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TargetHigh affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8A
LigandBDBM50259108
Substrate/Competitorn/a
Meas. Tech.ChEMBL_500741 (CHEMBL970520)
IC50>10000±n/a nM
Citation Deninno, MPAndrews, MBell, ASChen, YEller-Zarbo, CEshelby, NEtienne, JBMoore, DEPalmer, MJVisser, MSYu, LJZavadoski, WJMichael Gibbs, E The discovery of potent, selective, and orally bioavailable PDE9 inhibitors as potential hypoglycemic agents. Bioorg Med Chem Lett19:2537-41 (2009) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
High affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8A
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
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM50259108
n/a
NameBDBM50259108
Synonyms:(-)3-Isopropyl-5-{[(trans)-2-(pyrimidin-2-ylamino)cyclohexyl]methyl}-1,6-dihydro-7H-pyrazolo[4,3-d]pyrimidin-7-one | CHEMBL466481
TypeSmall organic molecule
Emp. Form.C19H25N7O
Mol. Mass.367.4481
SMILESCC(C)c1[nH]nc2c1nc(C[C@@H]1CCCC[C@H]1Nc1ncccn1)[nH]c2=O |r|
Structure
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