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TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4A
LigandBDBM14386
Substrate/CompetitorBDBM10851
Meas. Tech.PDE Activity Assay
pH8±n/a
Temperature295.15±n/a K
Ki 223±72 nM
Citation Whitehead JWLee GPGharagozloo PHofer PGehrig AWintergerst PSmyth DMcCoull WHachicha MPatel AKyle DJ 8-Substituted analogues of 3-(3-cyclopentyloxy-4-methoxy-benzyl)-8-isopropyladenine: highly potent and selective PDE4 inhibitors. J Med Chem 48:1237-43 (2005) [PubMed]  Article
More Info.:Get all data from this article,  Inhibition_Run data,   Solution Info,  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:
BDBM14386
BDBM10851
NameBDBM14386
Synonyms:3-(3-Cyclopentyloxy-4-methoxy-benzyl)-8-[1,1-dimethyl-2-(thiophen-3-yloxy)-ethyl]-3H-purin-6-ylamine | 3-{[3-(cyclopentyloxy)-4-methoxyphenyl]methyl}-8-[2-methyl-1-(thiophen-3-yloxy)propan-2-yl]-3H-purin-6-amine | V11294 Analogue 5v
TypeSmall organic molecule
Emp. Form.C26H31N5O3S
Mol. Mass.493.621
SMILESCOc1ccc(Cn2cnc(N)c3nc(nc23)C(C)(C)COc2ccsc2)cc1OC1CCCC1
Structure
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