Ki Summary BindingDB logo
myBDB logout
Reaction Details
Report a problem with these data
TargetHigh affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8A
LigandBDBM289653
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1661917 (CHEMBL4011529)
IC50 8400±n/a nM
Citation Dyck, BBranstetter, BGharbaoui, THudson, ARBreitenbucher, JGGomez, LBotrous, IMarrone, TBarido, RAllerston, CKCedervall, EPXu, RSridhar, VBarker, RAertgeerts, KSchmelzer, KNeul, DLee, DMassari, MEAndersen, CBSebring, KZhou, XPetroski, RLimberis, JAugustin, MChun, LEEdwards, TEPeters, MTabatabaei, A Discovery of Selective Phosphodiesterase 1 Inhibitors with Memory Enhancing Properties. J Med Chem60:3472-3483 (2017) [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:
BDBM289653
n/a
NameBDBM289653
Synonyms:6-(2-Fluoro-4-methoxybenzyl)-9-((tetrahydro-2H-pyran-4-yl)methyl)-8,9,10,11-tetrahydropyrido[4',3':4,5]thieno[3,2-e][1,2,4]triazolo[1,5-c]pyrimidin-5 (6H)-one | US10092575, Example 141 | US10376514, Example 141
TypeSmall organic molecule
Emp. Form.C24H26FN5O3S
Mol. Mass.483.558
SMILESCOc1ccc(Cn2c3sc4CN(CC5CCOCC5)CCc4c3c3ncnn3c2=O)c(F)c1
Structure
Search PDB for entries with ligand similarity:Similarity to this molecule at least: