Assay Detail
Functional
CHEMBL4843848
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at PAR4 in human platelet-rich plasma assessed as inhibition of PAR4 AP AYPGKF-NH2-induced platelet aggregation by photo-turbidimetry assay
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Tissue | Plasma |
| Cell Type | Platelet |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis and evaluation of novel and potent protease activated receptor 4 (PAR4) antagonists based on a quinazolin-4(3H)-one scaffold.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 7.57 | 8.47 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3716552 | BMS-986141 | 2.0 | 1 | 8.47 |
| CHEMBL4855875 | — | — | 1 | 8.18 |
| CHEMBL3716726 | — | — | 1 | 8.01 |
| CHEMBL4860533 | — | — | 1 | 7.71 |
| CHEMBL4866566 | — | — | 1 | 7.54 |
| CHEMBL4849569 | — | — | 1 | 7.40 |
| CHEMBL4871001 | — | — | 1 | 7.11 |
| CHEMBL4870185 | — | — | 1 | 6.97 |
| CHEMBL4859532 | — | — | 1 | 6.76 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3716552 | BMS-986141 | IC50 | = | 3.35 | nM | 8.47 |
| CHEMBL4855875 | — | IC50 | = | 6.59 | nM | 8.18 |
| CHEMBL3716726 | — | IC50 | = | 9.7 | nM | 8.01 |
| CHEMBL4860533 | — | IC50 | = | 19.6 | nM | 7.71 |
| CHEMBL4866566 | — | IC50 | = | 28.5 | nM | 7.54 |
| CHEMBL4849569 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL4871001 | — | IC50 | = | 77.8 | nM | 7.11 |
| CHEMBL4870185 | — | IC50 | = | 106.7 | nM | 6.97 |
| CHEMBL4859532 | — | IC50 | = | 174.0 | nM | 6.76 |