High-throughput receptor-binding methods for somatostatin receptor 2

Three high-throughput screening methods for quantitating I-125-SS14 binding to human somatostatin receptor 2 (hSST2) have been developed. Microplate-based separation assays were performed in Packard Unifilter and Millipore Multiscreen plates. A homogeneous ligand-binding assay was developed by employing wheat germ agglutinin (WGA)-coated Flashplates. Apparent dissociation constants for I-125-SS14 binding to hSST2 were obtained with each method. IC50 values were determined for 12 compounds using each of the methods. Similar IC50 Values were obtained for each compound with all of the methods. The WGA-Flashplate is suitable for fully automated high-throughput screening whereas the Unifilter and Multiscreen methods are more suitable for semiautomated and manual screening applications. (C) 2002 Elsevier Science (USA). All rights reserved.