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Assay Detail

CHEMBL3429522

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

Binding
Agonist activity at RXRalpha (unknown origin) expressed in COS1 cells incubated for 18 hrs by luciferase reporter gene assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type COS-1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Positron emission tomography to elucidate pharmacokinetic differences of regioisomeric retinoid x receptor agonists.
Kobayashi T, Furusawa Y, Yamada S, Akehi M, Takenaka F, Sasaki T, Akahoshi A, Hanada T, Matsuura E, Hirano H, Tai A, Kakuta H.
ACS Med Chem Lett (2015) 6 : 334 -338
PubMed 25815156 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 5 7.29 7.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3425764 1 7.92
CHEMBL1688383 1 7.72
CHEMBL1023 BEXAROTENE 4.0 1 7.70
CHEMBL3425765 1 6.77
CHEMBL3425828 1 6.35

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3425764 EC50 = 12.0 nM 7.92
CHEMBL1688383 EC50 = 19.0 nM 7.72
CHEMBL1023 BEXAROTENE EC50 = 20.0 nM 7.70
CHEMBL3425765 EC50 = 169.0 nM 6.77
CHEMBL3425828 EC50 = 450.0 nM 6.35