Target
High affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8B
Ligand
BDBM50390384
Substrate
n/a
Meas. Tech.
ChEMBL_835072 (CHEMBL2073616)
IC50
31.5±n/a nM
Citation
 DeNinno, MPWright, SWEtienne, JBOlson, TVRocke, BNCorbett, JWKung, DWDiRico, KJAndrews, KMMillham, MLParker, JCEsler, Wvan Volkenburg, MBoyer, DDHouseknecht, KLDoran, SD Discovery of triazolopyrimidine-based PDE8B inhibitors: exceptionally ligand-efficient and lipophilic ligand-efficient compounds for the treatment of diabetes. Bioorg Med Chem Lett 22:5721-6 (2012) [PubMed]  Article 
Target
Name:
High affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8B
Synonyms:
PDE8B | PDE8B_HUMAN | Phosphodiesterase 8 | Phosphodiesterase 8B
Type:
PROTEIN
Mol. Mass.:
98984.88
Organism:
Homo sapiens (Human)
Description:
ChEMBL_876321
Residue:
885
Sequence:
MGCAPSIHVSQSGVIYCRDSDESSSPRQTTSVSQGPAAPLPGLFVQTDAADAIPPSRASGPPSVARVRRARTELGSGSSAGSAAPAATTSRGRRRHCCSSAEAETQTCYTSVKQVSSAEVRIGPMRLTQDPIQVLLIFAKEDSQSDGFWWACDRAGYRCNIARTPESALECFLDKHHEIIVIDHRQTQNFDAEAVCRSIRATNPSEHTVILAVVSRVSDDHEEASVLPLLHAGFNRRFMENSSIIACYNELIQIEHGEVRSQFKLRACNSVFTALDHCHEAIEITSDDHVIQYVNPAFERMMGYHKGELLGKELADLPKSDKNRADLLDTINTCIKKGKEWQGVYYARRKSGDSIQQHVKITPVIGQGGKIRHFVSLKKLCCTTDNNKQIHKIHRDSGDNSQTEPHSFRYKNRRKESIDVKSISSRGSDAPSLQNRRYPSMARIHSMTIEAPITKVINIINAAQENSPVTVAEALDRVLEILRTTELYSPQLGTKDEDPHTSDLVGGLMTDGLRRLSGNEYVFTKNVHQSHSHLAMPITINDVPPCISQLLDNEESWDFNIFELEAITHKRPLVYLGLKVFSRFGVCEFLNCSETTLRAWFQVIEANYHSSNAYHNSTHAADVLHATAFFLGKERVKGSLDQLDEVAALIAATVHDVDHPGRTNSFLCNAGSELAVLYNDTAVLESHHTALAFQLTVKDTKCNIFKNIDRNHYRTLRQAIIDMVLATEMTKHFEHVNKFVNSINKPMAAEIEGSDCECNPAGKNFPENQILIKRMMIKCADVANPCRPLDLCIEWAGRISEEYFAQTDEEKRQGLPVVMPVFDRNTCSIPKSQISFIDYFITDMFDAWDAFAHLPALMQHLADNYKHWKTLDDLKCKSLRLPSDS
  
Inhibitor
Name:
BDBM50390384
Synonyms:
CHEMBL2070925
Type:
Small organic molecule
Emp. Form.:
C18H21N7
Mol. Mass.:
335.4062
SMILES:
CN1Cc2ccccc2CC1Cn1nnc2c(N)nc(nc12)C1CC1
Structure:
Search PDB for entries with ligand similarity: