5XKM
Crystal structure of human phosphodiesterase 2A in complex with 6-methyl-N-(1-(4-(trifluoromethoxy)phenyl)propyl)pyrazolo[1,5-a]pyrimidine-3-carboxamide
Summary for 5XKM
Entry DOI | 10.2210/pdb5xkm/pdb |
Descriptor | cGMP-dependent 3',5'-cyclic phosphodiesterase, MAGNESIUM ION, ZINC ION, ... (5 entities in total) |
Functional Keywords | hydrolase, hydrolase inhibitor, pde2a |
Biological source | Homo sapiens (Human) |
Cellular location | Isoform PDE2A3: Cell membrane ; Lipid-anchor . Isoform PDE2A2: Mitochondrion matrix . Isoform PDE2A1: Cytoplasm . Isoform 5: Mitochondrion : O00408 |
Total number of polymer chains | 6 |
Total formula weight | 244249.29 |
Authors | |
Primary citation | Mikami, S.,Sasaki, S.,Asano, Y.,Ujikawa, O.,Fukumoto, S.,Nakashima, K.,Oki, H.,Kamiguchi, N.,Imada, H.,Iwashita, H.,Taniguchi, T. Discovery of an Orally Bioavailable, Brain-Penetrating, in Vivo Active Phosphodiesterase 2A Inhibitor Lead Series for the Treatment of Cognitive Disorders. J. Med. Chem., 60:7658-7676, 2017 Cited by PubMed: 28759228DOI: 10.1021/acs.jmedchem.7b00709 PDB entries with the same primary citation |
Experimental method | X-RAY DIFFRACTION (2.16 Å) |
Structure validation
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