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Assay Detail

CHEMBL4434136

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

Binding
Agonist activity at human RXRalpha expressed in African green monkey COS1 cells harboring CRBP2-tk-luc reporter incubated for 18 hrs by steady-glo luciferase reporter gene assay
5
Total Activities
5
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

3H-Imidazo[4,5-b]pyridine-6-carboxylic acid derivatives as rexinoids with reduced teratogenicity.
Takamura Y, Takahashi M, Nishii M, Shibahara O, Watanabe M, Fujihara M, Kakuta H.
Bioorg Med Chem Lett (2019) 29 : 1891 -1894
PubMed 31160175 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 5 7.30 7.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2332887 1 7.82
CHEMBL1023 BEXAROTENE 4.0 1 7.70
CHEMBL4465555 1 7.57
CHEMBL2146901 1 6.84
CHEMBL4546707 1 6.56

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2332887 EC50 = 15.0 nM 7.82
CHEMBL1023 BEXAROTENE EC50 = 20.0 nM 7.70
CHEMBL4465555 EC50 = 27.0 nM 7.57
CHEMBL2146901 EC50 = 143.0 nM 6.84
CHEMBL4546707 EC50 = 275.0 nM 6.56