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TargetPhosphodiesterase Type 10 (PDE10A)
LigandBDBM50350804
Substrate/Competitorn/a
Meas. Tech.ChEMBL_763299
IC50 247±n/a nM
Citation Helal, CJKang, ZHou, XPandit, JChappie, TAHumphrey, JMMarr, ESFennell, KFChenard, LKFox, CSchmidt, CJWilliams, RDChapin, DSSiuciak, JLebel, LMenniti, FCianfrogna, JFonseca, KRNelson, FRO'Connor, RMacDougall, MMcDowell, LLiras, S Use of structure-based design to discover a potent, selective, in vivo active phosphodiesterase 10A inhibitor lead series for the treatment of schizophrenia. J Med Chem54:4536-47 (2011) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Phosphodiesterase Type 10 (PDE10A)
Name:Phosphodiesterase Type 10 (PDE10A)
Synonyms:Phosphodiesterase 10 | Phosphodiesterase 10A (PDE10A2) | Rat recombinant PDE10a (rPDE10a) | cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A
Type:Enzyme
Mol. Mass.:90160.88
Organism:Rattus norvegicus (rat)
Description:PDE10A was generated from the full-length recombinant rat clone transfected into Sf9 cells.
Residue:794
Sequence:
MEDGPSNNASCFRRLTECFLSPSLTDEKVKAYLSLHPQVLDEFVSESVSAETVEKWLKRK
NNKAEDEPSPKEVSRYQDTNMQGVVYELNSYIEQRLDTGGDNHLLLYELSSIIRIATKAD
GFALYFLGECNNSLCVFTPPGMKEGQPRLIPAGPITQGTTISAYVAKSRKTLLVEDILGD
ERFPRGTGLESGTRIQSVLCLPIVTAIGDLIGILELYRHWGKEAFCLSHQEVATANLAWA
SVAIHQVQVCRGLAKQTELNDFLLDVSKTYFDNIVAIDSLLEHIMIYAKNLVNADRCALF
QVDHKNKELYSDLFDIGEEKEGKPVFKKTKEIRFSIEKGIAGQVARTGEVLNIPDAYADP
RFNREVDLYTGYTTRNILCMPIVSRGSVIGVVQMVNKISGSAFSKTDENNFKMFAVFCAL
ALHCANMYHRIRHSECIYRVTMEKLSYHSICTSEEWQGLMHFNLPARICRDIELFHFDIG
PFENMWPGIFVYMIHRSCGTSCFELEKLCRFIMSVKKNYRRVPYHNWKHAVTVAHCMYAI
LQNNNGLFTDLERKGLLIACLCHDLDHRGFSNSYLQKFDHPLAALYSTSTMEQHHFSQTV
SILQLEGHNIFSTLSSSEYEQVLEIIRKAIIATDLALYFGNRKQLEEMYQTGSLNLHNQS
HRDRVIGLMMTACDLCSVTKLWPVTKLTANDIYAEFWAEGDEMKKLGIQPIPMMDRDKRD
EVPQGQLGFYNAVAIPCYTTLTQILPPTEPLLKACRDNLNQWEKVIRGEETAMWISGPAT
SKSTSEKPTRKVDD
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  Blast E-value cutoff:
BDBM50350804
NameBDBM50350804
Synonyms:CHEMBL1819128
TypeSmall organic molecule
Emp. Form.C27H28N4O2
Mol. Mass.440.5368
SMILESCOc1cc2ncnc(N3CCCC(C3)c3ccccc3)c2cc1OCCc1ccccn1
Structure
n/a