Assay Detail
Binding
CHEMBL813561
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Inhibitory activity against thrombin.
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Unique overlap in the prerequisites for thrombin inhibition and oral bioavailability resulting in potent oral antithrombotics.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 28 | 8.61 | 9.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL140078 | — | — | 1 | 9.85 |
| CHEMBL343794 | — | — | 1 | 9.68 |
| CHEMBL139051 | — | — | 1 | 9.54 |
| CHEMBL337780 | — | — | 1 | 9.54 |
| CHEMBL2370858 | — | — | 1 | 9.52 |
| CHEMBL336229 | — | — | 1 | 9.48 |
| CHEMBL341581 | — | — | 1 | 9.38 |
| CHEMBL138267 | — | — | 1 | 9.30 |
| CHEMBL139359 | — | — | 1 | 9.09 |
| CHEMBL343804 | — | — | 1 | 9.08 |
| CHEMBL342672 | CYCLOTHEONAMIDE A | — | 1 | 9.00 |
| CHEMBL139242 | — | — | 1 | 8.96 |
| CHEMBL139280 | — | — | 1 | 8.85 |
| CHEMBL266349 | MELAGATRAN | 4.0 | 1 | 8.70 |
| CHEMBL344916 | — | — | 1 | 8.70 |
| CHEMBL137945 | — | — | 1 | 8.59 |
| CHEMBL336048 | — | — | 1 | 8.46 |
| CHEMBL446372 | — | — | 1 | 7.89 |
| CHEMBL138986 | — | — | 1 | 7.82 |
| CHEMBL1166 | ARGATROBAN | 4.0 | 1 | 7.72 |
| CHEMBL141724 | — | — | 1 | 7.55 |
| CHEMBL342850 | — | — | 1 | 6.84 |
| CHEMBL342632 | — | — | 1 | 6.69 |
| CHEMBL136164 | — | — | 1 | 6.42 |
| CHEMBL139119 | — | — | 1 | - |
| CHEMBL139247 | — | — | 1 | - |
| CHEMBL334701 | — | — | 1 | - |
| CHEMBL138664 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL140078 | — | Ki | = | 0.14 | nM | 9.85 |
| CHEMBL343794 | — | Ki | = | 0.21 | nM | 9.68 |
| CHEMBL139051 | — | Ki | = | 0.29 | nM | 9.54 |
| CHEMBL337780 | — | Ki | = | 0.29 | nM | 9.54 |
| CHEMBL2370858 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL336229 | — | Ki | = | 0.33 | nM | 9.48 |
| CHEMBL341581 | — | Ki | = | 0.42 | nM | 9.38 |
| CHEMBL138267 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL139359 | — | Ki | = | 0.82 | nM | 9.09 |
| CHEMBL343804 | — | Ki | = | 0.84 | nM | 9.08 |
| CHEMBL342672 | CYCLOTHEONAMIDE A | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL139242 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL139280 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL266349 | MELAGATRAN | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL344916 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL137945 | — | Ki | = | 2.6 | nM | 8.59 |
| CHEMBL336048 | — | Ki | = | 3.5 | nM | 8.46 |
| CHEMBL446372 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL138986 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL1166 | ARGATROBAN | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL141724 | — | Ki | = | 28.0 | nM | 7.55 |
| CHEMBL342850 | — | Ki | = | 146.0 | nM | 6.84 |
| CHEMBL342632 | — | Ki | = | 204.0 | nM | 6.69 |
| CHEMBL136164 | — | Ki | = | 376.0 | nM | 6.42 |
| CHEMBL139119 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL139247 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL334701 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL138664 | — | Ki | > | 1000.0 | nM | - |