Small ligands interacting with the phosphotyrosine binding pocket of the Src SH2 protein.

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Deprez P, Mandine E, Gofflo D, Meunier S, Lesuisse D

Small ligands interacting with the phosphotyrosine binding pocket of the Src SH2 protein.

Bioorg Med Chem Lett. 2002 May 6;12(9):1295-8.

PubMed ID
11965374 [ View in PubMed
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Abstract

Various small fragments bearing phosphate, phosphonate or phosphonic acid moieties have been prepared through parallel synthesis and their binding potencies evaluated on the Src SH2 protein using a BIAcore assay. This provided us insight into the requirement of the Src SH2 pTyr binding pocket and some promising small ligands have been characterised.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
DPI59Proto-oncogene tyrosine-protein kinase SrcIC 50 (nM)>5000000N/AN/ADetails
ISO24Proto-oncogene tyrosine-protein kinase SrcIC 50 (nM)4400000N/AN/ADetails
PAS219Proto-oncogene tyrosine-protein kinase SrcIC 50 (nM)2300000N/AN/ADetails
PhenylphosphateProto-oncogene tyrosine-protein kinase SrcIC 50 (nM)2500000N/AN/ADetails
RU78262Proto-oncogene tyrosine-protein kinase SrcIC 50 (nM)200000N/AN/ADetails
RU78300Proto-oncogene tyrosine-protein kinase SrcIC 50 (nM)900000N/AN/ADetails