Lead identification of novel and selective TYK2 inhibitors was written by Liang, Jun;Tsui, Vickie;Van Abbema, Anne;Bao, Liang;Barrett, Kathy;Beresini, Maureen;Berezhkovskiy, Leo;Blair, Wade S.;Chang, Christine;Driscoll, James;Eigenbrot, Charles;Ghilardi, Nico;Gibbons, Paul;Halladay, Jason;Johnson, Adam;Kohli, Pawan Bir;Lai, Yingjie;Liimatta, Marya;Mantik, Priscilla;Menghrajani, Kapil;Murray, Jeremy;Sambrone, Amy;Xiao, Yisong;Shia, Steven;Shin, Young;Smith, Jan;Sohn, Sue;Stanley, Mark;Ultsch, Mark;Zhang, Birong;Wu, Lawren C.;Magnuson, Steven. And the article was included in European Journal of Medicinal Chemistry in 2013.Quality Control of 3-Aminopyridazine This article mentions the following:
A therapeutic rationale is proposed for the treatment of inflammatory diseases, such as psoriasis and inflammatory bowel diseases (IBD), by selective targeting of TYK2. Hit triage, following a high-throughput screen for TYK2 inhibitors, revealed pyridine (I) as a promising starting point for lead identification. Initial expansion of 3 sep. regions of the mol. led to eventual identification of cyclopropyl amide (II), a potent lead analog with good kinase selectivity, physicochem. properties, and pharmacokinetic profile. Anal. of the binding modes of the series in TYK2 and JAK2 crystal structures revealed key interactions leading to good TYK2 potency and design options for future optimization of selectivity. In the experiment, the researchers used many compounds, for example, 3-Aminopyridazine (cas: 5469-70-5Quality Control of 3-Aminopyridazine).
3-Aminopyridazine (cas: 5469-70-5) belongs to pyridazine derivatives. The pyridazine derivatives are mostly present in biologically active compounds and are also present with different pharmacophores. In the past decade, X-ray data were reported with regard to the characterization and structural elucidation of a number of pyridazine-metal complexes, including pyridazine ligands with zinc, nickel, copper, cadmium and ruthenium.Quality Control of 3-Aminopyridazine
Referemce:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem