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Assay Detail

CHEMBL5133907

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

Binding
Transactivation of Gal4-fused human PPARalpha expressed in CHO cells co expressing pG5-Luc reporter
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Discovery and structure-based design of a new series of potent and selective PPARδ agonists utilizing a virtual screening method.
Kato T, Ohara T, Suzuki N, Muto S, Tokuyama R, Mizutani M, Fukasawa H, Matsumura KI, Itai A.
Bioorg Med Chem Lett (2022) 59 : 128567 -128567
PubMed 35063634 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 6 5.87 6.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5180328 1 6.22
CHEMBL5180073 1 6.20
CHEMBL5193666 1 6.02
CHEMBL38943 GW501516 2.0 1 5.66
CHEMBL5185420 1 5.65
CHEMBL5183133 1 5.44

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5180328 EC50 = 603.0 nM 6.22
CHEMBL5180073 EC50 = 637.0 nM 6.20
CHEMBL5193666 EC50 = 955.0 nM 6.02
CHEMBL38943 GW501516 EC50 = 2200.0 nM 5.66
CHEMBL5185420 EC50 = 2220.0 nM 5.65
CHEMBL5183133 EC50 = 3600.0 nM 5.44