PT  - JOURNAL ARTICLE
AU  - Rafael M. Couñago
AU  - Alison D. Axtman
AU  - Stephen J. Capuzzi
AU  - Hátylas Azevedo
AU  - David H. Drewry
AU  - Jonathan M. Elkins
AU  - Opher Gileadi
AU  - Cristiano R. W. Guimarães
AU  - Alessandra Mascarello
AU  - Ricardo A. M. Serafim
AU  - Carrow I. Wells
AU  - Timothy M. Willson
AU  - William J. Zuercher
TI  - Development of Narrow Spectrum ATP-competitive Kinase Inhibitors as Probes for BIKE and AAK1
AID  - 10.1101/094631
DP  - 2017 Jan 01
TA  - bioRxiv
PG  - 094631
4099  - http://biorxiv.org/content/early/2017/03/02/094631.short
4100  - http://biorxiv.org/content/early/2017/03/02/094631.full
AB  - Understanding the structural determinants of inhibitor selectivity would facilitate the design and preparation of kinase probes. We describe a pair of matched compounds differing only by one degree of saturation but showing dramatic differential activities at select kinases. We utilized x-ray crystallography and computational analysis to rationalize the basis of the differential activity.