Assay Detail
Binding
CHEMBL5730293
Review assay metadata, readout intent, target linkage, and publication context from the same page.
G402-Based Assay: Herein we identified the use of the G-402 cell line as a host cell to ectopically express (transiently or stably) enzymes of the CYP11 family. Specifically we developed stable G-402 cells expressing ectopically human CYP11B1, human CYP11B2, human CYP11A1, cynmolgus CYP11B1 or cynomolgus CYP11B2 enzyme activity. Importantly the identified cell line G-402 expresses co-factors (adrenodoxin and adrenodoxin reductase) important for the activity of the CYP11 family and no relevant enzyme activity of the CYP11 family (in comparison to H295R cells) was detected in these cells. Therefore the G-402 cell line is uniquely suited as a host cell for the ectopic expression of enzymes from the CYP11 family.Cellular enzyme assays were performed in DMEM/F12 medium containing 2.5% charcoal treated FCS and appropriate concentration of substrate (0.3-10 uM 11-Deoxycorticosterone, 11-Deoxycortisol or Corticosterone). For assaying enzymatic activity, cells were plated onto 96 well plates and incubated for 16 h. An aliquot of the supernatant is then transferred and analyzed for the concentration of the expected product (Aldosterone for CYP11B2; Cortisol for CYP11B1). The concentrations of these steroids can be determined using HTRF assays from CisBio analyzing either Aldosterone or Cortisol.
90
Total Activities
30
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Dihydroquinoline-2-one derivatives
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 30 | 9.33 | 10.92 |
| kon | 30 | - | - |
| k_off | 30 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3916961 | — | — | 3 | 10.92 |
| CHEMBL3986059 | — | — | 3 | 10.00 |
| CHEMBL3923975 | — | — | 3 | 10.00 |
| CHEMBL3959070 | — | — | 3 | 10.00 |
| CHEMBL3911527 | — | — | 3 | 10.00 |
| CHEMBL3969143 | — | — | 3 | 10.00 |
| CHEMBL3939497 | — | — | 3 | 10.00 |
| CHEMBL3930515 | — | — | 3 | 10.00 |
| CHEMBL3948274 | — | — | 3 | 9.70 |
| CHEMBL3890700 | — | — | 3 | 9.70 |
| CHEMBL3897028 | — | — | 3 | 9.70 |
| CHEMBL3984990 | — | — | 3 | 9.70 |
| CHEMBL3936019 | — | — | 3 | 9.70 |
| CHEMBL3950364 | — | — | 3 | 9.52 |
| CHEMBL3928063 | — | — | 3 | 9.52 |
| CHEMBL3902519 | — | — | 3 | 9.52 |
| CHEMBL3982418 | — | — | 3 | 9.52 |
| CHEMBL3896815 | — | — | 3 | 9.40 |
| CHEMBL3944873 | — | — | 3 | 9.30 |
| CHEMBL3904594 | — | — | 3 | 9.15 |
| CHEMBL3978582 | — | — | 3 | 8.89 |
| CHEMBL3973445 | — | — | 3 | 8.85 |
| CHEMBL3952507 | — | — | 3 | 8.70 |
| CHEMBL3960269 | — | — | 3 | 8.66 |
| CHEMBL3907972 | — | — | 3 | 8.64 |
| CHEMBL3907745 | — | — | 3 | 8.44 |
| CHEMBL3965248 | — | — | 3 | 8.30 |
| CHEMBL3967847 | — | — | 3 | 8.17 |
| CHEMBL3900120 | — | — | 3 | 7.90 |
| CHEMBL3922645 | — | — | 3 | 7.85 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3916961 | — | EC50 | = | 0.012 | nM | 10.92 |
| CHEMBL3969143 | — | EC50 | = | 0.1 | nM | 10.00 |
| CHEMBL3986059 | — | EC50 | = | 0.1 | nM | 10.00 |
| CHEMBL3930515 | — | EC50 | = | 0.1 | nM | 10.00 |
| CHEMBL3923975 | — | EC50 | = | 0.1 | nM | 10.00 |
| CHEMBL3959070 | — | EC50 | = | 0.1 | nM | 10.00 |
| CHEMBL3939497 | — | EC50 | = | 0.1 | nM | 10.00 |
| CHEMBL3911527 | — | EC50 | = | 0.1 | nM | 10.00 |
| CHEMBL3984990 | — | EC50 | = | 0.2 | nM | 9.70 |
| CHEMBL3936019 | — | EC50 | = | 0.2 | nM | 9.70 |
| CHEMBL3890700 | — | EC50 | = | 0.2 | nM | 9.70 |
| CHEMBL3948274 | — | EC50 | = | 0.2 | nM | 9.70 |
| CHEMBL3897028 | — | EC50 | = | 0.2 | nM | 9.70 |
| CHEMBL3950364 | — | EC50 | = | 0.3 | nM | 9.52 |
| CHEMBL3902519 | — | EC50 | = | 0.3 | nM | 9.52 |
| CHEMBL3928063 | — | EC50 | = | 0.3 | nM | 9.52 |
| CHEMBL3982418 | — | EC50 | = | 0.3 | nM | 9.52 |
| CHEMBL3896815 | — | EC50 | = | 0.4 | nM | 9.40 |
| CHEMBL3944873 | — | EC50 | = | 0.5 | nM | 9.30 |
| CHEMBL3904594 | — | EC50 | = | 0.7 | nM | 9.15 |
| CHEMBL3978582 | — | EC50 | = | 1.3 | nM | 8.89 |
| CHEMBL3973445 | — | EC50 | = | 1.4 | nM | 8.85 |
| CHEMBL3952507 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3960269 | — | EC50 | = | 2.2 | nM | 8.66 |
| CHEMBL3907972 | — | EC50 | = | 2.3 | nM | 8.64 |
| CHEMBL3907745 | — | EC50 | = | 3.6 | nM | 8.44 |
| CHEMBL3965248 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3967847 | — | EC50 | = | 6.8 | nM | 8.17 |
| CHEMBL3900120 | — | EC50 | = | 12.7 | nM | 7.90 |
| CHEMBL3922645 | — | EC50 | = | 14.1 | nM | 7.85 |
| CHEMBL3978582 | — | kon | = | - | — | - |
| CHEMBL3967847 | — | k_off | = | - | s-1 | - |
| CHEMBL3904594 | — | k_off | = | - | s-1 | - |
| CHEMBL3904594 | — | kon | = | - | — | - |
| CHEMBL3960269 | — | kon | = | - | — | - |
| CHEMBL3986059 | — | k_off | = | - | s-1 | - |
| CHEMBL3986059 | — | kon | = | - | — | - |
| CHEMBL3984990 | — | kon | = | - | — | - |
| CHEMBL3952507 | — | k_off | = | - | s-1 | - |
| CHEMBL3952507 | — | kon | = | - | — | - |
| CHEMBL3960269 | — | k_off | = | - | s-1 | - |
| CHEMBL3922645 | — | kon | = | - | — | - |
| CHEMBL3928063 | — | k_off | = | - | s-1 | - |
| CHEMBL3967847 | — | kon | = | - | — | - |
| CHEMBL3922645 | — | k_off | = | - | s-1 | - |
| CHEMBL3928063 | — | kon | = | - | — | - |
| CHEMBL3900120 | — | k_off | = | - | s-1 | - |
| CHEMBL3900120 | — | kon | = | - | — | - |
| CHEMBL3959070 | — | kon | = | - | — | - |
| CHEMBL3959070 | — | k_off | = | - | s-1 | - |