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Assay Detail

CHEMBL4712049

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

Binding
Inhibition of PTPN1 (unknown origin) pre-incubated for 20 mins followed by fluorescence substrate addition and measured after 120 mins by DiFMUP assay
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 1 (CHEMBL335)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

From Pyrazolones to Azaindoles: Evolution of Active-Site SHP2 Inhibitors Based on Scaffold Hopping and Bioisosteric Replacement.
Mostinski Y,Heynen GJJE,López-Alberca MP,Paul J,Miksche S,Radetzki S,Schaller D,Shanina E,Seyffarth C,Kolomeets Y,Ziebart N,de Schryver J,Oestreich S,Neuenschwander M,Roske Y,Heinemann U,Rademacher C,Volkamer A,von Kries JP,Birchmeier W,Nazaré M
J Med Chem (2020) 63 : 14780 -14804
PubMed 33210922 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 6.39 6.39

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4750435 1 6.39

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4750435 IC50 = 410.0 nM 6.39