Assay Detail
Binding
CHEMBL813669
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro inhibition constant (Ki) against human thrombin
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Efficacious and orally bioavailable thrombin inhibitors based on a 2,5-thienylamidine at the P1 position: discovery of N-carboxymethyl-d-diphenylalanyl-l-prolyl[(5-amidino-2-thienyl)methyl]amide.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 25 | 10.10 | 11.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL120079 | — | — | 1 | 11.00 |
| CHEMBL121212 | — | — | 1 | 11.00 |
| CHEMBL330949 | — | — | 1 | 10.89 |
| CHEMBL124300 | — | — | 1 | 10.82 |
| CHEMBL420540 | — | — | 1 | 10.82 |
| CHEMBL119877 | — | — | 1 | 10.82 |
| CHEMBL331571 | — | — | 1 | 10.77 |
| CHEMBL120308 | — | — | 1 | 10.70 |
| CHEMBL122410 | — | — | 1 | 10.70 |
| CHEMBL120187 | — | — | 1 | 10.52 |
| CHEMBL332819 | — | — | 1 | 10.00 |
| CHEMBL121694 | — | — | 1 | 9.92 |
| CHEMBL332764 | — | — | 1 | 9.80 |
| CHEMBL333969 | — | — | 1 | 9.77 |
| CHEMBL120950 | — | — | 1 | 9.40 |
| CHEMBL439970 | — | — | 1 | 9.37 |
| CHEMBL121379 | — | — | 1 | 9.22 |
| CHEMBL121150 | — | — | 1 | 9.19 |
| CHEMBL120918 | — | — | 1 | 8.85 |
| CHEMBL1166 | ARGATROBAN | 4.0 | 1 | 8.40 |
| CHEMBL331847 | — | — | 1 | - |
| CHEMBL331742 | — | — | 1 | - |
| CHEMBL1795037 | — | — | 1 | - |
| CHEMBL331771 | — | — | 1 | - |
| CHEMBL269575 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL120079 | — | Ki | = | 0.01 | nM | 11.00 |
| CHEMBL121212 | — | Ki | = | 0.01 | nM | 11.00 |
| CHEMBL330949 | — | Ki | = | 0.013 | nM | 10.89 |
| CHEMBL124300 | — | Ki | = | 0.015 | nM | 10.82 |
| CHEMBL420540 | — | Ki | = | 0.015 | nM | 10.82 |
| CHEMBL119877 | — | Ki | = | 0.015 | nM | 10.82 |
| CHEMBL331571 | — | Ki | = | 0.017 | nM | 10.77 |
| CHEMBL120308 | — | Ki | = | 0.02 | nM | 10.70 |
| CHEMBL122410 | — | Ki | = | 0.02 | nM | 10.70 |
| CHEMBL120187 | — | Ki | = | 0.03 | nM | 10.52 |
| CHEMBL332819 | — | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL121694 | — | Ki | = | 0.12 | nM | 9.92 |
| CHEMBL332764 | — | Ki | = | 0.16 | nM | 9.80 |
| CHEMBL333969 | — | Ki | = | 0.17 | nM | 9.77 |
| CHEMBL120950 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL439970 | — | Ki | = | 0.43 | nM | 9.37 |
| CHEMBL121379 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL121150 | — | Ki | = | 0.64 | nM | 9.19 |
| CHEMBL120918 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL1166 | ARGATROBAN | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL331847 | — | Ki | = | 0.008 | nM | - |
| CHEMBL331742 | — | Ki | = | 0.004 | nM | - |
| CHEMBL1795037 | — | Ki | = | 0.005 | nM | - |
| CHEMBL331771 | — | Ki | = | 0.003 | nM | - |
| CHEMBL269575 | — | Ki | = | 0.003 | nM | - |