Reaction Details |
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Target | cGMP-dependent 3',5'-cyclic phosphodiesterase |
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Ligand | BDBM50258923 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEBML_1690806 |
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IC50 | 8.7±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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cGMP-dependent 3',5'-cyclic phosphodiesterase |
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Name: | cGMP-dependent 3',5'-cyclic phosphodiesterase |
Synonyms: | CGS-PDE | Cyclic GMP-stimulated phosphodiesterase | Homo sapiens phosphodiesterase 2A (PDE2A) | NM_002599 | PDE2A | PDE2A_HUMAN | cGSPDE |
Type: | Enzyme Catalytic Domain |
Mol. Mass.: | 105691.58 |
Organism: | Homo sapiens (Human) |
Description: | O00408 |
Residue: | 941 |
Sequence: | MGQACGHSILCRSQQYPAARPAEPRGQQVFLKPDEPPPPPQPCADSLQDALLSLGSVIDI
SGLQRAVKEALSAVLPRVETVYTYLLDGESQLVCEDPPHELPQEGKVREAIISQKRLGCN
GLGFSDLPGKPLARLVAPLAPDTQVLVMPLADKEAGAVAAVILVHCGQLSDNEEWSLQAV
EKHTLVALRRVQVLQQRGPREAPRAVQNPPEGTAEDQKGGAAYTDRDRKILQLCGELYDL
DASSLQLKVLQYLQQETRASRCCLLLVSEDNLQLSCKVIGDKVLGEEVSFPLTGCLGQVV
EDKKSIQLKDLTSEDVQQLQSMLGCELQAMLCVPVISRATDQVVALACAFNKLEGDLFTD
EDEHVIQHCFHYTSTVLTSTLAFQKEQKLKCECQALLQVAKNLFTHLDDVSVLLQEIITE
ARNLSNAEICSVFLLDQNELVAKVFDGGVVDDESYEIRIPADQGIAGHVATTGQILNIPD
AYAHPLFYRGVDDSTGFRTRNILCFPIKNENQEVIGVAELVNKINGPWFSKFDEDLATAF
SIYCGISIAHSLLYKKVNEAQYRSHLANEMMMYHMKVSDDEYTKLLHDGIQPVAAIDSNF
ASFTYTPRSLPEDDTSMAILSMLQDMNFINNYKIDCPTLARFCLMVKKGYRDPPYHNWMH
AFSVSHFCYLLYKNLELTNYLEDIEIFALFISCMCHDLDHRGTNNSFQVASKSVLAALYS
SEGSVMERHHFAQAIAILNTHGCNIFDHFSRKDYQRMLDLMRDIILATDLAHHLRIFKDL
QKMAEVGYDRNNKQHHRLLLCLLMTSCDLSDQTKGWKTTRKIAELIYKEFFSQGDLEKAM
GNRPMEMMDREKAYIPELQISFMEHIAMPIYKLLQDLFPKAAELYERVASNREHWTKVSH
KFTIRGLPSNNSLDFLDEEYEVPDLDGTRAPINGCCSLDAE
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BDBM50258923 |
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n/a |
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Name | BDBM50258923 |
Synonyms: | CHEMBL4085207 |
Type | Small organic molecule |
Emp. Form. | C19H19F3N4O4 |
Mol. Mass. | 424.3738 |
SMILES | COCC(NC(=O)N1CC(=O)Nc2cc(C)cnc12)c1ccc(OC(F)(F)F)cc1 |
Structure |
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