PDB IDa | Ligand | Efficacy | Fusion Partnerb | Binding Partner | Resolution (Å) | References |
---|---|---|---|---|---|---|
2RH1 | Carazolol | Inverse agonist | T4 lysozyme (T4L) in ICL3 | None | 2.40 | Cherezov et al., 2007; Rosenbaum et al., 2007 |
2R4R | Carazolol | Inverse agonist | None | Fab5 | 3.40 | Rasmussen et al., 2007 |
2R4S | Carazolol | Inverse agonist | None | Fab5 | 3.40 | Rasmussen et al., 2007 |
3D4S | Timolol | Inverse agonist | T4L in ICL3 | None | 2.80 | Hanson et al., 2008 |
3KJ6 | Carazolol | Inverse agonist | None | Fab5 | 3.40 | Bokoch et al., 2010 |
3NY8 | ICI 118551 | Inverse agonist | T4L in ICL3 | None | 2.84 | Wacker et al., 2010 |
3NY9 | Compound 2ac | Inverse agonist | T4L in ICL3 | None | 2.84 | Wacker et al., 2010 |
3NYA | Alprenolol | Antagonist | T4L in ICL3 | None | 3.16 | Wacker et al., 2010 |
4GBR | Carazolol | Inverse agonist | N-terminal T4L | None | 3.99 | Zou et al., 2012 |
5D5A | Carazolol | Inverse agonist | T4L in ICL3 | None | 2.48 | Huang et al., 2016a |
5D5B | Carazolol | Inverse agonist | T4L in ICL3 | None | 3.80 | Huang et al., 2016a |
5JQH | Carazolol | Inverse agonist | N-terminal T4L | Nanobody Nb60 | 3.20 | Staus et al., 2016 |
5D5B | Carazolol | Inverse agonist | T4L in ICL3 | None | 3.20 | Ma et al., 2017 |
5X7D | Carazolol and intracellular antagonist Cmpd-15PA | Inverse agonist and allosteric antagonist | T4L in ICL3 | None | 2.70 | Liu et al., 2017 |
3PDS | FAUC50 | Covalent agonist | T4L in ICL3 | None | 3.50 | Rosenbaum et al., 2011 |
3P0G | BI-167107 | Full agonist | None | Nanobody Nb80 | 3.50 | Rasmussen et al., 2011a |
3SN6 | BI-167107 | Full agonist | N-terminal T4L | Gs heterotrimer | 3.20 | Rasmussen et al., 2011b |
4LDE | BI-167107 | Full agonist | N-terminal T4L | Nanobody Nb6B9 | 2.79 | Ring et al., 2013 |
4LDL | Hydroxybenzyl isoproterenol | Full agonist | N-terminal T4L | Nanobody Nb6B9 | 3.10 | Ring et al., 2013 |
4LDO | Adrenaline (epinephrine) | Full agonist | N-terminal T4L | Nanobody Nb6B9 | 3.20 | Ring et al., 2013 |
4QKX | Compound 2bc | Covalent agonist | N-terminal T4L | Nanobody Nb6B9 | 3.30 | Weichert et al., 2014 |
6MXT | Salmeterol | Partial agonist | N-terminal T4L | Nanobody Nb71 | 2.96 | Masureel et al., 2018 |
↵a PDB, https://www.rcsb.org/.
↵b Inserting a small protein into GPCRs either at the ICL3 or at the N-terminal ends has been widely used to facilitate crystallization.
↵c Compound 2a and compound 2b are unrelated. They were both named “compound 2” in the literature. Here we use 2a and 2b to avoid confusion.
ICL3, intracellular loop 3.