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Assay Detail

CHEMBL931808

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Functional
Agonist activity at human recombinant PPARgamma in HEK293 cells by GAL4 transactivation assay
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

SAR-oriented discovery of peroxisome proliferator-activated receptor pan agonist with a 4-adamantylphenyl group as a hydrophobic tail.
Kasuga J, Yamasaki D, Ogura K, Shimizu M, Sato M, Makishima M, Doi T, Hashimoto Y, Miyachi H.
Bioorg Med Chem Lett (2008) 18 : 1110 -1115
PubMed 18162399 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 12 6.61 7.37

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL402840 1 7.37
CHEMBL270664 1 7.30
CHEMBL402841 1 7.16
CHEMBL272137 1 7.08
CHEMBL270451 1 6.92
CHEMBL402161 1 6.92
CHEMBL270801 1 6.66
CHEMBL270665 1 6.55
CHEMBL270587 1 6.50
CHEMBL255426 1 6.21
CHEMBL271877 1 5.64
CHEMBL255392 1 5.03

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL402840 EC50 = 43.0 nM 7.37
CHEMBL270664 EC50 = 50.0 nM 7.30
CHEMBL402841 EC50 = 70.0 nM 7.16
CHEMBL272137 EC50 = 83.0 nM 7.08
CHEMBL270451 EC50 = 120.0 nM 6.92
CHEMBL402161 EC50 = 120.0 nM 6.92
CHEMBL270801 EC50 = 220.0 nM 6.66
CHEMBL270665 EC50 = 280.0 nM 6.55
CHEMBL270587 EC50 = 320.0 nM 6.50
CHEMBL255426 EC50 = 620.0 nM 6.21
CHEMBL271877 EC50 = 2300.0 nM 5.64
CHEMBL255392 EC50 = 9400.0 nM 5.03