Assay Detail
Binding
CHEMBL3868073
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Inhibition of recombinant CYP11B1 (unknown origin) overexpressed in human AD293 cells assessed as reduction in cortisol formation preincubated for 60 mins followed by addition of 11-deoxycortisol as substrate measured after 12 hrs by LC-MS/MS analysis
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | AD293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Design, synthesis, and evaluation of (2S,4R)-Ketoconazole sulfonamide analogs as potential treatments for Metabolic Syndrome.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 7.15 | 7.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3891718 | — | — | 1 | 7.77 |
| CHEMBL3968178 | — | — | 1 | 7.54 |
| CHEMBL3938615 | — | — | 1 | 7.50 |
| CHEMBL3894912 | — | — | 1 | 7.40 |
| CHEMBL3922888 | — | — | 1 | 7.24 |
| CHEMBL3913908 | — | — | 1 | 7.20 |
| CHEMBL3980889 | — | — | 1 | 7.17 |
| CHEMBL3952032 | — | — | 1 | 7.16 |
| CHEMBL3960724 | — | — | 1 | 7.09 |
| CHEMBL3964421 | — | — | 1 | 6.96 |
| CHEMBL157101 | KETOCONAZOLE | 4.0 | 1 | 6.94 |
| CHEMBL3931836 | — | — | 1 | 6.73 |
| CHEMBL3983734 | — | — | 1 | 6.30 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3891718 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL3968178 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL3938615 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL3894912 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL3922888 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL3913908 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL3980889 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL3952032 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL3960724 | — | IC50 | = | 82.0 | nM | 7.09 |
| CHEMBL3964421 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL157101 | KETOCONAZOLE | IC50 | = | 116.0 | nM | 6.94 |
| CHEMBL3931836 | — | IC50 | = | 187.0 | nM | 6.73 |
| CHEMBL3983734 | — | IC50 | = | 500.0 | nM | 6.30 |