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TargetcAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A
LigandBDBM50350798
Substrate/Competitorn/a
Meas. Tech.ChEMBL_763299 (CHEMBL1820393)
IC50 17±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
 
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A
Name:cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A
Synonyms:PDE10_RAT | Pde10a | Phosphodiesterase 10 | Phosphodiesterase 10A (PDE10A2) | Phosphodiesterase Type 10 (PDE10A) | Rat recombinant PDE10a (rPDE10a)
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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BDBM50350798
n/a
NameBDBM50350798
Synonyms:CHEMBL1738857
TypeSmall organic molecule
Emp. Form.C20H17N3O2
Mol. Mass.331.3679
SMILESCOc1cc2cncnc2cc1OCCc1ccc2ccccc2n1
Structure
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