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Assay Detail

CHEMBL5378938

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Agonist activity at full length human RXR alpha expressed in HEK293T cells measured after 16 hrs by Dual-glo luciferase assay
11
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293T
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Retinoic acid receptor RXR-alpha (CHEMBL2061)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structural Fusion of Natural and Synthetic Ligand Features Boosts RXR Agonist Potency.
Adouvi G, Nawa F, Ballarotto M, Rüger LA, Knümann L, Kasch T, Arifi S, Schubert-Zsilavecz M, Willems S, Marschner JA, Pabel J, Merk D.
J Med Chem (2023) 66 : 16762 -16771
PubMed 38064686 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 11 6.77 9.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5404648 2 9.15
CHEMBL5412777 1 7.80
CHEMBL5407623 1 7.66
CHEMBL5436895 1 7.46
CHEMBL5399947 1 6.03
CHEMBL5395851 1 5.92
CHEMBL5394779 1 5.52
CHEMBL5398853 1 4.98
CHEMBL5417665 1 4.89
CHEMBL5423123 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5404648 EC50 = 0.7 nM 9.15
CHEMBL5404648 EC50 = 5.0 nM 8.30
CHEMBL5412777 EC50 = 16.0 nM 7.80
CHEMBL5407623 EC50 = 22.0 nM 7.66
CHEMBL5436895 EC50 = 35.0 nM 7.46
CHEMBL5399947 EC50 = 930.0 nM 6.03
CHEMBL5395851 EC50 = 1200.0 nM 5.92
CHEMBL5394779 EC50 = 3000.0 nM 5.52
CHEMBL5398853 EC50 = 10400.0 nM 4.98
CHEMBL5417665 EC50 = 13000.0 nM 4.89
CHEMBL5423123 EC50 > 10000.0 nM -