Reaction Details |
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Target | cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A |
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Ligand | BDBM50350798 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_763299 (CHEMBL1820393) |
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IC50 | 17±n/a nM |
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Citation | Helal, CJ; Kang, Z; Hou, X; Pandit, J; Chappie, TA; Humphrey, JM; Marr, ES; Fennell, KF; Chenard, LK; Fox, C; Schmidt, CJ; Williams, RD; Chapin, DS; Siuciak, J; Lebel, L; Menniti, F; Cianfrogna, J; Fonseca, KR; Nelson, FR; O'Connor, R; MacDougall, M; McDowell, L; Liras, S Use of structure-based design to discover a potent, selective, in vivo active phosphodiesterase 10A inhibitor lead series for the treatment of schizophrenia. J Med Chem54:4536-47 (2011) [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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BDBM50350798 |
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n/a |
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Name | BDBM50350798 |
Synonyms: | CHEMBL1738857 |
Type | Small organic molecule |
Emp. Form. | C20H17N3O2 |
Mol. Mass. | 331.3679 |
SMILES | COc1cc2cncnc2cc1OCCc1ccc2ccccc2n1 |
Structure |
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