Reaction Details |
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Target | cGMP-inhibited 3',5'-cyclic phosphodiesterase 3A [388-1112] |
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Ligand | BDBM15310 |
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Substrate/Competitor | BDBM10851 |
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Meas. Tech. | PDE SPA Enzyme Inhibition Assay |
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IC50 | 0.11±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 3A [388-1112] |
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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 |
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BDBM10851 |
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Name | BDBM15310 |
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 |
Type | Small organic molecule |
Emp. Form. | C28H27N3O2S |
Mol. Mass. | 469.598 |
SMILES | C[C@@H]1CC(=O)NN=C1c1ccc(NC2=C(Cc3cccc(c3)-c3ccsc3)C(=O)CCC2)cc1 |r,c:6,14| |
Structure |
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