JNJ-67569762, A 2-Aminotetrahydropyridine-Based Selective BACE1 Inhibitor Targeting the S3 Pocket: From Discovery to Clinical Candidate.
Sign Up to like & getrecommendations! Published in 2021 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.1c00935
Abstract: The discovery of a novel 2-aminotetrahydropyridine class of BACE1 inhibitors is described. Their pKa and lipophilicity were modulated by a pending sulfonyl group, while good permeability and brain penetration were achieved via intramolecular hydrogen bonding.… read more here.
Keywords: bace1 inhibitor; selective bace1; jnj 67569762; discovery ... See more keywords
Discovery of Clinical Candidate CHF-6366: A Novel Super-soft Dual Pharmacology Muscarinic Antagonist and β2 Agonist (MABA) for the Inhaled Treatment of Respiratory Diseases.
Sign Up to like & getrecommendations! Published in 2022 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.2c00609
Abstract: The development of molecules embedding two distinct pharmacophores acting as muscarinic antagonists and β2 agonists (MABAs) promises to be an excellent opportunity to reduce formulation issues and boost efficacy through cross-talk and allosteric interactions. Herein,… read more here.
Keywords: clinical candidate; maba; pharmacology; chf 6366 ... See more keywords
Discovery of Clinical Candidate AZD0095, a Selective Inhibitor of Monocarboxylate Transporter 4 (MCT4) for Oncology.
Sign Up to like & getrecommendations! Published in 2022 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.2c01342
Abstract: Due to increased reliance on glycolysis, which produces lactate, monocarboxylate transporters (MCTs) are often upregulated in cancer. MCT4 is associated with the export of lactic acid from cancer cells under hypoxia, so inhibition of MCT4… read more here.
Keywords: oncology; monocarboxylate; clinical candidate; candidate azd0095 ... See more keywords
HSF1 Pathway Inhibitor Clinical Candidate (CCT361814/NXP800) Developed from a Phenotypic Screen as a Potential Treatment for Refractory Ovarian Cancer and Other Malignancies
Sign Up to like & getrecommendations! Published in 2023 at "Journal of Medicinal Chemistry"
DOI: 10.1021/acs.jmedchem.3c00156
Abstract: CCT251236 1, a potent chemical probe, was previously developed from a cell-based phenotypic high-throughput screen (HTS) to discover inhibitors of transcription mediated by HSF1, a transcription factor that supports malignancy. Owing to its activity against… read more here.
Keywords: cct361814 nxp800; clinical candidate; treatment refractory; candidate cct361814 ... See more keywords
An Analysis of Successful Hit-to-Clinical Candidate Pairs.
Sign Up to like & getrecommendations! Published in 2023 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.3c00521
Abstract: An analysis of 156 published clinical candidates from the Journal of Medicinal Chemistry between 2018 and 2021 was conducted to identify lead generation strategies most frequently employed leading to drug candidates. As in a previous… read more here.
Keywords: clinical candidate; hit clinical; chemistry; analysis ... See more keywords
Resurrecting the Condemned: Identification of N-Benzoxaborole Benzofuran GSK8175 as a Clinical Candidate with Reduced Metabolic Liability.
Sign Up to like & getrecommendations! Published in 2019 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.9b00415
Abstract: Recently, in a program designed to improve the metabolic stability of the HCV inhibitor GSK5852, N-benzoxaborole benzofuran (GSK8175) emerged as a clinical candidate that not only retains the broad-spectrum activity against HCV subgenomic replicons but… read more here.
Keywords: benzoxaborole benzofuran; chemistry; clinical candidate; benzofuran gsk8175 ... See more keywords
New Percutaneous Options for Tricuspid Intervention: How to Identify the Good Clinical Candidate
Sign Up to like & getrecommendations! Published in 2020 at "Frontiers in Cardiovascular Medicine"
DOI: 10.3389/fcvm.2020.583307
Abstract: The tricuspid valve has been neglected for a long time and severe tricuspid regurgitation (TR) was largely undertreated in the past due to a high operative risk. In the last years we observed the development… read more here.
Keywords: tricuspid intervention; options tricuspid; clinical candidate; percutaneous options ... See more keywords