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Target
cAMP-specific 3',5'-cyclic phosphodiesterase 4A
Ligand
BDBM50347343
Substrate
n/a
Meas. Tech.
ChEMBL_755117 (CHEMBL1805697)
IC50
0.51±n/a nM
Citation
 Gallant, M; Aspiotis, R; Day, S; Dias, R; Dubé, D; Dubé, L; Friesen, RW; Girard, M; Guay, D; Hamel, P; Huang, Z; Lacombe, P; Laliberté, S; Lévesque, JF; Liu, S; Macdonald, D; Mancini, J; Nicholson, DW; Styhler, A; Townson, K; Waters, K; Young, RN; Girard, Y Discovery of MK-0952, a selective PDE4 inhibitor for the treatment of long-term memory loss and mild cognitive impairment. Bioorg Med Chem Lett 20:6387-93 (2010) [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:
BDBM50347343
Synonyms:
CHEMBL1801155
Type:
Small organic molecule
Emp. Form.:
C27H20F3N3O4
Mol. Mass.:
507.4606
SMILES:
OC(=O)C1CC1c1ccc(cc1)-c1cccc(c1)-n1cc(C(=O)NCC(F)(F)F)c(=O)c2cccnc12
Structure:
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