Found 21 hits Enz. Inhib. hit(s) with Target = 'cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A' and Ligand = 'BDBM14754' Target/Host (Institution) | Ligand | Target/Host Links | Ligand Links | Trg + Lig Links | Ki nM | ΔG° kJ/mole | IC50 nM | Kd nM | EC50/IC50 nM | koff s-1 | kon M-1s-1 | pH | Temp °C |
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A
(Rattus norvegicus (rat)) | BDBM14754
(1-[(3,4-dimethoxyphenyl)methyl]-6,7-dimethoxy-isoq...)Show InChI InChI=1S/C20H21NO4/c1-22-17-6-5-13(10-18(17)23-2)9-16-15-12-20(25-4)19(24-3)11-14(15)7-8-21-16/h5-8,10-12H,9H2,1-4H3 | PDB MMDB
Reactome pathway KEGG
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| PDB Article PubMed
| 17 | -43.9 | n/a | n/a | n/a | n/a | n/a | 7.5 | 22 |
Pfizer
| Assay Description PDE activity was monitored by measuring the hydrolysis of [3H]-cAMP to [3H]-AMP using a scintillation proximity assay (SPA). [3H]-AMP was captured by... |
J Med Chem 50: 182-5 (2007)
Article DOI: 10.1021/jm060653b BindingDB Entry DOI: 10.7270/Q2930RDX |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A
(Homo sapiens (Human)) | BDBM14754
(1-[(3,4-dimethoxyphenyl)methyl]-6,7-dimethoxy-isoq...)Show InChI InChI=1S/C20H21NO4/c1-22-17-6-5-13(10-18(17)23-2)9-16-15-12-20(25-4)19(24-3)11-14(15)7-8-21-16/h5-8,10-12H,9H2,1-4H3 | PDB MMDB
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| n/a | n/a | 17 | n/a | n/a | n/a | n/a | n/a | n/a |
Universit£ di Sassari
Curated by ChEMBL
| Assay Description Inhibition of human PDE10A expressed in Sf9 cells using [3H]cAMP by scintillation proximity assay |
Bioorg Med Chem 19: 642-9 (2011)
Article DOI: 10.1016/j.bmc.2010.10.038 BindingDB Entry DOI: 10.7270/Q2TT4R73 |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A
(Homo sapiens (Human)) | BDBM14754
(1-[(3,4-dimethoxyphenyl)methyl]-6,7-dimethoxy-isoq...)Show InChI InChI=1S/C20H21NO4/c1-22-17-6-5-13(10-18(17)23-2)9-16-15-12-20(25-4)19(24-3)11-14(15)7-8-21-16/h5-8,10-12H,9H2,1-4H3 | PDB MMDB
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| n/a | n/a | 21 | n/a | n/a | n/a | n/a | n/a | n/a |
Washington University
Curated by ChEMBL
| Assay Description Inhibition of human recombinant PDE10A assessed as reduction in hydrolysis of [3H]cAMP by scintillation proximity assay |
Eur J Med Chem 46: 3986-95 (2011)
Article DOI: 10.1016/j.ejmech.2011.05.072 BindingDB Entry DOI: 10.7270/Q279452C |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A
(Rattus norvegicus (rat)) | BDBM14754
(1-[(3,4-dimethoxyphenyl)methyl]-6,7-dimethoxy-isoq...)Show InChI InChI=1S/C20H21NO4/c1-22-17-6-5-13(10-18(17)23-2)9-16-15-12-20(25-4)19(24-3)11-14(15)7-8-21-16/h5-8,10-12H,9H2,1-4H3 | PDB MMDB
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| n/a | n/a | 36 | n/a | n/a | n/a | n/a | n/a | n/a |
AstraZeneca
Curated by ChEMBL
| Assay Description Competitive inhibition of rat recombinant PDE10A by scintillation proximity assay in presence of cAMP |
Bioorg Med Chem Lett 26: 197-202 (2016)
Article DOI: 10.1016/j.bmcl.2015.10.100 BindingDB Entry DOI: 10.7270/Q21Z47FT |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A
(Rattus norvegicus (rat)) | BDBM14754
(1-[(3,4-dimethoxyphenyl)methyl]-6,7-dimethoxy-isoq...)Show InChI InChI=1S/C20H21NO4/c1-22-17-6-5-13(10-18(17)23-2)9-16-15-12-20(25-4)19(24-3)11-14(15)7-8-21-16/h5-8,10-12H,9H2,1-4H3 | PDB MMDB
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| PDB Article PubMed
| n/a | n/a | 36 | n/a | n/a | n/a | n/a | n/a | n/a |
Asubio Pharma Co., Ltd.
Curated by ChEMBL
| Assay Description Inhibition of recombinant rat PDE10A expressed in Sf9 cells using cGMP/cAMP as substrate by scintillation proximity assay |
Bioorg Med Chem Lett 29: 1419-1422 (2019)
Article DOI: 10.1016/j.bmcl.2019.03.021 BindingDB Entry DOI: 10.7270/Q2PK0KFJ |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A
(Homo sapiens (Human)) | BDBM14754
(1-[(3,4-dimethoxyphenyl)methyl]-6,7-dimethoxy-isoq...)Show InChI InChI=1S/C20H21NO4/c1-22-17-6-5-13(10-18(17)23-2)9-16-15-12-20(25-4)19(24-3)11-14(15)7-8-21-16/h5-8,10-12H,9H2,1-4H3 | PDB MMDB
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| n/a | n/a | 36 | n/a | n/a | n/a | n/a | n/a | n/a |
Washington University School of Medicine
Curated by ChEMBL
| Assay Description Binding affinity to PDE10A (unknown origin) |
Bioorg Med Chem Lett 25: 919-24 (2015)
Article DOI: 10.1016/j.bmcl.2014.12.054 BindingDB Entry DOI: 10.7270/Q2H41T6N |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A
(Homo sapiens (Human)) | BDBM14754
(1-[(3,4-dimethoxyphenyl)methyl]-6,7-dimethoxy-isoq...)Show InChI InChI=1S/C20H21NO4/c1-22-17-6-5-13(10-18(17)23-2)9-16-15-12-20(25-4)19(24-3)11-14(15)7-8-21-16/h5-8,10-12H,9H2,1-4H3 | PDB MMDB
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| DrugBank PDB Article PubMed
| n/a | n/a | 36 | n/a | n/a | n/a | n/a | n/a | n/a |
Washington University School of Medicine
Curated by ChEMBL
| Assay Description Inhibition of PDE10A (unknown origin) |
Bioorg Med Chem 22: 2648-54 (2014)
Article DOI: 10.1016/j.bmc.2014.03.028 BindingDB Entry DOI: 10.7270/Q26M38C2 |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A
(Homo sapiens (Human)) | BDBM14754
(1-[(3,4-dimethoxyphenyl)methyl]-6,7-dimethoxy-isoq...)Show InChI InChI=1S/C20H21NO4/c1-22-17-6-5-13(10-18(17)23-2)9-16-15-12-20(25-4)19(24-3)11-14(15)7-8-21-16/h5-8,10-12H,9H2,1-4H3 | PDB MMDB
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| n/a | n/a | 36 | n/a | n/a | n/a | n/a | n/a | n/a |
Mitsubishi Tanabe Pharma Corporation
Curated by ChEMBL
| Assay Description Inhibition of PDE10A (unknown origin) |
Bioorg Med Chem 27: 3440-3450 (2019)
Article DOI: 10.1016/j.bmc.2019.06.021 BindingDB Entry DOI: 10.7270/Q2SB492B |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A
(Rattus norvegicus (rat)) | BDBM14754
(1-[(3,4-dimethoxyphenyl)methyl]-6,7-dimethoxy-isoq...)Show InChI InChI=1S/C20H21NO4/c1-22-17-6-5-13(10-18(17)23-2)9-16-15-12-20(25-4)19(24-3)11-14(15)7-8-21-16/h5-8,10-12H,9H2,1-4H3 | PDB MMDB
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| n/a | n/a | 36 | n/a | n/a | n/a | n/a | n/a | n/a |
Washington University
Curated by ChEMBL
| Assay Description Inhibition of rat PDE10A |
Eur J Med Chem 46: 3986-95 (2011)
Article DOI: 10.1016/j.ejmech.2011.05.072 BindingDB Entry DOI: 10.7270/Q279452C |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A
(Homo sapiens (Human)) | BDBM14754
(1-[(3,4-dimethoxyphenyl)methyl]-6,7-dimethoxy-isoq...)Show InChI InChI=1S/C20H21NO4/c1-22-17-6-5-13(10-18(17)23-2)9-16-15-12-20(25-4)19(24-3)11-14(15)7-8-21-16/h5-8,10-12H,9H2,1-4H3 | PDB MMDB
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| DrugBank PDB Article PubMed
| n/a | n/a | 36 | n/a | n/a | n/a | n/a | n/a | n/a |
AstraZeneca
Curated by ChEMBL
| Assay Description Inhibition of human recombinant full length PDE10A using cAMP as substrate preincubated for 20 mins measured after 4 hrs |
Bioorg Med Chem Lett 22: 1944-8 (2012)
Article DOI: 10.1016/j.bmcl.2012.01.046 BindingDB Entry DOI: 10.7270/Q2KH0NTP |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A
