A High-Throughput Screening-Compatible Strategy for the Identification of Inositol Pyrophosphate Kinase Inhibitors
Fig 2
Application of the PKIS library to judge performance of the HTS assay.
(A) Representative technical replicates measured on the same day. (B) Comparison of the mean values of biological replicates (black and white circles) obtained on two different days. R2 = 0.98. (C) Z’ Factor (0.78 ± 0.03) (D) %CV (7.5 ± 1.6) (E) Signal:background ratio (15.8 ± 1.5) (F) These plates included negative controls (DMSO; gray circles, broken line and positive controls (100 μM UNC10225354; gray square, broken line). Each plate also contained one 10-point titration for UNC10225354; data (black circles) depict means and SEMs (n = 5). IC50 = 4.8 ± 0.3 μM. In these experiments, 100% activity is equivalent to consumption of 19.3 ± 1.1% of the ATP.