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Assay Detail

CHEMBL4706439

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

Binding
Binding affinity to PPAR-gamma (unknown origin) by TR-FRET assay
11
Total Activities
11
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
Ki 11 5.47 7.02

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL595 PIOGLITAZONE 4.0 1 7.02
CHEMBL1254751 1 5.91
CHEMBL413686 1 5.48
CHEMBL4758410 1 5.45
CHEMBL1254667 1 5.41
CHEMBL1254750 1 5.39
CHEMBL4760772 1 5.15
CHEMBL4740559 1 5.14
CHEMBL4756797 1 5.12
CHEMBL4799672 1 5.12
CHEMBL4748172 1 5.02

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL595 PIOGLITAZONE Ki = 96.0 nM 7.02
CHEMBL1254751 Ki = 1230.0 nM 5.91
CHEMBL413686 Ki = 3330.0 nM 5.48
CHEMBL4758410 Ki = 3560.0 nM 5.45
CHEMBL1254667 Ki = 3890.0 nM 5.41
CHEMBL1254750 Ki = 4070.0 nM 5.39
CHEMBL4760772 Ki = 7040.0 nM 5.15
CHEMBL4740559 Ki = 7300.0 nM 5.14
CHEMBL4756797 Ki = 7660.0 nM 5.12
CHEMBL4799672 Ki = 7660.0 nM 5.12
CHEMBL4748172 Ki = 9550.0 nM 5.02