Reaction Details |
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Target | cAMP-specific 3',5'-cyclic phosphodiesterase 4B |
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Ligand | BDBM50174020 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_326770 (CHEMBL860120) |
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IC50 | 0.4±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 4B |
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Name: | cAMP-specific 3',5'-cyclic phosphodiesterase 4B |
Synonyms: | 3',5'-cyclic phosphodiesterase | DPDE4 | Isoform PDE4B1 | PDE32 | PDE4B | PDE4B1 | PDE4B_HUMAN | Phosphodiesterase 4B | Phosphodiesterase 4B (PDE4B) | Phosphodiesterase 4B (PDE4B1) | Phosphodiesterase Type 4 (PDE4B) |
Type: | Protein |
Mol. Mass.: | 83318.87 |
Organism: | Homo sapiens (Human) |
Description: | Q07343 |
Residue: | 736 |
Sequence: | MKKSRSVMTVMADDNVKDYFECSLSKSYSSSSNTLGIDLWRGRRCCSGNLQLPPLSQRQS
ERARTPEGDGISRPTTLPLTTLPSIAITTVSQECFDVENGPSPGRSPLDPQASSSAGLVL
HATFPGHSQRRESFLYRSDSDYDLSPKAMSRNSSLPSEQHGDDLIVTPFAQVLASLRSVR
NNFTILTNLHGTSNKRSPAASQPPVSRVNPQEESYQKLAMETLEELDWCLDQLETIQTYR
SVSEMASNKFKRMLNRELTHLSEMSRSGNQVSEYISNTFLDKQNDVEIPSPTQKDREKKK
KQQLMTQISGVKKLMHSSSLNNTSISRFGVNTENEDHLAKELEDLNKWGLNIFNVAGYSH
NRPLTCIMYAIFQERDLLKTFRISSDTFITYMMTLEDHYHSDVAYHNSLHAADVAQSTHV
LLSTPALDAVFTDLEILAAIFAAAIHDVDHPGVSNQFLINTNSELALMYNDESVLENHHL
AVGFKLLQEEHCDIFMNLTKKQRQTLRKMVIDMVLATDMSKHMSLLADLKTMVETKKVTS
SGVLLLDNYTDRIQVLRNMVHCADLSNPTKSLELYRQWTDRIMEEFFQQGDKERERGMEI
SPMCDKHTASVEKSQVGFIDYIVHPLWETWADLVQPDAQDILDTLEDNRNWYQSMIPQSP
SPPLDEQNRDCQGLMEKFQFELTLDEEDSEGPEKEGEGHSYFSSTKTLCVIDPENRDSLG
ETDIDIATEDKSPVDT
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BDBM50174020 |
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n/a |
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Name | BDBM50174020 |
Synonyms: | (S)-(+)-3-{2-[(3-Cyclopropyloxy-4-difluromethoxy)-phenyl]-2-[5-(2-(1-hydroxy-1-trifluoromethyl-2,2,2-trifluoro)ethyl)-thiazolyl]ethyl}pyridine N-Oxide | 2-{5-[(S)-1-(3-cyclopropoxy-4-difluoromethoxy-phenyl)-2-(1-oxy-pyridin-3-yl)-ethyl]-thiazol-2-yl}-1,1,1,3,3,3-hexafluoro-propan-2-ol | CHEMBL199015 | L-869298 |
Type | Small organic molecule |
Emp. Form. | C23H18F8N2O4S |
Mol. Mass. | 570.452 |
SMILES | OC(c1ncc(s1)[C@@H](Cc1ccc[n+]([O-])c1)c1ccc(OC(F)F)c(OC2CC2)c1)(C(F)(F)F)C(F)(F)F |
Structure |
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