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Target
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A
Ligand
BDBM124430
Substrate
n/a
Meas. Tech.
Enzyme Inhibition Assay
Temperature
298.15±n/a K
IC50
0.249±n/a nM
Comments
extracted
Citation
 Allen, JR; Biswas, K; Chavez, Jr., F; Chen, N; De Morin, FF; Falsey, JR; Frohn, MJ; Harrington, PE; Home, DB; Harrington, EH; Kaller, MR; Kunz, RK; Monenschein, H; Nguyen, TT; Pickrell, AJ; Reichelt, A; Rumfelt, S; Rzasa, RM; Sham, K; Yao, G Pyridine and pyrimidine derivatives as phosphodiesterase 10 inhibitors US Patent  US8759532 Publication Date 6/24/2014 
Target
Name:
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A
Synonyms:
3',5'-cyclic phosphodiesterase | PDE10A | PDE10_HUMAN | Phosphodiesterase 10 (PDE10) | Phosphodiesterase 10A
Type:
Protein
Mol. Mass.:
88412.52
Organism:
Homo sapiens (Human)
Description:
Q9Y233
Residue:
779
Sequence:
MRIEERKSQHLTGLTDEKVKAYLSLHPQVLDEFVSESVSAETVEKWLKRKNNKSEDESAPKEVSRYQDTNMQGVVYELNSYIEQRLDTGGDNQLLLYELSSIIKIATKADGFALYFLGECNNSLCIFTPPGIKEGKPRLIPAGPITQGTTVSAYVAKSRKTLLVEDILGDERFPRGTGLESGTRIQSVLCLPIVTAIGDLIGILELYRHWGKEAFCLSHQEVATANLAWASVAIHQVQVCRGLAKQTELNDFLLDVSKTYFDNIVAIDSLLEHIMIYAKNLVNADRCALFQVDHKNKELYSDLFDIGEEKEGKPVFKKTKEIRFSIEKGIAGQVARTGEVLNIPDAYADPRFNREVDLYTGYTTRNILCMPIVSRGSVIGVVQMVNKISGSAFSKTDENNFKMFAVFCALALHCANMYHRIRHSECIYRVTMEKLSYHSICTSEEWQGLMQFTLPVRLCKEIELFHFDIGPFENMWPGIFVYMVHRSCGTSCFELEKLCRFIMSVKKNYRRVPYHNWKHAVTVAHCMYAILQNNHTLFTDLERKGLLIACLCHDLDHRGFSNSYLQKFDHPLAALYSTSTMEQHHFSQTVSILQLEGHNIFSTLSSSEYEQVLEIIRKAIIATDLALYFGNRKQLEEMYQTGSLNLNNQSHRDRVIGLMMTACDLCSVTKLWPVTKLTANDIYAEFWAEGDEMKKLGIQPIPMMDRDKKDEVPQGQLGFYNAVAIPCYTTLTQILPPTEPLLKACRDNLSQWEKVIRGEETATWISSPSVAQKAAASED
  
Inhibitor
Name:
BDBM124430
Synonyms:
US8759532, 83
Type:
Small organic molecule
Emp. Form.:
C24H19N5O
Mol. Mass.:
393.4406
SMILES:
Cn1c(Nc2ccc(Oc3ncccc3-c3cccnc3)cc2)nc2ccccc12
Structure:
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