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TargetcGMP-specific 3',5'-cyclic phosphodiesterase
LigandBDBM50308555
Substrate/Competitorn/a
Meas. Tech.ChEMBL_613534
IC50 0.720000±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 Chem 53:2656-60 (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:
BDBM50308555
n/a
NameBDBM50308555
Synonyms:3-(4-(2-hydroxyethyl)-1,4-diazepan-1-yl)-1-(2-isopropoxyethyl)-7-(6-methoxypyridin-3-yl)pyrido[3,4-b]pyrazin-2(1H)-one | CHEMBL590545
TypeSmall organic molecule
Emp. Form.C25H34N6O4
Mol. Mass.482.5753
SMILESCCCOCCn1c2cc(ncc2nc(N2CCCN(CCO)CC2)c1=O)-c1ccc(OC)nc1
Structure
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