Target
High affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8B
Ligand
BDBM50344032
Substrate
n/a
Meas. Tech.
ChEMBL_748479 (CHEMBL1780332)
IC50
16.5±n/a nM
Citation
 DeNinno, MPWright, SWVisser, MSEtienne, JBMoore, DEOlson, TVRocke, BNAndrews, MPZarbo, CMillham, MLBoscoe, BPBoyer, DDDoran, SDHouseknecht, KL 1,5-Substituted nipecotic amides: selective PDE8 inhibitors displaying diastereomer-dependent microsomal stability. Bioorg Med Chem Lett 21:3095-8 (2011) [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:
BDBM50344032
Synonyms:
CHEMBL1780086 | trans-(3R,5R)-N-((6-aminopyridin-2-yl)methyl)-5-ethyl-1-((5-methyl-2-morpholinooxazol-4-yl)methyl)piperidine-3-carboxamide
Type:
Small organic molecule
Emp. Form.:
C23H34N6O3
Mol. Mass.:
442.5545
SMILES:
CC[C@@H]1C[C@H](CN(Cc2nc(oc2C)N2CCOCC2)C1)C(=O)NCc1cccc(N)n1 |r|
Structure:
Search PDB for entries with ligand similarity: