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Target
cGMP-specific 3',5'-cyclic phosphodiesterase
Ligand
BDBM50296252
Substrate
n/a
Meas. Tech.
ChEMBL_584078 (CHEMBL1058319)
IC50
2.4±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:
BDBM50296252
Synonyms:
6-(6-methoxypyridin-3-yl)-2-(2-morpholinoethylamino)-4-(2-propoxyethyl)pyrido[2,3-b]pyrazin-3(4H)-one | 6-(6-methoxypyridin-3-yl)-2-(2-morpholinoethylamino)-4-(2-propoxyethyl)pyrido[3,2-b]pyrazin-3(4H)-one | 6-(6-methoxypyridin-3-yl)-2-[(2-morpholin-4-ylethyl)amino]-4-(2-propoxyethyl)pyrido[2,3-b]pyrazin-3(4H)-one | CHEMBL564374
Type:
Small organic molecule
Emp. Form.:
C24H32N6O4
Mol. Mass.:
468.5487
SMILES:
CCCOCCn1c2nc(ccc2nc(NCCN2CCOCC2)c1=O)-c1ccc(OC)nc1
Structure:
Search PDB for entries with ligand similarity: