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Assay Detail

CHEMBL980391

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

Binding
Displacement of [3H2]nTZD4 from human PPARalpha by scintillation proximity assay
23
Total Activities
23
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

Peroxisome proliferator-activated receptor alpha (CHEMBL239)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Effects of modifications of the linker in a series of phenylpropanoic acid derivatives: Synthesis, evaluation as PPARalpha/gamma dual agonists, and X-ray crystallographic studies.
Casimiro-Garcia A, Bigge CF, Davis JA, Padalino T, Pulaski J, Ohren JF, McConnell P, Kane CD, Royer LJ, Stevens KA, Auerbach BJ, Collard WT, McGregor C, Fakhoury SA, Schaum RP, Zhou H.
Bioorg Med Chem (2008) 16 : 4883 -4907
PubMed 18394907 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 6.09 6.48
Activity 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL478725 1 6.48
CHEMBL477298 1 6.28
CHEMBL104850 1 6.16
CHEMBL477095 1 6.04
CHEMBL478334 1 5.84
CHEMBL477323 1 5.72
CHEMBL515972 1 -
CHEMBL477318 1 -
CHEMBL478335 1 -
CHEMBL515181 1 -
CHEMBL477690 1 -
CHEMBL516129 1 -
CHEMBL513904 1 -
CHEMBL514696 1 -
CHEMBL479002 1 -
CHEMBL479001 1 -
CHEMBL477941 1 -
CHEMBL477940 1 -
CHEMBL476897 1 -
CHEMBL476896 1 -
CHEMBL478726 1 -
CHEMBL478563 1 -
CHEMBL477094 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL478725 IC50 = 330.0 nM 6.48
CHEMBL477298 IC50 = 529.0 nM 6.28
CHEMBL104850 IC50 = 697.0 nM 6.16
CHEMBL477095 IC50 = 912.0 nM 6.04
CHEMBL478334 IC50 = 1430.0 nM 5.84
CHEMBL477323 IC50 = 1900.0 nM 5.72
CHEMBL515972 IC50 - -
CHEMBL477318 IC50 > 3300.0 nM -
CHEMBL478335 IC50 - -
CHEMBL515181 IC50 - -
CHEMBL477690 IC50 - -
CHEMBL516129 IC50 - -
CHEMBL513904 IC50 - -
CHEMBL514696 IC50 - -
CHEMBL479002 IC50 > 3300.0 nM -
CHEMBL479001 IC50 - -
CHEMBL477941 IC50 - -
CHEMBL477940 IC50 - -
CHEMBL476897 IC50 - -
CHEMBL476896 IC50 - -
CHEMBL478726 IC50 - -
CHEMBL478563 Activity - -
CHEMBL477094 IC50 - -