Assay Detail
Functional
CHEMBL869244
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Antithrombotic activity in rabbit arterio-venous shunt thrombosis model
8
Total Activities
8
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Oryctolagus cuniculus |
| Confidence | 1 — Organism |
| Curated By | Expert |
Publication
1-[3-Aminobenzisoxazol-5'-yl]-3-trifluoromethyl-6-[2'-(3-(R)-hydroxy-N-pyrrolidinyl)methyl-[1,1']-biphen-4-yl]-1,4,5,6-tetrahydropyrazolo-[3,4-c]-pyridin-7-one (BMS-740808) a highly potent, selective, efficacious, and orally bioavailable inhibitor of blood coagulation factor Xa.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 6.39 | 6.87 |
| ID50 | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL378093 | — | — | 1 | 6.87 |
| CHEMBL211410 | — | — | 1 | 6.65 |
| CHEMBL206335 | RAZAXABAN | 2.0 | 1 | 6.47 |
| CHEMBL213888 | — | — | 1 | 6.29 |
| CHEMBL263767 | — | — | 1 | 6.22 |
| CHEMBL436791 | — | — | 1 | 6.22 |
| CHEMBL402881 | — | — | 1 | 6.00 |
| CHEMBL380405 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL378093 | — | IC50 | = | 135.0 | nM | 6.87 |
| CHEMBL211410 | — | IC50 | = | 223.0 | nM | 6.65 |
| CHEMBL206335 | RAZAXABAN | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL213888 | — | IC50 | = | 510.0 | nM | 6.29 |
| CHEMBL263767 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL436791 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL402881 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL380405 | — | ID50 | = | 0.6 | ug/hr.kg | - |