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Assay Detail

CHEMBL759455

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Binding
Inhibitory activity of compound against the binding of human Peroxisome proliferator activated receptor gamma was determined
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Design and synthesis of a potent and selective triazolone-based peroxisome proliferator-activated receptor alpha agonist.
Xu Y, Mayhugh D, Saeed A, Wang X, Thompson RC, Dominianni SJ, Kauffman RF, Singh J, Bean JS, Bensch WR, Barr RJ, Osborne J, Montrose-Rafizadeh C, Zink RW, Yumibe NP, Huang N, Luffer-Atlas D, Rungta D, Maise DE, Mantlo NB.
J Med Chem (2003) 46 : 5121 -5124
PubMed 14613314 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 5.53 6.28

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL148639 1 6.28
CHEMBL278590 GSK-9578 1 6.26
CHEMBL344282 1 5.77
CHEMBL149438 1 5.77
CHEMBL149676 1 5.31
CHEMBL345721 1 5.21
CHEMBL148774 1 5.21
CHEMBL356170 1 5.21
CHEMBL424133 LY-518674 2.0 1 5.19
CHEMBL147086 1 5.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL148639 IC50 = 520.0 nM 6.28
CHEMBL278590 GSK-9578 IC50 = 550.0 nM 6.26
CHEMBL344282 IC50 = 1700.0 nM 5.77
CHEMBL149438 IC50 = 1700.0 nM 5.77
CHEMBL149676 IC50 = 4900.0 nM 5.31
CHEMBL345721 IC50 = 6200.0 nM 5.21
CHEMBL148774 IC50 = 6100.0 nM 5.21
CHEMBL356170 IC50 = 6100.0 nM 5.21
CHEMBL424133 LY-518674 IC50 = 6500.0 nM 5.19
CHEMBL147086 IC50 = 7900.0 nM 5.10