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. Author manuscript; available in PMC: 2023 Sep 8.
Published in final edited form as: Angew Chem Int Ed Engl. 2018 May 9;57(24):7220–7224. doi: 10.1002/anie.201801666

Figure 2. Interaction of 5-iTU with various human kinases.

Figure 2

A) Temperature shift assays show high ΔTm values preferentially for kinases harboring an aromatic gatekeeper. B) The distribution of gatekeeper residues reveals that the majority of high-ΔTm hits harbor a phenylalanine gatekeeper. C) The binding mode of 5-iTU in the off-target CLK1, including the iodide–gatekeeper interaction, is highly conserved. CLK1 has a high affinity for 5-iTU as measured by ITC (D) and indicated by a slow off-rate (E), as assessed by BLI.