Assay Detail
Binding
CHEMBL4055735
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of MBP-tagged human CYP24A1 expressed Escherichia coli BL21-Gold(DE3) incubated for 25 mins in presence of Adx, AdR 1,25(OH)2D3 and NADPH by HPLC method
12
Total Activities
12
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 |
Target
1,25-dihydroxyvitamin D(3) 24-hydroxylase, mitochondrial (CHEMBL4521) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Synthesis, molecular modelling and CYP24A1 inhibitory activity of novel of (E)-N-(2-(1H-imidazol-1-yl)-2-(phenylethyl)-3/4-styrylbenzamides.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 6.70 | 6.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3329769 | — | — | 1 | 6.96 |
| CHEMBL4105510 | — | — | 1 | 6.96 |
| CHEMBL4080128 | — | — | 1 | 6.92 |
| CHEMBL4066700 | — | — | 1 | 6.82 |
| CHEMBL4087998 | — | — | 1 | 6.80 |
| CHEMBL4103700 | — | — | 1 | 6.75 |
| CHEMBL4104362 | — | — | 1 | 6.72 |
| CHEMBL4087325 | — | — | 1 | 6.68 |
| CHEMBL4076840 | — | — | 1 | 6.51 |
| CHEMBL4060725 | — | — | 1 | 6.47 |
| CHEMBL4079445 | — | — | 1 | 6.46 |
| CHEMBL157101 | KETOCONAZOLE | 4.0 | 1 | 6.30 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3329769 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL4105510 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL4080128 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL4066700 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL4087998 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL4103700 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL4104362 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL4087325 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL4076840 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL4060725 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL4079445 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL157101 | KETOCONAZOLE | IC50 | = | 500.0 | nM | 6.30 |