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Assay Detail

CHEMBL4808635

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

Binding
Agonist activity at human PPARgamma expressed in CHO cells assessed as increase in receptor transcriptional activity incubated for 24 hrs by dual luciferase reporter gene assay
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Structure-Activity Relationship Study and Biological Evaluation of 2-(Disubstituted phenyl)-indole-5-propanoic Acid Derivatives as GPR40 Full Agonists.
Zhao X, Yoon DO, Yoo J, Park HJ.
J Med Chem (2021) 64 : 4130 -4149
PubMed 33769827 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 18 4.41 4.56

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4854804 1 4.56
CHEMBL4859651 1 4.25
CHEMBL4866406 1 -
CHEMBL4852222 1 -
CHEMBL4869870 1 -
CHEMBL4866568 1 -
CHEMBL4852865 1 -
CHEMBL4848974 1 -
CHEMBL4858086 1 -
CHEMBL4855306 1 -
CHEMBL4877893 1 -
CHEMBL4868676 1 -
CHEMBL4859407 1 -
CHEMBL4847662 1 -
CHEMBL4872298 1 -
CHEMBL4865460 1 -
CHEMBL4850966 1 -
CHEMBL4857550 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4854804 EC50 = 27770.0 nM 4.56
CHEMBL4859651 EC50 = 56940.0 nM 4.25
CHEMBL4866406 EC50 - -
CHEMBL4852222 EC50 - -
CHEMBL4869870 EC50 - -
CHEMBL4866568 EC50 - -
CHEMBL4852865 EC50 - -
CHEMBL4848974 EC50 - -
CHEMBL4858086 EC50 - -
CHEMBL4855306 EC50 - -
CHEMBL4877893 EC50 - -
CHEMBL4868676 EC50 - -
CHEMBL4859407 EC50 - -
CHEMBL4847662 EC50 - -
CHEMBL4872298 EC50 - -
CHEMBL4865460 EC50 - -
CHEMBL4850966 EC50 - -
CHEMBL4857550 EC50 - -