Investigation of SAR requirements of SR 142801 through an indexed combinatorial library in solution

To rapidly gain information on structure-activity relationship (SAR) requirements of the human neurokinin 3 (hNK-3) receptor antagonist SR 142801, an indexed combinatorial library was synthesised in solution and screened on the hNK-3 receptor. SAR considerations drawn from binding affinity of combinatorial mixtures were confirmed through the synthesis and biological evaluation of some individual compounds.