TABLE 2

Analogs of MLS1547 active in both cAMP and β-arrestin assays

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 RecruitmentBias Activity
Emax (% Control ± S.E.M.)EC50 (μM ± S.E.M.)Log (Emax/EC50)Emax (% Control ± S.E.M.)EC50 (μM ± S.E.M.)Log (Emax/EC50)
Embedded ImageNCGC0031913995.5 ± 2.00.03 ± 0.013.5089.3 ± 9.42.0 ± 0.51.651.85
Embedded ImageNCGC0031913784.1 ± 4.50.02 ± 0.0013.6284.7 ± 2.51.6 ± 0.31.721.90
Embedded ImageNCGC0031913693.8 ± 1.40.1 ± 0.042.9776.4 ± 2.90.7 ± 0.072.040.93
Embedded ImageNCGC0009278577.0 ± 10.90.04 ± 0.013.2873.8 ± 1.20.4 ± 0.022.271.02
Embedded ImageNCGC0031913486.1 ± 14.40.1 ± 0.042.9474.7 ± 1.80.3 ± 0.032.400.54
Embedded ImageNCGC0031913189.6 ± 0.50.2 ± 0.12.6566.0 ± 0.20.8 ± 0.011.920.73
Embedded ImageNCGC0031913278.9 ± 100.1 ± 0.012.9059.2 ± 4.20.3 ± 0.042.300.60
Embedded ImageNCGC0031913386.5 ± 14.70.01 ± 0.0013.9487.6 ± 2.00.2 ± 0.032.641.30
Embedded ImageNCGC0031913071.0 ± 17.10.1 ± 0.022.8566.0 ± 0.22.1 ± 0.41.501.35
Embedded ImageNCGC0031913583.3 ± 14.41.4 ± 0.11.7768.9 ± 4.913.2 ± 6.60.721.06
Embedded ImageNCGC0031914092.5 ± 5.52.0 ± 0.21.6766.2 ± 18.620.5 ± 9.60.511.16
Embedded ImageNCGC0031912897.2 ± 0.70.4 ± 0.12.3970.0 ± 5.93.4 ± 0.51.311.07
Embedded ImageNCGC0034638890.9 ± 1.90.2 ± 0.12.6656.8 ± 7.11.0 ± 0.61.750.90
Embedded ImageNCGC0034587297.1 ± 0.90.3 ± 0.12.5158.0 ± 8.40.9 ± 0.31.810.70
Embedded ImageNCGC0034587393.1 ± 1.60.1 ± 0.072.9763.3 ± 8.90.9 ± 0.61.851.12
Embedded ImageDopamine1000.06 ± 0.023.221000.09 ± 0.033.050.18