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. Author manuscript; available in PMC: 2017 Dec 8.
Published in final edited form as: J Med Chem. 2016 Nov 16;59(23):10601–10618. doi: 10.1021/acs.jmedchem.6b01208

Table 3.

SFSR of combination compounds.a

Cmpd Structure β-arrestin cAMP
Emax (%) EC50 (nM) Emax (%) EC50 (nM)
46 graphic file with name nihms827411t23.jpg <20 N/C 43 98
47 graphic file with name nihms827411t24.jpg <20 N/C 33 72
48 graphic file with name nihms827411t25.jpg <20 N/C 33 62
49 graphic file with name nihms827411t26.jpg <20 N/C 32 8.3
50 graphic file with name nihms827411t27.jpg 33 6.4 41 1.0
51 graphic file with name nihms827411t28.jpg 36 16 48 2.8
52 graphic file with name nihms827411t29.jpg N/A N/A N/A N/A
53 graphic file with name nihms827411t30.jpg <20 N/C 37 5.5
54 graphic file with name nihms827411t31.jpg <20 N/C 47 50
55 graphic file with name nihms827411t32.jpg <20 N/C 31 28
56 graphic file with name nihms827411t33.jpg 29 6.5 49 1.1
57 graphic file with name nihms827411t34.jpg N/A N/A N/A N/A
58 graphic file with name nihms827411t35.jpg 24 460 56 88
a

EC50 and Emax values are the average of at least three independent experiments performed in triplicate. SEM: < ± 20%.

N/C. not calculated. N/A. no activity.