MPEP [Ligand Id: 1426] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL66654
  • GluN2B/Glutamate [NMDA] receptor subunit epsilon 2 in Human [ChEMBL: CHEMBL1904] [GtoPdb: 457] [UniProtKB: Q13224]
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  • Luciferin 4-monooxygenase in Photinus pyralis [ChEMBL: CHEMBL5567] [UniProtKB: P08659]
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  • 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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  • mGlu2 receptor/Metabotropic glutamate receptor 2 in Human [ChEMBL: CHEMBL5137] [GtoPdb: 290] [UniProtKB: Q14416]
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  • mGlu3 receptor/Metabotropic glutamate receptor 3 in Human [ChEMBL: CHEMBL2888] [GtoPdb: 291] [UniProtKB: Q14832]
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  • mGlu4 receptor/Metabotropic glutamate receptor 4 in Human [ChEMBL: CHEMBL2736] [GtoPdb: 292] [UniProtKB: Q14833]
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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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  • mGlu6 receptor/Metabotropic glutamate receptor 6 in Human [ChEMBL: CHEMBL4573] [GtoPdb: 294] [UniProtKB: O15303]
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  • mGlu7 receptor/Metabotropic glutamate receptor 7 in Human [ChEMBL: CHEMBL3777] [GtoPdb: 295] [UniProtKB: Q14831]
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  • mGlu8 receptor/Metabotropic glutamate receptor 8 in Human [ChEMBL: CHEMBL3228] [GtoPdb: 296] [UniProtKB: O00222]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
GluN2B/Glutamate [NMDA] receptor subunit epsilon 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1904] [GtoPdb: 457] [UniProtKB: Q13224]
ChEMBL Tested for in vitro antagonistic activity against human N-methyl-D-aspartate glutamate receptor 2B F 4.74 pIC50 18000 nM IC50 J Med Chem (2003) 46: 204-206 [PMID:12519057]
Luciferin 4-monooxygenase in Photinus pyralis (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5567] [UniProtKB: P08659]
ChEMBL Inhibition of Photinus pyralis luciferase by Steady-Glo reporter gene assay B 4 pIC50 >100000 nM IC50 J Med Chem (2008) 51: 2372-2386 [PMID:18363348]
ChEMBL Inhibition of Photinus pyralis luciferase by BrightGlo reporter gene assay B 4.52 pIC50 30000 nM IC50 J Med Chem (2008) 51: 2372-2386 [PMID:18363348]
ChEMBL Inhibition of Photinus pyralis luciferase by Easy lite assay B 5.13 pIC50 7400 nM IC50 J Med Chem (2008) 51: 2372-2386 [PMID:18363348]
ChEMBL Inhibition of Photinus pyralis luciferase by PK-Light assay B 5.18 pIC50 6600 nM IC50 J Med Chem (2008) 51: 2372-2386 [PMID:18363348]
ChEMBL Inhibition of Photinus pyralis luciferase B 5.33 pIC50 4700 nM IC50 J Med Chem (2008) 51: 2372-2386 [PMID:18363348]
mGlu1 receptor/Metabotropic glutamate receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3772] [GtoPdb: 289] [UniProtKB: Q13255]
ChEMBL Agonist potency against cloned human metabotropic glutamate receptor 1 F 4.52 pKi 30000 nM Ki J Med Chem (2000) 43: 2609-2645 [PMID:10893301]
ChEMBL Antagonist activity at human mGLUR1 F 7.44 pKi 36 nM Ki Bioorg Med Chem Lett (2010) 20: 4371-4375 [PMID:20615697]
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]
mGlu2 receptor/Metabotropic glutamate receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5137] [GtoPdb: 290] [UniProtKB: Q14416]
ChEMBL Antagonist potency against cloned Metabotropic glutamate receptor 2 F 4 pKi >100000 nM Ki J Med Chem (2000) 43: 2609-2645 [PMID:10893301]
mGlu3 receptor/Metabotropic glutamate receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2888] [GtoPdb: 291] [UniProtKB: Q14832]
