Assay Detail
Binding
CHEMBL813433
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Binding inhibition against thrombin was measured by nonlinear regression analysis using Morrison's equation for tight-binding inhibition
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Dibasic benzo[b]thiophene derivatives as a novel class of active site directed thrombin inhibitors: 2. Sidechain optimization and demonstration of in vivo efficacy.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 17 | 8.68 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL168171 | — | — | 1 | 9.52 |
| CHEMBL350351 | — | — | 1 | 9.40 |
| CHEMBL159133 | — | — | 1 | 9.30 |
| CHEMBL167741 | — | — | 1 | 9.30 |
| CHEMBL434671 | — | — | 1 | 9.05 |
| CHEMBL18778 | — | — | 1 | 9.05 |
| CHEMBL19511 | — | — | 1 | 8.72 |
| CHEMBL275206 | — | — | 1 | 8.68 |
| CHEMBL350373 | — | — | 1 | 8.64 |
| CHEMBL352279 | — | — | 1 | 8.42 |
| CHEMBL18495 | — | — | 1 | 8.39 |
| CHEMBL19242 | — | — | 1 | 8.29 |
| CHEMBL164246 | — | — | 1 | 8.29 |
| CHEMBL273196 | EFEGATRAN | 2.0 | 1 | 8.26 |
| CHEMBL351476 | — | — | 1 | 8.15 |
| CHEMBL418004 | — | — | 1 | 8.14 |
| CHEMBL18516 | — | — | 1 | 7.96 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL168171 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL350351 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL159133 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL167741 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL434671 | — | Ki | = | 0.9 | nM | 9.05 |
| CHEMBL18778 | — | Ki | = | 0.9 | nM | 9.05 |
| CHEMBL19511 | — | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL275206 | — | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL350373 | — | Ki | = | 2.3 | nM | 8.64 |
| CHEMBL352279 | — | Ki | = | 3.8 | nM | 8.42 |
| CHEMBL18495 | — | Ki | = | 4.1 | nM | 8.39 |
| CHEMBL19242 | — | Ki | = | 5.1 | nM | 8.29 |
| CHEMBL164246 | — | Ki | = | 5.1 | nM | 8.29 |
| CHEMBL273196 | EFEGATRAN | Ki | = | 5.5 | nM | 8.26 |
| CHEMBL351476 | — | Ki | = | 7.0 | nM | 8.15 |
| CHEMBL418004 | — | Ki | = | 7.2 | nM | 8.14 |
| CHEMBL18516 | — | Ki | = | 11.0 | nM | 7.96 |