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TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4A
LigandBDBM50174025
Substrate/Competitorn/a
Meas. Tech.ChEMBL_326769 (CHEMBL860119)
IC50 0.47±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 Lett15:5241-6 (2005) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
cAMP-specific 3',5'-cyclic phosphodiesterase 4A
Name:cAMP-specific 3',5'-cyclic phosphodiesterase 4A
Synonyms:3',5'-cyclic phosphodiesterase | DPDE2 | PDE46 | PDE4A | PDE4A_HUMAN | Phosphodiesterase 4 (PDE4) | Phosphodiesterase 4A | 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:
BDBM50174025
n/a
NameBDBM50174025
Synonyms:6-isopropyl-8-(3-(2-(4-(methylsulfonyl)phenyl)-2-(thiazol-2-yl)vinyl)phenyl)quinoline | CHEMBL196969
TypeSmall organic molecule
Emp. Form.C30H26N2O2S2
Mol. Mass.510.67
SMILESCC(C)c1cc(-c2cccc(\C=C(\c3nccs3)c3ccc(cc3)S(C)(=O)=O)c2)c2ncccc2c1
Structure
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