Discovery of a highly potent, functionally-selective muscarinic M1 agonist, WAY-132983 using rational drug design and receptor modelling.

A L Sabb, G M Husbands, J Tokolics, R P Stein, R P Tasse, C A Boast, J A Moyer, M Abou-Gharbia

Wyeth-Ayerst Research, Princeton, NJ 08543-8000, USA.

Bioorganic & medicinal chemistry letters 1999 Jul 19

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Rational drug design utilizing a receptor homology model of the human muscarinic M1 receptor led to the discovery of the highly potent (Ki = 2 nM), efficacious, and in vivo functionally-selective M1 agonist, WAY-132983.

Citation

A L Sabb, G M Husbands, J Tokolics, R P Stein, R P Tasse, C A Boast, J A Moyer, M Abou-Gharbia. Discovery of a highly potent, functionally-selective muscarinic M1 agonist, WAY-132983 using rational drug design and receptor modelling. Bioorganic & medicinal chemistry letters. 1999 Jul 19;9(14):1895-900