Author/Authors :
Kelly McClure، نويسنده , , Michael Hack، نويسنده , , Liming Huang، نويسنده , , Clark Sehon، نويسنده , , Magda Morton، نويسنده , , Lina Li، نويسنده , , Terrance D. Barrett، نويسنده , , Nigel Shankley، نويسنده , , J. Guy Breitenbucher، نويسنده ,
Abstract :
High throughput screening revealed compound 1 as a potent antagonist of the CCK1 receptor. Evaluation of the CCK1 SAR in a series of these diarylpyrazole antagonists was conducted in a matrix synthesis format revealing additive (Free–Wilson) and non-additive SAR. This use of additive QSAR modeling in conjunction with combinatorial libraries represents a unique approach to the evaluation of SAR interactions between the variables of any combinatorial matrix.
Keywords :
combinatorial , Additivity , Pyrazole , CCK1 , cholecystokinin