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Assay Detail

CHEMBL3398879

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

Binding
Inhibition of STEP (unknown origin) pre-incubated for 10 mins before addition of p-nitrophenyl phosphate substrate in presence of 1 mM GSH
10
Total Activities
10
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

Tyrosine-protein phosphatase non-receptor type 5 (CHEMBL2007628)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis of benzopentathiepin analogs and their evaluation as inhibitors of the phosphatase STEP.
Baguley TD, Nairn AC, Lombroso PJ, Ellman JA.
Bioorg Med Chem Lett (2015) 25 : 1044 -1046
PubMed 25666825 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 4.70 5.06

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3398242 1 5.06
CHEMBL3398246 1 4.82
CHEMBL3398244 1 4.77
CHEMBL3398243 1 4.77
CHEMBL3398250 1 4.70
CHEMBL3398247 1 4.62
CHEMBL3398249 1 4.57
CHEMBL3398245 1 4.48
CHEMBL3398251 1 4.47
CHEMBL3398248 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3398242 IC50 = 8800.0 nM 5.06
CHEMBL3398246 IC50 = 15000.0 nM 4.82
CHEMBL3398244 IC50 = 17000.0 nM 4.77
CHEMBL3398243 IC50 = 17000.0 nM 4.77
CHEMBL3398250 IC50 = 20000.0 nM 4.70
CHEMBL3398247 IC50 = 24000.0 nM 4.62
CHEMBL3398249 IC50 = 27000.0 nM 4.57
CHEMBL3398245 IC50 = 33000.0 nM 4.48
CHEMBL3398251 IC50 = 34000.0 nM 4.47
CHEMBL3398248 IC50 > 50000.0 nM -