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A guide to picking the most selective kinase inhibitor tool compounds for pharmacological validation of drug targets
July 5, 2012
CiteULike: rajarshi's library
British Journal of Pharmacology, Vol. 166, No. 3. (2012), pp. 858-876, doi:10.1111/j.1476-5381.2012.01859.x To establish the druggability of a target, genetic validation needs to be supplemented with pharmacological validation. Pharmacological studies, especially in the kinase field, are hampered by the fact that many reference inhibitors are not fully selective for one target. Fortunately, the initial trickle of selective inhibitors released in the public domain has steadily swelled into a stream. However, rationally picking the most selective tool compound out of the increasing amounts of available inhibitors has become progressively difficult due to the lack of accurate quantitative descriptors of drug selectivity. A recently published approach, termed ‘selectivity entropy’, is an improved way of expressing selectivity as a single-value parameter and enables rank ordering of inhibitors. We provide a guide to select the best tool compounds for pharmacological validation experiments... -
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