Showing papers on "Chemical library published in 1998"

Exploiting chemical libraries, structure, and genomics in the search for kinase inhibitors.

Abstract: Selective protein kinase inhibitors were developed on the basis of the unexpected binding mode of 2,6,9-trisubstituted purines to the adenosine triphosphate-binding site of the human cyclin-dependent kinase 2 (CDK2). By iterating chemical library synthesis and biological screening, potent inhibitors of the human CDK2-cyclin A kinase complex and of Saccharomyces cerevisiae Cdc28p were identified. The structural basis for the binding affinity and selectivity was determined by analysis of a three-dimensional crystal structure of a CDK2-inhibitor complex. The cellular effects of these compounds were characterized in mammalian cells and yeast. In the latter case the effects were characterized on a genome-wide scale by monitoring changes in messenger RNA levels in treated cells with high-density oligonucleotide probe arrays. Purine libraries could provide useful tools for analyzing a variety of signaling and regulatory pathways and may lead to the development of new therapeutics.

Method of generating chemical compounds having desired properties

Abstract: A computer based, iterative process for generating chemical entities with defined physical, chemical and/or bioactive properties. During each iteration of the process, (1) a directed diversity chemical library is robotically generated in accordance with robotic synthesis instructions; (2) the compounds in the directed diversity chemical library are analyzed to identify compounds with the desired properties; (3) structure-property data are used to select compounds to be synthesized in the next iteration; and (4) new robotic synthesis instructions are automatically generated to control the synthesis of the directed diversity chemical library for the next iteration.

Method of purifying and identifying a large multiplicity of chemical reaction products simultaneously

Abstract: The invention provides a system utilizing computer databases, high pressure liquid chromatography and mass spectrometry to isolate, purify and identify compounds present in a chemical library of reaction products, especially products of liquid phase (solution) chemical reaction, to produce a purified chemical library with each purified compound tracked to the reaction product from which it originated.

Radiofrequency encoded chemical library synthesis particles

Abstract: A radiofrequency encoded chemical library synthesis particle which comprises a read-only radiofrequency tag linked to a solid phase. Chemical libraries synthesised on such particles and their use in biological screening methods.

Process for the preparation of a chemical library

Abstract: A method for the preparation of a chemical library, which method comprises synthesising the library on a plurality of synthesis particles comprising random features, recording such features during library synthesis, so as to provide a chemical library on a plurality of synthesis particles and wherein the identity of library compound(s) associated with a synthesis particle is established by reference to the particle's random features.

Method for the preparation of a chemical library

Abstract: A method for the preparation of a chemical library, which method comprises synthesising the library on a plurality of individually coded synthesis particles and wherein the particles are tracked during library synthesis under the control of robotic apparatus.