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Assay Detail

CHEMBL1227768

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Functional
Agonist activity at RXRalpha by luciferase reporter gene assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Modification at the acidic domain of RXR agonists has little effect on permissive RXR-heterodimer activation.
Fujii S, Ohsawa F, Yamada S, Shinozaki R, Fukai R, Makishima M, Enomoto S, Tai A, Kakuta H.
Bioorg Med Chem Lett (2010) 20 : 5139 -5142
PubMed 20656484 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 3 7.56 8.28

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1221641 1 8.28
CHEMBL1023 BEXAROTENE 4.0 1 7.70
CHEMBL1221640 1 6.69

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1221641 EC50 = 5.28 nM 8.28
CHEMBL1023 BEXAROTENE EC50 = 19.8 nM 7.70
CHEMBL1221640 EC50 = 205.0 nM 6.69