| Reaction Details |
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 | Report a problem with these data |
| Target | cAMP-specific 3',5'-cyclic phosphodiesterase 4A |
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| Ligand | BDBM30031 |
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| Substrate/Competitor | BDBM10851 |
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| Meas. Tech. | PDE4A Inhibition Assay |
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| pH | 7.2±n/a |
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| Temperature | 295.15±n/a K |
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| IC50 | 20±0.9 nM |
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| Citation |  Skoumbourdis, AP; Leclair, CA; Stefan, E; Turjanski, AG; Maguire, W; Titus, SA; Huang, R; Auld, DS; Inglese, J; Austin, CP; Michnick, SW; Xia, M; Thomas, CJ Exploration and optimization of substituted triazolothiadiazines and triazolopyridazines as PDE4 inhibitors. Bioorg Med Chem Lett19:3686-92 (2009) [PubMed] Article |
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| More Info.: | Get all data from this article, Inhibition_Run data, Solution Info, Assay Method |
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| cAMP-specific 3',5'-cyclic phosphodiesterase 4A |
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| Name: | cAMP-specific 3',5'-cyclic phosphodiesterase 4A |
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| Synonyms: | 3',5'-cyclic phosphodiesterase | DPDE2 | PDE46 | PDE4A | PDE4A_HUMAN | Phosphodiesterase 4 (PDE4) | Phosphodiesterase 4A | Phosphodiesterase 4A (PDE4) |
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| Type: | Enzyme |
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| Mol. Mass.: | 98113.27 |
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| Organism: | Homo sapiens (Human) |
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| Description: | P27815 |
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| Residue: | 886 |
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| Sequence: | MEPPTVPSERSLSLSLPGPREGQATLKPPPQHLWRQPRTPIRIQQRGYSDSAERAERERQ
PHRPIERADAMDTSDRPGLRTTRMSWPSSFHGTGTGSGGAGGGSSRRFEAENGPTPSPGR
SPLDSQASPGLVLHAGAATSQRRESFLYRSDSDYDMSPKTMSRNSSVTSEAHAEDLIVTP
FAQVLASLRSVRSNFSLLTNVPVPSNKRSPLGGPTPVCKATLSEETCQQLARETLEELDW
CLEQLETMQTYRSVSEMASHKFKRMLNRELTHLSEMSRSGNQVSEYISTTFLDKQNEVEI
PSPTMKEREKQQAPRPRPSQPPPPPVPHLQPMSQITGLKKLMHSNSLNNSNIPRFGVKTD
QEELLAQELENLNKWGLNIFCVSDYAGGRSLTCIMYMIFQERDLLKKFRIPVDTMVTYML
TLEDHYHADVAYHNSLHAADVLQSTHVLLATPALDAVFTDLEILAALFAAAIHDVDHPGV
SNQFLINTNSELALMYNDESVLENHHLAVGFKLLQEDNCDIFQNLSKRQRQSLRKMVIDM
VLATDMSKHMTLLADLKTMVETKKVTSSGVLLLDNYSDRIQVLRNMVHCADLSNPTKPLE
LYRQWTDRIMAEFFQQGDRERERGMEISPMCDKHTASVEKSQVGFIDYIVHPLWETWADL
VHPDAQEILDTLEDNRDWYYSAIRQSPSPPPEEESRGPGHPPLPDKFQFELTLEEEEEEE
ISMAQIPCTAQEALTAQGLSGVEEALDATIAWEASPAQESLEVMAQEASLEAELEAVYLT
QQAQSTGSAPVAPDEFSSREEFVVAVSHSSPSALALQSPLLPAWRTLSVSEHAPGLPGLP
STAAEVEAQREHQAAKRACSACAGTFGEDTSALPAPGGGGSGGDPT
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| BDBM30031 |
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| BDBM10851 |
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| Name | BDBM30031 |
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| Synonyms: | triazolothiadiazine, 25 |
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| Type | Small organic molecule |
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| Emp. Form. | C22H22N4O4S |
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| Mol. Mass. | 438.499 |
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| SMILES | COc1ccc(cc1OC1CCOC1)C1=Nn2c(SC1)nnc2-c1ccccc1OC |t:16| |
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| Structure | 
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