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Assay Detail

CHEMBL4008129

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

Binding
Transactivation of GAL4-fused human PPARalpa LBD expressed in human HepG2 cells after 20 hrs by luciferase reporter gene assay
5
Total Activities
5
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

New diphenylmethane derivatives as peroxisome proliferator-activated receptor alpha/gamma dual agonists endowed with anti-proliferative effects and mitochondrial activity.
Piemontese L, Cerchia C, Laghezza A, Ziccardi P, Sblano S, Tortorella P, Iacobazzi V, Infantino V, Convertini P, Dal Piaz F, Lupo A, Colantuoni V, Lavecchia A, Loiodice F.
Eur J Med Chem (2017) 127 : 379 -397
PubMed 28076827 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 5 6.99 7.41

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4064900 1 7.41
CHEMBL4073499 1 7.38
CHEMBL4092600 1 7.34
CHEMBL4100336 1 7.00
CHEMBL295416 PIRINIXIC ACID 2.0 1 5.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4064900 EC50 = 39.0 nM 7.41
CHEMBL4073499 EC50 = 42.0 nM 7.38
CHEMBL4092600 EC50 = 46.0 nM 7.34
CHEMBL4100336 EC50 = 100.0 nM 7.00
CHEMBL295416 PIRINIXIC ACID EC50 = 1600.0 nM 5.80