Structure of PDB 4tpm Chain A

Receptor sequence
>4tpmA (length=303) Species: 9606 (Homo sapiens) [Search protein sequence]
LPVRLCKEIELFHFDIGPFENMWPGIFVYMVHRSCGTSCFELEKLCRFIM
SVKKNYRRVPYHNWKHAVTVAHCMYAILQNNHTLFTDLERKGLLIACLCH
DLDHRGFSNSYLQKFDHPLAALYSTSTMEQHHFSQTVSILQLEGHNIFST
LSSSEYEQVLEIIRKAIIATDLALYFGNRKQLEEMYQTGSLNLNNQSHRD
RVIGLMMTACDLCSVTKLWPVTKLTANDIYAEFWAEGDEMKKLGIQPIPM
MDRDKKDEVPQGQLGFYNAVAIPCYTTLTQILPPTEPLLKACRDNLSQWE
KVI
3D structure
PDB4tpm Synthesis and preliminary biological evaluation of potent and selective 2-(3-alkoxy-1-azetidinyl) quinolines as novel PDE10A inhibitors with improved solubility.
ChainA
Resolution2.77 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 35E A L665 T675 I682 Y683 P702 M703 E711 V712 G715 F719 L212 T222 I229 Y230 P249 M250 E258 V259 G262 F266 PDBbind-CN: -logKd/Ki=8.62,IC50=2.4nM
BindingDB: IC50=2.4nM
BS02 ZN A H519 H553 D554 D664 H66 H100 D101 D211
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:4tpm, PDBe:4tpm, PDBj:4tpm
PDBsum4tpm
PubMed25456383
UniProtQ9Y233|PDE10_HUMAN cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A (Gene Name=PDE10A)

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