Table S3.

Compound 15-mediated allosteric inhibition of β₂AR signals stimulated with different agonists

Agonists	G-protein cAMP		β-Arrestin recruitment		125I-CYP competition binding
	Inhibition Emax, %	EC50 shift, fold	Inhibition Emax, %	EC50 shift, fold	EC50 shift, fold
Isoproterenol	31.5 ± 2.5***	7.1 ± 1.2***	61.7 ± 2.0***	7.4 ± 1.2***	9.1 ± 1.1***
Epinephrine	36.5 ± 5.1***	7.4 ± 1.3***	71.8 ± 2.4***	5.9 ± 1.2***	5.8 ± 1.1***
Fenoterol	55.7 ± 3.4***	2.6 ± 1.3***	81.2 ± 3.2***	2.1 ± 1.4***	1.9 ± 1.1***
Clenbuterol	78.1 ± 6.9***	No shift	88.4 ± 21.5***	No shift	1.1 ± 1.1***

The values of 15-induced maximal “Inhibition E_max, %” and “EC₅₀ shift, fold” were obtained from the data presented in Fig. 2A (for competition binding with isoproterenol), Fig. 3 (for functional data with isoproterenol), and Fig. S5 (for all of the data with the other agonists). Each value represents mean ± SEM. Statistical analyses were performed as described in SI Materials and Methods. ***P < 0.001 compared with the value from the vehicle (DMSO)-treated control sample.