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Assay Detail

CHEMBL3369562

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Binding
Agonist activity at human PPARgamma
12
Total Activities
12
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

Molecular dynamics study-guided identification of cyclic amine structures as novel hydrophobic tail components of hPPARγ agonists.
Tanaka Y, Gamo K, Oyama T, Ohashi M, Waki M, Matsuno K, Matsuura N, Tokiwa H, Miyachi H.
Bioorg Med Chem Lett (2014) 24 : 4001 -4005
PubMed 25017035 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 12 8.15 8.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3317860 1 8.72
CHEMBL3317867 1 8.66
CHEMBL3317863 1 8.66
CHEMBL1651239 1 8.44
CHEMBL3317865 1 8.28
CHEMBL3317864 1 8.17
CHEMBL3317859 1 8.17
CHEMBL3317861 1 8.15
CHEMBL3317862 1 7.98
CHEMBL3317866 1 7.93
CHEMBL3317455 1 7.41
CHEMBL3317858 1 7.28

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3317860 EC50 = 1.9 nM 8.72
CHEMBL3317867 EC50 = 2.2 nM 8.66
CHEMBL3317863 EC50 = 2.2 nM 8.66
CHEMBL1651239 EC50 = 3.6 nM 8.44
CHEMBL3317865 EC50 = 5.3 nM 8.28
CHEMBL3317864 EC50 = 6.7 nM 8.17
CHEMBL3317859 EC50 = 6.7 nM 8.17
CHEMBL3317861 EC50 = 7.0 nM 8.15
CHEMBL3317862 EC50 = 10.4 nM 7.98
CHEMBL3317866 EC50 = 11.7 nM 7.93
CHEMBL3317455 EC50 = 38.9 nM 7.41
CHEMBL3317858 EC50 = 52.7 nM 7.28