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Target
cAMP-specific 3',5'-cyclic phosphodiesterase 4D
Ligand
BDBM50174017
Substrate
n/a
Meas. Tech.
ChEMBL_326772 (CHEMBL860122)
IC50
2.5±n/a nM
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 Lett 15:5241-6 (2005) [PubMed]  Article 
Target
Name:
cAMP-specific 3',5'-cyclic phosphodiesterase 4D
Synonyms:
3',5'-cyclic phosphodiesterase | DPDE3 | PDE43 | PDE4D | PDE4D_HUMAN | Phosphodiesterase 4D
Type:
Protein
Mol. Mass.:
91092.69
Organism:
Homo sapiens (Human)
Description:
Q08499
Residue:
809
Sequence:
MEAEGSSAPARAGSGEGSDSAGGATLKAPKHLWRHEQHHQYPLRQPQFRLLHPHHHLPPPPPPSPQPQPQCPLQPPPPPPLPPPPPPPGAARGRYASSGATGRVRHRGYSDTERYLYCRAMDRTSYAVETGHRPGLKKSRMSWPSSFQGLRRFDVDNGTSAGRSPLDPMTSPGSGLILQANFVHSQRRESFLYRSDSDYDLSPKSMSRNSSIASDIHGDDLIVTPFAQVLASLRTVRNNFAALTNLQDRAPSKRSPMCNQPSINKATITEEAYQKLASETLEELDWCLDQLETLQTRHSVSEMASNKFKRMLNRELTHLSEMSRSGNQVSEFISNTFLDKQHEVEIPSPTQKEKEKKKRPMSQISGVKKLMHSSSLTNSSIPRFGVKTEQEDVLAKELEDVNKWGLHVFRIAELSGNRPLTVIMHTIFQERDLLKTFKIPVDTLITYLMTLEDHYHADVAYHNNIHAADVVQSTHVLLSTPALEAVFTDLEILAAIFASAIHDVDHPGVSNQFLINTNSELALMYNDSSVLENHHLAVGFKLLQEENCDIFQNLTKKQRQSLRKMVIDIVLATDMSKHMNLLADLKTMVETKKVTSSGVLLLDNYSDRIQVLQNMVHCADLSNPTKPLQLYRQWTDRIMEEFFRQGDRERERGMEISPMCDKHNASVEKSQVGFIDYIVHPLWETWADLVHPDAQDILDTLEDNREWYQSTIPQSPSPAPDDPEEGRQGQTEKFQFELTLEEDGESDTEKDSGSQVEEDTSCSDSKTLCTQDSESTEIPLDEQVEEEAVGEEEESQPEACVIDDRSPDT
  
Inhibitor
Name:
BDBM50174017
Synonyms:
8-(3-(2-(3-methylcyclopenta-1,3-dienyl)-2-(4-(methylsulfonyl)phenyl)vinyl)phenyl)-6-(2-(methylsulfonyl)propan-2-yl)quinoline | 8-(3-methoxyphenyl)-6-(pyridin-4-ylmethyl)quinoline | CHEMBL198432
Type:
Small organic molecule
Emp. Form.:
C22H18N2O
Mol. Mass.:
326.3911
SMILES:
COc1cccc(c1)-c1cc(Cc2ccncc2)cc2cccnc12
Structure:
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