Fig. 2. Features of the Ro5256390-bound orthosteric binding pocket of hTA1.
A The orthosteric binding pocket (OBP) of hTA1 and key residues are shown from three angles, with residues chosen for mutagenic study highlighted in cyan. Grey dashed lines denote an ionic interaction between Ro5256390 and the receptor. Light blue, hTA1; Ro5256390, magenta. B Effects of distinct mutations of the potency and efficacy of hTA1 agonists. Data are shown as differences between mutant and wild type receptor with potencies determined as pEC50s and efficacies measured as Emax. Data represent mean of two independent experiments (n = 2). ND denotes that no reliable pEC50/ΔpEC50 values could be obtained due to low compound activity. See Supplementary Table 1 for fitted parameter values.