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Assay Detail

CHEMBL3784069

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

Binding
Agonist activity at Renilla luciferase/GFP2-tagged RXRalpha/Nurr1 (unknown origin) expressed in HEK293T cells by BRET2 assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK-293T
Confidence 7 — Homologous single protein target
Curated By Autocuration

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 5 7.53 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1023 BEXAROTENE 4.0 1 8.00
CHEMBL3780763 1 7.90
CHEMBL3781132 1 7.90
CHEMBL3780806 1 6.30
CHEMBL3781879 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1023 BEXAROTENE EC50 = 10.0 nM 8.00
CHEMBL3780763 EC50 = 12.59 nM 7.90
CHEMBL3781132 EC50 = 12.59 nM 7.90
CHEMBL3780806 EC50 = 501.19 nM 6.30
CHEMBL3781879 EC50 > 3162.28 nM -