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Target
cAMP-specific 3',5'-cyclic phosphodiesterase 4A
Ligand
BDBM50308557
Substrate
n/a
Meas. Tech.
ChEMBL_613560 (CHEMBL1074186)
IC50
>2000±n/a nM
Citation
 Hughes, RO; Rogier, DJ; Jacobsen, EJ; Walker, JK; Macinnes, A; Bond, BR; Zhang, LL; Yu, Y; Zheng, Y; Rumsey, JM; Walgren, JL; Curtiss, SW; Fobian, YM; Heasley, SE; Cubbage, JW; Moon, JB; Brown, DL; Acker, BA; Maddux, TM; Tollefson, MB; Mischke, BV; Owen, DR; Freskos, JN; Molyneaux, JM; Benson, AG; Blevis-Bal, RM Design, synthesis, and biological evaluation of 3-[4-(2-hydroxyethyl)piperazin-1-yl]-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)pyrido[3,4-b]pyrazin-2(1H)-one, a potent, orally active, brain penetrant inhibitor of phosphodiesterase 5 (PDE5). J Med Chem 53:2656-60 (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:
BDBM50308557
Synonyms:
3-(4-(2-hydroxyethyl)piperazin-1-yl)-1-(2-propoxyethyl)-7-(6-methoxypyridin-3-yl)pyrido[3,4-b]pyrazin-2(1H)-one | CHEMBL591501
Type:
Small organic molecule
Emp. Form.:
C24H32N6O4
Mol. Mass.:
468.5487
SMILES:
CCCOCCn1c2cc(ncc2nc(N2CCN(CCO)CC2)c1=O)-c1ccc(OC)nc1
Structure:
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