Assay Detail
Binding
CHEMBL4047052
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of N-terminal MBP-tagged human CYP24A1 expressed in Escherichia coli assessed as reduction in hydrolase activity incubated for 25 mins using Adx, AdR and 1,25(OH)2D3
3
Total Activities
3
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
Analysis of the binding sites of vitamin D 1α-hydroxylase (CYP27B1) and vitamin D 24-hydroxylase (CYP24A1) for the design of selective CYP24A1 inhibitors: Homology modelling, molecular dynamics simulations and identification of key binding requirements.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 3 | 5.83 | 6.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL157101 | KETOCONAZOLE | 4.0 | 1 | 6.30 |
| CHEMBL4104395 | — | — | 1 | 5.60 |
| CHEMBL4074768 | — | — | 1 | 5.58 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL157101 | KETOCONAZOLE | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL4104395 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL4074768 | — | IC50 | = | 2600.0 | nM | 5.58 |