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Assay Detail

CHEMBL3821237

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

Binding
Agonist activity at Gal4-tagged human PPARalpha ligand binding domain expressed in COS-7 cells measured after overnight incubation by dual-glo luciferase reporter gene assay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type COS-7
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Design and synthesis of fused soluble epoxide hydrolase/peroxisome proliferator-activated receptor modulators
Blocher R, Lamers C, Wittmann SK, Diehl O, Hanke T, Merk D, Steinhilber D, Schubert-Zsilavecz M, Kahnt AS, Proschak E
Medchemcomm (2016) 7 : 1209 -1216
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 11 5.97 7.17

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3318038 1 7.17
CHEMBL3818976 1 5.60
CHEMBL264374 BEZAFIBRATE 3.0 1 5.15
CHEMBL3819535 1 -
CHEMBL3818218 1 -
CHEMBL3818149 1 -
CHEMBL3817950 1 -
CHEMBL3818537 1 -
CHEMBL3819103 1 -
CHEMBL3818875 GSK2256294 2.0 1 -
CHEMBL1231797 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3318038 EC50 = 67.0 nM 7.17
CHEMBL3818976 EC50 = 2500.0 nM 5.60
CHEMBL264374 BEZAFIBRATE EC50 = 7100.0 nM 5.15
CHEMBL3819535 EC50 - -
CHEMBL3818218 EC50 - -
CHEMBL3818149 EC50 - -
CHEMBL3817950 EC50 - -
CHEMBL3818537 EC50 - -
CHEMBL3819103 EC50 - -
CHEMBL3818875 GSK2256294 EC50 - -
CHEMBL1231797 EC50 - -