ChEMBL ligand: CHEMBL8759 (Eglumegad, 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 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]