Assay Detail
Binding
CHEMBL814934
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of thrombin-catalyzed hydrolysis of a standard substrate
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Discovery and development of the novel potent orally active thrombin inhibitor N-(9-hydroxy-9-fluorenecarboxy)prolyl trans-4-aminocyclohexylmethyl amide (L-372,460): coapplication of structure-based design and rapid multiple analogue synthesis on solid support.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 7.28 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL130119 | — | — | 1 | 8.52 |
| CHEMBL364255 | — | — | 1 | 8.40 |
| CHEMBL334727 | — | — | 1 | 8.30 |
| CHEMBL125181 | — | — | 1 | 8.22 |
| CHEMBL434417 | — | — | 1 | 8.00 |
| CHEMBL131999 | — | — | 1 | 7.96 |
| CHEMBL334482 | — | — | 1 | 7.30 |
| CHEMBL341171 | — | — | 1 | 7.24 |
| CHEMBL338939 | — | — | 1 | 7.22 |
| CHEMBL335906 | — | — | 1 | 7.05 |
| CHEMBL420689 | — | — | 1 | 7.00 |
| CHEMBL128724 | — | — | 1 | 6.97 |
| CHEMBL130505 | — | — | 1 | 6.92 |
| CHEMBL335225 | — | — | 1 | 6.85 |
| CHEMBL422803 | — | — | 1 | 6.72 |
| CHEMBL435393 | — | — | 1 | 6.64 |
| CHEMBL435799 | — | — | 1 | 6.64 |
| CHEMBL338321 | — | — | 1 | 6.42 |
| CHEMBL339525 | — | — | 1 | 6.04 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL130119 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL364255 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL334727 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL125181 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL434417 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL131999 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL334482 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL341171 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL338939 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL335906 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL420689 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL128724 | — | IC50 | = | 106.0 | nM | 6.97 |
| CHEMBL130505 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL335225 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL422803 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL435393 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL435799 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL338321 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL339525 | — | IC50 | = | 910.0 | nM | 6.04 |