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Assay Detail

CHEMBL5258381

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

Binding
Binding affinity to human RXRalpha-LBD (224 to 462 residues) expressed in Escherichia coli BL21 (DE3) assessed as dissociation constant using PGC-1alpha as coactivator peptide by isothermal titration calorimetry analysis
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Ligand Screening System for the RXRα Heterodimer Using the Fluorescence RXR Agonist CU-6PMN.
Kawasaki M, Motoyama T, Yamada S, Watanabe M, Fujihara M, Kambe A, Nakano S, Kakuta H, Ito S.
ACS Med Chem Lett (2023) 14 : 291 -296
PubMed 36923911 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 3 6.33 6.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2146901 1 6.55
CHEMBL1688383 1 6.47
CHEMBL4449685 1 5.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2146901 Kd = 280.0 nM 6.55
CHEMBL1688383 Kd = 340.0 nM 6.47
CHEMBL4449685 Kd = 1110.0 nM 5.96