Assay Detail
Binding
CHEMBL811969
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro inhibitory constant against human thrombin (FIIa).
35
Total Activities
35
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Non-covalent thrombin inhibitors featuring P(3)-heterocycles with P(1)-monocyclic arginine surrogates.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 35 | 8.12 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL19831 | — | — | 1 | 10.00 |
| CHEMBL19666 | — | — | 1 | 10.00 |
| CHEMBL277695 | — | — | 1 | 9.92 |
| CHEMBL431292 | CVS-2359 | — | 1 | 9.85 |
| CHEMBL19731 | — | — | 1 | 9.43 |
| CHEMBL19599 | CVS-2139 | — | 1 | 9.25 |
| CHEMBL19359 | — | — | 1 | 9.24 |
| CHEMBL11157 | L-374087 | — | 1 | 9.17 |
| CHEMBL19811 | — | — | 1 | 9.00 |
| CHEMBL19080 | L-375378 | — | 1 | 9.00 |
| CHEMBL274968 | — | — | 1 | 8.96 |
| CHEMBL416912 | — | — | 1 | 8.80 |
| CHEMBL417635 | — | — | 1 | 8.72 |
| CHEMBL19548 | — | — | 1 | 8.49 |
| CHEMBL19619 | — | — | 1 | 8.44 |
| CHEMBL19453 | — | — | 1 | 8.28 |
| CHEMBL19689 | — | — | 1 | 8.26 |
| CHEMBL19740 | — | — | 1 | 8.23 |
| CHEMBL19798 | — | — | 1 | 8.23 |
| CHEMBL279199 | — | — | 1 | 8.22 |
| CHEMBL282028 | — | — | 1 | 8.01 |
| CHEMBL417457 | — | — | 1 | 7.88 |
| CHEMBL283555 | — | — | 1 | 7.68 |
| CHEMBL19644 | — | — | 1 | 7.51 |
| CHEMBL283945 | — | — | 1 | 7.07 |
| CHEMBL19700 | — | — | 1 | 6.99 |
| CHEMBL19037 | — | — | 1 | 6.87 |
| CHEMBL19527 | — | — | 1 | 6.85 |
| CHEMBL19241 | — | — | 1 | 6.80 |
| CHEMBL19071 | — | — | 1 | 6.71 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL19831 | — | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL19666 | — | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL277695 | — | Ki | = | 0.12 | nM | 9.92 |
| CHEMBL431292 | CVS-2359 | Ki | = | 0.14 | nM | 9.85 |
| CHEMBL19731 | — | Ki | = | 0.37 | nM | 9.43 |
| CHEMBL19599 | CVS-2139 | Ki | = | 0.56 | nM | 9.25 |
| CHEMBL19359 | — | Ki | = | 0.57 | nM | 9.24 |
| CHEMBL11157 | L-374087 | Ki | = | 0.68 | nM | 9.17 |
| CHEMBL19811 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL19080 | L-375378 | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL274968 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL416912 | — | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL417635 | — | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL19548 | — | Ki | = | 3.2 | nM | 8.49 |
| CHEMBL19619 | — | Ki | = | 3.6 | nM | 8.44 |
| CHEMBL19453 | — | Ki | = | 5.3 | nM | 8.28 |
| CHEMBL19689 | — | Ki | = | 5.5 | nM | 8.26 |
| CHEMBL19740 | — | Ki | = | 5.9 | nM | 8.23 |
| CHEMBL19798 | — | Ki | = | 5.9 | nM | 8.23 |
| CHEMBL279199 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL282028 | — | Ki | = | 9.8 | nM | 8.01 |
| CHEMBL417457 | — | Ki | = | 13.2 | nM | 7.88 |
| CHEMBL283555 | — | Ki | = | 20.8 | nM | 7.68 |
| CHEMBL19644 | — | Ki | = | 30.8 | nM | 7.51 |
| CHEMBL283945 | — | Ki | = | 85.2 | nM | 7.07 |
| CHEMBL19700 | — | Ki | = | 103.2 | nM | 6.99 |
| CHEMBL19037 | — | Ki | = | 136.0 | nM | 6.87 |
| CHEMBL19527 | — | Ki | = | 140.8 | nM | 6.85 |
| CHEMBL19241 | — | Ki | = | 157.9 | nM | 6.80 |
| CHEMBL19071 | — | Ki | = | 196.8 | nM | 6.71 |
| CHEMBL18873 | — | Ki | = | 276.2 | nM | 6.56 |
| CHEMBL19728 | — | Ki | = | 281.0 | nM | 6.55 |
| CHEMBL18759 | — | Ki | = | 323.8 | nM | 6.49 |
| CHEMBL19438 | — | Ki | = | 357.1 | nM | 6.45 |
| CHEMBL19767 | — | Ki | = | 461.9 | nM | 6.33 |