Assay Detail
Binding
CHEMBL3097587
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of thrombin (unknown origin)
7
Total Activities
7
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
5-Chlorothiophene-2-carboxylic acid [(S)-2-[2-methyl-3-(2-oxopyrrolidin-1-yl)benzenesulfonylamino]-3-(4-methylpiperazin-1-yl)-3-oxopropyl]amide (SAR107375), a selective and potent orally active dual thrombin and factor Xa inhibitor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 7.95 | 8.40 |
| Ki | 3 | 7.93 | 8.35 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL256941 | — | — | 1 | 8.40 |
| CHEMBL48361 | DABIGATRAN | 3.0 | 1 | 8.35 |
| CHEMBL431577 | — | — | 1 | 8.10 |
| CHEMBL3091516 | — | — | 1 | 7.70 |
| CHEMBL1270156 | TANOGITRAN | 2.0 | 1 | 7.58 |
| CHEMBL3091517 | — | — | 1 | 7.51 |
| CHEMBL198362 | RIVAROXABAN | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL256941 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL48361 | DABIGATRAN | Ki | = | 4.5 | nM | 8.35 |
| CHEMBL431577 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3091516 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL1270156 | TANOGITRAN | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL3091517 | — | Ki | = | 31.0 | nM | 7.51 |
| CHEMBL198362 | RIVAROXABAN | Ki | > | 1000.0 | nM | - |