Table 1. Data for BMT-108908.
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 |