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Target
High affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8A
Ligand
BDBM50150264
Substrate
n/a
Meas. Tech.
ChEMBL_1556450 (CHEMBL3772481)
Ki
8200±n/a nM
Citation
 Li, P; Zheng, H; Zhao, J; Zhang, L; Yao, W; Zhu, H; Beard, JD; Ida, K; Lane, W; Snell, G; Sogabe, S; Heyser, CJ; Snyder, GL; Hendrick, JP; Vanover, KE; Davis, RE; Wennogle, LP Discovery of Potent and Selective Inhibitors of Phosphodiesterase 1 for the Treatment of Cognitive Impairment Associated with Neurodegenerative and Neuropsychiatric Diseases. J Med Chem 59:1149-64 (2016) [PubMed]  Article 
Target
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:
MGCAPSIHISERLVAEDAPSPAAPPLSSGGPRLPQGQKTAALPRTRGAGLLESELRDGSGKKVAVADVQFGPMRFHQDQLQVLLVFTKEDNQCNGFCRACEKAGFKCTVTKEAQAVLACFLDKHHDIIIIDHRNPRQLDAEALCRSIRSSKLSENTVIVGVVRRVDREELSVMPFISAGFTRRYVENPNIMACYNELLQLEFGEVRSQLKLRACNSVFTALENSEDAIEITSEDRFIQYANPAFETTMGYQSGELIGKELGEVPINEKKADLLDTINSCIRIGKEWQGIYYAKKKNGDNIQQNVKIIPVIGQGGKIRHYVSIIRVCNGNNKAEKISECVQSDTHTDNQTGKHKDRRKGSLDVKAVASRATEVSSQRRHSSMARIHSMTIEAPITKVINIINAAQESSPMPVTEALDRVLEILRTTELYSPQFGAKDDDPHANDLVGGLMSDGLRRLSGNEYVLSTKNTQMVSSNIITPISLDDVPPRIARAMENEEYWDFDIFELEAATHNRPLIYLGLKMFARFGICEFLHCSESTLRSWLQIIEANYHSSNPYHNSTHSADVLHATAYFLSKERIKETLDPIDEVAALIAATIHDVDHPGRTNSFLCNAGSELAILYNDTAVLESHHAALAFQLTTGDDKCNIFKNMERNDYRTLRQGIIDMVLATEMTKHFEHVNKFVNSINKPLATLEENGETDKNQEVINTMLRTPENRTLIKRMLIKCADVSNPCRPLQYCIEWAARISEEYFSQTDEEKQQGLPVVMPVFDRNTCSIPKSQISFIDYFITDMFDAWDAFVDLPDLMQHLDNNFKYWKGLDEMKLRNLRPPPE
  
Inhibitor
Name:
BDBM50150264
Synonyms:
CHEMBL3769817
Type:
Small organic molecule
Emp. Form.:
C29H27N7O
Mol. Mass.:
489.571
SMILES:
[H][C@@]12CCC[C@]1([H])N1C(=N2)N(C)C(=O)c2c(Nc3ccccc3)n(Cc3ccc(cc3)-c3ccccn3)nc12 |r,c:9|
Structure:
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