Assay Detail
Functional
CHEMBL3721140
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity against PAR4 in human platelet rich plasma assessed as inhibition of gamma-thrombin-induced platelet aggregation pre-incubated for 5 mins before gamma-thrombin addition by microplate aggregation assay
68
Total Activities
68
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Tissue | Plasma |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Imidazothiadiazole and imidazopyrazine derivatives as protease activated receptor 4 (par4) inhibitors for treating platelet aggregation
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 68 | 7.69 | 9.03 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3715367 | — | — | 1 | 9.03 |
| CHEMBL3717746 | — | — | 1 | 9.02 |
| CHEMBL3719256 | — | — | 1 | 9.00 |
| CHEMBL3716096 | — | — | 1 | 8.92 |
| CHEMBL3715516 | — | — | 1 | 8.80 |
| CHEMBL3717956 | — | — | 1 | 8.80 |
| CHEMBL3717885 | — | — | 1 | 8.72 |
| CHEMBL3716904 | — | — | 1 | 8.72 |
| CHEMBL3718360 | — | — | 1 | 8.72 |
| CHEMBL3716160 | — | — | 1 | 8.72 |
| CHEMBL3719253 | — | — | 1 | 8.70 |
| CHEMBL3719060 | — | — | 1 | 8.70 |
| CHEMBL3715025 | — | — | 1 | 8.70 |
| CHEMBL3716552 | BMS-986141 | 2.0 | 1 | 8.68 |
| CHEMBL3718433 | — | — | 1 | 8.68 |
| CHEMBL3714941 | — | — | 1 | 8.66 |
| CHEMBL3715600 | — | — | 1 | 8.44 |
| CHEMBL3715848 | — | — | 1 | 8.33 |
| CHEMBL3718927 | — | — | 1 | 8.24 |
| CHEMBL3716726 | — | — | 1 | 8.12 |
| CHEMBL3716230 | — | — | 1 | 7.64 |
| CHEMBL3716754 | — | — | 1 | 7.64 |
| CHEMBL3717259 | — | — | 1 | 7.64 |
| CHEMBL3714842 | — | — | 1 | 7.62 |
| CHEMBL3716197 | — | — | 1 | 7.62 |
| CHEMBL3716623 | — | — | 1 | 7.60 |
| CHEMBL3716644 | — | — | 1 | 7.60 |
| CHEMBL3716372 | — | — | 1 | 7.58 |
| CHEMBL3718490 | — | — | 1 | 7.58 |
| CHEMBL3718707 | — | — | 1 | 7.57 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3715367 | — | IC50 | = | 0.94 | nM | 9.03 |
| CHEMBL3717746 | — | IC50 | = | 0.96 | nM | 9.02 |
| CHEMBL3719256 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3716096 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL3715516 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL3717956 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL3717885 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL3716904 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL3718360 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL3716160 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL3719253 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3719060 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3715025 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3718433 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL3716552 | BMS-986141 | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL3714941 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL3715600 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL3715848 | — | IC50 | = | 4.7 | nM | 8.33 |
| CHEMBL3718927 | — | IC50 | = | 5.7 | nM | 8.24 |
| CHEMBL3716726 | — | IC50 | = | 7.6 | nM | 8.12 |
| CHEMBL3716230 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL3716754 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL3717259 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL3714842 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL3716197 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL3716623 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL3716644 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL3716372 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL3718490 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL3718707 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL3717972 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL3719223 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL3718639 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL3715685 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL3718626 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL3715391 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL3715578 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL3718657 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL3718382 | — | IC50 | = | 156.0 | nM | 6.81 |
| CHEMBL3718116 | — | IC50 | = | 2034.0 | nM | 5.69 |
| CHEMBL3715692 | — | IC50 | = | 2338.0 | nM | 5.63 |
| CHEMBL3714991 | — | IC50 | = | 2359.0 | nM | 5.63 |
| CHEMBL3717789 | — | IC50 | = | 2324.0 | nM | 5.63 |
| CHEMBL3715686 | — | IC50 | = | 2382.0 | nM | 5.62 |
| CHEMBL3718007 | — | IC50 | = | 2632.0 | nM | 5.58 |
| CHEMBL3715728 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL3717529 | — | IC50 | = | 3132.0 | nM | 5.50 |
| CHEMBL3716173 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL3718893 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL3718695 | — | IC50 | > | 3000.0 | nM | - |