N-desmethyl Zolmitriptan (DZT) is an active metabolite of the serotonin (5-HT) receptor subtype 5-HT1B and 5-HT1D agonist zolmitriptan . DZT is an agonist of 5-HT1B receptors that induces contraction of isolated human cerebral arteries (EC50 = 100 nM).
PF-05139962 is a novel potent mTOR inhibitor with excellent mTOR biochemical inhibition, cellular potency, kinase selectivity and in vitro ADME properties. PF-05139962 has pS473 and pS6 cellular IC50 = 48 and 6 nM respectively. PF-05139962 has great selectivity against other receptors and kinases. No genotoxicity was observed on this compound and no more than 25% inhibiton was observed for major CYP enzymes (3A4, 1A2, 2C9, 2D6) at 3 uM. This compound has LE = 0.35 and LipE up to 6.8 which is in a very desirable range for a kinase inhibitor.