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Assay Detail

CHEMBL765406

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Binding
Inhibitory activity against human Peroxisome proliferator activated receptor alpha
11
Total Activities
11
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 alpha (CHEMBL239)
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 11 7.02 7.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL344282 1 7.92
CHEMBL148639 1 7.82
CHEMBL149676 1 7.80
CHEMBL345721 1 7.72
CHEMBL424133 LY-518674 2.0 1 7.62
CHEMBL148774 1 7.57
CHEMBL278590 GSK-9578 1 6.92
CHEMBL356170 1 6.66
CHEMBL149438 1 6.60
CHEMBL147086 1 6.02
CHEMBL981 FENOFIBRIC ACID 4.0 1 4.62

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL344282 IC50 = 12.0 nM 7.92
CHEMBL148639 IC50 = 15.0 nM 7.82
CHEMBL149676 IC50 = 16.0 nM 7.80
CHEMBL345721 IC50 = 19.0 nM 7.72
CHEMBL424133 LY-518674 IC50 = 24.0 nM 7.62
CHEMBL148774 IC50 = 27.0 nM 7.57
CHEMBL278590 GSK-9578 IC50 = 120.0 nM 6.92
CHEMBL356170 IC50 = 220.0 nM 6.66
CHEMBL149438 IC50 = 250.0 nM 6.60
CHEMBL147086 IC50 = 960.0 nM 6.02
CHEMBL981 FENOFIBRIC ACID IC50 = 24000.0 nM 4.62