Assay Detail
Binding
CHEMBL800653
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Inhibition of binding to human Retinoic acid receptor RXR DEF domain
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Conformationally defined 6-s-trans-retinoic acid analogs. 3. Structure-activity relationships for nuclear receptor binding, transcriptional activity, and cancer chemopreventive activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 10 | 7.68 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL705 | ALITRETINOIN | 4.0 | 1 | 8.52 |
| CHEMBL2114968 | — | — | 1 | 7.80 |
| CHEMBL2111790 | — | — | 1 | 7.48 |
| CHEMBL2111792 | — | — | 1 | 6.92 |
| CHEMBL38 | TRETINOIN | 4.0 | 1 | - |
| CHEMBL122823 | — | — | 1 | - |
| CHEMBL46398 | — | — | 1 | - |
| CHEMBL333032 | — | — | 1 | - |
| CHEMBL2111791 | — | — | 1 | - |
| CHEMBL121659 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL705 | ALITRETINOIN | Kd | = | 3.0 | nM | 8.52 |
| CHEMBL2114968 | — | Kd | = | 16.0 | nM | 7.80 |
| CHEMBL2111790 | — | Kd | = | 33.0 | nM | 7.48 |
| CHEMBL2111792 | — | Kd | = | 120.0 | nM | 6.92 |
| CHEMBL38 | TRETINOIN | Kd | > | 200.0 | nM | - |
| CHEMBL122823 | — | Kd | > | 200.0 | nM | - |
| CHEMBL46398 | — | Kd | > | 200.0 | nM | - |
| CHEMBL333032 | — | Kd | > | 200.0 | nM | - |
| CHEMBL2111791 | — | Kd | > | 200.0 | nM | - |
| CHEMBL121659 | — | Kd | > | 200.0 | nM | - |