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TargetcGMP-specific 3',5'-cyclic phosphodiesterase
LigandBDBM14408
Substrate/CompetitorBDBM14391
Meas. Tech.PDE Enzyme Inhibitor Assays
IC50 0.9±n/a nM
Citation Allerton, CMBarber, CGBeaumont, KCBrown, DGCole, SMEllis, DLane, CAMaw, GNMount, NMRawson, DJRobinson, CMStreet, SDSummerhill, NW A novel series of potent and selective PDE5 inhibitors with potential for high and dose-independent oral bioavailability. J Med Chem49:3581-94 (2006) [PubMed]  Article
More Info.:Get all data from this article,   Solution Info,  Assay Method
 
cGMP-specific 3',5'-cyclic phosphodiesterase
Name:cGMP-specific 3',5'-cyclic phosphodiesterase
Synonyms:3',5'-cyclic phosphodiesterase | CGB-PDE | PDE5 | PDE5A | PDE5A_HUMAN | Phosphodiesterase 2 and 5 (PDE2 and PDE5) | Phosphodiesterase 5 (PDE5) | Phosphodiesterase 5A | Phosphodiesterase 5A (PDE5A) | cGMP-binding cGMP-specific phosphodiesterase | cGMP-specific 3',5'-cyclic phosphodiesterase
Type:Protein
Mol. Mass.:99975.83
Organism:Homo sapiens (Human)
Description:O76074
Residue:875
Sequence:
MERAGPSFGQQRQQQQPQQQKQQQRDQDSVEAWLDDHWDFTFSYFVRKATREMVNAWFAE
RVHTIPVCKEGIRGHTESCSCPLQQSPRADNSAPGTPTRKISASEFDRPLRPIVVKDSEG
TVSFLSDSEKKEQMPLTPPRFDHDEGDQCSRLLELVKDISSHLDVTALCHKIFLHIHGLI
SADRYSLFLVCEDSSNDKFLISRLFDVAEGSTLEEVSNNCIRLEWNKGIVGHVAALGEPL
NIKDAYEDPRFNAEVDQITGYKTQSILCMPIKNHREEVVGVAQAINKKSGNGGTFTEKDE
KDFAAYLAFCGIVLHNAQLYETSLLENKRNQVLLDLASLIFEEQQSLEVILKKIAATIIS
FMQVQKCTIFIVDEDCSDSFSSVFHMECEELEKSSDTLTREHDANKINYMYAQYVKNTME
PLNIPDVSKDKRFPWTTENTGNVNQQCIRSLLCTPIKNGKKNKVIGVCQLVNKMEENTGK
VKPFNRNDEQFLEAFVIFCGLGIQNTQMYEAVERAMAKQMVTLEVLSYHASAAEEETREL
QSLAAAVVPSAQTLKITDFSFSDFELSDLETALCTIRMFTDLNLVQNFQMKHEVLCRWIL
SVKKNYRKNVAYHNWRHAFNTAQCMFAALKAGKIQNKLTDLEILALLIAALSHDLDHRGV
NNSYIQRSEHPLAQLYCHSIMEHHHFDQCLMILNSPGNQILSGLSIEEYKTTLKIIKQAI
LATDLALYIKRRGEFFELIRKNQFNLEDPHQKELFLAMLMTACDLSAITKPWPIQQRIAE
LVATEFFDQGDRERKELNIEPTDLMNREKKNKIPSMQVGFIDAICLQLYEALTHVSEDCF
PLLDGCRKNRQKWQALAEQQEKMLINGESGQAKRN
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  Blast E-value cutoff:
BDBM14408
BDBM14391
NameBDBM14408
Synonyms:5-(2-butoxy-5-acetylpyridin-3-yl)-3-ethyl-2-[(1-methyl-1H-imidazol-2-yl)methyl]-2H,6H,7H-pyrazolo[4,3-d]pyrimidin-7-one | 5-(5-Acetyl-2-butoxy-3-pyridinyl)-3-ethyl-2-[(1-methyl-1H-imidazol-2-yl)methyl]-2,6-dihydro-7H-pyrazolo[4,3-d]pyrimidin-7-one | Sildenafil 5-methyl ketone analogue 49
TypeSmall organic molecule
Emp. Form.C23H27N7O3
Mol. Mass.449.5056
SMILESCCCCOc1ncc(cc1-c1nc2c(CC)n(Cc3nccn3C)nc2c(=O)[nH]1)C(C)=O
Structure
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