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Assay Detail

CHEMBL4704897

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Binding
Agonist activity at GAL4-tagged PPARalpha-LBD (unknown origin) expressed in HEK293 cells assessed as induction of receptor transactivation incubated for 16 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
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

A Novel N-Substituted Valine Derivative with Unique Peroxisome Proliferator-Activated Receptor γ Binding Properties and Biological Activities.
Peiretti F,Montanari R,Capelli D,Bonardo B,Colson C,Amri EZ,Grimaldi M,Balaguer P,Ito K,Roeder RG,Pochetti G,Brunel JM
J Med Chem (2020) 63 : 13124 -13139
PubMed 33142057 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 5 6.16 8.27

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL21241 GW7647 1 8.27
CHEMBL4743677 1 5.72
CHEMBL264374 BEZAFIBRATE 3.0 1 4.50
CHEMBL4741141 1 -
CHEMBL4795671 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL21241 GW7647 EC50 = 5.4 nM 8.27
CHEMBL4743677 EC50 = 1882.0 nM 5.72
CHEMBL264374 BEZAFIBRATE EC50 = 31700.0 nM 4.50
CHEMBL4741141 EC50 - -
CHEMBL4795671 EC50 - -