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TargetcGMP-dependent 3',5'-cyclic phosphodiesterase
LigandBDBM50026821
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1690400 (CHEMBL4040970)
IC50 10.0±n/a nM
Citation Mikami, SSasaki, SAsano, YUjikawa, OFukumoto, SNakashima, KOki, HKamiguchi, NImada, HIwashita, HTaniguchi, T Discovery of an Orally Bioavailable, Brain-Penetrating, in Vivo Active Phosphodiesterase 2A Inhibitor Lead Series for the Treatment of Cognitive Disorders. J Med Chem60:7658-7676 (2017) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
cGMP-dependent 3',5'-cyclic phosphodiesterase
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
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM50026821
n/a
NameBDBM50026821
Synonyms:CHEMBL3331521 | US11419874, Example 10 | US9669035, B-1b
TypeSmall organic molecule
Emp. Form.C24H28N6O2
Mol. Mass.432.5181
SMILESCCCCOc1cncc(c1)-c1nnc2c(C)nc3ccc(CN4CCOCC4)cc3n12
Structure
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