Structure–activity study of N-((trans)-4-(2-(7-cyano-3,4-dihydroisoquinolin-2(1H)-yl)ethyl)cyclohexyl)-1H-indole-2-carboxamide (SB269652), a bitopic ligand that acts as a negative allosteric modulator of the dopamine D2 receptor

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Structure–activity study of N-((trans)-4-(2-(7-cyano-3,4-dihydroisoquinolin-2(1H)-yl)ethyl)cyclohexyl)-1H-indole-2-carboxamide (SB269652), a bitopic ligand that acts as a negative allosteric modulator of the dopamine D2 receptor

We recently demonstrated that SB269652 (1) engages one protomer of a dopamine D2 receptor (D2R) dimer in a bitopic mode to allosterically inhibit the binding of dopamine at the other protomer. Herein, we investigate structural deter- minants for allostery, focusing on modifications to three moieties...

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Bibliographic Details
Main Authors:	Shonberg, Jeremy, Draper-Joyce, Christopher, Mistry, Shailesh N., Christopoulos, Arthur, Scammells, Peter J., Lane, J. Robert, Capuano, Ben
Format:	Article
Published:	American Chemical Society 2015
Online Access:	https://eprints.nottingham.ac.uk/30314/

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