Assay Detail
Binding
CHEMBL5732889
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition Assay: The expression plasmids contains the ORF for either human/cyno CYP11B1 or CYP11B2 under the control of a suitable promoter (CMV-promoter) and a suitable resistance marker (neomycin). Using standard techniques the expression plasmid is transfected into G-402 cells and these cells are then selected for expressing the given resistance markers. Individual cell-clones are then selected and assessed for displaying the desired enzymatic activity using 11-Deoxycorticosterone (Cyp11B2) or 11-Deoxycortisol (Cyp11B1) as a substrate.G-402 cells expressing CYP11 constructs were established as described above and maintained in McCoy's 5a Medium Modified, ATCC Catalog No. 30-2007 containing 10% FCS and 400 μg/ml G418 (Geneticin) at 37° C. under an atmosphere of 5% CO2/95% air. 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.
78
Total Activities
23
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 pyrazolyl compounds
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 26 | 10.65 | 10.92 |
| kon | 26 | - | - |
| k_off | 26 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5767596 | — | — | 6 | 10.92 |
| CHEMBL5877749 | — | — | 3 | 10.92 |
| CHEMBL5960934 | — | — | 3 | 10.85 |
| CHEMBL5870745 | — | — | 3 | 10.82 |
| CHEMBL5760532 | — | — | 3 | 10.80 |
| CHEMBL5848123 | — | — | 3 | 10.77 |
| CHEMBL5840628 | — | — | 3 | 10.72 |
| CHEMBL5816213 | — | — | 6 | 10.70 |
| CHEMBL6039670 | — | — | 3 | 10.55 |
| CHEMBL5919201 | — | — | 3 | 10.55 |
| CHEMBL5843772 | — | — | 3 | 10.54 |
| CHEMBL5867538 | — | — | 3 | 10.42 |
| CHEMBL5773604 | — | — | 3 | 10.30 |
| CHEMBL6043991 | — | — | 3 | 10.19 |
| CHEMBL5757854 | — | — | 3 | - |
| CHEMBL5762046 | — | — | 3 | - |
| CHEMBL6034791 | — | — | 3 | - |
| CHEMBL5972697 | — | — | 6 | - |
| CHEMBL6026082 | — | — | 3 | - |
| CHEMBL5991777 | — | — | 3 | - |
| CHEMBL5985475 | — | — | 3 | - |
| CHEMBL6006147 | — | — | 3 | - |
| CHEMBL5835870 | — | — | 3 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5877749 | — | EC50 | = | 0.012 | nM | 10.92 |
| CHEMBL5767596 | — | EC50 | = | 0.012 | nM | 10.92 |
| CHEMBL5960934 | — | EC50 | = | 0.014 | nM | 10.85 |
| CHEMBL5870745 | — | EC50 | = | 0.015 | nM | 10.82 |
| CHEMBL5760532 | — | EC50 | = | 0.016 | nM | 10.80 |
| CHEMBL5848123 | — | EC50 | = | 0.017 | nM | 10.77 |
| CHEMBL5840628 | — | EC50 | = | 0.019 | nM | 10.72 |
| CHEMBL5816213 | — | EC50 | = | 0.02 | nM | 10.70 |
| CHEMBL6039670 | — | EC50 | = | 0.028 | nM | 10.55 |
| CHEMBL5919201 | — | EC50 | = | 0.028 | nM | 10.55 |
| CHEMBL5843772 | — | EC50 | = | 0.029 | nM | 10.54 |
| CHEMBL5867538 | — | EC50 | = | 0.038 | nM | 10.42 |
| CHEMBL5773604 | — | EC50 | = | 0.05 | nM | 10.30 |
| CHEMBL6043991 | — | EC50 | = | 0.064 | nM | 10.19 |
| CHEMBL5991777 | — | EC50 | = | 0.003 | nM | - |
| CHEMBL5972697 | — | kon | = | - | — | - |
| CHEMBL5991777 | — | kon | = | - | — | - |
| CHEMBL5991777 | — | k_off | = | - | s-1 | - |
| CHEMBL6043991 | — | kon | = | - | — | - |
| CHEMBL5773604 | — | k_off | = | - | s-1 | - |
| CHEMBL6043991 | — | k_off | = | - | s-1 | - |
| CHEMBL5773604 | — | kon | = | - | — | - |
| CHEMBL5877749 | — | kon | = | - | — | - |
| CHEMBL5877749 | — | k_off | = | - | s-1 | - |
| CHEMBL6006147 | — | EC50 | = | 0.006 | nM | - |
| CHEMBL6006147 | — | kon | = | - | — | - |
| CHEMBL5848123 | — | kon | = | - | — | - |
| CHEMBL5762046 | — | kon | = | - | — | - |
| CHEMBL5762046 | — | EC50 | = | 0.002 | nM | - |
| CHEMBL5767596 | — | k_off | = | - | s-1 | - |
| CHEMBL5767596 | — | kon | = | - | — | - |
| CHEMBL5972697 | — | k_off | = | - | s-1 | - |
| CHEMBL5757854 | — | kon | = | - | — | - |
| CHEMBL5867538 | — | kon | = | - | — | - |
| CHEMBL5870745 | — | k_off | = | - | s-1 | - |
| CHEMBL6034791 | — | k_off | = | - | s-1 | - |
| CHEMBL6034791 | — | kon | = | - | — | - |
| CHEMBL6034791 | — | EC50 | = | 0.007 | nM | - |
| CHEMBL5843772 | — | k_off | = | - | s-1 | - |
| CHEMBL5843772 | — | kon | = | - | — | - |
| CHEMBL5757854 | — | k_off | = | - | s-1 | - |
| CHEMBL6026082 | — | k_off | = | - | s-1 | - |
| CHEMBL5757854 | — | EC50 | = | 0.007 | nM | - |
| CHEMBL5840628 | — | k_off | = | - | s-1 | - |
| CHEMBL5840628 | — | kon | = | - | — | - |
| CHEMBL5867538 | — | k_off | = | - | s-1 | - |
| CHEMBL5870745 | — | kon | = | - | — | - |
| CHEMBL6006147 | — | k_off | = | - | s-1 | - |
| CHEMBL6026082 | — | EC50 | = | 0.005 | nM | - |
| CHEMBL6026082 | — | kon | = | - | — | - |