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Assay Detail

CHEMBL4812203

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

Binding
Agonist activity at human Gal4 fused PPARgamma LBD expressed in COS-7 cells incubated for 24 hrs by firefly luciferase reporter gene assay
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type COS-7
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Design, synthesis, and biological evaluation of a novel dual peroxisome proliferator-activated receptor alpha/delta agonist for the treatment of diabetic kidney disease through anti-inflammatory mechanisms.
Liu K, Zhao X, Qi X, Hou DL, Li HB, Gu YH, Xu QL.
Eur J Med Chem (2021) 218 : 113388 -113388
PubMed 33784603 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 20 5.61 6.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4875481 1 6.00
CHEMBL4853930 1 5.79
CHEMBL4872726 1 5.76
CHEMBL3707395 ELAFIBRANOR 4.0 1 5.55
CHEMBL4872922 1 5.38
CHEMBL4856271 1 5.20
CHEMBL4861167 1 -
CHEMBL4860504 1 -
CHEMBL4873389 1 -
CHEMBL4853743 1 -
CHEMBL4852230 1 -
CHEMBL4859752 1 -
CHEMBL4847495 1 -
CHEMBL4869134 1 -
CHEMBL4848052 1 -
CHEMBL4855296 1 -
CHEMBL4869342 1 -
CHEMBL21241 GW7647 1 -
CHEMBL38943 GW501516 2.0 1 -
CHEMBL121 ROSIGLITAZONE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4875481 EC50 = 1000.0 nM 6.00
CHEMBL4853930 EC50 = 1630.0 nM 5.79
CHEMBL4872726 EC50 = 1720.0 nM 5.76
CHEMBL3707395 ELAFIBRANOR EC50 = 2790.0 nM 5.55
CHEMBL4872922 EC50 = 4220.0 nM 5.38
CHEMBL4856271 EC50 = 6360.0 nM 5.20
CHEMBL4861167 EC50 > 10000.0 nM -
CHEMBL4860504 EC50 > 10000.0 nM -
CHEMBL4873389 EC50 > 10000.0 nM -
CHEMBL4853743 EC50 > 10000.0 nM -
CHEMBL4852230 EC50 > 10000.0 nM -
CHEMBL4859752 EC50 > 10000.0 nM -
CHEMBL4847495 EC50 > 10000.0 nM -
CHEMBL4869134 EC50 > 10000.0 nM -
CHEMBL4848052 EC50 > 10000.0 nM -
CHEMBL4855296 EC50 > 10000.0 nM -
CHEMBL4869342 EC50 > 10000.0 nM -
CHEMBL21241 GW7647 EC50 - -
CHEMBL38943 GW501516 EC50 - -
CHEMBL121 ROSIGLITAZONE EC50 = 191500.0 nM -