Mapping the efficiency and physicochemical trajectories of successful optimizations
The practices and tactics employed in successful optimizations are examined, judged from
the trajectories of ligand efficiency and property evolution. A wide range of targets is …
the trajectories of ligand efficiency and property evolution. A wide range of targets is …
Small molecule allosteric modulators of G-protein-coupled receptors: drug–target interactions
S Lu, J Zhang - Journal of medicinal chemistry, 2018 - ACS Publications
G-protein-coupled receptors (GPCRs) are the largest class of signaling receptors that are
most frequently targeted by therapeutic drugs. Allosteric modulators bound to GPCRs at …
most frequently targeted by therapeutic drugs. Allosteric modulators bound to GPCRs at …
Novel substituted 4-(Arylethynyl)-Pyrrolo [2, 3-d] pyrimidines negative allosteric modulators (NAMs) of the metabotropic glutamate receptor subtype 5 (mGlu5) Treat …
Y Du, F Gao, H Sun, C Wu, G Zhu, M Zhu - European Journal of Medicinal …, 2023 - Elsevier
In view of the fact that the G-protein-coupled receptors (GPCRs) sit at the top of the signaling
pathways triggering a diverse range of signaling cascades towards a cellular event, GPCRs …
pathways triggering a diverse range of signaling cascades towards a cellular event, GPCRs …
Pharmacology, Signaling and Therapeutic Potential of Metabotropic Glutamate Receptor 5 Negative Allosteric Modulators
JA Kos, M Langiu, SD Hellyer… - ACS Pharmacology & …, 2024 - ACS Publications
Metabotropic glutamate receptors are a family of eight class CG protein-coupled receptors
regulating higher order brain functions including cognition and motion. Metabotropic …
regulating higher order brain functions including cognition and motion. Metabotropic …
Synthesis, crystal structure, insecticidal activities, molecular docking and QSAR studies of some new phospho guanidines and phospho pyrazines as cholinesterase …
K Gholivand, F Mohammadpanah, M Pooyan… - Pesticide biochemistry …, 2019 - Elsevier
Novel phospho guanidine and phospho pyrazine derivatives were synthesized and
characterized by 31 P, 13 C, 1 HNMR and IR spectroscopy to obtain novel and human-safe …
characterized by 31 P, 13 C, 1 HNMR and IR spectroscopy to obtain novel and human-safe …
A “Neat” Synthesis of Substituted 2-Hydroxy-pyrido [1, 2-a] pyrimidin-4-ones
G Gaube, J Mutter, DC Leitch - Canadian Journal of Chemistry, 2024 - cdnsciencepub.com
We report the synthesis of a series of substituted 2-hydroxy-pyrido [1, 2-a] pyrimidin-4-ones
through a condensation of 2-aminopyridines and diethyl malonate. This method is …
through a condensation of 2-aminopyridines and diethyl malonate. This method is …
2-氨基吡啶在构建五元, 六元氮稠环合成中的应用
陈淇， 陈思鸿， 吴汉清， 曾晓晴， 陈伟清， 孙国星… - 有机化学, 2021 - sioc-journal.cn
氨基吡啶是一类重要的合成子, 具有独特的双亲核结构, 可与酮, 醛, 酸, 多官能团酯类以及卤代
芳烃等化合物反应, 以构建五元, 六元含氮稠杂环. 近年来, 基于2-氨基吡啶的成环反应倍受关注 …
芳烃等化合物反应, 以构建五元, 六元含氮稠杂环. 近年来, 基于2-氨基吡啶的成环反应倍受关注 …
Application of 2-aminopyridines in the synthesis of five-and six-membered azaheterocycles
C Qi, C Sihong, W Hanqing, Z Xiaoqing… - Chinese Journal of …, 2021 - sioc-journal.cn
Aminopyridine is a significant synthetic synthon, with unique dual nucleophilic structure. It
can react with ketones, aldehydes, acids, multifunctional esters, halogenated aromatics and …
can react with ketones, aldehydes, acids, multifunctional esters, halogenated aromatics and …
[PDF][PDF] Development of Clickable, Covalent Ligands for the Adenosine A1 and Metabotropic Glutamate Subtype 5 Receptors
DCJ Weng - 2021 - ourarchive.otago.ac.nz
Abstract The Adenosine A1 receptor (A1AR) and metabotropic glutamate subtype 5
(mGluR5) receptor are class AG protein-coupled receptors (GPCRs) which have been …
(mGluR5) receptor are class AG protein-coupled receptors (GPCRs) which have been …