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. 2018 Apr 13;9(5):472–477. doi: 10.1021/acsmedchemlett.8b00080

Table 1. Data for BMT-108908.

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assay result
rat forebrain GluN2B Ki (nM) 1.4 ± 0.5
GluN2B oocyte EP IC50 (nM) 4.2
mouse occupancy study dose (mg/kg, i.v.) 0.3, 1
ex vivo GluN2B occupancy (%) 60, 95
total plasma conc. of 7 (nM) 70 ± 5, 340 ± 35
mFST MED (mg/kg, i.v.) 0.56
ex vivo GluN2B occupancy (%) 75
total plasma conc. of 7 (nM) 150 ± 70
plasma free fraction:human, rat, mouse (%) 10, 11, 12
pKa (protonated amine), spectrophotometric 6.8
hERG PC IC50 (nM) 620