| Reaction Details |
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 | Report a problem with these data |
| Target | High affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8A |
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| Ligand | BDBM50246909 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_1677117 (CHEMBL4027260) |
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| IC50 | 3560±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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| High affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8A |
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| Name: | High affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8A |
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| Synonyms: | High-affinity cAMP-specific and IBMX-insensitive 3 ,5 -cyclic phosphodiesterase 8A | PDE8A | PDE8A_HUMAN | Phosphodiesterase 8 | Phosphodiesterase 8 (PDE8) | Phosphodiesterase 8A (PDE8A) | Phosphodiesterase 8A (PDE8A1) | Phosphodiesterase 8A1 | Phosphodiesterase Type 8 (PDE8A) |
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| Type: | Enzyme Catalytic Domain |
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| Mol. Mass.: | 93295.89 |
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| Organism: | Homo sapiens (Human) |
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| Description: | Recombinant catalytic domain (M1-E829) of human PDE8A. |
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| Residue: | 829 |
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| Sequence: | MGCAPSIHISERLVAEDAPSPAAPPLSSGGPRLPQGQKTAALPRTRGAGLLESELRDGSG
KKVAVADVQFGPMRFHQDQLQVLLVFTKEDNQCNGFCRACEKAGFKCTVTKEAQAVLACF
LDKHHDIIIIDHRNPRQLDAEALCRSIRSSKLSENTVIVGVVRRVDREELSVMPFISAGF
TRRYVENPNIMACYNELLQLEFGEVRSQLKLRACNSVFTALENSEDAIEITSEDRFIQYA
NPAFETTMGYQSGELIGKELGEVPINEKKADLLDTINSCIRIGKEWQGIYYAKKKNGDNI
QQNVKIIPVIGQGGKIRHYVSIIRVCNGNNKAEKISECVQSDTHTDNQTGKHKDRRKGSL
DVKAVASRATEVSSQRRHSSMARIHSMTIEAPITKVINIINAAQESSPMPVTEALDRVLE
ILRTTELYSPQFGAKDDDPHANDLVGGLMSDGLRRLSGNEYVLSTKNTQMVSSNIITPIS
LDDVPPRIARAMENEEYWDFDIFELEAATHNRPLIYLGLKMFARFGICEFLHCSESTLRS
WLQIIEANYHSSNPYHNSTHSADVLHATAYFLSKERIKETLDPIDEVAALIAATIHDVDH
PGRTNSFLCNAGSELAILYNDTAVLESHHAALAFQLTTGDDKCNIFKNMERNDYRTLRQG
IIDMVLATEMTKHFEHVNKFVNSINKPLATLEENGETDKNQEVINTMLRTPENRTLIKRM
LIKCADVSNPCRPLQYCIEWAARISEEYFSQTDEEKQQGLPVVMPVFDRNTCSIPKSQIS
FIDYFITDMFDAWDAFVDLPDLMQHLDNNFKYWKGLDEMKLRNLRPPPE
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| BDBM50246909 |
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| n/a |
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| Name | BDBM50246909 |
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| Synonyms: | CHEMBL4075951 |
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| Type | Small organic molecule |
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| Emp. Form. | C31H31Cl2F2N3O8S2 |
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| Mol. Mass. | 746.626 |
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| 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| |
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| Structure | 
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