| 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 | BDBM50174021 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_326769 (CHEMBL860119) |
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| IC50 | 1±n/a nM |
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| Citation |  Macdonald, D; Mastracchio, A; Perrier, H; Dubé, D; Gallant, M; Lacombe, P; Deschênes, D; Roy, B; Scheigetz, J; Bateman, K; Li, C; Trimble, LA; Day, S; Chauret, N; Nicoll-Griffith, DA; Silva, JM; Huang, Z; Laliberté, F; Liu, S; Ethier, D; Pon, D; Muise, E; Boulet, L; Chan, CC; Styhler, A; Charleson, S; Mancini, J; Masson, P; Claveau, D; Nicholson, D; Turner, M; Young, RN; Girard, 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 |
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| More Info.: | Get all data from this article, 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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| BDBM50174021 |
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| n/a |
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| Name | BDBM50174021 |
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| Synonyms: | (Z)-3-(3-(6-(2-cyanopropan-2-yl)quinolin-8-yl)phenyl)-N-isopropyl-2-(4-(methylsulfonyl)phenyl)acrylamide | CHEMBL198853 |
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| Type | Small organic molecule |
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| Emp. Form. | C32H31N3O3S |
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| Mol. Mass. | 537.672 |
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| SMILES | CC(C)NC(=O)C(=C/c1cccc(c1)-c1cc(cc2cccnc12)C(C)(C)C#N)\c1ccc(cc1)S(C)(=O)=O |
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| Structure | 
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