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Target
cAMP-specific 3',5'-cyclic phosphodiesterase 4B
Ligand
BDBM14359
Substrate
BDBM10851
Meas. Tech.
PDE4 Activity Assay
pH
7.5±n/a
Temperature
295.15±n/a K
IC50
0.4±0.2 nM
Comments
The IC50 values were similar to their apparent Ki values under conditions in which 0.1 uM cAMP was used in comparison with their similar Km values of 2 uM.
Citation
 Huai, Q; Sun, Y; Wang, H; Macdonald, D; Aspiotis, R; Robinson, H; Huang, Z; Ke, H Enantiomer discrimination illustrated by the high resolution crystal structures of type 4 phosphodiesterase. J Med Chem 49:1867-73 (2006) [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:
BDBM14359
Synonyms:
(+)-1 | (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 | 3-[(2S)-2-[3-cyclopropoxy-4-(difluoromethoxy)phenyl]-2-[5-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)-1,3-thiazol-2-yl]ethyl]-1-oxidopyridin-1-ium | L-869298
Type:
Small organic molecule
Emp. Form.:
C23H18F8N2O4S
Mol. Mass.:
570.452
SMILES:
OC(c1cnc(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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Substrate
Name:
BDBM10851
Synonyms:
(4aR,6R,7R,7aS)-6-(6-amino-9H-purin-9-yl)-2,7-dihydroxy-hexahydro-1,3,5,2-furo[3,2-d][1,3,2]dioxaphosphinin-2-one | (4aR,6R,7R,7aS)-6-(6-amino-9H-purin-9-yl)tetrahydro-4H-furo[3,2-d][1,3,2]dioxaphosphinine-2,7-diol 2-oxide | ADENOSINE-3 ,5 -CYCLIC-MONOPHOSPHATE | Cyclic adenosine monophosphate | cAMP | cid_23902375
Type:
Small organic molecule
Emp. Form.:
C10H12N5O6P
Mol. Mass.:
329.2059
SMILES:
Nc1ncnc2n(cnc12)[C@@H]1O[C@@H]2COP(O)(=O)O[C@H]2[C@H]1O
Structure:
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