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Assay Detail

CHEMBL3371803

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

Binding
Agonist activity at GAL4-tagged PPARalpha ligand-binding domain (unknown origin) expressed in HEK293T cells incubated for 16 to 19 hrs by beta-lactamase reporter gene assay
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK-293T
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Biological evaluation and structural insights for design of subtype-selective peroxisome proliferator activated receptor-α (PPAR-α) agonists.
Gangwal RP, Damre MV, Das NR, Sharma SS, Sangamwar AT.
Bioorg Med Chem Lett (2015) 25 : 270 -275
PubMed 25491112 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 9 8.52 9.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3354987 1 9.80
CHEMBL247951 PEMAFIBRATE 4.0 1 9.00
CHEMBL1494365 1 8.96
CHEMBL3354989 1 8.40
CHEMBL1934476 1 8.30
CHEMBL435523 1 8.30
CHEMBL1934484 1 8.22
CHEMBL3354988 1 7.92
CHEMBL21241 GW7647 1 7.81

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3354987 EC50 = 0.16 nM 9.80
CHEMBL247951 PEMAFIBRATE EC50 = 1.0 nM 9.00
CHEMBL1494365 EC50 = 1.1 nM 8.96
CHEMBL3354989 EC50 = 4.0 nM 8.40
CHEMBL1934476 EC50 = 5.0 nM 8.30
CHEMBL435523 EC50 = 5.0 nM 8.30
CHEMBL1934484 EC50 = 6.0 nM 8.22
CHEMBL3354988 EC50 = 12.1 nM 7.92
CHEMBL21241 GW7647 EC50 = 15.4 nM 7.81