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Assay Detail

CHEMBL3784067

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

Binding
Agonist activity at histidine-tagged ligand binding domain of human RXRalpha expressed in Escherichia coli BL21 (DE3) by luciferase reporter gene assay
11
Total Activities
11
Compounds Tested
2
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

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 8 7.31 8.20
pEC50 3 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3781132 1 8.20
CHEMBL3780763 1 7.70
CHEMBL3779935 1 7.60
CHEMBL1023 BEXAROTENE 4.0 1 7.50
CHEMBL3781998 1 7.30
CHEMBL3780004 1 7.30
CHEMBL3781771 1 6.90
CHEMBL3780806 1 6.00
CHEMBL3781879 1 -
CHEMBL3781759 1 -
CHEMBL3781374 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3781132 EC50 = 6.31 nM 8.20
CHEMBL3780763 EC50 = 19.95 nM 7.70
CHEMBL3779935 EC50 = 25.12 nM 7.60
CHEMBL1023 BEXAROTENE EC50 = 31.62 nM 7.50
CHEMBL3781998 EC50 = 50.12 nM 7.30
CHEMBL3780004 EC50 = 50.12 nM 7.30
CHEMBL3781771 EC50 = 125.89 nM 6.90
CHEMBL3780806 EC50 = 1000.0 nM 6.00
CHEMBL3781879 pEC50 - -
CHEMBL3781759 pEC50 - -
CHEMBL3781374 pEC50 - -