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TargetcAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A
LigandBDBM50362736
Substrate/Competitorn/a
Meas. Tech.ChEMBL_797637 (CHEMBL1943755)
Ki 419±n/a nM
Citation Ho, GDYang, SWSmotryski, JBercovici, ANechuta, TSmith, EMMcElroy, WTan, ZTulshian, DMcKittrick, BGreenlee, WJHruza, AXiao, LRindgen, DMullins, DGuzzi, MZhang, XBleickardt, CHodgson, R The discovery of potent, selective, and orally active pyrazoloquinolines as PDE10A inhibitors for the treatment of Schizophrenia. Bioorg Med Chem Lett22:1019-22 (2012) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A
Name:cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A
Synonyms:3',5'-cyclic phosphodiesterase | 3.1.4.17 | PDE10A | PDE10_HUMAN | Phosphodiesterase 10 (PDE10) | Phosphodiesterase 10A
Type:Protein
Mol. Mass.:88412.52
Organism:Homo sapiens (Human)
Description:Q9Y233
Residue:1055
Sequence:
MASLEEPLAPRPQGPLPAAGDEPGCGPGKLRPEPRLSAAGGGSAAGPGPAPEWPGRGRAE
RAAPPRPPLSSAGRPSPAGGPGALSARGGGCGWVAARAPLALAFSSRVPSSSPSFFYFWP
PPPPPPPSFLPSSSAFHLPVRLPGREGAAAAAAAGGGGDAGGGGGGGQEAAPLSVPTSSS
HRGGGGSGGGRRRLFLSPALQGLLLPARAGPRPPPPPRLPLGQAARRAGSPGFPGAGPGG
GGQTPRRPQGASFALAAAAALLFGSDMEDGPSNNASCFRRLTECFLSPSLTDEKVKAYLS
LHPQVLDEFVSESVSAETVEKWLKRKNNKSEDESAPKEVSRYQDTNMQGVVYELNSYIEQ
RLDTGGDNQLLLYELSSIIKIATKADGFALYFLGECNNSLCIFTPPGIKEGKPRLIPAGP
ITQGTTVSAYVAKSRKTLLVEDILGDERFPRGTGLESGTRIQSVLCLPIVTAIGDLIGIL
ELYRHWGKEAFCLSHQEVATANLAWASVAIHQVQVCRGLAKQTELNDFLLDVSKTYFDNI
VAIDSLLEHIMIYAKNLVNADRCALFQVDHKNKELYSDLFDIGEEKEGKPVFKKTKEIRF
SIEKGIAGQVARTGEVLNIPDAYADPRFNREVDLYTGYTTRNILCMPIVSRGSVIGVVQM
VNKISGSAFSKTDENNFKMFAVFCALALHCANMYHRIRHSECIYRVTMEKLSYHSICTSE
EWQGLMQFTLPVRLCKEIELFHFDIGPFENMWPGIFVYMVHRSCGTSCFELEKLCRFIMS
VKKNYRRVPYHNWKHAVTVAHCMYAILQNNHTLFTDLERKGLLIACLCHDLDHRGFSNSY
LQKFDHPLAALYSTSTMEQHHFSQTVSILQLEGHNIFSTLSSSEYEQVLEIIRKAIIATD
LALYFGNRKQLEEMYQTGSLNLNNQSHRDRVIGLMMTACDLCSVTKLWPVTKLTANDIYA
EFWAEGDEMKKLGIQPIPMMDRDKKDEVPQGQLGFYNAVAIPCYTTLTQILPPTEPLLKA
CRDNLSQWEKVIRGEETATWISSPSVAQKAAASED
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM50362736
n/a
NameBDBM50362736
Synonyms:CHEMBL1939786
TypeSmall organic molecule
Emp. Form.C15H16ClN5
Mol. Mass.301.774
SMILESCc1n[nH]c2nc3ccc(Cl)cc3c(N3CCNCC3)c12
Structure
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