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. Author manuscript; available in PMC: 2018 Jun 1.
Published in final edited form as: Bioorg Med Chem Lett. 2017 Apr 4;27(11):2479–2483. doi: 10.1016/j.bmcl.2017.04.009

Table 2.

Structures and mAChR activities of analogs 17a–h.

graphic file with name nihms869431u4.jpg
Compound R hM4 IC50 (μM)a [% ACh Min ±SEM] hM4 pIC50 (±SEM)a
17a graphic file with name nihms869431t1.jpg >10 >5
17b graphic file with name nihms869431t2.jpg 0.58 [5.5±2.9] 6.25±0.09
17c graphic file with name nihms869431t3.jpg 2.47 [11.8±1.5] 5.62±0.08
17d graphic file with name nihms869431t4.jpg 0.41 [5.1±0.6] 6.39±0.05
17e graphic file with name nihms869431t5.jpg 0.34 [18.4±2.3] 6.49±0.06
17f graphic file with name nihms869431t6.jpg 1.04 [6.0±0.5] 6.00±0.05
17g graphic file with name nihms869431t7.jpg >10 >5
17h graphic file with name nihms869431t8.jpg >10 >5
a

Mean of three independent determinations in a calcium mobilization assay using recombinant hM4-expressing Chinese hamster ovary cells co-transfected with chimeric Gqi5 in the presence of an ACh EC80.