MPEP [Ligand Id: 1426] 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: CHEMBL66654 |
|---|
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!
|
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!
|
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!
|
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 |
|---|---|---|---|---|---|---|---|---|
| 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] |
| histone deacetylase 6/Histone deacetylase 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1865] [GtoPdb: 2618] [UniProtKB: Q9UBN7] | ||||||||
| ChEMBL | Determination of IC50 values for inhibition of enzymatic assay of human HDAC6 with custom peptide substrate | B | 6.32 | pIC50 | 475.8 | nM | IC50 | HDAC6 screening dataset using tau-based substrate in an enzymatic assay yields selective inhibitors and activators |
| 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 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]
