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TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4A
LigandBDBM50174020
Substrate/Competitorn/a
Meas. Tech.ChEMBL_326769
IC50 0.4±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
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  Blast E-value cutoff:
BDBM50174020
n/a
NameBDBM50174020
Synonyms:(S)-(+)-3-{2-[(3-Cyclopropyloxy-4-difluromethoxy)-phenyl]-2-[5-(2-(1-hydroxy-1-trifluoromethyl-2,2,2-trifluoro)ethyl)-thiazolyl]ethyl}pyridine N-Oxide | 2-{5-[(S)-1-(3-cyclopropoxy-4-difluoromethoxy-phenyl)-2-(1-oxy-pyridin-3-yl)-ethyl]-thiazol-2-yl}-1,1,1,3,3,3-hexafluoro-propan-2-ol | CHEMBL199015 | L-869298
TypeSmall organic molecule
Emp. Form.C23H18F8N2O4S
Mol. Mass.570.452
SMILESOC(c1ncc(s1)[C@@H](Cc1ccc[n+]([O-])c1)c1ccc(OC(F)F)c(OC2CC2)c1)(C(F)(F)F)C(F)(F)F
Structure
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