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Target
cGMP-inhibited 3',5'-cyclic phosphodiesterase 3B [387-1112]
Ligand
BDBM15334
Substrate
BDBM10851
Meas. Tech.
PDE SPA Enzyme Inhibition Assay
IC50
6.3±n/a nM
Citation
Edmondson, SD; Mastracchio, A; He, J; Chung, CC; Forrest, MJ; Hofsess, S; MacIntyre, E; Metzger, J; O'Connor, N; Patel, K; Tong, X; Tota, MR; Van der Ploeg, LH; Varnerin, JP; Fisher, MH; Wyvratt, MJ; Weber, AE; Parmee, ER Benzyl vinylogous amide substituted aryldihydropyridazinones and aryldimethylpyrazolones as potent and selective PDE3B inhibitors. Bioorg Med Chem Lett 13:3983-7 (2003) [PubMed] Article
More Info.:
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:
BDBM15334
Synonyms:
3-[2-chloro-4-({2-[(2-chlorophenyl)methyl]-3-oxocyclohex-1-en-1-yl}amino)phenyl]-4,4-dimethyl-4,5-dihydro-1H-pyrazol-5-one | Aryldimethylpyrazolone 18m
Type:
Small organic molecule
Emp. Form.:
C24H23Cl2N3O2
Mol. Mass.:
456.364
SMILES:
CC1(C)C(=O)NN=C1c1ccc(NC2=C(Cc3ccccc3Cl)C(=O)CCC2)cc1Cl |c:6,14|
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