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Assay Detail

CHEMBL5145447

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

Binding
Reversible inhibition of wild-type human SHP2 using DiFMUP as substrate and measured by jump dilution assay
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

Structure-based design, synthesis and biological evaluation of aminopyrazines as highly potent, selective, and cellularly active allosteric SHP2 inhibitors.
Tang K, Zhao M, Wu YH, Wu Q, Wang S, Dong Y, Yu B, Song Y, Liu HM.
Eur J Med Chem (2022) 230 : 114106 -114106
PubMed 35063735 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 2 7.42 7.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4789106 1 7.66
CHEMBL4060033 1 7.17

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4789106 Ki = 22.0 nM 7.66
CHEMBL4060033 Ki = 67.0 nM 7.17