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TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4A
LigandBDBM30032
Substrate/CompetitorBDBM10851
Meas. Tech.PDE4A Inhibition Assay
pH7.2±n/a
Temperature295.15±n/a K
IC50 11±0.7 nM
Citation Skoumbourdis, APLeclair, CAStefan, ETurjanski, AGMaguire, WTitus, SAHuang, RAuld, DSInglese, JAustin, CPMichnick, SWXia, MThomas, CJ Exploration and optimization of substituted triazolothiadiazines and triazolopyridazines as PDE4 inhibitors. Bioorg Med Chem Lett19:3686-92 (2009) [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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BDBM30032
NameBDBM30032
Synonyms:triazolothiadiazine, 26
TypeSmall organic molecule
Emp. Form.C22H22N4O4S
Mol. Mass.438.499
SMILESCOc1ccc(cc1O[C@@H]1CCOC1)C1=Nn2c(SC1)nnc2-c1ccccc1OC |r,t:16|
Structure
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BDBM10851
NameBDBM10851
Synonyms:(4aR,6R,7R,7aS)-6-(6-amino-9H-purin-9-yl)-2,7-dihydroxy-hexahydro-1,3,5,2-furo[3,2-d][1,3,2]dioxaphosphinin-2-one | (4aR,6R,7R,7aS)-6-(6-amino-9H-purin-9-yl)tetrahydro-4H-furo[3,2-d][1,3,2]dioxaphosphinine-2,7-diol 2-oxide | ADENOSINE-3 ,5 -CYCLIC-MONOPHOSPHATE | Cyclic adenosine monophosphate | cAMP | cid_23902375
TypeSmall organic molecule
Emp. Form.C10H12N5O6P
Mol. Mass.329.2059
SMILESNc1ncnc2n(cnc12)[C@@H]1O[C@@H]2COP(O)(=O)O[C@H]2[C@H]1O
Structure
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