MTEP [Ligand Id: 3336] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL292065 (MTEP)
  • mGlu1 receptor/Metabotropic glutamate receptor 1 in Human [ChEMBL: CHEMBL3772] [GtoPdb: 289] [UniProtKB: Q13255]
  • mGlu1 receptor/Metabotropic glutamate receptor 1 in Rat [ChEMBL: CHEMBL4477] [GtoPdb: 289] [UniProtKB: P23385]
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  • mGlu5 receptor/Metabotropic glutamate receptor 5 in Human [ChEMBL: CHEMBL3227] [GtoPdb: 293] [UniProtKB: P41594]
  • mGlu5 receptor/Metabotropic glutamate receptor 5 in Rat [ChEMBL: CHEMBL2564] [GtoPdb: 293] [UniProtKB: P31424]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
mGlu1 receptor/Metabotropic glutamate receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3772] [GtoPdb: 289] [UniProtKB: Q13255]
ChEMBL Tested for in vitro antagonistic activity against Metabotropic glutamate receptor 1 F 4 pIC50 >100000 nM IC50 J Med Chem (2003) 46: 204-206 [PMID:12519057]
mGlu1 receptor/Metabotropic glutamate receptor 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4477] [GtoPdb: 289] [UniProtKB: P23385]
ChEMBL Displacement of [3H]R214127 from rat cloned mGluR1 receptor expressed in CHO-T-Rex cells after 30 mins by liquid scintillation spectrometry B 5 pKi >10000 nM Ki Bioorg Med Chem (2015) 23: 3040-3058 [PMID:26014480]
ChEMBL Displacement of [3H]MPEP from rat mGlu1 receptor expressed in CHO-TREx cell membranes after 30 mins by liquid scintillation spectrometric analysis B 5 pKi >10000 nM Ki J Med Chem (2019) 62: 1246-1273 [PMID:30624919]
mGlu5 receptor/Metabotropic glutamate receptor 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3227] [GtoPdb: 293] [UniProtKB: P41594]
ChEMBL Displacement of [3H]MPEP from human cloned mGluR5 receptor expressed in CHO-T-Rex cells after 60 mins by liquid scintillation spectrometry B 7.49 pKi 32.7 nM Ki Bioorg Med Chem (2015) 23: 3040-3058 [PMID:26014480]
ChEMBL Displacement of [3H]MPEP from human mGlu5 receptor expressed in CHO-TREx cell membranes after 60 mins by liquid scintillation spectrometric analysis B 7.49 pKi 32.7 nM Ki J Med Chem (2019) 62: 1246-1273 [PMID:30624919]
GtoPdb - - 7.8 pKi 16 nM Ki Eur J Neurosci (2002) 16: 2241-4 [PMID:12473093]
ChEMBL Activity in agonist-induced phosphoinositide hydrolysis in CHO cells expressing mGluR5a F 6.34 pIC50 462 nM IC50 J Med Chem (2006) 49: 1080-1100 [PMID:16451073]
ChEMBL Antagonist activity against mGluR5 expressed in CHO cells assessed as inhibition of agonist-induced phosphoinositide hydrolysis F 6.34 pIC50 462 nM IC50 Bioorg Med Chem Lett (2006) 16: 3371-3375 [PMID:16678408]
ChEMBL Activity at human mGluR5 assessed as effect on glutamate-induced calcium ion mobilization by FLIPR F 7.11 pIC50 77 nM IC50 Bioorg Med Chem Lett (2006) 16: 4792-4795 [PMID:16839764]
ChEMBL Negative allosteric modulation of human mGlu5 receptor expressed in CHO-TREx cell membranes assessed as reduction in quisqualate-induced Ca2+ mobilization incubated for 18 hrs and measured every 1.5 secs intervals for 60 secs by Fluo-4/AM dye-based fluorescence analysis F 7.33 pIC50 47.3 nM IC50 J Med Chem (2019) 62: 1246-1273 [PMID:30624919]
ChEMBL Negative allosteric modulatory activity at human cloned mGluR5 receptor expressed in CHO-T-Rex cells assessed as inhibiton of quisqualate-induced calcium mobilization treated 10 mins prior to agonist application by fluorescence analysis F 7.33 pIC50 47.3 nM IC50 Bioorg Med Chem (2015) 23: 3040-3058 [PMID:26014480]
ChEMBL Negative allosteric modulation of human mGluR5 expressed in HEK293 cells assessed as calcium mobilization by FLIPR assay F 7.92 pIC50 12 nM IC50 Bioorg Med Chem Lett (2013) 23: 2134-2139 [PMID:23434029]
