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. Author manuscript; available in PMC: 2019 Feb 8.
Published in final edited form as: J Med Chem. 2018 Jan 5;61(3):1182–1203. doi: 10.1021/acs.jmedchem.7b01654

Table 3.

SAR of the linker

graphic file with name nihms967105u4.jpg
Compound −X− pKa(N1)a Tb IC50,b μM Hs IC50,c μM Tb427 EC50,d μM
7 −NH− 7.3 3.7 (3.3–4.1) 27% at 180 5.6 (4.5–7.1)
28 −NMe− 7.2 81 (74–89) >180 38 (34–43)
29 −S− 4.3 >180 >180 >25
30 −NH(CH2)− 8.1 139 (130–150) >180 11 (9.9–13)
31 −NH(CH2)2− 8.2 28 (25–32) 29% at 180 5.7 (1.6–21)
a, b, c, d

See footnotes for Table 1.