Assay Detail
Binding
CHEMBL1768149
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of CYP26A1 in human MCF7 cell microsomes using [3H]ATRA after 1 hr by scintillation counting
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | MCF7 |
| Subcellular | Microsome |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Small molecule inhibitors of retinoic acid 4-hydroxylase (CYP26): synthesis and biological evaluation of imidazole methyl 3-(4-(aryl-2-ylamino)phenyl)propanoates.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 7.59 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1766007 | — | — | 1 | 8.52 |
| CHEMBL1766005 | — | — | 1 | 8.52 |
| CHEMBL1766003 | — | — | 1 | 8.22 |
| CHEMBL1766001 | — | — | 1 | 8.10 |
| CHEMBL1766006 | — | — | 1 | 8.10 |
| CHEMBL1766008 | — | — | 1 | 8.00 |
| CHEMBL1766000 | — | — | 1 | 8.00 |
| CHEMBL517438 | — | — | 1 | 8.00 |
| CHEMBL1766011 | — | — | 1 | 7.58 |
| CHEMBL1766010 | — | — | 1 | 7.40 |
| CHEMBL1766013 | — | — | 1 | 7.30 |
| CHEMBL1766009 | — | — | 1 | 7.00 |
| CHEMBL1766004 | — | — | 1 | 6.90 |
| CHEMBL1766012 | — | — | 1 | 6.85 |
| CHEMBL1766002 | — | — | 1 | 6.60 |
| CHEMBL389433 | LIAROZOLE | 2.0 | 1 | 6.27 |
| CHEMBL1766014 | — | — | 1 | - |
| CHEMBL1766015 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1766007 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL1766005 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL1766003 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL1766001 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL1766006 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL1766008 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL1766000 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL517438 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL1766011 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL1766010 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL1766013 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL1766009 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL1766004 | — | IC50 | = | 125.0 | nM | 6.90 |
| CHEMBL1766012 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL1766002 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL389433 | LIAROZOLE | IC50 | = | 540.0 | nM | 6.27 |
| CHEMBL1766014 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL1766015 | — | IC50 | > | 1000.0 | nM | - |