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MK-3697
CAS No. : 1224846-01-8
Biological Activity：MK-3697 is an isonicotinamide small molecule, acting as a potent and selective Orexin 2 receptor antagonist with Ki = 0.95 nM.
IC50 value: 0.95 nM(Ki)
Target: Orexin 2 receptor antagonist
MK-3697 is a highly potent, orally bioavailable selective orexin 2 receptor antagonists (2-SORAs) that possess acceptable profiles for clinical development. Herein we report additional SAR studies within the “triaryl” amide 2-SORA series focused on improvements in compound stability in acidic media and time-dependent inhibition of CYP3A4. MK-3697 has improved stability and TDI profiles as well as excellent sleep efficacy across species.
Research Area：Neurological Disease|Endocrinology
Targets：Orexin Receptor (OX Receptor)
Related Screening Libraries:Bioactive Compound Library Plus;GPCR/G Protein Compound Library;Neuronal Signaling Compound Library;Endocrinology Compound Library;Orally Active Compound Library;
Related Small Molecules:JNJ-54717793;TCS-OX2-29;IPSU;Seltorexant hydrochloride;Orexin B, rat, mouse;SB-649868;Orexin A (human, rat, mouse) (acetate);SB-408124 Hydrochloride;OX2R-IN-1;EMPA;Orexin B, human;SB-334867 free base;MK-1064;Almorexant-13C,d3;YNT-185 dihydrochloride;Orexin 2 Receptor Agonist;[Ala11,D-Leu15]-Orexin B(human);Suntinorexton;Almorexant;SB-674042;Filorexant;Orexin receptor antagonist 4;OXA(17-33) TFA;Lemborexant;Danavorexton
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