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Target
High affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8B
Ligand
BDBM50344014
Substrate
n/a
Meas. Tech.
ChEMBL_748479 (CHEMBL1780332)
IC50
0.9±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:
BDBM50344014
Synonyms:
CHEMBL1779987 | trans-(3R,5S)-1-((5-methyl-2-phenyloxazol-4-yl)methyl)-N-((6-methylpyridin-2-yl)methyl)-5-phenylpiperidine-3-carboxamide
Type:
Small organic molecule
Emp. Form.:
C30H32N4O2
Mol. Mass.:
480.6007
SMILES:
Cc1oc(nc1CN1C[C@@H](C[C@H](C1)c1ccccc1)C(=O)NCc1cccc(C)n1)-c1ccccc1 |r|
Structure:
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