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Assay Detail

CHEMBL5527748

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

Binding
Agonist activity at Gal4-fused human RXRalpha transfected in HEK293T cells incubated for 16 hrs by firefly/renilla based Dual-Glo luciferase assay
8
Total Activities
8
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 Optimization of Oxaprozin for Selective Inverse Nurr1 Agonism.
Willems S, Busch R, Nawa F, Ballarotto M, Lillich FF, Kasch T, López-García Ú, Marschner JA, Rüger LA, Renelt B, Ohrndorf J, Arifi S, Zaienne D, Proschak E, Pabel J, Merk D.
J Med Chem (2024) 67 : 13324 -13348
PubMed 39081058 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 8 5.31 6.03

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5399947 1 6.03
CHEMBL5395851 1 5.92
CHEMBL5394779 1 5.52
CHEMBL5567943 1 5.40
CHEMBL5558226 1 5.25
CHEMBL5398853 1 4.98
CHEMBL5417665 1 4.89
CHEMBL5567959 1 4.48

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5399947 EC50 = 930.0 nM 6.03
CHEMBL5395851 EC50 = 1200.0 nM 5.92
CHEMBL5394779 EC50 = 3000.0 nM 5.52
CHEMBL5567943 EC50 = 4000.0 nM 5.40
CHEMBL5558226 EC50 = 5600.0 nM 5.25
CHEMBL5398853 EC50 = 10400.0 nM 4.98
CHEMBL5417665 EC50 = 13000.0 nM 4.89
CHEMBL5567959 EC50 = 33000.0 nM 4.48