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TargetcGMP-inhibited 3',5'-cyclic phosphodiesterase B
LigandBDBM50308557
Substrate/Competitorn/a
Meas. Tech.ChEMBL_613559
IC50>2000±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-inhibited 3',5'-cyclic phosphodiesterase B
Name:Phosphodiesterase 3 and 5 (PDE3 and PDE5)
Synonyms:CGI-PDE B | CGIP1 | CGIPDE1 | Cyclic GMP-inhibited phosphodiesterase B | Phosphodiesterase 3B | Phosphodiesterase 3B (PDE3B) | Phosphodiesterase Type 3 (PDE3B) | cGMP-inhibited 3,5-cyclic phosphodiesterase B
Type:Enzyme
Mol. Mass.:124318.95
Organism:Homo sapiens (Human)
Description:PDE3B was generated from the full-length recombinant human clone transfected into Sf9 cells.
Residue:1112
Sequence:
MRRDERDAKAMRSLQPPDGAGSPPESLRNGYVKSCVSPLRQDPPRGFFFHLCRFCNVELR
PPPASPQQPRRCSPFCRARLSLGALAAFVLALLLGAEPESWAAGAAWLRTLLSVCSHSLS
PLFSIACAFFFLTCFLTRTKRGPGPGRSCGSWWLLALPACCYLGDFLVWQWWSWPWGDGD
AGSAAPHTPPEAAAGRLLLVLSCVGLLLTLAHPLRLRHCVLVLLLASFVWWVSFTSLGSL
PSALRPLLSGLVGGAGCLLALGLDHFFQIREAPLHPRLSSAAEEKVPVIRPRRRSSCVSL
GETAASYYGSCKIFRRPSLPCISREQMILWDWDLKQWYKPHYQNSGGGNGVDLSVLNEAR
NMVSDLLTDPSLPPQVISSLRSISSLMGAFSGSCRPKINPLTPFPGFYPCSEIEDPAEKG
DRKLNKGLNRNSLPTPQLRRSSGTSGLLPVEQSSRWDRNNGKRPHQEFGISSQGCYLNGP
FNSNLLTIPKQRSSSVSLTHHVGLRRAGVLSSLSPVNSSNHGPVSTGSLTNRSPIEFPDT
ADFLNKPSVILQRSLGNAPNTPDFYQQLRNSDSNLCNSCGHQMLKYVSTSESDGTDCCSG
KSGEEENIFSKESFKLMETQQEEETEKKDSRKLFQEGDKWLTEEAQSEQQTNIEQEVSLD
LILVEEYDSLIEKMSNWNFPIFELVEKMGEKSGRILSQVMYTLFQDTGLLEIFKIPTQQF
MNYFRALENGYRDIPYHNRIHATDVLHAVWYLTTRPVPGLQQIHNGCGTGNETDSDGRIN
HGRIAYISSKSCSNPDESYGCLSSNIPALELMALYVAAAMHDYDHPGRTNAFLVATNAPQ
AVLYNDRSVLENHHAASAWNLYLSRPEYNFLLHLDHVEFKRFRFLVIEAILATDLKKHFD
FLAEFNAKANDVNSNGIEWSNENDRLLVCQVCIKLADINGPAKVRDLHLKWTEGIVNEFY
EQGDEEANLGLPISPFMDRSSPQLAKLQESFITHIVGPLCNSYDAAGLLPGQWLEAEEDN
DTESGDDEDGEELDTEDEEMENNLNPKPPRRKSRRRIFCQLMHHLTENHKIWKEIVEEEE
KCKADGNKLQVENSSLPQADEIQVIEEADEEE
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BDBM50308557
n/a
NameBDBM50308557
Synonyms:3-(4-(2-hydroxyethyl)piperazin-1-yl)-1-(2-propoxyethyl)-7-(6-methoxypyridin-3-yl)pyrido[3,4-b]pyrazin-2(1H)-one | CHEMBL591501
TypeSmall organic molecule
Emp. Form.C24H32N6O4
Mol. Mass.468.5487
SMILESCCCOCCn1c2cc(ncc2nc(N2CCN(CCO)CC2)c1=O)-c1ccc(OC)nc1
Structure
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