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. Author manuscript; available in PMC: 2022 Sep 9.
Published in final edited form as: J Med Chem. 2021 Aug 26;64(17):12705–12722. doi: 10.1021/acs.jmedchem.1c00759

Table 4.

Fraction Unbound ( f u ) in Mouse Plasma and Brain Homogenate of the Selected Nln Activators a

compound A50 (μM; 95% CI) fu in plasma fu in brain
1 (His–Tyr) 85.5 (65.1 to 112.2) 0.66 ± 0.08 N.D.b
4 (His–Trp) 39.4 (27 to 57.4) 0.93 ± 0.13 N.D.
9d 6.3 (4.3 to 9.2) 0.63 ± 0.076 0.14 ± 0.012
10c 4.2 (3.17 to 5.6) 0.45 ± 0.013 0.052 ± 0.003
11a 7.0 (4.9 to 9.9) 0.41 ± 0.081 0.062 ± 0.011
a

Data expressed as the mean of three experiments ± SD.

b

Not determined.