| Reaction Details |
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 | Report a problem with these data |
| Target | cGMP-dependent 3',5'-cyclic phosphodiesterase |
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| Ligand | BDBM50491653 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_962032 (CHEMBL2387855) |
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| IC50 | 102±n/a nM |
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| Citation |  Plummer, MS; Cornicelli, J; Roark, H; Skalitzky, DJ; Stankovic, CJ; Bove, S; Pandit, J; Goodman, A; Hicks, J; Shahripour, A; Beidler, D; Lu, XK; Sanchez, B; Whitehead, C; Sarver, R; Braden, T; Gowan, R; Shen, XQ; Welch, K; Ogden, A; Sadagopan, N; Baum, H; Miller, H; Banotai, C; Spessard, C; Lightle, S Discovery of potent, selective, bioavailable phosphodiesterase 2 (PDE2) inhibitors active in an osteoarthritis pain model, part I: transformation of selective pyrazolodiazepinone phosphodiesterase 4 (PDE4) inhibitors into selective PDE2 inhibitors. Bioorg Med Chem Lett23:3438-42 (2013) [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 |
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| Synonyms: | CGS-PDE | Cyclic GMP-stimulated phosphodiesterase | Homo sapiens phosphodiesterase 2A (PDE2A) | NM_002599 | PDE2A | PDE2A_HUMAN | cGSPDE |
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| Type: | Enzyme Catalytic Domain |
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| Mol. Mass.: | 105691.58 |
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| Organism: | Homo sapiens (Human) |
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| Description: | O00408 |
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| Residue: | 941 |
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| Sequence: | MGQACGHSILCRSQQYPAARPAEPRGQQVFLKPDEPPPPPQPCADSLQDALLSLGSVIDI
SGLQRAVKEALSAVLPRVETVYTYLLDGESQLVCEDPPHELPQEGKVREAIISQKRLGCN
GLGFSDLPGKPLARLVAPLAPDTQVLVMPLADKEAGAVAAVILVHCGQLSDNEEWSLQAV
EKHTLVALRRVQVLQQRGPREAPRAVQNPPEGTAEDQKGGAAYTDRDRKILQLCGELYDL
DASSLQLKVLQYLQQETRASRCCLLLVSEDNLQLSCKVIGDKVLGEEVSFPLTGCLGQVV
EDKKSIQLKDLTSEDVQQLQSMLGCELQAMLCVPVISRATDQVVALACAFNKLEGDLFTD
EDEHVIQHCFHYTSTVLTSTLAFQKEQKLKCECQALLQVAKNLFTHLDDVSVLLQEIITE
ARNLSNAEICSVFLLDQNELVAKVFDGGVVDDESYEIRIPADQGIAGHVATTGQILNIPD
AYAHPLFYRGVDDSTGFRTRNILCFPIKNENQEVIGVAELVNKINGPWFSKFDEDLATAF
SIYCGISIAHSLLYKKVNEAQYRSHLANEMMMYHMKVSDDEYTKLLHDGIQPVAAIDSNF
ASFTYTPRSLPEDDTSMAILSMLQDMNFINNYKIDCPTLARFCLMVKKGYRDPPYHNWMH
AFSVSHFCYLLYKNLELTNYLEDIEIFALFISCMCHDLDHRGTNNSFQVASKSVLAALYS
SEGSVMERHHFAQAIAILNTHGCNIFDHFSRKDYQRMLDLMRDIILATDLAHHLRIFKDL
QKMAEVGYDRNNKQHHRLLLCLLMTSCDLSDQTKGWKTTRKIAELIYKEFFSQGDLEKAM
GNRPMEMMDREKAYIPELQISFMEHIAMPIYKLLQDLFPKAAELYERVASNREHWTKVSH
KFTIRGLPSNNSLDFLDEEYEVPDLDGTRAPINGCCSLDAE
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| BDBM50491653 |
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| n/a |
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| Name | BDBM50491653 |
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| Synonyms: | CHEMBL2387136 |
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| Type | Small organic molecule |
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| Emp. Form. | C19H24N4O2 |
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| Mol. Mass. | 340.4195 |
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| SMILES | CCC(CC)c1nn(CCO)c2c1N=C(CNC2=O)c1ccccc1 |c:14| |
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| Structure | 
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