Ki Summary BindingDB logo
myBDB logout
Reaction Details
Report a problem with these data
TargetcAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A
LigandBDBM14749
Substrate/CompetitorBDBM10851
Meas. Tech.PDE Competitive Enzyme Inhibition Assay
pH7.5±n/a
Temperature295.15±n/a K
Ki 171±20 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
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM14749
BDBM10851
NameBDBM14749
Synonyms:(R)-4-[3-(3-Isopropyl-phenoxy)-pyrrolidin-1-yl]-6,7-dimethoxy-quinazoline | 6,7-Dimethoxy-4-pyrrolidylquinazoline 12 | 6,7-dimethoxy-4-[(3R)-3-[3-(propan-2-yl)phenoxy]pyrrolidin-1-yl]quinazoline
TypeSmall organic molecule
Emp. Form.C23H27N3O3
Mol. Mass.393.4788
SMILESCOc1cc2ncnc(N3CC[C@H](C3)Oc3cccc(c3)C(C)C)c2cc1OC |r|
Structure
Search PDB for entries with ligand similarity:Similarity to this molecule at least: