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Chembiochem. 2005 Mar;6(3):506-12.

The discovery of novel protein kinase inhibitors by using fragment-based high-throughput x-ray crystallography.

Author information

1
Astex Technology, 436 Cambridge Science Park, Milton Road, Cambridge, CB4 0QA, UK. a.gill@astex-technology.com

Abstract

This article describes the application of a high-throughput X-ray crystallographic fragment-based screening methodology to identify low-molecular-weight leads for structure-based optimisation into protein kinase inhibitors. The identification of two novel p38alpha MAP kinase inhibitors (with IC50=65 and 150 nM) starting from low-molecular-weight fragments is described.

PMID:
15696598
DOI:
10.1002/cbic.200400188
[Indexed for MEDLINE]

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