Target
cGMP-inhibited 3',5'-cyclic phosphodiesterase 3B [387-1112]
Ligand
BDBM15316
Substrate
BDBM10851
Meas. Tech.
PDE SPA Enzyme Inhibition Assay
IC50
0.61±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 Lett 13:3983-7 (2003) [PubMed]  Article 
Target
Name:
cGMP-inhibited 3',5'-cyclic phosphodiesterase 3B [387-1112]
Synonyms:
CGI-PDE B | CGIP1 | CGIPDE1 | Cyclic GMP-inhibited phosphodiesterase B | PDE3B | PDE3B_HUMAN | Phosphodiesterase Type 3 (PDE3B) | cGMP-inhibited 3',5'-cyclic phosphodiesterase B [387-1112] | cGMP-inhibited 3,5-cyclic phosphodiesterase B
Type:
Enzyme
Mol. Mass.:
81944.98
Organism:
Homo sapiens (Human)
Description:
PDE3B (387-1112) was expressed as soluble proteins in Escherichia coli.
Residue:
726
Sequence:
MGAFSGSCRPKINPLTPFPGFYPCSEIEDPAEKGDRKLNKGLNRNSLPTPQLRRSSGTSGLLPVEQSSRWDRNNGKRPHQEFGISSQGCYLNGPFNSNLLTIPKQRSSSVSLTHHVGLRRAGVLSSLSPVNSSNHGPVSTGSLTNRSPIEFPDTADFLNKPSVILQRSLGNAPNTPDFYQQLRNSDSNLCNSCGHQMLKYVSTSESDGTDCCSGKSGEEENIFSKESFKLMETQQEEETEKKDSRKLFQEGDKWLTEEAQSEQQTNIEQEVSLDLILVEEYDSLIEKMSNWNFPIFELVEKMGEKSGRILSQVMYTLFQDTGLLEIFKIPTQQFMNYFRALENGYRDIPYHNRIHATDVLHAVWYLTTRPVPGLQQIHNGCGTGNETDSDGRINHGRIAYISSKSCSNPDESYGCLSSNIPALELMALYVAAAMHDYDHPGRTNAFLVATNAPQAVLYNDRSVLENHHAASAWNLYLSRPEYNFLLHLDHVEFKRFRFLVIEAILATDLKKHFDFLAEFNAKANDVNSNGIEWSNENDRLLVCQVCIKLADINGPAKVRDLHLKWTEGIVNEFYEQGDEEANLGLPISPFMDRSSPQLAKLQESFITHIVGPLCNSYDAAGLLPGQWLEAEEDNDTESGDDEDGEELDTEDEEMENNLNPKPPRRKSRRRIFCQLMHHLTENHKIWKEIVEEEEKCKADGNKLQVENSSLPQADEIQVIEEADEEE
  
Inhibitor
Name:
BDBM15316
Synonyms:
6-{4-[(2-benzyl-3-oxocyclohex-1-en-1-yl)amino]-3-methylphenyl}-5-methyl-2,3,4,5-tetrahydropyridazin-3-one | dihydropyridazinone 14j
Type:
Small organic molecule
Emp. Form.:
C25H27N3O2
Mol. Mass.:
401.5008
SMILES:
CC1CC(=O)NN=C1c1ccc(NC2=C(Cc3ccccc3)C(=O)CCC2)c(C)c1 |c:6,14|
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
BDBM10851
Synonyms:
(4aR,6R,7R,7aS)-6-(6-amino-9H-purin-9-yl)-2,7-dihydroxy-hexahydro-1,3,5,2-furo[3,2-d][1,3,2]dioxaphosphinin-2-one | (4aR,6R,7R,7aS)-6-(6-amino-9H-purin-9-yl)tetrahydro-4H-furo[3,2-d][1,3,2]dioxaphosphinine-2,7-diol 2-oxide | ADENOSINE-3 ,5 -CYCLIC-MONOPHOSPHATE | Cyclic adenosine monophosphate | cAMP | cid_23902375
Type:
Small organic molecule
Emp. Form.:
C10H12N5O6P
Mol. Mass.:
329.2059
SMILES:
Nc1ncnc2n(cnc12)[C@@H]1O[C@@H]2COP(O)(=O)O[C@H]2[C@H]1O
Structure:
Search PDB for entries with ligand similarity: