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Identification of kinase inhibitors

  • US 20030232391A1
  • Filed: 03/20/2003
  • Published: 12/18/2003
  • Est. Priority Date: 03/21/2002
  • Status: Active Grant
First Claim
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1. A method for identifying a ligand binding to an inactive conformation of a target protein kinase, comprising (a) contacting the inactive conformation of said target protein kinase, which contains or is modified to contain a reactive group at or near a binding site of interest, with one or more ligand candidates capable of covalently bonding to said reactive group thereby forming a kinase-ligand conjugate;

  • and (b) detecting the formation of said kinase-ligand conjugate and identifying the ligand present in said kinase-ligand conjugate.

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