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Target
cAMP-specific 3',5'-cyclic phosphodiesterase 4A
Ligand
BDBM50128690
Substrate
n/a
Meas. Tech.
ChEMBL_70496 (CHEMBL677056)
IC50
38±n/a nM
Citation
 Friesen, RW; Ducharme, Y; Ball, RG; Blouin, M; Boulet, L; Côté, B; Frenette, R; Girard, M; Guay, D; Huang, Z; Jones, TR; Laliberté, F; Lynch, JJ; Mancini, J; Martins, E; Masson, P; Muise, E; Pon, DJ; Siegl, PK; Styhler, A; Tsou, NN; Turner, MJ; Young, RN; Girard, Y Optimization of a tertiary alcohol series of phosphodiesterase-4 (PDE4) inhibitors: structure-activity relationship related to PDE4 inhibition and human ether-a-go-go related gene potassium channel binding affinity. J Med Chem 46:2413-26 (2003) [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:
BDBM50128690
Synonyms:
4-Hydroxy-7-{2-[2-(3-phenethyloxy-propane-1-sulfonyl)-ethylamino]-ethyl}-3H-benzothiazol-2-one | CHEMBL82663 | SB-07499
Type:
Small organic molecule
Emp. Form.:
C22H28N2O5S2
Mol. Mass.:
464.598
SMILES:
Oc1ccc(CCNCCS(=O)(=O)CCCOCCc2ccccc2)c2sc(=O)[nH]c12
Structure:
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