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. 2020 Jan;72(1):1–49. doi: 10.1124/pr.118.016899

TABLE 3.

Structures of human M1, M2, and M4 receptors, and rat M3 receptor

Receptor PDB ID Ligand Efficacy Fusion Partner Resolution (Å) References
M1R 5CXV Tiotropium Inverse agonist T4 lysozyme (T4L) in ICL3 2.70 Thal et al., 2016
M2R 3UON QNB Inverse agonist T4L in ICL3 3.00 Haga et al., 2012
M2R 4MQS Iperoxo Full agonist None 3.50 Kruse et al., 2013a
M2R 4MQT Iperoxo, LY2119620 Full agonist, PAM None 3.70 Kruse et al., 2013a
M2R 5ZK8 NMS Inverse agonist Cytochrome b562RIL (BRIL) in ICL3 3.00 Suno et al., 2018
M2R (S110R) 5ZKC NMS Inverse agonist BRIL in ICL3 2.30 Suno et al., 2018
M2R (S110R) 5ZKB AF-DX 384 Antagonist BRIL in ICL3 2.95 Suno et al., 2018
M2R (S110R) 5ZK3 QNB Inverse agonist BRIL in ICL3 2.60 Suno et al., 2018
M2R (S110R) 5YC8 NMS, Hg Inverse agonist, cation BRIL in ICL3 2.50 Suno et al., 2018
M3R 4DAJ Tiotropium Inverse agonist T4L in ICL3 3.40 Kruse et al., 2012
M3R 4U14 Tiotropium Inverse agonist Disulfide stabilized T4L in ICL3 3.57 Thorsen et al., 2014
M3R 4U15 Tiotropium Inverse agonist Minimal T4L (mT4L) in ICL3 2.80 Thorsen et al., 2014
M3R 4U16 NMS Inverse agonist mT4L in ICL3 3.70 Thorsen et al., 2014
M3R 5ZHP Compound 6o (BS46) Antagonist mT4L in ICL3 3.10 Liu et al., 2018
M4R 5DSG Tiotropium Inverse agonist mT4L in ICL3 2.60 Thal et al., 2016