Assay Detail
Functional
CHEMBL1010177
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antithrombotic activity against iv dosed rabbit arterio-venous shunt model assessed as inhibition of thrombus formation
12
Total Activities
6
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Oryctolagus cuniculus |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Highly efficacious factor Xa inhibitors containing alpha-substituted phenylcycloalkyl P4 moieties.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 6 | 7.02 | 7.54 |
| ID50 | 6 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL453208 | — | — | 2 | 7.54 |
| CHEMBL518253 | — | — | 2 | 7.33 |
| CHEMBL446752 | — | — | 2 | 7.17 |
| CHEMBL445335 | — | — | 2 | 7.09 |
| CHEMBL231779 | APIXABAN | 4.0 | 2 | 6.49 |
| CHEMBL206335 | RAZAXABAN | 2.0 | 2 | 6.47 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL453208 | — | EC50 | = | 29.0 | nM | 7.54 |
| CHEMBL518253 | — | EC50 | = | 47.0 | nM | 7.33 |
| CHEMBL446752 | — | EC50 | = | 68.0 | nM | 7.17 |
| CHEMBL445335 | — | EC50 | = | 81.0 | nM | 7.09 |
| CHEMBL231779 | APIXABAN | EC50 | = | 325.0 | nM | 6.49 |
| CHEMBL206335 | RAZAXABAN | EC50 | = | 340.0 | nM | 6.47 |
| CHEMBL518253 | — | ID50 | = | 0.27 | umol/kg/hr | - |
| CHEMBL453208 | — | ID50 | = | 0.08 | umol/kg/hr | - |
| CHEMBL446752 | — | ID50 | = | 0.19 | umol/kg/hr | - |
| CHEMBL445335 | — | ID50 | = | 0.16 | umol/kg/hr | - |
| CHEMBL206335 | RAZAXABAN | ID50 | = | 1.6 | umol/kg/hr | - |
| CHEMBL231779 | APIXABAN | ID50 | = | 0.57 | umol/kg/hr | - |