5K9R

PDE10a with imidazopyrazine inhibitor

Summary for 5K9R

• Entry DOI: 10.2210/pdb5k9r/pdb
• Descriptor: cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A, ZINC ION, MAGNESIUM ION, ... (5 entities in total)
• Functional Keywords: hydrolase-hydrolase inhibitor complex, hydrolase/hydrolase inhibitor
• Biological source: Homo sapiens (Human)
• Cellular location: Cytoplasm: Q9Y233
• Total number of polymer chains: 2
• Total formula weight: 73403.94

Authors

Gibbs, A.G.,Schubert, C. (deposition date: 2016-06-01, release date: 2016-08-24, Last modification date: 2024-11-20)

Primary citation

Meegalla, S.K.,Huang, H.,Illig, C.R.,Parks, D.J.,Chen, J.,Lee, Y.K.,Wilson, K.J.,Patel, S.K.,Cheung, W.S.,Lu, T.,Kirchner, T.,Askari, H.B.,Geisler, J.,Patch, R.J.,Gibbs, A.C.,Rady, B.,Connelly, M.,Player, M.R.
Discovery of novel potent imidazo[1,2-b]pyridazine PDE10a inhibitors.
Bioorg.Med.Chem.Lett., 26:4216-4222, 2016

PubMed Abstract: Design and optimization of a novel series of imidazo[1,2-b]pyridazine PDE10a inhibitors are described. Compound 31 displays excellent pharmacokinetic properties and was also evaluated as an insulin secretagogue in vitro and in vivo.

PubMed: 27491708
DOI: 10.1016/j.bmcl.2016.07.054

Experimental method

X-RAY DIFFRACTION (2.7 Å)