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Target
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A
Ligand
BDBM50350800
Substrate
n/a
Meas. Tech.
ChEMBL_763299 (CHEMBL1820393)
IC50
5±n/a nM
Citation
Helal, CJ; Kang, Z; Hou, X; Pandit, J; Chappie, TA; Humphrey, JM; Marr, ES; Fennell, KF; Chenard, LK; Fox, C; Schmidt, CJ; Williams, RD; Chapin, DS; Siuciak, J; Lebel, L; Menniti, F; Cianfrogna, J; Fonseca, KR; Nelson, FR; O'Connor, R; MacDougall, M; McDowell, L; Liras, S Use of structure-based design to discover a potent, selective, in vivo active phosphodiesterase 10A inhibitor lead series for the treatment of schizophrenia. J Med Chem 54:4536-47 (2011) [PubMed] Article
More Info.:
Target
Name:
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A
Synonyms:
PDE10_RAT | Pde10a | Phosphodiesterase 10 | Phosphodiesterase 10A (PDE10A2) | Phosphodiesterase Type 10 (PDE10A) | Rat recombinant PDE10a (rPDE10a)
Type:
Enzyme
Mol. Mass.:
90160.88
Organism:
Rattus norvegicus (rat)
Description:
PDE10A was generated from the full-length recombinant rat clone transfected into Sf9 cells.
Residue:
794
Sequence:
MEDGPSNNASCFRRLTECFLSPSLTDEKVKAYLSLHPQVLDEFVSESVSAETVEKWLKRKNNKAEDEPSPKEVSRYQDTNMQGVVYELNSYIEQRLDTGGDNHLLLYELSSIIRIATKADGFALYFLGECNNSLCVFTPPGMKEGQPRLIPAGPITQGTTISAYVAKSRKTLLVEDILGDERFPRGTGLESGTRIQSVLCLPIVTAIGDLIGILELYRHWGKEAFCLSHQEVATANLAWASVAIHQVQVCRGLAKQTELNDFLLDVSKTYFDNIVAIDSLLEHIMIYAKNLVNADRCALFQVDHKNKELYSDLFDIGEEKEGKPVFKKTKEIRFSIEKGIAGQVARTGEVLNIPDAYADPRFNREVDLYTGYTTRNILCMPIVSRGSVIGVVQMVNKISGSAFSKTDENNFKMFAVFCALALHCANMYHRIRHSECIYRVTMEKLSYHSICTSEEWQGLMHFNLPARICRDIELFHFDIGPFENMWPGIFVYMIHRSCGTSCFELEKLCRFIMSVKKNYRRVPYHNWKHAVTVAHCMYAILQNNNGLFTDLERKGLLIACLCHDLDHRGFSNSYLQKFDHPLAALYSTSTMEQHHFSQTVSILQLEGHNIFSTLSSSEYEQVLEIIRKAIIATDLALYFGNRKQLEEMYQTGSLNLHNQSHRDRVIGLMMTACDLCSVTKLWPVTKLTANDIYAEFWAEGDEMKKLGIQPIPMMDRDKRDEVPQGQLGFYNAVAIPCYTTLTQILPPTEPLLKACRDNLNQWEKVIRGEETAMWISGPATSKSTSEKPTRKVDD