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Assay Detail

CHEMBL4431937

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

Binding
Inhibition of SHP2 in human KYSE520 cells assessed as inhibition of ERK phosphorylation measured after 2 hrs by AlphaScreen assay
3
Total Activities
3
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

Allosteric Inhibition of SHP2: Identification of a Potent, Selective, and Orally Efficacious Phosphatase Inhibitor.
Garcia Fortanet J, Chen CH, Chen YN, Chen Z, Deng Z, Firestone B, Fekkes P, Fodor M, Fortin PD, Fridrich C, Grunenfelder D, Ho S, Kang ZB, Karki R, Kato M, Keen N, LaBonte LR, Larrow J, Lenoir F, Liu G, Liu S, Lombardo F, Majumdar D, Meyer MJ, Palermo M, Perez L, Pu M, Ramsey T, Sellers WR, Shultz MD, Stams T, Towler C, Wang P, Williams SL, Zhang JH, LaMarche MJ.
J Med Chem (2016) 59 : 7773 -7782
PubMed 27347692 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 6.17 6.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4060033 1 6.60
CHEMBL4540461 1 6.21
CHEMBL4445214 1 5.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4060033 IC50 = 250.0 nM 6.60
CHEMBL4540461 IC50 = 620.0 nM 6.21
CHEMBL4445214 IC50 = 1980.0 nM 5.70