MTEP [Ligand Id: 3336] activity data from GtoPdb and ChEMBL
Click here for a description of the charts and data table
Please tell us if you are using this feature and what you think!
| ChEMBL ligand: CHEMBL292065 (MTEP) |
|---|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
| 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 33:
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]
