Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL2214360

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

Binding
Agonist activity at human GAL4-fused PPARalpha ligand binding domain expressed in HepG2 cells after 20 hrs by luciferase reporter gene transactivation assay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HepG2
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Synthesis, characterization and biological evaluation of ureidofibrate-like derivatives endowed with peroxisome proliferator-activated receptor activity.
Porcelli L, Gilardi F, Laghezza A, Piemontese L, Mitro N, Azzariti A, Altieri F, Cervoni L, Fracchiolla G, Giudici M, Guerrini U, Lavecchia A, Montanari R, Di Giovanni C, Paradiso A, Pochetti G, Simone GM, Tortorella P, Crestani M, Loiodice F.
J Med Chem (2012) 55 : 37 -54
PubMed 22081932 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 11 6.95 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL479207 1 8.52
CHEMBL2206302 1 7.60
CHEMBL477312 1 7.52
CHEMBL477119 1 7.25
CHEMBL2206304 1 6.91
CHEMBL2206303 1 6.21
CHEMBL295416 PIRINIXIC ACID 2.0 1 5.80
CHEMBL2206305 1 5.76
CHEMBL153057 1 -
CHEMBL121 ROSIGLITAZONE 4.0 1 -
CHEMBL2206306 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL479207 EC50 = 3.0 nM 8.52
CHEMBL2206302 EC50 = 25.0 nM 7.60
CHEMBL477312 EC50 = 30.0 nM 7.52
CHEMBL477119 EC50 = 56.0 nM 7.25
CHEMBL2206304 EC50 = 122.0 nM 6.91
CHEMBL2206303 EC50 = 620.0 nM 6.21
CHEMBL295416 PIRINIXIC ACID EC50 = 1600.0 nM 5.80
CHEMBL2206305 EC50 = 1720.0 nM 5.76
CHEMBL153057 EC50 - -
CHEMBL121 ROSIGLITAZONE EC50 - -
CHEMBL2206306 EC50 - -