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TargetHigh affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8A
LigandBDBM50180268
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1583588 (CHEMBL3815675)
IC50>10000±n/a nM
Citation Yoshikawa, MHitaka, THasui, TFushimi, MKunitomo, JKokubo, HOki, HNakashima, KTaniguchi, T Design and synthesis of potent and selective pyridazin-4(1H)-one-based PDE10A inhibitors interacting with Tyr683 in the PDE10A selectivity pocket. Bioorg Med Chem24:3447-55 (2016) [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
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  Blast E-value cutoff:
BDBM50180268
n/a
NameBDBM50180268
Synonyms:CHEMBL3814662
TypeSmall organic molecule
Emp. Form.C28H27N7O2
Mol. Mass.493.5597
SMILESO=c1c(OCCN2CCn3c2nc2ccccc32)cn(CC2CC2)nc1-c1ccnn1-c1ccccc1
Structure
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