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Assay Detail

CHEMBL4668494

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Binding
Inhibition of N-terminal His6-tagged TEV cleavage site-fused human SHP2 (225 to 541 residues) expressed in Escherichia coli BL21(DE3)RILcodon+ or BL21(DE3)RPcodon+ using 4-nitrophenylphosphate as substrate
2
Total Activities
2
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 2 5.94 6.20

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4757579 1 6.20
CHEMBL1765357 1 5.68

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4757579 IC50 = 630.0 nM 6.20
CHEMBL1765357 IC50 = 2100.0 nM 5.68