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Target
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A
Ligand
BDBM343266
Substrate
n/a
Meas. Tech.
Phosphodiersterase Evaluation Assay
IC50
<5±n/a nM
Citation
 Okano, A; Ogawa, K Pyrazole derivative US Patent  US9777000 Publication Date 10/3/2017 
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:
BDBM343266
Synonyms:
N-(6-fluoro-2-phenyl-[1,2,4]triazolo[1,5-a]pyridin-7-yl)-1-methyl-4-(6-(trifluoromethyl)pyridin-2-yl)-1H-pyrazole-5-carboxamide | US9777000, Example 3.1 | US9777000, Example 3.10
Type:
Small organic molecule
Emp. Form.:
C23H15F4N7O
Mol. Mass.:
481.4051
SMILES:
Cn1ncc(c1C(=O)Nc1cc2nc(nn2cc1F)-c1ccccc1)-c1cccc(n1)C(F)(F)F
Structure:
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