ChEMBL Agonist potency against cloned Metabotropic glutamate receptor 3 (mGluR-3). F 4 pKi >100000 nM Ki J Med Chem (2000) 43: 2609-2645 [PMID:10893301]
mGlu4 receptor/Metabotropic glutamate receptor 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2736] [GtoPdb: 292] [UniProtKB: Q14833]
ChEMBL Agonist potency against cloned human Metabotropic glutamate receptor 4 (mGluR-4) F 4 pKi >100000 nM Ki J Med Chem (2000) 43: 2609-2645 [PMID:10893301]
GtoPdb - - 6.6 pEC50 260 nM EC50 Br J Pharmacol (2003) 138: 1026-30 [PMID:12684257]
mGlu5 receptor/Metabotropic glutamate receptor 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3227] [GtoPdb: 293] [UniProtKB: P41594]
ChEMBL Binding affinity to human mGluR5 expressed in HEK293 cell membranes expressing GLAST by scintillation counting B 8.07 pKd 8.6 nM Kd Bioorg Med Chem Lett (2012) 22: 6974-6979 [PMID:23046966]
ChEMBL Binding affinity to human mGluR5 B 7.44 pKi 36.31 nM Ki Bioorg Med Chem Lett (2010) 20: 3737-3741 [PMID:20483612]
ChEMBL Agonist potency against cloned metabotropic glutamate receptor 5 F 7.44 pKi 36 nM Ki J Med Chem (2000) 43: 2609-2645 [PMID:10893301]
ChEMBL Displacement of [3H]ABP688 from human mGluR5 receptor expressed in L (tk-) cells B 7.7 pKi 20 nM Ki Bioorg Med Chem (2007) 15: 903-914 [PMID:17110115]
ChEMBL Displacement of [3H]MPEP from cloned mGluR5 expressed in HEK293T cells by scintillation counting B 7.89 pKi 13 nM Ki J Med Chem (2009) 52: 3563-3575 [PMID:19445453]
ChEMBL Displacement of [3H]MPEP from human mGlu5 receptor expressed in CHO-TREx cell membranes after 60 mins by liquid scintillation spectrometric analysis B 7.98 pKi 10.4 nM Ki J Med Chem (2019) 62: 1246-1273 [PMID:30624919]
ChEMBL Displacement of [3H]MPEP from human cloned mGluR5 receptor expressed in CHO-T-Rex cells after 60 mins by liquid scintillation spectrometry B 7.98 pKi 10.4 nM Ki Bioorg Med Chem (2015) 23: 3040-3058 [PMID:26014480]
ChEMBL Displacement of [3H]-M-MPEP from mGluR5 StaR domain (569 to 836 residues) (unknown origin) expressed in HEK293 cell membranes B 8.46 pKi 3.5 nM Ki Bioorg Med Chem Lett (2016) 26: 484-494 [PMID:26706173]
ChEMBL Displacement of [3H]-ABP688 from human mGluR5 expressed in HEK293 cells after 60 mins by scintillation counting B 8.47 pKi 3.4 nM Ki Bioorg Med Chem Lett (2013) 23: 1398-1406 [PMID:23357634]
ChEMBL Antagonist activity against mGluR5 expressed in CHO cells assessed as inhibition of agonist-induced phosphoinositide hydrolysis F 7.41 pIC50 39 nM IC50 Bioorg Med Chem Lett (2006) 16: 3371-3375 [PMID:16678408]
ChEMBL Activity in agonist-induced phosphoinositide hydrolysis in CHO cells expressing mGluR5a F 7.41 pIC50 39 nM IC50 J Med Chem (2006) 49: 1080-1100 [PMID:16451073]
ChEMBL Negative allosteric modulation of recombinant human mGlu5a receptor assessed as inhibition of quisqualate-stimulated phosphoinositide hydrolysis by cell based assay B 7.44 pIC50 36 nM IC50 Eur J Med Chem (2017) 127: 567-576 [PMID:28109949]
ChEMBL In vitro for inhibitory activity of compound against recombinant Metabotropic glutamate receptor 5 evaluated as inhibition of quisqualate-stimulated phosphoinositide (PI) hydrolysis F 7.44 pIC50 36 nM IC50 Bioorg Med Chem Lett (2002) 12: 407-409 [PMID:11814808]
ChEMBL Compound was tested for it's antagonist activity against Ser152 and Thr175 (Metabotropic glutamate receptor 5) F 7.44 pIC50 36 nM IC50 J Med Chem (1999) 42: 5390-5401 [PMID:10639281]
ChEMBL Negative allosteric modulator activity against human mGluR5 expressed in HEK293 cells assessed as inhibition of glutamate-induced inositol phosphate accumulation by IP-one HTRF assay F 7.49 pIC50 32 nM IC50 Bioorg Med Chem Lett (2015) 25: 3135-3141 [PMID:26112438]
