Reaction Details |
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Target | Dual specificity calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1A |
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Ligand | BDBM50258896 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEBML_1690773 |
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IC50 | 2497±n/a nM |
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Citation | Mikami, S; Nakamura, S; Ashizawa, T; Nomura, I; Kawasaki, M; Sasaki, S; Oki, H; Kokubo, H; Hoffman, ID; Zou, H; Uchiyama, N; Nakashima, K; Kamiguchi, N; Imada, H; Suzuki, N; Iwashita, H; Taniguchi, T Discovery of Clinical Candidate N-((1S)-1-(3-Fluoro-4-(trifluoromethoxy)phenyl)-2-methoxyethyl)-7-methoxy-2-oxo-2,3-dihydropyrido[2,3-b]pyrazine-4(1H)-carboxamide (TAK-915): A Highly Potent, Selective, and Brain-Penetrating Phosphodiesterase 2A Inhibitor for the Treatment of Cognitive Disorders. J Med Chem60:7677-7702 (2017) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Dual specificity calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1A |
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Name: | Dual specificity calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1A |
Synonyms: | 61 kDa Cam-PDE | Calcium/calmodulin-dependent 3',5'-cyclic phosphodiesterase 1A | Cam-PDE 1A | PDE1A | PDE1A_HUMAN | hCam-1 |
Type: | Protein |
Mol. Mass.: | 61245.69 |
Organism: | Homo sapiens (Human) |
Description: | P54750 |
Residue: | 535 |
Sequence: | MGSSATEIEELENTTFKYLTGEQTEKMWQRLKGILRCLVKQLERGDVNVVDLKKNIEYAA
SVLEAVYIDETRRLLDTEDELSDIQTDSVPSEVRDWLASTFTRKMGMTKKKPEEKPKFRS
IVHAVQAGIFVERMYRKTYHMVGLAYPAAVIVTLKDVDKWSFDVFALNEASGEHSLKFMI
YELFTRYDLINRFKIPVSCLITFAEALEVGYSKYKNPYHNLIHAADVTQTVHYIMLHTGI
MHWLTELEILAMVFAAAIHDYEHTGTTNNFHIQTRSDVAILYNDRSVLENHHVSAAYRLM
QEEEMNILINLSKDDWRDLRNLVIEMVLSTDMSGHFQQIKNIRNSLQQPEGIDRAKTMSL
ILHAADISHPAKSWKLHYRWTMALMEEFFLQGDKEAELGLPFSPLCDRKSTMVAQSQIGF
IDFIVEPTFSLLTDSTEKIVIPLIEEASKAETSSYVASSSTTIVGLHIADALRRSNTKGS
MSDGSYSPDYSLAAVDLKSFKNNLVDIIQQNKERWKELAAQEARTSSQKCEFIHQ
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BDBM50258896 |
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n/a |
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Name | BDBM50258896 |
Synonyms: | CHEMBL4060569 | US11419874, TAK-915 |
Type | Small organic molecule |
Emp. Form. | C19H18F4N4O5 |
Mol. Mass. | 458.3636 |
SMILES | COC[C@@H](NC(=O)N1CC(=O)Nc2cc(OC)cnc12)c1ccc(OC(F)(F)F)c(F)c1 |r| |
Structure |
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