Assay Detail
Binding
CHEMBL4330008
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Inhibition of recombinant human CYP1A1 expressed in Escherichia coli membranes co-expressing NADPH-P450 reductase assessed as reduction in ethoxyresorufin O-de-ethylation preincubated for 3 mins followed by NADPH addition and measured after 10 mins by fluorometric method
4
Total Activities
4
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
Adaptable Small Ligand of CYP1 Enzymes for Use in Understanding the Structural Features Determining Isoform Selectivity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 7.10 | 7.39 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4447260 | — | — | 1 | 7.39 |
| CHEMBL283196 | ALPHA-NAPHTHOFLAVONE | — | 1 | 7.26 |
| CHEMBL42428 | — | — | 1 | 7.21 |
| CHEMBL46909 | — | — | 1 | 6.52 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4447260 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL283196 | ALPHA-NAPHTHOFLAVONE | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL42428 | — | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL46909 | — | IC50 | = | 300.0 | nM | 6.52 |