MPEP [Ligand Id: 1426] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL66654 |
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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 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]
