An article A Thieno[2,3-d]pyrimidine Scaffold Is a Novel Negative Allosteric Modulator of the Dopamine D-2 Receptor WOS:000455561400011 published article about LIGAND DISCOVERY; D-3; PHARMACOLOGY; SELECTIVITY; INHIBITORS; SB269652; D2 in [Fyfe, Tim J.; Scammells, Peter J.; Capuano, Ben] Monash Univ, Med Chem, Monash Inst Pharmaceut Sci, Parkville, Vic 3052, Australia; [Fyfe, Tim J.; Lim, Herman D.; Lane, J. Robert] Monash Univ, Monash Inst Pharmaceut Sci, Drug Discovery Biol, Parkville, Vic 3052, Australia; [Fyfe, Tim J.; Kellam, Barrie; Mistry, Shailesh N.] Univ Nottingham, Ctr Biomol Sci, Sch Pharm, Nottingham NG7 2RD, England; [Zarzycka, Barbara; Katrich, Vsevolod] Univ Southern Calif, Bridge Inst, Dept Biol Sci, Los Angeles, CA 90089 USA; [Katrich, Vsevolod] Univ Southern Calif, Bridge Inst, Dept Chem, Los Angeles, CA 90089 USA in 2019, Cited 41. The Name is 3-(Trifluoromethyl)phenol. Through research, I have a further understanding and discovery of 98-17-9. Name: 3-(Trifluoromethyl)phenol
Recently, a novel negative allosteric modulator (NAM) of the D-2-like dopamine receptors 1 was identified through virtual ligand screening. This ligand comprises a thieno[2,3-d]pyrimidine scaffold that does not feature in known dopaminergic ligands. Herein, we provide pharmacological validation of an allosteric mode of action for 1, revealing that it is a NAM of dopamine efficacy and identify the structural determinants of this allostery. We find that key structural moieties are important for functional affinity and negative cooperativity, while functionalization of the thienopyrimidine at the 5- and 6-positions results in analogues with divergent cooperativity profiles. Successive compound iterations have yielded analogues exhibiting a 10-fold improvement in functional affinity, as well as enhanced negative cooperativity with dopamine affinity and efficacy. Furthermore, our study reveals a fragment-like core that maintains low mu M affinity and robust negative cooperativity with markedly improved ligand efficiency.
About 3-(Trifluoromethyl)phenol, If you have any questions, you can contact Fyfe, TJ; Zarzycka, B; Lim, HD; Kellam, B; Mistry, SN; Katrich, V; Scammells, PJ; Lane, JR; Capuano, B or concate me.. Name: 3-(Trifluoromethyl)phenol
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,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles