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Approaches to Kinase Lead Generation

AstraZeneca, Oncology Innovative Medicines, Alderley Park, Macclesfield, SK10 4TG, UK [Pg.54]

RSC Drug Discovery Series No. 19 Kinase Drug Discovery [Pg.54]

In a similar manner, allosteric kinase inhibitors can be discovered by spin-labeled adenine analogs (Fig. 15.2-8(b)). The degree of paramagnetic relaxation enhancement allows an estimation of the distance of the ligand relative to the spin label. This method is ideally suited to the fragment-linking approach of lead generation [79, 80],... [Pg.878]

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Leads generation

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