Assay Detail
Binding
CHEMBL3789264
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Inhibition of microsomal fraction of human CYP26A1 expressed in Sf9 cells using 9-cis-RA as substrate preincubated for 5 mins followed by NADPH addition measured after 1 min by HPLC analysis in presence of rat P450 reductase
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Development and Characterization of Novel and Selective Inhibitors of Cytochrome P450 CYP26A1, the Human Liver Retinoic Acid Hydroxylase.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 24 | 6.00 | 8.29 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL459505 | TALAROZOLE | 2.0 | 1 | 8.29 |
| CHEMBL3786184 | — | — | 1 | 7.22 |
| CHEMBL3786620 | — | — | 1 | 6.96 |
| CHEMBL3786581 | — | — | 1 | 6.62 |
| CHEMBL3787323 | — | — | 1 | 6.57 |
| CHEMBL3787627 | — | — | 1 | 6.47 |
| CHEMBL323626 | — | — | 1 | 5.89 |
| CHEMBL309282 | — | — | 1 | 5.79 |
| CHEMBL3786324 | — | — | 1 | 5.78 |
| CHEMBL389433 | LIAROZOLE | 2.0 | 1 | 5.72 |
| CHEMBL3785511 | — | — | 1 | 5.55 |
| CHEMBL3787691 | — | — | 1 | 5.46 |
| CHEMBL3787564 | — | — | 1 | 5.40 |
| CHEMBL95949 | — | — | 1 | 5.33 |
| CHEMBL112715 | — | — | 1 | 5.11 |
| CHEMBL3786043 | — | — | 1 | 4.97 |
| CHEMBL1023 | BEXAROTENE | 4.0 | 1 | 4.87 |
| CHEMBL3785701 | — | — | 1 | - |
| CHEMBL101308 | — | — | 1 | - |
| CHEMBL3785624 | — | — | 1 | - |
| CHEMBL3786927 | — | — | 1 | - |
| CHEMBL3785557 | — | — | 1 | - |
| CHEMBL3786340 | — | — | 1 | - |
| CHEMBL3785761 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL459505 | TALAROZOLE | IC50 | = | 5.1 | nM | 8.29 |
| CHEMBL3786184 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL3786620 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL3786581 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL3787323 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL3787627 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL323626 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL309282 | — | IC50 | = | 1630.0 | nM | 5.79 |
| CHEMBL3786324 | — | IC50 | = | 1660.0 | nM | 5.78 |
| CHEMBL389433 | LIAROZOLE | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL3785511 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL3787691 | — | IC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL3787564 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL95949 | — | IC50 | = | 4700.0 | nM | 5.33 |
| CHEMBL112715 | — | IC50 | = | 7800.0 | nM | 5.11 |
| CHEMBL3786043 | — | IC50 | = | 10600.0 | nM | 4.97 |
| CHEMBL1023 | BEXAROTENE | IC50 | = | 13500.0 | nM | 4.87 |
| CHEMBL3785701 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL101308 | — | IC50 | > | 25000.0 | nM | - |
| CHEMBL3785624 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL3786927 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL3785557 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL3786340 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL3785761 | — | IC50 | > | 5000.0 | nM | - |