Extended Data Table 2 Influence of gradient transfection of \({{\bf{GEM}}}_{{\bf{ago\mbox{--}PAM}}}^{{\bf{TM5}}{\boldsymbol{/}}{\bf{6}}{\boldsymbol{/}}{\bf{7}}}\) on cAMP accumulation and β-arrestin 2 recruitment mediated by D1R

From: De novo design of GPCR exoframe modulators

  1. aGloSensor results of cAMP accumulation for D1R (WT and GEM binding) and BRET assay of β-arrestin 2 recruitment were normalized to the maximal response of WT D1R without GEM. Data are presented as means ± SEM from at least two 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 > 0.9999, > 0.9999, > 0.9999, = 0.8548, = 0.1578 from top to bottom for pEC50 in the cAMP accumulation assay; P > 0.9999, > 0.9999, = 0.9327, <0.0001, <0.0001 from top to bottom for pEC50 in the in the β-arrestin 2 recruitment assay; P = 0.2517, = 0.0010, <0.0001, <0.0001, <0.0001 from top to bottom for relative response in the cAMP accumulation assay; P = 0.8677, = 0.0874, = 0.0089, = 0.0141, = 0.0212 from top to bottom for relative response in the in the β-arrestin 2 recruitment assay).
  2. bThe relative response is defined as the basal activity of D1R with GEM, normalized by the activity of D1R stimulated by 1 μM dopamine for GloSensor assay and 100 μM dopamine for BRET assay.
  3. cThe Surface expression ratio is defined as the proportion of D1R or GEM present on the cell surface relative to its total cellular amount.
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