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Assay Detail

CHEMBL4158239

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

Binding
Inhibition of recombinant human cytosolic PTPepsilon expressed in Escherichia coli BL21 (DE3) using E527-P-Q-pY530-Q-P-G-E-N-L536 as substrate after 60 mins by malachite green assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Receptor-type tyrosine-protein phosphatase epsilon (CHEMBL4850)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Identification of N-(5-(phenoxymethyl)-1,3,4-thiadiazol-2-yl)acetamide derivatives as novel protein tyrosine phosphatase epsilon inhibitors exhibiting anti-osteoclastic activity.
Ku B, Yun HY, Lee KW, Shin HC, Lee SR, Kim CH, Park H, Yi KY, Lee CH, Kim SJ.
Bioorg Med Chem (2018) 26 : 5204 -5211
PubMed 30249496 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 5.57 5.73

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4174865 1 5.73
CHEMBL4160163 1 5.70
CHEMBL4170383 1 5.61
CHEMBL4168082 1 5.43
CHEMBL4159748 1 5.38

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4174865 IC50 = 1860.0 nM 5.73
CHEMBL4160163 IC50 = 2010.0 nM 5.70
CHEMBL4170383 IC50 = 2470.0 nM 5.61
CHEMBL4168082 IC50 = 3700.0 nM 5.43
CHEMBL4159748 IC50 = 4170.0 nM 5.38