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Assay Detail

CHEMBL760605

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Functional
Cotransfection activity against human Peroxisome proliferator activated receptor alpha
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
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
EC50 11 7.09 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL148639 1 8.70
CHEMBL344282 1 8.40
CHEMBL149676 1 8.22
CHEMBL345721 1 7.51
CHEMBL424133 LY-518674 2.0 1 7.38
CHEMBL149438 1 7.25
CHEMBL148774 1 7.06
CHEMBL356170 1 6.66
CHEMBL359053 1 5.66
CHEMBL147086 1 5.57
CHEMBL148856 1 5.55

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL148639 EC50 = 2.0 nM 8.70
CHEMBL344282 EC50 = 4.0 nM 8.40
CHEMBL149676 EC50 = 6.0 nM 8.22
CHEMBL345721 EC50 = 31.0 nM 7.51
CHEMBL424133 LY-518674 EC50 = 42.0 nM 7.38
CHEMBL149438 EC50 = 56.0 nM 7.25
CHEMBL148774 EC50 = 88.0 nM 7.06
CHEMBL356170 EC50 = 220.0 nM 6.66
CHEMBL359053 EC50 = 2200.0 nM 5.66
CHEMBL147086 EC50 = 2700.0 nM 5.57
CHEMBL148856 EC50 = 2800.0 nM 5.55