Assay Method Information |
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| SAR Selectivity Analysis of small molecule inhibitors of PEST using pCAP in a fluorescence assay |
Description: | Data Source: Sanford-Burnham Center for Chemical Genomics (SBCCG) Source Affiliation: Sanford-Burnham Medical Research Institute (SBMRI, San Diego, CA) Network: NIH Molecular Libraries Probe Production Centers Network(MLPCN) Grant Number: 1R21NS056945-01 Assay Provider: Dr. Nunzio Bottini, La Jolla Institute for Allergy and Immunology, La Jolla, CA PTP-PEST, encoded by PTPN12 gene, is a protein tyrosine phosphatase that contains a C-terminal PEST motif, which serves as a protein-protein interaction domain. This PTP dephosphorylates c-ABL, and may play a role in oncogenesis. This is a selectivity counterscreen to aid with identification of specific inhibitors of LYP phosphatase (AID 2135). This assay uses a phosphorylated coumarin amino acid (pCAP) moiety attached to a 14-mer peptide, which is a substrate for LYP. This dose response assay is developed and performed to assess selectivity of hits originally found in "uHTS identification of small molecule inhibitors of LYP via a fluo |
Affinity data for this assay | |
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