eglumegad [Ligand Id: 1393] 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: CHEMBL8759 (Eglumegad, Eglumetad, Eglumetad anhydrous, LY354740, LY-354740)
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!
  • mGlu1 receptor/Metabotropic glutamate receptor 1 in Human [ChEMBL: CHEMBL3772] [GtoPdb: 289] [UniProtKB: Q13255]
There should be some charts here, you may need to enable JavaScript!
  • mGlu2 receptor/Metabotropic glutamate receptor 2 in Human [ChEMBL: CHEMBL5137] [GtoPdb: 290] [UniProtKB: Q14416]
  • mGlu2 receptor/Metabotropic glutamate receptor 2 in Rat [ChEMBL: CHEMBL2851] [GtoPdb: 290] [UniProtKB: P31421]
There should be some charts here, you may need to enable JavaScript!
  • mGlu3 receptor/Metabotropic glutamate receptor 3 in Human [ChEMBL: CHEMBL2888] [GtoPdb: 291] [UniProtKB: Q14832]
  • mGlu3 receptor/Metabotropic glutamate receptor 3 in Rat [ChEMBL: CHEMBL3067] [GtoPdb: 291] [UniProtKB: P31422]
There should be some charts here, you may need to enable JavaScript!
  • mGlu4 receptor/Metabotropic glutamate receptor 4 in Human [ChEMBL: CHEMBL2736] [GtoPdb: 292] [UniProtKB: Q14833]
  • mGlu4 receptor/Metabotropic glutamate receptor 4 in Rat [ChEMBL: CHEMBL2787] [GtoPdb: 292] [UniProtKB: P31423]
There should be some charts here, you may need to enable JavaScript!
  • mGlu5 receptor/Metabotropic glutamate receptor 5 in Human [ChEMBL: CHEMBL3227] [GtoPdb: 293] [UniProtKB: P41594]
There should be some charts here, you may need to enable JavaScript!
  • mGlu6 receptor/Metabotropic glutamate receptor 6 in Human [ChEMBL: CHEMBL4573] [GtoPdb: 294] [UniProtKB: O15303]
There should be some charts here, you may need to enable JavaScript!
  • mGlu7 receptor/Metabotropic glutamate receptor 7 in Human [ChEMBL: CHEMBL3777] [GtoPdb: 295] [UniProtKB: Q14831]
There should be some charts here, you may need to enable JavaScript!
  • mGlu8 receptor/Metabotropic glutamate receptor 8 in Human [ChEMBL: CHEMBL3228] [GtoPdb: 296] [UniProtKB: O00222]
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
GluN1/GluN2A/GluN2B/GluN2C/GluN2D/GluN3B/GluN3A/Glutamate NMDA receptor in Rat (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL1907608] [GtoPdb: 455456457458459461460] [UniProtKB: P35439Q00959Q00960Q00961Q62645Q8VHN2Q9R1M7]
ChEMBL Inhibitory concentration against radioligand [3H]CGS-19,755 binding to N-methyl-D-aspartate glutamate receptor in rat forebrain membranes B 4 pIC50 >100000 nM IC50 J Med Chem (1997) 40: 528-537 [PMID:9046344]
ChEMBL Inhibitory concentration against radioligand [3H]CGS-19,755 binding to N-methyl-D-aspartate glutamate receptor in rat forebrain membranes B 4 pIC50 >100000 nM IC50 J Med Chem (1997) 40: 528-537 [PMID:9046344]
ChEMBL Inhibitory concentration against radioligand [3H]CGS-19,755 binding to N-methyl-D-aspartate glutamate receptor in rat forebrain membranes B 4 pIC50 >100000 nM IC50 J Med Chem (1997) 40: 528-537 [PMID:9046344]
GluA1/GluA2/GluA3/GluA4/Glutamate receptor ionotropic, AMPA in Rat (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2093871] [GtoPdb: 444445446447] [UniProtKB: P19490P19491P19492P19493]
ChEMBL Inhibitory concentration against radioligand [3H]AMPA binding to Ionotropic glutamate receptor AMPA in rat forebrain membranes B 4 pIC50 >100000 nM IC50 J Med Chem (1997) 40: 528-537 [PMID:9046344]
ChEMBL Inhibitory concentration against radioligand [3H]AMPA binding to Ionotropic glutamate receptor AMPA in rat forebrain membranes B 4 pIC50 >100000 nM IC50 J Med Chem (1997) 40: 528-537 [PMID:9046344]
ChEMBL Inhibitory concentration against radioligand [3H]AMPA binding to Ionotropic glutamate receptor AMPA in rat forebrain membranes B 4 pIC50 >100000 nM IC50 J Med Chem (1997) 40: 528-537 [PMID:9046344]
ChEMBL Binding affinity against Ionotropic glutamate receptor AMPA using [3H]AMPA as radioligand. B 4 pIC50 >100000 nM IC50 J Med Chem (1999) 42: 1027-1040 [PMID:10090786]
GluK1/GluK2/GluK3/GluK4/GluK5/Glutamate receptor ionotropic, kainate in Rat (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2094119] [GtoPdb: 450451452453454] [UniProtKB: P22756P42260P42264Q01812Q63273]
ChEMBL Inhibitory concentration against radioligand [3H]-Kainate binding to Ionotropic glutamate receptor kainate in rat forebrain membranes B 4 pIC50 >100000 nM IC50 J Med Chem (1997) 40: 528-537 [PMID:9046344]
ChEMBL Inhibitory concentration against radioligand [3H]-Kainate binding to Ionotropic glutamate receptor kainate in rat forebrain membranes B 4 pIC50 >100000 nM IC50 J Med Chem (1997) 40: 528-537 [PMID:9046344]
ChEMBL Inhibitory concentration against radioligand [3H]-Kainate binding to Ionotropic glutamate receptor kainate in rat forebrain membranes B 4 pIC50 >100000 nM IC50 J Med Chem (1997) 40: 528-537 [PMID:9046344]
ChEMBL Ability to displace [3H]-KA binding to Ionotropic glutamate receptor kainate from rat forebrain B 4 pIC50 >100000 nM IC50 J Med Chem (1999) 42: 1027-1040 [PMID:10090786]
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 pKi >100000 nM Ki J Med Chem (2000) 43: 2609-2645 [PMID:10893301]
ChEMBL Inhibition of forskolin stimulated cAMP production in RGT cells expressing recombinant human mGluR1a F 4 pEC50 >100000 nM EC50 J Med Chem (1999) 42: 1027-1040 [PMID:10090786]
mGlu2 receptor/Metabotropic glutamate receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5137] [GtoPdb: 290] [UniProtKB: Q14416]
GtoPdb - - 6.9 pKi - - - Neuropharmacology (1999) 38: 1519-29 [PMID:10530814]
ChEMBL Inhibition of [3H]LY-341,495 binding to recombinant human mGlu2 receptors B 7.07 pKi 84.7 nM Ki J Med Chem (2005) 48: 5305-5320 [PMID:16078848]
ChEMBL Displacement of [3H]LY341495 from human recombinant mGluR2 in RGT cells B 7.13 pKi 74.9 nM Ki J Med Chem (2007) 50: 233-240 [PMID:17228865]
ChEMBL Ability to displace [3H]LY-341,495 from recombinant human Metabotropic glutamate receptor 2 subtypes expressed in RGT cells. B 7.13 pKi 74.9 nM Ki J Med Chem (1999) 42: 1027-1040 [PMID:10090786]
ChEMBL Displacement of [3H]-341495 binding to membranes expressing recombinant human Metabotropic glutamate receptor 2 B 7.13 pKi 74 nM Ki J Med Chem (2005) 48: 3605-3612 [PMID:15887967]
ChEMBL Displacement of [3H]-459477 from human recombinant mGlu2 receptor expressed in AV12 cells after 90 mins by liquid scintillation counting B 7.14 pKi 71.7 nM Ki J Med Chem (2015) 58: 7526-7548 [PMID:26313429]
ChEMBL Displacement of [3H]-LY459477 from recombinant human mGlu2 receptor expressed in HEK cell membranes after 90 mins by liquid scintillation counting B 7.14 pKi 71.7 nM Ki J Med Chem (2018) 61: 2303-2328 [PMID:29350927]
ChEMBL Binding affinity at Metabotropic glutamate receptor 2 B 7.89 pKi 13 nM Ki J Med Chem (2002) 45: 3171-3183 [PMID:12109902]
ChEMBL Agonist potency against cloned Metabotropic glutamate receptor 2 (mGluR-2). F 7.96 pKi 11 nM Ki J Med Chem (2000) 43: 2609-2645 [PMID:10893301]
ChEMBL Agonist activity at mGlu2 (unknown origin) B 8.15 pIC50 7 nM IC50 J Med Chem (2016) 59: 10974-10993 [PMID:28002967]
ChEMBL Antagonist activity at human mGlu2 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 assessed as inhibition of forskolin-stimulated cAMP production after 20 mins by HTRF assay F 8.25 pIC50 5.6 nM IC50 J Med Chem (2013) 56: 4442-4455 [PMID:23675965]
ChEMBL Agonist activity at human recombinant mGlu2 receptor expressed in AV12 cells assessed as stimulation of Ca2+ mobilization after 1 hr by FLIPR assay F 7.46 pEC50 34.4 nM EC50 J Med Chem (2015) 58: 7526-7548 [PMID:26313429]
ChEMBL Inhibition of forskolin stimulated cAMP production in RGT cells expressing recombinant human Metabotropic glutamate receptor 2 F 7.95 pEC50 11.1 nM EC50 J Med Chem (1999) 42: 1027-1040 [PMID:10090786]
ChEMBL Agonist activity at human mGluR2 assessed as effect on cAMP production in RGT cells F 7.95 pEC50 11.1 nM EC50 J Med Chem (2007) 50: 233-240 [PMID:17228865]
ChEMBL Evaluation of the functional effect on cAMP responses in RGT cells expressing human mGlu2 receptor F 8 pEC50 10 nM EC50 J Med Chem (2005) 48: 3605-3612 [PMID:15887967]
ChEMBL Agonist activity at human mGlu2 receptor expressed in HEK cells assessed as inhibition of forskolin-stimulated cAMP formation after 20 mins by HTRF assay F 8.15 pEC50 7 nM EC50 J Med Chem (2018) 61: 2303-2328 [PMID:29350927]
ChEMBL Agonist activity at human recombinant mGlu2 receptor expressed in AV12 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 hr by fluorescence assay F 8.15 pEC50 7 nM EC50 J Med Chem (2015) 58: 7526-7548 [PMID:26313429]
ChEMBL Compound was evaluated for agonist activity against human mGluR2 F 8.29 pEC50 5.1 nM EC50 Bioorg Med Chem Lett (1998) 8: 925-930 [PMID:9871513]
ChEMBL Agonistic activity against Human Metabotropic glutamate receptor 2 F 8.29 pEC50 5.1 nM EC50 J Med Chem (1998) 41: 1641-1650 [PMID:9572889]
mGlu2 receptor/Metabotropic glutamate receptor 2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2851] [GtoPdb: 290] [UniProtKB: P31421]
ChEMBL Tested for binding affinity against Metabotropic glutamate receptor 2 in CHO cells using [3H]-7 as radioligand B 7.63 pKi 23.4 nM Ki J Med Chem (2000) 43: 4893-4909 [PMID:11123999]
GtoPdb - - 7.9 pKi - - - Br J Pharmacol (1998) 123: 497-504 [PMID:9504391];
Neuropharmacology (2000) 39: 1700-6 [PMID:10884552]
ChEMBL Tested for the agonistic activity against Metabotropic glutamate receptor 2 F 7.46 pEC50 35 nM EC50 Bioorg Med Chem Lett (1997) 7: 601-606
ChEMBL Agonist activity against Metabotropic glutamate receptor 2 expressed in CHO cells was evaluated by measuring forskolin-induced cyclic AMP formation F 7.74 pEC50 18.3 nM EC50 J Med Chem (2000) 43: 4893-4909 [PMID:11123999]
