Assay Detail
Binding
CHEMBL956028
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Inhibition of human Factor-10a
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Exploration of 4,4-disubstituted pyrrolidine-1,2-dicarboxamides as potent, orally active Factor Xa inhibitors with extended duration of action.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 9.64 | 10.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL475682 | — | — | 1 | 10.70 |
| CHEMBL476618 | — | — | 1 | 10.30 |
| CHEMBL515107 | — | — | 1 | 10.10 |
| CHEMBL474271 | — | — | 1 | 10.10 |
| CHEMBL474678 | — | — | 1 | 10.00 |
| CHEMBL514510 | — | — | 1 | 9.96 |
| CHEMBL474070 | — | — | 1 | 9.80 |
| CHEMBL475280 | — | — | 1 | 9.74 |
| CHEMBL476412 | — | — | 1 | 9.74 |
| CHEMBL515941 | — | — | 1 | 9.66 |
| CHEMBL477229 | — | — | 1 | 9.51 |
| CHEMBL448927 | — | — | 1 | 9.47 |
| CHEMBL515156 | — | — | 1 | 9.30 |
| CHEMBL515147 | — | — | 1 | 9.30 |
| CHEMBL477228 | — | — | 1 | 9.27 |
| CHEMBL476186 | ERIBAXABAN | 2.0 | 1 | 9.24 |
| CHEMBL475481 | — | — | 1 | 8.92 |
| CHEMBL476187 | — | — | 1 | 8.34 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL475682 | — | IC50 | = | 0.02 | nM | 10.70 |
| CHEMBL476618 | — | IC50 | = | 0.05 | nM | 10.30 |
| CHEMBL515107 | — | IC50 | = | 0.08 | nM | 10.10 |
| CHEMBL474271 | — | IC50 | = | 0.08 | nM | 10.10 |
| CHEMBL474678 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL514510 | — | IC50 | = | 0.11 | nM | 9.96 |
| CHEMBL474070 | — | IC50 | = | 0.16 | nM | 9.80 |
| CHEMBL475280 | — | IC50 | = | 0.18 | nM | 9.74 |
| CHEMBL476412 | — | IC50 | = | 0.18 | nM | 9.74 |
| CHEMBL515941 | — | IC50 | = | 0.22 | nM | 9.66 |
| CHEMBL477229 | — | IC50 | = | 0.31 | nM | 9.51 |
| CHEMBL448927 | — | IC50 | = | 0.34 | nM | 9.47 |
| CHEMBL515156 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL515147 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL477228 | — | IC50 | = | 0.54 | nM | 9.27 |
| CHEMBL476186 | ERIBAXABAN | IC50 | = | 0.57 | nM | 9.24 |
| CHEMBL475481 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL476187 | — | IC50 | = | 4.6 | nM | 8.34 |