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Target
Isoform PDE10A2 of cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A (PDE10A2)
Ligand
BDBM194113
Substrate
n/a
Meas. Tech.
Fluorescence Polarization Assay
Ki
0.003±n/a nM
Citation
 Cox, CD; Dudkin, VY; Kim, JJ; Kuduk, SD; McVean, CA; Reger, T; Sheen, JT; Steele, T Triazolyl PDE10 inhibitors US Patent  US9200001 Publication Date 12/1/2015 
Target
Name:
Isoform PDE10A2 of cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A (PDE10A2)
Synonyms:
PDE10A | PDE10_HUMAN | Phosphodiesterase 10A | Phosphodiesterase 10A (PDE10A2) | Phosphodiesterase 10A2 | Phosphodiesterase 10A2 (PDE10A) | cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A (PDE10A2)
Type:
Enzyme
Mol. Mass.:
89387.03
Organism:
Homo sapiens (Human)
Description:
Q9Y233-2
Residue:
789
Sequence:
MEDGPSNNASCFRRLTECFLSPSLTDEKVKAYLSLHPQVLDEFVSESVSAETVEKWLKRKNNKSEDESAPKEVSRYQDTNMQGVVYELNSYIEQRLDTGGDNQLLLYELSSIIKIATKADGFALYFLGECNNSLCIFTPPGIKEGKPRLIPAGPITQGTTVSAYVAKSRKTLLVEDILGDERFPRGTGLESGTRIQSVLCLPIVTAIGDLIGILELYRHWGKEAFCLSHQEVATANLAWASVAIHQVQVCRGLAKQTELNDFLLDVSKTYFDNIVAIDSLLEHIMIYAKNLVNADRCALFQVDHKNKELYSDLFDIGEEKEGKPVFKKTKEIRFSIEKGIAGQVARTGEVLNIPDAYADPRFNREVDLYTGYTTRNILCMPIVSRGSVIGVVQMVNKISGSAFSKTDENNFKMFAVFCALALHCANMYHRIRHSECIYRVTMEKLSYHSICTSEEWQGLMQFTLPVRLCKEIELFHFDIGPFENMWPGIFVYMVHRSCGTSCFELEKLCRFIMSVKKNYRRVPYHNWKHAVTVAHCMYAILQNNHTLFTDLERKGLLIACLCHDLDHRGFSNSYLQKFDHPLAALYSTSTMEQHHFSQTVSILQLEGHNIFSTLSSSEYEQVLEIIRKAIIATDLALYFGNRKQLEEMYQTGSLNLNNQSHRDRVIGLMMTACDLCSVTKLWPVTKLTANDIYAEFWAEGDEMKKLGIQPIPMMDRDKKDEVPQGQLGFYNAVAIPCYTTLTQILPPTEPLLKACRDNLSQWEKVIRGEETATWISSPSVAQKAAASED
  
Inhibitor
Name:
BDBM194113
Synonyms:
US9200001, 28
Type:
Small organic molecule
Emp. Form.:
C28H29N7O2
Mol. Mass.:
495.5756
SMILES:
COc1ccc(Cc2nc(C)nn2-c2cc(nc(C)n2)C2CC2c2nc3ccccc3n2C)cc1OC
Structure:
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