Structure of PDB 4p0n Chain A

Receptor sequence
>4p0nA (length=307) Species: 9606 (Homo sapiens) [Search protein sequence]
TLPVRLCKEIELFHFDIGPFENMWPGIFVYMVHRSCGTSCFELEKLCRFI
MSVKKNYRRVPYHNWKHAVTVAHCMYAILQNNHTLFTDLERKGLLIACLC
HDLDHRGFSNSYLQKFDHPLAALYSTSTMEQHHFSQTVSILQLEGHNIFS
TLSSSEYEQVLEIIRKAIIATDLALYFGNRKQLEEMYQTGSLNLNNQSHR
DRVIGLMMTACDLCSVTKLWPVTKLTANDIYAEFWAEGDEMKKLGIQPIP
MMDRDKKDEVPQGQLGFYNAVAIPCYTTLTQILPPTEPLLKACRDNLSQW
EKVIRGE
3D structure
PDB4p0n Discovery of Novel Imidazo[4,5-b]pyridines as Potent and Selective Inhibitors of Phosphodiesterase 10A (PDE10A).
ChainA
Resolution2.08 Å
3D
structure
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Enzymatic activity
Enzyme Commision number 3.1.4.17: 3',5'-cyclic-nucleotide phosphodiesterase.
Interaction with ligand
Site
#		 Ligand Ligand
chain		 Binding residues on receptor
(original residue number in PDB)		 Binding residues on receptor
(residue number reindexed from 1)		 Binding affinity
BS01 1IS A I682 Y683 P702 M703 E711 V712 G715 Q716 F719 I230 Y231 P250 M251 E259 V260 G263 Q264 F267 MOAD: ic50=0.8nM
PDBbind-CN: -logKd/Ki=8.66,IC50=2.2nM
BindingDB: IC50=0.800000nM
BS02 1IR A I682 Y683 P702 M703 E711 V712 G715 Q716 F719 I230 Y231 P250 M251 E259 V260 G263 Q264 F267 MOAD: ic50=3.4nM
BindingDB: IC50=2.2nM
BS03 ZN A H519 H553 D554 D664 H67 H101 D102 D212
Gene Ontology
Molecular Function
GO:0004114 3',5'-cyclic-nucleotide phosphodiesterase activity
GO:0008081 phosphoric diester hydrolase activity
Biological Process
GO:0007165 signal transduction

View graph for
Molecular Function
View graph for
Biological Process
External links
PDB RCSB:4p0n, PDBe:4p0n, PDBj:4p0n
PDBsum4p0n
PubMed24944747
UniProtQ9Y233|PDE10_HUMAN cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A (Gene Name=PDE10A)

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