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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 2.

SFSR of the LHS Phenylpiperazine Moiety.a

graphic file with name nihms827411t12.jpg
Compound LHS Group β-arrestin cAMP
Emax (%) EC50 (nM) Emax (%) EC50 (nM)
1 graphic file with name nihms827411t13.jpg 23 13 50 15
30 graphic file with name nihms827411t14.jpg 31 49 66 76
31 graphic file with name nihms827411t15.jpg <20 N/C 22 1.9
32 graphic file with name nihms827411t16.jpg 25 8.5 61 68
34 graphic file with name nihms827411t17.jpg N/A N/A N/A N/A
36 graphic file with name nihms827411t18.jpg <20 N/C 25 15
39 graphic file with name nihms827411t19.jpg <20 N/C 29 5.2
40 graphic file with name nihms827411t20.jpg 35 3.6 50 0.64
44 graphic file with name nihms827411t21.jpg N/A N/A N/A N/A
45 graphic file with name nihms827411t22.jpg 88 0.36 90 0.27
a

EC50 and Emax values are the average of at least 3 independent experiments performed in triplicate. SEM: < ± 20%.

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