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. Author manuscript; available in PMC: 2018 Mar 15.
Published in final edited form as: Bioorg Med Chem Lett. 2017 Feb 13;27(6):1356–1359. doi: 10.1016/j.bmcl.2017.02.020

Table 1.

Structures and activities for hM5 NAM 1 and analogs 4.

graphic file with name nihms854579t1.jpg
Cpd NR1R2 hM5
IC50 (μM)a
[% ACh Min ± SEM]		 hM5 pIC50 (±SEM)a
1 ML375 “Cl” 1.11      
[2.3 ± 0.3]		 5.98±0.04
4a graphic file with name nihms854579t2.jpg 6.04     
[10.5±2.8]		 5.22±0.04
4b graphic file with name nihms854579t3.jpg 4.28      
[13.6 ± 1.0]		 5.37 ± 0.04
4c graphic file with name nihms854579t4.jpg 6.36       
[6.9 ± 1.7]		 5.20 ± 0.03
4d graphic file with name nihms854579t5.jpg 1.46       
[3.1 ± 0.2]		 5.84 ± 0.04
4e graphic file with name nihms854579t6.jpg 5.70      
[2.6 ± 0.1]		 5.84 ± 0.04
4f graphic file with name nihms854579t7.jpg 1.82         
[3.1 ± 0.2]		 5.74 ± 0.04
4g graphic file with name nihms854579t8.jpg 3.42      
[3.2 ± 0.2]		 5.47 ± 0.03
4h graphic file with name nihms854579t9.jpg 4.01      
[3.6 ± 0.2]		 5.40 ± 0.4
4i graphic file with name nihms854579t10.jpg 7.29      
[26.3 ± 6.2]		 5.14 ± 0.05
4k graphic file with name nihms854579t11.jpg 8.21      
[20.1 ± 7.7]		 5.11 ± 0.10
4l graphic file with name nihms854579t12.jpg 4.55         
[27.0 ± 7.7]		 5.35 ± 0.05
4m graphic file with name nihms854579t13.jpg 1.32       
[2.6 ± 0.9]		 5.89 ± 0.08
4n graphic file with name nihms854579t14.jpg 6.92      
[25.5 ± 9.3]		 5.17 ± 0.08
4o graphic file with name nihms854579t15.jpg 3.09      
[3.3 ± 0.3]		 5.52 ± 0.05
4p graphic file with name nihms854579t16.jpg >10       
[26.2 ± 3.5]		 >5
4q graphic file with name nihms854579t17.jpg 3.50       
[6.0 ± 0.3]		 5.46 ± 0.03
4r graphic file with name nihms854579t18.jpg 9.49       
[7.5 ± 2.4]		 5.06 ± 0.14
a

Mean of three independent determinations performed in triplicate via an intracellular calcium mobilization assay with recombinant hM5 cells in the presence of an ACh EC80.