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Target
High affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8B
Ligand
BDBM50344036
Substrate
n/a
Meas. Tech.
ChEMBL_748479 (CHEMBL1780332)
IC50
35.2±n/a nM
Citation
 DeNinno, MP; Wright, SW; Visser, MS; Etienne, JB; Moore, DE; Olson, TV; Rocke, BN; Andrews, MP; Zarbo, C; Millham, ML; Boscoe, BP; Boyer, DD; Doran, SD; Houseknecht, 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:
BDBM50344036
Synonyms:
CHEMBL1780103 | trans-(3R,5R)-5-(3-methyl-1,2,4-oxadiazol-5-yl)-1-((5-methyl-2-phenyloxazol-4-yl)methyl)-N-(((S)-tetrahydrofuran-2-yl)methyl)piperidine-3-carboxamide
Type:
Small organic molecule
Emp. Form.:
C25H31N5O4
Mol. Mass.:
465.5447
SMILES:
Cc1noc(n1)[C@@H]1C[C@H](CN(Cc2nc(oc2C)-c2ccccc2)C1)C(=O)NC[C@@H]1CCCO1 |r|
Structure:
Search PDB for entries with ligand similarity: