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Target
Isoform PDE10A2 of cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A (PDE10A2)
Ligand
BDBM193240
Substrate
n/a
Meas. Tech.
In Vitro Assay
IC50
<1±n/a nM
Citation
 Player, MR; Meegalla, SK; Illig, CR; Chen, J; Wilson, KJ; Lee, Y; Parks, DJ; Cheung, WS; Huang, H; Patch, RJ PDE 10a inhibitors for the treatment of type II diabetes US Patent  US9193736 Publication Date 11/24/2015 
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:
BDBM193240
Synonyms:
US9193736, 164
Type:
Small organic molecule
Emp. Form.:
C30H27N5O3
Mol. Mass.:
505.5671
SMILES:
OC(=O)c1ccc(cc1)-c1c(nc2c(ccnn12)N1CCOCC1)[C@H]1C[C@@H](C1)c1ccc2ccccc2n1 |wU:24.27,wD:26.32,(4.46,-12.1,;4.14,-10.59,;2.67,-10.12,;5.28,-9.56,;4.96,-8.06,;6.11,-7.03,;7.57,-7.5,;7.89,-9.01,;6.75,-10.04,;8.72,-6.47,;8.55,-4.94,;9.96,-4.31,;10.99,-5.46,;12.53,-5.46,;13.3,-6.79,;12.53,-8.12,;10.99,-8.12,;10.22,-6.79,;13.3,-4.12,;12.53,-2.79,;13.3,-1.46,;14.84,-1.46,;15.61,-2.79,;14.84,-4.12,;7.22,-4.17,;5.73,-4.57,;5.33,-3.08,;6.82,-2.68,;4,-2.31,;4,-.77,;2.67,,;1.33,-.77,;;-1.33,-.77,;-1.33,-2.31,;,-3.08,;1.33,-2.31,;2.67,-3.08,)|
Structure:
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