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TargetcGMP-inhibited 3',5'-cyclic phosphodiesterase 3A [388-1112]
LigandBDBM15310
Substrate/CompetitorBDBM10851
Meas. Tech.PDE SPA Enzyme Inhibition Assay
IC50 0.11±n/a nM
Citation Edmondson, SDMastracchio, AHe, JChung, CCForrest, MJHofsess, SMacIntyre, EMetzger, JO'Connor, NPatel, KTong, XTota, MRVan der Ploeg, LHVarnerin, JPFisher, MHWyvratt, MJWeber, AEParmee, ER Benzyl vinylogous amide substituted aryldihydropyridazinones and aryldimethylpyrazolones as potent and selective PDE3B inhibitors. Bioorg Med Chem Lett13:3983-7 (2003) [PubMed]  Article
More Info.:Get all data from this article,   Solution Info,  Assay Method
 
cGMP-inhibited 3',5'-cyclic phosphodiesterase 3A [388-1112]
Name:cGMP-inhibited 3',5'-cyclic phosphodiesterase 3A [388-1112]
Synonyms:CGI-PDE A | Cyclic GMP-inhibited phosphodiesterase A | PDE3A | PDE3A_HUMAN | Phosphodiesterase Type 3 (PDE3A) | cGMP-inhibited 3',5'-cyclic phosphodiesterase A [388-1112] | cGMP-inhibited 3,5-cyclic phosphodiesterase A
Type:Enzyme
Mol. Mass.:80817.39
Organism:Homo sapiens (Human)
Description:PDE3A (388-1112) was expressed as soluble proteins in Escherichia coli.
Residue:725
Sequence:
QAIHKPRVNPVTSLSENYTCSDSEESSEKDKLAIPKRLRRSLPPGLLRRVSSTWTTTTSA
TGLPTLEPAPVRRDRSTSIKLQEAPSSSPDSWNNPVMMTLTKSRSFTSSYAISAANHVKA
KKQSRPGALAKISPLSSPCSSPLQGTPASSLVSKISAVQFPESADTTAKQSLGSHRALTY
TQSAPDLSPQILTPPVICSSCGRPYSQGNPADEPLERSGVATRTPSRTDDTAQVTSDYET
NNNSDSSDIVQNEDETECLREPLRKASACSTYAPETMMFLDKPILAPEPLVMDNLDSIME
QLNTWNFPIFDLVENIGRKCGRILSQVSYRLFEDMGLFEAFKIPIREFMNYFHALEIGYR
DIPYHNRIHATDVLHAVWYLTTQPIPGLSTVINDHGSTSDSDSDSGFTHGHMGYVFSKTY
NVTDDKYGCLSGNIPALELMALYVAAAMHDYDHPGRTNAFLVATSAPQAVLYNDRSVLEN
HHAAAAWNLFMSRPEYNFLINLDHVEFKHFRFLVIEAILATDLKKHFDFVAKFNGKVNDD
VGIDWTNENDRLLVCQMCIKLADINGPAKCKELHLQWTDGIVNEFYEQGDEEASLGLPIS
PFMDRSAPQLANLQESFISHIVGPLCNSYDSAGLMPGKWVEDSDESGDTDDPEEEEEEAP
APNEEETCENNESPKKKTFKRRKIYCQITQHLLQNHKMWKKVIEEEQRLAGIENQSLDQT
PQSHS
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BDBM15310
BDBM10851
NameBDBM15310
Synonyms:(5R)-5-methyl-6-{4-[(3-oxo-2-{[3-(thiophen-3-yl)phenyl]methyl}cyclohex-1-en-1-yl)amino]phenyl}-2,3,4,5-tetrahydropyridazin-3-one | dihydropyridazinone 9a
TypeSmall organic molecule
Emp. Form.C28H27N3O2S
Mol. Mass.469.598
SMILESC[C@@H]1CC(=O)NN=C1c1ccc(NC2=C(Cc3cccc(c3)-c3ccsc3)C(=O)CCC2)cc1 |r,c:6,14|
Structure
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