Assay Detail
Functional
CHEMBL1696021
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at RXRalpha transfected in human COS1 cells after 18 hrs by luciferase reporter gene transactivation assay
20
Total Activities
15
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Cell Type | COS-1 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Modification at the Lipophilic Domain of RXR Agonists Differentially Influences Activation of RXR Heterodimers.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 15 | 6.92 | 8.28 |
| Activity | 5 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1221641 | — | — | 2 | 8.28 |
| CHEMBL1688383 | — | — | 2 | 7.72 |
| CHEMBL1023 | BEXAROTENE | 4.0 | 1 | 7.70 |
| CHEMBL1688382 | — | — | 1 | 7.18 |
| CHEMBL1688385 | — | — | 1 | 6.96 |
| CHEMBL1688386 | — | — | 1 | 6.80 |
| CHEMBL1688387 | — | — | 1 | 6.80 |
| CHEMBL1688390 | — | — | 2 | 6.80 |
| CHEMBL1688392 | — | — | 2 | 6.80 |
| CHEMBL1688389 | — | — | 1 | 6.75 |
| CHEMBL1688391 | — | — | 1 | 6.55 |
| CHEMBL1688384 | — | — | 2 | 6.54 |
| CHEMBL1688393 | — | — | 1 | 6.48 |
| CHEMBL1688388 | — | — | 1 | 6.35 |
| CHEMBL1688394 | — | — | 1 | 6.09 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1221641 | — | EC50 | = | 5.3 | nM | 8.28 |
| CHEMBL1688383 | — | EC50 | = | 19.0 | nM | 7.72 |
| CHEMBL1023 | BEXAROTENE | EC50 | = | 20.0 | nM | 7.70 |
| CHEMBL1688382 | — | EC50 | = | 66.0 | nM | 7.18 |
| CHEMBL1688385 | — | EC50 | = | 110.0 | nM | 6.96 |
| CHEMBL1688390 | — | EC50 | = | 160.0 | nM | 6.80 |
| CHEMBL1688392 | — | EC50 | = | 160.0 | nM | 6.80 |
| CHEMBL1688387 | — | EC50 | = | 160.0 | nM | 6.80 |
| CHEMBL1688386 | — | EC50 | = | 160.0 | nM | 6.80 |
| CHEMBL1688389 | — | EC50 | = | 180.0 | nM | 6.75 |
| CHEMBL1688391 | — | EC50 | = | 280.0 | nM | 6.55 |
| CHEMBL1688384 | — | EC50 | = | 290.0 | nM | 6.54 |
| CHEMBL1688393 | — | EC50 | = | 330.0 | nM | 6.48 |
| CHEMBL1688388 | — | EC50 | = | 450.0 | nM | 6.35 |
| CHEMBL1688394 | — | EC50 | = | 820.0 | nM | 6.09 |
| CHEMBL1221641 | — | Activity | - | — | - | |
| CHEMBL1688383 | — | Activity | - | — | - | |
| CHEMBL1688384 | — | Activity | - | — | - | |
| CHEMBL1688390 | — | Activity | - | — | - | |
| CHEMBL1688392 | — | Activity | - | — | - |