TABLE 2.

Structures of human β₂AR bound to various ligands

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

^aPDB, https://www.rcsb.org/.

^bInserting a small protein into GPCRs either at the ICL3 or at the N-terminal ends has been widely used to facilitate crystallization.

^cCompound 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.