In vitro kinome profiling measuring drug binding

AA Albert A. Antolin
MA Malaka Ameratunga
UB Udai Banerji
PC Paul A. Clarke
PW Paul Workman
BA Bissan Al-Lazikani
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The DiscoveRx KinomeScan platform (https://www.discoverx.com), utilizing an in vitro active site-directed competition binding assay, was used to quantitatively measure interactions between the four clinical PARP inhibitors and their largest available kinase panel. At the time when the assays were performed (date: 29/11/2016), 468 in vitro binding assays were available, corresponding to 392 unique human kinases (76% of the human kinome)39 (Supplementary Table 5).

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