Structure-Based Drug Discovery of N-((R)-3-(7-Methyl-1 H-indazol-5-yl)-1-oxo-1-(((S)-1-oxo-3-(piperidin-4-yl)-1-(4-(pyridin-4-yl)piperazin-1-yl)propan-2-yl)amino)propan-2-yl)-2′-oxo-1′,2′-dihydrospiro[piperidine-4,4′-pyrido[2,3- d][1,3]oxazine]-1-carboxam

Article abstract of DOI:10.1021/acs.jmedchem.0c01003

Structure-based drug design enabled the discovery of 8, HTL22562, a calcitonin gene-related peptide (CGRP) receptor antagonist. The structure of 8 complexed with the CGRP receptor was determined at a 1.6 ? resolution. Compound 8 is a highly potent, select