L. A. Dakin et al. / Bioorg. Med. Chem. Lett. 22 (2012) 4599–4604
4603
Figure 3. Example 23 tested in the Ambit kinase selectivity panel. Red circles correspond to kinases that are inhibited >65%, with size proportional to activity.25
11. Peltola, K.; Hollmen, M.; Maula, S.-M.; Rainio, E.; Ristamäki, R.; Luukkaa, M.;
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ally, we have shown the beneficial effects on the potency of this
series through the incorporation of basic amines into the ribose
pocket and the strategic placement of hydrophobic groups. Sig-
nificantly, these inhibitors have been demonstrated to have good
anti-proliferative activity in the MOLM-16 cell line, high in vitro
stability, limited hERG activity, and high aqueous solubilities. As
such, this series of PIM inhibitors is currently under further
investigation, and those findings will be reported in due course.
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Supplementary data
Supplementary data associated with this article can be found, in
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References and notes
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using Michaelis–Menten equation. PIM-1 Km [ATP] = 100
[ATP] = 5 M; PIM-3 Km [ATP] = 50 M.
lM; PIM-2 Km
l
l
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