Reaction Details |
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Target | High affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8A |
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Ligand | BDBM50319163 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_635691 (CHEMBL1120089) |
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IC50 | >1000±n/a nM |
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Citation | Höfgen, N; Stange, H; Schindler, R; Lankau, HJ; Grunwald, C; Langen, B; Egerland, U; Tremmel, P; Pangalos, MN; Marquis, KL; Hage, T; Harrison, BL; Malamas, MS; Brandon, NJ; Kronbach, T Discovery of imidazo[1,5-a]pyrido[3,2-e]pyrazines as a new class of phosphodiesterase 10A inhibitiors. J Med Chem53:4399-411 (2010) [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 |
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) |
Type: | Enzyme Catalytic Domain |
Mol. Mass.: | 93295.89 |
Organism: | Homo sapiens (Human) |
Description: | Recombinant catalytic domain (M1-E829) of human PDE8A. |
Residue: | 829 |
Sequence: | MGCAPSIHISERLVAEDAPSPAAPPLSSGGPRLPQGQKTAALPRTRGAGLLESELRDGSG
KKVAVADVQFGPMRFHQDQLQVLLVFTKEDNQCNGFCRACEKAGFKCTVTKEAQAVLACF
LDKHHDIIIIDHRNPRQLDAEALCRSIRSSKLSENTVIVGVVRRVDREELSVMPFISAGF
TRRYVENPNIMACYNELLQLEFGEVRSQLKLRACNSVFTALENSEDAIEITSEDRFIQYA
NPAFETTMGYQSGELIGKELGEVPINEKKADLLDTINSCIRIGKEWQGIYYAKKKNGDNI
QQNVKIIPVIGQGGKIRHYVSIIRVCNGNNKAEKISECVQSDTHTDNQTGKHKDRRKGSL
DVKAVASRATEVSSQRRHSSMARIHSMTIEAPITKVINIINAAQESSPMPVTEALDRVLE
ILRTTELYSPQFGAKDDDPHANDLVGGLMSDGLRRLSGNEYVLSTKNTQMVSSNIITPIS
LDDVPPRIARAMENEEYWDFDIFELEAATHNRPLIYLGLKMFARFGICEFLHCSESTLRS
WLQIIEANYHSSNPYHNSTHSADVLHATAYFLSKERIKETLDPIDEVAALIAATIHDVDH
PGRTNSFLCNAGSELAILYNDTAVLESHHAALAFQLTTGDDKCNIFKNMERNDYRTLRQG
IIDMVLATEMTKHFEHVNKFVNSINKPLATLEENGETDKNQEVINTMLRTPENRTLIKRM
LIKCADVSNPCRPLQYCIEWAARISEEYFSQTDEEKQQGLPVVMPVFDRNTCSIPKSQIS
FIDYFITDMFDAWDAFVDLPDLMQHLDNNFKYWKGLDEMKLRNLRPPPE
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BDBM50319163 |
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n/a |
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Name | BDBM50319163 |
Synonyms: | 8-Methoxy-3-methyl-4-methylsulfonylamino-1-propyl-imidazo[1,5-a]pyrido[3,2-e]pyrazine | CHEMBL1085374 |
Type | Small organic molecule |
Emp. Form. | C15H19N5O3S |
Mol. Mass. | 349.408 |
SMILES | CCCc1nc(C)c2c(NS(C)(=O)=O)nc3ccc(OC)nc3n12 |
Structure |
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