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TargetcGMP-dependent 3',5'-cyclic phosphodiesterase
LigandBDBM50402945
Substrate/Competitorn/a
Meas. Tech.ChEMBL_885312 (CHEMBL2215175)
IC50>10000±n/a nM
Citation Rzasa, RMHu, ERumfelt, SChen, NAndrews, KLChmait, SFalsey, JRZhong, WJones, ADPorter, ALouie, SWZhao, XTreanor, JJAllen, JR Discovery of selective biaryl ethers as PDE10A inhibitors: improvement in potency and mitigation of Pgp-mediated efflux. Bioorg Med Chem Lett22:7371-5 (2012) [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:
BDBM50402945
n/a
NameBDBM50402945
Synonyms:CHEMBL2206213
TypeSmall organic molecule
Emp. Form.C25H26N4O2
Mol. Mass.414.4995
SMILESOCC1CCN(CC1)c1ccccc1Oc1ccc(Nc2nc3ccccc3[nH]2)cc1
Structure
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