Reaction Details |
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Target | cAMP-specific 3',5'-cyclic phosphodiesterase 4A |
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Ligand | BDBM30035 |
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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 | 21±1 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 |
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
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BDBM30035 |
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BDBM10851 |
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Name | BDBM30035 |
Synonyms: | triazolothiadiazine, 29 |
Type | Small organic molecule |
Emp. Form. | C21H19ClN4O2S |
Mol. Mass. | 426.919 |
SMILES | COc1ccc(cc1OCC1CC1)C1=Nn2c(SC1)nnc2-c1ccccc1Cl |t:15| |
Structure |
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