Enamine Library SPR Screening results
The Enamine library (654 compounds) was screened against PaMurC, PaMurD, PaMurE using the Biacore T200.
The experiments were run with a running buffer containing 20 mM HEPES pH 7.5, 200 mM NaCl, 10 mM MgCl2, and 5% DMSO. Proteins PaMurC/D/E were immobilised in an NTA sensor using His6-tagged proteins and amine coupling. The first single shot screen was performed at concentrations of 500 uM. Results were analysed and the top 32 compounds inhibiting at least two Mur ligases were selected for dose response experiments.
The results are summarised in the following table. The last column collects the percentage of activity shown at the enzymatic assay screens carried out by Becca on SagaMurD. Full validation with activity assays should be considered.
*nsb = none specific binding
