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Assay Detail

CHEMBL798968

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

Binding
Ability to activate gene expression at Retinoic acid receptor RXR-gamma was evaluated in a cotransfection assay.
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Retinoic acid receptor RXR-gamma (CHEMBL4402)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Design and synthesis of potent retinoid X receptor selective ligands that induce apoptosis in leukemia cells.
Boehm MF, Zhang L, Zhi L, McClurg MR, Berger E, Wagoner M, Mais DE, Suto CM, Davies JA, Heyman RA.
J Med Chem (1995) 38 : 3146 -3155
PubMed 7636877 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 16 6.87 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL288436 1 8.40
CHEMBL109117 1 8.30
CHEMBL106896 1 7.77
CHEMBL1023 BEXAROTENE 4.0 1 7.70
CHEMBL106817 1 7.33
CHEMBL25244 1 6.62
CHEMBL98172 1 6.61
CHEMBL105979 1 6.47
CHEMBL105805 1 6.37
CHEMBL432587 1 6.36
CHEMBL106837 1 6.30
CHEMBL108402 1 6.22
CHEMBL110629 1 6.19
CHEMBL107039 1 5.58
CHEMBL108162 1 -
CHEMBL105806 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL288436 EC50 = 4.0 nM 8.40
CHEMBL109117 EC50 = 5.0 nM 8.30
CHEMBL106896 EC50 = 17.0 nM 7.77
CHEMBL1023 BEXAROTENE EC50 = 20.0 nM 7.70
CHEMBL106817 EC50 = 47.0 nM 7.33
CHEMBL25244 EC50 = 240.0 nM 6.62
CHEMBL98172 EC50 = 246.0 nM 6.61
CHEMBL105979 EC50 = 340.0 nM 6.47
CHEMBL105805 EC50 = 430.0 nM 6.37
CHEMBL432587 EC50 = 440.0 nM 6.36
CHEMBL106837 EC50 = 500.0 nM 6.30
CHEMBL108402 EC50 = 600.0 nM 6.22
CHEMBL110629 EC50 = 650.0 nM 6.19
CHEMBL107039 EC50 = 2600.0 nM 5.58
CHEMBL108162 EC50 > 10000.0 nM -
CHEMBL105806 EC50 > 10000.0 nM -