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. Author manuscript; available in PMC: 2022 Mar 31.
Published in final edited form as: J Med Chem. 2021 Apr 6;64(8):4913–4946. doi: 10.1021/acs.jmedchem.1c00019

Figure 1.

Figure 1.

Figure 1.

A. Schematic for primary biochemical qHTS assay; B. Assay performance as measured by Z’ factor and S:B ratio; C. Workflow for the identification of small molecule inhibitors of mutant IDH1; D. Dose-dependent activity of hit 1 against R132H mIDH1, IDH-WT, and in a readout interference counterscreen.