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Target
High affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8B
Ligand
BDBM50390371
Substrate
n/a
Meas. Tech.
ChEMBL_835072 (CHEMBL2073616)
IC50
17.1±n/a nM
Citation
 DeNinno, MP; Wright, SW; Etienne, JB; Olson, TV; Rocke, BN; Corbett, JW; Kung, DW; DiRico, KJ; Andrews, KM; Millham, ML; Parker, JC; Esler, W; van Volkenburg, M; Boyer, DD; Houseknecht, KL; Doran, 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:
BDBM50390371
Synonyms:
CHEMBL2070912
Type:
Small organic molecule
Emp. Form.:
C16H17FN6O2
Mol. Mass.:
344.3436
SMILES:
Nc1nc(COc2cccc(F)c2)nc2n(CC3CCCO3)nnc12
Structure:
Search PDB for entries with ligand similarity: