The Ligandable Human Proteome

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cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A

3'5'-cyclic nucleotide phosphodiesterase, catalytic domain

IndexLigand NameStructurePDB codeCompound Potency nM
14xuPDE10 complexed with 6-chloro-N-[(2,4-dimethylthiazol-5-yl)methyl]-5-methyl-2-[3-(2-quinolyl)propoxy]pyrimidin-4-amine5c2h0.0082
24lpCrystal structure of the catalytic domain of PDE10A complexed with highly potent and brain-penetrant PDE10A Inhibitor with 2-oxindole scaffold5axq0.08
315jCrystal Structure of PDE10A with a biaryl ether inhibitor ((1-(3-(4-((1H-benzo[d]imidazol-2-yl)amino)phenoxy)pyridin-2-yl)piperidin-4-yl)methanol)4heu0.097
42w1Crystal Structure of PDE10A with 1H-benzimidazol-2-yl(4-((3-(tetrahydro-2H-pyran-4-yl)-2-pyridinyl)oxy)phenyl)methanone4phw0.1
55ayPDE10 complexed with N-[(1-methylpyrazol-4-yl)methyl]-5-[[(1S,2S)-2-(2-pyridyl)cyclopropyl]methoxy]pyrazolo[1,5-a]pyrimidin-7-amine5dh50.23
60t6Potent and Selective Phosphodiesterase 10A Inhibitors4fcd0.28
75m9human PDE10A, 6-Chloro-5,8-dimethyl-2-[2-(2-methyl-5-pyrrolidin-1-yl-2H-[1,2,4]triazol-3-yl)-ethyl]-[1,2,4]triazolo[1,5-a]pyridine, 2.20A, H3, Rfree=23.5%5edi0.3
8pf9Discovery of novel inhibitors of PDE10A3hr10.37
96dtCrystal structure of the catalytic domain of human PDE10A complexed with N-(4-((5-methyl-5H-pyrrolo[3,2-d]pyrimidin-4-yl)oxy)phenyl)-1H-benzimidazol-2-amine5b4k0.46
10540Highly Potent, Selective, and Orally Active Phosphodiestarase 10A Inhibitors3sn70.7
116dwCrystal structure of the catalytic domain of human PDE10A complexed with 1-(cyclopropylmethyl)-5-(2-(2,3-dihydro-1H-imidazo[1,2-a]benzimidazol-1-yl)ethoxy)-3-(1-phenyl-1H-pyrazol-5-yl)pyridazin-4(1H)-one5b4l0.76
12c1lDiscovery of orally active pyrazoloquinoline as a potent PDE10 inhibitor for the management of schizophrenia3ui71
1315hCrystal Structure of PDE10A with a biaryl ether inhibitor (1-(1-(3-(4-(benzo[d]thiazol-2-ylamino)phenoxy)pyrazin-2-yl)piperidin-4-yl)ethanol)4hf42.4
140t7Potent and Selective Phosphodiesterase 10A Inhibitors4fcb2.9
15pfjCrystal structure of the catalytic domain of rat phosphodiesterase 10A2ovy4
162f5Crystal Structure of PDE10A with Novel Keto-Benzimidazole Inhibitor4mvh4.5
174y2PDE10 complexed with 6-chloro-2-cyclopropyl-N-[(2,4-dimethylthiazol-5-yl)methyl]-5-methyl-pyrimidin-4-amine5c2a4.8
180jqPDE10a Crystal Structure Complexed with Novel Inhibitor4ddl4.9
19490Crystal structure of PDE10A in complex with ASP94364xy28
202f4Crystal Structure of PDE10A with Novel Keto-Benzimidazole Inhibitor4muw9.7
21546Highly Potent, Selective, and Orally Active Phosphodiestarase 10A Inhibitors3sni11
22pf6Discovery of novel inhibitors of PDE10A3hqy11.5
23pfwStructure of PDE10-inhibitor complex3qpp12
24pfhCrystal structure of the catalytic domain of rat phosphodiesterase 10A2ovv12
254hnPDE10A in complex with the inhibitor AZ54ael12
26axcTriazoloquinazolines as a novel class of phosphodiesterase 10A (PDE10A) inhibitors, part 2, Lead-optimisation.2y0j12
27pfkStructure of PDE10-inhibitor complex3qpn17
28227Crystal structure of the catalytic domain of rat phosphodiesterase 10A2o8h25
298q7Crystal structure of human PDE10A in complex with inhibitor 16d5uwf59
30ev1Human PDE-papaverine complex obtained by ligand soaking of cross- linked protein crystals2wey76
31x4cCrystal structure of PDE10A in complex with a benzimidazole inhibitor3ws8210
32pfrStructure of PDE10-inhibitor complex3qpo247
334xyPDE10 complexed with 6-chloro-2-cyclopropyl-5-methyl-N-propyl-pyrimidin-4-amine5c29880