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Assay Detail

CHEMBL803331

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Functional
Antagonist activity against Retinoic acid receptor RXR-alpha expressed in CV-1 cell transcriptional activation assay
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type CV-1
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Design and synthesis of fluorinated RXR modulators.
Gernert DL, Ajamie R, Ardecky RA, Bell MG, Leibowitz MD, Mais DA, Mapes CM, Michellys PY, Rungta D, Reifel-Miller A, Tyhonas JS, Yumibe N, Grese TA.
Bioorg Med Chem Lett (2003) 13 : 3191 -3195
PubMed 12951091 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 8 7.15 8.48

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL110195 1 8.48
CHEMBL325592 1 8.47
CHEMBL92050 1 8.19
CHEMBL111217 1 8.17
CHEMBL107555 1 7.42
CHEMBL107554 1 6.09
CHEMBL326673 1 5.32
CHEMBL110921 1 5.06

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL110195 EC50 = 3.3 nM 8.48
CHEMBL325592 EC50 = 3.4 nM 8.47
CHEMBL92050 EC50 = 6.4 nM 8.19
CHEMBL111217 EC50 = 6.8 nM 8.17
CHEMBL107555 EC50 = 38.0 nM 7.42
CHEMBL107554 EC50 = 805.8 nM 6.09
CHEMBL326673 EC50 = 4842.1 nM 5.32
CHEMBL110921 EC50 = 8712.8 nM 5.06