ChEMBL ligand: CHEMBL8759 (Eglumetad, Eglumetad anhydrous, LY-354740, LY354740)
GluN1/GluN2A/GluN2B/GluN2C/GluN2D/GluN3B/GluN3A/Glutamate NMDA receptor in Rat [ChEMBL: CHEMBL1907608] [GtoPdb: 455, 456, 457, 458, 459, 461, 460] [UniProtKB: P35439, Q00959, Q00960, Q00961, Q62645, Q8VHN2, Q9R1M7] There should be some charts here, you may need to enable JavaScript!
GluA1/GluA2/GluA3/GluA4/Glutamate receptor ionotropic, AMPA in Rat [ChEMBL: CHEMBL2093871] [GtoPdb: 444, 445, 446, 447] [UniProtKB: P19490, P19491, P19492, P19493] There should be some charts here, you may need to enable JavaScript!
GluK1/GluK2/GluK3/GluK4/GluK5/Glutamate receptor ionotropic, kainate in Rat [ChEMBL: CHEMBL2094119] [GtoPdb: 450, 451, 452, 453, 454] [UniProtKB: P22756, P42260, P42264, Q01812, Q63273] 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: 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]
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]
GtoPdb	-	-	7.7	pKd	-	-	-	Neuropharmacology (2000) 39: 1700-6 [PMID:10884552]
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]
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]
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]
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]
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]

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]