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Target
High affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8A
Ligand
BDBM50362048
Substrate
n/a
Meas. Tech.
ChEMBL_798761 (CHEMBL1942896)
Ki
>10000±n/a nM
Citation
Yang, SW; Smotryski, J; McElroy, WT; Tan, Z; Ho, G; Tulshian, D; Greenlee, WJ; Guzzi, M; Zhang, X; Mullins, D; Xiao, L; Hruza, A; Chan, TM; Rindgen, D; Bleickardt, C; Hodgson, R Discovery of orally active pyrazoloquinolines as potent PDE10 inhibitors for the management of schizophrenia. Bioorg Med Chem Lett 22:235-9 (2011) [PubMed] Article
More Info.:
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:
Human
Description:
Recombinant catalytic domain (M1-E829) of human PDE8A.
Residue:
829
Sequence:
MGCAPSIHISERLVAEDAPSPAAPPLSSGGPRLPQGQKTAALPRTRGAGLLESELRDGSGKKVAVADVQFGPMRFHQDQLQVLLVFTKEDNQCNGFCRACEKAGFKCTVTKEAQAVLACFLDKHHDIIIIDHRNPRQLDAEALCRSIRSSKLSENTVIVGVVRRVDREELSVMPFISAGFTRRYVENPNIMACYNELLQLEFGEVRSQLKLRACNSVFTALENSEDAIEITSEDRFIQYANPAFETTMGYQSGELIGKELGEVPINEKKADLLDTINSCIRIGKEWQGIYYAKKKNGDNIQQNVKIIPVIGQGGKIRHYVSIIRVCNGNNKAEKISECVQSDTHTDNQTGKHKDRRKGSLDVKAVASRATEVSSQRRHSSMARIHSMTIEAPITKVINIINAAQESSPMPVTEALDRVLEILRTTELYSPQFGAKDDDPHANDLVGGLMSDGLRRLSGNEYVLSTKNTQMVSSNIITPISLDDVPPRIARAMENEEYWDFDIFELEAATHNRPLIYLGLKMFARFGICEFLHCSESTLRSWLQIIEANYHSSNPYHNSTHSADVLHATAYFLSKERIKETLDPIDEVAALIAATIHDVDHPGRTNSFLCNAGSELAILYNDTAVLESHHAALAFQLTTGDDKCNIFKNMERNDYRTLRQGIIDMVLATEMTKHFEHVNKFVNSINKPLATLEENGETDKNQEVINTMLRTPENRTLIKRMLIKCADVSNPCRPLQYCIEWAARISEEYFSQTDEEKQQGLPVVMPVFDRNTCSIPKSQISFIDYFITDMFDAWDAFVDLPDLMQHLDNNFKYWKGLDEMKLRNLRPPPE