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Assay Detail

CHEMBL829956

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
In vitro inhibition of 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

Conversion of human-selective PPARalpha agonists to human/mouse dual agonists: a molecular modeling analysis.
Wang M, Winneroski LL, Ardecky RJ, Babine RE, Brooks DA, Etgen GJ, Hutchison DR, Kauffman RF, Kunkel A, Mais DE, Montrose-Rafizadeh C, Ogilvie KM, Oldham BA, Peters MK, Rito CJ, Rungta DK, Tripp AE, Wilson SB, Xu Y, Zink RW, McCarthy JR.
Bioorg Med Chem Lett (2004) 14 : 6113 -6116
PubMed 15546740 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 6.77 7.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL81248 1 7.68
CHEMBL82034 1 7.38
CHEMBL366138 1 7.19
CHEMBL366335 1 6.88
CHEMBL187258 1 6.83
CHEMBL81676 1 6.78
CHEMBL362759 1 6.71
CHEMBL189712 1 6.51
CHEMBL363018 1 6.43
CHEMBL312717 1 6.30
CHEMBL412371 1 5.81

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL81248 IC50 = 21.0 nM 7.68
CHEMBL82034 IC50 = 42.0 nM 7.38
CHEMBL366138 IC50 = 64.0 nM 7.19
CHEMBL366335 IC50 = 133.0 nM 6.88
CHEMBL187258 IC50 = 149.0 nM 6.83
CHEMBL81676 IC50 = 167.0 nM 6.78
CHEMBL362759 IC50 = 196.0 nM 6.71
CHEMBL189712 IC50 = 306.0 nM 6.51
CHEMBL363018 IC50 = 375.0 nM 6.43
CHEMBL312717 IC50 = 503.0 nM 6.30
CHEMBL412371 IC50 = 1546.0 nM 5.81