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Target
High affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8A
Ligand
BDBM50236225
Substrate
n/a
Meas. Tech.
ChEMBL_1658914 (CHEMBL4008526)
IC50
>10000±n/a nM
Citation
 Gomez, L; Massari, ME; Vickers, T; Freestone, G; Vernier, W; Ly, K; Xu, R; McCarrick, M; Marrone, T; Metz, M; Yan, YG; Yoder, ZW; Lemus, R; Broadbent, NJ; Barido, R; Warren, N; Schmelzer, K; Neul, D; Lee, D; Andersen, CB; Sebring, K; Aertgeerts, K; Zhou, X; Tabatabaei, A; Peters, M; Breitenbucher, JG Design and Synthesis of Novel and Selective Phosphodiesterase 2 (PDE2a) Inhibitors for the Treatment of Memory Disorders. J Med Chem 60:2037-2051 (2017) [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:
BDBM50236225
Synonyms:
CHEMBL4074744 | US11186582, Example 269 | US11419874, DNS-8254
Type:
Small organic molecule
Emp. Form.:
C18H15BrF3N5O
Mol. Mass.:
454.244
SMILES:
Cc1cc([C@@H]2CN(CC(F)(F)C2)C(=O)c2ccc(F)c(Br)c2)n2ncnc2n1 |r|
Structure:
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