Assay Detail
Binding
CHEMBL3383457
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of N-terminally MBP-fused human CYP24A1 by cell-free assay
28
Total Activities
14
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
Novel styryl-indoles as small molecule inhibitors of 25-hydroxyvitamin D-24-hydroxylase (CYP24A1): Synthesis and biological evaluation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 5.77 | 6.72 |
| Ki | 14 | 6.92 | 7.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3344395 | — | — | 2 | 7.85 |
| CHEMBL3344394 | — | — | 2 | 7.85 |
| CHEMBL3344392 | — | — | 2 | 7.58 |
| CHEMBL3344393 | — | — | 2 | 7.51 |
| CHEMBL157101 | KETOCONAZOLE | 4.0 | 2 | 7.46 |
| CHEMBL3344397 | — | — | 2 | 7.43 |
| CHEMBL3344396 | — | — | 2 | 7.43 |
| CHEMBL3344400 | — | — | 2 | 6.64 |
| CHEMBL3344398 | — | — | 2 | 6.47 |
| CHEMBL3344402 | — | — | 2 | 6.27 |
| CHEMBL3344403 | — | — | 2 | 6.19 |
| CHEMBL3344399 | — | — | 2 | 6.14 |
| CHEMBL3344401 | — | — | 2 | 6.13 |
| CHEMBL3344404 | — | — | 2 | 5.92 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3344394 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL3344395 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL3344392 | — | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL3344393 | — | Ki | = | 31.0 | nM | 7.51 |
| CHEMBL157101 | KETOCONAZOLE | Ki | = | 35.0 | nM | 7.46 |
| CHEMBL3344397 | — | Ki | = | 37.0 | nM | 7.43 |
| CHEMBL3344396 | — | Ki | = | 37.0 | nM | 7.43 |
| CHEMBL3344395 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL3344394 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL3344400 | — | Ki | = | 230.0 | nM | 6.64 |
| CHEMBL3344398 | — | Ki | = | 340.0 | nM | 6.47 |
| CHEMBL3344392 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL3344393 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL157101 | KETOCONAZOLE | IC50 | = | 470.0 | nM | 6.33 |
| CHEMBL3344397 | — | IC50 | = | 520.0 | nM | 6.28 |
| CHEMBL3344396 | — | IC50 | = | 520.0 | nM | 6.28 |
| CHEMBL3344402 | — | Ki | = | 540.0 | nM | 6.27 |
| CHEMBL3344403 | — | Ki | = | 640.0 | nM | 6.19 |
| CHEMBL3344399 | — | Ki | = | 730.0 | nM | 6.14 |
| CHEMBL3344401 | — | Ki | = | 740.0 | nM | 6.13 |
| CHEMBL3344404 | — | Ki | = | 1190.0 | nM | 5.92 |
| CHEMBL3344400 | — | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL3344398 | — | IC50 | = | 4800.0 | nM | 5.32 |
| CHEMBL3344402 | — | IC50 | = | 7600.0 | nM | 5.12 |
| CHEMBL3344403 | — | IC50 | = | 9000.0 | nM | 5.05 |
| CHEMBL3344401 | — | IC50 | = | 10500.0 | nM | 4.98 |
| CHEMBL3344399 | — | IC50 | = | 10400.0 | nM | 4.98 |
| CHEMBL3344404 | — | IC50 | = | 16900.0 | nM | 4.77 |