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Target
cAMP-specific 3',5'-cyclic phosphodiesterase 4B
Ligand
BDBM50174029
Substrate
n/a
Meas. Tech.
ChEMBL_326770 (CHEMBL860120)
IC50
0.3±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 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:
MKKSRSVMTVMADDNVKDYFECSLSKSYSSSSNTLGIDLWRGRRCCSGNLQLPPLSQRQSERARTPEGDGISRPTTLPLTTLPSIAITTVSQECFDVENGPSPGRSPLDPQASSSAGLVLHATFPGHSQRRESFLYRSDSDYDLSPKAMSRNSSLPSEQHGDDLIVTPFAQVLASLRSVRNNFTILTNLHGTSNKRSPAASQPPVSRVNPQEESYQKLAMETLEELDWCLDQLETIQTYRSVSEMASNKFKRMLNRELTHLSEMSRSGNQVSEYISNTFLDKQNDVEIPSPTQKDREKKKKQQLMTQISGVKKLMHSSSLNNTSISRFGVNTENEDHLAKELEDLNKWGLNIFNVAGYSHNRPLTCIMYAIFQERDLLKTFRISSDTFITYMMTLEDHYHSDVAYHNSLHAADVAQSTHVLLSTPALDAVFTDLEILAAIFAAAIHDVDHPGVSNQFLINTNSELALMYNDESVLENHHLAVGFKLLQEEHCDIFMNLTKKQRQTLRKMVIDMVLATDMSKHMSLLADLKTMVETKKVTSSGVLLLDNYTDRIQVLRNMVHCADLSNPTKSLELYRQWTDRIMEEFFQQGDKERERGMEISPMCDKHTASVEKSQVGFIDYIVHPLWETWADLVQPDAQDILDTLEDNRNWYQSMIPQSPSPPLDEQNRDCQGLMEKFQFELTLDEEDSEGPEKEGEGHSYFSSTKTLCVIDPENRDSLGETDIDIATEDKSPVDT
  
Inhibitor
Name:
BDBM50174029
Synonyms:
(E)-3-(3-(6-(2-cyanopropan-2-yl)quinolin-8-yl)phenyl)-N-isopropyl-2-(4-(methylsulfonyl)phenyl)acrylamide | CHEMBL371037
Type:
Small organic molecule
Emp. Form.:
C32H31N3O3S
Mol. Mass.:
537.672
SMILES:
CC(C)NC(=O)C(=C\c1cccc(c1)-c1cc(cc2cccnc12)C(C)(C)C#N)\c1ccc(cc1)S(C)(=O)=O
Structure:
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