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Assay Detail

CHEMBL4706451

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

Binding
Agonist activity at PPARgamma LBD (unknown origin) assessed as increase in recruitment of coactivator peptide fluorescein-TRAP220/DRIP by TR-FRET assay
4
Total Activities
4
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 gamma (CHEMBL235)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery and Structure-Activity Relationships of Novel Template, Truncated 1'-Homologated Adenosine Derivatives as Pure Dual PPARγ/δ Modulators.
An S,Kim G,Kim HJ,Ahn S,Kim HY,Ko H,Hyun YE,Nguyen M,Jeong J,Liu Z,Han J,Choi H,Yu J,Kim JW,Lee HW,Jacobson KA,Cho WJ,Kim YM,Kang KW,Noh M,Jeong LS
J Med Chem (2020) 63 : 16012 -16027
PubMed 33325691 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 4 5.95 7.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL434063 1 7.77
CHEMBL408 TROGLITAZONE 4.0 1 5.86
CHEMBL1254751 1 5.16
CHEMBL4758410 1 5.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL434063 EC50 = 17.0 nM 7.77
CHEMBL408 TROGLITAZONE EC50 = 1380.0 nM 5.86
CHEMBL1254751 EC50 = 6850.0 nM 5.16
CHEMBL4758410 EC50 = 9950.0 nM 5.00