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Assay Detail

CHEMBL4121954

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

Binding
Inhibition of allosterically sensitized mutant form of His6-tagged human HePTP catalytic domain overexpressed in Escherichia coli crude cell lysate using pNPP as substrate incubated for 90 mins by quenched phosphatase activity assay
1
Total Activities
1
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

Tyrosine-protein phosphatase non-receptor type 7 (CHEMBL2219)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Optimized allosteric inhibition of engineered protein tyrosine phosphatases with an expanded palette of biarsenical small molecules.
Korntner S, Pomorski A, Krężel A, Bishop AC.
Bioorg Med Chem (2018) 26 : 2610 -2620
PubMed 29673715 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 6.60 6.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL454668 1 6.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL454668 IC50 = 250.0 nM 6.60