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. Author manuscript; available in PMC: 2019 Feb 15.
Published in final edited form as: Bioorg Med Chem Lett. 2018 Jan 12;28(4):694–699. doi: 10.1016/j.bmcl.2018.01.015

Table 1.

Structural characteristics and inhibitory potency against R132H mutant IDH1 for the synthesized compounds.

Compound M. Wt. clogP Polar Surface Area (PSA) IC50 vs. IDH1-R132H (μM)
AGI-5198 462.6 4.7 65.0 0.03
1 570.5 5.7 65.0 <0.01
2 492.6 5.8 73.8 1.39
3 535.6 6.4 70. 7 26.31