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Quantitative high-throughput screen of 15-PGDH.

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posted on 2010-11-02, 00:27 authored by Frank H. Niesen, Lena Schultz, Ajit Jadhav, Chitra Bhatia, Kunde Guo, David J. Maloney, Ewa S. Pilka, Minghua Wang, Udo Oppermann, Tom D. Heightman, Anton Simeonov

A. Plot of the Z' factor associated with each plate, showing high stability over the entire duration of the screen (completed in five days). The average Z' was 0.86. B. Hit frequency for the library of tested compounds, measured as the distribution of compounds according to binned potencies. C. Typical effect of a non-fluorescent screening hit (inhibitor 13, titrated between 3.5 nM and 57.5 µM) on the time course of NAD+-reduction upon addition of PGE2. D. Dose-dependent reduction in enzyme activity caused by compound 13, as detected during the screen.