Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL762741

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

Functional
Agonist activity on Gal4 chimeric human Peroxisome proliferator activated receptor gamma expressed in KRP-297 cells
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type KRP-297
Confidence 9 — Direct single protein target
Curated By Expert

Target

Peroxisome proliferator-activated receptor gamma (CHEMBL235)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, synthesis, and evaluation of substituted phenylpropanoic acid derivatives as human peroxisome proliferator activated receptor activators. Discovery of potent and human peroxisome proliferator activated receptor alpha subtype-selective activators.
Nomura M, Tanase T, Ide T, Tsunoda M, Suzuki M, Uchiki H, Murakami K, Miyachi H.
J Med Chem (2003) 46 : 3581 -3599
PubMed 12904063 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 15 5.53 6.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL120009 1 6.40
CHEMBL24458 1 6.10
CHEMBL122070 1 5.62
CHEMBL331206 1 5.60
CHEMBL325723 1 5.55
CHEMBL120744 1 5.55
CHEMBL118483 1 5.52
CHEMBL122009 1 5.52
CHEMBL119791 1 5.40
CHEMBL118279 1 5.27
CHEMBL116947 1 5.21
CHEMBL331469 1 5.13
CHEMBL118198 1 5.00
CHEMBL264374 BEZAFIBRATE 3.0 1 -
CHEMBL118939 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL120009 EC50 = 400.0 nM 6.40
CHEMBL24458 EC50 = 800.0 nM 6.10
CHEMBL122070 EC50 = 2400.0 nM 5.62
CHEMBL331206 EC50 = 2500.0 nM 5.60
CHEMBL325723 EC50 = 2800.0 nM 5.55
CHEMBL120744 EC50 = 2800.0 nM 5.55
CHEMBL118483 EC50 = 3000.0 nM 5.52
CHEMBL122009 EC50 = 3000.0 nM 5.52
CHEMBL119791 EC50 = 4000.0 nM 5.40
CHEMBL118279 EC50 = 5400.0 nM 5.27
CHEMBL116947 EC50 = 6200.0 nM 5.21
CHEMBL331469 EC50 = 7400.0 nM 5.13
CHEMBL118198 EC50 = 10000.0 nM 5.00
CHEMBL264374 BEZAFIBRATE EC50 > 137000.0 nM -
CHEMBL118939 EC50 > 10000.0 nM -