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Target
cGMP-specific 3',5'-cyclic phosphodiesterase
Ligand
BDBM50297797
Substrate
n/a
Meas. Tech.
ChEMBL_584078 (CHEMBL1058319)
IC50
0.400000±n/a nM
Citation
 Owen, DR; Walker, JK; Jon Jacobsen, E; Freskos, JN; Hughes, RO; Brown, DL; Bell, AS; Brown, DG; Phillips, C; Mischke, BV; Molyneaux, JM; Fobian, YM; Heasley, SE; Moon, JB; Stallings, WC; Joseph Rogier, D; Fox, DN; Palmer, MJ; Ringer, T; Rodriquez-Lens, M; Cubbage, JW; Blevis-Bal, RM; Benson, AG; Acker, BA; Maddux, TM; Tollefson, MB; Bond, BR; Macinnes, A; Yu, Y Identification, synthesis and SAR of amino substituted pyrido[3,2b]pyrazinones as potent and selective PDE5 inhibitors. Bioorg Med Chem Lett 19:4088-91 (2009) [PubMed]  Article 
Target
Name:
cGMP-specific 3',5'-cyclic phosphodiesterase
Synonyms:
3',5'-cyclic phosphodiesterase | CGB-PDE | PDE5 | PDE5A | PDE5A_HUMAN | Phosphodiesterase 2 and 5 (PDE2 and PDE5) | Phosphodiesterase 5 (PDE5) | Phosphodiesterase 5A | Phosphodiesterase 5A (PDE5A) | cGMP-binding cGMP-specific phosphodiesterase | cGMP-specific 3',5'-cyclic phosphodiesterase
Type:
Protein
Mol. Mass.:
99975.83
Organism:
Homo sapiens (Human)
Description:
O76074
Residue:
875
Sequence:
MERAGPSFGQQRQQQQPQQQKQQQRDQDSVEAWLDDHWDFTFSYFVRKATREMVNAWFAERVHTIPVCKEGIRGHTESCSCPLQQSPRADNSAPGTPTRKISASEFDRPLRPIVVKDSEGTVSFLSDSEKKEQMPLTPPRFDHDEGDQCSRLLELVKDISSHLDVTALCHKIFLHIHGLISADRYSLFLVCEDSSNDKFLISRLFDVAEGSTLEEVSNNCIRLEWNKGIVGHVAALGEPLNIKDAYEDPRFNAEVDQITGYKTQSILCMPIKNHREEVVGVAQAINKKSGNGGTFTEKDEKDFAAYLAFCGIVLHNAQLYETSLLENKRNQVLLDLASLIFEEQQSLEVILKKIAATIISFMQVQKCTIFIVDEDCSDSFSSVFHMECEELEKSSDTLTREHDANKINYMYAQYVKNTMEPLNIPDVSKDKRFPWTTENTGNVNQQCIRSLLCTPIKNGKKNKVIGVCQLVNKMEENTGKVKPFNRNDEQFLEAFVIFCGLGIQNTQMYEAVERAMAKQMVTLEVLSYHASAAEEETRELQSLAAAVVPSAQTLKITDFSFSDFELSDLETALCTIRMFTDLNLVQNFQMKHEVLCRWILSVKKNYRKNVAYHNWRHAFNTAQCMFAALKAGKIQNKLTDLEILALLIAALSHDLDHRGVNNSYIQRSEHPLAQLYCHSIMEHHHFDQCLMILNSPGNQILSGLSIEEYKTTLKIIKQAILATDLALYIKRRGEFFELIRKNQFNLEDPHQKELFLAMLMTACDLSAITKPWPIQQRIAELVATEFFDQGDRERKELNIEPTDLMNREKKNKIPSMQVGFIDAICLQLYEALTHVSEDCFPLLDGCRKNRQKWQALAEQQEKMLINGESGQAKRN
  
Inhibitor
Name:
BDBM50297797
Synonyms:
4-(cyclohexylmethyl)-6-(6-methoxypyridin-3-yl)-2-(2-morpholinoethylamino)pyrido[2,3-b]pyrazin-3(4H)-one | CHEMBL560408
Type:
Small organic molecule
Emp. Form.:
C26H34N6O3
Mol. Mass.:
478.5866
SMILES:
COc1ccc(cn1)-c1ccc2nc(NCCN3CCOCC3)c(=O)n(CC3CCCCC3)c2n1
Structure:
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