Target
cAMP-specific 3',5'-cyclic phosphodiesterase 4A
Ligand
BDBM50274027
Substrate
n/a
Meas. Tech.
ChEMBL_536739 (CHEMBL984533)
IC50
0.45±n/a nM
Citation
 Guay, DBoulet, LFriesen, RWGirard, MHamel, PHuang, ZLaliberté, FLaliberté, SMancini, JAMuise, EPon, DStyhler, A Optimization and structure-activity relationship of a series of 1-phenyl-1,8-naphthyridin-4-one-3-carboxamides: identification of MK-0873, a potent and effective PDE4 inhibitor. Bioorg Med Chem Lett 18:5554-8 (2008) [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:
BDBM50274027
Synonyms:
1-(4-chlorophenyl)-N-(3,5-dichloropyridin-4-yl)-4-oxo-1,4-dihydro-1,8-naphthyridine-3-carboxamide | CHEMBL456171
Type:
Small organic molecule
Emp. Form.:
C20H11Cl3N4O2
Mol. Mass.:
445.686
SMILES:
Clc1ccc(cc1)-n1cc(C(=O)Nc2c(Cl)cncc2Cl)c(=O)c2cccnc12
Structure:
Search PDB for entries with ligand similarity: