Assay Detail
Binding
CHEMBL3119469
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Competitive inhibition of human APC using S-2366 as substrate
16
Total Activities
16
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 |
|---|---|---|---|
| Ki | 16 | 6.45 | 7.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3115901 | — | — | 1 | 7.40 |
| CHEMBL3115900 | — | — | 1 | 7.00 |
| CHEMBL3115904 | — | — | 1 | 7.00 |
| CHEMBL3115897 | — | — | 1 | 6.70 |
| CHEMBL3115903 | — | — | 1 | 6.52 |
| CHEMBL3115899 | — | — | 1 | 6.52 |
| CHEMBL3115898 | — | — | 1 | 6.52 |
| CHEMBL3115894 | — | — | 1 | 6.52 |
| CHEMBL3115893 | — | — | 1 | 6.40 |
| CHEMBL3115905 | — | — | 1 | 6.30 |
| CHEMBL215295 | — | — | 1 | 6.30 |
| CHEMBL3115906 | — | — | 1 | 6.10 |
| CHEMBL3115896 | — | — | 1 | 6.05 |
| CHEMBL3115892 | — | — | 1 | 6.05 |
| CHEMBL3115902 | — | — | 1 | 5.96 |
| CHEMBL3115907 | — | — | 1 | 5.80 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3115901 | — | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL3115900 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL3115904 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL3115897 | — | Ki | = | 200.0 | nM | 6.70 |
| CHEMBL3115903 | — | Ki | = | 300.0 | nM | 6.52 |
| CHEMBL3115899 | — | Ki | = | 300.0 | nM | 6.52 |
| CHEMBL3115898 | — | Ki | = | 300.0 | nM | 6.52 |
| CHEMBL3115894 | — | Ki | = | 300.0 | nM | 6.52 |
| CHEMBL3115893 | — | Ki | = | 400.0 | nM | 6.40 |
| CHEMBL3115905 | — | Ki | = | 500.0 | nM | 6.30 |
| CHEMBL215295 | — | Ki | = | 500.0 | nM | 6.30 |
| CHEMBL3115906 | — | Ki | = | 800.0 | nM | 6.10 |
| CHEMBL3115896 | — | Ki | = | 900.0 | nM | 6.05 |
| CHEMBL3115892 | — | Ki | = | 900.0 | nM | 6.05 |
| CHEMBL3115902 | — | Ki | = | 1100.0 | nM | 5.96 |
| CHEMBL3115907 | — | Ki | = | 1600.0 | nM | 5.80 |