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Assay Detail

CHEMBL4668476

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

Binding
Allosteric inhibition of dPEG8 peptide-activated SHP2 (unknown origin) using DiFMUP as substrate preincubated for 30 followed by substrate addition and measured after 30 mins by fluorescence method
5
Total Activities
5
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 5 8.25 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4752599 1 8.52
CHEMBL4789817 1 8.40
CHEMBL4752704 1 8.15
CHEMBL4761760 1 8.10
CHEMBL4792498 1 8.08

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4752599 IC50 = 3.0 nM 8.52
CHEMBL4789817 IC50 = 4.0 nM 8.40
CHEMBL4752704 IC50 = 7.0 nM 8.15
CHEMBL4761760 IC50 = 8.0 nM 8.10
CHEMBL4792498 IC50 = 8.3 nM 8.08