Assay Detail
Binding
CHEMBL813668
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro activity against human thrombin.
31
Total Activities
31
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Discovery of 1-[3-(aminomethyl)phenyl]-N-3-fluoro-2'-(methylsulfonyl)-[1,1'-biphenyl]-4-yl]-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide (DPC423), a highly potent, selective, and orally bioavailable inhibitor of blood coagulation factor Xa.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 31 | 6.06 | 7.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL347846 | — | — | 1 | 7.40 |
| CHEMBL358835 | — | — | 1 | 7.30 |
| CHEMBL154238 | — | — | 1 | 7.16 |
| CHEMBL152281 | — | — | 1 | 6.92 |
| CHEMBL440733 | — | — | 1 | 6.75 |
| CHEMBL152859 | — | — | 1 | 6.70 |
| CHEMBL347307 | — | — | 1 | 6.68 |
| CHEMBL422688 | — | — | 1 | 6.64 |
| CHEMBL152854 | — | — | 1 | 6.52 |
| CHEMBL154512 | — | — | 1 | 6.52 |
| CHEMBL346834 | — | — | 1 | 6.52 |
| CHEMBL347931 | — | — | 1 | 6.52 |
| CHEMBL359132 | — | — | 1 | 6.52 |
| CHEMBL346686 | — | — | 1 | 6.40 |
| CHEMBL152276 | — | — | 1 | 6.35 |
| CHEMBL444074 | — | — | 1 | 6.22 |
| CHEMBL346857 | — | — | 1 | 6.05 |
| CHEMBL356016 | — | — | 1 | 6.05 |
| CHEMBL152274 | — | — | 1 | 6.05 |
| CHEMBL154322 | — | — | 1 | 5.85 |
| CHEMBL154680 | — | — | 1 | 5.70 |
| CHEMBL153611 | — | — | 1 | 5.55 |
| CHEMBL153946 | — | — | 1 | 5.24 |
| CHEMBL559015 | — | — | 1 | 5.22 |
| CHEMBL421808 | — | — | 1 | 5.13 |
| CHEMBL154572 | — | — | 1 | 4.92 |
| CHEMBL154504 | — | — | 1 | 4.85 |
| CHEMBL422351 | — | — | 1 | 4.85 |
| CHEMBL134736 | — | — | 1 | 4.68 |
| CHEMBL156775 | — | — | 1 | 4.68 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL347846 | — | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL358835 | — | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL154238 | — | Ki | = | 70.0 | nM | 7.16 |
| CHEMBL152281 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL440733 | — | Ki | = | 180.0 | nM | 6.75 |
| CHEMBL152859 | — | Ki | = | 200.0 | nM | 6.70 |
| CHEMBL347307 | — | Ki | = | 210.0 | nM | 6.68 |
| CHEMBL422688 | — | Ki | = | 230.0 | nM | 6.64 |
| CHEMBL152854 | — | Ki | = | 300.0 | nM | 6.52 |
| CHEMBL154512 | — | Ki | = | 300.0 | nM | 6.52 |
| CHEMBL346834 | — | Ki | = | 300.0 | nM | 6.52 |
| CHEMBL347931 | — | Ki | = | 300.0 | nM | 6.52 |
| CHEMBL359132 | — | Ki | = | 300.0 | nM | 6.52 |
| CHEMBL346686 | — | Ki | = | 400.0 | nM | 6.40 |
| CHEMBL152276 | — | Ki | = | 450.0 | nM | 6.35 |
| CHEMBL444074 | — | Ki | = | 600.0 | nM | 6.22 |
| CHEMBL346857 | — | Ki | = | 900.0 | nM | 6.05 |
| CHEMBL356016 | — | Ki | = | 900.0 | nM | 6.05 |
| CHEMBL152274 | — | Ki | = | 900.0 | nM | 6.05 |
| CHEMBL154322 | — | Ki | = | 1400.0 | nM | 5.85 |
| CHEMBL154680 | — | Ki | = | 2000.0 | nM | 5.70 |
| CHEMBL153611 | — | Ki | = | 2800.0 | nM | 5.55 |
| CHEMBL153946 | — | Ki | = | 5800.0 | nM | 5.24 |
| CHEMBL559015 | — | Ki | = | 6000.0 | nM | 5.22 |
| CHEMBL421808 | — | Ki | = | 7400.0 | nM | 5.13 |
| CHEMBL154572 | — | Ki | = | 12000.0 | nM | 4.92 |
| CHEMBL154504 | — | Ki | = | 14000.0 | nM | 4.85 |
| CHEMBL422351 | — | Ki | = | 14000.0 | nM | 4.85 |
| CHEMBL134736 | — | Ki | = | 21000.0 | nM | 4.68 |
| CHEMBL156775 | — | Ki | = | 21000.0 | nM | 4.68 |
| CHEMBL358834 | — | Ki | > | 2000.0 | nM | - |