Found 25 hits Enz. Inhib. hit(s) with Target = 'Metabotropic glutamate receptor 2' and Ligand = 'BDBM17657' 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 |
Metabotropic glutamate receptor 2
(Homo sapiens (Human)) | BDBM17657
((2S)-2-aminopentanedioic acid | (S)-Glu | D-Glutam...)Show InChI InChI=1S/C5H9NO4/c6-3(5(9)10)1-2-4(7)8/h3H,1-2,6H2,(H,7,8)(H,9,10)/t3-/m0/s1 | PDB
UniProtKB/SwissProt
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Patents
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| PubMed
| 1.10E+3 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
F. Hoffmann-La Roche Ltd.
Curated by PDSP Ki Database
| |
Mol Pharmacol 53: 228-33 (1998)
BindingDB Entry DOI: 10.7270/Q2MP51T5 |
More data for this Ligand-Target Pair | |
Metabotropic glutamate receptor 2
(Homo sapiens (Human)) | BDBM17657
((2S)-2-aminopentanedioic acid | (S)-Glu | D-Glutam...)Show InChI InChI=1S/C5H9NO4/c6-3(5(9)10)1-2-4(7)8/h3H,1-2,6H2,(H,7,8)(H,9,10)/t3-/m0/s1 | PDB
UniProtKB/SwissProt
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| Article PubMed
| 1.26E+3 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Case Western Reserve University
Curated by PDSP Ki Database
| |
J Pharmacol Exp Ther 305: 131-42 (2003)
Article DOI: 10.1124/jpet.102.047092 BindingDB Entry DOI: 10.7270/Q2VT1QN7 |
More data for this Ligand-Target Pair | |
Metabotropic glutamate receptor 2
(Homo sapiens (Human)) | BDBM17657
((2S)-2-aminopentanedioic acid | (S)-Glu | D-Glutam...)Show InChI InChI=1S/C5H9NO4/c6-3(5(9)10)1-2-4(7)8/h3H,1-2,6H2,(H,7,8)(H,9,10)/t3-/m0/s1 | PDB
UniProtKB/SwissProt
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Patents
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| Article PubMed
| 4.00E+3 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Emory University
Curated by PDSP Ki Database
| |
Annu Rev Pharmacol Toxicol 37: 205-37 (1997)
Article DOI: 10.1146/annurev.pharmtox.37.1.205 BindingDB Entry DOI: 10.7270/Q2M043ZH |
More data for this Ligand-Target Pair | |
Metabotropic glutamate receptor 2
(Homo sapiens (Human)) | BDBM17657
((2S)-2-aminopentanedioic acid | (S)-Glu | D-Glutam...)Show InChI InChI=1S/C5H9NO4/c6-3(5(9)10)1-2-4(7)8/h3H,1-2,6H2,(H,7,8)(H,9,10)/t3-/m0/s1 | PDB
UniProtKB/SwissProt
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Patents
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| Article PubMed
| 4.40E+3 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
The Royal Danish School of Pharmacy
Curated by PDSP Ki Database
| |
Eur J Pharmacol 350: 311-6 (1998)
Article DOI: 10.1016/s0014-2999(98)00246-5 BindingDB Entry DOI: 10.7270/Q2FT8JK6 |
More data for this Ligand-Target Pair | |
Metabotropic glutamate receptor 2
(Homo sapiens (Human)) | BDBM17657
((2S)-2-aminopentanedioic acid | (S)-Glu | D-Glutam...)Show InChI InChI=1S/C5H9NO4/c6-3(5(9)10)1-2-4(7)8/h3H,1-2,6H2,(H,7,8)(H,9,10)/t3-/m0/s1 | PDB
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| Article PubMed
| 6.40E+3 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Universit£ di Salerno
Curated by ChEMBL
| Assay Description Displacement of [3H]Quisqualate from human mGluR2 receptor expressed in BHK cells |
Bioorg Med Chem 17: 242-50 (2008)
Article DOI: 10.1016/j.bmc.2008.11.015 BindingDB Entry DOI: 10.7270/Q2HD7WKF |
More data for this Ligand-Target Pair | |
Metabotropic glutamate receptor 2
(Homo sapiens (Human)) | BDBM17657