ChEMBL Negative allosteric modulation of human mGluR5a expressed in CHO cells assessed as reduction in DHPG-induced cytosolic Ca2+ influx after 10 to 20 mins by fluo-4/AM-dye based fluorometric analysis F 7.51 pIC50 31 nM IC50 J Med Chem (2017) 60: 2470-2484 [PMID:28212015]
ChEMBL Antagonist activity at mGluR5 by FLIPR F 7.54 pIC50 29 nM IC50 Bioorg Med Chem Lett (2007) 17: 1307-1311 [PMID:17196387]
ChEMBL Inhibition of glutamate-induced calcium influx in human mGluR5d by FLIPR F 7.66 pIC50 22 nM IC50 Bioorg Med Chem Lett (2006) 16: 2467-2469 [PMID:16481165]
ChEMBL Activity at human mGluR5 assessed as effect on glutamate-induced calcium ion mobilization by FLIPR F 7.66 pIC50 22 nM IC50 Bioorg Med Chem Lett (2006) 16: 4792-4795 [PMID:16839764]
ChEMBL Tested in vitro binding affinity for displacement of [3H]M-MPEP from membrane of L(-tk) cells expressing the Metabotropic glutamate receptor 5, activity expressed as IC50 B 7.7 pIC50 20 nM IC50 Bioorg Med Chem Lett (2002) 12: 407-409 [PMID:11814808]
GtoPdb - - 7.7 pIC50 - - - Bioorg Med Chem Lett (2002) 12: 407-9 [PMID:11814808];
Neuropharmacology (1999) 38: 1493-503 [PMID:10530811]
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 7.95 pIC50 11.2 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 7.95 pIC50 11.2 nM IC50 Bioorg Med Chem (2015) 23: 3040-3058 [PMID:26014480]
ChEMBL Binding affinity towards human mGlu5 receptors expressed in LtK-cells B 7.96 pIC50 11 nM IC50 Bioorg Med Chem Lett (2003) 13: 351-354 [PMID:12565928]
ChEMBL Antagonist activity at human mGluR5 expressed in CHO cells assessed as increase in intracellular calcium level by FLIPR F 8 pIC50 10 nM IC50 Bioorg Med Chem Lett (2008) 18: 1804-1809 [PMID:18304814]
ChEMBL Displacement of [3H]MPEP from mGlu5 receptor B 8.4 pIC50 4 nM IC50 Bioorg Med Chem Lett (2007) 17: 1307-1311 [PMID:17196387]
ChEMBL Antagonist activity at human mGluR5 expressed in HEK293 cells assessed as inhibition of Ca2+ mobilization by FLIPR assay F 8.64 pIC50 2.3 nM IC50 Bioorg Med Chem Lett (2013) 23: 1398-1406 [PMID:23357634]
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 8.7 pIC50 2 nM IC50 Bioorg Med Chem Lett (2003) 13: 351-354 [PMID:12565928]
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 8.7 pIC50 2 nM IC50 J Med Chem (2003) 46: 204-206 [PMID:12519057]
ChEMBL Antagonist activity at human mGluR5 receptor expressed in CHOK1 cells assessed as inhibition of glutamate-mediated internal calcium mobilization F 8.82 pIC50 1.5 nM IC50 J Med Chem (2007) 50: 3388-3391 [PMID:17569516]
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 rat brain membrane B 7.68 pKi 21 nM Ki Bioorg Med Chem Lett (2007) 17: 2074-2079 [PMID:17336520]
ChEMBL Displacement of [3H]MPEP from mGluR5 in rat brain membrane B 7.7 pKi 20 nM Ki Bioorg Med Chem Lett (2007) 17: 2987-2991 [PMID:17446071]
ChEMBL Displacement of [3H]ABP688 from mGluR5 in rat brain membrane B 7.72 pKi 19 nM Ki Bioorg Med Chem (2007) 15: 903-914 [PMID:17110115]
ChEMBL Displacement of [3H]methoxy-PEPY from rat mGluR5 expressed in human HEK-293 cells by liquid scintillation counting B 7.73 pKi 18.7 nM Ki Bioorg Med Chem Lett (2011) 21: 3243-3247 [PMID:21546249]
ChEMBL Displacement of [3H]MPEP from mGluR5 in Sprague-Dawley rat brain membrane after 60 mins by liquid scintillation counting B 7.79 pKi 16.3 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 7.82 pKi 15.3 nM Ki Bioorg Med Chem (2015) 23: 3040-3058 [PMID:26014480]
ChEMBL Displacement of [3H]-MPEP from rat mGluR5 B 7.89 pKi 13 nM Ki Bioorg Med Chem Lett (2011) 21: 2650-2654 [PMID:21295978]
