Assay Detail
Binding
CHEMBL4181948
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human CYP1B1 expressed in yeast microsomal membranes using 7-ethoxyresorufin as substrate measured after 10 mins by fluorescence assay
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
(E)-3-(3,4,5-Trimethoxyphenyl)-1-(pyridin-4-yl)prop-2-en-1-one, a heterocyclic chalcone is a potent and selective CYP1A1 inhibitor and cancer chemopreventive agent.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 6.29 | 7.50 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2237710 | — | — | 1 | 7.50 |
| CHEMBL4214111 | — | — | 1 | 7.39 |
| CHEMBL4209004 | — | — | 1 | 7.32 |
| CHEMBL283196 | ALPHA-NAPHTHOFLAVONE | — | 1 | 7.30 |
| CHEMBL4212722 | — | — | 1 | 7.27 |
| CHEMBL4202990 | — | — | 1 | 6.77 |
| CHEMBL1568243 | — | — | 1 | 6.19 |
| CHEMBL4213815 | — | — | 1 | 6.16 |
| CHEMBL4210776 | — | — | 1 | 5.68 |
| CHEMBL4210137 | — | — | 1 | 5.54 |
| CHEMBL4205073 | — | — | 1 | 5.42 |
| CHEMBL4218749 | — | — | 1 | 5.28 |
| CHEMBL2237704 | — | — | 1 | 5.16 |
| CHEMBL4211876 | — | — | 1 | 5.06 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2237710 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL4214111 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL4209004 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL283196 | ALPHA-NAPHTHOFLAVONE | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL4212722 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL4202990 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL1568243 | — | IC50 | = | 650.0 | nM | 6.19 |
| CHEMBL4213815 | — | IC50 | = | 698.0 | nM | 6.16 |
| CHEMBL4210776 | — | IC50 | = | 2110.0 | nM | 5.68 |
| CHEMBL4210137 | — | IC50 | = | 2920.0 | nM | 5.54 |
| CHEMBL4205073 | — | IC50 | = | 3810.0 | nM | 5.42 |
| CHEMBL4218749 | — | IC50 | = | 5210.0 | nM | 5.28 |
| CHEMBL2237704 | — | IC50 | = | 7000.0 | nM | 5.16 |
| CHEMBL4211876 | — | IC50 | = | 8620.0 | nM | 5.06 |