Assay Detail
Binding
CHEMBL900663
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Binding affinity to human F10a
39
Total Activities
39
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 | 39 | 8.98 | 10.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL378093 | — | — | 1 | 10.52 |
| CHEMBL235265 | — | — | 1 | 10.15 |
| CHEMBL231779 | APIXABAN | 4.0 | 1 | 10.10 |
| CHEMBL237228 | — | — | 1 | 10.10 |
| CHEMBL237226 | — | — | 1 | 9.85 |
| CHEMBL221296 | — | — | 1 | 9.74 |
| CHEMBL206335 | RAZAXABAN | 2.0 | 1 | 9.72 |
| CHEMBL392526 | — | — | 1 | 9.64 |
| CHEMBL391484 | — | — | 1 | 9.62 |
| CHEMBL395371 | — | — | 1 | 9.60 |
| CHEMBL264106 | — | — | 1 | 9.60 |
| CHEMBL237419 | — | — | 1 | 9.54 |
| CHEMBL443578 | — | — | 1 | 9.52 |
| CHEMBL235064 | — | — | 1 | 9.51 |
| CHEMBL393393 | — | — | 1 | 9.48 |
| CHEMBL237420 | — | — | 1 | 9.44 |
| CHEMBL235907 | — | — | 1 | 9.33 |
| CHEMBL395142 | — | — | 1 | 9.32 |
| CHEMBL235694 | — | — | 1 | 9.30 |
| CHEMBL235710 | — | — | 1 | 9.27 |
| CHEMBL396088 | — | — | 1 | 9.20 |
| CHEMBL439214 | — | — | 1 | 9.17 |
| CHEMBL395372 | — | — | 1 | 9.07 |
| CHEMBL279187 | — | — | 1 | 9.01 |
| CHEMBL395373 | — | — | 1 | 8.96 |
| CHEMBL235492 | — | — | 1 | 8.77 |
| CHEMBL399822 | — | — | 1 | 8.77 |
| CHEMBL391787 | — | — | 1 | 8.70 |
| CHEMBL235906 | — | — | 1 | 8.68 |
| CHEMBL396087 | — | — | 1 | 8.64 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL378093 | — | Ki | = | 0.03 | nM | 10.52 |
| CHEMBL235265 | — | Ki | = | 0.07 | nM | 10.15 |
| CHEMBL237228 | — | Ki | = | 0.08 | nM | 10.10 |
| CHEMBL231779 | APIXABAN | Ki | = | 0.08 | nM | 10.10 |
| CHEMBL237226 | — | Ki | = | 0.14 | nM | 9.85 |
| CHEMBL221296 | — | Ki | = | 0.18 | nM | 9.74 |
| CHEMBL206335 | RAZAXABAN | Ki | = | 0.19 | nM | 9.72 |
| CHEMBL392526 | — | Ki | = | 0.23 | nM | 9.64 |
| CHEMBL391484 | — | Ki | = | 0.24 | nM | 9.62 |
| CHEMBL395371 | — | Ki | = | 0.25 | nM | 9.60 |
| CHEMBL264106 | — | Ki | = | 0.25 | nM | 9.60 |
| CHEMBL237419 | — | Ki | = | 0.29 | nM | 9.54 |
| CHEMBL443578 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL235064 | — | Ki | = | 0.31 | nM | 9.51 |
| CHEMBL393393 | — | Ki | = | 0.33 | nM | 9.48 |
| CHEMBL237420 | — | Ki | = | 0.36 | nM | 9.44 |
| CHEMBL235907 | — | Ki | = | 0.47 | nM | 9.33 |
| CHEMBL395142 | — | Ki | = | 0.48 | nM | 9.32 |
| CHEMBL235694 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL235710 | — | Ki | = | 0.54 | nM | 9.27 |
| CHEMBL396088 | — | Ki | = | 0.63 | nM | 9.20 |
| CHEMBL439214 | — | Ki | = | 0.67 | nM | 9.17 |
| CHEMBL395372 | — | Ki | = | 0.85 | nM | 9.07 |
| CHEMBL279187 | — | Ki | = | 0.97 | nM | 9.01 |
| CHEMBL395373 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL235492 | — | Ki | = | 1.7 | nM | 8.77 |
| CHEMBL399822 | — | Ki | = | 1.7 | nM | 8.77 |
| CHEMBL391787 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL235906 | — | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL396087 | — | Ki | = | 2.3 | nM | 8.64 |
| CHEMBL237242 | — | Ki | = | 3.9 | nM | 8.41 |
| CHEMBL235268 | — | Ki | = | 4.8 | nM | 8.32 |
| CHEMBL235905 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL236752 | — | Ki | = | 6.7 | nM | 8.17 |
| CHEMBL237441 | — | Ki | = | 7.6 | nM | 8.12 |
| CHEMBL238301 | — | Ki | = | 9.6 | nM | 8.02 |
| CHEMBL428199 | — | Ki | = | 180.0 | nM | 6.75 |
| CHEMBL391876 | — | Ki | = | 610.0 | nM | 6.21 |
| CHEMBL393727 | — | Ki | = | 1600.0 | nM | 5.80 |