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TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4A
LigandBDBM50174023
Substrate/Competitorn/a
Meas. Tech.ChEMBL_326769
IC50 0.5±n/a nM
Citation Macdonald DMastracchio APerrier HDubé DGallant MLacombe PDeschênes DRoy BScheigetz JBateman KLi CTrimble LADay SChauret NNicoll-Griffith DASilva JMHuang ZLaliberté FLiu SEthier DPon DMuise EBoulet LChan CCStyhler ACharleson SMancini JMasson PClaveau DNicholson DTurner MYoung RNGirard Y Discovery of a substituted 8-arylquinoline series of PDE4 inhibitors: structure-activity relationship, optimization, and identification of a highly potent, well tolerated, PDE4 inhibitor. Bioorg Med Chem Lett 15:5241-6 (2005) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
cAMP-specific 3',5'-cyclic phosphodiesterase 4A
Name:Phosphodiesterase 4 and 5 (PDE4 and PDE5)
Synonyms:DPDE2 | PDE46 | PDE4A | Phosphodiesterase 4A (PDE4)
Type:Enzyme
Mol. Mass.:98113.27
Organism:Homo sapiens (Human)
Description:P27815
Residue:886
Sequence:
MEPPTVPSERSLSLSLPGPREGQATLKPPPQHLWRQPRTPIRIQQRGYSDSAERAERERQ
PHRPIERADAMDTSDRPGLRTTRMSWPSSFHGTGTGSGGAGGGSSRRFEAENGPTPSPGR
SPLDSQASPGLVLHAGAATSQRRESFLYRSDSDYDMSPKTMSRNSSVTSEAHAEDLIVTP
FAQVLASLRSVRSNFSLLTNVPVPSNKRSPLGGPTPVCKATLSEETCQQLARETLEELDW
CLEQLETMQTYRSVSEMASHKFKRMLNRELTHLSEMSRSGNQVSEYISTTFLDKQNEVEI
PSPTMKEREKQQAPRPRPSQPPPPPVPHLQPMSQITGLKKLMHSNSLNNSNIPRFGVKTD
QEELLAQELENLNKWGLNIFCVSDYAGGRSLTCIMYMIFQERDLLKKFRIPVDTMVTYML
TLEDHYHADVAYHNSLHAADVLQSTHVLLATPALDAVFTDLEILAALFAAAIHDVDHPGV
SNQFLINTNSELALMYNDESVLENHHLAVGFKLLQEDNCDIFQNLSKRQRQSLRKMVIDM
VLATDMSKHMTLLADLKTMVETKKVTSSGVLLLDNYSDRIQVLRNMVHCADLSNPTKPLE
LYRQWTDRIMAEFFQQGDRERERGMEISPMCDKHTASVEKSQVGFIDYIVHPLWETWADL
VHPDAQEILDTLEDNRDWYYSAIRQSPSPPPEEESRGPGHPPLPDKFQFELTLEEEEEEE
ISMAQIPCTAQEALTAQGLSGVEEALDATIAWEASPAQESLEVMAQEASLEAELEAVYLT
QQAQSTGSAPVAPDEFSSREEFVVAVSHSSPSALALQSPLLPAWRTLSVSEHAPGLPGLP
STAAEVEAQREHQAAKRACSACAGTFGEDTSALPAPGGGGSGGDPT
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM50174023
n/a
NameBDBM50174023
Synonyms:(E)-6-isopropyl-8-(3-(2-(3-methyl-1,2,4-oxadiazol-5-yl)-2-(pyridin-2-yl)vinyl)phenyl)quinoline | CHEMBL197494
TypeSmall organic molecule
Emp. Form.C28H24N4O
Mol. Mass.432.5164
SMILESCC(C)c1cc(-c2cccc(\C=C(\c3nc(C)no3)c3ccccn3)c2)c2ncccc2c1
Structure
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