Results 191 to 200 of about 213,179 (224)

Molecular Dynamics Simulations and Structure-Based Rational Design Lead to Allosteric HCV NS5B Polymerase Thumb Pocket 2 Inhibitor with Picomolar Cellular Replicon Potency

Journal of Medicinal Chemistry, 2013
The design and preliminary SAR of a new series of 1H-quinazolin-4-one (QAZ) allosteric HCV NS5B thumb pocket 2 (TP-2) inhibitors was recently reported. To support optimization efforts, a molecular dynamics (MD) based modeling workflow was implemented, providing information on QAZ binding interactions with NS5B.
Oliver Hucke, René Coulombe, Pierre Bonneau, Mégan Bertrand-Laperle, Christian Brochu, James Gillard, Marc‐Andre Joly, Serge Landry, Olivier Lepage, Montse Llinàs‐Brunet, Marc Pesant, Martin Poirier, Maude Poirier, Ginette McKercher, Martin Marquis, George Kukolj, Pierre L. Beaulieu, Timothy A. Stammers   +17 more
semanticscholar   +4 more sources

ChemInform Abstract: From Rigid Cyclic Templates to Conformationally Stabilized Acyclic Scaffold. Part 1. The Discovery of CCR3 Antagonist Development Candidate BMS‐639623 with Picomolar Inhibition Potency Against Eosinophil Chemotaxis.

ChemInform, 2008
AbstractChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.
John V. Duncia, NULL AUTHOR_ID
semanticscholar   +3 more sources

ChemInform Abstract: Discovery of Oxazole‐Based PDE4 Inhibitors with Picomolar Potency.

ChemInform, 2012
AbstractA series of quinolyloxazoles with 4‐benzylcarboxamide and 5‐α‐aminoethyl groups, which show picomolar potency against PDE4, is discovered.
Rongze Kuang, NULL AUTHOR_ID
openalex   +2 more sources

HIV‐1 Protease Inhibitors with Picomolar Potency Against PI‐Resistant HIV‐1 by Modification of the P₁′ Substituent.

ChemInform, 2003
AbstractFor Abstract see ChemInform Abstract in Full Text.
Joseph Duffy, NULL AUTHOR_ID
openalex   +2 more sources

HIV Protease Inhibitors with Picomolar Potency Against PI‐Resistant HIV‐1 by Extension of the P₃ Substituent.

ChemInform, 2003
AbstractFor Abstract see ChemInform Abstract in Full Text.
Joseph Duffy, NULL AUTHOR_ID
openalex   +2 more sources

Synthesis and Monoamine Transporter Affinity of New 2β‐Carbomethoxy‐3β‐[4‐(substituted thiophenyl)]phenyltropanes: Discovery of a Selective SERT Antagonist with Picomolar Potency.

, 2005
Gilles Tamagnan, David Alagille, Xing Fu, Nora S. Kula, Ross J. Baldessarini, Robert B. Innis, Ronald M. Baldwin   +6 more
openalex   +2 more sources

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N-Terminus to Arginine Side-Chain Cyclization of Linear Peptidic Neuropeptide Y Y4 Receptor Ligands Results in Picomolar Binding Constants.

Journal of Medicinal Chemistry, 2021
The family of neuropeptide Y (NPY) receptors comprises four subtypes (Y1R, Y2R, Y4R, Y5R), which are addressed by at least three endogenous peptides, i.e., NPY, peptide YY, and pancreatic polypeptide (PP), the latter showing a preference for Y4R.
A. Konieczny, Marcus Conrad, Fabian J Ertl, Jakob Gleixner, Albert O. Gattor, Lukas Grätz, Maximilian F. Schmidt, Eduard Neu, Anselm H. C. Horn, David Wifling, Peter Gmeiner, T. Clark, Heinrich Sticht, M. Keller   +13 more
semanticscholar   +1 more source

Modeling relationship of pharmacokinetics, in vitro potency, and α4β7 receptor occupancy with intestinal cell trafficking in a gut-homing mouse model of IBD with MORF-057

Journal of Immunology, 2021
MORF-057 is an orally bioavailable, selective, and potent small molecule inhibitor of α4β7 integrin being developed for inflammatory bowel diseases (IBD) that is currently in phase 1 clinical testing.
Naresh S. Redhu, Ali Hussain, S. Srinivasan, Dooyoung Lee, Brianna Bannister, N. Blanco, Raegan Bonesteel, A. Camblin, L. Cappellucci, Rhianna Cohen, B. Harrison, K. Hahn, Kwangsoo Kim, M. Krumpoch, F. Lin, Kevin McManus, M. McShea, Jessica R. Pondish, P. Linde, A. Lugovskoy, M. Mangada, Terence Moy, Allison L Sang, Sarah St. Gelais, Andrew Sullivan, D. Troast, C. Zhong, Liangsu Wang, D. Cui, M. Bursavich, B. Lippa, B. Rogers, A. Ray, J. Wong   +33 more
semanticscholar   +1 more source

Potency-Enhanced Peptidomimetic VHL Ligands with Improved Oral Bioavailability.

Journal of Medicinal Chemistry
The von Hippel-Lindau (VHL) protein plays a pivotal role in regulating the hypoxic stress response and has been extensively studied and utilized in the targeted protein degradation field, particularly in the context of bivalent degraders.
Hao Wu, Jeremy Murray, Noriko Ishisoko, Alexandra Frommlet, Gauri Deshmukh, Antonio DiPasquale, Melinda M. Mulvihill, Donglu Zhang, John G Quinn, Robert A. Blake, Wayne J Fairbrother, Jakob Fuhrmann   +11 more
semanticscholar   +1 more source

From N-0385 to N-0920: Unveiling a Host-Directed Protease Inhibitor with Picomolar Antiviral Efficacy against Prevalent SARS-CoV-2 Variants.

Journal of Medicinal Chemistry
The worldwide spread of new SARS-CoV-2 variants emphasizes the need to diversify existing therapeutic strategies. TMPRSS2, a host protease crucial for SARS-CoV-2 entry, has garnered significant research attention as a potential target for therapeutic ...
Gabriel Lemieux, Jimena Pérez-Vargas, A. Désilets, Malihe Hassanzadeh, C. A. Thompson, Alice Gravel-Trudeau, Alexandre Joushomme, S. Ennis, Ivan Villanueva, Étienne Marouseau, Bryan J. Fraser, William Champagne, Matthieu Lepage, Masahiro Niikura, Cheryl H. Arrowsmith, François Jean, Richard Leduc, Pierre-Luc Boudreault   +17 more
semanticscholar   +1 more source