Assay Detail
Binding
CHEMBL2015356
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Inhibition of human CYP11B2 expressed in hamster V79 MZ cells using [3H] 11 deoxycorticosterone as substrate by HPLC radioflow detector
44
Total Activities
44
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | V79 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Optimization of the First Selective Steroid-11β-hydroxylase (CYP11B1) Inhibitors for the Treatment of Cortisol Dependent Diseases.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 44 | 6.14 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL681 | ETOMIDATE | 4.0 | 1 | 10.00 |
| CHEMBL157101 | KETOCONAZOLE | 4.0 | 1 | 7.17 |
| CHEMBL934 | METYRAPONE | 4.0 | 1 | 7.14 |
| CHEMBL2011246 | — | — | 1 | 6.62 |
| CHEMBL2011431 | — | — | 1 | 6.60 |
| CHEMBL2011432 | — | — | 1 | 6.55 |
| CHEMBL2011430 | — | — | 1 | 6.38 |
| CHEMBL2011257 | — | — | 1 | 6.31 |
| CHEMBL2011248 | — | — | 1 | 6.28 |
| CHEMBL2011243 | — | — | 1 | 6.24 |
| CHEMBL2011254 | — | — | 1 | 6.11 |
| CHEMBL2011437 | — | — | 1 | 6.08 |
| CHEMBL2011255 | — | — | 1 | 6.07 |
| CHEMBL2011260 | — | — | 1 | 6.04 |
| CHEMBL2011242 | — | — | 1 | 6.04 |
| CHEMBL2011263 | — | — | 1 | 6.03 |
| CHEMBL2011264 | — | — | 1 | 6.01 |
| CHEMBL2011433 | — | — | 1 | 5.94 |
| CHEMBL2011261 | — | — | 1 | 5.91 |
| CHEMBL402522 | — | — | 1 | 5.78 |
| CHEMBL2011244 | — | — | 1 | 5.76 |
| CHEMBL2011253 | — | — | 1 | 5.68 |
| CHEMBL272749 | — | — | 1 | 5.67 |
| CHEMBL2011247 | — | — | 1 | 5.67 |
| CHEMBL428780 | — | — | 1 | 5.56 |
| CHEMBL2011435 | — | — | 1 | 5.55 |
| CHEMBL2011262 | — | — | 1 | 5.49 |
| CHEMBL273205 | — | — | 1 | 5.47 |
| CHEMBL2011256 | — | — | 1 | 5.40 |
| CHEMBL402298 | — | — | 1 | 5.36 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL681 | ETOMIDATE | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL157101 | KETOCONAZOLE | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL934 | METYRAPONE | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL2011246 | — | IC50 | = | 237.0 | nM | 6.62 |
| CHEMBL2011431 | — | IC50 | = | 251.0 | nM | 6.60 |
| CHEMBL2011432 | — | IC50 | = | 281.0 | nM | 6.55 |
| CHEMBL2011430 | — | IC50 | = | 416.0 | nM | 6.38 |
| CHEMBL2011257 | — | IC50 | = | 487.0 | nM | 6.31 |
| CHEMBL2011248 | — | IC50 | = | 528.0 | nM | 6.28 |
| CHEMBL2011243 | — | IC50 | = | 576.0 | nM | 6.24 |
| CHEMBL2011254 | — | IC50 | = | 782.0 | nM | 6.11 |
| CHEMBL2011437 | — | IC50 | = | 830.0 | nM | 6.08 |
| CHEMBL2011255 | — | IC50 | = | 851.0 | nM | 6.07 |
| CHEMBL2011260 | — | IC50 | = | 914.0 | nM | 6.04 |
| CHEMBL2011242 | — | IC50 | = | 911.0 | nM | 6.04 |
| CHEMBL2011263 | — | IC50 | = | 929.0 | nM | 6.03 |
| CHEMBL2011264 | — | IC50 | = | 968.0 | nM | 6.01 |
| CHEMBL2011433 | — | IC50 | = | 1157.0 | nM | 5.94 |
| CHEMBL2011261 | — | IC50 | = | 1243.0 | nM | 5.91 |
| CHEMBL402522 | — | IC50 | = | 1665.0 | nM | 5.78 |
| CHEMBL2011244 | — | IC50 | = | 1736.0 | nM | 5.76 |
| CHEMBL2011253 | — | IC50 | = | 2075.0 | nM | 5.68 |
| CHEMBL272749 | — | IC50 | = | 2153.0 | nM | 5.67 |
| CHEMBL2011247 | — | IC50 | = | 2114.0 | nM | 5.67 |
| CHEMBL428780 | — | IC50 | = | 2768.0 | nM | 5.56 |
| CHEMBL2011435 | — | IC50 | = | 2832.0 | nM | 5.55 |
| CHEMBL2011262 | — | IC50 | = | 3265.0 | nM | 5.49 |
| CHEMBL273205 | — | IC50 | = | 3407.0 | nM | 5.47 |
| CHEMBL2011256 | — | IC50 | = | 3955.0 | nM | 5.40 |
| CHEMBL402298 | — | IC50 | = | 4391.0 | nM | 5.36 |
| CHEMBL2011434 | — | IC50 | = | 5159.0 | nM | 5.29 |
| CHEMBL255759 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL2011249 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL2011250 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL2011251 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL2011252 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL2011245 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL2011259 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL2011241 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL258097 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL2011436 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL1556445 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL2011240 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL1440486 | — | IC50 | > | 1000.0 | nM | - |