mGlu3 receptor/Metabotropic glutamate receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2888] [GtoPdb: 291] [UniProtKB: Q14832]
ChEMBL Inhibition of [3H]LY-341,495 binding to recombinant human mGlu3 receptors B 6.9 pKi 125.6 nM Ki J Med Chem (2005) 48: 5305-5320 [PMID:16078848]
ChEMBL Displacement of [3H]-459477 from human recombinant mGlu3 receptor expressed in AV12 cells after 90 mins by liquid scintillation counting B 6.97 pKi 107 nM Ki J Med Chem (2015) 58: 7526-7548 [PMID:26313429]
ChEMBL Displacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in HEK cell membranes after 90 mins by liquid scintillation counting B 6.97 pKi 107 nM Ki J Med Chem (2018) 61: 2303-2328 [PMID:29350927]
ChEMBL Ability to displace [3H]LY-341,495 from recombinant human Metabotropic glutamate receptor 3 expressed in RGT cells. B 7.03 pKi 93.3 nM Ki J Med Chem (1999) 42: 1027-1040 [PMID:10090786]
ChEMBL Displacement of [3H]LY341495 from human recombinant mGluR3 in RGT cells B 7.03 pKi 93.3 nM Ki J Med Chem (2007) 50: 233-240 [PMID:17228865]
ChEMBL Displacement of [3H]-341495 binding to membranes expressing recombinant human Metabotropic glutamate receptor 3 B 7.03 pKi 93 nM Ki J Med Chem (2005) 48: 3605-3612 [PMID:15887967]
ChEMBL Agonist potency against cloned Metabotropic glutamate receptor 3 (mGluR-3). F 7.42 pKi 38 nM Ki J Med Chem (2000) 43: 2609-2645 [PMID:10893301]
GtoPdb - - 8.9 pKi - - - Neuropharmacology (1999) 38: 1519-29 [PMID:10530814]
ChEMBL Agonist activity at mGlu3 (unknown origin) B 7.55 pIC50 27.9 nM IC50 J Med Chem (2016) 59: 10974-10993 [PMID:28002967]
ChEMBL Agonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as stimulation of Ca2+ mobilization after 1.5 hrs by FLIPR assay F 6.85 pEC50 140 nM EC50 J Med Chem (2015) 58: 7526-7548 [PMID:26313429]
ChEMBL Inhibition of forskolin stimulated cAMP production in RGT cells expressing recombinant human Metabotropic glutamate receptor 3 F 7.42 pEC50 38 nM EC50 J Med Chem (1999) 42: 1027-1040 [PMID:10090786]
ChEMBL Evaluation of the functional effect on cAMP responses in RGT cells expressing human mGlu3 receptor F 7.42 pEC50 38 nM EC50 J Med Chem (2005) 48: 3605-3612 [PMID:15887967]
ChEMBL Agonist activity at human mGluR3 assessed as effect on cAMP production in RGT cells F 7.42 pEC50 38 nM EC50 J Med Chem (2007) 50: 233-240 [PMID:17228865]
ChEMBL Agonist activity at human mGlu3 receptor expressed in HEK cells assessed as inhibition of forskolin-stimulated cAMP formation after 20 mins by HTRF assay F 7.55 pEC50 27.9 nM EC50 J Med Chem (2018) 61: 2303-2328 [PMID:29350927]
ChEMBL Agonist activity at human recombinant mGlu3 receptor expressed in AV12 cells assessed as inhibition of forskolin-stimulated cAMP production after 1 hr by fluorescence assay F 7.55 pEC50 27.9 nM EC50 J Med Chem (2015) 58: 7526-7548 [PMID:26313429]
ChEMBL Agonist activity at human mGlu3 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by HTRF assay B 7.57 pEC50 27.1 nM EC50 J Med Chem (2013) 56: 4442-4455 [PMID:23675965]
ChEMBL Agonistic activity against Human Metabotropic glutamate receptor 3 F 7.61 pEC50 24.3 nM EC50 J Med Chem (1998) 41: 1641-1650 [PMID:9572889]
