Assay Detail
ADMET
CHEMBL4016909
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Inhibition of human CYP11B2 expressed in hamster V79MZ cells using [1,2-3H]-11-deoxycorticosterone as substrate after 6 hrs by HPLC analysis
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | ADMET |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Lead Optimization Generates CYP11B1 Inhibitors of Pyridylmethyl Isoxazole Type with Improved Pharmacological Profile for the Treatment of Cushing's Disease.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 29 | 7.16 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3099695 | OSILODROSTAT | 4.0 | 1 | 9.70 |
| CHEMBL4068439 | — | — | 1 | 8.22 |
| CHEMBL4093884 | — | — | 1 | 8.10 |
| CHEMBL4096366 | — | — | 1 | 7.80 |
| CHEMBL4079408 | — | — | 1 | 7.77 |
| CHEMBL4103666 | — | — | 1 | 7.62 |
| CHEMBL4070031 | — | — | 1 | 7.62 |
| CHEMBL4097298 | — | — | 1 | 7.57 |
| CHEMBL4067404 | — | — | 1 | 7.57 |
| CHEMBL4078318 | — | — | 1 | 7.55 |
| CHEMBL4095910 | — | — | 1 | 7.52 |
| CHEMBL4059931 | — | — | 1 | 7.50 |
| CHEMBL934 | METYRAPONE | 4.0 | 1 | 7.14 |
| CHEMBL4079276 | — | — | 1 | 7.09 |
| CHEMBL4088179 | — | — | 1 | 7.05 |
| CHEMBL4086201 | — | — | 1 | 7.01 |
| CHEMBL4097224 | — | — | 1 | 6.94 |
| CHEMBL4072324 | — | — | 1 | 6.92 |
| CHEMBL4066317 | — | — | 1 | 6.82 |
| CHEMBL4099271 | — | — | 1 | 6.76 |
| CHEMBL4068593 | — | — | 1 | 6.76 |
| CHEMBL4104108 | — | — | 1 | 6.74 |
| CHEMBL4101613 | — | — | 1 | 6.67 |
| CHEMBL4104045 | — | — | 1 | 6.34 |
| CHEMBL4074925 | — | — | 1 | 6.29 |
| CHEMBL4086130 | — | — | 1 | 6.28 |
| CHEMBL4089578 | — | — | 1 | 6.23 |
| CHEMBL4078239 | — | — | 1 | 6.18 |
| CHEMBL4096290 | — | — | 1 | 5.88 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3099695 | OSILODROSTAT | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL4068439 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4093884 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL4096366 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL4079408 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL4103666 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL4070031 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL4097298 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL4067404 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL4078318 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL4095910 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL4059931 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL934 | METYRAPONE | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL4079276 | — | IC50 | = | 82.0 | nM | 7.09 |
| CHEMBL4088179 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL4086201 | — | IC50 | = | 97.0 | nM | 7.01 |
| CHEMBL4097224 | — | IC50 | = | 116.0 | nM | 6.94 |
| CHEMBL4072324 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL4066317 | — | IC50 | = | 152.0 | nM | 6.82 |
| CHEMBL4099271 | — | IC50 | = | 174.0 | nM | 6.76 |
| CHEMBL4068593 | — | IC50 | = | 173.0 | nM | 6.76 |
| CHEMBL4104108 | — | IC50 | = | 182.0 | nM | 6.74 |
| CHEMBL4101613 | — | IC50 | = | 215.0 | nM | 6.67 |
| CHEMBL4104045 | — | IC50 | = | 459.0 | nM | 6.34 |
| CHEMBL4074925 | — | IC50 | = | 507.0 | nM | 6.29 |
| CHEMBL4086130 | — | IC50 | = | 520.0 | nM | 6.28 |
| CHEMBL4089578 | — | IC50 | = | 586.0 | nM | 6.23 |
| CHEMBL4078239 | — | IC50 | = | 657.0 | nM | 6.18 |
| CHEMBL4096290 | — | IC50 | = | 1304.0 | nM | 5.88 |