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. Author manuscript; available in PMC: 2018 Mar 15.
Published in final edited form as: ACS Chem Neurosci. 2016 Nov 23;8(3):486–500. doi: 10.1021/acschemneuro.6b00221

Table 2.

Functional Profiles of SK609 and Its Analogues for G-Protein-Dependent and β-Arrestin-Dependent Signaling Mechanisms at D3Ra

compound [35S]GTPγS binding
ERK1/2 phosphorylation
β-arrestin recruitment
EC50 Emax EC50 Emax EC50 Emax
DA 11.3 ± 2.7 nM 100 5.2 ± 1.0 nM 100 ND ND
PD128907 1.2 ± 0.18 nM 96.1 ± 2.1 7.1 ± 0.5 nM 100 5.5 ± 0.18 nM 100
SK609 1.1 ± 0.2 μM 74.3 ± 2.3 50.2 ± 5.9 nM 81 ± 4.5 14.4 ± 2.7 μM 57.3 ± 2.5
SK213 1.3 ± 0.3 μM 98.4 ± 7.9 39.2 ± 4.2 nM 95 ± 5.5 6.8 ± 0.5 μM 66.1 ± 6.5
SK232 3.5 ± 0.9 μM 95.6 ± 8.1 859 ± 232 nM 106 ± 6.5 ND ND
SK608 33.5 ± 8.4 nM 81.1 ± 5.5 84.6 ± 21.4 nM 76 ± 1.4 ND ND
a

For ERK1/2 phosphorylation, CHO-D3R cells were treated with DA or test compounds for 5 min at 37 °C. ND, not determined.