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Non-endogenous, constitutively activated known G protein-coupled receptors

  • US 7,381,522 B2
  • Filed: 04/14/2006
  • Issued: 06/03/2008
  • Est. Priority Date: 04/07/2000
  • Status: Expired due to Fees
First Claim
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1. A method for directly identifying a non-endogenous compound as a compound having inverse agonist, agonist, or partial agonist activity to a non-endogenous, constitutively activated version of a known G protein-coupled receptor, wherein said non-endogenous, constitutively activated version comprises the amino acid sequence of SEQ.ID.No.:

  • 471, said method comprising;

    (a) contacting a non-endogenous candidate compound with said non-endogenous, constitutively activated version of the known GPCR comprising the amino acid sequence of SEQ.ID.No.;

    471; and

    (b) measuring the compound efficacy at said contacted receptor, and identifying whether said non-endogenous compound has inverse agonist activity, agonist activity, or partial agonist activity at said contacted receptor.

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