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Assay Detail

CHEMBL3784071

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

Binding
Agonist activity at Renilla luciferase/GFP2-tagged RXRalpha homodimer (unknown origin) expressed in HEK293T cells by BRET2 assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK-293T
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Chiral Dihydrobenzofuran Acids Show Potent Retinoid X Receptor-Nuclear Receptor Related 1 Protein Dimer Activation.
Sundén H, Schäfer A, Scheepstra M, Leysen S, Malo M, Ma JN, Burstein ES, Ottmann C, Brunsveld L, Olsson R.
J Med Chem (2016) 59 : 1232 -1238
PubMed 26820900 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 3 7.63 7.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3780763 1 7.80
CHEMBL3781132 1 7.60
CHEMBL1023 BEXAROTENE 4.0 1 7.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3780763 EC50 = 15.85 nM 7.80
CHEMBL3781132 EC50 = 25.12 nM 7.60
CHEMBL1023 BEXAROTENE EC50 = 31.62 nM 7.50