eglumegad [Ligand Id: 1393] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL8759 (Eglumegad, Eglumetad, Eglumetad anhydrous, LY354740, LY-354740) |
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| 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: 455, 456, 457, 458, 459, 461, 460] [UniProtKB: P35439, Q00959, Q00960, Q00961, Q62645, Q8VHN2, Q9R1M7] | ||||||||
| 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: 444, 445, 446, 447] [UniProtKB: P19490, P19491, P19492, P19493] | ||||||||
| 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: 450, 451, 452, 453, 454] [UniProtKB: P22756, P42260, P42264, Q01812, Q63273] | ||||||||
| 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 31:
Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]
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