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Assay Detail

CHEMBL935696

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

Binding
Binding affinity at human PPARalpha by fluorescence polarization
21
Total Activities
21
Compounds Tested
1
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

Design, synthesis, and structure-activity relationships of piperidine and dehydropiperidine carboxylic acids as novel, potent dual PPARalpha/gamma agonists.
Ye XY, Li YX, Farrelly D, Flynn N, Gu L, Locke KT, Lippy J, O'Malley K, Twamley C, Zhang L, Ryono DE, Zahler R, Hariharan N, Cheng PT.
Bioorg Med Chem Lett (2008) 18 : 3545 -3550
PubMed 18511276 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 21 6.16 7.47

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL255309 1 7.47
CHEMBL403432 1 7.31
CHEMBL256142 1 7.06
CHEMBL257345 1 6.96
CHEMBL256358 1 6.89
CHEMBL401534 1 6.88
CHEMBL186179 MURAGLITAZAR 3.0 1 6.72
CHEMBL255872 1 6.54
CHEMBL257164 1 6.35
CHEMBL257165 1 5.90
CHEMBL256569 1 5.88
CHEMBL255271 1 5.86
CHEMBL257180 1 5.52
CHEMBL255097 1 5.51
CHEMBL256134 1 5.35
CHEMBL402956 1 5.33
CHEMBL258212 1 5.22
CHEMBL255251 1 5.13
CHEMBL445942 1 5.11
CHEMBL256505 1 -
CHEMBL258428 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL255309 IC50 = 34.0 nM 7.47
CHEMBL403432 IC50 = 49.0 nM 7.31
CHEMBL256142 IC50 = 88.0 nM 7.06
CHEMBL257345 IC50 = 110.0 nM 6.96
CHEMBL256358 IC50 = 130.0 nM 6.89
CHEMBL401534 IC50 = 133.0 nM 6.88
CHEMBL186179 MURAGLITAZAR IC50 = 190.0 nM 6.72
CHEMBL255872 IC50 = 287.0 nM 6.54
CHEMBL257164 IC50 = 450.0 nM 6.35
CHEMBL257165 IC50 = 1250.0 nM 5.90
CHEMBL256569 IC50 = 1320.0 nM 5.88
CHEMBL255271 IC50 = 1384.0 nM 5.86
CHEMBL257180 IC50 = 3036.0 nM 5.52
CHEMBL255097 IC50 = 3089.0 nM 5.51
CHEMBL256134 IC50 = 4510.0 nM 5.35
CHEMBL402956 IC50 = 4730.0 nM 5.33
CHEMBL258212 IC50 = 6030.0 nM 5.22
CHEMBL255251 IC50 = 7400.0 nM 5.13
CHEMBL445942 IC50 = 7692.0 nM 5.11
CHEMBL256505 IC50 > 27500.0 nM -
CHEMBL258428 IC50 > 27300.0 nM -