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ChEMBL ligand: CHEMBL292065 (MTEP) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]