((2S)-2-aminopentanedioic acid | (S)-Glu | D-Glutam...)Show InChI InChI=1S/C5H9NO4/c6-3(5(9)10)1-2-4(7)8/h3H,1-2,6H2,(H,7,8)(H,9,10)/t3-/m0/s1 | PDB
UniProtKB/SwissProt
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| >1.00E+4 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
UPR Centre
Curated by PDSP Ki Database
| |
Mol Pharmacol 50: 923-30 (1996)
BindingDB Entry DOI: 10.7270/Q2M61HS5 |
More data for this Ligand-Target Pair | |
Metabotropic glutamate receptor 2
(Homo sapiens (Human)) | BDBM17657
((2S)-2-aminopentanedioic acid | (S)-Glu | D-Glutam...)Show InChI InChI=1S/C5H9NO4/c6-3(5(9)10)1-2-4(7)8/h3H,1-2,6H2,(H,7,8)(H,9,10)/t3-/m0/s1 | PDB
UniProtKB/SwissProt
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| Article PubMed
| 1.10E+4 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
Universit£ di Perugia
Curated by ChEMBL
| Assay Description Displacement of [3H]LY341495 from mGluR2 receptor expressed in BHK cells |
J Med Chem 50: 4630-41 (2007)
Article DOI: 10.1021/jm070322e BindingDB Entry DOI: 10.7270/Q2DF6S12 |
More data for this Ligand-Target Pair | |
Metabotropic glutamate receptor 2
(Homo sapiens (Human)) | BDBM17657
((2S)-2-aminopentanedioic acid | (S)-Glu | D-Glutam...)Show InChI InChI=1S/C5H9NO4/c6-3(5(9)10)1-2-4(7)8/h3H,1-2,6H2,(H,7,8)(H,9,10)/t3-/m0/s1 | PDB
UniProtKB/SwissProt
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| PubMed
| 1.20E+4 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
The Royal Danish School of Pharmacy
Curated by ChEMBL
| Assay Description Potency against cloned Metabotropic glutamate receptor 2 agonist |
J Med Chem 43: 2609-45 (2000)
BindingDB Entry DOI: 10.7270/Q2DZ090Q |
More data for this Ligand-Target Pair | |
Metabotropic glutamate receptor 2
(Homo sapiens (Human)) | BDBM17657
((2S)-2-aminopentanedioic acid | (S)-Glu | D-Glutam...)Show InChI InChI=1S/C5H9NO4/c6-3(5(9)10)1-2-4(7)8/h3H,1-2,6H2,(H,7,8)(H,9,10)/t3-/m0/s1 | PDB
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Patents
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| Article PubMed
| n/a | n/a | n/a | n/a | 2.35E+3 | n/a | n/a | n/a | n/a |
Eli Lilly and Company
Curated by ChEMBL
| Assay Description Agonist activity at human recombinant mGlu2 receptor E273D mutant expressed in AV12 cells assessed as stimulation of Ca2+ mobilization after 1 hr by ... |
J Med Chem 58: 7526-48 (2015)
Article DOI: 10.1021/acs.jmedchem.5b01124 BindingDB Entry DOI: 10.7270/Q29S1ST0 |
More data for this Ligand-Target Pair | |
Metabotropic glutamate receptor 2
(Homo sapiens (Human)) | BDBM17657
((2S)-2-aminopentanedioic acid | (S)-Glu | D-Glutam...)Show InChI InChI=1S/C5H9NO4/c6-3(5(9)10)1-2-4(7)8/h3H,1-2,6H2,(H,7,8)(H,9,10)/t3-/m0/s1 | PDB
UniProtKB/SwissProt
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Patents
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| Article PubMed
| n/a | n/a | n/a | n/a | 1.77E+3 | n/a | n/a | n/a | n/a |
Eli Lilly and Company
Curated by ChEMBL
| Assay Description Agonist activity at human recombinant mGlu2 receptor L300Q mutant expressed in AV12 cells assessed as stimulation of Ca2+ mobilization after 1 hr by ... |
J Med Chem 58: 7526-48 (2015)
Article DOI: 10.1021/acs.jmedchem.5b01124 BindingDB Entry DOI: 10.7270/Q29S1ST0 |
More data for this Ligand-Target Pair | |
Metabotropic glutamate receptor 2
(Homo sapiens (Human)) | BDBM17657
((2S)-2-aminopentanedioic acid | (S)-Glu | D-Glutam...)Show InChI InChI=1S/C5H9NO4/c6-3(5(9)10)1-2-4(7)8/h3H,1-2,6H2,(H,7,8)(H,9,10)/t3-/m0/s1 | PDB
