Reaction Details |
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Target | cGMP-inhibited 3',5'-cyclic phosphodiesterase 3B [387-1112] |
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Ligand | BDBM15318 |
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Substrate/Competitor | BDBM10851 |
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Meas. Tech. | PDE SPA Enzyme Inhibition Assay |
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IC50 | 0.24±n/a nM |
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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 Lett13:3983-7 (2003) [PubMed] Article |
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More Info.: | Get all data from this article, Solution Info, Assay Method |
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cGMP-inhibited 3',5'-cyclic phosphodiesterase 3B [387-1112] |
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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: | MGAFSGSCRPKINPLTPFPGFYPCSEIEDPAEKGDRKLNKGLNRNSLPTPQLRRSSGTSG
LLPVEQSSRWDRNNGKRPHQEFGISSQGCYLNGPFNSNLLTIPKQRSSSVSLTHHVGLRR
AGVLSSLSPVNSSNHGPVSTGSLTNRSPIEFPDTADFLNKPSVILQRSLGNAPNTPDFYQ
QLRNSDSNLCNSCGHQMLKYVSTSESDGTDCCSGKSGEEENIFSKESFKLMETQQEEETE
KKDSRKLFQEGDKWLTEEAQSEQQTNIEQEVSLDLILVEEYDSLIEKMSNWNFPIFELVE
KMGEKSGRILSQVMYTLFQDTGLLEIFKIPTQQFMNYFRALENGYRDIPYHNRIHATDVL
HAVWYLTTRPVPGLQQIHNGCGTGNETDSDGRINHGRIAYISSKSCSNPDESYGCLSSNI
PALELMALYVAAAMHDYDHPGRTNAFLVATNAPQAVLYNDRSVLENHHAASAWNLYLSRP
EYNFLLHLDHVEFKRFRFLVIEAILATDLKKHFDFLAEFNAKANDVNSNGIEWSNENDRL
LVCQVCIKLADINGPAKVRDLHLKWTEGIVNEFYEQGDEEANLGLPISPFMDRSSPQLAK
LQESFITHIVGPLCNSYDAAGLLPGQWLEAEEDNDTESGDDEDGEELDTEDEEMENNLNP
KPPRRKSRRRIFCQLMHHLTENHKIWKEIVEEEEKCKADGNKLQVENSSLPQADEIQVIE
EADEEE
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BDBM15318 |
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BDBM10851 |
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Name | BDBM15318 |
Synonyms: | 6-{4-[(2-benzyl-3-oxocyclohex-1-en-1-yl)amino]-2-fluorophenyl}-5-methyl-2,3,4,5-tetrahydropyridazin-3-one | dihydropyridazinone 14l |
Type | Small organic molecule |
Emp. Form. | C24H24FN3O2 |
Mol. Mass. | 405.4647 |
SMILES | CC1CC(=O)NN=C1c1ccc(NC2=C(Cc3ccccc3)C(=O)CCC2)cc1F |c:6,14| |
Structure |
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