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TargetcAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A
LigandBDBM144390
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1849279 (CHEMBL4349820)
IC50 0.062000±n/a nM
Citation Koizumi, YTanaka, YMatsumura, TKadoh, YMiyoshi, HHongu, MTakedomi, KKotera, JSasaki, TTaniguchi, HWatanabe, YTakakuwa, MKojima, KBaba, NNakamura, IKawanishi, E Discovery of a pyrazolo[1,5-a]pyrimidine derivative (MT-3014) as a highly selective PDE10A inhibitor via core structure transformation from the stilbene moiety. Bioorg Med Chem27:3440-3450 (2019) [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:
BDBM144390
n/a
NameBDBM144390
Synonyms:US8969376, 1.006
TypeSmall organic molecule
Emp. Form.C23H25F2N7O
Mol. Mass.453.4877
SMILESCc1nc2ccc(F)cc2nc1-c1cc2nc(cc(NCC(C)(C)O)n2n1)N1CC[C@@H](F)C1 |r|
Structure
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