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Assay Detail

CHEMBL1809823

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

Binding
Agonist activity at PPARalpha ligand binding domain expressed in HEK293 cells co-expressing GAL4 after 18 hrs by dual-luciferase activity based transactivation assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type HEK293
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Benzothiazole-based N-(phenylsulfonyl)amides as a novel family of PPARα antagonists.
Ammazzalorso A, Giancristofaro A, D'Angelo A, Filippis BD, Fantacuzzi M, Giampietro L, Maccallini C, Amoroso R.
Bioorg Med Chem Lett (2011) 21 : 4869 -4872
PubMed 21742490 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 3 5.09 6.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL21241 GW7647 1 6.70
CHEMBL1808555 1 4.30
CHEMBL683 CLOFIBRIC ACID 2.0 1 4.26

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL21241 GW7647 EC50 = 200.0 nM 6.70
CHEMBL1808555 EC50 = 50600.0 nM 4.30
CHEMBL683 CLOFIBRIC ACID EC50 = 55000.0 nM 4.26