Assay Detail
Binding
CHEMBL865059
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Inhibition of thrombin
28
Total Activities
28
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
Orally active thrombin inhibitors. Part 1: optimization of the P1-moiety.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 28 | 7.58 | 9.01 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL208140 | — | — | 1 | 9.01 |
| CHEMBL377681 | — | — | 1 | 9.00 |
| CHEMBL206205 | — | — | 1 | 8.89 |
| CHEMBL381709 | — | — | 1 | 8.86 |
| CHEMBL206418 | — | — | 1 | 8.78 |
| CHEMBL207981 | — | — | 1 | 8.75 |
| CHEMBL382843 | — | — | 1 | 8.67 |
| CHEMBL207770 | — | — | 1 | 8.57 |
| CHEMBL208494 | — | — | 1 | 8.37 |
| CHEMBL207129 | — | — | 1 | 8.21 |
| CHEMBL208394 | — | — | 1 | 8.19 |
| CHEMBL427037 | — | — | 1 | 8.01 |
| CHEMBL207128 | — | — | 1 | 7.95 |
| CHEMBL379258 | — | — | 1 | 7.68 |
| CHEMBL207590 | — | — | 1 | 7.47 |
| CHEMBL206841 | — | — | 1 | 7.36 |
| CHEMBL207568 | — | — | 1 | 7.31 |
| CHEMBL207271 | — | — | 1 | 7.29 |
| CHEMBL382145 | — | — | 1 | 7.29 |
| CHEMBL206963 | — | — | 1 | 7.24 |
| CHEMBL266349 | MELAGATRAN | 4.0 | 1 | 7.16 |
| CHEMBL207966 | — | — | 1 | 6.63 |
| CHEMBL377667 | — | — | 1 | 6.25 |
| CHEMBL207813 | — | — | 1 | 5.99 |
| CHEMBL207184 | — | — | 1 | 5.97 |
| CHEMBL206473 | — | — | 1 | 5.86 |
| CHEMBL207441 | — | — | 1 | 5.84 |
| CHEMBL207337 | — | — | 1 | 5.56 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL208140 | — | IC50 | = | 0.98 | nM | 9.01 |
| CHEMBL377681 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL206205 | — | IC50 | = | 1.29 | nM | 8.89 |
| CHEMBL381709 | — | IC50 | = | 1.39 | nM | 8.86 |
| CHEMBL206418 | — | IC50 | = | 1.68 | nM | 8.78 |
| CHEMBL207981 | — | IC50 | = | 1.76 | nM | 8.75 |
| CHEMBL382843 | — | IC50 | = | 2.15 | nM | 8.67 |
| CHEMBL207770 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL208494 | — | IC50 | = | 4.28 | nM | 8.37 |
| CHEMBL207129 | — | IC50 | = | 6.2 | nM | 8.21 |
| CHEMBL208394 | — | IC50 | = | 6.4 | nM | 8.19 |
| CHEMBL427037 | — | IC50 | = | 9.88 | nM | 8.01 |
| CHEMBL207128 | — | IC50 | = | 11.2 | nM | 7.95 |
| CHEMBL379258 | — | IC50 | = | 20.8 | nM | 7.68 |
| CHEMBL207590 | — | IC50 | = | 33.9 | nM | 7.47 |
| CHEMBL206841 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL207568 | — | IC50 | = | 49.1 | nM | 7.31 |
| CHEMBL207271 | — | IC50 | = | 51.2 | nM | 7.29 |
| CHEMBL382145 | — | IC50 | = | 50.9 | nM | 7.29 |
| CHEMBL206963 | — | IC50 | = | 57.4 | nM | 7.24 |
| CHEMBL266349 | MELAGATRAN | IC50 | = | 69.2 | nM | 7.16 |
| CHEMBL207966 | — | IC50 | = | 232.0 | nM | 6.63 |
| CHEMBL377667 | — | IC50 | = | 566.0 | nM | 6.25 |
| CHEMBL207813 | — | IC50 | = | 1020.0 | nM | 5.99 |
| CHEMBL207184 | — | IC50 | = | 1080.0 | nM | 5.97 |
| CHEMBL206473 | — | IC50 | = | 1370.0 | nM | 5.86 |
| CHEMBL207441 | — | IC50 | = | 1430.0 | nM | 5.84 |
| CHEMBL207337 | — | IC50 | = | 2780.0 | nM | 5.56 |