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Target
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A
Ligand
BDBM115249
Substrate
n/a
Meas. Tech.
Enzyme Inhibition Assay
Temperature
298.15±n/a K
IC50
306.6±n/a nM
Comments
extracted
Citation
 Allen, JR; Chen, N; Falsey, JR; Frohn, MJ; Harrington, PE; Harrington, EH; Kaller, MR; Kunz, RK; Nguyen, TT; Pickrell, AJ; Reichelt, A; Rumfelt, S; Rzasa, RM; Sham, K; Siegmund, AC; Yao, G Aminopyridine and carboxypyridine compounds as phosphodiesterase 10 inhibitors US Patent  US8637500 Publication Date 1/28/2014 
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:
BDBM115249
Synonyms:
US8637500, 56
Type:
Small organic molecule
Emp. Form.:
C23H26N4O2
Mol. Mass.:
390.4781
SMILES:
COCC1CCN(CC1)c1cccnc1Oc1ccc(Nc2ccccn2)cc1
Structure:
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