TABLE 1

Analogs of MLS1547 active in cAMP assays yet lacking β-arrestin recruitment activity

The compounds were assayed in agonist mode using the DiscoveRx cAMP and β-arrestin assays as described in Materials and Methods.

StructureCompound IDD2R cAMP ResponseD2R β-Arrestin Recruitment
Emax (% Control ± S.E.M.)EC50 (μM ± S.E.M.)Log (Emax/EC50)Emax (% Control ± S.E.M.)EC50 (μM ± S.E.M.)
Embedded ImageMLS00005154797.1 ± 3.70.26 ± 0.072.57InactiveNA
Embedded ImageNCGC0031912487.3 ± 14.75.5 ± 0.91.20InactiveNA
Embedded ImageNCGC0031912793.9 ± 4.64.7 ± 1.71.30InactiveNA
Embedded ImageNCGC0031912566.8 ± 3.92.8 ± 1.21.38InactiveNA
Embedded ImageNCGC0034638794.8 ± 2.11.4 ± 0.81.83InactiveNA
Embedded ImageNCGC0031914189.5 ± 5.20.7 ± 0.72.11InactiveNA
Embedded ImageMLS00086044984.9 ± 2.74.5 ± 3.01.28InactiveNA
Embedded ImageNCGC031912974.8 ± 23.89.5 ± 5.60.90InactiveNA
Embedded ImageNCGC0031912662.8 ± 7.71.1 ± 0.61.76InactiveNA
Embedded ImageDopamine1000.06 ± 0.023.221000.09 ± 0.03
  • NA, not applicable.