(Homo sapiens) | BDBM14754
(1-[(3,4-dimethoxyphenyl)methyl]-6,7-dimethoxy-isoq...)Show InChI InChI=1S/C20H21NO4/c1-22-17-6-5-13(10-18(17)23-2)9-16-15-12-20(25-4)19(24-3)11-14(15)7-8-21-16/h5-8,10-12H,9H2,1-4H3 | MMDB
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| | n/a | n/a | 36 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
| Assay Description Antagonist activity at CCK2 receptor in immature rat stomach assessed as pentagastrin-induced acid secretion |
Citation and Details
|
More data for this Ligand-Target Pair | |
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A
(Rattus norvegicus (rat)) | BDBM14754
(1-[(3,4-dimethoxyphenyl)methyl]-6,7-dimethoxy-isoq...)Show InChI InChI=1S/C20H21NO4/c1-22-17-6-5-13(10-18(17)23-2)9-16-15-12-20(25-4)19(24-3)11-14(15)7-8-21-16/h5-8,10-12H,9H2,1-4H3 | PDB MMDB
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| PDB Article PubMed
| n/a | n/a | 36 | n/a | n/a | n/a | n/a | n/a | n/a |
Sichuan Academy of Medical Science & Sichuan Provincial People's Hospital
Curated by ChEMBL
| Assay Description Inhibition of recombinant rat PDE10A expressed in Sf9 insect cells using cGMP or cAMP as substrate by scintillation proximity assay |
Eur J Med Chem 150: 742-756 (2018)
Article DOI: 10.1016/j.ejmech.2018.03.046 BindingDB Entry DOI: 10.7270/Q2JM2D83 |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A
(Homo sapiens (Human)) | BDBM14754
(1-[(3,4-dimethoxyphenyl)methyl]-6,7-dimethoxy-isoq...)Show InChI InChI=1S/C20H21NO4/c1-22-17-6-5-13(10-18(17)23-2)9-16-15-12-20(25-4)19(24-3)11-14(15)7-8-21-16/h5-8,10-12H,9H2,1-4H3 | PDB MMDB
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| n/a | n/a | 38 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
| Assay Description Inhibition of human recombinant PDE10A using cAMP as substrate incubated for 20 mins measured by Kinase Glo reagent based microplate reader assay |
Citation and Details
Article DOI: 10.1016/j.ejmech.2020.112854 BindingDB Entry DOI: 10.7270/Q2RJ4P6F |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A
(Homo sapiens (Human)) | BDBM14754
(1-[(3,4-dimethoxyphenyl)methyl]-6,7-dimethoxy-isoq...)Show InChI InChI=1S/C20H21NO4/c1-22-17-6-5-13(10-18(17)23-2)9-16-15-12-20(25-4)19(24-3)11-14(15)7-8-21-16/h5-8,10-12H,9H2,1-4H3 | PDB MMDB
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| DrugBank PDB Article PubMed
| n/a | n/a | 40 | n/a | n/a | n/a | n/a | n/a | n/a |
Pfizer Inc.
Curated by ChEMBL
| Assay Description Inhibition of PDE10A |
J Med Chem 55: 7299-331 (2012)
Article DOI: 10.1021/jm3004976 BindingDB Entry DOI: 10.7270/Q2C24XJK |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A
(Homo sapiens (Human)) | BDBM14754
(1-[(3,4-dimethoxyphenyl)methyl]-6,7-dimethoxy-isoq...)Show InChI InChI=1S/C20H21NO4/c1-22-17-6-5-13(10-18(17)23-2)9-16-15-12-20(25-4)19(24-3)11-14(15)7-8-21-16/h5-8,10-12H,9H2,1-4H3 | PDB MMDB
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| n/a | n/a | 56.9 | n/a | n/a | n/a | n/a | n/a | n/a |
Biotie Therapies GmbH
Curated by ChEMBL
| Assay Description Inhibition of human recombinant PDE10A expressed in baculovirus-SF21 cell system assessed as hydrolysis of [3H]cAMP after 1 hr by liquid scintillatio... |
J Med Chem 53: 4399-411 (2010)
Article DOI: 10.1021/jm1002793 BindingDB Entry DOI: 10.7270/Q2MK6D3N |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A
(Homo sapiens (Human)) | BDBM14754
(1-[(3,4-dimethoxyphenyl)methyl]-6,7-dimethoxy-isoq...)Show InChI InChI=1S/C20H21NO4/c1-22-17-6-5-13(10-18(17)23-2)9-16-15-12-20(25-4)19(24-3)11-14(15)7-8-21-16/h5-8,10-12H,9H2,1-4H3 | PDB MMDB
