Found 4 hits Enzyme Inhibition Constant Data 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
(313/334 = 94%)† (Rattus norvegicus (rat)) | BDBM98891
(US8497265, 217 | US8497265, 239)Show SMILES OCC1CCN(CC1)c1nccnc1OC1CN(C1)c1ccc2ccccc2n1 Show InChI InChI=1S/C22H25N5O2/c28-15-16-7-11-26(12-8-16)21-22(24-10-9-23-21)29-18-13-27(14-18)20-6-5-17-3-1-2-4-19(17)25-20/h1-6,9-10,16,18,28H,7-8,11-15H2 | PDB MMDB
Reactome pathway KEGG
UniProtKB/SwissProt
B.MOAD GoogleScholar AffyNet
| PC cid PC sid PDB UniChem
Similars
| PDB US Patent
| n/a | n/a | 2.30 | n/a | n/a | n/a | n/a | n/a | n/a |
Amgen Inc.
US Patent
| Assay Description Enzyme activity: An IMAP TR-FRET assay was used to analyze the enzyme activity (Molecular Devices Corp., Sunnyvale, Calif). |
US Patent US8497265 (2013)
BindingDB Entry DOI: 10.7270/Q2VD6X39 |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A
(338/338 = 100%)† (Homo sapiens (Human)) | BDBM98891
(US8497265, 217 | US8497265, 239)Show SMILES OCC1CCN(CC1)c1nccnc1OC1CN(C1)c1ccc2ccccc2n1 Show InChI InChI=1S/C22H25N5O2/c28-15-16-7-11-26(12-8-16)21-22(24-10-9-23-21)29-18-13-27(14-18)20-6-5-17-3-1-2-4-19(17)25-20/h1-6,9-10,16,18,28H,7-8,11-15H2 | PDB MMDB
Reactome pathway KEGG
UniProtKB/SwissProt
B.MOAD DrugBank antibodypedia GoogleScholar AffyNet
| PC cid PC sid PDB UniChem
Similars
| PDB Article PubMed
| n/a | n/a | 2.40 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
Curated by ChEMBL
| Assay Description Inhibition of human PDE10A2 using FAM-cAMP substrate by TR-FRET progressive binding assay |
Bioorg Med Chem 22: 6570-85 (2015)
Article DOI: 10.1016/j.bmc.2014.10.013 BindingDB Entry DOI: 10.7270/Q2RB766Q |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A
(313/334 = 94%)† (Rattus norvegicus (rat)) | BDBM98891
(US8497265, 217 | US8497265, 239)Show SMILES OCC1CCN(CC1)c1nccnc1OC1CN(C1)c1ccc2ccccc2n1 Show InChI InChI=1S/C22H25N5O2/c28-15-16-7-11-26(12-8-16)21-22(24-10-9-23-21)29-18-13-27(14-18)20-6-5-17-3-1-2-4-19(17)25-20/h1-6,9-10,16,18,28H,7-8,11-15H2 | PDB MMDB
Reactome pathway KEGG
UniProtKB/SwissProt
B.MOAD GoogleScholar AffyNet
| PC cid PC sid PDB UniChem
Similars
| PDB US Patent
| n/a | n/a | 23.3 | n/a | n/a | n/a | n/a | n/a | n/a |
Amgen Inc.
US Patent
| Assay Description Enzyme activity: An IMAP TR-FRET assay was used to analyze the enzyme activity (Molecular Devices Corp., Sunnyvale, Calif). |
US Patent US8497265 (2013)
BindingDB Entry DOI: 10.7270/Q2VD6X39 |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A
(338/338 = 100%)† (Homo sapiens (Human)) | BDBM98891
(US8497265, 217 | US8497265, 239)Show SMILES OCC1CCN(CC1)c1nccnc1OC1CN(C1)c1ccc2ccccc2n1 Show InChI InChI=1S/C22H25N5O2/c28-15-16-7-11-26(12-8-16)21-22(24-10-9-23-21)29-18-13-27(14-18)20-6-5-17-3-1-2-4-19(17)25-20/h1-6,9-10,16,18,28H,7-8,11-15H2 | PDB MMDB
Reactome pathway KEGG
UniProtKB/SwissProt
B.MOAD DrugBank antibodypedia GoogleScholar AffyNet
| PC cid PC sid PDB UniChem
Similars
| PDB Article PubMed
| n/a | n/a | 2.40E+3 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
Curated by ChEMBL
| Assay Description Inhibition of human PDE10A using FAM-cAMP substrate by TR-FRET progressive binding assay |
Bioorg Med Chem 22: 6570-85 (2015)
Article DOI: 10.1016/j.bmc.2014.10.013 BindingDB Entry DOI: 10.7270/Q2RB766Q |
More data for this Ligand-Target Pair | 3D Structure (crystal) |