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Assay Detail

CHEMBL886017

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

Binding
Effect on PPARgamma transactivation activity in HEK293 cells
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Peroxisome proliferator-activated receptor gamma (CHEMBL235)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, synthesis, and evaluation of potent, structurally novel peroxisome proliferator-activated receptor (PPAR) delta-selective agonists.
Kasuga J, Nakagome I, Aoyama A, Sako K, Ishizawa M, Ogura M, Makishima M, Hirono S, Hashimoto Y, Miyachi H.
Bioorg Med Chem (2007) 15 : 5177 -5190
PubMed 17532641 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 19 5.69 6.19

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL376165 1 6.19
CHEMBL229573 1 6.00
CHEMBL229525 1 6.00
CHEMBL375471 1 5.96
CHEMBL229778 1 5.89
CHEMBL389903 1 5.89
CHEMBL229836 1 5.85
CHEMBL229837 1 5.82
CHEMBL425666 1 5.75
CHEMBL387914 1 5.66
CHEMBL229831 1 5.64
CHEMBL390116 1 5.62
CHEMBL118939 1 5.58
CHEMBL229786 1 5.44
CHEMBL426371 1 5.21
CHEMBL427071 1 5.16
CHEMBL38943 GW501516 2.0 1 5.07
CHEMBL229785 1 -
CHEMBL229888 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL376165 EC50 = 650.0 nM 6.19
CHEMBL229573 EC50 = 1000.0 nM 6.00
CHEMBL229525 EC50 = 1000.0 nM 6.00
CHEMBL375471 EC50 = 1100.0 nM 5.96
CHEMBL229778 EC50 = 1300.0 nM 5.89
CHEMBL389903 EC50 = 1300.0 nM 5.89
CHEMBL229836 EC50 = 1400.0 nM 5.85
CHEMBL229837 EC50 = 1500.0 nM 5.82
CHEMBL425666 EC50 = 1800.0 nM 5.75
CHEMBL387914 EC50 = 2200.0 nM 5.66
CHEMBL229831 EC50 = 2300.0 nM 5.64
CHEMBL390116 EC50 = 2400.0 nM 5.62
CHEMBL118939 EC50 = 2600.0 nM 5.58
CHEMBL229786 EC50 = 3600.0 nM 5.44
CHEMBL426371 EC50 = 6200.0 nM 5.21
CHEMBL427071 EC50 = 7000.0 nM 5.16
CHEMBL38943 GW501516 EC50 = 8600.0 nM 5.07
CHEMBL229785 EC50 > 10000.0 nM -
CHEMBL229888 EC50 > 10000.0 nM -