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| Article PubMed
| n/a | n/a | n/a | n/a | 1.82E+3 | n/a | n/a | n/a | n/a |
University of Copenhagen
Curated by ChEMBL
| Assay Description Agonist activity at rat mGlu2 receptor expressed in HEK293 cells by [35S]GTP-gamma binding assay |
J Med Chem 59: 914-24 (2016)
Article DOI: 10.1021/acs.jmedchem.5b01333 BindingDB Entry DOI: 10.7270/Q2000408 |
More data for this Ligand-Target Pair | |
Metabotropic glutamate receptor 2
(Homo sapiens (Human)) | BDBM17657
((2S)-2-aminopentanedioic acid | (S)-Glu | D-Glutam...)Show InChI InChI=1S/C5H9NO4/c6-3(5(9)10)1-2-4(7)8/h3H,1-2,6H2,(H,7,8)(H,9,10)/t3-/m0/s1 | PDB
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| Article PubMed
| n/a | n/a | n/a | n/a | 1.80E+3 | n/a | n/a | n/a | n/a |
University of Copenhagen
Curated by ChEMBL
| Assay Description Agonist activity at rat mGlu2 receptor expressed in HEK293 cells by [35S]GTP-gamma binding assay |
J Med Chem 59: 914-24 (2016)
Article DOI: 10.1021/acs.jmedchem.5b01333 BindingDB Entry DOI: 10.7270/Q2000408 |
More data for this Ligand-Target Pair | |
Metabotropic glutamate receptor 2
(Homo sapiens (Human)) | BDBM17657
((2S)-2-aminopentanedioic acid | (S)-Glu | D-Glutam...)Show InChI InChI=1S/C5H9NO4/c6-3(5(9)10)1-2-4(7)8/h3H,1-2,6H2,(H,7,8)(H,9,10)/t3-/m0/s1 | PDB
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| Article PubMed
| n/a | n/a | n/a | n/a | 1.31E+4 | n/a | n/a | n/a | n/a |
University of Copenhagen
Curated by ChEMBL
| Assay Description Agonist activity at rat mGlu2 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assay |
J Med Chem 59: 914-24 (2016)
Article DOI: 10.1021/acs.jmedchem.5b01333 BindingDB Entry DOI: 10.7270/Q2000408 |
More data for this Ligand-Target Pair | |
Metabotropic glutamate receptor 2
(Homo sapiens (Human)) | BDBM17657
((2S)-2-aminopentanedioic acid | (S)-Glu | D-Glutam...)Show InChI InChI=1S/C5H9NO4/c6-3(5(9)10)1-2-4(7)8/h3H,1-2,6H2,(H,7,8)(H,9,10)/t3-/m0/s1 | PDB
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| Article PubMed
| n/a | n/a | n/a | n/a | 1.61E+4 | n/a | n/a | n/a | n/a |
University of Copenhagen
Curated by ChEMBL
| Assay Description Agonist activity at rat mGlu2 receptor by FRET based mGlu sensor assay |
J Med Chem 59: 914-24 (2016)
Article DOI: 10.1021/acs.jmedchem.5b01333 BindingDB Entry DOI: 10.7270/Q2000408 |
More data for this Ligand-Target Pair | |
Metabotropic glutamate receptor 2
(Homo sapiens (Human)) | BDBM17657
((2S)-2-aminopentanedioic acid | (S)-Glu | D-Glutam...)Show InChI InChI=1S/C5H9NO4/c6-3(5(9)10)1-2-4(7)8/h3H,1-2,6H2,(H,7,8)(H,9,10)/t3-/m0/s1 | PDB
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Patents
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| PubMed
| n/a | n/a | n/a | n/a | 7.40E+3 | n/a | n/a | n/a | n/a |
Universit£ di Perugia
Curated by ChEMBL
| Assay Description Antagonistic activity against stimulation of GTP (gamma) 35 S binding by glutamate in membranes from CHO cells expressing human mGluR2 |
Bioorg Med Chem Lett 11: 3179-82 (2001)
BindingDB Entry DOI: 10.7270/Q27M08H1 |
More data for this Ligand-Target Pair | |
Metabotropic glutamate receptor 2
(Homo sapiens (Human)) | BDBM17657
((2S)-2-aminopentanedioic acid | (S)-Glu | D-Glutam...)Show InChI InChI=1S/C5H9NO4/c6-3(5(9)10)1-2-4(7)8/h3H,1-2,6H2,(H,7,8)(H,9,10)/t3-/m0/s1 | PDB
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Patents
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| PubMed
| n/a | n/a | n/a | n/a | 4.00E+3 | n/a | n/a | n/a | n/a |
CNS Research
Curated by ChEMBL
| Assay Description Concentration for half maximal activation of metabotropic glutamate mGluR2 in rat |
J Med Chem 38: 1417-26 (1995)
BindingDB Entry DOI: 10.7270/Q20R9Q1R |
More data for this Ligand-Target Pair | |
Metabotropic glutamate receptor 2
(Homo sapiens (Human)) | BDBM17657
((2S)-2-aminopentanedioic acid | (S)-Glu | D-Glutam...)Show InChI InChI=1S/C5H9NO4/c6-3(5(9)10)1-2-4(7)8/h3H,1-2,6H2,(H,7,8)(H,9,10)/t3-/m0/s1 | PDB
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Patents
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| PubMed
| n/a | n/a | n/a | n/a | 4.70E+3 | n/a | n/a | n/a | n/a |
CNS Research
Curated by ChEMBL
| Assay Description Concentration for half maximal activation of metabotropic glutamate mGluR2 in human |
J Med Chem 38: 1417-26 (1995)
BindingDB Entry DOI: 10.7270/Q20R9Q1R |
More data for this Ligand-Target Pair | |
Metabotropic glutamate receptor 2
(Homo sapiens (Human)) | BDBM17657
((2S)-2-aminopentanedioic acid | (S)-Glu | D-Glutam...)Show InChI InChI=1S/C5H9NO4/c6-3(5(9)10)1-2-4(7)8/h3H,1-2,6H2,(H,7,8)(H,9,10)/t3-/m0/s1 | PDB
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Patents
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| Article PubMed
| n/a | n/a | n/a | n/a | 8.50E+3 | n/a | n/a | n/a | n/a |
Royal Danish School of Pharmacy
Curated by ChEMBL
| Assay Description Agonistic activity at mGlu2 receptor expressed in CHO cells |
J Med Chem 39: 3188-94 (1996)
Article DOI: 10.1021/jm9602569 BindingDB Entry DOI: 10.7270/Q2M909BH |
More data for this Ligand-Target Pair | |
Metabotropic glutamate receptor 2
(Homo sapiens (Human)) | BDBM17657
((2S)-2-aminopentanedioic acid | (S)-Glu | D-Glutam...)Show InChI InChI=1S/C5H9NO4/c6-3(5(9)10)1-2-4(7)8/h3H,1-2,6H2,(H,7,8)(H,9,10)/t3-/m0/s1 | PDB
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Patents
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| Article PubMed
| n/a | n/a | n/a | n/a | 2.60E+4 | n/a | n/a | n/a | n/a |
Universit£ di Perugia
Curated by ChEMBL
| Assay Description Activity at human mGluR2 from BHK cells in [35S]GTP-gamma-S stimulation assay |
Bioorg Med Chem Lett 16: 196-9 (2005)
Article DOI: 10.1016/j.bmcl.2005.09.014 BindingDB Entry DOI: 10.7270/Q2DZ0932 |
More data for this Ligand-Target Pair | |
Metabotropic glutamate receptor 2
(Rattus norvegicus) | BDBM17657
((2S)-2-aminopentanedioic acid | (S)-Glu | D-Glutam...)Show InChI InChI=1S/C5H9NO4/c6-3(5(9)10)1-2-4(7)8/h3H,1-2,6H2,(H,7,8)(H,9,10)/t3-/m0/s1 | PDB
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Patents
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| PubMed
| n/a | n/a | n/a | n/a | 1.60E+4 | n/a | n/a | n/a | n/a |
Universit£ Ren£ Descartes
Curated by ChEMBL
| Assay Description Agonist activity in rat at Metabotropic glutamate receptor 2 expressed in HEK293 cells |
Bioorg Med Chem Lett 11: 1569-72 (2001)
BindingDB Entry DOI: 10.7270/Q2M61KRJ |
More data for this Ligand-Target Pair | |
Metabotropic glutamate receptor 2
(Homo sapiens (Human)) | BDBM17657
((2S)-2-aminopentanedioic acid | (S)-Glu | D-Glutam...)Show InChI InChI=1S/C5H9NO4/c6-3(5(9)10)1-2-4(7)8/h3H,1-2,6H2,(H,7,8)(H,9,10)/t3-/m0/s1 | PDB
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Patents
