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Discovery of the Potent and Selective M1 PAM-Agonist N-[(3R,4S)-3-Hydroxytetrahydro-2H-pyran-4-yl]-5-methyl-4-[4-(1,3-thiazol-4-yl)benzyl]pyridine-2-carboxamide (PF-06767832): Evaluation of Efficacy and Cholinergic Side Effects JOURNAL ARTICLE published 14 July 2016 in Journal of Medicinal Chemistry |
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Directionally Modified Fluorophores for Super-Resolution Imaging of Target Enzymes: A Case Study with Carboxylesterases JOURNAL ARTICLE published 11 November 2021 in Journal of Medicinal Chemistry Research funded by National Natural Science Foundation of China (21703245) |
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Discovery of Novel, Potent Benzamide Inhibitors of 11β-Hydroxysteroid Dehydrogenase Type 1 (11β-HSD1) Exhibiting Oral Activity in an Enzyme Inhibition ex Vivo Model▽ JOURNAL ARTICLE published July 2008 in Journal of Medicinal Chemistry |
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Molecular Determinants of Topoisomerase I Poisoning by Lamellarins: Comparison with Camptothecin and Structure−Activity Relationships JOURNAL ARTICLE published 1 June 2005 in Journal of Medicinal Chemistry |
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Antimalarial Lead-Optimization Studies on a 2,6-Imidazopyridine Series within a Constrained Chemical Space To Circumvent Atypical Dose–Response Curves against Multidrug Resistant Parasite Strains JOURNAL ARTICLE published 25 October 2018 in Journal of Medicinal Chemistry Research funded by Medicines for Malaria Venture (MMV09/0002) |
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Small Molecule Disruptors of the Glucokinase–Glucokinase Regulatory Protein Interaction: 3. Structure–Activity Relationships within the Aryl Carbinol Region of the N-Arylsulfonamido-N′-arylpiperazine Series JOURNAL ARTICLE published 10 April 2014 in Journal of Medicinal Chemistry |
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Development of Dual Inhibitors Targeting Epidermal Growth Factor Receptor in Cancer Therapy JOURNAL ARTICLE published 14 April 2022 in Journal of Medicinal Chemistry Research funded by Ministry of Science and Technology of the People's Republic of China (2018ZX09201018-021) | National Natural Science Foundation of China (81874290,81903502,81922064,82073318) | National Clinical Research Center for Geriatrics, Sichuan University (Z20201004) | Sichuan Science and Technology Program (2019YFS0003) |
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Discovery of Novel Class I Histone Deacetylase Inhibitors with Promising in Vitro and in Vivo Antitumor Activities JOURNAL ARTICLE published 8 October 2015 in Journal of Medicinal Chemistry Research funded by National Natural Science Foundation of China (21172220,21472191) |
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Structure-Based Design of Potent HIV-1 Protease Inhibitors with Modified P1-Biphenyl Ligands: Synthesis, Biological Evaluation, and Enzyme–Inhibitor X-ray Structural Studies JOURNAL ARTICLE published 9 July 2015 in Journal of Medicinal Chemistry Research funded by National Institute of General Medical Sciences (GM62920) |
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Lipopeptides containing 2-(palmitoylamino)-6,7-bis(palmitoyloxy)heptanoic acid: synthesis, stereospecific stimulation of B-lymphocytes and macrophages and adjuvanticity in vivo and in vitro JOURNAL ARTICLE published July 1991 in Journal of Medicinal Chemistry |
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In Vitro and In Vivo Evaluation of ABCG2 (BCRP) Inhibitors Derived from Ko143 JOURNAL ARTICLE published 25 May 2023 in Journal of Medicinal Chemistry Research funded by Schweizerischer Nationalfonds zur F??rderung der Wissenschaftlichen Forschung (NCCR TransCure - Multidrug transporter ABCG2) |
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Novel Allosteric Inhibitor-Derived AKT Proteolysis Targeting Chimeras (PROTACs) Enable Potent and Selective AKT Degradation in KRAS/BRAF Mutant Cells JOURNAL ARTICLE published 27 October 2022 in Journal of Medicinal Chemistry Research funded by National Cancer Institute (P30 CA196521,R35CA220491) |
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Investigations on the 4-Quinolone-3-carboxylic Acid Motif. 1. Synthesis and Structure−Activity Relationship of a Class of Human Immunodeficiency Virus type 1 Integrase Inhibitors JOURNAL ARTICLE published 1 August 2008 in Journal of Medicinal Chemistry |
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G-Quadruplex DNA as a Target in Pathogenic Bacteria: Efficacy of an Extended Naphthalene Diimide Ligand and Its Mode of Action JOURNAL ARTICLE published 24 March 2022 in Journal of Medicinal Chemistry Research funded by Nederlandse Organisatie voor Wetenschappelijk Onderzoek (16433,NWA.1228.191.006) |
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Discovery of Novel 3-Piperidinyl Pyridine Derivatives as Highly Potent and Selective Cholesterol 24-Hydroxylase (CH24H) Inhibitors JOURNAL ARTICLE published 24 February 2022 in Journal of Medicinal Chemistry |
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Discovery of a PDZ Domain Inhibitor Targeting the Syndecan/Syntenin Protein–Protein Interaction: A Semi-Automated “Hit Identification-to-Optimization” Approach JOURNAL ARTICLE published 13 April 2023 in Journal of Medicinal Chemistry Research funded by Agence Nationale de la Recherche (ANR-11-IDEX-0001-02,ANR-18-CE13-0017) | Institut National Du Cancer (2013-105) |
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Inhibition of UDP-N-Acetylglucosamine Import into Golgi Membranes by Nucleoside Monophosphates JOURNAL ARTICLE published 1 January 1996 in Journal of Medicinal Chemistry |
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Derivation and Validation of Toxicophores for Mutagenicity Prediction JOURNAL ARTICLE published 1 January 2005 in Journal of Medicinal Chemistry |
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Nanomolar Inhibitors of the Peptidyl Prolyl Cis/Trans Isomerase Pin1 from Combinatorial Peptide Libraries JOURNAL ARTICLE published 1 April 2006 in Journal of Medicinal Chemistry |
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Identification of 2-{2-[2-(5-Bromo-2- methoxyphenyl)-ethyl]-3-fluorophenyl}-4,5-dihydro-1H-imidazole (ML00253764), a Small Molecule Melanocortin 4 Receptor Antagonist That Effectively Reduces Tumor-Induced Weight Loss in a Mouse Model JOURNAL ARTICLE published 1 March 2004 in Journal of Medicinal Chemistry |