five

Crystallographically confirmed fragment hits.

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aPrimary screening data, expressed as the mean ± standard deviation for triplicate determinations at a compound concentration of 300 µM. The positive control compound 27 (See Figure S4 for details) gave a percentage inhibition of 62.7±2.2 at a concentration of 10 µM. bMean ± standard deviations for triplicate measurements. The positive control compound 28 (See Figure S4 for details) gave an IC50 value of 0.37±0.1 µM. cThe highest value of two independent measurements. dMean ΔTm, ligand of two independent measurements. The positive control ATP gave a ΔTm, ligand of 7.2°C at a concentration of 2 mM. eLigand efficiencies were calculated using the mean mobility shift assay IC50 values [84]. fValue from a single measurement.
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