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Assay Detail

CHEMBL4668490

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

Binding
Inhibition of PTP1B (unknown origin) using 6,8-difluoro-4-methylum-belliferylphosphate as substrate preincubated for 1 hr followed by substrate 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 1 (CHEMBL335)
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 5.17 5.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4762771 1 5.50
CHEMBL4784105 1 5.18
CHEMBL4780471 1 5.17
CHEMBL4746515 1 5.05
CHEMBL4750975 1 4.97

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4762771 IC50 = 3170.0 nM 5.50
CHEMBL4784105 IC50 = 6560.0 nM 5.18
CHEMBL4780471 IC50 = 6800.0 nM 5.17
CHEMBL4746515 IC50 = 8930.0 nM 5.05
CHEMBL4750975 IC50 = 10600.0 nM 4.97