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. Author manuscript; available in PMC: 2020 Sep 12.
Published in final edited form as: J Med Chem. 2019 Aug 20;62(17):8357–8363. doi: 10.1021/acs.jmedchem.9b00340

Table 5.

Structures and NTR1 activities of analogs 23

graphic file with name nihms-1046925-t0040.jpg
Cpd
#		 R1 EC50, μMa Emax (%)b
23a 5-F 0.59 ± 0.08 (8) 95
23b 8-F 0.16 ± 0.04 (8) 100
23c 5-Me 1.26 ± 0.36 (8) 93
23d 7-Me 0.56 ± 0.11 88
23e 8-Me 0.16 ± 0.04 (8) 87
23f 5-Cl 0.50 ± 0.16 91
23g 7-Cl 0.60 ± 0.24 (23) 98
23h 8-Cl 0.22 ± 0.14 95
a

β-Arrestin2-GFP NTR1 potency measured relative to the EC100 (100 nM) of the NT(8–13) peptide control average ± SEM (n=4 unless otherwise noted);

b

Emax was calculated as the % of the response obtained with NT(8–13) peptide. None of the compounds from this series showed activity in the NTR2 (>80 μM) counterscreen.