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Assay Detail

CHEMBL1059362

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Functional
Agonist activity at human PPARgamma assessed as luciferase activity by transactivation assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

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

Publication

7-Hydroxy-benzopyran-4-one derivatives: a novel pharmacophore of peroxisome proliferator-activated receptor alpha and -gamma (PPARalpha and gamma) dual agonists.
Matin A, Gavande N, Kim MS, Yang NX, Salam NK, Hanrahan JR, Roubin RH, Hibbs DE.
J Med Chem (2009) 52 : 6835 -6850
PubMed 19807106 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 5 4.62 4.81

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL583378 1 4.81
CHEMBL575075 1 4.72
CHEMBL573966 1 4.65
CHEMBL486176 PSEUDOBAPTOGENIN 1 4.57
CHEMBL121 ROSIGLITAZONE 4.0 1 4.36

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL583378 EC50 = 15380.0 nM 4.81
CHEMBL575075 EC50 = 18860.0 nM 4.72
CHEMBL573966 EC50 = 22290.0 nM 4.65
CHEMBL486176 PSEUDOBAPTOGENIN EC50 = 26940.0 nM 4.57
CHEMBL121 ROSIGLITAZONE EC50 = 43710.0 nM 4.36