Assay Detail
Binding
CHEMBL4418432
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of CYP8B1 in human liver microsomes using D7-7alpha-hydroxy-4-cholesten-3-one as substrate preincubated for 20 mins followed by substrate addition in presence of NADPH by UPLC-ESI-MS/MS analysis
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Tissue | Liver |
| Subcellular | Microsomes |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
7-alpha-hydroxycholest-4-en-3-one 12-alpha-hydroxylase (CHEMBL4523494) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Cyp8b1 and uses thereof in therapeutic and diagnostic methods
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 5.63 | 6.51 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL808 | ECONAZOLE | 4.0 | 1 | 6.51 |
| CHEMBL104 | CLOTRIMAZOLE | 4.0 | 1 | 6.10 |
| CHEMBL91 | MICONAZOLE | 4.0 | 1 | 5.82 |
| CHEMBL157101 | KETOCONAZOLE | 4.0 | 1 | 5.66 |
| CHEMBL4442751 | — | — | 1 | 5.58 |
| CHEMBL1397 | POSACONAZOLE | 4.0 | 1 | 5.42 |
| CHEMBL64391 | ITRACONAZOLE | 4.0 | 1 | 5.33 |
| CHEMBL4468145 | — | — | 1 | 5.12 |
| CHEMBL3989843 | TRANYLCYPROMINE | 4.0 | 1 | 5.11 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL808 | ECONAZOLE | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL104 | CLOTRIMAZOLE | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL91 | MICONAZOLE | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL157101 | KETOCONAZOLE | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL4442751 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL1397 | POSACONAZOLE | IC50 | = | 3800.0 | nM | 5.42 |
| CHEMBL64391 | ITRACONAZOLE | IC50 | = | 4700.0 | nM | 5.33 |
| CHEMBL4468145 | — | IC50 | = | 7600.0 | nM | 5.12 |
| CHEMBL3989843 | TRANYLCYPROMINE | IC50 | = | 7800.0 | nM | 5.11 |