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TargetcAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A
LigandBDBM14753
Substrate/CompetitorBDBM10851
Meas. Tech.PDE Competitive Enzyme Inhibition Assay
pH7.5±n/a
Temperature295.15±n/a K
Ki 67±29 nM
Citation Chappie, TAHumphrey, JMAllen, MPEstep, KGFox, CBLebel, LALiras, SMarr, ESMenniti, FSPandit, JSchmidt, CJTu, MWilliams, RDYang, FV Discovery of a series of 6,7-dimethoxy-4-pyrrolidylquinazoline PDE10A inhibitors. J Med Chem50:182-5 (2007) [PubMed]  Article
More Info.:Get all data from this article,   Solution Info,  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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BDBM14753
BDBM10851
NameBDBM14753
Synonyms:(R)-4-[3-(3,4-Dimethoxy-phenoxy)-pyrrolidin-1-yl]-6,7-dimethoxy-quinazoline | 4-[(3R)-3-(3,4-dimethoxyphenoxy)pyrrolidin-1-yl]-6,7-dimethoxyquinazoline | 6,7-Dimethoxy-4-pyrrolidylquinazoline 16
TypeSmall organic molecule
Emp. Form.C22H25N3O5
Mol. Mass.411.451
SMILESCOc1ccc(O[C@@H]2CCN(C2)c2ncnc3cc(OC)c(OC)cc23)cc1OC |r|
Structure
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