | 5 | 5.0 | - | 0 | Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity 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 | 114547 | None | 0 | Human | Binding | pIC50 | = | 5 | 5.0 | - | 0 | 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 | 114547 | None | 0 | Human | Binding | pIC50 | = | 5 | 5.0 | - | 0 | 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 | 135397 | None | 0 | Human | Binding | pIC50 | = | 5 | 5.0 | - | 0 | 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 | 135397 | None | 0 | Human | Binding | pIC50 | = | 5 | 5.0 | - | 0 | 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 | 186197 | None | 0 | Mouse | Binding | pIC50 | = | 6.0 | 6.0 | - | 0 | Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity 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 | 186197 | None | 0 | Mouse | Binding | pIC50 | = | 6.0 | 6.0 | - | 0 | Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity 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 | 144082 | None | 0 | Human | Binding | pIC50 | = | 6.0 | 6.0 | - | 0 | 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 | 144082 | None | 0 | Human | Binding | pIC50 | = | 6.0 | 6.0 | - | 0 | 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 | 144082 | None | 0 | Human | Binding | pIC50 | = | 6.0 | 6.0 | - | 0 | 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 | 144082 | None | 0 | Human | Binding | pIC50 | = | 6.0 | 6.0 | - | 0 | 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 | 144503 | None | 0 | Human | Binding | pIC50 | = | 8.0 | 8.0 | - | 0 | 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 | 144503 | None | 0 | Human | Binding | pIC50 | = | 8.0 | 8.0 | - | 0 | 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 | 185885 | None | 0 | Mouse | Binding | pIC50 | = | 7.0 | 7.0 | - | 0 | Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity 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 | 185885 | None | 0 | Mouse | Binding | pIC50 | = | 7.0 | 7.0 | - | 0 | Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity 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 | 135546 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | 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 | 135546 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | 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 | 170064 | None | 0 | Human | Binding | pIC50 | = | 5.9 | 5.9 | - | 0 | 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 | 170064 | None | 0 | Human | Binding | pIC50 | = | 5.9 | 5.9 | - | 0 | 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 | 149938 | None | 0 | Human | Binding | pIC50 | = | 5.9 | 5.9 | - | 0 | Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of 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 | 149938 | None | 0 | Human | Binding | pIC50 | = | 5.9 | 5.9 | - | 0 | Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of 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 | 149938 | None | 0 | Human | Binding | pIC50 | = | 5.9 | 5.9 | - | 0 | Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of 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 | 149938 | None | 0 | Human | Binding | pIC50 | = | 5.9 | 5.9 | - | 0 | Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of 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 | 185427 | None | 0 | Mouse | Binding | pIC50 | = | 5.9 | 5.9 | - | 0 | Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity 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 | 185427 | None | 0 | Mouse | Binding | pIC50 | = | 5.9 | 5.9 | - | 0 | Antagonist activity at PAR4 in ICR mouse platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assayAntagonist activity 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 | 151651 | None | 0 | Human | Binding | pIC50 | = | 5.9 | 5.9 | - | 0 | Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of 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 | 151651 | None | 0 | Human | Binding | pIC50 | = | 5.9 | 5.9 | - | 0 | Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysisAntagonist activity at PAR4 in human platelets assessed as inhibition of 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 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | 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 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | 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 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | 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 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | 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 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | 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 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | 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 | 169899 | None | 0 | Human | Binding | pIC50 | = | 5.9 | 5.9 | - | 0 | 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 | 169899 | None | 0 | Human | Binding | pIC50 | = | 5.9 | 5.9 | - | 0 | 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 | ||
Showing 1 to 50 of 478 entries