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Assay Detail

CHEMBL2033817

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

Binding
Transactivation of human PPARalpha expressed in african green monkey CV1 cells by luciferase reporter gene assay
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CV-1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Total synthesis and dual PPARα/γ agonist effects of amorphastilbol and its synthetic derivatives.
Kim T, Lee W, Jeong KH, Song JH, Park SH, Choi P, Kim SN, Lee S, Ham J.
Bioorg Med Chem Lett (2012) 22 : 4122 -4126
PubMed 22579420 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 13 5.22 6.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL295416 PIRINIXIC ACID 2.0 1 6.89
CHEMBL2031858 1 5.40
CHEMBL2031860 1 5.22
CHEMBL2031956 1 5.22
CHEMBL2031955 1 5.10
CHEMBL500257 AMORPHASTILBOL 1 4.92
CHEMBL2031957 1 4.85
CHEMBL2031856 1 4.72
CHEMBL2031859 1 4.70
CHEMBL2031857 1 -
CHEMBL2031952 1 -
CHEMBL2031953 1 -
CHEMBL2031954 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL295416 PIRINIXIC ACID EC50 = 130.0 nM 6.89
CHEMBL2031858 EC50 = 4000.0 nM 5.40
CHEMBL2031860 EC50 = 6000.0 nM 5.22
CHEMBL2031956 EC50 = 6000.0 nM 5.22
CHEMBL2031955 EC50 = 8000.0 nM 5.10
CHEMBL500257 AMORPHASTILBOL EC50 = 12000.0 nM 4.92
CHEMBL2031957 EC50 = 14000.0 nM 4.85
CHEMBL2031856 EC50 = 19000.0 nM 4.72
CHEMBL2031859 EC50 = 20000.0 nM 4.70
CHEMBL2031857 EC50 - -
CHEMBL2031952 EC50 - -
CHEMBL2031953 EC50 - -
CHEMBL2031954 EC50 - -