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TargetcGMP-specific 3',5'-cyclic phosphodiesterase
LigandBDBM14394
Substrate/CompetitorBDBM14391
Meas. Tech.PDE Enzyme Inhibitor Assays
pH7.4±n/a
Temperature303.15±n/a K
IC50 3.1±n/a nM
CommentscGMP in a 3:1 ratio unlabeled to 3H-labeled at a concentration 1/3Km, such that IC50 = Ki.
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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BDBM14394
BDBM14391
NameBDBM14394
Synonyms:5-(2-butoxy-5-acetylpyridin-3-yl)-3-ethyl-2-(pyridin-2-ylmethyl)-2H,6H,7H-pyrazolo[4,3-d]pyrimidin-7-one | 5-(5-Acetyl-2-butoxy-3-pyridinyl)-3-ethyl-2-(2-pyridinylmethyl)-2,6-dihydro-7H-pyrazolo[4,3-d]pyrimidin-7-one | Sildenafil 5-methyl ketone analogue 9
TypeSmall organic molecule
Emp. Form.C24H26N6O3
Mol. Mass.446.5016
SMILESCCCCOc1ncc(cc1-c1nc2c(CC)n(Cc3ccccn3)nc2c(=O)[nH]1)C(C)=O
Structure
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