Reaction Details |
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Target | cAMP-specific 3',5'-cyclic phosphodiesterase 4A |
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Ligand | BDBM50174028 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_326769 (CHEMBL860119) |
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IC50 | 0.2±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 |
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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BDBM50174028 |
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n/a |
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Name | BDBM50174028 |
Synonyms: | (E)-6-isopropyl-8-(3-(2-(5-methylpyridin-2-yl)-2-(4-(methylsulfonyl)phenyl)vinyl)phenyl)quinoline | CHEMBL197392 |
Type | Small organic molecule |
Emp. Form. | C33H30N2O2S |
Mol. Mass. | 518.669 |
SMILES | CC(C)c1cc(-c2cccc(\C=C(/c3ccc(cc3)S(C)(=O)=O)c3ccc(C)cn3)c2)c2ncccc2c1 |
Structure |
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