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Assay Detail

CHEMBL760258

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

Binding
Binding affinity for Peroxisome proliferator activated receptor gamma was determined
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Peroxisome proliferator-activated receptor gamma (CHEMBL4797)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Design, synthesis, and structure-activity relationship studies of novel 6,7-locked-[7-(2-alkoxy-3,5-dialkylbenzene)-3-methylocta]-2,4,6-trienoic acids.
Michellys PY, Ardecky RJ, Chen JH, D'Arrigo J, Grese TA, Karanewsky DS, Leibowitz MD, Liu S, Mais DA, Mapes CM, Montrose-Rafizadeh C, Ogilvie KM, Reifel-Miller A, Rungta D, Thompson AW, Tyhonas JS, Boehm MF.
J Med Chem (2003) 46 : 4087 -4103
PubMed 12954061 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 15 5.40 5.76

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL339298 1 5.76
CHEMBL129887 1 5.58
CHEMBL340555 1 5.50
CHEMBL131561 1 5.50
CHEMBL335751 1 5.37
CHEMBL340074 1 5.33
CHEMBL336086 1 5.33
CHEMBL42314 1 5.25
CHEMBL335762 1 5.18
CHEMBL337719 1 5.18
CHEMBL129976 1 -
CHEMBL132488 1 -
CHEMBL288436 1 -
CHEMBL130577 1 -
CHEMBL445634 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL339298 Ki = 1750.0 nM 5.76
CHEMBL129887 Ki = 2607.0 nM 5.58
CHEMBL340555 Ki = 3149.0 nM 5.50
CHEMBL131561 Ki = 3151.0 nM 5.50
CHEMBL335751 Ki = 4285.0 nM 5.37
CHEMBL340074 Ki = 4715.0 nM 5.33
CHEMBL336086 Ki = 4706.0 nM 5.33
CHEMBL42314 Ki = 5590.0 nM 5.25
CHEMBL335762 Ki = 6571.0 nM 5.18
CHEMBL337719 Ki = 6571.0 nM 5.18
CHEMBL129976 Ki > 10000.0 nM -
CHEMBL132488 Ki > 10000.0 nM -
CHEMBL288436 Ki > 1000.0 nM -
CHEMBL130577 Ki > 10000.0 nM -
CHEMBL445634 Ki > 10000.0 nM -