ChEMBL Tested for displacement of [3H]3-methoxy-5-(pyridin-2-ylethynyl) pyridine from Metabotropic glutamate receptor 5 in rat cortical membrane B 7.92 pKi 12 nM Ki J Med Chem (2003) 46: 204-206 [PMID:12519057]
ChEMBL Displacement of [3H]M-MPEP from mGluR5 in Sprague-Dawley rat cerebrocortical membranes after 60 mins B 8.02 pKi 9.6 nM Ki J Med Chem (2017) 60: 2470-2484 [PMID:28212015]
ChEMBL Displacement of [3H]MPEP from mGlu5 receptor in rat brain B 8.24 pKi 5.7 nM Ki Bioorg Med Chem Lett (2007) 17: 4415-4418 [PMID:17590335]
ChEMBL Displacement of [3H]3methoxy-5-(pyridin-2-ylethynyl)pyridine from rat mGluR5 B 8.33 pKi 4.7 nM Ki Bioorg Med Chem Lett (2009) 19: 6623-6626 [PMID:19854049]
ChEMBL Displacement of [3H]3methoxy-5-(pyridin-2-ylethynyl)pyridine from rat mGluR5 B 8.33 pKi 4.7 nM Ki Bioorg Med Chem Lett (2009) 19: 6623-6626 [PMID:19854049]
ChEMBL Negative allosteric modulator activity at rat mGlu5 receptor expressed in HEK293 cells assessed as effect on quisqualate-induced inositol phosphate accumulation incubated for 30 mins by florescence assay F 7.05 pIC50 89 nM IC50 Medchemcomm (2014) 5: 1548-1554
ChEMBL Concentration required for 50% growth inhibition of rat metabotropic glutamate receptor 5 was determined using inositol phosphate hydrolysis assay B 7.44 pIC50 36 nM IC50 Bioorg Med Chem Lett (2005) 15: 945-949 [PMID:15686891]
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 7.51 pIC50 31 nM IC50 ACS Med Chem Lett (2012) 3: 544-549 [PMID:22924094]
ChEMBL Binding affinity towards mGlu5 receptors in rat brain membranes was evaluated B 7.7 pIC50 20 nM IC50 Bioorg Med Chem Lett (2003) 13: 351-354 [PMID:12565928]
ChEMBL Inhibition of [3H]MPEP binding to mGluR5 in rat brain membrane B 7.89 pIC50 13 nM IC50 Bioorg Med Chem Lett (2006) 16: 3371-3375 [PMID:16678408]
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 8.45 pIC50 3.54 nM IC50 J Med Chem (2009) 52: 3563-3575 [PMID:19445453]
ChEMBL Antagonist activity at rat mGluR5 expressed in HEK293T cells assessed as inhibition of glutamate-induced calcium flux by calcium fluorescence assay F 8.45 pIC50 3.54 nM IC50 Bioorg Med Chem Lett (2011) 21: 2650-2654 [PMID:21295978]
ChEMBL Antagonist activity at rat mGluR5 expressed in human HEK-293 cells assessed as inhibition of glutamate-induced intracellular calcium mobilization F 8.53 pIC50 2.93 nM IC50 Bioorg Med Chem Lett (2011) 21: 3243-3247 [PMID:21546249]
ChEMBL Activity at rat mGlu5 receptor expressed in CHO cells assessed as inhibition of quisqualate-stimulated calcium mobilization by FLIPR assay F 9.7 pIC50 0.2 nM IC50 Bioorg Med Chem Lett (2007) 17: 4415-4418 [PMID:17590335]
mGlu6 receptor/Metabotropic glutamate receptor 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4573] [GtoPdb: 294] [UniProtKB: O15303]
ChEMBL Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6). F 5 pKi >10000 nM Ki J Med Chem (2000) 43: 2609-2645 [PMID:10893301]
mGlu7 receptor/Metabotropic glutamate receptor 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3777] [GtoPdb: 295] [UniProtKB: Q14831]
ChEMBL Agonist potency against cloned Metabotropic glutamate receptor 7 (mGluR-7). F 4 pKi >100000 nM Ki J Med Chem (2000) 43: 2609-2645 [PMID:10893301]
mGlu8 receptor/Metabotropic glutamate receptor 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3228] [GtoPdb: 296] [UniProtKB: O00222]
ChEMBL Agonist potency against cloned Metabotropic glutamate receptor 8 (mGluR-8). F 4 pKi >100000 nM Ki J Med Chem (2000) 43: 2609-2645 [PMID:10893301]
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 F 5.1 pIC50 8000 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]