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Target
Isoform PDE10A2 of cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A (PDE10A2)
Ligand
BDBM193246
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:
BDBM193246
Synonyms:
US9193736, 170
Type:
Small organic molecule
Emp. Form.:
C33H31N5O3
Mol. Mass.:
545.6309
SMILES:
OC(=O)[C@@H]1C[C@@H]1c1ccc(cc1)-c1c(nc2c(ccnn12)N1CCOCC1)[C@H]1C[C@@H](C1)c1ccc2ccccc2n1 |wU:27.31,wD:3.2,29.36,5.6,(-1.64,-8.26,;-.49,-7.23,;.97,-7.71,;-.81,-5.72,;-1.84,-4.58,;-.34,-4.26,;.81,-3.23,;.49,-1.72,;1.63,-.69,;3.1,-1.17,;3.42,-2.67,;2.27,-3.7,;4.24,-.14,;4.08,1.39,;5.49,2.02,;6.52,.88,;8.06,.88,;8.83,-.46,;8.06,-1.79,;6.52,-1.79,;5.75,-.46,;8.83,2.21,;8.06,3.54,;8.83,4.88,;10.37,4.88,;11.14,3.54,;10.37,2.21,;2.75,2.16,;1.26,1.77,;.86,3.25,;2.35,3.65,;-.47,4.02,;-.47,5.56,;-1.81,6.33,;-3.14,5.56,;-4.47,6.33,;-5.81,5.56,;-5.81,4.02,;-4.47,3.25,;-3.14,4.02,;-1.81,3.25,)|
Structure:
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