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Assay Detail

CHEMBL2341204

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

Binding
Agonist activity at human PPARdelta expressed in HEK293 cells cotransfected with PPREx4-TK-luc assessed as activation of luciferase activity measured after 48 hrs by transactivation assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Peroxisome proliferator-activated receptor delta (CHEMBL3979)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

The discovery of novel isoflavone pan peroxisome proliferator-activated receptor agonists.
Matin A, Doddareddy MR, Gavande N, Nammi S, Groundwater PW, Roubin RH, Hibbs DE.
Bioorg Med Chem (2013) 21 : 766 -778
PubMed 23265844 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 5 4.68 4.91

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL573966 1 4.91
CHEMBL575075 1 4.76
CHEMBL486176 PSEUDOBAPTOGENIN 1 4.65
CHEMBL583378 1 4.61
CHEMBL264374 BEZAFIBRATE 3.0 1 4.45

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL573966 EC50 = 12440.0 nM 4.91
CHEMBL575075 EC50 = 17170.0 nM 4.76
CHEMBL486176 PSEUDOBAPTOGENIN EC50 = 22340.0 nM 4.65
CHEMBL583378 EC50 = 24390.0 nM 4.61
CHEMBL264374 BEZAFIBRATE EC50 = 35740.0 nM 4.45