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Assay Detail

CHEMBL1764348

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

Functional
Partial agonist activity at human PPARgamma expressed in CHO cells co-transfected with Gal4-responsive luciferase reporter plasmid after 24 hrs by transactivation assay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Peroxisome proliferator-activated receptor gamma (CHEMBL235)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and pharmacological evaluation of novel benzoylazole-based PPAR α/γ activators.
Ushiroda K, Maruta K, Takazawa T, Nagano T, Taiji M, Kohno T, Sato Y, Horai S, Yanagi K, Nagata R.
Bioorg Med Chem Lett (2011) 21 : 1978 -1982
PubMed 21377875 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 11 5.65 6.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1760559 1 6.89
CHEMBL595 PIOGLITAZONE 4.0 1 6.41
CHEMBL1760558 1 5.77
CHEMBL1760557 1 5.52
CHEMBL1760561 1 5.48
CHEMBL1760554 1 5.34
CHEMBL1760556 1 5.32
CHEMBL1760560 1 5.22
CHEMBL1760555 1 4.92
CHEMBL981 FENOFIBRIC ACID 4.0 1 -
CHEMBL1760553 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1760559 EC50 = 130.0 nM 6.89
CHEMBL595 PIOGLITAZONE EC50 = 390.0 nM 6.41
CHEMBL1760558 EC50 = 1700.0 nM 5.77
CHEMBL1760557 EC50 = 3000.0 nM 5.52
CHEMBL1760561 EC50 = 3300.0 nM 5.48
CHEMBL1760554 EC50 = 4600.0 nM 5.34
CHEMBL1760556 EC50 = 4800.0 nM 5.32
CHEMBL1760560 EC50 = 6000.0 nM 5.22
CHEMBL1760555 EC50 = 12000.0 nM 4.92
CHEMBL981 FENOFIBRIC ACID EC50 - -
CHEMBL1760553 EC50 > 10000.0 nM -