Assay Detail
ADMET
CHEMBL1787756
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Inhibition of human CYP2C9 expressed in Escherichia coli by fluorimetric assay
17
Total Activities
17
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | ADMET |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
p38alpha mitogen-activated protein kinase inhibitors: optimization of a series of biphenylamides to give a molecule suitable for clinical progression.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 4.64 | 5.70 |
| pIC50 | 3 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1784164 | — | — | 1 | 5.70 |
| CHEMBL478649 | — | — | 1 | 5.40 |
| CHEMBL1784168 | — | — | 1 | 4.90 |
| CHEMBL1784171 | — | — | 1 | 4.80 |
| CHEMBL1784173 | — | — | 1 | 4.50 |
| CHEMBL1088752 | LOSMAPIMOD | 3.0 | 1 | 4.50 |
| CHEMBL1784177 | — | — | 1 | 4.50 |
| CHEMBL1784175 | — | — | 1 | 4.40 |
| CHEMBL1232887 | — | — | 1 | 4.40 |
| CHEMBL1784176 | — | — | 1 | 4.40 |
| CHEMBL1784174 | — | — | 1 | 4.40 |
| CHEMBL1784170 | — | — | 1 | 4.20 |
| CHEMBL1784172 | — | — | 1 | 4.20 |
| CHEMBL1784167 | — | — | 1 | - |
| CHEMBL1784166 | — | — | 1 | - |
| CHEMBL1784169 | — | — | 1 | - |
| CHEMBL1784165 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1784164 | — | IC50 | = | 1995.26 | nM | 5.70 |
| CHEMBL478649 | — | IC50 | = | 3981.07 | nM | 5.40 |
| CHEMBL1784168 | — | IC50 | = | 12589.25 | nM | 4.90 |
| CHEMBL1784171 | — | IC50 | = | 15848.93 | nM | 4.80 |
| CHEMBL1784173 | — | IC50 | = | 31622.78 | nM | 4.50 |
| CHEMBL1088752 | LOSMAPIMOD | IC50 | = | 31622.78 | nM | 4.50 |
| CHEMBL1784177 | — | IC50 | = | 31622.78 | nM | 4.50 |
| CHEMBL1784175 | — | IC50 | = | 39810.72 | nM | 4.40 |
| CHEMBL1232887 | — | IC50 | = | 39810.72 | nM | 4.40 |
| CHEMBL1784176 | — | IC50 | = | 39810.72 | nM | 4.40 |
| CHEMBL1784174 | — | IC50 | = | 39810.72 | nM | 4.40 |
| CHEMBL1784170 | — | IC50 | = | 63095.73 | nM | 4.20 |
| CHEMBL1784172 | — | IC50 | = | 63095.73 | nM | 4.20 |
| CHEMBL1784167 | — | pIC50 | - | — | - | |
| CHEMBL1784166 | — | pIC50 | - | — | - | |
| CHEMBL1784169 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL1784165 | — | pIC50 | - | — | - |