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Target
High affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8A
Ligand
BDBM50357870
Substrate
n/a
Meas. Tech.
ChEMBL_787244 (CHEMBL1918966)
IC50
>500±n/a nM
Citation
 Malamas, MS; Ni, Y; Erdei, J; Stange, H; Schindler, R; Lankau, HJ; Grunwald, C; Fan, KY; Parris, K; Langen, B; Egerland, U; Hage, T; Marquis, KL; Grauer, S; Brennan, J; Navarra, R; Graf, R; Harrison, BL; Robichaud, A; Kronbach, T; Pangalos, MN; Hoefgen, N; Brandon, NJ Highly potent, selective, and orally active phosphodiesterase 10A inhibitors. J Med Chem 54:7621-38 (2011) [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:
BDBM50357870
Synonyms:
CHEMBL1916130
Type:
Small organic molecule
Emp. Form.:
C20H17F3N4O
Mol. Mass.:
386.3704
SMILES:
COc1cc(cc2c1nc(C)c1c(C)nc(-c3ccncc3C)n21)C(F)(F)F
Structure:
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