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Assay Detail

CHEMBL5032690

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

Binding
Agonist activity at human PPARgamma transfected in COS-7 cells assessed luciferase activity measured after 24 hrs by cell based luciferase transactivation assay
10
Total Activities
10
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

Synthesis and Evaluation of PPARδ Agonists That Promote Osteogenesis in a Human Mesenchymal Stem Cell Culture and in a Mouse Model of Human Osteoporosis.
Kress BJ, Kim DH, Mayo JR, Farris JT, Heck B, Sarver JG, Andy D, Trendel JA, Heck BE, Erhardt PW.
J Med Chem (2021) 64 : 6996 -7032
PubMed 33988379 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 10 5.18 6.84

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL121 ROSIGLITAZONE 4.0 1 6.84
CHEMBL5080884 1 5.89
CHEMBL205434 1 5.28
CHEMBL38508 1 5.02
CHEMBL5080057 1 4.88
CHEMBL5071965 1 4.77
CHEMBL5076771 1 4.61
CHEMBL457 GEMFIBROZIL 4.0 1 4.17
CHEMBL5081804 1 -
CHEMBL5088887 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL121 ROSIGLITAZONE EC50 = 144.0 nM 6.84
CHEMBL5080884 EC50 = 1300.0 nM 5.89
CHEMBL205434 EC50 = 5280.0 nM 5.28
CHEMBL38508 EC50 = 9530.0 nM 5.02
CHEMBL5080057 EC50 = 13200.0 nM 4.88
CHEMBL5071965 EC50 = 17000.0 nM 4.77
CHEMBL5076771 EC50 = 24700.0 nM 4.61
CHEMBL457 GEMFIBROZIL EC50 = 68400.0 nM 4.17
CHEMBL5081804 EC50 - -
CHEMBL5088887 EC50 - -