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Target
High affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8A
Ligand
BDBM50176521
Substrate
n/a
Meas. Tech.
ChEMBL_327543 (CHEMBL854358)
IC50
>16000±n/a nM
Citation
 Chambers, RJ; Abrams, K; Garceau, NY; Kamath, AV; Manley, CM; Lilley, SC; Otte, DA; Scott, DO; Sheils, AL; Tess, DA; Vellekoop, AS; Zhang, Y; Lam, KT A new chemical tool for exploring the physiological function of the PDE2 isozyme. Bioorg Med Chem Lett 16:307-10 (2005) [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:
BDBM50176521
Synonyms:
5-methyl-6-oxo-6,7-dihydro-5H-furo[2,3-f]indole-7-carboxylic acid [1,3,4]thiadiazol-2-ylamide | CHEMBL200906
Type:
Small organic molecule
Emp. Form.:
C14H10N4O3S
Mol. Mass.:
314.319
SMILES:
CN1C(=O)C(C(=O)Nc2nncs2)c2cc3occc3cc12
Structure:
Search PDB for entries with ligand similarity: