Assay Detail
ADMET
CHEMBL989845
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Inhibition of human recombinant CYP2C9 expressed in baculovirus-infected insect microsomes
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | ADMET |
| Organism | Homo sapiens |
| Subcellular | Microsome |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
In vivo active aldosterone synthase inhibitors with improved selectivity: lead optimization providing a series of pyridine substituted 3,4-dihydro-1H-quinolin-2-one derivatives.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 4.80 | 5.54 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL456390 | — | — | 1 | 5.54 |
| CHEMBL499007 | — | — | 1 | 4.89 |
| CHEMBL460178 | — | — | 1 | 4.79 |
| CHEMBL462093 | — | — | 1 | 4.55 |
| CHEMBL62811 | — | — | 1 | 4.23 |
| CHEMBL448743 | — | — | 1 | - |
| CHEMBL446083 | — | — | 1 | - |
| CHEMBL1109 | SULFAPHENAZOLE | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL456390 | — | IC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL499007 | — | IC50 | = | 12900.0 | nM | 4.89 |
| CHEMBL460178 | — | IC50 | = | 16300.0 | nM | 4.79 |
| CHEMBL462093 | — | IC50 | = | 28300.0 | nM | 4.55 |
| CHEMBL62811 | — | IC50 | = | 58900.0 | nM | 4.23 |
| CHEMBL448743 | — | IC50 | = | 123000.0 | nM | - |
| CHEMBL446083 | — | IC50 | = | 125000.0 | nM | - |
| CHEMBL1109 | SULFAPHENAZOLE | IC50 | = | 318000.0 | nM | - |