Target
cAMP-specific 3',5'-cyclic phosphodiesterase 4A
Ligand
BDBM50183803
Substrate
n/a
Meas. Tech.
ChEMBL_353740 (CHEMBL866234)
IC50
0.3±n/a nM
Citation
 Lacombe, PDeschênes, DDubé, DDubé, LGallant, MMacdonald, DMastracchio, APerrier, HCharleson, SHuang, ZLaliberté, FLiu, SMancini, JAMasson, PSalem, MStyhler, AGirard, Y Nitrogen-bridged substituted 8-arylquinolines as potent PDE IV inhibitors. Bioorg Med Chem Lett 16:2608-12 (2006) [PubMed]  Article 
Target
Name:
cAMP-specific 3',5'-cyclic phosphodiesterase 4A
Synonyms:
3',5'-cyclic phosphodiesterase | DPDE2 | PDE46 | PDE4A | PDE4A_HUMAN | Phosphodiesterase 4 (PDE4) | Phosphodiesterase 4A | Phosphodiesterase 4A (PDE4)
Type:
Enzyme
Mol. Mass.:
98113.27
Organism:
Homo sapiens (Human)
Description:
P27815
Residue:
886
Sequence:
MEPPTVPSERSLSLSLPGPREGQATLKPPPQHLWRQPRTPIRIQQRGYSDSAERAERERQPHRPIERADAMDTSDRPGLRTTRMSWPSSFHGTGTGSGGAGGGSSRRFEAENGPTPSPGRSPLDSQASPGLVLHAGAATSQRRESFLYRSDSDYDMSPKTMSRNSSVTSEAHAEDLIVTPFAQVLASLRSVRSNFSLLTNVPVPSNKRSPLGGPTPVCKATLSEETCQQLARETLEELDWCLEQLETMQTYRSVSEMASHKFKRMLNRELTHLSEMSRSGNQVSEYISTTFLDKQNEVEIPSPTMKEREKQQAPRPRPSQPPPPPVPHLQPMSQITGLKKLMHSNSLNNSNIPRFGVKTDQEELLAQELENLNKWGLNIFCVSDYAGGRSLTCIMYMIFQERDLLKKFRIPVDTMVTYMLTLEDHYHADVAYHNSLHAADVLQSTHVLLATPALDAVFTDLEILAALFAAAIHDVDHPGVSNQFLINTNSELALMYNDESVLENHHLAVGFKLLQEDNCDIFQNLSKRQRQSLRKMVIDMVLATDMSKHMTLLADLKTMVETKKVTSSGVLLLDNYSDRIQVLRNMVHCADLSNPTKPLELYRQWTDRIMAEFFQQGDRERERGMEISPMCDKHTASVEKSQVGFIDYIVHPLWETWADLVHPDAQEILDTLEDNRDWYYSAIRQSPSPPPEEESRGPGHPPLPDKFQFELTLEEEEEEEISMAQIPCTAQEALTAQGLSGVEEALDATIAWEASPAQESLEVMAQEASLEAELEAVYLTQQAQSTGSAPVAPDEFSSREEFVVAVSHSSPSALALQSPLLPAWRTLSVSEHAPGLPGLPSTAAEVEAQREHQAAKRACSACAGTFGEDTSALPAPGGGGSGGDPT
  
Inhibitor
Name:
BDBM50183803
Synonyms:
CHEMBL206968 | N-((3-(6-(2-cyanopropan-2-yl)quinolin-8-yl)phenyl)methyl)-5-methyl-N-(4-(methylsulfonyl)phenyl)isoxazole-3-carboxamide
Type:
Small organic molecule
Emp. Form.:
C32H28N4O4S
Mol. Mass.:
564.654
SMILES:
Cc1cc(no1)C(=O)N(Cc1cccc(c1)-c1cc(cc2cccnc12)C(C)(C)C#N)c1ccc(cc1)S(C)(=O)=O
Structure:
Search PDB for entries with ligand similarity: