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This unique fluorescent probe was successfully applied to the screening of a kinase focused compound library.
PI3K and mTOR inhibitors were revealed by screening of a kinase inhibitor chemical library to positively combine with both DDR1-IN-1 and DDR1-IN-2.
The primary screening of a kinase inhibitor (KI) library comprised of 244 KIs was purchased from EMD Chemicals, and diluted with DMSO to 2 mM concentrations for high-throughput screening purposes.
In this work, we have demonstrated the potential to use WAC in combination with mass spectrometry (MS) detection for fragment screening of a kinase target cyclin G-associated kinase (GAK).
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Cell-based screening of a preselected kinase-based small molecule compound library identified A-770041 as one of the most effective drug resistance reversing agents in two osteosarcoma MDR cell line models, U-2OSMR and KHOSR2, having defined overexpression of the major MDR transporters, ABCB1/Pgp.
Herein we report a screen of a focused kinase library against T. brucei GSK3.
This work involved a high-throughput screen of a focussed kinase set of ∼3400 compounds to identify potent and parasite-selective inhibitors of an enzymatic Leishmania CRK3 cyclin 6 complex.
In summary, we have shown that a screen of a focused kinase library led to the identification of ligand-efficient inhibitors of TbGSK3 with sub-micromolar potency.
A road map of phenotypic screen of a mammalian kinase inhibitor -> target ID by chemical proteomics in gel -> chemical proteomics using ITRAQ -> RNAi screen of candidate targets -> target engagement studies -> reconfirmation with recombinant enzymes, possibly as a figure, would help.
A screen of a focused kinase inhibitor library against Trypanosoma brucei rhodesiense led to the identification of seven series, totaling 121 compounds, which showed >50%% inhibition at 5 μ m.
Finally, compounds must be able to penetrate cells and have a sufficient free fraction in the assay to elicit their response, eliminating compounds with inappropriate properties.[ 12– 14] We therefore decided to conduct a phenotypic screen of a focused kinase compound library against whole parasites.
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