Target
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A
Ligand
BDBM173083
Substrate
n/a
Meas. Tech.
Inhibition Assay
Temperature
298.15±n/a K
IC50
8.8±n/a nM
Comments
extracted
Citation
 Püschl, ANielsen, JKehler, JKilburn, JPMarigo, MLanggård, M Heteroaromatic phenylimidazole derivatives as PDE10A enzyme inhibitors US Patent  US9096589 Publication Date 8/4/2015 
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:
BDBM173083
Synonyms:
US9096589, 5,7-Dimethyl-2-[(E)-2-(1-methyl-4-thiophen-2-yl-1H-imidazol-2-yl)-vinyl]-imidazo[1,2-a]pyrimidine | US9669029, 3 5,7-Dimethyl-2-[(E)-2-(1-methyl-4-thiophen-2-yl-1H-imidazol-2-yl)-vinyl]-imidazo[1,2-a]pyrimidine
Type:
Small organic molecule
Emp. Form.:
C18H17N5S
Mol. Mass.:
335.426
SMILES:
Cc1cc(C)n2cc(\C=C\c3nc(cn3C)-c3cccs3)nc2n1
Structure:
Search PDB for entries with ligand similarity: