Table S2.

Compound 15-mediated allosteric inhibition of β-arrestin recruitment and endocytosis by different receptors

Receptors	β-Arrestin recruitment		β-Arrestin endocytosis
	Inhibition Emax, %	EC50 shift, fold	Inhibition Emax, %	EC50 shift, fold
β2AR	32.6 ± 4.8***	8.0 ± 1.4***
β2V2R	30.6 ± 4.7***	7.1 ± 1.4***	30.1 ± 4.3***	10.5 ± 1.3***
β1AR	30.6 ± 8.6***	1.2 ± 1.8***
V2R	13.9 ± 4.0***	3.4 ± 1.3***	11.0 ± 3.8***	3.9 ± 1.2***
VIPR	18.4 ± 3.6***	1.1 ± 1.2***
AT1R	10.9 ± 10.2***	0.8 ± 1.9***	10.5 ± 3.4***	0.8 ± 1.2

The values of 15-induced maximal “Inhibition E_max, %” and “EC₅₀ shift, fold” were obtained from the data presented in Fig. 4 and Fig. S4. Each value represents mean ± SEM. Statistical analyses were performed as described in SI Materials and Methods. ***P < 0.001 compared with the control value obtained in the presence of the vehicle (DMSO).