Patent ID: 6806054
Filing Date: 2004-10-19
Classification: A61K,C07K,G01N

Abstract:
A method for directly identifying a non-endogenous compound as a compound having an activity selected from the group consisting of: inverse agonists, agonists, and partial agonists, to a non-endogenous, constitutively activated version of a known G protein-coupled receptor, said receptor comprising a transmembrane-6 region and an intracellular region, comprising the steps of:(a) selecting a non-endogenous version of a known GPCR; (b) confirming that the selected non-endogenous GPCR of step (a) is constitutively active; (c) contacting a non-endogenous candidate compound with the non-endogenous, constitutively activated GPCR of step of (b); and (d) determining, by measurement of the compound efficacy at said contacted receptor, whether said non-endogenous compound is an inverse agonist, an agonist, or a partial agonist to said receptor of step (b); wherein said receptor of step (b) comprises the amino acid sequence of SEQ ID NO:449.