| Affinity for H3Rs | Off-target binding | Log D7.4 | Efflux ratio (MDR1) | ||
---|---|---|---|---|---|---|
Rat, IC50 | Monkey, IC50 | Sigma 1, IC50 | Adrenergic α2c, IC50 | |||
nM (n = 3) | nM (n = 3) | nM | nM | |||
TASP0390136 | 2.74 | 1.06 | 167 | >1000 | 1.36 | 6.29 |
TASP0410457 | 2.34 | 1.80 | 379 | >1000 | 1.79 | 1.64 |
TASP0434988 | 0.783 | 0.565 | 257 | 528 | 2.22 | 2.14 |