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Target
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A
Ligand
BDBM125599
Substrate
n/a
Meas. Tech.
Homogenous Time-Resolved Fluorescence Resonance Energy Transfer Assay
pH
7.4±n/a
IC50
1.4±n/a nM
Comments
extracted
Citation
 Leblond, B; Donello, JE; Chauvignac, C; Taverne, T; Beausoleil, E; Casagrande, A; Désiré, L; Pando, MP; Yang, R Substituted 6,7-dialkoxy-3-isoquinolinol derivatives as inhibitors of phosphodiesterase 10 (PDE10A) US Patent  US8772316 Publication Date 7/8/2014 
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:
BDBM125599
Synonyms:
US8772316, 82
Type:
Small organic molecule
Emp. Form.:
C26H28FN3O4
Mol. Mass.:
465.5166
SMILES:
CCNc1nc2cc(F)c(OC)cc2cc1Cc1c2cc(OC)c(OC)cc2c(CC)[nH]c1=O
Structure:
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