Assay Detail
Binding
CHEMBL3119477
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human coagulation factor 10a using S-2765 as substrate preincubated for 300 seconds followed by substrate addition measured after 40 mins by spectrophotometric analysis
6
Total Activities
6
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
Design, synthesis, and SAR of a series of activated protein C (APC) inhibitors with selectivity against thrombin for the treatment of haemophilia.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 4.51 | 4.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL266349 | MELAGATRAN | 4.0 | 1 | 4.68 |
| CHEMBL3115900 | — | — | 1 | 4.64 |
| CHEMBL3115903 | — | — | 1 | 4.38 |
| CHEMBL215295 | — | — | 1 | 4.32 |
| CHEMBL3115901 | — | — | 1 | - |
| CHEMBL3115894 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL266349 | MELAGATRAN | IC50 | = | 21000.0 | nM | 4.68 |
| CHEMBL3115900 | — | IC50 | = | 23000.0 | nM | 4.64 |
| CHEMBL3115903 | — | IC50 | = | 42000.0 | nM | 4.38 |
| CHEMBL215295 | — | IC50 | = | 48000.0 | nM | 4.32 |
| CHEMBL3115901 | — | IC50 | > | 44000.0 | nM | - |
| CHEMBL3115894 | — | IC50 | > | 130000.0 | nM | - |