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Assay Detail

CHEMBL772126

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

Functional
Synergistic activation of BRL-49653 mediated PPAR gamma and retinoid X receptor alpha expressed in CV-1 cell transcriptional activation assay
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type CV-1
Confidence 7 — Homologous single protein target
Curated By Expert

Target

RXR alpha/PPAR gamma (CHEMBL2111394)
Type PROTEIN COMPLEX
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 9 7.63 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL92050 1 8.70
CHEMBL325592 1 8.57
CHEMBL42314 1 8.51
CHEMBL111217 1 8.19
CHEMBL110195 1 8.04
CHEMBL326673 1 6.84
CHEMBL107555 1 6.78
CHEMBL110921 1 6.60
CHEMBL107554 1 6.44

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL92050 EC50 = 2.0 nM 8.70
CHEMBL325592 EC50 = 2.7 nM 8.57
CHEMBL42314 EC50 = 3.1 nM 8.51
CHEMBL111217 EC50 = 6.4 nM 8.19
CHEMBL110195 EC50 = 9.2 nM 8.04
CHEMBL326673 EC50 = 143.4 nM 6.84
CHEMBL107555 EC50 = 167.4 nM 6.78
CHEMBL110921 EC50 = 249.1 nM 6.60
CHEMBL107554 EC50 = 359.4 nM 6.44