Table 2Structure and SAR for Analogues 13

Image ml173fu15.jpg
CIDR2R3Rat M4 EC50 (μM)aRat M4 ACh fold-shiftb
45142477
Image ml173fu4.jpg
Image ml173fu16.jpg
2.587x
45142478
Image ml173fu5.jpg
Image ml173fu17.jpg
2.7514x
45142479
Image ml173fu6.jpg
Image ml173fu18.jpg
7.4240x
45142480
Image ml173fu6.jpg
Image ml173fu19.jpg
6.2567x
45142489
Image ml173fu6.jpg
Image ml173fu20.jpg
5.8151x
45142482
Image ml173fu6.jpg
Image ml173fu21.jpg
7.1536x
45142483
Image ml173fu6.jpg
Image ml173fu22.jpg
8.7362x
45142484
Image ml173fu14.jpg
Image ml173fu23.jpg
5.4028x
45142485
Image ml173fu14.jpg
Image ml173fu24.jpg
> 1041x
45142486
Image ml173fu12.jpg
Image ml173fu23.jpg
2.4444x
45142487
Image ml173fu12.jpg
Image ml173fu24.jpg
3.7864x
a

Data represent the mean vales from at least 3 experiments with similar results.

b

Leftward shift of an ACh CRC in the presence of 30 μM compound relative to ACh CRC control.

From: Discovery of a Highly Selective in vitro and in vivo M4 Positive Allosteric Modulator (PAM) Series with Greatly Improved Human Receptor Activity

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Probe Reports from the NIH Molecular Libraries Program [Internet].
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