Assay Detail
Binding
CHEMBL5733872
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Inhibition Assay: Eighteen compounds were tested as potential inhibitors of CYP26A1 and CYP26B1. The formation of 9-cis-4-OH-RA metabolite was monitored and the percent activity remaining in the presence of the inhibitor in comparison to the solvent only control was quantified.
48
Total Activities
16
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Specific inhibitors of cytochrome P450 26 retinoic acid hydroxylase
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 5.55 | 8.37 |
| kon | 16 | - | - |
| k_off | 16 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5785788 | — | — | 3 | 8.37 |
| CHEMBL459505 | TALAROZOLE | 2.0 | 3 | 8.29 |
| CHEMBL157101 | KETOCONAZOLE | 4.0 | 3 | 6.18 |
| CHEMBL389433 | LIAROZOLE | 2.0 | 3 | 5.72 |
| CHEMBL3785511 | — | — | 3 | 5.49 |
| CHEMBL6054609 | — | — | 3 | 5.41 |
| CHEMBL3787564 | — | — | 3 | 5.36 |
| CHEMBL275311 | — | — | 3 | 5.25 |
| CHEMBL69367 | — | — | 3 | 5.19 |
| CHEMBL1201375 | TAZAROTENIC ACID | -1.0 | 3 | 5.12 |
| CHEMBL5755195 | — | — | 3 | 5.00 |
| CHEMBL451835 | — | — | 3 | 4.98 |
| CHEMBL25202 | TAMIBAROTENE | 4.0 | 3 | 4.88 |
| CHEMBL4216904 | — | — | 3 | 4.83 |
| CHEMBL4792252 | — | — | 3 | 4.40 |
| CHEMBL6018534 | — | — | 3 | 4.37 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5785788 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL459505 | TALAROZOLE | IC50 | = | 5.1 | nM | 8.29 |
| CHEMBL157101 | KETOCONAZOLE | IC50 | = | 660.0 | nM | 6.18 |
| CHEMBL389433 | LIAROZOLE | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL3785511 | — | IC50 | = | 3250.0 | nM | 5.49 |
| CHEMBL6054609 | — | IC50 | = | 3900.0 | nM | 5.41 |
| CHEMBL3787564 | — | IC50 | = | 4400.0 | nM | 5.36 |
| CHEMBL275311 | — | IC50 | = | 5600.0 | nM | 5.25 |
| CHEMBL69367 | — | IC50 | = | 6500.0 | nM | 5.19 |
| CHEMBL1201375 | TAZAROTENIC ACID | IC50 | = | 7600.0 | nM | 5.12 |
| CHEMBL5755195 | — | IC50 | = | 9900.0 | nM | 5.00 |
| CHEMBL451835 | — | IC50 | = | 10500.0 | nM | 4.98 |
| CHEMBL25202 | TAMIBAROTENE | IC50 | = | 13050.0 | nM | 4.88 |
| CHEMBL4216904 | — | IC50 | = | 14800.0 | nM | 4.83 |
| CHEMBL4792252 | — | IC50 | = | 40200.0 | nM | 4.40 |
| CHEMBL6018534 | — | IC50 | = | 42500.0 | nM | 4.37 |
| CHEMBL157101 | KETOCONAZOLE | kon | = | - | — | - |
| CHEMBL157101 | KETOCONAZOLE | k_off | = | - | s-1 | - |
| CHEMBL459505 | TALAROZOLE | kon | = | - | — | - |
| CHEMBL459505 | TALAROZOLE | k_off | = | - | s-1 | - |
| CHEMBL5785788 | — | kon | = | - | — | - |
| CHEMBL5785788 | — | k_off | = | - | s-1 | - |
| CHEMBL25202 | TAMIBAROTENE | kon | = | - | — | - |
| CHEMBL6054609 | — | kon | = | - | — | - |
| CHEMBL69367 | — | kon | = | - | — | - |
| CHEMBL69367 | — | k_off | = | - | s-1 | - |
| CHEMBL275311 | — | kon | = | - | — | - |
| CHEMBL275311 | — | k_off | = | - | s-1 | - |
| CHEMBL3787564 | — | kon | = | - | — | - |
| CHEMBL3787564 | — | k_off | = | - | s-1 | - |
| CHEMBL3785511 | — | kon | = | - | — | - |
| CHEMBL3785511 | — | k_off | = | - | s-1 | - |
| CHEMBL389433 | LIAROZOLE | k_off | = | - | s-1 | - |
| CHEMBL389433 | LIAROZOLE | kon | = | - | — | - |
| CHEMBL25202 | TAMIBAROTENE | k_off | = | - | s-1 | - |
| CHEMBL5755195 | — | kon | = | - | — | - |
| CHEMBL6018534 | — | k_off | = | - | s-1 | - |
| CHEMBL6018534 | — | kon | = | - | — | - |
| CHEMBL451835 | — | k_off | = | - | s-1 | - |
| CHEMBL451835 | — | kon | = | - | — | - |
| CHEMBL1201375 | TAZAROTENIC ACID | k_off | = | - | s-1 | - |
| CHEMBL1201375 | TAZAROTENIC ACID | kon | = | - | — | - |
| CHEMBL4216904 | — | k_off | = | - | s-1 | - |
| CHEMBL4216904 | — | kon | = | - | — | - |
| CHEMBL6054609 | — | k_off | = | - | s-1 | - |
| CHEMBL4792252 | — | k_off | = | - | s-1 | - |
| CHEMBL5755195 | — | k_off | = | - | s-1 | - |
| CHEMBL4792252 | — | kon | = | - | — | - |