Assay Detail
Binding
CHEMBL879195
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Inhibition of human alpha-thrombin.
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Potent thrombin inhibitors that probe the S1 subsite: tripeptide transition state analogues based on a heterocycle-activated carbonyl group.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 14 | 7.50 | 9.72 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL270437 | — | — | 1 | 9.72 |
| CHEMBL102121 | — | — | 1 | 8.47 |
| CHEMBL322205 | — | — | 1 | 8.44 |
| CHEMBL105584 | — | — | 1 | 8.42 |
| CHEMBL256381 | — | — | 1 | 8.09 |
| CHEMBL273196 | EFEGATRAN | 2.0 | 1 | 8.00 |
| CHEMBL1166 | ARGATROBAN | 4.0 | 1 | 8.00 |
| CHEMBL101855 | — | — | 1 | 7.92 |
| CHEMBL102919 | — | — | 1 | 7.82 |
| CHEMBL272931 | — | — | 1 | 7.30 |
| CHEMBL404728 | — | — | 1 | 7.07 |
| CHEMBL256591 | — | — | 1 | 5.62 |
| CHEMBL319615 | — | — | 1 | 5.28 |
| CHEMBL322444 | — | — | 1 | 4.80 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL270437 | — | Ki | = | 0.19 | nM | 9.72 |
| CHEMBL102121 | — | Ki | = | 3.4 | nM | 8.47 |
| CHEMBL322205 | — | Ki | = | 3.6 | nM | 8.44 |
| CHEMBL105584 | — | Ki | = | 3.8 | nM | 8.42 |
| CHEMBL256381 | — | Ki | = | 8.1 | nM | 8.09 |
| CHEMBL273196 | EFEGATRAN | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL1166 | ARGATROBAN | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL101855 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL102919 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL272931 | — | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL404728 | — | Ki | = | 85.0 | nM | 7.07 |
| CHEMBL256591 | — | Ki | = | 2400.0 | nM | 5.62 |
| CHEMBL319615 | — | Ki | = | 5300.0 | nM | 5.28 |
| CHEMBL322444 | — | Ki | = | 16000.0 | nM | 4.80 |