Assay Detail
Binding
CHEMBL900664
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Inhibition of human thrombin
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Discovery of 1-(4-methoxyphenyl)-7-oxo-6-(4-(2-oxopiperidin-1-yl)phenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxamide (apixaban, BMS-562247), a highly potent, selective, efficacious, and orally bioavailable inhibitor of blood coagulation factor Xa.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 30 | 5.72 | 7.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL393393 | — | — | 1 | 7.00 |
| CHEMBL235265 | — | — | 1 | 6.85 |
| CHEMBL264106 | — | — | 1 | 6.75 |
| CHEMBL221296 | — | — | 1 | 6.48 |
| CHEMBL391787 | — | — | 1 | 6.02 |
| CHEMBL395372 | — | — | 1 | 6.01 |
| CHEMBL237242 | — | — | 1 | 6.01 |
| CHEMBL395142 | — | — | 1 | 6.01 |
| CHEMBL395373 | — | — | 1 | 6.00 |
| CHEMBL235064 | — | — | 1 | 5.75 |
| CHEMBL395371 | — | — | 1 | 5.72 |
| CHEMBL235710 | — | — | 1 | 5.60 |
| CHEMBL231779 | APIXABAN | 4.0 | 1 | 5.51 |
| CHEMBL235907 | — | — | 1 | 5.48 |
| CHEMBL235906 | — | — | 1 | 5.41 |
| CHEMBL392526 | — | — | 1 | 5.36 |
| CHEMBL238301 | — | — | 1 | 5.34 |
| CHEMBL399822 | — | — | 1 | 5.32 |
| CHEMBL235268 | — | — | 1 | 5.16 |
| CHEMBL236752 | — | — | 1 | 5.03 |
| CHEMBL235492 | — | — | 1 | 4.96 |
| CHEMBL396088 | — | — | 1 | 4.92 |
| CHEMBL439214 | — | — | 1 | 4.92 |
| CHEMBL396087 | — | — | 1 | - |
| CHEMBL235905 | — | — | 1 | - |
| CHEMBL235694 | — | — | 1 | - |
| CHEMBL391876 | — | — | 1 | - |
| CHEMBL428199 | — | — | 1 | - |
| CHEMBL393727 | — | — | 1 | - |
| CHEMBL237441 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL393393 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL235265 | — | Ki | = | 140.0 | nM | 6.85 |
| CHEMBL264106 | — | Ki | = | 180.0 | nM | 6.75 |
| CHEMBL221296 | — | Ki | = | 330.0 | nM | 6.48 |
| CHEMBL391787 | — | Ki | = | 950.0 | nM | 6.02 |
| CHEMBL395372 | — | Ki | = | 970.0 | nM | 6.01 |
| CHEMBL237242 | — | Ki | = | 980.0 | nM | 6.01 |
| CHEMBL395142 | — | Ki | = | 980.0 | nM | 6.01 |
| CHEMBL395373 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL235064 | — | Ki | = | 1800.0 | nM | 5.75 |
| CHEMBL395371 | — | Ki | = | 1900.0 | nM | 5.72 |
| CHEMBL235710 | — | Ki | = | 2520.0 | nM | 5.60 |
| CHEMBL231779 | APIXABAN | Ki | = | 3100.0 | nM | 5.51 |
| CHEMBL235907 | — | Ki | = | 3300.0 | nM | 5.48 |
| CHEMBL235906 | — | Ki | = | 3900.0 | nM | 5.41 |
| CHEMBL392526 | — | Ki | = | 4400.0 | nM | 5.36 |
| CHEMBL238301 | — | Ki | = | 4600.0 | nM | 5.34 |
| CHEMBL399822 | — | Ki | = | 4800.0 | nM | 5.32 |
| CHEMBL235268 | — | Ki | = | 7000.0 | nM | 5.16 |
| CHEMBL236752 | — | Ki | = | 9400.0 | nM | 5.03 |
| CHEMBL235492 | — | Ki | = | 11000.0 | nM | 4.96 |
| CHEMBL396088 | — | Ki | = | 12000.0 | nM | 4.92 |
| CHEMBL439214 | — | Ki | = | 12000.0 | nM | 4.92 |
| CHEMBL396087 | — | Ki | > | 2500.0 | nM | - |
| CHEMBL235905 | — | Ki | > | 13400.0 | nM | - |
| CHEMBL235694 | — | Ki | > | 6300.0 | nM | - |
| CHEMBL391876 | — | Ki | > | 6300.0 | nM | - |
| CHEMBL428199 | — | Ki | > | 6300.0 | nM | - |
| CHEMBL393727 | — | Ki | > | 6300.0 | nM | - |
| CHEMBL237441 | — | Ki | > | 20000.0 | nM | - |