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Target
cAMP-specific 3',5'-cyclic phosphodiesterase 4C
Ligand
BDBM50174025
Substrate
n/a
Meas. Tech.
ChEMBL_326771 (CHEMBL860121)
IC50
0.7±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 4C
Synonyms:
3',5'-cyclic phosphodiesterase | DPDE1 | NP_000914.2 | PDE21 | PDE4C | PDE4C1
Type:
Enzyme Catalytic Domain
Mol. Mass.:
79875.54
Organism:
Homo sapiens (Human)
Description:
Q08493
Residue:
712
Sequence:
MENLGVGEGAEACSRLSRSRGRHSMTRAPKHLWRQPRRPIRIQQRFYSDPDKSAGCRERDLSPRPELRKSRLSWPVSSCRRFDLENGLSCGRRALDPQSSPGLGRIMQAPVPHSQRRESFLYRSDSDYELSPKAMSRNSSVASDLHGEDMIVTPFAQVLASLRTVRSNVAALARQQCLGAAKQGPVGNPSSSNQLPPAEDTGQKLALETLDELDWCLDQLETLQTRHSVGEMASNKFKRILNRELTHLSETSRSGNQVSEYISRTFLDQQTEVELPKVTAEEAPQPMSRISGLHGLCHSASLSSATVPRFGVQTDQEEQLAKELEDTNKWGLDVFKVAELSGNRPLTAIIFSIFQERDLLKTFQIPADTLATYLLMLEGHYHANVAYHNSLHAADVAQSTHVLLATPALEAVFTDLEILAALFASAIHDVDHPGVSNQFLINTNSELALMYNDASVLENHHLAVGFKLLQAENCDIFQNLSAKQRLSLRRMVIDMVLATDMSKHMNLLADLKTMVETKKVTSLGVLLLDNYSDRIQVLQNLVHCADLSNPTKPLPLYRQWTDRIMAEFFQQGDRERESGLDISPMCDKHTASVEKSQVGFIDYIAHPLWETWADLVHPDAQDLLDTLEDNREWYQSKIPRSPSDLTNPERDGPDRFQFELTLEEAEEEDEEEEEEGEETALAKEALELPDTELLSPEAGPDPGDLPLDNQRT
  
Inhibitor
Name:
BDBM50174025
Synonyms:
6-isopropyl-8-(3-(2-(4-(methylsulfonyl)phenyl)-2-(thiazol-2-yl)vinyl)phenyl)quinoline | CHEMBL196969
Type:
Small organic molecule
Emp. Form.:
C30H26N2O2S2
Mol. Mass.:
510.67
SMILES:
CC(C)c1cc(-c2cccc(\C=C(\c3nccs3)c3ccc(cc3)S(C)(=O)=O)c2)c2ncccc2c1
Structure:
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