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TargetcGMP-specific 3',5'-cyclic phosphodiesterase
LigandBDBM50297810
Substrate/Competitorn/a
Meas. Tech.ChEMBL_584078 (CHEMBL1058319)
IC50 13±n/a nM
Citation Owen, DRWalker, JKJon Jacobsen, EFreskos, JNHughes, ROBrown, DLBell, ASBrown, DGPhillips, CMischke, BVMolyneaux, JMFobian, YMHeasley, SEMoon, JBStallings, WCJoseph Rogier, DFox, DNPalmer, MJRinger, TRodriquez-Lens, MCubbage, JWBlevis-Bal, RMBenson, AGAcker, BAMaddux, TMTollefson, MBBond, BRMacinnes, AYu, Y Identification, synthesis and SAR of amino substituted pyrido[3,2b]pyrazinones as potent and selective PDE5 inhibitors. Bioorg Med Chem Lett19:4088-91 (2009) [PubMed]  Article
More Info.:Get all data from this article,  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
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM50297810
n/a
NameBDBM50297810
Synonyms:4-(cyclohexylmethyl)-6-(4-fluorophenyl)-2-(pyridin-3-ylmethylamino)pyrido[2,3-b]pyrazin-3(4H)-one | CHEMBL563661
TypeSmall organic molecule
Emp. Form.C26H26FN5O
Mol. Mass.443.5159
SMILESFc1ccc(cc1)-c1ccc2nc(NCc3cccnc3)c(=O)n(CC3CCCCC3)c2n1
Structure
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