Reaction Details Report a problem with these data
Target
cAMP-specific 3',5'-cyclic phosphodiesterase 4A
Ligand
BDBM50232731
Substrate
n/a
Meas. Tech.
ChEMBL_755117 (CHEMBL1805697)
IC50
0.540±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
More Info.:
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:
BDBM50232731
Synonyms:
2-{3'-[6-(1-methanesulfonyl-1-methyl-ethyl)-quinolin-8-yl]-biphenyl-4-yl}-cyclopropanecarboxylic acid | CHEMBL253083
Type:
Small organic molecule
Emp. Form.:
C29H27NO4S
Mol. Mass.:
485.594
SMILES:
CC(C)(c1cc(-c2cccc(c2)-c2ccc(cc2)C2CC2C(O)=O)c2ncccc2c1)S(C)(=O)=O |w:18.19,20.23|