Assay Detail
Binding
CHEMBL4330009
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human CYP1A2 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 | 7.35 | 8.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4447260 | — | — | 1 | 8.82 |
| CHEMBL42428 | — | — | 1 | 7.96 |
| CHEMBL283196 | ALPHA-NAPHTHOFLAVONE | — | 1 | 7.12 |
| CHEMBL46909 | — | — | 1 | 5.51 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4447260 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL42428 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL283196 | ALPHA-NAPHTHOFLAVONE | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL46909 | — | IC50 | = | 3100.0 | nM | 5.51 |