Reaction Details |
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Target | cGMP-dependent 3',5'-cyclic phosphodiesterase |
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Ligand | BDBM14776 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_305052 (CHEMBL831689) |
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IC50 | >10000±n/a nM |
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Citation | Boyle, CD; Xu, R; Asberom, T; Chackalamannil, S; Clader, JW; Greenlee, WJ; Guzik, H; Hu, Y; Hu, Z; Lankin, CM; Pissarnitski, DA; Stamford, AW; Wang, Y; Skell, J; Kurowski, S; Vemulapalli, S; Palamanda, J; Chintala, M; Wu, P; Myers, J; Wang, P Optimization of purine based PDE1/PDE5 inhibitors to a potent and selective PDE5 inhibitor for the treatment of male ED. Bioorg Med Chem Lett15:2365-9 (2005) [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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BDBM14776 |
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n/a |
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Name | BDBM14776 |
Synonyms: | 2-{2-ethoxy-5-[(4-ethylpiperazine-1-)sulfonyl]phenyl}-5-methyl-7-propyl-3H,4H-imidazo[1,5-a][1,2,4]triazin-4-one | CHEMBL1520 | Vardenafil | citric acid;2-[2-ethoxy-5-(4-ethylpiperazino)sulfonyl-phenyl]-5-methyl-7-propyl-1H-imidazo[5,1-f][1,2,4]triazin-4-one |
Type | Small organic molecule |
Emp. Form. | C23H32N6O4S |
Mol. Mass. | 488.603 |
SMILES | CCCc1nc(C)c2n1nc([nH]c2=O)-c1cc(ccc1OCC)S(=O)(=O)N1CCN(CC)CC1 |
Structure |
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