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Assay Detail

CHEMBL857024

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

Functional
Compound was tested functionally in vitro for inducing 50% of the maximum alkaline phosphatase activity (Transactivation) against murine Peroxisome proliferator activated receptor gamma using transfection assay in CV-1 cells
3
Total Activities
3
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 Autocuration

Target

Peroxisome proliferator-activated receptor gamma (CHEMBL2459)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

N-(2-Benzoylphenyl)-L-tyrosine PPARgamma agonists. 1. Discovery of a novel series of potent antihyperglycemic and antihyperlipidemic agents.
Henke BR, Blanchard SG, Brackeen MF, Brown KK, Cobb JE, Collins JL, Harrington WW, Hashim MA, Hull-Ryde EA, Kaldor I, Kliewer SA, Lake DH, Leesnitzer LM, Lehmann JM, Lenhard JM, Orband-Miller LA, Miller JF, Mook RA, Noble SA, Oliver W, Parks DJ, Plunket KD, Szewczyk JR, Willson TM.
J Med Chem (1998) 41 : 5020 -5036
PubMed 9836620 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 3 8.55 9.45

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL107367 FARGLITAZAR 2.0 1 9.45
CHEMBL423026 1 8.33
CHEMBL434063 1 7.88

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL107367 FARGLITAZAR EC50 = 0.3548 nM 9.45
CHEMBL423026 EC50 = 4.677 nM 8.33
CHEMBL434063 EC50 = 13.18 nM 7.88