Assay Detail
Functional
CHEMBL4843850
Review assay metadata, readout intent, target linkage, and publication context from the same page.
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 assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| 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 | 6 | 8.71 | 9.28 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4860533 | — | — | 1 | 9.28 |
| CHEMBL3716726 | — | — | 1 | 9.15 |
| CHEMBL4855875 | — | — | 1 | 8.92 |
| CHEMBL4871001 | — | — | 1 | 8.49 |
| CHEMBL4866566 | — | — | 1 | 8.24 |
| CHEMBL4849569 | — | — | 1 | 8.17 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4860533 | — | IC50 | = | 0.53 | nM | 9.28 |
| CHEMBL3716726 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL4855875 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL4871001 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL4866566 | — | IC50 | = | 5.7 | nM | 8.24 |
| CHEMBL4849569 | — | IC50 | = | 6.8 | nM | 8.17 |