Extended Data Table 5 Relative efficacy of D1R mediated by \({{\bf{D1R\mbox{--}GEM}}}_{{\bf{BAM}}}^{{\bf{TM3}}{\boldsymbol{/}}{\bf{4}}{\boldsymbol{/}}{\bf{5}}}\) and \({{\bf{GEM}}}_{{\bf{ago\mbox{--}PAM}}}^{{\bf{TM5}}{\boldsymbol{/}}{\bf{6}}{\boldsymbol{/}}{\bf{7}}}\)

From: De novo design of GPCR exoframe modulators

  1. aGloSensor results of cAMP accumulation and BRET assay of β-arrestin 2 recruitment for D1R (WT, mutant and GEM binding) were normalized to the maximal response of WT D1R. Data are presented as means ± SEM from at least three independent experiments performed in technical triplicate. NSP > 0.05, *P < 0.05, **P < 0.01, ***P < 0.001 and ****P < 0.0001 by one-way ANOVA followed by Dunnett’s post-test compared with WT D1R (P = 0.9987, = 0.5961, = 0.0002 from top to bottom in the cAMP accumulation assay; P < 0.0001, = 0.0669, <0.0001 from top to bottom in the β-arrestin 2 recruitment assay).
  2. bThe relative response is defined as the activity of D1R stimulated by 10 μM dopamine or the basal activity of D1R with GEM.
Back to article page