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Assay Detail

CHEMBL5252415

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

Binding
Agonist activity at human PPARalpha incubated for 22 to 24 hrs by luciferase assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Design, Synthesis, and Structure-Activity Relationships of Biaryl Anilines as Subtype-Selective PPAR-alpha Agonists.
Lee JJ, Hu Z, Wang YA, Nath D, Liang W, Cui Y, Ma JX, Duerfeldt AS.
ACS Med Chem Lett (2023) 14 : 766 -776
PubMed 37312852 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 6 7.06 8.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL21241 GW7647 1 8.24
CHEMBL5273730 1 7.19
CHEMBL5282696 1 7.10
CHEMBL5289051 1 7.08
CHEMBL5290621 1 6.52
CHEMBL5285590 1 6.23

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL21241 GW7647 EC50 = 5.7 nM 8.24
CHEMBL5273730 EC50 = 64.0 nM 7.19
CHEMBL5282696 EC50 = 80.0 nM 7.10
CHEMBL5289051 EC50 = 83.0 nM 7.08
CHEMBL5290621 EC50 = 300.0 nM 6.52
CHEMBL5285590 EC50 = 590.0 nM 6.23