| 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 | BDBM50258898 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEBML_1690782 |
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| IC50 | >10000±n/a nM |
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| Citation |  Mikami, S; Nakamura, S; Ashizawa, T; Nomura, I; Kawasaki, M; Sasaki, S; Oki, H; Kokubo, H; Hoffman, ID; Zou, H; Uchiyama, N; Nakashima, K; Kamiguchi, N; Imada, H; Suzuki, N; Iwashita, H; Taniguchi, T Discovery of Clinical Candidate N-((1S)-1-(3-Fluoro-4-(trifluoromethoxy)phenyl)-2-methoxyethyl)-7-methoxy-2-oxo-2,3-dihydropyrido[2,3-b]pyrazine-4(1H)-carboxamide (TAK-915): A Highly Potent, Selective, and Brain-Penetrating Phosphodiesterase 2A Inhibitor for the Treatment of Cognitive Disorders. J Med Chem60:7677-7702 (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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| BDBM50258898 |
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| n/a |
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| Name | BDBM50258898 |
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| Synonyms: | CHEMBL4064344 |
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| Type | Small organic molecule |
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| Emp. Form. | C18H17F3N4O3 |
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| Mol. Mass. | 394.3478 |
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| SMILES | CCC(NC(=O)N1CC(=O)Nc2cccnc12)c1ccc(OC(F)(F)F)cc1 |
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| Structure | 
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