Reaction Details |
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Target | cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A |
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Ligand | BDBM50014905 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1347862 (CHEMBL3266764) |
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IC50 | 60±n/a nM |
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Citation | Bartolomé-Nebreda, JM; Delgado, F; Martín-Martín, ML; Martínez-Viturro, CM; Pastor, J; Tong, HM; Iturrino, L; Macdonald, GJ; Sanderson, W; Megens, A; Langlois, X; Somers, M; Vanhoof, G; Conde-Ceide, S Discovery of a potent, selective, and orally active phosphodiesterase 10A inhibitor for the potential treatment of schizophrenia. J Med Chem57:4196-212 (2014) [PubMed] Article |
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More Info.: | Get all data from this article, 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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BDBM50014905 |
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n/a |
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Name | BDBM50014905 |
Synonyms: | CHEMBL3262043 |
Type | Small organic molecule |
Emp. Form. | C18H24N6O2 |
Mol. Mass. | 356.4222 |
SMILES | CO[C@@H](C)Cn1cc(cn1)-c1c(C)nc2c(nccn12)N1CCOCC1 |r| |
Structure |
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