1. Dasatinib and Iressa represent excellent test reagents for a new chemoproteomic method since their target profiles have been extensively interrogated using in vitro kinome assays in addition to orthogonal chemoproteomic methods. 2. Affinity binning possessed a high positive predictive potential for the main targets of both Iressa and Dasatinib from HeLa and K562 cellular lysates, respectively. 3. Affinity binning experiments can be conducted in a rapid format, informing on target profiles of relevant chemical matter on a time scale amenable to the progression of a drug discovery program. 4. A small number of targets from Dasatinib did not produce positive affinity binning results, potentially due to the formation of target:target complexes or from sample processing errors. 5. More complex multi-targeted inhibitors may benefit from the combination of affinity binning and competition datasets. 6. Determination of phenotype contributions from the relevant targets will require integration of the chemoproteomic datasets with pathway analyses and gene expression data.
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