Target
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A
Ligand
BDBM50365964
Substrate
n/a
Meas. Tech.
ChEMBL_834693 (CHEMBL2072669)
Ki
1.18±n/a nM
Citation
 Hu, EMa, JBiorn, CLester-Zeiner, DCho, RRumfelt, SKunz, RKNixey, TMichelsen, KMiller, SShi, JWong, JHill Della Puppa, GAble, JTalreja, SHwang, DRHitchcock, SAPorter, AImmke, DAllen, JRTreanor, JChen, H Rapid identification of a novel small molecule phosphodiesterase 10A (PDE10A) tracer. J Med Chem 55:4776-87 (2012) [PubMed]  Article 
Target
Name:
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A
Synonyms:
PDE10_RAT | Pde10a | Phosphodiesterase 10 | Phosphodiesterase 10A (PDE10A2) | Phosphodiesterase Type 10 (PDE10A) | Rat recombinant PDE10a (rPDE10a)
Type:
Enzyme
Mol. Mass.:
90160.88
Organism:
Rattus norvegicus (rat)
Description:
PDE10A was generated from the full-length recombinant rat clone transfected into Sf9 cells.
Residue:
794
Sequence:
MEDGPSNNASCFRRLTECFLSPSLTDEKVKAYLSLHPQVLDEFVSESVSAETVEKWLKRKNNKAEDEPSPKEVSRYQDTNMQGVVYELNSYIEQRLDTGGDNHLLLYELSSIIRIATKADGFALYFLGECNNSLCVFTPPGMKEGQPRLIPAGPITQGTTISAYVAKSRKTLLVEDILGDERFPRGTGLESGTRIQSVLCLPIVTAIGDLIGILELYRHWGKEAFCLSHQEVATANLAWASVAIHQVQVCRGLAKQTELNDFLLDVSKTYFDNIVAIDSLLEHIMIYAKNLVNADRCALFQVDHKNKELYSDLFDIGEEKEGKPVFKKTKEIRFSIEKGIAGQVARTGEVLNIPDAYADPRFNREVDLYTGYTTRNILCMPIVSRGSVIGVVQMVNKISGSAFSKTDENNFKMFAVFCALALHCANMYHRIRHSECIYRVTMEKLSYHSICTSEEWQGLMHFNLPARICRDIELFHFDIGPFENMWPGIFVYMIHRSCGTSCFELEKLCRFIMSVKKNYRRVPYHNWKHAVTVAHCMYAILQNNNGLFTDLERKGLLIACLCHDLDHRGFSNSYLQKFDHPLAALYSTSTMEQHHFSQTVSILQLEGHNIFSTLSSSEYEQVLEIIRKAIIATDLALYFGNRKQLEEMYQTGSLNLHNQSHRDRVIGLMMTACDLCSVTKLWPVTKLTANDIYAEFWAEGDEMKKLGIQPIPMMDRDKRDEVPQGQLGFYNAVAIPCYTTLTQILPPTEPLLKACRDNLNQWEKVIRGEETAMWISGPATSKSTSEKPTRKVDD
  
Inhibitor
Name:
BDBM50365964
Synonyms:
CHEMBL1956235 | CHEMBL2070530
Type:
Small organic molecule
Emp. Form.:
C19H22N4O2
Mol. Mass.:
338.4036
SMILES:
COc1cc2nncc(-c3cnc(NC(C)C)c(C)c3)c2cc1OC
Structure:
Search PDB for entries with ligand similarity: