Assay Detail
Binding
CHEMBL964660
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Displacement of [3H]haTRAP from PAR1 in human platelets
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of a novel, orally active himbacine-based thrombin receptor antagonist (SCH 530348) with potent antiplatelet activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 24 | 7.96 | 8.74 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL442649 | — | — | 1 | 8.74 |
| CHEMBL453277 | — | — | 1 | 8.43 |
| CHEMBL500551 | — | — | 1 | 8.39 |
| CHEMBL493633 | — | — | 1 | 8.36 |
| CHEMBL523854 | — | — | 1 | 8.32 |
| CHEMBL458264 | — | — | 1 | 8.23 |
| CHEMBL446344 | — | — | 1 | 8.23 |
| CHEMBL493983 | — | — | 1 | 8.21 |
| CHEMBL493632 | — | — | 1 | 8.21 |
| CHEMBL494618 | — | — | 1 | 8.19 |
| CHEMBL493792 | — | — | 1 | 8.19 |
| CHEMBL493982 | VORAPAXAR | 4.0 | 1 | 8.09 |
| CHEMBL447996 | — | — | 1 | 8.00 |
| CHEMBL495422 | — | — | 1 | 7.96 |
| CHEMBL521531 | — | — | 1 | 7.96 |
| CHEMBL493975 | — | — | 1 | 7.96 |
| CHEMBL507697 | — | — | 1 | 7.96 |
| CHEMBL449425 | — | — | 1 | 7.89 |
| CHEMBL494816 | — | — | 1 | 7.77 |
| CHEMBL498785 | — | — | 1 | 7.70 |
| CHEMBL447913 | — | — | 1 | 7.52 |
| CHEMBL455020 | — | — | 1 | 7.36 |
| CHEMBL506808 | — | — | 1 | 7.05 |
| CHEMBL460583 | — | — | 1 | 6.43 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL442649 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL453277 | — | Ki | = | 3.7 | nM | 8.43 |
| CHEMBL500551 | — | Ki | = | 4.1 | nM | 8.39 |
| CHEMBL493633 | — | Ki | = | 4.4 | nM | 8.36 |
| CHEMBL523854 | — | Ki | = | 4.8 | nM | 8.32 |
| CHEMBL458264 | — | Ki | = | 5.9 | nM | 8.23 |
| CHEMBL446344 | — | Ki | = | 5.9 | nM | 8.23 |
| CHEMBL493983 | — | Ki | = | 6.1 | nM | 8.21 |
| CHEMBL493632 | — | Ki | = | 6.2 | nM | 8.21 |
| CHEMBL494618 | — | Ki | = | 6.5 | nM | 8.19 |
| CHEMBL493792 | — | Ki | = | 6.4 | nM | 8.19 |
| CHEMBL493982 | VORAPAXAR | Ki | = | 8.1 | nM | 8.09 |
| CHEMBL447996 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL495422 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL521531 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL493975 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL507697 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL449425 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL494816 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL498785 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL447913 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL455020 | — | Ki | = | 44.0 | nM | 7.36 |
| CHEMBL506808 | — | Ki | = | 89.0 | nM | 7.05 |
| CHEMBL460583 | — | Ki | = | 367.0 | nM | 6.43 |