Assay Detail
Binding
CHEMBL4683857
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Inhibition of recombinant human CYP1B1 expressed in baculovirus infected insect cells using 7-ethoxyresorufin as substrate preincubated for 5 mins followed by NADPH addition and measured after 15 mins by EROD assay
13
Total Activities
13
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
Design and synthesis of α-naphthoflavone chimera derivatives able to eliminate cytochrome P450 (CYP)1B1-mediated drug resistance via targeted CYP1B1 degradation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 8.02 | 9.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4748722 | — | — | 1 | 9.40 |
| CHEMBL3422338 | — | — | 1 | 9.22 |
| CHEMBL3422257 | — | — | 1 | 8.85 |
| CHEMBL4792004 | — | — | 1 | 8.68 |
| CHEMBL283196 | ALPHA-NAPHTHOFLAVONE | — | 1 | 8.39 |
| CHEMBL4757820 | — | — | 1 | 7.02 |
| CHEMBL4749570 | — | — | 1 | 7.00 |
| CHEMBL4763775 | — | — | 1 | 6.82 |
| CHEMBL4746654 | — | — | 1 | 6.78 |
| CHEMBL4751054 | — | — | 1 | - |
| CHEMBL4787701 | — | — | 1 | - |
| CHEMBL4786434 | — | — | 1 | - |
| CHEMBL4745698 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4748722 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL3422338 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL3422257 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL4792004 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL283196 | ALPHA-NAPHTHOFLAVONE | IC50 | = | 4.1 | nM | 8.39 |
| CHEMBL4757820 | — | IC50 | = | 95.1 | nM | 7.02 |
| CHEMBL4749570 | — | IC50 | = | 101.2 | nM | 7.00 |
| CHEMBL4763775 | — | IC50 | = | 152.7 | nM | 6.82 |
| CHEMBL4746654 | — | IC50 | = | 166.2 | nM | 6.78 |
| CHEMBL4751054 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4787701 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4786434 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4745698 | — | IC50 | > | 10000.0 | nM | - |