Kits for determining the interaction of a test compound with two associated receptors

摘要

A kit for determining whether and/or the extent to which a test compound interacts with a second receptor when the second receptor is associated with a first receptor, the first receptor being different from the second receptor, the kit comprising: (i) a first receptor coupled to a first reporter component; (ii) an interacting group coupled to a second reporter component; and (iii) a second receptor capable of associating with the interacting group, wherein proximity of the first and second reporter components generates a signal; wherein the test compound is capable of modulating the association of the interacting group with the second receptor by interacting with the second receptor, either alone, or simultaneously with the first receptor. A kit for screening a test compound for selective activity against a heterodimer of a first receptor and a second receptor, the kit comprising: (a) said test compound at increasing concentrations and (b) a system comprising: (i) a first receptor coupled to a first reporter component; ii) an interacting group coupled to a second reporter component; and iii) a second receptor, wherein the second receptor is different from the first receptor; the second receptor capable of associating with the interacting group, wherein proximity of the first and second reporter components generates a signal; wherein the test compound is capable of modulating the association of the interacting group with the second receptor by interacting with the second receptor, either alone, or simultaneously with the first receptor; wherein the signal is a determination of whether said test compound modulates said association of the interacting group with the second receptor at each concentration to produce a dose-response curve; and wherein a Hill slope of the dose-response curve in excess of 1 indicates interaction of the test compound with the hetero-dimer.