Assay Detail
Binding
CHEMBL1011986
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Activity at human RARbeta ligand binding domain expressed in COS7 cells co-transfected with Gal4-DBD assessed as transcriptional activation after 16 hrs by Gal4 response element-driven luciferase reporter gene assay
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | COS-7 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Novel non-carboxylic acid retinoids: 1,2,4-oxadiazol-5-one derivatives.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 10 | 8.04 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL451835 | — | — | 1 | 9.52 |
| CHEMBL1657 | TAZAROTENE | 4.0 | 1 | 9.10 |
| CHEMBL69367 | — | — | 1 | 8.07 |
| CHEMBL457775 | — | — | 1 | 8.00 |
| CHEMBL38 | TRETINOIN | 4.0 | 1 | 7.92 |
| CHEMBL468608 | — | — | 1 | 7.58 |
| CHEMBL511855 | — | — | 1 | 6.09 |
| CHEMBL468607 | — | — | 1 | - |
| CHEMBL467748 | — | — | 1 | - |
| CHEMBL468623 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL451835 | — | EC50 | = | 0.3 | nM | 9.52 |
| CHEMBL1657 | TAZAROTENE | EC50 | = | 0.8 | nM | 9.10 |
| CHEMBL69367 | — | EC50 | = | 8.6 | nM | 8.07 |
| CHEMBL457775 | — | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL38 | TRETINOIN | EC50 | = | 12.0 | nM | 7.92 |
| CHEMBL468608 | — | EC50 | = | 26.0 | nM | 7.58 |
| CHEMBL511855 | — | EC50 | = | 820.0 | nM | 6.09 |
| CHEMBL468607 | — | EC50 | > | 1000.0 | nM | - |
| CHEMBL467748 | — | EC50 | > | 1000.0 | nM | - |
| CHEMBL468623 | — | EC50 | > | 1000.0 | nM | - |