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Assay Detail

CHEMBL4668475

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

Binding
Allosteric inhibition of [H2N-LN(pY)AQLWHA(PEG8)LTI(pY)ATIRRF-amide]-activated N-terminal His6-fused human full length SHP2 (Met 1 to Arg 593 residues) expressed in Escherichia coli BL21 (DE3) cells using DiFMUP as substrate preincubated for 30 followed by substrate addition and by fluorescence method
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 Autocuration

Target

Tyrosine-protein phosphatase non-receptor type 11 (CHEMBL3864)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Recent Advances of SHP2 Inhibitors in Cancer Therapy: Current Development and Clinical Application.
Yuan X,Bu H,Zhou J,Yang CY,Zhang H
J Med Chem (2020) 63 : 11368 -11396
PubMed 32460492 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 8.82 8.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4752026 1 8.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4752026 IC50 = 1.5 nM 8.82