TABLE 1

Selectivity of JNJ-1930942 toward various nAChR subtypes and 5-HT3A receptors measured by Ca2+-fluorometry (n = 1–3)

ReceptorAgonism pEC50Antagonism pIC50PAM pEC50
α7 nAChR
    Human<4.5N.D.5.7
    MouseN.D.N.D.5.4
    RatN.D.N.D.5.2
Human α4β2-nAChR<4.5<4.5<4.5
Human α3β4-nAChR<4.5<4.5<4.5
Human 5-HT3A<4.5<4.5<4.5

  • N.D., not determined.