Assay Detail
Binding
CHEMBL4016908
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human CYP11B1 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 | Binding |
| 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 | 7.86 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4093884 | — | — | 1 | 9.00 |
| CHEMBL4068439 | — | — | 1 | 9.00 |
| CHEMBL4096366 | — | — | 1 | 8.70 |
| CHEMBL4097298 | — | — | 1 | 8.70 |
| CHEMBL4079408 | — | — | 1 | 8.70 |
| CHEMBL4103666 | — | — | 1 | 8.52 |
| CHEMBL3099695 | OSILODROSTAT | 4.0 | 1 | 8.52 |
| CHEMBL4067404 | — | — | 1 | 8.52 |
| CHEMBL4078318 | — | — | 1 | 8.40 |
| CHEMBL4059931 | — | — | 1 | 8.40 |
| CHEMBL4079276 | — | — | 1 | 8.30 |
| CHEMBL4095910 | — | — | 1 | 8.30 |
| CHEMBL4070031 | — | — | 1 | 8.05 |
| CHEMBL4097224 | — | — | 1 | 7.85 |
| CHEMBL4072324 | — | — | 1 | 7.85 |
| CHEMBL934 | METYRAPONE | 4.0 | 1 | 7.82 |
| CHEMBL4086201 | — | — | 1 | 7.80 |
| CHEMBL4068593 | — | — | 1 | 7.70 |
| CHEMBL4088179 | — | — | 1 | 7.66 |
| CHEMBL4104108 | — | — | 1 | 7.38 |
| CHEMBL4066317 | — | — | 1 | 7.32 |
| CHEMBL4101613 | — | — | 1 | 7.24 |
| CHEMBL4099271 | — | — | 1 | 7.24 |
| CHEMBL4104045 | — | — | 1 | 7.21 |
| CHEMBL4078239 | — | — | 1 | 6.98 |
| CHEMBL4089578 | — | — | 1 | 6.86 |
| CHEMBL4096290 | — | — | 1 | 6.83 |
| CHEMBL4086130 | — | — | 1 | 6.82 |
| CHEMBL4074925 | — | — | 1 | 6.29 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4093884 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4068439 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4096366 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4097298 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4079408 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4103666 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3099695 | OSILODROSTAT | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL4067404 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL4078318 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4059931 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4079276 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4095910 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4070031 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL4097224 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4072324 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL934 | METYRAPONE | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4086201 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL4068593 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4088179 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL4104108 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL4066317 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL4101613 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL4099271 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL4104045 | — | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL4078239 | — | IC50 | = | 104.0 | nM | 6.98 |
| CHEMBL4089578 | — | IC50 | = | 137.0 | nM | 6.86 |
| CHEMBL4096290 | — | IC50 | = | 148.0 | nM | 6.83 |
| CHEMBL4086130 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL4074925 | — | IC50 | = | 516.0 | nM | 6.29 |