Assay Detail
ADMET
CHEMBL4009475
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human liver CYP3A4 expressed in Saccharomyces cerevisiae YY7 microsomal membranes using DBF as substrate after 10 mins by fluorescence assay
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | ADMET |
| Organism | Homo sapiens |
| Subcellular | Microsomal Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery and characterization of novel CYP1B1 inhibitors based on heterocyclic chalcones: Overcoming cisplatin resistance in CYP1B1-overexpressing lines.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 4.96 | 5.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4099058 | — | — | 1 | 5.89 |
| CHEMBL4072091 | — | — | 1 | 5.82 |
| CHEMBL4071959 | — | — | 1 | 5.22 |
| CHEMBL4092737 | — | — | 1 | 4.97 |
| CHEMBL427692 | — | — | 1 | 4.96 |
| CHEMBL4087973 | — | — | 1 | 4.96 |
| CHEMBL2237709 | — | — | 1 | 4.93 |
| CHEMBL1413330 | — | — | 1 | 4.92 |
| CHEMBL4065284 | — | — | 1 | 4.90 |
| CHEMBL4084977 | — | — | 1 | 4.85 |
| CHEMBL4068333 | — | — | 1 | 4.82 |
| CHEMBL4059677 | — | — | 1 | 4.75 |
| CHEMBL4080095 | — | — | 1 | 4.58 |
| CHEMBL4063333 | — | — | 1 | 4.55 |
| CHEMBL4063471 | — | — | 1 | 4.28 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4099058 | — | IC50 | = | 1280.0 | nM | 5.89 |
| CHEMBL4072091 | — | IC50 | = | 1520.0 | nM | 5.82 |
| CHEMBL4071959 | — | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL4092737 | — | IC50 | = | 10600.0 | nM | 4.97 |
| CHEMBL427692 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL4087973 | — | IC50 | = | 11100.0 | nM | 4.96 |
| CHEMBL2237709 | — | IC50 | = | 11800.0 | nM | 4.93 |
| CHEMBL1413330 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL4065284 | — | IC50 | = | 12500.0 | nM | 4.90 |
| CHEMBL4084977 | — | IC50 | = | 14000.0 | nM | 4.85 |
| CHEMBL4068333 | — | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL4059677 | — | IC50 | = | 18000.0 | nM | 4.75 |
| CHEMBL4080095 | — | IC50 | = | 26000.0 | nM | 4.58 |
| CHEMBL4063333 | — | IC50 | = | 28000.0 | nM | 4.55 |
| CHEMBL4063471 | — | IC50 | = | 53000.0 | nM | 4.28 |