Assay Detail
Binding
CHEMBL3369890
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human MBP-tagged CYP24A1 expressed in Escherichia coli using 1,25(OH)2D3 substrate in presence of bovine adrenodoxin, adrenodoxin reductase and NADPH incubated at 37 degC for 25 mins by HPLC method
37
Total Activities
22
Compounds Tested
2
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
Small-molecule inhibitors of 25-hydroxyvitamin D-24-hydroxylase (CYP24A1): synthesis and biological evaluation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 6.61 | 8.64 |
| Ki | 18 | 7.39 | 8.11 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL389433 | LIAROZOLE | 2.0 | 1 | 8.64 |
| CHEMBL389014 | — | — | 1 | 8.19 |
| CHEMBL3329769 | — | — | 2 | 8.11 |
| CHEMBL3329770 | — | — | 2 | 8.01 |
| CHEMBL3329774 | — | — | 2 | 7.96 |
| CHEMBL3329778 | — | — | 2 | 7.89 |
| CHEMBL1170908 | — | — | 1 | 7.82 |
| CHEMBL3329767 | — | — | 2 | 7.72 |
| CHEMBL3360784 | — | — | 1 | 7.68 |
| CHEMBL3329768 | — | — | 2 | 7.62 |
| CHEMBL2105705 | LUNACALCIPOL | 2.0 | 1 | 7.57 |
| CHEMBL1171494 | — | — | 2 | 7.55 |
| CHEMBL157101 | KETOCONAZOLE | 4.0 | 2 | 7.48 |
| CHEMBL3329771 | — | — | 2 | 7.44 |
| CHEMBL3360783 | — | — | 1 | 7.41 |
| CHEMBL3329779 | — | — | 2 | 7.38 |
| CHEMBL3360785 | — | — | 1 | 7.38 |
| CHEMBL3329772 | — | — | 2 | 7.04 |
| CHEMBL3329773 | — | — | 2 | 6.82 |
| CHEMBL3329777 | — | — | 2 | 6.68 |
| CHEMBL3329776 | — | — | 2 | 6.42 |
| CHEMBL3329775 | — | — | 2 | 6.40 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL389433 | LIAROZOLE | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL389014 | — | IC50 | = | 6.5 | nM | 8.19 |
| CHEMBL3329769 | — | Ki | = | 7.8 | nM | 8.11 |
| CHEMBL3329770 | — | Ki | = | 9.7 | nM | 8.01 |
| CHEMBL3329774 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL3329778 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL1170908 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3329767 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL3360784 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL3329768 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL2105705 | LUNACALCIPOL | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL1171494 | — | Ki | = | 28.0 | nM | 7.55 |
| CHEMBL157101 | KETOCONAZOLE | Ki | = | 33.0 | nM | 7.48 |
| CHEMBL3329771 | — | Ki | = | 36.0 | nM | 7.44 |
| CHEMBL3360783 | — | Ki | = | 39.0 | nM | 7.41 |
| CHEMBL3329779 | — | Ki | = | 42.0 | nM | 7.38 |
| CHEMBL3360785 | — | Ki | = | 42.0 | nM | 7.38 |
| CHEMBL3329772 | — | Ki | = | 91.0 | nM | 7.04 |
| CHEMBL3329769 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL3329770 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL3329773 | — | Ki | = | 150.0 | nM | 6.82 |
| CHEMBL3329774 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL3329778 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL3329777 | — | Ki | = | 210.0 | nM | 6.68 |
| CHEMBL3329767 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL3329768 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL3329776 | — | Ki | = | 380.0 | nM | 6.42 |
| CHEMBL3329775 | — | Ki | = | 400.0 | nM | 6.40 |
| CHEMBL1171494 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL157101 | KETOCONAZOLE | IC50 | = | 470.0 | nM | 6.33 |
| CHEMBL3329771 | — | IC50 | = | 510.0 | nM | 6.29 |
| CHEMBL3329779 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL3329772 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL3329773 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL3329777 | — | IC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL3329776 | — | IC50 | = | 5400.0 | nM | 5.27 |
| CHEMBL3329775 | — | IC50 | = | 5600.0 | nM | 5.25 |