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| Article PubMed
| n/a | n/a | n/a | n/a | 2.60E+4 | n/a | n/a | n/a | n/a |
Universit£ di Perugia
Curated by ChEMBL
| Assay Description Activity at human recombinant mGluR2 expressed in BHK cells assessed as stimulation of [35S]GTP-gamma-S binding |
Bioorg Med Chem 15: 3161-70 (2007)
Article DOI: 10.1016/j.bmc.2007.02.040 BindingDB Entry DOI: 10.7270/Q2CN74RR |
More data for this Ligand-Target Pair | |
Metabotropic glutamate receptor 2
(Rattus norvegicus) | BDBM17657
((2S)-2-aminopentanedioic acid | (S)-Glu | D-Glutam...)Show InChI InChI=1S/C5H9NO4/c6-3(5(9)10)1-2-4(7)8/h3H,1-2,6H2,(H,7,8)(H,9,10)/t3-/m0/s1 | PDB
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| PubMed
| n/a | n/a | n/a | n/a | 610 | n/a | n/a | n/a | n/a |
Georgetown University Medical Center
Curated by ChEMBL
| Assay Description Agonistic activity evaluated in CHO(Chinese hamster ovary) cells expressing mGluR2 receptor |
Bioorg Med Chem Lett 9: 1721-6 (1999)
BindingDB Entry DOI: 10.7270/Q2V69K37 |
More data for this Ligand-Target Pair | |
Metabotropic glutamate receptor 2
(Homo sapiens (Human)) | BDBM17657
((2S)-2-aminopentanedioic acid | (S)-Glu | D-Glutam...)Show InChI InChI=1S/C5H9NO4/c6-3(5(9)10)1-2-4(7)8/h3H,1-2,6H2,(H,7,8)(H,9,10)/t3-/m0/s1 | PDB
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DrugBank MCE KEGG MMDB PC cid PC sid PDB UniChem
Patents
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| PubMed
| n/a | n/a | n/a | n/a | 4.00E+3 | n/a | n/a | n/a | n/a |
CNS Research
Curated by ChEMBL
| Assay Description Concentration for half maximal activation of metabotropic glutamate mGluR2 in rat |
J Med Chem 38: 1417-26 (1995)
BindingDB Entry DOI: 10.7270/Q20R9Q1R |
More data for this Ligand-Target Pair | |
Metabotropic glutamate receptor 2
(Homo sapiens (Human)) | BDBM17657
((2S)-2-aminopentanedioic acid | (S)-Glu | D-Glutam...)Show InChI InChI=1S/C5H9NO4/c6-3(5(9)10)1-2-4(7)8/h3H,1-2,6H2,(H,7,8)(H,9,10)/t3-/m0/s1 | PDB
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DrugBank MCE KEGG MMDB PC cid PC sid PDB UniChem
Patents
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| Article PubMed
| n/a | n/a | n/a | n/a | 2.58E+3 | n/a | n/a | n/a | n/a |
Eli Lilly and Company
Curated by ChEMBL
| Assay Description Agonist activity at human recombinant mGlu2 receptor E273D and L300Q mutant expressed in AV12 cells assessed as stimulation of Ca2+ mobilization afte... |
J Med Chem 58: 7526-48 (2015)
Article DOI: 10.1021/acs.jmedchem.5b01124 BindingDB Entry DOI: 10.7270/Q29S1ST0 |
More data for this Ligand-Target Pair | |
Metabotropic glutamate receptor 2
(Homo sapiens (Human)) | BDBM17657
((2S)-2-aminopentanedioic acid | (S)-Glu | D-Glutam...)Show InChI InChI=1S/C5H9NO4/c6-3(5(9)10)1-2-4(7)8/h3H,1-2,6H2,(H,7,8)(H,9,10)/t3-/m0/s1 | PDB
UniProtKB/SwissProt
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DrugBank MCE KEGG MMDB PC cid PC sid PDB UniChem
Patents
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| Article PubMed
| n/a | n/a | n/a | n/a | 1.83E+3 | n/a | n/a | n/a | n/a |
Eli Lilly and Company
Curated by ChEMBL
| Assay Description Agonist activity at wild type human recombinant mGlu2 receptor expressed in AV12 cells assessed as stimulation of Ca2+ mobilization after 1 hr by FLI... |
J Med Chem 58: 7526-48 (2015)
Article DOI: 10.1021/acs.jmedchem.5b01124 BindingDB Entry DOI: 10.7270/Q29S1ST0 |
More data for this Ligand-Target Pair | |