mGlu3 receptor/Metabotropic glutamate receptor 3 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3067] [GtoPdb: 291] [UniProtKB: P31422]
ChEMBL Tested for binding affinity against Metabotropic glutamate receptor 3 in CHO cells using [3H]-7 as radioligand B 7.27 pKi 53.5 nM Ki J Med Chem (2000) 43: 4893-4909 [PMID:11123999]
GtoPdb - - 7.3 pKi - - - Neuropharmacology (2000) 39: 1700-6 [PMID:10884552]
ChEMBL Agonist potency against cloned Metabotropic glutamate receptor 3 F 7.2 pEC50 62.8 nM EC50 J Med Chem (2000) 43: 4893-4909 [PMID:11123999]
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]
ChEMBL Inhibition of forskolin stimulated cAMP production in RGT cells expressing recombinant human mGluR4a F 4 pEC50 >100000 nM EC50 J Med Chem (1999) 42: 1027-1040 [PMID:10090786]
mGlu4 receptor/Metabotropic glutamate receptor 4 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2787] [GtoPdb: 292] [UniProtKB: P31423]
ChEMBL Stimulation of [3H]phosphatidylinositol accumulation by rat Metabotropic glutamate receptor 4 co-expressed with Gqi9 protein in HEK 293 cells; Inactive F 4 pEC50 >100000 nM EC50 J Med Chem (2005) 48: 2534-2547 [PMID:15801843]
mGlu5 receptor/Metabotropic glutamate receptor 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3227] [GtoPdb: 293] [UniProtKB: P41594]
ChEMBL Agonist potency against cloned metabotropic glutamate receptor 5 F 4 pKi >100000 nM Ki J Med Chem (2000) 43: 2609-2645 [PMID:10893301]
ChEMBL Inhibition of forskolin stimulated cAMP production in RGT cells expressing recombinant human mGluR5a F 4 pEC50 >100000 nM EC50 J Med Chem (1999) 42: 1027-1040 [PMID:10090786]
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 5.52 pKi 3000 nM Ki J Med Chem (2000) 43: 2609-2645 [PMID:10893301]
GtoPdb - - 5.5 pIC50 - - - J Med Chem (1999) 42: 1027-40 [PMID:10090786]
ChEMBL Agonist activity at human mGlu6 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay B 5.47 pEC50 3360 nM EC50 J Med Chem (2013) 56: 4442-4455 [PMID:23675965]
ChEMBL Inhibition of forskolin stimulated cAMP production in RGT cells expressing recombinant human mGluR6 F 5.52 pEC50 2990 nM EC50 J Med Chem (1999) 42: 1027-1040 [PMID:10090786]
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]
ChEMBL Inhibition of forskolin stimulated cAMP production in RGT cells expressing recombinant human mGluR7 F 4 pEC50 >100000 nM EC50 J Med Chem (1999) 42: 1027-1040 [PMID:10090786]
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 4.92 pKi 12000 nM Ki J Med Chem (2000) 43: 2609-2645 [PMID:10893301]
ChEMBL Agonist activity at human mGlu8 receptor expressed in golden Syrian hamster AV12 cells coexpressing EAAT1 after 20 mins by FLIPR assay B 4.6 pEC50 >25000 nM EC50 J Med Chem (2013) 56: 4442-4455 [PMID:23675965]
ChEMBL Inhibition of forskolin stimulated cAMP production in RGT cells expressing recombinant human mGluR8 F 4.94 pEC50 11500 nM EC50 J Med Chem (1999) 42: 1027-1040 [PMID:10090786]
ChEMBL Agonist activity at human mGluR8 assessed as effect on cAMP production in RGT cells F 4.94 pEC50 11470 nM EC50 J Med Chem (2007) 50: 233-240 [PMID:17228865]
GtoPdb - - 5.1 pEC50 - - - Brain Res Mol Brain Res (1999) 67: 201-10 [PMID:10216218]

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]