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Assay Detail

CHEMBL760604

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

Functional
Maximal reporter activity against human Peroxisome proliferator activated receptor alpha Gal4 chimeric in transiently transfected CV-1 cells by functional assay.
6
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Cell Type CV-1
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Peroxisome proliferator-activated receptor alpha (CHEMBL239)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and biological activity of L-tyrosine-based PPARgamma agonists with reduced molecular weight.
Liu KG, Lambert MH, Ayscue AH, Henke BR, Leesnitzer LM, Oliver WR, Plunket KD, Xu HE, Sternbach DD, Willson TM.
Bioorg Med Chem Lett (2001) 11 : 3111 -3113
PubMed 11720854 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 6 5.73 6.35

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL107367 FARGLITAZAR 2.0 1 6.35
CHEMBL321634 1 6.08
CHEMBL104850 2 5.89
CHEMBL106666 GW7845 1 5.46
CHEMBL104246 1 5.16

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL107367 FARGLITAZAR EC50 = 450.0 nM 6.35
CHEMBL321634 EC50 = 830.0 nM 6.08
CHEMBL104850 EC50 = 1300.0 nM 5.89
CHEMBL106666 GW7845 EC50 = 3500.0 nM 5.46
CHEMBL104850 EC50 = 3600.0 nM 5.44
CHEMBL104246 EC50 = 6900.0 nM 5.16