Reaction Details |
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Target | cGMP-dependent 3',5'-cyclic phosphodiesterase |
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Ligand | BDBM50246909 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1677111 (CHEMBL4027254) |
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IC50 | >30000±n/a nM |
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Citation | Carzaniga, L; Amari, G; Rizzi, A; Capaldi, C; De Fanti, R; Ghidini, E; Villetti, G; Carnini, C; Moretto, N; Facchinetti, F; Caruso, P; Marchini, G; Battipaglia, L; Patacchini, R; Cenacchi, V; Volta, R; Amadei, F; Pappani, A; Capacchi, S; Bagnacani, V; Delcanale, M; Puccini, P; Catinella, S; Civelli, M; Armani, E Discovery and Optimization of Thiazolidinyl and Pyrrolidinyl Derivatives as Inhaled PDE4 Inhibitors for Respiratory Diseases. J Med Chem60:10026-10046 (2017) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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cGMP-dependent 3',5'-cyclic phosphodiesterase |
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Name: | cGMP-dependent 3',5'-cyclic phosphodiesterase |
Synonyms: | CGS-PDE | Cyclic GMP-stimulated phosphodiesterase | Homo sapiens phosphodiesterase 2A (PDE2A) | NM_002599 | PDE2A | PDE2A_HUMAN | cGSPDE |
Type: | Enzyme Catalytic Domain |
Mol. Mass.: | 105691.58 |
Organism: | Homo sapiens (Human) |
Description: | O00408 |
Residue: | 941 |
Sequence: | MGQACGHSILCRSQQYPAARPAEPRGQQVFLKPDEPPPPPQPCADSLQDALLSLGSVIDI
SGLQRAVKEALSAVLPRVETVYTYLLDGESQLVCEDPPHELPQEGKVREAIISQKRLGCN
GLGFSDLPGKPLARLVAPLAPDTQVLVMPLADKEAGAVAAVILVHCGQLSDNEEWSLQAV
EKHTLVALRRVQVLQQRGPREAPRAVQNPPEGTAEDQKGGAAYTDRDRKILQLCGELYDL
DASSLQLKVLQYLQQETRASRCCLLLVSEDNLQLSCKVIGDKVLGEEVSFPLTGCLGQVV
EDKKSIQLKDLTSEDVQQLQSMLGCELQAMLCVPVISRATDQVVALACAFNKLEGDLFTD
EDEHVIQHCFHYTSTVLTSTLAFQKEQKLKCECQALLQVAKNLFTHLDDVSVLLQEIITE
ARNLSNAEICSVFLLDQNELVAKVFDGGVVDDESYEIRIPADQGIAGHVATTGQILNIPD
AYAHPLFYRGVDDSTGFRTRNILCFPIKNENQEVIGVAELVNKINGPWFSKFDEDLATAF
SIYCGISIAHSLLYKKVNEAQYRSHLANEMMMYHMKVSDDEYTKLLHDGIQPVAAIDSNF
ASFTYTPRSLPEDDTSMAILSMLQDMNFINNYKIDCPTLARFCLMVKKGYRDPPYHNWMH
AFSVSHFCYLLYKNLELTNYLEDIEIFALFISCMCHDLDHRGTNNSFQVASKSVLAALYS
SEGSVMERHHFAQAIAILNTHGCNIFDHFSRKDYQRMLDLMRDIILATDLAHHLRIFKDL
QKMAEVGYDRNNKQHHRLLLCLLMTSCDLSDQTKGWKTTRKIAELIYKEFFSQGDLEKAM
GNRPMEMMDREKAYIPELQISFMEHIAMPIYKLLQDLFPKAAELYERVASNREHWTKVSH
KFTIRGLPSNNSLDFLDEEYEVPDLDGTRAPINGCCSLDAE
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BDBM50246909 |
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n/a |
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Name | BDBM50246909 |
Synonyms: | CHEMBL4075951 |
Type | Small organic molecule |
Emp. Form. | C31H31Cl2F2N3O8S2 |
Mol. Mass. | 746.626 |
SMILES | CN(C)C(=O)c1cccc(c1)S(=O)(=O)N1CCS[C@H]1C(=O)O[C@@H](Cc1c(Cl)c[n+]([O-])cc1Cl)c1ccc(OC(F)F)c(OCC2CC2)c1 |r| |
Structure |
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