Structure of PDB 4yqh Chain A

Receptor sequence
>4yqhA (length=321) Species: 9606 (Homo sapiens) [Search protein sequence]
SICTSEEWQGLMQFTLPVRLCKEIELFHFDIGPFENMWPGIFVYMVHRSC
GTSCFELEKLCRFIMSVKKNYRRVPYHNWKHAVTVAHCMYAILQNNHTLF
TDLERKGLLIACLCHDLDHRGFSNSYLQKFDHPLAALYSTSTMEQHHFSQ
TVSILQLEGHNIFSTLSSSEYEQVLEIIRKAIIATDLALYFGNRKQLEEM
YQTGSLNLNNQSHRDRVIGLMMTACDLCSVTKLWPVTKLTANDIYAEFWA
EGDEMKKLGIQPIPMMDRDKKDEVPQGQLGFYNAVAIPCYTTLTQILPPT
EPLLKACRDNLSQWEKVIRGE
3D structure
PDB4yqh Evolution and synthesis of novel orally bioavailable inhibitors of PDE10A.
ChainA
Resolution2.308 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 ZN A H529 H563 D564 D674 H81 H115 D116 D226
BS02 MG A D564 H595 D116 H147
BS03 4F7 A S677 I692 Y693 P712 M713 E721 V722 G725 Q726 F729 S229 I244 Y245 P264 M265 E273 V274 G277 Q278 F281 MOAD: ic50=0.009uM
PDBbind-CN: -logKd/Ki=8.05,IC50=0.009uM
BindingDB: IC50=<500nM
Gene Ontology
Molecular Function
GO:0004114 3',5'-cyclic-nucleotide phosphodiesterase activity
GO:0008081 phosphoric diester hydrolase activity
Biological Process
GO:0007165 signal transduction

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Molecular Function
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Biological Process
External links
PDB RCSB:4yqh, PDBe:4yqh, PDBj:4yqh
PDBsum4yqh
PubMed25863433
UniProtQ9Y233|PDE10_HUMAN cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A (Gene Name=PDE10A)

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