Assay Detail
Binding
CHEMBL4430346
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Agonist activity at human RXR binding domain and activation domain expressed in human HCT116 cells assessed as rexinoid activity incubated for 24 hrs by luciferase reporter gene based mammalian two-hybrid assay
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Publication
Modeling, Synthesis, and Biological Evaluation of Potential Retinoid X Receptor (RXR)-Selective Agonists: Analogues of 4-[1-(3,5,5,8,8-Pentamethyl-5,6,7,8-tetrahydro-2-naphthyl)ethynyl]benzoic Acid (Bexarotene) and 6-(Ethyl(5,5,8,8-tetrahydronaphthalen-2-yl)amino)nicotinic Acid (NEt-TMN).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 13 | 7.10 | 8.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4547228 | — | — | 1 | 8.10 |
| CHEMBL4459731 | — | — | 1 | 7.86 |
| CHEMBL1221641 | — | — | 1 | 7.86 |
| CHEMBL4545837 | — | — | 1 | 7.74 |
| CHEMBL4476213 | — | — | 1 | 7.47 |
| CHEMBL4574155 | — | — | 1 | 7.39 |
| CHEMBL1023 | BEXAROTENE | 4.0 | 1 | 7.28 |
| CHEMBL4560758 | — | — | 1 | 6.90 |
| CHEMBL4475014 | — | — | 1 | 6.84 |
| CHEMBL4440825 | — | — | 1 | 6.53 |
| CHEMBL4468317 | — | — | 1 | 6.44 |
| CHEMBL4476114 | — | — | 1 | 4.74 |
| CHEMBL4441103 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4547228 | — | EC50 | = | 7.9 | nM | 8.10 |
| CHEMBL4459731 | — | EC50 | = | 13.8 | nM | 7.86 |
| CHEMBL1221641 | — | EC50 | = | 13.8 | nM | 7.86 |
| CHEMBL4545837 | — | EC50 | = | 18.2 | nM | 7.74 |
| CHEMBL4476213 | — | EC50 | = | 33.8 | nM | 7.47 |
| CHEMBL4574155 | — | EC50 | = | 40.9 | nM | 7.39 |
| CHEMBL1023 | BEXAROTENE | EC50 | = | 52.0 | nM | 7.28 |
| CHEMBL4560758 | — | EC50 | = | 125.6 | nM | 6.90 |
| CHEMBL4475014 | — | EC50 | = | 143.4 | nM | 6.84 |
| CHEMBL4440825 | — | EC50 | = | 295.5 | nM | 6.53 |
| CHEMBL4468317 | — | EC50 | = | 364.3 | nM | 6.44 |
| CHEMBL4476114 | — | EC50 | = | 18200.0 | nM | 4.74 |
| CHEMBL4441103 | — | EC50 | > | 80000.0 | nM | - |