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Assay Detail

CHEMBL4704909

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Binding
Agonist activity at PPARg-LBD (unknown origin) expressed in HEK293 cells assessed as displacement of NCoR incubated for 16 hrs by luciferase reporter gene based mammalian two hybrid assay
2
Total Activities
2
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 gamma (CHEMBL235)
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
IC50 2 6.54 7.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL121 ROSIGLITAZONE 4.0 1 7.05
CHEMBL4743677 1 6.02

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL121 ROSIGLITAZONE IC50 = 88.4 nM 7.05
CHEMBL4743677 IC50 = 956.2 nM 6.02