Assay Detail
Binding
CHEMBL4275702
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Transactivation of recombinant human VDR/RXRalpha expressed in HEK293 cells after 24 hrs by Dual-luciferase reporter gene assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 7 — Homologous single protein target |
| Curated By | Intermediate |
Target
Retinoic acid receptor RXR-alpha/Vitamin D3 receptor (CHEMBL3885632) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
Sulfonyl-containing phenyl-pyrrolyl pentane analogues: Novel non-secosteroidal vitamin D receptor modulators with favorable physicochemical properties, pharmacokinetic properties and anti-tumor activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 4 | 8.15 | 8.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL846 | CALCITRIOL | 4.0 | 1 | 8.80 |
| CHEMBL4288947 | — | — | 1 | 8.19 |
| CHEMBL2434990 | — | — | 1 | 8.17 |
| CHEMBL4290851 | — | — | 1 | 7.42 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL846 | CALCITRIOL | EC50 | = | 1.58 | nM | 8.80 |
| CHEMBL4288947 | — | EC50 | = | 6.41 | nM | 8.19 |
| CHEMBL2434990 | — | EC50 | = | 6.81 | nM | 8.17 |
| CHEMBL4290851 | — | EC50 | = | 38.2 | nM | 7.42 |