ChEMBL Inhibitory concentration against human recombinant metabotropic glutamate receptor 5 (mGlu5) in Ltk cells determined using fluorescence detection method B 8.3 pIC50 5 nM IC50 Bioorg Med Chem Lett (2005) 15: 1197-1200 [PMID:15686941]
ChEMBL Tested in vitro against human recombinant Metabotropic glutamate receptor 5 stably expressed in LtK cells by [Ca2+] flux assay using glutamate as antagonist F 8.3 pIC50 5 nM IC50 J Med Chem (2003) 46: 204-206 [PMID:12519057]
ChEMBL In vitro functional potency using an automated assay employing LtK-cells stably expressing human recombinant mGlu5 receptor by measuring changes in cytosolic [Ca2+] concentration F 8.3 pIC50 5 nM IC50 Bioorg Med Chem Lett (2003) 13: 351-354 [PMID:12565928]
ChEMBL In vitro potency against human recombinant mGlu5 receptor was determined by [Ca2+] flux assay using glutamate as agonist F 8.3 pIC50 5 nM IC50 Bioorg Med Chem Lett (2004) 14: 3993-3996 [PMID:15225713]
mGlu5 receptor/Metabotropic glutamate receptor 5 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2564] [GtoPdb: 293] [UniProtKB: P31424]
ChEMBL Displacement of [3H]MPEP from mGluR5 in Sprague-Dawley rat brain membrane after 60 mins by liquid scintillation counting B 7.38 pKi 42 nM Ki ACS Med Chem Lett (2012) 3: 544-549 [PMID:22924094]
ChEMBL Displacement of [3H]MPEP from mGluR5 receptor in Sprague-Dawley rat forebrain membrane after 60 mins by liquid scintillation spectrometry B 7.41 pKi 38.5 nM Ki Bioorg Med Chem (2015) 23: 3040-3058 [PMID:26014480]
ChEMBL Tested for displacement of [3H]3-methoxy-5-(pyridin-2-ylethynyl) pyridine from Metabotropic glutamate receptor 5 in rat cortical membrane B 7.8 pKi 16 nM Ki J Med Chem (2003) 46: 204-206 [PMID:12519057]
ChEMBL Displacement of [3H]methoxy-PEPY from rat mGluR5 expressed in human HEK-293 cells by liquid scintillation counting B 7.8 pKi 16 nM Ki Bioorg Med Chem Lett (2011) 21: 3243-3247 [PMID:21546249]
ChEMBL Displacement of [3HMPEP from rat cloned mGluR5 expressed in HEK293T cells by by scintillation counting B 7.8 pKi 16 nM Ki Bioorg Med Chem (2010) 18: 3026-3035 [PMID:20382541]
ChEMBL Displacement of [3H]-3-methoxy-5-(pyridin-2-ylethynyl)pyridine from mGlu5R in rat cortical membranes by liquid scintillation spectrometric analysis B 7.8 pKi 16 nM Ki Bioorg Med Chem Lett (2016) 26: 484-494 [PMID:26706173]
ChEMBL Displacement by compound of [3H]3-methoxy-5-(pyridin-2-ylethynyl)pyridine from rat cortical membranes B 7.92 pKi 12 nM Ki Bioorg Med Chem Lett (2004) 14: 3993-3996 [PMID:15225713]
ChEMBL Inverse agonist activity at rat mGluR5 expressed in HEK293A cells coexpressing Gqalpha assessed as inhibition of quisqualic-induced D-myo-inositol 1 production by ELISA F 6.96 pIC50 110 nM IC50 ACS Med Chem Lett (2012) 3: 544-549 [PMID:22924094]
ChEMBL Antagonist activity at rat mGluR5 expressed in HEK293A cells assessed as glutamate-induced calcium flux preincubated for 140 sec before glutamate challenge by calcium fluorescence assay F 7.87 pIC50 13.6 nM IC50 J Med Chem (2009) 52: 3563-3575 [PMID:19445453]
ChEMBL Antagonist activity at rat mGluR5 expressed in human HEK-293 cells assessed as inhibition of glutamate-induced intracellular calcium mobilization F 8.3 pIC50 5 nM IC50 Bioorg Med Chem Lett (2011) 21: 3243-3247 [PMID:21546249]
Monoamine oxidase A in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3681] [GtoPdb: 2489] [UniProtKB: Q64133]
ChEMBL Tested for in vitro antagonistic activity against Monoamine oxidase A F 4.52 pIC50 30000 nM IC50 J Med Chem (2003) 46: 204-206 [PMID:12519057]

ChEMBL data shown on this page come from version 32:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]