Assay Detail
Binding
CHEMBL3383458
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Inhibition of mouse CYP27B1 by cell-free assay
14
Total Activities
7
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Mus musculus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
25-hydroxyvitamin D-1 alpha hydroxylase, mitochondrial (CHEMBL3329080) ↗| Type | SINGLE PROTEIN |
| Organism | Mus musculus |
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 | 7 | 6.74 | 7.00 |
| Ki | 7 | 7.53 | 7.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3344395 | — | — | 2 | 7.77 |
| CHEMBL3344393 | — | — | 2 | 7.66 |
| CHEMBL3344397 | — | — | 2 | 7.62 |
| CHEMBL3344394 | — | — | 2 | 7.60 |
| CHEMBL3344392 | — | — | 2 | 7.47 |
| CHEMBL3344396 | — | — | 2 | 7.34 |
| CHEMBL157101 | KETOCONAZOLE | 4.0 | 2 | 7.24 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3344395 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL3344393 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL3344397 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL3344394 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL3344392 | — | Ki | = | 34.0 | nM | 7.47 |
| CHEMBL3344396 | — | Ki | = | 46.0 | nM | 7.34 |
| CHEMBL157101 | KETOCONAZOLE | Ki | = | 58.0 | nM | 7.24 |
| CHEMBL3344395 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL3344393 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL3344394 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL3344397 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL3344392 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL3344396 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL157101 | KETOCONAZOLE | IC50 | = | 360.0 | nM | 6.44 |