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| DrugBank PDB Article PubMed
| n/a | n/a | 56.9 | n/a | n/a | n/a | n/a | n/a | n/a |
Biotie Therapies GmbH
Curated by ChEMBL
| Assay Description Inhibition of human recombinant PDE10A expressed in baculovirus-SF21 cell system assessed as hydrolysis of [3H]cAMP after 1 hr by liquid scintillatio... |
J Med Chem 53: 4399-411 (2010)
Article DOI: 10.1021/jm1002793 BindingDB Entry DOI: 10.7270/Q2MK6D3N |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A
(Homo sapiens (Human)) | BDBM14754
(1-[(3,4-dimethoxyphenyl)methyl]-6,7-dimethoxy-isoq...)Show InChI InChI=1S/C20H21NO4/c1-22-17-6-5-13(10-18(17)23-2)9-16-15-12-20(25-4)19(24-3)11-14(15)7-8-21-16/h5-8,10-12H,9H2,1-4H3 | PDB MMDB
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| n/a | n/a | 76 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
| |
Citation and Details
Article DOI: 10.1016/j.ejmech.2022.114170 BindingDB Entry DOI: 10.7270/Q2RX9H3Q |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A
(Homo sapiens (Human)) | BDBM14754
(1-[(3,4-dimethoxyphenyl)methyl]-6,7-dimethoxy-isoq...)Show InChI InChI=1S/C20H21NO4/c1-22-17-6-5-13(10-18(17)23-2)9-16-15-12-20(25-4)19(24-3)11-14(15)7-8-21-16/h5-8,10-12H,9H2,1-4H3 | PDB MMDB
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| DrugBank PDB Article PubMed
| n/a | n/a | 97 | n/a | n/a | n/a | n/a | n/a | n/a |
Asubio Pharma Co., Ltd.
Curated by ChEMBL
| Assay Description Inhibition of human MOLT4 cell-derived PDE10A using [3H]cAMP as substrate measured after 2 hrs in presence of rolipram/milrinone by topcount method |
Bioorg Med Chem Lett 29: 1419-1422 (2019)
Article DOI: 10.1016/j.bmcl.2019.03.021 BindingDB Entry DOI: 10.7270/Q2PK0KFJ |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A
(Homo sapiens (Human)) | BDBM14754
(1-[(3,4-dimethoxyphenyl)methyl]-6,7-dimethoxy-isoq...)Show InChI InChI=1S/C20H21NO4/c1-22-17-6-5-13(10-18(17)23-2)9-16-15-12-20(25-4)19(24-3)11-14(15)7-8-21-16/h5-8,10-12H,9H2,1-4H3 | PDB MMDB
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| n/a | n/a | 210 | n/a | n/a | n/a | n/a | n/a | n/a |
H. Lundbeck A/S
Curated by ChEMBL
| Assay Description Inhibition of PDE10A |
Bioorg Med Chem Lett 21: 3738-42 (2011)
Article DOI: 10.1016/j.bmcl.2011.04.067 BindingDB Entry DOI: 10.7270/Q24B31PT |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A
(Homo sapiens (Human)) | BDBM14754
(1-[(3,4-dimethoxyphenyl)methyl]-6,7-dimethoxy-isoq...)Show InChI InChI=1S/C20H21NO4/c1-22-17-6-5-13(10-18(17)23-2)9-16-15-12-20(25-4)19(24-3)11-14(15)7-8-21-16/h5-8,10-12H,9H2,1-4H3 | PDB MMDB
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| DrugBank PDB Article PubMed
| n/a | n/a | 210 | n/a | n/a | n/a | n/a | n/a | n/a |
H. Lundbeck A/S
Curated by ChEMBL
| Assay Description Inhibition of PDE10A (unknown origin) |
Bioorg Med Chem 21: 6053-62 (2013)
Article DOI: 10.1016/j.bmc.2013.07.030 BindingDB Entry DOI: 10.7270/Q27P929Z |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A
(Homo sapiens (Human)) | BDBM14754
(1-[(3,4-dimethoxyphenyl)methyl]-6,7-dimethoxy-isoq...)Show InChI InChI=1S/C20H21NO4/c1-22-17-6-5-13(10-18(17)23-2)9-16-15-12-20(25-4)19(24-3)11-14(15)7-8-21-16/h5-8,10-12H,9H2,1-4H3 | PDB MMDB
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| n/a | n/a | 3.16E+3 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
| |
Citation and Details
Article DOI: 10.1016/j.ejmech.2022.114218 BindingDB Entry DOI: 10.7270/Q2TX3KDX |
More data for this Ligand-Target Pair | 3D Structure (crystal) |