Reaction Details |
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Target | cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A |
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Ligand | BDBM14749 |
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Substrate/Competitor | BDBM10851 |
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Meas. Tech. | PDE Competitive Enzyme Inhibition Assay |
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pH | 7.5±n/a |
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Temperature | 295.15±n/a K |
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Ki | 171±20 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 |
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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BDBM14749 |
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BDBM10851 |
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Name | BDBM14749 |
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 |
Type | Small organic molecule |
Emp. Form. | C23H27N3O3 |
Mol. Mass. | 393.4788 |
SMILES | COc1cc2ncnc(N3CC[C@H](C3)Oc3cccc(c3)C(C)C)c2cc1OC |r| |
Structure |
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