| Reaction Details |
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 | Report a problem with these data |
| Target | cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A |
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| Ligand | BDBM14758 |
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| Substrate/Competitor | BDBM10851 |
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| Meas. Tech. | PDE Competitive Enzyme Inhibition Assay |
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| Ki | 128±n/a nM |
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| Citation |  Chappie, TA; Humphrey, JM; Allen, MP; Estep, KG; Fox, CB; Lebel, LA; Liras, S; Marr, ES; Menniti, FS; Pandit, J; Schmidt, CJ; Tu, M; Williams, RD; Yang, FV Discovery of a series of 6,7-dimethoxy-4-pyrrolidylquinazoline PDE10A inhibitors. J Med Chem50:182-5 (2007) [PubMed] Article |
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| More Info.: | Get all data from this article, Solution Info, Assay Method |
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| cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A |
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| Name: | cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A |
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| Synonyms: | PDE10_RAT | Pde10a | Phosphodiesterase 10 | Phosphodiesterase 10A (PDE10A2) | Phosphodiesterase Type 10 (PDE10A) | Rat recombinant PDE10a (rPDE10a) |
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| Type: | Enzyme |
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| Mol. Mass.: | 90160.88 |
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| Organism: | Rattus norvegicus (rat) |
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| Description: | PDE10A was generated from the full-length recombinant rat clone transfected into Sf9 cells. |
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| Residue: | 794 |
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| Sequence: | MEDGPSNNASCFRRLTECFLSPSLTDEKVKAYLSLHPQVLDEFVSESVSAETVEKWLKRK
NNKAEDEPSPKEVSRYQDTNMQGVVYELNSYIEQRLDTGGDNHLLLYELSSIIRIATKAD
GFALYFLGECNNSLCVFTPPGMKEGQPRLIPAGPITQGTTISAYVAKSRKTLLVEDILGD
ERFPRGTGLESGTRIQSVLCLPIVTAIGDLIGILELYRHWGKEAFCLSHQEVATANLAWA
SVAIHQVQVCRGLAKQTELNDFLLDVSKTYFDNIVAIDSLLEHIMIYAKNLVNADRCALF
QVDHKNKELYSDLFDIGEEKEGKPVFKKTKEIRFSIEKGIAGQVARTGEVLNIPDAYADP
RFNREVDLYTGYTTRNILCMPIVSRGSVIGVVQMVNKISGSAFSKTDENNFKMFAVFCAL
ALHCANMYHRIRHSECIYRVTMEKLSYHSICTSEEWQGLMHFNLPARICRDIELFHFDIG
PFENMWPGIFVYMIHRSCGTSCFELEKLCRFIMSVKKNYRRVPYHNWKHAVTVAHCMYAI
LQNNNGLFTDLERKGLLIACLCHDLDHRGFSNSYLQKFDHPLAALYSTSTMEQHHFSQTV
SILQLEGHNIFSTLSSSEYEQVLEIIRKAIIATDLALYFGNRKQLEEMYQTGSLNLHNQS
HRDRVIGLMMTACDLCSVTKLWPVTKLTANDIYAEFWAEGDEMKKLGIQPIPMMDRDKRD
EVPQGQLGFYNAVAIPCYTTLTQILPPTEPLLKACRDNLNQWEKVIRGEETAMWISGPAT
SKSTSEKPTRKVDD
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| BDBM14758 |
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| BDBM10851 |
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| Name | BDBM14758 |
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| Synonyms: | (R)-6,7-Dimethoxy-4-[3-(pyridin-3-yloxy)-pyrrolidin-1-yl]-quinazoline | 6,7-Dimethoxy-4-pyrrolidylquinazoline 19 | 6,7-dimethoxy-4-[(3R)-3-(pyridin-3-yloxy)pyrrolidin-1-yl]quinazoline |
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| Type | Small organic molecule |
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| Emp. Form. | C19H20N4O3 |
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| Mol. Mass. | 352.3871 |
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| SMILES | COc1cc2ncnc(N3CC[C@H](C3)Oc3cccnc3)c2cc1OC |r| |
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| Structure | 
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