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Assay Detail

CHEMBL4813050

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Binding
Agonist activity at Gal4-fused human PPARalpha co-expressed with RXRalpha in monkey CV1 cells assessed as PPRE transcriptional activation incubated for 45 hrs by luciferase reporter gene assay
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CV-1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Discovery of novel modulators for the PPARα (peroxisome proliferator activated receptor α): Potential therapies for nonalcoholic fatty liver disease.
Yu DD, Van Citters G, Li H, Stoltz BM, Forman BM.
Bioorg Med Chem (2021) 41 : 116193 -116193
PubMed 34022528 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 8 8.80 9.07

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4866115 1 9.07
CHEMBL4861761 1 9.06
CHEMBL4879102 1 9.02
CHEMBL4855604 1 9.00
CHEMBL4847453 1 9.00
CHEMBL4877444 1 8.82
CHEMBL4870407 1 8.52
CHEMBL4847989 1 7.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4866115 EC50 = 0.85 nM 9.07
CHEMBL4861761 EC50 = 0.87 nM 9.06
CHEMBL4879102 EC50 = 0.95 nM 9.02
CHEMBL4855604 EC50 = 1.0 nM 9.00
CHEMBL4847453 EC50 = 1.0 nM 9.00
CHEMBL4877444 EC50 = 1.5 nM 8.82
CHEMBL4870407 EC50 = 3.0 nM 8.52
CHEMBL4847989 EC50 = 12.0 nM 7.92