Index | Ligand Name | Structure | PDB code | Compound Potency nM |
1 | 4xu | PDE10 complexed with 6-chloro-N-[(2,4-dimethylthiazol-5-yl)methyl]-5-methyl-2-[3-(2-quinolyl)propoxy]pyrimidin-4-amine | 5c2h | 0.0082 |
2 | 4lp | Crystal structure of the catalytic domain of PDE10A complexed with highly potent and brain-penetrant PDE10A Inhibitor with 2-oxindole scaffold | 5axq | 0.08 |
3 | 15j | Crystal 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) | 4heu | 0.097 |
4 | 2w1 | Crystal Structure of PDE10A with 1H-benzimidazol-2-yl(4-((3-(tetrahydro-2H-pyran-4-yl)-2-pyridinyl)oxy)phenyl)methanone | 4phw | 0.1 |
5 | 5ay | PDE10 complexed with N-[(1-methylpyrazol-4-yl)methyl]-5-[[(1S,2S)-2-(2-pyridyl)cyclopropyl]methoxy]pyrazolo[1,5-a]pyrimidin-7-amine | 5dh5 | 0.23 |
6 | 0t6 | Potent and Selective Phosphodiesterase 10A Inhibitors | 4fcd | 0.28 |
7 | 5m9 | human 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% | 5edi | 0.3 |
8 | pf9 | Discovery of novel inhibitors of PDE10A | 3hr1 | 0.37 |
9 | 6dt | Crystal 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-amine | 5b4k | 0.46 |
10 | 540 | Highly Potent, Selective, and Orally Active Phosphodiestarase 10A Inhibitors | 3sn7 | 0.7 |
11 | 6dw | Crystal 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)-one | 5b4l | 0.76 |
12 | c1l | Discovery of orally active pyrazoloquinoline as a potent PDE10 inhibitor for the management of schizophrenia | 3ui7 | 1 |
13 | 15h | Crystal 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) | 4hf4 | 2.4 |
14 | 0t7 | Potent and Selective Phosphodiesterase 10A Inhibitors | 4fcb | 2.9 |
15 | pfj | Crystal structure of the catalytic domain of rat phosphodiesterase 10A | 2ovy | 4 |
16 | 2f5 | Crystal Structure of PDE10A with Novel Keto-Benzimidazole Inhibitor | 4mvh | 4.5 |
17 | 4y2 | PDE10 complexed with 6-chloro-2-cyclopropyl-N-[(2,4-dimethylthiazol-5-yl)methyl]-5-methyl-pyrimidin-4-amine | 5c2a | 4.8 |
18 | 0jq | PDE10a Crystal Structure Complexed with Novel Inhibitor | 4ddl | 4.9 |
19 | 490 | Crystal structure of PDE10A in complex with ASP9436 | 4xy2 | 8 |
20 | 2f4 | Crystal Structure of PDE10A with Novel Keto-Benzimidazole Inhibitor | 4muw | 9.7 |
21 | 546 | Highly Potent, Selective, and Orally Active Phosphodiestarase 10A Inhibitors | 3sni | 11 |
22 | pf6 | Discovery of novel inhibitors of PDE10A | 3hqy | 11.5 |
23 | pfw | Structure of PDE10-inhibitor complex | 3qpp | 12 |
24 | pfh | Crystal structure of the catalytic domain of rat phosphodiesterase 10A | 2ovv | 12 |
25 | 4hn | PDE10A in complex with the inhibitor AZ5 | 4ael | 12 |
26 | axc | Triazoloquinazolines as a novel class of phosphodiesterase 10A (PDE10A) inhibitors, part 2, Lead-optimisation. | 2y0j | 12 |
27 | pfk | Structure of PDE10-inhibitor complex | 3qpn | 17 |
28 | 227 | Crystal structure of the catalytic domain of rat phosphodiesterase 10A | 2o8h | 25 |
29 | 8q7 | Crystal structure of human PDE10A in complex with inhibitor 16d | 5uwf | 59 |
30 | ev1 | Human PDE-papaverine complex obtained by ligand soaking of cross- linked protein crystals | 2wey | 76 |
31 | x4c | Crystal structure of PDE10A in complex with a benzimidazole inhibitor | 3ws8 | 210 |
32 | pfr | Structure of PDE10-inhibitor complex | 3qpo | 247 |
33 | 4xy | PDE10 complexed with 6-chloro-2-cyclopropyl-5-methyl-N-propyl-pyrimidin-4-amine | 5c29 | 880 |