Assay Detail
Binding
CHEMBL870018
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of thrombin by chromogenic assay
25
Total Activities
25
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 2: optimization of the P2-moiety.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 25 | 7.49 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL377303 | — | — | 1 | 9.00 |
| CHEMBL208140 | — | — | 1 | 9.00 |
| CHEMBL206418 | — | — | 1 | 8.77 |
| CHEMBL3559601 | — | — | 1 | 8.77 |
| CHEMBL377681 | — | — | 1 | 8.74 |
| CHEMBL207187 | — | — | 1 | 8.57 |
| CHEMBL206891 | — | — | 1 | 8.49 |
| CHEMBL208055 | — | — | 1 | 8.47 |
| CHEMBL383314 | — | — | 1 | 7.83 |
| CHEMBL377132 | — | — | 1 | 7.80 |
| CHEMBL208262 | — | — | 1 | 7.70 |
| CHEMBL208474 | — | — | 1 | 7.50 |
| CHEMBL205766 | — | — | 1 | 7.36 |
| CHEMBL207788 | — | — | 1 | 7.33 |
| CHEMBL377056 | — | — | 1 | 7.25 |
| CHEMBL379920 | — | — | 1 | 7.23 |
| CHEMBL266349 | MELAGATRAN | 4.0 | 1 | 7.16 |
| CHEMBL207836 | — | — | 1 | 7.15 |
| CHEMBL208190 | — | — | 1 | 7.12 |
| CHEMBL208137 | — | — | 1 | 6.99 |
| CHEMBL208306 | — | — | 1 | 6.54 |
| CHEMBL207603 | — | — | 1 | 6.54 |
| CHEMBL204468 | — | — | 1 | 6.24 |
| CHEMBL207564 | — | — | 1 | 5.39 |
| CHEMBL378185 | — | — | 1 | 4.27 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL377303 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL208140 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL206418 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL3559601 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL377681 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL207187 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL206891 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL208055 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL383314 | — | IC50 | = | 14.8 | nM | 7.83 |
| CHEMBL377132 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL208262 | — | IC50 | = | 20.2 | nM | 7.70 |
| CHEMBL208474 | — | IC50 | = | 31.9 | nM | 7.50 |
| CHEMBL205766 | — | IC50 | = | 44.2 | nM | 7.36 |
| CHEMBL207788 | — | IC50 | = | 47.3 | nM | 7.33 |
| CHEMBL377056 | — | IC50 | = | 56.3 | nM | 7.25 |
| CHEMBL379920 | — | IC50 | = | 58.4 | nM | 7.23 |
| CHEMBL266349 | MELAGATRAN | IC50 | = | 69.2 | nM | 7.16 |
| CHEMBL207836 | — | IC50 | = | 71.2 | nM | 7.15 |
| CHEMBL208190 | — | IC50 | = | 76.8 | nM | 7.12 |
| CHEMBL208137 | — | IC50 | = | 103.0 | nM | 6.99 |
| CHEMBL208306 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL207603 | — | IC50 | = | 288.0 | nM | 6.54 |
| CHEMBL204468 | — | IC50 | = | 581.0 | nM | 6.24 |
| CHEMBL207564 | — | IC50 | = | 4090.0 | nM | 5.39 |
| CHEMBL378185 | — | IC50 | = | 53600.0 | nM | 4.27 |