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TargetcGMP-specific 3',5'-cyclic phosphodiesterase
LigandBDBM50300958
Substrate/Competitorn/a
Meas. Tech.ChEMBL_613534
IC50 1.1±n/a nM
Citation Hughes, RORogier, DJJacobsen, EJWalker, JKMacinnes, ABond, BRZhang, LLYu, YZheng, YRumsey, JMWalgren, JLCurtiss, SWFobian, YMHeasley, SECubbage, JWMoon, JBBrown, DLAcker, BAMaddux, TMTollefson, MBMischke, BVOwen, DRFreskos, JNMolyneaux, JMBenson, AGBlevis-Bal, RM Design, synthesis, and biological evaluation of 3-[4-(2-hydroxyethyl)piperazin-1-yl]-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)pyrido[3,4-b]pyrazin-2(1H)-one, a potent, orally active, brain penetrant inhibitor of phosphodiesterase 5 (PDE5). J Med Chem53:2656-60 (2010) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
cGMP-specific 3',5'-cyclic phosphodiesterase
Name:3',5'-cyclic phosphodiesterase
Synonyms:CGB-PDE | PDE5 | PDE5A | Phosphodiesterase 5 (PDE5) | Phosphodiesterase 5A | Phosphodiesterase 5A (PDE5A) | cGMP-binding cGMP-specific 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:
BDBM50300958
NameBDBM50300958
Synonyms:3-(2-(2-hydroxyethylamino)ethylamino)-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)pyrido[3,4-b]pyrazin-2(1H)-one | CHEMBL567252
TypeSmall organic molecule
Emp. Form.C22H30N6O4
Mol. Mass.442.5114
SMILESCCCOCCn1c2cc(ncc2nc(NCCNCCO)c1=O)-c1ccc(OC)nc1
Structure
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n/a