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Design of a Potent, Soluble Glucokinase Activator With Increased Pharmacokinetic Half-Life

Kurt G Pike, Joanne V Allen, Peter W R Caulkett, David S Clarke, Craig S Donald, Mark L Fenwick, Keith M Johnson, Craig Johnstone, Darren McKerrecher, John W Rayner, Rolf P Walker, Ingrid Wilson

Bioorg Med Chem Lett. 2011 Jun 1;21(11):3467-70.

PMID: 21515051

Abstract:

The continued optimization of a series of glucokinase activators is described, including attempts to understand the interplay between molecular structure and the composite parameter of unbound clearance. These studies resulted in the discovery of a new scaffold for glucokinase activators and further exploration of this scaffold led to the identification of GKA60. GKA60 maintains an excellent balance of potency and physical properties whilst possessing a significantly different, but complimentary, pre-clinical pharmacokinetic profile compared with the previously disclosed compound GKA50.

Chemicals Related in the Paper:

Catalog Number Product Name Structure CAS Number Price
AP851884872 GKA50 GKA50 851884-87-2 Price
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